鼻内舒马曲坦的临床药物动力学。

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Fuseau E, Petricoul O,摩尔KH,手推车,Ibbotson T

鼻内舒马曲坦的临床药物动力学。

41 Pharmacokinet。2002; (11): 801 - 11。

PubMed ID

12190330 (在PubMed

]

文摘

相当大一部分偏头痛患者胃停滞和遭受严重的恶心和/或呕吐在偏头痛发作。这可能导致不稳定的从胃肠道吸收,使口腔治疗不满意。对于这样的病人,一个鼻内制定可能是有利的。舒马曲坦是一个强有力的5 -羟色胺(5 ht (1 b / 1 d)受体激动剂广泛用于治疗偏头痛;鼻内制定的有效性(20毫克)已经被建立在一些临床研究。本文综述了药物动力学的鼻内舒马曲坦,包括口服和皮下的比较管理。鼻内政府后,舒马曲坦直接和迅速吸收,以60%的最大血浆浓度(C (max))发生在30分钟后管理一个20毫克剂量。鼻内政府后,大约10%更舒马曲坦可能通过鼻粘膜吸收相比,口服。意味着C (max)后20毫克鼻内剂量大约是13.1到14.4 ng / mL, C (max)与平均时间约1 - 1.75小时。作为单剂量时,鼻内舒马曲坦显示剂量比例在其吸收程度和C (max)在剂量范围5 - 10毫克,但不是5至20毫克为C (max)。 The elimination phase half-life is approximately 2 hours, consistent with administration by other routes. Sumatriptan is metabolised by monoamine oxidase (MAO; predominantly the A isozyme, MAO-A) to an inactive metabolite. Coadministration with a MAO-A inhibitor, moclobemide, leads to a significant increase in sumatriptan plasma concentrations and is contraindicated. Single-dose pharmacokinetics in paediatric and adolescent patients following intranasal sumatriptan were studied to determine the effect of changes in nasal morphology during growth, and of body size, on pharmacokinetic parameters. The pharmacokinetic profile observed in adults was maintained in the adolescent population; generally, factors such as age, bodyweight or height did not significantly affect the pharmacokinetics. In children below 12 years, C(max) is comparable to that seen in adolescents and adults, but total exposure (area under the concentration-time curve from zero to infinity) was lower in children compared with older patients, especially in younger children treated with 5mg. Clinical experience suggests that intranasal sumatriptan has some advantages over the tablet (more rapid onset of effect and use in patients with gastrointestinal complaints) or subcutaneous (noninvasive and fewer adverse events) formulations.

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药物酶

药物	酶	类	生物	药理作用	行动
舒马曲坦	胺氧化酶(flavin-containing)	蛋白质	人类	未知的	底物	细节