APO-ESOMEPRAZOLE

What it is

APO-ESOMEPRAZOLE contains esomeprazole as magnesium dihydrate in enteric-coated tablets. The medicine is available in two strengths: 20 mg and 40 mg tablets. The 20 mg tablets are light pink, and the 40 mg tablets are pink, both elliptically shaped and biconvex. Esomeprazole reversibly reduces gastric acid secretion by specifically inhibiting the gastric enzyme H+, K+-ATPase proton pump in the parietal cell.

Approved indications —

Treatment of erosive reflux oesophagitis — Long-term management of patients with healed oesophagitis to prevent relapse — Symptomatic treatment of gastro-oesophageal reflux disease (GORD) — Short-term treatment of upper gastrointestinal symptoms associated with non-steroidal anti-inflammatory drug (NSAID) therapy (non-selective and COX-2 selective) — Healing of gastric ulcers associated with NSAID (non-selective and COX-2 selective) therapy — Prevention of gastric and duodenal ulcers associated with NSAID (non-selective and COX-2 selective) therapy in patients at risk — Prevention of rebleeding of gastric or duodenal ulcers following treatment with intravenous esomeprazole — Pathological hypersecretory conditions including Zollinger-Ellison syndrome and idiopathic hypersecretion — In combination with appropriate antibiotics for healing of duodenal ulcer associated with Helicobacter pylori — In combination with appropriate antibiotics for eradication of Helicobacter pylori in patients with active or healed peptic ulcer

Dosing overview

For adults with GORD, the usual dose is 40 mg once daily for four weeks to treat erosive reflux oesophagitis, 20 mg once daily for long-term management of healed oesophagitis, or 20 mg once daily for four weeks for symptomatic GORD in patients with normal endoscopy. For short-term treatment of upper gastrointestinal symptoms associated with NSAID therapy, the dose is 20 mg once daily. For healing gastric ulcers associated with NSAID therapy, the usual dose is 20 mg once daily for 4 to 8 weeks; for prevention of gastric and duodenal ulcers in patients at risk, the dose is 20 mg once daily. For pathological hypersecretory conditions, the recommended initial dosage is 40 mg twice daily, with individualised adjustment and continuation as long as clinically indicated. For Helicobacter pylori eradication in combination with appropriate antibiotics, the dose is 20 mg twice daily for 7 days.

Key safety warnings

When gastric ulcer is suspected or present, malignancy should be excluded, as esomeprazole treatment may alleviate symptoms and delay diagnosis. Treatment with proton pump inhibitors may lead to slightly increased risk of gastrointestinal infections such as Salmonella and Campylobacter and, in hospitalised patients, possibly also Clostridium difficile. Acute tubulointerstitial nephritis has been observed in patients taking proton pump inhibitors including esomeprazole, which may occur at any point during therapy and is generally attributed to idiopathic hypersensitivity reaction; it can progress to renal failure. Daily treatment with acid-suppressing medicines over a long period of time, longer than 3 years, may lead to malabsorption of cyanocobalamin (vitamin B-12) caused by hypo- or achlorhydria. Some published studies suggest that proton pump inhibitor therapy may be associated with an increased risk for osteoporosis-related fractures, particularly with high-dose and long-term therapy; patients should use the lowest dose and shortest duration of PPI therapy appropriate to the condition being treated. Subacute cutaneous lupus erythematosus has been reported with PPIs; if lesions occur in sun-exposed areas accompanied by arthralgia, medical help should be sought promptly and esomeprazole should be considered for stopping. Hypomagnesaemia, symptomatic and asymptomatic, has been reported rarely in PPI-treated patients, with serious adverse events including tetany, arrhythmias and seizures; in most patients, treatment required magnesium replacement and discontinuation of the PPI. Severe cutaneous adverse reactions such as erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis and drug reaction with eosinophilia and systemic symptoms, which can be life-threatening or fatal, have been reported very rarely; esomeprazole should be discontinued immediately upon signs and symptoms of severe skin reactions.

Contraindications

APO-ESOMEPRAZOLE is contraindicated in patients with known hypersensitivity to esomeprazole, substituted benzimidazoles or any other constituents of the formulation. Esomeprazole should not be administered with atazanavir. Esomeprazole is contraindicated in patients taking cilostazol.

Regulatory history

APO-ESOMEPRAZOLE 40 mg and 20 mg enteric-coated tablets were first listed on the ARTG on 9 February 2012.