Peringatan Keamanan

The oral LD50 of alfuzosin is 2300 mg/kg in male mice and 1950 mg/kg in female mice.L31648
An overdose of alfuzosin can cause hypotension. Cardiovascular support should be initiated immediately. The patient should be kept in the supine position to aid in restoring pressure and managing heart rate. Fluid resuscitation should also be considered in severe cases; sometimes, vasopressors are required. Renal function should be monitored frequently. Dialysis may not be of benefit to alfuzosin protein binding of up to 90%.L9251

Alfuzosin

DB00346

small molecule approved investigational

Deskripsi

Benign prostatic hyperplasia (BPH) refers to a benign growth or hyperplasia of the prostate and leads to lower urinary tract symptoms in men, such as urgency, frequency and changes to urine flow. The prevalence of BPH is as high as 50%-60% for males in their 60's, and this prevalence increases to 80%-90% of those over 70.A228483 Alfuzosin is an alpha-1 adrenergic blocker used in the symptomatic treatment of BPH that works by relaxing the muscles in the prostate and bladder neck.L31593 It was initially approved by the FDA in 2003 and is marketed by several pharmaceutical companies.L9251

Struktur Molekul 2D

Berat 389.4488
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The apparent elimination half-life of alfuzosin after oral administration is about 10 hours.[L9251] The terminal half-life is 3-5 hours.[L31638]
Volume Distribusi The volume of distribution of alfuzosin after intravenous administration in healthy volunteers is about 3.2 L/kg.[L9251] Alfuzosin distributes heavily to the tissues of the prostate.[A228693]
Klirens (Clearance) Exercise caution if renal clearance is < 30 mL/min.[L9251] The clearance of alfuzosin is increased in renal insufficiency (with or without dialysis), due to an increase in the free fraction.[L31638]

Absorpsi

Alfuzosin is readily absorbed in the gastrointestinal tract and the absolute bioavailability under fed conditions is 49%.L9251 In patients over 75 years of age, alfuzosin is absorbed more rapidly and peak plasma levels are higher.L31638 One source mentions a bioavailability of 64%.L31638 After multiple doses under fed conditions, Cmax is achieved in 8 hours. Cmax and AUC0-24 values are about 13.6 ng/mL and 194 ng·h/mL, respectively. Steady-state plasma concentrations are achieved after the second dose and are 1.2 to 1.6 times higher than after a single dose.L9251 With the extended-release formulation, alfuzosin release is sustained over 20 hours with a rate of dissolution ranging between 2 and 12 hours.A516

Metabolisme

Alfuzosin undergoes extensive hepatic metabolism; only 11% of the administered dose is detected unchanged in the urine. Alfuzosin is metabolism occurs via three metabolic pathways: oxidation, O-demethylations, and N-dealkylation. Metabolites of alfuzosin are not pharmacologically active and CYP3A4 is main hepatic cytochrome enzyme responsible for its metabolism.L9251

Rute Eliminasi

It is partially metabolised and excreted mainly in the bile and faeces. Following oral administration of a radiolabeled alfuzosin solution, the detection of radioactivity after one week was 69% in the feces and 24% in the urine.L9251

Interaksi Makanan

1 Data
  • 1. Take after a meal. Take alfuzosin after the same meal everyday. Do not take on an empty stomach.

Interaksi Obat

873 Data
Valsartan Alfuzosin may increase the hypotensive activities of Valsartan.
Ramipril Alfuzosin may increase the hypotensive activities of Ramipril.
Esmolol Alfuzosin may increase the hypotensive activities of Esmolol.
Betaxolol Alfuzosin may increase the hypotensive activities of Betaxolol.
Reserpine Alfuzosin may increase the hypotensive activities of Reserpine.
Remikiren Alfuzosin may increase the hypotensive activities of Remikiren.
Torasemide Alfuzosin may increase the hypotensive activities of Torasemide.
Bethanidine Alfuzosin may increase the hypotensive activities of Bethanidine.
Guanadrel Alfuzosin may increase the hypotensive activities of Guanadrel.
Metoprolol Alfuzosin may increase the hypotensive activities of Metoprolol.
Olmesartan Alfuzosin may increase the hypotensive activities of Olmesartan.
Chlorthalidone Alfuzosin may increase the hypotensive activities of Chlorthalidone.
Nitroprusside Alfuzosin may increase the hypotensive activities of Nitroprusside.
Atenolol Alfuzosin may increase the hypotensive activities of Atenolol.
Minoxidil Alfuzosin may increase the hypotensive activities of Minoxidil.
Timolol Alfuzosin may increase the hypotensive activities of Timolol.
Treprostinil Alfuzosin may increase the hypotensive activities of Treprostinil.
Amlodipine Alfuzosin may increase the hypotensive activities of Amlodipine.
Nimodipine Alfuzosin may increase the hypotensive activities of Nimodipine.
Nisoldipine Alfuzosin may increase the hypotensive activities of Nisoldipine.
Bendroflumethiazide Alfuzosin may increase the hypotensive activities of Bendroflumethiazide.
Fosinopril Alfuzosin may increase the hypotensive activities of Fosinopril.
Trandolapril Alfuzosin may increase the hypotensive activities of Trandolapril.
Metolazone Alfuzosin may increase the hypotensive activities of Metolazone.
Benazepril Alfuzosin may increase the hypotensive activities of Benazepril.
Bosentan Alfuzosin may increase the hypotensive activities of Bosentan.
Propranolol Alfuzosin may increase the hypotensive activities of Propranolol.
Clonidine Alfuzosin may increase the hypotensive activities of Clonidine.
Enalapril Alfuzosin may increase the hypotensive activities of Enalapril.
Cyclothiazide Alfuzosin may increase the hypotensive activities of Cyclothiazide.
Bisoprolol Alfuzosin may increase the hypotensive activities of Bisoprolol.
Candoxatril Alfuzosin may increase the hypotensive activities of Candoxatril.
Guanabenz Alfuzosin may increase the hypotensive activities of Guanabenz.
Mecamylamine Alfuzosin may increase the hypotensive activities of Mecamylamine.
Moexipril Alfuzosin may increase the hypotensive activities of Moexipril.
Eplerenone Alfuzosin may increase the hypotensive activities of Eplerenone.
Lisinopril Alfuzosin may increase the hypotensive activities of Lisinopril.
Nitroglycerin Alfuzosin may increase the hypotensive activities of Nitroglycerin.
Metyrosine Alfuzosin may increase the hypotensive activities of Metyrosine.
Hydroflumethiazide Alfuzosin may increase the hypotensive activities of Hydroflumethiazide.
Cryptenamine Alfuzosin may increase the hypotensive activities of Cryptenamine.
Perindopril Alfuzosin may increase the hypotensive activities of Perindopril.
Candesartan cilexetil Alfuzosin may increase the hypotensive activities of Candesartan cilexetil.
Fenoldopam Alfuzosin may increase the hypotensive activities of Fenoldopam.
Indapamide Alfuzosin may increase the hypotensive activities of Indapamide.
Tadalafil Alfuzosin may increase the hypotensive activities of Tadalafil.
Alprenolol Alfuzosin may increase the hypotensive activities of Alprenolol.
Eprosartan Alfuzosin may increase the hypotensive activities of Eprosartan.
Chlorothiazide Alfuzosin may increase the hypotensive activities of Chlorothiazide.
Quinapril Alfuzosin may increase the hypotensive activities of Quinapril.
Omapatrilat Alfuzosin may increase the hypotensive activities of Omapatrilat.
Pindolol Alfuzosin may increase the hypotensive activities of Pindolol.
Telmisartan Alfuzosin may increase the hypotensive activities of Telmisartan.
Methyldopa Alfuzosin may increase the hypotensive activities of Methyldopa.
Hydrochlorothiazide Alfuzosin may increase the hypotensive activities of Hydrochlorothiazide.
Guanfacine Alfuzosin may increase the hypotensive activities of Guanfacine.
Trichlormethiazide Alfuzosin may increase the hypotensive activities of Trichlormethiazide.
Deserpidine Alfuzosin may increase the hypotensive activities of Deserpidine.
Pentolinium Alfuzosin may increase the hypotensive activities of Pentolinium.
Trimethaphan Alfuzosin may increase the hypotensive activities of Trimethaphan.
Diazoxide Alfuzosin may increase the hypotensive activities of Diazoxide.
Bretylium Alfuzosin may increase the hypotensive activities of Bretylium.
Guanethidine Alfuzosin may increase the hypotensive activities of Guanethidine.
Rescinnamine Alfuzosin may increase the hypotensive activities of Rescinnamine.
Acebutolol Alfuzosin may increase the hypotensive activities of Acebutolol.
Captopril Alfuzosin may increase the hypotensive activities of Captopril.
Nadolol Alfuzosin may increase the hypotensive activities of Nadolol.
Epoprostenol Alfuzosin may increase the hypotensive activities of Epoprostenol.
Bepridil Alfuzosin may increase the hypotensive activities of Bepridil.
Practolol Alfuzosin may increase the hypotensive activities of Practolol.
Polythiazide Alfuzosin may increase the hypotensive activities of Polythiazide.
Cilazapril Alfuzosin may increase the hypotensive activities of Cilazapril.
Saprisartan Alfuzosin may increase the hypotensive activities of Saprisartan.
Spirapril Alfuzosin may increase the hypotensive activities of Spirapril.
Penbutolol Alfuzosin may increase the hypotensive activities of Penbutolol.
Oxprenolol Alfuzosin may increase the hypotensive activities of Oxprenolol.
Pargyline Alfuzosin may increase the hypotensive activities of Pargyline.
Dexpropranolol Alfuzosin may increase the hypotensive activities of Dexpropranolol.
Tienilic acid Alfuzosin may increase the hypotensive activities of Tienilic acid.
Debrisoquine Alfuzosin may increase the hypotensive activities of Debrisoquine.
Celiprolol Alfuzosin may increase the hypotensive activities of Celiprolol.
Nebivolol Alfuzosin may increase the hypotensive activities of Nebivolol.
Lofexidine Alfuzosin may increase the hypotensive activities of Lofexidine.
Ambrisentan Alfuzosin may increase the hypotensive activities of Ambrisentan.
Diethylnorspermine Alfuzosin may increase the hypotensive activities of Diethylnorspermine.
Pinacidil Alfuzosin may increase the hypotensive activities of Pinacidil.
Bupranolol Alfuzosin may increase the hypotensive activities of Bupranolol.
Temocapril Alfuzosin may increase the hypotensive activities of Temocapril.
Riociguat Alfuzosin may increase the hypotensive activities of Riociguat.
Macitentan Alfuzosin may increase the hypotensive activities of Macitentan.
Indenolol Alfuzosin may increase the hypotensive activities of Indenolol.
Hexamethonium Alfuzosin may increase the hypotensive activities of Hexamethonium.
Aliskiren Alfuzosin may increase the hypotensive activities of Aliskiren.
Nicorandil Alfuzosin may increase the hypotensive activities of Nicorandil.
Lacidipine Alfuzosin may increase the hypotensive activities of Lacidipine.
Moxonidine Alfuzosin may increase the hypotensive activities of Moxonidine.
Rauwolfia serpentina root Alfuzosin may increase the hypotensive activities of Rauwolfia serpentina root.
Enalaprilat Alfuzosin may increase the hypotensive activities of Enalaprilat.
Selexipag Alfuzosin may increase the hypotensive activities of Selexipag.
Angiotensin 1-7 Alfuzosin may increase the hypotensive activities of Angiotensin 1-7.

Target Protein

Alpha-1 adrenergic receptors ADRA1A
Alpha-1A adrenergic receptor ADRA1A
Alpha-1B adrenergic receptor ADRA1B
Alpha-1D adrenergic receptor ADRA1D

Referensi & Sumber

Synthesis reference: Mathias Scheer, "Alfuzosin tablets and synthesis." U.S. Patent US20060062845, issued March 23, 2006.
Artikel (PubMed)
  • PMID: 11893233
    McKeage K, Plosker GL: Alfuzosin: a review of the therapeutic use of the prolonged-release formulation given once daily in the management of benign prostatic hyperplasia. Drugs. 2002;62(4):633-53.
  • PMID: 7682910
    Wilde MI, Fitton A, McTavish D: Alfuzosin. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in benign prostatic hyperplasia. Drugs. 1993 Mar;45(3):410-29.
  • PMID: 9122046
    Andersson KE, Lepor H, Wyllie MG: Prostatic alpha 1-adrenoceptors and uroselectivity. Prostate. 1997 Feb 15;30(3):202-15.
  • PMID: 16553574
    Elhilali MM: Alfuzosin: an alpha1-receptor blocker for the treatment of lower urinary tract symptoms associated with benign prostatic hyperplasia. Expert Opin Pharmacother. 2006 Apr;7(5):583-96.
  • PMID: 11750253
    Roehrborn CG: Alfuzosin: overview of pharmacokinetics, safety, and efficacy of a clinically uroselective alpha-blocker. Urology. 2001 Dec;58(6 Suppl 1):55-63; discussion 63-4.
  • PMID: 16985902
    Roehrborn CG: Benign prostatic hyperplasia: an overview. Rev Urol. 2005;7 Suppl 9:S3-S14.
  • PMID: 18304211
    Schwinn DA, Roehrborn CG: Alpha1-adrenoceptor subtypes and lower urinary tract symptoms. Int J Urol. 2008 Mar;15(3):193-9. doi: 10.1111/j.1442-2042.2007.01956.x.
  • PMID: 12814682
    Mottet N, Bressolle F, Delmas V, Robert M, Costa P: Prostatic tissual distribution of alfuzosin in patients with benign prostatic hyperplasia following repeated oral administration. Eur Urol. 2003 Jul;44(1):101-5. doi: 10.1016/s0302-2838(03)00154-4.

Contoh Produk & Brand

Produk: 49 • International brands: 15
Produk
  • Alfuzosin
    Tablet, extended release • 10 mg • Oral • Canada • Approved
  • Alfuzosin
    Tablet, extended release • 10 mg • Oral • Canada • Approved
  • Alfuzosin
    Tablet, extended release • 10 mg • Oral • Canada • Approved
  • Alfuzosin Hydrochloride
    Tablet, extended release • 10 mg/1 • Oral • US • Generic • Approved
  • Alfuzosin Hydrochloride
    Tablet • 10 mg/1 • Oral • US • Generic • Approved
  • Alfuzosin Hydrochloride
    Tablet, extended release • 10 mg/1 • Oral • US • Generic • Approved
  • Alfuzosin hydrochloride
    Tablet, extended release • 10 mg/1 • Oral • US • Generic • Approved
  • Alfuzosin hydrochloride
    Tablet, extended release • 10 mg/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 49 produk.
International Brands
  • Alcinin — Pharmathen
  • Alfasin XR — Incepta
  • Alfetim — Sanofi-Aventis
  • Alfoo — Dr. Reddy's
  • Alfu — Rowex
  • Alfuran — Terapia
  • Alfusozina — Grey Inversiones
  • Flotral — Ranbaxy
  • Fual — Alkem
  • Profuzo — Neiss

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