Zoleric Cap 20 Mg 2×7’s(Esomeprazole)-Potential Overview

• Brand Name: Zoleric
• Generic Name: Esomeprazole
• Strength: 20 mg per capsule
• Pack Size: 2×7 capsules (14 capsules per pack)

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Zoleric Cap 20 mg 2×7’s (Esomeprazole) is a proton pump inhibitor (PPI) used primarily for managing conditions associated with excess stomach acid, such as gastroesophageal reflux disease (GERD), gastric ulcers, and Helicobacter pylori eradication. Esomeprazole is the S-isomer of omeprazole, offering enhanced efficacy in reducing gastric acid production.

Potential Uses and Benefits:

• GERD: Zoleric helps relieve heartburn and acid reflux by significantly reducing gastric acid secretion.
• Peptic Ulcers: It aids in the healing of ulcers and reduces the recurrence of bleeding ulcers.
• Helicobacter pylori Eradication: Esomeprazole is used in combination therapy to eradicate H. pylori in patients with duodenal ulcers.
• Zollinger-Ellison Syndrome: Used to manage severe acid-related conditions.

Mechanism of Action:

Esomeprazole works by blocking the proton pump in the stomach lining, specifically the H+/K+ ATPase enzyme, which is responsible for the final step of acid secretion. By inhibiting this proton pump, esomeprazole effectively decreases stomach acidity, providing relief from symptoms like heartburn and preventing damage to the esophagus and stomach lining.

Drug Interactions:

• With Other Medications: Esomeprazole can interact with drugs like clopidogrel, warfarin, and diazepam, altering their effectiveness due to CYP enzyme inhibition.
• With Food: Food has little effect on esomeprazole absorption, but taking it before meals can optimize its effectiveness.

Side Effects:

• Common Side Effects: Headaches, abdominal pain, nausea, and diarrhea.
• Serious Effects: Long-term use can lead to vitamin B12 deficiency, kidney damage, and bone fractures.

Precautions:

• Kidney and Liver Function: Patients with liver or kidney disease should use esomeprazole cautiously.
• Pregnancy: Esomeprazole is generally considered safe for use during pregnancy but should be used under medical supervision

Pharmacist Related Data

Chemical Name and Formula:

• Chemical Name: (S)-5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]benzimidazole
• Molecular Formula: C17H18N3O3S

Pharmacokinetics:

1. Absorption:
   • Esomeprazole is rapidly absorbed after oral administration. The peak plasma concentration is usually reached within 1 to 2 hours.
   • The absorption can be slightly delayed when taken with food, but the overall bioavailability is not significantly affected.
2. Half-life:
   • The elimination half-life of esomeprazole is approximately 1 to 1.5 hours, but the therapeutic effects (acid suppression) last for up to 24 hours due to the prolonged action at the proton pump.
3. Metabolism:
   • Esomeprazole is metabolized in the liver via the CYP2C19 and CYP3A4 enzymes.
   • It is converted into inactive metabolites, which are primarily excreted through the urine.
4. Excretion:
   • About 80% of the drug is excreted in the urine, with a small amount being eliminated in the feces.

Pharmacodynamics:

• Esomeprazole inhibits the proton pump (H+/K+ ATPase enzyme) in the gastric parietal cells, which is responsible for the final step in gastric acid secretion.
• By reducing the acidity in the stomach, esomeprazole helps heal ulcers, relieve symptoms of GERD, and prevent further acid-related damage in the esophagus and stomach lining.

Drug Interactions:

1. With Other Medications:
   • Clopidogrel: Esomeprazole may reduce the effectiveness of clopidogrel, an anti-platelet drug, by inhibiting its conversion to its active form via the CYP2C19 enzyme.
   • Warfarin, Diazepam, Phenytoin: Esomeprazole can alter the metabolism of drugs processed by CYP2C19 and CYP3A4, potentially increasing their plasma levels and effects.
   • Methotrexate: Concurrent use with esomeprazole can increase the risk of methotrexate toxicity, particularly at high doses.
2. With Food:
   • Food may slightly delay the absorption of esomeprazole but does not significantly affect its overall absorption. It is generally recommended to take esomeprazole before meals to optimize its effect.
3. With Alcohol:
   • Alcohol should be avoided while using esomeprazole, as it may exacerbate gastrointestinal irritation and reduce the drug’s effectiveness.