Flibanserin

DB04908

small molecule approved investigational

Deskripsi

Flibanserin is the first drug to be approved for hypoactive sexual desire disorder (HSDD) in premenopausal women by the FDA in August 2015. It was originally developed as an antidepressant medication by Boehringer Ingelheim, but showed lack of efficacy in trials and was further developed as a hypoactive sexual disorder drug by Sprout Pharmaceuticals. Flibanserin's mechanism of action is attributed to its high affinity for 5-HTA1 and 5-HTA2 receptors, displaying agonist activity on 5-HTA1 and antagonist on 5-HTA2, resulting in lowering of serotonin in the brain as well as an effect on increasing norepinephrine and dopamine neurotransmitters.

Struktur Molekul 2D

Berat 390.4021
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) ?11 hours
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

Flibanserin has an absolute oral availability of 33%.

Metabolisme

Metabolism is primarily via CYP3A4, slightly CYP2C19. Minimal involvement of CYP1A2, CYP2B6, CYP2C8, CYP2C9 or CYP2D6. At least 35 metabolites of flibanserin are produced, 2 of which reach plasma concentrations as high as parent drug, however they are pharmacologically inactive.

Rute Eliminasi

Elimination via feces (51%) and urine (44%) following a single oral 50 mg dose of flibanserin solution.

Interaksi Makanan

4 Data
  • 1. Avoid alcohol. Avoid alcohol. Ingesting alcohol may increase the CNS depressant and hypotensive effects of flibanserin. If you have consumed two drinks, wait two hours before taking flibanserin. Do not take flibanserin if you have consumed more than three drinks.
  • 2. Avoid grapefruit products.
  • 3. Avoid St. John's Wort.
  • 4. Take with or without food. Taking flibanserin with food (especially a high-fat meal) may increase its AUC, Cmax, and Tmax.

Interaksi Obat

1322 Data
Afatinib The serum concentration of Afatinib can be increased when it is combined with Flibanserin.
Bosutinib The serum concentration of Bosutinib can be increased when it is combined with Flibanserin.
Brentuximab vedotin The serum concentration of Brentuximab vedotin can be increased when it is combined with Flibanserin.
Colchicine The serum concentration of Colchicine can be increased when it is combined with Flibanserin.
Edoxaban The serum concentration of Edoxaban can be increased when it is combined with Flibanserin.
Ledipasvir The serum concentration of Ledipasvir can be increased when it is combined with Flibanserin.
Naloxegol The serum concentration of Naloxegol can be increased when it is combined with Flibanserin.
Pazopanib The serum concentration of Pazopanib can be increased when it is combined with Flibanserin.
Prucalopride The serum concentration of Prucalopride can be increased when it is combined with Flibanserin.
Ranolazine The serum concentration of Ranolazine can be increased when it is combined with Flibanserin.
Silodosin The excretion of Silodosin can be decreased when combined with Flibanserin.
Topotecan The serum concentration of Topotecan can be increased when it is combined with Flibanserin.
Ticlopidine The serum concentration of Flibanserin can be increased when it is combined with Ticlopidine.
Chloramphenicol The serum concentration of Flibanserin can be increased when it is combined with Chloramphenicol.
Lansoprazole The serum concentration of Flibanserin can be increased when it is combined with Lansoprazole.
Imipramine The serum concentration of Flibanserin can be increased when it is combined with Imipramine.
Zafirlukast The serum concentration of Flibanserin can be increased when it is combined with Zafirlukast.
Gemfibrozil The serum concentration of Flibanserin can be increased when it is combined with Gemfibrozil.
Clomipramine The serum concentration of Flibanserin can be increased when it is combined with Clomipramine.
Valsartan Flibanserin may decrease the antihypertensive activities of Valsartan.
Ramipril Flibanserin may decrease the antihypertensive activities of Ramipril.
Esmolol Flibanserin may decrease the antihypertensive activities of Esmolol.
Betaxolol Flibanserin may decrease the antihypertensive activities of Betaxolol.
Remikiren Flibanserin may decrease the antihypertensive activities of Remikiren.
Torasemide Flibanserin may decrease the antihypertensive activities of Torasemide.
Guanadrel Flibanserin may decrease the antihypertensive activities of Guanadrel.
Olmesartan Flibanserin may decrease the antihypertensive activities of Olmesartan.
Chlorthalidone Flibanserin may decrease the antihypertensive activities of Chlorthalidone.
Nitroprusside Flibanserin may decrease the antihypertensive activities of Nitroprusside.
Atenolol Flibanserin may decrease the antihypertensive activities of Atenolol.
Minoxidil Flibanserin may decrease the antihypertensive activities of Minoxidil.
Treprostinil Flibanserin may decrease the antihypertensive activities of Treprostinil.
Bendroflumethiazide Flibanserin may decrease the antihypertensive activities of Bendroflumethiazide.
Fosinopril Flibanserin may decrease the antihypertensive activities of Fosinopril.
Trandolapril Flibanserin may decrease the antihypertensive activities of Trandolapril.
Metolazone Flibanserin may decrease the antihypertensive activities of Metolazone.
Benazepril Flibanserin may decrease the antihypertensive activities of Benazepril.
Labetalol Flibanserin may decrease the antihypertensive activities of Labetalol.
Cyclothiazide Flibanserin may decrease the antihypertensive activities of Cyclothiazide.
Candoxatril Flibanserin may decrease the antihypertensive activities of Candoxatril.
Mecamylamine Flibanserin may decrease the antihypertensive activities of Mecamylamine.
Moexipril Flibanserin may decrease the antihypertensive activities of Moexipril.
Lisinopril Flibanserin may decrease the antihypertensive activities of Lisinopril.
Nitroglycerin Flibanserin may decrease the antihypertensive activities of Nitroglycerin.
Hydroflumethiazide Flibanserin may decrease the antihypertensive activities of Hydroflumethiazide.
Cryptenamine Flibanserin may decrease the antihypertensive activities of Cryptenamine.
Perindopril Flibanserin may decrease the antihypertensive activities of Perindopril.
Candesartan cilexetil Flibanserin may decrease the antihypertensive activities of Candesartan cilexetil.
Fenoldopam Flibanserin may decrease the antihypertensive activities of Fenoldopam.
Eprosartan Flibanserin may decrease the antihypertensive activities of Eprosartan.
Chlorothiazide Flibanserin may decrease the antihypertensive activities of Chlorothiazide.
Quinapril Flibanserin may decrease the antihypertensive activities of Quinapril.
Telmisartan Flibanserin may decrease the antihypertensive activities of Telmisartan.
Methyldopa Flibanserin may decrease the antihypertensive activities of Methyldopa.
Hydrochlorothiazide Flibanserin may decrease the antihypertensive activities of Hydrochlorothiazide.
Trichlormethiazide Flibanserin may decrease the antihypertensive activities of Trichlormethiazide.
Deserpidine Flibanserin may decrease the antihypertensive activities of Deserpidine.
Pentolinium Flibanserin may decrease the antihypertensive activities of Pentolinium.
Trimethaphan Flibanserin may decrease the antihypertensive activities of Trimethaphan.
Diazoxide Flibanserin may decrease the antihypertensive activities of Diazoxide.
Bretylium Flibanserin may decrease the antihypertensive activities of Bretylium.
Terazosin Flibanserin may decrease the antihypertensive activities of Terazosin.
Captopril Flibanserin may decrease the antihypertensive activities of Captopril.
Epoprostenol Flibanserin may decrease the antihypertensive activities of Epoprostenol.
Bevantolol Flibanserin may decrease the antihypertensive activities of Bevantolol.
Practolol Flibanserin may decrease the antihypertensive activities of Practolol.
Polythiazide Flibanserin may decrease the antihypertensive activities of Polythiazide.
Cilazapril Flibanserin may decrease the antihypertensive activities of Cilazapril.
Saprisartan Flibanserin may decrease the antihypertensive activities of Saprisartan.
Spirapril Flibanserin may decrease the antihypertensive activities of Spirapril.
Dexpropranolol Flibanserin may decrease the antihypertensive activities of Dexpropranolol.
Tienilic acid Flibanserin may decrease the antihypertensive activities of Tienilic acid.
Diethylnorspermine Flibanserin may decrease the antihypertensive activities of Diethylnorspermine.
Bupranolol Flibanserin may decrease the antihypertensive activities of Bupranolol.
Temocapril Flibanserin may decrease the antihypertensive activities of Temocapril.
Indenolol Flibanserin may decrease the antihypertensive activities of Indenolol.
Trimazosin Flibanserin may decrease the antihypertensive activities of Trimazosin.
Nicorandil Flibanserin may decrease the antihypertensive activities of Nicorandil.
Rauwolfia serpentina root Flibanserin may decrease the antihypertensive activities of Rauwolfia serpentina root.
Enalaprilat Flibanserin may decrease the antihypertensive activities of Enalaprilat.
Angiotensin 1-7 Flibanserin may decrease the antihypertensive activities of Angiotensin 1-7.
Imidapril Flibanserin may decrease the antihypertensive activities of Imidapril.
BQ-123 Flibanserin may decrease the antihypertensive activities of BQ-123.
Landiolol Flibanserin may decrease the antihypertensive activities of Landiolol.
Cicletanine Flibanserin may decrease the antihypertensive activities of Cicletanine.
Dihydralazine Flibanserin may decrease the antihypertensive activities of Dihydralazine.
Zofenopril Flibanserin may decrease the antihypertensive activities of Zofenopril.
Guanoxan Flibanserin may decrease the antihypertensive activities of Guanoxan.
Delapril Flibanserin may decrease the antihypertensive activities of Delapril.
Vincamine Flibanserin may decrease the antihypertensive activities of Vincamine.
Linsidomine Flibanserin may decrease the antihypertensive activities of Linsidomine.
Guanoxabenz Flibanserin may decrease the antihypertensive activities of Guanoxabenz.
Tolonidine Flibanserin may decrease the antihypertensive activities of Tolonidine.
Endralazine Flibanserin may decrease the antihypertensive activities of Endralazine.
Esatenolol Flibanserin may decrease the antihypertensive activities of Esatenolol.
Cadralazine Flibanserin may decrease the antihypertensive activities of Cadralazine.
Cloranolol Flibanserin may decrease the antihypertensive activities of Cloranolol.
Cyclopenthiazide Flibanserin may decrease the antihypertensive activities of Cyclopenthiazide.
Bietaserpine Flibanserin may decrease the antihypertensive activities of Bietaserpine.
Guanazodine Flibanserin may decrease the antihypertensive activities of Guanazodine.

Target Protein

5-hydroxytryptamine receptor 1A HTR1A
5-hydroxytryptamine receptor 2A HTR2A
D(4) dopamine receptor DRD4

Referensi & Sumber

Artikel (PubMed)
  • PMID: 12890707
    Invernizzi RW, Sacchetti G, Parini S, Acconcia S, Samanin R: Flibanserin, a potential antidepressant drug, lowers 5-HT and raises dopamine and noradrenaline in the rat prefrontal cortex dialysate: role of 5-HT(1A) receptors. Br J Pharmacol. 2003 Aug;139(7):1281-8.
  • PMID: 11243720
    Scandroglio A, Monferini E, Borsini F: Ex vivo binding of flibanserin to serotonin 5-HT1A and 5-HT2A receptors. Pharmacol Res. 2001 Feb;43(2):179-83.
  • PMID: 11755137
    Borsini F, Cesana R: Mechanism of action of flibanserin in the learned helplessness paradigm in rats. Eur J Pharmacol. 2001 Dec 14;433(1):81-9.
  • PMID: 12177684
    Borsini F, Evans K, Jason K, Rohde F, Alexander B, Pollentier S: Pharmacology of flibanserin. CNS Drug Rev. 2002 Summer;8(2):117-42.
  • PMID: 26412054
    Deeks ED: Flibanserin: First Global Approval. Drugs. 2015 Oct;75(15):1815-22. doi: 10.1007/s40265-015-0474-y.
  • PMID: 25659981
    Stahl SM: Mechanism of action of flibanserin, a multifunctional serotonin agonist and antagonist (MSAA), in hypoactive sexual desire disorder. CNS Spectr. 2015 Feb;20(1):1-6. doi: 10.1017/S1092852914000832. Epub 2015 Feb 9.

Contoh Produk & Brand

Produk: 2 • International brands: 1
Produk
  • Addyi
    Tablet • 100 mg • Oral • Canada • Approved
  • Addyi
    Tablet, film coated • 100 mg/1 • Oral • US • Approved
International Brands
  • Ectris

Sekuens Gen/Protein (FASTA)

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