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- Pilocarpine (2)
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Pilocarpine
From Wikipedia, the free encyclopedia
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Pilocarpine
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| Systematic (IUPAC) name | |
| (3S,4R)-3-ethyl-4- [(3-methylimidazol-4-yl) methyl]oxolan-2-one | |
| Identifiers | |
| CAS number | 54-71-7 |
| ATC code | N07 S01EB01 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C11H16N2O2 |
| Mol. mass | 208.257 g/mol |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Metabolism | ? |
| Half life | 0.76 hours |
| Excretion | ? |
| Therapeutic considerations | |
| Pregnancy cat. |
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| Legal status | |
| Routes | ? |
Pilocarpine is a muscarinic alkaloid obtained from the leaves of tropical American shrubs from the genus Pilocarpus. It acts as a muscarinic receptor agonist in the parasympathetic nervous system.
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Pilocarpine has been used in the treatment of chronic open-angle glaucoma and acute angle-closure glaucoma for over 100 years.[1] It acts on a subtype of muscarinic receptor (M3) found on the iris sphincter muscle, causing the muscle to contract and produce miosis. This opens the trabecular meshwork through increased tension on the scleral spur. This action facilitates the rate that aqueous humor leaves the eye to decrease intraocular pressure.
Pilocarpine is also used to treat dry mouth (xerostomia). Pilocarpine stimulates the secretion of large amounts of saliva and sweat. It may also cause hypotension and bradycardia in the cardiovascular system, and bronchospasm and increased bronchial secretion in the lungs due to its non-selective muscarinic action.
Pilocarpine is used to stimulate sweat glands in a sweat test to measure the concentration of chloride and sodium that is excreted in sweat. It is used to diagnose cystic fibrosis (CF).
Pilocarpine is available under several trade names such as: Diocarpine (Dioptic), Isopto Carpine (Alcon), Miocarpine (CIBA Vision), Ocusert Pilo-20 and -40 (Alza), Pilopine HS (Alcon), Salagen (Pharmacia & Upjohn), Scheinpharm Pilocarpine (Schein Pharmaceutical), and Timpilo (Merck Frosst).
Use of pilocarpine may result in a range of adverse effects, most of them related to its action as a muscarinic receptor agonist. Pilocarpine has been known to cause excessive sweating, excessive salivation, bronchospasm, increased bronchial mucus secretion, bradycardia, hypotension, browache (when used as eye drops) and diarrhea. It can also result in miosis when used chronically as an eye drop.
The therapeutic uses of pilocarpine are limited by its adverse effects.
- Katzung, Bertram. Basic and Clinical Pharmacology, 9th ed. (2004). ISBN 0-07-141092-9
- Brenner, G. M. (2000). Pharmacology. Philadelphia, PA: W.B. Saunders Company. ISBN 0-7216-7757-6
- Canadian Pharmacists Association (2000). Compendium of Pharmaceuticals and Specialties (25th ed.). Toronto, ON: Webcom. ISBN 0-919115-76-4
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| Sympathomimetics | Apraclonidine, Brimonidine, Clonidine, Dipivefrine, Epinephrine |
| Parasympathomimetics | Aceclidine, Acetylcholine, Carbachol, Demecarium, Echothiophate, Fluostigmine, Neostigmine, Paraoxon, Physostigmine, Pilocarpine |
| Carbonic anhydrase inhibitors | Acetazolamide, Brinzolamide, Diclofenamide, Dorzolamide, Methazolamide |
| Beta blocking agents | Befunolol, Betaxolol, Carteolol, Levobunolol, Metipranolol, Timolol |
| Prostaglandin analogues | Bimatoprost, Latanoprost, Travoprost, Unoprostone |
| Other agents | Dapiprazole, Guanethidine |