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

Increased intraocular pressure, glaucoma- Acute attack of closed angle glaucoma;
– secondary glaucoma; (vascular, posttraumatic (burns)), primary open angle glaucoma (in combination with beta-adrenoblockers or other drugs that reduce intraocular pressure);
– need for pupil contraction after mydriatic instillation.

Active ingredient

Pilocarpine

Composition

Per 1 liter
Active ingredient:
Pilocarpine hydrochloride – 10 g
Excipients:
boric acid – 19 g
water for injection – up to 1 liter.

How to take, the dosage

The drug is instilled into the conjunctival sac 1 to 2 drops 1-3 times a day. The number of instillations may vary depending on indications and individual sensitivity of a patient.

For treatment of an acute attack of closed-angle glaucoma during the first hour pilocarpine solution is instilled in 1 drop every 15 min, during 2-3 hours every 30 min, during 4-6 hours every 60 min and further 3-6 times a day until the attack is stopped.

If pupil constriction is necessary after mydriatic instillation, 1-2 drops are injected into the conjunctival sac 2-6 times a day.

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

Pilocarpine application is not recommended while wearing soft contact lenses.

In order to decrease absorption into the systemic blood flow it is recommended after instillation to squeeze tear ducts for 1-2 minutes by pressing with the finger at the inner angle of the eye in the projection area of the lacrimal sac.

After opening use within 14 days.

In case of initial cataract myotic effect may cause transient visual impairment. That is why during the treatment period caution shall be exercised while driving motor transport and doing other potentially dangerous activities that require high concentration and quick psychomotor reactions.

Contraindications

Individual sensitivity to the drug components, iritis, cyclitis, iridocyclitis, keratitis, conditions after ophthalmic surgery and other eye diseases in which pupil constriction is undesirable. Children under 18 years of age. Pregnancy, lactation.

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

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

In case of overdose the drug develops persistent miosis, pain in the eye, visual impairment, headache, bronchospasm may develop.
In case of these symptoms the drug is discontinued, instillation of antagonist drugs – tropicamide, atropine or other its derivatives is carried out.