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
(3-Phosphoryloxymethyl)phenytoin
Cerebyx
Fosfenitoina
Fosphenytoin
Fosphenytoine
Fosphenytoinum
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Cerebyxinjection, solution50 mg/mLintramuscular; intravenousPfizer Laboratories2013-10-28Not applicableUs
Cerebyxliquid75 mgintramuscular; intravenousErfa Canada 2012 Inc2000-03-01Not applicableCanada
Cerebyxinjection, solution50 mg/mLintramuscular; intravenousPfizer Laboratories2013-10-28Not applicableUs
Cerebyxinjection, solution50 mg/mLintramuscular; intravenousPfizer Laboratories2013-10-28Not applicableUs
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Fosphenytoininjection, solution50 mg/mLintramuscular; intravenousFresenius Kabi USA, LLC2009-12-14Not applicableUs
Fosphenytoin Sodiuminjection, solution50 mg/mLintramuscular; intravenousWest ward Pharmaceutical Corp2009-12-02Not applicableUs
Fosphenytoin Sodiuminjection, solution50 mg/mLintramuscular; intravenousGenera Medix Inc.2007-08-06Not applicableUs
Fosphenytoin Sodiuminjection50 mg/mLintramuscular; intravenousWest Ward Pharmaceutical Corp.2007-08-06Not applicableUs
Fosphenytoin Sodiuminjection50 mg/mLintramuscular; intravenousAmneal Pharmaceuticals of New York, LLC2013-05-17Not applicableUs
Fosphenytoin Sodiuminjection50 mg/mLintramuscular; intravenousWest Ward Pharmaceutical Corp.2007-08-06Not applicableUs
Fosphenytoin Sodiuminjection50 mg/mLintramuscular; intravenousAmneal Pharmaceuticals of New York, LLC2013-05-17Not applicableUs
Fosphenytoin Sodiuminjection, solution50 mg/mLintramuscular; intravenousAmerican Regent, Inc.2010-07-30Not applicableUs
Fosphenytoin Sodiuminjection, solution50 mg/mLintramuscular; intravenousHospira, Inc.2007-08-06Not applicableUs
Fosphenytoin Sodiuminjection, solution50 mg/mLintramuscular; intravenousSun Pharma Global FZE2009-08-14Not applicableUs
Fosphenytoin Sodiuminjection, solution50 mg/mLintramuscular; intravascularWest ward Pharmaceutical Corp2009-12-02Not applicableUs
Fosphenytoin Sodiuminjection, solution50 mg/mLintramuscular; intravenousSun Pharma Global FZE2009-08-14Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
ProdilantinNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Fosphenytoin sodium
Thumb
  • InChI Key: GQPXYJNXTAFDLT-UHFFFAOYSA-L
  • Monoisotopic Mass: 406.03066202
  • Average Mass: 406.2375
DBSALT000296
Categories
UNIIB4SF212641
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
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as phenylhydantoins. These are heterocyclic aromatic compounds containing an imiazolidinedione moiety substituted by a phenyl group.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassAzolidines
Sub ClassImidazolidines
Direct ParentPhenylhydantoins
Alternative Parents
Substituents
  • 5-phenylhydantoin
  • Diphenylmethane
  • Phenylimidazolidine
  • Monoalkyl phosphate
  • Ureide
  • Benzenoid
  • Alkyl phosphate
  • Phosphoric acid ester
  • Organic phosphoric acid derivative
  • Organic phosphate
  • Monocyclic benzene moiety
  • Urea
  • Tertiary amine
  • Carboxamide group
  • Azacycle
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Amine
  • Aromatic heteromonocyclic compound
Molecular FrameworkAromatic heteromonocyclic compounds
External DescriptorsNot Available
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.
Related Articles
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
PropertyValueProbability
Human Intestinal Absorption-0.5244
Blood Brain Barrier+0.9215
Caco-2 permeable-0.639
P-glycoprotein substrateSubstrate0.5
P-glycoprotein inhibitor INon-inhibitor0.7952
P-glycoprotein inhibitor IINon-inhibitor0.8466
Renal organic cation transporterNon-inhibitor0.8731
CYP450 2C9 substrateNon-substrate0.7094
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateNon-substrate0.6873
CYP450 1A2 substrateNon-inhibitor0.8477
CYP450 2C9 inhibitorNon-inhibitor0.7802
CYP450 2D6 inhibitorNon-inhibitor0.8859
CYP450 2C19 inhibitorNon-inhibitor0.7169
CYP450 3A4 inhibitorNon-inhibitor0.7672
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9083
Ames testNon AMES toxic0.614
CarcinogenicityNon-carcinogens0.7835
BiodegradationNot ready biodegradable0.9674
Rat acute toxicity2.4215 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9578
hERG inhibition (predictor II)Non-inhibitor0.7299
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Injection, solutionintramuscular; intravenous50 mg/mL
Liquidintramuscular; intravenous75 mg
Injectionintramuscular; intravenous50 mg/mL
Injection, solutionintramuscular; intravascular50 mg/mL
Prices
Unit descriptionCostUnit
Cerebyx 500 mg pe/10 ml vial8.63USD ml
Fosphenytoin 500 mg pe/10 ml0.61USD ml
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 Solubility0.145 mg/mLALOGPS
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 Area116.17 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity87.05 m3·mol-1ChemAxon
Polarizability33.23 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
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
References
Synthesis Reference

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

US20050272706
General References
  1. Johnson J, Wrenn K: Inappropriate fosphenytoin use in the ED. Am J Emerg Med. 2001 Jul;19(4):293-4. [PubMed:11447516 ]
  2. Applebaum J, Levine J, Belmaker RH: Intravenous fosphenytoin in acute mania. J Clin Psychiatry. 2003 Apr;64(4):408-9. [PubMed:12716241 ]
  3. McCleane GJ: Intravenous infusion of fosphenytoin produces prolonged pain relief: a case report. J Pain. 2002 Apr;3(2):156-8. [PubMed:14622802 ]
  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:19443931 ]
External Links
ATC CodesN03AB05
AHFS Codes
  • 28:12.12
PDB EntriesNot Available
FDA labelDownload (820 KB)
MSDSNot Available
Interactions
Drug Interactions
Drug
AbirateroneThe serum concentration of Abiraterone can be decreased when it is combined with Fosphenytoin.
AcenocoumarolFosphenytoin may increase the anticoagulant activities of Acenocoumarol.
AcetaminophenThe serum concentration of Acetaminophen can be decreased when it is combined with Fosphenytoin.
AcetazolamideThe risk or severity of adverse effects can be increased when Acetazolamide is combined with Fosphenytoin.
AfatinibThe serum concentration of Afatinib can be decreased when it is combined with Fosphenytoin.
AlprazolamThe serum concentration of Fosphenytoin can be increased when it is combined with Alprazolam.
AminophyllineThe serum concentration of Aminophylline can be decreased when it is combined with Fosphenytoin.
AmiodaroneFosphenytoin may increase the QTc-prolonging activities of Amiodarone.
AmlodipineThe serum concentration of Fosphenytoin can be increased when it is combined with Amlodipine.
AmrinoneThe serum concentration of Fosphenytoin can be increased when it is combined with Amrinone.
ApixabanThe serum concentration of Apixaban can be decreased when it is combined with Fosphenytoin.
ApremilastThe serum concentration of Apremilast can be decreased when it is combined with Fosphenytoin.
AripiprazoleThe serum concentration of Aripiprazole can be decreased when it is combined with Fosphenytoin.
ArtemetherThe serum concentration of the active metabolites of Artemether can be reduced when Artemether is used in combination with Fosphenytoin resulting in a loss in efficacy.
AtorvastatinThe serum concentration of Atorvastatin can be decreased when it is combined with Fosphenytoin.
Atracurium besylateFosphenytoin may decrease the neuromuscular blocking activities of Atracurium besylate.
AxitinibThe serum concentration of Axitinib can be decreased when it is combined with Fosphenytoin.
AzelastineFosphenytoin 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 Fosphenytoin.
BazedoxifeneThe serum concentration of Bazedoxifene can be decreased when it is combined with Fosphenytoin.
BedaquilineThe serum concentration of Bedaquiline can be decreased when it is combined with Fosphenytoin.
BepridilThe serum concentration of Fosphenytoin can be increased when it is combined with Bepridil.
BoceprevirThe serum concentration of Boceprevir can be decreased when it is combined with Fosphenytoin.
BortezomibThe serum concentration of Bortezomib can be decreased when it is combined with Fosphenytoin.
BosutinibThe serum concentration of Bosutinib can be decreased when it is combined with Fosphenytoin.
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be decreased when it is combined with Fosphenytoin.
BrexpiprazoleThe serum concentration of Brexpiprazole can be decreased when it is combined with Fosphenytoin.
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Fosphenytoin.
BromazepamThe serum concentration of Fosphenytoin can be increased when it is combined with Bromazepam.
BumetanideFosphenytoin may decrease the diuretic activities of Bumetanide.
BuprenorphineFosphenytoin may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
BusulfanThe serum concentration of Busulfan can be decreased when it is combined with Fosphenytoin.
CabozantinibThe serum concentration of Cabozantinib can be decreased when it is combined with Fosphenytoin.
CamazepamThe serum concentration of Fosphenytoin can be increased when it is combined with Camazepam.
CanagliflozinThe serum concentration of Canagliflozin can be decreased when it is combined with Fosphenytoin.
CannabidiolThe serum concentration of Cannabidiol can be decreased when it is combined with Fosphenytoin.
CapecitabineThe serum concentration of Fosphenytoin can be increased when it is combined with Capecitabine.
CarbamazepineThe serum concentration of Carbamazepine can be decreased when it is combined with Fosphenytoin.
CefazolinThe protein binding of Fosphenytoin can be decreased when combined with Cefazolin.
CeritinibThe serum concentration of Ceritinib can be decreased when it is combined with Fosphenytoin.
ChlordiazepoxideThe serum concentration of Fosphenytoin can be increased when it is combined with Chlordiazepoxide.
ChlormezanoneThe serum concentration of Fosphenytoin can be increased when it is combined with Chlormezanone.
ChlorotrianiseneThe therapeutic efficacy of Chlorotrianisene can be decreased when used in combination with Fosphenytoin.
ChlorphenamineThe serum concentration of Fosphenytoin can be increased when it is combined with Chlorphenamine.
CimetidineThe risk or severity of adverse effects can be increased when Cimetidine is combined with Fosphenytoin.
CinolazepamThe serum concentration of Fosphenytoin can be increased when it is combined with Cinolazepam.
CiprofloxacinFosphenytoin may increase the QTc-prolonging activities of Ciprofloxacin.
CisplatinThe serum concentration of Fosphenytoin can be decreased when it is combined with Cisplatin.
CitalopramFosphenytoin may increase the QTc-prolonging activities of Citalopram.
ClarithromycinThe serum concentration of the active metabolites of Clarithromycin can be increased when Clarithromycin is used in combination with Fosphenytoin.
ClobazamThe serum concentration of Fosphenytoin can be increased when it is combined with Clobazam.
ClonazepamThe serum concentration of Fosphenytoin can be increased when it is combined with Clonazepam.
ClotiazepamThe serum concentration of Fosphenytoin can be increased when it is combined with Clotiazepam.
CloxazolamThe serum concentration of Fosphenytoin can be increased when it is combined with Cloxazolam.
ClozapineThe serum concentration of Clozapine can be decreased when it is combined with Fosphenytoin.
CobicistatThe serum concentration of Cobicistat can be decreased when it is combined with Fosphenytoin.
CrizotinibThe serum concentration of Crizotinib can be decreased when it is combined with Fosphenytoin.
CyclosporineThe serum concentration of Cyclosporine can be decreased when it is combined with Fosphenytoin.
Dabigatran etexilateThe serum concentration of Dabigatran etexilate can be decreased when it is combined with Fosphenytoin.
DabrafenibThe serum concentration of Fosphenytoin can be decreased when it is combined with Dabrafenib.
DaclatasvirThe serum concentration of Daclatasvir can be decreased when it is combined with Fosphenytoin.
DarunavirThe serum concentration of Darunavir can be decreased when it is combined with Fosphenytoin.
DasatinibThe serum concentration of Dasatinib can be decreased when it is combined with Fosphenytoin.
DeferasiroxThe serum concentration of Deferasirox can be decreased when it is combined with Fosphenytoin.
DelavirdineThe serum concentration of Delavirdine can be decreased when it is combined with Fosphenytoin.
DexamethasoneThe serum concentration of Dexamethasone can be decreased when it is combined with Fosphenytoin.
DexketoprofenThe risk or severity of adverse effects can be increased when Dexketoprofen is combined with Fosphenytoin.
DexmethylphenidateThe serum concentration of Fosphenytoin can be increased when it is combined with Dexmethylphenidate.
DiazoxideThe serum concentration of Fosphenytoin can be decreased when it is combined with Diazoxide.
DiclofenacThe serum concentration of Diclofenac can be decreased when it is combined with Fosphenytoin.
DiclofenamideThe risk or severity of adverse effects can be increased when Diclofenamide is combined with Fosphenytoin.
DicoumarolFosphenytoin may increase the anticoagulant activities of Dicoumarol.
DienogestThe serum concentration of Dienogest can be decreased when it is combined with Fosphenytoin.
DiltiazemThe serum concentration of Fosphenytoin can be increased when it is combined with Diltiazem.
DisopyramideDisopyramide may increase the QTc-prolonging activities of Fosphenytoin.
DisulfiramThe serum concentration of Fosphenytoin can be increased when it is combined with Disulfiram.
DofetilideFosphenytoin may increase the QTc-prolonging activities of Dofetilide.
DolutegravirThe serum concentration of Dolutegravir can be decreased when it is combined with Fosphenytoin.
DoxofyllineThe serum concentration of Doxofylline can be decreased when it is combined with Fosphenytoin.
DoxorubicinThe serum concentration of Doxorubicin can be decreased when it is combined with Fosphenytoin.
DoxycyclineThe serum concentration of Doxycycline can be decreased when it is combined with Fosphenytoin.
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Fosphenytoin.
DronabinolThe serum concentration of Dronabinol can be decreased when it is combined with Fosphenytoin.
DronedaroneThe serum concentration of Dronedarone can be decreased when it is combined with Fosphenytoin.
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Fosphenytoin.
EfavirenzThe serum concentration of Efavirenz can be decreased when it is combined with Fosphenytoin.
EliglustatThe serum concentration of Eliglustat can be decreased when it is combined with Fosphenytoin.
ElvitegravirThe serum concentration of Elvitegravir can be decreased when it is combined with Fosphenytoin.
EnzalutamideThe serum concentration of Enzalutamide can be decreased when it is combined with Fosphenytoin.
ErlotinibThe serum concentration of Erlotinib can be decreased when it is combined with Fosphenytoin.
Eslicarbazepine acetateThe serum concentration of Eslicarbazepine acetate can be decreased when it is combined with Fosphenytoin.
EstazolamThe serum concentration of Fosphenytoin can be increased when it is combined with Estazolam.
Etacrynic acidFosphenytoin may decrease the diuretic activities of Ethacrynic acid.
EthanolEthanol may increase the central nervous system depressant (CNS depressant) activities of Fosphenytoin.
EthosuximideEthosuximide may increase the central nervous system depressant (CNS depressant) activities of Fosphenytoin.
EthoxzolamideThe risk or severity of adverse effects can be increased when Ethoxzolamide is combined with Fosphenytoin.
EtonogestrelThe therapeutic efficacy of Etonogestrel can be decreased when used in combination with Fosphenytoin.
EtoposideThe serum concentration of Etoposide can be decreased when it is combined with Fosphenytoin.
EtravirineThe serum concentration of Etravirine can be decreased when it is combined with Fosphenytoin.
EverolimusThe serum concentration of Everolimus can be decreased when it is combined with Fosphenytoin.
ExemestaneThe serum concentration of Exemestane can be decreased when it is combined with Fosphenytoin.
EzogabineThe serum concentration of Ezogabine can be decreased when it is combined with Fosphenytoin.
FelbamateThe serum concentration of Felbamate can be decreased when it is combined with Fosphenytoin.
FelodipineThe serum concentration of Fosphenytoin can be increased when it is combined with Felodipine.
FentanylThe serum concentration of Fentanyl can be decreased when it is combined with Fosphenytoin.
FlibanserinThe serum concentration of Flibanserin can be decreased when it is combined with Fosphenytoin.
FloxuridineThe serum concentration of Fosphenytoin can be increased when it is combined with Floxuridine.
FluconazoleThe metabolism of Fosphenytoin can be decreased when combined with Fluconazole.
FludiazepamThe serum concentration of Fosphenytoin can be increased when it is combined with Fludiazepam.
FludrocortisoneThe serum concentration of Fludrocortisone can be decreased when it is combined with Fosphenytoin.
FlunarizineThe serum concentration of Flunarizine can be decreased when it is combined with Fosphenytoin.
FlunisolideThe metabolism of Flunisolide can be increased when combined with Fosphenytoin.
FlunitrazepamThe serum concentration of Fosphenytoin can be increased when it is combined with Flunitrazepam.
FluorouracilThe serum concentration of Fosphenytoin can be increased when it is combined with Fluorouracil.
FluoxetineFosphenytoin may increase the QTc-prolonging activities of Fluoxetine.
FluvastatinThe serum concentration of Fluvastatin can be decreased when it is combined with Fosphenytoin.
FluvoxamineThe serum concentration of Fosphenytoin can be increased when it is combined with Fluvoxamine.
Folic AcidThe serum concentration of Fosphenytoin can be decreased when it is combined with Folic Acid.
FosamprenavirThe serum concentration of Fosamprenavir can be increased when it is combined with Fosphenytoin.
FurosemideFosphenytoin may decrease the diuretic activities of Furosemide.
GabapentinThe serum concentration of Fosphenytoin can be increased when it is combined with Gabapentin.
GefitinibThe serum concentration of Gefitinib can be decreased when it is combined with Fosphenytoin.
GoserelinFosphenytoin may increase the QTc-prolonging activities of Goserelin.
GuanfacineThe serum concentration of Guanfacine can be decreased when it is combined with Fosphenytoin.
HalazepamThe serum concentration of Fosphenytoin can be increased when it is combined with Halazepam.
HalothaneThe serum concentration of Fosphenytoin can be increased when it is combined with Halothane.
HydrocodoneFosphenytoin may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
HydrocortisoneThe serum concentration of Hydrocortisone can be decreased when it is combined with Fosphenytoin.
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Fosphenytoin.
IbrutinibThe serum concentration of Ibrutinib can be decreased when it is combined with Fosphenytoin.
IdelalisibThe serum concentration of Idelalisib can be decreased when it is combined with Fosphenytoin.
ImatinibThe serum concentration of Imatinib can be decreased when it is combined with Fosphenytoin.
IrinotecanThe serum concentration of the active metabolites of Irinotecan can be reduced when Irinotecan is used in combination with Fosphenytoin resulting in a loss in efficacy.
IsavuconazoniumThe serum concentration of the active metabolites of Isavuconazonium can be reduced when Isavuconazonium is used in combination with Fosphenytoin resulting in a loss in efficacy.
IsoniazidThe serum concentration of Fosphenytoin can be increased when it is combined with Isoniazid.
IsradipineThe serum concentration of Fosphenytoin can be increased when it is combined with Isradipine.
ItraconazoleThe serum concentration of Itraconazole can be decreased when it is combined with Fosphenytoin.
IvabradineThe serum concentration of Ivabradine can be decreased when it is combined with Fosphenytoin.
IvacaftorThe serum concentration of Ivacaftor can be decreased when it is combined with Fosphenytoin.
IxabepiloneThe serum concentration of Ixabepilone can be decreased when it is combined with Fosphenytoin.
KetazolamThe serum concentration of Fosphenytoin can be increased when it is combined with Ketazolam.
KetoconazoleThe serum concentration of Ketoconazole can be decreased when it is combined with Fosphenytoin.
LacosamideThe serum concentration of Lacosamide can be decreased when it is combined with Fosphenytoin.
LamotrigineThe serum concentration of Lamotrigine can be decreased when it is combined with Fosphenytoin.
LapatinibThe serum concentration of Lapatinib can be decreased when it is combined with Fosphenytoin.
LedipasvirThe serum concentration of Ledipasvir can be decreased when it is combined with Fosphenytoin.
LercanidipineThe serum concentration of Fosphenytoin can be increased when it is combined with Lercanidipine.
LeucovorinThe serum concentration of Fosphenytoin can be decreased when it is combined with Leucovorin.
LeuprolideFosphenytoin may increase the QTc-prolonging activities of Leuprolide.
LevodopaThe therapeutic efficacy of Levodopa can be decreased when used in combination with Fosphenytoin.
LevomefolateThe serum concentration of Fosphenytoin can be decreased when it is combined with Levomefolate.
LevonorgestrelThe therapeutic efficacy of Levonorgestrel can be decreased when used in combination with Fosphenytoin.
LevothyroxineThe serum concentration of Levothyroxine can be decreased when it is combined with Fosphenytoin.
LinagliptinThe serum concentration of Linagliptin can be decreased when it is combined with Fosphenytoin.
LiothyronineThe serum concentration of Liothyronine can be decreased when it is combined with Fosphenytoin.
LiotrixThe serum concentration of Liotrix can be decreased when it is combined with Fosphenytoin.
LithiumThe risk or severity of adverse effects can be increased when Fosphenytoin is combined with Lithium.
LopinavirThe serum concentration of Lopinavir can be decreased when it is combined with Fosphenytoin.
LorazepamThe serum concentration of Fosphenytoin can be increased when it is combined with Lorazepam.
LovastatinThe serum concentration of Lovastatin can be decreased when it is combined with Fosphenytoin.
LuliconazoleThe serum concentration of Fosphenytoin can be increased when it is combined with Luliconazole.
LumacaftorThe serum concentration of Fosphenytoin can be decreased when it is combined with Lumacaftor.
LumefantrineThe serum concentration of Lumefantrine can be decreased when it is combined with Fosphenytoin.
LurasidoneThe serum concentration of Lurasidone can be decreased when it is combined with Fosphenytoin.
MacitentanThe serum concentration of MACITENTAN can be decreased when it is combined with Fosphenytoin.
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Fosphenytoin.
MaravirocThe serum concentration of Maraviroc can be decreased when it is combined with Fosphenytoin.
MebendazoleThe serum concentration of Mebendazole can be decreased when it is combined with Fosphenytoin.
Medroxyprogesterone acetateThe therapeutic efficacy of Medroxyprogesterone Acetate can be decreased when used in combination with Fosphenytoin.
MefloquineThe therapeutic efficacy of Fosphenytoin can be decreased when used in combination with Mefloquine.
MethadoneThe serum concentration of Methadone can be decreased when it is combined with Fosphenytoin.
MethotrexateThe serum concentration of Fosphenytoin can be decreased when it is combined with Methotrexate.
MethotrimeprazineFosphenytoin may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
MethylphenidateThe serum concentration of Fosphenytoin can be increased when it is combined with Methylphenidate.
MethylprednisoloneThe serum concentration of Methylprednisolone can be decreased when it is combined with Fosphenytoin.
MetronidazoleThe serum concentration of Metronidazole can be decreased when it is combined with Fosphenytoin.
MetyraponeThe serum concentration of Metyrapone can be decreased when it is combined with Fosphenytoin.
MetyrosineFosphenytoin may increase the sedative activities of Metyrosine.
MexiletineThe serum concentration of Mexiletine can be decreased when it is combined with Fosphenytoin.
MianserinThe therapeutic efficacy of Fosphenytoin can be decreased when used in combination with Mianserin.
MiconazoleThe serum concentration of Fosphenytoin can be increased when it is combined with Miconazole.
MifepristoneThe serum concentration of Mifepristone can be decreased when it is combined with Fosphenytoin.
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Fosphenytoin.
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Fosphenytoin.
NaloxegolThe serum concentration of Naloxegol can be decreased when it is combined with Fosphenytoin.
NelfinavirThe serum concentration of Nelfinavir can be decreased when it is combined with Fosphenytoin.
NetupitantThe serum concentration of Netupitant can be decreased when it is combined with Fosphenytoin.
NicardipineThe serum concentration of Fosphenytoin can be increased when it is combined with Nicardipine.
NifedipineThe serum concentration of Nifedipine can be decreased when it is combined with Fosphenytoin.
NilotinibThe serum concentration of Nilotinib can be decreased when it is combined with Fosphenytoin.
NimodipineThe serum concentration of Nimodipine can be decreased when it is combined with Fosphenytoin.
NintedanibThe serum concentration of Nintedanib can be decreased when it is combined with Fosphenytoin.
NisoldipineThe serum concentration of Nisoldipine can be decreased when it is combined with Fosphenytoin.
NitrazepamThe serum concentration of Fosphenytoin can be increased when it is combined with Nitrazepam.
NitrendipineThe serum concentration of Fosphenytoin can be increased when it is combined with Nitrendipine.
NorethisteroneThe therapeutic efficacy of Norethindrone can be decreased when used in combination with Fosphenytoin.
OlaparibThe serum concentration of Olaparib can be decreased when it is combined with Fosphenytoin.
OmeprazoleThe serum concentration of Fosphenytoin can be increased when it is combined with Omeprazole.
OrlistatThe serum concentration of Fosphenytoin can be decreased when it is combined with Orlistat.
OrphenadrineFosphenytoin may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
OxazepamThe serum concentration of Fosphenytoin can be increased when it is combined with Oxazepam.
OxcarbazepineThe 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.
PalbociclibThe serum concentration of Palbociclib can be decreased when it is combined with Fosphenytoin.
PaliperidoneThe serum concentration of Paliperidone can be decreased when it is combined with Fosphenytoin.
PanobinostatThe serum concentration of Panobinostat can be decreased when it is combined with Fosphenytoin.
PantoprazoleThe metabolism of Pantoprazole can be increased when combined with Fosphenytoin.
ParaldehydeFosphenytoin may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
ParoxetineThe risk or severity of adverse effects can be increased when Fosphenytoin is combined with Paroxetine.
PazopanibThe serum concentration of Pazopanib can be decreased when it is combined with Fosphenytoin.
PerampanelThe serum concentration of Perampanel can be decreased when it is combined with Fosphenytoin.
PerhexilineThe serum concentration of Fosphenytoin can be increased when it is combined with Perhexiline.
PethidineThe serum concentration of Pethidine can be decreased when it is combined with Fosphenytoin.
PhenobarbitalFosphenytoin may increase the central nervous system depressant (CNS depressant) activities of Phenobarbital.
PhenytoinThe metabolism of FosPhenytoin can be increased when combined with Phenytoin.
PonatinibThe serum concentration of Ponatinib can be decreased when it is combined with Fosphenytoin.
PosaconazoleThe serum concentration of Posaconazole can be decreased when it is combined with Fosphenytoin.
PramipexoleFosphenytoin may increase the sedative activities of Pramipexole.
PravastatinThe serum concentration of Pravastatin can be decreased when it is combined with Fosphenytoin.
PraziquantelThe serum concentration of Praziquantel can be decreased when it is combined with Fosphenytoin.
PrednisoloneThe serum concentration of Prednisolone can be decreased when it is combined with Fosphenytoin.
PrednisoneThe serum concentration of Prednisone can be decreased when it is combined with Fosphenytoin.
PrenylamineThe serum concentration of Fosphenytoin can be increased when it is combined with Prenylamine.
PrimidoneThe metabolism of Primidone can be increased when combined with Fosphenytoin.
PropacetamolThe serum concentration of the active metabolites of Propacetamol can be reduced when Propacetamol is used in combination with Fosphenytoin resulting in a loss in efficacy.
PropafenoneThe serum concentration of Propafenone can be decreased when it is combined with Fosphenytoin.
PyridoxineThe metabolism of Fosphenytoin can be increased when combined with Pyridoxine.
QuazepamThe serum concentration of Fosphenytoin can be increased when it is combined with Quazepam.
QuetiapineThe serum concentration of Quetiapine can be decreased when it is combined with Fosphenytoin.
QuinidineFosphenytoin may increase the QTc-prolonging activities of Quinidine.
QuinineThe serum concentration of Quinine can be decreased when it is combined with Fosphenytoin.
RanolazineThe serum concentration of Ranolazine can be decreased when it is combined with Fosphenytoin.
RegorafenibThe serum concentration of Regorafenib can be decreased when it is combined with Fosphenytoin.
RifampicinThe serum concentration of Fosphenytoin can be decreased when it is combined with Rifampicin.
RilpivirineThe serum concentration of Rilpivirine can be decreased when it is combined with Fosphenytoin.
RisedronateThe serum concentration of Fosphenytoin can be increased when it is combined with Risedronate.
RitonavirThe serum concentration of Ritonavir can be decreased when it is combined with Fosphenytoin.
RivaroxabanThe serum concentration of Rivaroxaban can be decreased when it is combined with Fosphenytoin.
RoflumilastThe serum concentration of Roflumilast can be decreased when it is combined with Fosphenytoin.
RolapitantThe serum concentration of Rolapitant can be decreased when it is combined with Fosphenytoin.
RomidepsinThe serum concentration of Romidepsin can be decreased when it is combined with Fosphenytoin.
RopiniroleFosphenytoin may increase the sedative activities of Ropinirole.
RotigotineFosphenytoin may increase the sedative activities of Rotigotine.
RufinamideThe serum concentration of Rufinamide can be decreased when it is combined with Fosphenytoin.
SaquinavirThe serum concentration of Saquinavir can be decreased when it is combined with Fosphenytoin.
SaxagliptinThe serum concentration of Saxagliptin can be decreased when it is combined with Fosphenytoin.
SecobarbitalThe metabolism of Fosphenytoin can be increased when combined with Secobarbital.
SertralineThe serum concentration of Sertraline can be decreased when it is combined with Fosphenytoin.
SildenafilThe metabolism of Sildenafil can be increased when combined with Fosphenytoin.
SimeprevirThe serum concentration of Simeprevir can be decreased when it is combined with Fosphenytoin.
SimvastatinThe serum concentration of Simvastatin can be decreased when it is combined with Fosphenytoin.
SirolimusThe serum concentration of Sirolimus can be decreased when it is combined with Fosphenytoin.
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Fosphenytoin.
SofosbuvirThe serum concentration of Sofosbuvir can be decreased when it is combined with Fosphenytoin.
SonidegibThe serum concentration of Sonidegib can be decreased when it is combined with Fosphenytoin.
SorafenibThe serum concentration of Sorafenib can be decreased when it is combined with Fosphenytoin.
SulfisoxazoleThe metabolism of Fosphenytoin can be decreased when combined with Sulfisoxazole.
SunitinibThe serum concentration of Sunitinib can be decreased when it is combined with Fosphenytoin.
SuvorexantThe serum concentration of Suvorexant can be decreased when it is combined with Fosphenytoin.
TacrolimusThe serum concentration of Tacrolimus can be decreased when it is combined with Fosphenytoin.
TadalafilThe serum concentration of Tadalafil can be decreased when it is combined with Fosphenytoin.
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Fosphenytoin.
TasimelteonThe serum concentration of Tasimelteon can be decreased when it is combined with Fosphenytoin.
TegafurThe serum concentration of Fosphenytoin can be increased when it is combined with Tegafur.
TelaprevirThe serum concentration of Fosphenytoin can be increased when it is combined with Telaprevir.
TemazepamThe serum concentration of Fosphenytoin can be increased when it is combined with Temazepam.
TemsirolimusThe serum concentration of Temsirolimus can be decreased when it is combined with Fosphenytoin.
TeniposideThe serum concentration of Teniposide can be decreased when it is combined with Fosphenytoin.
ThalidomideFosphenytoin may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
TheophyllineThe serum concentration of Theophylline can be decreased when it is combined with Fosphenytoin.
Thyroid, porcineThe serum concentration of Thyroid extract can be decreased when it is combined with Fosphenytoin.
TicagrelorThe serum concentration of the active metabolites of Ticagrelor can be reduced when Ticagrelor is used in combination with Fosphenytoin resulting in a loss in efficacy.
TiclopidineThe serum concentration of Fosphenytoin can be increased when it is combined with Ticlopidine.
TipranavirThe serum concentration of Tipranavir can be decreased when it is combined with Fosphenytoin.
TofacitinibThe serum concentration of Tofacitinib can be decreased when it is combined with Fosphenytoin.
TofisopamThe serum concentration of Fosphenytoin can be increased when it is combined with Tofisopam.
TolvaptanThe serum concentration of Tolvaptan can be decreased when it is combined with Fosphenytoin.
TopiramateThe serum concentration of Topiramate can be decreased when it is combined with Fosphenytoin.
TopotecanThe serum concentration of Topotecan can be decreased when it is combined with Fosphenytoin.
TorasemideFosphenytoin may decrease the diuretic activities of Torasemide.
ToremifeneThe serum concentration of Toremifene can be decreased when it is combined with Fosphenytoin.
TrabectedinThe serum concentration of Trabectedin can be decreased when it is combined with Fosphenytoin.
TrazodoneThe serum concentration of Trazodone can be decreased when it is combined with Fosphenytoin.
TreprostinilThe serum concentration of Treprostinil can be decreased when it is combined with Fosphenytoin.
TriazolamThe serum concentration of Fosphenytoin can be increased when it is combined with Triazolam.
TrimethoprimThe serum concentration of Trimethoprim can be decreased when it is combined with Fosphenytoin.
UlipristalThe serum concentration of Ulipristal can be decreased when it is combined with Fosphenytoin.
Valproic AcidThe serum concentration of Fosphenytoin can be decreased when it is combined with Valproic Acid.
VandetanibThe serum concentration of Vandetanib can be decreased when it is combined with Fosphenytoin.
VemurafenibThe serum concentration of Vemurafenib can be decreased when it is combined with Fosphenytoin.
VerapamilThe serum concentration of Fosphenytoin can be increased when it is combined with Verapamil.
VigabatrinThe serum concentration of Fosphenytoin can be decreased when it is combined with Vigabatrin.
VilazodoneThe serum concentration of Vilazodone can be decreased when it is combined with Fosphenytoin.
VincristineThe serum concentration of Vincristine can be decreased when it is combined with Fosphenytoin.
VorapaxarThe serum concentration of Vorapaxar can be decreased when it is combined with Fosphenytoin.
VoriconazoleThe serum concentration of Voriconazole can be decreased when it is combined with Fosphenytoin.
VortioxetineThe serum concentration of Vortioxetine can be decreased when it is combined with Fosphenytoin.
WarfarinFosphenytoin may increase the anticoagulant activities of Warfarin.
ZaleplonThe serum concentration of Zaleplon can be decreased when it is combined with Fosphenytoin.
ZolpidemFosphenytoin may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
ZonisamideThe serum concentration of Zonisamide can be decreased when it is combined with Fosphenytoin.
Food Interactions
  • Avoid alcohol.
  • Do not take calcium, aluminum, magnesium or Iron supplements within 2 hours of taking this medication.
  • Take with food.

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 protein forms a sodium-selective channel through which Na(+) ions may pass in accordance with their electrochemical gradient. It is a tetrodotoxin-resistant Na(+) channel isoform. This channel is respon...
Gene Name:
SCN5A
Uniprot ID:
Q14524
Molecular Weight:
226937.475 Da
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:15001403 ]
  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. doi: 10.1016/S1474-4422(10)70059-4. [PubMed:20298965 ]
  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:15066664 ]
  4. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinducer
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. In the epoxidation of arachidonic acid it generates only 14,15- and 11,12-cis-epoxyeicosatrienoic acids. It is the principal enzyme...
Gene Name:
CYP2C8
Uniprot ID:
P10632
Molecular Weight:
55824.275 Da
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:12920163 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinducer
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. Anderson GD: Pharmacokinetic, pharmacodynamic, and pharmacogenetic targeted therapy of antiepileptic drugs. Ther Drug Monit. 2008 Apr;30(2):173-80. doi: 10.1097/FTD.0b013e318167d11b. [PubMed:18367977 ]
  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. doi: 10.1177/0091270009343006. Epub 2009 Jul 17. [PubMed:19617466 ]
  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:17375979 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inducer
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. 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:15123723 ]
  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:14977870 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinducer
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. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenyto...
Gene Name:
CYP2C9
Uniprot ID:
P11712
Molecular Weight:
55627.365 Da
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. doi: 10.1002/jbt.20264. [PubMed:19202563 ]
  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:19515014 ]
  3. Goldstein JA: Clinical relevance of genetic polymorphisms in the human CYP2C subfamily. Br J Clin Pharmacol. 2001 Oct;52(4):349-55. [PubMed:11678778 ]
  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:17375979 ]
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 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. Zhou SF: Drugs behave as substrates, inhibitors and inducers of human cytochrome P450 3A4. Curr Drug Metab. 2008 May;9(4):310-22. [PubMed:18473749 ]

Carriers

Kind
Protein
Organism
Human
Pharmacological action
no
Actions
other/unknown
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 colloidal osmotic pressure of blood. Major zinc transporter in plasma, typically binds about 80% of all plasma zinc.
Gene Name:
ALB
Uniprot ID:
P02768
Molecular Weight:
69365.94 Da
References
  1. Walker MC, Patsalos PN: Clinical pharmacokinetics of new antiepileptic drugs. Pharmacol Ther. 1995;67(3):351-84. [PubMed:8577822 ]
Comments
comments powered by Disqus
Drug created on June 30, 2007 11:18 / Updated on August 17, 2016 12:23