Oftan^® Pilocarpin (Drops) Instructions for Use

Marketing Authorization Holder

Santen, Oy (Finland)

ATC Code

S01EB01 (Pilocarpine)

Active Substance

Pilocarpine (BAN)

Dosage Form

Oftan® Pilocarpine

Eye drops 1%: dropper bottle 10 ml

Dosage Form, Packaging, and Composition

Eye drops 1% as a clear, colorless solution.

Excipients: benzalkonium chloride, polyvinyl alcohol, citric acid, sodium citrate, water for injections.

10 ml – plastic dropper bottles (1) – cardboard packs.

Clinical-Pharmacological Group

Antiglaucoma drug – m-cholinomimetic

Pharmacotherapeutic Group

Antiglaucoma agent – M-cholinomimetic

Pharmacological Action

M-cholinomimetic, a methylimidazole derivative. It has a direct m-cholinomimetic effect.

When used topically in ophthalmology, it causes pronounced miosis, spasm of accommodation, and reduces intraocular pressure.

The reduction in intraocular pressure is due to the contraction of the ciliary muscle and the iris muscle, which leads to the widening of the anterior chamber angle and changes the physical structure of the trabecular meshwork, facilitating the outflow of aqueous humor.

Pharmacokinetics

Pilocarpine penetrates the cornea well and is well absorbed through the conjunctiva. It is practically not absorbed in the conjunctival sac.

When applied topically, C_max in the aqueous humor of the eye is reached 30 minutes after instillation.

Pilocarpine binds to many eye tissues. T_1/2 from the eye media is 1.5 – 2.5 hours.

Pilocarpine is not metabolized in the eye tissues and is excreted unchanged with the intraocular fluid.

It is converted to an inactive form by hydrolysis in blood serum and the liver. T_1/2 from plasma is about 30 minutes.

Indications

Acute attack of angle-closure glaucoma, secondary glaucoma (vascular, post-traumatic), primary open-angle glaucoma (in combination with β-blockers or other drugs that reduce intraocular pressure). The need to constrict the pupil after the instillation of mydriatics.

ICD codes

Dosage Regimen

Instill the drops into the conjunctival sac. The regimen is set individually based on the indication and severity of the condition.

For an acute attack of angle-closure glaucoma, instill one drop into the affected eye every 5 to 10 minutes for three to six doses, then reduce to one drop every 1 to 3 hours until the attack resolves.

For chronic open-angle glaucoma and other chronic forms, the usual dose is one drop applied to the affected eye(s) up to four times daily. The frequency of administration may be adjusted based on the patient’s response.

For post-mydriatic miosis, instill one drop into the eye(s) that received the mydriatic agent.

To minimize systemic absorption, apply gentle pressure to the lacrimal sac at the inner corner of the eye for 1 to 2 minutes immediately after instillation.

Avoid allowing the dropper tip to contact the eye, eyelids, or any other surface to prevent contamination of the solution.

If using other topical ophthalmic agents, administer them at least 5 minutes apart from Pilocarpine.

Adverse Reactions

Possible headache, short-term pain in the eye area; myopia; decreased vision, especially at dusk, lacrimation, rhinorrhea, superficial keratitis, allergic reactions; with prolonged use – follicular conjunctivitis, contact dermatitis of the eyelids, reversible lens opacity.
Rarely: systemic reactions – bronchospasm, slowing of the heart rate, increased secretion of the salivary glands, rhinorrhea.

Contraindications

Hypersensitivity to pilocarpine; iritis, iridocyclitis; conditions in which miosis is undesirable (for example, after eye surgery, except in cases where it is necessary to constrict the pupil immediately after surgery to prevent the formation of synechiae); retinal detachment (including in the anamnesis) and conditions predisposing to retinal detachment; children and adolescents under 18 years of age.

With caution in young patients with high myopia.

Use in Pregnancy and Lactation

During pregnancy and breastfeeding, it should be used only after consultation with a doctor, in cases where the intended benefit to the mother outweighs the potential risk to the fetus or infant.

Pediatric Use

Contraindicated for use in children and adolescents under 18 years of age.

Special Precautions

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

To prevent pilocarpine from entering the systemic circulation, it is recommended to press a finger on the inner corner of the eye for 1-2 minutes after instillation.

The use of pilocarpine is not recommended when wearing soft contact lenses.

In the presence of incipient cataract, the miotic effect may cause transient visual impairment.

Effect on the ability to drive vehicles and mechanisms

Miosis can cause impaired dark adaptation. After instillation of pilocarpine, caution should be exercised when driving vehicles at night or in poor lighting conditions. At the very beginning of treatment, young patients may develop a spasm of accommodation, which may lead to decreased visual acuity.

Drug Interactions

Antagonists of pilocarpine are atropine and other m-cholinoblockers. When used concomitantly with adrenomimetics, antagonism of action may be observed.

Timolol and phenylephrine enhance the reduction of intraocular pressure by reducing the production of intraocular fluid.

Pilocarpine can be used in combination with sympathomimetics, β-blockers, carbonic anhydrase inhibitors.

The m-cholinomimetic activity of pilocarpine is reduced by tricyclic antidepressants, phenothiazine derivatives, chlorprothixene, clozapine; it is enhanced by cholinesterase inhibitors.

The development of bradycardia and a decrease in blood pressure is possible during general anesthesia with halothane in patients using Pilocarpine eye drops.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

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.