Version May 2024
| Agent | Regimen tested | Oral bioavailability | Time to peak (hours) | Cmax (micrograms/mL) | AUC0-24 (mg•h/L) | Metabolism and clearance | Half-life (hours)* | pKa¶ |
| Dexlansoprazole | 30 mg once daily | May be increased if taken with food | 1 to 2 (peak 1) 4 to 5 (peak 2) | 0.7 | 3.3 | Hepatically by CYP2C19Δ and 3A4; inactive metabolites are excreted in urine and feces | 1 to 2 | Not available |
| Esomeprazole | 20 mg once daily | 64% (single dose); 90% (after multiple doses if taken on an empty stomach; bioavailability is reduced by approximately 50% if taken with food) | 1 to 1.6 | 2.1 (micromol/L) | 4.2 (micromol•h/L) | Hepatically by CYP2C19Δ and 3A4; inactive metabolites are excreted in urine and feces | 1.2 to 1.5 | 4.0 |
| Lansoprazole | 30 mg once daily | >80% (taken on an empty stomach; absorption is reduced by approximately 50 to 70% if taken with food) | 1.5 to 3 | 0.5 to 1.0 | 3.2 | Hepatically by CYP2C19Δ and 3A4; inactive metabolites are excreted in feces via bile and in urine | 0.9 to 1.5 | 4.0 |
| Omeprazole | 20 mg once daily (delayed release capsule) | 30 to 45% (single dose) Varies by formulation; absorption is significantly increased after multiple doses | 0.5 to 3.5 | 0.7 | 3.3 | Hepatically by CYP2C19Δ and 3A4; inactive metabolites are excreted in urine and bile | 0.5 to 1 | 4.0 |
| Pantoprazole | 40 mg once daily | Approximately 77% | 2.5 | 2.5 | 4.8 (range 1.4 to 13.3) | Hepatically by CYP2C19Δ and 3A4; inactive metabolites are excreted in urine and feces via bile | 1 (increased to 3.5 to 10 hours in CYP2C19 poor metabolizers) | 3.9 |
| Rabeprazole | 20 mg once daily | Approximately 52% | 2 to 5 (delayed up to 4 hours if taken with high fat meal) | 0.4 to 0.48 | 0.9 | Hepatically by CYP2C19Δ and 3A4; inactive metabolites are excreted in urine and feces via bile | 1 to 2 | 5.0 |
AUC0-24: cumulative systemic drug exposure as measured by the area under the plasma concentration versus time curve over 24 hours; Cmax: maximum plasma concentration; pKa: acid dissociation constant transformed by negative log; PPI: proton pump inhibitor.
* Reported half-lives of 1 to 2 hours refer to conversion of the parent prodrug to active (thiophilic sulfenamide) form; half-life of the active form is considerably longer. The duration of antisecretory effect of PPIs exceeds that predicted by half-life due to irreversible binding at site of action (ie, parietal proton pumps).
¶ PPIs are converted to their active form (ie, protonated) when pH of parietal cell is lower than pKa of the individual PPI (ie, in presence of gastric acidity). For detail, refer to accompanying text.
Δ Drug metabolism via hepatic CYP2C19 enzymes is polymorphic; thus, PPI systemic exposure (AUC0-24) can be increased several (ie, 2 to 12) times in patients who are intermediate or poor metabolizers compared with those who are extensive metabolizers (ie, most patients). Up to 20 to 30% of persons within certain South and East Asian populations are CYP2C19 poor metabolizer phenotypes.[1]Data from:
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