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奥司他韦的药代动力学:一种用于治疗和预防不同人群流感的口服抗病毒药物。

Pharmacokinetics of oseltamivir: an oral antiviral for the treatment and prophylaxis of influenza in diverse populations.

机构信息

Hoffmann-La Roche Inc., 340 Kingsland Street, Nutley, NJ 07110, USA.

出版信息

J Antimicrob Chemother. 2010 Apr;65 Suppl 2(Suppl 2):ii5-ii10. doi: 10.1093/jac/dkq015.

Abstract

Influenza is a transmissible viral pathogen that continues to cause substantial morbidity and mortality. Oseltamivir is an orally administered antiviral medication that selectively inhibits the influenza neuraminidase enzymes that are essential for viral replication. Treatment of infected children > or =1 year and adults of all ages may decrease the severity and duration of the symptoms of infection, while prophylactic dosing can prevent their onset. Oseltamivir is ingested in the form of a prodrug (oseltamivir phosphate) that is rapidly converted by hepatic esterases into the active metabolite, oseltamivir carboxylate. Oseltamivir carboxylate has high bioavailability and penetrates sites of infection at concentrations that are sufficient to inhibit viral replication. The pharmacokinetics of oseltamivir and oseltamivir carboxylate are dose proportional after repeated doses of up to 500 mg twice daily. This predictable profile means that oseltamivir is suitable for use in diverse patient populations, which may include young children and elderly patients, various ethnic groups and those with renal or hepatic impairment. As the potential for drug interactions is low, oseltamivir is also suitable for use in patients with co-morbid conditions who are likely to be receiving concomitant medications.

摘要

流感是一种具有传染性的病毒病原体,它会持续导致大量发病率和死亡率。奥司他韦是一种口服抗病毒药物,可选择性抑制流感神经氨酸酶,而这种酶对病毒复制至关重要。治疗 1 岁及 1 岁以上的感染儿童和所有年龄段的成年感染者,可以减轻感染症状的严重程度和持续时间,而预防性剂量可以预防其发病。奥司他韦以前药(磷酸奥司他韦)的形式被摄入,这种前药在肝酯酶的作用下迅速转化为活性代谢物,即奥司他韦羧酸。奥司他韦羧酸具有很高的生物利用度,并能穿透感染部位,其浓度足以抑制病毒复制。在每日两次、每次 500 毫克重复剂量后,奥司他韦和奥司他韦羧酸的药代动力学呈剂量比例。这种可预测的特征意味着奥司他韦适合用于不同的患者群体,包括儿童和老年患者、不同种族以及肾功能或肝功能受损的患者。由于药物相互作用的潜力较低,奥司他韦也适合用于可能同时服用其他药物的合并症患者。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0ca3/2835511/e346bf72849c/dkq01501.jpg

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