Esomeprazole

FORMULA TION
Each capsule contains:
Esomepr azole (as Magnesium Trihydrate)
Eq. to Esomeprazole ……40 mg

PHARMACOLOGY
Esomepr azole is a compound that inhibits gastric acid secretion and is indicated in the treatment of gastroesophageal reflux disease (GERD), the healing of erosive esophagitis, and H. pylori eradication to reduce the risk of duodenal ulcer recurrence. Esomepr azole belongs to a new class of antisecretory the substituted benzimidazoles, that do not exhibit anticholinergic or H2 histamine compounds, antagonistic proper ties, but that suppress gastric acid secretion by specific inhibition of the H+/K + ATPase enzyme system at the secretory surface of the gastric parietal cell. Because this enzyme system is regarded as the acid (proton) pump within the gastric mucosa, Esomepr azole has been characterized as a gastric acid- pump inhibitor, in that it blocks the final step of acid production. This effect is dose-r elated and leads to inhibition of both basal and stimulated acid secretion irrespective of the stimulus.

PHARMA COKINETICS
Absorption: At repeated once-daily dosing with 40 mg, the systemic bioavailability is approximately 90% compared to 64% after a single dose of 40 mg.

Distribution
Esomepr azole is 97% bound to plasma proteins. Plasma protein binding is constant over the concentration range of 2 to 20 1/4mol/L. The apparent volume of distribution at steady state in healthy volunteers is approximately 16 L. Metabolism: Esomepr azole is extensively metabolized in the liver by the cytochrome P450 (CYP) enzyme system. The metabolites of esomeprazole lack antisecretory activity. The major part of esomeprazole’s metabolism is dependent upon the hydroxy and desmethyl metabolites. The remaining amount is dependent on CYP 3A4 which forms the sulphonemetabolite.

Excretion
The plasma elimination half-life of esomeprazole is approximately 1 to 1.5 hours. Less than 1%of parent drug is excreted in the urine. Approximately 80% of an oral dose of esomeprazole is excreted as inactive metabolites in the urine, and the remainder is found as inactive metabolites in the feces.

INDICATIONS
For the treatment of peptic ulcer disease, and other conditions where inhibition of gastric acid secretion may be beneficial, including aspiration syndrome, Healing of Erosive Esophagitis, dyspepsia, gastro- esophageal reflux disease, Zollinger Ellison Syndrome.

DOSAGE AND ADMINISTRATION
The usual dose for adults is 1 to 2 capsules once a day.
Dyspepsia -10 mg or 20 mg daily for 2 to 4 weeks. Gas tro-oesophageal Reflux Disease -20 mg to 40 mg once daily for 4 to 12 weeks, or maximum daily dose of 40 mg given 4 to 12 weeks.
Erosive reflux oesophagitis- 40 mg once daily for 4 weeks.
Peptic ulcer disease- 20 mg once daily or 40 mg daily in severe cases. Treatment is continued for 4 weeks for duodenal and 8 weeks for gastric ulcer. A dose of 10 mg to 20 mg once daily may be given for maintenance.
Zollinger Ellison Syndrome- The recommended initial dosage is Esomeprazole 40 mg twice daily. The dosage should then be individually adjusted and treatment continues as long as clinically indicated. Based on the clinical data available, the majority of patients can be controlled on doses between 80 and 160 mg esomeprazole daily. With doses above 80 mg daily, the dose should be divided and given twice-daily.
NSAID -Associated Ulceration -20 mg daily. Or as prescribed by the physician.

WARNING AND PRECAUTIONS
Patients know that antacids may be used while taking Esomeprazole, Esomeprazole can interfere with antiretroviral drugs and drugs that are affected by gastric pH changes

Pregnancy
Esomeprazole is not recommended in pregnancy.

ADVERSE EFFECT
Esomeprazole, like other PPIs, is well-tolerated. The most common side effects are diarrhea, nausea, vomiting, headaches, rash and dizziness. Nervousness, abnormal heartbeat, muscle pain, weakness, leg cramps and water retention occur infrequently.

DRUG INTERA CTIONS
Esomeprazole potentially can increase the concentration in blood of diazepam by decreasing the elimination of diazepam in the liver. Esomeprazole may have fewer drug interactions than omeprazole. The absorption of certain drugs may be affected by stomach acidity. Therefore, esomeprazole and other PPIs that reduce stomach acid also reduce the absorption and concentration in blood of ketoconazole and increase the absorption and concentration in blood of digoxin. This ma y lead to r educed effectiveness of ketoconazole or increased digoxin toxicity, respectively. Through unknown mechanisms, esomeprazole may increase blood levels of saquinavir and reduce blood levels of nelfinavir and atazanavir, Therefore, nelfinavir or atazanavir should not be administered with esomeprazole, and physicians should consider reducing the dose of saquinavir in order to avoid side effects from saquinavir.

CAUTION
Foods, Drugs, Devices, and Cosmetics Act, prohibits dispensing without prescription.

STORAGE
Store at temperatures not exceeding 300C.

Keep all medicine out of children’s reach.

AVAILABILITY
Alu / Alu blister pack (Box of 14 Capsules).

“For suspected adverse drug reaction, report to the FDA: www.fda.gov.ph”.