Pilocarpine (parasympathomimetic agent)

Pilocarpine is a parasympathomimetic agent that is available as systemic and local preparations.

Know the basics

What is pilocarpine used for?

Pilocarpine reduces the amount of fluid in the eye, which decreases pressure inside the eye.

Pilocarpine ophthalmic (for the eyes) is used to treat glaucoma or ocular hypertension (high pressure inside the eye).

How should I take pilocarpine?

Use this medication exactly as prescribed by your doctor. Do not use it in larger amounts or for longer than recommended. Follow the directions on your prescription label.

Wash your hands before using the eye drops.

To apply the eye drops:

• Tilt your head back slightly and pull down your lower eyelid to create a small pocket. Hold the dropper above the eye with the dropper tip down. Look up and away from the dropper as you squeeze out a drop, then close your eye.
• Gently press your finger to the inside corner of the eye (near your nose) for about 1 minute to keep the liquid from draining into your tear duct.
• If you use any other eye medications, wait about 5 minutes after using pilocarpine eye drops before using the other medication.
• Do not allow the dropper tip to touch any surface, including the eyes or hands. If the dropper becomes contaminated it could cause an infection in your eye, which can lead to vision loss or serious damage to the eye.
• Do not use the eye drops if the liquid has changed colors or has particles in it. Call your doctor for a new prescription.

How do I store pilocarpine?

This product is best stored at room temperature away from direct light and moisture. To prevent drug damage, you should not store it in the bathroom or the freezer. 

There may be different brands of this drug that may have different storage needs. So, it is important to always check the product package for instructions on storage, or ask your pharmacist. For safety, you should keep all medicines away from children and pets.

You should not flush this product down the toilet or pour them into a drain unless instructed to do so. Additionally, it is important to properly discard this product when it is expired or no longer needed. Consult your pharmacist for more details about how to safely discard your product.

Know the precautions & warnings

What should I know before using pilocarpine?

Before using this drug, tell your doctor if you are/have:

• Pregnant or breastfeeding.
• Taking any other medicines. This includes any prescription, OTC, and herbal remedies.
• An allergy to any of the ingredients of this product.
• Any other illnesses, disorders, or medical conditions.

Is it safe to take pilocarpine during pregnancy or breast-feeding?

Unfortunately, there isn’t enough information about the safety of using this drug during pregnancy and breastfeeding. Please always consult with your doctor to weigh the potential benefits and risks before taking any medication.

This medication is pregnancy risk category C according to the US Food and Drug Administration (FDA).

FDA pregnancy risk category reference below:

• A=No risk
• B=No risk in some studies
• C=There may be some risk
• D=Positive evidence of risk
• X=Contraindicated
• N=Unknown

Know the side effects

What are the side effects of pilocarpine?

Like all drugs, this product may have side effects. If they occur, side effects are generally mild and resolve once treatment is finished or the dose is lowered. Some reported side effects include:

• Blurred vision
• Brow or headache
• Eye pain
• Myopia
• Burning or itching of the eyes
• Flu-like symptoms
• Rhinitis
• Conjunctivitis
• Nausea, vomiting
• Diarrhea, constipation
• Bloating, flatulence
• Dyspepsia
• Dizziness
• Flushing
• Hypertension
• Palpitations
• Increased urination and frequency
• Watery eyes
• Skin reddening or itchiness
• Sweating

However, not everyone experiences these side effects. In addition, some people may experience other side effects. So, if you have any concerns about a side effect, please consult your doctor or pharmacist.

Know the interactions

What drugs may interact with pilocarpine?

This medication may interact with other drugs that you are currently taking, which can change how your drug works or increase your risk for serious side effects. 

To avoid any potential drug interactions, you should keep a list of all the drugs you are using (including prescription drugs, nonprescription drugs, and herbal products) and share it with your doctor and pharmacist. 

Drugs with known interactions:

• Beta blockers
• Other miotics
• Other parasympathomimetic drugs
• Anticholinergics

If you experience an adverse drug interaction, inform your doctor immediately to reevaluate your treatment plan. Approaches include dose adjustment, drug substitution, or ending therapy.

Does food or alcohol interact with pilocarpine?

This drug may interact with food or alcohol by altering the way the drug works or increase the risk for serious side effects. Avoid consuming high-fat meals. Please discuss with your doctor or pharmacist any potential food or alcohol interactions before using this drug.

What health conditions may interact with pilocarpine?

This drug may interact with underlying conditions. This interaction may worsen your health condition or alter the way the drug works. Therefore, it is important to always let your doctor and pharmacist know all the health conditions you currently have.

Understand the dosage

The information provided is not a substitute for any medical advice. Therefore, you should always consult with your doctor or pharmacist before using any medication.

What is the dose for an adult?

Open-Angle Glaucoma

Ophthalmic Solution: Instill 1 to 2 drops of pilocarpine in the affected eye 3 to 4 times daily. Wait at least 5 minutes before instilling other eyedrops. Remove contact lenses before administration of benzalkonium chloride-containing solutions and wait at least 15 minutes before reinserting them.

Ophthalmic Gel: Apply one-half inch ribbon of gel in the lower conjunctival sac of the affected eye daily at bedtime. If other eyedrops are used, they should be instilled at least 5 minutes before the gel is applied.

Ophthalmic Insert: Insert one system into lower conjunctival cul-de-sac at bedtime. Replace every 7 days.

Intraocular Hypertension

Ophthalmic Solution: Instill 1 to 2 drops in the affected eye 3 to 4 times daily. Wait at least 5 minutes before instilling other eyedrops. Remove contact lenses before administration of benzalkonium chloride-containing solutions and wait at least 15 minutes before reinserting them.

Ophthalmic Gel: Apply one-half inch ribbon of gel in the lower conjunctival sac of the affected eye daily at bedtime. If other eyedrops are used, they should be instilled at least 5 minutes before the gel is applied.

Ophthalmic Insert: Insert one system into lower conjunctival cul-de-sac at bedtime. Replace every 7 days.

What is the dose for a child?

Glaucoma

2 to 18 years:

Ophthalmic Solution: Instill 1 to 2 drops in the affected eye(s) 3 to 4 times daily.

Wait at least 5 minutes before instilling other eyedrops. Remove contact lenses before administration of benzalkonium chloride-containing solutions and wait at least 15 minutes before reinserting them.

Ophthalmic Gel: Apply one-half inch ribbon of gel in the lower conjunctival sac of the affected eye daily at bedtime. If other eyedrops are used, they should be instilled at least 5 minutes before the gel is applied.

Intraocular Hypertension

2 to 18 years:

Ophthalmic Solution: Instill 1 to 2 drops in the affected eye 3 to 4 times daily.

Wait at least 5 minutes before instilling other eyedrops. Remove contact lenses before administration of benzalkonium chloride-containing solutions and wait at least 15 minutes before reinserting them.

Ophthalmic Gel: Apply one-half inch ribbon of gel in the lower conjunctival sac of the affected eye daily at bedtime. If other eyedrops are used, they should be instilled at least 5 minutes before the gel is applied.

0 to 2 years

Instill one drop in the affected eye(s) 3 times daily. Start with the lowest available strength.

How is pilocarpine available?

Pilocarpine is available in the following dosage forms and strengths:

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

Gel, Ophthalmic, as hydrochloride:

Pilopine HS: 4% (4g) [contains benzalkonium chloride, edetete disodium]

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)

What should I do in case of an emergency or overdose?

In case of an emergency or an overdose, call your local emergency services or go to the nearest emergency room.

What should I do if I miss a dose?

If you miss a dose, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and take your regular dose as scheduled. Do not take a double dose.