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.
2(3 H )-Furanone, 3-ethyldihydro-4-[(1-methyl-1 H -imidazol-5-yl)-methyl]-, monohydrochloride,(3S-cis)-.
PILOPINE HS Gel--Each Gram Contains: Active: Pilocarpine Hydrochloride 4% (40 mg). Preservative Benzalkonium Chloride 0.008%. Inactive: Carbopol 940, Edetate Disodium, Hydrochloric Acid and/or Sodium Hydroxide (to adjust pH) and Purified Water.
Clinical Pharmacology: Pilocarpine 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.
and Usage: Pilocarpine Hydrochloride 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.
Contraindications: Miotics are contraindicated where constriction is undesirable, such as in acute iritis, and in those persons showing hypersensitivity to any of their components.
: For topical use only.
Precautions: 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: 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® Gel 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.
Adverse Reactions: 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 Gel. 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.
Overdosage: 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 may be flushed from the eye(s) with warm tap water.
Dosage and Administration: Apply a one-half inch ribbon in the lower conjunctival sac of the affected eye(s) once a day at bedtime.
How Supplied: PILOPINE HS Gel 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.