Dole V P, Kreek M J
Proc Natl Acad Sci U S A. 1973 Jan;70(1):10. doi: 10.1073/pnas.70.1.10.
Binding of methadone in body tissues limits the rise in plasma concentration and prolongs the pharmacological action in patients receiving a daily maintenance dose. An opiate with equal intrinsic activity but greater binding affinity would, therefore, be a better drug than methadone for maintenance treatment; it would be safer when taken in a single dose and longer in its duration of action when taken on a regular schedule.
美沙酮与人体组织的结合限制了血浆浓度的升高,并延长了接受每日维持剂量患者的药理作用。因此,一种具有同等内在活性但结合亲和力更高的阿片类药物,作为维持治疗用药会比美沙酮更好;单次服用时会更安全,按常规服用时作用持续时间会更长。