NITROGLYCERINE (Nitroglycerinum; synonym: Anginine, Glyceryl trinitrate, Nitrangin, Nitrocardiol, Nitroglycerol, Nitroglyn, Trinitrin, Trinitroglycerol, Trinitrol etc.; GFH, joint venture. B) — anti-anginal means. Trinitrate of glycerin; With 3 H 6 N 3 O 9 :
Colorless oily liquid, low solubility in water, well alcohol-soluble, ether, chloroform. Pier. weight 227,09.
The N reduces a tone of vessels, increases contractility of a myocardium, exerts the oppressing impact on the central component of a sympathetic tone. The central action of N. is shown by reduction of reflex categories in sympathetic nerves and reduction of intensity of the system and regional pressor vasomotor reflexes arising at stimulation of afferent fibers of Aa of group which are carrying out to c. N of page signals of primary pain. Differs in this N. from narcotic analgetik, to-rye reduce a vegetative component not only primary, but also secondary pain. It is supposed that the central effect of N. substantially defines elimination of pain at an attack of stenocardia.
On ability to expand coronary vessels of N. concedes to other anti-anginal drugs and almost does not increase a total coronary blood stream. There are data that N. more expands coronary vessels of large caliber in comparison with vessels of small caliber and arterioles. It is possible that such selectivity of action of N. leads to redistribution of blood from not ischemic sites of a myocardium and to increase due to this blood supply of zones of ischemia what it is connected with, obviously, absence at N.'s use at patients with coronary heart disease of a phenomenon of «burglarizing of a myocardium», to-ry is observed at use of many other coronarodilator drugs (karbokhromen, Dipiridamolum, etc.). Consider that anti-anginal action of N. of hl. obr. it is connected with reorganization of the general hemodynamics, namely with reduction of venous return of blood to heart owing to its deposition in venous system. The vasodilating effect of N. differs from similar effect of other vasodilating drugs in the fact that N. in much bigger degree reduces a tone of venous vessels in comparison with arterial. The phlebectasia along with reduction of resistance in arteries leads to decrease before - both afterloads on heart and to reduction of its metabolic cost. Importance at the same time Ikhmeet the decrease in final diastolic pressure in cardial cavities which is result of reduction of venous return and stimulation of sokratitelny function of a myocardium that promotes improvement of blood supply of the most vulnerable to ischemia of endocardial layers. Exerts the stimulating impact on inotropic function of heart of N. Apparently, N.'s efficiency at the heart failure developing in the acute period of a myocardial infarction is explained by it. On a wedge, to data of a number of researchers, N. at long drop intravenous administration stops heart failure in such cases.
Numerous pilot studies showed that N.'s action on cardiovascular system is substantially connected with influence of drug on adrenergic processes of regulation of blood circulation. The N reduces sensitivity and - adrenoreaktiv-nykh structures of vessels to catecholamines, activity of enzyme of phosphodiesterase oppresses, promoting manifestation of the effects connected with stimulation of ^-adrenoceptors of vessels and hearts and also stimulates release of noradrenaline from the terminations of sympathetic nerves. The central effect is also connected with N.'s influence on adrenergic processes of regulation of blood circulation since it increases the maintenance of free functionally active catecholamines in adrenergic neurons of a brain that leads to strengthening of the descending reticulospinal braking and limits the reflex influences which are carried out through sympathetic department of c. the N
of page H. is well soaked up through mucous membranes and skin. In went. - kish. a path does not collapse. However it renders the most expressed antiangi-nalny effect at sublingual introduction since at this way of introduction it is very quickly soaked up in blood. After N.'s reception inside absorption happens more slowly owing to what the speed of development of anti-anginal action and efficiency of drug decrease. In N.'s organism it is metabolized with formation of nitrites, to-rye are allocated with urine.
N. apply both for stopping of attacks of stenocardia, and for their prevention during the mezhpristupny period. The N can appoint at coronary heart disease irrespective of its weight and a form. In this respect N. favourably differs from other anti-anginal means.
According to a number of scientists, at treatment of coronary heart disease simultaneous use of N. and beta adrenoblockers is especially effective (an anaprilina, etc.). There are instructions on the fact that N. has antiarrhytmic effect at patients with an acute myocardial infarction and can serve as means for prevention of arrhythmias at hron, coronary insufficiency. Sometimes N. apply at a retinal embolism, a spasm of a sphincter of Oddi and to treatment of night tonic spasms of extremities.
For stopping of attacks of stenocardia of N. appoint sublingual in the form of the tablets containing 0,0005 g of drug or in the form of 1% of solution. At the same time 0,5 — 1 tablet is placed under language and held to a full rassasyvaniye. In the form of solution H. apply as follows: 1 — 2 drops of 1% of solution H. apply on language or place under language a piece of sugar with 2 — 3 drops of N. and hold it in a mouth to a full rassasyvaniye.
For prevention of attacks of stenocardia and according to other testimonies of N. appoint usually in the form of 1% of solution inside in the same doses. Besides, for intake in the same purposes use special dosage forms of N. of the prolonged action (so-called drugs of depot nitroglycerine) in the form of the tablets or capsules containing N. in the microencapsulated look. Sustac, Nitrongum in tablets and capsular nitropoppy belong to such drugs of foreign production. N. which is contained in them slowly is allocated and gradually soaked up in went. - kish. a path, in this regard duration of effect of such drugs makes 4 — 6 and more hours.
In the USSR drug Trinitrolongum in the form of the capsules containing polymeric plates with N. and separate polymeric plates with N is developed and offered for practical application. Capsules of Trinitrolongum are intended for intake, a plate — for application on a mucous membrane of an oral cavity. On duration of action Trinitrolongum corresponds to Sustac and can be used for prevention of attacks of stenocardia. It is possible to appoint plates of Trinitrolongum also for stopping of attacks of stenocardia.
There are also messages that for prevention of stenocardia of N. it is effective and in the form of the ointment containing 2% oil solution H. to-ruyu apply on skin of a breast, a stomach or hands within a day through everyone hour
the Highest doses for adults: 1% solution — one-time 4 drops, daily 16 drops; tablets — one-time 1V2 tablets, daily 6 tablets.
Side effect N — a headache, a sonitus, dizziness. In nek-ry cases of N. causes decrease in the ABP up to a collapse.
If necessary for stopping of the collapse caused by N. it is possible to use adrenomimetichesky drugs (adrenaline, etc.).
N. it is contraindicated with the increased intracranial pressure, a hematencephalon. In bvyaz with the fact that N. in high doses causes formation of a methemoglobin it is necessary to appoint with care it the patient suffering from the expressed anemia.
During the work with solutions H. it is necessary to be careful since in case of considerable evaporation of solvent (alcohol) drug becomes explosive.
Forms of release: 1% solution in bottles on 5 ml; the tablets containing 0,0005 g of N. Storage: solution — in well corked bottles in the cool, protected from light place (far from fire), tablets — in the place protected from light.
See also Anti-anginal means .
Bibliography: Kaverina N. V. Pharmacology of coronary circulation, page 220, M., 1963; it, the Principles of modern pharmacotherapy of coronary heart disease, Rubbed. arkh., t. 49, No. 1, page 22, 1977; Clinical pharmacology, under the editorship of V. V. Zakusov, page 194, M., 1978; Pharmacology of monoaminergichesky processes, under the editorship of V. V. Zakusov and N. V. Kaverina, page 195, M., 1971; Kaverina N. V. a. Chumburidze V. Century of Antianginal drugs, Pharmac. Ther., v. 4, p. 109, 1979; The pharmacological basis of therapeutics, ed. by L. S. Goodman a. A. Gilman, p. 729, N. Y. a. o., 1975; Rowe G. G. Responses of the coronary circulation to physiologic changes and pharmacologic agents, Anesthesiology, v. 41, p. 182, 1974.
H. V. Kaverina.