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METHADONE Drug Record

  • Summary
  • Interactions
  • Claims
  • METHADONE chembl:CHEMBL651 Approved

    Alternate Names:

    DOLOPHINE
    METHADONE
    WESTADONE
    METHADOSE
    SYMORON
    IDS-NM-002
    PHY
    PHYSEPTONE
    AMIDONE
    HEPTADON

    Drug Info:

    FDA Approval Approved before 1982
    Drug Class small molecule
    Drug Indications Antitussive Agents
    Drug Indications Analgesics, Opioid
    Drug Categories cytochrome p-450 cyp3a inducers
    Year of Approval approved before 1982
    Drug Class analgesics, opioid
    Drug Class antitussive agents
    Drug Categories anticholinergic agents
    Drug Categories antidepressive agents
    Drug Categories cytochrome p-450 cyp2b6 inducers
    Drug Categories cytochrome p-450 cyp2b6 inducers (strength unknown)
    Drug Categories cytochrome p-450 cyp2c18 substrates
    Drug Categories cytochrome p-450 cyp2d6 inhibitors (strength unknown)
    Drug Categories cytochrome p-450 cyp3a substrates
    Drug Categories cytochrome p-450 cyp3a4 inducers
    Drug Categories cytochrome p-450 cyp3a4 inducers (strength unknown)
    Drug Categories cytochrome p-450 cyp3a4 inhibitors
    Drug Categories cytochrome p-450 cyp3a4 inhibitors (strength unknown)
    Drug Categories cytochrome p-450 cyp3a5 substrates
    Drug Categories cytochrome p-450 cyp3a7 substrates
    Drug Categories cytochrome p-450 enzyme inducers
    Drug Categories cytochrome p-450 enzyme inhibitors
    Drug Categories cytochrome p-450 substrates
    Drug Categories drugs that are mainly renally excreted
    Drug Categories drugs used in addictive disorders
    Drug Categories drugs used in opioid dependence
    Drug Categories high-risk opioids
    Drug Categories nicotinic antagonists
    Drug Categories nmda receptor antagonists
    Drug Categories opiate agonists
    Drug Categories opioid agonist
    Drug Categories opioids
    Drug Categories p-glycoprotein inhibitors
    Drug Categories qtc prolonging agents
    Drug Categories serotonergic drugs shown to increase risk of serotonin syndrome
    Drug Categories serotonin agents
    Drug Categories thyroxine-binding globulin inducers
    (5 More Sources)

    Publications:

    Crettol S et al., 2006, ABCB1 and cytochrome P450 genotypes and phenotypes: influence on methadone plasma levels and response to treatment., Clin Pharmacol Ther
    Tian JN et al., 2012, UGT2B7 genetic polymorphisms are associated with the withdrawal symptoms in methadone maintenance patients., Pharmacogenomics
    Eap CB et al., 2007, Stereoselective block of hERG channel by (S)-methadone and QT interval prolongation in CYP2B6 slow metabolizers., Clin Pharmacol Ther
    Csajka C et al., 2016, Population Genetic-Based Pharmacokinetic Modeling of Methadone and its Relationship with the QTc Interval in Opioid-Dependent Patients., Clin Pharmacokinet
    Uehlinger C et al., 2007, Increased (R)-methadone plasma concentrations by quetiapine in cytochrome P450s and ABCB1 genotyped patients., J Clin Psychopharmacol
    Mactier H et al., 2017, Variations in Infant CYP2B6 Genotype Associated with the Need for Pharmacological Treatment for Neonatal Abstinence Syndrome in Infants of Methadone-Maintained Opioid-Dependent Mothers., Am J Perinatol
    Hung CC et al., 2011, Impact of genetic polymorphisms in ABCB1, CYP2B6, OPRM1, ANKK1 and DRD2 genes on methadone therapy in Han Chinese patients., Pharmacogenomics
    Amunugama HT et al., 2012, Mechanism-based inactivation of cytochrome P450 2B6 by methadone through destruction of prosthetic heme., Drug Metab Dispos
    Zanger UM et al., 2007, Polymorphic CYP2B6: molecular mechanisms and emerging clinical significance., Pharmacogenomics
    Dobrinas M et al., 2013, Contribution of CYP2B6 alleles in explaining extreme (S)-methadone plasma levels: a CYP2B6 gene resequencing study., Pharmacogenet Genomics
    Crettol S et al., 2005, Methadone enantiomer plasma levels, CYP2B6, CYP2C19, and CYP2C9 genotypes, and response to treatment., Clin Pharmacol Ther
    Lang T et al., 2001, Extensive genetic polymorphism in the human CYP2B6 gene with impact on expression and function in human liver., Pharmacogenetics
    Zahari Z et al., 2016, Relationship between CYP2B6*6 and cold pressor pain sensitivity in opioid dependent patients on methadone maintenance therapy (MMT)., Drug Alcohol Depend
    Victorri-Vigneau C et al., 2019, Relevance of CYP2B6 and CYP2D6 genotypes to methadone pharmacokinetics and response in the OPAL study., Br J Clin Pharmacol
    Levran O et al., 2013, CYP2B6 SNPs are associated with methadone dose required for effective treatment of opioid addiction., Addict Biol
    Mouly S et al., 2015, Methadone dose in heroin-dependent patients: role of clinical factors, comedications, genetic polymorphisms and enzyme activity., Br J Clin Pharmacol
    Kakko et al., 2008, Mood and neuroendocrine response to a chemical stressor, metyrapone, in buprenorphine-maintained heroin dependence., Biol. Psychiatry
    Eap CB et al., 2002, Interindividual variability of the clinical pharmacokinetics of methadone: implications for the treatment of opioid dependence., Clin Pharmacokinet
    Kvam et al., 2004, Genetic analysis of the murine mu opioid receptor: increased complexity of Oprm gene splicing., J. Mol. Med.
    Sotgiu et al., 2009, Cooperative N-methyl-D-aspartate (NMDA) receptor antagonism and mu-opioid receptor agonism mediate the methadone inhibition of the spinal neuron pain-related hyperactivity in a rat model of neuropathic pain., Pharmacol. Res.
    Shi et al., 2002, Sequence variations in the mu-opioid receptor gene (OPRM1) associated with human addiction to heroin., Hum. Mutat.
    Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov
    Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov
    Hronová K et al., 2016, Sufentanil and midazolam dosing and pharmacogenetic factors in pediatric analgosedation and withdrawal syndrome., Physiol Res
    Duan L et al., 2020, Association of <i>COMT</i> Gene Polymorphisms with Response to Methadone Maintenance Treatment Among Chinese Opioid-Dependent Patients., Genet Test Mol Biomarkers
    De Gregori M et al., 2013, Genetic variability at COMT but not at OPRM1 and UGT2B7 loci modulates morphine analgesic response in acute postoperative pain., Eur J Clin Pharmacol
    Klepstad P et al., 2011, Influence from genetic variability on opioid use for cancer pain: a European genetic association study of 2294 cancer pain patients., Pain
    Landau R et al., 2013, The effect of OPRM1 and COMT genotypes on the analgesic response to intravenous fentanyl labor analgesia., Anesth Analg
    De Gregori M et al., 2016, Human Genetic Variability Contributes to Postoperative Morphine Consumption., J Pain
    Aubrun F et al., 2018, Opioid-related genetic polymorphisms do not influence postoperative opioid requirement: A prospective observational study., Eur J Anaesthesiol
    Cargnin S et al., 2013, An opposite-direction modulation of the COMT Val158Met polymorphism on the clinical response to intrathecal morphine and triptans., J Pain
    Matic M et al., 2014, Rescue morphine in mechanically ventilated newborns associated with combined OPRM1 and COMT genotype., Pharmacogenomics
    Candiotti KA et al., 2014, Catechol-o-methyltransferase polymorphisms predict opioid consumption in postoperative pain., Anesth Analg
    Lötsch J et al., 2009, Cross-sectional analysis of the influence of currently known pharmacogenetic modulators on opioid therapy in outpatient pain centers., Pharmacogenet Genomics
    Matic M et al., 2017, Advanced cancer pain: the search for genetic factors correlated with interindividual variability in opioid requirement., Pharmacogenomics
    Elens L et al., 2016, Genetic Predisposition to Poor Opioid Response in Preterm Infants: Impact of KCNJ6 and COMT Polymorphisms on Pain Relief After Endotracheal Intubation., Ther Drug Monit
    Wang et al., 2003, Involvement of CYP3A4, CYP2C8, and CYP2D6 in the metabolism of (R)- and (S)-methadone in vitro., Drug Metab. Dispos.
    Rendic S et al., 1997, Human cytochrome P450 enzymes: a status report summarizing their reactions, substrates, inducers, and inhibitors., Drug Metab Rev
    Chen CH et al., 2011, Genetic polymorphisms in CYP3A4 are associated with withdrawal symptoms and adverse reactions in methadone maintenance patients., Pharmacogenomics
    Lieb B et al., 2009, Intensity of opiate withdrawal in relation to the 825C&gt;T polymorphism of the G-protein beta 3 subunit gene., Prog Neuropsychopharmacol Biol Psychiatry
    Gross et al., 2009, Acute methadone treatment reduces myocardial infarct size via the delta-opioid receptor in rats during reperfusion., Anesth. Analg.
    Fang CP et al., 2020, Genetic polymorphisms in the opioid receptor delta 1 (OPRD1) gene are associated with methadone dose in methadone maintenance treatment for heroin dependence., J Hum Genet
    Levran O et al., 2012, Nerve growth factor β polypeptide (NGFB) genetic variability: association with the methadone dose required for effective maintenance treatment., Pharmacogenomics J
    Levran O et al., 2013, Association of genetic variation in pharmacodynamic factors with methadone dose required for effective treatment of opioid addiction., Pharmacogenomics
    Housová et al., 2005, Adipocyte-derived hormones in heroin addicts: the influence of methadone maintenance treatment., Physiol Res
    Fonseca F et al., 2014, ALDH5A1 variability in opioid dependent patients could influence response to methadone treatment., Eur Neuropsychopharmacol
    Seidler et al., 1982, Delays in growth and biochemical development of rat brain caused by maternal methadone administration: are the alterations in synaptogenesis and cellular maturation independent of reduced maternal food intake?, Dev. Neurosci.
    Zhang Q et al., 2020, κ Opioid Receptor 1 Single Nucleotide Polymorphisms were Associated with the Methadone Dosage., Genet Test Mol Biomarkers
    Nanovskaya et al., 2005, Role of P-glycoprotein in transplacental transfer of methadone., Biochem. Pharmacol.
    Crettol S et al., 2008, Association of dopamine and opioid receptor genetic polymorphisms with response to methadone maintenance treatment., Prog Neuropsychopharmacol Biol Psychiatry
    Doehring A et al., 2009, Genetic variants altering dopamine D2 receptor expression or function modulate the risk of opiate addiction and the dosage requirements of methadone substitution., Pharmacogenet Genomics
    Roden DM, 2004, Drug-induced prolongation of the QT interval., N Engl J Med
    Kuo HW et al., 2018, Inflammatory chemokine eotaxin-1 is correlated with age in heroin dependent patients under methadone maintenance therapy., Drug Alcohol Depend
    Crist RC et al., 2018, Pharmacogenetic analysis of opioid dependence treatment dose and dropout rate., Am J Drug Alcohol Abuse
    de Cid et al., 2008, BDNF variability in opioid addicts and response to methadone treatment: preliminary findings., Genes Brain Behav.
    Lötsch J et al., 2010, A KCNJ6 (Kir3.2, GIRK2) gene polymorphism modulates opioid effects on analgesia and addiction but not on pupil size., Pharmacogenet Genomics
    Deeb et al., 2009, Direct subunit-dependent multimodal 5-hydroxytryptamine3 receptor antagonism by methadone., Mol. Pharmacol.
    Shi Y et al., 2020, GAD1 but not GAD2 polymorphisms are associated with heroin addiction phenotypes., Neurosci Lett
    Robinson et al., 1993, Prenatal exposure to methadone delays the development of striatal cholinergic neurons., Brain Res. Dev. Brain Res.
    Talka R et al., 2015, Methadone's effect on nAChRs--a link between methadone use and smoking?, Biochem Pharmacol
    Talka R et al., 2015, Methadone is a non-competitive antagonist at the α4β2 and α3* nicotinic acetylcholine receptors and an agonist at the α7 nicotinic acetylcholine receptor., Basic Clin Pharmacol Toxicol
    Hanania T et al., 2020, The N-methyl-D-aspartate receptor antagonist d-methadone acutely improves depressive-like behavior in the forced swim test performance of rats., Exp Clin Psychopharmacol
  • METHADONE   CYP2A7P1

    Interaction Score: 3.34

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    28320034


    Sources:
    PharmGKB

  • METHADONE   GAD1

    Interaction Score: 1.11

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    31866536


    Sources:
    PharmGKB

  • METHADONE   CCL11

    Interaction Score: 1.11

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    29222992


    Sources:
    PharmGKB

  • METHADONE   TXNRD2

    Interaction Score: 1.11

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    32407152


    Sources:
    PharmGKB

  • METHADONE   CDH2

    Interaction Score: 0.84

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • METHADONE   PNOC

    Interaction Score: 0.84

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • METHADONE   NGF

    Interaction Score: 0.72

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    21358750 23651024


    Sources:
    PharmGKB

  • METHADONE   COMT

    Interaction Score: 0.62

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    28006928 32407152 23686330 21398039 23302985 26902643 29474345 23773341 25155931 25185591 19514130 28745577 27027462


    Sources:
    PharmGKB

  • METHADONE   CYP2B6

    Interaction Score: 0.55

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    17329992 27286724 17178267 17502774 28320034 21902500 22685215 17638512 23249875 16338275 11470993 27289271 30907440 21790905 25556837


    Sources:
    DTC PharmGKB

  • METHADONE   KCNJ6

    Interaction Score: 0.42

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20220551


    Sources:
    PharmGKB

  • METHADONE   ALDH5A1

    Interaction Score: 0.42

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    24230997


    Sources:
    PharmGKB

  • METHADONE   ANKK1

    Interaction Score: 0.26

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    23651024


    Sources:
    PharmGKB

  • METHADONE   GNB3

    Interaction Score: 0.26

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    19303909


    Sources:
    PharmGKB

  • METHADONE   UGT2B7

    Interaction Score: 0.24

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    17178267 22676193


    Sources:
    PharmGKB

  • METHADONE   TH

    Interaction Score: 0.22

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    6125371


    Sources:
    NCI

  • METHADONE   LEP

    Interaction Score: 0.22

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15717844


    Sources:
    NCI

  • METHADONE   CHRNB2

    Interaction Score: 0.19

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    26231941 25196810


    Sources:
    DrugBank

  • METHADONE   CHRNA3

    Interaction Score: 0.17

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    26231941 25196810


    Sources:
    DrugBank

  • METHADONE   GRIN1

    Interaction Score: 0.15

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    12405865 19717013 17139284 31368772 17016423


    Sources:
    DrugBank

  • METHADONE   OPRM1

    Interaction Score: 0.13

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Direct Interaction? True
    Endogenous Drug? False
    Specific Action of the Ligand Agonist

    PMIDs:
    17850768 12405865 14991152 19717013 11933204 17139284 17016423


    Sources:
    TEND TdgClinicalTrial DrugBank GuideToPharmacology

  • METHADONE   OPRD1

    Interaction Score: 0.1

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:

    PMIDs:
    12405865 19843777 31907389


    Sources:
    PharmGKB DrugBank

  • METHADONE   BDNF

    Interaction Score: 0.1

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    23651024 18182069


    Sources:
    NCI PharmGKB

  • METHADONE   CHRNA4

    Interaction Score: 0.09

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    26231941 25196810


    Sources:
    DrugBank

  • METHADONE   CHRNA7

    Interaction Score: 0.08

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:

    PMIDs:
    26231941 25196810


    Sources:
    DrugBank

  • METHADONE   NTRK2

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    23651024


    Sources:
    PharmGKB

  • METHADONE   HTR3A

    Interaction Score: 0.05

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    19131665


    Sources:
    DrugBank

  • METHADONE   ACHE

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    8149590


    Sources:
    NCI

  • METHADONE   DRD2

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    21902500 23651024 18687376 19373123 25556837


    Sources:
    PharmGKB

  • METHADONE   SLC6A4

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    29333880


    Sources:
    PharmGKB

  • METHADONE   OPRK1

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    31940240


    Sources:
    PharmGKB

  • METHADONE   KCNH2

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    17329992 14999113


    Sources:
    PharmGKB

  • METHADONE   ABCB1

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15876424


    Sources:
    NCI

  • METHADONE   NR1I2

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • METHADONE   CYP3A4

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    12756206 9187528 21902501


    Sources:
    NCI PharmGKB

  • DrugBank: DB00333

    • Version: 5.1.7

    Alternate Names:
    76-99-3 CAS Number
    Adolan Drug Brand
    Depridol Drug Brand

    Drug Info:
    Drug Type small molecule
    Drug Groups approved
    Drug Categories analgesics

    Publications:
    Talka R et al., 2015, Methadone's effect on nAChRs--a link between methadone use and smoking?, Biochem Pharmacol
    Talka R et al., 2015, Methadone is a non-competitive antagonist at the α4β2 and α3* nicotinic acetylcholine receptors and an agonist at the α7 nicotinic acetylcholine receptor., Basic Clin Pharmacol Toxicol
    Eap CB et al., 2002, Interindividual variability of the clinical pharmacokinetics of methadone: implications for the treatment of opioid dependence., Clin Pharmacokinet

  • TEND: METHADONE

    • Version: 01-August-2011

    Alternate Names:

    Drug Info:
    Drug Class antitussive agents
    Drug Class analgesics, opioid
    Year of Approval approved before 1982

    Publications:

  • TdgClinicalTrial: METHADONE

    • Version: January-2014

    Alternate Names:

    Drug Info:
    Drug Indications Analgesics, Opioid
    Drug Indications Antitussive Agents
    Drug Class small molecule

    Publications:

  • NCI: METHADONE

    • Version: 14-September-2017

    Alternate Names:
    C638 NCI drug code

    Drug Info:

    Publications:
    Housová et al., 2005, Adipocyte-derived hormones in heroin addicts: the influence of methadone maintenance treatment., Physiol Res
    Wang et al., 2003, Involvement of CYP3A4, CYP2C8, and CYP2D6 in the metabolism of (R)- and (S)-methadone in vitro., Drug Metab. Dispos.
    de Cid et al., 2008, BDNF variability in opioid addicts and response to methadone treatment: preliminary findings., Genes Brain Behav.

  • DTC: METHADONE

    • Version: 02-September-2020

    Alternate Names:
    CHEMBL651 ChEMBL Drug ID

    Drug Info:

    Publications:
    Amunugama HT et al., 2012, Mechanism-based inactivation of cytochrome P450 2B6 by methadone through destruction of prosthetic heme., Drug Metab Dispos

  • PharmGKB: methadone

    • Version: 18-August-2020

    Alternate Names:

    Drug Info:

    Publications:
    Fang CP et al., 2020, Genetic polymorphisms in the opioid receptor delta 1 (OPRD1) gene are associated with methadone dose in methadone maintenance treatment for heroin dependence., J Hum Genet
    Fonseca F et al., 2014, ALDH5A1 variability in opioid dependent patients could influence response to methadone treatment., Eur Neuropsychopharmacol
    Eap CB et al., 2007, Stereoselective block of hERG channel by (S)-methadone and QT interval prolongation in CYP2B6 slow metabolizers., Clin Pharmacol Ther

  • TTD: Methadone

    • Version: 2020.06.01

    Alternate Names:
    D09OJQ TTD Drug ID

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL651

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

  • GuideToPharmacology: 178102108

    • Version: 29-September-2020

    Alternate Names:

    Drug Info:

    Publications:

Disclaimer: This resource is intended for purely research purposes. It should not be used for emergencies or medical or professional advice.

A finding of a drug-gene interaction or potentially druggable category does not necessarily indicate effectiveness (or lack thereof) of any drug or treatment regimen. A finding of no interaction or no potentially druggable category does not necessarily indicate lack of effectiveness of any drug or treatment regimen. Drug-gene interactions or potentially druggable categories are not presented in ranked order of potential or predicted efficacy.

The dgidb.org website does not provide any medical or healthcare products, services or advice, and is not for medical emergencies or urgent situations. IF YOU THINK YOU MAY HAVE A MEDICAL EMERGENCY, CALL YOUR DOCTOR OR 911 IMMEDIATELY. Information contained on this website is not a substitute for a doctor's medical judgment or advice. We recommend that you discuss your specific, individual health concerns with your doctor or health care professional.

DGIdb (v4.2.0 - sha1 afd9f30b) • Last updated 2020-10-21