The clinical pharmacology of intranasal l-methamphetamine.
The clinical pharmacology of intranasal l-methamphetamine.
复制标题
DOI：
10.1186/1472-6904-8-4
复制
发表时间：
2008-07-21
期刊：
影响因子：
--
通讯作者：
Jones, Reese T
中科院分区：
文献类型：
--
作者：
Mendelson, John E;McGlothlin, Dana;Harris, Debra S;Foster, Elyse;Everhart, Tom;Jacob, Peyton 3rd;Jones, Reese T
我们研究了l-甲基苯丙胺的药理学，滥用较少的异构体，当用作鼻减充血剂。12名受试者从非处方吸入器中以推荐剂量（6小时内吸入16次）自我给药l-甲基苯丙胺，然后以该剂量的2倍和4倍（32次和64次吸入）给药。在单独的阶段中，静脉内给予苯丙氨酸（200 μg）和l-甲基苯丙胺（5 mg），以确定α激动剂药理学和生物利用度。测量生理、心血管、药代动力学和主观效应。血浆L-甲基苯丙胺水平通常低于定量水平，因此通过比较静脉和吸入剂量的尿排泄来估计生物利用度，得出递增暴露量的递送剂量估计值为74.0 ± 56.1、124.7 ± 106.6和268.1 ± 220.5 μg（平均4.2 ± 3.3 μg/吸入）。生理变化极轻微，且无剂量依赖性。观察到每搏输出量和心输出量小幅下降，提示轻度心脏抑制。从非处方产品中吸入l-甲基苯丙胺产生的影响最小，但可能是心脏病。
We studied the pharmacology of l-methamphetamine, the less abused isomer, when used as a nasal decongestant. 12 subjects self-administered l-methamphetamine from a nonprescription inhaler at the recommended dose (16 inhalations over 6 hours) then at 2 and 4 (32 and 64 inhalations) times this dose. In a separate session intravenous phenylephrine (200 μg) and l-methamphetamine (5 mg) were given to define alpha agonist pharmacology and bioavailability. Physiological, cardiovascular, pharmacokinetic, and subjective effects were measured. Plasma l-methamphetamine levels were often below the level of quantification so bioavailability was estimated by comparing urinary excretion of the intravenous and inhaled doses, yielding delivered dose estimates of 74.0 ± 56.1, 124.7 ± 106.6, and 268.1 ± 220.5 μg for ascending exposures (mean 4.2 ± 3.3 μg/inhalation). Physiological changes were minimal and not dose-dependent. Small decreases in stroke volume and cardiac output suggesting mild cardiodepression were seen. Inhaled l-methamphetamine delivered from a non-prescription product produced minimal effects but may be a cardiodepressant.