ESOMEPRAZOLE MAGNESIUM
| ESOMEPRAZOLE MAGNESIUM (e-so-me'pra-zole) Nexium Classifications: proton pump inhibitor; Therapeutic: antiulcer; proton pump inhibitor Prototype: Omeprazole Pregnancy Category: B |
Availability
20 mg, 40 mg capsules; 20 mg, 40 mg powder for injection
Action
Isomer of omeprazole. A weak base that is converted to the active form in the highly acidic environment of the gastric parietal cells. Inhibits the enzyme H+K+-ATPase (the acid pump), thus suppressing gastric acid secretion.
Therapeutic Effect
Due to inhibition of the H+K+-ATPase, esomeprazole substantially decreases both basal and stimulated acid secretion through inhibition of the acid pump in parietal cells.
Uses
Erosive esophagitis, gastrointestinal reflux disease (GERD), duodenal ulcer associated with H. pylori in combination with antibiotics.
Contraindications
Hypersensitivity to esomeprazole magnesium, omeprazole, or other proton pump inhibitors; gastric malignancy; lactation.
Cautious Use
Severe renal insufficiency; severe hepatic impairment; treatment for more than a year; gastric ulcers; pregnancy (category B). Safety and efficacy in children are not established.
Route & Dosage
| Healing of Erosive Esophagitis Adult: PO/IV 20–40 mg q.d. at least 1 h before meals times 4–8 wk GERD, Erosive Esophagitis Maintenance Adult: PO 20 mg q.d. Duodenal Ulcer Adult: PO 40 mg q.d. times 10 d Hepatic Impairment Child-Pugh Class C: Do not exceed 20 mg/d |
Administration
Oral- Give at least 1 h before eating.
- Do not crush or chew capsule. Must be swallowed whole.
- Open capsule and mix pellets with applesauce (cold or room temperature) if patient cannot swallow capsules. Do NOT crush pellets. Applesauce should be swallowed immediately after mixing without chewing.
- May take with antacids.
- Store in the original blister package 15°–30° C (59°–86° F).
| Intravenous PREPARE: Direct: Reconstitute powder with 5 mL of NS. IV Infusion: Further dilute reconstituted solution in 50 mL of NS, LR, or D5W. ADMINISTER: Direct: Withdraw 5 mL of reconstituted solution and give over no less than 3 min. IV Infusion: Give IV solution over 10–30 min. INCOMPATIBILITIES Do not give simultaneously with any other medication through the same IV site or line. Flush IV line with NS, LR, or D5W before/after infusion. |
- Store reconstituted solution at room temperature up to 30° C (86° F); give within 12 h of reconstitution with NS or LR and within 6 h of reconstitution with D5W.
Adverse Effects (≥1%)
CNS: Headache. GI: Nausea, vomiting, diarrhea, constipation, abdominal pain, flatulence, dry mouth.Interactions
Drug: May increase diazepam, phenytoin, warfarin levels. Food: Food decreases absorption by up to 35%.Pharmacokinetics
Absorption: Destroyed in acidic environment, therefore capsules are designed for delayed absorption in the small intestine. 70% reaches systemic circulation. Metabolism: In liver by CYP2C19. Elimination: Inactive metabolites excreted in both urine and feces. Half-Life: 1.5 h.Nursing Implications
Assessment & Drug Effects
- Monitor for S&S of adverse CNS effects (vertigo, agitation, depression) especially in severely ill patients.
- Monitor phenytoin levels with concurrent use.
- Monitor INR/PT with concurrent warfarin use.
- Lab tests: Periodic liver function tests, CBC, Hct & Hbg, urinalysis for hematuria and proteinuria.
Patient & Family Education
- Report any changes in urinary elimination such as pain or discomfort associated with urination to physician.
- Report severe diarrhea. Drug may need to be discontinued.
Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; 
Canadian drug name; 
Prototype drug