AZATHIOPRINE tablet

Land: USA

Språk: engelsk

Kilde: NLM (National Library of Medicine)

Aktiv ingrediens:

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

Tilgjengelig fra:

Cardinal Health

INN (International Name):

AZATHIOPRINE

Sammensetning:

AZATHIOPRINE 50 mg

Resept typen:

PRESCRIPTION DRUG

Autorisasjon status:

Abbreviated New Drug Application

Preparatomtale

AZATHIOPRINE- AZATHIOPRINE TABLET
CARDINAL HEALTH
----------
AZATHIOPRINE TABLETS USP, 50 MG
RX ONLY
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. 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 anhydrous lactose,
magnesium stearate, povidone, pregelatinized starch (corn starch), 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. 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 bl