Description

Simple

An anticoagulant or "blood thinner" used to treat or prevent blood clots in various illnesses including heart attacks.

Clinical

An anticoagulant drug used in the prevention of thromboembolic diseases in infarction and transient ischemic attacks, as well as management of deep vein thrombosis and myocardial infarction.

Overview

Acenocoumarol is a coumarin derivative used as an anticoagulant. Coumarin derivatives inhibit the reduction of vitamin K by vitamin K reductase. This prevents carboxylation of vitamin K-dependent clotting factors, II, VII, IX and X, and interferes with coagulation.[6] Hematocrit, hemoglobin, international normalized ratio and liver panel should be monitored. Patients on acenocoumarol are prohibited from giving blood.

Pharmacology

Indication

For the treatment and prevention of thromboembolic diseases. More specifically, it is indicated for the prevention of cerebral embolism, deep vein thrombosis, pulmonary embolism, thromboembolism in infarction and transient ischemic attacks. It is used for the treatment of deep vein thrombosis and my... Read more

Pharmacodynamic

Acenocoumarol inhibits the reduction of vitamin K by vitamin K reductase. This prevents carboxylation of certain glutamic acid residues near the N-terminals of clotting factors II, VII, IX and X, the vitamin K-dependent clotting factors. Glutamic acid carboxylation is important for the interaction b... Read more

Mechanism of action

Acenocoumarol inhibits vitamin K reductase, resulting in depletion of the reduced form of vitamin K (vitamin KH2). As vitamin K is a cofactor for the carboxylation of glutamate residues on the N-terminal regions of vitamin K-dependent clotting factors, this limits the gamma-carboxylation and subsequ... Read more

Absorption

Rapidly absorbed orally with greater than 60% bioavailability. Peak plasma levels are attained 1 to 3 hours following oral administration.

Protein binding

98.7% protein bound, mainly to albumin

Volume of distribution

The volume of distribution at steady-state appeared to be significantly dose dependent: 78 ml/kg for doses < or = 20 microg/kg and 88 ml/kg for doses > 20 microg/kg respectively

Clearance

Information currently not available.

Half life

8 to 11 hours.

Route of elimination

Mostly via the kidney as metabolites

Toxicity

The onset and severity of the symptoms are dependent on the individual's sensitivity to oral anticoagulants, the severity of the overdosage, and the duration of treatment. Bleeding is the major sign of toxicity with oral anticoagulant drugs. The most frequent symptoms observed are: cutaneous bleedin... Read more

Adverse Effects

Effect Regions Age Groups Incidences Evidence Type

Contraindications

Information currently not available.

Food Interactions

Avoid herbs and supplements with anticoagulant/antiplatelet activity.

Ensure consistent Vitamin K intake. Changes in vitamin K intake may impact coagulation. Foods containing vitamin K include spinach, kale, and swiss chard.

Exercise caution with St. John's Wort.