A-Z Drug Facts > Esomeprazole

Esomeprazole

Pronouncation: (ES-oh-MEP-ra-zole)
Class: Proton pump inhibitor Esomeprazole Magnesium

Trade Names:
Nexium
- Capsules, delayed-release 20 mg
- Capsules, delayed-release 40 mg

Esomeprazole Sodium

Trade Names:
Nexium I.V.
- Injection 20 mg
- Injection 40 mg

Pharmacology

Feedback for Esomeprazole As a treatment for... Avg User Ratings [?] Heartburn 9.6 5 comments  Rate it! Erosive Esophagitis 5.0 1 comments  Rate it! Helicobacter Pylori Infection Be the first to rate it 0 comments   Showing 3 of 6 conditions - Show All... Compare with other drugs.

Suppresses gastric acid secretion by blocking proton pump within gastric parietal cells.

Pharmacokinetics

Absorption

T _max is 1.5 h. Bioavailability is approximately 90% (repeated once-daily dosing) and 64% (single dose). Food decreases AUC 43% to 53%. Take at least 1 h before meals. C _max following IV administration of 20 and 40 mg for 5 days is 3.86 and 7.51 mcmol/L, respectively.

Distribution

Esomeprazole is 97% protein bound. Vd is approximately 16 L (at steady state).

Metabolism

Metabolized in the liver by CYP2C19 and CYP3A4 to inactive metabolites.

Elimination

The t _½ is approximately 1 to 1.5 h. Less than 1% of parent drug excreted in urine; approximately 80% excreted as inactive metabolites in the urine, and the remainder is found in feces.

Special Populations

Hepatic Function Impairment

AUC was 2 to 3 times higher in patients with severe hepatic function impairment. Do not exceed a dose of 20 mg once daily in these patients.

Elderly

AUC and C _max were increased 25% and 18%, respectively.

Gender

AUC and C _max were higher (13%) in women than men.

Indications and Usage

Oral

Treatment of heartburn and other symptoms of gastroesophageal reflux disease (GERD); short-term treatment in healing and symptomatic resolution of erosive esophagitis; maintenance of symptom resolution and healing of erosive esophagitis; in combination with amoxicillin and clarithromycin for treatment of Helicobacter pylori infection and duodenal ulcer disease to eradicate H. pylori ; reduction in occurrence of gastric ulcers associated with continuous NSAID therapy in patients at risk of developing gastric ulcers; long-term treatment of pathological hypersecretory conditions, including Zollinger-Ellison syndrome.

IV

As an alternative to oral therapy when oral therapy with esomeprazole delayed-release capsules is not possible or appropriate for the short-term treatment (up to 10 days) of GERD in patients with history of erosive esophagitis.

Contraindications

Hypersensitivity to any component of the formulation or to substituted benzimidazoles.

Dosage and Administration

Symptomatic GERD
Adults

PO 20 mg once daily for 4 wk.

Healing of Erosive Esophagitis
Adults

PO 20 or 40 mg once daily for 4 to 8 wk.

Maintenance of Healing of Erosive Esophagitis
Adults

PO 20 mg once daily.

H. Pylori Eradication to Reduce Risk of Duodenal Ulcer Recurrence
Adults

PO 40 mg once daily for 10 days in combination with amoxicillin 1,000 mg twice daily and clarithromycin 500 mg twice daily for 10 days.

Risk Reduction of NSAID-Associated Gastric Ulcer
Adults

PO 20 or 40 mg once daily for up to 6 mo.

GERD With History of Erosive Esophagitis
Adults

IV 20 or 40 mg once daily.

Pathological Hypersecretory Conditions Including Zollinger-Ellison Syndrome
Adults

PO 40 mg twice daily for 4 to 8 wk. For patients who do not heal after 4 to 8 wk, consider an additional 4 to 8 wk of treatment.

Short-Term Treatment of GERD
Children 12 to 17 yr of age

PO 20 to 40 mg once daily for 8 wk.

Hepatic Function Impairment
Adults and children (GERD)

IV/PO For severe impairment (Child Pugh class C), do not exceed a dose of 20 mg.

General Advice

PO

• May be used concomitantly with antacids and sucralfate.
• Administer esomeprazole at least 30 min prior to sucralfate.
• Instruct patient to swallow capsule whole and not to chew or crush.
• For patient who has difficulty swallowing capsule, contents of the capsule (pellets) may be emptied onto 1 Tbsp of cool or cold applesauce in a bowl, gently mixed, and then swallowed immediately without chewing. Do not prepare mixture ahead of time and store for future use.
• For administration via nasogastric (NG) tube, remove plunger from 60 mL syringe and empty contents of capsule into the syringe. Add 50 mL of water, replace the plunger, and shake vigorously for 15 sec to produce a suspension. Hold syringe with tip up and check for pellets remaining in tip. Immediately attach syringe to NG tube and deliver contents through the NG tube into the stomach. Flush NG tube with additional water. Do not administer if pellets have dissolved or disintegrated. Do not prepare suspension ahead of time and store for future use.

IV

• For use when oral therapy is not possible or appropriate. Replace IV therapy with oral therapy as soon as possible.
• For IV injection or infusion only. Not for intradermal, subcutaneous, IM, or intra-arterial administration.
• Visually inspect solution before administration. Do not administer if solution is cloudy, discolored, or contains particulate matter.
• Do not add other medications or additives to IV container or infuse simultaneously through same IV line.
• Flush IV line with compatible IV fluid (sodium chloride 0.9% injection, Ringer's lactate solution, or dextrose 5% injection) before and after esomeprazole administration if same IV line is used for sequential administration of different drugs.

Storage/Stability

PO

Store capsules at 59° to 86°F. Keep container tightly closed.

IV

Store vials for injection at 59° to 86°F. Protect from light. Store in carton until time of use.

Drug Interactions

Atazanavir

Plasma concentrations may be reduced by esomeprazole, decreasing the efficacy.

Diazepam

Plasma concentrations may be increased by esomeprazole; however, the increase not likely to be clinically important.

Drugs dependent on gastric pH for bioavailability (eg, ampicillin, cyanocobalamin, digoxin, iron salts, ketoconazole)

Absorption of these drugs may be affected.

Warfarin

Risk of bleeding may be increased.

Laboratory Test Interactions

None well documented.

Adverse Reactions

CNS

Headache (11%); dizziness (2%); aggression, agitation, depression, hallucination, psychiatric disorders (postmarketing).

Dermatologic

Pruritus (1%); alopecia, erythema multiforme, hyperhidrosis, photosensitivity, Stevens-Johnson syndrome, toxic epidermal necrolysis (postmarketing).

EENT

Blurred vision (postmarketing).

GI

Flatulence (10%); abdominal pain, dyspepsia, nausea (6%); diarrhea, dry mouth (4%); constipation (2%); GI candidiasis, pancreatitis, stomatitis, taste disturbance (postmarketing).

Genitourinary

Gynecomastia, interstitial nephritis (postmarketing).

Hepatic

Hepatic encephalopathy, hepatic failure, hepatitis with or without jaundice (postmarketing).

Hematologic-Lymphatic

Agranulocytosis, pancytopenia (postmarketing).

Local

Application-site reactions including mild local erythema and pruritus with IV administration (2%).

Musculoskeletal

Muscular weakness, myalgia (postmarketing).

Respiratory

Sinusitis (2%); respiratory tract infection (1%); bronchospasm (postmarketing).

Miscellaneous

Anaphylactic reaction, shock (postmarketing).

Precautions

Monitor Response to therapy Frequently assess patient's response to treatment. Therapy review Ensure therapy is reviewed periodically to determine if therapy needs to be continued without change or if a dose change (eg, increase, decrease, discontinuation) is indicated.

Pregnancy

Category B .

Lactation

Undetermined.

Children

Safety and efficacy not established for uses other than GERD.

In the treatment of GERD, safety and efficacy not established in children younger than 12 yr of age.

Overdosage

Symptoms

Blurred vision, confusion, diaphoresis, drowsiness, dry mouth, flushing, headache, nausea, tachycardia.

Patient Information

• Advise patient or caregiver that injection is used when oral therapy is not feasible or appropriate. Advise patient or caregiver that injection will be prepared and administered by health care provider in a health care setting and that oral therapy will be started as soon as possible.

• Oral
• Instruct patient to take each dose on an empty stomach at least 1 h before eating.
• Instruct patient who also is taking sucralfate to take esomeprazole at least 30 min before the sucralfate.
• Instruct patient to swallow capsule whole and not to crush or chew.
• Advise patient that if they experience difficulty swallowing the capsule, they may open the capsule and gently mix the pellets with 1 Tbsp of cool or cold applesauce and then immediately swallow the mixture without chewing. Remind patient not to crush or chew the pellets and not to prepare the pellet/applesauce mixture ahead of time or store for future use.
• Remind patient that esomeprazole is to be taken every day and not as needed or only when symptoms are present.
• Remind patient that antacids may be taken concurrently with esomeprazole.
• Instruct patient to report any of the following to health care provider: bloody or coffee-ground–like vomit; black, tarry stools; recurrent heartburn; recurrent indigestion or abdominal pain; increased need for antacid use; bothersome adverse reactions (eg, headache, constipation, gas).

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