Peringatan Keamanan

LD50, oral, mouse = 19 mg/kg
LD50, oral, rat = 21 mg/kg

Dalfampridine

DB06637

small molecule approved

Deskripsi

Dalfampridine is a potassium channel blocker used to help multiple sclerosis patients walk. This is the first drug that was specifically approved to help with mobility in these patients. FDA approved on January 22, 2010.

Struktur Molekul 2D

Berat 94.1145
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Immediate release form = 3.5 hours; Extended release form = 5.47 hours;
Volume Distribusi 10 mg extended release = 2.6 L/kg
Klirens (Clearance) -

Absorpsi

Orally-administered dalfampridine is rapidly and completely absorbed from the gastrointestinal tract. Tmax, immediate release form = 1 hour; Tmax, extended release form = 3.5 hours; Cmax, 10 mg extended release = 17.3 - 21.6 ng/mL; Relative bioavailability of 10 mg extended-release tablets compared to aqueous oral solution = 96%

Metabolisme

Not extensively metabolized by the liver therefore drugs effecting the cytochrome P450 enzyme system that are concomitantly administered with dalfampridine are not expected to interact with each other. Metabolites include 3-hydroxy-4-aminopyridine and 3-hydroxy-4-aminopyridine sulfate and both are inactive. CYP2E1 is the enzyme responsible for 3-hydroxylation of dalfampridine.

Rute Eliminasi

Almost all of the dose and its metabolites are completely eliminated by the kidneys after 24 hours. Urine (96%; 90% of total dose as unchanged drug); Feces (0.5%)

Interaksi Makanan

1 Data
  • 1. Take with or without food. High-fat meals increase drug absorption, but not to a clinically significant extent.

Interaksi Obat

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

Target Protein

Potassium voltage-gated channel subfamily A member 1 KCNA1
Potassium voltage-gated channel subfamily A member 2 KCNA2
Potassium voltage-gated channel subfamily A member 3 KCNA3
Potassium voltage-gated channel subfamily A member 4 KCNA4
Potassium voltage-gated channel subfamily A member 5 KCNA5
Potassium voltage-gated channel subfamily A member 6 KCNA6
Potassium voltage-gated channel subfamily A member 7 KCNA7
Potassium voltage-gated channel subfamily A member 10 KCNA10
Potassium voltage-gated channel subfamily B member 1 KCNB1
Potassium voltage-gated channel subfamily B member 2 KCNB2
Voltage-gated potassium channel KCNC1 KCNC1
Voltage-gated potassium channel KCNC2 KCNC2
Voltage-gated potassium channel KCNC3 KCNC3
A-type voltage-gated potassium channel KCND1 KCND1
A-type voltage-gated potassium channel KCND2 KCND2
A-type voltage-gated potassium channel KCND3 KCND3

Referensi & Sumber

Synthesis reference: Fabio GARAVAGLIA, Alessandro BAROZZA, Jacopo ROLETTO, Paolo PAISSONI, "ONE-POT PROCESS FOR THE SYNTHESIS OF DALFAMPRIDINE." U.S. Patent US20110319628, issued December 29, 2011.
Artikel (PubMed)
  • PMID: 21635193
    Panitch H, Applebee A: Treatment of walking impairment in multiple sclerosis: an unmet need for a disease-specific disability. Expert Opin Pharmacother. 2011 Jul;12(10):1511-21. doi: 10.1517/14656566.2011.586338. Epub 2011 Jun 2.
  • PMID: 22764324
    Pikoulas TE, Fuller MA: Dalfampridine: a medication to improve walking in patients with multiple sclerosis. Ann Pharmacother. 2012 Jul-Aug;46(7-8):1010-5. doi: 10.1345/aph.1Q714. Epub 2012 Jul 3.
  • PMID: 22497693
    Cornblath DR, Bienen EJ, Blight AR: The safety profile of dalfampridine extended release in multiple sclerosis clinical trials. Clin Ther. 2012 May;34(5):1056-69. doi: 10.1016/j.clinthera.2012.03.007. Epub 2012 Apr 11.
  • PMID: 22135060
    McDonald S, Clements JN: Dalfampridine: a new agent for symptomatic management of multiple sclerosis. Am J Health Syst Pharm. 2011 Dec 15;68(24):2335-40. doi: 10.2146/ajhp110134.
  • PMID: 16472864
    Judge SI, Bever CT Jr: Potassium channel blockers in multiple sclerosis: neuronal Kv channels and effects of symptomatic treatment. Pharmacol Ther. 2006 Jul;111(1):224-59. Epub 2006 Feb 9.

Contoh Produk & Brand

Produk: 23 • International brands: 2
Produk
  • Ampyra
    Tablet, film coated, extended release • 10 mg/1 • Oral • US • Approved
  • Ampyra
    Tablet, film coated, extended release • 10 mg/1 • Oral • US • Approved
  • Dalfampridine
    Tablet, extended release • 10 mg/1 • Oral • US • Generic • Approved
  • Dalfampridine
    Tablet, film coated, extended release • 10 mg/1 • Oral • US • Generic • Approved
  • Dalfampridine
    Tablet, film coated, extended release • 10 mg/1 • Oral • US • Generic • Approved
  • Dalfampridine
    Tablet, film coated, extended release • 10 mg/1 • Oral • US • Generic • Approved
  • Dalfampridine
    Tablet, film coated, extended release • 10 mg/1 • Oral • US • Generic • Approved
  • Dalfampridine
    Tablet, extended release • 10 mg/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 23 produk.
International Brands
  • Avitrol
  • Fampridine-SR

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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