esomeprazole magnesium (perprazole, S-omeprazole)

esomeprazole magnesium (perprazole, S-omeprazole)

(ess oh me' pray zol)

Nexium, Nexium IV

Pregnancy Category B

Drug classes

Antisecretory drug

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

·        GERD—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

·        Short-term treatment of GERD with a history of erosive-esophagitis by IV route for up to 10 days, when oral therapy is not possible.

·        As part of combination therapy for the treatment of duodenal ulcer associated with Helicobacter pylori

·        Reduction in occurrence of gastric ulcers associated with continuous NSAID use in patients at risk (> 60 yr, history of gastric ulcers) for developing gastric ulcers

Contraindications and cautions

·        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; injection—20, 40 mg/vial

Dosages

ADULTS

·        Healing of erosive esophagitis: 20–40 mg PO daily for 4–8 wk. An additional 4–8 wk course of therapy can be considered for patients who have not healed.

·        Maintenance of healing erosive esophagitis: 20 mg daily.

·        Symptomatic GERD: 20 mg daily for 4 wk. An additional 4-wk course of therapy can be considered if symptoms have not resolved.

·        Short-term treatment of GERD when oral therapy is not possible: 20–40 mg IV by injection over at least 3 min or IV infusion over 10–30 min.

·        Duodenal ulcer: 40 mg/day PO for 10 days with 1,000 mg PO bid ampicillin and 500 mg PO bid clarithromycin.

·        Reduction of risk of gastric ulcers with NSAID use: 20–40 mg/day PO for 6 mo.

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	Onset	Peak	Duration
Oral	1–2 hr	1.5 hr	17 hr

Metabolism: Hepatic; T_1/2: 1–1.5 hr

Distribution: Crosses placenta; may enter breast milk

Excretion: Bile, urine

IV facts

Preparation: Reconstitute with 5 mL of 0.9% sodium chloride injection; withdraw 5 mL of reconstituted solution. May be further diluted with 0.9% sodium chloride, lactated ringer's, or 5% dextrose to a volume of 50 mL for infusion. Do not use if particulate matter is seen in solution, or solution is discolored. May be stored at room temperature for up to 12 hr.

Injection: Inject 5 mL directly or into line of running IV over no less than 3 min.

Infusion: Infuse dilute solution (50 mL) over 10–30 min.

Incompatibilities: Do not mix with other medications; flush tubing before and after each dose with 0.9% sodium chloride, lactated ringers, 5% dextrose.

Adverse effects

·        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

·        History: Hypersensitivity to any proton pump inhibitor; hepatic dysfunction; pregnancy, lactation

·        Physical: Skin lesions; T; reflexes, affect; urinary output, abdominal examination; respiratory auscultation, LFTs

Interventions

·        WARNING: 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.

·        Administer IV for maximum of 10 days; switch to oral form as soon as possible.

·        Ensure that the patient swallows capsule whole; do not crush, or chew; patients having difficulty swallowing may open capsule and sprinkle in applesauce or disperse in tap water, orange or apple juice, or yogurt; do not crush or chew pellets.

·        Obtain baseline LFTs and monitor periodically during therapy.

·        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

·        Take the drug at least 1 hour 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 weeks, 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.

·        You may experience these side effects: 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 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.