Pilocarpine Renewal, eye drops 1% 5 ml

M-cholinomimetic, has myotic and anti-glaucoma effect.

Causes contraction of the circular (miosis) and ciliary muscles (accommodation spasm), increases anterior chamber angle (iris root is retracted), increases permeability of the trabecular zone (trabecula is stretched and blocked areas of Schlemm’s canal are opened), improves outflow of aqueous humor from the eye and eventually reduces intraocular pressure.

In primary open-angle glaucoma instillation of 1% solution decreases intraocular pressure by 25-26 %. The effect starts after 30-40 minutes and peaks after 1.5-2 hours and lasts for 4-14 hours.

Systems with prolonged pilocarpine release provide control of intraocular pressure for 1 day while induced myopia occurring during the first hours decreases rapidly and usually does not exceed 0.5 diopters.

Pharmacokinetics

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

Time required to reach maximum concentration in the intraocular fluid is 30 min. It is retained in eye tissues which prolongs its half-life period from eye tissues which is 1.5-2.5 h.

It is eliminated unchanged with intraocular fluid.
The system with prolonged pilocarpine release (eye film) is wetted with lacrimal fluid and transformed into elastic (soft) state and is kept in the lower conjunctival arch until complete dissolution. The release of the active ingredient begins immediately after the film comes into contact with the conjunctiva.

Indications

Active ingredient

Composition

How to take, the dosage

Interaction

Atropine and other m-cholinoblocking agents are antagonists of pilocarpine hydrochloride. Antagonism of action (on pupil diameter) may be observed when used concomitantly with adrenostimulants.

Timolol and mesaton increase the decrease in intraocular pressure by reducing intraocular fluid production.

Pilocarpine may be used in combination with sympathomimetics, beta-adrenoblockers, and carboangiradase inhibitors.

M-cholinostimulatory activity of pilocarpine is reduced by tricyclic antidepressants, phenothiazid derivatives, chlorprotixen, clozapine; it is enhanced by anticholinesterase agents.

Bradycardia and decreased arterial blood pressure may develop during general anesthesia with fluorotonan (in patients using pilocarpine in eye drops).

Special Instructions

Contraindications

Side effects

Visually: local reactions – pain in the eye area; myopia, decreased vision, especially in the dark (due to the development of persistent myosis and accommodation spasm); lacrimation, superficial keratitis.

In prolonged use it is possible to develop follicular conjunctivitis, contact dermatitis of the eyelids. Rarely – nuclear cataract, corneal endothelial edema, keratopathy, retinal detachment.

Systemic: headache (temporal or periorbital areas), rhinorrhea, bronchospasm, hypersalivation, vomiting, diarrhea, increased or decreased blood pressure, allergic reactions.

Overdose