Pilopine HS

Last updated on RxList: 8/28/2008

Drug Summary

Last reviewed on RxList 4/21/2016

Pilopine HS (pilocarpine hydrochloride) Ophthalmic Gel 4% is a cholinergic agent that works by decreasing the amount of fluid within the eye used to treat glaucoma or ocular hypertension (high pressure inside the eye). Common side effects of Pilopine HS include:

  • temporary irritation/burning/stinging/discomfort of the eye
  • temporary blurred vision
  • poor vision in dim or dark light
  • headache, or
  • brow ache

The recommended dose of Pilopine HS is to apply a one-half inch ribbon in the lower conjunctival sac of the affected eye(s) once a day at bedtime. Other drugs may interact with Pilopine HS. Tell your doctor all medications and supplements you use. During pregnancy, Pilopine HS should be used only when prescribed. It is unknown if this medication passes into breast milk. Consult your doctor before breastfeeding.

Our Pilopine HS (pilocarpine hydrochloride) Side Effects Drug Center provides a comprehensive view of available drug information on the potential side effects when taking this medication.

Drug Description

PILOPINE HS® (pilocarpine hydrochloride ophthalmic gel) 4% is a sterile topical ophthalmic aqueous gel which contains more than 90% water and employs carbopol 940, a synthetic high molecular weight cross-linked polymer of acrylic acid, to impart a high viscosity. The active ingredient, pilocarpine hydrochloride, is a cholinergic agent and is represented by the chemical structure:

PILOPINE HS® (pilocarpine hydrochloride) Structural Formula Illustration

Established name: Pilocarpine Hydrochloride

Chemical name: 2(3H)-Furanone, 3-ethyldihydro-4-[(1-methyl-1H-imidazol-5-yl)-methyl]-, monohydrochloride, (3S-cis)-.

PILOPINE HS® (pilocarpine hydrochloride ophthalmic gel) 4% - Each Gram Contains: Active: pilocarpine hydrochloride 4% (40 mg). Preservative: benzalkonium chloride 0.008%. Inactives: carbopol 940, edetate disodium, hydrochloric acid and/or sodium hydroxide (to adjust pH) and purified water.

Indications & Dosage


PILOPINE HS® (pilocarpine hydrochloride ophthalmic gel) 4% is a miotic (parasympathomimetic) used to control intraocular pressure. It may be used in combination with other miotics, beta-blockers, carbonic anhydrase inhibitors, sympathomimetics or hyperosmotic agents.


Apply a one-half inch ribbon in the lower conjunctival sac of the affected eye(s) once a day at bedtime.


PILOPINE HS® (pilocarpine hydrochloride ophthalmic gel) 4% is supplied as a 4% sterile aqueous gel in 4 gram tubes with ophthalmic tip.

4 gram: NDC 0065-0215-35


Store at room temperature 2°-27°C (36° - 80° F). Avoid excessive heat. Do not freeze.

Rev: October 2007. ALCON LABORATORIES, INC. Fort Worth, Texas 76134, USA. FDA rev date: 04/17/08

Side Effects & Drug Interactions


The following adverse experiences associated with pilocarpine therapy have been reported: lacrimation, burning or discomfort, temporal or periorbital headache, ciliary spasm, conjunctival vascular congestion, superficial keratitis and induced myopia. Systemic reactions following topical administration are extremely rare, but occasional patients are peculiarly sensitive to develop sweating and gastrointestinal overactivity following suggested dosage and administration. Ocular reactions usually occur during initiation of therapy and often will not persist with continued therapy. Reduced visual acuity in poor illumination is frequently experienced in older individuals and in those with lens opacity. A subtle corneal granularity was observed in about 10% of patients treated with PILOPINE HS® (pilocarpine hydrochloride ophthalmic gel) . Cases of retinal detachment have been reported during treatment with miotic agents; especially in young myopic patients. Lens opacity may occur with prolonged use of pilocarpine.


No information provided.

Warnings & Precautions





The miosis usually causes difficulty in dark adaptation. Patient should be advised to exercise caution in night driving and other hazardous occupations in poor illumination.

Information For Patients

Do not touch tube tip to any surface, as this may contaminate the gel.

Carcinogenesis, Mutagenesis, Impairment of Fertility

There have been no long-term studies done using pilocarpine hydrochloride in animals to evaluate carcinogenic potential.

Pregnancy: Category C.

Animal reproduction studies have not been conducted with pilocarpine hydrochloride. It is also not known whether pilocarpine hydrochloride can cause fetal harm when administered to a pregnant woman or can affect reproduction capacity. PILOPINE HS® (pilocarpine hydrochloride ophthalmic gel) should be given to a pregnant woman only if clearly needed.

Nursing Mothers

It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when pilocarpine hydrochloride is administered to a nursing woman.

Pediatric Use

Safety and effectiveness in pediatric patients have not been established.

Geriatric Use

No overall differences in safety or effectiveness have been observed between elderly and younger patients.

Overdose & Contraindications


Overdosage can produce sweating, salivation, nausea, tremors, and slowing of the pulse and a decrease in blood pressure. Bronchial constriction may develop in asthmatic patients. In moderate overdosage, spontaneous recovery is to be expected and is aided by intravenous fluids to compensate for dehydration. For cases demonstrating severe poisoning, atropine is the pharmacologic antagonist to pilocarpine.

A topical ocular overdose of an ophthalmic product containing pilocarpine hydrochloride may be flushed from the eye(s) with warm tap water.


Miotics are contraindicated where constriction is undesirable, such as in acute iritis, and in those persons showing hypersensitivity to any of their components.

Clinical Pharmacology


Pilocarpine (pilocarpine hydrochloride ophthalmic gel) 4% is a direct acting cholinergic parasympathomimetic agent which acts through direct stimulation of muscarinic neuro receptors and smooth muscle such as the iris and secretory glands. Pilocarpine produces miosis through contraction of the iris sphincter, causing increased tension on the scleral spur and opening of the trabecular meshwork spaces to facilitate outflow of aqueous humor. Outflow resistance is thereby reduced, lowering intraocular pressure.

Medication Guide


How to use PILOPINE HS® (pilocarpine hydrochloride ophthalmic gel) 4%


PILOPINE HS® (pilocarpine hydrochloride ophthalmic gel) 4% is an eye pressure lowering medication. The pilocarpine is absorbed into the eye at night to control intraocular pressure throughout the day. Apply about a half-inch ribbon (try not to put in too much) in the affected eye(s) every night just before going to bed. Should you occasionally apply too much and awaken with some gel on the eyelids, simply wash it away with warm water. You may initially experience some difficulty applying the gel or mild pilocarpine symptoms such as blurred vision in the morning. This is normal and you should soon become accustomed to both. If discomfort persists, consult your ophthalmologist. If you use other glaucoma medication at bedtime, use the drops first and wait at least five minutes before applying PILOPINE HS® (pilocarpine hydrochloride ophthalmic gel) .

How to use PILOPINE HS - illustration 1

Wash and dry your hands. Remove cap from the tube and place it on a clean surface nearby. Gently pull down the lower eyelid to form a pocket for the gel.

How to use PILOPINE HS - illustration 2

Gently squeeze tube and apply a continuous strip (about a half-inch) of gel into and along the pocket. A half-inch is approximately as wide as your iris (the colored part of your eye).

How to use PILOPINE HS - illustration 3

Gently grasp lower eyelid below lashes; lift lower eyelid and look downward as you close your eye. This will help move the gel deep into the pocket you have formed.

How to use PILOPINE HS - illustration 4

Keep eye closed for a minute or so to prevent excess blinking or tearing which might dilute the medication. Repeat the procedure for your other eye. Replace cap. Shown below is another approach you can use if your ophthalmologist recommends working up to the full daily dosage.


Start with a small amount of gel. As you become more familiar with the technique, you will be able to apply larger strips until you reach the half-inch maximum dose. Do not use too much gel. Individual situations vary, so be sure to follow your ophthalmologist's recommendations.

Easy Fingertip Application - illustration 1

Wash hands thoroughly. Apply the correct amount of Pilopine HS® (pilocarpine hydrochloride ophthalmic gel) to the edge of your index finger.

Easy Fingertip Application - illustration 2

Pull down lower eyelid with middle finger of other hand to form a pouch. Gently roll the strip of gel into the eye pouch.

Easy Fingertip Application - illustration 3

Gently squeeze the lower eyelid and pull it slightly away from your face.

Easy Fingertip Application - illustration 4

Look down and then close your eye for a moment. Wipe off any excess gel with a tissue. Repeat in the other eye if so directed by your ophthalmologist. Replace cap.

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