Zyloprim

— THERAPEUTIC CATEGORIES —
  • Gout
  • Hyperuricemia
  • Miscellaneous urogenital disorders
PAGE CONTENTS
  • Jump to Section
  • Generic Name & Formulations
  • Indications
  • Dosage and Administration
  • Contraindications
  • Boxed Warnings
  • Warnings/Precautions
  • Pharmacokinetics
  • Interactions
  • Adverse Reactions
  • Clinical Trials
  • Note
  • Patient Counseling

    • Zyloprim Generic Name & Formulations

    Legal Class

    Rx

    General Description

    Allopurinol 100mg, 200mg, 300mg; scored tabs.

    Pharmacological Class

    Xanthine oxidase inhibitor.

    How Supplied

    Tabs—90, 100, 500, 1000

    Storage

    Store at 20°C to 25°C (68°F to 77°F) in a dry place.

    Manufacturer

    Casper Pharma

    Generic Availability

    Tabs 100mg, 300mg (YES); 200mg (NO)

    Mechanism of Action

    Allopurinol acts on purine catabolism, without disrupting the biosynthesis of purines. It reduces the production of uric acid by inhibiting the biochemical reactions immediately preceding its formation. Allopurinol is a structural analogue of the natural purine base, hypoxanthine. It is an inhibitor of xanthine oxidase, the enzyme responsible for the conversion of hypoxanthine to xanthine and of xanthine to uric acid, the end product of purine metabolism in man.

    Zyloprim Indications

    Indications

    Gout.

    Limitations of Use

    Not for the treatment of asymptomatic hyperuricemia.

    Zyloprim Dosage and Administration

    Adult

    See full labeling. Take with fluids and after meals. Initially 100mg daily. Maintain prophylactic therapy (eg, colchicine, anti-inflammatory agent) upon initiation. Increase by 100mg weekly increments until a serum uric acid level ≤6mg/dL; max 800mg/day and 300mg/dose. Usual range (mild): 200–300mg daily; (moderate to severe): 400–600mg daily. Renal impairment (eGFR >30–60mL/min): 50mg/day; (eGFR >15–30mL/min): 50mg every other day; (eGFR 5–15 mL/min): 50mg twice weekly; (eGFR <5mL/min): 50mg once weekly.

    Children

    Not established.

    Zyloprim Contraindications

    Not Applicable

    Zyloprim Boxed Warnings

    Not Applicable

    Zyloprim Warnings/Precautions

    Warnings/Precautions

    Discontinue at 1st sign of skin rash. HLA-B*58:01 positive patients: not recommended. Consider screening for HLA-B*58:01 allele in high-risk populations prior to initiation (African, Asian [eg, Han Chinese, Korean, Thai], Native Hawaiian/Pacific Islander). Pre-existing liver or renal disease (including chronic renal disease or history of kidney stones). Maintain neutral or alkaline urine and increase urine output to ≥2 liters daily in adults. Monitor blood counts, hepatic, and renal function frequently during early stages of therapy. Discontinue if elevated liver enzymes develop. Pregnancy. Nursing mothers: not recommended (during and for 1 week after the last dose).

    Zyloprim Pharmacokinetics

    Absorption

    Approximately 90% absorbed from the GI tract. Peak plasma levels: 1.5 hours. Maximum plasma levels: ~3mcg/mL (after a 300 mg single dose).

    Elimination

    Renal (80%), fecal (20%). Half-life: ~1–2 hours.

    Zyloprim Interactions

    Interactions

    Increased risk of skin rash with ampicillin, amoxicillin, bendamustine, thiazides. Monitor renal function with thiazides; reduce allopurinol dose. Increased myelosuppression with cyclophosphamide and other cytotoxic agents (eg, doxorubicin, bleomycin, procarbazine, mechlorethamine), azathioprine, mercaptopurine; monitor blood count and reduce doses. Concomitant pegloticase may blunt the rise of serum uric acid levels and increase risk of pegloticase related anaphylaxis (if uric acid level rise >6mg/dL); discontinue and do not start allopurinol therapy. May antagonize capecitabine, fluorouracil; avoid. Antagonized by uricosurics; monitor. Potentiates anticoagulants (eg, dicumarol, warfarin); monitor prothrombin time and INR, respectively. May potentiate theophylline (with allopurinol ≥600mg/day), cyclosporine; monitor and adjust dose. Increased risk of hypoglycemia (with renal insufficiency) with chlorpropamide; monitor. Additive CNS depressant effects with alcohol and other CNS depressants.

    Zyloprim Adverse Reactions

    Adverse Reactions

    Nausea, diarrhea, increase in liver function tests, rash, drowsiness, somnolence, dizziness; serious skin reactions (eg, TEN, SJS, DRESS), nephrotoxicity, hepatotoxicity, myelosuppression.

    Zyloprim Clinical Trials

    See Literature

    Zyloprim Note

    Not Applicable

    Zyloprim Patient Counseling

    See Literature

    Zyloprim Generic Name & Formulations

    Legal Class

    Rx

    General Description

    Allopurinol 100mg, 200mg, 300mg; scored tabs.

    Pharmacological Class

    Xanthine oxidase inhibitor.

    How Supplied

    Tabs—90, 100, 500, 1000

    Storage

    Store at 20°C to 25°C (68°F to 77°F) in a dry place.

    Manufacturer

    Casper Pharma

    Generic Availability

    Tabs 100mg, 300mg (YES); 200mg (NO)

    Mechanism of Action

    Allopurinol acts on purine catabolism, without disrupting the biosynthesis of purines. It reduces the production of uric acid by inhibiting the biochemical reactions immediately preceding its formation. Allopurinol is a structural analogue of the natural purine base, hypoxanthine. It is an inhibitor of xanthine oxidase, the enzyme responsible for the conversion of hypoxanthine to xanthine and of xanthine to uric acid, the end product of purine metabolism in man.

    Zyloprim Indications

    Indications

    Management of hyperuricosuria and hyperuricemia in patients with leukemia, lymphoma, and solid tumor malignancies due to cancer therapy.

    Limitations of Use

    Not for the treatment of asymptomatic hyperuricemia.

    Zyloprim Dosage and Administration

    Adult

    See full labeling. Take with fluids and after meals. 300–800mg/day for 2–3 days prior to starting chemotherapy. Renal impairment (eGFR 10–20mL/min): 200mg/day; (eGFR <10mL/min): 100mg/day; (on dialysis): 50mg every 12hrs or 100mg every 24hrs.

    Children

    See full labeling. Take with fluids and after meals. 100mg/m2 every 8–12hrs (10mg/kg/day; max 800mg/day). BSA <0.5m2: consider alternative allopurinol formulation. Renal impairment: insufficient data.

    Zyloprim Contraindications

    Not Applicable

    Zyloprim Boxed Warnings

    Not Applicable

    Zyloprim Warnings/Precautions

    Warnings/Precautions

    Discontinue at 1st sign of skin rash. HLA-B*58:01 positive patients: not recommended. Consider screening for HLA-B*58:01 allele in high-risk populations prior to initiation (African, Asian [eg, Han Chinese, Korean, Thai], Native Hawaiian/Pacific Islander). Pre-existing liver or renal disease (including chronic renal disease or history of kidney stones). Maintain neutral or alkaline urine and increase urine output to ≥2 liters daily in adults or ≥100mL/m2/hr in children. Monitor blood counts, hepatic, and renal function at least daily during early stages of therapy. Discontinue if elevated liver enzymes develop. Pregnancy. Nursing mothers: not recommended (during and for 1 week after the last dose).

    Zyloprim Pharmacokinetics

    Absorption

    Approximately 90% absorbed from the GI tract. Peak plasma levels: 1.5 hours. Maximum plasma levels: ~3mcg/mL (after a 300 mg single dose).

    Elimination

    Renal (80%), fecal (20%). Half-life: ~1–2 hours.

    Zyloprim Interactions

    Interactions

    Increased risk of skin rash with ampicillin, amoxicillin, bendamustine, thiazides. Monitor renal function with thiazides; reduce allopurinol dose. Increased myelosuppression with cyclophosphamide and other cytotoxic agents (eg, doxorubicin, bleomycin, procarbazine, mechlorethamine), azathioprine, mercaptopurine; monitor blood count and reduce doses. Concomitant pegloticase may blunt the rise of serum uric acid levels and increase risk of pegloticase related anaphylaxis (if uric acid level rise >6mg/dL); discontinue and do not start allopurinol therapy. May antagonize capecitabine, fluorouracil; avoid. Antagonized by uricosurics; monitor. Potentiates anticoagulants (eg, dicumarol, warfarin); monitor prothrombin time and INR, respectively. May potentiate theophylline (with allopurinol ≥600mg/day), cyclosporine; monitor and adjust dose. Increased risk of hypoglycemia (with renal insufficiency) with chlorpropamide; monitor. Additive CNS depressant effects with alcohol and other CNS depressants.

    Zyloprim Adverse Reactions

    Adverse Reactions

    Nausea, diarrhea, increase in liver function tests, rash, drowsiness, somnolence, dizziness; serious skin reactions (eg, TEN, SJS, DRESS), nephrotoxicity, hepatotoxicity, myelosuppression.

    Zyloprim Clinical Trials

    See Literature

    Zyloprim Note

    Not Applicable

    Zyloprim Patient Counseling

    See Literature

    Zyloprim Generic Name & Formulations

    Legal Class

    Rx

    General Description

    Allopurinol 100mg, 200mg, 300mg; scored tabs.

    Pharmacological Class

    Xanthine oxidase inhibitor.

    How Supplied

    Tabs—90, 100, 500, 1000

    Storage

    Store at 20°C to 25°C (68°F to 77°F) in a dry place.

    Manufacturer

    Casper Pharma

    Generic Availability

    Tabs 100mg, 300mg (YES); 200mg (NO)

    Mechanism of Action

    Allopurinol acts on purine catabolism, without disrupting the biosynthesis of purines. It reduces the production of uric acid by inhibiting the biochemical reactions immediately preceding its formation. Allopurinol is a structural analogue of the natural purine base, hypoxanthine. It is an inhibitor of xanthine oxidase, the enzyme responsible for the conversion of hypoxanthine to xanthine and of xanthine to uric acid, the end product of purine metabolism in man.

    Zyloprim Indications

    Indications

    In adults with recurrent calcium oxalate calculi whose daily uric acid excretion exceeds 800mg/day (males) and 750mg/day (females), despite lifestyle changes (eg, reduction of dietary sodium, non-dairy animal protein, oxylate rich foods, refined sugars and increases in oral fluids, fruits, and vegetables).

    Limitations of Use

    Not for the treatment of asymptomatic hyperuricemia.

    Zyloprim Dosage and Administration

    Adult

    See full labeling. Take with fluid and after meals. 200–300mg daily. Adjust based on 24-hour urinary urate levels. Renal impairment: insufficient data.

    Children

    Not established.

    Zyloprim Contraindications

    Not Applicable

    Zyloprim Boxed Warnings

    Not Applicable

    Zyloprim Warnings/Precautions

    Warnings/Precautions

    Discontinue at 1st sign of skin rash. HLA-B*58:01 positive patients: not recommended. Consider screening for HLA-B*58:01 allele in high-risk populations prior to initiation (African, Asian [eg, Han Chinese, Korean, Thai], Native Hawaiian/Pacific Islander). Pre-existing liver or renal disease (including chronic renal disease or history of kidney stones). Maintain neutral or alkaline urine and increase urine output to ≥2 liters daily in adults. Monitor blood counts, hepatic, and renal function frequently during early stages of therapy. Discontinue if elevated liver enzymes develop. Pregnancy. Nursing mothers: not recommended (during and for 1 week after the last dose).

    Zyloprim Pharmacokinetics

    Absorption

    Approximately 90% absorbed from the GI tract. Peak plasma levels: 1.5 hours. Maximum plasma levels: ~3mcg/mL (after a 300 mg single dose).

    Elimination

    Renal (80%), fecal (20%). Half-life: ~1–2 hours.

    Zyloprim Interactions

    Interactions

    Increased risk of skin rash with ampicillin, amoxicillin, bendamustine, thiazides. Monitor renal function with thiazides; reduce allopurinol dose. Increased myelosuppression with cyclophosphamide and other cytotoxic agents (eg, doxorubicin, bleomycin, procarbazine, mechlorethamine), azathioprine, mercaptopurine; monitor blood count and reduce doses. Concomitant pegloticase may blunt the rise of serum uric acid levels and increase risk of pegloticase related anaphylaxis (if uric acid level rise >6mg/dL); discontinue and do not start allopurinol therapy. May antagonize capecitabine, fluorouracil; avoid. Antagonized by uricosurics; monitor. Potentiates anticoagulants (eg, dicumarol, warfarin); monitor prothrombin time and INR, respectively. May potentiate theophylline (with allopurinol ≥600mg/day), cyclosporine; monitor and adjust dose. Increased risk of hypoglycemia (with renal insufficiency) with chlorpropamide; monitor. Additive CNS depressant effects with alcohol and other CNS depressants.

    Zyloprim Adverse Reactions

    Adverse Reactions

    Nausea, diarrhea, increase in liver function tests, rash, drowsiness, somnolence, dizziness; serious skin reactions (eg, TEN, SJS, DRESS), nephrotoxicity, hepatotoxicity, myelosuppression.

    Zyloprim Clinical Trials

    See Literature

    Zyloprim Note

    Not Applicable

    Zyloprim Patient Counseling

    See Literature

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