Antimuscarinic agents

Dr. Mohamed Samai

Bsc (Hons), Msc,
MBBS, PGCRM, PhD
Head, Department of
Pharmacology
COMAHS, USL.
Overview

 Introduction
 History
 List of drugs
 Mode of actions
 Pharmacological actions
 pharmacokinetics
 Clinical uses
 Side effects and contra-indications
Introduction

 Antimuscarinic agents are drugs that inhibit

the action of Ach or cholinergic agonists or
PNS stimulation at muscarinic receptors
 Atropine is the prototype
 Also known as atropine-like drugs
 Isolated from belladonna alkaloids
List of drugs

 Atropine  Tolterone
 Methyl atropine  oxybutynin
 Scopolamine  Tropicamide
 Homatropine  Tropicamide
 Pirenzepine  Cyclopentolate
 Telenzepine  Glycopyrrolate
 Ipratropium  Benztropine
methybromide  Trihexyphenidyl
 tiotropium
Pharmacological actions of
Atropine
 CVS: dose dependent
-Low dose →↓HR
-high dose (TD) →↑HR
-BVs: no effect (no innervation) but toxic
doses cause profound vasodilatation
 GIT: ↓intestinal tone, ↓motility, ↑tone to sphincters
 GUT: relaxation of BSMs, contraction of
vesical sphincters
 Respiratory: bronchodilatation, ↓bronchial
 Pharmacological actions of
Atropine

 Eye: mydriasis, accommodation for far vision, decrease

outflow of aqueous humour, cycloplegia (relaxation of
ciliary muscle)
 Exocrine glands: ↓salivation, gastric acid secretion,
sweating, lacrimation
 CNS: dose dependent: -Therapeutic doses: CNS
stimulation- restlessness, irritability, disorientation,
hallucinations or delirium
 -Large doses: depression leading to circulatory
collapse, paralysis, coma, respiratory failure & death
 Pharmacological actions of
Atropine

 CNS: Scopolamine: -Therapeutic doses: CNS

depression- drowsiness, amnesia, fatigue, dreamless
sleep, euphoria (can be abuse)
 Pharmacokinetics

 Belladona alkaloids, tertiary synthetic and semi-synthetic derivatives

are rapidly absorbed
 Systemic absorption of inhaled or orally administered quaternary agents
is minimal
 Quaternary derivatives also penetrate the conjunctiva and BBB less
readily
 T1/2 of atropine is 4hrs
 50% is metabolized in the liver
 50% excreted unchanged
 Ipratropium-inhalation (90% is swallowed and most appears in feces);
effects lasts for 4-6 hrs
 Tiotropium effects last for 24 hrs
Clinical Uses

 Parkinson’s disease e.g.atropine, benztropine,

trihexyphenidyl
 Pre-anesthetic medication: atropine, glycopyrrolate
 Ophthalmology: mydriasis for examination of the
retina and optic disc- atropine, scopolamine,
cyclopentolate, tropicamide
 Motion sickness-scopolamine
 Bronchial asthma- ipratropium, tiotropium, atropine
 Hyperactive carotid sinus reflex (severe bradycardia
and syncope): atropine
 Bradycardia following MI: atropine
Clinical uses

 Peptic ulcer- atropine, scopolamine, pirenzepine,

telenzepine
 Irritable bowel syndrome: scopolamine
 Diarrhoea: atropine
 Overactive bladder: enuresis; urge incontinence-
oxybutynin, tolterodine
 Antidote for: (atropine)
-Organophosphorus poisoning (Nerve gases,
parathion); -Mushroom poisoning (muscarine)
Side effects and contra-indications

 CNS: agitation, delirium, confusion, restlessness, irritability,

disorientation, hallucinations or delirium, convulsions, coma, death
 Dry mouth, thirst -difficulty to speech and swallowing
 Dry skin
 Hot skin-atropine fever
 Constipation
 Urinary retention
 Bradycardia, tachycardia
 Palpitations
 Blurred vision
 Mydriasis (photophobia)
 Cycloplegia
 Skin flush
Thank you very
Much