A dose ranging study of atenolol in hypertension: fall in blood pressure and plasma renin activity, beta‐blockade and steady‐state pharmacokinetics.

Abstract

I The relationship between the oral dosage and plasma concentration of the long-acting cardioselective /3-adrenoceptor blocker atenolol and the antihypertensive response to the degree of f8-adrenoceptor blockade and change in plasma renin activity (PRA) was evaluated in patients with mild-tomoderate essential hypertension in a double-blind, randomized, between-patient, dose-ranging (25, 50 or 100 mg once daily for 4 weeks) study. 2 The optimum, or minimum, daily dose of atenolol to treat patients with mild-to-moderate hypertension was not clearly identified in this study. A between-treatment comparison did not demonstrate that all blood pressure falls were always less in the 25 mg group than in the other two groups. Calculation of ,8-error or the power for the negative results between doses suggested that a large sample size is required to draw a conclusion that no dose-antihypertensive relationship of atenolol exists in the treatment of mild-to-moderate hypertension. 3 A relatively flat plasma concentration-antihypertensive response relationship was observed. 4 Steady-state plasma concentrations of atenolol were dose-related and renal drug clearance was well correlated with individual creatinine clearance.5 ,3-adrenoceptor blockade was better correlated with plasma atenolol concentration. Correlations which were less strong were between plasma drug concentration and change in various blood pressures and between blood pressure falls and /3-adrenoceptor blockade. 6 There was no relationship between the fall in blood pressure and change in PRA. Atenolol appeared to suppress PRA in an all-or-none fashion.

A ‘Dilute and Shoot’ Liquid Chromatography-Mass Spectrometry Method for Multiclass Drug Analysis in Pre-Cut Dried Blood Spots

“…However, the use of small volume of sample is at the same time an advantage and a weakness whose only solution would be the adoption of very sensitive and powerful instrumentation. This requirement also dictated by the low blood concentrations of the selected drugs at therapeutic doses [ 38 , 39 , 40 , 41 ]. These considerations led us to the use of an UPLC system for the analyte separation and a tandem mass spectrometer for the detection.…”

Losartan and atenolol on hypertension induced by adenosine receptor blockade

“…However, three different mechanisms can account for the effect of atenolol on DPSPX‐induced morphological alterations: (1) the prevention of blood pressure rise avoids its associated vascular changes; (2) the inhibition of renin release due to sympathetic stimulation leads to decreased angiotensin II levels; and (3) the inherent tendency of atenolol to increase cell diameter could offset the inhibition of DPSPX‐induced morphological alterations. However, no correlation has been found between reduction in blood pressure and decrease in plasma renin activity during atenolol treatment (Nilsson, Karlberg, Ohlsson, Thulin & Tolagen, 1979; Ishizaki et al. , 1983).…”

The effect of apixaban on the pharmacokinetics of digoxin and atenolol in healthy subjects

“…An atenolol dose of 100 mg was chosen for this study as representative of the upper end of the dose range. 21 , 29 An apixaban dose of 10 mg was selected on the basis of safety data available at the time, and reflected exposures likely to be observed in patients, as the Phase 3 clinical trials evaluated apixaban doses ranging from 2.5 to 10 mg twice daily for reducing the risk of stroke in NVAF, prophylaxis of thrombosis-related events following hip or knee replacement surgery, or treatment of DVT and PE. 3 – 9 , 30 Atenolol 100-mg tablets were supplied by the investigator and manufactured by AstraZeneca Pharmaceuticals LP (Wilmington, DE, USA), and apixaban 5-mg tablets were supplied and manufactured by Bristol-Myers Squibb Company.…”