AZATHIOPRINE tablet

País: Estados Unidos

Língua: inglês

Origem: NLM (National Library of Medicine)

Ingredientes ativos:

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

Disponível em:

Avera McKennan Hospital

DCI (Denominação Comum Internacional):

AZATHIOPRINE

Composição:

AZATHIOPRINE 50

Tipo de prescrição:

PRESCRIPTION DRUG

Status de autorização:

Abbreviated New Drug Application

Características técnicas

AZATHIOPRINE- AZATHIOPRINE TABLET
AVERA MCKENNAN HOSPITAL
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AZATHIOPRINE TABLETS, USP
BOXED WARNING
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 is an immunosuppressive antimetabolite. Each uncoated
azathioprine tablet intended for
oral administration contains 50 mg of azathioprine. In addition, each
tablet contains the following
inactive ingredients: croscarmellose sodium, lactose monohydrate,
magnesium stearate, povidone and
starch.
Azathioprine is chemically
6-[(1-methyl-4-nitro-_1H_-imidazol-5-yl)thio]-_1H_-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, USP is a pale yellow, odorless powder. It is insoluble
in water, soluble in dilute
solutions of alkali hydroxides, sparingly soluble in dilute mineral
acids, very slightly soluble in alcohol
and in chloroform. The sodium salt of azathioprine is sufficiently
soluble to make a 10 mg/mL water
solution which is stable for 24 hours at 59° to 77°F (15° to
25°C). 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-azathiop