Peringatan Keamanan

The oral LD50 in rats is >3 g/kg.L42505

There is limited clinical data on stiripentol overdose in humans. In mice, high doses of stiripentol (600 to 1800 mg/kg i.p.) caused decreased motor activity and respiration. Overdose should be managed with supportive and symptomatic treatment.L42500

Stiripentol

DB09118

small molecule approved

Deskripsi

Stiripentol is an antiepileptic agent that is an aromatic allylic alcohol drug, which makes it structurally unique from other antiepileptic drugs.A19740, A250825 The clinical development and marketing of stiripentol were first delayed due to the drug's potent inhibitory effects on hepatic cytochrome P450 (CYP) enzymes.A250825 However, its clinical efficacy as adjunctive therapy for epilepsies stems from its inhibitory action on CYP enzymes, as stiripentol reduces the degradation of CYP-sensitive antiepileptic drugs, hence boosting their therapeutic efficacy. Stiripentol may also exhibit direct anticonvulsant properties, although the exact mechanism of action is fully understood.A19739

Approved in the US, Canada, and Europe, stiripentol is used to treat seizures associated with Dravet syndrome.L880,L42500,L42510 It is marketed under the brand name Diacomit.

Struktur Molekul 2D

Berat 234.295
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The elimination half life is approximately ranges from 4.5 to 13 hours, in a dose-dependent manner.[L42500]
Volume Distribusi The average volume of distribution is 1.03 L/kg but does not display a dose-dependent relationship. Following administration, stiripentol enters the brain and accumulates in the cerebellum and medulla.[A19740]
Klirens (Clearance) Plasma clearance decreases markedly at high doses; it falls from approximately 40 L/kg/day at the dose of 600 mg/day to about 8 L/kg/day at the dose of 2,400 mg. Clearance is decreased after repeated administration of stiripentol, probably due to inhibition of the cytochrome P450 isoenzymes responsible for its metabolism.[L880]

Absorpsi

After oral administration, stiripentol is quickly and readily absorbed A19740 with a median Tmax of two to three hours.L42500 The systemic exposure increases dose-proportionally.L880 Stiripentol has a low bioavailability due to water insolubility and extensive metabolism.A19740

Metabolisme

Stiripentol is extensively metabolized. About 13 different metabolites have been found in urine. The main metabolic processes are demethylenation (oxidative cleavage of the methylenedioxy ring system) and glucuronidation, although precise identification of the enzymes involved has not yet been achieved.L880, L42510 Other metabolic pathways include O-methylation of catechol metabolites, hydroxylation of the t-butyl group, and conversion of the allylic alcohol side-chain to the isomeric 3-pentanone structure.A19740 In vitro studies suggested that the phase I metabolism of stiripentol is catalyzed by CYP1A2, CYP2C19 and CYP3A4 and possibly other enzymes.L42510

Rute Eliminasi

Stiripentol is mainly eliminated via metabolism.A19740 Its metabolites are excreted mainly via the kidney. Urinary metabolites of stiripentol accounted collectively for the majority (73%) of an oral acute dose whereas a further 13-24% was recovered in feces as unchanged drug.L880

Interaksi Makanan

5 Data
  • 1. Avoid excessive or chronic alcohol consumption. Ingesting alcohol may increase the risk of sedation and somnolence that can be caused by stiripentol.
  • 2. Avoid milk and dairy products. These products may interfere with the absorption of stiripentol.
  • 3. Limit caffeine intake. Stiripentol may attenuate CYP1A2-mediated metabolism of caffeine.
  • 4. Take with a full glass of water. Oral capsules should be swallowed whole with a glass of water during a meal and oral suspension should be mixed in a glass of water and should be taken immediately after mixing during a meal.
  • 5. Take with food. Stiripentol degrades rapidly in an acidic environment.

Interaksi Obat

2136 Data
Cilostazol The serum concentration of Cilostazol can be increased when it is combined with Stiripentol.
Citalopram The serum concentration of Citalopram can be increased when it is combined with Stiripentol.
Deferasirox The serum concentration of Stiripentol can be increased when it is combined with Deferasirox.
Peginterferon alfa-2b The metabolism of Peginterferon alfa-2b can be decreased when combined with Stiripentol.
Leflunomide The excretion of Leflunomide can be decreased when combined with Stiripentol.
Teriflunomide The excretion of Teriflunomide can be decreased when combined with Stiripentol.
Buprenorphine Stiripentol 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 Stiripentol.
Dronabinol The metabolism of Dronabinol can be decreased when combined with Stiripentol.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Stiripentol.
Hydroxyzine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Stiripentol.
Magnesium sulfate The therapeutic efficacy of Stiripentol can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine The metabolism of Methotrimeprazine can be decreased when combined with Stiripentol.
Metyrosine Stiripentol may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Stiripentol.
Mirtazapine The metabolism of Mirtazapine can be decreased when combined with Stiripentol.
Nabilone The metabolism of Nabilone can be decreased when combined with Stiripentol.
Orphenadrine The metabolism of Orphenadrine can be decreased when combined with Stiripentol.
Paraldehyde Stiripentol may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
Perampanel The metabolism of Perampanel can be decreased when combined with Stiripentol.
Pramipexole Stiripentol may increase the sedative activities of Pramipexole.
Rotigotine The metabolism of Rotigotine can be decreased when combined with Stiripentol.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Stiripentol.
Sodium oxybate Stiripentol may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Stiripentol 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 Stiripentol.
Thalidomide Stiripentol may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Stiripentol may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Dabrafenib The metabolism of Dabrafenib can be decreased when combined with Stiripentol.
Clopidogrel The metabolism of Clopidogrel can be decreased when combined with Stiripentol.
Eliglustat The metabolism of Eliglustat can be decreased when combined with Stiripentol.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Stiripentol.
Luliconazole The serum concentration of Stiripentol can be increased when it is combined with Luliconazole.
Colchicine The serum concentration of Colchicine can be increased when it is combined with Stiripentol.
Fentanyl The metabolism of Fentanyl can be decreased when combined with Stiripentol.
Iloperidone The metabolism of Iloperidone can be decreased when combined with Stiripentol.
Retapamulin The metabolism of Retapamulin can be decreased when combined with Stiripentol.
Tofacitinib The metabolism of Tofacitinib can be decreased when combined with Stiripentol.
Vardenafil The metabolism of Vardenafil can be decreased when combined with Stiripentol.
Mefloquine The therapeutic efficacy of Stiripentol can be decreased when used in combination with Mefloquine.
Mianserin The therapeutic efficacy of Stiripentol can be decreased when used in combination with Mianserin.
Orlistat Orlistat can cause a decrease in the absorption of Stiripentol resulting in a reduced serum concentration and potentially a decrease in efficacy.
Phenytoin The serum concentration of Phenytoin can be increased when it is combined with Stiripentol.
Fosphenytoin The metabolism of Fosphenytoin can be decreased when combined with Stiripentol.
Topotecan The excretion of Topotecan can be decreased when combined with Stiripentol.
Zolmitriptan The metabolism of Zolmitriptan can be decreased when combined with Stiripentol.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Stiripentol.
Alprazolam The metabolism of Alprazolam can be decreased when combined with Stiripentol.
Atomoxetine The metabolism of Atomoxetine can be decreased when combined with Stiripentol.
R,S-Warfarin alcohol The serum concentration of R,S-Warfarin alcohol can be increased when it is combined with Stiripentol.
S,R-Warfarin alcohol The serum concentration of S,R-Warfarin alcohol can be increased when it is combined with Stiripentol.
Midazolam The serum concentration of Midazolam can be increased when it is combined with Stiripentol.
Tetracosactide The risk or severity of liver damage can be increased when Tetracosactide is combined with Stiripentol.
Tacrolimus The metabolism of Tacrolimus can be decreased when combined with Stiripentol.
Atorvastatin The metabolism of Atorvastatin can be decreased when combined with Stiripentol.
Primidone The serum concentration of Stiripentol can be decreased when it is combined with Primidone.
Methylphenobarbital The serum concentration of Stiripentol can be decreased when it is combined with Methylphenobarbital.
Phenobarbital The serum concentration of Stiripentol can be decreased when it is combined with Phenobarbital.
Abiraterone The metabolism of Abiraterone can be decreased when combined with Stiripentol.
Cyproterone acetate The metabolism of Cyproterone acetate can be decreased when combined with Stiripentol.
Ethanol Stiripentol may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Stiripentol may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Brimonidine Brimonidine may increase the central nervous system depressant (CNS depressant) activities of Stiripentol.
Zimelidine The risk or severity of adverse effects can be increased when Stiripentol is combined with Zimelidine.
Seproxetine The risk or severity of adverse effects can be increased when Stiripentol is combined with Seproxetine.
Ritanserin The metabolism of Ritanserin can be decreased when combined with Stiripentol.
Alaproclate The risk or severity of adverse effects can be increased when Stiripentol is combined with Alaproclate.
Duloxetine The metabolism of Duloxetine can be decreased when combined with Stiripentol.
Trospium The metabolism of Trospium can be decreased when combined with Stiripentol.
Cyproheptadine The risk or severity of CNS depression can be increased when Cyproheptadine is combined with Stiripentol.
Lamotrigine The risk or severity of CNS depression can be increased when Lamotrigine is combined with Stiripentol.
Propiomazine The risk or severity of CNS depression can be increased when Propiomazine is combined with Stiripentol.
Propantheline Propantheline may decrease the excretion rate of Stiripentol which could result in a higher serum level.
Dicyclomine Dicyclomine may decrease the excretion rate of Stiripentol which could result in a higher serum level.
Biperiden The metabolism of Biperiden can be decreased when combined with Stiripentol.
Flavoxate Flavoxate may decrease the excretion rate of Stiripentol which could result in a higher serum level.
Pizotifen The risk or severity of CNS depression can be increased when Pizotifen is combined with Stiripentol.
Aclidinium Aclidinium may decrease the excretion rate of Stiripentol which could result in a higher serum level.
Brompheniramine The risk or severity of CNS depression can be increased when Brompheniramine is combined with Stiripentol.
Cocaine The metabolism of Cocaine can be decreased when combined with Stiripentol.
Rifampin The metabolism of Stiripentol can be increased when combined with Rifampicin.
Moxifloxacin The metabolism of Stiripentol can be decreased when combined with Moxifloxacin.
Gatifloxacin The metabolism of Stiripentol can be decreased when combined with Gatifloxacin.
Pazufloxacin The metabolism of Stiripentol can be decreased when combined with Pazufloxacin.
Caffeine The metabolism of Stiripentol can be decreased when combined with Caffeine.
Pentobarbital The metabolism of Stiripentol can be increased when combined with Pentobarbital.
Thiopental The metabolism of Thiopental can be decreased when combined with Stiripentol.
Thioridazine The metabolism of Thioridazine can be decreased when combined with Stiripentol.
Rabeprazole The metabolism of Rabeprazole can be decreased when combined with Stiripentol.
Proguanil The metabolism of Proguanil can be decreased when combined with Stiripentol.
Hexobarbital The metabolism of Hexobarbital can be decreased when combined with Stiripentol.
Barbital The metabolism of Barbital can be decreased when combined with Stiripentol.
Methsuximide The metabolism of Methsuximide can be decreased when combined with Stiripentol.
Dexrabeprazole The metabolism of Dexrabeprazole can be decreased when combined with Stiripentol.
Methylene blue The metabolism of Methylene blue can be decreased when combined with Stiripentol.
Pentamidine The metabolism of Pentamidine can be decreased when combined with Stiripentol.
Labetalol The metabolism of Labetalol can be decreased when combined with Stiripentol.
Nilutamide The metabolism of Nilutamide can be decreased when combined with Stiripentol.
Formoterol The metabolism of Formoterol can be decreased when combined with Stiripentol.
Gliclazide The metabolism of Gliclazide can be decreased when combined with Stiripentol.

Target Protein

GABA(A) Receptor GABRA1
Gamma-aminobutyric acid receptor subunit gamma-3 GABRG3
L-lactate dehydrogenase A chain LDHA
L-lactate dehydrogenase B chain LDHB

Referensi & Sumber

Artikel (PubMed)
  • PMID: 16650136
    Quilichini PP, Chiron C, Ben-Ari Y, Gozlan H: Stiripentol, a putative antiepileptic drug, enhances the duration of opening of GABA-A receptor channels. Epilepsia. 2006 Apr;47(4):704-16.
  • PMID: 15886413
    Trojnar MK, Wojtal K, Trojnar MP, Czuczwar SJ: Stiripentol. A novel antiepileptic drug. Pharmacol Rep. 2005 Mar-Apr;57(2):154-60.
  • PMID: 25792327
    Sada N, Lee S, Katsu T, Otsuki T, Inoue T: Epilepsy treatment. Targeting LDH enzymes with a stiripentol analog to treat epilepsy. Science. 2015 Mar 20;347(6228):1362-7. doi: 10.1126/science.aaa1299.
  • PMID: 24001087
    Grosenbaugh DK, Mott DD: Stiripentol in refractory status epilepticus. Epilepsia. 2013 Sep;54 Suppl 6:103-5. doi: 10.1111/epi.12291.
  • PMID: 31617141
    Frampton JE: Stiripentol: A Review in Dravet Syndrome. Drugs. 2019 Nov;79(16):1785-1796. doi: 10.1007/s40265-019-01204-y.
  • PMID: 17199026
    Chiron C: Stiripentol. Neurotherapeutics. 2007 Jan;4(1):123-5. doi: 10.1016/j.nurt.2006.10.001.

Contoh Produk & Brand

Produk: 21 • International brands: 0
Produk
  • Diacomit
    Capsule • 250 mg/1 • Oral • US • Approved
  • Diacomit
    Capsule • 500 mg/1 • Oral • US • Approved
  • Diacomit
    Powder, for suspension • 250 mg/1 • Oral • US • Approved
  • Diacomit
    Powder, for suspension • 500 mg/1 • Oral • US • Approved
  • Diacomit
    Capsule • 250 mg • Oral • Canada • Approved
  • Diacomit
    Capsule • 500 mg • Oral • Canada • Approved
  • Diacomit
    Powder, for suspension • 250 mg / sachet • Oral • Canada • Approved
  • Diacomit
    Powder, for suspension • 500 mg / sachet • Oral • Canada • Approved
Menampilkan 8 dari 21 produk.

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