ETIMIZOL (Aethimizolum; joint venture. B) — analeptic. An encore - (methylamide) -
1 - an ethylimidazole - 4,5 - dicarbonic to - you; CeH14N402:
White crystal powder. Let's badly dissolve in water, it is alcohol-soluble. Water solutions (pH 6,5 — 7,2) will sterilize at t ° 100 ° within 30 min. Exerts the stimulating impact on subcrustal formations of a brain and the centers of a myelencephalon. At the same time AA. exerts a nek-swarm the oppressing impact on a cerebral cortex. Stimulates adrenocorticotropic function of a hypophysis that leads to increase in level of glucocorticoids in blood.
The mechanism of effect of drug on c. the N of page is connected with activation of puriner-gichesky receptors and increase in level cyclic 3', 5 '-AMF (tsAMF) as a result of activation adenosine - sensitive adenylatecyclase. Besides, E. reduces activity of the phosphodiesterase catalyzing disintegration of tsAMF. Stimulates fabric exchange and promotes synthesis of makroergichesky phosphates. Improves processes of memory and training, and also accelerates reparative processes in fabrics.
It is well soaked up at various ways of introduction and rather evenly distributed in fabrics, easily gets through a blood-brain barrier. It is allocated in the form of metabolites, it is preferential with urine, time of half-decay in an organism after intake makes apprx. 11/2 hour.
Apply E. as a respiratory analeptic at poisonings narcotic and hypnagogues, narcotic analgetics, at an atelectasis slight, craniocereberal injuries. AA. it is effective at asphyxia and postasfiktiche-sky states at newborns. Because E. exerts the stimulating impact on adrenocorticotropic function of a hypophysis, drug can be used for treatment of bronchial asthma and arthritises.
As stimulator of breath E. enter the adult intramusculary or intravenously slowly in the form of 1 — 1,5% of solution at the rate of 0,6 — 1 mg/kg of 1 — 2 time a day. At asphyxia of newborns the drug is administered in an umbilical vein in the form of 0,3% of solution at the rate of
1 mg/kg. At bronchial asthma drug 3 — 4 times a day appoint in the beginning intramusculary по2^ 1,5% of solution 2 times a day, and then inside on 0,1 g. As anti-inflammatory and antiallergenic drug E. appoint inside the adult 0,1 g 3 — 4 times a day within 20 — 30 days.
AA. can cause side effects: nausea, vomiting, concern, dizziness, sleep disorder. In these cases it is recommended to reduce a dose of drug and not to appoint it in the evening. It is contraindicated at a hyperexcitability, sleeplessness.
Form of release: powder; tablets on 0,1 g; ampoules on 3 and 5ml1% or 1,5% of solution. Storage: in the place protected from light.
See also Analeptical means.
Bibliography: Borodkin Yu. S. Anti-feiny, L., 1966; Borodkin Yu. S. and Zaytsev THAT. B. Neurochemical and functional bases of a long-term memory, L., 1982; Broth B. B. and Moreva E. V. Influence of an etimizol on energy balance in a brain, Bulletin ekspery. biol. and medical, t. 83, No. 2,
page 185, 1977; Factory I. S.,
Migas E. A. and Novikov V. P., Molecular bases of action by these is ashes, Pharm. and toksikol., t. 45, Jvfe 2, page 5, 1982; Factory I. S., Mo roar E. V. and Novikova N. A. Influence of neurotropic funds for neurogenic damages of heart, M., 1977; Factory I. S., etc. Klinikofarmakologichesky studying of some neurotropic cure for neurogenic diseases of cardiovascular system and stomach, Pharm. and toksikol., t. 46, No. 3, page 17, 1983; Migas E. A. Pu-rinergichesky action of an etimizol, Bulletin ekspery. biol. and medical, t. 94, No. 9,
page 70, 1982. I. S. Zavodskaya.