Muscarinic antagonist
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A muscarinic receptor antagonist is an agent that reduces the activity of the muscarinic acetylcholine receptor. Most of them are synthetic, but scopolamine atropine are belladonna alkaloids, and are naturally extracted.
Important[1] muscarinic agonists include atropine, hyoscine, ipratropium, tropicamide, cyclopentolate and pirenzepine.
Contents |
| Substance | Trade names | Mechanism[2] | Clinical use[2] | Adverse effects[2] |
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| Atropine (D/L-Hyoscyamine) | non-selective antagonism, CNS stimulation |
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| Scopolamine (L-Hyoscine) | non-selective antagonism, CNS depression |
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| Ipratropium | non-selective antagonism, without any mucociliary excretion inhibition. |
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| Tropicamide | short acting non-selective antagonism, CNS depression |
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| Pirenzepine | M1 receptor-selective antagonist
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(fewer than non-selective ones) | |
| Diphenhydramine | Benadryl | |||
| Dimenhydrinate | Dramamine | |||
| dicyclomine | ||||
| flavoxate | ||||
| oxybutynin | ||||
| tiotropium | Spiriva | |||
| cyclopentolate | short acting non-selective antagonism, CNS depression |
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| atropine methonitrate | non-selective antagonism, blocks transmission in ganglia |
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| trihexyphenidyl | ||||
| tolterodine | Detrusitol | |||
| solifenacin | Vesicare | |||
| darifenacin | Enablex | |||
| benztropine | Cogentin |
- ^ Rang, H. P. (2003). Pharmacology. Edinburgh: Churchill Livingstone. ISBN 0-443-07145-4. Page 147
- ^ a b c Unless else specified in table boxes, then ref is: Rang, H. P. (2003). Pharmacology. Edinburgh: Churchill Livingstone. ISBN 0-443-07145-4. Page 147
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| Drugs for functional bowel disorders | antimuscarinics: Mebeverine - Dicycloverine - Propantheline
papaverine and derivatives: Papaverine - Drotaverine - Moxaverine acting on serotonin receptors: 5-HT3 antagonists (Alosetron, Cilansetron) - 5HT4 agonists (Mosapride, Tegaserod) other: Diisopromine - Isometheptene - Phloroglucinol - Proglumide - Tridihexethyl |
| Belladonna and derivatives (antimuscarinics) |
Atropine - Hyoscyamine - Butylscopolamine - Methylscopolamine |
| Propulsives | primarily dopamine antagonists (Metoclopramide/Bromopride, Domperidone, Alizapride) - serotonin agonists (Cisapride) - Clebopride |
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| Anticholinergics/antimuscarinics | Atropine - Scopolamine - Methylscopolamine - Cyclopentolate - Homatropine - Tropicamide |
| Sympathomimetics | Phenylephrine - Ephedrine - Ibopamine |