Absorption Metabolism and Excretion

Warfarin is rapidly and almost completely absorbed after oral administration and is bound extensively (>95%) to plasma proteins. Since it is the unbound drug that produces the anticoagulant effect, displacement of albumin-bound warfarin by other agents may result in bleeding. Although these drugs do not cross the blood-brain barrier, they can cross the placenta and may cause teratogenicity and hemorrhage in the fetus.

Warfarin is inactivated by hepatic P450 isozymes; hydroxylated metabolites are excreted into the bile and then into the intestine. Hepatic disease may potentiate the anticoagulant response.

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