Premium
Acebutolol disposition after intravenous administration
Author(s) -
Meffin Peter J.,
Winkle Roger A.,
Peters Flora A.,
Harrison Donald C.
Publication year - 1977
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1002/cpt1977225part1557
Subject(s) - acebutolol , disposition , medicine , administration (probate law) , pharmacology , anesthesia , psychology , law , social psychology , political science , propranolol
The disposition of acebutolol has been studied following intravenous doses of 0.25 to 1.0 mg/kg in 9 healthy subjects using a specific chromatographic assay to determine concentrations of drug in blood. The mean blood clearance was 6.55 mllmin/kg and the mean renal clearance, 2.68 mllmin/kg. Blood clearance was found to have a coefficient of variation of 14% for the group, to be independent of dose, and to remain essentially constant over approximately 3 wk. The fraction of the dose excreted in the urine unchanged was 0.405. Data were fitted to an equation for a two‐compartment model. The mean fast and slow half‐lives were 6.08 and 156.8 min, respectively. The volume of the central compartment was 0.223 L/kg, and the volume of distribution at steady‐state was 1.165 L/kg. The fraction of acebutolol unbound to plasma proteins was 0.743 and was independent of drug concentration in the range examined. Data obtained from 15‐min infusions were used to predict plateau blood concentrations with good accuracy during an 8‐hr dosage regimen.