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Description of the medicine: Neodicumarinum (Neodicumarinum)

NEODICUMARIN (Neodicumarinum).

Ethyl ester of di- (4-oxycoumarinyl-3) -acetic acid, or 3,3'-carboethoxymethylene-bis (4-oxicoumarin).

Synonyms: Pelentan, Aethylis biscoumacetas, Dicumacyl, Dicumaryl, Ethyl biscumacetate, Pelentan, Trombarin, Trombex, Trombolysan, Tromexan, and others.

White or white with a slightly yellowish tint fine crystalline powder odorless. Very slightly soluble in water and alcohol.

Neodicumarin is similar in structure and mechanism of action with dicumarin, which was the first and main representative of anticoagulants of the 4-oxycoumarin group. However, due to the high toxicity, dicumarin has been taken out of use in recent years.

Neodikumarin and other derivatives of 4-oxycoumarin are classified as anticoagulants of indirect effect, which are effective only when introduced into the body and do not affect coagulation when mixed with blood outside the body. According to modern ideas, they are antagonists of vitamin K, necessary for the formation of prothrombin in the liver.

The effect of indirect anticoagulants is associated with a violation of the biosynthesis of prothrombin, proconvertin (factor VII) and other coagulation factors (IX, X).

Unlike anticoagulants, direct action has an effect not immediately, but slowly and continuously, have cumulative properties. Different drugs of this group have different speed and strength of action, as well as different degrees of cumulation. In comparison with dicoumarin, neodiquumarin has a smaller cumulative effect and is less toxic.

Neodicumarin is relatively quickly absorbed when taken orally. The therapeutic effect begins to appear after 2 to 3 hours, reaches a maximum after 12 to 30 hours. In the blood plasma, neodicumarin binds to proteins (mainly with albumins). Excreted mainly with urine.

Under the influence of neodicumarin, along with a decrease in prothrombin, there is a decrease in the content of proconvertin, a certain slowing of plasma recalcification and a decrease in tolerance to heparin.

Neodicumarin also causes a decrease in lipid levels in the blood, increases vascular permeability. There are indications that under the influence of neodicumarin and other derivatives of 4-oxycoumarin, prostacyclin-synthesizing activity in the walls of blood vessels increases (see Prostaglandins).

Neodicumarin and other anticoagulants of indirect action should be used with caution. In overdose and prolonged use, they can cause serious complications (bleeding), associated not only with changes in blood coagulability, but also with an increase in the permeability of capillaries. There may be micro- and macrohematuria, bleeding from the oral cavity and nasopharynx, gastric and intestinal bleeding; Hemorrhage in the muscles, etc.