Esomeprazole Action, History, Best Uses, Dosage, Side effects and Top 10 Brands in Pakistan

Introduction

Esomeprazole is a widely prescribed medication that belongs to a class of drugs known as proton pump inhibitors (PPIs). This proton pump inhibitor (PPI) is used to treat gastroesophageal reflux disease (GERD), peptic ulcers, and other acid-related disorders.  These medications work by reducing the amount of acid produced in the stomach, providing relief from acid-related conditions, and promoting healing of the esophagus and stomach lining.

Chemical Composition and Mechanism of Action

Esomeprazole is the S-isomer of omeprazole, which means it is a more active form of the parent drug. It blocks the proton pump (H+/K+ ATPase) in the stomach lining, effectively reducing gastric acid secretion. This inhibition allows for the healing of acid-damaged tissues and provides symptom relief.

Efficacy of Esomeprazole

A 2006 meta-analysis concluded that esomeprazole offers a modest overall benefit in esophageal healing and symptom relief compared to other proton pump inhibitors (PPIs). This benefit was minimal for individuals with mild disease (number needed to treat: 50), but more significant for those with severe disease (number needed to treat: 8). Another meta-analysis found that it significantly increased the rate of erosive esophageal healing (>95% healing rate) when compared to standard doses in a broad patient population. Additionally, a 2017 study identified esomeprazole as one of several effective PPIs.

History and Availability

Esomeprazole was patented in 1993 and approved for medical use in 2000. It is available as a generic medication and sold over the counter in many countries. In 2021, it was the 125th most commonly prescribed medication in the United States, with over 4 million prescriptions. Lower-dose formulations of esomeprazole are available without a prescription in the United States, the United Kingdom, Australia, Canada, and New Zealand.

Medical Uses of Esomeprazole

Esomeprazole is used to treat a variety of conditions caused by excessive stomach acid. Below are some of the primary medical uses:

Gastroesophageal Reflux Disease (GERD)

GERD is a chronic condition where stomach acid frequently flows back into the esophagus, irritating. Esomeprazole helps in reducing acid production, thereby alleviating symptoms such as heartburn, regurgitation, and esophageal inflammation.

Peptic Ulcers

Peptic ulcers are sores that develop on the lining of the stomach, small intestine, or esophagus due to acid erosion. Esomeprazole aids in ulcer healing and prevention by reducing stomach acid levels.

Zollinger-Ellison Syndrome

This rare condition involves tumors in the pancreas or duodenum that cause excessive stomach acid production. Esomeprazole is effective in managing the high acid levels associated with this syndrome.

Erosive Esophagitis

Erosive esophagitis is the inflammation and damage to the esophagus caused by stomach acid. Esomeprazole promotes healing and prevents further damage by controlling acid production.

Esomeprazole uses in urdu

ایسومیپرازول ایک قسم کی دوائی ہے جو زیادہ مقدار میں پیٹ کے اسید کی وجہ سے پیدا ہونے والے مختلف حالات کا علاج کرنے میں استعمال ہوتی ہے۔ یہاں کچھ اہم استعمالات دیے گئے ہیں

گیسٹرواِیسوفیجیل ریفلکس بیماری (جی آئی آر ڈی)

جی آئی آر ڈی ایک دائمی بیماری ہے جہاں پیٹ کا اسید بار بار مری میں واپس آتا ہے، جس سے دل کا دھڑکنا، اسید کا نکالنا، اور مری کی سوزش جیسے علامات پیدا ہوتے ہیں۔ ایسومیپرازول اسید کی پیداوار کو کم کرکے ان علامات کو ختم کرتا ہے۔

پیپٹک السر

پیپٹک السر ایک بیماری ہے جس میں پیٹ، چھوٹے آنت، یا مری کی لائننگ پر سوراخ پڑ جاتے ہیں، جو اسید کی تباہی کی وجہ سے ہوتا ہے۔ ایسومیپرازول پیپٹک السر کی بھرتی اور روک تھام میں مدد فراہم کرتا ہے، اسید کی مقدار کو کم کرکے۔

زولنگر-ایلیسن سنڈروم

یہ نادر بیماری میں پینکریس یا دوڈینم میں غیر معمولی پیٹ کا اسید کی پیداوار ہوتی ہے۔ ایسومیپرازول اس سنڈروم کے ساتھ جڑے بلند اسیدی سطحوں کو کنٹرول کرنے میں مؤثر ہوتا ہے۔

ائروسویٹو اسوفیجایٹس

ایروسویٹو اسوفیجایٹس ایسوفیجس کی سوزش اور نقصان کو پیٹ کا اسید کے ذریعہ روکنے اور علاج کرنے کیلئے ایسومیپرازول کی مدد فراہم کرتا ہے۔

Benefits

Som key benefits of esomeprazole include:

Effective Acid Reduction

Esomeprazole is highly effective in reducing stomach acid and providing relief from acid reflux, heartburn, and other related symptoms.

Healing of Acid-Damaged Tissue

By reducing acid levels, this medicine aids in the healing of the esophagus, stomach, and duodenal lining, promoting recovery from conditions like GERD and peptic ulcers.

Prevention of Ulcers

It is beneficial in preventing the formation of stomach and duodenal ulcers, particularly in patients who are at risk due to long-term use of NSAIDs (non-steroidal anti-inflammatory drugs).

Symptom Management in Zollinger-Ellison Syndrome

For patients with Zollinger-Ellison Syndrome, Esomeprazole effectively manages excessive acid production, providing symptom relief and preventing complications.

Dosage Guideline

The dosage of Esomeprazole can vary based on the condition being treated, the patient’s age, and the response to treatment. Common dosages include:

For Gastroesophageal Reflux Disease (GERD) or Erosive Esophagitis

Adult Dosage (18 years and older)

• Healing erosive esophagitis: 20 mg or 40 mg once daily for 4 to 8 weeks. If necessary, the treatment may be extended for another 4 to 8 weeks.
• Maintenance of healed erosive esophagitis: 20 mg once daily.
• Treatment of symptomatic GERD: 20 mg once daily for 4 weeks.

Child Dosage (12 to 17 years)

• Healing erosive esophagitis: 20 mg or 40 mg once daily for 4 to 8 weeks.
• Symptomatic GERD: 20 mg once daily for 4 weeks.

Child Dosage (1 to 11 years)

• Symptomatic GERD: 10 mg once daily for 8 weeks.
• Erosive esophagitis:
  • Children <44 lb (20 kg): 10 mg once daily for 8 weeks.
  • Children ≥44 lb (20 kg): 10 or 20 mg once daily for 8 weeks.

Child Dosage (1 to 11 months)

• • Children 6.6–11 lb (3–5 kg): 2.5 mg once daily for up to 6 weeks.
  • Children >11–16.5 lb (>5–7.5 kg): 5 mg once daily for up to 6 weeks.
  • Children >16.5–26.5 lb (>7.5–12 kg): 10 mg once daily for up to 6 weeks.

For Stomach Ulcer

Adults: 20 or 40 mg once daily for up to 6 months.

For H. pylori Infection

Adult Dosage (18 years and older): 40 mg once daily for 10 days, in combination with amoxicillin and clarithromycin.

For Zollinger-Ellison Syndrome

Typically 40 mg twice daily, with possible doses up to 240 mg per day

Administration Guidelines

Esomeprazole is typically taken at least one hour before meals, ensuring optimal absorption. It can be taken with or without food, but consistency is key to maintaining stable blood levels of the medication.

Special Considerations

• Renal Impairment: No dosage adjustment is usually necessary.
• Hepatic Impairment: Dosage may need adjustment in severe hepatic impairment.
• Elderly Patients: No specific dosage adjustment, but caution is advised.

Pharmacokinetics of Esomeprazole

Single oral doses of 20 to 40 mg of esomeprazole typically result in peak plasma concentrations of 0.5-1.0 mg/L within 1 to 4 hours. With repeated once-daily dosing over several days, these levels may increase by approximately 50%. A 30-minute intravenous infusion of a similar dose generally produces peak plasma levels of 1-3 mg/L. The drug is rapidly cleared from the body, primarily through urinary excretion of pharmacologically inactive metabolites such as 5-hydroxymethyl esomeprazole and 5-carboxyesomeprazole. Esomeprazole and its metabolites are indistinguishable from omeprazole and its metabolites without the use of chiral analytical techniques.

Side Effects

While Esomeprazole is generally well-tolerated, some patients may experience side effects. Common side effects include:

Common Side Effects

• Headache
• Nausea
• Diarrhea
• Abdominal Pain
• Constipation
• Flatulence

Serious Side Effects

Though rare, serious side effects can occur and may require immediate medical attention:

• Severe Allergic Reactions: Rash, itching, swelling, severe dizziness, trouble breathing
• Bone Fractures: Long-term use may increase the risk of bone fractures, particularly in the hip, wrist, or spine.
• Kidney Problems: Symptoms may include changes in the amount of urine, blood in urine, or flank pain.
• Low Magnesium Levels: Symptoms include muscle spasms, irregular heartbeat, and seizures.
• Vitamin B12 Deficiency: Prolonged use can interfere with vitamin B12 absorption, leading to deficiency.

Drug Interactions

Esomeprazole can interact with various medications, potentially altering their effects or increasing the risk of side effects:

Increased Risk of Side Effects

Taking esomeprazole with these medications can heighten their side effects:

• Clopidogrel: Esomeprazole can inhibit clopidogrel’s effectiveness. Your doctor might suggest an alternative antiplatelet drug.
• Diazepam: It causes diazepam to accumulate, leading to increased side effects.
• Warfarin: Esomeprazole can enhance warfarin’s blood-thinning effects, raising the risk of severe bleeding. Your doctor may adjust your warfarin dose and monitor you closely.
• Cilostazol: This drug slows cilostazol breakdown, increasing its levels in your body. Dosage adjustments may be necessary.
• Digoxin: It elevates digoxin levels. Your doctor might check your digoxin levels and adjust the dose if needed.
• Methotrexate: Esomeprazole can increase methotrexate levels, potentially causing severe side effects such as nausea, vomiting, headache, fatigue, and liver and kidney damage. High doses of methotrexate may require temporary discontinuation of esomeprazole.
• Saquinavir: This PPI raises saquinavir levels, potentially causing side effects like fatigue, confusion, abdominal and back pain, nausea, vomiting, and liver damage. Dosage adjustments may be required.
• Tacrolimus: This medication increases tacrolimus levels, potentially causing high blood pressure and kidney damage. Monitoring and dosage adjustments might be needed.

Increased Esomeprazole Levels

Some medications can increase esomeprazole levels, raising the risk of side effects:

• Voriconazole: Can double esomeprazole levels. Dose reduction of esomeprazole might be necessary, especially in high-dose cases such as Zollinger-Ellison syndrome.
• Clarithromycin: Similar effects to voriconazole.

Reduced Effectiveness of Other Drugs

Certain medications may be less effective when taken with esomeprazole:

• Antiretrovirals (Atazanavir, Nelfinavir): Esomeprazole can reduce their absorption, making them less effective. Avoid using esomeprazole with these drugs.
• Mycophenolate Mofetil: Esomeprazole may alter stomach acid balance, reducing mycophenolate absorption. Consult your doctor about the safety of this combination.

Reduced Effectiveness of Esomeprazole

Esomeprazole may be less effective when taken with these drugs:

• St. John’s Wort: Avoid using together.
• Rifampin: Avoid using together.

Managing Drug Interactions

Patients should inform their healthcare provider of all medications and supplements they are taking to manage potential interactions effectively. Regular monitoring and dosage adjustments may be necessary.

Special Populations

Pregnancy and Breastfeeding

• Pregnancy: Esomeprazole is classified as Category C by the FDA, indicating that risk to the fetus cannot be ruled out. It should be used during pregnancy only if needed.
• Breastfeeding: Esomeprazole is excreted in breast milk, and caution is advised when administered to breastfeeding women.

Pediatric Use

Esomeprazole is approved for use in children for certain conditions, such as GERD. Dosages are adjusted based on the child’s weight and the specific condition being treated.

Elderly Patients

Elderly patients may be more susceptible to the side effects of Esomeprazole, especially bone fractures and renal issues. Careful monitoring and appropriate dosage adjustments are recommended.

Long-Term Use and Risks

Bone Health

Long-term use of Esomeprazole has been associated with an increased risk of bone fractures. Patients, especially those with osteoporosis or other risk factors, should discuss preventive measures with their healthcare provider.

Vitamin and Mineral Deficiencies

Prolonged use of Esomeprazole can interfere with the absorption of certain vitamins and minerals, such as vitamin B12 and magnesium. Regular monitoring and supplementation may be necessary.

Kidney Health

Chronic use of Esomeprazole may be linked to an increased risk of kidney problems, including acute interstitial nephritis and chronic kidney disease. Patients should be monitored for signs of renal impairment.

Alternatives to Esomeprazole

For patients who cannot tolerate Esomeprazole or do not respond adequately, several alternatives are available:

Other Proton Pump Inhibitors (PPIs)

• Omeprazole
• Lansoprazole
• Pantoprazole
• Rabeprazole

H2 Receptor Antagonists

• Ranitidine
• Famotidine
• Cimetidine
• Nizatidine

Lifestyle and Dietary Changes

• Diet Modification: Avoiding trigger foods such as spicy, fatty, and acidic foods can help manage symptoms.
• Weight Management: Maintaining a healthy weight reduces pressure on the stomach, minimizing reflux.
• Elevating the Head of the Bed: Helps prevent nighttime symptoms by keeping stomach acid from flowing back into the esophagus.
• Avoiding Late Meals: Eating several hours before bedtime can reduce nighttime reflux.

Brands in Pakistan

• Nexum is manufactured by Getz Pharma.
• Smart Healer Pharmaceuticals manufactures Esmolec.
• Arysa is Manufactured by  Helix Pharma.
• E-Zole is manufactured by Bio-Labs (Pvt) Ltd.
• Sami Pharmaceutical manufactures Novoteph.
• Hilton Pharmaceuticals manufactures Dolgina.
• Esvin is manufactured by Martin Dow Pharma.
• Axesom is manufactured by High Noon Laboratories.
• Esante is manufactured by Macter International Ltd.
• Wilson’s pharmaceutical company manufactures Gocid.

Conclusion

Esomeprazole is a highly effective medication for managing conditions related to excessive stomach acid. While it offers significant benefits in treating GERD, peptic ulcers, and other acid-related disorders, patients should be aware of potential side effects and interactions. Regular monitoring and consultation with a healthcare provider are essential to ensure safe and effective use of this drug. By understanding its uses, benefits, and risks, patients can make informed decisions about their treatment and maintain optimal digestive health.