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Identification
Name Fosphenytoin
Accession Number DB01320
Type small molecule
Groups approved
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
Download: MOL | SDF | SMILES | InChI
Display: 2D Structure | 3D Structure
Synonyms
(3-Phosphoryloxymethyl)phenytoin
Fosfenitoina [inn-spanish]
Fosphenytoin sodium
Fosphenytoine [inn-french]
Fosphenytoinum [inn-latin]
Salts Not Available
Brand names
Name Company
Cerebyx
Prodilantin
Brand mixtures Not Available
Categories
  • Anticonvulsants
CAS number 93390-81-9
Weight Average: 362.2739
Monoisotopic: 362.066772734
Chemical Formula C16H15N2O6P
InChI Key InChIKey=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)
Plain Text
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
Plain Text
Mass Spec Not Available
Taxonomy
Kingdom Organic
Classes
  • Diphenylmethanes
Substructures
  • Imidazolidinediones
  • Hydroxy Compounds
  • Phosphonic Acids and Derivatives
  • Amino Ketones
  • Organophosphate Esters
  • Benzene and Derivatives
  • Ureas and Derivatives
  • Imidazolidines
  • Diphenylmethanes
  • Phenethylamines
  • Heterocyclic compounds
  • Aromatic compounds
  • Carboxamides and Derivatives
  • Phosphinic Acids and Derivatives
  • Carboxylic Acids and Derivatives
Pharmacology
Indication For 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.
Pharmacodynamics Fosphenytoin 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 action Fosphenytoin 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.
Absorption Fosphenytoin is completely bioavailable following lM administration.
Volume of distribution
  • 4.3 to 10.8 L
Protein binding Extensively bound (95% to 99%) to human plasma proteins, primarily albumin.
Metabolism Hepatic.
Route of elimination Phenytoin 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 life Fosphenytoin has a half-life of approximately 15 minutes.
Clearance Not Available
Toxicity Nausea, 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
Pathway Name SMPDB ID
Smp00326 Fosphenytoin (Antiarrhythmic) Pathway SMP00326
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
Form Route Strength
Liquid Intravenous
Liquid Intravenous
Prices
Unit description Cost Unit
Cerebyx 500 mg pe/10 ml vial 8.63 USD ml
Fosphenytoin 500 mg pe/10 ml 0.61 USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents Not Available
Properties
State solid
Experimental Properties Not Available
Predicted Properties
Property Value Source
water solubility 1.45e-01 g/l ALOGPS
logP 1.08 ALOGPS
logP 1.67 ChemAxon
logS -3.4 ALOGPS
pKa (strongest acidic) 1.46 ChemAxon
pKa (strongest basic) -9.7 ChemAxon
physiological charge -2 ChemAxon
hydrogen acceptor count 5 ChemAxon
hydrogen donor count 3 ChemAxon
polar surface area 116.17 ChemAxon
rotatable bond count 5 ChemAxon
refractivity 87.05 ChemAxon
polarizability 33.23 ChemAxon
References
Synthesis Reference Not Available
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
Resource Link
KEGG Compound C07840 Link_out
PubChem Compound 56339 Link_out
PubChem Substance 46505168 Link_out
ChemSpider 50839 Link_out
Therapeutic Targets Database DAP000520 Link_out
PharmGKB PA164746820 Link_out
Drug Product Database 2230988 Link_out
RxList http://www.rxlist.com/cgi/generic/fosphen.htm Link_out
Drugs.com http://www.drugs.com/cdi/fosphenytoin.html Link_out
Wikipedia http://en.wikipedia.org/wiki/Fosphenytoin Link_out
ATC Codes
  • N03AB05
AHFS Codes
  • 28:12.12
PDB Entries Not Available
FDA label show (820 KB)
MSDS Not Available
Interactions
Drug Interactions
Drug Interaction
Acenocoumarol Increased hydantoin levels and risk of bleeding
Alprazolam Fosphenytoin may increase the metabolism of alprazolam via CYP3A4.
Aminophylline Decreased effect of both products
Amiodarone Amiodarone may increase the effect of fosphenytoin.
Anisindione Increased hydantoin levels and risk of bleeding
Aprepitant The CYP3A4 inducer, fosphenytoin, may decrease the effect of aprepitant.
Atracurium Phenytoin decreases the effect of muscle relaxant
Betamethasone The enzyme inducer, fosphenytoin, may decrease the effect of the corticosteroid, betamethasone.
Bleomycin The antineoplasic agent decreases the effect of hydantoin
Capecitabine Capecitabine increases the effect of hydantoin
Carboplatin The antineoplasic agent decreases the effect of hydantoin
Carmustine The antineoplasic agent decreases the effect of hydantoin
Chloramphenicol Increases phenytoin, modifies chloramphenicol
Chlordiazepoxide Fosphenytoin may increase the metabolism of chlordiazepoxide via CYP3A4.
Chlorotrianisene The enzyme inducer, fosphenytoin, decreases the effect of the hormone agent, chlorotrianisene.
Chlorpheniramine The antihistamine increases the effect of hydantoin
Cimetidine Cimetidine 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.
Cisplatin The antineoplasic agent decreases the effect of hydantoin
Clarithromycin Clarithromycin may increase the therapeutic and adverse effects of fosphenytoin.
Clomifene The enzyme inducer, fosphenytoin, decreases the effect of the hormone agent, clomifene.
Clorazepate Fosphenytoin may increase the metabolism of clorazepate via CYP3A4.
Clozapine Hydantoin decreases the effect of clozapine
Conjugated Estrogens The enzyme inducer, fosphenytoin, decreases the effect of the hormone agent, conjugated estrogens.
Cortisone acetate The enzyme inducer, fosphenytoin, may decrease the effect of the corticosteroid, cortisone acetate.
Cyclosporine The hydantoin decreases the effect of cyclosporine
Delavirdine The anticonvulsant, fosphenytoin, decreases the effect of delavirdine.
Dexamethasone The enzyme inducer, fosphenytoin, may decrease the effect of the corticosteroid, dexamethasone.
Diazepam Fosphenytoin may increase the metabolism of diazepam via CYP3A4.
Diazoxide Diazoxide decreases the hydantoin effect
Dicumarol Increased hydantoin levels and risk of bleeding
Diethylstilbestrol The enzyme inducer, fosphenytoin, may decrease the therapeutic effect of diethylstilbestrol.
Disopyramide The hydantoin decreases the effect of disopyramide
Disulfiram Disulfiram may increase the effect of fosphenytoin.
Dopamine Risk of severe hypotension
Doxacurium chloride Phenytoin decreases the effect of muscle relaxant
Doxycycline The anticonvulsant, fosphenytoin, decreases the effect of doxycycline.
Dyphylline Decreased effect of both products
Estradiol The enzyme inducer, fosphenytoin, decreases the effect of the hormone agent, estradiol.
Estradiol valerate/Dienogest Affects CYP3A4 metabolism, decreases or effects levels of Estradiol valerate/Dienogest.
Estriol The enzyme inducer, fosphenytoin, decreases the effect of the hormone agent, estriol.
Estrone The enzyme inducer, fosphenytoin, decreases the effect of the hormone agent, estrone.
Estropipate The enzyme inducer, fosphenytoin, decreases the effect of the hormone agent, estropipate.
Ethinyl Estradiol This product may cause a slight decrease of contraceptive effect
Felbamate Increased phenytoin levels and decreased felbamate levels
Felodipine The hydantoin decreases the effect of felodipine
Fluconazole Fluconazole may increase the effect of hydantoin.
Fludrocortisone The enzyme inducer, fosphenytoin, may decrease the effect of the corticosteroid, fludrocortisone.
Fluorouracil Fluorouracil increases the effect of hydantoin
Fluoxetine Fluoxetine increases the effect of phenytoin
Flurazepam Fosphenytoin may increase the metabolism of flurazepam via CYP3A4.
Fluvoxamine Fluvoxamine may increase the therapeutic and adverse effects of fosphenytoin.
Folic Acid Folic acid decreases the levels of hydantoin
Furosemide The hydantoin decreases the effect of furosemide
Gabapentin Gabapentin may increase the effect of fosphenytoin.
Gefitinib The CYP3A4 inducer, fosphenytoin, may decrease the serum concentration and therapeutic effects of gefitinib.
Hydrocortisone The enzyme inducer, fosphenytoin, may decrease the effect of the corticosteroid, hydrocortisone.
Imatinib The hydantoin decreases the levels of imatinib
Irinotecan The hydantoin decreases the effect of irinotecan
Isoniazid Isoniazid may increase the effect of phenytoin in 20% of patients.
Itraconazole Phenytoin decreases the effect of itraconazole
Lamotrigine Phenytoin may reduce levels of lamotrigine
Levodopa The hydantoin decreases the effect of levodopa
Levonorgestrel Phenytoin decreases the contraceptive effect
Lopinavir Levels of both drugs are affected
Lurasidone Concomitant therapy with a CYP3A4 inducer will decrease levels of lurasidone. Coadministration with lurasidone is contraindicated.
Mebendazole The hydantoin decreases the efficiency of mebendazole
Medroxyprogesterone The enzyme inducer, fosphenytoin, may decrease the effect of the hormone, medroxyprogesterone.
Megestrol The enzyme inducer, fosphenytoin, may decrease the effect of the hormone, megestrol.
Mestranol This product may cause a slight decrease of contraceptive effect
Methadone The hydantoin decreases the effect of methadone
Methotrexate The antineoplasic agent decreases the effect of hydantoin
Methoxsalen The hydantoin decreases the effect of psoralene
Methylprednisolone The enzyme inducer, fosphenytoin, may decrease the effect of the corticosteroid, methylprednisolone.
Metocurine Phenytoin decreases the effect of muscle relaxant
Metyrapone The combination renders the test invalid
Mexiletine The hydantoin decreases the effect of mexiletine
Midazolam Fosphenytoin may increase the metabolism of midazolam via CYP3A4.
Mirtazapine The hydantoins may reduce mirtazapine plasma concentrations and pharmacological effects
Mivacurium Phenytoin decreases the effect of muscle relaxant
Nisoldipine Phenytoin decreases the efficiency of nisoldipine
Norethindrone This product may cause a slight decrease of contraceptive effect
Omeprazole Omeprazole increases the effect of hydantoin
Oxcarbazepine Oxcarbazepine increases the effect of hydantoin
Oxtriphylline Decreased effect of both products
Oxyphenbutazone The NSAID, oxphenbutazone, may increase the hydantoin effect of fosphenytoin.
Pancuronium Phenytoin decreases the effect of muscle relaxant
Paramethasone The enzyme inducer, fosphenytoin, may decrease the effect of the corticosteroid, paramethasone.
Phenylbutazone The NSAID, phenylbutazone, may increase the hydantoin effect of fosphenytoin.
Posaconazole Modifications of drug levels for both agents
Prednisolone The enzyme inducer, fosphenytoin, may decrease the effect of the corticosteroid, prednisolone.
Prednisone The enzyme inducer, fosphenytoin, may decrease the effect of the corticosteroid, prednisone.
Quetiapine Phenytoin decreases the effect of quetiapine
Quinestrol The enzyme inducer, fosphenytoin, decreases the effect of the hormone agent, quinestrol.
Quinidine The anticonvulsant, fosphenytoin, decreases the effect of quinidine.
Quinupristin This combination presents an increased risk of toxicity
Rifampin Rifampin may decrease the effect of fosphenytoin.
Sertraline Sertraline increases the effect of hydantoin
Sirolimus The hydantoin decreases sirolimus levels
Sucralfate Sucralfate decreases the effect of hydantoin
Sulfadiazine The sulfonamide increases the effect of hydantoin
Sulfamethizole The sulfonamide increases the effect of hydantoin
Tacrolimus The hydantoin decreases the effect of tacrolimus
Telithromycin Fosphenytoin may decrease the plasma concentration of Telithromycin. Consider alternate therapy.
Temsirolimus Fosphenytoin may increase the metabolism of Temsirolimus decreasing its efficacy. Concomitant therapy should be avoided.
Theophylline Decreased effect of both products
Thiotepa Possible increase in thiotepa levels
Ticlopidine Ticlopidine 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.
Tolbutamide Tolbutamide, 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.
Topiramate Increased phenytoin/decreased topiramate
Tramadol Fosphenytoin may decrease the effect of Tramadol by increasing Tramadol metabolism and clearance.
Trazodone The 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.
Tretinoin The 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.
Triamcinolone The enzyme inducer, fosphenytoin, may decrease the effect of the corticosteroid, triamcinolone.
Triazolam Fosphenytoin may increase the metabolism of triazolam via CYP3A4.
Trimethoprim Trimethoprim increases the effect of hydantoin
Trioxsalen The hydantoin decreases the effect of psoralene
Triprolidine The CNS depressants, Triprolidine and Fosphenytoin, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
Tubocurarine Phenytoin decreases the effect of muscle relaxant
Vecuronium Phenytoin decreases the effect of muscle relaxant
Vigabatrin Vigabatrin decreases the effect of hydantoin
Vinblastine The antineoplasic agent decreases the effect of hydantoin
Voriconazole The hydantoin decreases the effect of voriconazole
Warfarin Increased 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

Pharmacological action: yes
Actions: inhibitor

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 responsible for the initial upstroke of the action potential in the electrocardiogram

Organism class: human
UniProt ID: Q14524 Link_out
Gene: SCN5A Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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

Actions: substrate, inducer

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, phenytoin, tolbutamide and losartan

UniProt ID: P11712 Link_out
Gene: CYP2C9
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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

Actions: substrate, inducer

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 responsible for the metabolism the anti- cancer drug paclitaxel (taxol)

UniProt ID: P10632 Link_out
Gene: CYP2C8
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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

Actions: substrate, inducer

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

UniProt ID: P33261 Link_out
Gene: CYP2C19 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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

Actions: inducer

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 xenobiotics. The enzyme also hydroxylates etoposide

UniProt ID: P08684 Link_out
Gene: CYP3A4
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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

Actions: inducer

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

UniProt ID: P20813 Link_out
Gene: CYP2B6 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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

Actions: other/unknown

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

UniProt ID: P02768 Link_out
Gene: ALB Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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 February 08, 2013 16:20