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

机译:奥司他韦的药代动力学:一种口服抗病毒药用于治疗和预防不同人群的流感

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摘要

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 ≥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.
机译:流感是一种可传播的病毒病原体,继续导致大量发病和死亡。奥瑟他韦是一种口服抗病毒药物,可选择性抑制病毒复制所必需的流感神经氨酸酶。 ≥1岁的感染儿童和各个年龄段的成年人的治疗均可以降低感染症状的严重程度和持续时间,而预防性用药可以预防其发作。奥司他韦以前药(磷酸奥司他韦)的形式被摄入,该药物通过肝酯酶迅速转化为活性代谢产物奥司他韦羧酸盐。奥司他韦羧酸盐具有很高的生物利用度,并以足以抑制病毒复制的浓度穿透感染部位。每天两次重复剂量达500毫克后,奥司他韦和羧酸奥司他韦的药代动力学与剂量成正比。这种可预测的特征意味着奥司他韦适用于各种患者人群,其中可能包括幼儿和老年患者,不同种族的人群以及肾或肝功能不全的人群。由于药物相互作用的可能性很低,奥司他韦也适用于合并症患者,可能正在接受伴随药物治疗。

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