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用于恶性疟的肌肉注射奎宁负荷剂量:药代动力学与毒性

Intramuscular loading dose of quinine for falciparum malaria: pharmacokinetics and toxicity.

作者信息

Wattanagoon Y, Phillips R E, Warrell D A, Silamut K, Looareesuwan S, Nagachinta B, Back D J

出版信息

Br Med J (Clin Res Ed). 1986 Jul 5;293(6538):11-3. doi: 10.1136/bmj.293.6538.11.

Abstract

In a study of intramuscular injection of quinine eight adults with moderately severe falciparum malaria resistant to chloroquine were treated with quinine dihydrochloride, being given a loading dose of 20 mg salt (16.7 mg base)/kg followed by three or four eight hourly maintenance doses of 10 mg salt (8.3 mg base)/kg injected into the anterior thigh. All patients responded to treatment. Fever and parasite clearance times (mean (SD) 60 (23) h and 53 (22) h respectively) were comparable with those obtained with intravenous quinine. The mean peak plasma quinine concentration of 11.0 mg/l (34.4 mu mol/l) [corrected] was reached a median of five hours after administration of the loading dose. In all patients plasma quinine concentrations exceeded the high minimum inhibitory concentration for Plasmodium falciparum malaria prevalent in Thailand within four hours of the start of treatment but did not cause toxicity other than mild cinchonism. When intravenous infusion is not possible an intramuscular quinine loading dose is an effective means of starting treatment in patients with moderately severe falciparum malaria who cannot swallow tablets.

摘要

在一项关于肌肉注射奎宁的研究中,8名对氯喹耐药的中度严重恶性疟原虫疟疾成年患者接受了二盐酸奎宁治疗,给予20mg盐(16.7mg碱基)/kg的负荷剂量,随后在前臂注射8小时一次、每次10mg盐(8.3mg碱基)/kg的维持剂量,共三次或四次。所有患者对治疗均有反应。发热和寄生虫清除时间(分别平均(标准差)为60(23)小时和53(22)小时)与静脉注射奎宁时的情况相当。负荷剂量给药后5小时中位数达到血浆奎宁平均峰值浓度11.0mg/l(34.4μmol/l)[校正后]。所有患者在治疗开始后4小时内血浆奎宁浓度均超过泰国流行的恶性疟原虫疟疾的高最低抑菌浓度,但除轻度金鸡纳中毒外未引起毒性反应。当无法进行静脉输注时,肌肉注射奎宁负荷剂量是对不能吞咽片剂的中度严重恶性疟原虫疟疾患者开始治疗的有效方法。

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本文引用的文献

1
Intramuscular or intralipomatous injections?肌内注射还是脂肪内注射?
N Engl J Med. 1982 Aug 5;307(6):356-8. doi: 10.1056/NEJM198208053070607.
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Quinine disposition kinetics.奎宁处置动力学。
Br J Clin Pharmacol. 1983 Oct;16(4):399-403. doi: 10.1111/j.1365-2125.1983.tb02184.x.
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Intramuscular chloroquine in children.儿童肌肉注射氯喹
Lancet. 1984 Aug 4;2(8397):288. doi: 10.1016/s0140-6736(84)90328-3.
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Pharmacokinetics of quinine in children.奎宁在儿童中的药代动力学。
J Pediatr. 1985 Mar;106(3):506-10. doi: 10.1016/s0022-3476(85)80692-2.
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Trans R Soc Trop Med Hyg. 1979;73(2):230-2. doi: 10.1016/0035-9203(79)90221-9.

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