Shivansh Pande Clinical Pharmacist Apollo Hospitals, Jubilee Hills, Hyderabad

Cholinergic Drugs
Cholinergic drugs or parasympathomimetic drugs are

agents which activate the actions of the cholinergic/parasympathetic system.

Acetylcholine Acetylcholine is the neurotransmitter of the

cholinergic system. It is synthesized locally in the cholinergic nerve endings.

Acetyl CoEn-A+Choline>Acetylcholine>(cholinesterase)>Choline+Acetate

Cholinergic Receptors
There are 2 types of cholinergic receptors:
Muscarinic: G-protein coupled receptor Stimulated by muscarine and blocked by atropine Three subtypes:M1, M2, M3 Nicotinic: Ligand gated ion channel receptor Stimulated by nicotine and blocked by tubocurarine Two subtypes: NN, NM

Cholinergic Receptors
M1 Location
Autonomic ganglia Gastric Glands CNS

M2
SA Node AV Node Atrium Ventricle Cholinergic nerve endings rate of impulse velocity of conduction Contractility Ach release

M3
Visceral Smooth Muscle Exocrine Glands Vascular endothelium

Function

Depolarisation Acid secretion

Muscle contraction Secretion Vasodilation

Agonist

Oxotremorine

Methacholine

Bethanechol

Antagonist

Pirenzepine

Methoctramine

Darifenacin

Cholinergic Receptors
NM NN

Location

Neuromuscular Junction

Autonomic Ganglia Adrenal medulla CNS

Function

Contraction of skeletal Postganglionic muscle impulse generation Catecholamine release Site specific action
PTMA, Nicotine Tubocurarine DMPP, Nicotine Hexamethonium

Agonist Antagonist

Cholinergic Drugs
(cholinomimetic/parasympathomimetic)
These are drugs which produceactions similar to Ach,

by directly interacting with cholinergic receptors

Choline esters: Acetylcholine, methacholine, Carbachol, Bethanechol Alkaloids: Muscarine, Pilocarpine, Arecoline

Pharmacological Actions
Ach is the prototype drug

A: Muscarinic Actions
Heart: At SA Node: Hyperpolarisation> rate of contraction>Bradycardia At AV Node: Refractory period increased>conduction>force of atrial contraction Ventricular contractility is also decreased

Pharmacological Actions
Blood Vessels All blood vessels are dilated: release of endothelium dependent relaxing factor (EDRF) Fall in BP and flushing Smooth Muscle: GIT: Tone and peristalsis is increased, sphincters relaxes>abdominal cramps and evacuation of bowel Peristalsis in ureter is increased>voiding of bladder Lungs: Bronchial muscles constrict>dyspnoea, asthma attack

Pharmacological Actions
Glands: Secretion of all glands is increased Sweating, salivation, lacrymation, tracheobronchial and gastric secretion increased. Eye: Contraction of circular muscle>miosis Contraction of ciliary muscle>spasm of accomodation, increased outflow facility, IOT

Pharmacological Actions
B: Nicotinic
Autonomic ganglia: High Dose: Both sympathetic and parasympathetic ganglia are stimulated Skeletal Muscle: Muscle: At muscle end plate>contraction of fibre>twitching and fasciculations

Indications/Uses
Postoperative/postpartum nonobstructive urinary

retention (bethanechol) Neurogenic bladder atony, congential megacolon, GERD Pilocarpine (alkaloid from leaves of Pilocarpus microphyllus)
Open angle glaucoma Miosis, ciliary muscle contraction To counteract mydriatics after refraction testing To break adheshions of iris with lens or cornea by

alternating with mydriatics