High-risk opioids

Strong or potent agonists of the opioid receptors, which include various types of phenanthrenes, phenylheptylamines, and phenylpiperidines. These agents are more potent, conferring a higher risk of adverse effects and drug interactions.
DrugDrug NameDrug Description
DB00813FentanylAn opioid analgesic used in anesthesia, for breakthrough cancer pain, or round the clock pain management.
DB00454MeperidineAn opioid agonist with analgesic and sedative properties used to manage severe pain.
DB00333MethadoneAn opioid analgesic indicated for management of severe pain that is not responsive to alternative treatments. Also used to aid in detoxification and maintenance treatment of opioid addiction.
DB01192OxymorphoneAn opioid analgesic used in the management of moderate-to-severe pain and for analgesic therapies.
DB00327HydromorphoneAn opioid analgesic used to treat moderate to severe pain when the use of an opioid is indicated.
DB00295MorphineAn opioid agonist used for the relief of moderate to severe acute and chronic pain.
DB01535CarfentanilCarfentanil is similar (but more potent) to the opioid analgesic fentanyl. It is used as a tranquilizer for large animals.
DB00802AlfentanilAn opioid agonist used to induce and maintain anesthesia, as well as an analgesic.
DB00899RemifentanilAn opioid analgesic used in anesthesia.
DB00708SufentanilAn opioid used to induce and maintain anesthesia, to act as an analgesic in labor and delivery, and to treat severe, acute pain.
DrugDrug NameTargetType
DB00813FentanylMu-type opioid receptortarget
DB00813FentanylDelta-type opioid receptortarget
DB00813FentanylCytochrome P450 3A4enzyme
DB00813FentanylCytochrome P450 3A7enzyme
DB00813FentanylP-glycoprotein 1transporter
DB00813FentanylKappa-type opioid receptortarget
DB00813FentanylP-glycoprotein 1target
DB00813FentanylSerum albumincarrier
DB00813Fentanylalpha1-acid glycoproteincarrier
DB00454MeperidineKappa-type opioid receptortarget
DB00454MeperidineCytochrome P450 2D6enzyme
DB00454MeperidineCytochrome P450 2B6enzyme
DB00454MeperidineGlutamate receptor ionotropic, NMDA 1target
DB00454MeperidineGlutamate receptor ionotropic, NMDA 2Btarget
DB00454MeperidineGlutamate receptor ionotropic, NMDA 2Atarget
DB00454MeperidineGlutamate receptor ionotropic, NMDA 2Ctarget
DB00454MeperidineGlutamate receptor ionotropic, NMDA 2Dtarget
DB00454MeperidineCytochrome P450 2C19enzyme
DB00454MeperidineCytochrome P450 3A4enzyme
DB00454MeperidineSerum albumincarrier
DB00454MeperidineAlpha-1-acid glycoprotein 1carrier
DB00454MeperidineMuscarinic acetylcholine receptortarget
DB00454MeperidineMu-type opioid receptortarget
DB00454MeperidineSodium-dependent dopamine transportertarget
DB00454MeperidineSodium-dependent noradrenaline transportertarget
DB00454MeperidineSodium-dependent serotonin transportertarget
DB00454MeperidineLiver carboxylesterase 1target
DB00454MeperidineCytochrome P450 1A2enzyme
DB00333MethadoneNMDA receptortarget
DB00333MethadoneMu-type opioid receptortarget
DB00333MethadoneCytochrome P450 2B6enzyme
DB00333MethadoneCytochrome P450 3A4enzyme
DB00333MethadoneCytochrome P450 2C19enzyme
DB00333MethadoneDelta-type opioid receptortarget
DB00333MethadoneCytochrome P450 3A7enzyme
DB00333MethadoneCytochrome P450 2D6enzyme
DB00333MethadoneP-glycoprotein 1transporter
DB00333MethadoneCytochrome P450 2C8enzyme
DB00333MethadoneCytochrome P450 19A1enzyme
DB00333MethadoneCytochrome P450 1A2enzyme
DB00333MethadoneCytochrome P450 2C18enzyme
DB00333MethadoneCytochrome P450 2C9enzyme
DB00333Methadone5-hydroxytryptamine receptor 3Atarget
DB00333MethadoneAlpha-1-acid glycoprotein 1carrier
DB00333MethadoneSerum albumincarrier
DB00333MethadoneNeuronal acetylcholine receptor subunit alpha-7target
DB00333MethadoneNeuronal acetylcholine receptor subunit alpha-3target
DB00333MethadoneNeuronal acetylcholine receptor subunit alpha-4target
DB00333MethadoneNeuronal acetylcholine receptor subunit beta-2target
DB01192OxymorphoneMu-type opioid receptortarget
DB01192OxymorphoneCytochrome P450 2D6enzyme
DB01192OxymorphoneDelta-type opioid receptortarget
DB01192OxymorphoneCytochrome P450 3A4enzyme
DB00327HydromorphoneMu-type opioid receptortarget
DB00327HydromorphoneDelta-type opioid receptortarget
DB00327HydromorphoneKappa-type opioid receptortarget
DB00327HydromorphoneCytochrome P450 2C9enzyme
DB00327HydromorphoneUDP-glucuronosyltransferase 1-3enzyme
DB00327HydromorphoneUDP-glucuronosyltransferase 2B7enzyme
DB00327HydromorphoneSerum albumincarrier
DB00295MorphineMu-type opioid receptortarget
DB00295MorphineDelta-type opioid receptortarget
DB00295MorphineKappa-type opioid receptortarget
DB00295MorphineP-glycoprotein 1transporter
DB00295MorphineCytochrome P450 2C8enzyme
DB00295MorphineCytochrome P450 3A4enzyme
DB00295MorphineUDP-glucuronosyltransferase 2B7enzyme
DB00295MorphineUDP-glucuronosyltransferase 1-1enzyme
DB00295MorphineUDP-glucuronosyltransferase 1-8enzyme
DB00295MorphineUDP-glucuronosyltransferase 2B15enzyme
DB00295MorphineUDP-glucuronosyltransferase 2B4enzyme
DB00295MorphineUDP-glucuronosyltransferase 1-3enzyme
DB00295MorphineLymphocyte antigen 96target
DB00295MorphineSerum albumincarrier
DB01535CarfentanilMu-type opioid receptortarget
DB01535CarfentanilKappa-type opioid receptortarget
DB01535CarfentanilDelta-type opioid receptortarget
DB00802AlfentanilMu-type opioid receptortarget
DB00802AlfentanilCytochrome P450 3A4enzyme
DB00802AlfentanilCytochrome P450 3A5enzyme
DB00802AlfentanilAlpha-1-acid glycoprotein 1carrier
DB00802AlfentanilSerum albumincarrier
DB00802AlfentanilCytochrome P450 3A7enzyme
DB00802AlfentanilP-glycoprotein 1transporter
DB00899RemifentanilMu-type opioid receptortarget
DB00899RemifentanilDelta-type opioid receptortarget
DB00899RemifentanilKappa-type opioid receptortarget
DB00708SufentanilMu-type opioid receptortarget
DB00708SufentanilDelta-type opioid receptortarget
DB00708SufentanilKappa-type opioid receptortarget
DB00708SufentanilCytochrome P450 3A4enzyme