PILOCARPINUM (Pilocarpinum) — m - cholinomimetic means; the alkaloid which is contained in leaves of different types of a plant a jaborandi leaf (Pilocarpus pinnatifolius Jaborandi, etc.). 3-Etil-4-(1-methyl-5-imidazolilmetil) - tetrahydrofuran - 2 - it; With 11 H 16 O 2 N 2 .
Dense, colorless liquid, nonvolatile, bitter taste; easily mixes up with water, alcohol, chloroform; it is not dissolved in ether and gasoline; with to-tami forms crystal salts.
In medical practice apply in the form of hydrochloric salt — Pilocarpinum hydrochloride (Pilocarpini hydrochloridum; synonym: Pilocarpinum hydrochloricum, Pilocarpol etc.; GF H, cn. A); With 11 H 16 O 2 N 2 - HCl:
Colourless crystals or inodorous white crystal powder, we will very easily dissolve in water, it is easily alcohol-soluble; it is hygroscopic. Water solutions (pH 5,0 — 5,5) will sterilize at t ° 100 ° within 30 min.
P. selectively excites m-holinoretseptory of effector bodies and in this regard strengthens secretion of glands (especially salivary and stalemate), raises a tone of smooth muscles of bronchial tubes, a stomach, intestines, bilious and a bladder, a uterus. The item smooth muscles affects more weakly, than glands. P.'s action on eyes is expressed by reduction of a sphincter of an iris of the eye of eyes and a ciliary muscle that leads to narrowing of a pupil, a spasm of accommodation and decrease in intraocular pressure (due to the strengthened outflow of watery moisture), to improvement of a trophicity. Besides, P. promotes expansion of fields of vision thanks to stimulation of peripheral departments of a retina. These effects of P. are most expressed at its topical administration.
Apply Item of hl. obr. in ophthalmologic practice: at glaucoma, 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, at vitreous hemorrhages, and also for the termination of effect of mydriatic means from group of m-holinoblokatorov (atropine, etc.).
The item in the form of water solutions (eye drops) exerts short-term impact on intraocular pressure in this connection in practice often use solutions with addition of the polymeric connections (sodium-carboxymethyl cellulose, methyl cellulose, etc.) prolonging P.'s action by Krome togo, P. appoint in the form of oculentums and special eye films from polymeric materials. 1 and 2% appoint water solutions P. on 1 — 2 drops 3 — 4 times a day, solutions of the prolonged action — on 1 — 2 drops of 1 — 2 time a day; 1 — 2% put pilokarpinovy ointment before going to bed for eyelids, eye films with P. — by means of tweezers for a lower eyelid of 1 — 2 time a day. For reduction of number of instillations of P. it is possible to appoint in combination with others miotocs (see).
At prolonged use of P. emergence or development of dystrophic processes in muscles of an iris of the eye, disturbance of metabolic processes in a retina of an eye is possible.
In cases of acute poisoning of P. with the earliest symptom of its resorptive action strengthening salivary and sweating is. Then there are bradycardia, hypotension, vomiting, a diarrhea, the oppression of mentality, cyanosis and other manifestations characteristic of acute poisonings are observed cholinomimetic substances (see) and antikholinesterazny means (see). The main symptoms of poisoning of P. are stopped by repeated injections of atropine or others a m-cholineregional eye-torov. Besides, subcutaneously enter caffeine, camphor; do artificial respiration (see), warm a body of the patient.
Forms of release: powder; 1 and 2% solutions in bottles on 5 and 10 ml; 1% solution with methyl cellulose in bottles on 5 and 10 ml; 2% solution snatry-carboxymethylcellulose in bottles on 5 and ml; 1 and 2% oculentum; films eye medicinal (Membranullae ophthalmicae cum Pilocarpini hydrochlorido) in cases, on 30 pieces in a case with contents in each film on 2,7 mg of Pilocarpinum of a hydrochloride. Storage: powder — in densely corked banks, saving from dampness; solutions — in well corked container protecting from effect of light; eye films — at t ° 15 — 25 °.
Pilocarpinum in the medicolegal relation
P.'s Poisonings meet seldom, generally at its oral administration. Morfol. changes at court. - a medical research of a corpse are not specific: cyanosis of the person, a sharp miosis, traces of involuntary defecation and an urination, a fluid lungs, foamy slime in a gleam of respiratory tracts. The diagnosis of poisoning of P. as causes of death is based generally on a wedge, manifestations and results court. - chemical researches. From biol, material P. isolate the acidified water or alcohol and extraction by chloroform from the vodnoshchelochny environment or ether from acid and alkaline extraction. For qualitative test of P. use microcrystallic reactions with solutions of gold bromide or platinum chloride (crystals of a characteristic form are formed). Quantitative definition is carried out by methods spektrofotometriya (see) and gas-liquid chromatography (see).
Items use in court. - medical practice for establishment of prescription of approach of death. The way is based on ability of the worrying muscle of a sphincter of an iris of the eye of an eye to answer with reduction introduction to an anterior chamber of an eye to 1% of solution of Pilocarpinum that it is shown by sharp narrowing of a pupil. Test is positive within the first days after approach of death.
Bibliography: The pharmacological basis of therapeutics, ed. by L. S. Goodman a. A. Gilman, N. Y. a. o., 1975.
I. V. Zaikonnikova, A. F. Rubtsov (court. - medical).