Esomeprazole

Esomeprazole is used to treat certain stomach and esophagus problems (such as acid reflux, ulcers). It works by decreasing the amount of acid your stomach makes. It relieves symptoms such as heartburn, difficulty swallowing, and persistent cough. This medication helps heal acid damage to the stomach and esophagus, helps prevent ulcers, and may help prevent cancer of the esophagus. Esomeprazole belongs to a class of drugs known as proton pump inhibitors (PPIs).

• Esomeprazole is available under the following different brand names: Nexium, and Nexium 24HR

Dosage Forms and Strengths

Capsule, delayed-release (as magnesium)

• 20 mg (Rx/OTC)
• 40 mg
• 24.65 mg (strontium salt) (adult only)
• 49.3 mg (strontium salt) (adult only)

Tablet delayed-release (as magnesium)

• 20 mg

Injection, powder for reconstitution

• 20 mg/vial
• 40 mg/vial

Packets for oral suspension

• 10 mg
• 20 mg
• 40 mg

Dosage Considerations – Should be Given as Follows:

GERD Without Erosive Esophagitis

Adult:

• 20 mg orally once/day for 4 weeks; consider an additional 4 weeks of treatment if symptoms do not resolve completely in the first 4 weeks

Pediatric:

Oral

• Children under 1 year: Safety and efficacy not established
• Children 1-12 years: 10-20 mg orally once/day for up to 8 weeks
• Children older than 12 years: 20-40 mg orally once/day for up to 8 weeks

Intravenous (IV)

Short-term treatment of GERD with erosive esophagitis when oral therapy is not possible or appropriate

• Children under 1 month: Safety and efficacy not established
• Children 1 month to 1 year: 0.5 mg/kg intravenously (IV) once/day
• Children 1 year and older (less than 55 kg): 10 mg IV once/day
• Children 1 year and older (55 kg and greater): 20 mg IV once/day

GERD with Erosive Esophagitis

Adult

• 20-40 mg orally once/day for 4-8 weeks
• If oral therapy is inappropriate or not possible: 20-40 mg once/day intravenously (IV) up to 10 days; switch to orally once patient able to swallow
• Maintenance: 20 mg orally once/day for up to 6 months

Pediatric

Children under 1 month: Safety and efficacy not established

Children 1 month to 1 year

• 3.5 kg: 2.5 mg orally once/day for up to 6 weeks
• Greater than 3.5-7.5 kg: 5 mg orally once/day for up to 6 weeks
• Greater than 7.5 kg: 10 mg orally once/day for up to 6 weeks

Children 1-12 years

• Less than 20 kg: 10 mg orally once/day for 8 weeks
• 20 kg or greater: 10-20 mg once/day for 8 weeks

Children over 12 years

• 20-40 mg orally once/day for 4-8 weeks
• Maintenance: 20 mg orally once/day up to 6 months

Helicobacter Pylori Eradication

• Combination therapy (with amoxicillin and clarithromycin) for eradication of H pylori in patients with duodenal ulcer
• 40 mg orally once/day for 10 days, PLUS
• Amoxicillin 1000 mg orally every 12 hours for 10 days, PLUS
• Clarithromycin 500 mg orally every 12 hours for 10 days

Risk Reduction of NSAID-Associated Gastric Ulcer

• 20-40 mg orally once/day for up to 6 months

NSAID-Induced Gastric Ulcer

• 20 mg orally once/day for 4-8 weeks

Zollinger-Ellison Syndrome

• 80 mg orally divided every 12 hours (initial); adjust regimen to efficacy; up to 240 mg orally once/day, OR
• 120 mg orally every 12 hours administered to patients

Gastric or Duodenal Ulcers Following Therapeutic Endoscopy

• Intravenous (IV) indicated for risk reduction of re-bleeding of gastric or duodenal ulcers following therapeutic endoscopy in adults
• 80 mg IV infused over 30 min, THEN continuous IV infusion of 8 mg/hour for a total treatment duration of 72 hours
• Follow IV therapy with oral acid-suppressive therapy

Frequent Heartburn

• Over-the-counter (OTC): 20 mg orally once/day for 14 days

Hepatic Impairment

Oral administration

• Mild to moderate (Child-Pugh A/B): No dosage adjustment required
• Severe (Child-Pugh C): Not to exceed 20 mg/day

GERD - Intravenous (IV)

• Mild to moderate (Child-Pugh A/B): No dosage adjustment required
• Severe (Child-Pugh C): Not to exceed 20 mg/day IV

Bleeding gastric or duodenal ulcers - Intravenous (IV)

• No dosage adjustment required with an initial 80 mg/30 min IV dose
• Adjust dose for continuous IV infusion
• Mild-to-moderate (Child-Pugh A/B): Not to exceed 6 mg/hour
• Severe (Child-Pugh C): Not to exceed 4 mg/hour

Common side effects of esomeprazole include:

• Headache
• Gas (flatulence)
• Indigestion
• Nausea
• Abdominal/stomach pain
• Diarrhea
• Dry mouth
• Dizziness
• Constipation
• Drowsiness
• Itching
• Vomiting
• Rash
• Nervousness

Less common side effects of esomeprazole include:

• Blood and lymphatic system disorders: Agranulocytosis, pancytopenia
• Blurred vision
• GI disorders: Pancreatitis, stomatitis, microscopic colitis
• Hepatobiliary disorders: Liver failure, hepatitis with or without jaundice
• Anaphylactic reaction/shock
• Gastrointestinal (GI) candidiasis
• Low blood magnesium (hypomagnesemia)
• Musculoskeletal disorders: Muscular weakness, muscle pain, bone fracture
• Nervous system disorders: Hepatic encephalopathy, taste disturbance
• Psychiatric disorders: Aggression, agitation, depression, hallucination
• Interstitial nephritis
• Breast enlargement in males
• Bronchospasm
• Skin and subcutaneous tissue disorders: Hair loss, erythema multiforme, hyperhidrosis, photosensitivity, Stevens-Johnson syndrome, toxic epidermal necrolysis (sometimes fatal)

Postmarketing side effects of esomeprazole reported include:

• Cutaneous and systemic lupus erythematosus
• Cyanocobalamin (Vitamin B-12) deficiency
• Clostridium difficile-associated diarrhea

This document does not contain all possible side effects and others may occur. Check with your physician for additional information about side effects.

If your doctor has directed you to use this medication, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider, or pharmacist first.

• Severe Interactions of esomeprazole include:
  • erlotinib
  • nelfinavir
  • rilpivirine
• Esomeprazole has serious interactions with at least 21 different drugs.
• Esomeprazole has moderate interactions with at least 64 different drugs.
• Esomeprazole has mild interactions with at least 37 different drugs.

This information does not contain all possible interactions or adverse effects. Therefore, before using this product, tell your doctor or pharmacist of all the products you use. Keep a list of all your medications with you, and share this information with your doctor and pharmacist. Check with your health care professional or doctor for additional medical advice, or if you have health questions, concerns, or for more information about this medicine.

Warnings

• This medication contains esomeprazole. Do not take Nexium, or Nexium 24HR if you are allergic to esomeprazole or any ingredients contained in this drug.
• Keep out of reach of children. In case of overdose, get medical help or contact a Poison Control Center immediately.

Contraindications

• Hypersensitivity to esomeprazole or other proton pump inhibitors (PPIs)

Effects of Drug Abuse

• No information available

Short-Term Effects

• See "What Are Side Effects Associated with Using Esomeprazole?"

Long-Term Effects

• Published observational studies suggest that PPI therapy may be associated with an increased risk for osteoporosis-related fractures of the hip, wrist, or spine; particularly with prolonged (more than 1 year), high-dose therapy
• Low blood magnesium levels (hypomagnesemia) may occur with prolonged use (i.e., greater than1 year; adverse effects may result and include tetany, arrhythmias, and seizures; in 25% of cases reviewed, magnesium supplementation alone did not improve low serum magnesium levels, and the PPI had to be discontinued; consider monitoring magnesium levels prior to initiation of PPI treatment and periodically
• Daily long-term use (e.g., longer than 3 years) may lead to malabsorption or a deficiency of cyanocobalamin
• See "What Are Side Effects Associated with Using Esomeprazole?"

Cautions

• Proton pump inhibitors (PPIs) are possibly associated with increased incidence of Clostridium difficile-associated diarrhea (CDAD); consider the diagnosis of CDAD for patients taking PPIs who have diarrhea that does not improve
• PPIs may decrease the efficacy of clopidogrel by reducing the formation of the active metabolite
• Severe hepatic impairment
• Cutaneous lupus erythematosus (CLE) and systemic lupus erythematosus (SLE) reported with PPIs; avoid using for longer than medically indicated; discontinue if signs or symptoms consistent with CLE or SLE are observed and refer patient to a specialist; most patients improve with discontinuation of PPI alone in 4-12 weeks; serological testing (e.g. ANA) may be positive and elevated serological test results may take longer to resolve than clinical manifestations
• Relief of symptoms does not eliminate the possibility of a gastric malignancy; consider additional follow-up and diagnostic testing in adult patients who have a suboptimal response or early symptomatic relapse after completing treatment with a PPI
• Breastfeeding
• Therapy increases the risk of Salmonella, Campylobacter, and other infections
• Contains enteric-coated granules (acid-labile); do not chew or crush; take 1 hour before meals
• Published observational studies suggest that PPI therapy may be associated with an increased risk for osteoporosis-related fractures of the hip, wrist, or spine; particularly with prolonged (more than 1 year), high-dose therapy
• Decreased gastric acidity increases serum chromogranin A (CgA) levels and may cause false-positive diagnostic results for neuroendocrine tumors; temporarily discontinue PPIs before assessing CgA levels
• Low blood magnesium levels (hypomagnesemia) may occur with prolonged use (i.e., greater than1 year; adverse effects may result and include tetany, arrhythmias, and seizures; in 25% of cases reviewed, magnesium supplementation alone did not improve low serum magnesium levels, and the PPI had to be discontinued; consider monitoring magnesium levels prior to initiation of PPI treatment and periodically
• Daily long-term use (e.g., longer than 3 years) may lead to malabsorption or a deficiency of cyanocobalamin
• Acute interstitial nephritis was reported in patients taking proton pump inhibitors
• May elevate and/or prolong serum concentrations of methotrexate and/or its metabolite when administered concomitantly with PPIs, possibly leading to toxicity; consider a temporary withdrawal of PPI therapy with high dose methotrexate administration

Pregnancy and Lactation

• Use oral esomeprazole during pregnancy with caution if benefits outweigh risks
• Animal studies show risk and human studies are not available or neither animal nor human studies were done
• Intravenous esomeprazole may be acceptable for use during pregnancy
• Either animal studies show no risk but human studies are not available or animal studies showed minor risks and human studies were done and showed no risk
• It is unknown whether esomeprazole is distributed into breast milk; discontinue using the drug or do not nurse