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Sample records for lidocaine anesthetic activity

  1. Synthesis and antispasmodic activity of lidocaine derivatives endowed with reduced local anesthetic action.

    Science.gov (United States)

    Costa, Jorge C S; Neves, Josiane S; de Souza, Marcus V N; Siqueira, Rodrigo A; Romeiro, Nelilma C; Boechat, Nubia; e Silva, Patrícia M R; Martins, Marco A

    2008-02-01

    The present structure-activity relationship (SAR) study focused on chemical modifications of the structure of the local anesthetic lidocaine, and indicated analogues having reduced anesthetic potency, but with superior potency relative to the prototype in preventing anaphylactic or histamine-evoked ileum contraction. From the SAR analysis, 2-(diethylamino)-N-(trifluoromethyl-phenyl) and 2-(diethylamino)-N-(dimethyl-phenyl) acetamides were selected as the most promising compounds. New insights into the applicability of non-anesthetic lidocaine derivatives as templates in drug discovery for allergic syndromes are provided.

  2. Endothelial Barrier Protection by Local Anesthetics: Ropivacaine and Lidocaine Block Tumor Necrosis Factor-α–induced Endothelial Cell Src Activation

    Science.gov (United States)

    Piegeler, Tobias; Votta-Velis, E. Gina; Bakhshi, Farnaz R.; Mao, Mao; Carnegie, Graeme; Bonini, Marcelo G.; Schwartz, David E.; Borgeat, Alain; Beck-Schimmer, Beatrice; Minshall, Richard D.

    2014-01-01

    Background Pulmonary endothelial barrier dysfunction mediated in part by Src-kinase activation plays a crucial role in acute inflammatory disease. Proinflammatory cytokines, such as tumor necrosis factor-α (TNFα), activate Src via phosphatidylinositide 3-kinase/Akt-dependent nitric oxide generation, a process initiated by recruitment of phosphatidylinositide 3-kinase regulatory subunit p85 to TNF-receptor-1. Because amide-linked local anesthetics have well-established anti-inflammatory effects, the authors hypothesized that ropivacaine and lidocaine attenuate inflammatory Src signaling by disrupting the phosphatidylinositide 3-kinase–Akt–nitric oxide pathway, thus blocking Src-dependent neutrophil adhesion and endothelial hyperpermeability. Methods Human lung microvascular endothelial cells, incubated with TNFα in the absence or presence of clinically relevant concentrations of ropivacaine and lidocaine, were analyzed by Western blot, probing for phosphorylated/activated Src, endothelial nitric oxide synthase, Akt, intercellular adhesion molecule-1, and caveolin-1. The effect of ropivacaine on TNFα-induced nitric oxide generation, co-immunoprecipitation of TNF-receptor-1 with p85, neutrophil adhesion, and endothelial barrier disruption were assessed. Results Ropivacaine and lidocaine attenuated TNFα-induced Src activation (half-maximal inhibitory concentration [IC50] = 8.611 × 10−10 M for ropivacaine; IC50 = 5.864 × 10−10 M for lidocaine) and endothelial nitric oxide synthase phosphorylation (IC50 = 7.572 × 10−10 M for ropivacaine; IC50 = 6.377 × 10−10 M for lidocaine). Akt activation (n = 7; P = 0.006) and stimulus-dependent binding of TNF-receptor-1 and p85 (n = 6; P = 0.043) were blocked by 1 nM of ropivacaine. TNFα-induced neutrophil adhesion and disruption of endothelial monolayers via Src-dependent intercellular adhesion molecule-1- and caveolin-1-phosphorylation, respectively, were also attenuated. Conclusions Ropivacaine and lidocaine

  3. Bupivacaine Lozenge Compared with Lidocaine Spray as Topical Pharyngeal Anesthetic before Unsedated Upper Gastrointestinal Endoscopy

    DEFF Research Database (Denmark)

    Salale, Nesrin; Treldal, Charlotte; Mogensen, Stine;

    2014-01-01

    Unsedated upper gastrointestinal endoscopy (UGE) can induce patient discomfort, mainly due to a strong gag reflex. The aim was to assess the effect of a bupivacaine lozenge as topical pharyngeal anesthetic compared with standard treatment with a lidocaine spray before UGE. Ninety-nine adult...... with a lidocaine spray proved to be a superior option as topical pharyngeal anesthetic before an UGE....

  4. Improvement of Lidocaine Local Anesthetic Action Using Lallemantia royleana Seed Mucilage as an Excipient.

    Science.gov (United States)

    Atabaki, Rabi; Hassanpour-Ezatti, Majid

    2014-01-01

    Lallemantia royleana (Balangu) is a well known Iranian medicinal plant that its seed mucilage has many applications in modern pharmacology. Plant mucilage traditionally was used as a gel supplement, and natural matrix for sustained release of drugs. But it seems that these compounds are not a simple additive and also have many undiscovered pharmacological properties. In this research, the anesthetic action of gel prepared from Balangu mucilage alone and its mixture with lidocaine hydrochloride are compared with the effect of commercial 2% lidocaine gel by rat tail flick test. Mucilage of Balangu seed alone showed analgesic effect. Duration and potency of anesthesia induced by gel containing mucilage alone (0.01 g/mL) were identical to commercial 2% lidocaine gel. But, local anesthetic potency and duration of gel made from 2% lidocaine-mucilage gel mixture was significantly higher than commercial 2% lidocaine gel. The gel prepared from mucilage causes a good analgesia with unknown mechanism. Besides, mixture of Balangu mucilage prepared gel with lidocaine improves lidocaine anesthesia. The increase in potency of lidocaine action results from mucilage dermal penetration enhancing effects; and longer anesthetic duration of this mixture are related to the capability of mucilage based gel for sustained drug release.

  5. Plasma concentration and cardiovascular effects of lidocaine during continuous epidural administration in dogs anesthetized with isoflurane.

    Science.gov (United States)

    Sakonju, Iwao; Maeda, Kenichi; Karasawa, Koichi; Tadokoro, Toshiyuki; Kakuta, Tomoko; Takase, Katsuaki

    2011-03-01

    The cardiovascular effects of continuous epidural administration (CEA) of lidocaine were investigated in anesthetized dogs. Loading epidural injections of 2, 4, or 6 mg/kg of lidocaine were followed by CEA with 1, 2, or 3 mg/kg/hr lidocaine, respectively, for 2 hr under 2.0% isoflurane anesthesia. Heart rate, direct blood pressure, cardiac index, and stroke volume decreased dose-dependently during CEA, whereas systemic vascular resistance did not significantly differ with dose, and no characteristic changes were observed in any groups. Plasma lidocaine concentration reached a steady state during CEA and increased in a dose-dependent manner. Circulatory suppression caused by lidocaine CEA was not attributable to peripheral vasodilation, but rather to the direct cardiac action of systemic lidocaine absorption from the peridural space.

  6. The relation between the duty cycle and anesthetic effect in lidocaine iontophoresis using alternating current.

    Science.gov (United States)

    Wakita, Ryo; Nakajima, Atsushi; Haida, Yu; Umino, Masahiro; Fukayama, Haruhisa

    2011-01-01

    We assessed the effect of the duty cycle on the anesthetic effect during lidocaine alternating current (AC) iontophoresis. A solution of 2% lidocaine was delivered to the medial antecubital skin for 20 minutes using AC iontophoresis with a duty cycle of 60%, 70%, or 80%. The von Frey test was then performed to evaluate the anesthetic effect. In the groups treated with a duty cycle of 80% or 70% the touch thresholds (TT) were significantly elevated from 0 minutes to 30 minutes and from 0 minutes to 20 minutes. TT were significantly elevated at 0 minutes in the group treated with a 60% duty cycle. The anesthetic effect was significantly enhanced in a duty cycle-dependent manner.

  7. A comparison of the anesthetic efficacy of articaine and lidocaine in patients with irreversible pulpitis.

    Science.gov (United States)

    Tortamano, Isabel Peixoto; Siviero, Marcelo; Costa, Carina Gisele; Buscariolo, Inês Aparecida; Armonia, Paschoal Laércio

    2009-02-01

    The purpose of the present study was to compare the anesthetic efficacy of 4% articaine with 1:100,000 epinephrine with that of 2% lidocaine with 1:100,000 epinephrine during pulpectomy in patients with irreversible pulpitis in mandibular posterior teeth. Forty volunteers, patients with irreversible pulpitis admitted to the Emergency Center of the School of Dentistry at the University of São Paulo, randomly received a conventional inferior alveolar nerve block containing 3.6 mL of either 4% articaine with 1:100,000 epinephrine or 2% lidocaine with 1:100,000 epinephrine. During the subsequent pulpectomy, we recorded the patients' subjective assessments of lip anesthesia, the absence/presence of pulpal anesthesia through electric pulp stimulation, and the absence/presence of pain through a verbal analogue scale. All tested patients reported lip anesthesia after the application of either inferior alveolar nerve block. Regarding pulpal anesthesia success as measured with the pulp tester, the lidocaine solution had a higher success rate (70%) than the articaine solution (65%). For patients reporting none or mild pain during pulpectomy, the success rate of the articaine solution (65%) was higher than that of the lidocaine solution (45%). Yet, none of the observed differences between articaine and lidocaine were statistically significant. Apparently, therefore, both local anesthetic solutions had similar effects on the patients with irreversible pulpitis in mandibular posterior teeth. Neither of the solutions, however, resulted in an effective pain control during irreversible pulpitis treatments.

  8. Improvement of Lidocaine Local Anesthetic Action Using Lallemantia royleana Seed Mucilage as an Excipient

    OpenAIRE

    Atabaki, Rabi; Hassanpour-Ezatti, Majid

    2014-01-01

    Lallemantia royleana (Balangu) is a well known Iranian medicinal plant that its seed mucilage has many applications in modern pharmacology. Plant mucilage traditionally was used as a gel supplement, and natural matrix for sustained release of drugs. But it seems that these compounds are not a simple additive and also have many undiscovered pharmacological properties. In this research, the anesthetic action of gel prepared from Balangu mucilage alone and its mixture with lidocaine hydrochlorid...

  9. Methemoglobin levels in generally anesthetized pediatric dental patients receiving prilocaine versus lidocaine.

    Science.gov (United States)

    Gutenberg, Lauren L; Chen, Jung-Wei; Trapp, Larry

    2013-01-01

    The purpose of this study was to measure and compare peak methemoglobin levels and times to peak methemoglobin levels following the use of prilocaine and lidocaine in precooperative children undergoing comprehensive dental rehabilitation under general anesthesia. Ninety children, 3-6 years of age, undergoing dental rehabilitation under general anesthesia were enrolled and randomly assigned into 3 equal groups: group 1, 4% prilocaine plain, 5 mg/kg; group 2, 2% lidocaine with 1:100,000 epinephrine, 2.5 mg/kg; and group 3, no local anesthetic. Subjects in groups 1 and 2 were administered local anesthetic prior to restorative dental treatment. Methemoglobin levels (SpMET) were measured and recorded throughout the procedure using a Masimo Radical-7 Pulse Co-Oximeter (Masimo Corporation, Irvine, Calif, RDS-1 with SET software with methemoglobin interface). Data were analyzed using chi-square, one-way analysis of variance (ANOVA), and Pearson correlation (significance of P < .05). Group 1 had a significantly higher mean peak SpMET level at 3.55% than groups 2 and 3 at 1.63 and 1.60%, respectively. The mean time to peak SpMET was significantly shorter for group 3 at 29.50 minutes than that of group 1 at 62.73 and group 2 at 57.50 minutes. Prilocaine, at 5 mg/kg in pediatric dental patients, resulted in significantly higher peak SpMET levels than lidocaine and no local anesthetic. In comparison to no local anesthetic, the administration of prilocaine and lidocaine caused peak SpMET levels to occur significantly later in the procedure.

  10. Anesthetic success of 1.8ml lidocaine 2% for mandibular tooth extraction. A pilot study

    Directory of Open Access Journals (Sweden)

    Pedro Aravena

    2013-04-01

    Full Text Available Aim: To determine the anesthetic effect of a 1.8ml cartridge of anesthetic lidocaine 2% with epinephrine 1:100,000 in inferior alveolar nerve block (NAI for the extraction in mandibular teeth. Material and methods: A pilot study with analitic design. Participating patients of Dental Emergency Service volunteers from Valdivia-Chile for mandibular teeth extractions attending between May and July of 2010. The anesthetic technique was performed by a dentist using only one cartridge of anesthetic to the NAI. After 15 minutes, the effect was considered effective when anesthetic not require reinforcement with additional anesthesia during extraction of teeth. We analyzed the relationship between success anesthetic effect with sex, age, diagnosis of tooth and type and level of pain observed (chi-square and logistic regression, p<0.05. Results: 62 patients were selected, of which only 47(75.8% was achieved anesthetic success. There was no statistical association with sex, age, type or dental diagnosis and perceived pain. Conclusion: Using a 1.8ml cartridge of anesthesia was effective in three of four patients treated by extraction of mandibular teeth. It suggests further research in relation to the clinical effectiveness of other anesthetics with the same dose in NAI.

  11. Safety, efficacy, and patient acceptability of lidocaine hydrochloride ophthalmic gel as a topical ocular anesthetic for use in ophthalmic procedures

    Directory of Open Access Journals (Sweden)

    Michael A Page

    2009-10-01

    Full Text Available Michael A Page, Frederick W FraunfelderDepartment of Ophthalmology (Casey Eye Institute, Oregon Health and Science University, Portland, OR, USAPurpose: To review the current literature on safety, efficacy, and measures of surgeon and patient satisfaction with lidocaine hydrochloride gel as a tool for ocular anesthesia.Methods: Pubmed search using keywords “lidocaine gel,” “ophthalmic,” and “surgery” and compiling cross-references. Twenty-six total references were reviewed, including 15 prospective randomized controlled trials (RCTs, total N = 933, average N = 62, 6 nonrandomized prospective studies (total N = 234, average N = 39, 2 animal studies, 1 microbiologic study, and 2 letters to the editor.Results: The RCTs and nonrandomized prospective studies evaluated a number of measures including timing of onset of anesthesia, duration of anesthesia, intraoperative and postoperative pain, need for additional anesthetic applications, intracameral lidocaine levels, and adverse effects. Control groups received topical drops, subconjunctival anesthetic, retrobulbar anesthetic, or sham gel. Lidocaine gel was shown to be at least as effective for pain control as alternative therapies in all studies, with longer duration of action than topical drops. Patient and surgeon satisfaction were high, and adverse effects were rare and comparable to those for anesthetic drop formulations. Surgical settings included cataract, pterygium, trabeculectomy, strabismus, intravitreal injection, vitrectomy, and penetrating keratoplasty.Conclusions: Lidocaine gel is a safe, effective, and potentially underutilized tool for ophthalmic surgery.Keywords: lidocaine, gel, topical, ophthalmic, ocular, anesthetic

  12. Effect of Lidocaine-Ketamine Infusions Combined with Morphine or Fentanyl in Sevoflurane-Anesthetized Pigs.

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    Re, Michela; Canfrán, Susana; Largo, Carlota; Gómez de Segura, Ignacioa A

    2016-01-01

    Providing lidocaine, ketamine, and an opioid greatly decreases the minimum alveolar concentration (MAC) of volatile anesthetics in dogs. However, the efficacy of this combination shows marked interspecies variation, and opioids are likely to be less effective in pigs than in other species. The aim of the study was to determine the effects of constant-rate infusion of lidocaine and ketamine combined with either morphine or fentanyl on the MAC of sevoflurane in pigs. In a prospective, randomized, crossover design, 8 healthy crossbred pigs were premedicated with ketamine and midazolam, and anesthesia was induced and maintained with sevoflurane. Pigs then received ketamine (0.6 mg/kg/h) and lidocaine (3 mg/kg/h) combined with either morphine (0.24 mg/kg/h; MLK) or fentanyl (0.0045 mg/kg/h; FLK) after a loading dose; the control group received Ringers lactate solution. The anesthetic-sparing action of the 2 infusion protocols was calculated according to the MAC, by using dewclaw clamping as the standard noxious stimulus. The sevoflurane MAC (mean ± 1 SD) was 2.0% ± 0.2%, 1.9% ± 0.4%, and 1.8% ± 0.2% in the control, MLK, and FLK groups, respectively. No differences among groups or treatments were found. In conclusion, the administration of MLK or FLK at the studied doses did not reduce the MAC of sevoflurane in pigs.

  13. An estimation of the minimum effective anesthetic volume of 2% lidocaine in ultrasound-guided axillary brachial plexus block.

    LENUS (Irish Health Repository)

    O'Donnell, Brian D

    2009-07-01

    Ultrasound guidance facilitates precise needle and injectate placement, increasing axillary block success rates, reducing onset times, and permitting local anesthetic dose reduction. The minimum effective volume of local anesthetic in ultrasound-guided axillary brachial plexus block is unknown. The authors performed a study to estimate the minimum effective anesthetic volume of 2% lidocaine with 1:200,000 epinephrine (2% LidoEpi) in ultrasound-guided axillary brachial plexus block.

  14. Effect of intraoperative lidocaine on anesthetic consumption, and bowel function, pain intensity, analgesic consumption and hospital stay after breast surgery.

    Science.gov (United States)

    Choi, Soo Joo; Kim, Myung Hee; Jeong, Hui Yeon; Lee, Jeong Jin

    2012-05-01

    Perioperative lidocaine infusion improves postoperative outcomes, mostly after abdominal and urologic surgeries. Knowledge of the effect of lidocaine on peripheral surgeries is limited. Presently, we investigated whether intraoperative lidocaine infusion reduced anesthetic consumption, duration of ileus, pain intensity, analgesic consumption and hospital stay after breast plastic surgeries. Sixty female patients, aged 20-60 years, enrolled in this prospective study were randomly and equally divided to two groups. One group (n = 30) received a 1.5 mg/kg bolus of lidocaine approximately 30 min before incision followed by continuous infusion of lidocaine (1.5 mg/kg/h) until skin closure (lidocaine group). The other group (n = 30) was untreated (control group). Balanced inhalation (sevoflurane) anesthesia and multimodal postoperative analgesia were standardized. End tidal sevoflurane concentration during surgery, time to the first flatus and defecation, visual analog pain scale (0-10), analgesic consumption and associated side effects at 24, 48, and 72 h after surgery, hospital stay, and patient's general satisfaction were assessed. Compared to the control group, intraoperative lidocaine infusion reduced by 5% the amount of sevoflurane required at similar bispectral index (P = 0.014). However, there were no significant effects of lidocaine regarding the return of bowel function, postoperative pain intensity, analgesic sparing and side effects at all time points, hospital stay, and level of patient's satisfaction for pain control. Low dose intraoperative lidocaine infusion offered no beneficial effects on return of bowel function, opioid sparing, pain intensity and hospital stay after various breast plastic surgeries.

  15. Efficacy of articaine and lidocaine in a primary intraligamentary injection administered with a computer-controlled local anesthetic delivery system.

    Science.gov (United States)

    Berlin, Jeffrey; Nusstein, John; Reader, Al; Beck, Mike; Weaver, Joel

    2005-03-01

    The purpose of this prospective, randomized, double-blind study was to compare the anesthetic efficacy of the intraligamentary injection of 4% articaine with 1:100,000 epinephrine and of 2% lidocaine with 1:100,000 epinephrine, administered with computer-controlled local anesthetic delivery system, in mandibular posterior teeth. Using a crossover design, intraligamentary injections of 1.4 mL of 4% articaine with 1:100,000 epinephrine and of 1.4 mL of 2% lidocaine with 1:100,000 epinephrine were randomly administered with a computer-controlled local anesthetic delivery system, in a double-blind manner on the mesial and distal aspects of a mandibular first molar, at 2 separate appointments to 51 subjects. A pulp tester was used to test for anesthesia, in 2-minute cycles for 60 minutes, of the mandibular first and second molars and second premolar. Anesthesia was considered successful when 2 consecutive 80 readings (highest output) were obtained within 20 minutes. Successful pulpal anesthesia was obtained 86% of the time for the first molar using the articaine solution and 74% of the time using the lidocaine solution. There were no significant differences (P > .05) between the articaine and lidocaine solutions. The mean onset times of pulpal anesthesia for the first molar were 1.3 minutes with articaine solution and 2.2 minutes with lidocaine solution. Duration of pulpal anesthesia for the first molar was 34 minutes for the articaine solution and 31 minutes for the lidocaine solution. The efficacy of 4% articaine with 1:100,000 epinephrine was similar to the efficacy of 2% lidocaine with 1:100,000 epinephrine for intraligamentary injections.

  16. Preparation and characterization of poly(ε-caprolactone) nanospheres containing the local anesthetic lidocaine.

    Science.gov (United States)

    Ramos Campos, Estefânia Vangelie; Silva de Melo, Nathalie Ferreira; Guilherme, Viviane Aparecida; de Paula, Eneida; Rosa, André Henrique; de Araújo, Daniele Ribeiro; Fraceto, Leonardo Fernandes

    2013-01-01

    The objective of this work was to develop a modified release system for the local anesthetic lidocaine (LDC), using poly(ε-caprolactone) (PCL) nanospheres (NSs), to improve the pharmacological properties of the drug when administered by the infiltration route. In vitro experiments were used to characterize the system and investigate the release mechanism. The NSs presented a polydispersion index of 0.072, an average diameter of 449.6 nm, a zeta potential of -20.1 mV, and an association efficiency of 93.3%. The release profiles showed that the release of associated LDC was slower than that of the free drug. Atomic force microscopy analyses showed that the spherical structure of the particles was preserved as a function of time, as well as after the release experiments. Cytotoxicity and pharmacological tests confirmed that association with the NSs reduced the toxicity of LDC, and prolonged its anesthetic action. This new formulation could potentially be used in applications requiring gradual anesthetic release, especially dental procedures.

  17. Inhibition of brain cell excitability by lidocaine, QX314, and tetrodotoxin: a mechanism for analgesia from infused local anesthetics?

    Science.gov (United States)

    Butterworth, J; Cole, L; Marlow, G

    1993-07-01

    Local anesthetic infusions have been used to provide analgesia in a variety of painful conditions. The mechanism for this drug effect remains unknown. To better define the electrical effects of lidocaine concentrations comparable to those obtained during analgesic infusions, lidocaine (0.05-3 mmol.l-1), QX314 (an obligatorily charged, quaternary lidocaine derivative applied within the cells), and tetrodotoxin (10 mmol.l-1) were applied to rat hippocampal pyramidal cells. The three drugs, which inhibit Na+ currents by varying mechanisms, produced tonic increases in (firing) current threshold, and decreases in the amplitude of action potentials measured using an intracellular microelectrode technique. Lidocaine inhibited action potential spikes and increased current threshold in a concentration-dependent fashion. Lidocaine 50 and 100 mumol.l-1 did not inhibit action potentials, but increased firing threshold by nearly 100%. Lidocaine 1-3 mmol.l-1 significantly inhibited action potential amplitude and increased threshold by as much as 800%. Similarly, QX314 and tetrodotoxin produced greater increases in current threshold than in action potential amplitude. QX314 produced phasic (or frequency-dependent) block during trains of stimuli at 1 Hz, even when almost no tonic block was present. Lidocaine produced less phasic block than QX314, and required both greater tonic block and more frequent stimulation to produce the phenomenon. Tetrodotoxin demonstrated no phasic block. Increases in current threshold occurred in lidocaine concentrations associated with analgesia and toxicity; inhibition of action potentials occurred scarcely at all at these concentrations. Thus, tonic increases in current threshold may underlie analgesia and supplementation of general anesthesia by intravenous lidocaine.

  18. Hyperalgesia by low doses of the local anesthetic lidocaine involves cannabinoid signaling: an fMRI study in mice.

    Science.gov (United States)

    Bosshard, Simone C; Grandjean, Joanes; Schroeter, Aileen; Baltes, Christof; Zeilhofer, Hanns U; Rudin, Markus

    2012-07-01

    Lidocaine is clinically widely used as a local anesthetic inhibiting propagation of action potentials in peripheral nerve fibers. Correspondingly, the functional magnetic resonance imaging (fMRI) response in mouse brain to peripheral noxious input is largely suppressed by local lidocaine administered at doses used in a clinical setting. We observed, however, that local administration of lidocaine at doses 100 × lower than that used clinically led to a significantly increased sensitivity of mice to noxious forepaw stimulation as revealed by fMRI. This hyperalgesic response could be confirmed by behavioral readouts using the von Frey filament test. The increased sensitivity was found to involve a type 1 cannabinoid (CB(1)) receptor-dependent pathway as global CB(1) knockout mice, as well as wild-type mice pretreated systemically with the CB(1) receptor blocker rimonabant, did not display any hyperalgesic effects after low-dose lidocaine. Additional experiments with nociceptor-specific CB(1) receptor knockout mice indicated an involvement of the CB(1) receptors located on the nociceptors. We conclude that low concentrations of lidocaine leads to a sensitization of the nociceptors through a CB(1) receptor-dependent process. This lidocaine-induced sensitization might contribute to postoperative hyperalgesia.

  19. Local anesthesia for extracorporeal shock wave lithotripsy: a study comparing eutetic mixture of local anesthetics cream and lidocaine infiltration

    DEFF Research Database (Denmark)

    Honnens de Lichtenberg, M; Miskowiak, J; Mogensen, P

    1992-01-01

    A study of the anesthetic efficacy of a eutetic mixture of local anesthetics (EMLA cream) versus lidocaine infiltration in extracorporeal shock wave lithotripsy (ESWL) was done. A total of 46 patients had 30 gm. of EMLA cream applied to the skin over the kidney and 45 had subcutaneous infiltration...... anesthesia with 20 ml. 1% lidocaine with epinephrine. All patients received an intravenous dose of morphine just before ESWL. The patients were comparable with regard to age, sex, weight, morphine dosage, number of shock waves given and duration of treatment. Median pain score and the amount of supplementary...... analgesics were not significantly different between the 2 groups. There were no significant differences between the groups with regard to post-ESWL skin changes. Therefore, EMLA cream can be recommended for ESWL provided it is applied correctly....

  20. Activation of TRPA1 by membrane permeable local anesthetics

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    Kronewald Sergej

    2011-08-01

    Full Text Available Abstract Background Low concentrations of local anesthetics (LAs suppress cellular excitability by inhibiting voltage-gated Na+ channels. In contrast, LAs at high concentrations can be excitatory and neurotoxic. We recently demonstrated that LA-evoked activation of sensory neurons is mediated by the capsaicin receptor TRPV1, and, to a lesser extent by the irritant receptor TRPA1. LA-induced activation and sensitization of TRPV1 involves a domain that is similar, but not identical to the vanilloid-binding domain. Additionally, activation of TRPV1 by LAs involves PLC and PI(4,5P2-signalling. In the present study we aimed to characterize essential structural determinants for LA-evoked activation of TRPA1. Results Recombinant rodent and human TRPA1 were expressed in HEK293t cells and investigated by means of whole-cell patch clamp recordings. The LA lidocaine activates TRPA1 in a concentration-dependent manner. The membrane impermeable lidocaine-derivative QX-314 is inactive when applied extracellularly. Lidocaine-activated TRPA1-currents are blocked by the TRPA1-antagonist HC-030031. Lidocaine is also an inhibitor of TRPA1, an effect that is more obvious in rodent than in human TRPA1. This species-specific difference is linked to the pore region (transmembrane domain 5 and 6 as described for activation of TRPA1 by menthol. Unlike menthol-sensitivity however, lidocaine-sensitivity is not similarly determined by serine- and threonine-residues within TM5. Instead, intracellular cysteine residues known to be covalently bound by reactive TRPA1-agonists seem to mediate activation of TRPA1 by LAs. Conclusions The structural determinants involved in activation of TRPA1 by LAs are disparate from those involved in activation by menthol or those involved in activation of TRPV1 by LAs.

  1. Local anesthesia for extracorporeal shock wave lithotripsy: a study comparing eutetic mixture of local anesthetics cream and lidocaine infiltration

    DEFF Research Database (Denmark)

    Honnens de Lichtenberg, M; Miskowiak, J; Mogensen, P

    1992-01-01

    A study of the anesthetic efficacy of a eutetic mixture of local anesthetics (EMLA cream) versus lidocaine infiltration in extracorporeal shock wave lithotripsy (ESWL) was done. A total of 46 patients had 30 gm. of EMLA cream applied to the skin over the kidney and 45 had subcutaneous infiltration...... analgesics were not significantly different between the 2 groups. There were no significant differences between the groups with regard to post-ESWL skin changes. Therefore, EMLA cream can be recommended for ESWL provided it is applied correctly....

  2. Anesthetic and recovery profiles of lidocaine versus mepivacaine for spinal anesthesia in patients undergoing outpatient orthopedic arthroscopic procedures.

    Science.gov (United States)

    Pawlowski, Julius; Orr, Kevin; Kim, Ku-Mie; Pappas, Ana Lucia; Sukhani, Radha; Jellish, W Scott

    2012-03-01

    To compare isobaric lidocaine and mepivacaine in outpatient arthroscopic surgery. Prospective, randomized, double-blinded study. Ambulatory surgery center affiliated with an academic tertiary-care hospital. 84 adult, ASA physical status 1, 2, and 3 ambulatory patients, age 18-70 years, undergoing arthroscopic knee surgery. Patients were randomized to receive a combination spinal-epidural anesthetic using 80 mg of either isobaric 2% mepivacaine or isobaric 2% lidocaine. Patients also received a femoral 3-in-1 block with 0.5% bupivacaine applied to the affected extremity. Demographic data and level and duration of the block were recorded. The use of supplemental epidural anesthesia was noted along with frequency of bradycardia, hypotension, and episodes of nausea and vomiting. Duration of block and times to ambulation and voiding were recorded. Delayed variables, including fatigue, difficulty urinating, back pain, and transient neurologic symptoms (TNS) were obtained. No demographic differences were noted between groups, and surgical duration was similar. Satisfactory anesthesia was achieved in all cases, with no differences noted in hypotension, bradycardia, nausea, or vomiting. Onset of sensory and motor block was similar. Duration of block before epidural supplementation was 94 ± 21 minutes with lidocaine versus 122 ± 23 minutes for mepivacaine (P mepivacaine but did not affect PACU stay. Twenty-four and 48-hour recovery was similar with no TNS symptoms reported. No major differences were noted between lidocaine and mepivacaine spinal anesthesia. Time to ambulation and voiding were longer in patients who received mepivacaine as was time to first dose of epidural catheter. Neither group had TNS symptoms. Lidocaine and mepivacaine are both appropriate spinal anesthetics for ambulatory orthopedic lower extremity procedures. Copyright © 2012 Elsevier Inc. All rights reserved.

  3. Comparative Evaluation of Anesthetic Efficacy of 2% Lidocaine, 4% Articaine, and 0.5% Bupivacaine on Inferior Alveolar Nerve Block in Patients with Symptomatic Irreversible Pulpitis: A Prospective, Randomized, Double-blind Clinical Trial.

    Science.gov (United States)

    Aggarwal, Vivek; Singla, Mamta; Miglani, Sanjay

    2017-01-01

    To compare the anesthetic efficacy of 1.8 mL of 2% lidocaine with 1:200,000 epinephrine, 4% articaine with 1:100,000 epinephrine, and 0.5% bupivacaine with 1:200,000 epinephrine on producing inferior alveolar nerve block (IANB) in patients with symptomatic irreversible pulpitis. A total of 91 adult patients who were actively experiencing mandibular molar pain were involved in this study. The patients were randomly divided into three groups on the basis of the anesthetic solution used. The first group received IANB with 1.8 mL of 2% lidocaine with 1:200,000 epinephrine, the second group received IANB with 4% articaine with 1:100,000 epinephrine, and the third group received IANB with 0.5% bupivacaine with 1:200,000 epinephrine. After 15 minutes of IANB, conventional endodontic access preparation was started. The pain during the treatment was noted on a Heft-Parker visual analog scale (HP VAS). The primary outcome measure was anesthetic success, and anesthesia was considered successful if the patient reported no pain or weak/mild pain (HP VAS score 2% lidocaine, 4% articaine, and 0.5% bupivacaine were 23%, 33%, and 17%, respectively. The differences were statistically insignificant (P > .05). The 2% lidocaine solution used for IANB had similar success rates when compared with 4% articaine and 0.5% bupivacaine.

  4. Infiltration anesthetic lidocaine inhibits cancer cell invasion by modulating ectodomain shedding of heparin-binding epidermal growth factor-like growth factor (HB-EGF).

    Science.gov (United States)

    Mammoto, Tadanori; Higashiyama, Shigeki; Mukai, Mutsuko; Mammoto, Akiko; Ayaki, Masako; Mashimo, Takashi; Hayashi, Yukio; Kishi, Yoshihiko; Nakamura, Hiroyuki; Akedo, Hitoshi

    2002-09-01

    Although the mechanism is unknown, infiltration anesthetics are believed to have membrane-stabilizing action. We report here that such a most commonly used anesthetic, lidocaine, effectively inhibited the invasive ability of human cancer (HT1080, HOS, and RPMI-7951) cells at concentrations used in surgical operations (5-20 mM). Ectodomain shedding of heparin-binding epidermal growth factor-like growth factor (HB-EGF) from the cell surface plays an important role in invasion by HT1080 cells. Lidocaine reduced the invasion ability of these cells by partly inhibiting the shedding of HB-EGF from the cell surface and modulation of intracellular Ca2+ concentration contributed to this action. The anesthetic action of lidocaine (sodium channel blocking ability) did not contribute to this anti-invasive action. In addition, lidocaine (5-30 mM), infiltrated around the inoculation site, inhibited pulmonary metastases of murine osteosarcoma (LM 8) cells in vivo. These data point to previously unrecognized beneficial actions of lidocaine and suggest that lidocaine might be an ideal infiltration anesthetic for surgical cancer operations.

  5. Enhancement of the 1-Octanol/Water Partition Coefficient of the Anti-Inflammatory Indomethacin in the Presence of Lidocaine and Other Local Anesthetics.

    Science.gov (United States)

    Tateuchi, Ryo; Sagawa, Naoki; Shimada, Yohsuke; Goto, Satoru

    2015-07-30

    Side effects and excessive potentiation of drug efficacy caused by polypharmacy are becoming important social issues. The apparent partition coefficient of indomethacin (log P'IND) increases in the presence of lidocaine, and this is used as a physicochemical model for investigating polypharmacy. We examined the changes in log P'IND caused by clinically used local anesthetics-lidocaine, tetracaine, mepivacaine, bupivacaine, and dibucaine-and by structurally similar basic drugs-procainamide, imipramine, and diltiazem. The quantitative structure-activity relationship study of log P'IND showed that the partition coefficient values (log PLA) and the structural entropic terms (ΔSobs, log f) of the additives affect log P'IND. These results indicate that the local anesthetics and structurally similar drugs function as phase-transfer catalysts, increasing the membrane permeability of indomethacin via heterogeneous intermolecular association. Therefore, we expect that the potency of indomethacin, an acidic nonsteroidal anti-inflammatory drug, will be increased by concurrent administration of the other drugs.

  6. 穿膜肽纳米类脂质体包载利多卡因的透皮特性及表面麻醉效果初探%Preliminary study on transdermal characteristics and sunface anesthetic effects of lidocaine hydrochloride loaded trans-activator of transcription peptide conjugated nano-niosome in animals

    Institute of Scientific and Technical Information of China (English)

    王悦; 张连云; 李长义; 王汉杰; 李芹

    2015-01-01

    Objective To prepare a new dental topical anesthetics,lidocaine hydrochloride loaded trans-activator of transcription peptide conjugated nano-niosome(LID-TAT-N),and to evaluate its transdermal properties and topical anesthesia effects.Methods LID-TAT-N was prepared using reversephase evaporation method,and lidocaine loaded conventional liposome(LID-CL) was prepared in the same manner as positive control.The diameter,ξ potential and encapsulation efficiency of LID-TAT-N and LID-CL were measured.The skin permeation of LID-TAT-N was examined,and compared with LID-CL and lidocaine injection(LID-IJ,as negative control),using a Franz diffusion cell mounted with depilated mouse skin in vitro for 12 hours.Each experiment was repeated six times.The anesthetic effect of the new topical anesthetic was investigated on the cornea of rabbits.Results The mean diameter of LID-TAT-N was smaller than that of LID-CL[(152.7 ± 10.6) nm vs.(259.5 ± 15.5) nm,P<0.01].The 12 h cumulative permeation amount was significantly higher in LID-TAT-N group[(1 340.0±97.5) μg· cm-2] than those of LID-CL and LID-IJ groups[(1 060.6±80.2),(282.6±65.1) μg· cm-2,respectively,P<0.05].Rabbit corneal reflex results showed that LID-TAT-N had anesthetic effect and the duration of analgesia[(24.8±2.8) min] was also longer than that of LID-IJ[(14.5 ± 2.3) min,P<0.05].Conclusions LID-TAT-N had good transdermal ability,and the advanced skin penetration feature can improve its tropical anesthetic effect.%目的 研究穿膜肽纳米类脂质体包载利多卡因(lidocaine hydrochloride loaded transactivator of transcription peptide conjugated nano-niosome,LID-TAT-N)在动物体内外透皮情况及其表面麻醉效果,为研制新型口腔表面麻醉剂提供依据.方法 制备LID-TAT-N,传统脂质体包载利多卡因(lidocaine hydrochloride loaded conventional liposome,LID-CL),分别检测粒径、电势和包封率.用离体小鼠皮进行12h体外透皮实验,测定并比较LID-TAT-N组

  7. Comparison of O2 saturation, heart and respiratory rate following injection of vasoconstrictor containing anesthetic (lidocaine 2% and without vasoconstrictor anesthetic (Mepivacaine

    Directory of Open Access Journals (Sweden)

    Bayat M.

    2005-07-01

    Full Text Available Background and Aim: Along with higher usage of dental local anesthesia with risks to people health together with their positive role, the important goal of dentistry, patients’ health, has been stressed repeatedly nowadays. This study was conducted to compare O2 saturation, respiratory rate and heart rate of patients following injection of anesthetic containing vasoconstrictor (lidocaine 2% and without vasoconstrictor (Mepivacaine. Materials and Methods: This experimental study was conducted on 32 healthy humans (16 females and 16 males with 25-50 years age range and no history of drug usage. Cases were classified into two matched groups. O2 saturation, heart and respiratory rate were recorded before extraction of a mandibular posterior tooth. In the first group, 3.6 ml lidocaine 2% with 1:80,000 epinephrine and in the second group Mepivacaine 3% was injected, using inferior alveolar dental nerve block with aspiration. Variables were measured and recorded. Tooth extraction was performed and the mentioned variables were recorded again. Data were analyzed with SPSS software using t and Paired t-test with P<0.05 as the limit of significance. Results: After injection of lidocaine, the heart rate was increased (12.25±1.75 bpm, and the time to reach the maximum rate was 64.75±11.26 seconds. After extraction of tooth, heart rate in both groups was increased not considering the type of injection. Conclusion: The study showed that the injection of lidocaine (containing epinephrine in patients without contraindication has no risk. Also, possible increase in heart rate is not risky and is not associated with O2 saturation decrease and respiratory interruption.

  8. Dexmedetomidine (12.5 μg/mL) improves tissue distribution, anesthetic action, and hemodynamic effects of lidocaine after palatal infiltration in rats.

    Science.gov (United States)

    Akimoto, Takuma; Hashimoto, Shuichi; Sunada, Katsuhisa

    2016-09-01

    Dexmedetomidine hydrochloride (DEX) is a α2-adrenergic receptor agonist that causes vasoconstriction by acting on α2B-adrenergic receptors in peripheral blood vessels. The authors aimed to determine the influence of DEX on tissue distribution, anesthetic action, and hemodynamic effects of lidocaine in rats. The investigators injected indigo carmine-containing (14)C-labeled lidocaine hydrochloride (2 %) without and with 3.1, 12.5, or 50 μg/mL DEX or 10 μg/mL epinephrine into the right palatal mucosa mesial to the maxillary first molar of specific pathogen-free male Wistar rats. Autoradiography and liquid scintillation counting were performed to evaluate (14)C-labeled lidocaine concentrations in the palatal mucosa, maxillary bone, maxillary nerve, and peripheral blood. Somatosensory-evoked potentials were measured to analyze anesthetic action, and blood pressure and pulse rate were measured to compare hemodynamic effects. DEX extended the tissue distribution of lidocaine in a concentration-dependent manner. Lidocaine with 12.5 μg/mL DEX had similar blood peak arrival time and peak-to-peak amplitude as lidocaine with 10 μg/mL epinephrine, but it reduced pulse rate. The results of this study suggest that 12.5 μg/mL DEX improves tissue distribution, anesthetic action, and hemodynamic effects of lidocaine in rats. Therefore, 12.5 μg/mL DEX may be a suitable alternative to epinephrine in lidocaine formulations, especially for patients with ischemic heart disease and hypertension.

  9. Review of Lidocaine/Tetracaine Cream as a Topical Anesthetic for Dermatologic Laser Procedures

    National Research Council Canada - National Science Library

    Alster, Tina

    2013-01-01

    .... The lidocaine/tetracaine cream (Pliaglis®, Galderma Laboratories, Texas, USA), one of the newer combination options, offers effective pain alleviation that has been evaluated in numerous clinical trials...

  10. Inhibition of human two-pore domain K+ channel TREK1 by local anesthetic lidocaine: negative cooperativity and half-of-sites saturation kinetics.

    Science.gov (United States)

    Nayak, Tapan K; Harinath, S; Nama, S; Somasundaram, K; Sikdar, S K

    2009-10-01

    TWIK-related K+ channel TREK1, a background leak K+ channel, has been strongly implicated as the target of several general and local anesthetics. Here, using the whole-cell and single-channel patch-clamp technique, we investigated the effect of lidocaine, a local anesthetic, on the human (h)TREK1 channel heterologously expressed in human embryonic kidney 293 cells by an adenoviral-mediated expression system. Lidocaine, at clinical concentrations, produced reversible, concentration-dependent inhibition of hTREK1 current, with IC(50) value of 180 muM, by reducing the single-channel open probability and stabilizing the closed state. We have identified a strategically placed unique aromatic couplet (Tyr352 and Phe355) in the vicinity of the protein kinase A phosphorylation site, Ser348, in the C-terminal domain (CTD) of hTREK1, that is critical for the action of lidocaine. Furthermore, the phosphorylation state of Ser348 was found to have a regulatory role in lidocaine-mediated inhibition of hTREK1. It is interesting that we observed strong intersubunit negative cooperativity (Hill coefficient = 0.49) and half-of-sites saturation binding stoichiometry (half-reaction order) for the binding of lidocaine to hTREK1. Studies with the heterodimer of wild-type (wt)-hTREK1 and Delta119 C-terminal deletion mutant (hTREK1(wt)-Delta119) revealed that single CTD of hTREK1 was capable of mediating partial inhibition by lidocaine, but complete inhibition necessitates the cooperative interaction between both the CTDs upon binding of lidocaine. Based on our observations, we propose a model that explains the unique kinetics and provides a plausible paradigm for the inhibitory action of lidocaine on hTREK1.

  11. In vitro synergistic activity of lidocaine and miconazole against Candida albicans

    Directory of Open Access Journals (Sweden)

    Maria da Conceição dos Santos Oliveira Cunha

    2017-08-01

    Full Text Available Candida albicans is the main yeast isolated from vulvovaginal candidiasis(VVC and a major antifungal used to treat VVC is miconazole (MZ, it shows local toxic effects, such as irritation and burns. The lidocaine (LD is a local anesthetic. The aim of this study was to evaluate the synergistic activity of LD/MZ against 19 strains of C. albicans isolated from vaginal secretion. 78.9% of the strains were susceptible to the combination LD/MZ, demonstrating synergism of drugs. These drugs can be used to produce vaginal creams to treat VVC, especially drug resistant.

  12. Regional anesthetic activity of new decahydroquinolinyl derivative by the experimental model of terminal anesthesia

    Directory of Open Access Journals (Sweden)

    Goncharuk V.V.

    2014-09-01

    Full Text Available anesthesia. Material and Methods. Decahydroquinolinyl derivative under laboratory code PAS-68 synthesized in the A. B. Bekturov Institute of Chemical Sciences under the guidance of K. D. Praliev has been studied. Benzocaine, lido-caine and tetracaine were used as the comparison drugs. Male rabbits of 2,0-3,5 kg weight were used as experimental animals. A threshold of corneal sensitivity to tactile effects (Rainier index was determined by the standard method. Computer prognosis of PAS-68 acute toxicity also was made. Results. The local anesthetic activity of 1 %, 0,5% and 0,25% solutions of PAS-68 were identified as higher than that for lidocaine and benzocaine in similar concentrations (p <0,05 but lower than that for tetracaine (p<0,05. PAS-68 has no local irritating action. The duration of anesthesia, 0,5% and 1 % PAS 68 exceeds that for benzocaine and lidocaine at equivalent concentrations (p<0,05. By this kind of activity PAS-68 is a second to the duration of anesthesia by tetracaine (p<0,05. The latent period of anesthesia induced by PAS-68 is shorter than the latent periods induced by benzocaine, lidocaine and tetracaine. On the base of predictive analysis it was concluded that PAS-68 is of low toxicity. Conclusion. PAS-68 exceeds benzocaine and lidocaine by the local anesthetic activity and duration of anesthesia and is second only to tetracaine. The latent period of anesthesia PAC-68 is shorter than the latent period of benzocaine, lidocaine and tetracaine respectively.

  13. The success rate of bupivacaine and lidocaine as anesthetic agents in inferior alveolar nerve block in teeth with irreversible pulpitis without spontaneous pain

    Directory of Open Access Journals (Sweden)

    Masoud Parirokh

    2015-05-01

    Full Text Available Objectives Achieving adequate anesthesia with inferior alveolar nerve blocks (IANB is of great importance during dental procedures. The aim of the present study was to assess the success rate of two anesthetic agents (bupivacaine and lidocaine for IANB when treating teeth with irreversible pulpitis. Materials and Methods Sixty volunteer male and female patients who required root canal treatment of a mandibular molar due to caries participated in the present study. The inclusion criteria included prolonged pain to thermal stimulus but no spontaneous pain. The patients were randomly allocated to receive either 2% lidocaine with 1:80,000 epinephrine or 0.5% bupivacaine with 1:200,000 epinephrine as an IANB injection. The sensitivity of the teeth to a cold test as well as the amount of pain during access cavity preparation and root canal instrumentation were recorded. Results were statistically analyzed with the Chi-Square and Fischer's exact tests. Results At the final step, fifty-nine patients were included in the study. The success rate for bupivacaine and lidocaine groups were 20.0% and 24.1%, respectively. There was no significant difference between the two groups at any stage of the treatment procedure. Conclusions There was no difference in success rates of anesthesia when bupivacaine and lidocaine were used for IANB injections to treat mandibular molar teeth with irreversible pulpitis. Neither agent was able to completely anesthetize the teeth effectively. Therefore, practitioners should be prepared to administer supplemental anesthesia to overcome pain during root canal treatment.

  14. Are one or two dangerous? Lidocaine and topical anesthetic exposures in children.

    Science.gov (United States)

    Curtis, Liesl A; Dolan, Teresa Sullivan; Seibert, H Edward

    2009-07-01

    Topical anesthetics are found in a variety of prescription and non-prescription preparations, from teething gels to hemorrhoid creams. In 2003, there were 8576 exposures to local/topical anesthetics reported to the American Association of Poison Control Centers, with 67% of cases in the age group younger than 6 years old. This report reviews the available literature involving topical anesthetic exposures in children younger than 6 years old, including the National Library of Medicine's Pub Med database (limited to English language) and data from POISINDEX. Additionally, we reviewed the American Association of Poison Control Centers' annual reports from 1983 to 2003. There were 7 deaths in this age range from topical anesthetics. Although the number of deaths is low, the fact that there have been deaths reveals the serious nature of the toxicity that can result from these readily available non-prescription analgesics. Toxicity may result from topical absorption, ingestion, or aspiration. Additionally, toxicity can result from unintentional as well as therapeutic mishaps. Although the number of cases is limited, these medications can be toxic at low doses-which, in children younger than 6 years of age, may amount to as little as a teaspoon.

  15. Lumbar segmental nerve blocks with local anesthetics, pain relief, and motor function: a prospective double-blind study between lidocaine and ropivacaine.

    Science.gov (United States)

    Wolff, André P; Wilder Smith, Oliver H G; Crul, Ben J P; van de Heijden, Marc P; Groen, Gerbrand J

    2004-08-01

    Selective segmental nerve blocks with local anesthetics are applied for diagnostic purposes in patients with chronic back pain to determine the segmental level of the pain. We performed this study to establish myotomal motor effects after L4 spinal nerve blocks by lidocaine and ropivacaine and to evaluate the relationship with pain. Therefore, 20 patients, of which 19 finished the complete protocol, with chronic lumbosacral radicular pain without neurological deficits underwent segmental nerve blocks at L4 with both lidocaine and ropivacaine. Pain intensity scores (verbal numeric rating scale; VNRS) and the maximum voluntary muscle force (MVMF; using a dynamometer expressed in newtons) of the tibialis anterior and quadriceps femoris muscles were measured on the painful side and on the control side. The median VNRS decrease was 4.0 (P control side (P = 0.016; Tukey test). Multiple regression revealed a significant negative correlation for change in VNRS score versus change in median MVMF (Spearman R = -0.48: P = 0.00001). This study demonstrates that in patients with unilateral chronic low back pain radiating to the leg, pain reduction induced by local anesthetic segmental nerve (L4) block is associated with increased quadriceps femoris and tibialis anterior MVMF, without differences for lidocaine and ropivacaine.

  16. Comparison of the Anesthetic Efficacy of Mepivacaine and Lidocaine in Patients with Irreversible Pulpitis: A Double-blind Randomized Clinical Trial.

    Science.gov (United States)

    Visconti, Renata Pieroni; Tortamano, Isabel Peixoto; Buscariolo, Inês Aparecida

    2016-09-01

    The objective of this study was to compare the anesthetic efficacy of 2% mepivacaine combined with 1:100,000 epinephrine with 2% lidocaine combined with 1:100,000 epinephrine during pulpectomy of mandibular posterior teeth in patients with irreversible pulpitis. Forty-two patients with irreversible pulpitis who were admitted to the Emergency Center at the University of São Paulo School of Dentistry volunteered to take part in the study and were randomized to receive conventional inferior alveolar nerve block containing 1.8 or 3.6 mL of either 2% mepivacaine with 1:100,000 epinephrine or 2% lidocaine with 1:100,000 epinephrine. We recorded patients' subjective assessments of lip anesthesia, absence/presence of pulpal anesthesia tested by using electric pulp stimulation, and absence/presence of pain during the subsequent pulpectomy by using a verbal analogue scale. All patients tested reported lip anesthesia after application of either type of inferior alveolar nerve block. Pulpal anesthesia success rates measured by using the pulp tester were satisfactory for both solutions (86% for mepivacaine and 67% for lidocaine). Success rates according to patient report of no pain or mild pain during pulpectomy were higher for mepivacaine solution (55%) than for lidocaine solution (14%). The differences between mepivacaine and lidocaine were statistically significant. Mepivacaine resulted in effective pain control during irreversible pulpitis treatments. The success rates with either solution were not high enough to ensure complete pulpal anesthesia. Copyright © 2016 American Association of Endodontists. Published by Elsevier Inc. All rights reserved.

  17. Does the combination of 3% mepivacaine plain plus 2% lidocaine with epinephrine improve anesthesia and reduce the pain of anesthetic injection for the inferior alveolar nerve block? A prospective, randomized, double-blind study.

    Science.gov (United States)

    Lammers, Emily; Nusstein, John; Reader, Al; Drum, Melissa; Beck, Mike; Fowler, Sara

    2014-09-01

    In theory, using 3% mepivacaine initially for an inferior alveolar nerve (IAN) block would decrease the pain of injection, provide faster onset, and increase anesthetic success. The purpose of this prospective, randomized, double-blind study was to compare the degree of pulpal anesthesia obtained with a combination of 3% mepivacaine/2% lidocaine (1:100,000 epinephrine) versus a combination of 2% lidocaine (1:100,000 epinephrine)/2% lidocaine (1:100,000 epinephrine) in IAN blocks. Injection pain was also studied. One hundred asymptomatic subjects were randomly given a combination of a 1-cartridge volume of 3% mepivacaine plus a 1-cartridge volume of 2% lidocaine with 1:100,000 epinephrine and a combination of a 1-cartridge volume of 2% lidocaine with 1:100,000 epinephrine plus a 1-cartridge volume of 2% lidocaine with 1:100,000 epinephrine for the IAN block at 2 separate appointments. Subjects rated the pain of injection. The molars, premolars, and incisors were tested with an electric pulp tester in 4-minute cycles for 60 minutes. Anesthetic success was defined as the subject achieving 2 consecutive 80 readings within 15 minutes after completion of the IAN blocks and sustaining the 80 reading for 60 minutes. Success was not significantly different (P > .05) between the 2 combinations. No statistical differences in injection pain or onset times were found. The combination of 3% mepivacaine plus 2% lidocaine with 1:100,000 epinephrine was equivalent to the combination of 2 cartridges of 2% lidocaine with 1:100,000 epinephrine in terms of injection pain, onset time, and pulpal anesthetic success for the IAN block. Copyright © 2014 American Association of Endodontists. Published by Elsevier Inc. All rights reserved.

  18. A prospective, randomized, double-blind comparison of the anesthetic efficacy of two percent lidocaine with 1:100,000 epinephrine and three percent mepivacaine in the maxillary high tuberosity second division nerve block.

    Science.gov (United States)

    Forloine, Amy; Drum, Melissa; Reader, Al; Nusstein, John; Beck, Mike

    2010-11-01

    The purpose of this prospective, randomized, double-blind study was to compare the anesthetic efficacy of 2% lidocaine with 1:100,000 epinephrine and 3% mepivacaine in the maxillary high tuberosity second division nerve block. Fifty subjects randomly received maxillary high tuberosity second division nerve blocks by using 3.6 mL of 2% lidocaine with 1:100,000 epinephrine and 3.6 mL of 3% mepivacaine at 2 separate appointments spaced at least 1 week apart. The anterior, premolar, and molar teeth were pulp tested in 4-minute cycles for a total of 60 minutes. Success was defined as no subject response to 2 consecutive 80 readings with the electric pulp tester. The high tuberosity approach to the maxillary second division nerve block with both anesthetic formulations resulted in a high success rate (92%-98%) for the first and second molars. Approximately 76%-78% of the second premolars were anesthetized with both anesthetic formulations. Both anesthetic formulations were ineffective for the anterior teeth and first premolars. The use of 3% mepivacaine provided a significantly shorter duration of pulpal anesthesia than 2% lidocaine with 1:100,000 epinephrine in the molars and premolars. Copyright © 2010 American Association of Endodontists. Published by Elsevier Inc. All rights reserved.

  19. Design and evaluation of lidocaine- and prilocaine-coloaded nanoparticulate drug delivery systems for topical anesthetic analgesic therapy: a comparison between solid lipid nanoparticles and nanostructured lipid carriers

    Directory of Open Access Journals (Sweden)

    You P

    2017-09-01

    Full Text Available Peijun You,1 Ran Yuan,2 Chuanyu Chen1 1Department of Anesthesiology, Shandong Jining No 1 People’s Hospital, Shandong, People’s Republic of China; 2Department of Anesthesiology, Affiliated Hospital of Jining Medical College, Jining, Shandong, People’s Republic of China Purpose: Topical anesthesia analgesic therapy has diverse applicability in solving the barrier properties of skin and unfavorable physicochemical properties of drugs. Lidocaine (LID combined with prilocaine (PRI has been used as a topical preparation for dermal anesthesia for treatment of conditions such as paresthesia. Materials and methods: In this study, for combination anesthesia and overcoming the drawbacks of LID and PRI, respectively, LID- and PRI-loaded solid lipid nanoparticles (SLNs and nanostructured lipid carriers (NLCs were prepared and characterized by determination of their particle size, drug loading capacity, stability, in vitro drug release behavior and in vitro cellular viability. Ex vivo skin permeation and in vivo anesthesia analgesic efficiency of these two systems were also evaluated and compared. Results: Results revealed that combination delivery of the dual drugs exhibited more remarkable efficiency than signal drug-loaded systems. SLN systems have better ex vivo skin permeation ability than NLCs. NLC systems revealed a stronger in vivo anesthesia analgesic effect than SLN systems. Conclusion: It can be concluded that SLNs and NLCs have different advantages, and that both carriers are promising dual drug delivery systems for topical anesthetic analgesic therapy. Keywords: topical anesthesia, prilocaine, lidocaine, solid lipid nanoparticles, nanostructured lipid carriers

  20. Isobolographic analysis of caramiphen and lidocaine on spinal anesthesia in rats.

    Science.gov (United States)

    Chen, Yu-Wen; Chu, Chin-Chen; Chen, Yu-Chung; Wang, Jhi-Joung; Hung, Ching-Hsia

    2010-01-18

    The aims of the study were to evaluate the spinal anesthetic effect of caramiphen and also assess spinal anesthetic interactions of caramiphen with lidocaine. Lidocaine, a common local anesthetic, was used as control. Dose-dependent responses of intrathecal caramiphen on spinal anesthesia were compared with lidocaine in rats. The interactions of caramiphen with lidocaine were evaluated via an isobolographic analysis. Caramiphen and lidocaine produced a dose-dependent local anesthetic effect as spinal anesthesia. On a 50% effective dose (ED(50)) basis, the spinal anesthetic effect of caramiphen was more potent than lidocaine (P<0.01 for each comparison). Co-administration of caramiphen with lidocaine produced an additive effect. Caramiphen and lidocaine are known to have local anesthetic effects as spinal anesthesia in rats. The spinal anesthetic effects of adding caramiphen to lidocaine are similar to the combinations of other anesthetics with lidocaine.

  1. Anesthetics impact the resolution of inflammation.

    Directory of Open Access Journals (Sweden)

    Nan Chiang

    Full Text Available BACKGROUND: Local and volatile anesthetics are widely used for surgery. It is not known whether anesthetics impinge on the orchestrated events in spontaneous resolution of acute inflammation. Here we investigated whether a commonly used local anesthetic (lidocaine and a widely used inhaled anesthetic (isoflurane impact the active process of resolution of inflammation. METHODS AND FINDINGS: Using murine peritonitis induced by zymosan and a systems approach, we report that lidocaine delayed and blocked key events in resolution of inflammation. Lidocaine inhibited both PMN apoptosis and macrophage uptake of apoptotic PMN, events that contributed to impaired PMN removal from exudates and thereby delayed the onset of resolution of acute inflammation and return to homeostasis. Lidocaine did not alter the levels of specific lipid mediators, including pro-inflammatory leukotriene B(4, prostaglandin E(2 and anti-inflammatory lipoxin A(4, in the cell-free peritoneal lavages. Addition of a lipoxin A(4 stable analog, partially rescued lidocaine-delayed resolution of inflammation. To identify protein components underlying lidocaine's actions in resolution, systematic proteomics was carried out using nanospray-liquid chromatography-tandem mass spectrometry. Lidocaine selectively up-regulated pro-inflammatory proteins including S100A8/9 and CRAMP/LL-37, and down-regulated anti-inflammatory and some pro-resolution peptides and proteins including IL-4, IL-13, TGF-â and Galectin-1. In contrast, the volatile anesthetic isoflurane promoted resolution in this system, diminishing the amplitude of PMN infiltration and shortening the resolution interval (Ri approximately 50%. In addition, isoflurane down-regulated a panel of pro-inflammatory chemokines and cytokines, as well as proteins known to be active in cell migration and chemotaxis (i.e., CRAMP and cofilin-1. The distinct impact of lidocaine and isoflurane on selective molecules may underlie their opposite

  2. Doxepin Has a Potent and Long-Acting Spinal Anesthetic Effect in Rats

    Directory of Open Access Journals (Sweden)

    Bor-Chin Cheng

    2006-02-01

    Full Text Available Doxepin, a tricyclic antidepressant, was recently found to be effective in the treatment of various acute and chronic painful conditions. However, the mechanism of its actions was not clear, especially when involving the spine. The aim of our study was to evaluate the spinal anesthetic effect of doxepin. Two commonly used traditional local anesthetics, bupivacaine and lidocaine, were used as controls. The potencies and durations of the drugs' action were evaluated in male Sprague-Dawley rats. We found that intrathecally administered doxepin, like bupivacaine and lidocaine, produced dose-related spinal anesthetic effects on motor activity, proprioception, and nociception. Among the three drugs, doxepin produced spinal anesthetic effects in rats more potent than that of lidocaine (p < 0.001, in each comparison and longer than that of bupivacaine and lidocaine (p < 0.001, in each comparison. The spinal activity of doxepin may provide some explanation of its clinical effect in pain management.

  3. Tumescent Liposuction without Lidocaine

    Science.gov (United States)

    Goldman, Joshua J.; Fang, Xin-Hua; Williams, Shelley J.; Baynosa, Richard C.

    2016-01-01

    Background: Our previous study demonstrated that lidocaine has a negative impact on adipose-derived stem cell (ASC) survival. Currently for large-volume liposuction, patients often undergo general anesthesia; therefore, lidocaine subcutaneous anesthesia is nonessential. We hypothesized that removing lidocaine from tumescent might improve stromal vascular fraction (SVF) and ASC survival from the standard tumescent with lidocaine. Ropivacaine is also a commonly used local anesthetic. The effect of ropivacaine on ASC survival was examined. Methods: Adults who underwent liposuction on bilateral body areas were included (n = 10). Under general anesthesia, liposuction on 1 area was conducted under standard tumescent with lidocaine. On the contralateral side, liposuction was conducted under the modified tumescent without lidocaine. Five milliliters of lipoaspirate were processed for the isolation of SVF. The adherent ASCs were counted after 24 hours of SVF culture. Apoptosis and necrosis of SVF cells were examined by Annexin/propidium iodide staining and analyzed by flow cytometry. Results: Average percentage of live SVF cells was 68.0% ± 4.0% (28.5% ± 3.8% of apoptosis and 3.4% ± 1.0% of necrosis) in lidocaine group compared with 86.7% ± 3.7% (11.5% ± 3.1% of apoptosis and 1.8% ± 0.7% of necrosis) in no-lidocaine group (P = 0.002). Average number of viable ASC was also significantly lower (367,000 ± 107) in lidocaine group compared with that (500,000 ± 152) in no-lidocaine group (P = 0.04). No significant difference was found between lidocaine and ropivacaine on ASC cytotoxicity. Conclusions: Removing lidocaine from tumescent significantly reduced SVF and ASC apoptosis in the lipoaspirate. We recommend tumescent liposuction without lidocaine, particularly if patient’s lipoaspirate will be used for fat grafting. PMID:27622097

  4. fMRI investigation of the effect of local and systemic lidocaine on noxious electrical stimulation-induced activation in spinal cord.

    Science.gov (United States)

    Zhao, Fuqiang; Williams, Mangay; Welsh, Denise C; Meng, Xiangjun; Ritter, Amy; Abbadie, Catherine; Cook, Jacquelynn J; Reicin, Alise S; Hargreaves, Richard; Williams, Donald S

    2009-09-01

    Spinal cord fMRI offers an excellent opportunity to quantify nociception using neuronal activation induced by painful stimuli. Measurement of the magnitude of stimulation-induced activation, and its suppression with analgesics can provide objective measures of pain and efficacy of analgesics. This study investigates the feasibility of using spinal cord fMRI in anesthetized rats as a pain assay to test the analgesic effect of locally and systemically administered lidocaine. Blood volume (BV)-weighted fMRI signal acquired after intravenous injection of ultrasmall superparamagnetic iron oxide (USPIO) particles was used as an indirect readout of the neuronal activity. Transcutaneous noxious electrical stimulation was used as the pain model. BV-weighted fMRI signal could be robustly quantified on a run-by-run basis, opening the possibility of measuring pharmacodynamics (PD) of the analgesics with a temporal resolution of approximately 2 min. Local administration of lidocaine was shown to ablate all stimulation-induced fMRI signals by the total blockage of peripheral nerve transmission, while the analgesic effect of systemically administered lidocaine was robustly detected after intravenous infusion of approximately 3mg/kg, which is similar to clinical dosage for human. This study establishes spinal cord fMRI as a viable assay for analgesics. With respect to the mode of action of lidocaine, this study suggests that systemic lidocaine, which is clinically used for the treatment of neuropathic pain, and believed to only block the peripheral nerve transmission of abnormal neural activity (ectopic discharge) originating from the damaged peripheral nerves, also blocks the peripheral nerve transmission of normal neural activity induced by transcutaneous noxious electrical stimulation.

  5. Conformation and kinetic characteristics of interactions between local anesthetics and aqueous solutions of hydroxypropylmethylcellulose.

    Science.gov (United States)

    Galenko-Yaroshevskii, A P; Varlashkina, I A; Takhchidi, Kh P; Malyugin, B E; Dukhanin, A S

    2007-05-01

    Conformation and kinetic characteristics of the interactions of local anesthetics lidocaine (xycaine), tetracaine (dicaine), bupivacaine, and new RU-1117 compound with proven anesthetic activity with Visiton (1% hydroxypropylmethylcellulose in phosphate buffer) were studied. It was found that complex formation between the local anesthetics and hydroxypropylmethylcellulose is a time-dependent reversible process. The equilibrium is attained within 2.5-8.0 h and depends on the chemical nature of local anesthetic.

  6. A prospective, randomized, double-blind comparison of the anesthetic efficacy of two percent lidocaine with 1:100,000 and 1:50,000 epinephrine and three percent mepivacaine in the intraoral, infraorbital nerve block.

    Science.gov (United States)

    Berberich, Gerhard; Reader, Al; Drum, Melissa; Nusstein, John; Beck, Mike

    2009-11-01

    The purpose of this prospective, randomized, double-blind study was to compare the anesthetic efficacy of 2% lidocaine with 1:100,000 epinephrine, 2% lidocaine with 1:50,000 epinephrine, and 3% mepivacaine in the intraoral, infraorbital nerve block. Forty subjects randomly received intraoral, infraorbital nerve blocks by using a cartridge of 2% lidocaine with 1:100,000 or 1:50,000 epinephrine and a cartridge of 3% mepivacaine at 3 separate appointments spaced at least 1 week apart. The anteriors, premolars, and first molar were pulp tested in 4-minute cycles for a total of 60 minutes. The intraoral, infraorbital nerve block was ineffective in providing profound pulpal anesthesia of the maxillary central incisor, lateral incisor, and first molar. Successful pulpal anesthesia of the canine and first and second premolars ranged from 75%-92% by using 2% lidocaine with 1:100,000 and 1:50,000 epinephrine. However, pulpal anesthesia did not last for 60 minutes. The use of 3% mepivacaine provided a shorter duration of anesthesia than the lidocaine formulations with epinephrine in the canines and premolars.

  7. Benzocaine-loaded polymeric nanocapsules: study of the anesthetic activities.

    Science.gov (United States)

    De Melo, Nathalie Ferreira Silva; De Araújo, Daniele Ribeiro; Grillo, Renato; Moraes, Carolina Morales; De Matos, Angélica Prado; de Paula, Eneida; Rosa, André Henrique; Fraceto, Leonardo Fernandes

    2012-03-01

    This paper describes a comparison of different polymeric nanocapsules (NCs) prepared with the polymers poly(D,L-lactide-co-glycolide), poly(L-lactide) (PLA), and poly(ε-caprolactone) and used as carrier systems for the local anesthetic (LA) benzocaine (BZC). The systems were characterized and their anesthetic activities investigated. The results showed particle size distributions with polydispersity indices below 0.135, average diameters up to 120 nm, zeta potentials up to -30 mV, and entrapment efficiencies around 70%. Formulations of BZC using the polymeric NCs presented slower release profiles, compared with that of free BZC. Slowest release (release constant, k = 0.0016 min(-1)) was obtained using the PLA NC system. Pharmacological evaluation showed that encapsulation of BZC in PLA NCs prolonged its anesthetic action. This new formulation could potentially be used in future applications involving the gradual release of local anesthetics (LAs).

  8. Lidocaine alters the input resistance and evokes neural activity in crayfish sensory neurons.

    Science.gov (United States)

    Keceli, M B; Purali, N

    2007-03-01

    Lidocaine, a use-dependent Na(+) channel blocker, paradoxically evokes neural activation in the slowly adapting stretch receptor organ of crayfish at 5-10 mmol/l concentration. For elucidating the underlying mechanisms of this paradoxical effect, a series of conventional electrophysiological experiments were performed in the stretch receptor neurons of crayfish. In the presence of tetrodotoxin, lidocaine did not evoke impulse activity, however, a slowly developing and dose-dependent depolarization occurred in both the rapidly and slowly adapting stretch receptors. Similar effects were observed by perfusion of equivalent concentrations of benzocaine but not of procaine or prilocaine. Lidocaine did not evoke neural activity in the rapidly adapting neuron which fires action potential(s) in response to rapid changes in membrane potential. Slowly developing mode of the depolarization indicated the reason why only depolarization but not action potential responses were observed in the rapidly adapting neuron. The depolarizing effect of lidocaine was independent from any ionic channel or exchanger system. However, lidocaine and benzocaine but not procaine and prilocaine evoked a dose-dependent alteration in the input resistance of the neuron. It was proposed that the principal mechanism of the effect could stem from a change in the physical properties of the neuronal membrane.

  9. Lidocaine-induced apoptosis of gingival fibroblasts: participation of cAMP and PKC activity.

    Science.gov (United States)

    Villarruel, Emmanuel Quinteros; Borda, Enri; Sterin-Borda, Leonor; Orman, Betina

    2011-08-01

    Local anaesthetics are drugs that prevent or relieve pain by interrupting nervous conduction and are the most commonly used drugs in dentistry. Their main targets of action are voltage-dependent Na+ channels. The Na+ channel is modulated by phosphorylation of two enzymes: PKA (protein kinase A) and PKC (protein kinase C). We studied the ability of lidocaine to modulate programmed cell death of human gingival fibroblasts and the mechanisms involved in this process. Lidocaine (10-5 to 10-7 M) stimulated apoptosis in primary cultures and the caspase-3 activity in a concentration-dependent manner. The stimulatory effect of lidocaine on apoptosis was attenuated in the presence of HA 1004 (PKA inhibitor) and stimulated by staurosporine and Go 6976 (PKC inhibitors). Lidocaine-induced apoptotic nuclei correlated positively with cAMP accumulation and negatively with PKC activity. These results show that lidocaine promotes apoptosis in human gingival fibroblasts at concentrations used for local anaesthesia. The mechanism involves PKA stimulation and PKC inhibition, which in turn stimulates caspase-3 and leads to programmed cell death.

  10. Prolongation of lidocaine-induced epidural anesthesia by medium molecular weight hyaluronic acid formulations: pharmacodynamic and pharmacokinetic studies in the rabbit.

    Science.gov (United States)

    Doherty, M M; Hughes, P J; Korszniak, N V; Charman, W N

    1995-04-01

    We evaluated the utility of medium molecular weight hyaluronic acid for prolonging the local anesthetic activity of lidocaine in a rabbit model of epidural analgesia. Equiviscous formulations were prepared as either a physical mixture of lidocaine hydrochloride and sodium hyaluronate (where drug release occurred via diffusion) or as a lidocaine-hyaluronate complex (where drug release occurred via diffusional and electrostatic processes). The novel hyaluronic acid formulations were functionally evaluated, relative to lidocaine solution, in an intact, conscious rabbit model. The hyaluronate formulations were well tolerated. The duration of sensory block and loss of weight-bearing was prolonged twofold by the lidocaine-hyaluronate complex relative to the solution (P lidocaine plasma concentration-time data indicated that the rate of drug absorption from the lidocaine-hyaluronate complex was decreased fourfold relative to the solution (P hyaluronic acid may offer advantages for the prolongation of epidural analgesia.

  11. Tedisamil and lidocaine enhance each other's antiarrhythmic activity against ischaemia-induced arrhythmias in rats

    OpenAIRE

    Sarraf, Guilda; Barrett, Terrance D; Walker, Michael J A

    2003-01-01

    Combinations of the action potential-widening drug tedisamil (Class III antiarrhythmic activity), and the inactivated state sodium channel blocker lidocaine (Class Ib antiarrhythmic activity) were assessed for antiarrhythmic actions in a rat model of ischaemia-induced arrhythmias and for electrophysiological actions in normal rat myocardial tissue.Both tedisamil and lidocaine dose-dependently suppressed ischaemia-induced arrhythmias. The ED50 values were 3.0±1.3 and 4.9±0.6 μmol kg−1 min−1, r...

  12. Neuroprotective and anti-inflammatory effects of lidocaine in kainic acid-injected rats.

    Science.gov (United States)

    Chiu, Kuan Ming; Lu, Cheng Wei; Lee, Ming Yi; Wang, Ming Jiuh; Lin, Tzu Yu; Wang, Su Jane

    2016-05-04

    Lidocaine, the most commonly used local anesthetic, inhibits glutamate release from nerve terminals. Given the involvement of glutamate neurotoxicity in the pathogenesis of various neurological disorders, this study investigated the role of lidocaine in hippocampal neuronal death and inflammatory events induced by an i.p. injection of kainic acid (KA) (15 mg/kg), a glutamate analog. The results showed that KA significantly led to neuronal death in the CA3 pyramidal layers of the hippocampus and this effect was attenuated by the systemic administration of lidocaine (0.8 or 4 mg/kg, i.p.) 30 min before KA injection. Moreover, KA-induced microglia activation and gene expression of proinflammatory cytokines, namely, interleukin-1β, interleukin-6, and tumor necrosis factor-α, in the hippocampus were reduced by the lidocaine pretreatment. Altogether, the results suggest that lidocaine can effectively treat glutamate excitotoxicity-related brain disorders.

  13. Systemic Lidocaine Shortens Length of Hospital Stay After Colorectal Surgery

    Science.gov (United States)

    Herroeder, Susanne; Pecher, Sabine; Schönherr, Marianne E.; Kaulitz, Grit; Hahnenkamp, Klaus; Friess, Helmut; Böttiger, Bernd W.; Bauer, Harry; Dijkgraaf, ↶oMarcel G. W.; Durieux, Marcel E.; Hollmann, Markus W.

    2007-01-01

    Objective: To characterize the beneficial effects of perioperative systemic lidocaine on length of hospital stay, gastrointestinal motility, and the inflammatory response after colorectal surgery. Summary Background Data: Surgery-induced stimulation of the inflammatory response plays a major role in the development of several postoperative disorders. Local anesthetics possess anti-inflammatory activity and are thought to positively affect patients' outcome after surgery. This double-blinded, randomized, and placebo-controlled trial aimed to evaluate beneficial effects of systemic lidocaine and to provide insights into underlying mechanisms. Methods: Sixty patients undergoing colorectal surgery, not willing or unable to receive an epidural catheter, were randomly assigned to lidocaine or placebo treatment. Before induction of general anesthesia, an intravenous lidocaine bolus (1.5 mg/kg) was administered followed by a continuous lidocaine infusion (2 mg/min) until 4 hours postoperatively. Length of hospital stay, gastrointestinal motility, and pain scores were recorded and plasma levels or expression of pro- and anti-inflammatory mediators determined. Results: Lidocaine significantly accelerated return of bowel function and shortened length of hospital stay by one day. No difference could be observed in daily pain ratings. Elevated plasma levels of IL-6, IL-8, complement C3a, and IL-1ra as well as expression of CD11b, l- and P-selectin, and platelet-leukocyte aggregates were significantly attenuated by systemic lidocaine. Conclusions: Perioperative intravenous lidocaine not only improved gastrointestinal motility but also shortened length of hospital stay significantly. Anti-inflammatory activity modulating the surgery-induced stress response may be one potential mechanism. Systemic lidocaine may thus provide a convenient and inexpensive approach to improve outcome for patients not suitable for epidural anesthesia. PMID:17667496

  14. [Neurotoxicity of intrathecal lidocaine].

    Science.gov (United States)

    Pavón, A; Anadón Senac, P

    2001-01-01

    Lidocaine is a local anesthetic belonging to the amide group and has been administered intrathecally for over 40 years. Although no serious complications had been attributed to lidocaine before the 1990s, subarachnoid administration is now the subject of controversy following its implication in numerous cases of neurological complication. The clinical pictures described in the literature are cauda equina syndrome, which is mainly associated with continuous subarachnoid anesthesia through microcatheters, and transitory neurological symptoms, also termed radicular irritation syndrome and associated with single injections. The literature reveals a clearly higher incidence of transitory neurological symptoms with lidocaine than with other local anesthetics. Although the underlying mechanism remains unclear, the main hypotheses being the neurotoxicity of lidocaine itself or the malpositioning of the paravertebral musculature due to extreme relaxation. The various factors that can lead to neuropathy have been widely described in the many articles reporting complications. Arthroscopy and lithotomy positions are significantly related to the appearance of symptoms, as are early ambulation or the use of small-gauge needles or pencil-point needles. Further clinical studies should be undertaken. No consensus on subarachnoid administration of lidocaine has emerged, yet no alternative has been demonstrated to be safe and to offer similar pharmacological features (short latency, short duration of action and good muscle relaxation). Prilocaine, mepivacaine, articaine and bupivacaine at low doses have been suggested as alternatives.

  15. Tedisamil and lidocaine enhance each other's antiarrhythmic activity against ischaemia-induced arrhythmias in rats.

    Science.gov (United States)

    Sarraf, Guilda; Barrett, Terrance D; Walker, Michael J A

    2003-08-01

    1. Combinations of the action potential-widening drug tedisamil (Class III antiarrhythmic activity), and the inactivated state sodium channel blocker lidocaine (Class Ib antiarrhythmic activity) were assessed for antiarrhythmic actions in a rat model of ischaemia-induced arrhythmias and for electrophysiological actions in normal rat myocardial tissue. 2. Both tedisamil and lidocaine dose-dependently suppressed ischaemia-induced arrhythmias. The ED(50) values were 3.0+/-1.3 and 4.9+/-0.6 micro mol kg(-1) min(-1), respectively. 3. Combinations of the two drugs acted synergistically such that the ED(50) for tedisamil was reduced to 0.8+/-0.2 micro mol kg(-1) min(-1) in the presence of 2 micro mol kg(-1) min(-1) lidocaine. Similarly, the ED(50) for lidocaine was reduced to 0.7+/-0.2 micro mol kg(-1) min(-1) in the presence of 2 micro mol kg(-1) min(-1) tedisamil (both Plidocaine produced a leftward shift in the dose-response curve for tedisamil's effect on effective refractory period (Plidocaine had no effect on its own. These data indicate that the synergistic actions of combinations of tedisamil and lidocaine were mediated, at least in part, by extension of effective refractory period in normal myocardial tissue. 5. In contrast to the strategy of developing drugs that are selective for a single electrophysiological mechanism, the results of the present study suggest that effective antiarrhythmic drugs might be developed by optimising the combination of two complimentary electrophysiological mechanisms (i.e., action potential-prolonging activity and inactivated state sodium channel blockade).

  16. Tolperisone: evaluation of the lidocaine-like activity by molecular modeling.

    Science.gov (United States)

    Fels, G

    1996-04-01

    Tolperisone (1), a muscle relaxant with lidocaine-like activity, was compared to lidocaine (2) by molecular modeling methods. Conformational search analysis has been employed to find the global minima of these compounds along with numerous low energy conformations from which specific conformers were extracted that show good superimposition of the structural features important for protein binding. Two additional compounds, mepi- (3) and bupivacaine (4), were included in the analysis to validate the method as these ligands show very close structural and pharmacological relationship to lidocaine (2) and are assumed to bind to an identical site. As a result we find conformers of all four ligands that have exactly the same position and orientation of the potential sites for hydrogen bonding with the rest of the molecule showing close comparison of the three-dimensional geometry. Semiempirical calculations furthermore reveal good agreement of the electrostatic potentials of these conformations indicating similar interactions with a receptor. We conclude that tolperisone (1) and lidocaine (2) despite their chemical divergence can still attach to identical protein binding sites.

  17. Lidocaine Induces Apoptosis and Suppresses Tumor Growth in Human Hepatocellular Carcinoma Cells In Vitro and in a Xenograft Model In Vivo.

    Science.gov (United States)

    Xing, Wei; Chen, Dong-Tai; Pan, Jia-Hao; Chen, Yong-Hua; Yan, Yan; Li, Qiang; Xue, Rui-Feng; Yuan, Yun-Fei; Zeng, Wei-An

    2017-05-01

    Recent epidemiologic studies have focused on the potential beneficial effects of regional anesthetics, and the differences in cancer prognosis may be the result of anesthetics on cancer biologic behavior. However, the function and underlying mechanisms of lidocaine in hepatocellular carcinoma both in vitro and in vivo have been poorly studied. Human HepG2 cells were treated with lidocaine. Cell viability, colony formation, cell cycle, and apoptosis were assessed. The effects of lidocaine on apoptosis-related and mitogen-activated protein kinase protein expression were evaluated by Western blot analysis. The antitumor activity of lidocaine in hepatocellular carcinoma with or without cisplatin was investigated with in vitro experiments and also with animal experiments. Lidocaine inhibited the growth of HepG2 cells in a dose- and time-dependent manner. The authors also found that lidocaine arrested cells in the G0/G1 phase of the cell cycle (63.7 ± 1.7% vs. 72.4 ± 3.2%; P = 0.0143) and induced apoptosis (1.7 ± 0.3% vs. 5.0 ± 0.7%; P = 0.0009). Lidocaine may exert these functions by causing an increase in Bax protein and activated caspase-3 and a corresponding decrease in Bcl-2 protein through the extracellular signal-regulated kinase 1/2 and p38 pathways. More importantly, for the first time, xenograft experiments (n = 8 per group) indicated that lidocaine suppressed tumor development (P lidocaine vs. control) and enhanced the sensitivity of cisplatin (P = 0.0008; lidocaine plus cisplatin vs. cisplatin). The authors' findings suggest that lidocaine may exert potent antitumor activity in hepatocellular carcinoma. Furthermore, combining lidocaine with cisplatin may be a novel treatment option for hepatocellular carcinoma.

  18. Lidocaine-induced CNS toxicity--a case report.

    Science.gov (United States)

    Chiang, Y Y; Tseng, K F; Lih, Y W; Tsai, T C; Liu, C T; Leung, H K

    1996-12-01

    Lidocaine is the first local anesthetic of the amide type to be introduced to clinical practice. It is a versatile drug and in anesthesia, is the most commonly used local anesthetic because of its aptness of potency, rapid onset, moderate duration of action and topical activity. It is relatively safe and useful in many other clinical settings. Unfortunately, systemic intoxication and psychotic reaction associated with its use often occur because of its popularity and wider safety margin, for which guide in use is often ignored and overdose becomes commonplace. Moreover, due to its universality in use seldom reports have recently dealt with lidocaine, particularly regarding its toxic reaction. Here, we present a case of lidocaine intoxication occurring during circumcision for a reviewal of the problem. A healthy young male, weighing 65 kg, underwent circumcision for phimosis under penile block with 2% lidocaine which totaled 600 mg. Twenty minutes after injection the patient developed headache, tinnitus, visual and auditory disturbances. Muscle twitching over the mouth angles, trismus and rigidity of extremities were also noted. Later in the course he became restless, agitative, hallucinative, talkative, and verbose with repetitious words. The whole course of the disorder lasted about 5 h. It was believed that lidocaine-induced CNS intoxication, manifested by psychotic reaction broke out. Treatment with thiopental was not very impressive. Also, we took this opportunity to discuss and review the toxic reaction associated with the use of lidocaine, its risk factors, mechanism, treatment and prevention. The complicated associations of lidocaine-induced CNS toxic reaction with central control of behavior and the neurotransmitter systems (adrenergic, dopaminergic and serotonin) were also touched.

  19. A comparative evaluation of anesthetic efficacy of articaine 4% and lidocaine 2% with anterior middle superior alveolar nerve block and infraorbital nerve block: An in vivo study

    Science.gov (United States)

    Saraf, Suma Prahlad; Saraf, Prahlad Annappa; Kamatagi, Laxmikant; Hugar, Santosh; Tamgond, Shridevi; Patil, Jayakumar

    2016-01-01

    Background: The ideal maxillary injection should produce a rapid onset of profound pulpal anesthesia for multiple teeth from a single needle penetration. The main objective is to compare the efficacy of articaine 4% and lidocaine 2% and to compare anterior middle superior alveolar nerve block (AMSANB) and infraorbital nerve block (IONB) for anesthesia of maxillary teeth. Materials and Methods: Forty patients undergoing root canal treatment of maxillary anteriors and premolars were included and randomly divided into four groups of ten each. Group I: patients receiving AMSANB with articaine, Group II: Patients receiving IONB with articaine, Group III: Patients receiving AMSANB with lidocaine, Group IV: Patients receiving IONB with lidocaine. The scores of onset of anesthesia and pain perception were statistically analyzed. Results: Onset of action was fastest for articaine with AMSANB and slowest for lidocaine with IONB by Tukey's test. A significant change was observed in the electrical pulp test readings at onset and at 30 min by paired t-test. All patients experienced mild pain during the procedure recorded by visual analog scale. Conclusion: Articaine 4% proved to be more efficacious than lidocaine 2%, and AMSANB was more advantageous than IONB in securing anesthesia of maxillary anteriors and premolars. PMID:27994313

  20. Intrathecal lidocaine pretreatment attenuates immediate neuropathic pain by modulating Nav1.3 expression and decreasing spinal microglial activation

    Science.gov (United States)

    2011-01-01

    Background Intrathecal lidocaine reverses tactile allodynia after nerve injury, but whether neuropathic pain is attenuated by intrathecal lidocaine pretreatment is uncertain. Methods Sixty six adult male Sprague-Dawley rats were divided into three treatment groups: (1) sham (Group S), which underwent removal of the L6 transverse process; (2) ligated (Group L), which underwent left L5 spinal nerve ligation (SNL); and (3) pretreated (Group P), which underwent L5 SNL and was pretreated with intrathecal 2% lidocaine (50 μl). Neuropathic pain was assessed based on behavioral responses to thermal and mechanical stimuli. Expression of sodium channels (Nav1.3 and Nav1.8) in injured dorsal root ganglia and microglial proliferation/activation in the spinal cord were measured on post-operative days 3 (POD3) and 7 (POD7). Results Group L presented abnormal behavioral responses indicative of mechanical allodynia and thermal hyperalgesia, exhibited up-regulation of Nav1.3 and down-regulation of Nav1.8, and showed increased microglial activation. Compared with ligation only, pretreatment with intrathecal lidocaine before nerve injury (Group P), as measured on POD3, palliated both mechanical allodynia (p lidocaine prior to SNL blunts the response to noxious stimuli by attenuating Nav1.3 up-regulation and suppressing activation of spinal microglia. Although its effects are limited to 3 days, intrathecal lidocaine pretreatment can alleviate acute SNL-induced neuropathic pain. PMID:21676267

  1. Local anesthetics as pain therapy in horses.

    Science.gov (United States)

    Doherty, Thomas J; Seddighi, M Reza

    2010-12-01

    This article describes the rationale behind the use of systemically administered lidocaine as an analgesic. The analgesic efficacy of intravenously administered lidocaine is well documented by studies in human patients and laboratory animals. The mechanism by which systemically administered lidocaine produces analgesia is uncertain but is thought to include action at sodium, calcium, and potassium channels and the N-methyl-D-aspartate acid receptor. In addition, the anti-inflammatory actions of lidocaine are important in producing analgesia because inflammatory mediators augment neuronal excitability. The available studies of systemically administered lidocaine in horses provide evidence for the analgesic and anesthetic effects of intravenous lidocaine in this species.

  2. Faster onset and more comfortable injection with alkalinized 2% lidocaine with epinephrine 1:100,000.

    Science.gov (United States)

    Malamed, Stanley F; Tavana, Susan; Falkel, Mic

    2013-02-01

    The pH of lidocaine with epinephrine in dental cartridges ranges between 2.9 and 4.4. In this pH range, less than 0.1% of the anesthetic is in the de-ionized or "active" form. The acidity of the anesthetic may delay onset and contribute to injection pain. The study compared anesthetic latency and injection pain for alkalinized versus non-alkalinized anesthetic in inferior alveolar nerve blocks (IANBs). The study buffered the anesthetic directly in the cartridges using a mixing pen device. The study included 20 participants, each receiving one control and one test IANB injection. The control solution was non-alkalinized 2% lidocaine/epinephrine 1:100,000 at pH 3.85. The test solution was 2% lidocaine/ epinephrine 1:100,000 alkalinized to pH 7.31. Latency was measured using endodontic ice confirmed with an electric pulp tester (EPT), and injection pain was measured using a visual analog scale (VAS). ONSET TIME: With the alkalinized anesthetic, 71% of participants achieved pulpal analgesia in 2 minutes or less. With non-alkalinized anesthetic, 12% achieved pulpal analgesia in 2 minutes or less (P = 0.001). The average time to pulpal analgesia for the non-alkalinized anesthetic was 6:37 (range 0:55 to 13:25). Average time to pulpal analgesia for alkalinized anesthetic was 1:51 (range 0:11 to 6:10) (P = 0.001). INJECTION PAIN RESULTS: 72% of the participants rated the alkalinized injection as more comfortable, 11% rated the non-alkalinized injection as more comfortable, and 17% reported no preference (P = 0.013). Forty-four percent of the patients receiving alkalinized anesthetic rated the injection pain as zero ("no pain") on a 100-mm VAS, compared to 6% of the patients who received non-alkalinized anesthetic (P = 0.056). Alkalinizing lidocaine with epinephrine toward physiologic pH immediately before injection significantly reduces anesthetic onset time and increases the comfort of the injection. Clinicians can begin procedures more quickly and give a more comfortable

  3. New lidocaine lozenge as topical anesthesia compared to lidocaine viscous oral solution before upper gastrointestinal endoscopy

    DEFF Research Database (Denmark)

    Mogensen, Stine; Treldal, Charlotte; Feldager, Erik

    2012-01-01

    To evaluate the effect and acceptance of a new lidocaine lozenge compared with a lidocaine viscous oral solution as a pharyngeal anesthetic before upper gastrointestinal endoscopy (UGE), a diagnostic procedure commonly performed worldwide during which many patients experience severe discomfort mo...

  4. Lidocaine action and conformational changes in cytoskeletal protein network in human red blood cells.

    Science.gov (United States)

    Nishiguchi, E; Hamada, N; Shindo, J

    1995-11-03

    The mechanism of action of lidocaine, which is commonly used clinically as a local anesthetic, was studied in human red blood cells. The influx of [14C]lidocaine through the cell membrane induced reversible transformation of human red blood cells from discocytes to stomatocytes. This change in shape depended on the lidocaine concentration and required both ATP and carbonic anhydrase. The lidocaine-induced shape change occurred as a result of spectrin aggregation, which altered the intracellular environment of the human red blood cells, mediated by carbonic anhydrase and activation of vacuolar type H(+)-ATPase (V-ATPase). Lidocaine controlled the influx of 22Na into the human red blood cells in a concentration-dependent manner. When incubated in media containing 6-chloro-9-[(4-diethylamino)-1-methyl-butyl]amino-2-methoxyacridine (mepacrine), an inhibitor of Na+ channels, human red blood cells changed shape from discocytes to stomatocytes and the intracellular pH decreased. This phenomenon was very similar to the shape change induced by lidocaine. These results suggest that the mode of action of lidocaine is related to a conformational change in the cytoskeletal protein network.

  5. Comparison Effcacy of Local Anesthetic Tetracaineand Lidocaine in Nasal Endoscopy%局麻药物丁卡因与利多卡因在鼻内镜中的疗效比较

    Institute of Scientific and Technical Information of China (English)

    张良

    2016-01-01

    Objective To determine whether there is a difference in the efficacy between atomized 1% tetracaine and 2% lidocaine as a topical anesthetic prior to transnasal endoscopy.Methods A total of 100 patients received oxymetazoline and were randomized to receive either 1%tetracaine or 2% lidocaine prior to transnasal endoscopy. Immediately following the procedure, participants completed a survey assessing level of discomfort and other adverse symptoms pertaining to the procedure using a 10-point visual analog scale. Results There were no significant differences in scores between the lidocaine and tetracaine groups. There were also no signiifcant differences between genders in overall scores and in the lidocaine and tetracaine subgroups. Older patients demonstrated significantly less discomfort or a sensation of bad taste overall. In contrast to patients receiving lidocaine, older patients receiving tetracaine experienced signiifcantly less overall pain and discomfort, unpleasant taste, and dyspnea. Conclusion In patients undergoing transnasal endoscopy, use of either 1%tetracaine or 2%lidocaine has similar effect. Tetracaine may be a better choice in older patients.%目的鼻内镜常用于耳鼻咽喉科的诊断与治疗。患者通常在该手术之前进行局部麻醉,以减轻不适,提高可视化。在优化术中患者体验方面,哪种局部麻醉是最有效的,目前还没有共识。因此,本研究的目的是为了明确雾化1%丁卡因和作为鼻内镜前局部麻醉药的2%利多卡因之间的疗效是否存在差异。方法共有100例患者在鼻内镜前接受羟甲唑啉,并随机分组,分别接受1%丁卡因或2%利多卡因。手术后,患者立即进行调查量表的评分以及与手术有关不良症状级别的评估。结果利多卡因和丁卡因组之间的各条目评分没有明显统计学差异。在全部人群中不同性别之间的各条目评分之间没有统计学差异,在利多卡因组和丁卡因组

  6. Intrathecal lidocaine pretreatment attenuates immediate neuropathic pain by modulating Nav1.3 expression and decreasing spinal microglial activation

    Directory of Open Access Journals (Sweden)

    Wang Hung-Chen

    2011-06-01

    Full Text Available Abstract Background Intrathecal lidocaine reverses tactile allodynia after nerve injury, but whether neuropathic pain is attenuated by intrathecal lidocaine pretreatment is uncertain. Methods Sixty six adult male Sprague-Dawley rats were divided into three treatment groups: (1 sham (Group S, which underwent removal of the L6 transverse process; (2 ligated (Group L, which underwent left L5 spinal nerve ligation (SNL; and (3 pretreated (Group P, which underwent L5 SNL and was pretreated with intrathecal 2% lidocaine (50 μl. Neuropathic pain was assessed based on behavioral responses to thermal and mechanical stimuli. Expression of sodium channels (Nav1.3 and Nav1.8 in injured dorsal root ganglia and microglial proliferation/activation in the spinal cord were measured on post-operative days 3 (POD3 and 7 (POD7. Results Group L presented abnormal behavioral responses indicative of mechanical allodynia and thermal hyperalgesia, exhibited up-regulation of Nav1.3 and down-regulation of Nav1.8, and showed increased microglial activation. Compared with ligation only, pretreatment with intrathecal lidocaine before nerve injury (Group P, as measured on POD3, palliated both mechanical allodynia (p p 1.3 up-regulation (p = 0.003, and mitigated spinal microglial activation (p = 0.026 by inhibiting phosphorylation (activation of p38 MAP kinase (p = 0.034. p38 activation was also suppressed on POD7 (p = 0.002. Conclusions Intrathecal lidocaine prior to SNL blunts the response to noxious stimuli by attenuating Nav1.3 up-regulation and suppressing activation of spinal microglia. Although its effects are limited to 3 days, intrathecal lidocaine pretreatment can alleviate acute SNL-induced neuropathic pain.

  7. Lidocaine lozenges for pharyngeal anesthesia during upper gastrointestinal endoscopy: A randomized controlled trial

    Directory of Open Access Journals (Sweden)

    Avinash Supe

    2014-01-01

    Full Text Available Background and Objectives: A novel lozenge formulation with advantages of ease of drug administration, palatable taste and improved patient compliance could be the preferred mode of topical pharyngeal anesthesia during upper gastrointestinal endoscopy (UGE. This randomized, open-label, active-controlled study was conducted to evaluate the efficacy and safety of lidocaine lozenges versus lidocaine spray in the diagnostic gastroduodenal endoscopy in Indian patients. Subjects and Methods: Two hundred and forty-seven patients of either sex (18-80 years undergoing diagnostic gastroduodenal endoscopy were randomized either to; lidocaine lozenge 200 mg or lidocaine spray 200 mg to be applied as a single dose before gastroduodenal endoscopy. Ease of procedure, level of gag reflex, ease of application of the local anesthetic, and investigators global assessment were the primary efficacy endpoints. Need for rescue medication and patient′s global assessment were secondary efficacy endpoints. The incidence of any adverse event was the safety endpoint. Between groups, comparison was done by using appropriate statistical test. Results: Investigator reported significantly lesser procedural difficulty (P = 0.0007 and suppressed gag reflex (P < 0.0001 during UGE with lidocaine lozenge compared to spray. Ease of application of local anesthetic was reported easy in significantly more patients as compared with lidocaine spray (P = 0.001. Global assessment by patient and physician was favorable toward lozenge. Incidences of adverse events were similar in both the groups. Conclusions: The study suggests that lidocaine lozenges are an easier way of applying local oropharyngeal anesthesia, produces better suppression of gag reflex and makes the procedure easier when compared with lidocaine spray.

  8. Lidocaine induces ROCK-dependent membrane blebbing and subsequent cell death in rabbit articular chondrocytes.

    Science.gov (United States)

    Maeda, Tsutomu; Toyoda, Futoshi; Imai, Shinji; Tanigawa, Hitoshi; Kumagai, Kousuke; Matsuura, Hiroshi; Matsusue, Yoshitaka

    2016-05-01

    Local anesthetics are administered intraarticularly for pain control in orthopedic clinics and surgeries. Although previous studies have shown that local anesthetics can be toxic to chondrocytes, the underlying cellular mechanisms remain unclear. The present study investigates acute cellular responses associated with lidocaine-induced toxicity to articular chondrocytes. Rabbit articular chondrocytes were exposed to lidocaine and their morphological changes were monitored with live cell microscopy. The viability of chondrocytes was evaluated using a fluorescence based LIVE/DEAD assay. Acute treatment of chondrocytes with lidocaine (3-30 mM) induced spherical protrusions on the cell surface (so called "membrane blebbing") in a time- and concentration-dependent manner. The concentration-response relationship for the lidocaine effect was shifted leftward by elevating extracellular pH, as expected for the non-ionized lidocaine being involved in the bleb formation. ROCK (Rho-kinase) inhibitors Y-27632 and fasudil completely prevented the lidocaine-induced membrane blebbing, suggesting that ROCK activation is required for bleb formation. Caspase-3 levels were unchanged by 10 mM lidocaine (p = 0.325) and a caspase inhibitor z-VAD-fmk did not affect the lidocaine-induced blebbing (p = 0.964). GTP-RhoA levels were significantly increased (p ROCK inhibitors or a myosin-II inhibitor blebbistatin (p ROCK-dependent membrane blebbing and thereby produces a cytotoxic effect on chondrocytes. © 2015 Orthopaedic Research Society. Published by Wiley Periodicals, Inc. J Orthop Res 34:754-762, 2016.

  9. Analysis of the action of lidocaine on insect sodium channels.

    Science.gov (United States)

    Song, Weizhong; Silver, Kristopher S; Du, Yuzhe; Liu, Zhiqi; Dong, Ke

    2011-01-01

    A new class of sodium channel blocker insecticides (SCBIs), which include indoxacarb, its active metabolite, DCJW, and metaflumizone, preferably block inactivated states of both insect and mammalian sodium channels in a manner similar to that by which local anesthetic (LA) drugs block mammalian sodium channels. A recent study showed that two residues in the cockroach sodium channel, F1817 and Y1824, corresponding to two key LA-interacting residues identified in mammalian sodium channels are not important for the action of SCBIs on insect sodium channels, suggesting unique interactions of SCBIs with insect sodium channels. However, the mechanism of action of LAs on insect sodium channels has not been investigated. In this study, we examined the effects of lidocaine on a cockroach sodium channel variant, BgNa(v)1-1a, and determined whether F1817 and Y1824 are also critical for the action of LAs on insect sodium channels. Lidocaine blocked BgNa(v)1-1a channels in the resting state with potency similar to that observed in mammalian sodium channels. Lidocaine also stabilized both fast-inactivated and slow-inactivated states of BgNa(v)1-1a channels, and caused a limited degree of use- and frequency-dependent block, major characteristics of LA action on mammalian sodium channels. Alanine substitutions of F1817 and Y1824 reduced the sensitivity of the BgNa(v)1-1a channel to the use-dependent block by lidocaine, but not to tonic blocking and inactivation stabilizing effects of lidocaine. Thus, similar to those on mammalian sodium channels, F1817 and Y1824 are important for the action of lidocaine on cockroach sodium channels. Our results suggest that the receptor sites for lidocaine and SCBIs are different on insect sodium channels.

  10. Abdominal expiratory muscle activity in anesthetized vagotomized neonatal rats.

    Science.gov (United States)

    Iizuka, Makito

    2009-05-01

    The pattern of respiratory activity in abdominal muscles was studied in anesthetized, spontaneously breathing, vagotomized neonatal rats at postnatal days 0-3. Anesthesia (2.0% isoflurane, 50% O(2)) depressed breathing and resulted in hypercapnia. Under this condition, abdominal muscles showed discharge late in the expiratory phase (E2 activity) in most rats. As the depth of anesthesia decreased, the amplitude of discharges in the diaphragm and abdominal muscles increased. A small additional burst frequently occurred in abdominal muscles just after the termination of diaphragmatic inspiratory activity (E1 or postinspiratory activity). Since this E1 activity is not often observed in adult rats, the abdominal respiratory pattern likely changes during postnatal development. Anoxia-induced gasping after periodic expiratory activity without inspiratory activity, and in most rats, abdominal expiratory activity disappeared before terminal apnea. These results suggest that a biphasic abdominal motor pattern (a combination of E2 and E1 activity) is a characteristic of vagotomized neonatal rats during normal respiration.

  11. Anesthetic efficacy of X-tip intraosseous injection using 2% lidocaine with 1:80,000 epinephrine in patients with irreversible pulpitis after inferior alveolar nerve block: A clinical study

    Directory of Open Access Journals (Sweden)

    Pushpendra Kumar Verma

    2013-01-01

    Full Text Available Introduction: The inferior alveolar nerve block (IAN is the most frequently used mandibular injection technique for achieving local anesthesia in endodontics. Supplemental injections are essential to overcome failure of IAN block in patients with irreversible pulpitis. Aim: To evaluate the anesthetic efficacy of X-tip intraosseous injection (2% lidocaine with 1:80,000 epinephrine in patients with irreversible pulpitis in mandibular posterior teeth when conventional IAN block failed. Materials and Methods: Thirty emergency patients diagnosed with irreversible pulpitis in a mandibular posterior tooth received an IAN block and experienced moderate to severe pain on endodontic access or initial instrumentation. The X-tip system was used to administer 1.8 ml of 2% lidocaine with 1:80,000 epinephrine. The success of X-tip intraosseous injection was defined as none or mild pain (Heft-Parker visual analogue scale ratings < 54 mm on endodontic access or initial instrumentation. Results: Ninety-three percent of X-tip injections were successful and 7% were unsuccessful. Discomfort rating for X-tip perforation: 96.66% patients reported none or mild pain, whereas 3.34% reported moderate to severe pain. For discomfort rating during solution deposition, 74.99% patients reported none or mild pain and 24.92% reported moderate to severe pain. Ninety-six percent of the patients had subjective/objective increase in heart rate. Conclusions: Supplemental X-tip intraosseous injection using 2% lignocaine with 1:80,000 epinephrine has a statistically significant influence in achieving pulpal anesthesia in patients with irreversible pulpitis.

  12. Activated endothelial interleukin-1beta, -6, and -8 concentrations and intercellular adhesion molecule-1 expression are attenuated by lidocaine.

    LENUS (Irish Health Repository)

    Lan, Wei

    2012-02-03

    Endothelial cells play a key role in ischemia reperfusion injury. We investigated the effects of lidocaine on activated human umbilical vein endothelial cell (HUVEC) interleukin (IL)-1beta, IL-6, and IL-8 concentrations and intercellular adhesion molecule-1 (ICAM-1) expression. HUVECs were pretreated with different concentrations of lidocaine (0 to 0.5 mg\\/mL) for 60 min, thereafter tumor necrosis factor-alpha was added at a concentration of 2.5 ng\\/mL and the cells incubated for 4 h. Supernatants were harvested, and cytokine concentrations were analyzed by enzyme-linked immunosorbent assay. Endothelial ICAM-1 expression was analyzed by using flow cytometry. Differences were assessed using analysis of variance and post hoc unpaired Student\\'s t-test where appropriate. Lidocaine (0.5 mg\\/mL) decreased IL-1beta (1.89 +\\/- 0.11 versus 4.16 +\\/- 1.27 pg\\/mL; P = 0.009), IL-6 (65.5 +\\/- 5.14 versus 162 +\\/- 11.5 pg\\/mL; P < 0.001), and IL-8 (3869 +\\/- 785 versus 14,961 +\\/- 406 pg\\/mL; P < 0.001) concentrations compared with the control. IL-1beta, IL-6, and IL-8 concentrations in HUVECs treated with clinically relevant plasma concentrations of lidocaine (0.005 mg\\/mL) were similar to control. ICAM-1 expression on lidocaine-treated (0.05 mg\\/mL) HUVECs was less than on controls (198 +\\/- 52.7 versus 298 +\\/- 50.3; Mean Channel Fluorescence; P < 0.001). Activated endothelial IL-1beta, IL-6, and IL-8 concentrations and ICAM-1 expression are attenuated only by lidocaine at concentrations larger than clinically relevant concentrations.

  13. Molecularly imprinted polymer in microextraction by packed sorbent for the simultaneous determination of local anesthetics: lidocaine, ropivacaine, mepivacaine and bupivacaine in plasma and urine samples.

    Science.gov (United States)

    Daryanavard, Seyed Mosayeb; Jeppsson-Dadoun, Amin; Andersson, Lars I; Hashemi, Mahdi; Colmsjö, Anders; Abdel-Rehim, Mohamed

    2013-11-01

    This study presents the use of molecularly imprinted polymer (MIP) as packing material for microextraction by packed syringe (MEPS) to achieve higher extraction selectivity. Pentycaine was used as template for MIP. Development and validation of the determination of lidocaine, ropivacaine, mepivacaine and bupivacaine in human plasma and urine samples utilizing MIP-MEPS and liquid chromatography-tandem mass spectrometry (LC-MS/MS) were carried out. The MEPS MIP-cartridge could be used for 100 extractions before it was discarded. The extraction recovery ranged from 60 to 80%. The correlation coefficients values were >0.999 for all assays using lidocaine, ropivacaine, mepivacaine and bupivacaine in the calibration range 5-2000 nmol/L. The accuracy of the studied compounds, given as a percentage variation from the nominal concentration values, ranged from -4.9 to 8.4% using plasma and urine samples. The between-batch precision, given as the relative standard deviation, at three different concentrations (quality control samples) was ranged from -4.7 to 14.0% and from 1.8 to 12.7% in plasma and urine, respectively. The lower limit of quantification and limit of detection of the studied substances were 5.0 and 1.0 nm, respectively. Copyright © 2013 John Wiley & Sons, Ltd.

  14. 静脉麻醉药抑制利多卡因致大鼠惊厥作用的比较%Comparisons of anticonvulsant action of intravenous anesthetics against lidocaine-induced convulsion in rats

    Institute of Scientific and Technical Information of China (English)

    王春平; 张山; 刘红梅; 韩倩

    2012-01-01

    Objective To compare the anticonvulsant action of midazolam, propofol, etomidate and thiopental on lidocaine-induced convulsion in rats. Methods Thirty-six male Wistar rats weighing (250±20) g were equally randomized into 6 groups: (1) control group (group C); (2) lidocaine group (group L: lidocaine 4 mg ·k1 ·min-1 until convulsion); (3) lidocaine and propofol group (group P, lidocaine and propofol 12.5 mg/kg), (4) lidocaine and etomidate group (group E: lidocaine and etomidate 1. 85 mg/kg) , (5) lidocaine and midazolam group (group M: lidocaine and midazolam 0. 65 mg/kg) , (6) lidocaine and thiopental group (group T: lidocaine and thiopental 30. 85 mg/kg). Animals were decapitated 2 hours after convulsion and the brains were removed. One side of hippocampus was obtained for detecting expressions of c-fos protein. The other side was obtained to measure the concentration of nitric oxide (NO) and the activity of nitric oxide synthase (N()S). Results The c-fos positive cells, the concentration of NO and the activity of NOS increased significantly in group L compared with group C (P<0. 05). The c-fos positive cells, the NO concentration and the activity of NO.S were significantly lower in groups P, M, E and T compared with group L (P<0. 05), and especially in groups M and T. Conclusion Propofol, midazolam, etomidate and thiopental can inhibit lidocaine-induced convulsion in rats and it is more significant by midazolam and thiopental.%目的 比较静脉麻醉药丙泊酚、依托咪酯、咪达唑仑及硫喷妥钠拮抗利多卡因致大鼠惊厥的作用.方法 雄性Wistar大鼠36只,体重(250±20)g,随机均分为六组:空白对照组(C组)、利多卡因组(L组:利多卡因4 mg· kg- 1·min-1)、利多卡因+丙泊酚组(P组:利多卡因+丙泊酚12.5ng/kg)、利多卡因+依托咪酯组(E组:利多卡因+依托咪酯1.85mg/kg)、利多卡因+咪达唑仑组(M组:利多卡因+咪达唑仑0.65mg/kg)和利多卡因+硫喷妥钠组(T组:

  15. Pharmacological profile of N-(2,6-dichlorophenyl)-2-(4-methyl-1-piperidinyl)acetamide, a novel analogue of lidocaine.

    Science.gov (United States)

    Déciga-Campos, Myrna; Navarrete-Vázquez, Gabriel; López-Muñoz, Francisco Javier; Librowski, Tadeusz; Sánchez-Recillas, Amanda; Yañez-Pérez, Victor; Ortiz-Andrade, Rolffy

    2016-06-15

    N-(2,6-Dichlorophenyl)-2-(4-methyl-1-piperidinyl)acetamide (LIA), a lidocaine analogue, has potential applications in treating neuropathic pain. The aim of this work was to characterize the pharmacological activity of LIA related with central nervous system and cardiovascular activity. Anesthetic effect was tested in guinea pigs and mice. Ambulatory activity, anti-anxiety effect, sodium pentobarbital (PB)-induced hypnosis and pentylenetetrazol (PTZ)-induced seizures test were evaluated in mice to determine the possible central nervous system activity. The cardiovascular activities in vivo and ex vivo were analyzed in rats. LIA (2%) presents, similar to lidocaine (2%), anesthetic activity on the corneal reflex, infiltration anesthesia and tail immersion test. LIA (1-100mg/kg, i.p.), similar to lidocaine (1-100mg/kg, i.p.), presents a dose-dependent sedative-hypnotic effect in mice. Both compounds did not produce anti-anxiety activity in mice. LIA did not prevent PTZ-induced seizures. However, LIA itself did not produce seizures at high doses in mice, as lidocaine does. LIA is a vasorelaxant compound for smooth muscle cells and presents hypotensive effect in vivo without increments to the heart rate significantly. High doses of lidocaine produce seizures and vasoconstriction. In this study, we found that LIA shares a similar pharmacological profile as lidocaine's but without the primary adverse effects of seizures and vasoconstriction. Copyright © 2016 Elsevier Inc. All rights reserved.

  16. Clinical efficacy of lidocaine, mepivacaine, and articaine for local infiltration.

    Science.gov (United States)

    Srisurang, Suttapreyasri; Narit, Leepong; Prisana, Pripatnanont

    2011-02-01

      To assess and compare the efficacy of single buccal and palatal infiltration of lidocaine, mepivacaine, or articaine with 1:100 000 epinephrine by maxillary anesthetic injection.   A double-blinded, randomized, clinical trial was conducted with 33 patients undergoing upper premolar extraction. The patients were randomly allocated into one of three groups, according to the local anesthetic agent used: 2% lidocaine, 2% mepivacaine, or 4% articaine, all with 1:100 000 epinephrine, and were blinded to the anesthetic used. The extent of anesthetization, pulpal anesthetization in adjacent teeth, pain on injection, and adverse effects of the anesthetic agents were assessed.   The extent of anesthetization produced by 4% articaine (42 mm) was statistically more significant (P ≤ 0.05) than 2% lidocaine (33 mm) and 2% mepivacaine (32.5 mm). The successful anesthetization of adjacent teeth occurred more often in the articaine group than in the lidocaine and mepivacine groups, although not to a statistically-significant extent. The pain scores for the injections were comparable between the three groups.   Local anesthetization using 4% articaine with 1:100 000 epinephrine covers a wider area of soft tissue and adjacent teeth than 2% lidocaine or 2% mepivacaine with 1:100 000 epinephrine, which is sufficient for the extraction of one or two teeth. © 2010 Blackwell Publishing Asia Pty Ltd.

  17. Preparation and characterization of lidocaine rice gel for oral application.

    Science.gov (United States)

    Okonogi, Siriporn; Kaewpinta, Adchareeya; Yotsawimonwat, Songwut; Khongkhunthian, Sakornrat

    2015-12-01

    The objective of the present study was to prepare buccal anesthetic gels using rice as gelling agent. Rice grains of four rice varieties, Jasmine (JM), Saohai (SH), Homnil (HN), and Doisket (DS) were chemically modified. Buccal rice gels, containing lidocaine hydrochloride as local anesthetic drug were formulated using the respective modified rice varieties. The gels were evaluated for outer appearance, pH, color, gel strength, foaming property, adhesion, in vitro drug release and in vivo efficacy. It was found that the developed rice gels possessed good texture. Rice varieties showed influence on gel strength, color, turbidity, adhesive property, release property, and anesthetic efficacy. JM gel showed the lowest turbidity with light transmission of 86.76 ± 1.18% whereas SH gel showed the highest gel strength of 208.78 ± 10.42 g/cm(2). Lidocaine hydrochloride can cause a decrease in pH and adhesive property but an increase in turbidity of the gels. In vitro drug release profile within 60 min of lidocaine SH gel and lidocaine HN gel showed that lidocaine could be better released from SH gel. Evaluation of in vivo anesthetic efficacy in 100 normal volunteers indicates that both lidocaine rice gels have high efficacy but different levels. Lidocaine SH gel possesses faster onset of duration and longer duration of action than lidocaine HN gel.

  18. Lidocaine Metabolism and Toxicity: A Laboratory Experiment for Dental Students.

    Science.gov (United States)

    Kusek, J. C.

    1980-01-01

    A laboratory exercise for dental students is presented using a toxic dose of lidocaine in place of an anesthetic dose of pentobarbital. The use of lidocaine demonstrates its toxic and lethal actions and increases the relevance of the experience for dental students. (Author/MLW)

  19. Capsaicin facilitates carotid sinus baroreceptor activity in anesthetized rats

    Institute of Scientific and Technical Information of China (English)

    HaoZHANG; Yi-xianLIU; Yu-mingWU; Ze-minWANG; Rui-rongHE

    2004-01-01

    AIM: To study the effect of capsaicin on carotid sinus baroreceptor activity (CBA). METHODS: The functional curve of carotid baroreceptor (FCCB) was constructed and the functional parameters of carotid sinus baroreceptor were measured by recording sinus nerve afferent discharge in anesthetized rats with perfused isolated carotid sinus. RESULTS: Low-concentration of capsaicin (0.2μmol/L) had no significant effect on CBA, while perfusion of the isolated carotid sinus with middle-concentration of capsaicin (1μmol/L) could shift FCCB to the left and upward,with peak slope (PS) increased from (2.47%±0.14%)/mmHg to (2.88%±0.10%)/mmHg (P<0.05) and peak integral value of carotid sinus nerve discharge (PIV) enhanced from 211%±5% to 238%±6% (P<0.01). The threshold pressure (TP) and saturation pressure (SP) were significantly decreased from 68.0±1.1 to 62.7±1.0mmHg (P<0.01) and from 171.0±1.6 to 165.0±0.6 mmHg (P<0.01). By perfusing with high-concentration of capsaicin (5μmol/L), FCCB was shifted to the left and upward further and the changes of the functional parameters such as PS, TP, and SP were concentration-dependent. Pretreatment with ruthenium red (100μmol/L), an antagonist of vanilloid receptor subtype 1 (VR1), blocked the effect of capsaicin on CBA. Preperfusion with glibenclamide(20μmol/L), a KATP channel blocker, could eliminate the effect of capsaicin on CBA. CONCLUSION: Capsaicin exerts a facilitatory role on the isolated carotid baroreceptor in a concentration-dependent manner. The facilitatory action of capsaicin may be attributed to the opening of KATP channels mediated by VR1.

  20. Capsaicin facilitates carotid sinus baroreceptor activity in anesthetized rats

    Institute of Scientific and Technical Information of China (English)

    Hao ZHANG; Yi-xian LIU; Yu-ming WU; Ze-min WANG; Rui-rong HE

    2004-01-01

    AIM: To study the effect of capsaicin on carotid sinus baroreceptor activity (CBA). METHODS: The functional curve of carotid baroreceptor (FCCB) was constructed and the functional parameters of carotid sinus baroreceptor were measured by recording sinus nerve afferent discharge in anesthetized rats with perfused isolated carotid sinus.RESULTS: Low-concentration of capsaicin (0.2 μmol/L) had no significant effect on CBA, while perfusion of the isolated carotid sinus with middle-concentration of capsaicin (1 μmol/L) could shift FCCB to the left and upward,with peak slope (PS) increased from (2.47 %±0.14 %)/mmHg to (2.88 %±0.10 %)/mmHg (P<0.05) and peak integral value of carotid sinus nerve discharge (PIV) enhanced from 211%±5 % to 238 %±6 % (P<0.01). The threshold pressure (TP) and saturation pressure (SP) were significantly decreased from 68.0±1.1 to 62.7±1.0mmHg (P<0.01) and from 171.0±1.6 to 165.0±0.6 mmHg (P<0.01). By perfusing with high-concentration of capsaicin (5 μmol/L), FCCB was shifted to the left and upward further and the changes of the functional parameters such as PS, TP, and SP were concentration-dependent. Pretreatment with ruthenium red (100 μmol/L), an antagonist of vanilloid receptor subtype 1 (VR1), blocked the effect of capsaicin on CBA. Preperfusion with glibenclamide(20 μmol/L), a KATp channel blocker, could eliminate the effect of capsaicin on CBA. CONCLUSION: Capsaicin exerts a facilitatory role on the isolated carotid baroreceptor in a concentration-dependent manner. The facilitatory action of capsaicin may be attributed to the opening of KATP channels mediated by VR1.

  1. A Prospective, Comparative Study of the Pain of Local Anesthesia Using 2% Lidocaine, 2% Lidocaine With Epinephrine, and 2% Lidocaine With Epinephrine-Bupivicaine Mixture for Eyelid Surgery.

    Science.gov (United States)

    Han, Jung-Woo; Nah, Seung Kwan; Lee, Sang Yeul; Kim, Chang Yeom; Yoon, Jin Sook; Jang, Sun Young

    A mixture of 2% lidocaine with epinephrine and bupivacaine was developed to achieve the fast-onset anesthetic effect of lidocaine and the long-lasting effect of bupivacaine. The authors compared pain scores between 2% lidocaine, 2% lidocaine with epinephrine, and 2% lidocaine with epinephrine-bupivicaine mixture during local anesthesia for eyelid surgeries. This was a double-blind, randomized, prospective, comparative study. In total, 120 consecutive patients (43 males, 77 females, mean age = 47.2 ± 21.2) who underwent bilateral eyelid surgery under subcutaneous anesthesia were asked to report pain scores for each eye during the first injection of anesthesia. Each patient was randomly assigned to receive 1 of the 3 anesthetic agents in 1 eyelid, and 1 of the remaining 2 agents in the other. The pH values of the 2% lidocaine, 2% lidocaine with epinephrine, and 2% lidocaine with epinephrine-bupivicaine mixture were 6.23 ± 0.21, 4.21 ± 0.37, and 3.87 ± 0.19, respectively. The pain scores of each were 4.3 ± 1.8, 5.1 ± 1.8, and 5.7 ± 1.9, respectively. The 2% lidocaine with epinephrine produced a statistically significantly higher pain score than 2% lidocaine (p = 0.044, generalized estimating equation method). The mixture also showed a significantly higher pain score than 2% lidocaine (p = 0.003, generalized estimating equation method). Epinephrine seemed to increase subjective pain scores. Compared with 2% lidocaine with epinephrine, 2% lidocaine with epinephrine-bupivicaine mixture was not significantly different in terms of subjective symptoms or pH.

  2. Qualification of fMRI as a biomarker for pain in anesthetized rats by comparison with behavioral response in conscious rats.

    Science.gov (United States)

    Zhao, Fuqiang; Williams, Mangay; Bowlby, Mark; Houghton, Andrea; Hargreaves, Richard; Evelhoch, Jeffrey; Williams, Donald S

    2014-01-01

    fMRI can objectively measure pain-related neural activities in humans and animals, providing a valuable tool for studying the mechanisms of nociception and for developing new analgesics. However, due to its extreme sensitivity to subject motion, pain fMRI studies are performed in animals that are immobilized, typically with anesthesia. Since anesthesia could confound the nociceptive processes, it is unknown how well nociceptive-related neural activities measured by fMRI in anesthetized animals correlate with nociceptive behaviors in conscious animals. The threshold to vocalization (VT) in response to an increasing noxious electrical stimulus (NES) was implemented in conscious rats as a behavioral measure of nociception. The antinociceptive effect of systemic (intravenous infusion) lidocaine on NES-induced fMRI signals in anesthetized rats was compared with the corresponding VT in conscious rats. Lidocaine infusion increased VT and suppressed the NES-induced fMRI signals in most activated brain regions. The temporal characteristics of the nociception signal by fMRI and by VT in response to lidocaine infusion were highly correlated with each other, and with the pharmacokinetics (PK) of lidocaine. These results indicate that the fMRI activations in these regions may be used as biomarkers of acute nociception in anesthetized rats. Interestingly, systemic lidocaine had no effect on NES-induced fMRI activations in the primary somatosensory cortex (S1), a result that warrants further investigation.

  3. [Magistral prepared lidocaine-gel for topical aplication on skin].

    Science.gov (United States)

    Sklenár, Zbynĕk; Horácková, Katerína; Bakhouche, Hana; Slanar, Ondrej

    2012-08-01

    Due to a limited availability of industrially manufactured products containing local anesthetics for skin application and an increased demand for lidocaine-containing gel applicable prior to a product containing capsaicin for neuropathic pain treatment, it is necessary to prepare a topical semi-solid preparation containing the local anesthetic in pharmacies. Our aim was to create a mixed system of a hydrophilic gel with the emulsified drug, using excipients to decrease the lidocaine melting point, thereby creating a eutectic mixture with a high concentration of lidocaine in the oil phase. Based on bibliographic data, thymol creating a binary eutectic system containing lidocaine has been chosen. After addition of other excipients, an emulsion system was prepared and the drug was stabilized in the oil phase by a mixed nonionic emulsifier and carbomera. For the optimal anesthetic effects, the pH value should be adjusted; trometamol has been chosen as a suitable basic reacting excipient. Based on the addition of different amounts of trometamol, pH values of individual emulgels have been measured and the final composition of lidocaine emulgel has been created. A recipe for a 5 % lidocaine emulgel with the pH value of 9.1 has been created, based on the gel-forming substance carbomera with an emulsion of the oil phase containing a eutectic mixture of lidocaine and thymol, with an addition of ethanol and propylenglycol, stabilized by a mixed nonionic emulsifier. The advantage is the absence of other local anesthetics.

  4. Pain fiber anesthetic reduces brainstem Fos after tooth extraction.

    Science.gov (United States)

    Badral, B; Davies, A J; Kim, Y H; Ahn, J S; Hong, S D; Chung, G; Kim, J S; Oh, S B

    2013-11-01

    We recently demonstrated that pain-sensing neurons in the trigeminal system can be selectively anesthetized by co-application of QX-314 with the TRPV1 receptor agonist, capsaicin (QX cocktail). Here we examined whether this new anesthetic strategy can block the neuronal changes in the brainstem following molar tooth extraction in the rat. Adult male Sprague-Dawley rats received infiltration injection of anesthetic 10 min prior to lower molar tooth extraction. Neuronal activation was determined by immunohistochemistry for the proto-oncogene protein c-Fos in transverse sections of the trigeminal subnucleus caudalis (Sp5C). After tooth extraction, c-Fos-like immunoreactivity (Fos-LI) detected in the dorsomedial region of bilateral Sp5C was highest at 2 hrs (p tooth extraction; reduced Fos-LI was also observed with the conventional local anesthetic lidocaine. Pulpal anesthesia by infiltration injection was confirmed by inhibition of the jaw-opening reflex in response to electrical tooth pulp stimulation. Our results suggest that the QX cocktail anesthetic is effective in reducing neuronal activation following tooth extraction. Thus, a selective pain fiber 'nociceptive anesthetic' strategy may provide an effective local anesthetic option for dental patients in the clinic.

  5. Cardiovascular Complications Resulting from Topical Lidocaine Application

    Directory of Open Access Journals (Sweden)

    Feng Lin

    2008-12-01

    Full Text Available Topical lidocaine is one of the most commonly used anesthetics in the emergency department (ED. The advantages of topical anesthesia include ease of application, minimal discomfort on administration, and rapid onset of anesthesia. Systemic toxic effects after topical lidocaine application are rare. We present a case of a man aged 48 years with no history of heart disease and no evidence of bradycardia in previous electrocardiograms. The patient had sprayed lidocaine solution on the glans of his penis before sex during the 2 weeks prior to admission. Cardiovascular adverse events occurred, including chest tightness and bradycardia. After 2 hours conservative treatment at our ED, his symptoms were alleviated. He was discharged from the ED without any medication. The case suggests that detailed patient histories are necessary for accurate diagnosis and that rapid diagnosis and implementation of treatment is necessary for successful patient outcomes in cases of cardiovascular complications resulting from topical lidocaine application.

  6. Trigeminal nerve injury associated with injection of local anesthetics

    DEFF Research Database (Denmark)

    Hillerup, Søren; Jensen, Rigmor H.; Ersbøll, Bjarne Kjær

    2011-01-01

    anesthetics (from 1995 through 2007), 292 reports to the Danish Medicines Agency, Copenhagen, Denmark, of adverse reactions to local anesthetic drugs, and a clinical sample of 115 patients with NSD associated with local anesthetics. The authors assessed lidocaine 2 percent, mepivacaine 2 percent and 3 percent...

  7. Intraperitoneal lidocaine & tenoxicam for pain relief after gynaecological laparoscopy

    Institute of Scientific and Technical Information of China (English)

    Ibrahim A Abdelazim; Mohammed Al-Kadi; Maged Mahmoud El Shourbagy; Ahmed Abdelazim Mohamed; Mohannad Lutfi Abu faza

    2013-01-01

    Objective: To detect the effect of intra-peritoneal instillation of local anesthetic with or without NSAIDs on pain relief after gynecological laparoscopy. Methods: Seventy five patients scheduled for laparoscopy were included in the study and randomly divided into three groups. At the end of the laparoscopic procedure, 100 mL normal saline in the first group, or 100 mL normal saline contains 200 mg lidocaine in the second group, or 100 mL normal slaine containing 200 mg lidocaine and 20 mg tenoxicam in the third group were splashed into the pelvis by the surgeon. Post-operative pain were monitored and compared. Results: The incidence and severity of immediate postoperative shoulder pain reduced from 44% of patients scoring 2-5 in saline group to 16% scoring 2-3 in lidocaine group and 8% scoring 2-3 in lidocaine-tenoxicam group. Compared with saline group, abdominal pain scores were significantly lower in lidocaine group and lidocaine-tenoxicam group over 24 hours after surgery. At 12 and 24 hours after surgery, abdominal pain scores were significantly reduced in lidocaine-tenoxicam group compared with lidocaine group. No pain on deep respiration was reported in 84%, and 68% in lidocaine-tenoxicam and lidocaine groups respectively compared to 12% in those in the saline group. The mean time to first request for analgesia was increased from (2.3 ±1.9) hours in saline group to (4.4 ± 2.4) hours in lidocaine group and to (8.3 ± 10.2) hours in lidocaine-tenoxicam group. Conclusion: Intraperitoneal balanced analgesia (local anesthetics ± NSAIDS) is a simple and safe technique for analgesia following gynaecological Laparoscopy.

  8. 21 CFR 346.16 - Analgesic, anesthetic, and antipruritic active ingredients.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 5 2010-04-01 2010-04-01 false Analgesic, anesthetic, and antipruritic active ingredients. 346.16 Section 346.16 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) DRUGS FOR HUMAN USE ANORECTAL DRUG PRODUCTS FOR OVER-THE-COUNTER HUMAN USE Active Ingredients § 346.16 Analgesic,...

  9. 21 CFR 348.10 - Analgesic, anesthetic, and antipruritic active ingredients.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 5 2010-04-01 2010-04-01 false Analgesic, anesthetic, and antipruritic active ingredients. 348.10 Section 348.10 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) DRUGS FOR HUMAN USE EXTERNAL ANALGESIC DRUG PRODUCTS FOR OVER-THE-COUNTER HUMAN USE Active Ingredients § 348.10 Analgesi...

  10. A comparison between articaine HCl and lidocaine HCl in pediatric dental patients.

    Science.gov (United States)

    Malamed, S F; Gagnon, S; Leblanc, D

    2000-01-01

    Three identical single-dose, randomized, double-blind, parallel-group, active-controlled multicenter studies were conducted to compare the safety and efficacy of articaine HCl (4% with epinephrine 1:100,000) to that of lidocaine HCl (2% with epinephrine 1:100,000) in patients aged 4 years to 79 years, with subgroup analysis on subjects 4 to < 13 years. Fifty subjects under the age of 13 years were treated in the articaine group and 20 subjects under the age of 13 were treated with lidocaine. Subjects were randomized in a 2:1 ratio to receive articaine or lidocaine. Efficacy was determined on a gross scale immediately following the procedure by having both the subject and investigator rate the pain experienced by the subject during the procedure using a visual analog scale (VAS). Safety was evaluated by measuring vital signs before and after administration of anesthetic (1 and 5 minutes post-medication and at the end of the procedure) and by assessing adverse events throughout the study. Adverse events were elicited during telephone follow-up at 24 hours and 7 days after the procedure. Pediatric patients received equal volumes, but higher mg/kg doses, of articaine than lidocaine during both simple and complex dental procedures. Pain ratings: Articaine: VAS (Visual Analogue Scale) scores (from 0 to 10 cm) by patients 4 to < 13 years of age were 0.5 for simple procedures and 1.1 for complex procedures, and average investigator scores were 0.4 and 0.6 for simple and complex procedures, respectively. Lidocaine: patients 0.7 (simple) and 2.3 (complex); investigators 0.3 (simple) and 2.8 (complex). Adverse events: No serious adverse events related to the articaine occurred. The only adverse event considered related to articaine was accidental lip injury in one patient. VAS scores indicate that articaine is an effective local anesthetic in children and that articaine is as effective as lidocaine when measured on this gross scale. Articaine 4% with epinephrine 1:100,000 is

  11. Anesthetic activity of Brazilian native plants in silver catfish (Rhamdia quelen

    Directory of Open Access Journals (Sweden)

    Lenise de Lima Silva

    Full Text Available There is an increasing demand for inexpensive and safe anesthetics that can reduce fish stress caused by some procedures such as capture and handling. In this context, the present study evaluated the potential of essential oils (EO of three Brazilian native plants (Hesperozygis ringens, Lippia sidoides and Ocotea acutifolia as anesthetics for the silver catfish - Rhamdia quelen. Moreover, an analysis was made of the chemical composition of these oils and their influence on stress parameter. EO of H. ringens and O. acutifolia were effective as anesthetics, without behavioral side effects. EO of O. acutifolia (150 µL L-1 promoted an increase in blood glucose level. Regarding to the composition, pulegone accounts for 96.63% of the EO of H. ringens, and caryophyllene oxide amounts to 56.90% of the EO of O. acutifolia. Two chemotypes, thymol and carvacrol (68.40% and 67.89%, respectively were verified for EO of L. sidoides. Both samples of EO of L. sidoides showed anesthetic activity in silver catfish, but exposure also caused loss of mucus and mortality. Thus, only the EO of H. ringens and O. acutifolia are advised for anesthetic use

  12. An Anesthetic Drug Demonstration and an Introductory Antioxidant Activity Experiment with "Eugene, the Sleepy Fish"

    Science.gov (United States)

    Barcena, Homar; Chen, Peishan

    2016-01-01

    Students are introduced to spectrophotometry in comparing the antioxidant activity of pure eugenol and oil of cloves from a commercial source using a modified ferric reducing antioxidant power (FRAP) assay. The extraction of the essential oil from dried cloves is demonstrated to facilitate discussions on green chemistry. The anesthetic properties…

  13. Lidocaine toxicity in primary afferent neurons from the rat.

    Science.gov (United States)

    Gold, M S; Reichling, D B; Hampl, K F; Drasner, K; Levine, J D

    1998-05-01

    Evidence from both clinical studies and animal models suggests that the local anesthetic, lidocaine, is neurotoxic. However, the mechanism of lidocaine-induced toxicity is unknown. To test the hypothesis that toxicity results from a direct action of lidocaine on sensory neurons we performed in vitro histological, electrophysiological and fluorometrical experiments on isolated dorsal root ganglion (DRG) neurons from the adult rat. We observed lidocaine-induced neuronal death after a 4-min exposure of DRG neurons to lidocaine concentrations as low as 30 mM. Consistent with an excitotoxic mechanism of neurotoxicity, lidocaine depolarized DRG neurons at concentrations that induced cell death (EC50 = 14 mM). This depolarization occurred even though voltage-gated sodium currents and action potentials were blocked effectively at much lower concentrations. (EC50 values for lidocaine-induced block of tetrodotoxin-sensitive and -resistant voltage-gated sodium currents were 41 and 101 microM, respectively.) At concentrations similar to those that induced neurotoxicity and depolarization, lidocaine also induced an increase in the concentration of intracellular Ca++ ions ([Ca++]i; EC50 = 21 mM) via Ca++ influx through the plasma membrane as well as release of Ca++ from intracellular stores. Finally, lidocaine-induced neurotoxicity was attenuated significantly when lidocaine was applied in the presence of nominally Ca(++)-free bath solution to DRG neurons preloaded with 1,2-bis(2-aminophenoxy)ethane-N,N,N',N'-tetraacetic acid (BAPTA). Our results indicate: 1) that lidocaine is neurotoxic to sensory neurons; 2) that toxicity results from a direct action on sensory neurons; and 3) that a lidocaine-induced increase in intracellular Ca++ is a mechanism of lidocaine-induced neuronal toxicity.

  14. Articaine and lidocaine for maxillary infiltration anesthesia.

    Science.gov (United States)

    Vähätalo, K.; Antila, H.; Lehtinen, R.

    1993-01-01

    This study was undertaken to compare the anesthetic properties of articaine hydrochloride with 1:200,000 epinephrine (Ultracain DS) and lidocaine with 1:80,000 epinephrine (Xylocain-Adrenalin) for maxillary infiltration anesthesia. Twenty healthy dental student volunteers were included in this double-blind study. Each subject received 0.6 mL of each test solution at different times. Infiltration anesthesia was performed on the upper lateral incisor. The onset and duration of anesthesia were monitored using an electric pulp tester. No statistically significant differences were seen in the onset and duration of anesthesia between the articaine and lidocaine solutions. PMID:7943919

  15. More methemoglobin is produced by benzocaine treatment than lidocaine treatment in human in vitro systems.

    Science.gov (United States)

    Hartman, Neil R; Mao, Jinzhe J; Zhou, Hongfei; Boyne, Michael T; Wasserman, Adam M; Taylor, Kellie; Racoosin, Judith A; Patel, Vikram; Colatsky, Thomas

    2014-10-01

    The clinical use of local anesthetic products to anesthetize mucous membranes has been associated with methemoglobinemia (MetHba), a serious condition in which the blood has reduced capacity to carry oxygen. An evaluation of spontaneous adverse event reporting of MetHba submitted to FDA through 2013 identified 375 reports associated with benzocaine and 16 reports associated with lidocaine. The current study was performed to determine the relative ability of benzocaine and lidocaine to produce methemoglobin (MetHb) in vitro. Incubation of 500μM benzocaine with whole human blood and pooled human liver S9 over 5h resulted in MetHb levels equaling 39.8±1.2% of the total hemoglobin. No MetHb formation was detected for 500μM lidocaine under the same conditions. Because liver S9 does not readily form lidocaine hydrolytic metabolites based on xylidine, a primary metabolic pathway, 500μM xylidine was directly incubated with whole blood and S9. Under these conditions MetHb levels of 4.4±0.4% were reached by 5h. Studies with recombinant cytochrome P450 revealed benzocaine to be extensively metabolized by CYP 1A2, with 2B6, 2C19, 2D6, and 2E1 also having activity. We conclude that benzocaine produces much more MetHb in in vitro systems than lidocaine or xylidine and that benzocaine should be more likely to cause MetHba in vivo as well.

  16. Diphenytoin, riluzole and lidocaine: three sodium channel blockers, with different mechanisms of action, decrease hippocampal epileptiform activity.

    Science.gov (United States)

    Diao, Lihong; Hellier, Jennifer L; Uskert-Newsom, Jessica; Williams, Philip A; Staley, Kevin J; Yee, Audrey S

    2013-10-01

    Epilepsy is a condition affecting 1-2% of the population, characterized by the presence of spontaneous, recurrent seizures. The most common type of acquired epilepsy is temporal lobe epilepsy (TLE). Up to 30% of patients with TLE are refractory to currently available compounds, and there is an urgent need to identify novel targets for therapy. Here, we utilized the in-vitro CA3 burst preparation to examine alterations in network excitability, characterized by changes in interburst interval. Specifically, we show that bath application of three different sodium channel blockers-diphenytoin, riluzole, and lidocaine-slow spontaneous CA3 bursts. This in turn, decreased the epileptiform activity. These compounds work at different sites on voltage-gated sodium channels, but produce a similar network phenotype of decreased excitability. In the case of diphenytoin and riluzole, the change in network activity (i.e., increased interburst intervals) was persistent following drug washout. Lidocaine application, however, only increased the CA3 interburst interval when it was in the bath solution. Thus, its action was not permanent and resulted in returning CA3 bursting to baseline levels. These data demonstrate that the CA3 burst preparation provides a relatively easy and quick platform for identifying compounds that can decrease network excitability, providing the initial screen for further and more complex in-vivo, freely-behaving animal studies.

  17. Articaine hydrochloride: a study of the safety of a new amide local anesthetic.

    Science.gov (United States)

    Malamed, S F; Gagnon, S; Leblanc, D

    2001-02-01

    Articaine is an amide local anesthetic introduced clinically in Germany in 1976 and subsequently throughout Europe, Canada and, in 2000, the United States. The authors report on three identical single-dose, randomized, double-blind, parallel-group, active-controlled multicenter studies that were conducted to compare the safety and efficacy of articaine (4 percent with epinephrine 1:100,000) with that of lidocaine (2 percent with epinephrine 1:100,000). A total of 1,325 subjects participated in these studies, 882 of whom received articaine 4 percent with epinephrine 1:100,000 and 443 of whom received lidocaine 2 percent with epinephrine 1:100,000. The overall incidence of adverse events in the combined studies was 22 percent for the articaine group and 20 percent for the lidocaine group. The most frequently reported adverse events in the articaine group, excluding postprocedural dental pain, were headache (4 percent), facial edema, infection, gingivitis and paresthesia (1 percent each). The incidence of these events was similar to that reported for subjects who received lidocaine. The adverse events most frequently reported as related to articaine use were paresthesia (0.9 percent), hypesthesia (0.7 percent), headache (0.55 percent), infection (0.45 percent), and rash and pain (0.3 percent each). Articaine is a well-tolerated, safe and effective local anesthetic for use in clinical dentistry.

  18. Evaluation of local anesthetic and antipyretic activities of Cinchona ...

    African Journals Online (AJOL)

    yeast-induced pyrexia in rats, using aspirin (300 mg/kg) as reference. Results: C. ... Materials. Xylocaine, sodium chloride, Brewer's yeast, and ... Preparation of C. officinalis extract ..... Flavonoid glucosides are hydrolyzed and thus activated.

  19. The effect of perioperative intravenous lidocaine on postoperative pain and immune function

    National Research Council Canada - National Science Library

    Yardeni, Israel Z; Beilin, Benzion; Mayburd, Eduard; Levinson, Yuri; Bessler, Hanna

    2009-01-01

    .... These cytokines can induce peripheral and central sensitization, leading to pain augmentation. Recently, a frequently used local anesthetic, lidocaine, was introduced as a part of a perioperative pain management technique...

  20. Intravenously administered lidocaine in therapeutic doses increases the intraspinal release of acetylcholine in rats

    DEFF Research Database (Denmark)

    Abelson, Klas S P; Höglund, A Urban

    2002-01-01

    The local anesthetic lidocaine suppresses different pain conditions when administered systemically. Part of the antinociceptive effect appears to be mediated via receptor mechanisms. We have previously shown that muscarinic and nicotinic agonists that produce antinociception increase the intraspi...

  1. 复方阿替卡因与利多卡因用于老年人拔牙麻醉的临床效果比较%Clinical comparison of anesthetic efficacy on compound articaine and lidocaine used for the tooth extraction in elderly people

    Institute of Scientific and Technical Information of China (English)

    夏雨凝; 许一起; 王霞

    2014-01-01

    Objective:To investigate the anesthetic efficacy and adverse reaction of the compound articaine used in tooth extraction.in elderly people.Methods:479 cases of elderly patients with conventional tooth extraction, selected from the Department of stomatology in Urumqi General Hospital of Lanzhou Military Region, Urumqi,, were randomly divided into compound articaine anesthesia group (treatment group, n= 242) and lidocaine anesthesia group (control group, n= 237), The clinical effect of anesthesia and anesthesia adverse reaction were evaluated according to the facial expression of patients and a visual analogue scale (VAS). The incidence of adverse reaction were also determined. Anesthetic efficacy was marked as totally valid, good valid, valid and invalid.Results:The anesthetic efficacy and VAS scores in the treatment group were statistically better than those in the control group (P<0.01). Onset time of anesthesia in compound articaine group was statistically better than that of lidocaine anesthesia group (P<0.05).Conclusions:The anesthetic effect of articaine has obvious advantages compared to lidocaine, a kind of traditional anesthetic. Compound articaine has the advantages of fast acting, powerful anesthetic effect, long duration and less adverse reaction. It can eliminate the mental anxiety and fear of elderly patients during tooth extraction to avoid sharp increase in blood pressure. Compound articaine is a safe and useful local anaesthetic, worth of promoting in oral surgery.%目的:探讨复方阿替卡因在我院口腔科对老年人拔牙术中观察麻醉镇痛临床疗效和不良反应的研究。方法:选自我院口腔科接受常规拔牙术的老年患者479例,随机分为复方阿替卡因麻醉组(实验组)242例和利多卡因麻醉组(对照组)各237例,比较两组的临床麻醉效果和麻醉不良反应。行拔牙术中根据患者表情和医生评价确定麻醉效果,麻醉分为完全、良好、有效

  2. Systemic administration of lidocaine suppresses the excitability of rat cervical dorsal horn neurons and tooth-pulp-evoked jaw-opening reflex.

    Science.gov (United States)

    Takeda, Mamoru; Oshima, Katsuo; Takahashi, Masayuki; Matsumoto, Shigeji

    2009-10-01

    Although systemic lidocaine has been demonstrated to have analgesic actions in neuropathic pain conditions, the effect of intravenous lidocaine on trigeminal pain has not been elucidated. The aim of the present study is to investigate the effect of intravenous lidocaine administration on the excitability of the upper cervical dorsal horn (C1) neuron having convergent inputs from both tooth-pulp (TP) and facial skin as well as nociceptive jaw-opening reflex (JOR). After electrical stimulation of TP, extracellular single-unit recordings from 19 C1 neurons and the digastric muscle electromyogram (dEMG) were made in pentobarbital-anesthetized rats. These neurons also responded to non-noxious and noxious mechanical stimulation (touch and pinch) of facial skin, and every neuron was considered to be a wide dynamic range (WDR) neuron. The TP-evoked C1 neuronal and dEMG activities were dose-dependently inhibited by systematic administration of lidocaine (1-2 mg/kg, i.v.). After intravenous injection of lidocaine, the unit discharges induced by both touch and pinch stimuli were inhibited, and the size of the receptive field for pinch was also significantly decreased. The mean spontaneous discharge frequencies were significantly inhibited by the application of lidocaine. These changes were reversed within -20 min. These results suggest that in the absence of neuropathic pain intravenous lidocaine injection suppresses the trigeminal nociceptive reflex as well as the excitability of C1 neurons having convergent inputs from TP and somatic afferents. Systemic lidocaine administration, therefore, may contribute to the alleviation of trigeminal-referred pain associated with tooth pain.

  3. The Use of Topical Lidocaine Gel During Intermaxillary Fixation Procedure.

    Science.gov (United States)

    Jeong, Yeon Jin; Kim, Ho Jun; Kwon, Ho; Shim, Hyung-Sup; Seo, Bommie Florence; Jung, Sung-No

    2016-07-01

    This study aimed to validate the usefulness of lidocaine gel during intermaxillary fixation using arch bars in patients with mandible fracture by comparing 2 patient groups: one group using lidocaine gel in intermaxillary fixation and the other group undergoing traditional local infiltration.Subjects were patients with mandible fracture undergoing intermaxillary fixation using arch bars from March 2003 to February 2007. Twenty-three patients were anesthetized in the upper and lower gingiva by 2% local lidocaine solution injection; another 23 underwent topical anesthesia with 2% lidocaine hydrochloride gel applied to the upper and lower gingiva. The convenience of fixation was measured in terms of operation time and degree of pain according to the visual analog scale; arch bar loosening rate was assessed postoperatively.The mean operation times were 63 and 47 minutes in the groups undergoing local infiltration and using topical lidocaine gel, respectively. For pain degree according to the visual analog scale, the mean scores were 6.4 and 3.2 in the groups using local infiltration and topical lidocaine gel, respectively. When the arch bar loosening rate was measured postoperatively, the 2 groups differed significantly, with a rate of 26% in the group using local infiltration and 13% in the group using topical lidocaine gel.Application of topical lidocaine gel during intermaxillary fixation using arch bars in patients with mandible fracture relieves pain and offers convenience in performing the procedure. It can be a useful alternative method for patients who are sensitive to pain or have needle phobia.

  4. Lidocaine Concentration in Oral Tissue by the Addition of Epinephrine.

    Science.gov (United States)

    Tanaka, Eri; Yoshida, Kenji; Kawaai, Hiroyoshi; Yamazaki, Shinya

    2016-01-01

    The vasoconstrictive effect due to the addition of epinephrine to local anesthetic has been clearly shown by measuring blood-flow volume or blood anesthetic concentration in oral mucosal tissue. However, there are no reports on the measurement of anesthetic concentration using samples directly taken from the jawbone and oral mucosal tissue. Consequently, in this study, the effect of lidocaine concentration in the jawbone and oral mucosal tissue by the addition of epinephrine to the local anesthetic lidocaine was considered by quantitatively measuring lidocaine concentration within the tissue. Japanese white male rabbits (n = 96) were used as test animals. General anesthesia was induced by sevoflurane and oxygen, and then cannulation to the femoral artery was performed while arterial pressure was constantly recorded. Infiltration anesthesia was achieved by 0.5 mL of 2% lidocaine containing 1 : 80,000 epinephrine in the upper jawbone (E(+)) and 0.5 mL of 2% of epinephrine additive-free lidocaine (E(0)) under the periosteum. At specified time increments (10, 20, 30, 40, 50, and 60 minutes), samples from the jawbone, oral mucosa, and blood were collected, and lidocaine concentration was directly measured by high-performance liquid chromatography. No significant differences in the change in blood pressure were observed either in E(+) or E(0). In both E(+) and E(0) groups, the serum lidocaine concentration peaked 10 minutes after local anesthesia and decreased thereafter. At all time increments, serum lidocaine concentration in E(+) was significantly lower than that in E(0). There were no significant differences in measured lidocaine concentration between jawbone and mucosa within either the E(+) or the E(0) groups at all time points, although the E(0) group had significantly lower jawbone and mucosa concentrations than the E(+) group at all time points when comparing the 2 groups to each other. Addition of epinephrine to the local anesthetic inhibited systemic

  5. Dual effect of local anesthetics on the function of excitable rod outer segment disk membrane

    Energy Technology Data Exchange (ETDEWEB)

    Mashimo, T.; Abe, K.; Yoshiya, I.

    1986-04-01

    The effects of local anesthetics and a divalent cation, Ca2+, on the function of rhodopsin were estimated from the measurements of light-induced proton uptake. The light-induced proton uptake by rhodopsin in the rod outer segment disk membrane was enhanced at lower pH (4) but depressed at higher pHs (6 to 8) by the tertiary amine local anesthetics lidocaine, bupivacaine, tetracaine, and dibucaine. The order of local anesthetic-induced depression of the proton uptake followed that of their clinical anesthetic potencies. The depression of the proton uptake versus the concentration of the uncharged form of local anesthetic nearly describes the same curve for small and large dose of added anesthetic. Furthermore, a neutral local anesthetic, benzocaine, depressed the proton uptake at all pHs between 4 and 7. These results indicate that the depression of the proton uptake is due to the effect of only the uncharged form. It is hypothesized that the uncharged form of local anesthetics interacts hydrophobically with the rhodopsin in the disk membrane. The dual effect of local anesthetics on the proton uptake, on the other hand, suggests that the activation of the function of rhodopsin may be caused by the charged form. There was no significant change in the light-induced proton uptake by rhodopsin when 1 mM of Ca2+ was introduced into the disk membrane at varying pHs in the absence or presence of local anesthetics. This fact indicates that Ca2+ ion does not influence the diprotonating process of metarhodopsin; neither does it interfere with the local anesthetic-induced changes in the rhodopsin molecule.

  6. Anesthetics interacting with lipid rafts.

    Science.gov (United States)

    Bandeiras, Cátia; Serro, Ana Paula; Luzyanin, Konstantin; Fernandes, Anabela; Saramago, Benilde

    2013-01-23

    The exact mechanism by which anesthetics induce cell membrane-mediated modifications is still an open question. Although the fluidization effect of the anesthetic molecules on the cellular membrane is widely recognized, it is not known if anesthetics show any preference for specific membrane domains, namely the lipid rafts. The importance of these membrane micro-domains derives from the fact that they have been associated with cell signaling pathways, as well as with specific drug interactions. The objective of this work is to contribute for the elucidation of this question through the comparison of the anesthetic interactions with membranes of various lipid compositions. Liposomes prepared with an equimolar mixture of POPC, sphingomyelin and cholesterol, were chosen as models for lipid rafts. The interactions of these liposomes with two local anesthetics, tetracaine and lidocaine, and one general anesthetic, propofol, were studied. The effect of cholesterol was investigated by comparing anesthetic interactions with POPC/SM liposomes and POPC/SM/CHOL liposomes. The following experimental techniques were used: quartz crystal microbalance with dissipation, differential scanning calorimetry and phosphorus nuclear magnetic resonance. Although the liposomes investigated by the different techniques are not in the same conditions, it is possible to assemble the information obtained from all experimental techniques employed to reach a general conclusion. Tetracaine interacts more with raftlike domains, lidocaine induces stronger modifications on POPC/SM liposomes and the results for propofol are not fully conclusive but it seems to be the least prone to lipid interactions. The results were compared with those obtained with DMPC-containing liposomes, reported in a previous work.

  7. Trigeminal nerve injury associated with injection of local anesthetics: needle lesion or neurotoxicity?

    DEFF Research Database (Denmark)

    Hillerup, Søren; Jensen, Rigmor H; Ersbøll, Bjarne Kjær

    2011-01-01

    anesthetics (from 1995 through 2007), 292 reports to the Danish Medicines Agency, Copenhagen, Denmark, of adverse reactions to local anesthetic drugs, and a clinical sample of 115 patients with NSD associated with local anesthetics. The authors assessed lidocaine 2 percent, mepivacaine 2 percent and 3 percent...

  8. [Comparison of two modified lidocaine solutions for local anesthesia in blepharoplasty].

    Science.gov (United States)

    Fonseca Júnior, Nilson Lopes da; Lucci, Lucia Miriam Dumont; Badessa, Marianne Peixoto Sobral Giroldo; Rehder, José Ricardo Carvalho Lima

    2009-01-01

    To compare pain on injection of two modified anesthetic lidocaine solutions for use in upper blepharoplasty: 2% lidocaine with 1:100,000 epinephrine, and 2% lidocaine with 1:100,000 epinephrine buffered 9:1 with 8.4% sodium bicarbonate. In this prospective, double-masked study, 25 consecutive patients undergoing upper blepharoplasty were submitted to the anesthesic procedure. Each eyelid received one of two modified lidocaine solutions. Heart rate, systemic arterial pressure and oxygen saturation level were obtained before, during and after injection of two different anesthetic solutions. Patients used a 4-point scale to rate the perceived pain on injection. All parameters were statistically analyzed and there was a significant difference in heart rate and oxygen saturation level. Pain on injection of eyelid anesthesia does not differ significantly with either buffered or unmodified lidocaine solutions.

  9. Nanoethosomes for Dermal Delivery of Lidocaine

    Science.gov (United States)

    Babaie, Soraya; Ghanbarzadeh, Saeed; Davaran, Soodabeh; Kouhsoltani, Maryam; Hamishehkar, Hamed

    2015-01-01

    Purpose: It is necessary for local anesthetics to pass through the stratum corneum to provide rapid pain relief. Many techniques have been reported to enhance intradermal penetration of local anesthetics such as vesicular lipid carriers. Ethosomes are lipid vesicles containing phospholipids, ethanol at relatively high concentration. We hypothesized that synergistic effects of phospholipids and high concentration of ethanol in formulation could accelerate penetration of nanoethosomes in deep layers of skin. Methods: Lidocaine-loaded nanoethosomes were prepared and characterized by size and zeta analyzer, scanning electron microscopy (SEM) and X-ray diffractometer (XRD). Furthermore, encapsulation efficiency (EE), loading capacity (LC), and skin penetration capability were evaluated by in vitro and in vivo experiments. Results: results showed that the particle size, zeta potential, EE and LC of optimum formulation were 105.4 ± 7.9 nm, -33.6 ± 2.4 mV, 40.14 ± 2.5 %, and 8.02 ± 0.71 respectively. SEM results confirmed the non-aggregated nano-scale size of prepared nanoethosomes. Particle size of ethosomes and EE of Lidocaine were depended on the phospholipid and ethanol concentrations. XRD results demonstrated the drug encapsulation in amorphous status interpreting the achieved high drug EE and LC values. In vitro and in vivo assays confirmed the appropriate skin penetration of Lidocaine with the aid of nanoethosomes and existence of deposition of nanoethosomes in deep skin layers, respectively. Conclusion: The developed nanoethosomes are proposed as a suitable carrier for topical delivery of anesthetics such as Lidocaine. PMID:26819928

  10. Evaluation of lidocaine and mepivacaine for inferior third molar surgery.

    Science.gov (United States)

    Porto, Gabriela Granja; Vasconcelos, Belmiro Cavalcanti Do Egito; Gomes, Ana Cláudia Amorim; Albert, Daniela

    2007-01-01

    The aim of this study was to compare 2% lidocaine and 2% mepivacaine with 1:100,000 epinephrine for postoperative pain control. A group of 35 patients, both genders were recruited, whose had ages ranged from 13 to 27 years-old and had two inferior third molars in similar positions to be extracted. The cartridges were distributed to the patients according to a randomised pattern, where lidocaine was in the control group and mepivacaine in the experimental group. Results showed no significant association between the anesthetics and postoperative pain, pulp sensibility after one hour, gender, tooth position and duration of the surgical procedure. It was shown that lidocaine and mepivacaine have similar time of anesthesia, they are adequate for surgical procedures that last one hour, and there was no difference between the two anesthetics in relation to the severety of post-operative pain.

  11. Ketamine reduces lidocaine-induced seizures in mice.

    Science.gov (United States)

    Guler, Gulen; Erdogan, Fusun; Golgeli, Asuman; Akin, Aynur; Boyaci, Adem

    2005-08-01

    Systemic toxic reactions to local anesthetics are brought about by absolute overdosage, and, most commonly, inadvertent intravascular injections. The anti-convulsant action of ketamine has been studied. However, the effect of ketamine on lidocaine-induced convulsions has not been reported. This study investigated the effect of ketamine on lidocaine-induced seizures in mice. Mice (32-41 g) were divided into 2 groups, 15 in each group, and were pretreated with intraperitoneal normal saline solution or intraperitenoeal (ip) ketamine before lidocaine. Group 1 (N = 15) received 75 mg kg ip lidocaine; Group 2 (N = 15) received 20 mg kg ketamin ip; 5 min later 75 mg kg lidokaine ip were applied. Clinical features, incidences, latencies, durations, and mortality rate of convulsions were recorded. After 75 mg kg lidocaine injection, ataxia, loss of righting reflex, and generalized tonic-clonic convulsions were seen within 2-5 min in Group 1. Generalized tonic-clonic convulsions were seen in 8 mice and deep sedation was seen in 7 mice in Group 2 (p .05). It was concluded that ketamine significantly prevented lidocaine-induced generalized tonic-clonic seizures; on the other hand, the lethality of lidocaine was least reduced by ketamine.

  12. The quaternary lidocaine derivative, QX-314, exerts biphasic effects on transient receptor potential vanilloid subtype 1 channels in vitro

    DEFF Research Database (Denmark)

    Rivera-Acevedo, Ricardo E; Pless, Stephan Alexander; Ahern, Christopher A;

    2011-01-01

    BACKGROUND: Transient receptor potential vanilloid subfamily member 1 (TRPV1) channels are important integrators of noxious stimuli with pronounced expression in nociceptive neurons. The experimental local anesthetic, QX-314, a quaternary (i.e., permanently charged) lidocaine derivative, recently...

  13. Pharmacokinetics of Lidocaine With Epinephrine Following Local Anesthesia Reversal With Phentolamine Mesylate

    OpenAIRE

    Moore, Paul A.; Hersh, Elliot V.; Papas, Athena S; Goodson, J. Max; Yagiela, John A; Rutherford, Bruce; Rogy, Seigried; Navalta, Laura

    2008-01-01

    Phentolamine mesylate accelerates recovery from oral soft tissue anesthesia in patients who have received local anesthetic injections containing a vasoconstrictor. The proposed mechanism is that phentolamine, an alpha-adrenergic antagonist, blocks the vasoconstriction associated with the epinephrine used in dental anesthetic formulations, thus enhancing the systemic absorption of the local anesthetic from the injection site. Assessments of the pharmacokinetics of lidocaine and phentolamine, a...

  14. [Cytotoxic effects of local anesthesia through lidocaine/ropivacaine on human melanoma cell lines].

    Science.gov (United States)

    Kang, Ding-Kun; Zhao, Li-Yan; Wang, Hong-Li

    Local anesthetics (LAs) are generally considered as safe, but cytotoxicity has been reported for several local anesthetics used in humans, which is not well investigated. In the present study, the cytotoxicity of lidocaine, ropivacaine and the combination of lidocaine and ropivacaine were evaluated on human melanoma cell lines. Melphalan, a nitrogen mustard alkylating agent, was used as a control agent for comparison of cytotoxic activity. Melanoma cell lines, A375 and Hs294T, were exposed to 1h to different concentrations of above agents. Cell-viability after exposure was determined by flow cytometry. Investigated LAs showed detrimental cytotoxicity on studied melanoma cell lines in time- (p<0.001), concentration- (p<0.001), and agent dependant. In both A375 and Hs294T cell lines, minimum cell viability rates were found after 72h of exposure to these agents. Lidocaine 2% caused a reduction of vital cells to 10%±2% and 14%±2% in A375 and Hs294T, respectively after 72h of exposure. Ropivacaine 0.75% after 72h reduced viable cells to 15%±3% and 25%±3% in A375 and Hs294T, respectively. Minimum cell viability after 72h exposure to the combination was 10%±2% and 18%±2% in A375 and Hs294T, respectively. Minimum cell viability after 72h exposure to melphalan was 8%±1% and 12%±2%, in A375 and Hs294T, respectively. LAs have cytotoxic activity on human melanoma cell lines in a time-, concentration- and agent-dependant manner. Apoptosis in the cell lines was mediated through activity of caspases-3 and caspases-8. Copyright © 2016 Sociedade Brasileira de Anestesiologia. Publicado por Elsevier Editora Ltda. All rights reserved.

  15. Cytotoxic effects of local anesthesia through lidocaine/ropivacaine on human melanoma cell lines.

    Science.gov (United States)

    Kang, Ding-Kun; Zhao, Li-Yan; Wang, Hong-Li

    Local anesthetics (LAs) are generally considered as safe, but cytotoxicity has been reported for several local anesthetics used in humans, which is not well investigated. In the present study, the cytotoxicity of lidocaine, ropivacaine and the combination of lidocaine and ropivacaine were evaluated on human melanoma cell lines. Melphalan, a nitrogen mustard alkylating agent, was used as a control agent for comparison of cytotoxic activity. Melanoma cell lines, A375 and Hs294T, were exposed to 1h to different concentrations of above agents. Cell-viability after exposure was determined by flow cytometry. Investigated LAs showed detrimental cytotoxicity on studied melanoma cell lines in time- (p<0.001), concentration- (p<0.001), and agent dependant. In both A375 and Hs294T cell lines, minimum cell viability rates were found after 72h of exposure to these agents. Lidocaine 2% caused a reduction of vital cells to 10%±2% and 14%±2% in A375 and Hs294T, respectively after 72h of exposure. Ropivacaine 0.75% after 72h reduced viable cells to 15%±3% and 25%±3% in A375 and Hs294T, respectively. Minimum cell viability after 72h exposure to the combination was 10%±2% and 18%±2% in A375 and Hs294T, respectively. Minimum cell viability after 72h exposure to melphalan was 8%±1% and 12%±2%, in A375 and Hs294T, respectively. LAs have cytotoxic activity on human melanoma cell lines in a time-, concentration- and agent-dependant manner. Apoptosis in the cell lines was mediated through activity of caspases-3 and caspases-8. Copyright © 2016 Sociedade Brasileira de Anestesiologia. Published by Elsevier Editora Ltda. All rights reserved.

  16. Lidocaine block of cardiac sodium channels.

    Science.gov (United States)

    Bean, B P; Cohen, C J; Tsien, R W

    1983-05-01

    Lidocaine block of cardiac sodium channels was studied in voltage-clamped rabbit purkinje fibers at drug concentrations ranging from 1 mM down to effective antiarrhythmic doses (5-20 muM). Dose-response curves indicated that lidocaine blocks the channel by binding one-to-one, with a voltage-dependent K(d). The half-blocking concentration varied from more than 300 muM, at a negative holding potential where inactivation was completely removed, to approximately 10 muM, at a depolarized holding potential where inactivation was nearly complete. Lidocaine block showed prominent use dependence with trains of depolarizing pulses from a negative holding potential. During the interval between pulses, repriming of I (Na) displayed two exponential components, a normally recovering component (tauless than 0.2 s), and a lidocaine-induced, slowly recovering fraction (tau approximately 1-2 s at pH 7.0). Raising the lidocaine concentration magnified the slowly recovering fraction without changing its time course; after a long depolarization, this fraction was one-half at approximately 10 muM lidocaine, just as expected if it corresponded to drug-bound, inactivated channels. At less than or equal to 20 muM lidocaine, the slowly recovering fraction grew exponentially to a steady level as the preceding depolarization was prolonged; the time course was the same for strong or weak depolarizations, that is, with or without significant activation of I(Na). This argues that use dependence at therapeutic levels reflects block of inactivated channels, rather than block of open channels. Overall, these results provide direct evidence for the "modulated-receptor hypothesis" of Hille (1977) and Hondeghem and Katzung (1977). Unlike tetrodotoxin, lidocaine shows similar interactions with Na channels of heart, nerve, and skeletal muscle.

  17. Volatile anesthetics inhibit the activity of calmodulin by interacting with its hydrophobic site

    Institute of Scientific and Technical Information of China (English)

    ZHOU Miao-miao; XIA Hui-min; LIU Jiao; XU You-nian; XIN Nai-xin; ZHANG Shi-hai

    2012-01-01

    Background Volatile anesthetics (VAs) may affect varied and complex physiology processes by manipulating Ca2+-calmodulin (CaM).However,the detailed mechanism about the action of VAs on CaM has not been elucidated.This study was undertaken to examine the effects of VAs on the conformational change,hydrophobic site,and downstream signaling pathway of CaM,to explore the possible mechanism of anesthetic action of VAs.Methods Real-time second-harmonic generation (SHG) was performed to monitor the conformational change of CaM in the presence of VAs, each plus 100 μmol/L Ca2+. A hydrophobic fluorescence indicator,8-anilinonaphthalene-1-sulfonate (ANS),was utilized to define whether the VAs would interact with CaM at the hydrophobic site or not.High-performance liquid chromatography (HPLC) was carried out to analyze the activity of CaM-dependent phosphodiesterase (PDE1) in the presence of VAs.The VAs studied were ether,enflurane,isoflurane,and sevoflurane,with their aqueous concentrations 7.6,9.5,11.4 mmol/L; 0.42,0.52,0.62 mmol/L; 0.25,0.31,0.37 mmol/L and 0.47,0.59,0.71 mmol/L respectively,each were equivalent to their 0.8,1.0 and 1.2 concentration for 50% of maximal effect (EC50) for general anesthesia.Results The second-harmonic radiation of CaM in the presence of Ca2+ was largely inhibited by the VAs.The fluorescence intensity of ANS,generated by binding of Ca2+ to CaM,was reversed by the VAs.HPLC results also showed that AMP,the product of the hydrolysis of cAMP by CaM-dependent PDE1,was reduced by the VAs.Conclusions Our findings demonstrate that the above VAs interact with the hydrophobic core of Ca2+-CaM and the interaction results in the inhibition of the conformational change and activity of CaM.This in vitro study may provide us insight into the possible mechanism of anesthetic action of VAs in vivo.

  18. Is lidocaine patch as effective as intravenous lidocaine in pain and illus reduction after laparoscopic colorectal surgery? A randomized clinical trial

    Science.gov (United States)

    Elhafz, Ahmed Ali Abd; Elgebaly, Ahmed Said; Bassuoni, Ahmed Sobhy; El Dabaa, Ahmed Ali

    2012-01-01

    Objective: To evaluate the efficacy of lidocaine patch applied around wound in laparoscopic colorectal surgery in reduction of postoperative pain and illus compared to intravenous lidocaine infusion and placebo. Background: Postoperative illus and pain after colorectal surgery is a challenging problem associated with increased morbidity and cost. Inflammatory response to surgery plays crucial rule in inducing postoperative illus. Systemic local anesthetics proved to have anti-inflammatory properties that may be beneficial in preventing ileus added to its analgesic actions. The lidocaine patch evaluated in many types of pain with promising results. We try to evaluate the patch in perioperative field as a more simple and safe technique than the intravenous route. Materials and Methods: Prospective, randomized, controlled study was conducted, comparing three groups. Group 1 (placebo) received saline infusion, group 2 received i.v. lidocaine infusion after induction of anesthesia, 2 mg/min if body weight >70 kg or 1 mg/min if body weight lidocaine patch 5%, three patches each one divided into two equal parts and applied around the three wounds just before induction. Data collected were, pain scores (VAS), morphine consumption, return of bowel function, pro-inflammatory cytokines plasma levels and plasma lidocaine level. Results: Pain intensity (VAS) scores at rest and during coughing were significantly lower during the first 72 h postoperative in i.v. lidocaine group and patch group compared to the placebo group. Mean morphine consumption were significantly lower in the i.v. lidocaine group and patch group compared to placebo group. Return of the bowel function was significantly earlier in i.v. lidocaine group in comparison to the other groups. Proinflammatory cytokines (IL6, IL8, and C3a) were significantly lower in i.v. lidocaine group compared to the other two groups. Conclusion: The lidocaine patch was equal to i.v. lidocaine infusion in decreasing pain scores and

  19. Endomorphins decrease heart rate and blood pressure possibly by activating vagal afferents in anesthetized rats.

    Science.gov (United States)

    Kwok, E H; Dun, N J

    1998-08-24

    Endomorphin 1 (10, 30, 100 nmol/kg) administered intravenously (i.v. ) to urethane-anesthetized rats consistently and dose-dependently lowered heart rate (HR) and mean arterial pressure (MAP); the decrease in blood pressure recovered faster as compared to the HR. The effects of endomorphin 2 were qualitatively similar. Naloxone (2 mg/kg, i.v.) completely antagonized the bradycardia and hypotension caused by endomorphin 1. Pretreatment of the rats with atropine methylnitrate, atropine sulfate (2 mg/kg, i.v.) or bilateral vagotomy nearly abolished the bradycardia and attenuated the hypotensive effect of endomorphin 1. Our studies suggest that the bradycardia effect following systemic administration of the new opioid peptide may be explained by activation of vagal afferents and the hypotensive effect may be secondary to a reduction of cardiac output and/or a direct vasodilation.

  20. Comparison of Two Anesthetic Methods for Intravitreal Ozurdex Injection

    Directory of Open Access Journals (Sweden)

    V. Levent Karabaş

    2015-01-01

    Full Text Available Purpose. To determine whether subconjunctival lidocaine injection maintains additional anesthetic effect during intravitreal Ozurdex injection. Methods. 63 patients who were diagnosed as central or branch retinal vein occlusion and planned to receive Ozurdex injection for macular edema were prospectively included in the study. The patients were randomized into one of the two anesthetic groups. The first group received topical proparacaine drop and lidocaine applied pledget. The second group received subconjunctival lidocaine injection in addition to the anesthetics in group 1. Results. Mean pain score was 1.90±2.39 in group 1 and 1.71 ± 2.09 in group 2 (p=0.746. Mean subconjunctival hemorrhage grade was 1.67±0.17 in group 1 and 0.90±0.14 in group 2 (p=0.001. There was no relationship between the amount of subconjunctival hemorrhage and pain score of the patients. Conclusions. There was no difference in pain scores between the two anesthetic methods. The addition of subconjunctival lidocaine injection offered no advantage in pain relief compared to lidocaine-applied pledgets.

  1. Comparação entre a lidocaína e a acupuntura no tratamento da taquicardia ventricular induzida com dopamina em equinos anestesiados com halotano Comparative study between lidocaine and acupunture in the treatment of ventricular tachycardia induced by dopamine in horses anesthetized with halothane

    Directory of Open Access Journals (Sweden)

    J.J. Cárdenas

    2009-08-01

    Full Text Available Os efeitos da lidocaina e da acupuntura nos pontos bilaterais associados ao pericárdio 6 (Pc6-Neiguan e ao coração 7 (C7-Shenmen, no tratamento da taquicardia ventricular (TV induzida por dopamina em equinos anestesiados com halotano, foram avaliados e comparados. Seis equinos, distribuídos em três grupos: grupo-controle (GC, grupo tratado com acupuntura (GA e grupo tratado com lidocaína (GL, foram anestesiados três vezes cada, com intervalo de uma semana entre cada anestesia. Avaliaram-se os parâmetros cardiovasculares (frequência cardíaca, pressão arterial e eletrocardiografia, os respiratórios (frequência respiratória, capnografía, saturação de hemoglobina e hemogasometria e o escore de recuperação. A dose arritmogênica da dopamina (DAD foi determinada a partir da infusão de 70µg/kg/min IV durante 10 minutos, sem interrupção, preenchendo o critério arritmogênico: quatro ou mais complexos ventriculares prematuros seguidos, com duração de pelo menos 15 segundos ou TV sustentada. O tempo médio de aparecimento da DAD ou da TV foi de 6,05±0,45 minutos nos animais não tratados, e a TV se reverteu espontaneamente aos 2,7±0,2 minutos. O grupo tratado com acupuntura reverteu a TV no tempo médio de 1,8±0,2 (PThe effects of lidocaine and acupuncture in the associated bilateral points, i.e. pericardium 6 (Pc 6- Neiguan and heart 7 (H7 - Shenmen, on the ventricular tachycardia (VT induced by dopamine were evaluated in horses anesthetized with halothane. Six horses were distributed in three groups: control group (CG, acupuncture treated group (AG, and lidocaine treated group (LG. They were anesthetized three times each one using halothane with one week interval between each anesthesic procedure. Cardiovascular (heart rate, arterial pressure, and ECG and respiratory (respiratory rate, capnometry, hemoglobin saturation, and blood gas analysis parameters and recovery score were evaluated. The arrhythmogenic dose of dopamine

  2. Use of Lidocaine 2% Gel Does Not Reduce Pain during Flexible Cystoscopy and Is Not Cost-Effective.

    Science.gov (United States)

    Cano-Garcia, Maria Del Carmen; Casares-Perez, Rosario; Arrabal-Martin, Miguel; Merino-Salas, Sergio; Arrabal-Polo, Miguel Angel

    2015-11-14

    To compare the use of lubricant gel with lidocaine versus lubricant gel without anesthetic in flexible cystoscopy in terms of pain and tolerability. In this observational non-randomized study, 72 patients were divided into two groups. Group 1 included 38 patients in whom lidocaine gel 2% was used and group 2 included 34 patients in whom lubricant gel without anesthetic was administered. The main variables analyzed were score in visual analogue scale (VAS) and score in Spanish Pain Questionnaire (SPQ). Student's t-test and Chi-square test were used to compare differences between 2 groups. The P values lidocaine is 1.25 euro and gel without anesthetic 0.22 euro. The use of lidocaine gel does not produce benefit in terms of pain relief in flexible cystoscopy and also is costly.

  3. Decreasing Effect of Lidocaine·HCl on the Thickness of the Neuronal and Model Membrane

    OpenAIRE

    Park, Sung-Min; Park, Jong-Sun; Kim, Jae-Han; Baek, Jin-Hyun; Yoon, Tae-Gyun; Lee, Do-Keun; Ryu, Won-Hyang; Chung, In-Kyo; Sohn, Uy Dong; Jang, Hye-Ock; Yun, Il

    2013-01-01

    This study examined the mechanism of action of a local anesthetic, lidocaine·HCl. Energy transfer between the surface fluorescent probe, 1-anilinonaphthalene-8-sulfonic acid, and the hydrophobic fluorescent probe, 1,3-di(1-pyrenyl) propane, was used to determine the effect of lidocaine·HCl on the thickness (D) of the synaptosomal plasma membrane vesicles (SPMV) isolated from the bovine cerebral cortex, and liposomes of the total lipids (SPMVTL) and phospholipids (SPMVPL) extracted from the SP...

  4. Fast-onset lidocaine block of rat NaV1.4 channels suggests involvement of a second high-affinity open state.

    Science.gov (United States)

    Gingrich, Kevin J; Wagner, Larry E

    2016-06-01

    Local anesthetics (LAs) block resting, open, and inactivated states of voltage-gated Na(+) channels where inactivated states are thought to bind with highest affinity. However, reports of fast-onset block occurring over milliseconds hint at high-affinity block of open channels. Movement of voltage-sensor domain IV-segment 4 (DIVS4) has been associated with high affinity LA block termed voltage-sensor block (VSB) that also leads to a second open state. These observations point to a second high-affinity open state that may underlie fast-onset block. To test for this state, we analyzed the modulation of Na(+) currents by lidocaine and its quaternary derivative (QX222) from heterologously expressed (Xenopus laevis oocytes) rat skeletal muscle μ1 NaV1.4 (rSkM1) with β1 (WT-β1), and a mutant form (IFM-QQQ mutation in the III-IV interdomain, QQQ) lacking fast inactivation, in combination with Markov kinetic gating models. 100 μM lidocaine induced fast-onset (τonset≈2 ms), long-lived (τrecovery≈120 ms) block of WT-β1 macroscopic currents. Lidocaine blocked single-channel and macroscopic QQQ currents in agreement with our previously described mechanism of dual, open-channel block (DOB mechanism). A DOB kinetic model reproduced lidocaine effects on QQQ currents. The DOB model was extended to include trapping fast-inactivation and activation gates, and a second open state (OS2); the latter arising from DIVS4 translocation that precedes inactivation and exhibits high-affinity, lidocaine binding (apparent Kd=25 μM) that accords with VSB (DOB-S2VSB mechanism). The DOB-S2VSB kinetic model predicted fast-onset block of WT-β1. The findings support the involvement of a second, high-affinity, open state in lidocaine modulation of Na(+) channels.

  5. Prospective randomized study of viscous lidocaine versus benzocaine in a GI cocktail for dyspepsia.

    Science.gov (United States)

    Vilke, Gary M; Jin, Albert; Davis, Daniel P; Chan, Theodore C

    2004-07-01

    We hypothesized that Benzocaine (Hurricaine) would work as quickly and effectively as viscous Lidocaine in this preparation. This was a prospective randomized, single-blinded comparison between Benzocaine and Lidocaine as the topical anesthetic in a gastrointestinal (GI) cocktail. Patients 18 years or older were approached for participation when a GI cocktail was ordered by the Emergency Physician. Patients were randomized to equivalent doses of either Benzocaine or viscous Lidocaine in addition to 30 cc of Maalox and 10 cc of Donnatal. Assessment using a visual analog pain scale occurred at time intervals of 0, 5, 15, and 30 min. Eighty-two patients were enrolled (44 to Benzocaine, 38 to viscous Lidocaine), with each group having a statistically significant improvement in pain (p Benzocaine and viscous Lidocaine groups in terms of the relief of symptoms at each of the assessment times. There were no adverse outcomes in either group.

  6. Evaluation of chemical enhancers in the transdermal delivery of lidocaine.

    Science.gov (United States)

    Lee, Philip J; Ahmad, Naina; Langer, Robert; Mitragotri, Samir; Prasad Shastri, V

    2006-02-03

    The effect of various classes of chemical enhancers was investigated for the transdermal delivery of the anesthetic lidocaine across pig and human skin in vitro. The lipid disrupting agents (LDA) oleic acid, oleyl alcohol, butenediol, and decanoic acid by themselves or in combination with isopropyl myristate (IPM) showed no significant flux enhancement. However, the binary system of IPM/n-methyl pyrrolidone (IPM/NMP) improved drug transport. At 2% lidocaine dose, this synergistic enhancement peaked at 25:75 (v/v) IPM:NMP with a steady state flux of 57.6 +/- 8.4 microg cm(-2) h(-1) through human skin. This observed flux corresponds to a four-fold enhancement over a 100% NMP solution and over 25-fold increase over 100% IPM at the same drug concentration (p enhancement due to LDA. These findings allow a more rational approach for designing oil-based formulations for the transdermal delivery of lidocaine free base and similar drugs.

  7. How lidocaine influences the bilayer thickness and bending elasticity of biomembranes

    Energy Technology Data Exchange (ETDEWEB)

    Zheng Yi; Nagao, Michihiro; Bossev, Dobrin P, E-mail: zhyi@indiana.edu

    2010-11-01

    We have studied how local anesthetics influence the structural and dynamical properties of model bio-membranes. The measurements of small-angle neutron scattering have been performed on 1,2-dimyristoyl-sn-glycero-3-phosphocholine (DMPC) unilamellar vesicles with different concentrations of lidocaine in D{sub 2}O to determine the bilayer thickness as a function of the lidocaine concentration. The neutron-spin echo spectroscopy (NSE) has been used to study the influence of lidocaine on the bending elasticity of DMPC bilayers in fluid crystal phase (L{sub {alpha}}) and the ripple gel (P{sub {beta}}') phase.

  8. High-resolution measurement of electrically-evoked vagus nerve activity in the anesthetized dog

    Science.gov (United States)

    Yoo, Paul B.; Lubock, Nathan B.; Hincapie, Juan G.; Ruble, Stephen B.; Hamann, Jason J.; Grill, Warren M.

    2013-04-01

    Objective. Not fully understanding the type of axons activated during vagus nerve stimulation (VNS) is one of several factors that limit the clinical efficacy of VNS therapies. The main goal of this study was to characterize the electrical recruitment of both myelinated and unmyelinated fibers within the cervical vagus nerve. Approach. In anesthetized dogs, recording nerve cuff electrodes were implanted on the vagus nerve following surgical excision of the epineurium. Both the vagal electroneurogram (ENG) and laryngeal muscle activity were recorded in response to stimulation of the right vagus nerve. Main results. Desheathing the nerve significantly increased the signal-to-noise ratio of the ENG by 1.2 to 9.9 dB, depending on the nerve fiber type. Repeated VNS following nerve transection or neuromuscular block (1) enabled the characterization of A-fibers, two sub-types of B-fibers, and unmyelinated C-fibers, (2) confirmed the absence of stimulation-evoked reflex compound nerve action potentials in both the ipsilateral and contralateral vagus nerves, and (3) provided evidence of stimulus spillover into muscle tissue surrounding the stimulating electrode. Significance. Given the anatomical similarities between the canine and human vagus nerves, the results of this study provide a template for better understanding the nerve fiber recruitment patterns associated with VNS therapies.

  9. 复方利多卡因乳膏对喉罩插入不良反应的抑制作用%Surface anesthetic effect of compound lidocaine cream-coated laryngeal mask airway in patients undergoing modified radical mastectomy under general anesthesia

    Institute of Scientific and Technical Information of China (English)

    张锦英; 沈途

    2011-01-01

    目的 观察复方利多卡因乳膏乳癌改良根治术中喉罩插入时不良反应的抑制作用.方法 择期行全麻乳癌改良根治术的患者80例,ASA Ⅰ~Ⅲ级,随机均分为复方利多卡因乳膏喉罩组(A组)和石蜡油喉罩组(B组),将复方利多卡因乳膏和石蜡油涂抹于喉罩表面.麻醉诱导后插入喉罩,记录麻醉诱导前、喉罩插入前、喉罩插入即刻及喉罩插人后3 min患者SBP、DBP、HR,以及术后咽痛或咽部不适的发生率.结果 与喉罩插入前和A组比较,B组喉罩插入即刻和喉罩插入后3min时SBP、DBP明显升高,HR明显增快(P<0.01).A组患者术中呛咳和术后咽痛、咽部不适感发生率明显低于B组(P<0.05).结论 复方利多卡因乳膏能有效抑制全麻乳癌改良根治术中喉罩插人所引起的咽反射和术后咽痛.%Objective To evaluate the surface anesthetic effect of compound lidocaine crearcoated laryngeal mask airway (LMA) in patients undergoing modified radical mastectomy under general anesthesia. Methods Eighty ASA Ⅰ-Ⅲ patients undergoing modified radical mastectomy under general anesthesia received insertion of LMA coated with either compound lidocaine cream (group A, n = 40) or paraffin oil (group B, n = 40). Systolic blood pressure(SBP), diastolic blood pressure(DBP) and heart rate(HR)were measured during LMA insertion. Incidence of irritating cough and sore throat was recorded after operation. Results Compared with group B, not only SBP, DBP or HR at 0 min, 3 min after LMA insertion were lower, but the incidence of irritating cough and sore throat was significantly also lower in group A (P<0. 01). SBP, DBP and HR at 0 min, 3 min after LMA insertion was higher than that before LMA insertion in B group ( P< 0. 01 ). Conclusion Compound lidocaine cream-coated LMA can inhibit the pharyngeal reaction and reduce the incidence of sore throat in patients undergoing modified radical mastectomy under general anesthesia.

  10. 复方利多卡因乳膏在喉罩全麻腹腔镜胆囊切除术中的应用%Surface anesthetic effect of compound lidocaine cream-coated laryngeal mask airway in patients undergoing laparoscopic cholecystectomy and general anesthesia

    Institute of Scientific and Technical Information of China (English)

    卢静; 兰志勋

    2009-01-01

    目的 观察复方利多卡因在喉罩全麻腹腔镜胆囊切除术中抑制咽反射和术后咽喉痛的效果.方法 将120例ASA Ⅰ~Ⅲ级择期行全麻腹腔镜胆囊切除术的患者随机分为试验组(A组,n=60)和对照组(B组,n=60),分别将复方利多卡因乳膏和石蜡油涂抹于喉罩表面,在麻醉诱导后王入喉罩,记录麻醉诱导前、喉罩置入前、喉罩置入即刻及喉罩置入后3min患者收缩压(SBP)、舒张压(DBP)、心率(HR)以及术后咽痛或咽部不适的发生率.结果 与置入喉罩前相比,A组患者置入喉罩后即刻和置入喉罩后3min时SBP、DBP、HR差异无统计学意义(P>0.05);B组患者上述指标则明显升高,差异有统计学意义(P<0.01).组间比较,A组置入喉罩后的SBP、DBP、HR均低于B组,差异有统计学意义(P<0.01).A组患者术中呛咳和术后咽痛、咽部不适感发生率明显低于B组(P<0.05).结论 复方利多卡因乳膏能有效抑制喉罩全麻胆囊切除术所引起的咽反射和术后咽痛.%Objective To evaluate the surface anesthetic effect of compound lidocaine cream-coated laryngeal mask air-way (LMA) in patients undergoing laparoscopic cholecystectomy (LC) and general anesthesia. Methods 120 ASA Ⅰ~Ⅲ pa-tients undergoing LC and general anesthesia received insertion of LMA coated with either compound lidocaine cream ( A group, n=60) or paraffin oil (B group, n=60). Systolic blood pressure (SBP), diastolic blood pressure (DBP) and heart rate (HR) were measured during LMA insertion. Irritating cough, sore throat were recorded after operation. Results Compared with B group, not only SBP, DBP and HR at 0min,3min after LMA insertion but also the incidence of irritating cough and sore throat was significantly lower in A group (P<0.01). No difference was observed in SBP, DBP and HR before LMA insertion, at 0min, 3min after LMA insertion in A group but SBP, DBP and HR at Omin,3min after LMA insertion was higher than that before LMA insertion

  11. Genistein inhibits carotid sinus baroreceptor activity in anesthetized male rats1

    Institute of Scientific and Technical Information of China (English)

    Hui-juan MA; Yi-xian LIU; Fu-wei WANG; Li-xuan WANG; Rui-rong HE; Yu-ming WU

    2005-01-01

    Aim: To study the effect of genistein (GST) on carotid baroreceptor activity (CBA).Methods: The functional curve of carotid baroreceptor (FCCB) was constructed and the functional parameters of carotid baroreceptor were measured by recording sinus nerve afferent discharge in anesthetized male rats with perfused isolated carotid sinus.Results: GST at 50, 100, and 200 μmol/L inhibited the CBA, which shifted FCCB to the right and downward, with a marked decrease in peak slope and peak integral value of carotid sinus nerve discharge in a concentration-dependent manner.Pretreatment with 100 μmol/L NG-nitro-L-arginine methyl ester, an inhibitor of nitric oxide synthase, did not affect the effect of GST on CBA.Pretreatment with 500 nmol/L Bay K8644, an agonist of calcium channels,could completely abolish the effect of GST on CBA.A potent inhibitor of tyrosine phosphatase, sodium orthovanadate (1 mmol/L), could attenuate the inhibitory effect of GST.Conclusion: GST inhibits CBA, and the effect may be mediated by protein tyrosine kinase inhibition and a decrease in Ca2+ influx through the stretchactivated channels.

  12. Hypertonic saline does not reverse the sodium channel blocking actions of lidocaine: evidence from electrophysiologic and defibrillation studies.

    Science.gov (United States)

    Ujhelyi, M R; Schur, M; Frede, T; Bottorff, M B; Gabel, M; Markel, M L

    1997-01-01

    Studies have shown that increasing extracellular sodium concentration can partially reverse sodium channel blockade. However, there is conflicting in vitro evidence in this regard for lidocaine. The effects of lidocaine on cardiac electrophysiology and defibrillation were studied in a basal and hypernatremic state to determine reversibility of sodium channel blockade. Electrophysiologic studies measured right ventricular effective refractory period at 350 ms pacing cycle length and QRS interval, JT interval, and monophasic action potential duration during sinus rhythm and right ventricular pacing (350 ms cycle length) in 14 pentobarbital-anesthetized swine (25-30 kg). Defibrillation threshold (DFT) was measured by quantitating successful conversion of sustained ventricular fibrillation to normal sinus rhythm. Each pig was randomly assigned to a treatment group with three study phases; group 1 = baseline, lidocaine (20 mg/kg/h), and lidocaine plus placebo (D5W; n = 7); and group 2 = baseline, lidocaine, and lidocaine plus hypertonic saline (2-3 mM/kg/h; n = 7). In groups 1 and 2, lidocaine infused alone significantly (p Lidocaine alone reduced right ventricular action potential duration (APD) in groups 1 and 2 (214 +/- 18 to 206 +/- 20 ms; p lidocaine, DFT and QRS duration values were unaffected (14.7 +/- 5.4 to 16.1 +/- 3.7 J and 103 +/- 12 to 100 +/- 11 ms, respectively). However, APD and JT intervals returned to basal values when hypertonic saline was added to lidocaine (212 +/- 8 to 225 +/- 13; p Lidocaine slowed ventricular conduction velocity and reduced APD. The administration of hypertonic saline to increase extracellular sodium concentrations failed to reverse the effect of lidocaine on conduction-velocity slowing or elevated DFT values. Hypertonic saline did reverse the effects of lidocaine on repolarization parameters. These data suggest that shortening of repolarization is not a mechanism by which lidocaine makes it more difficult to defibrillate the

  13. Hydrogen sulfide facilitates carotid sinus baroreceptor activity in anesthetized male rats

    Institute of Scientific and Technical Information of China (English)

    XIAO Lin; WU Yu-ming; WANG Ru; LIU Yi-xian; WANG Fu-wei; HE Rui-rong

    2007-01-01

    Background It has been reported that hydrogen sulfide (H2S) could relax vascular smooth muscle by direct activation of KATP channels and hyperpolarization of the membrane potential. Recently, our study has shown that H2S facilitated carotid baroreflex. This study was conducted to investigate the effect of H2S on carotid baroreceptor activity (CBA).Methods The functional curve of carotid baroreceptor (FCCB) was constructed and the functional parameters of carotid baroreceptor were measured by recording sinus nerve afferent discharge in anesthetized male rats with perfused isolated carotid sinus.Results H2S (derived from NarHS) 25, 50 and 100 μmol/L facilitated CBA, which shifted FCCB to the left and upward.There was a marked increase in peak slope (PS) and peak integral value of carotid sinus nerve charge (PIV) in a concentration-dependent manner. Pretreatment with glibenclamide (20 μmol/L), a KATP channel blocker, the above effects of H2S on CBA were abolished. Pretreatment with Bay K8644 (an agonist of calcium channels, 500 nmol/L) eliminated the role of H2S on CBA. An inhibitor of cystathionine Y-lyase (CSE), DL-propargylglycine (PPG, 200 μmol/L) inhibited CBA in male rats and shifted FCCB to the right and downward.Conclusions Our results suggest that exogenous H2S exerts a facilitatory role on isolated CBA through opening KATP channels and further closing the calcium channels in vascular smooth muscle. Endogenous H2S may activate CBA in vivo.

  14. Effect of dexmedetomidine priming on convulsion reaction induced by lidocaine.

    Science.gov (United States)

    Wang, Xi-Feng; Luo, Xiao-Ling; Liu, Wei-Cheng; Hou, Ben-Chao; Huang, Jian; Zhan, Yan-Ping; Chen, Shi-Biao

    2016-10-01

    To study the effect of dexmedetomidine priming on convulsion reaction induced by lidocaine.The New Zealand white rabbits were applied for the mechanism study of dexmedetomidine priming for preventing convulsion reaction induced by lidocaine. The influence of dexmedetomidine priming with different doses on the time for convulsion occurrence and the duration time of convulsion induced by lidocaine, as well as contents of excitatory amino acids (aspartate [Asp], glutamate [Glu]) and inhibitory amino acids (glycine [Gly], γ-aminobutyric acid [GABA]) in the brain tissue were investigated.With 3 and 5 μg/kg dexmedetomidine priming, the occurrence times of convulsion were prolonged from 196 seconds to 349 and 414 seconds, respectively. With dexmedetomidine priming, the contents of excitatory amino acids (Asp, Glu) were much reduced at occurrence time of convulsion comparing with that without dexmedetomidine priming, while content of inhibitory amino acids Gly was much enhanced.The application of dexmedetomidine before local anesthetics can improve intoxication dose threshold of the lidocaine, delay occurrence of the convulsion, and helped for the recovery of convulsion induced by lidocaine. The positive effect of dexmedetomidine on preventing convulsion would owe to not only the inhibition of excitatory amino acids (Asp, Glu), but also the promotion of inhibitory amino acids Gly secretion.

  15. Dimethylsulfoxide potentiates the nerve conduction-blocking effect of lidocaine without augmentation of the intracellular lidocaine concentration in the giant axon of crayfish in vitro.

    Science.gov (United States)

    Yano, Takeshi; Ibusuki, Shoichiro; Takasaki, Mayumi; Tsuneyoshi, Isao

    2013-08-01

    The purpose of this study was to investigate how dimethylsulfoxide (DMSO) potentiates the blocking action of lidocaine. A giant axon removed from a crayfish was used to investigate nerve conduction and intracellular lidocaine concentration. The maximum values of the differential waveform (dV/dt max) calculated from evoked action potentials were used for evaluating an inhibition of nerve conduction. The inhibition of the dV/dt max in low-frequency stimulation (tonic block) and high-frequency stimulation (phasic block) after perfusion of 1 mm lidocaine with or without 0.2 vol % DMSO, in which the concentration of DMSO alone had no anesthetic effect, was measured to evaluate the potentiating action of DMSO. The intracellular lidocaine concentration was measured via a lidocaine-sensitive glass microelectrode during 30 min of perfusion of 1 mm lidocaine alone or in combination with DMSO. When applied without lidocaine, DMSO caused a dose-dependent nerve conduction block when used at concentrations >1 vol %. The dV/dt max in the tonic block was significantly decreased when 0.2 vol % DMSO was added to the lidocaine solution (P = 0.004). In the phasic block, there was no significant potentiating action of DMSO. There were no significant differences in the intracellular lidocaine concentrations with or without DMSO. The potentiating effects of DMSO were observed only in the condition of low-frequency stimulation and were not related to the intracellular lidocaine concentration in the giant axon of crayfish in vitro.

  16. Interaction between lidocaine hydrochloride (with and without adrenaline) and various irrigants: A nuclear magnetic resonance analysis

    Science.gov (United States)

    Vidhya, Nirmal; Karthikeyan, Balasubramanian Saravana; Velmurugan, Natanasabapathy; Abarajithan, Mohan; Nithyanandan, Sivasankaran

    2014-01-01

    Background: Interaction between local anesthetic solution, lidocaine hydrochloride (with and without adrenaline), and root canal irrigants such as sodium hypochlorite (NaOCl), ethylene diamine tetra-acetic acid (EDTA), and chlorhexidine (CHX) has not been studied earlier. Hence, the purpose of this in vitro study was to evaluate the chemical interaction between 2% lidocaine hydrochloride (with and without adrenaline) and commonly used root canal irrigants, NaOCl, EDTA, and CHX. Materials and Methods: Samples were divided into eight experimental groups: Group I-Lidocaine hydrochloride (with adrenaline)/3% NaOCl, Group II-Lidocaine hydrochloride (with adrenaline)/17% EDTA, Group III- Lidocaine hydrochloride (with adrenaline)/2% CHX, Group IV-Lidocaine hydrochloride (without adrenaline)/3% NaOCl, Group V-Lidocaine hydrochloride (without adrenaline)/17% EDTA, Group VI-Lidocaine hydrochloride (without adrenaline)/2% CHX, and two control groups: Group VII-Lidocaine hydrochloride (with adrenaline)/deionized water and Group VIII-Lidocaine hydrochloride (without adrenaline)/deionized water. The respective solutions of various groups were mixed in equal proportions (1 ml each) and observed for precipitate formation. Chemical composition of the formed precipitate was then analysed by nuclear magnetic resonance spectroscopy (NMR) and confirmed with diazotation test. Results: In groups I and IV, a white precipitate was observed in all the samples on mixing the respective solutions, which showed a color change to reddish brown after 15 minutes. This precipitate was then analysed by NMR spectroscopy and was observed to be 2,6-xylidine, a reported toxic compound. The experimental groups II, III, V, and VI and control groups VII and VIII showed no precipitate formation in any of the respective samples, until 2 hours. Conclusion: Interaction between lidocaine hydrochloride (with and without adrenaline) and NaOCl showed precipitate formation containing 2,6-xylidine, a toxic compound

  17. [New anesthetics].

    Science.gov (United States)

    Malamed, S F

    2000-01-01

    Since the introduction of cocaine local analgesia in 1886, and the subsequent development of procaine (1904) and other closely related ester-type compounds, dentistry has prided itself on being as close to 'painless' as possible. In the late 1940s the newest group of the local anesthetic compounds, the amides, was introduced. The initial amide local analgesic, lignocaine (Xylocaine), revolutionised pain control in dentistry worldwide. In succeeding years other amide-type local anesthetics, mepivacaine, prilocaine, bupivacaine and etidocaine, were introduced. They gave the dental practitioner a local anesthetic armamentarium which provided pulpal analgesia for periods of from 20 minutes (mepivacaine) to as long as three hours (bupivacaine and etidocaine with adrenaline). In addition these popular drugs proved to be more rapid-acting than the older ester-type drug and, at least from the perspective of allergenicity, more safe. In 1976, in Germany, the newest amide local analgesic, carticaine HCl was introduced into dentistry. Articaine (the generic name was changed) possesses properties similar to lignocaine but has additional properties which made the drug quite attractive to the general dental practitioner. In 1986 articaine was introduced in North America (Canada) where it has become the most used local anesthetic, supplanting lignocaine. Articaine has been approved for use in the United Kingdom. In this introductory discussion we review the development of articaine and discuss its place in the dental local analgesic armamentarium.

  18. The Effect of Lidocaine · HCl on the Fluidity of Native and Model Membrane Lipid Bilayers

    OpenAIRE

    Park, Jun-Seop; Jung, Tae-Sang; Noh, Yang-Ho; Kim, Woo-Sung; Park, Won-Ick; Kim, Young-Soo; Chung, In-Kyo; Sohn, Uy Dong; Bae, Soo-Kyung; Bae, Moon-Kyoung; Jang, Hye-Ock; Yun, Il

    2012-01-01

    The purpose of this study is to investigated the mechanism of pharmacological action of local anesthetic and provide the basic information about the development of new effective local anesthetics. Fluorescent probe techniques were used to evaluate the effect of lidocaine·HCl on the physical properties (transbilayer asymmetric lateral and rotational mobility, annular lipid fluidity and protein distribution) of synaptosomal plasma membrane vesicles (SPMV) isolated from bovine cerebral cortex, a...

  19. Anti-metastatic Potential of Amide-linked Local Anesthetics: Inhibition of Lung Adenocarcinoma Cell Migration and Inflammatory Src Signaling Independent of Sodium Channel Blockade

    Science.gov (United States)

    Piegeler, Tobias; Votta-Velis, E. Gina; Liu, Guoquan; Place, Aaron T.; Schwartz, David E.; Beck-Schimmer, Beatrice; Minshall, Richard D.; Borgeat, Alain

    2012-01-01

    Background Retrospective analysis of patients undergoing cancer surgery suggests the use of regional anesthesia may reduce cancer recurrence and improve survival. Amide-linked local anesthetics have anti-inflammatory properties, although the mechanism of action in this regard is unclear. As inflammatory processes involving Src tyrosine protein kinase and intercellular adhesion molecule-1 are important in tumor growth and metastasis, we hypothesized that amide-linked local anesthetics may inhibit inflammatory Src-signaling involved in migration of adenocarcinoma cells. Methods NCI-H838 lung cancer cells were incubated with Tumor Necrosis Factor-α in absence/presence of ropivacaine, lidocaine, or chloroprocaine (1nM-100μM). Cell migration and total cell lysate Src-activation and Intercellular Adhesion Molecule-1 phosphorylation were assessed. The role of voltage-gated sodium-channels in the mechanism of local anesthetic effects was also evaluated. Results Ropivacaine treatment (100μM) of H838 cells for 20 minutes decreased basal Src activity by 62% (p=0.003), and both ropivacaine and lidocaine co-administered with Tumor Necrosis Factor-α statistically significantly decreased Src-activation and Intercellular Adhesion Molecule-1 phosphorylation, whereas chloroprocaine had no such effect. Migration of these cells at 4 hours was inhibited by 26% (p=0.005) in presence of 1μM ropivacaine and 21% by 1μM lidocaine (p=0.004). These effects of ropivacaine and lidocaine were independent of voltage-gated sodium-channel inhibition. Conclusions This study indicates that amide-, but not ester-linked local anesthetics may provide beneficial anti-metastatic effects. The observed inhibition of NCI-H838 cell migration by lidocaine and ropivacaine was associated with the inhibition of Tumor Necrosis Factor-α-induced Src-activation and Intercellular Adhesion Molecule-1 phosphorylation, providing the first evidence of a molecular mechanism which appears to be independent of their

  20. Local Anesthetic Activity from Extracts, Fractions and Pure Compounds from the Roots of Ottonia anisum Spreng. (Piperaceae).

    Science.gov (United States)

    López, Kelvin S E; Marques, André M; Moreira, Davyson DE L; Velozo, Leosvaldo S; Sudo, Roberto T; Zapata-Sudo, Gisele; Guimarães, Elsie F; Kaplan, Maria Auxiliadora C

    2016-01-01

    Piperaceae species can be found worldwide in tropical and subtropical areas and many of them have been used for centuries in traditional folk medicine and in culinary. In Brazil, species of Piperaceae are commonly used in some communities as local anesthetic and analgesic. Countrified communities have known some species of the genus Ottonia as "anestesia" and it is a common habit of chewing leaves and roots of Ottonia species to relief toothache. The purpose of this study is to report our findings on new molecules entities obtained from the roots of Ottonia anisum Spreng, in which local anesthetic activity (sensory blockage) is demonstrated for the first time in vivo guinea pig model. Phytochemical investigation led to the isolation of three amides (pipercallosidine, piperine and valeramide) and in an enriched mixture of seven amides (valeramide, 4,5-dihydropiperlonguminine, N-isobutil-6-piperonil-2-hexenamide, piperovatine, dihydropipercallosidine, pipercallosidine and pipercallpsine). Our findings demonstrated the anesthetic potential for the methanolic extract from roots, its n-hexane partition and amides from O. anisum and it is in agreement with ethnobotanical survey.

  1. Local Anesthetic Activity from Extracts, Fractions and Pure Compounds from the Roots of Ottonia anisum Spreng. (Piperaceae

    Directory of Open Access Journals (Sweden)

    KELVIN S.E. LÓPEZ

    Full Text Available ABSTRACT Piperaceae species can be found worldwide in tropical and subtropical areas and many of them have been used for centuries in traditional folk medicine and in culinary. In Brazil, species of Piperaceae are commonly used in some communities as local anesthetic and analgesic. Countrified communities have known some species of the genus Ottonia as "anestesia" and it is a common habit of chewing leaves and roots of Ottonia species to relief toothache. The purpose of this study is to report our findings on new molecules entities obtained from the roots of Ottonia anisum Spreng, in which local anesthetic activity (sensory blockage is demonstrated for the first time in vivo guinea pig model. Phytochemical investigation led to the isolation of three amides (pipercallosidine, piperine and valeramide and in an enriched mixture of seven amides (valeramide, 4,5-dihydropiperlonguminine, N-isobutil-6-piperonil-2-hexenamide, piperovatine, dihydropipercallosidine, pipercallosidine and pipercallpsine. Our findings demonstrated the anesthetic potential for the methanolic extract from roots, its n-hexane partition and amides from O. anisum and it is in agreement with ethnobotanical survey.

  2. The General Anesthetic Propofol Excites Nociceptors by Activating TRPV1 and TRPA1 Rather than GABAA Receptors*

    Science.gov (United States)

    Fischer, Michael J. M.; Leffler, Andreas; Niedermirtl, Florian; Kistner, Katrin; Eberhardt, Mirjam; Reeh, Peter W.; Nau, Carla

    2010-01-01

    Anesthetic agents can induce a paradox activation and sensitization of nociceptive sensory neurons and, thus, potentially facilitate pain processing. Here we identify distinct molecular mechanisms that mediate an activation of sensory neurons by 2,6-diisopropylphenol (propofol), a commonly used intravenous anesthetic known to elicit intense pain upon injection. Clinically relevant concentrations of propofol activated the recombinant transient receptor potential (TRP) receptors TRPA1 and TRPV1 heterologously expressed in HEK293t cells. In dorsal root ganglion (DRG) neurons, propofol-induced activation correlated better to expression of TRPA1 than of TRPV1. However, pretreatment with the protein kinase C activator 4β-phorbol 12-myristate 13-acetate (PMA) resulted in a significantly sensitized propofol-induced activation of TRPV1 in DRG neurons as well as in HEK293t cells. Pharmacological and genetic silencing of both TRPA1 and TRPV1 only partially abrogated propofol-induced responses in DRG neurons. The remaining propofol-induced activation was abolished by the selective γ-aminobutyric acid, type A (GABAA) receptor antagonist picrotoxin. Propofol but not GABA evokes a release of calcitonin gene-related peptide, a key component of neurogenic inflammation, from isolated peripheral nerves of wild-type but not TRPV1 and TRPA1-deficient mice. Moreover, propofol but not GABA induced an intense pain upon intracutaneous injection. As both the release of calcitonin gene-related peptide and injection pain by propofol seem to be independent of GABAA receptors, our data identify TRPV1 and TRPA1 as key molecules for propofol-induced excitation of sensory neurons. This study warrants further investigations into the role of anesthetics to induce nociceptor sensitization and to foster postoperative pain. PMID:20826794

  3. Pharmacokinetics of lidocaine with epinephrine following local anesthesia reversal with phentolamine mesylate.

    Science.gov (United States)

    Moore, Paul A; Hersh, Elliot V; Papas, Athena S; Goodson, J Max; Yagiela, John A; Rutherford, Bruce; Rogy, Seigried; Navalta, Laura

    2008-01-01

    Phentolamine mesylate accelerates recovery from oral soft tissue anesthesia in patients who have received local anesthetic injections containing a vasoconstrictor. The proposed mechanism is that phentolamine, an alpha-adrenergic antagonist, blocks the vasoconstriction associated with the epinephrine used in dental anesthetic formulations, thus enhancing the systemic absorption of the local anesthetic from the injection site. Assessments of the pharmacokinetics of lidocaine and phentolamine, and the impact of phentolamine on the pharmacokinetics of lidocaine with epinephrine were performed to characterize this potentially valuable strategy. The blood levels of phentolamine were determined following its administration intraorally and intravenously. Additionally, the effects of phentolamine mesylate on the pharmacokinetics of intraoral injections of lidocaine with epinephrine were evaluated. Sixteen subjects were enrolled in this phase 1 trial, each receiving 4 drug treatments: 1 cartridge lidocaine/epinephrine followed after 30 minutes by 1 cartridge phentolamine (1L1P), 1 cartridge phentolamine administered intravenously (1Piv), 4 cartridges lidocaine/epinephrine followed after 30 minutes by 2 cartridges phentolamine (4L2P), and 4 cartridges lidocaine/epinephrine followed by no phentolamine (4L). Pharmacokinetic parameters estimated for phentolamine, lidocaine, and epinephrine included peak plasma concentration (Cmax), time to peak plasma concentration (Tmax), area under the plasma concentration-time curve from 0 to the last time point (AUClast) or from time 0 to infinity (AUCinf), elimination half-life (t1/2), clearance (CL), and volume of distribution (Vd). The phentolamine Tmax occurred earlier following the intravenous administration of 1Piv (7 minutes than following its submucosal administration in treatment 1L1P (15 minutes) or 4L2P (11 minutes). The phentolamine t1/2, CL, and Vd values were similar for 1L1P, 1Piv, and 4L2P. The Tmax for lidocaine occurred

  4. Antinociceptive effects of systemic lidocaine: involvement of the spinal glycinergic system.

    Science.gov (United States)

    Muth-Selbach, Uta; Hermanns, Henning; Stegmann, Jens Ulrich; Kollosche, Kathrin; Freynhagen, Rainer; Bauer, Inge; Lipfert, Peter

    2009-06-24

    Beside their action on voltage-gated Na(+) channels, local anesthetics are known to exert a variety of effects via alternative mechanisms. The antinociceptive effect of lidocaine is well documented, yet the exact mechanism is not fully understood. Whether glycinergic mechanisms, which play a pivotal role in pain modulation, are involved in lidocaine-induced antinociception is hitherto unclear. In the present study, lidocaine was injected intravenously in rats using the formalin test for acute pain and the chronic constriction injury model for neuropathic pain. The effect of intrathecally administered d-serine (an agonist at the glycine-binding site at the NMDA-receptor), its inactive isomer l-serine, CGP 78608 (antagonist at the glycineB-site of the NMDA-receptor) and strychnine (antagonist at inhibitory glycine-receptors) on lidocaine-induced antinociception was examined. Systemically administered lidocaine was antinociceptive in both acute and chronic pain model. In the formalin test, the effect of lidocaine was antagonized by d-serine, but not by l-serine or strychnine. In the chronic constriction injury model, antinociception evoked by lidocaine was reduced by d-serine, strychnine and CGP 78608, while l-serine had no effect. These results indicate a modulatory effect of lidocaine on the NMDA-receptor. Additionally, since in our study lidocaine-induced antinociception was antagonized by both glycineB-site modulators and strychnine our results may favor the hypothesis of a general glycine-like action of lidocaine or some of its metabolites on inhibitory strychnine-sensitive receptors and on strychnine-insensitive glycine receptors.

  5. Comparison of Iontophoretic Lidocaine to EMLA Cream for Pain Reduction Prior to Intravenous Fannulation in Adults

    Science.gov (United States)

    2000-10-01

    1957, used iontophoresis of local anesthetics for the treatment of trigeminal neuralgia . Gibson and Cooke, in 1959, used lidocaine and pilocarpine...al. 1994). Other clinical uses of EMLA cream include: lumbar puncture, epidural injections, drug reservoir injections, skin surgery, genitourinary...surgery, ear, nose, throat, oral surgery, lithotripsy, and there are some anecdotal reports of its use for the treatment of postherpetic neuralgia

  6. Determination of lidocaine in plasma by direct solid-phase microextraction combined with gas chromatography

    NARCIS (Netherlands)

    Koster, EHM; Wemes, C; Morsink, JB; de Jong, GJ

    2000-01-01

    Direct-immersion solid-phase microextraction (SPME) has been used to extract the local anesthetic lidocaine from human plasma. A simplified model shows the relationship between the total amount of drug in plasma and the amount of drug extracted. The model takes into account that the drug participate

  7. Alkalinized lidocaine versus lidocaine gel as local anesthesia prior to intra-vesical botulinum toxin (BoNTA) injections: A prospective, single center, randomized, double-blind, parallel group trial of efficacy and morbidity.

    Science.gov (United States)

    Nambiar, Arjun K; Younis, Ayman; Khan, Zainab A; Hildrup, Iona; Emery, Simon J; Lucas, Malcolm G

    2016-04-01

    To assess the efficacy and morbidity of alkalinized lidocaine solution compared to lidocaine gel for intra-vesical anesthesia during botulinum toxin (BoNTA) injections in a statistically powered, prospective, parallel group, double-blind randomized controlled trial. Fifty-four patients of either sex were randomized to receive either alkalinized lidocaine (AL) solution (10 ml 8.4% sodium bicarbonate + 20 ml 2% lidocaine solution + 22 ml sterile Aquagel®) or lidocaine gel (LG) (22 ml standard 2% lidocaine gel Instillagel® + 30 ml 0.9% normal saline solution). Primary outcome was average pain (assessed by 100 mm visual analog score) felt during intra-vesical BoNTA injections performed at least 20 min after instillation. Secondary outcome was the rate of adverse events. Of 60 randomized patients 54 received the allocated intervention and were analyzed. Mean pain score in the AL group was 17.11 mm (95%CI 8.65-25.57 mm) and in the LG group was 19.53 mm (95%CI 13.03-26.03mm) with no significant difference between the groups. Cost of interventional medication in the AL group was almost double that of the LG group. No adverse events were attributable to local anesthetic instillation in either group. Alkalinized lidocaine solution is not superior to lidocaine gel for anesthesia during intra-vesical BoNTA injections, and the higher cost precludes its use over lidocaine gel at our centre. We have used the results of this study to adapt our local protocol for BoNTA injections and continue to use lidocaine gel as the local anesthetic of choice. Neurourol. Urodynam. 35:522-527, 2016. © 2015 Wiley Periodicals, Inc. © 2015 Wiley Periodicals, Inc.

  8. Intraarticular lidocaine versus intravenous analgesic for reduction of acute anterior shoulder dislocations. A prospective randomized study.

    Science.gov (United States)

    Matthews, D E; Roberts, T

    1995-01-01

    We performed a prospective, randomized study to evaluate the use of injected lidocaine as an anesthetic for closed reduction of acute anterior shoulder dislocations. Thirty consecutive patients who presented at the emergency department with acute anterior shoulder dislocations were randomly placed in one of two groups. One group received an intraarticular injection of 20 ml of 1% lidocaine and the other group, intravenous injections of morphine sulfate and midazolam. The groups were compared regarding time of reduction maneuver, difficulty of reduction, subjective pain, complications, and total time spent in the emergency department. The lidocaine provided adequate anesthesia and secondary relief of muscle spasm in 15 of 15 (100%) patients. When compared with the intravenous sedation group, the lidocaine group showed no statistically significant difference in time for reduction maneuver, difficulty of reduction, or subjective pain. The lidocaine group had no complications and had a statistically significant shorter emergency department visit when compared with the intravenous sedation group (mean, 78 minutes versus 186 minutes; P = 0.004). Lidocaine provides excellent anesthesia for patients with uncomplicated anterior shoulder dislocations and can be very beneficial when sedation is contraindicated. Lidocaine injections also proved to be cost effective in our institution, reducing total costs by as much as 62%.

  9. Identifying and Managing Local Anesthetic Allergy in Dermatologic Surgery.

    Science.gov (United States)

    Fathi, Ramin; Serota, Marc; Brown, Mariah

    2016-02-01

    Local anesthetic (LA) allergy is a concern for dermatologic surgeons given the large number of procedures performed yearly with LAs. Many patients also have anxiety about past or potential anesthesia allergy. This article will review the symptoms of IgE-mediated allergic reactions, the prevalence of IgE-mediated LA allergy, discuss common mimics of LA, and propose a practical approach for diagnostic and therapeutic options for LA allergy for the dermatologic surgeon in practice. A literature search of Pubmed using keywords "lidocaine," "local anesthetic," "hypersensitivity," and "allergy" was performed. Amide anesthetics result in the most reports of true local anesthetic immediate hypersensitivity. True IgE-mediated anaphylaxis to local anesthesia is very rare. Dermatologic surgeons should be aware of the symptoms of anesthetic allergy and its mimickers, as well as how to manage allergic reactions in their clinical practice.

  10. Preemptive analgesic effect of lidocaine in a chronic neuropathic pain model Efeito analgésico preemptivo da lidocaína em modelo de dor crônica neuropática

    OpenAIRE

    Batista, Leonardo M; Igor M. Batista; Almeida, João P.; Carlos H. Carvalho; Castro-Costa,Samuel B. de; CASTRO-COSTA,CARLOS M. DE

    2009-01-01

    Preemptive analgesia inhibits the progression of pain caused by surgical lesions. To analyze the effect of lidocaine on postoperative pain relief, we performed compression of the right sciatic nerve in Wistar rats and observed the differences on behavior between the group that received lidocaine and the group that was not treated with the local anesthetics pre-operatively. Group 1 was not operated (control); group 2 underwent the sciatic nerve ligature without lidocaine; group 3, underwent su...

  11. In Vivo Quantitation of Local Anesthetic Suppression of Leukocyte Adherence

    Science.gov (United States)

    Giddon, D. B.; Lindhe, J.

    1972-01-01

    Using intravital microscopy, topically applied amide-type local anesthetics suppressed the adherence of leukocytes to the venular endothelium within surgical defects in the hamster cheek pouch. The response was reversible with physiologic saline and was localized to venules within the defect. Quantitation in terms of the percent of initially adhering leukocytes remaining in place on the venule wall at each minute following application of lidocaine and physiologic saline, respectively, revealed the suppression to be reliably related to the concentration, viz: 20.0 >10.0 >5.0 >0.0 mg ml of commercially available Xylocaine® (lidocaine) HCl. ImagesFig 1Fig 1 PMID:5049429

  12. Liposomal formulations of prilocaine, lidocaine and mepivacaine prolong analgesic duration.

    Science.gov (United States)

    Cereda, Cíntia Maria Saia; Brunetto, Giovana Bruschini; de Araújo, Daniele Ribeiro; de Paula, Eneida

    2006-11-01

    A laboratory investigation was undertaken to compare the in vivo antinociceptive effects of 2% liposomal formulations of prilocaine (PLC), lidocaine (LDC) and mepivacaine (MVC) compared to plain solutions of each of these three local anesthetics. Large unilamellar vesicles were prepared by extrusion (400 nm), at pH 7.4. The membrane/water partition coefficients were obtained from encapsulation efficiency values, after incorporation of each local anesthetic to the vesicles. The anesthetic effect of each liposomal formulation was compared to the respective local anesthetic solution in water, using the infraorbital nerve-blockade test, in rats. The partition coefficients were: 57 for PLC, 114 for LDC and 93 for MVC. In vivo results showed that local anesthetic-free liposomes, used as control, had no analgesic effect. In contrast, the encapsulated formulations induced increased intensities of total anesthetic effect (35.3%, 26.1% and 57.1%) and time for recovery (percentage increases of 30%, 23.1% and 56%), respectively, for PLC, LDC and MVC when compared to the plain solutions (P Mepivacaine was affected to the greatest extent, while LDC benefited least from liposome encapsulation, possibly due to greater vasodilatory properties of LDC.

  13. Recognition of local anesthetics by alphabeta+ T cells.

    Science.gov (United States)

    Zanni, M P; von Greyerz, S; Hari, Y; Schnyder, B; Pichler, W J

    1999-02-01

    Patients with drug allergy show a specific immune response to drugs. Chemically nonreactive drugs like, for example, local anesthetics are directly recognized by alphabeta+ T cells in an HLA-DR restricted way, as neither drug metabolism nor protein processing is required for T cell stimulation. In this study we identified some of the structural requirements that determine cross-reactivity of T cells to local anesthetics, with the aim to improve the molecular basis for the selection of alternatives in individuals sensitized to a certain local anesthetic and to better understand presentation and T cell recognition of these drugs. Fifty-five clones (52 lidocaine specific, three mepivacaine specific from two allergic donors) were analyzed. Stimulatory compounds induced a down-regulation of the T cell receptor, demonstrating that these non-peptide antigens are recognized by the T cell receptor itself. A consistent cross-reactivity between lidocaine and mepivacaine was found, as all except one lidocaine specific clone proliferated to both drugs tested. Sixteen chemically related local anesthetics (including ester local anesthetics, OH- and desalkylated metabolites) were used to identify structural requirements for T cell recognition. Each of the four clones examined in detail was uniquely sensitive to changes in the structures of the local anesthetic: clone SFT24, i.e., did not recognize any of the tested OH- or desalkylated metabolites, while the clone OFB2 proliferated to all OH-metabolites and other differently modified molecules. The broadly reactive clone OFB2 allowed us to propose a model, suggesting that the structure of the amine side chain of local anesthetics is essential for recognition by the T cell receptor.

  14. Comparison of hemodynamic effects of lidocaine, prilocaine and mepivacaine solutions without vasoconstrictor in hypertensive patients.

    Science.gov (United States)

    Ezmek, Bahadir; Arslan, Ahmet; Delilbasi, Cagri; Sencift, Kemal

    2010-01-01

    Local anesthetic solutions with vasoconstrictors are not contraindicated in hypertensive patients, but due to their hemodynamic effects, local anesthetics without vasoconstrictors are mainly preferred by the clinicians. The aim of this study was to compare hemodynamic effects of three different local anesthetics without vasoconstrictors during tooth extraction in hypertensive patients. Sixty-five mandibular molars and premolars were extracted in 60 hypertensive patients (29 females and 31 males; mean age: 66.95 ± 10.87 years; range: 38 to 86 years old). Inferior alveolar and buccal nerve blocks were performed with 2% lidocaine hydrochloride (HCl), 2% prilocaine HCl or 3% mepivacaine HCl without vasoconstrictor. Hemodynamic parameters namely systolic blood pressure (SBP), diastolic blood pressure (DBP), mean arterial pressure (MAP), heart rate (HR), saturation rate (SR), rate pressure product (RPP) and pressure rate quotient (PRQ) were investigated before and at different intervals after anesthetic injection. The hemodynamic effects of the three agents were similar to each other, although some significance was observed for DBP, MAP, RPP and PRQ values in the lidocaine, prilocaine and mepivacaine groups. Lidocaine, prilocaine and mepivacaine solutions without vasoconstrictor can be safely used in hypertensive patients. It is advisable that dental practitioners select anesthetic solutions for hypertensive patients considering their cardiovascular effects in order to provide patient comfort and safety.

  15. Comparison of hemodynamic effects of lidocaine, prilocaine and mepivacaine solutions without vasoconstrictor in hypertensive patients

    Directory of Open Access Journals (Sweden)

    Bahadir Ezmek

    2010-08-01

    Full Text Available OBJECTIVE: Local anesthetic solutions with vasoconstrictors are not contraindicated in hypertensive patients, but due to their hemodynamic effects, local anesthetics without vasoconstrictors are mainly preferred by the clinicians. The aim of this study was to compare hemodynamic effects of three different local anesthetics without vasoconstrictors during tooth extraction in hypertensive patients. MATERIAL AND METHODS: Sixty-five mandibular molars and premolars were extracted in 60 hypertensive patients (29 females and 31 males; mean age: 66.95 ± 10.87 years; range: 38 to 86 years old. Inferior alveolar and buccal nerve blocks were performed with 2% lidocaine hydrochloride (HCl, 2% prilocaine HCl or 3% mepivacaine HCl without vasoconstrictor. Hemodynamic parameters namely systolic blood pressure (SBP, diastolic blood pressure (DBP, mean arterial pressure (MAP, heart rate (HR, saturation rate (SR, rate pressure product (RPP and pressure rate quotient (PRQ were investigated before and at different intervals after anesthetic injection. RESULTS: The hemodynamic effects of the three agents were similar to each other, although some significance was observed for DBP, MAP, RPP and PRQ values in the lidocaine, prilocaine and mepivacaine groups. CONCLUSION: Lidocaine, prilocaine and mepivacaine solutions without vasoconstrictor can be safely used in hypertensive patients. It is advisable that dental practitioners select anesthetic solutions for hypertensive patients considering their cardiovascular effects in order to provide patient comfort and safety.

  16. Nebulized lidocaine blunts airway hyper-responsiveness in experimental feline asthma.

    Science.gov (United States)

    Nafe, Laura A; Guntur, Vamsi P; Dodam, John R; Lee-Fowler, Tekla M; Cohn, Leah A; Reinero, Carol R

    2013-08-01

    Nebulized lidocaine may be a corticosteroid-sparing drug in human asthmatics, reducing airway resistance and peripheral blood eosinophilia. We hypothesized that inhaled lidocaine would be safe in healthy and experimentally asthmatic cats, diminishing airflow limitation and eosinophilic airway inflammation in the latter population. Healthy (n = 5) and experimentally asthmatic (n = 9) research cats were administered 2 weeks of nebulized lidocaine (2 mg/kg q8h) or placebo (saline) followed by a 2-week washout and crossover to the alternate treatment. Cats were anesthetized to measure the response to inhaled methacholine (MCh) after each treatment. Placebo and doubling doses of methacholine (0.0625-32.0000 mg/ml) were delivered and results were expressed as the concentration of MCh increasing baseline airway resistance by 200% (EC200Raw). Bronchoalveolar lavage was performed after each treatment and eosinophil numbers quantified. Bronchoalveolar lavage fluid (BALF) % eosinophils and EC200Raw within groups after each treatment were compared using a paired t-test (P eosinophils in asthmatic cats treated with lidocaine (36±10%) or placebo (33 ± 6%). However, lidocaine increased the EC200Raw compared with placebo 10 ± 2 versus 5 ± 1 mg/ml; P = 0.043). Chronic nebulized lidocaine was well-tolerated in all cats, and lidocaine did not induce airway inflammation or airway hyper-responsiveness in healthy cats. Lidocaine decreased airway response to MCh in asthmatic cats without reducing airway eosinophilia, making it unsuitable for monotherapy. However, lidocaine may serve as a novel adjunctive therapy in feline asthmatics with beneficial effects on airflow obstruction.

  17. Vasoconstriction Potency Induced by Aminoamide Local Anesthetics Correlates with Lipid Solubility

    Directory of Open Access Journals (Sweden)

    Hui-Jin Sung

    2012-01-01

    Full Text Available Aminoamide local anesthetics induce vasoconstriction in vivo and in vitro. The goals of this in vitro study were to investigate the potency of local anesthetic-induced vasoconstriction and to identify the physicochemical property (octanol/buffer partition coefficient, pKa, molecular weight, or potency of local anesthetics that determines their potency in inducing isolated rat aortic ring contraction. Cumulative concentration-response curves to local anesthetics (levobupivacaine, ropivacaine, lidocaine, and mepivacaine were obtained from isolated rat aorta. Regression analyses were performed to determine the relationship between the reported physicochemical properties of local anesthetics and the local anesthetic concentration that produced 50% (ED50 of the local anesthetic-induced maximum vasoconstriction. We determined the order of potency (ED50 of vasoconstriction among local anesthetics to be levobupivacaine > ropivacaine > lidocaine > mepivacaine. The relative importance of the independent variables that affect the vasoconstriction potency is octanol/buffer partition coefficient > potency > pKa > molecular weight. The ED50 in endothelium-denuded aorta negatively correlated with the octanol/buffer partition coefficient of local anesthetics (r2=0.9563; P<0.001. The potency of the vasoconstriction in the endothelium-denuded aorta induced by local anesthetics is determined primarily by lipid solubility and, in part, by other physicochemical properties including potency and pKa.

  18. Mimosa pudica, Dionaea muscipula and anesthetics.

    Science.gov (United States)

    De Luccia, Thiago Paes de Barros

    2012-09-01

    Some studies showed that anesthetics reduce the response of physical stimuli in Mimosa pudica and in Venus Flytrap (Dionaea muscipula), peculiar plants that have the ability to respond to touch stimuli. In this research we tested the effects of ketamine, lidocaine, diethyl ether, and amlodipine on the movements of Mimosa pudica and Venus Flytrap. With a literature review, we tried to bring elements to theorize about the interaction of these substances with these plants. The angular displacement in Mimosa´s petiole and in Dionaea leaves is what was measured to compare the drugs group with control groups.

  19. Effects of mixture of lidocaine and ropivacaine at different concentrations on the central nervous system and cardiovascular toxicity in rats

    Institute of Scientific and Technical Information of China (English)

    WAN Qiu-xia; BO Yu-long; LI Hai-bo; LI Wen-zhi

    2010-01-01

    Background Lidocaine and ropivacaine are often combined in clinical practice to obtain a rapid onset and a prolonged duration of action. However, the systemic toxicity of their mixture at different concentrations is unclear. This study aimed to compare the systemic toxicity of the mixture of ropivacaine and lidocaine at different concentrations when administered intravenously in rats.Methods Forty-eight male Wistar rats were randomly divided into 4 groups (n=12 each): 0.5% ropivacaine (group Ⅰ); 1.0% ropivacaine and 1.0% lidocaine mixture (group Ⅱ); 1.0% ropivacaine and 2.0% lidocaine mixture (group Ⅲ); and 1.0% lidocaine (group IV). Local anesthetics were infused at a constant rate until cardiac arrest. Electrocardiogram, electroencephalogram and arterial blood pressure were continuously monitored. The onset of toxic manifestations (seizure, dysrhythmia, and cardiac arrest) was recorded, and then the doses of local anesthetics were calculated. Arterial blood samples were drawn for the determination of local anesthetics concentrations by high-performance liquid chromatography.Results The onset of dysrhythmia was later significantly in group IV than in group Ⅰ, group Ⅱ, and group Ⅲ (P 0.05). The onset of seizure, cardiac arrest in group Ⅰ ((9.2±1.0) min, (37.0±3.0) min) was similar to that in group Ⅱ ((9.1±0.9) min, (35.0±4.0) min) (P>0.05), but both were later in group Ⅲ ((7.5±0.7) min, (28.0±3.0) min) (P0.05).Conclusions The systemic toxicity of the mixture of 1.0% ropivacaine and 2.0% lidocaine is the greatest while that of 1.0% lidocaine is the least. However, the systemic toxicity of the mixture of 1.0% ropivacaine and 1.0% lidocaine is similar to that of 0.5% ropivacaine alone.

  20. Chronic Treatment with Anesthetic Propofol Improves Cognitive Function and Attenuates Caspase Activation in Both Aged and Alzheimer's Disease Transgenic Mice

    Science.gov (United States)

    Dong, Yuanlin; Yu, Buwei; Xia, Weiming; Xie, Zhongcong

    2014-01-01

    There is a need to seek new treatment(s) for Alzheimer's disease (AD). A recent study showed that AD patients may have decreased levels of functional GABA receptors. Propofol, a commonly used anesthetic, is a GABA receptor agonist. We therefore set out to perform a proof of concept study to determine whether chronic treatment with propofol (50 mg/kg/week) can improve cognitive function in both aged wild-type (WT) and AD transgenic (Tg) mice. Propofol was administrated to the WT and AD Tg mice once a week for 8 or 12 weeks, respectively. Morris water maze was used to assess the cognitive function of the mice following the propofol treatment. Activation of caspase-3, caspase-9, and caspase-8 was investigated using western blot analysis at the end of the propofol treatment. In the mechanistic studies, effects of propofol, amyloid-β protein (Aβ), and GABA receptor antagonist flumazenil on caspase-3 activation and opening of the mitochondrial permeability transition pore were assessed in H4 human neuroglioma and mouse neuroblastoma cells by western blot analysis and flow cytometry. Here we showed that the propofol treatment improved cognitive function and attenuated brain caspase-3 and caspase-9 activation in both aged WT and AD Tg mice. Propofol attenuated Aβ-induced caspase-3 activation and opening of the mitochondrial permeability transition pore in the cells, and flumazenil inhibited the propofol's effects. These results suggested that propofol might improve cognitive function via attenuating the Aβ-induced mitochondria dysfunction and caspase activation, which explored the potential that anesthetic propofol could improve cognitive function in elderly and AD patients. PMID:24643139

  1. Evaluation of sciatic nerve damage following intraneural injection of bupivacaine, levobupivacaine and lidocaine in rats.

    Science.gov (United States)

    Sen, Oznur; Sayilgan, Nevzat Cem; Tutuncu, Ayse Cigdem; Bakan, Mefkur; Koksal, Guniz Meyanci; Oz, Huseyin

    2016-01-01

    The local anesthetics may cause neurotoxicity. We aimed to compare the neurotoxic potential of different local anesthetics, local anesthetic induced nerve damage and pathological changes of a peripheral nerve. Sixty Wistar rats weighing 200-350g were studied. Rats were assigned into 3 groups and 26-gauge needle was inserted under magnification into the left sciatic nerve and 0.2mL of 0.5% bupivacaine, 5% levobupivacaine, and 2% lidocaine were injected intraneurally. An individual who was blind to the specifics of the injection monitored the neurologic function on postoperative 1st day, and daily thereafter. Neurologic examination included assessment for the presence and severity of nociception and grasping reflexes. At the 7th day sciatic nerve specimen was taken for evaluation of histopathologic changes. There was no statistical difference detected among groups regarding grasping reflex and histopathologic evaluation. Two cases in bupivacaine group, 1 case in levobupivacaine group and 2 cases in lidocaine group had slight grasping, while 1 case in lidocaine group had no grasping reflex on the seventh day. Severe axonal degeneration was observed in all groups, respectively in bupivacaine group 4 (20%), levobupivacaine group 3 (15%), and lidocaine group 6 (30%). In all groups, histopathological damage frequency and severity were more than the motor deficiency. Copyright © 2015 Sociedade Brasileira de Anestesiologia. Published by Elsevier Editora Ltda. All rights reserved.

  2. [Evaluation of sciatic nerve damage following intraneural injection of bupivacaine, levobupivacaine and lidocaine in rats].

    Science.gov (United States)

    Sen, Oznur; Sayilgan, Nevzat Cem; Tutuncu, Ayse Cigdem; Bakan, Mefkur; Koksal, Guniz Meyanci; Oz, Huseyin

    2016-01-01

    The local anesthetics may cause neurotoxicity. We aimed to compare the neurotoxic potential of different local anesthetics, local anesthetic induced nerve damage and pathological changes of a peripheral nerve. Sixty Wistar rats weighing 200-350g were studied. Rats were assigned into 3 groups and 26-gauge needle was inserted under magnification into the left sciatic nerve and 0.2mL of 0.5% bupivacaine, 5% levobupivacaine, and 2% lidocaine were injected intraneurally. An individual who was blind to the specifics of the injection monitored the neurologic function on postoperative 1st day, and daily thereafter. Neurologic examination included assessment for the presence and severity of nociception and grasping reflexes. At the 7th day sciatic nerve specimen was taken for evaluation of histopathologic changes. There was no statistical difference detected among groups regarding grasping reflex and histopathologic evaluation. Two cases in bupivacaine group, 1 case in levobupivacaine group and 2 cases in lidocaine group had slight grasping, while 1 case in lidocaine group had no grasping reflex on the seventh day. Severe axonal degeneration was observed in all groups, respectively in bupivacaine group 4 (20%), levobupivacaine group 3 (15%), and lidocaine group 6 (30%). In all groups, histopathological damage frequency and severity were more than the motor deficiency. Copyright © 2015 Sociedade Brasileira de Anestesiologia. Publicado por Elsevier Editora Ltda. All rights reserved.

  3. Evaluation of sciatic nerve damage following intraneural injection of bupivacaine, levobupivacaine and lidocaine in rats

    Directory of Open Access Journals (Sweden)

    Oznur Sen

    2016-06-01

    Full Text Available ABSTRACT OBJECTIVE: The local anesthetics may cause neurotoxicity. We aimed to compare the neurotoxic potential of different local anesthetics, local anesthetic induced nerve damage and pathological changes of a peripheral nerve. METHODS: Sixty Wistar rats weighing 200-350 g were studied. Rats were assigned into 3 groups and 26-gauge needle was inserted under magnification into the left sciatic nerve and 0.2 mL of 0.5% bupivacaine, 5% levobupivacaine, and 2% lidocaine were injected intraneurally. An individual who was blind to the specifics of the injection monitored the neurologic function on postoperative 1st day, and daily thereafter. Neurologic examination included assessment for the presence and severity of nociception and grasping reflexes. At the 7th day sciatic nerve specimen was taken for evaluation of histopathologic changes. RESULTS: There was no statistical difference detected among groups regarding grasping reflex and histopathologic evaluation. Two cases in bupivacaine group, 1 case in levobupivacaine group and 2 cases in lidocaine group had slight grasping, while 1 case in lidocaine group had no grasping reflex on the seventh day. Severe axonal degeneration was observed in all groups, respectively in bupivacaine group 4 (20%, levobupivacaine group 3 (15%, and lidocaine group 6 (30%. CONCLUSION: In all groups, histopathological damage frequency and severity were more than the motor deficiency.

  4. Anesthetic activity and bio-guided fractionation of the essential oil of Aloysia gratissima (Gillies & Hook. Tronc. in silver catfish Rhamdia quelen

    Directory of Open Access Journals (Sweden)

    SIMONE C. BENOVIT

    2015-09-01

    Full Text Available This work aimed to determine the efficacy of the essential oil of A. gratissima as anesthetic for silver catfish, and to perform the bio-guided fractionation of essential oil aiming to isolate compounds responsible for the noted effects. Fish were submitted to anesthesia bath with essential oil, its fractions and isolated compounds to determine time of anesthetic induction and recovery. Eugenol (50 mg L-1 was used as positive control. Essential oil of A. gratissima was effective as an anesthetic at concentrations of 300 to 900 mg L-1. Fish presented involuntary muscle contractions during induction and recovery. The bio-guided fractionation of essential oil furnishedE-(--pinocamphone, (--caryophyllene oxide, (--guaiol and (+-spathulenol. E-(--pinocamphone caused the same side effects observed for essential oil. (--Caryophyllene oxide, (--guaiol and (+-spathulenol showed only sedative effects at proportional concentrations to those of the constituents in essential oil. (+-Spathulenol (51.2 mg L-1 promoted deep anesthesia without side effects. A higher concentration of (+-spathulenol, and lower or absent amounts ofE-(--pinocamphone could contribute to increase the activity and safety of the essential oil of A. gratissima. (+-Spathulenol showed potent sedative and anesthetic activities in silver catfish, and could be considered as a viable compound for the development of a new anesthetic.

  5. Anesthetic activity and bio-guided fractionation of the essential oil of Aloysia gratissima (Gillies & Hook.) Tronc. in silver catfish Rhamdia quelen.

    Science.gov (United States)

    Benovit, Simone C; Silva, Lenise L; Salbego, Joseânia; Loro, Vania L; Mallmann, Carlos A; Baldisserotto, Bernardo; Flores, Erico M M; Heinzmann, Berta M

    2015-09-01

    This work aimed to determine the efficacy of the essential oil of A. gratissima as anesthetic for silver catfish, and to perform the bio-guided fractionation of essential oil aiming to isolate compounds responsible for the noted effects. Fish were submitted to anesthesia bath with essential oil, its fractions and isolated compounds to determine time of anesthetic induction and recovery. Eugenol (50 mg L(-1)) was used as positive control. Essential oil of A. gratissima was effective as an anesthetic at concentrations of 300 to 900 mg L(-1). Fish presented involuntary muscle contractions during induction and recovery. The bio-guided fractionation of essential oil furnished E-(-)-pinocamphone, (-)-caryophyllene oxide, (-)-guaiol and (+)-spathulenol. E-(-)-pinocamphone caused the same side effects observed for essential oil. (-)-Caryophyllene oxide, (-)-guaiol and (+)-spathulenol showed only sedative effects at proportional concentrations to those of the constituents in essential oil. (+)-Spathulenol (51.2 mg L(-1)) promoted deep anesthesia without side effects. A higher concentration of (+)-spathulenol, and lower or absent amounts ofE-(-)-pinocamphone could contribute to increase the activity and safety of the essential oil of A. gratissima. (+)-Spathulenol showed potent sedative and anesthetic activities in silver catfish, and could be considered as a viable compound for the development of a new anesthetic.

  6. [Action of a dental anesthetic on cell respiration].

    Science.gov (United States)

    di Jeso, F; Truscello, A; Martinotti, G; Colli, S

    1987-01-01

    It is often required to employ local anesthetics in practising dentistry, particularly when children have to be treated. Our researches on neurotropic drugs in the last years follow our hypothesis that the strong effects on nervous system have always hidden more widespread effects on all tissues and cells. In vitro essays carried out on rat liver mitochondria show that a dental anesthetic, lidocaine, depress respiration coupled to phosphorylation in mitochondria having a good respiratory control; so respiratory control too is depressed, but P/O ratio is unaffected; also respiration uncoupled by 2,4-dinitrophenol is depressed. Depressing respiration cooperates with anesthesia; unchanging P/O is good for the health of the cells and tissues treated by the lidocaine.

  7. The role of hyaluronidase on lidocaine and bupivacaine pharmacokinetics after peribulbar blockade.

    Science.gov (United States)

    Nathan, N; Benrhaiem, M; Lotfi, H; Debord, J; Rigaud, G; Lachatre, G; Adenis, J P; Feiss, P

    1996-05-01

    Orbital regional anesthesia is the only circumstance where hyaluronidase is routinely added to local anesthetics to accelerate the onset of the block. The aim of this study was to compare the pharmacokinetics of lidocaine and bupivacaine with or without hyaluronidase for peribulbar blockade. Twenty-one patients scheduled for cataract surgery with lens implantation were included in this prospective randomized study. Peribulbar blocks were achieved with plain bupivacaine 0.5% (5.5 mL), lidocaine 2% (5.5 mL), and hyaluronidase (100 IU = 2 mL) (n = 10) ir sterile water (2 mL) (n = 11). Plasma bupivacaine and lidocaine concentrations were measured by high-performance liquid chromatography at regular intervals from the end of the local anesthetic injection until the 360th minute. Maximum plasma concentration (Cmax) and time to reach Cmax (Tmax) were obtained for all the patients except one who needed a supplementary injection and was excluded from the study. The time to onset and duration of the analgesia and akinesia were monitored at the times of sampling. Motor blockade was incomplete in two patients in each group without affecting surgery. The Tmax and absorption half-life (t1/2a) of lidocaine and bupivacaine were not different within each group (P > 0.05). The Tmax of lidocaine was shorter in the presence of hyaluronidase (17.1 +/- 2.6 min vs 32.7 +/- 6.0 min) as well as the Tmax of bupivacaine (16.8 +/- 3.0 min vs 26.5 +/- 4.4 min). The Cmax of lidocaine and bupivacaine were not modified by the addition of hyaluronidase. The clearance, terminal half-life, and volume of distribution were not different between groups. The absorption of lidocaine and bupivacaine from the peribulbar space are hastened by the addition of hyaluronidase. The Tmax of lidocaine is not different from that of bupivacaine within each group suggesting that the absorption of local anesthetics is minimally influenced by the liposolubility of the drugs. Moreover, hyaluronidase influences the

  8. The neurotoxicity of intrathecal lidocaine is enhanced in postpartum compared to virgin rats.

    Science.gov (United States)

    Xu, Fei; Zhang, Bingxi; Li, Tianzuo

    2013-08-01

    During the perinatal period, the pharmacokinetics and pharmacodynamics of drugs may be altered. Data about the neurotoxicity of intrathecal local anesthetics in the peripartum period are lacking. So we hypothesized that the neurotoxicity of intrathecal lidocaine during perinatal period may be changed. Therefore, we designed the present study to determine whether the neurotoxicity of intrathecal lidocaine in postpartum rats would be different from that in nonpregnant, virgin rats. Postpartum and nonpregnant rats randomly received an intrathecal infusion of lidocaine 50 mg/mL in saline, lidocaine 20 mg/mL in saline, or saline for 1 h at a rate of 1 μL/min. Four days after drug infusion, the rats were assessed for persistent impairment of sensory and motor function (MF) using the tail-flick (TF) test, paw pressure test, and MF score. Spinal cords and nerve roots were obtained for light and electron microscopic examinations, and the injury scores were compared between groups. The TF latencies and the mean nerve injury scores of the postpartum group were significantly higher than those of nonpregnant group. Lidocaine induced a dose-dependent impairment in TF latencies and nerve injury scores. There was no significant interaction between postpartum and the drug. Our results suggest that the neurotoxicity of intrathecal lidocaine is enhanced in rats during the early postpartum period compared with nonpregnant, virgin rats.

  9. Comparative Study of Intrathecal Dexamethasone with Epinephrine as Adjuvants to Lidocaine in Cesarean Section

    Directory of Open Access Journals (Sweden)

    Fereshteh Naziri

    2013-09-01

    Full Text Available Background: Different additives have been used with local anesthetics to provide prolonged duration of sensory block in spinal anesthesia. The aim of present study was to evaluate the onset and duration of sensory block of intrathecal dexamethasone and epinephrine as adjuvants to lidocaine in patients who were candidate for cesarean section. Materials and Methods: This double-blind clinical trial research was conducted on 90 pregnant women candidate for cesarean section under spinal anesthesia. Patients were randomly allocated to receive intrathecally either 75 mg hyperbaric lidocaine plus 100 μg epinephrine or 75 mg hyperbaric lidocaine plus 4 mg dexamethasone or 75 mg hyperbaric lidocaine. The onset and duration of sensory block as well as postoperative analgesia were assessed. Results: The time to reach the peak sensory block in lidocaine group was shorter than that of other two groups (p<0.001. Duration of sensory block in the control group, dexamethasone group, and epinephrine group were 64.16±7.99 min, 74.79±12.78 min, and 99.30±10.93 min, respectively (p<0.001. Conclusion: The present research shows that intrathecal dexamethasone and intrathecal epinephrine as adjuvant to lidocaine increases sensory block duration in the women candidate for cesarean section.

  10. Immediate reaction to lidocaine with periorbital edema during upper blepharoplasty

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    Benjamin Presman

    2016-01-01

    Conclusion: In clinical practice, we recommend that patient should be informed about the possibility of recurrence of an adverse reaction in case of re-exposure to lidocaine, even in the vast majority of cases where true allergy could not be proven. In case of further need for local anesthesia with history of an adverse event, a different agent may be chosen even from the same class (another amide as cross-reactions in the amide group are rare. Otherwise, an anesthetic from the ester group can also be safely used.

  11. Trigeminal nerve injury associated with injection of local anesthetics

    DEFF Research Database (Denmark)

    Hillerup, Søren; Jensen, Rigmor H.; Ersbøll, Bjarne Kjær

    2011-01-01

    , prilocaine 3 percent, and articaine 4 percent sold in cartridges. Results. The study results showed a highly significant overrepresentation of NSDs associated with articaine 4 percent, in particular with mandibular blocks. Conclusions. The distribution of NSDs was disproportionate to the market share......Background. The authors used comprehensive national registry and clinical data to conduct a study of adverse drug reactions (ADRs), in particular neurosensory disturbance (NSD), associated with local anesthetics used in dentistry. Methods. The study included data sets of annual sales of local...... anesthetics (from 1995 through 2007), 292 reports to the Danish Medicines Agency, Copenhagen, Denmark, of adverse reactions to local anesthetic drugs, and a clinical sample of 115 patients with NSD associated with local anesthetics. The authors assessed lidocaine 2 percent, mepivacaine 2 percent and 3 percent...

  12. Organ-specific activation of the gastric branch of the efferent vagus nerve by ghrelin in urethane-anesthetized rats.

    Science.gov (United States)

    Habara, Hiromi; Hayashi, Yujiro; Inomata, Norio; Niijima, Akira; Kangawa, Kenji

    2014-01-01

    Ghrelin plays multiple physiological roles such as growth hormone secretion and exerting orexigenic actions; however, its physiological roles in the electrical activity of autonomic nerves remain unclear. Here, we investigated the effects of human ghrelin on several autonomic nerve activities in urethane-anesthetized rats using an electrophysiological method. Intravenous injection of ghrelin at 3 μg/kg significantly and transiently potentiated the efferent activity of the gastric vagus nerve; however, it did not affect the efferent activity of the hepatic vagus nerve. The activated response to ghrelin in the gastric efferent vagus nerve was not affected by the gastric afferent vagotomy, suggesting that this effect was not induced via the gastric afferent vagus nerve. Ghrelin did not affect the efferent activity of the brown adipose tissue, adrenal gland sympathetic nerve, and the renal sympathetic nerve. In addition, rectal temperature and the plasma concentrations of norepinephrine, corticosterone, and renin were also not changed by ghrelin. These findings demonstrate that ghrelin stimulates the gastric efferent vagus nerve in an organ-specific manner without affecting the gastric afferent vagus nerve and that ghrelin does not acutely affect the efferent basal activity of the sympathetic nerve in rats.

  13. Effect of anesthetics on bending elasticity of lipid membranes

    Science.gov (United States)

    Yi, Zheng; Michihiro, Nagao; Bossev, Dobrin

    2008-03-01

    Change in physical and chemical properties of bio-membranes is of great interest for understanding the mechanism of anesthetic action on membranes. Hypothetically the anesthetic alters the lipid membrane structure (promoting pore formation across membranes or at least switching transmembrane channels) and therefore the biophysical properties of the membrane. We have used neutron spin echo (NSE) spectroscopy to study the effect of anesthetic molecule, lidocaine, on the bending elasticity (BE) of lipid membranes. BE of lipid bilayers made of (1,2-Dimyristoyl-sn-Glycero-3-Phosphocholine) DMPC and 1,2-Dipalmitoyl-sn-Glycero-3-Phosphocholine (DPPC) have been measured at different temperatures and different in the fluid (Lα) phase. Using Zilman-Granek theory the BE were obtained from the decay of the NSE intermediate scattering function. We have found that in the presence of lidocaine the BE of DMPC and DPPC bilayers increases. The results were correlated with those from differential scanning calorimetry. Increase in the lidocaine concentration leads to decrease in the liquid/crystalline transition temperature.

  14. Anesthetic Efficacy in Irreversible Pulpitis: A Randomized Clinical Trial.

    Science.gov (United States)

    Allegretti, Carlos E; Sampaio, Roberta M; Horliana, Anna C R T; Armonia, Paschoal L; Rocha, Rodney G; Tortamano, Isabel Peixoto

    2016-01-01

    Inferior alveolar nerve block has a high failure rate in the treatment of mandibular posterior teeth with irreversible pulpitis. The aim of this study was to compare the anesthetic efficacy of 4% articaine, 2% lidocaine and 2% mepivacaine, all in combination with 1:100,000 epinephrine, in patients with irreversible pulpitis of permanent mandibular molars during a pulpectomy procedure. Sixty-six volunteers from the Emergency Center of the School of Dentistry, University of São Paulo, randomly received 3.6 mL of local anesthetic as a conventional inferior alveolar nerve block (IANB). The subjective signal of lip numbness, pulpal anesthesia and absence of pain during the pulpectomy procedure were evaluated respectively, by questioning the patient, stimulation using an electric pulp tester and a verbal analogue scale. All patients reported the subjective signal of lip numbness. Regarding pulpal anesthesia success as measured with the pulp tester, the success rate was respectively 68.2% for mepivacaine, 63.6% for articaine and 63.6% for lidocaine. Regarding patients who reported no pain or mild pain during the pulpectomy, the success rate was, respectively 72.7% for mepivacaine, 63.6% for articaine and 54.5% for lidocaine. These differences were not statistically significant. Neither of the solutions resulted in 100% anesthetic success in patients with irreversible pulpitis of mandibular molars.

  15. Intravenous lidocaine for postmastectomy pain treatment: randomized, blind, placebo controlled clinical trial

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    Tania Cursino de Menezes Couceiro

    2015-06-01

    Full Text Available BACKGROUND AND OBJECTIVE: Postoperative pain treatment in mastectomy remains a major challenge despite the multimodal approach. The aim of this study was to investigate the analgesic effect of intravenous lidocaine in patients undergoing mastectomy, as well as the postoperative consumption of opioids. METHODS: After approval by the Human Research Ethics Committee of the Instituto de Medicina Integral Prof. Fernando Figueira in Recife, Pernambuco, a randomized, blind, controlled trial was conducted with intravenous lidocaine at a dose of 3 mg/kg infused over 1 h in 45 women undergoing mastectomy under general anesthesia. One patient from placebo group was. RESULTS: Groups were similar in age, body mass index, type of surgery, and postoperative need for opioids. Two of 22 patients in lidocaine group and three of 22 patients in placebo group requested opioid (p = 0.50. Pain on awakening was identified in 4/22 of lidocaine group and 5/22 of placebo group (p = 0.50; in the post-anesthetic recovery room in 14/22 and 12/22 (p = 0.37 of lidocaine and placebo groups, respectively. Pain evaluation 24 h after surgery showed that 2/22 and 3/22 patients (p = 0.50 of lidocaine and placebo groups, respectively, complained of pain. CONCLUSION: Intravenous lidocaine at a dose of 3 mg/kg administered over a period of an hour during mastectomy did not promote additional analgesia compared to placebo in the first 24 h, and has not decreased opioid consumption. However, a beneficial effect of intravenous lidocaine in selected and/or other therapeutic regimens patients cannot be ruled out.

  16. Cardiovascular And Etectrocardiographic Effects Of Lidocaine And Mepivacaine With And Without Adrenaline Using Mandibular Nerve Block Anesthesia Technique In Healthy Volunteers

    OpenAIRE

    Rodríguez Alfaro, Miguel; Docentes del Departamento Académico de Ciencias Básicas FO UNMSM.; Chumpitaz Cerrate, Manuel; Docentes del Departamento Académico de Ciencias Básicas FO UNMSM.; Burga Sánchez, Jonny; Ex Docentes del Departamento Académico de Ciencias Básicas FO UNMSM.; Ramón Rosales, Arturo; Ex Docentes del Departamento Académico de Ciencias Básicas FO UNMSM.; Aguirre Siancas, Ernesto; Ex Docentes del Departamento Académico de Ciencias Básicas FO UNMSM.; Zegarra Cuya, Manuel; Ex Docentes del Departamento Académico de Ciencias Básicas FO UNMSM.; Cabrejos Álvarez, José; Ex Docente del Departamento Académico de Estomatologia Médico-Quirúrgica FO UNMSM

    2014-01-01

    The objective of the present study was to evaluate and compare the effect of Iidocaine and mepivacaine alone and associated with epinephrine on the cardiovascular and electrocardiographic parameters,60 healthy volunteers were assigned in 4 groups: A (2% lidocaine), B (2% lidocaine with epinephrine 1: 100,000); C (3% mepivacaine), D (mepivacaine 2% with epinephrine 1: 100,000). Therefore of assigned, it was injected ldental cartridge of correspondent anesthetic to each volunteer, using the ner...

  17. Interaction of local anesthetics with a peptide encompassing the IV/S4-S5 linker of the Na+ channel.

    Science.gov (United States)

    Fraceto, Leonardo F; Oyama, Sérgio; Nakaie, Clóvis R; Spisni, Alberto; de Paula, Eneida; Pertinhez, Thelma A

    2006-08-20

    The peptide pIV/S4-S5 encompasses the cytoplasmic linker between helices S4-S5 in domain IV of the voltage-gated Na+ channel, residues 1644-1664. The interaction of two local anesthetics (LA), lidocaine and benzocaine, with pIV/S4-S5 has been studied by DOSY, heteronuclear NMR 1H-15N-HSQC spectroscopy and computational methods. DOSY indicates that benzocaine, a neutral ester, exhibits stronger interaction with pIV/S4-S5 than lidocaine, a charged amine-amide. Weighted average chemical shifts, Deltadelta(1H-15N), show that benzocaine affects residues L1653, M1655 and S1656 while lidocaine slightly perturbs residues I1646, L1649 and A1659, L1660, near the N- and C-terminus, respectively. Computational methods confirmed the stability of the benzocaine binding and the existence of two binding sites for lidocaine. Even considering that the approach of studying the peptide in the presence of a co-solvent (TFE/H2O, 30%/70% v/v) has an inherently limited implication, our data strongly support the existence of multiple LA binding sites in the IV/S4-S5 linker, as suggested in the literature. In addition, we consider that LA can bind to the S4-S5 linker with diverse binding modes and strength since this linker is part of the receptor for the "inactivation gate particle". Conditions for devising new functional studies, aiming to better understand Na+ channel functionality as well as the various facets of LA pharmacological activity are proposed in this work.

  18. Comparative effect of lidocaine and bupivacaine on glucose uptake and lactate production in the perfused working rat heart

    Energy Technology Data Exchange (ETDEWEB)

    Cronau, L.H. Jr.; Merin, R.G.; Aboulish, E.; Steenberg, M.L.; Maljorda, A.

    1986-03-01

    It has been suggested that at equivalent therapeutic concentrations, lidocaine and bupivacaine may have different cardiotoxic potency. In the isolated working rat heart preparation, the effect of a range of lidocaine and bupivacaine concentrations on glucose uptake and lactate production (LP) were observed. Insulin was added, 10 ..mu../L, to Ringer's solution containing /sup 3/H-labeled glucose to measure the glycolytic flux (GF). The effect of the local anesthetics on LP at the indicated concentrations were similar. Lidocaine appears to depress the glycolytic flux from exogenous glucose to a lesser degree. Bupivacaine, 10 mg/L, depresses VO/sub 2/ to a greater degree than does lidocaine, 40 mg/L.

  19. Recurrent seizures after lidocaine ingestion.

    Science.gov (United States)

    Aminiahidashti, Hamed; Laali, Abolghasem; Nosrati, Nazanin; Jahani, Fatemeh

    2015-01-01

    Lidocaine has a concentration-dependent effect on seizures. Concentrations above 15 μg/mL frequently result in seizures in laboratory animals and human. We report a case of central nervous system (CNS) lidocaine toxicity and recurrent seizure after erroneous ingestion of lidocaine solution. A 4-year-old boy presented to the Emergency Department of Imam Hospital of Sari in December 2013 due to tonic-clonic generalized seizures approximately 30 min ago. 3 h before seizure, his mother gave him 2 spoons (amount 20-25 cc) lidocaine hydrochloride 2% solution instead of pediatric gripe by mistake. Seizure with generalized tonic-clonic occurred 3 times in home. Neurological examination was essentially unremarkable except for the depressed level of consciousness. Personal and medical history was unremarkable. There was no evidence of intracranial ischemic or hemorrhagic lesions in computed tomography scan. There were no further seizures, the condition of the patient remained stable, and he was discharged 2 days after admission. The use of viscous lidocaine may result in cardiovascular and CNS toxicity, particularly in children. Conservative management is the best option for treatment of lidocaine induced seizure.

  20. Recurrent seizures after lidocaine ingestion

    Directory of Open Access Journals (Sweden)

    Hamed Aminiahidashti

    2015-01-01

    Full Text Available Lidocaine has a concentration-dependent effect on seizures. Concentrations above 15 μg/mL frequently result in seizures in laboratory animals and human. We report a case of central nervous system (CNS lidocaine toxicity and recurrent seizure after erroneous ingestion of lidocaine solution. A 4-year-old boy presented to the Emergency Department of Imam Hospital of Sari in December 2013 due to tonic-clonic generalized seizures approximately 30 min ago. 3 h before seizure, his mother gave him 2 spoons (amount 20-25 cc lidocaine hydrochloride 2% solution instead of pediatric gripe by mistake. Seizure with generalized tonic-clonic occurred 3 times in home. Neurological examination was essentially unremarkable except for the depressed level of consciousness. Personal and medical history was unremarkable. There was no evidence of intracranial ischemic or hemorrhagic lesions in computed tomography scan. There were no further seizures, the condition of the patient remained stable, and he was discharged 2 days after admission. The use of viscous lidocaine may result in cardiovascular and CNS toxicity, particularly in children. Conservative management is the best option for treatment of lidocaine induced seizure.

  1. Comparison of topical tetracaine, adrenaline, and cocaine anesthesia with lidocaine infiltration for repair of lacerations in children.

    Science.gov (United States)

    Hegenbarth, M A; Altieri, M F; Hawk, W H; Greene, A; Ochsenschlager, D W; O'Donnell, R

    1990-01-01

    Local anesthetic infiltration is painful and frightening for children. We prospectively compared a topical alternative, TAC solution (tetracaine 0.5%, adrenaline 1:2,000, cocaine 11.8%), with 1% lidocaine infiltration for use in laceration repair in 467 children. Adequate anesthesia of facial and scalp wounds was achieved for 81% of TAC-treated wounds versus 87% of lidocaine-treated wounds (P = .005). TAC was less effective on extremity wounds; 43% had effective anesthesia compared with 89% of lidocaine-treated extremity wounds (P less than .0001). No systemic toxicity was observed. The incidence of wound infection was 2.2% for both TAC and lidocaine. Wound dehiscence occurred in seven TAC- and two lidocaine-treated facial or scalp wounds (4.5% vs 1.8%, NS) and in five TAC- and four lidocaine-treated extremity wounds (20% vs 17.4%, NS). The unusually high rate of dehiscence was due partially to recurrent trauma or coincident infection. TAC was well accepted by patients and parents. We encourage the careful use of TAC as a less painful alternative to lidocaine infiltration for selected scalp and facial lacerations in children.

  2. A comparison of mepivacaine versus lidocaine for episcleral (sub-tenon's) block for cataract surgery in an ambulatory setting.

    Science.gov (United States)

    Ripart, Jacques; Nouvellon, Emmanuel; Chaumeron, Arnaud; Chanial-Bourgaux, Catherine; Mahamat, Aba

    2006-01-01

    For eye surgery, motor block is still often requested by the surgeon. For cataract surgery, rapid block resolution allows eyelids to move and allows eye-patch removal. Therefore, short-duration block is useful in early rehabilitation for ambulatory surgery. Lidocaine is classically assumed to have shorter duration than mepivacaine. Therefore, lidocaine alone might be considered as an alternative to mepivacaine. In this randomized, double-blind study, we compared mepivacaine 2% (n = 22) and lidocaine 2% (n = 25) in 47 patients who received episcleral (sub-Tenon's) block for cataract surgery. Akinesia score was measured 1, 5, 10, and 15 minutes and 1, 2, 4, and 6 hours after the end of injection. Primary outcome was block duration (time from injection to full recovery). Secondary outcomes were time to block onset and best akinesia score for each patient. Complications were recorded. The 2 groups were similar for demographic and anesthetic features. We observed no significant difference between mepivacaine and lidocaine in terms of onset, quality of akinesia, and block duration. One case of ocular hypertonia and 1 case of strabismus were observed in the lidocaine group, which could be imputed to hyaluronidase unavailability during the study period or to increased lidocaine myotoxicity. We found no argument to favor lidocaine over mepivacaine in episcleral (sub-Tenon's) eye block, especially in terms of motor-block duration.

  3. Use of adrenalin with lidocaine in hand surgery ,

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    Ronaldo Antonio de Freitas Novais Junior

    2014-10-01

    Full Text Available Objective:Because of the received wisdom within our setting that claims that local anesthesia should not be used with adrenalin in hand surgery; we conducted a study using lidocaine with adrenalin, to demonstrate its safety, utility and efficacy.Methods:We conducted a prospective study in which, in wrist, hand and finger surgery performed from July 2012 onwards, we used local anesthesia comprising a 1% lidocaine solution with adrenalin at 1:100,000. We evaluated the quantity of bleeding, systemic alterations, signs of arterial deficit and complications, among other parameters. We described the infiltration techniques for specific procedures individually.Results:We operated on 41 patients and chose to describe separately the raising of a lateral microsurgical flap on the arm, which was done without excessive bleeding and within the usual length of time. In only three cases was there excessive bleeding or use of bipolar tweezers. No systemic alterations were observed by the anesthesiologists or any complications relating to ischemia and necrosis in the wounds or in the fingers, and use of tourniquets was not necessary in any case.Conclusions:Use of lidocaine with adrenalin in hand surgery was shown to be a safe local anesthetic technique, without complications relating to necrosis. It provided efficient exsanguination of the surgical field and made it possible to perform the surgical procedures without using a pneumatic tourniquet, thereby avoiding its risks and benefiting the patient through lower sedation.

  4. β–Cyclodextrin–Propyl Sulfonic Acid Catalysed One-Pot Synthesis of 1,2,4,5-Tetrasubstituted Imidazoles as Local Anesthetic Agents

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    Yan Ran

    2015-11-01

    Full Text Available Some functionalized 1,2,4,5-tetrasubstituted imidazole derivatives were synthesized using a one-pot, four component reaction involving 1,2-diketones, aryl aldehydes, ammonium acetate and substituted aromatic amines. The synthesis has been efficiently carried out in a solvent free medium using β-cyclodextrin-propyl sulfonic acid as a catalyst to afford the target compounds in excellent yields. The local anesthetic effect of these derivatives was assessed in comparison to lidocaine as a standard using a rabbit corneal and mouse tail anesthesia model. The three most potent promising compounds were subjected to a rat sciatic nerve block assay where they showed considerable local anesthetic activity, along with minimal toxicity. Among the tested analogues, 4-(1-benzyl-4,5-diphenyl-1H-imidazol-2-yl-N,N-dimethylaniline (5g was identified as most potent analogue with minimal toxicity. It was further characterized by a more favourable therapeutic index than the standard.

  5. Use of topical lidocaine in the treatment of muscle tension dysphonia.

    Science.gov (United States)

    Dworkin, J P; Meleca, R J; Simpson, M L; Garfield, I

    2000-12-01

    This investigation explored the potential usefulness of topical lidocaine in the treatment of muscle tension dysphonia. Three patients with this disorder, who were previously unresponsive to standard voice therapy, were treated with lidocaine. In each case, the outcome was prompt, clinically significant, and sustained. Persistently high-pitched and shrill vocal quality was converted to near normal voice patterns within 15 minutes after transcricothyroid membrane lidocaine injection. We suggest that this temporary and simple laryngeal and tracheal anesthetic technique may have helped to break the perverse cycle of hyperactive glottal and supraglottal muscle contractions evident in each of these patients during phonation efforts. We discuss the possible sensorimotor mechanism of action of this therapeutic technique.

  6. Efficacy of 2% Lidocaine Injection as a Topical Agent in Cataract Surgery

    Institute of Scientific and Technical Information of China (English)

    Wenyong Huang; Bin Liu; Jiewei Liu; Jinxing Xu; Zhende Lin

    2003-01-01

    Purpose: To determine whether 2% Lidocaine injection is an effective topical anesthetic agent for non-phaco small incision cataract surgery.Setting: Charity eye clinic supported by Hellen Keller International.Methods:One hundred and twenty-five consecutive cataract surgery patients received topical anesthesia with 2% Lidocaine injection solution just 1 and 0.5 minutes prior to non-phaco small incision cataract extraction and intraocular lens implantation. Each patient was asked about pain or piessure sensation during the operation.Results: The surgeon felt ease in the operations. Many patients (93/125) were comfort during the whole surgery. Only 9 patients′ score was above level 3,mostly complained during the nucleus extraction; Among those whose score was level 1~2, 82.6%(19/23)claimed discomfort at middle of the operation (nucleus extraction) or the beginning (creating the conjunctival flap).Conclusion: Lidocaine injection solution(2%) was an effective topical anesthesia agent in cataract surgery.

  7. Thermodynamic studies of mixtures for topical anesthesia: Lidocaine-salol binary phase diagram

    Energy Technology Data Exchange (ETDEWEB)

    Lazerges, Mathieu [Laboratoire de Chimie Physique (EA 4066), Faculte des Sciences Pharmaceutiques et Biologiques, Universite Paris Descartes, 4 Avenue de l' Observatoire, 75270 Paris Cedex 06 (France); Rietveld, Ivo B., E-mail: ivo.rietveld@parisdescartes.fr [Laboratoire de Chimie Physique (EA 4066), Faculte des Sciences Pharmaceutiques et Biologiques, Universite Paris Descartes, 4 Avenue de l' Observatoire, 75270 Paris Cedex 06 (France); Corvis, Yohann; Ceolin, Rene; Espeau, Philippe [Laboratoire de Chimie Physique (EA 4066), Faculte des Sciences Pharmaceutiques et Biologiques, Universite Paris Descartes, 4 Avenue de l' Observatoire, 75270 Paris Cedex 06 (France)

    2010-01-10

    The lidocaine-salol binary system has been investigated by differential scanning calorimetry, direct visual observations, and X-ray powder diffraction, resulting in a temperature-composition phase diagram with a eutectic equilibrium. The eutectic mixture, found at 0.423 {+-} 0.007 lidocaine mole-fraction, melts at 18.2 {+-} 0.5 {sup o}C with an enthalpy of 17.3 {+-} 0.5 kJ mol{sup -1}. This indicates that the liquid phase around the eutectic composition is stable at room temperature. Moreover, the undercooled liquid mixture does not easily crystallize. The present binary mixture exhibits eutectic behavior similar to the prilocaine-lidocaine mixture in the widely used EMLA topical anesthetic preparation.

  8. Atomic determinants of state-dependent block of sodium channels by charged local anesthetics and benzocaine.

    Science.gov (United States)

    Tikhonov, Denis B; Bruhova, Iva; Zhorov, Boris S

    2006-11-13

    Molecular modeling predicts that a local anesthetic (LA) lidocaine binds to the resting and open Na(v)1.5 in different modes, interacting with LA-sensing residues known from experiments. Besides the major pathway via the open activation gate, LAs can reach the inner pore via a "sidewalk" between D3S6, D4S6, and D3P. The ammonium group of a cationic LA binds in the focus of the pore-helices macrodipoles, which also stabilize a Na(+) ion chelated by two benzocaine molecules. The LA's cationic group and a Na(+) ion in the selectivity filter repel each other suggesting that the Na(+) depletion upon slow inactivation would stabilize a LA, while a LA would stabilize slow-inactivated states.

  9. The Effect of Lidocaine · HCl on the Fluidity of Native and Model Membrane Lipid Bilayers.

    Science.gov (United States)

    Park, Jun-Seop; Jung, Tae-Sang; Noh, Yang-Ho; Kim, Woo-Sung; Park, Won-Ick; Kim, Young-Soo; Chung, In-Kyo; Sohn, Uy Dong; Bae, Soo-Kyung; Bae, Moon-Kyoung; Jang, Hye-Ock; Yun, Il

    2012-12-01

    The purpose of this study is to investigated the mechanism of pharmacological action of local anesthetic and provide the basic information about the development of new effective local anesthetics. Fluorescent probe techniques were used to evaluate the effect of lidocaine·HCl on the physical properties (transbilayer asymmetric lateral and rotational mobility, annular lipid fluidity and protein distribution) of synaptosomal plasma membrane vesicles (SPMV) isolated from bovine cerebral cortex, and liposomes of total lipids (SPMVTL) and phospholipids (SPMVPL) extracted from the SPMV. An experimental procedure was used based on selective quenching of 1,3-di(1-pyrenyl)propane (Py-3-Py) and 1,6-diphenyl-1,3,5-hexatriene (DPH) by trinitrophenyl groups, and radiationless energy transfer from the tryptophans of membrane proteins to Py-3-Py. Lidocaine·HCl increased the bulk lateral and rotational mobility of neuronal and model membrane lipid bilayes, and had a greater fluidizing effect on the inner monolayer than the outer monolayer. Lidocaine·HCl increased annular lipid fluidity in SPMV lipid bilayers. It also caused membrane proteins to cluster. The most important finding of this study is that there is far greater increase in annular lipid fluidity than that in lateral and rotational mobilities by lidocaine·HCl. Lidocaine·HCl alters the stereo or dynamics of the proteins in the lipid bilayers by combining with lipids, especially with the annular lipids. In conclusion, the present data suggest that lidocaine, in addition to its direct interaction with proteins, concurrently interacts with membrane lipids, fluidizing the membrane, and thus inducing conformational changes of proteins known to be intimately associated with membrane lipid.

  10. Dopamine D2-like receptor activation antagonizes long-term depression of orofacial sensorimotor processing in anesthetized mice.

    Science.gov (United States)

    Ellrich, Jens

    2005-02-21

    Long-term depression (LTD) of orofacial sensorimotor processing recently has been demonstrated in anesthetized mice. Due to the remarkable role of dopamine in central nervous system LTD, the influence of dopamine D2 receptor activation on LTD of the jaw-opening reflex (JOR) was investigated. Electric low-frequency stimulation (LFS, 1 Hz) of the tongue suppressed the JOR integral by 43% for at least 1 h. After systemic administration of the dopamine D2-like receptor agonist quinpirole, LTD was significantly attenuated to 14%. JOR decreased for only about 15 min after LFS according to a short-term depression. Under systemic application of the dopamine D2-like receptor antagonist sulpiride, LTD significantly increased to 64%, again for at least 1 h. Thus, D2-like receptor activation prevented LTD, and D2-like receptor blockade amplified LTD of the reflex. The time course of inhibition may be due to a dopaminergic D2-like receptor mechanism that antagonizes the transfer from short-term into long-term depression. Considering a putative mediation of LTD by the endogenous pain control system, the results correspond to the known inhibitory control of this system by a D2-like receptor mechanism.

  11. Decreasing Effect of Lidocaine·HCl on the Thickness of the Neuronal and Model Membrane.

    Science.gov (United States)

    Park, Sung-Min; Park, Jong-Sun; Kim, Jae-Han; Baek, Jin-Hyun; Yoon, Tae-Gyun; Lee, Do-Keun; Ryu, Won-Hyang; Chung, In-Kyo; Sohn, Uy Dong; Jang, Hye-Ock; Yun, Il

    2013-08-01

    This study examined the mechanism of action of a local anesthetic, lidocaine·HCl. Energy transfer between the surface fluorescent probe, 1-anilinonaphthalene-8-sulfonic acid, and the hydrophobic fluorescent probe, 1,3-di(1-pyrenyl) propane, was used to determine the effect of lidocaine·HCl on the thickness (D) of the synaptosomal plasma membrane vesicles (SPMV) isolated from the bovine cerebral cortex, and liposomes of the total lipids (SPMVTL) and phospholipids (SPMVPL) extracted from the SPMV. The thickness (D) of the intact SPMV, SPMVTL and SPMVPL were 1.044±0.008, 0.914±0.005 and 0.890±0.003 (arbitrary units, n=5) at 37℃ (pH 7.4), respectively. Lidocaine·HCl decreased the thickness of the neuronal and model membrane lipid bilayers in a dose-dependent manner with a significant decrease in the thickness, even at 0.1 mM. The decreasing effect of lidocaine·HCl on the membrane thickness might be responsible for some, but not all of its anesthetic action.

  12. Reduced anesthetic requirements in aged rats: association with altered brain synaptic plasma membrane Ca(2+)-ATPase pump and phospholipid methyltransferase I activities.

    Science.gov (United States)

    Horn, J L; Janicki, P K; Singh, G; Wamil, A W; Franks, J J

    1996-01-01

    Aging is associated with a decrease in anesthetic requirements. Animal models of aging manifest alteration of brain Ca2+ homeostasis and increased methyltransferase I (PLMTI) activity. In this study we evaluated concurrently anesthetic requirements and brain plasma membrane Ca(2+)-ATPase (PMCA) and PLMTI activities in young and aged rats. Halothane, desflurane, isoflurane and xenon MEDs (lowest partial pressures that suppress a pain response) were measured in 2 and 25 month old, male Fisher-344 rats. Halothane MED was also measured in 2 and 30 month old F344/BNF1 rats, a strain that undergoes aging with less debilitation. PMCA pumping and PLMTI activities were measured in synaptic plasma membranes (SPM) prepared from the cortex and diencephalon-mesencephalon (DM). For aged Fisher-344 rats, MEDs for halothane, desflurane, isoflurane and xenon were reduced to 81%, 82%, 67% and 86%, respectively, of young controls; PMCA activity was diminished to 91% in cortical SPM and 82% in DM SPM; and cortical and DM PLMTI activities were increased to 131% and 114% of young control. For F344/BNF1 rats, MED for halothane was reduced to 87%, PMCA activity was diminished to 90% in cortical SPM and 72% DM SPM, and PLMTI activity was increased to 133% in cortical SPM and 112% in DM SPM. The strong association between age and reduced anesthetic requirements for inhalational agents on the one hand and altered PMCA and PLMTI activity on the other lends support to the underlying hypothesis that PMCA and PLMTI may be involved in the production of the anesthetic state.

  13. Accelerated activation of SOCE current in myotubes from two mouse models of anesthetic- and heat-induced sudden death.

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    Viktor Yarotskyy

    Full Text Available Store-operated calcium entry (SOCE channels play an important role in Ca(2+ signaling. Recently, excessive SOCE was proposed to play a central role in the pathogenesis of malignant hyperthermia (MH, a pharmacogenic disorder of skeletal muscle. We tested this hypothesis by characterizing SOCE current (ISkCRAC magnitude, voltage dependence, and rate of activation in myotubes derived from two mouse models of anesthetic- and heat-induced sudden death: 1 type 1 ryanodine receptor (RyR1 knock-in mice (Y524S/+ and 2 calsequestrin 1 and 2 double knock-out (dCasq-null mice. ISkCRAC voltage dependence and magnitude at -80 mV were not significantly different in myotubes derived from wild type (WT, Y524S/+ and dCasq-null mice. However, the rate of ISkCRAC activation upon repetitive depolarization was significantly faster at room temperature in myotubes from Y524S/+ and dCasq-null mice. In addition, the maximum rate of ISkCRAC activation in dCasq-null myotubes was also faster than WT at more physiological temperatures (35-37°C. Azumolene (50 µM, a more water-soluble analog of dantrolene that is used to reverse MH crises, failed to alter ISkCRAC density or rate of activation. Together, these results indicate that while an increased rate of ISkCRAC activation is a common characteristic of myotubes derived from Y524S/+ and dCasq-null mice and that the protective effects of azumolene are not due to a direct inhibition of SOCE channels.

  14. Xyloglucan Based In Situ Gel of Lidocaine HCl for the Treatment of Periodontosis

    OpenAIRE

    Pandit, Ashlesha P.; Vaibhav V. Pol; Kulkarni, Vinit S.

    2016-01-01

    The present study was aimed at formulating thermoreversible in situ gel of local anesthetic by using xyloglucan based mucoadhesive tamarind seed polysaccharide (TSP) into periodontal pocket. Temperature-sensitive in situ gel of lidocaine hydrochloride (LH) (2% w/v) was formulated by cold method. A full 32 factorial design was employed to study the effect of independent variables concentrations of Lutrol F127 and TSP to optimize in situ gel. The dependent variables evaluated were gelation temp...

  15. Lidocaine stabilizes the open state of CNS voltage-dependent sodium channels.

    Science.gov (United States)

    Castañeda-Castellanos, David R; Nikonorov, Igor; Kallen, Roland G; Recio-Pinto, E

    2002-03-28

    We have previously reported that the lidocaine action is different between CNS and muscle batrachotoxin-modified Na+ channels [Salazar et al., J. Gen. Physiol. 107 (1996) 743-754; Brain Res. 699 (1995) 305-314]. In this study we examined lidocaine action on CNS Na+ currents, to investigate the mechanism of lidocaine action on this channel isoform and to compare it with that proposed for muscle Na+ currents. Na+ currents were measured with the whole cell voltage clamp configuration in stably transfected cells expressing the brain alpha-subunit (type IIA) by itself (alpha-brain) or together with the brain beta(1)-subunit (alphabeta(1)-brain), or the cardiac alpha-subunit (hH1) (alpha-cardiac). Lidocaine (100 microM) produced comparable levels of Na+ current block at positive potentials and of hyperpolarizing shift of the steady-state inactivation curve in alpha-brain and alphabeta(1)-brain Na+ currents. Lidocaine accelerated the rates of activation and inactivation, produced an hyperpolarizing shift in the steady-state activation curve and increased the current magnitude at negative potentials in alpha-brain but not in alphabeta(1)-brain Na+ currents. The lidocaine action in alphabeta(1)-brain resembled that observed in alpha-cardiac Na+ currents. The lidocaine-induced increase in current magnitude at negative potentials and the hyperpolarizing shift in the steady-state activation curve of alpha-brain, are novel effects and suggest that lidocaine treatment does not always lead to current reduction/block when it interacts with Na+ channels. The data are explained by using a modified version of the model proposed by Vedantham and Cannon [J. Gen. Physiol., 113 (1999) 7-16] in which we postulate that the difference in lidocaine action between alpha-brain and alphabeta(1)-brain Na+ currents could be explained by differences in the lidocaine action on the open channel state.

  16. Perfusion of isolated carotid sinus with hydrogen sulfide attenuated the renal sympathetic nerve activity in anesthetized male rats.

    Science.gov (United States)

    Guo, Q; Wu, Y; Xue, H; Xiao, L; Jin, S; Wang, R

    2016-07-18

    The purpose of the present study was to define the indirect central effect of hydrogen sulfide (H(2)S) on baroreflex control of sympathetic outflow. Perfusing the isolated carotid sinus with sodium hydrosulfide (NaHS), a H(2)S donor, the effect of H(2)S was measured by recording changes of renal sympathetic nerve activity (RSNA) in anesthetized male rats. Perfusion of isolated carotid sinus with NaHS (25, 50, 100 micromol/l) dose and time-dependently inhibited sympathetic outflow. Preconditioning of glibenclamide (20 micromol/l), a ATP-sensitive K(+) channels (K(ATP)) blocker, the above effect of NaHS was removed. With 1, 4-dihydro-2, 6-dimethyl-5-nitro-4-(2-[trifluoromethyl] phenyl) pyridine-3-carboxylic acid methyl ester (Bay K8644, 500 nmol/l) pretreatment, which is an agonist of L-calcium channels, the effect of NaHS was eliminated. Perfusion of cystathionine gamma-lyase (CSE) inhibitor, DL-propargylglycine (PPG, 200 micromol/l), increased sympathetic outflow. The results show that exogenous H(2)S in the carotid sinus inhibits sympathetic outflow. The effect of H(2)S is attributed to opening K(ATP) channels and closing the L-calcium channels.

  17. The analgesic efficacy of intravenous lidocaine infusion after laparoscopic fundoplication: a prospective, randomized, double-blind, placebo-controlled trial

    Directory of Open Access Journals (Sweden)

    Dale GJ

    2016-12-01

    Full Text Available Gregory J Dale,1 Stephanie Phillips,2 Gregory L Falk3 1Westmead Hospital Clinical School, The University of Sydney, 2Sydney Adventist Hospital Clinical School, The University of Sydney, 3Concord Clinical School, The University of Sydney, Sydney, Australia Abstract: This study aimed to determine if intravenous lidocaine infusion reduces postoperative pain intensity following laparoscopic fundoplication surgery and to also validate the safety of intravenous lidocaine at the dose tested. This was an equally randomized, double-blind, placebo-controlled, parallel-group, single center trial. Adult patients undergoing laparoscopic fundoplication were recruited. The intervention group received 1 mg/kg intravenous lidocaine bolus prior to induction of anesthesia, then an intravenous infusion at 2 mg/kg/h for 24 hours. The primary outcome was pain, measured using a numeric rating scale for 30 hours postoperatively. Secondary outcomes were nausea and vomiting, opioid requirements, adverse events, serum lidocaine concentration, and length of hospital stay. The study was terminated after an interim analysis of 24 patients showed evidence of futility. There was no difference in postoperative pain scores (lidocaine versus control, mean ± standard deviation at rest (2.0 ± 2.7 vs 2.1 ± 2.4, P=0.286 or with movement (2.0 ± 2.6 vs 2.6 ± 2.7, P=0.487. Three adverse events occurred in the lidocaine group (25% of patients. Intravenous lidocaine did not provide clinically significant analgesia to patients undergoing laparoscopic fundoplication. The serum lidocaine concentration of patients who experienced adverse events were within the therapeutic range. This trial cannot confirm the safety of intravenous lidocaine at the dose tested. Keywords: analgesia, local anesthetics, intravenous infusions, pharmacokinetics

  18. Duration of action of mepivacaine and lidocaine in equine palmar digital perineural blocks in an experimental lameness model.

    Science.gov (United States)

    Hoerdemann, Mona; Smith, Rachael L; Hosgood, Giselle

    2017-10-01

    To establish and compare the onset and duration of action of 2 local anesthetics based on objective lameness and skin sensitivity assessment. Interventional crossover experimental trial with balanced randomization. Eight horses. Reversible forelimb lameness was induced in 8 horses. A palmar digital nerve block (PDNB) was applied with mepivacaine or lidocaine (both 2%). Quantitative lameness and skin sensitivity data were collected with an inertial sensor system and a force gauge, respectively. The times to lameness resolution/skin desensitization (T1), consistent lameness detection/partial return of skin sensitivity (T2), and complete return of lameness/skin sensitivity (T3) were determined and compared between treatments and assessment methods. Mepivacaine blocks resolved lameness in 8/8 horses, compared to 3/8 horses with lidocaine blocks. Both agents led to skin desensitization in 8/8 horses. Skin desensitization occurred sooner than lameness resolution after mepivacaine (P = .047). Duration of action was longer with mepivacaine than lidocaine (mean T3_lameness mepivacaine 366 minutes, lidocaine 113 minutes (P = .038); T3_skin mepivacaine 195 minutes, lidocaine 63 minutes [P ≤ .001]). Skin sensitivity returned sooner than lameness after lidocaine block at T3 (P = .015). The use of lidocaine in PDNBs for the purpose of lameness diagnosis should be reassessed, as it may not resolve lameness despite loss of skin sensation. Mepivacaine is superior, with a reliable onset and longer duration of action. Skin desensitization as an indicator for the onset of action or effectiveness of PDNBs for mepivacaine and lidocaine, or as a measure of the duration of action of lidocaine PDNBs should be interpreted with caution. © 2017 The American College of Veterinary Surgeons.

  19. Effect of Intracameral Lidocaine Anesthesia on the Anterior Segment of Rabbit Eyes

    Institute of Scientific and Technical Information of China (English)

    Hui Yang; Danying Zheng; Zhenping Zhang

    2002-01-01

    Purpose: To evaluate the effect of intracameral anesthesia on the anterior segment ofrabbit eyes using chinese-made lidocaine.Method: The study comprised eight eyes of four white rabbits which were divided intothree groups according to the concentration of the lidocaine given. They are 0.5%, 1%,2% lidocaine groups and balanced salt solution(BSS)control group. Each groupcontained two eyes.After 0.5 ml of the anesthetic agent was injected into the anteriorchamber and retainedthere for ten minutes, the rabbits were executed and the eye balls wereenucleated. Pathological examinations of the anterior segment, including cornea, iris andcilliary body, were carried out immediately.Result:The pathological study revealed no abnormal findings in lidocaine 0. 5% and 1%groups compared with the control group, where as in the lidocaine 2% group, muchabnormal pathological change was found, including the shrinkage of corneal endothelium,stroma edema of iris and cilliary body.Conclusion: Using intracameral anesthesia of high concentration of chinese-made lidocainewould run a risk of damaging the anterior segment of rabbit eye. But at the low concentrationusually usedin cataract surgery, no adverse effect was found.

  20. Effect of lidocaine volume and concentration on preventing incidence and severity of propofol injection pain.

    Science.gov (United States)

    Gharavi, Mohammad; Sabzevari, Alireza; Ghorbanian, Ehsanolah; Sajadi, Rasoul; Akhondi, Mohsen

    2014-03-01

    Propofol is one of common anesthetic drugs used in anesthesia. The most common side effects of propofol are local pain. Pretreatment with lidocaine can reduce propofol injection pain. The aim of the present study was to assess and compare the efficiency of lidocaine 0.4% and 2% in reducing the incidence and severity of propofol injection pain. This was a double blind prospective clinical trial on children 4-8 years old with class ASA I and II candidates who were referred to Dr. Shaikh Hospital in Mashhad for elective surgery. Sample size calculated 50 patients in each groups based on pilot study. 100 children's were randomly divided equally in two groups, who were injected with lidocaine solutions 2% and 0.4% respectively. patient's pain evaluation based on VSD (verbal descriptor scale) and NRS (Numeric Rating Scale) using patient's verbal reaction and behavior namely fretting, hand drag and tearing. The collated data was analyzed. There was nosignificant difference as to the first three variables (age, gender and weight P > 0.2). The significant difference regarding pain experience in both groups was noteworthy (P > 0.2). Most of the studies compared lidocaine with other drugs or its efficiency at different doses. Our study is different in that we applied a constant dose of lidocaine in various volumes and concentration. This result shows that lidocaine with the same does but lower concentration and higher volume is more effective in preventing propofol injection pain. Using diluted lidocaine with the dosage of 1 mg/kg and a concentration of 0.4% is an effective way to relieve pain caused by propofol injection in children.

  1. Pain and efficacy of local anesthetics for central venous access

    Directory of Open Access Journals (Sweden)

    William C Culp Jr

    2008-11-01

    Full Text Available William C Culp Jr1, Mohammed Yousaf2, Benjamin Lowry1, Timothy C McCowan3, William C Culp21Division of Cardiothoracic Anesthesiology, Scott and White Hospital, The Texas A&M University College of Medicine, Temple, TX, USA; 2Division of Interventional Radiology, University of Arkansas for Medical Sciences, Little Rock, AR, USA; 3Department of Radiology, University of Mississippi Medical Center, Jackson, MS, USAPurpose: To compare pain during injection and efficacy of analgesia of local anesthetics during central venous line placement.Methods: Sixty-two patients were studied in a randomized, double-blinded prospective fashion. Patients received 1% lidocaine (L, buffered 1% lidocaine (LB, or 2% chloroprocaine (CP injected around the internal jugular vein for procedural analgesia for central venous access. Patients reported pain via a standard linear visual analog scale, with 0 representing no pain and 10 being the worst pain imaginable.Results: Overall patient perception of pain was better with CP and L than LB with mean scores of CP 2.4, L 2.6, LB 4.2. Pain with injection mean scores were CP 2.1, L 2.5, LB 3.2. Pain with catheter placement scores were CP 2.5, L 1.7, LB 3.4. Operator assessment of overall pain values were CP 1.9, L 2.2, LB 3.4. LB consistently scored the worst, though compared with CP, this only reached statistical significance in overall patient pain and pain at catheter insertion compared with L.Conclusion: Though chloroprocaine scored better than lidocaine in 3 of 4 parameters, this trend did not achieve statistical significance. Adding sodium bicarbonate to lidocaine isn’t justified in routine practice, nor is routine replacement of lidocaine with chloroprocaine.Keywords: local anesthesia, analgesia, central venous access, lidocaine, chloroprocaine

  2. Anesthetic activity of the essential oil of Ocimum americanum in Rhamdia quelen (Quoy & Gaimard, 1824 and its effects on stress parameters

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    Lenise de Lima Silva

    Full Text Available ABSTRACT The aim of this study was to evaluate the anesthetic activity of the essential oil (EO of Ocimum americanum L. in silver catfish (Rhamdia quelen . In the first experiment, the depressor effects and chemical composition of the leaf EO (LEO and inflorescence EO (IEO were compared. Juveniles (n = 10 were placed in aquaria containing different concentrations of EO (25 - 500 mg L-1 to determine the point at which anesthesia was induced and the length of the recovery period. In the following experiment, the effects of 300 and 500 mg L-1 LEO exposure on stress parameters (plasma cortisol, glucose and sodium levels after air exposure for 1 min were assayed. Fish (n = 10 per sampling time were sampled immediately or transferred to anesthetic-free aquaria until sampling (15, 30, 60 or 240 min. LEO was composed mainly of β-linalool and 1,8-cineole in similar proportions, whereas IEO showed β-linalool as major compound. Anesthesia was obtained in silver catfish with 200-500 mg L-1 between 4-8 min for LEO and 6-16 min for IEO. Lower EO concentrations did not reach anesthetic stage up to 30 min. LEO used as anesthetic prevented the cortisol increase and sodium loss induced by aerial exposure. Glucose levels were raised in catfish exposed to LEO compared to basal group (not air exposed in almost all observation times. EO of O. americanum obtained from leaves was considered suitable to anesthetic procedures due to its fast induction and handling-induced stress prevention.

  3. Membrane fluidization by ether, other anesthetics, and certain agents abolishes P-glycoprotein ATPase activity and modulates efflux from multidrug-resistant cells.

    Science.gov (United States)

    Regev, R; Assaraf, Y G; Eytan, G D

    1999-01-01

    The anesthetics benzyl alcohol and the nonaromatic chloroform and diethyl ether, abolish P-glycoprotein (Pgp) ATPase activity in a mode that does not fit classical competitive, noncompetitive, or uncompetitive inhibition. At concentrations similar to those required for inhibition of ATPase activity, these anesthetics fluidize membranes leading to twofold acceleration of doxorubicin flip-flop across lipid membranes and prevent photoaffinity labeling of Pgp with [125I]-iodoarylazidoprazosin. Similar concentrations of ether proved nontoxic and modulated efflux from Pgp-overexpressing cells. A similar twofold acceleration of doxorubicin flip-flop rate across membranes was observed with neutral mild detergents, including Tween 20, Nonidet P-40 and Triton X-100, and certain Pgp modulators, such as verapamil and progesterone. Concentrations of these agents, similar to those required for membrane fluidization, inhibited Pgp ATPase activity in a mode similar to that observed with the anesthetics. The mode of inhibition, i.e. lack of evidence for classical enzyme inhibition and the correlation of Pgp ATPase inhibition with membrane fluidization over a wide range of concentrations and structures of drugs favors the direct inhibition of Pgp ATPase activity by membrane fluidization. The unusual sensitivity of Pgp to membrane fluidization, as opposed to acceleration of ATPase activity of ion transporters, could fit the proposed function of Pgp as a 'flippase', which is in close contact with the membrane core.

  4. Lidocaine Stimulates the Function of Natural Killer Cells in Different Experimental Settings.

    Science.gov (United States)

    Cata, Juan P; Ramirez, Maria F; Velasquez, Jose F; Di, A I; Popat, Keyuri U; Gottumukkala, Vijaya; Black, Dahlia M; Lewis, Valerae O; Vauthey, Jean N

    2017-09-01

    One of the functions of natural killer (NK) cells is to eliminate cancer cells. The cytolytic activity of NK cells is tightly regulated by inhibitory and activation receptors located in the surface membrane. Lidocaine stimulates the function of NK cells at clinically relevant concentrations. It remains unknown whether this effect of lidocaine has an impact on the expression of surface receptors of NK cells, can uniformly stimulate across different cancer cell lines, and enhances the function of cells obtained during oncological surgery. NK cells from healthy donors and 43 patients who had undergone surgery for cancer were isolated. The function of NK cells was measured by lactate dehydrogenase release assay. NK cells were incubated with clinically relevant concentrations of lidocaine. By flow cytometry, we determined the impact of lidocaine on the expression of galactosylgalactosylxylosylprotein3-beta-glucuronosytranferase 1, marker of cell maturation (CD57), killer cell lectin like receptor A, inhibitory (NKG2A) receptors and killer cell lectin like receptor D, activation (NKG2D) receptors of NK cells. Differences in expression at pcells against ovarian, pancreatic and ovarian cancer cell lines. Lidocaine also increased the cytolytic activity of NK cells from patients who underwent oncological surgery, except for those who had orthopedic procedures. Lidocaine showed an important stimulatory activity on NK cells. Our findings suggest that lidocaine might be used perioperatively to minimize the impact of surgery on NK cells. Copyright© 2017, International Institute of Anticancer Research (Dr. George J. Delinasios), All rights reserved.

  5. Efficacy of articaine: a new amide local anesthetic.

    Science.gov (United States)

    Malamed, S F; Gagnon, S; Leblanc, D

    2000-05-01

    The authors compared the safety and efficacy of 4 percent articaine with epinephrine 1:100,000 with 2 percent lidocaine with epinephrine 1:100,000. In three identical randomized, double-blind, multicenter trials, subjects 4 to 80 years of age received either 4 percent articaine with epinephrine 1:100,000 or 2 percent lidocaine with epinephrine 1:100,000 for simple or complex dental procedures. In each trial, the authors randomized the subjects in a 2:1 ratio to receive articaine or lidocaine. Efficacy was determined by both subject and investigator using a visual analog scale, or VAS. The authors used the Kruskal-Wallis test to analyze the data. A total of 882 subjects received articaine, and 443 received lidocaine. The authors found no statistical differences between the groups (P = .05). They also compared drug volumes for both articaine and lidocaine groups (2.5 milliliters +/- 0.07 standard error of mean, or SEM, vs. 2.6 mL +/- 0.09 SEM for simple procedures and 4.2 mL +/- 0.15 SEM vs. 4.5 mL +/- 0.21 SEM for complex procedures). The procedures' durations were comparable for both the articaine and lidocaine groups. The authors found no statistical difference between the two treatment groups (P = .05) with respect to subject or investigator pain ratings using the VAS; the mean pain scores determined by both patients and investigators for all groups tested were less than 1.0. The authors found that 4 percent articaine with epinephrine 1:100,000 was well-tolerated in 882 subjects. It also provided clinically effective pain relief during most dental procedures and had a time to onset and duration of anesthesia appropriate for clinical use and comparable to those observed for other commercially available local anesthetics. Pain control is a major component of patient comfort and safety. Local anesthetics form the backbone of pain control techniques in dentistry. Four percent articaine with epinephrine is an amide local anesthetic that will meet the clinical

  6. Multichannel Detrended Fluctuation Analysis Reveals Synchronized Patterns of Spontaneous Spinal Activity in Anesthetized Cats

    OpenAIRE

    Erika E Rodríguez; Enrique Hernández-Lemus; Itzá-Ortiz, Benjamín A.; Ismael Jiménez; Pablo Rudomín

    2011-01-01

    The analysis of the interaction and synchronization of relatively large ensembles of neurons is fundamental for the understanding of complex functions of the nervous system. It is known that the temporal synchronization of neural ensembles is involved in the generation of specific motor, sensory or cognitive processes. Also, the intersegmental coherence of spinal spontaneous activity may indicate the existence of synaptic neural pathways between different pairs of lumbar segments. In this stu...

  7. Reduced respiratory neural activity elicits a long-lasting decrease in the CO2 threshold for apnea in anesthetized rats.

    Science.gov (United States)

    Baertsch, N A; Baker, T L

    2017-01-01

    Two critical parameters that influence breathing stability are the levels of arterial pCO2 at which breathing ceases and subsequently resumes - termed the apneic and recruitment thresholds (AT and RT, respectively). Reduced respiratory neural activity elicits a chemoreflex-independent, long-lasting increase in phrenic burst amplitude, a form of plasticity known as inactivity-induced phrenic motor facilitation (iPMF). The physiological significance of iPMF is unknown. To determine if iPMF and neural apnea have long-lasting physiological effects on breathing, we tested the hypothesis that patterns of neural apnea that induce iPMF also elicit changes in the AT and RT. Phrenic nerve activity and end-tidal CO2 were recorded in urethane-anesthetized, ventilated rats to quantify phrenic nerve burst amplitude and the AT and RT before and after three patterns of neural apnea that differed in their duration and ability to elicit iPMF: brief intermittent neural apneas, a single brief "massed" neural apnea, or a prolonged neural apnea. Consistent with our hypothesis, we found that patterns of neural apnea that elicited iPMF also resulted in changes in the AT and RT. Specifically, intermittent neural apneas progressively decreased the AT with each subsequent neural apnea, which persisted for at least 60min. Similarly, a prolonged neural apnea elicited a long-lasting decrease in the AT. In both cases, the magnitude of the AT decrease was proportional to iPMF. In contrast, the RT was transiently decreased following prolonged neural apnea, and was not proportional to iPMF. No changes in the AT or RT were observed following a single brief neural apnea. Our results indicate that the AT and RT are differentially altered by neural apnea and suggest that specific patterns of neural apnea that elicit plasticity may stabilize breathing via a decrease in the AT.

  8. [Anesthetic Management of a Patient who Developed Intraoperative Paroxysmal Supraventricular Tachycardia with Pulseless Electric Activity].

    Science.gov (United States)

    Hakone, Masako; Yamada, Tatsuya; Motoyasu, Akira; Kasuya, Youhei; Yorozu, Tomoko

    2016-06-01

    A 75-year-old woman was scheduled to undergo an ileus operation under general combined with epidural anesthesia. Preoperative electrocardiogram (ECG) showed first-degree atrioventricular block. The patient received no preoperative antiarrhythmic medication. During surgery, paroxysmal supraventricular tachycardia (PSVT) occurred unexpectedly with radial artery pulsation disappearing, indicating pulseless electric activity (PEA). After a five-second episode of PSVT, her sinus rhythm recovered spontaneously. However, the patient had repeated short duration of PSVT with PEA. Continuous infusion of ultra-short-acting β-blocker landiolol successfully terminated the PSVT, and sinus rhythm was restored. Postoperative ECG showed sinus rhythm. This case report indicates that β-blocker can be a drug of choice in patients with PSVT associated with PEA.

  9. Anesthetics drug pharmacodynamics.

    Science.gov (United States)

    Bischoff, P; Schneider, G; Kochs, E

    2008-01-01

    Anesthesia cannot be defined in an unambiguous manner. The essential components of general anesthesia are absence of consciousness and pain. This translates into two particular qualities: (1) sedation and hypnosis, i.e., mental blockade and (2) analgesia/antinociception, i.e., sensory blockade. Anesthetic actions on these two subcomponents are difficult to separate. On the one hand, very few anesthetics act exclusively on one of these components. On the other hand, these components are closely related to each other. Unconsciousness prevents (conscious) perception of pain, and nociception may serve as an arousal stimulus and change the level of sedation and hypnosis. The art of anesthesia lies in adequate dosing of drugs to reach both mental and sensory blockade. Drug administration can be based on pharmacokinetic considerations. Pharmacokinetic models allow an estimation of what happens to the administered drug in the body. Models with an effect site compartment may facilitate a tailored administration of anesthetic drugs. Finally, the quantification of pharmacodynamic effects allows a precise titration of drugs. Clinical assessment of mental blockade is often dichotomous, and therefore not very helpful to guide drug administration. Several scoring systems exist, but once consciousness is lost they become less reliable, in particular because reaction to stimuli is assessed, which mixes assessment of mental blockade with assessment of sensory blockade. Clinical assessment of analgesia requires a conscious patient, so antinociception is difficult to measure. Several methods of objective quantification on the basis of electrical brain activity are discussed including EEG and evoked potentials. Despite numerous indexes of the hypnotic component of anesthesia, there is no parameter that unambiguously quantifies the level of mental or sensory blockade.

  10. Effects of Various Antiepileptics Used to Alleviate Neuropathic Pain on Compound Action Potential in Frog Sciatic Nerves: Comparison with Those of Local Anesthetics

    Directory of Open Access Journals (Sweden)

    Yuhei Uemura

    2014-01-01

    Full Text Available Antiepileptics used for treating neuropathic pain have various actions including voltage-gated Na+ and Ca2+ channels, glutamate-receptor inhibition, and GABAA-receptor activation, while local anesthetics are also used to alleviate the pain. It has not been fully examined yet how nerve conduction inhibitions by local anesthetics differ in extent from those by antiepileptics. Fast-conducting compound action potentials (CAPs were recorded from frog sciatic nerve fibers by using the air-gap method. Antiepileptics (lamotrigine and carbamazepine concentration dependently reduced the peak amplitude of the CAP (IC50=0.44 and 0.50 mM, resp.. Carbamazepine analog oxcarbazepine exhibited an inhibition smaller than that of carbamazepine. Antiepileptic phenytoin (0.1 mM reduced CAP amplitude by 15%. On the other hand, other antiepileptics (gabapentin, sodium valproate, and topiramate at 10 mM had no effect on CAPs. The CAPs were inhibited by local anesthetic levobupivacaine (IC50=0.23 mM. These results indicate that there is a difference in the extent of nerve conduction inhibition among antiepileptics and that some antiepileptics inhibit nerve conduction with an efficacy similar to that of levobupivacaine or to those of other local anesthetics (lidocaine, ropivacaine, and cocaine as reported previously. This may serve to know a contribution of nerve conduction inhibition in the antinociception by antiepileptics.

  11. Water solvent and local anesthetics: A computational study

    Science.gov (United States)

    Bernardi, R. C.; Gomes, D. E. B.; Pascutti, P. G.; Ito, A. S.; Taft, C. A.; Ota, A. T.

    There are various experimental studies regarding the toxicity and the time of action of local anesthetics, which contain general insights about their pharmacological and physicochemical properties. Although a detailed microscopic analysis of the local anesthetics would contribute to understanding these properties, there are relatively few theoretical studies about these molecules. In this article, we present the results from calculations performed for three local anesthetics: tetracaine, procaine, and lidocaine, both in their charged and uncharged forms, in aqueous environment. We have used the density functional theory and molecular dynamics simulations to study the structural characteristics of these compounds. The radial distribution function g(r) was used to examine the structure of water molecules surrounding different regions of the local anesthetics. We demonstrated the nonhomogeneous character of the anesthetics with respect to their affinity to water solvent molecules as well as the modifications in their affinity to water caused by changes in their charge state. We also observed that the biological potency of the anesthetics is more related to the behavior of specific groups within the molecule, which are responsible for the interaction with the lipid phase of membranes, rather than the general properties of the molecule as a whole.

  12. Use-dependent effects of lidocaine on conduction in canine myocardium: application of the modulated receptor hypothesis in vivo.

    Science.gov (United States)

    Davis, J; Matsubara, T; Scheinman, M M; Katzung, B; Hondeghem, L H

    1986-07-01

    Lidocaine is a commonly used antiarrhythmic drug that causes use-dependent blockade of sodium channels in vitro and reduces conduction velocity in vitro and in vivo. According to the modulated receptor hypothesis of antiarrhythmic drug action, lidocaine has a low affinity for rested sodium channels but a high affinity for open and inactivated channels. In the present experiments, we characterized use-dependent conduction slowing and recovery from slowing by lidocaine in anesthetized dogs. The His-to-ventricular conduction interval was used as the indicator of conduction velocity. We found that prolongation of conduction time was greater as the stimulation frequency was increased. Moreover, on abruptly changing the stimulation frequency, a new steady-state conduction time was approached in two to three depolarizations. On discontinuation of stimulation, the conduction time of progressively less premature extrastimuli shortened exponentially with a terminal phase time constant of 152 +/- 115 msec. These effects by lidocaine were enhanced during acidosis and enhancement was reversed by correction of the acidosis. It is concluded that the effects in vivo of lidocaine on conduction under several conditions of rate, rhythm, and pH are similar to its effects on the maximum upstroke velocity of the action potential in vitro. Although these experiments were not designed to validate the modulated receptor hypothesis, it appears that the modulated receptor hypothesis can predict the effects of lidocaine on conduction in vivo.

  13. Time Course of the Soleus M Response and H Reflex after Lidocaine Tibial Nerve Block in the Rat

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    Kévin Buffenoir

    2013-01-01

    Full Text Available Aims. In spastic subjects, lidocaine is often used to induce a block predictive of the result provided by subsequent surgery. Lidocaine has been demonstrated to inhibit the Hoffmann (H reflex to a greater extent than the direct motor (M response induced by electrical stimulation, but the timecourse of these responses has not been investigated. Methods. An animal (rat model of the effects of lidocaine on M and H responses was therefore developed to assess this time course. M and H responses were recorded in 18 adult rats before and after application of lidocaine to the sciatic nerve. Results. Two to five minutes after lidocaine injection, M responses were markedly reduced (mean reduction of 44% and H reflexes were completely abolished. Changes were observed more rapidly for the H reflex. The effects of lidocaine then persisted for 100 minutes. The effect of lidocaine was therefore more prolonged on the H reflex than on the M response. Conclusion. This study confirms that lidocaine blocks not only alpha motoneurons but also Ia afferent fibres responsible for the H reflex. The authors describe, for the first time, the detailed time course of the effect of lidocaine on direct or reflex activation of motoneurons in the rat.

  14. A prospective, randomized, double-blind comparison of 2% lidocaine with 1:100,000 and 1:50,000 epinephrine and 3% mepivacaine for maxillary infiltrations.

    Science.gov (United States)

    Mason, Rick; Drum, Melissa; Reader, Al; Nusstein, John; Beck, Mike

    2009-09-01

    The purpose of this prospective, randomized, double-blind crossover study was to evaluate the anesthetic efficacy of 2% lidocaine with 1:100,000 and 1:50,000 epinephrine and 3% mepivacaine in maxillary lateral incisors and first molars. Sixty subjects randomly received, in a double-blind manner, maxillary lateral incisor and first molar infiltrations of 1.8 mL of 2% lidocaine with 1:100,000 epinephrine, 2% lidocaine with 1:50,000 epinephrine, and 3% mepivacaine at three separate appointments spaced at least 1 week apart. The teeth were pulp tested in 3-minute cycles for a total of 60 minutes. Anesthetic success and the onset of pulpal anesthesia were not significantly different between 2% lidocaine with either 1:100,000 or 1:50,000 epinephrine and 3% mepivacaine for the lateral incisor and first molar. Increasing the epinephrine concentration from 1:100,000 to 1:50,000 in a 2% lidocaine formulation significantly decreased pulpal anesthesia of short duration for the lateral incisor but not the first molar. For both the lateral incisor and first molar, 3% mepivacaine significantly increased pulpal anesthesia of short duration compared with 2% lidocaine with either 1:100,000 or 1:50,000 epinephrine.

  15. Onset and duration of anesthesia for local anesthetic combinations commonly used in forefoot surgery; surprise results with sequential blocks.

    Science.gov (United States)

    Blazer, Marie Mantini; Petrozzi, Rocco; Harris, Samantha Y; Greer, Hillary; Goldfarb, Jacqueline; Biernacki, Tomasz; Kawalec, Jill S

    2015-06-01

    Local anesthetic nerve blocks are frequently used for postoperative analgesia and to the best of our knowledge no studies have evaluated the effects of injecting bupivacaine into an area previously injected with lidocaine. Sensation was tested in three groups of subjects receiving local anesthetic digital blocks. Group A received bupivacaine 0.25% plain. Group B received a 1:1 mixture of lidocaine 1% plain and bupivacaine 0.25%. Group C received an initial block of lidocaine 1% plain sequentially followed by bupivacaine 0.25% 1h later. Bupivacaine exhibited a delayed onset and the longest duration when compared to the other two groups. The group receiving the 1:1 mixture showed a rapid onset that resembled that of lidocaine and a shortened duration that did not resemble bupivacaine. The group receiving the sequential injections showed that even after a 1h interval following the lidocaine infiltration, there was a deleterious effect on duration of action of the bupivacaine. Using bupivacaine as a post-surgical block in the presence of residual lidocaine from a preoperative block is not warranted as once again, the extended duration of bupivacaine is mitigated. Bupivacaine alone as an initial operative block affords clinically acceptable onset of anesthesia while also providing extended duration of action.

  16. Evaluation of the efficacy and safety of a lidocaine and tetracaine (7%/7%) cream for induction of local dermal anesthesia for facial soft tissue augmentation with hyaluronic Acid.

    Science.gov (United States)

    Cohen, Joel L; Gold, Michael H

    2014-10-01

    Injection of dermal fillers for soft tissue augmentation is a minimally invasive cosmetic procedure with growing popularity. However, patients often express concern about pain with such procedures. A topical anesthetic cream formulated with lidocaine/tetracaine 7%7% was approved by the United States Food and Drug Administration in 2006 and recently reintroduced to the market for use during superficial dermatological procedures. A Phase 3 study was conducted to assess the efficacy and safety of lidocaine/tetracaine 7%7% cream versus placebo cream when used to induce local dermal anesthesia during injections with hyaluronic acid. Mean visual analog scale scores significantly favored lidocaine/tetracaine 7%7% cream. A significant percent of subjects also indicated that lidocaine/tetracaine 7%7% cream provided adequate pain relief and that they would use lidocaine/tetracaine 7%7% cream again. Investigators also rated lidocaine/tetracaine 7%7% cream significantly better than placebo cream for providing adequate pain relief and on the assessment of pain scale. Lidocaine/tetracaine 7%7% cream was safe and well tolerated with most subjects reporting no erythema, edema, or blanching. No related adverse events were reported with lidocaine/tetracaine 7%7% cream; one related adverse event of erythema was reported with placebo cream. The results of this study indicate that lidocaine/tetracaine 7%7% cream is efficacious and safe at providing pain relief for soft tissue augmentation with hyaluronic acid.

  17. Ion-transfer voltammetry of local anesthetics at an organic solvent/water interface and pharmacological activity vs. ion partition coefficient relationship.

    Science.gov (United States)

    Kubota, Y; Katano, H; Senda, M

    2001-01-01

    The ion-transfer reaction of local anesthetics at an organic solvent/water interface has been studied using cyclic voltammetry (CV) with a stationary nitrobenzene (NB)/water (W) interface. Procaine and seven other local anesthetics gave reversible or quasi-reversible voltammograms at the NB/W interface in the pH range between 0.9 and 9.6. These drugs are present in aqueous solution in either neutral or ionic form, or both forms. The half-wave potential, as determined by the midpoint potential in CV, vs. pH curves, were determined and analyzed to determine the partition coefficients of both neutral and ionic forms of the drugs between NB and W. The partition coefficients of the ionic forms were derived from their formal potential of transfer at an NB/W interface. The dissociation constants of ionic forms of the drugs in NB were also deduced. A high correlation between the pharmacological activity and the partition coefficient of the ionic form of amide-linked local anesthetics has been shown.

  18. Interactions of some local anesthetics and alcohols with membranes.

    Science.gov (United States)

    Frangopol, P T.; Mihăilescu, D

    2001-09-01

    A review of the results obtained by our group in the last decade regarding the interactions of procaine, lidocaine, dibucaine and tetracaine with membranes is presented in the context of the literature data. The action upon membranes, in first approximation monomolecular film of stearic acid spread at the air/water interface used as a membrane model, the modification of biomembrane structure and function using diffraction methods, lipid phase transition, fluidity of lipids and proteins, membrane expansion and platelet aggregation were studied. The thermodynamic knowledge of membrane-alcohol interactions improved by using highly sensitive calorimetric techniques are briefly reported. One of the main conclusions is that the physical state of a monolayer model membrane was the result of competitive interactions between film-film and film-substrate interactions. It was taken into account that local anesthetics, such as lidocaine, carbisocaine, mesocaine, showed changes in the bilayer structure, reflected in macroscopic mechanical properties. This restructuring of the lipid bilayer has a significant influence on the operation of functional subunits, e.g. ionic channels formed by gramicidin. The results support the concept of non-specific interactions of local anesthetics with lipid bilayers. The theoretical modeling of the interactions of local anesthetics is closely compared with experimental data. Our new theory of relaxation for these interactions is using a non-archimedean formalism based on a process resulting from superpositions of different component processes which take place at different scales of time.

  19. Comparison of the effects of mepivacaine and lidocaine on rat myocardium.

    Science.gov (United States)

    David, J-S; Amour, J; Duracher, C; Ferretti, C; Precloux, P; Petit, P; Riou, B; Gueugniaud, P-Y

    2007-02-01

    To compare the inotropic and lusitropic effect of lidocaine and mepivacaine on rat papillary muscle. Effects of lidocaine and mepivacaine (10-8-10-3 M) were studied in rat left ventricular papillary muscles in vitro at a calcium concentration of 1 mmol, under low (isotony) and high (isometric) loads. Lidocaine induced a significant negative inotropic effect in isotonic and isometric conditions whereas mepivacaine did not. Mepivacaine only induced a negative inotropic effect when added as a bolus for the highest concentration and this effect was significantly more pronounced with lidocaine than with mepivacaine (active force at 10-3 M: 63 +/- 10 vs. 84 +/- 10% of baseline, P mepivacaine groups (197 +/- 22% of baseline) when compared to the lidocaine group (163 +/- 19% of baseline, P mepivacaine and suggested an impairment of sarcoplasmic reticulum function. Lidocaine and mepivacaine did not modify post-rest potentiation but significantly depressed the force-frequency relationship. The negative inotropic and lusitropic effects induced by lidocaine were more important than that of mepivacaine and may involve an impairment of intracellular Ca2+ handling.

  20. Acute physiological responses to castration-related pain in piglets: the effect of two local anesthetics with or without meloxicam.

    Science.gov (United States)

    Bonastre, C; Mitjana, O; Tejedor, M T; Calavia, M; Yuste, A G; Úbeda, J L; Falceto, M V

    2016-09-01

    Methods to reduce castration-related pain in piglets are still issues of concern and interest for authorities and producers. Our objectives were to estimate the effectiveness of two protocols of local anesthesia (lidocaine and the combination of lidocaine+bupivacaine) as well as the use of meloxicam as a postoperative analgesic in alleviating castration-related pain, measured by acute physiological responses. Eight groups (15 piglets/group) were included in the study: (1) castration without anesthesia or analgesia, without meloxicam (TRAD WITHOUT), (2) castration without anesthesia or analgesia, but with meloxicam (TRAD WITH), (3) handling without meloxicam (SHAM WITHOUT), (4) handling with meloxicam (SHAM WITH), (5) castration after local anesthesia with lidocaine but without meloxicam (LIDO WITHOUT), (6) castration after local anesthesia with lidocaine and meloxicam (LIDO WITH), (7) castration after local anesthesia with lidocaine+bupivacaine without meloxicam (LIDO+BUPI WITHOUT), (8) castration after local anesthesia with lidocaine+bupivacaine and meloxicam (LIDO+BUPI WITH). Acute physiological responses measured included skin surface temperature and serum glucose and cortisol concentrations. On days 4 and 11 post-castration BW was recorded and average daily gain was calculated over this period. Furthermore, piglet mortality was recorded over the 11-day post-castration period. Administration of local anesthetic or meloxicam did not prevent the decrease in skin surface temperature associated with castration. Lidocaine reduced the increase in glucose concentration associated with castration. For castrated pigs, the joint use of lidocaine and meloxicam caused a significant decrease in cortisol concentration; the combination of intratesticular lidocaine and bupivacaine did not seem to be more effective than lidocaine alone. No effect of treatments on mortality and growth were detected.

  1. Isobolographic analysis of interaction between spinal endomorphin-1, a newly isolated endogenous opioid peptide, and lidocaine in the rat formalin test.

    Science.gov (United States)

    Hao, S; Takahata, O; Iwasaki, H

    1999-12-10

    Endomorphin-1, a newly isolated endogenous opioid ligand, has a potential affinity with mu-opioid receptor. We investigated antinociception of intrathecal endomorphin-1 and lidocaine in the rat formalin test and examined the interaction between the two agents using isobolographic analysis. Intrathecal endomorphin-1 caused dose-dependent suppression of the formalin-induced biphasic behavioral response. Intrathecal lidocaine produced dose-dependent inhibition of phase-2 behavioral response. Isobolographic analysis confirmed that combination of intrathecal endomorphin-1 and lidocaine, given at a fixed dose ratio, produced synergistic suppression of phase-2 behavioral response. These data demonstrate that spinal endomorphin-1 synergistically interacts with local anesthetic lidocaine in producing antinociception in the formalin test.

  2. Effect of PaCO2 and PaO2 on lidocaine and articaine toxicity.

    Science.gov (United States)

    Barcelos, K C; Furtado, D P; Ramacciato, J C; Cabral, A M; Haas, D A

    2010-01-01

    Alterations in arterial PaCO₂ can influence local anesthetic toxicity. The objective of this study was to evaluate the effect of stress-induced changes in PaCO₂ and PaO₂ on the seizure threshold of lidocaine and articaine. Lidocaine (2% with 1 : 100,000 epinephrine) or articaine (4% with 1 : 100,000 epinephrine) was administered intravenously under rest or stress conditions to 36 rats separated into 4 groups. Propranolol and prazosin were administered preoperatively to minimize cardiovascular effects of epinephrine. Mean arterial pressure (MAP), heart rate (HR), and arterial pH, PaCO₂, and PaO₂ were measured. Results showed no differences in MAP, HR, or pH. Stress significantly increased the latency period for the first tonic-clonic seizure induced by a toxic dose of both lidocaine and articaine (P < .05). Seizures were brought on more rapidly by articaine. No significant difference between toxic doses of lidocaine and articaine was noted. Stress raised the seizure threshold dose for both drugs and significantly (P < .01) increased arterial PaO₂ from 94.0 ± 1.90 mm Hg to 113.0 ± 2.20 mm Hg, and reduced PaCO₂ from 36.0 ± 0.77 mm Hg to 27.0 ± 0.98 mm Hg. In conclusion, reduction in PaCO₂ and/or increase in PaO₂ raised the seizure threshold of lidocaine and articaine. This study also confirmed that lidocaine and articaine have equipotent central nervous system toxicity.

  3. A Comparison of Equivalent Doses of Lidocaine and Articaine in Maxillary Posterior Tooth Extractions: Case Series

    Directory of Open Access Journals (Sweden)

    Christopher C. Friedl

    2012-06-01

    Full Text Available Objectives: Local anaesthesia is the standard of care during dental extractions. With the advent of newer local anesthetic agents, it is often difficult for the clinician to decide which agent would be most efficacious in a given clinical scenario. This study assessed the efficacy of equal-milligram doses of lidocaine and articaine in achieving surgical anaesthesia of maxillary posterior teeth diagnosed with irreversible pulpitis. Material and Methods: This case-series evaluated a total of 41 patients diagnosed with irreversible pulpitis in a maxillary posterior tooth. Patients randomly received an infiltration of either 3.6 mL (72 mg 2% lidocaine with 1:100,000 epinephrine or 1.8 mL (72 mg 4% articaine with 1:100,000 epinephrine in the buccal fold and palatal soft tissue adjacent to the tooth. After 10 minutes, initial anaesthesia of the tooth was assessed by introducing a sterile 27-gauge needle into the gingival tissue adjacent to the tooth, followed by relief of the gingival cuff. Successful treatment was considered to have occurred when the tooth was extracted with no reported pain. Data was analyzed with the Fisher’s exact test, unpaired t-test and normality test. Results: Twenty-one patients received lidocaine and 20 received articaine. Forty of the 41 patients achieved initial anaesthesia 10 minutes after injection: 21 after lidocaine and 19 after articaine (P = 0.488. Pain-free extraction was accomplished in 33 patients: 19 after lidocaine and 14 after articaine buccal and palatal infiltrations (P = 0.226. Conclusions: There was no significant difference in efficacy between equivalent doses of lidocaine and articaine in the anaesthesia of maxillary posterior teeth with irreversible pulpitis.

  4. Use-dependent block of cardiac sodium channels by quaternary derivatives of lidocaine.

    Science.gov (United States)

    Gintant, G A; Hoffman, B F

    1984-02-01

    Modulation of the reduction of fast inward sodium current by local anesthetics due to changes in electrical activity has been termed use-dependent block ( Courtney 1975). To determine the mechanisms responsible for use-dependent block of cardiac sodium channels and to compare use-dependent block in cardiac and nerve preparations, we investigated use-dependent block of cardiac sodium channels by the quaternary lidocaine analogues QX -314 and QX -222 (two agents previously studied in nerve). We used canine cardiac Purkinje fibers, and assessed changes in the fast inward sodium current using changes in the maximum rate of rise of the action potential upstroke (Vmax). Two microelectrode voltage clamp and current clamp techniques were used to control membrane potential prior to stimulated upstrokes . Use-dependent block was not affected by shortening the action potential duration during rapid stimulation. Partial recovery from use-dependent block was observed during rapid stimulation with brief depolarizing prepulses terminating immediately prior to the upstroke. Similar prepulses also prevented the development of use-dependent block following an abrupt increase in the stimulation rate. Hyperpolarizing prepulses during rapid stimulation caused recovery from use-dependent block; recovery was greater and more rapid with increasingly negative prepulses . Hyperpolarization during periods of electrical quiescence also caused greater recovery. These results, interpreted using the modulated receptor hypothesis ( Hille 1977; Hondeghem and Katzung 1977), suggest that use-dependent block of cardiac sodium channels by quaternary local anesthetics is due to drug association with the inactivated sodium channel receptor which occurs only after these drugs gain access to the receptor site through open sodium channels.

  5. Effects of a quaternary lidocaine derivative, QX-314, on the respiratory activity in brainstem-spinal cord preparation from newborn rats.

    Science.gov (United States)

    Takahashi, Kenichi; Hayakawa, Chikara; Onimaru, Hiroshi

    2016-04-21

    In the clinical setting, the use of QX-314 (a quaternary derivative of lidocaine) has been proposed to achieve the selective inhibition of nociceptors that express transient receptor potential vanilloid 1 (TRPV1) channels with fewer motor deficits. However, it has been also reported that QX-314 may produce systemic CNS toxicities with relative potencies that are approximately twice as high as those of lidocaine. There are no reports concerning the effects of extracellular QX-314 on the rhythm-generating neurons in the respiratory center. In the present study, we examined the effects of QX-314 on respiratory rhythm generation in brainstem-spinal cord preparations from newborn rats. The extracellular application of QX-314 (200μM) decreased the C4 burst rate, amplitude and slope during the initial rising phase, and the effects slowly developed with a half-decay time of approximately 20min. The combined application of capsaicin (10 or 100μM) with QX-314 (100μM) showed no additional effect. The intracellular application of QX-314 (100μM) to respiratory neurons depressed the action potentials with a half-decay time of around 5min. Our findings could explain one of the mechanisms underlying the central toxicities that occur after the systemic application of QX-314.

  6. Cardiovascular alterations after injection of 2% lidocaine with norepinephrine 1:50,000 (xylestesin) in rats.

    Science.gov (United States)

    Faraco, Fatima Neves; Armonia, Paschoal Laercio; Malamed, Stanley F

    2007-01-01

    The purpose of the present study is to determine the cardiovascular effects produced by intravascular injection of 2% lidocaine with 20 microg/mL of norepinephrine on systolic, diastolic, and mean arterial pressures and heart rate of rats at the following times: control period, during the injection (first 15 seconds), during the first minute, and at the end of 1, 2, 3, 4, 5, 10, 15, 20, 25, and 30 minutes after drug administration. The study was performed on 13 male Wistar rats with weights between 200 grams and 220 grams that were awake during the recording of these parameters. The dose administered was proportional to 1 cartridge of local anesthetic (1.8 mL) in an average-size human, which is equivalent to 0.51 mg/kg of lidocaine hydrochloride and 0.51 microg/kg of norepinephrine hydrochloride. The average time of injection was 15.7 seconds. The results of this study showed significant increases in systolic, diastolic, and mean arterial pressure and a noticeable decrease in heart rate. The greatest variation occurred in the systolic blood pressure. The greatest alterations occurred during injection and within the first minute following administration of the anesthetic solution. We would anticipate these changes in the parameters analyzed to be clinically significant. Thus, dentists using 2% lidocaine with norepinephrine 20 mug/mL should be very careful to avoid intravascular injection.

  7. Cardiovascular Alterations After Injection of 2% Lidocaine With Norepinephrine 1:50,000 (Xylestesin) in Rats

    Science.gov (United States)

    Faraco, Fatima Neves; Armonia, Paschoal Laercio; Malamed, Stanley F

    2007-01-01

    The purpose of the present study is to determine the cardiovascular effects produced by intravascular injection of 2% lidocaine with 20 μg/mL of norepinephrine on systolic, diastolic, and mean arterial pressures and heart rate of rats at the following times: control period, during the injection (first 15 seconds), during the first minute, and at the end of 1, 2, 3, 4, 5, 10, 15, 20, 25, and 30 minutes after drug administration. The study was performed on 13 male Wistar rats with weights between 200 grams and 220 grams that were awake during the recording of these parameters. The dose administered was proportional to 1 cartridge of local anesthetic (1.8 mL) in an average-size human, which is equivalent to 0.51 mg/kg of lidocaine hydrochloride and 0.51 μg/kg of norepinephrine hydrochloride. The average time of injection was 15.7 seconds. The results of this study showed significant increases in systolic, diastolic, and mean arterial pressure and a noticeable decrease in heart rate. The greatest variation occurred in the systolic blood pressure. The greatest alterations occurred during injection and within the first minute following administration of the anesthetic solution. We would anticipate these changes in the parameters analyzed to be clinically significant. Thus, dentists using 2% lidocaine with norepinephrine 20 μg/mL should be very careful to avoid intravascular injection. PMID:17579502

  8. Tolerance of local anesthetic for transrectal ultrasound-guided prostate biopsy: our experience and a literature review

    Energy Technology Data Exchange (ETDEWEB)

    Buckley, M.R.E.; Bryant, N.J.; Brown, J.A.; Tiwari, P.; Cooperberg, P.L.; Wong, A.D. [St Paul' s Hospital, Ultrasound Dept., Vancouver, British Columbia (Canada)]. E-mail: twong@providcencehealth.bc.ca

    2006-06-15

    To determine whether local anesthetic injection or gel reduced pain during transrectal ultrasound-guided prostate biopsies and whether there was significant difference between quadrant and apex-only anesthesia. Between September 2001 and May 2002, 240 male patients with elevated prostate-specific antigen and (or) abnormal digital rectal examination were randomized into 1 of 4 groups: 1) transrectal lidocaine gel, 2) quadrant lidocaine injections, 3) apex-only lidocaine injections, or 4) no local anesthetic. Patients scored their pain on a numerical rating scale where 0 indicated no pain and 10 indicated worst pain. We analyzed mean and standard deviations of scores, using a 1-way analysis of variance (ANOVA) and post hoc multiple comparisons with Tukey's honestly significant difference (HSD) studentized range test to determine whether there were significant differences across the groups. There was no significant difference between local anesthetic gel (mean 3.1, SD 1.9) and no anesthetic (mean 3.5, SD 1.9) or between quadrant (mean 1.7, SD 1.7) and apex-only (mean 2.0, SD 1.8) local anesthetic injections. There was significant difference between quadrant injections (mean 1.7, SD 1.7) and no local anesthetic (mean 3.5, SD 1.9) and between apex-only injections (mean 2.0, SD 1.8) and no local anesthetic (mean 3.5, SD 1.9). There was significant pain reduction with local anesthetic injections but not with gel, and since there was no significant difference in efficacy between quadrant and apex-only injections, we recommend apex-only local anesthetic injections for transrectal ultrasound-guided prostate biopsies because it simplifies the injection procedure. (author)

  9. Do lubricants with 2% lidocaine gel have an effect on patient comfort in diagnostic cystoscopy?

    Science.gov (United States)

    Goktug, Hasan Nedim Goksel; Ozturk, Ufuk; Sener, Nevzat Can; Tuygun, Can; Bakırtas, Hasan; Imamoglu, M Abdurrahim

    2014-01-01

    Patients undergoing both rigid and flexible cystoscopic evaluation suffer from a great deal of pain and discomfort. In this study, we aimed to investigate the effect of lidocaine gel anestesia on patient comfort on diagnostic rigid cystoscopy. 11 mL of lubricant gel applied to each patient via the external meatus in 10 s. Patients were randomized into three groups. In group 1, liquid glycerine was applied and cystoscopy was immediately performed, in group 2 lidocaine gel (Aqua Touch™: İstem Tıbbi Cihaz Ve Sanayi Ltd.Şti, Ostim, Ankara, Türkiye) was applied and the procedure undergone immediately and in group 3, lidocaine gel was applied and penis was clemped for 10 minutes before the procedure. VAS forms were filled to determine the discomfort and pain during cystoscopy and the first micturation after. After the evaluation between groups, VAS scores were significantly lower in Group II and III than Group I and in Group III than in Group II (p ocal anesthetic lidocaine gel in rigid cystoscopy, is a practical, safe and efficient method to improve patient comfort when applied in appropriate dose and waiting duration.

  10. NaHCO3-Buffered Lidocaine Gel for Outpatient Rigid Cystoscopy in Men.

    Science.gov (United States)

    Li, Hong; Cheng, Yanxin; Li, Jun; Chen, Yongxue; Yuan, Jinge; Yang, Shuhong; Shi, Huiqiao; Li, Wenpin; Yang, Shijie; Wang, Wei; Xu, Guanjie; Zhao, Senming

    2016-04-01

    The purpose of this study was to explore the effect of NaHCO3-buffered lidocaine gel as a topical anesthetic agent for pain relief for rigid cystoscopy. Prospective randomized controlled trial. ASA I-II male patients undergoing rigid cystoscopy randomly received 10 mL 2% Carbocaine lidocaine gel with 1 mL 0.9% saline (group 1) or 1 mL 5% NaHCO3 solution (group 2). After 3 minutes exposure, the cystoscope was inserted into the urethra. On receiving the gel, cystoscope insertion, and intravesical observation, pain score was recorded using the visual analog scale. The gel pH with or without NaHCO3 was 7.20 and 6.41, respectively. The concentration of soluble lidocaine in the gel was stable for 24 hours or more. The visual analog scale score in group 2 was significantly lower (1.3 ± 0.9) than in group 1 (5.28 ± 1.99). No adverse effects were recorded. Alkalized lidocaine gel resulted in successful analgesia for rigid cystoscopy in men without adverse effects. Copyright © 2016 American Society of PeriAnesthesia Nurses. Published by Elsevier Inc. All rights reserved.

  11. Safe extensive tumescent liposuction with segmental infiltration of lower concentration lidocaine under monitored anesthesia care.

    Science.gov (United States)

    Wang, Gang; Cao, Wei-Gang; Li, Sheng-Li; Liu, Li-Na; Jiang, Zhao-Hua

    2015-01-01

    Tumescent anesthesia makes it feasible to perform liposuction in an office setting. There are often patients who desire extensive liposuction on approximately 30% of total body surface area, which means the lidocaine total dose might be over the dosing recommendation. So the segmental infiltration is applied, although the concentration of lidocaine in tumescent fluid is gradually reduced to 0.0252%. Moreover, supplemental intravenous (IV) sedation using monitored anesthesia care is usually applied concurrently to help alleviate discomfort and pain of the patients during tumescent anesthetic infusion and fat extraction which in turn increases the risks of potential lidocaine toxicity due to possible drug interactions. This study was to demonstrate the safety of segmental infiltration of tumescent fluid with lower lidocaine concentration combined with IV sedation in extensive liposuction and determine whether the risk of lidocaine toxicity is increased in this protocol. Ten female patients who requested the extensive liposuction participated in the study. The targeted areas were divided into 2 segments and treated in turn in 1 session. Lidocaine (1600 mg) was infiltrated into the first segment, and approximately 928 mg lidocaine was subsequently infiltrated after accomplishment of the first segment operation. Serum levels of lidocaine were taken every 4 hours during the first 24 hours after the second infiltration. The average time of the procedure is 222 (33) minutes. The dose and total amount of lidocaine injected are 40.7 (5.8) mg/kg and 2528.2 (155.2) mg, respectively. The total volume of the infusates and aspirates are 9918.1 (494) and 6325 (1461.6) mL, respectively, the ratio of total infusates to total aspirates is 1.66 (0.45). The total aspirated fat and fluids are 3280 (1051.8) and 3045 (824.1) mL, respectively. The peak lidocaine levels [2.18 (0.63) μg/mL] occurred after 12 to 20 hours [16.4 (2.27) hours]. No significant correlation between dose per

  12. Effectiveness of topical anesthetics on reducing tactile sensitivity in the paws of newborn rats.

    Science.gov (United States)

    Strain, Misty M; Vineyard, Mary Ann; Roberto, Megan E; Brumley, Michele R

    2014-01-01

    The aim of this study was to evaluate the effectiveness of three local, topical anesthetics on touch response thresholds of the paws of 1-day-old rats. Touch response thresholds were measured using Semmes Weinstein monofilaments after treatment of the paws with EMLA (2.5% lidocaine and 2.5% prilocaine), alcaine (.5% proparacaine), triocaine (20% benzocaine, 6% lidocaine, and 4% tetracaine), or petroleum jelly (treatment control). Touch thresholds significantly increased after treatment with EMLA 18% of the time, and there was no evidence of a systemic effect. Touch thresholds were not significantly altered after treatment with alcaine, triocaine, or petroleum jelly. Therefore, EMLA appears to be a slightly effective topical anesthetic for reducing tactile sensitivity in newborn rats.

  13. Subcutaneous Injection of Triamcinolone and Lidocaine to Prevent Postherpetic Neuralgia.

    Science.gov (United States)

    Ni, Jiaxiang; Wang, Xiaoping; Tang, Yuanzhang; Yang, Liqiang; Zeng, Yuanjie; Guo, Yuna

    2017-07-01

    Herpes zoster (HZ) is associated with inflammation of the peripheral nerves, which is considered to be an important cause of postherpetic neuralgia (PHN). Interventions aimed at reducing this inflammation could prevent PHN. One option is the epidural administration of corticosteroid and local anesthetic. However, several authors have reported a risk of arachnoiditis with epidural corticosteroids. Subcutaneous injection in an outpatient setting is a safer option. However, there is limited evidence of the effectiveness of this alternative for preventing PHN. The aim of this study was to assess the effectiveness of subcutaneous injection of triamcinolone and lidocaine for the prevention of PHN in elderly HZ patients. Randomized, single-center, clinical trial. Department of pain management of a teaching hospital in Beijing, China. Patients with acute HZ with rash subcutaneous injection of triamcinolone and lidocaine. The severity of pain was assessed using a numeric rating scale (NRS) at enrollment and at one, 3, and 6 months after rash onset. Quality of life (QoL) was evaluated by the SF-36 before treatment and at 3 and 6 months after rash onset. The primary endpoint was the presence of zoster-associated pain (ZAP) at 3 months after rash onset. At enrollment, all patients reported ZAP with average NRS scores of 6.64 ± 1.44 and 7.16 ± 1.22 in the standard group and subcutaneous group, respectively. At 3 and 6 months after rash onset, the pain had decreased in both groups, but the decrease was significantly greater in the subcutaneous injection group. At 3 months, 2 (4%) patients in the subcutaneous injection group vs. 10 (20%) patients in the standard group had ZAP with NRS > 3 (P = 0.014). Both groups showed significant improvement in QoL at 3 and 6 months. No patient had major adverse events related to the subcutaneous injection. The main limitation of the study was the absence of a placebo subcutaneous injection in the standard group. Subcutaneous injection of

  14. Efficacy of caudal epidural injection of lidocaine, xylazine and xylazine plus hyaluronidase in reducing discomfort produced by electroejaculation in bulls.

    Science.gov (United States)

    Pagliosa, Ronaldo C; Derossi, Rafael; Costa, Deiler S; Faria, Fabio J C

    2015-11-01

    To test the hypothesis that epidural administration of lidocaine, xylazine or xylazine plus hyaluronidase provides reduced pain and stress during electroejaculation in bulls, eight 30-month-old Nellore bulls received saline solution (control), 2% lidocaine, 2% xylazine or 2% xylazine plus hyaluronidase injected into the first intercoccygeal (Co1-Co2) epidural space in randomized order. Heart rate, respiratory rate, mean arterial pressure, analgesia, animal behavior and motor blockade were evaluated before treatment and at predetermined intervals during and after treatment. Pain and stress were scored subjectively, and semen quality was evaluated. The onset of anesthetic action was significantly faster with lidocaine (3.0 ± 1.2 min) than with xylazine or xylazine plus hyaluronidase (8.9 ± 1.5 and 5.5 ± 2.6 min, P=0.021 and P=0.012, respectively), and the onset of anesthesia with xylazine plus hyaluronidase was significantly faster than that with xylazine alone (P=0.032). Treatment with xylazine or xylazine plus hyaluronidase resulted in less discomfort than treatment with lidocaine, as indicated by animal behavior. Changes in heart rate, respiratory rate and arterial pressure were within acceptable limits. Penile protrusion and semen emission occurred in all animals during all four treatments. Our results suggest that xylazine plus hyaluronidase reduced discomfort during electroejaculation more effectively than xylazine or lidocaine alone. Further experiments are necessary to determine whether electroejaculation with xylazine plus hyaluronidase is feasible for obtaining semen from Nellore bulls unaccustomed to being handled or restrained.

  15. Lidocaine for systemic sclerosis: a double-blind randomized clinical trial

    Directory of Open Access Journals (Sweden)

    Trevisani Virgínia FM

    2011-02-01

    Full Text Available Abstract Background Systemic sclerosis (scleroderma; SSc is an orphan disease with the highest case-specific mortality of any connective-tissue disease. Excessive collagen deposit in affected tissues is a key for the disease's pathogenesis and comprises most of the clinical manifestations. Lidocaine seems to be an alternative treatment for scleroderma considering that: a the patient's having excessive collagen deposits in tissues affected by scleroderma; b the patient's demonstrating increased activity of the enzyme prolyl hydroxylase, an essential enzyme for the biosynthesis of collagen; and c lidocaine's reducing the activity of prolyl hydroxylase. The aim of this study was to evaluate the efficacy and safety of lidocaine in treating scleroderma. Methods A randomized double-blind clinical trial included 24 patients with scleroderma randomized to receive lidocaine or placebo intravenously in three cycles of ten days each, with a one-month interval between them. Outcomes: cutaneous (modified Rodnan skin score, oesophageal (manometry and microvascular improvement (nailfold capillaroscopy; improvement in subjective self-assessment and in quality of life (HAQ. Results There was no statistically significant difference between the groups for any outcome after the treatment and after 6-months follow-up. Improvement in modified Rodnan skin score occurred in 66.7% and 50% of placebo and lidocaine group, respectively (p = 0.408. Both groups showed an improvement in subjective self-assessment, with no difference between them. Conclusions Despite the findings of a previous cohort study favouring the use of lidocaine, this study demonstrated that lidocaine at this dosage and means of administration showed a lack of efficacy for treating scleroderma despite the absence of significant adverse effects. However, further similar clinical trials are needed to evaluate the efficacy of lidocaine when administered in different dosages and by other means.

  16. 必兰浸润麻醉与利多卡因阻滞麻醉在下颌阻生齿微创拔牙术中的临床对照研究%A comparison of the clinical anesthetic efficacy of articaine infiltration and lidocaine blocking for microport extraction of impacted mandibular molar

    Institute of Scientific and Technical Information of China (English)

    黄元丁; 夏辉; 李晓东; 杨小竺; 裴仲秋; 夏熹

    2011-01-01

    Objective To compare the clinical efficacy of the infiltration anesthesia with primacaine and the nerve blocking anesthesia with lidocaine for microport extraction of impacted lower third molar. Methods 104 chosen patients had both sides of impacted lower third molars extracted in this study. Patients were given local anesthesia with either primacaine or lidocaine randomly at each side, and then underwent microport extraction. Clinical factors including effective proportion (EP), effecting time point (ETP), visual analogue scale of pain (VASp), alteration of systolic pressures (ASP) and analgesia duration (AD) were evaluated statistically by means of paired t-test. Results The EP of experimental group was higher than the control group (P=0.024). The ETP of soft tissue and alveoli-dental pulp was (1.04±0.21), (2.44±2.60)min in the experimental group, and much earlier than that of the control group(P=0.002,P=0.032). The VASp and ASP of experimental group were lower than the control group(P=0.041, P=0.018). AD was (103.6±35.5) min, and higher than the control group (P=0.04). Conclusion The infiltration anesthesia with primacaine has been proven to be a easier, reliable and quick-acting method. We suggest it an alternative method replacing the 2% lidocaine blocking during microport extraction of impacted lower third molar.%目的 比较必兰浸润麻醉与利多卡因阻滞麻醉法在下颌第三磨牙阻生齿微创拔牙术中的疗效.方法 选择双侧阻生齿拔除患者104名,在同一患者双侧下颌分别行必兰浸润麻醉或2%利多卡因阻滞麻醉,并行高速涡轮机微创拔牙,比较2组的麻醉显效率、麻醉显效时间、术中疼痛程度和术前后收缩压差及无痛持续时间,按配对样本t检验法行统计分析.结果 实验组麻醉显效率高于对照组(P=0.024).实验组软组织麻醉显效时间和牙槽突、牙髓麻醉显效时间分别为(1.04±0.21)、(2.44±2.60)min,较对照组均有降低(P=0.002,P=0

  17. Inhalational and local anesthetics reduce tactile and thermal responses in mimosa pudica.

    Science.gov (United States)

    Milne, A; Beamish, T

    1999-03-01

    In reaction to a variety of stimuli, the sensitive plant mimosa pudica closes its leaflets and drops its stems. The objective was to investigate the effects of anaesthetics on the reaction of mimosa pudica to a variety of stimuli. The ability of the plants leaflets to close (n=4, Q5min.) was tested after exposure to halothane 4% and 6L x min(-1) O2, or 6L x min(-1) O2. Lidocaine 2% or vehicle were administered through the roots, cut stems, or sprayed on the leaves (n=4). The test consisted of stimulating the leaves, by burning their tips (lidocaine experiments) or touching them with a metal rod (halothane); the closing of the leaflets, or the lack thereof was then observed. After 15 min exposure to halothane, the mimosas had slow and incomplete reactions to tactile stimulation. Following 20 min exposure, the plants had no visible reaction to touch, a stimulus which would normally cause the collapse of the entire leaf. After one minute, mimosa leaves sprayed with lidocaine had no reaction to a lit match being touched to the tips of the leaves, contrary to the control in which the leaves collapsed completely. After exposure to lidocaine 2% through the roots and cut stems, the mimosa's reactivity gradually decreased; after four hours the leaves were insensitive or had slow reaction to tactile stimuli. Inhalational and local anesthetics inhibited motor mechanisms of the mimosa plant. This may be a model to elucidate the mechanisms of action of anesthetics.

  18. Bupivacaine versus lidocaine analgesia for neonatal circumcision

    Directory of Open Access Journals (Sweden)

    Stolik-Dollberg Orit C

    2005-05-01

    Full Text Available Abstract Background Analgesia for neonatal circumcision was recently advocated for every male infant, and its use is considered essential by the American Academy of Pediatrics. We compared the post-operative analgesic quality of bupivacaine to that of lidocaine for achieving dorsal penile nerve block (DPNB when performing neonatal circumcision. Methods Data were obtained from 38 neonates following neonatal circumcision. The infants had received DPNB analgesia with either lidocaine or bupivacaine. The outcome variable was the administration by the parents of acetaminophen during the ensuing 24 hours. Results Seventeen infants received lidocaine and 19 received bupivacaine DPNB. Ten infants in the lidocaine group (59% were given acetaminophen following circumcision compared to only 3 (16% in the bupivacaine group (P 2 = 20.6; P = 0.006. Conclusion DPNB with bupivacaine for neonatal circumcision apparently confers better analgesia than lidocaine as judged by the requirement of acetaminophen over the ensuing 24-hour period.

  19. Prophylactic lidocaine for myocardial infarction.

    Science.gov (United States)

    Martí-Carvajal, Arturo J; Simancas-Racines, Daniel; Anand, Vidhu; Bangdiwala, Shrikant

    2015-08-21

    Coronary artery disease is a major public health problem affecting both developed and developing countries. Acute coronary syndromes include unstable angina and myocardial infarction with or without ST-segment elevation (electrocardiogram sector is higher than baseline). Ventricular arrhythmia after myocardial infarction is associated with high risk of mortality. The evidence is out of date, and considerable uncertainty remains about the effects of prophylactic use of lidocaine on all-cause mortality, in particular, in patients with suspected myocardial infarction. To determine the clinical effectiveness and safety of prophylactic lidocaine in preventing death among people with myocardial infarction. We searched the Cochrane Central Register of Controlled Trials (CENTRAL) (2015, Issue 3), MEDLINE Ovid (1946 to 13 April 2015), EMBASE (1947 to 13 April 2015) and Latin American Caribbean Health Sciences Literature (LILACS) (1986 to 13 April 2015). We also searched Web of Science (1970 to 13 April 2013) and handsearched the reference lists of included papers. We applied no language restriction in the search. We included randomised controlled trials assessing the effects of prophylactic lidocaine for myocardial infarction. We considered all-cause mortality, cardiac mortality and overall survival at 30 days after myocardial infarction as primary outcomes. We performed study selection, risk of bias assessment and data extraction in duplicate. We estimated risk ratios (RRs) for dichotomous outcomes and measured statistical heterogeneity using I(2). We used a random-effects model and conducted trial sequential analysis. We identified 37 randomised controlled trials involving 11,948 participants. These trials compared lidocaine versus placebo or no intervention, disopyramide, mexiletine, tocainide, propafenone, amiodarone, dimethylammonium chloride, aprindine and pirmenol. Overall, trials were underpowered and had high risk of bias. Ninety-seven per cent of trials (36

  20. INTRAOCULAR PRESSURE, MEAN ARTERIAL BLOOD PRESSURE AND PUPILLARY DIAMETER IN RABBITS ( (Oryctolagus cuniculus SUBJECTED TO RETROBULBAR BLOCK WITH DIFFERENT ANESTHETIC PROTOCOLS

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    Renata Maria Monção da Silva

    2015-10-01

    Full Text Available The aim of this study was to evaluate four protocols of loco regional anesthesia for ophthalmic procedures that could provide safety and life support, in addition to maintain intraocular pressure stable, with eye centralization and eyelid akinesia. 20 New Zealand rabbits were used to perform local anesthesia by retrobulbar block with four protocols: 2% lidocaine with epinephrine, 2% lidocaine without epinephrine associated with tramadol, 1% ropivacaine and bupivacaine 0.5 %. Each animal received an anesthetic volume of 1 mL. All anesthetic protocols used promoted eyelid akinesia and centralization of the eye during the assessment period. The retrobulbar block with the proposed anesthetic protocols proved to be feasible and safe for the maintenance of intraocular pressure, invasive blood pressure and pupillary diameter and can be used in intraocular surgeries, respecting the time of action of each anesthetic. All protocols showed an excellent blockage action but bupivacaine promoted the highest pupil diameter compared to the other drugs tested.

  1. Lidocaine spray alone is similar to spray plus viscous solution for pharyngeal observation during transoral endoscopy: a clinical randomized trial

    Science.gov (United States)

    Hayashi, Tomoyuki; Asahina, Yoshiro; Waseda, Yohei; Kitamura, Kazuya; Kagaya, Takashi; Seike, Takuya; Okada, Kazuhiro; Inada, Yuki; Takabatake, Hisashi; Orita, Noriaki; Yanase, Yuko; Yamashita, Tatsuya; Ninomiya, Itasu; Yoshimura, Kenichi; Kaneko, Shuichi

    2017-01-01

    Background and study aims It is important to examine the pharynx during upper gastrointestinal endoscopy. Pharyngeal anesthesia using topical lidocaine is generally used as pretreatment. In Japan, lidocaine viscous solution is the anesthetic of choice, but lidocaine spray is applied when the former is considered insufficient. However, the relationship between the extent of pharyngeal anesthesia and accuracy of observation is unclear. We compared the performance of lidocaine spray alone versus lidocaine spray combined with lidocaine viscous solution for pharyngeal observation during transoral endoscopy. Patients and methods In this prospective, double-blinded, randomized clinical trial conducted between January and March 2015, 327 patients were randomly assigned to lidocaine spray alone (spray group, n = 157) or a combination of spray and viscous solution (combination group, n = 170). We compared the number of pharyngeal observable sites (non-inferiority test), pain by visual analogue scale, observation time, and the number of gag reflexes between the two groups. Results The mean number of images of suitable quality taken at the observable pharyngeal sites in the spray group was 8.33 (95 % confidence interval [CI]: 7.94 – 8.72) per patient, and 8.77 (95 % CI: 8.49 – 9.05) per patient in the combination group. The difference in the number of observable pharyngeal sites was – 0.44 (95 % CI: – 0.84 to – 0.03, P = 0.01). There were no differences in pain, observation time, or number of gag reflexes between the 2 groups. Subgroup analysis of the presence of sedation revealed no differences between the two groups for the number of pharyngeal observation sites and the number of gag reflexes. However, the number of gag reflexes was higher in the spray group compared to the combination group in a subgroup analysis that looked at the absence of sedation. Conclusions Lidocaine spray for pharyngeal anesthesia was not

  2. Brain activation by short-term nicotine exposure in anesthetized wild-type and beta2-nicotinic receptors knockout mice: a BOLD fMRI study

    Energy Technology Data Exchange (ETDEWEB)

    Suarez, S.V.; Changeux, J.P.; Granon, S. [Unite de Neurobiologie Integrative du Systeme Cholinergique, URA CNRS 2182, Institut Pasteur, Departement de Neuroscience, 25 rue du Dr Roux, 75015 Paris (France); Amadon, A.; Giacomini, E.; Le Bihan, D. [Service Hospitalier Frederic Joliot, 4 place du general Leclerc, 91400 Orsay (France); Wiklund, A. [Section of Anaesthesiology and Intensive Care Medicine, Department of Physiology and Pharmacology, Karolinska Institutet, Stockholm (Sweden)

    2009-07-01

    Rationale: The behavioral effects of nicotine and the role of the beta2-containing nicotinic receptors in these behaviors are well documented. However, the behaviors altered by nicotine rely on the functioning on multiple brain circuits where the high-affinity {beta}2-containing nicotinic receptors ({beta}2*nAChRs) are located. Objectives We intend to see which brain circuits are activated when nicotine is given in animals naive for nicotine and whether the {beta}2*nAChRs are needed for its activation of the blood oxygen level dependent (BOLD) signal in all brain areas. Materials and methods: We used functional magnetic resonance imaging (fMRI) to measure the brain activation evoked by nicotine (1 mg/kg delivered at a slow rate for 45 min) in anesthetized C57BL/6J mice and {beta}2 knockout (KO) mice. Results: Acute nicotine injection results in a significant increased activation in anterior frontal, motor, and somatosensory cortices and in the ventral tegmental area and the substantia nigra. Anesthetized mice receiving no nicotine injection exhibited a major decreased activation in all cortical and subcortical structures, likely due to prolonged anesthesia. At a global level, {beta}2 KO mice were not rescued from the globally declining BOLD signal. However, nicotine still activated regions of a meso-cortico-limbic circuit likely via {alpha}7 nicotinic receptors. Conclusions: Acute nicotine exposure compensates for the drop in brain activation due to anesthesia through the meso-cortico-limbic network via the action of nicotine on {beta}2*nAChRs. The developed fMRI method is suitable for comparing responses in wild-type and mutant mice. (authors)

  3. Prevalence of hypersensitivity to dental local anesthetic drugs in patients referred to Tehran Allergy clinic (2005-2007

    Directory of Open Access Journals (Sweden)

    Akhlaghi F.

    2009-03-01

    Full Text Available "nBackground and Aim: According to controversies in the prevalence of hypersensitivity to dental local anesthetic drugs and patients who claim hypersensitivity to these drugs, the aim of this study was to determine the prevalence of hypersensitivity to dental amide local anesthetic drugs in patients referred to Tehran Allergy Clinic in 2005-2007. "nMaterials and Methods: In this Study (Review of existing data, records of 130 patients who were referred to "Tehran allergy Clinic" (2005-2007 were studied. "nResults: The average age of patients was 29.5±18.8 years. 34% of cases showed positive skin reactions to at least one of the tested Lidocain concentrations and 10% of cases showed positive skin reactions to at least one of the tested Prilocain concentrations. There was a statistically significant difference in hypersensitivity to Lidocain 0.01 and 0.001 (p=0.017 and also between Lidocain 0.001 and 0.0001 (p<0.01. There was no statistically significant difference between other tested drug concentrations (p>0.05. "nConclusion: Many patients with history of hypersensitivity, show positive reaction to local dental anesthetic drugs. Prilocain hypersensitivity reactions are less than Lidocain. So application of Prilocain accompanies with less risk but its application should not be considered completely safe.

  4. Skin biopsy and quantitative sensory testing do not predict response to lidocaine patch in painful neuropathies.

    Science.gov (United States)

    Herrmann, David N; Pannoni, Valerie; Barbano, Richard L; Pennella-Vaughan, Janet; Dworkin, Robert H

    2006-01-01

    Predictors of response to neuropathic pain treatment in patients with painful distal sensory neuropathies are lacking. The 5% lidocaine patch is believed to exert its effects on neuropathic pain via a local stabilizing effect on cutaneous sensory afferents. As such, it provides a model to assess whether the status of epidermal innervation as determined by skin biopsy or quantitative sensory testing (QST) of small- and large-diameter sensory afferents might serve as predictors of response to topical, locally active treatment. In this study we assessed associations between epidermal nerve fiber (ENF) densities, sensory nerve conduction studies (NCS), QST, and response to a 5% lidocaine patch in patients with painful distal sensory neuropathies. We observed no association between distal leg epidermal and subepidermal innervation and response to the lidocaine patch. Several patients with complete loss of distal leg ENF showed a response to the lidocaine patch. Similarly we observed no consistent association between treatment response and QST for vibration, cooling, warm, heat-pain, and cold-pain thresholds, or distal sensory NCS. Thus, distal-leg skin biopsy, QST, and sensory NCS cannot be used to identify patients with painful polyneuropathy likely to respond to a lidocaine patch in clinical practice. Further studies are required to clarify precisely the mechanism and site of action of the lidocaine patch in patients with peripheral neuropathic pain.

  5. Anesthetizing the obese child

    DEFF Research Database (Denmark)

    Mortensen, Anette; Lenz, Katja; Abildstrøm, Hanne

    2011-01-01

    The prevalence of childhood obesity is increasing. The focus of this review is the special anesthetic considerations regarding the perioperative management of obese children. With obesity the risk of comorbidity such as asthma, obstructive sleep apnea, hypertension, and diabetes increases....... The obese child has an increased risk of perioperative complications especially related to airway management and ventilation. There is a significantly increased risk of difficult mask ventilation and perioperative desaturation. Furthermore, obesity has an impact on the pharmacokinetics of most anesthetic...

  6. Analgesic effects of adding lidocaine to morphine pumps after orthopedic surgeries

    Directory of Open Access Journals (Sweden)

    Mahmoud Reza Alebouyeh

    2014-01-01

    Full Text Available Background: Opiate is used in patient-controlled intravenous analgesia pumps (PCIA for controlling pain in post-surgical patients. Other drugs are remarkably added to opioid pumps to enhance quality, lengthen analgesia, and reduce side effects. Lidocaine, a local anesthetic which inhibits sodium channels, has anesthetic and analgesic effects when injected locally or intravenously. The objective of this study is to evaluate the analgesic effects of adding lidocaine 1% to different doses of morphine via IV pump to patient-controlled analgesia (PCA after orthopedic surgeries. Materials and Methods: In a randomized clinical trial, 60 patients who had undergone orthopedic surgery of lower extremities were divided into three equal groups to control postoperative pain. Intravenous pump with 5 ml/h flow rate was used as the analgesic method. The solution consisted of lidocaine 1% plus 20 mg morphine for the first group, lidocaine 1% plus 10 mg morphine for the second group, and only 20 mg morphine for the third group (control group. Patients were checked every 12 h, and Visual Analog Scale (VAS, extra opioid doses, nausea/vomiting, and sedation scale were examined. Results: Pain score was lower in the first group compared to the other two groups. Mean VAS was 2.15 ± 0.2, 2.75 ± 0.2, and 2 ± 0.25 on the first day and 1.88 ± 0.1, 2.74 ± 0.3, and 2.40 ± 0.3 on the second day, respectively, in the three groups and the difference was statistically significant (P < 0.01 and <0.05, respectively. Also, 10% of patients in the first group needed extra opioid doses, while this figure was 30% in the second group and 25% in the third group (P < 0.01. Nausea/vomiting and sedation scores were not statistically different among the three groups. Conclusion: Compared to lidocaine 1% plus 10 mg morphine or 20 mg morphine alone in PCIA, adding lidocaine 1% to 20 mg morphine decreases the pain score and opioid dose after orthopedic surgeries without having side

  7. Adding metoclopramide to lidocaine for intravenous regional anesthesia in trauma patients

    Directory of Open Access Journals (Sweden)

    Mohammadreza Safavi

    2014-01-01

    Full Text Available Background: Metoclopromide have local anesthetic properties. The main object of performing the present study was to evaluate the analgesic effect of metoclopromide 10 mg when added to lidocaine for intravenous regional anesthesia (IVRA of upper extremities in trauma patients. Materials and Methods: Ninety patients undergoing upper limb producer were randomly allocated to the three groups to receive 3 mg/kg 2% lidocaine diluted with saline to a total dose of 40 ml (Group L, n = 30 or 10 mg metoclopromide plus 3 mg/kg 2% lidocaine diluted with saline to a total dose of 40 ml (group LM, n = 30 or 3 mg/kg 2% lidocaine diluted with saline to a total dose of 40 ml plus 10 mg metoclopromide intravenously (Group IM, n = 30. Results: Our study showed that the onset times for sensory and motor block were significantly shorter in Group LM compared with Group L and Group IM (4.5 ± 0.7 vs. 5.0 ± 0.7 and 5.0 ± 0.6, respectively, P = 0.006 for sensory block; 6.3 ± 0.7 vs. 5.1 ± 0.9 and 5.9 ± 0.6 respectively, P = 0.000 for motor block. The postoperative VAS scores were significantly less at 1, 5, 10, 15, and 30 minutes after tourniquet release in Group LM compared with Group L and Group IM ( P < 0.05. Conclusion: The results of our study showed that adding 10 mg metoclopromide to lidocaine for IVRG in trauma patients reduced intraoperative and postoperative analgesic use till 24 hours and improve quality of anesthesia.

  8. Ropivacaine plus lidocaine versus Bupivacaine plus lidocaine for peribulbar double injection regional anesthesia

    OpenAIRE

    Omar Elsafty MD, Ahmed M.S. Hamed MD, Sherif Wadie MD

    2003-01-01

    Our study was designed to evaluate the efficacy of Ropivacaine 0.75% plus Lidocaine 2% versus Bupivacaine 0.5 % plus lidocaine 2 % to provide peribulbar anaesthesia for cataract surgery .Time to adequate block for surgery, ocular eyelid movement scores at 8 min after block and quality for postoperative analgesia were recorded. Sixty patients are randomly divided into two groups of 30, to receive a peribulbar block with 8 ­ 10 ml of either Ropivacaine ­ Lidocaine or Bupivacaine ­ lidocaine,and...

  9. Scientometrics of anesthetic drugs and their techniques of administration, 1984–2013

    Directory of Open Access Journals (Sweden)

    Vlassakov KV

    2014-12-01

    Full Text Available Kamen V Vlassakov, Igor Kissin Department of Anesthesiology, Perioperative and Pain Medicine, Brigham and Women’s Hospital, Harvard Medical School, Boston, MA, USA Abstract: The aim of this study was to assess progress in the field of anesthetic drugs over the past 30 years using scientometric indices: popularity indices (general and specific, representing the proportion of articles on a drug relative to all articles in the field of anesthetics (general index or the subfield of a specific class of anesthetics (specific index; index of change, representing the degree of growth in publications on a topic from one period to the next; index of expectations, representing the ratio of the number of articles on a topic in the top 20 journals relative to the number of articles in all (>5,000 biomedical journals covered by PubMed; and index of ultimate success, representing a publication outcome when a new drug takes the place of a common drug previously used for the same purpose. Publications on 58 topics were assessed during six 5-year periods from 1984 to 2013. Our analysis showed that during 2009–2013, out of seven anesthetics with a high general popularity index (≥2.0, only two were introduced after 1980, ie, the inhaled anesthetic sevoflurane and the local anesthetic ropivacaine; however, only sevoflurane had a high index of expectations (12.1. Among anesthetic adjuncts, in 2009–2013, only one agent, sugammadex, had both an extremely high index of change (>100 and a high index of expectations (25.0, reflecting the novelty of its mechanism of action. The index of ultimate success was positive with three anesthetics, ie, lidocaine, isoflurane, and propofol, all of which were introduced much longer than 30 years ago. For the past 30 years, there were no new anesthetics that have produced changes in scientometric indices indicating real progress. Keywords: anesthetics, anesthetic adjuvants, mortality, safety margins, therapeutic indices

  10. Comparison of the Analgesic Efficacy of Lidocaine/Prilocaine (EMLA Cream and Needle-Free Delivery of Lidocaine During Fine-Needle Aspiration Biopsy of Thyroid Nodules

    Directory of Open Access Journals (Sweden)

    Alptekin Gürsoy

    2009-06-01

    Full Text Available Objective: Efficacy of eutectic mixture of local anesthetic (EMLA cream and the needle-free injection of local anesthesia for reducing pain associated with fine-needle aspiration biopsy (FNAB of thyroid nodules has been previously reported. However, there has not been a direct comparison of the analgesic efficacy of these methods. The aim of this study was to compare the analgesic efficacy of EMLA cream and needle-free injection of lidocaine for FNAB-associated pain. Materials and Methods: A total of 138 patients having their first ultrasonography-guided thyroid nodule biopsy were randomly assigned to receive either EMLA cream (n=68 or needle-free injection of lidocaine (n=70 before FNAB of thyroid nodules. Four needle passes for biopsy of each nodule were performed. Patients rated pain associated with the procedure according to a 100-mm visual analog scale (VAS, an 11-point numeric rating scale (NRS, and 4-category verbal rating scale (VRS. Results: There were no significant differences between groups in age, sex, thyroid volume, nodule size, or nodule site. Significant differences between groups were noted in ratings of all three pain scales. When the effectiveness of EMLA was compared with that of needle-free injection of lidocaine, the mean VAS score was 23.4±20.5 mm versus 12.7±15.5 mm (p=0.001, and the mean NRS score was 2.8±2.1 points versus 1.6±1.7 points (p<0.001. There was also a significant difference between groups in VRS score (p=0.001. Conclusions: Needle-free injection of lidocaine provides more effective and faster analgesia than EMLA cream application during the FNAB. Turk Jem 2009; 13: 5-7

  11. Comparison of orbital muscle akinesia caused by rocuronium versus hyaluronidase mixed to the local anesthetic in single injection peribulbar block for cataract surgery

    Science.gov (United States)

    Messeha, Medhat M.; Elhesy, Abd-Elmonem

    2015-01-01

    Background: The aim of this study was to compare orbital muscle akinesia caused by rocuronium versus hyaluronidase when mixed with the local anesthetic in single-injection peribulbar anesthesia (PBA). Patients and Methods: Sixty patients were included in the study and subjected to cataract extraction using phacoemulsification technique with intraocular lens implantation. Group I received peribulbar block with 5 ml mixture of 30 IU/ml hyaluronidase and 2% lidocaine. Group II received peribulbar block with 5 ml mixture of rocuronium 5 mg and 2% lidocaine. The onset and duration of akinesia were assessed; the akinesia score at 2, 5, and 10 min was measured after injection. The need for supplementary injection was also recorded. Results and Conclusion: PBA using a mixture of rocuronium and lidocaine provides optimal globe akinesia and faster establishment of suitable conditions to start eye surgery and shortens the block onset time as compared with the addition of hyaluronidase to lidocaine. PMID:26712977

  12. Juvéderm Volbella with Lidocaine for Lip and Perioral Enhancement: A Prospective, Randomized, Controlled Trial

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    Hervé Raspaldo, MD

    2015-03-01

    Conclusions: Juvéderm Volbella with Lidocaine is effective for lip enhancement, improves perioral lines and oral commissures, and results in less short-term swelling and disruption in daily activities than Restylane-L.

  13. Biphasic drug absorption from the epidural space of the dog may limit the utility of a slow release medium molecular weight hyaluronic acid-lidocaine ionic complex formulation.

    Science.gov (United States)

    Doherty, M M; Hughes, P J; Charman, S A; Brock, K V; Korszniak, N V; Charman, W N

    1996-12-01

    Previous epidural studies conducted in rabbits have described a viscous lidocaine-hyaluronate formulation (L-HA) that prolonged the duration of sensory blockade twofold and decreased the rate of drug absorption fourfold relative to a solution formulation. As further evaluation of the L-HA formulation required studies in a larger animal that more closely reflected the characteristic absorption kinetics observed in humans, a conscious dog model was used to functionally and kinetically evaluate the viscous formulation relative to lidocaine solution. In terms of the measured pharmacodynamic end point (loss of weight-bearing ability in hind legs), epidural administration of the L-HA formulation did not prolong the duration of action relative to lidocaine solution in spite of a markedly altered pharmacokinetic profile. For example, administration of L-HA reduced the mean plasma lidocaine Cmax value approximately 50% and increased the Tmax value approximately fivefold relative to lidocaine solution. However, the viscous L-HA formulation did cause a significant prolongation in the latency of onset (P lidocaine solution. The dog exhibited "flip-flop" pharmacokinetics and absorption was biphasic after epidural administration of lidocaine solution (apparent t1/2 of the fast and slow absorption phases were 4 min and 131 min, respectively). The L-HA formulation markedly altered the absorption kinetics such that a single, slow absorption phase was evident (apparent t1/2 of 56 min), although this rate was more rapid than the slow phase observed after lidocaine solution. It is possible that the inability of the hyaluronate-based formulation to further reduce the magnitude of the slow absorption phase resulted in the failure to prolong the duration of action. These data highlight the need to carefully consider the absorption kinetics and pharmacokinetic characteristics of the animal models chosen to evaluate new formulation of epidurally administered local anesthetics.

  14. Effect of Lidocaine and Amiodarone on Transmural Heterogeneityricular Repolarization in Isolated Rabbit Hearts Model of Sustained Global Ischemia

    Institute of Scientific and Technical Information of China (English)

    YOU Binquan; PU Jun; LIU Nian; YU Ronghui; RUAN Yanfei; LI Yang; WANG Lin

    2005-01-01

    To study the effect of of lidocaine and amiodarone on the transmural heterogeneity of ventricular repolarization in isolated rabbit hearts model of sustained global ischemia and to explore the mechanisms underlying the antiarrhythmic activity of lidocaine and amiodarone, rabbits were randomly divided into 4 groups: control group, ischemia group, lidocaine group and amiodarone group. By the monophasic action potential (MAP) recording technique, MAPs of recorded across the left ventricular free wall in rabbit hearts perfused transmural dispersion of repolarization (TDR) and arrhythmic induced by ischemia. Our results showed that TDR of three myocardial layers in ischemia group were significantly lengthened after ischemia. TDR was increased from 17.5±3.9 ms to 31.2±4.6 ms at the time that concided with the onset of sustained ventricle arrhythmic. Amiodarone could decrease TDR, but lidocaine could increase TDR at initial ischemia, and no significant difference was found at other ischemia time points. 5 cases had ventriclar arrhythmia in ischemia group (62.5 %), but no case in lidocaine group (P<0.01) and only 1 case in amiodarone group had ventrilar arrhythmia (P< 0.01). No significant difference was found between amiodarone group and lidocaine group. It is concluded that TDR of of three myocardial layers increases significantly at ischemia and it is closely associated with development of ventricular arrhythmia, and amiodarone could decrease TDR, but lidocaine could increase TDR at initial ischemia and has no effects at other ischemia time points.

  15. Relapse of Neuromyelitis Optica Spectrum Disorder Associated with Intravenous Lidocaine

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    Akiyuki Uzawa

    2011-01-01

    Full Text Available Lidocaine unmasks silent symptoms and eases neuropathic pain in multiple sclerosis patients; however, the effects of lidocaine in neuromyelitis optica have never been reported. We describe the case of a 59-year-old Japanese woman with neuromyelitis optica spectrum disorder who developed optic neuritis 1 day after intravenous lidocaine injection for treating allodynia. Her symptom seemed to result from a relapse of neuromyelitis optica induced by lidocaine administration, and not because of the transient effects of intravenous lidocaine administration. The possibility that lidocaine administration results in relapse of neuromyelitis optica due to its immunomodulating effects cannot be ruled out.

  16. Comparison of the efficacy and safety of 2% lidocaine HCl with different epinephrine concentration for local anesthesia in participants undergoing surgical extraction of impacted mandibular third molars: A multicenter, randomized, double-blind, crossover, phase IV trial.

    Science.gov (United States)

    Karm, Myong-Hwan; Park, Fiona Daye; Kang, Moonkyu; Kim, Hyun Jeong; Kang, Jeong Wan; Kim, Seungoh; Kim, Yong-Deok; Kim, Cheul-Hong; Seo, Kwang-Suk; Kwon, Kyung-Hwan; Kim, Chul-Hwan; Lee, Jung-Woo; Hong, Sung-Woon; Lim, Mi Hyoung; Nam, Seung Kwan; Cho, Jae Min

    2017-05-01

    The most commonly impacted tooth is the third molar. An impacted third molar can ultimately cause acute pain, infection, tumors, cysts, caries, periodontal disease, and loss of adjacent teeth. Local anesthesia is employed for removing the third molar. This study aimed to evaluate the efficacy and safety of 2% lidocaine with 1:80,000 or 1:200,000 epinephrine for surgical extraction of bilateral impacted mandibular third molars. Sixty-five healthy participants underwent surgical extraction of bilateral impacted mandibular third molars in 2 separate visits while under local anesthesia with 2% lidocaine with different epinephrine concentration (1:80,000 or 1:200,000) in a double-blind, randomized, crossover trial. Visual analog scale pain scores obtained immediately after surgical extraction were primarily evaluated for the 2 groups receiving different epinephrine concentrations. Visual analog scale pain scores were obtained 2, 4, and 6 hours after administering an anesthetic. Onset and duration of analgesia, onset of pain, intraoperative bleeding, operator's and participant's overall satisfaction, drug dosage, and hemodynamic parameters were evaluated for the 2 groups. There were no statistically significant differences between the 2 groups in any measurements except hemodynamic factors (P >.05). Changes in systolic blood pressure and heart rate following anesthetic administration were significantly greater in the group receiving 1:80,000 epinephrine than in that receiving 1:200,000 epinephrine (P ≤.01). The difference in epinephrine concentration between 1:80,000 and 1:200,000 in 2% lidocaine liquid does not affect the medical efficacy of the anesthetic. Furthermore, 2% lidocaine with 1:200,000 epinephrine has better safety with regard to hemodynamic parameters than 2% lidocaine with 1:80,000 epinephrine. Therefore, we suggest using 2% lidocaine with 1:200,000 epinephrine rather than 2% lidocaine with 1:80,000 epinephrine for surgical extraction of impacted

  17. [Delayed convulsion after lidocaine instillation for bronchoscopy].

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    Gaïes, E; Jebabli, N; Lakhal, M; Klouz, A; Salouage, I; Trabelsi, S

    2016-05-01

    Lidocaine toxicity usually appears rapidly and is directly correlated with plasma concentrations of the drug. We report a case of a late neurologic toxicity occurring after instillation of lidocaine during fibre-optic bronchoscopy. A patient with bronchiolitis obliterans underwent a diagnostic bronchoscopy. She received multiples instillations of Xylocaine(®) 2% (lidocaine). Three and a half hours later, she had a tonic-clonic seizure. Seven hours later, this recurred. Lidocaine plasma levels were in the toxic range at the time of the first seizure (18.32μg/mL) with a significant decrease in the concentration noted 24hours later. The slow absorption of lidocaine into the blood from the bronchial tree explains the delayed neurologic toxicity. Our observation is a reminder that complications can occur due to high doses of lidocaïne administrated by instillation. Thus, if the recommended dose of lidocaine is exceeded, it is essential to monitor patients closely for a prolonged period, especially those with fibrosing lung disease in order to avoid possible late toxicity. Copyright © 2015 SPLF. Published by Elsevier Masson SAS. All rights reserved.

  18. Evaluation of prilocaine for the reduction of pain associated with transmucosal anesthetic administration.

    Science.gov (United States)

    Kramp, L. F.; Eleazer, P. D.; Scheetz, J. P.

    1999-01-01

    This investigation evaluated the use and efficacy of prilocaine HCl (4% plain Citanest) for minimizing pain associated with the intraoral administration of local anesthesia. Clinical anecdotes support the hypothesis that prilocaine without a vasoconstrictor reduces pain during injection. To determine relative injection discomfort, use of 4% plain prilocaine was compared with use of 2% lidocaine with 1:100,000 epinephrine and 2% mepivacaine with 1:20,000 levonordefrin. Prior to routine endodontic procedures, 150 adult patients received 0.3 to 1.8 mL of local anesthetic via the same gauge needle without the use of a topical local anesthetic. Injection methods included buccal infiltration, labial infiltration, palatal infiltration, and inferior alveolar nerve block. Following each injection, patients were asked to describe the level of discomfort by scoring on a visual analog scale of 1 to 10, where 1 = painless and 10 = severe pain. Analyses via 2-way analysis of variance revealed no interaction between anesthetic and site of injection. However, there were statistically significant differences among the injection sites. Post hoc analysis revealed that prilocaine was associated with significantly less pain perception when compared to mepivacaine and lidocaine. These results suggest that differences in initial pain perception during transmucosal injection may be a function of the local anesthetic use, and prilocaine can produce less discomfort than the others tested. Images Figure 1 PMID:10853565

  19. Risk of acquired methemoglobinemia with different topical anesthetics during endoscopic procedures

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    Vallurupalli S

    2011-07-01

    Full Text Available Srikanth Vallurupalli1, Shalini Manchanda21Division of General Internal Medicine, Department of Medicine, Southern Illinois University School of Medicine, Springfield, IL, USA; 2Division of Pulmonary, Allergy, Critical Care, and Occupational Medicine, Department of Medicine, Indiana University School of Medicine, Indianapolis, IN, USAIntroduction: Methemoglobinemia is a recognized complication of the use of topical anesthetic sprays. The true scope of the problem or the risk with different topical anesthetic sprays and endoscopic procedures is unknown.Methods: We retrospectively identified all cases of methemoglobinemia that occurred in a university affiliated community hospital from 2001 to 2007.Results: Eleven cases of methemoglobinemia were identified over the 6-year period. Nine (82% occurred with use of benzocaine spray during transesophageal echocardiography (TEE. Patients who developed methemoglobinemia secondary to the topical anesthetic spray compared to other causes were more likely to be older, have lower mean hemoglobin levels (10.5 ± 0.5 g/dL vs 11.3 ± 0.0 g/dL, and a higher mean methemoglobin concentration at diagnosis (40.8% ± 5.2% vs 24% ± 10%. However, only age reached statistical significance (P = 0.004.Conclusion: In a university-affiliated community hospital, topical anesthetic sprays account for most of the burden of methemoglobinemia. Benzocaine use in the context of TEE caused more methemoglobinemia compared to lidocaine and other endoscopic procedures. This observation supports previous data and findings deserve further study.Keywords: methemoglobinemia, benzocaine, lidocaine, transesophageal echocardiography, endoscopy

  20. Sedative and anesthetic activities of the essential oils of Hyptis mutabilis (Rich. Briq. and their isolated components in silver catfish (Rhamdia quelen

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    L.L. Silva

    2013-09-01

    Full Text Available This study evaluated the sedative and anesthetic effects of the essential oils (EO of Hyptis mutabilis (Rich. Briq. and their isolated components on silver catfish (Rhamdia quelen. Quantitative chemical differences between the EOs obtained from leaves and inflorescences were verified, and a new chemotype rich in globulol was described. Although there were no significant differences in the time of induction for sedation and anesthesia between the EOs, only the leaf EO at 344 mg/L anesthetized all fish without side effects. Fractionation of the leaf EO was carried out by column chromatography. The isolated compounds [(+-1-terpinen-4-ol and (--globulol] showed different activity from that detected for the leaf EO in proportional concentrations and similar sedation to a eugenol control at 10 mg/L. However, fish exposed to 1-terpinen-4-ol (3 and 10 mg/L did not remain sedated for 30 min. Anesthesia was obtained with 83-190 mg/L globulol, but animals showed loss of mucus during induction and mortality at these concentrations. Synergism of the depressor effects was detected with the association of globulol and benzodiazepine (BDZ, compared with either drug alone. Fish exposed to BDZ or globulol+BDZ association showed faster recovery from anesthesia in water containing flumazenil, but the same did not occur with globulol. In conclusion, the use of globulol in aquaculture procedures should be considered only at sedative concentrations of 10 and 20 mg/L, and its mechanism of action seems not to involve the GABAA-BDZ system.

  1. Effect of topical lidocaine in the oral and facial regions on tactile sensory and pain thresholds.

    Science.gov (United States)

    Okayasu, Ichiro; Komiyama, Osamu; Ayuse, Takao; De Laat, Antoon

    2016-12-01

    The aim of the present study was to examine the effect of lidocaine application to the face, tongue and hand on sensory and pain thresholds of symptom-free subjects. Eighteen females (mean age 25.7 years, range 22-38) participated. Using Semmes-Weinstein monofilaments, the tactile detection threshold (TDT) and the filament-prick pain detection threshold (FPT) were measured on the cheek skin (CS), tongue tip (TT) and palm side of the thenar skin (TS). Subjects were tested in 2 sessions at a 1week interval in randomised order. Lidocaine (session A) or placebo gel (session B) was applied for 5min. The TDT and FPT were measured before and after application. The TDT at all sites in session A significantly increased after 5min, but a significant session effect on the TDT was only found at the TT (Pthreshold (FPT) is more susceptible to local anesthetics than the sensory threshold (TDT), but further study is needed to use topical lidocaine for the control of oral and facial pain in the clinic. Copyright © 2016 Elsevier Ltd. All rights reserved.

  2. Effect of Duration and Amplitude of Direct Current when Lidocaine Is Delivered by Iontophoresis

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    Ethan N. Saliba

    2011-12-01

    Full Text Available Dosage for the galvanic stimulation for iontophoresis varies. Clinicians manipulate the duration or the amplitude of the current, but it is not known which is more effective. We compared the anesthetic effect of lidocaine HCL (2% by manipulating the current parameters on 21 healthy volunteers (age: 21.2 ± 4.2, height 170.7 ± 10.2 cm, mass 82.1 ± 19.2 kg. Three conditions were administered in a random order using a Phoresor II® with 2 mL, 2% lidocaine HCL in an iontophoresis electrode. (1 HASD (40 mA*min: High amplitude (4 mA, short duration (10 min; (2 LALD (40 mA.min: Low amplitude (2 mA, long duration (20 min; (3 Sham condition (0 mA, 20 min. Semmes-Weinstein monofilament (SWM scores were taken pre and post intervention to measure sensation changes. Two-way ANOVA with repeated measures was used to compare sensation. Both iontophoresis treatments: LALD (4.2 ± 0.32 mm and HASD (4.2 ± 0.52 mm significantly increased SWM scores, indicating an increase in anesthesia, compared to the sham condition (3.6 ± 0.06 mm p < 0.05. Neither LALD nor HASD was more effective and there was no difference in anesthesia with the sham. Lidocaine delivered via iontophoresis reduces cutaneous sensation. However, there was no benefit in either a HASD or LALD treatment.

  3. Effectiveness of various formulations of local anesthetics and additives for topical anesthesia – a prospective, randomized, double-blind, placebo-controlled study

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    Weilbach C

    2017-05-01

    Full Text Available Christian Weilbach,1 Christian Hoppe,2 Matthias Karst,3 Michael Winterhalter,4 Konstantinos Raymondos,3 Arthur Schultz,3 Niels Rahe-Meyer2 1Department of Anesthesiology, Intensive Care, Emergency Medicine and Pain Therapy, St. Josefs-Hospital Cloppenburg, Cloppenburg, 2Clinic for Anesthesiology and Operational Intensive Care, Franziskus Hospital Bielefeld, Bielefeld, 3Clinic for Anesthesiology and Intensive Care, Medizinische Hochschule Hannover, Hannover, 4Clinic for Anesthesiology and Pain Therapy, Klinikum Bremen-Mitte, Bremen, Germany Background: Topical anesthesia is used to control pain associated with many procedures in medicine. Today, the product most commonly applied for topical anesthesia in Germany is EMLA® (lidocaine/prilocaine. However, since prilocaine is a methemoglobin-inducing agent, there are limitations to its use, especially in neonates and infants. The aim of this study was to evaluate the effect of prilocaine and lidocaine as well as propylene glycol, a penetration enhancer, and trometamol, a buffer substance, in anesthetic creams.Patients and methods: Twenty-nine healthy adults participated in this study. Standardized creams with eight different compositions were applied and left for 20, 40 or 60 min. After exposure to standardized painful stimuli (blunt/sharp with pressures of 0.2, 0.4 or 0.8 N, subjects rated the experimental pain using a visual analog scale.Results: Significant results were only found with an exposure time of 60 min and a stamp pressure of 0.8 N. At a concentration of 20%, lidocaine was more effective compared to placebo and equally effective compared to lidocaine/prilocaine in controlling pain. The analgesic effect of the cream containing lidocaine 10% and additional trometamol was significantly superior to that of placebo and non-inferior to that of lidocaine/prilocaine. In this study, the penetration enhancer propylene glycol did not accelerate the onset of the analgesic effect. In contrast

  4. Diminished brain synaptic plasma membrane Ca(2+)-ATPase activity in rats with streptozocin-induced diabetes: association with reduced anesthetic requirements.

    Science.gov (United States)

    Janicki, P K; Horn, J L; Singh, G; Franks, W T; Franks, J J

    1994-01-01

    Recent evidence suggests that chronic hyperglycemia may inhibit plasma membrane Ca(2+)-ATPase (PMCA) in cells from several tissues. Inhalational anesthetics (IA) can inhibit brain synaptic PMCA activity. We proposed that diabetic rats may manifest chronic inhibition of brain synaptic PMCA and thus provide a model for testing the hypothesis that synaptic PMCA plays a key role in IA pharmacodynamics. Ca2+ pumping activity of PMCA was measured in cerebral synaptic plasma membrane (SPM) vesicles prepared from rats with streptozocin (STZ)-induced diabetes and from control, normoglycemic rats. Dose requirements for halothane and xenon were estimated in treated and untreated rats. Brain PMCA activity in hyperglycemic rats was depressed by about 8.4%, compared to controls. In vitro glycation also caused a significant decrease in PMCA pumping activity. Halothane requirement for STZ-hyperglycemic rats was dramatically reduced to about 65% of control. Xenon requirement was also significantly reduced, to 88% of control. Correlation of IA dose with percent glycated hemoglobin for each rat revealed a strong association between reduced requirements for halothane or xenon and increased protein glycation. These results indicate that inhibition of brain synaptic PMCA in chronically hyperglycemic rats is associated with a significant reduction in IA requirement.

  5. Lidocaine concentration in mandibular bone after subperiosteal infiltration anesthesia decreases with elevation of periosteal flap and irrigation with saline.

    Science.gov (United States)

    Ogawa, Sachie; Watanabe, Masahiro; Kawaai, Hiroyoshi; Tada, Hitoshi; Yamazaki, Shinya

    2014-01-01

    It has been reported that the action of infiltration anesthesia on the jawbone is attenuated significantly by elevation of the periosteal flap with saline irrigation in clinical studies; however, the reason is unclear. Therefore, the lidocaine concentration in mandibular bone after subperiosteal infiltration anesthesia was measured under several surgical conditions. The subjects were 48 rabbits. Infiltration anesthesia by 0.5 mL of 2% lidocaine with 1 : 80,000 epinephrine (adrenaline) was injected into the right mandibular angle and left mandibular body, respectively. Under several surgical conditions (presence or absence of periosteal flap, and presence or absence of saline irrigation), both mandibular bone samples were removed at a fixed time after subperiosteal infiltration anesthesia. The lidocaine concentration in each mandibular bone sample was measured by high-performance liquid chromatography. As a result, elevation of the periosteal flap with saline irrigation significantly decreased the lidocaine concentration in the mandibular bone. It is suggested that the anesthetic in the bone was washed out by saline irrigation. Therefore, supplemental conduction and/or general anesthesia should be utilized for long operations that include elevation of the periosteal flap with saline irrigation.

  6. Lidocaine Concentration in Mandibular Bone After Subperiosteal Infiltration Anesthesia Decreases With Elevation of Periosteal Flap and Irrigation With Saline

    Science.gov (United States)

    Ogawa, Sachie; Watanabe, Masahiro; Kawaai, Hiroyoshi; Tada, Hitoshi; Yamazaki, Shinya

    2014-01-01

    It has been reported that the action of infiltration anesthesia on the jawbone is attenuated significantly by elevation of the periosteal flap with saline irrigation in clinical studies; however, the reason is unclear. Therefore, the lidocaine concentration in mandibular bone after subperiosteal infiltration anesthesia was measured under several surgical conditions. The subjects were 48 rabbits. Infiltration anesthesia by 0.5 mL of 2% lidocaine with 1 : 80,000 epinephrine (adrenaline) was injected into the right mandibular angle and left mandibular body, respectively. Under several surgical conditions (presence or absence of periosteal flap, and presence or absence of saline irrigation), both mandibular bone samples were removed at a fixed time after subperiosteal infiltration anesthesia. The lidocaine concentration in each mandibular bone sample was measured by high-performance liquid chromatography. As a result, elevation of the periosteal flap with saline irrigation significantly decreased the lidocaine concentration in the mandibular bone. It is suggested that the anesthetic in the bone was washed out by saline irrigation. Therefore, supplemental conduction and/or general anesthesia should be utilized for long operations that include elevation of the periosteal flap with saline irrigation. PMID:24932978

  7. Xyloglucan Based In Situ Gel of Lidocaine HCl for the Treatment of Periodontosis

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    Ashlesha P. Pandit

    2016-01-01

    Full Text Available The present study was aimed at formulating thermoreversible in situ gel of local anesthetic by using xyloglucan based mucoadhesive tamarind seed polysaccharide (TSP into periodontal pocket. Temperature-sensitive in situ gel of lidocaine hydrochloride (LH (2% w/v was formulated by cold method. A full 32 factorial design was employed to study the effect of independent variables concentrations of Lutrol F127 and TSP to optimize in situ gel. The dependent variables evaluated were gelation temperature (Y1 and drug release (Y2. The results revealed the surface pH of 6.8, similar to the pH of saliva. Viscosity study showed the marked increase in the viscosity of gel at 37°C due to sol-gel conversion. TSP was found to act as good mucoadhesive component to retain gel at the site of application in dental pocket. Gelation of formulation occurred near to body temperature. In vitro study depicted the fast onset of drug action but lasting the release (90% till 2 h. Formulation F7 was considered as optimized batch, containing 18% Lutrol F127 and 1% tamarind seed polysaccharide. Thus, lidocaine hydrochloride thermoreversible in situ gel offered an alternative to painful injection therapy of anesthesia during dental surgery, with fast onset of anesthetic action lasting throughout the dental procedure.

  8. Xyloglucan Based In Situ Gel of Lidocaine HCl for the Treatment of Periodontosis.

    Science.gov (United States)

    Pandit, Ashlesha P; Pol, Vaibhav V; Kulkarni, Vinit S

    2016-01-01

    The present study was aimed at formulating thermoreversible in situ gel of local anesthetic by using xyloglucan based mucoadhesive tamarind seed polysaccharide (TSP) into periodontal pocket. Temperature-sensitive in situ gel of lidocaine hydrochloride (LH) (2% w/v) was formulated by cold method. A full 3(2) factorial design was employed to study the effect of independent variables concentrations of Lutrol F127 and TSP to optimize in situ gel. The dependent variables evaluated were gelation temperature (Y 1) and drug release (Y 2). The results revealed the surface pH of 6.8, similar to the pH of saliva. Viscosity study showed the marked increase in the viscosity of gel at 37°C due to sol-gel conversion. TSP was found to act as good mucoadhesive component to retain gel at the site of application in dental pocket. Gelation of formulation occurred near to body temperature. In vitro study depicted the fast onset of drug action but lasting the release (90%) till 2 h. Formulation F7 was considered as optimized batch, containing 18% Lutrol F127 and 1% tamarind seed polysaccharide. Thus, lidocaine hydrochloride thermoreversible in situ gel offered an alternative to painful injection therapy of anesthesia during dental surgery, with fast onset of anesthetic action lasting throughout the dental procedure.

  9. Xyloglucan Based In Situ Gel of Lidocaine HCl for the Treatment of Periodontosis

    Science.gov (United States)

    Pandit, Ashlesha P.; Pol, Vaibhav V.; Kulkarni, Vinit S.

    2016-01-01

    The present study was aimed at formulating thermoreversible in situ gel of local anesthetic by using xyloglucan based mucoadhesive tamarind seed polysaccharide (TSP) into periodontal pocket. Temperature-sensitive in situ gel of lidocaine hydrochloride (LH) (2% w/v) was formulated by cold method. A full 32 factorial design was employed to study the effect of independent variables concentrations of Lutrol F127 and TSP to optimize in situ gel. The dependent variables evaluated were gelation temperature (Y1) and drug release (Y2). The results revealed the surface pH of 6.8, similar to the pH of saliva. Viscosity study showed the marked increase in the viscosity of gel at 37°C due to sol-gel conversion. TSP was found to act as good mucoadhesive component to retain gel at the site of application in dental pocket. Gelation of formulation occurred near to body temperature. In vitro study depicted the fast onset of drug action but lasting the release (90%) till 2 h. Formulation F7 was considered as optimized batch, containing 18% Lutrol F127 and 1% tamarind seed polysaccharide. Thus, lidocaine hydrochloride thermoreversible in situ gel offered an alternative to painful injection therapy of anesthesia during dental surgery, with fast onset of anesthetic action lasting throughout the dental procedure. PMID:27034908

  10. Interaction of anesthetics with neurotransmitter release machinery proteins.

    Science.gov (United States)

    Xie, Zheng; McMillan, Kyle; Pike, Carolyn M; Cahill, Anne L; Herring, Bruce E; Wang, Qiang; Fox, Aaron P

    2013-02-01

    General anesthetics produce anesthesia by depressing central nervous system activity. Activation of inhibitory GABA(A) receptors plays a central role in the action of many clinically relevant general anesthetics. Even so, there is growing evidence that anesthetics can act at a presynaptic locus to inhibit neurotransmitter release. Our own data identified the neurotransmitter release machinery as a target for anesthetic action. In the present study, we sought to examine the site of anesthetic action more closely. Exocytosis was stimulated by directly elevating the intracellular Ca(2+) concentration at neurotransmitter release sites, thereby bypassing anesthetic effects on channels and receptors, allowing anesthetic effects on the neurotransmitter release machinery to be examined in isolation. Three different PC12 cell lines, which had the expression of different release machinery proteins stably suppressed by RNA interference, were used in these studies. Interestingly, there was still significant neurotransmitter release when these knockdown PC12 cells were stimulated. We have previously shown that etomidate, isoflurane, and propofol all inhibited the neurotransmitter release machinery in wild-type PC12 cells. In the present study, we show that knocking down synaptotagmin I completely prevented etomidate from inhibiting neurotransmitter release. Synaptotagmin I knockdown also diminished the inhibition produced by propofol and isoflurane, but the magnitude of the effect was not as large. Knockdown of SNAP-25 and SNAP-23 expression also changed the ability of these three anesthetics to inhibit neurotransmitter release. Our results suggest that general anesthetics inhibit the neurotransmitter release machinery by interacting with multiple SNARE and SNARE-associated proteins.

  11. Assessing patient satisfaction with cataract surgery under topical anesthesia supplemented by intracameral lidocaine combined with sedation

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    Manuela Bezerril Cipião Fernandes

    2013-12-01

    Full Text Available PURPOSE: Ocular akinesia, the use of anticoagulants, and patient collaboration are some of the factors that must be taken into consideration when choosing the appropriate anesthesia for phacoemulsification cataract surgery. The satisfaction of patients with the use of topical anesthesia and conscious sedation for this procedure has not been enough described in Brazil. Conscious sedation allows patient walk and answer a voice command. To assess the satisfaction, pain, and perioperative hemodynamic alterations of patients subjected to phacoemulsification under conscious sedation and topical anesthesia supplemented with intracameral lidocaine. METHODS: Prospective cohort non-controlled study that included patients treated by the same surgical team over a 70-day period. Sedation was performed with midazolam at a total dose of 3 mg and topical anesthesia with 0.5% proxymetacaine chlorhydrate and 2% lidocaine gel combined with 2% lidocaine by intracameral route. The intraoperative vital parameters, scores based on the Iowa Satisfaction with Anesthesia Scale (ISAS, and the pain visual analog scale (VAS were recorded at several time points after surgery. RESULTS: A total of 106 patients were enroled in study (73.6% female, the mean age was 65.9 years. The surgical procedures lasted 11.2 minutes on average. The hemodynamic parameters did not exhibit significant changes at any of the investigated time points. The average ISAS score was 2.67 immediately after surgery and 2.99 eight hours after the surgery; this increase was statistically significant (p<0.0001. More than two-thirds (68.9% of the participants (73 patients did not report any pain in the transoperative period, and 98.1% of patients denied the occurrence of pain after surgery. CONCLUSIONS: Patients that received topical anesthesia supplemented by intracameral lidocaine combined with sedation for phacoemulsification cataract surgery reported adequate level of satisfaction with the anesthetic

  12. Addition of lidocaine to levobupivacaine reduces intrathecal block duration: randomized controlled trial

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    Dilek Yazicioglu

    2014-06-01

    Full Text Available Background: The duration of the spinal block is a concern for anesthetists. Low dose intrathecal lidocaine has vasodilatory effects and increases the local anesthetic clearance from the intrathecal space. The aim was to investigate whether this effect of lidocaine can be used to increase the resolution of levobupivacaine spinal anesthesia. Method: After obtaining ethical approval and informed patient consent, 40 patients underwent transurethral prostate resection were studied. Patients were randomized into two groups and patients received either levobupivacaine 6.75 mg + 0.3 mL 2% lidocaine (Group L or levobupivacaine 6.75 mg + saline (Group C. The main outcome measures were the difference between groups regarding the duration of the spinal block and PACU stay. Secondary outcome measures were the difference between groups in onset and resolution of the spinal block, adverse events and treatments were also investigated. Results: Spinal block resolved faster in Group L than Group C; 162.43 ± 39.4 min vs 219.73 ± 37.3 min (p = 0.000. PACU time was shorter in Group L (109 ± 49.9 min in Group L vs 148 ± 56.8 min in Group C (p = 0.036. There was no difference between groups with respect to the incidence of adverse events and treatments. Groups were also similar regarding complications. PDPH and TNS were not observed in any group. Conclusion: Addition of low dose lidocaine to hyperbaric levobupivacaine reduces the duration of the intrathecal block provided by hyperbaric levobupivacaine. This technique can be used to reduce the spinal block duration for relatively short procedures like TUR-P.

  13. Effect of Lidocaine–Ketamine Infusions Combined with Morphine or Fentanyl in Sevoflurane-Anesthetized Pigs

    Science.gov (United States)

    Re, Michela; Canfrán, Susana; Largo, Carlota; de Segura, Ignacio A Gómez

    2016-01-01

    Providing lidocaine, ketamine, and an opioid greatly decreases the minimum alveolar concentration (MAC) of volatile anesthetics in dogs. However, the efficacy of this combination shows marked interspecies variation, and opioids are likely to be less effective in pigs than in other species. The aim of the study was to determine the effects of constant-rate infusion of lidocaine and ketamine combined with either morphine or fentanyl on the MAC of sevoflurane in pigs. In a prospective, randomized, crossover design, 8 healthy crossbred pigs were premedicated with ketamine and midazolam, and anesthesia was induced and maintained with sevoflurane. Pigs then received ketamine (0.6 mg/kg/h) and lidocaine (3 mg/kg/h) combined with either morphine (0.24 mg/kg/h; MLK) or fentanyl (0.0045 mg/kg/h; FLK) after a loading dose; the control group received Ringers lactate solution. The anesthetic-sparing action of the 2 infusion protocols was calculated according to the MAC, by using dewclaw clamping as the standard noxious stimulus. The sevoflurane MAC (mean ± 1 SD) was 2.0% ± 0.2%, 1.9% ± 0.4%, and 1.8% ± 0.2% in the control, MLK, and FLK groups, respectively. No differences among groups or treatments were found. In conclusion, the administration of MLK or FLK at the studied doses did not reduce the MAC of sevoflurane in pigs. PMID:27177566

  14. Lipid emulsion-mediated reversal of toxic-dose aminoamide local anesthetic-induced vasodilation in isolated rat aorta

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    Ok, Seong-Ho; Han, Jeong Yeol; Lee, Soo Hee; Shin, Il-Woo; Lee, Heon Keun; Chung, Young-Kyun; Choi, Mun-Jeoung; Sohn, Ju-Tae

    2013-01-01

    Background Intravenous lipid emulsion has been used to treat systemic toxicity of local anesthetics. The goals of this in vitro study were to determine the ability of two lipid emulsions (Intralipid® and Lipofundin® MCT/LCT) to reverse toxic dose local anesthetic-induced vasodilation in isolated rat aortas. Methods Isolated endothelium-denuded aortas were suspended for isometric tension recording. Vasodilation was induced by bupivacaine (3 × 10-4 M), ropivacaine (10-3 M), lidocaine (3 × 10-3 ...

  15. Intraperitoneal Instillation of Lidocaine Improves Postoperative Analgesia at Cesarean Delivery: A Randomized, Double-Blind, Placebo-Controlled Trial.

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    Patel, Ruchira; Carvalho, Jose C A; Downey, Kristi; Kanczuk, Marcelo; Bernstein, Paul; Siddiqui, Naveed

    2017-02-01

    Cesarean delivery is a commonly performed procedure worldwide. Despite improvements in balanced multimodal analgesia, there remains a proportion of women for whom postoperative pain relief and patient satisfaction are still inadequate. Intraperitoneal instillation of local anesthetic has been shown to be effective in reducing postoperative pain after abdominal surgery. We sought to investigate the effect of intraperitoneal instillation of lidocaine on postcesarean delivery pain as part of a multimodal analgesia regimen. We studied women scheduled for elective cesarean delivery under spinal anesthesia. Spinal anesthesia was performed with 0.75% hyperbaric bupivacaine, fentanyl, and morphine. At the end of the cesarean delivery, immediately before parietal peritoneum or fascia closure, patients were randomized to receive either lidocaine (20 mL 2% lidocaine with epinephrine) or placebo (20 mL normal saline) instilled into the peritoneal cavity. The primary outcome was pain score on movement at 24 hours. Secondary outcomes were pain score at rest and on movement at 2, 24, and 48 hours; maternal satisfaction score; analgesic consumption; incidence of nausea, vomiting, and itching; and return of bowel function. Two hundred four women were recruited. Baseline characteristics were similar between the lidocaine and placebo groups. Pain scores at 24 hours postcesarean delivery on movement (parameter estimate 0.02 [95% confidence interval {CI} -0.14 to 0.18]; P = .823) and at rest (parameter estimate 0.00 [95% CI -0.32 to 0.33]; P = .986) were similar in both groups. Pain scores at 2 hours postcesarean delivery on movement (parameter estimate -0.58 [95% CI -0.90 to -0.26]; P = .001) and at rest (parameter estimate -1.00 [95% CI -1.57 to -0.43]; P = .001) were lower in the lidocaine group. Subgroup analysis of patients with peritoneum closure revealed significantly lower pain scores at 24 hours on movement (parameter estimate -0.33 [95% CI -0.64 to -0.03]; P = .032) in the

  16. Pharmacokinetic based adjustment of lidocaine antiarrhythmic schedule.

    Science.gov (United States)

    Voicu, V; Mircioiu, C; Jinga, M; Ionescu, M; Burcea, X; Ionescu, D D; Lupescu, G

    1994-01-01

    Administration of lidocaine, 200 mg/day i.m. or 275 mg orally, decreased sudden death after myocardial infarct (from 20.7% to 10.3%) although such schedules are not considered adequate to guarantee efficient plasma levels. Inclusion of lidocaine in a polyethylene matrix assured a slow release and complete disappearance of known side effects. Lidocaine was administered 200 mg intramuscularly to hospitalized patients every 6 h or 275 mg oral tablets to healthy volunteers every 8 h and plasma levels evaluated. Plasma levels after oral administration to healthy volunteers showed a great variability, so that it was not possible to draw a statistically significant conclusion about the accumulation of lidocaine in a period of 1 week. In coronary artery disease patients, plasma levels slowly increased with time, but clinical signs indicated, in some cases, a much more rapid accumulation. The therapeutic efficiency at low repeated doses was explained as a consequence of a slow accumulation on the one hand and of the addition of the action of MEGX, the major metabolite of lidocaine, on the other hand.

  17. Anesthetic management of ostriches.

    Science.gov (United States)

    Cornick, J L; Jensen, J

    1992-06-01

    We evaluated and characterized several anesthetic induction protocols used to facilitate intubation and anesthetic maintenance with isoflurane in 7 adult ostriches and 1 juvenile ostrich. Induction protocols included IV administration of zolazepam/tiletamine, IV administration of diazepam/ketamine with and without xylazine, IV administration of xylazine/ketamine, IM administration of carfentanil or xylazine/carfentanil, and mask induction with isoflurane. General anesthesia was maintained with isoflurane in 100% oxygen for various procedures, including proventriculotomy (6 birds), tibial (1 bird) or mandibular (1 bird) fracture repair, and drainage of an iatrogenic hematoma (1 bird). Heart rate and respiratory rate varied greatly among birds. The arterial blood pressure values recorded from 6 of the birds during maintenance of general anesthesia were higher than values recorded for most mammalian species, but were comparable to values reported for awake chickens and turkeys.

  18. Anesthetic effectiveness of the supplemental intraligamentary injection, administered with a computer-controlled local anesthetic delivery system, in patients with irreversible pulpitis.

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    Nusstein, John; Claffey, Elizabeth; Reader, Al; Beck, Mike; Weaver, Joel

    2005-05-01

    The purpose of this study was to determine the anesthetic effectiveness of the supplemental intraligamentary injection, administered with a computer-controlled local anesthetic delivery system, in mandibular posterior teeth diagnosed with irreversible pulpitis when the conventional inferior alveolar nerve block failed. Fifty-four emergency patients, diagnosed with irreversible pulpitis of a mandibular posterior tooth, received an inferior alveolar nerve block and had moderate to severe pain upon endodontic access. A computer-controlled local anesthetic delivery system was then used to administer intraligamentary injections of 1.4 ml of 2% lidocaine with 1:100,000 epinephrine. Success of the intraligamentary injection was defined as none or mild pain upon endodontic access or initial instrumentation. The results demonstrated that anesthetic success was obtained in 56% (30 of 54) of the patients. We concluded that when the inferior alveolar nerve block failed to provide profound pulpal anesthesia in mandibular posterior teeth of patients presenting with irreversible pulpitis, the intraligamentary injection administered with a computer-controlled local anesthetic delivery system was successful approximately 56% of the time.

  19. [Studying the mechanism of antiarrhythmic action of a tertiary derivative of lidocaine].

    Science.gov (United States)

    Blinov, D S; Kostin, Ia V; Skachilova, S Ia

    2004-01-01

    The investigation of electrophysiological parameters of the cardiac activity in cats showed that, a derivative of lidocaine with glutamic acid (anion), does not influence the cardiac pacemaker and the myocardial excitability of atrium and ventricles, but decreases the atrioventricular conduction and increases the refractory period of myocardium in the left ventricle of intact heart. Under the conditions of myocardial ischemia, LKhT-3-00 exhibits a negative chronotropic effect. Lidocaine glutamate increases the refractory period of atrium and decreases the excitability and refractory period of ventricles.

  20. Lidocaine block of cardiac sodium channels

    OpenAIRE

    Bean, BP; Cohen, CJ; Tsien, RW

    1983-01-01

    Lidocaine block of cardiac sodium channels was studied in voltage-clamped rabbit purkinje fibers at drug concentrations ranging from 1 mM down to effective antiarrhythmic doses (5-20 μM). Dose-response curves indicated that lidocaine blocks the channel by binding one-to-one, with a voltage-dependent K(d). The half-blocking concentration varied from more than 300 μM, at a negative holding potential where inactivation was completely removed, to approximately 10 μM, at a depolarized holding pote...

  1. Neonatal bilateral lidocaine administration into the ventral hippocampus caused postpubertal behavioral changes: An animal model of neurodevelopmental psychopathological disorders

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    Vanessa Blas-Valdivia

    2008-12-01

    Full Text Available Vanessa Blas-Valdivia, Edgar Cano-Europa, Adelaida Hernández-García, Rocio Ortiz-ButrónDepartamento de Fisiología “Mauricio Russek Berman”, Escuela Nacional de Ciencias Biológicas, I.P.N., Carpio y Plan de Ayala, MéxicoAbstract: Our aim was to investigate if neonatal bilateral administration of lidocaine into the ventral hippocampus would cause behavioral changes related to schizophrenia. A neonatal ventral-hippocampal lesion (nVH lesion was made with lidocaine in Wistar male pups. Two groups were formed, the first received lidocaine (4 μg/0.3 μL and the second an equal volume of vehicle. At day 35 and 56, both groups were tested for social contact, immobility caused by clamping the neck and dorsal immobility, locomotor activity in an open field, and tail flick (TF latency after a painful heat stimulus. All animals were then killed. Coronal cuts (7 μm of the brain were obtained and each brain section was stained with cresyl violet-eosin. The animals which received the nVH lesion with lidocaine had decreased social interaction at both ages. The rats with lesions, only at day 58 postnatal, increased their distance traveled and ambulatory time, with a decrease in their nonambulatory and reset time. The rats with lesions had a longer duration of immobility caused by clamping the neck and a longer dorsal immobility at both days 34 and 57 compared to control rats. The lidocaine-treated group spent less time to deflect the tail compared to the control group at postpubertal age. The neonatal bilateral administration of lidocaine into the ventral hippocampus caused some alterations, such as chromatin condensation, nucleolus loss, and cell shrinkage, but glial proliferation was not seen. Neonatal bilateral lidocaine administration into the ventral hippocampus caused postpubertal behavioral changes.Keywords: lidocaine, hippocampus, neonatal lesion, behavior, animal model, psychopathological disorders

  2. Efficacy of intravenous lidocaine to reduce pain and distress associated with propofol infusion in pediatric patients during procedural sedation.

    Science.gov (United States)

    Depue, Kent; Christopher, Norman C; Raed, Mona; Forbes, Michael L; Besunder, James; Reed, Michael D

    2013-01-01

    Research suggests that young children experience an increased incidence and severity of discomfort during propofol infusion. Evaluations of varied interventions to reduce or eliminate this discomfort with adult subjects suggest that premedication with intravenously administered lidocaine (0.5 mg/kg) offers the best overall effectiveness. Because this regimen's efficacy in a pediatric population is undocumented, we conducted a randomized, double-blind, placebo-controlled study to determine the effectiveness of intravenous lidocaine pretreatment to alleviate pain in pediatric subjects before propofol infusion. Subjects (aged 2-7 years) scheduled for painless diagnostic procedures received either a saline placebo or 1 of 2 lidocaine doses before administering propofol. To capture the patient's baseline behavioral state, a trained observer administered the validated face, legs, activity, cry, consolability pain assessment scale before propofol infusion. During deep sedation induction, the sedating physician, a trained research assistant, and the patient's parent documented maximum distress using a 100-mm visual analog scale (VAS). Ninety-one subjects participated. We found no difference in VAS pain scores between groups pretreated with lidocaine 0.25 mg/kg, lidocaine 0.5 mg/kg, and placebo. Statistical analysis also found no interrater differences between parents, physician, or observer VAS scores. Our data do not support using lidocaine pretreatment to alleviate pain/discomfort in pediatric patients during propofol infusion.

  3. Lidocaine versus lidocaine plus benzydamine as a topical anesthesia regimen for unsedated upper gastrointestinal endoscopy: A comparison study.

    Science.gov (United States)

    İbiş, Mehmet; Arhan, Mehmet; İbiş, Tuba; Önal, İbrahim Koral; Erdal, Harun; Utku, Özlem Gül

    2015-05-01

    The aim was to assess the efficacy of adding benzydamine (B) spray to standard treatment with a lidocaine (L) spray before upper gastrointestinal endoscopy (UGE) as a topical anaesthetic regimen. A total of 118 adult patients undergoing outpatient UGE were randomly assigned to receive L (n=44), LB (n=38) or B (n=36) before the procedure. The primary outcome was the patient tolerance score, which represents a summative evaluation of the taste of the anesthetic agent, the intensity of pharyngeal numbness, the amount of coughing or gagging and the degree of discomfort during oesophageal intubation. The median (min-max) patient tolerance scores were comparable between groups LB (10.5; range 5-12) and L (10; range 4-13) (p=0.235) and significantly lower in group B (7.5; range 3-12) (psore throat (4 [10.5%] vs 15 [34.1%], p=0.011) in LB compared to L. LB is not superior to L in terms of overall patient tolerance, but LB may be preferred over L in cases with difficult oesophageal intubation or a previous history of postprocedural sore throat.

  4. CLINICAL EVALUATION OF EPIDURAL ADMINISTRATION OF MORPHINE, FENTANYL, METHADONE, LIDOCAINE AND LIDOCAINE WITH EPINEPHRINE IN CATTLE

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    A. Tabatabaei Naeine, A. Rezakhani and J. Fazlinia

    2004-01-01

    Full Text Available The purpose of this study was to determine the analgesic efficacy and clinical effects of morphine, fentanyl, methadone, lidocaine, lidocaine with epinephrine and saline (control when injected epidurally into the caudal epidural space in cattle. Epidural analgesia was achieved in five cattle on five successive occasions at weekly intervals. Analgesia was defined as a lack of response to hemostat pressure and pinprick in the skin of the perineal area and ventral aspect of the tail. The results demonstrated that while epidural lidocaine and lidocaine with epinephrine decreased the response to hemostat and pinprick compared to control, there was no reduction in response after the administration of morphine, methadone or fentanyl. Heart rate, pulse and respiratory rates were not significantly altered by any of the drugs. Neither did the drugs produce any change in the electrocardiogram (ECG of the animals.

  5. Under Utilization of Local Anesthetics in Infant Lumbar Punctures

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    Gorchynski, Julie

    2008-01-01

    Full Text Available Background: Lumbar Puncture (LP is an invasive procedure frequently used to diagnose meningitis among the pediatric population. Neonates and infants have not routinely received local anesthesia prior to LP. Study Objective: To determine whether emergency medicine physicians and pediatricians use local analgesics on neonates and infants prior to performing an LP and to identify which local anesthetics, if any, were used. Methods: Prospective, cohort study of all infants, six months of age or less, that received an LP in the emergency department (ED or inpatient pediatric units for suspected meningitis during a period of year at a university tertiary care hospital. Results: A total sample population of 111 infants that received an LP within the study period. A control population of 42 adults received an LP. Only 40.4% (45/111 of the infants received local analgesia prior to LP: either 1% lidocaine, EMLA or a combination of the two. Infants were less likely to receive lidocaine or EMLA prior to LP compared to adult subjects (OR= 0.27; 95% CI0.12 to 0.62. No neonates that were less than one month of age received local procedural anesthesia by emergency medicine or pediatric physicians. ED physicians’ use of local anesthesia prior to LP increased with increasing age of the infant. The pediatricians in this study used local anesthesia prior to LP when the infant was at least five months of age. Discussion: The data objectively support recent literature regarding the under use or lack of use of analgesia prior to LP among neonates and infants. Local anesthetics should be used routinely without exception prior to performing an LP in the pediatric population.

  6. BLOCKADE OF ROSTRAL VENTROLATERAL MEDULLA (RVLM BOMBESIN RECEPTOR TYPE 1 DECREASES BLOOD PRESSURE AND SYMPATHETIC ACTIVITY IN ANESTHETIZED SPONTANEOUSLY HYPERTENSIVE RATS

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    Izabella Silva De Jesus Pinto

    2016-06-01

    Full Text Available IIntrathecal injection of bombesin (BBS promoted hypertensive and sympathoexcitatory effects in normotensive (NT rats. However, the involvement of rostral ventrolateral medulla (RVLM in these responses is still unclear. In the present study, we investigated: (1 the effects of BBS injected bilaterally into RVLM on cardiorespiratory and sympathetic activity in NT and spontaneously hypertensive rats (SHR; (2 the contribution of RVLM bombesin type 1 receptors (BB1 to the maintenance of hypertension in SHR. Urethane-anesthetized rats (1.2 g · kg−1, i.v. were instrumented to record mean arterial pressure (MAP, diaphragm (DIA motor and renal sympathetic nerve activity (RSNA. In NT rats and SHR, BBS (0.3 mM nanoinjected into RVLM increased MAP (33.9 ± 6.6 mmHg and 37.1 ± 4.5 mmHg, respectively; p < 0.05 and RSNA (97.8 ± 12.9 % and 84.5 ± 18.1 %, respectively; p < 0.05. In SHR, BBS also increased DIA burst amplitude (115.3 ± 22.7 %; p < 0.05. BB1 receptors antagonist (BIM-23127; 3 mM reduced MAP (-19.9 ± 4.4 mmHg; p < 0.05 and RSNA (-17.7 ± 3.8 %; p < 0.05 in SHR, but not in NT rats (-2.5 ± 2.8 mmHg; -2.7 ± 5.6 %, respectively. These results show that BBS can evoke sympathoexcitatory and pressor responses by activating RVLM BB1 receptors. This pathway might be involved in the maintenance of high levels of arterial blood pressure in SHR.

  7. Biodegradable nanofiber-membrane for sustainable release of lidocaine at the femoral fracture site as a periosteal block: In vitro and in vivo studies in a rabbit model.

    Science.gov (United States)

    Chou, Ying-Chao; Cheng, Yi-Shiun; Hsu, Yung-Heng; Yu, Yi-Hsun; Liu, Shih-Jung

    2016-04-01

    The aim of this study was to evaluate the efficacy of a biodegradable, lidocaine-embedded, nanofibrous membrane for the sustainable analgesic release onto fragments of a segmental femoral fracture site. Membranes of three different lidocaine concentrations (10%, 30%, and 50%) were produced via an electrospinning technique. In vitro lidocaine release was assessed by high-performance liquid chromatography. A femoral segmental fracture, with intramedullary Kirschner-wire fixation and polycaprolactone stent enveloping the fracture site, was set-up in a rabbit model for in vivo assessment of post-operative recovery of activity. Eighteen rabbits were randomly assigned to three groups (six rabbits per group): group A comprised of rabbits with femoral fractures and underwent fixation; group B comprised of a comparable fracture model to that of group A with the implantation of lidocaine-loaded nanofibers; and group C, the control group, received only anesthesia. The following variables were measured: change in body weight, food and water intake before and after surgery, and total activity count post-surgery. All membranes eluted effective levels of lidocaine for more than 3 weeks post-surgery. Rabbits in group B showed faster recovery of activity post-operatively, compared with those in group A, which confirmed the pain relief efficacy of the lidocaine-embedded nanofibers. Nanofibers with sustainable lidocaine release have adequate efficacy and durability for pain relief in rabbits with segmental long bone fractures.

  8. Age-related response to lidocaine-prilocaine (EMLA) emulsion and effect of music distraction on the pain of intravenous cannulation.

    Science.gov (United States)

    Arts, S E; Abu-Saad, H H; Champion, G D; Crawford, M R; Fisher, R J; Juniper, K H; Ziegler, J B

    1994-05-01

    To compare the efficacy of a local anesthetic cream and music distraction in reducing or preventing pain from needle puncture (intravenous cannulation) in children. A secondary aim was to examine the influence of age on the pain report and behavior and on the therapeutic outcome. Children aged 4 to 16 years (N = 180) who were to undergo surgery under general anesthesia via intravenous cannulation were randomly allocated to one of three interventions. The comparison of lidocaine-prilocaine emulsion (EMLA, Astra) and a placebo emulsion was double-blind. Stratification by age group (4 to 6, 7 to 11, 12 to 16) ensured an equal number of children (20) in each intervention/age group category. A global assessment of the behavioral reaction to the procedure was made by the principal investigator, taking into account vocal, verbal, facial, and motor responses. The child was asked to assess pain severity on the Faces Pain Scale (FPS) and a visual analogue toy (VAT). The scales were applied conservatively as ordinal scales: FPS 0 to 6; VAT 0 to 10. Children who received lidocaine-prilocaine emulsion reported less pain (mean FPS score = 1.42) compared with placebo emulsion (mean FPS score = 2.58) and with music distraction (mean FPS = 2.62). There was a highly significant therapeutic effect (P pain than the older children (mean FPS scores: 2.85, 2.33, 1.43 for age groups 4 to 6, 7 to 11, and 12 to 16 respectively; P pain-related behavior, and multiple regression analysis confirmed significant age and treatment effects and revealed interaction between therapeutic effect and age. Although a trend favoring the active emulsion was evident in the older children (7 to 11, 12 to 16) the differences were not significant. The pain scores were influenced by the type (gauge) of cannula, but this did not affect the conclusion regarding therapeutic and age effects. There was no influence of sex, experience with venipuncture, or whether the child was anxious on arrival in the operating room

  9. Llama anesthetic programs.

    Science.gov (United States)

    Heath, R B

    1989-03-01

    Llamas are anesthetized conveniently with guaifenesin thiamylal mixes, or, for short periods of time, with xylazine/ketamine. Small individuals must be accurately weighed. Estimating weight without experience is dangerous in this species. The greatest levels of safety and control, especially for critical patients, is afforded by inhalation anesthesia techniques using small animal equipment. All neonates and juveniles can be masked readily but in adults intravenous induction is most satisfactory. Intubation is aided by a long blade laryngoscope. Blood pressure monitoring is best accomplished with an arterial line in the ear artery. However, doppler equipment on the tail or distal leg usually works well.

  10. TASK-3 knockout mice exhibit exaggerated nocturnal activity, impairments in cognitive functions, and reduced sensitivity to inhalation anesthetics.

    Science.gov (United States)

    Linden, Anni-Maija; Sandu, Cristina; Aller, M Isabel; Vekovischeva, Olga Y; Rosenberg, Per H; Wisden, William; Korpi, Esa R

    2007-12-01

    The TASK-3 channel is an acid-sensitive two-pore-domain K+ channel, widely expressed in the brain and probably involved in regulating numerous neuronal populations. Here, we characterized the behavioral and pharmacological phenotypes of TASK-3 knockout (KO) mice. Circadian locomotor activity measurements revealed that the nocturnal activity of the TASK-3 KO mice was increased by 38% (P walking on a rotating rod or along a 1.2-cm-diameter beam. However, they fell more frequently from a narrower 0.8-cm beam. The KO mice showed impaired working memory in the spontaneous alternation task, with the alternation percentage being 62 +/- 3% for the wild-type mice and 48 +/- 4% (P rhythms, cognitive functions, and mediating specific pharmacological effects.

  11. Fentanyl supplement expedites the onset time of sensory and motor blocking in interscalene lidocaine anesthesia

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    RS Moharari

    2010-12-01

    Full Text Available Background and the purpose of the study: Opioids are usually used in regional anesthesia, with or without local anesthetics to improve the regional block or postoperative pain control. Since no data are available on fentanyl's effect on the onset time of lidocaine interscalene anesthesia, the purpose of this study was to examine its effect on the onset time of sensory and motor blockade during interscalene anesthesia.  Methods: In a prospective, randomized, double-blind study, ninety patients scheduled for elective shoulder, arm and forearm surgeries under an  interscalene brachial plexus block .They were randomly allocated to receive either 30 ml of  1.5 % lidocaine with 1.5 ml of isotonic saline  (control group, n = 39 or 30 ml of 1.5%  lidocaine with 1.5 ml (75µg of  fentanyl (fentanyl group,n=41. Then the onset time of sensory and motor blockades of the shoulder, arm and forearm were evaluated every 60 sec. The onset time of the sensory and motor blockades was defined as the time between the last injection and the total abolition of the pinprick response and complete paralysis. The duration of sensory blocks were considered as the time interval between the administration of the local anesthetic and the first postoperative pain sensation. Results: Ten patients were excluded because of unsuccessful blockade or unbearable pain during the surgery. The onset time of the sensory block was significantly faster in the fentanyl group (186.54± 62.71sec compared with the control group (289.51± 81.22, P < 0.01. The onset times of the motor block up to complete paralysis in forearm flexion was significantly faster in the fentanyl group (260.61± 119.91sec than the control group (367.08± 162.43sec, P < 0.01 There was no difference in the duration of the sensory block between two groups. Conclusion: Results of the study showed that the combination of 75 µg fentanyl and 1.5% lidocaine solution accelerated the onset of sensory and motor

  12. Anesthetic-Induced Developmental Neurotoxicity

    Institute of Scientific and Technical Information of China (English)

    Jia-RenLiu; Qian Liu; Jing Li; Sulpicio G. Soriano

    2011-01-01

    1 IntroductionMillions of newborn and infants receive anesthetic,sedative and analgesic drugs for surgery and painful procedures on a daily basis.Recent laboratory reports clearly demonstrate that anesthetic and sedative drugs induced both neuroapoptosis and neurocognitive deficits in laboratory models.This issue is of paramount interest to pediatric anesthesiologists and intensivists because it questions the safety of anesthetics used for fetal and neonatal anesthesia[1-2].In an attempt to summarize the rapidly expanding laboratorybased literature on anesthetic-induced developmental neurotoxicity (AIDN),this review will examine published reports on the characterization,mechanisms and alleviation of this phenomenon.

  13. Passive and active mechanical properties of the superficial and deep digital flexor muscles in the forelimbs of anesthetized Thoroughbred horses.

    Science.gov (United States)

    Swanstrom, Michael D; Zarucco, Laura; Stover, Susan M; Hubbard, Mont; Hawkins, David A; Driessen, Bernd; Steffey, Eugene P

    2005-03-01

    The superficial (SDF) and deep digital flexor (DDF) muscles are critical for equine forelimb locomotion. Knowledge of their mechanical properties will enhance our understanding of limb biomechanics. Muscle contractile properties derived from architectural-based algorithms may overestimate real forces and underestimate shortening capacity because of simplistic assumptions regarding muscle architecture. Therefore, passive and active (=total - passive) force-length properties of the SDF and DDF muscles were measured directly in vivo. Muscles from the right forelimbs of four Thoroughbred horses were evaluated during general anesthesia. Limbs were fixed to an external frame with the muscle attached to a linear actuator and load cell. Each muscle was stretched from an unloaded state to a range of prefixed lengths, then stimulated while held at that length. The total force did not exceed 4000 N, the limit for the clamping device. The SDF and DDF muscles produced 716+/-192 and 1577+/-203 N maximum active isometric force (F(max)), had ascending force-length ranges (R(asc)) of 5.1+/-0.2 and 9.1+/-0.4 cm, and had passive stiffnesses of 1186+/-104 and 1132+/-51 N/cm, respectively. The values measured for F(max) were much smaller than predicted based on conservative estimates of muscle specific tension and muscle physiological cross-sectional area. R(asc) were much larger than predicted based on muscle fiber length estimates. These data suggest that accurate prediction of the active mechanical behavior of architecturally complex muscles such as the equine DDF and SDF requires more sophisticated algorithms.

  14. Optical recording of neuronal activity with a genetically-encoded calcium indicator in anesthetized and freely moving mice

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    Henry Lütcke

    2010-04-01

    Full Text Available Fluorescent calcium (Ca2+ indicator proteins (FCIPs are promising tools for functional imaging of cellular activity in living animals. However, they have still not reached their full potential for in vivo imaging of neuronal activity due to limitations in expression levels, dynamic range, and sensitivity for reporting action potentials. Here, we report that viral expression of the ratiometric Ca2+ sensor yellow cameleon 3.60 (YC3.60 in pyramidal neurons of mouse barrel cortex enables in vivo measurement of neuronal activity with high dynamic range and sensitivity across multiple spatial scales. By combining juxtacellular recordings and two-photon imaging in vitro and in vivo, we demonstrate that YC3.60 can resolve single action potential (AP-evoked Ca2+ transients and reliably reports bursts of APs with negligible saturation. Spontaneous and whisker-evoked Ca2+ transients were detected in individual apical dendrites and somata as well as in local neuronal populations. Moreover, bulk measurements using wide-field imaging or fiber-optics revealed sensory-evoked YC3.60 signals in large areas of the barrel field. Fiber-optic recordings in particular enabled measurements in awake, freely moving mice and revealed complex Ca2+ dynamics, possibly reflecting different behavior-related brain states. Viral expression of YC3.60 - in combination with various optical techniques - thus opens a multitude of opportunities for functional studies of the neural basis of animal behavior, from dendrites to the levels of local and large-scale neuronal populations.

  15. Central 5-HT2A receptors modulate the vagal bradycardia in response to activation of the von Bezold-Jarisch reflex in anesthetized rats

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    H.A. Futuro Neto

    2011-03-01

    Full Text Available Activation of 5-hydroxytryptamine (5-HT 5-HT1A, 5-HT2C, 5-HT3, and 5-HT7 receptors modulates the excitability of cardiac vagal motoneurones, but the precise role of 5-HT2A/2B receptors in these phenomena is unclear. We report here the effects of intracisternal (ic administration of selective 5-HT2A/2B antagonists on the vagal bradycardia elicited by activation of the von Bezold-Jarisch reflex with phenylbiguanide. The experiments were performed on urethane-anesthetized male Wistar rats (250-270 g, N = 7-9 per group. The animals were placed in a stereotaxic frame and their atlanto-occipital membrane was exposed to allow ic injections. The rats received atenolol (1 mg/kg, iv to block the sympathetic component of the reflex bradycardia; 20-min later, the cardiopulmonary reflex was induced with phenylbiguanide (15 µg/kg, iv injected at 15-min intervals until 3 similar bradycardias were obtained. Ten minutes after the last pre-drug bradycardia, R-96544 (a 5-HT2A antagonist; 0.1 µmol/kg, SB-204741 (a 5-HT2B antagonist; 0.1 µmol/kg or vehicle was injected ic. The subsequent iv injections of phenylbiguanide were administered 5, 20, 35, and 50 min after the ic injection. The selective 5-HT2A receptor antagonism attenuated the vagal bradycardia and hypotension, with maximal effect at 35 min after the antagonist (pre-drug = -200 ± 11 bpm and -42 ± 3 mmHg; at 35 min = -84 ± 10 bpm and -33 ± 2 mmHg; P < 0.05. Neither the 5-HT2B receptor antagonists nor the vehicle changed the reflex. These data suggest that central 5-HT2A receptors modulate the central pathways of the parasympathetic component of the von Bezold-Jarisch reflex.

  16. Pharmacokinetics of lidocaine and bupivacaine following subarachnoid administration in surgical patients: simultaneous investigation of absorption and disposition kinetics using stable isotopes

    Energy Technology Data Exchange (ETDEWEB)

    Burm, A.G.; Van Kleef, J.W.; Vermeulen, N.P.; Olthof, G.; Breimer, D.D.; Spierdijk, J.

    1988-10-01

    The pharmacokinetics of lidocaine and bupivacaine following subarachnoid administration were studied in 12 surgical patients using a stable isotope method. After subarachnoid administration of the agent to be evaluated, a deuterium-labelled analogue was administered intravenously. Blood samples were collected for 24 h. Plasma concentrations of the unlabelled and the deuterium-labelled local anesthetics were determined using a combination of capillary gas chromatography and mass fragmentography. Bi-exponential functions were fitted to the plasma concentration-time data of the deuterium-labelled local anesthetics. The progression of the absorption was evaluated using deconvolution. Mono- and bi-exponential functions were then fitted to the fraction absorbed versus time data. The distribution and elimination half-lives of the deuterium-labelled analogues were 25 +/- 13 min (mean +/- SD) and 121 +/- 31 min for lidocaine and 19 +/- 10 min and 131 +/- 33 min for bupivacaine. The volumes of the central compartment and steady-state volumes of distribution were: lidocaine 57 +/- 10 l and 105 +/- 25 l, bupivacaine 25 +/- 6 l and 63 +/- 22 l. Total plasma clearance values averaged 0.97 +/- 0.21 l/min for lidocaine and 0.56 +/- 0.14 l/min for bupivacaine. The absorption of lidocaine could be described by a single first order absorption process, characterized by a half-life of 71 +/- 17 min in five out of six patients. The absorption of bupivacaine could be described adequately assuming two parallel first order absorption processes in all six patients. The half-lives, characterizing the fast and slow absorption processes of bupivacaine, were 50 +/- 27 min and 408 +/- 275 min, respectively. The fractions of the dose, absorbed in the fast and slow processes, were 0.35 +/- 0.17 and 0.61 +/- 0.16, respectively.

  17. Efficacy of Topical Anesthetics in the Treatment of Ingrown Nail

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    Fatma Gülru Erdoğan

    2011-06-01

    Full Text Available Background and Design: One of the reasons for preferring conservative methods for ingrown nails is lack of local anesthesia for the painful step. Moreover, ingrown nail is a painful condition per se. It may be very difficult to intervene patients with high basal pain levels. Here, we aimed to assess the efficacy of topical anesthetics (2.5% lidocaine, 2.5% prilocaine mixture and 20% benzocaine gel by determining basal pain level and pain during and after manipulation in patients with severe pain who applied with ingrown nail complaint.Material and Method: In this study, we included a total of 29 patients (12 male, 17 female who had complaint of ingrown nail and for whom nail brace treatment was planned. The patients were divided randomly into two groups regardless of the stage of ingrown nail: with lidocain-prilocain mixture application and with benzocaine gel application. Benzocaine gel was applied 10 minutes before the procedure and lidocaine-prilocaine mixture was applied under occlusion, 2 hours prior to the procedure. Pain levels were evaluated on a numerical pain rating scale before and after topical anesthesia as well as during and half an hour after the procedure in both groups.Results: Statistical difference was not detected between the pain levels of the two groups before and after topical anesthesia and during and half an hour after the procedure. Regardless of the stage of ingrown nail, the pain levels after topical anesthesia and half an hour after procedure were found to decrease significantly compared to the levels before topical anesthesia in both groups. Pain levels of both groups increased during the procedure and were similar to the basal levels. Considering the stage of ingrown nail, while lidocaine-prilocaine mixture did not decrease pain significantly in the cases with stage 2-3, benzocaine did. Conclusion: Due to ease of application and especially to efficacy in stage 2-3 ingrown nails, 20% benzocaine gel may help in

  18. History of T-cain: a local anesthetic developed and manufactured in Japan.

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    Tobe, Masaru; Saito, Shigeru

    2015-10-01

    In many anesthesia textbooks written in English, lidocaine, tetracaine, bupivacaine, ropivacaine, and chloroprocaine are listed as useful local anesthetics for spinal anesthesia. In contrast, T-cain is not included in these lists, even though it has been reported to be suitable for spinal anesthesia in Japan. T-cain was developed as a local anesthetic in the early 1940s by Teikoku Kagaku Sangyo Inc. in Itami, Japan, by replacing a methyl group on tetracaine (Pantocaine(®)) with an ethyl group. T-cain was clinically approved for topical use in Japan in November 1949, and a mixture of dibucaine and T-cain (Neo-Percamin S(®)) was approved for spinal use in May 1950. Simply because of a lack of foreign marketing strategy, T-cain has never attracted global attention as a local anesthetic. However, in Japan, T-cain has been used topically or intrathecally (as Neo-Percamin S(®)) for more than 60 years. Other than the side effects generally known for all local anesthetics, serious side effects have not been reported for T-cain. In fact, several articles have reported that T-cain decreases the neurotoxicity of dibucaine. In this historical review, the characteristics of T-cain and its rise to become a major spinal anesthetic in Japan are discussed.

  19. Randomized double-blind clinical trial comparing two anesthetic techniques for ultrasound-guided transvaginal follicular puncture

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    de Oliveira, Gilvandro Lins; Serralheiro, Fernando Cesar; Fonseca, Fernando Luiz Affonso; Ribeiro, Onésimo Duarte; Adami, Fernando; Christofolini, Denise Maria; Bianco, Bianca; Barbosa, Caio Parente

    2016-01-01

    ABSTRACT Objective: To compare the anesthetic techniques using propofol and fentanyl versus midazolam and remifentanil associated with a paracervical block with lidocaine in performing ultrasound-guided transvaginal oocyte aspiration. Methods: A randomized double-blind clinical trial (#RBR-8kqqxh) performed in 61 women submitted to assisted reproductive treatment. The patients were divided into two groups: anesthetic induction with 1mcg/kg of fentanyl associated with 1.5mg/kg of propofol (FP Group, n=32), in comparison with anesthetic induction using 0.075mg/kg of midazolam associated with 0.25mcg/kg/min of remifentanil, and paracervical block with 3mL of 2% lidocaine (MRPB Group, n=29). Main outcome measures: human reproduction outcomes, modified Aldrete-Kroulik index, hemodynamic parameters, and salivary cortisol. Results: The results revealed a higher number of embryos formed in the FP Group (p50=2 versus 1; p=0.025), gestation rate two times higher in the FP Group (44.4% versus 22.2%; p=0.127), less time to reach AK=10 in the MRPB Group (p50=10 versus 2; p<0.001), and lower mean of hemodynamic parameters in the MRPB Group (p<0.05). Conclusion: Anesthesia with fentanyl and propofol as well as with midazolam, remifentanil, and paracervical block offered satisfactory anesthetic conditions when performing assisted reproduction procedures, providing comfort for the patient and physician. PMID:27759816

  20. Effect on postoperative sore throat of spraying the endotracheal tube cuff with benzydamine hydrochloride, 10% lidocaine, and 2% lidocaine.

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    Hung, Nan-Kai; Wu, Ching-Tang; Chan, Shun-Ming; Lu, Chueng-He; Huang, Yuan-Shiou; Yeh, Chun-Chang; Lee, Meei-Shyuan; Cherng, Chen-Hwan

    2010-10-01

    Postoperative sore throat (POST) is a common complication after endotracheal intubation. We compared the effectiveness on POST of spraying the endotracheal tube (ETT) cuff with benzydamine hydrochloride, 10% lidocaine, and 2% lidocaine. Three hundred seventy-two patients were randomly allocated into 4 groups. The ETT cuffs in each group were sprayed with benzydamine hydrochloride, 10% lidocaine hydrochloride, 2% lidocaine hydrochloride, or normal saline before endotracheal intubation. After insertion, the cuffs were inflated to an airway leak pressure of 20 cm H(2)O. Anesthesia was maintained with propofol. The patients were examined for sore throat (none, mild, moderate, or severe) at 1, 6, 12, and 24 hours after extubation. The highest incidence of POST occurred at 6 hours after extubation in all groups. There was a significantly lower incidence of POST in the benzydamine group than 10% lidocaine, 2% lidocaine, and normal saline groups (P benzydamine group (17.0%) compared with 10% lidocaine (53.7%), 2% lidocaine (37.0%), and normal saline (40.8%) groups (P benzydamine group had significantly decreased severity of POST compared with the 10% lidocaine, 2% lidocaine, and normal saline groups (P benzydamine hydrochloride on the ETT cuff is a simple and effective method to reduce the incidence and severity of POST.

  1. Identification of the epidural space: loss of resistance with air, lidocaine, or the combination of air and lidocaine.

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    Evron, Samuel; Sessler, Daniel; Sadan, Oscar; Boaz, Mona; Glezerman, Marek; Ezri, Tiberiu

    2004-07-01

    The ideal technique for identifying the epidural space remains unclear. Five-hundred-forty-seven women in labor who requested epidural analgesia were randomly allocated to three groups according to the technique by which the epidural space was identified: 1) loss-of-resistance with air (air; n = 180), 2) loss-of-resistance with lidocaine (lidocaine; n = 185), and 3) loss-of-resistance with both air and lidocaine (air-plus-lidocaine; n = 182). We assessed ease of epidural catheter insertion, characteristics of the blockade, quality of analgesia, and complications. The inability to thread the epidural catheter occurred in 16% of the air, 4% of the lidocaine, and 3% of the air-plus-lidocaine patients (P air group had unblocked segments (6.6% versus 3.2% and 2.2%, respectively; P air group (1.7% versus 0% in the other two groups; P space with air was more difficult and caused more dural punctures than with lidocaine or air plus lidocaine. Additionally, sequential use of air and lidocaine had no advantage over lidocaine alone.

  2. Use of eutectic mixture of local anesthetics in children.

    Science.gov (United States)

    Dutta, S

    1999-01-01

    The Eutectic Mixture of Local Anesthetics (EMLA) is a topical application, which has proved to be a useful medication for providing pain relief among children. It is an emulsion containing a 1:1 mixture of lidocaine and prilocaine. The high concentration of the uncharged anesthetic base in the microdroplets of the emulsion ensure effective skin penetration. In the pediatric population EMLA has been shown to be efficacious when it is used prior to venipuncture, cannulation, lumbar puncture, laser treatment of port wine stains, curettage of molluscum contagiosum or vaccination. For several of these indications, the efficacy has been documented by double blind controlled trials, that have used objective and quasi-objective scales for assessing pain relief. The dose of EMLA is between 0.5 to 1 gram, and the cream should be applied half to one hour prior to the procedure. Local side effects are very mild, and the only systemic side effect of importance is the risk of methemoglobinemia in young infants. The literature has conflicting reports about the safety of EMLA in neonates.

  3. Comparison of Gating Properties and Use-Dependent Block of Nav1.5 and Nav1.7 Channels by Anti-Arrhythmics Mexiletine and Lidocaine.

    Science.gov (United States)

    Wang, Ying; Mi, Jianxun; Lu, Ka; Lu, Yanxin; Wang, KeWei

    2015-01-01

    Mexiletine and lidocaine are widely used class IB anti-arrhythmic drugs that are considered to act by blocking voltage-gated open sodium currents for treatment of ventricular arrhythmias and relief of pain. To gain mechanistic insights into action of anti-arrhythmics, we characterized biophysical properties of Nav1.5 and Nav1.7 channels stably expressed in HEK293 cells and compared their use-dependent block in response to mexiletine and lidocaine using whole-cell patch clamp recordings. While the voltage-dependent activation of Nav1.5 or Nav1.7 was not affected by mexiletine and lidocaine, the steady-state fast and slow inactivation of Nav1.5 and Nav1.7 were significantly shifted to hyperpolarized direction by either mexiletine or lidocaine in dose-dependent manner. Both mexiletine and lidocaine enhanced the slow component of closed-state inactivation, with mexiletine exerting stronger inhibition on either Nav1.5 or Nav1.7. The recovery from inactivation of Nav1.5 or Nav1.7 was significantly prolonged by mexiletine compared to lidocaine. Furthermore, mexiletine displayed a pronounced and prominent use-dependent inhibition of Nav1.5 than lidocaine, but not Nav1.7 channels. Taken together, our findings demonstrate differential responses to blockade by mexiletine and lidocaine that preferentially affect the gating of Nav1.5, as compared to Nav1.7; and mexiletine exhibits stronger use-dependent block of Nav1.5. The differential gating properties of Nav1.5 and Nav1.7 in response to mexiletine and lidocaine may help explain the drug effectiveness and advance in new designs of safe and specific sodium channel blockers for treatment of cardiac arrhythmia or pain.

  4. Comparison of Gating Properties and Use-Dependent Block of Nav1.5 and Nav1.7 Channels by Anti-Arrhythmics Mexiletine and Lidocaine.

    Directory of Open Access Journals (Sweden)

    Ying Wang

    Full Text Available Mexiletine and lidocaine are widely used class IB anti-arrhythmic drugs that are considered to act by blocking voltage-gated open sodium currents for treatment of ventricular arrhythmias and relief of pain. To gain mechanistic insights into action of anti-arrhythmics, we characterized biophysical properties of Nav1.5 and Nav1.7 channels stably expressed in HEK293 cells and compared their use-dependent block in response to mexiletine and lidocaine using whole-cell patch clamp recordings. While the voltage-dependent activation of Nav1.5 or Nav1.7 was not affected by mexiletine and lidocaine, the steady-state fast and slow inactivation of Nav1.5 and Nav1.7 were significantly shifted to hyperpolarized direction by either mexiletine or lidocaine in dose-dependent manner. Both mexiletine and lidocaine enhanced the slow component of closed-state inactivation, with mexiletine exerting stronger inhibition on either Nav1.5 or Nav1.7. The recovery from inactivation of Nav1.5 or Nav1.7 was significantly prolonged by mexiletine compared to lidocaine. Furthermore, mexiletine displayed a pronounced and prominent use-dependent inhibition of Nav1.5 than lidocaine, but not Nav1.7 channels. Taken together, our findings demonstrate differential responses to blockade by mexiletine and lidocaine that preferentially affect the gating of Nav1.5, as compared to Nav1.7; and mexiletine exhibits stronger use-dependent block of Nav1.5. The differential gating properties of Nav1.5 and Nav1.7 in response to mexiletine and lidocaine may help explain the drug effectiveness and advance in new designs of safe and specific sodium channel blockers for treatment of cardiac arrhythmia or pain.

  5. Axillary block duration and related hemodynamic changes: high versus low dose Adrenaline addition to Lidocaine

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    Shariat Moharari R

    2009-03-01

    Full Text Available "nBackground: Axillary block is used for inducing anesthesia in outpatient hand and forearm surgeries. Few researches have studied hemodynamic and blockade effects of low doses of Epinephrine. The aim of the present study was to compare the duration of analgesia and hemodynamic changes following the injection of high/low epinephrine doses in such surgeries. "nMethods: The present randomized clinical trial study was conducted on healthy individuals (ASA I-II who were candidates for hand and forearm surgeries. The patients were randomly divided into three groups. The first two groups were allocated to receive lidocaine with low (0.6µg/cc and high (5µg/cc doses of epinephrine whereas lidocaine plus normal saline was injected in the third group. The hemodynamic changes (Mean arterial blood pressure and heart rate and the occurance of any side-effects along with the duration of analgesia and motor block were recorded. "nResults: From among the total of 75 patients, 15 cases were excluded due to incomplete blockade or failure needing general anesthesia. The duration of analgesia and the motor block were longer in the high dose epinephrine group, the difference, however, was not statistically significant. Heart rate changes within the groups was significant in the 4th-7th and 10th minutes. Mean arterial blood pressure changes was only significant in the 4th minute, within the groups. "nConclusions: Administering low doses of epinephrine plus lidocaine as a local anesthetic not only provides acceptable analgesia compared to higher doses of the medication, but also is associated with fewer side effects.

  6. Nematocyst discharge in Pelagia noctiluca (Cnidaria, Scyphozoa) oral arms can be affected by lidocaine, ethanol, ammonia and acetic acid.

    Science.gov (United States)

    Morabito, Rossana; Marino, Angela; Dossena, Silvia; La Spada, Giuseppa

    2014-06-01

    Nematocyst discharge and concomitant delivery of toxins is triggered to perform both defence and predation strategies in Cnidarians, and may lead to serious local and systemic reactions in humans. Pelagia noctiluca (Cnidaria, Scyphozoa) is a jellyfish particularly abundant in the Strait of Messina (Italy). After accidental contact with this jellyfish, not discharged nematocysts or even fragments of tentacles or oral arms may tightly adhere to the human skin and, following discharge, severely increase pain and the other adverse consequences of the sting. The aim of the present study is to verify if the local anesthetic lidocaine and other compounds, like alcohols, acetic acid and ammonia, known to provide pain relief after jellyfish stings, may also affect in situ discharge of nematocysts. Discharge was induced by a combined physico-chemical stimulation of oral arms by chemosensitizers (such as N-acetylated sugars, aminoacids, proteins and nucleotides), in the presence or absence of 1% lidocaine, 70% ethanol, 5% acetic acid or 20% ammonia, followed by mechanical stimulation by a non-vibrating test probe. The above mentioned compounds failed to induce discharge per se, and dramatically impaired the chemosensitizer-induced discharge response. We therefore suggest that prompt local treatment of the stung epidermis with lidocaine, acetic acid, ethanol and ammonia may provide substantial pain relief and help in reducing possible harmful local and systemic adverse reaction following accidental contact with P. noctiluca specimens.

  7. Phospholipid microemulsion-based hydrogel for enhanced topical delivery of lidocaine and prilocaine: QbD-based development and evaluation.

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    Negi, Poonam; Singh, Bhupinder; Sharma, Gajanand; Beg, Sarwar; Raza, Kaisar; Katare, Om Prakash

    2016-01-01

    Topical delivery of local anesthetics has been an area of interest for researchers considering the barrier properties of skin and unfavorable physicochemical properties of drugs. In the present study, efforts have been made to modify the in vivo efficacy of eutectic mixture of lidocaine and prilocaine by exploiting the phospholipid modified microemulsion based delivery systems. The strategic QbD (D-optimal mixture design) enabled systematic optimization approach, after having obtained the isotropic area of interest by ternary phase diagram, has resulted into the system with most desirable attributes. Latter include nano-scale, globular structures with an average size of 40.6 nm, as characterized by TEM and DLS. The optimized microemulsion systems in gel dosage forms revealed the better permeability over commercial cream (CC) through abdominal rat skin. Enhancement in the flux from MOPT-NMP gel was 3.22-folds for prilocaine and 4.94-folds for lidocaine, in comparison to that of CC. This enhanced skin permeability is very well reflected in the in vivo studies, wherein intensity and duration of action was augmented significantly. The skin compliance of the optimized formulation was revealed in histopathological studies. The overall benefit relating to efficacy and safety-compliance could be correlated to the uniqueness of the carriers, composed of phospholipids and other components. Hence, the developed phospholipid-microemulsion based gel formulation has been proposed as more useful alternative for the topical delivery of lidocaine and prilocaine.

  8. Manipulations of extracellular Loop 2 in α1 GlyR ultra-sensitive ethanol receptors (USERs) enhance receptor sensitivity to isoflurane, ethanol, and lidocaine, but not propofol.

    Science.gov (United States)

    Naito, A; Muchhala, K H; Trang, J; Asatryan, L; Trudell, J R; Homanics, G E; Alkana, R L; Davies, D L

    2015-06-25

    We recently developed ultra-sensitive ethanol receptors (USERs) as a novel tool for investigation of single receptor subunit populations sensitized to extremely low ethanol concentrations that do not affect other receptors in the nervous system. To this end, we found that mutations within the extracellular Loop 2 region of glycine receptors (GlyRs) and γ-aminobutyric acid type A receptors (GABAARs) can significantly increase receptor sensitivity to micro-molar concentrations of ethanol resulting in up to a 100-fold increase in ethanol sensitivity relative to wild-type (WT) receptors. The current study investigated: (1) Whether structural manipulations of Loop 2 in α1 GlyRs could similarly increase receptor sensitivity to other anesthetics; and (2) If mutations exclusive to the C-terminal end of Loop 2 are sufficient to impart these changes. We expressed α1 GlyR USERs in Xenopus oocytes and tested the effects of three classes of anesthetics, isoflurane (volatile), propofol (intravenous), and lidocaine (local), known to enhance glycine-induced chloride currents using two-electrode voltage clamp electrophysiology. Loop 2 mutations produced a significant 10-fold increase in isoflurane and lidocaine sensitivity, but no increase in propofol sensitivity compared to WT α1 GlyRs. Interestingly, we also found that structural manipulations in the C-terminal end of Loop 2 were sufficient and selective for α1 GlyR modulation by ethanol, isoflurane, and lidocaine. These studies are the first to report the extracellular region of α1 GlyRs as a site of lidocaine action. Overall, the findings suggest that Loop 2 of α1 GlyRs is a key region that mediates isoflurane and lidocaine modulation. Moreover, the results identify important amino acids in Loop 2 that regulate isoflurane, lidocaine, and ethanol action. Collectively, these data indicate the commonality of the sites for isoflurane, lidocaine, and ethanol action, and the structural requirements for allosteric modulation on

  9. Cardiorespiratory and antinociceptive effects of two different doses of lidocaine administered to horses during a constant intravenous infusion of xylazine and ketamine

    Science.gov (United States)

    2013-01-01

    Background This study investigated the antinociceptive effects of a constant rate infusion (CRI) of lidocaine during xylazine and ketamine anesthesia in horses and aimed to correlate these effects with cardiorespiratory variables, bispectral index (BIS) and plasma lidocaine concentrations. Six adult crossbred mares weighing 320–400 kg were anesthetized on three different occasions. Sedation was performed with xylazine (0.75 mg/kg IV) and anesthetic induction with guaifenesin (75 mg/kg IV) and ketamine (2 mg/kg IV). Anesthesia was maintained with 37.5 μg/kg/min of xylazine and 87.5 μg/kg/min of ketamine both administered intravenously for 75 min. The three treatments consisted of: lidocaine (loading dose: 5 mg/kg, CRI: 100 μg/kg/min; THL); lidocaine (loading dose: 2.5 mg/kg; CRI: 50 μg/kg/min: TLL); and saline (TS); all given 15 min after induction and maintained for 1 h. Antinociception was measured by response to electrical stimulation and bispectral index (BIS) was recorded during anesthesia. Parametric and non-parametric data were compared using ANOVA followed by Student-Newman-Keuls and Friedman tests, respectively. Results Plasma lidocaine concentrations peaked at the end of lidocaine loading dose and was greater in THL (9.61 ± 2.75 μg/mL) vs TLL (4.50 ± 3.34 μg/mL). Electrical noxious stimulation caused purposeful movement in all horses from TS, but no response in THL. The BIS was decreased in THL only and was less when compared to the other treatments throughout anesthesia. Blood pressure, PaO2 and PaCO2 increased and heart rate (HR), respiratory rate (RR), pH, total plasma protein and temperature decreased during anesthesia in all treatments. PaCO2 and HR were greater and RR and pH less in THL compared to TLL and TS at 30 min during anesthesia. All recoveries were considered excellent. Time to standing was longer after THL (60 ± 20 min) than following TLL and TS (32 ± 17 and 30 ± 15 min, respectively

  10. Guest:host interactions of lidocaine and prilocaine with natural cyclodextrins: Spectral and molecular modeling studies

    Science.gov (United States)

    Rajendiran, N.; Mohandoss, T.; Saravanan, J.

    2014-11-01

    Inclusion complex formation of two local anesthetics drugs (lidocaine (LC) and prilocaine (PC)) with α- and β-cyclodextrins (CDs) in aqueous solution were studied by absorption, fluorescence, time-resolved fluorescence and molecular modeling methods. The formation of inclusion complexes was confirmed by 1H NMR, FTIR, differential scanning calorimetry, SEM, TEM and X-ray diffractometry. Both drugs formed 1:1 inclusion complex and exhibit biexponential decay in water whereas triexponential decay in the CD solution. Nanosized self-aggregated particles of drug: CD complexes were found by TEM. Both experimental and theoretical studies revealed that the phenyl ring with the amide group of the drug is encapsulated in the hydrophobic CD nanocavity. Investigations of energetic and thermodynamic properties confirmed the stability of the inclusion complexes. van der Waals interactions are mainly responsible for enthalpy driven complex formation of LC and PC with CDs.

  11. Lidocaine for preventing postoperative sore throat.

    Science.gov (United States)

    Tanaka, Yuu; Nakayama, Takeo; Nishimori, Mina; Tsujimura, Yuka; Kawaguchi, Masahiko; Sato, Yuki

    2015-07-14

    Sore throat is a common side-effect of general anaesthesia and is reported by between 30% and 70% of patients after tracheal intubation. The likelihood of a sore throat varies with the type, diameter, and cuff pressure of the endotracheal tube used. If intubation is essential, it may be helpful to give drugs prophylactically to alleviate postoperative sore throat. Local anaesthetics and steroids have been used for this purpose. This review was originally published in 2009 and was updated in 2015. The objective of this review was to evaluate the efficacy and any harm caused by topical and systemic lidocaine used prophylactically to prevent postoperative sore throat in adults undergoing general anaesthesia with endotracheal intubation. We searched CENTRAL (The Cochrane Library 2013, Issue 9), MEDLINE (January 1966 to October 2013), and EMBASE (1980 to October 2013). We also contacted manufacturers and researchers in the field. The original search was undertaken in June 2007. We reran the search in February 2015 and found four studies of interest. We will deal with those studies when we next update the review. We included randomized controlled trials (RCTs) of topical and systemic prophylactic lidocaine therapy versus control (using air or saline) that reported on the risk and severity of postoperative sore throat as an outcome. Two authors independently assessed trial quality and extracted data. We contacted study authors for additional information, such as the risk of any adverse effects. We included 19 studies involving 1940 participants in this updated review. Of those 1940 participants, 952 received topical or systemic lidocaine therapy and 795 were allocated to the control groups. Topical and systemic lidocaine therapy appeared to reduce the risk of postoperative sore throat (16 studies, 1774 participants, risk ratio (RR) was 0.64 (95% confidence interval (CI) 0.48 to 0.85), the quality of the evidence was low), although when only high-quality trials were

  12. Addition of lidocaine injection immediately before physiotherapy for frozen shoulder: a randomized controlled trial.

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    Wei-Chun Hsu

    Full Text Available The intraarticular injection of lidocaine immediately before a physiotherapy session may relieve pain during the stretching and mobilization of the affected joint in patients with a frozen shoulder, thus enhancing the treatment effect. To compare the effects of intraarticular injection of lidocaine plus physiotherapy to that of physiotherapy alone in the treatment of a frozen shoulder, a prospective randomized controlled trial was conducted in the rehabilitation department of a private teaching hospital. Patients with a frozen shoulder were randomized into the physiotherapy group or the lidocaine injection plus physiotherapy (INJPT group. The subjects in the INJPT group underwent injection of 3 ml of 1% lidocaine into the affected shoulder 10 to 20 minutes before each physiotherapy session. In each group, the treatment lasted 3 months. The primary outcome measures were the active and passive range of motion of the affected shoulder. The secondary outcome measures were the results of the Shoulder Disability Questionnaire, the Shoulder Pain and Disability Index, and the 36-item Short-Form Health Survey (SF-36. The outcome measures were evaluated before treatment and 1, 2, 3, 4, and 6 months after the start of treatment. The group comparisons showed significantly greater improvement in the INJPT group, mainly in active and passive shoulder range of motion in flexion and external rotation and improvements in pain and disability (P < 0.05; however, no significant group difference was seen in the SF-36 results. The intraarticular injection of lidocaine immediately before a physiotherapy session might be superior to physiotherapy alone in the treatment of a frozen shoulder. Trial registration: ClinicalTrials.gov NCT01817348.

  13. The quest for effective pain control during suture adjustment after strabismus surgery: a study evaluating supplementation of 2% lidocaine with 0.4% ropivacaine

    Directory of Open Access Journals (Sweden)

    Palte HD

    2015-01-01

    Full Text Available Howard D Palte, Kara M Cavuoto, Lalitha Sundararaman, Steven Gayer, Joyce Schiffman, Hilda CapoBascom Palmer Eye Institute, Miami, FL, USAPurpose: To determine whether the addition of 0.4% ropivacaine to the standard 2% lidocaine peribulbar anesthetic block improves pain scores during suture adjustment in patients undergoing strabismus surgery with adjustable sutures.Methods: Prospective, double-blind study of 30 adult patients aged 21–84 years scheduled for elective strabismus surgery with adjustable sutures. Patients were divided into two groups of 15 patients each based on the local anesthetic. Group A received 2% lidocaine and Group B received 2% lidocaine/0.4% ropivacaine. Pain was assessed using the visual analog scale (VAS preoperatively and at 2, 4, and 6 hours postoperatively. The Lancaster red-green test was used to measure ocular motility at the same time points.Results: The pain scores in the two groups were low and similar at all measurement intervals. The VAS for Group A versus Group B at 2 hours (1.7 versus 2.4, P=0.5 and 4 hours (3.5 versus 3.7, P=0.8 showed no benefit from the addition of ropivacaine. At 6 hours, the VAS (3.7 versus 2.7 was not statistically significant, but the 95% confidence interval indicated that ropivacaine may provide some benefit. A repeated measures ANOVA did not find a statistically significant difference in VAS scores over time (P=0.9. In addition, the duration of akinesia was comparable in both groups (P=0.7.Conclusion: We conclude that the 50:50 mixture of 2% lidocaine with 0.4% ropivacaine as compared to 2% lidocaine in peribulbar anesthetic blocks in adjustable-suture strabismus surgery does not produce significant improvements in pain control during the postoperative and adjustment phases. In addition, ropivacaine did not impair return of full ocular motility at 6 hours, which is advantageous in adjustable-suture strabismus surgery.Keywords: adjustable-suture strabismus surgery, postoperative

  14. Tolerability of NGX-4010, a capsaicin 8% dermal patch, following pretreatment with lidocaine 2.5%/prilocaine 2.5% cream in patients with post-herpetic neuralgia

    Directory of Open Access Journals (Sweden)

    Webster Lynn R

    2011-12-01

    Full Text Available Abstract Background Post-herpetic neuralgia (PHN is a common type of neuropathic pain that can severely affect quality of life. NGX-4010, a capsaicin 8% dermal patch, is a localized treatment that can provide patients with significant pain relief for up to 3 months following a single 60-minute application. The NGX-4010 application can be associated with application-site pain and in previous clinical trials pretreatment with a topical 4% lidocaine anesthetic was used to enhance tolerability. The aim of the current investigation was to evaluate tolerability of NGX-4010 after pretreatment with lidocaine 2.5%/prilocaine 2.5% anesthetic cream. Methods Twenty-four patients with PHN were pretreated with lidocaine 2.5%/prilocaine 2.5% cream for 60 minutes before receiving a single 60-minute application of NGX-4010. Tolerability was assessed by measuring patch application duration, the proportion of patients completing over 90% of the intended treatment duration, application site-related pain using the Numeric Pain Rating Scale (NPRS, and analgesic medication use to relieve such pain. Safety was assessed by monitoring adverse events (AEs and dermal irritation using dermal assessment scores. Results The mean treatment duration of NGX-4010 was 60.2 minutes and all patients completed over 90% of the intended patch application duration. Pain during application was transient. A maximum mean change in NPRS score of +3.0 was observed at 55 minutes post-patch application; pain scores gradually declined to near pre-anesthetic levels (+0.71 within 85 minutes of patch removal. Half of the patients received analgesic medication on the day of treatment; by Day 7, no patients required medication. The most common AEs were application site-related pain, erythema, edema, and pruritus. All patients experienced mild dermal irritation 5 minutes after patch removal, which subsequently decreased; at Day 7, no irritation was evident. The maximum recorded dermal assessment

  15. Hypoxic pulmonary vasoconstriction: physiology and anesthetic implications.

    Science.gov (United States)

    Lumb, Andrew B; Slinger, Peter

    2015-04-01

    Hypoxic pulmonary vasoconstriction (HPV) represents a fundamental difference between the pulmonary and systemic circulations. HPV is active in utero, reducing pulmonary blood flow, and in adults helps to match regional ventilation and perfusion although it has little effect in healthy lungs. Many factors affect HPV including pH or PCO2, cardiac output, and several drugs, including antihypertensives. In patients with lung pathology and any patient having one-lung ventilation, HPV contributes to maintaining oxygenation, so anesthesiologists should be aware of the effects of anesthesia on this protective reflex. Intravenous anesthetic drugs have little effect on HPV, but it is attenuated by inhaled anesthetics, although less so with newer agents. The reflex is biphasic, and once the second phase becomes active after about an hour of hypoxia, this pulmonary vasoconstriction takes hours to reverse when normoxia returns. This has significant clinical implications for repeated periods of one-lung ventilation.

  16. Evaluation of Analgesic Effect of Caudal Epidural Tramadol, Tramadol-Lidocaine, and Lidocaine in Water Buffalo Calves (Bubalus bubalis)

    OpenAIRE

    Ayman Atiba; Alaa Ghazy; Naglaa Gomaa; Tarek Kamal; Mustafa Shukry

    2015-01-01

    Aim of this study was to compare the analgesic effect of tramadol and a combination of tramadol-lidocaine with that produced by lidocaine administration in the epidural space in buffalo calves. In a prospective randomized crossover study, ten male buffalo calves were used to compare the epidural analgesic effect of tramadol (1 mg/kg) and tramadol-lidocaine combination (0.5 mg/kg and 0.11 mg/kg, resp.) with that produced by 2% lidocaine (0.22 mg/kg). Loss of sensation was examined by pin-prick...

  17. Effects of lidocaine and magnesium sulfate in attenuating hemodynamic response to tracheal intubation: single-center, prospective, double-blind, randomized study.

    Science.gov (United States)

    Mendonça, Fabricio Tavares; de Queiroz, Lucas Macedo da Graça Medeiros; Guimarães, Cristina Carvalho Rolim; Xavier, Alexandre Cordeiro Duarte

    Hemodynamic response to airway stimuli is a common phenomenon and its management is important to reduce the systemic repercussions. The objective of this study is to compare the efficacy of intravenous magnesium sulfate versus lidocaine on this reflex hemodynamics after laryngoscopy and tracheal intubation. This single-center, prospective, double-blind, randomized study evaluated 56 patients ASA 1 or 2, aged 18-65 years, scheduled for elective surgeries under general anesthesia with intubation. The patients were allocated into two groups: Group F received 30mg·kg(-1) of magnesium sulphate and Group L, 2mg·kg(-1) of lidocaine, continuous infusion, immediately before the anesthetic induction. Blood pressure (BP), heart rate (HR), and bispectral index (BIS) were measured in both groups at six different times related to administration of the study drugs. In both groups there was an increase in HR and BP after laryngoscopy and intubation, compared to baseline. Group M showed statistically significant increase in the values of systolic and diastolic blood pressure after intubation, which was clinically unimportant. There was no difference in the BIS values between groups. Among patients receiving magnesium sulfate, three (12%) had high blood pressure versus only one among those receiving lidocaine (4%), with no statistical difference. Magnesium sulfate and lidocaine have good efficacy and safety for hemodynamic management in laryngoscopy and intubation. Copyright © 2016 Sociedade Brasileira de Anestesiologia. Published by Elsevier Editora Ltda. All rights reserved.

  18. [Cervical epidural anesthesia for upper extremity surgery using three different formulations of local anesthetics].

    Science.gov (United States)

    Guevara-López, Uriah; Bárcenas-Olivares, Juan; Gutiérrez-Sougarret, Bernardo; Aldrete, J Antonio; Olascoaga-Ortega, Gabriela

    2005-01-01

    To evaluate the efficiency and safety of the cervical epidural blockade (CEB) in upper extremity surgery, using lidocaine 2%, bupivacaine 5% and a mixture of both local analgesics. Eighty five patients were submitted to upper limb surgery under CEB. They were assigned into one of three groups: group I received 100 mg of 2% lidocaine; group II received 30 mg of 0.5% bupivacaine, and group III received a mixture of 60 mg of 2% lidocaine and 15 mg of 0.5% bupivacaine. We evaluated their effects on vital signs, blockade quality, adverse effects, and patient comfort. Anesthesiologist and surgeon evaluated the technique as "good" in 80% of the patients. Significant differences were found for motor blockade. Group II developed complete motor block (100%). Observed adverse effects were vomiting in groups II and III and dural puncture was present in 6.7% of the cases in group II. This study confirms the safety of cervical epidural anesthesia for upper limb surgery using three different formulations of local anesthetics.

  19. Inhibition of serotonin transporters by cocaine and meprylcaine through 5-TH2C receptor stimulation facilitates their seizure activities.

    Science.gov (United States)

    Morita, Katsuya; Hamamoto, Masahiro; Arai, Shigeaki; Kitayama, Shigeo; Irifune, Masahiro; Kawahara, Michio; Kihira, Kenji; Dohi, Toshihiro

    2005-09-28

    The present study examined whether the inhibition of serotonin transporters (SERT) contributes to cocaine- and other local anesthetics-induced convulsions, and which subtypes of 5-HT receptor are involved in the convulsions. For this purpose, cocaine, meprylcaine and lidocaine, all of which have different effects on SERT, were used as convulsants and the effects of serotonin reuptake inhibitors (SSRIs), specific agonists and antagonists for 5-HT receptor subtypes were evaluated in mice. Administration of SSRI, zimelidine, citalopram and fluoxetine, 5-HT(2A,2C) receptor agonist, R(-)-DOI and the 5-HT2C receptor agonists, mCPP, and MK212 resulted in a marked increase in incidence of convulsions and a reduction in the threshold of lidocaine-induced convulsions, while the 5-HT2B receptor agonist, BW723C86, had little influence. On the other hand, SSRI did not affect the measured parameters in meprylcaine- and cocaine-induced convulsions. R(-)-DOI, mCPP, and MK212 reduced the threshold of meprylcaine or cocaine with less extent than the reduction of lidocaine threshold. Incidence of cocaine- and meprylcaine-induced convulsions was significantly reduced by 5-HT(2A,2B,2C) antagonist, LY-53857, and 5-HT2C antagonist, RS 102221. The threshold of cocaine and meprylcaine was significantly increased by both antagonists. 5-HT2A antagonists MDL 11,939 and ketanserin, and 5-HT2B antagonist SB 204741 except at high doses had little effect on cocaine- and meprylcaine-induced convulsions. None of these antagonists altered the parameters of lidocaine-induced convulsions. Pretreatment with fluoxetine but not citalopram increased the plasma concentration of lidocaine. These results suggest that the increase of serotonergic neuronal activity through 5-HT2C receptor stimulation was responsible for increased activity of local anesthetics-induced convulsions and support the involvement of this mechanism in cocaine- and meprylcaine- but not in lidocaine-induced convulsions through their

  20. Effects of single injection of local anesthetic agents on intervertebral disc degeneration: ex vivo and long-term in vivo experimental study.

    Directory of Open Access Journals (Sweden)

    Koji Iwasaki

    Full Text Available Analgesic discography (discoblock can be used to diagnose or treat discogenic low back pain by injecting a small amount of local anesthetics. However, recent in vitro studies have revealed cytotoxic effects of local anesthetics on intervertebral disc (IVD cells. Here we aimed to investigate the deteriorative effects of lidocaine and bupivacaine on rabbit IVDs using an organotypic culture model and an in vivo long-term follow-up model.For the organotypic culture model, rabbit IVDs were harvested and cultured for 3 or 7 days after intradiscal injection of local anesthetics (1% lidocaine or 0.5% bupivacaine. Nucleus pulposus (NP cell death was measured using confocal microscopy. Histological and TUNEL assays were performed. For in vivo study, each local anesthetic was injected into rabbit lumbar IVDs under a fluoroscope. Six or 12 months after the injection, each IVD was prepared for magnetic resonance imaging (MRI and histological analysis.In the organotypic culture model, both anesthetic agents induced time-dependent NP cell death; when compared with injected saline solution, significant effects were detected within 7 days. Compared with the saline group, TUNEL-positive NP cells were significantly increased in the bupivacaine group. In the in vivo study, MRI analysis did not show any significant difference. Histological analysis revealed that IVD degeneration occurred to a significantly level in the saline- and local anesthetics-injected groups compared with the untreated control or puncture-only groups. However, there was no significant difference between the saline and anesthetic agents groups.In the in vivo model using healthy IVDs, there was no strong evidence to suggest that discoblock with local anesthetics has the potential of inducing IVD degeneration other than the initial mechanical damage of the pressurized injection. Further studies should be performed to investigate the deteriorative effects of the local injection of analgesic agents

  1. Evaluation of the Efficacy and Safety of a Lidocaine and Tetracaine (7%/7%) Cream for Induction of Local Dermal Anesthesia for Facial Soft Tissue Augmentation with Hyaluronic Acid

    OpenAIRE

    Cohen, Joel L.; Gold, Michael H.

    2014-01-01

    Injection of dermal fillers for soft tissue augmentation is a minimally invasive cosmetic procedure with growing popularity. However, patients often express concern about pain with such procedures. A topical anesthetic cream formulated with lidocaine/tetracaine 7%7% was approved by the United States Food and Drug Administration in 2006 and recently reintroduced to the market for use during superficial dermatological procedures. A Phase 3 study was conducted to assess the efficacy and safety o...

  2. Local anesthetic effects of cocaethylene and isopropylcocaine on rat peripheral nerves.

    Science.gov (United States)

    Tokuno, Hajime A; Bradberry, Charles W; Everill, Brian; Agulian, Samuel K; Wilkes, Steven; Baldwin, Ronald M; Tamagnan, Gilles D; Kocsis, Jeffery D

    2004-01-23

    Cocaethylene is a naturally occurring cocaine derivative that has been used as a tool in both clinical studies of cocaine reward and as a potential model compound for agonist substitution therapy in cocaine dependence. It is equipotent to cocaine at inhibiting dopamine uptake in-vitro and in-vivo. Because it has been reported that local anesthetic properties may influence the reinforcing effects of dopamine uptake inhibitors, we investigated the local anesthetic properties of cocaethylene as well as isopropylcocaine, another potential pharmacological tool in studies of cocaine reward and agonist substitution therapy. We compared the efficacy of nerve impulse blockade by lidocaine, cocaine, cocaethylene and isopropylcocaine using rat sciatic nerves and dorsal roots (DRs). Nerves were placed in a modified sucrose gap chamber and repetitively stimulated at high frequency. The amplitude of compound action potentials (CAPs) at the beginning and end of each stimulus train was measured before and after exposure to each compound. All compounds produced concentration-dependent and use-dependent decrements in CAP amplitude, but cocaethylene and isopropylcocaine at medium to high concentration (0.375-1.875 mM) showed a more prolonged block after washout relative to cocaine or lidocaine. Patch clamp studies on dorsal root ganglion (DRG) neurons indicated a use-dependent blockade of sodium channels. These studies provide a more complete understanding of the pharmaocology of potential agonist treatment candidates, and suggest a mechanism whereby cocaethylene produces a decreased euphoria in humans compared to cocaine.

  3. 21 CFR 522.810 - Embutramide, chloroquine, and lidocaine solution.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Embutramide, chloroquine, and lidocaine solution. 522.810 Section 522.810 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN... ANIMAL DRUGS § 522.810 Embutramide, chloroquine, and lidocaine solution. (a) Specifications....

  4. 21 CFR 862.3555 - Lidocaine test system.

    Science.gov (United States)

    2010-04-01

    ... lidocaine, an antiarrythmic and anticonvulsant drug, in serum and plasma. Measurements obtained by this... 21 Food and Drugs 8 2010-04-01 2010-04-01 false Lidocaine test system. 862.3555 Section 862.3555 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED...

  5. Isothermal crystallization kinetics of lidocaine in supersaturated lidocaine/polyacrylate pressure sensitive adhesive systems.

    Science.gov (United States)

    Cui, Yong; Frank, Sylvan G

    2005-09-01

    Isothermal crystallization of lidocaine (LC) in supersaturated LC/Duro-Tak 87-2287 (DT2287) polyacrylate pressure sensitive adhesive (PSA) systems has been studied by differential scanning calorimetry (DSC). It was found that crystallization of LC in supersaturated LC/DT2287 systems was governed by the nucleation process, which in turn was dependent on temperature and composition of the systems. A critical temperature T(crit) was found at approximately 26 degrees C, above which the crystallization of LC in LC/DT2287 systems becomes slow. The lack of dependence of T(crit) on the composition of the mixtures indicates that the presence of the PSA affected the kinetics (diffusion) rather than the thermodynamics of the nucleation process. A critical degree of saturation S(crit) of approximately 4 was also found, above which the nucleation rate sharply increases. Kinetic analysis based on the classical theory of nucleation indicates that nucleation of LC in the PSA medium is a diffusion-controlled process. The activation energy of crystallization had a two-phase dependence on temperature suggesting that the mechanism of crystallization may change at the transition temperatures. As the weight fraction of LC increased in the systems, the activation energy of crystallization, DeltaG(c), was minimal at approximately 15 degrees C, indicating that the nucleation of LC in the LC/DT2287 systems is at its fastest rate around this temperature. These fundamental analyses of nucleation and crystallization mechanisms are of practical significance in the design of supersaturated drug delivery systems.

  6. Diclofenac plus lidocaine gel for pain relief during intrauterine device insertion. A randomized, double-blinded, placebo-controlled study.

    Science.gov (United States)

    Fouda, Usama M; Salah Eldin, Noha M; Elsetohy, Khaled A; Tolba, Hoda A; Shaban, Mona M; Sobh, Sherin M

    2016-06-01

    To determine the effectiveness of diclofenac potassium combined with 2% lidocaine gel in reducing the pain of intrauterine device (IUD) insertion. We randomized 90 parous women requesting copper T380A IUD insertion in a 1:1 ratio to active or placebo treatment. Active treatment included administration of two 50-mg diclofenac potassium tablets 1h before IUD insertion, application of 3mL of 2% lidocaine gel on the anterior cervical lip 3min before IUD insertion and placement of a cotton swab soaked in 2% lidocaine gel in the cervical canal 3min before IUD insertion. Women in the placebo group received placebo tablets and gel. Participants assessed pain intensity using a 10-cm visual analog scale (VAS). We considered a 2-cm difference in VAS pain score between both groups during IUD insertion to be a clinically significant difference. Subjects receiving active treatment, as compared to placebo, experienced less pain during tenaculum placement (1.66±0.85 vs. 2.33±1.19, p=.003) and IUD insertion (3.14±0.92 vs. 3.94±1.3, p=.001). Women who delivered only by cesarean section had higher pain scores with IUD insertion compared with women with previous vaginal deliveries (4.41±1.24 vs. 3.29±1.05, p=.001). Diclofenac potassium combined with 2% lidocaine gel slightly reduced pain scores during tenaculum application and copper IUD insertion in parous women; however, the reduction in pain scores lacked clinical significance. Although we found a statistically significant lowering of pain scores with pretreatment with diclofenac potassium and lidocaine gel in parous women having copper IUD placement, the reduction is not clinically relevant. These findings may be more relevant for nulliparous women who experience more pain than parous women with IUD insertion and support studies of diclofenac potassium and lidocaine gel in this population. Copyright © 2016 Elsevier Inc. All rights reserved.

  7. Memory-impairing effects of local anesthetics in an elevated plus-maze test in mice

    Directory of Open Access Journals (Sweden)

    S.L. Blatt

    1998-04-01

    Full Text Available Post-training intracerebroventricular administration of procaine (20 µg/µl and dimethocaine (10 or 20 µg/µl, local anesthetics of the ester class, prolonged the latency (s in the retention test of male and female 3-month-old Swiss albino mice (25-35 g body weight; N = 140 in the elevated plus-maze (mean ± SEM for 10 male mice: control = 41.2 ± 8.1; procaine = 78.5 ± 10.3; 10 µg/µl dimethocaine = 58.7 ± 12.3; 20 µg/µl dimethocaine = 109.6 ± 5.73; for 10 female mice: control = 34.8 ± 5.8; procaine = 55.3 ± 13.4; 10 µg/µl dimethocaine = 59.9 ± 12.3 and 20 µg/µl dimethocaine = 61.3 ± 11.1. However, lidocaine (10 or 20 µg/µl, an amide class type of local anesthetic, failed to influence this parameter. Local anesthetics at the dose range used did not affect the motor coordination of mice exposed to the rota-rod test. These results suggest that procaine and dimethocaine impair some memory process(es in the plus-maze test. These findings are interpreted in terms of non-anesthetic mechanisms of action of these drugs on memory impairment and also confirm the validity of the elevated plus-maze for the evaluation of drugs affecting learning and memory in mice

  8. Heart rate effects of intraosseous injections using slow and fast rates of anesthetic solution deposition.

    Science.gov (United States)

    Susi, Louis; Reader, Al; Nusstein, John; Beck, Mike; Weaver, Joel; Drum, Melissa

    2008-01-01

    The authors, using a crossover design, randomly administered, in a single-blind manner, 3 primary intraosseous injections to 61 subjects using: the Wand local anesthetic system at a deposition rate of 45 seconds (fast injection); the Wand local anesthetic system at a deposition rate of 4 minutes and 45 seconds (slow injection); a conventional syringe injection at a deposition rate of 4 minutes and 45 seconds (slow injection), in 3 separate appointments spaced at least 3 weeks apart. A pulse oximeter measured heart rate (pulse). The results demonstrated the mean maximum heart rate was statistically higher with the fast intraosseous injection (average 21 to 28 beats/min increase) than either of the 2 slow intraosseous injections (average 10 to 12 beats/min increase). There was no statistically significant difference between the 2 slow injections. We concluded that an intraosseous injection of 1.4 mL of 2% lidocaine with 1 : 100,000 epinephrine with the Wand at a 45-second rate of anesthetic deposition resulted in a significantly higher heart rate when compared with a 4-minute and 45-second anesthetic solution deposition using either the Wand or traditional syringe.

  9. Application of a three-microneedle device for the delivery of local anesthetics

    Directory of Open Access Journals (Sweden)

    Ishikawa K

    2015-04-01

    Full Text Available Kayoko Ishikawa,1 Hidekazu Fukamizu,1 Tetsuya Takiguchi,1 Yusuke Ohta,1 Yoshiki Tokura2 1Department of Plastic and Reconstructive Surgery, Hamamatsu University School of Medicine, Hamamatsu, Japan; 2Department of Dermatology, Hamamatsu University School of Medicine, Hamamatsu, Japan Purpose: We investigated the effectiveness of a newly developed device for the delivery of local anesthetics in the treatment of axillary osmidrosis and hyperhidrosis. We developed a device with three fine, stainless steel needles fabricated with a bevel angle facing outside (“three-microneedle device” [TMD] to release a drug broadly and homogeneously into tissue in the horizontal plane. Use of this device could reduce the risk of complications when transcutaneous injections are undertaken.Patients and methods: Sixteen Japanese patients were enrolled. The mean volume of lidocaine hydrochloride per unit area needed to elicit anesthesia when using a TMD was compared with that the volume required when using a conventional 27-gauge needle. The visual analog scale (VAS score of needlestick pain and injection-associated pain was also compared.Results: The mean volume of lidocaine hydrochloride per unit area to elicit anesthesia using the TMD was significantly lower than that the volume required when using the conventional 27-gauge needle. The VAS score of needlestick pain for the TMD was significantly lower than that the VAS score for the 27-gauge needle.Conclusion: These data suggest that the TMD could be useful for the delivery of local anesthetics in terms of clinical efficacy and avoidance of adverse effects. Keywords: three-microneedle device, transcutaneous drug delivery, local anesthesia, lidocaine, pain

  10. Effects of local anesthetics on Na+ channels containing the equine hyperkalemic periodic paralysis mutation.

    Science.gov (United States)

    Sah, R L; Tsushima, R G; Backx, P H

    1998-08-01

    We examined the ability of local anesthetics to correct altered inactivation properties of rat skeletal muscle Na+ channels containing the equine hyperkalemic periodic paralysis (eqHPP) mutation when expressed in Xenopus oocytes. Increased time constants of current decay in eqHPP channels compared with wild-type channels were restored by 1 mM benzocaine but were not altered by lidocaine or mexiletine. Inactivation curves, which were determined by measuring the dependence of the relative peak current amplitude after depolarization to -10 mV on conditioning prepulse voltages, could be shifted in eqHPP channels back toward that observed for wild-type (WT) channels using selected concentrations of benzocaine, lidocaine, and mexiletine. Recovery from inactivation at -80 mV (50-ms conditioning pulse) in eqHPP channels followed a monoexponential time course and was markedly accelerated compared with wild-type channels (tauWT = 10.8 +/- 0.9 ms; taueqHPP = 2.9 +/- 0.4 ms). Benzocaine slowed the time course of recovery (taueqHPP,ben = 9.6 +/- 0.4 ms at 1 mM) in a concentration-dependent manner. In contrast, the recovery from inactivation with lidocaine and mexiletine had a fast component (taufast,lid = 3.2 +/- 0.2 ms; taufast,mex = 3.1 +/- 0.2 ms), which was identical to the recovery in eqHPP channels without drug, and a slow component (tauslow,lid = 1,688 +/- 180 ms; tauslow,mex = 2,323 +/- 328 ms). The time constant of the slow component of the recovery from inactivation was independent of the drug concentration, whereas the fraction of current recovering slowly depended on drug concentrations and conditioning pulse durations. Our results show that local anesthetics are generally incapable of fully restoring normal WT behavior in inactivation-deficient eqHPP channels.

  11. Monitoring Lidocaine Single-Crystal Dissolution by Ultraviolet Imaging

    DEFF Research Database (Denmark)

    Ostergaard, Jesper; Ye, Fengbin; Rantanen, Jukka

    2011-01-01

    Dissolution critically affects the bioavailability of Biopharmaceutics Classification System class 2 compounds. When unexpected dissolution behaviour occurs, detailed studies using high information content technologies are warranted. In the present study, an evaluation of real‐time ultraviolet (UV......) imaging for conducting single‐crystal dissolution studies was performed. Using lidocaine as a model compound, the aim was to develop a setup capable of monitoring and quantifying the dissolution of lidocaine into a phosphate buffer, pH 7.4, under stagnant conditions. A single crystal of lidocaine...... was placed in the quartz dissolution cell and UV imaging was performed at 254 nm. Spatially and temporally resolved mapping of lidocaine concentration during the dissolution process was achieved from the recorded images. UV imaging facilitated the monitoring of lidocaine concentrations in the dissolution...

  12. ANESTHETIC MANAGEMENT FOR A PATIENT WITH ACUTE INTERMITTENT PORPHYRIA

    Directory of Open Access Journals (Sweden)

    Nenad Savić

    2010-09-01

    Full Text Available Acute intermittent porphyria is a rare metabolic disorder resulting from a partial deficiency of porphobilinogen deaminase, enzyme in the heme biosynthetic pathway. Its inheritance is autosomal dominant. A deficiency of porphobilinogen deaminase is not sufficient by its self to produce acute intermittent porphyria, and other activating factors must also be present. These include some drugs, hormones, infection, injury and alcohol. Besides others, anesthetics have been implicated in the triggering of a number of severe porphyric reactions. Although there is no clinical evidence, the fear of hypothesized porphyrinogenicity of repetitive anesthetics exposures still remains. Despite these doubts, we report here the case of uneventful repeated exposure to anesthetics in a patient suffering from acute intermittent porphyria, within a fifteen- month period. On both occasions, the patient was safely exposed to certain anesthetics included: propofol, sevoflurane, rocuronium, midazolam and fentanyl.

  13. A prospective, randomized, double-blind comparison of 2% mepivacaine with 1 : 20,000 levonordefrin versus 2% lidocaine with 1 : 100,000 epinephrine for maxillary infiltrations.

    Science.gov (United States)

    Lawaty, Ingrid; Drum, Melissa; Reader, Al; Nusstein, John

    2010-01-01

    The purpose of this prospective, randomized, double-blind crossover study was to compare the anesthetic efficacy of 2% mepivacaine with 1 : 20,000 levonordefrin versus 2% lidocaine with 1 : 100,000 epinephrine in maxillary central incisors and first molars. Sixty subjects randomly received, in a double-blind manner, maxillary central incisor and first molar infiltrations of 1.8 mL of 2% mepivacaine with 1 : 20,000 levonordefrin and 1.8 mL of 2% lidocaine with 1 : 100,000 epinephrine at 2 separate appointments spaced at least 1 week apart. The teeth were electric pulp tested in 2-minute cycles for a total of 60 minutes. Anesthetic success (obtaining 2 consecutive 80 readings with the electric pulp tester within 10 minutes) was not significantly different between 2% mepivacaine with 1 : 20,000 levonordefrin and 2% lidocaine with 1 : 100,000 epinephrine for the central incisor and first molar. However, neither anesthetic agent provided an hour of pulpal anesthesia.

  14. Reduction of Environmental Temperature Mitigates Local Anesthetic Cytotoxicity in Bovine Articular Chondrocytes

    Directory of Open Access Journals (Sweden)

    Tarik Onur, Alexis Dang

    2014-09-01

    Full Text Available The purpose of this study was to assess whether reducing environmental temperature will lead to increased chondrocyte viability following injury from a single-dose of local anesthetic treatment. Bovine articular chondrocytes from weight bearing portions of femoral condyles were harvested and cultured. 96-well plates were seeded with 15,000 chondrocytes per well. Chondrocytes were treated with one of the following conditions: ITS Media, 1x PBS, 2% lidocaine, 0.5% bupivacaine, or 0.5% ropivacaine. Each plate was then incubated at 37°C, 23°C, or 4°C for one hour and then returned to media at 37°C. Chondrocyte viability was assessed 24 hours after treatment. Chondrocyte viability is presented as a ratio of the fluorescence of the treatment group over the average of the media group at that temperature (ratio ± SEM. At 37°C, lidocaine (0.35 ± 0.04 and bupivacaine (0.30 ± 0.05 treated chondrocytes show low cell viability when compared to the media (1.00 ± 0.03 control group (p < 0.001. Lidocaine treated chondrocytes were significantly more viable at 23°C (0.84 ± 0.08 and 4°C (0.86±0.085 than at 37°C (p < 0.001. Bupivacaine treated chondrocytes were significantly more viable at 4°C (0.660 ± 0.073 than at 37°C or 23°C (0.330 ± 0.069 (p < 0.001 and p = 0.002 respectively. Reducing the temperature from 37°C to 23°C during treatment with lidocaine increases chondrocyte viability following injury. Chondrocytes treated with bupivacaine can be rescued by reducing the temperature to 4°C.

  15. Anesthetic activity of the essential oil of Aloysia triphylla and effectiveness in reducing stress during transport of albino and gray strains of silver catfish, Rhamdia quelen.

    Science.gov (United States)

    Parodi, Thaylise V; Cunha, Mauro A; Becker, Alexssandro G; Zeppenfeld, Carla C; Martins, Dirlaine I; Koakoski, Gessi; Barcellos, Leonardo Gil; Heinzmann, Berta M; Baldisserotto, Bernardo

    2014-04-01

    This study investigated the efficacy of the essential oil (EO) of Aloysia triphylla as an anesthetic for albino and gray strains of silver catfish, Rhamdia quelen. Juveniles were exposed to concentrations between 20 and 800 μL L(-1) EO of A. triphylla to evaluate time of induction and recovery from anesthesia. In another experiment, both strains were divided into four groups such as 0 (control), 30, 40, or 50 μL L(-1) EO and transported for 5 h. The longest time for anesthetic induction and recovery was observed in the albinos. Both strains reached anesthesia in the 100-800 μL L(-1) (11.1-1.24 min) range, without mortality, being 200 μL L(-1) the best response considering time to anesthesia (5.35 min). Albinos transported with all EO concentrations showed higher values of carbon dioxide in the water of transport, but lower levels were observed in grays transported with 40 and 50 μL L(-1) EO when compared to control fish. The same concentrations did not prevent significant whole-body cortisol rise at the end of transport in the albino strain. Juveniles of both strains transported with EO presented lower ion loss to the water compared to control fish. The EO of A. triphylla is an effective anesthetic for albino and gray silver catfish. This EO increases whole-body cortisol levels in the albino strain, but as it reduces net ion loss as in the gray strain, it can be also recommended for transport.

  16. The influence of Lidocaine temperature on pain during subcutaneous injection.

    Science.gov (United States)

    Lundbom, Janne S; Tangen, Lena F; Wågø, Kathrine J; Skarsvåg, Trine I; Ballo, Solveig; Hjelseng, Tonje; Foss, Olav A; Finsen, Vilhjalmur

    2017-04-01

    Injection of local anaesthetics is an uncomfortable procedure. The purpose of this study was to determine the influence of lidocaine temperature on pain during subcutaneous injection. A randomised, double blind trial with 36 healthy volunteers was performed. Each subject received three injections of 4.5 ml 1% lidocaine subcutaneously on the abdomen; refrigerated (8 °C), at room temperature (21 °C), and warmed to body temperature (37 °C). By giving every subject injections of all three temperatures they served as their own controls. The participants were asked to evaluate the pain felt during the injection by placing a pencil mark on a 100 mm Visual Analogue Scale without intermediate markings immediately after every injection. They were told that the scale ranged from no pain to worst imaginable pain (0 = best; 100 = worst). Retrospectively the participants did a verbal assessment of the most and least painful injection. The median VAS score for the heated lidocaine was 16 (range =11-28), lidocaine at room temperature 25 (13-40) and for the cold 24 (11-35). The VAS scores for the heated lidocaine was significantly lower than for lidocaine at room temperature (p = 0.004). Also, the verbal assessment of heated lidocaine being less painful than the injection at room temperature was statistically significant (p = 0.015). Injection with lidocaine heated to around body temperature was less painful than injection with lidocaine at room temperature. There was no statistically significant difference in verbal assessment or VAS scores between the cold lidocaine and that at room temperature.

  17. [EEG bispectral index as an indicator of the electrical activity of the central nervous system in children during anesthetic maintenance and intensive care].

    Science.gov (United States)

    Lazarev, V V; Subbotin, V V

    2009-01-01

    The paper presents different investigators' data on the use of the bispectral (BIS) index in children during anesthetic maintenance and intensive care. The most of publications deal with the use of the BIS index during anesthesia with sevoflurane, which shows its high efficiency in estimating the depth of sleep. There are positive aspects in the use of the BIS index in the evaluation of sedative tolerance and central nervous system function, when brain death is diagnosed, cerebral oxygenation adequateness, etc. Data are given on the ambiguity of BIS index values in infants less than a year of age.

  18. Analysis of the action of lidocaine on insect sodium channels

    OpenAIRE

    Song, Weizhong; Silver, Kristopher S.; Du, Yuzhe; Liu, Zhiqi; Dong, Ke

    2010-01-01

    A new class of sodium channel blocker insecticides (SCBIs), which include indoxacarb, its active metabolite, DCJW, and metaflumizone, preferably block inactivated states of both insect and mammalian sodium channels in a manner similar to that by which local anesthetic (LA) drugs block mammalian sodium channels. A recent study showed that two residues in the cockroach sodium channel, F1817 and Y1824, corresponding to two key LA-interacting residues identified in mammalian sodium channels are n...

  19. Brachial plexus block using lidocaine/epinephrine or lidocaine/xylazine in fat-tailed sheep

    Directory of Open Access Journals (Sweden)

    Safoura Ghadirian

    2013-09-01

    Full Text Available This blinded, randomized experimental study was designed to evaluate the analgesic effects of adding epinephrine or xylazine to lidocaine solution for brachial plexus block (BPB in sheep. Nine healthy, fat-tailed female lambs (26.6 ± 1.5 kg were randomly allocated into three groups: lidocaine 2%, 5 mg kg-1 (LID, n = 6, lidocaine (5 mg kg-1 with epinephrine 5 μg mL-1 (LIDEP, n = 6 or lidocaine (5 mg kg-1 with xylazine 0.05 mg kg-1 (LIDXY, n = 6. Each animal was tested twice. The sheep received a total volume of 0.25 mL kg-1 for BPB. A nerve stimulator was used to locate the nerves of the brachial plexus. Onset and duration of analgesia of the forelimb were evaluated using superficial and deep pin prick and pinching of skin with a hemostat clamp. Heart and respiratory rates, and rectal temperature were recorded before and at predetermined intervals following the completion of the block. Brachial administration of LID, LIDEP or LIDXY produced forelimb analgesia within 11.3, 11.0 and 7.0 minutes, respectively. The mean duration of analgesia was 100.0 min in LID and 133.2 min in LIDEP group. The mean duration of analgesia in LIDXY group (186.8 min was significantly longer compared with LID group. In LIDEP group a significant increase in heart rate occurred 5 min after drug administration. Heart rate decreased from 35 to 80 min in sheep received LIDXY. In conclusion, the addition of xylazine to lidocaine solution for BBP provided a prolonged duration of action without any adverse effects in fat-tailed sheep.

  20. Evaluation of cranial tibial and extensor carpi radialis reflexes before and after anesthetic block in cats.

    Science.gov (United States)

    Tudury, Eduardo Alberto; de Figueiredo, Marcella Luiz; Fernandes, Thaiza Helena Tavares; Araújo, Bruno Martins; Bonelli, Marília de Albuquerque; Diogo, Camila Cardoso; Silva, Amanda Camilo; Santos, Cássia Regina Oliveira; Rocha, Nadyne Lorrayne Farias Cardoso

    2017-02-01

    Objectives This study aimed to test the extensor carpi radialis and cranial tibial reflexes in cats before and after anesthetic block of the brachial and lumbosacral plexus, respectively, to determine whether they depend on a myotatic reflex arc. Methods Fifty-five cats with a normal neurologic examination that were referred for elective gonadectomy were divided into group 1 (29 cats) for testing the extensor carpi radialis reflex, and group 2 (26 cats) for testing the cranial tibial reflex. In group 1, the extensor carpi radialis reflex was tested after anesthetic induction and 15 mins after brachial plexus block with lidocaine. In group 2, the cranial tibial, withdrawal and patellar reflexes were elicited in 52 hindlimbs and retested 15 mins after epidural anesthesia. Results In group 1, before the anesthetic block, 55.17% of the cats had a decreased and 44.83% had a normal extensor carpi radialis reflex. After the block, 68.96% showed a decreased and 27.59% a normal reflex. No cat had an increased or absent reflex before anesthetic block. In group 2, prior to the anesthetic block, 15.38% of the cats had a decreased cranial tibial reflex and 84.62% had a normal response, whereas after the block it was decreased in 26.92% and normal in 73.08% of the cats. None of the cats had an increased or absent reflex. Regarding the presence of both reflexes before and after anesthetic block, there was no significant difference at 1% ( P = 0.013). Conclusions and relevance The extensor carpi radialis and cranial tibial reflexes in cats are not strictly myotatic reflexes, as they are independent of the reflex arc, and may be idiomuscular responses. Therefore, they are not reliable for neurologic examination in this species.

  1. Lidocaine self-sacrificially improves the skin permeation of the acidic and poorly water-soluble drug etodolac via its transformation into an ionic liquid.

    Science.gov (United States)

    Miwa, Yasushi; Hamamoto, Hidetoshi; Ishida, Tatsuhiro

    2016-05-01

    Poor transdermal penetration of active pharmaceutical ingredients (APIs) impairs both bioavailability and therapeutic benefits and is a major challenge in the development of transdermal drug delivery systems. Here, we transformed a poorly water-soluble drug, etodolac, into an ionic liquid in order to improve its hydrophobicity, hydrophilicity and skin permeability. The ionic liquid was prepared by mixing etodolac with lidocaine (1:1, mol/mol). Both the free drug and the transformed ionic liquid were characterized by differential scanning colorimetry (DSC), infrared spectroscopy (IR), and saturation concentration measurements. In addition, in vitro skin-permeation testing was carried out via an ionic liquid-containing patch (Etoreat patch). The lidocaine and etodolac in ionic liquid form led to a relatively lower melting point than either lidocaine or etodolac alone, and this improved the lipophilicity/hydrophilicity of etodolac. In vitro skin-permeation testing demonstrated that the Etoreat patch significantly increased the skin permeation of etodolac (9.3-fold) compared with an etodolac alone patch, although an Etoreat patch did not increase the skin permeation of lidocaine, which was consistent with the results when using a lidocaine alone patch. Lidocaine appeared to self-sacrificially improve the skin permeation of etodolac via its transformation into an ionic liquid. The data suggest that ionic liquids composed of approved drugs may substantially expand the formulation preparation method to meet the challenges of drugs which are characterized by poor rates of transdermal absorption.

  2. 斯康杜尼与肾上腺素利多卡因在老年拔牙麻醉中的临床效果比较%Anesthesia effects of Scandonest and lidocaine on tooth extration

    Institute of Scientific and Technical Information of China (English)

    李风华

    2011-01-01

    Objective: To compare local anesthesia effect of Scandonest and lidocaine on tooth extraction. Methods: 584 elderly patients required tooth extraction were randomly divided into two groups and injected with lidocaine and Scandonest respectively. Pain during injection, effect of anesthetic and the change of blood pressure and heart rate before and after anesthesia were recorded and analyzed. Results: Scandonest was more effective than lidocaine for the anesthesia of maxilla teeth and mandibular anteriors and premolars. Lidocaine was more effective for the anesthesia of mandibular molars. Scandonest was superior to lidocaine in pain intensity. The blood pressure and heart rate remained similar before and after anesthesia. Conclusions: For elderly patients required tooth extraction, scandonest is an effective anesthetic for infiltration anaesthesia, lidocaine is an effective anesthetic for conduction anaesthesia. Both of the two anesthetic are safety for elderly patients.%目的:比较斯康杜尼与利多卡因在老年拔牙麻醉中的临床效果.方法:将584例进行拔牙治疗的老年患者随机分成2组,分别采用斯康杜尼和1/10万u肾上腺素利多卡因进行局部麻醉,观察分析患者注射时疼痛度、拔牙时麻醉效果,并监测麻醉前后患者血压、心率的变化.结果:斯康杜尼在注射时的疼痛VAS分值低于利多卡因(P<0.05).对于上颌前牙、前磨牙、磨牙,下颌前牙、前磨牙斯康杜尼的局部麻醉效果优于利多卡因(P<0.05);对于下颌磨牙利多卡因的的局部麻醉效果优于斯康杜尼(P<0.05).利多卡因和斯康杜尼注射后,患者的血压、心率与注射前无显著性差异(P<0.05).结论:对于老年拔牙患者,1/10万u肾上腺素利多卡因与斯康杜尼均具有较高的安全性,斯康杜尼局部浸润麻醉效果较好,利多卡因传导阻滞麻醉效果较好.

  3. Day-surgery patients anesthetized with propofol have less postoperative pain than those anesthetized with sevoflurane.

    LENUS (Irish Health Repository)

    Tan, Terry

    2012-02-01

    BACKGROUND: There have been recent studies suggesting that patients anesthetized with propofol have less postoperative pain compared with patients anesthetized with volatile anesthetics. METHODS: In this randomized, double-blind study, 80 patients undergoing day-case diagnostic laparoscopic gynecological surgery were either anesthetized with IV propofol or sevoflurane. The primary outcome measured was pain on a visual analog scale. RESULTS: Patients anesthetized with propofol had less pain compared with patients anesthetized with sevoflurane (P = 0.01). There was no difference in any of the other measured clinical outcomes. CONCLUSIONS: The patients anesthetized with propofol appeared to have less pain than patients anesthetized with sevoflurane.

  4. The position of the fast-inactivation gate during lidocaine block of voltage-gated Na+ channels.

    Science.gov (United States)

    Vedantham, V; Cannon, S C

    1999-01-01

    Lidocaine produces voltage- and use-dependent inhibition of voltage-gated Na+ channels through preferential binding to channel conformations that are normally populated at depolarized potentials and by slowing the rate of Na+ channel repriming after depolarizations. It has been proposed that the fast-inactivation mechanism plays a crucial role in these processes. However, the precise role of fast inactivation in lidocaine action has been difficult to probe because gating of drug-bound channels does not involve changes in ionic current. For that reason, we employed a conformational marker for the fast-inactivation gate, the reactivity of a cysteine substituted at phenylalanine 1304 in the rat adult skeletal muscle sodium channel alpha subunit (rSkM1) with [2-(trimethylammonium)ethyl]methanethiosulfonate (MTS-ET), to determine the position of the fast-inactivation gate during lidocaine block. We found that lidocaine does not compete with fast-inactivation. Rather, it favors closure of the fast-inactivation gate in a voltage-dependent manner, causing a hyperpolarizing shift in the voltage dependence of site 1304 accessibility that parallels a shift in the steady state availability curve measured for ionic currents. More significantly, we found that the lidocaine-induced slowing of sodium channel repriming does not result from a slowing of recovery of the fast-inactivation gate, and thus that use-dependent block does not involve an accumulation of fast-inactivated channels. Based on these data, we propose a model in which transitions along the activation pathway, rather than transitions to inactivated states, play a crucial role in the mechanism of lidocaine action.

  5. Anesthetic Maintenance of Thyroid Surgery

    Directory of Open Access Journals (Sweden)

    A. A. Negovsky

    2008-01-01

    Full Text Available Thyroid diseases are most common in endocrinology. Thyrotoxicosis induces dysfunction of virtually all organs and systems, the blood circulatory system being subjected to considerable changes. Cardiovascular diseases affect not only the quality of life in a patient, but significantly increase a risk from surgery that is the only radical treatment. For this reason, most authors consider thyrotoxicosis to be a contraindication to elective surgical intervention. At the same time it is known that drug compensation of thyrotoxicosis may be attained in not all patients. In this case, the results of treatment and a patient’s safety during surgery depend on the type and quality of anesthetic protection. The capabilities of anesthetic maintenance of thyroid surgery have recently expanded substantially. The paper deals with the preparation of patients with thyrotoxicosis for surgical intervention and the perioperative management of these patients. Key words: thyroid, toxic goiter, thyrotoxicosis, premedication, anesthetic mode, sevoflurane, xenon.

  6. Spreading of a Lidocaine Formulation on Microneedle-Treated Skin.

    Science.gov (United States)

    Nayak, Atul; Das, Diganta B; Chao, Tzu C; Starov, Victor M

    2015-12-01

    The spreadability of a liquid drug formulation on skin is an indication of it either remaining stationary or distributing (spreading) as a droplet. Factors determining droplet spreadability of the formulation are spreading area, diameter of the droplet base, viscosity of the liquid, contact angle, volume of droplet on skin and any others. The creation of microcavities from the application of microneedle (MN) has the potential to control droplet spreading, and hence, target specific areas of skin for drug delivery. However, there is little work that demonstrates spreading of liquid drug formulation on MN-treated skin. Below, spreading of a lidocaine hydrogel formulation and lidocaine solution (reference liquid) on porcine skin is investigated over MN-treated skin. Controlled spreadability was achieved with the lidocaine hydrogel on MN-treated skin as compared with lidocaine solution. It was observed that the droplet spreading parameters such as spreading radius, droplet height and dynamic contact angle were slightly lower for the lidocaine hydrogel than the lidocaine solution on skin. Also, the lidocaine hydrogel on MN-treated skin resulted in slower dynamic reduction of droplet height, contact angle and reduced time taken in attaining static advancing droplets because of the MN microcavities.

  7. Vestibular effects of lidocaine intratympanic injection in rats.

    Science.gov (United States)

    Lee, H H; Kim, M J; Jo, Y K; Kim, J Y; Han, G C

    2014-11-01

    When lidocaine is locally delivered into the inner ear, it rapidly paralyzes the peripheral vestibular afferent neurons and induces unilateral vestibular loss. The goals of this study were to explore the possibility of developing intratympanic injection (IT) of lidocaine as a modality for treating acute vertigo. To evaluate the minimum concentration required, latent time, action duration, and possibility of lidocaine IT readministration to the vestibular system, we compared the development of horizontal nystagmus after IT of 2, 4, 6, 8, and 10% lidocaine solutions in rats. To identify the induction of vestibular compensation, c-Fos-like protein expression was observed in the vestibular nucleus. Results of our investigation showed that lidocaine IT concentrations greater than 4% induced vestibular hyporeflexia in the injected ear. In order to induce hyporeflexia 4 and 6% lidocaine solutions could also be repeatedly injected. Regardless of concentration, effects of the lidocaine IT dissipated gradually over time. Our findings could be used to develop novel methods for symptom control in vestibular disorder patients.

  8. Procainamide and lidocaine produce dissimilar changes in ventricular repolarization and arrhythmogenicity in guinea-pig.

    Science.gov (United States)

    Osadchii, Oleg E

    2014-08-01

    Procainamide is class Ia Na(+) channel blocker that may prolong ventricular repolarization secondary to inhibition of IK r , the rapid component of the delayed rectifier K(+) current. In contrast to selective IN a blockers such as lidocaine, procainamide was shown to produce arrhythmogenic effects in the clinical setting. This study examined whether pro-arrhythmic responses to procainamide may be accounted for by drug-induced repolarization abnormalities including impaired electrical restitution kinetics, spatial gradients in action potential duration (APD), and activation-to-repolarization coupling. In perfused guinea-pig hearts, procainamide was found to prolong the QT interval on ECG and left ventricular (LV) epicardial monophasic APD, increased the maximum slope of electrical restitution, enhanced transepicardial APD variability, and eliminated the inverse correlation between the local APD and activation time values determined at distinct epicardial recording sites prior to drug infusion. In contrast, lidocaine had no effect on electrical restitution, the degree of transepicardial repolarization heterogeneities, and activation-to-repolarization coupling. Spontaneous episodes of monomorphic ventricular tachycardia were observed in 57% of procainamide-treated heart preparations. No arrhythmia was induced by lidocaine. In summary, this study suggests that abnormal changes in repolarization may contribute to pro-arrhythmic effects of procainamide.

  9. Effects of lidocaine on torn rotator cuff tendons.

    Science.gov (United States)

    Honda, Hirokazu; Gotoh, Masafumi; Kanazawa, Tomonoshin; Nakamura, Hidehiro; Ohta, Keisuke; Nakamura, Kei-Ichiro; Shiba, Naoto

    2016-09-01

    We determined lidocaine's action on torn rotator cuff tendons in vitro and in vivo. For in vitro experiments, cell proliferation and viability assays were performed using tenocytes derived from human torn rotator cuff tendons. For in vivo experiments, acute rotator cuff tears were made on the supraspinatus tendons in the rats' bilateral shoulders; before closure, lidocaine was injected into the shoulder and saline into the contralateral shoulder (control). After sacrifice, the specimens underwent biomechanical testing or histological analysis at 24 h and at 2, 4, and 8 weeks after surgery. The extent of collagen organization and apoptosis were semi-quantitatively evaluated using collagen picrosirius red staining. Apoptosis was examined using TUNEL staining and electron microscopy. Cell proliferation decreased dose-dependently. After exposure to 0.1% lidocaine for 24 h, cell viability decreased. Two and 4 weeks after surgery, the ultimate load to failure decreased more in the lidocaine group than in the control group, with significantly reduced stiffness in the lidocaine group 2 weeks after surgery. Collagen organization significantly decreased in the lidocaine group by 4 weeks after surgery but returned to baseline at 8 weeks. TUNEL staining detected numerous apoptotic tenocytes at the torn tendon edge exposed to lidocaine 24 h after surgery; electron microscopy confirmed the condensed cell nuclei. These changes were not observed in controls. Lidocaine caused cytotoxicity to tenocytes under both conditions, decreased biomechanical properties, and induced apoptosis and delay of collagen organization in this model. Subacromial lidocaine injections in patients with rotator cuff tears should be performed carefully. © 2016 Orthopaedic Research Society. Published by Wiley Periodicals, Inc. J Orthop Res 34:1620-1627, 2016.

  10. The effect of sub-anesthetic and anesthetic ketamine on water maze memory acquisition, consolidation and retrieval.

    Science.gov (United States)

    Moosavi, Maryam; Yadollahi Khales, Golnaz; Rastegar, Karim; Zarifkar, Asadollah

    2012-02-29

    Ketamine, a non-selective inhibitor of NMDA (N-methyl-D-aspartate) channels is used in anesthetic or sub-anesthetic doses to induce analgesia, amnesia, to suppress fear, anxiety and depression. Although the ketamine's effect on memory acquisition is known, its effects on other aspects of memory are controversial. Morris water maze is a task which assesses spatial learning and memory. This study was aimed to assess the ketamine's differential effect on water maze memory acquisition, consolidation and retrieval. Male Sprague-Dawley rats (250-350 g) were trained in water maze single training session. 24h later a probe trial which was consisted of a single trial without platform was done. To assess the effect of ketamine on water maze memory acquisition it was administered before training; to assess its effect on memory consolidation it was administered immediately after training and to assess its effect on memory retrieval it was injected before probe trial. Ketamine both in sub-anesthetic and anesthetic doses impaired water maze memory acquisition, its anesthetic dose but not sub-anesthetic dose impaired memory consolidation and on retrieval stage, both doses deteriorated memory retrieval. It seems that NMDA receptor activity is not just necessary during water maze memory acquisition but also their post-learning reactivation is required to maintain memory consolidation and retrieval.

  11. Brief reports: a clinical evaluation of block characteristics using one milliliter 2% lidocaine in ultrasound-guided axillary brachial plexus block.

    LENUS (Irish Health Repository)

    O'Donnell, Brian

    2010-09-01

    We report onset and duration of ultrasound-guided axillary brachial plexus block using 1 mL of 2% lidocaine with 1:200,000 epinephrine per nerve (total local anesthetic volume 4 mL). Block performance time, block onset time, duration of surgery, and block duration were measured. Seventeen consecutive patients were recruited. The mean (SD) block performance and onset times were 271 (67.9) seconds and 9.7 (3.7) minutes, respectively. Block duration was 160.8 (30.7) minutes. All operations were performed using regional anesthesia alone. The duration of anesthesia obtained is sufficient for most ambulatory hand surgery.

  12. Addition of lacal anesthetics to contrast media. Pt. 2. Increase of acute mortality in mice with intravenous contrast administration

    Energy Technology Data Exchange (ETDEWEB)

    Nilsson, P.; Almen, T.; Golman, K.; Jonsson, K.; Nyman, U.

    The acute intravenous toxicity (i.v. LD/sub 50/) of solutions of the ratio 1.5 contrast media metrizoate or diatrizoate and the ratio 3.0 contrast medium metrizamide was determined in mice with and without the addition of local anesthetics to the solutions. The two local anesthetics mepivacaine or lidocaine were added to final concentrations up to 2.0 mg/ml of the contrast medium solutions. This corresponds to clinically used concentrations. All additions of local anesthetics to the solutions increased the mortalities caused by the contrast medium solutions. Addition of local anesthetics to a final concentration of 2 mg/ml approximately doubled the acute intravenous toxicity of the contrast media. The ratio 3 contrast media produce less hypertonic solutions than the ratio 1.5 contrast media and should be preferred for angiography because they cause less pain and do not require the addition of local anesthetics which increase the acute toxicity of the solutions.

  13. Development of an ANN optimized mucoadhesive buccal tablet containing flurbiprofen and lidocaine for dental pain

    Directory of Open Access Journals (Sweden)

    Hussain Amjad

    2016-06-01

    Full Text Available A novel mucoadhesive buccal tablet containing flurbiprofen (FLB and lidocaine HCl (LID was prepared to relieve dental pain. Tablet formulations (F1-F9 were prepared using variable quantities of mucoadhesive agents, hydroxypropyl methyl cellulose (HPMC and sodium alginate (SA. The formulations were evaluated for their physicochemical properties, mucoadhesive strength and mucoadhesion time, swellability index and in vitro release of active agents. Release of both drugs depended on the relative ratio of HPMC:SA. However, mucoadhesive strength and mucoadhesion time were better in formulations, containing higher proportions of HPMC compared to SA. An artificial neural network (ANN approach was applied to optimise formulations based on known effective parameters (i.e., mucoadhesive strength, mucoadhesion time and drug release, which proved valuable. This study indicates that an effective buccal tablet formulation of flurbiprofen and lidocaine can be prepared via an optimized ANN approach.

  14. Peripheral lidocaine, but not ketamine inhibit capsaicin-induced hyperalgesia in humans

    DEFF Research Database (Denmark)

    Gottrup, Hanne; Bach, Flemming Winther; Arendt-Nielsen, Lars

    2000-01-01

    micrograms capsaicin was injected intradermally in one volar forearm 10 min after the skin had been pretreated with lidocaine 20.0 mg in 2.0 ml or 0.9% saline 2.0 ml at the capsaicin injection site. In experiment 2, a similar capsaicin test was given 10 min after the skin had been pretreated with ketamine 5......We examined the effect of the subcutaneous infiltration of ketamine, lidocaine and saline before injury on capsaicin-induced pain and hyperalgesia. Twelve healthy volunteers participated in two separate, randomized, double-blind, placebo-controlled crossover experiments. In experiment 1, 100...... mg in 2.0 ml or 0.9% saline 2.0 ml. To control for possible systemic effects, the capsaicin injection site was pretreated by injection of saline into the skin and the contralateral arm was treated with active drug, and vice versa. Outcome measures were spontaneous pain, pain evoked by punctate...

  15. Nanostructured lipid carriers as robust systems for topical lidocaine-prilocaine release in dentistry.

    Science.gov (United States)

    Ribeiro, Lígia N M; Franz-Montan, Michelle; Breitkreitz, Márcia C; Alcântara, Ana C S; Castro, Simone R; Guilherme, Viviane A; Barbosa, Raquel M; de Paula, Eneida

    2016-10-10

    In dental practice, local anesthesia causes pain, fear, and stress, and is frequently the reason that patients abandon treatment. Topical anesthetics are applied in order to minimize the discomfort caused by needle insertion and injection, and to reduce the symptoms of superficial trauma at the oral mucosa, but there are still no efficient commercially available formulations. Factorial design is a multivariate data analysis procedure that can be used to optimize the manufacturing processes of lipid nanocarriers, providing valuable information and minimizing development time. This work describes the use of factorial design to optimize a process for the preparation of nanostructured lipid carriers (NLC) based on cetyl palmitate and capric/caprylic triglycerides as structural lipids and Pluronic 68 as the colloidal stabilizer, for delivery of the local anesthetics lidocaine and prilocaine (both at 2.5%). The factors selected were the excipient concentrations, and three different responses were followed: particle size, polydispersity index and zeta potential. The encapsulation efficiency of the most effective formulations (NLC 2, 4, and 6) was evaluated by the ultrafiltration/centrifugation method. The formulations that showed the highest levels of encapsulation were tested using in vitro release kinetics experiments with Franz diffusion cells. The NLC6 formulation exhibited the best sustained release profile, with 59% LDC and 66% PLC released after 20h. This formulation was then characterized using different techniques (IR-ATR, DSC, DRX, TEM, and NTA) to obtain information about its molecular organization and its physicochemical stability, followed during 14months of storage at 25°C. This thorough pre-formulation study represents an important advance towards the development of an efficient pre-anesthetic for use in dentistry.

  16. Progress of lidocaine in the prevention of rocuronium-induced injection pain%利多卡因预防罗库溴铵静脉注射痛的研究进展

    Institute of Scientific and Technical Information of China (English)

    朱琳佳; 桂波; 蒋金娣; 钱燕宁

    2012-01-01

    Background Lidocaine,an amide local anesthetic,is often used in the prevention of injection pain induced by rocuronium.The possible mechanisms are that lidocaine can block the peripheral nerve cell membrane voltage-gated sodium channels,inhibit influx of sodium,and have membrane stabilizing action.Objective This paper intends to review the progress of lidocaine in the prevention of injection pain caused by rocuronium.Content From the mechanism of action and the comparison with other drugs,we reviewed the effects of lidocaine in the prevention of rocuronium-induced injection pain.Trend As one of the classic local anesthetics,the clinical application of lidocaine is quite promising in anesthesia.%背景 利多卡因作为酰胺类局部麻醉药,常用于预防罗库溴铵引发的静脉注射痛,可能机制为阻断外周神经细胞膜电压门控Na+通道,抑制Na+内流,产生膜稳定作用,并阻断痛觉传导通路,最终缓解注射痛.目的 本文拟对利多卡因预防罗库溴铵静脉注射痛的研究进展进行综述,为该药在临床工作中的应用提供参考. 内容 本文分别从作用机制以及同其他药物比较两个方面,综述利多卡因预防罗库溴铵注射痛的效果.趋向 利多卡因作为经典局部麻醉药之一,其在临床麻醉中具有越来越广泛的用途.

  17. Influência de anestésicos locais sobre o bloqueio neuromuscular produzido pelo rocurônio: ação da lidocaína e da mistura enantiomérica em excesso de 50% de bupivacaína na junção neuromuscular Influencia de anestésicos locales sobre el bloqueo neuromuscular producido por el rocuronio: acción de la lidocaína y de la mezcla enantiomérica en exceso de 50% de bupivacaína en la junción neuromuscular Influence of local anesthetics on the neuromuscular blockade produced by rocuronium: effects of lidocaine and 50% enantiomeric excess bupivacaine on the neuromuscular junction

    Directory of Open Access Journals (Sweden)

    Angélica de Fátima de Assunção Braga

    2009-12-01

    acción presináptica y postsináptica.BACKGROUND AND OBJECTIVES: The effects of local anesthetics (LA on neuromuscular transmission and their influence on the neuromuscular blockade produced by competitive neuromuscular blockers have not been fully investigated. The objective of this study was to evaluate, in vitro, the effects of lidocaine and 50% enantiomeric excess bupivacaine (S75-R25 on the neuromuscular blockade produced by rocuronium. METHODS: The rats were divided in five groups (n = 5 according to the drug used: isolated lidocaine, bupivacaine (S75-R25, or rocuronium (groups I, II, and II; and rocuronium in preparations previously exposed to LAs (groups IV and V. The concentrations used were as follows: 20 µg.mL-1, 5 µg.mL-1, and 4 µg.mL-1 of lidocaine, bupivacaine (S75-R25, and rocuronium, respectively. The following parameters were evaluated: 1 the strength of muscular contraction of the diaphragm to indirect electrical stimulations, before and 60 minutes after the isolated addition of the LAs and rocuronium, and the association AL-rocuronium; and 2 the effects of LAs on membrane potential (MP and miniature end-plate potentials (MEPP. The effect of LAs on muscle contraction in response to acetylcholine was evaluated in chick biventer cervicis preparations. RESULTS: Isolated lidocaine and bupivacaine (S75-R25 did not change the muscular response and the levels of MPs. In preparations exposed to LAs, rocuroniuminduced blockade was significantly greater than that produced by rocuronium alone. In chick biventer cervicis preparations, lidocaine and bupivacaine (S75R25 decreased contraction in response to acetylcholine. Lidocaine increased the frequency of MEPPs, which was followed by the blockade; bupivacaine (S75R25 caused a reduction in MEPPs followed by blockade. CONCLUSIONS: Local anesthetics caused a potentiation of the neuromuscular blockade produced by rocuronium. The results showed pre- and post-synaptic effects.

  18. Endotracheal tube cuff lidocaine is not superior to intravenous lidocaine in short pediatric surgeries.

    Science.gov (United States)

    Behzadi, Mehrdad; Hajimohamadi, Fatemeh; Alagha, Afshar Etemadi; Abouzari, Mehdi; Rashidi, Armin

    2010-05-01

    Instillation of lidocaine into the endotracheal tube cuff is a method with reported efficiency in promoting a smoother emergence from anesthesia with endotracheal intubation. However, whether or not this method is helpful in children and in surgeries with short duration has not been investigated previously. 176 ASA I-II children undergoing adenotonsillectomy were enrolled in this prospective, double-blind, randomized clinical trial. Patients were randomly allocated to two groups. Patients in the ECL group (n=88) were injected 2% lidocaine into their endotracheal tube cuff and received saline (1.5mg/kg) intravenously. The IVL group (n=88) received 1.5mg/kg of 2% lidocaine intravenously and saline into the endotracheal tube cuff. In both groups, intra-cuff injections were initiated immediately after insertion of the endotracheal tube and terminated before the cuff pressure reached 20 cmH(2)O. The parameters measured were: coughing (graded by a scale of 3 at the time of extubation), systolic and diastolic blood pressures and heart rate (from the time of extubation up to 5 min after extubation at 1-min intervals), and laryngospasm (defined as the presence of hoarseness or absence of airflow). The groups were not different in sex, age, weight, height, body mass index, anesthesia duration, and baseline hemodynamic parameters. The grade of coughing was significantly higher in the ECL group. The incidence of laryngospasm and hemodynamic trends did not differ between the groups. Our results indicate that intra-cuff lidocaine may not be beneficial in children and in surgeries with a short duration. Copyright (c) 2010 Elsevier Ireland Ltd. All rights reserved.

  19. Amide-type local anesthetics and human mesenchymal stem cells: clinical implications for stem cell therapy.

    Science.gov (United States)

    Dregalla, Ryan C; Lyons, Nicolette F; Reischling, Patrick D; Centeno, Christopher J

    2014-03-01

    In the realm of regenerative medicine, human mesenchymal stem cells (hMSCs) are gaining attention as a cell source for the repair and regeneration of tissues spanning an array of medical disciplines. In orthopedics, hMSCs are often delivered in a site-specific manner at the area of interest and may require the concurrent application of local anesthetics (LAs). To address the implications of using hMSCs in combination with anesthetics for intra-articular applications, we investigated the effect that clinically relevant doses of amide-type LAs have on the viability of bone marrow-derived hMSCs and began to characterize the mechanism of LA-induced hMSC death. In our study, culture-expanded hMSCs from three donors were exposed to the amide-type LAs ropivacaine, lidocaine, bupivacaine, and mepivacaine. To replicate the physiological dilution of LAs once injected into the synovial capsule, each anesthetic was reduced to 12.5%, 25%, and 50% of the stock solution and incubated with each hMSC line for 40 minutes, 120 minutes, 360 minutes, and 24 hours. At each time point, cell viability assays were performed. We found that extended treatment with LAs for 24 hours had a significant impact on both hMSC viability and adhesion. In addition, hMSC treatment with three of the four anesthetics resulted in cell death via apoptosis following brief exposures. Ultimately, we concluded that amide-type LAs induce hMSC apoptosis in a time- and dose-dependent manner that may threaten clinical outcomes, following a similar trend that has been established between these particular anesthetics and articular chondrocytes both in vitro and in vivo.

  20. Amide-Type Local Anesthetics and Human Mesenchymal Stem Cells: Clinical Implications for Stem Cell Therapy

    Science.gov (United States)

    Lyons, Nicolette F.; Reischling, Patrick D.; Centeno, Christopher J.

    2014-01-01

    In the realm of regenerative medicine, human mesenchymal stem cells (hMSCs) are gaining attention as a cell source for the repair and regeneration of tissues spanning an array of medical disciplines. In orthopedics, hMSCs are often delivered in a site-specific manner at the area of interest and may require the concurrent application of local anesthetics (LAs). To address the implications of using hMSCs in combination with anesthetics for intra-articular applications, we investigated the effect that clinically relevant doses of amide-type LAs have on the viability of bone marrow-derived hMSCs and began to characterize the mechanism of LA-induced hMSC death. In our study, culture-expanded hMSCs from three donors were exposed to the amide-type LAs ropivacaine, lidocaine, bupivacaine, and mepivacaine. To replicate the physiological dilution of LAs once injected into the synovial capsule, each anesthetic was reduced to 12.5%, 25%, and 50% of the stock solution and incubated with each hMSC line for 40 minutes, 120 minutes, 360 minutes, and 24 hours. At each time point, cell viability assays were performed. We found that extended treatment with LAs for 24 hours had a significant impact on both hMSC viability and adhesion. In addition, hMSC treatment with three of the four anesthetics resulted in cell death via apoptosis following brief exposures. Ultimately, we concluded that amide-type LAs induce hMSC apoptosis in a time- and dose-dependent manner that may threaten clinical outcomes, following a similar trend that has been established between these particular anesthetics and articular chondrocytes both in vitro and in vivo. PMID:24436443

  1. [Clinical anesthetic effects of epidural ropivacaine with tramadol].

    Science.gov (United States)

    Cai, Jin; Guo, Qu-Lian; Zou, Wang-Yuan

    2004-04-01

    To observe the anesthesic effects of epidural ropivacaine with tramadol during lower limbs surgery. Thirty patients (ASA I - II) scheduled for the lower limbs surgery were randomly divided into 2 groups with 15 patients in each group: group ropivacaine (R) and group ropivacaine with tramadol (T). The puncture was performed at the interspace of L2-3. Each patient was given 2% lidocaine 3 ml with 0.75% ropivacaine 10 ml which included NS 1 ml in Group R or tramadol 50 mg in Group T. The potency of analgesia, the time of sensation block to T12 and T10, the time to the highest plane of analgesia, the lasting time of analgesia, the degree of sedation, the degree of motor block, and the side effects were recorded and analyzed during anesthesia after the first dose. The time of sensation block which reached T12 and T10 and the time to the highest plane of analgesia decreased significantly in Group T than that in Group R (P 0.05). The epidural ropivacaine with tramadol enhanced the anesthetic effects of ropivacaine.

  2. Anterior and posterior tibial anesthetic block in diabetic foot surgery.

    Directory of Open Access Journals (Sweden)

    José Julio Ojeda González

    2004-12-01

    Full Text Available Fundament: Diabetes Mellitus is a disease of high and increasing prevalence and its complications follow a parallel course. Its morbidity is derived from its own complications which are produced at a long or short term and peripheral vascular disease hihglights among them.Objective: to check the usefulness of the anterior and posterior blockade of the tibia for the surgery of the diabetic foot. Method: Prospective study carried out from January to December 2003 at the University Hospital ¨Dr. Gustavo Aldereguía Lima¨ to patients who are carriers of a diabetic foot and who were initially assisted at the service of Angiology and later at the service of Anesthesiology when the surgical procedures were decided. All the patients were applied an anterior and posterior blockade of the tibial nerve . The variables measured were: age, weight, height, surgical time, type of surgery, cardiac frequency medium arterial pressure, and classification of patients according to the American Association of Anesthesiology All the patients were applied a scale for assessing pain in three different moments.Result: There was a predominance of females . The blockade of the posterior tibial nerve with lidocaine 1 % in different points permitted the performance of the surgical techniques proposed. The anesthetic procedure was favorable, and economic since the patients did not requiere of the use of analgesic in the post operatory stage.

  3. The Effect of Local Anesthetic Volume Within the Adductor Canal on Quadriceps Femoris Function Evaluated by Electromyography

    DEFF Research Database (Denmark)

    Grevstad, Ulrik; Jæger, Pia; Sørensen, Johan Kløvgaard;

    2016-01-01

    BACKGROUND: Single-injection adductor canal block (ACB) provides analgesia after knee surgery. Which nerves that are blocked by an ACB and what influence-if any-local anesthetic volume has on the effects remain undetermined. We hypothesized that effects on the nerve to the vastus medialis muscle...... (which besides being a motor nerve innervates portions of the knee) are volume-dependent. METHODS: In this assessor- and subject-blinded randomized trial, 20 volunteers were included. On 3 separate days, subjects received an ACB with different volumes (10, 20, and 30 mL) of lidocaine 1%. In addition......L was used (P = 0.0001). No statistically significant differences were found between volume and effect on the vastus lateralis (P = 0.81) or in muscle strength (P = 0.15). CONCLUSIONS: For ACB, there is a positive correlation between local anesthetic volume and effect on the vastus medialis muscle. Despite...

  4. Local anesthetic failure associated with inflammation: verification of the acidosis mechanism and the hypothetic participation of inflammatory peroxynitrite

    Directory of Open Access Journals (Sweden)

    Takahiro Ueno

    2008-11-01

    Full Text Available Takahiro Ueno1, Hironori Tsuchiya2, Maki Mizogami1, Ko Takakura11Department of Anesthesiology, Asahi University School of Dentistry, Mizuho, Gifu, Japan; 2Department of Dental Basic Education, Asahi University School of Dentistry, Mizuho, Gifu, JapanAbstract: The presence of inflammation decreases local anesthetic efficacy, especially in dental anesthesia. Although inflammatory acidosis is most frequently cited as the cause of such clinical phenomena, this has not been experimentally proved. We verified the acidosis mechanism by studying the drug and membrane lipid interaction under acidic conditions together with proposing an alternative hypothesis. Liposomes and nerve cell model membranes consisting of phospholipids and cholesterol were treated at different pH with lidocaine, prilocaine and bupivacaine (0.05%–0.2%, w/v. Their membrane-interactive potencies were compared by the induced-changes in membrane fluidity. Local anesthetics fluidized phosphatidylcholine membranes with the potency being significantly lower at pH 6.4 than at pH 7.4 (p < 0.01, supporting the acidosis theory. However, they greatly fluidized nerve cell model membranes even at pH 6.4 corresponding to inflamed tissues, challenging the conventional mechanism. Local anesthetics acted on phosphatidylserine liposomes, as well as nerve cell model membranes, at pH 6.4 with almost the same potency as that at pH 7.4, but not on phosphatidylcholine, phosphatidylethanolamine and sphingomyelin liposomes. Since the positively charged anesthetic molecules are able to interact with nerve cell membranes by ion-paring with anionic components like phosphatidylserine, tissue acidosis is not essentially responsible for the local anesthetic failure associated with inflammation. The effects of local anesthetics on nerve cell model membranes were inhibited by treating with peroxynitrite (50 μM, suggesting that inflammatory cells producing peroxynitrite may affect local anesthesia

  5. Effects of the morphine-lidocaine-ketamine combination on cardiopulmonary function and isoflurane sparing in sheep

    Directory of Open Access Journals (Sweden)

    Suzane Lilian Beier

    2014-10-01

    Full Text Available The aims of this study were to evaluate the isoflurane sparing and clinical effects of a constant rate infusion of morphine – lidocaine – ketamine (MLK in healthy sheep undergoing experimental gastrointestinal surgery. Twelve adult female sheep (Texel breed were used, weighing 36.5 ± 8.1 kg. The sheep were anesthetized for the implantation of duodenal cannulas. The sheep were premedicated with 0.3 mg kg-1 intramuscular (IM morphine and 20 ?g kg-1 intravenous (IV detomidine. After premedication, anesthesia was induced using 5 mg kg-1 ketamine and 0.5 mg kg-1 diazepam IV and maintained using isoflurane in 100% oxygen. After the induction of anesthesia, the animals were allocated into two groups (each n=6; the GMLK (MLK group – 10 mg morphine, 150 mg lidocaine, 30 mg de ketamine were added in 500 mL saline received a 10 mL kg-1h-1 MLK infusion during the maintenance of anesthesia, and GCON (control group received 10 mL kg-1h-1 of 0.9% sodium chloride. The animals were mechanically ventilated. Cardiopulmonary variables and end-tidal isoflurane concentration (FE´Iso were measured at baseline (immediately before the surgery and 15, 30 and 45 minutes after initiation of surgery. In GMLK, there was a decrease in the FE´Iso at 15, 30 and 45 minutes, a reduction of up to 75.6% during the surgery. The HR was lower in GMLK compared with GCON at 30 minutes, and the MAP was at during baseline in GCON compared with GMLK. The standing time was less in GMLK than in GCON. The use of intravenous MLK was demonstrated to offer great efficiency as part of a balanced anesthesia protocol in sheep, with a 75.6% reduction in the need for isoflurane, providing stability of the cardiovascular parameters and blood gases with a shortened recovery period.

  6. Lidocaine patches reduce pain in trauma patients with rib fractures.

    Science.gov (United States)

    Zink, Karen A; Mayberry, John C; Peck, Ellen G; Schreiber, Martin A

    2011-04-01

    Rib fracture pain is notoriously difficult to manage. The lidocaine patch is effective in other pain scenarios with an excellent safety profile. This study assesses the efficacy of lidocaine patches for treating rib fracture pain. A prospectively gathered cohort of patients with rib fracture was retrospectively analyzed for use of lidocaine patches. Patients treated with lidocaine patches were matched to control subjects treated without patches. Subjective pain reports and narcotic use before and after patch placement, or equivalent time points for control subjects, were gathered from the chart. All patients underwent long-term follow-up, including a McGill Pain Questionnaire (MPQ). Twenty-nine patients with lidocaine patches (LP) and 29 matched control subjects (C) were analyzed. During the 24 hours before patch placement, pain scores and narcotic use were similar (LP 5.3, C 4.6, P = 0.19 and LP 51, C 32 mg morphine, P = 0.17). In the 24 hours after patch placement, LP patients had a greater decrease in pain scores (LP 1.2, C 0.0, P = 0.01) with no change in narcotic use (LP -8.4, C 0.5-mg change in morphine, P = 0.25). At 60 days, LP patients had a lower MPQ pain score (LP 7.7, C 12.2, P rib fracture pain. Lidocaine patches resulted in a sustained reduction in pain, outlasting the duration of therapy.

  7. Anesthetic efficacy of the intraosseous injection in maxillary and mandibular teeth.

    Science.gov (United States)

    Coggins, R; Reader, A; Nist, R; Beck, M; Meyers, W J

    1996-06-01

    The objective of this study was to determine the anesthetic efficacy of the intraosseous injection as a primary technique in human maxillary and mandibular teeth. Forty subjects received two sets of intraosseous injections with 1.8 ml of 2% lidocaine with 1:100,000 epinephrine at two successive appointments. The experimental teeth consisted of 40 groups of maxillary and mandibular first molars and lateral incisors. Each experimental tooth and adjacent teeth were tested with an electric pulp tester at 4-minute cycles for 60 minutes. Anesthetic success was defined as no subject response to the maximum output of the pulp tester (80 reading) for two consecutive readings. Anesthetic success occurred in 75% of mandibular first molars, in 93% of maxillary first molars, in 78% of mandibular lateral incisors, and in 90% of maxillary lateral incisors. Overall, for the intraosseous injection onset was immediate, the duration of pulpal anesthesia steadily declined over the 60 minutes, there was a 78% incidence of subjective increase in heart rate, the majority of the subjects had no pain or mild pain with perforation and solution deposition, and 3% of the subjects had slow healing perforation sites. The results of this study indicate that the intraosseous injection may provide pulpal anesthesia in 75% to 93% of noninflamed teeth as a primary technique. However, the duration of pulpal anesthesia declines steadily over an hour.

  8. Genotoxicity of Anesthetics Evaluated In Vivo (Animals)

    Science.gov (United States)

    Braz, Mariana G.; Karahalil, Bensu

    2015-01-01

    The anesthesia has been improved all over the years. However, it can have impact on health, in both patients and animals anesthetized, as well as professionals exposed to inhaled anesthetics. There is continuing effort to understand the possible effects of anesthetics at molecular levels. Knowing the effects of anesthetic agents on genetic material could be a valuable basic support to better understand the possible mechanisms of these agents. Thus, the purpose of this review is to provide an overview on the genotoxic potential, evaluated in animal models, of many anesthetics that have already been used and those currently used in anesthesia. PMID:26199936

  9. Novel serine-based gemini surfactants as chemical permeation enhancers of local anesthetics: A comprehensive study on structure-activity relationships, molecular dynamics and dermal delivery.

    Science.gov (United States)

    Teixeira, Raquel S; Cova, Tânia F G G; Silva, Sérgio M C; Oliveira, Rita; do Vale, M Luísa C; Marques, Eduardo F; Pais, Alberto A C C; Veiga, Francisco J B

    2015-06-01

    This work aims at studying the efficacy of a series of novel biocompatible, serine-based surfactants as chemical permeation enhancers for two different local anesthetics, tetracaine and ropivacaine, combining an experimental and computational approach. The surfactants consist of gemini molecules structurally related, but with variations in headgroup charge (nonionic vs. cationic) and in the hydrocarbon chain lengths (main and spacer chains). In vitro permeation and molecular dynamics studies combined with cytotoxicity profiles were performed to investigate the permeation of both drugs, probe skin integrity, and rationalize the interactions at molecular level. Results show that these enhancers do not have significant deleterious effects on the skin structure and do not cause relevant changes on cell viability. Permeation across the skin is clearly improved using some of the selected serine-based gemini surfactants, namely the cationic ones with long alkyl chains and shorter spacer. This is noteworthy in the case of ropivacaine hydrochloride, which is not easily administered through the stratum corneum. Molecular dynamics results provide a mechanistic view of the surfactant action on lipid membranes that essentially corroborate the experimental observations. Overall, this study suggests the viability of these serine-based surfactants as suitable and promising delivery agents in pharmaceutical formulations.

  10. Sustained relief of pain from osteosynthesis surgery of rib fracture by using biodegradable lidocaine-eluting nanofibrous membranes.

    Science.gov (United States)

    Yu, Yi-Hsun; Hsu, Yung-Heng; Chou, Ying-Chao; Fan, Chin-Lung; Ueng, Steve W N; Kau, Yi-Chuan; Liu, Shih-Jung

    2016-10-01

    Various effective methods are available for perioperative pain control in osteosynthesis surgery, but they are seldom applied intraoperatively. The aim of this study was to evaluate a biodegradable poly([d,l]-lactide-co-glycolide) (PLGA)/lidocaine nanofibrous membrane for perioperative pain control in rib fracture surgery. Scanning electron microscopy showed high porosity of the membrane, and an ex vivo high-performance liquid chromatography study revealed an excellent release profile for both burst and controlled release of lidocaine within 30days. Additionally, the PLGA/lidocaine nanofibrous membrane was applied in an experimental rabbit rib osteotomy model. Implantation of the membrane around the osteotomized rib during osteosynthesis surgery resulted in a significant increase in weight gain, food and water consumption, and daily activity compared to the study group without the membrane. In addition, all osteotomized ribs were united. Thus, application of the PLGA/lidocaine nanofibrous membrane may be effective for sustained relief of pain in oeteosynthesis surgery. Copyright © 2016 Elsevier Inc. All rights reserved.

  11. Mechanism of Modification, by Lidocaine, of Fast and Slow Recovery from Inactivation of Voltage-Gated Na⁺ Channels.

    Science.gov (United States)

    Gawali, Vaibhavkumar S; Lukacs, Peter; Cervenka, Rene; Koenig, Xaver; Rubi, Lena; Hilber, Karlheinz; Sandtner, Walter; Todt, Hannes

    2015-11-01

    The clinically important suppression of high-frequency discharges of excitable cells by local anesthetics (LA) is largely determined by drug-induced prolongation of the time course of repriming (recovery from inactivation) of voltage-gated Na(+) channels. This prolongation may result from periodic drug-binding to a high-affinity binding site during the action potentials and subsequent slow dissociation from the site between action potentials ("dissociation hypothesis"). For many drugs it has been suggested that the fast inactivated state represents the high-affinity binding state. Alternatively, LAs may bind with high affinity to a native slow-inactivated state, thereby accelerating the development of this state during action potentials ("stabilization hypothesis"). In this case, slow recovery between action potentials occurs from enhanced native slow inactivation. To test these two hypotheses we produced serial cysteine mutations of domain IV segment 6 in rNav1.4 that resulted in constructs with varying propensities to enter fast- and slow-inactivated states. We tested the effect of the LA lidocaine on the time course of recovery from short and long depolarizing prepulses, which, under drug-free conditions, recruited mainly fast- and slow-inactivated states, respectively. Among the tested constructs the mutation-induced changes in native slow recovery induced by long depolarizations were not correlated with the respective lidocaine-induced slow recovery after short depolarizations. On the other hand, for long depolarizations the mutation-induced alterations in native slow recovery were significantly correlated with the kinetics of lidocaine-induced slow recovery. These results favor the "dissociation hypothesis" for short depolarizations but the "stabilization hypothesis" for long depolarizations. Copyright © 2015 by The American Society for Pharmacology and Experimental Therapeutics.

  12. The Effect of Topical Local Anesthetics on Thermal Pain Sensitivity in Patients with Irritable Bowel Syndrome

    Directory of Open Access Journals (Sweden)

    Anthony Rodrigues

    2012-01-01

    Full Text Available Generalized hypersensitivity that extends into somatic areas is common in patients with irritable bowel syndrome (IBS. The sensitized state, particularly assessed by experimental methods, is known to persist even during remissions of clinical pain. It was hypothesized that disease-related nociceptive activity in the gut maintains a systemic-sensitized state. The present study evaluated responses to prolonged thermal stimuli maintained at constant temperature or constant pain intensity during stimulation. The effect of topically applied rectal lidocaine on heat sensitivity was also evaluated. The question is whether silencing potential intestinal neural activity (which may not always lead to a conscious pain experience with lidocaine attenuates sensitization of somatic areas. Tests were also performed where lidocaine was applied orally to control for systemic or placebo effects of the drug. The IBS subjects exhibited a greater sensitivity to somatic heat stimuli compared to controls; however, lidocaine had no discernible effect on sensitization in this sample of IBS patients, where most of the individuals did not have clinical pain on the day of testing.

  13. Comparison of Emla cream and topical lidocaine tape for pain relief of V-beam laser treatment.

    Science.gov (United States)

    Horikiri, Masaru; Ueda, Kazuki; Sakaba, Takao

    2017-06-23

    The authors compared the analgesic effects of two topical applications; Emla(®) cream (Sato Pharmaceutical Co. Ltd., Tokyo, Japan) and 60% lidocaine tape (Penles(®) tape; Maruho, Osaka, Japan). The authors examined 20 outpatients with capillary malformations. Emla(®) cream or Penles(®) tape was applied 1 h before laser irradiation using V-Beam. After V-Beam irradiation, pain intensity was measured using Pain Vision(®) (NIPRO, Osaka, Japan), while subjective pain was converted into numerical values using the VAS system. In the assessment using Pain Vision(®), pain was significantly lower in patients who received Emla(®) cream (Welch test), whereas no difference was observed in VAS ratings between the two applications (student's t test). The objective system showed that Emla(®) cream had a significantly greater analgesic effect. We plan to evaluate the analgesic effects of these topical anesthetics by applying them to other anatomical areas.

  14. Anesthetic Related Advances with Cyclodextrins

    OpenAIRE

    Mark Welliver; John P. McDonough

    2007-01-01

    Cyclodextrins encapsulate and electrostatically bind to lipophilic molecules. The exterior of cyclodextrins are water-soluble and maintain aqueous solubility despite encapsulation of non-aqueous soluble molecules. This unique ability to encapsulate lipophilic molecules and maintain water solubility confers numerous pharmacologic advantages for both drug delivery and removal. Cyclodextrins, a component part of supramolecular chemistry, may be in its infancy of anesthetic application but recent...

  15. Potent Inhalational Anesthetics for Dentistry.

    Science.gov (United States)

    Satuito, Mary; Tom, James

    2016-01-01

    Nitrous oxide and the volatile inhalational anesthetics have defined anxiety and pain control in both dentistry and medicine for over a century. From curious experimentation to spectacular public demonstrations, the initial work of 2 dentists, Horace Wells and William T. G. Morton, persists to this day in modern surgery and anesthesia. This article reviews the history, similarities, differences, and clinical applications of the most popular inhalational agents used in contemporary dental surgical settings.

  16. Efficacy of Benzocaine 20% Topical Anesthetic Compared to Placebo Prior to Administration of Local Anesthesia in the Oral Cavity: A Randomized Controlled Trial.

    Science.gov (United States)

    de Freiras, Guilherme Camponogara; Pozzobon, Roselaine Terezinha; Blaya, Diego Segatto; Moreira, Carlos Heitor

    2015-01-01

    The aim of the present study was to compare the effects of a topical anesthetic to a placebo on pain perception during administration of local anesthesia in 2 regions of the oral cavity. A split-mouth, double-blind, randomized clinical trial design was used. Thirty-eight subjects, ages 18-50 years, American Society of Anesthesiologists I and II, received 4 anesthetic injections each in regions corresponding to the posterior superior alveolar nerve (PSA) and greater palatine nerve (GPN), totaling 152 sites analyzed. The side of the mouth where the topical anesthetic (benzocaine 20%) or the placebo was to be applied was chosen by a flip of a coin. The needle used was 27G, and the anesthetic used for administration of local anesthesia was 2% lidocaine with 1:100,000 epinephrine. After receiving the administration of local anesthesia, each patient reported pain perception on a visual analog scale (VAS) of 100-mm length. The results showed that the topical anesthetic and the placebo had similar effects: there was no statistically significant VAS difference between the PSA and the GPN pain ratings. A higher value on the VAS for the anesthesia of the GPN, relative to the PSA, was observed for both groups. Regarding gender, male patients had higher values on the VAS compared with female patients, but these differences were not meaningful. The topical anesthetic and the placebo had similar effects on pain perception for injection of local anesthesia for the PSA and GPN.

  17. 盐酸利多卡因分析方法进展%Review on assays of lidocaine hydrochloride

    Institute of Scientific and Technical Information of China (English)

    刘翠; 吐尔洪·买买提; 穆赫塔尔·伊米尔艾山

    2011-01-01

    Lidocaine hydrochloride is widely used as a local anesthetic and arrhythmia drug. This article reviewed determination of lidocaine hydrochloride in pharmaceutical preparations and pretreatment as well as determination of biological samples such as serum and plasma with efficient thin - layer chromatography, high performance liquid chromatography and micellar electrokinetic capillary electrophoresis , providing reference for future research.%盐酸利多卡因是目前常用的一种局部麻醉药和抗心律不齐药物.本文主要综述有关利多卡因药品制剂的容量分析、光度分析、色谱分析,以及血清和血浆样品预处理及其高效薄层色谱法、高效液相色谱及胶束电动毛细管电泳法的研究情况,希望为以后的研究提供借鉴.

  18. Lidocaine 5 % patches as an effective short-term co-analgesic in cancer pain. Preliminary results.

    Science.gov (United States)

    Garzón-Rodríguez, Cristina; Casals Merchan, Miquel; Calsina-Berna, Agnes; López-Rómboli, Eugenia; Porta-Sales, Josep

    2013-11-01

    To analyze the short-term efficacy and patients' subjective perception of the use of lidocaine 5 % patches for painful scars (post-thoracotomy and post-mastectomy) and pain caused by chest wall tumors. This is a prospective, descriptive, non-controlled, non-randomized, open-label study of patients seen in the palliative care outpatient clinic. Demographic data, variables relating to the severity of the pain, and concomitant therapy both at the start and end of treatment, the need for interventional anesthetic techniques (IAT), patients' subjective perception and treatment-related side effects were all recorded. Twenty patients were included with a mean follow-up of 29.2 days. The treatment led to a statistically significant clinical improvement in pain severity. There was no clinically significant opioid dose escalation during the treatment period. Only three patients required IAT to relieve the pain. Sixty five percent of patients were very satisfied with the therapy. No systemic or local adverse events were reported. The addition of lidocaine 5 % patches is effective in the short term for the treatment of neuropathic cancer pain accompanied by allodynia, whether deriving from a painful scar or chest wall tumor. These findings need to be confirmed by randomized controlled trials with larger samples.

  19. Comparison of the Effects of Articaine and Lidocaine Adjuvant Treatment of Acute Pericoronitis%阿替卡因与利多卡因辅助治疗急性智齿冠周炎的疗效比较

    Institute of Scientific and Technical Information of China (English)

    戴杰; 卓文杰; 王灵萍; 王文敏

    2012-01-01

    OBJECTIVE: To compare the local anesthetic effect of articaine and lidocaine for acute pericoronitis. METHODS: 160 cases of acute wisdom pericoronitis were divided into articaine group and lidocaine group according to outpatient order with 80 cases in each group. They were given articaine and lidocaine for pericoronitis local infiltration anesthesia. Anesthetic effect and the effect of adjuvant therapy of 2 groups were observed and compared. RESULTS: Anesthetic effect of articaine group at pericoronitis washing was better than lidocaine group (P0.05). CONCLUSION: Articaine can be used for local infiltration anesthesia of acute pericoronitis washing. The anesthetic effect is good, safe, and reliable, better than lidocaine.%目的:比较阿替卡因与利多卡因治疗急性智齿冠周炎的局部麻醉效果.方法:将急性智齿冠周炎患者160例按门诊顺序均分成阿替卡因组和利多卡因组,分别采用阿替卡因和利多卡因行冠周局部浸润麻醉,观察比较2组的麻醉效果、辅助治疗效果及不良反应情况.结果:阿替卡因组冠周冲洗时麻醉效果优于利多卡因组(P<0.01),24 h后的治疗效果也优于利多卡因组(P<0.05);从整个疗程上看,阿替卡因组冠周炎的炎症控制用时少于利多卡因组(P<0.01);2组不良反应比较差异无统计学意义(P>0.05).结论:阿替卡因可作为急性智齿冠周炎冠周冲洗时局部浸润麻醉药,具有麻醉效果好,安全、可靠等优点,效果优于利多卡因.

  20. Effects of mitogen-activated protein kinases on neurotoxicity of local anesthetics%丝裂原活化蛋白激酶家族在局麻药神经毒性中的作用

    Institute of Scientific and Technical Information of China (English)

    李乐; 徐世元; 卢爱珠

    2013-01-01

    背景 局麻药(local anesthetic,LA)广泛用于神经阻滞、镇痛,其可能引起的神经毒性引起了麻醉医生的关注,其中关于此种毒性作用机制的研究取得了较大的进展. 目的 分析总结各种丝裂原活化蛋白激酶家族(mitogen-activated protein kinases,MAPKs)成员在LA神经毒性中的作用. 内容 越来越多的证据证明LA的神经毒性作用可能与细胞凋亡有关.MAPKs是一种广泛存在细胞内的丝氨酸/苏氨酸蛋白激酶,在细胞凋亡过程中发挥重要作用.故MAPK信号通路逐渐成为LA毒性作用研究中的重点,其中关于细胞外信号调节激酶(extracellular signal-regulated kinase,ERK),c-Jun N-末端激酶(c-jun nterminal kinase,JNK)以及p38MAPK信号转导通路的研究较为成熟. 趋向 MAPKs在LA神经毒性的具体机制中发挥重要作用,这为LA的临床应用及毒性作用防治提供依据和理论指导.%Background The potential toxicity is a well-known side effect of local anesthetics (LA) which is widely used in nerve block and analgesia.The mechanisms of local anesthetic toxicity were further investigated.Objective This review summarized the recent studies examining the mitogen-activated protein kinases (MAPKs) signaling pathway and their regulation,and discussed the effects of MAPKs on neurotoxicity of LA.Content Accumulating evidences indicate that neurotoxicity of LA is related to apoptosis.MAPKs,a serine-threonine protein kinase family,play a crucial role in apoptosis of cells.So that the effects of MAPKs signaling pathway on neurotoxicity of LA is becoming a hot issue to be researched.And the impact of extracellular signalregulated kinase (ERK),c-Jun N-terminal kinase (JNK),p38MAPK are more concerned.Trend The MAPKs signaling pathway and their regulation play an important part in the underlying mechanisms of local anesthetic neurotoxicity which could provide evidences and theory for clinical use of LA.

  1. Lack of effect of flurothyl, a non-anesthetic fluorinated ether, on rat brain synaptic plasma membrane calcium-ATPase.

    Science.gov (United States)

    Horn, J L; Janicki, P K; Franks, J J

    1999-01-01

    Plasma membrane Ca2+-ATPase (PMCA), a regulator of intracellular calcium, is inhibited by volatile anesthetics and by xenon and nitrous oxide. Response of a cellular system to anesthetics, particularly to volatile agents, raises the question of non-specific, even toxic, side effects unrelated to anesthetic action. Compounds with chemical and physical properties similar to halogenated anesthetics, but which lack anesthetic effect, have been used to address this question. We have compared the effects of halothane and flurothyl, a non-anesthetic fluorinated ether, on PMCA Ca2+ transport across isolated brain synaptic plasma membranes (SPM). Flurothyl, at concentrations predicted by the Meyer-Overton curve to range from 0.4 to 2.6 MAC (minimum alveolar concentration), had no significant on PMCA activity. In contrast halothane, 1.3 MAC, reduced Ca2+ transport 30 to 40%. These findings provide further evidence for a specific effect of inhalation anesthetics on neuronal plasma membrane Ca2+-ATPase.

  2. Lidocaine for prolonged and intensified spinal anesthesia by coadministration of propranolol in the rat.

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    Chen, Yu-Wen; Chu, Chin-Chen; Chen, Yu-Chung; Hung, Ching-Hsia; Li, Yung-Tsung; Wang, Jhi-Joung

    2011-09-26

    Although the coadministration of lidocaine with propranolol interferes with the metabolic profile (pharmacokinetics), its pharmacodynamics is still unclear. In this report, we investigate whether propranolol can potentiate the effect of lidocaine. Rats received spinal anesthesia with lidocaine co-injected with propranolol. After intrathecal injections of drugs in rats, three neurobehavioral examinations (motor function, proprioception, and nociception) were performed. We showed that lidocaine and propranolol elicited a spinal blockade in motor function, proprioception, and nociception. Propranolol at the dose of 0.82 μmol/kg produced no spinal anesthesia. Co-administration of lidocaine [50% effective dose (ED(50)) or ED(95)] and propranolol (0.82 μmol/kg) produced greater spinal anesthesia than lidocaine (ED(50) or ED(95)), respectively. These preclinical findings demonstrated that propranolol and lidocaine displayed spinal anesthesia. When combined with propranolol, lidocaine elicited a supra-additive effect of spinal anesthesia.

  3. Remifentanil vs. Lidocaine on Response to Tracheal Tube during Emergence of General Anesthesia

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    Kambiz Sadegi

    2014-08-01

    Conclusion: we specified Remifentanil reduces cough during the emergence from general anesthesia more effective than Lidocaine in patients undergoing general surgery. In addition, Remifentanil and i.v. lidocaine revealed comparable impact regarding VAS scoring, sedation level and pethidine consumption.

  4. Hypnotic Actions of Local Anesthetics in Mice%局部麻醉药对小鼠催眠作用的研究

    Institute of Scientific and Technical Information of China (English)

    阿里·塞德; 孟庆涛; 夏中元; 陈向东

    2012-01-01

    目的:研究局部麻醉药的全身麻醉作用及其基本机制.方法:C57BL/6小鼠通过尾静脉分别注射利多卡因、布比卡因和罗哌卡因,同时使用或不使用氯胺酮、钠通道阻滞剂TTX和NMDA受体阻滞剂MK-801.通过翻正反射的消失(LORR)来评估这些药物对小鼠的催眠作用.结果:局部麻醉药利多卡因(15 mg/kg),布比卡因(5mg/kg),罗哌卡因(5 mg/kg)的全身应用均可产生直接的催眠作用,并达到其半数有效浓度(EC50).利多卡因可以增强氯胺酮的催眠作用(达到EC50的氯胺酮+利多卡因),表明了利多卡因和氯胺酮的联合使用可以增强其对小鼠的催眠作用.而钠通道阻滞剂不能改变利多卡因的催眠作用.NMDA受体阻滞剂(11-15 mg/kg)可增强并达到EC50利多卡因的LORR.结论:局部麻醉药可以产生直接的催眠作用,全身麻醉药氯胺酮可增强其麻醉效应,而钠通道阻滞剂则不能,NMDA受体阻滞剂可增强利多卡因的催眠作用.%Objective:. To investigate the systemic action of local anesthetics and their underlying mechanisms. Methods: Lidocaine, bupivacaine, and ropivacaine respectively were injected into C57BL/ 6 mice through tail vein intravenously, and loss of righting reflex (LORR) was used to evaluate the hypnotic action of these drugs with or without ketamine, sodium channel blocker TTX and NMDA receptor blocker MK-801. Results: Systemic application of all three local anesthetics directly produced hypnotic action with half effective concentration (EC50) of 15 mg/kg for lidocaine and 5 mg/kg for bupivacaine and ropivacaine. Lidocaine also enhanced the hypnotic action of ketamine, yielding an EC50 fraction of ketamine plus lidocaine of 1. 09, which suggested that lidocaine and ketamine have additive hypnotic action in mice. Blocking of sodium channel by TTX failed to alter hypnotic action of lidocaine. Blocking of NMDA receptor enhanced the LORR of lidocaine with EC50 from 11 mg/kg to 15 mg/kg. Conclusion

  5. Effect of 4% lidocaine inhalation in bronchial asthma.

    Science.gov (United States)

    Prakash, G S; Sharma, S K; Pande, J N

    1990-01-01

    The effect of 4% lidocaine inhalation was studied in a single-blind fashion in 18 patients with chronic stable asthma. Inhalation of normal saline solution was used as placebo. None of the parameters except flow rate at 50% of vital capacity (V50) showed any statistically significant change from baseline values. V50 at 15 min was significantly lower (p less than 0.05) after 4% lidocaine inhalation. Considering more than 10% change from the baseline value as significant, 8 of 15 patients showed decrease in airway resistance (Raw) and 7 of the 15 patients showed an increase in specific airway conductance (SGaw) after 15 min of inhalation. However, V50 (8/18 patients), flow rate at 25% vital capacity [V25 (6/15 patients], and forced expiratory flow rate at 25-75% of the vital capacity (FEF25-75) (5/15 patients) showed a decrease after 15 min of 4% lidocaine inhalation. No change in pulmonary function was noted after 30 min of lidocaine inhalation. It is concluded from this study that lidocaine produces a small bronchodilatory effect on the large airways and a bronchoconstrictor effect on the small airways after 15 min of inhalation, but this effect is not statistically significant. It can be safely used as topical agent for bronchoscopy in patients with bronchial asthma.

  6. Local anesthetic failure associated with inflammation: verification of the acidosis mechanism and the hypothetic participation of inflammatory peroxynitrite.

    Science.gov (United States)

    Ueno, Takahiro; Tsuchiya, Hironori; Mizogami, Maki; Takakura, Ko

    2008-01-01

    The presence of inflammation decreases local anesthetic efficacy, especially in dental anesthesia. Although inflammatory acidosis is most frequently cited as the cause of such clinical phenomena, this has not been experimentally proved. We verified the acidosis mechanism by studying the drug and membrane lipid interaction under acidic conditions together with proposing an alternative hypothesis. Liposomes and nerve cell model membranes consisting of phospholipids and cholesterol were treated at different pH with lidocaine, prilocaine and bupivacaine (0.05%-0.2%, w/v). Their membrane-interactive potencies were compared by the induced-changes in membrane fluidity. Local anesthetics fluidized phosphatidylcholine membranes with the potency being significantly lower at pH 6.4 than at pH 7.4 (p acidosis theory. However, they greatly fluidized nerve cell model membranes even at pH 6.4 corresponding to inflamed tissues, challenging the conventional mechanism. Local anesthetics acted on phosphatidylserine liposomes, as well as nerve cell model membranes, at pH 6.4 with almost the same potency as that at pH 7.4, but not on phosphatidylcholine, phosphatidylethanolamine and sphingomyelin liposomes. Since the positively charged anesthetic molecules are able to interact with nerve cell membranes by ion-paring with anionic components like phosphatidylserine, tissue acidosis is not essentially responsible for the local anesthetic failure associated with inflammation. The effects of local anesthetics on nerve cell model membranes were inhibited by treating with peroxynitrite (50 μM), suggesting that inflammatory cells producing peroxynitrite may affect local anesthesia.

  7. Anesthetic related advances with cyclodextrins.

    Science.gov (United States)

    Welliver, Mark; McDonough, John

    2007-03-02

    Cyclodextrins encapsulate and electrostatically bind to lipophilic molecules. The exterior of cyclodextrins are water-soluble and maintain aqueous solubility despite encapsulation of non-aqueous soluble molecules. This unique ability to encapsulate lipophilic molecules and maintain water solubility confers numerous pharmacologic advantages for both drug delivery and removal. Cyclodextrins, a component part of supramolecular chemistry, may be in its infancy of anesthetic application but recent advances have been described as novel and revolutionary. A review of current research coupled with an understanding of cyclodextrin properties is necessary to fully appreciate the current uses and future potentials of these unique molecules.

  8. Anesthetic Related Advances with Cyclodextrins

    Directory of Open Access Journals (Sweden)

    Mark Welliver

    2007-01-01

    Full Text Available Cyclodextrins encapsulate and electrostatically bind to lipophilic molecules. The exterior of cyclodextrins are water-soluble and maintain aqueous solubility despite encapsulation of non-aqueous soluble molecules. This unique ability to encapsulate lipophilic molecules and maintain water solubility confers numerous pharmacologic advantages for both drug delivery and removal. Cyclodextrins, a component part of supramolecular chemistry, may be in its infancy of anesthetic application but recent advances have been described as novel and revolutionary. A review of current research coupled with an understanding of cyclodextrin properties is necessary to fully appreciate the current uses and future potentials of these unique molecules.

  9. Strabismus complications from local anesthetics.

    Science.gov (United States)

    Guyton, David L

    2008-01-01

    Strabismus developing after retrobulbar or peribulbar anesthesia for both anterior and posterior segment eye surgery may be due to myotoxicity to an extraocular muscle from the local anesthetic agent. Initial paresis often causes diplopia immediately after surgery, but later progressive segmental fibrosis occurs, and/or hypertrophy of the muscle, producing diplopia in the opposite direction from the direction of the initial diplopia. The inferior rectus muscle is most commonly affected. Usually a large recession on an adjustable suture of the involved muscle(s) yields good alignment. Using topical anesthesia or sub-Tenon's anesthesia can avoid this complication.

  10. Effects of epidural lidocaine analgesia on labor and delivery: A randomized, prospective, controlled trial

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    Nafisi Shahram

    2006-12-01

    Full Text Available Abstract Background Whether epidural analgesia for labor prolongs the active-first and second labor stages and increases the risk of vacuum-assisted delivery is a controversial topic. Our study was conducted to answer the question: does lumbar epidural analgesia with lidocaine affect the progress of labor in our obstetric population? Method 395 healthy, nulliparous women, at term, presented in spontaneous labor with a singleton vertex presentation. These patients were randomized to receive analgesia either, epidural with bolus doses of 1% lidocaine or intravenous, with meperidine 25 to 50 mg when their cervix was dilated to 4 centimeters. The duration of the active-first and second stages of labor and the neonatal apgar scores were recorded, in each patient. The total number of vacuum-assisted and cesarean deliveries were also measured. Results 197 women were randomized to the epidural group. 198 women were randomized to the single-dose intravenous meperidine group. There was no statistical difference in rates of vacuum-assisted delivery rate. Cesarean deliveries, as a consequence of fetal bradycardia or dystocia, did not differ significantly between the groups. Differences in the duration of the active-first and the second stages of labor were not statistically significant. The number of newborns with 1-min and 5-min Apgar scores less than 7, did not differ significantly between both analgesia groups. Conclusion Epidural analgesia with 1% lidocaine does not prolong the active-first and second stages of labor and does not increase vacuum-assisted or cesarean delivery rate.

  11. Oral mexiletine for lidocaine-responsive neonatal epilepsy.

    Science.gov (United States)

    Nakazawa, Mika; Okumura, Akihisa; Niijima, Shinichi; Yamashita, Shintaro; Shimono, Kuriko; Hirose, Shinichi; Shimizu, Toshiaki

    2013-08-01

    We report a patient with lidocaine-responsive neonatal epilepsy treated successfully with oral mexiletine. The patient was a male neonate who had seizures since 2days of age. While his seizures were refractory to phenobarbital, lamotrigine, vitamin B6, and midazolam, they were controlled by continuous lidocaine infusion. Oral mexiletine at serum levels of 0.2-0.4μg/ml was used successfully for long-term treatment of his seizures. No delay in psychomotor development was observed at the last follow-up at 20months of age. No mutation was identified in any of four genes: SCN1A, SCN1B, KCNQ2, and KCNQ3. Our patient demonstrates that oral mexiletine can be useful for long-term treatment of patients with lidocaine-responsive epilepsy. Copyright © 2012 The Japanese Society of Child Neurology. Published by Elsevier B.V. All rights reserved.

  12. Clinical observation on lidocaine's application in phacoemulsification as surface anesthesia

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    Yong Liu

    2013-08-01

    Full Text Available AIM: To evaluate the effect of surface anesthesia for phacoemulsification using 20g/L lidocaine.METHODS: There were 1 850 patients(2 600 eyeswho underwent phacoemulsification via surface anesthesia using 20g/L lidocaine. The analgesic effect was observed. RESULTS: Totally 93% of 1 850 patients had not any pain during the surgery, a nice analgesic effect was showed, there was no complications duo to anaesthesia. Seven percent of all patients felt swelling pain during surgery but could tolerate. The naked or corrected visual acuity of 89.4% eyes was ≥0.6 one month after surgery.CONCLUSION: Surface anesthesia of using 20g/L lidocaine is safe and painless for phacoemulsification.

  13. Anxiety in preoperative anesthetic procedures.

    Science.gov (United States)

    Valenzuela Millán, Jaquelyn; Barrera Serrano, José René; Ornelas Aguirre, José Manuel

    2010-01-01

    Preoperative anxiety is a common and poorly evaluated condition in patients who will undergo an anesthetic and surgical intervention. The objective of this study was to determine the prevalence of anxiety in a group of patients undergoing elective surgery, as assessed by the Amsterdam Anxiety Preoperative and Information (AAPI) scale. We studied 135 patients scheduled for elective surgery applying the AAPI scale 24 h before the surgical procedure to evaluate the presence of anxiety and patient characteristics. A descriptive analysis with mean +/- standard deviation for categorical variables was done. For intragroup differences, chi(2) test was used. Pearson correlation for the association between anxiety and postoperative complications was carried out. A value of p =0.05 was considered significant. One hundred six patients were surgically treated, 88% were female (average age 44 +/- 12 years). Some degree of preoperative anxiety was present in 72 patients (76%; p = 0.001) with a grade point average on the AAPI scale equal to 17 +/- 7 points, of which 95 (70%, OR = 5.08; p = 0.002) were females. Results of this study suggest the presence of high levels of preoperative anxiety in patients scheduled for elective surgery. The origin of the anxiety appears to be related to many factors that can be evaluated in pre-anesthetic consultation. Further study is needed to prevent the presence of this disorder.

  14. Methemoglobin and sulfhemoglobin formation due to benzocaine and lidocaine in macaques

    Energy Technology Data Exchange (ETDEWEB)

    Martin, D.G.; Woodard, C.L.; Gold, M.B.; Watson, C.E.; Baskin, S.I.

    1993-05-13

    Benzocaine (BNZ) and lidocaine (LC) are commonly used topical (spray) anesthetics approved for use in humans. BNZ has structural similarities to methemoglobin (MHb) forming drugs that are current candidates for cyanide prophylaxis, while LC has been reported to increase MHb in man. We therefore, compared MHb and sulfhemoglobin (SHb) production in three groups of Macaques (Macaca mulata, Chinese rhesus and Indian rhesus, and Macaca nemistrina, Pig-tailed Macaques) after exposure to BNZ and LC. Formation of SHb, unlike MHb, is not thought to be reversible and is considered to be toxic. MHb and SHb levels were measured periodically on a CO-Oximeter. All rhesus (n=8) were dosed intratrachealy/intranasaly with 56 mg and 280 mg BNZ and with 40 mg of LC in a randomized cross-over design. Pig-tailed macaques (n=6) were dosed with BNZ intranasaly 56 mg and with 40 mg of LC. Since no differences in the peak MHb or time to peak (mean +/- SD) were observed among the three macaque subspecies, the data were pooled. LC did not cause MHb or SHb formation above baseline in any monkey.

  15. Lidocaine versus mepivacaine in sedated pediatric dental patients: randomized, prospective clinical study.

    Science.gov (United States)

    Çalış, Aylin Sipahi; Cagiran, Esra; Efeoglu, Candan; Ak, Aslı Topaloglu; Koca, Huseyın

    2014-01-01

    Dental anxiety is usually seen in the pediatric patients. specially in the case of minor oral surgical procedures and exodontia, cooperation of the patients and their families with the dentist will lead to superior treatment outcomes. Pain control is important in dentistry. The aim of this randomized prospective clinical study is to compare the local anaesthetic and haemodynamic effects of 2% lidocaine (Group 1) and 3% mepivacaine (Group 2) in sedated pediatric patients undergoing primary tooth extraction. 60 pediatric patients undergoing sedation for elective primary tooth extraction was prospectively included in the study in a randomized fashion. Inclusion and exclusion criteria were assigned. Patients were given premedication via oral route. Local anesthesia was achieved before extraction(s). There were no significant differences between the groups in patient demographics, number of teeth extracted, duration of the operation and time from the end of the procedure to discharge (p ≥ 0.05). FLACC pain scale scores were not statistically significant between the groups, except at 20 minutes post-operatively when the score is significantly lower in Group 2 (p=0.029). Prevention of pain during dental procedures can nurture the relationship of the patient and dentist. Tooth extraction under sedation in pediatric patients could be safe with both local anesthetics.

  16. Lidocaine/tetracaine medicated plaster: in minor dermatological and needle puncture procedures.

    Science.gov (United States)

    Croxtall, Jamie D

    2010-11-12

    The lidocaine/tetracaine medicated plaster comprises a lidocaine/tetracaine 70 mg/70 mg patch and a controlled heat-assisted drug delivery pod that increases the diffusion of lidocaine and tetracaine into the dermis. Following a 1-hour application period, systemic absorption of lidocaine or tetracaine from the plaster was minimal. The lidocaine/tetracaine medicated plaster provided effective pain relief for adult (including elderly) patients undergoing minor dermatological procedures and for adult and paediatric patients undergoing vascular access procedures. In randomized, double-blind clinical trials, patient-reported median pain scores were significantly lower with the lidocaine/tetracaine medicated plaster than with an identical plaster containing placebo in patients undergoing minor dermatological or vascular access procedures. Furthermore, patient-reported median pain scores were significantly lower with the lidocaine/tetracaine medicated plaster than with a lidocaine/prilocaine cream in patients undergoing vascular access procedures. In a large, randomized, double-blind trial in paediatric patients undergoing venipuncture, the overall incidence of pain was significantly lower with the lidocaine/tetracaine medicated plaster than with a lidocaine/prilocaine plaster. The lidocaine/tetracaine medicated plaster was well tolerated, with the most frequent treatment-related adverse events resolving spontaneously.

  17. A Comparative Study Between 1% and 0.1% Lidocain with Adrenaline in Skin Local Anesthesia

    Directory of Open Access Journals (Sweden)

    A. Zamanian

    2005-01-01

    Full Text Available Lidocain solution 1-2% have used with or without adrenaline for skin local anesthesia. Also normal salin, diphenhydramine and bacteriostatic salin have been used. The purpose of this study was to compare the effectiveness of 1% lidocain with 0.1% lidocain in local skin anesthesia.This study was carried out by triple blind method on 140 patients that submitted to Hamedan Sina Hospital in 2000. These patients divided in two groups randomly, 70 cases received 1% lidocain and other 70 cases received 0.1% lidocain. The pain assessment score was between 0-10 that was asked from each patient and collected data analyzed by statistical methods.This study showed that 51.1% of patients that received 1% lidocain and 48.9% that received 0.1% lidocain did not have any pain during injection (P>0.05. Also 54.3% of patients that received 1% lidocain and 45.7% that received 0.1% lidocain solution did not have any pain throw the procedure (P>0.05.The effect of 0.1% lidocain solution had no much difference from 1% lidocain in skin local anesthesia and thus it is suggested to use it for wide anesthesia in skin surgeries.

  18. Caudal epidural analgesia using lidocaine alone or in combination with ketamine in dromedary camels (Camelus dromedarius

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    Omid Azari

    2014-02-01

    Full Text Available This study was performed to investigate the analgesic effect of lidocaine and a combination of lidocaine and ketamine following epidural administration in dromedary camels. Ten 12–18-month-old camels were randomly divided into two equal groups. In group L, the animals received 2% lidocaine (0.22 mg/kg and in group LK the animals received a mixture of 10% ketamine (1 mg/kg and 2% lidocaine (0.22 mg/kg administered into the first intercoccygeal (Co1–Co2 epidural space while standing. Onset time and duration of caudal analgesia, sedation level and ataxia were recorded after drug administration. Data were analysed by U Mann-Whitney tests and significance was taken as p < 0.05. The results showed that epidural lidocaine and co-administration of lidocaine and ketamine produced complete analgesia in the tail, anus and perineum. Epidural administration of the lidocaine-ketamine mixture resulted in mild to moderate sedation, whilst the animals that received epidural lidocaine alone were alert and nervous during the study. Ataxia was observed in all test subjects and was slightly more severe in camels that received the lidocaine-ketamine mixture. It was concluded that epidural administration of lidocaine plus ketamine resulted in longer caudal analgesia in standing conscious dromedary camels compared with the effect of administering lidocaine alone.

  19. TRPA1 insensitivity of human sural nerve axons after exposure to lidocaine.

    Science.gov (United States)

    Docherty, Reginald J; Ginsberg, Lionel; Jadoon, Saqiba; Orrell, Richard W; Bhattacharjee, Anupam

    2013-09-01

    TRPA1 is an ion channel of the TRP family that is expressed in some sensory neurons. TRPA1 activity provokes sensory symptoms of peripheral neuropathy, such as pain and paraesthesia. We have used a grease gap method to record axonal membrane potential and evoked compound action potentials (ECAPs) in vitro from human sural nerves and studied the effects of mustard oil (MO), a selective activator of TRPA1. Surprisingly, we failed to demonstrate any depolarizing response to MO (50, 250 μM) in any human sural nerves. There was no effect of MO on the A wave of the ECAP, but the C wave was reduced at 250 μM. In rat saphenous nerve fibres MO (50, 250 μM) depolarized axons and reduced the C wave of the ECAP but had no effect on the A wave. By contrast, both human and rat nerves were depolarized by capsaicin (0.5 to 5 μM) or nicotine (50 to 200 μM). Capsaicin caused a profound reduction in C fibre conduction in both species but had no effect on the amplitude of the A component. Lidocaine (30 mM) depolarized rat saphenous nerves acutely, and when rat nerves were pretreated with 30 mM lidocaine to mimic the exposure of human nerves to local anaesthetic during surgery, the effects of MO were abolished whilst the effects of capsaicin were unchanged. This study demonstrates that the local anaesthetic lidocaine desensitizes TRPA1 ion channels and indicates that it may have additional mechanisms for treating neuropathic pain that endure beyond simple sodium channel blockade.

  20. Hydrogen-1 NMR relaxation time studies in membrane: anesthetic systems; Variacao dos tempos de relaxacao longitudinal de protons em sistemas membranares contendo anestesicos locais

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    Pinto, L.M.A.; Fraceto, L.; Paula, E. de [Universidade Estadual de Campinas, SP (Brazil). Dept. de Bioquimica; Franzoni, L.; Spisni, A. [Universita degli Studi di Parma, Parma (Italy). Ist. di Chimica Biologica

    1997-12-31

    The study of local anesthetics`(LA) interaction with model phospholipid membranes is justified by the direct correlation between anesthetic`s hydrophobicity and its potency/toxicity. By the same reason, uncharged LA species seems to play a crucial role in anesthesia. Most clinically used LA are small amphiphilics with a protonated amine group (pKa around 8). Although both charged (protonated) and uncharged forms can coexist at physiological pH, it has been shown (Lee, Biochim. Biophys. Acta 514:95, 1978; Screier et al. Biochim. Biophys. Acta 769:231, 1984) that the real anesthetic pka can be down-shifted, due to differential partition into membranes, increasing the ratio of uncharged species at pH 7.4. We have measured {sup 1}H-NMR longitudinal relaxation times (T{sub 1}) for phospholipid and three local anesthetics (tetracaine, lidocaine, benzocaine), in sonicated vesicles at a 3:1 molar ratio. All the LA protons have shown smaller T{sub 1} in this system than in isotropic phases, reflecting LA immobilization caused by insertion in the membrane. T{sub 1} values for the lipid protons in the presence of LA were analyzed, in an attempt to identify specific LA:lipid contact regions. (author) 13 refs., 3 figs., 1 tabs.

  1. Relief of Injection Pain During Delivery of Local Anesthesia by Computer-Controlled Anesthetic Delivery System for Periodontal Surgery: Randomized Clinical Controlled Trial.

    Science.gov (United States)

    Chang, Hyeyoon; Noh, Jiyoung; Lee, Jungwon; Kim, Sungtae; Koo, Ki-Tae; Kim, Tae-Il; Seol, Yang-Jo; Lee, Yong-Moo; Ku, Young; Rhyu, In-Chul

    2016-07-01

    Pain from local anesthetic injection makes patients anxious when visiting a dental clinic. This study aims to determine differences in pain according to types of local anesthetizing methods and to identify the possible contributing factors (e.g., dental anxiety, stress, and sex). Thirty-one patients who underwent open-flap debridement in maxillary premolar and molar areas during treatment for chronic periodontitis were evaluated for this study. A randomized, split-mouth, single-masked clinical trial was implemented. The dental anxiety scale (DAS) and perceived stress scale (PSS) were administered before surgery. Two lidocaine ampules for each patient were used for local infiltration anesthesia (supraperiosteal injection). Injection pain was measured immediately after local infiltration anesthesia using the visual analog pain scale (VAS) questionnaire. Results from the questionnaire were used to assess degree of pain patients feel when a conventional local anesthetic technique (CNV) is used compared with a computer-controlled anesthetic delivery system (CNR). DAS and PSS did not correlate to injection pain. VAS scores were lower for CNR than for CNV regardless of the order in which anesthetic procedures were applied. VAS score did not differ significantly with sex. Pearson coefficient for correlation between VAS scores for the two procedures was 0.80, also indicating a strong correlation. Within the limitations of the present study, relief from injection pain is observed using CNR.

  2. The effects of lidocaine or a lidocaine-bupivacaine mixture administered into the infraorbital canal in dogs.

    Science.gov (United States)

    Pascoe, Peter J

    2016-07-01

    OBJECTIVE To determine the onset, duration, and extent of regional nerve blocks performed by administration of lidocaine or lidocaine-bupivacaine into the infraorbital canal in dogs. ANIMALS 6 healthy hound-type dogs. PROCEDURES Under general anesthesia, stimulating needles were inserted into the gingiva dorsolateral to both maxillary canine (MC) teeth and the maxillary fourth premolar (MPM4) and second molar (MM2) teeth on the treatment side. A reflex-evoked muscle potential (REMP) was recorded from the digastricus muscle after noxious electrical stimulation at each site. After baseline measurements, 1 mL of 2% lidocaine solution or a 2% lidocaine-0.5% bupivacaine mixture (0.5 mL each) was injected into the infraorbital canal (at approx two-thirds of the canal length measured rostrocaudally). The REMPs were recorded for up to 7 hours. The REMP data for the contralateral (untreated control) canine tooth were used to normalize results for all stimulation sites. RESULTS With both treatments, nerve block for MC teeth on the treated side was achieved by 5 (n = 5 dogs) or 10 (1) minutes after injection, but nerve block for ipsilateral MPM4 and MM2 teeth was successful for only 3 dogs and 1 dog, respectively. Mean duration of nerve blocks for MC teeth was 120 and 277 minutes following injection of lidocaine and lidocaine-bupivacaine, respectively. CONCLUSIONS AND CLINICAL RELEVANCE Local anesthesia, as performed in this study, successfully blocked innervation of MC teeth, but results for MPM4 and MM2 teeth were inconsistent. This specific technique should not be used during tooth extractions caudal to the MC teeth.

  3. Buffered 1% Lidocaine With Epinephrine Is as Effective as Non-Buffered 2% Lidocaine With Epinephrine for Mandibular Nerve Block.

    Science.gov (United States)

    Warren, Victor T; Fisher, Anson G; Rivera, Eric M; Saha, Pooja T; Turner, Blake; Reside, Glenn; Phillips, Ceib; White, Raymond P

    2017-07-01

    To assess outcomes for pulpal anesthesia and pain on injection for buffered 1% lidocaine with 1:100,000 epinephrine (EPI) versus non-buffered 2% lidocaine with 1:100,000 EPI. In a randomized cross-over trial approved by the institutional review board, buffered 1% lidocaine with 1:100,000 EPI was compared with non-buffered 2% lidocaine with 1:100,000 EPI. After mandibular nerve block with buffered lidocaine 40 mg or non-buffered lidocaine 80 mg, patients reported responses at the mandibular first molar and canine after cold and electrical pulp testing (EPT). Patients also reported pain on injection with a 10-point Likert-type scale. Teeth were tested before nerve block and at 30-minute intervals until a positive response returned. Two weeks later, patients were tested with the alternate drug combinations. The same outcomes were assessed. Predictor variables were alternate drug formulations. Outcome variables were patients' responses to cold and EPT stimulation of the mandibular first molar and canine and pain on injection. An assessment of treatment difference was performed using Wilcoxon rank-sum tests with Proc NPAR1WAY (SAS 9.3, SAS Institute, Cary, NC). Significance was set at a P value less than .05. Fifty-seven percent of patients were women and 43% were men. Seventy percent were Caucasian, 17% were African American, and 13% had another ethnicity. Median age was 25 years (interquartile range [IQR], 21-26 yr) and median body weight was 140 lbs (IQR, 120-155 lbs). After the cold test and EPT, the time to sensation return for the molar or canine was not statistically different between the 2 drug formulations. Patients reported significantly lower pain scores with the buffered versus non-buffered drug (P lidocaine with EPI can produce similar clinical outcomes for duration of pulpal anesthesia as non-buffered 2% lidocaine with EPI and lower pain on injections, which are a potential benefit to patients. Copyright © 2017 American Association of Oral and

  4. Anesthetizing animals: Similar to humans yet, peculiar?

    Science.gov (United States)

    Kurdi, Madhuri S; Ramaswamy, Ashwini H

    2015-01-01

    From time immemorial, animals have served as models for humans. Like humans, animals too have to undergo several types of elective and emergency surgeries. Several anesthetic techniques and drugs used in humans are also used in animals. However, unlike humans, the animal kingdom includes a wide variety of species, breeds, and sizes. Different species have variable pharmacological responses, anatomy, temperament, behavior, and lifestyles. The anesthetic techniques and drugs have to suit different species and breeds. Nevertheless, there are several drugs and many peculiar anesthetic techniques used in animals but not in human beings. Keeping this in mind, literature was hand searched and electronically searched using the words "veterinary anesthesia," "anesthetic drugs and techniques in animals" using Google search engine. The interesting information so collected is presented in this article which highlights some challenging and amazing aspects of anesthetizing animals including the preanesthetic assessment, preparation, premedication, monitoring, induction of general anesthesia, intubation, equipment, regional blocks, neuraxial block, and perioperative complications.

  5. Inhibition of firefly luciferase by general anesthetics: effect on in vitro and in vivo bioluminescence imaging.

    Directory of Open Access Journals (Sweden)

    Marleen Keyaerts

    Full Text Available UNLABELLED: Bioluminescence imaging is routinely performed in anesthetized mice. Often isoflurane anesthesia is used because of its ease of use and fast induction/recovery. However, general anesthetics have been described as important inhibitors of the luciferase enzyme reaction. AIM: To investigate frequently used mouse anesthetics for their direct effect on the luciferase reaction, both in vitro and in vivo. MATERIALS AND METHODS: isoflurane, sevoflurane, desflurane, ketamine, xylazine, medetomidine, pentobarbital and avertin were tested in vitro on luciferase-expressing intact cells, and for non-volatile anesthetics on intact cells and cell lysates. In vivo, isoflurane was compared to unanesthetized animals and different anesthetics. Differences in maximal photon emission and time-to-peak photon emission were analyzed. RESULTS: All volatile anesthetics showed a clear inhibitory effect on the luciferase activity of 50% at physiological concentrations. Avertin had a stronger inhibitory effect of 80%. For ketamine and xylazine, increased photon emission was observed in intact cells, but this was not present in cell lysate assays, and was most likely due to cell toxicity and increased cell membrane permeability. In vivo, the highest signal intensities were measured in unanesthetized mice and pentobarbital anesthetized mice, followed by avertin. Isoflurane and ketamine/medetomidine anesthetized mice showed the lowest photon emission (40% of unanesthetized, with significantly longer time-to-peak than unanesthetized, pentobarbital or avertin-anesthetized mice. We conclude that, although strong inhibitory effects of anesthetics are present in vitro, their effect on in vivo BLI quantification is mainly due to their hemodynamic effects on mice and only to a lesser extent due to the direct inhibitory effect.

  6. [Monoethylglycinexylidide--a metabolite of lidocaine--as an index of liver function in chronic hepatic parenchymal diseases].

    Science.gov (United States)

    Kupcová, V; Turecký, L; Szántová, M; Schmidtová, K

    1999-01-01

    The changes of biotransformation enzyme system (b.e.s.) activity and capacity in liver diseases significantly influence the metabolism of various xenobiotics. Lidocaine is metabolised through oxidative N-deethylation by b.e.s. resulting in the production of monoethylglycinexylide (MEGX). The aim of this study was the determination of serum MEGX concentration as a model substance for indirect evaluation of liver b.e.s. function in patients with liver steatofibrosis and cirrhosis and the assessment of the possibilities to use it as a quantitave test of liver functional state. The study group consisted of 53 patients, 36 of them with liver disease of different etiology (postviral, ethyltoxic, cryptogenic, liver cirrhosis on the basis of autoimmune hepatitis, liver cirrhosis induced by primary sclerosing cholangitis, primary biliary cirrhosis in the stage of cirrhosis, Wilson's disease in the stage of cirrhosis), 7 patients with liver steatofibrosis and 10 control persons. After intravenous administration of lidocaine (1 mg/kg of body weight), concentration of MEGX was assessed by fluorescence polarization immunoassay (FPIA) using Tdx system in venous blood. The concentration was assesed prior to administration of lidocaine and 15 and 30 minutes after. In the group of liver steatofibrosis the concentrations in the 15th minute after administration were lower comparing to controls, in the 30th minute the difference was less significant. The values of MEGX in cirrhosis group were significantly decreased 15 and 30 minutes after lidocaine administration in comparison with control group. The cirrhosis group was divided into two subgroups: compensated (Ci c) and decompensated (Ci d) and independently of this division into three parts according to score system of Child-Pugh classification (Ci A, Ci B, Ci C). The concentrations 15 and 30 minutes after lidocaine administration in patients with Ci c and Ci d were significantly different, similarly there were statistically

  7. Effects of local anesthetics and hemicholinium-3 on 45-Ca efflux in barnacle muscle fibers.

    Science.gov (United States)

    Chen, S S

    1975-04-01

    Benzocaine, which occurs in the uncharged form in the physiological range of pH, caused inhibition of 45-Ca efflux in branacle muscle fibers. By contrast, in the presence of a low external Ca-2+ concentration it produced stimulation of the efflux. Both the inhibitory and stimulatory actions of benzocaine appeared to be less potent than those of procaine. Hemicholinium-3 (HC-3), on the other hand, which exists only in the charged form, caused a large stimulation of the 45-Ca efflux following microinjection, and the potency of this action was found to be at least 10 times greater than that of procaine. External application of HC-3 produced inhibition occasionally. Effects of tetracaine were similar to those produced by procaine; however, its inhibitory action was greater in more alkaline solution, which is the opposite of that observed with procaine. Lidocaine produced a less consistent effect than procaine; the inhibitory action of the former was less potent but the stimulatory action of the two anesthetics were comparable, p-Aminobenzoic acid was without effect on 45-Ca efflux. These results indicate that both the charged and uncharged forms of local anesthetics are capable of causing stimulatory and inhibitory effects on 45-Ca efflux in barnacle muscle fibers, and that the inhibition produced is the result of action on the CA-Ca exchange system whereas the stimulation is the result of release of Ca from internal storage sites.

  8. The efficacy of local anesthetics in reducing post operative pain after appendectomy

    Directory of Open Access Journals (Sweden)

    Masood Baghaee vaji

    2004-09-01

    Full Text Available Reducing post operative pain is a common issue in surgeries. This study was to evaluate the efficacy of wound infiltration with local anesthetics in reducing postoperative pain after appendectomy. This is a double-blind, placebo-controlled, randomized clinical trial on 40 patients with non-complicated acute appendicitis. Cases received a combination of lidocaine hydrochloride and bupivacaine hydrochloride after appendectomy and before closing the wound. Controls received the same volume of saline solution. Injections were done both under the fascia of external oblique muscle and intradermal. Pain assessment was done by two pain measuring scales, VAS and NRS, in 4, 8, 12 and 24 hours after the operation. Cases and controls were the same in age, sex, and history of opium addiction. Pain peaked in the 8th hour after operation in both groups and reduced afterwards. Pain assessments showed the same pattern using the NRS and VAS measuring scales. T-test showed the pain to be significantly less in cases comparing with the controls in all time points. No significant difference was seen in the time of receiving the first analgesic after the operation but the frequency of analgesic consumption was significantly lower in controls. This study showed local anesthetic infiltration to be effective in reducing the postoperative pain in patients undergoing appendectomy which is in contrast with the previous studies. This may be due to a different infiltration technique or pain assessment in the first 24 hours after the operation.

  9. Anesthetic management of a patient with Sturge-Weber syndrome undergoing oral surgery.

    Science.gov (United States)

    Yamashiro, Mikiko; Furuya, Hideki

    2006-01-01

    This case involves a possible complication of excessive bleeding or rupture of hemangiomas. Problems and anesthetic management of the patient are discussed. A 35-year-old man with Sturge-Weber syndrome was to undergo teeth extraction and gingivectomy. Hemangiomas covered his face and the inside of the oral cavity. We used intravenous conscious sedation with propofol and N2O-O2 to reduce the patient's emotional stress. It was previously determined that stress caused marked expansion of this patient's hemangiomas. Periodontal ligament injection was chosen as the local anesthesia technique. Teeth were extracted without excessive bleeding or rupture of hemangiomas, but the planned gingivectomies were cancelled. Deep sedation requiring airway manipulation should be avoided because there are possible difficulties in airway maintenance. Because this was an outpatient procedure, propofol was selected as the sedative agent primarily because of its rapid onset and equally rapid recovery. Periodontal ligament injection with 2% lidocaine containing 1: 80,000 epinephrine was chosen for local anesthesia. Gingivectomy was cancelled because hemostasis was challenging. As part of preoperative preparation, equipment for prompt intubation was available in case of rupture of the hemangiomas. The typically seen elevation of blood pressure was suppressed under propofol sedation so that expansion of the hemangiomas and significant intraoperative bleeding was prevented. Periodontal ligament injection as a local anesthetic also prevented bleeding from the injection site.

  10. Comparative Evaluation of Pain Scores during Periodontal Probing with or without Anesthetic Gels

    Directory of Open Access Journals (Sweden)

    Ashank Mishra

    2016-01-01

    Full Text Available Context. The initial periodontal examination which includes full-mouth periodontal probing is one of the discomforting procedures for a patient. Aim. To evaluate the efficacy of two local anesthetic gels in the reduction of pain during periodontal probing using Florida probe in CGP patients in comparison with manual probing. Materials and Methods. Ninety systemically healthy patients with moderate to severe CGP patients were recruited. In each patient, the quadrants were randomly assigned to manual probing with UNC-15 probe, probing with Florida probe, and Florida probing with lidocaine 10% gel and with benzocaine 20% gel. In the quadrants undergoing probing with anesthetic gels, the sites were isolated and the gel was injected using syringe and a blunt-end cannula. Pain was measured using 10 mm horizontal VAS. Statistical Analysis. The analysis was carried out using SPSS version 18. The comparison of mean VAS scores was done using repeated measures ANOVA with post hoc Bonferroni test. Results. Mean VAS for manual probing was significantly more than Florida probing. Further, the mean VAS score for Florida probing was higher than the two gels. Conclusion. It is suggested that the gels might be useful in reducing pain experienced during full-mouth periodontal probing in patients with CGP.

  11. [Treatment of persistent postmastectomy pain with 5% Lidocaine medicated plaster].

    Science.gov (United States)

    Cruto, M E; Baricocchi, E; Battistella, M; Bona, F; Giacoletto, G; Iacobellis, A; Moselli, N; Palomba, G; Sardo, E; Savojardo, M; Suita, L; Zocca, E; Debernardi, F

    2015-04-01

    Persistent postmastectomy pain (PPMP) syndrome is characterized by neuropathic pain that develops following surgery in breast cancer patients. The reported incidence of PPMP ranges between 30% and 50% and is estimated to increase as the number of women surviving cancer continues to rise. Though effective, today's drug treatments are poorly tolerated, limiting their use and reducing adherence to therapy. Since neuropathic pain is localized, international guidelines suggest that topical treatment with 5% Lidocaine medicated plaster either alone or combined with systemic drugs can be considered for pain management. In this retrospective study we reviewed the medical records of 11 patients treated with 5% lidocaine medicated plaster for moderate-to-severe PPMP at our institute between November 2013 and October 2014. Analysis showed that treatment with 5% Lidocaine medicated plaster, either alone or in combination with systemic drugs, achieved significant pain control already after the first week of therapy. The effectiveness and tolerability of 5% Lidocaine medicated plaster we observed suggests that it is a viable option in the management of PPMP.

  12. Continuous intravenous perioperative lidocaine infusion for postoperative pain and recovery.

    Science.gov (United States)

    Kranke, Peter; Jokinen, Johanna; Pace, Nathan Leon; Schnabel, Alexander; Hollmann, Markus W; Hahnenkamp, Klaus; Eberhart, Leopold H J; Poepping, Daniel M; Weibel, Stephanie

    2015-07-16

    The management of postoperative pain and recovery is still unsatisfactory in clinical practice. Opioids used for postoperative analgesia are frequently associated with adverse effects including nausea and constipation. These adverse effects prevent smooth postoperative recovery. On the other hand not all patients may be suited to, and take benefit from, epidural analgesia used to enhance postoperative recovery. The non-opioid lidocaine was investigated in several studies for its use in multi-modal management strategies to reduce postoperative pain and enhance recovery. The aim of this review was to assess the effects (benefits and risks) of perioperative intravenous lidocaine infusion compared to placebo/no treatment or compared to epidural analgesia on postoperative pain and recovery in adults undergoing various surgical procedures. We searched the Cochrane Central Register of Controlled Trials (CENTRAL, Issue 5 2014), MEDLINE (January 1966 to May 2014), EMBASE (1980 to May 2014), CINAHL (1982 to May 2014), and reference lists of articles. We searched the trial registry database ClinicalTrials.gov, contacted researchers in the field, and handsearched journals and congress proceedings. We did not apply any language restrictions. We included randomized controlled trials comparing the effect of continuous perioperative intravenous lidocaine infusion either with placebo, or no treatment, or with epidural analgesia in adults undergoing elective or urgent surgery under general anaesthesia. The intravenous lidocaine infusion must have been started intraoperatively prior to incision and continued at least until the end of surgery. Trial quality was independently assessed by two authors according to the methodological procedures specified by the Cochrane Collaboration. Data were extracted by two independent authors. We collected trial data on postoperative pain, recovery of gastrointestinal function, length of hospital stay, postoperative nausea and vomiting (PONV), opioid

  13. Research on lidocaine in the application of induced abortion

    Institute of Scientific and Technical Information of China (English)

    Hai-Tao Tong

    2015-01-01

    Objective:To observe the effect of lidocaine in the application of induced abortion.Methods:A total of 120 pregnant women with 6-10 week gestational age and ASA I-II level who were volunteered to receive induced abortions from January, 2010 to January, 2013 were included in the study, among which 60 cases were given lidocaine during the operation and served as the observation group, while 60 cases were not given lidocaine during the operation and served as the control group. The heart rate, blood pressure, the change of oxygen saturation, pain, and the occurrence of abortion syndrome before and after operation between the two groups were compared.Results:The fineness rates of analgesia and anesthesia evaluation in the observation group were significantly higher than those in the control group (P0.05). The postoperative heart rate and blood pressure in the control group were significantly lower than those before operation and in the observation group with a slow recovery (P0.05). The occurrence rate of abortion syndrome in the observation group was significantly lower than that in the control group (P<0.05). Conclusions:Application of lidocaine in the induced abortion can relieve the pain and reduce the occurrence rate of abortion syndrome with a simple and safe operation; therefore, it deserves to be widely recommended.

  14. Evaluation of gentamicin and lidocaine release profile from gum acacia-crosslinked-poly(2-hydroxyethylmethacrylate)-carbopol based hydrogels.

    Science.gov (United States)

    Singh, Baljit; Dhiman, Abhishek

    2017-01-27

    In this manuscript an attempt has been made to incorporate both, antibiotic agent 'gentamicin' and pain relieving agent 'lidocaine' into the gum acacia-poly(2-hydroxyethylmethacrylate)-carbopol based hydrogel for wound dressing application. Drug release, gel strength, network parameter, antimicrobial activity and biodegradation properties of hydrogel have been evaluated. Porous microstructure of the hydrogel was observed in cryo-SEM images. The hydrogel showed mesh size 37.29 nm, cross-link density 2.19× 10-5 mol/cm3, molecular weight between two cross-links 60.25× 10-3 g/mol and gel strength 0.625±0.112 N in simulated wound fluid. The hydrogels were evaluated as a drug carrier for model drugs gentamicin and lidocaine. The release of these drugs occurred through Fickian diffusion mechanism and release profile of the drugs was best fitted in first order kinetic model.

  15. [Comparative study between benzydamine hydrochloride gel, lidocaine 5% gel and lidocaine 10% spray on endotracheal tube cuff as regards postoperative sore throat].

    Science.gov (United States)

    Mekhemar, Nashwa Abdallah; El-Agwany, Ahmed Samy; Radi, Wafaa Kamel; El-Hady, Sherif Mohammed

    2016-01-01

    Postoperative sore throat is a common complication after endotracheal intubation. After tracheal intubation, the incidence of sore throat varies from 14.4% to 50%. The aim of the study was to compare between benzydamine hydrochloride gel, lidocaine 5% gel and lidocaine 10% spray on the endotracheal tube cuff as regards postoperative sore throat. The present study was carried out on 124 patients admitted to Alexandria university hospitals for lumbar fixation surgery requiring general anesthesia. Patients were randomly allocated into 4 groups. Benzydamine hydrochloride gel, 5% lidocaine hydrochloride gel, 10% lidocaine hydrochloride spray, or normal saline were applied on endotracheal tube cuffs before endotracheal intubation. The patients were examined for sore throat (none, mild, moderate, or severe) at 0, 1, 6, 12, and 24h after extubation. The results were collected, analyzed and presented in table and figure. The highest incidence of postoperative sore throat occurred at 6h after extubation in all groups. There was a significantly lower incidence of postoperative sore throat in the benzydamine group than 5% lidocaine gel, 10% lidocaine spray, and normal saline groups. The benzydamine group had significantly decreased severity of postoperative sore throat compared with the 10% lidocaine, 5% lidocaine, and normal saline groups at observation time point. Compared with the 5% lidocaine the 10% lidocaine group had significantly increased incidence and severity of postoperative sore throat after extubation. Compared with normal saline the 10% lidocaine group had increased incidence of postoperative sore throat. There were no significant differences among groups in local or systemic side effects. So in conclusion, benzydamine hydrochloride gel on the endotracheal tube cuff is a simple and effective method to reduce the incidence and severity of postoperative sore throat. Application of 10% lidocaine spray should be avoided because of worsening of postoperative sore

  16. Comparative study between benzydamine hydrochloride gel, lidocaine 5% gel and lidocaine 10% spray on endotracheal tube cuff as regards postoperative sore throat

    Directory of Open Access Journals (Sweden)

    Nashwa Abdallah Mekhemar

    2016-06-01

    Full Text Available ABSTRACT Postoperative sore throat is a common complication after endotracheal intubation. After tracheal intubation, the incidence of sore throat varies from 14.4% to 50%. The aim of the study was to compare between benzydamine hydrochloride gel, lidocaine 5% gel and lidocaine 10% spray on the endotracheal tube cuff as regards postoperative sore throat. The present study was carried out on 124 patients admitted to Alexandria university hospitals for lumbar fixation surgery requiring general anesthesia. Patients were randomly allocated into 4 groups. Benzydamine hydrochloride gel, 5% lidocaine hydrochloride gel, 10% lidocaine hydrochloride spray, or normal saline were applied on endotracheal tube cuffs before endotracheal intubation. The patients were examined for sore throat (none, mild, moderate, or severe at 0, 1, 6, 12, and 24 h after extubation. The results were collected, analyzed and presented in table and figure. The highest incidence of postoperative sore throat occurred at 6 h after extubation in all groups. There was a significantly lower incidence of postoperative sore throat in the benzydamine group than 5% lidocaine gel, 10% lidocaine spray, and normal saline groups. The benzydamine group had significantly decreased severity of postoperative sore throat compared with the 10% lidocaine, 5% lidocaine, and normal saline groups at observation time point. Compared with the 5% lidocaine the 10% lidocaine group had significantly increased incidence and severity of postoperative sore throat after extubation. Compared with normal saline the 10% lidocaine group had increased incidence of postoperative sore throat. There were no significant differences among groups in local or systemic side effects. So in conclusion, benzydamine hydrochloride gel on the endotracheal tube cuff is a simple and effective method to reduce the incidence and severity of postoperative sore throat. Application of 10% lidocaine spray should be avoided because of

  17. Comparative study between benzydamine hydrochloride gel, lidocaine 5% gel and lidocaine 10% spray on endotracheal tube cuff as regards postoperative sore throat.

    Science.gov (United States)

    Mekhemar, Nashwa Abdallah; El-Agwany, Ahmed Samy; Radi, Wafaa Kamel; El-Hady, Sherif Mohammed

    2016-01-01

    Postoperative sore throat is a common complication after endotracheal intubation. After tracheal intubation, the incidence of sore throat varies from 14.4% to 50%. The aim of the study was to compare between benzydamine hydrochloride gel, lidocaine 5% gel and lidocaine 10% spray on the endotracheal tube cuff as regards postoperative sore throat. The present study was carried out on 124 patients admitted to Alexandria university hospitals for lumbar fixation surgery requiring general anesthesia. Patients were randomly allocated into 4 groups. Benzydamine hydrochloride gel, 5% lidocaine hydrochloride gel, 10% lidocaine hydrochloride spray, or normal saline were applied on endotracheal tube cuffs before endotracheal intubation. The patients were examined for sore throat (none, mild, moderate, or severe) at 0, 1, 6, 12, and 24h after extubation. The results were collected, analyzed and presented in table and figure. The highest incidence of postoperative sore throat occurred at 6h after extubation in all groups. There was a significantly lower incidence of postoperative sore throat in the benzydamine group than 5% lidocaine gel, 10% lidocaine spray, and normal saline groups. The benzydamine group had significantly decreased severity of postoperative sore throat compared with the 10% lidocaine, 5% lidocaine, and normal saline groups at observation time point. Compared with the 5% lidocaine the 10% lidocaine group had significantly increased incidence and severity of postoperative sore throat after extubation. Compared with normal saline the 10% lidocaine group had increased incidence of postoperative sore throat. There were no significant differences among groups in local or systemic side effects. So in conclusion, benzydamine hydrochloride gel on the endotracheal tube cuff is a simple and effective method to reduce the incidence and severity of postoperative sore throat. Application of 10% lidocaine spray should be avoided because of worsening of postoperative sore

  18. Does Immediate Pain Relief After an Injection into the Sacroiliac Joint with Anesthetic and Corticosteroid Predict Subsequent Pain Relief?

    Science.gov (United States)

    Schneider, Byron J; Huynh, Lisa; Levin, Josh; Rinkaekan, Pranathip; Kordi, Ramin; Kennedy, David J

    2017-05-17

    To determine if immediate pain response following an injection with local anesthetic and corticosteroid predicts subsequent relief.  Prospective observational cohort.  An institutional review board-approved prospective study from a single academic medical center.  Patients with clinical diagnosis of sacroiliac (SIJ) pain and referred for SIJ injection were enrolled; 1 cc of 2% lidocaine and 1 cc of triamcinolone 40 mg/mL were injected into the SIJ. Pain score on 0-10 numeric rating scale (NRS) during provocation maneuvers was recorded immediately before injection, immediately after injection, and at two and four weeks of follow-up. Oswestry Disability Index (ODI) was also recorded.  Various cutoffs were identified to establish positive anesthetic response and successful outcomes at follow-up. These were used to calculated likelihood ratios. Of those with 100% anesthetic response, six of 11 (54.5%, 95% confidence interval [CI]+/-29.4%, +LR 2.6, 95% CI = 1.1-5.9) demonstrated 50% or greater pain relief at follow-up, and four of 11 (36.5%, 95% CI+/-28.4%, +LR 3.00, 95% CI = 1.4-5.1) had 100% relief at two to four weeks. Fourteen of 14 (100%, 95% CI+/-21.5%, -LR 0.0, 95% CI = 0.0-2.1) with an initial negative block failed to achieve 100% relief at follow-up.  Patients who fail to achieve initial relief after SIJ injection with anesthetic and steroid are very unlikely to achieve significant pain relief at follow-up; negative likelihood ratios (LR) in this study, based on how success is defined, range between 0 and 0.9. Clinically significant positive likelihood ratios of anesthetic response to SIJ injection are more limited and less robust, but are valuable in predicting 50% relief or 100% relief at two to four weeks.

  19. High-dose lidocaine does not affect defibrillation efficacy: implications for defibrillation mechanisms.

    Science.gov (United States)

    Ujhelyi, M R; Sims, J J; Miller, A W

    1998-04-01

    This study assessed the effect of low (10 mg.kg-1.h-1) and very high (18 mg.kg-1.h-1) doses of lidocaine on defibrillation energy requirements (DER) to relate changes in indexes of sodium-channel blockade with changes in DER values using a dose-response study design. In group 1 (control; n = 6 pigs), DER values were determined at baseline and during treatment with 5% dextrose in water (D5W) and with D5W added to D5W. In group 2 (n = 7), DER values were determined at baseline and during treatment with low-dose lidocaine followed by high-dose lidocaine. In group 3 (n = 3), DER values were determined at baseline and high-dose lidocaine. Group 3 controlled for the order of lidocaine treatment with the addition of high-dose lidocaine after baseline. DER values in group 1 did not change during D5W. In group 2, low-dose lidocaine increased DER values by 51% (P = 0.01), whereas high-dose lidocaine added to low-dose lidocaine reduced DER values back to within 6% of baseline values (P = 0.02, low dose vs. high dose). DER values during high-dose lidocaine in group 3 also remained near baseline values (16.2 +/- 2.7 to 12.9 +/- 2.7 J), demonstrating that treatment order had no impact on group 2. Progressive sodium-channel blockade was evident as incremental reduction in ventricular conduction velocity as the lidocaine dose increased. Lidocaine also significantly increased ventricular fibrillation cycle length as the lidocaine dose increased. However, the greatest increase in DER occurred when ventricular fibrillation cycle length was minimally affected, demonstrating a negative correlation (P = 0.04). In summary, lidocaine has an inverted U-shaped DER dose-response curve. At very high lidocaine doses, DER values are similar to baseline and tend to decrease rather than increase. Increased refractoriness during ventricular fibrillation may be the electrophysiological mechanism by which high-dose lidocaine limits the adverse effects that low-dose lidocaine has on DER values

  20. The incidence of transient neurologic syndrome after spinal anesthesia with lidocaine or bupivacaine: The effects of needle type and surgical position: brief report

    Directory of Open Access Journals (Sweden)

    Etezadi F

    2011-10-01

    Full Text Available "nBurning Transient Neurologic Syndrome (TNS which was first described by Schneider et al in 1993, is defined as a transient pain and dysesthesia in waist, buttocks and the lower limbs after spinal anesthesia.1,2 The incidence of TNS after spinal anesthesia with lidocaine is reported to be as high as 10-40%.3,4 This prospective study was designed to determine the incidence of TNS with two different types of drugs, lidocaine and bupivacaine, in lithotomy or supine positions as the primary outcomes and to determine the association between two different types of needles and surgical positions with the occurrence of TNS as the secondary outcome."nThe present study was conducted on 250 patients (ASA I-II, aged 18-60 years old, who were candidates for surgery in supine or lithotomy positions. According to the needle type (Sprotte or Quincke and the local anesthetic (lidocaine or bupivacaine all patients were randomly divided into four groups. After establishing standard monitoring, spinal anesthesia was performed in all sitting patients by attending anesthesiologists at L2-L3 or L3-L4 levels. The patients were placed in supine or lithotomy position, in regards to the surgical procedure. During the first three postoperative days, patients were observed for post spinal anesthesia complications, especially TNS. Any sensation of pain, dysesthesia, paresthesia or hyperalgesia in the low back area, buttocks, the anterior or posterior thigh, knees, either foot or both feet were recorded. Moreover, duration of pain, its radiation and its relation to sleep and the patients' position were all carefully considered. Ultimately, the patients' response to opioid (pethidine for analgesia was determined."nThe incidence of TNS was higher when spinal anesthesia was induced with lidocaine (68% vs. 22%, P=0.003. TNS developed in 85% of the patients in lidocaine group and 58% in bupivacaine group after surgery in lithotomy position (P=0.002. In 77 patients pain

  1. Blockade of the voltage-dependent sodium current in isolated rat hippocampal neurons by tetrodotoxin and lidocaine.

    Science.gov (United States)

    Kaneda, M; Oyama, Y; Ikemoto, Y; Akaike, N

    1989-04-10

    The effects of tetrodotoxin and lidocaine on the voltage-dependent sodium current (INa) were studied in the CA1 pyramidal neurons isolated acutely from rat hippocampus using a 'concentration-clamp' technique which combines the intracellular perfusion with a rapid external solution change within a few ms. Tetrodotoxin (TTX) exerted its inhibitory action in time- and dose-dependent manner on the peak amplitude of INa without any apparent effects on both the current activation and inactivation processes of the current. The time course for reaching a steady-state of the inhibitory action shortened with increasing TTX concentration, but the time course of recovery from the inhibition after washing out the toxin was quite the same at any concentrations used. Lidocaine also inhibited dose-dependently the INa, though with slightly accelerating both the activation and inactivation processes. The time courses for reaching the steady-state inhibition and the recovery from the inhibition were much shorter than those in the case of TTX. The results indicate that the voltage-dependent sodium channel of mammalian brain neuron is TTX-sensitive as well as that of peripheral neuron and that the mode of TTX inhibition on the INa is quite different from that of lidocaine.

  2. Effect of patient age, breast density, and topical anesthetic cream on perceived pain with sentinel lymph node scintigraphy.

    Science.gov (United States)

    Chandler, Kimberly J; Hunt, Christopher H; Morreale, Robert; Johnson, Geoffrey B; Peller, Patrick J

    2012-03-01

    Although an extremely useful technique for sentinel lymph node (SLN) identification in breast cancer, injections of (99m)Tc-sulfur colloid can be quite painful. The purpose of this study was to determine whether there is a correlation between perceived pain of injection and age, breast density, or timing of topical anesthetic cream administration. A retrospective review was conducted of women with breast cancer who received injections for sentinel lymphoscintigraphy from 2008 to 2010. After receiving 4 unilateral, intradermal, periareolar injections, women ranked their pain using a comparative scale (0 = no pain; 10 = unbearable pain). There were 3 categories based on length of time that topical anesthetic cream (2.5% lidocaine and 2.5% prilocaine) was applied before injection (1 h prior, 20 min prior, or no cream). In addition, other demographic information and breast density on mammography were analyzed for correlation with the comparative pain scale. Among the 82 women (mean age, 58 y; range, 32-87 y), a wide spectrum on the comparative pain scale was recorded (mean, 4.0; SD, 2.6), with 35% attesting to significant pain, rated 5 or greater. The demographic information and breast density per the Breast Imaging Reporting and Data System were retrospectively reviewed (density: fatty, 14.6%; scattered fibroglandular, 36.6%; heterogeneous, 39.0%; extremely dense, 9.8%). Using bivariate linear regression, no correlation between the comparative pain scale and age (R(2) = 0.0029, P = 0.63) or breast density (R(2) = 0.00049, P = 0.84) was identified. Most patients had topical anesthetic cream applied 20 min before injection (n = 47, or 57.3%) with 24 (29.3%) having topical anesthetic cream applied 1 h beforehand. Eleven women (13.4%) had no topical anesthetic cream applied because of patient preference or concern about allergy. Again, no correlation was found between comparative pain scale and time of application or use of topical anesthetic cream (Kruskal-Wallis: χ(2

  3. Design, Synthesis, and Evaluation of Novel 2,6-Disubstituted Phenol Derivatives as General Anesthetics.

    Science.gov (United States)

    Qin, Linlin; Ren, Lei; Wan, Songlin; Liu, Guoliang; Luo, Xinfeng; Liu, Zhenhong; Li, Fangqiong; Yu, Yan; Liu, Jianyu; Wei, Yonggang

    2017-05-11

    A novel series of optically active 2,6-disubstituted alkylphenols with improved anesthetic profiles compared to widely used propofol were synthesized. The incorporation of the cyclopropyl group not only increased the steric effect but also introduced stereoselective effects over their anesthetic properties. Compounds 1, 2, and 6 were selected as potential candidates for further preclinical development including studies of their water-soluble prodrugs. Clinical studies of candidate compound 6 (Haisco HSK3486) as a general anesthetic are being performed in Australia and China.

  4. The disposition of lidocaine during a 12-hour intravenous infusion to postoperative horses.

    Science.gov (United States)

    Milligan, M; Kukanich, B; Beard, W; Waxman, S

    2006-12-01

    Lidocaine is administered as an intravenous infusion to horses for a variety of reasons, but no study has assessed plasma lidocaine concentrations during a 12-h infusion to horses. The purpose of this study was to evaluate the plasma concentrations and pharmacokinetics of lidocaine during a 12-h infusion to postoperative horses. A second purpose of the study was to evaluate the in vitro plasma protein binding of lidocaine in equine plasma. Lidocaine hydrochloride was administered as a loading dose, 1.3 mg/kg over 15 min, then by a constant rate IV infusion, 50 microg/kg/min to six postoperative horses. Lidocaine plasma concentrations were measured by a validated high-pressure liquid chromatography method. One horse experienced tremors and collapsed 5.5 h into the study. The range of plasma concentrations during the infusion was 1.21-3.13 microg/mL. Lidocaine plasma concentrations were significantly increased at 0.5, 4, 6, 8, 10 and 12 h compared with 1, 2 and 3 h. The in vitro protein binding of lidocaine in equine plasma at 2 microg/mL was 53.06+/-10.28% and decreased to 27.33+/-9.72% and 29.52+/-6.44% when in combination with ceftiofur or the combination of ceftiofur and flunixin, respectively. In conclusion, a lower lidocaine infusion rate may need to be administered to horses on long-term lidocaine infusions. The in vitro protein binding of lidocaine is moderate in equine plasma, but highly protein bound drugs may displace lidocaine increasing unbound concentrations and the risk of lidocaine toxicity.

  5. Closed Continuous Irrigation With Lidocaine and Immediate Mobilization for Treatment of Pyogenic Tenosynovitis.

    Science.gov (United States)

    Knackstedt, Rebecca; Tyler, Joyce; Bernard, Steven

    2017-09-01

    Pyogenic flexor tenosynovitis treatment consists of either closed continuous irrigation with sterile saline or antibiotic solution, or open debridement and irrigation. These treatment approaches serve to resolve the infection, but are extremely painful and residual stiffness can be devastating to the patient. We describe herein our approach to managing pyogenic flexor tenosynovitis. To provide continuous irrigation, a butterfly catheter with needle removed is utilized with irrigation holes cut into the tubing. The catheter is inserted into the tendon sheath at the level of the Al pulley and brought out at the level of the A5 pulley. A knot is tied in the end of the catheter for retention, eliminating the need for sutures. Immediately postoperative, continuous irrigation with sterile saline mixed with lidocaine is initiated and is titrated to achieve pain-free motion in the finger. Occupational therapy begins an aggressive course of active and passive range of motion exercises immediate postoperatively, which is continued for the remainder of hospitalization. Our approach of continuous infusion of a lidocaine solution allows for pain-free movement immediately postoperatively to mechanically debride tissue, as well as allow for early active range of motion. We have obtained excelleepaknt results with this technique in all of our cases.

  6. Child with aplastic anemia: Anesthetic management

    Directory of Open Access Journals (Sweden)

    Manpreet Kaur

    2012-01-01

    Full Text Available Aplastic anemia is a rare heterogeneous disorder of hematopoietic stem cells causing pancytopenia and marrow hypoplasia with the depletion of all types of blood cells. This results in anemia, neutropenia and thrombocytopenia, which pose a challenge to both surgical and anesthetic management of such cases. We report a child with aplastic anemia who sustained traumatic ulcer on the arm and underwent split-thickness skin grafting under general anesthesia. There are only two case reports on anesthetic considerations in aplastic anemia patients in the literature. The anesthetic management is challenging because of the rarity of the disease, associated pancytopenia and immunosuppression.

  7. Development of a behavioral assessment of craniofacial muscle pain in lightly anesthetized rats.

    Science.gov (United States)

    Ro, Jin Y; Capra, Norman; Masri, Radi

    2003-07-01

    In this study, a new behavioral assessment of craniofacial muscle pain in the lightly anesthetized rat is described. Intramuscular injections with algesic agents in lightly anesthetized rats evoked a characteristic ipsilateral hindpaw shaking behavior for several minutes similar to previously described orofacial pain-induced grooming behavior in awake rats (Neurosci Lett 103 (1989) 349, Pain 62 (1995) 295). Eighty-two male Sprague-Dawley rats were used in a series of experiments to study whether this behavior could serve as a valid measure of craniofacial muscle pain. First, we demonstrated that different algesic chemicals, mustard oil (20%), formalin (3%) or hypertonic saline (5%) injected in the mid-region of the masseter muscle effectively elicited the hindpaw shaking behavior. The behavior was only minimally evoked with vehicle injection. Repeated administrations of hypertonic saline, a short duration non-sensitizing algogen, demonstrated reproducibility of the assay. Second, we showed that the peak and overall magnitude of the shaking behavior evoked by injections with different concentrations of mustard oil (1 and 5%) changed in a concentration dependent manner. Finally, we showed that systemic administration of morphine sulfate (3 and 0.3 mg/kg, i.p.) dose dependently attenuated mustard oil induced hindpaw-shaking behavior. Lidocaine injected locally 5 min prior to mustard oil injection also significantly decreased the hindpaw shaking behavior. Based on these results we concluded that ipsilateral hindpaw shaking in lightly anesthetized rats is a stereotypical behavior evoked by noxious muscle stimulation and can be used as a reliable behavioral measure to assess craniofacial muscle pain.

  8. Local anesthetics: dentistry's most important drugs.

    Science.gov (United States)

    Malamed, S F

    1994-12-01

    One hundred and fifty years ago, Horace Wells opened the door to local anesthetics. Since then, many advances have been made in pain control. The development of dentistry's most important drugs is highlighted here.

  9. LOCAL ANESTHETICS IN PATIENTS WITH CARDIOVASCULAR DISEASES.

    Directory of Open Access Journals (Sweden)

    risto Daskalov

    2015-03-01

    Full Text Available A significant problem in the dental medicine is pain alleviation. Many studies in the dental anesthesiology result in the production of new agents for locoregional anesthesia. Objective: This article aim to present the results of the last studies on the effect of the local anesthetics used in the oral surgery on patients with cardiovascular diseases. Material: A general review of the existing literature on the effect of the adrenaline, included as vasoconstrictor in the local anesthetics, used in patients with cardiovascular diseases is made. The benefits of vasoconstrictors for the quality of the anesthetic effect are proven. Conclusion: A small amount of adrenaline in the anesthetic solution does not result in complications development in patients with controlled cardiovascular diseases. Articaine is recommended agent of first choice for local anesthesia in the oral surgery.

  10. [Facial locoregional anesthetics: principles and precautions].

    Science.gov (United States)

    Lefort, H; Lacroix, G; Cordier, A; Bey, E; Duhamel, P

    2009-12-01

    Facial locoregional anesthetics (ALR) with nervous blocks are simple and reliable to perform, need little technical resources with a very low iatrogenic risk. These blocks allow anesthesia without deforming wound banks using the same materials as usual local anesthetic procedures. Three principal nervous blocks, in a straight line along the vertical pupil axis, allow managing - even extensive - facial wounds. Few side effects may occur which can be easily prevented. It is a good alternative to local anesthetic for the treatment of extensive and deep areas which is performed with a lower number of injections and a high rate of success. These techniques are easy to learn and practise. These anesthetic techniques allow a nice treatment of different kinds of facial wounds from simple suture to flaps.

  11. SYSTEMIC TOXIC REACTIONS TO LOCAL ANESTHETICS

    Science.gov (United States)

    Moore, Daniel C.; Green, John

    1956-01-01

    The topical use of anesthetic agents involves an element of risk. Systemic toxic reactions are rare, but they do occur and may result in death. When a reaction occurs from a topical application, it usually progresses rapidly to respiratory and cardiovascular collapse, and thus therapy must be instituted with more haste to avoid deaths. Fatal systemic toxic reactions from topically administered anesthetic drugs are, in effect, usually not due to well informed use of the drug but to misuse owing to less than complete understanding of absorption. Emphasis is placed on the causes, prophylaxis and treatment of severe systemic toxic reactions which follow the topical application of local anesthetic drugs. If systemic toxic reactions resulting from a safe dose of a local anesthetic agent are correctly treated, there will usually follow an uneventful recovery rather than a catastrophe. PMID:13343009

  12. The immediate effects of lidocaine iontophoresis using interferential current on pressure sense threshold and tactile sensation.

    Science.gov (United States)

    Yoosefinejad, Amin Kordi; Motealleh, Alireza; Abbasnia, Keramatollah

    2016-01-01

    Iontophoresis is the noninvasive delivery of ions using direct current. The direct current has some disadvantages such as skin burning. Interferential current is a kind of alternating current without limitations of direct current; so the purpose of this study is to investigate and compare the effects of lidocaine, interferential current and lidocaine iontophoresis using interferential current. 30 healthy women aged 20-24 years participated in this randomized clinical trial study. Pressure, tactile and pain thresholds were evaluated before and after the application of treatment methods. Pressure, tactile and pain sensitivity increased significantly after the application of lidocaine alone (p < 0.005) and lidocaine iontophoresis using interferential current (p < 0.0001). Lidocaine iontophoresis using interferential current can increase perception threshold of pain, tactile stimulus and pressure sense more significantly than lidocaine and interferential current alone.

  13. Chronic Intermittent Hypobaric Hypoxia Pretreatment Ameliorates Ischemia-Induced Cognitive Dysfunction Through Activation of ERK1/2-CREB-BDNF Pathway in Anesthetized Mice.

    Science.gov (United States)

    Wang, Jintian; Zhang, Shixiao; Ma, Huijuan; Yang, Shijie; Liu, Zhao; Wu, Xiaolei; Wang, Sheng; Zhang, Yi; Liu, Yixian

    2017-02-01

    Chronic intermittent hypobaric hypoxia (CIHH) has protective effects on heart and brain against ischemia injury through mobilizing endogenous adaptive mechanisms. However, whether CIHH prevents against cognitive impairment was not elucidated. The present study aimed to investigate the effect and mechanism of CIHH treatment on ischemia/reperfusion (IR)-induced cognitive dysfunction. Mice were randomly divided into 8 groups: Control, Sham, CIHH (simulating 5000 m high-altitude for 28 days, 6 h per day), IR (three 16-min occlusions of bilateral common carotid arteries interrupted by two 10-min intervals), CIHH + IR, PD98059 (inhibitor of MEK1/2) + CIHH + IR, PD98059 + Sham and PD98059 + IR group. Morris water maze and step-down passive avoidance tests were performed to evaluate the capability of learning and memory 1 month after ischemia. Thionine dyeing was to examine histological manifestations of pyramidal neurons in hippocampus CA1 region. Western blotting assay was for measurement of the protein expressions in ERK1/2-CREB-BDNF signaling pathway. There were a shorter escape latency and a longer percentage of time retaining in the target quadrant in Morris water maze test, fewer times of errors in the step-down avoidance test and a higher neuronal density of the hippocampal CA1 subfield in CIHH + IR group than in IR group. CIHH upregulated the expressions of BDNF, phosphorylated CREB, ERK1/2 and TrkB with or without ischemia. The protective effects of CIHH were abolished by PD98059 administration 15 min before ischemia. CIHH ameliorated ischemia-induced cognitive dysfunction through activation of ERK1/2-CREB-BDNF signaling pathway.

  14. Anesthetizing animals: Similar to humans yet, peculiar?

    OpenAIRE

    Madhuri S Kurdi; Ramaswamy, Ashwini H

    2015-01-01

    From time immemorial, animals have served as models for humans. Like humans, animals too have to undergo several types of elective and emergency surgeries. Several anesthetic techniques and drugs used in humans are also used in animals. However, unlike humans, the animal kingdom includes a wide variety of species, breeds, and sizes. Different species have variable pharmacological responses, anatomy, temperament, behavior, and lifestyles. The anesthetic techniques and drugs have to suit differ...

  15. The mechanism and site of action of lidocaine hydrochloride in guinea pig inner ear.

    Science.gov (United States)

    Laurikainen, E; Lin, X; Nuttall, A L; Dolan, D F

    1997-07-01

    Lidocaine was applied to the round window (RW) in order to localize its site of action in the cochlea. Cochlear microphonic (CM), summating potential (SP), and compound action potential (CAP) input/output functions were measured to a 16 kHz tone burst to assess the functional changes of the cochlea. In separate experiments, the effect of lidocaine on the whole cell current of isolated outer hair cells (OHC) was studied. A dose of 2 microliters of 40 mM lidocaine in saline solution, when applied to the RW, caused a small change in all measured variables, indicating a passage of the drug through the RW membrane to sites of action. However, 160 mM of lidocaine further decreased CM, SP, and CAP by a total of 40% from the control. A partial recovery occurred for CM during the 30 min follow-up period. CAP and SP continued to decline. In isolated OHCs, lidocaine decreased the whole cell current in a dose-dependent fashion. The KD for lidocaine effect on OHCs was 7 mM. Our in vivo results indicate that lidocaine affects OHCs and reduces CM, causing a subsequent reduction in SP and CAP. The increased effect of lidocaine on CAP and SP, while CM is recovering, suggests an additional specific effect of lidocaine on the cochlear nerve and/or on inner hair cells. Considering that lidocaine alters OHC current (in isolated hair cells) and that lidocaine does not affect endocochlear potential [Laurikainen et al. Acta Otolaryngol (Stockh) 1991: 112: 800-9], the observed CM changes are most likely due to an in vivo effect on OHCs. Thus, the early effect of lidocaine on the cochlea appears to be due to a significant change in organ of Corti function, rather than to direct anesthesia of the cochlear nerve. Later, an independent effect of the drug may occur on neural tissues in the inner ear.

  16. A pilot study of the effect of pressure-driven lidocaine spray on airway topical anesthesia for conscious sedation intubation

    Institute of Scientific and Technical Information of China (English)

    JIANG Hai; MIAO Hai-sheng; JIN San-qing; CHEN Li-hong; TIAN Jing-ling

    2011-01-01

    Background Difficult airway remains not only a challenge to the anesthesiologists,but also a life-threatening event to the patients.Awake intubation is the principal choice to deal with difficult airway,and a key point for awake intubation is airway topical anesthesia.Yet,so far there is no ideal topical anesthesia approach for awake intubation.This study aimed at evaluating the effect of pressure-driven (by 10 L/min oxygen flow) lidocaine spray on airway topical anesthesia in order to find a powerful and convenient method for airway topical anesthesia for conscious sedation intubation.Methods Thirty adult patients referred for elective surgery under general anesthesia,aged 18-60 years and Mallampati class Ⅰ or Ⅱ,were recruited for the study.Before topical anesthesia,the observer's assessment of alert and sedation (OAA/S) scale was controlled between 3 and 4 by intravenous midazolam (0.03 mg/kg),propofol (2 mg.kg1·h-1) andremifentanil (0.05 μg.kg-1·min-1).Ten minutes after sedation,topical anesthesia was performed with the pressure-driven lidocaine spray; the driving pressure was achieved by an oxygen flow of 10 L/min.After topical anesthesia,tracheal intubation was performed and the intubation condition was assessed with modified the Erhan's intubation condition score by an experienced anesthesiologist,and a score of less than 10 was considered to be satisfactory.Attempts to intubate the patient were recorded,and the complications such as local anesthetic toxicity,mucosa injury,and respiration depression were also recorded.The mean arterial blood pressure (MAP),heart rate (HR) and pulse oxygen saturation (SpO2) were recorded at different time points before and after intubation.Patients were asked 24 hours after the operation whether they could recall the events during intubation.Results All patients were intubated at the first attempt,the average intubation condition score was 7.0±1.1,from 6 to 10,satisfied intubation condition.MAP and HR increased

  17. Anaphylactic shock following intraurethral lidocaine administration during transurethral resection of the prostate

    Directory of Open Access Journals (Sweden)

    M Sinha

    2008-01-01

    Full Text Available Anaphylactic shock was noted following an apparently uneventful transurethral resection of the prostate (TURP. Lidocaine jelly was used prior to urethral dilatation and before placement of three-way Foley. Lidocaine sensitivity was diagnosed serendipitously when lidocaine jelly was used for application of ECG electrodes. Anaphylaxis may be one of the rare differentials to be considered in a patient with postoperative shock following TURP. This report highlights a potentially fatal complication of an apparently innocuous and ubiquitous urological use of lidocaine.

  18. The effect of perioperative intravenous lidocaine and ketamine on recovery after abdominal hysterectomy

    National Research Council Canada - National Science Library

    Grady, Martin V; Mascha, Edward; Sessler, Daniel I; Kurz, Andrea

    2012-01-01

    Perioperative ketamine infusion reduces postoperative pain; perioperative lidocaine infusion reduces postoperative narcotic consumption, speeds recovery of intestinal function, improves postoperative fatigue, and shortens hospital stay...

  19. Intravenous lidocaine infusion--a new treatment of chronic painful diabetic neuropathy?

    DEFF Research Database (Denmark)

    Kastrup, J; Petersen, P; Dejgård, A

    1987-01-01

    In a randomized double-blind, cross-over study the effect of intravenous lidocaine (5 mg/kg body weight) on the symptoms and signs of painful diabetic neuropathy of more than 6 months duration has been evaluated. Using a clinical symptom scale, there was significant beneficial effect 1 and 8 days...... alternative treatment of chronic painful diabetic neuropathy....... after lidocaine infusion compared to after saline infusion (P less than 0.05 and P less than 0.02, respectively). The duration of the individual effect ranged from 3 to 21 days. Lidocaine infusion had no effect on the objective measurements of neuropathy. Intravenous lidocaine infusion seems to be a new...

  20. Evaluation of the Population Pharmacokinetic Properties of Lidocaine and its Metabolites After Long-Term Multiple Applications of a Lidocaine Plaster in Post-Herpetic Neuralgia Patients.

    Science.gov (United States)

    Bursi, Roberta; Piana, Chiara; Grevel, Joachim; Huntjens, Dymphy; Boesl, Irmgard

    2017-01-12

    Lidocaine 5% medicated plaster is the first lidocaine containing product for chronic use. As no previous investigations have been conducted to evaluate the population pharmacokinetics of long-term exposure to lidocaine 5% medicated plasters, further insights into the evaluation of the pharmacokinetic properties of lidocaine and its metabolites were needed for the assessment of its safety. The population pharmacokinetic properties of lidocaine and its metabolites were evaluated after multiple applications of lidocaine 5% medicated plasters based on data collected for up to 14.5 months from two phase III clinical trials (up to 2.5 months in the first trial, and up to 12 months in a follow-up trial) in post-herpetic neuralgia patients. Modeling was performed using nonlinear mixed effects as implemented in NONMEM(®) (nonlinear mixed-effect modeling) v.5. A stepwise forward inclusion and backward elimination procedure were used for covariate model building. The model provides reliable estimates of the pharmacokinetic behavior of lidocaine after medicated plaster application. It was validated using simulations and showed adequate predictive properties. Apparent Clearance was estimated to be 48 L/h after application of two or fewer plasters, whereas its value increased to 67 L/h after application of three plasters. Model-based simulations predicted no accumulation of lidocaine or any of its metabolites after long-term exposure of three simultaneous plasters up to 1 year. The variability explained by adding covariates into the model for the long-term exposures of lidocaine following one plaster or three simultaneous plaster applications was found to be very small with respect to the overall between-subject variability. In conclusion, exposure to lidocaine after the application of the lidocaine medicated plaster was found to be primarily affected by the number of plasters simultaneously applied, i.e., it increased with the number of applied patches, but less than

  1. The bonding of anesthetics and antibiotics on the carboxymethylcellulose

    Directory of Open Access Journals (Sweden)

    Rodić-Grabovac Branka B.

    2007-01-01

    Full Text Available The preparation of biologically active material is one of the most interesting trends in the chemical modification of cellulose. The possibility of obtaining biologically active cellulosic material by sorption of procaine hydrochloride and gentamicin sulphate on CMC was investigated in this paper. The sorption of therapeutics on CMC samples with different degree of substitution was carried out in water solutions of anesthetic and antibiotic, while the desorption was done in 0.95% NaCl solution. The amount of bonded and released therapeutics was determined by UV spe-ctrophotometry. It was found that degree of substitution of car-boxymethylcellulose and concentration of chemotherapeutic water solution have significant influence on the amount of bonded anesthetic and antibiotic. The maximum amount of bonded chemotherapeutic was 72.15 mg of procaine hydrochloride and 165.49 mg of gentamicin sulphate per gram CMC. In both cases the amounts of bonded chemotherape-utics correspond to the concentration of local anesthetic and antibiotic preparation that are used in therapeutic purposes.

  2. The P-glycoprotein inhibitor quinidine decreases the threshold for bupivacaine-induced, but not lidocaine-induced, convulsions in rats.

    Science.gov (United States)

    Funao, Tomoharu; Oda, Yutaka; Tanaka, Katsuaki; Asada, Akira

    2003-10-01

    To examine whether inhibition of P-glycoprotein (P-gp) activity by quinidine affects the central nervous system toxicity of lidocaine and racemic bupivacaine (bupivacaine). Forty male Sprague-Dawley rats were randomly divided into four groups (n = 10). Fifteen minutes following administration of 15 mg x kg(-1) of quinidine (QL and QB groups) or saline (L and B groups), lidocaine (L and QL groups, 4 mg x kg(-1) x min(-1)) or bupivacaine (B and QB groups, 1 mg x kg(-1) x min(-1)) was infused until convulsions occurred. Concentrations of lidocaine and its primary metabolite, monoethylglycinexylidide (MEGX) and bupivacaine in plasma and in the brain at the onset of convulsions were measured by high-performance liquid chromatography. There were no differences in the dose of lidocaine required to induce convulsions between the L and QL groups. There were no differences in the concentrations of total (L = 17.2 +/- 3.5, QL = 16.6 +/- 2.6 micro g x mL(-1)) or unbound lidocaine (L = 7.8 +/- 2.5, QL = 7.3 +/- 2.3 micro g x mL(-1)), total (L = 1.2 +/- 0.5, QL = 1.3 +/- 0.7 micro g x mL(-1)) or unbound MEGX (L = 0.9 +/- 0.5, QL = 0.8 +/- 0.4 micro g x mL(-1)) in plasma, total lidocaine or MEGX in the brain at the onset of convulsions between the L and QL groups. The dose of bupivacaine required to induce convulsions was comparable in the B and QB groups. At the onset of convulsions, plasma concentrations of both total (B = 4.9 +/- 1.1, QB = 4.0 +/- 0.6 micro g x mL(-1), P = 0.03) and unbound bupivacaine (B = 1.4 +/- 0.6, QB = 0.9 +/- 0.2 micro g x mL(-1), P = 0.02) were significantly lower in the QB group than in the B group. There were no differences in concentration of total bupivacaine in the brain between the B and QB groups. These results suggest that quinidine inhibited P-gp activity, resulting in increased brain/plasma concentration ratio of bupivacaine, but not of lidocaine, and decreased the threshold of plasma concentration for bupivacaine-induced convulsions.

  3. 利多卡因注射液滴眼用于激光角膜原位磨镶术表面麻醉的效果研究%The effect of Lidocaine on topical anesthesia for LASIK

    Institute of Scientific and Technical Information of China (English)

    李淑萍; 刘运甲; 李志强

    2011-01-01

    Objective To discuss the effect of 2% Lidocaine solution for injection on topical anesthesia for laser in situ keratomileusis (LASIK). Methods Totally 100 cases (200 eyes) were randomly divided into two groups,2% Lidocaine group and Oxybuprocaine group. Each group contained 50 cases ( 100eyes). LASIK was done under the topical anesthesia of those two medicine respectively. The anesthetic effect was assessed by the feeling of pain and tactile perception of the patients. Results The surgery was done smoothly in 98 eyes under Lidocaine anesthesia. There was mild pain in two eyes during the surgery. The pain disappeared when an additional drop of Lidocaine was used. In Oxybuprocaine group, the surgery was done smoothly in 99 eyes. There was mild discomfort in one eye, and the surgery was done without additional treatment. Conclusion 2% Lidocaine injection can provide good topical anesthetic effect for LASIK.%目的 探讨2%利多卡因注射液滴眼用于准分子激光角膜原位磨镶术(LASIK)表面麻醉的效果.方法 100例(200眼)随机分成利多卡因组和奥布卡因组,每组50例(100眼).两组分别在两种药物的表面麻醉下进行LASIK,根据术中患者对疼痛和触觉的感受评价麻醉效果.结果 利多卡因组中98眼能顺利完成手术,2眼稍感疼痛,追加滴利多卡因1滴后顺利完成手术.奥布卡因组99眼顺利完成手术,1眼稍感不适,未做处理,也顺利完成手术.结论 2%利多卡因注射液滴眼用于LASIK表面麻醉效果良好.

  4. Evaluation of the effect of locally administered amitriptyline gel as adjunct to local anesthetics in irreversible pulpitis pain

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    Moghadamnia A

    2009-01-01

    Full Text Available Background: Amitriptyline is one of the most common tricyclic antidepressants, which binds to pain sensory nerve fibers close to the sodium channel; hence, it could interact to some degree with receptors of local anesthetics. This study was designed to assess the additional analgesic effects of 2% Amitriptyline local gel administration in irreversible pulpitis pain of the molars. Materials and Methods: This study was a randomized, double-blind clinical trial that was performed on 56 consented adult patients who did not receive enough analgesia after a lidocaine nerve block for their tooth pulpitis pain. Patients were treated with 0.2 ml of either 2% amitriptyline or placebo, which was directly injected into their mandibular molar pulp chamber after they had received two routine lidocaine injections. Patients were asked to score their pain as a mark on a 10-cm Visual Analogue Scale (VAS at different timepoints: 0 (just before gel administration, 1, 3, 5, 7, and 9 minutes after the treatments. Results: There was a 92.5% decrease in VAS scores of patients 9 minutes after amitriptyline administration compared to Time 0, while in the placebo group this difference was only 13.5%. Further, in the amitriptyline group, the VAS score at all timepoints was statistically different from Time 0 ( P < 0.01. The overall pain reduction and its trend was significantly higher in the amitriptyline group compared with the placebo group ( P < 0.001. Conclusion: Inter-pulp space administration of amitriptyline 2% gel for completing analgesia in irreversible pulpitis pain could be effective and useful as a conjunctive therapy to injections of local anesthetics.

  5. Lidocaine preferentially inhibits the function of purinergic P2X7 receptors expressed in Xenopus oocytes.

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    Okura, Dan; Horishita, Takafumi; Ueno, Susumu; Yanagihara, Nobuyuki; Sudo, Yuka; Uezono, Yasuhito; Minami, Tomoko; Kawasaki, Takashi; Sata, Takeyoshi

    2015-03-01

    Lidocaine has been widely used to relieve acute pain and chronic refractory pain effectively by both systemic and local administration. Numerous studies reported that lidocaine affects several pain signaling pathways as well as voltage-gated sodium channels, suggesting the existence of multiple mechanisms underlying pain relief by lidocaine. Some extracellular adenosine triphosphate (ATP) receptor subunits are thought to play a role in chronic pain mechanisms, but there have been few studies on the effects of lidocaine on ATP receptors. We studied the effects of lidocaine on purinergic P2X3, P2X4, and P2X7 receptors to explore the mechanisms underlying pain-relieving effects of lidocaine. We investigated the effects of lidocaine on ATP-induced currents in ATP receptor subunits, P2X3, P2X4, and P2X7 expressed in Xenopus oocytes, by using whole-cell, two-electrode, voltage-clamp techniques. Lidocaine inhibited ATP-induced currents in P2X7, but not in P2X3 or P2X4 subunits, in a concentration-dependent manner. The half maximal inhibitory concentration for lidocaine inhibition was 282 ± 45 μmol/L. By contrast, mepivacaine, ropivacaine, and bupivacaine exerted only limited effects on the P2X7 receptor. Lidocaine inhibited the ATP concentration-response curve for the P2X7 receptor via noncompetitive inhibition. Intracellular and extracellular N-(2,6-dimethylphenylcarbamoylmethyl) triethylammonium bromide (QX-314) and benzocaine suppressed ATP-induced currents in the P2X7 receptor in a concentration-dependent manner. In addition, repetitive ATP treatments at 5-minute intervals in the continuous presence of lidocaine revealed that lidocaine inhibition was use-dependent. Finally, the selective P2X7 receptor antagonists Brilliant Blue G and AZ11645373 did not affect the inhibitory actions of lidocaine on the P2X7 receptor. Lidocaine selectively inhibited the function of the P2X7 receptor expressed in Xenopus oocytes. This effect may be caused by acting on sites in the ion

  6. Adjuvants to local anesthetics: Current understanding and future trends

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    Swain, Amlan; Nag, Deb Sanjay; Sahu, Seelora; Samaddar, Devi Prasad

    2017-01-01

    Although beneficial in acute and chronic pain management, the use of local anaesthetics is limited by its duration of action and the dose dependent adverse effects on the cardiac and central nervous system. Adjuvants or additives are often used with local anaesthetics for its synergistic effect by prolonging the duration of sensory-motor block and limiting the cumulative dose requirement of local anaesthetics. The armamentarium of local anesthetic adjuvants have evolved over time from classical opioids to a wide array of drugs spanning several groups and varying mechanisms of action. A large array of opioids ranging from morphine, fentanyl and sufentanyl to hydromorphone, buprenorphine and tramadol has been used with varying success. However, their use has been limited by their adverse effect like respiratory depression, nausea, vomiting and pruritus, especially with its neuraxial use. Epinephrine potentiates the local anesthetics by its antinociceptive properties mediated by alpha-2 adrenoreceptor activation along with its vasoconstrictive properties limiting the systemic absorption of local anesthetics. Alpha 2 adrenoreceptor antagonists like clonidine and dexmedetomidine are one of the most widely used class of local anesthetic adjuvants. Other drugs like steroids (dexamethasone), anti-inflammatory agents (parecoxib and lornoxicam), midazolam, ketamine, magnesium sulfate and neostigmine have also been used with mixed success. The concern regarding the safety profile of these adjuvants is due to its potential neurotoxicity and neurological complications which necessitate further research in this direction. Current research is directed towards a search for agents and techniques which would prolong local anaesthetic action without its deleterious effects. This includes novel approaches like use of charged molecules to produce local anaesthetic action (tonicaine and n butyl tetracaine), new age delivery mechanisms for prolonged bioavailability (liposomal

  7. Ketamine prevents lidocaine-caused neurotoxicity in the CA3 hippocampal and basolateral amygdala regions of the brain in adult rats.

    Science.gov (United States)

    Lopez-Galindo, Gabriel Eduardo; Cano-Europa, Edgar; Ortiz-Butron, Rocio

    2008-01-01

    Our objective was to prove whether blocking the action of glutamate on N-methyl-D: -aspartate (NMDA) receptors could prevent the neuronal damage caused by the acute administration of lidocaine. Twenty male 2-month-old Wistar rats were randomly assigned to the following groups (n = 5 in each group): groups I and II received 0.9% saline i.p., and groups III and IV received 100 mg x kg(-1) of ketamine i.p. Thirty minutes later, groups I and III were again dosed with 0.9% saline i.p., and groups II and IV received 60 mg x kg(-1) of lidocaine i.p. During treatment, the rectal temperature of the animals was monitored and maintained at 37.5 +/- 0.5 degrees C. Ten days after administration of the agents, all rats were transcardially perfused, under pentobarbital anesthesia, with 10% formaldehyde. Their brains were removed and were embedded in paraffin. Coronal cuts of 7 microm were obtained from -2.3 to -3.8 mm from the bregma. Each brain section was stained with cresyl violet-eosin. The number of normal and abnormal pyramidal neurons in the CA3 hippocampal region and the number of large and medium neurons in the basolateral amygdala within an area of 10 000 microm2 were evaluated. We found that lidocaine significantly reduced the number of normal neurons in both the CA3 hippocampal region (F (3,16) = 225.8; P lidocaine-induced damage in the CA3 hippocampal region and the basolateral amygdala. These results demonstrate the participation of NMDA-receptor activation by lidocaine in the CA3 hippocampal and basolateral amygdala regions as a neurotoxic mechanism.

  8. Sevoflurane: a new inhalational anesthetic agent.

    Science.gov (United States)

    Wallin, R F; Regan, B M; Napoli, M D; Stern, I J

    1975-01-01

    Laboratory screening of a series of halogenated methyl isopropyl ethers revealed sevoflurane (fluoromethyl-1,1,1,3,3,3,-hexafluroro-2-propyl ether) as a potent nonexplosive inhalational anesthetic agent. Sevoflurance, a pleasant-smelling liquid, boils at 58.5 degrees C at 760 torr and has a vapor pressure of 200 torr at 25 degrees C. It is nonflammable in air and has lower flammability limits of 11 vols percent in O2 and 10 vols percent in N2O. Sevoflurane exhibits limited chemical reactivity in vitro; it is subject to slight but measurable hydrolysis, and reacts with soda lime to form traces of related ethers. It provides rapid anesthetic induction and recovery consistent with its low distribution coefficients (blood:gas, 0.6; corn oil:gas, 41.6; olive oil:gas, 53.4). In dogs, anesthetic concentrations of sevoflurane did not produce spontaneous cardiac arrhythmias and did not sensitize the heart to epinephrine. Electroencephalographic patterns were similar to those observed during anesthesia with halothane. In rats, small increases in the urinary excretion of inorganic fluoride ion occurred during the first 24 hours after anesthesia. Subacute studies in dogs and rats, using closed-circle absorption with soda lime, revealed no toxicologically significant changes in animals anesthetized frequently for 2 weeks. Sevoflurane appears to be a unique volatile anesthetic agent worthy of further study.

  9. Stable inhibition of brain synaptic plasma membrane calcium ATPase in rats anesthetized with halothane.

    Science.gov (United States)

    Franks, J J; Horn, J L; Janicki, P K; Singh, G

    1995-01-01

    The authors recently showed that plasma membrane Ca(2+)-ATPase (PMCA) activity in cerebral synaptic plasma membrane (SPM) is diminished in a dose-related fashion during exposure in vitro to halothane, isoflurane, xenon, and nitrous oxide at clinically relevant partial pressures. They have now extended their work to in vivo studies, examining PMCA pumping in SPM obtained from control rats decapitated without anesthetic exposure, from rats decapitated during halothane anesthesia, and from rats decapitated after recovery from halothane anesthesia. Three treatment groups were studied: 1) C, control rats that were decapitated without anesthetic exposure, 2) A, anesthetized rats exposed to 1 minimum effective dose (MED) for 20 min and then decapitated, and 3) R, rats exposed to 1 MED for 20 min and then decapitated after recovery from anesthesia, defined as beginning to groom. Plasma membrane Ca(2+)-ATPase pumping and Ca(2+)-dependent ATPase hydrolytic activity, as well as sodium-calcium exchanger activity and Na+-K+-ATPase hydrolytic activity, were assessed in cerebral SPM. In addition, halothane effect on smooth endoplasmic reticulum Ca(2+)-ATPase (SERCA) was examined. Plasma membrane Ca(2+)-ATPase transport of Ca2+ into SPM vesicles from anesthetized rats was reduced to 71% of control (P SPM from rats killed while anesthetized