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氟甲喹在鸽子(家鸽)静脉注射、肌肉注射和口服给药后的临床药理学和药代动力学

Clinical pharmacology and pharmacokinetics of flumequine after intravenous, intramuscular and oral administration in pigeons (Columba livia).

作者信息

Dorrestein G M, van Gogh H, Buitelaar M N, Nouws J F

出版信息

J Vet Pharmacol Ther. 1983 Dec;6(4):281-92. doi: 10.1111/j.1365-2885.1983.tb00003.x.

Abstract

The in-vitro activity of flumequine against 157 strains of bacteria isolated from birds was determined. The minimum inhibitory concentration (MIC) of 96.3% of the Enterobacteriaceae, Proteus spp. and Yersinia pseudotuberculosis studied (n = 135) was less than or equal to 1 microgram/ml. Pharmacokinetics of flumequine in pigeons (Columba livia) was investigated after intravenous, intramuscular and oral administration. From the blood disappearance curves after i.v. bolus injection (10 mg/kg body weight) clearance rate, blood half-time and distribution volume were calculated. The recovery of unchanged flumequine from the droppings in 24 h was 37 +/- 10% of the administered dose. Flumequine was also given i.m. at two dose levels, 10 and 60 mg/kg body weight. The availability of flumequine as intact drug was 22 and 23%, respectively, in 24 h. Therapeutic blood levels were maintained for 4 and 10 h, respectively. After an oral dose of flumequine (60 mg/kg body weight) an availability of 6.7 +/- 2.5% and a peak blood concentration of 2.68 +/- 0.92 microgram/ml at 2 h after administration were found. The recovery of unchanged flumequine from the droppings in 24 h was 1.55 +/- 0.79% of the administered dose. With the exception of the i.m. dose of 10 mg/kg, all flumequine administrations made the pigeons vomit. It appears that blood concentrations below 3 micrograms/ml will not induce vomiting. On the basis of the present data, a dosage regimen for flumequine in pigeons of a priming dose of 30 mg/kg i.m., followed after 8 h by oral administration of 30 mg/kg, this dose being repeated every 8-12 h, would be expected to give blood concentrations between 1.44 and 2.88 micrograms/ml.

摘要

测定了氟甲喹对从鸟类分离出的157株细菌的体外活性。所研究的96.3%的肠杆菌科、变形杆菌属和假结核耶尔森菌(n = 135)的最低抑菌浓度(MIC)小于或等于1微克/毫升。在静脉内、肌肉内和口服给药后,研究了氟甲喹在鸽子(家鸽)体内的药代动力学。从静脉推注(10毫克/千克体重)后的血药消除曲线计算清除率、血液半衰期和分布容积。24小时内从粪便中回收的未变化氟甲喹占给药剂量的37±10%。氟甲喹也以10和60毫克/千克体重两个剂量水平进行肌肉注射。氟甲喹作为完整药物的生物利用度在24小时内分别为22%和23%。治疗性血药浓度分别维持4小时和10小时。口服氟甲喹(60毫克/千克体重)后,生物利用度为6.7±2.5%,给药后2小时血药峰值浓度为2.68±0.92微克/毫升。24小时内从粪便中回收的未变化氟甲喹占给药剂量的1.55±0.79%。除了10毫克/千克的肌肉注射剂量外,所有氟甲喹给药均使鸽子呕吐。似乎血药浓度低于3微克/毫升不会引起呕吐。根据目前的数据,鸽子使用氟甲喹的给药方案为:首剂30毫克/千克肌肉注射,8小时后口服30毫克/千克,此剂量每8 - 12小时重复一次,预计血药浓度在1.44至2.88微克/毫升之间。

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