Esomeprazole

Esomeprazole is the first single optical isomer proton pump inhibitor (S-isomer of omeprazole) that suppresses gastric acid secretion by specific inhibition of the (H⁺/K⁺-ATPase) in gastric parietal cells, offering better acid control.

Indicated for relieving chronic heartburn and GERD symptoms, healing and maintaining healing of erosive esophagitis, H. pylori eradication in combination therapy, Zollinger-Ellison Syndrome, acid-related dyspepsia, and peptic ulcers.

Proton Pump Inhibitor

Acts as a proton pump inhibitor suppressing gastric acid secretion via specific (H⁺/K⁺-ATPase) inhibition. Administered as enteric-coated pellets reaching peak plasma levels (Cₘₐₓ) at approximately 1.5 hours.

Binds to and inhibits the (H⁺/K⁺-ATPase) pump located on the secretory surface of gastric parietal cells, thereby blocking the final step of acid production and reducing gastric acidity.

Oral: Erosive Esophagitis healing 20-40 mg once daily for 4-8 weeks; maintenance 20 mg once daily. GERD 20 mg once daily. H. pylori eradication: 40 mg once daily for 10 days. Zollinger-Ellison: 20-80 mg daily. IV injection/infusion: 10 mg to 80 mg based on condition and age.

Swallow tablets or capsules whole with water at least 1 hour before a meal. Oral suspension is mixed in 15 ml water, left to thicken for 2-3 minutes, and consumed within 30 minutes. IV injection over at least 3 minutes; IV infusion over 10-30 minutes.

Take the missed dose as soon as remembered. Skip it if it is almost time for your next scheduled dose; never double up on doses.

Frequently reported adverse events include headache, diarrhea, nausea, flatulence, abdominal pain, constipation, and dry mouth. Safety profile remains consistent during long-term treatment up to 12 months.

Symptomatic response does not preclude gastric malignancy. Long-term use may be associated with bone fractures and mineral deficiencies (e.g., magnesium). Use cautiously in severe hepatic impairment.

Contraindicated in patients with known hypersensitivity to Esomeprazole or any components of the formulation.

Metabolized by CYP2C19 and CYP3A4. Can decrease the clearance of diazepam. May interfere with the absorption of drugs where gastric pH determines bioavailability, such as ketoconazole, iron salts, and digoxin.

Should be taken on an empty stomach at least one hour before a meal to ensure optimal absorption and efficacy.

No adequate and well-controlled studies in pregnant women. Animal studies revealed no teratogenic effects. Use during pregnancy only if clearly necessary.

The excretion of esomeprazole in breast milk has not been studied. Breast-feeding should be discontinued if the use of esomeprazole is considered essential.

IV use is approved for specific pediatric age groups (1 month to 17 years) with weight-based dosing. Safety and effectiveness in pediatric oral use have not been fully established.

No overall differences in safety and efficacy have been observed between elderly and younger individuals, though greater sensitivity in some older individuals cannot be ruled out.

Mild-to-moderate hepatic impairment requires no adjustment; however, in severe hepatic impairment, a maximum dose of 20 mg daily should not be exceeded. Renal impairment requires no adjustment as excretion via urine is minimal.

Symptoms of acute toxicity include reduced motor activity, changes in respiratory frequency, tremor, ataxia, and intermittent clonic convulsions. Management should be symptomatic and supportive.

Store at a temperature not exceeding 30°C in a dry place. Protect from light and moisture. Keep out of the reach of children.

C₁₇H₁₉N₃O₃S (Molecular Formula)