Celecoxib inhibits metabolism of cytochrome P450 2D6 substrate metoprolol in humans.
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Celecoxib inhibits metabolism of cytochrome P450 2D6 substrate metoprolol in humans. / Werner, Ulrike; Werner, Dierk; Rau, Thomas; Fromm, Martin F; Hinz, Burkhard; Brune, Kay.
in: CLIN PHARMACOL THER, Jahrgang 74, Nr. 2, 2, 2003, S. 130-137.Publikationen: SCORING: Beitrag in Fachzeitschrift/Zeitung › SCORING: Zeitschriftenaufsatz › Forschung › Begutachtung
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TY - JOUR
T1 - Celecoxib inhibits metabolism of cytochrome P450 2D6 substrate metoprolol in humans.
AU - Werner, Ulrike
AU - Werner, Dierk
AU - Rau, Thomas
AU - Fromm, Martin F
AU - Hinz, Burkhard
AU - Brune, Kay
PY - 2003
Y1 - 2003
N2 - OBJECTIVE: In vitro data have shown that celecoxib inhibits the metabolism of cytochrome P450 (CYP) 2D6 substrates. However, very limited data are available on the influence of cyclooxygenase 2 inhibitors on the disposition of CYP2D6 substrates in humans. Therefore the objective of this study was to examine the effect of celecoxib and rofecoxib on the pharmacokinetics of the clinically relevant CYP2D6 substrate metoprolol. METHODS: An open, randomized, 3-period crossover study was performed in 12 healthy male volunteers. Metoprolol (50 mg) was given in all 3 periods without or after 7 days of pretreatment with celecoxib (200 mg twice daily) or rofecoxib (25 mg daily) to achieve steady-state conditions of cyclooxygenase 2 inhibitors in periods 2 and 3. RESULTS: Celecoxib significantly increased the area under the plasma concentration-time curve of metoprolol from 271 to 414 micro g. h/L (64% +/- 57%, P
AB - OBJECTIVE: In vitro data have shown that celecoxib inhibits the metabolism of cytochrome P450 (CYP) 2D6 substrates. However, very limited data are available on the influence of cyclooxygenase 2 inhibitors on the disposition of CYP2D6 substrates in humans. Therefore the objective of this study was to examine the effect of celecoxib and rofecoxib on the pharmacokinetics of the clinically relevant CYP2D6 substrate metoprolol. METHODS: An open, randomized, 3-period crossover study was performed in 12 healthy male volunteers. Metoprolol (50 mg) was given in all 3 periods without or after 7 days of pretreatment with celecoxib (200 mg twice daily) or rofecoxib (25 mg daily) to achieve steady-state conditions of cyclooxygenase 2 inhibitors in periods 2 and 3. RESULTS: Celecoxib significantly increased the area under the plasma concentration-time curve of metoprolol from 271 to 414 micro g. h/L (64% +/- 57%, P
M3 - SCORING: Zeitschriftenaufsatz
VL - 74
SP - 130
EP - 137
JO - CLIN PHARMACOL THER
JF - CLIN PHARMACOL THER
SN - 0009-9236
IS - 2
M1 - 2
ER -
