Alfuzosin
Identification
- Name
- Alfuzosin
- Accession Number
- DB00346
- Description
Alfuzosin (INN, provided as the hydrochloride salt) is an alpha-adrenergic blocker used to treat benign prostatic hyperplasia (BPH). It works by relaxing the muscles in the prostate and bladder neck, making it easier to urinate.
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
Structure for Alfuzosin (DB00346)
- Weight
- Average: 389.4488
Monoisotopic: 389.206304377 - Chemical Formula
- C19H27N5O4
- Synonyms
- (±)-N-[3-[(4-amino-6,7-dimethoxy-2-quinazolinyl)methylamino]propyl]tetrahydro-2-furamide
- Alfuzosin
- Alfuzosina
- Alfuzosine
- Alfuzosinum
- N-[3-[(4-amino-6,7-dimethoxy-quinazolin-2-yl)- methyl-amino]propyl] tetrahydrofuran- 2-carboxamide
- External IDs
- SL 77499-10
Pharmacology
- Indication
For the reduction of urinary obstruction and relief of associated manifestations (eg. sensation of incomplete bladder emptying or straining, urgency, interrupted or weak stream) in patients with symptomatic beningn prostatic hyperplasia.
- Associated Conditions
- Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
Learn More- Pharmacodynamics
Alfuzosin is a quinazoline-derivative alpha-adrenergic blocking agent used to treat hypertension and benign prostatic hyperplasia. Accordingly, alfuzosin is a selective inhibitor of the alpha(1) subtype of alpha adrenergic receptors. In the human prostate, alfuzosin antagonizes phenylephrine (alpha(1) agonist)-induced contractions, in vitro, and binds with high affinity to the alpha1a adrenoceptor, which is thought to be the predominant functional type in the prostate. Studies in normal human subjects have shown that alfuzosin competitively antagonized the pressor effects of phenylephrine (an alpha(1) agonist) and the systolic pressor effect of norepinephrine. The antihypertensive effect of alfuzosin results from a decrease in systemic vascular resistance and the parent compound alfuzosin is primarily responsible for the antihypertensive activity.
- Mechanism of action
Alfuzosin is a non-subtype specific alpha(1)-adrenergic blocking agent that exhibits selectivity for alpha(1)-adrenergic receptors in the lower urinary tract. Inhibition of these adrenoreceptors leads to the relaxation of smooth muscle in the bladder neck and prostate, resulting in the improvement in urine flow and a reduction in symptoms in benign prostate hyperplasia. Alfuzosin also inhibits the vasoconstrictor effect of circulating and locally released catecholamines (epinephrine and norepinephrine), resulting in peripheral vasodilation.
Target Actions Organism AAlpha-1A adrenergic receptor antagonistHumans AAlpha-1B adrenergic receptor antagonistHumans AAlpha-1D adrenergic receptor antagonistHumans UPotassium voltage-gated channel subfamily H member 2 inhibitorHumans - Absorption
Absorption is 50% lower under fasting conditions
- Volume of distribution
- 3.2 L/kg [healthy male middle-aged volunteers]
- Protein binding
82%-90%
- Metabolism
Hepatic. Alfuzosin undergoes extensive metabolism by the liver, with only 11% of the administered dose excreted unchanged in the urine. Alfuzosin is metabolized by three metabolic pathways: oxidation, O-demethylations, and N-dealkylation. The metabolites are not pharmacologically active. CYP3A4 is the principal hepatic enzyme isoform involved in its metabolism.
- Route of elimination
Following oral administration of 14C-labeled alfuzosin solution, the recovery of radioactivity after 7 days (expressed as a percentage of the administered dose) was 69% in feces and 24% in urine.
- Half-life
10 hours
- Clearance
- Not Available
- Adverse Effects
Learn about our commercial Adverse Effects data.
Learn More- Toxicity
Side effects are dizziness (due to postural hypotension), upper respiratory tract infection, headache, and fatigue.
- Affected organisms
- Humans and other mammals
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Unlock Additional DataAbametapir The serum concentration of Alfuzosin can be increased when it is combined with Abametapir. Acalabrutinib The metabolism of Alfuzosin can be decreased when combined with Acalabrutinib. Acebutolol Alfuzosin may increase the hypotensive activities of Acebutolol. Acetaminophen The metabolism of Alfuzosin can be decreased when combined with Acetaminophen. Acetazolamide The metabolism of Alfuzosin can be decreased when combined with Acetazolamide. Acrivastine The risk or severity of QTc prolongation can be increased when Alfuzosin is combined with Acrivastine. Adenosine The risk or severity of QTc prolongation can be increased when Alfuzosin is combined with Adenosine. Ajmaline The risk or severity of QTc prolongation can be increased when Alfuzosin is combined with Ajmaline. Aldesleukin The metabolism of Alfuzosin can be decreased when combined with Aldesleukin. Alimemazine The risk or severity of QTc prolongation can be increased when Alfuzosin is combined with Alimemazine. Additional Data Available- Extended DescriptionExtended Description
Extended description of the mechanism of action and particular properties of each drug interaction.
Learn more - Severity
- Evidence Level
- ActionAction
An effect category for each drug interaction. Know how this interaction affects the subject drug.
Learn more
- Food Interactions
- Take after a meal.
Products
- Product Ingredients
Ingredient UNII CAS InChI Key Alfuzosin hydrochloride 75046A1XTN 81403-68-1 YTNKWDJILNVLGX-UHFFFAOYSA-N - Product Images
- International/Other 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) / Rantral (Ranbaxy) / Uriten (Square) / Xantral (Sanofi-Aventis) / Xelflo (Sun) / Zatral (Eskayef)
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Unlock Additional DataAlfuzosin Tablet, extended release Oral Sivem Pharmaceuticals Ulc 2015-11-25 Not applicable Canada 
Alfuzosin Tablet, extended release Oral Pro Doc Limitee 2013-11-21 2018-11-30 Canada Uroxatral Tablet, extended release 10 mg/1 Oral Physicians Total Care, Inc. 2004-06-22 Not applicable US 
Uroxatral Tablet, extended release 10 mg/1 Oral Sanofi Aventis 2009-06-05 2015-09-30 US 
Uroxatral Tablet, extended release 10 mg/1 Oral Stat Rx USA 2009-06-05 Not applicable US Uroxatral Tablet, extended release 10 mg/1 Oral Concordia Pharmaceuticals Inc. 2013-06-03 Not applicable US Uroxatral Tablet, extended release 10 mg/1 Oral Covis Pharmaceuticals, Inc. 2013-06-03 2016-04-30 US Xatral Tablet, extended release Oral Sanofi Aventis 2002-02-21 Not applicable Canada Additional Data Available- Application NumberApplication Number
A unique ID assigned by the FDA when a product is submitted for approval by the labeller.
Learn more - Product CodeProduct Code
A governmentally-recognized ID which uniquely identifies the product within its regulatory market.
Learn more
- Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Unlock Additional DataAlfuzosin hydrochloride Tablet, extended release 10 mg/1 Oral bryant ranch prepack 2016-03-15 Not applicable US Alfuzosin Hydrochloride Tablet, extended release 10 mg/1 Oral Directrx 2015-12-21 Not applicable US Alfuzosin Hydrochloride Tablet, film coated, extended release 10 mg/1 Oral Aurobindo Pharma Limited 2012-08-30 Not applicable US Alfuzosin hydrochloride Tablet, extended release 10 mg/1 Oral Aphena Pharma Solutions Tennessee, Inc. 2012-10-02 Not applicable US Alfuzosin Hydrochloride Tablet, extended release 10 mg/1 Oral Mylan Pharmaceuticals Inc. 2011-08-09 2019-10-31 US Alfuzosin Hydrochloride Tablet, film coated, extended release 10 mg/1 Oral Rising Health, Llc 2012-08-30 Not applicable US Alfuzosin Hydrochloride Tablet, extended release 10 mg/1 Oral Aidarex Pharmaceuticals LLC 2011-11-22 Not applicable US Alfuzosin Hydrochloride Tablet, extended release 10 mg/1 Oral Apotex Corp. 2011-07-18 2020-12-31 US 
Alfuzosin Hydrochloride Tablet, extended release 10 mg/1 Oral bryant ranch prepack 2011-11-22 2017-01-30 US 
Alfuzosin hydrochloride Tablet, extended release 10 mg/1 Oral Exelan Pharmaceuticals Inc. 2012-10-02 Not applicable US Additional Data Available- Application NumberApplication Number
A unique ID assigned by the FDA when a product is submitted for approval by the labeller.
Learn more - Product CodeProduct Code
A governmentally-recognized ID which uniquely identifies the product within its regulatory market.
Learn more
Categories
- ATC Codes
- G04CA01 — Alfuzosin
- G04CA — Alpha-adrenoreceptor antagonists
- G04C — DRUGS USED IN BENIGN PROSTATIC HYPERTROPHY
- G04 — UROLOGICALS
- G — GENITO URINARY SYSTEM AND SEX HORMONES
- Drug Categories
- Adrenergic Agents
- Adrenergic alpha-1 Receptor Antagonists
- Adrenergic alpha-Antagonists
- Adrenergic Antagonists
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 Substrates
- Drugs Used in Benign Prostatic Hypertrophy
- Genito Urinary System and Sex Hormones
- Heterocyclic Compounds, Fused-Ring
- Neurotransmitter Agents
- Peripheral alpha-1 blockers
- Potential QTc-Prolonging Agents
- Prostatic Hyperplasia
- QTc Prolonging Agents
- Selective Alfa-1-adrenergic Blocking Agents
- Urological Agents
- Urologicals
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as quinazolinamines. These are heterocyclic aromatic compounds containing a quianazoline moiety substituted by one or more amine groups.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Diazanaphthalenes
- Sub Class
- Benzodiazines
- Direct Parent
- Quinazolinamines
- Alternative Parents
- Dialkylarylamines / Anisoles / Aminopyrimidines and derivatives / Alkyl aryl ethers / Imidolactams / Tetrahydrofurans / Heteroaromatic compounds / Propargyl-type 1,3-dipolar organic compounds / Oxacyclic compounds / Dialkyl ethers show 4 more
- Substituents
- Alkyl aryl ether / Aminopyrimidine / Anisole / Aromatic heteropolycyclic compound / Azacycle / Benzenoid / Carboximidic acid / Carboximidic acid derivative / Dialkyl ether / Dialkylarylamine show 15 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- monocarboxylic acid amide, tetrahydrofuranol, quinazolines (CHEBI:51141)
Chemical Identifiers
- UNII
- 90347YTW5F
- CAS number
- 81403-80-7
- InChI Key
- WNMJYKCGWZFFKR-UHFFFAOYSA-N
- InChI
- InChI=1S/C19H27N5O4/c1-24(8-5-7-21-18(25)14-6-4-9-28-14)19-22-13-11-16(27-3)15(26-2)10-12(13)17(20)23-19/h10-11,14H,4-9H2,1-3H3,(H,21,25)(H2,20,22,23)
- IUPAC Name
- N-{3-[(4-amino-6,7-dimethoxyquinazolin-2-yl)(methyl)amino]propyl}oxolane-2-carboxamide
- SMILES
- COC1=CC2=C(C=C1OC)C(N)=NC(=N2)N(C)CCCNC(=O)C1CCCO1
References
- Synthesis Reference
Mathias Scheer, "Alfuzosin tablets and synthesis." U.S. Patent US20060062845, issued March 23, 2006.
US20060062845- General References
- 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. [PubMed:11893233]
- 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. [PubMed:7682910]
- Andersson KE, Lepor H, Wyllie MG: Prostatic alpha 1-adrenoceptors and uroselectivity. Prostate. 1997 Feb 15;30(3):202-15. [PubMed:9122046]
- 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. [PubMed:16553574]
- 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. [PubMed:11750253]
- FDA Approved Drug Products: Alfuzosin Extended Release Tablets [Link]
- External Links
- Human Metabolome Database
- HMDB0014490
- KEGG Drug
- D07124
- PubChem Compound
- 2092
- PubChem Substance
- 46508512
- ChemSpider
- 2008
- BindingDB
- 50033110
- 17300
- ChEBI
- 51141
- ChEMBL
- CHEMBL709
- Therapeutic Targets Database
- DCL000664
- PharmGKB
- PA164774795
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- PDRhealth
- PDRhealth Drug Page
- Wikipedia
- Alfuzosin
- AHFS Codes
- 12:16.04.12 — Selective Alfa-1-adrenergic Blocking Agents
- FDA label
- Download (72.9 KB)
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Completed Treatment Benign Prostatic Hyperplasia (BPH) 1 4 Completed Treatment Benign Prostatic Hyperplasia (BPH) / Choroid Disease / Pupil Anomaly 1 4 Completed Treatment Benign Prostatic Hyperplasia (BPH) / Lower Urinary Tract Symptoms (LUTS) 1 4 Completed Treatment Benign Prostatic Hypertrophy 1 4 Completed Treatment BPH/LUTS/Sexual Functions 1 4 Completed Treatment Prostatic Diseases 1 4 Completed Treatment Prostatic Hyperplasia 4 4 Unknown Status Treatment Renal Colic 1 4 Withdrawn Treatment Benign Prostatic Hyperplasia (BPH) 1 3 Completed Not Available Ureteral Stent Discomfort 1
Pharmacoeconomics
- Manufacturers
- Sanofi aventis us llc
- Packagers
- A-S Medication Solutions LLC
- Atlantic Biologicals Corporation
- Heartland Repack Services LLC
- Lake Erie Medical and Surgical Supply
- Murfreesboro Pharmaceutical Nursing Supply
- Nucare Pharmaceuticals Inc.
- Physicians Total Care Inc.
- Sanofi-Aventis Inc.
- Stat Rx Usa
- Dosage Forms
Form Route Strength Tablet, extended release Oral Tablet, extended release Oral 10 MG Tablet, extended release Oral 5 MG Tablet, film coated, extended release Oral 10 mg/1 Tablet Oral 10 mg/1 Tablet, film coated Oral 2.5 MG Tablet, coated 2.5 MG Tablet, coated 5 MG Tablet Tablet, extended release Oral 10 mg/1 Tablet, extended release 10 mg Tablet, film coated Oral 5 mg Tablet 10 mg - Prices
Unit description Cost Unit Uroxatral 10 mg 24 Hour tablet 4.06USD tablet Uroxatral 10 mg tablet 3.95USD tablet DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region Unlock Additional DataUS4661491 No 1987-04-28 2011-01-18 US CA2264250 No 2005-07-05 2017-08-22 Canada US6149940 Yes 2000-11-21 2018-02-22 US Additional Data Available- Filed On
Properties
- State
- Solid
- Experimental Properties
Property Value Source logP 1.4 Not Available - Predicted Properties
Property Value Source Water Solubility 0.282 mg/mL ALOGPS logP 2.02 ALOGPS logP 1.19 ChemAxon logS -3.1 ALOGPS pKa (Strongest Acidic) 14.64 ChemAxon pKa (Strongest Basic) 7.3 ChemAxon Physiological Charge 1 ChemAxon Hydrogen Acceptor Count 8 ChemAxon Hydrogen Donor Count 2 ChemAxon Polar Surface Area 111.83 Å2 ChemAxon Rotatable Bond Count 8 ChemAxon Refractivity 107.11 m3·mol-1 ChemAxon Polarizability 42.71 Å3 ChemAxon Number of Rings 3 ChemAxon Bioavailability 1 ChemAxon Rule of Five Yes ChemAxon Ghose Filter Yes ChemAxon Veber's Rule No ChemAxon MDDR-like Rule Yes ChemAxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 1.0 Blood Brain Barrier + 0.6215 Caco-2 permeable - 0.5504 P-glycoprotein substrate Substrate 0.8105 P-glycoprotein inhibitor I Inhibitor 0.5971 P-glycoprotein inhibitor II Non-inhibitor 0.5479 Renal organic cation transporter Non-inhibitor 0.7288 CYP450 2C9 substrate Non-substrate 0.8722 CYP450 2D6 substrate Non-substrate 0.7748 CYP450 3A4 substrate Substrate 0.7766 CYP450 1A2 substrate Non-inhibitor 0.9045 CYP450 2C9 inhibitor Non-inhibitor 0.9071 CYP450 2D6 inhibitor Non-inhibitor 0.9231 CYP450 2C19 inhibitor Non-inhibitor 0.9025 CYP450 3A4 inhibitor Non-inhibitor 0.8309 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.8017 Ames test Non AMES toxic 0.559 Carcinogenicity Non-carcinogens 0.8721 Biodegradation Not ready biodegradable 0.9945 Rat acute toxicity 2.6826 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.8527 hERG inhibition (predictor II) Inhibitor 0.5929
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Protein heterodimerization activity
- Specific Function
- This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) prot...
- Gene Name
- ADRA1A
- Uniprot ID
- P35348
- Uniprot Name
- Alpha-1A adrenergic receptor
- Molecular Weight
- 51486.005 Da
References
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
- Kenny BA, Miller AM, Williamson IJ, O'Connell J, Chalmers DH, Naylor AM: Evaluation of the pharmacological selectivity profile of alpha 1 adrenoceptor antagonists at prostatic alpha 1 adrenoceptors: binding, functional and in vivo studies. Br J Pharmacol. 1996 Jun;118(4):871-8. [PubMed:8799556]
- Lee M: Alfuzosin hydrochloride for the treatment of benign prostatic hyperplasia. Am J Health Syst Pharm. 2003 Jul 15;60(14):1426-39. [PubMed:12892027]
- Andersson KE, Lepor H, Wyllie MG: Prostatic alpha 1-adrenoceptors and uroselectivity. Prostate. 1997 Feb 15;30(3):202-15. [PubMed:9122046]
- Lowe FC: Role of the newer alpha, -adrenergic-receptor antagonists in the treatment of benign prostatic hyperplasia-related lower urinary tract symptoms. Clin Ther. 2004 Nov;26(11):1701-13. [PubMed:15639685]
- Martin DJ, Lluel P, Guillot E, Coste A, Jammes D, Angel I: Comparative alpha-1 adrenoceptor subtype selectivity and functional uroselectivity of alpha-1 adrenoceptor antagonists. J Pharmacol Exp Ther. 1997 Jul;282(1):228-35. [PubMed:9223558]
- Faure C, Pimoule C, Vallancien G, Langer SZ, Graham D: Identification of alpha 1-adrenoceptor subtypes present in the human prostate. Life Sci. 1994;54(21):1595-605. [PubMed:8196478]
- Beique L, Por CP, Evans MF: Are the new selective alpha-blockers better than non-selective alpha-blockers for benign prostatic hyperplasia? Can Fam Physician. 1998 Dec;44:2659-62. [PubMed:9870119]
- McVary KT: BPH: epidemiology and comorbidities. Am J Manag Care. 2006 Apr;12(5 Suppl):S122-8. [PubMed:16613526]
- 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. [PubMed:16553574]
- 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. [PubMed:11750253]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Protein heterodimerization activity
- Specific Function
- This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) prot...
- Gene Name
- ADRA1B
- Uniprot ID
- P35368
- Uniprot Name
- Alpha-1B adrenergic receptor
- Molecular Weight
- 56835.375 Da
References
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
- Kenny BA, Miller AM, Williamson IJ, O'Connell J, Chalmers DH, Naylor AM: Evaluation of the pharmacological selectivity profile of alpha 1 adrenoceptor antagonists at prostatic alpha 1 adrenoceptors: binding, functional and in vivo studies. Br J Pharmacol. 1996 Jun;118(4):871-8. [PubMed:8799556]
- Andersson KE, Lepor H, Wyllie MG: Prostatic alpha 1-adrenoceptors and uroselectivity. Prostate. 1997 Feb 15;30(3):202-15. [PubMed:9122046]
- Lowe FC: Role of the newer alpha, -adrenergic-receptor antagonists in the treatment of benign prostatic hyperplasia-related lower urinary tract symptoms. Clin Ther. 2004 Nov;26(11):1701-13. [PubMed:15639685]
- Faure C, Pimoule C, Vallancien G, Langer SZ, Graham D: Identification of alpha 1-adrenoceptor subtypes present in the human prostate. Life Sci. 1994;54(21):1595-605. [PubMed:8196478]
- Beique L, Por CP, Evans MF: Are the new selective alpha-blockers better than non-selective alpha-blockers for benign prostatic hyperplasia? Can Fam Physician. 1998 Dec;44:2659-62. [PubMed:9870119]
- McVary KT: BPH: epidemiology and comorbidities. Am J Manag Care. 2006 Apr;12(5 Suppl):S122-8. [PubMed:16613526]
- 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. [PubMed:16553574]
- 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. [PubMed:11750253]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Alpha1-adrenergic receptor activity
- Specific Function
- This alpha-adrenergic receptor mediates its effect through the influx of extracellular calcium.
- Gene Name
- ADRA1D
- Uniprot ID
- P25100
- Uniprot Name
- Alpha-1D adrenergic receptor
- Molecular Weight
- 60462.205 Da
References
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
- Kenny BA, Miller AM, Williamson IJ, O'Connell J, Chalmers DH, Naylor AM: Evaluation of the pharmacological selectivity profile of alpha 1 adrenoceptor antagonists at prostatic alpha 1 adrenoceptors: binding, functional and in vivo studies. Br J Pharmacol. 1996 Jun;118(4):871-8. [PubMed:8799556]
- Andersson KE, Lepor H, Wyllie MG: Prostatic alpha 1-adrenoceptors and uroselectivity. Prostate. 1997 Feb 15;30(3):202-15. [PubMed:9122046]
- Lowe FC: Role of the newer alpha, -adrenergic-receptor antagonists in the treatment of benign prostatic hyperplasia-related lower urinary tract symptoms. Clin Ther. 2004 Nov;26(11):1701-13. [PubMed:15639685]
- Faure C, Pimoule C, Vallancien G, Langer SZ, Graham D: Identification of alpha 1-adrenoceptor subtypes present in the human prostate. Life Sci. 1994;54(21):1595-605. [PubMed:8196478]
- McVary KT: BPH: epidemiology and comorbidities. Am J Manag Care. 2006 Apr;12(5 Suppl):S122-8. [PubMed:16613526]
- 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. [PubMed:16553574]
- 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. [PubMed:11750253]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarization
- Specific Function
- Pore-forming (alpha) subunit of voltage-gated inwardly rectifying potassium channel. Channel properties are modulated by cAMP and subunit assembly. Mediates the rapidly activating component of the ...
- Gene Name
- KCNH2
- Uniprot ID
- Q12809
- Uniprot Name
- Potassium voltage-gated channel subfamily H member 2
- Molecular Weight
- 126653.52 Da
References
- Derek Chadwick, Jamie Goode (2005). The HERG Cardiac Potassium Channel: Structure, Function and Long QT Syndrome, Novartis Foundation Symposium. Wiley. [ISBN:0470021411]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Vitamin d3 25-hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
- Gene Name
- CYP3A4
- Uniprot ID
- P08684
- Uniprot Name
- Cytochrome P450 3A4
- Molecular Weight
- 57342.67 Da
References
- Guay DR: Extended-release alfuzosin hydrochloride: a new alpha-adrenergic receptor antagonist for symptomatic benign prostatic hyperplasia. Am J Geriatr Pharmacother. 2004 Mar;2(1):14-23. [PubMed:15555475]
Drug created on June 13, 2005 07:24 / Updated on October 26, 2020 22:41
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