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Identification
NameClobazam
Accession NumberDB00349  (APRD00307)
TypeSmall Molecule
GroupsApproved, Illicit
Description

Clobazam belongs to the 1,5-benzodiazepine class of drugs and is expected to have a better side-effect profile compared to older 1,4-benzodiazepines. It has been marketed as an anxiolytic since 1975 and an anticonvulsant since 1984. The oral preparation was FDA approved on October 21, 2011. An oral suspension is expected to be available in 2013.

Structure
Thumb
Synonyms
1-phenyl-5-methyl-8-chloro-1,2,4,5-tetrahydro-2,4-dioxo-3H-1,5-benzodiazepine
7-Chloro-1-methyl-5-phenyl-1,5-dihydro-benzo[b][1,4]diazepine-2,4-dione
Clobazam
Clobazamum
External Identifiers
  • H 4723
  • HR 376
  • LM 2717
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Clobazam-10tablet10 mgoralPro Doc Limitee2003-12-09Not applicableCanada
Dom-clobazamtablet10 mgoralDominion Pharmacal2003-03-27Not applicableCanada
Frisium Tab 10mgtablet10 mgoralHoechst Canada Inc.1991-12-311996-08-29Canada
Frisium Tablet 10mgtablet10 mgoralLundbeck LLC1997-03-24Not applicableCanada
Frisium Tablets 10mgtablet10 mgoralHoechst Roussel Canada Inc.1994-12-311999-08-11Canada
Novo-clobazamtablet10 mgoralTeva Canada Limited1998-07-07Not applicableCanada
Ntp-clobazamtablet10 mgoralTeva Canada LimitedNot applicableNot applicableCanada
Onfitablet5 mg/1oralLundbeck LLC2011-10-212016-02-28Us
Onfitablet20 mg/1oralLundbeck LLC2013-12-10Not applicableUs
Onfitablet10 mg/1oralLundbeck LLC2013-12-10Not applicableUs
Onfisuspension2.5 mg/mLoralLundbeck LLC2012-12-14Not applicableUs
Onfitablet20 mg/1oralLundbeck LLC2013-08-12Not applicableUs
Onfitablet10 mg/1oralLundbeck LLC2013-08-12Not applicableUs
PMS-clobazamtablet10 mgoralPharmascience Inc2001-11-16Not applicableCanada
Ratio-clobazamtablet10 mgoralRatiopharm Inc Division Of Teva Canada Limited1998-11-302010-08-02Canada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-clobazam Tabletstablet10 mgoralApotex Inc2001-11-28Not applicableCanada
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
AedonSanofi-Aventis
CastiliumSanofi-Aventis
ClobamSquare
ClobamaxSherfarma
FrisiumSanofi-Aventis
GrifoclobamChile
MystanDainippon Sumitomo
NoiafrenSanofi Aventis
SederlonaNot Available
UrbanilSanofi-Aventis
UrbanolSanofi-Aventis
UrbanylSanofi-Aventis
VeniumHudson
Brand mixturesNot Available
SaltsNot Available
Categories
UNII2MRO291B4U
CAS number22316-47-8
WeightAverage: 300.74
Monoisotopic: 300.066555377
Chemical FormulaC16H13ClN2O2
InChI KeyInChIKey=CXOXHMZGEKVPMT-UHFFFAOYSA-N
InChI
InChI=1S/C16H13ClN2O2/c1-18-13-8-7-11(17)9-14(13)19(16(21)10-15(18)20)12-5-3-2-4-6-12/h2-9H,10H2,1H3
IUPAC Name
7-chloro-1-methyl-5-phenyl-2,3,4,5-tetrahydro-1H-1,5-benzodiazepine-2,4-dione
SMILES
CN1C2=C(C=C(Cl)C=C2)N(C2=CC=CC=C2)C(=O)CC1=O
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as benzodiazepines. These are organic compounds containing a benzene ring fused to either isomers of diazepine(unsaturated seven-member heterocycle with two nitrogen atoms replacing two carbon atoms).
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassBenzodiazepines
Sub ClassNot Available
Direct ParentBenzodiazepines
Alternative Parents
Substituents
  • Benzodiazepine
  • Chlorobenzene
  • Para-diazepine
  • Benzenoid
  • 1,3-dicarbonyl compound
  • Monocyclic benzene moiety
  • Aryl halide
  • Aryl chloride
  • Tertiary carboxylic acid amide
  • Tertiary amine
  • Lactam
  • Carboxamide group
  • Azacycle
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Organochloride
  • Organohalogen compound
  • Carbonyl group
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationFor treatment and management of epilepsy and seizures associated with Lennox-Gastaut syndrome, a difficult-to-treat form of childhood epilepsy.
PharmacodynamicsSimilar to other benzodiazepines, clobazam binds to the interface of the α and γ2-subunit of the GABA-A receptor. However, it is considered a partial agonist to GABA-A receptors which sets clobazam apart from 1,4-benzodiazepines which are full agonist. The significance of this difference is that one may experience less sedation with clobazam than with other benzodiazepines. Unlike the endogenous GABA ligand, clobazam binds allosterically to the GABA receptor to increase the frequency of the chloride channel opening and membrane permeability to chloride ions. Pharmacodynamic tolerance has been demonstrated in animal models.
Mechanism of actionClobazam binds at distinct binding sites associated with the chloride ionopore at the post-synaptic GABA receptor. These GABA receptors are in various locations in the CNS (limbic, reticular formation) and clobazam increases the duration of time for which the chloride ionopore is open. As a result, hyper polarization and stabilization of the membrane occur as the post-synaptic inhibitory effect of GABA is enhanced.
Related Articles
AbsorptionAfter oral administration of clobazam, it is almost completely absorbed (87% of dose). Bioavailability relative to solution was almost at 100%. Food does not affect absorption. Tmax = 1-3 hours.
Volume of distribution

Vdss = 100 L. This high volume of distribution suggests extensive distribution to body tissues.

Protein bindingClobazam is the primary circulating entity in the serum and is highly protein-bound (80-90%).
Metabolism

Clobazam is extensively metabolized in the liver via N-demethylation and hydroxylation. Clobazam has two major metabolites: N-desmethylclobazam (norclobazam) and 4'-hydroxyclobazam, the former of which is active. Norclobazam is one-fourth the potency of clobazam. The main enzyme that facilitates the process of N-demethylation is CYP3A4, and to a lesser extent by CYP2C19 and CYP2B6. Norclobazam itself is also metabolized via hydroxylation, primarily by CYP2C19. The formation of 4'-hydroxyclobazam is facilitated by CYP2C18 and CYP2C19. A factor in determining extent of metabolism is the genetic profile of the individual patient as CYP2C19 is a polymorphic enzyme.

SubstrateEnzymesProduct
Clobazam
norclobazamDetails
Clobazam
Not Available
4'-hydroxyclobazamDetails
Route of eliminationClobazam is eliminated via the urine (~94%) as metabolites.
Half lifeThe mean elimination half life of an oral dose of clobazam 40 mg is 32 hours. It's main metabolite, norclobazam, as a half life of 57 hours. The half life in adult patients with epilepsy are higher than those that are healthy.
Clearance

Median estimated clearance = 2.49 L/h

ToxicityThe most common adverse effects include somnolence, pyrexia, upper respiratory tract infection, and lethargy.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug Reactions
Interacting Gene/EnzymeSNP RS IDAllele nameDefining changeAdverse ReactionReference(s)
Cytochrome P450 2C19
Gene symbol: CYP2C19
UniProt: P33261
rs4244285 CYP2C19*2G > A/CClobazem is metabolized into N-desmethylclobazem (NCLB) mostly by CYP3A4. NCLB is primarily metabolized by 2C19. Those with one 2C19*2 allele mutation (1*/2*) are intermediate metabolizers of NCLB. Those with two (2*/2*) mutations will metabolize NCLB poorly in comparisone to extensive metabolizers (1*/1*). Levels of NCLB can be five times higher in poor metabolizers, and two times higher in intermediate metabolizers as compared to individuals who are extensive metabolizers. The safety and efficacy of clobazem may be affected by polymorphic expression of CYP2C19*2.15483195
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.99
Blood Brain Barrier+0.9904
Caco-2 permeable+0.7487
P-glycoprotein substrateNon-substrate0.5733
P-glycoprotein inhibitor INon-inhibitor0.5462
P-glycoprotein inhibitor IINon-inhibitor0.9204
Renal organic cation transporterNon-inhibitor0.7373
CYP450 2C9 substrateNon-substrate0.7058
CYP450 2D6 substrateNon-substrate0.8607
CYP450 3A4 substrateSubstrate0.6871
CYP450 1A2 substrateNon-inhibitor0.6829
CYP450 2C9 inhibitorNon-inhibitor0.5296
CYP450 2D6 inhibitorNon-inhibitor0.8908
CYP450 2C19 inhibitorNon-inhibitor0.5791
CYP450 3A4 inhibitorInhibitor0.7008
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.5308
Ames testNon AMES toxic0.9132
CarcinogenicityNon-carcinogens0.7846
BiodegradationNot ready biodegradable1.0
Rat acute toxicity1.7313 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9896
hERG inhibition (predictor II)Non-inhibitor0.8651
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
Tabletoral10 mg
Suspensionoral2.5 mg/mL
Tabletoral10 mg/1
Tabletoral20 mg/1
Tabletoral5 mg/1
Prices
Unit descriptionCostUnit
Apo-Clobazam 10 mg Tablet0.23USD tablet
Novo-Clobazam 10 mg Tablet0.23USD tablet
Pms-Clobazam 10 mg Tablet0.23USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point180-182Hauptmann, K.H., Weber, K.-H., Zeile, K., Danneberg, P. and Giesemann, R.; South African Patent 68/0803; February 7,1968; assigned to Boehringer lngelheim GmbH, Germany.
water solubility188 mg/LNot Available
logP2.12HENCZI,M ET AL. (1995)
Predicted Properties
PropertyValueSource
Water Solubility0.164 mg/mLALOGPS
logP2.14ALOGPS
logP2.55ChemAxon
logS-3.3ALOGPS
pKa (Strongest Acidic)4.07ChemAxon
pKa (Strongest Basic)-6.7ChemAxon
Physiological Charge-1ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area40.62 Å2ChemAxon
Rotatable Bond Count1ChemAxon
Refractivity80.3 m3·mol-1ChemAxon
Polarizability30.07 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Download (11.4 KB)
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
MSMass Spectrum (Electron Ionization)splash10-0pb9-6392000000-a76f30f353b3407df0c6View in MoNA
References
Synthesis Reference

Hauptmann, K.H., Weber, K.-H., Zeile, K., Danneberg, P. and Giesemann, R.; South African
Patent 68/0803; February 7,1968; assigned to Boehringer lngelheim GmbH, Germany.

General References
  1. Freche C: [Study of an anxiolytic, clobazam, in otorhinolaryngology in psychosomatic pharyngeal manifestations]. Sem Hop Ther. 1975 Apr;51(4):261-3. [PubMed:5777 ]
  2. Authors unspecified: Clobazam in treatment of refractory epilepsy: the Canadian experience. A retrospective study. Canadian Clobazam Cooperative Group. Epilepsia. 1991 May-Jun;32(3):407-16. [PubMed:2044502 ]
  3. Wildin JD, Pleuvry BJ, Mawer GE, Onon T, Millington L: Respiratory and sedative effects of clobazam and clonazepam in volunteers. Br J Clin Pharmacol. 1990 Feb;29(2):169-77. [PubMed:2106335 ]
  4. Kilpatrick C, Bury R, Fullinfaw R, Moulds R: Clobazam in the treatment of epilepsy. Clin Exp Neurol. 1987;23:139-44. [PubMed:3117456 ]
  5. Giarratano M, Standley K, Benbadis SR: Clobazam for treatment of epilepsy. Expert Opin Pharmacother. 2012 Feb;13(2):227-33. doi: 10.1517/14656566.2012.647686. Epub 2012 Jan 13. [PubMed:22242724 ]
  6. Yang LP, Scott LJ: Clobazam : in patients with Lennox-Gastaut syndrome. CNS Drugs. 2012 Nov;26(11):983-91. doi: 10.1007/s40263-012-0007-0. [PubMed:23034582 ]
  7. Walzer M, Bekersky I, Blum RA, Tolbert D: Pharmacokinetic drug interactions between clobazam and drugs metabolized by cytochrome P450 isoenzymes. Pharmacotherapy. 2012 Apr;32(4):340-53. doi: 10.1002/j.1875-9114.2012.01028.x. Epub 2012 Mar 15. [PubMed:22422635 ]
External Links
ATC CodesN05BA09
AHFS Codes
  • 28:24.08
PDB EntriesNot Available
FDA labelDownload (595 KB)
MSDSDownload (57.5 KB)
Interactions
Drug Interactions
Drug
AminophyllineThe therapeutic efficacy of Clobazam can be decreased when used in combination with Aminophylline.
AripiprazoleThe serum concentration of Aripiprazole can be decreased when it is combined with Clobazam.
AzelastineClobazam may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
BaclofenThe risk or severity of adverse effects can be increased when Baclofen is combined with Clobazam.
BortezomibThe metabolism of Clobazam can be decreased when combined with Bortezomib.
BrexpiprazoleThe serum concentration of Brexpiprazole can be increased when it is combined with Clobazam.
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Clobazam.
BuprenorphineClobazam may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
ChlorotrianiseneThe serum concentration of Chlorotrianisene can be decreased when it is combined with Clobazam.
ClozapineThe risk or severity of adverse effects can be increased when Clobazam is combined with Clozapine.
CodeineThe therapeutic efficacy of Codeine can be decreased when used in combination with Clobazam.
DabrafenibThe serum concentration of Clobazam can be decreased when it is combined with Dabrafenib.
DeferiproneThe serum concentration of Deferiprone can be increased when it is combined with Clobazam.
DienogestThe serum concentration of Dienogest can be decreased when it is combined with Clobazam.
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Clobazam.
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Clobazam.
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Clobazam.
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Clobazam.
DyphyllineThe therapeutic efficacy of Clobazam can be decreased when used in combination with Dyphylline.
EliglustatThe serum concentration of Eliglustat can be increased when it is combined with Clobazam.
EthanolEthanol may increase the central nervous system depressant (CNS depressant) activities of Clobazam.
EtonogestrelThe serum concentration of Etonogestrel can be decreased when it is combined with Clobazam.
FesoterodineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Clobazam.
FluvoxamineThe metabolism of Clobazam can be decreased when combined with Fluvoxamine.
FosphenytoinThe serum concentration of Fosphenytoin can be increased when it is combined with Clobazam.
Gamma Hydroxybutyric AcidClobazam may increase the central nervous system depressant (CNS depressant) activities of Gamma Hydroxybutyric Acid.
HydrocodoneClobazam may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Clobazam.
LevonorgestrelThe serum concentration of Levonorgestrel can be decreased when it is combined with Clobazam.
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Clobazam.
LuliconazoleThe serum concentration of Clobazam can be increased when it is combined with Luliconazole.
LumacaftorThe serum concentration of Clobazam can be decreased when it is combined with Lumacaftor.
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Clobazam.
Medroxyprogesterone acetateThe serum concentration of Medroxyprogesterone Acetate can be decreased when it is combined with Clobazam.
MefloquineThe therapeutic efficacy of Clobazam can be decreased when used in combination with Mefloquine.
MethadoneClobazam may increase the central nervous system depressant (CNS depressant) activities of Methadone.
MethotrimeprazineClobazam may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Clobazam.
MetyrosineClobazam may increase the sedative activities of Metyrosine.
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Clobazam.
MirtazapineClobazam may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Clobazam.
NebivololThe serum concentration of Nebivolol can be increased when it is combined with Clobazam.
NimodipineThe serum concentration of Nimodipine can be decreased when it is combined with Clobazam.
NorethisteroneThe serum concentration of Norethindrone can be decreased when it is combined with Clobazam.
OlanzapineThe risk or severity of adverse effects can be increased when Olanzapine is combined with Clobazam.
OrlistatThe serum concentration of Clobazam can be decreased when it is combined with Orlistat.
OrphenadrineClobazam may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
ParaldehydeClobazam may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
ParoxetineThe risk or severity of adverse effects can be increased when Clobazam is combined with Paroxetine.
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Clobazam.
PhenytoinThe serum concentration of Phenytoin can be increased when it is combined with Clobazam.
PramipexoleClobazam may increase the sedative activities of Pramipexole.
PropafenoneThe serum concentration of Clobazam can be increased when it is combined with Propafenone.
RopiniroleClobazam may increase the sedative activities of Ropinirole.
RotigotineClobazam may increase the sedative activities of Rotigotine.
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Clobazam.
SaxagliptinThe serum concentration of Saxagliptin can be decreased when it is combined with Clobazam.
Sodium oxybateClobazam may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
StiripentolThe serum concentration of Stiripentol can be increased when it is combined with Clobazam.
SuvorexantClobazam may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
TamoxifenThe serum concentration of the active metabolites of Tamoxifen can be reduced when Tamoxifen is used in combination with Clobazam resulting in a loss in efficacy.
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Clobazam.
TeduglutideThe serum concentration of Clobazam can be increased when it is combined with Teduglutide.
ThalidomideClobazam may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
TheophyllineThe therapeutic efficacy of Clobazam can be decreased when used in combination with Theophylline.
ThioridazineThe serum concentration of Thioridazine can be increased when it is combined with Clobazam.
TramadolThe therapeutic efficacy of Tramadol can be decreased when used in combination with Clobazam.
YohimbineThe therapeutic efficacy of Clobazam can be decreased when used in combination with Yohimbine.
ZolpidemClobazam may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Food Interactions
  • Alcohol increases clobazam absorption by 50%.
  • Take without regard to meals.

Targets

Kind
Protein group
Organism
Human
Pharmacological action
yes
Actions
positive allosteric modulator
General Function:
Inhibitory extracellular ligand-gated ion channel activity
Specific Function:
Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine. Functions as receptor for diazepines and various anesthetics, such as pentobarbital; these are bound at a separate allosteric effector binding site. Functions as ligand-gated chloride channel (By similarity).
Components:
NameUniProt IDDetails
Gamma-aminobutyric acid receptor subunit alpha-1P14867 Details
Gamma-aminobutyric acid receptor subunit alpha-2P47869 Details
Gamma-aminobutyric acid receptor subunit alpha-3P34903 Details
Gamma-aminobutyric acid receptor subunit alpha-4P48169 Details
Gamma-aminobutyric acid receptor subunit alpha-5P31644 Details
Gamma-aminobutyric acid receptor subunit alpha-6Q16445 Details
Gamma-aminobutyric acid receptor subunit beta-1P18505 Details
Gamma-aminobutyric acid receptor subunit beta-2P47870 Details
Gamma-aminobutyric acid receptor subunit beta-3P28472 Details
Gamma-aminobutyric acid receptor subunit deltaO14764 Details
Gamma-aminobutyric acid receptor subunit epsilonP78334 Details
Gamma-aminobutyric acid receptor subunit gamma-1Q8N1C3 Details
Gamma-aminobutyric acid receptor subunit gamma-2P18507 Details
Gamma-aminobutyric acid receptor subunit gamma-3Q99928 Details
Gamma-aminobutyric acid receptor subunit piO00591 Details
Gamma-aminobutyric acid receptor subunit thetaQ9UN88 Details
References
  1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090 ]
  2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [PubMed:18384456 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
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 imipramine.
Gene Name:
CYP2C19
Uniprot ID:
P33261
Molecular Weight:
55930.545 Da
References
  1. 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
substrate
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 reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. 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
substrate
General Function:
Steroid 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 oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Acts as a 1,4-cineole 2-exo-monooxygenase.
Gene Name:
CYP2B6
Uniprot ID:
P20813
Molecular Weight:
56277.81 Da
References
  1. 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
substrate
General Function:
Steroid 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 oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP2C18
Uniprot ID:
P33260
Molecular Weight:
55710.075 Da
References
  1. 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
inhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
Molecular Weight:
55768.94 Da

Transporters

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
Other
General Function:
Neurotransmitter:sodium symporter activity
Specific Function:
Terminates the action of GABA by its high affinity sodium-dependent reuptake into presynaptic terminals.
Gene Name:
SLC6A1
Uniprot ID:
P30531
Molecular Weight:
67073.0 Da
References
  1. Giarratano M, Standley K, Benbadis SR: Clobazam for treatment of epilepsy. Expert Opin Pharmacother. 2012 Feb;13(2):227-33. doi: 10.1517/14656566.2012.647686. Epub 2012 Jan 13. [PubMed:22242724 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
Other
General Function:
Neurotransmitter:sodium symporter activity
Specific Function:
Terminates the action of GABA by its high affinity sodium-dependent reuptake into presynaptic terminals.
Gene Name:
SLC6A11
Uniprot ID:
P48066
Molecular Weight:
70605.145 Da
References
  1. Giarratano M, Standley K, Benbadis SR: Clobazam for treatment of epilepsy. Expert Opin Pharmacother. 2012 Feb;13(2):227-33. doi: 10.1517/14656566.2012.647686. Epub 2012 Jan 13. [PubMed:22242724 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name:
ABCB1
Uniprot ID:
P08183
Molecular Weight:
141477.255 Da
Comments
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23