SULFASALAZINE tablet

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

SULFASALAZINE (UNII: 3XC8GUZ6CB) (SULFASALAZINE - UNII:3XC8GUZ6CB)

Available from:

Actavis Pharma, Inc.

INN (International Name):

SULFASALAZINE

Composition:

SULFASALAZINE 500 mg

Administration route:

ORAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Sulfasalazine tablets are indicated: a) in the treatment of mild to moderate ulcerative colitis, and as adjunctive therapy in severe ulcerative colitis; and b) for the prolongation of the remission period between acute attacks of ulcerative colitis. Sulfasalazine tablets are contraindicated in: Patients with intestinal or urinary obstruction, Patients with porphyria as sulfonamides have been reported to precipitate an acute attack, Patients hypersensitive to sulfasalazine, its metabolites, sulfonamides, or salicylates. None reported.

Product summary:

Sulfasalazine tablets USP, 500 mg are round, mustard-colored, biconvex, debossed “WATSON ” and “796 ” on one side and partial bisect on the other side. They are available in the following package sizes: Bottles of 100              NDC 0591-0796-01 Bottles of 500              NDC 0591-0796-05 Bottles of 1000            NDC 0591-0796-10 Store at 20° to 25°C (68° to 77°F) [See USP Controlled Room Temperature].

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

SULFASALAZINE- SULFASALAZINE TABLET
ACTAVIS PHARMA, INC.
----------
SULFASALAZINE TABLETS, USP
RX ONLY
DESCRIPTION
Sulfasalazine tablets USP, 500 mg for oral administration.
THERAPEUTIC CLASSIFICATION: Anti-inflammatory agent.
CHEMICAL DESIGNATION: 5-([_p_-(2-pyridylsulfamoyl)phenyl]azo)
salicylic acid.
CHEMICAL STRUCTURE:
C
H
N O S
The molecular weight of sulfasalazine is 398.39.
INACTIVE INGREDIENTS: magnesium stearate, pregelatinized corn starch,
sodium starch
glycolate and stearic acid.
CLINICAL PHARMACOLOGY
PHARMACODYNAMICS
The mode of action of sulfasalazine (SSZ) or its metabolites,
5-aminosalicylic acid (5-
ASA) and sulfapyridine (SP), may be related to the anti-inflammatory
and/or
immunomodulatory properties that have been observed in animal and _in
vitro _models, to
its affinity for connective tissue, and/or to the relatively high
concentration it reaches in
serous fluids, the liver and intestinal walls, as demonstrated in
autoradiographic studies
in animals. In ulcerative colitis, clinical studies utilizing rectal
administration of SSZ, SP,
and 5-ASA have indicated that the major therapeutic action may reside
in the 5-ASA
moiety.
PHARMACOKINETICS
_In vivo _studies have indicated that the absolute bioavailability of
orally administered SSZ
is less than 15% for parent drug. In the intestine, SSZ is metabolized
by intestinal
18
14
4
5
bacteria to SP and 5-ASA. Of the two species, SP is relatively well
absorbed from the
intestine and highly metabolized, while 5-ASA is much less well
absorbed.
Absorption:
Following oral administration of 1 g of SSZ to 9 healthy males, less
than 15% of a dose
of SSZ is absorbed as parent drug. Detectable serum concentrations of
SSZ have been
found in healthy subjects within 90 minutes after the ingestion.
Maximum concentrations
of SSZ occur between 3 and 12 hours post-ingestion, with the mean peak
concentration
(6 mcg/mL) occurring at 6 hours.
In comparison, peak plasma levels of both SP and 5-ASA occur
approximately 10 hours
after dosing. This longer time to peak is indicat