Pilocarpine

Pharmacologic Category

Ophthalmic Agent, Antiglaucoma; Ophthalmic Agent, Miotic

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.

* See Dosage and Administration in AHFS Essentials for additional information.

Dosing: Geriatric

Refer to adult dosing.

Dosing: Renal Impairment: Adult

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

Dosing: Hepatic Impairment: Adult

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

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)

Dosing: Renal Impairment: Pediatric

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

Dosing: Hepatic Impairment: Pediatric

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

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

* See Uses in AHFS Essentials for additional information.

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.

Administration: Pediatric

For ophthalmic use. Solution: Shake well before use; 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 (Urtti 1993; Zimmerman 1982). 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/Stability

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

Medication Patient Education with HCAHPS Considerations

• 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.

Medication Safety Issues

Sound-alike/look-alike issues:

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)

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.

* See Cautions in AHFS Essentials for additional information.

Geriatric Considerations

Evaluate the patient's or caregiver's ability to safely administer the correct dose of ophthalmic medication.

Pregnancy Risk Factor

C

Pregnancy Considerations

Animal reproduction studies have not been conducted.

Breast-Feeding Considerations

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.

Briggs' Drugs in Pregnancy & Lactation

• Pilocarpine Ophthalmic

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

* See Cautions in AHFS Essentials for additional information.

Metabolism/Transport Effects

None known.

Drug Interactions Open Interactions

Acetylcholinesterase Inhibitors: May enhance the adverse/toxic effect of Cholinergic Agonists. Risk C: 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. Risk C: Monitor therapy

Cyclopentolate: May diminish the therapeutic effect of Pilocarpine (Ophthalmic). Risk C: 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. Risk D: Consider therapy modification

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

Advanced Practitioners Physical Assessment/Monitoring

Assess results of intraocular pressure testing, fundoscopic exam, and visual field testing on a periodic basis. Teach patient appropriate administration.

Nursing Physical Assessment/Monitoring

Monitor results of intraocular pressure testing and visual field testing on a periodic basis. Teach patient appropriate administration.

Dosage Forms: US

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)

Dosage Forms: Canada

Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Solution, Ophthalmic, as hydrochloride:

Isopto Carpine: 1% ([DSC]); 2% (15 mL); 4% (15 mL) [contains benzalkonium chloride]

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

Anatomic Therapeutic Chemical (ATC) Classification

• S01EB01

Generic Available (US)

Yes

Pricing: US

Solution (Isopto Carpine Ophthalmic)

1% (per mL): $7.44

2% (per mL): $7.61

4% (per mL): $7.98

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

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.

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)

Pharmacodynamics/Kinetics

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

Peak effect: 0.5 to 1 hour

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

Local Anesthetic/Vasoconstrictor Precautions

No information available to require special precautions

Effects on Dental Treatment

No significant effects or complications reported

Effects on Bleeding

No information available to require special precautions

Index Terms

Pilocarpine HCl; Pilocarpine Hydrochloride

FDA Approval Date

July 29, 1974

References

Isopto Carpine (pilocarpine hydrochloride) [prescribing information]. Fort Worth, TX: Alcon Laboratories; June 2010.

Isopto Carpine (pilocarpine hydrochloride) [product monograph]. Dorval, Quebec, Canada: Novartis Pharmaceuticals Canada Inc; February 2017.

Krawitz PL, Podos SM. Use of apraclonidine in the treatment of acute angle closure glaucoma. Arch Ophthalmol. 1990;108(9):1208-1209.[PubMed 2205180]

Page RL 2nd, O'Bryant CL, Cheng D, et al; American Heart Association Clinical Pharmacology and Heart Failure and Transplantation Committees of the Council on Clinical Cardiology; Council on Cardiovascular Surgery and Anesthesia; Council on Cardiovascular and Stroke Nursing; and Council on Quality of Care and Outcomes Research. Drugs That May Cause or Exacerbate Heart Failure: A Scientific Statement From the American Heart Association [published correction appears in Circulation. 2016;134(12):e261]. Circulation. 2016;134(6):e32-e69.[PubMed 27400984]

Pokhrel PK, Loftus SA. Ocular emergencies [published correction appears in: Am Fam Physician. 2008;77(7):920]. Am Fam Physician. 2007;76(6):829-836.[PubMed 27400984]

Urtti A, Salminen L. Minimizing systemic absorption of topically administered ophthalmic drugs. Surv Ophthalmol. 1993;37(6):435-456.[PubMed 8100087]

Weizer JS. Angle-closure glaucoma. Post TW, ed. UpToDate. Waltham, MA: UpToDate Inc. http://www.uptodate.com. Accessed February 4, 2019.

Zimmerman TJ, Kooner KS, Kandarakis AS, Ziegler LP. Improving the therapeutic index of topically applied ocular drugs. Arch Ophthalmol. 1984;102(4):551-553.[PubMed 6704011]

Brand Names: International

Apicarpine (JO, QA); Asthenopin (PH); Carpine (BD); Isopto Carpina (AR, CO, ES, PE, PY, UY, VE); Isopto Carpine (AE, AU, BB, BF, BJ, CI, CY, EE, EG, ET, FI, GH, GM, GN, GR, HK, HN, IE, IQ, IR, IS, JO, KE, KW, LB, LK, LR, LU, LY, MA, ML, MR, MU, MW, NE, NG, NL, OM, PH, PL, SA, SC, SD, SG, SL, SN, SY, TH, TN, TW, TZ, UG, YE, ZM, ZW); Isopto Pilocarpina (CL); Isopto Pilocarpine (FR); Isopto-Carpine (VN); Liocarpina (IT); Locarp (IN); Medicarpine (PK); Miokar (ID); O.P.D. (TW); Ocu-Carpine (KR); Ocucarpine (EG); Ocusert Pilo-20 (GB); Ocusert Pilo-40 (GB); Ocusert Pilocarpine (GB); Oftan-Pilocarpin (FI); P.V. Carpine Liquifilm Ophthalimic Solution (AU, NZ); Pil Ofteno (GT, SV); Pilo (FR); Pilocan (BR); Pilocar (VE); Pilocarpol (DE); Pilogel (GB, IE, TW); Pilogel HS (CL, CZ, SG, SI); Pilokarpin (DK, SI, SK); Pilomann (DE); Pilomin (BD, BG); Pilopes (BD); Pilopine-HS (AE, BF, BJ, CI, CY, ET, GH, GM, GN, IQ, IR, JO, KE, KW, LB, LR, LY, MA, ML, MR, MU, MW, NE, NG, OM, SA, SC, SD, SL, SN, SY, TN, TZ, UG, YE, ZM, ZW); Pilopos (CZ); Pilopt Eye Drops (AU, NZ); Pilotina (QA); Pilotonina (IT); Sno Pilo (AE, IE); Spersacarpin (DE); Spersacarpine (CH, MY, PK, SE, TW); Zhenrui (CN)

Last Updated 2/10/20