Clinical pharmacology of acebutolol

Abstract

The clinical pharmacology and pharmacokinetics of acebutolol are summarized. Acebutolol and its longer-acting metabolite, diacetolol, are rapidly absorbed into the circulation from the gastrointestinal tract, and their bioavailability, unlike that of propranolol and metoprolol, is not significantly altered by whether the patient has recently eaten. Acebutolol is extensively metabolized by the liver, and elimination pathways involve approximately 30% to 40% through renal excretion and 50% to 60% by nonrenal mechanisms, including the bile and direct passage through the intestinal wall. The decreased hepatic metabolism and renal clearance rates seen in elderly patients may lead to the accumulation of both acebutolol and its metabolite, as has been reported with propranolol. In studies conducted to ascertain acebutolol's possible effect on common concurrently administered medications, the drug did not significantly alter either serum digoxin levels or serum insulin levels in diabetic patients treated with tolbutamide, nor did it change prothrombin time in patients treated with sodium warfarin.