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Identification
NameAlfuzosin
Accession NumberDB00346  (APRD00490)
TypeSmall Molecule
GroupsApproved, Investigational
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. [Wikipedia]

Structure
Thumb
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 Identifiers
  • SL 77499-10
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Alfuzosintablet (extended-release)10 mgoralSivem Pharmaceuticals Ulc2015-11-25Not applicableCanada
Alfuzosintablet (extended-release)10 mgoralPro Doc Limitee2013-11-21Not applicableCanada
Auro-alfuzosintablet (extended-release)10 mgoralAuro Pharma Inc2015-09-02Not applicableCanada
Sandoz Alfuzosintablet (extended-release)10 mgoralSandoz Canada Incorporated2008-08-28Not applicableCanada
Teva-alfuzosin Prtablet (extended-release)10 mgoralTeva Canada Limited2010-08-31Not applicableCanada
Uroxatraltablet, extended release10 mg/1oralSanofi Aventis U.S. Llc2009-06-05Not applicableUs
Uroxatraltablet, extended release10 mg/1oralConcordia Pharmaceuticals Inc.2013-06-03Not applicableUs
Uroxatraltablet, extended release10 mg/1oralPhysicians Total Care, Inc.2004-06-22Not applicableUs
Uroxatraltablet, extended release10 mg/1oralCovis Pharmaceuticals Inc.2013-06-03Not applicableUs
Uroxatraltablet, extended release10 mg/1oralStat Rx USA2009-06-05Not applicableUs
Xatraltablet (extended-release)10 mgoralSanofi Aventis Canada Inc2002-02-21Not applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Alfuzosin Hydrochloridetablet, film coated, extended release10 mg/1oralAurobindo Pharma Limited2012-08-30Not applicableUs
Alfuzosin Hydrochloridetablet, extended release10 mg/1oralMylan Pharmaceuticals Inc.2011-08-09Not applicableUs
Alfuzosin Hydrochloridetablet, extended release10 mg/1oralPhysicians Total Care, Inc.2012-02-22Not applicableUs
Alfuzosin Hydrochloridetablet10 mg/1oralWockhardt USA LLC.2012-08-15Not applicableUs
Alfuzosin Hydrochloridetablet, extended release10 mg/1oralSun Pharma Global FZE2011-11-22Not applicableUs
Alfuzosin Hydrochloridetablet, extended release10 mg/1oralDIRECT RX2015-12-21Not applicableUs
Alfuzosin Hydrochloridetablet, extended release10 mg/1oralApotex Corp.2011-07-18Not applicableUs
Alfuzosin Hydrochloridetablet, extended release10 mg/1oralAidarex Pharmaceuticals LLC2011-11-22Not applicableUs
Alfuzosin Hydrochloridetablet, extended release10 mg/1oralGolden State Medical Supply, Inc.2011-07-18Not applicableUs
Alfuzosin Hydrochloridetablet, film coated, extended release10 mg/1oralCitron Pharma LLC2012-08-30Not applicableUs
Alfuzosin Hydrochloridetablet, extended release10 mg/1oralExelan Pharmaceuticals Inc.2012-10-02Not applicableUs
Alfuzosin Hydrochloridetablet, extended release10 mg/1oralTorrent Pharmaceuticals Limited2011-07-18Not applicableUs
Alfuzosin Hydrochloridetablet, extended release10 mg/1oralUnichem Pharmaceuticals (USA), Inc.2016-03-15Not applicableUs
Alfuzosin Hydrochloridetablet10 mg/1oralWockhardt Limited2012-08-15Not applicableUs
Alfuzosin Hydrochloride ERtablet, extended release10 mg/1oralAv Kare, Inc.2012-03-13Not applicableUs
Alfuzosin Hydrochloride Extended Releasetablet10 mg/1oralCamber Pharmaceuticals2012-01-18Not applicableUs
Apo-alfuzosintablet (extended-release)10 mgoralApotex Inc2008-08-20Not applicableCanada
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
AlcininPharmathen
Alfasin XRIncepta
AlfetimSanofi-Aventis
AlfooDr. Reddy's
AlfuRowex
AlfuranTerapia
AlfusozinaGrey Inversiones
FlotralRanbaxy
FualAlkem
ProfuzoNeiss
RantralRanbaxy
UritenSquare
XantralSanofi-Aventis
XelfloSun
ZatralEskayef
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Alfuzosin Hydrochloride
ThumbNot applicableDBSALT001063
Categories
UNII90347YTW5F
CAS number81403-80-7
WeightAverage: 389.4488
Monoisotopic: 389.206304377
Chemical FormulaC19H27N5O4
InChI KeyInChIKey=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=C(OC)C=C2C(N)=NC(=NC2=C1)N(C)CCCNC(=O)C1CCCO1
Taxonomy
DescriptionThis 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.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassNaphthyridines
Sub ClassQuinazolines
Direct ParentQuinazolinamines
Alternative Parents
Substituents
  • Quinazolinamine
  • Dialkylarylamine
  • Anisole
  • Aminopyrimidine
  • Alkyl aryl ether
  • Imidolactam
  • Benzenoid
  • Pyrimidine
  • Primary aromatic amine
  • Saccharide
  • Heteroaromatic compound
  • Oxolane
  • Tertiary amine
  • Secondary carboxylic acid amide
  • Carboxamide group
  • Oxacycle
  • Azacycle
  • Ether
  • Dialkyl ether
  • Carboxylic acid derivative
  • Carboxylic acid amide
  • Hydrocarbon derivative
  • Primary amine
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationFor 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.
PharmacodynamicsAlfuzosin 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 actionAlfuzosin 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.
Related Articles
AbsorptionAbsorption is 50% lower under fasting conditions
Volume of distribution
  • 3.2 L/kg [healthy male middle-aged volunteers]
Protein binding82%-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 eliminationFollowing 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 life10 hours
ClearanceNot Available
ToxicitySide effects are dizziness (due to postural hypotension), upper respiratory tract infection, headache, and fatigue.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.6215
Caco-2 permeable-0.5504
P-glycoprotein substrateSubstrate0.8105
P-glycoprotein inhibitor IInhibitor0.5971
P-glycoprotein inhibitor IINon-inhibitor0.5479
Renal organic cation transporterNon-inhibitor0.7288
CYP450 2C9 substrateNon-substrate0.8722
CYP450 2D6 substrateNon-substrate0.7748
CYP450 3A4 substrateSubstrate0.7766
CYP450 1A2 substrateNon-inhibitor0.9045
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorNon-inhibitor0.9231
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorNon-inhibitor0.8309
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8017
Ames testNon AMES toxic0.559
CarcinogenicityNon-carcinogens0.8721
BiodegradationNot ready biodegradable0.9945
Rat acute toxicity2.6826 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8527
hERG inhibition (predictor II)Inhibitor0.5929
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Sanofi aventis us llc
Packagers
Dosage forms
FormRouteStrength
Tablet, film coated, extended releaseoral10 mg/1
Tabletoral10 mg/1
Tablet, extended releaseoral10 mg/1
Tablet (extended-release)oral10 mg
Prices
Unit descriptionCostUnit
Uroxatral 10 mg 24 Hour tablet4.06USD tablet
Uroxatral 10 mg tablet3.95USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2264250 No2005-07-052017-08-22Canada
US4661491 No1994-01-182011-01-18Us
US6149940 Yes1998-02-222018-02-22Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
logP1.4Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.282 mg/mLALOGPS
logP2.02ALOGPS
logP1.19ChemAxon
logS-3.1ALOGPS
pKa (Strongest Acidic)14.64ChemAxon
pKa (Strongest Basic)7.3ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count8ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area111.83 Å2ChemAxon
Rotatable Bond Count8ChemAxon
Refractivity107.11 m3·mol-1ChemAxon
Polarizability42.71 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

Mathias Scheer, “Alfuzosin tablets and synthesis.” U.S. Patent US20060062845, issued March 23, 2006.

US20060062845
General References
  1. 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 ]
  2. 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 ]
  3. Andersson KE, Lepor H, Wyllie MG: Prostatic alpha 1-adrenoceptors and uroselectivity. Prostate. 1997 Feb 15;30(3):202-15. [PubMed:9122046 ]
  4. 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 ]
  5. 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 ]
External Links
ATC CodesG04CA01G04CA51
AHFS Codes
  • 92:00.00
PDB EntriesNot Available
FDA labelDownload (72.9 KB)
MSDSNot Available
Interactions
Drug Interactions
Drug
AcebutololAcebutolol may increase the orthostatic hypotensive activities of Alfuzosin.
AliskirenAlfuzosin may increase the hypotensive activities of Aliskiren.
AmilorideAlfuzosin may increase the hypotensive activities of Amiloride.
AmlodipineAlfuzosin may increase the hypotensive activities of Amlodipine.
AprepitantThe serum concentration of Alfuzosin can be increased when it is combined with Aprepitant.
ArticaineAlfuzosin may decrease the vasoconstricting activities of Articaine.
AtazanavirThe serum concentration of Alfuzosin can be increased when it is combined with Atazanavir.
AtenololAtenolol may increase the orthostatic hypotensive activities of Alfuzosin.
AvanafilAvanafil may increase the hypotensive activities of Alfuzosin.
Azilsartan medoxomilAlfuzosin may increase the hypotensive activities of Azilsartan medoxomil.
BatimastatThe serum concentration of Alfuzosin can be increased when it is combined with Batimastat.
BenazeprilAlfuzosin may increase the hypotensive activities of Benazepril.
BendroflumethiazideBendroflumethiazide may increase the orthostatic hypotensive activities of Alfuzosin.
BetaxololBetaxolol may increase the orthostatic hypotensive activities of Alfuzosin.
BexaroteneThe serum concentration of Alfuzosin can be decreased when it is combined with Bexarotene.
BisoprololBisoprolol may increase the orthostatic hypotensive activities of Alfuzosin.
BoceprevirThe serum concentration of Alfuzosin can be increased when it is combined with Boceprevir.
BosentanThe serum concentration of Alfuzosin can be decreased when it is combined with Bosentan.
BumetanideAlfuzosin may increase the hypotensive activities of Bumetanide.
CandesartanAlfuzosin may increase the hypotensive activities of Candesartan.
CaptoprilAlfuzosin may increase the hypotensive activities of Captopril.
CarteololCarteolol may increase the orthostatic hypotensive activities of Alfuzosin.
CarvedilolCarvedilol may increase the orthostatic hypotensive activities of Alfuzosin.
CeritinibThe serum concentration of Alfuzosin can be increased when it is combined with Ceritinib.
ChlorothiazideAlfuzosin may increase the hypotensive activities of Chlorothiazide.
ChlorthalidoneAlfuzosin may increase the hypotensive activities of Chlorthalidone.
CilazaprilAlfuzosin may increase the hypotensive activities of Cilazapril.
CitalopramAlfuzosin may increase the QTc-prolonging activities of Citalopram.
ClarithromycinThe serum concentration of Alfuzosin can be increased when it is combined with Clarithromycin.
ClevidipineAlfuzosin may increase the hypotensive activities of Clevidipine.
ClonidineAlfuzosin may increase the hypotensive activities of Clonidine.
CobicistatThe serum concentration of Alfuzosin can be increased when it is combined with Cobicistat.
ConivaptanThe serum concentration of Alfuzosin can be increased when it is combined with Conivaptan.
DabrafenibThe serum concentration of Alfuzosin can be decreased when it is combined with Dabrafenib.
DapoxetineDapoxetine may increase the orthostatic hypotensive activities of Alfuzosin.
DarunavirThe serum concentration of Alfuzosin can be increased when it is combined with Darunavir.
DasatinibThe serum concentration of Alfuzosin can be increased when it is combined with Dasatinib.
DeferasiroxThe serum concentration of Alfuzosin can be decreased when it is combined with Deferasirox.
DiltiazemAlfuzosin may increase the hypotensive activities of Diltiazem.
DipivefrinAlfuzosin may decrease the vasoconstricting activities of Dipivefrin.
DofetilideAlfuzosin may increase the QTc-prolonging activities of Dofetilide.
DopamineAlfuzosin may decrease the vasoconstricting activities of Dopamine.
DoxazosinAlfuzosin may increase the antihypertensive activities of Doxazosin.
EnalaprilAlfuzosin may increase the hypotensive activities of Enalapril.
EnalaprilatAlfuzosin may increase the hypotensive activities of Enalaprilat.
EphedrineAlfuzosin may decrease the vasoconstricting activities of Ephedrine.
EpinephrineAlfuzosin may decrease the vasoconstricting activities of Epinephrine.
EplerenoneAlfuzosin may increase the hypotensive activities of Eplerenone.
EprosartanAlfuzosin may increase the hypotensive activities of Eprosartan.
EsmololEsmolol may increase the orthostatic hypotensive activities of Alfuzosin.
Etacrynic acidAlfuzosin may increase the hypotensive activities of Ethacrynic acid.
FelodipineAlfuzosin may increase the hypotensive activities of Felodipine.
FluconazoleThe metabolism of Alfuzosin can be decreased when combined with Fluconazole.
FosamprenavirThe serum concentration of Alfuzosin can be increased when it is combined with Fosamprenavir.
FosaprepitantThe serum concentration of Alfuzosin can be increased when it is combined with Fosaprepitant.
FosinoprilAlfuzosin may increase the hypotensive activities of Fosinopril.
FurosemideAlfuzosin may increase the hypotensive activities of Furosemide.
Fusidic AcidThe serum concentration of Alfuzosin can be increased when it is combined with Fusidic Acid.
GoserelinAlfuzosin may increase the QTc-prolonging activities of Goserelin.
GuanfacineAlfuzosin may increase the hypotensive activities of Guanfacine.
HydralazineAlfuzosin may increase the hypotensive activities of Hydralazine.
HydrochlorothiazideAlfuzosin may increase the hypotensive activities of Hydrochlorothiazide.
IdelalisibThe serum concentration of Alfuzosin can be increased when it is combined with Idelalisib.
IndapamideAlfuzosin may increase the hypotensive activities of Indapamide.
IndinavirThe serum concentration of Alfuzosin can be increased when it is combined with Indinavir.
IrbesartanAlfuzosin may increase the hypotensive activities of Irbesartan.
IsoflurophateThe serum concentration of Alfuzosin can be increased when it is combined with Isoflurophate.
IsradipineAlfuzosin may increase the hypotensive activities of Isradipine.
ItraconazoleThe serum concentration of Alfuzosin can be increased when it is combined with Itraconazole.
IvacaftorThe serum concentration of Alfuzosin can be increased when it is combined with Ivacaftor.
KetoconazoleThe serum concentration of Alfuzosin can be increased when it is combined with Ketoconazole.
LabetalolLabetalol may increase the orthostatic hypotensive activities of Alfuzosin.
LeuprolideAlfuzosin may increase the QTc-prolonging activities of Leuprolide.
LevonordefrinAlfuzosin may decrease the vasoconstricting activities of Levonordefrin.
LisinoprilAlfuzosin may increase the hypotensive activities of Lisinopril.
LosartanAlfuzosin may increase the hypotensive activities of Losartan.
LuliconazoleThe serum concentration of Alfuzosin can be increased when it is combined with Luliconazole.
MannitolAlfuzosin may increase the hypotensive activities of Mannitol.
MecamylamineAlfuzosin may increase the hypotensive activities of Mecamylamine.
MepivacaineAlfuzosin may decrease the vasoconstricting activities of Mepivacaine.
MethyclothiazideAlfuzosin may increase the hypotensive activities of Methyclothiazide.
MethyldopaAlfuzosin may increase the hypotensive activities of Methyldopa.
MetolazoneAlfuzosin may increase the hypotensive activities of Metolazone.
MetoprololMetoprolol may increase the orthostatic hypotensive activities of Alfuzosin.
MidodrineAlfuzosin may decrease the vasoconstricting activities of Midodrine.
MifepristoneThe serum concentration of Alfuzosin can be increased when it is combined with Mifepristone.
MinoxidilAlfuzosin may increase the hypotensive activities of Minoxidil.
MitotaneThe serum concentration of Alfuzosin can be decreased when it is combined with Mitotane.
MoexiprilAlfuzosin may increase the hypotensive activities of Moexipril.
MoxonidineAlfuzosin may increase the hypotensive activities of Moxonidine.
NadololNadolol may increase the orthostatic hypotensive activities of Alfuzosin.
NaphazolineAlfuzosin may decrease the vasoconstricting activities of Naphazoline.
NebivololNebivolol may increase the orthostatic hypotensive activities of Alfuzosin.
NefazodoneThe serum concentration of Alfuzosin can be increased when it is combined with Nefazodone.
NelfinavirThe serum concentration of Alfuzosin can be increased when it is combined with Nelfinavir.
NetupitantThe serum concentration of Alfuzosin can be increased when it is combined with Netupitant.
NicardipineAlfuzosin may increase the hypotensive activities of Nicardipine.
NifedipineAlfuzosin may increase the hypotensive activities of Nifedipine.
NimodipineAlfuzosin may increase the hypotensive activities of Nimodipine.
NisoldipineAlfuzosin may increase the hypotensive activities of Nisoldipine.
NitroglycerinAlfuzosin may increase the hypotensive activities of Nitroglycerin.
NitroprussideAlfuzosin may increase the hypotensive activities of Nitroprusside.
NorepinephrineAlfuzosin may decrease the vasoconstricting activities of Norepinephrine.
OlmesartanAlfuzosin may increase the hypotensive activities of Olmesartan.
OxymetazolineAlfuzosin may decrease the vasoconstricting activities of Oxymetazoline.
PalbociclibThe serum concentration of Alfuzosin can be increased when it is combined with Palbociclib.
PenbutololPenbutolol may increase the orthostatic hypotensive activities of Alfuzosin.
PerindoprilAlfuzosin may increase the hypotensive activities of Perindopril.
PhenelzinePhenelzine may increase the orthostatic hypotensive activities of Alfuzosin.
PheniramineAlfuzosin may decrease the vasoconstricting activities of Pheniramine.
PhenoxybenzamineAlfuzosin may increase the antihypertensive activities of Phenoxybenzamine.
PhentolamineAlfuzosin may increase the antihypertensive activities of Phentolamine.
PhenylephrineAlfuzosin may decrease the vasoconstricting activities of Phenylephrine.
PhenytoinThe metabolism of Alfuzosin can be increased when combined with Phenytoin.
PindololPindolol may increase the orthostatic hypotensive activities of Alfuzosin.
PosaconazoleThe serum concentration of Alfuzosin can be increased when it is combined with Posaconazole.
PrazosinPrazosin may increase the antihypertensive activities of Alfuzosin.
PropranololPropranolol may increase the orthostatic hypotensive activities of Alfuzosin.
PropylhexedrineAlfuzosin may decrease the vasoconstricting activities of Propylhexedrine.
PseudoephedrineAlfuzosin may decrease the vasoconstricting activities of Pseudoephedrine.
QuinaprilAlfuzosin may increase the hypotensive activities of Quinapril.
RacepinephrineAlfuzosin may decrease the vasoconstricting activities of Racepinephrine.
RamiprilAlfuzosin may increase the hypotensive activities of Ramipril.
ReserpineAlfuzosin may increase the hypotensive activities of Reserpine.
RitonavirThe serum concentration of Alfuzosin can be increased when it is combined with Ritonavir.
SaquinavirThe serum concentration of Alfuzosin can be increased when it is combined with Saquinavir.
SildenafilSildenafil may increase the hypotensive activities of Alfuzosin.
SilodosinAlfuzosin may increase the antihypertensive activities of Silodosin.
SiltuximabThe serum concentration of Alfuzosin can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Alfuzosin can be increased when it is combined with Simeprevir.
SotalolSotalol may increase the orthostatic hypotensive activities of Alfuzosin.
SpironolactoneAlfuzosin may increase the hypotensive activities of Spironolactone.
St. John's WortThe serum concentration of Alfuzosin can be decreased when it is combined with St. John's Wort.
StiripentolThe serum concentration of Alfuzosin can be increased when it is combined with Stiripentol.
TadalafilTadalafil may increase the hypotensive activities of Alfuzosin.
TamsulosinAlfuzosin may increase the antihypertensive activities of Tamsulosin.
TelaprevirThe serum concentration of Alfuzosin can be increased when it is combined with Telaprevir.
TelithromycinThe serum concentration of Alfuzosin can be increased when it is combined with Telithromycin.
TelmisartanAlfuzosin may increase the hypotensive activities of Telmisartan.
TerazosinAlfuzosin may increase the antihypertensive activities of Terazosin.
TimololTimolol may increase the orthostatic hypotensive activities of Alfuzosin.
TipranavirThe serum concentration of Alfuzosin can be increased when it is combined with Tipranavir.
TocilizumabThe serum concentration of Alfuzosin can be decreased when it is combined with Tocilizumab.
TorasemideAlfuzosin may increase the hypotensive activities of Torasemide.
TrandolaprilAlfuzosin may increase the hypotensive activities of Trandolapril.
TranylcypromineTranylcypromine may increase the orthostatic hypotensive activities of Alfuzosin.
TriamtereneAlfuzosin may increase the hypotensive activities of Triamterene.
TriprolidineAlfuzosin may decrease the vasoconstricting activities of Triprolidine.
ValsartanAlfuzosin may increase the hypotensive activities of Valsartan.
VardenafilVardenafil may increase the hypotensive activities of Alfuzosin.
VerapamilAlfuzosin may increase the hypotensive activities of Verapamil.
VoriconazoleThe serum concentration of Alfuzosin can be increased when it is combined with Voriconazole.
Food Interactions
  • Take after a meal (always the same meal), product bioavailability is reduced when taken on an empty stomach.

Targets

Kind
Protein
Organism
Human
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) proteins. Nuclear ADRA1A-ADRA1B heterooligomers regulate phenylephrine(PE)-stimulated ERK signaling in cardiac myocytes.
Gene Name:
ADRA1A
Uniprot ID:
P35348
Molecular Weight:
51486.005 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  2. 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 ]
  3. 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 ]
  4. Andersson KE, Lepor H, Wyllie MG: Prostatic alpha 1-adrenoceptors and uroselectivity. Prostate. 1997 Feb 15;30(3):202-15. [PubMed:9122046 ]
  5. 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 ]
  6. 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 ]
  7. 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 ]
  8. 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 ]
  9. McVary KT: BPH: epidemiology and comorbidities. Am J Manag Care. 2006 Apr;12(5 Suppl):S122-8. [PubMed:16613526 ]
  10. 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 ]
  11. 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
Human
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) proteins. Nuclear ADRA1A-ADRA1B heterooligomers regulate phenylephrine (PE)-stimulated ERK signaling in cardiac myocytes.
Gene Name:
ADRA1B
Uniprot ID:
P35368
Molecular Weight:
56835.375 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  2. 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 ]
  3. Andersson KE, Lepor H, Wyllie MG: Prostatic alpha 1-adrenoceptors and uroselectivity. Prostate. 1997 Feb 15;30(3):202-15. [PubMed:9122046 ]
  4. 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 ]
  5. 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 ]
  6. 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 ]
  7. McVary KT: BPH: epidemiology and comorbidities. Am J Manag Care. 2006 Apr;12(5 Suppl):S122-8. [PubMed:16613526 ]
  8. 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 ]
  9. 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
Human
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
Molecular Weight:
60462.205 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  2. 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 ]
  3. Andersson KE, Lepor H, Wyllie MG: Prostatic alpha 1-adrenoceptors and uroselectivity. Prostate. 1997 Feb 15;30(3):202-15. [PubMed:9122046 ]
  4. 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 ]
  5. 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 ]
  6. McVary KT: BPH: epidemiology and comorbidities. Am J Manag Care. 2006 Apr;12(5 Suppl):S122-8. [PubMed:16613526 ]
  7. 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 ]
  8. 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
Human
Pharmacological action
unknown
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 delayed rectifying potassium current in heart (IKr). Isoforms USO have no channel activity by themself, but modulates channel characteristics by forming heterotetramers with other isoforms which are r...
Gene Name:
KCNH2
Uniprot ID:
Q12809
Molecular Weight:
126653.52 Da
References
  1. 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
Human
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 reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. 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 ]
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Drug created on June 13, 2005 07:24 / Updated on July 30, 2016 03:07