Timolol pharmacokinetics and effects on heart rate and blood pressure after acute and chronic administration

摘要: The pharmacokinetics and effects of various oral doses timolol administered either acutely or after chronic medication for 7 days were studied in healthy volunteers. After acute administration maximum plasma concentrations attained within 1–2 h thereafter declined exponentially with time. mean apparent half-life elimination from was 2.5 independent dose. Area under the concentration-time curve (AUC) proportional to orally Plasma concentrations, AUC not altered one week administration. effect on heart rate blood pressure response three sequentially increasing ‘steady state’ work loads studied. reduction systolic pressure, resting rate, different parameters work-heart (or pressure) relationships produced by 5 mg timolol. Increasing dose prolonged duration over which these variables reduced. relationship between concentration inhibition exercise hyperbolic half at about 3–4 ng/ml above 30 ng/ml. Maximum drug action similar