Zurig Tab 40 Mg 20’S

Potential Overview:

• Brand Name: Zurig
• Generic Name: Febuxostat
• Strength: 40 mg
• Form: Tablet

This is a medication that contains the active ingredient febuxostat and is typically used to treat gout and hyperuricemia (elevated uric acid levels in the blood).

Mechanism of Action:

• Febuxostat works by inhibiting the enzyme xanthine oxidase, which is responsible for producing uric acid in the body. By blocking this enzyme, febuxostat reduces the production of uric acid, helping to lower levels in the blood and prevent gout attacks and kidney stones.
  

  Indication:

  Zurig (febuxostat) is used primarily to lower uric acid levels in the body, which helps in the management of:

  • Gout: A condition where uric acid crystals accumulate in the joints, leading to inflammation and pain.
  • Hyperuricemia: High uric acid levels in the blood, which may increase the risk of gout or kidney stones.
    

    Dosage:

    • Starting Dose: 40 mg once daily, with or without food.
    • Maintenance Dose: The dose can be increased to 80 mg daily, depending on the patient’s response and the target uric acid levels.
    • The exact dose and duration of treatment should be determined by a healthcare provider based on the patient’s condition and response to the drug.

    Common Side Effects:

    • Headache
    • Nausea
    • Liver enzyme abnormalities (which requires monitoring during treatment)
    • Joint pain (may worsen initially due to uric acid crystal mobilization)
    • Rash
    • Abdominal discomfort or diarrhea

    Precautions:

    • Liver Function: Febuxostat may cause liver enzyme abnormalities. Regular monitoring of liver function is recommended.
    • Cardiovascular Risk: Use with caution in patients with a history of heart disease. Febuxostat may increase the risk of cardiovascular events (heart attack or stroke) in patients with pre-existing cardiovascular conditions.
    • Acute Gout Flare-ups: Gout symptoms may worsen in the early stages of treatment as the uric acid levels decrease. Patients may need additional medications (like colchicine) to prevent flare-ups.
    • Kidney Function: Dose adjustments might be required for patients with impaired kidney function.

    Contraindications:

    • Severe liver or kidney impairment.
    • Pregnancy: Febuxostat should only be used during pregnancy if clearly needed, as its safety during pregnancy has not been established.
    • Breastfeeding: The safety of febuxostat during breastfeeding is not well-established, so it should be used with caution.

                             

     Pharmacist Related Data

                            

 Chemical Name and Formula:

• Chemical Name: (S)-4-[3-cyano-4-(2-methylthiazol-4-yl)-phenyl]thiazol-2-yl]-2-(trifluoromethyl)-benzenesulfonamide
• Chemical Formula: C16H16N4O3S (Febuxostat)

 Half-Life:

• Elimination Half-Life: Approximately 5 to 8 hours. This is the time it takes for the concentration of the drug in the bloodstream to decrease by half.

 Metabolism:

• Primary Metabolism: Febuxostat is extensively metabolized in the liver primarily via CYP450 enzymes, especially CYP1A2 and CYP3A4.
• Metabolites: The major metabolite is a 6-hydroxyfebuxostat, which is pharmacologically inactive.
• Excretion: Metabolites and the unchanged drug are primarily excreted via the urine (approximately 49%) and feces (approximately 46%).

 Drug Interactions:

With Food:

• Food does not significantly affect the absorption of febuxostat, meaning it can be taken with or without food.

With Other Medications:

• Xanthine oxidase inhibitors: Avoid concurrent use with allopurinol (another gout medication) as it may increase the risk of adverse effects like severe skin reactions.
• Thiazide Diuretics: Use with caution, as thiazides can increase uric acid levels, potentially reducing febuxostat’s effectiveness.
• Theophylline: Febuxostat may increase the blood levels of theophylline (a bronchodilator), which can lead to toxic effects.
• Antacids: No significant interactions with antacids, but it’s always good practice to separate the administration of these.
• Warfarin (Anticoagulants): Some studies suggest febuxostat may increase the effect of warfarin, increasing bleeding risk. Monitor INR levels carefully if used together.
• Azathioprine and Mercaptopurine: Concomitant use with febuxostat can increase blood levels of these immunosuppressive drugs, possibly leading to toxicity. Use caution and consider dose adjustment.

 Pharmacodynamics:

• Mechanism of Action:
  Febuxostat is a selective inhibitor of the enzyme xanthine oxidase, which is responsible for converting hypoxanthine and xanthine into uric acid. By inhibiting xanthine oxidase, febuxostat reduces the synthesis of uric acid in the body.
  • Result: Decrease in blood uric acid levels, reducing the formation of uric acid crystals in joints and tissues, thus preventing gout attacks and lowering the risk of kidney stone formation.
• Pharmacological Effects:
  • Anti-gout: Lowers uric acid levels and reduces inflammation in gout.
  • Hyperuricemia management: Treats elevated uric acid in blood, which is associated with gout, but also other conditions like kidney stones.

7. Pharmacokinetics:

Absorption:

• Febuxostat is well-absorbed orally, with a bioavailability of approximately 49%.
• Time to Peak Plasma Concentration: About 1 to 1.5 hours after oral administration.

Distribution:

• Febuxostat is widely distributed throughout the body, with a volume of distribution (Vd) of about 2.5 L/kg.
• Plasma Protein Binding: Approximately 99% of febuxostat is bound to plasma proteins (primarily albumin), which can affect its interaction with other medications that also bind to proteins.

Metabolism:

• As mentioned earlier, febuxostat is metabolized in the liver, primarily by the CYP1A2 and CYP3A4 enzymes. It is converted into several metabolites, most of which are inactive.

Excretion:

• The drug and its metabolites are primarily excreted in the urine (about 49%) and feces (about 46%).
• Very little unchanged drug is excreted in the urine, indicating extensive metabolism