COCAINE (Cocainum; synonym: Cocain, Kokain, Erythroxylin, Kokayeen, Neurocaine) — mestnoanesteziruyushchy means, the alkaloid which is contained in leaves of the South American shrubby plant of Erythroxylon coca Lam, this. Erythroxylaceae. In medical practice use in the form of cocaine of a hydrochloride (Cocaini hydrochloridum, a synonym of Cocainum hydrochloricum; GFH, SI. A); methyl ether of benzoylecgonine hydrochloride; With 17 H 21 NO 4 - HCl.
Colourless acicular crystals or inodorous white crystal powder, bitter taste, the feeling of numbness causes in language. Let's very easily dissolve in water (1:0,5), it is easily alcohol-soluble (1:10), we will dissolve in chloroform and glycerin, it is almost insoluble on air. Water solutions will sterilize tindallization. For stabilization of solutions K. add salt to - that to pH 3,5-4,0.
To. — active mestnoanesteziruyushchy means. Surpasses in activity novocaine (see), at surface anesthesia concedes to Pyromecainum and to Dicainum (see). Has vasoconstrictive effect. To. quickly, however more slowly, than Dicainum, is soaked up by mucous membranes: anesthesia comes in 2 — 5 min. and 10 — 40 min. last (depending on concentration of solution). At influence approximately, except anesthesia and vasoconstriction, To. causes a mydriasis (the maximum of action is observed in 30 — 40 min., reverting in 6 — 8 hours), skoroprokhodyashchy paralysis of accommodation and change of intraocular pressure, a cut can raise in connection with the reduction of m. dilatator pupillae which is followed by disturbance of outflow of liquid from a cavity of an eye in a venous sine of a sclera (helmets the channel) owing to a prelum of spaces of an angle of iris (fontanovy spaces), or to go down in connection with vasoconstriction of the choroid of an eye producing intraocular liquid. In an organism To. almost completely collapses, and only a small part of the entered dose (no more than 5%) is allocated with kidneys in not changed look. To. it is highly toxic: 1% solution by 2 — 3 times toksichny solution of novocaine, Trimecainum and Pyromecainum. On the width of therapeutic action To. concedes to Trimecainum and Pyromecainum, but surpasses Dicainum. Resorptive action To. it is characterized by the expressed influence on c. N of page: drug causes its excitement, then oppression in the beginning. To. exerts the noticeable stimulating impact on adrenergic structures causing increase of reductions of heart, vasoconstriction, braking of a vermicular movement of intestines. In the mechanism of adrenomimetichesky action To. the major role is played by reduction of the return capture of catecholamines (noradrenaline and adrenaline) a presynaptic membrane of nerve termination.
To. apply only for surface anesthesia in ophthalmology, otorhinolaryngology, surgery and urology. For anesthesia of a conjunctiva and a cornea drug is used in the form of 1 — 3% of solutions on 2 — 3 drops in an eye; for anesthesia of mucous membranes of an oral cavity, a nose, a throat — 2% solution; at bronkho-and ezofagoskopiya, bronchographies and in urology — 3 — 5% solutions. To. include in structure of the drops and ointments applied to treatment of rhinitises, sinusitis, conjunctivitis. The highest one-time (and daily) a dose for adult 0,03 g.
For reduction of absorption and decrease in toxicity to 5 ml of solution K. add 3 — 5 drops of 0,1% of solution of Adrenalinum hydrochloricum.
At prolonged use To. causes disturbance of functions of nervous and cardiovascular systems, breath, went. - kish. path; can cause pathological addiction (see. Cocainism ). To. often causes side effects and complications: exfoliating of an epithelium of a cornea, local irritation, sometimes damage of tissues of oral cavity, especially sialadens; at elderly people To. can cause increase in intraocular pressure and a bad attack of glaucoma. Special danger is constituted by the individual intolerance and the general intoxication caused by bystry absorption To. at its drawing on mucous membranes.
Symptoms of poisoning: pallor, dizziness, nausea, vomiting, heartbeat, laryngospasm, faint, collapse, spasms. At intoxication during anesthesia apply oxygen, under skin enter caffeine-sodium benzoate, at spasms — Thiopentalum-natrium (into a vein), carry out symptomatic therapy.
Use To. contraindicated at individual intolerance, glaucoma, diseases of cardiovascular system at advanced age, at bronchial asthma. Appointment To. demands big care, especially at a tonsilectomy and a bronkhoskopiya.
Form of release: powder; store in well corked banks from orange glass in the place protected from light.
See also Anesthetics .
Cocaine in the medicolegal relation
At poisoning To. death comes usually owing to paralysis of a respiratory center. The pathoanatomical picture has no idiosyncrasies.
In an organism To. is exposed to decomposition with formation of an ekogonin therefore the scheme court. - chemical researches on To. it is based on detection of alkaloids: isolation by the acidified water (pH 2,0 — 3,0) or alcohol, then extraction by chloroform from an aqueous phase after alkalifying by solution of ammonia to pH 8,0 — 10,0 and further high-quality detection and quantitative definition. It is possible to make prerefining allocated To. by means of a chromatography in a thin coat of a sorbent. Qualitative tests are based on formation of permanganate of cocaine in the form of red-violet rectangular and square plates. An identification limit — 4 mkg at cultivation 1:10 000. For confirmation of chemical reactions conduct animal experiment (a frog, a white mouse): cause a mydriasis by instillation of an extract in an eye. Quantitative definition is carried out spektrofotometrichesk or fotoelektrokalorimetrichesk on the basis of reaction with dye (bromkrezolovy red, etc.).
Bibliography: Pryanishnikova H. T. The anesthetizing substances, in book: Progress in creation of new pharmaceuticals, under the editorship of D. A. Harkevich, page 227, M., 1973, bibliogr.; Cherkasova E. M and d river. Achievements in chemistry of anesthetics (1961 — 1971), Usp. chemical, t. 42, No. 10, page 1892, 1973, bibliogr.; Sh in and y to about in and M. D. Toxicological chemistry, page 195, M., 1975; Innes I. R. a. Mail hot R. Effect of cocaine on the affinity of a-adreno-receptors for noradrenaline, Brit. J. Pharmacol., v. 48, p. 139, 1973; Isolation and identification of drugs in pharmaceuticals body, fluids and post-mortem material, ed, by E. G. G. Clarke, L., 1971; Trendelenburg U., Graefe K. H. a. Eckert E. The prejunctional effect of cocaine on the isolated nictitating membrane of the cat, Naunyn-Scpmiedeberg’s Arch. Pharmacol., v. 275, p. 69, 1972.
H. T. Pryanishnikova; M. D. Shvaykova (court.).