IMURAN- azathioprine tablet

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

azathioprine (UNII: MRK240IY2L) (azathioprine - UNII:MRK240IY2L)

Available from:

Prometheus Laboratories Inc.

INN (International Name):

azathioprine

Composition:

azathioprine 50 mg

Administration route:

ORAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

IMURAN is indicated as an adjunct for the prevention of rejection in renal homotransplantation. It is also indicated for the management of active rheumatoid arthritis to reduce signs and symptoms. Renal Homotransplantation: IMURAN is indicated as an adjunct for the prevention of rejection in renal homotransplantation. Experience with over 16,000 transplants shows a 5-year patient survival of 35% to 55%, but this is dependent on donor, match for HLA antigens, anti-donor or anti-B-cell alloantigen antibody, and other variables. The effect of IMURAN on these variables has not been tested in controlled trials. Rheumatoid Arthritis: IMURAN is indicated for the treatment of active rheumatoid arthritis (RA) to reduce signs and symptoms. Aspirin, non-steroidal anti-inflammatory drugs and/or low dose glucocorticoids may be continued during treatment with IMURAN. The combined use of IMURAN with disease modifying anti-rheumatic drugs (DMARDs) has not been studied for either added benefit or unexpected adverse effects

Product summary:

50 mg overlapping circle-shaped, yellow to off-white, scored tablets imprinted with “IMURAN” and “50” on each tablet; bottle of 100 (NDC 65483-590-10). Store at 20-25 °C (USP Controlled Room Temperature) (68° to 77°F) in a dry place and protect from light.

Authorization status:

New Drug Application

Summary of Product characteristics

IMURAN- AZATHIOPRINE TABLET
PROMETHEUS LABORATORIES INC.
----------
IMURAN (AZATHIOPRINE)
50-MG SCORED TABLETS
PRODUCT INFORMATION
Rx only
WARNING - MALIGNANCY
Chronic immunosuppression with IMURAN, a purine antimetabolite
increases _risk of malignancy_
in humans. Reports of malignancy include post-transplant lymphoma and
hepatosplenic T-cell
lymphoma (HSTCL) in patients with inflammatory bowel disease.
Physicians using this drug
should be very familiar with this risk as well as with the mutagenic
potential to both men and
women and with possible hematologic toxicities. Physicians should
inform patients of the risk of
malignancy with IMURAN. See WARNINGS.
DESCRIPTION:
IMURAN (azathioprine), an immunosuppressive antimetabolite, is
available in tablet form for oral
administration. Each scored tablet contains 50 mg azathioprine and the
inactive ingredients lactose,
magnesium stearate, potato starch, povidone, and stearic acid.
Azathioprine is chemically
6-[(1-methyl-4-nitro-1_H_-imidazol-5-yl)thio]-1_H_-purine. The
structural
formula of azathioprine is:
It is an imidazolyl derivative of 6-mercaptopurine and many of its
biological effects are similar to those
of the parent compound.
Azathioprine is insoluble in water, but may be dissolved with addition
of one molar equivalent of alkali.
Azathioprine is stable in solution at neutral or acid pH but
hydrolysis to mercaptopurine occurs in
excess sodium hydroxide (0.1N), especially on warming. Conversion to
mercaptopurine also occurs in
the presence of sulfhydryl compounds such as cysteine, glutathione,
and hydrogen sulfide.
CLINICAL PHARMACOLOGY:
Azathioprine is well absorbed following oral administration. Maximum
serum radioactivity occurs at 1
to 2 hours after oral
S-azathioprine and 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
S-containing metabolites of the drug.
Because of extensive metabolism, only a fraction of the radioactivity
is present as azathioprine. Usual
doses produce blo