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  • Title: Plasma levels and negative chronotropic effect of metoprolol following single doses of a conventional and sustained-release formulation.
    Author: Quaterman CP, Kendall MJ, Welling PG.
    Journal: Eur J Clin Pharmacol; 1979 Mar 26; 15(2):97-103. PubMed ID: 436924.
    Abstract:
    Plasma levels and associated reduction in exercise-induced tachycardia have been examined following the administration of single doses of metoprolol in conventional and slow-release tablets at different times to six healthy male subjects. The study was carried out in two parts. Initially, the tablets were given at 9 a.m. and the subjects were studied up to 14 h and then at 24 h. Subsequently, the same doses were given at 9 p.m. and the subjects were studied 12-24 h after drug administration (i.e. 9 a.m.-9 p.m. the next day). After giving the slow-release tablets the peak plasma levels were significantly lower but the drug persisted in the plasma at higher levels than after the conventional tablet. However, the beta-blocking effect was comparable from the two dosages. The results obtained for the period 12-24 h after the evening dose differed from the corresponding values after morning administration in that the plasma levels were higher and the beta-blocking effects more marked. Furthermore, the half-life values calculated from these data were significantly longer.
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