Brands, Medical Use, Clinical Data
Drug Category
- Cholinergic Agents
- Muscarinic Agonists
- Miotics
Dosage Forms
- Drops
- Gel
- Implant
- Liquid
- Solution
Brands / Synonyms
Adsorbocarpine; Akarpine; Almocarpine; Ami-Pilo; Amistura P; Beta-pilocarpine hydrochloride; Betoptic Pilo; Epicar; Isopto Carpine; Isoptocarpine; Mi-Pilo; Mi-Pilo Ophth Sol; Minims Pilocarpine; Miocarpine; Mistura P; 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]; Pilocarpol; Pilocel; Pilokarpin; Pilokarpin monohydrochloride; Pilokarpol; Pilomiotin; Pilopine HS; Piloptic-1; Piloptic-1/2; Piloptic-2; Piloptic-3; Piloptic-4; Piloptic-6; Pilostat; Pilovisc; Salagen; Sno Pilo; Spersacarpine; Spersacarpine hydrochloride; Syncarpine
Indications
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.
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
Toxicity
Not Available
Biotrnasformation / Drug Metabolism
Possibly occurs at the neuronal synapses and in the plasma
Contraindications
SALAGEN® Tablets are contraindicated in patients with uncontrolled asthma, known hypersensitivity
to pilocarpine, and when miosis is undesirable, e.g., in acute iritis and in narrow-angle (angle closure)
glaucoma.
Drug Interactions
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.
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