临床药物动力学almotriptan,血清素5 - (1 b / 1 d)受体激动剂治疗偏头痛。
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麦肯罗JD, Fleishaker JC
临床药物动力学almotriptan,血清素5 - (1 b / 1 d)受体激动剂治疗偏头痛。
Pharmacokinet。2005; 44 (3): 237 - 46。
- PubMed ID
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15762767 (在PubMed]
- 文摘
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almotriptan的药物代谢动力学情况是线性的范围在健康志愿者口服剂量200毫克。复合半衰期约为3个小时。Almotriptan口服后吸收良好,平均绝对生物利用度为69.1%。最大血浆浓度达到1.5到4小时后剂量管理;然而,政府后1小时内,等离子体浓度大约68%的值在3小时后管理。食品不明显影响almotriptan吸收。Almotriptan不是高度蛋白结合的,在体内广泛分布。大约50% almotriptan剂量不变排出的尿液;这是主要的单淘汰机制。肾清除率是介导的,在某种程度上,通过积极的管状分泌,平衡almotriptan剂量是不活跃的化合物代谢。 The predominant route of metabolism is via monoamine oxidase-A, and cytochrome P450 (CYP) mediated oxidation (via CYP3A4 and CYP2D6) occurs to a minor extent. Almotriptan clearance is moderately reduced in elderly subjects, but the magnitude of this effect does not warrant a dose reduction. Sex has no significant effect on almotriptan pharmacokinetics. Almotriptan pharmacokinetic parameters do not differ between adolescents and adults, and absorption is not affected during a migraine attack. As expected, renal dysfunction results in reduced clearance of almotriptan. Patients with moderate-to-severe renal dysfunction should use the lowest dose of almotriptan and the total daily dose should not exceed 12.5 mg. Similar dosage recommendations are valid for patients with hepatic impairment, based on the clearance mechanisms for almotriptan. Drug-drug interaction studies were conducted between almotriptan and the following compounds: fluoxetine, moclobemide, propranolol, verapamil and ketoconazole. No significant pharmacokinetic or pharmacodynamic interactions with almotriptan were observed for fluoxetine or propranolol. Almotriptan clearance was reduced, to a modest degree, by moclobemide and verapamil, which was consistent with the contribution of monoamine oxidase-A and CYP3A4 to the metabolic clearance of almotriptan. Although ketoconazole has a greater effect on almotriptan clearance than verapamil, no dosage adjustment is required when almotriptan is given with these drugs.
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- 药物酶
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药物 酶 类 生物 药理作用 行动 Almotriptan 胺氧化酶(flavin-containing) 蛋白质 人类 未知的底物细节 Almotriptan 细胞色素P450 2 d6 蛋白质 人类 未知的底物细节 Almotriptan 细胞色素P450 3 a4 蛋白质 人类 未知的底物细节 - 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Almotriptan 例如 的新陈代谢Almotriptan结合例如时可以减少。 Almotriptan 甲硫咪唑 的新陈代谢时可以减少Almotriptan结合甲巯基咪唑。 Almotriptan 胺碘酮 的新陈代谢Almotriptan时可以减少与胺碘酮相结合。 Almotriptan Midostaurin 的新陈代谢Almotriptan结合Midostaurin时可以减少。 Almotriptan 伏立康唑 的新陈代谢时可以减少Almotriptan结合伏立康唑。 Almotriptan 依法韦伦 的新陈代谢时可以减少Almotriptan结合依法韦伦。 Almotriptan Delavirdine 的新陈代谢Almotriptan结合Delavirdine时可以减少。 Almotriptan Telithromycin 的新陈代谢Almotriptan结合Telithromycin时可以减少。 Almotriptan 酮康唑 的新陈代谢时可以减少Almotriptan结合酮康唑。 Almotriptan Atazanavir 的新陈代谢Almotriptan结合Atazanavir时可以减少。
