Sowunmi Akintunde, Gbotosho Grace O, Happi Christian T, Adedeji Ahmed A, Bolaji Olayinka M, Fehintola Fatai A, Fateye Babasola A, Oduola Ayoade M J
Department of Pharmacology and Therapeutics, Institute for Medical Research and Training, University of Ibadan, Ibadan, Nigeria.
Mem Inst Oswaldo Cruz. 2007 Jun;102(3):417-9. doi: 10.1590/s0074-02762007005000038.
Resistance in Plasmodium falciparum to amodiaquine (AQ) can be reversed in vitro with with antihistaminic and tricyclic antidepressant compounds, but its significance in vivo is unclear. The present report presents the enhancement of the antimalarial efficacy of AQ by chlorpheniramine, an H1 receptor antagonist that reverses chloroquine (CQ) resistance in vitro and enhances its efficacy in vivo, in five children who failed CQ and/or AQ treatment, and who were subsequently retreated and cured with a combination of AQ plus CP, despite the fact that parasites infecting the children harboured mutant pfcrtT76 and pfmdr1Y86 alleles associated with AQ resistance. This suggests a potential clinical application of the reversal phenomenon.
恶性疟原虫对阿莫地喹（AQ）的耐药性在体外可被抗组胺药和三环类抗抑郁药逆转，但其在体内的意义尚不清楚。本报告介绍了氯苯那敏增强AQ抗疟疗效的情况。氯苯那敏是一种H1受体拮抗剂，在体外可逆转氯喹（CQ）耐药性并增强其体内疗效。5名CQ和/或AQ治疗失败的儿童随后接受了AQ加氯苯那敏联合治疗并治愈，尽管感染这些儿童的疟原虫携带与AQ耐药性相关的pfcrtT76和pfmdr1Y86突变等位基因。这表明这种逆转现象具有潜在的临床应用价值。
