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Identification
NameFosphenytoin
Accession NumberDB01320
Typesmall molecule
Groupsapproved
Description

Fosphenytoin is a water-soluble phenytoin prodrug used only in hospitals for the treatment of epileptic seizures. It works by slowing down impulses in the brain that cause seizures. Its main mechanism is to block frequency-dependent, use-dependent and voltage-dependent neuronal sodium channels, and therefore limit repetitive firing of action potentials.

Structure
Thumb
Synonyms
SynonymLanguageCode
(3-Phosphoryloxymethyl)phenytoinNot AvailableNot Available
FosfenitoinaSpanishINN
FosphenytoineFrenchINN
FosphenytoinumLatinINN
Salts
Name/CAS Structure Properties
Fosphenytoin sodium
Thumb
  • InChI Key: GQPXYJNXTAFDLT-UHFFFAOYSA-L
  • Monoisotopic Mass: 406.03066202
  • Average Mass: 406.2375
DBSALT000296
Brand names
NameCompany
CerebyxNot Available
ProdilantinNot Available
Brand mixturesNot Available
Categories
CAS number93390-81-9
WeightAverage: 362.2739
Monoisotopic: 362.066772734
Chemical FormulaC16H15N2O6P
InChI KeyInChIKey=XWLUWCNOOVRFPX-UHFFFAOYSA-N
InChI
InChI=1S/C16H15N2O6P/c19-14-16(12-7-3-1-4-8-12,13-9-5-2-6-10-13)17-15(20)18(14)11-24-25(21,22)23/h1-10H,11H2,(H,17,20)(H2,21,22,23)
IUPAC Name
[(2,5-dioxo-4,4-diphenylimidazolidin-1-yl)methoxy]phosphonic acid
SMILES
OP(O)(=O)OCN1C(=O)NC(C1=O)(C1=CC=CC=C1)C1=CC=CC=C1
Mass SpecNot Available
Taxonomy
KingdomOrganic Compounds
SuperclassHeterocyclic Compounds
ClassAzolidines
SubclassImidazolidines
Direct parentPhenylhydantoins
Alternative parentsDiphenylmethanes; Phenylimidazolidines; Ureides; Organic Phosphoric Acids; N-substituted Carboxylic Acid Imides; Organophosphate Esters; Tertiary Carboxylic Acid Amides; Tertiary Amines; Polyamines; Carboxylic Acids
Substituentsphenylimidazolidine; ureide; phosphoric acid ester; carboxylic acid imide, n-substituted; organic phosphate; benzene; tertiary carboxylic acid amide; tertiary amine; carboxamide group; polyamine; carboxylic acid derivative; carboxylic acid; amine; organonitrogen compound
Classification descriptionThis compound belongs to the phenylhydantoins. These are heterocyclic aromatic compounds containing an imiazolidinedione moiety substituted by a phenyl group.
Pharmacology
IndicationFor the control of generalized convulsive status epilepticus and prevention and treatment of seizures occurring during neurosurgery. It can also be substituted, short-term, for oral phenytoin.
PharmacodynamicsFosphenytoin is a water-soluble phenytoin prodrug used only in hospitals for the treatment of epileptic seizures. Following parenteral administration of fosphenytoin, fosphenytoin is converted to the anticonvulsant phenytoin by endogenous phosphatases. For every mmol of fosphenytoin administered, one mmol of phenytoin is produced. The pharmacological and toxicological effects of fosphenytoin include those of phenytoin.
Mechanism of actionFosphenytoin is a prodrug of phenytoin and accordingly, its anticonvulsant effects are attributable to phenytoin. Phenytoin acts on sodium channels on the neuronal cell membrane, limiting the spread of seizure activity and reducing seizure propagation. By promoting sodium efflux from neurons, phenytoin tends to stabilize the threshold against hyperexcitability caused by excessive stimulation or environmental changes capable of reducing membrane sodium gradient. This includes the reduction of post-tetanic potentiation at synapses. Loss of post-tetanic potentiation prevents cortical seizure foci from detonating adjacent cortical areas.
AbsorptionFosphenytoin is completely bioavailable following lM administration.
Volume of distribution
  • 4.3 to 10.8 L
Protein bindingExtensively bound (95% to 99%) to human plasma proteins, primarily albumin.
Metabolism

Hepatic.

SubstrateEnzymesProduct
Fosphenytoin
    PhenytoinDetails
    Route of eliminationPhenytoin derived from administration of Cerebyx is extensively metabolized in the liver and excreted in urine primarily as 5-(p-hydroxyphenyl)-5-phenylhydantoin and its glucuronide; little unchanged phenytoin (1%–5% of the Cerebyx dose) is recovered in urine.
    Half lifeFosphenytoin has a half-life of approximately 15 minutes.
    ClearanceNot Available
    ToxicityNausea, vomiting, lethargy, tachycardia, bradycardia, asystole, cardiac arrest, hypotension, syncope, hypocalcemia, metabolic acidosis, and death have been reported in cases of overdosage with fosphenytoin. The median lethal dose of fosphenytoin given intravenously in mice and rats was 156 mg PE/kg and approximately 250 mg PE/kg, or about 0.6 and 2 times, respectively, the maximum human loading dose on a mg/m2 basis. Signs of acute toxicity in animals included ataxia, labored breathing, ptosis, and hypoactivity.
    Affected organisms
    • Humans and other mammals
    Pathways
    PathwayCategorySMPDB ID
    Fosphenytoin (Antiarrhythmic) Action PathwayDrug actionSMP00326
    Fosphenytoin (Antiarrhythmic) Metabolism PathwayDrug metabolismSMP00618
    SNP Mediated EffectsNot Available
    SNP Mediated Adverse Drug ReactionsNot Available
    ADMET
    Predicted ADMET features
    Property Value Probability
    Human Intestinal Absorption - 0.5244
    Blood Brain Barrier + 0.9215
    Caco-2 permeable - 0.639
    P-glycoprotein substrate Substrate 0.5
    P-glycoprotein inhibitor I Non-inhibitor 0.7952
    P-glycoprotein inhibitor II Non-inhibitor 0.8466
    Renal organic cation transporter Non-inhibitor 0.8731
    CYP450 2C9 substrate Non-substrate 0.7094
    CYP450 2D6 substrate Non-substrate 0.9116
    CYP450 3A4 substrate Non-substrate 0.6873
    CYP450 1A2 substrate Non-inhibitor 0.8477
    CYP450 2C9 substrate Non-inhibitor 0.7802
    CYP450 2D6 substrate Non-inhibitor 0.8859
    CYP450 2C19 substrate Non-inhibitor 0.7169
    CYP450 3A4 substrate Non-inhibitor 0.7672
    CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.9083
    Ames test Non AMES toxic 0.614
    Carcinogenicity Non-carcinogens 0.7835
    Biodegradation Not ready biodegradable 0.9674
    Rat acute toxicity 2.4215 LD50, mol/kg Not applicable
    hERG inhibition (predictor I) Weak inhibitor 0.9578
    hERG inhibition (predictor II) Non-inhibitor 0.7299
    Pharmacoeconomics
    Manufacturers
    • Parke davis div warner lambert co
    • Akorn strides llc
    • Apotex inc richmond hill
    • App pharmaceuticals llc
    • Baxter healthcare corp anesthesia and critical care
    • Bedford laboratories div ben venue laboratories inc
    • Hikma farmaceutica (portugal) sa
    • Hospira inc
    • Luitpold pharmaceuticals inc
    • Pharmaforce inc
    • Strides arcolab limited
    • Sun pharma global inc
    • Teva parenteral medicines inc
    • Wockhardt ltd
    Packagers
    Dosage forms
    FormRouteStrength
    LiquidIntravenous
    LiquidIntravenous
    Prices
    Unit descriptionCostUnit
    Cerebyx 500 mg pe/10 ml vial8.63USDml
    Fosphenytoin 500 mg pe/10 ml0.61USDml
    DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
    PatentsNot Available
    Properties
    Statesolid
    Experimental PropertiesNot Available
    Predicted Properties
    PropertyValueSource
    water solubility1.45e-01 g/lALOGPS
    logP1.08ALOGPS
    logP1.67ChemAxon
    logS-3.4ALOGPS
    pKa (strongest acidic)1.46ChemAxon
    pKa (strongest basic)-9.7ChemAxon
    physiological charge-2ChemAxon
    hydrogen acceptor count5ChemAxon
    hydrogen donor count3ChemAxon
    polar surface area116.17ChemAxon
    rotatable bond count5ChemAxon
    refractivity87.05ChemAxon
    polarizability33.23ChemAxon
    number of rings3ChemAxon
    bioavailability1ChemAxon
    rule of fiveYesChemAxon
    Ghose filterYesChemAxon
    Veber's ruleNoChemAxon
    MDDR-like ruleNoChemAxon
    Spectra
    SpectraNot Available
    References
    Synthesis Reference

    Volker Kirsch, “Process for the preparation of sodium fosphenytoin.” U.S. Patent US20050272706, issued December 08, 2005.

    US20050272706
    General Reference
    1. Johnson J, Wrenn K: Inappropriate fosphenytoin use in the ED. Am J Emerg Med. 2001 Jul;19(4):293-4. Pubmed
    2. Applebaum J, Levine J, Belmaker RH: Intravenous fosphenytoin in acute mania. J Clin Psychiatry. 2003 Apr;64(4):408-9. Pubmed
    3. McCleane GJ: Intravenous infusion of fosphenytoin produces prolonged pain relief: a case report. J Pain. 2002 Apr;3(2):156-8. Pubmed
    4. Browne TR, Kugler AR, Eldon MA: Pharmacology and pharmacokinetics of fosphenytoin. Neurology. 1996 Jun;46(6 Suppl 1):S3-7. Pubmed 8649612
    5. Luszczki JJ: Third-generation antiepileptic drugs: mechanisms of action, pharmacokinetics and interactions. Pharmacol Rep. 2009 Mar-Apr;61(2):197-216. Pubmed
    External Links
    ResourceLink
    KEGG CompoundC07840
    PubChem Compound56339
    PubChem Substance46505168
    ChemSpider50839
    Therapeutic Targets DatabaseDAP000520
    PharmGKBPA164746820
    Drug Product Database2230988
    RxListhttp://www.rxlist.com/cgi/generic/fosphen.htm
    Drugs.comhttp://www.drugs.com/cdi/fosphenytoin.html
    WikipediaFosphenytoin
    ATC CodesNot Available
    AHFS Codes
    • 28:12.12
    PDB EntriesNot Available
    FDA labelshow(820 KB)
    MSDSNot Available
    Interactions
    Drug Interactions
    Drug
    AcenocoumarolIncreased hydantoin levels and risk of bleeding
    AlprazolamFosphenytoin may increase the metabolism of alprazolam via CYP3A4.
    AminophyllineDecreased effect of both products
    AmiodaroneAmiodarone may increase the effect of fosphenytoin.
    AnisindioneIncreased hydantoin levels and risk of bleeding
    AprepitantThe CYP3A4 inducer, fosphenytoin, may decrease the effect of aprepitant.
    AtracuriumPhenytoin decreases the effect of muscle relaxant
    BetamethasoneThe enzyme inducer, fosphenytoin, may decrease the effect of the corticosteroid, betamethasone.
    BleomycinThe antineoplasic agent decreases the effect of hydantoin
    Boceprevir Strong CYP3A4 inducers will decrease levels of boceprevir. Concomitant therapy is contraindicated.
    CapecitabineCapecitabine increases the effect of hydantoin
    CarboplatinThe antineoplasic agent decreases the effect of hydantoin
    CarmustineThe antineoplasic agent decreases the effect of hydantoin
    ChloramphenicolIncreases phenytoin, modifies chloramphenicol
    ChlordiazepoxideFosphenytoin may increase the metabolism of chlordiazepoxide via CYP3A4.
    ChlorotrianiseneThe enzyme inducer, fosphenytoin, decreases the effect of the hormone agent, chlorotrianisene.
    ChlorphenamineThe antihistamine increases the effect of hydantoin
    CimetidineCimetidine may increase the serum concentration of fosphenytoin by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of fosphenytoin if cimetidine is initiated, discontinued or dose changed.
    CisplatinThe antineoplasic agent decreases the effect of hydantoin
    ClarithromycinClarithromycin may increase the therapeutic and adverse effects of fosphenytoin.
    ClomifeneThe enzyme inducer, fosphenytoin, decreases the effect of the hormone agent, clomifene.
    ClorazepateFosphenytoin may increase the metabolism of clorazepate via CYP3A4.
    ClozapineHydantoin decreases the effect of clozapine
    Conjugated EstrogensThe enzyme inducer, fosphenytoin, decreases the effect of the hormone agent, conjugated estrogens.
    Cortisone acetateThe enzyme inducer, fosphenytoin, may decrease the effect of the corticosteroid, cortisone acetate.
    CyclosporineThe hydantoin decreases the effect of cyclosporine
    DelavirdineThe anticonvulsant, fosphenytoin, decreases the effect of delavirdine.
    DexamethasoneThe enzyme inducer, fosphenytoin, may decrease the effect of the corticosteroid, dexamethasone.
    DiazepamFosphenytoin may increase the metabolism of diazepam via CYP3A4.
    DiazoxideDiazoxide decreases the hydantoin effect
    DicoumarolIncreased hydantoin levels and risk of bleeding
    DiethylstilbestrolThe enzyme inducer, fosphenytoin, may decrease the therapeutic effect of diethylstilbestrol.
    DisopyramideThe hydantoin decreases the effect of disopyramide
    DisulfiramDisulfiram may increase the effect of fosphenytoin.
    DopamineRisk of severe hypotension
    Doxacurium chloridePhenytoin decreases the effect of muscle relaxant
    DoxycyclineThe anticonvulsant, fosphenytoin, decreases the effect of doxycycline.
    DyphyllineDecreased effect of both products
    EstradiolThe enzyme inducer, fosphenytoin, decreases the effect of the hormone agent, estradiol.
    Estradiol valerate/DienogestAffects CYP3A4 metabolism, decreases or effects levels of Estradiol valerate/Dienogest.
    EstriolThe enzyme inducer, fosphenytoin, decreases the effect of the hormone agent, estriol.
    EstroneThe enzyme inducer, fosphenytoin, decreases the effect of the hormone agent, estrone.
    EstropipateThe enzyme inducer, fosphenytoin, decreases the effect of the hormone agent, estropipate.
    Ethinyl EstradiolThis product may cause a slight decrease of contraceptive effect
    EtravirineEtravirine, when administered concomitantly with fosphenytoin, may experience a decrease in serum concentration. It is recommended to avoid this combination.
    FelbamateIncreased phenytoin levels and decreased felbamate levels
    FelodipineThe hydantoin decreases the effect of felodipine
    FluconazoleFluconazole may increase the effect of hydantoin.
    FludrocortisoneThe enzyme inducer, fosphenytoin, may decrease the effect of the corticosteroid, fludrocortisone.
    FluorouracilFluorouracil increases the effect of hydantoin
    FluoxetineFluoxetine increases the effect of phenytoin
    FlurazepamFosphenytoin may increase the metabolism of flurazepam via CYP3A4.
    FluvoxamineFluvoxamine may increase the therapeutic and adverse effects of fosphenytoin.
    Folic AcidFolic acid decreases the levels of hydantoin
    FurosemideThe hydantoin decreases the effect of furosemide
    GabapentinGabapentin may increase the effect of fosphenytoin.
    GefitinibThe CYP3A4 inducer, fosphenytoin, may decrease the serum concentration and therapeutic effects of gefitinib.
    HydrocortisoneThe enzyme inducer, fosphenytoin, may decrease the effect of the corticosteroid, hydrocortisone.
    ImatinibThe hydantoin decreases the levels of imatinib
    IrinotecanThe hydantoin decreases the effect of irinotecan
    IsoniazidIsoniazid may increase the effect of phenytoin in 20% of patients.
    ItraconazolePhenytoin decreases the effect of itraconazole
    L-DOPAThe hydantoin decreases the effect of levodopa
    LamotriginePhenytoin may reduce levels of lamotrigine
    LevonorgestrelPhenytoin decreases the contraceptive effect
    LopinavirLevels of both drugs are affected
    LurasidoneConcomitant therapy with a CYP3A4 inducer will decrease levels of lurasidone. Coadministration with lurasidone is contraindicated.
    MebendazoleThe hydantoin decreases the efficiency of mebendazole
    Medroxyprogesterone AcetateThe enzyme inducer, fosphenytoin, may decrease the effect of the hormone, medroxyprogesterone.
    Megestrol acetateThe enzyme inducer, fosphenytoin, may decrease the effect of the hormone, megestrol.
    MestranolThis product may cause a slight decrease of contraceptive effect
    MethadoneThe hydantoin decreases the effect of methadone
    MethotrexateThe antineoplasic agent decreases the effect of hydantoin
    MethoxsalenThe hydantoin decreases the effect of psoralene
    MethylprednisoloneThe enzyme inducer, fosphenytoin, may decrease the effect of the corticosteroid, methylprednisolone.
    MetocurinePhenytoin decreases the effect of muscle relaxant
    MetyraponeThe combination renders the test invalid
    MexiletineThe hydantoin decreases the effect of mexiletine
    MidazolamFosphenytoin may increase the metabolism of midazolam via CYP3A4.
    MirtazapineThe hydantoins may reduce mirtazapine plasma concentrations and pharmacological effects
    MivacuriumPhenytoin decreases the effect of muscle relaxant
    NisoldipinePhenytoin decreases the efficiency of nisoldipine
    NorethindroneThis product may cause a slight decrease of contraceptive effect
    OmeprazoleOmeprazole increases the effect of hydantoin
    OxcarbazepineOxcarbazepine increases the effect of hydantoin
    OxtriphyllineDecreased effect of both products
    OxyphenbutazoneThe NSAID, oxphenbutazone, may increase the hydantoin effect of fosphenytoin.
    PancuroniumPhenytoin decreases the effect of muscle relaxant
    ParamethasoneThe enzyme inducer, fosphenytoin, may decrease the effect of the corticosteroid, paramethasone.
    PhenylbutazoneThe NSAID, phenylbutazone, may increase the hydantoin effect of fosphenytoin.
    PosaconazoleModifications of drug levels for both agents
    PrednisoloneThe enzyme inducer, fosphenytoin, may decrease the effect of the corticosteroid, prednisolone.
    PrednisoneThe enzyme inducer, fosphenytoin, may decrease the effect of the corticosteroid, prednisone.
    QuetiapinePhenytoin decreases the effect of quetiapine
    QuinestrolThe enzyme inducer, fosphenytoin, decreases the effect of the hormone agent, quinestrol.
    QuinidineThe anticonvulsant, fosphenytoin, decreases the effect of quinidine.
    QuinupristinThis combination presents an increased risk of toxicity
    RifampicinRifampin may decrease the effect of fosphenytoin.
    RoflumilastAffects CYP3A4 metabolism, decreases level or effect of roflumilast.
    SertralineSertraline increases the effect of hydantoin
    SirolimusThe hydantoin decreases sirolimus levels
    SucralfateSucralfate decreases the effect of hydantoin
    SulfadiazineThe sulfonamide increases the effect of hydantoin
    SulfamethizoleThe sulfonamide increases the effect of hydantoin
    TacrolimusThe hydantoin decreases the effect of tacrolimus
    TelithromycinFosphenytoin may decrease the plasma concentration of Telithromycin. Consider alternate therapy.
    TemsirolimusFosphenytoin may increase the metabolism of Temsirolimus decreasing its efficacy. Concomitant therapy should be avoided.
    TheophyllineDecreased effect of both products
    ThiotepaPossible increase in thiotepa levels
    TiclopidineTiclopidine may decrease the metabolism and clearance of Fosphenytoin. Consider alternate therapy or monitor for adverse/toxic effects of Fosphenytoin if Ticlopidine is initiated, discontinued or dose changed.
    TolbutamideTolbutamide, a strong CYP2C9 inhibitor, may decrease the metabolism and clearance of Fosphenytoin. Consider alternate therapy or monitor for changes in Fosphenytoin therapeutic and adverse effects if Tolbutamide is initiated, discontinued or dose changed.
    TopiramateIncreased phenytoin/decreased topiramate
    TramadolFosphenytoin may decrease the effect of Tramadol by increasing Tramadol metabolism and clearance.
    TrazodoneThe CYP3A4 inducer, Fosphenytoin, may decrease Trazodone efficacy by increasing Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Fosphenytoin is initiated, discontinued or dose changed.
    TretinoinThe strong CYP2C8 inducer, Fosphenytoin, may increase the metabolism and clearance of oral Tretinoin. Consider alternate therapy to avoid failure of Tretinoin therapy or monitor for changes in Tretinoin effectiveness and adverse/toxic effects if Fosphenytoin is initiated, discontinued or dose changed.
    TriamcinoloneThe enzyme inducer, fosphenytoin, may decrease the effect of the corticosteroid, triamcinolone.
    TriazolamFosphenytoin may increase the metabolism of triazolam via CYP3A4.
    TrimethoprimTrimethoprim increases the effect of hydantoin
    TrioxsalenThe hydantoin decreases the effect of psoralene
    TriprolidineThe CNS depressants, Triprolidine and Fosphenytoin, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
    TubocurarinePhenytoin decreases the effect of muscle relaxant
    VandetanibDecreases levels of vandetanib by affecting CYP3A4 metabolism. Contraindicated.
    VecuroniumPhenytoin decreases the effect of muscle relaxant
    VigabatrinVigabatrin decreases the effect of hydantoin
    VinblastineThe antineoplasic agent decreases the effect of hydantoin
    VoriconazoleThe hydantoin decreases the effect of voriconazole
    WarfarinIncreased hydantoin levels and risk of bleeding
    Food Interactions
    • Avoid alcohol.
    • Do not take calcium, aluminum, magnesium or Iron supplements within 2 hours of taking this medication.
    • Take with food.

    1. Sodium channel protein type 5 subunit alpha

    Kind: protein

    Organism: Human

    Pharmacological action: yes

    Actions: inhibitor

    Components

    Name UniProt ID Details
    Sodium channel protein type 5 subunit alpha Q14524 Details

    References:

    1. Swadron SP, Rudis MI, Azimian K, Beringer P, Fort D, Orlinsky M: A comparison of phenytoin-loading techniques in the emergency department. Acad Emerg Med. 2004 Mar;11(3):244-52. Pubmed
    2. Mantegazza M, Curia G, Biagini G, Ragsdale DS, Avoli M: Voltage-gated sodium channels as therapeutic targets in epilepsy and other neurological disorders. Lancet Neurol. 2010 Apr;9(4):413-24. Pubmed
    3. Lenkowski PW, Ko SH, Anderson JD, Brown ML, Patel MK: Block of human NaV1.5 sodium channels by novel alpha-hydroxyphenylamide analogues of phenytoin. Eur J Pharm Sci. 2004 Apr;21(5):635-44. Pubmed
    4. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed

    1. Cytochrome P450 2C9

    Kind: protein

    Organism: Human

    Pharmacological action: unknown

    Actions: substrate inducer

    Components

    Name UniProt ID Details
    Cytochrome P450 2C9 P11712 Details

    References:

    1. Sahi J, Shord SS, Lindley C, Ferguson S, LeCluyse EL: Regulation of cytochrome P450 2C9 expression in primary cultures of human hepatocytes. J Biochem Mol Toxicol. 2009 Jan-Feb;23(1):43-58. Pubmed
    2. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. Pubmed
    3. Goldstein JA: Clinical relevance of genetic polymorphisms in the human CYP2C subfamily. Br J Clin Pharmacol. 2001 Oct;52(4):349-55. Pubmed
    4. Klotz U: The role of pharmacogenetics in the metabolism of antiepileptic drugs: pharmacokinetic and therapeutic implications. Clin Pharmacokinet. 2007;46(4):271-9. Pubmed

    2. Cytochrome P450 2C8

    Kind: protein

    Organism: Human

    Pharmacological action: unknown

    Actions: substrate inducer

    Components

    Name UniProt ID Details
    Cytochrome P450 2C8 P10632 Details

    References:

    1. Kim KA, Park JY: Inhibitory effect of glyburide on human cytochrome p450 isoforms in human liver microsomes. Drug Metab Dispos. 2003 Sep;31(9):1090-2. Pubmed

    3. Cytochrome P450 2C19

    Kind: protein

    Organism: Human

    Pharmacological action: unknown

    Actions: substrate inducer

    Components

    Name UniProt ID Details
    Cytochrome P450 2C19 P33261 Details

    References:

    1. Anderson GD: Pharmacokinetic, pharmacodynamic, and pharmacogenetic targeted therapy of antiepileptic drugs. Ther Drug Monit. 2008 Apr;30(2):173-80. Pubmed
    2. Hennessy S, Leonard CE, Freeman CP, Metlay JP, Chu X, Strom BL, Bilker WB: CYP2C9, CYP2C19, and ABCB1 genotype and hospitalization for phenytoin toxicity. J Clin Pharmacol. 2009 Dec;49(12):1483-7. Epub 2009 Jul 17. Pubmed
    3. Klotz U: The role of pharmacogenetics in the metabolism of antiepileptic drugs: pharmacokinetic and therapeutic implications. Clin Pharmacokinet. 2007;46(4):271-9. Pubmed

    4. Cytochrome P450 3A4

    Kind: protein

    Organism: Human

    Pharmacological action: unknown

    Actions: inducer

    Components

    Name UniProt ID Details
    Cytochrome P450 3A4 P08684 Details

    References:

    1. Zhou SF: Drugs behave as substrates, inhibitors and inducers of human cytochrome P450 3A4. Curr Drug Metab. 2008 May;9(4):310-22. Pubmed

    5. Cytochrome P450 2B6

    Kind: protein

    Organism: Human

    Pharmacological action: unknown

    Actions: inducer

    Components

    Name UniProt ID Details
    Cytochrome P450 2B6 P20813 Details

    References:

    1. Wang H, Faucette S, Moore R, Sueyoshi T, Negishi M, LeCluyse E: Human constitutive androstane receptor mediates induction of CYP2B6 gene expression by phenytoin. J Biol Chem. 2004 Jul 9;279(28):29295-301. Epub 2004 Apr 28. Pubmed
    2. Faucette SR, Wang H, Hamilton GA, Jolley SL, Gilbert D, Lindley C, Yan B, Negishi M, LeCluyse EL: Regulation of CYP2B6 in primary human hepatocytes by prototypical inducers. Drug Metab Dispos. 2004 Mar;32(3):348-58. Pubmed

    1. Serum albumin

    Kind: protein

    Organism: Human

    Pharmacological action: no

    Actions: other/unknown

    Components

    Name UniProt ID Details
    Serum albumin P02768 Details

    References:

    1. Walker MC, Patsalos PN: Clinical pharmacokinetics of new antiepileptic drugs. Pharmacol Ther. 1995;67(3):351-84. Pubmed

    Comments
    Drug created on June 30, 2007 11:18 / Updated on September 16, 2013 17:14