Pilocarpine: profile and news

Prostaglandin Analog Improves Results of Selective Laser ... May 3, 2006
...analog users. Patients received 1 drop of 1% pilocarpine in the operative eye 20 minutes before the laser procedure. Researchers ... - DG News

Other information

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 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.

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.

Drug Category
Cholinergic Agents; Muscarinic Agonists; Miotics; ATC:N07AX01; ATC:S01EB01

Brand Names/Synonyms
Adsorbocarpine; Akarpine; Almocarpine; Ami-Pilo; Amistura P; Beta-Pilocarpine Hydrochloride; Epicar; HSDB 3163; Isopto Carpine; Isoptocarpine; Mi-Pilo; Mi-Pilo Ophth Sol; Minims Pilocarpine; Miocarpine; Mistura P; NSC5746; Ocu-Carpine; Ocusert P 20; Ocusert Pilo; Ocusert Pilo-20; Ocusert Pilo-40; P.V. Carpine Liquifilm; Pilagan; Pilocar; Pilocar Smp; Pilocarpal; Pilocarpin; Pilocarpine; Pilocarpine Chloride; Pilocarpine Hcl; Pilocarpine Hydrochloride; Pilocarpine Monohydrochloride; Pilocarpine Muriate; Pilocarpine [Usan:Ban:Jan]; Pilocarpine, Hydrochloride; Pilocarpine, Monohydrochloride; Pilocarpine-; Pilocarpol; Pilocel; Pilokarpin; Pilokarpin Monohydrochloride; Pilokarpol; Pilomiotin; Pilopine Hs; Piloptic-&Frac12;; Piloptic-1; Piloptic-2; Piloptic-3; Piloptic-4; Piloptic-6; Piloptic-½; Pilostat; Pilovisc; Salagen; Sno Pilo; Spersacarpine; Spersacarpine Hydrochloride; Syncarpine

Dosage Forms
DROPS; GEL; IMPLANT; LIQUID; SOLUTION

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

Interactions
Interactions for Pilocarpine:

Pilocarpine should be administered with caution to patients taking beta adrenergic antagonists because of the possibility of conduction disturbances. Drugs with parasympathomimetic effects administered concurrently with pilocarpine would be expected to result in additive pharmacologic effects. Pilocarpine might antagonize the anticholinergic effects of drugs used concomitantly. These effects should be considered when anticholinergic properties may be contributing to the therapeutic effect of concomitant medication (e.g., atropine, inhaled ipratropium).

While no formal drug interaction studies have been performed, the following concomitant drugs were used in at least 10% of patients in either or both Sjögrens efficacy studies: acetylsalicylic acid, artificial tears, calcium, conjugated estrogens, hydroxychloroquine sulfate, ibuprofen, levothyroxine sodium, medroxyprogesterone acetate, methotrexate, multivitamins, naproxen, omeprazole, paracetamol, and prednisone.

Chemical IUPAC Name
3-ethyl-4-[(3-methylimidazol-4-yl)methyl]oxolan-2-one

Chemical Formula
C11H16N2O2

Half Life
0.76 hours

Drug Type
Approved Drug

# Accession No
APRD00382

CAS Registry Number
54-71-7