Pilocarpine Hydrochloride (Page 2 of 2)

11 DESCRIPTION

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:

ab

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: C11 H16 N2 O2 • HCl

Molecular Weight: 244.72

Pilocarpine hydrochloride, USP is a white or almost white, crystalline powder or colorless crystals hygroscopic. It is very soluble in water, freely soluble in alcohol, slightly soluble in chloroform and insoluble in ether.

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: 0.5% hypromellose 2910; boric acid; sodium citrate; sodium chloride (present in 1% product 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 5.5 and an osmolality of 270 to 350 mOsm/kg (1% product), 290 to 350 mOsm/kg (2% product) and 500 to 600 mOsm/kg (4% product).

12 CLINICAL PHARMACOLOGY

12.1 Mechanism of Action

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.

12.3 Pharmacokinetics

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 Cmax 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) Cmax and AUC0-last values on Day 8 were 3.7 (3.2) ng/mL and 7.7 (8.4) ng×hour/mL, respectively. The Tmax values on Day 8 ranged from 0.5 to 1 hour.

13 NONCLINICAL TOXICOLOGY

13.1 Carcinogenesis, Mutagenesis, Impairment of Fertility

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

14 CLINICAL STUDIES

In clinical trials reported in the medical literature, pilocarpine ophthalmic solution reduced intraocular pressure (IOP) by 3 mm Hg to 7 mm Hg 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.

16 HOW SUPPLIED/STORAGE AND HANDLING

Pilocarpine Hydrochloride Ophthalmic Solution USP, 1% , 2% and 4% is supplied sterile in natural low density polyethylene plastic bottles and natural low density polyethylene tips with dark green high density polyethylene caps.

It is available as follows:

1%:

15 mL in 15 mL Container: NDC 69238-1745-8

2%:

15 mL in 15 mL Container: NDC 69238-1746-8

4%:

15 mL in 15 mL Container: NDC 69238-1747-8

STORAGE: Store at 15º to 25°C (59º to 77°F) and protect from freezing.

17 PATIENT COUNSELING INFORMATION

17.1 Avoiding Contamination of the Product

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

17.2 Night Driving

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

17.3 Accommodative Spasm

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.

17.4 Contact Lens Wear

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

17.5 Concomitant Topical Ocular Therapy

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

17.6 Systemic Exposure

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.

Rx Only

Manufactured by:

Amneal Pharmaceuticals Pvt. Ltd.

Parenteral Unit

Ahmedabad 382213, INDIA

Distributed by:

Amneal Pharmaceuticals LLC

Bridgewater, NJ 08807

Rev. 01-2021-02

PRINCIPAL DISPLAY PANEL

NDC 69238-1745-8
Pilocarpine hydrochloride ophthalmic solution USP, 1%
Rx only
Amneal Pharmaceuticals LLC

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NDC 69238-1746-8
Pilocarpine hydrochloride ophthalmic solution USP, 2%
Rx only
Amneal Pharmaceuticals LLC

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1
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NDC 69238-1747-8
Pilocarpine hydrochloride ophthalmic solution USP, 4%
Rx only
Amneal Pharmaceuticals LLC

1
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1
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PILOCARPINE HYDROCHLORIDE
pilocarpine hydrochloride solution/ drops
Product Information
Product Type HUMAN PRESCRIPTION DRUG Item Code (Source) NDC:69238-1745
Route of Administration OPHTHALMIC DEA Schedule
Active Ingredient/Active Moiety
Ingredient Name Basis of Strength Strength
PILOCARPINE HYDROCHLORIDE (PILOCARPINE) PILOCARPINE HYDROCHLORIDE 10 mg in 1 mL
Inactive Ingredients
Ingredient Name Strength
BENZALKONIUM CHLORIDE
BORIC ACID
HYDROCHLORIC ACID
HYPROMELLOSE 2910 (10000 MPA.S)
SODIUM CHLORIDE
SODIUM CITRATE
SODIUM HYDROXIDE
WATER
Packaging
# Item Code Package Description Multilevel Packaging
1 NDC:69238-1745-8 1 BOTTLE in 1 CARTON contains a BOTTLE
1 15 mL in 1 BOTTLE This package is contained within the CARTON (69238-1745-8)
Marketing Information
Marketing Category Application Number or Monograph Citation Marketing Start Date Marketing End Date
ANDA ANDA214193 09/23/2020
PILOCARPINE HYDROCHLORIDE
pilocarpine hydrochloride solution/ drops
Product Information
Product Type HUMAN PRESCRIPTION DRUG Item Code (Source) NDC:69238-1746
Route of Administration OPHTHALMIC DEA Schedule
Active Ingredient/Active Moiety
Ingredient Name Basis of Strength Strength
PILOCARPINE HYDROCHLORIDE (PILOCARPINE) PILOCARPINE HYDROCHLORIDE 20 mg in 1 mL
Inactive Ingredients
Ingredient Name Strength
BENZALKONIUM CHLORIDE
BORIC ACID
HYDROCHLORIC ACID
HYPROMELLOSE 2910 (10000 MPA.S)
SODIUM CITRATE
SODIUM HYDROXIDE
WATER
Packaging
# Item Code Package Description Multilevel Packaging
1 NDC:69238-1746-8 1 BOTTLE in 1 CARTON contains a BOTTLE
1 15 mL in 1 BOTTLE This package is contained within the CARTON (69238-1746-8)
Marketing Information
Marketing Category Application Number or Monograph Citation Marketing Start Date Marketing End Date
ANDA ANDA214193 09/23/2020
PILOCARPINE HYDROCHLORIDE
pilocarpine hydrochloride solution/ drops
Product Information
Product Type HUMAN PRESCRIPTION DRUG Item Code (Source) NDC:69238-1747
Route of Administration OPHTHALMIC DEA Schedule
Active Ingredient/Active Moiety
Ingredient Name Basis of Strength Strength
PILOCARPINE HYDROCHLORIDE (PILOCARPINE) PILOCARPINE HYDROCHLORIDE 40 mg in 1 mL
Inactive Ingredients
Ingredient Name Strength
BENZALKONIUM CHLORIDE
BORIC ACID
HYDROCHLORIC ACID
HYPROMELLOSE 2910 (10000 MPA.S)
SODIUM CITRATE
SODIUM HYDROXIDE
WATER
Packaging
# Item Code Package Description Multilevel Packaging
1 NDC:69238-1747-8 1 BOTTLE in 1 CARTON contains a BOTTLE
1 15 mL in 1 BOTTLE This package is contained within the CARTON (69238-1747-8)
Marketing Information
Marketing Category Application Number or Monograph Citation Marketing Start Date Marketing End Date
ANDA ANDA214193 09/23/2020
Labeler — Amneal Pharmaceuticals NY LLC (123797875)

Revised: 01/2021 Amneal Pharmaceuticals NY LLC

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