Medicinal Chemistry, 2nd Edition

Chapter 23

Cholinergic Drugs

LEARNING OBJECTIVES

• Define acetyl choline and cholinergic receptors

• Describe the actions and uses of cholinomimetics

• Describe the structural requirements for cholinergic agonist

• Define acetylcholinesterase and the utility of inhibitors

• Define antimuscarinics and classify based on structure

• Compare the tertiary and quarternary amines as antimuscarinics

• List the newer drugs in the class of cholinergic agents

23.1 INTRODUCTION

Cholinergic nerves (parasympathetic nerves) are found in the peripheral and the central nervous system of humans. Cholinergic neurons synthesise, store, and release acetylcholine (ACh). Acetylcholine is prepared at the nerve ending by the transfer of an acetyl group from acetyl-CoA to choline. ...