氟伏沙明的药物代谢动力学情况的概述。
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范Harten J
氟伏沙明的药物代谢动力学情况的概述。
Pharmacokinet。1995; 29增刊1:1-9。doi: 10.2165 / 00003088-199500291-00003。
- PubMed ID
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8846617 (在PubMed]
- 文摘
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氟伏沙明、药物动力学的一种选择性5 -羟色胺再摄取抑制剂(SSRI)与抗抑郁药物特性,建立了。口服后,药物是几乎完全从胃肠道吸收,吸收的程度是影响食品的存在。尽管完全吸收,口服生物利用度的人是大约50%的初步的肝的新陈代谢。等离子体氟伏沙明峰值浓度达到4到12个小时(肠溶片)或2到8个小时(胶囊、包膜缓释药片)管理。稳态等离子体浓度达到后5到10天内开始治疗和30 - 50%从单剂量数据高于预期。氟伏沙明治疗剂量范围显示非线性稳态药物动力学,用不成比例地提高等离子体浓度更高的剂量。等离子体浓度氟伏沙明显示没有明确与抗抑郁药物反应或不良反应的严重程度的关系。氟伏沙明进行大面积氧化代谢,最有可能在肝脏。九个代谢物已确定,没有一个已知的药物活性。特定的细胞色素P450 (CYP)同功酶参与代谢氟伏沙明是未知的。 CYP2D6, which is crucially involved in the metabolism of paroxetine and fluoxetine, appears to play a clinically insignificant role in the metabolism of fluvoxamine. The drug is excreted in the urine, predominantly as metabolites, with only negligible amounts ( < 4%) of the parent compound. Fluvoxamine shows a biphasic pattern of elimination with a mean terminal elimination half-life of 12 to 15 hours after a single oral dose; this is prolonged by 30 to 50% at steady-state. Plasma protein binding of fluvoxamine (77%) is low compared with that of other SSRIs. Fluvoxamine pharmacokinetics are substantially unaltered by increased age or renal impairment. However, its elimination is prolonged in patients with hepatic cirrhosis. Fluvoxamine inhibits oxidative drug metabolising enzymes (particularly CYP1A2, and less potently and much less potently CYP3A4 and CYP2D6, respectively) and has the potential for clinically significant drug interactions. Drugs whose metabolic elimination is impaired by fluvoxamine include tricyclic antidepressants (tertiary, but not secondary, amines), alprazolam, bromazepam, diazepam, theophylline, propranolol, warfarin and, possibly, carbamazepine. Fluvoxamine is a second generation antidepressant that selectively inhibits neuronal reuptake of serotonin (5-hydroxytryptamine; 5-HT). Fluvoxamine exhibits antidepressant activity similar to that of the tricyclic antidepressants, but has a somewhat improved tolerability profile, particularly with respect to a lower incidence of anticholinergic effects and reduced cardiotoxic potential. However, gastrointestinal adverse effects, especially nausea, are seen more frequently with fluvoxamine than with the tricyclic antidepressants. Fluvoxamine does not have an asymmetric carbon in its structure (fig. 1) and therefore does not exist as optical isomers. For this reason, the potentially confounding problem of stereoisomerism does not arise with fluvoxamine.
DrugBank数据引用了这篇文章
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药物 酶 类 生物 药理作用 行动 氟伏沙明 细胞色素P450 3 a4 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);">
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药物 交互 整合药物之间
在您的软件的交互醋丁洛尔 西布曲明 醋丁洛尔的血清浓度可以增加时结合西布曲明。 醋丁洛尔 奈法唑酮 醋丁洛尔的血清浓度可以增加时结合奈法唑酮。 醋丁洛尔 Zimelidine 醋丁洛尔的血清浓度时可以增加与Zimelidine相结合。 醋丁洛尔 Dapoxetine 醋丁洛尔的血清浓度时可以增加与Dapoxetine相结合。 醋丁洛尔 Milnacipran 醋丁洛尔的血清浓度时可以增加与Milnacipran相结合。 醋丁洛尔 Desvenlafaxine 醋丁洛尔的血清浓度时可以增加与Desvenlafaxine相结合。 醋丁洛尔 Seproxetine 醋丁洛尔的血清浓度时可以增加与Seproxetine相结合。 醋丁洛尔 Levomilnacipran 醋丁洛尔的血清浓度时可以增加与Levomilnacipran相结合。 醋丁洛尔 Indalpine 醋丁洛尔的血清浓度时可以增加与Indalpine相结合。 醋丁洛尔 Alaproclate 醋丁洛尔的血清浓度时可以增加与Alaproclate相结合。
