esomeprazole

General

Pronunciation
es-o-MEP-ra-zole [Pronunciation]

Trade Name(s)

• NexIUM

Genetic Implications

Pregnancy Category
Category B

Ther. class.
antiulcer agents

Pharm. class.
proton pump inhibitors

Indications

• PO, IV: GERD/erosive esophagitis (IV therapy should only be used if PO therapy is not possible/appropriate).

• PO: Hypersecretory conditions, including Zollinger-Ellison syndrome.

• PO: With amoxicillin and clarithromycin to eradicate Helicobacter pylori in duodenal ulcer disease or history of duodenal ulcer disease.

• PO: 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 Effect(s):

• 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 and Excretion: Extensively metabolized by the liver (cytochrome P450 [CYP450] system, primarily CYP2C19 isoenzyme, but also 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 yrs:0.42–0.88 hr; Adults:1.0–1.5 hr.

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

Contraindication/Precautions

Contraindicated in:

• Hypersensitivity;

• Lactation: Not recommended;

• Concurrent use of atazanavir or nelfinavir .

Use Cautiously in:

• Severe hepatic impairment;

• Patients using high-doses for >1 year (↑ risk of hip, wrist, or spine fractures);

• OB: Use only if clearly needed;

Adverse Reactions/Side Effects

CNS: headache.

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

F and E: hypomagnesemia (especially if treatment duration ≥3 mo).

MS: bone fracture.

*CAPITALS indicates life-threatening.
*italic indicates most frequent.

Interactions

Drug-Drug

• May ↓ levels of atazanavir and nelfinavir (avoid concurrent use with either of these antiretrovirals).

• May ↑ levels and risk of toxicity of saquinavir (may need to ↓ dose of saquinavir).

• May ↓ absorption of drugs requiring acid pH, including ketoconazole , itraconazole , atazanavir , ampicillin , and iron salts .

• May ↑ risk of bleeding with warfarin (monitor INR and PT).

• Voriconazole may ↑ levels.

• May ↓ the antiplatelet effects of clopidogrel .

• May ↑ levels of cilostazol ; consider ↓ dose of cilostazol from 100 mg twice daily to 50 mg twice daily.

• Rifampin may ↓ levels and may ↓ response (avoid concurrent use).

• Hypomagnesemia ↑ risk of digoxin toxicity.

• May ↑ levels of tacrolimus .

Drug-Natural Products
St. John's wort may ↓ levels and may ↓ response (avoid concurrent use).

Route/Dosage

Gastroesophageal Reflux Disease

• PO (Adults): Healing of erosive esophagitis—20 mg 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 wk may be considered for nonresponders)..

• PO (Children 12–17 yr): Short-term treatment of GERD—20–40 mg once daily up to 8 wk..

• PO (Children 1–11 yr): Short-term treatment of GERD—10 mg once daily up to 8 wk; Healing of erosive esophagitis—<20 kg: 10 mg once daily for 8 wk; ≥20 kg: 10–20 mg once daily for 8 wk..

• PO (Infants and Children 1–24 mo): 0.25–1 mg/kg/dose once daily.

• IV (Adults): 20 or 40 mg once daily..

• IV (Children 1–17 yr): <55 kg—10 mg once daily; ≥55 kg—20 mg once daily..

• IV (Children 1 mo-<1 yr): 0.5 mg/kg once daily..

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

• PO (Adults): 40 mg once daily for 10 days with amoxicillin 1000 mg twice daily for 10 days and clarithromycin 500 mg twice daily for 10 days..

Decrease Gastric Ulcer During Continuous NSAID Therapy

• PO (Adults): 20 or 40 mg once daily for up to 6 mo..

Pathological Hypersecretory Conditions Including Zollinger-Ellison Syndrome

• PO (Adults): 40 mg twice daily..

Hepatic Impairment

• PO, IV (Adults): Severe hepatic impairment—Dose should not exceed 20 mg/day..

Availability

• Delayed-release capsules: 20 mg, 40 mg

» Cost: 20 mg $547.96/90, 40 mg $524.97/90.

• Delayed-release oral suspension packets: 10 mg/pkt, 20 mg/pkt, 40 mg/pkt

» Cost: 10 mg $559.00/90 pkts, 20 mg $559.99/90 pkts, 40 mg $559.99/90 pkts.

• Powder for injection (requires reconstitution): 20 mg/vial, 40 mg/vial

• In combination with: naproxen (Vimovo).

Assessment

• Assess routinely for epigastric or abdominal pain and frank or occult blood in the stool, emesis, or gastric aspirate.

Lab Test Considerations

• May cause ↑ serum creatinine, uric acid, total bilirubin, alkaline phosphatase, AST, and ALT.

» May alter hemoglobin, WBC, platelets, serum sodium, potassium, and thyroxine levels.

» May cause hypomagnesemia. Monitor serum magnesium prior to and periodically during therapy.

Potential Nursing Diagnoses

• Acute pain (Indications)

Implementation

• Do not confuse Nexium with Nexavar.

• Antacids may be used while taking esomeprazole.

• PO: Administer at least 1 hr before meals. Capsules should be swallowed whole.

» Delayed-release capsules: For patients with difficulty swallowing, place 1 tbsp of applesauce in an empty bowl. Open capsule and carefully empty the pellets inside onto applesauce. Mix pellets with applesauce and swallow immediately. Applesauce should not be hot and should be soft enough to swallow without chewing. Do not store applesauce mixture for future use. Tap water, orange juice, apple juice, and yogurt have also been used. Do not crush or chew pellets.

» For patients with an NG tube, delayed-release capsules can be opened and intact granules emptied into a 60-mL syringe and mixed with 50 mL of water. Replace plunger and shake syringe vigorously for 15 sec. Hold syringe with tip up and check for granules in tip. Attach syringe to NG tube and administer solution. After administering, flush syringe with additional water. Do not administer if granules have dissolved or disintegrated. Administer immediately after mixing.

» For Delayed-release oral suspension: Mix contents of packet with 1 tbsp (15 mL) of water, leave 2–3 min to thicken, stir and drink within 30 minutes.

» For Delayed-Release Oral Suspension Nasogastric or Gastric Tube: Add 15 mL of water to a syringe and then add contents of packet. Shake the syringe, leave 2–3 min to thicken. Shake the syringe and inject through the nasogastric or gastric tube within 30 min.

IV Adminstration:

• pH:
9.0–11.0.

• Direct IV:
Reconstitute each vial with 5 mL of 0.9% NaCl, LR, or D5W. Do not administer solutions that are discolored or contain a precipitate. Stable at room temperature for up to 12 hr.

• Rate:
Administer over at least 3 min.

• Intermittent Infusion:

Diluent: Dilute reconstituted solution to a volume of 50 mL with D5W, 0.9% NaCl, or LR for adults and with 0.9% NaCl for pediatric patients.
Concentration: 0.8 mg/mL (40 mg vial) or 0.4 mg/mL (20 mg vial). Solutions diluted with 0.9% NaCl or LR are stable for 12 hr and those diluted with D5W are stable for 6 hr at room temperature.

• Rate:
Administer over 10–30 min.

• Y-Site Compatibility:

» ceftaroline

» doripenem

• Y-Site Incompatibility:

» tacrolimus

» telavancin

Do not administer with other medication or solutions. Flush line with 0.9% NaCl, LR, or D5W before and after administration.

Patient/Family Teaching

• Instruct patient to take medication as directed for the full course of therapy, even if feeling better. Take missed doses as soon as remembered but not if almost time for next dose. Do not double doses. Advise patient to read the Patient Information sheet prior to starting therapy and with each Rx refill in case of changes.

• Advise patient to avoid alcohol, products containing aspirin or NSAIDs, and foods that may cause an increase in GI irritation.

• Advise patient to report onset of black, tarry stools; diarrhea; abdominal pain; or persistent headache to health care professional promptly.

• Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications, especially St. John's wort.

• Advise patient to notify health care professional if signs of hypomagnesemia (seizures, dizziness, abnormal or fast heart beat, jitteriness, jerking movements or shaking, muscle weakness, spasms of the hands and feet, cramps or muscle aches, spasm of the voice box) occur.

• Advise female patient to notify health care professional if pregnancy is planned or suspected or if breastfeeding.

Evaluation/Desired Outcomes

• Decrease in abdominal pain or prevention of gastric irritation and bleeding. Healing of duodenal ulcers can be seen on x-ray examination or endoscopy.

• Decrease in symptoms of GERD and erosive esophagitis. Sustained resolution of symptoms usually occurs in 5–8 days. Therapy is continued for 4–8 wk after initial episode.

• Decreased incidence of gastric ulcer during continuous NSAID therapy.

• Eradication of H. Pylori in duodenal ulcer disease.

• Decrease in symptoms of hypersecretory conditions, including Zollinger-Ellison.