Warfarin

Варфарин Drug photo

The description is actual on 03.06.2016

  • Latin name: Warfarin
  • ATH code: B01AA03
  • Active ingredient: Warfarin (Warfarin)
  • Producer: Kanonfarm production closed joint stock company, Ozone of Ltd company, Obolensky — the pharmaceutical enterprise (Russia)

Structure

As a part of the tablets Warfarin Nikomed is active agent sodium warfarin, and also additional ingredients: corn starch, lactose, indigo carmine dihydrate of calcium of hydrophosphate, magnesium stearate, povidone 30.

Release form

It is made in the form of tablets. Warfarin is tablets of a round form, light blue color, with crosswise risky. Tablets are packed into bottles from plastic on 50 or 100 pieces. Bottles are closed by covers which screw on.

Pharmacological action

Warfarin in a human body blocks in a liver synthesis process vitamin of K-dependent blood-coagulation factors (II, VII, IX, X), it reduces their concentration in plasma owing to what there is a blood coagulation process delay.

Pharmacokinetics and pharmacodynamics

After the first reception anticoagulative action is observed 36–72 hours later. The maximum action is noted in 5–7 days after the beginning of a course of reception. After drug intake was complete, activity vitamin of K-dependent blood-coagulation factors is recovered for 4-5 days.

From the alimentary system it is soaked up quickly and almost completely. Communication with proteins of plasma – for 97–99%. The metabolism occurs in a liver.

Warfarin — racemic mix, R-and S-isomers are metabolized in a liver in the different ways. Each isomer will be transformed to the main two metabolites.

Out of an organism in the form of inactive metabolites it is brought with bile, metabolites reabsorbirutsya in a digestive tract, are allocated with urine.

Time of semi-removal is equal from 20 to 60 hours. Semi-removal of R-enantiomera – from 37 to 89 hours, semi-removal of S-enantiomera — from 21 to 43 hours.

Indications to Warfarin use

Means is applied for the purpose of treatment and prevention of an embolism and thromboses of blood vessels. Such indications to Warfarin use are defined:

  • venous thrombosis in an acute form, and also recurrent;
  • embolism of a pulmonary artery;
  • strokes, passing ischemic attacks;
  • prevention of tromboembolic episodes at the people who had a myocardial infarction;
  • secondary prevention of a myocardial infarction;
  • prevention of tromboembolic episodes at people with defeats of valves of heart, fibrillation of auricles, and also at those who transferred prosthetics of valves of heart;
  • prevention of display of postoperative thromboses.

Contraindications

Before taking medicine, it is necessary to consider those contraindications which are specified in the instruction to drug:

  • manifestation of high sensitivity to components of means or suspicion on hypersensitivity;
  • acute bleeding;
  • serious illnesses of a liver and kidneys;
  • first trimester of pregnancy and last 4 weeks of incubation of a fruit;
  • acute IDCS;
  • thrombocytopenia;
  • lack of proteins C and S;
  • varicosity of a digestive tract;
  • aneurism of arteries;
  • the increased risk of display of bleedings, including hemorrhagic frustration;
  • stomach ulcer and duodenum;
  • heavy wounds, including postoperative;
  • lumbar puncture;
  • bacterial endocarditis;
  • hypertensia is malignant;
  • intracraneal hemorrhage;
  • hemorrhagic stroke.

Side effects of Warfarin

In the course of treatment such side effects of Warfarin can be shown:

  • bleeding — it is frequent;
  • increase in sensitivity to Warfarin after long treatment;
  • abdominal pains, vomiting, diarrhea, anemia — infrequently;
  • increase in activity of enzymes of a liver, eosinophilia, urticaria, jaundice, eczema,  skin necrosis, itch, rash, nephrite, urolithiasis, vasculitis, tubular necrosis — is rare.

Manifestations of bleeding are noted approximately at 8% of patients who receive Warfarin. From these cases of 1% are heavy, demanding hospitalization, another 0,25% are defined as fatal. A major factor of risk for development of intracraneal hemorrhage is uncontrollable or not treated hypertensia. Also the probability at treatment by Warfarin increases at people of advanced age, in the presence in the anamnesis of bleedings from a gastrointestinal tract and strokes, at the high intensity accompanying anticoagulating and antiagregantny treatment and also people with polymorphism of a gene have CYP2C9.

In rare instances at therapy by Warfarin as a side effect the coumarinic necrosis can be shown. As a rule, this phenomenon begins with emergence of a swelling and darkening of integuments of buttocks or legs, less often such signs appear in other places. Later such defeats become necrotic. Approximately this by-effect develops in 90% of cases at women. It is noted from the third to the tenth day of drug intake. Its origin is connected with insufficiency of an antitrombichesky protein of C or S. At inborn insufficiency of these proteins it is necessary to begin reception of Warfarin with small doses and at the same time to enter heparin. At development of such complication it is necessary to stop treatment and to enter heparin until defeats do not begin to live.

Seldom or never the palmar and bottom syndrome can develop. This complication develops at men who have atherosclerosis. Development of purple symmetric damages of skin on soles of feet and on fingers at which thermalgias are noted is characteristic of this complication. Symptoms disappear when drug intake stops.

Application instruction of Warfarin (Way and dosage)

Medicine should be taken inside, once a day. It is recommended to drink tablets every day at the same time. To define, how much time you need to accept drug, the doctor individually has to.

Before beginning treatment, it is necessary to define MHO then laboratory researches are conducted in 4-8 weeks regularly.

The application instruction of Warfarin Nikomed provides that to people who did not take this medicine earlier appoint 5 mg in knocks (2 tab.) for 4 days. For the 5th day it is necessary to define MNO then, according to the received results of research, appoint a maintenance dose. As a rule, it makes 2,5–7,5 mg of medicine a day.

To those patients who already accepted Warfarin for two days appoint a double dose of the known maintenance dose of drug, further appoint one maintenance dose of medicine a day. For the fifth day carry surely out control of MHO then the dose is adjusted according to the received results of researches.

It is recommended to support an indicator of MNO at the level from 2 to 3 if treatment or prevention of an embolism of a pulmonary artery, venous thrombosis, the complicated diseases of valves of heart, fibrillation of auricles is carried out.

The norm has to be supported by MNO at reception of Warfarin at the level from 2,5 to 3,5 if treatment of patients who transferred prosthetics of valves of heart, and also at the acute complicated myocardial infarction is carried out.

Control of MNO at reception of Warfarin is obligatory. The dosage and the detailed scheme of reception is defined by the attending physician.

There are no sufficient data about Warfarin reception by children. As a rule, the initial dose of medicine makes 0,2 mg / on 1 kg of weight of the child a day if the liver functions normally, and 0,1 mg / on 1 kg of weight of the child a day if functions of a liver are broken. At selection of a maintenance dose MHO indicators are surely considered. It is recommended to support the same levels, as at adult patients. Only the specialist can make the decision on purpose of Warfarin to children.

It is important to conduct careful supervision over elderly people who accept Warfarin. Careful control of indicators of MNO at people with a liver failure is necessary. The people having a renal failure do not need to adjust doses.

Overdose

In the course of reception of those doses which are appointed for treatment insignificant bleedings can develop. At small bleedings it is necessary to lower a dose of medicine or for a certain term to stop therapy (until until MNO reaches necessary level).

At development of heavy bleeding treatment of overdose needs to be begun with administration intravenously of vitamin K. Also to the patient appoint Absorbent carbon, freshly frozen plasma or a concentrate of factors of coagulation.

Depending on the MNO level it is necessary to work as follows:

At insignificant bleeding:

  • MNO less than 5: the following dose of drug needs to be passed then to accept smaller doses of Warfarin.
  • MHO 5-9: to pass the following 1-2 doses then to accept lower doses. Or to pass 1 dose and to accept in 1–2,5 mg of vitamin K.
  • MNO more than 9: to suspend use of medicine, to practice oral administration of 3-5 mg of vitamin K.

It is necessary to cancel drug:

  • MNO more than 9 (if an operative measure is planned): use of medicine is stopped, practice reception of 2-4 mg of Warfarin orally (one day before the planned operation).
  • MNO more than 20 (if severe bleeding is noted): slow administration intravenously of vitamin K in a dose of 10 mg is appointed, transfusion of freshly frozen plasma or concentrates of factors of a prothrombin complex also practices. If there is a need, vitamin K is entered by each 12 hours.

After treatment was carried out, it is necessary to watch the patient as time of semi-removal of Warfarin is equal to 20-60 hours.

Interaction

It is not necessary to begin therapy or to stop it without preliminary consultation with the doctor. Also it is impossible to change a dosage independently.

At appointment along with other drugs it is important to consider impact of the termination of induction or inhibition of influence of Warfarin other drugs.

The risk of display of heavy bleedings increases if to accept Warfarin along with drugs which influence primary hemostasis and level of thrombocytes. This is Klopidogrel, acetylsalicylic acid, tiklopidin, Dipiridamolum, high doses of penicillin, and also the majority of NPVS (an exception TsOG-2 inhibitors are),

Danger of development of bleeding increases if to accept Warfarin along with drugs which possess the expressed inhibiting effect on system of P450 cytochrome (chloramphenicol, Cimetidinum).

A number of medicines strengthen effect of Warfarin on an organism. These are the drugs Amiodaronum, Allopyrinolum, azithromycin, alpha and beta interferon, acetylsalicylic acid, Amitriptyline, azapropazon, a vaccine antiinfluenzal, vitamins A, E, bezafibrat, the glucagon, heparin, grepafloksatsin, gemfibrozit, Glibenclamidum, dextropropoxyphene, danazol, Digoxin, diazoxide, Disulfiramum, Disopyramidum, zafirlukast, itrakonazol, ifosfamid, Indometacin, codeine, Klaritromitsin, Clofibratum, ketokonazol, lovastatin, Levamisole, metolazon, Miconazolum, metronidazole, a methotrexate, Norfloxacin, Acidum nalidixicum, Omeprazol, oksifenbutazon, ofloxacin, propranolol, paroksetin, propafenon, paracetamol, proguanil, piroxicam, roksitromitsin, Simvastatin, sertraline, sulfametizol, sulfafurazol, sulfamethoxazole Trimethoprimum, sulfafenazol, sulindak, Sulfinpyrazonum, androgenic and anabolic steroid hormones, Tegafurum, Tamoxifenum, tetracyclines, testosterone, tolmetin, thiensilt acid, troglitazon, trastuzumab, feprazon, Flukonazol, Phenytoinum, fenofibrat, phenylbutazone, Ftoruratsil, fluoxetine, fluvoksamin, Flutamid, fluvastatin, Chlorali hydras, Quinine, chloramphenicol, quinidine, Cefalexin, tsefamandol, tselekoksib, Tsefuroksy, tsefmenoksy, tsefoperazon, tsefmetazol, Cyclophosphamide, ciprofloxacin, Cimetidinum, Etopozid, erythromycin, ethanol.

Also drugs of a number of medicinal plants can strengthen effect of Warfarin: ginkgo, garlic, papaya, medicinal angelica, sage.

The effect of Warfarin is reduced by a St. John's Wort, a ginseng. It is not necessary to accept any drugs of a St. John's Wort at the same time. At reception of such drugs it is necessary to check MHO and to suspend reception.

Influence of Warfarin can strengthen quinine which contains in tonics.

Warfarin strengthens effect of peroral hypoglycemic drugs of derivatives of a sulfonilmochevina.

Effect of Warfarin can decrease if the patient at the same time takes the following medicine: aminoglutetimid, Azathioprinum, barbiturates, vitamins C, To, valproic acid, griseofulvin, glutetimid, Disopyramidum, dikloksatsillin, Colestyraminum, carbamazepine, coenzyme Q10, mesalazin, mianserin, Mercaptopurinum, Mitotanum, naftsillin, Primidonum, ritonavir, retinoids, rofekoksib, rifampicin, sukralfat, Spironolactonum, Trazodonum, phenazone, Chlortalidonum, chlordiazepoxide, cyclosporine. At reception of diuretics on condition of the expressed hypovolemic influence increase in concentration of factors of coagulability can be noted that leads to decrease in effect of anticoagulants. At the combination of reception of Warfarin and drugs which are listed above it is important to control MHO before therapy, after its termination and several weeks later.

A certain diet  at Warfarin reception has to be kept. It is necessary to consider that the use of products with the high content of vitamin K reduces effect of medicine. Therefore food at reception of tablets should not include a large number of greens, avocado, cabbage, onions, a coriander, fruits of a kiwi, salad lettuce, olive oil, peas, soybeans, etc.

Terms of sale

It is possible to get according to the recipe, the attending physician writes out the recipe on Latin.

Storage conditions

Warfarin needs to be kept at a temperature up to 25 °C, to protect from access for children.

Period of validity

It is possible to store 5 years.

Special instructions

In the course of treatment the patient without fail needs to adhere to the appointed dosage.

It is necessary to consider that the patients having dementia or alcoholism can be incapable to observe a drug dosage.

Effect of the medicine can amplify at certain states: fever, dekompensirovanny heart failure, a hyperthyroidism, alcoholism with damage of a liver. At a nephrotic syndrome or a renal failure the effect can both go down, and to raise. At a liver failure action amplifies. At all specified states it is important to carry out control of MNO.

It is recommended to people who receive medical treatment for Warfarin to apply as anesthetics Tramadol, paracetamol or opiates.

At people with a mutation of a gene which codes CYP2C9 enzyme, more long elimination half-life is noted. Therefore such patients need to appoint lower doses of medicine.

To patients with deficit of enzyme of lactase, intolerance of a galactose, disturbance of absorption of glucose and a galactose Warfarin is not appointed. At need to gain fast antitrombotichesky effect it is recommended to begin therapy with administration of heparin, further for 5-7 days to carry out the combined treatment by heparin and Warfarin until the MHO level remain for two days.

To avoid manifestation of a coumarinic necrosis people at whom hereditary insufficiency of an antitrombichesky protein of C or S is noted need initially to enter heparin. It is necessary to enter it within 5-7 days. The initial dose of Warfarin should not be higher than 5 mg.

At individual resistance to Warfarin the patient needs to enter 5-20 shock doses of medicine.

Analogs of Warfarin

Coincidence on the ATH code of the 4th level:

Now the following analogs of Warfarin are made: Varfareks, Marevan, Pradaksa, Ksarelto. What it is possible to replace drug with, in each case only the attending physician has to define. Any substitute needs to be selected taking into account the diagnosis and symptoms.

Ksarelto or Warfarin — what is better?

Ksarelto's medicine provokes smaller quantity of by-effects, and at its reception it is not necessary to control MNO so carefully. However this medicine, unlike Warfarin, is not appointed at defeat of valves of heart of rheumatic character or in the presence of artificial valves.

Warfarin or Phenilinum?

Phenilinum belongs to group of indirect anticoagulants. Indications to use of medicine are similar to those which appear in the instruction to Warfarin. Means also provokes manifestation of a number of side effects. What of drugs to choose, the doctor individually defines.

Zdravzona

  • Warfarin 2,5mg No. 50 of a tabletkikanonfarm production closed joint stock company
  • Warfarin 2,5mg No. 100 of a tabletkikanonfarm production closed joint stock company
  • Warfarin nikomed 2,5mg No. 100 of a tabletkitaked of JV Farm. z lake of the lake.
  • Warfarin nikomed 2,5mg No. 50 of a tabletkitaked of JV Farm. z lake of the lake.

Drugstore of IFC

  • Warfarin tbl 2.5mg No. 50, Nycomed Danmark Aspdaniya
  • Warfarin tbl 2.5mg No. 100, Nycomed Danmark Aspdaniya
  • Warfarin tbl 2.5mg No. 50, Nycomed Pharma Sp. z.o.o.polsha
  • Warfarin tbl 2.5mg No. 100, Kanonfarm Production Zaorossiya
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Apteka24

  • No. 100farmastart tablet 2.5mg warfarin (Ukraine, Kiev)
  • Warfarin Nikomed of table 2.5 mg No. 100nikomed (Austria)
  • Warfarin of a tablet 3 of mg No. 100 Orion (Finland)
  • Warfarin of a tablet 3 of mg No. 100farmastart (Ukraine, Kiev)
  • Warfarin of a tablet 3 of mg No. 30 Orion (Finland)

BIOSPHERE

  • Warfarin of 2,5 mg No. 100 of table.
  • Warfarin of 2,5 mg No. 50 of table.
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Section: For blood
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Education: "Pharmacy" graduated from the Rovno state basic medical college majoring in. Graduated from the Vinnytsia state medical university of M. I. Pirogov and internship on its base.

Experience: From 2003 to 2013 – worked at positions of the pharmacist and manager of a pharmaceutical booth. It is awarded by diplomas and distinctions for long-term and honest work. Articles on medical subject were published in local editions (newspaper) and on various Internet portals.

PAY ATTENTION! Information on drugs on the website is help generalizing, collected from public sources and can form the basis for making decision on use of medicines it is not aware of treatment. Before medicine use Warfarin surely consult with the attending physician.