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NERVOUS SYSTEM › OTHER NERVOUS SYSTEM DRUGS › PARASYMPATHOMIMETICS › Other parasympathomimetics
pilocarpine
N07AX01
Forms & Strengths
- Oral tablet: 5 mg
- Ophthalmic solution: 1%, 2%, 4%
- Ophthalmic gel: 4%
Adult Dosing
- Oral (Xerostomia): 5 mg orally 3 times daily; may titrate up to 10 mg 3 times daily based on efficacy and tolerance
- Ophthalmic (Glaucoma): Instill 1 to 2 drops of 1% to 4% solution up to 4 times daily, or apply a 0.5-inch ribbon of 4% gel once daily at bedtime
Pediatric Dosing
- Oral (Xerostomia): Safety and efficacy not established
- Ophthalmic (Glaucoma): Instill 1 to 2 drops of 1% to 2% solution up to 3 times daily as directed by ophthalmologist
Indications
- Treatment of symptoms of dry mouth (xerostomia) from salivary gland hypofunction caused by radiotherapy for head and neck cancer
- Treatment of symptoms of dry mouth in Sjögren's syndrome
- Reduction of intraocular pressure in ocular hypertension and open-angle or angle-closure glaucoma
- Induction of miosis
Mechanism of Action
- Acts as a direct-acting cholinergic parasympathomimetic agent
- Stimulates muscarinic (M3) receptors, causing secretion of exocrine glands (salivary, sweat, lacrimal)
- Contracts the iris sphincter muscle causing miosis and contraction of the ciliary muscle leading to increased outflow of aqueous humor to lower intraocular pressure
Contraindications
- Uncontrolled asthma
- Known hypersensitivity to pilocarpine
- Conditions where miosis is undesirable, such as acute iritis and acute-angle closure glaucoma (for systemic use or when pupillary constriction is contraindicated)
Adverse Reactions
- Excessive sweating (diaphoresis)
- Nausea and vomiting
- Rhinitis and excessive lacrimation
- Urinary frequency
- Flushing and dizziness
- Chills and headache
- Blurred vision and impaired night vision (ophthalmic formulations)
Drug Interactions
- Beta-blockers: Potential for conduction disturbances when used with ophthalmic pilocarpine
- Anticholinergic agents: May antagonize the pharmacological effects of pilocarpine
- CYP2A6 inhibitors/substrates: Potential for pharmacokinetic interactions though primarily eliminated via renal excretion
Curated Content: Needs Vetting Before Put to Clinical Use