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Drugs reference index «Esomeprazole»

Esomeprazole


Esomeprazole

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

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

Trade Names:Nexium- Powder for suspension, delayed-release 10 mg- Powder for suspension, delayed-release 20 mg- Powder for suspension, delayed-release 40 mg

Esomeprazole Sodium

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

Pharmacology

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

Pharmacokinetics

Absorption

Oral

T max is 1.5 h. Bioavailability is approximately 90% (repeated once-daily dosing) and 64% (single dose). Food decreases AUC by 43% to 53%. 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 half-life 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

Renal Function Impairment

Less than 1% of the dose is excreted unchanged in the urine. Dosage adjustment is not necessary.

Hepatic Function Impairment

AUC was 2 to 3 times higher in patients with severe hepatic function impairment.

Elderly

AUC and C max were increased by 25% and 18%, respectively. Dosage adjustment is not necessary.

Gender

AUC and C max were higher (13%) in women than men. Dosage adjustment is not necessary.

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.

Unlabeled Uses

Non-GERD dyspepsia; Barrett esophagus; stress ulcer prophylaxis (oral); stress ulcer prophylaxis (IV).

Contraindications

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

Dosage and Administration

Healing of Erosive EsophagitisAdults

PO 20 or 40 mg once 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.

Children 1 to 11 yr of age PO Weight of less than 20 kg

Administer 10 mg once daily for 8 wk.

Weight of 20 kg or more

Administer 10 or 20 mg once daily for 8 wk.

H. Pylori Eradication to Reduce Risk of Duodenal Ulcer RecurrenceAdults

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.

GERD With History of Erosive EsophagitisAdults

IV 20 or 40 mg once daily.

Maintenance of Healing of Erosive EsophagitisAdults

PO 20 mg once daily.

Pathological Hypersecretory Conditions Including Zollinger-Ellison SyndromeAdults

PO 40 mg twice daily.

Risk Reduction of NSAID-Associated Gastric UlcerAdults

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

Short-Term Treatment of GERDChildren 12 to 17 yr of age

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

Children 1 to 11 yr of age

PO 10 mg once daily for up to 8 wk.

Symptomatic GERDAdults

PO 20 mg once daily for 4 wk. If symptoms do not resolve after 4 wk, an additional 4 wk of treatment may be considered.

Hepatic Function Impairment

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

General Advice

Delayed-Release Capsules
  • Administer at least 1 h before meals.
  • 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 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.
Delayed-Release Oral Suspension
  • To administer delayed-release oral suspension, empty contents of 10, 20, or 40 mg packet into a container containing 1 Tbsp (15 mL) of water and stir. Leave 2 to 3 min to thicken, then stir and drink within 30 min. If material remains after drinking, add more water, stir, and drink immediately.
  • For patients who have an NG or gastric tube, add 15 mL of water to a catheter-tipped syringe and add contents of a 10, 20, or 40 mg packet. Immediately shake the syringe and leave 2 to 3 min to thicken. Shake the syringe and inject through the NG or gastric tube, French size 6 or larger, into the stomach within 30 min. Refill the syringe with 15 mL of water. Shake and flush any remaining contents from the NG or gastric tube into the stomach.
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.
  • For IV injection, reconstitute the freeze-dried powder with 5 mL of sodium chloride 0.9% injection. Withdraw 5 mL of reconstituted solution and administer as an IV injection over no less than 3 min.
  • For IV infusion, reconstitute 1 vial with 5 mL of sodium chloride 0.9%, Ringer's lactate, or dextrose 5% injection, and further dilute the resulting solution to 50 mL. Administer over 10 to 30 min.
  • 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

Oral

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

IV

Store vials for injection at 59° to 86°F. Administer reconstituted solution within 12 h after reconstitution. Administer IV infusion within 12 h after mixing with sodium chloride 0.9% injection or Ringer's lactate injection or 6 h after mixing with dextrose 5% injection. Protect from light. Store in carton until time of use.

Drug Interactions

Atazanavir, nelfinavir

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

Clarithromycin, voriconazole

Esomeprazole plasma concentrations may be elevated, increasing the pharmacologic effects and adverse reactions.

Clopidogrel

The antiplatelet activity of clopidogrel may be decreased. Avoid coadministration unless there is a specific indication for a proton pump inhibitor. H 2 - receptor antagonists (eg, ranitidine) may be a safer alternative.

Diazepam

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

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

Absorption of these drugs may be affected (eg, digoxin concentrations may be increased, itraconazole and ketoconazole concentrations may be decreased).

Tolterodine

Plasma concentrations may be elevated by esomeprazole, increasing the pharmacologic effects and adverse reactions. Closely monitor the patient and adjust the tolterodine dose as needed.

Warfarin

Risk of bleeding may be increased.

Laboratory Test Interactions

None well documented.

Adverse Reactions

CNS

Headache (11%); dizziness (3%); somnolence (2%); aggression, agitation, depression, hallucination (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 (3%); 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).

Lab Tests

Increased alkaline phosphate, ALT, AST, hemoglobin, creatinine, platelets, potassium, serum gastrin, sodium, thyroxine, total bilirubin, TSH, uric acid, and WBC. Decreased hemoglobin, platelets, potassium, sodium, thyroxine, and WBC.

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

Pregnancy

Category B .

Lactation

Undetermined.

Children

Oral

Safety and efficacy not established for uses other than short-term treatment of GERD. In the short-term treatment of GERD, safety and efficacy not established in children younger than 1 yr of age.

IV

Safety and efficacy not established.

Elderly

No differences in safety and efficacy have been observed between elderly and younger patients.

Hypersensitivity

May occur; angioedema and anaphylactic reaction/shock have been reported.

Atrophic gastritis

Has been reported in patients receiving long-term treatment with omeprazole, of which esomeprazole is an enantiomer.

Overdosage

Symptoms

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

Patient Information

  • IV
  • 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 patients 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.
  • 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, constipation, gas, headache).

Copyright © 2009 Wolters Kluwer Health.

  • Esomeprazole MedFacts Consumer Leaflet (Wolters Kluwer)
  • esomeprazole Oral, Intravenous Advanced Consumer (Micromedex) - Includes Dosage Information
  • Nexium Detailed Consumer Information (PDR)
  • Nexium Delayed-Release Capsules MedFacts Consumer Leaflet (Wolters Kluwer)
  • Nexium Consumer Overview
  • Nexium Prescribing Information (FDA)
  • Nexium I.V. Consumer Overview

See Also...

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