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 Indication
DB00813FentanylFentanyl intravenous or intramuscular injections are indicated for short term analgesia during induction, maintenance, and recovery from general or regional anesthesia.[Label] These injections are also used with a neuroleptic for premedication, induction, and as an adjunct to maintenance of anesthesia.[Label] Finally, fentanyl intravenous or intramuscular injections are used with oxygen for anesthesia in high risk patients.[Label] Fentanyl sublingual tablets, transmucosal lozenges, buccal tablets, sublingual sprays, transdermal systems, and nasal sprays are indicated for the management of breakthrough pain in opioid tolerant cancer patients who require around the clock pain management.[L6598,L6601,L6604,L6607,L922,L6610]
DB00454MeperidineUsed to control moderate to severe pain.
DB00333MethadoneFor the treatment of dry cough, drug withdrawal syndrome, opioid type drug dependence, and pain.
DB01192OxymorphoneFor the treatment of moderate-to-severe pain.
DB00327HydromorphoneHydromorphone is indicated for the management of moderate to severe acute pain and severe chronic pain. Due to its addictive potential and overdose risk, hydromorphone is only prescribed when other first-line treatments have failed.[A176468] The WHO has proposed a three-step ladder for the management of pain in which it is suggested to start with a non-opioid medication followed by addition of weak opioids to the non-opioid treatment for moderate pain and finishing in the use of strong opioids such as hydromorphone along with the existing regimen for cases of severe pain.[A176471] Off-label, hydromorphone can be administered for the suppression of refractory cough.[A176468]
DB00295MorphineMorphine is used for the management of chronic moderate-to-severe pain.[A176050] Opioids, including morphine, can manage pain effectively when used for a short amount of time. The use of opioids for longer periods needs to be monitored as they can develop a physical dependence, addiction disorder and drug abuse.[L5728]
DB01535CarfentanilCarfentanil is similar (but more potent) to the opioid analgesic fentanyl. It is used as a tranquilizer for large animals.
DB00802AlfentanilFor the management of postoperative pain and the maintenance of general anesthesia.
DB00899RemifentanilFor use during the induction and maintenance of general anesthesia.
DB00708SufentanilThe indications for this drug are as follows: 1. As an analgesic adjunct in the maintenance of balanced general anesthesia in patients who are intubated and ventilated. 2. As a primary anesthetic agent for the induction and maintenance of anesthesia with 100% oxygen in patients undergoing major surgical procedures, in patients who are intubated and ventilated, such as cardiovascular surgery or neurosurgical procedures in the sitting position, to provide favorable myocardial and cerebral oxygen balance or when extended postoperative ventilation is anticipated. 3. For epidural administration as an analgesic combined with low dose (usually 12.5 mg per administration) bupivacaine usually during labor and vaginal delivery 4. The sublingual form is indicated for the management of acute pain in adults that is severe to warrant the use of an opioid analgesic in certified medically supervised healthcare settings, including hospitals, surgical centers, and emergency departments. [FDA label]
DrugDrug NameTargetType
DB00813FentanylMu-type opioid receptortarget
DB00813FentanylDelta-type opioid receptortarget
DB00813FentanylCytochrome P450 3A4enzyme
DB00813FentanylCytochrome P450 3A5enzyme
DB00813FentanylCytochrome P450 3A7enzyme
DB00813FentanylMultidrug resistance protein 1transporter
DB00813FentanylKappa-type opioid receptortarget
DB00813FentanylMultidrug resistance protein 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
DB00333MethadoneGlutamate receptor ionotropic, NMDA 3Atarget
DB00333MethadoneMu-type opioid receptortarget
DB00333MethadoneNeuronal acetylcholine receptor subunit alpha-10target
DB00333MethadoneCytochrome P450 2B6enzyme
DB00333MethadoneCytochrome P450 3A4enzyme
DB00333MethadoneCytochrome P450 2C19enzyme
DB00333MethadoneDelta-type opioid receptortarget
DB00333MethadoneCytochrome P450 3A5enzyme
DB00333MethadoneCytochrome P450 3A7enzyme
DB00333MethadoneCytochrome P450 2D6enzyme
DB00333MethadoneMultidrug resistance protein 1transporter
DB00333MethadoneCytochrome P450 2C8enzyme
DB00333MethadoneCytochrome P450 19A1enzyme
DB00333MethadoneCytochrome P450 1A2enzyme
DB00333MethadoneCytochrome P450 2C18enzyme
DB00333MethadoneCytochrome P450 2C9enzyme
DB00333Methadone5-hydroxytryptamine receptor 3Atarget
DB00333MethadoneLymphocyte antigen 96target
DB00333MethadoneAlpha-1-acid glycoprotein 2target
DB00333MethadoneThyroxine-binding globulincarrier
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 3A4enzyme
DB00327HydromorphoneCytochrome P450 2C9enzyme
DB00327HydromorphoneUDP-glucuronosyltransferase 1-3enzyme
DB00327HydromorphoneUDP-glucuronosyltransferase 2B7enzyme
DB00327HydromorphoneSerum albumincarrier
DB00295MorphineMu-type opioid receptortarget
DB00295MorphineDelta-type opioid receptortarget
DB00295MorphineKappa-type opioid receptortarget
DB00295MorphineCytochrome P450 2D6enzyme
DB00295MorphineMultidrug resistance protein 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
DB00802AlfentanilMultidrug resistance protein 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