Brown G L, Hunt R D, Ebert M H, Bunney W E, Kopin I J
Psychopharmacology (Berl). 1979 Apr 11;62(2):133-40. doi: 10.1007/BF00427126.
Amphetamine has been clearly documented to be an efficacious treatment for hyperactive children. The pharmacokinetics of amphetamine have been studied in adults, but not in children. Sixteen male children who scored greater than 2SD from norms on Factors I and IV of Conner's Teacher Rating Scale and who were not excluded for reasons to do with medical or psychiatric conditions, intelligence, or age, had a plasma d-amphetamine apparent elimination half-life of 6.8 +/- 0.5h. Peak plasma level occurred between 3 and 4h (62.7 +/- 3.8 and 65.9 +/- 3.6 ng/ml, respectively). Six of these children had a repeat study and there were no significant differences within subject in apparent elimination half-lives and attained peak blood levels. The variation in plasma levels was greater during absorption than during elimination. Both behavioral and motor activity responses as analyzed by differences between amphetamine and placebo days (by paired t-tests) indicate significant responses between hours 1--4; however, these responses do not correlate with plasma amphetamine levels; they occur during the absorption phase. The decreased response to later similar plasma levels of d-amphetamine may be related to depletion of catecholamine stores, to replacement by a 'false neurotransmitter' metabolite of amphetamine, or to alteration in receptor sensitivity.
苯丙胺已被明确证明是治疗多动症儿童的有效药物。苯丙胺的药代动力学已在成人中进行了研究，但尚未在儿童中进行研究。16名男性儿童在康纳教师评定量表的因子I和IV上的得分高于正常标准2个标准差，且未因医学或精神疾病、智力或年龄等原因被排除，其血浆右旋苯丙胺的表观消除半衰期为6.8±0.5小时。血浆峰值水平出现在3至4小时之间（分别为62.7±3.8和65.9±3.6纳克/毫升）。其中6名儿童进行了重复研究，受试者的表观消除半衰期和达到的血药峰值水平没有显著差异。血浆水平在吸收过程中的变化大于消除过程。通过苯丙胺和安慰剂日之间的差异分析（配对t检验）得出的行为和运动活动反应均表明，在1-4小时之间有显著反应；然而，这些反应与血浆苯丙胺水平无关；它们发生在吸收阶段。对后来类似血浆水平的右旋苯丙胺反应降低可能与儿茶酚胺储存耗竭、被苯丙胺的“假神经递质”代谢产物替代或受体敏感性改变有关。
