Chanthavanich P, Looareesuwan S, White N J, Warrell D A, Warrell M J, DiGiovanni J H, von Bredow J
Am J Trop Med Hyg. 1985 Nov;34(6):1028-36. doi: 10.4269/ajtmh.1985.34.1028.
Mefloquine has proved effective in chloroquine- and quinine-resistant falciparum malaria, but it cannot be given parenterally. We have measured the absorption of mefloquine hydrochloride suspension (mean 15.6, range 9.7-28.6 mg/kg) given by nasogastric tube to 19 cerebral malaria patients already receiving intravenous quinine. Absorption was rapid with both dose schedules used; mean absorption half-times were 1.5 and 1.8 hr, and plasma mefloquine concentrations exceeded 200 ng/g within 3 hr of completing administration in all but one exceptionally ill patient who died 40 hr later. Steady state plasma concentrations over 7 days ranged from 300 to 1,050 (mean 561) ng/g. Bioavailability of mefloquine suspension in cerebral malaria therefore appears to be adequate for treatment in all but the most severely ill patients. Although intragastric mefloquine cannot now be recommended as an alternative to intravenous quinine for the treatment of severe chloroquine-resistant falciparum malaria, this situation could change if quinine resistance increases further.
甲氟喹已被证明对氯喹和奎宁耐药的恶性疟有效，但不能胃肠外给药。我们测定了通过鼻胃管给予19例已接受静脉注射奎宁的脑型疟患者盐酸甲氟喹混悬液（平均15.6mg/kg，范围9.7 - 28.6mg/kg）后的吸收情况。所采用的两种剂量方案吸收均迅速；平均吸收半衰期分别为1.5小时和1.8小时，除1例病情极重的患者在给药后40小时死亡外，所有患者在给药结束后3小时内血浆甲氟喹浓度均超过200ng/g。7天的稳态血浆浓度范围为300至1050（平均561）ng/g。因此，除病情最重的患者外，甲氟喹混悬液在脑型疟中的生物利用度似乎足以用于治疗。虽然目前不能推荐胃内给予甲氟喹替代静脉注射奎宁来治疗严重的氯喹耐药恶性疟，但如果奎宁耐药性进一步增加，这种情况可能会改变。
