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Dicumarol
- indication:For decreasing blood clotting. Often used along with heparin for treatment of deep vein thrombosis.
- pharmacologypharmacology:
- mechanism: Dicumarol 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 proteins, 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. Depression of three of the four vitamin K-dependent coagulation factors (factors II, VII, and X) results in decresed prothrombin levels and a decrease in the amount of thrombin generated and bound to fibrin. This reduces the thrombogenicity of clots.
- toxicity: LD<sub>50</sub>=233 mg/kg (orally in mice); LD<sub>50</sub>=250 mg/kg (orally in rats)
- absorprion:
- halflife:
- roouteelimination:
- volumedistribution:
- clearance: