Pilocarpine

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT PILOCARPINE

Composition:

active substance: pilocarpine;

1 ml of eye drops contains 10 mg of pilocarpine hydrochloride;

excipients: boric acid, sodium tetraborate, water for injections.

Pharmaceutical form. Eye drops, solution.

Main physicochemical properties: clear, colorless liquid.

Pharmacotherapeutic group.

Medicinal products used in ophthalmology. Antiglaucoma and miotic agents.

ATC code S01E B01.

Pharmacological Properties

Pharmacodynamics

Pilocarpine hydrochloride belongs to M-cholinomimetic agents. Its mechanism of action is based on stimulation of peripheral M-cholinergic receptors, resulting in contraction of the iris sphincter muscle and ciliary muscle, accompanied by pupillary constriction (miosis) and opening of the anterior chamber angle. This enhances outflow of intraocular fluid, thereby reducing intraocular pressure and improving trophic processes in ocular tissues. The reduction in ophthalmotonic pressure reaches 3–4 mm Hg.

Pharmacokinetics

Following instillation onto the conjunctiva, pilocarpine hydrochloride penetrates through the cornea and reaches maximum concentration in the aqueous humor of the eye within 30–40 minutes. The elimination half-life from the eye is 1.5–2 hours, although the effect on intraocular pressure lasts for 4–8 hours. Pilocarpine hydrochloride is not metabolized in ocular tissues; it is eliminated with intraocular fluid and is inactivated by hydrolysis in blood serum and liver. The plasma elimination half-life is 30 minutes.

Clinical characteristics.

Indications.

Primary and chronic open-angle glaucoma. Acute attack of closed-angle glaucoma. Chronic closed-angle glaucoma (prior to surgical intervention). Secondary glaucoma (resulting from central retinal vein thrombosis, acute retinal artery occlusion, optic nerve atrophy, pigmentary retinal degeneration, vitreous hemorrhage). Need for pupillary constriction in cases of mydriatic overdose, for diagnostic purposes, and during surgical procedures (except in individuals with high-degree myopia).

Contraindications.

Hypersensitivity to the components of the drug. Iritis, iridocyclitis, iridocyclitic crisis, uveitis, cyclitis, keratitis, and other eye diseases in which pupillary constriction is undesirable (after eye surgery to prevent formation of posterior synechiae), acute inflammatory diseases of ocular tissues, history of bronchial asthma; paradoxical reaction to the drug in chronic glaucoma.

Interaction with other medicinal products and other types of interactions.

Antagonists of Pilocarpine are atropine and other M-cholinoblocking agents. When used concomitantly with adrenergic stimulants, antagonism of effects occurs (regarding pupil diameter).

Timolol and phenylephrine enhance intraocular pressure reduction (by decreasing production of aqueous humor).

Possible use in combination with sympathomimetics, beta-adrenergic blockers, and carbonic anhydrase inhibitors.

M-cholinostimulating activity is reduced by tricyclic antidepressants, phenothiazine derivatives, chlorprothixene, clozapine; enhanced – by anticholinesterase drugs.

The effect of Pilocarpine may be potentiated by MAO inhibitors and antihistamine agents.

Bradycardia and decreased arterial pressure may occur during general anesthesia with halothane (in patients using Pilocarpine eye drops).

Special precautions for use.

An examination of the fundus should be performed before initiating therapy.

The drug should be used with caution in patients with a history of retinal detachment and in young patients with high myopia.

Immediately before use, hold the bottle in the palm of the hand to warm it to body temperature. Unscrew and remove the cap, then gently squeeze the bottle to instill the solution into the eye. After instillation, securely screw the cap back on.

Miotic agents should be prescribed only in the absence of newly formed blood vessels in the iris.

Increasing the concentration or frequency of instillations (6 or more times) is not advisable, as it does not enhance the hypotensive effect and may lead to systemic adverse reactions.

Pilocarpine hydrochloride has practically no effect on intraocular pressure in healthy individuals, but is effective in patients with various forms of glaucoma. It is recommended to replace Pilocarpine with other non-miotic agents for 1–3 months during the course of a year. With prolonged instillation, miosis persists continuously, which is important for elderly patients with incipient cataract or lens sclerosis.

When using other eye drops concomitantly, the interval between instillations should be at least 15 minutes.

Use with caution in the following conditions:

• Acute heart failure;
• Severe bradycardia;
• Arterial hypotension/hypertension;
• Hyperthyroidism;
• Epilepsy;
• Peptic ulcer;
• Urinary tract obstruction;
• Vasomotor instability;
• Parkinson’s disease;
• As well as in patients who have recently suffered myocardial infarction.

Use during pregnancy or breastfeeding.

Use during pregnancy or breastfeeding is possible only if, in the physician’s opinion, the expected benefit outweighs the potential risk of adverse effects.

Ability to influence reaction speed when driving or operating machinery.

Driving vehicles or engaging in other potentially hazardous activities requiring sharp vision is not recommended during treatment with this drug.

Method of Administration and Dosage

Opening the vial is performed by puncturing the top part of the neck with a twisting motion of the cap until it stops.

Pilocarpine should be instilled into each eye, 1–2 drops, 2–4 times daily. The daily dose and duration of treatment are determined by the physician depending on the level of intraocular pressure. If necessary, the drug may be combined with β-adrenergic blockers.

In acute attacks of angle-closure glaucoma, Pilocarpine should be administered as follows: during the first hour – 1 drop every 15 minutes; during the 2nd–3rd hour – 1 drop every 30 minutes; during the 4th–6th hour – 1 drop every 60 minutes; thereafter – 3–6 times daily until the attack is controlled.

Children. Do not use.

Overdose.

Symptoms: nausea, bradycardia, persistent miosis, eye pain, visual disturbances, headache.

Treatment: discontinue the drug upon appearance of these symptoms. Specific antidote – atropine.

Atropine and tropicamide can be used as specific antidotes. In case of pronounced bradycardia due to overdose of parasympathomimetics, administer 0.5–2 mg of atropine parenterally. Symptomatic therapy.

Adverse reactions.

Eye disorders: ocular discomfort and burning sensation; miosis; accommodative spasm as a result of persistent miosis (during night time); decreased visual acuity; transient eye pain; redness; increased lacrimation; allergic conjunctivitis and eyelid skin dermatitis; ciliary muscle spasm; superficial keratitis; retinal detachment; itching around the eyes; myopia; photophobia; conjunctival hyperemia; corneal edema and erosion; increased pupillary block; hemorrhage into the vitreous body. Prolonged treatment may lead to follicular conjunctivitis, contact eyelid dermatitis, keratopathy, cataract, reversible lens clouding, and changes in conjunctival tissue.

Nervous system disorders: headache in the temples and periorbital areas, tremor, dizziness.

Gastrointestinal disorders: hypersalivation, nausea, vomiting, diarrhea.

Cardiovascular disorders: increased blood pressure, arterial hypotension, bradycardia, cardiac rhythm changes, vascular disturbances.

Skin disorders: increased sweating.

Respiratory, thoracic and mediastinal disorders: bronchospasm, pulmonary edema, rhinorrhea.

When using sustained-release delivery systems – development of tolerance.

Shelf life. 3 years.

Shelf life after opening the bottle – 28 days.

Do not use the medicinal product after the expiry date stated on the packaging.

Storage conditions. Store in a light-protected place at a temperature between 8 °C and 15 °C. Keep out of reach of children.

Packaging. 5 ml or 10 ml in a bottle. 1 bottle per pack.

Prescription status. Prescription only.

Manufacturer. JSC "Pharmak".

Manufacturer's address and place of business.
Ukraine, 04080, Kyiv, Kyrylivska St., 74.