AZATHIOPRINE tablet

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

AZATHIOPRINE (UNII: MRK240IY2L) (AZATHIOPRINE - UNII:MRK240IY2L)

Available from:

Mylan Institutional Inc.

INN (International Name):

AZATHIOPRINE

Composition:

AZATHIOPRINE 50 mg

Administration route:

ORAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Azathioprine tablets are 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. Azathioprine tablets are 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 azathioprine tablets on these variables has not been tested in controlled trials. Azathioprine tablets are 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 azathioprine tablets. The combined use of azathioprine tablets with disease modifying anti-rheumatic drugs (DMARDs) has not been studied for either added be

Product summary:

Azathioprine Tablets, USP are available containing 50 mg of azathioprine, USP. The 50 mg tablets are yellow, round, scored tablets debossed with A to the left of the score and Z to the right of the score on one side of the tablet and blank on the other side. They are available as follows: NDC 51079-620-06 – Unit dose blister packages of 50 (5 cards of 10 tablets each). Store at 20° to 25°C (68° to 77°F). [See USP Controlled Room Temperature.] Store in a dry place and protect from light.

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

AZATHIOPRINE- AZATHIOPRINE TABLET
MYLAN INSTITUTIONAL INC.
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WARNING - MALIGNANCY
CHRONIC IMMUNOSUPPRESSION WITH AZATHIOPRINE, 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
AZATHIOPRINE TABLETS. SEE
WARNINGS.
DESCRIPTION
Azathioprine, an immunosuppressive antimetabolite, is available in
tablet form for oral administration.
Each scored tablet contains 50 mg azathioprine, USP and the inactive
ingredients corn starch, lactose
monohydrate, magnesium stearate, povidone and stearic acid.
Azathioprine is chemically
6-[(1-Methyl-4-nitroimidazol-5-yl)thio]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 blood levels of azathioprine, and of mercaptopurine
derived