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Tetracaine

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https://www.readbyqxmd.com/read/28060026/exponential-decay-metrics-of-topical-tetracaine-hydrochloride-administration-describe-corneal-anesthesia-properties-mechanistically
#1
Jason Ethington, David Goldmeier, Bruce I Gaynes
PURPOSE: To identify pharmacodynamic (PD) and pharmacokinetic (PK) metrics that aid in mechanistic understanding of dosage considerations for prolonged corneal anesthesia. METHODS: A rabbit model using 0.5% tetracaine hydrochloride was used to induce corneal anesthesia in conjunction with Cochet-Bonnet anesthesiometry. Metrics were derived describing PD-PK parameters of the time-dependent domain of recovery in corneal sensitivity. Curve fitting used a 1-phase exponential dissociation paradigm assuming a 1-compartment PK model...
January 4, 2017: Cornea
https://www.readbyqxmd.com/read/28046151/pain-alleviation-during-castration-of-piglets-a-comparative-study-of-different-farm-options
#2
F Gottardo, A Scollo, B Contiero, A Ravagnani, G Tavella, D Bernardini, G M De Benedictis, S A Edwards
Pain alleviation associated with castration of piglets is an important welfare issue. The present study compares the effect of different approaches and products suitable for farmer use, with the aim to alleviate pain due to castration in piglets. A randomized within-litter design, with 28 replicate litters, compared 7 treatments: handling () restraint of the piglet and manipulation of the scrotum, castration without pain relief (), 2 treatments (, ) with different concentrations of tetracaine (2 and 6%) applied topically 10 min before and immediately post-surgery, and 3 treatments with i...
December 2016: Journal of Animal Science
https://www.readbyqxmd.com/read/28017670/presynaptic-facilitation-by-tetracaine-of-glutamatergic-spontaneous-excitatory-transmission-in-the-rat-spinal-substantia-gelatinosa-involvement-of-trpa1-channels
#3
Lian-Hua Piao, Tsugumi Fujita, Ting Yu, Eiichi Kumamoto
The amide-type local anesthetic (LA) lidocaine activates transient receptor potential (TRP) ankyrin-1 (TRPA1) channels to facilitate spontaneous L-glutamate release onto spinal substantia gelatinosa (SG) neurons, which play a crucial role in regulating nociceptive transmission. In contrast, the ester-type LA procaine reduces the spontaneous release of L-glutamate in SG neurons. In order to determine whether TRPA1 activation by LAs is specific to amide-types, we examined the actions of tetracaine, another ester-type LA, and other amide-type LAs on glutamatergic spontaneous excitatory transmission in SG neurons by focusing on TRP activation...
December 22, 2016: Brain Research
https://www.readbyqxmd.com/read/27981712/corneal-anesthetic-effect-and-ocular-tolerance-of-3-5-lidocaine-gel-in-comparison-with-0-5-aqueous-proparacaine-and-0-5-viscous-tetracaine-in-normal-canines
#4
Francesca Venturi, Tiffany Blocker, Darryl Dustin Dees, Richard Madsen, Julius Brinkis
OBJECTIVE: To compare the degree and duration of corneal anesthesia of a novel viscous ophthalmic lidocaine hydrochloride preparation vs. two commonly used ophthalmic anesthetic preparations. METHODS: Each subject was randomly selected to receive 2 of 4 treatments at 2 different time periods separated by a 1 week washout: 3.5% lidocaine hydrochloride gel (Akten(®) ; Akorn Inc., Lake Forest, Illinois, USA), 0.5% aqueous proparacaine hydrochloride (Akorn Inc.), 0...
December 15, 2016: Veterinary Ophthalmology
https://www.readbyqxmd.com/read/27957755/occupational-allergic-contact-dermatitis-caused-by-tetracaine-in-an-otorhinolaryngologist
#5
Morten S Opstrup, Henrik B Sørensen, Claus Zachariae
No abstract text is available yet for this article.
January 2017: Contact Dermatitis
https://www.readbyqxmd.com/read/27920067/injectable-diphenhydramine-used-as-anaesthetic-for-wide-local-excision-with-flap-closure
#6
Laura E Pickett, Jillian Macdonald
BACKGROUND: Lidocaine-allergic patients pose a challenge for cutaneous surgical procedures. We present a case of a successful wide local excision with flap closures on the face using topical tetracaine followed by infiltration with 1% diphenhydramine. CASE SUMMARY: An 84-year-old woman, with a lidocaine intolerance, presented to the Mohs surgery clinic for wide local excision of a nodular basal cell carcinoma on her right medial cheek. Successful anaesthesia was achieved using topical 4% tetracaine followed by intradermal and subcutaneous injection of 1% diphenhydramine...
December 5, 2016: Journal of Cutaneous Medicine and Surgery
https://www.readbyqxmd.com/read/27860187/autophagy-activated-by-tuberin-mtor-p70s6k-suppression-is-a-protective-mechanism-against-local-anaesthetics-neurotoxicity
#7
Jingwei Xiong, Qiuyue Kong, Leyang Dai, He Ma, Xiaofei Cao, Li Liu, Zhengnian Ding
The local anaesthetics (LAs) are widely used for peripheral nerve blocks, epidural anaesthesia, spinal anaesthesia and pain management. However, exposure to LAs for long duration or at high dosage can provoke potential neuronal damages. Autophagy is an intracellular bulk degradation process for proteins and organelles. However, both the effects of LAs on autophagy in neuronal cells and the effects of autophagy on LAs neurotoxicity are not clear. To answer these questions, both lipid LAs (procaine and tetracaine) and amide LAs (bupivacaine, lidocaine and ropivacaine) were administrated to human neuroblastoma SH-SY5Y cells...
November 15, 2016: Journal of Cellular and Molecular Medicine
https://www.readbyqxmd.com/read/27806708/ryanodine-induced-vasoconstriction-of-the-gerbil-spiral-modiolar-artery-depends-on-the-ca-2-sensitivity-but-not-on-ca-2-sparks-or-bk-channels
#8
Gayathri Krishnamoorthy, Katrin Reimann, Philine Wangemann
BACKGROUND: In many vascular smooth muscle cells (SMCs), ryanodine receptor-mediated Ca(2+) sparks activate large-conductance Ca(2+)-activated K(+) (BK) channels leading to lowered SMC [Ca(2+)]i and vasodilation. Here we investigated whether Ca(2+) sparks regulate SMC global [Ca(2+)]i and diameter in the spiral modiolar artery (SMA) by activating BK channels. METHODS: SMAs were isolated from adult female gerbils, loaded with the Ca(2+)-sensitive flourescent dye fluo-4 and pressurized using a concentric double-pipette system...
November 2, 2016: BMC Physiology
https://www.readbyqxmd.com/read/27646144/intranasal-tetracaine-and-oxymetazoline-a-newly-approved-drug-formulation-that-provides-maxillary-dental-anesthesia-without-needles
#9
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
https://www.readbyqxmd.com/read/27592116/local-anesthetics-affect-gramicidin-a-channels-via-membrane-electrostatic-potentials
#10
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...
December 2016: Journal of Membrane Biology
https://www.readbyqxmd.com/read/27582594/glaucoma-surgery-in-pregnancy-a-case-series-and-literature-review
#11
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
https://www.readbyqxmd.com/read/27576666/investigating-the-ability-of-nanoparticle-loaded-hydroxypropyl-methylcellulose-and-xanthan-gum-gels-to-enhance-drug-penetration-into-the-skin
#12
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...
November 20, 2016: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/27557558/study-of-procaine-and-tetracaine-in-the-lipid-bilayer-using-molecular-dynamics-simulation
#13
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
https://www.readbyqxmd.com/read/27556810/biophysical-and-pharmacological-characterization-of-nav1-9-voltage-dependent-sodium-channels-stably-expressed-in-hek-293-cells
#14
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
https://www.readbyqxmd.com/read/27541625/self-initiated-and-concentration-dependent-degradation-of-tetracaine-in-neat-standard-solutions-a-trouble-shooting-story
#15
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
https://www.readbyqxmd.com/read/27531114/-clinical-results-of-transepithelial-corneal-collagen-cross-linking-in-the-treatment-of-keratoconus
#16
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
https://www.readbyqxmd.com/read/27464585/contact-allergy-to-ingredients-of-topical-medications-results-of-the-european-surveillance-system-on-contact-allergies-essca-2009-2012
#17
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 (www.essca-dc.org) 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
https://www.readbyqxmd.com/read/27441100/selected-antimicrobial-activity-of-topical-ophthalmic-anesthetics
#18
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
https://www.readbyqxmd.com/read/27436060/population-pharmacokinetics-of-an-intranasally-administered-combination-of-oxymetazoline-and-tetracaine-in-healthy-volunteers
#19
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 oxymetazoline/tetracaine. Thirty-six subjects contributing a total of 1791 plasma concentration results from 2 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...
February 2017: Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/27404634/embutramide-a-component-of-tanax-%C3%A2-t-61-as-a-new-drug-of-abuse
#20
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
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