It is used to treat dry mouth (xerostomia), particularly in Sjögren's syndrome, but also as a side effect of radiation therapy for head and neck cancer. It has also been used in the treatment of chronic open-angle glaucoma and acute angle-closure glaucoma for over 100 years.
Pilocarpine is a cholinergic agonist exerting a broad spectrum of pharmacologic effects with predominant muscarinic action. Pilocarpine, in appropriate dosage, can increase secretion by the exocrine glands such as sweat, salivary, lacrimal, gastric, pancreatic, and intestinal glands and the mucous cells of the respiratory tract. The tone and motility of urinary tract, gallbladder and biliary duct, smooth muscle may be enhanced.
ORAL Dry mouth after radiotherapy for malignant neoplasms of the head & neck: Adult: Initial dose: 5 mg tid. If necessary, increase dose gradually after 4 wk until adequate response is achieved. Max dose: 10mg tid. Sjogren’s syndrome: Adult: 5mg 4 times daily. Max: 30 mg daily. Stop treatment if no improvement after 3 mth. OPHTHALMIC Open-angle glaucoma: Adult: As HCI or nitrate: Instill a 0.5-4% soln into the eye 4 times daily. As modifiedrelease preparation: insert prep into the conjunctival sac which releases 20-40 mcg/ hr for 7 days. As 4% ophth gel: apply once nightly into the affected eye(s).
Pilocarpine should be administered with caution to patients taking beta adrenergic antagonists because of the possibility of conduction disturbances. Pilocarpine might antagonize the anticholinergic effects of drugs used concomitantly.
Angle-closure glaucoma; acute iritis, anterior uveitis; hypersensitivity. Pregnancy. Retinal detachment; corneal or conjunctival damage. Patients w/ cognitive or psychiatric disorders, renal impairment, biliary tract disorders. Prolonged use may lead to lens opacities. May impair ability to drive or operate machines. Lactation.
Ocular: Pain & irritation, blurred vision, lachrymation, browache, conjunctival vascular congestion, superficial keratitis, vitreous haemorrhage, increased pupillary block.
Pilocarpine has been assigned to pregnancy category C by the FDA. Animal studies have revealed evidence of fetotoxicity, fetolethality, and embryolethality. There are no controlled data in human pregnancy. Pilocarpine is only recommended for use during pregnancy when benefit outweighs risk. There are no data on the excretion of pilocarpine into human milk. The manufacturer recommends that due to the potential for serious adverse reactions in nursing infants, a decision should be made to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother.
Dilution with water and other fluids is the usual response to accidental or deliberate overdose.
Ophthalmic: Store at room temperature and protect from light. It is desirable that the contents should not be used more than 4 weeks after first opening of the bottle.
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