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Pilocarpine (Ophthalmic)

Medically reviewed by Drugs.com. Last updated on Aug 17, 2020.

Pronunciation

(pye loe KAR peen)

Index Terms

  • Pilocarpine HCl
  • Pilocarpine Hydrochloride

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Solution, Ophthalmic, as hydrochloride:

Isopto Carpine: 1% (15 mL); 2% (15 mL); 4% (15 mL)

Generic: 1% (15 mL); 2% (15 mL); 4% (15 mL)

Brand Names: U.S.

  • Isopto Carpine

Pharmacologic Category

  • Ophthalmic Agent, Antiglaucoma
  • Ophthalmic Agent, Miotic

Pharmacology

Directly stimulates cholinergic receptors in the eye causing miosis (by contraction of the iris sphincter), loss of accommodation (by constriction of ciliary muscle), and lowering of intraocular pressure (with decreased resistance to aqueous humor outflow)

Onset of Action

Miosis: 10 to 30 minutes; Intraocular pressure reduction: 1 hour

Peak effect: 0.5 to 1 hour

Duration of Action

Miosis: 4 to 8 hours; Intraocular pressure reduction: 4 to 12 hours

Use: Labeled Indications

Elevated intraocular pressure: Reduction of elevated intraocular pressure (IOP) in patients with open-angle glaucoma or ocular hypertension or as part of a 4-drug medical management regimen in acute angle-closure glaucoma when the patient cannot be seen by an ophthalmologist for ≥1 hour (off-label use) (Pokhrel 2007).

Miosis: Induction of miosis

Prevention of postoperative elevated IOP: Prevention of postoperative elevated IOP associated with laser surgery

Contraindications

US labeling: There are no contraindications listed in the manufacturer's labeling.

Canadian labeling: Hypersensitivity to pilocarpine or any component of the formulation; conditions where pupillary constriction is undesirable (eg, acute iritis, anterior uveitis)

Dosing: Adult

Elevated intraocular pressure: Ophthalmic:

Open-angle glaucoma or ocular hypertension: Instill 1 drop of 1%, 2%, or 4% solution into the affected eye(s) up to 4 times daily; initiate pilocarpine-naive patients on the 1% concentration. Note: Strength of solution and frequency of instillation dependent on degree of pressure elevation and patient miotic response.

Angle-closure glaucoma, acute: Instill 1 drop of 2% solution into the affected eye as part of a 4-drug regimen; may repeat in 30 to 60 minutes if intraocular pressure remains elevated (eg, >40 mm Hg). Note: Reserve medical management for emergency situations when an assessment by an ophthalmologist will be delayed by ≥1 hour (Pokhrel 2007).

Miosis: Ophthalmic: Instill 1 drop (or 2 drops 5 minutes apart) of 1%, 2%, or 4% solution into the affected eye(s).

Prevention of postoperative elevated intraocular pressure: Ophthalmic: Instill 1 drop (or 2 drops 5 minutes apart) of 1%, 2%, or 4% solution into the affected eye(s) 15 to 60 minutes prior to surgery.

Dosing: Geriatric

Refer to adult dosing.

Dosing: Pediatric

Glaucoma, open-angle; elevated intraocular pressure:

Infants and Children <2 years: Ophthalmic: 1% Solution: Instill 1 drop into the affected eye(s) 3 times daily

Children ≥2 years and Adolescents: Note: Strength of solution and frequency of instillation dependent on degree of pressure elevation and patient miotic response; individualize therapy. Ophthalmic: 1%, 2%, or 4% solution: Instill one drop into the affected eye(s) up to 4 times daily; for pilocarpine-naive patients, initiate therapy with the 1% concentration

Glaucoma, acute angle closure:

Infants and Children <2 years: Ophthalmic: 1% solution: Instill 1 drop into the affected eye(s) 3 times daily

Children ≥2 years and Adolescents: Ophthalmic: 1% or 2% solution: Initial: Instill 1 drop into the affected eye(s) up to 3 times over a 30-minute period; pretreatment with secretory suppressant and hyperosmotic agent may be required to lower IOP below 50 mm Hg and relieve iris ischemia. If laser iridoplasty or iridomy required to break the attack, instill 1 drop of 4% solution prior to the procedure; following laser iridoplasty, instill 1 drop of 1% solution 4 times daily until an iridotomy can be performed.

Miosis induction; prior to goiniotomy or trabeculectomy:

Infants and Children: Ophthalmic: 1% or 2% solution: Instill 1 drop into the eye(s) 15 to 60 minutes prior to surgery

Adolescents: Ophthalmic: 1%, 2%, or 4% solution: Instill 1 or 2 drops (5 minutes apart) into the affected eye(s)

Administration

Ophthalmic: Gently apply finger pressure to the lacrimal sac for 2 minutes following administration. Remove contact lenses prior to instillation and wait 10 to 15 minutes before reinserting. In most cases, separate administration of other ophthalmic agents by at least 5 minutes. When treating acute angle-closure glaucoma, separate administration of other ophthalmic agents by ≥1 minute (Pokhrel 2007; Weizer 2019). Do not touch the tip of the dropper to the eye, fingertips, or other surface.

Storage

Store at 15°C to 25°C (59°F to 77°F). Protect from freezing.

Drug Interactions

Acetylcholinesterase Inhibitors: May enhance the adverse/toxic effect of Cholinergic Agonists. Specifically, cholinergic effects may be enhanced or increased. Monitor therapy

Beta-Blockers: May enhance the adverse/toxic effect of Cholinergic Agonists. Of particular concern are the potential for cardiac conduction abnormalities and bronchoconstriction. Monitor therapy

Cyclopentolate: May diminish the therapeutic effect of Pilocarpine (Ophthalmic). Monitor therapy

Sincalide: Drugs that Affect Gallbladder Function may diminish the therapeutic effect of Sincalide. Management: Consider discontinuing drugs that may affect gallbladder motility prior to the use of sincalide to stimulate gallbladder contraction. Consider therapy modification

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.

Frequency not defined.

Cardiovascular: Hypertension, tachycardia

Gastrointestinal: Diarrhea, nausea, salivation, vomiting

Ocular: Burning, ciliary spasm, conjunctival vascular congestion, corneal granularity (gel 10%), lacrimation, lens opacity, myopia, retinal detachment, supraorbital or temporal headache, visual acuity decreased

Respiratory: Bronchial spasm, pulmonary edema

Miscellaneous: Diaphoresis

Warnings/Precautions

Concerns related to adverse effects:

• Ophthalmic effects: Use caution when driving at night and other hazardous occupations in poor illumination; may cause decreased visual acuity, especially at night or with reduced lighting. In addition, miotics may also cause accommodative spasm.

Disease-related concerns:

• Asthma: Use with caution in patients with asthma.

• Cardiovascular disease: Use with caution in patients with acute heart failure, recent myocardial infarction (MI), hypertension and/or hypotension. In a scientific statement from the American Heart Association, ophthalmic cholinergic agents have been determined to be agents that may exacerbate underlying myocardial dysfunction (magnitude: minor) (AHA [Page 2016]).

• GI disease: Use with caution in patients with peptic ulcer disease or GI spasm.

• Hyperthyroidism: Use with caution in patients with hyperthyroidism.

• Ocular inflammation: Use is not recommended when iritis is present. Avoid miotics in acute inflammatory diseases of the anterior chamber.

• Parkinson disease: Use with caution in patients with Parkinson disease.

• Retinal disease: Rare cases of retinal detachment have been reported; use with caution in susceptible patients and those with preexisting retinal disease; a thorough examination of retina (including funduscopy) is recommended prior to initiation of therapy.

• Urinary tract obstruction: Use with caution in patients with urinary tract obstruction.

Special populations:

• Pediatric: Use with caution in pediatric patients with primary congenital glaucoma for control of IOP; cases of paradoxical increase in IOP have been reported. Use is not recommended in pediatric patients diagnosed with glaucoma secondary to anterior segment dysgenesis or uveitis (especially if uveitis is active).

Other warnings/precautions:

• Contact lens wearers: May contains benzalkonium chloride which may be adsorbed and cause discoloration of soft contact lenses; remove contacts prior to administration and wait 10 to 15 minutes before reinserting.

Monitoring Parameters

Intraocular pressure (30 to 60 minutes after administration for acute angle-closure glaucoma (Pokhrel 2007), funduscopic exam (before therapy initiation), visual field testing

Pregnancy Risk Factor

C

Pregnancy Considerations

Animal reproduction studies have not been conducted.

Patient Education

What is this drug used for?

• It is used to treat glaucoma.

• It is used to lower high eye pressure.

• It may be given to you for other reasons. Talk with the doctor.

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

• Tearing

• Burning

• Blurred vision

• Decreased night vision

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Headache

• Vision changes

• Eye pain

• Severe eye irritation

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.

Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.

Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a limited summary of general information about the medicine's uses from the patient education leaflet and is not intended to be comprehensive. This limited summary does NOT include all information available about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not intended to provide medical advice, diagnosis or treatment and does not replace information you receive from the healthcare provider. For a more detailed summary of information about the risks and benefits of using this medicine, please speak with your healthcare provider and review the entire patient education leaflet.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.