Details
Stereochemistry | RACEMIC |
Molecular Formula | C15H14N2O2 |
Molecular Weight | 254.2839 |
Optical Activity | ( + / - ) |
Defined Stereocenters | 0 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
NC(=O)N1C2=CC=CC=C2CC(O)C3=C1C=CC=C3
InChI
InChIKey=BMPDWHIDQYTSHX-UHFFFAOYSA-N
InChI=1S/C15H14N2O2/c16-15(19)17-12-7-3-1-5-10(12)9-14(18)11-6-2-4-8-13(11)17/h1-8,14,18H,9H2,(H2,16,19)
Molecular Formula | C15H14N2O2 |
Molecular Weight | 254.2839 |
Charge | 0 |
Count |
|
Stereochemistry | RACEMIC |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 1 |
E/Z Centers | 0 |
Optical Activity | ( + / - ) |
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 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 |
|
Second generation anticonvulsant medications: their use in children. | 2001 Apr |
|
Clinical pharmacology and therapeutic use of the new antiepileptic drugs. | 2001 Dec |
|
Suppressive effects of oxcarbazepine on tooth pulp-evoked potentials recorded at the trigeminal spinal tract nucleus in cats. | 2001 Mar |
|
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 |
|
Anticonvulsants in the treatment of mood disorders: assessing current and future roles. | 2001 Oct |
|
Treatment of epilepsy in women of reproductive age: pharmacokinetic considerations. | 2002 |
|
Interactions between antiepileptic drugs and hormonal contraception. | 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 |
|
The 'number needed to treat' with levetiracetam (LEV): comparison with the other new antiepileptic drugs (AEDs). | 2002 Apr |
|
Gabapentin: new indication. Little impact on partial epilepsy in children between 3 and 12. | 2002 Apr |
|
Oxcarbazepine and hepatic porphyria. | 2002 Apr |
|
Oxcarbazepine-induced syndrome of inappropriate secretion of antidiuretic hormone. | 2002 Aug |
|
Women with PTSD: the psychodynamic aspects of psychopharmacologic and "hands-on" psychiatric management. | 2002 Fall |
|
Mechanisms of action of carbamazepine and its derivatives, oxcarbazepine, BIA 2-093, and BIA 2-024. | 2002 Feb |
|
Metabolism of 10,11-dihydro-10-hydroxyimino-5H-dibenz/b, f/azepine-5-carboxamide, a potent anti-epileptic drug. | 2002 Feb |
|
The promise of new antiepileptic drugs. | 2002 Feb |
|
Long-term cohort study comparing medical (oxcarbazepine) and surgical management of intractable trigeminal neuralgia. | 2002 Feb |
|
Enzyme-inducing antiepileptic drugs in pregnancy and the risk of bleeding in the neonate. | 2002 Feb 26 |
|
Pediatric partial and generalized seizures. | 2002 Jan |
|
Using the new antiepilepsy drugs in children. | 2002 Jan |
|
Three new drugs for epilepsy: levetiracetam, oxcarbazepine, and zonisamide. | 2002 Jan |
|
Oxcarbazepine. | 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 |
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Gateways to Clinical Trials. June 2002. | 2002 Jun |
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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 |
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Some common issues in the use of antiepileptic drugs. | 2002 Mar |
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Oxcarbazepine and hyponatremia. | 2002 Mar 1 |
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Effects of oxcarbazepine on sodium concentration and water handling. | 2002 May |
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[New antiepileptic drugs: new therapeutic options]. | 2002 May |
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LC determination of oxcarbazepine and its active metabolite in human serum. | 2002 May 15 |
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Oxcarbazepine final market image tablet formulation bioequivalence study after single administration and at steady state in healthy subjects. | 2002 Nov |
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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 |
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Progress report on new antiepileptic drugs: a summary of the Sixth Eilat Conference (EILAT VI). | 2002 Sep |
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Octakis-6-sulfato-gamma-cyclodextrin as additive for capillary electrokinetic chromatography of dibenzoazepines: carbamazepine, oxcarbamazepine and their metabolites. | 2002 Sep |
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Use of anticonvulsants for treatment of neuropathic pain. | 2002 Sep 10 |
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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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Safety, tolerability, and pharmacokinetic profile of BIA 2-093, a novel putative antiepileptic, in a rising multiple-dose study in young healthy humans. | 2004 Aug |
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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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Eyeblink conditioning anomalies in bipolar disorder suggest cerebellar dysfunction. | 2009 Feb |
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Binding of licarbazepine enantiomers to mouse and human plasma proteins. | 2010 Jul |
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
Created
by
admin
on
Edited
Wed Jul 05 23:23:55 UTC 2023
by
admin
on
Wed Jul 05 23:23:55 UTC 2023
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Record UNII |
XFX1A5KJ3V
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Validated (UNII)
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C264
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BINDER->LIGAND |
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PRODRUG -> METABOLITE ACTIVE |
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ACTIVE MOIETY |
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