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![INTRODUCTION :
• Agents which block the effects of Ach on cholinergic
receptors.
• Commonly antimuscarinic drugs are considered as
anticholinergic drugs.
• [PARASYMPATHOLYTIC DRUGS]
• Atropine is the prototype drug.](https://image.slidesharecdn.com/anticholinergicdrugs-200624095142/75/Anticholinergic-drugs-2-2048.jpg)
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Anticholinergic drugs
This document summarizes anticholinergic drugs. It discusses that they block the effects of acetylcholine on cholinergic receptors, with atropine being the prototype drug. The document classifies anticholinergic drugs into natural alkaloids like atropine and hyoscine, semisynthetic derivatives, and synthetic derivatives. It then describes the mechanism of action, effects, pharmacokinetics, adverse effects, belladonna poisoning, and uses of these anticholinergic drugs like atropine.
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Anticholinergic drugs
- 1.
- 2. INTRODUCTION : • Agentswhich block the effects of Ach on cholinergic receptors. • Commonly antimuscarinic drugs are considered as anticholinergic drugs. • [PARASYMPATHOLYTIC DRUGS] • Atropine is the prototype drug.
- 3. CLASSIFICATION : Natural alkaloids Atropine, Hyoscine(scopolamine) Semisynthetic derivatives Homatropine,Atropine methonitrate, Hyoscine butyl bromide, Ipratropium bromide, Tiotropium bromide Synthetic derivatives Mydriatics Cyclopentolate, Tropicamide Antisecretory – antispasmodics Quaternary compounds Propantheline, Oxyphenonium, Clidinium, Pipenzolate methyl bromide, Isopropamide, Glycopyrolate Tertiary amines Dicyclomine, Valethamate, Pirenzepine Vasicoselective Oxybutynin, Flavoxate, Tolterodine Antiparkinsonian Trihexyphenidyl (Benzhexol), Procyclidine, Biperiden
- 4. ATROPINE • It isa natural alkaloid Obtained from atropine belladonna. • They are muscarinic antagonist.
- 5. MECHANISM OF ACTION: • Bind to muscarinic receptors & block the effects of acetylcholine at the receptors. • Competitive antagonist. • Antagonism reversible by increasing the concentration of agonist. • Acetylcholine & scopolamine are non- selective antagonist & block all the sub types (M1 to M5)
- 6. ACTIONS : • CVS: oHeart - ↑ heart rate by blocking M2 receptor in SA node. • Secretions : oReduces all secretions except milk. • Smooth muscle : • GIT – reduces the tone & motility & relives spasm • Biliary tract – relives biliary spasm • Bronchi : Bronchodilation • Genitourinary bladder – relaxes ureters & bladders. • Eye : • Mydriasis (passive) – relaxing sphincter pupillae • Cyclopegia – paralysis of ciliary muscle • ↑ IOP – block the drainage of aqueous humor. • CNS : • Restlessness, disorientation, hallucination, delirium.
- 7. PHARMACOKINETICS : • Wellabsorbed • Cross BBB • Metabolised in the liver. • T 1 2 : 3-4 hrs
- 8. ADVERSE EFFECTS : •Blurring of vision • Dry mouth • Dysphagia • Dry skin • Fever • Constipation • Urinary retention
- 9. BELLADONNA POISONING : •Symptoms : • Palpitation, flushing, restlessness, delirium, hallucination, psychosis, circulatory collapse, respiratory failure, convulsion, coma. • Rx. • Symptomatic • Gastric lavage • Physostigmine can also be administered.
- 10. USES : • Cardiovasculardisease – bradycardia due to excessive vagal stimulation • Eye • Diagnostic (testing of errors of refraction & fundoscopic examination • Therapeutic : mydriatics + miotics – to break adhesion between iris & lens • To provide rest to iris in iritis, iridocyclitis, keratitis • Antispasmodic : renal colic, biliary colic, abdominal colic • Pre- anaesthetic medication : ↓ salivary secretion & prevent laryngospasm, bradycardia, aspiration pneumonia • Poisoning : Organophosphorus, curare • Motion sickness - hyoscine
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