ESOMAC 20

Indications

• Mild to moderate dehydration
• Severe dehydration
• Diarrhea-related dehydration
• Vomiting-related dehydration
• Heat-related illnesses
• Post-operative fluid replacement

Dosage

Children: In children, the oral rehydration solution is typically administered at a rate of 75

Adults: The specific dosage for rehydration will vary based on the severity of dehydration. In mild cases, oral rehydration solutions can be administered at a rate of 50-100 mL/kg over 2-4 hours. For moderate to severe dehydration, intravenous fluids may be indicated, and specific protocols should be followed based on clinical guidelines.

Mechanism of action

Dehydration itself does not have a mechanism of action as it is a physiological state rather than a pharmacological agent. However, the treatment for dehydration typically involves the administration of fluids and electrolytes, either orally or intravenously, to restore hydration status. The rehydration process helps to restore normal blood volume and electrolyte balance, facilitating cellular functions and overall metabolic processes.

Pharmacodynamics

The pharmacodynamics of rehydration solutions involve the restoration of body fluid levels and the correction of electrolyte imbalances. Oral rehydration solutions (ORS) contain a balanced ratio of salts and sugars, which enhance the absorption of water in the intestines. This process helps to re-establish osmotic balance, improve hydration, and support physiological functions. In severe cases, intravenous fluids may be required to rapidly replenish lost fluids and electrolytes.

Pharmacokinetics

The pharmacokinetics of rehydration fluids depend on the type of fluid administered. Oral rehydration solutions are absorbed primarily in the small intestine, with the absorption rate influenced by the osmolarity and composition of the solution. Intravenous fluids are distributed directly into the bloodstream, with effects seen almost immediately. The elimination of excess fluids occurs through renal excretion, which helps maintain homeostasis.

Contra-indications

• Hypersensitivity to the active substance or any of the excipients
• Severe dehydration
• Acute kidney injury

Adverse effects

• Electrolyte imbalance
• Hypotension
• Dizziness
• Dry mouth
• Thirst
• Skin rash
• Nausea
• Vomiting

Interactions

• Caution with concomitant use of diuretics
• May interact with other medications affecting electrolyte levels
• Potential interaction with medications that affect kidney function

Precautions

• Use with caution in patients with renal impairment
• Monitor electrolyte levels during therapy
• Ensure adequate hydration during treatment

Pregnancy

Use only if clearly needed and prescribed by a healthcare professional. Risk-benefit should be considered.

Breast-feeding

Consult healthcare provider before use. Monitor infant for any adverse effects.

Storage

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

Formulations

• Oral solution
• Oral powder
• Intravenous solution

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