PILOCARPINE HYDROCHLORIDE- pilocarpine hydrochloride ophthalmic solution solution/ drops

Pilocarpine Hydrochloride by

Drug Labeling and Warnings

Pilocarpine Hydrochloride by is a Prescription medication manufactured, distributed, or labeled by Somerset Therapeutics, LLC, Wintac Limited. Drug facts, warnings, and ingredients follow.

Drug Details [pdf]

  • 1 INDICATIONS AND USAGE

    Pilocarpine hydrochloride ophthalmic solution, is indicated for the:

    1.1 Reduction of Elevated Intraocular Pressuare (IOP) in Patients with Open-Angle Glaucoma or Ocular Hypertension

    1.2 Management of Acute Angle-Closure Glaucoma

    1.3 Prevention of Postoperative Elevated IOP Associated with Laser Surgery

    1.4 Induction of Miosis

  • 2 DOSAGE AND ADMINISTRATION

    2.1 Reduction of Elevated Intraocular Pressure (IOP) in Patients with Open-Angle Glaucoma or Ocular Hypertension

    One drop of pilocarpine hydrochloride ophthalmic solution 1%, 2% or 4% should be applied topically in the eye(s) up to 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.

    2.2 Management of Acute Angle-Closure Glaucoma

    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.

    2.3 Prevention of Postoperative Elevated IOP Associated with Laser 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) 15 to 60 minutes prior to surgery.

    2.4 Induction of Miosis

    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).

    2.5 Use with Other Topical Ophthalmic Medications

    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.

    2.6 Use in Pediatric Patients

    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.

  • 3 DOSAGE FORMS AND STRENGTHS

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

  • 4 CONTRAINDICATIONS

    None.

  • 5 WARNINGS AND PRECAUTIONS

    5.1 Poor Illumination

    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.

    5.2 Pre-existing Retinal Disease

    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.

    5.3 Iritis

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

    5.4 Primary Congenital Glaucoma

    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).

    5.5 Contact Lens Wear

    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.

  • 6 ADVERSE REACTIONS

    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.

  • 8 USE IN SPECIFIC POPULATIONS

    8.1 Pregnancy

    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.

    8.3 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 ophthalmic solution is administered to a nursing woman.

    8.4 Pediatric Use

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

    8.5 Geriatric Use

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

  • 10 OVERDOSAGE

    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.

  • 11 DESCRIPTION

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

    Image

    Molecular Structure

    Established name: pilocarpine hydrochloride

    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 contains: Active: pilocarpine hydrochloride 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 has a pH of 3.5 to 5.5 and an osmolality of 290 to 350 mOsm/kg (1% and 2% products) and 550 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 3-7 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.

  • 16 HOW SUPPLIED/STORAGE AND HANDLING

    Pilocarpine hydrochloride ophthalmic solution USP, 1%, 2% and 4% is clear colorless solution supplied sterile in natural LDPE bottles plugged with natural LDPE nozzle and green coloured HDPE cap.

    15 mL in 15 mL bottles

    1%: NDC 70069-181-01

    2%: NDC 70069-191-01

    4%: NDC 70069-201-01

    STORAGE: Store between 15º to 25ºC (59º to 77ºF) and protect from freezing; [see USP Controlled Room Temperature].

  • 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 for:

    Somerset Therapeutics, LLC

    Hollywood, FL 33024

    Made in India

    Code No.: KR/DRUGS/KTK/28/289/97

    ST-PIL/P/00

  • PACKAGE LABEL.PRINCIPAL DISPLAY PANEL

    Container Label: Pilocarpine hydrochloride ophthalmic solution USP, 1%

    Container 1%

    Carton Label: Pilocarpine hydrochloride ophthalmic solution USP, 1%

    Carton 1%

    Container Label: Pilocarpine hydrochloride ophthalmic solution USP, 2%

    Container 2%

    Carton Label: Pilocarpine hydrochloride ophthalmic solution USP, 2%

    Carton 2%

    Container Label: Pilocarpine hydrochloride ophthalmic solution USP, 4 %

    Container 4%

    Carton Label: Pilocarpine hydrochloride ophthalmic solution USP, 4 %

    Carton 4%
  • INGREDIENTS AND APPEARANCE
    PILOCARPINE HYDROCHLORIDE 
    pilocarpine hydrochloride ophthalmic solution solution/ drops
    Product Information
    Product TypeHUMAN PRESCRIPTION DRUGItem Code (Source)NDC: 70069-181
    Route of AdministrationOPHTHALMIC
    Active Ingredient/Active Moiety
    Ingredient NameBasis of StrengthStrength
    PILOCARPINE HYDROCHLORIDE (UNII: 0WW6D218XJ) (PILOCARPINE - UNII:01MI4Q9DI3) PILOCARPINE HYDROCHLORIDE10 mg  in 1 mL
    Inactive Ingredients
    Ingredient NameStrength
    BENZALKONIUM CHLORIDE (UNII: F5UM2KM3W7)  
    HYPROMELLOSE 2910 (4000 MPA.S) (UNII: RN3152OP35)  
    BORIC ACID (UNII: R57ZHV85D4)  
    SODIUM CITRATE (UNII: 1Q73Q2JULR)  
    SODIUM CHLORIDE (UNII: 451W47IQ8X)  
    HYDROCHLORIC ACID (UNII: QTT17582CB)  
    SODIUM HYDROXIDE (UNII: 55X04QC32I)  
    WATER (UNII: 059QF0KO0R)  
    Product Characteristics
    ColorWHITE (Clear Colorless Solution) Score    
    ShapeSize
    FlavorImprint Code
    Contains    
    Packaging
    #Item CodePackage DescriptionMarketing Start DateMarketing End Date
    1NDC: 70069-181-011 in 1 CARTON11/25/2019
    115 mL in 1 BOTTLE; Type 0: Not a Combination Product
    Marketing Information
    Marketing CategoryApplication Number or Monograph CitationMarketing Start DateMarketing End Date
    ANDAANDA21038411/25/2019
    PILOCARPINE HYDROCHLORIDE 
    pilocarpine hydrochloride ophthalmic solution solution/ drops
    Product Information
    Product TypeHUMAN PRESCRIPTION DRUGItem Code (Source)NDC: 70069-191
    Route of AdministrationOPHTHALMIC
    Active Ingredient/Active Moiety
    Ingredient NameBasis of StrengthStrength
    PILOCARPINE HYDROCHLORIDE (UNII: 0WW6D218XJ) (PILOCARPINE - UNII:01MI4Q9DI3) PILOCARPINE HYDROCHLORIDE20 mg  in 1 mL
    Inactive Ingredients
    Ingredient NameStrength
    BENZALKONIUM CHLORIDE (UNII: F5UM2KM3W7)  
    HYPROMELLOSE 2910 (4000 MPA.S) (UNII: RN3152OP35)  
    BORIC ACID (UNII: R57ZHV85D4)  
    SODIUM CITRATE (UNII: 1Q73Q2JULR)  
    HYDROCHLORIC ACID (UNII: QTT17582CB)  
    SODIUM HYDROXIDE (UNII: 55X04QC32I)  
    WATER (UNII: 059QF0KO0R)  
    Product Characteristics
    ColorWHITE (Clear Colorless Solution) Score    
    ShapeSize
    FlavorImprint Code
    Contains    
    Packaging
    #Item CodePackage DescriptionMarketing Start DateMarketing End Date
    1NDC: 70069-191-011 in 1 CARTON11/25/2019
    115 mL in 1 BOTTLE; Type 0: Not a Combination Product
    Marketing Information
    Marketing CategoryApplication Number or Monograph CitationMarketing Start DateMarketing End Date
    ANDAANDA21038411/25/2019
    PILOCARPINE HYDROCHLORIDE 
    pilocarpine hydrochloride ophthalmic solution solution/ drops
    Product Information
    Product TypeHUMAN PRESCRIPTION DRUGItem Code (Source)NDC: 70069-201
    Route of AdministrationOPHTHALMIC
    Active Ingredient/Active Moiety
    Ingredient NameBasis of StrengthStrength
    PILOCARPINE HYDROCHLORIDE (UNII: 0WW6D218XJ) (PILOCARPINE - UNII:01MI4Q9DI3) PILOCARPINE HYDROCHLORIDE40 mg  in 1 mL
    Inactive Ingredients
    Ingredient NameStrength
    BENZALKONIUM CHLORIDE (UNII: F5UM2KM3W7)  
    HYPROMELLOSE 2910 (4000 MPA.S) (UNII: RN3152OP35)  
    BORIC ACID (UNII: R57ZHV85D4)  
    SODIUM CITRATE (UNII: 1Q73Q2JULR)  
    HYDROCHLORIC ACID (UNII: QTT17582CB)  
    SODIUM HYDROXIDE (UNII: 55X04QC32I)  
    WATER (UNII: 059QF0KO0R)  
    Product Characteristics
    ColorWHITE (Clear Colorless Solution) Score    
    ShapeSize
    FlavorImprint Code
    Contains    
    Packaging
    #Item CodePackage DescriptionMarketing Start DateMarketing End Date
    1NDC: 70069-201-011 in 1 CARTON11/25/2019
    115 mL in 1 BOTTLE; Type 0: Not a Combination Product
    Marketing Information
    Marketing CategoryApplication Number or Monograph CitationMarketing Start DateMarketing End Date
    ANDAANDA21038411/25/2019
    Labeler - Somerset Therapeutics, LLC (079947873)
    Registrant - Somerset Therapeutics, LLC (079947873)
    Establishment
    NameAddressID/FEIBusiness Operations
    Wintac Limited677236695ANALYSIS(70069-181, 70069-191, 70069-201) , LABEL(70069-181, 70069-191, 70069-201) , PACK(70069-181, 70069-191, 70069-201) , MANUFACTURE(70069-181, 70069-191, 70069-201)
    • © 2024 FDA.report
    This site is not affiliated with or endorsed by the FDA.