Achieving optimal beta(1)-blockade with metoprotol CR/Zok

Authors
Citation
J. Wikstrand, Achieving optimal beta(1)-blockade with metoprotol CR/Zok, BAS R CARD, 95, 2000, pp. 46-51
Citations number
14
Categorie Soggetti
Cardiovascular & Hematology Research
Journal title
BASIC RESEARCH IN CARDIOLOGY
ISSN journal
03008428 → ACNP
Volume
95
Year of publication
2000
Supplement
1
Pages
46 - 51
Database
ISI
SICI code
0300-8428(2000)95:<46:AOBWMC>2.0.ZU;2-9
Abstract
The metoprolol CR/Zok is a multi-unit formulation containing metoprolol suc cinate controlled release (CR/Zok) in the form of individual drug delivery units (microcapsules). Each microcapsule acts as a diffusion cell and is de signed to deliver metoprolol succinate at a near constant rate for about 20 hours independently of food intake, pH and other physiological variations. Taking the half-life of metoprolol into account this yields an even plasma concentration over 24 hours with a once daily dosage scheme. The formulati on allows for once daily dosing,, avoiding peaks and troughs in the plasma concentration of the drug. This leads to an even beta(1)-blockade over 24 h ours in dose ranges from 12.5 mg to 200 mg once daily. Plasma fluctuations are considerably decreased compared with immediate release formulations and cardioselectivity is well maintained also on 200 mg CR/Zok. Vital importan t beta(1)-blockade is maintained for 24 hours. Metoprolol CR/Zok is well to lerated and well-being has been shown to be improved with metoprolol CR/Zok in patients with chronic heart failure as illustrated in the findings from the MERIT-HF study.