Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C21H29NO.ClH |
| Molecular Weight | 347.922 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.CC[C@H](O)C(C[C@H](C)N(C)C)(C1=CC=CC=C1)C2=CC=CC=C2
InChI
InChIKey=GMNBUMFCZAZBQG-ZHXLSBKVSA-N
InChI=1S/C21H29NO.ClH/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;/h6-15,17,20,23H,5,16H2,1-4H3;1H/t17-,20-;/m0./s1
Approval Year
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
139 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/15380290 |
80 mg 1 times / 2 days steady-state, oral dose: 80 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
DINORACETYLMETHADOL plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
184 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/15380290 |
80 mg 1 times / 2 days steady-state, oral dose: 80 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
NORACYMETHADOL plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
188 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/15380290 |
80 mg 1 times / 2 days steady-state, oral dose: 80 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
LEVOMETHADYL ACETATE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
5892 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/15380290 |
80 mg 1 times / 2 days steady-state, oral dose: 80 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
DINORACETYLMETHADOL plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
6056 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/15380290 |
80 mg 1 times / 2 days steady-state, oral dose: 80 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
NORACYMETHADOL plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
2995 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/15380290 |
80 mg 1 times / 2 days steady-state, oral dose: 80 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
LEVOMETHADYL ACETATE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
Doses
| Dose | Population | Adverse events |
|---|---|---|
3 mg/kg multiple, oral Studied dose Dose: 3 mg/kg Route: oral Route: multiple Dose: 3 mg/kg Sources: |
unhealthy, 23 - 57 years n = 6 Health Status: unhealthy Condition: heroin dependency Age Group: 23 - 57 years Sex: M+F Population Size: 6 Sources: |
Disc. AE: Cardiotoxicity... AEs leading to discontinuation/dose reduction: Cardiotoxicity (6 patients) Sources: |
AEs
| AE | Significance | Dose | Population |
|---|---|---|---|
| Cardiotoxicity | 6 patients Disc. AE |
3 mg/kg multiple, oral Studied dose Dose: 3 mg/kg Route: oral Route: multiple Dose: 3 mg/kg Sources: |
unhealthy, 23 - 57 years n = 6 Health Status: unhealthy Condition: heroin dependency Age Group: 23 - 57 years Sex: M+F Population Size: 6 Sources: |
Overview
| CYP3A4 | CYP2C9 | CYP2D6 | hERG |
|---|---|---|---|
OverviewOther
| Other Inhibitor | Other Substrate | Other Inducer |
|---|---|---|
Drug as victim
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
Page: 7.0 |
minor | |||
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minor | |||
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minor | |||
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minor | |||
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Page: 7.0 |
minor | |||
| yes | likely (co-administration study) Comment: the addition of drugs that induce this enzyme (such as rifampin, phenobarbital, and phenytoin) or inhibit this enzyme (such as ketoconazole, erythromycin, and saquinavir) could increase the levels of parent drug or its active metabolites in a patient that was previously at steady-state, and this could potentially precipitate serious arrhythmias, including torsade de pointes |
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3041255
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DTXSID1048916
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8OCN5S2969
Created by
admin on Sat Dec 16 10:10:15 GMT 2023 , Edited by admin on Sat Dec 16 10:10:15 GMT 2023
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53757-34-9
Created by
admin on Sat Dec 16 10:10:15 GMT 2023 , Edited by admin on Sat Dec 16 10:10:15 GMT 2023
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SUBSTANCE RECORD
