diacerein的临床药物动力学。
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尼古拉斯·P, Tod M Padoin C,佩提特金O
diacerein的临床药物动力学。
Pharmacokinet。1998年11月,35 (5):347 - 59。
- PubMed ID
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9839088 (在PubMed]
- 文摘
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Diacerein药物治疗骨关节炎患者。这种药是口服50毫克每日两次。Diacerein完全转化为大黄酸在到达体循环之前。大黄酸本身就是被肾路线(20%)或共轭在肝脏,大黄酸葡糖苷酸(60%)和大黄酸硫酸(20%);这些代谢物主要通过肾脏排除。diacerein差不多的药物动力学特征的年轻健康的志愿者和老年人正常的肾功能,后两个单剂量(50毫克)或重复剂量75毫克每天两次(25)。大黄酸动力学在单一口服剂量的diacerein线性范围50到200毫克。然而,大黄酸动力学时间,因为nonrenal间隙随重复剂量。这导致了一个温和的最大血浆浓度的增加,血浆浓度时间曲线下的面积和消除半衰期。然而,达到稳态的第三个政府和消除半衰期是大约7到8小时。 Taking diacerein with a standard meal delays systemic absorption, but is associated with a 25% increase in the amount absorbed. Mild-to-severe (Child Pugh's grade B to C) liver cirrhosis does not change the kinetics of diacerein, whereas mild-to-severe renal insufficiency (creatinine clearance < 2.4 L/h) is followed by accumulation of rhein which justifies a 50% reduction of the standard daily dosage. Rhein is highly bound to plasma proteins (about 99%), but this binding is not saturable so that no drug interactions are likely to occur, in contrast to those widely reported with nonsteroidal anti-inflammatory drugs. Except for moderate and transient digestive disturbances (soft stools, diarrhoea), diacerein is well tolerated and seems neither responsible for gastrointestinal bleeding nor for renal, liver or haematological toxicity.
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- 药物
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反应 细节
