Peringatan Keamanan

There is limited information regarding the signs, symptoms, and treatment of a cenobamate overdose.L10653 Symptomatic and supportive treatment is recommended and there is limited data on the utility of dialysis to remove cenobamate from blood.L10653

Cenobamate

DB06119

small molecule approved investigational

Deskripsi

Cenobamate, or YKP-3089, is an antiepileptic drug developed by SK Pharmaceuticals and used to treat partial onset seizures.A188442,L10653 The exact mechanism of action has not been described in the literature, though it positively modulates GABAA and inhibits voltage gated sodium channels.L10653

Cenobamate was granted FDA approval on 21 November 2019.L10653

Struktur Molekul 2D

Berat 267.67
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 cenobamate is 50-60h.[L10653]
Volume Distribusi The apparent volume of distribution of cenobamate is 40-50L.[L10653]
Klirens (Clearance) The apparent oral clearance of cenobamate is 0.45-0.63L/h for a 100-400mg/day dose.[L10653]

Absorpsi

Cenobamate is 88% orally bioavailable with a Tmax of 1-4 hours.L10653 A high fat meal does not significantly impact the pharmacokinetics of cenobamate.L10653 Plasma Cmax and AUC for cenobamate crushed tablets mixed in water, administered either orally or through a nasogastric tube, were similar to whole tablets. The median Tmax for crushed tablets is 0.5 hours.L51043

Metabolisme

Data regarding the metabolism of cenobamate is lacking, however it is mostly glucuronidated by UGT2B7 and UGT2B4 or oxidized by a number of cytochromes.L10653

Rute Eliminasi

Cenobamate is 87.8% eliminated in the urine and 5.2% in the feces.L10653

Interaksi Makanan

2 Data
  • 1. Avoid alcohol. Alcohol may increase somnolence and sedation.
  • 2. Take with or without food.

Interaksi Obat

1131 Data
Dabrafenib The serum concentration of Cenobamate can be decreased when it is combined with Dabrafenib.
Eliglustat The metabolism of Eliglustat can be decreased when combined with Cenobamate.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Cenobamate.
Luliconazole The serum concentration of Cenobamate can be increased when it is combined with Luliconazole.
Cilostazol The serum concentration of Cilostazol can be increased when it is combined with Cenobamate.
Colchicine The metabolism of Colchicine can be decreased when combined with Cenobamate.
Fentanyl The serum concentration of Fentanyl can be decreased when it is combined with Cenobamate.
Iloperidone The metabolism of Iloperidone can be decreased when combined with Cenobamate.
Retapamulin The metabolism of Retapamulin can be decreased when combined with Cenobamate.
Tofacitinib The metabolism of Tofacitinib can be decreased when combined with Cenobamate.
Vardenafil The metabolism of Vardenafil can be decreased when combined with Cenobamate.
Lovastatin The metabolism of Lovastatin can be decreased when combined with Cenobamate.
Mefloquine The therapeutic efficacy of Cenobamate can be decreased when used in combination with Mefloquine.
Mianserin The therapeutic efficacy of Cenobamate can be decreased when used in combination with Mianserin.
Orlistat Orlistat can cause a decrease in the absorption of Cenobamate resulting in a reduced serum concentration and potentially a decrease in efficacy.
Topotecan Cenobamate may increase the excretion rate of Topotecan which could result in a lower serum level and potentially a reduction in efficacy.
Alfuzosin The metabolism of Alfuzosin can be decreased when combined with Cenobamate.
Alprazolam The metabolism of Alprazolam can be decreased when combined with Cenobamate.
Ifosfamide The metabolism of Ifosfamide can be increased when combined with Cenobamate.
Perampanel The metabolism of Perampanel can be increased when combined with Cenobamate.
R,S-Warfarin alcohol The serum concentration of R,S-Warfarin alcohol can be increased when it is combined with Cenobamate.
S,R-Warfarin alcohol The serum concentration of S,R-Warfarin alcohol can be increased when it is combined with Cenobamate.
Midazolam The serum concentration of Midazolam can be increased when it is combined with Cenobamate.
Tetracosactide The risk or severity of liver damage can be increased when Tetracosactide is combined with Cenobamate.
Tacrolimus The serum concentration of Tacrolimus can be increased when it is combined with Cenobamate.
Atorvastatin The metabolism of Atorvastatin can be decreased when combined with Cenobamate.
Lumacaftor The serum concentration of Cenobamate can be decreased when it is combined with Lumacaftor.
Erlotinib The serum concentration of Erlotinib can be decreased when it is combined with Cenobamate.
Chloramphenicol The metabolism of Cenobamate can be decreased when combined with Chloramphenicol.
Isoniazid The metabolism of Cenobamate can be decreased when combined with Isoniazid.
Miconazole The metabolism of Cenobamate can be decreased when combined with Miconazole.
Zafirlukast The metabolism of Cenobamate can be decreased when combined with Zafirlukast.
Eslicarbazepine acetate The metabolism of Cenobamate can be decreased when combined with Eslicarbazepine acetate.
Tranylcypromine The metabolism of Cenobamate can be decreased when combined with Tranylcypromine.
Caffeine Cenobamate may increase the excretion rate of Caffeine which could result in a lower serum level and potentially a reduction in efficacy.
Dyphylline Cenobamate may increase the excretion rate of Dyphylline which could result in a lower serum level and potentially a reduction in efficacy.
Pentoxifylline Cenobamate may increase the excretion rate of Pentoxifylline which could result in a lower serum level and potentially a reduction in efficacy.
Mercaptopurine Cenobamate may increase the excretion rate of Mercaptopurine which could result in a lower serum level and potentially a reduction in efficacy.
Oxtriphylline Cenobamate may increase the excretion rate of Oxtriphylline which could result in a lower serum level and potentially a reduction in efficacy.
Theobromine Cenobamate may increase the excretion rate of Theobromine which could result in a lower serum level and potentially a reduction in efficacy.
Fenethylline Cenobamate may increase the excretion rate of Fenethylline which could result in a lower serum level and potentially a reduction in efficacy.
8-azaguanine Cenobamate may increase the excretion rate of 8-azaguanine which could result in a lower serum level and potentially a reduction in efficacy.
7,9-Dimethylguanine Cenobamate may increase the excretion rate of 7,9-Dimethylguanine which could result in a lower serum level and potentially a reduction in efficacy.
Xanthine Cenobamate may increase the excretion rate of Xanthine which could result in a lower serum level and potentially a reduction in efficacy.
7-Deazaguanine Cenobamate may increase the excretion rate of 7-Deazaguanine which could result in a lower serum level and potentially a reduction in efficacy.
Guanine Cenobamate may increase the excretion rate of Guanine which could result in a lower serum level and potentially a reduction in efficacy.
9-Methylguanine Cenobamate may increase the excretion rate of 9-Methylguanine which could result in a lower serum level and potentially a reduction in efficacy.
Peldesine Cenobamate may increase the excretion rate of Peldesine which could result in a lower serum level and potentially a reduction in efficacy.
Hypoxanthine Cenobamate may increase the excretion rate of Hypoxanthine which could result in a lower serum level and potentially a reduction in efficacy.
9-Deazaguanine Cenobamate may increase the excretion rate of 9-Deazaguanine which could result in a lower serum level and potentially a reduction in efficacy.
Propentofylline Cenobamate may increase the excretion rate of Propentofylline which could result in a lower serum level and potentially a reduction in efficacy.
Valomaciclovir Cenobamate may increase the excretion rate of Valomaciclovir which could result in a lower serum level and potentially a reduction in efficacy.
3-isobutyl-1-methyl-7H-xanthine Cenobamate may increase the excretion rate of 3-isobutyl-1-methyl-7H-xanthine which could result in a lower serum level and potentially a reduction in efficacy.
Uric acid Cenobamate may increase the excretion rate of Uric acid which could result in a lower serum level and potentially a reduction in efficacy.
Doxofylline Cenobamate may increase the excretion rate of Doxofylline which could result in a lower serum level and potentially a reduction in efficacy.
Lisofylline Cenobamate may increase the excretion rate of Lisofylline which could result in a lower serum level and potentially a reduction in efficacy.
Lobucavir Cenobamate may increase the excretion rate of Lobucavir which could result in a lower serum level and potentially a reduction in efficacy.
Cafedrine Cenobamate may increase the excretion rate of Cafedrine which could result in a lower serum level and potentially a reduction in efficacy.
Theodrenaline Cenobamate may increase the excretion rate of Theodrenaline which could result in a lower serum level and potentially a reduction in efficacy.
Bamifylline Cenobamate may increase the excretion rate of Bamifylline which could result in a lower serum level and potentially a reduction in efficacy.
Proxyphylline Cenobamate may increase the excretion rate of Proxyphylline which could result in a lower serum level and potentially a reduction in efficacy.
Acefylline Cenobamate may increase the excretion rate of Acefylline which could result in a lower serum level and potentially a reduction in efficacy.
Etamiphylline Cenobamate may increase the excretion rate of Etamiphylline which could result in a lower serum level and potentially a reduction in efficacy.
Pentifylline Cenobamate may increase the excretion rate of Pentifylline which could result in a lower serum level and potentially a reduction in efficacy.
Bufylline Cenobamate may increase the excretion rate of Bufylline which could result in a lower serum level and potentially a reduction in efficacy.
Bromotheophylline Cenobamate may increase the excretion rate of Bromotheophylline which could result in a lower serum level and potentially a reduction in efficacy.
Furafylline Cenobamate may increase the excretion rate of Furafylline which could result in a lower serum level and potentially a reduction in efficacy.
8-chlorotheophylline Cenobamate may increase the excretion rate of 8-chlorotheophylline which could result in a lower serum level and potentially a reduction in efficacy.
PCS-499 Cenobamate may increase the excretion rate of PCS-499 which could result in a lower serum level and potentially a reduction in efficacy.
Apalutamide The serum concentration of Cenobamate can be increased when it is combined with Apalutamide.
Pitolisant The serum concentration of Cenobamate can be decreased when it is combined with Pitolisant.
Segesterone acetate The metabolism of Segesterone acetate can be increased when combined with Cenobamate.
Metreleptin The metabolism of Cenobamate can be increased when combined with Metreleptin.
Alectinib The metabolism of Alectinib can be increased when combined with Cenobamate.
Pexidartinib The metabolism of Pexidartinib can be increased when combined with Cenobamate.
Cimetidine The metabolism of Cenobamate can be decreased when combined with Cimetidine.
Ciprofloxacin The metabolism of Cenobamate can be decreased when combined with Ciprofloxacin.
Troglitazone The metabolism of Cenobamate can be decreased when combined with Troglitazone.
Seproxetine The metabolism of Cenobamate can be decreased when combined with Seproxetine.
Letermovir The metabolism of Cenobamate can be decreased when combined with Letermovir.
Curcumin sulfate The metabolism of Cenobamate can be decreased when combined with Curcumin sulfate.
Clofazimine The metabolism of Cenobamate can be decreased when combined with Clofazimine.
Levoketoconazole The serum concentration of Levoketoconazole can be decreased when it is combined with Cenobamate.
Reserpine The metabolism of Cenobamate can be increased when combined with Reserpine.
Thalidomide The serum concentration of Thalidomide can be decreased when it is combined with Cenobamate.
Cortivazol The metabolism of Cenobamate can be increased when combined with Cortivazol.
Cloprednol The metabolism of Cenobamate can be increased when combined with Cloprednol.
Prednisolone hemisuccinate The metabolism of Cenobamate can be increased when combined with Prednisolone hemisuccinate.
Prednisone acetate The metabolism of Cenobamate can be increased when combined with Prednisone acetate.
Clocortolone acetate The metabolism of Cenobamate can be increased when combined with Clocortolone acetate.
Melengestrol acetate The metabolism of Cenobamate can be increased when combined with Melengestrol acetate.
Cortisone The metabolism of Cenobamate can be increased when combined with Cortisone.
Oxcarbazepine The metabolism of Cenobamate can be increased when combined with Oxcarbazepine.
Daunorubicin The metabolism of Cenobamate can be increased when combined with Daunorubicin.
Torasemide The metabolism of Torasemide can be increased when combined with Cenobamate.
Ketorolac The metabolism of Ketorolac can be increased when combined with Cenobamate.
Piroxicam The metabolism of Piroxicam can be increased when combined with Cenobamate.
Amodiaquine The metabolism of Amodiaquine can be increased when combined with Cenobamate.
Naproxen The metabolism of Naproxen can be increased when combined with Cenobamate.
Tazarotene The metabolism of Tazarotene can be increased when combined with Cenobamate.

Target Protein

Voltage-gated sodium channel alpha subunit SCN1A
Gamma-aminobutyric acid receptor subunit alpha-1 GABRA1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 31063770
    Nakamura M, Cho JH, Shin H, Jang IS: Effects of cenobamate (YKP3089), a newly developed anti-epileptic drug, on voltage-gated sodium channels in rat hippocampal CA3 neurons. Eur J Pharmacol. 2019 Jul 15;855:175-182. doi: 10.1016/j.ejphar.2019.05.007. Epub 2019 May 4.
  • PMID: 31292226
    Kasteleijn-Nolst Trenite DGA, DiVentura BD, Pollard JR, Krauss GL, Mizne S, French JA: Suppression of the photoparoxysmal response in photosensitive epilepsy with cenobamate (YKP3089). Neurology. 2019 Aug 6;93(6):e559-e567. doi: 10.1212/WNL.0000000000007894. Epub 2019 Jul 10.

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