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Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Chapter 16 Drugs That Block Nicotinic Cholinergic Transmission: Neuromuscular Blocking Agents and Ganglionic Blocking Agents
2Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Neuromuscular Blockers Prevent acetylcholine from activating nicotinic M Cause muscle relaxation (paralysis) No oral forms Cannot cross Blood-brain barrier No impact on CNS (paralysis, not sedation) No impact on CNS (paralysis, not sedation) Placenta Minimal effects on fetus Minimal effects on fetus
3Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Control of Muscle Contractions Basic concepts (see Fig. 16-1) Polarization Depolarization Repolarization Steps in muscle contraction (see Fig. 16-2)
4Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Classification of Neuromuscular Blocking Agents Competitive neuromuscular blockers I: tubocurarine (no longer used) Competitive neuromuscular blockers II: others Depolarizing neuromuscular blockers: succinylcholine
5Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Fig The depolarization-repolarization cycle of the motor end-plate and muscle membrane. (ACh = acetylcholine.)
6Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Fig Steps in excitation-contraction coupling. (ACh = acetylcholine.)
7Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Competitive Neuromuscular Blockers I: Tubocurarine Oldest competitive neuromuscular blocker (NMB) No longer used in United States Replaced by newer NMBs One of active principles found in curare, a poison used by primitive arrow hunters
8Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Competitive Neuromuscular Blockers Chemistry Quaternary nitrogen atom Mechanism of action Competes with ACh for nicotinic M receptors Pharmacologic effects Muscle relaxation: flaccid paralysis Hypotension Central nervous system
9Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Competitive Neuromuscular Blockers Pharmacokinetics Rapid onset of paralysis Adverse effects Respiratory arrest Cardiovascular effects
10Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Competitive Neuromuscular Blockers I: Tubocurarine Precautions and contraindications Myasthenia gravis Electrolyte disturbances Drug interactions General anesthetics Antibiotics Cholinesterase inhibitors
11Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Competitive Neuromuscular Blockers I: Tubocurarine Toxicology Overdose Prolonged apnea, massive histamine release, and cardiovascular collapse Prolonged apnea, massive histamine release, and cardiovascular collapse Preparations, dosage, and administration No longer used in the United States
12Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Competitive Neuromuscular Blockers II: Others Long-acting agents Doxacurium Metocurine Pipecuronium Intermediate- acting agents Cisatracurium Pancuronium Rocuronium Vecuronium Short-acting agents Mivacurium
13Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Fig Structural formulas of representative neuromuscular blocking agents. Note that all of these agents contain quaternary nitrogen atoms and therefore cross membranes poorly. Consequently, they must be administered parenterally and have little effect on the central nervous system or a developing fetus.
14Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Fig Mechanism of competitive neuromuscular blockade. Tubocurarine competes with acetylcholine (ACh) for binding to nicotinic M receptors on the motor end-plate. Binding of tubocurarine does not depolarize the end-plate and therefore does not cause contraction. At the same time, the presence of tubocurarine prevents ACh from binding to the receptor, hence contraction is prevented.
15Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Depolarizing Neuromuscular Blockers: Succinylcholine Mechanism of action Pharmacologic effects Ultrashort-acting (peak 1 min, fades 4–10 min) (peak 1 min, fades 4–10 min) Muscle relaxation Central nervous system Pharmacokinetics Eliminated by plasma cholinesterases Therapeutic uses Muscle relaxation during intubation
16Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Depolarizing Neuromuscular Blockers: Succinylcholine Adverse effects Prolonged apnea in patients with low pseudocholinesterase activity Malignant hyperthermia Postoperative muscle pain Hyperkalemia
17Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Depolarizing Neuromuscular Blockers: Succinylcholine Drug interactions Cholinesterase inhibitors Antibiotics Toxicology Preparations, dosage, and administration
18Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Therapeutic Uses of Neuromuscular Blockers Muscle relaxation during surgery Facilitation of mechanical ventilation Adjunct to electroconvulsive therapy Endotracheal intubation Diagnosis of myasthenia gravis
19Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Ganglionic Blocking Agents Mechanism of action Pharmacologic effects Pharmacokinetics Therapeutic use Adverse effects Antimuscarinic effects Antimuscarinic effects Orthostatic hypotension Orthostatic hypotension CNS effects CNS effects Preparations, dosage, and administration
Skeletal muscle relaxants Prof. Hanan Hagar. Skeletal muscle relaxants Are drugs used to induce muscle relaxation Classification Peripherally acting.
Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Chapter 15 Cholinesterase Inhibitors and Their Use in Myasthenia Gravis.
Skeletal muscle relaxants Prof. Hanan Hagar. Learning objectives By the end of this lecture, students should be able to: - Identify classification of.
Skeletal muscle relaxants Classification Peripherally acting (Neuromuscular blockers). Centrally acting skeletal muscle relaxants e.g. Baclofen - Diazepam.
1 Copyright © The McGraw-Hill Companies, Inc. Permission required for reproduction or display. CHAPTER 9 Skeletal Muscle Relaxants.
NEUROMUSCULAR JUNCTION BLOCKERS BY :DR ISRAA OMAR.
NEUROMUSCULAR BLOCKERS and CENTRAL MUSCLE RELAXANTS DR.ABDUL LATIF MAHESAR PHARMACOLOGY Dr.Alia Al-Shanawani December 17,2011 References: Basic and clinical.
Mosby items and derived items © 2008, 2002 by Mosby, Inc., an affiliate of Elsevier Inc. Chapter 18 Skeletal Muscle Relaxants (Neuromuscular Blocking Agents)
Autonomic Nervous System 6-Anticholinergic Drugs أ0م0د.وحدة بشير اليوزبكي.
The Neuromuscular Junction. The Neuromuscular Junction: a Specialized form of synaptic transmission: communication between neurons and muscle.
Skeletal Muscle Relaxants Dept. of Pharmacology Faculty of Medicine & Health Sciences AIMST.
Neuromuscular Blocking Agents Dr. Ahmed Haki Ismael.
Pharmacology DOR 101 Abdelkader Ashour, Ph.D. 5 th Lecture.
Skeletal Muscle Relaxants Dr Naser Ashraf. Types of skeletal muscle relaxants: 2 groups Neuromuscular blockers Relax normal muscles (surgery and assistance.
1 Cholinergic Receptors Antagonists Section 2, lecture 3.
11/22/20151 SKELETAL MUSCLE RELAXANTS. 211/22/2015 Classification on basis of site of action and mechanism of action A)PERIPHERALLY ACTING Neuromuscular.
Pharmacology-1 PHL 211 Twelfth Lecture By Abdelkader Ashour, Ph.D. Phone:
1 Copyright © 2010, Elsevier Inc. All rights Reserved Fig 2.1 Chapter 2.
Michael H. Ossipov, Ph.D. Department of Pharmacology Neuromuscular Blocking Drugs.
Neuromuscular Blockers Bernie Miller, MD Medical Student Lecture Series.
8/19/20151 SKELETAL MUSCLE RELAXANTS Dr. Abdul Latif Mahesar King Saud University.
Skeletal Muscle Relaxants Dr. Alia Shatanawi
Dr: Samah Gaafar Al-shaygi بسم الله الرحمن الرحيم.
1 Copyright © 2010, Elsevier Inc. All rights Reserved Fig 3.1 Chapter 3.
1 Chapter 40 - Physiology and Pathophysiology of Diuretic Action Copyright © 2013 Elsevier Inc. All rights reserved.
Pharmacology-1 PHL 313 Parasympathetic Nervous System Fifth Lecture By Abdelkader Ashour, Ph.D. Phone:
Antinicotinics 1. Classification of Antinicotinics Antinicotinics Neuromuscular Junction blockers (NMJ) Ganglionic blockers 2.
Muscle Relaxants are classified as: I)Peripherally acting A.Neuromuscular blocking agents :- 1) Depolarizing muscle relaxants. 2) Non-depolarizing muscle.
ANTICHOLINESTERASES Acetylcholinesterase is an enzyme that specifically cleaves acetylcholine to acetate and choline. It is located both pre-and post-synaptically.
Cholinergic antagonists. Anti- muscarinic agents sites of action 1. Secretions by salivary, bronchial and sweat glands. 2. The eye and cardiac responses.
Chapter 13 Drugs Affecting Muscle Function Copyright © 2011 Delmar, Cengage Learning.
© 2004 by Thomson Delmar Learning, a part of the Thomson Corporation. Fundamentals of Pharmacology for Veterinary Technicians Chapter 13 Drugs Affecting.
Skeletal Muscle Relaxants By S. Bohlooli, PhD. Drugs affecting skeletal muscle function Neuromuscular blockers Used during surgical procedures and ICU.
Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Chapter 34 Sedative-Hypnotic Drugs.
Cholinergic agonists & Cholinergic antagonists Adrenergic agonists & Adrenergic antagonists.
SHANNON KEHR PHYSIOLOGY APRIL 1, 2014 Muscle Relaxers.
Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Chapter 26 Local Anesthetics.
Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Chapter 18 Adrenergic Antagonists.
Parasympathlytic (Cholinergic antagonists) (Anticholinergic ) (Cholinergic Blockers) (Cholinergic Blockers)
Drugs affecting neuromuscular transmission Professor Ian Hughes, 9.83; motor nerve - skeletal (striated) muscle ONLY single long.
Mosby items and derived items © 2007, 2005, 2002 by Mosby, Inc., an affiliate of Elsevier Inc. CHAPTER 11 General and Local Anesthetics.
Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Chapter 19 Indirect-Acting Antiadrenergic Agents.
Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Chapter 14 Muscarinic Agonists and Antagonists.
INDIRECT CHOLINOMIMETICS Prof. Hanan Hagar Pharmacology Department.
Addition 1’s to
Pharmacologic Adjuncts to Airway Management and Ventilation EMS 352 DR AQEELA BANO.
Agents Used to Treat Musculoskeletal Health Alterations.
What students should know: Classification of indirect acting cholinomimetics Mechanism of action, kinetics, dynamics and uses of anticholinesterases.
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