Sugrue David, Bogner Robin, Ehret Megan J
David Sugrue, B.S., is a 2015 Pharm.D. candidate; Robin Bogner, M.S., Ph.D., is Associate Professor of Pharmaceutics; and Megan J. Ehret, Pharm.D., M.S., BCPP, is Associate Professor of Pharmacy Practice, School of Pharmacy, University of Connecticut, Storrs.
Am J Health Syst Pharm. 2014 Jul 15;71(14):1163-70. doi: 10.2146/ajhp130638.
Current literature on the safety and efficacy of various intermediate- and long-acting preparations of methylphenidate and dexmethylphenidate for pediatric attention-deficit/hyperactivity disorder (ADHD) is reviewed.
The efficacy of methylphenidate in controlling ADHD symptoms is firmly established. Given the drug's relatively short half-life in pediatric patients (about 2.5 hours), a number of intermediate- and long-acting products have been developed; these extended-release methylphenidate products provide the same efficacy as immediate-release (IR) formulations, with the convenience of less frequent dosing. Intermediate-acting methylphenidate preparations have effects lasting as long as 8 hours, but peak concentrations are not attained for up to 5 hours, and many patients may require twice-daily dosing. Long-acting methylphenidate products developed to address these challenges include a controlled-release tablet and bimodal-delivery capsules containing mixtures of IR and extended-release beads (durations of effect, 8-12 hours). Options for patients with difficulty swallowing tablets or capsules include a once-daily transdermal delivery system and a once-daily liquid formulation. Dexmethylphenidate (the more pharmacologically active d-isomer of racemic methylphenidate) can provide efficacy comparable to that of IR methylphenidate at half the dose; an extended-release form of dexmethylphenidate can provide less fluctuation in peak and trough concentrations than the IR form. Methylphenidate and dexmethylphenidate products in capsule form can be opened and sprinkled on applesauce.
The various formulations of IR and intermediate- and extended-release methylphenidate and dexmethylphenidate can be useful options in satisfying patients' individual needs in the management of ADHD. All are equally efficacious in controlling ADHD symptoms.
综述目前关于哌醋甲酯和右哌醋甲酯各种中长效制剂治疗儿童注意力缺陷多动障碍（ADHD）的安全性和有效性的文献。
哌醋甲酯在控制ADHD症状方面的有效性已得到确证。鉴于该药物在儿科患者中的半衰期相对较短（约2.5小时），已开发出多种中长效产品；这些缓释哌醋甲酯产品提供与速释（IR）制剂相同的疗效，且给药频率较低，使用方便。中效哌醋甲酯制剂的作用持续长达8小时，但在长达5小时内无法达到峰值浓度，许多患者可能需要每日给药两次。为应对这些挑战而开发的长效哌醋甲酯产品包括控释片和含有速释和缓释珠混合物的双峰释放胶囊（作用持续时间为8 - 12小时）。对于吞咽片剂或胶囊有困难的患者，选择包括每日一次的透皮给药系统和每日一次的液体制剂。右哌醋甲酯（消旋哌醋甲酯的药理活性更强的d - 异构体）可以以一半的剂量提供与IR哌醋甲酯相当的疗效；右哌醋甲酯的缓释形式与IR形式相比，峰浓度和谷浓度的波动较小。胶囊形式的哌醋甲酯和右哌醋甲酯产品可以打开并撒在苹果酱上。
IR、中效和长效哌醋甲酯以及右哌醋甲酯的各种制剂在满足患者治疗ADHD的个体需求方面可能是有用的选择。所有这些制剂在控制ADHD症状方面同样有效。
