P-Aminobenzoic Acid Derivatives Benzocaine

Total Page：16

File Type：pdf, Size：1020Kb

P-aminobenzoic acid derivatives Benzocaine Mechanism of action oThe loca l anaesthe tics decrease the excitabilit y of nerve cells by decreasing the entry of Na+ ions during upstroke of action pottiltential. oThe local anaesthetics interact with a receptor situated within the voltage sensitiesensitive Na+ channel and raise the threshold of channel opening. oLocal anaesthetic blocks Na+ conductance by two possible modes of action, the tonic and the phasic inhibition. oTonic inhibition results from the binding of LA to nonactivated closed channel while phasic inhibition results from the binding of LA to open state or inactivate state of channels. Uses: For general use as a lubricant and topical anesthetic on esophagus, larynx, mouth, nasal cavity, rectum, respiratory tract or trachea and urinary tract. Procaine MOA: Similar to benzocaine Uses: For general use as a lubricant and topical anesthetic on esophagus, larynx, mouth, nasal cavity, rectum, respiratory tract or trachea and urinary tract. Butamben IUPAC: Butyl 4-aminobenzoate MOA: Similar to benzocaine Uses: For general use as a lubricant and topical anesthetic on esophagus, larynx, mouth, nasal cavity, rectum, respiratory tract or trachea and urinary tract. Butacaine IUPAC: 3-(dibutylamino)propyl 4´-aminobenzoate MOA: Similar to benzocaine Uses: For general use as a lubricant and topical anesthetic on esophagus, larynx, mouth, nasal cavity, rectum, respiratory tract or trachea and urinary tract. Benox inate IUPAC: 2-(diethylamino)ethyl 4´-amino-3´-butoxybenzoate MOA: Similar to benzocaine Uses: For general use as a lubricant and topical anesthetic on esophagus, larynx, mouth, nasal cavity, rectum, respiratory tract or trachea and urinary tract. Tetracaine IUPAC: 2-(dimethylamino)ethyl 4´-(butylamino)benzoate MOA: Similar to benzocaine Uses: For general use as a lubricant and topical anesthetic on esoppghagus, laryyypynx, mouth, nasal cavity, rectum, respiratory tract or trachea and urinary tract..

Copy Link

Recommended publications

Europæisk Patentskrift
(19) DANMARK (1°) DK/EP 2968225 T3 (12) Oversættelse af europæisk patentskrift Patent- og Varemærkestyrelsen (51) lnt.CI.: A 61 K 31/137 (2006.01) A 61 K 9/00 (2006.01) A 61 K 31/245 (2006.01) A 61 K 31/445 (2006.01) A 61 K 31/519 (2006.01) A 61 K 31/52 (2006.01) A 61 P 43/00 (2006.01) (45) Oversættelsen bekendtgjort den: 2019-05-27 (80) Dato for Den Europæiske Patentmyndigheds bekendtgørelse om meddelelse af patentet: 2019-02-20 (86) Europæisk ansøgning nr.: 14719486.4 (86) Europæisk indleveringsdag: 2014-03-17 (87) Den europæiske ansøgnings publiceringsdag: 2016-01-20 (86) International ansøgning nr.: US2014030372 (87) Internationalt publikationsnr.: WO2014145580 (30) Prioritet: 2013-03-15 US 201361789054 P (84) Designerede stater: AL AT BE BG CH CY CZ DE DK EE ES Fl FR GB GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR (73) Patenthaver: The Children's Medical Center Corporation, 55 Shattuck Street, Boston, Massachusetts 02115, USA (72) Opfinder: BERDE, Charles, 14 Doran Road, Bookline, MA 02146, USA KOHANE, Daniel S., 119 Willard Street, Newton, MA 02461, USA (74) Fuldmægtig i Danmark: AWA Denmark A/S, Strandgade 56,1401 København K, Danmark (54) Benævnelse: NEOSAXITOXINKOMBINATIONSFORMULERINGER TIL FORLÆNGET LOKALANÆSTESI (56) Fremdragne publikationer: WO-A2-98/51290 ALBERTO J. RODRIGUEZ-NAVARRO ET AL: "Potentiation of Local Anesthetic Activity of Neosaxitoxin with Bupivacaine or Epinephrine: Development of a Long-Acting Pain Blocker", NEUROTOXICITY RESEARCH, vol. 16, no. 4, 28 July 2009 (2009-07-28), pages 408-415, XP055122925, ISSN: 1029-8428, DOI: 10.1007/s12640-009- 9092-3 cited in the application Anonymous: "NCT01786655 on 2013_02_11: ClinicalTrials.gov Archive",, 11 February 2013 (2013-02-11), XP055122935, Retrieved from the Internet: URL:http://clinicaltrials.gov/archive/NCTO 1786655/2013_02_11 [retrieved on 2014-06-12] CHARLES B.
[Show full text]
3-Local-Anesthetics.Pdf
Overview • Local anesthetics produce a transient and reversible loss of sensation (analgesia) in a circumscribed region of the body without loss of consciousness. • Normally, the process is completely reversible. • Local anesthetics are generally classified as either esters or amides and are usually linked to: – a lipophilic aromatic group – to a hydrophilic, ionizable tertiary (sometimes secondary) amine. • Most are weak bases with pKa ( 8 – 9), and at physiologic pH they are primarily in the charged, cationic form. • The potency of local anesthetics is positively correlated with their lipid solubility, which may vary 16-fold, and negatively correlated with their molecular size. • These anesthetics are selected for use on the basis of: 1. the duration of drug action • Short: 20 min • Intermediate: 1—1.5 hrs • Long: 2—4 hrs 2. effectiveness at the administration site 3. potential for toxicity Mechanism of action Local anesthetics act by blocking sodium channels and the conduction of action potentials along sensory nerves. • Blockade is voltage dependent and time dependent. a. At rest, the voltage-dependent sodium (Na+) channels of sensory nerves are in the resting (closed) state. • Following the action potential the Na+ channel becomes active (open) and then converts to an inactive (closed) state that is insensitive to depolarization. • Following repolarization of the plasma membrane there is a slow reversion of channels from the inactive to the resting state, which can again be activated by depolarization. • During excitation the cationic charged form of local anesthetics interacts preferentially with the inactivated state of the Na+ channels on the inner aspect of the sodium channel to block sodium current and increase the threshold for excitation.
[Show full text]
Prolonged Release of the Local Anesthetic Butamben for Potential Use in Pain Management
Pharmacology & Pharmacy, 2012, 3, 291-294 291 http://dx.doi.org/10.4236/pp.2012.33038 Published Online July 2012 (http://www.SciRP.org/journal/pp) Prolonged Release of the Local Anesthetic Butamben for Potential Use in Pain Management Ashish Rastogi1,2, Salomon Stavchansky2, Phillip D. Bowman1* 1US Army Institute of Surgical Research, Fort Sam Houston, USA; 2Division of Pharmaceutics, College of Pharmacy, The Univer- sity of Texas at Austin, Austin, USA. Email: [email protected], *[email protected] Received March 20th, 2012; revised April 29th, 2012; accepted May 11th, 2012 ABSTRACT Continuous delivery of local anesthetics might be useful for management of localized and chronic pain. Controlled re- lease injectable anesthetics have been developed but they can deliver the drug for only few days and the release is not zero-order. A drug delivery system (DDS) consisting of a perforated reservoir for drug containment and release and its potential for management of chronic pain is described. Proof of principle is detailed for long-term zero order delivery of butamben. In this study, the DDS was a polyimide tube with a 0.20 mm hole and butamben release was evaluated in vitro. It is envisioned that the DDS could be implanted in proximity to a nerve, enervating the pain source, for long-term control of chronic pain. Keywords: Controlled Release; Prolonged Drug Delivery; Pain Management; Butamben 1. Introduction operated, and not suitable for everyone [9]. Persistent cerebrospinal fluid leak during its insertion is also a Long-term drug therapy for pain management is chal- known complication [10].
[Show full text]
15-CETY-040, Cetecaine Gel Sell Sheet FA No Crops
Cetacaine® TOPICAL ANESTHETIC GEL (Benzocaine 14.0%, Butamben 2.0%, Tetracaine Hydrochloride 2.0%) Proven more effective than benzocaine alone1 Cetacaine® Topical Anesthetic Gel is a fast-acting, long-lasting prescription topical anesthetic. Applied directly to the mucous membrane, Cetacaine is primarily used to control pain and ease discomfort at the application site. The protective pump-top jar controls the amount of Cetacaine dispensed while keeping the remaining contents safe from cross contamination. The outside lid helps to keep the pump surface clean and intact. Please see the Brief Summary of the Prescribing Information on the reverse side. You are encouraged to report negative side effects of prescription drugs to the FDA. Visit www.fda.gov/medwatch, or call 1-800-FDA-1088. Cetacaine Gel is indicated for anesthesia of all Description Size Item No. accessible mucous membrane except the eyes. Cetacaine Topical Anesthetic Gel 32 g 0217 Cetacaine is not for injection. Features & Benefits • Onset of action: Approximately 30 seconds* • Applies evenly and consistently, tissue need not be dried • Duration of action: 30-60 minutes* • Reacts with body temperature to melt and absorb quickly into tissue • Controls pain and eases discomfort at the application site • Made in USA • Pleasant strawberry flavor • Study shows Cetacaine’s triple formula is more effective than • Lubricating qualities Benzocaine alone Important Safety Information • On rare occasions, methemoglobinemia has been reported in • The most common adverse reaction caused by local anesthetics is connection with the use of benzocaine-containing products. contact dermatitis characterized by erythema and pruritus that If a patient becomes cyanotic, treat appropriately to counteract may progress to vesiculation and oozing.
[Show full text]
Procaine Elisa Kit Instructions Product #103219 & 103216 Forensic Use Only
Neogen Corporation 944 Nandino Blvd., Lexington KY 40511 USA 800/477-8201 USA/Canada | 859/254-1221 Fax: 859/255-5532 | E-mail: [email protected] | Web: www.neogen.com/Toxicology PROCAINE ELISA KIT INSTRUCTIONS PRODUCT #103219 & 103216 FORENSIC USE ONLY INTENDED USE: For the determination of trace quantities of Procaine and/or other metabolites in human urine, blood, oral fluid. DESCRIPTION Neogen Corporation’s Procaine ELISA (Enzyme-Linked ImmunoSorbent Assay) test kit is a qualitative one-step kit designed for use as a screening device for the detection of drugs and/or their metabolites. The kit was designed for screening purposes and is intended for forensic use only. It is recommended that all suspect samples be confirmed by a quantitative method such as gas chromatography/mass spectrometry (GC/MS). ASSAY PRINCIPLES Neogen Corporation’s test kit operates on the basis of competition between the drug or its metabolite in the sample and the drug-enzyme conjugate for a limited number of antibody binding sites. First, the sample or control is added to the microplate. Next, the diluted drug-enzyme conjugate is added and the mixture is incubated at room temperature. During this incubation, the drug in the sample or the drug-enzyme conjugate binds to antibody immobilized in the microplate wells. After incubation, the plate is washed 3 times to remove any unbound sample or drug-enzyme conjugate. The presence of bound drug-enzyme conjugate is recognized by the addition of K-Blue® Substrate (TMB). After a 30 minute substrate incubation, the reaction is halted with the addition of Red Stop Solution.
[Show full text]
Cetacaine Gel Prescribing Information
colored skin (cyanosis); headache; rapid heart rate; shortness of breath; who are hypersensitive to any of its ingredients or to patients known to have lightheadedness; or fatigue. cholinesterase deficiencies. Tolerance may vary with status of the patient. Hypersensitivity Reactions: Unpredictable adverse reactions (i.e. hypersensitivity, Cetacaine Topical Anesthetic Gel should not be used under dentures or cotton including anaphylaxis) are extremely rare. Localized allergic reactions may occur rolls, as retention of the active gel ingredients under a denture or cotton roll could after prolonged or repeated use of any aminobenzoate anesthetic. The most possibly cause an escharotic effect. Routine precaution for the use of any topical Only common adverse reaction caused by local anesthetics is contact dermatitis anesthetic should be observed when using Cetacaine Topical Anesthetic Gel. characterized by erythema and pruritus that may progress to vesiculation and oozing. This occurs most commonly in patients following prolonged How Supplied Cetacaine Topical Anesthetic Gel (Strawberry), 32 g jar Active Ingredients: self-medication, which is contraindicated. If rash, urticaria, edema, or other Benzocaine ...................................................................14.0% manifestations of allergy develop during use, the drug should be discontinued. NDC 10223-0217-3 To minimize the possibility of a serious allergic reaction, Cetacaine Topical Item# 0217 Butamben .......................................................................2.0%
[Show full text]
Local Anesthetics – Substances with Multiple Application in Medicine
ISSN 2411-958X (Print) European Journal of January-April 2016 ISSN 2411-4138 (Online) Interdisciplinary Studies Volume 2, Issue 1 Local Anesthetics – Substances with Multiple Application in Medicine Rodica SÎRBU Ovidius University of Constanta, Faculty of Pharmacy, Campus Corp B, University Alley No. 1, Constanta, Romania Emin CADAR UMF Carol Davila Bucharest, Faculty of Pharmacy, Str. Traian Vuia No. 6, Sector 2, Bucharest, Romania Cezar Laurențiu TOMESCU Ovidius University of Constanta, Faculty of Medicine, Campus Corp B, University Alley No. 1, Constanta, Romania Cristina-Luiza ERIMIA Corresponding author, [email protected] Ovidius University of Constanta, Faculty of Pharmacy, Campus Corp B, University Alley No. 1, Constanta, Romania Stelian PARIS Ovidius University of Constanta, Faculty of Pharmacy, Campus Corp B, University Alley No. 1, Constanta, Romania Aneta TOMESCU Ovidius University of Constanta, Faculty of Medicine, Campus Corp B, University Alley No. 1, Constanta, Romania Abstract Local anesthetics are substances which, by local action groups on the runners, cause loss of reversible a painful sensation, delimited corresponding to the application. They allow small surgery, short in duration and the endoscopic maneuvers. May be useful in soothe teething pain of short duration and in the locking of the nervous disorders in medical care. Local anesthesia is a process useful for the carrying out of surgery and of endoscopic maneuvers, to soothe teething pain in certain conditions, for depriving the temporary structures peripheral nervous control. Reversible locking of the transmission nociceptive, the set of the vegetative and with a local anesthetic at the level of the innervations peripheral nerve, roots and runners, a trunk nervous, around the components of a ganglion or coolant is cefalorahidian practice anesthesia loco-regional.
[Show full text]
Therapeutic Approaches to Genetic Ion Channelopathies and Perspectives in Drug Discovery
fphar-07-00121 May 7, 2016 Time: 11:45 # 1 REVIEW published: 10 May 2016 doi: 10.3389/fphar.2016.00121 Therapeutic Approaches to Genetic Ion Channelopathies and Perspectives in Drug Discovery Paola Imbrici1*, Antonella Liantonio1, Giulia M. Camerino1, Michela De Bellis1, Claudia Camerino2, Antonietta Mele1, Arcangela Giustino3, Sabata Pierno1, Annamaria De Luca1, Domenico Tricarico1, Jean-Francois Desaphy3 and Diana Conte1 1 Department of Pharmacy – Drug Sciences, University of Bari “Aldo Moro”, Bari, Italy, 2 Department of Basic Medical Sciences, Neurosciences and Sense Organs, University of Bari “Aldo Moro”, Bari, Italy, 3 Department of Biomedical Sciences and Human Oncology, University of Bari “Aldo Moro”, Bari, Italy In the human genome more than 400 genes encode ion channels, which are transmembrane proteins mediating ion ﬂuxes across membranes. Being expressed in all cell types, they are involved in almost all physiological processes, including sense perception, neurotransmission, muscle contraction, secretion, immune response, cell proliferation, and differentiation. Due to the widespread tissue distribution of ion channels and their physiological functions, mutations in genes encoding ion channel subunits, or their interacting proteins, are responsible for inherited ion channelopathies. These diseases can range from common to very rare disorders and their severity can be mild, Edited by: disabling, or life-threatening. In spite of this, ion channels are the primary target of only Maria Cristina D’Adamo, University of Perugia, Italy about 5% of the marketed drugs suggesting their potential in drug discovery. The current Reviewed by: review summarizes the therapeutic management of the principal ion channelopathies Mirko Baruscotti, of central and peripheral nervous system, heart, kidney, bone, skeletal muscle and University of Milano, Italy Adrien Moreau, pancreas, resulting from mutations in calcium, sodium, potassium, and chloride ion Institut Neuromyogene – École channels.
[Show full text]
'Butamben, a Specific Local Anesthetic and Aspecific Ion Channel Modulator' Beekwilder, J.P
'Butamben, a specific local anesthetic and aspecific ion channel modulator' Beekwilder, J.P. Citation Beekwilder, J. P. (2008, May 22). 'Butamben, a specific local anesthetic and aspecific ion channel modulator'. Retrieved from https://hdl.handle.net/1887/12865 Version: Corrected Publisher’s Version Licence agreement concerning inclusion of doctoral License: thesis in the Institutional Repository of the University of Leiden Downloaded from: https://hdl.handle.net/1887/12865 Note: To cite this publication please use the final published version (if applicable). 'BUTAMBEN, A SPECIFIC LOCAL ANESTHETIC AND ASPECIFIC ION CHANNEL MODULATOR' PROEFSCHRIFT ter verkrijging van de graad van Doctor aan de Universiteit Leiden, op gezag van Rector Magnificus prof. mr. P.F. van der Heijden, volgens besluit van het College voor Promoties te verdedigen op donderdag 22 mei 2008 klokke 13.45 uur door Jeroen Petrus Beekwilder geboren te Helmond in 1973 Promotiecommissie Promotor: Prof. Dr. D.L. Ypey Copromotor: Dr. R.J. van den Berg Referent: Dr. M.W. Veldkamp (Academisch Medisch Centrum, Amsterdam) Overige leden: Prof. Dr. A. Dahan Prof Dr. W.J. Wadman (Universiteit van Amsterdam) The publication of the thesis has been supported financially by Cyberonics Europe, Vagus Nerve Stimulation (VNS), which is gratefully acknowledged. INDEX/INHOUDSOPGAVE Chapter 1 General Introduction 5 Chapter 2 Kv1.1 channels of dorsal root ganglion neurons are 33 inhibited by n‐butyl‐p‐aminobenzoate, a promising anesthetic for the treatment of chronic pain Chapter 3 Block of Total and N‐type Calcium Conductance in 57 Mouse Sensory Neurons by the Local Anesthetic n‐ Butyl‐p‐Aminobenzoate (Butamben) Chapter 4 The local anesthetic Butamben inhibits and 73 accelerates low‐voltage activated T‐type currents in small sensory neurons.
[Show full text]
Drug and Medication Classification Schedule
KENTUCKY HORSE RACING COMMISSION UNIFORM DRUG, MEDICATION, AND SUBSTANCE CLASSIFICATION SCHEDULE KHRC 8-020-1 (11/2018) Class A drugs, medications, and substances are those (1) that have the highest potential to influence performance in the equine athlete, regardless of their approval by the United States Food and Drug Administration, or (2) that lack approval by the United States Food and Drug Administration but have pharmacologic effects similar to certain Class B drugs, medications, or substances that are approved by the United States Food and Drug Administration. Acecarbromal Bolasterone Cimaterol Divalproex Fluanisone Acetophenazine Boldione Citalopram Dixyrazine Fludiazepam Adinazolam Brimondine Cllibucaine Donepezil Flunitrazepam Alcuronium Bromazepam Clobazam Dopamine Fluopromazine Alfentanil Bromfenac Clocapramine Doxacurium Fluoresone Almotriptan Bromisovalum Clomethiazole Doxapram Fluoxetine Alphaprodine Bromocriptine Clomipramine Doxazosin Flupenthixol Alpidem Bromperidol Clonazepam Doxefazepam Flupirtine Alprazolam Brotizolam Clorazepate Doxepin Flurazepam Alprenolol Bufexamac Clormecaine Droperidol Fluspirilene Althesin Bupivacaine Clostebol Duloxetine Flutoprazepam Aminorex Buprenorphine Clothiapine Eletriptan Fluvoxamine Amisulpride Buspirone Clotiazepam Enalapril Formebolone Amitriptyline Bupropion Cloxazolam Enciprazine Fosinopril Amobarbital Butabartital Clozapine Endorphins Furzabol Amoxapine Butacaine Cobratoxin Enkephalins Galantamine Amperozide Butalbital Cocaine Ephedrine Gallamine Amphetamine Butanilicaine Codeine
[Show full text]
Recommended Methods for the Identification and Analysis of Cocaine in Seized Materials
Recommended methods for the Identification and Analysis of Cocaine in Seized Materials MANUAL FOR USE BY NATIONAL DRUG ANALYSIS LABORATORIES Photo credits: UNODC Photo Library; UNODC/Ioulia Kondratovitch; Alessandro Scotti. Laboratory and Scientific Section UNITED NATIONS OFFICE ON DRUGS AND CRIME Vienna Recommended Methods for the Identification and Analysis of Cocaine in Seized Materials (Revised and updated) MANUAL FOR USE BY NATIONAL DRUG ANALYSIS LABORATORIES UNITED NATIONS New York, 2012 Note Operating and experimental conditions are reproduced from the original reference materials, including unpublished methods, validated and used in selected national laboratories as per the list of references. A number of alternative conditions and substitution of named commercial products may provide comparable results in many cases, but any modification has to be validated before it is integrated into laboratory routines. Mention of names of firms and commercial products does not imply the endorse- ment of the United Nations. ST/NAR/7/REV.1 Original language: English © United Nations, March 2012. All rights reserved. The designations employed and the presentation of material in this publication do not imply the expression of any opinion whatsoever on the part of the Secretariat of the United Nations concerning the legal status of any country, territory, city or area, or of its authorities, or concerning the delimitation of its frontiers or boundaries. This publication has not been formally edited. Publishing production: English, Publishing and Library Section, United Nations Office at Vienna. ii Contents Page 1. Introduction ................................................. 1 1.1 Background .............................................. 1 1.2 Purpose and use of the manual .............................. 1 2. Physical appearance and chemical characteristics of coca leaf and illicit materials containing cocaine ................................
[Show full text]
WO 2008/034819 Al
(12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date PCT (10) International Publication Number 27 March 2008 (27.03.2008) WO 2008/034819 Al (51) International Patent Classification: (81) Designated States (unless otherwise indicated, for every A61K9/00 (2006.01) A61K 31/16 (2006.01) kind of national protection available): AE, AG, AL, AM, A61K 47/18 (2006.01) AT,AU, AZ, BA, BB, BG, BH, BR, BW, BY,BZ, CA, CH, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, (21) International Application Number: ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, PCT/EP2007/059827 IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY,MA, MD, ME, MG, MK, MN, MW, (22) International Filing Date: MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PG, PH, PL, 18 September 2007 (18.09.2007) PT, RO, RS, RU, SC, SD, SE, SG, SK, SL, SM, SV, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, (25) Filing Language: English ZM, ZW (26) Publication Language: English (84) Designated States (unless otherwise indicated, for every kind of regional protection available): ARIPO (BW, GH, (30) Priority Data: GM, KE, LS, MW, MZ, NA, SD, SL, SZ, TZ, UG, ZM, 06121 134.8 22 September 2006 (22.09.2006) EP ZW), Eurasian (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM), (71) Applicant (for all designated States except US): PHAR- European (AT,BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, MATEX ITALIA SRL [IT/IT]; Via Andrea Appiani, 2, FR, GB, GR, HU, IE, IS, IT, LT,LU, LV,MC, MT, NL, PL, 1-20121 Milano (IT).
[Show full text]