Buprenorphine - Wikipedia Buprenorphine Buprenorphine Clinical data Trade names Subutex, others AHFS / Drugs.com Monograph MedlinePlus a605002 License data EU EMA : by INN Pregnancy category AU : C US : C ( Risk not ruled out ) Routes of administration Under the tongue, through the cheek, IM, transdermal, intranasal, rectally, by mouth ATC code N02AE01 ( WHO ) N07BC01 ( WHO ) Legal status Legal status AU : S8 ( Controlled ) CA : Schedule I DE : Anlage III ( Special prescription form required ) UK : Class C US : Schedule III Pharmacokinetic data Bioavailability Sublingual : 30 % Intranasal : 48 % Protein binding 96 % Metabolism Liver ( CYP3A4, CYP2C8 ) Onset of action Within 30 min Elimination half - life 37 hours ( range 20 -- 70 hours ) Duration of action Up to 24 hrs Excretion Biliary and kidney Identifiers IUPAC name ( 2S ) - 2 - ( ( 5R, 6R, 7R, 14S ) - 17 - cyclopropylmethyl - 4, 5 - epoxy - 6, 14 - ethano - 3 - hydroxy - 6 - methoxymorphinan - 7 - yl ) - 3, 3 - dimethylbutan - 2 - ol CAS Number 52485 - 79 - 7 PubChem CID 644073 IUPHAR / BPS 1670 DrugBank DB00921 ChemSpider 559124 UNII 40D3SCR4GZ KEGG D07132 ChEBI CHEBI : 3216 ChEMBL CHEMBL511142 ECHA InfoCard 100.052. 664 Chemical and physical data Formula C H NO Molar mass 467.64 g / mol 3D model ( JSmol ) Interactive image SMILES Oc7ccc5c1c7O ( C@H ) 3 ( C @ ) 6 ( OC ) ( C@H ) ( C ( C @ @ ) 2 ( ( C@H ) ( N ( CC ( C @ @ ) 123 ) CC4CC4 ) C5 ) CC6 ) ( C @ @ ) ( O ) ( C ) C ( C ) ( C ) C InChI InChI = 1S / C29H41NO4 / c1 - 25 ( 2, 3 ) 26 ( 4, 32 ) 20 - 15 - 27 - 10 - 11 - 29 ( 20, 33 - 5 ) 24 - 28 ( 27 ) 12 - 13 - 30 ( 16 - 17 - 6 - 7 - 17 ) 21 ( 27 ) 14 - 18 - 8 - 9 - 19 ( 31 ) 23 ( 34 - 24 ) 22 ( 18 ) 28 / h8 - 9, 17, 20 - 21, 24, 31 - 32H, 6 - 7, 10 - 16H2, 1 - 5H3 / t20 -, 21 -, 24 -, 26 +, 27 -, 28 +, 29 - / m1 / s1 Key : RMRJXGBAOAMLHD - IHFGGWKQSA - N ( what is this ? ) ( verify ) Buprenorphine, sold under the brand name Subutex, among others, is an opioid used to treat opioid addiction, acute pain, and chronic pain. It can be used under the tongue, by injection, as a skin patch, or as an implant. For opioid addiction it is typically only started when withdrawal symptoms have begun and for the first two days of treatment under direct observation of a health care provider. For longer term treatment of addiction a combination formulation of buprenorphine / naloxone is recommended to prevent misuse by injection. Maximum pain relief is generally within an hour with effects up to 24 hours. Side effects may include respiratory depression ( decreased breathing ), sleepiness, adrenal insufficiency, QT prolongation, low blood pressure, allergic reactions, and opioid addiction. Among those with a history of seizures, there is a risk of further seizures. Opioid withdrawal following stopping buprenorphine is generally less severe than with other opioids. It is unclear if use during pregnancy is safe and use while breastfeeding is not recommended. Buprenorphine affects different types of opioid receptors in different ways. Depending on the type of receptor it may be an agonist, partial agonist, or antagonist. Buprenorphine was approved for medical use in the United States in 1981. In 2012, 9.3 million prescriptions for the medication were written in the United States. Buprenorphine may also be used recreationally by injection or in the nose for the high it produces. Occasionally it is used recreationally instead of heroin. In the United States it is a Schedule III controlled substance. For the tablets the wholesale cost in the United States is between US $ 0.86 and US $ 1.32 per daily dose as of 2017. Contents 1 Medical uses 1.1 Opioid addiction 1.1. 1 Buprenorphine versus methadone 1.2 Chronic pain 2 Adverse effects 2.1 Respiratory effects 2.2 Buprenorphine dependence 2.3 Pain management 3 Pharmacology 3.1 Pharmacodynamics 3.1. 1 Opioid receptor modulator 3.1. 2 Other actions 3.2 Pharmacokinetics 4 Chemistry 4.1 Detection in body fluids 5 History 6 Society and culture 6.1 Regulation 6.2 Brand names 7 Veterinary medicine 8 Research 8.1 Depression 8.2 Cocaine dependence 8.3 Neonatal abstinence 8.4 Obsessive -- compulsive disorder 9 References 10 External links Medical uses Opioid addiction Its primary use is for the initial treatment of those with opioid addiction. It should only be started once symptoms of withdrawal have begun. For longer term treatment of addiction a combination formulation of buprenorphine / naloxone is usually recommended. A once a month injection, sold under the brandname Sublocade, has been approved in the United States and it should be available in 2018. Buprenorphine versus methadone Both buprenorphine and methadone are medications used for detoxification, short - and long - term opioid replacement therapy. Effectiveness of buprenorphine and methadone appear similar, with similar side effects. Buprenorphine may have less respiratory depression in cases of abuse. Chronic pain Butrans patches in the pouch with packaging. A removed patch is shown on the left. A transdermal patch is available for the treatment of chronic pain. These patches are not indicated for use in acute pain, pain that is expected to last only for a short period of time, or pain after surgery, nor are they recommended for opioid addiction. Adverse effects A 2007 assessment of harm from recreational drug use ( mean physical harm and mean dependence liability ). Buprenorphine was ranked 9th in dependence, 8th in physical harm, and 11th in social harm. Common adverse drug reactions associated with the use of buprenorphine are similar to those of other opioids and include : nausea and vomiting, drowsiness, dizziness, headache, memory loss, cognitive and neural inhibition, perspiration, itchiness, dry mouth, shrinking of the pupils of the eyes ( miosis ), orthostatic hypotension, male ejaculatory difficulty, decreased libido, and urinary retention. Constipation and CNS effects are seen less frequently than with morphine. Allergic contact dermatitis from buprenorphine patch ( few days after removal ) Respiratory effects The most severe side effect associated with buprenorphine is respiratory depression ( insufficient breathing ). It occurs more often in those who are also taking benzodiazepines, alcohol, or have underlying lung disease. The usual reversal agents for opioids, such as naloxone, may be only partially effective and additional efforts to support breathing may be required. Respiratory depression may be less than with other opioids, particularly with chronic use. However, in the setting of acute pain management, buprenorphine appears to cause the same rate of respiratory depression as other opioids such as morphine Buprenorphine dependence Buprenorphine treatment carries the risk of causing psychological or physical dependence. Buprenorphine has a slow onset and a long half - life of 24 to 60 hours. Once a person has stabilized on the medication, there are three options : continual use, switching to buprenorphine / naloxone, or medically supervised withdrawal. Pain Management It is difficult to achieve acute opioid analgesia in persons using buprenorphine for opioid replacement therapy. Pharmacology Pharmacodynamics Buprenorphine Site K ( nM ) Action Species Ref MOR 0.21 -- 1.5 0.081 Partial agonist Human Monkey DOR 2.9 -- 6.1 0.82 Antagonist Human Monkey KOR 0.62 -- 2.5 0.44 Antagonist Human Monkey NOP 77.4 Partial agonist Human σ > 100,000 ND ND σ ND ND ND ND NMDA ND ND ND ND TLR4 > 10,000 Agonist Human SERT > 100,000 ND Rat NET > 100,000 ND Rat DAT ND ND ND ND VGSC 33,000 ( IC ) Inhibitor Rodent Values are K ( nM ), unless otherwise noted. The smaller the value, the more strongly the drug binds to the site. Opioid receptor modulator Buprenorphine has been reported to possess the following pharmacological activity : μ - Opioid receptor ( MOR ) : Partial agonist. Binds with high affinity, but only partially activates the receptor. This property allows buprenorphine to act similarly to full opioid agonists at lower doses ( mainly in non-tolerant individuals ), reaching a ceiling / plateau at higher doses after which there is no further increase in typical opioid effects ( theraputic or recreational ). This behavior is responsible for buprenorphine 's ability to block most MOR agonists and the phenomenon of withdrawal effects when used in actively opioid dependent persons. κ - Opioid receptor ( KOR ) : Antagonist. δ - Opioid receptor ( DOR ) : Antagonist. Nociceptin receptor ( NOP, ORL - 1 ) : Weak affinity. Very weak partial agonist. May be involved in lack of respiratory depression with buprenorphine in overdose. In simplified terms, buprenorphine can essentially be thought of as a non-selective, mixed agonist -- antagonist opioid receptor modulator, acting as a weak partial agonist of the MOR, an antagonist of the KOR, an antagonist of the DOR, and a relatively low - affinity, very weak partial agonist of the ORL - 1. Although buprenorphine is a partial agonist of the MOR, human studies have found that it acts like a full agonist with respect to analgesia in non-opioid - tolerant individuals. Conversely, buprenorphine behaves like a partial agonist of the MOR with respect to respiratory depression. Buprenorphine is also known to bind to with high affinity and antagonize the putative ε - opioid receptor. Full analgesic efficacy of buprenorphine requires both exon 11 - and exon 1 - associated μ - opioid receptor splice variants. The active metabolites of buprenorphine are not thought to be clinically important in its central nervous system effects. Other actions Unlike some other opioids and opioid antagonists, buprenorphine binds only weakly to and possesses little if any activity at the sigma receptor. Buprenorphine also blocks voltage - gated sodium channels via the local anesthetic binding site, and this underlies its potent local anesthetic properties. Similarly to various other opioids, buprenorphine has also been found to act as an agonist of the toll - like receptor 4, albeit with very low affinity. Pharmacokinetics Buprenorphine is metabolized by the liver, via CYP3A4 ( also CYP2C8 seems to be involved ) isozymes of the cytochrome P450 enzyme system, into norbuprenorphine ( by N - dealkylation ). The glucuronidation of buprenorphine is primarily carried out by UGT1A1 and UGT2B7, and that of norbuprenorphine by UGT1A1 and UGT1A3. These glucuronides are then eliminated mainly through excretion into bile. The elimination half - life of buprenorphine is 20 to 73 hours ( mean 37 hours ). Due to the mainly hepatic elimination, there is no risk of accumulation in people with renal impairment. One of the major active metabolites of buprenorphine is norbuprenorphine, which, in contrast to buprenorphine itself, is a full agonist of the MOR, DOR, and ORL - 1, and a partial agonist at the KOR. However, relative to buprenorphine, norbuprenorphine has extremely little antinociceptive potency ( 1 / 50th that of buprenorphine ), but markedly depresses respiration ( 10-fold more than buprenorphine ). This may be explained by very poor brain penetration of norbuprenorphine due to a high affinity of the compound for P - glycoprotein. In contrast to norbuprenorphine, buprenorphine and its glucuronide metabolites are negligibly transported by P - glycoprotein. The glucuronides of buprenorphine and norbuprenorphine are also biologically active, and represent major active metabolites of buprenorphine. Buprenorphine - 3 - glucuronide has affinity for the MOR ( K = 4.9 pM ), DOR ( K = 270 nM ) and ORL - 1 ( K = 36 μM ), and no affinity for the KOR. It has a small antinociceptive effect and no effect on respiration. Norbuprenorphine - 3 - glucuronide has no affinity for the MOR or DOR, but does bind to the KOR ( K = 300 nM ) and ORL - 1 ( K = 18 μM ). It has a sedative effect but no effect on respiration. Chemistry Buprenorphine is a semi-synthetic analogue of thebaine and is fairly soluble in water, as its hydrochloride salt. It degrades in the presence of light. Detection in body fluids Buprenorphine and norbuprenorphine may be quantitated in blood or urine to monitor use or abuse, confirm a diagnosis of poisoning, or assist in a medicolegal investigation. There is a significant overlap of drug concentrations in body fluids within the possible spectrum of physiological reactions ranging from asymptomatic to comatose. Therefore, it is critical to have knowledge of both the route of administration of the drug and the level of tolerance to opioids of the individual when results are interpreted. History In 1969, researchers at Reckitt & Colman ( now Reckitt Benckiser ) had spent 10 years attempting to synthesize an opioid compound `` with structures substantially more complex than morphine ( that ) could retain the desirable actions whilst shedding the undesirable side effects ''. Physical dependence and withdrawal from buprenorphine itself remain important issues since buprenorphine is a long - acting opioid. Reckitt found success when researchers synthesized RX6029 which had showed success in reducing dependence in test animals. RX6029 was named buprenorphine and began trials on humans in 1971. By 1978, buprenorphine was first launched in the UK as an injection to treat severe pain, with a sublingual formulation released in 1982. Society and culture Regulation In the United States, buprenorphine ( Subutex ) and buprenorphine with naloxone ( Suboxone ) were approved for opioid addiction by the United States Food and Drug Administration in October 2002. The FDA rescheduled buprenorphine from a Schedule V drug to a Schedule III drug just before approval of Subutex and Suboxone. The ACSCN for buprenorphine is 9064, and being a Schedule III substance it does not have an annual manufacturing quota imposed by the DEA. The salt in use is the hydrochloride, which has a free base conversion ratio of 0.928. In the years prior to Suboxone 's approval, Reckitt Benckiser had lobbied Congress to help craft the Drug Addiction Treatment Act of 2000 ( DATA 2000 ), which gave authority to the Secretary of Health and Human Services to grant a waiver to physicians with certain training to prescribe and administer Schedule III, IV, or V narcotic drugs for the treatment of addiction or detoxification. Prior to the passage of this law, such treatment was not permitted in outpatient settings except for clinics designed specifically for drug addiction. The waiver, which can be granted after the completion of an eight - hour course, is required for outpatient treatment of opioid addiction with Subutex and Suboxone. Initially, the number of patients each approved physician could treat was limited to ten. This was eventually modified to allow approved physicians to treat up to a hundred patients with buprenorphine for opioid addiction in an outpatient setting. This limit was recently increased by the Obama administration, raising the number of patients to which doctors can prescribe to 275. Still, due to this patient limit and the requisite eight - hour training course, many continuing patients can find it very difficult to get a prescription, despite the drug 's effectiveness. In the European Union, Subutex and Suboxone, buprenorphine 's high - dose sublingual tablet preparations, were approved for opioid addiction treatment in September 2006. In the Netherlands, buprenorphine is a List II drug of the Opium Law, though special rules and guidelines apply to its prescription and dispensation. Brand names Buprenorphine is available under the trade names Cizdol, Suboxone, Subutex ( typically used for opioid addiction ), Temgesic ( sublingual tablets for moderate to severe pain ), Buprenex ( solutions for injection often used for acute pain in primary - care settings ), Norspan and Butrans ( transdermal preparations used for chronic pain ). Buprenorphine has been introduced in most European countries as a transdermal formulation ( marketed as Transtec ) for the treatment of chronic pain not responding to non-opioids. Veterinary Medicine It has veterinary medical use for treatment of pain in dogs and cats. Research Depression Some evidence supports the use of buprenorphine for depression. Buprenorphine / samidorphan, a combination product of buprenorphine and samidorphan ( a preferential μ - opioid receptor antagonist ), appears useful for treatment - resistant depression. Cocaine dependence In combination with samidorphan or naltrexone ( μ - opioid receptor antagonists ), buprenorphine is under investigation for the treatment of cocaine dependence, and recently demonstrated effectiveness for this indication in a large - scale ( n = 302 ) clinical trial ( at a high buprenorphine dose of 16 mg but not a low dose of 4 mg ). Neonatal abstinence Buprenorphine has been used in the treatment of the neonatal abstinence syndrome, a condition in which newborns exposed to opioids during pregnancy demonstrate signs of withdrawal. Use currently is limited to infants enrolled in a clinical trial conducted under an FDA approved investigational new drug ( IND ) application. 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External links U.S. Federal government buprenorphine program for opioid addiction Australian national buprenorphine policy `` The bitter pill '' : A Wired magazine article on Suboxone `` Subu Must Die -- How a nation of junkies went cold turkey '' : A New Republic article on Subutex abuse in the nation of Georgia ) Analgesics ( N02A, N02B ) Opioids Opiates / opium Codeine ( + paracetamol, + aspirin ) Morphine ( + naltrexone ) Opium Laudanum Paregoric Semisynthetic Acetyldihydrocodeine Benzylmorphine Buprenorphine ( + naloxone ) Desomorphine Diamorphine ( heroin ) Dihydrocodeine ( + paracetamol ) Dihydromorphine Ethylmorphine Hydrocodone ( + paracetamol, + ibuprofen, + aspirin ) Hydromorphinol Hydromorphone Nicocodeine Nicodicodeine Nicomorphine Oxycodone ( + paracetamol, + aspirin, + ibuprofen, + naloxone, + naltrexone ) Oxymorphone Thebacon Synthetic Alfentanil Alphaprodine Anileridine Butorphanol Carfentanil Dextromoramide Dextropropoxyphene Dezocine Fentanyl ( + fluanisone ) Ketobemidone Levorphanol Lofentanil Meptazinol Methadone Nalbuphine NFEPP Pentazocine Pethidine ( meperidine ) Phenadoxone Phenazocine Piminodine Piritramide Propiram Remifentanil Sufentanil Tapentadol Tilidine Tramadol Paracetamol - type Acetanilide Bucetin Butacetin Paracetamol ( acetaminophen ) Parapropamol Phenacetin Propacetamol NSAIDs Propionates Fenoprofen Flurbiprofen Ibuprofen Ketoprofen Naproxen Oxaprozin Oxicams Meloxicam Piroxicam Acetates Diclofenac Indometacin Ketorolac Nabumetone Sulindac Tolmetin COX - 2 inhibitors Celecoxib Etoricoxib Lumiracoxib Parecoxib Rofecoxib Valdecoxib Fenamates Meclofenamic acid Mefenamic acid Salicylates Aspirin ( acetylsalicylic acid ) ( + paracetamol / caffeine ) Benorylate Diflunisal Ethenzamide Magnesium salicylate Salicin Salicylamide Salsalate Wintergreen ( methyl salicylate ) Pyrazolones Aminophenazone Ampyrone Metamizole ( dipyrone ) Nifenazone Phenazone Propyphenazone ( + paracetamol / caffeine ) Others Glafenine Cannabinoids Cannabidiol Cannabis Nabilone Nabiximols Tetrahydrocannabinol ( dronabinol ) Ion channel modulators Calcium blockers Gabapentin Gabapentin enacarbil Pregabalin Ziconotide Sodium blockers Carbamazepine Lacosamide Local anesthetics ( e.g., cocaine, lidocaine ) Mexiletine Nefopam Tricyclic antidepressants ( e.g., amitriptyline ) Na 1.7 / 1.8 - selective : DSP - 2230 Funapide PF - 05089771 Potassium openers Flupirtine Myorelaxants Carisoprodol Chlorzoxazone Cyclobenzaprine Mephenoxalone Methocarbamol Orphenadrine Others Analgesic adjuvant Analgecine Camphor Capsaicin Clonidine Ketamine Menthol Methoxyflurane Nefopam Proglumide Tricyclic antidepressants ( e.g., amitriptyline ) WHO - EM Withdrawn from market Clinical trials : Phase III Never to phase III Treatment of drug dependence ( N07B ) Nicotine dependence Bupropion Cytisine Lobeline Mecamylamine Varenicline AA ( Clonidine ) Alcohol dependence AD inhibitor ( Disulfiram Calcium carbimide Hydrogen cyanamide ) Acamprosate Opioid antagonists ( Naltrexone Nalmefene ) Topiramate AA ( Clonidine ) Baclofen Metadoxine Phenibut Opioid dependence AA ( Clonidine Lofexidine ) Ibogaine Opioids Buprenorphine ( + naloxone ) Levacetylmethadol Methadone Dihydrocodeine Dihydroetorphine Hydromorphone ( extended - release ) Morphine ( extended - release ) Opioid antagonists ( Naltrexone Nalmefene ) Benzodiazepine dependence AA ( Clonidine ) Benzodiazepines ( Diazepam Lorazepam Chlordiazepoxide Oxazepam ) Barbiturates ( Phenobarbital ) Research Salvia divinorum Antidepressants ( N06A ) hide Specific reuptake inhibitors and / or receptor modulators SSRIs Citalopram Escitalopram Fluoxetine Fluvoxamine Indalpine Paroxetine Sertraline Zimelidine SNRIs Desvenlafaxine Duloxetine Levomilnacipran Milnacipran Tofenacin Venlafaxine NRIs Atomoxetine Reboxetine Viloxazine NDRIs Amineptine Bupropion Nomifensine NaSSAs Mianserin Mirtazapine Setiptiline SARIs Etoperidone Nefazodone Trazodone SMS Vilazodone Vortioxetine Others Agomelatine Amisulpride Esketamine Etryptamine Indeloxazine flupentixol Ketamine Medifoxamine Metryptamine Oxaflozane Pivagabine Tandospirone Teniloxazine Tianeptine hide Tricyclic and tetracyclic antidepressants TCAs Amineptine Amitriptyline Amitriptylinoxide Butriptyline Clomipramine Demexiptiline Desipramine Dibenzepin Dimetacrine Dosulepin Doxepin Imipramine Imipraminoxide Iprindole Lofepramine Melitracen Metapramine Nitroxazepine Nortriptyline Noxiptiline Opipramol Pipofezine Propizepine Protriptyline Quinupramine Tianeptine Trimipramine TeCAs Amoxapine Maprotiline Mianserin Mirtazapine Setiptiline Others Tiazesim hide Monoamine oxidase inhibitors Non-selective Irreversible : Benmoxin Iproclozide Iproniazid Isocarboxazid Isoniazid Linezolid Mebanazine Nialamide Octamoxin Phenelzine Pheniprazine Phenoxypropazine Pivhydrazine Safrazine Tedizolid Tranylcypromine Reversible : Caroxazone Mixed : Bifemelane MAO - selective Reversible : Eprobemide Metralindole Minaprine Moclobemide Pirlindole Tetrindole Toloxatone MAO - selective Irreversible : Selegiline hide Adjunctive therapies Atypical antipsychotics ( aripiprazole, brexpiprazole, lurasidone, olanzapine, quetiapine, risperidone ) Buspirone Lithium ( lithium carbonate, lithium citrate ) Thyroid hormones ( triiodothyronine ( T ), levothyroxine ( T ) ) hide Miscellaneous Ademetionine ( SAMe ) Hypericum perforatum ( St. John 's Wort ) Oxitriptan ( 5 - HTP ) Rubidium chloride ( RbCl ) Tryptophan WHO - EM Withdrawn from market Clinical trials : Phase III Never to phase III Opioid receptor modulators MOR Agonists ( abridged ; see here for a full list ) : 3 - HO - PCP 7 - Acetoxymitragynine 7 - Hydroxymitragynine ψ - Akuammigine α - Chlornaltrexamine α - Narcotine Acetyldihydrocodeine Acetylfentanyl Acrylfentanyl Adrenorphin ( metorphamide ) AH - 7921 Akuammicine Akuammidine Alfentanil Anileridine Apparicine β - Endorphin BAM - 12P BAM - 18P BAM - 22P Benzhydrocodone Benzylmorphine Bezitramide Biphalin BU08070 Buprenorphine Butorphan Butorphanol Butyrfentanyl BW - 373U86 Carfentanil Casokefamide Cebranopadol Chloroxymorphamine Codeine DADLE DAMGO ( DAGO ) Dermorphin Desmetramadol ( desmethyltramadol ) Desomorphine Dextromoramide Dextropropoxyphene ( propoxyphene ) Dezocine Dimenoxadol Dimethylaminopivalophenone Eluxadoline Diamorphine ( heroin ) Dihydrocodeine Dihydroetorphine Dihydromorphine Dinalbuphine sebacate Diphenoxylate Dipipanone Dynorphin A Embutramide Endomorphin - 1 Endomorphin - 2 Eseroline Ethylmorphine Etorphine Fentanyl Fluorophen Frakefamide Furanylfentanyl Hemorphin - 4 Herkinorin Hodgkinsine Hydrocodone Hydromorphinol Hydromorphone IBNtxA Ketamine Ketobemidone Kratom Laudanosine Lefetamine Leu - enkephalin Levacetylmethadol Levomethorphan Levorphanol Lexanopadol Loperamide Loxicodegol Matrine Meptazinol Met - enkephalin ( metenkefalin ) Methadone Metkefamide Metopon Mitragynine Mitragynine pseudoindoxyl Morphiceptin Morphine Nalbuphine NalBzOH Nalmexone Naltalimide Neopine NFEPP Nicocodeine Nicodicodeine Nicomorphine NKTR - 181 Norketamine Octreotide Oliceridine OM - 3 - MNZ Oripavine Oxycodone Oxymorphazone Oxymorphonazine Oxymorphone Oxymorphone phenylhydrazone OxyPNPH Papaver somniferum ( opium ) Pentazocine Pericine Pethidine ( meperidine ) Phenazocine Phencyclidine Piminodine Piritramide PL - 017 Prodine Propiram PZM21 Racemethorphan Racemorphan Remifentanil Salsolinol SC - 17599 Sinomenine Sufentanil Tapentadol Tetrahydropapaveroline TH - 030418 Thebaine Thienorphine Tianeptine Tilidine Tramadol Trimebutine TRIMU 5 TRV734 Tubotaiwine U-47700 Valorphin Viminol Xorphanol PAMs : BMS - 986121 BMS - 986122 Antagonists : ( 3S, 4S ) - Picenadol 2 - ( S ) - N, N - ( R ) - Viminol 3CS - nalmefene 4 - Caffeoyl - 1, 5 - quinide 4 ′ - Hydroxyflavanone 4 ', 7 - Dihydroxyflavone 6β - Naltrexol 6β - Naltrexol - d4 18 - MC α - Gliadin β - Chlornaltrexamine β - Funaltrexamine Akuammine Alvimopan AM - 251 Apigenin AT - 076 Axelopran Bevenopran Catechin Catechin gallate Clocinnamox CTAP CTOP Cyclofoxy Cyprodime Diacetylnalorphine Diprenorphine ECG EGC Epicatechin Eptazocine Gemazocine Ginsenoside R Hyperoside Ibogaine Levallorphan Lobeline LY - 255582 LY - 2196044 Methocinnamox Methylnaltrexone Methylsamidorphan chloride Naldemedine Nalmefene Nalodeine ( N - allylnorcodeine ) Nalorphine Nalorphine dinicotinate Naloxazone Naloxegol Naloxol Naloxonazine Naloxone Naltrexazone Naltrexonazine Naltrexone Naltrindole Naringenin Noribogaine Oxilorphan Pawhuskin A Rimonabant Quadazocine Samidorphan Taxifolin Unknown / unsorted : Cannabidiol Coronaridine Cyproterone acetate Dihydroakuuamine Tabernanthine Tetrahydrocannabinol DOR Agonists : 3CS - nalmefene 6 ' - GNTI 7 - SIOM ADL - 5747 ( PF - 04856881 ) ADL - 5859 Alazocine ( SKF - 10047 ) Amoxapine AR - M100390 ( ARM390 ) AZD2327 β - Endorphin BAM - 18P Biphalin BU - 48 Butorphan Butorphanol BW - 373U86 Casokefamide Cebranopadol Codeine Cyclazocine DADLE Deltorphin A Deltorphin I Deltorphin II Desmethylclozapine Desmetramadol ( desmethyltramadol ) Dezocine Diamorphine ( heroin ) Dihydroetorphine Dihydromorphine DPDPE DPI - 221 DPI - 3290 DSLET Ethylketazocine Etorphine Fentanyl FIT Fluorophen Hemorphin - 4 Hydrocodone Hydromorphone Ibogaine Isomethadone JNJ - 20788560 KNT - 127 Kratom Laudanosine Leu - enkephalin Levomethorphan Levorphanol Lexanopadol Lofentanil Met - enkephalin ( metenkefalin ) Metazocine Metkefamide Mitragynine Mitragynine pseudoindoxyl Morphine N - Phenethyl - 14 - ethoxymetopon Norbuprenorphine NalBzOH Oripavine Oxycodone Oxymorphone Pethidine ( meperidine ) Proglumide Racemethorphan Racemorphan RWJ - 394674 Samidorphan SB - 235863 SNC - 80 SNC - 162 TAN - 67 ( SB - 205,607 ) TH - 030418 Thebaine Thiobromadol ( C - 8813 ) Tonazocine Tramadol TRV250 Xorphanol Zenazocine Antagonists : 4 ', 7 - Dihydroxyflavone 5 ' - NTII 6β - Naltrexol 6β - Naltrexol - d4 α - Santolol β - Chlornaltrexamine Apigenin AT - 076 Axelopran Bevenopran BNTX Catechin Catechin gallate Clocinnamox Diacetylnalorphine Diprenorphine ECG EGC Eluxadoline Epicatechin ICI - 154129 ICI - 174864 LY - 255582 LY - 2196044 Methylnaltrexone Methylnaltrindole N - Benzylnaltrindole Nalmefene Nalorphine Naltrexone Naltriben Naltrindole Naloxone Naringenin Noribogaine Pawhuskin A Quadazocine SDM25N SoRI - 9409 Taxifolin Thienorphine Unknown / unsorted : 18 - MC Cannabidiol Coronaridine Cyproterone acetate Tabernanthine Tetrahydrocannabinol KOR Agonists : 3CS - nalmefene 6 ' - GNTI 8 - CAC 18 - MC 14 - Methoxymetopon β - Chlornaltrexamine β - Funaltrexamine Adrenorphin ( metorphamide ) Akuuamicine Alazocine ( SKF - 10047 ) Allomatrine Apadoline Asimadoline BAM - 12P BAM - 18P BAM - 22P Big dynorphin Bremazocine BRL - 52537 Butorphan Butorphanol BW - 373U86 Cebranopadol Ciprefadol CR665 Cyclazocine Cyclorphan Cyprenorphine Desmetramadol ( desmethyltramadol ) Diamorphine ( heroin ) Diacetylnalorphine Difelikefalin Dihydroetorphine Dihydromorphine Dinalbuphine sebacate Diprenorphine Dynorphin A Dynorphin B ( rimorphin ) Eluxadoline Enadoline Eptazocine Erinacine E Ethylketazocine Etorphine Fedotozine Fentanyl Gemazocine GR - 89696 GR - 103545 Hemorphin - 4 Herkinorin HS665 Hydromorphone HZ - 2 Ibogaine ICI - 199,441 ICI - 204,448 Ketamine Ketazocine Laudanosine Leumorphin ( dynorphin B - 29 ) Levallorphan Levomethorphan Levorphanol Lexanopadol Lofentanil LPK - 26 Lufuradom Matrine MB - 1C - OH Menthol Metazocine Metkefamide Mianserin Mirtazapine Morphine Moxazocine MR - 2034 N - MPPP Nalbuphine NalBzOH Nalfurafine Nalmefene Nalodeine ( N - allylnorcodeine ) Nalorphine Naltriben Niravoline Norbuprenorphine Norbuprenorphine - 3 - glucuronide Noribogaine Norketamine Oripavine Oxilorphan Oxycodone Pentazocine Pethidine ( meperidine ) Phenazocine Proxorphan Racemethorphan Racemorphan RB - 64 Salvinorin A ( salvia ) Salvinorin B ethoxymethyl ether Salvinorin B methoxymethyl ether Samidorphan Spiradoline ( U-62,066 ) TH - 030418 Thienorphine Tifluadom Tricyclic antidepressants ( e.g., amitriptyline, desipramine, imipramine, nortriptyline ) U-50,488 U-54,494 A U-69,593 Xorphanol Antagonists : 4 ′ - Hydroxyflavanone 4 ', 7 - Dihydroxyflavone 5 ' - GNTI 6 ' - GNTI 6β - Naltrexol 6β - Naltrexol - d4 β - Chlornaltrexamine Buprenorphine / samidorphan Amentoflavone ANTI Apigenin Arodyne AT - 076 Axelopran AZ - MTAB Binaltorphimine BU09059 Buprenorphine Catechin Catechin gallate CERC - 501 ( LY - 2456302 ) Clocinnamox Cyclofoxy Dezocine DIPPA EGC ECG Epicatechin Hyperoside JDTic LY - 255582 LY - 2196044 LY - 2444296 LY - 2459989 LY - 2795050 MeJDTic Methylnaltrexone ML190 ML350 MR - 2266 N - Fluoropropyl - JDTic Naloxone Naltrexone Naltrindole Naringenin Norbinaltorphimine Noribogaine Pawhuskin A PF - 4455242 RB - 64 Quadazocine Taxifolin UPHIT Zyklophin Unknown / unsorted : Akuammicine Akuammine Coronaridine Cyproterone acetate Dihydroakuuamine Ibogamine Tabernanthine NOP Agonists : ( Arg14, Lys15 ) Nociceptin ( ( pF ) Phe ) Nociceptin ( 1 - 13 ) NH ( Phe Ψ ( CH - NH ) Gly ) Nociceptin ( 1 - 13 ) NH Ac - RYYRWK - NH Ac - RYYRIK - NH BU08070 Buprenorphine Cebranopadol Dihydroetorphine Etorphine JNJ - 19385899 Levomethorphan Levorphanol Levorphanol Lexanopadol MCOPPB MT - 7716 NNC 63 - 0532 Nociceptin ( orphanin FQ ) Nociceptin ( 1 - 11 ) Nociceptin ( 1 - 13 ) NH Norbuprenorphine Racemethorphan Racemorphan Ro64 - 6198 Ro65 - 6570 SCH - 221510 SCH - 486757 SR - 8993 SR - 16435 TH - 030418 Antagonists : ( Nphe ) Nociceptin ( 1 - 13 ) NH AT - 076 BAN - ORL - 24 BTRX - 246040 ( LY - 2940094 ) J - 113397 JTC - 801 NalBzOH Nociceptin ( 1 - 7 ) Nocistatin SB - 612111 SR - 16430 Thienorphine Trap - 101 UFP - 101 Unsorted β - Casomorphins Amidorphin BAM - 20P Cytochrophin - 4 Deprolorphin Gliadorphin ( gluteomorphin ) Gluten exorphins Hemorphins Kava constituents MEAGL MEAP NEM Neoendorphins Nepetalactone ( catnip ) Peptide B Peptide E Peptide F Peptide I Rubiscolins Soymorphins Others Enkephalinase inhibitors : Amastatin BL - 2401 Candoxatril D - Phenylalanine Dexecadotril ( retorphan ) Ecadotril ( sinorphan ) Kelatorphan Racecadotril ( acetorphan ) RB - 101 RB - 120 RB - 3007 Opiorphan Selank Semax Spinorphin Thiorphan Tynorphin Ubenimex ( bestatin ) Propeptides : β - Lipotropin ( proendorphin ) Prodynorphin Proenkephalin Pronociceptin Proopiomelanocortin ( POMC ) Others : Kyotorphin ( met - enkephalin releaser / degradation stabilizer ) See also : Receptor / signaling modulators Signaling peptide / protein receptor modulators Ion channel modulators Calcium VDCCs Blockers L - type - selective : Dihydropyridines : Amlodipine Aranidipine Azelnidipine Barnidipine Clevidipine Cronidipine Darodipine Dexniguldipine Elgodipine Elnadipine Felodipine Flordipine Furnidipine Iganidipine Isradipine Lacidipine Lemildipine Lercanidipine Levamlodipine Levniguldipine Manidipine Mepirodipine Mesudipine Nicardipine Nifedipine Niguldipine Niludipine Nilvadipine Nimodipine Nisoldipine Nitrendipine Olradipine Oxodipine Palonidipine Pranidipine Ryodipine ( riodipine ) Sagandipine Sornidipine Teludipine Tiamdipine Trombodipine Vatanidipine ; Diltiazem derivatives : Clentiazem Diltiazem Iprotiazem Nictiazem Siratiazem ; Phenylalkylamines : Anipamil Dagapamil Devapamil Dexverapamil Emopamil Etripamil Falipamil Gallopamil Levemopamil Nexopamil Norverapamil Ronipamil Tiapamil Verapamil ; Others : AH - 1058 Brinazarone Budiodarone Celivarone Cyproheptadine Dronedarone Fantofarone SR - 33805 Tetrahydropalmatine N - type - selective : ω - Conotoxins ω - Conotoxin GVIA Caroverine Huwentoxin XVI Leconotide ( ω - conotoxin CVID ) PD - 173212 Ralfinamide Safinamide Z160 Ziconotide ( ω - conotoxin MVIIA ) P - type - selective : ω - Agatoxin IVA ω - Agatoxin IVB R - type - selective : SNX - 482 T - type - selective : ABT - 639 ML - 218 Niflumic acid NNC 55 - 0396 ProTx I Z944 Zonisamide Non-selective : ω - Agatoxin TK ω - Conotoxin MVIIC Benidipine Bepridil Cilnidipine Cinnarizine Dotarizine Efonidipine Flunarizine Lamotrigine Levetiracetam Lomerizine Loperamide Mibefradil NP078585 Ruthenium red TROX - 1 α δ subunit - selective ( gabapentinoids ) : 4 - Methylpregabalin Arbaclofen Arbaclofen placarbil Atagabalin Baclofen Gabapentin Gabapentin enacarbil Imagabalin Mirogabalin PD - 200,347 PD - 217,014 PD - 299,685 Phenibut Pregabalin Others / unsorted : Bencyclane Berbamine Bevantolol Canadine Carboxyamidotriazole Cycleanine Dauricine Dimeditiapramine Diproteverine Enpiperate Eperisone Elpetrigine Ethadione Ethanol ( alcohol ) Ethosuximide Fasudil Fendiline Fostedil Imepitoin JTV - 519 Lidoflazine Magnesium Manoalide Mesuximide Monatepil Naftopidil Ochratoxin A Osthol Otilonium bromide Paramethadione Phensuximide Pinaverium bromide Prenylamine Rhynchophylline Sesamodil Silperisone Sipatrigine Terodiline Tetrandrine Tolperisone Trimethadione Valperinol Activators L - type - selective : Bay K8644 Potassium VGKCs Blockers 3, 4 - Diaminopyridine ( amifampridine ) 4 - Aminopyridine ( fampridine / dalfampridine ) Adekalant Almokalant Amiodarone Azimilide Bretylium Bunaftine Charybdotoxin Clamikalant Conotoxins Dalazatide Dendrotoxin Dofetilide Dronedarone E-4031 Hanatoxin HgeTx1 HsTx1 Ibutilide Inakalant Kaliotoxin Linopirdine Lolitrem B Maurotoxin Nifekalant Notoxin Paxilline Pinokalant Quinidine ShK - 186 Sotalol Tedisamil Terikalant Tetraethylammonium Vernakalant hERG ( KCNH2, K 11.1 ) - specific : Ajmaline Amiodarone AmmTX3 Astemizole Azaspiracid AZD1305 Azimilide Bedaquiline BeKm - 1 BmTx3 BRL - 32872 Chlorpromazine Cisapride Clarithromycin Darifenacin Dextropropoxyphene Diallyl trisulfide Domperidone E-4031 Ergtoxins Erythromycin Gigactonine Haloperidol Ketoconazole Norpropoxyphene Orphenadrine Pimozide PNU - 282,987 Promethazine Quinidine Ranolazine Roxithromycin Sertindole Solifenacin Tamulotoxin Terodiline Terfenadine Thioridazine Tolterodine Vanoxerine Vernakalant KCNQ ( K 7 ) - specific : Linopirdine XE - 991 Spooky toxin ( SsTx ) Activators KCNQ ( K 7 ) - specific : Flupirtine Retigabine IRKs Blockers K - specific : Acetohexamide Carbutamide Chlorpropamide Glibenclamide ( glyburide ) Glibornuride Glicaramide Gliclazide Glimepiride Glipizide Gliquidone Glisoxepide Glyclopyramide Glycyclamide Metahexamide Mitiglinide Nateglinide Repaglinide Tolazamide Tolbutamide GIRK - specific : Barium Caramiphen Cloperastine Clozapine Dextromethorphan Ethosuximide Ifenprodil Tertiapin Tipepidine Activators K - specific : Aprikalim Bimakalim Cromakalim Diazoxide Emakalim Levcromakalim Mazokalim Minoxidil Naminidil Nicorandil Pinacidil Rilmakalim Sarakalim GIRK - specific : ML - 297 ( VU0456810 ) Blockers BK - specific : Ethanol ( alcohol ) GAL - 021 Activators BK - specific : Flufenamic acid Meclofenamic acid Niflumic acid Nimesulide Rottlerin ( mallotoxin ) Tolfenamic acid K2Ps Blockers 12 - O - Tetradecanoylphorbol - 13 - acetate Arachidonic acid Fluoxetine Norfluoxetine Activators Riluzole Sodium VGSCs Blockers Antianginals : Ranolazine Antiarrhythmics ( class I ) : Ajmaline Aprindine Disopyramide Dronedarone Encainide Flecainide Lidocaine Lorajmine Lorcainide Mexiletine Moricizine Pilsicainide Prajmaline Procainamide Propafenone Quinidine Sparteine Tocainide Anticonvulsants : Acetylpheneturide Carbamazepine Cenobamate Chlorphenacemide Elpetrigine Eslicarbazepine acetate Ethotoin Fosphenytoin Lacosamide Licarbazepine Mephenytoin Oxcarbazepine Oxitriptyline Phenacemide Pheneturide Phenytoin Rufinamide Sipatrigine Topiramate Sodium valproate Valnoctamide Valproate pivoxil Valproate semisodium Valproic acid Valpromide Zonisamide Local anesthetics : pFBT Amylocaine Articaine Benzocaine Bupivacaine ( Levobupivacaine, Ropivacaine ) Butacaine Butamben Chloroprocaine Cinchocaine Cocaine Cyclomethycaine Dimethocaine Diphenhydramine Etidocaine Hexylcaine Iontocaine Lidocaine Mepivacaine Meprylcaine Metabutoxycaine Orthocaine Piperocaine Prilocaine Procaine Propoxycaine Proxymetacaine Risocaine Tetracaine Trimecaine Analgesics : AZD - 3161 DSP - 2230 Funapide GDC - 0276 NKTR - 171 PF - 04531083 PF - 05089771 Ralfinamide Raxatrigine RG7893 ( GDC - 0287 ) Toxins : Conotoxins Neosaxitoxin Saxitoxin Tetrodotoxin Zetekitoxin AB Others : Buprenorphine Evenamide Menthol ( mint ) Safinamide Tricyclic antidepressants Activators Aconitine Atracotoxins ( Robustoxin, Versutoxin ) Batrachotoxin Ciguatoxins Grayanotoxins Poneratoxin ENaC Blockers Amiloride Benzamil Triamterene Activators Solnatide ASICs Blockers A-317567 Amiloride Aspirin Ibuprofen PcTX1 Chloride CaCCs Blockers Crofelemer DIDS Ethacrynic acid Flufenamic acid Fluoxetine Furosemide Glibenclamide Mefloquine Mibefradil Niflumic acid Activators Carbachol CFTR Blockers Glibenclamide Lonidamine Piretanide Activators 1, 7 - Phenanthroline 1, 10 - Phenanthroline 4, 7 - Phenanthroline 7, 8 - Benzoquinoline Ivacaftor Phenanthridine Unsorted Blockers Bumetanide Flufenamic acid Meclofenamic acid Mefenamic acid Mepacrine Niflumic acid Talniflumate Tolfenamic acid Trifluoperazine Others TRPs See here instead. See also : Receptor / signaling modulators Transient receptor potential channel modulators Retrieved from `` https://en.wikipedia.org/w/index.php?title=Buprenorphine&oldid=855976690 '' Categories : Alcohols Cat medications Dog medications Delta - opioid antagonists Drug rehabilitation Ethers Euphoriants Kappa antagonists Morphinans Mu - opioid agonists Nociceptin receptor agonists Nociceptin receptor antagonists Oripavines Phenols Semisynthetic opioids Sodium channel blockers Hidden categories : Webarchive template wayback links Use dmy dates from December 2017 Use American English from December 2017 All Wikipedia articles written in American English Template : drugs.com link with non-standard subpage Articles with changed EBI identifier ECHA InfoCard ID from Wikidata Drug has EMA link Drugboxes which contain changes to verified fields Drugboxes which contain changes to watched fields RTT Talk Contents About Wikipedia تۆرکجه বাংলা Български Čeština Cymraeg Dansk Deutsch Ελληνικά Español Euskara فارسی Français Հայերեն Italiano ქართული Magyar Nederlands 日本 語 Norsk ଓଡ଼ିଆ Polski Português Română Русский Српски / srpski Srpskohrvatski / српскохрватски Suomi Svenska ไทย 21 more Edit links This page was last edited on 22 August 2018, at 03 : 13 ( UTC ). 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Question: bupernorphine (buprenex® subutex® suboxone®) is used to treat which substance use disorder
Answer: opioid addiction