Obesity and beta-blockers: influence of body fat on their kinetics and cardiovascular effects.
Beta-blockers are among the most widely used antihypertensive drugs. They differ from each other in regard to several factors such as: beta-agonist activity, beta 1-selectivity and solubility. Aim of this work was to evaluate the influence of obesity on the kinetics and the antihypertensive effect of two Beta-blockers with different solubility such as: the water-soluble, atenolol and the liposoluble, metoprolol. The study was carried out according to an open randomized cross-over design. Eight obese hypertensive patients, after a two week washout period, were randomly allocated to a four week treatment. After a two week intermediate washout period, each patient switched to the other treatment for an additional four week period. On the first and the last day of each treatment the subjects were hospitalized to collect blood samples for the assay of the two drugs and to measure cardiovascular parameters. Obesity does not exert any effect on the kinetics of the water-soluble beta-blocker, atenolol, while markedly interferes with that of the liposoluble, without any apparent influence on its anti-hypertensive effect. These findings extend to obese hypertensives the concept that the plasma concentrations of beta-blocking agents are not reliable predictors of their therapeutic effect.
Galletti
F
F
Institute of Internal Medicine and Metabolic Diseases, Second Medical School, University of Naples, Italy.
Fasano
M L
ML
Ferrara
L A
LA
Groppi
A
A
Montagna
M
M
Mancini
M
M
D000273:Adipose Tissue / Q000378:metabolism*; D001262:Atenolol / Q000097:blood / Q000493:pharmacokinetics* / Q000627:therapeutic use; D001794:Blood Pressure / Q000187:drug effects; D005260:Female; D006339:Heart Rate / Q000187:drug effects; D006801:Humans; D006973:Hypertension / Q000150:complications* / Q000188:drug therapy / Q000378:metabolism; D007700:Kinetics; D008297:Male; D008790:Metoprolol / Q000097:blood / Q000493:pharmacokinetics* / Q000627:therapeutic use; D008875:Middle Aged; D009765:Obesity / Q000150:complications / Q000378:metabolism*; D011897:Random Allocation
D001262:Atenolol; D008790:Metoprolol