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阿苯达唑作为人类包虫病的一种潜在治疗方法。

Albendazole as a potential treatment for human hydatidosis.

作者信息

Saimot A G, Meulemans A, Cremieux A C, Giovanangeli M D, Hay J M, Delaitre B, Coulaud J P

出版信息

Lancet. 1983 Sep 17;2(8351):652-6. doi: 10.1016/s0140-6736(83)92533-3.

Abstract

The pharmacokinetics of albendazole was evaluated in 11 patients with hydatid disease who underwent surgery 12 h after the last dose of drug. Albendazole and its main metabolite, albendazole-sulphoxide, were assayed in the serum from peripheral and portal blood, the liver, bile, lungs, and hydatid cyst walls and fluid. After a 10-14 mg/kg daily oral dose of albendazole, concentrations of 1844 +/- 904 ng/g wet tissue of albendazole-sulphoxide were found in the liver and 749 +/- 34 ng/g wet tissue in the lungs. The level in hydatid cyst fluid was 921 +/- 314 ng/ml. The drug was also excreted through the bile. The same daily oral dose produced very stable blood levels after 2 to 4 days of treatment (600-1000 ng/ml). In another part of the study 3 patients with liver cysts, 2 with peritoneal cysts, and 5 with bone cysts received 7 mg/kg twice a day prophylactically and/or therapeutically for 30 days. In all cases the treatment was repeated several times after intervals of 2 weeks. The 3 patients with liver cysts were cured (probably due to treatment); there was no recurrence in the 2 patients with peritoneal cysts and very slight improvement in the 5 cases with bone cysts. The drug was clinically and biologically extremely well tolerated.

摘要

对11例包虫病患者进行了阿苯达唑的药代动力学评估,这些患者在最后一剂药物服用12小时后接受了手术。在周围血和门静脉血、肝脏、胆汁、肺以及包虫囊肿壁和囊液中检测了阿苯达唑及其主要代谢产物阿苯达唑亚砜。每日口服10 - 14mg/kg阿苯达唑后,肝脏中阿苯达唑亚砜的浓度为1844±904ng/g湿组织,肺中为749±34ng/g湿组织。包虫囊肿液中的水平为921±314ng/ml。药物也通过胆汁排泄。治疗2至4天后,相同的每日口服剂量产生非常稳定的血药浓度(600 - 1000ng/ml)。在该研究的另一部分中,3例肝囊肿患者、2例腹膜囊肿患者和5例骨囊肿患者预防性和/或治疗性地接受每日两次7mg/kg的剂量,持续30天。在所有情况下,治疗在间隔2周后重复数次。3例肝囊肿患者治愈(可能归因于治疗);2例腹膜囊肿患者无复发,5例骨囊肿患者有非常轻微的改善。该药物在临床和生物学上耐受性极佳。

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