|Trade names||Azulfidine, Salazopyrin, Sulazine, others|
|Elimination half-life||5-10 hours|
|Chemical and physical data|
|Molar mass||398.394 g/mol|
|3D model (JSmol)|
|(what is this?)|
Sulfasalazine (SSZ), sold under the trade name Azulfidine among others, is a medication used to treat rheumatoid arthritis, ulcerative colitis, and Crohn's disease. It is often considered as a first line treatment in rheumatoid arthritis. It is taken by mouth.
Significant side effects occur in about 25% of people. Commonly these include loss of appetite, nausea, headache, and rash. Severe side effects include bone marrow suppression, liver problems, and kidney problems. It should not be used in people allergic to aspirin or sulfonamide. Use during pregnancy appears to be safe for the baby. Sulfasalazine is in the disease-modifying antirheumatic drugs (DMARDs) family of medications. It is unclear exactly how it works but is broken down into sulfapyridine and 5-aminosalicylic acid.
Sulfasalazine was approved for medical use in the United States in 1950. It is on the World Health Organization's List of Essential Medicines, the most effective and safe medicines needed in a health system. Sulfasalazine is available as a generic medication. The wholesale cost in the developing world is about US$9–33 a month. In the United States it costs $25–50 per month.
Sulfasalazine is used in the treatment of inflammatory bowel disease, including ulcerative colitis and Crohn's disease. It is also indicated for use in rheumatoid arthritis and used in other types of inflammatory arthritis (e.g. psoriatic arthritis and reactive arthritis).
It is usually not given to children under 2 years of age.
Sulfasalazine metabolizes to sulfapyridine. Serum levels should be monitored every three months, and more frequently at the outset. Serum levels above 50 μg/l are associated with side effects. In rare cases, Sulfasalazine can cause severe depression in young males. It can also cause oligospermia and temporary infertility. Immune thrombocytopenia has been reported.
Around 90% of a dose of sulfasalazine reaches the colon, where most of it is metabolized by bacteria into sulfapyridine and mesalazine (also known as 5-aminosalicylic acid or 5-ASA). Both metabolites are active; most of the sulfapyridine is absorbed and then further metabolized, but most mesalazine is not, and remains in the colon.
A mix of unchanged, hydroxylated, and glucuronidated sulfapyridine is eliminated in urine, as is acetylated mesalazine and unmetabolized sulfasalazine.
The mechanism of action is not clear, but it appears that sulfasalazine and its metabolites have immunosuppressive, antibacterial, and anti-inflammatory effects. It also appears to inhibit the cystine-glutamate antiporter.
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