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 |
|---|---|---|---|---|
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 |
|
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 |
|
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 |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
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 |
|
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 |
|
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 |
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 Health Status: unhealthy Age Group: 23 - 57 years Sex: M+F 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 Health Status: unhealthy Age Group: 23 - 57 years Sex: M+F 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 | |||
Page: 7.0 |
minor | |||
Page: 7.0 |
minor | |||
Page: 7.0 |
minor | |||
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minor | |||
Page: 7.0 |
minor | |||
Page: 7.0 |
minor | |||
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
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53757-34-9
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SUBSTANCE RECORD
