Syncumarum

General characteristics. Structure:

Active ingredients 

Atsenokumarol of 2 mg

Inactive ingredients 

Lactose, starch, talc, gelatin, magnesium stearate.

Description.

White, inodorous, flat and round tablets with slanted edges. On one party a text of "SYNCU", on other party dividing risk. A break surface - white.

Pharmacological properties:

Atsenokumarol belongs to anticoagulants of indirect action to antagonists of vitamin K – dioxycoumarin derivatives. Atsenokumarol breaks synthesis of factors P (prothrombin), unitary enterprise, 1X and the X blood coagulations. The maximum effect is reached after 3-5 days of administration of drug as in plasma the synthesized earlier active factors of a prothrombin complex circulate. Lengthening of a prothrombin time in the first day of treatment is reached due to decrease of the activity of a factor unitary enterprise which elimination half-life makes 4-6 hours. Further there is a decrease of the activity of the factor 1X having an elimination half-life 20-24 hour, a factor of X, which elimination half-life 48-76 hours, and a prothrombin with an elimination half-life of 72-100 hours.

Pharmacokinetics. Atsenokumarol is well soaked up from a digestive tract. The maximum concentration in plasma is reached in 3 hours after administration of drug. 98% of the drug which came to an organism contact proteins of plasma. Elimination half-life

drug makes about 8-9 hours. Atsenokumarol is metabolized in a liver. About 60% of the drug which came to an organism are allocated with urine, mainly in the form of metabolites, the remained quantity is distinguished with a stake. Extent of lengthening of a prothrombin time or increase in a prothrombin ratio does not depend on concentration of an atsenokumarol in blood.

Indications to use:

Thrombosis, thrombophlebitis, tromboembolic episodes at a myocardial infarction, embolisms of various bodies (prevention and treatment). In surgical practice for the prevention of tromboembolic episodes in the postoperative period.

Route of administration and doses:

Drug is used inside. The dose of drug is established individually depending on blood coagulation indicators. In the first day the dose makes 6-8 mg a day, further 4 mg a day under control of a prothrombin time which has to be within 2,0-3,5 seconds. Reception frequency – once a day at the same time.

Features of use:

It is necessary to control prothrombin level in blood and a prothrombin ratio (the prothrombin time should not exceed 4), the general analysis of urine (existence of erythrocytes in urine). It is necessary to warn the patient about a possibility of emergence of bleeding and bleedings and need to coordinate reception of other drugs with the attending physician. At patients of advanced and senile age, especially with the expressed atherosclerosis, and patients with heart failure the thicket needs to carry out laboratory control of therapy and it is possible to reduce a drug dose. The patients applying аценокумарол should avoid purpose of intramuscular injections if it is impossible, then intramuscular injections to do in upper extremities where possible bleedings are quicker diagnosed, and it is easier to apply a compressing bandage. In 2-3 days prior to the planned operation or an odontectomy it is necessary to stop administration of drug, the prothrombin time has to become less than 1,5. In need of an urgent operative measure it is possible to enter intravenously 5-10 mg of vitamin K that usually provides achievement of a prothrombin time less than 1,5 within 24 hours.

During therapy atsenokumaroly it is necessary to watch the general condition of the patient and changes in coagulant system of blood carefully. At emergence against the background of therapy of bleeding or bleedings аценокумарол it is necessary to cancel.

The need for the atsenokumarol increases at a hypothyroidism, a lipidemia, the increased intake of vitamin K with food, a nephrotic syndrome, hypostases.

The need for the atsenokumarol decreases at starvation, a hypoalbuminemia owing to a disease of a liver and kidneys, diarrhea, a syndrome of the broken absorption, a hyperthyroidism, fever, a circulatory unefficiency with developments of stagnation.

In case of significant increase in a prothrombin time without hemorrhagic manifestations it is necessary to refrain from use of an atsenokumarol, to daily check a prothrombin time, purpose of vitamin K in tablets in a dose of 2,5 - 5 mg is possible.

Side effects:

Nausea, diarrhea, alopecia, headache, allergic reactions in the form of skin rash and a Quincke's edema, bleeding, hemorrhages on skin and mucous membranes (on extent of reduction of frequency of occurrence): hamaturia, odontorrhagias, petechias, posttraumatic hematoma, melena, metrorrhagias, hemarthrosis, hemorrhagic stroke. Very seldom the syndrome of purple feet and a necrosis of skin and hypodermic cellulose can develop. Probably cholesteric microblood clots are the reason of a syndrome of purple feet. This complication appears after several weeks of administration of drug and is shown by a bluish hyperpegmentation of feet and thumbs of feet, and also pain in thumbs of feet. The hyperpegmentation disappears when pressing and raising an extremity. The skin necrosis has in the beginning the form of an erythema or spotty and papular rash which develops on a breast, hips and buttocks, can be also on upper extremities, the person and generative organs. In case of the first symptoms of a necrosis of skin it is necessary to cancel immediately drug and to appoint vitamin K or heparin which can prevent development of a full necrosis.

Withdrawal – increase in risk of a thrombogenesis.

Interaction with other medicines:

Strengthening of action of an atsenokumarol is caused: Allopyrinolum, Amiodaronum, antibiotics (aminoglycosides, cephalosporins for parenteral administration, macroleads, intravenous penicillin in high doses, hinolona and ftorkhinolona, tetracyclines), азапропазон, quinidine sulfate, Chlorali hydras, Chlorpromazinum, Cimetidinum, dextrothyroxine, Disulfiramum, фенофибрат, phenylbutazone, a glucagon, an ibuprofen, indometacin, MAO inhibitors, Clofibratum, acetylsalicylic acid (aspirin), Acidum etacrynicum, mefenamovy acid, ловастин, metamizole sodium (analginum), metronidazole, Methyldopum, Miconazolum, Naproxenum, пентоксифиллин, пропафенон, salicylates, anabolic hormones, Sulfinpyrazonum, it is long the operating streptocides (Trimethoprimum, sulfamethoxazole), Tamoxifenum, means for an inhalation anesthesia.

Weakening of action of an atsenokumarol is caused: aminoglutethimide, peroral contraceptive means, barbiturates, chlordiazepoxide, Phenytoinum, griseofulvin, haloperidol, carbamazepine, колестипол, meprobamate, Mercaptopurinum, rifampicin, сукральфат, ascorbic acid (vitamin C), sodium Menadionum bisulphite (vitamin K), antihistamines.

Alcohol, diuretics (for example, furosemide) and ranitidine can both strengthen, and to weaken action of an atsenokumarol.

Atsenokumarol strengthens action of derivatives of sulphonylurea (Chlorproramidum. Tolbutamidum), anti-epileptic means (Phenytoinum, phenobarbital).

Action of an atsenokumarol is weakened after meal, rich with vitamin K (broccoli, a cauliflower, green peas, cabbage, salad, spinach, a liver, soy grain). The best anesthetic for the patients receiving аценокумарол is paracetamol as non-steroidal anti-inflammatory drugs strengthen antitrombotichesky action of an atsenokumarol.

If the patient accepts any means interacting with atsenokumaroly or other drugs with unknown influence on аценокумарол, it is necessary to control often a prothrombin time for the purpose of selection of an individual dose.

Contraindications:

The hemorrhagic diathesis and other diseases which are followed by the lowered coagulability of blood, a renal failure, the expressed abnormal liver functions, an arterial hypertension, malignant new growths, a diabetic retinopathy, physical exhaustion, a prothrombinopenia (less than 70%), a hypovitaminosis To and With, bleeding from open wounds, a peptic ulcer of a stomach and duodenum, ulcer colitis, a hemorrhagic stroke (the first 2 months), pregnancy, the lactation period, the menacing abortion, a puerperal eclampsia and a preeclampsia, a long endocarditis, a pericardis, the stratified aortic aneurysm, directly after surgical interventions in an oftalmogiya, neurology and stomatology after a lumbar puncture, a biopsy of bodies or a puncture of an aorta within 4 days.

Overdose:

In case of overdose of drug hemorrhagic diathesis in the form of formation of bruises, bleedings from a nose and gums, long bleeding from superficial wounds, a hamaturia and menorrhagias is most often observed.

In the presence of a hemorrhagic syndrome and sharp lengthening of a prothrombin time it is recommended to enter intravenously slowly 5 – 10 mg of vitamin K (phytomenadionum),

the effect will occur in 6 – 10 hours. At life-threatening bleeding it is necessary to pour in addition freshly frozen plasma of 10 – 15 ml on kg of body weight or a concentrate of the prothrombin complex containing a factor of VII.

Storage conditions:

List A. In the place, unavailable to children, at a temperature not above 30 °C. Period of validity of 5 years. After a period of validity not to apply.

Issue conditions:

According to the recipe

Packaging:

Tablets on 2 mg in blisters on 10 pieces, 5 blisters in a cardboard box together with the instruction on a medical use.