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Sulfasalazine

 

A medication used to treat rheumatoid arthritis, ulcerative colitis, and Crohn’s disease.

 

 

Trade name Azulfidine.

 

 

It is an oral agent.

 

 

US: B (No risk in non-human studies) 

 

 

Sulfonamide

 

 

Bioavailability <15%

 

 

Elimination half-life 5-10 hours

 

 

Side effects occur in about 25% of people.

 

 

Common side effects include loss of appetite, nausea, headache, and rash.

 

 

Severe side effects include bone marrow suppression, liver problems, Stevens–Johnson syndrome, and kidney impairment.

 

 

The drug should not be used in people allergic to aspirin or sulfonamide.

 

 

Use during pregnancy appears to be safe.

 

 

It is characterized as adisease-modifying antirheumatic drugs (DMARDs) family of medications.

 

 

A proposed mechanism for bowel disease is the inhibition of prostaglandins, resulting in local anti-inflammatory effects in the colon.

 

 

It  is broken down by intestinal bacteria into sulfapyridine and 5-aminosalicylic acid.

 

 

It is used in the treatment of inflammatory bowel disease, including ulcerative colitis and Crohn’s disease, rheumatoid arthritis and used in other types of inflammatory arthritis.

 

 

It is usually not given to children under two years of age.

 

 

Contraindicated in people with sulfa allergies and in those with urinary tract obstructions, intestinal obstructions, and severe liver or kidney problems.

 

 

Serum levels should be monitored every three months, and more frequently at the outset: levels above 50 μg/l are associated with side effects. 

 

 

In rare cases it can cause severe depression in young males. 

 

 

It can also cause oligospermia temporary infertility. 

 

 

Immune thrombocytopenia has been reported.

 

 

It inhibits dihydropteroate synthase, and can cause folate deficiency and megaloblastic anemia.

 

 

It  can cause hemolytic anemia in people with G6PD deficiency.

 

 

Side effects include: stomach upset, nausea, vomiting, loss of appetite, headache, dizziness, or unusual tiredness.

 

 

Skin and urine can become orange in color.

 

 

Sulfasalazine may cause sulfhemoglobinemia.

 

 

Approximately 90% of a dose reaches the colon, where most of it is metabolized by bacteria into sulfapyridine and 5-aminosalicylic acid.

 

 

Sulfasalazine and its metabolites have immunosuppressive, antibacterial, and anti-inflammatory effects.

 

 

 

 

 

 

 

 

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