PMID: 7371709Feb 1, 1980Paper

A single and multiple dose pharmacokinetic and pharmacodynamic comparison of conventional and slow-release metroprolol

European Journal of Clinical Pharmacology
M J KendallP G Welling

Abstract

Pharmacokinetic and pharmacodynamic profiles for metoprolol have been measured in six healthy volunteers after single and multiple dosing with 100 mg conventional formulation twice daily and 200 mg slow-release formulation once daily. Both multidose regimes produced measurable predosing plasma concentrations of metoprolol. The plasma concentrations on the eighth day were greater than predicted by the single-dose data as indicated by the comparison of the total areas under the curve for the single dose and the dosage interval areas during multiple dosing. This increase may be associated with a change in the bioavailability and/or clearance of the drug and is currently being investigated. The peak concentrations for the two regimens were comparable but the times to peak with the slow-release regimen were significantly delayed. Both regimes produced significant beta-blocking effects over 24 h during multiple dosing, the reductions in exercise heart rate at 0 and 24 h on the eighth day corresponding to more than 20% of the maximum effect. Resting pulse rates and blood pressures were affected to a similar extent by the two regimens but neither significantly altered respiratory peak flow rates. The effects during multiple dosing were...Continue Reading

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Citations

Jan 1, 1982·European Journal of Clinical Pharmacology·D S LawrenceJ M Cruickshank
Apr 1, 1985·European Journal of Drug Metabolism and Pharmacokinetics·J MattilaP Männistö
Jan 1, 1983·Pharmacology & Therapeutics·M J Kendall, L Beeley
Aug 1, 2000·International Journal of Pharmaceutics·S A Mostafavi, R T Foster
Apr 21, 1983·The New England Journal of Medicine
Aug 20, 2010·AAPS PharmSciTech·Sabahuddin SiddiquePapiya Bigoniya
Jun 27, 2002·Clinical Pharmacokinetics·William H Frishman, Mamata Alwarshetty
Jan 1, 1985·European Journal of Clinical Pharmacology·M van BaakF T Verstappen
Aug 11, 2010·International Journal of Pharmaceutics·R KumaravelrajanK Bhaskar
Nov 11, 2006·British Journal of Clinical Pharmacology·Jean LefebvreYves Lacourciere
Nov 10, 1983·The American Journal of Cardiology·M J Kendall, V A John
Jun 1, 1989·Journal of Clinical Pharmacy and Therapeutics·M J Kendall
Jun 1, 1983·Journal of Clinical and Hospital Pharmacy·M J Kendall, S R Smith
Aug 1, 1983·British Journal of Clinical Pharmacology·D B JackC P Quarterman
Mar 1, 1982·Journal of Clinical and Hospital Pharmacy·M J KendallD J Worthington
Jan 1, 1985·British Journal of Clinical Pharmacology·J GodbillonJ Hirtz
May 1, 1987·Journal of Clinical Pharmacology·D C GargD J Weidler
May 1, 1981·British Journal of Clinical Pharmacology·D W Harron, R G Shanks
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Nov 10, 1983·The American Journal of Cardiology·M J Kendall
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Sep 1, 1984·British Journal of Clinical Pharmacology·M J KendallS Rolf Smith
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Jul 16, 2019·Thérapie·Béatrice BouhanickPeggy Gandia

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