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Pharm Ch8
Cholinergic Pharm
| Question | Answer |
|---|---|
| Blocks high-affinity transporter for choline (blocks Ach synthesis) | Hemicholinium-3 |
| Blocks Ach-H+ antiporter (prevents Ach storage) | Vesamicol |
| Degrades synaptobrevin, prevents synaptic vesicle fusion w/ the axon terminal (presynaptic) membrane (inhibits Ach release) | Botulinum toxin |
| Acetylcholinesterase (AchE) Inhibitors: noncovalent (reversible), rapid, lasts 2-10min (short-acting); Dx: muscle weakness d/t depolarizing blockade; Tx: Myasthenia gravis (MG), Eaton-Lambert syndrome | Edrophonium |
| Acetylcholinesterase (AchE) Inhibitors: lasts 3-8 hrs, longer-acting AchE’s (for chronic Tx MG); Tx: ↓IOP (glaucoma), ↑GI motility, relieves abdominal distention | Ambenonium Pyridostigmine Neostigmine Physostigmine |
| Acetylcholinesterase (AchE) Inhibitors: reverses anticholinergic drug poisoning | Physostigmine |
| Acetylcholinesterase (AchE) Inhibitors: Irreversible d/t “aging” | Diisopropyl fluorophosphate |
| Acetylcholinesterase (AchE) Inhibitors: strong nucleophile admin before “aging” to recover enzymatic AchE function | Pralidoxime |
| Acetylcholinesterase (AchE) Inhibitors: rarely used d/t hepatotoxicity | Tacrine |
| Acetylcholinesterase (AchE) Inhibitors: reversible, 100% bioavail, 3-5h | Donepezil |
| Acetylcholinesterase (AchE) Inhibitors: “pseudo-irreversible” | Rivastigmine |
| Acetylcholinesterase (AchE) Inhibitors: reversible, non-potentiating ligand of nicotinic receptors | Galantamine |
| Tx, ADRs and CIs of AchE inhibitors? | Tx: mild-moderate AD ADRs: N/V/D, flatulence, loose stools, anorexia, abdominal cramping CI: unstable cardiac disease, epilepsy, PUD |
| Muscarinic Receptor Agonists (parasympathomimetic): cardiac vagomimetic, unpredictable; only used to Dx asthma | Methacholine |
| Muscarinic Receptor Agonists (parasympathomimetic): Tx: topical miotic, glaucoma (↓IOP) | Carbachol |
| Muscarinic Receptor Agonists (parasympathomimetic): Tx: GI, urinary tract motility (post-op, post-partum, drug-related urinary retention), hypotonic neurogenic bladder | Bethanechol |
| Muscarinic Receptor Agonists (parasympathomimetic): quaternary amine alkaloid, poor bioavailability | Muscarine |
| Muscarinic Receptor Agonists (parasympathomimetic): most clinically used alkaloid, miotic agent, sialagogue (saliva-inducing), Tx: xerostomia (dry mouth) | Pilocarpine |
| Muscarinic Receptor Agonists (parasympathomimetic): M1/M3 agonist, Tx: xerostomia in Sjogren’s syndrome | Cevimeline |
| Nicotinic Receptor (nAchR) Agonist: induces flaccid paralysis in surgery via depolarizing blockade, can be unpredictable | Succinylcholine |
| Muscarinic Receptor Antagonists (sympathomimetic): Tx: induces mydriasis, reverse sinus bradycardia, inhibit excessive salivation and mucus secretion (surgery), counteract mushroom muscarine poisoning | Atropine |
| Muscarinic Receptor Antagonists (sympathomimetic): ADRs: anterograde amnesia, inattention; Tx: motion sickness, nausea (chemotherapy) | Scopolamine |
| Muscarinic Receptor Antagonists (sympathomimetic): quaternary amine antimuscarinics (low CNS penetration); Tx: PUD, decrease GI spasm, prevent bradycardia, decrease oral secretions | Methscopolamine Glycopyrrolate |
| Muscarinic Receptor Antagonists (sympathomimetic): M1/M4, Tx: PUD | Pirenzepine |
| Muscarinic Receptor Antagonists (sympathomimetic): quaternary ammonium, Tx: COPD | Ipratropium |
| Muscarinic Receptor Antagonists (sympathomimetic): bronchodilator, Tx: COPD | Tiotropium |
| Nonspecific Muscarinic Receptor Antagonists (sympathomimetic): Tx: overactive bladder; ADRs: tachycardia, delirium, hallucinations, seziures, blurred vision (cycloplegia/mydriasis); CI: patients with glaucoma, BPH | Oxybutynin Propantheline Trospium Tolterodine Terodiline |
| Muscarinic Receptor Antagonists (sympathomimetic): newer selective M3; less dry mouth and constipation | Darifenacin, Solifenacin |
| Nicotinic Receptor Antagonists: Nondepolarizing competitive NM blockade; ADRs: muscular paralysis (reversed by AchE inhibitors): very long-lasting | D-tubocurarine Pancuronium |
| Nicotinic Receptor Antagonists: Nondepolarizing competitive NM blockade; ADRs: muscular paralysis (reversed by AchE inhibitors): intermediate | Vecuronium Rocuronium |
| Nicotinic Receptor Antagonists: Nondepolarizing competitive NM blockade; ADRs: muscular paralysis (reversed by AchE inhibitors): rapidly degraded | Mivacurium |
| Nicotinic Receptor Antagonists: administered when ganglionic blockade is desired; Tx: HTN in acute aortic dissection | Mecamylamine Trimethaphan |
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