Drug/Small Molecule:
methadone

PharmGKB contains no dosing guidelines for this drug/small molecule. To report known genotype-based dosing guidelines, or if you are interested in developing guidelines, click here.

PharmGKB contains no drug labels with pharmacogenomic information for this drug/small molecule. To report a drug label with PGx, click here.

PharmGKB contains no Clinical Variants that meet the highest level of criteria.

To see more Clinical Variants with lower levels of criteria, click the button at the bottom of the page.

Disclaimer: The PharmGKB's clinical annotations reflect expert consensus based on clinical evidence and peer-reviewed literature available at the time they are written and are intended only to assist clinicians in decision-making and to identify questions for further research. New evidence may have emerged since the time an annotation was submitted to the PharmGKB. The annotations are limited in scope and are not applicable to interventions or diseases that are not specifically identified.

The annotations do not account for individual variations among patients, and cannot be considered inclusive of all proper methods of care or exclusive of other treatments. It remains the responsibility of the health-care provider to determine the best course of treatment for a patient. Adherence to any guideline is voluntary, with the ultimate determination regarding its application to be made solely by the clinician and the patient. PharmGKB assumes no responsibility for any injury or damage to persons or property arising out of or related to any use of the PharmGKB clinical annotations, or for any errors or omissions.

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This is a non-comprehensive list of genetic tests with pharmacogenetics relevance, typically submitted by the manufacturer and manually curated by PharmGKB. The information listed is provided for educational purposes only and does not constitute an endorsement of any listed test or manufacturer.

A more complete listing of genetic tests is found at the Genetic Testing Registry (GTR).

PGx Test Variants Assayed Gene?

The table below contains information about pharmacogenomic variants on PharmGKB. Please follow the link in the "Variant" column for more information about a particular variant. Each link in the "Variant" column leads to the corresponding PharmGKB Variant Page. The Variant Page contains summary data, including PharmGKB manually curated information about variant-drug pairs based on individual PubMed publications. The PMIDs for these PubMed publications can be found on the Variant Page.

The tags in the first column of the table indicate what type of information can be found on the corresponding Variant Page.

Links in the "Gene" column lead to PharmGKB Gene Pages.

Gene ? Variant?
(138)
Alternate Names / Tag SNPs ? Drugs ? Alleles ?
(+ chr strand)
Function ? Amino Acid?
Translation
No VIP available No VIP available VA CYP2B6 *1 N/A N/A N/A
No VIP available No VIP available VA CYP2B6 *6 N/A N/A N/A
No VIP available No Clinical Annotations available VA
rs1045280 1037C>T, 4226012C>T, 4622638C>T, 786+54C>T, 795C>T, 840C>T, 903C>T, Ser265=, Ser280=, Ser301=
C > T
Not Available
Ser265Ser
No VIP available No Clinical Annotations available VA
rs1045642 208920T>A, 208920T>C, 25171488A>G, 25171488A>T, 3435T>A, 3435T>C, 87138645A>G, 87138645A>T, ABCB1*6, ABCB1: 3435C>T, ABCB1: C3435T, ABCB1: c.3435C>T, ABCB1:3435C>T, Ile1145=, Ile1145Ile, MDR1 3435C>T, MDR1 C3435T, PGP C3435T, c.3435C>T, mRNA 3853C>T
A > T
A > G
Synonymous
Ile1145Ile
No VIP available No Clinical Annotations available VA
rs1076560 113283688C>A, 16846104C>A, 67314G>T, 724-83G>T, 811-83G>T
C > A
Intronic
No VIP available CA VA
rs10835210 -128-15437G>T, -21-15778G>T, -421-21G>T, -58-21G>T, 25-15778G>T, 27635910C>A, 27695910C>A, 4-15778G>T, 52696G>T, 585+15135C>A, 586-1214C>A, 586-2619C>A, 655-2619C>A, 655-934C>A, 67-15778G>T
C > A
Intronic
No VIP available No Clinical Annotations available VA
rs11030118 -1356C>T, -1374C>T, -1481C>T, -2110C>T, -22+17995C>T, -22+18830C>T, -22+18913C>T, -22+19128C>T, -241C>T, -480C>T, -557C>T, -604C>T, -862C>T, -967C>T, 25543C>T, 27663063G>A, 27723063G>A, 3+19896C>T
G > A
5' Flanking
No VIP available No Clinical Annotations available VA
rs11030119 -22+12956C>T, -22+13791C>T, -22+13874C>T, -22+14089C>T, 20504C>T, 27668102G>A, 27728102G>A, 3+14857C>T
G > A
Intronic
No VIP available No Clinical Annotations available VA
rs1128503 1236T>C, 167964T>C, 25212444A>G, 87179601A>G, ABCB1 1236C>T, ABCB1*8, ABCB1: c.1236T>C, ABCB1:1236C>T, ABCB1:1236T>C, Gly412=, Gly412Gly, mRNA 1654T>C, p.Gly412Gly
A > G
Synonymous
Gly412Gly
No VIP available No Clinical Annotations available VA
rs11940316 -1112T>C, 10171794T>C, 69961127T>C
T > C
5' Flanking
No VIP available No Clinical Annotations available VA
rs12233719 10173116G>T, 211G>T, 69962449G>T, Ala71Ser, UGT2B7*3, UGT2B7:211G>T, UGT2B7:A71S
G > T
G > A
Missense
Ala71Thr
Ala71Ser
No VIP available CA VA
rs1491850 27689725T>C, 27749725T>C
T > C
Not Available
No VIP available No Clinical Annotations available VA
rs1714984 122-1135A>G, 12221075A>G, 12617701A>G, 53495A>G
A > G
Intronic
No VIP available No Clinical Annotations available VA
rs1799971 -11+28644A>G, 118A>G, 154360797A>G, 34162A>G, 397A>G, 47+29103A>G, 58530254A>G, Asn133Asp, Asn40Asp, OPRM1: A118G
A > G
Missense
Asn40Asp
No VIP available No Clinical Annotations available VA
rs1799978 -585A>G, 113346351T>C, 16908767T>C, 4651A>G, DRD2: -241A>G, DRD2:A-241G
T > C
5' Flanking
No VIP available No Clinical Annotations available VA
rs1800497 113270828G>A, 16833244G>A, 17316G>A, 2137G>A, 32806C>T, DRD2 Taq1A, DRD2:32806C>T, DRD2:Taq1A, DRD2:Taq1A A1, DRD2:TaqIA allele, Glu713Lys, Taq1A
G > A
Missense
Glu713Lys
No VIP available No Clinical Annotations available VA
rs1861591 107416927T>C, 159-957A>G, 69560233T>C
T > C
Intronic
No VIP available CA VA
rs1948308 16780789G>A, 2125-18864G>A, 2173-18864G>A, 337792G>A, 87616257G>A
G > A
Intronic
No VIP available No Clinical Annotations available VA
rs1967554 -129+2152T>G, -22+21499T>G, -22+2152T>G, -22+2170T>G, -22+22334T>G, -22+22417T>G, -22+22632T>G, -22+2664T>G, -22+2969T>G, -22+3285T>G, -422+2959T>G, -59+2959T>G, 1120A>C, 1278A>C, 1877A>C, 24+1370T>G, 27659559A>C, 27719559A>C, 29047T>G, 3+23400T>G, 66+2959T>G
A > C
Intronic
No VIP available No Clinical Annotations available VA
rs2030324 -22+14143T>C, -22+14978T>C, -22+15061T>C, -22+15276T>C, 21691T>C, 27666915A>G, 27726915A>G, 3+16044T>C
A > G
Intronic
No VIP available No Clinical Annotations available VA
rs2032582 186947T>A, 186947T>G, 25193461A>C, 25193461A>T, 2677A, 2677G, 2677T, 2677T>A, 2677T>G, 3095G>T/A, 87160618A>C, 87160618A>T, 893 Ala, 893 Ser, 893 Thr, ABCB1*7, ABCB1: 2677G>T/A, ABCB1: 2677T/A>G, ABCB1: A893S, ABCB1: G2677T/A, ABCB1: c.2677G>T/A, ABCB1:2677G>A/T, ABCB1:2677G>T/A, ABCB1:A893T, Ala893Ser/Thr, MDR1, MDR1 G2677T/A, Ser893Ala, Ser893Thr, mRNA 3095G>T/A, p.Ala893Ser/Thr
A > C
A > T
Missense
Ser893Ala
Ser893Thr
No VIP available No Clinical Annotations available VA
rs2036657 *825G>A, *931G>A, 2252G>A, 4228533G>A, 4625159G>A
G > A
3' Flanking
No VIP available No Clinical Annotations available VA
rs2070995 206732A>G, 24748836T>C, 39086965T>C, 495A>G, Pro165=
T > C
Synonymous
Pro165Pro
No VIP available CA VA
rs2120266 1397-19604G>A, 1397-25807G>A, 16620883G>A, 177886G>A, 87456351G>A
G > A
Intronic
No VIP available CA VA
rs2239622 -136-1338T>C, 115837709A>G, 48149T>C, 85809627A>G
A > G
Intronic
No VIP available No Clinical Annotations available VA
rs2242480 1023+12G>A, 1026+12G>A, 25343G>A, 37394309C>T, 99361466C>T
C > T
Intronic
No VIP available No Clinical Annotations available VA
rs2246709 21090T>C, 37398562A>G, 670+258T>C, 99365719A>G
A > G
Intronic
No VIP available CA VA
rs2279343 13783481A>G, 23060A>G, 41515263A>G, 785A>G, CYP2B6*4, CYP2B6:18053A>G, CYP2B6:785A>G, CYP2B6:K262R, CYP2B6:Lys262Arg, Lys262Arg, part of CYP2B6*6
A > G
Missense
Lys262Arg
No VIP available CA VA
rs2283265 113285536C>A, 16847952C>A, 65466G>T, 723+607G>T, 724-353G>T
C > A
Intronic
No VIP available CA VA
rs2289658 16727902T>C, 1717-7T>C, 1765-7T>C, 284905T>C, 87563370T>C
T > C
Intronic
No VIP available CA VA
rs2378676 16783955A>C, 2125-15698A>C, 2173-15698A>C, 340958A>C, 87619423A>C
A > C
Intronic
No VIP available No Clinical Annotations available VA
rs28365062 10174938A>G, 69964271A>G, 735A>G, Thr245=
A > G
Synonymous
Thr245Thr
No VIP available No Clinical Annotations available VA
rs3211371 13790933C>T, 1459C>T, 30512C>T, 41522715C>T, Arg487Cys, CYP2B6*5, CYP2B6*7, CYP2B6:1459C>T, CYP2B6:Arg487Cys, part of CYP2B6*1C
C > T
Missense
Arg487Cys
No VIP available No Clinical Annotations available VA
rs34230287 -159C>T, -387C>T, 4217004C>T, 4613630C>T
C > T
5' Flanking
No VIP available No Clinical Annotations available VA
rs3735451 1414-124A>G, 1417-124A>G, 30834A>G, 37388818T>C, 99355975T>C
T > C
Intronic
No VIP available CA VA
rs3745274 13781059G>T, 20638G>T, 41512841G>T, 516G>T, CYP2B6*6, CYP2B6:516G>T, CYP2B6:Gln172His, Gln172His, Q172H
G > T
Missense
Gln172His
No VIP available No Clinical Annotations available VA
rs3786047 23+1059A>G, 251+1059A>G, 4218472A>G, 4615098A>G
A > G
Intronic
No VIP available No Clinical Annotations available VA
rs4292394 10183616C>G, 1059C>G, 69972949C>G, Leu353=
C > G
Synonymous
Leu353Leu
No VIP available CA VA
rs4358872 16765501T>G, 2124+30537T>G, 2172+30537T>G, 322504T>G, 87600969T>G
T > G
Intronic
No VIP available No Clinical Annotations available VA
rs45482602 13783473C>A, 13783473C>T, 23052C>A, 23052C>T, 41515255C>A, 41515255C>T, 777C>A, 777C>T, Ser259=, Ser259Arg
C > A
Missense
Ser259Arg
No VIP available No Clinical Annotations available VA
rs4554144 -1684C>T, 10171222C>T, 69960555C>T
C > T
5' Flanking
No VIP available No Clinical Annotations available VA
rs4646437 21726C>T, 37397926G>A, 671-202C>T, 671-205C>T, 99365083G>A
G > A
Intronic
No VIP available No Clinical Annotations available VA
rs4646440 1023+608C>T, 1026+608C>T, 25939C>T, 37393713G>A, 99360870G>A
G > A
Intronic
No VIP available No Clinical Annotations available VA
rs4648317 -32+14266C>T, 113331532G>A, 16893948G>A, 19470C>T
G > A
Intronic
No VIP available No Clinical Annotations available VA
rs4680 1-5G>A, 19951271G>A, 27009G>A, 3103421G>A, 322G>A, 472G>A, COMP: Val158Met, COMT:Val108Met, Val108Met, Val158Met
G > A
5' Flanking
Val158Met
No VIP available CA VA
rs4877900 16796850C>T, 2125-2803C>T, 2173-2803C>T, 353853C>T, 87632318C>T
C > T
Intronic
No VIP available No Clinical Annotations available VA
rs5443 10501C>T, 47295C>T, 6894875C>T, 6954875C>T, 825C>T, GNB3:825C>T, GNB3:Ser275Ser, Ser275=
C > T
Synonymous
Ser275Ser
No VIP available CA VA
rs558025 115330A>G, 1164+29358A>G, 154441965A>G, 58611422A>G
A > G
Intronic
No VIP available CA VA
rs6275 113283477A>G, 16845893A>G, 67525T>C, 852T>C, 939T>C, His284=, His313=
A > G
Synonymous
His284His
No VIP available No Clinical Annotations available VA
rs6277 113283459G>A, 16845875G>A, 67543C>T, 870C>T, 957C>T, C957T, DRD2: C957T, DRD2:1035C>T, DRD2:1122C>T, DRD2:957C>T, Pro290=, Pro319=
G > A
Synonymous
Pro290Pro
No VIP available No Clinical Annotations available VA
rs6600879 -1852C>G, 10171054C>G, 69960387C>G
C > G
5' Flanking
No VIP available No Clinical Annotations available VA
rs6600880 -1759T>A, 10171147T>A, 69960480T>A
T > A
5' Flanking
No VIP available No Clinical Annotations available VA
rs6600893 *251+196T>C, 10189568T>C, 69978901T>C
T > C
Intronic
No VIP available CA VA
rs7118900 113266821G>A, 13309G>A, 16829237G>A, 715G>A, Ala239Thr
G > A
Missense
Ala239Thr
No VIP available No Clinical Annotations available VA
rs7127507 -129+6827A>G, -22+26174A>G, -22+27009A>G, -22+27092A>G, -22+27307A>G, -22+6827A>G, -22+6845A>G, -22+7339A>G, -22+7644A>G, -22+7960A>G, -422+7634A>G, -59+7634A>G, 1342+2197T>C, 24+6045A>G, 27654884T>C, 27714884T>C, 3+28075A>G, 33722A>G, 586-4141T>C, 66+7634A>G, 744-4141T>C
T > C
Intronic
No VIP available No Clinical Annotations available VA
rs7438135 -900G>A, 10172006G>A, 69961339G>A
G > A
5' Flanking
No VIP available No Clinical Annotations available VA
rs7439366 10175005T>C, 69964338T>C, 802T>C, Tyr268His, UGT2B7*2, UGT2B7:802C>T, UGT2B7:H268Y, UGT2B7Y
T > C
Missense
Tyr268His
No VIP available No Clinical Annotations available VA
rs7662029 -327A>G, 10172579A>G, 69961912A>G
A > G
5' Flanking
No VIP available No Clinical Annotations available VA
rs7668258 -161T>C, 10172745T>C, 69962078T>C
T > C
5' Flanking
VIP No Clinical Annotations available No Variant Annotations available
rs776746 12083G>A, 219-237G>A, 321-1G>A, 37303382C>T, 581-237G>A, 689-1G>A, 99270539C>T, CYP3A5*1, CYP3A5*3, CYP3A5*3C, CYP3A5:6986A>G, g.6986A>G, intron 3 splicing defect, rs776746 A>G
C > T
Acceptor
No VIP available CA VA
rs7934165 -22+10208C>T, -22+9075C>T, -22+9910C>T, -22+9993C>T, 16623C>T, 27671983G>A, 27731983G>A, 3+10976C>T
G > A
Intronic
No VIP available No Clinical Annotations available VA
rs9479757 154411344G>A, 343+31G>A, 400+31G>A, 58580801G>A, 643+31G>A, 84709G>A, 922+31G>A
G > A
Intronic
No VIP available No Clinical Annotations available VA
rs988748 -1923G>C, -22+16313G>C, -22+17148G>C, -22+17231G>C, -22+17446G>C, 23861G>C, 27664745C>G, 27724745C>G, 3+18214G>C
C > G
Intronic
Alleles, Functions, and Amino Acid Translations are all sourced from dbSNP 138
2D structure from PubChem
provided by PubChem

Overview

Generic Names
  • (+/-)-Methadone
  • (+/-)-Methadone hydrochloride
  • DL-Methadone hydrochloride
  • Methadon
  • Methadone HCL
  • Methadone hydrochloride
  • Phenadone hydrochloride
  • dl-Methadone
Trade Names
  • Adanon
  • Adanon hydrochloride
  • Adolan
  • Algidon
  • Algolysin
  • Algovetin
  • Althose hydrochloride
  • Amidon
  • Amidone
  • Biscuits
  • Butalgin
  • Depridol
  • Diaminon
  • Diaminon hydrochloride
  • Dollies
  • Dolly
  • Dolofin hydrochloride
  • Dolohepton
  • Dolophin
  • Dolophin hydrochloride
  • Dolophine
  • Dolophine HCL
  • Fenadon
  • Fenadone
  • Heptadon
  • Heptadone
  • Heptanon
  • Ketalgin
  • Ketalgin hydrochloride
  • Mecodin
  • Mephenon
  • Methadone HCL Intensol
  • Methadone M
  • Methadose
  • Methaquaione
  • Miadone
  • Moheptan
  • Phenadone
  • Physeptone
  • Polamidon
  • Polamidone
  • Tussol
  • Westadone
Brand Mixture Names
  • (+/-)-Tussal

PharmGKB Accession Id:
PA450401

Description

A synthetic opioid that is used as the hydrochloride. It is an opioid analgesic that is primarily a mu-opioid agonist. It has actions and uses similar to those of morphine. It also has a depressant action on the cough center and may be given to control intractable cough associated with terminal lung cancer. Methadone is also used as part of the treatment of dependence on opioid drugs, although prolonged use of methadone itself may result in dependence. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1082-3)

Source: Drug Bank

Indication

For the treatment of dry cough, drug withdrawal syndrome, opioid type drug dependence, and pain.

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

Mechanism of Action

Methadone is a mu-agonist; a synthetic opioid analgesic with multiple actions qualitatively similar to those of morphine, the most prominent of which involves the central nervous system and organs composed of smooth muscle. The principal therapeutic uses for methadone are for analgesia and for detoxification or maintenance in opioid addiction. The methadone abstinence syndrome, although qualitatively similar to that of morphine, differs in that the onset is slower, the course is more prolonged, and the symptoms are less severe. Some data also indicate that methadone acts as an antagonist at the N-methyl-D-aspartate (NMDA) receptor. The contribution of NMDA receptor antagonism to methadone's efficacy is unknown. Other NMDA receptor antagonists have been shown to produce neurotoxic effects in animals.

Source: Drug Bank

Pharmacology

Methadone is a synthetic opioid analgesic with multiple actions quantitatively similar to those at morphine, the most prominent of which involve the central nervous system and organs composed of smooth muscle. However, Methadone is more active and more toxic than morphine. Methadone is indicated for relief of severe pain, for detoxification treatment of narcotic addiction, and for temporary maintenance treatment of narcotic addiction. The principal actions of therapeutic value are analgesia and sedation and detoxification or temporary maintenance in narcotic addiction. The Methadone abstinence syndrome, although qualitatively similar to that of morphine, differs in that the onset is slower, the course is more prolonged, and the symptoms are less severe.

Source: Drug Bank

Food Interaction

Take without regard to meals. Avoid alcohol. Usually diluted in fruit juice.

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Hepatic. Cytochrome P450 enzymes, primarily CYP3A4, CYP2B6, and CYP2C19 and to a lesser extent CYP2C9 and CYP2D6, are responsible for conversion of methadone to EDDP and other inactive metabolites, which are excreted mainly in the urine.

Source: Drug Bank

Protein Binding

In plasma, methadone is predominantly bound to alpha1-acid glycoprotein (85% to 90%).

Source: Drug Bank

Absorption

Well absorbed following oral administration. The bioavailability of methadone ranges between 36 to 100%.

Source: Drug Bank

Half-Life

24-36 hours

Source: Drug Bank

Toxicity

In severe overdosage, particularly by the intravenous route, apnea, circulatory collapse, cardiac arrest, and death may occur.

Source: Drug Bank

Clearance

  • 1.4 to 126 L/h

Source: Drug Bank

Route of Elimination

The elimination of methadone is mediated by extensive biotransformation, followed by renal and fecal excretion.
Unmetabolized methadone and its metabolites are excreted in urine to a variable degree.

Source: Drug Bank

Volume of Distribution

  • 1.0 to 8.0 L/kg

Source: Drug Bank

Chemical Properties

Chemical Formula

C21H27NO

Source: Drug Bank

Isomeric SMILES

CCC(=O)C(CC(C)N(C)C)(c1ccccc1)c2ccccc2

Source: OpenEye

Canonical SMILES

CCC(=O)C(CC(C)N(C)C)(C1=CC=CC=C1)C1=CC=CC=C1

Source: Drug Bank

Average Molecular Weight

309.4452

Source: Drug Bank

Monoisotopic Molecular Weight

309.209264491

Source: Drug Bank

PharmGKB Curated Pathways

Pathways created internally by PharmGKB based primarily on literature evidence.

  1. Antiarrhythmic Pathway, Pharmacodynamics
    Pharmacodynamic pathway of antiarrhythmic drugs in a stylized cardiac myocyte.

External Pathways

Links to non-PharmGKB pathways.

PharmGKB contains no links to external pathways for this drug. To report a pathway, click here.

Genes that are associated with this drug in PharmGKB's database based on (1) variant annotations, (2) literature review, (3) pathways or (4) information automatically retrieved from DrugBank, depending on the "evidence" and "source" listed below.

Curated Information ?

Drug Targets

Gene Description
CHRNA10 (source: Drug Bank)
GRIN3A (source: Drug Bank)
OPRD1 (source: Drug Bank)
OPRM1 (source: Drug Bank)

Drug Interactions

Drug Description
methadone The protease inhibitor decreases the effect of methadone (source: Drug Bank)
methadone The protease inhibitor, amprenavir, may decrease the effect of methadone. (source: Drug Bank)
methadone Decreases levels of methadone (source: Drug Bank)
methadone Decreases levels of methadone (source: Drug Bank)
methadone Increases the effect of the narcotic (source: Drug Bank)
methadone Increases the effect of the narcotic (source: Drug Bank)
methadone The antiretroviral agent decreases the effect of mathadone (source: Drug Bank)
methadone The antiretroviral agent decreases the effect of mathadone (source: Drug Bank)
methadone Fluvoxamine increases the effect and toxicity of methadone (source: Drug Bank)
methadone Fluvoxamine increases the effect and toxicity of methadone (source: Drug Bank)
methadone The protease inhibitor decreases the effect of methadone (source: Drug Bank)
methadone The protease inhibitor, fosamprenavir, may decrease the effect of methadone. (source: Drug Bank)
methadone The hydantoin decreases the effect of methadone (source: Drug Bank)
amobarbital The barbiturate decreases the effect of methadone (source: Drug Bank)
amobarbital The barbiturate, amobarbital, decreases the effect of methadone. (source: Drug Bank)
amprenavir The protease inhibitor decreases the effect of methadone (source: Drug Bank)
amprenavir The protease inhibitor, amprenavir, may decrease the effect of methadone. (source: Drug Bank)
aprobarbital The barbiturate decreases the effect of methadone (source: Drug Bank)
aprobarbital The barbiturate, aprobarbital, decreases the effect of methadone. (source: Drug Bank)
butabarbital The barbiturate decreases the effect of methadone (source: Drug Bank)
butabarbital The barbiturate, butabarbital, decreases the effect of methadone. (source: Drug Bank)
butalbital The barbiturate decreases the effect of methadone (source: Drug Bank)
butalbital The barbiturate, butalbital, decreases the effect of methadone. (source: Drug Bank)
butethal The barbiturate decreases the effect of methadone (source: Drug Bank)
butethal The barbiturate, butethal, decreases the effect of methadone. (source: Drug Bank)
carbamazepine Carbamazepine decreases levels of methadone (source: Drug Bank)
carbamazepine Carbamazepine decreases levels of methadone (source: Drug Bank)
cimetidine Cimetidine increases the effect of the narcotic (source: Drug Bank)
cimetidine Cimetidine increases the effect of the narcotic (source: Drug Bank)
efavirenz The antiretroviral agent decreases the effect of methadone (source: Drug Bank)
efavirenz The antiretroviral agent decreases the effect of methadone (source: Drug Bank)
ethotoin The hydantoin decreases the effect of methadone (source: Drug Bank)
ethotoin The hydantoin decreases the effect of methadone (source: Drug Bank)
fluvoxamine Fluvoxamine increases the effect and toxicity of methadone (source: Drug Bank)
fluvoxamine Fluvoxamine increases the effect and toxicity of methadone (source: Drug Bank)
fosamprenavir The protease inhibitor decreases the effect of methadone (source: Drug Bank)
fosamprenavir The protease inhibitor, fosamprenavir, may decrease the effect of methadone. (source: Drug Bank)
fosphenytoin The hydantoin decreases the effect of methadone (source: Drug Bank)
fosphenytoin The hydantoin decreases the effect of methadone (source: Drug Bank)
heptabarbital The barbiturate decreases the effect of methadone (source: Drug Bank)
heptabarbital The barbiturate, heptabarbital, decreases the effect of methadone. (source: Drug Bank)
hexobarbital The barbiturate decreases the effect of methadone (source: Drug Bank)
hexobarbital The barbiturate, hexobarbital, decreases the effect of methadone. (source: Drug Bank)
mephenytoin The hydantoin decreases the effect of methadone (source: Drug Bank)
mephenytoin The hydantoin decreases the effect of methadone (source: Drug Bank)
methohexital The barbiturate decreases the effect of methadone (source: Drug Bank)
methohexital The barbiturate, methohexital, decreases the effect of methadone. (source: Drug Bank)
methylphenobarbital The barbiturate decreases the effect of methadone (source: Drug Bank)
methylphenobarbital The barbiturate, methylphenobarbital, decreases the effect of methadone. (source: Drug Bank)
naltrexone Naltrexone may precipitate a withdrawal syndrome in opioid-dependent individuals (source: Drug Bank)
naltrexone Naltrexone may precipitate a withdrawal syndrome in opioid-dependent individuals (source: Drug Bank)
nelfinavir Nelfinavir decreases the effect of methadone (source: Drug Bank)
nelfinavir Nelfinavir decreases the effect of methadone (source: Drug Bank)
nevirapine The antiretroviral agent decreases the effect of methadone (source: Drug Bank)
nevirapine The antiretroviral agent decreases the effect of methadone (source: Drug Bank)
pentobarbital The barbiturate decreases the effect of methadone (source: Drug Bank)
pentobarbital The barbiturate, pentobarbital, decreases the effect of methadone. (source: Drug Bank)
phenobarbital The barbiturate decreases the effect of methadone (source: Drug Bank)
phenobarbital The barbiturate, phenobarbital, decreases the effect of methadone. (source: Drug Bank)
phenytoin The hydantoin decreases the effect of methadone (source: Drug Bank)
phenytoin The hydantoin decreases the effect of methadone (source: Drug Bank)
primidone The barbiturate decreases the effect of methadone (source: Drug Bank)
primidone The barbiturate, primidone, decreases the effect of methadone. (source: Drug Bank)
quinidine The barbiturate decreases the effect of methadone (source: Drug Bank)
quinidine The barbiturate, quinidine barbiturate, decreases the effect of methadone. (source: Drug Bank)
rifabutin The rifamycin decreases the effect of methadone (source: Drug Bank)
rifabutin The rifamycin decreases the effect of methadone (source: Drug Bank)
rifampin The rifamycin decreases the effect of methadone (source: Drug Bank)
rifampin The rifamycin decreases the effect of methadone (source: Drug Bank)
rifapentine The rifamycin decreases the effect of methadone (source: Drug Bank)
rifapentine The rifamycin decreases the effect of methadone (source: Drug Bank)
ritonavir The protease inhibitor decreases the effect of methadone (source: Drug Bank)
ritonavir The protease inhibitor, ritonavir, may decrease the effect of methadone. (source: Drug Bank)
secobarbital The barbiturate decreases the effect of methadone (source: Drug Bank)
secobarbital The barbiturate, secobarbital, decreases the effect of methadone. (source: Drug Bank)
talbutal The barbiturate decreases the effect of methadone (source: Drug Bank)
talbutal The barbiturate, talbutal, decreases the effect of methadone. (source: Drug Bank)
zidovudine Methadone increases the effect and toxicity of zidovudine (source: Drug Bank)
zidovudine Methadone increases the effect and toxicity of zidovudine (source: Drug Bank)
methadone Naltrexone may precipitate a withdrawal syndrome in opioid-dependent individuals (source: Drug Bank)
methadone Naltrexone may precipitate a withdrawal syndrome in opioid-dependent individuals (source: Drug Bank)
methadone Nelfinavir decreases the effect of methadone (source: Drug Bank)
methadone Nelfinavir decreases the effect of methadone (source: Drug Bank)
methadone The antiretroviral agent decreases the effect of methadone (source: Drug Bank)
methadone The antiretroviral agent decreases the effect of methadone (source: Drug Bank)
methadone The barbiturate decreases the effect of methadone (source: Drug Bank)
methadone The barbiturate, phenobarbital, decreases the effect of methadone. (source: Drug Bank)
methadone The barbiturate decreases the effect of methadone (source: Drug Bank)
methadone The barbiturate, primidone, decreases the effect of methadone. (source: Drug Bank)
methadone The rifamycin decreases the effect of methadone (source: Drug Bank)
methadone The rifamycin decreases the effect of methadone (source: Drug Bank)
methadone The rifamycin decreases the effect of methadone (source: Drug Bank)
methadone The rifamycin decreases the effect of methadone (source: Drug Bank)
methadone Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
methadone Methadone may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
methadone Methadone may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
methadone Methadone, a CYP2D6 inhibitor, may decrease the metabolism and clearance of Tamsulosin, a CYP2D6 substrate. Monitor for changes in therapeutic/adverse effects of Tamsulosin if Methadone is initiated, discontinued, or dose changed. (source: Drug Bank)
methadone Methadone, a CYP2D6 inhibitor, may decrease the metabolism and clearance of Tamsulosin, a CYP2D6 substrate. Monitor for changes in therapeutic/adverse effects of Tamsulosin if Methadone is initiated, discontinued, or dose changed. (source: Drug Bank)
methadone Telithromycin may reduce clearance of Methadone. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Methadone if Telithromycin is initiated, discontinued or dose changed. (source: Drug Bank)
methadone Thiopental may decrease the effect of Methadone by increasing Methadone metabolism. Methadone withdrawal may occur. (source: Drug Bank)
methadone Thiopental may decrease the effect of Methadone by increasing Methadone metabolism. Methadone withdrawal may occur. (source: Drug Bank)
methadone May cause additive QTc-prolonging effects. Increased risk of ventricular arrhythmias. Consider alternate therapy. Thorough risk:benefit assessment is required prior to co-administration. (source: Drug Bank)
methadone May cause additive QTc-prolonging effects. Increased risk of ventricular arrhythmias. Consider alternate therapy. Thorough risk:benefit assessment is required prior to co-administration. (source: Drug Bank)
methadone Tipranavir, co-administered with Ritonavir, decreases the Methadone concentration. Monitor for symptoms of opiate withdrawal. (source: Drug Bank)
methadone Additive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Consider alternate therapy. A thorough risk:benefit assessment is required prior to co-administration. (source: Drug Bank)
methadone Methadone may decrease the effect of Tramadol by decreasing active metabolite production. (source: Drug Bank)
methadone Additive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
methadone The CNS depressants, Triprolidine and Methadone, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy. (source: Drug Bank)
methadone The CNS depressants, Triprolidine and Methadone, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy. (source: Drug Bank)
methadone Voriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of methadone by decreasing its metabolism. Additive QTc prolongation may also occur. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of methadone if voriconazole is initiated, discontinued or dose changed. (source: Drug Bank)
methadone Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP). (source: Drug Bank)
methadone Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated. (source: Drug Bank)
methadone Additive QTc prolongation may occur. Consider alternate therapy or use caution and monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP). (source: Drug Bank)

Curated Information ?

Relationships from National Drug File - Reference Terminology (NDF-RT)

May Treat
Contraindicated With

Publications related to methadone: 42

No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
CYP2B6 SNPs are associated with methadone dose required for effective treatment of opioid addiction. Addiction biology. 2013. Levran Orna, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Association of OPRM1 and COMT single-nucleotide polymorphisms with hospital length of stay and treatment of neonatal abstinence syndrome. JAMA : the journal of the American Medical Association. 2013. Wachman Elisha M, et al. PubMed
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Association of genetic variation in pharmacodynamic factors with methadone dose required for effective treatment of opioid addiction. Pharmacogenomics. 2013. Levran Orna, et al. PubMed
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Cytochrome P450-mediated drug metabolism in the brain. Journal of psychiatry & neuroscience : JPN. 2012. Miksys Sharon, et al. PubMed
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Reduced methadone clearance during aromatase inhibition. Journal of clinical psychopharmacology. 2012. Lu Wenjie Jessie, et al. PubMed
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PharmGKB summary: very important pharmacogene information for CYP3A5. Pharmacogenetics and genomics. 2012. Lamba Jatinder, et al. PubMed
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UGT2B7 genetic polymorphisms are associated with the withdrawal symptoms in methadone maintenance patients. Pharmacogenomics. 2012. Tian Jia-Ni, et al. PubMed
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Impact of genetic polymorphisms in ABCB1, CYP2B6, OPRM1, ANKK1 and DRD2 genes on methadone therapy in Han Chinese patients. Pharmacogenomics. 2011. Hung Chin-Chuan, et al. PubMed
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Genetic polymorphisms in CYP3A4 are associated with withdrawal symptoms and adverse reactions in methadone maintenance patients. Pharmacogenomics. 2011. Chen Chia-Hui, et al. PubMed
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beta-Arrestin2 influences the response to methadone in opioid-dependent patients. The pharmacogenomics journal. 2011. Oneda B, et al. PubMed
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Uniform assessment and ranking of opioid μ receptor binding constants for selected opioid drugs. Regulatory toxicology and pharmacology : RTP. 2011. Volpe Donna A, et al. PubMed
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Pharmacogenomics of the RNA world: structural RNA polymorphisms in drug therapy. Clinical pharmacology and therapeutics. 2011. Sadee W, et al. PubMed
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Nerve growth factor beta polypeptide (NGFB) genetic variability: association with the methadone dose required for effective maintenance treatment. The pharmacogenomics journal. 2011. Levran O, et al. PubMed
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Absorption, distribution, metabolism and excretion pharmacogenomics of drugs of abuse. Pharmacogenomics. 2011. Meyer Markus R, et al. PubMed
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Breaking Barriers in the Genomics and Pharmacogenetics of Drug Addiction. Clinical pharmacology and therapeutics. 2010. Ho M K, et al. PubMed
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Methadone adverse reaction presenting with large increase in plasma methadone binding: a case series. Journal of medical case reports. 2011. Lu Wenjie J, et al. PubMed
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KCNH2 pharmacogenomics summary. Pharmacogenetics and genomics. 2010. Oshiro Connie, et al. PubMed
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Drug-induced long QT syndrome. Pharmacological reviews. 2010. Kannankeril Prince, et al. PubMed
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OPRM1 and CYP2B6 gene variants as risk factors in methadone-related deaths. Clinical pharmacology and therapeutics. 2010. Bunten H, et al. PubMed
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Methadone: a substrate and mechanism-based inhibitor of CYP19 (aromatase). Drug metabolism and disposition: the biological fate of chemicals. 2010. Lu Wenjie Jessie, et al. PubMed
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PharmGKB summary: very important pharmacogene information for CYP2B6. Pharmacogenetics and genomics. 2010. Thorn Caroline F, et al. PubMed
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Response to methadone maintenance treatment is associated with the MYOCD and GRM6 genes. Molecular diagnosis & therapy. 2010. Fonseca Francina, et al. PubMed
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A KCNJ6 (Kir3.2, GIRK2) gene polymorphism modulates opioid effects on analgesia and addiction but not on pupil size. Pharmacogenetics and genomics. 2010. Lötsch Jörn, et al. PubMed
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Methadone induces the expression of hepatic drug-metabolizing enzymes through the activation of pregnane X receptor and constitutive androstane receptor. Drug metabolism and disposition: the biological fate of chemicals. 2009. Tolson Antonia H, et al. PubMed
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Utilization of pharmacogenomics and therapeutic drug monitoring for opioid pain management. Pharmacogenomics. 2009. Jannetto Paul J, et al. PubMed
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Cross-sectional analysis of the influence of currently known pharmacogenetic modulators on opioid therapy in outpatient pain centers. Pharmacogenetics and genomics. 2009. Lötsch Jörn, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Genetic variants altering dopamine D2 receptor expression or function modulate the risk of opiate addiction and the dosage requirements of methadone substitution. Pharmacogenetics and genomics. 2009. Doehring Alexandra, et al. PubMed
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Functional pharmacogenetics/genomics of human cytochromes P450 involved in drug biotransformation. Analytical and bioanalytical chemistry. 2008. Zanger Ulrich M, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Association of dopamine and opioid receptor genetic polymorphisms with response to methadone maintenance treatment. Progress in neuro-psychopharmacology & biological psychiatry. 2008. Crettol Séverine, et al. PubMed
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CYP2B6: new insights into a historically overlooked cytochrome P450 isozyme. Current drug metabolism. 2008. Wang Hongbing, et al. PubMed
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BDNF variability in opioid addicts and response to methadone treatment: preliminary findings. Genes, brain, and behavior. 2008. de Cid R, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
ABCB1 (MDR1) genetic variants are associated with methadone doses required for effective treatment of heroin dependence. Human molecular genetics. 2008. Levran Orna, et al. PubMed
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Pharmacogenetic treatments for drug addiction: alcohol and opiates. The American journal of drug and alcohol abuse. 2008. Haile Colin N, et al. PubMed
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Polymorphic CYP2B6: molecular mechanisms and emerging clinical significance. Pharmacogenomics. 2007. Zanger Ulrich M, et al. PubMed
Stereoselective block of hERG channel by (S)-methadone and QT interval prolongation in CYP2B6 slow metabolizers. Clinical pharmacology and therapeutics. 2007. Eap C B, et al. PubMed
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Pharmacogenetics of opioids. Clinical pharmacology and therapeutics. 2007. Somogyi Andrew A, et al. PubMed
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ABCB1 and cytochrome P450 genotypes and phenotypes: influence on methadone plasma levels and response to treatment. Clinical pharmacology and therapeutics. 2006. Crettol Séverine, et al. PubMed
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ABCB1 genetic variability and methadone dosage requirements in opioid-dependent individuals. Clinical pharmacology and therapeutics. 2006. Coller Janet K, et al. PubMed
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Modulation of the central nervous effects of levomethadone by genetic polymorphisms potentially affecting its metabolism, distribution, and drug action. Clinical pharmacology and therapeutics. 2006. Lötsch Jörn, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Methadone enantiomer plasma levels, CYP2B6, CYP2C19, and CYP2C9 genotypes, and response to treatment. Clinical pharmacology and therapeutics. 2005. Crettol Séverine, et al. PubMed
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The influence of P-glycoprotein on cerebral and hepatic concentrations of nortriptyline and its metabolites. Drug metabolism and drug interactions. 2006. Ejsing Thomas Broeng, et al. PubMed
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Med-psych drug-drug interactions update. Psychosomatics. 2002. Armstrong Scott C, et al. PubMed

LinkOuts

Web Resource:
Wikipedia
National Drug Code Directory:
64019-553-67
DrugBank:
DB00333
ChEBI:
6807
KEGG Compound:
C07163
PubChem Compound:
4095
PubChem Substance:
149416
46505722
IUPHAR Ligand:
1605
Drugs Product Database (DPD):
2247698
ChemSpider:
3953
Therapeutic Targets Database:
DAP000267
FDA Drug Label at DailyMed:
5e70e915-b946-4a80-bcc6-3f49bc30f2f5
da0a54c6-8b53-4774-8c40-e615ac8d804d

Clinical Trials

These are trials that mention methadone and are related to either pharmacogenetics or pharmacogenomics.

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Sources for PharmGKB drug information: DrugBank, Open Eye Scientific Software.