Version May 2024
Elevated intraocular pressure: Ophthalmic:
Open-angle glaucoma or ocular hypertension: 1%, 2%, 4% solution: Instill 1 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.
Angle-closure glaucoma, acute: 2% solution: Instill 1 drop 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 (Ref).
Miosis: Ophthalmic: 1%, 2%, 4% solution: Instill 1 drop (or 2 drops 5 minutes apart) into the affected eye(s).
Presbyopia: Ophthalmic: 1.25% solution: Instill 1 drop into each eye once daily; 1 additional drop may be instilled into each eye 3 to 6 hours after the first dose.
Prevention of postoperative elevated intraocular pressure: Ophthalmic: 1%, 2%, 4% solution: Instill 1 drop (or 2 drops 5 minutes apart) into the affected eye(s) 15 to 60 minutes prior to surgery.
There are no dosage adjustments provided in the manufacturer's labeling.
There are no dosage adjustments provided in the manufacturer's labeling.
Refer to adult dosing.
(For additional information see "Pilocarpine (ophthalmic): Pediatric drug information")
Glaucoma, open-angle; reduction of elevated intraocular pressure (IOP):
Infants and Children <2 years: 1% solution: Ophthalmic: Instill 1 drop into the affected eye(s) 3 times daily.
Children ≥2 years and Adolescents: 1%, 2%, or 4% solution: Ophthalmic: Instill 1 drop into the affected eye(s) up to 4 times daily. Note: Strength of solution and frequency of instillation dependent on degree of pressure elevation and patient miotic response; individualize therapy; for pilocarpine-naive patients, initiate therapy with the 1% concentration.
Glaucoma, acute angle closure:
Infants and Children <2 years: 1% solution: Ophthalmic: Instill 1 drop into the affected eye(s) 3 times daily.
Children ≥2 years and Adolescents: 1% or 2% solution: Ophthalmic: 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 iridotomy 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 goniotomy or trabeculectomy:
Infants, Children, and Adolescents: 1% or 2% solution: Ophthalmic: Instill 1 drop into the eye(s) 15 to 60 minutes prior to surgery.
There are no dosage adjustments provided in the manufacturer's labeling.
There are no dosage adjustments provided in the manufacturer's labeling.
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Adverse reactions reported in adults.
1% to 10%:
Nervous system: Headache
Ophthalmic: Accommodation disturbance, blurred vision, conjunctival hyperemia, eye irritation, eye pain, increased lacrimation, supraorbital pain, visual impairment (including dim, dark, or jumping vision), vitreous opacity
Postmarketing: Ophthalmic: Retinal detachment, retinal hole without detachment, vitreous detachment, vitreous traction
Isopto Carpine: There are no contraindications listed in the US 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).
Vuity: Hypersensitivity to pilocarpine or any component of the formulation.
Concerns related to adverse effects:
• Ophthalmic effects: Miotics may cause accommodative spasm, as well as temporary dim or dark vision. Do not drive if vision is not clear; use caution when driving at night and other hazardous activities in poor illumination.
Disease-related concerns:
• Cardiovascular disease: 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]).
• Ocular inflammation: Use is not recommended when iritis is present. Avoid miotics in acute inflammatory diseases of the anterior chamber.
• Retinal disease: Rare cases of retinal detachment and retinal tear have been reported; patients with preexisting retinal disease are at increased risk. Sudden onset of flashing lights, floaters, or vision loss should be reported immediately.
Special populations:
• Pediatric: Use with caution in pediatric patients with primary congenital glaucoma for control of intraocular pressure (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 contain benzalkonium chloride, which may be adsorbed and cause discoloration of soft contact lenses; remove contacts prior to administration and wait 10 minutes before reinserting.
Qlosi 0.4% ophthalmic solution: FDA approved October 2023; availability anticipated in the first half of 2024. Information pertaining to this product within the monograph is pending revision. Qlosi is indicated for the treatment of presbyopia in adults. Consult the prescribing information for additional information.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Solution, Ophthalmic, as hydrochloride:
Isopto Carpine: 1% (15 mL [DSC]); 2% (15 mL [DSC]); 4% (15 mL [DSC])
Vuity: 1.25% (2.5 mL, 5 mL) [contains benzalkonium chloride]
Generic: 1% (15 mL); 2% (15 mL); 4% (15 mL)
Yes
Solution (Pilocarpine HCl Ophthalmic)
1% (per mL): $6.18 - $6.57
2% (per mL): $6.32 - $6.72
4% (per mL): $6.63 - $7.05
Solution (Vuity Ophthalmic)
1.25% (per mL): $37.04
Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Solution, Ophthalmic, as hydrochloride:
Isopto Carpine: 2% (15 mL); 4% ([DSC]) [contains benzalkonium chloride]
Generic: 1% ([DSC]); 2% ([DSC]); 4% ([DSC])
Solution, Ophthalmic, as nitrate:
Generic: 2% (0.3 mL)
Ophthalmic: Gently apply finger pressure to the lacrimal sac for 2 minutes following administration. Remove contact lenses prior to instillation and wait 10 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 (Ref). Do not touch the tip of the dropper to the eye, fingertips, or other surface.
Ophthalmic: For ophthalmic use only. Solution: Instill into affected eye(s); apply finger pressure to lacrimal sac for 2 minutes after instillation to decrease drainage into the nose and throat and minimize possible systemic absorption (Ref). Remove contact lenses prior to instillation and wait ≥10 minutes before reinserting. Separate administration of other ophthalmic agents by ≥5 minutes. Do not touch the tip of the dropper to the eye, fingertips, or other surface.
Elevated intraocular pressure (1%, 2%, 4% solution): 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 (1%, 2%, 4% solution): Induction of miosis.
Presbyopia (1.25% solution): Treatment of presbyopia in adults.
Prevention of postoperative elevated IOP (1%, 2%, 4% solution): Prevention of postoperative elevated IOP associated with laser surgery.
Isopto Carpine may be confused with Isopto Carbachol
None known.
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.
Cyclopentolate: May diminish the therapeutic effect of Pilocarpine (Ophthalmic). Risk C: Monitor therapy
Tropicamide: May diminish the therapeutic effect of Pilocarpine (Ophthalmic). Risk C: Monitor therapy
Animal reproduction studies have not been conducted.
It is not known if pilocarpine (ophthalmic) is excreted in breast milk. The manufacturer recommends that caution be exercised when administering pilocarpine (ophthalmic) to nursing women.
Intraocular pressure (30 to 60 minutes after administration for acute angle-closure glaucoma (Pokhrel 2007), funduscopic exam (before therapy initiation), visual field testing
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.
Duration: Miosis: 4 to 8 hours; Intraocular pressure reduction: 4 to 14 hours.
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