SULFASALAZINE- sulfasalazine tablet

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

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

Available from:

Par Pharmaceutical

INN (International Name):

SULFASALAZINE

Composition:

SULFASALAZINE 500 mg

Administration route:

ORAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Sulfasalazine tablets, USP are indicated: - in the treatment of mild to moderate ulcerative colitis, and as adjunctive therapy in severe ulcerative colitis; and - 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, gold-colored, scored tablets, debossed "5904" and "V" on one side and plain on the reverse side. They are available in the following package sizes: 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
PAR PHARMACEUTICAL
----------
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.
STRUCTURAL FORMULA:
INACTIVE INGREDIENTS:
corn starch, croscarmellose sodium, magnesium stearate,
microcrystalline cellulose, povidone,
pregelatinized starch, and talc.
CLINICAL PHARMACOLOGY
PHARMACODYNAMICS
The mode of action of sulfasalazine (SSZ) or its metabolites,
5-aminosalicylic acid (5-ASA) and
sulfapyridine (SP), is still under investigation, but 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 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 indica