Cardiovascular (β‐Adrenergic Blocking Effects of Bornaprolol in Humans: Relation to Dose and Plasma Concentration

  title={Cardiovascular ($\beta$‐Adrenergic Blocking Effects of Bornaprolol in Humans: Relation to Dose and Plasma Concentration},
  author={Georges Cheymol and Patrice Jaillon and Bertrand Lecoq and V Lecoq and Andr{\'e} Cheymol and Michel Krumenacker},
  journal={Journal of Cardiovascular Pharmacology},
The cardiovascular (β-blocking effects of bornaprolol were studied in healthy male volunteers after four single oral doses. The inhibition of isoproterenol-induced tachycardia was monitored for 72 h in six subjects, and the inhibition of exercise-induced tachycardia and rise of systolic blood pressure were monitored for 167 h in six other subjects. Plasma drug concentrations were determined by gas chromatography. Bornaprolol significantly reduced the resting heart rate, isoproterenol- and… 
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Pharmacokinetics and pharmacodynamics of conventional and controlled-release formulations of metipranolol in man

Relatively constant plasma concentrations and a clinically significant reduction of exercise-induced tachycardia were maintained throughout a 24 h dosing interval and an individual deacetylmetipranolol plasma concentration-effect relationship was evaluated using the Emax model.

Pharmacokinetic characteristics of bornaprolol in healthy volunteers.

Bornaprolol is principally eliminated after metabolism, this process did not increase with increasing oral doses and bioavailability seemed to decrease inversely with oral dose, and maximum plasma concentrations and area under the plasma concentration-time curve increased in a non-dose-dependent manner.