Pilocarpine Prolong (Drops) Instructions for Use

Marketing Authorization Holder

Sintez PJSC (Russia)

ATC Code

S01EB51 (Pilocarpine in combination with other drugs)

Active Substances

Pilocarpine (BAN)

Hypromellose (Rec.INN)

Dosage Form

Pilocarpine Prolong

Eye drops 10 mg+4.3 mg/1 ml: dropper bottle 5 ml

Dosage Form, Packaging, and Composition

Eye drops transparent or slightly opalescent, colorless or slightly colored, viscous.

Excipients: disodium edetate – 0.1 mg, benzalkonium chloride – 2 mg, boric acid – 10 mg, water for injections – up to 1 ml.

5 ml – polymer dropper bottles (1) – cardboard packs.

Clinical-Pharmacological Group

Antiglaucoma drug – m-cholinomimetic

Pharmacotherapeutic Group

Antiglaucoma agent – M-cholinomimetic

Pharmacological Action

Antiglaucoma drug. The drug contains two active substances: pilocarpine hydrochloride and Hypromellose (hydroxypropyl methylcellulose).

Pilocarpine is an m-cholinomimetic that has a miotic effect. It causes contraction of the circular and ciliary muscles, which is accompanied by pupil constriction and widening of the anterior chamber angle. As a result, the outflow of aqueous humor improves and intraocular pressure decreases. In primary open-angle glaucoma, instillation of a 1% solution causes a decrease in intraocular pressure by 17-20% from the baseline. The onset of the drug’s effect is within 10-30 minutes, reaches a maximum in 1.5-2 hours, and lasts for 4-6 hours.

Hypromellose has a lubricating and softening effect on eye tissues; it reduces the locally irritating effect of pilocarpine. Possessing high viscosity, Hypromellose increases the duration of contact of the pilocarpine solution with the cornea.

Pharmacokinetics

Pilocarpine penetrates the cornea well. T_max in the intraocular fluid is 30 minutes. It is retained in the eye tissues, which prolongs its T_1/2, which is 1.5-2.5 hours. It is excreted with the intraocular fluid and undergoes partial metabolism in the blood plasma.

Hypromellose prolongs the T_1/2 of pilocarpine from the eye tissues.

Indications

• Acute attack of angle-closure glaucoma;
• Secondary glaucoma (vascular, post-traumatic, e.g., burns);
• Primary open-angle glaucoma (as monotherapy and in combination with beta-blockers or other drugs that reduce intraocular pressure);
• Chronic angle-closure glaucoma;
• When pupil constriction is necessary after instillation of mydriatics (except for persons with high myopia).

ICD codes

Dosage Regimen

Instill 1-2 drops into the conjunctival sac 1-3 times/day. The number of instillations may vary depending on the indications and individual sensitivity of the patient.

For the treatment of an acute attack of angle-closure glaucoma, instill 1 drop of the pilocarpine solution every 15 minutes during the first hour, every 30 minutes during hours 2-3, every 60 minutes during hours 4-6, and then 3-6 times/day until the attack is relieved.

A combination with adrenomimetics, beta-blockers, and carbonic anhydrase inhibitors is possible.

Adverse Reactions

From the organ of vision local reactions – eye pain; myopia; decreased vision, especially at night (due to the development of persistent miosis and accommodation spasm); lacrimation, superficial keratitis. With prolonged use, the development of follicular conjunctivitis and eyelid contact dermatitis is possible. Rarely – nuclear cataract, corneal endothelial edema, keratopathy, retinal detachment.

Systemic reactions headache (in the temporal or periorbital areas), rhinorrhea, bronchospasm, hypersalivation, vomiting, diarrhea, increase or decrease in blood pressure, allergic reactions.

Contraindications

• Iritis;
• Cyclitis;
• Iridocyclitis;
• Keratitis;
• Condition after ophthalmic surgeries and other eye diseases in which pupil constriction is undesirable;
• Age under 18 years;
• Hypersensitivity to pilocarpine.

With caution: in patients with a history of retinal detachment and in young patients with high myopia.

Use in Pregnancy and Lactation

Use during pregnancy is contraindicated. If necessary to prescribe during lactation, breastfeeding should be discontinued during treatment.

Pediatric Use

Contraindicated in children under 18 years of age.

Special Precautions

Treatment should be carried out with regular monitoring of intraocular pressure.

To reduce absorption into the systemic circulation, it is recommended to compress the lacrimal canaliculi for 1-2 minutes after instillation by pressing a finger at the inner corner of the eye in the area of the lacrimal sac projection.

Effect on the ability to drive vehicles and mechanisms

In the presence of incipient cataract, the miotic effect may cause transient visual impairment (a feeling of myopia), so caution should be exercised when driving and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions during the treatment period.

Overdose

In case of accidental ingestion, it manifests as a significant increase in m-cholinomimetic effects, including the development of severe cardiovascular failure and bronchoconstriction.

Treatment: gastric lavage, administration of atropine (0.5-1 mg subcutaneously or intravenously), epinephrine (0.3-1 mg subcutaneously or intramuscularly), as well as a sufficient amount of fluid.

Drug Interactions

Antagonists of pilocarpine are atropine and other m-cholinoblocking agents.

When used concomitantly with adrenomimetics, antagonism of action (effect on pupil diameter) is noted.

Concomitant use with adrenomimetics (including phenylephrine), beta-blockers (including timolol), and carbonic anhydrase inhibitors enhances the reduction of intraocular pressure.

The m-cholinomimetic activity of pilocarpine decreases when combined with tricyclic antidepressants, phenothiazine derivatives, chlorprothixene, clozapine; it increases when combined with cholinesterase inhibitors.

The development of bradycardia and a decrease in blood pressure is possible during general anesthesia with halothane.

Storage Conditions

The drug should be stored out of the reach of children, protected from light, at a temperature from 15°C (59°F) to 25°C (77°F). Do not freeze.

Shelf Life

Shelf life – 2 years.

Dispensing Status

The drug is dispensed by prescription.

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.