Betaxolol: A New Long‐Acting Beta₁‐Selective Adrenergic Blocker

Abstract

Betaxolol (Searle, Skokie, Illinois) is a new beta 1-selective adrenergic blocker with no partial agonist action and minimal membrane stabilizing activity. Its pharmacokinetic profile is characterized by a long serum half-life and excellent oral bioavailability, with little first-pass metabolism. The mean 16-hour half-life of betaxolol has been shown to provide full 24-hour control of blood pressure and heart rate. Betaxolol has been proven to be a safe and effective antihypertensive agent, and was recently approved for clinical use in the United States for this indication.

Evaluation of human intestinal absorption data and subsequent derivation of a quantitative structure–activity relationship (QSAR) with the Abraham descriptors

“…The names of drug and drug‐like compounds and related data are listed in Table 1 and 2. The absorption data was collected and evaluated from 244 papers 1–5, 8–12, 18–251. The following information concerning human drug absorption was recorded from the literature: absorption data given from the literature;oral bioavailability or absolute bioavailability;percentage of cumulative urinary excretion of unchanged drug and its metabolites following oral and intravenous administration;percentage of metabolites in urine or first‐pass effect following oral and intravenous administration;percentage of unchanged drug in urine following oral and intravenous administration;percentage of excretion of drug in bile following oral and intravenous administration;percentage of cumulative excretion of drug in feces following oral and intravenous administration;total recovery of drug in urine and feces following oral and intravenous administration;single dose level in mg or mg/kg and daily oral dose in mg. …”

Prediction of Human Intestinal Absorption of Drug Compounds from Molecular Structure

“…The set of 86 drug and drug-like compounds and their experimentally derived %HIA values used in this study were gathered from literature sources. These compounds are listed in Table with their experimental %HIA values and references. ,,,,− …”