CORAZOLUM (Corazolum; synonym: Cardiazol, Leptazol, Metrazol, Pentamethazolum, Pentetrazolum, Pentylentetrazol, Tetracor; GFH, joint venture. B) — analeptical means. 1,5-Pentametilentetrazol; With 6 H 10 N 4 :
Inodorous white crystal powder, we will very easily dissolve in water, alcohol and chloroform, it is ether-soluble, t ° pl 58 — 61 °.
To. exerts the stimulating impact on the center of breath and a vasomotor center. Strengthening of breath and increase in the ABP under influence To. are more expressed if the bulbar centers are in a condition of oppression. On action on c. N of page. To. is an antagonist narcotic and hypnagogues. In high doses causes spasms, preferential clonic character. Developing of spasms is caused generally by influence To. on excitability of supraspinal structures of c. N of page and to a lesser extent action on a spinal cord. In experimental pharmacology korazolovy spasms use as the test by search and studying of anticonvulsants. A promoting effect To. on c. by N of page it is connected, apparently, with increase under its influence of permeability of membranes of nervous cells for potassium ions that leads to partial depolarization of membranes and increase in their excitability. On mechanisms pre-and postsynaptic braking in c. N of page. To. does not influence.
To. it is easily soaked up from went. - kish. a path, a hypodermic fatty tissue and muscles, it is evenly distributed in fabrics. In an organism quickly is exposed to an inactivation (preferential in a liver). Transmutation products To. do not possess pharmakol, activity and are removed generally by kidneys.
Apply To. hl. obr. at oppression of cardiovascular system and breath. At shock, asphyxia, falling of cordial activity, etc. drug is entered intravenously (slowly) on 1 ml of 10% of solution. Further in case of need enter subcutaneously or intramusculary 1 — 2 more ml of the same solution. At the menacing asphyxia of a fruit To. enter to women in labor on 1 ml 10% of solution (intravenously or intramusculary). It must be kept in mind, however, that therapeutic value To. as stimulator of breath it is rather low. At poisonings with opiates it is more reasonable to apply specific antagonists of these means (e.g., Nalorfinum, etc.). It is also necessary to consider that To. and other analeptics can increase the need of a brain for oxygen and by that to promote development of a secondary hypoxia.
Sometimes To. apply to convulsive therapy of schizophrenia. For this purpose 3 — 5 ml of 10% of solution K. enter intravenously (through a needle of a large diameter) with a speed of 1 ml during 1 sec. (the dose used at the same time exceeds the highest single dose). The convulsive attack comes during an injection or in 15 — 20 sec. after it. If from the specified dose the attack of spasms does not develop, then at the following injection the dose is increased by 0,5 — 1 ml of 10% of solution. During the performing convulsive therapy it is necessary to take measures for prevention at the patient of injuries.
The highest doses To. for adults inside, under skin and in a vein: one-time 0,2 g, daily 0,5 g.
To. it is contraindicated at severe damages of heart, pulmonary diseases, especially at tuberculosis in an active form, acute feverish states, predisposition to convulsive reactions.
Forms of release: powder, tablets on 0,1 g and ampoules on 1 ml of 10% of solution. Store in the place protected a reflected light.
See also Analeptical means .
Bibliography: Luzhniki E. A., Dagayev V. N. and F and r with about in H. H. Fundamentals of resuscitation at acute poisonings, M., 1977, bibliogr.; The pharmacological basis of therapeutics, ed. by L. S. Goodman a. A. Gilman, p. 363, L., 1975.
V. V. Churyukanov.