Description
Generic Medicine Info
Indications and Dosage Intravenous Adult: 20 mg once daily via slow inj over at least 3 minutes or infusion over 10-30 minutes. Switch to oral therapy as soon possible.
Intravenous Adult: Prophylaxis of rebleeding following therapeutic endoscopy: 80 mg via infusion over 30 minutes, may be followed by 8 mg/hour continuous infusion over 72 hours, then may switch to oral therapy given as 40 mg once daily for 4 weeks.
Intravenous Adult: Erosive reflux oesophagitis: 40 mg once daily. Symptomatic treatment of GERD: 20 mg once daily. Doses are given via slow inj over at least 3 minutes or infusion over 10-30 minutes. Switch to oral therapy as soon possible.
Oral Adult: 20 mg once daily for 4-8 weeks.
Oral Adult: 20 or 40 mg once daily for up to 6 months.
Oral Adult: Initially, 40 mg bid, may be individually adjusted according to response. Usual range: 80-160 mg daily may be increased up to 240 mg daily if necessary. Daily doses >80 mg should be given in 2 divided doses.
Oral Adult: 20 mg bid for 7 days, or 40 mg once daily for 10 days given as a triple therapy in combination with amoxicillin and clarithromycin.
Oral Adult: Erosive reflux oesophagitis: 20 or 40 mg once daily for 4 weeks, may extend for further 4 weeks if necessary. Maintenance (to prevent relapse of healed erosive oesophagitis): 20 mg once daily for up to 6 months. Symptomatic treatment of GERD (without oesophagitis): 20 mg once daily for 4 weeks; assess treatment if symptoms do not resolve after 4 weeks, may extend for further 4 weeks if necessary. |
Special Patient Group CYP2C19 is the main enzyme responsible in esomeprazole metabolism and to a lesser extent the CYP3A4 isoenzyme. CYP2C19 ultrarapid metabolisers (carriers of 2 increased function alleles e.g. *17/*17) CYP2C19 poor metabolisers (carriers of loss-of-function allele *2 e.g. *2/*2, *2/*3, *3/*3) Currently, recommendations for CYP2C19 genetic testing in esomeprazole treatment have not been provided. |
Hepatic Impairment Severe: Max: 20 mg daily. Intravenous |
Administration Delayed-Release Cap: Should be taken on an empty stomach. Take 1 hr before meals. |
Reconstitution IV inj: Reconstitute vial labelled as 20 mg or 40 mg with 5 mL 0.9% NaCl. IV infusion (10-30 minutes): Reconstitute vial with 5 mL of 0.9% NaCl, lactated Ringer’s inj or 5% dextrose in water, then further dilute to reach final volume of 50 mL. IV infusion (loading dose and continuous infusion): Reconstitute 2 vials labelled as 40 mg with 5 mL normal saline each, then further dilute the 2 vials in 100 mL normal saline. |
Contraindications Concomitant use with rilpivirine, atazanavir, and nelfinavir. |
Special Precautions Patient with gastric malignancy, reduced body stores or risk factors for reduced vitamin B12 absorption, or those at risk of fractures and osteoporosis. Severe renal and hepatic impairment. Children. Pregnancy and lactation. CYP2C19 ultrarapid metabolisers. |
Adverse Reactions Significant: Hypomagnesaemia, osteoporosis-related fractures, fundic gland polyp, subacute cutaneous lupus erythematosus, SLE, acute interstitial nephritis, atrophic gastritis, Clostridium difficile-associated diarrhoea, gastrointestinal infections (e.g. Salmonella, Campylobacter), vitamin B12 deficiency (long-term therapy). |
IV/Parenteral/PO: C |
Patient Counseling Information This drug may cause dizziness and blurred vision, if affected, do not drive or operate machinery. |
Monitoring Parameters Monitor serum Mg levels prior to treatment initiation and periodically thereafter. Assess for signs or symptoms of rebleeding, bone fractures, and Clostridium difficile-associated diarrhoea (CDAD). |
Overdosage Symptoms: Weakness, confusion, headache, drowsiness, tachycardia, nausea, diaphoresis, flushing, dry mouth and other gastrointestinal symptoms. Management: Symptomatic and supportive treatment. |
Drug Interactions Increased risk of digoxin-induced cardiotoxic effects. May diminish the therapeutic effects of clopidogrel. Increased risk of hypomagnesaemia with diuretics. May increase serum concentrations of tacrolimus, methotrexate, cilostazol, and drugs metabolised by CYP2C19 (e.g. diazepam, citalopram, imipramine, phenytoin). May reduce absorption of ketoconazole, itraconazole, Fe salts, erlotinib. Concomitant use with warfarin may increase INR and prothrombin time. Esomeprazole serum levels may be decreased with CYP2C19 or CYP3A4 inducers (e.g. rifampicin) and increased with CYP3A4 inhibitors (e.g. voriconazole, clarithromycin). May prolong elimination half-life of cisapride. |
Food Interaction Decreased serum concentrations with St. John’s wort. |
Lab Interference May increase serum chromogranin A (CgA) levels causing false-positive result in diagnostic test for neuroendocrine tumours. |
Action Description: Esomeprazole, the S-isomer of omeprazole, is a substituted benzimidazole proton pump inhibitor (PPI) that blocks the final step in gastric acid secretion by specific inhibition of H+/K+-ATPase enzyme system present on the secretory surface of the gastric parietal cells. |
Chemical Structure
Esomeprazole Source: National Center for Biotechnology Information. PubChem Database. Esomeprazole, CID=9568614, https://pubchem.ncbi.nlm.nih.gov/compound/Esomeprazole (accessed on Jan. 22, 2020) |
Storage Store between 20-25°C. Protect from light and moisture. |
MIMS Class |
ATC Classification A02BC05 – esomeprazole ; Belongs to the class of proton pump inhibitors. Used in the treatment of peptic ulcer and gastro-oesophageal reflux disease (GERD) |