Zyloric 100Mg Tab 50 s Potential Overview:

Generic Name: Allopurinol
Brand Name: Zyloric
Formulation: 100 mg tablets
Pack Size: 50 tablets

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Zyloric 100 mg Tablets (50 tablets) is a medication commonly prescribed for the treatment of gout and hyperuricemia (high levels of uric acid in the blood), which are conditions that can lead to painful joint inflammation due to the buildup of uric acid crystals.

Mechanism of Action:

Allopurinol works by inhibiting the enzyme xanthine oxidase, which is responsible for the production of uric acid in the body. By reducing the amount of uric acid, it helps prevent gout attacks and the formation of uric acid crystals in the joints, which can lead to painful inflammation.

Indications:

1. Gout: Zyloric is used to treat gout, a form of arthritis that occurs due to elevated levels of uric acid in the blood, leading to the formation of uric acid crystals in joints.
2. Hyperuricemia: High levels of uric acid in the blood, which can result from conditions like kidney disease, can be managed with Zyloric to reduce the risk of gout.
3. Kidney Stones: Allopurinol is sometimes used to prevent the formation of uric acid kidney stones.

Dosage:

• Adults: The usual starting dose of allopurinol is typically 100 mg per day. This may be increased depending on the individual’s response and uric acid levels, but the typical maintenance dose ranges from 200 mg to 300 mg per day. Some patients may need higher doses (up to 800 mg per day), but this is usually divided into several doses.
• For Gout: Dosing often starts low and gradually increases to avoid any sudden shifts in uric acid levels, which could potentially trigger a gout flare.

Common Dosage Forms:

• Zyloric comes in 100 mg tablets, and in some cases, higher doses (e.g., 300 mg tablets) may also be available.

Side Effects:

Allopurinol is generally well-tolerated, but like all medications, it can cause side effects. Some potential side effects include:

• Common Side Effects:
  • Rash
  • Nausea
  • Diarrhea
  • Headache
  • Drowsiness
• Serious Side Effects:
  • Severe skin reactions (e.g., Stevens-Johnson syndrome), though rare, can be serious and require immediate medical attention.
  • Liver problems (e.g., jaundice, dark urine, fatigue).
  • Kidney problems: Allopurinol can affect kidney function, so monitoring kidney function is important, especially at higher doses.
• Allergic Reactions: Some people may have hypersensitivity to allopurinol, leading to allergic reactions like skin rashes, itching, or more severe conditions like anaphylaxis.

Precautions:

1. Kidney Impairment: People with impaired kidney function should use Zyloric cautiously, as the drug is metabolized in the kidneys. The dosage may need to be reduced.
2. Drug Interactions: Allopurinol may interact with other medications, including certain diuretics, antibiotics, and medications used to treat cancer. It’s essential to inform your doctor about any other medications you are taking, including over-the-counter drugs and supplements.
3. Hydration: It’s important to stay well-hydrated when taking allopurinol, as it can help reduce the risk of kidney stones or other kidney-related issues.

Pharmacist Related Data

Chemical Formula:

Allopurinol
Chemical formula: C5H4N4O

Half-Life:

The elimination half-life of allopurinol is approximately 1 to 2 hours, but its active metabolite, oxypurinol, has a much longer half-life of about 15-30 hours.

Metabolism:

• Allopurinol is primarily metabolized in the liver to oxypurinol (also known as alloxanthine), which is responsible for the drug’s therapeutic effects.
• Oxypurinol is excreted in the urine.
• The metabolism of allopurinol may be impaired in patients with renal insufficiency, leading to the accumulation of its active metabolite (oxypurinol).

Drug Interactions:

1. With Other Medications:
   • Azathioprine or Mercaptopurine: Allopurinol inhibits the metabolism of these drugs, leading to an increased risk of toxicity (e.g., bone marrow suppression).
   • Warfarin: Allopurinol may enhance the effects of warfarin, increasing the risk of bleeding.
   • Cyclophosphamide: There is a risk of increased toxicity.
   • Diuretics (e.g., thiazides): Can increase the risk of allopurinol-induced hypersensitivity reactions.
   • Rifampicin, Phenytoin, and other drugs metabolized by the liver may alter the effectiveness of allopurinol by modifying its metabolism.
2. With Food:
   • Food does not significantly affect the absorption of allopurinol, but it is advisable to take it after meals to reduce the risk of gastrointestinal upset.
   • Alcohol: Excessive alcohol consumption may interfere with the action of allopurinol and increase the risk of gout attacks.
3. With Other Gout Medications:
   • Colchicine or NSAIDs: These can be used in combination with allopurinol to manage acute gout attacks. However, the risk of gastrointestinal side effects (e.g., nausea) may increase when combined with colchicine.

Pharmacodynamics:

Allopurinol is a xanthine oxidase inhibitor. Xanthine oxidase is an enzyme responsible for converting purines into uric acid. By inhibiting this enzyme, allopurinol reduces the production of uric acid, which is helpful in managing conditions like gout, hyperuricemia, and kidney stones associated with high uric acid levels.

• Therapeutic Effects:
  • Reduces serum uric acid levels, helping to prevent gout attacks and manage chronic gout.
  • It also reduces the risk of urate crystal deposition in tissues and joints.
  • Helps prevent kidney stones in patients with high uric acid levels.

Pharmacokinetics:

• Absorption: Allopurinol is well absorbed from the gastrointestinal tract after oral administration, with peak plasma concentrations occurring within 1.5-2 hours of ingestion.
• Distribution: It is moderately bound to plasma proteins (20-30%).
• Metabolism: As mentioned, allopurinol is metabolized into oxypurinol in the liver, and oxypurinol is responsible for the primary pharmacologic action of the drug.
• Excretion: Allopurinol and its metabolites are primarily excreted in the urine, with about 80% of the drug being excreted as oxypurinol.