Armodafinil

DB06413

small molecule approved investigational

Deskripsi

Armodafinil is the enantiopure of the wakefulness-promoting agent modafinil (Provigil), and is indicated to improve wakefulness in adult patients with excessive sleepiness associated with obstructive sleep apnea (OSA), narcolepsy, or shift work disorder (SWD). Research has shown that armodafinil significantly improves driving simulator performance in patients with SWD. Armodafinil consists of the (?)-R-enantiomer of the racemic modafinil. Armodafinil is produced by the pharmaceutical company Cephalon Inc. (a wholly owned subsidiary of Teva Pharmaceutical Industries Ltd.) and was approved by the U.S. Food and Drug Administration (FDA) in June 2007.

Struktur Molekul 2D

Berat 273.35
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Terminal half-life is approximately 15 hours.
Volume Distribusi Apparent volume of distribution: 42L.
Klirens (Clearance) The oral clearance of armodafinil is approximately 33 mL/min.

Absorpsi

Tmax is 2 hours when fasted and can be delayed approximately 2-4 hours by food, potentially affecting the onset of action.

Metabolisme

In vitro and in vivo data show that armodafinil undergoes hydrolytic deamidation, S-oxidation, and aromatic ring hydroxylation, with subsequent glucuronide conjugation of the hydroxylated products. Amide hydrolysis is the single most prominent metabolic pathway, with sulfone formation by cytochrome P450 (CYP) 3A4/5 being next in importance. The other oxidative products are formed too slowly in vitro to enable identification of the enzyme(s) responsible. Only two metabolites reach appreciable concentrations in plasma (i.e., R-modafinil acid and modafinil sulfone). Data specific to armodafinil disposition are not available.

Rute Eliminasi

Data eliminasi belum tersedia.

Interaksi Makanan

4 Data
  • 1. Avoid alcohol.
  • 2. Exercise caution with grapefruit products. Armodafinil is partially metabolized by CYP3A4, and grapefruit is a CYP3A4 inhibitor.
  • 3. Exercise caution with St. John's Wort. Armodafinil is partially metabolized by CYP3A4, and St. John's Wort is a CYP3A4 inducer.
  • 4. Take with or without food. Taking armodafinil with food can delay the Tmax by 2-4 hours.

Interaksi Obat

661 Data
Dofetilide The metabolism of Dofetilide can be increased when combined with Armodafinil.
Theophylline The metabolism of Theophylline can be increased when combined with Armodafinil.
Carbamazepine The metabolism of Carbamazepine can be increased when combined with Armodafinil.
Warfarin The metabolism of Warfarin can be increased when combined with Armodafinil.
Tacrolimus The metabolism of Tacrolimus can be increased when combined with Armodafinil.
Sirolimus The metabolism of Sirolimus can be increased when combined with Armodafinil.
Quinidine The metabolism of Quinidine can be increased when combined with Armodafinil.
Phenprocoumon The metabolism of Phenprocoumon can be increased when combined with Armodafinil.
Busulfan The metabolism of Busulfan can be increased when combined with Armodafinil.
Pimozide The metabolism of Pimozide can be increased when combined with Armodafinil.
Amiodarone The metabolism of Amiodarone can be increased when combined with Armodafinil.
Aminophylline The metabolism of Aminophylline can be increased when combined with Armodafinil.
Paclitaxel The metabolism of Paclitaxel can be increased when combined with Armodafinil.
Dasatinib The metabolism of Dasatinib can be increased when combined with Armodafinil.
Fosphenytoin The metabolism of Fosphenytoin can be increased when combined with Armodafinil.
Digitoxin The metabolism of Digitoxin can be increased when combined with Armodafinil.
Acenocoumarol The metabolism of Acenocoumarol can be increased when combined with Armodafinil.
Everolimus The metabolism of Everolimus can be increased when combined with Armodafinil.
Dronedarone The metabolism of Dronedarone can be increased when combined with Armodafinil.
Temsirolimus The metabolism of Temsirolimus can be increased when combined with Armodafinil.
Tianeptine The metabolism of Tianeptine can be increased when combined with Armodafinil.
Sorafenib The metabolism of Sorafenib can be increased when combined with Armodafinil.
Teniposide The metabolism of Teniposide can be increased when combined with Armodafinil.
Vincristine The metabolism of Vincristine can be increased when combined with Armodafinil.
Irinotecan The metabolism of Irinotecan can be increased when combined with Armodafinil.
Etoposide The metabolism of Etoposide can be increased when combined with Armodafinil.
Docetaxel The metabolism of Docetaxel can be increased when combined with Armodafinil.
Sunitinib The metabolism of Sunitinib can be increased when combined with Armodafinil.
Trastuzumab emtansine The metabolism of Trastuzumab emtansine can be increased when combined with Armodafinil.
Romidepsin The metabolism of Romidepsin can be increased when combined with Armodafinil.
Cabazitaxel The metabolism of Cabazitaxel can be increased when combined with Armodafinil.
Crizotinib The metabolism of Crizotinib can be increased when combined with Armodafinil.
Ponatinib The metabolism of Ponatinib can be increased when combined with Armodafinil.
Olaparib The metabolism of Olaparib can be increased when combined with Armodafinil.
Copanlisib The metabolism of Copanlisib can be increased when combined with Armodafinil.
Bortezomib The metabolism of Bortezomib can be increased when combined with Armodafinil.
Trabectedin The metabolism of Trabectedin can be increased when combined with Armodafinil.
Dacomitinib The metabolism of Dacomitinib can be increased when combined with Armodafinil.
Erdafitinib The metabolism of Erdafitinib can be increased when combined with Armodafinil.
Enasidenib The metabolism of Enasidenib can be increased when combined with Armodafinil.
Cobimetinib The metabolism of Cobimetinib can be increased when combined with Armodafinil.
Ceritinib The metabolism of Ceritinib can be increased when combined with Armodafinil.
Osimertinib The metabolism of Osimertinib can be increased when combined with Armodafinil.
Ribociclib The metabolism of Ribociclib can be increased when combined with Armodafinil.
Alpelisib The metabolism of Alpelisib can be increased when combined with Armodafinil.
Pazopanib The metabolism of Pazopanib can be increased when combined with Armodafinil.
Pomalidomide The metabolism of Pomalidomide can be increased when combined with Armodafinil.
Astemizole The metabolism of Astemizole can be increased when combined with Armodafinil.
Lomitapide The metabolism of Lomitapide can be increased when combined with Armodafinil.
Siponimod The metabolism of Siponimod can be increased when combined with Armodafinil.
Clonidine The metabolism of Clonidine can be increased when combined with Armodafinil.
Methotrexate The metabolism of Methotrexate can be increased when combined with Armodafinil.
Vinorelbine The metabolism of Vinorelbine can be increased when combined with Armodafinil.
Vinblastine The metabolism of Vinblastine can be increased when combined with Armodafinil.
Doxorubicin The serum concentration of Doxorubicin can be decreased when it is combined with Armodafinil.
Thiotepa The metabolism of Thiotepa can be increased when combined with Armodafinil.
Vandetanib The metabolism of Vandetanib can be increased when combined with Armodafinil.
Vemurafenib The metabolism of Vemurafenib can be increased when combined with Armodafinil.
Alectinib The metabolism of Alectinib can be increased when combined with Armodafinil.
Venetoclax The metabolism of Venetoclax can be increased when combined with Armodafinil.
Vinflunine The metabolism of Vinflunine can be increased when combined with Armodafinil.
Acalabrutinib The metabolism of Acalabrutinib can be increased when combined with Armodafinil.
Zanubrutinib The metabolism of Zanubrutinib can be increased when combined with Armodafinil.
Cabergoline The metabolism of Cabergoline can be increased when combined with Armodafinil.
Vindesine The metabolism of Vindesine can be increased when combined with Armodafinil.
Ixabepilone The metabolism of Ixabepilone can be increased when combined with Armodafinil.
Nilotinib The metabolism of Nilotinib can be increased when combined with Armodafinil.
Midostaurin The metabolism of Midostaurin can be increased when combined with Armodafinil.
Panobinostat The metabolism of Panobinostat can be increased when combined with Armodafinil.
Bosutinib The metabolism of Bosutinib can be increased when combined with Armodafinil.
Brentuximab vedotin The metabolism of Brentuximab vedotin can be increased when combined with Armodafinil.
Ruxolitinib The metabolism of Ruxolitinib can be increased when combined with Armodafinil.
Dabrafenib The metabolism of Dabrafenib can be increased when combined with Armodafinil.
Palbociclib The metabolism of Palbociclib can be increased when combined with Armodafinil.
Sonidegib The metabolism of Sonidegib can be increased when combined with Armodafinil.
Neratinib The metabolism of Neratinib can be increased when combined with Armodafinil.
Brigatinib The metabolism of Brigatinib can be increased when combined with Armodafinil.
Pexidartinib The metabolism of Pexidartinib can be increased when combined with Armodafinil.
Ivosidenib The metabolism of Ivosidenib can be increased when combined with Armodafinil.
Idelalisib The metabolism of Idelalisib can be increased when combined with Armodafinil.
Ixazomib The metabolism of Ixazomib can be increased when combined with Armodafinil.
Tolvaptan The metabolism of Tolvaptan can be increased when combined with Armodafinil.
Regorafenib The metabolism of Regorafenib can be increased when combined with Armodafinil.
Abemaciclib The metabolism of Abemaciclib can be increased when combined with Armodafinil.
Dihydroergotamine The metabolism of Dihydroergotamine can be increased when combined with Armodafinil.
Ergotamine The metabolism of Ergotamine can be increased when combined with Armodafinil.
Conivaptan The metabolism of Conivaptan can be increased when combined with Armodafinil.
Bicalutamide The metabolism of Bicalutamide can be increased when combined with Armodafinil.
Nortriptyline The metabolism of Nortriptyline can be increased when combined with Armodafinil.
Levacetylmethadol The metabolism of Levacetylmethadol can be increased when combined with Armodafinil.
Cyclosporine The serum concentration of Cyclosporine can be decreased when it is combined with Armodafinil.
Aripiprazole The metabolism of Aripiprazole can be increased when combined with Armodafinil.
Aripiprazole lauroxil The metabolism of Aripiprazole lauroxil can be increased when combined with Armodafinil.
Cilostazol The serum concentration of Cilostazol can be increased when it is combined with Armodafinil.
Citalopram The serum concentration of Citalopram can be increased when it is combined with Armodafinil.
Clopidogrel The serum concentration of the active metabolites of Clopidogrel can be reduced when Clopidogrel is used in combination with Armodafinil resulting in a loss in efficacy.
Ifosfamide The metabolism of Ifosfamide can be increased when combined with Armodafinil.
Perampanel The metabolism of Perampanel can be increased when combined with Armodafinil.
R,S-Warfarin alcohol The metabolism of R,S-Warfarin alcohol can be increased when combined with Armodafinil.
S,R-Warfarin alcohol The metabolism of S,R-Warfarin alcohol can be increased when combined with Armodafinil.

Target Protein

Alpha-1D adrenergic receptor ADRA1D
Sodium-dependent dopamine transporter SLC6A3

Referensi & Sumber

Synthesis reference: http://www.google.com/patents/EP2649187A2?cl=en http://www.google.com/patents/US20100036164
Artikel (PubMed)
  • PMID: 18363520
    Lankford DA: Armodafinil: a new treatment for excessive sleepiness. Expert Opin Investig Drugs. 2008 Apr;17(4):565-73. doi: 10.1517/13543784.17.4.565 .
  • PMID: 25325498
    Drake C, Gumenyuk V, Roth T, Howard R: Effects of armodafinil on simulated driving and alertness in shift work disorder. Sleep. 2014 Dec 1;37(12):1987-94. doi: 10.5665/sleep.4256.
Link

Contoh Produk & Brand

Produk: 67 • International brands: 1
Produk
  • Armodafinil
    Tablet • 150 mg/1 • Oral • US • Generic • Approved
  • Armodafinil
    Tablet • 150 mg/1 • Oral • US • Generic • Approved
  • Armodafinil
    Tablet • 250 mg/1 • Oral • US • Generic • Approved
  • Armodafinil
    Tablet • 150 mg/1 • Oral • US • Generic • Approved
  • Armodafinil
    Tablet • 50 mg/1 • Oral • US • Generic • Approved
  • Armodafinil
    Tablet • 150 mg/1 • Oral • US • Generic • Approved
  • Armodafinil
    Tablet • 200 mg/1 • Oral • US • Generic • Approved
  • Armodafinil
    Tablet • 250 mg/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 67 produk.
International Brands
  • Neoresotyl — Drugtech

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