[Pharmacology of oral anticoagulants]

The present view on the mechanism of vitamin K-dependent synthesis of the clotting factors II, VII, IX and X in the liver and its inhibition by 4-hydroxycoumarine and 1,3-indandione-type anticoagulants is given. The discovery of gamma-carboxyglutamyl residues in intact clotting factors and the role of this amino acid as the calcium-binding principle is pointed out. After general considerations on the pharmacokinetics of coumarine-type anticoagulants detailed information on the pharmacokinetics of phenprocoumon, almost exclusively used in the GDR, is presented. The importance of pharmacokinetic aspects for control of oral anticoagulation is emphasized. As a possible tool for evaluation of individual pharmacokinetic parameters during already ongoing medication the additional administration of a single dose of radioactively labelled anticoagulant is proposed. Toxic effects in case of overdosage, untoward reactions and interference with oral anticoagulants by comedication are described.