NEODIKUMARIN (Neodicumarinum).

     Ethyl ether di - (4-oksikumarinil-3), acetic acid, or 3, 3 'karboetoksimetilen- - bis - (4-oksikumarin).

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

     White or white to slightly yellowish sheen melkokristallichesky odourless powder. Very malorastvorim in water and alcohol.

     Neodikumarin similar in structure and mechanism of action dikumarinom, which was first and foremost an anti-representative group of 4-oksikumarina. However, due to the high toxicity dikumarin in recent years has been withdrawn from use.

     Neodikumarin and other derivative 4-oksikumarina consider I have anti indirect actions, which are only effective when introduced into the body and do not affect the coagulation of blood mixing with the outside body. In modern, they are vitamin K antagonists to education protrombina liver.

     Effects of anti proximity to a failure biosynthesis protrombina, prokonvertina (factor VII), and other factors such as blood clotting (IX; X).

     Unlike anti direct action has no effect immediately, but slowly and continuously, have a cumulative properties. Other drugs in this group have with varying speed and force action, as well as varying degrees of cumulation. Compared with dikumarinom neodikumarin cumulative effect has less and less toxic.

     Neodikumarin relatively rapidly absorbed by ingestion. Therapeutic effects become apparent after 2 to 3 hours, reaching a peak after 12-30 h. In plasma neodikumarin associated with protein (mainly NPZ). Provided mainly with urine.

     Influenced neodikumarina the waning protrombina occur decrease prokonvertina, some slowdown rekaltsifikatsii plasma and lower tolerance to incidents.

     Neodikumarin is also lowering lipid in the blood, increases vascular permeability. There are indications that the pressures of neodikumarina and other derivative 4-oksikumarina prostatsiklinsinteziruyuschaya increased activity in the walls of blood vessels (see Prostaglandiny).

     Neodikumarin and other anticoagulants indirect actions to be applied with caution. In overdose and use long they could cause serious complications (bleeding), related not only to change blood coagulability, and increased capillary permeability. There may be micro-and makrogematuriya, bleeding from the mouth and lying, stomach and intestinal bleeding; Bleeding in the muscle, etc.

     Neodikumarin applied to reduce blood coagulability long in the prevention and treatment of thrombosis, tromboflebitov, thromboembolitic complications of heart attack, embolicheskih (but not haemorrhagic) stroke, embolicheskih defeat various organs. In surgical practice is also employed to prevent tromboobrazovaniya in aftercare period.

     Neodikumarin also apply in addition to the treatment of heparin.

     Is inside.

     Treatment must be carried out under the close supervision of a medical monitoring of blood protrombina and other factors such as blood clotting. Systematically also produce urine for the early detection of hematuria. Index protrombina kept at the level of 50-40%.

     In 1-day treatment is usually 0.3 to 2 g preparation times or three times the 0.2 grams (0.6 grams) per day; In Day 2 of 0.15 g three times, then 0, 2-0.1 g / day depending on the content in the blood protrombina.

     Higher doses for adults inside : single 0.3 g daily 0.9 g.

     After declining protrombina to 50-40% continue to treat small doses, supporting the index to neodikumarinom long as there is a danger tromboobrazovaniya.

     Termination treatment neodikumarinom and similar drugs should be gradually decreasing and increasing the dose interval receptions (up to 1 times a day or every other day); The sudden cancellation of this and other anti can cause rapid compensatory increase in the risk of protrombina thrombosis.

     When treating neodikumarinom and other drugs in this group to closely monitor the state of the patient and the changes in blood coagulation system. At least 1 in every 2 - 3 days to determine the index protrombina and explore the urine (hematuria given potential, which is an early sign of overdose). Ignoring these rules could lead to heavy bleeding.

     It should be borne in mind that the index protrombina (for one-way Kwik) is not always enough to detect changes that have occurred in the blood coagulation system. Haemorrhage may arise in the normal figure protrombina, so to better control should produce and other studies. Recommended tolerance to investigate incidents, plasma fibrin, and the time rekaltsifikatsii protrombinovy index, or (if possible) protrombina content (by definition produce two).

     Neodikumarin contraindicated in protrombina original content below 70%, haemorrhagic diathesis and other diseases involving low blood coagulation, and increased vascular permeability, pregnancy violations as liver and kidney, malignant tumors, ulcer disease zheludochnokishechnogo tract, perikarditah.

     There should be appointed neodikumarin during menstruation (receiving drugs stop for 2 days before menstruation) and in the first days after birth. Prudence requires the appointment of the elderly. In some cases, there are headache, diarrhea, allergic skin reactions.

     In krovotecheniyah should repeal preparation immediate introduction of vitamin K (see Fitomenodion, Vikasol) to designate products group vitamin E, ascorbic acid, calcium chloride, transfusion gemostaticheskih doses (75, 150 ml) fresh odnogruppovoy blood.

     Be aware that the use of barbiturates in the "induction" liver enzymes (see Phenobarbital) neodikumarina relaxed. Patients who are receiving neodikumarin while receiving barbiturates, lifting latest in the continuing recruitment neodikumarina in doses that caused prior to lowering the index protrombina could lead to dangerous bleeding.

     While neodikumarinom (as with other anti) should not appoint musk, as they lead to the dissociation of neodikumarina with plasma proteins and the increasing concentration of free anticoagulant in the blood. 4-Oksikumariny may exacerbate the effects butamida (hypoglycemia), difenina (toxic hazards), glucocorticoids (ultserogenny effects and the possibility of bleeding gastric ulcer).

     Product : tablets for 0.05 and 0.1 g.

     Storage : A. In a list ukuporennoy packaging keeps out of light and moisture. Pill-in the dark spot.

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