Randrianarivelojosia M, Harisoa J L Sahondra, Rabarijaona L P, Raharimalala L A, Ranaivo L, Pietra V, Duchemin J B, Rakotomanana F, Robert V, Mauclere P, Ariey F
Groupe de Recherche sur le Paludisme, Institut Pasteur de Madagascar, BP 1274, Antananarivo 101, République de Madagascar.
Parassitologia. 2002 Dec;44(3-4):141-7.
Chloroquine has been used in Madagascar since 1945 and remains the first-line treatment for uncomplicated cases of malaria. Low-grades of resistance type R1 and R2 have been reported. Thus, in vitro tests were performed in order to monitor the drug sensitivity of Plasmodium falciparum from different study sites, with the aim of identifying alternatives to chloroquine. Chloroquine IC50 values ranged from 0.2 nM to 283.4 nM (n = 190, mean IC50 = 52.6 nM; 95% CI = 46.1-59.1 nM). Fifteen isolates (7.9%) were chloroquine-resistant. One mefloquine-resistant isolate was detected (1/139). The test isolates were sensitive to amodiaquine (n = 118), quinine (n = 212), pyrimethamine (n = 86) and cycloguanil (n = 79). The median IC50 for amodiaquine was 12.3 nM (mean IC50 = 15.3 nM, 95% CI = 13.3-17.3 nM). Amodiaquine was 3.4 times as active as chloroquine in vitro and 7 times as active as quinine against P. falciparum. These results indicate that amodiaquine may be a potent alternative to chloroquine in Madagascar. There was positive correlation between tested quinoline-containing drugs activities, which suggests in vitro cross-susceptibility.
自1945年以来，氯喹一直在马达加斯加使用，仍然是无并发症疟疾病例的一线治疗药物。已有低水平R1和R2耐药类型的报告。因此，进行了体外试验以监测来自不同研究地点的恶性疟原虫的药物敏感性，目的是确定氯喹的替代药物。氯喹的IC50值范围为0.2 nM至283.4 nM（n = 190，平均IC50 = 52.6 nM；95%置信区间 = 46.1 - 59.1 nM）。15株分离株（7.9%）对氯喹耐药。检测到1株对甲氟喹耐药的分离株（1/139）。受试分离株对阿莫地喹（n = 118）、奎宁（n = 212）、乙胺嘧啶（n = 86）和环氯胍（n = 79）敏感。阿莫地喹的中位IC50为12.3 nM（平均IC50 = 15.3 nM，95%置信区间 = 13.3 - 17.3 nM）。在体外，阿莫地喹对恶性疟原虫的活性是氯喹的3.4倍，是奎宁的7倍。这些结果表明，在马达加斯加，阿莫地喹可能是氯喹的有效替代药物。受试含喹啉类药物的活性之间存在正相关，这表明存在体外交叉敏感性。
