Peringatan Keamanan

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.

Fosphenytoin

DB01320

small molecule approved investigational

Deskripsi

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.

Struktur Molekul 2D

Berat 362.2739
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Fosphenytoin has a conversion half-life of approximately 15 minutes. The resulting phenytoin has a wide range of mean total half-life values (12 to 28.9 hours), with longer half-life times at higher administered doses.[L20619]
Volume Distribusi The volume of distribution of fosphenytoin increases with dose and rate, ranging between 4.3 and 10.8 L.[L20619]
Klirens (Clearance) -

Absorpsi

Fosphenytoin at 15 to 20 mg PE/kg infused at 100 to 150 mg PE/min intravenously yields free plasma phenytoin concentrations similar to an equivalent dose of phenytoin sodium administered at 50 mg/min. Single intravenous administration of fosphenytoin shows a linear increase in mean maximum total phenytoin concentration while the mean maximum unbound phenytoin concentrations increase with both dose and infusion rate. Fosphenytoin is rapidly converted to phenytoin following intravenous administration with a half-life of 15 minutes; if administered intramuscularly, the peak plasma phenytoin concentration is not reached until three hours.L20619

Metabolisme

Fosphenytoin is metabolized, likely by phosphatases, to phenytoin, phosphate, and formaldehyde; the formaldehyde is subsequently converted into formate. The phenytoin produced is metabolized hepatically by CYP2C9 and, to a lesser extent, by CYP2C19.L20619

Rute Eliminasi

Phenytoin derived from fosphenytoin administration is excreted in the urine primarily as 5-(p-hydroxyphenyl)-5-phenylhydantoin and its glucuronide. There is little unchanged phenytoin (1%–5% of the administered dose), and essentially no fosphenytoin recovered in urine.L20619

Interaksi Makanan

2 Data
  • 1. Avoid alcohol. Acute alcohol consumption may increase phenytoin serum concentration, but chronic alcohol use may reduce phenytoin serum concentration.
  • 2. Avoid St. John's Wort. This herb may reduce the serum concentration of phenytoin.

Interaksi Obat

1781 Data
Modafinil The metabolism of Fosphenytoin can be increased when combined with Modafinil.
Armodafinil The metabolism of Fosphenytoin can be increased when combined with Armodafinil.
Cyclosporine The serum concentration of Cyclosporine can be decreased when it is combined with Fosphenytoin.
Aripiprazole The metabolism of Aripiprazole can be increased when combined with Fosphenytoin.
Tetrahydrofolic acid The serum concentration of Fosphenytoin can be decreased when it is combined with Tetrahydrofolic acid.
Folic acid The serum concentration of Fosphenytoin can be decreased when it is combined with Folic acid.
Leucovorin The serum concentration of Fosphenytoin can be decreased when it is combined with Leucovorin.
(6S)-5,6,7,8-tetrahydrofolic acid The serum concentration of Fosphenytoin can be decreased when it is combined with (6S)-5,6,7,8-tetrahydrofolic acid.
Triglu-5-formyl-tetrahydrofolate The serum concentration of Fosphenytoin can be decreased when it is combined with Triglu-5-formyl-tetrahydrofolate.
(6R)-Folinic acid The serum concentration of Fosphenytoin can be decreased when it is combined with (6R)-Folinic acid.
5-methyltetrahydrofolic acid The serum concentration of Fosphenytoin can be decreased when it is combined with 5-methyltetrahydrofolic acid.
Levomefolic acid The serum concentration of Fosphenytoin can be decreased when it is combined with Levomefolic acid.
Levoleucovorin The serum concentration of Fosphenytoin can be decreased when it is combined with Levoleucovorin.
Pyridoxine The metabolism of Fosphenytoin can be increased when combined with Pyridoxine.
Phenytoin The metabolism of Fosphenytoin can be increased when combined with Phenytoin.
Azithromycin The metabolism of Azithromycin can be increased when combined with Fosphenytoin.
Methysergide The metabolism of Methysergide can be increased when combined with Fosphenytoin.
Chlorpromazine The metabolism of Chlorpromazine can be increased when combined with Fosphenytoin.
Cephalexin The metabolism of Cephalexin can be increased when combined with Fosphenytoin.
Doxazosin The metabolism of Doxazosin can be increased when combined with Fosphenytoin.
Cisapride The metabolism of Cisapride can be increased when combined with Fosphenytoin.
Astemizole The metabolism of Astemizole can be increased when combined with Fosphenytoin.
Norethisterone The metabolism of Norethisterone can be increased when combined with Fosphenytoin.
Fenofibrate The metabolism of Fenofibrate can be increased when combined with Fosphenytoin.
Rosuvastatin The metabolism of Rosuvastatin can be increased when combined with Fosphenytoin.
Pimozide The metabolism of Pimozide can be increased when combined with Fosphenytoin.
Drospirenone The metabolism of Drospirenone can be increased when combined with Fosphenytoin.
Allylestrenol The metabolism of Allylestrenol can be increased when combined with Fosphenytoin.
Zuclopenthixol The metabolism of Zuclopenthixol can be increased when combined with Fosphenytoin.
Roflumilast The metabolism of Roflumilast can be increased when combined with Fosphenytoin.
Cobimetinib The serum concentration of Cobimetinib can be decreased when it is combined with Fosphenytoin.
Fosaprepitant The metabolism of Fosaprepitant can be increased when combined with Fosphenytoin.
Lomitapide The metabolism of Lomitapide can be increased when combined with Fosphenytoin.
Linagliptin The metabolism of Linagliptin can be increased when combined with Fosphenytoin.
Vorapaxar The metabolism of Vorapaxar can be increased when combined with Fosphenytoin.
Netupitant The metabolism of Netupitant can be increased when combined with Fosphenytoin.
Idelalisib The metabolism of Idelalisib can be increased when combined with Fosphenytoin.
Ceritinib The metabolism of Ceritinib can be increased when combined with Fosphenytoin.
Tasimelteon The metabolism of Tasimelteon can be increased when combined with Fosphenytoin.
Nintedanib The metabolism of Nintedanib can be increased when combined with Fosphenytoin.
Tenofovir alafenamide The serum concentration of Tenofovir alafenamide can be decreased when it is combined with Fosphenytoin.
Dihydroergocornine The metabolism of Dihydroergocornine can be increased when combined with Fosphenytoin.
Isavuconazole The metabolism of Isavuconazole can be increased when combined with Fosphenytoin.
Ebastine The metabolism of Ebastine can be increased when combined with Fosphenytoin.
Duvelisib The metabolism of Duvelisib can be increased when combined with Fosphenytoin.
Dacomitinib The metabolism of Dacomitinib can be increased when combined with Fosphenytoin.
Gilteritinib The metabolism of Gilteritinib can be increased when combined with Fosphenytoin.
9-aminocamptothecin The metabolism of 9-aminocamptothecin can be increased when combined with Fosphenytoin.
Methylprednisone The metabolism of Methylprednisone can be increased when combined with Fosphenytoin.
Dihydroergocristine The metabolism of Dihydroergocristine can be increased when combined with Fosphenytoin.
Dihydroergocryptine The metabolism of Dihydroergocryptine can be increased when combined with Fosphenytoin.
Medical Cannabis The metabolism of Medical Cannabis can be increased when combined with Fosphenytoin.
Tazemetostat The metabolism of Tazemetostat can be increased when combined with Fosphenytoin.
Pretomanid The serum concentration of Pretomanid can be decreased when it is combined with Fosphenytoin.
Fluvoxamine The serum concentration of Fosphenytoin can be increased when it is combined with Fluvoxamine.
Buprenorphine Fosphenytoin may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
Doxylamine Doxylamine may increase the central nervous system depressant (CNS depressant) activities of Fosphenytoin.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Fosphenytoin.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Fosphenytoin.
Hydroxyzine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Fosphenytoin.
Magnesium sulfate The therapeutic efficacy of Fosphenytoin can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Fosphenytoin may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Fosphenytoin may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Fosphenytoin.
Mirtazapine Fosphenytoin may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Fosphenytoin.
Orphenadrine Fosphenytoin may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Fosphenytoin may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
Pramipexole Fosphenytoin may increase the sedative activities of Pramipexole.
Rotigotine Fosphenytoin may increase the sedative activities of Rotigotine.
Sodium oxybate The risk or severity of CNS depression can be increased when Fosphenytoin is combined with Sodium oxybate.
Suvorexant Fosphenytoin may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Tapentadol Tapentadol may increase the central nervous system depressant (CNS depressant) activities of Fosphenytoin.
Thalidomide Fosphenytoin may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Fosphenytoin may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Amphetamine The therapeutic efficacy of Fosphenytoin can be decreased when used in combination with Amphetamine.
Phentermine The therapeutic efficacy of Fosphenytoin can be decreased when used in combination with Phentermine.
Pseudoephedrine The therapeutic efficacy of Fosphenytoin can be decreased when used in combination with Pseudoephedrine.
Benzphetamine The therapeutic efficacy of Fosphenytoin can be decreased when used in combination with Benzphetamine.
Diethylpropion The therapeutic efficacy of Fosphenytoin can be decreased when used in combination with Diethylpropion.
Lisdexamfetamine The therapeutic efficacy of Fosphenytoin can be decreased when used in combination with Lisdexamfetamine.
Mephentermine The therapeutic efficacy of Fosphenytoin can be decreased when used in combination with Mephentermine.
MMDA The therapeutic efficacy of Fosphenytoin can be decreased when used in combination with MMDA.
Midomafetamine The therapeutic efficacy of Fosphenytoin can be decreased when used in combination with Midomafetamine.
2,5-Dimethoxy-4-ethylamphetamine The therapeutic efficacy of Fosphenytoin can be decreased when used in combination with 2,5-Dimethoxy-4-ethylamphetamine.
4-Bromo-2,5-dimethoxyamphetamine The therapeutic efficacy of Fosphenytoin can be decreased when used in combination with 4-Bromo-2,5-dimethoxyamphetamine.
Tenamfetamine The therapeutic efficacy of Fosphenytoin can be decreased when used in combination with Tenamfetamine.
Chlorphentermine The therapeutic efficacy of Fosphenytoin can be decreased when used in combination with Chlorphentermine.
Methylenedioxyethamphetamine The therapeutic efficacy of Fosphenytoin can be decreased when used in combination with Methylenedioxyethamphetamine.
Dextroamphetamine The therapeutic efficacy of Fosphenytoin can be decreased when used in combination with Dextroamphetamine.
Metamfetamine The therapeutic efficacy of Fosphenytoin can be decreased when used in combination with Metamfetamine.
Iofetamine I-123 The therapeutic efficacy of Fosphenytoin can be decreased when used in combination with Iofetamine I-123.
Ritobegron The therapeutic efficacy of Fosphenytoin can be decreased when used in combination with Ritobegron.
Mephedrone The therapeutic efficacy of Fosphenytoin can be decreased when used in combination with Mephedrone.
Methoxyphenamine The therapeutic efficacy of Fosphenytoin can be decreased when used in combination with Methoxyphenamine.
Gepefrine The therapeutic efficacy of Fosphenytoin can be decreased when used in combination with Gepefrine.
2,5-Dimethoxy-4-ethylthioamphetamine The therapeutic efficacy of Fosphenytoin can be decreased when used in combination with 2,5-Dimethoxy-4-ethylthioamphetamine.
Phendimetrazine The therapeutic efficacy of Fosphenytoin can be decreased when used in combination with Phendimetrazine.
Halazepam The serum concentration of Fosphenytoin can be increased when it is combined with Halazepam.
Camazepam The serum concentration of Fosphenytoin can be increased when it is combined with Camazepam.

Target Protein

Sodium channel protein type 5 subunit alpha SCN5A

Referensi & Sumber

Synthesis reference: Volker Kirsch, "Process for the preparation of sodium fosphenytoin." U.S. Patent US20050272706, issued December 08, 2005.
Artikel (PubMed)
  • PMID: 11447516
    Johnson J, Wrenn K: Inappropriate fosphenytoin use in the ED. Am J Emerg Med. 2001 Jul;19(4):293-4.
  • PMID: 12716241
    Applebaum J, Levine J, Belmaker RH: Intravenous fosphenytoin in acute mania. J Clin Psychiatry. 2003 Apr;64(4):408-9.
  • PMID: 14622802
    McCleane GJ: Intravenous infusion of fosphenytoin produces prolonged pain relief: a case report. J Pain. 2002 Apr;3(2):156-8.
  • PMID: 8649612
    Browne TR, Kugler AR, Eldon MA: Pharmacology and pharmacokinetics of fosphenytoin. Neurology. 1996 Jun;46(6 Suppl 1):S3-7.
  • PMID: 19443931
    Luszczki JJ: Third-generation antiepileptic drugs: mechanisms of action, pharmacokinetics and interactions. Pharmacol Rep. 2009 Mar-Apr;61(2):197-216.

Contoh Produk & Brand

Produk: 43 • International brands: 2
Produk
  • Cerebyx
    Injection, solution • 50 mg/1mL • Intramuscular; Intravenous • US • Approved
  • Cerebyx
    Injection, solution • 50 mg/1mL • Intramuscular; Intravenous • US • Approved
  • Cerebyx
    Injection, solution • 50 mg/1mL • Intramuscular; Intravenous • US • Approved
  • Cerebyx
    Injection, solution • 50 mg/1mL • Intramuscular; Intravenous • US • Approved
  • Cerebyx
    Injection, solution • 50 mg/1mL • Intramuscular; Intravenous • US • Approved
  • Cerebyx
    Solution • 75 mg / mL • Intramuscular; Intravenous • Canada • Approved
  • Fosphenytoin
    Injection, solution • 50 mg/1mL • Intramuscular; Intravenous • US • Generic • Approved
  • Fosphenytoin Sodium
    Injection • 50 mg/1mL • Intravenous • US • Generic • Approved
Menampilkan 8 dari 43 produk.
International Brands
  • Prodilantin
  • Sesquient

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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