Peringatan Keamanan

Experience with avanafil overdose is limited. Single doses of up to 800mg and repeat doses of up to 300mg have been administered - these patients experienced adverse effects similar to those seen at therapeutic doses but with increased incidence and severity.L32233 Patients experiencing an overdosage of avanafil should be treated with standard symptomatic and supportive measures. Dialysis is unlikely to be of benefit in cases of overdose as avanafil is highly protein-bound in plasma.L32058

Avanafil

DB06237

small molecule approved

Deskripsi

Avanafil is a phosphodiesterase-5 (PDE5) inhibitor used in the treatment of erectile dysfunction. In comparison with other drugs of the same class, it shows greater selectivity for PDE5 over PDE6 than both sildenafil and vardenafil but less selectivity than tadalafil, suggesting a relatively lower risk of visual disturbances associated with off-target PDE6 inhibition.L32113

It first received FDA approval on April 27, 2012,L32058 with subsequent EMA approval in June 2013.L32113

Struktur Molekul 2D

Berat 483.951
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Studies have demonstrated variability in the terminal elimination half-life of avanafil, with estimates ranging between 5 - 17 hours.[L32113]
Volume Distribusi The apparent volume of distribution of avanafil is 47 to 83 L.[L32113]
Klirens (Clearance) -

Absorpsi

Avanafil is rapidly absorbed following oral administration (Tmax of 30-45 minutes)L32058 and appears to have low to moderate oral bioavailability, though formal studies have not been conducted.L32113 Administration with a meal results in a mean delay in Tmax of 1.12 to 1.25 hours, a 39% mean reduction in Cmax, and a negligible effect on AUC.L32058,L32113

Metabolisme

Avanafil is extensively metabolized, primarily by CYP3A4 and to a lesser extent by CYP2C9.L32058,L32233 There are two major metabolites formed, M4 and M16, which exist in the plasma at concentrations 23% and 29% that of the parent compound, respectively. The M16 metabolite lacks pharmacologic effect, but the M4 metabolite has an inhibitory potency for PDE5 18% that of avanafil and accounts for approximately 4% of the observed pharmacologic activity of avanafil.L32058

Rute Eliminasi

Following oral administration, avanafil is extensively metabolized. Approximately 62% of a given dose is excreted as metabolites in the feces and approximately 21% as metabolites in the urine.L32058

Interaksi Makanan

2 Data
  • 1. Avoid excessive or chronic alcohol consumption. Substantial alcohol consumption (e.g. >3 units) in combination with avanafil may increase the risk of hypotension.
  • 2. Take with or without food. High-fat meals slow absorption, but not to a clinically significant extent.

Interaksi Obat

1244 Data
Ranolazine The serum concentration of Avanafil can be increased when it is combined with Ranolazine.
Cyclosporine The metabolism of Avanafil can be decreased when combined with Cyclosporine.
Fluvoxamine The metabolism of Avanafil can be decreased when combined with Fluvoxamine.
Fluconazole The metabolism of Avanafil can be decreased when combined with Fluconazole.
Isoniazid The metabolism of Avanafil can be decreased when combined with Isoniazid.
Zimelidine The metabolism of Avanafil can be decreased when combined with Zimelidine.
Seproxetine The metabolism of Avanafil can be decreased when combined with Seproxetine.
Erythromycin The metabolism of Avanafil can be decreased when combined with Erythromycin.
Lovastatin The serum concentration of Avanafil can be increased when it is combined with Lovastatin.
Ziprasidone The metabolism of Avanafil can be decreased when combined with Ziprasidone.
Isradipine The metabolism of Avanafil can be decreased when combined with Isradipine.
Diltiazem The metabolism of Avanafil can be decreased when combined with Diltiazem.
Clozapine The metabolism of Avanafil can be decreased when combined with Clozapine.
Haloperidol The metabolism of Avanafil can be decreased when combined with Haloperidol.
Nicardipine The metabolism of Avanafil can be decreased when combined with Nicardipine.
Verapamil The metabolism of Avanafil can be decreased when combined with Verapamil.
Aprepitant The metabolism of Avanafil can be decreased when combined with Aprepitant.
Primaquine The metabolism of Avanafil can be decreased when combined with Primaquine.
Miconazole The metabolism of Avanafil can be decreased when combined with Miconazole.
Fusidic acid The metabolism of Avanafil can be decreased when combined with Fusidic acid.
Dronedarone The metabolism of Avanafil can be decreased when combined with Dronedarone.
Milnacipran The metabolism of Avanafil can be decreased when combined with Milnacipran.
Isavuconazole The metabolism of Avanafil can be decreased when combined with Isavuconazole.
Simeprevir The metabolism of Avanafil can be decreased when combined with Simeprevir.
Isavuconazonium The metabolism of Avanafil can be decreased when combined with Isavuconazonium.
Desvenlafaxine The metabolism of Avanafil can be decreased when combined with Desvenlafaxine.
Nilvadipine The metabolism of Avanafil can be decreased when combined with Nilvadipine.
Crizotinib The serum concentration of Avanafil can be increased when it is combined with Crizotinib.
Linagliptin The metabolism of Avanafil can be decreased when combined with Linagliptin.
Indalpine The metabolism of Avanafil can be decreased when combined with Indalpine.
Netupitant The metabolism of Avanafil can be decreased when combined with Netupitant.
Barnidipine The metabolism of Avanafil can be decreased when combined with Barnidipine.
Benidipine The metabolism of Avanafil can be decreased when combined with Benidipine.
Venetoclax The metabolism of Avanafil can be decreased when combined with Venetoclax.
Fosnetupitant The metabolism of Avanafil can be decreased when combined with Fosnetupitant.
Ciprofloxacin The metabolism of Avanafil can be decreased when combined with Ciprofloxacin.
Berotralstat The metabolism of Avanafil can be decreased when combined with Berotralstat.
Alprostadil The risk or severity of hypotension and priapism can be increased when Avanafil is combined with Alprostadil.
Amyl Nitrite Avanafil may increase the hypotensive activities of Amyl Nitrite.
Dapoxetine The risk or severity of orthostatic hypotension can be increased when Dapoxetine is combined with Avanafil.
Riociguat Avanafil may increase the hypotensive activities of Riociguat.
Sapropterin Sapropterin may increase the hypotensive activities of Avanafil.
Ethanol Ethanol may increase the hypotensive activities of Avanafil.
Ramipril Ramipril may increase the hypotensive activities of Avanafil.
Esmolol Esmolol may increase the hypotensive activities of Avanafil.
Betaxolol Betaxolol may increase the hypotensive activities of Avanafil.
Remikiren Remikiren may increase the hypotensive activities of Avanafil.
Bethanidine Bethanidine may increase the hypotensive activities of Avanafil.
Guanadrel Guanadrel may increase the hypotensive activities of Avanafil.
Olmesartan Olmesartan may increase the hypotensive activities of Avanafil.
Chlorthalidone Chlorthalidone may increase the hypotensive activities of Avanafil.
Nitroprusside Nitroprusside may increase the hypotensive activities of Avanafil.
Atenolol Atenolol may increase the hypotensive activities of Avanafil.
Minoxidil Minoxidil may increase the hypotensive activities of Avanafil.
Timolol Timolol may increase the hypotensive activities of Avanafil.
Treprostinil Treprostinil may increase the hypotensive activities of Avanafil.
Bendroflumethiazide Bendroflumethiazide may increase the hypotensive activities of Avanafil.
Fosinopril Fosinopril may increase the hypotensive activities of Avanafil.
Trandolapril Trandolapril may increase the hypotensive activities of Avanafil.
Metolazone Metolazone may increase the hypotensive activities of Avanafil.
Benazepril Benazepril may increase the hypotensive activities of Avanafil.
Cyclothiazide Cyclothiazide may increase the hypotensive activities of Avanafil.
Candoxatril Candoxatril may increase the hypotensive activities of Avanafil.
Guanabenz Guanabenz may increase the hypotensive activities of Avanafil.
Mecamylamine Mecamylamine may increase the hypotensive activities of Avanafil.
Moexipril Moexipril may increase the hypotensive activities of Avanafil.
Lisinopril Lisinopril may increase the hypotensive activities of Avanafil.
Metyrosine Metyrosine may increase the hypotensive activities of Avanafil.
Hydroflumethiazide Hydroflumethiazide may increase the hypotensive activities of Avanafil.
Cryptenamine Cryptenamine may increase the hypotensive activities of Avanafil.
Perindopril Perindopril may increase the hypotensive activities of Avanafil.
Candesartan cilexetil Candesartan cilexetil may increase the hypotensive activities of Avanafil.
Fenoldopam Fenoldopam may increase the hypotensive activities of Avanafil.
Alprenolol Alprenolol may increase the hypotensive activities of Avanafil.
Eprosartan Eprosartan may increase the hypotensive activities of Avanafil.
Chlorothiazide Chlorothiazide may increase the hypotensive activities of Avanafil.
Quinapril Quinapril may increase the hypotensive activities of Avanafil.
Omapatrilat Omapatrilat may increase the hypotensive activities of Avanafil.
Pindolol Pindolol may increase the hypotensive activities of Avanafil.
Telmisartan Telmisartan may increase the hypotensive activities of Avanafil.
Methyldopa Methyldopa may increase the hypotensive activities of Avanafil.
Hydrochlorothiazide Hydrochlorothiazide may increase the hypotensive activities of Avanafil.
Trichlormethiazide Trichlormethiazide may increase the hypotensive activities of Avanafil.
Deserpidine Deserpidine may increase the hypotensive activities of Avanafil.
Pentolinium Pentolinium may increase the hypotensive activities of Avanafil.
Trimethaphan Trimethaphan may increase the hypotensive activities of Avanafil.
Diazoxide Diazoxide may increase the hypotensive activities of Avanafil.
Bretylium Bretylium may increase the hypotensive activities of Avanafil.
Rescinnamine Rescinnamine may increase the hypotensive activities of Avanafil.
Acebutolol Acebutolol may increase the hypotensive activities of Avanafil.
Captopril Captopril may increase the hypotensive activities of Avanafil.
Nadolol Nadolol may increase the hypotensive activities of Avanafil.
Epoprostenol Epoprostenol may increase the hypotensive activities of Avanafil.
Practolol Practolol may increase the hypotensive activities of Avanafil.
Polythiazide Polythiazide may increase the hypotensive activities of Avanafil.
Cilazapril Cilazapril may increase the hypotensive activities of Avanafil.
Saprisartan Saprisartan may increase the hypotensive activities of Avanafil.
Spirapril Spirapril may increase the hypotensive activities of Avanafil.
Penbutolol Penbutolol may increase the hypotensive activities of Avanafil.
Oxprenolol Oxprenolol may increase the hypotensive activities of Avanafil.

Target Protein

cGMP-specific 3',5'-cyclic phosphodiesterase PDE5A

Referensi & Sumber

Artikel (PubMed)
  • PMID: 18491987
    Gur S, Sikka SC, Hellstrom WJ: Novel phosphodiesterase-5 (PDE5) inhibitors in the alleviation of erectile dysfunction due to diabetes and ageing-induced oxidative stress. Expert Opin Investig Drugs. 2008 Jun;17(6):855-64. doi: 10.1517/13543784.17.6.855 .
  • PMID: 23675780
    Bruzziches R, Francomano D, Gareri P, Lenzi A, Aversa A: An update on pharmacological treatment of erectile dysfunction with phosphodiesterase type 5 inhibitors. Expert Opin Pharmacother. 2013 Jul;14(10):1333-44. doi: 10.1517/14656566.2013.799665. Epub 2013 May 16.
  • PMID: 23372609
    Kedia GT, Uckert S, Assadi-Pour F, Kuczyk MA, Albrecht K: Avanafil for the treatment of erectile dysfunction: initial data and clinical key properties. Ther Adv Urol. 2013 Feb;5(1):35-41. doi: 10.1177/1756287212466282.

Contoh Produk & Brand

Produk: 37 • International brands: 1
Produk
  • Avanafil
    Tablet • 50 mg/1 • Oral • US • Generic • Approved
  • Avanafil
    Tablet • 100 mg/1 • Oral • US • Generic • Approved
  • Avanafil
    Tablet • 200 mg/1 • Oral • US • Generic • Approved
  • Spedra
    Tablet • 50 mg • Oral • EU • Approved
  • Spedra
    Tablet • 50 mg • Oral • EU • Approved
  • Spedra
    Tablet • 50 mg • Oral • EU • Approved
  • Spedra
    Tablet • 100 mg • Oral • EU • Approved
  • Spedra
    Tablet • 100 mg • Oral • EU • Approved
Menampilkan 8 dari 37 produk.
International Brands
  • Spedra — A. Menarini Farmaceutica Internazionale SRL

Sekuens Gen/Protein (FASTA)

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