Pharmacokinetics of Histamine (H₂)-Receptor Antagonists, including Roxatidine, in Chronic Renal Failure

Abstract

In this paper the effects of chronic renal failure on the pharmacokinetics of H₂-antagonists are reviewed and the results obtained with roxatidine presented. In normal renal function renal clearance is around 60–80% of total plasma clearance of all H₂-antagonists. Consequently, prolongation of serum half-life, mainly due to a decrease in urinary excretion, is noted in patients with decreasing glomerular filtration rate. In chronic renal failure, a dose reduction is therefore necessary with all H₂-antagonists, including roxatidine. It appears that neither haemodialysis nor peritoneal dialysis substantially influences the pharmacokinetics of these drugs. Therefore, the same dosage schedule as in uraemia may be applied in patients with dialysis. Finally, in the elderly the dosage of all H₂-antagonists should be adapted to the expected decrease in renal function.

Key Words:

• H₂-antagonists
• pharmacokinetics
• renal failure
• roxatidine