Sample records for benzocaine

  1. Antipyrine-Benzocaine Otic (United States)

    Antipyrine and benzocaine otic is used to relieve ear pain and swelling caused by middle ear infections. It may be used ... of ear wax in the ear. Antipyrine and benzocaine are in a class of medications called analgesics. ...

  2. Methemoglobinemia and benzocaine. (United States)

    Moos, Daniel D; Cuddeford, James D


    Benzocaine administration to facilitate upper endoscopic procedures can result in the relatively uncommon but potentially fatal complication known as methemoglobinemia. For this reason, the Veterans Health Administration (VA) announced on February 8, 2006, that they would stop using benzocaine-containing sprays for procedures involving the mouth and throat. Methemoglobinemia should be considered in any patient who demonstrates cyanosis, respiratory distress, headache, lightheadedness, and a dark, chocolate-colored blood after receiving pharyngeal anesthesia. Prompt recognition of this rare (but potentially fatal) condition is important. Once identified, treatment is generally rapid with methylene blue. The patient should be monitored in the intensive care setting for recurrence. Knowledge of this adverse medication reaction is essential for all gastroenterology nurses.

  3. Labelling of benzocaine with tritium

    Energy Technology Data Exchange (ETDEWEB)

    Malik, Sohail (Washington Univ., Seattle, WA (United States))


    A convenient method is described to label a local anesthetic, benzocaine, with tritium. The bromoester of para-aminobenzoic acid (PABA) was prepared from para-nitrotoluene and was reduced with tritium. The generation of isotopic hydrogen and labelling of benzocaine was achieved in one-step. A mixture of sodium borohydride (NaB[sup 3]H[sub 4]) with cobalt (II) chloride was used to generate tritium gas. 5% Pd/C was used as a catalyst. This constitutes the first report of tritium labelled benzocaine. (author).

  4. 76 FR 12916 - Benzocaine; Weight Control Drug Products for Over-the-Counter Human Use (United States)


    ... benzocaine be classified as nonmonograph at any concentration for use in OTC weight control drug products... daily) Group 4: Glucose hard candy containing benzocaine, caffeine, and vitamins (benzocaine...

  5. Death of an infant involving benzocaine. (United States)

    Logan, Barry K; Gordon, Ann Marie


    This report describes the death of a four-month-old Hispanic male which may be related to benzocaine toxicity. A toxicological evaluation revealed benzocaine at a concentration of 3.48 mg/L, and postmortem methemoglobin of 36% (normal 0.4-1.5). Methemoglobinemia is a complication of benzocaine toxicity. In light of the toxicology findings, the coroner investigated the source of the benzocaine and discovered that the child was treated with Zenith Goldline Allergen Ear Drops containing 0.25% w/v benzocaine and 5.4% w/v antipyrine. There was an admission by a caregiver that on the day prior to the child's death, he had been treated with three times the prescribed dose. Blood benzocaine concentrations in nine other unrelated cases were determined and concentrations ranged from benzocaine positive cases ranged from 6-69%; however, methemoglobin concentrations in postmortem cases are frequently elevated and should be interpreted with caution. The unknown significance of the benzocaine, and the circumstances of the case raise questions about the ultimate attribution of this death to SIDS.

  6. Atypical presentations of methemoglobinemia from benzocaine spray. (United States)

    Tantisattamo, Ekamol; Suwantarat, Nuntra; Vierra, Joseph R; Evans, Samuel J


    Widely used for local anesthesia, especially prior to endoscopic procedures, benzocaine spray is one of the most common causes of iatrogenic methemoglobinemia. The authors report an atypical case of methemoglobinemia in a woman presenting with pale skin and severe hypoxemia, after a delayed repeat exposure to benzocaine spray. Early recognition and prompt management of methemoglobinemia is needed in order to lessen morbidity and mortality from this entity.

  7. Benzocaine-induced methaemoglobinaemia: a case study. (United States)

    Bittmann, Stefan; Krüger, Carsten

    Benzocaine is a widely used topical anaesthetic and has been reported to cause toxic methaemoglobinaemia in otherwise healthy individuals with no predisposing risk factors. This article reports on a rare case of benzocaine-induced methaemoglobinaemia following adenotonsillectomy in a 5-year-old girl. Topical benzocaine was applied orally for the relief of postoperative wound pain on the eighth postoperative day. Two hours after application, generalized cyanosis, mild dyspnoea and some degree of agitation developed. The methaemoglobin level was 38.5%. Treatment with methylene blue was initiated immediately. Symptoms completely disappeared 4 hours after initiation of methylene blue therapy. The further course was uneventful. Therefore, all health professionals should be aware that topical anaesthetics after surgery can induce methaemoglobinaemia in children, even after a prolonged interval, and especially when applied on wound surfaces.

  8. Protomers of benzocaine: solvent and permittivity dependence. (United States)

    Warnke, Stephan; Seo, Jongcheol; Boschmans, Jasper; Sobott, Frank; Scrivens, James H; Bleiholder, Christian; Bowers, Michael T; Gewinner, Sandy; Schöllkopf, Wieland; Pagel, Kevin; von Helden, Gert


    The immediate environment of a molecule can have a profound influence on its properties. Benzocaine, the ethyl ester of para-aminobenzoic acid that finds an application as a local anesthetic, is found to adopt in its protonated form at least two populations of distinct structures in the gas phase, and their relative intensities strongly depend on the properties of the solvent used in the electrospray ionization process. Here, we combine IR-vibrational spectroscopy with ion mobility-mass spectrometry to yield gas-phase IR spectra of simultaneously m/z and drift-time-resolved species of benzocaine. The results allow for an unambiguous identification of two protomeric species: the N- and O-protonated forms. Density functional theory calculations link these structures to the most stable solution and gas-phase structures, respectively, with the electric properties of the surrounding medium being the main determinant for the preferred protonation site. The fact that the N-protonated form of benzocaine can be found in the gas phase is owed to kinetic trapping of the solution-phase structure during transfer into the experimental setup. These observations confirm earlier studies on similar molecules where N- and O-protonation have been suggested.

  9. Diffusion kinetics of the ion exchange of benzocaine on sulfocationites (United States)

    Al'tshuler, O. G.; Shkurenko, G. Yu.; Gorlov, A. A.; Al'tshuler, G. N.


    The theory of the ion exchange kinetics on strong acid cationites with the participation of weak electrolytes is discussed. The kinetics of desorption of benzocaine in the protonated and molecular forms from strong acid cationites, sulfonated polycalixarene, and KU-23 30/100 sulfocationite, is studied experimentally. It is shown that the flow of protonated benzocaine from cationite upon desorption proceeding by the ion-exchange mechanism is more intense than upon desorption of nonionized benzocaine molecules. It is established that the diffusion coefficient of benzocaine cations is (1.21 ± 0.23) × 10-12 m2/s in KU-23 30/100 sulfocation and (0.65 ± 0.06) × 10-13 m2/s in sulfonated polycalixarene, while the diffusion coefficient of benzocaine molecules is (0.65 ± 0.15) × 10-14 m2/s in sulfonated polycalixarene.

  10. Topical benzocaine-induced methemoglobinemia in the pediatric population. (United States)

    So, Tsz-Yin; Farrington, Elizabeth


    Topical benzocaine is an anesthetic agent that is often used before procedures and clinical tests, such as esophagoscopy, bronchoscopy, and endotracheal intubation. However, a potential deadly condition known as methemoglobinemia can occur with this agent. It causes the oxidation of hemoglobin to methemoglobinemia to occur more rapidly than the reduction of methemoglobin back to hemoglobin. Certain congenital and clinical conditions that affect oxygen delivery can increase the patient's risk of having methemoglobinemia develop with the use of benzocaine. Topical benzocaine-induced methemoglobinemia can occur in the pediatric population. Prompt management with intravenous methylene blue should be initiated for reversal.

  11. Allergic contact dermatitis from ethyl chloride and benzocaine. (United States)

    Carazo, Juan Luis Anguita; Morera, Blanca Sáenz de San Pedro; Colom, Luis Palacios; Gálvez Lozano, José Manuel


    Ethyl chloride (EC) or chloroethane (C2H5Cl) is a volatile halogenated hydrocarbon. Reports of contact sensitivity to this gas are infrequent considering its widespread use as a local anesthetic, and it may have a relatively low sensitization potential. Benzocaine is another local anesthetic derivative of the ethyl ester of para-aminobenzoic acid, previously reported as a causative agent of delayed hypersensitivity reactions. We present a patient who developed a generalized itching dermatitis after the application of a medical aerosol containing EC, as well as facial angioedema and tongue swelling after the local application of benzocaine. Patch-test results were positive for EC "as is" (++), benzocaine 5% in petrolatum (++), and caine mix (+++) at 96 hours (day 4). The possibility of cross-sensitization between both drugs would not have been chemically plausible. We report the first published clinical case of contact allergic dermatitis from two chemically unrelated local anesthetics (EC and benzocaine) in the same patient.

  12. Removal of benzocaine from water by filtration with activated carbon (United States)

    Howe, G.E.; Bills, T.D.; Marking, L.L.


    Benzocaine is a promising candidate for registration with the U.S. Food and Drug Administration for use as an anesthetic in fish culture, management, and research. A method for the removal of benzocaine from hatchery effluents could speed registration of this drug by eliminating requirements for data on its residues, tolerances, detoxification, and environmental hazards. Carbon filtration effectively removes many organic compounds from water. This study tested the effectiveness of three types of activated carbon for removing benzocaine from water by column filtration under controlled laboratory conditions. An adsorptive capacity was calculated for each type of activated carbon. Filtrasorb 400 (12 x 40 mesh; U.S. standard sieve series) showed the greatest capacity for benzocaine adsorption (76.12 mg benzocaine/g carbon); Filtrasorb 300 (8 x 30 mesh) ranked next (31.93 mg/g); and Filtrasorb 816 (8 x 16 mesh) absorbed the least (1.0 mg/g). Increased adsorptive capacity was associated with smaller carbon particle size; however, smaller particle size also impeded column flow. Carbon filtration is a practical means for removing benzocaine from treated water.

  13. Metabolism and elimination of benzocaine by rainbow-trout, Oncorhynchus mykiss (United States)

    Meinertz, J.R.; Gingerich, W.H.; Allen, J.L.


    1. Branchial and urinary elimination of benzocaine residues was evaluated in adult rainbow trout, oncorhynchus mykiss, given a single dorsal aortic dose of c-14-benzocaine hydrochloride.^2. Branchial elimination of benzocaine residues was rapid and accounted for 59.2% Of the dose during the first 3 h after dosing. Renal elimination of radioactivity was considerably slower; the kidney excreted 2.7% Dose within 3 h and 9.0% Within 24 h. Gallbladder bile contained 2.0% Dose 24 h after injection.^3. Of the radioactivity in radiochromatograms from water taken 3 min after injection, 87.3% Was benzocaine and 12.7% Was n-acetylated benzocaine. After 60 min, 32.7% Was benzocaine and 67.3% Was n-acetylated benzocaine.^4. Of the radioactivity in radiochromatograms from urine taken 1 h after dosing, 7.6% Was para-aminobenzoic acid, 59.7% Was n-acetylated para-aminobenzoic acid, 19.5% Was benzocaine, and 8.0% Was n-acetylated benzocaine. The proportion of the radioactivity in urine changed with time so that by 20 h, 1.0% Was para-aminobenzoic acid and 96.6% Was n-acetylated para-aminobenzoic acid.^5. Benzocaine and a more hydrophobic metabolite, n-acetylated benzocaine, were eliminated primarily through the gills; renal and biliary pathways were less significant elimination routes for benzocaine residues.

  14. Determination of benzocaine in rainbow trout plasma (United States)

    Bernardy, Jeffery A.; Coleman, K.S.; Stehly, G.R.; Gingerich, William H.


    A liquid chromatographic method is described for analysis of benzocaine (BZ), a proposed fish anesthetic, in rainbow trout plasma, Mean recoveries of BZ from plasma samples fortified at 44-10 100 ng/mL were 96-100%. The method detection limit is 10 ng/mL, and the limit of quantitation is 37 ng/mL. Acetylation of BZ occurs in whole blood after storage at room temperature (i.e., 21 degrees C) for 10 min. However, no acetylation of BZ was detected in plasma samples held at room temperature for 4 h, Mean method precision for plasma samples with incurred BZ residue is similar to that for fortified samples in the same concentration range (relative standard deviations of 0.9 and 1.2%, respectively).

  15. Stability of benzocaine formulated in commercial oral disintegrating tablet platforms. (United States)

    Köllmer, Melanie; Popescu, Carmen; Manda, Prashanth; Zhou, Leon; Gemeinhart, Richard A


    Pharmaceutical excipients contain reactive groups and impurities due to manufacturing processes that can cause decomposition of active drug compounds. The aim of this investigation was to determine if commercially available oral disintegrating tablet (ODT) platforms induce active pharmaceutical ingredient (API) degradation. Benzocaine was selected as the model API due to known degradation through ester and primary amino groups. Benzocaine was either compressed at a constant pressure, 20 kN, or at pressure necessary to produce a set hardness, i.e., where a series of tablets were produced at different compression forces until an average hardness of approximately 100 N was achieved. Tablets were then stored for 6 months under International Conference on Harmonization recommended conditions, 25°C and 60% relative humidity (RH), or under accelerated conditions, 40°C and 75% RH. Benzocaine degradation was monitored by liquid chromatography-mass spectrometry. Regardless of the ODT platform, no degradation of benzocaine was observed in tablets that were kept for 6 months at 25°C and 60% RH. After storage for 30 days under accelerated conditions, benzocaine degradation was observed in a single platform. Qualitative differences in ODT platform behavior were observed in physical appearance of the tablets after storage under different temperature and humidity conditions.

  16. Nosocomial Methemoglobinemia Resulting from Self-Administration of Benzocaine Spray

    Directory of Open Access Journals (Sweden)

    Christopher Hoffman


    Full Text Available Methemoglobinemia is life-threatening and bears pathognomonic signs difficult to diagnose in real time. Local anesthetics are widely used and are known for eliciting this condition. We report a case of methemoglobinemia secondary to self-administered use of benzocaine spray. A 27-year-old woman was found to be in respiratory distress during postoperative recovery. After desaturation persisted, arterial blood gas yielded a methemoglobin level of 47%. The patient was successfully treated with intravenous methylene blue. Review of the events revealed self-administered doses of benzocaine spray to alleviate discomfort from a nasogastric tube. We review this case in detail in addition to discussing methemoglobinemia and its relevant biochemistry, pathophysiology, clinical presentation, and medical management. Given the recognized risk of methemoglobinemia associated with benzocaine use, we recommend its removal from the market in favor of safer alternatives.

  17. Benzocaine-induced methemoglobinemia in an acute-exposure rat model. (United States)

    Von Tungeln, Linda S; Zhou, Tong; Woodling, Kellie A; Doerge, Daniel R; Greenlees, Kevin J; Beland, Frederick A


    Tricaine methanesulfonate, a sedative for temporarily immobilizing fish, has a 21-day withdrawal time. Benzocaine has been proposed as an alternative sedative because a withdrawal period may not be required. Since benzocaine is known to induce methemoglobinemia, the potential for orally administered benzocaine to induce methemoglobin was assessed in rats. Sprague-Dawley rats were given a single gavage administration of 64mg benzocaine hydrochloride per kg bw and then euthanized at intervals up to 120min. Plasma levels of benzocaine were relatively low at all times, whereas methemoglobin peaked at 24min. Additional rats were orally gavaged with 0-1024mg benzocaine hydrochloride per kg bw and euthanized after 24min. Plasma levels of benzocaine increased from 0.01μM at 2mg per kg bw to 2.9μM at 1024mg per kg bw. Methemoglobin levels did not differ from controls at doses up to 32mg per kg bw in females and 64mg per kg bw in males, whereupon the value increased to ∼80% at 1024mg per kg bw. These data were used to estimate the potential impact of benzocaine residues in fish and suggest that the consumption of fish treated with benzocaine hydrochloride will not cause methemoglobinemia in humans.

  18. Multivariate Stable Isotope Analysis to Determine Linkages between Benzocaine Seizures (United States)

    Kemp, H. F.; Meier-Augenstein, W.; Collins, M.; Salouros, H.; Cunningham, A.; Harrison, M.


    In July 2010, a woman was jailed for nine years in the UK after the prosecution successfully argued that attempting to import a cutting agent was proof of involvement in a conspiracy to supply Cocaine. That landmark ruling provided law enforcement agencies with much greater scope to tackle those involved in this aspect of the drug trade, specifically targeting those importing the likes of benzocaine or lidocaine. Huge quantities of these compounds are imported into the UK and between May and August 2010, four shipments of Benzocaine amounting to more then 4 tons had been seized as part of Operation Kitley, a joint initiative between the UK Border Agency and the Serious Organised Crime Agency (SOCA). By diluting cocaine, traffickers can make it go a lot further for very little cost, leading to huge profits. In recent years, dealers have moved away from inert substances, like sugar and baby milk powder, in favour of active pharmaceutical ingredients (APIs), including anaesthetics like Benzocaine and Lidocaine. Both these mimic the numbing effect of cocaine, and resemble it closely in colour, texture and some chemical behaviours, making it easier to conceal the fact that the drug has been diluted. API cutting agents have helped traffickers to maintain steady supplies in the face of successful interdiction and even expand the market in the UK, particularly to young people aged from their mid teens to early twenties. From importation to street-level, the purity of the drug can be reduced up to a factor of 80 and street level cocaine can have a cocaine content as low as 1%. In view of the increasing use of Benzocaine as cutting agent for Cocaine, a study was carried out to investigate if 2H, 13C, 15N and 18O stable isotope signatures could be used in conjunction with multivariate chemometric data analysis to determine potential linkage between benzocaine exhibits seized from different locations or individuals to assist with investigation and prosecution of drug

  19. Efficacy of benzocaine as an anesthetic for salmonid fishes (United States)

    Gilderhus, P.A.


    Benzocaine was tested in the laboratory to determine the effective concentrations for anesthetizing juvenile chinook salmon Oncorhynchus tshawytscha an rainbow trout O. mykiss (formerly Salmo gairdneri ). Tests were conducted at three water temperatures, in waters ranging from very soft to very hard, and with groups of rainbow trout from 5 to 47 cm long and chinook salmon 20 cm long. Effective concentrations were defined as those that rendered the fish fully handleable in 3 min or less, allowed recovery of most fish within 10 min, and caused no mortality after 15-min exposures. Concentrations of 25-45 mg/L anesthetized both species over the entire range of conditions tested. Although efficacy was essentially unrelated to species or water quality, it was related to water temperature and size of fish; the concentrations of benzocaine required were highest at the lowest water temperature and for the largest fish.

  20. A Quick and Easy Simplification of Benzocaine's NMR Spectrum (United States)

    Carpenter, Suzanne R.; Wallace, Richard H.


    The preparation of benzocaine is a common experiment used in sophomore-level organic chemistry. Its straightforward procedure and predictable good yields make it ideal for the beginning organic student. Analysis of the product via NMR spectroscopy, however, can be confusing to the novice interpreter. An inexpensive, quick, and effective method for simplifying the NMR spectrum is reported. The method results in a spectrum that is cleanly integrated and more easily interpreted.

  1. Efficacy of a benzocaine lozenge in the treatment of uncomplicated sore throat. (United States)

    Chrubasik, Sigrun; Beime, Beate; Magora, Florella


    Benzocaine lozenges are popular in symptomatic treatment of acute sore throat. The aim of this study was to evaluate if sucking a benzocaine lozenge was superior to a placebo lozenge in patients with pain while swallowing. Volunteers with acute, uncomplicated sore throat received randomly and double-blind either a benzocaine 8 mg or a placebo lozenge. Pain was assessed on a numerical visual rating scale. The primary outcome measure was the sum of the pain intensity differences (SPID) over 2 h. Secondary outcome measures included the number of patients who reported 50% or more of their baseline pain score (responders) and those with worthwhile and complete pain relief, the times to worthwhile/complete pain relief and to pain recurrence and the occurrence of any adverse effects. A predefined interim analysis after including 50 patients revealed the superiority of benzocaine versus placebo in the SPID (p = 0.0086). At this time, a total of 165 patients had been recruited (full analysis set, FAS) and underwent statistical analysis. In the FAS, median SPID had significantly more decreased in patients receiving benzocaine compared to placebo (-12 vs. - 5, p = 0.001). There were significantly more responders and patients with worthwhile pain relief in group benzocaine. The number of patients with complete pain relief was very small. Median time to worthwhile pain relief was 20 min (benzocaine) and >45 min (placebo). Adverse events were not observed. Benzocaine lozenges are superior to placebo lozenges and a useful, well-tolerated treatment option to reduce painful pharyngeal discomfort.

  2. Thermodynamic study of benzocaine insertion into different lipid bilayers (United States)

    Cascales, J. J. López; Costa, S. D. Oliveira; Porasso, R. D.


    Despite the general consensus concerning the role played by sodium channels in the molecular mechanism of local anesthetics, the potency of anaesthetic drugs also seems to be related with their solubility in lipid bilayers. In this respect, this work represents a thermodynamic study of benzocaine insertion into lipid bilayers of different compositions by means of molecular dynamics simulation. Thus, the free energy profiles associated with benzocaine insertion into symmetric lipid bilayers composed of different proportions of dipalmitoylphosphatidylcholine and dipalmitoylphosphatidylserine were studied. From the simulation results, a maximum in the free energy (ΔG) profile was measured in the region of the lipid/solution interface. This free energy barrier appears to be very much dependent on the lipid composition of the membrane. On the other hand, the minimum free energy (ΔG) within the bilayer remained almost independent of the lipid composition of the bilayer. By repeating the study at different temperatures, it was seen how the spontaneity of benzocaine insertion into the lipid bilayer is due to an increase in the entropy associated with the process.

  3. Effects of the local anesthetic benzocaine on the human erythrocyte membrane and molecular models. (United States)

    Suwalsky, Mario; Schneider, Carlos; Villena, Fernando; Norris, Beryl; Cárdenas, Hernán; Cuevas, Francisco; Sotomayor, Carlos P


    The interaction of the local anesthetic benzocaine with the human erythrocyte membrane and molecular models is described. The latter consisted of isolated unsealed human erythrocyte membranes (IUM), large unilamellar vesicles (LUV) of dimyristoylphospatidylcholine (DMPC), and phospholipid multilayers of DMPC and dimyristoylphospatidyletanolamine (DMPE), representatives of phospholipid classes located in the outer and inner monolayers of the human erythrocyte membrane, respectively. Optical and scanning electron microscopy of human erythrocytes revealed that benzocaine induced the formation of echinocytes. Experiments performed on IUM and DMPC LUV by fluorescence spectroscopy showed that benzocaine interacted with the phospholipid bilayer polar groups and hydrophobic acyl chains. X-ray diffraction analysis of DMPC confirmed these results and showed that benzocaine had no effects on DMPE. The effect on sodium transport was also studied using the isolated toad skin. Electrophysiological measurements indicated a significant decrease in the potential difference (PD) and in the short-circuit current (Isc) after the application of benzocaine, reflecting inhibition of active ion transport.

  4. The in vitro and in vivo genotoxicity of benzocaine: a brief communication. (United States)

    Brock, William J; Bell, Thomas A


    Benzocaine has a long history of use in human medicine. However, benzocaine also has been used in aquaculture with finfish for more than 40 years for sedating fish for marking, transport, surgery, and so on, although benzocaine does not have a current Food and Drug Administration (FDA) approval for this application in the United States. As part of a FDA approval for use as an animal drug, the genotoxicity of benzocaine was evaluated in the in vitro bacterial reverse mutation assay and the forward mutation assay and in vivo in the mouse micronucleus assay. These studies were conducted in compliance with Good Laboratory Practice regulations and according to Veterinary International Conference on Harmonisation guidelines. Based on the results of these studies, benzocaine was determined not to be genotoxic.

  5. Inclusion complex of benzocaine and β-cyclodextrin: 1H NMR and isothermal titration calorimetry studies (United States)

    Mic, Mihaela; Pırnǎu, Adrian; Bogdan, Mircea; Turcu, Ioan


    The supramolecular structure of the inclusion complex of β-cyclodextrin with benzocaine in aqueous solution has been investigated by 1H NMR spectroscopy and isothermal titration nanocalorimetry (ITC). Analysis of 1H NMR data by continuous variation method indicates that the benzocaine: β-cyclodextrin inclusion complex occurs and has a 1:1 stoichiometry. Rotating frame NOE spectroscopy (ROESY) was used to ascertain the solution geometry of the host-guest complex which indicates that the benzocaine molecule was included with the aromatic ring into the cyclodextrin cavity. Although the affinity of benzocaine for cyclodextrin is relatively high, the association constant cannot be measured using ITC due to the low solubility of benzocaine in water.

  6. Prospective randomized study of viscous lidocaine versus benzocaine in a GI cocktail for dyspepsia. (United States)

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


    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.

  7. Evaluation and management of acquired methemoglobinemia associated with topical benzocaine use. (United States)

    Taleb, Mohammed; Ashraf, Zubair; Valavoor, Shahul; Tinkel, Jodi


    Benzocaine is a widely used topical oropharyngeal anesthetic and has been reported to cause methemoglobinemia. We discuss benzocaine-induced methemoglobinemia and review the causes, presentation, and management of this serious complication. Treatment with methylene blue will result in reversal of methemoglobinemia and clinical recovery in most cases but needs to be used at appropriate doses in carefully selected individuals. Physicians who perform procedures involving the application of benzocaine for topical anesthesia need to rapidly identify and treat methemoglobinemia to avoid significant associated morbidity and mortality.

  8. Methemoglobinemia with the use of benzocaine spray for awake fiberoptic intubation. (United States)

    Abdel-Aziz, Samer; Hashmi, Nazish; Khan, Sabina; Ismaeil, Mohamed


    We report a case in which the use of benzocaine spray to facilitate awake fiber optic intubation (FOI) in a patient with a difficult airway caused methemoglobinemia intraoperatively. Local benzocaine was sprayed to numb the patient's airway for a total time of one second, fifteen minutes later SpO2 decreased to 85% on the pulse oximeter. Arterial blood gas (ABG) showed a MetHb of 24.6% of total Hemoglobin. The patient was successfully treated with methylene blue intravenously and recovered uneventfully. Small amounts of local benzocaine sprayed to numb the airway can cause significant methemoglobinemia that requires immediate recognition and appropriate management.

  9. In vitro skin absorption and metabolism of benzoic acid, p-aminobenzoic acid, and benzocaine in the hairless guinea pig. (United States)

    Nathan, D; Sakr, A; Lichtin, J L; Bronaugh, R L


    The percutaneous absorption and metabolism of three structurally related compounds, benzoic acid, p-aminobenzoic acid (PABA), and ethyl aminobenzoate (benzocaine), were determined in vitro through hairless guinea pig skin. Benzocaine was also studied in human skin. Absorption of benzocaine was rapid and similar through both viable and nonviable skin. The absorption of the two acidic compounds, benzoic acid and PABA, was greater through nonviable skin. A small portion (6.9%) of absorbed benzoic acid was conjugated with glycine to form hippuric acid. Although N-acetyl-benzocaine had not been observed as a metabolite of benzocaine when studied by other routes of administration, both PABA and benzocaine were extensively N-acetylated during percutaneous absorption. Thus, the metabolism of these compounds should be considered in an accurate assessment of absorption after topical application.

  10. Unraveling the benzocaine-receptor interaction at molecular level using mass-resolved spectroscopy. (United States)

    Aguado, Edurne; León, Iker; Millán, Judith; Cocinero, Emilio J; Jaeqx, Sander; Rijs, Anouk M; Lesarri, Alberto; Fernández, José A


    The benzocaine-toluene cluster has been used as a model system to mimic the interaction between the local anesthetic benzocaine and the phenylalanine residue in Na(+) channels. The cluster was generated in a supersonic expansion of benzocaine and toluene in helium. Using a combination of mass-resolved laser-based experimental techniques and computational methods, the complex was fully characterized, finding four conformational isomers in which the molecules are bound through N-H···π and π···π weak hydrogen bonds. The structures of the detected isomers closely resemble those predicted for benzocaine in the inner pore of the ion channels, giving experimental support to previously reported molecular chemistry models.

  11. Benzocaine-induced methaemoglobinaemia: a life-threatening complication after a transoesophageal echocardiogram (TEE). (United States)

    Aryal, Madan Raj; Gupta, Shobhit; Giri, Smith; Fraga, Julian Diaz


    Acquired methaemoglobinaemia is a potentially fatal impairment in oxygen delivery if not recognised early and treated appropriately. Benzocaine used as an anaesthetic for endoscopic procedures is an uncommon but clinically important precipitant of acquired methaemoglobinaemia. We present a case of an elderly woman who developed perioral cyanosis and desaturation 20 min after a transoesophageal echocardiogram. Further evaluation led to the diagnosis of benzocaine-induced methaemoglobinaemia and timely treatment with intravenous methylene blue was initiated.

  12. Prevalence of benzocaine and lidocaine patch test sensitivity in Denmark: temporal trends and relevance

    DEFF Research Database (Denmark)

    Thyssen, Jacob P; Engkilde, Kåre; Menné, Torkil;


    BACKGROUND. Allergens included in the European baseline series should result in positive patch test reactions in at least 1% of a patch test population. Inclusion of local anaesthetics other than benzocaine in the baseline series has previously been debated.......BACKGROUND. Allergens included in the European baseline series should result in positive patch test reactions in at least 1% of a patch test population. Inclusion of local anaesthetics other than benzocaine in the baseline series has previously been debated....

  13. Simple spectrophotometric methods for the simultaneous determination of antipyrine and benzocaine

    Directory of Open Access Journals (Sweden)

    Hanan A. Merey


    Full Text Available Antipyrine and benzocaine are formulated together for the treatment of ear inflammation and to relieve pain. Four spectrophotometric methods were developed for the simultaneous determination of antipyrine (AN and benzocaine (BE in their combined dosage form. Method A depends on applying dual wavelength method where antipyrine was determined by measuring the absorbance at 254.1 and 309.1 nm (corresponding to zero difference of benzocaine, while the absorbance difference at 230.1 and 263.5 nm (corresponding to zero difference of antipyrine was selected for benzocaine determination in the laboratory prepared spectrum. Method B depends on measuring the peak amplitude of first derivative at 305 nm for calculating benzocaine concentration then the total concentration of both drugs was determined using isoabsorptive point at 257.4 nm (antipyrine concentration was then calculated by subtraction. Method C is based on measuring the peak difference of the ratio spectra at Δp (239.1–285 nm and Δp (301.4–250 nm for the determination of antipyrine and benzocaine, respectively. Method D depends on measuring peak to peak amplitude of the first derivative of ratio spectra at (234.5 + 244.2 nm and peak amplitude at 295.5 nm for the determination of antipyrine and benzocaine, respectively. The proposed methods were validated and applied for the analysis of antipyrine and benzocaine in their laboratory prepared mixtures and pharmaceutical formulation. Statistical comparison between the results of the proposed methods and those of the reported methods showed no significant difference.

  14. Residues of benzocaine in rainbow trout, largemouth bass, and fish meal (United States)

    Allen, J.L.


    Residues of the anesthetic benzocaine in muscle tissue of rainbow trout (Salmo gairdneri ) and largemouth bass (Micropterus salmoides ) were determined after exposure of the fish to 50 mg benzocaine/L for 15 min and withdrawal times of 0-24 h. The mean concentration of benzocaine residues in fish sampled immediately after exposure was 14.0 mu g/g in rainbow trout and 10.6 mu g/g in largemouth bass. Residues were below the control value after 8 h of withdrawal in largemouth bass and near the control value after 4 h of withdrawal in rainbow trout. Although residues of benzocaine were high in fish immediately after exposure, the concentration declined rapidly when the fish were held in flowing fresh water. Fish meal prepared from Pacific salmon (Oncorhynchus sp.) that had been anesthetized with benzocaine or tricaine (MS-222) contained residues of 45.1 mu g benzocaine/g or 47.7 mu g tricaine/g.

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


    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).

  16. Benzocaine and lidocaine induced methemoglobinemia after bronchoscopy: a case report

    Directory of Open Access Journals (Sweden)

    Kwok Sophie


    Full Text Available Abstract Introduction Methemoglobinemia is a rare cause of hypoxemia, characterized by abnormal levels of oxidized hemoglobin that cannot bind to and transport oxygen. Case presentation A 62-year-old male underwent bronchoscopy where lidocaine oral solution and Hurricaine spray (20% benzocaine were used. He developed central cyanosis and his oxygen saturation was 85% via pulse oximetry. An arterial blood gas revealed pH 7.45, PCO2 42, PO2 282, oxygen saturation 85%. Co-oximetry performed revealed a methemoglobin level of 17.5% (normal 0.6–2.5%. The patient was continued on 15 L/minute nonrebreathing face mask and subsequent oxygen saturation improved to 92% within two hours. With hemodynamic stability and improved SpO2, treatment with methylene blue was withheld. Conclusion Methemoglobinemia is a potentially lethal condition after exposure to routinely used drugs. Physicians should be aware of this complication for early diagnosis and treatment.

  17. Drug action of benzocaine on the sarcoplasmic reticulum Ca-ATPase from fast-twitch skeletal muscle. (United States)

    Di Croce, D; Trinks, P W; Grifo, M B; Takara, D; Sánchez, G A


    The effect of the local anesthetic benzocaine on sarcoplasmic reticulum membranes isolated from fast-twitch muscles was tested. The effects on Ca-ATPase activity, calcium binding and uptake, phosphoenzyme accumulation and decomposition were assessed using radioisotopic methods. The calcium binding to the Ca-ATPase was noncompetitively inhibited, and the enzymatic activity decreased in a concentration-dependent manner (IC50 47.1 mM). The inhibition of the activity depended on the presence of the calcium ionophore calcimycin and the membrane protein concentration. The pre-exposure of the membranes to benzocaine enhanced the enzymatic activity in the absence of calcimycin, supporting the benzocaine permeabilizing effect, which was prevented by calcium. Benzocaine also interfered with the calcium transport capability by decreasing the maximal uptake (IC50 40.3 mM) without modification of the calcium affinity for the ATPase. It inhibited the phosphorylation of the enzyme, and at high benzocaine concentration, the dephosphorylation step became rate-limiting as suggested by the biphasic profile of phosphoenzyme accumulation at different benzocaine concentrations. The data reported in this paper revealed a complex pattern of inhibition involving two sites for interaction with low and high benzocaine concentrations. It is concluded that benzocaine not only exerts an indirect action on the membrane permeability to calcium but also affects key steps of the Ca-ATPase enzymatic cycle.

  18. Microemulsion for simultaneous transdermal delivery of benzocaine and indomethacin: in vitro and in vivo evaluation. (United States)

    El Maghraby, Gamal M; Arafa, Mona F; Osman, Mohamed A


    This study investigated simultaneous transdermal delivery of indomethacin and benzocaine from microemulsion. Eucalyptus oil based microemulsion was used with Tween 80 and ethanol being employed as surfactant and cosurfactant, respectively. A microemulsion formulation comprising eucalyptus oil, polyoxyethylene sorbitan momooleate (Tween 80), ethanol and water (20:30:30:20) was selected. Indomethacin (1% w/w) and benzocaine (20% w/w) were incorporated separately or combined into this formulation before in vitro and in vivo evaluation. Application of indomethacin microemulsion enhanced the transdermal flux and reduced the lag time compared to saturated aqueous control. The same trend was evident for benzocaine microemulsion. Simultaneous application of the two drugs in microemulsion provided similar enhancement pattern. The in vivo evaluation employed the pinprick method and revealed rapid anesthesia after application of benzocaine microemulsion with the onset being 10 min and the action lasting for 50 min. For indomethacin microemulsion, the analgesic effect was recorded after 34.5 min and lasted for 70.5 min. Simultaneous application of benzocaine and indomethacin provided synergistic effect. The onset of action was achieved after 10 min and lasted for 95 min. The study highlighted the potential of microemulsion formulation in simultaneous transdermal delivery of two drugs.

  19. Study of the benzocaine transfer from aqueous solution to the interior of a biological membrane. (United States)

    Porasso, Rodolfo D; Bennett, W F Drew; Oliveira-Costa, S D; López Cascales, J J


    The precise molecular mechanism of general anesthetics remains unknown. It is therefore important to understand where molecules with anesthetic properties localize within biological membranes. We have determined the free energy profile of a benzocaine molecule (BZC) across a biological membrane using molecular dynamics simulation. We use an asymmetric phospholipid bilayer with DPPS in one leaflet of a DPPC bilayer (Lopez Cascales et al. J. Phys. Chem. B 2006, 110, 2358-2363) to model a biological bilayer. From the free energy profile, we predict the zone of actuation of a benzocaine is located in the hydrocarbon region or at the end of the lipid head, depending of the presence of charged lipids (DPPS) in the leaflet. We observe a moderate increase in the disorder of the membrane and in particular an increase in the disorder of DPPS. Static and dynamic physicochemical properties of the benzocaine, such as its dipole orientation, translational diffusion coefficient, and rotational relaxation time were measured.

  20. Benzocaine as a fish anesthetic: efficacy and safety for spawning-phase salmon (United States)

    Gilderhus, P.A.


    The anesthetic benzocaine was tested for efficacy and safety for spawning-phase chinook salmon (Oncorhynchus tshawytscha) and Atlantic salmon (Salmo salar) at federal fish hatcheries. Tests were conducted in the existing hatchery water supplies (soft water; temperatures, 10–13 °C. Crystalline benzocaine was dissolved in ethanol (1 g/30 mL), and aliquots of that stock solution were added to the water in test tanks. Benzocaine concentrations of 25–30 mg/L anesthetized most fish in less than 3.5 min, and most fish recovered in less than 10 min after 15 min of exposure. Safety margins were narrow; both species tolerated 30 mg/L for about 20 min, but 25 min of exposure caused deaths. For 15 min exposures, concentrations of 35 mg/L for chinook salmon and 40 mg/L for Atlantic salmon were lethal.

  1. Benzocaine-induced methemoglobinemia in two patients: interdisciplinary collaboration, management, and near misses. (United States)

    Throm, Melinda J; Stevens, Margie Dale; Hansen, Carol


    Methemoglobin, a form of hemoglobin that does not bind oxygen, is produced when iron in red blood cells is oxidized from the ferrous state to the ferric state. Methemoglobinemia develops in the presence of oxidizing agents, such as benzocaine-containing topical anesthetic sprays, and it is characterized by cyanosis. If untreated, methemoglobinemia may prove lethal. We describe two patients who developed methemoglobinemia after they were administered benzocaine-containing topical anesthetic sprays. Using the Naranjo adverse drug reaction probability scale, the relationship between the administration of the benzocaine-containing spray and the development of methemoglobinemia was probable (score of 7) in both patients. Collaboration among health care providers is necessary to efficiently recognize, treat, and manage this condition.

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


    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.

  3. Randomized controlled trial of benzocaine versus placebo spray for pain relief at hysterosalpingogram. (United States)

    Bachman, E A; Senapati, S; Sammel, M D; Kalra, S K


    Many women experience pain during hysterosalpingogram (HSG). This prospective, randomized, double-blinded, placebo-controlled study assessed whether the use of benzocaine spray during HSG is associated with reduced pain as compared with placebo. Thirty women presenting for HSG were enrolled and randomized to either benzocaine or saline spray. Treatment groups were similar in age, race, parity, pre-procedure oral analgesic use and history of dysmenorrhoea and/or chronic pelvic pain. Median change in pain score from baseline to procedure was 50.6mm (-7.4 to 98.8mm) in the benzocaine group and 70.4mm (19.8 to 100mm) in the placebo group. There was no difference between groups after adjusting for history of dysmenorrhoea. There was no difference in resolution of pain in benzocaine versus placebo groups at 5 min post procedure--median pain score difference -11.1 (-90.1 to 18.5) versus -37.0 (-100 to 1.2)--or at 30 min post procedure. Satisfaction scores did not differ by treatment and did not correlate with pain score during the procedure (rho=0.005). The use of benzocaine spray does not significantly improve pain relief during HSG nor does it hasten resolution of pain post HSG. Of interest, patient satisfaction was not correlated with pain. Many women experience pain during hysterosalpingogram (HSG), which is a test used to evaluate the uterine cavity and fallopian tube. We conducted a prospective, randomized, double-blinded, placebo-controlled study to assess whether the use of benzocaine spray during HSG is associated with reduced pain as compared with placebo. Thirty women presenting for HSG were enrolled and randomized to either benzocaine or saline spray. Treatment groups were similar in age, race, previous pregnancies, pre-procedure oral analgesic use and history of dysmenorrhoea (painful periods) and/or chronic pelvic pain. There was no difference in pain scores or resolution of pain between the two groups. Satisfaction scores did not differ by treatment group

  4. Synthesis and characterization of covalently bound benzocaine graphite oxide derivative (United States)

    Kabbani, Ahmad; Kabbani, Mohamad; Safadi, Khadija


    Graphite oxide (GO) derived materials include chemically functionalize or reduced graphene oxide (exfoliated from GO) sheets, assembled paper-like forms , and graphene-based composites GO consists of intact graphitic regions interspersed with sp3-hybridized carbons containing hydroxyl and epoxide functional groups on the top and bottom surfaces of each sheet and sp2-hybridized carbons containing carboxyl and carbonyl groups mostly at the sheet edges. Hence, GO is hydrophilic and readily disperses in water to form stable colloidal suspensions Due to the attached oxygen functional groups, GO was used to prepare different derivatives which result in some physical and chemical properties that are dramatically different from their bulk counterparts .The present work discusses the covalent cross linking of graphite oxide to benzocaine or ethyl ester of para-aminobenzoic acid,structure I,used in many over-the-counter ointment drug.Synthesis is done via diazotization of the amino group.The product is characterized via IR,Raman, X-ray photoelectron spectroscopy as well as electron microscopy.

  5. Liquid chromatographic determination of benzocaine and N-acetylbenzocaine in the edible fillet tissue from rainbow trout (United States)

    Meinertz, J.R.; Stehly, G.R.; Hubert, T.D.; Bernardy, J.A.


    A method was developed for determining benzocaine and N-acetylbenzocaine concentrations in fillet tissue of rainbow trout. The method involves extracting the analytes with acetonitrile, removing lipids or hydrophobic compounds from the extract with hexane, and providing additional clean-up with solid-phase extraction techniques. Analyte concentrations are determined using reversed-phase high-performance liquid chromatographic techniques with an isocratic mobile phase and UV detection. The accuracy (range, 92 to 121%), precision (R.S.D., benzocaine residues from fish exposed to benzocaine. Copyright (C) 1999.

  6. Benzocaine loaded biodegradable poly-(D,L-lactide-co-glycolide) nanocapsules: factorial design and characterization

    Energy Technology Data Exchange (ETDEWEB)

    Morales Moraes, Carolina; Prado de Matos, Angelica; Paula, Eneida de [Department of Biochemistry, Institute of Biology, State University of Campinas, Campinas, SP (Brazil); Rosa, Andre Henrique [Department of Environmental Engineering, State University of Sao Paulo, Sorocaba, Sao Paulo (Brazil); Fernandes Fraceto, Leonardo, E-mail: leonardo@sorocaba.unesp.b [Department of Biochemistry, Institute of Biology, State University of Campinas, Campinas, SP (Brazil); Department of Environmental Engineering, State University of Sao Paulo, Sorocaba, Sao Paulo (Brazil)


    Local anesthetics are able to induce pain relief since they bind to the sodium channel of excitable membranes, blocking the influx of sodium ions and the propagation of the nervous impulse. Benzocaine (BZC) is a local anesthetic that presents limited application in topical formulations due to its low water-solubility. This study aimed to develop polymeric nanocapsules as a drug delivery system for the local anesthetic benzocaine (BZC). To do so, BZC loaded poly(D,L-lactide-co-glycolide) (PLGA) nanocapsules were prepared using the nanoprecipitation method and were characterized. The factorial experimental design was used to study the influence of four different independent variables on response to nanocapsules drug loading. The physical characteristics of PLGA nanocapsules were evaluated by analyzing the particle size, the polydispersion index and the zeta potential, using a particle size analyzer. The results of the optimized formulation showed a size distribution with a polydispersity index of 0.12, an average diameter of 123 nm, zeta potential of -33.6 mV and a drug loading of more than 69%. The release profiles showed a significant difference in the release behavior for the pure drug in solution when compared with that containing benzocaine loaded PLGA nanocapsules. Thus, the prepared nanocapsules described here may be of clinical importance in both the processes of stabilization and delivery of benzocaine for pain treatment.

  7. Presumptive benzocaine-induced methemoglobinemia in a slender-tailed meerkat (Suricata suricatta). (United States)

    Gyimesi, Zoltan S; Burns, Roy B


    An 8-yr-old castrated male slender-tailed meerkat (Suricata suricatta) was anesthetized for physical examination and dental prophylaxis. To facilitate intubation, two short bursts of benzocaine spray were applied topically to the glottis. Shortly thereafter, the meerkat developed a muddy, blue-gray mucous membrane color and low oxygen saturation readings measured via pulse oximetry. Despite positive pressure ventilation and treatment with doxapram, the cyanosis and hypoxemia did not improve. Blood collected during the procedure was noticeably dark brown and a clinical diagnosis of methemoglobinemia was made. Because of persistent cyanosis and prolonged recovery, the meerkat was anesthetized a second time to facilitate treatment for methemoglobinemia via a slow intravenous bolus of methylene blue and subcutaneously administered dextrose. Within 20 min, the tongue and gingival color normalized. This is the first report of methemoglobinemia in this species. Although it is commonly used in small animal practice and in humans undergoing certain endoscopic procedures, and present in numerous over-the-counter preparations, the risk of topical benzocaine inducing methemoglobinemia is well described. Administration of topical benzocaine in all mammalian species, particularly small patients, should be done with caution. If it is utilized in zoo practice, clinicians are encouraged to administer benzocaine judiciously to avoid accidental overdose, and be familiar with the signs of methemoglobinemia and its treatment.

  8. Benzocaine and clove oil as anesthetics for pejerrey (Odontesthes bonariensis fingerlings

    Directory of Open Access Journals (Sweden)

    J. Morato-Fernandes


    Full Text Available Pejerrey (Odontesthes bonariensis is a native species from Rio Grande do Sul, Uruguay and Argentina where it is of great economic importance for artisanal fishing. One difficulty in laboratory research with pejerrey is related to its sensitivity, as it presents higher basal cortisol levels than other freshwater species. For this reason, the aim of this work was to evaluate the efficiency of benzocaine and clove oil as anesthetics for pejerrey fingerlings. Two experiments were done where fingerlings (57±7.8mm and 1.1±0.44g were exposed to benzocaine with concentrations between 40mgL-1 and 120mgL-1 and to clove oil with concentrations between 12mgL-1 and 75mgL-1. Survival, anesthesia induction time and recovery time for each pharmaceutics were evaluated. Both benzocaine and clove oil pharmaceutics showed efficiency as anesthetics for pejerrey fingerlings, with negative correlation between the dose of anesthetics and the anesthesia induction time. For benzocaine, the concentrations between 80mgL-1 and 100mgL-1 showed better results, as for clove oil the optimal concentrations were between 25mgL-1 and 50mgL-1. On the other hand, the anesthesia recovery time did not present significant variation on the different concentrations of the tested products. The tested products are highly metabolizable by pejerrey.

  9. Effects of temperature on the elimination of benzocaine and acetylated benzocaine residues from the edible fillet of rainbow trout (Oncorhynchus mykiss) (United States)

    Stehly, G.R.; Meinertz, J.R.; Gingerich, W.H.


    The effect of temperature (7 degrees C and 16 degrees C) on the extent of accumulation and the elimination of benzocaine (BNZ) and its metabolite, acetylated benzocaine (AcBNZ), in the fillet tissue of rainbow trout was investigated Residues were measured after bath exposure to an anesthetizing concentration of benzocaine (30 mg/l for 5 min) followed by a maintenance concentration (15 mg/l for 30 min). Immediately after exposure, the BNZ concentration in fillet tissue was approximately 27 mu g/g at both temperatures; AcBNZ was 0.3 mu g/g at 7 degrees C and 0.6 mu g/g at 16 degrees C. The rates for elimination (alpha and beta) of BNZ and AcBNZ were not significantly different between the two temperatures. Terminal half-lives of elimination for BNZ were 1.62 h at 7 degrees C and 1.63 h at 16 degrees C; half-lives for AcBNZ were 2.36 h at 7 degrees C and 2.77 h at 16 degrees C.

  10. Optimization of formulation variables of benzocaine liposomes using experimental design. (United States)

    Mura, Paola; Capasso, Gaetano; Maestrelli, Francesca; Furlanetto, Sandra


    This study aimed to optimize, by means of an experimental design multivariate strategy, a liposomal formulation for topical delivery of the local anaesthetic agent benzocaine. The formulation variables for the vesicle lipid phase uses potassium glycyrrhizinate (KG) as an alternative to cholesterol and the addition of a cationic (stearylamine) or anionic (dicethylphosphate) surfactant (qualitative factors); the percents of ethanol and the total volume of the hydration phase (quantitative factors) were the variables for the hydrophilic phase. The combined influence of these factors on the considered responses (encapsulation efficiency (EE%) and percent drug permeated at 180 min (P%)) was evaluated by means of a D-optimal design strategy. Graphic analysis of the effects indicated that maximization of the selected responses requested opposite levels of the considered factors: For example, KG and stearylamine were better for increasing EE%, and cholesterol and dicethylphosphate for increasing P%. In the second step, the Doehlert design, applied for the response-surface study of the quantitative factors, pointed out a negative interaction between percent ethanol and volume of the hydration phase and allowed prediction of the best formulation for maximizing drug permeation rate. Experimental P% data of the optimized formulation were inside the confidence interval (P < 0.05) calculated around the predicted value of the response. This proved the suitability of the proposed approach for optimizing the composition of liposomal formulations and predicting the effects of formulation variables on the considered experimental response. Moreover, the optimized formulation enabled a significant improvement (P < 0.05) of the drug anaesthetic effect with respect to the starting reference liposomal formulation, thus demonstrating its actually better therapeutic effectiveness.

  11. Effect of temperature on the pharmacokinetics of benzocaine in rainbow trout (Oncorhynchus mykiss) after bath exposures (United States)

    Stehly, G.R.; Meinertz, J.R.; Gingerich, W.H.


    The pharmacokinetics of benzocaine during bath exposures at 1 mg/L were determined in rainbow trout acclimated at 6 °C, 12 °C or 18 °C for at least 1 month. Individual fish were exposed to benzocaine in a recirculating system for 4 h and pharmacokinetic parameters were estimated in a unique manner from the concentration of benzocaine in the bath water vs. time curve. Elimination from plasma was also determined after the 4 h exposure. The uptake clearance and metabolic clearance increased with increased acclimatization temperatures (uptake clearance 581 ± 179 mL/min/kg at 6 °C and 1154 ± 447 mL/ min/kg at 18 °C; metabolic clearance 15.2 ± 4.1 mL/min/kg at 6 °C and 22.3 ± 4.2 mL/min/kg at 18 °C). The apparent volume of distribution had a trend for increasing with temperature that was not significant at the 5% level (2369 ± 678 mL/kg at 6 °C to 3260 ± 1182 mL/kg at 18 °C). The elimination half-life of benzocaine in plasma was variable and did not differ significantly with temperature (60.8 ± 30.3 min at 6 °C to 35.9 ± 13.0 min at 12 °C). Elimination of benzocaine from rainbow trout is relatively rapid and even more rapid at higher acclimatization temperatures based on calculated metabolic clearances and measured plasma concentrations, but was not evident by measurement of terminal plasma half-lifes.

  12. Stress of anesthesia with M.S. 222 and Benzocaine in Rainbow Trout (Salmo gairdneri) (United States)

    Wedemeyer, Gary


    Rainbow trout (Salmo gairdneri) anesthetized with M.S. 222 for periods up to 12 min experience interrenal ascorbate depletion, uremia, and moderate hypercholesterolemia. Anesthesia with neutralized M.S. 222 (pH 7) or benzocaine prevented these changes and significantly reduced the variability in plasma glucose, cholesterol, and cortisol, indicating that the stress of anesthesia with M.S. 222 is due to the low pK of the sulfonic acid moiety.

  13. Development, characterization and in vivo evaluation of benzocaine-loaded liposomes. (United States)

    Mura, Paola; Maestrelli, Francesca; González-Rodríguez, Maria Luisa; Michelacci, Ilaria; Ghelardini, Carla; Rabasco, Antonio M


    This study reports the development and in vivo evaluation of a liposomal formulation of the local anaesthetic benzocaine. Multi-lamellar (MLV) and small uni-lamellar (SUV) vesicles entrapping benzocaine were prepared using 50:50 w/w phosphatidylcholine-cholesterol as lipophilic phase and 50:50 v/v ethanol-water as hydrophilic phase. Liposome size, Zeta-potential, encapsulation efficiency and skin penetration properties were determined. Drug permeation from liposomal dispersions, as such or formulated in Carbopol gel, was evaluated through artificial lipophilic membranes and excised abdominal rat skin, whereas in vivo anaesthetic effect was tested on rabbits. Interestingly, addition of the drug into the hydrophilic phase, rather than into the lipophilic one, during liposome preparation enabled an improvement of the MLV's entrapment efficiency from 29.7% to 82.3%. On the other hand, sonication conditions to obtain SUV influenced size and polydispersity index of the vesicles and reduced the entrapment efficiency by about 30%. All liposomal-benzocaine formulations showed sustained release properties and a more intense anaesthetic effect than plain drug. Permeation experiments from drug solutions in gel containing the same amount of ethanol as in the liposomal formulations made it possible to exclude a possible enhancer effect of this solvent, at least when not used in liposomal formulations. MLV with the drug added into the hydrophilic phase gave the most effective formulation, showing a permeability coefficient value 2.5 times higher than that of the plain drug and allowing a significant improvement (Pbenzocaine. These results suggest that a suitably developed liposomal formulation of benzocaine can be of actual value for improving its clinical effectiveness in topical anaesthesia.

  14. Allergic contact dermatitis to benzocaine: the importance of concomitant positive patch test results. (United States)

    González-Rodríguez, A J; Gutiérrez-Paredes, E M; Revert Fernández, Á; Jordá-Cuevas, E


    Local anesthetics are widely used in clinical practice, and adverse effects are not uncommon. Delayed hypersensitivity reactions are among the most common effects, but immediate-type reactions may also occur. Patch testing should be considered in patients with hypersensitivity reactions. We present a case of allergic contact dermatitis to benzocaine that was detected incidentally by patch testing and highlight the importance of correctly interpreting patch test results when there are concomitant positive reactions.

  15. Benzocaine-Induced Methemoglobinemia: A Condition of which all Endoscopists Should Be Aware

    Directory of Open Access Journals (Sweden)

    C Armstrong


    Full Text Available Methemoglobinemia is a rare complication that can occur with the use of benzocaine-containing compounds. Two cases of methemoglobinemia are reported, and the pathophysiology and treatment of methemoglobinemia are reviewed. Both patients received topical 20% benzocaine spray before endoscopy. Immediately following the procedure, there was a reduction in O2 saturation assessed by pulse oximetry that was refractory to O2 therapy. Dramatic peripheral and central cyanosis developed. O2 saturation measured by pulse oximetry ranged from 83% to 87% on O2 by nasal prongs and 100% O2 by a nonrebreathing mask. Both patients were mildly confused and one patient complained of a significant headache. The diagnosis of methemoglobinemia was considered and arterial blood gas sampling was performed. In both patients, the arterial blood had a chocolate brown colour. A methemoglobin level of 48% and 18% was noted in patient 1 and patient 2, respectively. Both patients were treated with methylene blue, resulting in a significant improvement with gradual normalization of their O2 saturation within 10 min to 30 min. The use of benzocaine spray may not markedly alter the patient's perception of endoscopy and thus, the routine use of these agents should be questioned. If such agents are used, the physician must be aware of this association to prevent a delay in the diagnosis and management of this rare, but potentially lethal, condition.

  16. Influence of glyceryl guaiacolate ether on anesthetics in tilapia compared to benzocaine and eugenol

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    Geovana R. Cosenza


    Full Text Available Objective. The study aimed to investigate the effectiveness of glyceryl guaiacolate ether (GGE and compare the times of induction, recovery, hematological changes, total protein and glycaemia among anesthetics in Nile tilapia, Oreochromis niloticus. Materials and methods. A total of 60 tilapia distributed in 3 aquariums (N=20 were used, which formed the group benzocaine (100 mg/L, eugenol (50 mg/L and guaiacol glyceryl ether (9.000 mg/L. After the induction of anesthesia fish blood samples were collected to determine the complete hemogram and glycemia. Then the animals were placed in aquariums with running water for assessing the anesthesia recovery. Results. It was verified that GGE showed longer induction and recovery times as well a significant increase (p0.05. An increase in the number of monocytes in the group treated with benzocaine (p <0.05 was observed in the analysis of the hematological parameters with no difference between groups for other variables. Conclusions. Eugenol and benzocaine allow rapid induction and recovery in Nile tilapia, without evidence of stress during handling and GGE showed high induction and recovery times, being inadequate for anesthetic use in Nile tilapia.

  17. A new validated method for the simultaneous determination of benzocaine, propylparaben and benzyl alcohol in a bioadhesive gel by HPLC. (United States)

    Pérez-Lozano, P; García-Montoya, E; Orriols, A; Miñarro, M; Ticó, J R; Suñé-Negre, J M


    A new HPLC-RP method has been developed and validated for the simultaneous determination of benzocaine, two preservatives (propylparaben (nipasol) and benzyl alcohol) and degradation products of benzocaine in a semisolid pharmaceutical dosage form (benzocaine gel). The method uses a Nucleosil 120 C18 column and gradient elution. The mobile phase consisted of a mixture of methanol and glacial acetic acid (10%, v/v) at different proportion according to a time-schedule programme, pumped at a flow rate of 2.0 ml min(-1). The DAD detector was set at 258 nm. The validation study was carried out fulfilling the ICH guidelines in order to prove that the new analytical method, meets the reliability characteristics, and these characteristics showed the capacity of analytical method to keep, throughout the time, the fundamental criteria for validation: selectivity, linearity, precision, accuracy and sensitivity. The method was applied during the quality control of benzocaine gel in order to quantify the drug (benzocaine), preservatives and degraded products and proved to be suitable for rapid and reliable quality control method.

  18. Synthesis of Benzocaine%苯佐卡因的合成

    Institute of Scientific and Technical Information of China (English)



    Benzocaine was synthesized through the amidation,oxidation,hydrolysis,and esterification based on p-methyl-aniline.The results revealed that the total yield of benzocaine can reach 50%,including 96.4%amidation of p-methyl-aniline,96.5% oxidation,and 75.2% esterification.In the experiment,the product hydrolysis of amidation and oxidation had an effect on esterification.The hydrolysis reaction was studied through orthogonal experiment,and the result and data of the experiment were analyzed.The structure of benzocaine was determined through melting point detecting and IR spectra.%主要研究了以对甲基苯胺为原料通过酰胺化、氧化、水解和酯化合成苯佐卡因的合成工艺条件条件。实验结果表明,对甲基苯胺酰胺化反应收率可达96.4%,氧化反应收率可达96.5%,酯化反应收率为75.2%,苯佐卡因的总收率可达50%左右。实验中酰胺化氧化产物水解对酯化反应影响较大,实验中采用正交实验法对水解反应进行研究,并对实验结果和数据进行分析。通过红外光谱和熔点测定对目标化合物苯佐卡因进行了结构表征。

  19. Use of gelatin-acacia coacervate containing benzocaine in topical formulations. (United States)

    Ichwan, A M; Karimi, M; Dash, A K


    The in vitro release of a drug from topical formulations depends on the concentration of the drug in the formulation, the solubility of the drug in the base, the diffusion coefficient of the drug in the vehicle, and the partition coefficient of the drug between the vehicle, and the release medium. Incorporation of both complexing agents and cosolvents into such formulations has been used to enhance the in vitro release of a drug from topical formulations. In this investigation, a novel approach to enhance the in vitro release of benzocaine from different ointment formulations has been introduced. In this study, benzocaine was microencapsulated using gelatin-acacia complex coacervation technique. Various weight fractions of the coacervate, 5, 10, and 20% (w/w), were incorporated into both oleaginous and absorption bases. The in vitro release characteristics of benzocaine from the resulting ointments were studied using a modified USP Dissolution Apparatus 2. A plot of the cumulative amount of drug released (7-8%) per unit surface area versus (time)(1/2) was linear. Microscopic studies of the formulations revealed that the coacervates maintained their integrity in the formulation during the preparation and storage of the dosage form. Differential scanning calorimetric (DSC) studies indicated that the drug existed in the crystalline state in all formulations including those at a low drug load (0.5% w/w). DSC was also used to determine the solubility of the drug in the formulation. The rate and extent of drug release was higher in the absorption base as compared to the oleaginous base.

  20. Benzocaine complexation with p-sulfonic acid calix[n]arene: experimental ((1) H-NMR) and theoretical approaches. (United States)

    Arantes, Lucas M; Varejão, Eduardo V V; Pelizzaro-Rocha, Karin J; Cereda, Cíntia M S; de Paula, Eneida; Lourenço, Maicon P; Duarte, Hélio A; Fernandes, Sergio A


    The aim of this work was to study the interaction between the local anesthetic benzocaine and p-sulfonic acid calix[n]arenes using NMR and theoretical calculations and to assess the effects of complexation on cytotoxicity of benzocaine. The architectures of the complexes were proposed according to (1) H NMR data (Job plot, binding constants, and ROESY) indicating details on the insertion of benzocaine in the cavity of the calix[n]arenes. The proposed inclusion compounds were optimized using the PM3 semiempirical method, and the electronic plus nuclear repulsion energy contributions were performed at the DFT level using the PBE exchange/correlation functional and the 6-311G(d) basis set. The remarkable agreement between experimental and theoretical approaches adds support to their use in the structural characterization of the inclusion complexes. In vitro cytotoxic tests showed that complexation intensifies the intrinsic toxicity of benzocaine, possibly by increasing the water solubility of the anesthetic and favoring its partitioning inside of biomembranes.

  1. Solubility and phase separation of benzocaine and salicylic acid in 1,4-dioxane-water mixtures at several temperatures. (United States)

    Peña, M Angeles; Bustamante, Pilar; Escalera, Begoña; Reíllo, Aurora; Bosque-Sendra, Juan Manuel


    The solubilities of benzocaine and salicylic acid were determined in water-dioxane mixtures at several temperatures (5-40 degrees C for benzocaine and 10-40 degrees C for salicylic acid). The solubility curves as a function of dioxane ratio showed a maximum at 90% dioxane at all temperatures. Above 25 degrees C, the homogeneous mixture splits into two liquid immiscible phases. For benzocaine, the initial dioxane concentration range at which phase separation takes place increased with temperature (50-60% at 25 degrees C, 50-70% at 30-35 degrees C and 40-70% at 40 degrees C). For salicylic acid, the dioxane concentration required for phase separation (40-60% dioxane) did not change with temperature. Phase separation was not related to solid phase changes (polymorphism or solvates). The phase composition and drug extraction at the drug-rich phase were determined. The apparent enthalpies of the solution process were a nonlinear function of the dioxane ratio for both drugs. The apparent enthalpy of solution of benzocaine was larger than that expected at the upper limit of phase separation (70% dioxane), whereas for salicylic acid the apparent enthalpy of solution decreased abruptly at the region corresponding to phase separation (40-70% dioxane). Both drugs showed a nonlinear pattern of enthalpy-entropy compensation.

  2. High-performance liquid chromatographic assay for benzocaine and p-aminobenzoic acid including preliminary stability data. (United States)

    Narang, P K; Bird, G; Crouthamel, W G


    A high-performance liquid chromatographic assay was developed that separates and quantitates benzocaine and its primary degradation product, p-aminobenzoic acid. This method is rapid, sensitive, and specific. Preliminary stability data obtained with this method demonstrate its utility for this purpose.

  3. Reduced discomfort during High-Definition transcutaneous stimulation using 6% benzocaine

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    Berkan eGuleyupoglu


    Full Text Available AbstractBackground High-Definition transcranial Direct Current Stimulation (HD-tDCS allows for non-invasive neuromodulation using an array of compact (approximately 1 cm2 contact area High-Definition (HD electrodes, as compared to conventional tDCS (which uses two large pads that are approximately 35cm2. In a previous transcutaneous study, we developed and validated designs for HD electrodes that reduce discomfort over >20 min session with 2 mA electrode current.ObjectiveThe purpose of this study was to investigate the use of a chemical pretreatment with 6% benzocaine (topical numbing agent to further reduce subjective discomfort during transcutaneous stimulation and to allow for better sham controlled studies.MethodsPre-treatment with 6% benzocaine was compared with control (no pretreatment for 22 minutes 2 mA of stimulation, with either CCNY-4 or Lectron II electroconductive gel, for both cathodal and anodal transcutaneous (forearm stimulation (8 different combinations.Results Results show that for all conditions and polarities tested, stimulation with HD electrodes is safe and well tolerated and that pretreatment further reduced subjective discomfort. ConclusionPretreatment with a mild analgesic reduces discomfort during HD-tDCS.

  4. Double-blind comparison of two types of benzocaine lozenges for the treatment of acute pharyngitis. (United States)

    Busch, Regina; Graubaum, Hans-Joachim; Grünwald, Jörg; Schmidt, Mathias


    In a reference-controlled double-blind trial in patients with acute pharyngitis the effects of a newly developed lozenge containing 8 mg of benzocaine (p-aminobenzoic acid ethyl ester, CAS 94-09-7) were compared with those of an identically dosed commercial pastille. 246 patients were randomized to receive either the lozenges (group A, n = 123) or the pastilles (group B, n = 123). Each patient took a total of six doses within 12 h according to the double-dummy principle, with each single dose spaced by 2 h. The primary parameter was the assessment of the responder rate with = 50 % pain relief within 15 min post application. Further parameters included the relative relief of pain in the course of the study and the tolerability of the formulation. After application of the first unit the comparison of groups yielded very similar and statistically not differing results for efficacy in both groups, with responder rates of 25.2 % and 22.0 % in groups A and B, respectively. One adverse drug reaction was observed in group B (burning and tingling feeling on the tongue), which, however, did not lead to discontinuation of study participation. In all other cases tolerability was stated to be "good to very good". The application of the benzocaine lozenges was statistically non-inferior to the use of the pastilles.

  5. On the polymorphism of benzocaine; a low-temperature structural phase transition for form (II). (United States)

    Chan, Eric J; Rae, A David; Welberry, T Richard


    A low-temperature structural phase transition has been observed for form (II) of benzocaine (BZC). Lowering the temperature doubles the b-axis repeat and changes the space group from P2(1)2(1)2(1) to P112(1) with gamma now 99.37 degrees. The structure is twinned, the twin rule corresponding to a 2(1) screw rotation parallel to a. The phase transition is associated with a sequential displacement parallel to a of zigzag bi-layers of ribbons perpendicular to b*. No similar phase transition was observed for form (I) and this was attributed to the different packing symmetries of the two room-temperature polymorphic forms.

  6. Synthesis and methemoglobinemia-inducing properties of benzocaine isosteres designed as humane rodenticides. (United States)

    Conole, Daniel; Beck, Thorsten M; Jay-Smith, Morgan; Tingle, Malcolm D; Eason, Charles T; Brimble, Margaret A; Rennison, David


    A number of isosteres (oxadiazoles, thiadiazoles, tetrazoles and diazines) of benzocaine were prepared and evaluated for their capacity to induce methemoglobinemia-with a view to their possible application as humane pest control agents. It was found that an optimal lipophilicity for the formation of methemoglobin (metHb) in vitro existed within each series, with 1,2,4-oxadiazole 3 (metHb%=61.0±3.6) and 1,3,4-oxadiazole 10 (metHb%=52.4±0.9) demonstrating the greatest activity. Of the 5 candidates (compounds 3, 10, 11, 13 and 23) evaluated in vivo, failure to induce a lethal end-point at doses of 120mg/kg was observed in all cases. Inadequate metabolic stability, particularly towards hepatic enzymes such as the CYPs, was postulated as one reason for their failure.

  7. Atomic determinants of state-dependent block of sodium channels by charged local anesthetics and benzocaine. (United States)

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


    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.

  8. Methemoglobinemia induced by exposure to topical benzocaine for an awake nasal intubation--a case report. (United States)

    Lin, Shih-Kai; Wu, Ji-Leih; Lee, Yung-Lung; Tsao, Shao-Lun


    Topical benzocaine and lidocaine are widely used in general anesthesia to minimize the stimulation by awake intubation and in very rare occasion they may induce methemoglobinemia. Although this complication is uncommon, it may be potentially lethal. Here we report a 29-year-old female who was scheduled to receive correction of malocclusion and developed acute methemoglobinemia soon after induction of general anesthesia. Three weeks ago, she had received open reduction for fracture of mandible with intermaxillary fixation under general anesthesia, for which awake fiberoptic intubation was smoothly performed after premedication with 2% topical lidocaine and intravenous fentanyl. This time, trachomucosal block with 4 mL of 4% topical lidocaine and spray of 20% topical benzocaine over the oral cavity and nostrils were carried out before intubation. Awake blind intubation was performed because she could not open her mouth for more than 1 cm. A 6.5 mm-sized nasal endotracheal tube was smoothly placed in first attempt. About 10 min later, an unexplained cyanosis occurred and SpO2 fell to about 70%. Based on a high oxygen tension by arterial blood gas analysis (PaO2) with a contradictory fall of oxygen saturation by pulse oximetry (SpO2), acute methemoglobinemia was highly suspected. The diagnosis was confirmed by multiple-wavelength CO-oximetry. The methemoglobinemia was resolved gradually after methylene blue was given. In conclusion, we must always take the possibility of methemoglobinemia into consideration for differential diagnosis in case of unexplained cyanosis, particularly when patients have prior exposure to methemoglobin-inducing agents.

  9. Screening of formulation variables for the preparation of poly(epsilon-caprolactone) nanocapsules containing the local anesthetic benzocaine. (United States)

    Moraes, Carolina Morales; de Matos, Angélica Prado; Grillo, Renato; de Melo, Nathalie F S; de Paula, Eneida; Dias Filho, Newton Luiz; Rosa, André Henrique; Fraceto, Leonardo Fernandes


    In this work we describe the screening of four parameters in the preparation, by nanoprecipitation, of poly(epsilon-caprolactone) nanocapsules, used as a drug carrier system for the local anesthetic, benzocaine. A 2(4-1) factorial experimental design was used to study the influence of four different independent variables (polymer, oily phase, Span 60 and Tween 80) on nanocapsule characteristics (size, polydispersion index, zeta potential) and drug loading capability. Best results were obtained using an aqueous formulation comprising 100 mg of polymer, 200 mg of oily phase, 40 mg of Span 60 and 60 mg of Tween 80 in a final volume of 10 mL which produced a colloidal system with particle size of 188 nm, zeta potential -32 mV, polydispersion index 0.07, and benzocaine association efficiency > 87%. These findings open the way for future clinical studies using such formulations.

  10. Benzocaine and eugenol as anesthetics for Brycon hilarii - doi: 10.4025/actascianimsci.v35i2.16644

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    Fábio Bittencourt


    Full Text Available Anesthetic products are frequently employed during fish handling practices; however, the correct doses of the various chemicals for different species are still unknown. This study determined the ideal concentrations of benzocaine and eugenol as anesthetics used in Brycon hilarii juveniles. The fish were acquired from a commercial fish farm located in western Paraná state, Brazil, totaling 104 juveniles, with average body weight and length of 50.04 ± 20.80 g and 16.30 ± 12.32 cm respectively. The study was carried out at the Aquiculture Laboratory from the Aquaculture Management Study Group - GEMAq at the West Parana State University. Five benzocaine concentrations (50.0, 100.0, 150.0, 200.0 and 250.0 mg L-1 and seven eugenol concentrations (50.0, 100.0, 150.0, 200.0, 250.0, 300.0 and 350 mg L-1 were evaluated in order to assess the induction time to anesthesia. The fish were transferred to anesthetic-free tanks to recover, and the time needed to return to normal activity was recorded. The best results were observed with the benzocaine dose of 100 mg L-1 and the eugenol dose between 100 and 150 mg L-1.  

  11. Tricaine (MS-222) is a safe anesthetic compound compared to benzocaine and pentobarbital to induce anesthesia in leopard frogs (Rana pipiens). (United States)

    Cakir, Yavuz; Strauch, Stephen M


    Tricaine (MS-222) is used commonly for sedation, immobilization, and anesthesia of poikilothermic animals. The anesthetic efficacy of different concentrations of MS-222 was compared to benzocaine and pentobarbital on the physiological changes, heart rate and ECG (electrocardiogram) parameters in the leopard frog, Rana pipiens. Loss of righting reflex (RR), loss of pain response (NR = nociceptor response) and recovery time were measured. Heart rate and ECG parameters were also tested before and during anesthesia. The time to loss of RR and NR decreased while recovery time markedly increased with the increasing concentration of MS-222. Benzocaine at 200 mg/l induced a rapid anesthesia, but all frogs needed resuscitation. Pentobarbital at 300 mg/l induced a slow anesthesia, however, all of the frogs also needed resuscitation. All anesthetics at the mentioned concentrations decreased heart rate significantly as well as altered the ECG parameters. All anesthetics prolonged the Q-T interval, and MS-222 at 800 mg/l and benzocaine at 200 mg/l were the most effective anesthetic concentrations in increasing the Q-T interval. Frogs anesthetized by benzocaine and pentobarbital and high concentrations of MS-222 required resuscitation due to hypoxia. Pentobarbital and benzocaine seem to be very effective compounds, but their safety margins are narrow because of ventilatory failure. Therefore, MS-222 at a concentration of 200 mg/l or less is highly recommended for leopard frogs because prolonged recovery, high mortality rate and significant ECG changes are observed with higher concentrations of MS-222.

  12. Dextran-5-(4-ethoxycarbonylphenylazo)salicylic acid ester, a polymeric colon-specific prodrug releasing 5-aminosalicylic acid and benzocaine, ameliorates TNBS-induced rat colitis. (United States)

    Nam, Joon; Kim, Wooseong; Lee, Sunyoung; Jeong, Seongkeun; Yoo, Jin-Wook; Kim, Min-Soo; Jung, Yunjin


    Local anesthetics have beneficial effects on colitis. Dextran-5-(4-ethoxycarbonylphenylazo)salicylic acid ester (Dex-5-ESA), designed as a polymeric colon-specific prodrug liberating 5-ASA and benzocaine in the large intestine, was prepared and its therapeutic activity against colitis was evaluated using a TNBS-induced rat colitis model. Dex-5-ESA liberated 5-ASA and benzocaine in the cecal contents while (bio)chemically stable in the small intestinal contents and mucosa. Oral administration of Dex-5-ESA (equivalent to 10 mg 5-ASA/kg, twice a day) alleviated colonic injury and reduced MPO activity in the inflamed colon. In parallel, pro-inflammatory mediators, COX-2, iNOS and CINC-3, elevated by TNBS-induced colitis, were substantially diminished in the inflamed colon. Dex-5-ESA was much more effective for the treatment of colitis than 5-(4-ethoxycarbonylphenylazo)salicylic acid (5-ESA) that may not deliver benzocaine to the large intestine. Our data suggest that Dex-5-ESA is a polymeric colon-specific prodrug, liberating 5-ASA and benzocaine in the target site (large intestine), probably exerting anti-colitic effects by combined action of 5-ASA and benzocaine.

  13. Methemoglobin and sulfhemoglobin formation due to benzocaine and lidocaine in macaques

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    Martin, D.G.; Woodard, C.L.; Gold, M.B.; Watson, C.E.; Baskin, S.I.


    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.

  14. Benzocaine polymorphism: pressure-temperature phase diagram involving forms II and III. (United States)

    Gana, Inès; Barrio, Maria; Do, Bernard; Tamarit, Josep-Lluís; Céolin, René; Rietveld, Ivo B


    Understanding the phase behavior of an active pharmaceutical ingredient in a drug formulation is required to avoid the occurrence of sudden phase changes resulting in decrease of bioavailability in a marketed product. Benzocaine is known to possess three crystalline polymorphs, but their stability hierarchy has so far not been determined. A topological method and direct calorimetric measurements under pressure have been used to construct the topological pressure-temperature diagram of the phase relationships between the solid phases II and III, the liquid, and the vapor phase. In the process, the transition temperature between solid phases III and II and its enthalpy change have been determined. Solid phase II, which has the highest melting point, is the more stable phase under ambient conditions in this phase diagram. Surprisingly, solid phase I has not been observed during the study, even though the scarce literature data on its thermal behavior appear to indicate that it might be the most stable one of the three solid phases.

  15. Molecular dynamics simulation of the partitioning of benzocaine and phenytoin into a lipid bilayer. (United States)

    Martin, Lewis J; Chao, Rebecca; Corry, Ben


    Molecular dynamics simulations were used to examine the partitioning behaviour of the local anaesthetic benzocaine and the anti-epileptic phenytoin into lipid bilayers, a factor that is critical to their mode of action. Free energy methods are used to quantify the thermodynamics of drug movement between water and octanol as well as for permeation across a POPC membrane. Both drugs are shown to favourably partition into the lipid bilayer from water and are likely to accumulate just inside the lipid headgroups where they may alter bilayer properties or interact with target proteins. Phenytoin experiences a large barrier to cross the centre of the bilayer due to less favourable energetic interactions in this less dense region of the bilayer. Remarkably, in our simulations both drugs are able to pull water into the bilayer, creating water chains that extend back to bulk, and which may modify the local bilayer properties. We find that the choice of atomic partial charges can have a significant impact on the quantitative results, meaning that careful validation of parameters for new drugs, such as performed here, should be performed prior to their use in biomolecular simulations.

  16. Quantification of benzocaine and its metabolites in channel catfish tissues and fluids by HPLC. (United States)

    Szoke, A; Hayton, W L; Schultz, I R


    Methods for extraction and gradient HPLC quantification were developed for benzocaine (BZ) and three of its metabolites to be used in conjunction with a reverse isotope technique. The metabolites were p-aminobenzoic acid (PABA), acetyl-p-aminobenzoic acid (AcPABA) and acetylbenzocaine (AcBZ). The matrixes studied were white muscle, red muscle, skin, liver, trunk kidney, head kidney, plasma and the bile of channel catfish. Analytes were validated for each of the compounds at 25 and 100 nmol per sample in the various tissues and fluids. The intraday variability (R.S.D.) was less than 13% in all tissues and fluids except for BZ in the liver. Recoveries varied from matrix to matrix for each analyte. The highest recoveries were obtained from plasma which ranged from 82.8-99.8% depending on the concentration. The average recovery of the compounds from tissues was between 50 and 78%, except for liver where the recovery of PABA and BZ was below 30%. Detection was by UV absorbance at 286 nm and the linear range was 2.5-15 nmol 100 ml-1 for all analytes. The method was selective; no interference peaks coeluted with the analytes.

  17. An Atypical Case of Methemoglobinemia due to Self-Administered Benzocaine

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    Thomas M. Nappe


    Full Text Available Acquired methemoglobinemia is an uncommon hemoglobinopathy that results from exposure to oxidizing agents, such as chemicals or medications. Although, as reported in the adult population, it happens most often due to prescribed medication or procedural anesthesia and not due to easily accessed over-the-counter medications, the authors will describe an otherwise healthy male adult with no known medical history and no prescribed medications, who presented to the emergency department reporting generalized weakness, shortness of breath, headache, dizziness, and pale gray skin. In addition, the patient reported that he also had a severe toothache for several days, which he had been self-treating with an over-the-counter oral benzocaine gel. Ultimately, the diagnosis of methemoglobinemia was made by clinical history, physical examination, and the appearance of chocolate-colored blood and arterial blood gas (ABG with cooximetry. After 2 mg/kg of intravenous methylene blue was administered, the patient had complete resolution of all signs and symptoms. This case illustrates that emergency physicians should be keenly aware of the potential of toxic hemoglobinopathy secondary to over-the-counter, nonprescribed medications. Discussion with patients regarding the dangers of inappropriate use of these medicines is imperative, as such warnings are typically not evident on product labels.

  18. An Atypical Case of Methemoglobinemia due to Self-Administered Benzocaine. (United States)

    Nappe, Thomas M; Pacelli, Anthony M; Katz, Kenneth


    Acquired methemoglobinemia is an uncommon hemoglobinopathy that results from exposure to oxidizing agents, such as chemicals or medications. Although, as reported in the adult population, it happens most often due to prescribed medication or procedural anesthesia and not due to easily accessed over-the-counter medications, the authors will describe an otherwise healthy male adult with no known medical history and no prescribed medications, who presented to the emergency department reporting generalized weakness, shortness of breath, headache, dizziness, and pale gray skin. In addition, the patient reported that he also had a severe toothache for several days, which he had been self-treating with an over-the-counter oral benzocaine gel. Ultimately, the diagnosis of methemoglobinemia was made by clinical history, physical examination, and the appearance of chocolate-colored blood and arterial blood gas (ABG) with cooximetry. After 2 mg/kg of intravenous methylene blue was administered, the patient had complete resolution of all signs and symptoms. This case illustrates that emergency physicians should be keenly aware of the potential of toxic hemoglobinopathy secondary to over-the-counter, nonprescribed medications. Discussion with patients regarding the dangers of inappropriate use of these medicines is imperative, as such warnings are typically not evident on product labels.

  19. Physico-chemical characterization of benzocaine-beta-cyclodextrin inclusion complexes. (United States)

    Pinto, Luciana M A; Fraceto, Leonardo Fernandes; Santana, Maria Helena A; Pertinhez, Thelma A; Junior, Sérgio Oyama; de Paula, Eneida


    Local anesthetics are able to induce pain relief by binding to the sodium channel of excitable membranes, blocking the influx of sodium ions and the propagation of the nervous impulse. Benzocaine (BZC) is a local anesthetic whose low water-solubility limits its application to topical formulations. The present work focuses on the characterization of inclusion complexes of BZC in beta-cyclodextrin (beta-CD). Differential scanning calorimetry and electron microscopy gave evidences of the formation and the morphology of the complex. Fluorescence spectroscopy showed a BZC/beta-CD 1:1 stoichiometry. Phase-solubility diagrams allowed the determination of the association constants between BZC and beta-CD (549 M(-1)) and revealed that a three-fold increase in BZC solubility can be reached upon complexation with beta-CD. The details of BZC/beta-CD molecular interaction were analyzed by 1H 2D NMR allowing the proposition of an inclusion model for BZC into beta-CD where the aromatic ring of the anesthetic is located near the head of the beta-CD cavity. Moreover, in preliminary toxicity studies, the complex seems to be less toxic than BZC alone, since it induced a decrease in the in vitro oxidation of human hemoglobin. These results suggest that the BZC/beta-CD complex represents an effective novel formulation to enhance BZC solubility in water, turning it promising for use outside its traditional application, i.e., in infiltrative anesthesia.

  20. Severe methemoglobinemia complicating topical benzocaine use during endoscopy in a toddler: a case report and review of the literature. (United States)

    Dahshan, Ahmed; Donovan, G Kevin


    Severe methemoglobinemia resulting from the use of topical benzocaine has been reported in adults as a rare complication. Here we report a case of severe acquired methemoglobinemia resulting from topical use of benzocaine spray during diagnostic upper gastrointestinal endoscopy in a 3-year-old boy with repeated episodes of hematemesis 3 weeks posttonsillectomy. He developed marked cyanosis and became increasingly agitated immediately after completion of his unremarkable endoscopic procedure, which was performed under intravenous sedation. He did not respond to maximum supplemental oxygen and had increased respiratory effort. His pulse oximetry dropped to 85%, but simultaneous arterial blood-gas analysis showed marked hypoxemia (Po2 = 29%) and severe methemoglobinemia (methemoglobin = 39%). His cyanosis and altered mental status promptly resolved after intravenous administration of methylene blue. In patients with methemoglobinemia, pulse oximetry tends to overestimate the actual oxygen saturation and is not entirely reliable. Posttonsillectomy bleeding is a rare but occasionally serious complication that could occur weeks after the surgery, although it more commonly occurs within the first few days. Physicians should remain aware of the possibility of its late onset. This case illustrates the severity of acquired methemoglobinemia that may result from even small doses of topical benzocaine and highlights the fact that prompt treatment of the disorder can be life saving. We question the rationale for routine use of topical anesthetic spray for sedated upper gastrointestinal endoscopy in children. By bringing the attention of pediatricians to this rare but serious complication, we hope that it will result in its improved recognition and possible prevention.

  1. Desenvolvimento e caracterização de nanocápsulas de poli (L-lactídeo contendo benzocaína Development and characterization of poli (L-lactide nanocapsules containing benzocaine

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    Nathalie Ferreira Silva de Melo


    Full Text Available In this paper we describe the preparation poly (L-lactide (PLA nanocapsules as a drug delivery system for the local anesthetic benzocaine. The characterization and in vitro release properties of the system were investigated. The characterization results showed a polydispersity index of 0.14, an average diameter of 190.1± 3 nm, zeta potential of -38.5 mV and an entrapment efficiency of 73%. The release profile of Benzocaine loaded in PLA nanocapsules showed a significant different behavior than that of the pure anesthetic in solution. This study is important to characterize a drug release system using benzocaine for application in pain treatment.


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    尹大伟; 刘玉婷


    Benzocaine was synthesized using chitosan sulfate as catalyst.Simultaneously, the effect of some factors, such as the amount of catalysts, pH, time and reaction temperature on the yield of benzocaine were studied.The experiment results affirmed the best reaction conditions: pH= 2, the mass of chitosan sulfate was 0.8 g, reaction tiome was 4 h, refluxing temperature was 65 ℃, the yield of benzocaine was 86.8 %.Using chitosan sulfate in synthesis of benzocaine, the reaction condition was mild, nonexpendable, non-corrosive, and can be reused.%采用壳聚糖硫酸盐催化合成苯佐卡因(对氨基苯甲酸乙酯),讨论了催化剂用量、体系pH、反应时间和回流温度对酯产率的影响,确定了最佳的反应条件:体系pH=2,催化剂用量0.8 g (对氨基苯甲酸0.01 mol),反应时间4 h,回流温度65 ℃,苯佐卡因产率为86.8%.壳聚糖硫酸盐具有良好的催化性能,反应条件温和,无废酸产生,无腐蚀,而且可以重复使用.

  3. Controlled Release of Benzocaine from Monomer and Copolymer Carriers in Synthetic Gastro-intestinal Media

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    Houaria Merine


    Full Text Available New dosage forms able to control drug release in the gastro-intestinal media have been prepared and investigated in this paper. Two different type of medicinal agent bonding (MA, in our case Benzocaine (Bz, were chosen in order to examine drug release. i MA attached to ethylenic monomer (m,p-vinylbenzaldehyde, condensation reaction. ii The copolymer carrier (Cp is obtained by copolymerizing this monomer. These two carriers were well characterized by microanalysis, FTIR, DSC (Tg and GPC (Ip and the two fraction α and β were calculated from elemental analyses of Cp. The results showed good polydispersity and low average molecular weight. MA linked to an organic product by the azomethine function (C=N, hydrolytically sensitive, allowed controlled release of Bz, from the monomer carrier and from the bending Schiff bases groups. Theoretical and experimental analyses of controlled release of Bz kinetics from monomer and copolymer carriers were conducted for the case of contact with synthetic gastro-intestinal fluids at various pH (1,2; 6,0 and 8,0 at 37°C. The process was found to be controlled by the nature of media (heterogeneous, which involved the preliminary hydrolysis, and the drug (Bz diffusing out of structure of copolymer (Cp to the external aqueous media. The results obtained on the rate of delivery showed a clear difference between pH = 1,2 and pH = 6,0 and 8,0 based on: i The cation of p-aminoniumbenzoic acid (PABAH+ release at pH = 1,2 ii Bz release at pH = 6,0 and 8,0

  4. Investigation on the pH-dependent binding of benzocaine and lysozyme by fluorescence and absorbance (United States)

    Li, Shihui; Li, Daojin


    The interaction mechanism between benzocaine (BZC) and lysozyme (Lys) has been investigated by fluorescence, synchronous fluorescence, ultraviolet-vis (UV) absorption spectra, and three-dimensional fluorescence (3-D) in various pH medium. The observations of fluorescence spectra were mainly rationalized in terms of a static quenching process at lower concentration of BZC ( CBZC/ CLys 9) at pH 7.4 and 8.4. However, the fluorescence quenching was mainly arisen from static quenching by complex formation in all studied drug concentrations at pH 3.5. The structural characteristics of BZC and Lys were probed, and their binding affinities were determined under different pH conditions (pH 3.5, 7.4, and 8.4). The results indicated that the binding abilities of BZC to Lys decreased at the pH below and above the simulative physiological condition (pH 7.4) due to the alterations of the protein secondary and tertiary structures or the structural change of BZC. The effect of BZC on the conformation of Lys was analyzed using UV, synchronous fluorescence and three-dimensional fluorescence under different pH conditions. These results indicate that the binding of BZC to Lys causes apparent change in the secondary and tertiary structures of Lys. The effect of Zn 2+ on the binding constant of BZC with Lys under various pH conditions (pH 3.5, 7.4, and 8.4) was also studied.

  5. Effect of preparation technique on the properties and in vivo efficacy of benzocaine-loaded ethosomes. (United States)

    Maestrelli, Francesca; Capasso, Gaetano; González-Rodríguez, Maria L; Rabasco, Antonio M; Ghelardini, Carla; Mura, Paola


    This study aimed to investigate the influence of the preparation conditions on the performance of an ethosomal formulation for topical delivery of the local anesthetic agent, benzocaine (BZC). Ethosomes were prepared with different techniques, such as thin-layer evaporation, freezing and thawing, reverse-phase evaporation, extrusion and sonication, obtaining, respectively, multilayer vesicles (MLVs), frozen and thawed MLV (FATMLV), large unilamellar vesicles (LUVs), and small unilamellar vesicles (SUVs). The obtained vesicles were characterized for morphology, size, zeta potential, and entrapment efficiency (EE%), and their stability was monitored during storage at 4 degrees C. In vitro permeation properties from gels incorporating drug ethosomal dispersions were evaluated in vitro by using artificial lipophilic membranes, while their anesthetic effect was determined in vivo on rabbits. The results suggested that the vesicle preparation method plays an important role in affecting the properties and effectiveness of ethosomal formulations. MLVs and LUVs exhibited higher drug EE% and better stability than FATMLV and SUV vesicles. The In vitro drug permeation rate was directly related to the vesicle EE% and varied in the order MLV>LUV approximately FATMLV>SUV. The therapeutic efficacy of BZC ethosomal formulations was significantly improved with respect to the corresponding BZC solution. The best results, in terms of enhanced intensity of anesthetic effect, were given by formulations containing MLVs and LUVs, and the order of effectiveness was MLV approximately LUV>FATMLV approximately SUV, rather similar to that found in permeation studies. On the contrary, unexpectedly, the effectiveness order in increasing the duration of drug action was SUV> or =MLV>LUV approximately FATMLV. The highest efficacy of SUVs was probably due to the more intimate contact with the epithelium due to their greatest surface area, which allowed the longest extension of drug therapeutic

  6. Immobilization of paracetamol and benzocaine pro-drug derivatives as long-range self-organized monolayers on graphite. (United States)

    Popoff, Alexandre; Fichou, Denis


    We show here by means of scanning tunneling microscopy (STM) at the liquid/solid interface that paracetamol and benzocaine molecules bearing a long aliphatic chain can be immobilized on highly oriented pyrolitic graphite (HOPG) as perfectly ordered two-dimensional domains extending over several hundreds of nanometers. In both cases, high-resolution STM images reveal that compounds 1 and 2 self-assemble into parallel lamellae having a head-to-head arrangement. The paracetamol heads of 1 are in a zigzag position with entangled n-dodecyloxy side chains while benzocaine heads of compound 2 are perfectly aligned as a double row and have their palmitic side chains on either sides of the head alignment. We attribute the very long-range ordering of these two pro-drug derivatives on HOPG to the combined effects of intermolecular H-bonding on one side and Van der Waals interactions between aliphatic side chains and graphite on the other side. The 2D immobilization of pro-drug derivatives via a non-destructive physisorption mechanism could prove to be useful for applications such as drug delivery if it can be realized on a biocompatible substrate.

  7. Intraoperative detection of methemoglobinemia in a patient given benzocaine spray to relieve discomfort from a nasogastric tube: a case report. (United States)

    Young, Barb


    A 27-year-old man who had 2 admissions 1 month apart for abdominal surgery had a high methemoglobin (MHb) level secondary to liberal use of benzocaine oral spray. A co-oximetry level for MHb of greater than 0.30 proportion of total hemoglobin (30.1%) was detected intraoperatively. The patient was successfully treated with methylene blue intravenously and recovered uneventfully. When the arterial blood gas with a normal partial pressure of oxygen is inconsistent with a low pulse oximeter reading and with the physical appearance of the patient, methemoglobinemia should be considered as a differential diagnosis. This case illustrates the acquired form of methemoglobinemia. Adequate oxygen delivery to the tissues in the body is compromised when MHb overwhelms the capacity of the red blood cells to carry oxygen. If methemoglobinemia is left untreated, it may be fatal.

  8. Predicting the excess solubility of acetanilide, acetaminophen, phenacetin, benzocaine, and caffeine in binary water/ethanol mixtures via molecular simulation (United States)

    Paluch, Andrew S.; Parameswaran, Sreeja; Liu, Shuai; Kolavennu, Anasuya; Mobley, David L.


    We present a general framework to predict the excess solubility of small molecular solids (such as pharmaceutical solids) in binary solvents via molecular simulation free energy calculations at infinite dilution with conventional molecular models. The present study used molecular dynamics with the General AMBER Force Field to predict the excess solubility of acetanilide, acetaminophen, phenacetin, benzocaine, and caffeine in binary water/ethanol solvents. The simulations are able to predict the existence of solubility enhancement and the results are in good agreement with available experimental data. The accuracy of the predictions in addition to the generality of the method suggests that molecular simulations may be a valuable design tool for solvent selection in drug development processes.

  9. Evaluation of supercritical fluid technology as preparative technique of benzocaine-cyclodextrin complexes--comparison with conventional methods. (United States)

    Al-Marzouqi, Ali H; Jobe, Baboucarr; Dowaidar, Ali; Maestrelli, Francesca; Mura, Paola


    The objective of this study was to investigate the effect of the preparation method on the physico-chemical properties of complexes prepared between beta-cyclodextrin (beta-Cyd) and benzocaine (BZC). In particular, the effectiveness of a new technique based on supercritical carbon dioxide (SC CO(2)) for preparing solid drug-cyclodextrin complexes was investigated and compared to other more conventional methods such as kneading (KN), co-evaporation (COE), co-grinding (GR) and sealed-heating (S.H.). Effects of temperature, pressure and exposure time on the properties of complexes prepared by SC CO(2) technology were also studied. The different systems were characterized by differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR), powder X-ray diffractometry (PXRD) and dissolution test according to the dispersed amount method. The co-grinding (GR) method resulted in amorphous products while other methods led to crystalline or partially amorphous products depending on both the method and its experimental conditions. SC CO(2) method revealed to be an effective technique for preparing solid systems between beta-cyclodextrin and benzocaine, avoiding the use of organic solvents (and problems of their complete removal) and allowing an easy scale-up of the process. As for the influence of the experimental conditions in promoting the solid-state drug-carrier interaction when using the SC CO(2) method, temperature seemed to play the major role, whereas pressure and exposure times had more limited effects. Dissolution tests confirmed a limited but favourable effect in increasing the exposure time, while indicated a possible interaction effect between temperature and pressure in influencing the dissolution performance of the final product. The best product obtained by the SC CO(2) method showed dissolution properties similar to those of the co-ground product and only slightly lower than the system obtained by sealed-heating, which was the most

  10. Effect of the interfacial tension and ionic strength on the thermodynamic barrier associated to the benzocaine insertion into a cell membrane. (United States)

    López Cascales, J J; Oliveira Costa, S D


    The insertion of local anaesthetics into a cell membrane is a key aspect for explaining their activity at a molecular level. It has been described how the potency and response time of local anaesthetics is improved (for clinical applications) when they are dissolved in a solution of sodium bicarbonate. With the aim of gaining insight into the physico-chemical principles that govern the action mechanism of these drugs at a molecular level, simulations of benzocaine in binary lipid bilayers formed by DPPC/DPPS were carried out for different ionic strengths of the aqueous solution. From these molecular dynamic simulations, we observed how the thermodynamic barrier associated with benzocaine insertion into the lipid bilayers diminished exponentially as the fraction of DPPS in the bilayer increased, especially when the ionic strength of the aqueous solution increased. In line with these results, we also observed how this thermodynamic barrier diminished exponentially with the phospholipid/water interfacial tension.

  11. Development, characterization, and in vitro and in vivo evaluation of benzocaine- and lidocaine-loaded nanostructrured lipid carriers. (United States)

    Puglia, Carmelo; Sarpietro, Maria Grazia; Bonina, Francesco; Castelli, Francesco; Zammataro, Magda; Chiechio, Santina


    The present study concerns the in vitro and in vivo evaluation of benzocaine (BENZO) and lidocaine (LIDO) topical delivery from nanostructured lipid carriers (NLCs). Morphology and dimensional distribution of NLCs have been, respectively, characterized by differential scanning calorimetry (DSC) and photon correlation spectroscopy. The release pattern of BENZO and LIDO from NLCs was evaluated in vitro determining drug percutaneous absorption through excised human skin. Radiant heat tail-flick test was carried out in mice to determine the antinociceptive effect of BENZO and LIDO from NLC. DSC studies revealed that the inner oil phase of NLC plays a significant role in stabilizing the particle architecture and increasing the drug solubility. In vitro evidences show that BENZO and LIDO, when incorporated in viscosized NLC dispersions, exhibited a lower flux with respect to formulations containing the free drugs in the aqueous phase. In vivo study enabled to demonstrate that BENZO and LIDO can be released in a prolonged fashion when incorporated into lipid carriers. The results obtained pointed out NLC capability to act as an effective drug reservoir, thus prolonging the anesthetic effect of BENZO and LIDO.

  12. Liposomal-benzocaine gel formulation: correlation between in vitro assays and in vivo topical anesthesia in volunteers. (United States)

    Franz-Montan, Michelle; Cereda, Cintia Maria Saia; Gaspari, Adele; da Silva, Camila Morais Gonçalves; de Araújo, Daniele Ribeiro; Padula, Cristina; Santi, Patrizia; Narvaes, Eliene; Novaes, Pedro Duarte; Groppo, Francisco Carlos; de Paula, Eneida


    The aim of the present study was to characterize a liposome-based benzocaine (BZC) formulation designed for topical use on the oral mucosa and to evaluate its in vitro retention and permeation using the Franz-type diffusion cells through pig esophagus mucosa. To predict the effectiveness of new designed formulations during preclinical studies, a correlation between in vitro assays and in vivo efficacy was performed. Liposomal BZC was characterized in terms of membrane/water partition coefficient, encapsulation efficiency, size, polydispersity, zeta potential, and morphology. Liposomal BZC (BL10) was incorporated into gel formulation and its performances were compared to plain BZC gel (B10) and the commercially available BZC gel (B20). BL10 and B10 presented higher flux and retention on pig esophagus mucosa with a shorter lag time, when compared to B20. BZC flux was strongly correlated with in vivo anesthetic efficacy, but not with topical anesthesia duration. The retention studies did not correlate with any of the in vivo efficacy parameters. Thus, in vitro permeation study can be useful to predict anesthetic efficacy during preclinical tests, because a correlation between flux and anesthetic efficacy was observed. Therefore, in vitro assays, followed by in vivo efficacy, are necessary to confirm anesthetic performance.

  13. Combined experimental and theoretical study of the benzocaine/Ar van der Waals system in supersonic expansions. (United States)

    León, Iker; Aguado, Edurne; Lesarri, Alberto; Fernández, José A; Castaño, Fernando


    The electronic spectra of Benzocaine x Ar(n), n = 0-4 were obtained using two-color resonance enhanced multiphoton ionization; the 1:1 and 1:2 clusters were investigated by ultraviolet/ultraviolet hole burning, stimulated emission pumping, and other laser spectroscopies. A single isomer was found for the 1:1 cluster, while two isomers of the 1:2 cluster were found: one with the two Ar atoms on the same side of the chromophore, and the other with the two Ar atoms sitting on opposite sides of the chromophore. The observed shifts point to the existence of a single isomer for the 1:3 and 1:4 species. Dissociation energies for the neutral ground and first excited electronic state and the ion ground electronic state of the complexes have been determined by the fragmentation threshold method and by ab initio calculations conducted at the MP2 level with 6-31++g(2d, p), 6-311++g(2d, p) and AUG-cc-pVTZ basis sets. The results are compared with those obtained for other similar systems.

  14. Locating the route of entry and binding sites of benzocaine and phenytoin in a bacterial voltage gated sodium channel. (United States)

    Martin, Lewis J; Corry, Ben


    Sodium channel blockers are used to control electrical excitability in cells as a treatment for epileptic seizures and cardiac arrhythmia, and to provide short term control of pain. Development of the next generation of drugs that can selectively target one of the nine types of voltage-gated sodium channel expressed in the body requires a much better understanding of how current channel blockers work. Here we make use of the recently determined crystal structure of the bacterial voltage gated sodium channel NavAb in molecular dynamics simulations to elucidate the position at which the sodium channel blocking drugs benzocaine and phenytoin bind to the protein as well as to understand how these drugs find their way into resting channels. We show that both drugs have two likely binding sites in the pore characterised by nonspecific, hydrophobic interactions: one just above the activation gate, and one at the entrance to the the lateral lipid filled fenestrations. Three independent methods find the same sites and all suggest that binding to the activation gate is slightly more favourable than at the fenestration. Both drugs are found to be able to pass through the fenestrations into the lipid with only small energy barriers, suggesting that this can represent the long posited hydrophobic entrance route for neutral drugs. Our simulations highlight the importance of a number of residues in directing drugs into and through the fenestration, and in forming the drug binding sites.

  15. Locating the route of entry and binding sites of benzocaine and phenytoin in a bacterial voltage gated sodium channel.

    Directory of Open Access Journals (Sweden)

    Lewis J Martin


    Full Text Available Sodium channel blockers are used to control electrical excitability in cells as a treatment for epileptic seizures and cardiac arrhythmia, and to provide short term control of pain. Development of the next generation of drugs that can selectively target one of the nine types of voltage-gated sodium channel expressed in the body requires a much better understanding of how current channel blockers work. Here we make use of the recently determined crystal structure of the bacterial voltage gated sodium channel NavAb in molecular dynamics simulations to elucidate the position at which the sodium channel blocking drugs benzocaine and phenytoin bind to the protein as well as to understand how these drugs find their way into resting channels. We show that both drugs have two likely binding sites in the pore characterised by nonspecific, hydrophobic interactions: one just above the activation gate, and one at the entrance to the the lateral lipid filled fenestrations. Three independent methods find the same sites and all suggest that binding to the activation gate is slightly more favourable than at the fenestration. Both drugs are found to be able to pass through the fenestrations into the lipid with only small energy barriers, suggesting that this can represent the long posited hydrophobic entrance route for neutral drugs. Our simulations highlight the importance of a number of residues in directing drugs into and through the fenestration, and in forming the drug binding sites.

  16. Benzocaine hydrochloride anesthesia in carp (Cyprinus carpio / Cloridrato de benzocaína na anestesia de carpas (Cyprinus carpio

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    Marco Antonio da Rocha


    Full Text Available Fish anesthesia is indicated to allow the accomplishment of several procedures such as biometry, tagging, transportation, physical examination, surgical procedures, and reproductive management. The doses of benzocaine in the carp anesthesia (Cyprinus carpio were determined, carrying through six phases with 40 fish each. The average weight of carps in each phase was of 147.45±7.99g, 173.32±9.15g, 191.26±14.05g, 269.84±19.24g, 285.25±17.97g, and 300.91±16.45g. In each phase, fish had been captured and placed in four containers each one with different concentrations of benzocaine (100, 140, 180 and 220 mg/L respectively. The induction time (IT was registered for each fish and after that the anesthetic induction biometry was performed. In each phase the minimal dose of benzocaine was calculated using the Linear Response Plateau (LRP, in a model that included dose and IT. The LRP was calculated for each phase: 125.79mg/L in 114.33s, 155.68mg/L in 115.75s, 145.33mg/L in 102.52s, 149.50mg/L in 140.53s, 166.42mg/L in 116.15s, and 158.34mg/L in 102.00s. The optimal dose was related with the weight, resulting in the equation: dose=114.230+0.158 x weight (r2=0.53. The equation shows that an increase in the weight in 1g corresponds to an increase of 0.158 mg/L in the dose of benzocaine hydrochloride for carps.A anestesia em peixes é indicada para permitir a realização de diversos procedimentos como: biometria, marcação, transporte, exame físico, procedimentos cirúrgicos e manejo reprodutivo. Determinou-se a dose de benzocaína na anestesia de carpas (Cyprinus carpio, com a realização de seis etapas com 40 peixes cada. O peso médio das carpas em cada etapa foi de 147,45±7,99g, 173,32±9,15g, 191,26±14,05g, 269,84±19,24g, 285,25±17,97g, e 300,91±16,45g. Em cada etapa, os peixes foram capturados e colocados em quatro recipientes com benzocaína nas concentrações de 100, 140, 180 e 220 mg/L respectivamente. O tempo de indução (TI foi

  17. Influence of Sex, Age and Smoking Status on Patient Comfort during Gastroscopy with Pharyngeal Anesthesia by a New Benzocaine-Tetracaine Preparation

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    André L Gelly


    Full Text Available Thirty-seven patients underwent gastroscopy under pharyngeal anaesthesia with benzocaine-tetracaine (Endospray; Axcan Pharma. Patients recorded their perception of intubation, of the rest of the procedure, of taste and of throat well-being on visual analogue scales. Throat well-being and taste scores were better for men than for women. There was a strong trend for smokers to be more intolerant to intubation than nonsmokers. There was a weak but significant correlation for younger patients to be more intolerant to intubation. This study points to age and smoking status as possible factors influencing the perception of gastroscopy under pharyngeal anesthesia.

  18. 一种新型苯佐卡因衍生物的合成%Synthesize of a novel benzocaine derivative

    Institute of Scientific and Technical Information of China (English)

    刘玉婷; 张韩利; 尹大伟


    A novel benzocaine derivative (4-formyl-4′-ethoxycarbonyldiphenylamine ) was syn-thesized by the reaction of p-fluorobenzaldehde and benzocaine .The benzocaine is synthesized from oxidization ,esterification and reduction reaction of p-nitrotoluene .The structure of the object was confirmed by IR ,1 H NMR and elemental analysis .The synthesis conditions was studied and the effect of factors such as reaction temperature and reaction time on the reac-tion system was discussed .The result indicated that the optimum condition which synthe-sized benzocaine derivative 4-formyl-4′-ethoxycarbonyldiphenylamine was in DM F ,the reac-tion temperature was 154 ℃ ,the reaction time was 12 hours ,catalyst amount was 0 .004 mol and raw material mole of ratio was :benzocaine∶p-fluorobenzaldehde=1∶1 .2 .%以对硝基甲苯为原料分别经氧化、酯化和还原合成苯佐卡因,再由苯佐卡因与对氟苯甲醛反应生成一种新型苯佐卡因衍生物(4-甲酰基-4′-乙氧羰基二苯胺),经IR、1 H NMR和元素分析测试确认了其结构,并研究了其合成条件,讨论了反应温度、反应时间等因素对反应体系的影响.结果表明,合成苯佐卡因衍生物4-甲酰基-4′-乙氧羰基二苯胺的最佳条件为:以DM F为溶剂,反应温度控制在154℃,反应时间为12 h ,催化剂用量为0.004 mol ,原料的摩尔比为:苯佐卡因∶对氟苯甲醛=1∶1.2.

  19. Benzocaine loaded solid lipid nanoparticles: Formulation design, in vitro and in vivo evaluation of local anesthetic effect. (United States)

    Basha, Mona; Abd El-Alim, Sameh Hosam; Kassem, Ahmed Alaa; El Awdan, Sally; Awad, Gamal


    The aim of the present work is the development and evaluation of solid lipid nanoparticles (SLNs) as carrier system for topical delivery of benzocaine (BZC) improving its local anesthesia aiming to produce a fast acting and long lasting topical formulation. BZC loaded SLNs were prepared using a full factorial design to study the influence of the type of polyoxyethylene sorbitan ester surfactants as well as their concentration as independent variables on the particle size, entrapment efficacy and zeta potential selected as dependent variables. Design of experiment (DOE) and the analysis of variance (ANOVA) were conducted to assess the optimization of the developed formulations. The results indicated that the fatty acid chain length of tested surfactants and their concentration had a significant effect on the studied responses. The optimized formulations were spherical in shape of mean particle diameters<350 nm with negatively charged surface <-20mV. Particles were characterized using differential scanning calorimetry and X-ray powder diffraction confirming the amorphous nature and the uniformity of drug inclusion in the lipid matrix. Optimized BZC-SLNs were incorporated into hydrogels characterized by a pseudoplastic non-Newtonian behavior. In vitro release study revealed an apparently biphasic release process with sustained release profile following Higuchi kinetics. BZC loaded SLNs hydrogels showed more potent anesthetic effect compared to BZC hydrogel evaluated using tail-flick analgesimeter, confirming significant improvement in both the intensity and duration of anesthetic effect. The above results proved that SLNs represent good candidates to encapsulate BZC improving its therapeutic efficacy for the topical treatment of pain.

  20. 复方苯佐卡因凝胶的局部毒性研究%Studies on topical toxicity of Benzocaine compound gel

    Institute of Scientific and Technical Information of China (English)

    韦宝伟; 刘布鸣; 陈力力; 刘元; 姚树汉


    Objective To evaluate the topical irritation and sensitization of Benzocaine compound gel. Methods Irritation tests of rat oral mucosa, rabbit eyes, and skin hypersensitivity tests in guinea pigs were used, in accordance with the 'Guidance for Irritation, Sensitization and Hemolytic Tests for Chemicals' by the State Food and Drug Administration. Results By application of 3 g·kg-1 to rat oral mucosa, or 0.1 g to rabbit eyes, Benzocaine compound gel exhibited no irritation or other toxicity. No sensitization was found when 0.2 g of the gel was applied to the guinea pig skin. Conclusion Benzocaine compound gel is not irritative to oral mucosa, and does not cause skin allergy.%目的 评价复方苯佐卡因凝胶的局部刺激性和致敏性.方法 依照国家食品药品监督管理局《化学药物刺激性、过敏性和溶血性研究技术指导原则》(以下简称指导原则),采用大鼠口腔黏膜刺激性实验法、兔眼刺激性实验法以及豚鼠皮肤致敏实验法.结果 复方苯佐卡因凝胶给大鼠口腔正常黏膜连续涂药3次,相当于3 g·kg-1,均无刺激和毒性反应;一次性按每只0.1g给兔眼结膜涂药,亦未出现刺激性反应;给每只豚鼠皮肤0.2g致敏接触和激发接触,均无过敏反应发生.结论 复方苯佐卡因凝胶对口腔黏膜无刺激性,对皮肤也没有致敏性.

  1. ¹H, ¹³C, ¹⁵N HMBC, and ¹⁹F NMR spectroscopic characterisation of seized flephedrone, cut with benzocaine. (United States)

    Alotaibi, Majdah R; Husbands, Stephen M; Blagbrough, Ian S


    Flephedrone (4-fluoromethcathinone, 4-FMC) was analysed using (1)H, (13)C, (15)N HMBC, and (19)F observe spectroscopy, gas chromatography-flame ionisation detection (GC-FID), and electrospray ionisation-mass spectrometry (ESI-MS). Analysis of four 4-FMC samples (from a Bristol nightclub in 2013) showed that they all contained benzocaine as the cutting agent present in different amounts from 5 to 12%. Using these methods, we successfully differentiated between flephedrone regioisomers and mephedrone in an analytical method validated for flephedrone as a substituted cathinone. The data show that these now illegal cathinone-derived stimulants (highs) are now being cut; users cannot be certain of the purity of the drug they are taking. Furthermore, there are risks from the pharmaceutically active cutting agents themselves.

  2. Benzocaína e eugenol como anestésicos para juvenis do pampo Trachinotus marginatus Benzocaine and eugenol as anaesthetics for pompano juvenile Trachinotus marginatus

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    Marcelo Hideo Okamoto


    Full Text Available O objetivo deste trabalho foi avaliar a eficácia da benzocaína e do eugenol como anestésicos para juvenis de Trachinotus marginatus. Foram testadas concentrações de 25, 50, 75, 100 e 150ppm de benzocaína e de 25, 37,5, 50, 62,5 e 75ppm de eugenol. Os testes foram realizados em aquários de vidro contendo 30l de água (salinidade 30‰ e temperatura 19°C. Os peixes (51,4±13,5g foram expostos individualmente às diferentes concentrações de cada anestésico (n=5 para cada concentração. Enquanto ainda anestesiados, eles foram medidos e pesados para posteriormente serem colocados em um aquário sem anestésico para recuperação. Posteriormente, os peixes foram colocados em um aquário sem anestésico para observação da recuperação. O tratamento estatístico dos resultados foi feito pela Análise de Variância (One-Way - ANOVA com 95% de significância e, quando encontradas diferenças significativas, o teste de Duncan foi aplicado. Os períodos para atingir a latência para os juvenis de pampos variaram entre 11min para a concentração de 25ppm e 2min na concentração de 150ppm para a benzocaína e de 10min (25ppm a 2min (75ppm para o eugenol. Os tempos de recuperação foram entre 3min para 25ppm e 14min para a concentração de 150ppm para a benzocaína e de 2min (25ppm a 8min (75ppm para o eugenol. A dose de 50ppm de benzocaína e eugenol proporcionou um período de latência e recuperação dentro da faixa considerada adequada (3mim para a latência e 5mim para a recuperação. Entretanto, é importante salientar que o custo da benzocaína para anestesiar juvenis de pampo é 1/3 inferior ao custo do eugenol.The aim of this experiment was to evaluate the efficacy of benzocaine and eugenol as anesthetics for Trachinotus marginatus juveniles. Five concentrations of benzocaine (25, 50, 75, 100, and 150ppm and eugenol (25, 37.5, 50, 62.5, and 75ppm were tested. The trials were conducted in glass aquariums filled with 30l seawater

  3. Anestesia do pirarucu por aspersão da benzocaína diretamente nas brânquias Anesthesia in pirarucu by benzocaine sprays in the gills

    Directory of Open Access Journals (Sweden)

    Alexandre Honczaryk


    Full Text Available O pirarucu (Arapaima gigas é um peixe que pode atingir mais de 2m e 100kg. No entanto, por ser um animal de grande porte, o risco de acidentes é bastante elevado durante o manejo. Logo, anestésicos são essenciais para segurança no trabalho. Nesse contexto, estudou-se a possibilidade do uso da benzocaína aspergida diretamente nas brânquias do pirarucu, para indução à anestesia do peixe pulmonado da Amazônia sem riscos de afogamento. Foram testadas as concentrações de 25, 50 e 75mg L-1 em indivíduos adultos (55,1±7,0kg e 1,80±0,1m e as concentrações de 50 e 100mg L-1 em juvenis (6,0±0,6kg e 87,2±5,6cm. Os resultados mostram viabilidade do uso da benzocaína aspergida diretamente nas brânquias do pirarucu em concentrações de 50 a 100mg L-1, proporcionando anestesia com ausência de movimentação por aproximadamente 2min, tempo suficiente para procedimentos rápidos, como biometria, injeções, marcação, coleta de raspados de muco na superfície do corpo e brânquias. Mortalidade de animais não foi observada mesmo um mês após os testes.Pirarucu (Arapaima gigas is a fish that may achieve more than 2m and 100kg. Thus handling of this fish may impose risks to workers. In this way, anesthetics are imperative for safety at work, but usual anesthetics baths are not feasible for pirarucu because of the fish size and the species pulmonary respiration. Pirarucu may die drowned if submersed as the other fishes in anesthetics baths. Therefore, this work tested the possible use of benzocaine directly sprinkled in the gills of pirarucu. In the first experiment, benzocaine solutions in concentrations of 25, 50 and 75mg L-1 were tested for adult fish (55.1±7.0kg e 1.80±0.1m. In the second one, the anesthetic in concentrations of 50 and 100mg L-1 were tested for juveniles (6.0±0.6kg e 87.2±5.6cm. Benzocaine sprinkled directly in the gills of pirarucu showed to be an efficient anesthetic both for juveniles and adult fish. It was

  4. Preparation and Formulation Optimization of Compound Benzocaine Film%复方苯佐卡因膜剂的制备及处方优化

    Institute of Scientific and Technical Information of China (English)

    陶明涛; 李人宇


    OBJECTIVE:To prepare Compound benzocaine film and optimize the formulation. METHODS:Compound benzo-caine film was prepared with the base materials of polyving akohol-1788 (PVA) and sodium carboxymethyl cellulose (CMC-Na). With the factors of amounts of the base materials PVA and CMC-Na and the additives glycerol and polysorbate 80,and the indexes of the average of the cumulative release rates (0.25 h and 2 h) of the main drugs benzocaine (BZ) and dexamethasone acetate (DA),the orthogonal experiment was conducted to optimize the formulation,and then the optimal formulation was verified. HPLC was adopted to determine the contents of BZ and DA in the preparation for the calculation of cumulative release rates. RESULTS:The optimal formulation was as follows as PVA of 1.2 g,CMC-Na of 1.2 g,glycerol of 1.6 g, polysorbate 80 of 1.5 ml. The con-tents of BZ and DA in the single film prepared respectively were 21.607 mg(RSD=0.71%,n=6)and 4.375 mg(RSD=0.55%, n=6);the average cumulative release rates were respectively 32.7%(RSD=2.01%)and 69.25%(RSD=1.43%)at 0.25 h and 2 h. CONCLUSIONS:The method of preparing the above-mentioned film with homogeneous contents is simple.%目的:制备复方苯佐卡因膜剂并优化其处方。方法:以聚乙烯醇1788(PVA)、羧甲基纤维素钠(CMC-Na)为基质,制备复方苯佐卡因膜剂。以基质PVA、CMC-Na和附加剂甘油、聚山梨酯80的用量为因素,以主药苯佐卡因(BZ)和醋酸地塞米松(DA)累积释放度(0.25、2 h)的平均值为指标,采用正交试验优选处方,并对最优处方进行验证。采用高效液相色谱法测定制剂中BZ和DA的含量,计算累积释放度。结果:最优处方为PVA 1.2 g,CMC-Na 1.2 g,甘油1.6 g,聚山梨酯801.5 ml。所制单片药膜中BZ、DA的含量分别为21.607 mg(RSD=0.71%,n=6)、4.375 mg(RSD=0.55%,n=6),0.25、2 h的平均累积释放度分别为32.7%(RSD=2.01%)、69.25%(RSD=1

  5. 复方苯佐卡因凝胶对试验性牙痛模型的影响%Effects of Benzocaine compound gel on experimental toothache

    Institute of Scientific and Technical Information of China (English)

    韦宝伟; 刘布鸣; 陈力力; 刘元; 姚树汉


    Objective To compare analgesic efficacy of the copied Benzocaine compound gel and its original product Orajel Mouth-Aid, an over the counter drug product made in USA. Methods Pain thresholds in dental pulp of rabbits, and in tail flick of rat model were used. Results By topical application, these two products exhibited dose-dependent analgesic actions in rabbits and rats. Conclusion These two products have analgesic efficacy with similar potency, and they are good for toothache.%目的 对比仿制药复方苯佐卡因凝胶与其被仿制品Orajel Mouth-Aid (OMA)的镇痛作用.方法 采用电刺激家兔牙髓法和光电刺激大鼠尾巴法.结果 局部给药后,复方苯佐卡因凝胶和OMA均能提高动物痛阈,有良好的镇痛作用且具有剂量依赖性.结论 复方苯佐卡因凝胶和OMA均有镇痛作用且作用强度相当,可用于牙痛的治疗.

  6. Determination of Benzocaine in Condom by HPLC%高效液相色谱法测定避孕套中苯佐卡因的含量

    Institute of Scientific and Technical Information of China (English)

    母瑞红; 柯林楠; 周红娇


    目的:采用高效液相色谱法(HPLC)测定避孕套中苯佐卡因(benzocaine)的含量.材料与方法:采用Polaris C18-A(5μm 250×4.6mm)色谱柱,用乙腈-水60:40作为流动相,检测波长为265nm,流速:1.0ml*min-1,进样量10μl.结果:苯佐卡因在98.5μg/ml~492.5μg/ml范围内呈良好的线性关系(相关系数R2=0.9998),精密度(RSD)0.7%,平均回收率为102.4%.结论:该方法操作简便可行,适用于含苯佐卡因避孕套中苯佐卡因含量的质量控制.

  7. Molecularly imprinted microspheres synthesized by a simple, fast, and universal suspension polymerization for selective extraction of the topical anesthetic benzocaine in human serum and fish tissues. (United States)

    Sun, Hui; Lai, Jia-Ping; Chen, Fang; Zhu, De-Rong


    A simple, fast, and universal suspension polymerization method was used to synthesize the molecularly imprinted microspheres (MIMs) for the topical anesthetic benzocaine (BZC). The desired diameter (10-20 μm) and uniform morphology of the MIMs were obtained easily by changing one or more of the synthesis conditions, including type and amount of surfactant, stirring rate, and ratio of organic to water phase. The MIMs obtained were used as a molecular-imprinting solid-phase-extraction (MISPE) material for extraction of BZC in human serum and fish tissues. The MISPE results revealed that the BZC in these biosamples could be enriched effectively after the MISPE operation. The recoveries of BZC on MIMs cartridges were higher than 90% (n = 3). Finally, an MISPE-HPLC method with UV detection was developed for highly selective extraction and fast detection of trace BZC in human serum and fish tissues. The developed method could also be used for the enrichment and detection of BZC in other complex biosamples.

  8. Efficacy of Benzocaine 20% Topical Anesthetic Compared to Placebo Prior to Administration of Local Anesthesia in the Oral Cavity: A Randomized Controlled Trial. (United States)

    de Freiras, Guilherme Camponogara; Pozzobon, Roselaine Terezinha; Blaya, Diego Segatto; Moreira, Carlos Heitor


    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.

  9. Anesthetic Effect of Benzocaine in Simulated Transport of Juvenile Oreochromis niloticus%对氨基苯甲酸乙酯在罗非鱼幼鱼模拟运输中的麻醉效果

    Institute of Scientific and Technical Information of China (English)

    汤保贵; 戴东辉; 张健东; 陈刚; 施钢; 黄建盛; 周晖; 潘传豪; 王忠良


    为对氨基苯甲酸乙酯在罗非鱼运输中的应用提供理论依据,分别用5 mg/L、10 mg/L和15 mg/L4个浓度梯度的对氨基苯甲酸乙酯进行罗非鱼幼鱼处理,在密封式塑料袋中模拟罗非鱼幼鱼麻醉运输过程,并测定各时段的平均耗氧率与排氨率,以测试其麻醉运输效果.结果表明:在0~7 h内,对氨基苯甲酸乙酯麻醉能显著降低罗非鱼的耗氧率与排氨率,其中15 mg/L的对氨基苯甲酸乙酯适宜于吉富品系罗非鱼幼鱼运输.%In order to provide a theoretical basis for applying benzocaine in transporting tilapia, the juvenile tilapia were treated with benzocaine in four gradient concentrations to simulate the transport,and the oxygen consumption rate and ammonia excretion rate of each period were measured to evaluate the effect of anesthesia. The results showed that the oxygen consumption rate and ammonia excretion rate were both significantly decreased in 0~7 hours, and 15 mg/L benzocaine was suitable for juvenile tilapia transport.

  10. Single-crystal diffuse scattering studies on polymorphs of molecular crystals. I. The room-temperature polymorphs of the drug benzocaine. (United States)

    Chan, E J; Welberry, T R; Goossens, D J; Heerdegen, A P; Beasley, A G; Chupas, P J


    The drug benzocaine (ethyl 4-aminobenzoate), commonly used as a local anaesthetic, is a bimorphic solid at room temperature. Form (I) is monoclinic P2(1)/c, while the metastable form (II) is orthorhombic P2(1)2(1)2(1). Three-dimensional diffuse X-ray scattering data have been collected for the two forms on the 11-ID-B beamline at the Advanced Photon Source (APS). Both forms show strong and highly structured diffuse scattering. The data have been interpreted and analysed using Monte Carlo (MC) modelling on the basis that the scattering is purely thermal in origin and indicates the presence of highly correlated molecular motions. In both forms (I) and (II) broad diffuse streaks are observed in the 0kl section which indicate strong longitudinal displacement correlations between molecules in the 031 directions, extending over distances of up to 50 A. Streaks extending between Bragg peaks in the hk0 section normal to [100] correspond to correlated motions of chains of molecules extending along a that are linked by N-H...O=C hydrogen bonds and which occur together as coplanar ribbon pairs. The main difference between the two forms is in the dynamical behaviour of the ribbon pairs and in particular how they are able to slide relative to each other. While for form (I) a model involving harmonic springs is able to describe the motion satisfactorily, as simple excursions away from the average structure, there is evidence in form (II) of anharmonic effects that are precursors of a phase transition to a new low-temperature phase, form (III), that was subsequently found.

  11. Mentol e eugenol como substitutos da benzocaína na indução anestésica de juvenis de pacu = Menthol and eugenol as benzocaine substitutes in anesthetic induction of pacu juveniles

    Directory of Open Access Journals (Sweden)

    André Fernando Nascimento Gonçalves


    Full Text Available Objetivou-se verificar a eficiência de anestésicos naturais na indução à anestesia de juvenis de pacu. Foram avaliadas quatro concentrações de mentol (50, 100, 150 e 200 mg L-1, quatro de eugenol (10, 25, 50 e 100 mg L-1 e uma de benzocaína (100 mg L-1. Durante o procedimento de anestesia, foram monitorados e avaliados quatro estágios de sedação, da redução dos movimentos operculares até a perda total de reação à manipulação. Após o procedimento de biometria, foram avaliados o tempo de recuperação e a mortalidade até48h após anestesia. As concentrações de 100, 150 e 200 mg L-1 de mentol e as concentrações de 50 e 100 mg L-1 de eugenol apresentaram tempos de indução à anestesia e recuperação similares aos da benzocaína. Os resultados obtidos mostraram que o mentol e o eugenol são anestésicos eficientes para pacus em substituição à benzocaína, sugerindo a concentração de 100 mg L-1 de mentol e 50 mg L-1 de eugenol.This study aimed to verify the efficacy of natural anestheticinduction of pacu juveniles. Were evaluated four menthol (50, 100, 150 and 200 mg L-1, four eugenol (10, 25, 50 and 100 mg L-1 and one benzocaine (100 mg L-1 concentrations. During the anesthetic procedure, four sedative stages were monitored and evaluated until no reaction of the fish to handling was registered. After performingbiometric evaluation on the anesthetized fish, were recorded the recovery time and mortality rate up to 48 hours after the anesthetic experiments. Concentrations of 100, 150 and 200 mg L-1 of menthol, 50 and 100 mg L-1 of eugenol showed anesthetic induction timeand recovery time similar to that of benzocaine. The obtained results showed that menthol and eugenol are efficient anesthetics for pacu juveniles in substitution of benzocaine, suggesting the concentration of 100 mg L-1 of menthol and 50 mg L-1 of eugenol.

  12. 气相色谱-质谱联用法测定乳液化妆品中的苯唑卡因%Determination of benzocaine in daily chemical products by gas chromatography-mass spectrometry

    Institute of Scientific and Technical Information of China (English)

    田玉平; 顾玲玲


    This paper established the method of analysing benzocaine by gas chromatography-mass spectrometry. Linearity of the calibration curve was in the range of 0.2- 8.0 μg · mL-1(r = 0.995), the detection limit was 0.06 mg · L-1, and the recovery was 90.7%,RSD 4.2%(n= 9).%建立了气相色谱-质谱联用仪分析乳液化妆品中苯唑卡因的方法,线性范围0.2~8.0 mg · L-1(r=0.995),方法检测限0.06 mg · L-1(S/N>3),1.0 mg · L-1的加标回收率90.7%(n=6)。

  13. 复方苯佐卡因凝胶治疗豚鼠口腔溃疡的实验研究%Effects of Benzocaine compound gel on oral canker sore in guinea pigs

    Institute of Scientific and Technical Information of China (English)

    韦宝伟; 刘布鸣; 陈力力; 刘元; 姚树汉


    Objective: To compare the effects of benzocaine compound gel ( Gel) and its original product " Orajel? Mouth-Aid " ( OMA ) in the treatment of oral canker sore in guinea pigs. Methods: Oral canker sore models were induced by acetic acid, slaphylo-coccus epidermidis and Candida alhicans respectively in guinea pigs. The canker sore was treated by Gel and OMA at various dosed respectively. The treatment effects were analysed by the canker sore area change before and after treatment. Results; Cel and OMA showed similar effectiveness and dose-dependent effects in the treatment of canker sore in guinea pigs. Conclusion; Benzocain gel and OMA are effective in promoting the healing of oral canker sore.%目的:对比仿制药复方苯佐卡因凝胶(以下简称凝胶)与其被仿品(美国非处方药品“Orajel(R)Mouth-Aid,OMA)”对实验性口腔溃疡治疗作用.方法:采用醋酸、细菌或真菌诱发豚鼠口腔溃疡模型观察药物抗口腔溃疡作用.结果:局部给药,凝胶和OMA均能显著促进醋酸、细菌或真菌诱发的豚鼠口腔溃疡愈合,均具有剂量依赖性.结论:凝腔和OMA均具有促进口腔溃疡愈合作用,耐药作片强度相当.

  14. Influência da concentração de benzocaína e do comprimento dos peixes na anestesia e na recuperação de tilápias-do-nilo Effect of benzocaine concentration and fish size on anesthesia and recovery in Nile tilapia

    Directory of Open Access Journals (Sweden)

    Daniel Okamura


    Full Text Available Com o objetivo de avaliar a influência da concentração de benzocaína na indução e recuperação da anestesia em tilápias-do-nilo (Oreochromis niloticus de diferentes comprimentos, desenvolveu-se um experimento em blocos casualizados, em esquema fatorial 4 × 4, composto de quatro comprimentos de peixes (6; 10; 14 e 18 cm de comprimento total e quatro concentrações de benzocaína (60; 120; 180 e 240 mg por litro de água. A indução e a recuperação da anestesia foram divididas em três estágios, de acordo com o comportamento dos peixes sob efeito do anestésico, registrando-se o tempo de permanência em cada estágio. As diferenças de comprimento não influenciaram de forma significativa os tempos de anestesia e recuperação. Regressões lineares com plateau foram geradas para estimar o ponto em que o aumento da dose deixou de ter efeito. Durante a indução à anestesia, o plateau ocorreu na concentração de 132 mg/L e o tempo estimado para atingir a sedação total (estágio 3 foi de 86 segundos. Para permanência do peixe sob sedação total, é necessária concentração de benzocaína de 190 mg/L e o tempo estimado de permanência neste estágio é de 91,1 segundos. Concentrações superiores a 190 mg de benzocaína por litro de água não produzem efeitos que justifiquem seu emprego.To evaluate the influence of benzocaine concentration on the induction and recovery from anesthesia in different sized Nile tilapia (Oreochromis niloticus, it was developed a random block experiment design in 4 × 4 factorial consisted of four fish lengths (6; 10; 14 and 18 cm total lenght and four benzocaine concentrations (60; 120; 180 and 240 mg of benzocaine per liter of water. The induction and the recovery from anesthesia were divided in three stages based on the behavior of the fishes under anesthetic effect. The time spent in each stage was recorded. Differences in length did not affect significantly the anesthesia and recovery time

  15. HPLC-MS/MS determination of illegal drug benzocaine added in weight-loss functional foods%高效液相色谱-串联质谱法测定减肥保健食品中非法添加药物苯佐卡因

    Institute of Scientific and Technical Information of China (English)

    马微; 代汉慧; 张英春; 陈冬东; 王海波; 柳彩云; 王秀君; 唐英章


    建立了测定减肥保健食品中非法添加药物笨佐卡因的高效液相色谱-串联质谱分析方法.减肥咖啡、减肥茶、减肥胶囊、减肥片刺、减肥饼干等不同类型的减肥保健食品经超声萃取后,以Waters Atlantis T3柱(150mm×2.1mm,3μm)分离后,采用多反应监测(MRM)正离子模式检测,定性离子对为m/z166与m/z138和m/z166与m/z94,采用m/z166与m/z138进行定量.实验结果表明,苯佐卡因在0.01~50μg/L的范围内呈良好的线性关系,相关系数为0.9985,在低、中、高的3个添加水平范围内的平均回收率为69.3%~95.6%.同时研究了苯佐卡因的电喷雾电离质谱特征,推测其裂解途径.本方法灵敏度高,操作简便,可用于不同减肥保健食品中非法添加苯佐卡因的检测.%A comprehensive analytical method based on high performance liquid chromatography tandem mass spectrometry was developed for the determination of benzocaine.Various weight-loss functional foods, including weight-loss coffee, tea, capsule, tablet and biscuit were extracted under ultrasonication and were separated on Waters Atlantis T3 ( 150mm × 2.1 mm, 3μm) column.Benzocaine was detected by MS/MS technique using positive electrospray ionization and multiple reaction monitoring (MRM) mode, and employing two precursor- product ion pairs: m/z166 and m/z 138, m/z166 and m/z 94, as qualitative ion pairs, m/z1 66 and m/z 138 as quantification ion pairs.The results showed that the calibration curve showed good linearity for benzocaine in the ranges of 0.01~50μg/L,and the correlative coefficient was 0.9985.The mean recoveries at the three spiked levels (low, middle,high)were 69.3%~95.6%.The mass spectrum characterization of benzocaine and speculated on fragmentation pathways were also studied.The method is sensitive, simple and adapt to the determination of benzocaine in the different weight-loss functional foods.

  16. Mentol e eugenol como substitutos da benzocaína na indução anestésica de juvenis de pacu - DOI: 10.4025/actascianimsci.v30i3.1081 Eugenol and menthol as benzocaine substitutes in anaesthesic induction of pacu juveniles - DOI: 10.4025/actascianimsci.v30i3.1081

    Directory of Open Access Journals (Sweden)

    João Batista Kochenborger Fernandes


    Full Text Available Objetivou-se verificar a eficiência de anestésicos naturais na indução à anestesia de juvenis de pacu. Foram avaliadas quatro concentrações de mentol (50, 100, 150 e 200 mg L-1, quatro de eugenol (10, 25, 50 e 100 mg L-1 e uma de benzocaína (100 mg L-1. Durante o procedimento de anestesia, foram monitorados e avaliados quatro estágios de sedação, da redução dos movimentos operculares até a perda total de reação à manipulação. Após o procedimento de biometria, foram avaliados o tempo de recuperação e a mortalidade até 48h após anestesia. As concentrações de 100, 150 e 200 mg L-1 de mentol e as concentrações de 50 e 100 mg L-1 de eugenol apresentaram tempos de indução à anestesia e recuperação similares aos da benzocaína. Os resultados obtidos mostraram que o mentol e o eugenol são anestésicos eficientes para pacus em substituição à benzocaína, sugerindo a concentração de 100 mg L-1 de mentol e 50 mg L-1 de eugenol.Anaesthetics represents important tool for management procedures in aquaculture. This study aimed to verify the efficacy of natural anaesthesic induction of pacu juvenile. Were evaluated four menthol concentrations (50, 100, 150 and 200 mg L-1, four eugenol (10, 25, 50 and 100 mg L-1 and one of benzocaine (100 mg L-1. During the anaesthesic procedure were monitored and evaluated four sedative stages, until no reaction to handling. After biometric was evaluated recovery time and mortality 48 hours after anaesthesia. Concentrations 100, 150 and 200 mg L-1 of menthol, 50 and 100 mg L-1 of eugenol showed anaesthesic induction time and recovery time similar of benzocaine. The obtained results showed that menthol is an efficient anaesthesic for pacu juvenile in substitution of benzocaine, suggesting the concentration of 100 mg L-1 of menthol and 50 mg L-1 of eugenol.

  17. Determination of the optimal dose of benzocaine hydrochloride in anesthesia of tilápia (Oreochromis niloticusDeterminação da dose ótima de cloridrato de benzocaína na anestesia de tilápias (Oreochromis niloticus

    Directory of Open Access Journals (Sweden)

    Marco Antonio da Rocha


    Full Text Available Fish anesthesia is indicated for several management procedures such as capturing, biometry, tagging, transporting, physical examination, reproductive management and surgical procedures. In this study the dose of benzocaine hydrochloride necessary for tilápia (Oreochromis niloticus anesthesia was determined through six phases with 240 fish. In each phase 40 fish were evaluated. The interval between phases was two months. Mean values for weight and (allometric condition factor, in each phase, were 25.64 (2.56, 167.58 (2.88, 286.12 (2.57, 388.24 (2.50, 518.19 (2.89, 592.71 (2.67, respectively. The values for allometric condition factors showed that the animals included in the experiments were in good body conditions (P > 0.05. In each phase, fishes were captured and kept in four containers with five liters of water and benzocaine hydrochloride diluted in 20 mL of ethanol, in concentrations of 100, 140, 180, and 220 mg/liter of water. The time of induction in seconds (TI was registered for each fish, and after the anesthetic induction the biometric analysis was conducted at fixed time of 10 minutes. After, the fishes were transferred to containers with 20 liters of water under constant flow, in order to evaluate the recovering time in seconds (TR. At each phase the minimum dose of benzocaine hydrochloride concentration was calculated using LRP (Linear Response Plateau. The model included the dose of benzocaine (mg/L and the time of induction in seconds. The values of LRP were, respectively, 146.60 and 67.45, 155.95 and 76.33, 160.45 and 87.42, 167.00 and 108.14, 165.87 and 174.03, 164.00 and 139.80. The optimum dose was related to the mean weight in each phase, resulting in the equation: Dose = 149.65 + 0.03183 x weigh (r2 = 0.73. This equation showed that an increase of 1g in the body weight corresponded to an increase of 0.032 mg/L in the dose of benzocaine hydrochloride.A anestesia em peixes é indicada para auxiliar a realização de diversos

  18. Anaesthesia effect of two anaesthetic chemicals, 2-phenoxyethanol and benzocaine, on the winged pearl oyster (Pteria penguin (Roiding))%苯佐卡因和乙二醇苯醚对企鹅珍珠贝麻醉效果的研究

    Institute of Scientific and Technical Information of China (English)

    万正平; 王梅芳; 李双波; 余祥勇


    为了寻找企鹅珍珠贝Pteria penguin(Rtiding)植核时安全与有效的麻醉方法,本实验比较了乙二醇苯醚和苯佐卡因对企鹅珍珠贝植核时的麻醉效果。结果表明,海水温度在25℃时,φ=0.1%,0.2%,0.3%的乙二醇苯醚与P=500,800,1000mg·L-1的苯佐卡因都有麻醉效果;随着麻醉剂用量的增加,企鹅珍珠贝麻醉所需时间减少,复苏时间变长;在一定剂量下,随水温的上升(21—27℃),麻醉和复苏时间均减少;妒:0.2%的乙二醇苯醚、P=800mg·L-1和1000mg·L-1的苯佐卡因对企鹅珍珠贝均具有较好的麻醉效果,30min内的麻醉效果均达到100%,麻醉贝复苏快,且1周后均存活。%Anaesthetics, as a means of reducing stress reaction, may have a role in the pearl seeding process. Anaesthetic chemicals were identified to facilitate the safe and effective anesthetization of wing pearl oysters ( Pteria penguin (Rtiding) ) in seeding. Two anaesthetic chemicals, 2-phenoxyethanol and henzocaine, were assessed for their ability to relax the wing pearl oyster. These reagents of different concentrations were added into containers of the oysters to observe their reactions at the temperatures ranging from 21,23, 25 and 27 ℃. At 25 ℃ 2-phenoxyethanol of 0.1% -0. 3% (v/v) and benzocaine of 500, 800, 1 000 mg·L-1 appeared promising. And 2-phenoxyethanol and benzocaine were selected to determine their effects on the time to relaxation and to recovery and on survival of the oysters after 7 days of relaxation. It was found that as anesthetic concentrations of the reagents increased, the time to relaxation of the oysters decreased while the time to recovery tended to increase. Increased duration of exposure to the relaxants increased the time to recovery. When the temperature increased both the time to relaxation and to recovery of the oysters decreased. The highest proportion of the relaxed oysters ( 100%

  19. Application of Pd/C-HCOONH4 Reductive System in the Synthesis of Benzocaine and its Analogues%Pd/C-HCOONH4还原体系在苯佐卡因及类似物合成中的应用

    Institute of Scientific and Technical Information of China (English)

    张莉; 金小平; 高浩其; 房江华; 李瑞丰; 方烨汶


    The catalytic transfer hydrogenation of ethyl p-nitrobenzoate to ethyl 4-aminobenzoate is studied at room temperature with ammonium format as the hydrogen donor and ethanol as the solvent using Pd/C as catalyst. Under the same catalytic condition, the analogs of benzocaine is also synthesized in high yields. The present catalytic transfer hydrogenation reaction can be made under mild reactions conditions with high catalytic reactivity and also shows a great scale-up prospect.%以对硝基苯甲酸乙酯为原料, Pd/C为催化剂,甲酸铵为供氢体,乙醇为溶剂,对在室温下反应得到对氨基苯甲酸乙酯的催化转移氢化反应进行了研究。在相同的催化体系下,本佐卡因的类似物也得以高效合成。该催化转移氢化反应除温和的反应条件和高催化活性外,还兼具良好的放大前景。

  20. Cloreto de sódio, benzocaína e óleo de cravo-da-índia na água de transporte de tilápia-do-nilo Sodium chloride, benzocaine and clove oil in tilapia transport water

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    José Ricardo Oliveira


    Full Text Available Testou-se a ação de diferentes concentrações de cloreto de sódio, benzocaína e óleo de cravo-da-índia na sobrevivência de alevinos e juvenis de tilápia (Oreochromis niloticus, linhagem chitralada, por 5 horas visando ao transporte. Utilizaram-se 1.350 alevinos (9,74 ± 0,04 g e 6,79 ± 0,01 cm e 270 juvenis (29,6 ± 0,06 g e 11,52 ± 0,01. Os peixes foram mantidos em jejum por 24 horas em quatro caixas de amianto (500 L com aeração constante. Em seguida, os peixes foram distribuídos em 54 sacos plásticos, capacidade para 5 L e mantidos em soluções de: cloreto de sódio nas concentrações de (0; 4; ou 8 g/L, benzocaína (0; 20; ou 40 mg/L e óleo de cravo (0; 2; ou 5 mg/L. O delineamento foi em blocos casualizados, com três repetições, em arranjo multifatorial, com três fatores: substâncias, peixes e concentrações de cada substância em estudo. Mensuraram-se, no início, os parâmetros oxigênio dissolvido, temperatura, pH, salinidade e amônia e, ao final do experimento, a glicose dos peixes. Maiores níveis de glicose foram registrados nos juvenis mantidos na água com óleo de cravo e cloreto de sódio. Não foi observada diferença significativa na sobrevivência entre os tipos de peixes e as substâncias. Entretanto, as dosagens de cloreto de sódio e benzocaína ocasionaram diferenças significativas na taxa de sobrevivência. A sobrevivência foi baixa nos alevinos com 0 g/L de cloreto de sódio e diferiu das dosagens 4 e 8 g/L. O óleo de cravo promoveu resultados similares, em todas as dosagens e substâncias, de taxas de glicose. Ao final do experimento, a sobrevivência foi satisfatória, com média geral de 97,26%, comprovando que as três substâncias podem ser usadas no transporte de alevinos e juvenis durante 5 horas. Sugere-se o cloreto de sódio por seu melhor custo-benefício.The action of different concentrations of sodium chloride, benzocaine and clove oil in the survival of fingerling and juvenile

  1. 苯佐卡因对大鼠背根神经节神经元河豚毒素不敏感型钠离子通道的影响%Effects of benzocaine on tetrodotoxin-resistant sodium channels in rat dorsal root ganglion neurons

    Institute of Scientific and Technical Information of China (English)

    章艳; 陈少锐; 贾岩岩; 刘培庆; 蒋建敏


    目的 研究苯佐卡因(BZC)对大鼠背根神经节(DRG)神经元河豚毒素不敏感型(TTX-r)钠电流的影响,探讨其镇痛作用的机制.方法 酶解法分离新生大鼠单个DRG神经元,应用全细胞膜片钳技术记录不同浓度BZC对TTX-r钠电流的影响.结果 BZC浓度依赖性静息阻断TTX-r钠电流,30、100和300 μmol·L-1的BZC分别使TTX-r钠电流峰值抑制率达(18.83 ± 8.51)%、(33.08 ± 9.19)%、(58.91 ± 12.02)%,并使TTX-r钠电流稳态失活曲线浓度依赖性向超极化方向移动.结论 BZC浓度依赖性阻断DRG神经元TTX-r钠离子通道并改变通道的失活,可能是其影响痛觉传导通路以及产生镇痛作用的机制之一.%Aim To investigate the effects of benzo-caine ( BZC ) on tetrodotoxin-resistant ( TTX-r ) Na+ currents in the rat dorsal root ganglion ( DRG ) neurons. Methods Neonatal rat DRG cells were isolated and the effects of BZC on TTX-r Na + currents were observed by whole cell patch clamp recordings. Results BZC tonically blocked the TTX-r Na+ currents con-centration-dependently, and the percentages of block by 30, 100 and 300 μnol. L-1 BZC on TTX-r Na + currents were ( 18. 83 ± 8.51 )% , ( 33.08 ± 9. 19 )% and ( 58. 91 ± 12. 02 )% respectively. Inaddition, BZC shifted the steady-state inactivation curves of TTX-r Na+ currents to the hyperpolarization direction, also in a concentration-dependent manner. Conclusion BZC may induce analgesic effect by inhibiting TTX-r Na + currents of DRG neurons and shifting steady-state inactivation curves to more negative potential values.

  2. Effects of MS-222 and Benzocaine on Electrolyte Levels of Oreochromis niloticus and Its Correlation with Content of Erythrocyte%MS-222和苯唑卡因麻醉后罗非鱼血清电解质变化及其与红细胞数的相关性

    Institute of Scientific and Technical Information of China (English)

    汤保贵; 杨思楷; 郑素碧; 倪芙镕; 周星星; 徐月容; 谢伟莹


    Nile Tilapia (Oreochromis niloticus) with body weight of (6.05 ± 1.71) g were exposed to MS-222 and benzocaine for 6 hours in 3 concentration gradients, then blood from caudal vein was abstracted, and variation of electrolyte (K+, Na+, Cl-and Ca2+) levels and its correlation with the content of erythrocyte was analyzed. The results showed that: 1) with the increase of MS-222 concentration, the level of K+ in serum decreased continuously, and Na+ concentration remained relatively stable, and Cl-concentration increased gradually, and Ca2+ concentration fluctuated, and absolute value order of correlation coefficients between inorganic ion concentration and erythrocyte amount was Cl-(0.911 6), K+(-0.551 9), Na+(0.337 5)and Ca2+(0.208 9), demonstrating a simultaneity of Cl-outflow and increasing of the amount of erythrocyte; 2) with the increase of benzocaine concentration, there was a “V” type fluctuation in serum K+ concentration, while Na+ concentrations remained relatively stable, and Cl-concentration showed a slight fluctuation, and Ca2+ concentration was in a down channel, and order of absolute value of correlation coefficients between inorganic ion concentration and erythrocyte amount was Ca2+ (0.970 1), Na+ (0.315 2), Cl-(0.265 3) and K+ (-0.049 9), demonstrating a simultaneity of erythrocyte amount decreaseand inflow of Ca2+; 3) treated with either anesthetic, the order of absolute value of correlation coefficients among concentrations of the four inorganic ions were similar, and the highest was K+-Na+, then K+-Cl-andNa+-Cl-.%分别用3个浓度梯度的MS-222和苯唑卡因对(6.05±1.71)g的尼罗罗非鱼(Oreochromis niloticus)进行6 h浸泡式麻醉,抽取尾部静脉血,研究血清中K+、Na+、Cl-、Ca2+等4种无机离子水平变化以其与红细胞数的相关性。结果表明:1)随 MS-222质量浓度的升高,血清中 K+浓度呈持续下降趋势,Na+浓度保持相对稳定,Cl-浓度逐步升高,Ca2+浓度呈现出

  3. Estresse devido ao transporte e à ação da benzocaína em parâmetros hematológicos e população de parasitas em matrinxã, Brycon cephalus (Günther, 1869 (Osteichthyes, Characidae Transport with different benzocaine concentrations and its consequences on hematological parameters and gill parasite population of matrinxã Brycon cephalus (Günther, 1869 (Osteichthyes, Characidae

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    Maurício Laterça Martins


    efeitos negativos das duas concentrações mais altas em vários parâmetros hematológicos e no número de Piscinoodinium sp. aderido às brânquias. Concluiu-se, portanto que o uso da benzocaína não reduziu o estresse causado pelo transporte em matrinxãs, atuando inclusive como agente estressor adicional.The objective of this study was to evaluate the transport stressing effects and the different benzocaine concentrations on hematological parameters and parasite population of matrinxã Brycon cephalus (Osteichthyes, Characidae. Thirty fish (1.0 kg mean weight were hauled in four 200-L plastic tanks for four hours, at different benzocaine concentrations (B0 = 0.0 g/L, B1 = 5.0 g/L, B2 = 10.0 g/L and B3 = 20 g/L. Before loading, blood and gills of 5 fish were collected. Other three samplings were performed after transport, and 24 and 96 hours later (recovery period. Blood cortisol, glucose, hematocrit, white cell differential count and the number of the gill parasite Piscinoodinium sp. were determined. Plasma cortisol increased in all treatments after transport, returning to initial levels 24 hours later. Blood glucose was also elevated after transport in all treatments, but only B0 and B1 fish recovered initial levels in 24 hours. B2 and B3 fish did not recover the initial levels until the end of the experimental period. After transport, the lymphocytes relative percentage decreased and the neuthrophils relative percentage increased, in all treatments. Ninety-six hours later, only B0 and B1 fish had recovered the initial levels of these parameters. The number of Piscinoodinium sp. on the gills of B3 fish was higher than in the other treatments 96 hours after transportation. The use of benzocaine did not mitigate stress responses and some negative effects were observed in fish transported with the highest concentrations.

  4. Synthesis and study for benzocaine%苯佐卡因的合成研究

    Institute of Scientific and Technical Information of China (English)

    马俊林; 刘栓柱



  5. 苯佐卡因合成工艺的改进%Improved synthesis of benzocaine

    Institute of Scientific and Technical Information of China (English)

    欧守珍; 陈年根; 任兆平; 符史干



  6. 苯佐卡因合成方法的改进%Improved Synthesis of Benzocaine

    Institute of Scientific and Technical Information of China (English)




  7. Reduced discomfort during high-definition transcutaneous stimulation using 6% benzocaine


    Guleyupoglu, Berkan; Febles, Nicole; Minhas, Preet; Hahn, Christoph; Bikson, Marom


    Background: High-Definition transcranial Direct Current Stimulation (HD-tDCS) allows for non-invasive neuromodulation using an array of compact (approximately 1 cm2 contact area) “High-Definition” (HD) electrodes, as compared to conventional tDCS (which uses two large pads that are approximately 35 cm2). In a previous transcutaneous study, we developed and validated designs for HD electrodes that reduce discomfort over >20 min session with 2 mA electrode current. Objective: The purpose of ...

  8. Benzocaine-Induced Methemoglobinemia Attributed to Topical Application of the Anesthetic in Several Laboratory Animal Species (United States)


    constitute a SVwere variable because of the screening nature of the danger for stressed or ill animals. Other commonly0 study and the topical route of...coefficient ically restrained by administration of a single dose of of variability < 5%.12 xylazine and ketamine, adjusted for species and weight

  9. 紫外分光光度法测定苯佐卡因软膏剂中苯佐卡因的含量%Determination of Benzocain in Benzocain Cream by UV

    Institute of Scientific and Technical Information of China (English)

    张燕; 谭会洁; 谭亚东; 孔茜



  10. Quantitative determination of benzocain in Benzocain cream by UV%紫外分光光度法测定苯佐卡因软膏中苯佐卡因的含量

    Institute of Scientific and Technical Information of China (English)

    王瑞; 张淼



  11. Study On the Improvememt of Benzocaine 'Synthesis%苯佐卡因的合成方法改进

    Institute of Scientific and Technical Information of China (English)

    彭彩云; 方渡; 李云耀


    目的 改进苯佐卡因的合成工艺.方法 评价了合成苯左卡因的主要合成路线,在较优合成路线的基础上进行了试验研究,在酯化反应阶段进行了工艺改进并优化反应条件.结果 氯化高锡是酯化反应适宜的催化剂,酯化反应收率92.6%以上;工艺改进后,氧化、酯化和还原三个阶段的总收率达80.2%以上,有较大提高.结论 实验证明工艺改进后,操作可行,总反应收率增加.

  12. 苯佐卡因合成实验的改进%Improvement of Synthesis Experiment of Benzocaine

    Institute of Scientific and Technical Information of China (English)

    秦永华; 张斌; 张雅娟; 张新波



  13. Improved Experiment for the Synthesis of Benzocaine%苯佐卡因合成实验方法的改进

    Institute of Scientific and Technical Information of China (English)

    王德平; 张复兴; 朱小明



  14. 苯佐卡因合成方法的改进%A study on the synthesizing line of Benzocaine and methods of improvement

    Institute of Scientific and Technical Information of China (English)

    张斌; 许莉勇



  15. 苯佐卡因合成方法的改进研究%Study on the Synthesizing Line of Benzocaine and Methods of Improvement

    Institute of Scientific and Technical Information of China (English)

    陈碧芬; 孙向东; 李爱元; 彭振博


    研究了以对氨基苯甲酸为原料,通过胺化和酯化反应合成苯佐卡因(对硝基苯甲酸乙酯).胺化反应中,以锡粒作为还原催化剂,产物收率为45.64%;酯化反应中固定5 g对氨基苯甲酸,添加10 mL浓硫酸,在70℃下加热回流60~80 min,以50%乙醇为溶剂,重结晶提纯产物,得产物收率为92.88%,经色谱检验,产物纯度为100%.

  16. 苯佐卡因糊剂治疗口腔溃疡的临床研究%The clinical study of benzocaine paste

    Institute of Scientific and Technical Information of China (English)

    俞未一; 梅预锋; 李振汉; 毛钊; 刘根娣



  17. 苯佐卡因的实验室合成方法研究%Study on Synthesis of Benzocaine in Laboratory

    Institute of Scientific and Technical Information of China (English)




  18. 21 CFR 310.531 - Drug products containing active ingredients offered over-the-counter (OTC) for the treatment of... (United States)


    ..., petrolatum, phenol, pine tar, rosin, rosin cerate, sassafras oil, sulfur, thymol, triclosan, and zinc oxide... product that contains benzocaine, ichthammol, sulfur, or triclosan initially introduced or...

  19. 多步骤有机合成实验教学研究——苯佐卡因的合成%Study on Experiment Teaching of Multi—step Organic Synthesis——Synthesis of Benzocaine

    Institute of Scientific and Technical Information of China (English)

    刘小玲; 彭梦侠



  20. 苯佐卡因缩芳醛席夫碱的合成及其抑菌活性%Synthesis and Bacteriostatic Activity of Benzocaine Aromatic Aldehyde Schiff Base

    Institute of Scientific and Technical Information of China (English)

    陈超; 吴校彬


    以苯佐卡因和芳醛为原料合成了3种标题化合物,用IR、1HNMR和元素分析对产物的结构进行了确证.采用滤纸片法测试了3种标题化合物对大肠杆菌、金黄色葡萄球菌及铜绿假单胞菌的抑菌性能.实验结果表明,标题化合物对所试3种细菌均有一定的抑菌活性能.其中,苯佐卡因缩水杨醛席夫碱对铜绿假单胞菌的抑菌效果最好,其抑菌圈直径达16.8 mm.

  1. 固体超强酸SO42-/ZrO2催化合成苯佐卡因%Synthesis of benzocaine catalyzed by solid superacid SO42-/ZrO2

    Institute of Scientific and Technical Information of China (English)

    刘永根; 吴良; 李海霞; 李娟; 李伟宏


    目的:探讨一种合成苯佐卡因的新方法.方法:以固体超强酸SO42-/ZrO2为催化剂,催化对氨基苯甲酸和乙醇发生酯化反应,合成苯佐卡因.结果:在固体超强酸SO42-/ZrO2催化作用下,对氨基苯甲酸和乙醇发生酯化反应生成苯佐卡因.当酯化反应反应时间为40 min,催化剂质量为对氨基苯甲酸质量的6%时,酸质量和醇体积比值为2:25时,苯佐卡因产率达91.2%.而且催化剂重复使用效果好.结论:该合成方法比传统方法具有产率高,反应平稳快速,催化剂容易分离,环境污染少等优点.

  2. Transport stress catabatic effect of anesthetic benzocaine on American shad Alosa sapidissima%苯唑卡因对美洲鲥运输应激的缓解作用研究

    Institute of Scientific and Technical Information of China (English)

    杜浩; 危起伟; 甘芳; 刘鉴毅; 杨德国; 陈细华; 张燕


    以苯唑卡因为麻醉剂,研究了人工养殖1+龄美洲鲥(Alosa sapidissima)幼鱼在有无麻醉剂作用下长途运输2 h后血清皮质醇和生化指标的变化,探索美洲鲥运输后高死亡率的原因以及麻醉剂对运输应激的缓解作用.实验对运输前、运输2 h、加20 mg/L苯唑卡因麻醉运输2 h后的美洲鲥血清中的皮质醇激素以及血液生化指标进行了比较.结果表明,运输应激对美洲鲥皮质醇和血液生理生化指标产生了显著的影响.运输2 h后美洲鲥血清皮质醇激素含量非麻醉运输组[(41.97±17.92)ng/mL,n=9]和麻醉运输组[(15.62±1.80)ng/mL,n=9]比运输前[(2.05±1.48)ng/mL,n=10]分别显著上升20倍和4倍左右(P<0.05),麻醉运输组鱼皮质醇激素显著低于非麻醉运输组(P<0.05).不加麻醉剂2 h运输应激后血清TP、AP、AKP、CHE、ALT、K+、Ca2+、GLU显著高于运输前水平(P<0.05),白蛋白与球蛋白之比AP/GP显著低于运输前水平(P<0.05),而麻醉运输组的上述指标与运输前没有显著差异.非麻醉运输组和麻醉剂组,运输后血清LDH、AST都呈不显著增加(P>0.05).实验结果显示,美洲鲥在运输应激后,心脏和肝脏等组织受到一定程度的损伤,可能是导致美洲鲥运输后较高死亡率的原因.麻醉剂苯唑卡因应用于长途运输有助于维持鱼体生化指标的稳定,对鱼体运输应激反应有很好的缓解作用.

  3. HPLC Detemination of Benzocaine, Dexamethasone Sodium Phosphate and Chlorhexidine Acetate in Pishi Cream%HPLC测定皮湿霜中苯佐卡因、地塞米松磷酸钠和醋酸氯己定含量

    Institute of Scientific and Technical Information of China (English)

    姜韧; 柯可; 刘刚; 张丽红; 薛克昌; 史宁


    目的:建立HPLC测定皮湿霜中苯佐卡因、地塞米松磷酸钠和醋酸氯己定含量的方法.方法:色谱柱:YWG C18分析色谱柱(4.6 mm×250 mm,10 μm);流动相:甲醇-水(62:37,含0.3%三乙胺,磷酸调pH 3.0);流速1 mL·min-1;检测波长240 nm.结果:苯佐卡因、地塞米松磷酸钠和醋酸氯己定的理论板数分别为5600,3500,3200;回归方程分别为:Y=1.382×107+1.550 ×107X(r=0.9998),Y=6.563×104+3.220×107X(r=0.9995),Y=-2.032×106+6.168×107X(r=0.9999);线性范围分别为6~18,0.09~0.27,0.6~1.8μg;平均回收率分别为97.6%(RSD=2.3%),96.8%(RSD=3.3%),102.4%(RSD=2.1%).结论:本法操作简便,结果准确可靠,可用于皮湿霜中苯佐卡因、地塞米松磷酸钠和醋酸氯己定的含量测定.

  4. Determination of Benzocain and Cidopirox Olamine in Compound Cidopirox Olamine Solution%HPLC法测定复方环吡酮胺溶液中有效成分的含量

    Institute of Scientific and Technical Information of China (English)

    戴博; 张华峰; 涂秀杰; 夏莹


    目的建立HPLC法同时测定复方环吡酮胺溶液中苯佐卡因和环吡酮胺两组分的含量.方法采用美国Agilent ZORBAX SB-C18色谱柱,以甲醇-乙腈-水-冰醋酸(15∶35∶50∶0.3)为流动相.检测波长为300nm,流速为1mL·min-1.结果 苯佐卡因和环吡酮胺在15min内完全分离,两者在10~120mg·L-1范围内线性关系良好,平均回收率分别为101.15%和100.70%,相对标准偏差(RSD)均小于2 %(n=9);日内精密度和日间精密度(RSD)均小于2%(n=5).结论本法准确、可靠、重复性好, 可有效控制环吡酮胺溶液的质量.

  5. 气相色谱-质谱联用法测定苯唑卡因不确定度的探讨%Discussion of the Detection Uncertainty of Benzocaine by Gas Chromatography-Mass Spectrometry

    Institute of Scientific and Technical Information of China (English)

    田玉平; 顾玲玲



  6. 荧光光谱法研究苯佐卡因与牛血清白蛋白的相互作用%Study on the interaction between benzocaine and bovine serum albumin with fluorescence spectroscopy

    Institute of Scientific and Technical Information of China (English)

    向灿辉; 王文君; 郭丹妮; 钟冬梅; 田亮


    利用荧光和紫外吸收光谱法研究了苯佐卡因与牛血清白蛋白的相互结合作用.测定了两者的结合位点数(n)和结合常数(Ka),结果分别为0.87和1.11×104 L·mo1-1,该结果表明复合物中苯佐卡因和牛血清白蛋白的结合比约为1∶1;不同温度下淬灭常数(kq)分别为1.52×1012L·mol-1 ·s-1(pH7.4,291 K)和1.39×1012 L·mol-1·s-1(pH 7.4,310 K),表明苯佐卡因与牛血清白蛋白作用过程中荧光猝灭为静态淬灭.结合同步荧光光谱分析,讨论了苯佐卡因对蛋白质构象的影响,结果表明苯佐卡因的存在对牛血清白蛋白中酪氨酸和色氨酸残基附近的微环境影响不明显.

  7. Determination of Benzocaine and Its Related Substances by RP HPLC%高效液相色谱法测定苯佐卡因含量及其有关物质

    Institute of Scientific and Technical Information of China (English)

    赵翠红; 陆巧燕; 闫莲姣; 黎瑞; 刘布鸣


    采用高效液相色谱法测定苯佐卡因的含量及其有关物质.色谱柱为ODS-BP柱(250mm×4.6mm,5μm),流动相为1.0mol/L冰醋酸溶液-甲醇(60:40),流速1.0 ml/min,检测波长290nm.苯佐卡因在5~125μg/ml浓度范围内线性良好(r=0.9999).重复性试验RSD为0.78%,苯佐卡因峰与其他峰之间的分离良好.本方法操作简单,测定快速、准确,专属性好,适用于苯佐卡因的含量及有关物质的测定.

  8. Drug: D00552 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D00552 Drug Ethyl aminobenzoate (JP16); Benzocaine (USP/INN); Parathesin (TN) C9H11...D00552 Ethyl aminobenzoate (JP16); Benzocaine (USP/INN) 2 Agents affecting individual organs 26 Epidermides ...264 Analgesics, anti-itchings, astringents, anti-inflammatory agents 2649 Others D00552 Ethyl aminobenzoate (JP16); anesthetics D00552 Ethyl aminobenzoate (JP16); Benzocaine (USP/INN) Anatomical Therapeutic Chemical (ATC...RHOIDS AND ANAL FISSURES FOR TOPICAL USE C05AD Local anesthetics C05AD03 Benzocai

  9. Aerospace Toxicology: An Overview (United States)


    convulsions, depressed heart action and respiratory rate, and possible death 70–80 Weak pulse, slow respiration, respiratory failure, and death within a...Labetalol Amitriptyline/Nortriptyline Lidocaine Amlodipine Maprotiline Atenolol Metoclopramide Atropine Metoprolol Azacyclonol Minoxidil Benzocaine

  10. Evaluation of three topical anaesthetic agents against pain : A clinical study

    Directory of Open Access Journals (Sweden)

    Nayak R


    Full Text Available AIM : To compare pain responses of children during local anaesthetic infiltration at bilateral buccal sites prepared with topical application of EMLA 5% cream, benzocaine 18% gel or lignocaine 5% ointment and also to find out the rapidity of onset of action of these agents. METHODS : 60 healthy children aged 6 to 12 years old, received bilateral buccal infiltration following application of topical anaesthetic agents applied in a double blind design. Pain responses were compared based on subject self report using visual analogue scale (VAS and operator assessment using Sound -Eye -Motor (SEM scale. RESULTS : Benzocaine gel had the rapidest onset of action. EMLA 5% cream proved to be superior in pain reduction compared to benzocaine and lignocaine. Taste acceptance was better with benzocaine gel. Further studies are required for EMLA cream with an improved formulation more suitable for mucosal application before its routine use in dentistry.

  11. Extracellular quaternary ammonium blockade of transient receptor potential vanilloid subtype 1 channels expressed in Xenopus laevis oocytes

    DEFF Research Database (Denmark)

    Rivera-Acevedo, Ricardo E; Pless, Stephan Alexander; Schwarz, Stephan K W;


    expressed in Xenopus laevis oocytes, whereas the neutral local anesthetic, benzocaine, does not, suggesting that a titratable amine is required for high-affinity inhibition. Consistent with this possibility, extracellular tetraethylammonium (TEA) and tetramethylammonium application produces potent, voltage...

  12. Varicose and other vein problems - self-care (United States)

    ... neomycin Drying lotions, such as calamine Lanolin, a natural moisturizer Benzocaine or other creams that numb the skin Watch for skin sores on your leg, especially around your ankle. Take care of sores right away to prevent infection. When ...

  13. 苯佐卡因含片治疗口腔溃疡、急性咽喉炎引起的疼痛的临床研究%The clinical study on the alleviation of pain caused by oral ulcer or acute pharyngitis :a solution using benzocaine lozenges

    Institute of Scientific and Technical Information of China (English)

    周永梅; 沈雪敏; 吴岚; 周曾同


    目的:评价苯佐卡因含片对口腔溃疡、急性咽喉炎引起的疼痛的临床疗效和安全性.方法:采用多中心、随机、双盲、对照基质平行对照试验.口腔溃疡病例数60对,咽喉炎病例数40对,观察疼痛指数及镇痛疗效.采用X2,t检验或非参数统计方法.结果:试验组用药第1 d、第2 d能有效减轻疼痛,用药第1 d镇痛维持时间长,与对照组相比有统计学意义(P<0.05),两组不良反应发生率无统计学意义(p=0.444).结论:苯佐卡因含片能有效缓解和消除口腔溃疡、急性咽喉炎引起的疼痛,且安全性好.

  14. Simultaneous determination of diclofenac sodium and benzocain in Yantongjing cream by HPLC%高效液相色谱法测定炎痛净乳膏中双氯芬酸钠和苯佐卡因的含量

    Institute of Scientific and Technical Information of China (English)

    茅志安; 姚健康; 张艳



  15. MS-222、丁香油、苯唑卡因对养殖美洲鲥幼鱼的麻醉效果%Anaesthetic effects of MS -222, clove oil and benzocaine on cultured American shad Alosa sapidissima finglings

    Institute of Scientific and Technical Information of China (English)

    杜浩; 危起伟; 杨德国; 刘鉴毅; 甘芳; 陈细华; 沈丽


    研究了MS-222、丁香油、苯唑卡因3种麻醉剂对美洲鲥Alosa sapidissima幼鱼的麻醉效果,并运用该3种麻醉剂的适宜剂量对美洲鲥幼鱼进行了运输试验.麻醉试验结果表明:在较高麻醉浓度(MS-222为75 mg/L以上,丁香油为20 mg/L以上,苯唑卡因为40 mg/L以上)下,鱼很快(30 min内)停止鳃盖张合运动,且停止鳃盖运动的鱼在空气中暴露一定时间(10 min内)后也能够复苏;在适宜的麻醉浓度(MS-222为20~30 mg/L,丁香油为8~10 mg/L;苯唑卡因为20~30 mg/L)下,鱼能够进入麻醉状态,且能保持很长时间(12 h);麻醉效果随着水温的升高而增强;在20 mg/L MS-222麻醉剂下,小规格鱼较大规格鱼更容易进入麻醉状态,而在10 mg/L丁香油和20 mg/L苯唑卡因麻醉剂下,小规格鱼却难进入麻醉状态.运输试验结果表明:麻醉运输组和对照组(非麻醉运输组)鱼血清中皮质醇的含量均显著高于基础组(运输前)(P<0.05);麻醉运输后鱼血清中皮质醇的含量虽均有一定程度的升高,但明显低于对照组,其中仅苯唑卡因麻醉运输组鱼血清中皮质醇的含量显著低于对照组(P<0.05).试验结果表明,苯唑卡因更适合用于运输美洲鲥的麻醉.

  16. Methemoglobinemia Caused by Topical Teething Preparation: A Case Report

    Directory of Open Access Journals (Sweden)

    Ran D. Balicer


    Full Text Available Methemoglobinemia (MetHb remains an uncommon, but potentially fatal disorder. Benzocaine (ethyl aminobenzoate, a topical anesthetic, has been reported to cause acquired MetHb when used during endoscopic or other ambulatory procedures. Reports of severe MetHb following benzocaine-containing preparations in the community, however, are very rare. We discuss this entity by describing an unusual case of severe MetHb in a 5-year-old child, caused by unattended self-use of a benzocaine-containing, pain-relief gel for teething. This case story illustrates the potential lethal risk of over-the-counter topical anesthetics for pediatric use. We review the risks of this potentially deadly disorder and the associated diagnostic challenges. Physicians not familiar with this rare complication may face diagnostic dilemmas, as its presentation is often nonspecific and rapid treatment is essential to prevent life-threatening complications.

  17. Marked differences in drug-induced methemoglobinemia in sheep are not due to RBC glucose-6-phosphate dehydrogenase, reduced glutathione, or methemoglobin reductase activity

    Energy Technology Data Exchange (ETDEWEB)

    Martin, D.G.; Guertler, A.T.; Lagutchik, M.S.; Woodard, C.L.; Leonard, D.A.


    Benzocaine is a commonly used topical anesthetic that is structurally similar to current candidates for cyanide prophylaxis. Benzocaine induces profound methemoglobinemia in some sheep but not others. After topical benzocaine administration certain sheep respond to form MHb (elevated MHb 16-50% after a 56-280 mg dose, a 2-10 second spray with benzocine), while other phenotypically similar sheep fail to significantly form MHb (less than a 2% increase from baseline). Deficiencies in Glucose-6-phosphate dehydrogenase (G-6-PD), reduced glutathione (GSH), and MHb reductase increase the susceptibility to methemoglobinemia in man and animals. Sheep are used as a model for G-6-PD deficiency in man, and differences in this enzyme level could cause the variable response seen in these sheep. Similarly, differences in GSH and MHb reductase could be responsible for the observed differences in MHb formation.

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

    Directory of Open Access Journals (Sweden)

    Goncharuk V.V.


    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.

  19. A study of correlations between the release of drugs from petrolatum-based gels containing nonionic surfactants and some physical and physico-chemical characteristics of the gel systems. (United States)

    Colo, G D; Nannipieri, E; Serafini, M F; Vitale, D


    Synopsis The in vitro release of benzocaine and 2-ethyIhexyl p-di-methylaminobenzoate (EH-PABA) from petrolatum-based gels either containing two nonionic surfactants, or not, was compared with some physical and/or physico-chemical characteristics of the drugs, the gels and the drug-gel systems. The surfactants had no effect on the release of EH-PABA, the less polar drug, whereas they decreased the release of benzocaine. Moreover, the release data show a complex dependence of diffusive properties of ben-zocaine on drug and surfactant concentration. Benzocaine appears to form mixed micelles with each of the two surfactants and/or undergoes self-aggregation phenomena within surfactant micelles. The results indicate that drug diffusion is influenced by gel porosity, drug molecular size and polarity and molecular interactions. Etude des corrélations entre la disponibilité des medicaments dans les gels a base de vaseline contenant des surfactifs non ioniques et quelques propriétés physiques et physicochimiques des gels.

  20. Synthesis of Two Local Anesthetics from Toluene: An Organic Multistep Synthesis in a Project-Oriented Laboratory Course (United States)

    Demare, Patricia; Regla, Ignacio


    This article describes one of the projects in the advanced undergraduate organic chemistry laboratory course concerning the synthesis of two local anesthetic drugs, prilocaine and benzocaine, with a common three-step sequence starting from toluene. Students undertake, in a several-week independent project, the multistep synthesis of a…

  1. Methemoglobinemia in postchemotherapy stomatitis topical treatment: 2 pediatric cases. (United States)

    Kaczorowska-Hac, Barbara; Stefanowicz, Joanna; Stachowicz-Stencel, Teresa; Kozlowska, Marta; Adamkiewicz-Drozynska, Elzbieta; Balcerska, Anna


    Methemoglobinemia is a rare congenital or acquired disease of increased blood methemoglobin concentration. We documented 2 cases of children suffering from neuroblastoma whose postchemotherapy anemia, leucopenia, and stomatitis were complicated by methemoglobinemia after using a formulary oral gel (7.5% benzocaine, doxycycline, nystatin, glycerin). The complication resulted in hospital treatment. Percutaneous oxygen saturation remained at 85% and 87% despite administration of 100% oxygen through a nonrebreather mask. Arterial blood gas analysis showed an oxygen saturation of 98% and 97%, respectively. Spectroscopic measurement showed methemoglobin concentration of 42% and 35.5%, respectively. After red blood cell transfusion and oral ascorbic acid in case 1 and methylene blue in case 2, the patients' condition improved. Although the benzocaine gel is not in use in several medical systems, it should be considered as a possible reason for methemoglobinemia.

  2. Synthesis of Some Streoregular Polydiacetylenes and the Slow Release of Drug Using Some Linear Polymers

    Directory of Open Access Journals (Sweden)

    *Mohammad S. Al-Ajely


    Full Text Available Some polydiacetylenes have been synthesized using UV light in topochemical polymerization technique. Some diacetylene compounds were reacted with benzocaine and procaine in an attempt to be used as biosensors in topochemical polymerization process (In vivo. The linear (Amorphous polymer was allowed to react with some commercial antibiotics and were studied as slow drug release polymers. Externally treatment of the drug containing polymers to groups of infected rabbits revealed that these polymers are effective against certain types of micro organisms.

  3. Interaction of local anesthetics with a peptide encompassing the IV/S4-S5 linker of the Na+ channel. (United States)

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


    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.

  4. Efficacy of tricaine methanesulfonate (MS-222 as an anesthetic agent for blocking sensory-motor responses in Xenopus laevis tadpoles.

    Directory of Open Access Journals (Sweden)

    Carlana Ramlochansingh

    Full Text Available Anesthetics are drugs that reversibly relieve pain, decrease body movements and suppress neuronal activity. Most drugs only cover one of these effects; for instance, analgesics relieve pain but fail to block primary fiber responses to noxious stimuli. Alternately, paralytic drugs block synaptic transmission at neuromuscular junctions, thereby effectively paralyzing skeletal muscles. Thus, both analgesics and paralytics each accomplish one effect, but fail to singularly account for all three. Tricaine methanesulfonate (MS-222 is structurally similar to benzocaine, a typical anesthetic for anamniote vertebrates, but contains a sulfate moiety rendering this drug more hydrophilic. MS-222 is used as anesthetic in poikilothermic animals such as fish and amphibians. However, it is often argued that MS-222 is only a hypnotic drug and its ability to block neural activity has been questioned. This prompted us to evaluate the potency and dynamics of MS-222-induced effects on neuronal firing of sensory and motor nerves alongside a defined motor behavior in semi-intact in vitro preparations of Xenopus laevis tadpoles. Electrophysiological recordings of extraocular motor discharge and both spontaneous and evoked mechanosensory nerve activity were measured before, during and after administration of MS-222, then compared to benzocaine and a known paralytic, pancuronium. Both MS-222 and benzocaine, but not pancuronium caused a dose-dependent, reversible blockade of extraocular motor and sensory nerve activity. These results indicate that MS-222 as benzocaine blocks the activity of both sensory and motor nerves compatible with the mechanistic action of effective anesthetics, indicating that both caine-derivates are effective as single-drug anesthetics for surgical interventions in anamniotes.

  5. Achieving pulpal anesthesia with a topical anesthetic paste

    Directory of Open Access Journals (Sweden)

    Bradley Carn


    Full Text Available Aim: The efficacy of a topically applied formulation of tetracaine base (6% was investigated against benzocaine in achieving pulpal anesthesia in a randomized, placebo-controlled, double-blind study. Materials and Methods: Subjects′ baseline pulpal responses to an electric pulp tester were measured, followed by a 10 min application of either tetracaine anesthetic paste (TAP, benzocaine (20%, or placebo. Treatments were removed and pulp testing was performed at 10 min, 15 min, and 20 min postapplication. Results: TAP produced significant pulpal anesthesia at 184% ± 7.2% above baseline versus 14% ± 1.7% above baseline for benzocaine at 15 min (P < 0.03. Differences between treatments were tested with the Wilcoxon test and the Steel-Dwass test, which is the nonparametric version of the all-pairs Tukey′s honestly significant difference test. Conclusion: Achieving profound anesthesia with a topical anesthetic paste could lead to injection less procedure, improved postsurgical incisional pain management, and ameliorate pain associated with a variety of lesions.

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

    Directory of Open Access Journals (Sweden)

    Vallurupalli S


    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

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

    Directory of Open Access Journals (Sweden)

    Fatma Gülru Erdoğan


    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

  8. Estudo do teste de Scott via técnicas espectroscópicas: um método alternativo para diferenciar cloridrato de cocaína e seus adulterantes

    Directory of Open Access Journals (Sweden)

    Vitor N. Conceição


    Full Text Available Cocaine is usually seized mixed with a wide variety of adulterants such as benzocaine, lidocaine, caffeine, and procaine. The forensic identification of cocaine in these street drug mixtures is normally performed using colorimetric testing kits, but these tests may suffer from interferences, producing false-positive results. Here, we describe the use of analytical techniques including attenuated total reflection Fourier transform infrared (ATR-FTIR and ultraviolet-visible (UV-VIS spectroscopies to distinguish between cocaine and other adulterants (lidocaine, promethazine, powdered milk and yeast that yield positive results on the Scott test using the thiocyanate cobalt reagent. A further 13 substances were also analyzed using the Scott test.

  9. Effectiveness of Two Topical Anaesthetic Agents used along with Audio Visual Aids in Paediatric Dental Patients (United States)

    Dhawan, Jayata; Kumar, Dipanshu; Anand, Ashish; Tangri, Karan


    Abstract Introduction Topical anaesthetic agents enable pain free intraoral procedures, symptomatic pain relief for toothache, superficial mucosal lesions and pain related to post extraction time. Most common anxiety provoking and fearful experience for children in dental operatory is administration of local anaesthesia because on seeing the needle, children usually become uncooperative. One of recent trend of behaviour management technique is using non-aversive techniques out of which audiovisual distraction has emerged as a very successful technique for managing children in dental settings. Audio visual distraction could decrease the procedure related anxiety of patients undergoing dental treatment and can be very relaxing for highly anxious patients. Aim The aim of the present study was to compare the efficacy of topical anaesthetics EMLA (Eutectic Mixture of Local Anaesthetics) cream and benzocaine (20%) gel in reducing the pain during the needle insertion with and without the use of Audio Visual (AV) aids. Materials and Methods The study was conducted on 120 children, the age range of 3-14 years attending the outpatient department for their treatment. EMLA and benzocaine gel (20%) were assessed for their effectiveness in reducing the pain on needle insertion during local anaesthesia administration. Based on the inclusion and the exclusion criteria, children requiring local anaesthesia for the dental treatment were randomly divided into four equal groups of 30 children based upon whether AV aids were used or not. AV aids were given using Sony Vaio laptop with earphones with nursery rhymes and cartoon movies DVD. The pain assessment was done by using the Visual Analogue Scale (VAS) scale and measurement of the physiological responses of pulse rate and oxygen saturation were done by pulse oximeter. Results There was a statistically significant difference in the mean pain score, pulse rate and mean oxygen saturation rate when it was compared between the four

  10. Crystal structure of ethyl 4-[(E-(4-hydroxy-3-methoxybenzylideneamino]benzoate: a p-hydroxy Schiff base

    Directory of Open Access Journals (Sweden)

    Jing Ling


    Full Text Available The title p-hydroxy Schiff base, C17H17NO4, was synthesized via the condensation reaction of benzocaine with vanillin. The benzylidine and benzoate rings are inclined to one another by 24.58 (8°, and the conformation about the C=N bond is E. In the crystal, molecules are linked by O—H...N hydrogen bonds, forming zigzag chains propagating along [010]. Adjacent chains are linked by C—H...π and weak offset π–π interactions [intercentroid distance = 3.819 (1 Å], forming sheets parallel to (10-2.

  11. Cosolvency and deviations from log-linear solubilization. (United States)

    Rubino, J T; Yalkowsky, S H


    The solubilities of three nonpolar drugs, phenytoin, diazepam, and benzocaine, have been measured in 14 cosolvent-water binary mixtures. The observed solubilities were examined for deviations from solubilities calculated by the equation log Sm = f log Sc + (1 - f) log Sw, where Sm is the solubility of the drug in the cosolvent-water mixture, Sc is the solubility of the drug in neat cosolvent, f is the volume fraction of cosolvent, and Sw is the solubility of the drug in water. When presented graphically, the patterns of the deviations were similar for all three drugs in mixtures of amphiprotic cosolvents (glycols, polyols, and alcohols) and water as well as nonpolar, aprotic cosolvents (dioxane, triglyme, dimethyl isosorbide) and water. The deviations were positive for phenytoin and benzocaine but negative for diazepam in mixtures of dipolar, aprotic cosolvents (dimethylsulfoxide, dimethylformamide, and dimethylacetamide) and water. The source of the deviations could not consistently be attributed to physical properties of the cosolvent-water mixtures or to alterations in the solute crystal. Similarities between the results of this study and those of previous investigations suggest that changes in the structure of the solvent play a role in the deviations from the expected solubilities.

  12. Anestésicos locais: interação com membranas de eritrócitos de sangue humano, estudada por ressonância magnética nuclear de 1H e 31P

    Directory of Open Access Journals (Sweden)

    Fraceto Leonardo Fernandes


    Full Text Available The literature carries many theories about the mechanism of action of local anesthetics (LA. We can highlight those focusing the direct effect of LA on the sodium channel protein and the ones that consider the interaction of anesthetic molecules with the lipid membrane phase. The interaction between local anesthetics and human erythrocyte membranes has been studied by ¹H and 31P nuclear magnetic resonance spectroscopy. It was found that lidocaine (LDC and benzocaine (BZC bind to the membranes, increase the mobility of the protons of the phospholipid's acyl chains, and decrease the mobility and/or change the structure of the polar head groups. The results indicate that lidocaine molecules are inserted across the polar and liquid interface of the membrane, establishing both electrostatic (charged form and hydrophobic (neutral form interactions. Benzocaine locates itself a little deeper in the bilayer, between the interfacial glycerol region and the hydrophobic core. These changes in mobility or conformation of membrane lipids could affect the Na+-channel protein insertion in the bilayer, stabilizing it in the inactivated state, thus causing anesthesia.

  13. Lidocaine alters the input resistance and evokes neural activity in crayfish sensory neurons. (United States)

    Keceli, M B; Purali, N


    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.

  14. Physiological and hematological responses of Nile tilapia (Oreochromis Niloticus to different anesthetics during simulated transport conditions

    Directory of Open Access Journals (Sweden)

    Rodrigo Diana Navarro


    Full Text Available Minimization of stress during the transportation of live fish is essential in maintaining the welfare and performance of the animals. In order to test the hypothesis that stress during transport of fingerlings of Nile tilapia (Oreochromis niloticus can be reduced with the aid of the anesthetics menthol, eugenol or benzocaine, we have assessed the effects of these agents at various concentrations on the physiological parameters and survival rates of fish subjected to conditions simulating those normally used in transportation. Fingerlings (N = 1200 were fasted for 24 hours and distributed in 20 L polyethylene bags (N = 50 per bag containing 5 L of water and an anesthetic at the appropriate concentration. Fingerlings treated with menthol at 75 mg L-1, or eugenol or benzocaine at 20 mg L-1, maintained levels of plasma cortisol and glucose that were lower than those of the stressed but untreated controls and within the physiological limits of the baseline values for this species. Under these conditions, the survival rate was 100%, suggesting that stress was substantially reduced despite dense consignment. Treatments involving higher doses of the studied agents induced significant anesthetic toxicity.

  15. Transportation of juvenile tambaqui (Colossoma macropomum in a closed system

    Directory of Open Access Journals (Sweden)

    L. C. Gomes

    Full Text Available The objective of this study was to investigate the effect of density, duration and the use of additives to the water during the transportation of juvenile tambaqui (Colossoma macropomum and use of this data to establish a safe transportation protocol for the species. The tested products and dosages were: salt (1000, 2000 and 3000 mg/L, gypsum (100, 300 and 500 mg/L and benzocaine (10, 20 and 30 mg/L. Fish were transported in closed systems (plastic bag at different densities and time periods of up to 24 h. Fish survival (FS and water quality parameters were monitored immediately after transportation. The remaining fish were kept in floating cages in order to evaluate mortality which occurred up to 96 h after transportation (S96. The best fish density, additives dosages and time period of the transportation was estimated with a general linear model. The effect of the condition factor on FS and S96 was also evaluated. As expected, FS and S96 were significantly related to time and density. FS but not S96, were also were significantly related to treatment. FS with gypsum treatment was not different from controls and FS with table salt and benzocaine treatments were significantly reduced. The condition factor was not related to either FS or S96. FS was inversely correlated with carbon dioxide concentration. It was concluded that the additives did not improve fish transportation survival. Linear models were developed to predict the best transportation densities as a function of time.

  16. Effects of local anesthetics and hemicholinium-3 on 45-Ca efflux in barnacle muscle fibers. (United States)

    Chen, S S


    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.

  17. Encapsulation altered starch digestion: toward developing starch-based delivery systems. (United States)

    Janaswamy, Srinivas


    Starch is an abundant biomaterial that forms a vital energy source for humans. Altering its digestion, e.g. increasing the proportions of slowly digestible starch (SDS) and resistant starch (RS), would revolutionize starch utility in addressing a number of health issues related to glucose absorption, glycemic index and colon health. The research reported in this article is based on my hypothesis that water channels present in the B-type starch crystalline matrix, particularly in tuber starches, can embed guest molecules such as nutraceuticals, drugs, flavor compounds and vitamins leading to altered starch digestion. Toward this goal, potato starch has been chosen as the model tuber starch, and ibuprofen, benzocaine, sulfapyridine, curcumin, thymol and ascorbic acid as model guest molecules. X-ray powder diffraction and FT-IR analyses clearly suggest the incorporation of guest molecules in the water channels of potato starch. Furthermore, the in vitro digestion profiles of complexes are intriguing with major variations occurring after 60 min of starch digestion and finally at 120 min. These changes are concomitantly reflected in the SDS and RS amounts, with about 24% decrease in SDS for benzocaine complex and 6% increase in RS for ibuprofen complex, attesting the ability of guest molecule encapsulation in modulating the digestion properties of potato starch. Overall, this research provides an elegant opportunity for the design and development of novel starch-based stable carriers that not only bestow tailored glucose release rates but could also transport health promoting and disease preventing compounds.

  18. Local anesthetics: interaction with human erythrocyte membranes as studied by {sup 1}H and {sup 31}P nuclear magnetic resonance; Anestesicos locais: interacao com membranas de eritrocitos de sangue humano, estudada por ressonancia magnetica nuclear de {sup 1}H e {sup 31}P

    Energy Technology Data Exchange (ETDEWEB)

    Fraceto, Leonardo Fernandes; Paula, Eneida de [Universidade Estadual de Campinas, SP (Brazil). Inst. de Biologia. Dept. de Bioquimica]. E-mail:


    The literature carries many theories about the mechanism of action of local anesthetics (LA). We can highlight those focusing the direct effect of LA on the sodium channel protein and the ones that consider the interaction of anesthetic molecules with the lipid membrane phase. The interaction between local anesthetics and human erythrocyte membranes has been studied by {sup 1}H and {sup 31}P nuclear magnetic resonance spectroscopy. It was found that lidocaine (LDC) and benzocaine (BZC) bind to the membranes, increase the mobility of the protons of the phospholipids acyl chains, and decrease the mobility and/or change the structure of the polar head groups. The results indicate that lidocaine molecules are inserted across the polar and liquid interface of the membrane, establishing both electrostatic (charged form) and hydrophobic (neutral form) interactions. Benzocaine locates itself a little deeper in the bilayer, between the interfacial glycerol region and the hydrophobic core. These changes in mobility or conformation of membrane lipids could affect the Na{sup +}-channel protein insertion in the bilayer, stabilizing it in the inactivated state, thus causing anesthesia. (author)

  19. Behavioral response and pain perception to computer controlled local anesthetic delivery system and cartridge syringe

    Directory of Open Access Journals (Sweden)

    T D Yogesh Kumar


    Full Text Available Aim: The present study evaluated and compared the pain perception, behavioral response, physiological parameters, and the role of topical anesthetic administration during local anesthetic administration with cartridge syringe and computer controlled local anesthetic delivery system (CCLAD. Design: A randomized controlled crossover study was carried out with 120 children aged 7-11 years. They were randomly divided into Group A: Receiving injection with CCLAD during first visit; Group B: Receiving injection with cartridge syringe during first visit. They were further subdivided into three subgroups based on the topical application used: (a 20% benzocaine; (b pressure with cotton applicator; (c no topical application. Pulse rate and blood pressure were recorded before and during injection procedure. Objective evaluation of disruptive behavior and subjective evaluation of pain were done using face legs activity cry consolability scale and modified facial image scale, respectively. The washout period between the two visits was 1-week. Results: Injections with CCLAD produced significantly lesser pain response, disruptive behavior (P < 0.001, and pulse rate (P < 0.05 when compared to cartridge syringe injections. Application of benzocaine produced lesser pain response and disruptive behavior when compared to the other two subgroups, although the result was not significant. Conclusion: Usage of techniques which enhance behavioral response in children like injections with CCLAD can be considered as a possible step toward achieving a pain-free pediatric dental practice.

  20. Effect of two anesthetics on oxygen-carrying related hematological parameters of Oreochromis niloticus%两种麻醉剂对罗非鱼携氧相关血液指标的影响

    Institute of Scientific and Technical Information of China (English)

    汤保贵; 杨思楷; 郑素碧; 倪芙镕; 周星星; 徐月容; 谢伟莹


    Oreochromis niloticus with body weight of (6.0500 ±1.7103 ) g was exposed to MS-222 and benzocaine for 6 hrs in 3 concentration gradients ( with water temperature of 30.7~32.3 ℃) , and blood from caudal vein was abstracted to determine the hematological parameters .The results showed that , the erythrocyte count ( Er) increased while exposed to MS-222 in high concentrations (25 mg/L and 40 mg/L), however, decreased dramatically while exposed to benzocaine . The mean corpuscular hemoglobin contents ( MCH) of fish exposed to anesthetics did not changed significantly comparing with the control group, so did the hemoglobin concentration (Hb) of fish exposed to MS-222.However, benzocaine gen-erated marked drop in Hb , furthermore, the drop became greater with the increasing of the anesthetic concentration .%分别用3个浓度梯度的MS-222和苯唑卡因对尼罗罗非鱼(Oreochromis niloticus)(6.0500±1.7103) g进行6 h浸泡式麻醉(水温30.7~32.3℃),然后抽取尾部静脉血,测定血液生理生化指标。重点分析了与生物携氧功能密切相关的6个指标的变化,结果显示:(1)较高浓度(25 mg/L、40 mg/L) MS-222导致红细胞数目( Er)升高,而苯唑卡因导致该值大幅下降;(2)两种麻醉剂对红细胞平均血红蛋白含量(MCH)都无显著影响,且MS-222处理后,血液的血红蛋白浓度( Hb)也无明显变化,但经苯唑卡因麻醉处理后, Hb显著下降,且降幅随药物浓度升高而显著增大。

  1. Anesthetic Method of Gobiocypris rarus%稀有鮈鲫麻醉方法研究

    Institute of Scientific and Technical Information of China (English)

    乔晔; 胡睿; 王剑伟


    在室养条件下观察了MS-222、苯佐卡因和乌拉坦对稀有鮈鲫(Gobiocypris rarus)的麻醉效果。结果表明,乌拉坦不宜作为稀有鮈鲫的麻醉剂,而一定浓度的MS-222或苯佐卡因可导致稀有鮈鲫的快速麻醉;不同麻醉剂浓度、不同的作用时间下,稀有鮈鲫在行为上呈现不同的反应,据此可分为轻度镇静、深度镇静、轻度麻醉、中度麻醉、深度麻醉和髓质麻醉阶段;根据反应时间、恢复时间、维持时间和存活率等,建议使用60mg/L的苯佐卡因或100~110mg/L的MS-222作为深度麻醉剂量。%As a new experimental fish,Gobiocypris rarus has been wildly used in scientific studies in China since 1990.In this study,narcosis effects of MS-222,Urethan and Benzocaine on Gobiocypris rarus were observed to provide anaesthetic method for the laboratory animal.The results showed that MS-222 and Benzocaine were effective to rapidly anaesthetize for Gobiocypris rarus,whereas Urethan was disable.Sequential effects on behavior were observed when the fish exposed to different concentrations of anesthetics at different times.Based on their behaviors,low-grade sedation,deep sedation,low-grade anesthesia,medium anesthesia,deep anesthesia and medullary anesthesia stages were determined.Considering the effect time,recovery time,maintain time and survival rate,60 mg/L of Benzocaine and 100-110 mg/L of MS-222 were suggested as the suitable dosage for deep anesthesia.

  2. Topical anesthesia

    Directory of Open Access Journals (Sweden)

    Mritunjay Kumar


    Full Text Available Topical anesthetics are being widely used in numerous medical and surgical sub-specialties such as anesthesia, ophthalmology, otorhinolaryngology, dentistry, urology, and aesthetic surgery. They cause superficial loss of pain sensation after direct application. Their delivery and effectiveness can be enhanced by using free bases; by increasing the drug concentration, lowering the melting point; by using physical and chemical permeation enhancers and lipid delivery vesicles. Various topical anesthetic agents available for use are eutectic mixture of local anesthetics, ELA-max, lidocaine, epinephrine, tetracaine, bupivanor, 4% tetracaine, benzocaine, proparacaine, Betacaine-LA, topicaine, lidoderm, S-caine patch™ and local anesthetic peel. While using them, careful attention must be paid to their pharmacology, area and duration of application, age and weight of the patients and possible side-effects.

  3. Crystal structure of ethyl 4-[(E)-(4-hy­droxy-3-meth­oxy­benzyl­idene)amino]­benzoate: a p-hy­droxy Schiff base (United States)

    Ling, Jing; Kavuru, Padmini; Wojtas, Lukasz; Chadwick, Keith


    The title p-hy­droxy Schiff base, C17H17NO4, was synthesized via the condensation reaction of benzocaine with vanillin. The benzyl­idine and benzoate rings are inclined to one another by 24.58 (8)°, and the conformation about the C=N bond is E. In the crystal, mol­ecules are linked by O—H⋯N hydrogen bonds, forming zigzag chains propagating along [010]. Adjacent chains are linked by C—H⋯π and weak offset π–π inter­actions [inter­centroid distance = 3.819 (1) Å], forming sheets parallel to (10-2). PMID:27555938

  4. Effectiveness of topical anesthetics on reducing tactile sensitivity in the paws of newborn rats. (United States)

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


    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.

  5. 1-芳基-2-吡咯烷酮衍生物的合成研究%Study on the Synthesis of 1-Aryl-2-pyrrolidinone Derivatives

    Institute of Scientific and Technical Information of China (English)

    赵军; 王德传; 曹燕


    1-芳基-2-吡咯烷酮衍生物是重要的有机合成中间体.以苯佐卡因为原料,经溴代、缩合、环合合成了目标产物,产物总收率达72.25%.其结构经1H NMR,MS进行了确证.该方法具有操作简便、成本低、收率高等优点.%1-Aryl-2-pyrrolidinone derivatives are important intermediates for organic synthesis. A novel process was developed for the synthesis of the title compound in an overall yield of 72.2% starting from benzocaine via bromination,nucleophilic substitution and cyclization. The structure of the target compound was confirmed with 1H NMR and MS. This method shows advantages of easy operation,low cost and high yield.

  6. UV light induced surface modification of HDPE films with bioactive compounds

    Energy Technology Data Exchange (ETDEWEB)

    Daniloska, Vesna; Blazevska-Gilev, Jadranka; Dimova, Vesna [Faculty of Technology and Metallurgy, University St. Cyril and Methodius, Ruger Boskovic 16, 1000 Skopje (Macedonia, The Former Yugoslav Republic of); Fajgar, Radek [Institute of Chemical Process Fundamentals, ASCR, Rozvojova 135, Prague 6-Suchdol (Czech Republic); Tomovska, Radmila, E-mail: [Institute for Polymer Materials, POLYMAT, Centro Joxe Mari Korta, University of the Basque Country, P.O. Box 1072, 20080 Donostia-San Sebastian (Spain); IKERBASQUE, Basque Foundation for Science, 48011 Bilbao (Spain)


    The development of different techniques for surface modification of polymers becomes popular in a last decade. These techniques preserve useful bulk polymer properties unchanged, while the activation of the polymer surface offers more possibilities for polymer applications. In this work, a new, one-step method for bio-activation of HDPE (high density polyethylene) surface by UV irradiation is presented. HDPE films coupled with selected active compound and a photoinitiator was treated by UV lamp, emitting light at 254 nm. For surface functionalization of HDPE films, the following compounds were employed: 2-aminopyridine (AP), N{sup 1}-(2-pyridylaminomethyl)-1,2,4-triazole (TA) and benzocaine (BC). The influence of irradiation time on the extent of surface changes was investigated. The modified polymer surfaces were investigated by Fourier transformed infrared (FTIR) and Raman spectroscopy, scanning electron microscopy (SEM) and contact angle measurements, demonstrating successful functionalization of HDPE surface.

  7. Sensitivity of juvenile striped bass to chemicals used in aquaculture

    Energy Technology Data Exchange (ETDEWEB)

    Bills, T.D.; Marking, L.L.; Howe, G.E.


    Efforts to restore anadromous striped bass (Morone saxatilis) populations by the U.S. Fish and Wildlife Service and other agencies over the past 20 years have concentrated on hatchery culture to supplement dwindling natural reproduction. Adult fish captured for artificial spawning are stressed by handling and crowding in rearing ponds and are often exposed to therapeutants, anesthetics, disinfectants, and herbicides used in fish culture. The authors determined the toxicity of 17 fishery chemicals (chloramine-T, erythromycin, formalin, Hyamine 3500, Roccal, malachite green, sulfamerazine, benzocaine, etomidate, Finquel (MS-222), metomidate, quinaldine sulfate, chlorine, potassium permanganate, Aquazine, copper sulfate, and Rodeo) to striped bass fry (average weight = 1 g) in reconstituted water (total hardness 40 mg/L) at 12 degrees C. The 96-h LC50's (concentration calculated to produce 50% mortality in a population) ranged from 0.129 mg/L for malachite green to 340 mg/L for erythromycin.

  8. Influence of metabolism in skin on dosimetry after topical exposure

    Energy Technology Data Exchange (ETDEWEB)

    Bronaugh, R.L.; Collier, S.W.; Macpherson, S.E.; Kraeling, M.E.K. [Food and Drug Administration, Washington, DC (United States)


    Metabolism of chemicals occurs in skin and therefore should be taken into account when one determines topical exposure dose. Skin metabolism is difficult to measure in vivo because biological specimens may also contain metabolites from other tissues. Metabolism in skin during percutaneous absorption can be studied with viable skin in flow-through diffusion cells. Several compounds metabolized by microsomal enzymes in skin (benzo[a]pyrene and 7-ethoxycoumarin) penetrated human and hairless guinea pig skin predominantly unmetabolized. However, compounds containing a primary amino group (p-aminobenzoic acid, benzocaine, and azo color reduction products) were substrates for acetyltransferase activity in skin and were substantially metabolized during absorption. A physiologically based pharmacokinetic model has been developed with an input equation, allowing modeling after topical exposure. 14 refs., 3 figs., 4 tabs.

  9. Influence of metabolism in skin on dosimetry after topical exposure. (United States)

    Bronaugh, R L; Collier, S W; Macpherson, S E; Kraeling, M E


    Metabolism of chemicals occurs in skin and therefore should be taken into account when one determines topical exposure dose. Skin metabolism is difficult to measure in vivo because biological specimens may also contain metabolites from other tissues. Metabolism in skin during percutaneous absorption can be studied with viable skin in flow-through diffusion cells. Several compounds metabolized by microsomal enzymes in skin (benzo[a]pyrene and 7-ethoxycoumarin) penetrated human and hairless guinea pig skin predominantly unmetabolized. However, compounds containing a primary amino group (p-aminobenzoic acid, benzocaine, and azo color reduction products) were substrates for acetyltransferase activity in skin and were substantially metabolized during absorption. A physiologically based pharmacokinetic model has been developed with an input equation, allowing modeling after topical exposure. Plasma concentrations in the hairless guinea pig were accurately predicted for the model compound, benzoic acid, from in vitro absorption, metabolism, and other pharmacokinetic parameters.

  10. Occupational contact dermatitis in hairdressers

    DEFF Research Database (Denmark)

    Schwensen, Jakob F; Johansen, Jeanne Duus; Veien, Niels K


    BACKGROUND: Occupational contact dermatitis among hairdressers is frequent, owing to daily exposure to irritants and allergens. OBJECTIVES: To identify sensitization to the most common allergens associated with the occupation of hairdressing. METHODS: Patch test results of 399 hairdressers and 1995...... matched controls with contact dermatitis, registered by the Danish Contact Dermatitis Group between January 2002 and December 2011, were analysed. All patients were patch tested with the European baseline series, and hairdressers were additionally tested with the hairdressing series. RESULTS: Occupational...... with a statistically significant association with the occupation of hairdressing were p-phenylenediamine, thiuram mix, and benzocaine. Frequent sensitizers from the hairdressing series were ammonium persulfate, toluene-2,5-diamine, 3-aminophenol, and 4-aminophenol. Cysteamine hydrochloride and chloroacetamide emerged...

  11. Diffuse Scattering as an Aid to the Understanding of Polymorphism in Pharmaceuticals (United States)

    Welberry, T. R.; Chan, E. J.; Goossens, D. J.; Heerdegen, A. P.


    Polymorphism occurs when the same molecular compound can crystallize in more than one distinct crystal structure. Its study is a field of great interest and activity. This is largely driven by its importance in the pharmaceutical industry, but polymorphism is also an issue in the pigments, dyes, and explosives industries. The polymorph formed by a compound generally exerts a strong influence on its solid-state properties. The polymorphic form of a drug molecule may affect the ease of manufacture and processing, shelf life, and most significantly the rate of uptake of the molecule by the human body. They can even vary in toxicity; one polymorph may be safe, while a second may be toxic. In this review of recently published work, we show how diffuse scattering experiments coupled with Monte Carlo (MC) computer modeling can aid in the understanding of polymorphism. Examples of the two common pharmaceuticals, benzocaine and aspirin, both of which are bimorphic, at ambient temperatures, are discussed.

  12. Separation of cold medicine ingredients using a precise MEKC method at elevated pH. (United States)

    Hasemann, Phillip; ter Balk, Marieke; Preu, Lutz; Wätzig, Hermann


    An MEKC method was developed in order to separate a cold medicine formulation containing acetaminophen, ephedrine sulfate, doxylamine succinate, and dextromethorphan hydrobromide as active pharmaceutical ingredients. Because of their similar physical and chemical properties, it was a challenge to separate the basic compounds without sample pretreatment. In addition, the high content of alcohol and sucrose together with the variety of further excipients had to be considered. Thus, the complex matrix required several optimization steps. These included the search for the optimum pH and for a suitable sodium dodecyl sulfate concentration to avoid matrix-capillary wall interaction and to ensure precision. As a second developing step, an internal standard (benzocaine) was chosen to guarantee a high level of quantitative performance. An RSD% value of the peak areas between 1.0 and 2.0 was reached. The employed method development strategy can be generalized to similar separation approaches in the future.

  13. Anesthesia by sprinkling method in the gills of tambaqui Colossoma macropomum does not influence intensity and morphology of monogeneans

    Directory of Open Access Journals (Sweden)

    C. L. Boijink

    Full Text Available Abstract The present study evaluates the influence of anesthesia on the parasitic fauna of monogenea fish parasites, as its intensity and viability. Two experiments were conducted: Evaluation of an anesthetic method by sprinkling eugenol directly on gills and evaluation of monogenea motility and viability; Comparison of immersion and directly sprinkling on the gills with benzocaine and eugenol followed by evaluation on parasite intensity. The results suggest that the anesthetic sprinkling didn’t interfere in the parasite motility, morphology and body surface integrity analyzed by fluorescence method. The monogenean intensity in the gills was lower in fish anesthetized by immersion method compared to the sprinkling method and the control group. This method of anesthesia can be used in parasitological studies.

  14. 薄荷脑和樟脑对复方苯海拉明乳膏透皮作用的影响%Effect of menthol and camphor on permeation of compound diphenhydramin cream in vitro

    Institute of Scientific and Technical Information of China (English)

    刘海乐; 周彦彬; 孙银香; 盛小茜; 张杰; 郑志难; 丁劲松


    Objective To determine the effect of menthol and camphor on the permeation of diphenhydramine hydrochloride and benzocaine in compound diphenhydramin cream.Methods The permeation experiments were performed in a modified Franz diffusion cell through porcine skin.The permeability coefficients and the accumulation amounts of diphenhydramine hydrochloride and benzocaine in the receptor fluid and skin were calculated.Results There was no significant difference (P>0.05) in the permeation and accumulation of diphenhydramine hydrochloride between cream with and without menthol and camphor.Menthol and camphor markedly prevented (P<0.01 ) the permeation of benzocaine transporting across the skin and promoted the skin accumulation after 12 h (P<0.05).Conclusion Menthol and camphor not only have pharmacological activities but also act as penetration enhancers.Those compounds, which can inhibit the benzocaine permeation transdermally and locally, may be beneficial to the topical treatment of compound diphenhydramin cream in clinical practice.%目的 研究薄荷脑和樟脑对复方苯海拉明乳膏中盐酸苯海拉明和苯佐卡因透皮作用的影响.方法 采用改良Franz直立式扩散池,以离体乳猪皮肤为渗透屏障进行体外透皮扩散试验,以盐酸苯海拉明和苯佐卡因的累积渗透量、稳态流量及皮肤滞留量为指标,考察薄荷脑和樟脑在处方中的透皮调节作用.结果 薄荷脑和樟脑对盐酸苯海拉明的累积渗透量、稳态流量及皮肤滞留量均无显著影响(P>0.05);对苯佐卡因的累积渗透量、稳态流量有显著抑制作用(P<0.01),并能提高其12 h皮肤滞留量(P<0.05).结论 薄荷脑和樟脑在复方苯海拉明乳膏中除发挥其药理活性外,还能调节药物的透皮吸收,其对苯佐卡因经皮渗透的抑制及皮肤滞留量的增加可能更有利于复方苯海拉明乳膏发挥局部治疗作用.

  15. Diffuse Scattering as an Aid to the Understanding of Polymorphism in Pharmaceuticals

    Energy Technology Data Exchange (ETDEWEB)

    Welberry, T.R.; Chan, E.J.; Goossens, D.J.; Heerdegen, A.P. (ANU)


    Polymorphism occurs when the same molecular compound can crystallize in more than one distinct crystal structure. Its study is a field of great interest and activity. This is largely driven by its importance in the pharmaceutical industry, but polymorphism is also an issue in the pigments, dyes, and explosives industries. The polymorph formed by a compound generally exerts a strong influence on its solid-state properties. The polymorphic form of a drug molecule may affect the ease of manufacture and processing, shelf life, and most significantly the rate of uptake of the molecule by the human body. They can even vary in toxicity; one polymorph may be safe, while a second may be toxic. In this review of recently published work, we show how diffuse scattering experiments coupled with Monte Carlo (MC) computer modeling can aid in the understanding of polymorphism. Examples of the two common pharmaceuticals, benzocaine and aspirin, both of which are bimorphic, at ambient temperatures, are discussed.

  16. Hematology of Nile tilapia (Oreochromis niloticus subjected to anesthesia and anticoagulation protocols

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    Nadia Cristine Weinert


    Full Text Available Clinical hematology facilitates the diagnosis of disease and can act as a prognostic indicator of pathological conditions in fish. The aim of the present study was to evaluate hematological parameters of Nile tilapia (Oreochromis niloticus subjected to different anesthetics and anticoagulants. Thirty apparently healthy fishes (average weight of 473 ± 35. 50 g and mean total length of 29. 33 ± 0. 37 cm, were selected from the local commercial fish farm in the Lages municipality (Santa Catarina, Brazil. The animals were randomly divided into three groups of 10. In two groups, anesthesia was induced with eugenol (70 mg·L- 1 (EG and Benzocaine hydrochloride (100 mg·L-1 (BG, respectively. Anesthesia was not administered to fish of the third group (CG/control group. Blood samples were obtained by venipuncture of the caudal vessels and placed into microtubes containing sodium heparin or Na2EDTA for further analysis. The results were analyzed by Sigma Stat for Windows, the paired t-test for significant differences between anticoagulants of the same group, and analysis of variance followed by the Tukey test for comparison of means between groups (p ? 0. 05. Most of the observed changes in the erythrogram were significantly higher for the anticoagulant heparin and benzocaine group in comparison to the control group. However, the values obtained for the leukogram were significantly higher for all groups subjected to the Na2EDTA anticoagulant, suggesting that heparin may cause cell clumping. The results suggest that the anesthetics under investigation effectively minimizes the effects of stress caused by handling and invasive procedures, and that the anticoagulant heparin causes less hemolysis in comparison to Na2EDTA for Nile tilapia. Thus, the hematological variations attributed to different anesthetic protocols and/or different anticoagulants should be considered for the species Oreochromis niloticus.

  17. Development and validation of an HPLC-DAD method for simultaneous determination of cocaine, benzoic acid, benzoylecgonine and the main adulterants found in products based on cocaine. (United States)

    Floriani, Gisele; Gasparetto, João Cleverson; Pontarolo, Roberto; Gonçalves, Alan Guilherme


    Here, an HPLC-DAD method was developed and validated for simultaneous determination of cocaine, two cocaine degradation products (benzoylecgonine and benzoic acid), and the main adulterants found in products based on cocaine (caffeine, lidocaine, phenacetin, benzocaine and diltiazem). The new method was developed and validated using an XBridge C18 4.6mm×250mm, 5μm particle size column maintained at 60°C. The mobile phase consisted of a gradient of acetonitrile and ammonium formate 0.05M - pH 3.1, eluted at 1.0mL/min. The volume of injection was 10μL and the DAD detector was set at 274nm. Method validation assays demonstrated suitable sensitivity, selectivity, linearity, precision and accuracy. For selectivity assay, a MS detection system could be directly adapted to the method without the need of any change in the chromatographic conditions. The robustness study indicated that the flow rate, temperature and pH of the mobile phase are critical parameters and should not be changed considering the conditions herein determined. The new method was then successfully applied for determining cocaine, benzoylecgonine, benzoic acid, caffeine, lidocaine, phenacetin, benzocaine and diltiazem in 115 samples, seized in Brazil (2007-2012), which consisted of cocaine paste, cocaine base and salt cocaine samples. This study revealed cocaine contents that ranged from undetectable to 97.2%, with 97 samples presenting at least one of the degradation products or adulterants here evaluated. All of the studied degradation products and adulterants were observed among the seized samples, justifying the application of the method, which can be used as a screening and quantification tool in forensic analysis.

  18. Eficacia del uso odontológico de la anestesia tópica previa a la punción anestésica infiltrativa: Estudio doble ciego Effectiveness of dental use of topical anesthesia prior to puncture and infiltration of the anesthetic: Double-blind study

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    M. Cabo Valle


    Full Text Available Objetivos: Comprobar la efectividad de la aplicación tópica de un gel de benzocaína en la reducción del dolor producido por el pinchazo y la infiltración anestésica de la mucosa vestibular de caninos superiores. Materiales y métodos: Realizamos un estudio doble ciego, sobre 152 pacientes (80 hombres y 72 mujeres, que precisaban anestesia en la mucosa vestibular de la zona canina. Valoramos el dolor del paciente al pinchazo y a la infiltración, y la existencia de experiencias previas dolorosas o no dolorosas al pinchazo e infiltración de la solución anestésica. Resultados: Los resultados confirmaron la efectividad de la benzocaína para reducir el dolor del pinchazo (p0,005. Discusión: La efectividad de los anestésicos tópicos en la prevención del dolor al pinchazo al igual que en la disminución de la percepción del dolor ante la existencia de experiencias previas desagradables ha sido comprobada. La infiltración anestésica tiene gran variedad de variables que influyen en la sensación álgica, que no pueden ser controladas por la sola aplicación del anestésico tópico.Purpose: To test the effectiveness of topical benzocaine gel in reducing the pain of the puncture and infiltration of anaesthesia, in vestibular mucosa of upper canine. Material and Methods: We conducted a double blind study on 152 patients (80 men and 72 women, who needed anaesthesia in the buccal mucosa of the canine area. We value the patient's pain to pinprick and infiltration, and the existence of prior experience painful or not painful to puncture and infiltration of the anaesthetic. Results: The results confirmed the effectiveness of benzocaine to reduce the pain of a prick (p0.005.

  19. A quantitative HPLC-MS/MS method for studying internal concentrations and toxicokinetics of 34 polar analytes in zebrafish (Danio rerio) embryos. (United States)

    Brox, Stephan; Ritter, Axel P; Küster, Eberhard; Reemtsma, Thorsten


    An analytical method using high-performance liquid chromatography-tandem mass spectrometry was developed to determine internal concentrations of 34 test compounds such as pharmaceuticals and pesticides in zebrafish embryos (ZFE), among them, cimetidine, 2,4-dichlorophenoxyacetic acid, metoprolol, atropine and phenytoin. For qualification and quantification, multiple reaction monitoring mode was used. The linear range extends from 0.075 ng/mL for thiacloprid and metazachlor and 7.5 ng/mL for coniine and clofibrate to 250 ng/mL for many of the test compounds. Matrix effects were strongest for nicotine, but never exceeded ±20 % for any of the developmental stages of the ZFE. Method recoveries ranged from 90 to 110 % from an analysis of nine pooled ZFE. These findings together with the simple sample preparation mean this approach is suitable for the determination of internal concentrations from only nine individual ZFE in all life stages up to 96 h post-fertilization. Exemplarily, the time course of the internal concentrations of clofibric acid, metribuzin and benzocaine in ZFE was studied over 96 h, and three different patterns were distinguished, on the basis of the speed and extent of uptake and whether or not a steady state was reached. Decreasing internal concentrations may be due to metabolism in the ZFE.

  20. Pain perception and anaesthesia in research frogs. (United States)

    Guénette, Sarah Annie; Giroux, Marie-Chantal; Vachon, Pascal


    Frogs possess pain receptors and pathways that support processing and perception of noxious stimuli however the level of organization is less well structured compared to mammals. It was long believed that the experience of pain was limited to 'higher' phylums of the animal kingdom. However, it is now commonly accepted that amphibians possess neuro-anatomical pathways conductive of a complete nociceptive experience. Xenopus laevis frogs have been one of the most popular aquatic research models for developmental studies and genetic research. These frogs have been extensively use in research for their eggs, that can be collected following hormonal stimulation either naturally or by surgical intervention. Many anaesthetics have been used in amphibians such as bath solutions of MS-222, benzocaine and eugenol as well as systemic injections of ketamine or tiletamine, barbiturates, propofol and gas administrations of methoxyflurane, halothane and isoflurane. Most of these anaesthetic drugs produce variability in depth and duration of anaesthesia. MS-222 appears to be one of the most reliable anaesthetics. This review will focus on the evidence of pain perception in frogs and will compare the effectiveness and limitations of different anaesthetics used in Xenopus leavis frogs.

  1. Thin layer chromatography coupled to paper spray ionization mass spectrometry for cocaine and its adulterants analysis. (United States)

    De Carvalho, Thays C; Tosato, Flavia; Souza, Lindamara M; Santos, Heloa; Merlo, Bianca B; Ortiz, Rafael S; Rodrigues, Rayza R T; Filgueiras, Paulo R; França, Hildegardo S; Augusti, Rodinei; Romão, Wanderson; Vaz, Boniek G


    Thin layer chromatography (TLC) is a simple and inexpensive type of chromatography that is extensively used in forensic laboratories for drugs of abuse analysis. In this work, TLC is optimized to analyze cocaine and its adulterants (caffeine, benzocaine, lidocaine and phenacetin) in which the sensitivity (visual determination of LOD from 0.5 to 14mgmL(-1)) and the selectivity (from the study of three different eluents: CHCl3:CH3OH:HCOOHglacial (75:20:5v%), (C2H5)2O:CHCl3 (50:50v%) and CH3OH:NH4OH (100:1.5v%)) were evaluated. Aiming to improve these figures of merit, the TLC spots were identified and quantified (linearity with R(2)>0.98) by the paper spray ionization mass spectrometry (PS-MS), reaching now lower LOD values (>1.0μgmL(-1)). The method developed in this work open up perspective of enhancing the reliability of traditional and routine TLC analysis employed in the criminal expertise units. Higher sensitivity, selectivity and rapidity can be provided in forensic reports, besides the possibility of quantitative analysis. Due to the great simplicity, the PS(+)-MS technique can also be coupled directly to other separation techniques such as the paper chromatography and can still be used in analyses of LSD blotter, documents and synthetic drugs.

  2. Anesthetic efficacy of Oraqix® versus Hurricaine® and placebo for pain control during non-surgical periodontal treatment (United States)

    Mayor-Subirana, Gemma; Yagüe-García, José; Arnabat-Domínguez, Josep; Berini-Aytés, Leonardo; Gay-Escoda, Cosme


    Objectives: To evaluate the efficacy of Oraqix® during scaling and root planing (SRP) in comparison with 20% benzocaine and placebo. Study Design: 15 patients requiring 4 sessions of SRP were enrolled. For each patient, Oraqix®, Hurricaine®, vaseline or no anesthetic product were randomly assigned each to a quadrant. Treatment pain was evaluated on a 100 mm Visual Analog Scale (VAS) and on a Verbal Rating Scale (VRS). The amount of product administered, the need to re-anesthetise, patient and operator satisfaction and the onset of side-effects were also recorded. Results: Oraqix® was significantly better than nothing, with a reduction of VAS score to 13.3 units, but without significant differences with Vaseline or Hurricaine®. Oraqix® was better in VRS reduction than not using any anesthetic (p=0.001) or using vaseline (p=0.024), but similar to Hurricaine® (p=0.232). Conclusions: Oraqix® effectively controls pain in SRP procedures, with few side-effects and a good acceptance on the part of patients and clinicians. Key words:Controlled clinical trial, topical anesthetic, scaling and root planing. PMID:24316699

  3. Honey and a mixture of honey, beeswax, and olive oil-propolis extract in treatment of chemotherapy-induced oral mucositis: a randomized controlled pilot study. (United States)

    Abdulrhman, Mamdouh; Elbarbary, Nancy Samir; Ahmed Amin, Dina; Saeid Ebrahim, Rania


    In spite of being one of the most investigated subjects among supportive care in cancer, no therapy has been found effective in treatment of chemotherapy-induced oral mucositis. Based on the observations that honey bees products have anti-inflammatory and wound healing effects, the present study tried to evaluate the effect of topical application of honey and a mixture of honey, olive oil-propolis extract, and beeswax (HOPE) in treatment of oral mucositis. This was a randomized controlled clinical trial conducted on 90 patients with acute lymphoblastic leukemia and oral mucositis grades 2 and 3. The mean age of enrolled patients was 6.9 years. The patients were assigned into 3 equal treatment groups: Honey, HOPE, and control groups. Topical treatment for each patient consists of honey, HOPE, and benzocaine gel for honey, HOPE, and control groups, respectively. Recovery time in grade 2 mucositis was significantly reduced in the honey group as compared with either HOPE or controls (P < .05). In grade 3 mucositis, recovery time did not differ significantly between honey and HOPE (P = 0.61) but compared with controls, healing was faster with either honey or HOPE (P < .01). Generally, in both grades of mucositis, honey produced faster healing than either HOPE or controls (P < .05). Based on our results that showed that honey produced faster healing in patients with grade 2/3 chemotherapy-induced mucositis, we recommend using honey and possibly other bee products and olive oil in future therapeutic trials targeting chemotherapy-induced mucositis.

  4. Hematological and morphometric blood value of four cultured species of economically important tropical foodfish

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    Genoefa Amália Dal'Bó

    Full Text Available The use and validation of fish health monitoring tools have become increasingly evident due to aquaculture expansion. This study investigated the hematology and blood morphometrics of Piaractus mesopotamicus, Brycon orbignyanus, Oreochromis niloticus and Rhamdia quelen. The fish were kept for 30 days in 300-liter aquariums, after which they were anesthetized with benzocaine and blood was collected from caudal vessels. In comparison to other species, B. orbignyanus presented the highest hematocrit (Ht, RBC averages and Mean Corpuscular Volume (MCV with a particular range of data. B. orbignyanus presented lower Ht, Hb, RBC averages and values, and Mean Corpuscular Hemoglobin Concentration (MCHC. Oreochromis niloticus presented lower Ht, Hb, RBC averages and values, and Mean Corpuscular Hemoglobin Concentration (MCHC. Rhamdia quelen and O. niloticus presented higher variation of White Blood Cells (WBC, neutrophils (Nf, lymphocytes (Lf, monocytes (Mf and thrombocytes (Trb. Data of large axes (LA, minor axes (MA, surface (SF and volume (VL are in the same variance range. This study has demonstrated that hematological variances can occur between animals of different species as well as of the same species.

  5. The Internet versus pediatricians as a source of infant teething information for parents in Turkey

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    Eda Haznedaroglu

    Full Text Available OBJECTIVES: Parents are increasingly searching the Internet to gather information about their children’s health care. This study compared infant teething information obtained from publically employed pediatricians in Istanbul with that obtained from different Turkish websites (parenting, health, professional, news and commercial. METHODS: This study had two parts. The first part used a descriptive design, with two checklists to assess the quality and comprehensiveness of the teething-specific content on 62 parenting or health websites. The second part was a cross-sectional study of 75 pediatricians at public hospitals who completed a structured self-administered questionnaire. RESULTS: In total, 54 websites (87.1% described infant teething as a normal developmental process. The lists that were found on the websites identified the most frequent signs of infant teething as fever and drooling/perioral rash. The most frequent management strategies were chewing non-chilled and chilled objects. For teething problems, some pediatricians recommended teething rings and oral benzocaine, while 23 pediatricians recommended nothing. CONCLUSIONS: Parents should be informed by health professionals, especially regarding specific treatment strategies.

  6. Do decapod crustaceans have nociceptors for extreme pH?

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    Sakshi Puri

    Full Text Available BACKGROUND: Nociception is the physiological detection of noxious stimuli. Because of its obvious importance, nociception is expected to be widespread across animal taxa and to trigger robust behaviours reliably. Nociception in invertebrates, such as crustaceans, is poorly studied. METHODOLOGY/PRINCIPAL FINDINGS: THREE DECAPOD CRUSTACEAN SPECIES WERE TESTED FOR NOCICEPTIVE BEHAVIOUR: Louisiana red swamp crayfish (Procambarus clarkii, white shrimp (Litopenaeus setiferus, and grass shrimp (Palaemonetes sp.. Applying sodium hydroxide, hydrochloric acid, or benzocaine to the antennae caused no change in behaviour in the three species compared to controls. Animals did not groom the stimulated antenna, and there was no difference in movement of treated individuals and controls. Extracellular recordings of antennal nerves in P. clarkii revealed continual spontaneous activity, but no neurons that were reliably excited by the application of concentrated sodium hydroxide or hydrochloric acid. CONCLUSIONS/SIGNIFICANCE: Previously reported responses to extreme pH are either not consistently evoked across species or were mischaracterized as nociception. There was no behavioural or physiological evidence that the antennae contained specialized nociceptors that responded to pH.

  7. Seasonal influence on the hematological parameters in cultured Nile tilapia from southern Brazil

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    GT. Jerônimo

    Full Text Available This study evaluated seasonality in hematological parameters of Nile tilapia cultured in the state of Santa Catarina, southern Brazil. A total of 240 fish were examined during four seasons between April 2007 and March 2008 in three different fish farms. After being anesthetised in a benzocaine solution, blood samples were withdrawn into syringes containing a drop of 10% EDTA for hematological analysis. The results were compared between fish farms and seasons, which are well delimited in southern Brazil. In a traditional fish farm in Joinville in the summer, there was an increase in the percentage of hematocrit and in the red blood cell count. The highest values of total leukocytes were found in fish from fee-fishing in Blumenau in the autumn while the lowest values occurred in those from swine consorted system in Ituporanga in the summer. Thrombocytosis was observed in the autumn, and lymphocytosis was found in both the autumn and winter in tilapia from all fish farms investigated. Neutrophilia was only observed in winter and autumn in fish from Blumenau and Ituporanga. This work demonstrated the influence of seasonality and the handling characteristics of each fish farm on certain hematological parameters in Nile tilapia.

  8. The individual tolerance concept is not the sole explanation for the probit dose-effect model

    Energy Technology Data Exchange (ETDEWEB)

    Newman, M.C.; McCloskey, J.T.


    Predominant methods for analyzing dose- or concentration-effect data (i.e., probit analysis) are based on the concept of individual tolerance or individual effective dose (IED, the smallest characteristic dose needed to kill an individual). An alternative explanation (stochasticity hypothesis) is that individuals do not have unique tolerances: death results from stochastic processes occurring similarly in all individuals. These opposing hypotheses were tested with two types of experiments. First, time to stupefaction (TTS) was measured for zebra fish (Brachydanio rerio) exposed to benzocaine. The same 40 fish were exposed during five trials to test if the same order for TTS was maintained among trials. The IED hypothesis was supported with a minor stochastic component being present. Second, eastern mosquitofish (Gambusia holbrooki) were exposed to sublethal or lethal NaCl concentrations until a large portion of the lethally exposed fish died. After sufficient time for recovery, fish sublethally exposed and fish surviving lethal exposure were exposed simultaneously to lethal NaCl concentrations. No statistically significant effect was found of previous exposure on survival time but a large stochastic component to the survival dynamics was obvious. Repetition of this second type of test with pentachlorophenol also provided no support for the IED hypothesis. The authors conclude that neither hypothesis alone was the sole or dominant explanation for the lognormal (probit) model. Determination of the correct explanation (IED or stochastic) or the relative contributions of each is crucial to predicting consequences to populations after repeated or chronic exposures to any particular toxicant.

  9. 苯佐卡因概况及制剂开发

    Institute of Scientific and Technical Information of China (English)



    @@苯佐卡因(Benzocaine)是一种局麻药,用于皮肤和粘膜的表面麻醉,它是缓解晒伤、瘙痒和轻度烧伤时应用最广泛的药物之一[1]. 1 药理作用 1.1 药理毒理本品局麻作用比普鲁卡因弱,不可作浸润麻醉(不溶于水),局部吸收缓慢持久.水解为对氨基苯甲酸,在正常使用浓度2%~10%时无刺激性和毒性,毒性仅相当于可卡因的5%或10%(可卡因成瘾、价贵),局部使用最大安全量为5 g或者20%溶液25 mL.

  10. Hydrogen-1 NMR relaxation time studies in membrane: anesthetic systems; Variacao dos tempos de relaxacao longitudinal de protons em sistemas membranares contendo anestesicos locais

    Energy Technology Data Exchange (ETDEWEB)

    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


    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.

  11. Fish welfare: the state of science by scientometrical analysis

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    Nédia de Castilhos Ghisi


    Full Text Available In 2014, Brazil produced 474.33 thousand tons of captive-bred fish. In addition, regulatory agencies of animal ethics and welfare have recently encouraged experiments to be done using simpler vertebrates, such as fish. The aim of this article was to perform a scientometric analysis of scientific production that deals with fish welfare, in an attempt to find trends and gaps in this line of research. Our analyses showed a growing concern about fish welfare, although several questions remained inadequately covered. The most studied species was the Atlantic salmon, with Norway having the most publications on this theme. There are controversies among scientists about fish capacity for suffering and enjoyment (sentience. As regards slaughter or euthanasia, some studies showed that some methods are more endorsed than others, because they effectively reduce suffering and improve the appearance of the meat. In respect of animals used for experimentation, the most recommended substances were benzocaine and MS222. Thus, despite the importance of this subject, few studies are decisive and there is still no consensus on how to improve fish welfare or even on how to reduce suffering at the moment of slaughter.

  12. Circadian changes in thyroid hormones of piau, Leporinus obtusidens Valenciennes, 1847 (Osteichthyes, Anostomidae after feeding - DOI: 10.4025/actascibiolsci.v31i4.5814

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    Lea Rosa Mourgués-Schurter


    Full Text Available To evaluate circadian changes in thyroid hormones of piau, Leporinus obtusidens Valenciennes, 1847, (Osteichthyes, Anostomidae after feeding were determined the plasma levels of thyroid hormones (TH of 128 fishes, same age, immature, both sexes, distributed into four classes of weight. They were kept in 16 aquaria (100 L, with artificial aeration and 2 L min. -1 water flow, from March to August, 1996, in Aquaculture Station of the Universidade Federal de Lavras (UFLA. Daily, feed was supplied at 5% body weight. For blood samples, the fishes were anesthetized with benzocaine 10%, and plasmatic levels of TH were determined at 1, 4, 7, 10, 13, 16 and 22h after food supply during 4 consecutive days in June and in August, period of lowest temperature. The classes of weight 63, 75, 82 and 91 g were considered homogeneous, showing that plasmatic concentrations of T3 and T4 were body weight independent for this fish species. The daily cycle of plasma TH were correlated with feed intake, reaching the highest levels 7 h after feeding supply (T3 = 1.75 ± 0.07 ng mL-1 and T4 = 14.9 ± 1.59 ng mL-1. It was also possible to verify that the daily intake is directly correlated with water temperature which is affected by day-light cycle

  13. Synthesis and Pharmacological Properties of Novel Esters Based on Monocyclic Terpenes and GABA

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    Mariia Nesterkina


    Full Text Available Novel esters of γ-aminobutyric acid (GABA with monocyclic terpenes were synthesized via Steglich esterification and characterized by 1H-NMR, IR and mass spectral studies. Their anticonvulsant, analgesic and anti-inflammatory activities were evaluated by a PTZ-induced convulsion model, AITC-induced hyperalgesia and AITC-induced paw edema, respectively. All studied esters, as well as their parent terpenes, were found to produce antinociceptive effects in the AITC-induced model and attenuate acute pain more than the reference drug benzocaine after their topical application. GABA esters of l-menthol and thymol were also shown to exceed the reference drug ibuprofen in their ability to decrease the inflammatory state induced by intraplantar injection of the TRPA1 activator AITC. The present findings indicate that GABA esters of carvacrol and guaiacol are not a classical prodrug and possess their own pharmacological activity. Prolonged antiseizure action of the ester based on the amino acid and guaiacol (200 mg/kg was revealed at 24 h after oral administration. Furthermore, orally co-administered gidazepam (1 mg/kg and GABA esters of l-menthol, thymol and carvacrol produce synergistic seizure prevention effects.

  14. Multitarget Molecular Hybrids of Cinnamic Acids

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    Aikaterini Peperidou


    Full Text Available In an attempt to synthesize potential new multitarget agents, 11 novel hybrids incorporating cinnamic acids and paracetamol, 4-/7-hydroxycoumarin, benzocaine, p-aminophenol and m-aminophenol were synthesized. Three hybrids—2e, 2a, 2g—and 3b were found to be multifunctional agents. The hybrid 2e derived from the phenoxyphenyl cinnamic acid and m-acetamidophenol showed the highest lipoxygenase (LOX inhibition and analgesic activity (IC50 = 0.34 μΜ and 98.1%, whereas the hybrid 3b of bromobenzyloxycinnamic acid and hymechromone exhibited simultaneously good LOX inhibitory activity (IC50 = 50 μΜ and the highest anti-proteolytic activity (IC50= 5 μΜ. The hybrid 2a of phenyloxyphenyl acid with paracetamol showed a high analgesic activity (91% and appears to be a promising agent for treating peripheral nerve injuries. Hybrid 2g which has an ester and an amide bond presents an interesting combination of anti-LOX and anti-proteolytic activity. The esters were found very potent and especially those derived from paracetamol and m-acetamidophenol. The amides follow. Based on 2D-structure–activity relationships it was observed that both steric and electronic parameters play major roles in the activity of these compounds. Molecular docking studies point to the fact that allosteric interactions might govern the LOX-inhibitor binding.

  15. Research on Synthesis of New Azo Calix[4]arene and its Dyeing Properties

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    Tang Jun


    Full Text Available With the raw materials of calix[4]arene, benzocaine, tricaine and procaine hydrochloride, three new azo calix[4]arene derivatives—6a, 6b and 6c are synthesized by diazotization–coupling reaction of an aromatic amine, with its yield of 83%, 81% and 83% respectively. The structural characterization is in a way of IR, 1H NMR and elemental analysis. This paper investigates the spectral properties of azo calix[4]arene derivatives under different solution pH conditions through the UV–visible spectroscopy, and researches the dyeing properties through the dyeing curve, color yield test and fastness test. The results show that, with the increase of pH value, the azo calix[4]arene derivatives—6a, 6b and 6c form azo–hydrazone tautomeric isomers with the maximum absorption peak redshift; the dyeing effect of the compound is good, of which the dye–uptake rate of the compound 6a is as high as 78%; the surface depth of color yield is 2.798, and the dry and wet rubbing fastness and the soaping fastness are respectively 4, which is a better disperse dye.

  16. Nitrogen narcosis and pressure reversal of anesthetic effects in node of Ranvier. (United States)

    Kendig, J J


    To compare sodium channel block by hyperbaric nitrogen with that induced by other anesthetics and to examine the basis for pressure antagonism to anesthetic condition block, voltage clamped nodes of Ranvier were exposed to nitrogen at pressures at 1-14 atm alone and in combination with helium to a total pressure of up to 100 atm. At 7 and 14 atm nitrogen, sodium currents were reversibly depressed without accompanying changes in the current-voltage relation. The curve relating steady-state inactivation (h infinity) to voltage was shifted in the hyperpolarizing direction, as is the case with other general anesthetic agents. The time constant of inactivation (tau h) was slightly decreased at depolarized potentials. The preceding companion paper demonstrated an opposite effect of hyperbaric helium on the properties of sodium inactivation. Addition of helium pressure in the presence of nitrogen at 14 atm did not increase peak sodium current with inactivation maximally removed, but it did shift the h infinity curve back toward control levels, thus increasing sodium current at points on the slope of the curve. It is proposed that these opposing shifts in steady-state inactivation levels are the basis for pressure antagonism to anesthetic conduction block. In the case of inert gases and volatile anesthetic agents, the antagonism may be direct but has not been shown to be so. In the case of the local anesthetic benzocaine, differences in the voltage dependence of anesthetic and pressure-induced changes in tau h indicate the antagonism is indirect.

  17. Trichodina nobilis Chen, 1963 and Trichodina reticulata Hirschmann et Partsch, 1955 from ornamental freshwater fishes in Brazil

    Directory of Open Access Journals (Sweden)

    ML Martins

    Full Text Available In the present work Trichodina reticulata and T. nobilis (Ciliophora: Trichodinidae are morphologically characterised from ornamental freshwater fish culture in the State of Santa Catarina, Brazil. The prevalence of infection and a list of comparative measurements are discussed. We examined "southern platyfish" Xiphophorus maculatus (n = 35, "goldfish" Carassius auratus (n = 31, "guppy" Poecilia reticulata (n = 20, "sailfin molly" Poecilia latipinna (n = 6, "beta" Betta splendens (n = 2 and "spotted headstander" Chilodus punctatus (n = 1. After being anesthetised in a benzocaine solution, fishes were examined for parasitological evaluation. A total of 51.57% fishes were parasitised by Trichodina spp. Carassius auratus was the most parasitised species, followed by X. maculatus and P. reticulata. Beta splendens, C. punctatus and P. latipinna were not parasitised by any trichodinid species. Two species of Trichodina were collected from the skin of fish: T. nobilis was found in C. auratus, P. reticulata and X. maculatus and T. reticulata was only observed in C. auratus. The importance of adequate handling in ornamental fish culture are also discussed.

  18. Do fish perceive anaesthetics as aversive?

    Directory of Open Access Journals (Sweden)

    Gareth D Readman

    Full Text Available This study addresses a fundamental question in fish welfare: are the anaesthetics used for fish aversive? Despite years of routine general use of many agents, within both scientific research and aquaculture, there is a paucity of information regarding their tolerance and associated behavioural responses by fish. This study examined nine of the most commonly used fish anaesthetic agents, and performed preference tests using adult mixed sex zebrafish (Danio rerio, the most commonly held laboratory fish. Video tracking software quantified swimming behaviour related to aversion for each anaesthetic at 50% of its standard recommended dose compared with clean water in a flow-through chemotaxic choice chamber. Results suggest that several commonly used anaesthetics were aversive, including two of the most commonly recommended and used: MS222 (ethyl 3-aminobenzoate methanesulphate and benzocaine. For ethical best practice, it is recommended that compounds that are aversive, even at low concentration, should no longer be used routinely for anaesthesia or indeed the first step of humane euthanasia of adult zebrafish. Two agents were found not to induce aversive behavioural responses: etomidate and 2,2,2 tribromoethanol. For the millions of adult zebrafish used in laboratories and breeding worldwide, etomidate appears best suited for future routine humane use.

  19. Comparative Evaluation of Pain Scores during Periodontal Probing with or without Anesthetic Gels

    Directory of Open Access Journals (Sweden)

    Ashank Mishra


    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.

  20. (19)F NMR spectroscopic characterization of the interaction of niflumic acid with human serum albumin. (United States)

    Kitamura, Keisuke; Omran, Ahmed A; Takegami, Shigehiko; Tanaka, Rumi; Kitade, Tatsuya


    The interaction of a non-steroidal anti-inflammatory drug, niflumic acid (NFA), with human serum albumin (HSA) has been investigated by (19)F nuclear magnetic resonance (NMR) spectroscopy. A (19)F NMR spectrum of NFA in a buffered (pH 7.4) solution of NaCl (0.1 mol L(-1)) contained a single sharp signal of its CF(3) group 14.33 ppm from the internal reference 2,2,2-trifluoroethanol. Addition of 0.6 mmol L(-1) HSA to the NFA buffer solution caused splitting of the CF(3) signal into two broadened signals, shifted to the lower fields of 14.56 and 15.06 ppm, with an approximate intensity ratio of 1:3. Denaturation of HSA by addition of 3.0 mol L(-1) guanidine hydrochloride (GU) restored a single sharp signal of CF(3) at 14.38 ppm, indicating complete liberation of NFA from HSA as a result of its denaturation. These results suggest that the binding is reversible and occurs in at least two HSA regions. Competitive (19)F NMR experiments using warfarin, dansyl-L: -asparagine, and benzocaine (site I ligands), and L: -tryptophan and ibuprofen (site II ligands) revealed that NFA binds to site I at two different regions, Ia and Ib, in the ratio 1:3. By use of (19)F NMR with NFA as an (19)F NMR probe the nonfluorinated site I-binding drugs sulfobromophthalein and iophenoxic acid were also found to bind sites Ia and Ib, respectively. These results illustrate the usefulness and convenience of (19)F NMR for investigation of the HSA binding of both fluorinated and nonfluorinated drugs.

  1. AC electrokinetic drug delivery in dentistry using an interdigitated electrode assembly powered by inductive coupling. (United States)

    Ivanoff, Chris S; Wu, Jie Jayne; Mirzajani, Hadi; Cheng, Cheng; Yuan, Quan; Kevorkyan, Stepan; Gaydarova, Radostina; Tomlekova, Desislava


    AC electrokinetics (ACEK) has been shown to deliver certain drugs into human teeth more effectively than diffusion. However, using electrical wires to power intraoral ACEK devices poses risks to patients. The study demonstrates a novel interdigitated electrode arrays (IDE) assembly powered by inductive coupling to induce ACEK effects at appropriate frequencies to motivate drugs wirelessly. A signal generator produces the modulating signal, which multiplies with the carrier signal to produce the amplitude modulated (AM) signal. The AM signal goes through the inductive link to appear on the secondary coil, then rectified and filtered to dispose of its carrier signal, and the positive half of the modulating signal appears on the load. After characterizing the device, the device is validated under light microscopy by motivating carboxylate-modified microspheres, tetracycline, acetaminophen, benzocaine, lidocaine and carbamide peroxide particles with induced ACEK effects. The assembly is finally tested in a common dental bleaching application. After applying 35 % carbamide peroxide to human teeth topically or with the IDE at 1200 Hz, 5 Vpp for 20 min, spectrophotometric analysis showed that compared to diffusion, the IDE enhanced whitening in specular optic and specular optic excluded modes by 215 % and 194 % respectively. Carbamide peroxide absorbance by the ACEK group was two times greater than diffusion as measured by colorimetric oxidation-reduction and UV-Vis spectroscopy at 550 nm. The device motivates drugs of variable molecular weight and structure wirelessly. Wireless transport of drugs to intraoral targets under ACEK effects may potentially improve the efficacy and safety of drug delivery in dentistry.

  2. Local Anesthetics in the Gas-Phase the Rotational Spectrum of Butamben and Isobutamben (United States)

    Vallejo-López, Montserrat; Ecija, Patricia; Caminati, Walther; Grabow, Jens-Uwe; Lesarri, Alberto; Cocinero, Emilio J.


    Benzocaine (BZ), butamben (BTN) and isobutamben (BTI) are local anesthetics characterized by a hydrophilic head and a lipophilic aliphatic tail linked by an aminobenzoate group. Previous rotational work on BZ (H2N-C6H4-COO-Et) showed that its ethyl aliphatic tail may adopt either in-plane (trans) or out of plane (gauche) conformations, with a low interconversion barrier below 50 cm-1. Here we extend the rotational study to BTN and BTI, isolated in a supersonic jet expansion and vaporized either by heating or UV ps-laser ablation methods. Both molecules share a 14 heavy-atoms skeleton, differing in their butyl (-(CH2)3-CH3) or isobutyl (-CH2-CH(CH3)2) four-carbon tail. We detected a single conformer for BTN and two conformers for BTI. The two molecules do not adopt an all-trans carbon skeleton. Conversely, the β-ethyl carbon in BTN is gauche. For BTI the β-carbon may be either trans or gauche. The microwave spectrum covered the cm- (BTN, BTI, 6-18 GHz) and mm-wave (BTW, 50-75 GHz) frequency ranges.In all the cases, rotational and centrifugal distortion constants as well as the diagonal elements of the 14N nuclear quadrupole coupling tensor were accurate determined and compared to the theoretical results (ab initio and DFT). No transitions belonging to configurations predicted as higher minima of the PES were found, pointing out that conformational interconversions may take place in the jet. A. Lesarri, S. T. Shipman, G. G. Brown, L. Alvarez-Valtierra, R. D. Suenram, B. H. Pate, Int. Symp. Mol. Spectrosc., 2008, Comm. RH07. E. Aguado, A. Longarte, E. Alejandro, J. A. Fernández, F. Castaño, J. Phys. Chem. A, 2006, 110, 6010.

  3. Effect of photoperiod stress assessment and locomotor activity of female lambari (Astyanax bimaculatu

    Directory of Open Access Journals (Sweden)

    Fernanda Keley Silva Pereira Navarro


    Full Text Available Some studies and scientific investments have been done in aquaculture aiming to minimize the stress of the fish due to different factors, as management, nutritional status, water quality, temperature, photoperiod, and salinity. This study aimed to verify the effect of photoperiod on locomotor activity and plasma levels of cortisol and glucose in female Lambari. One hundred and twenty female Lambari adult were maintained in aquaria of 20 liters each in a completely randomized design with three treatments (T1 = 0Light: 24Dark, T2 = 12L: 12D, T3 = 24L: 0D and four replications. The daily locomotor activity was registered during 15 days using an infrared photocell. After 40 days of experiment and previous fasting for 24 hours, fish were euthanized by a lethal dose of benzocaine. Female Lambari featured a diurnal rhythm of locomotor activity. Lambari subjected to 12:12 and LD photoperiod presented higher cortisol (12L:12E: 190.00 ± 37.73 ng/mL e 24L:0E: 148.850 ± 32.77 ng/mL and locomotor activity levels and also lower survival rates (30.0 ± 7.07% when compared to the LD photoperiod (cortisol: 85.570 ± 7.99 ng/mL, survival rates: 72.5 ± 4.330%. The glucose concentration (32.167 ± 22.73 mg/dL and the growth (7.050 ±0.59cm of fish subjected to LD photoperiod was significantly lower than in the other treatments. We conclude that light plays an important role in the growth, behavior and welfare of female Lambari. Besides, our data highlighted that fish submitted to a long light period present a more stressed and more aggressive status when compared to fish submitted to a continuous darkness.

  4. Rationalization of reduced penetration of drugs through ceramide gel phase membrane. (United States)

    Paloncýová, Markéta; DeVane, Russell H; Murch, Bruce P; Berka, Karel; Otyepka, Michal


    Since computing resources have advanced enough to allow routine molecular simulation studies of drug molecules interacting with biologically relevant membranes, a considerable amount of work has been carried out with fluid phospholipid systems. However, there is very little work in the literature on drug interactions with gel phase lipids. This poses a significant limitation for understanding permeation through the stratum corneum where the primary pathway is expected to be through a highly ordered lipid matrix. To address this point, we analyzed the interactions of p-aminobenzoic acid (PABA) and its ethyl (benzocaine) and butyl (butamben) esters with two membrane bilayers, which differ in their fluidity at ambient conditions. We considered a dioleoylphosphatidylcholine (DOPC) bilayer in a fluid state and a ceramide 2 (CER2, ceramide NS) bilayer in a gel phase. We carried out unbiased (100 ns long) and biased z-constraint molecular dynamics simulations and calculated the free energy profiles of all molecules along the bilayer normal. The free energy profiles converged significantly slower for the gel phase. While the compounds have comparable affinities for both membranes, they exhibit penetration barriers almost 3 times higher in the gel phase CER2 bilayer. This elevated barrier and slower diffusion in the CER2 bilayer, which are caused by the high ordering of CER2 lipid chains, explain the low permeability of the gel phase membranes. We also compared the free energy profiles from MD simulations with those obtained from COSMOmic. This method provided the same trends in behavior for the guest molecules in both bilayers; however, the penetration barriers calculated by COSMOmic did not differ between membranes. In conclusion, we show how membrane fluid properties affect the interaction of drug-like molecules with membranes.

  5. Is benzoquinone the prohapten in cross-sensitivity among aminobenzene compounds? (United States)

    Lisi, P; Hansel, K


    Cross-sensitivity in allergic contact dermatitis is a simultaneous allergy to 2 or more contact substances which have in common an antigenic determinant or a metabolic derivative. One of the most notable examples is the cross-sensitivity among aromatic compounds which may be oxidized in vivo to benzoquinone (BQ). However, it has also been hypothesized that the allergenicity and cross-sensitization are modulated by the chemical reactivity of the substituents in the para position. A serial dilution of BQ (from 1% to 0.1% in pet.) and three 1,4-substituted benzene derivatives (p-aminophenol, hydroquinone, metol), theoretically capable of conversion to BQ by oxidation, were patch tested in 22 p-phenylenediamine (PPD) positive patients and in 20 controls. The patients and a further 116 subjects with a positive history of sensitivity to 1 or more aminoaromatic compounds were also tested with some haptens of the para group (PPD, p-aminobenzoic acid, p-aminodiphenylamine, benzocaine, procaine chloride, p-toluenediamine sulfate). The results show that (i) the optimal patch test concentration for BQ was 0.2%, (ii) only 4 of the 22 patients allergic to PPD gave a clearly positive allergic reaction to BQ, and (iii) the number of positive reactions to the aromatic compounds was correlated with the presence of activating (-NH2, -OH, -CH3) and deactivating (-COOH) groups in the para position or, perhaps, with their effect on percutaneous penetration. The data suggest that BQ is not the only intermediate in the cross-sensitization of para group haptens. This is probably conditioned by other oxidation products and/or the chemical structure of the substituents in position 4 of the benzene ring.

  6. A survey of adulterants used to cut cocaine in samples seized in the Espírito Santo State by GC-MS allied to chemometric tools. (United States)

    de Souza, Lindamara M; Rodrigues, Rayza R T; Santos, Heloá; Costa, Helber B; Merlo, Bianca B; Filgueiras, Paulo R; Poppi, Ronei J; Vaz, Boniek G; Romão, Wanderson


    Cocaine is a stimulant drug of the central nervous system (CNS) extracted from the leaves of Erytroxylum coca. It is defined as a tropane alkaloid containing 1R-(exo,exo)-3-(benzoyloxy)-8-methyl-8-azabicyclo[3.2.1]octane-2-carboxylic acid methyl esther. However, despite its defined composition, a wide variety of chemical additives are present in cocaine found in the illicit market, such as benzocaine, lidocaine, caffeine, procaine and phenacetin. In this work, 512 cocaine samples seized by the Civil Police of Espirito Santo state (PC-ES, Brazil) were analyzed by gas chromatography mass spectrometry (GC-MS) allied to principal component analysis (PCA) in order to classify the samples as a function of seizure year (2008, 2009, 2010, 2011 and 2012) and location (metropolitan, north, south and central). The cocaine content (wt.%) and its adulterants were also estimated. Analyzing the samples seized between 2008 and 2011, three sample sets are clearly grouped according to the degree of adulteration with caffeine and lidocaine: 100-50 wt.% of cocaine; 50-20 wt.% of cocaine; and 20-80 wt.% of lidocaine and 60-80 wt.% of caffeine, simultaneously. The last group is formed by samples seized between 2008 and 2009, which proves the higher degree of adulteration during this period. In 2012, higher cocaine content was observed for the 191 analyzed samples than in samples from previous years. The PCA data also suggests that the metropolitan region samples had a higher degree of adulteration than the state countryside samples.

  7. 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.


    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.

  8. 固相萃取-液质联用分析药物和个人护理品%Determination of Pharmaceutical and Personal Care Products by Solid Phase Extraction Coupled with LC/MS

    Institute of Scientific and Technical Information of China (English)

    曾超; 蒋科伟; 钱佳; 周季堂; 刘敏敏


    A method for determination of pharmaceutical and personal care products ( PPCPs) was developed using solid phase ex-traction-liquid chromatography/mass spectrometry ( SPE-LC/MS) .The PPCPs were concentrated by Oasis HLB solid phase extrac-tion column at acidic and alkaline conditions .Thirty PPCPs were detected in Yixing City by the developed method with the correla-tion coefficient in the range of 0.990~0.999 and the detection limit in the range of 1.37~10.12 ng/L.The most frequently detec-ted PPCPs were diethyltoluamede , atenolol, paracetamol, procaine, beta-estradiol, carbamazepine and benzocaine .Atenolol had the highest concentration of these PPCPs with the range of 500~600 ng/L.Diethyltoluamede was the most frequently discovered PPCPs , however , the concentrations were low with the range of 1~50 ng/L.%建立了固相萃取-液质联用分析药物和个人护理品( PPCPs)的方法,采用Oasis HLB固相萃取柱分别在酸性条件下和碱性条件下对PPCPs进行富集提取,该法对于宜兴地区能够检出的30种PPCPs均具有良好的线性,相关系数为0.990~0.999,检出限为1.37~10.12 ng/L。应用该法对宜兴地区地表水中存在的PPCPs进行分析,结果显示30种PPCPs均有不同程度检出,分布最广泛的7种分别为避蚊胺、阿替洛尔、对乙酰氨基酚、普鲁卡因、β-雌二醇、卡马西平和苯佐卡因,阿替洛尔浓度较高,普遍为5~600 ng/L。避蚊胺虽然出现频率最高,但其在各个采样点浓度偏低,普遍为1~50 ng/L。

  9. 皮炎湿疹类皮肤病斑贴试验结果分析%Analysis of patch-test results of para eczema and dermatitis

    Institute of Scientific and Technical Information of China (English)

    张艳杰; 尚艳华; 王凯


    目的 探讨皮炎湿疹类皮肤病接触性致敏原及其特点,以期更好地诊断与治疗.方法 对340例皮炎湿疹类皮肤病患者采用标准筛选抗原进行斑贴试验.结果 340例患者中275例对20种标准筛选抗原中的18种出现1种或1种以上抗原阳性反应,总阳性反应率为80.88%,其中以硫酸镍阳性率最高,达29.70%,其余阳性率较高者依次为重铬酸钾(27.64%)、芳香混合物(22.35%)、卡巴混合物(20.29%)、硫柳汞(18.82%.)、苯唑卡因(17.94%).结论 硫酸镍、重铬酸钾、芳香混合物、卡巴混合物是目前引起皮炎湿疹类患者的主要变应原,斑贴试验有助于明确皮炎湿疹类变态反应性皮肤病及接触性致敏原及其性质.%Objective To investigate the characteristics of contact allergens in eczema and dermatitis for further diagnosis and treatment. Methods 340 cases with eczema and dermatitis were tested with a standardized screening antigen kit. Results (80. 88% ) of the 340 patients tested had at least one positive allergen among 18 of 20 standardized screening antigen. The first six allergens were nickel sulfate ( 29. 70% ), potassium dichroroate (27.64% ) ,fragrant mix(22.35% ) ,carba mix(20.29% ) ,thimerosal( 18. 82% ) ,benzocaine( 17.94% ). Conclusion Nickel sulfate,potassium dichromate,fragrance mix and carba mix were the main allergens causing dermatitis and eczema presently. Patch-testing was helpful in identifying the property of contact allergens in para eczema and dermatitis.

  10. Chemically modified carbon paste and membrane sensors for the determination of benzethonium chloride and some anionic surfactants (SLES, SDS, and LABSA): Characterization using SEM and AFM. (United States)

    Issa, Yousry M; Mohamed, Sabrein H; Baset, Mohamed Abd-El


    Chemically modified carbon-paste (CMCP) and membrane- sensors based on incorporating benzothonium-tetraphenylborate (BT-TPB) were constructed for the analysis of benzethonium chloride, and some other surfactants such as sodium lauryl ether sulphate (SLES), sodium dodecyl sulphate (SDS), and linear alkylbenzene sulphonic acid (LABSA). All sensors showed good sensitivity and reverse wide linearity over a concentration range of 5.97×10(-7) to 1.00×10(-3) and 5.96×10(-7) to 3.03×10(-3)molL(-1) with limit of detection of 3.92×10(-7)and 3.40×10(-7)molL(-1) for membrane and chemically modified carbon paste sensors, respectively, with respect to benzethonium chloride (BT.Cl). They could be used over a wide pH range of 2.0-10.0. The thermal coefficients of membrane and CMCP sensors are 5.40×10(-4), 1.17×10(-4)V/°C, respectively. The sensors indicated a wide selectivity over different inorganic cations. The effect of soaking on the surface morphology of the membrane sensor was studied using EDX-SEM and AFM techniques. The response time was <10s The freshly prepared, exhausted membrane, and CMCP sensors were successfully applied for the potentiometric determination of the pure BT.Cl solution. They were also used for the determination of its pharmaceutical formulation Dermoplast(®) antibacterial spray (20% benzocaine+0.2% benzethonium chloride) with recovery values ranging from 97.54±1.70 to 101.25±1.12 and from 96.32±2.49 to 101.23±2.15%. The second goal of these sensors is the potentiometric determination of different surfactants such as SLES, SDS, and LABSA with good recovery values using BT.Cl as a titrant in their pure forms, and in samples containing one of them (shampoo, Touri(®) dishwashing liquid, and waste water). The statistical analysis of the obtained data was studied.

  11. Circadian changes in thyroid hormones of piau, Leporinus obtusidens Valenciennes, 1847 (Osteichthyes, Anostomidae after feeding = Variações circadianas dos hormônios tireoidianos de piau, Leporinus obtusidens Valenciennes, 1847 (Osteichthyes, Anostomidae após alimentação

    Directory of Open Access Journals (Sweden)

    Walter Dias Junior


    Full Text Available To evaluate circadian changes in thyroid hormones of piau, Leporinusobtusidens Valenciennes, 1847, (Osteichthyes, Anostomidae after feeding were determined the plasma levels of thyroid hormones (TH of 128 fishes, same age, immature, both sexes, distributed into four classes of weight. They were kept in 16 aquaria (100 L, with artificial aeration and 2 L min.-1 water flow, from March to August, 1996, in Aquaculture Station of the Universidade Federal de Lavras (UFLA. Daily, feed was supplied at 5% body weight. For blood samples, the fishes were anesthetized with benzocaine 10%, and plasmatic levels of TH were determined at 1, 4, 7, 10, 13, 16 and 22h after food supply during 4 consecutive days in June and in August, period of lowest temperature. The classes of weight 63, 75, 82and 91 g were considered homogeneous, showing that plasmatic concentrations of T3 and T4 were body weight independent for this fish species. The daily cycle of plasma TH were correlated with feed intake, reaching the highest levels 7 h after feeding supply (T3 = 1.75 ± 0.07 ng mL-1 and T4 = 14.9 ± 1.59 ng mL-1. It was also possible to verify that the daily intake is directly correlated with water temperature which is affected by day-light cycle.Para avaliar as variações circadianas dos hormônios tireoidianos do piau, Leporinus obtusidens Valenciennes, 1847, (Osteichthyes, Anostomidae após alimentação, foram determinados os níveis plasmáticos dos hormônios tireoidianos (HT T3 e T4 de 128 peixes, de mesma idade, imaturos, ambos os sexos, distribuídos em quatro classes de peso e mantidos em 16 aquários (100 L, com aeração artificial e fluxo constante de água de 2 L min.-1, de março a agosto de 1996, na Estação de Aquicultura da Universidade Federal de Lavras (UFLA. Diariamente, a ração foi fornecida a 5% do peso corporal. Nas pesagens e amostragens de sangue, os animais foram anestesiados com benzocaína a 10% e os níveis plasmáticos dos HT foram

  12. Dermatite de contato em idosos Contact dermatitis in elderly patients

    Directory of Open Access Journals (Sweden)

    Ida Duarte


    patients had positive tests and 10 had negative tests. In the adult group, 436 had positive tests and 145 negative tests. The difference between the groups was statistically significant (p=0.02. The most frequent sensitizers in the elderly group were nickel sulfate (p=0.001, fragrance-mix (p=0.004, neomycin (p=0.0008, nitrofurazone (p=0.02, promethazine (p=0.03 and benzocaine (p=0.007. CONCLUSIONS: Allergic contact dermatitis in the elderly is as frequent as in other age groups. The substances related to topical medicines are important etiologic agents of allergic contact dermatitis in elderly individuals.

  13. Synthesis and dyeing properties of novel azo dye%新型偶氮染料的合成及其染色性能研究

    Institute of Scientific and Technical Information of China (English)

    陶康; 吕早生; 汤军; 任肖丽; 王丹丹; 严莉; 胡衍甜


    Three novel azocalix [4] arene compounds were synthesized through diazo-coupling reaction using calix [4] arene, benzocaine, tricaine and procaine hydrochloride as raw materials, and the yield of com⁃pounds 6a, 6b and 6c was up to 83%, 81% and 83%, respectively. The compound structure was character⁃ized by IR, 1H NMR and elemental analysis. The spectra properties of azocalix [4] arene in different pH of solu⁃tion were investigated by UV-Vis. The dyeing properties were studied by the dyeing curve, color depth and fastness test. The results indicated that the increase of pH led to azo-quinoid tautomerizm phenomena of azo⁃calix [4] arene compounds 6a, 6b and 6c, and the maximum absorption peak occurred red-shift. The novel azo⁃calix [4] arene compounds had an outstanding dyeing ability under basic condition than acid condition, and the dyeing percentage of compound 6a was as high as 78%, the K/S value was 2.798, the soaping fastness and dry and wet rubbing fastnesses were al level 4, indicating the compound 6a was a good disperse dye.%以杯[4]芳烃、苯佐卡因、三卡因和盐酸普鲁卡因为原料,通过芳胺的重氮化-偶合反应合成了3个新型的偶氮基杯[4]芳烃衍生物6a、6b、6c,收率分别为83%、81%、83%。经IR、1H NMR和元素分析进行结构表征。通过紫外可见光谱考察了偶氮基杯[4]芳烃衍生物在溶液不同pH条件下的光谱性质,并通过上染曲线、得色深度、色牢度研究其染色性能。结果表明,随着pH的增大,偶氮基杯[4]芳烃衍生物6a、6b、6c发生偶氮-醌腙异构互变,最大吸收峰红移;化合物在碱性条件下的染色效果比酸性条件好,其中化合物6a的上染率高达78%,表面得色深度为2.798,耐干、湿摩擦色牢度和耐皂洗色牢度均为4级,是一种较好的分散染料。

  14. Clove oil as anaesthetic for juveniles of matrinxã Brycon cephalus (Gunther, 1869 Óleo de cravo como anestésico para juvenis de matrinxã Brycon cephalus (Gunther, 1869

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    Luis Antônio Kioshi Aoki Inoue


    Full Text Available Many chemicals have been used as anaesthetics in fish farms and fish biology laboratories to keep the fish immobilized during handling procedures and to prevent accidents and animal stress. In Brazil, tricaine methane sulfonate (MS 222, quinaldine sulfate, benzocaine, and phenoxyethanol are the most common fish anaesthetics used to prevent fish stress during handling, but many side effects such as body and gill irritations, corneal damage and general risks of intoxication have been reported. Clove oil is a natural product proposed as an alternative fish anaesthetic by many researchers and it has been used in many countries with great economic advantages and no apparent toxic properties. In this work, we assessed the suitability of clove oil to anaesthetize matrinxã. Sixty-three juveniles of matrinxã were exposed to seven anaesthetic batches of clove oil (pharmaceutical grade namely 18, 20, 30, 40, 50, 60, and 70 mg/L. The times to reach total loss of equilibrium and to recover the upright position were measured. Clove oil concentration about 40 mg/L was enough to anaesthetize the fish in approximately one minute and the recovery time was independent in regard to anaesthetic concentration.Diversos produtos químicos têm sido empregados como anestésicos para peixes nas estações de piscicultura e laboratórios de biologia de peixes para a devida imobilização dos organismos, afim de se prevenir acidentes e ferimentos na superfície do corpo dos próprios peixes, que podem ficar susceptíveis a patógenos e taxas altas de mortalidade. A tricaina metano sulfonato (MS 222, a quinaldina, a benzocaina e o phenoxyethanol têm sido amplamente utilizados no Brasil, mas alguns efeitos colaterais são observados como perda de muco, irritação nas brânquias e olhos, e também alguns incômodos aos trabalhadores como a necessidade do uso de luvas. Dessa forma, o óleo de cravo é proposto como um anestésico alternativo por ser um produto natural de

  15. Haematological and gill responses in parasitized tilapia from valley of Tijucas River, SC, Brazil Respostas hematológica e branquial de tilápia parasitada do vale do Rio Tijucas, SC, Brasil

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    Tatiana Maslowa Pegado de Azevedo


    Full Text Available In the State of Santa Catarina there is no information about haematological and parasitological characteristics of fish maintained in feefishing operations and manured ponds. This work compared the haematological characteristics of Nile tilapia parasitized or not, captured in a property situated in Nova Trento, SC, Brazil, between August 2003 and July 2004. During the studied period, the water temperature, pH, dissolved oxygen, alkalinity, ammonia and transparency were measured. Ten fish were collected monthly either in a feefishing or in a pond receiving pig manure, and anesthetized with benzocaine solution for haematological, parasitological and histopathological exams. From a total of 360 analyzed fish, 64 (17.8% were parasitized with Cichlidogyrus sclerosus and Cichlidogyrus sp. (Monogenoidea: Ancyrocephalidae, 20 (5.5% with Trichodina sp. (Protozoa: Ciliophora, and four (1.1% with Lamproglena sp. (Crustacea: Lernaeidae. The total number of erythrocytes, thrombocytes and leucocytes, glucose rate and the percentages of hematocrit, lymphocytes, monocytes and neutrophils did not show relation with parasitism. Histopathological analysis showed moderate hyperplasia and absence of congestion. The low level of parasitism found in the animals was not responsible for haematological alterations.No Estado de Santa Catarina não existe informação sobre características hematológicas e parasitológicas que compare peixes mantidos em pesque-pague e com dejetos de suínos. Este trabalho estudou as características hematológicas da tilápia do Nilo parasitada ou não, capturada numa propriedade em Nova Trento, SC, Brasil, entre agosto de 2003 e julho de 2004. Durante o período a temperatura da água, pH, oxigênio, alcalinidade e transparência foram medidos. Dez peixes foram mensalmente coletados no pesque-pague e num viveiro que recebia dejetos de suínos, anestesiados com benzocaína para análise hematológica, parasitológica e histopatol

  16. Tatuaje de henna en niños: ¿natural y temporal? Henna tattooing in children: natural or temporary?

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    E. M. Lasa


    with a few side-effects. Nowadays black henna tattoos are usually performed even in children. The addition of several chemical agents to improve its cosmetic properties has increased the risk of developing contact dermatitis after exposure. Our aim is to determine the causative agents of contact dermatitis in two children wearing henna tattoos. Material and Methods: Case 1: A 12-year-old girl with no atopy presented local vesicles 10 hours after a black henna tattoo was applied. She had presented similar symptoms with a previous tattoo. Case 2: A 7-year-old atopic boy presented vesicles 2 weeks after a black henna tattoo was applied. He had dyed his hair previously without side effects. Both patients cured, after 3-4 weeks of treatment with topic corticosteroids, with residual hypo-pigmentation. Skin prick test with natural and commercial henna and epicutaneous test with TRUE-TEST®, PABA derivatives compounds tests, textile dyes and natural and commercial henna were performed. Results: The epicutaneous tests were positive for p-Metilaminophenol, p-Aminobencene, p-Phenilendiamine and p-Toluenodiamine in both patients. The first patient had also positive tests for Benzocaine, Hydroquinone, Isobutyl p-aminobenzoate, Yellow 1 and Orange 1 disperse; the second one for Red 1 and Orange 1 disperse. In both cases the prick and epicutaneous tests for henna were negative. Conclusions: Two children presented contact dermatitis after black henna tattoo due to added additives such as paraphenilendiamine.

  17. Analysis of the patch test results of 141 cases of cosmetic contact dermatitis%141例化妆品接触性皮炎患者斑贴试验结果分析

    Institute of Scientific and Technical Information of China (English)

    焦红; 关蕾; 战静; 程树军; 毕英杰; 赖唯; 任美玲; 陈晓清


    (25.62%, 31/121). 123 cases were allergic to at least one antigen in 27 kinds of European standard series antigens, the total positive rate was 87.2%. The several antigens which caused the top high positive rate were: potassium dichromate (43.97%), nickel sulphate (43.26%), cobalt chloride (36.17%), mixture of hydroxy benzoic acid (23.40%), spices mixture (20.57%) , methyldibromo glutaronitrile (16.31%), 4-phenylenediamine base (15.60%), benzocaine (14.90%), formaldehyde (14.89%), 5-chloro-2-methyl-4-isothiazolin (13.48%), aromatic compounds II (10.64%). Conclusion Heavy metals, mixed preservatives and mixed spices in cosmetic raw materials are the possible allergens of cosmetic contact dermatitis.

  18. LD5o of the bacteria Aeromonas hydrophila to matrinxã, Brycon amazonicus DL5o da bactéria Aeromonas hydrophila para o matrinxã, Brycon amazonicus

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    Sarah Ragonha de Oliveira


    Full Text Available In order to determine the lethal dose (96-h LD50 of the bacteria Aeromonas hydrophila to matrinxã, Brycon amazonicus, to be applied in challenge tests, 90 fish (63.23 ± 6.39 g were divided into five treatments, with different bacterial solutions: T1 - Control (0.9% NaCl saline solution; T2 (4 x 10(11 cells/ mL; T3 (5 x 10(11 cells/ mL; T4 (1.36 x 10(12 cells/ mL and T5 (3.06 x 10(12 cells/ mL. Fish were previously anesthetized with benzocaine (60 mg L-1, inoculated in the peritoneal cavity with the bacterial suspensions and then distributed into fifteen 80-L test chambers, where the water variables were monitored and fish mortality was observed. The experiment was randomly designed in three replicates and the 96-h LD50 was estimated according to the trimmed Spearman-Karber method. Water quality variables remained within adequate ranges for fish health and performance. Fish mortality rate increased with the bacterial concentrations of A. hydrophila (T1 = 0%; T2 = 16.66%; T3 = 44.44%; T4 = 72.22% and T5 = 100%, and the first mortalities were observed after 57 h, although the signs of the bacterial infection were already observed 24 h after the inoculation. The results indicate that the 96-h LD50 value of A. hydrophila to matrinxã is 6.66 x 10(11 cells/ mL.Para determinar a dose letal (DL50 96-h da bactéria Aeromonas hydrophila para o matrinxã, Brycon amazonicus, com aplicabilidade para testes de desafio, foram utilizados 90 peixes (63,23 ± 6,39 g, divididos em cinco tratamentos, com diferentes soluções bacterianas: T1 - Controle (solução salina 0,9% NaCl; T2 (4 x 10(11 células/ mL; T3 (5 x 10(11 células/ mL-1; T4 (1,36 x 10(12 células/mL-1 e T5 (3,06 x 10(12 células/ mL-1. Os peixes foram previamente anestesiados com benzocaína (60 mg L-1, inoculados na cavidade peritoneal com as suspensões bacterianas e distribuídos em 15 aquários de vidro de 80 L de capacidade, com aeração constante. O experimento teve duração de 96 h, no