Loading dose of leflunomide in rheumatoid ahritis is:
High-Yield Explanation
This immunomodulator inhibits proliferation of activated lymphocytes inpatients with active RA. Ahritic symptoms are suppressed and radiological progression of disease is retarded. In clinical trials its efficacy has been rated comparable to Mtx and onset of benefit is as fast (4 weeks). Leflunomide is rapidiy conveed in the body to an active metaboilite which inhibits dihydroorotate dehydrogenase d pyrimidine synthesis in actively dividing cells. Antibody production by B-cells may be depressed. The active metabolite has a long t1/2o f 2 weeks; leflunomide, therefore, is given in a loading dose of 100 mg dailv for 3 days followedby20 mg OD. ESSENTIALS OF MEDICAL PHARMACOLOGY;7TH EDITION;KD TRIPATHI;PAGE NO 212