Pilocarpine

Chemical name

(3S-цис)-3-Этилдигидро-4-[ (1-метил-1H-имидазол-5-ил )метил]-2(3H)-фуранон (and as hydrochloride or ammonium)

Gross

C11-H16-N2-O2

Characteristics

D. plants Pilocarpus pinnatifolius Jaborandi. Clear crystals or white crystalline powder and odourless, with gorkovatam taste; Gigroskopichen are easily soluble in water, easily-in spirit nerastvorim most nonpolar solvents; Aqueous solutions have pH 5-5,5.

Of drugs

The drugs-protivoglaucomnoe. Muskarinove stimulates receptors smooth muscles, incl. iris and digestive glands, bronchitis, external glands (salivary, port, etc.). The reduction circular (cramps) and ciliarna (patients ccomodation) Myshc.pri ingestion rapidly absorbed, the time of C_max is about 60 minutes. Metabolised in neurotransmission and in the plasma. T_1/2 at 0.76 h increases with the dose. Excreted mainly kidneys in the urine is found in an unmodified form and in the form of metabolites. In kongungualnom bag barely absorbed enough to be of general application. The prolonged release of the active ingredient (Ophthalmic film), smachivayasi slezna fluid nabuhaut and retained in the lower kongungualnom set. Releasing pilocarpina begins immediately after contact with the film Kongyunctiva.pri zakratougolna glaucome big exception is the offset iris angle from the front of the camera and to the opening of schlemmovykh channels and fontanovykh spaces. Patients who are open - glaucoma also offers schlemmov channel and trabekuliarnae slits and increases ciliarna tone muscles. In primary open-glaucome or ocular hypertension time backfilling 1% solution reduces vnutriglaznogo pressure on the 25-26%. Begins after one 30-40 minutes, reaches its maximum in 1.5-2 hours and lasts 4-8 hours Systems with the release of a long pilocarpina monitor vnutriglaznogo pressure within 1 day, and growing for the first time miopia induced decreases rapidly, and usually does not exceed 0.5 eye.

Indications

Glaucoma, incl. acute attack, a breach of trophic eye under tromboze central retinal vein or acute obstruction of arteries atrophy nerve membranes, in krovoislianiah steklovidne body, the removal of midriaticski atropine, gomatropina, Skopolamina.tabletki : dry mucous membranes of the mouth (xerostomia).

Contraindications

Hypersensitivity, and the exacerbation of asthma irit, iridotsyklit, condition after eye operations, the unaccounted for otsloicu retina, miopia high degree of the risk otslaki retina, zakratougolnaya glaucoma, pregnancy, child, adolescent and youth age (up to 18 years).

Side-Effects

Headache in visochnykh or periorbitalnah areas pain in the eyes, miopia, patients ccomodation, clear view of the twilight, slezotechenie, rinorea, follikuliarny conjunctivitis, superficial keratit contact dermatitis Century (rarely). The ingestion may also be sweating, fever, nausea, vomiting, diarrhoea, pain in the abdomen, disfagia, change of voice, difficulty in breathing, dizziness, fatigue, a sense of the tide of blood to a person aetiology, tachycardia, the AV conduction, hypertension or gipotenzia, increases urination, increased AD.

Patient interaction

The effect is weakened (end) holinomimetikami group atropine. Timolola maleinat and mezaton (reduced products vnutriglazna liquid) potenziruut decline vnutriglaznogo pressure. Perhaps increased side effects бета-адреноблокаторо�� (expressed aetiology, violations vnutriserdecna conductivity). Coupled with adrenomimetikami is mutual antagonism (by the pupil). M-holinomimetical activity declining tricyclic antidepressants, derivative fenotiazina, hlorprotiksenom, clozapinom rise antiholinesteraznami means. Perhaps the bradikardii and hypotension during ftorotanovogo narcosis in patients receiving pilocarpinom hydrochloride in eye drops.

Overdosing

There is a significant increase in m-holinomimeticakih effects including with the development of severe heart problems and bronhokonstriktion. Treatment includes washing the stomach, monitoring HR, AD respiratory functions, the introduction of atropine (0.5-1.0 mg p / to or / in), epinephrine (0.3-1.0 mg p / to or / m), as well as a sufficient amount of liquid.

Precautions

A regular monitoring vnutriglaznogo pressure. In order to reduce the intake of putting that 1-2 minutes perejimati slezny channel pull finger in a cat's eye. It should teach the patient use of a long-release drug and warn that the long-term use may develop tolerance. During treatment desirable refusal to breastfeed. Be wary appoint employees driving cars and other potentially hazardous activities that require a clear view, the increased attention and high speed response.

Dosing and Administration

In ophthalmic practice, the 1% or 2% solution 2-3-4 times a day at designated 5% and 6% solution. Before the night is over the mortgage held 1% or 2% ointment. The extended release pilocarpina (eye film) 20 µ g or 40 µ g designate where to normalize vnutriglaznogo pressure is not enough 3-4-razovogo backfilling per day; a film by pinceta Eye for the lower cat 1-2 times a day (in the immediate aftermath of this should retain eye-trailer during the 30-60 as a smachivanie films and the shift in the soft). Answers : inside, during or after delivery, squeezed one glass of water, to 5 mg three times daily (last admission combined with the evening reception food); Course 4-8 weeks. The maximum daily dose of 30 mg.

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