朱定球, 戴祖瑞, 李进才, 蒋增康. 长效抗疟药—喹哌防治鼠疟的实验研究J. 药学学报, 1982, 17(12): 894-898.
引用本文: 朱定球, 戴祖瑞, 李进才, 蒋增康. 长效抗疟药—喹哌防治鼠疟的实验研究J. 药学学报, 1982, 17(12): 894-898.
ZHU Ding-qiu, DAI Zu-rui, LI Jin-cai , JIANG Zeng-kang, . STUDIES ON PIPERAQUINE AS LONG-ACTING ANTIMALARIAL DRUG AGAINST PLASMODIUM BERGHEI IN MICEJ. Acta Pharmaceutica Sinica, 1982, 17(12): 894-898.
Citation: ZHU Ding-qiu, DAI Zu-rui, LI Jin-cai , JIANG Zeng-kang, . STUDIES ON PIPERAQUINE AS LONG-ACTING ANTIMALARIAL DRUG AGAINST PLASMODIUM BERGHEI IN MICEJ. Acta Pharmaceutica Sinica, 1982, 17(12): 894-898.

长效抗疟药—喹哌防治鼠疟的实验研究

STUDIES ON PIPERAQUINE AS LONG-ACTING ANTIMALARIAL DRUG AGAINST PLASMODIUM BERGHEI IN MICE

  • 摘要: 1,3双4′-(7′氯-喹啉基-4′)哌哔嗪-1丙烷(简称:喹哌-Piperaquine)的碱或盐,对鼠疟均有长效抑制性预防作用,其作用的持续时间长短,随给药剂量增大而延长。喹哌碱每天50 mg/kg和200 mg/kg,连续灌胃3天,对鼠疟分别有15和60天预防作用;喹哌盐100 mg(碱基)/kg和300 mg(碱基)/kg一次灌胃,对鼠疟分别有30和45天预防作用。相同的给药剂量,喹哌盐的长效作用比喹哌碱好。喹哌碱、喹哌盐及磷酸氯喹,在相同给药剂量对比下,磷酸氯喹无长效预防作用。喹哌碱对鼠疟亦有良好治疗效果,从原虫血症转阴和治疗后的动物存活看,喹哌优于氯喹。

     

    Abstract: Piperaquine, with the chemical structure of 1,3 bis 4'-(7'-chloroquinoly-4') piperazinyl-1 propane, was tested in mice infected with Plasmodium berghei for its antimalarial activity.The duration of its protection against malaria was found to be directly related to the dose of piperaquine administered. It gave mice complete protection for 15 and 60 days respectively against challenge with the parasite after oral administration of 50 mg (base)/kg and 200 mg (base)/kg of the drug for three consecutive days. However, chloroquine given orally at dosage of 50 mg (base)/kg for 3 days, failedto protect the animals for 15 days.A single dose 100 mg (base)/kg and 300 mg (base)/kg of the piperaquine salts separately administered gave mice almost complete protection for 30 and 60 days, respectively.Piperaquine is also a fairly good schizonicide, as it cleared the mice of the asexual blood parasites within 72 hours after administration of 12.5 mg (base)/kg for three consecutive days. These results seem to indicate that the drug is more effective and less toxic than chloroquine.

     

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