DGIdb - METHADONE Drug Record

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

(3 More Sources)

Publications:

Tian JN et al., 2012, UGT2B7 genetic polymorphisms are associated with the withdrawal symptoms in methadone maintenance patients., Pharmacogenomics
Crettol S et al., 2006, ABCB1 and cytochrome P450 genotypes and phenotypes: influence on methadone plasma levels and response to treatment., Clin Pharmacol Ther
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
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
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
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
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
Dobrinas M et al., 2013, Contribution of CYP2B6 alleles in explaining extreme (S)-methadone plasma levels: a CYP2B6 gene resequencing study., Pharmacogenet Genomics
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
Levran O et al., 2013, CYP2B6 SNPs are associated with methadone dose required for effective treatment of opioid addiction., Addict Biol
Uehlinger C et al., 2007, Increased (R)-methadone plasma concentrations by quetiapine in cytochrome P450s and ABCB1 genotyped patients., J Clin Psychopharmacol
Eap CB et al., 2007, Stereoselective block of hERG channel by (S)-methadone and QT interval prolongation in CYP2B6 slow metabolizers., Clin Pharmacol Ther
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
Zanger UM et al., 2007, Polymorphic CYP2B6: molecular mechanisms and emerging clinical significance., Pharmacogenomics
Amunugama HT et al., 2012, Mechanism-based inactivation of cytochrome P450 2B6 by methadone through destruction of prosthetic heme., Drug Metab Dispos
Kvam et al., 2004, Genetic analysis of the murine mu opioid receptor: increased complexity of Oprm gene splicing., J. Mol. Med.
Shi et al., 2002, Sequence variations in the mu-opioid receptor gene (OPRM1) associated with human addiction to heroin., Hum. Mutat.
Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov
Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov
Kakko et al., 2008, Mood and neuroendocrine response to a chemical stressor, metyrapone, in buprenorphine-maintained heroin dependence., Biol. Psychiatry
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.
Eap CB et al., 2002, Interindividual variability of the clinical pharmacokinetics of methadone: implications for the treatment of opioid dependence., Clin Pharmacokinet
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
Aubrun F et al., 2018, Opioid-related genetic polymorphisms do not influence postoperative opioid requirement: A prospective observational study., Eur J Anaesthesiol
Matic M et al., 2017, Advanced cancer pain: the search for genetic factors correlated with interindividual variability in opioid requirement., Pharmacogenomics
Hronová K et al., 2016, Sufentanil and midazolam dosing and pharmacogenetic factors in pediatric analgosedation and withdrawal syndrome., Physiol Res
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
De Gregori M et al., 2016, Human Genetic Variability Contributes to Postoperative Morphine Consumption., J Pain
Candiotti KA et al., 2014, Catechol-o-methyltransferase polymorphisms predict opioid consumption in postoperative pain., Anesth Analg
Matic M et al., 2014, Rescue morphine in mechanically ventilated newborns associated with combined OPRM1 and COMT genotype., Pharmacogenomics
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
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
Landau R et al., 2013, The effect of OPRM1 and COMT genotypes on the analgesic response to intravenous fentanyl labor analgesia., Anesth Analg
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
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
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
Wang et al., 2003, Involvement of CYP3A4, CYP2C8, and CYP2D6 in the metabolism of (R)- and (S)-methadone in vitro., Drug Metab. Dispos.
Lieb B et al., 2009, Intensity of opiate withdrawal in relation to the 825C>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., 2013, Association of genetic variation in pharmacodynamic factors with methadone dose required for effective treatment of opioid addiction., Pharmacogenomics
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
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.
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
Crettol S et al., 2008, Association of dopamine and opioid receptor genetic polymorphisms with response to methadone maintenance treatment., Prog Neuropsychopharmacol Biol Psychiatry
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
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.

METHADONE GAD1

Interaction Score: 4.42

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
31866536

Sources:
PharmGKB
METHADONE CYP2A7P1

Interaction Score: 4.42

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
28320034

Sources:
PharmGKB
METHADONE TXNRD2

Interaction Score: 2.21

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
32407152

Sources:
PharmGKB
METHADONE CCL11

Interaction Score: 1.47

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
29222992

Sources:
PharmGKB
METHADONE NGF

Interaction Score: 1.32

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23651024 21358750

Sources:
PharmGKB
METHADONE CDH2

Interaction Score: 1.1

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
METHADONE KCNJ6

Interaction Score: 1.1

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
20220551

Sources:
PharmGKB
METHADONE PNOC

Interaction Score: 1.1

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
METHADONE COMT

Interaction Score: 0.97

Interaction Types & Directionality:

n/a

Interaction Info:

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

Sources:
PharmGKB
METHADONE ALDH5A1

Interaction Score: 0.88

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
24230997

Sources:
PharmGKB
METHADONE CYP2B6

Interaction Score: 0.78

Interaction Types & Directionality:

n/a

Interaction Info:

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

Sources:
DTC PharmGKB
METHADONE ANKK1

Interaction Score: 0.37

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23651024

Sources:
PharmGKB
METHADONE GNB3

Interaction Score: 0.34

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
19303909

Sources:
PharmGKB
METHADONE UGT2B7

Interaction Score: 0.32

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22676193 17178267

Sources:
PharmGKB
METHADONE TH

Interaction Score: 0.32

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
6125371

Sources:
NCI
METHADONE LEP

Interaction Score: 0.29

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
15717844

Sources:
NCI
METHADONE OPRD1

Interaction Score: 0.22

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
19843777 31907389 12405865

Sources:
PharmGKB
METHADONE OPRM1

Interaction Score: 0.19

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
14991152 11933204 17016423 17139284 17850768 19717013 12405865

Sources:
TdgClinicalTrial TEND
METHADONE BDNF

Interaction Score: 0.14

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23651024 18182069

Sources:
NCI PharmGKB
METHADONE ACHE

Interaction Score: 0.11

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
8149590

Sources:
NCI
METHADONE NTRK2

Interaction Score: 0.11

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23651024

Sources:
PharmGKB
METHADONE SLC6A4

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
29333880

Sources:
PharmGKB
METHADONE DRD2

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
25556837 23651024 21902500 19373123 18687376

Sources:
PharmGKB
METHADONE OPRK1

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
31940240

Sources:
PharmGKB
METHADONE NR1I2

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
METHADONE KCNH2

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
14999113 17329992

Sources:
PharmGKB
METHADONE ABCB1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
15876424

Sources:
NCI
METHADONE CYP3A4

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
9187528 21902501 12756206

Sources:
NCI PharmGKB

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:

Trial Name	-
Novel drug target	Established target

METHADONE Drug Record

METHADONE chembl:CHEMBL651 Approved

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 31866536

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 28320034

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 32407152

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 29222992

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 23651024 21358750

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 20220551

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

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

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 24230997

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

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

Sources: DTC PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 23651024

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 19303909

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 22676193 17178267

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 6125371

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 15717844

Sources: NCI

Interaction Types & Directionality: agonist (activating)

Interaction Info:

PMIDs: 19843777 31907389 12405865

Sources: PharmGKB

Interaction Types & Directionality: agonist (activating)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 14991152 11933204 17016423 17139284 17850768 19717013 12405865

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 23651024 18182069

Interaction Types & Directionality:

n/a

PMIDs:
31866536

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
28320034

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
32407152

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
29222992

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
23651024 21358750

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
20220551

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

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

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
24230997

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

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

Sources:
DTC PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
23651024

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
19303909

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
22676193 17178267

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
6125371

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
15717844

Sources:
NCI

Interaction Types & Directionality:

agonist (activating)

PMIDs:
19843777 31907389 12405865

Sources:
PharmGKB

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
14991152 11933204 17016423 17139284 17850768 19717013 12405865

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

n/a

PMIDs:
23651024 18182069

Sources:
NCI PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
8149590

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
23651024

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
29333880

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
25556837 23651024 21902500 19373123 18687376

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
31940240

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
14999113 17329992

Sources:
PharmGKB

Interaction Types & Directionality:

n/a