Ereshefsky Larry, Mascarenas Cynthia A
Department of Pharmacology, University of Texas Health Science Center at San Antonio and Clinical Research Unit, San Antonio State Hospital, 78229, USA.
J Clin Psychiatry. 2003;64 Suppl 16:18-23.
Clinicians face a dilemma when choosing between short-acting atypical antipsychotics and long-acting conventional antipsychotics. Atypical antipsychotics offer better safety and efficacy, while depot formulations of conventional antipsychotics provide more reliable drug delivery, reduced differences in peak and trough plasma levels of drug, and greater dosing precision. Risperidone was recently approved by the U.S. Food and Drug Administration as the first atypical long-acting antipsychotic medication, given as biweekly gluteal injections. This long-acting formulation is synthesized using a microsphere encapsulation process, and gradual hydrolysis of the copolymer encapsulating the drug provides a steady release of medication. Consistent with other long-acting medications, plasma drug level fluctuation is reduced more with long-acting than with oral risperidone. Analyses are currently underway to further examine safety outcomes with long-acting risperidone.
临床医生在选择短效非典型抗精神病药物和长效传统抗精神病药物时面临两难境地。非典型抗精神病药物具有更好的安全性和疗效，而传统抗精神病药物的长效剂型能提供更可靠的药物递送，减少药物血浆峰谷水平差异，并具有更高的给药精度。利培酮最近被美国食品药品监督管理局批准为首个非典型长效抗精神病药物，通过每两周一次的臀肌注射给药。这种长效制剂采用微球包封工艺合成，包裹药物的共聚物逐渐水解可实现药物的持续释放。与其他长效药物一致，长效利培酮比口服利培酮更能降低血浆药物水平波动。目前正在进行分析，以进一步研究长效利培酮的安全性结果。
