Rheumatoid arthritis that cannot be managed with NSAIDs.
At least as effective as methotrexate, and
more effective than sulfasalazine.
Inhibits dihydroorotate dehydrogenase (DHODH),
and hence uridine synthesis.
Clinical response in 40–65% of patients.
Slows the rate of bone erosion on X-ray.
Diarrhoea, vomiting, alopecia.
Raised AST, ALT. Anaemia, pancytopaenia esp. with methotrexate.
Quickly metabolised to A77 1726 (M1).
Half life of M1 is approx. 2 weeks, hence loading dose is necessary.
Renal impairment: A77 1726 (M1) levels higher, and M1 is not
Cholestyramine 8g tds for 11 days.