Comparative Review of the Pharmacokinetics of Vitamin D Analogues

This article reviews the pharmacokinetic characteristics of calcitriol, paricalcitol, and doxercalciferol, and provides an overview of the metabolism of vitamin D. Calcitriol and paricalcitol have similar pharmacokinetic profiles, with terminal half-lives ranging from 5 to 10 hours in healthy subjects to 15-30 hours in patients undergoing dialysis. Both are active on intravenous administration and little of the active agent remains in the circulation after 24 hours, although they are normally given every 48-72 hours. Doxercalciferol is a prohormone, requiring hepatic metabolism to the active metabolite 1alpha,25-(OH)2D2. The half-life of 1alpha,25-(OH)2D2 is about 34 hours in healthy subjects and about 45 hours in dialysis patients, resembling physiologic blood concentrations of endogenous vitamin D. More studies are warranted to determine the disposition of the vitamin D analogues, especially in selected populations such as pediatric and geriatric dialysis patients.