作者: Joseph George
DOI: 10.1016/J.BCP.2020.113993
关键词: CYP3A4 、 Acedapsone 、 Pharmacology 、 Leprosy 、 Dapsone 、 Rifampicin 、 Clofazimine 、 Drug metabolism 、 Medicine 、 Mycobacterium leprae
摘要: Abstract Leprosy is a chronic infectious disease caused my Mycobacterium leprae that primarily affects peripheral nervous system and extremities prevalent in tropical countries. Treatment for leprosy with multidrug regimens very effective compared to monotherapy especially multibacillary cases. The three major antileprosy drugs currently use are 4, 4′-diaminodiphenyl sulfone (DDS, dapsone), rifampicin, clofazimine. During therapy, the potent antibiotic rifampicin induces metabolism of dapsone, which results decreased plasma half-life dapsone its metabolites. Furthermore, own decreases during monotherapy. Rifampicin upregulates several hepatic microsomal drug-metabolizing enzymes, cytochrome P450 (CYP) family turn induce dapsone. Clofazimine lacks significant induction any enzyme including CYP does not interact metabolism. clofazimine combination treatment. Administration acetylated form (acedapsone) can release drug slowly into circulation up 75 days could be useful treatment paucibacillary cases along rifampicin. This review summarizes aspects interactions role metabolizing CYP3A4 leprosy.