AZATHIOPRINE tablet

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

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

Available from:

Oceanside Pharmaceuticals

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. Renal Homotransplantation: 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. Rheumatoid Arthritis: 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 benefit or unexpected adverse effects. The use of Azathioprine Tablets with these agents cannot be recommended. Azathioprine Tablets should not be given to patients who have shown hypersensitivity to the drug. Azathioprine Tablets should not be used for treating rheumatoid arthritis in pregnant women. Patients with rheumatoid arthritis previously treated with alkylating agents (cyclophosphamide, chlorambucil, melphalan, or others) may have a prohibitive risk of malignancy if treated with Azathioprine Tablets.

Product summary:

Azathioprine Tablets, USP are available in: 75 mg, triangle-shaped, yellow, scored tablets, 100 count bottles (NDC 68682-231-01) 100 mg, diamond-shaped, yellow, scored tablets, 100 count bottles (NDC 68682-241-01) Store at 20° to 25°C (68° to 77°F) [See USP Controlled Room Temperature]. Store in a dry place and protect from light. Dispense in a tight, light-resistant container as defined in the USP.

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

AZATHIOPRINE- AZATHIOPRINE TABLET
OCEANSIDE PHARMACEUTICALS
----------
AZATHIOPRINE TABLETS, USP 75MG AND 100MG
WARNING - MALIGNANCY Chronic immunosuppression with this 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 75 mg or 100 mg
azathioprine and the
inactive ingredients lactose monohydrate, pregelatinized starch,
povidone, corn starch,
magnesium stearate, and stearic acid.
Azathioprine is chemically 1 _H_-purine, 6-[(1-methyl-4-nitro-1
_H_-imidazol-5-yl)thio]-. 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.
35
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. Us