ESOSOLE 40MG INJECTION

Indications

• Gastroesophageal reflux disease (GERD)
• Erosive esophagitis
• Peptic ulcer disease
• Zollinger-Ellison syndrome
• Prevention of NSAID-induced gastric ulcers

Dosage

Children: Refer to the BNF for Children for specific dosing recommendations.

Adults: Refer to the BNF for specific dosing recommendations.

Mechanism of action

Esomeprazole works by irreversibly inhibiting the H+/K+ ATPase enzyme system (proton pump) in the gastric parietal cells. This inhibition prevents the final step of gastric acid production, leading to reduced acidity in the stomach and duodenum.

Pharmacodynamics

The onset of action of esomeprazole typically occurs within 1 hour of administration, and its effects can last for up to 24 hours. Esomeprazole provides significant acid suppression, which aids in healing erosive esophagitis and alleviating symptoms of GERD. Long-term use may reduce the risk of gastric ulcers associated with nonsteroidal anti-inflammatory drugs (NSAIDs).

Pharmacokinetics

Esomeprazole is well absorbed after oral administration, with peak plasma concentrations occurring within 1 to 2 hours. It undergoes extensive hepatic metabolism, primarily via the cytochrome P450 system, and has a bioavailability of approximately 64%. The elimination half-life is about 1.5 hours, although the duration of acid inhibition can last much longer due to the drug's mechanism of action. The drug is primarily excreted in the urine.

Contra-indications

• Hypersensitivity to esomeprazole or any of its components
• Use in patients with a history of severe allergic reactions to proton pump inhibitors

Adverse effects

• Headache
• Nausea
• Diarrhea
• Abdominal pain
• Flatulence
• Constipation
• Dizziness
• Fatigue
• Rash
• Increased risk of Clostridium difficile infection in the colon

Interactions

• May interact with clopidogrel, reducing its effectiveness
• May affect the absorption of drugs that require an acidic environment for optimal absorption, such as ketoconazole and certain other antifungals
• Caution is advised when used with drugs metabolized by CYP2C19, as esomeprazole may inhibit this enzyme

Precautions

• Use with caution in patients with severe liver impairment
• Monitor for signs of magnesium deficiency, especially in long-term therapy
• Consider risk of bone fractures with long-term use, particularly in patients with other risk factors

Pregnancy

Esomeprazole is classified as category B in pregnancy. Limited studies in pregnant women have not demonstrated a risk to the fetus, but should only be used if clearly needed.

Breast-feeding

Esomeprazole is excreted in breast milk. Caution is recommended if used during breastfeeding.

Storage

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

Formulations

• Oral tablets
• Oral suspension
• Intravenous injection