Sulfasalazine Information
Sulfasalazine () Description
Sulfasalazine () Tablets, USP, 500 mg for oral administration.
CHNOS
The molecular weight of Sulfasalazine () is 398.39.
Sulfasalazine () Indications And Usage
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 () Contraindications
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.
Sulfasalazine () Warnings
Only after critical appraisal should Sulfasalazine () tablets be given to patients with hepatic or renal damage or blood dyscrasias. Deaths associated with the administration of Sulfasalazine () have been reported from hypersensitivity reactions, agranulocytosis, aplastic anemia, other blood dyscrasias, renal and liver damage, irreversible neuromuscular and central nervous system changes, and fibrosing alveolitis. The presence of clinical signs such as sore throat, fever, pallor, purpura, or jaundice may be indications of serious blood disorders or hepatotoxicity. Complete blood counts, as well as urinalysis with careful microscopic examination, should be done frequently in patients receiving Sulfasalazine () (see ). Discontinue treatment with Sulfasalazine () while awaiting the results of blood tests. Oligospermia and infertility have been observed in men treated with Sulfasalazine () ; however, withdrawal of the drug appears to reverse these effects.
Sulfasalazine () Precautions
Complete blood counts, including differential white cell count and liver function tests, should be performed before starting Sulfasalazine () and every second week during the first three months of therapy. During the second three months, the same tests should be done once monthly and thereafter once every three months, and as clinically indicated. Urinalysis and an assessment of renal function should also be done periodically during treatment with Sulfasalazine () .
The determination of serum sulfapyridine levels may be useful since concentrations greater than 50 mcg/mL appear to be associated with an increased incidence of adverse reactions.
Two-year oral carcinogenicity studies were conducted in male and female F344/N rats and B6C3F1 mice. Sulfasalazine () was tested at 84 (496 mg/m²), 168 (991 mg/m²), and 337.5 (1991 mg/m²) mg/kg/day doses in rats. A statistically significant increase in the incidence of urinary bladder transitional cell papillomas was observed in male rats. In female rats, two (4%) of the 337.5 mg/kg rats had transitional cell papilloma of the kidney. The increased incidence of neoplasms in the urinary bladder and kidney of rats was also associated with an increase in the renal calculi formation and hyperplasia of transitional cell epithelium. For the mouse study, Sulfasalazine () was tested at 675 (2025 mg/m²), 1350 (4050 mg/m²), and 2700 (8100 mg/m²) mg/kg/day. The incidence of hepatocellular adenoma or carcinoma in male and female mice was significantly greater than the control at all doses tested.
Sulfasalazine () did not show mutagenicity in the bacterial reverse mutation assay (Ames test) and in L51784 mouse lymphoma cell assay at the HGPRT gene. However, Sulfasalazine () showed equivocal mutagenic response in the micronucleus assay of mouse and rat bone marrow and mouse peripheral RBC and in the sister chromatid exchange, chromosomal aberration, and micronucleus assays in lymphocytes obtained from humans.
Impairment of male fertility was observed in reproductive studies performed in rats at a dose of 800 mg/kg/day (4800 mg/m²). Oligospermia and infertility have been described in men treated with Sulfasalazine () . Withdrawal of the drug appears to reverse these effects.
Sulfasalazine () Adverse Reactions
The most common adverse reactions associated with Sulfasalazine () are anorexia, headache, nausea, vomiting, gastric distress, and apparently reversible oligospermia. These occur in about one-third of the patients. Less frequent adverse reactions are skin rash, pruritus, urticaria, fever, Heinz body anemia, hemolytic anemia, and cyanosis, which may occur at a frequency of one in every thirty patients or less. Experience suggests that with a daily dosage of 4 g or more, or total serum sulfapyridine levels above 50 mcg/mL, the incidence of adverse reactions tends to increase. Although the listing which follows includes a few adverse reactions which have not been reported with this specific drug, the pharmacological similarities among the sulfonamides require that each of these reactions be considered when Sulfasalazine () tablets are administered. Less common or rare adverse reactions include:
The sulfonamides bear certain chemical similarities to some goitrogens, diuretics (acetazolamide and the thiazides), and oral hypoglycemic agents. Goiter production, diuresis and hypoglycemia have occurred rarely in patients receiving sulfonamides. Cross-sensitivity may exist with these agents. Rats appear to be especially susceptible to the goitrogenic effects of sulfonamides and long-term administration has produced thyroid malignancies in this species.
Sulfasalazine () Drug Abuse And Dependence
Sulfasalazine () Overdosage
There is evidence that the incidence and severity of toxicity following overdosage are directly related to the total serum sulfapyridine concentration. Symptoms of overdosage may include nausea, vomiting, gastric distress, and abdominal pains. In more advanced cases, central nervous system symptoms such as drowsiness, convulsions, etc., may be observed. Serum sulfapyridine concentrations may be used to monitor the progress of recovery from overdosage.
There are no documented reports of deaths due to ingestion of large single doses of Sulfasalazine () . Doses of Sulfasalazine () tablets of 16 g per day have been given to patients without mortality. A single oral dose of 12 g/kg was not lethal to mice.
Sulfasalazine () Dosage And Administration
The dosage of Sulfasalazine () tablets should be adjusted to each individual’s response and tolerance.
Sulfasalazine () How Supplied
Sulfasalazine () Tablets, USP, 500 mg are round, mustard-colored, biconvex, imprinted and on one side and partial bisect on the other side. They are available in the following package sizes: Bottles of 100 NDC 0591-0796-01Bottles of 500 NDC 0591-0796-05Bottles of 1000 NDC 0591-0796-10 Store at 20°-25°C (68°-77°F). [See USP Controlled Room Temperature].
Sulfasalazine () References
1. Mogadam M, et al. Pregnancy in inflammatory bowel disease: effect of Sulfasalazine () and corticosteroids on fetal outcome. Gastroenterology 1981;80:72-6.
2. Kaufman DW, editor. Birth defects and drugs during pregnancy. Littleton, MA: Publishing Sciences Group, Inc, 1977;296-313.
3. Jarnerot G. Fertility, sterility and pregnancy in chronic inflammatory bowel disease. Scand J Gastroenterol 1982;17:1-4.
4. Korelitz B, et al. Desensitization to Sulfasalazine () in allergic patients with IBD: an important therapeutic modality. Gastroenterology 1982;82:1104.
5. Holdworth CG. Sulphasalazine desensitization. Br Med J 1981;282:110.
6. Taffet SL, Das KM. Desensitization of patients with inflammatory bowel disease to Sulfasalazine () . Am J Med 1982;73:520-4.
Revised: May 2010 70021440
Sulfasalazine () Principal Display Panel
0591-0796-01Sulfasalazine () Tablets USP500 mgWatson 100 Tablets Rx only Sulfasalazine () USP, 500 mg
