Esomeprazole

1. Introduction

Esomeprazole is a proton pump inhibitor (PPI) used to reduce stomach acid production. It is widely used to treat acid-related conditions such as gastro-oesophageal reflux disease (GERD), peptic ulcers, and Zollinger-Ellison syndrome. Esomeprazole works by irreversibly inhibiting the proton pump (H+/K+ ATPase) in gastric parietal cells, reducing acid secretion and allowing healing of the stomach lining.

2. Indications

  • Approved Indications:
    • Gastro-oesophageal reflux disease (GERD).
    • Erosive oesophagitis.
    • Peptic ulcer disease (including NSAID-associated ulcers).
    • Zollinger-Ellison syndrome.
    • Helicobacter pylori eradication (in combination therapy).
    • Prevention of gastrointestinal ulcers in high-risk NSAID users.
  • Off-Label Uses:
    • Stress ulcer prophylaxis in critically ill patients.
    • Laryngopharyngeal reflux.

3. Dosage

  • Adults:
    • GERD and Erosive Oesophagitis: 20–40 mg once daily for 4–8 weeks.
    • H. pylori Eradication: 20 mg twice daily for 7–14 days (in combination with antibiotics).
    • Zollinger-Ellison Syndrome: 40 mg twice daily, adjusted as needed (maximum: 240 mg/day).
    • NSAID-Associated Ulcers: 20–40 mg once daily for 4–8 weeks.
  • Children (≥1 year, weight ≥10 kg):
    • GERD:
      • 10–20 mg once daily (1–11 years, based on weight).
      • 20–40 mg once daily (12–17 years).
  • Elderly:
    • No dose adjustment required, but monitor for long-term PPI side effects.

4. Administration

  • Take orally at least 1 hour before meals.
  • Capsules should be swallowed whole; for those who cannot swallow, open the capsule and mix the granules with a small amount of water or apple sauce.
  • IV administration should be given over 10–30 minutes as per hospital protocol.

5. Forms Available

  • Capsules: 20 mg, 40 mg.
  • Oral suspension: 10 mg/packet.
  • Injectable solution: 20 mg/vial, 40 mg/vial.

6. Side Effects

6.1. Common Side Effects

  • Nausea.
  • Headache.
  • Diarrhoea.
  • Abdominal pain.

6.2. Less Common Side Effects

  • Flatulence.
  • Constipation.
  • Dry mouth.

6.3. Rare but Serious Side Effects

  • Hypomagnesaemia (e.g., muscle cramps, arrhythmias).
  • Bone fractures (long-term use).
  • Clostridioides difficile-associated diarrhoea (CDAD).
  • Interstitial nephritis.

7. Warnings

  • Bone Fractures: Long-term use of high-dose PPIs may increase the risk of fractures, particularly in postmenopausal women.
  • Hypomagnesaemia: Monitor magnesium levels in patients on prolonged therapy or those taking medications that cause hypomagnesaemia.
  • C. difficile Infection: May increase the risk of C. difficile-associated diarrhoea.
  • Vitamin B12 Deficiency: Long-term use can impair B12 absorption, potentially leading to deficiency.

8. Precautions

  • Use cautiously in patients with severe liver impairment; maximum dose: 20 mg/day in such cases.
  • Avoid abrupt discontinuation after long-term use, as this may lead to rebound acid hypersecretion.
  • Prolonged therapy should only be used when clearly indicated.

9. Interactions

  • Drug-Drug Interactions:
    • Clopidogrel: May reduce clopidogrel’s efficacy by inhibiting CYP2C19.
    • Warfarin: Monitor INR as esomeprazole may increase warfarin levels.
    • Antiretrovirals (e.g., atazanavir): Reduced absorption and effectiveness.
    • Methotrexate: High-dose methotrexate may accumulate due to reduced renal clearance.
  • Drug-Food Interactions:
    • No significant food interactions, but take before meals for optimal effect.

10. Monitoring Parameters

  • Symptom improvement (e.g., reduction in heartburn, healing of ulcers).
  • Magnesium levels during prolonged therapy.
  • Signs of gastrointestinal infections or CDAD.
  • Bone density in patients on long-term therapy.

11. Use in Children

  • Safe and effective for GERD in children aged ≥1 year, with doses adjusted based on weight and condition severity.

12. Use in Pregnancy

  • Category B: Generally considered safe during pregnancy; consult a doctor before use.

13. Use in Elderly

  • Safe for use in elderly patients, but monitor for potential long-term side effects such as bone fractures and vitamin deficiencies.

14. Use in Kidney Disease

  • No dose adjustment required in patients with renal impairment.

15. Use in Liver Disease

  • Use cautiously in patients with severe liver impairment; limit the dose to 20 mg/day.

16. Patient Counselling Points

  • Take esomeprazole at least 1 hour before meals for optimal acid suppression.
  • Complete the full course of therapy, even if symptoms improve early.
  • Avoid long-term use unless directed by a healthcare provider.
  • Inform your doctor if you experience severe diarrhoea, muscle cramps, or persistent fatigue.
  • Do not crush or chew the capsules; for difficulty swallowing, mix the granules with water or apple sauce as directed.

17. Table of Brand Names, Manufacturers, and Prices

Brand NameManufacturerPrice (USD)
NexiumAstraZeneca$200–250 (30 capsules, 40 mg)
EssocamCipla$100–150 (30 capsules, 40 mg)
Generic EsomeprazoleVarious$20–50 (30 capsules, 40 mg)

18. FAQs (15 Questions)

  1. What is esomeprazole used for?
    Esomeprazole is used to treat GERD, peptic ulcers, and conditions that cause excess stomach acid.
  2. How does esomeprazole work?
    It blocks the proton pump in the stomach, reducing acid production.
  3. How long does esomeprazole take to work?
    Symptom relief usually occurs within 1–4 days, but full effects may take 4–8 weeks.
  4. What are the common side effects of esomeprazole?
    Common side effects include headache, nausea, abdominal pain, and diarrhoea.
  5. Can esomeprazole be taken long-term?
    Long-term use should only be under medical supervision due to potential risks like bone fractures and vitamin deficiencies.
  6. Is esomeprazole safe in pregnancy?
    Yes, it is generally considered safe during pregnancy.
  7. Does esomeprazole interact with other medications?
    Yes, it can interact with clopidogrel, warfarin, antiretrovirals, and methotrexate.
  8. What should I do if I miss a dose of esomeprazole?
    Take it as soon as you remember, but skip it if it’s close to the next dose. Do not double the dose.
  9. Can I take esomeprazole with antacids?
    Yes, but take them at least 1 hour apart.
  10. Does esomeprazole affect magnesium levels?
    Prolonged use may lead to hypomagnesaemia; regular monitoring is advised.
  11. Can children take esomeprazole?
    Yes, it is approved for use in children ≥1 year old for GERD.
  12. Can I stop esomeprazole suddenly?
    Avoid abrupt discontinuation after long-term use to prevent rebound acid hypersecretion.
  13. Is esomeprazole safe for elderly patients?
    Yes, but monitor for side effects, particularly with long-term use.
  14. How should esomeprazole be stored?
    Store at room temperature, away from light and moisture.
  15. Can I drink alcohol while taking esomeprazole?
    Alcohol may irritate the stomach and should be avoided if you have acid-related conditions.