Peringatan Keamanan

The oral LD50 of oxcarbazepine in mammals is 1240 mg/kg and the oral TDLo in children has been reported to be 73 mg/kg.L8672 Isolated cases of oxcarbazepine overdose have been reported - patients who ingested up to 24,000mg recovered with symptomatic treatment.L8627,L8630 Symptoms may include respiratory and CNS depression, movement-related disorders (e.g. dyskinesia, ataxia), nausea/vomiting, hyponatremia, or QTc prolongation. There is no antidote for oxcarbazepine overdose - management should consist of supportive and symptomatic treatment, and consideration should be given to the use of gastric lavage or activated charcoal.L8627,L8630

Oxcarbazepine

DB00776

small molecule approved

Deskripsi

Oxcarbazepine is an anti-epileptic medication used in the treatment of partial onset seizures that was first approved for use in the United States in 2000.L8627,L8630,L8633 It is a structural derivative of carbamazepineA186101 and exerts a majority of its activity via a pharmacologically active metabolite, MHD, which exists as a racemate in the blood - a pro-drug of the more active (S)-enantiomer is also marketed as a separate anti-epileptic under the name eslicarbazepine.A186011 Compared to other anti-epileptic drugs, which are generally metabolized via the cytochrome P450 system, oxcarbazepine has a reduced propensity for involvement in drug-drug interactions owing to its primarily reductive metabolism.A186032

Struktur Molekul 2D

Berat 252.268
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The plasma half-life of oxcarbazepine is approximately 2 hours and the plasma half-life of MHD is approximately 9 hours.[L8627,L8630,L8633]
Volume Distribusi The apparent volume of distribution of oxcarbazepine is 49 L.[L8627,L8630,L8633] The apparent volumes of distribution of (S)- and (R)-MHD were found to be 23.6 L and 31.7 L, respectively.[A186026]
Klirens (Clearance) Plasma clearance of oxcarbazepine has been estimated to be approximately 84.9 L/h, whereas plasma clearance of its active metabolite, MHD, was estimated to be 2.0 L/h.[A186026] Rapid metabolic clearance appears to be the main pathway for oxcarbazepine, while clearance of its metabolites occurs mainly via renal excretion.[A186032]

Absorpsi

Oxcarbazepine is completely absorbed following oral administration. A single 600mg dose of oxcarbazepine resulted in an MHD Cmax of 34 ?mol/L and a median Tmax of 4.5 hours.L8627,L8630,L8633 When administered twice daily, steady-state levels of MHD are attained within 2-3 days. The rate and extent of absorption of oxcarbazepine is not affected by food intake.L8627,L8630,L8633

Metabolisme

Oxcarbazepine is rapidly and extensively metabolized to its primary metabolite, MHD, which is responsible for the bulk of its anti-epileptic activity and exists in much higher concentrations in the plasma than the parent drug.L8627,L8630,L8633 MHD is formed via reduction by several members of the aldo-keto reductase family of cytosolic liver enzymes and exists as a racemate in plasma in an approximate ratio of 80% (S)-MHD to 20% (R)-MHD.A186011 MHD is further metabolized to glucuronide conjugate metabolites for excretion, and small amounts are oxidized to 10-,11-dihydro-10,11-dihydroxycarbamazepine (DHD) which is pharmacologically inactive.L8627,L8630,L8633,A186020 Only 10% of an administered dose of oxcarbazepine will remain as either the parent drug or glucuronide conjugates of the parent drug.A186026

Rute Eliminasi

Following oral administration, more than 95% of the administered dose of oxcarbazepine is found in the urine. Of this, approximately 49% is MHD glucuronide metabolites, 27% is unchanged MHD, 3% is inactive DHD metabolites, 13% is conjugated oxcarbazepine, and less than 1% is unchanged parent drug. Fecal elimination accounts for only 4% of the administered dose.L8627,L8630,L8633

Farmakogenomik

1 Varian
HLA-B (None)

Patients who carry this allele may be at an increased risk of Stevens-Johnson Syndrome and toxic epidermal necrolysis when treated with oxcarbazepine.

Interaksi Makanan

2 Data
  • 1. Avoid alcohol. Oxcarbazepine has CNS depressant properties that may be potentiated by co-administration with alcohol.
  • 2. Take with or without food. Co-administration with food does not significantly affect absorption.

Interaksi Obat

1088 Data
Aripiprazole lauroxil The metabolism of Aripiprazole lauroxil can be increased when combined with Oxcarbazepine.
Aripiprazole The metabolism of Aripiprazole can be increased when combined with Oxcarbazepine.
Cilostazol The serum concentration of Cilostazol can be increased when it is combined with Oxcarbazepine.
Buprenorphine Oxcarbazepine 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 Oxcarbazepine.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Oxcarbazepine.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Oxcarbazepine.
Hydrocodone Oxcarbazepine 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 Oxcarbazepine.
Magnesium sulfate The therapeutic efficacy of Oxcarbazepine can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Oxcarbazepine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Oxcarbazepine may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Oxcarbazepine.
Mirtazapine Oxcarbazepine 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 Oxcarbazepine.
Orphenadrine Oxcarbazepine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Oxcarbazepine may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
Pramipexole Oxcarbazepine may increase the sedative activities of Pramipexole.
Ropinirole Oxcarbazepine may increase the sedative activities of Ropinirole.
Rotigotine Oxcarbazepine may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Oxcarbazepine.
Sodium oxybate Oxcarbazepine may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Oxcarbazepine 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 Oxcarbazepine.
Thalidomide Oxcarbazepine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Oxcarbazepine may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Ibrutinib The metabolism of Ibrutinib can be increased when combined with Oxcarbazepine.
Fentanyl The risk or severity of CNS depression can be increased when Oxcarbazepine is combined with Fentanyl.
Iloperidone The risk or severity of CNS depression can be increased when Oxcarbazepine is combined with Iloperidone.
Retapamulin The metabolism of Retapamulin can be increased when combined with Oxcarbazepine.
Vardenafil The metabolism of Vardenafil can be increased when combined with Oxcarbazepine.
Zopiclone The risk or severity of adverse effects can be increased when Oxcarbazepine is combined with Zopiclone.
Lovastatin The metabolism of Lovastatin can be increased when combined with Oxcarbazepine.
Mefloquine The therapeutic efficacy of Oxcarbazepine can be decreased when used in combination with Mefloquine.
Mianserin The therapeutic efficacy of Oxcarbazepine can be decreased when used in combination with Mianserin.
Orlistat Orlistat can cause a decrease in the absorption of Oxcarbazepine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Methyclothiazide The risk or severity of hyponatremia can be increased when Methyclothiazide is combined with Oxcarbazepine.
Chlorthalidone The risk or severity of hyponatremia can be increased when Chlorthalidone is combined with Oxcarbazepine.
Bendroflumethiazide The risk or severity of hyponatremia can be increased when Bendroflumethiazide is combined with Oxcarbazepine.
Metolazone The risk or severity of hyponatremia can be increased when Metolazone is combined with Oxcarbazepine.
Benzthiazide The risk or severity of hyponatremia can be increased when Benzthiazide is combined with Oxcarbazepine.
Hydroflumethiazide The risk or severity of hyponatremia can be increased when Hydroflumethiazide is combined with Oxcarbazepine.
Indapamide The risk or severity of hyponatremia can be increased when Indapamide is combined with Oxcarbazepine.
Chlorothiazide The risk or severity of hyponatremia can be increased when Chlorothiazide is combined with Oxcarbazepine.
Hydrochlorothiazide The risk or severity of hyponatremia can be increased when Hydrochlorothiazide is combined with Oxcarbazepine.
Trichlormethiazide The risk or severity of hyponatremia can be increased when Trichlormethiazide is combined with Oxcarbazepine.
Polythiazide The risk or severity of hyponatremia can be increased when Polythiazide is combined with Oxcarbazepine.
Quinethazone The risk or severity of hyponatremia can be increased when Quinethazone is combined with Oxcarbazepine.
Cyclopenthiazide The risk or severity of hyponatremia can be increased when Cyclopenthiazide is combined with Oxcarbazepine.
Epitizide The risk or severity of hyponatremia can be increased when Epitizide is combined with Oxcarbazepine.
Topotecan Oxcarbazepine may increase the excretion rate of Topotecan which could result in a lower serum level and potentially a reduction in efficacy.
Valproic acid The serum concentration of the active metabolites of Oxcarbazepine can be decreased when Oxcarbazepine is used in combination with Valproic acid.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Oxcarbazepine.
Alprazolam The risk or severity of CNS depression can be increased when Alprazolam is combined with Oxcarbazepine.
Carbamazepine The serum concentration of the active metabolites of Oxcarbazepine can be reduced when Oxcarbazepine is used in combination with Carbamazepine resulting in a loss in efficacy.
Ifosfamide The metabolism of Ifosfamide can be increased when combined with Oxcarbazepine.
Perampanel The metabolism of Perampanel can be increased when combined with Oxcarbazepine.
Warfarin The metabolism of Warfarin can be increased when combined with Oxcarbazepine.
Acenocoumarol The metabolism of Acenocoumarol can be increased when combined with Oxcarbazepine.
(R)-warfarin The metabolism of (R)-warfarin can be increased when combined with Oxcarbazepine.
R,S-Warfarin alcohol The metabolism of R,S-Warfarin alcohol can be increased when combined with Oxcarbazepine.
S,R-Warfarin alcohol The metabolism of S,R-Warfarin alcohol can be increased when combined with Oxcarbazepine.
(S)-Warfarin The metabolism of (S)-Warfarin can be increased when combined with Oxcarbazepine.
Midazolam The risk or severity of sedation and CNS depression can be increased when Midazolam is combined with Oxcarbazepine.
Cobicistat The metabolism of Cobicistat can be increased when combined with Oxcarbazepine.
Selegiline Oxcarbazepine may increase the serotonergic activities of Selegiline.
Tetracosactide The risk or severity of liver damage can be increased when Tetracosactide is combined with Oxcarbazepine.
Tacrolimus The metabolism of Tacrolimus can be increased when combined with Oxcarbazepine.
Atorvastatin The metabolism of Atorvastatin can be increased when combined with Oxcarbazepine.
Eslicarbazepine acetate The risk or severity of adverse effects can be increased when Oxcarbazepine is combined with Eslicarbazepine acetate.
Eslicarbazepine The risk or severity of adverse effects can be increased when Oxcarbazepine is combined with Eslicarbazepine.
Azelastine Oxcarbazepine 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 Oxcarbazepine.
Zimelidine The risk or severity of adverse effects can be increased when Oxcarbazepine is combined with Zimelidine.
Seproxetine The risk or severity of adverse effects can be increased when Oxcarbazepine is combined with Seproxetine.
Ritanserin The risk or severity of adverse effects can be increased when Oxcarbazepine is combined with Ritanserin.
Alaproclate The risk or severity of adverse effects can be increased when Oxcarbazepine is combined with Alaproclate.
Trazodone The risk or severity of adverse effects can be increased when Oxcarbazepine is combined with Trazodone.
Fluvoxamine The risk or severity of adverse effects can be increased when Oxcarbazepine is combined with Fluvoxamine.
Duloxetine The risk or severity of adverse effects can be increased when Oxcarbazepine is combined with Duloxetine.
Paroxetine The risk or severity of adverse effects can be increased when Oxcarbazepine is combined with Paroxetine.
Sertraline The risk or severity of adverse effects can be increased when Oxcarbazepine is combined with Sertraline.
Sibutramine The risk or severity of adverse effects can be increased when Oxcarbazepine is combined with Sibutramine.
Nefazodone The risk or severity of adverse effects can be increased when Oxcarbazepine is combined with Nefazodone.
Escitalopram The risk or severity of adverse effects can be increased when Oxcarbazepine is combined with Escitalopram.
Dapoxetine The risk or severity of adverse effects can be increased when Oxcarbazepine is combined with Dapoxetine.
Desvenlafaxine The risk or severity of adverse effects can be increased when Oxcarbazepine is combined with Desvenlafaxine.
Indalpine The risk or severity of adverse effects can be increased when Oxcarbazepine is combined with Indalpine.
Erlotinib The serum concentration of Erlotinib can be decreased when it is combined with Oxcarbazepine.
Ethanol Ethanol may increase the sedative activities of Oxcarbazepine.
Cyproheptadine The risk or severity of CNS depression can be increased when Cyproheptadine is combined with Oxcarbazepine.
Amoxapine The risk or severity of CNS depression can be increased when Amoxapine is combined with Oxcarbazepine.
Propiomazine The risk or severity of CNS depression can be increased when Oxcarbazepine is combined with Propiomazine.
Maprotiline The risk or severity of CNS depression can be increased when Oxcarbazepine is combined with Maprotiline.
Pizotifen The risk or severity of CNS depression can be increased when Oxcarbazepine is combined with Pizotifen.
Dosulepin The risk or severity of CNS depression can be increased when Oxcarbazepine is combined with Dosulepin.
Brompheniramine The risk or severity of CNS depression can be increased when Oxcarbazepine is combined with Brompheniramine.
Promazine The risk or severity of CNS depression can be increased when Promazine is combined with Oxcarbazepine.
Amitriptyline The risk or severity of CNS depression can be increased when Amitriptyline is combined with Oxcarbazepine.
Chlorpromazine The risk or severity of CNS depression can be increased when Chlorpromazine is combined with Oxcarbazepine.

Target Protein

Sodium channel protein type 11 subunit alpha SCN11A
Sodium channel protein SCN1A

Referensi & Sumber

Synthesis reference: Judith Aronhime, "New crystal forms of oxcarbazepine and processes for their preparation." U.S. Patent US20030004154, issued January 02, 2003.
Artikel (PubMed)
  • PMID: 25063510
    Malatkova P, Havlikova L, Wsol V: The role of carbonyl reducing enzymes in oxcarbazepine in vitro metabolism in man. Chem Biol Interact. 2014 Sep 5;220:241-7. doi: 10.1016/j.cbi.2014.07.005. Epub 2014 Jul 22.
  • PMID: 28528287
    Antunes NJ, van Dijkman SC, Lanchote VL, Wichert-Ana L, Coelho EB, Alexandre Junior V, Takayanagui OM, Tozatto E, van Hasselt JGC, Della Pasqua O: Population pharmacokinetics of oxcarbazepine and its metabolite 10-hydroxycarbazepine in healthy subjects. Eur J Pharm Sci. 2017 Nov 15;109S:S116-S123. doi: 10.1016/j.ejps.2017.05.034. Epub 2017 May 17.
  • PMID: 21692796
    Zhang C, Zuo Z, Kwan P, Baum L: In vitro transport profile of carbamazepine, oxcarbazepine, eslicarbazepine acetate, and their active metabolites by human P-glycoprotein. Epilepsia. 2011 Oct;52(10):1894-904. doi: 10.1111/j.1528-1167.2011.03140.x. Epub 2011 Jun 21.
  • PMID: 28842369
    Thomas AM, Atkinson TJ: Old Friends With New Faces: Are Sodium Channel Blockers the Future of Adjunct Pain Medication Management? J Pain. 2018 Jan;19(1):1-9. doi: 10.1016/j.jpain.2017.08.001. Epub 2017 Aug 24.
  • PMID: 10845729
    Shorvon S: Oxcarbazepine: a review. Seizure. 2000 Mar;9(2):75-9. doi: 10.1053/seiz.2000.0391.
  • PMID: 12737829
    Schmidt D, Sachdeo R: Oxcarbazepine for Treatment of Partial Epilepsy: A Review and Recommendations for Clinical Use. Epilepsy Behav. 2000 Dec;1(6):396-405. doi: 10.1006/ebeh.2000.0126.
  • PMID: 3765657
    Schutz H, Feldmann KF, Faigle JW, Kriemler HP, Winkler T: The metabolism of 14C-oxcarbazepine in man. Xenobiotica. 1986 Aug;16(8):769-78. doi: 10.3109/00498258609043567.
  • PMID: 26844734
    Abou-Khalil BW: Antiepileptic Drugs. Continuum (Minneap Minn). 2016 Feb;22(1 Epilepsy):132-56. doi: 10.1212/CON.0000000000000289.
Menampilkan 8 dari 9 artikel.

Contoh Produk & Brand

Produk: 213 • International brands: 15
Produk
  • Apo-oxcarbazepine
    Tablet • 150 mg • Oral • Canada • Generic • Approved
  • Apo-oxcarbazepine
    Tablet • 300 mg • Oral • Canada • Generic • Approved
  • Apo-oxcarbazepine
    Tablet • 600 mg • Oral • Canada • Generic • Approved
  • Jamp-oxcarbazepine
    Tablet • 150 mg • Oral • Canada • Generic • Approved
  • Jamp-oxcarbazepine
    Tablet • 300 mg • Oral • Canada • Generic • Approved
  • Jamp-oxcarbazepine
    Tablet • 600 mg • Oral • Canada • Generic • Approved
  • Novo-oxcarbazepine
    Tablet • 150 mg • Oral • Canada • Generic • Approved
  • Novo-oxcarbazepine
    Tablet • 300 mg • Oral • Canada • Generic • Approved
Menampilkan 8 dari 213 produk.
International Brands
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  • Carbox
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  • Oxpin
  • Oxrate
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