Zurig Tab 80 Mg 20’S

Potential Overview:

Brand Name: Zurig Tab

Generic Name: Febuxostat

Strength: 80 mg

Formulation: Tablet

Pack Size: 20 Tablets

ZurigTab 80 mg is a brand name for a medication that contains Febuxostat as the active ingredient. It’s primarily used for the management of gout and hyperuricemia (elevated levels of uric acid in the blood). Here’s more detailed information about ZurigTab:

1. Mechanism of Action (MOA):

• Febuxostat works by inhibiting xanthine oxidase, an enzyme that is involved in the production of uric acid. By blocking this enzyme, Febuxostat reduces the production of uric acid, which helps to lower blood levels of uric acid, preventing the formation of urate crystals that cause gout and hyperuricemia.

2. Indications:

ZurigTab (Febuxostat 80 mg) is indicated for the treatment of:

• Chronic Gout: To manage hyperuricemia (elevated uric acid levels) and prevent gout attacks.
• Hyperuricemia: Particularly in patients with conditions like gout or tumor lysis syndrome, where elevated uric acid levels need to be managed.

3. Dosage:

• Starting Dose: 40 mg once daily.
• If uric acid levels remain elevated after 2 weeks, the dose may be increased to 80 mg once daily.
• Maximum Dose: 120 mg once daily, if needed, to achieve target uric acid levels.
• Administration:
  • Take ZurigTab (Febuxostat) once daily.
  • Can be taken with or without food.
  • Swallow tablets whole, do not crush or chew.
• Special Considerations:
  • Renal Impairment: No dose adjustment is necessary in patients with mild-to-moderate renal impairment. However, caution is advised in severe renal impairment.
  • Hepatic Impairment: Caution is required in patients with liver conditions.

4. Side Effects:

Common side effects of Febuxostat (ZurigTab):

• Headache.
• Gastrointestinal symptoms: Nausea, diarrhea, or constipation.
• Rash.

Serious side effects:

• Cardiovascular issues: Increased risk of heart attack, stroke, and other cardiovascular events, particularly in patients with pre-existing heart conditions.
• Liver enzyme abnormalities: Requires liver function monitoring during treatment.
• Severe allergic reactions: Rare, including anaphylaxis.
• Severe skin reactions: Rare but serious conditions like Stevens-Johnson syndrome and toxic epidermal necrolysis.
• Kidney problems: Increased risk of kidney damage, especially in long-term use.
• Gout flare-ups: Initial treatment may trigger acute gout attacks; preventive anti-inflammatory therapy may be used.

5. Precautions:

• Cardiovascular Risk: Febuxostat may increase the risk of cardiovascular events, such as heart attacks or strokes. It should be used cautiously in patients with a history of heart disease or stroke.
• Liver Function: Regular monitoring of liver enzymes is recommended, as Febuxostat may cause liver toxicity.
• Renal Function: Use with caution in patients with renal impairment. Periodic monitoring of kidney function is advised.
• Acute Gout Flare: During the initiation of treatment, an acute gout flare may occur as uric acid levels drop. Prophylactic treatment with colchicine or NSAIDs may be recommended for the first few months.
• Drug Interactions: Monitor for drug interactions, especially with medications like azathioprine, mercaptopurine, and theophylline, as Febuxostat can increase their levels and toxicity.

6. Contraindications (CI):

ZurigTab (Febuxostat) should not be used in the following conditions:

• Hypersensitivity: Known allergy or hypersensitivity to Febuxostat or any of its components.
• Severe Liver Impairment: Contraindicated in patients with severe liver dysfunction or active liver disease.
• Concomitant Use with Azathioprine or Mercaptopurine: Febuxostat inhibits the metabolism of these drugs, increasing their toxicity.
• Pregnancy: Category C (risk cannot be ruled out). It should be used only if clearly necessary and under strict medical supervision.
• Breastfeeding: It is not recommended during breastfeeding due to unknown excretion in milk.
• Severe Renal Impairment: Use with caution, though no specific contraindication, dosing adjustments may be needed.

Pharmacist Related  Data

Chemical Name and Formula:

• Chemical Name: 2-[3-cyano-4-(2-methylpropoxy)phenyl]thiazole-5-carboxylic acid
• Molecular Formula: C16H16N2O3S
• Molecular Weight: 320.39 g/mol

Half-Life:

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

Metabolism:

• Febuxostat is primarily metabolized in the liver.
• It undergoes oxidative metabolism through the cytochrome P450 enzyme system, specifically CYP1A2 and CYP2C9, to form inactive metabolites.
• The main metabolite is 2-hydroxyfebuxostat, which is pharmacologically inactive.
• Febuxostat is then excreted mainly in the urine (about 50% of the dose), with a smaller portion excreted in the feces.

Drug Interactions:

Drug Interactions with Medicines:

• Azathioprine and Mercaptopurine:
  • Febuxostat inhibits xanthine oxidase, which is responsible for the metabolism of azathioprine and mercaptopurine. The inhibition of this enzyme leads to an increase in the levels of these drugs, resulting in increased toxicity. These medications should not be used together with Febuxostat.
• Theophylline:
  • Febuxostat may increase the serum concentration of theophylline, a drug used for respiratory conditions, because it inhibits its metabolism. Close monitoring is recommended if these drugs must be used together.
• Warfarin:
  • Febuxostat may enhance the anticoagulant effect of warfarin, increasing the risk of bleeding. Regular monitoring of INR (International Normalized Ratio) is advised.
• Diuretics (e.g., Thiazide diuretics):
  • Diuretics, especially thiazides, may increase serum uric acid levels, which can counteract the effects of Febuxostat. Close monitoring is advised if these medications are used concurrently.
• Rash and Allergic Reactions:
  • When combined with other drugs that may cause skin reactions (e.g., allopurinol), there may be an increased risk of serious skin reactions. Caution is required.

Drug Interactions with Food:

• Food: There are no significant food interactions with Febuxostat. It can be taken with or without food without affecting its absorption or efficacy.
• Grapefruit and grapefruit juice: Although grapefruit juice typically affects the metabolism of many drugs, Febuxostat does not show significant interaction with grapefruit juice, making it safe to consume in moderation.

Pharmacodynamics:

• Febuxostat is a xanthine oxidase inhibitor that reduces uric acid production by inhibiting the xanthine oxidase enzyme, which plays a key role in converting hypoxanthine and xanthine into uric acid.
• This reduction in uric acid production helps prevent hyperuricemia and gout symptoms such as pain and inflammation caused by the deposition of urate crystals in joints.
• Febuxostat lowers serum uric acid levels, thereby reducing the risk of gout flares and promoting the dissolution of existing urate crystals in the joints.

Pharmacokinetics:

• Absorption:
  • Febuxostat is well absorbed after oral administration.
  • Peak plasma concentrations occur about 1.5 to 2 hours after oral dosing.
  • Bioavailability is approximately 49% when taken orally.
• Distribution:
  • Febuxostat is widely distributed in the body. It is highly protein-bound, around 99% to plasma proteins (mainly albumin), which suggests minimal distribution to the tissues that lack high protein content.
• Metabolism:
  • Febuxostat is metabolized by the liver through the cytochrome P450 (CYP) enzyme system, primarily CYP1A2 and CYP2C9.
  • It is metabolized to inactive metabolites, with 2-hydroxyfebuxostat being the main metabolite.
• Excretion:
  • Febuxostat and its metabolites are primarily excreted in the urine (approximately 50% of the dose) and to a lesser extent in the feces.
  • The half-life is about 5-8 hours, allowing for once-daily dosing.
• Steady-State:
  • It takes about 3 to 5 days of daily dosing to reach steady-state concentrations of the drug in the plasma