Pilokarpin-Darnitsa, cap. глазн. 1%

General characteristics. Structure:

International and chemical names: pilocarpine; (3S,4R) - 3-etil-4-[marked (1-methyl-1H-imidazole-5-silt)] дигидрофурон-2(3Н) - it is a hydrochloride;
main physical and chemical properties: transparent colourless liquid;
structure: 1 ml contains 10 mg of Pilocarpinum of a hydrochloride;
excipients: boric acid, water for injections or water high cleaning.

Pharmacological properties:

Pharmacodynamics. Protivoglaukomny drug for topical administration. At instillation in an eye stimulates m-holinoretseptory of smooth muscles of an iris of the eye and a ciliary body, causing reduction of a circular muscle (miosis) and a tsiliarny muscle (an accommodation spasm). 
When narrowing a pupil there is a shift of a radical part of an iris of the eye from a corner of an anterior chamber that promotes opening of a shlemmov of the channel and fontanovy spaces at closed-angle glaucoma. Reduction of a tsiliarny muscle leads to opening of a shlemmov of the channel and trabecular cracks at an open angle glaucoma. Due to these processes outflow of watery moisture from an anterior chamber of an eye with further decrease in intraocular pressure increases. Decrease in intraocular pressure after use of drug at glaucoma begins in 30-40 minutes, reaches a maximum in 1,5-2 hours and 4-8 hours proceed. 

Pharmacokinetics. Well gets through a cornea, concentration in watery moisture reaches the maximum values in 30 minutes; the elimination half-life makes 1,5-2,5 h of tissues of an eye. It is not metabolized in watery moisture of an eye, but removed at its outflow. Pilocarpinum is quickly hydrolyzed in blood serum and a liver to an inactive form. Plasma elimination half-life of blood - less than 30 min. 

Indications to use:

Open and closed-angle angle glaucoma, including bad attack of glaucoma. For achievement of a miosis (at surgical interventions, with the diagnostic purpose, at overdose of midriatik); for improvement of a trophicity of an eye at fibrinferment of the central vein of a retina, acute impassability of arteries of a retina, an atrophy of an optic nerve, vitreous hemorrhages.

Route of administration and doses:

To unscrew a bottle cover. To dig in on 1 drop of 2-6 times a day in a conjunctival sac of the affected eye by easy pressing a bottle bottom. The mode of dosing and duration of a course of treatment is established individually for each patient depending on weight of glaucoma.
At a bad attack of closed-angle glaucoma dig in on 1 drop each 15 min. for 1 hour, then - in 30 min. and each hour. Further the frequency of instillations is reduced to 6 times a day. If necessary it is possible to combine Pilocarpinum with β-adreno-blokator (Timololum) or inhibitors of a karboangidraza (Diacarbum). For the purpose of decrease in content of water in fabrics use means of osmotic action (urea, a mannitol, a sodium ascorbate, глицерол) and hypotensive drugs inside or parenterally. 

Features of use:

Treatment should be carried out at regular control of intraocular pressure. Pilocarpinum should be applied with extra care at patients with peeling of a retina in the anamnesis and at patients of young age with a myopia. The possible spasm of accommodation influences vision of the remote objects. The miosis can cause disturbance of dark adaptation in this connection use of Pilocarpinum is not recommended to drivers of motor transport, especially in evening and night time. The recommended dose for use of drug does not influence a lactation during the lactogenic period.

Side effects:

The short-term pricking eye pain, burning sensation, hyperemia, dacryagogue, rhinorrhea; myopia, disturbance of twilight sight, accommodation spasm; a headache in temples or periorbital area, indistinct sight, a superficial keratitis. At prolonged use follicular conjunctivitis or contact dermatitis are possible a century.

Interaction with other medicines:

The effect is weakened by holinoblokator of group of atropine. Hypotensive action of Pilocarpinum amplifies at simultaneous use with β-adreno-blokator (Timololum, проксодолол). 

Contraindications:

Iritis, iridocyclitis; a state after ophthalmologic operations; hypersensitivity to Pilocarpinum; pregnancy; children's, teenage and youthful age (up to 18 years).

Overdose:

The most probable symptoms: nausea, bradycardia. A symptomatic treatment, a specific antidote - atropine; at the expressed bradycardia or emergence of an asystolia - 0,5-2 mg of atropine parenterally.

Storage conditions:

To store in the unavailable to children, protected from light place, at a temperature from 8 °C to 15 °C. 

Term storages - 1 year. A period of validity after opening of a bottle - 28 days.

Issue conditions:

According to the recipe

Packaging:

On 5 ml or 10 ml in bottles with the closed covers droppers with control of opening from polymeric material. On 1 bottle in a pack.