esomeprazole

BEERS REMS

PO: IV: GERD/erosive esophagitis (IV therapy should only be used if PO therapy is not possible/appropriate).
IV: Reduction in risk of rebleeding following therapeutic endoscopy for acute bleeding gastric or duodenal ulcers
PO: Hypersecretory conditions, including Zollinger-Ellison syndrome.
PO: Eradication of
Helicobacter pylori
in duodenal ulcer disease or history of duodenal ulcer disease (in combination with amoxicillin and clarithromycin).
PO: Reduction in risk of gastric ulcer during continuous NSAID therapy.

OTC

Heartburn occurring at least twice/wk.

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*)

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.

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity to esomeprazole or related drugs (benzimidazoles);
Hypersensitivity;
Concurrent use of rilpivirine.

Use Cautiously in:

Severe hepatic impairment;
Patients using high-doses for >1 yr (↑ risk of hip, wrist, or spine fractures and fundic gland polyps);
Patients using therapy for >3 yr (↑ risk of vitamin B₁₂ deficiency);
Pre-existing risk of hypocalcemia;
OB: Safety not established in pregnancy;
Lactation: Safety not established in breastfeeding;
Geri: Appears on Beers list. risk of Clostridioides difficile infection, pneumonia, GI malignancies, bone loss, and fractures in older adults. Avoid scheduled use for >8 wk in older adults unless for high-risk patients (e.g. oral corticosteroid or chronic NSAID use) or patients with erosive esophagitis, Barrett's esophagitis, pathological hypersecretory condition, or demonstrated need for maintenance therapy (e.g. failure of H2 antagonist).

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:

May significantly ↓ levels of rilpivirine; concurrent use contraindicated.
May ↓ levels of atazanavir and nelfinavir; avoid concurrent use with either of these antiretrovirals.
May ↓ absorption of drugs requiring acid pH, including ketoconazole, itraconazole, ampicillin esters, iron salts, erlotinib, and mycophenolate mofetil.
May ↑ levels of digoxin and methotrexate.
May ↑ risk of bleeding with warfarin (monitor INR and PT).
Voriconazole may ↑ levels.
May ↓ the antiplatelet effects of clopidogrel; avoid concurrent use.
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 and hypokalemia ↑ risk of digoxin toxicity.
May ↑ levels of tacrolimus and methotrexate.

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); Heartburn: 20 mg once daily for 2 wk.
PO (Children 12–17 yr): Short-term treatment of GERD: 20–40 mg once daily for up to 8 wk.
PO (Children 1–11 yr): Short-term treatment of GERD: 10 mg once daily for 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 mo–<1 yr): >7.5–12 kg: 10 mg once daily for up to 6 wk; >5–7.5 kg: 5 mg once daily for up to 6 wk; 3–5 kg: 2.5 mg once daily for up to 6 wk.
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.

Hepatic Impairment

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

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

IV (Adults ): 80 mg over 30 min, then 8 mg/hr continuous infusion for 71.5 hr.

Hepatic Impairment

IV (Adults ): Mild to moderate hepatic impairment: Do not exceed continuous infusion rate of 6 mg/hr; Severe hepatic impairment: Do not exceed continuous infusion rate of 4 mg/hr.

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.

Hepatic Impairment

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

Reduction in Risk of Gastric Ulcer During Continuous NSAID Therapy

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

Hepatic Impairment

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

Pathological Hypersecretory Conditions Including Zollinger-Ellison Syndrome

PO (Adults ): 40 mg twice daily.

Hepatic Impairment

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

Availability ⬆ ⬇

(Generic available)

Delayed-release tablets: 20 mg^OTC
Delayed-release capsules: 20 mg^{Rx, OTC}; 40 mg
Delayed-release oral suspension packets: 2.5 mg/pkt; 5 mg/pkt; 10 mg/pkt; 20 mg/pkt; 40 mg/pkt
Powder for injection: 40 mg/vial
In combination with: naproxen (generic only).

Assessment ⬆ ⬇

Assess routinely for epigastric or abdominal pain and frank or occult blood in the stool, emesis, or gastric aspirate.
Monitor bowel function. Diarrhea, abdominal cramping, fever, and bloody stools should be reported to health care professional promptly as a sign of CDAD).

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.
- May cause false positive results in diagnostic investigations for neuroendocrine tumors due to ↑ serum chromogranin A (CgA) levels secondary to drug-induced ↓ gastric acidity. Temporarily stop esomeprazole at least 14 days before assessing CgA levels and consider repeating test if initial CgA levels are high.

Implementation ⬆ ⬇

Do not confuse Nexium with Nexavar.
Antacids may be used while taking esomeprazole.
PO: Administer at least 1 hr before meals. DNC: Swallow tablets and capsules whole.
- Delayed-release capsules: For patients with difficulty swallowing, place 1 tbsp of applesauce in an empty bowl. Open capsule and 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 min.
- For delayed-release oral suspension NG or gastric tube: Add 15 mL of water to a syringe and then add contents of packet. Shake syringe, leave 2–3 min to thicken. Shake syringe and inject through NG or gastric tube within 30 min.

IV Administration:

Reconstitution: Reconstitute each vial with 5 mL of 0.9% NaCl. Do not administer solutions that are discolored or contain a precipitate. Stable at room temperature for up to 12 hr.Do not administer with other medication or solutions. Flush line with 0.9% NaCl before and after administration.
Rate: Administer over at least 3 min.
Intermittent Infusion: Diluent: Dilute reconstituted solution to a volume of 45 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.
For 80-mg loading dose, reconstitute two 40-mg vials with 5 mL of 0.9% NaCl. Diluent: Further diluted in 100 mL 0.9% NaCl.
Rate: Administer loading dose over 30 min. Follow with infusion at a rate of 8 mg/hr for 71.5 hrs.
For 80 mg dose,Reconstitution: reconstitute two 40 mg vials with 5 mL of 0.9% NaCl. Diluent: Further diluted in 100 mL 0.9% NaCl.
Rate: Follow loading dose with infusion at a rate of 8 mg/hr for 71.5 hrs.

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 before 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 heartbeat, jitteriness, jerking movements or shaking, muscle weakness, spasms of the hands and feet, cramps or muscle aches, spasm of the voice box) occur.
Caution patient to notify health care professional if fever and diarrhea occur, especially if stool contains blood, pus, or mucus. Advise patient not to treat diarrhea without consulting health care professional.
Rep: Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding.

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇

Time/Action Profile ⬆ ⬇

Contraind./Precautions ⬆ ⬇

Adv. Reactions/Side Effects ⬆ ⬇

Interactions ⬆ ⬇

Route/Dosage ⬆ ⬇

Availability ⬆ ⬇

Assessment ⬆ ⬇

Implementation ⬆ ⬇

Patient/Family Teaching ⬆ ⬇

Evaluation/Desired Outcomes ⬆ ⬇

US Brand Names ⬆ ⬇

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