Peringatan Keamanan

LD50 information

The oral LD50 of doxazosin in mice is >1000 mg/kg.L7288

Overdose information

Symptoms of overdose include hypotension, changes in heart rate, and drowsiness.A180676 Administer supportive treatment in case of an overdose with doxazosin. Remove unabsorbed doxazosin from the gastrointestinal tract, correct hypotension, and closely monitor vital signs.A180676

Doxazosin

DB00590

small molecule approved

Deskripsi

Doxazosin is an alpha-1 antagonist used for the treatment of benign prostatic hypertrophy (BPH) symptoms and hypertension. Other members of this drug class include Prazosin, Terazosin, Tamsulosin, and Alfuzosin.A180661 Because of its long-lasting effects, doxazosin can be administered once a day.A180649 It is marketed by Pfizer and was initially approved by the FDA in 1990.L7285

Struktur Molekul 2D

Berat 451.4751
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The terminal elimination half-life of doxazosin has been estimated at 9-12 hours according to some resources.[A180646,A180658] The FDA label indicates the elimination half-life of doxazosin is 22 hours.[L7282]
Volume Distribusi The volume of distribution of doxazosin is 1.0-1.9 L/kg.[A180658,A180682] In a study of radiolabeled doxazosin administered to pregnant rats, doxazosin was found to cross the placenta.[L7282]
Klirens (Clearance) The clearance of doxazosin is low and ranges from approximately 1-2 ml/min/kg.[A180646,A180682]

Absorpsi

Doxazosin is rapidly absorbed in the gastrointestinal tract and peak concentrations are achieved within 2-3 hours after administration.A180682 The bioavailability is about 60%-70%.A180658,L7282 The intake of food with doxazosin is not expected to cause clinically significant effects.L7282

Metabolisme

Hepatic metabolism of doxazosin produces inactive O-demethylated and C-hydroxylated metabolites. Metabolism occurs via O-demethylation of the quinazoline nucleus of doxazosin or via hydroxylation of its benzodioxan portion.L7282 The enzymes involved in the metabolism of doxazosin include CYP2C19L7297, CYP2D6, CYP2C19, and CYP3A4, which is the primary metabolizing enzyme.L7294 Doxazosin itself is considered to be mainly responsible for its pharmacological actionA180658, however, some active metabolites have been identified whose pharmacokinetics have not been adequately characterized.L7282

Rute Eliminasi

In a pharmacokinetic study using a 1 mg IV radiolabeled dose and a 2 mg oral dose, 63% of the ingested doxazosin was found to be excreted in the feces and about 9% of the dose was found to be excreted in the urine.A180658,L7282 Traces of radiolabeled unchanged drug were found in the urine and about 5% of the administered drug was found as unchanged drug excreted in the feces.L7282

Interaksi Makanan

2 Data
  • 1. Avoid alcohol.
  • 2. Take with or without food.

Interaksi Obat

1367 Data
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Doxazosin is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Doxazosin is combined with Levodopa.
Risperidone Doxazosin may increase the hypotensive activities of Risperidone.
Phenytoin The metabolism of Doxazosin can be increased when combined with Phenytoin.
Fosphenytoin The metabolism of Doxazosin can be increased when combined with Fosphenytoin.
Amifostine Doxazosin may increase the hypotensive activities of Amifostine.
Diazoxide Diazoxide may increase the hypotensive activities of Doxazosin.
Methylphenidate Methylphenidate may decrease the antihypertensive activities of Doxazosin.
Dexmethylphenidate Dexmethylphenidate may decrease the antihypertensive activities of Doxazosin.
Obinutuzumab Doxazosin may increase the hypotensive activities of Obinutuzumab.
Pentoxifylline Pentoxifylline may increase the hypotensive activities of Doxazosin.
Rituximab Doxazosin may increase the hypotensive activities of Rituximab.
Desmopressin Desmopressin may decrease the antihypertensive activities of Doxazosin.
Zolmitriptan Zolmitriptan may decrease the antihypertensive activities of Doxazosin.
Doxapram Doxapram may decrease the antihypertensive activities of Doxazosin.
Atropine Atropine may decrease the antihypertensive activities of Doxazosin.
Phenmetrazine Phenmetrazine may decrease the antihypertensive activities of Doxazosin.
Naratriptan Naratriptan may decrease the antihypertensive activities of Doxazosin.
Rizatriptan Rizatriptan may decrease the antihypertensive activities of Doxazosin.
Frovatriptan Frovatriptan may decrease the antihypertensive activities of Doxazosin.
Epicaptopril Epicaptopril may decrease the antihypertensive activities of Doxazosin.
1-benzylimidazole 1-benzylimidazole may decrease the antihypertensive activities of Doxazosin.
Amineptine Amineptine may decrease the antihypertensive activities of Doxazosin.
Naluzotan Naluzotan may decrease the antihypertensive activities of Doxazosin.
Nitrous oxide Nitrous oxide may decrease the antihypertensive activities of Doxazosin.
Saralasin Saralasin may decrease the antihypertensive activities of Doxazosin.
Cinitapride Cinitapride may decrease the antihypertensive activities of Doxazosin.
Tyramine Tyramine may decrease the antihypertensive activities of Doxazosin.
Ifenprodil Ifenprodil may decrease the antihypertensive activities of Doxazosin.
Dimetacrine Dimetacrine may decrease the antihypertensive activities of Doxazosin.
Butriptyline Butriptyline may decrease the antihypertensive activities of Doxazosin.
Moxisylyte Moxisylyte may decrease the antihypertensive activities of Doxazosin.
Oxaprotiline Oxaprotiline may decrease the antihypertensive activities of Doxazosin.
Atipamezole Atipamezole may decrease the antihypertensive activities of Doxazosin.
Tetrahydrocannabivarin Tetrahydrocannabivarin may decrease the antihypertensive activities of Doxazosin.
Piclozotan Piclozotan may decrease the antihypertensive activities of Doxazosin.
Idazoxan Idazoxan may decrease the antihypertensive activities of Doxazosin.
Tramazoline Tramazoline may decrease the antihypertensive activities of Doxazosin.
Amitriptylinoxide Amitriptylinoxide may decrease the antihypertensive activities of Doxazosin.
Dibenzepin Dibenzepin may decrease the antihypertensive activities of Doxazosin.
Quinupramine Quinupramine may decrease the antihypertensive activities of Doxazosin.
Trichloroethylene Trichloroethylene may decrease the antihypertensive activities of Doxazosin.
Fenozolone Fenozolone may decrease the antihypertensive activities of Doxazosin.
Melitracen Melitracen may decrease the antihypertensive activities of Doxazosin.
Lofepramine Lofepramine may decrease the antihypertensive activities of Doxazosin.
Xenon Xenon may decrease the antihypertensive activities of Doxazosin.
Iprindole Iprindole may decrease the antihypertensive activities of Doxazosin.
Buflomedil Buflomedil may decrease the antihypertensive activities of Doxazosin.
Metergoline Metergoline may decrease the antihypertensive activities of Doxazosin.
Diethyl ether Diethyl ether may decrease the antihypertensive activities of Doxazosin.
Imipramine oxide Imipramine oxide may decrease the antihypertensive activities of Doxazosin.
Mefenorex Mefenorex may decrease the antihypertensive activities of Doxazosin.
5-methoxy-N,N-dimethyltryptamine 5-methoxy-N,N-dimethyltryptamine may decrease the antihypertensive activities of Doxazosin.
Quinoline Yellow WS Quinoline Yellow WS may decrease the antihypertensive activities of Doxazosin.
Solriamfetol Solriamfetol may decrease the antihypertensive activities of Doxazosin.
Omapatrilat Omapatrilat may decrease the antihypertensive activities of Doxazosin.
Rescinnamine Rescinnamine may decrease the antihypertensive activities of Doxazosin.
Isoflurane Isoflurane may decrease the antihypertensive activities of Doxazosin.
Remifentanil Remifentanil may decrease the antihypertensive activities of Doxazosin.
Desflurane Desflurane may decrease the antihypertensive activities of Doxazosin.
Dutasteride Dutasteride may decrease the antihypertensive activities of Doxazosin.
Lisuride Lisuride may decrease the antihypertensive activities of Doxazosin.
Sufentanil Sufentanil may decrease the antihypertensive activities of Doxazosin.
Almotriptan Almotriptan may decrease the antihypertensive activities of Doxazosin.
Methoxyflurane Methoxyflurane may decrease the antihypertensive activities of Doxazosin.
Ergoloid mesylate Ergoloid mesylate may decrease the antihypertensive activities of Doxazosin.
Halothane Halothane may decrease the antihypertensive activities of Doxazosin.
Finasteride Finasteride may decrease the antihypertensive activities of Doxazosin.
Sevoflurane Sevoflurane may decrease the antihypertensive activities of Doxazosin.
Yohimbine Yohimbine may decrease the antihypertensive activities of Doxazosin.
Solifenacin Solifenacin may decrease the antihypertensive activities of Doxazosin.
Lysergic acid diethylamide Lysergic acid diethylamide may decrease the antihypertensive activities of Doxazosin.
Flibanserin Flibanserin may decrease the antihypertensive activities of Doxazosin.
Cariprazine Cariprazine may decrease the antihypertensive activities of Doxazosin.
Mianserin Mianserin may decrease the antihypertensive activities of Doxazosin.
Terguride Terguride may decrease the antihypertensive activities of Doxazosin.
Sumatriptan Sumatriptan may decrease the antihypertensive activities of Doxazosin.
Eletriptan Eletriptan may decrease the antihypertensive activities of Doxazosin.
Protriptyline Protriptyline may decrease the antihypertensive activities of Doxazosin.
Alfentanil Alfentanil may decrease the antihypertensive activities of Doxazosin.
Fentanyl Fentanyl may decrease the antihypertensive activities of Doxazosin.
Opipramol Opipramol may decrease the antihypertensive activities of Doxazosin.
Selpercatinib Selpercatinib may decrease the antihypertensive activities of Doxazosin.
Naxitamab Naxitamab may decrease the antihypertensive activities of Doxazosin.
Dabrafenib The serum concentration of Doxazosin can be decreased when it is combined with Dabrafenib.
Luliconazole The serum concentration of Doxazosin can be increased when it is combined with Luliconazole.
Dapoxetine Dapoxetine may increase the orthostatic hypotensive activities of Doxazosin.
Lurasidone Doxazosin may increase the hypotensive activities of Lurasidone.
Mirabegron The serum concentration of Doxazosin can be increased when it is combined with Mirabegron.
Nicorandil Nicorandil may increase the hypotensive activities of Doxazosin.
Molsidomine Molsidomine may increase the hypotensive activities of Doxazosin.
Carteolol Carteolol may increase the hypotensive activities of Doxazosin.
Dorzolamide Doxazosin may increase the hypotensive activities of Dorzolamide.
Bimatoprost Doxazosin may increase the hypotensive activities of Bimatoprost.
Metipranolol Doxazosin may increase the hypotensive activities of Metipranolol.
Unoprostone Doxazosin may increase the hypotensive activities of Unoprostone.
Ramipril Ramipril may increase the hypotensive activities of Doxazosin.
Olmesartan Olmesartan may increase the hypotensive activities of Doxazosin.
Chlorthalidone Chlorthalidone may increase the hypotensive activities of Doxazosin.
Nitroprusside Nitroprusside may increase the hypotensive activities of Doxazosin.

Target Protein

Alpha-1A adrenergic receptor ADRA1A
Alpha-1D adrenergic receptor ADRA1D
HERG human cardiac K+ channel KCNH2
Alpha-1B adrenergic receptor ADRA1B

Referensi & Sumber

Synthesis reference: K. S. Keshava Murthy, Gamini Weeratunga, Tianhao Zhou, Bhaskar Reddy Guntoori, "Process for the manufacture of intermediates suitable to make doxazosin, terazosin, prazosin, tiodazosin and related antihypertensive medicines." U.S. Patent US5919931, issued September, 1986.
Artikel (PubMed)
  • PMID: 12461301
    Cushman WC, Ford CE, Cutler JA, Margolis KL, Davis BR, Grimm RH, Black HR, Hamilton BP, Holland J, Nwachuku C, Papademetriou V, Probstfield J, Wright JT Jr, Alderman MH, Weiss RJ, Piller L, Bettencourt J, Walsh SM: Success and predictors of blood pressure control in diverse North American settings: the antihypertensive and lipid-lowering treatment to prevent heart attack trial (ALLHAT). J Clin Hypertens (Greenwich). 2002 Nov-Dec;4(6):393-404.
  • PMID: 27405770
    Rao G: Diagnosis, Epidemiology, and Management of Hypertension in Children. Pediatrics. 2016 Aug;138(2). pii: peds.2015-3616. doi: 10.1542/peds.2015-3616. Epub 2016 Jul 12.
  • PMID: 17523910
    Liatsikos EN, Katsakiori PF, Assimakopoulos K, Voudoukis T, Kallidonis P, Constantinides C, Athanasopoulos A, Stolzenburg JU, Perimenis P: Doxazosin for the management of distal-ureteral stones. J Endourol. 2007 May;21(5):538-41. doi: 10.1089/end.2006.0107.
  • PMID: 2939865
    Kaye B, Cussans NJ, Faulkner JK, Stopher DA, Reid JL: The metabolism and kinetics of doxazosin in man, mouse, rat and dog. Br J Clin Pharmacol. 1986;21 Suppl 1:19S-25S. doi: 10.1111/j.1365-2125.1986.tb02849.x.
  • PMID: 2899495
    Young RA, Brogden RN: Doxazosin. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in mild or moderate hypertension. Drugs. 1988 May;35(5):525-41. doi: 10.2165/00003495-198835050-00003.
  • PMID: 15330733
    Doggrell SA: After ALLHAT: doxazosin for the treatment of benign prostatic hyperplasia. Expert Opin Pharmacother. 2004 Sep;5(9):1957-64. doi: 10.1517/14656566.5.9.1957 .
  • PMID: 2884857
    Elliott HL, Meredith PA, Reid JL: Pharmacokinetic overview of doxazosin. Am J Cardiol. 1987 May 29;59(14):78G-81G. doi: 10.1016/0002-9149(87)90162-7.
  • PMID: 16985889
    Kaplan SA: alpha-Blocker Therapy: Current Update. Rev Urol. 2005;7 Suppl 8:S34-42.
Menampilkan 8 dari 18 artikel.

Contoh Produk & Brand

Produk: 337 • International brands: 10
Produk
  • Apo-doxazosin
    Tablet • 1 mg / tab • Oral • Canada • Generic • Approved
  • Apo-doxazosin
    Tablet • 2 mg / tab • Oral • Canada • Generic • Approved
  • Apo-doxazosin
    Tablet • 4 mg / tab • Oral • Canada • Generic • Approved
  • Cardura
    Tablet • 1 mg/1 • Oral • US • Approved
  • Cardura
    Tablet • 2 mg/1 • Oral • US • Approved
  • Cardura
    Tablet • 4 mg/1 • Oral • US • Approved
  • Cardura
    Tablet • 8 mg/1 • Oral • US • Approved
  • Cardura
    Tablet • 1 mg/1 • Oral • US • Approved
Menampilkan 8 dari 337 produk.
International Brands
  • Alfadil — Pfizer (Sweden)
  • Cardenalin — Pfizer (Japan; discontinued)
  • Cardular — Pfizer (Germany)
  • Cardura-1 — Pfizer (Canada)
  • Cardura-2 — Pfizer (Canada)
  • Cardura-4 — Pfizer (Canada)
  • Carduran — Pfizer (Brazil, Denmark, Norway, Spain)
  • Diblocin — AstraZeneca (Germany)
  • Normothen — Bioindustria (Italy)
  • Supressin — Pfizer (Austria)

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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