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INTRODUCTION

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Chapter 6 Cholinergic Pharmacology is a combination of Chapter 9 Muscarinic Receptor Agonists and Antagonists Chapter 10 Anticholinesterase Agents, and Chapter 11 Agents Acting at the Neuromuscular Junction and Autonomic Ganglia in Goodman and Gilman’s The Pharmacological Basis of Therapeutics, 12th Edition. An understanding of the material in these chapters will be helpful in following the material presented in this chapter. In addition to the material presented here the above chapters in the 12th Edition include:

  • A complete discussion of the properties and subtypes of muscarinic receptors

  • The pharmacological effects of acetylcholine (ACh)

  • A detailed discussion of the pharmacological effects of atropine, a muscarinic receptor antagonist

  • A discussion of the toxicology of drugs with antimuscarinic properties

  • A review of the structure of acetylcholinesterase (AChE)

  • A discussion of the mechanism of AChE

  • A description of the nicotinic acetylcholine receptor

  • A description of the actions of neuromuscular blocking agents on various organ systems

  • A discussion of the pathophysiology and treatment of malignant hyperthermia

  • A discussion of ganglionic transmission

  • A description of the pharmacological actions of nicotine

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LEARNING OBJECTIVES

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  • Understand cholinergic pharmacology, including the different types and subtypes of cholinergic receptors expressed in the central nervous system (CNS), autonomic nervous system (ANS), and neuromuscular junction.

  • Know the mechanisms of synthesis, storage, release, and destruction of ACh in the CNS, parasympathetic and sympathetic ganglia, parasympathetic nerve fibers, and the neuromuscular junction.

  • Know the uses and toxicities of muscarinic receptor agonists and antagonists.

  • Know the uses and toxicities of drugs and agents that inhibit AChE.

  • Describe the uses and toxicities of drugs that block neuromuscular transmission.

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DRUGS (OR AGENTS) INCLUDED IN THIS CHAPTER

  • Acetylcholine (MIOCHOL-E)

  • Aldicarb (TEMIK)—Insecticide

  • Ambenonium chloride (MYTELASE)

  • Atracurium (TACRIUM, others)

  • Atropine

  • Benztropine mesylate (COGENTIN, others); see Chapter 13

  • Bethanechol (URECHOLINE)

  • Carbachol (MIOSTAT, ISOPTOCARBACHOL)

  • Carbaryl (SEVIN)—Insecticide

  • Cevimeline (EVOXAC)

  • Chlorpyrifos (DURSBAN, LORSBAN)—Insecticide

  • Cisatracurium (NIMBEX)

  • Cyclopentolate hydrochloride (CYCLOGYL, others)

  • Dantrolene (DANTRIUM, others)

  • Darifenacin (ENABLEX)

  • Diazinon (SPECTRICIDE, others)—Insecticide

  • Dicyclomine hydrochloride (BENTYL, others)

  • Donepezil (ARICEPT)

  • Doxacurium

  • Edrophonium

  • Fesoterodine (TOVIAZ)

  • Flavoxate (Urispas)

  • Galantamine (REMINYL)

  • Glycopyrrolate (ROBINUL, others)

  • Homatropine hydrobromide (ISOPTO HOMATROPRINE)

  • Ipratropium (ATROVENT, others)

  • Malathion (CHEMATHION, MALA-SPRAY)—Insecticide

  • Mecamylamine (INVERSINE)

  • Methacholine (PROVOCHOLINE)

  • Methscopolamine bromide (PAMINE)

  • Mivacurium (Not available in the United States)

  • Neostigmine bromide (PROSTIGMIN-oral)

  • Neostigmine methylsulfate (PROSTIGMIN-parenteral)

  • Nicotine gum or lozenge (NICOTINE POLACRILEX, NICORETTE, COMMIT, THRIVE, others)

  • Nicotine nasal spray or vapor inhaler (NICOTROL)

  • Nicotine transdermal patch (HABITROL, others)

  • Onabotulinum toxin A (BOTOX)

  • Oxybutynin (DITROPAN, others; OXYTROL-transdermal; GELNIQUE-gel)

  • Pancuronium

  • Physostigmine salicylate (ANTILIRIUM)

  • Pilocarpine (ISOPTO CARPINE)

  • Pilocarpine hydrochloride (SALAGEN, others)

  • Pipecuronium

  • Pralidoxime (2-PAM; PROTOPAM CHLORIDE)

  • Propoxur (BAYGON)—Insecticide

  • Pyridostigmine bromide (MESTINON-oral; REGINOL, MESTINON-parenteral)

  • Rimabotulinum toxin B (MYOBLOC)

  • Rivastigmine (EXELON)

  • Rocuronium (ZEMURON, others)

  • Sarin—Nerve gas

  • Scopolamine (TRANSDERM SCOP)

  • Solifenacin (VESICARE)

  • Soman—Nerve gas

  • Succinylcholine (ANECTINE, QUELICIN)

  • Tabun—Nerve gas

  • Tacrine (COGNEX)

  • Tiotropium (SPIRIVA)

  • Tolterodine (DETROL)

  • Trihexyphenidyl hydrochloride (ARTANE, others); see Chapter 13

  • Trimethaphan

  • Tropicamide (MYDRIACYL, others)

  • Trospium chloride (SANCTURA)

  • Varenicline (CHANTIX)

  • Vecuronium (NORCURON, others)

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Table Graphic Jump Location
MECHANISM OF ACTION MUSCARINIC AGONISTS AND ANTAGONISTS

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