DICUMARINUM (Dicumarinum; synonym: Antithrombosin, Bishydroxycoumarin, Cumid, Dicoumarolum, Kumoran, Melitoxin, Symparin, Trombosan etc.; GF X, SP. A) — the anticoagulant which is characterized by indirect long action. Dee - (4-oxycoumarinyl-3) - methane, or 3,3 '-metilen-bis-(4 oxycoumarin):
White or slightly cream fine-crystalline powder, t ° pl 288 °; it is almost water-insoluble, alcohol, ether, we will dissolve in caustic alkalis.
Is an antimetabolite of phthiocol; the specific antagonist D. — K1 vitamin. Breaks biosynthesis of blood-coagulation factors — a prothrombin (a factor of II), proconvertin (a factor of VII), a kristmasfaktor (IX) and a styuart-prauer-factor (X); as a result coagulability of blood goes down (see. Coagulant system of blood ). D.'s action develops gradually, reaching a maximum in 48 — 72 hours after single introduction and 2 — 4 days last. Drug actively influences breath and power activity of cells, separates oxidizing phosphorylation, reduces the level of lipids in blood, increases permeability of vessels, relaxes smooth muscles of intestines, bronchial tubes, increases rate of volume flow of a coronary blood-groove, increases allocation from an organism of salts uric to - you.
At intake of D. rather quickly, though not completely, it is soaked up from went. - kish. path. Content in blood varies it at people even at reception of identical doses. In plasma D. contacts proteins, generally albumine (99% of substance are in not dialyzed form), it is partially deposited in erythrocytes, then comes to fabrics — hl. obr. in a liver, and also in kidneys, lungs and a spleen; its most low concentration is found in skeletal muscles and a brain. Coming to cells of fabrics, D. is distributed in kernels and mitochondrions. Gets through a placental barrier. Under the influence of enzymes of a liver of D. turns into the metabolites which are not connected with proteins. They are allocated with bile in intestines from where again are soaked up in blood and removed by kidneys.
Apply to prevention and treatment of thromboembolic diseases: thromboses, thrombophlebitis, embolisms, tromboembolic episodes at a myocardial infarction. Treatment is carried out in stationary conditions under careful observation of the doctor with obligatory systematic control of content in blood of a prothrombin and other indicators of a condition of coagulant system of blood. The dose is selected individually taking into account initial coagulability of blood and its changes in process of treatment. In the 1st day usually appoint 0,05 — 0,1 g two-three times a day, in the next days — on 0,15 — 0,2 g a day, gradually reducing a dose to supporting (0,05 — 0,1 g a day). Due to duration of stage of latency of action of D. in the 1st day of treatment it is combined with the heparin or other anticoagulants having direct effect. The highest dose for adults inside: one-time 0,1 g, daily 0,3 g
Due to cumulative action of D. at its use it is necessary to be careful. Drug can cause bleedings, connected not only with change of coagulability of blood, but also with increase in permeability of capillaries. In these cases it is cancelled and immediately enter 1 — 2 ml of 1% of solution of Vikasolum, drugs of K1 vitamin, vitamin P or Rutinum, ascorbic to - that, calcium chloride and do transfusion of fresh odnogruppny blood in a haemo static dose (75 — 150 ml).
Is contraindicated at the initial maintenance of a prothrombin less than 70%, the hemorrhagic diathesis and other diseases which are followed by the lowered coagulability of blood at a hyperpermeability of vessels, pregnancy, abnormal liver functions and kidneys, malignant new growths, a peptic ulcer of a stomach and a duodenum, perikardita. It is not necessary to appoint D. along with salicylates.
Forms of release: powder and tablets on 0,1 g. Keep powder in well corked container, tablets in the dry, protected from light place.
See also Anticoagulants .
Bibliography: Lakin K. M. Medicinal regulation of a blood coagulation, M., 1971; Malinovsky H. N and Kozlov V. A. Anticoagulating and thrombolytic therapy in surgery, M., 1976; P e r l and to E. Anticoagulants, the lane with it., L., 1965, bibliogr.
K. M. Lakin.