section name header

Pronunciation

es-oh-MEP-ra-zole

Classifications

Therapeutic Classification: antiulcer agents

Pharmacologic Classification: proton pump inhibitors

Indications

BEERS REMS


OTC

Action

  • Binds to an enzyme on gastric parietal cells in the presence of acidic gastric pH, preventing the final transport of hydrogen ions into the gastric lumen.
Therapeutic effects:
  • Diminished accumulation of acid in the gastric lumen with lessened gastroesophageal reflux.
  • Healing of duodenal ulcers.
  • Decreased incidence of gastric ulcer during continuous NSAID therapy.

Pharmacokinetics

Absorption: 90% absorbed following oral administration; food absorption.

Distribution: Unknown.

Protein Binding: 97%.

Metabolism/Excretion: Primarily metabolized by the liver via the CYP2C19 isoenzyme, with some metabolism by the CYP3A4 isoenzyme; (the CYP2C19 enzyme system exhibits genetic polymorphism; 15–20% of Asian patients and 3–5% of Caucasian and Black patients may be poor metabolizers and may have significantly esomeprazole concentrations and an risk of adverse effects);<1% excreted unchanged in urine.

Half-Life: Children 1–11 yr: 0.42–0.88 hr; Adults: 1.0–1.5 hr.

Time/Action Profile

(plasma concentrations*)

ROUTEONSETPEAKDURATION
POrapid1.6 hr24 hr
IVrapidend of infusion24 hr



*Resolution of symptoms takes 5–8 days.

Contraind./Precautions

Contraindicated in:

Use Cautiously in:

Adv. Reactions/Side Effects

Derm: ACUTE GENERALIZED EXANTHEMATOUS PUSTULOSIS, cutaneous lupus erythematosus, DRUG REACTION WITH EOSINOPHILIA AND SYSTEMIC SYMPTOMS (DRESS), STEVENS-JOHNSON SYNDROME, TOXIC EPIDERMAL NECROLYSIS

F and E: hypocalcemia (especially if treatment duration 3 mo), hypokalemia (especially if treatment duration 3 mo), hypomagnesemia (especially if treatment duration 3 mo)

GI: abdominal pain, CLOSTRIDIOIDES DIFFICILE-ASSOCIATED DIARRHEA (CDAD), constipation, diarrhea, dry mouth, flatulence, fundic gland polyps, nausea

GU: acute tubulointerstitial nephritis

Hemat: vitamin B12 deficiency

MS: bone fracture

Neuro: headache

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS, ANGIOEDEMA, OR TUBULOINTERSTITIAL NEPHRITIS), systemic lupus erythematosus

Interactions

Drug-drug:

Drug-Natural Products:

Route/Dosage

Gastroesophageal Reflux Disease

Hepatic Impairment

Reduction of Risk of Rebleeding of Gastric or Duodenal Ulcers After Therapeutic Endoscopy

Hepatic Impairment

H. pylori Eradication to Reduce the Risk of Duodenal Ulcer Recurrence (Triple Therapy)

Hepatic Impairment

Reduction in Risk of Gastric Ulcer During Continuous NSAID Therapy

Hepatic Impairment

Pathological Hypersecretory Conditions Including Zollinger-Ellison Syndrome

Hepatic Impairment

Availability

(Generic available)

Assessment

Lab Test Considerations:

Implementation

IV Administration:

Patient/Family Teaching

Evaluation/Desired Outcomes

US Brand Names

NexIUM, NexIUM 24hr

Pill Image

esomperazole_195-8767.jpg

Code

NDC Code