QuickView for pilocarpine (compound)

Summary
General Info

PubChem

PubChem Compound 10285971

Name:	Pilocarpine
PubChem Compound ID:	10285971
Description:	A slowly hydrolyzed muscarinic agonist with no nicotinic effects. Pilocarpine is used as a miotic and in the treatment of glaucoma.
Molecular formula:	C₁₁H₁₇ClN₂O₂
Molecular weight:	244.718 g/mol

DrugBank

Identification

Name:	Pilocarpine
Name (isomeric):	DB01085
Drug Type:	small molecule
Description:	A slowly hydrolyzed muscarinic agonist with no nicotinic effects. Pilocarpine is used as a miotic and in the treatment of glaucoma.
Synonyms:	Spersacarpine; Beta-pilocarpine hydrochloride; Pilocarpine muriate; Pilocarpine HCl; Pilokarpin monohydrochloride; Pilocarpine chloride; Pilocarpine monohydrochloride; Pilocarpine hydrochloride; Adsorbocarpine; Spersacarpine hydrochloride. show more » Spersacarpine; Beta-pilocarpine hydrochloride; Pilocarpine muriate; Pilocarpine HCl; Pilokarpin monohydrochloride; Pilocarpine chloride; Pilocarpine monohydrochloride; Pilocarpine hydrochloride; Adsorbocarpine; Spersacarpine hydrochloride; Pilocarpin; Pilokarpin show less «
Brand:	Pilopine HS, Pilomiotin, Ocusert Pilo-40, Ocusert Pilo-20, Piloptic-2, Almocarpine, Pilocar SMP, Piloptic-1, Epicar, Ocu-Carpine, Akarpine, Isoptocarpine, Pilovisc, Mi-Pilo Ophth Sol, Pilagan, Mistura P, Pilokarpol, Ocusert P 20, Miocarpine, Piloptic-1/2, Amistura P, Pilocel, Pilocarpal, Pilostat, Syncarpine, Ami-Pilo, Ocusert Pilo, Pilocar, Piloptic-3, Piloptic-4, Isopto Carpine, P.V. Carpine Liquifilm, Piloptic-6, Sno Pilo, Salagen, Minims Pilocarpine, Pilocarpol, Mi-Pilo
Brand name mixture:	Timpilo 2(Pilocarpine Hydrochloride + Timolol Maleate), E-Pilo 4 Ophthalmic Solution(Epinephrine Bitartrate + Pilocarpine Hydrochloride), E-Pilo 1 Ophthalmic Solution(Epinephrine bitartrate + Pilocarpine hydrochloride), E-Pilo-4 Oph Soln(Epinephrine Bitartrate + Pilocarpine Hydrochloride), E-Pilo 6 Ophthalmic Solution(Epinephrine Bitartrate + Pi... show more » Timpilo 2(Pilocarpine Hydrochloride + Timolol Maleate), E-Pilo 4 Ophthalmic Solution(Epinephrine Bitartrate + Pilocarpine Hydrochloride), E-Pilo 1 Ophthalmic Solution(Epinephrine bitartrate + Pilocarpine hydrochloride), E-Pilo-4 Oph Soln(Epinephrine Bitartrate + Pilocarpine Hydrochloride), E-Pilo 6 Ophthalmic Solution(Epinephrine Bitartrate + Pilocarpine Hydrochloride), E-Pilo-1 Oph Soln(Epinephrine Bitartrate + Pilocarpine Hydrochloride), E-Pilo-2 Oph Soln(Epinephrine Bitartrate + Pilocarpine Hydrochloride), E-Pilo 2 Ophthalmic Solution(Epinephrine bitartrate + Pilocarpine hydrochloride), E-Pilo-6 Oph Soln(Epinephrine Bitartrate + Pilocarpine Hydrochloride), Timpilo 4(Pilocarpine Hydrochloride + Timolol Maleate) show less «
Category:	Miotics, Muscarinic Agonists, Cholinergic Agents
CAS number:	54-71-7

Pharmacology

Indication:	For the treatment of radiation-induced dry mouth (xerostomia) and symptoms of dry mouth in patients with Sjögrens syndrome.
Pharmacology:	Pilocarpine is a choline ester miotic and a positively charged quaternary ammonium compound. Pilocarpine, in appropriate dosage, can increase secretion by the exocrine glands. The sweat, salivary, lacrimal, gastric, pancreatic, and intestinal glands and the mucous cells of the respiratory tract may be stimulated. When applied topically to the eye a... show more » Pilocarpine is a choline ester miotic and a positively charged quaternary ammonium compound. Pilocarpine, in appropriate dosage, can increase secretion by the exocrine glands. The sweat, salivary, lacrimal, gastric, pancreatic, and intestinal glands and the mucous cells of the respiratory tract may be stimulated. When applied topically to the eye as a single dose it causes miosis, spasm of accommodation, and may cause a transitory rise in intraocular pressure followed by a more persistent fall. Dose-related smooth muscle stimulation of the intestinal tract may cause increased tone, increased motility, spasm, and tenesmus. Bronchial smooth muscle tone may increase. The tone and motility of urinary tract, gallbladder, and biliary duct smooth muscle may be enhanced. Pilocarpine may have paradoxical effects on the cardiovascular system. The expected effect of a muscarinic agonist is vasodepression, but administration of pilocarpine may produce hypertension after a brief episode of hypotension. Bradycardia and tachycardia have both been reported with use of pilocarpine. show less «
Mechanism of Action:	Pilocarpine is a cholinergic parasympathomimetic agent. It increase secretion by the exocrine glands, and produces contraction of the iris sphincter muscle and ciliary muscle (when given topically to the eyes) by mainly stimulating muscarinic receptors.
Absorption:	There was a decrease in the rate of absorption of pilocarpine from SALAGEN Tablets when taken with a high fat meal by 12 healthy male volunteers
Biotransformation:	Possibly occurs at the neuronal synapses and in the plasma
Half Life:	0.76 hours
Affected organisms:	Humans and other mammals

Interactions

Drug interaction:

Tacrine

The acetylcholinesterase inhibitor, Tacrine, may increase the adverse/toxic effects of Pilocarpine, a cholinergic agonist. Monitor for increased cholinergic effects and toxicity.

Targets

Muscarinic acetylcholine receptor M3

Muscarinic acetylcholine receptor M1

Muscarinic acetylcholine receptor M2

Enzymes

Cytochrome P450 2A6

Cytochrome P450 2E1

Cytochrome P450 3A4