Benzosulfa: Full Drug Profile

Benzosulfa - General Information

A drug that is used in the management of inflammatory bowel diseases. Its activity is generally considered to lie in its metabolic breakdown product, 5-aminosalicylic acid (see mesalamine) released in the colon. (From Martindale, The Extra Pharmacopoeia, 30th ed, p907)

Pharmacology of Benzosulfa

Benzosulfa is an anti-inflammatory indicated for the treatment of ulcerative colitis and rheumatoid arthritis.

Benzosulfa for patients

Benzosulfa Interactions

Reduced absorption of folic acid and digoxin have been reported when those agents were administered concomitantly with sulfasalazine.

When daily doses of sulfasalazine 2 g and weekly doses of methotrexate 7.5 mg were coadministered to 15 rheumatoid arthritis patients in a drug-drug interaction study, the pharmacokinetic disposition of the drugs was not altered.

Daily doses of sulfasalazine 2 g (maximum 3 g) and weekly doses of methotrexate 7.5 mg (maximum 15 mg) were administered alone or in combination to 310 rheumatoid arthritis patients in two controlled 52-week clinical studies. The overall toxicity profile of the combination revealed an increased incidence of gastrointestinal adverse events, especially nausea, when compared to the incidence associated with either drug administered alone.

Drug/Laboratory Test Interactions: The presence of sulfasalazine or its metabolites in body fluids has not been reported to interfere with laboratory test procedures.

REFERENCES

7.Farr M, et al. Immunodeficiencies associated with sulphasalazine therapy in inflammatory arthritis. British Jnl Rheum 1991;30:413-417.

Benzosulfa Contraindications

AZULFIDINE EN-tabs Tablets are contraindicated in:

Hypersensitivity to sulfasalazine, its metabolites, sulfonamides or salicylates,

Patients with intestinal or urinary obstruction,

Patients with porphyria, as the sulfonamides have been reported to precipitate an acute attack.

Additional information about Benzosulfa

Benzosulfa Indication

For the treatment of Crohn's disease and rheumatoid arthritis as a second-line agent.

Mechanism Of Action

The mode of action of Benzosulfa 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 Benzosulfa, SP and 5-ASA have indicated that the major therapeutic action may reside in the 5-ASA moiety. The relative contribution of the parent drug and the major metabolites in rheumatoid arthritis is unknown.

Food Interactions

Take with food.

Generic Name

Sulfasalazine

Synonyms

Sulphasalazine; Sulfasalazin

Drug Category

Antirheumatic Agents; Gastrointestinal Agents; Sulfonamides; Anti-Infective Agents; Anti-Inflammatory Agents, Non-Steroidal

Drug Type

Small Molecule; Approved

Other Brand Names containing Sulfasalazine

Accucol; Alti-Sulfasalazine; Asulfidine; Azlufidine EN-Tabs; Azopyrin; Azopyrine; Azulfidine; Azulfidine EN-Tabs; Benzosulfa; Colo-Pleon; PMS-Sulfasalazine; Pms-Sulfasalazine E.C.; Reupirin; Rorasul; S.A.S. Enteric-500; Salazopiridazin; Salazopyridin; Salazopyrin; Salazopyrin EN-Tabs; Salazosulfapyridin; Salazosulfapyridine; Salicylazosulfapyridine; Salisulf; Sulcolon; W-T Sasp Oral;

Half Life

5-10 hours

Dosage Forms of Benzosulfa

Tablet Oral

Chemical IUPAC Name

(3E)-6-oxo-3-[[4-(pyridin-2-ylsulfamoyl)phenyl]hydrazinylidene]cyclohexa-1,4-diene-1-carboxylic acid

Chemical Formula

C18H14N4O5S

Sulfasalazine on Wikipedia

https://en.wikipedia.org/wiki/Sulfasalazine

Organisms Affected

Humans and other mammals