Esomeprazole Magnesium

esomeprazole magnesium (perprazole, S-omeprazole) (ess oh me' pray zol) Nexium Pregnancy Category C Drug classes

Antisecretory agent Proton pump inhibitor Therapeutic actions

Gastric acid-pump inhibitor: suppresses gastric acid secretion by specific inhibition of the hydrogen–potassium ATPase enzyme system at the secretory surface of the gastric parietal cells; blocks the final step of acid production; is broken down less in the first pass through the liver than the parent compound omeprazole, allowing for increased serum levels. Indications

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Gastroesophageal reflux disease—treatment of heartburn and other related symptoms Erosive esophagitis—short-term (4–8 wk) treatment for healing and symptom relief; also used for maintenance therapy following healing of erosive esophagitis As part of combination therapy for the treatment of duodenal ulcer associated with Helicobacter pylori

Contraindications and cautions

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Contraindicated with hypersensitivity to omeprazole, esomeprazole, or other proton pump inhibitor. Use cautiously with hepatic dysfunction, pregnancy, lactation.

Available forms

Delayed-release capsules—20, 40 mg Dosages ADULTS

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Healing of erosive esophagitis: 20–40 mg PO daily for 4–8 wk. An additional course of therapy can be considered for patients who have not healed. Maintenance of healing erosive esophagitis: 20 mg daily. Symptomatic gastroesophageal reflux disease: 20 mg daily for 4 wk. An additional 4-wk course of therapy can be considered if symptoms have not resolved. Duodenal ulcer: 40 mg/day PO for 10 days with 1,000 mg PO bid ampicillin and 500 mg PO bid clarithromycin.

PEDIATRIC PATIENTS

Safety and efficacy not established. PATIENTS WITH HEPATIC DYSFUNCTION

Do not exceed 20 mg/day in patients with severe hepatic dysfunction. Pharmacokinetics Route Oral

Onset 1–2 hr

Peak 1.5 hr

Duration 17 hr

Metabolism: Hepatic; T1/2: 1–1.5 hr Distribution: Crosses placenta; may enter breast milk Excretion: Urine and bile Adverse effects

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CNS: Headache, dizziness, asthenia, vertigo, insomnia, apathy, anxiety, paresthesias, dream abnormalities Dermatologic: Rash, inflammation, urticaria, pruritus, alopecia, dry skin GI: Diarrhea, abdominal pain, nausea, vomiting, constipation, dry mouth, tongue atrophy, flatulence Respiratory: URI symptoms, sinusitis, cough, epistaxis

Interactions

Drug-drug • Increased serum levels and potential increase in toxicity of benzodiazepines and phenytoin when taken concurrently • May interfere with absorption of drugs dependent upon presence of acidic environment (eg ketoconazole, iron salts, digoxin) Nursing considerations CLINICAL ALERT!

Potential for name confusion exists between esomeprazole and omeprazole; use caution. Assessment

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History: Hypersensitivity to any proton pump inhibitor; hepatic dysfunction; pregnancy, lactation Physical: Skin lesions; body temperature; reflexes, affect; urinary output, abdominal exam; respiratory auscultation, liver function tests

Interventions

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Arrange for further evaluation of patient after 4 wk of therapy for gastroesophageal reflux disorders. Symptomatic improvement does not rule out gastric cancer. If administering antacids, they may be administered concomitantly with esomeprazole. Ensure that the patient swallows capsule whole; do not crush, or chew; patients having difficulty swallowing may open capsule and sprinkle in applesauce; do not crush or chew pellets. Obtain baseline liver function tests and monitor periodically during therapy.

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Maintain supportive treatment as appropriate for underlying problem. Provide additional comfort measures to alleviate discomfort from GI effects and headache. Establish safety precautions if dizziness or other CNS effects occur (use side rails, accompany patient).

Teaching points

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Take the drug at least 1 hr before meals. Swallow the capsules whole; do not chew or crush. If you cannot swallow the capsule, it can be opened and sprinkled in applesauce or mixed in tap water, orange or apple juice, or yogurt; do not crush or chew the pellets. This drug will need to be taken for 4–8 wk, at which time your condition will be reevaluated. Arrange to have regular medical follow-up while you are using this drug. Maintain all of the usual activities and restrictions that apply to your condition. If this becomes difficult, consult with your nurse or physician. These side effects may occur: Dizziness (avoid driving a car or performing hazardous tasks); headaches (consult with your health care provider if these become bothersome, medications may be available to help); nausea, vomiting, diarrhea (proper nutrition is important, consult with your dietitian to maintain nutrition; ensure ready access to bathroom facilities); symptoms of upper respiratory tract infection, cough (it may help to know that this is a drug effect, do not self-medicate, consult with your health care provider if this becomes uncomfortable). Report severe headache, worsening of symptoms, fever, chills, darkening of the skin, changes in color of urine or stool.

Adverse effects in Italic are most common; those in Bold are life-threatening.