Pharmacokinetic characteristics of omeprazole, esomeprazole, lansoprazole, pantoprazole, and rabeprazole following repeated oral doses in healthy subjects The recommended daily doses for these five PPIs are 20 mg for omeprazole, 40 mg for esomeprazole, 30 mg for lansoprazole, 40 mg for pantoprazole, and 20 mg for rabeprazole.
PPI | Oral Dose | CYP2C19 Genotype | Cmax | AUC | t1/2β | Reference | ||
|---|---|---|---|---|---|---|---|---|
| mg | μM | μmol · h/l | h | |||||
| Omeprazole | 20 (7th day) | EM | Mean ± S.D. | 1.6 ± 1.0 | 2.9 ± 2.8 | 0.8 ± 0.4 | Yasuda et al., 1995 | |
| PM | Mean ± S.D. | 3.1 ± 0.9 | 12.7 ± 7.2 | 2.1 ± 0.6 | ||||
| 20 (7th day) | EM | Mean ± S.D. | 1.1 ± 0.6 | 2.2 ± 1.9 | 0.9 ± 0.2 | Andersson et al., 1998 | ||
| PM | Mean | 3.2 | 12.0 | 2.3 | ||||
| 20 (8th day) | EM | Mean ± S.E.M. | 3.1 ± 0.6 | Shirai et al., 2001 | ||||
| PM | Mean ± S.E.M. | 20.7 ± 1.9 | ||||||
| Esomeprazole | 40 (5th day) | EM | Mean | 5.2 | 14.1 | AstraZeneca, 2002, data on file | ||
| PM | Mean | 6.7 | 19.7 | |||||
| Lansoprazole | 30 (7th day) | EM | Mean ± S.D. | 2.2 ± 0.7 | 4.9 ± 2.1 | 1.1 ± 0.3 | Andersson et al., 1998 | |
| PM | Mean | 4.8 | 28.8 | 4.8 | ||||
| 30 (8th day) | EM | Mean ± S.E.M. | 2.0 ± 0.3 | 4.6 ± 0.8 | 1.2 ± 0.1 | Ieiri et al., 2001 | ||
| PM | Mean ± S.E.M. | 3.8 ± 1.1 | 17.9 ± 2.4 | 3.9 ± 0.2 | ||||
| Pantoprazole | 40 (7th day) | EM | Mean ± S.D. | 5.4 ± 1.4 | 9.5 ± 3.5 | 1.3 ± 0.3 | Andersson et al., 1998 | |
| PM | Mean | 9.7 | 61.7 | 6.3 | ||||
| 80 (7th day) | EM | Mean ± S.D. | 12.8 ± 2.8 | 27.2 ± 6.5 | 1.2 ± 0.2 | Tanaka et al., 1996 | ||
| PM | Mean | 30.2 | 279.2 | 8.7 | ||||
| Rabeprazole | 20 (7th day) | EM | Mean ± S.D. | 1.2 ± 0.7 | 2.0 ± 0.9 | 1.0 ± 0.6 | Yasuda et al., 1995 | |
| PM | Mean ± S.D. | 1.7 ± 0.9 | 3.9 ± 1.1 | 1.6 ± 0.4 | ||||
| 20 (8th day) | EM | Mean ± S.E.M. | 1.3 ± 0.3 | Shirai et al., 2001 | ||||
| PM | Mean ± S.E.M. | 6.8 ± 0.5 | ||||||
| 10 (8th day) | EM | Mean ± S.E.M. | 0.6 ± 0.3 | 1.1 ± 0.3 | 0.9 ± 0.3 | Ieiri et al., 2001 | ||
| PM | Mean ± S.E.M. | 1.4 ± 0.3 | 4.1 ± 0.5 | 2.1 ± 0.1 | ||||
| Rabeprazole | 20 (7th day) | EM | Mean ± S.D. | 0.3 ± 0.2 | 2.4 ± 1.6 | 2.8 ± 0.7 | Yasuda et al., 1995 | |
| Thioether | PM | Mean ± S.D. | 0.6 ± 0.3 | 4.2 ± 3.2 | 3.0 ± 1.4 | |||
| 20 (8th day) | EM | Mean ± S.E.M. | 1.7 ± 0.5 | Shirai et al., 2001 | ||||
| PM | Mean ± S.E.M. | 4.9 ± 0.9 | ||||||
| 10 (8th day) | EM | Mean ± S.E.M. | 0.2 ± 0.06 | 0.8 ± 0.2 | 2.0 ± 0.2 | Ieiri et al., 2001 | ||
|
|
| PM | Mean ± S.E.M. | 0.26 ± 0.03 | 2.1 ± 0.3 | 6.2 ± 1.0 |
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Cmax, peak plasma drug concentration; t1/2β, terminal elimination half-life.