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.