esomeprazole magnesium trihydrate: clinical use

Prescribing considerations

• Confirm the indication and regularly review the need for continued acid suppression.
• Investigate alarm features such as weight loss, recurrent vomiting, dysphagia, haematemesis or melaena; symptom suppression can delay malignancy diagnosis.
• Consider every component’s interactions and contraindications during H. pylori eradication therapy.
• Use caution in severe renal impairment. Severe hepatic impairment increases exposure; follow product-specific restrictions.
• Acid suppression can slightly increase gastrointestinal infection susceptibility and reduce vitamin B12 absorption.
• Consider recent or planned endoscopy because esomeprazole may mask findings.

Contraindications and cautions

• Hypersensitivity to esomeprazole, another substituted benzimidazole or a formulation excipient.
• Concomitant nelfinavir; the selected non-prescription capsule also contraindicates oral rilpivirine.
• Observe formulation-specific restrictions for hereditary fructose intolerance, glucose-galactose malabsorption, sucrase-isomaltase insufficiency, galactose intolerance or lactase deficiency where relevant sugars are present.

Monitoring

• Regularly reassess long-term treatment.
• Consider magnesium before and periodically during prolonged use, particularly with digoxin or medicines that lower magnesium, such as diuretics.
• Consider vitamin B12 status where stores are reduced, malabsorption risks exist or symptoms suggest deficiency.
• Review fracture and osteoporosis risk during prolonged treatment.
• Monitor INR with warfarin or related anticoagulants when starting or stopping esomeprazole.
• Monitor phenytoin concentrations when esomeprazole is introduced or withdrawn.
• Esomeprazole can raise chromogranin A and interfere with neuroendocrine-tumour investigations; manage testing according to product information.

Clinical pharmacology

Esomeprazole is the S-isomer of omeprazole. After activation in the acidic secretory canaliculus, it irreversibly inhibits gastric parietal-cell H+/K+-ATPase. It is metabolised mainly by CYP2C19 and CYP3A4, inhibits CYP2C19, is highly protein-bound and is excreted predominantly as inactive urinary metabolites.

Formulation and product differences

• The selected Sandoz tablet contains lactose and sucrose; it can be dispersed in still water and administered through a suitable gastric tube.
• The selected Nexium tablet contains sucrose and can be dispersed in still water without crushing the enteric-coated pellets.
• The selected Nexium Control capsule contains sucrose and Allura Red AC; it must be swallowed intact and not opened.
• Sachet granules contain glucose and sucrose, form an oral suspension in still water and can be given through a suitable nasogastric or gastric tube.

Gastro-resistant capsule

Route: Oral

Strengths: 20 mg

Gastro-resistant tablet

Route: Oral

Strengths: 20 mg, 40 mg

Oral suspension

Route: Oral

Strengths: 10 mg