Pharmacology.
Leflunomide’s active metabolite (M1) inhibits dihydro-oratate dehydrogenase, thereby inhibiting pyrimidine biosynthesis. M1 exhibits immunomodulating and anti-inflammatory effects.
Administration and Adult Dosage.
PO for rheumatoid arthritis 100 mg/day for 3 days, then 20 mg/day. Reduce dose to 10 mg if 20 mg is not tolerated.
Pediatric Dosage.
Safety and efficacy not established.
Geriatric Dosage.
Same as adult dosage.
Dosage Forms.
Pharmacology.
Cyclophosphamide is inactive in vitro and must be enzymatically activated in the liver to yield active alkylating compounds and toxic metabolites. Cell-cycle phase nonspecific.
Administration and Adult Dosage.
IV or PO alone or in combination regimens 250-500 mg/m2 q 3-4 weeks. IV (usually) or PO in high-dose intermittent regimens (including bone marrow transplant) maximum of 40-50 mg/kg given once or over 2-5 days, repeat q 2-4 weeks-these doses are not well tolerated orally.
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