Cholinergics ANSLect 16_2010BbF - Cholinergics Agonists and...

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Cholinergics Agonists and Antagonists
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Lecture Objectives Review Examine drug manipulation of cholinergic system I. Cholinomimetics A. Natural and synthetic Ag B. Cholinesterase and inhibitors A. Reversible B. Irrerversible II. Muscarinic R ANT Atropine, Scopolamine & synthetic compounds III. Nicotinic R Ag IV. Nicotinic R ANT- ganglionic blockers FOCUS: mechanism/effects therapeutic use adverse effects
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In review: Neurotransmitter...? Selectivity between n &m R: BBB: Absorption and degradation: IV dose: all observed effects target “postganglionic” Role in periphery NMJ Role in ANS nACh and mACh R’s Physiological importance
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Acetylcholine Choline Choline Acetyl Coenzyme A Choline transporter + Acetyltransferase Acetylcholinesterase (AChE) ACh m or n Ach R Fig. 11.3 Kalant et al. Hemicholine Vesamicol
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