Imuran Generic Name & Formulations
Legal Class
General Description
Pharmacological Class
How Supplied
Manufacturer
Imuran Indications
Indications
Imuran Dosage and Administration
Adult
Children
Renal Impairment
Relatively oliguric patients, especially those with tubular necrosis in the immediate postcadaveric transplant period, may have delayed clearance of Imuran or its metabolites, may be particularly sensitive to this drug, and are usually given lower doses.
Other Modifications
Patients with TPMT and/or NUDT15 Deficiency
-
Consider testing for TPMT and NUDT15 deficiency in patients who experience severe bone marrow toxicities. Early drug discontinuation may be considered in patients with abnormal CBC results that do not respond to dose reduction.
Homozygous deficiency in either TPMT or NUDT15
-
Consider alternative therapies for patients who are known to have TPMT or NUDT15 deficiency due to the risk of increased toxicity.
Heterozygous deficiency in TPMT and/or NUDT15
-
Dosage reduction is recommended in patients known to have heterozygous deficiency of TPMT or NUDT15 due to the risk of increased toxicity. Patients who are heterozygous for both TPMT and NUDT15 deficiency may require more substantial dosage reductions.
Effect on Sperm in Animals
-
Imuran has been reported to cause temporary depression in spermatogenesis and reduction in sperm viability and sperm count in mice at doses 10 times the human therapeutic dose; a reduced percentage of fertile matings occurred when animals received 5 mg/kg.
Imuran Contraindications
Contraindications
Imuran Boxed Warnings
Boxed Warning
Imuran Warnings/Precautions
Warnings/Precautions
Imuran Pharmacokinetics
Absorption
Azathioprine is well absorbed following oral administration. Maximum serum radioactivity occurs at 1 to 2 hours after oral 35S-azathioprine.
Distribution
Azathioprine and mercaptopurine are moderately bound to serum proteins (30%) and are partially dialyzable.
Elimination
Azathioprine is metabolized to 6-mercaptopurine (6-MP). Both compounds are rapidly eliminated from blood and are oxidized or methylated in erythrocytes and liver; no azathioprine or mercaptopurine is detectable in urine after 8 hours.
Azathioprine decays with a half-life of 5 hours. This is not an estimate of the half-life of azathioprine itself, but is the decay rate for all 35S-containing metabolites of the drug. Because of extensive metabolism, only a fraction of the radioactivity is present as azathioprine.
Imuran Interactions
Interactions
Imuran Adverse Reactions
Adverse Reactions
Imuran Clinical Trials
See Literature
Imuran Note
Not Applicable
Imuran Patient Counseling
Imuran Generic Name & Formulations
Legal Class
General Description
Pharmacological Class
How Supplied
Manufacturer
Imuran Indications
Indications
Imuran Dosage and Administration
Adult
Children
Renal Impairment
Relatively oliguric patients, especially those with tubular necrosis in the immediate postcadaveric transplant period, may have delayed clearance of Imuran or its metabolites, may be particularly sensitive to this drug, and are usually given lower doses.
Other Modifications
Patients with TPMT and/or NUDT15 Deficiency
-
Consider testing for TPMT and NUDT15 deficiency in patients who experience severe bone marrow toxicities. Early drug discontinuation may be considered in patients with abnormal CBC results that do not respond to dose reduction.
Homozygous deficiency in either TPMT or NUDT15
-
Consider alternative therapies for patients who are known to have TPMT or NUDT15 deficiency due to the risk of increased toxicity.
Heterozygous deficiency in TPMT and/or NUDT15
-
Dosage reduction is recommended in patients known to have heterozygous deficiency of TPMT or NUDT15 due to the risk of increased toxicity. Patients who are heterozygous for both TPMT and NUDT15 deficiency may require more substantial dosage reductions.
Effect on Sperm in Animals
-
Imuran has been reported to cause temporary depression in spermatogenesis and reduction in sperm viability and sperm count in mice at doses 10 times the human therapeutic dose; a reduced percentage of fertile matings occurred when animals received 5 mg/kg.
Imuran Contraindications
Contraindications
Imuran Boxed Warnings
Boxed Warning
Imuran Warnings/Precautions
Warnings/Precautions
Imuran Pharmacokinetics
Absorption
Azathioprine is well absorbed following oral administration. Maximum serum radioactivity occurs at 1 to 2 hours after oral 35S-azathioprine.
Distribution
Azathioprine and mercaptopurine are moderately bound to serum proteins (30%) and are partially dialyzable.
Elimination
Azathioprine is metabolized to 6-mercaptopurine (6-MP). Both compounds are rapidly eliminated from blood and are oxidized or methylated in erythrocytes and liver; no azathioprine or mercaptopurine is detectable in urine after 8 hours.
Azathioprine decays with a half-life of 5 hours. This is not an estimate of the half-life of azathioprine itself, but is the decay rate for all 35S-containing metabolites of the drug. Because of extensive metabolism, only a fraction of the radioactivity is present as azathioprine.
Imuran Interactions
Interactions
Imuran Adverse Reactions
Adverse Reactions
Imuran Clinical Trials
See Literature
Imuran Note
Not Applicable