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Elliot V Hersh, Mana Saraghi, Paul A Moore
BACKGROUND: An intranasal formulation of 3% tetracaine and 0.05% oxymetazoline (Kovanaze) received FDA approval on 29 June 2016. This formulation appears to provide sufficient local anesthesia to perform routine dental restorative (filling) procedures in maxillary teeth from second premolar forward. OBJECTIVES: The aim of this paper is to provide an overview of the efficacy, pharmacokinetics and tolerability of 3% tetracaine plus 0.05% oxymetazoline when administered intranasally...
October 3, 2016: Current Medical Research and Opinion
Svetlana S Efimova, Anastasiia A Zakharova, Ludmila V Schagina, Olga S Ostroumova
The effects of local anesthetics (LAs), including aminoamides and aminoesters, on the characteristics of single gramicidin A (GA) channels in 1,2-dioleoyl-sn-glycero-3-phosphocholine (DOPC) bilayers were studied. Aminoamides, namely lidocaine (LDC), prilocaine (PLC), mepivacaine (MPV), and bupivacaine (BPV), reduced the conductance of GA channels. Aminoesters influenced the current fluctuations induced by GA differently; procaine (PC) did not affect the fluctuations, whereas tetracaine (TTC) distinctly reduced the conductance of single GA channels...
September 3, 2016: Journal of Membrane Biology
Mohammad Reza Razeghinejad, Masoumeh Masoumpour, Mohammad Hossein Eghbal, Jonathan S Myers, Marlene R Moster
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...
September 2016: Iranian Journal of Medical Sciences
X J Cai, P Mesquida, S A Jones
Nanoparticle-loaded topical formulations can disrupt drug aggregation through controlled drug-nanoparticle interactions to enhance topical drug delivery. However, the complex relationship between the drug, nanoparticle and formulation vehicle requires further understanding. The aim of this study was to use nanoparticle-loaded hydroxypropyl methylcellulose (HPMC) and xanthan gum gels to probe how the drug, nanoparticle and formulation vehicle interactions influenced the delivery of an aggregated drug into the skin...
August 28, 2016: International Journal of Pharmaceutics
Seifollah Jalili, Marzieh Saeedi
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...
August 24, 2016: European Biophysics Journal: EBJ
Zhixin Lin, Sonia Santos, Karen Padilla, David Printzenhoff, Neil A Castle
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...
2016: PloS One
Aimin Tan, Yanxin Wu, Guifen Gu, John C Fanaras
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...
October 15, 2016: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
S H Chen, J Zhang, Y N Li, P Ding, Q M Wang
OBJECTIVE: To evaluate the effect of transepithelial corneal collagen cross-linking (CXL) in the treatment of keratoconus. METHODS: 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...
July 2016: [Zhonghua Yan Ke za Zhi] Chinese Journal of Ophthalmology
Wolfgang Uter, Radoslaw Spiewak, Susan M Cooper, Mark Wilkinson, Javier Sánchez Pérez, Axel Schnuch, Marie-Louise Schuttelaar
PURPOSE: The aim of this study was to give an overview of the prevalence of contact allergy to active ingredients and excipients of topical medications across Europe. METHODS: Retrospective analysis of data collected by the European Surveillance System on Contact Allergies ( with substances applied to consecutively patch tested patients, 2009-2012, in 54 departments in 12 European countries. RESULTS: In view of the varying composition of the baseline series used in the previously mentioned departments and countries, between 58 833 (lanolin alcohols) and 16 498 patients (sodium metabisulfite) were patch tested with the topical agents covered in this study...
July 28, 2016: Pharmacoepidemiology and Drug Safety
Margaret M Reynolds, Kerryl E Greenwood-Quaintance, Robin Patel, Jose S Pulido
PURPOSE: Endophthalmitis is a rare complication of intravitreal injection (IVI). It is recommended that povidone-iodine be the last agent applied before IVI. Patients have reported povidone-iodine application to be the most bothersome part of IVIs. Topical anesthetics have been demonstrated to have antibacterial effects. This study compared the minimum inhibitory concentration (MIC) of topical anesthetic eye drops (proparacaine 0.5%, tetracaine 0.5%, lidocaine 2.0%) and the antiseptic, 5...
July 2016: Translational Vision Science & Technology
Anthony T Cacek, Jogarao V S Gobburu, Mathangi Gopalakrishnan
The primary objective of the current investigation was to establish the pharmacokinetic characteristics of oxymetazoline and tetracaine's primary metabolite, para-butylaminobenzoic acid (PBBA), after the intranasal administration of K305. Thirty six subjects contributing a total of 1791 plasma concentration results from two open label trials were utilized. Model development was achieved using data from the second trial (N = 24) in which 0.3 mg oxymetazoline/18 mg tetracaine was administered. External model validation utilized data from the first trial (N = 12) which included doses of 0...
July 19, 2016: Journal of Clinical Pharmacology
Anikó Lajtai, Mátyás Mayer, Ágnes Lakatos, Zoltán Porpáczy, Attila Miseta
Tanax(®) (T-61) is a euthanasia solution commonly used in veterinary medicine in Europe. It consists of three active components: embutramide, mebezonium iodide, and tetracaine hydrochloride. Human consumption of Tanax(®) (T-61) is usually associated with suicide attempts. In our 15-year-long practice, embutramide was detected only three times but within a short period. First, it was found in the urine of a 42-year-old veterinarian, and the other two observations were made in a 16-year-old young man. Urine samples were analyzed using Shimadzu Prominence TOX...
March 2016: Journal of Forensic Sciences
K Greveling, E P Prens, N Ten Bosch, M van Doorn
BACKGROUND: Pain is a common adverse effect during dermatological laser procedures. Currently, no standard topical anaesthetic cream exists for deeper dermal laser procedures. OBJECTIVE: To compare the efficacy of lidocaine/tetracaine cream and lidocaine/prilocaine cream in reducing self-reported pain during deeper dermal laser treatments of acne keloidalis nuchae (AKN) and tattoos. METHODS: We conducted two randomized, double-blind, controlled clinical trials with intra-patient, split-lesion design: Study A in patients with AKN (n=15), and Study B in patients with black tattoos (n=15)...
July 5, 2016: British Journal of Dermatology
Rosendo Pérez-Isidoro, J C Ruiz-Suárez
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...
September 2016: Biochimica et Biophysica Acta
Metavee Boonsiri, Katherine C Marks, Chérie M Ditre
Practitioners are increasingly using topical anesthetics in the field of dermatology. Application of topical anesthetics prior to performing dermatologic procedures has proven to decrease pain and discomfort associated with these procedures. Despite the prevalent use of topical anesthetics, there are few standard guidelines for about which products provide optimal and safest use. Adverse events are often correlated with improper application of topical anesthetics. A few case reports have cited adverse events related to the use of compounded products that the United States Food and Drug Administration has not approved, such as benzocaine, lidocaine, tetracaine...
March 2016: Journal of Clinical and Aesthetic Dermatology
Hui Wu, Yuan Hu, Xiao-Ru Shi, Feihong Xu, Chun-Ying Jiang, Rong Huang, Hui Jia
The present report describes the clinical course and treatment of a Mooren-like ulcer associated with abuse of topical anesthetics and dexamethasone. A 38-year-old male physician treated himself with lidocaine, tetracaine and dexamethasone (DEX) eye drops for severe pain and decline of vision in both eyes. After six months of treatment, his right cornea exhibited annular melting with full-thickness stromal infiltration at the limbus and central corneal haze. His left cornea was completely melted and exhibited iris prolapse...
July 2016: Experimental and Therapeutic Medicine
Esma N Okatan, Aysegul Toy Durak, Belma Turan
Myocardial contractility is controlled by intracellular Ca(2+) 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 Ca(2+) levels in rats with metabolic syndrome (MetS) induced by a 16-week high-sucrose drinking-water diet. Electric-field stimulated transient intracellular Ca(2+) changes in MetS cardiomyocytes exhibited significantly reduced amplitude (∼30%) and prolonged time courses (2-fold), as well as depressed SR Ca(2+) loading (∼55%) with increased basal Ca(2+) level...
April 12, 2016: Canadian Journal of Physiology and Pharmacology
T Kavanagh, A Dube, A Albert, V Gunka
BACKGROUND: Between 10-22% of the general population experience needle phobia. Needle phobic parturients are at increased risk of adverse outcomes. We assessed the efficacy of topical Ametop™ (tetracaine 4%) gel in reducing the pain associated with local anesthetic skin infiltration before neuraxial block in non-laboring women. METHODS: This was a prospective, randomized, double-blind, placebo-controlled study. Ametop™ or placebo was applied to the skin of the lower back at least 20min before neuraxial block using a standardized technique with 1% lidocaine skin infiltration...
August 2016: International Journal of Obstetric Anesthesia
Itai Shavit, Yael Peri-Front, Anda Rosen-Walther, Ruth E Grunau, Gal Neuman, Omri Nachmani, Gideon Koren, Dror Aizenbud
OBJECTIVE: To examine the comparative effectiveness of two topical anesthetics in controlling the pain associated with tongue-tie release (frenotomy) in young infants. DESIGN: Randomized trial. SETTING: A Pediatric Craniofacial Clinic. SUBJECTS: Forty-two infants who were referred for frenotomy were randomly allocated to receive the topical anesthetic gel 2% tetracaine or 20% benzocaine applied prior to frenotomy. Frenotomies were videotaped...
June 6, 2016: Pain Medicine: the Official Journal of the American Academy of Pain Medicine
Shihao Chen, Tommy C Y Chan, Jia Zhang, Ping Ding, Jason C K Chan, Marco C Y Yu, Yini Li, Vishal Jhanji, Qinmei Wang
PURPOSE: To report the 1-year visual and keratometric results of epithelium-on corneal collagen crosslinking (CXL) for advanced keratoconus (median maximum keratometry [K] ≥58.0 diopters [D]). SETTING: School of Ophthalmology and Optometry and Eye Hospital of Wenzhou Medical College, Wenzhou, China. DESIGN: Prospective case series. METHODS: Patients with bilateral progressive keratoconus had tetracaine-enhanced epithelium-on CXL...
May 2016: Journal of Cataract and Refractive Surgery
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