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Pharmacokinetics

Absorption

Bioavailability

Bioavailability is 64% after a single 40-mg oral dose. Bioavailability is 90% after repeated oral doses of 40 mg once daily.

Food

AUC decreased by 43–53% when a 40-mg oral dose was administered with food.

Special Populations

Following oral dosage of 40 mg once daily in patients with severe (Child-Pugh class C) hepatic impairment, steady-state AUCs were 2–3 times greater than those in patients with normal hepatic function.

Distribution

Extent

Not known whether esomeprazole is distributed into milk, but omeprazole is distributed into milk. Not known whether esomeprazole crosses the placenta.

Prolonged binding to gastric parietal proton pump enzyme.

Plasma Protein Binding

97%.

Elimination

Metabolism

Metabolized to inactive metabolites in the liver by CYP isoenzymes, principally by CYP2C19, and to lesser extent by CYP3A4.

Elimination Route

Excreted principally in urine (80% as inactive metabolites, <1% as active drug); remainder in feces as inactive metabolites.

Half-life

Adults, oral administration: 1–1.5 hours. Slower elimination than R-omeprazole or racemic omeprazole (0.5–1 hour).

Adults, IV administration: 1.1–1.4 hours; prolonged with increasing dose.

Adolescents 12–17 years of age, oral administration: 0.8–1.2 hours.

Special Populations

In patients with poor CYP2C19 metabolizer phenotype, steady-state AUCs were 2 times greater than those in patients with extensive (or rapid) metabolizer phenotype.

Stability

Storage

Oral

Capsules

25°C (may be exposed to 15–30°C) in tightly-closed containers.

Parenteral

Powder for IV Injection or Infusion

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

Reconstituted solution: Room temperature (up to 30°C) for up to 12 hours.

Admixture: Room temperature (up to 30°C) for up to 6 hours (in 50 mL of 5% dextrose injection) or 12 hours (in 50 mL of lactated Ringer’s or 0.9% sodium chloride injection).

Compatibility

Oral

Capsules

Use extemporaneous mixture of capsule contents (enteric-coated pellets) and applesauce immediately; do not store for future use. Applesauce should not be hot.

Parenteral

Solution Compatibility

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.
• More esomeprazole reaches and blocks proton pump than does R-omeprazole; therefore, provides greater intragastric pH control than racemic omeprazole.
• Suppresses H. pylori in patients with duodenal ulcer and/or reflux esophagitis who are infected with the organism. Combined therapy with esomeprazole and appropriate anti-infectives (i.e., amoxicillin, clarithromycin) can effectively eradicate H. pylori gastric infection.

Advice to Patients

Pending revision, the material in this section should be considered in light of more recently available information in the MEDWATCH notification at the beginning of this monograph.

• Importance of swallowing capsule intact, without crushing or chewing.
• Importance of taking 1 hour before a meal.
• If mixed with applesauce for administration, importance of mixing capsule contents with applesauce soft enough to swallow without chewing. Importance of not using hot applesauce. Importance of immediately swallowing mixture without crushing or chewing; do not store for later use.
• Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs. Antacids may be used concomitantly as needed for pain relief.
• Importance of women informing their clinicians if they are or plan to become pregnant or plan to breast-feed.
• Importance of informing patients of other important precautionary information. (See Cautions.)