AHFS DI® Essentials™ Page 1 of 7

Pilocarpine (EENT)

Introductory Information

Miotic; direct-acting parasympathomimetic agent.a, c, d, e

Class: 52:40.20 Miotics; op102 (VA primary)

Brands*: Isopto® Carpine, Pilopine HS®

*also available generically

Generic Name: Pilocarpine

CAS Number: 92-13-7

Generic Name: Pilocarpine Hydrochloride

CAS Number: 54-71-7

Generic Name: Pilocarpine Nitrate

CAS Number: 148-72-1

Uses

Open-angle Glaucoma

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

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

Angle-closure Glaucoma

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

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.b

Ocular Surgery

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

May use to control glaucoma which persists after surgery.b

Ophthalmologic Examinations

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Production of miosis to counteract mydriatic effects of sympathomimetic agents (e.g., phenylephrine)

after ophthalmoscopic examinations in glaucoma patients.b

Dosage and Administration

Administration

Ophthalmic Administration
Avoid contamination of the solution or gel container.c, d, e

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).a

Tonometric measurements recommended before and during therapy.a

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.a, c, e Not for injection.c, e

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.a Remove excess
solution around the eye with a tissue and rinse off any medication on hands immediately.a

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

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

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

Dosage

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

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

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

Adjust dosage of ophthalmic gel based on periodic tonometric readings.a

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

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

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.a To prevent a bilateral attack, 1 drop of a 1-2% solution in the
unaffected eye every 6-8 hours.a

Ocular Surgery
>Iridectomy
Ophthalmic: 1 drop of a 2% solution 4 times immediately prior to iridectomy has been used.a

>Congenital Glaucoma (Goniotomy)

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

Ophthalmologic Examinations
>Ophthalmic
1 drop of a 1% solution in the affected eye(s).a

Cautions

Contraindications

• Known hypersensitivity to pilocarpine or any ingredient in the formulation.c, d, e

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

Warnings/Precautions

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

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

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

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

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Follicular conjunctival hypertrophy may occur with prolonged therapy.b

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

Possible corneal opacities.c, d

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

Specific Populations
Pregnancy
Category C.c

Lactation
Not known whether pilocarpine is distributed into milk.c, d, e Use with caution.c, d, e

Pediatric Use
Safety and efficacy not established.d, e

Geriatric Use
Reduced visual acuity in dim light frequently experienced in geriatric patients.d, e

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.a, b, c, d, e

Interactions

Specific Drugs

Drug Interaction Comments

Ocular hypotensive Additive IOP lowering
Used to therapeutic advantageb
agents effectsb
Concomitant administration generally not recommendedb
Competitive inhibition Some clinicians recommend administration of pilocarpine
Anticholinesterase of miotic effect and at onset of long-acting anticholinesterase therapy followed
miotics presumably IOP- by gradual taper of pilocarpine so that antagonism between
lowering effect b the drugs allows full effects of the anticholinesterase to be
obtained graduallyb

Pharmacokinetics

Absorption

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Bioavailability
Penetrates cornea rapidly.b Application of ophthalmic gel results in increased corneal bioavailability
secondary to decreased elimination of pilocarpine from precorneal areas compared with a topically
applied solution.a IOP reduction and pupillary diameter are similar to values obtained following
application of a solution.a

Onset
Following topical application of a 1% solution to the conjunctival sac, miosis occurs within 10-30
minutes and is maximal within 30 minutes.a Reduction in IOP is detectable within 60 minutes and is
maximal within 75 minutes.a Spasms of accommodation begin in approximately 15 minutes.a

Duration
Following topical application of a 1% solution to the conjunctival sac, miosis usually persists 4-8 hours
or rarely up to 20 hours.a Reduced IOP persists 4-14 hours, depending on concentration of drug used.a
Spasms of accommodation persist 2-3 hours.a

Application of ophthalmic gel results in an increased duration of ocular effects compared with a
topically applied solution.a Following topical application of gel, IOP decreases for about 18-24 hours
after application.a

Distribution

Extent
Bound to serum and ocular tissues.b

Not known whether pilocarpine is distributed into milk.c, d, e

Elimination

Metabolism
Mechanism by which pilocarpine is inactivated in the body is unclear.b

Stability

Storage

Ophthalmic
Solution
8-27°C,c unless otherwise specified by manufacturer.

Gel
2-27°C.d Avoid excessive heat; do not freeze.d

Actions

• Directly stimulates cholinergic receptors, resulting in muscarinic and nicotinic effects.b, c

• Contracts the iris sphincter and the ciliary muscle, which produces constriction of the pupil (miosis)
and spasm of accommodation, respectively.b, c, e

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• Reduces IOP in normal and glaucomatous eyes.b, c

• Facilitates aqueous humor outflow by contracting the ciliary muscle and widening the trabecular
meshwork.b, c
• Decreases activity of extraocular muscles of convergence and causes vasodilation of blood vessels of
the conjunctiva, iris, and ciliary body and increased permeability of the blood-aqueous barrier, which
may lead to vascular congestion and ocular inflammation.b

Advice to Patients

• Importance of learning and adhering to proper administration techniques to avoid contamination of the
solution or gel container.b
• Importance of removing soft contact lenses before administration (since pilocarpine may be absorbed
by or preservatives in preparations may have a deleterious effect on the lenses).b
• Caution advised if driving at night or performing hazardous tasks in dim light.c, d, e
• Importance of informing clinicians of existing or contemplated concomitant therapy, including
prescription and OTC drugs.b
• Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-
feed.b, c, d, e
• Importance of informing patients of other precautionary information.a (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some
individuals; consult specific product labeling for details.

Pilocarpine Hydrochloride
Dosage
Routes Strengths Brand Names Manufacturer
Forms
Bulk Powder

Ophthalmic Gel 4% Pilopine HS® (with benzalkonium chloride Alcon

and edetate disodium)
Pilocarpine Hydrochloride Ophthalmic
Solution 0.5%* Bausch & Lomb
Solution

1%* Isopto® Carpine (with benzalkonium Alcon

chloride)
Pilocarpine Hydrochloride Ophthalmic Akorn, Bausch &
Solution Lomb, Falcon

2%* Isopto® Carpine (with benzalkonium Alcon

chloride)
Pilocarpine Hydrochloride Ophthalmic Akorn, Bausch &
Solution Lomb, Falcon
Pilocarpine Hydrochloride Ophthalmic
3%* Bausch & Lomb
Solution

4%* Isopto® Carpine (with benzalkonium Alcon

chloride)
Pilocarpine Hydrochloride Ophthalmic Akorn, Bausch &

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Solution Lomb, Falcon

Pilocarpine Hydrochloride Ophthalmic Bausch & Lomb,
6%*
Solution Falcon
* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary)
name

Comparative Pricing

This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing
information was updated 03/2011. For the most current and up-to-date pricing information, please visit
www.drugstore.com. Actual costs to patients will vary depending on the use of specific retail or mail-
order locations and health insurance copays.

Isopto Carpine 1% Solution (ALCON VISION): 15/$36.99 or 45/$100.97

Isopto Carpine 2% Solution (ALCON VISION): 15/$36.99 or 45/$103.97

Pilocarpine HCl 1% Solution (FALCON PHARMACEUTICALS): 15/$37.99 or 30/$66.97

Pilocarpine HCl 2% Solution (FALCON PHARMACEUTICALS): 15/$37.99 or 30/$68.97

Pilopine HS 4% Gel (ALCON VISION): 4/$79.99 or 12/$225.97

References

a. AHFS Drug Information 2003. McEvoy GK, ed. Pilocarpine. Bethesda, MD: American Society of
Health-System Pharmacists; 2003:2679-82.

b. AHFS Drug Information 2003. McEvoy GK, ed. Miotics General Statement. Bethesda, MD:
American Society of Health-System Pharmacists; 2003:2674-77.

c. Falcon. Pilocarpine hydrochloride 1%, 2%, 4%, or 6% Ophthalmic Solution prescribing

information. Fort Worth, TX; 2003 Aug.

d. Alcon. Pilopine HS® (pilocarpine hydrochloride) 4% Ophthalmic Gel prescribing information. Fort
Worth, TX; 1999 Mar.

e. Alcon. Isopto® Carpine (pilocarpine hydrochloride) ophthalmic solution prescribing information.

Fort Worth, TX; 2003 Oct.

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