Peringatan Keamanan

There is no direct experience of any patient taking an overdose of Frovatriptan. The maximum single dose of frovatriptan given to male and female patients with migraine was 40 mg (16 times the clinical dose) and the maximum single dose given to healthy male subjects was 100 mg (40 times the clinical dose) without significant adverse events.

Frovatriptan

DB00998

small molecule approved investigational

Deskripsi

Frovatriptan is a triptan drug developed by Vernalis for the treatment of migraine headaches, in particular those associated with menstruation. Frovatriptan causes vasoconstriction of arteries and veins that supply blood to the head.

Struktur Molekul 2D

Berat 243.3043
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) 26 hours
Volume Distribusi * 4.2 L/kg [males] * 3 L/kg [females]
Klirens (Clearance) * 220 mL/min [male receiving IV dose of 0.8 mg] * 130 mL/min [Female receiving IV dose of 0.8 mg]

Absorpsi

Frovatriptan is rapidly absorbed from the duodenum, but has low oral bioavailability.

Metabolisme

In vitro, cytochrome P450 1A2 appears to be the principal enzyme involved in the metabolism of frovatriptan to several metabolites including hydroxylated frovatriptan, N-acetyl desmethyl frovatriptan, hydroxylated N-acetyl desmethyl frovatriptan and desmethyl frovatriptan, and several other minor metabolites. Desmethyl frovatriptan has lower affinity for 5-HT1B/1D receptors compared to the parent compound. The N-acetyl desmethyl metabolite has no significant affinity for 5-HT receptors. The activity of the other metabolites is unknown.

Rute Eliminasi

Radiolabeled compounds excreted in urine were unchanged frovatriptan, hydroxylated frovatriptan, N-acetyl desmethyl frovatriptan, hydroxylated N-acetyl desmethyl frovatriptan and desmethyl frovatriptan, together with several other minor metabolites. Less than 10% of frovatriptan was excreted in urine after an oral dose.

Farmakogenomik

1 Varian
GNB3 (rs5443)

Patients with this genotype have an increased likelihood of responding to frovatriptan when treating (condition: cluster headache).

Interaksi Makanan

1 Data
  • 1. Take with or without food. Food does not affect bioavailability, but delays maximum concentrations by one hour.

Interaksi Obat

1288 Data
Deferasirox The serum concentration of Frovatriptan can be increased when it is combined with Deferasirox.
Peginterferon alfa-2b The serum concentration of Frovatriptan can be increased when it is combined with Peginterferon alfa-2b.
Leflunomide The serum concentration of Frovatriptan can be decreased when it is combined with Leflunomide.
Teriflunomide The serum concentration of Frovatriptan can be decreased when it is combined with Teriflunomide.
Valsartan Frovatriptan may decrease the antihypertensive activities of Valsartan.
Ramipril Frovatriptan may decrease the antihypertensive activities of Ramipril.
Esmolol Frovatriptan may decrease the antihypertensive activities of Esmolol.
Remikiren Frovatriptan may decrease the antihypertensive activities of Remikiren.
Torasemide Frovatriptan may decrease the antihypertensive activities of Torasemide.
Guanadrel Frovatriptan may decrease the antihypertensive activities of Guanadrel.
Metoprolol Frovatriptan may decrease the antihypertensive activities of Metoprolol.
Isradipine Frovatriptan may decrease the antihypertensive activities of Isradipine.
Olmesartan Frovatriptan may decrease the antihypertensive activities of Olmesartan.
Chlorthalidone Frovatriptan may decrease the antihypertensive activities of Chlorthalidone.
Nitroprusside Frovatriptan may decrease the antihypertensive activities of Nitroprusside.
Atenolol Frovatriptan may decrease the antihypertensive activities of Atenolol.
Diltiazem Frovatriptan may decrease the antihypertensive activities of Diltiazem.
Minoxidil Frovatriptan may decrease the antihypertensive activities of Minoxidil.
Timolol Frovatriptan may decrease the antihypertensive activities of Timolol.
Treprostinil Frovatriptan may decrease the antihypertensive activities of Treprostinil.
Amlodipine Frovatriptan may decrease the antihypertensive activities of Amlodipine.
Nimodipine Frovatriptan may decrease the antihypertensive activities of Nimodipine.
Nisoldipine Frovatriptan may decrease the antihypertensive activities of Nisoldipine.
Bendroflumethiazide Frovatriptan may decrease the antihypertensive activities of Bendroflumethiazide.
Prazosin Frovatriptan may decrease the antihypertensive activities of Prazosin.
Fosinopril Frovatriptan may decrease the antihypertensive activities of Fosinopril.
Trandolapril Frovatriptan may decrease the antihypertensive activities of Trandolapril.
Metolazone Frovatriptan may decrease the antihypertensive activities of Metolazone.
Lercanidipine Frovatriptan may decrease the antihypertensive activities of Lercanidipine.
Benazepril Frovatriptan may decrease the antihypertensive activities of Benazepril.
Bosentan Frovatriptan may decrease the antihypertensive activities of Bosentan.
Enalapril Frovatriptan may decrease the antihypertensive activities of Enalapril.
Doxazosin Frovatriptan may decrease the antihypertensive activities of Doxazosin.
Labetalol Frovatriptan may decrease the antihypertensive activities of Labetalol.
Cyclothiazide Frovatriptan may decrease the antihypertensive activities of Cyclothiazide.
Bisoprolol Frovatriptan may decrease the antihypertensive activities of Bisoprolol.
Candoxatril Frovatriptan may decrease the antihypertensive activities of Candoxatril.
Mecamylamine Frovatriptan may decrease the antihypertensive activities of Mecamylamine.
Losartan Frovatriptan may decrease the antihypertensive activities of Losartan.
Moexipril Frovatriptan may decrease the antihypertensive activities of Moexipril.
Eplerenone Frovatriptan may decrease the antihypertensive activities of Eplerenone.
Lisinopril Frovatriptan may decrease the antihypertensive activities of Lisinopril.
Nitroglycerin Frovatriptan may decrease the antihypertensive activities of Nitroglycerin.
Hydroflumethiazide Frovatriptan may decrease the antihypertensive activities of Hydroflumethiazide.
Cryptenamine Frovatriptan may decrease the antihypertensive activities of Cryptenamine.
Perindopril Frovatriptan may decrease the antihypertensive activities of Perindopril.
Candesartan cilexetil Frovatriptan may decrease the antihypertensive activities of Candesartan cilexetil.
Fenoldopam Frovatriptan may decrease the antihypertensive activities of Fenoldopam.
Indapamide Frovatriptan may decrease the antihypertensive activities of Indapamide.
Tadalafil Frovatriptan may decrease the antihypertensive activities of Tadalafil.
Eprosartan Frovatriptan may decrease the antihypertensive activities of Eprosartan.
Chlorothiazide Frovatriptan may decrease the antihypertensive activities of Chlorothiazide.
Quinapril Frovatriptan may decrease the antihypertensive activities of Quinapril.
Telmisartan Frovatriptan may decrease the antihypertensive activities of Telmisartan.
Methyldopa Frovatriptan may decrease the antihypertensive activities of Methyldopa.
Hydrochlorothiazide Frovatriptan may decrease the antihypertensive activities of Hydrochlorothiazide.
Trichlormethiazide Frovatriptan may decrease the antihypertensive activities of Trichlormethiazide.
Felodipine Frovatriptan may decrease the antihypertensive activities of Felodipine.
Irbesartan Frovatriptan may decrease the antihypertensive activities of Irbesartan.
Nitrendipine Frovatriptan may decrease the antihypertensive activities of Nitrendipine.
Deserpidine Frovatriptan may decrease the antihypertensive activities of Deserpidine.
Pentolinium Frovatriptan may decrease the antihypertensive activities of Pentolinium.
Trimethaphan Frovatriptan may decrease the antihypertensive activities of Trimethaphan.
Diazoxide Frovatriptan may decrease the antihypertensive activities of Diazoxide.
Bretylium Frovatriptan may decrease the antihypertensive activities of Bretylium.
Terazosin Frovatriptan may decrease the antihypertensive activities of Terazosin.
Guanethidine Frovatriptan may decrease the antihypertensive activities of Guanethidine.
Acebutolol Frovatriptan may decrease the antihypertensive activities of Acebutolol.
Captopril Frovatriptan may decrease the antihypertensive activities of Captopril.
Nadolol Frovatriptan may decrease the antihypertensive activities of Nadolol.
Epoprostenol Frovatriptan may decrease the antihypertensive activities of Epoprostenol.
Bepridil Frovatriptan may decrease the antihypertensive activities of Bepridil.
Hydralazine Frovatriptan may decrease the antihypertensive activities of Hydralazine.
Bevantolol Frovatriptan may decrease the antihypertensive activities of Bevantolol.
Practolol Frovatriptan may decrease the antihypertensive activities of Practolol.
Polythiazide Frovatriptan may decrease the antihypertensive activities of Polythiazide.
Cilazapril Frovatriptan may decrease the antihypertensive activities of Cilazapril.
Saprisartan Frovatriptan may decrease the antihypertensive activities of Saprisartan.
Spirapril Frovatriptan may decrease the antihypertensive activities of Spirapril.
Dexpropranolol Frovatriptan may decrease the antihypertensive activities of Dexpropranolol.
Tienilic acid Frovatriptan may decrease the antihypertensive activities of Tienilic acid.
Debrisoquine Frovatriptan may decrease the antihypertensive activities of Debrisoquine.
Celiprolol Frovatriptan may decrease the antihypertensive activities of Celiprolol.
Nebivolol Frovatriptan may decrease the antihypertensive activities of Nebivolol.
Sitaxentan Frovatriptan may decrease the antihypertensive activities of Sitaxentan.
Ambrisentan Frovatriptan may decrease the antihypertensive activities of Ambrisentan.
Diethylnorspermine Frovatriptan may decrease the antihypertensive activities of Diethylnorspermine.
Nilvadipine Frovatriptan may decrease the antihypertensive activities of Nilvadipine.
Pinacidil Frovatriptan may decrease the antihypertensive activities of Pinacidil.
Bupranolol Frovatriptan may decrease the antihypertensive activities of Bupranolol.
Temocapril Frovatriptan may decrease the antihypertensive activities of Temocapril.
Riociguat Frovatriptan may decrease the antihypertensive activities of Riociguat.
Macitentan Frovatriptan may decrease the antihypertensive activities of Macitentan.
Indenolol Frovatriptan may decrease the antihypertensive activities of Indenolol.
Aliskiren Frovatriptan may decrease the antihypertensive activities of Aliskiren.
Trimazosin Frovatriptan may decrease the antihypertensive activities of Trimazosin.
Nicorandil Frovatriptan may decrease the antihypertensive activities of Nicorandil.
Efonidipine Frovatriptan may decrease the antihypertensive activities of Efonidipine.
Lacidipine Frovatriptan may decrease the antihypertensive activities of Lacidipine.
Manidipine Frovatriptan may decrease the antihypertensive activities of Manidipine.

Target Protein

5-hydroxytryptamine receptor 1D HTR1D
5-hydroxytryptamine receptor 1B HTR1B

Referensi & Sumber

Synthesis reference: Samir Naik, Anthony Crasto, Narendra Joshi, Sachin Srivastava, "Amorphous frovatriptan succinate and process for the preparation thereof." U.S. Patent US20070299123, issued December 27, 2007.
Artikel (PubMed)
  • PMID: 18001261
    Markus F, Mikko K: Frovatriptan review. Expert Opin Pharmacother. 2007 Dec;8(17):3029-33.
  • PMID: 11735616
    Easthope SE, Goa KL: Frovatriptan. CNS Drugs. 2001;15(12):969-76; discussion 977-8.
  • PMID: 18360605
    Balbisi EA: Frovatriptan: a review of pharmacology, pharmacokinetics and clinical potential in the treatment of menstrual migraine. Ther Clin Risk Manag. 2006 Sep;2(3):303-8.
  • PMID: 15311727
    Balbisi EA: Frovatriptan succinate, a 5-HT1B/1D receptor agonist for migraine. Int J Clin Pract. 2004 Jul;58(7):695-705.
  • PMID: 15342617
    Elkind AH, Wade A, Ishkanian G: Pharmacokinetics of frovatriptan in adolescent migraineurs. J Clin Pharmacol. 2004 Oct;44(10):1158-65.
  • PMID: 11327198
    Jhee SS, Shiovitz T, Crawford AW, Cutler NR: Pharmacokinetics and pharmacodynamics of the triptan antimigraine agents: a comparative review. Clin Pharmacokinet. 2001;40(3):189-205.

Contoh Produk & Brand

Produk: 15 • International brands: 2
Produk
  • Apo-frovatriptan
    Tablet • 2.5 mg • Oral • Canada • Generic • Approved
  • Frova
    Tablet, film coated • 2.5 mg/1 • Oral • US • Approved
  • Frova
    Tablet, film coated • 2.5 mg/1 • Oral • US • Approved
  • Frova
    Tablet, film coated • 2.5 mg/1 • Oral • US • Approved
  • Frova
    Tablet, film coated • 2.5 mg/1 • Oral • US • Approved
  • Frova
    Tablet • 2.5 mg • Oral • Canada • Approved
  • Frovatriptan
    Tablet, film coated • 2.5 mg/1 • Oral • US • Generic • Approved
  • Frovatriptan
    Tablet, film coated • 2.5 mg/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 15 produk.
International Brands
  • Frova
  • Miguard

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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