SULFASALAZINE tablet

Страна: США

мова: англійська

Джерело: NLM (National Library of Medicine)

Активний інгредієнт:

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

Доступна з:

Major Pharmaceuticals

ІПН (Міжнародна Ім'я):

SULFASALAZINE

Склад:

SULFASALAZINE 500 mg

Тип рецепту:

PRESCRIPTION DRUG

Статус Авторизація:

New Drug Application Authorized Generic

Характеристики продукта

SULFASALAZINE- SULFASALAZINE TABLET
MAJOR PHARMACEUTICALS
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SULFASALAZINE TABLETS, USP
DESCRIPTION
Sulfasalazine tablets contain sulfasalazine, 500 mg, for oral
administration.
THERAPEUTIC CLASSIFICATION: Anti-inflammatory agent.
CHEMICAL DESIGNATION: 5-([p-(2-pyridylsulfamoyl)phenyl]azo) salicylic
acid.
CHEMICAL STRUCTURE:
MOLECULAR FORMULA: C
H N O S
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 μg/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 indicative of gastrointestinal transit to
the lower intestine where bacteria
mediated metabolism occurs. SP apparently is