WorldWideScience

Sample records for tetracaine

  1. Tetracaine gel vs EMLA cream for percutaneous anaesthesia in children

    DEFF Research Database (Denmark)

    Rømsing, Janne; Henneberg, S W; Walther-Larsen, S

    1999-01-01

    We have evaluated the anaesthetic effect of tetracaine gel 1 g, applied for 45 min, compared with EMLA cream 2 g, applied for 60 min, in a randomized, double-blind study in 60 children aged 3-15 yr. Venous cannulation was performed 15 min after removal of the EMLA cream (n = 20) and tetracaine gel...... (n = 20). Cannulation was performed up to 215 min after removal of the tetracaine gel in another 20 patients. Significantly lower pain scores were recorded by the children treated with tetracaine gel compared with EMLA cream (P children in the tetracaine groups reported...... no pain compared with only 10% in the EMLA group. Only minor adverse effects were observed. We conclude that tetracaine gel provided effective, rapid, long-lasting and safe local anaesthesia, and was significantly better than EMLA cream in reducing pain during venous cannulation in children using...

  2. Tetracaine gel vs EMLA cream for percutaneous anaesthesia in children

    DEFF Research Database (Denmark)

    Rømsing, Janne; Henneberg, S W; Walther-Larsen, S

    1999-01-01

    We have evaluated the anaesthetic effect of tetracaine gel 1 g, applied for 45 min, compared with EMLA cream 2 g, applied for 60 min, in a randomized, double-blind study in 60 children aged 3-15 yr. Venous cannulation was performed 15 min after removal of the EMLA cream (n = 20) and tetracaine gel...... (n = 20). Cannulation was performed up to 215 min after removal of the tetracaine gel in another 20 patients. Significantly lower pain scores were recorded by the children treated with tetracaine gel compared with EMLA cream (P ... no pain compared with only 10% in the EMLA group. Only minor adverse effects were observed. We conclude that tetracaine gel provided effective, rapid, long-lasting and safe local anaesthesia, and was significantly better than EMLA cream in reducing pain during venous cannulation in children using...

  3. Heated lidocaine/tetracaine patch (Synera™, Rapydan™) compared with lidocaine/prilocaine cream (EMLA®) for topical anaesthesia before vascular access

    National Research Council Canada - National Science Library

    Sawyer, J; Febbraro, S; Masud, S; Ashburn, M. A; Campbell, J. C

    2009-01-01

    Background We compared the lidocaine/tetracaine patch [Synera™ (USA), Rapydan™ (Europe)], a novel heat-aided patch using a eutectic mixture of lidocaine 70 mg and tetracaine 70 mg, with a eutectic mixture of lidocaine 25 mg ml...

  4. Topical local anesthesia: focus on lidocaine–tetracaine combination

    Directory of Open Access Journals (Sweden)

    Giordano D

    2015-11-01

    Full Text Available Davide Giordano,1 Maria Gabriella Raso,2 Carmine Pernice,1 Vanni Agnoletti,3 Verter Barbieri1 1Otorhinolaryngology Unit, Department of Surgery, Arcispedale Santa Maria Nuova – IRCCS, Reggio Emilia, 2Anesthesiology, Intensive Care, and Pain Medicine Unit, Department of Surgical Sciences, University Hospital of Parma, Parma, 3Anesthesiology and Intensive Care Unit, Department of Cardiology, Thoracic and Vascular Surgery, and Critical Care Medicine, Arcispedale Santa Maria Nuova – IRCCS, Reggio Emilia, Italy Abstract: In recent years, the popularity of aesthetic and cosmetic procedures, often performed in outpatient settings, has strongly renewed interest in topical anesthetics. A number of different options are widely used, alone or in combination, in order to minimize the pain related to surgery. Moreover, interest in local anesthetics in the treatment of some painful degenerative conditions such as myofascial trigger point pain, shoulder impingement syndrome, or patellar tendinopathy is increasing. Numerous clinical trials have shown that lidocaine–tetracaine combination, recently approved for adults aged 18 or older, is effective and safe in managing pain. The present paper gives an overview of the recent literature regarding the efficacy and safety of lidocaine–tetracaine combination use. Keywords: lidocaine, tetracaine, local anesthetics, efficacy, safety

  5. The effects of tetracaine on charge movement in fast twitch rat skeletal muscle fibres.

    Science.gov (United States)

    Hollingworth, S; Marshall, M W; Robson, E

    1990-02-01

    1. The effects of tetracaine, a local anaesthetic that inhibits muscle contraction, on membrane potential and intramembrane charge movements were investigated in fast twitch rat muscle fibres (extensor digitorum longus). 2. The resting membrane potentials of surface fibres from muscles bathed in isotonic Ringer solution containing 2 mM-tetracaine were well maintained, but higher concentrations of tetracaine caused a time-dependent fall of potential. Muscle fibres bathed in hypertonic solutions containing 2 mM-tetracaine were rapidly depolarized. In both isotonic and hypertonic solutions, the depolarizing effect of tetracaine could not be reversed. 3. Charge movement measurements were made using the middle-of-the-fibre voltage clamp technique. The voltage dependence of charge movements measured in cold isotonic solutions was well fitted by a Boltzmann distribution (Q(V) = Qmax/(1 + exp(-(V-V)/k] where Qmax = 37.3 +/- 2.8 nC muF-1, V = -17.9 +/- 1.2 mV and k = 12.6 +/- 0.8 mV (n = 6, 2 degrees C; means +/- S.E. of means). Similar values were obtained when 2 mM-tetracaine was added to the isotonic bathing fluid (Qmax = 40.6 +/- 2.3 nC microF-1, V = -14.1 +/- 1.3 mV, k = 15.3 +/- 0.8 mV; n = 8, 2 degrees C). 4. Charge movements measured around mechanical threshold in muscle fibres bathed in hypertonic solutions were reduced when 2 mM-tetracaine was added to the bathing fluid. The tetracaine-sensitive component of charge was well fitted with an unconstrained Boltzmann distribution which gave: Qmax = 7.5 nC microF-1, V = -46.5 mV, k = 5.5 mV. The e-fold rise of the foot of the curve was 9.3 mV.

  6. 21 CFR 524.1484b - Neomycin sulfate, isoflupredone acetate, tetracaine hydrochloride, and myristyl-gamma-picolinium...

    Science.gov (United States)

    2010-04-01

    ..., tetracaine hydrochloride, and myristyl-gamma-picolinium chloride, topical powder. 524.1484b Section 524.1484b... Neomycin sulfate, isoflupredone acetate, tetracaine hydrochloride, and myristyl-gamma-picolinium chloride... hydrochloride and .2 milligram of myristyl-gamma-picolinium chloride in each gram of the product in a special...

  7. Concentration-dependent effects of tetracaine on excitation-contraction coupling in frog skeletal muscle fibres.

    Science.gov (United States)

    Sárközi, S; Szentesi, P; Cseri, J; Kovács, L; Csernoch, L

    1996-12-01

    The effects of low (10-100 microM) concentrations of tetracaine on intermembrane charge movement and on the rate of calcium release (Rrel) from the sarcoplasmic reticulum (SR) were studied in cut skeletal muscle fibres of the frog using the voltage clamp technique. The fibres were mounted in a single or double vaseline gap chamber to study the events near the contraction threshold or in a wide membrane potential range. Although the 'hump' component of charge movement (Q gamma) was suppressed to some extent, the voltage dependence and the parameters of the Boltzmann distribution were not modified significantly at tetracaine concentrations below 50 microM. At 50 and 100 microM of tetracaine the midpoint voltage of the Boltzmann distribution was shifted to higher membrane potentials and the steepness was decreased. The total available charge remained the same at all concentrations tested. Using fura-2 to measure calcium transients at 100 microM tetracaine the threshold for calcium release was found to be significantly shifted to more positive membrane potentials. Tetracaine reversibly suppressed both the early inactivating peak and the steady-level of Rrel but the concentration dependence of the effects was markedly different. The inactivation component of calcium release was decreased with a Hill coefficient of approximately 1 and half effective concentration of 11.8 microM while the steady-level was decreased with a Hill coefficient of greater than 2 and a half effective concentration of 47.0 microM. These results favour two sites of action where tetracaine would suppress the calcium release from the SR.

  8. Prospective, randomized, contralateral eye comparison of tetracaine and proparacaine for pain control in laser in situ keratomileusis and photorefractive keratectomy

    Directory of Open Access Journals (Sweden)

    Moshirfar M

    2014-06-01

    Full Text Available Majid Moshirfar,1 Mark D Mifflin,1 Michael V McCaughey,2 Adam J Gess1 1John A Moran Eye Center, University of Utah, Salt Lake City, UT, USA; 2University of New Mexico School of Medicine, Albuquerque, NM, USA Background: Tetracaine and proparacaine are two of the most commonly used medications for providing topical anesthesia in laser in situ keratomileusis (LASIK and photorefractive keratectomy (PRK. These agents have not been previously compared in a prospective manner to determine their efficacy in these settings. Methods: This prospective, single-masked, randomized study comprised 256 eyes from 128 consecutive patients being treated with LASIK or PRK who were randomized to receive tetracaine in one eye and proparacaine in the other. The patients were blinded as to which anesthetic agent was used in each eye. Pain levels were graded on a 0–10 scale, and were assessed upon instillation, during surgery, immediately postoperatively, 30 minutes postoperatively, overnight, and on postoperative day 1. Patients were asked 30 minutes after surgery which anesthetic agent they would choose. Results: Both anesthetic agents resulted in diminished amounts of subjective pain in patients undergoing LASIK and PRK. Tetracaine caused significantly more pain upon instillation than proparacaine for both LASIK and PRK patients. LASIK patients noted significantly less pain 30 minutes after surgery when treated with tetracaine. Significantly more LASIK patients preferred the eye treated with tetracaine. These differences were not present in the PRK group. Conclusion: Both tetracaine and proparacaine are effective methods of topical anesthesia in LASIK and PRK. Tetracaine caused significantly more pain upon instillation in all patients, but resulted in greater analgesia 30 minutes after surgery in the LASIK group. Patients in the LASIK group expressed a preference for tetracaine over proparacaine. There was no significant drop preference among PRK patients

  9. Tetracaine – selective electrodes with polymer membranes and their application in pharmaceutical formulation control

    Directory of Open Access Journals (Sweden)

    Ahmed Khudhair Hassan

    2017-02-01

    Full Text Available The construction and electrochemical response characteristics of poly(vinyl chloride (PVC membrane electrodes for tetracaine hydrochloride (TCH are described. The sensing membranes incorporating ion-association complexes of tetracaine cation with phosphotungstic acid (PTA or phosphomolybdic acid (PMA or Sodium tetraphenyl borate (NaTPB as electroactive materials and di-n-butyl phthalate (DBPH or tri-n-butyl phosphate (TBP as a plasticizer in PVC matrixes were evaluated. The results obtained show the electrodes based on PTA or PMA as electroactive compounds and DBPH as plasticizer with a fast, stable and near-Nernstian response over a wide concentration range (1 × 10−5–5 × 10−2 M, with cationic slopes of 55.02 and 52.05 mV decade−1 over a pH range of (2.5–6.5. The electrodes show good discrimination of tetracaine from several inorganic cations and sugars. The electrodes were successfully applied for the determination of tetracaine in pharmaceutical formulations.

  10. 21 CFR 524.1484k - Neomycin sulfate, prednisolone, tetracaine, and squalane topical-otic suspension.

    Science.gov (United States)

    2010-04-01

    ... squalane topical-otic suspension. 524.1484k Section 524.1484k Food and Drugs FOOD AND DRUG ADMINISTRATION... TOPICAL DOSAGE FORM NEW ANIMAL DRUGS § 524.1484k Neomycin sulfate, prednisolone, tetracaine, and squalane..., and 0.25 milliliter squalane. (b) Sponsor. See 017030 in § 510.600(c) of this chapter. (c) Conditions...

  11. Study of procaine and tetracaine in the lipid bilayer using molecular dynamics simulation.

    Science.gov (United States)

    Jalili, Seifollah; Saeedi, Marzieh

    2017-04-01

    Despite available experimental results, the molecular mechanism of action of local anesthetics upon the nervous system and contribution of the cell membrane to the process are still controversial. In this work, molecular dynamics simulations were performed to investigate the effect of two clinically used local anesthetics, procaine and tetracaine, on the structure and dynamics of a fully hydrated dimyristoylphosphatidylcholine lipid bilayer. We focused on comparing the main effects of uncharged and charged drugs on various properties of the lipid membrane: mass density distribution, diffusion coefficient, order parameter, radial distribution function, hydrogen bonding, electrostatic potential, headgroup angle, and water dipole orientation. To compare the diffusive nature of anesthetic through the lipid membrane quantitatively, we investigated the hexadecane/water partition coefficient using expanded ensemble simulation. We predicted the permeability coefficient of anesthetics in the following order: uncharged tetracaine > uncharged procaine > charged tetracaine > charged procaine. We also shown that the charged forms of drugs are more potent in hydrogen bonding, disturbing the lipid headgroups, changing the orientation of water dipoles, and increasing the headgroup electrostatic potential more than uncharged drugs, while the uncharged drugs make the lipid diffusion faster and increase the tail order parameter. The results of these simulation studies suggest that the different forms of anesthetics induce different structural modifications in the lipid bilayer, which provides new insights into their molecular mechanism.

  12. Heated lidocaine/tetracaine patch for treatment of patellar tendinopathy pain

    Directory of Open Access Journals (Sweden)

    Gammaitoni AR

    2013-07-01

    Full Text Available Arnold R Gammaitoni,1 Henry T Goitz,2 Stephanie Marsh,2 Thomas B Marriott,3 Bradley S Galer1 1Pain Group, Nuvo Research US, West Chester, PA, USA; 2Sports Medicine, Detroit Medical Center, Warren, MI, USA; 3Pain Group, Nuvo Research US, Salt Lake City, UT, USA Introduction: The pain of patellar tendinopathy (PT may be mediated by neuronal glutamate and sodium channels. Lidocaine and tetracaine block both of these channels. This study tested the self-heated lidocaine-tetracaine patch (HLT patch in patients with PT confirmed by physical examination to determine if the HLT patch might relieve pain and improve function. Methods: Thirteen patients with PT pain of ≥14 days' duration and baseline average pain scores ≥4 (on a 0–10 scale enrolled in and completed this prospective, single-center pilot study. Patients applied one HLT patch to the affected knee twice daily for 2–4 hours for a total of 14 days. Change in average pain intensity and interference (Victorian Institute of Sport Assessment [VISA] scores from baseline to day 14 were assessed. No statistical inference testing was performed. Results: Average pain scores declined from 5.5 ± 1.3 (mean ± standard deviation at baseline to 3.8 ± 2.5 on day 14. Similarly, VISA scores improved from 45.2 ± 14.4 at baseline to 54.3 ± 24.5 on day 14. A clinically important reduction in pain score (≥30% was demonstrated by 54% of patients. Conclusion: The results of this pilot study suggest that topical treatment that targets neuronal sodium and glutamate channels may be useful in the treatment of PT. Keywords: patellar tendinopathy, patellar tendinosis, heated lidocaine/tetracaine patch, topical analgesic patch, knee pain

  13. Oxidation of Tetracaine Hydrochloride by Chloramine-B in Acid Medium: Kinetic Modeling

    Directory of Open Access Journals (Sweden)

    Jayachamarajapura Pranesh Shubha

    2014-01-01

    Full Text Available Tetracaine hydrochloride (TCH is one of the potent local anaesthetics. A kinetic study of oxidation of tetracaine hydrochloride by sodium N-chlorobenzenesulfonamide (chloramine-B or CAB has been carried in HClO4 medium at 303 K. The rate shows first-order dependence on [CAB]o, shows fractional–order dependence on [substrate]o, and is self-governing on acid concentration. Decrease of dielectric constant of the medium, by adding methanol, increased the rate. Variation of ionic strength and addition of benzenesulfonamide or NaCl have no significant effect on the rate. The reaction was studied at different temperatures and the activation parameters have been evaluated. The stoichiometry of the reaction was found to be 1 : 5 and the oxidation products were identified by spectral analysis. The conjugate free acid C6H5SO2NHCl of CAB is postulated as the reactive oxidizing species. The observed results have been explained by plausible mechanism and the related rate law has been deduced.

  14. Differential sensitivity to perchlorate and caffeine of tetracaine-resistant Ca2+ release in frog skeletal muscle.

    Science.gov (United States)

    Píriz, Nazira; Brum, Gustavo; Pizarro, Gonzalo

    2006-01-01

    In voltage clamped frog skeletal muscle fibres 0.2 mM tetracaine strongly suppresses Ca(2+) release. After this treatment Ca(2+) release flux lacks its characteristic initial peak and the remaining steady component is strongly reduced when compared with the control condition. We studied the effect of two agonists of Ca(2+) release on these tetracaine treated fibres. 8 mM ClO(4)(-) added after tetracaine potentiated release flux from 0.11 +/- 0.03 mM s(-1) to 0.34 +/- 0.07 mM s(-1) (n = 6) although without recovery of the peak at any test voltage. The voltage dependence of the increased release was shifted towards more negative potentials (approximately -10 mV). The effects of ClO(4)(-) on charge movement under these conditions showed the previously described characteristic changes consisting in a left shift of its voltage dependence (approximately -9 mV) together with a slower kinetics, both at the ON and OFF transients. Caffeine at 0.5 mM in the presence of the same concentration of tetracaine failed to potentiate release flux independently of the test voltage applied. When the cut ends of the fibre were exposed to a 10 mM BAPTA intracellular solution, in the absence of tetracaine, the peak was progressively abolished. Under these conditions caffeine potentiated release restoring the peak (from 0.63 +/- 0.12 mM s(-1) to 1.82 +/- 0.23 mM s(-1)) with no effect on charge movement. Taken together the present results suggest that tetracaine is blocking a Ca(2+) sensitive component of release flux. It is speculated that the suppressed release includes a component that is dependent on Ca(2+) and mainly mediated by the activation of the beta ryanodine receptors (the RyR3 equivalent isoform). These receptors are located parajunctionally in the frog and are not interacting with the dihydropyridine receptor.

  15. Characterization and comparison of lidocaine-tetracaine and lidocaine-camphor eutectic mixtures based on their crystallization and hydrogen-bonding abilities.

    Science.gov (United States)

    Gala, Urvi; Chuong, Monica C; Varanasi, Ravi; Chauhan, Harsh

    2015-06-01

    Eutectic mixtures formed between active pharmaceutical ingredients and/or excipients provide vast scope for pharmaceutical applications. This study aimed at the exploration of the crystallization abilities of two eutectic mixtures (EM) i.e., lidocaine-tetracaine and lidocaine-camphor (1:1 w/w). Thermogravimetric analysis (TGA) for degradation behavior whereas modulated temperature differential scanning calorimetry (MTDSC) set in first heating, cooling, and second heating cycles, was used to qualitatively analyze the complex exothermic and endothermic thermal transitions. Raman microspectroscopy characterized vibrational information specific to chemical bonds. Prepared EMs were left at room temperature for 24 h to visually examine their crystallization potentials. The degradation of lidocaine, tetracaine, camphor, lidocaine-tetracaine EM, and lidocaine-camphor EM began at 196.56, 163.82, 76.86, 146.01, and 42.72°C, respectively, which indicated that eutectic mixtures are less thermostable compared to their individual components. The MTDSC showed crystallization peaks for lidocaine, tetracaine, and camphor at 31.86, 29.36, and 174.02°C, respectively (n = 3). When studying the eutectic mixture, no crystallization peak was observed in the lidocaine-tetracaine EM, but a lidocaine-camphor EM crystallization peak was present at 18.81°C. Crystallization occurred in lidocaine-camphor EM after being kept at room temperature for 24 h, but not in lidocaine-tetracaine EM. Certain peak shifts were observed in Raman spectra which indicated possible interactions of eutectic mixture components, when a eutectic mixture was formed. We found that if the components forming a eutectic mixture have crystallization peaks close to each other and have sufficient hydrogen-bonding capability, then their eutectic mixture is least likely to crystallize out (as seen in lidocaine-tetracaine EM) or vice versa (lidocaine-camphor EM).

  16. Effect of tetracaine on DMPC and DMPC+cholesterol biomembrane models: liposomes and monolayers.

    Science.gov (United States)

    Serro, A P; Galante, R; Kozica, A; Paradiso, P; da Silva, A M P S Gonçalves; Luzyanin, K V; Fernandes, A C; Saramago, B

    2014-04-01

    Different types of lipid bilayers/monolayers have been used to simulate the cellular membranes in the investigation of the interactions between drugs and cells. However, to our knowledge, very few studies focused on the influence of the chosen membrane model upon the obtained results. The main objective of this work is to understand how do the nature and immobilization state of the biomembrane models influence the action of the local anaesthetic tetracaine (TTC) upon the lipid membranes. The interaction of TTC with different biomembrane models of dimyristoylphosphatidylcholine (DMPC) with and without cholesterol (CHOL) was investigated through several techniques. A quartz crystal microbalance with dissipation (QCM-D) was used to study the effect on immobilized liposomes, while phosphorus nuclear magnetic resonance ((31)P-NMR) and differential scanning calorimetry (DSC) were applied to liposomes in suspension. The effect of TTC on Langmuir monolayers of lipids was also investigated through surface pressure-area measurements at the air-water interface. The general conclusion was that TTC has a fluidizing effect on the lipid membranes and, above certain concentrations, induces membrane swelling or even solubilization. However, different models led to variable responses to the TTC action. The intensity of the disordering effect caused by TTC increased in the following order: supported liposomes

  17. Self-initiated and concentration-dependent degradation of tetracaine in neat standard solutions: A trouble-shooting story.

    Science.gov (United States)

    Tan, Aimin; Wu, Yanxin; Gu, Guifen; Fanaras, John C

    2016-10-15

    This paper presents the trouble-shooting for a very unusual stability case. Tetracaine was found unstable in neat solutions only at high concentrations, but not at low concentrations. Moreover, its stable-isotope labeled internal standard did not show similar behavior. A series of trouble-shooting experiments were conducted to uncover the root cause. Some generally applicable precautions/insights can be drawn from this investigation to avoid potential stability issues during bioanalytical method development and validation. Copyright © 2016 Elsevier B.V. All rights reserved.

  18. First-time success with needle procedures was higher with a warm lidocaine and tetracaine patch than an eutectic mixture of lidocaine and prilocaine cream.

    Science.gov (United States)

    Cozzi, Giorgio; Borrometi, Fabio; Benini, Franca; Neri, Elena; Rusalen, Francesca; Celentano, Loredana; Zanon, Davide; Schreiber, Silvana; Ronfani, Luca; Barbi, Egidio

    2017-05-01

    More than 50% of children report apian during venepuncture or intravenous cannulation and using local anaesthetics before needle procedures can lead to different success rates. This study examined how many needle procedures were successful at the first attempt when children received either a warm lidocaine and tetracaine patch or an eutectic mixture of lidocaine and prilocaine (EMLA) cream. We conducted this multicentre randomised controlled trial at three tertiary-level children's hospitals in Italy in 2015. Children aged three to 10 years were enrolled in an emergency department, paediatric day hospital and paediatric ward and randomly allocated to receive a warm lidocaine and tetracaine patch or EMLA cream. The primary outcome was the success rate at the first attempt. The analysis included 172 children who received a warm lidocaine and tetracaine patch and 167 who received an EMLA cream. The needle procedure was successful at the first attempt in 158 children (92.4%) who received the warm patch and in 142 children (85.0%) who received the cream (p = 0.03). The pain scores were similar in both groups. This study showed that the first-time needle procedure success was 7.4% higher in children receiving a warm lidocaine and tetracaine patch than EMLA cream. ©2017 Foundation Acta Paediatrica. Published by John Wiley & Sons Ltd.

  19. How effective is tetracaine 4% gel, before a venipuncture, in reducing procedural pain in infants: a randomized double-blind placebo controlled trial

    Directory of Open Access Journals (Sweden)

    Sherlock Rebecca

    2007-02-01

    Full Text Available Abstract Background Procedural pain relief is sub-optimal in neonates. Topical tetracaine provides pain relief in children. Evidence of its efficacy and safety in neonates is limited. The objective of this study was to assess the efficacy and safety of topical tetracaine on the pain response of neonates during a venipuncture. Methods Medically stable infants greater than or equal to 24 weeks gestation, requiring a venipuncture, were included. Following randomization and double blinding, 1.1 g of tetracaine or placebo was applied to the skin for 30 minutes. Participants received oral sucrose if they met local eligibility criteria. The venipuncture was performed according to a standard protocol. A medium effect size in the pain score (corresponding to about 2 point difference in the PIPP score was considered clinically significant, leading to a sample size of 142 infants, with 80% statistical power. Local skin reactions and immediate adverse cardiorespiratory events were noted. The primary outcome, PIPP score at 1 minute, was analysed using an independent Student's t-test. Results One hundred and forty two infants were included, 33 +/- 4 weeks gestation, 2100 +/- 900 grams and 6 +/- 3 days of age. There was almost no difference in PIPP scores at 1 minute between groups (mean difference -0.09; 95% confidence interval [CI]: -1.68 to 1.50; P = . 91. Similarly, there were no differences in PIPP scores during the 2nd, 3rd and 4th minute. Duration of cry did not differ between the groups (median difference, 0; 95% CI, -3 to 0; P = . 84. The majority of infants in both groups received sucrose 24%. Sucrose had a significant effect on the PIPP score, as assessed by an ANOVA model (p = 0.0026. Local skin erythema was observed transiently in 11 infants (7 in the tetracaine and 4 in the placebo group. No serious side effect was observed. Conclusion Tetracaine did not significantly decrease procedural pain in infants undergoing a venipuncture, when used in

  20. How effective is tetracaine 4% gel, before a peripherally inserted central catheter, in reducing procedural pain in infants: a randomized double-blind placebo controlled trial [ISRCTN75884221

    Directory of Open Access Journals (Sweden)

    Blanchard Colline

    2006-05-01

    Full Text Available Abstract Background Procedural pain relief is sub-optimal in infants, especially small and vulnerable ones. Tetracaine gel 4% (Ametop®, Smith-Nephew provides pain relief in children and larger infants, but its efficacy in smaller infants and for peripherally inserted central catheters (PICC remains uncertain. The objective of this trial was to assess the safety and efficacy of tetracaine gel on the pain response of very low birth weight (VLBW infants during insertion of a PICC. Methods Medically stable infants greater than or equal to 24 weeks gestation, requiring a non-urgent PICC, were included. Following randomization and double blinding, 1.1 g of tetracaine or placebo was applied to the skin for 30 minutes. The PICC was inserted according to a standard protocol. Pain was assessed using the Premature Infant Pain Profile (PIPP. A 3-point change in the pain score was considered clinically significant, leading to a sample size of 54 infants, with 90% statistical power. Local skin reactions and immediate adverse cardiorespiratory events were noted. The primary outcome, PIPP score at 1 minute, was analysed using an independent Student's t-test. Results Fifty-four infants were included, 27 +/- 2 weeks gestation, 916 +/- 292 grams and 6.5 +/- 3.2 days of age. Baseline characteristics were similar between groups. The mean PIPP score in the first minute was 10.88 in the treatment group as compared to 11.74 in the placebo group (difference 0.86, 95% CI -1.86, 3.58. Median duration of crying in non-intubated infants was 181 seconds in the tetracaine group compared to 68 seconds in the placebo group (difference -78, 95% CI -539, 117. Local skin erythema was observed transiently in 4 infants (3 in the treatment and 1 in the placebo group. No serious harms were observed. Conclusion Tetracaine 4% when applied for 30 minutes was not beneficial in decreasing procedural pain associated with a PICC in very small infants.

  1. Predicting Response to Subacromial Injections and Lidocaine/Tetracaine Patch from Pretreatment Pain Quality in Patients with Shoulder Impingement Syndrome.

    Science.gov (United States)

    Gammaitoni, Arnold R; Trudeau, Jeremiah J; Radnovich, Richard; Galer, Bradley S; Jensen, Mark P

    2015-07-01

    No existing pain treatment is effective for all pain problems, and response to pain treatment is highly variable. Knowledge regarding the patient factors that predict response to different treatments could benefit patients by providing an empirical foundation for patient-treatment matching. This study sought to test the hypothesis that improvements following two treatments thought to operate via similar mechanisms would be predicted by similar baseline pain qualities. Prospective prediction analysis using data from a previously published open label trial comparing a heated lidocaine/tetracaine patch versus subacromial corticosteroid injection for the treatment of pain in individuals with shoulder impingement syndrome. Consistent with the study hypothesis, the response to the two treatments were predicted by similar baseline pain qualities; specifically, higher baseline levels of unpleasant, electric, and sensitive pain predicted subsequent improvements in sleep interference, work/activity interference, and patient global ratings of improvement, respectively. The findings are consistent with the combined ideas that (1) those who have the most to gain (i.e., those reporting the highest levels of various pain qualities) can expect the best response to effective treatments and (2) different pain qualities may be associated with different types of outcomes. The findings support further research to examine how pain quality measures may be used to improve patient-treatment matching, and therefore, ultimately improve the efficiency, efficacy, and overall benefit-risk of pain treatment. Wiley Periodicals, Inc.

  2. Determination of tear break-up time reference values and ocular tolerance of tetracaine hydrochloride eyedops in healthy horses.

    Science.gov (United States)

    Monclin, S J; Farnir, F; Grauwels, M

    2011-01-01

    Tetracaine hydrochloride (THCl) has been reported to cause irritation in dogs. In man, some topical anaesthetics have been shown to disrupt the tear film. Tear break-up time (TBUT) is a useful test allowing an assessment of the quality of the precorneal tear film. Only one TBUT value has been reported in horses with no information on the technique used. To provide a method for performing the TBUT in horses and to report any side effects of a single application of THCl in clinically normal horses, particularly on the stability of the tear film. In Study 1, one drop of 0.5 or 1% THCl was applied to one eye of 20 horses divided in 2 groups. Treated eyes were assessed for the development of side effects 2.5 and 5 min after treatment. In Study 2, the TBUT was measured in both eyes of 2 groups of 10 horses, before and 2.5 and 5 min after, instillation of one drop of either 0.5 or 1% THCl. No animals developed any ocular side effect after instillation. Basal TBUT was 8.3±1.3 s. TBUT decreased from baseline 5 and 2.5 min after application of one drop of 0.5% THCl and one drop of 1% THCl, respectively. A technique to measure the TBUT in healthy horses is described and normal range values that could be used as a reference were obtained. THCl is well tolerated in horses but lowers the TBUT. © 2010 EVJ Ltd.

  3. Comparison of lidocaine/tetracaine cream and lidocaine/prilocaine cream for local anaesthesia during laser treatment of acne keloidalis nuchae and tattoo removal: Results of two randomized controlled trials

    NARCIS (Netherlands)

    K. Greveling (Karin); E.P. Prens (Errol); ten Bosch, N.; M.B.A. van Doorn (Martijn)

    2017-01-01

    textabstractBackground: Pain is a common adverse effect of dermatological laser procedures. Currently, no standard topical anaesthetic cream exists for deeper dermal laser procedures. Objectives: To compare the efficacy of lidocaine/tetracaine cream and lidocaine/prilocaine cream in reducing

  4. Effectiveness of a heated lidocaine/tetracaine topical patch for pain associated with myofascial trigger points: results of an open-label pilot study.

    Science.gov (United States)

    Rauck, Richard; Busch, Michael; Marriott, Thomas

    2013-09-01

    Evaluate potential usefulness of a heated lidocaine/tetracaine topical patch for treatment for pain associated with myofascial trigger points (MTPs). Depth and duration of analgesia when patch is used as indicated, on intact skin to provide local dermal analgesia for superficial venous access and dermatologic procedures, suggest utility in relief of MTP-associated pain. In this open-label, single-center outpatient pilot study, patients with ≥ 1-month history of pain associated with up to 3 MTPs and average pain intensity ≥ 4 on 11-point scale applied 1 patch to each MTP for 4 hours twice daily for 2 weeks, followed by 2 weeks with no treatment. Patients continued prescribed analgesic dosing regimens. Twenty patients enrolled; 17 completed the study. At baseline, mean ± SD average pain intensity was 6.3 ± 1.56. This decreased by 33% to 4.5 ± 2.31 (N = 20) at the end of treatment; 40% of patients had clinically significant (≥ 30%) decrease, and 25% had substantial (≥ 50%) decrease. Pain interference with general activity, mood, normal work, and enjoyment of life decreased by ≥ 50% in 35% of patients; and with walking, sleep, and relationship by ≥ 50% in 50% of patients (N = 20). Worst trigger point sensitivity improved in 45% of patients; 75% were satisfied or very satisfied with treatment; none required rescue medication. Two weeks after stopping treatment, average pain intensity was 5.0 ± 2.04; treatment benefit was maintained in 8 (40%) patients. The most common adverse event was erythema. The heated lidocaine/tetracaine patch has potential utility as a noninvasive pharmacologic approach for managing MTP pain. Further studies are warranted. © 2012 The Authors Pain Practice © 2012 World Institute of Pain.

  5. A randomized clinical study of the heated lidocaine/tetracaine patch versus subacromial corticosteroid injection for the treatment of pain associated with shoulder impingement syndrome

    Directory of Open Access Journals (Sweden)

    Radnovich R

    2014-12-01

    Full Text Available Richard Radnovich,1 Jeremiah Trudeau,2 Arnold R Gammaitoni3 1Injury Care Medical Center, Boise, ID, USA; 2Analgesic Solutions, Natick, MA, USA; 3Nuvo Research Inc., West Chester, PA, USA Background: Treatment for pain due to shoulder impingement syndrome (SIS typically begins conservatively with nonsteroidal anti-inflammatory drugs and physical therapy and can include subacromial injection of corticosteroids, particularly in patients unresponsive to conservative measures. The heated lidocaine/tetracaine (HLT patch has been reported to reduce SIS pain in a small case series. Methods: This was a prospective, randomized, open-label clinical trial in which adult patients with SIS pain lasting at least 14 days, with an average intensity of ≥4 on a 0–10 scale (0= no pain, 10= worst pain were randomized to treatment with the HLT patch or a single subacromial injection of triamcinolone acetonide (10 mg. Patients in the HLT patch group applied a single HLT patch to the shoulder for 4 hours twice daily, with a 12-hour interval between treatments during the first 14 days, and could continue to use the patch on an as-needed basis (up to twice daily during the second 14-day period. No treatment was allowed in the final 14-day period. At baseline and at days 14, 28, and 42, patients rated their pain and pain interference with specific activities (0–10 scale. Results: Sixty patients enrolled in the study (average age =51 years, range 18–75, n=21 female. Average pain scores declined from 6.0±1.6 at baseline to 3.5±2.4 at day 42 in the HLT patch group (n=29, P<0.001 and from 5.6±1.2 to 3.2±2.6 in the injection group (n=31, P<0.001. Similar improvements were seen in each group for worst pain; pain interference with general activity, work, or sleep; and range of motion. No significant between-group differences were seen for any pain or pain interference scores at any time point. Conclusion: These results suggest that short-term, noninvasive treatment

  6. Lidocaine/tetracaine peel in topical anesthesia prior to laser-assisted hair removal: Phase-II and Phase-III study results.

    Science.gov (United States)

    Alster, Tina; Garden, Jerome; Fitzpatrick, Richard; Rendon, Marta; Sarkany, Marlis; Adelglass, Jeffrey

    2014-04-01

    Patient comfort is essential during dermatologic procedures. To evaluate anesthetic efficacy in laser-assisted hair removal of a self-occluding topical anesthetic (lidocaine 70 mg/g and tetracaine 70 mg/g, "LT peel"), which air-dries and can be peeled off 30 min post-application. Studies A (Phase-II) and B (Phase-III) were randomized, double-blind, placebo-controlled and paired. Applications of LT peel and placebo were concurrent: in Study A, 60 subjects were randomized to 30, 45, or 60-min groups, and in Study B, 50 subjects had 30-min applications. After drug removal, the investigator assessed for erythema, edema, and blanching. Efficacy evaluations followed the procedure: subject's pain [Visual Analog Scale (VAS), no to worst pain (0 - 100)], subject's/investigator's impression of anesthetic adequacy, and investigator's pain ratings. Adverse events (AEs) were recorded. VAS scores were significantly lower (p peel: mean scores were 26.7 for LT Peel vs. 44.3 for placebo (Study A total population, similar between application times) and 23 vs. 31.7 (Study B), respectively. For both studies, subject's/investigator's ratings favored LT peel (p peel. After a 30-min application, LT peel was effective and well-tolerated in providing anesthesia for laser-assisted hair removal.

  7. The pain quality response profile of a corticosteroid injections and heated lidocaine/tetracaine patch in the treatment of shoulder impingement syndrome.

    Science.gov (United States)

    Jensen, Mark P; Trudeau, Jeremiah J; Radnovich, Richard; Galer, Bradley S; Gammaitoni, Arnold R

    2015-04-01

    To describe the effects of 2 pain treatments for shoulder impingement syndrome (SIS), and illustrate how investigators can use pain quality information to understand treatment response differences. This study presents pain quality data from a randomized open-label study comparing the effects of an injection of triamcinolone and up to twice daily application of a heated lidocaine/tetracaine (Trilexis) patch in individuals with SIS. Study participants completed a measure of pain quality at baseline and again on study days 14, 28, and 42 following initiation of 2 treatments for SIS. Baseline and posttreatment pain quality scores were graphed to provide a visual representation of treatment-associated changes. Analyses of variance were used to examine the differences between treatment conditions in changes in pain quality with treatment. Both treatments resulted in substantial (and similar) pretreatment to posttreatment improvements in many pain qualities. However, differences in the time course of treatment effects were observed for itchy and heavy qualities. Although 2 different pain treatments appear to have the same effects when only pretreatment to posttreatment changes are examined, treatment differences emerged when the time course of treatment is examined. The findings support the importance of assessing both pain qualities and time course of treatment as outcome domains. The results illustrate how investigators can use data from clinical trials to provide a more fine-tuned description of treatment effects, providing knowledge that could be helpful in selecting treatment options at the individual patient level. Examination of the effects of pain treatments on pain qualities over time will help researchers and clinicians understand if certain pain quality domains respond faster to one treatment versus another, and may identify differences between treatments that would not be observed by measures of global pain intensity alone.

  8. An open-label pilot study evaluating the effectiveness of the heated lidocaine/tetracaine patch for the treatment of pain associated with carpal tunnel syndrome.

    Science.gov (United States)

    Nalamachu, Srinivas; Nalamasu, Rohit; Jenkins, Julie; Marriott, Thomas

    2014-09-01

    Carpal tunnel syndrome (CTS) is a common entrapment neuropathy of the median nerve at the wrist that is characterized by pain, paresthesias, weakness, and loss of dexterity. This pilot study was conducted to evaluate the heated lidocaine/tetracaine patch (HLT patch) as a conservative treatment for pain of CTS. Twenty adult patients (mean age = 44 ± 12 years) with pain secondary to unilateral CTS and electrodiagnostic evidence of mild-to-moderate CTS enrolled in this open-label study. Patients were treated with a single HLT patch placed over the junction of forearm and wrist on the palmar aspect of the wrist twice daily (morning and evening at 12-hour intervals) for 2 hours. At baseline and during the 2-week study, patients graded their pain intensity with an 11-point numerical rating scale (0 = no pain, 10 = worst imaginable pain). Pain interference with general activity, work, and sleep was evaluated with a similar 0-to-10-point scale. Fifteen patients completed the 14-day treatment period. Mean average pain intensity score decreased from 5.1 ± 1.5 at baseline to 2.5 ± 1.6 at end of study in the per-protocol population (P patch was generally well tolerated. The HLT patch resulted in clinically meaningful reduction in pain intensity in the majority of patients with mild-to-moderate CTS and may represent a targeted nonsurgical treatment for pain associated with CTS. © 2013 World Institute of Pain.

  9. A randomized clinical study of the heated lidocaine/tetracaine patch versus subacromial corticosteroid injection for the treatment of pain associated with shoulder impingement syndrome.

    Science.gov (United States)

    Radnovich, Richard; Trudeau, Jeremiah; Gammaitoni, Arnold R

    2014-01-01

    Treatment for pain due to shoulder impingement syndrome (SIS) typically begins conservatively with nonsteroidal anti-inflammatory drugs and physical therapy and can include subacromial injection of corticosteroids, particularly in patients unresponsive to conservative measures. The heated lidocaine/tetracaine (HLT) patch has been reported to reduce SIS pain in a small case series. This was a prospective, randomized, open-label clinical trial in which adult patients with SIS pain lasting at least 14 days, with an average intensity of ≥4 on a 0-10 scale (0= no pain, 10= worst pain) were randomized to treatment with the HLT patch or a single subacromial injection of triamcinolone acetonide (10 mg). Patients in the HLT patch group applied a single HLT patch to the shoulder for 4 hours twice daily, with a 12-hour interval between treatments during the first 14 days, and could continue to use the patch on an as-needed basis (up to twice daily) during the second 14-day period. No treatment was allowed in the final 14-day period. At baseline and at days 14, 28, and 42, patients rated their pain and pain interference with specific activities (0-10 scale). Sixty patients enrolled in the study (average age =51 years, range 18-75, n=21 female). Average pain scores declined from 6.0±1.6 at baseline to 3.5±2.4 at day 42 in the HLT patch group (n=29, Pwork, or sleep; and range of motion. No significant between-group differences were seen for any pain or pain interference scores at any time point. These results suggest that short-term, noninvasive treatment with the HLT patch has similar efficacy to subacromial corticosteroid injections for the treatment of pain associated with SIS.

  10. A randomized clinical study of the heated lidocaine/tetracaine patch versus subacromial corticosteroid injection for the treatment of pain associated with shoulder impingement syndrome

    Science.gov (United States)

    Radnovich, Richard; Trudeau, Jeremiah; Gammaitoni, Arnold R

    2014-01-01

    Background Treatment for pain due to shoulder impingement syndrome (SIS) typically begins conservatively with nonsteroidal anti-inflammatory drugs and physical therapy and can include subacromial injection of corticosteroids, particularly in patients unresponsive to conservative measures. The heated lidocaine/tetracaine (HLT) patch has been reported to reduce SIS pain in a small case series. Methods This was a prospective, randomized, open-label clinical trial in which adult patients with SIS pain lasting at least 14 days, with an average intensity of ≥4 on a 0–10 scale (0= no pain, 10= worst pain) were randomized to treatment with the HLT patch or a single subacromial injection of triamcinolone acetonide (10 mg). Patients in the HLT patch group applied a single HLT patch to the shoulder for 4 hours twice daily, with a 12-hour interval between treatments during the first 14 days, and could continue to use the patch on an as-needed basis (up to twice daily) during the second 14-day period. No treatment was allowed in the final 14-day period. At baseline and at days 14, 28, and 42, patients rated their pain and pain interference with specific activities (0–10 scale). Results Sixty patients enrolled in the study (average age =51 years, range 18–75, n=21 female). Average pain scores declined from 6.0±1.6 at baseline to 3.5±2.4 at day 42 in the HLT patch group (n=29, P<0.001) and from 5.6±1.2 to 3.2±2.6 in the injection group (n=31, P<0.001). Similar improvements were seen in each group for worst pain; pain interference with general activity, work, or sleep; and range of motion. No significant between-group differences were seen for any pain or pain interference scores at any time point. Conclusion These results suggest that short-term, noninvasive treatment with the HLT patch has similar efficacy to subacromial corticosteroid injections for the treatment of pain associated with SIS. PMID:25525385

  11. Utility of the heated lidocaine/tetracaine patch in the treatment of pain associated with shoulder impingement syndrome: a pilot study.

    Science.gov (United States)

    Radnovich, Richard; Marriott, Thomas B

    2013-01-01

    Pain control is an important first step in the treatment of shoulder impingement syndrome (SIS) because fear of pain must be removed as an obstacle to participation in an appropriate physical therapy program. Adult patients with SIS-associated pain of at least 2 weeks' duration and who had an average pain score of ≥4 on the zero- to ten-point Numeric Pain Rating Scale were eligible to enroll in this 2-week pilot study. Patients were treated with the heated lidocaine/tetracaine (70 mg/70 mg) patch (HLT patch) placed over the site of shoulder tenderness each morning and evening for a period of 2 to 4 hours. Average and worst pain during the previous 24 hours and shoulder range of motion were assessed at baseline and on Day 14. Results were expressed as change and percent change from baseline to Day 14. This pilot study was not powered for rigorous statistical analysis. Twenty patients (seven male, 13 female; average age 51.2 ± 10.8 years [mean ± standard deviation]) enrolled in this study, and 18 patients completed the protocol. The mean average pain score at baseline was 5.5 ± 1.1 (range 4 to 8). In the per-protocol population, average and worst pain scores declined by 2.4 ± 2.0 and 3.7 ± 2.7 points, respectively. Two-thirds of the patients demonstrated a clinically meaningful ≥30% decline in average pain score, and half of the patients demonstrated a ≥50% decline in average pain score. Shoulder internal rotation increased by 29.7° ± 21.8° and abduction increased by 40.0° ± 44.2°. Application-site erythema was reported by ten patients at some time during the study. Patients treated with the HLT patch for 14 days demonstrated clinically meaningful improvement in pain intensity and range of motion. Further controlled research is necessary to characterize the efficacy and tolerability of the HLT patch in the treatment of SIS.

  12. Utility of the heated lidocaine/tetracaine patch in the treatment of pain associated with shoulder impingement syndrome: a pilot study

    Directory of Open Access Journals (Sweden)

    Radnovich R

    2013-07-01

    Full Text Available Richard Radnovich,1 Thomas B Marriott21Injury Care Medical Center, Boise, ID, USA; 2Pain Group, Nuvo Research US, Salt Lake City, UT, USAIntroduction: Pain control is an important first step in the treatment of shoulder impingement syndrome (SIS because fear of pain must be removed as an obstacle to participation in an appropriate physical therapy program.Methods: Adult patients with SIS-associated pain of at least 2 weeks’ duration and who had an average pain score of ≥4 on the zero- to ten-point Numeric Pain Rating Scale were eligible to enroll in this 2-week pilot study. Patients were treated with the heated lidocaine/tetracaine (70 mg/70 mg patch (HLT patch placed over the site of shoulder tenderness each morning and evening for a period of 2 to 4 hours. Average and worst pain during the previous 24 hours and shoulder range of motion were assessed at baseline and on Day 14. Results were expressed as change and percent change from baseline to Day 14. This pilot study was not powered for rigorous statistical analysis.Results: Twenty patients (seven male, 13 female; average age 51.2 ± 10.8 years [mean ± standard deviation] enrolled in this study, and 18 patients completed the protocol. The mean average pain score at baseline was 5.5 ± 1.1 (range 4 to 8. In the per-protocol population, average and worst pain scores declined by 2.4 ± 2.0 and 3.7 ± 2.7 points, respectively. Two-thirds of the patients demonstrated a clinically meaningful ≥30% decline in average pain score, and half of the patients demonstrated a ≥50% decline in average pain score. Shoulder internal rotation increased by 29.7° ± 21.8° and abduction increased by 40.0° ± 44.2°. Application-site erythema was reported by ten patients at some time during the study.Conclusion: Patients treated with the HLT patch for 14 days demonstrated clinically meaningful improvement in pain intensity and range of motion. Further controlled research is necessary to characterize the

  13. Effects of some antianginal and vasodilating drugs on sodium influx and on the binding of 3H-batrachotoxinin-A 20-alpha-benzoate and 3H-tetracaine.

    Science.gov (United States)

    Velly, J; Grima, M; Marciniak, G; Spach, M O; Schwartz, J

    1987-02-01

    The effects of antianginal drugs, especially arylalkylamines and structurally related derivatives, on 3H-batrachotoxinin-A 20-alpha-benzoate (3H-BTX-B) binding and on 3H-tetracaine binding were studied on rat synaptosomal and heart membrane preparations. The effect of the same drugs on the Na+ influx induced by protoveratrine B was studied on the rat synaptosomal preparation. Antianginal drugs tested inhibited 3H-BTX-B binding in rat synaptosomes, arylalkylamine derivatives being the most potent: IC50 values were 27 nM for flunarizine, 32 nM for prenylamine, 79 nM for cinnarizine. Similarly, these drugs were the most potent when tested in cardiac membrane preparations. All the drugs tested were very weak inhibitors of 3H-tetracaine binding (IC50 ranging from 0.01 mM to more than 1 mM) except for guanabenz, which was more potent (IC50:0.3 microM on the synaptosomal preparation). The various drugs tested inhibited the 22Na+ influx induced by protoveratrine B, with IC50 values ranging from 15 microM (prenylamine) to 110 microM (verapamil), with the exception of nifedipine which had an IC50 of more than 0.1 mM. The inhibition of 22Na+ influx correlated well with the inhibition of 3H-BTX-B binding. These findings suggest that some antianginal drugs, especially the arylalkylamines may have, in addition to their calcium antagonist activity, direct effects on sodium channels.

  14. Drug: D04816 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D04816 Mixture, Drug Ethyl aminobenzoate - tetracaine hydrochloride - dibucaine hydr...ochloride - homosulfamine mixt; Prones-pasta aroma (TN) Etyl aminobenzoate [DR:D00552], Tetracaine hydrochl...oride [DR:D00741], Dibucaine hydrochloride [DR:D02220], Homosulfamine [DR:D04815] Therapeutic category: 2710... Therapeutic category of drugs in Japan [BR:br08301] 2 Agents affecting individua...l organs 27 Dental preparations 271 Local anesthetics 2710 Local anesthetics D04816 Ethyl aminobenzoate - tetracaine hydr

  15. Role of the bandage soft contact lens in the postoperative laser in situ keratomileusis patient.

    Science.gov (United States)

    Ahmed, I I; Breslin, C W

    2001-12-01

    To determine whether a bandage soft contact lens (BSCL) is routinely needed in the postoperative laser in situ keratomileusis (LASIK) patient and whether topical tetracaine 0.5% or diclofenac sodium 0.1% (Voltaren) is more effective in relieving patient discomfort than a BSCL. LCA-Vision Center, Toronto, Ontario, Canada. In this prospective randomized comparative study, all patients had bilateral simultaneous LASIK procedures. Post-LASIK patient comfort was evaluated through 3 arms of the study: BSCL versus no BSCL, 40 consecutive patients with 1 eye randomized to receive a BSCL and no BSCL in the fellow eye; BSCL versus tetracaine 0.5%, 26 consecutive patients with 1 eye randomized to receive a BSCL and tetracaine 0.5% in the fellow eye; tetracaine 0.5% versus Voltaren, 54 consecutive patients with 1 eye randomized to receive tetracaine 0.5% and Voltaren in the fellow eye. The patient preferences after LASIK were as follows: BSCL versus no BSCL-12 (30%) versus 23 (58%) (P =.062); BSCL versus tetracaine 0.5%-4 (15%) versus 22 (85%) (P <.001). On average, the eyes with no BSCL had a 2-line improvement in uncorrected visual acuity over the BSCL eyes. Tetracaine 0.5% versus Voltaren-13 (24%) versus 21 (39%) (P =.170). The routine use of a BSCL in the postoperative LASIK patient is not necessary. Voltaren and tetracaine 0.5% were safe and more effective in relieving postoperative patient discomfort and resulted in improved visual acuity immediately postoperatively.

  16. 21 CFR 310.527 - Drug products containing active ingredients offered over-the-counter (OTC) for external use as...

    Science.gov (United States)

    2010-04-01

    ... all other B-vitamins, dexpanthenol, estradiol and other topical hormones, jojoba oil, lanolin, nucleic... paraffinic hydrocarbons, tetracaine hydrochloride, urea, and wheat germ oil have been marketed as ingredients...

  17. The influence of non polar and polar molecules in mouse motile cells membranes and pure lipid bilayers.

    Directory of Open Access Journals (Sweden)

    Francisco J Sierra-Valdez

    Full Text Available We report an experimental study of mouse sperm motility that shows chief aspects characteristic of neurons: the anesthetic (produced by tetracaine and excitatory (produced by either caffeine or calcium effects and their antagonic action. While tetracaine inhibits sperm motility and caffeine has an excitatory action, the combination of these two substances balance the effects, producing a motility quite similar to that of control cells. We also study the effects of these agents (anesthetic and excitatory on the melting points of pure lipid liposomes constituted by 1,2-dipalmitoyl-sn-glycero-3-phosphocholine (DPPC and dipalmitoyl phosphatidic acid (DPPA. Tetracaine induces a large fluidization of the membrane, shifting the liposomes melting transition temperature to much lower values. The effect of caffeine is null, but its addition to tetracaine-doped liposomes greatly screen the fluidization effect. A high calcium concentration stiffens pure lipid membranes and strongly reduces the effect of tetracaine. Molecular Dynamics Simulations are performed to further understand our experimental findings at the molecular level. We find a strong correlation between the effect of antagonic molecules that could explain how the mechanical properties suitable for normal cell functioning are affected and recovered.

  18. Corneal biomechanical parameters and intraocular pressure: the effect of topical anesthesia.

    Science.gov (United States)

    Ogbuehi, Kelechi C

    2012-01-01

    The intraocular pressures and biomechanical parameters measured by the ocular response analyzer make the analyzer a useful tool for the diagnosis and management of anterior segment disease. This observational study was designed to investigate the effect of topical anesthesia on the parameters measured by the ocular response analyzer: corneal hysteresis, corneal resistance factor, Goldmann-correlated intraocular pressure (IOPg), and corneal-compensated intraocular pressure (IOPcc). Two sets of measurements were made for 78 eyes of 39 subjects, approximately 1 week apart. In session 1, each eye of each subject was randomized into one of three groups: polyvinyl alcohol (0.5%), tetracaine hydrochloride (0.5%), or oxybuprocaine hydrochloride (0.4%). In session 2, eyes that were in the polyvinyl alcohol group in session 1 were assigned to the tetracaine group, those in the tetracaine group in session 1 were assigned to oxybuprocaine group, and those in the oxybuprocaine group in session 1 were assigned to the polyvinyl alcohol group. For both sessions, each subject first had his or her central corneal thickness assessed with a specular microscope, followed by measurements of intraocular pressure and corneal biomechanical parameters with the Ocular Response Analyzer. All measurements were repeated for 2 minutes and 5 minutes following the instillation of either polyvinyl alcohol, tetracaine, or oxybuprocaine. The level of statistical significance was 0.05. Polyvinyl alcohol, tetracaine hydrochloride, and oxybuprocaine hydrochloride had no statistically significant (P > 0.05) effect on any of the biomechanical parameters of the cornea. There was no statistically significant effect on either IOPg (P > 0.05) or IOPcc (P > 0.05) 2 minutes after the eye drops were instilled in either session. Five minutes after the eye drops were instilled, polyvinyl alcohol showed no statistically significant effect on either IOPg (P > 0.05) or IOPcc (P > 0.05) in either session

  19. Corneal biomechanical parameters and intraocular pressure: the effect of topical anesthesia

    Directory of Open Access Journals (Sweden)

    Ogbuehi KC

    2012-06-01

    Full Text Available Kelechi C OgbuehiCornea Research Chair, Department of Optometry and Vision Sciences, College of Applied Medical Sciences, King Saud University, Riyadh, Saudi ArabiaBackground: The intraocular pressures and biomechanical parameters measured by the ocular response analyzer make the analyzer a useful tool for the diagnosis and management of anterior segment disease. This observational study was designed to investigate the effect of topical anesthesia on the parameters measured by the ocular response analyzer: corneal hysteresis, corneal resistance factor, Goldmann-correlated intraocular pressure (IOPg, and corneal-compensated intraocular pressure (IOPcc.Methods: Two sets of measurements were made for 78 eyes of 39 subjects, approximately 1 week apart. In session 1, each eye of each subject was randomized into one of three groups: polyvinyl alcohol (0.5%, tetracaine hydrochloride (0.5%, or oxybuprocaine hydrochloride (0.4%. In session 2, eyes that were in the polyvinyl alcohol group in session 1 were assigned to the tetracaine group, those in the tetracaine group in session 1 were assigned to oxybuprocaine group, and those in the oxybuprocaine group in session 1 were assigned to the polyvinyl alcohol group. For both sessions, each subject first had his or her central corneal thickness assessed with a specular microscope, followed by measurements of intraocular pressure and corneal biomechanical parameters with the Ocular Response Analyzer. All measurements were repeated for 2 minutes and 5 minutes following the instillation of either polyvinyl alcohol, tetracaine, or oxybuprocaine. The level of statistical significance was 0.05.Results: Polyvinyl alcohol, tetracaine hydrochloride, and oxybuprocaine hydrochloride had no statistically significant (P > 0.05 effect on any of the biomechanical parameters of the cornea. There was no statistically significant effect on either IOPg (P > 0.05 or IOPcc (P > 0.05 2 minutes after the eye drops were instilled in

  20. Drug: D00741 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available [HSA:6334] [KO:K04840]; voltage-gated sodium channel (SCN9A) blocker [HSA:6335] [KO:K04841] map07015 Local a...s affecting nervous system and sensory organs 12 Agents affecting peripheral nervous system 121 Local...P) 2 Agents affecting individual organs 27 Dental preparations 271 Local anesthetics 2710 Local anesthetics ...OIDS AND ANAL FISSURES FOR TOPICAL USE C05AD Local anesthetics C05AD02 Tetracaine D00741 Tetracaine hydrochl...SENSORY ORGANS S01 OPHTHALMOLOGICALS S01H LOCAL ANESTHETICS S01HA Local anestheti

  1. Comparative Analysis Of The Effects Of Topical Anaesthetic Agents ...

    African Journals Online (AJOL)

    Thus, of these three topical anaesthetic agents, 0.5% tetracaine hydrochloride may be the preferred choice in optometric practice particularly in patients with Keratoconjunctivitis Sicca (KCS) in order to facilitate their tear film stability;while the use of proparacaine should be discouraged in patients with dry eye syndrome.

  2. 21 CFR 346.10 - Local anesthetic active ingredients.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 5 2010-04-01 2010-04-01 false Local anesthetic active ingredients. 346.10... § 346.10 Local anesthetic active ingredients. The active ingredient of the product consists of any of...) Lidocaine 2 to 5 percent. (g) Pramoxine hydrochloride 1 percent. (h) Tetracaine 0.5 to 1 percent. (i...

  3. membrane potential change effects on cationic and neutral drug

    African Journals Online (AJOL)

    USER

    1Department of Human Physiology, College of Health Sciences University Of Port Harcourt,. Nigeria. 2School of Pure and Applied Biology University of Wales, College of Cardiff, Cathay's Park,. Cardiff, U.K.. The effect of membrane potential change of the human erythrocytes on cationic drugs tetracaine and chlorpromazine ...

  4. Helping to alleviate pain for children having venepuncture.

    LENUS (Irish Health Repository)

    Gilboy, Siobhan

    2009-10-01

    This article reviews the literature on venepuncture and children. The evidence on the use of topical agents namely tetracaine (amethocaine) gel and lidocaine\\/prilocaine cream is discussed, along with the use and benefits of distraction techniques and parental presence to make this an easier procedure for the child, their families and the nurse.

  5. Accelerating Topical Anaesthesia Using Microneedles.

    Science.gov (United States)

    Davies, Lleucu B; Gateley, Christopher; Holland, Phillip; Coulman, Siôn A; Birchall, James C

    2017-09-08

    Topical anaesthetics reduce pain during venous access procedures in children. However, clinical use is hindered by a significant anaesthetic onset time. Restricted diffusion of the topical anaesthetic through the stratum corneum barrier is the principal reason for the delayed onset. Microneedles can painlessly pierce the skin. This study evaluated microneedle pre-treatment of ex vivo human skin as a means to increase the rate of tetracaine permeation, in order to accelerate the onset of anaesthesia. Franz-type diffusion cells were used to determine permeation of a commercial tetracaine formulation, Ametop gel, through human skin epidermis. Microneedle-assisted permeation was compared to untreated epidermis. Upon completion of the permeation studies, the epidermal membranes were visually characterised. At 30 min, 5.43 µg/cm2 of tetracaine had permeated through the untreated membrane compared to 12.13 µg/cm2 through the microneedle-treated membrane. Insertion of a hypodermic needle created a large single channel in the epidermis (approx. 4,250 μm2) whilst the punctured surface area following microneedle treatments was estimated to be 75,000 μm2. Pre-treatment of skin with microneedles significantly enhances the permeation of tetracaine. Microneedles have the potential to more than halve the onset time for anaesthesia when applying Ametop gel. © 2017 S. Karger AG, Basel.

  6. Membrane potential change effects on cationic and neutral drug ...

    African Journals Online (AJOL)

    The effect of membrane potential change of the human erythrocytes on cationic drugs tetracaine and chlorpromazine and neutral drug benzyl alcohol induced cell shape change and red cell uptake of drug has been quantitated using light microscopy and spectrophotometry respectively. At the drug concentration necessary ...

  7. Topical anesthesia

    Directory of Open Access Journals (Sweden)

    Mritunjay Kumar

    2015-01-01

    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.

  8. Anatomical distribution of voltage-dependent membrane capacitance in frog skeletal muscle fibers.

    Science.gov (United States)

    Huang, C L; Peachey, L D

    1989-03-01

    Components of nonlinear capacitance, or charge movement, were localized in the membranes of frog skeletal muscle fibers by studying the effect of 'detubulation' resulting from sudden withdrawal of glycerol from a glycerol-hypertonic solution in which the muscles had been immersed. Linear capacitance was evaluated from the integral of the transient current elicited by imposed voltage clamp steps near the holding potential using bathing solutions that minimized tubular voltage attenuation. The dependence of linear membrane capacitance on fiber diameter in intact fibers was consistent with surface and tubular capacitances and a term attributable to the capacitance of the fiber end. A reduction in this dependence in detubulated fibers suggested that sudden glycerol withdrawal isolated between 75 and 100% of the transverse tubules from the fiber surface. Glycerol withdrawal in two stages did not cause appreciable detubulation. Such glycerol-treated but not detubulated fibers were used as controls. Detubulation reduced delayed (q gamma) charging currents to an extent not explicable simply in terms of tubular conduction delays. Nonlinear membrane capacitance measured at different voltages was expressed normalized to accessible linear fiber membrane capacitance. In control fibers it was strongly voltage dependent. Both the magnitude and steepness of the function were markedly reduced by adding tetracaine, which removed a component in agreement with earlier reports for q gamma charge. In contrast, detubulated fibers had nonlinear capacitances resembling those of q beta charge, and were not affected by adding tetracaine. These findings are discussed in terms of a preferential localization of tetracaine-sensitive (q gamma) charge in transverse tubule membrane, in contrast to a more even distribution of the tetracaine-resistant (q beta) charge in both transverse tubule and surface membranes. These results suggest that q beta and q gamma are due to different molecules and that

  9. Comparison of Iontophoretic Lidocaine to EMLA Cream for Pain Reduction Prior to Intravenous Cannulation in Adults

    Science.gov (United States)

    2000-10-01

    site prior to insertion of the catheter. However, infiltration of local anesthetics can be uncomfortable. Topical eutectic mixture of local...12 2. Lidocaine: A local anesthetic used to produce infiltration anesthesia and epidural and peripheral nerve blocks. Operational definition: 1.75...10,000 to 1:50,000. The current used was 1 mA for 10 minutes. Gangarosa also noted lidocaine to be far superior to procaine , tetracaine, mepivacaine

  10. Research and Development in Preventive Dentistry.

    Science.gov (United States)

    1979-12-01

    local anes- thetics are administered in several ways including topically, by infiltration , and as a nerve block. The same agents are also employed in...spinal anesthesia (Ritchie and Cohen, 1975). In dental surgery, the two primary techniques for achieving localized anesthesia are by local infiltration of... procaine , which are commonly used, but these agents such as tetracaine and bupivacaine have also been found to be much more toxic (Bennet, 1974; Ritchie

  11. Effects of tertiary amine local anesthetics on the assembly and disassembly of brain microtubules in vitro.

    Science.gov (United States)

    Genna, J M; Coffe, G; Pudles, J

    1980-09-01

    From kinetic and electron microscopy studies on the effects of procaine, tetracaine and dibucaine on the polymerization and depolymerization of the microtubules isolated from pig and rat brains the following results were obtained. 1. Procaine or tetracaine, at the concentration range of 0.5--20 mM and of 0.5--5 mM respectively, increases the rate of tubulin polymerization (24 degrees C or 37 degrees C) and of microtubule depolymerization (4 degrees C) as a linear function of the concentration of the anesthetics, while identical amounts of microtubules are formed. In the absence of microtubule-associated proteins the polymerization of tubulin is not induced by 10 mM procaine, furthermore, the critical concentration of microtubule proteins necessary for assembly into microtubules is not affected at this concentration level of the anesthetic. This suggests that procaine affects not the nucleation, but rather the elongation process. 2. Dibucaine, from 0.5 mM to 3 mM increases the lag time of the polymerization reaction, while from 0.5 mM to 2 mM it linearly decreases both tubulin polymerization (24 degrees C) and microtubule depolymerization (4 degrees C) rates. Dibucaine, up to mM concentration, does not affect the extent of tubulin polymerization; however, above this concentration it induces the formation of amorphous aggregates. 3. Procaine or tetracaine enhances the depolymerizing effect of calcium on microtubules. The half-maximal values for the depolymerizing effect of calcium were 0.96, 0.71 and 0.51 mM for the control, in the presence of 10 mM procaine and 5 mM tetracaine respectively.

  12. Pharmacological studies of charge movement in frog skeletal muscle.

    Science.gov (United States)

    Hui, C S

    1983-04-01

    Charge movements in frog twitch fibres were studied using the three-microelectrode voltage-clamp technique. In a solution made moderately hypertonic with 350 mM-sucrose, fibre contraction was effectively blocked and a secondary hump appeared in the decay phase of the 'on' part of charge movement. At small depolarizations, the hump (Q gamma) is small and slow. As depolarization is increased, Q gamma becomes larger in magnitude and faster in kinetics until it merges with the main part of charge movement (Q beta). As the fibre is perfused extracellularly with a test solution saturated with dantrolene sodium, Q gamma disappears in about 30 min whereas the kinetics of Q beta are slowed down. After equilibration in the dantrolene sodium solution, the total moveable charge is reduced by about 20%, which could very well be the charge carried by Q gamma. Tetracaine also suppresses Q gamma but does not seem to have any effect on the kinetics of Q beta. The suppression of Q gamma appears to be dose-dependent, with complete abolition occurring at about 4 mM-tetracaine. Dissection of charge movement with tetracaine indicates that Q gamma might be bell-shaped and capacitive in nature. Q beta and Q gamma might be two distinct species of charge and Q gamma would probably be more closely associated with calcium release from the sarcoplasmic reticulum.

  13. Separation of intramembrane charging components in low-calcium solutions in frog skeletal muscle.

    Science.gov (United States)

    Huang, C L

    1991-08-01

    The inactivation of charge movement components by small (-100 to -70 mV) shifts in holding potential was examined in voltage-clamped intact amphibian muscle fibers in low [Ca2+], Mg(2+)-containing solutions. The pulse protocols used both large voltage excursions and smaller potential steps that elicited prolonged (q gamma) transients. Charge species were distinguished through the pharmacological effects of tetracaine. These procedures confirmed earlier observations in cut fibers and identified the following new properties of the q gamma charge. First, q gamma, previously defined as the tetracaine-sensitive charge, is also the component primarily responsible for the voltage-dependent inactivation induced by conditions of low extracellular [Ca2+]. Second, this inactivation separates a transient that includes a "hump" component and which has kinetics and a voltage dependence distinct from the monotonic decay that remains. Third, q gamma, previously associated with delayed charge movements, can also contribute significant charge transfer at early times. These findings suggest that the parallel inhibition of calcium signals and charge movements reported in low [Ca2+] solutions arises from influences on q gamma charge (Brum et al., 1988a, b). They also reconcile reports that implicate tetracaine-sensitive (q gamma) charge in excitation-contraction coupling with evidence that early intramembrane events are also involved in this process (Pizarro et al., 1989). Finally, they are relevant to hypotheses of possible feedback or feed-forward roles of q gamma in excitation-contraction coupling.

  14. Effects of local anesthetics on contractions of pregnant and non-pregnant rat myometrium in vitro.

    Science.gov (United States)

    Wei, Jin-Song; Jin, Zhe-Bin; Yin, Zhi-Qiang; Xie, Qiang-Min; Chen, Ji-Qiang; Li, Zi-Gang; Tang, Hui-Fang

    2014-06-01

    In order to determine whether local anesthetics directly affect the propagation and strength of myometrial contractions, we compared the effects of bupivacaine, ropivacaine, lidocaine and tetracaine on the contractions of myometrium isolated from pregnant and non-pregnant rats. Full-thickness myometrial strips were obtained from 18- to 21-day pregnant and non-pregnant Sprague-Dawley rats and incubated in an organ bath. When spontaneous contractions became regular, strips were exposed to cumulative concentrations of the four local anesthetics ranging from 0.01 to 300 μmol/L and the amplitude and frequency of contraction were recorded. All four compounds caused a concentration-dependent inhibition of the contractility of pregnant and non-pregnant uterine muscle. In pregnant myometrium, the concentration that caused 50% inhibition (IC(50)) was 100 μmol/L for bupivacaine, 157 μmol/L for ropivacaine, > 1000 μmol/L for lidocaine, and 26.3 μmol/L for tetracaine. In non-pregnant myometrium, the IC(50) was 26.9 μmol/L for bupivacaine, 40 μmol/L for ropivacaine, 384 μmol/L for lidocaine, and 7.4 μmol/L for tetracaine. These results suggested that local anesthetics do inhibit myometrial contractions in pregnant and non-pregnant rats in a concentration-dependent manner.

  15. Voltage-dependent block of charge movement components by nifedipine in frog skeletal muscle.

    Science.gov (United States)

    Huang, C L

    1990-09-01

    Potential-dependent inhibition of charge movement components by nifedipine was studied in intact, voltage-clamped, frog skeletal muscle fibers. Available charge was reduced by small shifts in holding potential (from -100 mV to -70 mV) in 2 microM nifedipine, without changes in the capacitance deduced from control (-120 mV to -100 mV) voltage steps made at a fully polarized (-100 mV) holding potential. These voltage-dependent effects did not occur in lower (0-0.5 microM) nifedipine concentrations. The voltage dependence of membrane capacitance at higher (10 microM) nifedipine concentrations was reduced even in fully polarized fibers, but shifting the holding voltage produced no further block. Voltage-dependent inhibition by nifedipine was associated with a fall in available charge, and a reduction in the charge and capacitance-voltage relationships and of late (q gamma) charging transients. It thus separated a membrane-capacitance with a distinct and steep steady-state voltage dependence. Tetracaine (2 mM) reduced voltage-dependent membrane capacitance and nonlinear charge more than did nifedipine. However, nifedipine did not exert voltage-dependent effects on charging currents, membrane capacitance, or inactivation of tetracaine-resistant (q beta) charge. This excludes participation of q beta, or the membrane charge as a whole, from the voltage-dependent effects of nifedipine. Rather, the findings suggest that the charge susceptible to potential-dependent block by nifedipine falls within the tetracaine-sensitive (q gamma) category of intramembrane charge.

  16. Pharmacological separation of charge movement components in frog skeletal muscle.

    Science.gov (United States)

    Huang, C L

    1982-03-01

    1. Charge movements to small 10 mV steps superimposed upon a wide range of closely spaced depolarizing voltage-clamp pulses were studied in frog skeletal muscles under different pharmacological conditions in hypertonic solutions.2. In control fibres, capacitance was strongly voltage-dependent, especially between potentials of -60 and -20 mV, confirming earlier work. There was a sharp increase in capacitance at around -50 mV. The dependence of non-linear charge on potential was asymmetrical and saturated at around 25 nC/muF.3. The presence of tetracaine abolished the ;hump' in the non-linear transients, which became simple monotonic decays. The dependence of capacitance upon potential was reduced. The maximum available amount of non-linear charge fell to 10 nC/muF.4. The presence of lidocaine abolished both the ;hump' as well as the monotonic part of the non-linear transients. This resulted in capacitance falling with depolarization from -85 mV.5. Comparing the steady-state properties of the non-linear charge under the different pharmacological conditions made it possible to deduce empirically the following components:(i) A lidocaine-resistant component (q(alpha)), which was responsible for the fall in observed capacitance with depolarization from the control voltage.(ii) A component resistant to tetracaine yet abolished by lidocaine (q(beta)). This possesses quasi-exponential kinetics, and a maximum charge of about 20 nC/muF.(iii) A component abolished by both lidocaine and tetracaine (q(gamma)), which possesses a maximum charge of 15 nC/muF. This has complex kinetics, and its steep dependence upon voltage resembles the potential-dependence of the development of tension in skeletal muscle.

  17. Adverse drug events leading to emergency department visits at an eye hospital: A brief report.

    Science.gov (United States)

    Alizadeh, Safa; Mohebbi, Niayesh; Gholami, Kheirollah; Jabbarvand, Mahmoud

    2017-06-01

    To evaluate adverse drug events (ADEs) resulting in emergency department visits in an eye hospital. Emergency department visits at Farabi Eye Hospital were assessed for a 7-day period. The patients' eye disorders and drug history were evaluated to detect ADEs. Of 1631 emergency visits, 5 (0.3%, 95% CI: 0.13-0.71%) were drug related. Tetracaine eye drops accounted for 4 (80%, 95% CI: 38-96%) cases with corneal involvement. The other case was an intense conjunctival injection due to naphazoline eye drops. ADEs should be considered in differential diagnosis of ocular emergency problems and preventive measure should be considered.

  18. Challenges Encountered Using Ophthalmic Anesthetics in Space Medicine

    Science.gov (United States)

    Bayuse, T.; Law, J.; Alexander, D.; Moynihan, S.; LeBlanc, C.; Langford, K.; Magalhaes, L.

    2015-01-01

    On orbit, ophthalmic anesthetics are used for tonometry and off-nominal corneal examinations. Proparacaine has been flown traditionally. However, the manufacturers recently changed its storage requirements from room temperature storage to refrigerated storage to preserve stability and prolong the shelf-life. Since refrigeration on orbit is not readily available and there were stability concerns about flying proparacaine unrefrigerated, tetracaine was selected as an alternative ophthalmic anesthetic in 2013. We will discuss the challenges encountered flying and using these anesthetics on the International Space Station.

  19. Experimental analysis of the relationship between charge movement components in skeletal muscle of Rana temporaria.

    Science.gov (United States)

    Adrian, R H; Huang, C L

    1984-08-01

    Experiments were performed to ascertain whether the monotonic (q beta) and delayed (q gamma) components of non-linear charge in skeletal muscle membranes form a sequential system, or are the result of separate, independent processes. The non-linear capacitance studied in a large number of fibres increased with fibre diameter. This dependence was attributable to tetracaine-sensitive (q gamma) but not to tetracaine-resistant (q beta and q alpha) charge. The kinetics and total quantity of q gamma charge moving in response to voltage steps from varying pre-pulse potentials to a fixed probe potential remained constant despite variations in the size of the early q beta decay. The kinetics of the delayed (q gamma) charging current obtained from a single 20 mV depolarizing step were compared with the sum of the responses to two 10 mV steps adding to the same voltage excursion. The respective transients superimposed only if one of the 10 mV steps did not reach the voltage at which q gamma first appears. In the two preceding experiments, total charge was conserved. These results are consistent with separate and functionally independent q beta and q gamma systems of potential-dependent charge, with q gamma residing in the transverse tubules and q beta on surface membrane. The findings can be discussed in terms of a contractile 'activator' with a steep sensitivity to voltage that begins only with depolarization beyond a level close to the actual mechanical threshold.

  20. [Alkalimetric titrations of salts of organic bases in the Pharmacopoeia].

    Science.gov (United States)

    Bezáková, Zelmíra; Stankovičová, Mária

    2013-12-01

    Modified methods - alkalimetry in ethanol 70% with a defined small volume of hydrochloric acid 0.01 mol/l added to the solution of the sample before the titration and alkalimetry in ethanol 70% or ethanol 96% alone with potentiometric end-point detection for the assay of halide salts of 11 organic N-bases has been investigated. The results were compared to those obtained by the method of the European Pharmacopoeia 7th Ed. (Ph. Eur. 7th Ed.). The Ph. Eur. 7th Ed. use for 8 investigated substances alkalimetry in alcohol 96 % with a defined small volume of hydrochloric acid 0.01 mol/l (5 ml) with potentiometric end-point detection: Cinchocaine hydrochloride, Codeine hydrochloride dihydrate, Ethylmorphine hydrochloride, Lidocaine hydrochloride, Papaverine hydrochloride, Pilocarpine hydrochloride, Quinine hydrochloride, Tetracaine hydrochloride. Our results revealed that the Ph. Eur. 7th Ed. method did not work for 5 drugs from this group: Cinchocaine hydrochloride, Ethylmorphine hydrochloride, Papaverine hydrochloride, Pilocarpine hydrochloride and Tetracaine hydrochloride. In the group of investigated substances we included also drugs with the character of weak organic bases for which Ph. Eur. 7th Ed. prescribed different methods for their assay: Thiamine hydrochloride and Pyridoxine hydrochloride - acidimetric titration in non-aqueous solvents with perchloric acid and Procaine hydrochloride - determination of primary aromatic amino-nitrogen (Ph. Eur. 7th Ed., chapter 2.5.8).

  1. Interaction of local and general anaesthetics with liposomal membrane models: a QCM-D and DSC study.

    Science.gov (United States)

    Paiva, José Gabriel; Paradiso, Patrizia; Serro, Ana Paula; Fernandes, Anabela; Saramago, Benilde

    2012-06-15

    The behaviour of four local anaesthetics (lidocaine, levobupivacaine, ropivacaine and tetracaine) and one general anaesthetic (propofol) is compared when interacting with two types of model membranes: supported layers of liposomes and liposomes in solution. Several liposomal compositions were tested: dimyristoylphosphatidylcholine (DMPC), binary mixtures of DMPC with cholesterol (CHOL), and ternary mixtures of dipalmitoylphosphatidylcholine (DPPC), DMPC, and CHOL. A quartz crystal microbalance with dissipation, QCM-D, was used to assess changes in the properties of supported layers of liposomes. The effect of the anaesthetics on the phase behaviour of the liposomes in suspension was determined by differential scanning calorimetry. Both techniques show that all anaesthetics have a fluidizing effect on the model membranes but, apparently, the solid supported liposomes are less affected by the anaesthetics than the liposomes in solution. Although the different anaesthetics were compared at different concentrations, tetracaine and propofol seem to induce the strongest perturbation on the liposome membrane. The resistance of the liposomes to the anaesthetic action was found to increase with the presence of cholesterol, while adding DPPC to the binary mixture DMPC+CHOL does not change its behaviour. The novelty of the present work resides upon three points: (1) the use of supported layers of liposomes as model membranes to study interactions with anaesthetics; (2) application of QCM-D to assess changes of the adsorbed liposomes; (3) a comparison of the effect of local and general anaesthetics interacting with various model membranes in similar experimental conditions. Copyright © 2012 Elsevier B.V. All rights reserved.

  2. Kinetic separation of charge movement components in intact frog skeletal muscle.

    Science.gov (United States)

    Huang, C L

    1994-12-01

    1. Procedures for a complete charge movement separation employed a combination of its steady-state inactivation and activation properties in intact frog skeletal muscle fibres in gluconate-containing solutions. 2. Holding potential shifts from -70 to -50 mV reduced the total charge available between -90 and -20 mV from 16.76 +/- 1.70 nC microF-1 (mean +/- S.E.M.; n = 4 fibres) to 9.25 +/- 1.43 nC microF-1 without significant loss of tetracaine-resistant charge (q beta). 3. The steady-state and kinetic properties of tetracaine-sensitive charge (q gamma) persisted through holding potential changes from -90 to -70 mV in the presence of gluconate and generally resembled activation properties established hitherto in sulphate-containing solutions. 4. Further holding potential displacement to -50 mV abolished q gamma charge movements and depressed the charge-voltage curve. 5. Test voltage steps applied from a -70 mV prepulse level gave rapid monotonic q beta decays and similarly depressed activation functions in 2 mM tetracaine unchanged by holding potential shifts between -70 and -50 mV. 6. The isolated 'on' q gamma charge movements, I(t), always included early transients that preceded any prolonged charging phases and which increased with depolarization. They decayed to stable baselines in the absence of prolonged time-dependent or inward-current phases and yielded integrals, Q(t), that monotonically increased with test voltage. 7. 'Off' steps always elicited rapid monotonic q gamma decays that fully returned the 'on' charge. 8. 'On' and 'off' q gamma currents, I(t), following voltage steps from fixed conditioning to varying test levels mapped onto topologically distinct higher-order phase-plane trajectories, I(Q), that steeply varied with test voltage. 9. In contrast, voltage steps to fixed test potentials of either -70 or -20 mV elicited identical q gamma phase-plane trajectories independent of prepulse history. 10. The q gamma current thus reflects an independent

  3. Intra-membrane molecular interactions of K+ channel proteins :

    Energy Technology Data Exchange (ETDEWEB)

    Moczydlowski, Edward G.

    2013-07-01

    Ion channel proteins regulate complex patterns of cellular electrical activity and ionic signaling. Certain K+ channels play an important role in immunological biodefense mechanisms of adaptive and innate immunity. Most ion channel proteins are oligomeric complexes with the conductive pore located at the central subunit interface. The long-term activity of many K+ channel proteins is dependent on the concentration of extracellular K+; however, the mechanism is unclear. Thus, this project focused on mechanisms underlying structural stability of tetrameric K+ channels. Using KcsA of Streptomyces lividans as a model K+ channel of known structure, the molecular basis of tetramer stability was investigated by: 1. Bioinformatic analysis of the tetramer interface. 2. Effect of two local anesthetics (lidocaine, tetracaine) on tetramer stability. 3. Molecular simulation of drug docking to the ion conduction pore. The results provide new insights regarding the structural stability of K+ channels and its possible role in cell physiology.

  4. Transdermal delivery of hydrophobic and hydrophilic local anesthetics from o/w and w/o Brij 97-based microemulsions.

    Science.gov (United States)

    Junyaprasert, Varaporn Buraphacheep; Boonme, Prapaporn; Songkro, Sarunyoo; Krauel, Karen; Rades, Thomas

    2007-01-01

    To characterize the physicochemical properties of drug-loaded oil-in-water (o/w) and water-in-oil (w/o) Brij 97-based microemulsions in comparison to their blank counterparts and to investigate the influence of microemulsion type on in vitro skin permeation of model hydrophobic drugs and their hydrophilic salts. The microemulsion systems were composed of isopropyl palmitate (IPP), water and a 2:1 w/w mixture of Brij 97 and 1-butanol. The samples were characterized by visual appearance, pH, refractive index, electrical conductivity, viscosity and determination of the state of water and IPP in the formulations using differential scanning calorimetry (DSC). Transdermal flux of lidocaine, tetracaine, dibucaine and their respective hydrochloride salts through heat-separated human epidermis was investigated in vitro using modified Franz diffusion cells. The physicochemical properties of drug-loaded microemulsions and their blank counterparts were generally similar; however, slight changes in some physicochemical properties (apparent pH and conductivity) were observed due to the intrinsic properties of the drugs. The o/w microemulsions resulted in the highest flux of lidocaine, tetracaine and dibucaine as compared to the other formulations with in the same group of drugs. The characterization results showed that incorporation of the model drugs into the microemulsions did not change the microemulsion type. The permeation data exhibited that the nature of the microemulsions was a crucial parameter for transdermal drug delivery. The o/w microemulsions containing hydrophobic drugs provided the highest skin permeation enhancement. In addition, skin permeation was depended on the molecular weight of the model drugs.

  5. Anesthetics interacting with lipid rafts.

    Science.gov (United States)

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

    2013-01-23

    The exact mechanism by which anesthetics induce cell membrane-mediated modifications is still an open question. Although the fluidization effect of the anesthetic molecules on the cellular membrane is widely recognized, it is not known if anesthetics show any preference for specific membrane domains, namely the lipid rafts. The importance of these membrane micro-domains derives from the fact that they have been associated with cell signaling pathways, as well as with specific drug interactions. The objective of this work is to contribute for the elucidation of this question through the comparison of the anesthetic interactions with membranes of various lipid compositions. Liposomes prepared with an equimolar mixture of POPC, sphingomyelin and cholesterol, were chosen as models for lipid rafts. The interactions of these liposomes with two local anesthetics, tetracaine and lidocaine, and one general anesthetic, propofol, were studied. The effect of cholesterol was investigated by comparing anesthetic interactions with POPC/SM liposomes and POPC/SM/CHOL liposomes. The following experimental techniques were used: quartz crystal microbalance with dissipation, differential scanning calorimetry and phosphorus nuclear magnetic resonance. Although the liposomes investigated by the different techniques are not in the same conditions, it is possible to assemble the information obtained from all experimental techniques employed to reach a general conclusion. Tetracaine interacts more with raftlike domains, lidocaine induces stronger modifications on POPC/SM liposomes and the results for propofol are not fully conclusive but it seems to be the least prone to lipid interactions. The results were compared with those obtained with DMPC-containing liposomes, reported in a previous work. Copyright © 2012 Elsevier B.V. All rights reserved.

  6. Biophysical and Pharmacological Characterization of Nav1.9 Voltage Dependent Sodium Channels Stably Expressed in HEK-293 Cells.

    Science.gov (United States)

    Lin, Zhixin; Santos, Sonia; Padilla, Karen; Printzenhoff, David; Castle, Neil A

    2016-01-01

    The voltage dependent sodium channel Nav1.9, is expressed preferentially in peripheral sensory neurons and has been linked to human genetic pain disorders, which makes it target of interest for the development of new pain therapeutics. However, characterization of Nav1.9 pharmacology has been limited due in part to the historical difficulty of functionally expressing recombinant channels. Here we report the successful generation and characterization of human, mouse and rat Nav1.9 stably expressed in human HEK-293 cells. These cells exhibit slowly activating and inactivating inward sodium channel currents that have characteristics of native Nav1.9. Optimal functional expression was achieved by coexpression of Nav1.9 with β1/β2 subunits. While recombinantly expressed Nav1.9 was found to be sensitive to sodium channel inhibitors TC-N 1752 and tetracaine, potency was up to 100-fold less than reported for other Nav channel subtypes despite evidence to support an interaction with the canonical local anesthetic (LA) binding region on Domain 4 S6. Nav1.9 Domain 2 S6 pore domain contains a unique lysine residue (K799) which is predicted to be spatially near the local anesthetic interaction site. Mutation of this residue to the consensus asparagine (K799N) resulted in an increase in potency for tetracaine, but a decrease for TC-N 1752, suggesting that this residue can influence interaction of inhibitors with the Nav1.9 pore. In summary, we have shown that stable functional expression of Nav1.9 in the widely used HEK-293 cells is possible, which opens up opportunities to better understand channel properties and may potentially aid identification of novel Nav1.9 based pharmacotherapies.

  7. Biophysical and Pharmacological Characterization of Nav1.9 Voltage Dependent Sodium Channels Stably Expressed in HEK-293 Cells.

    Directory of Open Access Journals (Sweden)

    Zhixin Lin

    Full Text Available The voltage dependent sodium channel Nav1.9, is expressed preferentially in peripheral sensory neurons and has been linked to human genetic pain disorders, which makes it target of interest for the development of new pain therapeutics. However, characterization of Nav1.9 pharmacology has been limited due in part to the historical difficulty of functionally expressing recombinant channels. Here we report the successful generation and characterization of human, mouse and rat Nav1.9 stably expressed in human HEK-293 cells. These cells exhibit slowly activating and inactivating inward sodium channel currents that have characteristics of native Nav1.9. Optimal functional expression was achieved by coexpression of Nav1.9 with β1/β2 subunits. While recombinantly expressed Nav1.9 was found to be sensitive to sodium channel inhibitors TC-N 1752 and tetracaine, potency was up to 100-fold less than reported for other Nav channel subtypes despite evidence to support an interaction with the canonical local anesthetic (LA binding region on Domain 4 S6. Nav1.9 Domain 2 S6 pore domain contains a unique lysine residue (K799 which is predicted to be spatially near the local anesthetic interaction site. Mutation of this residue to the consensus asparagine (K799N resulted in an increase in potency for tetracaine, but a decrease for TC-N 1752, suggesting that this residue can influence interaction of inhibitors with the Nav1.9 pore. In summary, we have shown that stable functional expression of Nav1.9 in the widely used HEK-293 cells is possible, which opens up opportunities to better understand channel properties and may potentially aid identification of novel Nav1.9 based pharmacotherapies.

  8. Holmium:YAG laser ablation combined intraurethral fluorouracil perfusion as treatment option for intraurethral Condyloma acuminata in men.

    Science.gov (United States)

    Ge, C-G; Jiang, J; Jiang, Q; Liu, C; Hu, Z-L; Liang, P-H; Zhang, W-L

    2014-03-01

    Intraurethral condylomata acuminata (CA) is caused by human papilloma virus (HPV) infection which is transmitted by close physical and sexual contact. CA is often difficult to cure. There is limited research on the treatment of the patients with intraurethral CA. Here, we have reviewed our experiences on the treatment of intraurethral condylomatous with Holmium:YAG Laser ablation. A new and convenient mean of administering fluorouracil and lidocaine for the treatment of intraurethral condyloma acuminata is discussed. This study aimed to evaluate the experience and efficacy of Holmium:YAG Laser ablation with ureteroscopy and local administration of fluorouracil in the treatment of patients with intraurethral CA. The effects were investigated based on the rate of cure and relapse and the incidence of complications. The study included patients with intraurethral condylomatous who had undergone Holmium:YAG Laser ablation and intraurethral perfusion of fluorouracil. From May 2005 to October 2008, 25 patients (mean age 31.3 years, 19-63 years) with cystourethroscopy confirmed extensive lesions at the anterior urethra and biopsy of the lesions was compatible with condyloma acuminata. They all underwent Holmium:YAG Laser ablation with a transurethral Wolf 8/9.8 Fr rigid ureteroscope. And a week later, the patients initially accepted intraurethral installation of the mixture containing 1% fluorouracil and 1% tetracaine hydrochloride gel (lubricating jelly) in a volume of 20 mL. This mixture was given intraurethrally once weekly, and tip of the penis was clamped immediately to close the urethral meatus after administration by using an occlusive penile clamp and was retained for 20 minutes. Six treatments were given initially and after six weeks of rest, another cycle of six weekly treatments was given. Ureteroscopic Holmium laser ablation was successfully performed in all patients with multifocal intraurethral CA. Mean CA warts body size was 3 mm (2-8) in diameter. Mean

  9. Assessing the safety and efficacy of drugs used in preparing the nose for diagnostic and therapeutic procedures: a systematic review.

    Science.gov (United States)

    Saif, A M; Farboud, A; Delfosse, E; Pope, L; Adke, M

    2016-10-01

    Local anaesthetics and vasoconstrictors are essential for pain control and to aid intra-operative haemostasis in nasal procedures. They also improve access, and reduce discomfort when performing nasal endoscopy. There are no clear guidelines on preparing the nose despite evermore diagnostic and therapeutic procedures utilising the nose as a point of access. This review aims to identify nasal preparations used in diagnostic and therapeutic nasal procedures and to examine their safety and efficacy. Systematic review. A search was carried out using PubMed, MEDLINE, Ovid EMBASE, the Cochrane library and references from the included articles. The inclusion criteria included: full-text English language articles with regard to nasal preparation for surgery. Case reports, systematic reviews, meta-analysis, double-blind placebo controlled randomised trials (RCTs) and case series were included. A total of 53 articles were retrieved: 13 articles on nasal preparation for operative procedures, six on functional endoscopic sinus surgery and 22 on nasendoscopy as well as six case reports. Cocaine was the most widely used topical preparation for operative procedures but was associated with more side-effects; thus, topical tetracaine and levobupivacaine infiltration are alternatives with equivalent efficacy but reduced adverse effects. All articles reviewed for functional endoscopic sinus surgery used a mixture containing lidocaine, adrenaline or both. Flexible nasendoscopy causes minimal patient discomfort and preparation is only recommended in selected patients, in contrast to rigid nasendoscopy which requires preparation. For operative procedures, such as septorhinoplasty, a single agent tetracaine or levobupivicaine provides an improved surgical field. In functional endoscopic sinus surgery, lidocaine-adrenaline preparations have resulted in significantly better surgical and patient outcomes. There is little evidence to support the routine use of pre-procedural nasal

  10. Calcium and protons affect the interaction of neurotransmitters and anesthetics with anionic lipid membranes.

    Science.gov (United States)

    Pérez-Isidoro, Rosendo; Ruiz-Suárez, J C

    2016-09-01

    We study how zwitterionic and anionic biomembrane models interact with neurotransmitters (NTs) and anesthetics (ATs) in the presence of Ca(2+) and different pH conditions. As NTs we used acetylcholine (ACh), γ-aminobutyric acid (GABA), and l-glutamic acid (LGlu). As ATs, tetracaine (TC), and pentobarbital (PB) were employed. By using differential scanning calorimetry (DSC), we analyzed the changes such molecules produce in the thermal properties of the membranes. We found that calcium and pH play important roles in the interactions of NTs and ATs with the anionic lipid membranes. Changes in pH promote deprotonation of the phosphate groups in anionic phospholipids inducing electrostatic interactions between them and NTs; but if Ca(2+) ions are in the system, these act as bridges. Such interactions impact the physical properties of the membranes in a similar manner that anesthetics do. Beyond the usual biochemical approach, we claim that these effects should be taken into account to understand the excitatory-inhibitory orchestrated balance in the nervous system. Copyright © 2016 Elsevier B.V. All rights reserved.

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

    Science.gov (United States)

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

    2015-07-30

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

  12. Water solvent and local anesthetics: A computational study

    Science.gov (United States)

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

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

  13. 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

    1997-12-31

    The study of local anesthetics`(LA) interaction with model phospholipid membranes is justified by the direct correlation between anesthetic`s hydrophobicity and its potency/toxicity. By the same reason, uncharged LA species seems to play a crucial role in anesthesia. Most clinically used LA are small amphiphilics with a protonated amine group (pKa around 8). Although both charged (protonated) and uncharged forms can coexist at physiological pH, it has been shown (Lee, Biochim. Biophys. Acta 514:95, 1978; Screier et al. Biochim. Biophys. Acta 769:231, 1984) that the real anesthetic pka can be down-shifted, due to differential partition into membranes, increasing the ratio of uncharged species at pH 7.4. We have measured {sup 1}H-NMR longitudinal relaxation times (T{sub 1}) for phospholipid and three local anesthetics (tetracaine, lidocaine, benzocaine), in sonicated vesicles at a 3:1 molar ratio. All the LA protons have shown smaller T{sub 1} in this system than in isotropic phases, reflecting LA immobilization caused by insertion in the membrane. T{sub 1} values for the lipid protons in the presence of LA were analyzed, in an attempt to identify specific LA:lipid contact regions. (author) 13 refs., 3 figs., 1 tabs.

  14. Systemic Side-Effects of Topical Ophthalmic Drops in a 17-Year Old Boy Candidate for Deep Viterectomy: a Case Report

    Directory of Open Access Journals (Sweden)

    A Maleki

    2012-07-01

    Full Text Available Background: Drugs applied topically to the eye may be absorbed systemically to a substantial degree, with the potential to cause serious systemic side-effects. Children may be particularly vulnerable to systemic effects of topically applied agents as topical doses are often not weight-adjusted. Case presentation: This article describes a case of serious systemic side-effect by the use of topical phenylephrine, tetracaine, tropicamide and atropine in a 17-year old boy candidate for deep viterectomy in Farabi Hospital in 1389. Following application of the aforesaid eye drops, the patient developed hypertension and subsequent loss of conciseness. Conclusion: Several types of eye drops and their repeated use can lead to their systemic absorption and medical complications due to overdose. Strategies to minimize systemic absorption should be applied, including use of low concentrations of ophthalmic drugs, administration of one type of the drug, use of microdrops and punctal occlusion to minimize absorption via the nasolacrimal duct. While administering ophthalmic drops, one should take these precautions to minimize the systemic effects of the drugs to prevent subsequent complications.

  15. Novel serine-based gemini surfactants as chemical permeation enhancers of local anesthetics: A comprehensive study on structure-activity relationships, molecular dynamics and dermal delivery.

    Science.gov (United States)

    Teixeira, Raquel S; Cova, Tânia F G G; Silva, Sérgio M C; Oliveira, Rita; do Vale, M Luísa C; Marques, Eduardo F; Pais, Alberto A C C; Veiga, Francisco J B

    2015-06-01

    This work aims at studying the efficacy of a series of novel biocompatible, serine-based surfactants as chemical permeation enhancers for two different local anesthetics, tetracaine and ropivacaine, combining an experimental and computational approach. The surfactants consist of gemini molecules structurally related, but with variations in headgroup charge (nonionic vs. cationic) and in the hydrocarbon chain lengths (main and spacer chains). In vitro permeation and molecular dynamics studies combined with cytotoxicity profiles were performed to investigate the permeation of both drugs, probe skin integrity, and rationalize the interactions at molecular level. Results show that these enhancers do not have significant deleterious effects on the skin structure and do not cause relevant changes on cell viability. Permeation across the skin is clearly improved using some of the selected serine-based gemini surfactants, namely the cationic ones with long alkyl chains and shorter spacer. This is noteworthy in the case of ropivacaine hydrochloride, which is not easily administered through the stratum corneum. Molecular dynamics results provide a mechanistic view of the surfactant action on lipid membranes that essentially corroborate the experimental observations. Overall, this study suggests the viability of these serine-based surfactants as suitable and promising delivery agents in pharmaceutical formulations. Copyright © 2015. Published by Elsevier B.V.

  16. Duodenal lipid sensing activates vagal afferents to regulate non-shivering brown fat thermogenesis in rats.

    Directory of Open Access Journals (Sweden)

    Clémence Blouet

    Full Text Available Previous evidence indicates that duodenal lipid sensing engages gut-brain neurocircuits to determine food intake and hepatic glucose production, but a potential role for gut-brain communication in the control of energy expenditure remains to be determined. Here, we tested the hypothesis that duodenal lipid sensing activates a gut-brain-brown adipose tissue neuraxis to regulate thermogenesis. We demonstrate that direct administration of lipids into the duodenum increases brown fat temperature. Co-infusion of the local anesthetic tetracaine with duodenal lipids abolished the lipid-induced increase in brown fat temperature. Systemic administration of the CCKA receptor antagonist devazepide blocked the ability of duodenal lipids to increase brown fat thermogenesis. Parenchymal administration of the N-methyl-d-aspartate receptor blocker MK-801 directly into the caudomedial nucleus of the solitary tract also abolished duodenal lipid-induced activation of brown fat thermogenesis. These findings establish that duodenal lipid sensing activates a gut-brain-brown fat axis to determine brown fat temperature, and thereby reveal a previously unappreciated pathway that regulates thermogenesis.

  17. [Clinical results of transepithelial corneal collagen cross-linking in the treatment of keratoconus].

    Science.gov (United States)

    Chen, S H; Zhang, J; Li, Y N; Ding, P; Wang, Q M

    2016-07-01

    To evaluate the effect of transepithelial corneal collagen cross-linking (CXL) in the treatment of keratoconus. Prospective study. Sixteen eyes of 16 patients with keratoconus underwent transepithelial CXL, and the fellow eyes were considered as the controls. The mean age was (22.4±6.5) years old. In the CXL group, topical anesthesia (0.1% tetracaine) was given for 15 minutes, and 0.5% riboflavin was applied until saturated in the anterior chamber. Then an ultraviolet A irradiance of 3 mW/cm(2) on the cornea was performed for 30 minutes. Postoperative corneal reepithelization time was recorded. Preoperative and postoperative examinations included uncorrected distance visual acuity (UDVA), corrected distance visual acuity (CDVA), refractive error, topography, corneal biomechanical parameters, thinnest corneal thickness, and endothelial cell density. The mean corneal reepithelization time was 1.0(1.0 to 2.0) days. In the transepithelial CXL group, at the end of the 12-month follow-up, CDVA and refractive outcomes were significantly improved (P0.05). The differences in the changes of UDVA, CDVA, spherical equivalent refraction, and maximum K-value between the CXL and control groups were significant at 12 months (P<0.05). Transepithelial CXL is effective in optimizing the irregular corneal surface of keratoconus, and might halt its progression. (Chin J Ophthalmol, 2016, 52: 525-530).

  18. Topical anaesthesia in children: reducing the need for specialty referral.

    LENUS (Irish Health Repository)

    O'Connor, Gabrielle

    2012-01-31

    OBJECTIVE: The management of wounds in children is stressful, not only for the child, but also for parents and staff. In our Emergency Department (ED), we currently do not have a paediatric sedation policy, and thus children requiring suturing, not amenable to distraction and infiltrative anaesthesia, are referred to specialty teams for general anaesthesia. We proposed that the introduction of a topical anaesthetic gel (lidocaine, adrenaline, tetracaine - LAT) might help to reduce the number of referrals, by allowing the ED staff to perform the procedures, in combination with nonpharmacological approaches. METHODS: We carried out a retrospective review of ED records of all children aged 14 years or less attending with wounds, over an 8-month period, from 01 May 2007 to 31 January 2008. RESULTS: Two hundred and one (50.6%) patients presented before the introduction of LAT gel, whereas 196 (49.3%) patients presented afterwards. A total of 39 (19.4%) patients were referred for specialty review pre-LAT, whereas only 19 (9.7%) patients were referred in the LAT group. Of these, 31 (15.4%) pre-LAT and 15 (7.7%) LAT group required general anaesthesia. There is a significant difference between these two groups, using Fischer\\'s exact test, P=0.018. CONCLUSION: We have found that the introduction of topical anaesthetic gel in ED has significantly reduced the number of children with wounds referred to specialty teams for general anaesthesia. This has important implications for patient safety and hospital resources.

  19. Glaucoma Surgery in Pregnancy: A Case Series and Literature Review

    Directory of Open Access Journals (Sweden)

    Mohammad Reza Razeghinejad

    2016-09-01

    Full Text Available Glaucoma management in pregnant patients is a real challenge, especially when the glaucoma is not controlled with medications. We report the results of 6 incisional glaucoma surgeries for the management of medically uncontrolled glaucoma patients during pregnancy. This retrospective, case series was conducted on the 6 eyes of 3pregnant patients with uncontrolled glaucoma using maximum tolerable medications. Details of the glaucoma surgical management of these patients as well as their postoperative care and pregnancy and clinical outcomes on longitudinal follow-up are discussed. All 3 patients had juvenile open-angle glaucoma and were on various anti-glaucoma medications, including oral acetazolamide. The first case described underwent trabeculectomy without antimetabolites in both eyes because of uncontrolled intraocular pressure with topical medications. The surgery was done with topical lidocaine jelly and subconjunctival lidocaine during the second and third trimesters. The second patient had an Ahmed valve implantation in both eyes during the second and third trimesters because of uncontrolled IOP with topical medications and no response to selective laser trabeculoplasty. Surgery was done with topical tetracaine and subconjunctival and sub-Tenon’s lidocaine. The third case had a Baerveldt valve implantation under general anesthesia in the second trimester. In selected pregnant glaucoma patients with medically uncontrolled intraocular pressure threatening vision, incisional surgery may lead to good outcomes for the patient with no risk for the fetus.

  20. Kinetic isoforms of intramembrane charge in intact amphibian striated muscle.

    Science.gov (United States)

    Huang, C L

    1996-04-01

    The effects of the ryanodine receptor (RyR) antagonists ryanodine and daunorubicin on the kinetic and steady-state properties of intramembrane charge were investigated in intact voltage-clamped frog skeletal muscle fibers under conditions that minimized time-dependent ionic currents. A hypothesis that RyR gating is allosterically coupled to configurational changes in dihydropyridine receptors (DHPRs) would predict that such interactions are reciprocal and that RyR modification should influence intramembrane charge. Both agents indeed modified the time course of charging transients at 100-200-microM concentrations. They independently abolished the delayed charging phases shown by q gamma currents, even in fibers held at fully polarized, -90-mV holding potentials; such waveforms are especially prominent in extracellular solutions containing gluconate. Charge movements consistently became exponential decays to stable baselines in the absence of intervening inward or other time-dependent currents. The steady-state charge transfers nevertheless remained equal through the ON and the OFF parts of test voltage steps. The charge-voltage function, Q(VT), shifted by approximately +10 mV, particularly through those test potentials at which delayed q gamma currents normally took place but retained steepness factors (k approximately 8.0 to 10.6 mV) that indicated persistent, steeply voltage-dependent q gamma contributions. Furthermore, both RyR antagonists preserved the total charge, and its variation with holding potential, Qmax (VH), which also retained similarly high voltage sensitivities (k approximately 7.0 to 9.0 mV). RyR antagonists also preserved the separate identities of q gamma and q beta species, whether defined by their steady-state voltage dependence or inactivation or pharmacological properties. Thus, tetracaine (2 mM) reduced the available steady-state charge movement and gave shallow Q(VT) (k approximately 14 to 16 mV) and Qmax (VH) (k approximately 14 to 17 m

  1. Estudo clínico e histológico das pálpebras e conjuntiva hígidas submetidas ao tratamento tópico com soluções anestésicas em coelhos Clinical and histological evaluation of healthy eyelid and conjunctiva subject to local treatment with anesthetic solutions in rabbits

    Directory of Open Access Journals (Sweden)

    A.V.C. Amaral

    2013-02-01

    Full Text Available Avaliaram-se as apresentações comerciais de colírios anestésicos aplicados em 63 coelhos da raça Nova Zelândia, distribuídos em três grupos (G1, G2 e G3 de 21 animais cada e que receberam instilação de uma gota em cada olho seis vezes ao dia. Os animais do G1 foram tratados com colírio de cloridrato de proparacaína a 0,5%; os do G2, com colírio de cloridrato de tetracaína a 1% associado à fenilefrina a 0,1%; e os do G3, com solução fisiológica. Cada grupo foi subdividido em três subgrupos com sete animais cada, os quais foram tratados por três, sete e 15 dias. No final de cada tratamento, dois animais de cada subgrupo foram sacrificados para exame histológico de fragmentos retirados da conjuntiva, da terceira pálpebra e das pálpebras. Observou-se, ao exame clínico, episclerite em graus diversos em 100% dos animais do G1, no terceiro, sétimo e 15º dia, e em apenas 17,8% nos do G2, nestes mesmos dias. Ao exame microscópico, observaram-se aumento do número de células califormes, proliferação de folículos linfoides, aumento do número de eosinófilos e aumento do espaço intersticial nas pálpebras dos animais do G1. Pôde-se concluir que o colírio de tetracaína a 1% associado à fenilefrina a 0,1% promoveu maior toxicidade à conjuntiva ocular e às pálpebras de coelhos quando comparado ao colírio de proparacaína a 0,5%.This work aimed to evaluate commercial presentations of anesthetic eye drops in sixty three New Zealand rabbits which were separated equally in three groups (G1, G2 and G3. The G1 group was treated with 0.5% proparacaine chloridrate eye drop, G2 group with 1% tetracaine chloridrate associated with 0.1% phenylephrine eye drop and G3 group with 0.9% physiologic solution eye drop. All of them received one drop in each eye six times a day. Each group was subdivided into three subgroups (seven rabbits, which are treated for 3, 7 and 15 days. At the end of each treatment, two animals in each subgroup

  2. Development of novel encapsulated formulations using albumin-chitosan as a polymer matrix for ocular drug delivery

    Science.gov (United States)

    Addo, Richard Tettey

    Designing formulations for ophthalmic drug delivery is one of the most challenging endeavors facing the pharmaceutical scientist due to the unique anatomy, physiology, and biochemistry of the eye. Current treatment protocols for administration of drugs in eye diseases are primarily solution formulations, gels or ointments. However, these modes of delivery have several drawbacks such as short duration of exposure, need for repeated administrations and non-specific toxicity. We hypothesize that development of ocular drugs in microparticles will overcome the deficiencies of the current modalities of treatment. We based the hypothesis on the preliminary studies conducted with encapsulated tetracaine, an anesthetic used for surgical purposes and atropine, a medication used for several ophthalmic indications including mydriatic and cycloplegic effects. However, atropine is well absorbed into the systemic circulation and has been reported to exert severe systemic side effects after ocular administration (Hoefnagel D. 1961, Morton H. G. 1939 and Lang J. C. 1995) and may lead to serious side effects including death in extreme cases with pediatric use. Based on these observations, the focus of this dissertation is to formulate microparticulate drug carrier for treatment of various conditions of the eye. Purpose: To prepare, characterize, study the in vitro and in vivo interaction of albumin-chitosan microparticles (BSA-CSN MS), a novel particulate drug carrier for ocular drug delivery. Method: Microparticle formulations were prepared by method of spray drying. The percentage drug loading and efficiency were assessed using USP (I) dissolution apparatus. Using Malvern Zeta-Sizer, we determined size and surface charge of the fabrication. Surface morphology of the microparticles was examined using Scanning Electron Microscopy. Microparticles were characterized in terms of thermal properties using Differential Scanning Calorimetry. Human corneal epithelial cells (HCET-1) were

  3. A quantitative description of the voltage-dependent capacitance in frog skeletal muscle in terms of equilibrium statistical mechanics.

    Science.gov (United States)

    Duane, S; Huang, C L

    1982-04-22

    We present an analysis of experimental steady-state properties of charge movements in voltage-clamped frog skeletal muscle; by adopting an approach based on equilibrium statistical mechanics, detailed assumptions about the dynamics of the charge movement were avoided. Different components of the charge movements, as characterized by their sensitivities to local anaesthetics, were taken to correspond to different types of independent subsystem (integral membrane proteins). Quantitative agreement with the data for the q beta and q gamma components was obtained for the simplest subsystems, having two energy levels; however, q alpha required three (or more) energy levels. Each of the subsystems can be interpreted as having a charged group, minimum valency z, able to occupy two or more positions within the membrane. The tetracaine-sensitive q gamma charge can be described in terms of an ensemble of subsystems having z = 4.5, each occupying one of two levels whose free energies at zero applied voltage differ by 1.7 x 10(-1) eV. Likewise, the lidocaine-sensitive q beta has z = 1.0, free energy difference 1.9 x 10(-2) eV. However, the simplest model for the lidocaine-resistant q alpha involves a charge of valency 1.7 moving between three levels having relative free energies at zero applied voltage -9.7 x 10(-2), 0, and 2.1 x 10(-2) eV respectively, where the intermediate level 'sees' about 50% of the applied voltage.

  4. Charge conservation in intact frog skeletal muscle fibres in gluconate-containing solutions.

    Science.gov (United States)

    Huang, C L

    1994-01-01

    1. The conservation of intramembrane charge was investigated in intact voltage-clamped frog skeletal muscle fibres under conditions that minimized time-dependent ionic currents and so facilitated precise determination of capacitative charge. 2. Prolonged (q gamma) transients were demonstrated in 3,4-diaminopyridine and tetraethyl-ammonium gluconate-containing low [Ca2+] solutions in response to 125 ms pulses that explored the voltage range -90 to -20 mV. The tetracaine-sensitive, q gamma, component then accounted for a significant proportion (over 50%) of available charge. 3. Both delayed 'on' q gamma currents and 'off' current tails decayed to steady direct current (DC) baselines without significant residual ionic current slopes in the chosen extracellular solutions. This suggested that the current transients represented capacitative decays. It was also compatible with the precise determination of effective charge by integration. 4. The advent of 'on' q gamma current was accompanied by increased 'off' charge. Thus, charge was conserved through all 'on' and 'off' steps and through test voltages that extended from the threshold appearance of q gamma as a slow transient to its full merger with the earlier q beta decay at stronger depolarizations. 5. Charge conservation persisted through a wide range of 'on' pulse durations between 60 and 370 ms and was therefore independent of the interval following the q gamma decay. 6. The quantity of q gamma charge remained a monotonic single-valued function of test voltage, whether this potential was reached directly from the -90 mV holding potential or following a prepulse to -10 mV. 7. These findings suggest that the q gamma charge movement represents the electrical signature of an intramembrane entity whose transitions are primarily driven by, and therefore conserved with, the steady-state potential.

  5. Comprehensive allergy evaluation is useful in the subsequent care of patients with drug hypersensitivity reactions during anesthesia.

    Science.gov (United States)

    Guyer, Autumn C; Saff, Rebecca R; Conroy, Michelle; Blumenthal, Kimberly G; Camargo, Carlos A; Long, Aidan A; Banerji, Aleena

    2015-01-01

    For patients with a history of drug hypersensitivity reaction (HSR) during anesthesia, strategies to minimize risk with subsequent anesthesia are unclear. Identification of the cause of HSR during anesthesia remains challenging. To determine the success of a comprehensive allergy evaluation and management plan for patients with HSR during anesthesia, including identification of the causative agent and review of outcomes during subsequent anesthesia exposure. We performed chart reviews of patients referred for the evaluation of HSR during anesthesia between 2003 and 2012. Data collection included patient characteristics, signs/symptoms of HSR during anesthesia, and subsequent outcomes. Patients underwent comprehensive allergy evaluation including skin testing for identifying potential culprit agents, and the results were used to provide recommendations for any subsequent anesthesia. Over the 10-year study period, 73 patients with HSR during anesthesia were referred for further evaluation. Thirteen patients (18%) had positive skin test results to a drug received during anesthesia. One patient with a positive skin test result was diagnosed with mastocytosis. The causative agents identified in these 13 patients included latex, β-lactam antibiotics, neuromuscular blockers, tetracaine, odansetron, and fentanyl. On follow-up, 47 of the 73 patients (64%) subsequently underwent procedures requiring anesthesia. Using our recommendations from evaluation and testing, 45 of these 47 patients (96%) successfully tolerated subsequent anesthesia. The 2 patients who developed recurrent HSR during anesthesia were later diagnosed with mast cell disorders. Our comprehensive evaluation and management plan minimizes risk with subsequent anesthesia even when the cause of HSR could not be identified. Baseline tryptase levels may be helpful in this patient population to diagnose mast cell disorders. Copyright © 2014 American Academy of Allergy, Asthma & Immunology. Published by Elsevier

  6. Topical cryoanesthesia for the relief of pain caused by steroid injections used to treat hypertrophic scar/span>s and keloids

    Science.gov (United States)

    Wang, Xiuxia; Wu, Xiaoli; Liu, Ke; Xia, Lingling; Lin, Xunxun; Liu, Wei; Gao, Zhen

    2017-01-01

    Abstract Intralesional steroid injections are the standard treatment for hypertrophic scar/span>s and keloids. The procedure is, however, quite painful and is unpopular with patients because of this. Topical application of anesthetic creams, such as Ametop gel (tetracaine) and EMLA cream (lidocaine and prilocaine), has limited efficacy because of poor drug penetration. The onset of the analgesic effect is also slow, which means that the use of topical anesthetics is time-consuming in clinical practice. We hypothesized that a commercially available cryotip could be used to provide fast-acting topical cryoanesthesia that would reduce the pain associated with steroid injections. Thirty patients with hypertrophic scar/span>s or keloids were enrolled in the study. Scars were injected with the steroid, triamcinolone acetonide, with or without prior application of the cryotip (−10 °C) for 15 seconds. The degree of pain was evaluated in each case using the visual analogue scale (VAS) and the verbal descriptor scale (VDS), together with any side-effects caused by application of the cryotip. The VAS pain scores showed a statistically significant (P scars (pain scores 7.87 ± 1.31 and 2.7 ± 1.37, respectively). The VDS pain scores also showed a statistically significant (P scars. And its average scores were 7.89 ± 0.32 and 2.68 ± 0.25, respectively. Application of the cryotip before injection could provide a rapid and effective means of reducing the pain associated with steroid injections. Painless would result in better therapeutic effect. PMID:29069016

  7. Electrical slow waves in the mouse oviduct are dependent on extracellular and intracellular calcium sources

    Science.gov (United States)

    Dixon, Rose Ellen; Britton, Fiona C.; Baker, Salah A.; Hennig, Grant W.; Rollings, Christina M.; Sanders, Kenton M.

    2011-01-01

    Spontaneous contractions of the myosalpinx are critical for oocyte transport along the oviduct. Slow waves, the electrical events that underlie myosalpinx contractions, are generated by a specialized network of pacemaker cells called oviduct interstitial cells of Cajal (ICC-OVI). The ionic basis of oviduct pacemaker activity is unknown. Intracellular recordings and Ca2+ imaging were performed to examine the role of extracellular and intracellular Ca2+ sources in slow wave generation. RT-PCR was performed to determine the transcriptional expression of Ca2+ channels. Molecular studies revealed most isoforms of L- and T-type calcium channels (Cav1.2,1.3,1.4,3.1,3.2,3.3) were expressed in myosalpinx. Reduction of extracellular Ca2+ concentration ([Ca2+]o) resulted in the abolition of slow waves and myosalpinx contractions without significantly affecting resting membrane potential (RMP). Spontaneous Ca2+ waves spread through ICC-OVI cells at a similar frequency to slow waves and were inhibited by reduced [Ca2+]o. Nifedipine depolarized RMP and inhibited slow waves; however, pacemaker activity returned when the membrane was repolarized with reduced extracellular K+ concentration ([K+]o). Ni2+ also depolarized RMP but failed to block slow waves. The importance of ryanodine and inositol 1,4,5 trisphosphate-sensitive stores were examined using ryanodine, tetracaine, caffeine, and 2-aminoethyl diphenylborinate. Results suggest that although both stores are involved in regulation of slow wave frequency, neither are exclusively essential. The sarco/endoplasmic reticulum Ca2+-ATPase (SERCA) pump inhibitor cyclopiazonic acid inhibited pacemaker activity and Ca2+ waves suggesting that a functional SERCA pump is necessary for pacemaker activity. In conclusion, results from this study suggest that slow wave generation in the oviduct is voltage dependent, occurs in a membrane potential window, and is dependent on extracellular calcium and functional SERCA pumps. PMID:21881003

  8. Electrical slow waves in the mouse oviduct are dependent on extracellular and intracellular calcium sources.

    Science.gov (United States)

    Dixon, Rose Ellen; Britton, Fiona C; Baker, Salah A; Hennig, Grant W; Rollings, Christina M; Sanders, Kenton M; Ward, Sean M

    2011-12-01

    Spontaneous contractions of the myosalpinx are critical for oocyte transport along the oviduct. Slow waves, the electrical events that underlie myosalpinx contractions, are generated by a specialized network of pacemaker cells called oviduct interstitial cells of Cajal (ICC-OVI). The ionic basis of oviduct pacemaker activity is unknown. Intracellular recordings and Ca(2+) imaging were performed to examine the role of extracellular and intracellular Ca(2+) sources in slow wave generation. RT-PCR was performed to determine the transcriptional expression of Ca(2+) channels. Molecular studies revealed most isoforms of L- and T-type calcium channels (Cav1.2,1.3,1.4,3.1,3.2,3.3) were expressed in myosalpinx. Reduction of extracellular Ca(2+) concentration ([Ca(2+)](o)) resulted in the abolition of slow waves and myosalpinx contractions without significantly affecting resting membrane potential (RMP). Spontaneous Ca(2+) waves spread through ICC-OVI cells at a similar frequency to slow waves and were inhibited by reduced [Ca(2+)](o). Nifedipine depolarized RMP and inhibited slow waves; however, pacemaker activity returned when the membrane was repolarized with reduced extracellular K(+) concentration ([K(+)](o)). Ni(2+) also depolarized RMP but failed to block slow waves. The importance of ryanodine and inositol 1,4,5 trisphosphate-sensitive stores were examined using ryanodine, tetracaine, caffeine, and 2-aminoethyl diphenylborinate. Results suggest that although both stores are involved in regulation of slow wave frequency, neither are exclusively essential. The sarco/endoplasmic reticulum Ca(2+)-ATPase (SERCA) pump inhibitor cyclopiazonic acid inhibited pacemaker activity and Ca(2+) waves suggesting that a functional SERCA pump is necessary for pacemaker activity. In conclusion, results from this study suggest that slow wave generation in the oviduct is voltage dependent, occurs in a membrane potential window, and is dependent on extracellular calcium and functional

  9. Systematization, distribution and territory of the caudal cerebral artery on the brain's surface of the turkey (Meleagris gallopavo

    Directory of Open Access Journals (Sweden)

    Amarílis Díaz de Carvalho

    2014-10-01

    Full Text Available Thirty Meleagris gallopavo heads with their neck segments were used. Animals were contained and euthanized with the association of mebezonium iodide, embutramide and tetracaine hydrochloride (T 61, Intervet by intravenous injection. The arterial system was rinsed with cold saline solution (15°C, with 5000IU heparin and filled with red-colored latex. The samples were fixed in 20% formaldehyde for seven days. The brains were removed with a segment of cervical spinal cord and after, the dura-mater was removed and the arteries dissected. The cerebral carotid arteries, after the intercarotid anastomosis, were projected around the hypophysis, until they reached the tuber cinereum and divided into their terminal branches, the caudal branch and the rostral branch. The rostral branch was projected rostrolateralwards and gave off, in sequence, two collateral branches, the caudal cerebral and the middle cerebral arteries and the terminal branch was as cerebroethmoidal artery. The caudal cerebral artery of one antimere formed the interhemispheric artery, which gave off dorsal hemispheric branches to the convex surface of both antimeres. Its dorsal tectal mesencephalic branch, of only one antimere, originated the dorsal cerebellar artery. In the interior of the cerebral transverse fissure, after the origin of the dorsal tectal mesencephalic artery, the caudal cerebral artery emitted occipital hemispheric branches, pineal branches and medial hemispheric branches, on both antimeres. The caudal cerebral artery's territory comprehended the entire surface of the dorsal hemioptic lobe, the rostral surface of the cerebellum, the diencephalic structures, the caudal pole and the medial surface of the cerebral hemisphere and in the convex surface, the sagittal eminence except for its most rostral third. Due to the asymmetry found in the caudal cerebral arteries' ramifications, the models were classified into three types and their respective subtypes.

  10. Pacemaker role of pericytes in generating synchronized spontaneous Ca2+ transients in the myenteric microvasculature of the guinea-pig gastric antrum.

    Science.gov (United States)

    Hashitani, Hikaru; Mitsui, Retsu; Masaki, Shota; Van Helden, Dirk F

    2015-11-01

    Properties of spontaneous Ca(2+) transients in the myenteric microvasculature of the guinea-pig stomach were investigated. Specifically, we explored the spatio-temporal origin of Ca(2+) transients and the role of voltage-dependent Ca(2+) channels (VDCCs) in their intercellular synchrony using fluorescence Ca(2+) imaging and immunohistochemistry. The microvasculature generated spontaneous Ca(2+) transients that were independent of both Ca(2+) transients in interstitial cells of Cajal (ICC) and neural activity. Spontaneous Ca(2+) transients were highly synchronous along the length of microvasculature, and appeared to be initiated in pericytes and spread to arteriolar smooth muscle cells (SMCs). In most cases, the generation or synchrony of Ca(2+) transients was not affected by blockers of L-type VDCCs. In nifedipine-treated preparations, synchronous spontaneous Ca(2+) transients were readily blocked by Ni(2+), mibefradil or ML216, blockers for T-type VDCCs. These blockers also suppressed the known T-type VDCC dependent component of ICC Ca(2+) transients or slow waves. Spontaneous Ca(2+) transients were also suppressed by caffeine, tetracaine or cyclopiazonic acid (CPA). After the blockade of both L- and T-type VDCCs, asynchronous Ca(2+) transients were generated in pericytes on precapillary arterioles and/or capillaries but not in arteriolar SMCs, and were abolished by CPA or nominally Ca(2+) free solution. Together these data indicate that pericytes in the myenteric microvasculature may act as the origin of synchronous spontaneous Ca(2+) transients. Pericyte Ca(2+) transients arise from Ca(2+) release from the sarco-endoplasmic reticulum and the opening of T-type Ca(2+) VDCCs is required for their synchrony and propagation to arteriolar SMCs. Copyright © 2015 Elsevier Ltd. All rights reserved.

  11. The European Society of Regional Anaesthesia and Pain Therapy/American Society of Regional Anesthesia and Pain Medicine Recommendations on Local Anesthetics and Adjuvants Dosage in Pediatric Regional Anesthesia.

    Science.gov (United States)

    Suresh, Santhanam; Ecoffey, Claude; Bosenberg, Adrian; Lonnqvist, Per-Anne; de Oliveira, Gildasio S; de Leon Casasola, Oscar; de Andrés, José; Ivani, Giorgio

    2018-02-01

    Dosage of local anesthetics (LAs) used for regional anesthesia in children is not well determined. In order to evaluate and come to a consensus regarding some of these controversial topics, The European Society of Regional Anaesthesia and Pain Therapy (ESRA) and the American Society of Regional Anesthesia and Pain Medicine (ASRA) developed a Joint Committee Practice Advisory on Local Anesthetics and Adjuvants Dosage in Pediatric Regional Anesthesia. Representatives from both ASRA and ESRA composed the joint committee practice advisory. Evidence-based recommendations were based on a systematic search of the literature. In cases where no literature was available, expert opinion was elicited. Spinal anesthesia with bupivacaine can be performed with a dose of 1 mg/kg for newborn and/or infant and a dose of 0.5 mg/kg in older children (>1 year of age). Tetracaine 0.5% is recommended for spinal anesthesia (dose, 0.07-0.13 mL/kg). Ultrasound-guided upper-extremity peripheral nerve blocks (eg, axillary, infraclavicular, interscalene, supraclavicular) in children can be performed successfully and safely using a recommended LA dose of bupivacaine or ropivacaine of 0.5 to 1.5 mg/kg. Dexmedetomidine can be used as an adjunct to prolong the duration of peripheral nerve blocks in children. High-level evidence is not yet available to guide dosage of LA used in regional blocks in children. The ASRA/ESRA recommendations intend to provide guidance in order to reduce the large variability of LA dosage currently observed in clinical practice.

  12. Dispersive liquid-liquid microextraction prior to field-amplified sample injection for the sensitive analysis of 3,4-methylenedioxymethamphetamine, phencyclidine and lysergic acid diethylamide by capillary electrophoresis in human urine.

    Science.gov (United States)

    Airado-Rodríguez, Diego; Cruces-Blanco, Carmen; García-Campaña, Ana M

    2012-12-07

    A novel capillary zone electrophoresis (CZE) with ultraviolet detection method has been developed and validated for the analysis of 3,4-methylenedioxymethamphetamine (MDMA), lysergic acid diethylamide (LSD) and phencyclidine (PCP) in human urine. The separation of these three analytes has been achieved in less than 8 min in a 72-cm effective length capillary with 50-μm internal diameter. 100 mM NaH(2)PO(4)/Na(2)HPO(4), pH 6.0 has been employed as running buffer, and the separation has been carried out at temperature and voltage of 20°C, and 25kV, respectively. The three drugs have been detected at 205 nm. Field amplified sample injection (FASI) has been employed for on-line sample preconcentration. FASI basically consists in a mismatch between the electric conductivity of the sample and that of the running buffer and it is achieved by electrokinetically injecting the sample diluted in a solvent of lower conductivity than that of the carrier electrolyte. Ultrapure water resulted to be the better sample solvent to reach the greatest enhancement factor. Injection voltage and time have been optimized to 5 kV and 20s, respectively. The irreproducibility associated to electrokinetic injection has been correcting by using tetracaine as internal standard. Dispersive liquid-liquid microextraction (DLLME) has been employed as sample treatment using experimental design and response surface methodology for the optimization of critical variables. Linear responses were found for MDMA, PCP and LSD in presence of urine matrix between 10.0 and 100 ng/mL approximately, and LODs of 1.00, 4.50, and 4.40 ng/mL were calculated for MDMA, PCP and LSD, respectively. The method has been successfully applied to the analysis of the three drugs of interest in human urine with satisfactory recovery percentages. Copyright © 2012 Elsevier B.V. All rights reserved.

  13. Binding sites for. alpha. -bungarotoxin and the noncompetitive inhibitor phencyclidine on a synthetic peptide comprising residues 172-227 of the. alpha. -subunit of the nicotinic acetylcholine receptor

    Energy Technology Data Exchange (ETDEWEB)

    Donnelly-Roberts, D.L.; Lentz, T.L. (Yale Univ., New Haven, CT (United States))

    1991-07-30

    The binding of the competitive antagonist {alpha}-bungarotoxin ({alpha}-Btx) and the noncompetitive inhibitor phencyclidine (PCP) to a synthetic peptide comprising residues 172-227 of the {alpha}-subunit of the Torpedo acetylcholine receptor has been characterized. {sup 125}I-{alpha}-Btx bound to the 172-227 peptide in a solid-phase assay and was competed by {alpha}-Btx d-tubocurarine and NaCl. In the presence of 0.02% sodium dodecyl sulfate, {sup 125}I-{alpha}-Btx bound to the 56-residue peptide with a K{sub D} of 3.5 nM, as determined by equilibrium saturation binding studies. Because {alpha}Btx binds to a peptide comprising residues 173-204 with the same affinity and does not bind to a peptide comprising residues 205-227, the competitive antagonist and hence agonist binding site lies between residues 173 and 204. After photoaffinity labeling, ({sup 3}H)PCP was bound to the 172-227 peptide. ({sup 3}H)PCP binding was inhibited by chlorpromazine, tetracaine, and dibucaine. It is concluded that a high-affinity binding site for PCP is located between residues 205 and 227, which includes the first 18 residues of transmembrane segment M1, and that a low-affinity site is located in the competitive antagonist binding site between residues 173 and 204. These results show that a synthetic peptide comprising residues 172-227 of the {alpha} subunit contains three binding sites, one for {alpha}-Btx and two for PCP. Previous studies on the intact receptor indicate high-affinity PCP binding occurs in the receptor channel.

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

    Energy Technology Data Exchange (ETDEWEB)

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

    1986-04-01

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

  15. Electrophysiological basis of metabolic-syndrome-induced cardiac dysfunction.

    Science.gov (United States)

    Okatan, Esma N; Durak, Aysegul Toy; Turan, Belma

    2016-10-01

    Myocardial contractility is controlled by intracellular Ca2+ cycling with the contribution of sarcoplasmic reticulum (SR). In this study, we aimed to investigate the role of altered SR function in defective regulation of intracellular Ca2+ levels in rats with metabolic syndrome (MetS) induced by a 16-week high-sucrose drinking-water diet. Electric-field stimulated transient intracellular Ca2+ changes in MetS cardiomyocytes exhibited significantly reduced amplitude (∼30%) and prolonged time courses (2-fold), as well as depressed SR Ca2+ loading (∼55%) with increased basal Ca2+ level. Consistent with these data, altered ryanodine receptor (RyR2) function and SERCA2a activity were found in MetS cardiomyocytes through Ca2+ spark measurements and caffeine application assay in a state in which sodium calcium exchanger was inhibited. Furthermore, tetracaine application assay results and hyperphosphorylated level of RyR2 also support the "leaky RyR2" hypothesis. Moreover, altered phosphorylation levels of phospholamban (PLN) support the depressed SERCA2a-activity thesis and these alterations in the phosphorylation of Ca2+-handling proteins are correlated with altered protein kinase and phosphatase activity in MetS cardiomyocytes. In conclusion, MetS-rat heart exhibits altered Ca2+ signaling largely due to altered SR function via changes in RyR2 and SERCA2a activity. These results point to RyR2 and SERCA2a as potential pharmacological targets for restoring intracellular Ca2+ homeostasis and, thereby, combatting dysfunction in MetS-rat heart.

  16. SR-targeted CaMKII inhibition improves SR Ca2+ handling, but accelerates cardiac remodeling in mice overexpressing CaMKIIδC

    Science.gov (United States)

    Huke, Sabine; DeSantiago, Jaime; Kaetzel, Marcia A.; Mishra, Shikha; Brown, Joan H.; Dedman, John R.; Bers, Donald M.

    2010-01-01

    Cardiac myocyte overexpression of CaMKIIδC leads to cardiac hypertrophy and heart failure (HF) possibly caused by altered myocyte Ca2+ handling. A central defect might be the marked CaMKII-induced increase in diastolic sarcoplasmic reticulum (SR) Ca2+ leak which decreases SR Ca2+ load and Ca2+ transient amplitude. We hypothesized that inhibition of CaMKII near the SR membrane would decrease the leak, improve Ca2+ handling and prevent the development of contractile dysfunction and HF. To test this hypothesis we crossbred CaMKIIδC overexpressing mice (CaMK) with mice expressing the CaMKII-inhibitor AIP targeted to the SR via a modified phospholamban (PLB)-transmembrane-domain (SR-AIP). There was a selective decrease in the amount of activated CaMKII in the microsomal (SR/membrane) fraction prepared from these double-transgenic mice (CaMK/SR-AIP) mice. In ventricular cardiomyocytes from CaMK/SR-AIP mice, SR Ca2+ leak, assessed both as diastolic Ca2+ shift into SR upon tetracaine in intact myocytes or integrated Ca2+ spark release in permeabilized myocytes, was significantly reduced. The reduced leak was accompanied by enhanced SR Ca2+ load and twitch amplitude in double-transgenic mice (vs. CaMK), without changes in SERCA expression or NCX function. However, despite the improved myocyte Ca2+ handling, cardiac hypertrophy and remodeling was accelerated in CaMK/SR-AIP and cardiac function worsened. We conclude that while inhibition of SR localized CaMKII in CaMK mice improves Ca2+ handling, it does not necessarily rescue the HF phenotype. This implies that a non-SR CaMKIIδC exerts SR-independent effects that contribute to hypertrophy and HF, and this CaMKII pathway may be exacerbated by the global enhancement of Ca transients. PMID:20971119

  17. Calmodulin kinase II inhibition limits the pro-arrhythmic Ca2+ waves induced by cAMP-phosphodiesterase inhibitors.

    Science.gov (United States)

    Bobin, Pierre; Varin, Audrey; Lefebvre, Florence; Fischmeister, Rodolphe; Vandecasteele, Grégoire; Leroy, Jérôme

    2016-05-01

    A major concern of using phosphodiesterase (PDE) inhibitors in heart failure is their potential to increase mortality by inducing arrhythmias. By diminishing cyclic adenosine monophosphate (cAMP) hydrolysis, they promote protein kinase A (PKA) activity under β-adrenergic receptor (β-AR) stimulation, hence enhancing Ca(2+) cycling and contraction. Yet, cAMP also activates CaMKII via PKA or the exchange protein Epac, but it remains unknown whether these pathways are involved in the pro-arrhythmic effect of PDE inhibitors. Excitation-contraction coupling was investigated in isolated adult rat ventricular myocytes loaded with Fura-2 and paced at 1 Hz allowing coincident measurement of intracellular Ca(2+) and sarcomere shortening. The PDE4 inhibitor Ro 20-1724 (Ro) promoted the inotropic effects of the non-selective β-AR agonist isoprenaline (Iso) and also spontaneous diastolic Ca(2+) waves (SCWs). PDE4 inhibition potentiated RyR2 and PLB phosphorylation at specific PKA and CaMKII sites increasing sarcoplasmic reticulum (SR) Ca(2+) load and SR Ca(2+) leak measured in a 0Na(+)/0Ca(2+) solution ± tetracaine. PKA inhibition suppressed all the effects of Iso ± Ro, whereas CaMKII inhibition prevented SR Ca(2+) leak and diminished SCW incidence without affecting the inotropic effects of Ro. Inhibition of Epac2 but not Epac1 diminished the occurrence of SCWs. PDE3 inhibition with cilostamide induced an SR Ca(2+) leak, which was also blocked by CaMKII inhibition. Our results show that PDE inhibitors exert inotropic effects via PKA but lead to SCWs via both PKA and CaMKII activation partly via Epac2, suggesting the potential use of CaMKII inhibitors as adjuncts to PDE inhibition to limit their pro-arrhythmic effects. Published on behalf of the European Society of Cardiology. All rights reserved. © The Author 2016. For permissions please email: journals.permissions@oup.com.

  18. Evaluation of antimicrobial effectiveness of ophthalmic drops according to the pharmacopeial tests criteria

    Directory of Open Access Journals (Sweden)

    N Samadi

    2009-03-01

    Full Text Available ABSTRACT Background: In this study antimicrobial effectiveness test was performed on eye-drops which had high microbial contaminations in hospital practice to find out whether their antimicrobial efficacies affect the magnitude of microbial contamination during their uses. Materials and Methods: Artificial tear, atropine sulfate, betamethasone, homatropine hydrobromide, phenylephrine hydrochloride, phenylephrine zinc, pilocarpine hydrochloride, tetracaine hydrochloride and tropicamide eye-drops were subjected to the United States Pharmacopeia (USP and British Pharmacopeia (BP antimicrobial preservative effectiveness tests. Results: The results of this study showed that eight out of the nine products met the BP 'B' and USP criteria. The preservative employed in phenylephrine zinc eye-drop did not possess adequate antimicrobial activity against P. aeruginosa. Other eye-drops showed appropriate reductions in bacterial viability after 6 hrs, 24 hrs and 7 days, but showed a very low bacterial recovery after 28 days which didn't comply with the no recovery (NR term of BP 'A' criteria. Since viable microbial counts were usually determined by plate count method, it seems that the term of NR should define an acceptable range. Conclusion: The results indicated that there is not a clear correlation between antimicrobial efficacy testing of eye-drops and the rate of their microbial contamination while are being used. Other factors such as hygienic practices of eye-drops, proper bottle design and training of patients could influence their microbial contaminations. Regulation of in-use efficacy testing of eye-drops which is influenced by the environment, the frequency and technique of use, might be essential

  19. Venom ophthalmia caused by venoms of spitting elapid and other snakes: Report of ten cases with review of epidemiology, clinical features, pathophysiology and management.

    Science.gov (United States)

    Chu, Edward R; Weinstein, Scott A; White, Julian; Warrell, David A

    2010-09-01

    Venom ophthalmia caused by venoms of spitting elapid and other snakes: report of ten cases with review of epidemiology, clinical features, pathophysiology and management. Chu, ER, Weinstein, SA, White, J and Warrell, DA. Toxicon XX:xxx-xxx. We present ten cases of ocular injury following instillation into the eye of snake venoms or toxins by spitting elapids and other snakes. The natural history of spitting elapids and the toxinology of their venoms are reviewed together with the medical effects and management of venom ophthalmia in humans and domestic animals including both direct and allergic effects of venoms. Although the clinical features and management of envenoming following bites by spitting elapids (genera Naja and Hemachatus) are well documented, these snakes are also capable of "spraying" venom towards the eyes of predators, a defensive strategy that causes painful and potentially blinding ocular envenoming (venom ophthalmia). Little attention has been given to the detailed clinical description, clinical evolution and efficacy of treatment of venom ophthalmia and no clear management guidelines have been formulated. Knowledge of the pathophysiology of ocular envenoming is based largely on animal studies and a limited body of clinical information. A few cases of ocular exposure to venoms from crotaline viperids have also been described. Venom ophthalmia often presents with pain, hyperemia, blepharitis, blepharospasm and corneal erosions. Delay or lack of treatment may result in corneal opacity, hypopyon and/or blindness. When venom is "spat" into the eye, cranial nerve VII may be affected by local spread of venom but systemic envenoming has not been documented in human patients. Management of venom ophthalmia consists of: 1) urgent decontamination by copious irrigation 2) analgesia by vasoconstrictors with weak mydriatic activity (e.g. epinephrine) and limited topical administration of local anesthetics (e.g. tetracaine) 3) exclusion of corneal abrasions

  20. Simultaneous determination of four local anesthetics by CE with ECL and study on interaction between procainamide and human serum albumin.

    Science.gov (United States)

    Duan, Hong-Bing; Cao, Jun-Tao; Yang, Jiu-Jun; Wang, Hui; Liu, Yan-Ming

    2016-07-01

    A new method of capillary electrophoresis (CE) coupled with tris(2, 2'-bipyridyl) ruthenium(II) electrochemiluminescence (ECL) detection has been developed to detect four local anesthetics procainamide (PAH), tetracaine (TCH), proparacaine (PCH) and cinchocaine (CIN) simultaneously. An europium (III)-doped prussian blue analogue film (Eu-PB) modified platinum electrode was prepared and applied to improve the detection sensitivity. The parameters including additives, concentration and pH of the running buffer, separation voltage and detection potential that affect CE separation and ECL detection were optimized in detail. The four local anesthetics were baseline separated and detected within 10min under the optimized conditions. The detection limits (LOD) of PAH, TCH, PCH and CIN are 5.5×10(-8), 9.6×10(-8), 2.5×10(-8) and 3.5×10(-8)molL(-1) (S/N=3), respectively. RSDs of the migration time for four analytes range from 1.2% to 2.5% within intraday and from 2.4% to 4.9% in interday, RSDs of the peak area for four analytes are from 1.7% to 3.3% within intraday and from 2.2% to 5.6% in interday, respectively. The limits of quantitation (LOQ) (S/N=10) for PAH, TCH, PCH and CIN in human urine sample are 5.9×10(-7), 9.2×10(-7), 8.3×10(-7) and 5.0×10(-7)molL(-1), separately. The recoveries (n=3) of four analytes in human urine are from 87.6% to 107.7% with less than 5.9% in RSDs. The developed method was used to determine four local anesthetics in human urine samples and investigate the interaction between PAH and human serum albumin (HSA). The number of binding sites and the binding constant of PAH with HSA were calculated to be 1.03 and 2.4×10(4)Lmol(-1), respectively. Copyright © 2016 Elsevier B.V. All rights reserved.

  1. Masked comparison of silicone hydrogel lotrafilcon A and etafilcon A extended-wear bandage contact lenses after photorefractive keratectomy.

    Science.gov (United States)

    Engle, Andrew T; Laurent, John M; Schallhorn, Steven C; Toman, Steven D; Newacheck, James S; Tanzer, David J; Tidwell, James L

    2005-04-01

    To compare the efficacy of 2 types of bandage contact lenses (BCLs) after photorefractive keratectomy (PRK). Navy Refractive Surgery Center, Naval Medical Center San Diego, San Diego, California, USA. In this prospective study, 100 patients received PRK in both eyes. Each patient received a BCL composed of etafilcon A (Acuvue [ACV], Vistakon Inc.) (14.0 diameter, 8.4/8.8 base curve) in 1 eye and lotrafilcon A (Focus Night & Day [N&D], Ciba Vision) (13.8 diameter, 8.4/8.6 base curve) in the fellow eye. The patient was masked to the lens type in each eye. The postoperative medication regimen was the same with both lenses. The epithelial defect size and subjective level of discomfort were measured at surgery and daily after surgery until both eyes had reepithelialized and the lenses were removed. The mean epithelial defect size at surgery was similar with both BCLs (ACV 57.07 mm(2) and N&D 57.53 mm(2); P=.422). On postoperative days 1 and 2, the mean defect size was significantly smaller in eyes with the N&D lens (day 1, ACV 21.53 and N&D 18.74; day 2, ACV 3.62 and N&D 2.12) (paired t test, Plenses and 13 eyes with ACV lenses had. On day 3, 70 eyes with N&D lenses and 66 eyes with ACV lenses had reepithelialized. The mean discomfort index was significantly higher in the eyes with ACV lenses on days 1 and 2 (paired t test, Plenses on days 1, 2, and 3 (paired t test, P<.001, P<.008, P<.003, respectively). No correlation between the use of tetracaine in the first 24 hours and the rate of reepithelialization was noted (R(2)=0.0025 for ACV and R(2)=0.0003 for N&D). The lotrafilcon A lens resulted in significantly faster corneal reepithelialization and reduced patient discomfort in most patients during the first 48 hours after PRK.

  2. Bupropion Binds to Two Sites in the Torpedo Nicotinic Acetylcholine Receptor Transmembrane Domain: A Photoaffinity Labeling Study with the Bupropion Analog [125I]-SADU-3-72

    Science.gov (United States)

    Pandhare, Akash; Hamouda, Ayman K.; Staggs, Brandon; Aggarwal, Shaili; Duddempudi, Phaneendra K.; Lever, John R.; Lapinsky, David J.; Jansen, Michaela; Cohen, Jonathan B.; Blanton, Michael P.

    2012-01-01

    Bupropion, a clinically-used antidepressant and smoking-cessation drug, acts as a noncompetitive antagonist of nicotinic acetylcholine receptors (nAChRs). To identify its binding site(s) in nAChRs, we developed a photoreactive bupropion analog, (±)-2-(N-tert-butylamino)-3′-[125I]-iodo-4′-azidopropiophenone (SADU-3-72). Based upon inhibition of [125I]SADU-3-72 binding, SADU-3-72 binds with high affinity (IC50 = 0.8 μM) to the Torpedo nAChR in the resting (closed channel) state and in the agonist-induced desensitized state, and bupropion binds to that site with three-fold higher affinity in the desensitized (IC50 = 1.2 μM) than in the resting state. Photolabeling of Torpedo nAChRs with [125I]SADU-3-72 followed by limited in-gel digestion of nAChR subunits with endoproteinase Glu-C established the presence of [125I]SADU-3-72 photoincorporation within nAChR subunit fragments containing M1-M2-M3 helices (αV8-20K, βV8-22/23K and γV8-24K) or M1-M2 helices (δV8-14). Photolabeling within βV8-22/23K, γV8-24K and δV8-14 was reduced in the desensitized state and inhibited by ion channel blockers selective for the resting (tetracaine) or desensitized (thienycyclohexylpiperidine (TCP)) state, and this pharmacologically specific photolabeling was localized to the M2-9 leucine ring (δLeu265, βLeu257) within the ion channel. In contrast, photolabeling within the αV8-20K was enhanced in the desensitized state and not inhibited by TCP, but was inhibited by bupropion. This agonist-enhanced photolabeling was localized to αTyr213 in αM1. These results establish the presence of two distinct bupropion binding sites within the Torpedo nAChR transmembrane domain: a high affinity site at the middle (M2-9) of the ion channel and a second site near the extracellular end of αM1 within a previously described halothane (general anesthetic) binding pocket. PMID:22394379

  3. Bupropion binds to two sites in the Torpedo nicotinic acetylcholine receptor transmembrane domain: a photoaffinity labeling study with the bupropion analogue [(125)I]-SADU-3-72.

    Science.gov (United States)

    Pandhare, Akash; Hamouda, Ayman K; Staggs, Brandon; Aggarwal, Shaili; Duddempudi, Phaneendra K; Lever, John R; Lapinsky, David J; Jansen, Michaela; Cohen, Jonathan B; Blanton, Michael P

    2012-03-27

    Bupropion, a clinically used antidepressant and smoking-cessation drug, acts as a noncompetitive antagonist of nicotinic acetylcholine receptors (nAChRs). To identify its binding site(s) in nAChRs, we developed a photoreactive bupropion analogue, (±)-2-(N-tert-butylamino)-3'-[(125)I]-iodo-4'-azidopropiophenone (SADU-3-72). Based on inhibition of [(125)I]SADU-3-72 binding, SADU-3-72 binds with high affinity (IC(50) = 0.8 μM) to the Torpedo nAChR in the resting (closed channel) state and in the agonist-induced desensitized state, and bupropion binds to that site with 3-fold higher affinity in the desensitized (IC(50) = 1.2 μM) than in the resting state. Photolabeling of Torpedo nAChRs with [(125)I]SADU-3-72 followed by limited in-gel digestion of nAChR subunits with endoproteinase Glu-C established the presence of [(125)I]SADU-3-72 photoincorporation within nAChR subunit fragments containing M1-M2-M3 helices (αV8-20K, βV8-22/23K, and γV8-24K) or M1-M2 helices (δV8-14). Photolabeling within βV8-22/23K, γV8-24K, and δV8-14 was reduced in the desensitized state and inhibited by ion channel blockers selective for the resting (tetracaine) or desensitized (thienycyclohexylpiperidine (TCP)) state, and this pharmacologically specific photolabeling was localized to the M2-9 leucine ring (δLeu(265), βLeu(257)) within the ion channel. In contrast, photolabeling within the αV8-20K was enhanced in the desensitized state and not inhibited by TCP but was inhibited by bupropion. This agonist-enhanced photolabeling was localized to αTyr(213) in αM1. These results establish the presence of two distinct bupropion binding sites within the Torpedo nAChR transmembrane domain: a high affinity site at the middle (M2-9) of the ion channel and a second site near the extracellular end of αM1 within a previously described halothane (general anesthetic) binding pocket.

  4. Comparison of two column characterisation systems based on pharmaceutical applications.

    Science.gov (United States)

    Haghedooren, Erik; Németh, Tamás; Dragovic, Sanja; Noszál, Béla; Hoogmartens, Jos; Adams, Erwin

    2008-05-02

    A useful column characterisation system should help chromatographers to select the most appropriate column to use, e.g. when a particular chromatographic column is not available or when facing the dilemma of selecting a suitable column for analysis according to an official monograph. Official monographs of the European Pharmacopoeia and the United States Pharmacopeia are not allowed to mention the brand name of the stationary phase used for the method development. Also given the overwhelming offer of several hundreds of commercially available reversed-phase liquid chromatographic columns, the choice of a suitable column could be difficult sometimes. To support rational column selection, a column characterisation study was started in our laboratory in 2000. In the same period, Euerby et al. also developed a column characterisation system, which is now released as Column Selector by ACD/Labs. The aim of this project was to compare the two existing column characterisation systems, i.e. the KUL system and the Euerby system. Other research groups active in this field will not be discussed here. Euerby et al. developed a column characterisation system based on 6 test parameters, while the KUL system is based on 4 chromatographic parameters. Comparison was done using a set of 63 columns. For 7 different pharmaceutical separations (fluoxetine, gemcitabine, erythromycin, tetracycline, tetracaine, amlodipine and bisacodyl), a ranking was built based on an F-value (KUL method) or Column Difference Factor value (Euerby method) versus a (virtual) reference column. Both methods showed a similar ranking. The KUL and Euerby methods do not perfectly match, but they yield very similar results, allowing with a relatively high certainty, the selection of similar or dissimilar columns as compared to a reference column. An analyst that uses either of the two methods, will end up with a similar ranking. From a practical point of view, it must be noted that the KUL method only includes 4

  5. Charge movements in intact amphibian skeletal muscle fibres in the presence of cardiac glycosides.

    Science.gov (United States)

    Huang, C L

    2001-04-15

    1. Intramembrane charge movements were examined in intact voltage-clamped amphibian muscle fibres following treatment with cardiac glycosides in the hypertonic gluconate-containing solutions hitherto reported to emphasise the features of q(gamma) at the expense of q(beta) charge. 2. The application of chlormadinone acetate (CMA) at concentrations known selectively to block Na(+)-K(+)-ATPase conserved the steady-state voltage dependence of intramembrane charge, contributions from delayed (q(gamma)) charging transients, and their inactivation characteristics brought about by shifts in holding potential. 3. The addition of either ouabain (125, 250 or 500 nM) or digoxin (5 nM) at concentrations previously reported additionally to influence excitation-contraction coupling similarly conserved the steady-state charge-voltage relationships, Q(V), in fully polarised fibres to give values of maximum charge, Q(max), transition voltage, V*, and steepness factor, k, that were consistent with a persistent q component as reported on earlier occasions (Q(max) approximately = 25-27 nC F-1, V* approximately = -45 to -50 mV, k approximately = 7-9 mV). 4. In both cases shifts in holding potential from -90 to -50 mV produced a partial inactivation that separated steeply and more gradually voltage-dependent charge components in agreement with previous characterisations. 5. However, charge movements that were observed in the presence of either digoxin or ouabain were monotonic decays in which delayed (q(gamma)) transients could not be distinguished from the early charging records. These features persisted despite the further addition of chlormadinone acetate over a 10-fold concentration range (5-50 microM) known to displace ouabain from the Na(+)-K(+)-ATPase. 6. Ouabain (500 nM) restored the steady-state charge movement that was previously abolished by the addition of 2.0 mM tetracaine in common with previous results of using ryanodine receptor (RyR)-specific agents. 7. Perchlorate (8

  6. Comparação entre a dor provocada pela facoemulsificação com anestesia tópica e a pela infiltração peribulbar sem sedação Comparison between the pain induced by phacoemulsification with topical anesthesia and by peribulbar anesthesia without sedation

    Directory of Open Access Journals (Sweden)

    Roberto Pinto Coelho

    2005-02-01

    Full Text Available OBJETIVO: Comparar a sensação de dor produzida pela realização de facoemulsificação com anestesia tópica com a induzida pela infiltração peribulbar de solução anestésica. MÉTODOS: Usando-se uma escala visual análoga de dor de 10 níveis, mediu-se em 20 pacientes, a dor provocada pela realização de facoemulsificação com anestesia tópica (tetracaína 2%. A mesma escala foi usada para medir em 21 outros pacientes, a dor provocada pela infiltração peribulbar de solução anestésica (lidocaína a 2% e bupivacaína 0,5%. As infiltrações peribulbares e cirurgias foram feitas pelo mesmo cirurgião. As facoemulsificações foram realizadas com acesso "clear cornea" e implante de lente intra-ocular dentro do saco capsular. Não foi administrada qualquer medicação venosa ou via oral. Os valores de dor nos dois grupos estudados foram comparados pelo teste, não paramétrico, de Mann-Whitney U. RESULTADOS: A distribuição dos valores de dor da facectomia com anestesia tópica variou de 0 a 5, com mediana igual a 2. Com a infiltração peribulbar a distribuição obtida foi mais ampla, de 0 a 7, com mediana igual a 3. O teste de Mann-Whitney U, revelou que o "rank" médio do grupo da cirurgia com anestesia tópica (15,78 foi significantemente diferente do obtido com a infiltração peribulbar (25,98 (p=0,0056. CONCLUSÃO: Quando não se emprega sedação, a sensação de dor induzida pela realização da cirurgia da facoemulsificação com anestesia tópica é menor do que a causada pela anestesia peribulbar.PURPOSE: To compare pain sensation induced by phacoemulsification with topical anesthesia with that by peribulbar anesthesia, without sedation. METHODS: Using a 10-level visual pain analogue scale, the pain induced by phacoemulsification with topical anesthesia (2% tetracaine drops was measured in 20 patients. The same scale was used to measure the pain induced by peribulbar anesthesia (2% lidocaine and 0.5% bupivacaine in 21