Sulfasalazine

DescriptionSulfasalazine (brand name Azulfidine in the U.S., Salazopyrin and Sulazine in Europe and Hong Kong) was developed in the 1950s specifically to treat rheumatoid arthritis. It was believed at the time that bacterial infections were the cause of rheumatoid arthritis. Sulfasalazine is a sulfa drug, (a derivative of mesalazine) and is formed by combining sulfa pyridine and salicylate with an azo bond. It may be abbreviated SSZ.

UsesAnti-inflammatory (gastrointestinal). Has been used in granulomatous colitis.

Usesanticolitis and Crohn's disease

UsesSulfasalazine is an anti-inflammatory (gastrointestinal). Sulfasalazine has been used in granulomatous colitis.

UsesSulfasalazine is a prodrug of the anti-inflammatory agent 5-aminosalicylic acid that is covalently linked to the antibiotic sulfapyridine by an azo bond. This bond is rapidly cleaved by bacteria in the terminal ileum and colon, thus releasing the active anti-inflammatory component. It has long been used in treatment of inflammatory bowel disease and rheumatoid arthritis because of its ability to induce T lymphocyte apoptosis, modulate inflammatory mediators from both cyclooxygenase/5-lipoxygenase pathways and NF-κB signaling pathways, attenuate transcription of proinflammatory cytokines, and activate PPARγ.[Cayman Chemical]

UsesAn inhibitor of of GSH-H-transferase and NF-kB activation and an apoptosis inducer

General DescriptionOdorless yellow or brownish-yellow to orange powder. Tasteless.

General DescriptionSulfasalazine (Azufidine) is an azo prodrug that is reducedby the bacterium present in the lower intestine to its activemetabolites, sulfapyridine and 5-aminosalicylic acid (5-ASA or mesalamine). It has been used for the treatment ofRA or ankylosing spondylitis, and inflammatory bowel diseases(IBDs) such as ulcerative colitis and Crohn disease.It is generally agreed that the therapeutic effects of sulfasalazinein treating IBDs are due mainly through its activemetabolite, 5-ASA. 5-ASA is believed to work, via similarmechanisms of action to the salicylates discussed earlier, byblocking prostaglandin synthesis in the lower intestine. On the other hand, because 5-ASA is completelyionized and very little of this metabolite can enter into systemiccirculation, the antirheumatic effects of sulfasalazinehave been attributed to its other active metabolite, sulfapyridine. In a more recent study, sulfasalazine and sulfapyridinewere found to inhibit 5-aminoimidazole-4-carboxamideribonucleotide transformylase, an enzyme involved in denovo purine biosynthesis. Sulfasalazine also inhibits neutrophilfunction, reduces immunoglobulin levels, and interfereswith T-cell function via suppression of NF-κB activation. Furthermore, like methotrexate, sulfasalazine hasalso been shown to inhibit osteoclastogenesis, thereby preventingbone erosion in arthritic patients.It should be pointed out that approximately one third of thepatients treated long term with sulfasalazine discontinued thedrug because of dose-related adverse effects including nausea,dyspepsia, vomiting, headache, rash, gastric distress, especiallyin patients on a daily dosage of greater than 4 g (or aserum sulfapyridine levels above 50 mg/mL).