NEXPRAZOLE 40MG CAPSULE (each capsule contains Esomeprasole

Indications

• Gastroesophageal reflux disease (GERD)
• Erosive esophagitis
• Peptic ulcers
• Zollinger-Ellison syndrome
• Prevention of gastric ulcers associated with NSAID use

Dosage

Children: Refer to the BNF for Children for specific paediatric dosing guidelines.

Adults: Refer to the BNF for specific adult dosing guidelines.

Mechanism of action

Esomeprazole works by specifically inhibiting the gastric proton pump, leading to a significant reduction in gastric acid production. This inhibition occurs in the parietal cells of the stomach where the drug is converted to its active form in the acidic environment, allowing for a prolonged effect on acid secretion.

Pharmacodynamics

Esomeprazole decreases gastric acidity, which aids in healing erosive esophagitis caused by acid reflux and alleviates symptoms of gastroesophageal reflux disease (GERD). The suppression of gastric acid also reduces the risk of peptic ulcers and promotes healing in those already present. The drug provides a dose-dependent reduction in gastric acid secretion, with effects lasting beyond 24 hours.

Pharmacokinetics

Esomeprazole is well absorbed from the gastrointestinal tract, with peak plasma concentrations occurring within 1 to 2 hours post-administration. It undergoes extensive hepatic metabolism, primarily via the cytochrome P450 system, with a half-life of approximately 1 to 1.5 hours. The majority of the drug is eliminated through urine as metabolites, with only a small fraction excreted unchanged. Its pharmacokinetics may be affected by factors such as age, liver function, and concurrent medications.

Contra-indications

• Hypersensitivity to esomeprazole or any component of the formulation
• Concomitant use with rilpivirine-containing products

Adverse effects

• Headache
• Diarrhea
• Nausea
• Vomiting
• Abdominal pain
• Flatulence
• Dizziness
• Fatigue
• Hypomagnesemia
• Clostridium difficile infection of the colon

Interactions

• Increased risk of nephrotoxicity with drugs that affect renal function
• May decrease the efficacy of clopidogrel due to inhibition of CYP2C19
• Increased serum levels of drugs metabolized by CYP2C19
• Potential interaction with methotrexate

Precautions

• Monitor for signs of gastrointestinal malignancy in patients with persistent symptoms
• Use caution in patients with hepatic impairment
• Long-term use may lead to vitamin B12 deficiency

Pregnancy

Esomeprazole should only be used during pregnancy if the potential benefit justifies the risk to the fetus, as data on use in pregnancy is limited.

Breast-feeding

Esomeprazole is excreted in breast milk; caution is advised when administering to nursing women.

Storage

Store at room temperature, away from moisture and heat. Keep out of reach of children.

Formulations

• Tablets: 20 mg, 40 mg
• Injectable formulation