Peringatan Keamanan

uncontrolled involuntary movement, falls, nausea, and trouble sleeping or falling asleep (insomnia)
Patients who have an overdose may experience hypertension (high blood pressure), orthostatic hypotension, hallucinations, psychomotor agitation, nausea, vomiting, and dyskinesia.

Safinamide

DB06654

small molecule approved investigational

Deskripsi

Safinamide is for the treatment of parkinson's disease. It was approved in Europe in February 2015, and in the United States on March 21, 2017.

Struktur Molekul 2D

Berat 302.349
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) 22 h
Volume Distribusi 1.8 litres/kg
Klirens (Clearance) total oral clearance of plasma , which accounts for parent safinamide as well as metabolites, was on average only 17.53 ± 2.71 ml/h × kg

Absorpsi

Rapid with peak plasma concentrations ranging from 2 to 4 h, total bioavailability is 95%. Food prolonged the rate and did not affect the extent of absorption of safinamide.

Metabolisme

The principal step is mediated by amidases which have not been identified, and produces safinamide acid. It is also metabolized to O-debenzylated safinamide and N-delkylated amine. The N-dealkylated amine is then oxidized to a carboxylic acid and finally glucuronidated. Dealkylation reactions are mediated by cytochrome P450s (CYPs), especially CYP3A4. Safinamide acid binds to organic anion transporter 3 (OAT3), but no clinical relevance of this interaction has been determined. Safinamide also binds to ABCG2 transiently. No other transporter affinities have been found in preliminary studies.

Rute Eliminasi

76% renal, 1.5% faeces

Interaksi Makanan

5 Data
  • 1. Avoid excessive or chronic alcohol consumption. Ingesting alcohol may increase the sedative effects of safinamide.
  • 2. Avoid St. John's Wort. This herb may increase the risk of serotonin syndrome, and therefore, concomitant use is contraindicated.
  • 3. Avoid tyramine-containing foods and supplements. Avoid foods containing high amounts of tyramine (>150mg) as these foods may cause a significant elevation in blood pressure. Tyramine-containing foods include cheese, red wine, fava beans, pickled food, cured food, and alcoholic beverages.
  • 4. Take at the same time every day.
  • 5. Take with or without food.

Interaksi Obat

1478 Data
Cilostazol The serum concentration of Cilostazol can be increased when it is combined with Safinamide.
Doxylamine Doxylamine may increase the central nervous system depressant (CNS depressant) activities of Safinamide.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Safinamide.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Safinamide.
Hydroxyzine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Safinamide.
Magnesium sulfate The therapeutic efficacy of Safinamide can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Safinamide may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Safinamide may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Safinamide.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Safinamide.
Orphenadrine Safinamide may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Safinamide may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
Perampanel Perampanel may increase the central nervous system depressant (CNS depressant) activities of Safinamide.
Pramipexole Safinamide may increase the sedative activities of Pramipexole.
Rotigotine Safinamide may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Safinamide.
Sodium oxybate Safinamide may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Safinamide may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Thalidomide Safinamide may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Safinamide may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Desmopressin The risk or severity of hypertension can be increased when Desmopressin is combined with Safinamide.
Icosapent The risk or severity of hypertension can be increased when Icosapent is combined with Safinamide.
Mesalazine The risk or severity of hypertension can be increased when Mesalazine is combined with Safinamide.
Tolmetin The risk or severity of hypertension can be increased when Tolmetin is combined with Safinamide.
Fenoprofen The risk or severity of hypertension can be increased when Fenoprofen is combined with Safinamide.
Sulindac The risk or severity of hypertension can be increased when Sulindac is combined with Safinamide.
Carprofen The risk or severity of hypertension can be increased when Carprofen is combined with Safinamide.
Phenmetrazine The risk or severity of hypertension can be increased when Phenmetrazine is combined with Safinamide.
Diflunisal The risk or severity of hypertension can be increased when Diflunisal is combined with Safinamide.
Meclofenamic acid The risk or severity of hypertension can be increased when Meclofenamic acid is combined with Safinamide.
Oxaprozin The risk or severity of hypertension can be increased when Oxaprozin is combined with Safinamide.
Balsalazide The risk or severity of hypertension can be increased when Balsalazide is combined with Safinamide.
Ephedrine The risk or severity of hypertension can be increased when Ephedrine is combined with Safinamide.
Magnesium salicylate The risk or severity of hypertension can be increased when Magnesium salicylate is combined with Safinamide.
Salsalate The risk or severity of hypertension can be increased when Salsalate is combined with Safinamide.
Choline magnesium trisalicylate The risk or severity of hypertension can be increased when Choline magnesium trisalicylate is combined with Safinamide.
Antrafenine The risk or severity of hypertension can be increased when Antrafenine is combined with Safinamide.
Tiaprofenic acid The risk or severity of hypertension can be increased when Tiaprofenic acid is combined with Safinamide.
Epicaptopril The risk or severity of hypertension can be increased when Epicaptopril is combined with Safinamide.
Taxifolin The risk or severity of hypertension can be increased when Taxifolin is combined with Safinamide.
Oxyphenbutazone The risk or severity of hypertension can be increased when Oxyphenbutazone is combined with Safinamide.
1-benzylimidazole The risk or severity of hypertension can be increased when 1-benzylimidazole is combined with Safinamide.
Benoxaprofen The risk or severity of hypertension can be increased when Benoxaprofen is combined with Safinamide.
Cimicoxib The risk or severity of hypertension can be increased when Cimicoxib is combined with Safinamide.
Amibegron The risk or severity of hypertension can be increased when Amibegron is combined with Safinamide.
Solabegron The risk or severity of hypertension can be increased when Solabegron is combined with Safinamide.
Saralasin The risk or severity of hypertension can be increased when Safinamide is combined with Saralasin.
Azapropazone The risk or severity of hypertension can be increased when Safinamide is combined with Azapropazone.
Salicylamide The risk or severity of hypertension can be increased when Safinamide is combined with Salicylamide.
Tyramine The risk or severity of hypertension can be increased when Safinamide is combined with Tyramine.
Adrafinil The risk or severity of hypertension can be increased when Safinamide is combined with Adrafinil.
Kebuzone The risk or severity of hypertension can be increased when Safinamide is combined with Kebuzone.
Isoxicam The risk or severity of hypertension can be increased when Safinamide is combined with Isoxicam.
Indoprofen The risk or severity of hypertension can be increased when Safinamide is combined with Indoprofen.
Ibuproxam The risk or severity of hypertension can be increased when Safinamide is combined with Ibuproxam.
Floctafenine The risk or severity of hypertension can be increased when Safinamide is combined with Floctafenine.
Fenbufen The risk or severity of hypertension can be increased when Safinamide is combined with Fenbufen.
Etofenamate The risk or severity of hypertension can be increased when Safinamide is combined with Etofenamate.
Etilefrine The risk or severity of hypertension can be increased when Safinamide is combined with Etilefrine.
Epirizole The risk or severity of hypertension can be increased when Safinamide is combined with Epirizole.
Benzydamine The risk or severity of hypertension can be increased when Safinamide is combined with Benzydamine.
Synephrine The risk or severity of hypertension can be increased when Safinamide is combined with Synephrine.
Moxisylyte The risk or severity of hypertension can be increased when Safinamide is combined with Moxisylyte.
Dexketoprofen The risk or severity of hypertension can be increased when Safinamide is combined with Dexketoprofen.
Droxicam The risk or severity of hypertension can be increased when Safinamide is combined with Droxicam.
Firocoxib The risk or severity of hypertension can be increased when Safinamide is combined with Firocoxib.
Clonixin The risk or severity of hypertension can be increased when Safinamide is combined with Clonixin.
Morniflumate The risk or severity of hypertension can be increased when Safinamide is combined with Morniflumate.
Talniflumate The risk or severity of hypertension can be increased when Safinamide is combined with Talniflumate.
DL-Methylephedrine The risk or severity of hypertension can be increased when Safinamide is combined with DL-Methylephedrine.
Amitraz The risk or severity of hypertension can be increased when Safinamide is combined with Amitraz.
Robenacoxib The risk or severity of hypertension can be increased when Safinamide is combined with Robenacoxib.
Tepoxalin The risk or severity of hypertension can be increased when Safinamide is combined with Tepoxalin.
Atipamezole The risk or severity of hypertension can be increased when Safinamide is combined with Atipamezole.
Flunixin The risk or severity of hypertension can be increased when Safinamide is combined with Flunixin.
Ractopamine The risk or severity of hypertension can be increased when Safinamide is combined with Ractopamine.
Tulobuterol The risk or severity of hypertension can be increased when Safinamide is combined with Tulobuterol.
Dopexamine The risk or severity of hypertension can be increased when Safinamide is combined with Dopexamine.
Idazoxan The risk or severity of hypertension can be increased when Safinamide is combined with Idazoxan.
Ebselen The risk or severity of hypertension can be increased when Safinamide is combined with Ebselen.
Higenamine The risk or severity of hypertension can be increased when Safinamide is combined with Higenamine.
Reproterol The risk or severity of hypertension can be increased when Safinamide is combined with Reproterol.
Tinoridine The risk or severity of hypertension can be increased when Safinamide is combined with Tinoridine.
Tramazoline The risk or severity of hypertension can be increased when Safinamide is combined with Tramazoline.
Alclofenac The risk or severity of hypertension can be increased when Safinamide is combined with Alclofenac.
Fentiazac The risk or severity of hypertension can be increased when Safinamide is combined with Fentiazac.
Suxibuzone The risk or severity of hypertension can be increased when Safinamide is combined with Suxibuzone.
Octopamine The risk or severity of hypertension can be increased when Safinamide is combined with Octopamine.
Bumadizone The risk or severity of hypertension can be increased when Safinamide is combined with Bumadizone.
Alminoprofen The risk or severity of hypertension can be increased when Safinamide is combined with Alminoprofen.
Fenozolone The risk or severity of hypertension can be increased when Safinamide is combined with Fenozolone.
Difenpiramide The risk or severity of hypertension can be increased when Safinamide is combined with Difenpiramide.
Norfenefrine The risk or severity of hypertension can be increased when Safinamide is combined with Norfenefrine.
Oxyfedrine The risk or severity of hypertension can be increased when Safinamide is combined with Oxyfedrine.
Nifenazone The risk or severity of hypertension can be increased when Safinamide is combined with Nifenazone.
Lonazolac The risk or severity of hypertension can be increased when Safinamide is combined with Lonazolac.
Xenon The risk or severity of adverse effects can be increased when Xenon is combined with Safinamide.
Tenidap The risk or severity of hypertension can be increased when Safinamide is combined with Tenidap.
Propyphenazone The risk or severity of hypertension can be increased when Safinamide is combined with Propyphenazone.
Proglumetacin The risk or severity of hypertension can be increased when Safinamide is combined with Proglumetacin.

Target Protein

Amine oxidase [flavin-containing] B MAOB

Referensi & Sumber

Artikel (PubMed)
  • PMID: 18549347
    Onofrj M, Bonanni L, Thomas A: An expert opinion on safinamide in Parkinson's disease. Expert Opin Investig Drugs. 2008 Jul;17(7):1115-25. doi: 10.1517/13543784.17.7.1115 .
  • PMID: 17030737
    Stocchi F, Vacca L, Grassini P, De Pandis MF, Battaglia G, Cattaneo C, Fariello RG: Symptom relief in Parkinson disease by safinamide: Biochemical and clinical evidence of efficacy beyond MAO-B inhibition. Neurology. 2006 Oct 10;67(7 Suppl 2):S24-9.
  • PMID: 15082032
    Marzo A, Dal Bo L, Monti NC, Crivelli F, Ismaili S, Caccia C, Cattaneo C, Fariello RG: Pharmacokinetics and pharmacodynamics of safinamide, a neuroprotectant with antiparkinsonian and anticonvulsant activity. Pharmacol Res. 2004 Jul;50(1):77-85.
  • PMID: 24136086
    Leuratti C, Sardina M, Ventura P, Assandri A, Muller M, Brunner M: Disposition and metabolism of safinamide, a novel drug for Parkinson's disease, in healthy male volunteers. Pharmacology. 2013;92(3-4):207-16. doi: 10.1159/000354805. Epub 2013 Oct 11.
  • PMID: 20707760
    Schapira AH: Safinamide in the treatment of Parkinson's disease. Expert Opin Pharmacother. 2010 Sep;11(13):2261-8. doi: 10.1517/14656566.2010.511612.

Contoh Produk & Brand

Produk: 16 • International brands: 0
Produk
  • Onstryv
    Tablet • 50 mg • Oral • Canada • Approved
  • Onstryv
    Tablet • 100 mg • Oral • Canada • Approved
  • Xadago
    Tablet, film coated • 50 mg/1 • Oral • US • Approved
  • Xadago
    Tablet, film coated • 100 mg/1 • Oral • US • Approved
  • Xadago
    Tablet, film coated • 50 mg/1 • Oral • US • Approved
  • Xadago
    Tablet, film coated • 100 mg/1 • Oral • US • Approved
  • Xadago
    Tablet, film coated • 50 mg • Oral • EU • Approved
  • Xadago
    Tablet, film coated • 100 mg • Oral • EU • Approved
Menampilkan 8 dari 16 produk.

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
© 2025 Digital Pharmacy Research - Universitas Esa Unggul