NONAKHLAZIN (Nonachlazinum, synonym Azachlorzin; joint venture. B) — anti-anginal means. 2-Hlor-10-[3-(1,4-diazabitsiklo-(4, 3, 0) - nonalil-4) - propionit] - a fenotiazina dihydrochloride; With 23 H 26 ClN 3 OS-2HCl:
Grayish-yellowish crystal powder, bitter on taste, we will dissolve in water, it is very little alcohol-soluble; t pl 218 — 228 °. Pier. weight 487. Renders expressed, but short (within 3 — 6 min.) influence on a total coronary blood stream, improves a collateral hemodynamics of a myocardium in the conditions of an experimental heart attack, increases blood supply of the center of ischemia of a myocardium due to redistribution of a blood-groove in favor of ischemic area, increases contractility of a myocardium, increases the stroke and minute output of heart. Peripheric resistance and the ABP increase a little after intravenous administration of N., but do not change at its reception inside. Unlike typical N.'s r-hell-renomimetikov does not cause tachycardia. It is connected with its ability to cause a partial block of beta adrenoceptors of heart, and also with direct hinidinopodobny action on a myocardium. Activating adenylatecyclase, N. promotes accumulation of cyclic AMF in a myocardium that leads to development of a positive inotropic effect and acceleration of a glycogenolysis (increase in activity of phosphorylase A in a myocardium). In experiences of in vitro and in vivo H. stimulates oxidizing phosphorylation. In the blood flowing from the center of ischemia the ratio lactate/pyruvate decreases.
The N possesses antiarrhytmic, broncholitic, weak analgetic and tranquilizing action. It is well soaked up from went. - kish. path. The maximum level in blood is reached in 2 hours after intake. From hmochy the hl is removed in insignificant quantity. obr. in the form of metabolites.
N. apply at treatment hron, coronary heart disease, for prevention and stopping of attacks of an angina of exertion and rest, and also against the background of the postponed or current myocardial infarction. For prevention of attacks of N. appoint inside in tablets 0,03 g 3 — 4 times a day. The daily dose can be increased to 0,18 — 0,24 g. The effect develops in 2 — 3 days after an initiation of treatment and is expressed in an urezheniya or the termination of attacks of stenocardia, reduction of number of receptions of nitroglycerine in days, increase in tolerance to an exercise stress. Duration of a course of treatment is 3 — 4 weeks.
Side effects at N.'s use arise very seldom and can be shown by increase in the ABP, a cut it is normalized at drug withdrawal. The N should not be applied at heavy disturbances of functions of a liver and kidneys, and also to combine with beta adrenoblockers.
Form of release: tablets on 0,03 g, coated. Keep in the dry, protected from light place.
See also Anti-anginal means .
Bibliography: Kaverina N. V. The principles of modern pharmacotherapy of coronary heart disease, Rubbed. arkh., t. 49, No., 1, page 22, 1977.
N. V. Kaverina.