Fight rheumatoid arthritis with leflunomide
by Nathan Wei, MD, FACP, FACR
Nathan Wei is a nationally known board-certified rheumatologist and author of the Second Opinion Arthritis Treatment Kit. It's available exclusively at this website... not available in stores.
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Leflunomide (Arava) is an immunomodulatory drug structurally unrelated to other drugs in its class. It is considered a disease-modifying anti-rheumatic drug (DMARD).
Information from the Arava website
Its mechanism is prevention of proliferation of T cells as well as inhibition of antibody production by B cells. Leflunomide preferentially selects autoimmune lymphocytes.
Leflunomide induces apoptosis (programmed cell death) in these activated lymphocytes.
The drug is well absorbed orally.
A loading dose of 100 mgs per day is taken for the first three days, and then a 20 mg per day maintenance dose is taken.
Potential side effects include rash, abdominal pain, cramps, diarrhea, weight loss, and hair fall. The hair fall is reversible. Hypertension occurs in some patients.
Elevation of liver function tests may occur and there have been reports of deaths in patients taking leflunomide. Leflunomide should be avoided in patients with compromised liver function or who have a history of hepatitis.
Finally, leflunomide is terrible teratogenic and should not be used in patients who are employing adequate contraceptive methods.
Leflunomide is eliminated slowly from the body. In order to get rid of leflunomide faster, it is necessary to use cholestyramine in a dose of 8 grams three times a day for eleven days to achieve undetectable blood levels of leflunomide.
Rapid reduction of blood levels can also be achieved with the use of activated charcoal administered as a oral slurry (50 grams every 6 hours for 24 hours.) This, as with the cholestyramine, can be repeated if necessary.
There does not appear to be an increased risk of infection in patients taking leflunomide.
Laboratory monitoring is similar to that for methotrexate. Complete blood count, liver and kidney function as well a urinalysis should be obtained at monthly intervals.
This is a drug that is not commonly used; however, it has a niche in that it is a useful DMARD for patients who can't tolerate methotrexate.
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