Sergel is indicated for the following:

Relief of chronic heartburn symptoms and other symptoms associated with GERD.

Healing of erosive esophagitis.

Maintenance of healing of erosive esophagitis.

Combination therapy with amoxicillin and clarithromycin for the eradication of Helicobacter pylori infection in patients with duodenal ulcer disease.

Zollinger-Ellison Syndrome.

Acid-related dyspepsia.

Duodenal and gastric ulcers.

Esomeprazole is a proton pump inhibitor (PPI) that suppresses gastric acid secretion by specifically inhibiting the H+/K+-ATPase enzyme in the gastric parietal cells. Esomeprazole, the S-isomer of omeprazole, is the first single optical isomer of PPIs and provides better acid control than racemic PPIs.

Absorption: Esomeprazole capsules contain an enteric-coated formulation of esomeprazole magnesium. After oral administration, peak plasma levels (Cmax) occur approximately 1.5 hours (Tmax). Cmax increases proportionally with dose, with a three-fold increase in the AUC from 20 mg to 40 mg. Repeated daily dosing achieves systemic bioavailability of ~90%, compared to 64% after a single dose. Food decreases AUC by 33-53%. Esomeprazole should be taken at least one hour before meals.

Distribution: Esomeprazole is 97% bound to plasma proteins. The volume of distribution at steady state is approximately 16 L in healthy individuals.

Metabolism: Metabolized extensively in the liver by CYP2C19 and CYP3A4 enzymes. Metabolites lack anti-secretory activity.

Excretion: The plasma elimination half-life is 1–1.5 hours. Less than 1% is excreted unchanged in urine, with ~80% excreted as inactive metabolites in urine and the rest in feces.

Combination Therapy with Antimicrobials:

Esomeprazole magnesium 40 mg once daily, combined with clarithromycin (500 mg twice daily) and amoxicillin (1000 mg twice daily) for 7 days, increases the AUC and Cmax of esomeprazole by 70% and 18%, respectively.

Oral Dosage Form:

Healing of Erosive Esophagitis: 20 mg or 40 mg once daily for 4–8 weeks. If not healed, an additional 4–8 weeks may be considered.

Maintenance of Healing of Erosive Esophagitis: 20 mg once daily (up to 6 months).

Symptomatic GERD: 20 mg once daily for 4 weeks. If symptoms persist, consider another 4 weeks of treatment.

H. pylori Eradication (Triple Therapy):

Esomeprazole 40 mg once daily for 10 days.

Amoxicillin 1000 mg twice daily for 10 days.

Clarithromycin 500 mg twice daily for 10 days.

Zollinger-Ellison Syndrome: 20–80 mg once daily, adjusted individually.

Acid-Related Dyspepsia: 20–40 mg once daily for 2–4 weeks.

Duodenal Ulcer: 20 mg once daily for 2–4 weeks.

Gastric Ulcer: 20–40 mg once daily for 4–8 weeks.

IV Injection or Infusion:

GERD with Erosive Esophagitis:

Adults (≥18 years): 20 mg or 40 mg once daily (IV injection over 3 minutes or infusion over 10–30 minutes).

Pediatric Patients (1 month to 17 years):

Weight <55 kg: 10 mg once daily.

Weight ≥55 kg: 20 mg once daily.

1 month to <1 year: 0.5 mg/kg once daily (infusion over 10–30 minutes).

Risk Reduction of Rebleeding after Gastric/Duodenal Ulcer:

80 mg as a 30-minute infusion, followed by a continuous infusion of 8 mg/h for 72 hours.

Tablet/Capsule: Swallow whole one hour before meals.

Oral Suspension: Mix the contents in 15 ml of water, stir, and allow to thicken for 2–3 minutes. Consume immediately.

IV Injection: Reconstitute with 5 ml of 0.9% sodium chloride and administer over 3 minutes. Use the solution within 12 hours.

Sergel is metabolized by CYP2C19 and CYP3A4, with no significant interactions with CYP enzymes like 1A2, 2A6, 2C9, 2D6, 2E1, and 3A4.

Drug Absorption: May interfere with drugs dependent on gastric pH for absorption (e.g., ketoconazole, iron salts, and digoxin).

Combination Therapy: Increases plasma levels of Sergel and 14-hydroxyclarithromycin.

Sergel is contraindicated in patients with hypersensitivity to esomeprazole or its formulation components.

Common side effects include:

Headache

Diarrhea

Nausea

Flatulence

Abdominal pain

Constipation

Dry mouth

Pregnancy: No adequate studies in pregnant women. Use only if necessary.

Lactation: Breastfeeding should be discontinued if esomeprazole is essential.

Pediatric Use: Safety and effectiveness in pediatric patients are not fully established.

Geriatric Use: No significant differences between elderly and younger patients.

Hepatic Impairment: Adjust dosage for severe hepatic insufficiency (do not exceed 20 mg/day).

Renal Impairment: No dosage adjustment required as less than 1% is excreted unchanged in urine.

Symptoms include reduced motor activity, respiratory changes, tremor, ataxia, and convulsions. Treat symptomatically and supportively. Esomeprazole is not removed by dialysis.