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Medications›Antiglaucoma›Pilocarpine

Pilocarpine

GoodRx

Pilocarpine 1%, 2%, 4% · ophthalmic solution

Antiglaucoma

Approved uses

Elevated IOP in open-angle glaucoma or ocular hypertension

1 drop of 1%, 2%, or 4% up to four times daily; start pilocarpine-naive patients on 1%

Acute angle-closure glaucoma

1 drop of 1% or 2% up to three times over a 30-minute period; 1 drop of 4% before laser iridoplasty or iridotomy, then 1 drop of 1% four times daily after iridoplasty until an iridotomy can be performed

Prevention of postoperative IOP elevation associated with laser surgery

1 drop of 1%, 2%, or 4%, or two drops administered five minutes apart, 15 to 60 minutes before surgery

Induction of miosis

1 drop of 1%, 2%, or 4%, or two drops five minutes apart; in children before goniotomy or trabeculotomy, 1 drop of 1% or 2% 15 to 60 minutes before surgery

OFF-LABELNot in the FDA label for this product

Adie tonic pupil, dilute pilocarpine test

one instillation of 0.0625% or 0.125%, prepared by dilution since neither is marketed, with the pupil measured 30 to 40 minutes later

Case-control · n=117

In a retrospective case-control study of 117 subjects, 56 with unilateral Adie tonic pupil and 61 controls with unilateral dilated pupils of other cause, 0.0625% discriminated better than 0.125% (area under the ROC curve 0.954 versus 0.840, P = 0.047). With 0.0625%, a change in maximal pupil diameter of at least 0.5 mm on dynamic pupillometry was 100% sensitive and 82.8% specific.

Other forms of Pilocarpine

Qlosi®
Vuity®

Other Antiglaucoma drugs

Alphagan-P®
Azopt®
Betagan®
Betoptic-S®
Combigan®
Cosopt PF®
Cosopt®
Diamox®

Browse all medications All Antiglaucoma drugs

Yoo YJ, Hwang JM, Yang HK. Sci Rep. 2021;11(1):10089, retrospective observational case-control study, PMID 33980910

Contraindications

None.

Available Forms

Ophthalmic solution, 1% (15 mL), 2% (15 mL), 4% (15 mL)

Mechanism of Action

Direct acting muscarinic cholinergic agonist that contracts the ciliary muscle, putting tension on the scleral spur and opening trabecular meshwork spaces so outflow resistance falls and IOP drops. Contraction of the iris sphincter produces miosis, which relieves appositional angle narrowing and closure and lowers IOP in certain types of angle-closure glaucoma.

Warnings & Precautions

Poor illumination: Caution with night driving and hazardous occupations in poor illumination; miotics may also cause accommodative spasm, and patients should not drive or use machinery while vision is not clear.
Pre-existing retinal disease: Rare cases of retinal detachment have been reported in susceptible individuals and in those with pre-existing retinal disease, so examine the retina including funduscopy in all patients before starting therapy.
Iritis: Not recommended for use when iritis is present.
Primary congenital glaucoma: Cases of a paradoxical increase in IOP have been reported in pediatric patients, and use is not recommended in pediatric glaucoma secondary to anterior segment dysgenesis or uveitis, especially active uveitis.
Acute angle-closure sequence: Secretory suppressants and hyperosmotic agents may be needed first to lower IOP below 50 mmHg and relieve iris ischemia.
Contact lens wear: Lenses should be removed before instillation and reinserted no sooner than 10 minutes after dosing.
Systemic exposure: Punctal occlusion for 2 minutes after instillation limits systemic exposure, and other topical ophthalmic drugs should be separated by at least 5 minutes.

Common Side Effects

Ocular, 5% or more: Headache or browache, accommodative change, blurred vision, eye irritation, visual impairment described as dim, dark, or jumping vision, and eye pain, reported in the 2% populations of four controlled trials of 90 days to 2 years that enrolled 317 patients in total.
Pediatric: Adverse reaction profile comparable to that seen in adults.

Systemic: Sweating and gastrointestinal overactivity in sensitive patients at labeled doses; overdosage produces sweating, salivation, nausea, tremors, slowing of the pulse, and a decrease in blood pressure.

Pregnancy & Lactation

Pregnancy: Category C; animal reproduction studies have not been conducted and fetal harm potential is unknown, so give only if clearly needed.

Lactation: Excretion in human milk is unknown; exercise caution in a nursing woman.

Pediatric Use

Safety and effectiveness established; children under 2 years are dosed at 1% three times daily.

Pilocarpine (Pilocarpine 1%, 2%, 4%) | EyeKnow O.D.