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The racemic metoprolol H 2 ‐antagonist interaction
Author(s) -
Toon Stephen,
Davidson Eva M,
Garstang Fiona M,
Batra Harsh,
Bowes Robert J,
Rowland Malcolm
Publication year - 1988
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1038/clpt.1988.34
Subject(s) - metoprolol , cimetidine , pharmacology , pharmacokinetics , pharmacodynamics , bioavailability , enantiomer , ranitidine , chemistry , clinical pharmacology , antagonist , drug interaction , medicine , anesthesia , receptor , stereochemistry , biochemistry
The effects of concomitant administration of cimetidine and ranitidine on the pharmacokinetics and pharmacodynamics of multiple‐dose metoprolol were investigated in 12 normal, healthy male volunteers. The pharmacokinetics of metoprolol were assessed in terms of racemic metoprolol and the individual (R)– and (S)–enantiomers with a stereoselective assay. Ranitidine had no effect on the pharmacodynamics or pharmacokinetics of metoprolol. Although not affecting the pharmacodynamics of metoprolol, cimetidine did produce an increase in the bioavailability of metoprolol through inhibition of enzymes responsible for the first‐pass elimination of the β‐blocker. The effect was stereoselective, with the major effect being on the less pharmacologically active (R)–enantiomer. Clinical Pharmacology and Therapeutics (1988) 43, 283–289 doi: 10.1038/clpt.1988.34