You are using an unsupported browser. Please upgrade your browser to a newer version to get the best experience on DrugBank.
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
CerebyxNot AvailableNot Available
FosfenitoinaSpanishINN
FosphenytoinNot AvailableNot Available
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 KeyXWLUWCNOOVRFPX-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
Not Available
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
BoceprevirStrong 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.

Targets

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

Enzymes

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

Carriers

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
comments powered by Disqus
Drug created on June 30, 2007 11:18 / Updated on September 16, 2013 17:14