Details
Stereochemistry | RACEMIC |
Molecular Formula | C21H27NO |
Molecular Weight | 309.4452 |
Optical Activity | ( + / - ) |
Defined Stereocenters | 0 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CCC(=O)C(CC(C)N(C)C)(C1=CC=CC=C1)C2=CC=CC=C2
InChI
InChIKey=USSIQXCVUWKGNF-UHFFFAOYSA-N
InChI=1S/C21H27NO/c1-5-20(23)21(16-17(2)22(3)4,18-12-8-6-9-13-18)19-14-10-7-11-15-19/h6-15,17H,5,16H2,1-4H3
Molecular Formula | C21H27NO |
Molecular Weight | 309.4452 |
Charge | 0 |
Count |
|
Stereochemistry | RACEMIC |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 1 |
E/Z Centers | 0 |
Optical Activity | ( + / - ) |
DescriptionCurator's Comment: description was created based on several sources, including:
http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/006134s040s041lbl.pdf | https://www.drugs.com/pro/diskets.html
Curator's Comment: description was created based on several sources, including:
http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/006134s040s041lbl.pdf | https://www.drugs.com/pro/diskets.html
Methadone, sold under the brand names Dolophine among others, is an synthetic opioid that is used as the hydrochloride to treat pain and as maintenance therapy or to help with detoxification in people with opioid dependence. Methadone hydrochloride is a mu-agonist; a synthetic opioid analgesic with multiple actions qualitatively similar to those of morphine. Some data also indicate that methadone acts as an antagonist at the NMDA-receptor. The contribution of NMDA receptor antagonism to methadone’s efficacy is unknown. Most common adverse reactions are: lightheadedness, dizziness, sedation, nausea, vomiting, and sweating. Avoid use mixed agonist/antagonist and partial agonist opioid analgesics with DOLOPHINE because they may reduce analgesic effect of DOLOPHINE or precipitate withdrawal symptoms.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL233 |
3.51 nM [Ki] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Palliative | DOLOPHINE HYDROCHLORIDE Approved UseFor the treatment of moderate to severe pain not responsive to non-narcotic analgesics. For detoxification treatment of opioid addiction (heroin or other morphine-like drugs). For maintenance treatment of opioid addiction (heroin or other morphine-like drugs), in conjunction with appropriate social and medical services. Note – Outpatient maintenance and outpatient detoxification treatment may be provided only by Opioid Treatment Programs (OTPs) certified by the Federal Substance Abuse and Mental Health Services Administration (SAMHSA) and registered by the Drug Enforcement Administration (DEA). This does not preclude the maintenance treatment of a patient with concurrent opioid addiction who is hospitalized for conditions other than opioid addiction and who requires temporary maintenance during the critical period of his/her stay, or of a patient whose enrollment has been verified in a program which has been certified for maintenance treatment with methadone. Launch Date1947 |
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Palliative | DOLOPHINE HYDROCHLORIDE Approved UseFor the treatment of moderate to severe pain not responsive to non-narcotic analgesics. For detoxification treatment of opioid addiction (heroin or other morphine-like drugs). For maintenance treatment of opioid addiction (heroin or other morphine-like drugs), in conjunction with appropriate social and medical services. Note – Outpatient maintenance and outpatient detoxification treatment may be provided only by Opioid Treatment Programs (OTPs) certified by the Federal Substance Abuse and Mental Health Services Administration (SAMHSA) and registered by the Drug Enforcement Administration (DEA). This does not preclude the maintenance treatment of a patient with concurrent opioid addiction who is hospitalized for conditions other than opioid addiction and who requires temporary maintenance during the critical period of his/her stay, or of a patient whose enrollment has been verified in a program which has been certified for maintenance treatment with methadone. Launch Date1947 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
494 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/15151520/ |
76 mg 1 times / day steady-state, oral dose: 76 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
METHADONE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
40.2 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/22621465/ |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
METHADONE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
548 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/8641323/ |
0.89 mg/kg 1 times / day steady-state, oral dose: 0.89 mg/kg route of administration: Oral experiment type: STEADY-STATE co-administered: |
METHADONE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
54 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/8641323/ |
0.89 mg/kg 1 times / day steady-state, oral dose: 0.89 mg/kg route of administration: Oral experiment type: STEADY-STATE co-administered: |
2-ETHYLIDENE-1,5-DIMETHYL-3,3-DIPHENYLPYRROLIDINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
8.27 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/15151520/ |
76 mg 1 times / day steady-state, oral dose: 76 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
METHADONE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
1073 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/22621465/ |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
METHADONE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
8.54 mg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/8641323/ |
0.89 mg/kg 1 times / day steady-state, oral dose: 0.89 mg/kg route of administration: Oral experiment type: STEADY-STATE co-administered: |
METHADONE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
0.61 mg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/8641323/ |
0.89 mg/kg 1 times / day steady-state, oral dose: 0.89 mg/kg route of administration: Oral experiment type: STEADY-STATE co-administered: |
2-ETHYLIDENE-1,5-DIMETHYL-3,3-DIPHENYLPYRROLIDINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
39 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/15151520/ |
76 mg 1 times / day steady-state, oral dose: 76 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
METHADONE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
39.3 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/22621465/ |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
METHADONE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
31.2 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/8641323/ |
0.89 mg/kg 1 times / day steady-state, oral dose: 0.89 mg/kg route of administration: Oral experiment type: STEADY-STATE co-administered: |
METHADONE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
Doses
Dose | Population | Adverse events |
---|---|---|
10 mg 3 times / day multiple, intravenous Recommended Dose: 10 mg, 3 times / day Route: intravenous Route: multiple Dose: 10 mg, 3 times / day Sources: |
pregnant, adult Health Status: pregnant Age Group: adult Sex: F Sources: |
Other AEs: Withdrawal syndrome neonatal... Other AEs: Withdrawal syndrome neonatal Sources: |
10 mg 3 times / day multiple, intravenous Recommended Dose: 10 mg, 3 times / day Route: intravenous Route: multiple Dose: 10 mg, 3 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
Other AEs: Respiratory depression, Addiction... Other AEs: Respiratory depression (grade 5) Sources: Addiction QT interval prolonged (grade 5) |
20 mg single, oral Recommended Dose: 20 mg Route: oral Route: single Dose: 20 mg Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
Other AEs: Respiratory depression, QT interval prolonged... Other AEs: Respiratory depression (grade 5) Sources: QT interval prolonged Arrhythmia (serious) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Withdrawal syndrome neonatal | 10 mg 3 times / day multiple, intravenous Recommended Dose: 10 mg, 3 times / day Route: intravenous Route: multiple Dose: 10 mg, 3 times / day Sources: |
pregnant, adult Health Status: pregnant Age Group: adult Sex: F Sources: |
|
Addiction | 10 mg 3 times / day multiple, intravenous Recommended Dose: 10 mg, 3 times / day Route: intravenous Route: multiple Dose: 10 mg, 3 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
|
QT interval prolonged | grade 5 | 10 mg 3 times / day multiple, intravenous Recommended Dose: 10 mg, 3 times / day Route: intravenous Route: multiple Dose: 10 mg, 3 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
Respiratory depression | grade 5 | 10 mg 3 times / day multiple, intravenous Recommended Dose: 10 mg, 3 times / day Route: intravenous Route: multiple Dose: 10 mg, 3 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
QT interval prolonged | 20 mg single, oral Recommended Dose: 20 mg Route: oral Route: single Dose: 20 mg Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
|
Respiratory depression | grade 5 | 20 mg single, oral Recommended Dose: 20 mg Route: oral Route: single Dose: 20 mg Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
Arrhythmia | serious | 20 mg single, oral Recommended Dose: 20 mg Route: oral Route: single Dose: 20 mg Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://pubmed.ncbi.nlm.nih.gov/20484152/ Page: 8.0 |
major [Inhibition 0.6 uM] | |||
no | ||||
no | ||||
no | ||||
no | ||||
Sources: https://pubmed.ncbi.nlm.nih.gov/20484152/ Page: 8.0 |
unlikely | |||
yes [Ki 100 uM] | ||||
yes [Ki 2.5 uM] |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
yes | ||||
yes | yes (co-administration study) Comment: CYP450 inducers: concomitant administration of rifampin resulted in a marked reduction in serum methadone levels and a concurrent appearance of withdrawal symptoms; phenytoin administration resulted in an approximately 50% reduction in methadone exposure and withdrawal symptoms occurred concurrently. CYP450 inhibitors: Repeat dose administration of oral voriconazole increased the peak plasma concentration (Cmax) and AUC of (R)-methadone by 31% and 47%, respectively, in subjects receiving a methadone maintenance dose. The Cmax and AUC of (S)-methadone increased by 65% and 103%, respectively Page: 29.0 |
|||
yes | yes (co-administration study) Comment: CYP450 inducers: concomitant administration of rifampin resulted in a marked reduction in serum methadone levels and a concurrent appearance of withdrawal symptoms; phenytoin administration resulted in an approximately 50% reduction in methadone exposure and withdrawal symptoms occurred concurrently. CYP450 inhibitors: Repeat dose administration of oral voriconazole increased the peak plasma concentration (Cmax) and AUC of (R)-methadone by 31% and 47%, respectively, in subjects receiving a methadone maintenance dose. The Cmax and AUC of (S)-methadone increased by 65% and 103%, respectively Page: 29.0 |
|||
yes | yes (co-administration study) Comment: CYP450 inducers: concomitant administration of rifampin resulted in a marked reduction in serum methadone levels and a concurrent appearance of withdrawal symptoms; phenytoin administration resulted in an approximately 50% reduction in methadone exposure and withdrawal symptoms occurred concurrently. CYP450 inhibitors: Repeat dose administration of oral voriconazole increased the peak plasma concentration (Cmax) and AUC of (R)-methadone by 31% and 47%, respectively, in subjects receiving a methadone maintenance dose. The Cmax and AUC of (S)-methadone increased by 65% and 103%, respectively Page: 29.0 |
|||
yes | yes (co-administration study) Comment: CYP450 inducers: concomitant administration of rifampin resulted in a marked reduction in serum methadone levels and a concurrent appearance of withdrawal symptoms; phenytoin administration resulted in an approximately 50% reduction in methadone exposure and withdrawal symptoms occurred concurrently. CYP450 inhibitors: Repeat dose administration of oral voriconazole increased the peak plasma concentration (Cmax) and AUC of (R)-methadone by 31% and 47%, respectively, in subjects receiving a methadone maintenance dose. The Cmax and AUC of (S)-methadone increased by 65% and 103%, respectively Page: 29.0 |
|||
yes | yes (co-administration study) Comment: CYP450 inducers: concomitant administration of rifampin resulted in a marked reduction in serum methadone levels and a concurrent appearance of withdrawal symptoms; phenytoin administration resulted in an approximately 50% reduction in methadone exposure and withdrawal symptoms occurred concurrently. CYP450 inhibitors: Repeat dose administration of oral voriconazole increased the peak plasma concentration (Cmax) and AUC of (R)-methadone by 31% and 47%, respectively, in subjects receiving a methadone maintenance dose. The Cmax and AUC of (S)-methadone increased by 65% and 103%, respectively Page: 29.0 |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
PubMed
Title | Date | PubMed |
---|---|---|
Rhabdomyolysis and acute renal failure following methadone abuse. | 1992 |
|
Cocaine-associated panic attacks in methadone-maintained patients. | 1992 |
|
Desipramine in opioid-dependent cocaine abusers maintained on buprenorphine vs methadone. | 1999 Sep |
|
Reversible spastic paraparesis induced by high-dose intravenous methadone. | 2001 Feb |
|
Bile duct dilation with chronic methadone use in asymptomatic patients: ERCP findings in 6 patients. | 2003 Jul |
|
The impact of methadone induction on cardiac conduction in opiate users. | 2003 Jul 15 |
|
Tiagabine increases cocaine-free urines in cocaine-dependent methadone-treated patients: results of a randomized pilot study. | 2003 Nov |
|
QTc interval prolongation associated with intravenous methadone. | 2003 Oct |
|
QT prolongation and Torsades de Pointes in patients infected with human immunodeficiency virus and treated with methadone. | 2003 Oct 15 |
|
Safety of injectable opioid maintenance treatment for heroin dependence. | 2003 Oct 15 |
|
[Torsade de pointes: a severe and unknown adverse effect in a patient taking methadone]. | 2003 Oct 8 |
|
[Development of transmural myocardial infarction in young persons with intact coronary arteries during methadone use for the treatment of heroine addiction]. | 2004 |
|
Relationship between prescribing and risk of opiate overdose among drug users in and out of maintenance treatment. | 2004 |
|
Cost effectiveness of disulfiram: treating cocaine use in methadone-maintained patients. | 2004 Apr |
|
QT interval prolongation in patients on methadone with concomitant drugs. | 2004 Aug |
|
Methadone metabolism by human placenta. | 2004 Aug 1 |
|
[Life-threatening, recurrent arrhythmia in patients on high-dose methadone treatment: torsade de pointes]. | 2004 Aug 30 |
|
Obsessive-compulsive symptoms precipitated by methadone tapering. | 2004 Dec |
|
Methadone-induced torsade de pointes in a patient with normal baseline QT interval. | 2004 Jul-Aug |
|
Directly observed therapy for the management of HIV-infected patients in a methadone program. | 2004 Jun 1 |
|
The effect of quinidine, used as a probe for the involvement of P-glycoprotein, on the intestinal absorption and pharmacodynamics of methadone. | 2004 May |
|
Agonist-like or antagonist-like treatment for cocaine dependence with methadone for heroin dependence: two double-blind randomized clinical trials. | 2004 May |
|
[Routine ECG in methadone-assisted rehabilitation is wrong prioritization]. | 2004 Nov 18 |
|
Oral methadone for cancer pain: no indication of Q-T interval prolongation or torsades de pointes. | 2004 Oct |
|
Intravenous ketamine infusion as an adjuvant to morphine in a 2-year-old with severe cancer pain from metastatic neuroblastoma. | 2004 Oct |
|
[Preclinical management of accidental methadone intoxication of a 4-year-old girl. Antagonist or intubation?]. | 2004 Oct |
|
[Long QT and torsade de pointes in a patient with acquired human immunodeficiency virus infection in multitherapy with drugs affecting cytochrome P450]. | 2004 Sep |
|
Epidural clonidine, bupivacaine and methadone as the sole analgesic agent after thoracotomy for lung resection. | 2004 Sep |
|
Cocaine-related torsade de pointes in a methadone maintenance patient. | 2005 |
|
Adipocyte-derived hormones in heroin addicts: the influence of methadone maintenance treatment. | 2005 |
|
QTc interval prolongation in patients on long-term methadone maintenance therapy. | 2005 |
|
Effects of buprenorphine on cardiac repolarization in a patient with methadone-related torsade de pointes. | 2005 Apr |
|
Torsades de pointes with methadone. | 2005 Apr |
|
Methadone-related Torsades de Pointes in a sickle cell patient treated for chronic pain. | 2005 Apr |
|
[Methadone-induced heart arrhythmia]. | 2005 Aug 11 |
|
Methadone versus buprenorphine with contingency management or performance feedback for cocaine and opioid dependence. | 2005 Feb |
|
Dextromethorphan-induced delirium and possible methadone interaction. | 2005 Mar |
|
Methadone-induced Torsade de pointes tachycardias. | 2005 May 14 |
|
QT prolongation and torsades de pointes among methadone users: reports to the FDA spontaneous reporting system. | 2005 Nov |
|
[Torsades de pointes during methadone treatment]. | 2005 Oct |
|
Methadone doses of 100 mg or greater are more effective than lower doses at suppressing heroin self-administration in opioid-dependent volunteers. | 2005 Oct |
|
QT prolongation and syncope with methadone, doxepin, and a beta-blocker. | 2005 Oct |
|
Central sleep apnea in stable methadone maintenance treatment patients. | 2005 Sep |
|
Methadone treatment of chronic non-malignant pain and opioid dependence--a long-term follow-up. | 2006 Apr |
|
Variables associated with perceived sleep disorders in methadone maintenance treatment (MMT) patients. | 2006 Apr 28 |
|
Does naltrexone treatment lead to depression? Findings from a randomized controlled trial in subjects with opioid dependence. | 2006 Jan |
|
Bradycardia during methadone therapy in an infant. | 2006 Jan |
|
A randomized controlled trial of interim methadone maintenance. | 2006 Jan |
|
Frequency of high-risk use of QT-prolonging medications. | 2006 Jun |
|
Changes in HIV risk behaviors among patients receiving combined pharmacological and behavioral interventions for heroin and cocaine dependence. | 2006 May |
Sample Use Guides
Chronic pain: oral initial dose - 2.5 mg every 8 to 12 hours; Intravenous initial dose: 2.5 mg to 10 mg every 8 to 12 hours
Opiate withdrawal: Initial dose - 20 to 30 mg orally; an additional 5 to 10 mg may be given orally after 2 to 4 hours if withdrawal symptoms have not been suppressed or if symptoms reappear.
-Maximum initial dose: 30 mg
-Maximum day 1 dose: 40 mg
Route of Administration:
Other
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/11561100
In the presence of 1 uM methadone, the maximum 86Rb+ efflux stimulated by nicotine (Emax) was markedly reduced, but the EC50 for nicotine was altered only slightly, if at all.
Substance Class |
Chemical
Created
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admin
on
Edited
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Record UNII |
UC6VBE7V1Z
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Record Status |
Validated (UNII)
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Record Version |
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Classification Tree | Code System | Code | ||
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WHO-ATC |
N07BC02
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NCI_THESAURUS |
C1506
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NDF-RT |
N0000175684
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WHO-ATC |
N02AC52
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NCI_THESAURUS |
C67413
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DEA NO. |
9250
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LIVERTOX |
NBK548084
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WHO-VATC |
QN07BC02
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CFR |
21 CFR 862.3620
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WHO-ESSENTIAL MEDICINES LIST |
24.5
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WHO-VATC |
QN02AC52
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NDF-RT |
N0000175690
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6813
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Methadone
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METHADONE
Created by
admin on Mon Mar 31 17:45:41 GMT 2025 , Edited by admin on Mon Mar 31 17:45:41 GMT 2025
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297-88-1
Created by
admin on Mon Mar 31 17:45:41 GMT 2025 , Edited by admin on Mon Mar 31 17:45:41 GMT 2025
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SUPERSEDED |
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SALT/SOLVATE -> PARENT |
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SALT/SOLVATE -> PARENT | |||
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METABOLIC ENZYME -> SUBSTRATE |
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METABOLIC ENZYME -> SUBSTRATE |
Involved in the metabolism of
methadone, but its contribution to the metabolism of (R)-methadone was smaller than that of CYP3A4.
For the metabolism of (S)-methadone, the roles of CYP2C8 and CYP3A4 appeared equal.
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METABOLIC ENZYME -> SUBSTRATE |
CYP2C19 preferentially metabolized (R)-methadone,
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METABOLIC ENZYME -> SUBSTRATE |
CYP2B6 preferentially metabolized (S)-methadone,
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PARENT -> SALT/SOLVATE |
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TARGET -> AGONIST |
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BINDER->LIGAND |
BINDING
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METABOLIC ENZYME -> SUBSTRATE |
CYP3A4 showed no preference between the two enantiomers.
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ACTIVE ENANTIOMER->RACEMATE |
approximately 50x the potency of the S-(+)-enantiomer as well as greater ?-opioid receptor selectivity
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SALT/SOLVATE -> PARENT |
APPROXIMATE PURE ANHYDROUS DRUG CONTENT (IN PERCENT)
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TARGET -> AGONIST |
Ki
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SALT/SOLVATE -> PARENT |
APPROXIMATE PURE ANHYDROUS DRUG CONTENT (IN PERCENT)
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TARGET -> AGONIST |
Prolonged exposure methadone induces MOPr internalization comparable with that induced by DAMGO, whereas morphine produces much less MOPr heroin during relapse is due to receptor internalization. The blunting of the response to desensitization not receptor antagonism.
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TRANSPORTER -> SUBSTRATE |
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METABOLITE INACTIVE -> PARENT |
The hierarchy of EDDPgeneration was CYP2B6 > CYP2C19zCYP3A4
MAJOR
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PARENT -> METABOLITE |
MINOR
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METABOLITE -> PARENT |
MINOR
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METABOLITE -> PARENT |
5-10% of the dose but there is a large individual variation due to pH, urine volume, dose and metabolic rate
MINOR
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METABOLITE ACTIVE -> PARENT |
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METABOLITE ACTIVE -> PARENT |
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METABOLITE ACTIVE -> PARENT |
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ACTIVE MOIETY |
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Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Biological Half-life | PHARMACOKINETIC |
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Elimination PHARMACOKINETIC |
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