Journal ArticleDOI
Displacement of warfarin from human albumin by diazoxide and ethacrynic, mefenamic, and nalidixic acids
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TLDR
Clinical use of mefenamic acid, ethacrynic acid, nalidixoic acid, and diazoxide would cause an increase of 66 to 400 per cent in free active warfarin and make it necessary to reduce anticoagulant dosage in order to prevent excessive hypoprothrombinemia and hemorrhage.Abstract:
Large doses of drugs that are highly bound to proteins can displace coumarin anticoagulants from plasma proteins and thereby potentiate anticoagulation. Mefenamic acid, ethacrynic acid, nalidixoic acid, and diazoxide displace significant amounts of warfarin from human albumin in vitro by a noncompetitive mechanism. The relative potency of these displacing agents is: mefenamic acid > ethacrynic acid > diazoxide > nalidixic acid. If this effect occw's in vivo, clinical use of these drugs would cause an increase of 66 to 400 per cent in free active warfarin and make it necessary to reduce anticoagulant dosage in order to prevent excessive hypoprothrombinemia and hemorrhage.read more
Citations
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Journal ArticleDOI
Plasma and Tissue Protein Binding of Drugs in Pharmacokinetics
William J. Jusko,Mark Gretch +1 more
Journal ArticleDOI
Drug Interactions with Coumarin Anticoagulants
Jan Koch-Weser,Edward M. Sellers +1 more
TL;DR: Interactions of Individual Drugs with Coumarins A very large number of drugs have been suspected of interacting with coumarin anticoagulants, and some such anecdotal reports, even when invalidated by subsequent careful studies, have gradually developed into "facts" and are endlessly repeated in the literature.
Journal ArticleDOI
Vasodilator drugs in the treatment of hypertension.
TL;DR: Treatment with vasodilating drugs specifically reverses the major hemodynamic abnormality of primary hypertension and well-tolerated doses of hydralazine (200 mg/day) can normalize the hemodynamics of most hypertensives.
Journal ArticleDOI
Clinically important drug interactions with anticoagulants. An update
TL;DR: The complex response of coumarins to concomitant drug therapy makes it difficult to predict the occurrence and degree of a deterioration of anticoagulant control in individual patients and it seems advisable that one should monitor for changes in prothrombin time when adding or deleting any newly approved drug or any drug suspected to cause an interaction.
Journal ArticleDOI
The effect of albumin conformation on the binding of warfarin to human serum albumin. The dependence of the binding of warfarin to human serum albumin on the hydrogen, calcium, and chloride ion concentrations as studied by circular dichroism, fluorescence, and equilibrium dialysis.
TL;DR: In this paper, the pH dependence of warfarin binding to human serum albumin has been studied by circular dichroism, fluorescence, and equilibrium dialysis, showing that albumin complexes at low drug to protein ratios parallel the neutral to base transition, occurring in the protein over the pH range 6 to 9.
References
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Journal Article
Pharmacological implications of microsomal enzyme induction
TL;DR: It is of considerable interest that certain inducers of liver microsomal enzymes have recently been used therapeutically for the treatment of hyperbilirubinemia in jaundiced children and for thetreatment of Cushing's syndrome.
Journal ArticleDOI
Potentiation of Anticoagulant Effect of Warfarin by Phenylbutazone
TL;DR: The administration of the pyrazolone derivatives, phenylbutazone and oxyphen butazone, to a patient already being treated with coumarin anticoagulant drugs can lead to serious hemorrhagic complications.