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Cholinergic Drugs
Cholinergic drugs or parasympathomimetic drugs are
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
Agonist
Oxotremorine
Methacholine
Bethanechol
Antagonist
Pirenzepine
Methoctramine
Darifenacin
Cholinergic Receptors
NM NN
Location
Neuromuscular Junction
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,
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