奈法唑酮的临床药物动力学。
文章的细节
-
引用
复制到剪贴板 -
格林DS, Barbhaiya RH
奈法唑酮的临床药物动力学。
Pharmacokinet。1997年10月,33 (4):260 - 75。doi: 10.2165 / 00003088-199733040-00002。
- PubMed ID
-
9342502 (在PubMed]
- 文摘
-
奈法唑酮是一种新的抗抑郁药物,化学与三环、四环的或选择性血清素再吸收抑制剂。奈法唑酮阻断5 -羟色胺5-HT2受体和可逆地抑制5 -羟色胺再摄取体内。奈法唑酮是完全,口服后迅速吸收血浆浓度峰值在2小时内观察到的管理。奈法唑酮经历重大的初步的代谢导致口服生物利用度约为20%。虽然是一个奈法唑酮生物利用度与食物增加18%,这一增长不是临床意义和奈法唑酮可以不考虑膳食管理。三种药物活性奈法唑酮代谢物已确定:hydroxy-nefazodone, triazoledione m-chlorophenylpiperazine (mCPP)。奈法唑酮的药物动力学是非线性的。奈法唑酮的血浆浓度的增加大于预期,如果他们与剂量的增加成正比。稳态血浆浓度的奈法唑酮是开始的4天内达到管理。奈法唑酮的药物代谢动力学情况没有明显改变患者的肾或轻度到中度肝损害。 However, nefazodone plasma concentrations are increased in severe hepatic impairment and in the elderly, especially in elderly females. Lower doses of nefazodone may be necessary in these groups. Nefazodone is a weak inhibitor of cytochrome P450 (CYP) 2D6 and does not inhibit CYP1A2. It is not anticipated that nefazodone will interact with drugs cleared by these isozymes. Indeed, nefazodone did not affect the pharmacokinetics of theophylline, a compound cleared by CYP1A2. Nefazodone is metabolised by and inhibits CYP3A4. Clinically significant interactions have been observed between nefazodone and the benzodiazepines triazolam and alprazolam, cyclosporin and carbamazepine. The potential for a clinically significant interaction between nefazodone and other drugs cleared by CYP3A4 (e.g. terfenadine) should be considered before the coadministration of these compounds. There was an increase in haloperidol plasma concentrations when coadministered with nefazodone; nefazodone pharmacokinetics were not affected after coadministration. No clinically significant interaction was observed when nefazodone was administered with lorazepam, lithium, alcohol, cimetidine, warfarin, theophylline or propranolol.
beplay体育安全吗DrugBank数据引用了这篇文章
- 药物酶
-
药物 酶 类 生物 药理作用 行动 奈法唑酮 细胞色素P450 2 d6 蛋白质 人类 未知的底物抑制剂细节 - 药物的相互作用Learn More" title="" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
-
药物 交互 整合药物之间
在您的软件的交互
