Acenocoumarol

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[edit] BRAND NAMES

[edit] STRUCTURE

File:Acenocoumarol.jpg

[edit] MECHANISM OF ACTION

Acenocoumarol, is a coumarin derivative that acts as a vitamin K antagonist.

Vitamin K antagonists produce their anticoagulant effect by inhibition of the vitamin K-epoxide-reductase, leading to the depletion of the reduced form of vitamin K (vitamin KH2). As vitamin KH2 is a cofactor for the carboxylation of certain glutamic acid residues near the N-terminals of vitamin K-dependent coagulation factors (II, VII, IX, and X). this ultimately results in reduced cleavage of fibrinogen into fibrin and decreased coagulability of the blood.

Acenocoumarol is not useful to dissolve already formed blood clots

Depending on the size of the initial dosage, acenocoumarol causes prolongation of the PT/INR within approx. 36 - 72 hours. Following withdrawal of the medication the PT/INR usually reverts to normal after a few days.

[edit] INDICATIONS

Treatment and the prevention of thromboembolism diseases

[edit] DOSAGE

The dosing of Acenocoumarol must be individualized. The usual starting dose in a normal weight person is between 2 mg/day to 4 mg/day without administration of a loading dose, if the PT/INR value before the start of treatment is within the normal range.

Treatment may also be initiated with a loading dose regimen, usually 6 mg on the first day followed by 4 mg on the second day. If the initial PT/INR value is abnormal, treatment should be instituted with caution.

tablets should be taken once a day and always at the same time.

Sensitivity to anticoagulants varies from patient to patient and may also fluctuate in the course of treatment. Therefore it is essential to perform regular testing of prothrombine time (PT)/ International Normalized Ratio (INR) and to adjust the patient's dosage accordingly. INR value should be between 2 and 3

[edit] CONTRAINDICATIONS

  • Known hypersensitivity to acenocoumarol and related coumarin derivatives
  • Pregnancy
  • In patients unable to cooperate and who are unsupervised (e.g. unsupervised senile patients, alcoholics and patients with psychiatric disorders)
  • Conditions where the risk of haemorrhage is greater than the possible clinical benefit

[edit] PRECAUTIONS

[edit] INTERACTIONS

Acenocoumarol is mainly metabolized by CYP2C9, therefore inhibitors of CYP2C9 may potentiate its anticoagulant effect.

[edit] PREGNANCY AND LACTATION

Acenocoumarol like other coumarin derivatives, may be associated with congenital malformation of the embryo. therefore it is contraindicated during pregnancy

[edit] SIDE EFFECTS

A common side effect is Haemorrhage in various organs

Other rare and very rare side effects include: Allergic reactions (e.g. urticaria, rash), Vasculitis, Loss of appetite, nausea, vomiting, Liver damage, Alopecia and Skin necrosis haemorrhagic.

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[edit] BIBLIOGRAPHY

[edit] REFERENCES