Pilocarpine Hydrochloride Solution/ Drops
FDA Label NDC 69315-316

Pilocarpine hydrochloride ophthalmic solution is indicated for the:

One drop of pilocarpine hydrochloride ophthalmic solution 1%, 2% or 4% should be applied topically in the eye(s) upto four times daily. Pilocarpine-naïve patients should be started on the 1% concentration as higher concentrations are often not tolerated initially. The frequency of instillation and concentration of pilocarpine hydrochloride ophthalmic solution are determined by the severity of the elevated intraocular pressure and miotic response of the patient.

To limit systemic exposure to pilocarpine, patients may be instructed to perform punctal occlusion for 2 minutes after instillation of pilocarpine hydrochloride ophthalmic solution.

Prior to pilocarpine hydrochloride ophthalmic solution use, treatment with secretory suppressants and hyperosmotic agents may be needed to lower IOP below 50 mmHg and relieve iris ischemia.

For initial management of acute angle-closure glaucoma, one drop of pilocarpine hydrochloride ophthalmic solution 1% or 2% may be applied topically in the eye(s) up to three times over a 30-minute period.

If laser iridoplasty or iridomy is used to break the attack, one drop of pilocarpine hydrochloride ophthalmic solution 4% should be administered prior to the procedure. Following laser iridoplasty, one drop of pilocarpine hydrochloride ophthalmic solution 1% should be administered four times daily until an iridotomy can be performed.

One drop of pilocarpine hydrochloride ophthalmic solution 1%, 2% or 4% (or two drops administered five minutes apart) should be applied topically in the eye(s) 15 to 60 minutes prior to surgery.

One drop of pilocarpine hydrochloride ophthalmic solution 1%, 2% or 4% (or two drops administered five minutes apart) should be applied topically in the eye(s).

Pilocarpine hydrochloride ophthalmic solution may be used in combination with beta-blockers, carbonic anhydrase inhibitors, sympathomimetics or hyperosmotic agents. If more than one topical ophthalmic drug is being used, the drugs should be administered at least five (5) minutes apart.

In children under 2 years of age, one drop of pilocarpine hydrochloride ophthalmic solution 1% should be applied topically in the eye(s) three times daily. Children 2 years of age and over should be dosed as for adults.

For the induction of miosis prior to goniotomy or trabeculotomy in children, one drop of pilocarpine hydrochloride ophthalmic solution 1% or 2% should be applied topically in the eye 15 to 60 minutes prior to surgery.

Bottle filled with 15 mL of 1% (10 mg/mL), 2% (20 mg/mL) or 4% (40 mg/mL) sterile pilocarpine hydrochloride ophthalmic solution, USP.

None.

Patients should be advised to exercise caution in night driving and other hazardous occupations in poor illumination. In addition, miotics may cause accommodative spasm. Patients should be advised not to drive or use machinery if vision is not clear.

As with all miotics, rare cases of retinal detachment have been reported when used in certain susceptible individuals and those with pre-existing retinal disease; therefore, a thorough examination of the retina including funduscopy is advised in all patients prior to the initiation of therapy.

Pilocarpine hydrochloride ophthalmic solution is not recommended to be used when iritis is present.

Caution is advised when using pilocarpine hydrochloride ophthalmic solution in pediatric patients with primary congenital glaucoma for control of intraocular pressure (IOP) as cases of a paradoxical increase in IOP have been reported. In addition, the use of pilocarpine hydrochloride ophthalmic solution is not recommended in pediatric patients diagnosed with glaucoma secondary to anterior segment dysgenesis or uveitis (especially if uveitis is active).

Contact lens wearers should be advised to remove their lenses prior to the instillation of pilocarpine hydrochloride ophthalmic solution and to wait 10 minutes after dosing before reinserting their contact lenses.

Clinical Studies Experience

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.
The safety data described below reflect exposure in four controlled clinical trials of 90 days to 2 years duration in 317 patients diagnosed with open-angle glaucoma or ocular hypertension. In the four clinical trials, patients were treated with pilocarpine hydrochloride ophthalmic solution 2%, two to four times daily or with pilocarpine 1%, 1.75% or 2% in fixed combination with betaxolol 0.25%, two or three times daily. The most frequently reported adverse reactions occurring in ≥ 5% of patients in the pilocarpine 2% populations were: headache/browache, accommodative change, blurred vision, eye irritation, visual impairment (dim, dark, or “jumping” vision), and eye pain.

The adverse reaction profile reported for the use of pilocarpine hydrochloride ophthalmic solution in pediatric patients is comparable to that seen in adult patients.

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. Pilocarpine hydrochloride ophthalmic solution should be given to a pregnant woman only if clearly needed.

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 ophthalmic solution is administered to a nursing woman.

Safety and effectiveness of pilocarpine hydrochloride ophthalmic solution in pediatric patients have been established.

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

Systemic toxicity following topical ocular administration of pilocarpine is rare, but occasionally patients who are sensitive may develop sweating and gastrointestinal overactivity following the suggested dosage and administration. Overdosage can produce sweating, salivation, nausea, tremors and slowing of the pulse and a decrease in blood pressure. In moderate overdosage, spontaneous recovery is to be expected and is aided by intravenous fluids to compensate for dehydration. For patients demonstrating severe poisoning, atropine, the pharmacologic antagonist to pilocarpine, should be used.

Pilocarpine hydrochloride ophthalmic solution, USP is a cholinergic agonist prepared as a sterile topical ophthalmic solution. The active ingredient is represented by the chemical structure:

Chemstricture (Chemstricture)

Established name: pilocarpine hydrochloride, USP

Chemical name: 2(3H)-furanone, 3-ethyldihydro-4-[(1-methyl-1H-imidazol-5-yl)-methyl]- monohydrochloride, (3S-cis)-. Molecular Formula: C₁₁H₁₆N₂O₂ • HCl; Molecular Weight: 244.72

Each mL of pilocarpine hydrochloride ophthalmic solution, USP contains:

Active: pilocarpine hydrochloride, USP 1% (10 mg/mL), 2% (20 mg/mL), or 4% (40 mg/mL).

Preservative: benzalkonium chloride 0.01%.

Inactives: hypromellose 2910, boric acid, sodium citrate, sodium chloride (present in 1% only); hydrochloric acid and/or sodium hydroxide (to adjust pH); water for injection.
Pilocarpine hydrochloride ophthalmic solution, USP has a pH of 3.5 to 5.0 and an osmolality of 270 to 350 mOsmol/kg (1% product), 290 to 350 mOsmol/kg (2% product) and 500 to 600 mOsmol/kg (4% product).

Pilocarpine hydrochloride is a direct acting cholinergic parasympathomimetic agent which acts through direct stimulation of muscarinic receptors and smooth muscle such as the iris and secretory glands. Pilocarpine contracts the ciliary muscle, causing increased tension on the scleral spur and opening of the trabecular meshwork spaces to facilitate outflow of aqueous humor. Outflow resistance is reduced, lowering intraocular pressure (IOP). Pilocarpine also produces miosis through contraction of the iris sphincter muscle. Miosis relieves appositional angle narrowing and closure, which lowers IOP in certain types of angle-closure glaucoma.

Systemic exposure to pilocarpine was evaluated in 14 healthy subjects administered 2 drops of pilocarpine hydrochloride ophthalmic solution 4% to both eyes four times daily for eight days. A comparison of C_max values on Days 5 and 8 indicated that pilocarpine concentrations in plasma reached steady-state following topical administration of pilocarpine hydrochloride ophthalmic solution 4%. The mean (SD) C_max and AUC_0-last values on Day 8 were 3.7 (3.2) ng/mL and 7.7 (8.4) ng×hour/mL, respectively. The T_max values on Day 8 ranged from 0.5 to 1 hour.

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

In clinical trials reported in the medical literature, pilocarpine ophthalmic solution reduced intraocular pressure (IOP) by 3-7 mmHg in patients with open-angle glaucoma. Pilocarpine ophthalmic solution has also been shown to be effective in the induction of miosis, in the prevention of postoperative elevated IOP, and in the management of acute angle-closure glaucoma.

Pilocarpine hydrochloride ophthalmic solution, USP 1%, 2% and 4% is supplied sterile in 15 mL labeled LDPE bottles with insert cap assembly comprising of green colored HDPE screw cap over a LDPE nozzle with tamper evident LDPE dust cover sealing the bottle cap.

15 mL in 15 mL bottles

1%: NDC 69315-314-15

2%: NDC 69315-315-15

4%: NDC 69315-316-15

STORAGE: Store at 20°C to 25°C (68°F to 77°F), excursions permitted between 15°C and 30°C (59°F and 86°F) [see USP Controlled Room Temperature]. Protect from freezing.

Do not touch dropper tip to any surface, as this may contaminate the contents.

Caution is advised with night driving and when hazardous activities are undertaken in poor illumination.

Pilocarpine hydrochloride ophthalmic solution may cause problems when changing focus between near objects and distant objects. Do not drive or use machinery if vision is not clear.

Contact lens should be removed prior to the instillation of pilocarpine hydrochloride ophthalmic solution. Wait 10 minutes after dosing before reinserting contact lenses.

If more than one topical ophthalmic medication is being used, the medicines must be administered at least 5 minutes apart.

To limit exposure to pilocarpine to the eye alone, close eyes gently and apply pressure with finger to the corner of eye by the nose for 2 minutes after instillation of pilocarpine hydrochloride ophthalmic solution.

PILOCARPINE HYDROCHLORIDE OPHTHALMIC SOLUTION, USP 1%, 2% AND 4% (pye″ loe kar′ peen hye″ droe klor′ ide).

This instructions for use contains information on how to use pilocarpine hydrochloride ophthalmic solution. Please follow these instructions carefully when using pilocarpine hydrochloride ophthalmic solution. Use pilocarpine hydrochloride ophthalmic solution as prescribed by your doctor. If you or your caregiver have any questions about how to use pilocarpine hydrochloride ophthalmic solution, talk to your doctor.

Important Information You Need to Know Before Using Pilocarpine Hydrochloride Ophthalmic Solution

• Pilocarpine hydrochloride ophthalmic solution is for use in the eye only.
• Use pilocarpine hydrochloride ophthalmic solution exactly as your doctor tells you to use it.
• If you use other eye medicines dropped into the eye (topically applied ophthalmic medicines), use the medicines at least 5 minutes before or 5 minutes after the use of pilocarpine hydrochloride ophthalmic solution.
• Wash your hands with soap and water before each use.
• Before using the medicine for the first time, be sure the dust cover seal is not broken or damaged.
• Pilocarpine hydrochloride ophthalmic solution contains benzalkonium chloride which may be absorbed by contact lenses. If you wear contact lenses, remove them before you use your pilocarpine hydrochloride ophthalmic solution. You can place your contact lenses back into your eyes 10 minutes after using your pilocarpine hydrochloride ophthalmic solution.
• If you do not handle eye medicines (ophthalmic medicines) the right way the medicine can become contaminated by common bacteria known to cause eye infection. If the dropper tip touches your eye or areas around your eye, the dropper tip can become contaminated with bacteria. Serious damage to the eye may happen, such as eye infection and other serious problems, including loss of vision when using contaminated ophthalmic medicines.
• If you think your medicine may be contaminated, or if you develop an eye infection, contact your doctor right away. Your doctor will decide if you should continue to use this bottle.
• The dropper tip is designed to provide a premeasured drop of the eye medicine. Therefore, do not enlarge the hole of the dropper tip.
• If you have any eye or skin reaction, especially pink eye (conjunctivitis) or eyelid reaction to pilocarpine hydrochloride ophthalmic solution, stop using it and call your doctor right away.
• If you are scheduled to have eye surgery or have a problem such as trauma to the eye or infection in your eye while using pilocarpine hydrochloride ophthalmic solution, call your doctor right away.
• After you have used all the pilocarpine hydrochloride ophthalmic solution doses, there will be some pilocarpine hydrochloride ophthalmic solution left in the bottle. You should not be concerned because you have received the full amount of pilocarpine hydrochloride ophthalmic solution that your doctor prescribed. An extra amount of pilocarpine hydrochloride ophthalmic solution has been added to the bottle. Do not attempt to remove any remaining medicine from the bottle.

Preparing to use Pilocarpine Hydrochloride Ophthalmic Solution
Step 1: Wash your hands with soap and water	Step 4: Pull off the dust cover and throw it away in your household trash. See Figure C. Figc (Figc) Figure C: Pull off the dust cover.
Step 2: Make sure the dust cover is on the bottle and the dust cover seal is not broken or damaged. See Figure A. Figa (Figa) Figure A: Bottle as you receive it.
Step 3: Snap off the dust cover by turning it to the right (clockwise) to break the dust cover seal. See Figure B. Figb (Figb) Figure B: Snap off the dust cover.	Step 5: Unscrew the green colored cap from the bottle by turning it to the left (counterclockwise). See Figure D. “Keep the green colored cap. Do not throw it away” Figd (Figd) Figure D: Unscrew the Cap, and do not throw it away.
Using Pilocarpine Hydrochloride Ophthalmic Solution
Step 6: Tilt your head backwards and look up. Pull down your lower eyelid with a clean finger. Gently squeeze the bottle to drop the medicine into your eye. See Figure E. Do not let the dropper tip touch the surface of your eye. Fige (Fige) Figure E: Tilt head backwards. Dispense drops with gentle pressure. Do not touch dropper tip to the surface of the eye.	Step 8: Repeat Step 6 and Step 7 with the other eye if instructed to do so by your doctor" and Step 9: Replace the green colored cap by screwing it down onto the bottle after each use. See Figure G. Figg (Figg) Figure G: Replace the green cap after every use, and screw the cap down.
Step 7: After using, gently close your eyelid and press a finger into the corner of your eye closest to your nose for 2 minutes. This helps to keep the medicine in your eye. See Figure F. Figf (Figf) Figure F: After using, press a finger into the corner of your eye, by the nose for 2 minutes. This helps keep the solution in your eye.

Storing Pilocarpine Hydrochloride Ophthalmic Solution:

• Store pilocarpine hydrochloride ophthalmic solution at room temperature between 68°F to 77°F (20°C to 25°C).
• Do not freeze pilocarpine hydrochloride ophthalmic solution.
• Safely throw away medicine that is out of date or no longer needed.

Keep pilocarpine hydrochloride ophthalmic solution and all medicines out of the reach of children.

This instructions for use has been approved by the U.S. Food and Drug Administration.

Manufactured by:

FDC Limited

B-8, MIDC Industrial Area,Waluj,

Chhatrapati Sambhajinagar - 431 136

Maharashtra, India.

Distributed by:

Leading Pharma, LLC

Fairfield, NJ07004.

Rx Only

Approved: 11/2025

Pilocarpine hydrochloride ophthalmic solution, USP 1%

15 mL in 15 mL bottles

1%: NDC 69315-314-15

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Pilocarpine hydrochloride ophthalmic solution, USP 2%

15 mL in 15 mL bottles

2%: NDC 69315-315-15

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Pilocarpine hydrochloride ophthalmic solution, USP 4%

15 mL in 15 mL bottles

4%: NDC 69315-316-15

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