{"id":"acetylmethadol","rwe":[],"tags":[{"label":"Small Molecule","category":"modality"},{"label":"Potassium voltage-gated channel subfamily H member 2","category":"target"},{"label":"KCNH2","category":"gene"},{"label":"OPRM1","category":"gene"},{"label":"Active","category":"status"},{"label":"Opioid dependence","category":"indication"},{"label":"Analgesics","category":"pharmacology"},{"label":"Analgesics, Opioid","category":"pharmacology"},{"label":"Central Nervous System Agents","category":"pharmacology"},{"label":"Central Nervous System Depressants","category":"pharmacology"},{"label":"Narcotics","category":"pharmacology"},{"label":"Peripheral Nervous System Agents","category":"pharmacology"},{"label":"Sensory System Agents","category":"pharmacology"}],"phase":"unknown","safety":{"commonSideEffects":[],"contraindications":["Acute exacerbation of asthma","Alcoholism","Benign intracranial hypertension","Benign prostatic hyperplasia","Cholecystitis","Chronic disease of respiratory system","Conduction disorder of the heart","Decreased respiratory function","Disease of liver","Disorder of gallbladder","Disorder of gastrointestinal tract","Drug AND/OR toxin-induced diarrhea","General anesthesia","Hypothyroidism","Injury of head","Kidney disease","Lesion of brain","Mood swings","Operation on gastrointestinal tract","Procedure on urinary system","Pseudomembranous enterocolitis","Suicidal thoughts","Urethral stricture"]},"trials":[],"aliases":[],"patents":[],"pricing":[],"_fixedAt":"2026-03-30T16:27:57.669103","allNames":"methadyl","offLabel":[],"synonyms":["methadyl","acemethadone","acetmethadon","acetylmethadol","acetylmethadone","methadyl acetate"],"timeline":[],"brandName":"Methadyl","ecosystem":[{"indication":"Opioid dependence","otherDrugs":[{"name":"buprenorphine","slug":"buprenorphine","company":"Reckitt Benckiser"},{"name":"levomethadyl acetate","slug":"levomethadyl-acetate","company":"Roxane"},{"name":"naloxone","slug":"naloxone","company":"Adapt"}],"globalPrevalence":null}],"mechanism":{"target":"Mu-type opioid receptor","targets":[{"gene":"OPRM1","source":"DrugCentral","target":"Mu-type opioid receptor","protein":"Mu-type opioid receptor","isPrimary":true,"activityType":"","activityValue":null},{"gene":"KCNH2","source":"DrugCentral","target":"Potassium voltage-gated channel subfamily H member 2","protein":"Potassium voltage-gated channel subfamily H member 2"}],"modality":"Small Molecule","explanation":"Imagine your brain is like a city with many busy streets. When you're addicted to opioids, those streets get really chaotic and hard to navigate. Methadyl helps calm down the streets by blocking the flow of potassium ions, which helps reduce the chaos and makes it easier to manage withdrawal symptoms.","oneSentence":"Methadyl works by blocking potassium channels in the brain to stabilize neuronal activity and reduce withdrawal symptoms.","technicalDetail":"Methadyl exerts its effects by selectively blocking the potassium voltage-gated channel subfamily H member 2 (KCNH2), a key ion channel involved in the regulation of neuronal excitability and the modulation of withdrawal symptoms in opioid-dependent individuals."},"_wikipedia":{"url":"https://en.wikipedia.org/wiki/Acetylmethadol","title":"Acetylmethadol","extract":"Acetylmethadol, also known as methadyl acetate, is a synthetic opioid analgesic. It is a racemic mixture of alphacetylmethadol (α-acetylmethadol) and betacetylmethadol (β-acetylmethadol), which are in turn racemic mixtures of levacetylmethadol and D-α-acetylmethadol and L-β-acetylmethadol and D-β-acetylmethadol, respectively. Hence, acetylmethadol has four possible optical isomers. All of these isomers have been shown to partially or fully substitute for the discriminative stimulus effects of heroin in rats, and thus it can be inferred that, in addition to LAAM which is used clinically as such, they are all likely to be active opioid analgesics in humans."},"commercial":{},"references":[{"id":1,"url":"https://drugcentral.org/drugcard/1729","fields":["approvals","synonyms","ATC","PK","indications","contraindications","DDIs","targets","patents","FAERS"],"source":"DrugCentral"},{"id":2,"url":"https://clinicaltrials.gov/search?intr=acetylmethadol","fields":["trials"],"source":"ClinicalTrials.gov"},{"id":3,"url":"https://pubmed.ncbi.nlm.nih.gov/?term=acetylmethadol","fields":["publications"],"source":"PubMed/NCBI"},{"id":4,"url":"https://en.wikipedia.org/wiki/Acetylmethadol","fields":["history","overview"],"source":"Wikipedia"}],"_enrichedAt":"2026-03-30T07:29:07.301412","biosimilars":[],"competitors":[{"drugName":"abemaciclib","drugSlug":"abemaciclib","fdaApproval":"2017-09-28","patentExpiry":"Sep 28, 2031","patentStatus":"Patent protected","relationship":"same-target"},{"drugName":"alosetron","drugSlug":"alosetron","fdaApproval":"2000-02-09","genericCount":6,"patentStatus":"Off-patent — generic available","relationship":"same-target"},{"drugName":"amiodarone","drugSlug":"amiodarone","fdaApproval":"1985-12-24","patentExpiry":"Mar 13, 2029","patentStatus":"Patent protected","relationship":"same-target"},{"drugName":"amitriptyline","drugSlug":"amitriptyline","fdaApproval":"1961-04-07","genericCount":33,"patentStatus":"Off-patent — generic available","relationship":"same-target"},{"drugName":"amodiaquine","drugSlug":"amodiaquine","fdaApproval":"","patentStatus":"Unknown","relationship":"same-target"},{"drugName":"aripiprazole","drugSlug":"aripiprazole","fdaApproval":"2002-11-15","patentExpiry":"Sep 24, 2033","patentStatus":"Patent protected","relationship":"same-target"},{"drugName":"arsenic trioxide","drugSlug":"arsenic-trioxide","fdaApproval":"2000-09-25","genericCount":11,"patentStatus":"Off-patent — generic available","relationship":"same-target"},{"drugName":"asciminib","drugSlug":"asciminib","fdaApproval":"2021-10-29","patentExpiry":"Oct 29, 2035","patentStatus":"Patent protected","relationship":"same-target"},{"drugName":"astemizole","drugSlug":"astemizole","fdaApproval":"1988-12-31","relationship":"same-target"},{"drugName":"atomoxetine","drugSlug":"atomoxetine","fdaApproval":"2002-11-26","genericCount":8,"patentStatus":"Off-patent — generic available","relationship":"same-target"}],"genericName":"acetylmethadol","indications":{"approved":[{"name":"Opioid dependence","source":"DrugCentral","snomedId":75544000,"regulator":"FDA"}],"offLabel":[],"pipeline":[]},"_fixedFields":["primaryTarget"],"drugCategory":"active","labelChanges":[],"relatedDrugs":[{"drugId":"abemaciclib","brandName":"abemaciclib","genericName":"abemaciclib","approvalYear":"2017","relationship":"same-target"},{"drugId":"alosetron","brandName":"alosetron","genericName":"alosetron","approvalYear":"2000","relationship":"same-target"},{"drugId":"amiodarone","brandName":"amiodarone","genericName":"amiodarone","approvalYear":"1985","relationship":"same-target"},{"drugId":"amitriptyline","brandName":"amitriptyline","genericName":"amitriptyline","approvalYear":"1961","relationship":"same-target"},{"drugId":"amodiaquine","brandName":"amodiaquine","genericName":"amodiaquine","approvalYear":"","relationship":"same-target"},{"drugId":"aripiprazole","brandName":"aripiprazole","genericName":"aripiprazole","approvalYear":"2002","relationship":"same-target"},{"drugId":"arsenic-trioxide","brandName":"arsenic trioxide","genericName":"arsenic trioxide","approvalYear":"2000","relationship":"same-target"},{"drugId":"asciminib","brandName":"asciminib","genericName":"asciminib","approvalYear":"2021","relationship":"same-target"},{"drugId":"astemizole","brandName":"astemizole","genericName":"astemizole","approvalYear":"1988","relationship":"same-target"},{"drugId":"atomoxetine","brandName":"atomoxetine","genericName":"atomoxetine","approvalYear":"2002","relationship":"same-target"}],"trialDetails":[{"nctId":"NCT01935830","phase":"EARLY_PHASE1","title":"LAAM-HAART PET Imaging","status":"COMPLETED","sponsor":"Washington University School of Medicine","startDate":"2013-08","conditions":["Healthy Volunteers"],"enrollment":10,"completionDate":"2015-09"},{"nctId":"NCT00000300","phase":"PHASE4","title":"Feasibility Study of Take-Home LAAM Medication - 3","status":"COMPLETED","sponsor":"University of California, Los Angeles","startDate":"1995-03","conditions":["Opioid-Related Disorders"],"enrollment":0,"completionDate":""},{"nctId":"NCT00158288","phase":"PHASE2","title":"The Efficacy of Methadyl Acetate (LAAM) and Contingency Management Procedures for Treating Dual Opioid and Cocaine Abuse - 1","status":"COMPLETED","sponsor":"National Institute on Drug Abuse (NIDA)","startDate":"1997-03","conditions":["Behavior Therapy","Cocaine","Contingency Management","Heroin Dependence","LAAM","Opioid Dependence","Substance-Related Disorders","Alcohol & Drug Use"],"enrollment":140,"completionDate":"2001-08"},{"nctId":"NCT00000356","phase":"PHASE2","title":"Evaluation of L-alpha-acetylmethadol (LAAM) in Methadone Patients - 5","status":"COMPLETED","sponsor":"National Institute on Drug Abuse (NIDA)","startDate":"1991-06","conditions":["Opioid-Related Disorders","Substance-Related Disorders"],"enrollment":0,"completionDate":"1992-10"},{"nctId":"NCT00218127","phase":"PHASE2","title":"Treatment of Opioid/Heroin Dependence: Comparison of Three Medication Dosing Regimens","status":"COMPLETED","sponsor":"National Institute on Drug Abuse (NIDA)","startDate":"2001-11","conditions":["Heroin Dependence","Opioid-Related Disorders"],"enrollment":142,"completionDate":"2005-07"}],"genericFilers":[],"latestUpdates":[],"manufacturing":[],"crossReferences":{"NUI":"N0000006653","UNII":"L59OC40KWJ","CHEBI":"CHEBI:135491","INN_ID":"654","RXNORM":"6814","UMLSCUI":"C0025607","ChEMBL_ID":"CHEMBL170179","KEGG_DRUG":"D04973","DRUGBANK_ID":"DB01433","PUBCHEM_CID":"10517","MESH_DESCRIPTOR_UI":"D008692"},"formularyStatus":[],"_enricherVersion":"v2","developmentCodes":[],"ownershipHistory":[],"pharmacokinetics":{"source":"DrugCentral","bioavailability":"47%"},"publicationCount":274,"therapeuticAreas":["Neuroscience"],"biosimilarFilings":[],"recentPublications":[],"companionDiagnostics":[],"genericManufacturerList":[],"status":"active","companyName":"","companyId":"unknown","modality":"Small Molecule","firstApprovalDate":"","aiSummary":"Methadyl, also known as acetylmethadol, is a synthetic opioid analgesic that is a racemic mixture of alphacetylmethadol and betacetylmethadol. It is a small molecule used in the treatment of opioid and cocaine abuse, often in combination with contingency management procedures and behavioral therapy.","enrichmentLevel":3,"visitCount":0,"trialStats":{"total":0,"withResults":0},"verificationStatus":"verified","dataCompleteness":{"mechanism":true,"indications":true,"safety":false,"trials":true,"score":3}}