Elucidation of molecular pharmacological profile of mu opioid receptor agonists, and clinical applications thereof

Increasing action of β-arrestin recruitment with fentanyl and methadone was increased by combination of loperamide and oxycodone. On the other hand, β-arrestin recruitment increasing action by fentanyl was remarkably decreased by hydromorphone together with fentanyl. After calculating the side effect coefficient based on constipation and painkilling strength of each strong opioid, and then analyzing the correlation of the bias coefficient by each strong opioid, no significant differences were observed between these coefficients. After performing comparison between morphine and TRV130 about painkilling, constipation, vomiting, nausea and spontaneous momentum, big differences were not recognized between two drugs.

本研究では、オピオイド受容体作動薬の薬理学的プロファイルを検討した。この研究成果から、オピオイド製剤の適正使用の理解が深まり、オピオイド使用に関するアルゴリズムの確立に寄与できたものと思われる。そして、オピオイドの適正使用や効率的なオピオイドスイッチングに有用な情報を与える事が出来るものと考える。