Description
DuloxetinehydrochlorideisacompetitiveinhibitorofSEROtoninandnorepinephrinetransporters(SERT,NET)thatisclinicallyusedtotreatdepression,anxiety,neuropathy,fibromyalgia,andstressurinaryincontinence.Duloxetine’sinhibitionofneurotransmitterreuptakealtersdownstreamsignalingmediatedbyNMDAreceptorsandNOaswell.Theinhibitoryactivityofthiscompoundonneurotransmitterreuptakeisrelatedtoitsantidepressantandanxiolyticcharacteristics.Theeffectsofduloxetineasatreatmentforneuropathyandfibromyalgia,however,arelikelyduetoitsantagoNISTactivityatvoltage-gatedNav1.7Na+channels,whichareinvolvedinfibromyalgiaandpainsignaling.
References
WangSY,CalderonJ,KuoWangG.BlockofneuronalNa+channelsbyantidepressantduloxetineinastate-dependentmanner.Anesthesiology.2010Sep;113(3):655-65.PMID:20693878.
CarterNJ,McCormackPL.Duloxetine:areviewofitsuseinthetreatmentofgeneralizedanxietydisorder.CNSDrugs.2009;23(6):523-41.PMID:19480470.
ApparsundaramS,StockdaleDJ,HenningsenRA,etal.Antidepressantstargetingtheserotoninreuptaketransporteractviaacompetitivemechanism.JPharmacolExpTher.2008Dec;327(3):982-90.PMID:18801947.
MüllerN,SchennachR,RiedelM,etal.Duloxetineinthetreatmentofmajorpsychiatricandneuropathicdisorders.ExpertRevNeurother.2008Apr;8(4):527-36.PMID:18416656.
SweeneyDD,ChancellorMB.Treatmentofstressurinaryincontinencewithduloxetinehydrochloride.RevUrol.2005Spring;7(2):81-6.PMID:16985814.
