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=CC=CC=C2CC(=O)C3=CC=CC=C13
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://adisinsight.springer.com/drugs/800020351 | https://www.ncbi.nlm.nih.gov/pubmed/28182284 | https://www.ncbi.nlm.nih.gov/pubmed/23861647http://www.accessdata.fda.gov/drugsatfda_docs/label/2009/021014s026,021285s021lbl.pdfCurator's Comment: Description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/11394728
Sources: http://adisinsight.springer.com/drugs/800020351 | https://www.ncbi.nlm.nih.gov/pubmed/28182284 | https://www.ncbi.nlm.nih.gov/pubmed/23861647http://www.accessdata.fda.gov/drugsatfda_docs/label/2009/021014s026,021285s021lbl.pdf
Curator's Comment: Description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/11394728
Oxcarbazepine and its active metabolite (10,11-dihydro-10-hydroxy-carbazepine, MHD) have been effective in animal models of epilepsy that generally predict efficacy in generalized tonic-clonic seizures and partial seizures in humans. The pharmacokinetic profile of oxcarbazepine is less complicated than that of carbamazepine, with less metabolism by the cytochrome P450 system, no production of an epoxide metabolite, and lower plasma protein binding. The clinical efficacy and tolerability of oxcarbazepine have been demonstrated in trials in adults, children, and the elderly. The pharmacological activity of oxcarbazepine is primarily exerted through the 10-monohydroxy metabolite (MHD) of oxcarbazepine. The precise mechanism by which oxcarbazepine and MHD exert their antiseizure effect is unknown; however, in vitro electrophysiological studies indicate that they produce blockade of voltage-sensitive sodium channels, resulting in stabilization of hyperexcited neural membranes, inhibition of repetitive neuronal firing, and diminution of propagation of
synaptic impulses. These actions are thought to be important in the prevention of seizure
spread in the intact brain. In addition, increased potassium conductance and modulation of high-voltage activated calcium channels may contribute to the anticonvulsant effects of the drug.
Originator
Sources: http://adisinsight.springer.com/drugs/800020351http://cdn.intechopen.com/pdfs-wm/19488.pdf
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 Date2000 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
30.7 μM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/18258749/ |
500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered: |
LICARBAZEPINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
77.6 μM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/18258749/ |
500 mg 3 times / day steady-state, oral dose: 500 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
LICARBAZEPINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE 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 |
|
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 |
|
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 |
|
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 |
|
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 |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
503 μM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/18258749/ |
500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered: |
LICARBAZEPINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
747 μM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/18258749/ |
500 mg 3 times / day steady-state, oral dose: 500 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
LICARBAZEPINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE 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 |
|
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 |
|
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 |
|
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 |
|
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 |
|
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 |
|
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 |
|
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 |
|
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 |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
9.3 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/18258749/ |
500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered: |
LICARBAZEPINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
11.3 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/18258749/ |
500 mg 3 times / day steady-state, oral dose: 500 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
LICARBAZEPINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
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 |
---|---|---|---|---|
70% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/20578208/ |
LICARBAZEPINE plasma | Homo sapiens population: HEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
||
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 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 Health Status: unhealthy Age Group: 1 month -4 years 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 |
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 Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Other AEs: Dizziness, Tremor... |
30600 mg single, oral Overdose Dose: 30600 mg Route: oral Route: single Dose: 30600 mg Sources: |
unhealthy, 36 years |
|
8 mg/kg 1 times / day steady, oral Recommended Dose: 8 mg/kg, 1 times / day Route: oral Route: steady Dose: 8 mg/kg, 1 times / day Sources: |
unhealthy, 4-16 years Health Status: unhealthy Age Group: 4-16 years 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 Dose: 12 mg/kg, 1 times / day Route: oral Route: steady Dose: 12 mg/kg, 1 times / day Sources: |
unhealthy, 6 years |
Disc. AE: Stevens Johnson syndrome... AEs leading to discontinuation/dose reduction: Stevens Johnson syndrome (1 patient) Sources: |
300 mg 2 times / day steady, oral Recommended Dose: 300 mg, 2 times / day Route: oral Route: steady Dose: 300 mg, 2 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
Disc. AE: Hyponatremia... AEs leading to discontinuation/dose reduction: Hyponatremia (2.5%) Sources: |
300 mg 2 times / day steady, oral Recommended Dose: 300 mg, 2 times / day Route: oral Route: steady Dose: 300 mg, 2 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult 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%) |
500 mg 2 times / day multiple, oral Studied dose Dose: 500 mg, 2 times / day Route: oral Route: multiple Dose: 500 mg, 2 times / day Sources: |
healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M Food Status: UNKNOWN Sources: |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Ataxia | 1.2% Disc. AE |
8 mg/kg 1 times / day steady, oral 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 Health Status: unhealthy Age Group: 1 month -4 years Sources: |
Status epilepticus | 1.2% Disc. AE |
8 mg/kg 1 times / day steady, oral 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 Health Status: unhealthy Age Group: 1 month -4 years Sources: |
Convulsions | 3.7% Disc. AE |
8 mg/kg 1 times / day steady, oral 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 Health Status: unhealthy Age Group: 1 month -4 years Sources: |
Vomiting | 1 patient | 15 g single, oral Overdose |
unhealthy, 13 years |
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 Health Status: unhealthy Age Group: 19-70 years Sex: M+F 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 Health Status: unhealthy Age Group: 19-70 years Sex: M+F 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 Health Status: unhealthy Age Group: 19-70 years Sex: M+F 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 Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
|
Fatigue | 1.1% Disc. AE |
8 mg/kg 1 times / day steady, oral Recommended Dose: 8 mg/kg, 1 times / day Route: oral Route: steady Dose: 8 mg/kg, 1 times / day Sources: |
unhealthy, 4-16 years Health Status: unhealthy Age Group: 4-16 years Sources: |
Nystagmus | 1.1% Disc. AE |
8 mg/kg 1 times / day steady, oral Recommended Dose: 8 mg/kg, 1 times / day Route: oral Route: steady Dose: 8 mg/kg, 1 times / day Sources: |
unhealthy, 4-16 years Health Status: unhealthy Age Group: 4-16 years Sources: |
Diplopia | 1.3% Disc. AE |
8 mg/kg 1 times / day steady, oral Recommended Dose: 8 mg/kg, 1 times / day Route: oral Route: steady Dose: 8 mg/kg, 1 times / day Sources: |
unhealthy, 4-16 years Health Status: unhealthy Age Group: 4-16 years Sources: |
Dizziness | 1.3% Disc. AE |
8 mg/kg 1 times / day steady, oral Recommended Dose: 8 mg/kg, 1 times / day Route: oral Route: steady Dose: 8 mg/kg, 1 times / day Sources: |
unhealthy, 4-16 years Health Status: unhealthy Age Group: 4-16 years Sources: |
Ataxia | 1.8% Disc. AE |
8 mg/kg 1 times / day steady, oral Recommended Dose: 8 mg/kg, 1 times / day Route: oral Route: steady Dose: 8 mg/kg, 1 times / day Sources: |
unhealthy, 4-16 years Health Status: unhealthy Age Group: 4-16 years Sources: |
Vomiting | 2% Disc. AE |
8 mg/kg 1 times / day steady, oral Recommended Dose: 8 mg/kg, 1 times / day Route: oral Route: steady Dose: 8 mg/kg, 1 times / day Sources: |
unhealthy, 4-16 years Health Status: unhealthy Age Group: 4-16 years Sources: |
Somnolence | 2.4% Disc. AE |
8 mg/kg 1 times / day steady, oral Recommended Dose: 8 mg/kg, 1 times / day Route: oral Route: steady Dose: 8 mg/kg, 1 times / day Sources: |
unhealthy, 4-16 years Health Status: unhealthy Age Group: 4-16 years Sources: |
Stevens Johnson syndrome | 1 patient Disc. AE |
12 mg/kg 1 times / day steady, oral Dose: 12 mg/kg, 1 times / day Route: oral Route: steady Dose: 12 mg/kg, 1 times / day Sources: |
unhealthy, 6 years |
Hyponatremia | 2.5% Disc. AE |
300 mg 2 times / day steady, oral Recommended Dose: 300 mg, 2 times / day Route: oral Route: steady Dose: 300 mg, 2 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
Hyponatremia | 1% Disc. AE |
300 mg 2 times / day steady, oral Recommended Dose: 300 mg, 2 times / day Route: oral Route: steady Dose: 300 mg, 2 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
Rash | 1.4% Disc. AE |
300 mg 2 times / day steady, oral Recommended Dose: 300 mg, 2 times / day Route: oral Route: steady Dose: 300 mg, 2 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
Abnormal gait | 1.7% Disc. AE |
300 mg 2 times / day steady, oral Recommended Dose: 300 mg, 2 times / day Route: oral Route: steady Dose: 300 mg, 2 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
Tremor | 1.8% Disc. AE |
300 mg 2 times / day steady, oral Recommended Dose: 300 mg, 2 times / day Route: oral Route: steady Dose: 300 mg, 2 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
Abnormal vision | 2.1% Disc. AE |
300 mg 2 times / day steady, oral Recommended Dose: 300 mg, 2 times / day Route: oral Route: steady Dose: 300 mg, 2 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
Fatigue | 2.1% Disc. AE |
300 mg 2 times / day steady, oral Recommended Dose: 300 mg, 2 times / day Route: oral Route: steady Dose: 300 mg, 2 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
Headache | 2.9% Disc. AE |
300 mg 2 times / day steady, oral Recommended Dose: 300 mg, 2 times / day Route: oral Route: steady Dose: 300 mg, 2 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
Somnolence | 3.8% Disc. AE |
300 mg 2 times / day steady, oral Recommended Dose: 300 mg, 2 times / day Route: oral Route: steady Dose: 300 mg, 2 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
Nausea | 4.9% Disc. AE |
300 mg 2 times / day steady, oral Recommended Dose: 300 mg, 2 times / day Route: oral Route: steady Dose: 300 mg, 2 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
Vomiting | 5.1% Disc. AE |
300 mg 2 times / day steady, oral Recommended Dose: 300 mg, 2 times / day Route: oral Route: steady Dose: 300 mg, 2 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
Ataxia | 5.2% Disc. AE |
300 mg 2 times / day steady, oral Recommended Dose: 300 mg, 2 times / day Route: oral Route: steady Dose: 300 mg, 2 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
Diplopia | 5.9% Disc. AE |
300 mg 2 times / day steady, oral Recommended Dose: 300 mg, 2 times / day Route: oral Route: steady Dose: 300 mg, 2 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
Dizziness | 6.4% Disc. AE |
300 mg 2 times / day steady, oral Recommended Dose: 300 mg, 2 times / day Route: oral Route: steady Dose: 300 mg, 2 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult 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 |
---|---|---|
Oxcarbazepine in the treatment of epilepsy. | 2001 Aug |
|
Removal of 10-hydroxycarbazepine by plasmapheresis. | 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 |
|
Thyroid function in men taking carbamazepine, oxcarbazepine, or valproate for epilepsy. | 2001 Jul |
|
Monotherapy trials: presurgical studies. | 2001 May |
|
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 |
|
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 |
|
Recommendations on the clinical use of oxcarbazepine in the treatment of epilepsy: a consensus view. | 2001 Sep |
|
Levetiracetam, oxcarbazepine, remacemide and zonisamide for drug resistant localization-related epilepsy: a systematic review. | 2001 Sep |
|
Oxcarbazepine (Trileptal) as monotherapy in patients with partial seizures. | 2001 Sep 11 |
|
Clinical pharmacodynamics and pharmacokinetics of antimanic and mood-stabilizing medications. | 2002 |
|
The 'number needed to treat' with levetiracetam (LEV): comparison with the other new antiepileptic drugs (AEDs). | 2002 Apr |
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Oxcarbazepine-induced syndrome of inappropriate secretion of antidiuretic hormone. | 2002 Aug |
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Women with PTSD: the psychodynamic aspects of psychopharmacologic and "hands-on" psychiatric management. | 2002 Fall |
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Oxcarbazepine treatment of refractory bipolar disorder: a retrospective chart review. | 2002 Feb |
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New antiepileptic drugs: review on drug interactions. | 2002 Feb |
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Enzyme-inducing antiepileptic drugs in pregnancy and the risk of bleeding in the neonate. | 2002 Feb 26 |
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Using the new antiepilepsy drugs in children. | 2002 Jan |
|
Newer therapies in the drug treatment of epilepsy. | 2002 Jan |
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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 |
|
Gateways to Clinical Trials. June 2002. | 2002 Jun |
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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 |
|
Oxcarbazepine final market image tablet formulation bioequivalence study after single administration and at steady state in healthy subjects. | 2002 Nov |
|
Oxcarbazepine for mood disorders. | 2002 Oct |
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[Monitoring serum levels of new antiepileptics]. | 2002 Sep |
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[Characteristics and indications of oxcarbazepine]. | 2002 Sep |
|
Octakis-6-sulfato-gamma-cyclodextrin as additive for capillary electrokinetic chromatography of dibenzoazepines: carbamazepine, oxcarbamazepine and their metabolites. | 2002 Sep |
|
Use of anticonvulsants for treatment of neuropathic pain. | 2002 Sep 10 |
|
Antiepileptic drug use during the first 12 months of vagus nerve stimulation therapy: a registry study. | 2002 Sep 24 |
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Pharmacokinetics of mood stabilizers and new anticonvulsants. | 2002 Winter |
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Assessment of the bioequivalence of two oxcarbazepine oral suspensions versus a film-coated tablet in healthy subjects. | 2003 Jul |
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Overview of the clinical pharmacokinetics of oxcarbazepine. | 2004 |
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Simultaneous liquid chromatographic determination of lamotrigine, oxcarbazepine monohydroxy derivative and felbamate in plasma of patients with epilepsy. | 2005 Dec 15 |
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Drug monitoring and toxicology: a procedure for the monitoring of oxcarbazepine metabolite by HPLC-UV. | 2006 Jan |
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A novel enantioselective microassay for the high-performance liquid chromatography determination of oxcarbazepine and its active metabolite monohydroxycarbazepine in human plasma. | 2007 Jun |
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Stereoselective disposition of S- and R-licarbazepine in mice. | 2008 Jun |
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Pharmacokinetics of licarbazepine in healthy volunteers: single and multiple oral doses and effect of food. | 2008 May |
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Binding of licarbazepine enantiomers to mouse and human plasma proteins. | 2010 Jul |
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Development and validation of an HPLC-UV method for the simultaneous quantification of carbamazepine, oxcarbazepine, eslicarbazepine acetate and their main metabolites in human plasma. | 2010 Jun |
Sample Use Guides
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/20578208
Free and bound fractions of S-licarbazepine (S-Lic) and R-licarbazepine (R-Lic) were separated by ultrafiltration after previous in vitro incubation of spiked plasma samples and protein solutions with each enantiomer at 10, 25 and 50 ug/ml.
Substance Class |
Chemical
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by
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on
Edited
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Record UNII |
VZI5B1W380
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Validated (UNII)
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NCI_THESAURUS |
C264
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LIVERTOX |
NBK548414
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NDF-RT |
N0000008486
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NDF-RT |
N0000175753
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WHO-VATC |
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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VZI5B1W380
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C036006
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VZI5B1W380
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2017
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32624
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758693
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100000092224
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34312
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7824
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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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BASIS OF STRENGTH->SUBSTANCE |
ASSAY (HPLC)
EP
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METABOLIC ENZYME -> INDUCER |
Ki
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Related Record | Type | Details | ||
---|---|---|---|---|
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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 | ||
---|---|---|---|---|
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IMPURITY -> PARENT |
UNSPECIFIED
EP
|
||
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IMPURITY -> PARENT |
UNSPECIFIED
EP
|
||
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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
|
||
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IMPURITY -> PARENT |
|
||
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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
|
||
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IMPURITY -> PARENT |
UNSPECIFIED
EP
|
||
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IMPURITY -> PARENT |
UNSPECIFIED
EP
|
||
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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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||
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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 |
|
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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