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IdentificationPharmacologyInteractionsReferencesTrialsEconomicsPropertiesSpectraTaxonomyIdentification
- Name
- Oxcarbazepine
- Accession Number
- DB00776 (APRD01308)
- Type
- Small Molecule
- Groups
- Approved
- Description
Oxcarbazepine is structurally a derivative of carbamazepine, adding an extra oxygen atom to the benzylcarboxamide group. This difference helps reduce the impact on the liver of metabolizing the drug, and also prevents the serious forms of anemia occasionally associated with carbamazepine. Aside from this reduction in side effects, it is thought to have the same mechanism as carbamazepine - sodium channel inhibition - and is generally used to treat partial seizures in epileptic children and adults.
- Structure
Structure for DB00776 (Oxcarbazepine)
- Synonyms
- 10,11-Dihydro-10-oxo-5H-dibenz(b,f)azepine-5-carboxamide
- OCBZ
- Oxcarbamazepine
- Oxcarbazepina
- Oxcarbazepinum
- External IDs
- GP 47680 / GP-47680 / KIN-493 / SPN-804
- Product Images
- Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Oxcarbazepine Tablet 600 mg Oral Jubilant Generics Limited Not applicable Not applicable Canada 
Oxcarbazepine Tablet 300 mg Oral Jubilant Generics Limited Not applicable Not applicable Canada Oxcarbazepine Tablet 150 mg Oral Jubilant Generics Limited Not applicable Not applicable Canada Oxtellar XR Tablet 300 mg/1 Oral Supernus 2013-01-17 Not applicable US 
Oxtellar XR Tablet 150 mg/1 Oral Supernus 2013-01-17 Not applicable US Oxtellar XR Tablet 600 mg/1 Oral Supernus 2013-01-17 Not applicable US 
Sandoz Oxcarbazepine Tablet 300 mg Oral Sandoz Canada Incorporated Not applicable Not applicable Canada Sandoz Oxcarbazepine Tablet 150 mg Oral Sandoz Canada Incorporated Not applicable Not applicable Canada Sandoz Oxcarbazepine Tablet 600 mg Oral Sandoz Canada Incorporated Not applicable Not applicable Canada Trileptal Tablet, film coated 150 mg/1 Oral Physicians Total Care, Inc. 2003-07-07 Not applicable US 
- Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Apo-oxcarbazepine Tablet 150 mg Oral Apotex Corporation 2006-08-01 Not applicable Canada Apo-oxcarbazepine Tablet 600 mg Oral Apotex Corporation 2006-08-01 Not applicable Canada Apo-oxcarbazepine Tablet 300 mg Oral Apotex Corporation 2006-08-01 Not applicable Canada Jamp-oxcarbazepine Tablet 150 mg Oral Jamp Pharma Corporation 2015-06-08 Not applicable Canada Jamp-oxcarbazepine Tablet 600 mg Oral Jamp Pharma Corporation 2015-06-08 Not applicable Canada Jamp-oxcarbazepine Tablet 300 mg Oral Jamp Pharma Corporation 2015-06-08 Not applicable Canada Novo-oxcarbazepine Tablet 300 mg Oral Novopharm Limited Not applicable Not applicable Canada Novo-oxcarbazepine Tablet 150 mg Oral Novopharm Limited Not applicable Not applicable Canada Novo-oxcarbazepine Tablet 600 mg Oral Novopharm Limited Not applicable Not applicable Canada Oxcarbazepine Suspension 60 mg/mL Oral Ranbaxy Inc. 2009-12-14 Not applicable US - International/Other Brands
- Actinium / Barzepin / Carbox / Deprectal / Lonazet / Oxalepsy / Oxetol / Oxpin / Oxrate / Oxypine / Pharozepine / Prolepsi / Timox / Trexapin / Trileptin
- Categories
- Anti-epileptic Agent
- Anticonvulsants
- Carboxamide Derivatives
- Cardiovascular Agents
- Central Nervous System Agents
- Central Nervous System Depressants
- Chemically-Induced Disorders
- Cytochrome P-450 CYP3A Inducers
- Cytochrome P-450 Enzyme Inducers
- Cytochrome P-450 Enzyme Inhibitors
- Dibenzazepines
- Enzyme Inducing Antiepileptic Drugs
- Membrane Transport Modulators
- Miscellaneous Anticonvulsants
- Nervous System
- Sodium Channel Blockers
- Voltage-Gated Sodium Channel Blockers
- UNII
- VZI5B1W380
- CAS number
- 28721-07-5
- Weight
- Average: 252.268
Monoisotopic: 252.089877638 - Chemical Formula
- C15H12N2O2
- InChI Key
- CTRLABGOLIVAIY-UHFFFAOYSA-N
- InChI
- 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)
- IUPAC Name
- 9-oxo-2-azatricyclo[9.4.0.0^{3,8}]pentadeca-1(15),3,5,7,11,13-hexaene-2-carboxamide
- SMILES
- NC(=O)N1C2=CC=CC=C2CC(=O)C2=C1C=CC=C2
Pharmacology
- Indication
For use as monotherapy or adjunctive therapy in the treatment of partial seizures in adults with epilepsy and as adjunctive therapy in the treatment of partial seizures in children ages 4-16 with epilepsy.
- Associated Conditions
- Pharmacodynamics
Oxcarbazepine is structurally a derivative of carbamazepine, adding an extra oxygen atom to the benzylcarboxamide group. This difference helps reduce the impact on the liver of metabolizing the drug, and also prevents the serious forms of anemia occasionally associated with carbamazepine. Aside from this reduction in side effects, it is thought to have the same mechanism as carbamazepine - sodium channel inhibition - and is generally used to treat the same conditions.
- Mechanism of action
The exact mechanism by which oxcarbazepine exerts its anticonvulsant effect is unknown. It is known that the pharmacological activity of oxcarbazepine occurs primarily through its 10-monohydroxy metabolite (MHD). In vitro studies indicate an MHD-induced blockade of voltage-sensitive sodium channels, resulting in stabilization of hyperexcited neuronal membranes, inhibition of repetitive neuronal discharges, and diminution of propagation of synaptic impulses.
Target Actions Organism ASodium channel protein type 5 subunit alpha inhibitorHuman - Absorption
Completely absorbed following oral administration. Food has no effect on the rate and extent of absorption of oxcarbazepine. After single-dose administration of Trileptal tablets to healthy male volunteers under fasted conditions, the median tmax was 4.5 (range 3 to 13) hours. After single-dose administration of Trileptal oral suspension to healthy male volunteers under fasted conditions, the median tmax was six hours. Steady-state plasma concentrations of MHD are reached within 2-3 days in patients when Trileptal is given twice a day.
- Volume of distribution
- 49 L
- Protein binding
Approximately 40% of the active 10-monohydroxy metabolite (MHD) is bound to serum proteins, predominantly to albumin. Neither oxcarbazepine nor its MHD binds with alpha-1-acid glycoprotein.
- Metabolism
Oxcarbazepine is completely absorbed and extensively metabolized to its pharmacologically active 10-monohydroxy metabolite (MHD) by cytosolic enzymes. MHD is metabolized further by conjugation with glucuronic acid.
- Route of elimination
Oxcarbazepine is cleared from the body mostly in the form of metabolites which are predominantly excreted by the kidneys. Fecal excretion accounts for less than 4% of the administered dose.
- Half life
The half-life of the parent is about 2 hours, while the half-life of MHD is about 9 hours, so that MHD is responsible for most anti-epileptic activity.
- Clearance
- Not Available
- Toxicity
Isolated cases of overdose with oxcarbazepine have been reported. The maximum dose taken was approximately 24,000 mg. All patients recovered with symptomatic treatment.
- Affected organisms
- Humans and other mammals
- Pathways
Pathway Category Carbamazepine Metabolism Pathway Drug metabolism - Pharmacogenomic Effects/ADRs
Interacting Gene/Enzyme Allele name Genotype(s) Defining Change(s) Type(s) Description Details HLA class I histocompatibility antigen, B-15 alpha chain HLA-B*15:02 Not Available HLA-B*15 ADR Directly Studied Patients who carry this allele may be at an increased risk of Stevens-Johnson Syndrome and toxic epidermal necrolysis when treated with oxcarbazepine. Details
Interactions
- Drug Interactions
Drug Interaction Drug group Aripiprazole The serum concentration of Aripiprazole can be decreased when it is combined with Oxcarbazepine. Approved, Investigational Asunaprevir The serum concentration of Asunaprevir can be decreased when it is combined with Oxcarbazepine. Approved, Investigational, Withdrawn Bendroflumethiazide The risk or severity of hyponatremia can be increased when Bendroflumethiazide is combined with Oxcarbazepine. Approved Benzthiazide The risk or severity of hyponatremia can be increased when Benzthiazide is combined with Oxcarbazepine. Approved Carbamazepine The serum concentration of the active metabolites of Oxcarbazepine can be reduced when Oxcarbazepine is used in combination with Carbamazepine resulting in a loss in efficacy. Approved, Investigational Chlormadinone The serum concentration of Chlormadinone can be decreased when it is combined with Oxcarbazepine. Experimental Chlorothiazide The risk or severity of hyponatremia can be increased when Chlorothiazide is combined with Oxcarbazepine. Approved, Vet Approved Chlorthalidone The risk or severity of hyponatremia can be increased when Chlorthalidone is combined with Oxcarbazepine. Approved Cilostazol The serum concentration of Cilostazol can be increased when it is combined with Oxcarbazepine. Approved, Investigational Cobicistat The serum concentration of Cobicistat can be decreased when it is combined with Oxcarbazepine. Approved Cyclopenthiazide The risk or severity of hyponatremia can be increased when Cyclopenthiazide is combined with Oxcarbazepine. Experimental Cyproterone acetate The serum concentration of Cyproterone acetate can be decreased when it is combined with Oxcarbazepine. Approved, Investigational Desogestrel The serum concentration of Desogestrel can be decreased when it is combined with Oxcarbazepine. Approved Dienogest The serum concentration of Dienogest can be decreased when it is combined with Oxcarbazepine. Approved Diethylstilbestrol The serum concentration of Diethylstilbestrol can be decreased when it is combined with Oxcarbazepine. Approved, Investigational Dolutegravir The serum concentration of Dolutegravir can be decreased when it is combined with Oxcarbazepine. Approved Doxofylline The serum concentration of Doxofylline can be decreased when it is combined with Oxcarbazepine. Approved, Investigational Drospirenone The serum concentration of Drospirenone can be decreased when it is combined with Oxcarbazepine. Approved Elvitegravir The serum concentration of Elvitegravir can be decreased when it is combined with Oxcarbazepine. Approved Epitizide The risk or severity of hyponatremia can be increased when Epitizide is combined with Oxcarbazepine. Experimental Eslicarbazepine acetate The risk or severity of adverse effects can be increased when Eslicarbazepine acetate is combined with Oxcarbazepine. Approved Estradiol The serum concentration of Estradiol can be decreased when it is combined with Oxcarbazepine. Approved, Investigational, Vet Approved Estradiol cypionate The serum concentration of Estradiol cypionate can be decreased when it is combined with Oxcarbazepine. Approved, Investigational, Vet Approved Estradiol valerate The serum concentration of Estradiol valerate can be decreased when it is combined with Oxcarbazepine. Approved, Investigational, Vet Approved Ethanol Ethanol may increase the central nervous system depressant (CNS depressant) activities of Oxcarbazepine. Approved Ethinyl Estradiol The serum concentration of Ethinyl Estradiol can be decreased when it is combined with Oxcarbazepine. Approved Ethynodiol diacetate The serum concentration of Ethynodiol diacetate can be decreased when it is combined with Oxcarbazepine. Approved Etonogestrel The serum concentration of Etonogestrel can be decreased when it is combined with Oxcarbazepine. Approved, Investigational Fosphenytoin The serum concentration of the active metabolites of Oxcarbazepine can be reduced when Oxcarbazepine is used in combination with Fosphenytoin resulting in a loss in efficacy. Approved, Investigational Gestodene The serum concentration of Gestodene can be decreased when it is combined with Oxcarbazepine. Approved, Investigational Gestrinone The serum concentration of Gestrinone can be decreased when it is combined with Oxcarbazepine. Approved Hydrochlorothiazide The risk or severity of hyponatremia can be increased when Hydrochlorothiazide is combined with Oxcarbazepine. Approved, Vet Approved Hydroflumethiazide The risk or severity of hyponatremia can be increased when Hydroflumethiazide is combined with Oxcarbazepine. Approved, Investigational Hydroxyprogesterone caproate The serum concentration of Hydroxyprogesterone caproate can be decreased when it is combined with Oxcarbazepine. Approved, Investigational Indapamide The risk or severity of hyponatremia can be increased when Indapamide is combined with Oxcarbazepine. Approved Ledipasvir The serum concentration of Ledipasvir can be decreased when it is combined with Oxcarbazepine. Approved Levonorgestrel The serum concentration of Levonorgestrel can be decreased when it is combined with Oxcarbazepine. Approved, Investigational Lynestrenol The serum concentration of Lynestrenol can be decreased when it is combined with Oxcarbazepine. Approved, Investigational Medroxyprogesterone acetate The serum concentration of Medroxyprogesterone acetate can be decreased when it is combined with Oxcarbazepine. Approved, Investigational Mefloquine The therapeutic efficacy of Oxcarbazepine can be decreased when used in combination with Mefloquine. Approved, Investigational Megestrol acetate The serum concentration of Megestrol acetate can be decreased when it is combined with Oxcarbazepine. Approved, Investigational, Vet Approved Mestranol The serum concentration of Mestranol can be decreased when it is combined with Oxcarbazepine. Approved Methyclothiazide The risk or severity of hyponatremia can be increased when Methyclothiazide is combined with Oxcarbazepine. Approved Metolazone The risk or severity of hyponatremia can be increased when Metolazone is combined with Oxcarbazepine. Approved Mianserin The therapeutic efficacy of Oxcarbazepine can be decreased when used in combination with Mianserin. Approved, Investigational Nomegestrol acetate The serum concentration of Nomegestrol acetate can be decreased when it is combined with Oxcarbazepine. Approved, Investigational Norelgestromin The serum concentration of Norelgestromin can be decreased when it is combined with Oxcarbazepine. Approved, Investigational Norethisterone The serum concentration of Norethisterone can be decreased when it is combined with Oxcarbazepine. Approved Norethynodrel The serum concentration of Norethynodrel can be decreased when it is combined with Oxcarbazepine. Approved Norgestimate The serum concentration of Norgestimate can be decreased when it is combined with Oxcarbazepine. Approved, Investigational Norgestrel The serum concentration of Norgestrel can be decreased when it is combined with Oxcarbazepine. Approved Norgestrienone The serum concentration of Norgestrienone can be decreased when it is combined with Oxcarbazepine. Experimental Orlistat The serum concentration of Oxcarbazepine can be decreased when it is combined with Orlistat. Approved, Investigational Perampanel The serum concentration of Oxcarbazepine can be increased when it is combined with Perampanel. Approved Phenobarbital The serum concentration of the active metabolites of Oxcarbazepine can be reduced when Oxcarbazepine is used in combination with Phenobarbital resulting in a loss in efficacy. Approved, Investigational Phenytoin The serum concentration of the active metabolites of Oxcarbazepine can be reduced when Oxcarbazepine is used in combination with Phenytoin resulting in a loss in efficacy. Approved, Vet Approved Polythiazide The risk or severity of hyponatremia can be increased when Polythiazide is combined with Oxcarbazepine. Approved Pregabalin The therapeutic efficacy of Oxcarbazepine can be decreased when used in combination with Pregabalin. Approved, Illicit, Investigational Quinethazone The risk or severity of hyponatremia can be increased when Quinethazone is combined with Oxcarbazepine. Approved Quingestanol The serum concentration of Quingestanol can be decreased when it is combined with Oxcarbazepine. Experimental Rilpivirine The serum concentration of Rilpivirine can be decreased when it is combined with Oxcarbazepine. Approved Saxagliptin The serum concentration of Saxagliptin can be decreased when it is combined with Oxcarbazepine. Approved Selegiline Oxcarbazepine may increase the serotonergic activities of Selegiline. Approved, Investigational, Vet Approved Sofosbuvir The serum concentration of Sofosbuvir can be decreased when it is combined with Oxcarbazepine. Approved Trichlormethiazide The risk or severity of hyponatremia can be increased when Trichlormethiazide is combined with Oxcarbazepine. Approved, Vet Approved Ulipristal The serum concentration of Ulipristal can be decreased when it is combined with Oxcarbazepine. Approved Valproic Acid The serum concentration of Oxcarbazepine can be decreased when it is combined with Valproic Acid. Approved, Investigational - Food Interactions
- Take without regard to meals. Avoid alcohol.
References
- Synthesis Reference
Judith Aronhime, "New crystal forms of oxcarbazepine and processes for their preparation." U.S. Patent US20030004154, issued January 02, 2003.
US20030004154- General References
- Mazza M, Della Marca G, Di Nicola M, Martinotti G, Pozzi G, Janiri L, Bria P, Mazza S: Oxcarbazepine improves mood in patients with epilepsy. Epilepsy Behav. 2007 May;10(3):397-401. Epub 2007 Feb 14. [PubMed:17300991]
- External Links
- Human Metabolome Database
- HMDB0014914
- KEGG Drug
- D00533
- KEGG Compound
- C07492
- PubChem Compound
- 34312
- PubChem Substance
- 46507580
- ChemSpider
- 31608
- BindingDB
- 34179
- ChEBI
- 7824
- ChEMBL
- CHEMBL1068
- Therapeutic Targets Database
- DAP000528
- PharmGKB
- PA450732
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- PDRhealth
- PDRhealth Drug Page
- Wikipedia
- Oxcarbazepine
- ATC Codes
- N03AF02 — Oxcarbazepine
- AHFS Codes
- 28:12.92 — Miscellaneous Anticonvulsants
- FDA label
- Download (195 KB)
Clinical Trials
- Clinical Trials
Pharmacoeconomics
- Manufacturers
- Ranbaxy laboratories ltd
- Novartis pharmaceuticals corp
- Apotex inc
- Breckenridge pharmaceutical inc
- Cadista pharmaceuticals inc
- Glenmark generics ltd
- Roxane laboratories inc
- Sun pharmaceutical industries ltd
- Taro pharmaceutical industries ltd
- Teva pharmaceuticals usa
- Packagers
- Amerisource Health Services Corp.
- Apotex Inc.
- Ascend Laboratories LLC
- Atlantic Biologicals Corporation
- Breckenridge Pharmaceuticals
- Bryant Ranch Prepack
- Cardinal Health
- Glenmark Generics Ltd.
- Innoviant Pharmacy Inc.
- Murfreesboro Pharmaceutical Nursing Supply
- Nexgen Pharma Inc.
- Novartis AG
- Nucare Pharmaceuticals Inc.
- PD-Rx Pharmaceuticals Inc.
- Physicians Total Care Inc.
- Ranbaxy Laboratories
- Rebel Distributors Corp.
- Remedy Repack
- Resource Optimization and Innovation LLC
- Roxane Labs
- Sandoz
- Southwood Pharmaceuticals
- Sun Pharmaceutical Industries Ltd.
- Taro Pharmaceuticals USA
- Teva Pharmaceutical Industries Ltd.
- Vangard Labs Inc.
- Dosage forms
Form Route Strength Suspension Oral 300 mg/5mL Suspension Oral 60 mg/mL Tablet Oral 150 mg/1 Tablet Oral 300 mg/1 Tablet Oral 600 mg/1 Tablet, film coated Oral 150 mg/1 Tablet, film coated Oral 300 mg/1 Tablet, film coated Oral 600 mg/1 Tablet Oral 150 mg Tablet Oral 300 mg Tablet Oral 600 mg Suspension Oral 60 mg - Prices
Unit description Cost Unit OXcarbazepine 300 mg/5ml Suspension 250ml Bottle 162.03USD bottle Trileptal 600 mg tablet 7.05USD tablet Oxcarbazepine 600 mg tablet 5.06USD tablet Trileptal 300 mg tablet 3.84USD tablet Oxcarbazepine 300 mg tablet 2.75USD tablet Trileptal 150 mg tablet 2.1USD tablet Oxcarbazepine 150 mg tablet 1.53USD tablet Trileptal 300 mg/5ml Suspension 0.79USD ml DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) CA2277791 No 2008-11-18 2018-02-12 Canada US7037525 Yes 1998-08-12 2018-08-12 US US8119148 Yes 2001-06-19 2021-06-19 US US7910131 No 2007-04-13 2027-04-13 US US9119791 No 2007-04-13 2027-04-13 US US8821930 No 2007-04-13 2027-04-13 US US8617600 No 2007-04-13 2027-04-13 US US7722898 No 2007-04-13 2027-04-13 US US9370525 No 2007-04-13 2027-04-13 US US9351975 No 2007-04-13 2027-04-13 US US9855278 No 2007-04-13 2027-04-13 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 215.5 °C PhysProp water solubility 308 mg/L at 25 °C (SRC PhysProp estimated -- MEYLAN,WM et al. (1996)) Not Available logP 1.5 Not Available - Predicted Properties
Property Value Source Water Solubility 0.16 mg/mL ALOGPS logP 1.76 ALOGPS logP 1.82 ChemAxon logS -3.2 ALOGPS pKa (Strongest Acidic) 13.18 ChemAxon pKa (Strongest Basic) -4.3 ChemAxon Physiological Charge 0 ChemAxon Hydrogen Acceptor Count 2 ChemAxon Hydrogen Donor Count 1 ChemAxon Polar Surface Area 63.4 Å2 ChemAxon Rotatable Bond Count 0 ChemAxon Refractivity 71.56 m3·mol-1 ChemAxon Polarizability 25.72 Å3 ChemAxon Number of Rings 3 ChemAxon Bioavailability 1 ChemAxon Rule of Five Yes ChemAxon Ghose Filter Yes ChemAxon Veber's Rule No ChemAxon MDDR-like Rule No ChemAxon - Predicted ADMET features
Property Value Probability Human Intestinal Absorption + 0.9894 Blood Brain Barrier + 0.9975 Caco-2 permeable + 0.6299 P-glycoprotein substrate Non-substrate 0.7157 P-glycoprotein inhibitor I Non-inhibitor 0.7193 P-glycoprotein inhibitor II Non-inhibitor 0.9348 Renal organic cation transporter Non-inhibitor 0.8176 CYP450 2C9 substrate Non-substrate 0.773 CYP450 2D6 substrate Non-substrate 0.9116 CYP450 3A4 substrate Non-substrate 0.6022 CYP450 1A2 substrate Non-inhibitor 0.7266 CYP450 2C9 inhibitor Non-inhibitor 0.7371 CYP450 2D6 inhibitor Non-inhibitor 0.9329 CYP450 2C19 inhibitor Non-inhibitor 0.7428 CYP450 3A4 inhibitor Non-inhibitor 0.8819 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.8034 Ames test Non AMES toxic 0.5078 Carcinogenicity Non-carcinogens 0.9118 Biodegradation Not ready biodegradable 0.8977 Rat acute toxicity 1.9871 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9327 hERG inhibition (predictor II) Non-inhibitor 0.869
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Taxonomy
- Description
- This compound belongs to the class of organic compounds known as dibenzazepines. These are compounds with two benzene rings connected by an azepine ring. Azepine is an unsaturated seven-member heterocycle with one nitrogen atom replacing a carbon atom.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Benzazepines
- Sub Class
- Dibenzazepines
- Direct Parent
- Dibenzazepines
- Alternative Parents
- Aryl alkyl ketones / Azepines / Benzenoids / Vinylogous amides / Isoureas / Azacyclic compounds / Organopnictogen compounds / Organic oxides / Imines / Hydrocarbon derivatives
- Substituents
- Dibenzazepine / Aryl ketone / Aryl alkyl ketone / Azepine / Benzenoid / Vinylogous amide / Isourea / Ketone / Carboximidic acid derivative / Azacycle
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- cyclic ketone, dibenzoazepine (CHEBI:7824)
Targets
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Voltage-gated sodium channel activity involved in sa node cell action potential
- Specific Function
- This protein mediates the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the pr...
- Gene Name
- SCN5A
- Uniprot ID
- Q14524
- Uniprot Name
- Sodium channel protein type 5 subunit alpha
- Molecular Weight
- 226937.475 Da
References
- Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
- Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
- Vohora D, Saraogi P, Yazdani MA, Bhowmik M, Khanam R, Pillai KK: Recent advances in adjunctive therapy for epilepsy: focus on sodium channel blockers as third-generation antiepileptic drugs. Drugs Today (Barc). 2010 Apr;46(4):265-77. doi: 10.1358/dot.2010.46.4.1445795. [PubMed:20502724]
Enzymes
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Steroid hydroxylase activity
- Specific Function
- Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and im...
- Gene Name
- CYP2C19
- Uniprot ID
- P33261
- Uniprot Name
- Cytochrome P450 2C19
- Molecular Weight
- 55930.545 Da
References
- Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
- Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- Inducer
- General Function
- Vitamin d3 25-hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
- Gene Name
- CYP3A4
- Uniprot ID
- P08684
- Uniprot Name
- Cytochrome P450 3A4
- Molecular Weight
- 57342.67 Da
References
- Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- Inducer
- General Function
- Oxygen binding
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP3A5
- Uniprot ID
- P20815
- Uniprot Name
- Cytochrome P450 3A5
- Molecular Weight
- 57108.065 Da
References
- Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Carriers
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Toxic substance binding
- Specific Function
- Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
- Gene Name
- ALB
- Uniprot ID
- P02768
- Uniprot Name
- Serum albumin
- Molecular Weight
- 69365.94 Da
Drug created on June 13, 2005 07:24 / Updated on June 20, 2018 23:54