Lipid effects of celiprolol, a new cardioselective beta-blocker, versus propranolol.
The metabolic effects of celiprolol, a new beta-adrenoceptor blocking agent with intrinsic sympathomimetic activity and alpha 2-blocking properties, were evaluated in a series of patients with hypertension, both with and without hyperlipidemia. Propranolol was tested as the reference drug in a randomized double-blind trial. Of the 35 patients of both sexes who completed the study, 17 were hyperlipidemic (low-density lipoprotein cholesterol greater than or equal to 170 mg/dl) and 18 were normolipidemic. Both drugs exerted a similar hypotensive effect after gradual dose adjustment; however, propranolol reduced heart rate to a higher extent (-20.5%) than celiprolol (-7.7%). Propranolol determined a significant rise of total and very low-density lipoprotein (VLDL) associated triglyceridemia, whereas high-density lipoprotein cholesterol (HDL cholesterol) levels and the total cholesterol/HDL cholesterol ratios were significantly depressed, particularly in hyperlipidemic patients. Celiprolol, in contrast, slightly decreased triglyceridemia (significantly in the hyperlipidemic group at week 12) and caused a 5% increase of the HDL cholesterol levels. The total cholesterol/HDL cholesterol ratio was reduced by celiprolol at week 16 in both hyperlipidemic and normolipidemic patients. The effects of the two beta-adrenoceptor blockers on HDL cholesterol and triglyceride levels differed significantly after 12 and 16 weeks of treatment, which confirm the divergent metabolic effects of the two agents.
Sirtori
C R
CR
Center E. Grossi Paoletti University of Milan, Italy.
Johnson
B
B
Vaccarino
V
V
Montanari
G
G
Cremoncini
M
M
Gianfranceschi
G
G
Sirtori
M
M
Dujovne
C A
CA
D000319:Adrenergic beta-Antagonists / Q000627:therapeutic use*; D000328:Adult; D000368:Aged; D017272:Celiprolol; D002784:Cholesterol / Q000097:blood; D002851:Chromatography, High Pressure Liquid; D004311:Double-Blind Method; D004341:Drug Evaluation; D005260:Female; D006339:Heart Rate / Q000187:drug effects; D006801:Humans; D006949:Hyperlipidemias / Q000150:complications; D006973:Hypertension / Q000097:blood* / Q000150:complications / Q000188:drug therapy; D008055:Lipids / Q000097:blood*; D008074:Lipoproteins / Q000097:blood; D008297:Male; D008875:Middle Aged; D011412:Propanolamines / Q000627:therapeutic use*; D011433:Propranolol / Q000627:therapeutic use*; D011897:Random Allocation; D014280:Triglycerides / Q000097:blood
D000319:Adrenergic beta-Antagonists; D008055:Lipids; D008074:Lipoproteins; D011412:Propanolamines; D014280:Triglycerides; D002784:Cholesterol; D011433:Propranolol; D017272:Celiprolol