Esomeprazole
Antipeptic Ulcerant · Proton pump inhibitor
Indications
Erosive reflux oesophagitis, prevention of relapse of oesophagitis, symptomatic treatment of GERD. Zollinger-Ellison syndrome, severe peptic ulcer bleeding (following endoscopic treatment). In combination with antibiotics for the eradication of H. pylori, healing of H. pylori-associated duodenal ulcer and prevention of relapse of H. pylori-associated peptic ulcers. Treatment and prevention of NSAID-associated peptic ulceration.
Dosage
ORAL: Adults: Erosive oesophagitis: 40 mg once daily for 4-8 wk. Prevention of relapse, 20 mg once daily. GERD without oesophagitis: 20 mg once daily for 4 wk. Maintenance, 20 mg once daily as required. Zollinger-Ellison syndrome: Initially 40 mg two times daily, can be altered according to response. Usual dose: 80-160 mg daily, doses over 80 mg must be given in two divided doses. Triple therapy vs H. pylori: 20 mg twice daily with amoxicillin 1 gm twice daily and clarithromycin 500 mg twice daily for 7 days. NSAID ulceration: 20 mg once daily for 4-8 wk, Prevention, 20 mg once daily. Children: Not recommended. INJECTION: Adults: Reflux oesophagitis: 40 mg once daily given as IV inj over a period of at least 3 min or as IV inf over a period of 10-30 min. Symptomatic treatment of reflux oesophagitis: 20 mg once daily, half of the reconstituted solution be given as IV inj over a period of…
Administration
Continuous or intermittent IV infusion in NaCl 0.9%: Reconstitution: Reconstitute 40-80 mg with up to 100 mL infusion fluid; For intermittent infusion, give requisite dose over 10-30 min. For IV injection: Adults: Reconstitute powder with 5 mL NS. For IV infusion: Children: Initially reconstitute powder with 5 mL of NS, then further dilute to a final volume of 50 mL. Adults: Initially reconstitute powder with 5 mL of NS, LR, D5W, then further dilute to a final volume of 50 mL. Reconstituted solution in NS or LR should be used in 12 hours. Stability: Store vials at 25°C; excursions permitted to 15°C-30°C. Protect from light. Reconstituted solution for infusion prepared in D5W should be used in 6 hours. Refrigeration is not required following reconstitution.
Adverse Effects
Headache, GI upset, skin reaction, dry mouth. Rarely angioedema, anaphylaxis, fundic gland polyps.
Risk Factor (Pregnancy/Lactation)
Pregnancy: No evidence of risk in humans. Lactation: Contraindicated or not recommended. Precautions: Exclude malignant disease before and during treatment. Impaired renal or hepatic function, increased risk of GI infection. Monitor patients on long term therapy.
Interactions
Phenytoin, warfarin, clopidogrel, ketoconazole, itraconazole, voriconazole, protease inhibitors, diazepam, citalopram, imipramine, clomipramine, other CYP2C19 substrates, CYP3A4 inhibitors or inducers, tacrolimus, digoxin, erlotinib, methotrexate.
Advice to Patient
Take at least 1 hour before meals. Do not crush or chew, swallow whole. If there is difficulty in swallowing, open the capsule and mix all contents in a tablespoon of applesauce. Swallow immediately without chewing. Contact prescriber if there is constant headache, diarrhoea, constipation, stomach pain, changes in urination or pain on urination, chest pain or palpitations, alteration in respiratory status, CNS changes, constant muscular aches or pain, ringing in ears or visual changes.
Pharmacokinetics
Metabolism: Hepatic. Bioavailability: Oral: 64% after a single dose, 90% with repeat dosing. Half-life elimination: Infants: 0.93 hrs. Children: 1-5 yrs: 0.42-0.74 hrs. 6-11 yrs: 0.73-0.88 hrs. 12-17 yrs: 0.82-1.22 hrs. Adults: Approx. 1-1.5 hrs. Time to peak: Oral: Infants: Median: 3 hrs. Children: 1-5 yrs: 1.33-1.44 hrs. 6-11 yrs: 1.75-1.79 hrs. 12-17 yrs: 1.96-2.04 hrs. Adults: 1.5-2 hrs. Excretion: Urine (80%), faeces (20%).
Brands with this active ingredient
Compiled by Healify Pharmacy from published drug references. How we compile it →
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