Opioid Dependence

Also known as: Opioid type dependence, unspecified use / Unspecified opioid dependence / Opiate Dependence / Dependence on opiates / Opioid type dependence

DrugDrug NameDrug Description
DB00921BuprenorphineBuprenorphine is a derivative of the opioid alkaloid thebaine that is a more potent (25 - 40 times) and longer lasting analgesic than morphine. It appears to act as a partial agonist at mu and kappa opioid receptors and as an antagonist at delta receptors. The lack of delta-agonist activity has been suggested to account for the observation that buprenorphine tolerance may not develop with chronic use.
DB01183NaloxoneNaloxone is an opioid antagonist medication used to block or reverse the effects of opioid drugs, particularly within the setting of drug overdoses which are rapidly becoming a leading cause of death worldwide. More specifically, naloxone has a high affinity for μ-opioid receptors, where it acts as an inverse agonist, causing the rapid removal of any other drugs bound to these receptors. When taken in large quantities, opioid medications such as morphine, hydromorphone, methadone, heroin, or fentanyl are capable of causing life-threatening symptoms such as respiratory depression, reduced heart rate, slurred speech, drowsiness, and constricted pupils. If untreated, this can progress to vomiting, absent pulse and breathing, loss of consciousness, and even death. Naloxone is indicated for the rapid reversal of these symptoms of central nervous system depression in opioid overdose. It's important to note that naloxone only works on opioid receptors within the body, and is therefore not capable of reversing the effects of non-opioid medications such as stimulants like methamphetamine or cocaine, or benzodiazepines like lorazepam or diazepam. Also known as the brand name product Narcan, naloxone is currently available by intramuscular (IM) or subcutaneous (SubQ) injection, nasal spray, or intravenous (IV) infusion. Naloxone IM injections are commonly available in the form of "kits", which is ideal for making overdose treatment accessible and readily available for administration by minimally trained individuals within the community. Kits commonly include the supplies necessary to treat an overdose in a non-medical setting such as alcohol swabs, syringes, a rescue breathing mask, and instructions for use. Frequently also carried by medical and emergency personnel and at events known to be associated with heavy drug use like music festivals, naloxone kits are considered a key component of harm reduction strategies. When injected intramuscularly (IM), naloxone acts within 3-5 minutes and can last from 30-60 minutes before its effects wear off. Administration of naloxone is associated with very few side effects. Notably, if injected into a person not currently using opioid medications, there would be no noticeable effects at all. However, for individuals using opioid medications or experiencing an overdose, IM injection of naloxone rapidly reverses opioid effects and can cause the injected individual to immediately experience withdrawal symptoms. Common symptoms of opioid withdrawal include nausea, vomiting, sweating, runny nose, aches, and diarrhea. Although certainly physically uncomfortable, opioid withdrawal symptoms are not life-threatening like they are for alcohol withdrawals. Administration of naloxone is therefore appropriate for any person appearing to have any symptoms of an opioid overdose. Due to its short duration of action, person's injected with naloxone should be monitored for responsiveness and potentially injected a second time or taken to the hospital. Naloxone is also available within the combination product Suboxone with the opioid medication buprenorphine. Suboxone is used for the maintentance treatment of opioid dependence and addiction. When taken orally, naloxone has no pharmacological effect and does not reduce the effectiveness of the opioid effect of buprenorphine. The primary purpose of including naloxone within Suboxone is to act as a deterrent to injection, as injected naloxone would rapidly reverse the effects of buprenorphine.
DB00704NaltrexoneDerivative of noroxymorphone that is the N-cyclopropylmethyl congener of naloxone. It is a narcotic antagonist that is effective orally, longer lasting and more potent than naloxone, and has been proposed for the treatment of heroin addiction. The FDA has approved naltrexone for the treatment of alcohol dependence.
DrugDrug NameTargetType
DB00921BuprenorphineKappa-type opioid receptortarget
DB00921BuprenorphineMu-type opioid receptortarget
DB00921BuprenorphineCytochrome P450 3A4enzyme
DB00921BuprenorphineCytochrome P450 2D6enzyme
DB00921BuprenorphineMultidrug resistance protein 1transporter
DB00921BuprenorphineATP-binding cassette sub-family G member 2transporter
DB00921BuprenorphineCytochrome P450 2C9enzyme
DB00921BuprenorphineCytochrome P450 3A5enzyme
DB00921BuprenorphineCytochrome P450 2C8enzyme
DB00921BuprenorphineCytochrome P450 3A7enzyme
DB00921BuprenorphineUDP-glucuronosyltransferase 1-9enzyme
DB00921BuprenorphineDelta-type opioid receptortarget
DB00921BuprenorphineCytochrome P450 1A2enzyme
DB00921BuprenorphineCytochrome P450 2A6enzyme
DB00921BuprenorphineCytochrome P450 2C18enzyme
DB00921BuprenorphineCytochrome P450 2C19enzyme
DB00921BuprenorphineNociceptin receptortarget
DB01183NaloxoneMu-type opioid receptortarget
DB01183NaloxoneEstrogen receptor alphatarget
DB01183NaloxoneCyclic AMP-responsive element-binding protein 1target
DB01183NaloxoneDelta-type opioid receptortarget
DB01183NaloxoneSolute carrier organic anion transporter family member 1A2transporter
DB01183NaloxoneMultidrug resistance protein 1transporter
DB01183NaloxoneKappa-type opioid receptortarget
DB01183NaloxoneCytochrome P450 2C8enzyme
DB01183NaloxoneCytochrome P450 3A4enzyme
DB01183NaloxoneSerum albumincarrier
DB01183NaloxoneToll-like receptor 4target
DB01183NaloxoneLiver carboxylesterase 1target
DB00704NaltrexoneMu-type opioid receptortarget
DB00704NaltrexoneKappa-type opioid receptortarget
DB00704NaltrexoneDelta-type opioid receptortarget
DB00704NaltrexoneMultidrug resistance protein 1transporter
DB00704NaltrexoneHCG20471, isoform CRA_ctarget
DB00704NaltrexoneUDP-glucuronosyltransferase 1-1enzyme
DrugDrug NamePhaseStatusCount
DB00107Oxytocin0Completed1
DB00673Aprepitant1Completed1
DB00921Buprenorphine1Completed1
DB00921Buprenorphine1Recruiting1
DB00327Hydromorphone1Completed1
DB04948Lofexidine1Completed3
DB00333Methadone1Completed1
DB01183Naloxone1Completed1
DB00704Naltrexone1Recruiting2
DB01273Varenicline1Completed1
DB00921Buprenorphine1 / 2Active Not Recruiting1
DB00921Buprenorphine1 / 2Completed1
DB00921Buprenorphine1 / 2Recruiting1
DB00575Clonidine1 / 2Completed1
DB00270Isradipine1 / 2Completed1
DB00295Morphine1 / 2Active Not Recruiting1
DB01183Naloxone1 / 2Completed1
DB01183Naloxone1 / 2Recruiting1
DB00704Naltrexone1 / 2Completed1
DB00107Oxytocin1 / 2Enrolling by Invitation1
DB00193Tramadol1 / 2Completed1
DB00921Buprenorphine2Completed2
DB00907Cocaine2Completed1
DB00822Disulfiram2Completed1
DB00996Gabapentin2Completed2
DB00741Hydrocortisone2Completed1
DB05266Ibudilast2Active Not Recruiting1
DB01202Levetiracetam2Completed1
DB00742Mannitol2Completed1
DB01043Memantine2Completed1
DB00333Methadone2Completed2
DB01183Naloxone2Completed2
DB00704Naltrexone2Active Not Recruiting1
DB00704Naltrexone2Completed1
DB00860Prednisolone2Terminated1
DB00297Bupivacaine2 / 3Not Yet Recruiting1
DB00921Buprenorphine2 / 3Recruiting1
DB00921Buprenorphine2 / 3Unknown Status1
DB00470Dronabinol2 / 3Completed1
DB00668Epinephrine2 / 3Not Yet Recruiting1
DB01043Memantine2 / 3Completed2
DB00333Methadone2 / 3Unknown Status1
DB01183Naloxone2 / 3Recruiting1
DB01183Naloxone2 / 3Unknown Status1
DB00704Naltrexone2 / 3Completed2
DB00921Buprenorphine3Active Not Recruiting1
DB00921Buprenorphine3Completed4
DB00921Buprenorphine3Enrolling by Invitation1
DB00921Buprenorphine3Terminated1
DB00921Buprenorphine3Withdrawn2
DB01156Bupropion3Not Yet Recruiting1
DB01452Heroin3Completed2
DB00327Hydromorphone3Completed1
DB04948Lofexidine3Completed1
DB00333Methadone3Completed3
DB00333Methadone3Not Yet Recruiting1
DB00295Morphine3Not Yet Recruiting1
DB01183Naloxone3Active Not Recruiting1
DB01183Naloxone3Completed1
DB01183Naloxone3Enrolling by Invitation1
DB01183Naloxone3Withdrawn2
DB00704Naltrexone3Active Not Recruiting1
DB11130Opium3Not Yet Recruiting1
DB00297Bupivacaine4Recruiting1
DB00921Buprenorphine4Completed2
DB00921Buprenorphine4Unknown Status1
DB06700Desvenlafaxine4Completed1
DB00996Gabapentin4Not Yet Recruiting1
DB00951Isoniazid4Not Yet Recruiting1
DB00333Methadone4Not Yet Recruiting1
DB01183Naloxone4Completed1
DB01183Naloxone4Unknown Status1
DB00704Naltrexone4Active Not Recruiting1
DB00704Naltrexone4Completed1
DB00704Naltrexone4Not Yet Recruiting1
DB01201Rifapentine4Not Yet Recruiting1
DB00813FentanylNot AvailableUnknown Status1
DB01017MinocyclineNot AvailableCompleted1
DB00704NaltrexoneNot AvailableCompleted1
DB00759TetracyclineNot AvailableCompleted1