Pharmacology of Antimuscarinic Agents
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Summary
The theoretical and practical significance of antimuscarinic drugs is more obvious today than ever before. Antimuscarinics have helped to explore the pathomechanisms of of Alzheimer's disease, and to treat the symptoms of Parkinson's, cardiovascular problems, gastrointestinal diseases, and even nerve gas poisoning. No other drug class can claim as long a history with so many therapeutic applications, yet the most significant developments in this broad chapter of pharmacology come from the discovery of different muscarinic receptor sites in the peripheral and central nervous system and from the availability of many new selective agents, notably antagonists, for these different receptor types.
Pharmacology of Antimuscarinic Agents, written by an expert in anesthesiology and drug research, focuses on the basic principles of antimuscarinic drugs, their therapeutic value, how they work, and what versions are now available in the U.S. and abroad. This is the first time in decades an author has reviewed historical and current literature to present a comprehensive, standard reference on the antimuscarinic family.
Table of Contents
Introduction
History
Nomenclature
Mechanism and Site of Action of Antimuscarinic Agents
Description and Classification of Acetylcholinergic Receptor Sites
The Role of ACh in Neuronal Conduction
Chemical Structural Aspects Related to Stimulation and Block of the ACh Receptors
The Tropane Alkaloids
Chemistry
Absorption, Distribution, Metabolism, and Elimination of Atropine and Related Tropane Alkaloids (Animal and Human Data)
Animal Pharmacology of Atropine
Resistance to Atropine
Hyosciamine
L (-) Hyoscine (Scopolamine) - Introduction
Atropine and L (-) Hyoscine as Pharmacologic Probes in the Pharmacologic Exploration of the CNS
Semisynthetic Derivatives of Tropane Alkaloids and Other Tropine Esters
N-Methylquaternary Derivatives of Tropane Alkaloids - Introduction
Other Tropeines
Synthetic Antimuscarinic Agents
Antimuscarinic Tropane Derivatives
Other Bicyclic and Polycyclic Amines
4-Acyloxy 2,6-Disubstituted Piperidines
Aliphatic and Alicyclic Aminoalcohol Esters of Aromatics Acids
1,3-Dioxolane Derivatives
Amino Alkanols and Amino Alkanes Substituted with Aromatic Groups
Aromatic Acid Amide and Nitrile Derivatives of Alkyl Amines
Aromatic Ether Derivatives of Amino Alkanols
Other Compounds of Various Chemical Structures with Antimuscarinic Properties
Synthetic Agents with Central Acetylcholinolytic Properties Used in Parkinson's Disease
Molecular Design of Antimuscarinic Agents
Muscarinic Receptor Subtype-Nonspecific Agents
Muscarinic Receptor Subtype-Specific Agents
Drug Interactions
Clinical Pharmacology and Therapeutic Uses of Antimuscarinic Agents
Pharmacokinetics
Effects on the Cardiovascular System in Man
Effects on Respiration
Effects on the Motor Functions of the Gastrointestinal and Genitourinary Tract
Action on Secretory Functions
Effects on the Eye
Effects of Antimuscarinics in the CNS
Clinical Studies with Other Antimuscarinic Agents and their Therapeutic Uses
Use of Antimuscarinic Agents as Adjuncts to Anesthesia
Use in Anticholinesterase Poisoning
Emesis and Motion Sickness
Use in Cerebral Injuries
Toxicity of Atropine
Toxicity in Animals
Toxicity in Man
Summary
References
Index
