Results of noncomparmental pharmacokinetic analysis of metoprolol enantiomers in 20 healthy, young women (16 extensive and four poor metabolizers) after the administration of 100 mg of metoprolol tartrate in the absence or presence of diphenhydramine dosed to steady state Results presented as mean ± S.D.
Parameter | EM (n = 16) | PM (n = 4) | ||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| R-MET-PCB | S-MET-PCB | R-MET-DPH | S-MET-DPH | R-MET-PCB | S-MET-PCB | R-MET-DPH | S-MET-DPH | |||||||
| Cmax (μmol/l) | 0.38 ± 0.20a | 0.51 ± 0.23b | 0.53 ± 0.17c | 0.65 ± 0.18d | 0.84 ± 0.15 | 0.90 ± 0.15 | 0.72 ± 0.17 | 0.79 ± 0.21 | ||||||
| Tmax (h) | 1.69 ± 0.63 | 1.72 ± 0.68 | 1.97 ± 0.7 | 2.02 ± 0.71 | 1.75 ± 0.20 | 1.75 ± 0.20 | 2.06 ± 0.72 | 2.06 ± 0.72 | ||||||
| t1/2 (h) | 2.74 ± 0.95a | 3.02 ± 0.90b | 3.98 ± 0.93c | 4.24 ± 0.93d | 7.4 ± 0.38 | 7.11 ± 0.95 | 7.38 ± 0.98 | 6.79 ± 0.63 | ||||||
| AUC0-∞ (μmol · h/l) | 1.63 ± 0.92a | 2.44 ± 1.25b | 3.39 ± 1.56c | 4.49 ± 1.84d | 8.5 ± 1.3 | 8.67 ± 1.3 | 7.01 ± 1.81 | 7.04 ± 1.24 | ||||||
| CL/F (l/h) | 147 ± 124a | 88.7 ± 68.4b | 55.6 ± 33.3c | 39.8 ± 21d | 17.5 ± 2.6 | 17.1 ± 2.52 | 21.8 ± 5.2 | 21.2 ± 3.28 | ||||||
| CLR (l/h) | 4.10 ± 2.18 | 3.86 ± 2.01 | 3.86 ± 1.46 | 3.73 ± 1.35 | 3.98 ± 0.82 | 3.41 ± 0.79 | 5.33 ± 2.85 | 4.74 ± 2.32 | ||||||
| CLNR (l/h) | 143.4 ± 123a | 85.66 ± 67.1b | 52.4 ± 32.9c | 36.7 ± 20.5d | 13.8 ± 1.48 | 13.9 ± 1.5 | 17.45 ± 2.60 | 16.41 ± 1.29 | ||||||