Peringatan Keamanan

Experience with ganaxolone overdose is limited to a single report of an unintentional overdose in a pediatric patient, in which the patient received ten-fold the prescribed dose. The patient was hospitalized for evaluation and recovered.L41130 No specific information is available regarding treatment of ganaxolone overdose - patients suspected of overdosage should be closely monitored and receive standard supportive care.L41130

Ganaxolone

DB05087

small molecule approved investigational

Deskripsi

Ganaxolone is the 3?-methylated synthetic analog of allopregnanolone,L41130 a metabolite of progesterone.A3197 Ganaxolone belongs to a class of compounds referred to as neurosteroids.A3197 Endogenous neurosteroids, which comprise certain metabolites of progesterone and deoxycorticosterone, bind potently and specifically to GABAA receptors to enhance their inhibitory effects, and are thus known to have anxiolytic, analgesic, anticonvulsant, sedative, hypnotic, and anesthetic properties.A245995

Ganaxolone, similar to its endogenous counterparts, is a positive allosteric modulator of GABAA receptors.L41130 It was approved under the brand name ZTALMY by the US FDA in March 2022 for the treatment of seizures associated with CDKL5 deficiency disorder (CDD), becoming the first FDA-approved treatment indicated specifically for CDD.L41135 In July 2023, ganaxolone was also approved under the same brand name and for the same indication by the EMA.L47636

Struktur Molekul 2D

Berat 332.528
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The terminal half-life of ganaxolone is 34 hours.[L41130]
Volume Distribusi Both ganaxolone and its metabolites are widely distributed into tissues following oral administration, with a typical tissue-to-plasma ratio >5:1.[A3197]
Klirens (Clearance) -

Absorpsi

Following oral administration, maximum plasma concentrations are reached within 2 to 3 hours.L41130

Metabolisme

Ganaxolone is extensively metabolized, primarily by CYP3A4/5 and, to a lesser extent, CYP2B6, CYP2C19, and CYP2D6.L41130 While data regarding ganaxolone metabolism are lacking, a 16-OH metabolite generated via CYP3A4 metabolism has been identified as one of its major metabolites.A3197

Rute Eliminasi

Following a single oral dose of radiolabeled ganaxolone in healthy male subjects, 55% of the administered radioactivity was recovered in the feces (2% as unchanged parent drug) and 18% was recovered in the urine (none of which comprised unchanged parent drug).L41130

Interaksi Makanan

1 Data
  • 1. Take with food. Co-administration with food increases ganaxalone Cmax and AUC by 3- and 2-fold, respectively. In clinical trials to establish efficacy, ganaxolone was administered with food.

Interaksi Obat

832 Data
Bexarotene The metabolism of Ganaxolone can be increased when combined with Bexarotene.
Bosentan The metabolism of Ganaxolone can be increased when combined with Bosentan.
Nafcillin The metabolism of Ganaxolone can be increased when combined with Nafcillin.
Efavirenz The metabolism of Ganaxolone can be increased when combined with Efavirenz.
Modafinil The metabolism of Ganaxolone can be increased when combined with Modafinil.
Dexamethasone The metabolism of Ganaxolone can be increased when combined with Dexamethasone.
Etravirine The metabolism of Ganaxolone can be increased when combined with Etravirine.
Avasimibe The metabolism of Ganaxolone can be increased when combined with Avasimibe.
Echinacea The metabolism of Ganaxolone can be increased when combined with Echinacea.
Dexamethasone acetate The metabolism of Ganaxolone can be increased when combined with Dexamethasone acetate.
Phenytoin The metabolism of Ganaxolone can be increased when combined with Phenytoin.
Pentobarbital The metabolism of Ganaxolone can be increased when combined with Pentobarbital.
Carbamazepine The metabolism of Ganaxolone can be increased when combined with Carbamazepine.
Mitotane The metabolism of Ganaxolone can be increased when combined with Mitotane.
Primidone The metabolism of Ganaxolone can be increased when combined with Primidone.
Rimexolone The metabolism of Ganaxolone can be increased when combined with Rimexolone.
Rifampin The metabolism of Ganaxolone can be increased when combined with Rifampicin.
Phenobarbital The metabolism of Ganaxolone can be increased when combined with Phenobarbital.
Rifapentine The metabolism of Ganaxolone can be increased when combined with Rifapentine.
Fosphenytoin The metabolism of Ganaxolone can be increased when combined with Fosphenytoin.
St. John's Wort The metabolism of Ganaxolone can be increased when combined with St. John's Wort.
Midostaurin The metabolism of Ganaxolone can be increased when combined with Midostaurin.
Enzalutamide The metabolism of Ganaxolone can be increased when combined with Enzalutamide.
Lumacaftor The metabolism of Ganaxolone can be increased when combined with Lumacaftor.
Apalutamide The metabolism of Ganaxolone can be increased when combined with Apalutamide.
Buprenorphine Ganaxolone 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 Ganaxolone.
Dronabinol The risk or severity of sedation, somnolence, and CNS depression can be increased when Dronabinol is combined with Ganaxolone.
Droperidol The risk or severity of sedation, somnolence, and CNS depression can be increased when Droperidol is combined with Ganaxolone.
Hydrocodone Ganaxolone may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Hydroxyzine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Ganaxolone.
Magnesium sulfate The therapeutic efficacy of Ganaxolone can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine The risk or severity of sedation, somnolence, and CNS depression can be increased when Methotrimeprazine is combined with Ganaxolone.
Metyrosine Ganaxolone may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Ganaxolone.
Mirtazapine The risk or severity of sedation, somnolence, and CNS depression can be increased when Mirtazapine is combined with Ganaxolone.
Nabilone The risk or severity of sedation, somnolence, and CNS depression can be increased when Nabilone is combined with Ganaxolone.
Orphenadrine The risk or severity of sedation, somnolence, and CNS depression can be increased when Orphenadrine is combined with Ganaxolone.
Paraldehyde The risk or severity of sedation, somnolence, and CNS depression can be increased when Paraldehyde is combined with Ganaxolone.
Perampanel The risk or severity of sedation, somnolence, and CNS depression can be increased when Perampanel is combined with Ganaxolone.
Pramipexole Ganaxolone may increase the sedative activities of Pramipexole.
Ropinirole Ganaxolone may increase the sedative activities of Ropinirole.
Rotigotine The risk or severity of sedation, somnolence, and CNS depression can be increased when Rotigotine is combined with Ganaxolone.
Rufinamide The risk or severity of sedation, somnolence, and CNS depression can be increased when Rufinamide is combined with Ganaxolone.
Sodium oxybate Ganaxolone may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Ganaxolone 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 Ganaxolone.
Thalidomide Ganaxolone may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Ganaxolone may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Mefloquine The therapeutic efficacy of Ganaxolone can be decreased when used in combination with Mefloquine.
Mianserin The therapeutic efficacy of Ganaxolone can be decreased when used in combination with Mianserin.
Orlistat Orlistat can cause a decrease in the absorption of Ganaxolone resulting in a reduced serum concentration and potentially a decrease in efficacy.
Topotecan Ganaxolone may increase the excretion rate of Topotecan which could result in a lower serum level and potentially a reduction in efficacy.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Ganaxolone.
Tetracosactide The risk or severity of liver damage can be increased when Tetracosactide is combined with Ganaxolone.
Ethanol Ganaxolone may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Ganaxolone may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Brimonidine The risk or severity of sedation, somnolence, and CNS depression can be increased when Brimonidine is combined with Ganaxolone.
Fluvoxamine The risk or severity of sedation, somnolence, and CNS depression can be increased when Fluvoxamine is combined with Ganaxolone.
Citalopram The risk or severity of sedation, somnolence, and CNS depression can be increased when Citalopram is combined with Ganaxolone.
Fluoxetine Ganaxolone may increase the central nervous system depressant (CNS depressant) activities of Fluoxetine.
Duloxetine The risk or severity of sedation, somnolence, and CNS depression can be increased when Duloxetine is combined with Ganaxolone.
Trazodone The risk or severity of sedation, somnolence, and CNS depression can be increased when Trazodone is combined with Ganaxolone.
Paroxetine The risk or severity of sedation, somnolence, and CNS depression can be increased when Paroxetine is combined with Ganaxolone.
Sertraline The risk or severity of sedation, somnolence, and CNS depression can be increased when Sertraline is combined with Ganaxolone.
Sibutramine The risk or severity of sedation, somnolence, and CNS depression can be increased when Sibutramine is combined with Ganaxolone.
Nefazodone The risk or severity of sedation, somnolence, and CNS depression can be increased when Nefazodone is combined with Ganaxolone.
Escitalopram The risk or severity of sedation, somnolence, and CNS depression can be increased when Escitalopram is combined with Ganaxolone.
Zimelidine The risk or severity of sedation, somnolence, and CNS depression can be increased when Zimelidine is combined with Ganaxolone.
Dapoxetine The risk or severity of sedation, somnolence, and CNS depression can be increased when Dapoxetine is combined with Ganaxolone.
Milnacipran The risk or severity of sedation, somnolence, and CNS depression can be increased when Milnacipran is combined with Ganaxolone.
Desvenlafaxine The risk or severity of sedation, somnolence, and CNS depression can be increased when Desvenlafaxine is combined with Ganaxolone.
Seproxetine The risk or severity of sedation, somnolence, and CNS depression can be increased when Seproxetine is combined with Ganaxolone.
Indalpine The risk or severity of sedation, somnolence, and CNS depression can be increased when Indalpine is combined with Ganaxolone.
Ritanserin The risk or severity of sedation, somnolence, and CNS depression can be increased when Ritanserin is combined with Ganaxolone.
Alaproclate The risk or severity of sedation, somnolence, and CNS depression can be increased when Alaproclate is combined with Ganaxolone.
Tramadol The risk or severity of CNS depression can be increased when Ganaxolone is combined with Tramadol.
Ziprasidone The risk or severity of adverse effects can be increased when Ganaxolone is combined with Ziprasidone.
Amitriptyline The risk or severity of sedation, somnolence, and CNS depression can be increased when Amitriptyline is combined with Ganaxolone.
Olanzapine The risk or severity of sedation, somnolence, and CNS depression can be increased when Olanzapine is combined with Ganaxolone.
Clozapine The risk or severity of sedation, somnolence, and CNS depression can be increased when Clozapine is combined with Ganaxolone.
Promazine The risk or severity of sedation, somnolence, and CNS depression can be increased when Promazine is combined with Ganaxolone.
Cyproheptadine The risk or severity of sedation, somnolence, and CNS depression can be increased when Cyproheptadine is combined with Ganaxolone.
Imipramine The risk or severity of sedation, somnolence, and CNS depression can be increased when Imipramine is combined with Ganaxolone.
Chlorpromazine The risk or severity of sedation, somnolence, and CNS depression can be increased when Chlorpromazine is combined with Ganaxolone.
Gallamine triethiodide The risk or severity of sedation, somnolence, and CNS depression can be increased when Gallamine triethiodide is combined with Ganaxolone.
Triflupromazine The risk or severity of sedation, somnolence, and CNS depression can be increased when Triflupromazine is combined with Ganaxolone.
Nortriptyline The risk or severity of sedation, somnolence, and CNS depression can be increased when Nortriptyline is combined with Ganaxolone.
Amoxapine The risk or severity of sedation, somnolence, and CNS depression can be increased when Amoxapine is combined with Ganaxolone.
Rocuronium The risk or severity of sedation, somnolence, and CNS depression can be increased when Rocuronium is combined with Ganaxolone.
Scopolamine The risk or severity of sedation, somnolence, and CNS depression can be increased when Scopolamine is combined with Ganaxolone.
Clidinium The risk or severity of sedation, somnolence, and CNS depression can be increased when Clidinium is combined with Ganaxolone.
Propiomazine The risk or severity of sedation, somnolence, and CNS depression can be increased when Propiomazine is combined with Ganaxolone.
Brompheniramine The risk or severity of sedation, somnolence, and CNS depression can be increased when Brompheniramine is combined with Ganaxolone.
Flupentixol The risk or severity of sedation, somnolence, and CNS depression can be increased when Flupentixol is combined with Ganaxolone.
Cocaine The risk or severity of methemoglobinemia can be increased when Ganaxolone is combined with Cocaine.
Quinidine The therapeutic efficacy of Ganaxolone can be decreased when used in combination with Quinidine.
Maprotiline The risk or severity of sedation, somnolence, and CNS depression can be increased when Maprotiline is combined with Ganaxolone.
Promethazine The risk or severity of sedation, somnolence, and CNS depression can be increased when Promethazine is combined with Ganaxolone.
Diphenhydramine The risk or severity of sedation, somnolence, and CNS depression can be increased when Diphenhydramine is combined with Ganaxolone.

Target Protein

GABA(A) Receptor GABRA1

Referensi & Sumber

Synthesis reference: Shaw, K., & Hutchison, A. (2011). METHOD FOR MAKING 3?-HYDROXY, 3?- METHYL-5?-PREGNAN-20-ONE (GANAXOLONE) (WO2011019821A2). World Intellectual Property Organization.
Artikel (PubMed)
  • PMID: 17199022
    Nohria V, Giller E: Ganaxolone. Neurotherapeutics. 2007 Jan;4(1):102-5.
  • PMID: 17634060
    Pieribone VA, Tsai J, Soufflet C, Rey E, Shaw K, Giller E, Dulac O: Clinical evaluation of ganaxolone in pediatric and adolescent patients with refractory epilepsy. Epilepsia. 2007 Oct;48(10):1870-4. Epub 2007 Jul 18.
  • PMID: 9579942
    Monaghan EP, Navalta LA, Shum L, Ashbrook DW, Lee DA: Initial human experience with ganaxolone, a neuroactive steroid with antiepileptic activity. Epilepsia. 1997 Sep;38(9):1026-31. doi: 10.1111/j.1528-1157.1997.tb01486.x.
  • PMID: 15959466
    Belelli D, Lambert JJ: Neurosteroids: endogenous regulators of the GABA(A) receptor. Nat Rev Neurosci. 2005 Jul;6(7):565-75. doi: 10.1038/nrn1703.

Contoh Produk & Brand

Produk: 3 • International brands: 0
Produk
  • Ztalmy
    Suspension • 50 mg/1mL • Oral • US • Approved
  • Ztalmy
    Suspension • 50 mg/ml • Oral • EU • Approved
  • Ztalmy
    Suspension • 50 mg/ml • Oral • EU • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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