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一种用于治疗急性疟疾的喹啉甲醇(WR 30090)。

A quinoline methanol (WR 30090) for treatment of acute malaria.

作者信息

Martin D C, Arnold J D, Clyde D F, al-Ibrahim M, Carson P E, Rieckmann K H, Willerson D

出版信息

Antimicrob Agents Chemother. 1973 Feb;3(2):214-9. doi: 10.1128/AAC.3.2.214.

Abstract

WR 30090 at a dose of 230 mg every 8 hr for 6 days has proven to be a safe, well-tolerated compound with photosensitivity proving to be a minor consideration. WR 30090 was found to be an effective medication for the treatment of acute malaria caused by several strains of Plasmodium falciparum. At the dose of 230 mg every 8 hr for 6 days, all of six men infected with a chloroquine-susceptible strain (Uganda I) were cured, all of 13 subjects infected with moderately chloroquine-resistant strains (Malayan Camp, Malayan Taylor, and Philippine Per) were cured, and 19 of 23 subjects infected with strains highly resistant to chloroquine (Vietnam Smith and Vietnam Crocker) were cured. All of five subjects infected with the chloroquine-resistant Vietnam Marks strain were cured with only 3 days of therapy. Blood-induced P. vivax (Chesson strain) infection showed a mixed response. Six out of seven volunteers were cured when treated for 3 days with WR 30090. The one recrudescence responded to a repeated course of therapy for 3 days. However, recrudescence occurred in one volunteer treated for 6 days. Treatment with WR 30090 failed to cure sporozoite-induced P. vivax (Chesson strain) infection in any of four subjects. In all subjects treated, there was good suppression of parasitemia and relief of symptoms. The susceptibility of the strains of malaria to WR 30090 to some degree parallels their susceptibility to chloroquine.

摘要

WR 30090以每8小时230毫克的剂量服用6天,已被证明是一种安全、耐受性良好的化合物,光敏性只是一个次要考虑因素。WR 30090被发现是一种治疗由几种恶性疟原虫菌株引起的急性疟疾的有效药物。在每8小时230毫克、持续6天的剂量下,6名感染氯喹敏感菌株(乌干达I)的男性全部治愈,13名感染中度氯喹耐药菌株(马来营地、马来泰勒和菲律宾佩尔)的受试者全部治愈,23名感染高度耐氯喹菌株(越南史密斯和越南克罗克)的受试者中有19名治愈。5名感染氯喹耐药的越南马克斯菌株的受试者仅接受3天治疗就全部治愈。血液诱导的间日疟原虫(切森菌株)感染呈现出混合反应。7名志愿者中有6名在接受WR 30090治疗3天后治愈。一名复发者对重复3天的治疗有反应。然而,一名接受6天治疗的志愿者出现了复发。WR 30090治疗未能治愈4名受试者中任何一人的子孢子诱导的间日疟原虫(切森菌株)感染。在所有接受治疗的受试者中,疟原虫血症得到了良好的抑制,症状得到了缓解。疟疾菌株对WR 30090的敏感性在一定程度上与它们对氯喹的敏感性相似。

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