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Pharmacokinetics

Absorption

Bioavailability

Well absorbed from GI tract (absolute bioavailability >80%). Peak plasma concentrations attained about 1.7 hours after oral administration.

Onset

Increased gastric pH occurred within 1–2 or 2–3 hours after a single 30- or 15-mg oral dose, respectively.

Duration

Gastric acid secretion normalized over 2–4 days after discontinuance; no apparent rebound.

Food

Absorption (peak plasma concentration, AUC) decreased by 50–70% when administered 30 minutes after food. No substantial food effect when administered before meals.

Special Populations

Peak plasma concentration and time to peak plasma concentration in patients with renal impairment similar to healthy individuals.

Peak plasma concentrations were comparable in patients in Asian and US studies.

Distribution

Extent

Distributed into milk in rats; not known whether distributed into human milk.

Prolonged binding to gastric parietal proton pump enzyme.

Plasma Protein Binding

97%.

Special Populations

Severe renal impairment decreased plasma protein binding by 1–1.5% after administration of 60 mg dose.

Elimination

Metabolism

In parietal cell secretory canaliculi, thought to be transformed into 2 active sulfenamide metabolites not present in systemic circulation. Also metabolized in the liver by CYP3A4 and CYP2C19. Metabolites found in plasma are inactive.

Elimination Route

Excreted principally in feces (about 67%) with remainder in urine; no unchanged drug excreted in urine.

Half-life

<2 hours.

Special Populations

Hepatic impairment increased plasma half-life to 3.2–7.2 hours.

Renal impairment decreased elimination half-life.

Stability

Storage

Oral

Capsules, Granules for Suspension, and Orally Disintegrating Tablets

25°C (may be exposed to 15–30°C).

Prevacid^® NapraPAC^® Kit

25°C (may be exposed to 15–30°C). Store and dispense in original container.

Prevpac^® Kit

20–25°C. Protect from light and moisture.

Parenteral

Powder for IV Infusion

Powder: 25°C (may be exposed to 15–30°C). Protect from light.

Reconstituted solution: 25°C for up to 1 hour before further dilution.

Admixture: 25°C for up to 12 hours (in 50 mL of 5% dextrose injection) or 24 hours (in 50 mL of lactated Ringer’s or 0.9% sodium chloride injection).

Compatibility

Oral

Capsules

Immediately use extemporaneous mixtures of capsule contents and food or juice. (See Oral Administration under Dosage and Administration.)

Granules for Suspension

Use immediately after mixing with water.

Parenteral

Solution Compatibility

Reconstitute powder with sterile water for injection; use of other diluents may result in precipitate or particulate formation. Further dilution in 5% dextrose, lactated Ringer’s, or 0.9% sodium chloride injection recommended by manufacturer.

Actions

• Inhibits basal and stimulated gastric acid secretion.
• Concentrates in acid conditions of parietal cell secretory canaliculi; forms active sulfenamide metabolite that irreversibly binds to and inactivates hydrogen-potassium ATPase (proton- or acid pump), blocking final step in secretion of hydrochloric acid.
• Acid secretion is inhibited until additional hydrogen-potassium ATPase is synthesized, resulting in prolonged duration of action.
• Combined therapy with lansoprazole and appropriate anti-infectives (i.e., amoxicillin, clarithromycin) can effectively eradicate H. pylori infection.