Introduction

Miotic; direct-acting parasympathomimetic agent.

Uses for Pilocarpine, Pilocarpine Hydrochloride, Pilocarpine Nitrate

Open-angle Glaucoma

Reduction of elevated intraocular pressure (IOP) in patients with primary open-angle (chronic simple, noncongestive) glaucoma.

May use concomitantly with other miotics, sympathomimetic agents, β-adrenergic blocking agents, carbonic anhydrase inhibitors, or hyperosmotic agents.

Angle-closure Glaucoma

Reduction of IOP in the emergency treatment of acute (congestive) angle-closure glaucoma prior to surgery. Because it may preclude successful surgery, do not use for long periods prior to surgical treatment.

Lack of response may be caused by paralysis of the iris sphincter by the extremely high IOP; systemic administration of acetazolamide or hyperosmotic solutions (e.g., glycerin or mannitol) may be required.

Ocular Surgery

Reduction of IOP and protection of the lens by causing miosis prior to goniotomy or iridectomy, including laser iridectomy.

May use to control glaucoma which persists after surgery.

Ophthalmologic Examinations

Production of miosis to counteract mydriatic effects of sympathomimetic agents (e.g., phenylephrine) after ophthalmoscopic examinations in glaucoma patients.

Pilocarpine, Pilocarpine Hydrochloride, Pilocarpine Nitrate Dosage and Administration

Administration

Ophthalmic Administration

Avoid contamination of the solution or gel container.

Ophthalmic solutions are preferred when an acute reduction in IOP and/or an intense miotic effect are necessary (e.g., prior to surgery, following ophthalmologic examinations).

Tonometric measurements recommended before and during therapy.

Ophthalmic Solution

Apply topically to the conjunctival sac of affected eye(s) as directed by clinician, usually 3–4 times daily; more frequent administration may be necessary in some patients. Not for injection.

Following topical instillation, apply finger pressure on the lacrimal sac for 1–2 minutes to minimize drainage into nose and throat and reduce risk of absorption and systemic reactions. Remove excess solution around the eye with a tissue and rinse off any medication on hands immediately.

Ophthalmic Gel

Apply topically to the lower conjunctival sac of affected eye(s) once daily at bedtime.

Measure IOP just before next dose following initiation of therapy to ensure adequate control of IOP throughout the 24-hour dosing interval.

If used concomitantly with ophthalmic solutions, instill solutions first and apply gel ≥5 minutes later.

Dosage

Available as pilocarpine hydrochloride; dosage expressed in terms of the salt.

Adjust concentration and frequency of solution instillation according to patient requirements and response, as determined by tonometric readings.

In patients with heavily pigmented irides, higher solution concentrations may be required.

Adjust dosage of ophthalmic gel based on periodic tonometric readings.

Adults

Open-Angle Glaucoma

Ophthalmic

1–2 drops of a 1–4% solution in the eye(s) every 4–12 hours. Solution concentrations >4% are only occasionally more effective than lower concentrations.

Apply a 1.3-cm (0.5-inch) ribbon of a 4% gel into lower conjunctival sac once daily at bedtime.

Acute Angle-Closure Glaucoma

Ophthalmic

1 drop of a 2% solution in the affected eye every 5–10 minutes for 3–6 doses, followed by 1 drop every 1–3 hours until pressure is controlled. To prevent a bilateral attack, 1 drop of a 1–2% solution in the unaffected eye every 6–8 hours.

Ocular Surgery

Iridectomy

1 drop of a 2% solution 4 times immediately prior to iridectomy has been used.

Congenital Glaucoma (Goniotomy)

1 drop of a 2% solution every 6 hours prior to surgery has been used.

May use a 2% solution to fill the gonioscopic lens prior to goniotomy, or may administer 1 drop of a 2% solution every 6 hours plus 3 times in the 30 minutes immediately preceding goniotomy, with or without concomitant administration of acetazolamide.

Ophthalmologic Examinations

Ophthalmic

1 drop of a 1% solution in the affected eye(s).

Contraindications

• Known hypersensitivity to pilocarpine or any ingredient in the formulation.

• Conditions in which pupillary constriction is undesirable (e.g., acute iritis, pupillary block).

Warnings/Precautions

Sensitivity Reactions

Hypersensitivity

Allergic conjunctivitis, dermatitis, or keratitis reported occasionally with miotics; these reactions are usually alleviated by changing to another miotic. In some instances, allergic reactions may be caused by preservatives in the preparations.

General Precautions

Ocular Effects

Retinal detachment reported rarely; use with extreme caution, if at all, in patients with a history or risk of retinal detachment, especially those who are young or aphakic. Carefully examine retinal periphery at least annually to detect an impending detachment.

Use with caution in patients with corneal abrasion to avoid excessive penetration and systemic toxicity.

Possible spasm of accommodation and poor vision in dim light, particularly in geriatric patients and patients with lens opacities. (See Advice to Patients.)

Follicular conjunctival hypertrophy may occur with prolonged therapy.

Possible transient increase in IOP even when the angle is open. In some patients with angle-closure glaucoma receiving miotics, IOP may be increased and acute attacks may be precipitated.

Possible corneal opacities.

Regular slit-lamp examinations recommended; discontinue therapy, at least temporarily, if iris cysts, iritis, synechiae, or lens opacities occur.

Specific Populations

Pregnancy

Category C.

Lactation

Not known whether pilocarpine is distributed into milk. Use with caution.

Pediatric Use

Safety and efficacy not established.

Geriatric Use

Reduced visual acuity in dim light frequently experienced in geriatric patients.

Common Adverse Effects

Ocular irritation (burning or discomfort), lacrimation, temporal or periorbital headache, painful ciliary or accommodative spasm, blurred vision or myopia, conjunctival vascular congestion, superficial keratitis, poor vision in dim light.

Administration

Ophthalmic Administration

Avoid contamination of the solution or gel container.

Ophthalmic solutions are preferred when an acute reduction in IOP and/or an intense miotic effect are necessary (e.g., prior to surgery, following ophthalmologic examinations).

Tonometric measurements recommended before and during therapy.

Ophthalmic Solution

Apply topically to the conjunctival sac of affected eye(s) as directed by clinician, usually 3–4 times daily; more frequent administration may be necessary in some patients. Not for injection.

Following topical instillation, apply finger pressure on the lacrimal sac for 1–2 minutes to minimize drainage into nose and throat and reduce risk of absorption and systemic reactions. Remove excess solution around the eye with a tissue and rinse off any medication on hands immediately.

Ophthalmic Gel

Apply topically to the lower conjunctival sac of affected eye(s) once daily at bedtime.

Measure IOP just before next dose following initiation of therapy to ensure adequate control of IOP throughout the 24-hour dosing interval.

If used concomitantly with ophthalmic solutions, instill solutions first and apply gel ≥5 minutes later.

Dosage

Available as pilocarpine hydrochloride; dosage expressed in terms of the salt.

Adjust concentration and frequency of solution instillation according to patient requirements and response, as determined by tonometric readings.

In patients with heavily pigmented irides, higher solution concentrations may be required.

Adjust dosage of ophthalmic gel based on periodic tonometric readings.

Adults

Open-Angle Glaucoma

Ophthalmic

1–2 drops of a 1–4% solution in the eye(s) every 4–12 hours. Solution concentrations >4% are only occasionally more effective than lower concentrations.

Apply a 1.3-cm (0.5-inch) ribbon of a 4% gel into lower conjunctival sac once daily at bedtime.

Acute Angle-Closure Glaucoma

Ophthalmic

1 drop of a 2% solution in the affected eye every 5–10 minutes for 3–6 doses, followed by 1 drop every 1–3 hours until pressure is controlled. To prevent a bilateral attack, 1 drop of a 1–2% solution in the unaffected eye every 6–8 hours.

Ocular Surgery

Iridectomy

1 drop of a 2% solution 4 times immediately prior to iridectomy has been used.

Congenital Glaucoma (Goniotomy)

1 drop of a 2% solution every 6 hours prior to surgery has been used.

May use a 2% solution to fill the gonioscopic lens prior to goniotomy, or may administer 1 drop of a 2% solution every 6 hours plus 3 times in the 30 minutes immediately preceding goniotomy, with or without concomitant administration of acetazolamide.

Ophthalmologic Examinations

Ophthalmic

1 drop of a 1% solution in the affected eye(s).

Specific Drugs