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INTRODUCTION

esomeprazole (es-oh-mep-ra-zole)

Nexium

Classification

Therapeutic: antiulcer agents

Pharmacologic: proton-pump inhibitors

Indications

GERD/erosive esophagitis. Hypersecretory conditions, including Zollinger-Ellison syndrome. With amoxicillin and clarithromycin to eradicate Helicobacter pylori in duodenal ulcer disease or history of duodenal ulcer disease. Decrease risk of gastric ulcer during continuous NSAID therapy.

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.

Adverse Reactions/Side Effects

CNS: headache. GI: abdominal pain, constipation, diarrhea, dry mouth, flatulence, nausea.

PHYSICAL THERAPY IMPLICATIONS

Examination and Evaluation

  • Monitor improvements in GI symptoms (gastritis, heartburn, and so forth) to help determine if drug therapy is successful.

Interventions

  • In cases of NSAID-induced gastritis, implement appropriate manual therapy techniques, physical agents, and therapeutic exercises to reduce pain and decrease the need for aspirin and other NSAIDs.

Patient/Client-Related Instruction

  • Advise patient to avoid alcohol and foods that may cause an increase in GI irritation.

  • Instruct patient to report bothersome or prolonged side effects, including headache or GI effects (nausea, constipation, diarrhea flatulence, abdominal pain, dry mouth).

Pharmacokinetics

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

Distribution: Unknown.

Protein Binding: 97%.

Metabolism and Excretion: Extensively metabolized by the liver (cytochrome P450 [CY P450] system, primarily CYP2C19 isoenzyme); <1% excreted unchanged in urine.

Half-life: 1.0–1.5 hr.

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TIME/ACTION PROFILE (blood levels*)

ROUTE ONSET PEAK DURATION
PO rapid 1.6 hr 24 hr
IV rapid end of infusion 24 hr

*Resolution of symptoms takes 5–8 days.

Contraindications/Precautions

Contraindicated in: Hypersensitivity; OB: Lactation (not recommended).

Use Cautiously in: Severe hepatic impairment (daily dose should not exceed 20 mg); Geri: Increased risk of hip fractures in patients using high doses for >1 year; OB: Pregnancy (use only if clearly needed); Pedi: Children <1 yr (safety not established).

Interactions

Drug-Drug: May ↓ absorption of drugs requiring acid pH, including ketoconazole, itraconazole, atazanavir, ampicillin, iron salts, and digoxin. May ↑ risk of bleeding with warfarin (monitor INR and PT).

Route/Dosage

Gastroesophageal Reflux Disease

PO (Adults): Healing of erosive esophagitis—20 or 40 mg once daily for 4–8 wk; maintenance of healing of erosive esophagitis—20 mg once daily; symptomatic GERD—20 mg once daily for 4 wk (additional 4 ...

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