Esomeprazole (Nexium) is a proton pump inhibitor. It is one of the most potent of the proton pump inhibitors and is used to suppress gastric acid secretion.

Esomeprazole (Nexium) Uses:

Oral:

• Esomeprazole magnesium and esomeprazole strontium:

  • Gastroesophageal reflux disease (Rx only):

    • Healing of erosive esophagitis:
      • Short-term treatment of 4 to 8 weeks of  erosive esophagitis
    • Maintenance of healing of erosive esophagitis:
      • Maintaining symptom resolution and healing of erosive esophagitis

  • Symptomatic gastroesophageal reflux disease:

    • Short-term  treatment of 4 to 8 weeks of symptomatic gastroesophageal reflux disease (GERD)

  • Helicobacter pylori eradication (Rx only):

    • As part of a multidrug regimen for Helicobacter pylori eradication in patients with duodenal ulcer disease (active or history of within the past 5 years)

  • Risk reduction of nonsteroidal anti-inflammatory drug-associated gastric ulcer (Rx only):

    • Prevention of gastric ulcers associated with continuous NSAID therapy in patients at risk (age ≥60 years and/or history of gastric ulcer)

  • Pathological hypersecretory conditions, including Zollinger-Ellison syndrome (Rx only):

    • Treatment (long-term) of pathological hypersecretory conditions including Zollinger-Ellison syndrome

• Esomeprazole magnesium:

  • Heartburn (OTC labeling):
    • Treatment of frequent heartburn (≥2 days per week).

IV:

• Esomeprazole sodium:

  • Gastroesophageal reflux disease (Rx only):

    • Short-term (≤10 days) treatment of gastroesophageal reflux disease (GERD) with erosive esophagitis in pediatric patients 1 month to 17 years of age and adults when oral therapy is not possible or appropriate

  • Risk reduction of ulcer rebleeding post-procedure (Rx only):

    • Decrease the risk of rebleeding post endoscopy for acute bleeding gastric or duodenal ulcers in adults

• Off Label Use of Esomeprazole in Adults:

  • Used in Barrett esophagus
  • Used in dyspepsia
  • Used in stress ulcer prophylaxis in critically ill patients
  • Used for the treatment of NSAID induced gastric ulcers

Esomeprazole (Nexium) Dose in Adults

Note:

• All dosing is expressed in terms of the esomeprazole base, regardless of the salt associated with the dosing information.
• Esomeprazole strontium 24.65 mg is equivalent to 20 mg of esomeprazole base; esomeprazole strontium 49.3 mg is equivalent to 40 mg of esomeprazole base.

Esomeprazole (Nexium) Dose in the treatment of Barrett esophagus (off-label):

• Oral: Utilize standard doses (20 or 40 mg) once in a day
• poorly controlled reflux symptoms or esophagitis may require twice in a day dosing.
• The use of 40 mg twice in a day (in combination with aspirin) also has been reported.

Esomeprazole (Nexium) Dose in the treatment of Dyspepsia (off-label):

• Oral: 40 mg once in a  day for up to 8 weeks.

Esomeprazole (Nexium) Dose in the treatment of Erosive esophagitis (healing):

• Oral: Esomeprazole magnesium, esomeprazole strontium:
• Initial:
  • 20 to 40 mg once in a day for 4 to 8 weeks;
  • if incomplete healing, may continue for an additional 4 to 8 weeks;
• maintenance:
  • 20 mg once in a day (controlled studies did not extend beyond 6 months)

Esomeprazole (Nexium) Dose in the treatment of Heartburn (OTC labeling):

• 20 mg once in a day for 14 days (maximum: 20 mg/day);
• The treatment may be repeated after 4 months if required.

Esomeprazole (Nexium) Dose in the treatment of Helicobacter pylori eradication: Oral:

• American College of Gastroenterology guidelines:

  • Clarithromycin triple regimen:

    • 20 to 40 mg two times in a day in combination with clarithromycin 500 mg two times in a day and either amoxicillin 1 g two times in a day or metronidazole 500 mg thrice in a day;
    • continue regimen for 2 weeks.
    • Note:
      • Avoid use of clarithromycin triple therapy in patients with risk factors for macrolide resistance (eg, prior macrolide exposure, local clarithromycin resistance rates ≥15 percent, eradication rates with clarithromycin-based regimens ≤85 percent ).

  • Bismuth quadruple regimen:

    • 20 mg twice in a day in combination with tetracycline 500 mg 4 times in a day, metronidazole 250 mg 4 times in a day or 500 mg 3 or 4 times in a day, and either bismuth subcitrate 120 to 300 mg 4 times in a day or bismuth subsalicylate 300 mg 4 times in a day;
    • continue regimen for 10 to 14 days.

  • Concomitant regimen:

    • 20 mg two times daily in combination with amoxicillin 1 g two times in a day, clarithromycin 500 mg two times in a day, and either metronidazole or tinidazole 500 mg two times in a day;
    • continue regimen for 10 to 14 days.

  • Sequential regimen:

    • 20 mg two times daily plus amoxicillin 1 g two times daily for 5 to 7 days;
    • then continue esomeprazole along with clarithromycin 500 mg two times in a  day, and either metronidazole or tinidazole 500 mg two times in a day for 5 to 7 days.

  • Hybrid regimen:

    • 20 mg two times in a day plus amoxicillin 1 g two times in a  day for a weak;
    • then continue esomeprazole and amoxicillin along with clarithromycin 500 mg two times in a  day, and either metronidazole or tinidazole 500 mg two times in a  day for a weak.

  • Levofloxacin triple regimen:

    • 20 mg two times in a day in combination with amoxicillin 1 g two times in a day and levofloxacin 500 mg once in a day;
    • continue regimen for 10 to 14 days.

• Manufacturer's labeling:

  • Dosing in the prescribing information may not reflect current clinical practice. Esomeprazole magnesium, esomeprazole strontium: 40 mg once in a day.

Esomeprazole (Nexium) Dose in the treatment of pathological hypersecretory conditions (Zollinger-Ellison syndrome):

• Oral: Esomeprazole magnesium, esomeprazole strontium:
  • 40 mg two times in a day;
  • adjust regimen to individual patient needs;
  • doses up to 240 mg every day have been administered.

Esomeprazole (Nexium) Dose in the Prevention of NSAID-induced gastric ulcers:

• Oral: Esomeprazole magnesium, esomeprazole strontium:
  • 20 to 40 mg once in a day for up to 6 months;
• Note:
  • 40 mg daily did not show additional benefit over 20 mg daily in clinical trials.

Esomeprazole (Nexium) Dose in the Prevention of recurrent gastric or duodenal ulcer bleeding post endoscopy:

• IV: 80 mg over 30 minutes, followed by 8 mg/hour continuous infusion for a total of 72 hours, then 40 mg orally once in a day for 27 additional days or
• may follow continuous infusion with any single daily-dose oral proton pump inhibitor (PPI) for a duration dictated by the underlying etiology.
• Note:
  • The use of intermittent PPIs was found to be comparable with the use of continuous infusion PPIs in patients with high-risk endoscopic findings and maybe preferred.

Esomeprazole (Nexium) Dose in the treatment of Symptomatic gastroesophageal reflux:

• Oral: Esomeprazole magnesium, esomeprazole strontium:
  • 20 mg once in a day  for 4 weeks; may consider an additional 4 weeks of treatment if symptoms do not resolve

Esomeprazole (Nexium) Dose in the Treatment of GERD (short-term):

• IV: 20 mg or 40 mg once in a day.
• Note:
  • Indicated only in cases where oral therapy is inappropriate or not possible; safety/efficacy ≥10 days has not been established.

Esomeprazole (Nexium) Dose in the Treatment of NSAID-induced gastric ulcers (off-label):

• Oral: Esomeprazole magnesium:
  • 20 mg once in a day for 8 weeks.

• Discontinuation of Esomeprazole (Nexium) therapy:

  • Oral: Some experts recommend a step-down approach in order to avoid worsening or rebound symptoms.
  • One recommendation is to decrease the dose by 50% over 2 weeks to 4 weeks.
  • If the patient is already on the lowest possible dose, alternate day therapy may be considered.
  • If symptoms worsen during treatment or after discontinuation, the patient should be re-evaluated.

Esomeprazole (Nexium) Dose in Childrens

Esomeprazole (Nexium) Dose in the treatment of Erosive esophagitis associated with GERD:

Oral:

• Infants:

Note: Safety and efficacy of doses >1.33 mg/kg/day has not been studied.

• • 3 to 5 kg:
    • 5 mg once in a day for up to 6 weeks
  • >5 to 7.5 kg:
    • 5 mg once in a day for up to 6 weeks
  • >7.5 kg:
    • 10 mg once in a day for up to 6 weeks

• Children 1 to 11 years:

Note: Safety and efficacy of doses >1 mg/kg/day has not been studied.

• • <20 kg:
    • 10 mg once in a day for 8 weeks
  • >20 kg:
    • 10 or 20 mg once in a day for 8 weeks

• Children ≥12 years and Adolescents:

  • 20 to 40 mg once in a day for 4 to 8 weeks

IV Esomeprazole (Nexium): Note: Indicated only in cases where oral therapy is inappropriate or not possible; safety and efficacy >10 days have not been established.

• Infants:

  • 5 mg/kg/dose once in a day

• Children and Adolescents ≤17 years:

  • <55 kg:
    • 10 mg once in a day
  • ≥55 kg:
    • 20 mg once in a day

Esomeprazole (Nexium) Dose in the treatment of symptomaticGERD:

• Fixed dosing: Oral:

  • Children 1 to 11 years:
    • 10 mg once in a day for up to 8 weeks.
    • Note: Safety and efficacy of doses >1 mg/kg/day has not been studied.
  • Children ≥12 years and Adolescents:
    • 20 mg once in a day for 4 to 8 weeks

• Weight-directed dosing: Oral:

  • Infants, Children, and Adolescents:
    • 0.7 to 3.3 mg/kg/day

Esomeprazole (Nexium) Pregnancy Risk Category: B

• There are many recommendations for treating GERD during pregnancy.
• Lifestyle modifications, followed by medication, are the first treatment for non-pregnant women.
• Based on the available data, PPIs can be used when clinically warranted (preferring an agent with more information during pregnancy).
• Esomeprazole is the s-isomer of omeprazole; refer to the omeprazole monograph for additional information.

Use of Esomeprazole while breastfeeding

• Esomeprazole, also known as omeprazole s-isomer, is the s-isomer for omeprazole. Esomeprazole can be found in breastmilk because it is omeprazole.
• According to the manufacturer of the product, when deciding whether to continue or stop breastfeeding during therapy, it should consider the risks to infant exposure, the benefits to the infant and the benefits to the mother.
• Refer to the omeprazole monograph for additional information.

Esomeprazole (Nexium) Dose in Kidney Disease:

• Oral:

  • Esomeprazole magnesium:

    • Mild-to-severe impairment:
      • No dosage adjustment required.

  • Esomeprazole strontium:

    • Mild-to-moderate impairment:
      • No dosage adjustment required.
    • Severe impairment:
      • Use is not recommended (has not been studied).
• IV:
  • Mild-to-severe impairment:
    • No dosage adjustment required.

Esomeprazole (Nexium) Dose in Liver disease:

• Oral:
  • Mild to moderate impairment (Child-Pugh class A or B):
    • No dosage adjustment required.
  • Severe impairment (Child-Pugh class C):
    • Maximum: 20 mg in a day.
• IV:

  • Treatment of GERD (short-term):

    • Mild to moderate impairment (Child-Pugh class A or B):
      • No dosage adjustment required.
    • Severe impairment (Child-Pugh class C):
      • The dose should not exceed 20 mg each day.

  • Prevention of recurrent gastric or duodenal ulcer bleeding post endoscopy:

    • Mild to moderate impairment (Child-Pugh class A or B):
      • 80 mg over 30 minutes, followed by a maximum continuous infusion of 6 mg/hour for a total of 72 hours
    • Severe impairment (Child-Pugh class C):
      • 80 mg over 30 minutes, followed by a maximum continuous infusion of 4 mg/hour for a total of 72 hour

Unless otherwise specified, percentages represent adverse reactions identified in clinical trials evaluating the oral formulation.

Common Side Effects of Esomeprazole (Nexium):

• Central nervous system:

  • Headache

Less Common Side Effects of Esomeprazole (Nexium):

• Central Nervous System:

  • Vertigo
  • Drowsiness
  • Irritability
  • Dizziness

• Dermatologic:

  • Pruritus

• Endocrine & Metabolic:

  • Altered Thyroid Hormone Levels
  • Increased Serum Potassium
  • Increased Serum Sodium
  • Increased Thyroid Stimulating Hormone Level
  • Increased Uric Acid
  • Decreased Serum Potassium
  • Decreased Serum Sodium
  • Decreased Thyroid Hormones
  • Increased Gastrin

• Gastrointestinal:

  • Flatulence
  • Diarrhea
  • Constipation
  • Abdominal Pain
  • Nausea
  • Vomiting
  • Xerostomia

• Hematologic & Oncologic:

  • Quantitative Disorders Of Platelets

• Hepatic:

  • Increased Serum Alkaline Phosphatase
  • Increased Serum Alanine Aminotransferase
  • Increased Serum Aspartate Aminotransferase

• Local:

  • Injection Site Reaction

• Renal:

  • Increased Serum Creatinine

• Respiratory:

  • Cough
  • Tachypnea

• Miscellaneous:

  • Fever

Rare Side effects of Esomeprazole (Nexium):

• Cardiovascular:

  • Esophageal Varices

• Gastrointestinal:

  • Barrett Esophagus
  • Duodenitis
  • Mucosal Discoloration
  • Esophageal Stenosis
  • Esophageal Ulcer
  • Esophagitis
  • Gastritis

• Hematologic & Oncologic:

  • Benign Polyp

• Miscellaneous:

  • Benign Nodule

Contraindications to Esomeprazole (Nexium):

• Hypersensitivity (eg anaphylaxis and bronchospasms, acute interstitial Nephritis or anaphylactic shock), to esomeprazole or other substituted benzimidazole pron pump inhibitors or any component of formulation

Canadian labeling: Additional contraindications not in US labeling

• Concurrent use with rilpivirine.

OTC labeling

• Use OTC for self-medication and do not consume if you experience difficulty swallowing or pain.
• You can vomit with blood or bloody stool;
• Heartburn that causes dizziness, lightheadedness or sweating.
• Chest pain, shoulder pain, shortness of breath, sweating or pain spreading to arms or neck, or lightheadedness.
• frequent chest pain

Warnings and precautions

• Carcinoma

  • No reports of enterochromaffin-like (ECL) cell carcinoids, dysplasia, or neoplasia have occurred.

• Clostridium difficile-associated diarrhea (CDAD), formerly Clostridium, is now Clostridioides

  • The best PPI therapy for your condition is the one that has the lowest dosage and longest duration.
  • Proton pump inhibitors (PPIs), especially when used in hospitals, may increase the risk for CDAD. Patients with persistent diarrhea should be diagnosed with CDAD if their condition does not improve.

• Cutaneous and systemic Lupus Erythematosus

  • This condition has been described as a new onset of or an exacerbation autoimmune disease. Most cases were cutaneous lupus erythematosus, but subacute CLE was more common.
  • If you notice any signs or symptoms of CLE/SLE, discontinue treatment and consult a specialist. Most patients feel better within 4 to 12 weeks.
  • Systemic lupus is less common and usually occurs in the early to middle ages.

• Fractures

  • Proton pump inhibitor (PPI), therapy may increase the incidence of osteoporosis-related fractures of bones in the hip, spine and wrist.
  • Patients receiving long-term or high-dose therapy for more than a year must be closely monitored.
  • To reduce fracture risk in patients at high risk, you should use the lowest effective dose for the shortest time.

• Polyps of the fundic gland:

  • A diagnosis of polyps can increase the likelihood of small intestinal obstruction.
  • Proton pump inhibitors (PPIs), especially if used for a long time, can increase the risk of fundic polyps.
  • It can occur without any symptoms, but may include nausea, vomiting, and abdominal pain. Ulcerated polyps may also cause GI bleeding, anemia, and/or anemia.
  • The best PPI therapy for your condition is the one that has the lowest dosage and longest duration.

• Gastrointestinal infection (eg, Salmonella, Campylobacter):

  • These infections can be exacerbated by the use of proton pump inhibitors.

• Hypomagnesemia:

  • Rarely reported, often with prolonged PPI usage of 3 or more months (most cases for more than 1 years).
  • It could be symptomatic, or not. Severe cases can cause seizures, tetany, or cardiac arrhythmias.
  • It is important to obtain serum magnesium levels before you begin long-term treatment, particularly if you are taking digoxin, diuretics or any other drugs that can cause hypomagnesemia. Also, it is important to check your blood regularly thereafter.
  • Magnesium supplementation may be used to correct hypomagnesemia. However, discontinuation of esomeprazole may prove necessary. Magnesium levels usually return to normal within a week.

• Interstitial nephritis:

  • If acute interstitial Nephritis occurs, discontinue use.
  • Patients taking PPIs have been known to experience acute interstitial nephritis. This can occur at any stage of therapy and is usually due to an idiopathic hypersensitivity reaction.

• Vitamin B deficiency:

  • Vitamin B malabsorption may occur if prolonged treatment is continued for more than two years.
  • The severity of the deficiency depends on the dose. It is more common in women than in men, and it is more prevalent in those who are younger than 30 years.

• Gastric cancer:

  • Gastric malignancy can still be present despite symptoms being relieved.

• Hepatic impairment

  • Patients suffering from severe hepatic impairment might need to reduce their dosage.

• Renal impairment

  • In renal impairment, the pharmacokinetics for esomeprazole are not expected to change.
  • For any degree of renal impairment, dosage adjustments are not required for esomeprazole potassium or magnesium.
  • The pharmacokinetics and safety of strontium in mild to moderate renal impairment may be affected.
  • However, it is not recommended that esomeprazole strontium be used in severe impairment. This has not been tested.

Esomeprazole: Drug Interaction

Note: Drug Interaction Categories:

• Risk Factor C: Monitor When Using Combination
• Risk Factor D: Consider Treatment Modification
• Risk Factor X: Avoid Concomitant Use

Monitoring parameters:

• Susceptibility testing  recommended in patients who fail H. pylori eradication regimen.
• Monitor for rebleeding in patients with peptic ulcer bleed.
• For patients expected to be on prolonged therapy or who take PPIs with medications such as digoxin or drugs that may cause hypomagnesemia (eg, diuretics), consider monitoring magnesium levels prior to initiation of treatment and periodically thereafter.

How to administer Esomeprazole (Nexium)?

Oral Esomeprazole, (Nexium),:

• Capsule:
  • Take the whole thing in your mouth and wait at least one hour before you eat. It is best to take it before breakfast.
  • You can open the capsule and mix 1 tablespoon of applesauce with it.
  • Take the mixture immediately and swallow it.
  • Granules might be more suitable for patients who have difficulty swallowing.
• Granules:
  • Mix the 2.5 mg and 5 mg packets in a container with 5mL water. The 10 mg, 20mg, and 40 mg packets can be put into a container with 15mL water. Stir the mixture for 2 to 3 minutes.
  • Mix and drink within 30 minutes.
  • Drink more water if any medicine is left after drinking.
• Tablet
  • Take it whole, don't chew or crush.
  • Take a glass of water with you before you start your morning.
• Tablet [Canadian Product]:
  • Drink the whole thing with water, or perhaps a half-a-glass of noncarbonated water.
  • Mix until the tablets are broken down. You can then drink the liquid with pellets right away or within 30 minutes.
  • Avoid crushing or chewing pellets.
  • Drink after you have finished drinking. Rinse the glass with water.

IV Esomeprazole, (Nexium).

• Before and after administration of LR, D5W, or NS, flush the line.
• Treatment for GERD
  • You can administer injections (>=3 min) or infusions intermittently (10–30 minutes).
• Endoscopy can prevent recurrent bleeding from the gastric and duodenal stomach.
  • Infuse the loading dose for 30 minutes. Then, continue the continuous infusion at 8 mg/hour for 71.5 hours. (Adjust the rate of continuous injection in patients with hepatic impairment).

Nasogastric tube

• Capsule
  • Place intact granules in a 60mL catheter-tip Syringe. Mix with 50mL water.
  • Turn the plunger upside down and shake vigorously for fifteen seconds.
  • Make sure that there are no granules in the tip of your syringe.
  • Do not give pellets that dissolve or are disintegrated.
  • Apply immediately following preparation. After administering, flush the tube with extra water.
• Granules
  • You can also give delayed-release oral suspensiongranules by gastric tube or nasogastric.
  • Use a packet containing 2.5 mg or 5 mg. First, add 5 mL water to a catheter-tipped needle, then add the packet's granules.
  • Use a packet containing 10 mg, 20mg, or 40mg. First, add 15 mL water to a catheter-tipped needle, and then add the granules from your packet.
  • Give the syringe a shake and allow it to thicken for 2 to 3 minutes.
  • In 30 minutes, shake the syringe before using it to administer the medication through a nasogastric tube or gastric tube (6 French or greater).
  • Fill the syringe again with equal amounts (5 mL or 15, mL) water. Shake and flush the tube.
• Tablet [Canadian Product]:
  • You can also give dispersed tablets by nasogastric tubes (sizes 8 to 20 French), using a disposable 25 to 60 mL syringe.
  • Use 50 mL water to disperse the tablet.
  • To flush the tube and syringe after administration, add 25-50 mL more water.
  • The dispersion volume can be reduced to 25 milliliters in larger nasogastric feeding tube sizes (e.g. size 14 French or higher).

Mechanism of action of Esomeprazole (Nexium):

A proton pump inhibitor reduces gastric acid secretion through inhibition of H+/K+-ATPase within the gastric parietal cells. Esomeprazole is the S-isomer of omeprazole.

Protein binding:

• 97 Percent

Metabolism:

• Hepatic via CYP2C19 primarily and (to a lesser extent) via 3A4 to hydroxy, desmethyl, and sulfone metabolites (all inactive)

Bioavailability: Oral:

• 64 after a single dose; 90 percent with repeat dosing

Half-life elimination:

• Infants:
  • 0.93 hours
• Children 1 to 5 years:
  • 0.42 to 0.74 hours
• Children 6 to 11 years:
  • 0.73 to 0.88 hours
• Children ≥12 years and Adolescents ≤17 years:
  • 0.82 to 1.22 hours
• Adults:
  • ~1 to 1.5 hours

Time to peak: Oral:

• Infants: Median:
  • 3 hours
• Children 1 to 5 years:
  • 1.33 to 1.44 hours
• Children 6 to 11 years:
  • 1.75 to 1.79 hours
• Children ≥12 years and Adolescents ≤17 years:
  • 1.96 to 2.04 hours
• Adults:
  • 1.5 to 2 hours

Excretion:

• Urine (80 percent , primarily as inactive metabolites; <1 percent as active drug);
• feces (20 percent )
• Clearance (with repeated dosing):
  • Children 1 to 5 years: 6 to 19.44 L/hour
  • Children 6 to 11 years: 7.84 to 9.22 L/hour
  • Children ≥12 years and Adolescents ≤17 years: 8.36 to 15.88 L/hour

International Brand Names of Esomeprazole:

• NexIUM
• PMS-Esomeprazole DR
• RAN-Esomeprazole
• SANDOZ Esomeprazole
• Aesopra
• Almiprazole
• Alton
• Axiago
• Carbum
• Ceso
• Emanera
• Emazole
• Emep
• Emess
• Emozul
• Empel
• Escadra
• Esmopump
• Esofag
• Esofax
• Esoflux
• Exozole
• Exzium
• Haxium
• Ignis
• Inexium
• Jubium-20
• Jubium-40
• Lanxium
• Maxima
• Nedox
• Neksium
• Nemeol
• Neopral
• Nepramel
• Nexazol
• Nexazole
• Nexiam
• Esoget DRT
• Esola
• Esomax
• Esomep
• Esonexa
• Esopra
• Esorest
• Esoroxen
• Esotec
• Esoxium
• Esoz-20
• Esoz-40
• Esozid
• Esural
• Exmezol
• Exocid
• Neximash
• Nexipra
• Nexird
• Nexium
• Nexium IV
• NexiumMUPS
• Nexmezol
• Nexpa
• Nexpro
• Ulcium
• Xsom
• Zoleric
• Zutura
• Nexpro-20
• Nexpro-40
• Nexum
• Pamezone
• Peprazom
• Prazia
• Proxium
• Raciper
• S-Omipin
• Solezol
• Sompraz
• Sompraz IV
• Stadnex

Esomeprazole Brand Names in Pakistan: