Details
Stereochemistry | ACHIRAL |
Molecular Formula | C15H12N2O2 |
Molecular Weight | 252.268 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
NC(=O)N1C2=C(CC(=O)C3=C1C=CC=C3)C=CC=C2
InChI
InChIKey=CTRLABGOLIVAIY-UHFFFAOYSA-N
InChI=1S/C15H12N2O2/c16-15(19)17-12-7-3-1-5-10(12)9-14(18)11-6-2-4-8-13(11)17/h1-8H,9H2,(H2,16,19)
Molecular Formula | C15H12N2O2 |
Molecular Weight | 252.268 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
DescriptionSources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2009/021014s026,021285s021lbl.pdfhttp://adisinsight.springer.com/drugs/800020351 | https://www.ncbi.nlm.nih.gov/pubmed/28182284 | https://www.ncbi.nlm.nih.gov/pubmed/23861647Curator's Comment: Description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/11394728
Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2009/021014s026,021285s021lbl.pdfhttp://adisinsight.springer.com/drugs/800020351 | https://www.ncbi.nlm.nih.gov/pubmed/28182284 | https://www.ncbi.nlm.nih.gov/pubmed/23861647
Curator's Comment: Description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/11394728
Licarbazepine is the pharmacologically active metabolite of oxcarbazepine, a drug indicated for the treatment of partial seizures and bipolar disorders. Phase III trials of licarbazepine were conducted in the US and Europe, and were initially delayed in November 2006. An isomer of licarbazepine, eslicarbazepine ((S)-(+)-licarbazepine), is an active metabolite of eslicarbazepine acetate.
Originator
Sources: http://cdn.intechopen.com/pdfs-wm/19488.pdfhttp://adisinsight.springer.com/drugs/800020351
Curator's Comment: # Novartis
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL2331043 Sources: https://www.ncbi.nlm.nih.gov/pubmed/8156978 |
50.0 nM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Unknown Approved UseUnknown |
|||
Primary | TRILEPTAL Approved UseOxcarbazepine tablets are indicated for use as monotherapy or adjunctive therapy in the treatment of partial seizures in adults and as monotherapy in the treatment of partial seizures in children aged 4 years and above with epilepsy, and as adjunctive therapy in children aged 2 years and above with partial seizures. Oxcarbazepine tablet is an antiepileptic drug indicated for: Adults: -Monotherapy or adjunctive therapy in the treatment of partial seizures Children: -Monotherapy in the treatment of partial seizures in children 4-16 years -Adjunctive therapy in the treatment of partial seizures in children 2-16 years (1) Launch Date9.4780798E11 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
1.55 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26514967 |
300 mg 2 times / day multiple, oral dose: 300 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
OXCARBAZEPINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
7119 ng/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00850174 |
600 mg single, oral dose: 600 mg route of administration: oral experiment type: single co-administered: |
LICARBAZEPINE plasma | Homo sapiens population: age: sex: food status: Fasted |
|
9349.83 ng/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00849797 |
600 mg single, oral dose: 600 mg route of administration: oral experiment type: single co-administered: |
LICARBAZEPINE plasma | Homo sapiens population: age: sex: food status: Fed |
|
1630.3 ng/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00850174 |
600 mg single, oral dose: 600 mg route of administration: oral experiment type: single co-administered: |
OXCARBAZEPINE plasma | Homo sapiens population: age: sex: food status: Fasted |
|
3537.63 ng/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00849797 |
600 mg single, oral dose: 600 mg route of administration: oral experiment type: single co-administered: |
OXCARBAZEPINE plasma | Homo sapiens population: age: sex: food status: Fed |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
3.76 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26514967 |
300 mg 2 times / day multiple, oral dose: 300 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
OXCARBAZEPINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
157372 ng*h/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00850174 |
600 mg single, oral dose: 600 mg route of administration: oral experiment type: single co-administered: |
LICARBAZEPINE plasma | Homo sapiens population: age: sex: food status: Fasted |
|
179002.4 ng*h/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00849797 |
600 mg single, oral dose: 600 mg route of administration: oral experiment type: single co-administered: |
LICARBAZEPINE plasma | Homo sapiens population: age: sex: food status: Fed |
|
173770 ng*h/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00850174 |
600 mg single, oral dose: 600 mg route of administration: oral experiment type: single co-administered: |
LICARBAZEPINE plasma | Homo sapiens population: age: sex: food status: Fasted |
|
197864.34 ng*h/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00849797 |
600 mg single, oral dose: 600 mg route of administration: oral experiment type: single co-administered: |
LICARBAZEPINE plasma | Homo sapiens population: age: sex: food status: Fed |
|
5309.5 ng*h/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00850174 |
600 mg single, oral dose: 600 mg route of administration: oral experiment type: single co-administered: |
OXCARBAZEPINE plasma | Homo sapiens population: age: sex: food status: Fasted |
|
9445.55 ng*h/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00849797 |
600 mg single, oral dose: 600 mg route of administration: oral experiment type: single co-administered: |
OXCARBAZEPINE plasma | Homo sapiens population: age: sex: food status: Fed |
|
5873.1 ng*h/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00850174 |
600 mg single, oral dose: 600 mg route of administration: oral experiment type: single co-administered: |
OXCARBAZEPINE plasma | Homo sapiens population: age: sex: food status: Fasted |
|
9679.79 ng*h/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00849797 |
600 mg single, oral dose: 600 mg route of administration: oral experiment type: single co-administered: |
OXCARBAZEPINE plasma | Homo sapiens population: age: sex: food status: Fed |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
2.38 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26514967 |
300 mg 2 times / day multiple, oral dose: 300 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
OXCARBAZEPINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
27% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26514967 |
300 mg 2 times / day multiple, oral dose: 300 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
OXCARBAZEPINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
Doses
Dose | Population | Adverse events |
---|---|---|
8 mg/kg 1 times / day steady, oral (starting) Recommended Dose: 8 mg/kg, 1 times / day Route: oral Route: steady Dose: 8 mg/kg, 1 times / day Sources: |
unhealthy, 1 month -4 years n = 241 Health Status: unhealthy Condition: partial seizures Age Group: 1 month -4 years Population Size: 241 Sources: |
Disc. AE: Convulsions, Status epilepticus... AEs leading to discontinuation/dose reduction: Convulsions (3.7%) Sources: Status epilepticus (1.2%) Ataxia (1.2%) |
15 g single, oral Overdose |
unhealthy, 13 years n = 1 Health Status: unhealthy Age Group: 13 years Sex: M Population Size: 1 Sources: |
Other AEs: Vomiting... |
2700 mg 1 times / day multiple, oral Highest studied dose Dose: 2700 mg, 1 times / day Route: oral Route: multiple Dose: 2700 mg, 1 times / day Sources: |
unhealthy, 19-70 years n = 71 Health Status: unhealthy Age Group: 19-70 years Sex: M+F Population Size: 71 Sources: |
Other AEs: Dizziness, Tremor... |
30600 mg single, oral Overdose Dose: 30600 mg Route: oral Route: single Dose: 30600 mg Sources: |
unhealthy, 36 years n = 1 Health Status: unhealthy Age Group: 36 years Sex: M Population Size: 1 Sources: |
|
8 mg/kg 1 times / day steady, oral (starting) Recommended Dose: 8 mg/kg, 1 times / day Route: oral Route: steady Dose: 8 mg/kg, 1 times / day Sources: |
unhealthy, 4-16 years n = 456 Health Status: unhealthy Condition: partial seizures Age Group: 4-16 years Population Size: 456 Sources: |
Disc. AE: Somnolence, Vomiting... AEs leading to discontinuation/dose reduction: Somnolence (2.4%) Sources: Vomiting (2%) Ataxia (1.8%) Diplopia (1.3%) Dizziness (1.3%) Fatigue (1.1%) Nystagmus (1.1%) |
12 mg/kg 1 times / day steady, oral (starting) Dose: 12 mg/kg, 1 times / day Route: oral Route: steady Dose: 12 mg/kg, 1 times / day Sources: |
unhealthy, 6 years n = 1 Health Status: unhealthy Condition: f benign rolandic epilepsy Age Group: 6 years Sex: M Population Size: 1 Sources: |
Disc. AE: Stevens Johnson syndrome... AEs leading to discontinuation/dose reduction: Stevens Johnson syndrome (1 patient) Sources: |
300 mg 2 times / day steady, oral (starting) Recommended Dose: 300 mg, 2 times / day Route: oral Route: steady Dose: 300 mg, 2 times / day Sources: |
unhealthy, adult n = 1524 Health Status: unhealthy Condition: epilepsy Age Group: adult Population Size: 1524 Sources: |
Disc. AE: Hyponatremia... AEs leading to discontinuation/dose reduction: Hyponatremia (2.5%) Sources: |
300 mg 2 times / day steady, oral (starting) Recommended Dose: 300 mg, 2 times / day Route: oral Route: steady Dose: 300 mg, 2 times / day Sources: |
unhealthy, adult n = 1537 Health Status: unhealthy Condition: partial seizures Age Group: adult Population Size: 1537 Sources: |
Disc. AE: Dizziness, Diplopia... AEs leading to discontinuation/dose reduction: Dizziness (6.4%) Sources: Diplopia (5.9%) Ataxia (5.2%) Vomiting (5.1%) Nausea (4.9%) Somnolence (3.8%) Headache (2.9%) Fatigue (2.1%) Abnormal vision (2.1%) Tremor (1.8%) Abnormal gait (1.7%) Rash (1.4%) Hyponatremia (1%) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Ataxia | 1.2% Disc. AE |
8 mg/kg 1 times / day steady, oral (starting) Recommended Dose: 8 mg/kg, 1 times / day Route: oral Route: steady Dose: 8 mg/kg, 1 times / day Sources: |
unhealthy, 1 month -4 years n = 241 Health Status: unhealthy Condition: partial seizures Age Group: 1 month -4 years Population Size: 241 Sources: |
Status epilepticus | 1.2% Disc. AE |
8 mg/kg 1 times / day steady, oral (starting) Recommended Dose: 8 mg/kg, 1 times / day Route: oral Route: steady Dose: 8 mg/kg, 1 times / day Sources: |
unhealthy, 1 month -4 years n = 241 Health Status: unhealthy Condition: partial seizures Age Group: 1 month -4 years Population Size: 241 Sources: |
Convulsions | 3.7% Disc. AE |
8 mg/kg 1 times / day steady, oral (starting) Recommended Dose: 8 mg/kg, 1 times / day Route: oral Route: steady Dose: 8 mg/kg, 1 times / day Sources: |
unhealthy, 1 month -4 years n = 241 Health Status: unhealthy Condition: partial seizures Age Group: 1 month -4 years Population Size: 241 Sources: |
Vomiting | 1 patient | 15 g single, oral Overdose |
unhealthy, 13 years n = 1 Health Status: unhealthy Age Group: 13 years Sex: M Population Size: 1 Sources: |
Dizziness | 2700 mg 1 times / day multiple, oral Highest studied dose Dose: 2700 mg, 1 times / day Route: oral Route: multiple Dose: 2700 mg, 1 times / day Sources: |
unhealthy, 19-70 years n = 71 Health Status: unhealthy Age Group: 19-70 years Sex: M+F Population Size: 71 Sources: |
|
Headache | 2700 mg 1 times / day multiple, oral Highest studied dose Dose: 2700 mg, 1 times / day Route: oral Route: multiple Dose: 2700 mg, 1 times / day Sources: |
unhealthy, 19-70 years n = 71 Health Status: unhealthy Age Group: 19-70 years Sex: M+F Population Size: 71 Sources: |
|
Somnolence | 2700 mg 1 times / day multiple, oral Highest studied dose Dose: 2700 mg, 1 times / day Route: oral Route: multiple Dose: 2700 mg, 1 times / day Sources: |
unhealthy, 19-70 years n = 71 Health Status: unhealthy Age Group: 19-70 years Sex: M+F Population Size: 71 Sources: |
|
Tremor | 2700 mg 1 times / day multiple, oral Highest studied dose Dose: 2700 mg, 1 times / day Route: oral Route: multiple Dose: 2700 mg, 1 times / day Sources: |
unhealthy, 19-70 years n = 71 Health Status: unhealthy Age Group: 19-70 years Sex: M+F Population Size: 71 Sources: |
|
Fatigue | 1.1% Disc. AE |
8 mg/kg 1 times / day steady, oral (starting) Recommended Dose: 8 mg/kg, 1 times / day Route: oral Route: steady Dose: 8 mg/kg, 1 times / day Sources: |
unhealthy, 4-16 years n = 456 Health Status: unhealthy Condition: partial seizures Age Group: 4-16 years Population Size: 456 Sources: |
Nystagmus | 1.1% Disc. AE |
8 mg/kg 1 times / day steady, oral (starting) Recommended Dose: 8 mg/kg, 1 times / day Route: oral Route: steady Dose: 8 mg/kg, 1 times / day Sources: |
unhealthy, 4-16 years n = 456 Health Status: unhealthy Condition: partial seizures Age Group: 4-16 years Population Size: 456 Sources: |
Diplopia | 1.3% Disc. AE |
8 mg/kg 1 times / day steady, oral (starting) Recommended Dose: 8 mg/kg, 1 times / day Route: oral Route: steady Dose: 8 mg/kg, 1 times / day Sources: |
unhealthy, 4-16 years n = 456 Health Status: unhealthy Condition: partial seizures Age Group: 4-16 years Population Size: 456 Sources: |
Dizziness | 1.3% Disc. AE |
8 mg/kg 1 times / day steady, oral (starting) Recommended Dose: 8 mg/kg, 1 times / day Route: oral Route: steady Dose: 8 mg/kg, 1 times / day Sources: |
unhealthy, 4-16 years n = 456 Health Status: unhealthy Condition: partial seizures Age Group: 4-16 years Population Size: 456 Sources: |
Ataxia | 1.8% Disc. AE |
8 mg/kg 1 times / day steady, oral (starting) Recommended Dose: 8 mg/kg, 1 times / day Route: oral Route: steady Dose: 8 mg/kg, 1 times / day Sources: |
unhealthy, 4-16 years n = 456 Health Status: unhealthy Condition: partial seizures Age Group: 4-16 years Population Size: 456 Sources: |
Vomiting | 2% Disc. AE |
8 mg/kg 1 times / day steady, oral (starting) Recommended Dose: 8 mg/kg, 1 times / day Route: oral Route: steady Dose: 8 mg/kg, 1 times / day Sources: |
unhealthy, 4-16 years n = 456 Health Status: unhealthy Condition: partial seizures Age Group: 4-16 years Population Size: 456 Sources: |
Somnolence | 2.4% Disc. AE |
8 mg/kg 1 times / day steady, oral (starting) Recommended Dose: 8 mg/kg, 1 times / day Route: oral Route: steady Dose: 8 mg/kg, 1 times / day Sources: |
unhealthy, 4-16 years n = 456 Health Status: unhealthy Condition: partial seizures Age Group: 4-16 years Population Size: 456 Sources: |
Stevens Johnson syndrome | 1 patient Disc. AE |
12 mg/kg 1 times / day steady, oral (starting) Dose: 12 mg/kg, 1 times / day Route: oral Route: steady Dose: 12 mg/kg, 1 times / day Sources: |
unhealthy, 6 years n = 1 Health Status: unhealthy Condition: f benign rolandic epilepsy Age Group: 6 years Sex: M Population Size: 1 Sources: |
Hyponatremia | 2.5% Disc. AE |
300 mg 2 times / day steady, oral (starting) Recommended Dose: 300 mg, 2 times / day Route: oral Route: steady Dose: 300 mg, 2 times / day Sources: |
unhealthy, adult n = 1524 Health Status: unhealthy Condition: epilepsy Age Group: adult Population Size: 1524 Sources: |
Hyponatremia | 1% Disc. AE |
300 mg 2 times / day steady, oral (starting) Recommended Dose: 300 mg, 2 times / day Route: oral Route: steady Dose: 300 mg, 2 times / day Sources: |
unhealthy, adult n = 1537 Health Status: unhealthy Condition: partial seizures Age Group: adult Population Size: 1537 Sources: |
Rash | 1.4% Disc. AE |
300 mg 2 times / day steady, oral (starting) Recommended Dose: 300 mg, 2 times / day Route: oral Route: steady Dose: 300 mg, 2 times / day Sources: |
unhealthy, adult n = 1537 Health Status: unhealthy Condition: partial seizures Age Group: adult Population Size: 1537 Sources: |
Abnormal gait | 1.7% Disc. AE |
300 mg 2 times / day steady, oral (starting) Recommended Dose: 300 mg, 2 times / day Route: oral Route: steady Dose: 300 mg, 2 times / day Sources: |
unhealthy, adult n = 1537 Health Status: unhealthy Condition: partial seizures Age Group: adult Population Size: 1537 Sources: |
Tremor | 1.8% Disc. AE |
300 mg 2 times / day steady, oral (starting) Recommended Dose: 300 mg, 2 times / day Route: oral Route: steady Dose: 300 mg, 2 times / day Sources: |
unhealthy, adult n = 1537 Health Status: unhealthy Condition: partial seizures Age Group: adult Population Size: 1537 Sources: |
Abnormal vision | 2.1% Disc. AE |
300 mg 2 times / day steady, oral (starting) Recommended Dose: 300 mg, 2 times / day Route: oral Route: steady Dose: 300 mg, 2 times / day Sources: |
unhealthy, adult n = 1537 Health Status: unhealthy Condition: partial seizures Age Group: adult Population Size: 1537 Sources: |
Fatigue | 2.1% Disc. AE |
300 mg 2 times / day steady, oral (starting) Recommended Dose: 300 mg, 2 times / day Route: oral Route: steady Dose: 300 mg, 2 times / day Sources: |
unhealthy, adult n = 1537 Health Status: unhealthy Condition: partial seizures Age Group: adult Population Size: 1537 Sources: |
Headache | 2.9% Disc. AE |
300 mg 2 times / day steady, oral (starting) Recommended Dose: 300 mg, 2 times / day Route: oral Route: steady Dose: 300 mg, 2 times / day Sources: |
unhealthy, adult n = 1537 Health Status: unhealthy Condition: partial seizures Age Group: adult Population Size: 1537 Sources: |
Somnolence | 3.8% Disc. AE |
300 mg 2 times / day steady, oral (starting) Recommended Dose: 300 mg, 2 times / day Route: oral Route: steady Dose: 300 mg, 2 times / day Sources: |
unhealthy, adult n = 1537 Health Status: unhealthy Condition: partial seizures Age Group: adult Population Size: 1537 Sources: |
Nausea | 4.9% Disc. AE |
300 mg 2 times / day steady, oral (starting) Recommended Dose: 300 mg, 2 times / day Route: oral Route: steady Dose: 300 mg, 2 times / day Sources: |
unhealthy, adult n = 1537 Health Status: unhealthy Condition: partial seizures Age Group: adult Population Size: 1537 Sources: |
Vomiting | 5.1% Disc. AE |
300 mg 2 times / day steady, oral (starting) Recommended Dose: 300 mg, 2 times / day Route: oral Route: steady Dose: 300 mg, 2 times / day Sources: |
unhealthy, adult n = 1537 Health Status: unhealthy Condition: partial seizures Age Group: adult Population Size: 1537 Sources: |
Ataxia | 5.2% Disc. AE |
300 mg 2 times / day steady, oral (starting) Recommended Dose: 300 mg, 2 times / day Route: oral Route: steady Dose: 300 mg, 2 times / day Sources: |
unhealthy, adult n = 1537 Health Status: unhealthy Condition: partial seizures Age Group: adult Population Size: 1537 Sources: |
Diplopia | 5.9% Disc. AE |
300 mg 2 times / day steady, oral (starting) Recommended Dose: 300 mg, 2 times / day Route: oral Route: steady Dose: 300 mg, 2 times / day Sources: |
unhealthy, adult n = 1537 Health Status: unhealthy Condition: partial seizures Age Group: adult Population Size: 1537 Sources: |
Dizziness | 6.4% Disc. AE |
300 mg 2 times / day steady, oral (starting) Recommended Dose: 300 mg, 2 times / day Route: oral Route: steady Dose: 300 mg, 2 times / day Sources: |
unhealthy, adult n = 1537 Health Status: unhealthy Condition: partial seizures Age Group: adult Population Size: 1537 Sources: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
inconclusive [Activation 39.8107 uM] | ||||
likely | ||||
no [IC50 >133 uM] | ||||
no [IC50 >133 uM] | ||||
no [IC50 >133 uM] | ||||
no [IC50 >133 uM] | ||||
Page: (Pharm) 18-19, (PMDA_I100) 154 |
no [Ki 1150 uM] | |||
Page: (Pharm) 18-19, (PMDA_I100) 155 |
no [Ki >1350 uM] | |||
Page: (Pharm) 18-19, (PMDA_I100) 154 |
no [Ki >1350 uM] | |||
Page: (Pharm) 18-19, (PMDA_I100) 155 |
no [Ki >1350 uM] | |||
Page: (Pharm) 18-19, (PMDA_I100) 154 |
no [Ki >1350 uM] | |||
Page: (Pharm) 18-19, (PMDA_I100) 155 |
no [Ki >1350 uM] | |||
Page: (Pharm) 18-19, (PMDA_I100) 154 |
no [Ki >1350 uM] | |||
Page: (Pharm) 18-19, (PMDA_I100) 155 |
no [Ki >1350 uM] | |||
Page: (Pharm) 18-19, (PMDA_I100) 154 |
no [Ki >1800 uM] | |||
Page: (Pharm) 18-19, (PMDA_I100) 155 |
no [Ki >1800 uM] | |||
Page: (Pharm) 18-19, (PMDA_I100) 154 |
no [Ki >900 uM] | |||
Page: (Pharm) 18-19, (PMDA_I100) 155 |
no [Ki >900 uM] | |||
Page: (Pharm) 18-19, (PMDA_I100) 154 |
weak [Ki 270 uM] | |||
Page: (Pharm) 18-19, (PMDA_I100) 155 |
weak [Ki 647 uM] | |||
weak | ||||
Page: (Pharm) 18-19, (PMDA_I100) 154 |
yes [Ki 228 uM] | |||
Page: (Pharm) 18-19, (PMDA_I100) 155 |
yes [Ki 88 uM] | |||
Page: (Label) 18 |
yes | |||
yes | ||||
yes | ||||
yes | yes (co-administration study) Comment: Coadministration of OXCARBAZEPINE decreased the AUC for Felodipine and Ethinylestradiol (both CYP3A4 substrate) Page: (Pharm) 19, (Label) 18 |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
major | ||||
major | ||||
minor | ||||
yes [Km 24.3 uM] | ||||
yes [Km 2583 uM] | ||||
yes [Km 59 uM] | ||||
yes [Km 90 uM] | ||||
yes | yes (co-administration study) Comment: Co-administration of verapamil (P-gp inhibitor) resulted in a modest increase of the apparent bioavailability of oxcarbazepine by 12% (10-28), but did not affect parent or metabolite clearances. |
PubMed
Title | Date | PubMed |
---|---|---|
[New antiepileptic drugs in childhood epilepsies: indications and limits]. | 2001 |
|
Effect of oxcarbazepine on kainic acid-induced seizure. | 2001 |
|
Is it Crohn's disease? A severe systemic granulomatous reaction to sulfasalazine in patient with rheumatoid arthritis. | 2001 |
|
Concerns with antiepileptic drug initiation: safety, tolerability, and efficacy. | 2001 |
|
Oxcarbazepine in the treatment of epilepsy. | 2001 Aug |
|
Clinical pharmacology and therapeutic use of the new antiepileptic drugs. | 2001 Dec |
|
Oxcarbazepine: new preparation. An alternative to carbamazepine in partial epilepsy. | 2001 Dec |
|
[Ad hoc change from carbamazepine to oxcarbazepine--effectiveness and tolerance. A retrospective analysis]. | 2001 Dec |
|
Symptomatic trigeminal-autonomic cephalalgia evolving to trigeminal neuralgia: report of a case associated with dual pathology. | 2001 Nov |
|
Transplacental passage of oxcarbazepine and its metabolites in vivo. | 2001 Nov |
|
Oxcarbazepine in affective and schizoaffective disorders. | 2001 Nov |
|
Change in oxcarbazepine (Trileptal) formulation is associated with more side effects and higher blood concentrations. | 2001 Nov |
|
Review of treatment options for refractory epilepsy: new medications and vagal nerve stimulation. | 2001 Nov |
|
Anticonvulsants in the treatment of mood disorders: assessing current and future roles. | 2001 Oct |
|
[Oxcarbazepine]. | 2001 Oct |
|
Infantile spasms: diagnosis and assessment of treatment response by video-EEG. | 2001 Oct |
|
Plasma concentration of topiramate correlates with cerebrospinal fluid concentration. | 2001 Oct |
|
What's new: newly approved drugs for children. | 2001 Oct |
|
Open pilot study on oxcarbazepine for the treatment of notalgia paresthetica. | 2001 Oct |
|
Development of a high throughput 96-well plate sample preparation method for the determination of trileptal (oxcarbazepine) and its metabolites in human plasma. | 2001 Oct 5 |
|
Treatment of epilepsy in women of reproductive age: pharmacokinetic considerations. | 2002 |
|
What do you do when they grow up? Approaches to seizures in developmentally delayed adults. | 2002 |
|
Clinical pharmacodynamics and pharmacokinetics of antimanic and mood-stabilizing medications. | 2002 |
|
Effect of antiepileptic drugs on cognitive function in individuals with epilepsy: a comparative review of newer versus older agents. | 2002 |
|
Anticonvulsants: aspects of their mechanisms of action. | 2002 |
|
Oxcarbazepine and hepatic porphyria. | 2002 Apr |
|
The novel anticonvulsant BIA 2-093 inhibits transmitter release during opening of voltage-gated sodium channels: a comparison with carbamazepine and oxcarbazepine. | 2002 Apr |
|
Women with PTSD: the psychodynamic aspects of psychopharmacologic and "hands-on" psychiatric management. | 2002 Fall |
|
Metabolism of 10,11-dihydro-10-hydroxyimino-5H-dibenz/b, f/azepine-5-carboxamide, a potent anti-epileptic drug. | 2002 Feb |
|
Long-term cohort study comparing medical (oxcarbazepine) and surgical management of intractable trigeminal neuralgia. | 2002 Feb |
|
Simultaneous determination of four antiepileptic drugs in serum by high-performance liquid chromatography. | 2002 Feb |
|
New antiepileptic drugs: review on drug interactions. | 2002 Feb |
|
Marketed new antiepileptic drugs: are they better than old-generation agents? | 2002 Feb |
|
Pediatric partial and generalized seizures. | 2002 Jan |
|
Oxcarbazepine. | 2002 Jan |
|
Oxcarbazepine. | 2002 Jan |
|
Pharmacotherapy of trigeminal neuralgia. | 2002 Jan-Feb |
|
Validated assay for quantification of oxcarbazepine and its active dihydro metabolite 10-hydroxycarbazepine in plasma by atmospheric pressure chemical ionization liquid chromatography/mass spectrometry. | 2002 Jul |
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Gateways to clinical trials. | 2002 Jul-Aug |
|
Oxcarbazepine for epilepsy--a useful new choice? | 2002 Jun |
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Serum concentrations of topiramate in patients with epilepsy: influence of dose, age, and comedication. | 2002 Jun |
|
Some common issues in the use of antiepileptic drugs. | 2002 Mar |
|
Oxcarbazepine and hyponatremia. | 2002 Mar 1 |
|
Effects of oxcarbazepine on sodium concentration and water handling. | 2002 May |
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LC determination of oxcarbazepine and its active metabolite in human serum. | 2002 May 15 |
|
Oxcarbazepine for mood disorders. | 2002 Oct |
|
[Monitoring serum levels of new antiepileptics]. | 2002 Sep |
|
[Characteristics and indications of oxcarbazepine]. | 2002 Sep |
|
Progress report on new antiepileptic drugs: a summary of the Sixth Eilat Conference (EILAT VI). | 2002 Sep |
|
Pharmacokinetics of mood stabilizers and new anticonvulsants. | 2002 Winter |
Sample Use Guides
In adults treatment with Trileptal (oxcarbazepine) should be initiated with a dose of 600 mg/day, given in a BID regimen. If clinically indicated, the dose may be increased by a maximum of 600 mg/day at approximately weekly intervals; the recommended daily dose is 1200 mg/day. In pediatric patients aged 4-16 years, treatment should be initiated at a daily dose of 8-10 mg/kg generally not to exceed 600 mg/day, given in a BID regimen.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/19575845
30 uM oxcarbazepine exerts neuroprotective effect toward oxygen and glucose deprivation in cultured rat hippocampal neurons
Substance Class |
Chemical
Created
by
admin
on
Edited
Wed Jul 05 22:38:08 UTC 2023
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Wed Jul 05 22:38:08 UTC 2023
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Record UNII |
VZI5B1W380
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NCI_THESAURUS |
C264
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LIVERTOX |
NBK548414
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NDF-RT |
N0000008486
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N0000175753
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QN03AF02
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WHO-ATC |
N03AF02
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DB00776
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28721-07-5
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SUB32960
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4585
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OXCARBAZEPINE
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SUB09510MIG
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Oxcarbazepine
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249-188-8
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VZI5B1W380
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C036006
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2017
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32624
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758693
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100000092224
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M8298
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DTXSID0045703
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CHEMBL1068
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C47643
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Related Record | Type | Details | ||
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BASIS OF STRENGTH->SUBSTANCE |
ASSAY (HPLC)
USP
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METABOLIC ENZYME -> INHIBITOR |
Ki
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METABOLIC ENZYME -> INDUCER |
CHROMATOGRAPHIC PURITY (HPLC/UV)
Ki
|
||
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EXCRETED UNCHANGED |
AMOUNT EXCRETED
URINE
|
||
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BINDER->LIGAND |
BINDING
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||
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BASIS OF STRENGTH->SUBSTANCE |
ASSAY (HPLC)
EP
|
||
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METABOLIC ENZYME -> INDUCER |
Ki
|
Related Record | Type | Details | ||
---|---|---|---|---|
|
METABOLITE -> PARENT |
|
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METABOLITE -> PARENT |
|
||
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METABOLITE ACTIVE -> PRODRUG |
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METABOLITE -> PARENT |
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METABOLITE -> PARENT |
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METABOLITE -> PARENT |
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METABOLITE -> PARENT |
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METABOLITE -> PARENT |
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Related Record | Type | Details | ||
---|---|---|---|---|
|
IMPURITY -> PARENT |
UNSPECIFIED
EP
|
||
|
IMPURITY -> PARENT |
UNSPECIFIED
EP
|
||
|
IMPURITY -> PARENT |
sum of impurities K and L: maximum 0.1 per cent
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
|
||
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IMPURITY -> PARENT |
UNSPECIFIED
EP
|
||
|
IMPURITY -> PARENT |
|
||
|
IMPURITY -> PARENT |
sum of impurities K and L: maximum 0.1 per cent
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
|
||
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IMPURITY -> PARENT |
UNSPECIFIED
EP
|
||
|
IMPURITY -> PARENT |
UNSPECIFIED
EP
|
||
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IMPURITY -> PARENT |
UNSPECIFIED
EP
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||
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IMPURITY -> PARENT |
UNSPECIFIED
EP
|
||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
|
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IMPURITY -> PARENT |
UNSPECIFIED
EP
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||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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Related Record | Type | Details | ||
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ACTIVE MOIETY |
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Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Tmax | PHARMACOKINETIC |
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FASTED CONDITION |
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Volume of Distribution | PHARMACOKINETIC |
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MHD PHARMACOKINETIC |
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Biological Half-life | PHARMACOKINETIC |
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MHD PHARMACOKINETIC PHARMACOKINETIC PHARMACOKINETIC PHARMACOKINETIC PHARMACOKINETIC |
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