Peringatan Keamanan

The most commonly reported adverse reactions to idebenone are mild to moderate diarrhoea (usually not requiring the discontinuation of the treatment), nasopharyngitis, cough and back pain FDA Label.

Idebenone

DB09081

small molecule approved investigational

Deskripsi

Idebenone is a synthetic analogue of ubiquinone (also known as Coenzyme Q10), a vital cell antioxidant and essential component of the Electron Transport Chain (ETC). It has been proposed that by interacting with the ETC, idebenone increases ATP production required for mitochondrial function, reduces free radicals, inhibits lipid peroxidation, and consequently protects the lipid membrane and mitochondria from oxidative damage A19768. More specifically, idebenone is thought to transfer electrons directly to complex III of the mitochondrial ETC, thereby circumventing complex I and restoring cellular energy (ATP) generation L885.

Due to its ability to reduce oxidative damage and improve ATP production, idebenone was originally investigated for its potential use in Alzheimer's Disease and other cognitivie disorders A19769. Lack of improvement in cognitive function halted its production for these conditions, however it continues to be investigated for use in other conditions associated with mitochondrial damage.

Idebenone is currently only indicated for use by the European Medicines Agency (EMA) for the treatment of visual impairment in adolescent and adult patients with
Leber’s Hereditary Optic Neuropathy (LHON). LHON is a mitochondrially inherited degeneration of retinal ganglion cells, resulting in acute central vision loss. Due to its biochemical mode of action, it's thought that idebenone may re-activate viable-but-inactive retinal ganglion cells (RGCs) in LHON patients L885. It is not currently approved for use by either the Food and Drug Administration (USA) or Health Canada.

Struktur Molekul 2D

Berat 338.444
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) -
Volume Distribusi Experimental data have shown that idebenone passes the blood-brain barrier and is distributed at significant concentrations in cerebral tissue. Following oral administration pharmacologically relevant concentrations of idebenone are detectable in the aqueous humor of the eye [L885].
Klirens (Clearance) -

Absorpsi

After oral administration, idebenone is rapidly absorbed. On repeat dosing, maximum plasma concentrations of idebenone are reached on average within 1 hour (median 0.67 h range: 0.33-2.00 h). Food increases the bioavailability of idebenone by approximately 5-7-fold and i therefore should always be administered with food L885.

Metabolisme

Metabolism occurs by means of oxidative shortening of the side chain and by reduction of the quinone ring and conjugation to glucuronides and sulphates. Idebenone shows a high first pass metabolism resulting in conjugates of idebenone (glucuronides and sulphates (IDE-C)) and the Phase I metabolites QS10, QS6, and QS4 as well as their corresponding Phase II metabolites (glucuronides and sulphates (QS10+QS10-C, QS6+QS6-C, QS4+QS4-C)). The main metabolites in plasma are IDE-C and QS4+QS4-C L885.

Rute Eliminasi

The main route of elimination is metabolism, with the majority of dose excreted via the kidneys as metabolites. After a single or repeated oral dose of 750 mg of idebenone, QS4+QS4-C were the most prominent idebenone-derived metabolites in urine, representing on average between 49.3% and 68.3% of the total administered dose. QS6+QS6 represented 6.45% to 9.46%, whereas QS10+QS10-C and IDE+IDE-C were close to 1% or below L885.

Interaksi Makanan

1 Data
  • 1. Take with food.

Interaksi Obat

726 Data
Cyclosporine Cyclosporine may decrease the excretion rate of Idebenone which could result in a higher serum level.
Icosapent Icosapent may decrease the excretion rate of Idebenone which could result in a higher serum level.
Cefotiam Cefotiam may decrease the excretion rate of Idebenone which could result in a higher serum level.
Mesalazine Mesalazine may decrease the excretion rate of Idebenone which could result in a higher serum level.
Cefmenoxime Cefmenoxime may decrease the excretion rate of Idebenone which could result in a higher serum level.
Cefmetazole Cefmetazole may decrease the excretion rate of Idebenone which could result in a higher serum level.
Pamidronic acid Pamidronic acid may decrease the excretion rate of Idebenone which could result in a higher serum level.
Tenofovir disoproxil Tenofovir disoproxil may decrease the excretion rate of Idebenone which could result in a higher serum level.
Indomethacin Indomethacin may decrease the excretion rate of Idebenone which could result in a higher serum level.
Cidofovir Cidofovir may decrease the excretion rate of Idebenone which could result in a higher serum level.
Cefpiramide Cefpiramide may decrease the excretion rate of Idebenone which could result in a higher serum level.
Ceftazidime Ceftazidime may decrease the excretion rate of Idebenone which could result in a higher serum level.
Loracarbef Loracarbef may decrease the excretion rate of Idebenone which could result in a higher serum level.
Cefalotin Cefalotin may decrease the excretion rate of Idebenone which could result in a higher serum level.
Nabumetone Nabumetone may decrease the excretion rate of Idebenone which could result in a higher serum level.
Ketorolac Ketorolac may decrease the excretion rate of Idebenone which could result in a higher serum level.
Tenoxicam Tenoxicam may decrease the excretion rate of Idebenone which could result in a higher serum level.
Celecoxib Celecoxib may decrease the excretion rate of Idebenone which could result in a higher serum level.
Cefotaxime Cefotaxime may decrease the excretion rate of Idebenone which could result in a higher serum level.
Tolmetin Tolmetin may decrease the excretion rate of Idebenone which could result in a higher serum level.
Foscarnet Foscarnet may decrease the excretion rate of Idebenone which could result in a higher serum level.
Rofecoxib Rofecoxib may decrease the excretion rate of Idebenone which could result in a higher serum level.
Piroxicam Piroxicam may decrease the excretion rate of Idebenone which could result in a higher serum level.
Methotrexate Methotrexate may decrease the excretion rate of Idebenone which could result in a higher serum level.
Cephalexin Cephalexin may decrease the excretion rate of Idebenone which could result in a higher serum level.
Fenoprofen Fenoprofen may decrease the excretion rate of Idebenone which could result in a higher serum level.
Valaciclovir Valaciclovir may decrease the excretion rate of Idebenone which could result in a higher serum level.
Valdecoxib Valdecoxib may decrease the excretion rate of Idebenone which could result in a higher serum level.
Diclofenac Diclofenac may decrease the excretion rate of Idebenone which could result in a higher serum level.
Sulindac Sulindac may decrease the excretion rate of Idebenone which could result in a higher serum level.
Bacitracin Bacitracin may decrease the excretion rate of Idebenone which could result in a higher serum level.
Amphotericin B Amphotericin B may decrease the excretion rate of Idebenone which could result in a higher serum level.
Cephaloglycin Cephaloglycin may decrease the excretion rate of Idebenone which could result in a higher serum level.
Flurbiprofen Flurbiprofen may decrease the excretion rate of Idebenone which could result in a higher serum level.
Adefovir dipivoxil Adefovir dipivoxil may decrease the excretion rate of Idebenone which could result in a higher serum level.
Pentamidine Pentamidine may decrease the excretion rate of Idebenone which could result in a higher serum level.
Etodolac Etodolac may decrease the excretion rate of Idebenone which could result in a higher serum level.
Mefenamic acid Mefenamic acid may decrease the excretion rate of Idebenone which could result in a higher serum level.
Acyclovir Acyclovir may decrease the excretion rate of Idebenone which could result in a higher serum level.
Naproxen Naproxen may decrease the excretion rate of Idebenone which could result in a higher serum level.
Sulfasalazine Sulfasalazine may decrease the excretion rate of Idebenone which could result in a higher serum level.
Phenylbutazone Phenylbutazone may decrease the excretion rate of Idebenone which could result in a higher serum level.
Meloxicam Meloxicam may decrease the excretion rate of Idebenone which could result in a higher serum level.
Carprofen Carprofen may decrease the excretion rate of Idebenone which could result in a higher serum level.
Cefaclor Cefaclor may decrease the excretion rate of Idebenone which could result in a higher serum level.
Diflunisal Diflunisal may decrease the excretion rate of Idebenone which could result in a higher serum level.
Tacrolimus Tacrolimus may decrease the excretion rate of Idebenone which could result in a higher serum level.
Ceforanide Ceforanide may decrease the excretion rate of Idebenone which could result in a higher serum level.
Salicylic acid Salicylic acid may decrease the excretion rate of Idebenone which could result in a higher serum level.
Meclofenamic acid Meclofenamic acid may decrease the excretion rate of Idebenone which could result in a higher serum level.
Acetylsalicylic acid Acetylsalicylic acid may decrease the excretion rate of Idebenone which could result in a higher serum level.
Carboplatin Carboplatin may decrease the excretion rate of Idebenone which could result in a higher serum level.
Oxaprozin Oxaprozin may decrease the excretion rate of Idebenone which could result in a higher serum level.
Ketoprofen Ketoprofen may decrease the excretion rate of Idebenone which could result in a higher serum level.
Balsalazide Balsalazide may decrease the excretion rate of Idebenone which could result in a higher serum level.
Ibuprofen Ibuprofen may decrease the excretion rate of Idebenone which could result in a higher serum level.
Cefditoren Cefditoren may decrease the excretion rate of Idebenone which could result in a higher serum level.
Atazanavir Atazanavir may decrease the excretion rate of Idebenone which could result in a higher serum level.
Colistimethate Colistimethate may decrease the excretion rate of Idebenone which could result in a higher serum level.
Cefuroxime Cefuroxime may decrease the excretion rate of Idebenone which could result in a higher serum level.
Cefapirin Cefapirin may decrease the excretion rate of Idebenone which could result in a higher serum level.
Cefadroxil Cefadroxil may decrease the excretion rate of Idebenone which could result in a higher serum level.
Cefprozil Cefprozil may decrease the excretion rate of Idebenone which could result in a higher serum level.
Ceftriaxone Ceftriaxone may decrease the excretion rate of Idebenone which could result in a higher serum level.
Olsalazine Olsalazine may decrease the excretion rate of Idebenone which could result in a higher serum level.
Lumiracoxib Lumiracoxib may decrease the excretion rate of Idebenone which could result in a higher serum level.
Cefamandole Cefamandole may decrease the excretion rate of Idebenone which could result in a higher serum level.
Cefazolin Cefazolin may decrease the excretion rate of Idebenone which could result in a higher serum level.
Cefonicid Cefonicid may decrease the excretion rate of Idebenone which could result in a higher serum level.
Cefoperazone Cefoperazone may decrease the excretion rate of Idebenone which could result in a higher serum level.
Cefotetan Cefotetan may decrease the excretion rate of Idebenone which could result in a higher serum level.
Cefoxitin Cefoxitin may decrease the excretion rate of Idebenone which could result in a higher serum level.
Ceftizoxime Ceftizoxime may decrease the excretion rate of Idebenone which could result in a higher serum level.
Cefradine Cefradine may decrease the excretion rate of Idebenone which could result in a higher serum level.
Magnesium salicylate Magnesium salicylate may decrease the excretion rate of Idebenone which could result in a higher serum level.
Salsalate Salsalate may decrease the excretion rate of Idebenone which could result in a higher serum level.
Choline magnesium trisalicylate Choline magnesium trisalicylate may decrease the excretion rate of Idebenone which could result in a higher serum level.
Cefepime Cefepime may decrease the excretion rate of Idebenone which could result in a higher serum level.
Cefacetrile Cefacetrile may decrease the excretion rate of Idebenone which could result in a higher serum level.
Ceftibuten Ceftibuten may decrease the excretion rate of Idebenone which could result in a higher serum level.
Cefpodoxime Cefpodoxime may decrease the excretion rate of Idebenone which could result in a higher serum level.
Antrafenine Antrafenine may decrease the excretion rate of Idebenone which could result in a higher serum level.
Aminophenazone Aminophenazone may decrease the excretion rate of Idebenone which could result in a higher serum level.
Antipyrine Antipyrine may decrease the excretion rate of Idebenone which could result in a higher serum level.
Tiaprofenic acid Tiaprofenic acid may decrease the excretion rate of Idebenone which could result in a higher serum level.
Lopinavir Lopinavir may decrease the excretion rate of Idebenone which could result in a higher serum level.
Etoricoxib Etoricoxib may decrease the excretion rate of Idebenone which could result in a higher serum level.
Hydrolyzed Cephalothin Hydrolyzed Cephalothin may decrease the excretion rate of Idebenone which could result in a higher serum level.
Cephalothin Group Cephalothin Group may decrease the excretion rate of Idebenone which could result in a higher serum level.
Oxyphenbutazone Oxyphenbutazone may decrease the excretion rate of Idebenone which could result in a higher serum level.
Latamoxef Latamoxef may decrease the excretion rate of Idebenone which could result in a higher serum level.
Nimesulide Nimesulide may decrease the excretion rate of Idebenone which could result in a higher serum level.
Benoxaprofen Benoxaprofen may decrease the excretion rate of Idebenone which could result in a higher serum level.
Metamizole Metamizole may decrease the excretion rate of Idebenone which could result in a higher serum level.
Zomepirac Zomepirac may decrease the excretion rate of Idebenone which could result in a higher serum level.
Ceftobiprole Ceftobiprole may decrease the excretion rate of Idebenone which could result in a higher serum level.
Cimicoxib Cimicoxib may decrease the excretion rate of Idebenone which could result in a higher serum level.
Ceftaroline fosamil Ceftaroline fosamil may decrease the excretion rate of Idebenone which could result in a higher serum level.
Lornoxicam Lornoxicam may decrease the excretion rate of Idebenone which could result in a higher serum level.
Aceclofenac Aceclofenac may decrease the excretion rate of Idebenone which could result in a higher serum level.

Referensi & Sumber

Artikel (PubMed)
  • PMID: 19125241
    Bodmer M, Vankan P, Dreier M, Kutz KW, Drewe J: Pharmacokinetics and metabolism of idebenone in healthy male subjects. Eur J Clin Pharmacol. 2009 May;65(5):493-501. doi: 10.1007/s00228-008-0596-1. Epub 2009 Jan 6.
  • PMID: 15374467
    Zs -Nagy I: Chemistry, toxicology, pharmacology and pharmacokinetics of idebenone: a review. Arch Gerontol Geriatr. 1990 Nov-Dec;11(3):177-86.
  • PMID: 7981485
    Gillis JC, Benefield P, McTavish D: Idebenone. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic use in age-related cognitive disorders. Drugs Aging. 1994 Aug;5(2):133-52.

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