TABLE 1

Noncompartmental pharmacokinetics of racemic metoprolol 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 ± standard deviation.


Parameter

EM (n = 16)

PM (n = 4)
MET-PCB
MET-DPH
MET-PCB
MET-DPH
Cmax (μmol/l) 0.89 ± 0.42 1.18 ± 0.34a 1.74 ± 0.31b 1.50 ± 0.38b
Tmax (h) 1.69 ± 0.63 1.97 ± 0.70 1.75 ± 0.20 2.06 ± 0.72
t1/2 (h) 2.88 ± 0.80 3.95 ± 0.81a 7.44 ± 0.8b 7.08 ± 0.80b
AUC0—∞ (μmol · h/l) 4.05 ± 2.15 7.76 ± 3.34a 17.18 ± 2.48b 14.08 ± 3b
CL/F (l/h) 111 ± 90 47 ± 26a 17 ± 2.5b 21 ± 4b
CLR (l/h) 3.98 ± 2.14 3.81 ± 1.39 3.64 ± 0.48 4.71 ± 1.99
CLNR (l/h) 107.23 ± 89.12 42.99 ± 24.95a 13.61 ± 2.29b 16.71 ± 4.10b
CLMET→α-OH-MET (l/h)
11.97 ± 12.70
3.91 ± 3.21a
0.04 ± 0.01b
0.04 ± 0.01b
  • a P < 0.05 EMs placebo versus EMs diphenhydramine.

  • b P < 0.05 significantly different between EMs and PMs in placebo as well as diphenhydramine week.