ACENOCOUMAROL ( NICOUMALONE )
BRAND NAME:- ACITROM,1,2,3 mg tabs.
Acenocoumarol is 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. Generic Name Acenocoumarol DrugBank Accession Number DB01418 Background.
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 between these clotting factors and calcium. Without this interaction, clotting cannot occur. Both the extrinsic (via factors VII, X and II) and intrinsic (via factors IX, X and II) are affected by acenocoumarol.
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 subsequent activation of the vitamin K-dependent coagulant proteins. The synthesis of vitamin K-dependent coagulation factors II, VII, IX, and X and anticoagulant proteins C and S is inhibited resulting in decreased prothrombin levels and a decrease in the amount of thrombin generated and bound to fibrin. This reduces the thrombogenicity of clots.
DOSE:-
The t½ of ACENOCOUMAROL as such in 8 hours, but an active metabolite is produced so that overall t½ is about 24 hours.
Acts more rapidly . As directed by your doctor.
ADVERSE EFFECTS:-
Bleeding as a result of extension of the desired pharmacological action is the most important problem causing ecchymosis , epistaxis , hematuria, bleeding in the g.i.t. intracranial or other internal haemorrhage may even be fatal. Bleeding is more likely if therapy is not properly monitored,or when INR exceeds 4,or interaction drugs/contraindications are present.
USED:-
In deep vein thrombosis, pulmonary Embolism,prevention of Blood clots.
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