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

– Acute attack of angle-closure glaucoma;
– secondary glaucoma; (vascular, post-traumatic (burns)), primary open-angle glaucoma (in combination with beta-blockers or other drugs that reduce intraocular pressure);
– the need for pupil constriction after instillation of mydriatics.

Pharmacological effect

M-cholinomimetic, has miotic and antiglaucoma effects.

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

In primary open-angle glaucoma, instillation of a 1% solution causes a decrease in intraocular pressure by 25-26%. The onset of the effect is after 30-40 minutes, reaches a maximum after 1.5-2 hours and lasts for 4-14 hours.

Extended-release systems of pilocarpine provide control of intraocular pressure for 1 day, while the induced myopia that develops during the first hours quickly decreases and usually does not exceed 0.5 diopters.

Pharmacokinetics

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

The time required to achieve maximum concentration in the intraocular fluid is 30 minutes. Retains in the tissues of the eye, which prolongs its half-life from the tissues of the eye, which is 1.5-2.5 hours.

It is excreted unchanged in the intraocular fluid.
The system with prolonged release of pilocarpine (eye film), wetted by tear fluid, becomes elastic (soft) and is retained in the lower conjunctival fornix until completely dissolved. The release of the active substance begins immediately after contact of the film with the conjunctiva.

Special instructions

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

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

To reduce absorption into the systemic bloodstream, it is recommended to clamp the lacrimal canals for 1-2 minutes after instillation, pressing with a finger at the inner corner of the eye in the area of ​​​​the projection of the lacrimal sac.

After opening, use within 14 days.

In the presence of initial cataracts, the miotic effect can cause a transient deterioration of vision, therefore, during the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Active ingredient

Pilocarpine

Composition

For 1 l
Active substance:
Pilocarpine hydrochloride – 10 g
Excipients:
boric acid – 19 g
water for injection – up to 1 l

Contraindications

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

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

Side Effects

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

With long-term use, the development of follicular conjunctivitis and contact dermatitis of the eyelids is possible. Rarely – nuclear cataract, corneal endothelial edema, keratopathy, retinal detachment.

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

Interaction

Antagonists of pilocarpine hydrochloride are atropine and other m-anticholinergic drugs. When used simultaneously with adrenergic stimulants, antagonism of action (on pupil diameter) may be observed.

Timolol and mesaton enhance the decrease in intraocular pressure, reducing the production of intraocular fluid.

It is possible to use pilocarpine in combination with sympathomimetics, beta-blockers, and carbonic anhydrase inhibitors.

The M-cholinergic stimulating activity of pilocarpine is reduced by tricyclic antidepressants, phenothiazide derivatives, chlorprothixene, clozapine; enhanced by anticholinesterase drugs.

It is possible to develop bradycardia and a decrease in blood pressure during general anesthesia with the use of fluorotane (in patients using pilocarpine in eye drops).

Overdose

In case of an overdose of the drug, persistent miosis, pain in the eye, blurred vision, headache develops, and bronchospasm may develop.
If these symptoms appear, the drug is discontinued and antagonist drugs are instilled – tropicamide, atropine or other derivatives.

Storage conditions

In a place protected from light at a temperature of 2 to 15 °C.
Keep out of the reach of children.

Shelf life

3 years.

Manufacturer

Update of PFC JSC, Russia