Leflunomide Pharmacology

Leflunomide is an isoxazole derivative first isolated and described nearly 20 years ago. Leflunomide is a prodrug that is converted nonenzymatically, primarily in the intestinal mucosa and plasma, but also by the liver, to the active metabolite malononitrilamide, termed A77 1726 (68). A77 1726 has a long half-life of approximately two weeks. Treatment with oral leflunomide is initiated with a loading dose of 100 mg once daily for three days and continued at a dose of 10-20 mg once daily. In placebo-controlled trials, leflunomide is superior to placebo in improving signs and symptoms of RA and is comparable with sulfasalazine and MTX in terms of clinical response rate (9,11,69). It is also comparable to MTX (9) and sulfasalazine (11) for reducing the rate of radiographic progression of RA. The overall withdrawal rates in clinical trials are approximately 28%, and these are mostly due to adverse effects including diarrhea, nausea, rash, elevated liver transamin-ases, and alopecia (9,11,69). To date, there are no studies looking at the pharmacogenetics of this agent in humans. There are however, several potential pathways in which genetic variability may exert an influence.

100 Hair Growth Tips

100 Hair Growth Tips

100 Hair Growth Tips EVERY Balding Person Should Know. This Report

Get My Free Ebook


Post a comment