Table 1.
Pharmacokinetic parameters of omeprazole and its metabolites with and without moclobemide (mean and 95% confidence interval).
| EM | PM | |||
|---|---|---|---|---|
| Omeprazole only (6 subjects) | +Moclobemide (8 subjects) | Omeprazole only (7 subjects) | +Moclobemide (8 subjects) | |
| Omeprazole | ||||
| tmax (h) | 1.83 (0.43, 3.23) | 2.18 (1.25, 3.11) | 2.14 (1.53, 2.75) | 2.45 (1.59, 3.31) |
| Cmax (ng ml−1) | 986.56 | 1649.31 | 2651.93 | 2609.33 |
| (413.65, 1559.47) | (1053.90, 2244.72)† | (1983.98, 3319.88) | (2136.78, 3081.88) | |
| t½ (h) | 1.58 (0.88, 2.28) | 1.66 (0.61, 2.71) | 2.06 (1.31, 2.81) | 2.70 (2.25, 3.15) |
| AUC(0,24 h) (ng ml−1 h) | 1834.34 | 3759.82 | 10424.84 | 12137.77 |
| (444.21, 3224.47) | (2268.22, 5251.42)† | (8103.49, 12746.19) | (9329.81, 14945.73) | |
| AUC(0,∞) (ng ml−1 h) | 1821.37 | 3774.26 | 10348.26 | 12112.38 |
| (448.94, 3193.8) | (2257.95, 5290.57)† | (7933.80, 12762.72) | (9267.89, 14956.87) | |
| Vd/F (l) | 104.11 (0, 235.24)* | 26.46 (13.52, 39.40)† | 11.63 (7.79, 15.47) | 13.48 (9.88, 17.08) |
| CL/F (l h−1) | 36.63 (6.16, 67.1) | 13.01 (6.90, 19.12)† | 4.02 (3.29, 4.75) | 3.55 (2.63, 4.47) |
| MRT (h) | 2.74 (1.40, 4.08) | 3.32 (2.05, 4.59) | 4.58 (3.56, 5.60) | 5.29 (4.52, 6.06) |
| Omeprazole sulphone | ||||
| Cmax (ng ml−1) | 123.89 (80.04, 167.74) | 247.53 (98.39, 396.67)† | 479.11 (319.68, 638.54) | 549.17 (351.13, 747.21) |
| AUC(0,24 h) (ng ml−1 h) | 798.98 | 2141.60 | 5648.47 | 7501.15 |
| (123.86, 1474.10) | (877.28, 3405.92)† | (4296.86, 7000.08) | (5278.57, 9723.73) | |
| AUC(0,∞) (ng ml−1 h) | 797.03 | 2215.67 | 6449.61 | 9349.84 |
| (102.82, 1491.24) | (1021.32, 3410.02)† | (5172.79, 7726.43) | (6896.11, 11803.57) | |
| AUC ratio (OMP/OMP-S) | 2.45 (1.97, 2.93) | 2.15 (1.50, 2.80) | 1.94 (1.24, 2.64) | 1.77 (1.13, 2.41) |
| 5-Hydroxyomeprazole | ||||
| Cmax (ng ml−1) | 350.34 (187.51, 513.17) | 206.03 (169.18, 242.88)† | 95.73 (56.34, 135.12) | 49.43 (30.88, 67.98)† |
| AUC(0,24 h) (ng ml−1 h) | 711.29 (550.14, 872.44) | 720.79 (576.59, 864.99) | 451.18 (297.02, 605.34) | 365.17 (227.30, 503.04)† |
| AUC(0,∞) (ng ml−1 h) | 711.71 (558.58, 864.84) | 710.23 (570.81, 849.65) | 436.88 (287.83, 585.93) | 356.09 (214.71, 497.47)† |
| AUC ratio (OMP/OH) | 2.50 (0.84, 4.56) | 5.31 (0, 14.76)†* | 25.67 (15.56, 35.78) | 38.02 (21.48, 54.56) |
†
P value<0.05 by Wilcoxon signed rank test when compared with omeprazole only data in the same genotype group.
*
lower margin of confidence interval smaller than 0.
OMP: Omeprazole.
OH: 5-Hydroxyomeprazole.
OMP-S: Omeprazole sulphone.