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Pilocarpine (Ophthalmic)

Pronunciation

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.

Gel, Ophthalmic, as hydrochloride:

Pilopine HS: 4% (4 g) [contains benzalkonium chloride, edetate disodium]

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
  • Pilopine HS

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

US labeling:

Elevated intraocular pressure: Reduction of elevated intraocular pressure (IOP) in patients with open-angle glaucoma or ocular hypertension

Glaucoma: Management of acute angle-closure glaucoma

Miosis: Induction of miosis

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

Canadian labeling: Elevated intraocular pressure: Reduction of IOP.

Use: Unlabeled

Counter effects of cycloplegics

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

US labeling:

Elevated intraocular pressure: Ophthalmic: Instill one drop 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

Glaucoma (acute angle closure): Ophthalmic: Initial: Instill 1 drop of 1% or 2% solution 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 pressure below 50 mm Hg and relieve iris ischemia. If laser iridoplasty or iridomy is used 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: Ophthalmic: Instill 1 drop (or 2 drops 5 minutes apart) into the affected eye(s)

Prevention of postoperative elevated IOP: Ophthalmic: Instill 1 drop (or 2 drops 5 minutes apart) into the affected eye(s) 15 to 60 minutes prior to surgery

Canadian labeling: Elevated intraocular pressure: Instill 2 drops into the affected eye(s) 3 or 4 times daily

To counteract the mydriatic effects of sympathomimetic agents (off-label use): Ophthalmic: Solution: Instill 1 drop of a 1% solution in the affected eye.

Dosing: Geriatric

Refer to adult dosing.

Dosing: Pediatric

Elevated intraocular pressure: Ophthalmic:

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

Children ≥2 years and Adolescents: Refer to adult dosing

Glaucoma (acute angle closure): Ophthalmic:

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

Children ≥2 years and Adolescents: Refer to adult dosing

Miosis: Ophthalmic: Infants, Children, and Adolescents: For induction of miosis prior to goniotomy or trabeculectomy, instill 1 drop of 1% or 2% solution into the eye(s) 15 to 60 minutes prior to surgery

Dosing: Renal Impairment

There are no dosage adjustments provided in the manufacturer’s labeling.

Dosing: Hepatic Impairment

There are no dosage adjustments provided in the manufacturer’s labeling.

Administration

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. Separate administration of other ophthalmic agents by at least 5 minutes. 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. 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. Management: Administer these agents in combination with caution, and monitor for conduction disturbances. Avoid methacholine with any beta blocker due to the potential for additive bronchoconstriction. Monitor therapy

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

Adverse Reactions

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.

• 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; the Canadian labeling contraindicates use in patients with acute iritis and anterior uveitis.

• 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:

• Geriatrics (>65 years of age): Elderly patients may be at a higher risk for pilocarpine-induced mental status changes, including psychosis and dementia of the Alzheimer type (Canadian labeling).

• 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, funduscopic exam (before therapy initiation), visual field testing

Pregnancy Risk Factor

C

Pregnancy Considerations

Animal reproduction studies have not been conducted.

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience tearing, burning, blurred vision or decreased night vision. Have patient report immediately to prescriber headache, vision changes, eye pain, or severe eye irritation (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.

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