Showing posts with label Tertiary M2-Muscarinic Antagonist. Show all posts
Showing posts with label Tertiary M2-Muscarinic Antagonist. Show all posts

Scopolamine (Transderm-Scop)

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Name: Scopolamine (Transderm-Scop)

Class: Tertiary M2-Muscarinic Antagonist

Mechanism: Bind to muscarinic receptors and competitively inhib. ACh interaction.

Absorption: Oral, transdermal, parenteral.

Dist.:

Metabolism.:

Excretion, :

Toxicity/S.E.s: Drowsiness, blurred vision, dry mouth, urinary retention, tachycardia, constipation, cycloplegia. Mostly avoided w/transdermal application.

Utility: Prevent motion sickness (transdermal patch). Give parenterally in advance to counteract nasty anesthesia side effects (cardiac slowing, salivation, bronchial secretions).

Features: In addition to atropine-like anti-musc properties, also produces central depressant and anti-motion sickness effects. Best if admin. prophylactically

 

Tropicamide (Mydriacil)

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Name: Tropicamide (Mydriacil)

Class: Tertiary M2-Muscarinic Antagonist

Mech.: Bind to muscarinic receptors and competitively inhib. ACh interaction.

Absorption: Eye drops

Dist.:

Metab.:

Excretion, :

Toxicity/S.E.s: Topical eye applic. can precipitate glaucoma.

Utility: Apply to conjunctival sac to produce mydriasis and cycloplegia (lasts ~6hr).

Special Features:

 

Scopolamine (Transderm-Scop)

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Name: Scopolamine (Transderm-Scop)

Class: Tertiary M2-Muscarinic Antagonist

Mech.: Bind to muscarinic receptors and competitively inhib. ACh interaction.

Absorption: Oral, transdermal, parenteral.

Dist.:

Metab.:

Excretion, :

Toxicity/S.E.s: Drowsiness, blurred vision, dry mouth, urinary retention, tachycardia, constipation, cyclopegia. Mostly avoided w/transdermal application.

Utility: Prevent motion sickness (transdermal patch). Give parenterally in advance to counteract nasty anesthesia side effects (cardiac slowing, salivation, bronchial secretions).

Features: In addition to atropine-like anti-musc properties, also produces central depressant and anti-motion sickness effects. Best if admin. prophylactically.

 

Atropine

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Name: Atropine

Class: Tertiary M2-Muscarinic Antagonist

Mech.: Bind to muscarinic receptors and competitively inhib. ACh interaction.

Absorption: Syst. absorption from eye drops. Oral good.—use gastric lavage to limit systemic absorption. IV.

Dist.: Selective doses (0.2-0.5 mg) act at muscar. receptors, not at nicot. receptors

Metab.:

Excretion, :

Toxicity/S.E.s: Dry as a bone (sweat/saliva blocked), blind as a bat (pupil dilation, no ciliary muscle contraction), red as a beet (flushing and rash over face, neck, upper part of trunk), hot as a hare (no sweat ® ­ temp), mad as a hatter (delirium, toxic psychosis). Urinary retention, constipation. Treat intoxication w/physostigmine. Diazepam relieves CNS effects. Topical eye applic. can precipitate glaucoma.

Utility: Give parenterally in advance to counteract nasty anesthesia side effects (cardiac slowing, salivation, bronchial secretions). Treat anticholinesterase poisoning. Treat urinary problems. Can be applied to eye to produce mydriasis and cyclopegia (lasts 7-12 days).