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SENSORY ORGANS › OPHTHALMOLOGICALS › ANTIGLAUCOMA PREPARATIONS AND MIOTICS › Parasympathomimetics
pilocarpine, combinations
S01EB51
Forms & Strengths
- Ophthalmic solution: Pilocarpine HCl 1% / Physostigmine salicylate 0.25%
- Ophthalmic solution: Pilocarpine HCl 2% / Physostigmine salicylate 0.25%
- Ophthalmic solution: Pilocarpine HCl 4% / Physostigmine salicylate 0.25%
Adult Dosing
- Instill 1 to 2 drops in the affected eye(s) up to 3 to 4 times daily as directed by the ophthalmologist.
Pediatric Dosing
- Safety and efficacy in pediatric patients have not been established; use is generally avoided or strictly individualized.
Indications
- Reduction of intraocular pressure in open-angle glaucoma
- Reduction of intraocular pressure in chronic angle-closure glaucoma
Mechanism of Action
- Pilocarpine acts as a direct-acting cholinergic parasympathomimetic agent, stimulating muscarinic receptors to contract the ciliary muscle and iris sphincter.
- Contraction of the ciliary muscle pulls on the scleral spur, opening the trabecular meshwork spaces to facilitate aqueous humor outflow and lower intraocular pressure.
- Physostigmine acts as a reversible acetylcholinesterase inhibitor, potentiating cholinergic effects at the neuromuscular junction in the eye.
Contraindications
- Hypersensitivity to pilocarpine, physostigmine, or any component of the formulation
- Conditions where miosis is undesirable, such as acute iritis and acute uveitis
- Secondary glaucoma where constriction of the pupil may exacerbate the condition
Adverse Reactions
- Transient stinging, burning, and ocular discomfort upon instillation
- Induced myopia and blurred vision due to spasm of accommodation
- Ciliary spasm, brow ache, and headache
- Reduced night vision (dim vision), particularly in patients with lens opacities
- Rare systemic cholinergic effects including excessive salivation, lacrimation, diaphoresis, nausea, vomiting, and diarrhea
Drug Interactions
- Concomitant use with other topical ophthalmic antiglaucoma agents may have additive intraocular pressure-lowering effects.
- Anticholinergic agents (e.g., atropine, cyclopentolate) may antagonize the therapeutic ocular effects of pilocarpine.
- Beta-blockers or cholinesterase inhibitors may potentiate systemic or local cholinergic effects.
Curated Content: Needs Vetting Before Put to Clinical Use