Porovnanie metabolického pomeru metoprolol/α-hydroxymetoprolol po jednorázovom a opakovanom užití

English version

Autoři: J. Ďuricová; I. Peřinová; I. Kacířová; M. Grundmann
Působiště autorů: Department of Clinical Pharmacology, University Hospital Ostrava, and Faculty of Medicine, University of Ostrava, Czech Republic
Vyšlo v časopise: Čes. slov. Farm., 2010; 59, 222-226
Kategorie: Původní práce

Souhrn

Metabolický pomer (MR) metoprololu/α-hydroxymetoprololu za 3 hod po užití jednorázovej dávky metoprololu sa používa na stanovenie fenotypu enzýmu cytochrómu P450 2D6. Cieľom tejto práce bolo porovnať metabolickú aktivitu cytochrómu P450 2D6 po prvom a opakovanom užití metoprololu. Do tejto práce bolo zahrnutých 13 pacientov s hypertenziou (7 žien), u ktorých bolo plánované nasadenie beta-blokátora metoprololu. Vek (priemer ± SD) bol 42,8 ± 12,9 rokov, telesná hmotnosť (priemer ± SD) bola 94,0 ± 25,4 kg. Dávka metoprololu bola u každého pacienta zvolená na základe klinického stavu pacienta v deň užitia prvej tablety. Krvné odbery boli urobené po užití prvej dávky metoprololu a najmenej 2 týždne od nasadenia metoprololu k zaručeniu ustáleného stavu (opakované užívanie). Na základe hodnôt MR boli všetci pacienti po jednorázovom i opakovanom užití zaradení do tej istej fenotypovej skupiny. Pozorovali sme tesnú koreláciu medzi MR po jednorázovom a opakovanom užití metoprololu (r_s = 0,8418, P = 0,0003). Všetci pacienti boli v oboch odberoch zaradení do rovnakej fenotypovej skupiny, extenzivný metabolizátor i napriek signifikantnému rozdielu medzi MR metoprololu/α-hydroxymetoprololu po jednorázovom a opakovanom užití (medián 0,59 vs. 0,81, P = 0,0266), Využitie MR metoprololu/α‑hydroxymetoprololu u pacientov na dlhodobej terapii metoprololom je vhodné pre stanovenie fenotypu enzýmu cytochrómu P450 2D6.

Kľúčové slová:
cytochróm P450 2D6 – fenotyp – substrátová látka – metoprolol

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