Table 2.
Pharmacological properties of proton-pump inhibitors.
| Variable | Drug | ||||||
|---|---|---|---|---|---|---|---|
| Rabeprazole (Aciphex®) | Pantoprazole (Protonix®) | Lansoprazole (Prevacid®) | Esomeprazole (Nexium®) | Omeprazole (Prilosec®) | Omeprazole IR – sodium bicarbonate (Zegerid®) | Dexlansoprazole (Kapidex™) | |
| Oral dose for active and maintenance therapy of gastroduodenal ulcers (mg) | 20 | 40 | 30 | 40 | 20 | 20–40 | 30–60* |
| Available formulations | Oral | Oral iv. | Oral | Oral iv. | Oral | Oral | Oral |
| pKa | ~5 | ~4 | ~4 | ~4 | ~4 | ~4 | ~4–5 |
| Bioavailability (%) | 52 | 77 | 80–85 | 64 | 30–40 | 30–40 | NA |
| Time to peak plasma concentration (h) | 1.0–2.0 | 1.1–3.1 | 1.7 | 1.5 | 0.5–3.5 | 2 | 1–5 |
| Plasma elimination half-life (h) | 1.0–2.0 | 1.0–1.9 | 1.3–1.7 | 1–1.5 | 0.5–1.0 | 0.4–3.2 | 1–2 |
| Protein binding (%) | 96 | 98 | 97 | 97 | 95 | 95 | 96.1–98.8 |
| Urinary excretion of oral dose (%) | 30–35 | 71–80 | 14–23 | 80 | 77 | 77 | 50.7 |
| Metabolism | Hepatic | Hepatic | Hepatic | Hepatic | Hepatic | Hepatic | Hepatic |
*
Dose registered for erosive esophagitis and gastroesophageal reflux disease.
iv.: Intravenous; NA: Nonavailable.