Opioid Antagonists

Name
Opioid Antagonists
Accession Number
DBCAT000935
Description

Agents inhibiting the effect of narcotics on the central nervous system.

Drugs
DrugDrug Description
PentazocineAn analgesic used to treat moderate to severe pain.
NaltrexoneA narcotic antagonist used in opioid overdose.
NalbuphineAn opioid agonist-antagonist used to treat pain, for pre and postoperative analgesia, and for analgesia in labor and delivery.
BuprenorphineA partial opioid agonist used for management of severe pain that is not responsive to alternative treatments. Also used for maintenance treatment of opioid addiction.
NaloxoneAn opioid receptor antagonist used to rapidly reverse an opioid overdose. Also included in some drug formulations as an abuse deterrent to prevent injection.
DiprenorphineDiprenorphine is indicated to reverse the effects of powerful opioids including etorphine and carfentanil, often used for tranquilizing large animals. This drug is not approved for use in humans.
MethylnaltrexoneA μ-opioid antagonist used for the treatment of opioid-induced constipation in palliative patients that are inadequately responding to laxative therapy.
NaloxegolA peripherally-selective opioid antagonist used to treat opioid-induced constipation (OIC) in adult patients with chronic non-cancer pain.
AlvimopanAn opioid antagonist used to reduce healing time of the upper and lower gastrointestinal tract following surgical procedures that involve bowel resection with primary anastomosis.
NaldemedineAn opioid antagonist used to to treat opioid-induced constipation.
NalmefeneAn opioid antagonist used in conjunction with psychosocial support to help adults with alcohol dependence reduce alcohol consumption.
LevallorphanFor the complete or partial reversal of narcotic depression, including respiratory depression, induced by opioids.
ButorphanolAn opioid agonist-antagonist used to treat moderate to severe pain.
NalorphineUsed to reverse opioid overdose.
AxelopranAxelopran has been used in trials studying the treatment of OIC and Opioid-induced Constipation.
SamidorphanSamidorphan has been used in trials studying the treatment of Schizophrenia, Alcohol Dependence, and Binge Eating Disorder.
OndelopranOndelopran has been used in trials studying the treatment of Alcohol Dependence.
MeptazinolNot Annotated
EluxadolineA mixed mu-opioid receptor agonist used to treat irritable bowel syndrome with diarrhea.
DezocineIndicated in the treatment of moderate to severe pain.
LY-2456302Ly2456302 has been used in trials studying the health services research and basic science of Anxiety Disorders and Alcohol Dependence.
Drugs & Drug Targets
DrugTargetType
PentazocineMu-type opioid receptortarget
PentazocineKappa-type opioid receptortarget
PentazocineSigma non-opioid intracellular receptor 1target
PentazocineP-glycoprotein 1transporter
NaltrexoneMu-type opioid receptortarget
NaltrexoneKappa-type opioid receptortarget
NaltrexoneDelta-type opioid receptortarget
NaltrexoneHCG20471, isoform CRA_ctarget
NaltrexoneUDP-glucuronosyltransferase 1-1enzyme
NalbuphineKappa-type opioid receptortarget
NalbuphineMu-type opioid receptortarget
NalbuphineDelta-type opioid receptortarget
BuprenorphineKappa-type opioid receptortarget
BuprenorphineMu-type opioid receptortarget
BuprenorphineCytochrome P450 3A4enzyme
BuprenorphineCytochrome P450 2D6enzyme
BuprenorphineP-glycoprotein 1transporter
BuprenorphineATP-binding cassette sub-family G member 2transporter
BuprenorphineCytochrome P450 2C9enzyme
BuprenorphineCytochrome P450 3A5enzyme
BuprenorphineCytochrome P450 2C8enzyme
BuprenorphineCytochrome P450 3A7enzyme
BuprenorphineDelta-type opioid receptortarget
BuprenorphineCytochrome P450 2C18enzyme
BuprenorphineCytochrome P450 2C19enzyme
BuprenorphineNociceptin receptortarget
NaloxoneMu-type opioid receptortarget
NaloxoneEstrogen receptor alphatarget
NaloxoneCyclic AMP-responsive element-binding protein 1target
NaloxoneDelta-type opioid receptortarget
NaloxoneSolute carrier organic anion transporter family member 1A2transporter
NaloxoneP-glycoprotein 1transporter
NaloxoneKappa-type opioid receptortarget
NaloxoneCytochrome P450 3A4enzyme
NaloxoneSerum albumincarrier
NaloxoneToll-like receptor 4target
NaloxoneLiver carboxylesterase 1target
NaloxoneUDP-glucuronosyltransferase 1-1enzyme
DiprenorphineE3 ubiquitin-protein ligase TRIM13target
DiprenorphineDelta-type opioid receptortarget
DiprenorphineKappa-type opioid receptortarget
DiprenorphineMu-type opioid receptortarget
MethylnaltrexoneMu-type opioid receptortarget
MethylnaltrexoneKappa-type opioid receptortarget
NaloxegolCytochrome P450 3A4enzyme
NaloxegolCytochrome P450 2D6enzyme
NaloxegolCytochrome P450 2C19enzyme
NaloxegolMu-type opioid receptortarget
AlvimopanMu-type opioid receptortarget
AlvimopanKappa-type opioid receptortarget
AlvimopanDelta-type opioid receptortarget
NaldemedineCytochrome P450 3A Subfamilyenzyme
NaldemedineUDP-glucuronosyltransferase 1-3enzyme
NaldemedineMu-type opioid receptortarget
NaldemedineDelta-type opioid receptortarget
NaldemedineKappa-type opioid receptortarget
NaldemedineATP-binding cassette sub-family B member 5transporter
NalmefeneMu-type opioid receptortarget
NalmefeneKappa-type opioid receptortarget
NalmefeneDelta-type opioid receptortarget
NalmefeneUDP-glucuronosyltransferase 2B7enzyme
NalmefeneUDP-glucuronosyltransferase 1-3enzyme
NalmefeneUDP-glucuronosyltransferase 1-8enzyme
LevallorphanMu-type opioid receptortarget
ButorphanolKappa-type opioid receptortarget
ButorphanolMu-type opioid receptortarget
ButorphanolDelta-type opioid receptortarget
EluxadolineMu-type opioid receptortarget
EluxadolineDelta-type opioid receptortarget
EluxadolineKappa-type opioid receptortarget
EluxadolineSolute carrier organic anion transporter family member 1B1transporter
EluxadolineCanalicular multispecific organic anion transporter 1transporter
EluxadolineSolute carrier family 22 member 8transporter
DezocineMu-type opioid receptortarget
DezocineKappa-type opioid receptortarget