pilocarpine ophthalmic (IsoptoCarpine, Pilopine HS, Akarpine): Dosing and Uses

Dosing and uses of IsoptoCarpine, Pilopine HS (pilocarpine ophthalmic)

• Adult
• Pediatric

Adult dosage forms and strengths

ophthalmic solution

• 1%
• 2%
• 4%

geL

• 4%

Intraocular Pressure

Solution: Apply 1-2 gtt up to q6hr; adjust concentration and frequency as necessary to control IOp

Gel: Apply 0.5-inch ribbon in lower conjunctival sac of affected eye(s) qHs

Counteract Mydriatic Effects of Sympathomimetic Agents (Off-label)

Ophthalmic solution: 1 gtt of 1% solution in affected eye

Other Indications & Uses

Antiglaucoma, miotic, green-top; reduces intraocular pressure (IOP) in patients with open & closed angle glaucoma

NOT effective in very high IOP seen in some closed angle attacks, should be used in combination with acetazolamide IV and mannitol IV

Pediatric dosage forms and strengths

Safety and efficacy not established

IsoptoCarpine, Pilopine HS (pilocarpine ophthalmic) adverse (side) effects

Frequency not defined

Accomodative spasm

Miosis

Ocular irritation

Difficulty seeing in poorly lit areas, especially in patients with cataracts

Ocular burning/itching

Temporal or supraorbital headache

Decreased visual acuity

Hypertension

Corneal glanularity (gel)

Tachycardia

Myopia

Conjunctival vascular congestion

Lacrimation

Salivation

Nausea

Vomiting

Headache

Bronchial spasm

Diaphoresis

Retinal detachment (rare)

Warnings

Contraindications

Hypersensitivity to drug or component; acute inflammatory disease of the anterior chamber

Pregnancy and lactation

Pregnancy category: C

Lactation: Excretion in breast milk unknown; use with caution

Pregnancy categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

Pharmacology of IsoptoCarpine, Pilopine HS (pilocarpine ophthalmic)

Mechanism of action

Causes miosis by stimulating cholinergic receptors by contracting the sphincter; loss of accomodation by constriction of ciliary muscle; lowers intraocular pressure

Pharmacokinetics

Onset: 10-30 min (miosis); 1 hr (IOP)

Duration: 4-8hr (miosis); 4-12hr (IOP)