酞普兰的临床药物动力学。

文章的细节

引用

Rao N

酞普兰的临床药物动力学。

Pharmacokinet。2007; 46 (4): 281 - 90。doi: 10.2165 / 00003088-200746040-00002。

PubMed ID
17375980 (在PubMed
]
文摘

酞(S)对映体的外消旋选择性5 -羟色胺再摄取抑制剂的抗抑郁药西酞普兰。临床研究表明,酞有效且耐受性良好治疗抑郁症和焦虑症。口服后,酞迅速吸收和达到最大血浆浓度约3 - 4小时后单或multiple-dose管理。酞普兰的吸收不受食物的影响。酞普兰的消除半衰期是即小时以及每日一次是一致的管理。7 - 10天内稳态浓度实现管理。酞低蛋白结合(56%)和不太可能导致与高度蛋白结合的药物的相互作用。广泛分布在整个组织,表观分布容积在终端阶段后口服(V (z) / F)约1100 l。Unmetabolised酞普兰是等离子体的主要化合物。S-demethylcitalopram (S-DCT)的主要代谢产物,是出席大约三分之一酞普兰的水平; however, S-DCT is a weak inhibitor of serotonin reuptake and does not contribute appreciably to the therapeutic activity of escitalopram. The didemethyl metabolite of escitalopram (S-DDCT) is typically present at or below quantifiable concentrations. Escitalopram and S-DCT exhibit linear and dose-proportional pharmacokinetics following single or multiple doses in the 10-30 mg/day dose range. Adolescents, elderly individuals and patients with hepatic impairment do not have clinically relevant differences in pharmacokinetics compared with healthy young adults, implying that adjustment of the dosage is not necessary in these patient groups. Escitalopram is metabolised by the cytochrome P450 (CYP) isoenzymes CYP2C19, CYP2D6 and CYP3A4. However, ritonavir, a potent inhibitor of CYP3A4, does not affect the pharmacokinetics of escitalopram. Coadministration of escitalopram 20mg following steady-state administration of cimetidine or omeprazole led to a 72% and 51% increase, respectively, in escitalopram exposure compared with administration alone. These changes were not considered clinically relevant. In vitro studies have shown that escitalopram has negligible inhibitory effects on CYP isoenzymes and P-glycoprotein, suggesting that escitalopram is unlikely to cause clinically significant drug-drug interactions. The favourable pharmacokinetic profile of escitalopram suggests clinical utility in a broad range of patients.

DrugBank数据引用了这篇文章

药物
药物酶
药物 生物 药理作用 行动
醛氧化酶 蛋白质 人类
没有
底物
细节
胺氧化酶(flavin-containing) 蛋白质 人类
没有
底物
细节
胺氧化酶(flavin-containing) B 蛋白质 人类
没有
底物
细节
细胞色素P450 2 d6 蛋白质 人类
没有
底物
抑制剂
细节
细胞色素P450 3 a4 蛋白质 人类
没有
底物
细节
药物反应
反应
细节
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
Boceprevir
酞普兰的血清浓度可以结合Boceprevir时下降。
识别潜在的药物的风险
容易将40药物与药物相互作用检查程序。
严重性评级,描述和管理建议。
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