SCOPOLAMINUM (Scopolaminum) — holinoblokiruyushchy means; alkaloid of a scopolia, belladonna, henbane, dope and other plants this. solanaceous (Solanaceae). In the chemical relation is ester of a skopin and tropic to - you:
In medical practice apply Scopolaminum hydrobromide (Scopolamini hydrobromidum; synonym: Scopolaminum hydrobromicum, Hyoscini hydrobromidum; GFH, joint venture. A); L - 0-tropoilskopina hydrobromide; With 17 H 21 NO 4 • HBr • 3H 2 0.
Colourless transparent crystals or white crystal powder. Let's easily dissolve in water, it is alcohol-soluble, we will dissolve in chloroform very little; t°pl 192 — 196 °; pier. weight (weight) 438,3. Water solutions (pH 2,8 — 3,0) will sterilize at t ° 100 ° within 30 min.
On a chemical structure and properties it is close to to atropine (see), the m-holinoblokiruyushchey has activity. On peripheral effects it is similar to atropine, but works less for a long time. Is stronger, than atropine, blocks m-holinoretsepto-ry of an iris, a ciliary body and nek-ry excretory (salivary, bronchial, stalemate) glands, but concedes to atropine on influence on m-holinoretseptory of heart, smooth muscles of bronchial tubes and intestines. Differs from atropine on influence on c. N of page. In therapeutic doses of S. usually has sedative effect, causes decrease in a physical activity, drowsiness, reduces duration of a «paradoxical» dream. The village has the expressed antiemetic activity (see. Antiemetics ), caused, obviously. its oppressing action on the emetic and vestibular centers and peripheral m-holinoblokiruyushchimi properties. Renders protivoparkinsonichesky effect.
Being basic nitrile, S. well gets through gistogema-tichesky barriers (hematoencephalic, placental, etc.) and is easily soaked up at various ways of introduction. At intake it is soaked up preferential from a small bowel. From a stomach it is soaked up badly as in acid medium it is almost completely ionized. It is brought out of an organism generally in the form of the metabolites which are formed in a liver. In not changed view with urine it is allocated apprx. 1% of the entered dose.
Page. apply as an antiemetic at so-called diseases of the movement, napr, at sea and aeroembolism. At nausea and vomiting of other genesis it is ineffective. As an antiemetic (is more often for this purpose appoint the tablets «Aeronum») S. use hl. obr. preventively, since at the developed symptoms its efficiency is much lower.
In S.'s neurology sometimes appoint for treatment of parkinsonism (generally at a trembling form), in anesthesiology as means for premedication before an anesthesia, in ophthalmology as mydriatic means (see) at irites, iridocyclites and in the diagnostic purposes instead of atropine.
Page. appoint inside the adult on 0,00025 — 0,0005 g on reception, subcutaneously on 0,5 — 1 ml of 0,05% of solution and as eye drops in the form of 0,25% of water solution.
The highest doses for adults inside and under skin: one-time — 0,0005 g, daily — 0,0015 g
of S. causes the same side effects, as atropine (a mydriasis, paralysis of accommodation, tachycardia, dryness in a mouth, etc.). Besides, the effects connected with its sedative action (slackness, drowsiness) are characteristic of it. In some cases S. in therapeutic doses can cause excitement, concern, hallucinations or nonsense.
Acute poisoning of S. on a wedge, a picture is similar to poisoning with atropine. First aid and treatment at S.'s poisoning same, as well as at poisoning with atropine (see. Poisonings, table ).
Like other m-holinoblokatoram of S. it is contraindicated at glaucoma and adenoma of a prostate.
Forms of release: powder; ampoules on 1 ml of 0,05% of solution. Store in the place protected from light. For use in Ophthalmolum. to practice along with 0,25% solution drug of the prolonged action — 0,25% solution of Scopolaminum of hydrobromide with methyl cellulose is produced (Solutio Scopolamini hydrobromidi 0; 25% of cum Methylcellulosa).
The page is a part of the tablets «Aeronum» (Tabulettae «Aeronum»; joint venture. B), the camphorate 0,0001 g containing Scopolaminum and Hyoscyaminum of camphorate 0,0004 g (see. Hyoscyaminum ). The tablets «Aeronum» appoint at sea and aeroembolism on 1 — 2 tablets in 30 — 60 min. - to a trip, if necessary in 6 hours — one more tablet, and also sometimes for the purpose of reduction salivary and a slizeotdeleniya at plastic surgeries on a face and upper airways operations on 2 tablets in 20 — 30 min. prior to operation.
See also Cholinolytic substances .
Bibliography: The pharmacological basis of therapeutics, ed. by A. G. Gilman a. o., p. 120, N. Y., 1980.
E. Yu. Lemina.