AZATHIOPRINE tablet

Land: Bandaríkin

Tungumál: enska

Heimild: NLM (National Library of Medicine)

Virkt innihaldsefni:

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

Fáanlegur frá:

Aphena Pharma Solutions - Tennessee, LLC

INN (Alþjóðlegt nafn):

AZATHIOPRINE

Samsetning:

AZATHIOPRINE 50 mg

Gerð lyfseðils:

PRESCRIPTION DRUG

Leyfisstaða:

Abbreviated New Drug Application

Vara einkenni

AZATHIOPRINE- AZATHIOPRINE TABLET
APHENA PHARMA SOLUTIONS - TENNESSEE, LLC
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AZATHIOPRINE TABLETS USP, 50 MG
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
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
d