DOCSLIB.ORG

Muscle Relaxants

Total Page：16

File Type：pdf, Size：1020Kb

Download full-text PDF Read full-text
Muscle Relaxants Muscle relaxants ●cause relaxation of striated (voluntary skeletal) musculature (in contrast to spasmolytics which relax unstriped musculature) Classification of myorelaxants 1. Neuromuscular blocking drugs ●periferial (direct) myorelaxants: interact with acetylcholine nicotinic (N) receptors of skeletal musculature a) stabilizing myorelaxants – N-receptors antagonists b) depolarizing myorelaxants – N-receptors agonists ●continuous N-receptors stimulation depolarization of cells functional antagonism: further leading of impulses imposible, no muscle contraction c) indirect myorelaxants: botulinum toxin ●irreversibly inhibits acetycholine releasing 2. Central muscle relaxants ●acts in CNS ●structurally heterogenic group ●compounds with various mechanisms of action Stabilizing myorelaxants ●N-receptors antagonists in skeletal muscle cells ●usage: surgical operative measures (often as a part of some form of anaesthesia) ●structures derived from curare alkaloids Curare: arrow poison of South American Indians ●preparation from various plants ●contained a complex mixture of alkaloids Curare classification: according to preparation and package in which it was shipped to Europe 1. Tubocurare: in hollow bamboo rods 2. Calebase curare: in bottle-shaped cucurbits (gourds, calabashes - from plants of genus Strychnos) 3. Pot curare: in ceramic vessels Structural types: 1. Benzyltetrahydroisoquinolines: tubocurarine (from tubocurare) atracurium besylate (synthetic) mivacurium besylate (synthetic) etc. 2. Indole derivatives: toxiferine C alcuronium chloride 3. Steroids with basic substituents: vecuronium bromide pancuronium bromide rocuronium bromide 1. Benzyltetrahydroisoquinolines H3C O H C O O CH3 3 H3C H + H3C H C O O H3C N O 3 OH H C 3 O O H3C H H H + CH + N 3 O O N OH O CH3 N CH3 O O O H3C O CH3 O CH3 tubocurarine atracurium ●used as besylate Tracrium ® inj. sol. 1. Benzyltetrahydroisoquinolines (continued) H C H C 3 O 3 O H3C O O O H3C O H O + H3C + H N CH3 N CH3 CH3 O O O CH3 O O CH3 O CH3 O CH3 mivacurium ●used as besylate Mivacron ® inj. sol. 2. Indole derivatives R OH + N O O H H H H N N H H H N H H H H N + N R HO ●for comparison: strychnine R = -CH toxiferine C 3 ●from Strychnos nux vomica ●natural ●in small amounts as central analeptic R = -CH CH=CH alcuronium 2 2 (obsolete) ●as chloride Stereochemistry: „playing cards symmetry“ toxiferin C alcuronium chloride ●structure similarity with strychnine, both indole alcaloids ●dimer ●2x pentacyclic system ●2 quarternary ammonium moieties Stereochemistry: ●chiral ●contain C2 symmetry axis: „playing cards symmetry“ Effects of alcuronium chloride ●more active than tubocurarine ●relatively short time of action ●not absorbed from GIT ●very stable, excreted in unchanged form Preparation: ●partial synthesis from strychnine 3. Steroids with basic substituents O H CH H C O 3 CH 3 O 3 H3C H H + CH3 H O + N CH3 + N O N H3C H H H C H CH H 3 3 H H N H3C O H H H H H H3C O H O vecuronium pancuronium Norcuron ® inj. Pavulon ® inj. sol. ●as bromides 3. Steroids with basic substituents (continued) H3C H3C H3C + H CH3 O N H3C O O CH3 H + H N H C O N 3 H H3C H O N H + O N H3C H H N CH H H 3 H H2C O H H CH3 H H HO H rocuronium pipecuronium Esmeron ® inj. sol. Arduan ® inj. sicc. + solv. ●facilitation of tracheal intubation Depolarizing myorelaxants ●agonist of N-receptor ●continuous depolarization leads to muscules slack Usage: introduction into general anaesthesia (intubation) Compounds: synthetic bis-quarternary ammonium salts ●originated by simplifying of tubocurarine structure H C 3 CH H3C + 3 O + N O N H C CH CH H3C 3 3 H3C 3 + + CH3 N N - - CH X H C CH3 3 X 3 - - O X X O dekamethonium (halide) suxamethonium (halide) ●non-hydrolyzable syn. succinylcholine (halide) ●comparatively toxic ●hydrolyzable ●long effect ●fast cleft by esterases short effect Succinylcholinjodid Valeant ® inj. plv. sol. Comparison of molecule sizes of direct muscule relaxants Indirect myorelaxants Botulinum toxin ●protein with M about 150, 000 r ●product of anaerobic bacterium Clostridium botulinum (serotypes A – G: A – Botox infusion; B - Neurobloc infusion) ●extremely toxic (food poisoning, potential biologic weapons) Indications: cervical dystonia, facial spasms, writer's cramp and other spasms ●in cosmetics for smoothing of wrinkles – very hazardous ●irreversibly inhibits acetylcholin release ●local injection into the particular muscle ●blocks transfer of impulse by means of acetylcholine to the muscle ●muscle paralysis ●to hands of qualified physicians only ●by no means can reach bloodstream ●new injection is possible after 3 – 4 months (the effect is poorly estimable in shorter intervals due to possible formation of antibodies) Central muscle relaxants (myotonolytics) Using: painful spasms of skeletal muscles (not in surgical measures) Structures: heterogenic group Mechanisms of action: various, not perfectly known in every case ●im most they act sedatively in high doses Central muscle relaxants (myotonolytics) Carbamates derived from diols CH3 CH3 CH3 O O O NH O O O O CH3 H2N NH2 H2N O CH3 H3C meprobamate carisoprodol ●myorelaxant, sedative, anxiolytic ●effectiveness unsure Cl NH2 O H OH baclophene ●GABA derivative ●GABA receptor agonist B 2+ ●blocks voltage-gated input of Ca into CNS neurons Usage: spasmodic conditions (sclerosis multiplex, cramps in crucial region etc.) O - + O N NH N Cl NH O N S N N N thizanidine O ●myorelaxant, analgesic, antihypertensive N ●probably receptors agonist O H 2 ●blocks release of excitation dantrolene transmitters (glutamate, ●hydantoine derivative aspartate) ●myorelaxant ●usage: eg. sclerosis ●Mode of action: directly to skeletal multiplex, ischias 2+ muscles; lowers Ca release .
Load more

Recommended publications
  • Pharmacy and Poisons (Third and Fourth Schedule Amendment) Order 2017
    Q UO N T FA R U T A F E BERMUDA PHARMACY AND POISONS (THIRD AND FOURTH SCHEDULE AMENDMENT) ORDER 2017 BR 111 / 2017 The Minister responsible for health, in exercise of the power conferred by section 48A(1) of the Pharmacy and Poisons Act 1979, makes the following Order: Citation 1 This Order may be cited as the Pharmacy and Poisons (Third and Fourth Schedule Amendment) Order 2017. Repeals and replaces the Third and Fourth Schedule of the Pharmacy and Poisons Act 1979 2 The Third and Fourth Schedules to the Pharmacy and Poisons Act 1979 are repealed and replaced with— “THIRD SCHEDULE (Sections 25(6); 27(1))) DRUGS OBTAINABLE ONLY ON PRESCRIPTION EXCEPT WHERE SPECIFIED IN THE FOURTH SCHEDULE (PART I AND PART II) Note: The following annotations used in this Schedule have the following meanings: md (maximum dose) i.e. the maximum quantity of the substance contained in the amount of a medicinal product which is recommended to be taken or administered at any one time. 1 PHARMACY AND POISONS (THIRD AND FOURTH SCHEDULE AMENDMENT) ORDER 2017 mdd (maximum daily dose) i.e. the maximum quantity of the substance that is contained in the amount of a medicinal product which is recommended to be taken or administered in any period of 24 hours. mg milligram ms (maximum strength) i.e. either or, if so specified, both of the following: (a) the maximum quantity of the substance by weight or volume that is contained in the dosage unit of a medicinal product; or (b) the maximum percentage of the substance contained in a medicinal product calculated in terms of w/w, w/v, v/w, or v/v, as appropriate.
    [Show full text]
  • Alkaloids Pp. 178-End.Pdf
    Hydrastine Found in the roots and rhizomes of Hydrastis canadensis (family: Ranunculaceae). Uses: To control uterine hemorrhage. Traditional use of this root as: 1. Tonic {a medicine that strengthens). Abusamra Yousef Dr. 2. Uterine hemorrhage. 3. Catarrhal conditions. 178 Berberine: Berberies species) and)البرباريسية From Berberidaceae . .(Hydrastis)الفصيلة ال َح ْوذانية Ranunculaceae . Used as antiemetic, antibacterial and anti-inflammatory. Also, it is used for liver diseases. Sanguinarine: blood) دموية From the roots of Sanguinaria canadensis . Dr. Yousef Abusamra Yousef Dr. root) {Family Papaveraceae}. Native to America. Its effect resembles colchicine, i.e. causes doubling of chromosomes number (polyploidy). 179 . Used for atonic dyspepsia with hepatic symptoms. عسر الهضم Jatrorrhizine A protoberberine Benefits: alkaloid Antifungal, antibacterial, Antidiabetic, antiinflammatory. Dr. Yousef Abusamra Yousef Dr. Berberine 180 A quaternary amine alkaloid. Hydrastine Curare alkaloids: Bis-benzylisoquinoline. obtained from the bark and stems of Chondrodendrum tomentosum (family: Menispermaceae). The name is derived from “urari”; an Indian word indicating “poison”. The term “curare” is used to indicate the crude extract prepared from different species. Abusamra Yousef Dr. Was used by certain natives of the Amazon regions of South America as arrow poison. Some of these extracts were poisonous by virtue of a convulsant action and 181 others by paralyzing action (Most remarkable). Mechanism of action of d-tubocurarine Dr. Yousef Abusamra Yousef Dr. 182 • Curare possesses: 1. A paralyzing effect on voluntary muscles. 2. A toxic effect on blood vessels. 3. A histamine–like effect. Most of the activity is attributed to d-tubocurarine. Uses: 1- In surgical anesthesia, as it produces muscular relaxation without deep anesthesia.
    [Show full text]
  • Veterinary Anaesthesia (Tenth Edition)
    W. B. Saunders An imprint of Harcourt Publishers Limited © Harcourt Publishers Limited 2001 is a registered trademark of Harcourt Publishers Limited The right of L.W. Hall, K.W. Clarke and C.M. Trim to be identified as the authors of this work have been asserted by them in accordance with the Copyright, Designs and Patents Act, 1988. All rights reserved. No part of this publication may be reproduced, stored in a retrieval system, or transmitted in any form or by any means, electronic, mechanical, photocopying, recording or otherwise, without either the prior permission of the publishers (Harcourt Publishers Limited, Harcourt Place, 32 Jamestown Road, London NW1 7BY), or a licence permitting restricted copying in the United Kingdom issued by the Copyright Licensing Agency Limited, 90 Tottenham Court Road, London W1P 0LP. First edition published in 1941 by J.G. Wright Second edition 1947 (J.G. Wright) Third edition 1948 (J.G. Wright) Fourth edition 1957 (J.G. Wright) Fifth edition 1961 (J.G. Wright and L.W. Hall) Sixth edition 1966 (L.W. Hall) Seventh edition 1971 (L.W. Hall), reprinted 1974 and 1976 Eighth edition 1983 (L.W. Hall and K.W. Clarke), reprinted 1985 and 1989 Ninth edition 1991 (L.W. Hall and K.W. Clarke) ISBN 0 7020 2035 4 Cataloguing in Publication Data: Catalogue records for this book are available from the British Library and the US Library of Congress. Note: Medical knowledge is constantly changing. As new information becomes available, changes in treatment, procedures, equipment and the use of drugs become necessary. The authors and the publishers have taken care to ensure that the information given in this text is accurate and up to date.
    [Show full text]
  • Modes of Action of Herbal Medicines and Plant Secondary Metabolites
    Medicines 2015, 2, 251-286; doi:10.3390/medicines2030251 OPEN ACCESS medicines ISSN 2305-6320 www.mdpi.com/journal/medicines Review Modes of Action of Herbal Medicines and Plant Secondary Metabolites Michael Wink Institute of Pharmacy and Molecular Biotechnology, Heidelberg University, INF 364, Heidelberg D-69120, Germany; E-Mail: [email protected]; Tel.: +49-6221-544-881; Fax: +49-6221-544-884 Academic Editor: Shufeng Zhou Received: 13 August 2015 / Accepted: 31 August 2015 / Published: 8 September 2015 Abstract: Plants produce a wide diversity of secondary metabolites (SM) which serve them as defense compounds against herbivores, and other plants and microbes, but also as signal compounds. In general, SM exhibit a wide array of biological and pharmacological properties. Because of this, some plants or products isolated from them have been and are still used to treat infections, health disorders or diseases. This review provides evidence that many SM have a broad spectrum of bioactivities. They often interact with the main targets in cells, such as proteins, biomembranes or nucleic acids. Whereas some SM appear to have been optimized on a few molecular targets, such as alkaloids on receptors of neurotransmitters, others (such as phenolics and terpenoids) are less specific and attack a multitude of proteins by building hydrogen, hydrophobic and ionic bonds, thus modulating their 3D structures and in consequence their bioactivities. The main modes of action are described for the major groups of common plant secondary metabolites. The multitarget activities of many SM can explain the medical application of complex extracts from medicinal plants for more health disorders which involve several targets.
    [Show full text]
  • EUROPEAN PHARMACOPOEIA 10.0 Index 1. General Notices
    EUROPEAN PHARMACOPOEIA 10.0 Index 1. General notices......................................................................... 3 2.2.66. Detection and measurement of radioactivity........... 119 2.1. Apparatus ............................................................................. 15 2.2.7. Optical rotation................................................................ 26 2.1.1. Droppers ........................................................................... 15 2.2.8. Viscosity ............................................................................ 27 2.1.2. Comparative table of porosity of sintered-glass filters.. 15 2.2.9. Capillary viscometer method ......................................... 27 2.1.3. Ultraviolet ray lamps for analytical purposes............... 15 2.3. Identification...................................................................... 129 2.1.4. Sieves ................................................................................. 16 2.3.1. Identification reactions of ions and functional 2.1.5. Tubes for comparative tests ............................................ 17 groups ...................................................................................... 129 2.1.6. Gas detector tubes............................................................ 17 2.3.2. Identification of fatty oils by thin-layer 2.2. Physical and physico-chemical methods.......................... 21 chromatography...................................................................... 132 2.2.1. Clarity and degree of opalescence of
    [Show full text]
  • PDF Hosted at the Radboud Repository of the Radboud University Nijmegen
    View metadata, citation and similar papers at core.ac.uk brought to you by CORE provided by Radboud Repository PDF hosted at the Radboud Repository of the Radboud University Nijmegen The following full text is a publisher's version. For additional information about this publication click this link. http://hdl.handle.net/2066/24502 Please be advised that this information was generated on 2017-12-05 and may be subject to change. Neuromuscular transmission and its pharmacological blockade Part 1: Neuromuscular transmission and general aspects of its blockade • Leo H. D. J. Boolj 1.1 .Introduction Muscle relaxation is an important tool in the treat­ ment of patients during anaesthesia for surgical and diagnostics procedures, and during treatment in the intensive care unit. Such muscle relaxation is obtained by pharmacological intervention with neuromuscular transmission with either depolarizing or non-depolar- izing relaxants. Suxamethonium presently is the only depolarizer in clinical use, but has many adverse effects. A large number of non-depolarizing relaxants has been introduced into clinical practice; however, none of them matches perfectly with the 'ideal mus­ cle relaxant7. This demands the development of new compounds. Some of the new development in neuro­ muscular transmission and its blockers are discussed. 1.2.Neuromuscular transmission For normal muscular functions an impulse must be transferred from the nerve terminal to the muscle. Such a transfer takes place at the neuromuscular junc­ tion, which consist of the nerve terminal, a 50-100 nm wide junctional cleft, and the postjunctional mus­ cle membrane [1], Booij LHDJ. Neuromuscular transmission and its pharmacologi - In research on the neuromuscular junction it has cal blockade.
    [Show full text]
  • Federal Register / Vol. 60, No. 80 / Wednesday, April 26, 1995 / Notices DIX to the HTSUS—Continued
    20558 Federal Register / Vol. 60, No. 80 / Wednesday, April 26, 1995 / Notices DEPARMENT OF THE TREASURY Services, U.S. Customs Service, 1301 TABLE 1.ÐPHARMACEUTICAL APPEN- Constitution Avenue NW, Washington, DIX TO THE HTSUSÐContinued Customs Service D.C. 20229 at (202) 927±1060. CAS No. Pharmaceutical [T.D. 95±33] Dated: April 14, 1995. 52±78±8 ..................... NORETHANDROLONE. A. W. Tennant, 52±86±8 ..................... HALOPERIDOL. Pharmaceutical Tables 1 and 3 of the Director, Office of Laboratories and Scientific 52±88±0 ..................... ATROPINE METHONITRATE. HTSUS 52±90±4 ..................... CYSTEINE. Services. 53±03±2 ..................... PREDNISONE. 53±06±5 ..................... CORTISONE. AGENCY: Customs Service, Department TABLE 1.ÐPHARMACEUTICAL 53±10±1 ..................... HYDROXYDIONE SODIUM SUCCI- of the Treasury. NATE. APPENDIX TO THE HTSUS 53±16±7 ..................... ESTRONE. ACTION: Listing of the products found in 53±18±9 ..................... BIETASERPINE. Table 1 and Table 3 of the CAS No. Pharmaceutical 53±19±0 ..................... MITOTANE. 53±31±6 ..................... MEDIBAZINE. Pharmaceutical Appendix to the N/A ............................. ACTAGARDIN. 53±33±8 ..................... PARAMETHASONE. Harmonized Tariff Schedule of the N/A ............................. ARDACIN. 53±34±9 ..................... FLUPREDNISOLONE. N/A ............................. BICIROMAB. 53±39±4 ..................... OXANDROLONE. United States of America in Chemical N/A ............................. CELUCLORAL. 53±43±0
    [Show full text]
  • Jämförelse Av Olika Övervakningstekniker För Monitorering Av Neuromuskulär Blockad Vid Ögonkirurgi Applicerbarhet Av Elektromyograf Tetragraph (Senzime) På Hund
    Fakulteten för veterinärmedicin och husdjursvetenskap Jämförelse av olika övervakningstekniker för monitorering av neuromuskulär blockad vid ögonkirurgi Applicerbarhet av elektromyograf TetraGraph (Senzime) på hund A comparative study of different techniques for monitoring of neuromuscular blockade during ophthalmology surgery Application of electromyograph TetraGraph (Senzime) in dogs Jonathan Sverud Uppsala 2020 Examensarbete 30 hp inom Veterinärprogrammet Jämförelse av olika övervakningstekniker för monitorering av neuromuskulär blockad vid ögonkirurgi Applicerbarhet av elektromyograf TetraGraph (Senzime) på hund A comparative study of different techniques for monitoring of neuromuscular blockade during ophthalmology surgery Application of electromyograph TetraGraph (Senzime) in dogs Jonathan Sverud Handledare: Görel Nyman, institutionen för kliniska vetenskaper Biträdande handledare: Lena Ström & Desiree Ferrari, institutionen för kliniska vetenskaper Examinator: Patricia Hedenqvist, institutionen för kliniska vetenskaper Examensarbete i veterinärmedicin Omfattning: 30 hp Nivå och fördjupning: Avancerad nivå, A2E Kurskod: EX0869 Kursansvarig institution: Institutionen för kliniska vetenskaper Utgivningsort: Uppsala Utgivningsår: 2020 Elektronisk publicering: https://stud.epsilon.slu.se Omslagsillustration: fotografiet taget av Desiree Ferrari Nyckelord: anestesi, övervakning, neuromuskulär blockad, acceleromyografi, elektromyografi, mekanomyografi, hund Key words: anaesthesia, monitor, neuromuscular blockade, acceleromyogaphy, electromyography,
    [Show full text]
  • Toxicology Information 2018-08-08
    Centre of Forensic Sciences Toxicology Section Centre of Forensic Sciences Investigators and Submitters Technical Information Sheets Toxicology Information Introduction The Toxicology Section performs analyses on biological samples (e.g., blood, urine, liver) to determine the absence/presence/concentration(s) of drugs, including alcohol and poisons. This document is intended as a convenient investigative reference but should not be relied upon as definitive or exhaustive. Please contact the Centre of Forensic Sciences (CFS) Toxicology Section for assistance with questions of an analytical or toxicological nature by e-mail or telephone 647 329-1400 or 647 329-1430. When calling please ask for the appropriate coordinator: Coroner’s Coordinator: [email protected] Criminal Coordinator: [email protected] Analytical Decision-making and Capability The screening methods employed in the Toxicology Section are: 1. Gas Chromatography (GC) and Gas Chromatography/Mass Spectrometry (GC/MS) 2. Immunoassay (IA) 3. Head-Space GC analysis for volatiles 4. Quadrupole Time-of-Flight MS (QTOF) The targeted/quantitation methods employed in the Toxicology Section are: 1. GC, GC/MS 2. Liquid Chromatography (LC), LC-MS/MS 3. Head-Space GC analysis for volatiles The capability of the screening methods is presented in Appendix 1. While these screening methods have wide-ranging capabilities not all drugs may be reliably detected. Appendix 2 contains a list of compounds that may not be identified by the screening methods but may be detected/quantitated by targeted methods. Many of the compounds contained in this list will not be tested for unless specifically requested. If use of a specific drug is known or suspected it should be noted in the case synopsis.
    [Show full text]
  • Stembook 2018.Pdf
    The use of stems in the selection of International Nonproprietary Names (INN) for pharmaceutical substances FORMER DOCUMENT NUMBER: WHO/PHARM S/NOM 15 WHO/EMP/RHT/TSN/2018.1 © World Health Organization 2018 Some rights reserved. This work is available under the Creative Commons Attribution-NonCommercial-ShareAlike 3.0 IGO licence (CC BY-NC-SA 3.0 IGO; https://creativecommons.org/licenses/by-nc-sa/3.0/igo). Under the terms of this licence, you may copy, redistribute and adapt the work for non-commercial purposes, provided the work is appropriately cited, as indicated below. In any use of this work, there should be no suggestion that WHO endorses any specific organization, products or services. The use of the WHO logo is not permitted. If you adapt the work, then you must license your work under the same or equivalent Creative Commons licence. If you create a translation of this work, you should add the following disclaimer along with the suggested citation: “This translation was not created by the World Health Organization (WHO). WHO is not responsible for the content or accuracy of this translation. The original English edition shall be the binding and authentic edition”. Any mediation relating to disputes arising under the licence shall be conducted in accordance with the mediation rules of the World Intellectual Property Organization. Suggested citation. The use of stems in the selection of International Nonproprietary Names (INN) for pharmaceutical substances. Geneva: World Health Organization; 2018 (WHO/EMP/RHT/TSN/2018.1). Licence: CC BY-NC-SA 3.0 IGO. Cataloguing-in-Publication (CIP) data.
    [Show full text]
  • Botulinum Toxin
    Botulinum toxin From Wikipedia, the free encyclopedia Jump to: navigation, search Botulinum toxin Clinical data Pregnancy ? cat. Legal status Rx-Only (US) Routes IM (approved),SC, intradermal, into glands Identifiers CAS number 93384-43-1 = ATC code M03AX01 PubChem CID 5485225 DrugBank DB00042 Chemical data Formula C6760H10447N1743O2010S32 Mol. mass 149.322,3223 kDa (what is this?) (verify) Bontoxilysin Identifiers EC number 3.4.24.69 Databases IntEnz IntEnz view BRENDA BRENDA entry ExPASy NiceZyme view KEGG KEGG entry MetaCyc metabolic pathway PRIAM profile PDB structures RCSB PDB PDBe PDBsum Gene Ontology AmiGO / EGO [show]Search Botulinum toxin is a protein and neurotoxin produced by the bacterium Clostridium botulinum. Botulinum toxin can cause botulism, a serious and life-threatening illness in humans and animals.[1][2] When introduced intravenously in monkeys, type A (Botox Cosmetic) of the toxin [citation exhibits an LD50 of 40–56 ng, type C1 around 32 ng, type D 3200 ng, and type E 88 ng needed]; these are some of the most potent neurotoxins known.[3] Popularly known by one of its trade names, Botox, it is used for various cosmetic and medical procedures. Botulinum can be absorbed from eyes, mucous membranes, respiratory tract or non-intact skin.[4] Contents [show] [edit] History Justinus Kerner described botulinum toxin as a "sausage poison" and "fatty poison",[5] because the bacterium that produces the toxin often caused poisoning by growing in improperly handled or prepared meat products. It was Kerner, a physician, who first conceived a possible therapeutic use of botulinum toxin and coined the name botulism (from Latin botulus meaning "sausage").
    [Show full text]
  • Chapter 13 – Pharmacology of Muscle Relaxants and Their Antagonists Mohamed Naguib, Cynthia A
    Chapter 13 – Pharmacology of Muscle Relaxants and Their Antagonists Mohamed Naguib, Cynthia A. Lien HISTORY AND CLINICAL USE In 1942 Griffith and Johnson[1] suggested that d-tubocurarine (dTc) is a safe drug to use during surgery to provide skeletal muscle relaxation. One year later, Cullen[2] described its use in 131 patients who had received general anesthesia for their surgery. In 1954, Beecher and Todd[3] reported a sixfold increase in mortality in patients receiving dTc versus those who had not received a relaxant. The increased mortality was due to a general lack of understanding of the pharmacology of neuromuscular blockers and their antagonism. The impact of residual neuromuscular blockade postoperatively was not appreciated, guidelines for monitoring muscle strength had not been established, and the importance of pharmacologically antagonizing residual blockade was not understood. Since then, the understanding of neuromuscular blocker pharmacology has improved, and relaxants have become an important component of many anesthetics and have facilitated the growth of surgery into new areas with the use of innovative techniques.[4] Succinylcholine, introduced by Thesleff[5] and by Foldes and colleagues in 1952,[4] changed anesthetic practice drastically. Its rapid onset of effect and ultrashort duration of action allowed for rapid tracheal intubation. In 1967, Baird and Reid first reported on clinical administration of the synthetic aminosteroid pancuronium.[6] Though similar to dTc, in terms of its duration of action, this compound had an improved cardiovascular side effect profile. It lacked ganglionic-blocking and histamine-releasing properties and was mildly vagolytic. The resulting increases in heart rate and blood pressure were considered significant improvements over its predecessors.
    [Show full text]