CPT

CPT 78(3), September 2005

• Ho & Kim, "Transporters and drug therapy: Implications for drug disposition and disease"
• Loetsch, et al, "The 5-hydroxytryptamine 4 receptor agonist mosapride does not antagonize morphine-induced respiratory depression"

 On the basis of experiments in rats, 5-HT₄ agonists have been proposed as a novel therapeutic strategy for the selective treatment of respiratory depression caused by opioids while leaving analgesic effects unaffected.

• だったのだが，ヒトでは結局だめだった．

 Our results show that, with mosapride, opioid-induced respiratory depression cannot be prevented, and because other 5-HT₄ agonists are not curently available for clinical use, a cure for opioid-induced respiratory depression as promised by the previous successful experiments in laboratory animals is not yet available in clinical practice.

This failure was probably a result of a low potency of mosapride or, alternatively, the limited amount of mosapride that entered the brain.