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)
Pharmacology
Mechanism of Action
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)
Pharmacokinetics/Pharmacodynamics
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; Weizer 2019).
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)
Dosage and Administration
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; Weizer 2019).
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. 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
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; Weizer 2019), funduscopic exam (before therapy initiation), visual field testing
Pregnancy
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.
