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:

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.

Last updated on RxList: 8/28/2008

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

Storage

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

Last updated on RxList: 8/27/2008

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®. 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.

Last updated on RxList: 8/27/2008

FOR TOPICAL OPHTHALMIC USE ONLY.

General

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® 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.

Last updated on RxList: 8/27/2008

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.

Last updated on RxList: 8/27/2008

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.

Last updated on RxList: 8/27/2008

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

PILOPINE HS® DOES NOT NEED TO BE REFRIGERATED. ENTIRE CONTENTS OF THIS TUBE MAY BE USED UP TO THE EXPIRATION DATE WHICH IS STAMPED ON THE CRIMP (BOTTOM) OF THE TUBE.

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®.

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.

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).

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.

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.

EASY "FINGERTIP" APPLICATION

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.

Wash hands thoroughly. Apply the correct amount of Pilopine HS® to the edge of your index finger.

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

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

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.

Last updated on RxList: 8/27/2008

IMPORTANT NOTE: This is a summary and does not contain all possible information about this product. For complete information about this product or your specific health needs, ask your health care professional. Always seek the advice of your health care professional if you have any questions about this product or your medical condition. This information is not intended as individual medical advice and does not substitute for the knowledge and judgment of your health care professional. This information does not contain any assurances that this product is safe, effective, or appropriate for you.

PILOCARPINE GEL - OPHTHALMIC

(pie-low-KAR-peen)

COMMON BRAND NAME(S): Pilopine HS

USES: This medication is used alone or with other medications to treat high pressure inside the eye due to glaucoma or other eye diseases (e.g., ocular hypertension). Lowering high pressure inside the eye helps to prevent blindness, vision loss, and nerve damage. Pilocarpine works by decreasing the amount of fluid within the eye.

HOW TO USE: This medication is usually used once daily at bedtime or as directed by your doctor. To apply eye gel, wash your hands first. To avoid contamination, be careful not to touch the tip of the tube to any surface or let it touch your eye.

Tilt your head back and pull down lower eyelid to make a pouch. Gently squeeze the tube to place a 1/2 inch (1.5 centimeters) ribbon of gel into the pouch of the eyelid, unless you have been told by your doctor to use a different amount. Let go of the eyelid, close your eyes, and roll your eyeball in all directions for 1 to 2 minutes to spread the gel. Try not to blink and do not rub your eye. Repeat these steps for your other eye if so directed.

Remove extra gel from the eyelids and eyelashes with a tissue. Wipe the tip of the tube with a clean tissue to remove extra medication before recapping it. Wash hands again to remove any gel that may be on them.

If you are using another kind of eye medication that is a solution, use it at least 5 minutes before applying this medication. If you are using another kind of eye gel or ointment, wait at least 10 minutes after using this medication before applying it. Use eye drops/gels before ointments to allow the eye drops/gels to enter the eye.

Use this medication regularly in order to get the most benefit from it. Most people with glaucoma or high pressure in the eyes do not have any symptoms. To help you remember, use it at the same time each day.

SIDE EFFECTS: Temporary irritation/burning/stinging of the eye, temporary blurred vision, poor vision in dim light, headache, or brow ache may occur. If any of these effects persist or worsen, contact your doctor or pharmacist promptly. (See also Precautions section.)

Crusting of the gel on the eyelids or eyelashes may occur overnight, causing them to stick together. If this occurs, wash them with water.

Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.

Tell your doctor immediately if any of these unlikely but serious side effects occur: eye pain, flushing, diarrhea, nausea, stomach/abdominal pain or cramps, increased saliva, unusual sweating, vision changes.

A very serious allergic reaction to this drug is rare. However, seek immediate medical attention if you notice any of the following symptoms of a serious allergic reaction: rash, itching, swelling, severe dizziness, trouble breathing.

This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.

Contact your doctor for medical advice about side effects. The following numbers do not provide medical advice, but in the US you may report side effects to the Food and Drug Administration (FDA) at 1-800-FDA-1088. In Canada, you may call Health Canada at 1-866-234-2345.

PRECAUTIONS: Before using pilocarpine, tell your doctor or pharmacist if you are allergic to it; or to preservatives (e.g., benzalkonium chloride); or if you have any other allergies.

Before using this medication, tell your doctor or pharmacist your medical history, especially of: asthma, other eye problems (e.g., iritis, detached retina), heart disease (e.g., heart failure, recent heart attack), low or high blood pressure, overactive thyroid (hyperthyroidism), Parkinsonism, stomach/intestinal problems (e.g., ulcers, spasms).

After you apply pilocarpine, your vision may become temporarily blurred or unstable. Vision in dim light may be affected. Use caution while driving (especially at night), using machinery, or doing any activity that requires clear vision. Limit alcoholic beverages.

During pregnancy, this drug should be used only when clearly needed. Discuss the risks and benefits with your doctor.

It is not known if this medication passes into breast milk. Consult your doctor before breast-feeding.

DRUG INTERACTIONS: Your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with them first.

Before using this medication, tell your doctor or pharmacist of all prescription and nonprescription/herbal products you may use, especially: other eye medications.

This document does not contain all possible interactions. Therefore, before using this product, tell your doctor or pharmacist of all the products you use. Keep a list of all your medications with you, and share the list with your doctor and pharmacist.

OVERDOSE: This medicine may be harmful if swallowed. If swallowing or overdose is suspected, contact your local poison control center or emergency room immediately. US residents should call the US National Poison Hotline at 1-800-222-1222. Canada residents should call a provincial poison control center. Symptoms of overdose may include: increased saliva, slow heartbeat, nausea, diarrhea, increased sweating.

NOTES: Do not share this medication with others.

Laboratory and/or medical tests (e.g., eye exams) should be performed periodically to monitor your progress or check for side effects. Consult your doctor for more details.

MISSED DOSE: If you miss a dose, apply it as soon as you remember. If it is near the time of the next dose, skip the missed dose and resume your usual dosing schedule. Do not double the dose to catch up.

STORAGE: Store between 36-80 degrees F (2-27 degrees C) away from light or moisture. Do not freeze. Do not store in the bathroom. Keep all medicines away from children and pets.

Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company for more details about how to safely discard your product.

Information last revised July 2008 Copyright(c) 2008 First DataBank, Inc.