Peringatan Keamanan

There are no adequate and well-controlled studies of the use of eslicarbazepine acetate in pregnant women. In studies conducted in pregnant mice, rats, and rabbits, eslicarbazepine acetate did show developmental toxicities, including teratogenicity, embryolethality, and fetal growth retardation, at clinically relevant doses.
Drug-induced liver injury ranging from mild to moderate elevations in transaminases (>3 times the upper limit of normal) to rare cases with concomitant elevations of total bilirubin (>2 times the upper limit of normal) have been reported with the use of eslicarbazepine.
Overdose with eslicarbazepine acetate appears similar to its known adverse reactions and includes symptoms of hyponatremia, dizziness, nausea, vomiting, somnolence, euphoria, oral paraesthesias, ataxia, and diplopia. There is no specific antidote for eslicarbazepine acetate overdose and it should be treated primarily with supportive measures. If required, the drug may be removed by gastric lavage, partially by hemodialysis or inactivated with activated charcoal.

Eslicarbazepine acetate

DB09119

small molecule approved

Deskripsi

Eslicarbazepine acetate (ESL) is an anticonvulsant medication approved for use in Europe, the United States and Canada as an adjunctive therapy for partial-onset seizures that are not adequately controlled with conventional therapy. Eslicarbazepine acetate is a prodrug that is rapidly converted to eslicarbazepine, the primary active metabolite in the body. Eslicarbazepine's mechanism of action is not well understood, but it is known that it does exert anticonvulsant activity by inhibiting repeated neuronal firing and stabilizing the inactivated state of voltage-gated sodium channels, thus preventing their return to the activated state during which seizure activity can occur.

Eslicarbazepine acetate is marketed as Aptiom in North America and Zebinix or Exalief in Europe. It is available in 200, 400, 600, or 800mg tablets that are taken once daily, with or without food. Eslicarbazepine acetate is associated with numerous side effects including dizziness, drowsiness, nausea, vomiting, diarrhea, headache, aphasia, lack of concentration, psychomotor retardation, speech disturbances, ataxia, depression and hyponatremia. It is recommended that patients taking eslicarbazepine acetate be monitored for suicidality.

Struktur Molekul 2D

Berat 296.326
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The apparent plasma half-life of eslicarbazepine is 10-20 hours in healthy subjects and 13-20 hours in epilepsy patients. Steady-state plasma concentrations are attained after 4 to 5 days of once daily dosing.
Volume Distribusi The apparent volume of distribution of eslicarbazepine is 61.3 L for a body weight of 70 kg based on population PK analysis.
Klirens (Clearance) Renal clearance of eslicarbazepine was found to be approximately 20 mL/min in healthy subjects with normal renal function.

Absorpsi

Eslicarbazepine active metabolite has a high bioavailability and reaches peak serum concentration 1-4 hours after a given dose. Eslicarbazepine acetate absorption is not affected by food.

Metabolisme

Eslicarbazepine acetate is rapidly and extensively metabolized to its major active metabolite, eslicarbazepine, via hydrolytic first-pass metabolism. Eslicarbazepine corresponds to about 92% of systemic exposure. Minor active metabolites (R)-licarbazepine and oxcarbazepine consist of <5% of systemic exposure. Active metabolites are then metabolized to inactive glucuronides that correspond to about 3% of systemic exposure. Eslicarbazepine had a moderate inhibitory effect on CYP2C19 and a mild activation of UGT1A1-mediated glucuronidation when studied in human hepatic microsomes. It has been shown to induce CYP3A4 enzymes in vivo.

Rute Eliminasi

Eslicarbazepine acetate and its metabolites are eliminated primarily via renal excretion. Eslicarbazepine active metabolite is excreted two-thirds in the unchanged form and one-third as a glucuronide conjugate. This accounts for around 90% of total metabolites excreted, with the remaining 10% being minor metabolites. Renal tubular reabsorption is expected to occur with eslicarbazepine.

Interaksi Makanan

1 Data
  • 1. Take with or without food.

Interaksi Obat

1007 Data
Aripiprazole The metabolism of Aripiprazole can be increased when combined with Eslicarbazepine acetate.
Aripiprazole lauroxil The metabolism of Aripiprazole lauroxil can be increased when combined with Eslicarbazepine acetate.
Cilostazol The serum concentration of Cilostazol can be increased when it is combined with Eslicarbazepine acetate.
Buprenorphine Eslicarbazepine acetate 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 Eslicarbazepine acetate.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Eslicarbazepine acetate.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Eslicarbazepine acetate.
Hydrocodone Eslicarbazepine acetate 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 Eslicarbazepine acetate.
Magnesium sulfate The therapeutic efficacy of Eslicarbazepine acetate can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Eslicarbazepine acetate may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Eslicarbazepine acetate may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Eslicarbazepine acetate.
Mirtazapine Eslicarbazepine acetate 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 Eslicarbazepine acetate.
Orphenadrine Eslicarbazepine acetate may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Eslicarbazepine acetate may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
Pramipexole Eslicarbazepine acetate may increase the sedative activities of Pramipexole.
Ropinirole Eslicarbazepine acetate may increase the sedative activities of Ropinirole.
Rotigotine Eslicarbazepine acetate may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Eslicarbazepine acetate.
Sodium oxybate Eslicarbazepine acetate may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Eslicarbazepine acetate 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 Eslicarbazepine acetate.
Thalidomide Eslicarbazepine acetate may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Eslicarbazepine acetate may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Citalopram The serum concentration of Citalopram can be increased when it is combined with Eslicarbazepine acetate.
Clopidogrel The serum concentration of the active metabolites of Clopidogrel can be reduced when Clopidogrel is used in combination with Eslicarbazepine acetate resulting in a loss in efficacy.
Mefloquine The therapeutic efficacy of Eslicarbazepine acetate can be decreased when used in combination with Mefloquine.
Mianserin The therapeutic efficacy of Eslicarbazepine acetate can be decreased when used in combination with Mianserin.
Orlistat Orlistat can cause a decrease in the absorption of Eslicarbazepine acetate resulting in a reduced serum concentration and potentially a decrease in efficacy.
Topotecan Eslicarbazepine acetate 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 Eslicarbazepine acetate.
Ifosfamide The metabolism of Ifosfamide can be increased when combined with Eslicarbazepine acetate.
Perampanel The metabolism of Perampanel can be increased when combined with Eslicarbazepine acetate.
Warfarin The metabolism of Warfarin can be increased when combined with Eslicarbazepine acetate.
Acenocoumarol The metabolism of Acenocoumarol can be increased when combined with Eslicarbazepine acetate.
(R)-warfarin The metabolism of (R)-warfarin can be increased when combined with Eslicarbazepine acetate.
R,S-Warfarin alcohol The metabolism of R,S-Warfarin alcohol can be increased when combined with Eslicarbazepine acetate.
S,R-Warfarin alcohol The metabolism of S,R-Warfarin alcohol can be increased when combined with Eslicarbazepine acetate.
(S)-Warfarin The metabolism of (S)-Warfarin can be increased when combined with Eslicarbazepine acetate.
Rifampin The metabolism of Eslicarbazepine acetate can be increased when combined with Rifampicin.
Nelfinavir The metabolism of Eslicarbazepine acetate can be increased when combined with Nelfinavir.
Zidovudine The metabolism of Eslicarbazepine acetate can be increased when combined with Zidovudine.
Ritonavir The metabolism of Eslicarbazepine acetate can be increased when combined with Ritonavir.
Lamotrigine The metabolism of Eslicarbazepine acetate can be increased when combined with Lamotrigine.
Efavirenz The metabolism of Eslicarbazepine acetate can be increased when combined with Efavirenz.
Testosterone propionate The metabolism of Eslicarbazepine acetate can be increased when combined with Testosterone propionate.
Tipranavir The metabolism of Eslicarbazepine acetate can be increased when combined with Tipranavir.
Tetracosactide The risk or severity of liver damage can be increased when Tetracosactide is combined with Eslicarbazepine acetate.
Carbamazepine The risk or severity of adverse effects can be increased when Carbamazepine is combined with Eslicarbazepine acetate.
Oxcarbazepine The risk or severity of adverse effects can be increased when Oxcarbazepine is combined with Eslicarbazepine acetate.
Phenytoin The serum concentration of Eslicarbazepine acetate can be decreased when it is combined with Phenytoin.
Fosphenytoin The serum concentration of Eslicarbazepine acetate can be decreased when it is combined with Fosphenytoin.
Mephenytoin The serum concentration of Eslicarbazepine acetate can be decreased when it is combined with Mephenytoin.
Primidone The serum concentration of Eslicarbazepine acetate can be decreased when it is combined with Primidone.
Phenobarbital The serum concentration of Eslicarbazepine acetate can be decreased when it is combined with Phenobarbital.
Ethanol Eslicarbazepine acetate may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Eslicarbazepine acetate 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 Eslicarbazepine acetate.
Fluvoxamine The risk or severity of adverse effects can be increased when Eslicarbazepine acetate is combined with Fluvoxamine.
Duloxetine The risk or severity of adverse effects can be increased when Eslicarbazepine acetate is combined with Duloxetine.
Trazodone The risk or severity of adverse effects can be increased when Eslicarbazepine acetate is combined with Trazodone.
Paroxetine The risk or severity of adverse effects can be increased when Eslicarbazepine acetate is combined with Paroxetine.
Sertraline The risk or severity of adverse effects can be increased when Eslicarbazepine acetate is combined with Sertraline.
Sibutramine The risk or severity of adverse effects can be increased when Eslicarbazepine acetate is combined with Sibutramine.
Nefazodone The risk or severity of adverse effects can be increased when Eslicarbazepine acetate is combined with Nefazodone.
Escitalopram The risk or severity of adverse effects can be increased when Eslicarbazepine acetate is combined with Escitalopram.
Zimelidine The risk or severity of adverse effects can be increased when Eslicarbazepine acetate is combined with Zimelidine.
Dapoxetine The risk or severity of adverse effects can be increased when Eslicarbazepine acetate is combined with Dapoxetine.
Desvenlafaxine The risk or severity of adverse effects can be increased when Eslicarbazepine acetate is combined with Desvenlafaxine.
Seproxetine The risk or severity of adverse effects can be increased when Eslicarbazepine acetate is combined with Seproxetine.
Indalpine The risk or severity of adverse effects can be increased when Eslicarbazepine acetate is combined with Indalpine.
Ritanserin The risk or severity of adverse effects can be increased when Eslicarbazepine acetate is combined with Ritanserin.
Alaproclate The risk or severity of adverse effects can be increased when Eslicarbazepine acetate is combined with Alaproclate.
Erlotinib The serum concentration of Erlotinib can be decreased when it is combined with Eslicarbazepine acetate.
Cyproheptadine The risk or severity of CNS depression can be increased when Cyproheptadine is combined with Eslicarbazepine acetate.
Amoxapine The risk or severity of CNS depression can be increased when Amoxapine is combined with Eslicarbazepine acetate.
Propiomazine The risk or severity of CNS depression can be increased when Propiomazine is combined with Eslicarbazepine acetate.
Cocaine The risk or severity of methemoglobinemia can be increased when Eslicarbazepine acetate is combined with Cocaine.
Maprotiline The risk or severity of CNS depression can be increased when Maprotiline is combined with Eslicarbazepine acetate.
Desipramine The risk or severity of CNS depression can be increased when Desipramine is combined with Eslicarbazepine acetate.
Pizotifen The risk or severity of CNS depression can be increased when Pizotifen is combined with Eslicarbazepine acetate.
Dosulepin The risk or severity of CNS depression can be increased when Eslicarbazepine acetate is combined with Dosulepin.
Quetiapine The risk or severity of CNS depression can be increased when Quetiapine is combined with Eslicarbazepine acetate.
Amitriptyline The risk or severity of CNS depression can be increased when Amitriptyline is combined with Eslicarbazepine acetate.
Doxepin The risk or severity of CNS depression can be increased when Doxepin is combined with Eslicarbazepine acetate.
Terfenadine The metabolism of Terfenadine can be increased when combined with Eslicarbazepine acetate.
Clozapine The serum concentration of Clozapine can be decreased when it is combined with Eslicarbazepine acetate.
Zopiclone The risk or severity of adverse effects can be increased when Eslicarbazepine acetate is combined with Zopiclone.
Botulinum toxin type B The risk or severity of CNS depression can be increased when Botulinum toxin type B is combined with Eslicarbazepine acetate.
Botulinum toxin type A The risk or severity of CNS depression can be increased when Botulinum toxin type A is combined with Eslicarbazepine acetate.
Tryptophan The risk or severity of CNS depression can be increased when Tryptophan is combined with Eslicarbazepine acetate.
Baclofen Baclofen may increase the central nervous system depressant (CNS depressant) activities of Eslicarbazepine acetate.
Lorazepam The risk or severity of CNS depression can be increased when Lorazepam is combined with Eslicarbazepine acetate.
Ethchlorvynol The risk or severity of CNS depression can be increased when Ethchlorvynol is combined with Eslicarbazepine acetate.
Succinylcholine The risk or severity of CNS depression can be increased when Succinylcholine is combined with Eslicarbazepine acetate.
Reserpine The risk or severity of CNS depression can be increased when Reserpine is combined with Eslicarbazepine acetate.
Enflurane The risk or severity of CNS depression can be increased when Enflurane is combined with Eslicarbazepine acetate.
Temazepam The risk or severity of CNS depression can be increased when Temazepam is combined with Eslicarbazepine acetate.

Target Protein

P2X purinoceptor 4 P2RX4

Referensi & Sumber

Synthesis reference: - Ravinder B, Reddy SR, Sridhar M, Mohan MM, Srinivas K, Reddy AP, Bandichhor R. An efficient synthesis for eslicarbazepine acetate, oxcarbazepine, and carbamazepine. Tetrahedron Letters. 2013 May 29;54(22):2841-4. - Desai S, Poddar A, Sawant K: Formulation of cyclodextrin inclusion complex-based orally disintegrating tablet of eslicarbazepine acetate for improved oral bioavailability. Mater Sci Eng C Mater Biol Appl. 2016 Jan 1;58:826-34. doi: 10.1016/j.msec.2015.09.019. Epub 2015 Sep 8. Pubmed(http://www.ncbi.nlm.nih.gov/pubmed/26478377).
Artikel (PubMed)
  • PMID: 25740561
    Banach M, Borowicz KK, Czuczwar SJ: Pharmacokinetic/pharmacodynamic evaluation of eslicarbazepine for the treatment of epilepsy. Expert Opin Drug Metab Toxicol. 2015 Apr;11(4):639-48. doi: 10.1517/17425255.2015.1021686. Epub 2015 Mar 5.
  • PMID: 20043029
    Bialer M, White HS: Key factors in the discovery and development of new antiepileptic drugs. Nat Rev Drug Discov. 2010 Jan;9(1):68-82. doi: 10.1038/nrd2997.
  • PMID: 22612290
    Bialer M, Soares-da-Silva P: Pharmacokinetics and drug interactions of eslicarbazepine acetate. Epilepsia. 2012 Jun;53(6):935-46. doi: 10.1111/j.1528-1167.2012.03519.x. Epub 2012 May 21.
  • PMID: 24908564
    Villanueva V, Serratosa JM, Guillamon E, Garces M, Giraldez BG, Toledo M, Salas-Puig J, Lopez Gonzalez FJ, Flores J, Rodriguez-Uranga J, Castillo A, Mauri JA, Camacho JL, Lopez-Gomariz E, Giner P, Torres N, Palau J, Molins A: Long-term safety and efficacy of eslicarbazepine acetate in patients with focal seizures: results of the 1-year ESLIBASE retrospective study. Epilepsy Res. 2014 Sep;108(7):1243-52. doi: 10.1016/j.eplepsyres.2014.04.014. Epub 2014 May 14.
  • PMID: 26038700
    Soares-da-Silva P, Pires N, Bonifacio MJ, Loureiro AI, Palma N, Wright LC: Eslicarbazepine acetate for the treatment of focal epilepsy: an update on its proposed mechanisms of action. Pharmacol Res Perspect. 2015 Mar;3(2):e00124. doi: 10.1002/prp2.124. Epub 2015 Mar 30.
  • PMID: 26136845
    Rocamora R: A review of the efficacy and safety of eslicarbazepine acetate in the management of partial-onset seizures. Ther Adv Neurol Disord. 2015 Jul;8(4):178-86. doi: 10.1177/1756285615589711.
  • PMID: 26465930
    Tomic MA, Pecikoza UB, Micov AM, Stepanovic-Petrovic RM: The Efficacy of Eslicarbazepine Acetate in Models of Trigeminal, Neuropathic, and Visceral Pain: The Involvement of 5-HT1B/1D Serotonergic and CB1/CB2 Cannabinoid Receptors. Anesth Analg. 2015 Dec;121(6):1632-9. doi: 10.1213/ANE.0000000000000953.
  • PMID: 25880756
    Jacobson MP, Pazdera L, Bhatia P, Grinnell T, Cheng H, Blum D: Efficacy and safety of conversion to monotherapy with eslicarbazepine acetate in adults with uncontrolled partial-onset seizures: a historical-control phase III study. BMC Neurol. 2015 Mar 28;15:46. doi: 10.1186/s12883-015-0305-5.
Menampilkan 8 dari 12 artikel.

Contoh Produk & Brand

Produk: 40 • International brands: 10
Produk
  • Aptiom
    Tablet • 200 mg/1 • Oral • US • Approved
  • Aptiom
    Tablet • 400 mg/1 • Oral • US • Approved
  • Aptiom
    Tablet • 600 mg/1 • Oral • US • Approved
  • Aptiom
    Tablet • 800 mg/1 • Oral • US • Approved
  • Aptiom
    Kit • - • Oral • US • Approved
  • Aptiom
    Kit • - • Oral • US • Approved
  • Aptiom
    Tablet • 200 mg • Oral • Canada • Approved
  • Aptiom
    Tablet • 400 mg • Oral • Canada • Approved
Menampilkan 8 dari 40 produk.
International Brands
  • Eksaliyef — Bial-Portela & Ca. S.A.
  • Erelib — Bial-Portela & Ca. S.A.
  • Eslicar — Emcure Pharmaceuticals Ltd
  • Eslify — Torrent Pharmaceuticals Ltd
  • Eslistar — Lupin Ltd
  • Eslizen — Intas Pharmaceuticals Ltd
  • Exalief — Bial-Portela & Ca. S.A.
  • Normictal — Abbott India Ltd
  • Stedesa
  • Zefretol — Sun Pharma Laboratories Ltd

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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