NEXOLE

What it is

NEXOLE is esomeprazole magnesium, a substituted benzimidazole. Esomeprazole is a proton pump inhibitor. NEXOLE is available as enteric-coated tablets containing esomeprazole magnesium equivalent to esomeprazole 20 mg or 40 mg.

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 NSAID (non-selective and COX-2 selective) therapy. — 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 esomeprazole solution administered by intravenous infusion. — Pathological hypersecretory conditions including Zollinger-Ellison syndrome and idiopathic hypersecretion. — Healing of duodenal ulcer associated with Helicobacter pylori in combination with appropriate antibiotics. — Eradication of Helicobacter pylori in patients with active or healed peptic ulcer in combination with appropriate antibiotics.

Dosing overview

NEXOLE tablets should be swallowed whole with liquid and should not be chewed or crushed. If required, tablets can be dispersed in half a glass of non-carbonated water only; stir until disintegrated and drink immediately or within 30 minutes.

Key safety warnings

The presence of any alarm symptom such as significant unintentional weight loss, recurrent vomiting, dysphagia, haematemesis or melaena, and when gastric ulcer is suspected or present, should prompt exclusion of malignancy, as treatment with esomeprazole may alleviate symptoms and delay diagnosis. Decreased gastric acidity due to proton pump inhibitors increases gastric counts of bacteria normally present in the gastrointestinal tract and may lead to slightly increased risk of gastrointestinal infections such as Salmonella and Campylobacter and possibly Clostridium difficile in hospitalised patients. Esomeprazole reduces exposure to the active metabolite of clopidogrel by an average of 40% and decreases maximum inhibition of platelet aggregation by an average of 14%; concomitant use of esomeprazole and clopidogrel should be avoided. Acute tubulointerstitial nephritis has been observed in patients taking proton pump inhibitors including esomeprazole, may occur at any point during therapy and is generally attributed to idiopathic hypersensitivity reaction; acute tubulointerstitial nephritis can progress to renal failure and esomeprazole should be discontinued if it develops. Daily treatment with acid-suppressing medicines over a long period of time, for example 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; the risk is increased in patients who received high-dose, defined as multiple daily doses, and long-term PPI therapy of a year or longer, and patients should use the lowest dose and shortest duration of PPI therapy appropriate to the condition being treated. Subacute cutaneous lupus erythematosus (SCLE) has been reported with the use of PPIs; if lesions occur, especially in sun-exposed areas of the skin and if accompanied by arthralgia, the patient should seek medical help promptly and the health care professional should consider stopping NEXOLE. Hypomagnesaemia, symptomatic and asymptomatic, has been reported rarely in patients treated with PPIs; serious adverse events include tetany, arrhythmias and seizures, and 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 with esomeprazole; patients should be advised of the signs and symptoms and should seek medical advice immediately when observing any indicative signs or symptoms, and esomeprazole should be discontinued immediately.

Contraindications

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

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