frovatriptan的临床药物动力学。

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巴肯P, Keywood C, C韦德,病房

frovatriptan的临床药物动力学。

头痛。2002年4月,42增刊2:s54 - 62。

PubMed ID

12028321 (在PubMed

]

文摘

目的:评估可用frovatriptan的临床药物动力学数据。背景:临床数据表明,frovatriptan的药动学特征可能不同于当前可用的药物。方法:健康志愿者的研究中,受试者对肾或肝损伤,老年人,偏头痛患者在和之间的攻击进行了综述。frovatriptan结果:口服生物利用度是22%到30%,尽管时间最大浓度通常是2至3小时,大约60%到70%的等离子体在1小时内达到最大浓度的剂量。Frovatriptan分配成红细胞,绑定可逆的和与时间有关的。终端消除半衰期相对较长(约26小时)带来良好的系统性风险和可能产生长期的治疗作用,从而减少偏头痛复发和redosing的必要性。系统性接触frovatriptan通常与剂量介于1和100毫克。血液和血浆frovatriptan浓度持续高于女性,但没有需要根据性别调整剂量。药物动力学本质上是不受食物影响,重复给药后可预测;稳态是接近大约4到5天。 Pharmacokinetics were changed only slightly in subjects with renal impairment or mild-to-moderate hepatic impairment, elderly individuals, and during migraine attacks. Frovatriptan is principally metabolized by the CYP1A2 isoenzyme of cytochrome P-450 and is cleared by the kidney and liver, each having sufficient capacity to compensate for impairment of the other. CONCLUSIONS: Frovatriptan can be taken without regard for food intake, and because of the large therapeutic margin and shallow dose-response curve, there is no need for dosage adjustment in the elderly, in women taking a combined oral contraceptive, in patients with mild-to-severe renal impairment, mild-to-moderate hepatic impairment, or according to gender. The long duration of exposure may reduce the likelihood of early migraine recurrence.

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
Frovatriptan	细胞色素P450 1 a2	蛋白质	人类	未知的	底物	细节