BEMEGRIDUM (Bemegridum; Ahypnon, Bemegride, Etimid, Eukraton, Glutemisol, Malysol, Megibal, Megimide, Methertharmide, Mikedimide, Pariam, Zentraleptin; GFH, joint venture. B) — analeptical means. 2-Metil-2-etil-glutarimid; With 9 H 13 NO 2 :
White crystal powder, we will dissolve in water (0,5%) and on air a little, it is difficult — in alcohol; pH of 0,5% of aqueous solution — 5,0 — 6,5; t°pl 126 — 128 °; in solution of racks, maintains sterilization at t ° 100 °.
B. it is well soaked up in went. - kish. a path, in hypodermic cellulose and in muscles, however rather high therapeutic concentration in an organism are created only at intravenous administration. Drug is quickly and rather evenly distributed in body tissues therefore its concentration in blood decreases. Contacts blood proteins a little. Works quickly. A part of the entered B. is inactivated by oxidation in a liver, a part is allocated with kidneys in not changed look. Practically has no local action of B.
On the nature of resorptive action is a typical analeptic: exerts the stimulating impact on c. N of page, first of all on a myelencephalon. Most brightly this action is shown at poisoning with somnolent and narcotic substances, and also at respiratory depression. B. is an effective, but not specific antagonist of barbiturates, with to-rymi has a certain similarity in a chemical structure: increases amplitude and frequency of respiratory movements and minute volume of lung ventilation, increases arterial pressure, accelerates recovery of reflexes, a muscle tone and spontaneous movements, getting out of the patient of coma and its awakening; reduces their toxic action. B. weakens also effect of other substances, the oppressing c. N of page. From the effects caused by it the basic is recovery of breath; influence on blood circulation is less expressed and is changeable. The intimate mechanism of action of B. is not found out.
Antagonism between B. and drugs — bilateral, but not competitive.
Apply B. at acute poisonings with barbiturates, and also other hypnotic drugs and narcotic substances and connections oppressing functions of the vital centers of a myelencephalon; for the prevention and elimination of complications, in particular an apnoea, during an anesthesia; for acceleration of removal of inhalation drugs. B.'s use does not exclude and does not replace other actions (artificial ventilation of the lungs, introduction of large amounts of liquid, osmotic diuretics, a hemodialysis, an oxygenotherapy etc.).
B. it can be used also as the provocative agent at elektroentsofalografichesky diagnosis of epilepsy.
Enter B. intravenously (slowly) in the form of 0,5% of solution. Total quantity of the entered solution (from 1 to 70 ml) depends on indications.
For removal of the patient from a condition of an anesthesia solution B. is entered in the separate portions on 5 — 10 — 20 ml every 3 — 5 min. before lasting effect (recovery of breath and reflexes). B. apply only under observation of the doctor. It is necessary to be careful at appointment as his patient with a hypertension and heart failure.
At B.'s overdose the toxic effects caused by its exciting action on c can be observed. N of page: muscular twitchings, a tremor, the increased reflex irritability, a hyperventilation, an eructation, vomiting, kloniko-tonic spasms; cardiac arrhythmias are possible. For stopping of these effects use barbiturates of short-term action (hexenal, Thiopentalum-natrium). B. it is contraindicated at epilepsy, poisoning with the substances increasing convulsive readiness (e.g., derivative a fenotiazina, Reserpinum, carbon dioxide gas).
Form of release: 0,5% sterile solution in ampoules on 10 ml and in bottletight bottles on 30 and 100 ml. Keep in the place protected from light; at storage in solution B. crystals which are dissolved at warming up to t ° 50 ° can be formed.
See also Analeptical means .
Bibliography: Erivantsev N. A. and Svadzhyan E. P. Clinical experience of use of new analeptics of Bemegridum (Megimidum) and Ahypnonum, Eksperim. hir., t. 8, No. 4, page 77, 1963; Kimenis A. A., Brits. And. and Schuster Ja. Ja. Antinarcotic action of Bemegridum and some connections, close to it, Pharm. and toksikol., t. 27, 3, page 278, 1984; Rayevskaya V. V. Use of the Soviet drug of Bemegridum at poisonings with barbiturates, Rubbed. arkh. t. 38, LA 12, page 105, 1984; HabnF. Analeptics, Pharmacol. Rer., v. 12, p. 447, I960; Nanni Costa P. e Giana-s i G. C. Analettici in medicina di urgenza; Acta anaesth. (Padova), 20, p. 371, 1969;
V. Ya. Maximov.