Protein Binding and Vascular Activity of Diazoxide

Abstract

Diazoxide is a potent arteriolar dilator effective in severe hypertension. Its pharmacokinetics show three unusual features. To achieve maximal hypotensive action the drug must be injected rapidly intravenously. The plasma half-life (26 hours) greatly exceeds the duration of its vascular activity (four to eight hours). Plasma levels of diazoxide do not correlate with the intensity of its hypotensive action.