Pilocarpinum

General characteristics. Structure:

Active ingredient: pilocarpine;

1 ml of drops contains Pilocarpinum of a hydrochloride 10 mg;

excipients: boric acid, water for injections.

Pharmacological properties:

Pharmacodynamics. Pilocarpinum the hydrochloride belongs to M-cholinomimetic means. The mechanism of action is caused by excitement peripheral M-holinoretseptorov that causes reduction of a circular muscle of an iris and a tsiliarny muscle, is followed by narrowing of a pupil and opening of a corner of an anterior chamber of an eye, improvement of outflow of intraocular liquid that in general causes decrease in intraocular pressure and improves trophic processes in eye tissues. Decrease in intraocular tension reaches 3-4 mm of mercury.

Pharmacokinetics. At instillation on Pilocarpinum conjunctiva the hydrochloride gets through a cornea and as much as possible concentrates in watery moisture of an eye in 30-40 minutes. The elimination half-life from an eye – nevertheless, effect of drug on the level of intraocular pressure proceeds 1,5-2 hours for 4-8 hours. Pilocarpinum the hydrochloride is not metabolized in eye tissues, and removed together with intraocular liquid, inactivated by hydrolysis in blood serum and a liver. Plasma elimination half-life – 30 minutes.

Pharmaceutical characteristics.

Main physical and chemical properties: transparent colourless liquid.

Indications to use:

Primary and chronic open angle glaucoma. Bad attack of closed-angle glaucoma. Chronic closed-angle glaucoma (to surgical intervention). Secondary glaucoma (as a result of thrombosis of the central vein of a retina, acute impassability of an artery of a retina, an atrophy of an optic nerve, a pigmental degeneration of a retina, a vitreous hemorrhage). Need of narrowing of a pupil at overdose of a midriatikama, with the diagnostic purpose and during surgical interventions (except persons with a myopia of high degree).

Route of administration and doses:

Pilocarpinum is dug in in each eye on 1-2 drop by 2-4 times a day. The daily dose and duration of a course of treatment is defined by the doctor depending on the level of intraocular pressure. If necessary drug can be combined with blockers of β-adrenoceptors..........

At a bad attack of closed-angle glaucoma Pilocarpinum is appointed: for the first hour – each 15 minutes on 1 drop; for 2-3 hours – each 30 minutes on 1 drop; for 4-6 hours – each 60 minutes on 1 drop; further – 3-6 times a day before stopping of an attack.

Features of use:

Just before use it is necessary to take a bottle with drug in a palm to warm up to body temperature. The lid is unscrewed, removed and, slightly pressing on the bottle case, dig in solution in an eye. After an instillation the lid is densely screwed up.

With care to apply to the patients with an acute heart failure who are recently postponed a myocardial infarction, heavy bradycardia, arterial hypotension, arterial hypertension, a hyperthyroidism, epilepsy, obstruction of uric ways, vasculomotor instability, Parkinson's disease.

Miotic drugs are used at absence in an iris of neogenic vessels.

Increase in concentration and frequency of instillation (6 and more) – is inexpedient because it does not lead to strengthening of hypotensive effect and causes the general negative reactions of an organism.

Pilocarpinum practically does not influence intraocular tension level at healthy people, but is effective the patient with glaucoma of different forms. It is desirable throughout for about 1-3 years of month Pilocarpinum to replace with other, not miotic drugs. At a long instillation the miosis remains all the time that important for elderly people with a phacosclerosis and a cataract of an initial stage.

Ability to influence speed of response at control of motor transport or work with other mechanisms.

At use of drug driving of motor transport and occupation is not recommended by other potentially dangerous types of activity demanding sight clearness.

Side effects:

During use of Pilocarpinum can develop:

– local by-effects: a miosis, short-term eye pain, reddening, an accommodation spasm as an effect of a resistant miosis (during the night period of days), decrease in visual acuity, a headache in temples and paraorbital areas, the strengthened dacryagogue, allergic conjunctivitis and dermatitis of skin a century, a superficial keratitis, an itch in eyes, a myopia, photophobia, a conjunctiva hyperemia, hypostasis and an erosion of a cornea, a spasm of a tsiliarny muscle; occasionally – peeling of a retina;

– system by-effects develop very seldom: a bronchospasm, a headache, dizziness, hypersalivation, a rhinorrhea, a fluid lungs, increase in arterial pressure, bradycardia, vascular disorders, arterial hypotension, the increased perspiration, nausea, vomiting, diarrhea;

– prolonged treatment can lead to follicular conjunctivitis, contact dermatitis a century, to a keratopathy, a cataract, a reversible cataract, changes of conjunctival fabric.

Interaction with other medicines:

Atropine and other M-cholinolytic drugs are antagonists of Pilocarpinum. At simultaneous use with adrenostimulyator antagonism of action (influence on diameter of a pupil) can be observed.

Timololum and phenylephine hydrochloride strengthen decrease in intraocular pressure.

Use of Pilocarpinum in a combination with β-adrenoblockers, karboangidraza inhibitors is possible.

M-holinostimuliruyushchee action of Pilocarpinum decreases at a combination with the tricyclic antidepressants derivative of a fenotiazin, chlorprothixene, clozapine; amplifies antikholinesterazny drugs.

Developing of bradycardia and lowering of arterial pressure is possible during the general anesthesia using Ftorotanum (at patients who apply Pilocarpinum in eye drops).

Contraindications:

Iritis, iridocyclitis, iridotsiklichesky crisis, uveitis, cyclitis, keratitis and other diseases of an eye at which narrowing of a pupil is not desirable (after surgical interventions on an eye for prevention of emergence of back synechias). Paradoxical reaction to drug at a congestive form of glaucoma.

Pilocarpinum should be applied carefully the patient with peeling of a retina in the anamnesis, to persons of young age with a myopia of high degree. Acute inflammatory diseases of tissues of eye. Allergic reactions to components of drug and bronchial asthma in the anamnesis.

Overdose:

The first symptoms of overdose – nausea, bradycardia, can develop a resistant miosis, eye pain, a vision disorder, a headache. With the advent of these symptoms drug is cancelled. Overdose treatment symptomatic. Atropine, тропикамид can be applied as specific antidotes. At the expressed bradycardia because of overdose of parasympathomimetics enter 0,5-2 mg of atropine parenterally.

Use during pregnancy or feeding by a breast.

Use during pregnancy or feeding by a breast perhaps only if, according to the doctor, the expected effect exceeds risk of possible side reactions.

Children.

Drug is not used to children.

Storage conditions:

Period of validity. 3 years. After opening of a bottle drug is good 28 days. Not to apply after the termination of the period of validity specified on packaging. To store in the place protected from light at a temperature from 8 °C to 15 °C. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

On 5 ml or 10 ml in a bottle. On 1 bottle in a pack.