THEOBROMINE (Theobrominum; synonym: Theostene, Thesal etc.; GFH, joint venture. B) — vasodilating, broncholitic and diuretic; the alkaloid which is contained in seeds of cocoa (Semina Cacao). 3,7 Dimethylxantine; With 7 H 8 N 4 O 2 :
Inodorous white crystal powder, bitter taste. We will dissolve in a cold water (1:700) very little, it is not enough — in hot water, we will dissolve in 95% alcohol, ether and chloroform very little, we will easily dissolve in divorced to-takh and alkalis; pier. weight (weight) 180,17.
On a chemical structure and pharmacological properties it is close to to caffeine (see) and to other alkaloids from group of derivatives of purine. Stimulates cordial activity, increases cordial emission. Strengthening of cardiac performance under the influence of T. is followed by increase in need of a myocardium for oxygen. Has vasodilating effect, a cut it is shown preferential concerning vessels of heart and kidneys. Caused by T. increase in a coronary blood-groove, perhaps, is caused not only by vasodilatation of heart, but also strengthening of its work. Besides, T. relaxes smooth muscles of bronchial tubes and has moderately expressed diuretic effect, a cut it is caused by decrease in a reabsorption of ions of sodium and chlorine in renal tubules, and also strengthening of a renal blood-groove. Unlike caffeine rather poorly stimulates c. N of page.
In mechanism of action T. and other alkaloids of a purine row an important role is played by their ability to inhibit phosphodiesterase, edges is the enzyme catalyzing transformation of cyclic AMF (tsAMF) into AMF. The inhibition of phosphodiesterase leads to increase in intracellular maintenance of tsAMF that is considered as one of the reasons of development of the main effects of purine alkaloids (relaxation of smooth muscles, strengthening of contractility of a myocardium, etc.).
T. it is well soaked up from went. - kish. path. The hl is metabolized. obr. in a liver. End products of metabolism of T. methyl derivatives are uric to-tyu to-rye are brought out of an organism through kidneys. Period of semi-life of T. at adults makes 3 — 5 hours. At cirrhosis it is extended several times.
Apply T. generally at vasospasms of a brain and at hron. koreynarny insufficiency it is frequent in a combination with others vasodilators (see). By efficiency at hron. coronary insufficiency of T. concedes to such anti-anginal means as beta adrenoblockers, etc.
Appoint inside the adult on 0,25 — 0,5 g on reception of 1 — 2 time a day. The highest doses for adults inside: one-time 1 g, daily 3 g.
Side effect T. it can be shown by dispeptic frustration. It must be kept in mind that at acute coronary insufficiency of T. can strengthen ischemia of a myocardium owing to increase in need of heart for oxygen.
Forms of release: powder and tablets on 0,25 g. T. is also a part of the combined tablets containing: a) theobromine of 0,25 g and Dibazolum of 0,02 g; b) theobromine of 0,25 g and papaverine of a hydrochloride of 0,02 g; c) theobromine of 0,25 g, Dibazolum and a papaverine of a hydrochloride on 0,02 or on 0,03 g; d) theobromine of 0,25 g, phenobarbital of 0,02 g; e) theobromine of 0,25 g, a papaverine of a hydrochloride and phenobarbital on 0,02 g Besides, the following combined tablets are issued, the T is a part to-rykh.: the tablets «Theminal» (Tabu-lettae «Theminalum») containing theobromine and pyramidon 0,25 g, phenobarbital of 0,02 g; the tablets «Theoverinum» (Tabulettae «Theoveri-num») containing theobromine of 0,25 g, a papaverine of a hydrochloride of 0,03 g and barbamyl of 0,075 g; the tablets «Teodinal» (Tabulettae «Theodina-lum») containing theobromine of 0,25 g, Dibazolum and phenobarbital 0,02 g; the tablets «Theodibaverinum» (Tabulettae «Theodibaverinum») containing theobromine of 0,15 g, a papaverine of a hydrochloride and Dibazolum 0,02 g.
T. and the tablets supporting him keep in well corked container.
Bibliography: Mashkovsky M. D. Pharmaceuticals, t. 1, page 454, M., 1984; The pharmacological basis of therapeutics, ed. by A. G. Gilman a. o., N. Y., 1980.
V. K. Muratov.