Pilocarpine
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.
Contraindications
None.
Available FormsOphthalmic solution, 1% (15 mL), 2% (15 mL), 4% (15 mL)
Mechanism of ActionDirect 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 & LactationPregnancy: 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 UseSafety and effectiveness established; children under 2 years are dosed at 1% three times daily.