AZATHIOPRINE SODIUM injection, powder, lyophilized, for solution

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

AZATHIOPRINE SODIUM (UNII: AM94R510MS) (AZATHIOPRINE - UNII:MRK240IY2L)

Available from:

Hikma Pharmaceuticals USA Inc.

INN (International Name):

AZATHIOPRINE SODIUM

Composition:

AZATHIOPRINE 100 mg in 10 mL

Administration route:

INTRAVENOUS

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Azathioprine Sodium for Injection, USP is 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 is indicated as an adjunct for the prevention of rejection in renal homotransplantation. Experience with over 16,000 transplants shows a five-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 on these variables has not been tested in controlled trials. Azathioprine is 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. The combined use of azathioprine with disease modifying anti-rheumatic drugs (DMARDs) has not been studied for either added benefit or unexpected ad

Product summary:

Azathioprine Sodium for Injection, USP, is supplied in a 20 mL vial, each containing azathioprine sodium, equivalent to 100 mg azathioprine. NDC 0143-9566-01. Store at 20° to 25°C (68° to 77°F) [See USP Controlled Room Temperature]. Protect from light. Retain in carton until time of use. The sterile, lyophilized sodium salt is yellow, and should be dissolved in Sterile Water for Injection (see DOSAGE AND ADMINISTRATION: Parenteral Administration ). To report SUSPECTED ADVERSE REACTIONS, contact Hikma Pharmaceuticals USA Inc. at 1-877-845-0689, or the FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. For Product Inquiry call 1-877-845-0689.

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

AZATHIOPRINE SODIUM- AZATHIOPRINE SODIUM INJECTION, POWDER,
LYOPHILIZED,
FOR SOLUTION
HIKMA PHARMACEUTICALS USA INC.
----------
AZATHIOPRINE SODIUM
FOR INJECTION, USP
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 Sodium for Injection, USP is a sterile lyophilized
material, which when
reconstituted with Sterile Water for Injection yields a solution for
intravenous
administration. Each vial contains azathioprine sodium equivalent to
100 mg
azathioprine, an immunosuppressive antimetabolite. Each vial also
contains sodium
hydroxide and, if necessary, hydrochloric acid to adjust the pH.
Azathioprine is chemically
6-[(1-methyl-4-nitroimidazol-5-yl)thio]purine. The structural
formula of azathioprine sodium is:
Molecular Formula: C H N O SNa Molecular Weight: 300.28
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. 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 administra