Alfuzosin

Identification

Summary

Alfuzosin is an alpha-1 adrenergic antagonist used in the symptomatic management of benign prostatic hypertrophy (BPH).

Brand Names
Uroxatral, Xatral
Generic Name
Alfuzosin
DrugBank Accession Number
DB00346
Background

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 70.6 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.10 It was initially approved by the FDA in 2003 and is marketed by several pharmaceutical companies.9

Type
Small Molecule
Groups
Approved, Investigational
Structure
Thumb
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

Alfuzosin is used to treat the signs and symptoms of benign prostatic hyperplasia (BPH).9

Pharmacology
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Associated Conditions
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Contraindications
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Pharmacodynamics

By selectively inhibiting alpha adrenergic receptors in the lower urinary tract, alfuzosin causes smooth muscle relaxation in the bladder neck and prostate, improving urine flow, thereby reducing BPH symptoms.9 Additionally, alfuzosin reduces the vasoconstrictor effect of catecholamines (epinephrine and norepinephrine), leading to peripheral vasodilation.11 This leads to a risk of postural hypotension/syncope, and prescribing information warns that caution should be exercised in patients who take nitrates, antihypertensives, or have experienced decreased blood pressure after using other medications.9

Mechanism of action

Alpha(1)-adrenoreceptors are found in the prostate, bladder base, bladder neck, prostatic capsule, and prostatic urethra; their activation may lead to contraction of smooth muscle and urinary symptoms in patients with BPH.7,9 Alfuzosin selectively binds to and inhibits alpha(1)-adrenergic receptors in the lower urinary tract.3 This leads to the relaxation of smooth muscle in both the prostate and bladder neck, resulting in the improvement in urine flow and a reduction of urinary symptoms.9

TargetActionsOrganism
AAlpha-1A adrenergic receptor
antagonist
Humans
AAlpha-1B adrenergic receptor
antagonist
Humans
AAlpha-1D adrenergic receptor
antagonist
Humans
AAlpha-1 adrenergic receptors
antagonist
Humans
Absorption

Alfuzosin is readily absorbed in the gastrointestinal tract and the absolute bioavailability under fed conditions is 49%.9 In patients over 75 years of age, alfuzosin is absorbed more rapidly and peak plasma levels are higher.12 One source mentions a bioavailability of 64%.12 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.9 With the extended-release formulation, alfuzosin release is sustained over 20 hours with a rate of dissolution ranging between 2 and 12 hours.1

Volume of distribution

The volume of distribution of alfuzosin after intravenous administration in healthy volunteers is about 3.2 L/kg.9 Alfuzosin distributes heavily to the tissues of the prostate.8

Protein binding

The protein biding of alfuzosin is moderate and ranges from 82% to 90%.9 Alfuzosin is 68.2% bound to human serum albumin and 52.5% bound to human serum alpha-glycoprotein.12

Metabolism

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.9

Route of elimination

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.9

Half-life

The apparent elimination half-life of alfuzosin after oral administration is about 10 hours.9 The terminal half-life is 3-5 hours.12

Clearance

Exercise caution if renal clearance is < 30 mL/min.9 The clearance of alfuzosin is increased in renal insufficiency (with or without dialysis), due to an increase in the free fraction.12

Adverse Effects
Adverseeffects
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Toxicity

The oral LD50 of alfuzosin is 2300 mg/kg in male mice and 1950 mg/kg in female mice.14 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%.9

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.
DrugInteraction
AbametapirThe serum concentration of Alfuzosin can be increased when it is combined with Abametapir.
AbirateroneThe metabolism of Alfuzosin can be decreased when combined with Abiraterone.
AcalabrutinibThe metabolism of Alfuzosin can be decreased when combined with Acalabrutinib.
AcebutololAlfuzosin may increase the hypotensive activities of Acebutolol.
AcetaminophenThe metabolism of Alfuzosin can be decreased when combined with Acetaminophen.
AcetazolamideThe metabolism of Alfuzosin can be decreased when combined with Acetazolamide.
AcrivastineThe risk or severity of QTc prolongation can be increased when Alfuzosin is combined with Acrivastine.
AdenosineThe risk or severity of QTc prolongation can be increased when Alfuzosin is combined with Adenosine.
AjmalineThe risk or severity of QTc prolongation can be increased when Alfuzosin is combined with Ajmaline.
AldesleukinThe metabolism of Alfuzosin can be decreased when combined with Aldesleukin.
Interactions
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Food Interactions
  • Take after a meal. Take alfuzosin after the same meal everyday. Do not take on an empty stomach.

Products

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Product Ingredients
IngredientUNIICASInChI Key
Alfuzosin hydrochloride75046A1XTN81403-68-1YTNKWDJILNVLGX-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
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
AlfuzosinTablet, extended release10 mgOralSivem Pharmaceuticals Ulc2015-11-25Not applicableCanada flag
AlfuzosinTablet, extended release10 mgOralPro Doc Limitee2013-11-212018-11-30Canada flag
UroxatralTablet, extended release10 mg/1OralCovis Pharmaceuticals, Inc.2013-06-032016-04-30US flag
UroxatralTablet, extended release10 mg/1OralConcordia Pharmaceuticals Inc.2013-06-03Not applicableUS flag
UroxatralTablet, extended release10 mg/1OralPhysicians Total Care, Inc.2004-06-22Not applicableUS flag54868 504620180907 15195 1m0apxe
UroxatralTablet, extended release10 mg/1OralSanofi Aventis2009-06-052015-09-30US flag00024 4200 10 nlmimage10 27201390
UroxatralTablet, extended release10 mg/1OralStat Rx USA2009-06-05Not applicableUS flag16590 027920210318 24370 18o2xaa
XatralTablet, extended release10 mgOralSanofi Aventis2002-02-21Not applicableCanada flag
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Alfuzosin HydrochlorideTablet, extended release10 mg/1OralSun Pharmaceutical Industries, Inc.2011-11-22Not applicableUS flag47335 0956 18 nlmimage10 ac12d656
Alfuzosin hydrochlorideTablet, extended release10 mg/1OralUnichem Pharmaceuticals (USA), Inc.2016-03-15Not applicableUS flag
Alfuzosin HydrochlorideTablet, extended release10 mg/1OralGolden State Medical Supply2011-12-152015-12-31US flag
Alfuzosin hydrochlorideTablet, extended release10 mg/1OralAphena Pharma Solutions Tennessee, Inc.2012-10-02Not applicableUS flag
Alfuzosin HydrochlorideTablet, extended release10 mg/1OralTorrent Pharmaceuticals Limited2011-07-18Not applicableUS flag13668 02120180913 8702 1118ud2
Alfuzosin HydrochlorideTablet10 mg/1OralWockhardt2012-08-15Not applicableUS flag
Alfuzosin hydrochlorideTablet, extended release10 mg/1Oralbryant ranch prepack2016-03-15Not applicableUS flag
Alfuzosin HydrochlorideTablet, extended release10 mg/1Oralbryant ranch prepack2011-11-22Not applicableUS flag
Alfuzosin HydrochlorideTablet, extended release10 mg/1OralMylan Pharmaceuticals Inc.2011-08-092019-10-31US flag
Alfuzosin HydrochlorideTablet, extended release10 mg/1Oralbryant ranch prepack2011-11-222017-01-30US flag63629 568720180907 15195 rbnpmb

Categories

ATC Codes
G04CA01 — AlfuzosinG04CA51 — Alfuzosin and finasteride
Drug Categories
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)
Affected organisms
  • Humans and other mammals
  • Rat
  • Mouse

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
  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. [Article]
  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. [Article]
  3. Andersson KE, Lepor H, Wyllie MG: Prostatic alpha 1-adrenoceptors and uroselectivity. Prostate. 1997 Feb 15;30(3):202-15. [Article]
  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. [Article]
  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. [Article]
  6. Roehrborn CG: Benign prostatic hyperplasia: an overview. Rev Urol. 2005;7 Suppl 9:S3-S14. [Article]
  7. 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. [Article]
  8. 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. [Article]
  9. FDA Approved Drug Products: Alfuzosin Extended Release Tablets [Link]
  10. NIH StatPearls: Benigh Prostatic Hyperplasia [Link]
  11. NIH StatPearls: Alpha adrenergic receptors [Link]
  12. Medicines UK: Alfuzosin hydrochloride tablets [Link]
  13. Cayman Chem: Alfuzosin MSDS [Link]
  14. Product monograph: Sandoz Alfuzosin (alfuzosin hydrochloride) prolonged-release tablets [Link]
Human Metabolome Database
HMDB0014490
KEGG Drug
D07124
PubChem Compound
2092
PubChem Substance
46508512
ChemSpider
2008
BindingDB
50033110
RxNav
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
FDA label
Download (72.9 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedTreatmentBenign Prostatic Hyperplasia (BPH)1
4CompletedTreatmentBenign Prostatic Hyperplasia (BPH) / Choroid Disease / Pupil Anomaly1
4CompletedTreatmentBenign Prostatic Hyperplasia (BPH) / Lower Urinary Tract Symptoms (LUTS)1
4CompletedTreatmentBenign Prostatic Hypertrophy1
4CompletedTreatmentBPH/LUTS/Sexual Functions1
4CompletedTreatmentProstatic Diseases1
4CompletedTreatmentProstatic Hyperplasia4
4Unknown StatusTreatmentRenal Colic1
4WithdrawnTreatmentBenign Prostatic Hyperplasia (BPH)1
3CompletedNot AvailableUreteral Stent Discomfort1

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
FormRouteStrength
Tablet, film coated, extended releaseOral10 mg/1
TabletOral10 mg/1
Tablet, extended releaseOral
Tablet, film coatedOral2.5 MG
Tablet, extended releaseOral5 MG
Tablet, coatedOral2.5 MG
Tablet, coatedOral5 MG
TabletOral
Tablet, extended releaseOral10 mg/1
Tablet, coatedOral
Tablet, film coatedOral
Tablet, extended releaseOral10 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)Region
US4661491No1987-04-282011-01-18US flag
CA2264250No2005-07-052017-08-22Canada flag
US6149940Yes2000-11-212018-02-22US flag

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)240https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021287s021lbl.pdf
boiling point (°C)688https://www.chemsrc.com/en/cas/81403-68-1_1026747.html
logP1.604https://www.researchgate.net/publication/235399114_Terpenes_Effect_of_lipophilicity_in_enhancing_transdermal_delivery_of_alfuzosin_hydrochloride
pKa8.13https://www.chemicalbook.com/ChemicalProductProperty_US_CB8703590.aspx
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 RuleNoChemAxon
MDDR-like RuleYesChemAxon
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)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-000i-0009000000-b390e2d32ee38fb79cf9
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-00dr-0039000000-1058f618ea52b7aa95e6
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-0aos-0195000000-97624e7dcce906c3a1ee
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-0udi-0391000000-6d58b29a79c5af262723
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-0udi-1970000000-b3cb9821b3584d86539f
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-0i6s-1920000000-50ca3c071a5548796b3a
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-014i-5900000000-b3a86e227650a23790ec
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-014i-9400000000-9929aaf0359abea0c166
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-014i-9100000000-b3dba930d4cfe0d28a8e
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0006-0009000000-58fd75abdf178ea1b331
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0006-0119000000-90a7799e494035d224e7
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0abi-5791000000-648d5529faeac9e35dc0
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-00di-9260000000-591f2bacf7d82aeba7e3
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-00di-9250000000-d107a0e9675604325bb1
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-00di-9340000000-f708562f3998488d7fce
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-00di-7910000000-3fe44ce2a42f727569e2
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-05fr-8900000000-dca38c682ad0b6c90b46
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0bvl-9300000000-bad5c36d48e0e93a82aa
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0006-0249000000-93552ff8c72ff220f172

Targets

Drugtargets2
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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
  1. 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. [Article]
  2. Lee M: Alfuzosin hydrochloride for the treatment of benign prostatic hyperplasia. Am J Health Syst Pharm. 2003 Jul 15;60(14):1426-39. [Article]
  3. Andersson KE, Lepor H, Wyllie MG: Prostatic alpha 1-adrenoceptors and uroselectivity. Prostate. 1997 Feb 15;30(3):202-15. [Article]
  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. [Article]
  5. 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. [Article]
  6. 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. [Article]
  7. 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. [Article]
  8. McVary KT: BPH: epidemiology and comorbidities. Am J Manag Care. 2006 Apr;12(5 Suppl):S122-8. [Article]
  9. 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. [Article]
  10. 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. [Article]
  11. FDA Approved Drug Products: Alfuzosin Extended Release Tablets [Link]
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
  1. 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. [Article]
  2. Andersson KE, Lepor H, Wyllie MG: Prostatic alpha 1-adrenoceptors and uroselectivity. Prostate. 1997 Feb 15;30(3):202-15. [Article]
  3. 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. [Article]
  4. 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. [Article]
  5. 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. [Article]
  6. McVary KT: BPH: epidemiology and comorbidities. Am J Manag Care. 2006 Apr;12(5 Suppl):S122-8. [Article]
  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. [Article]
  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. [Article]
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
  1. 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. [Article]
  2. Andersson KE, Lepor H, Wyllie MG: Prostatic alpha 1-adrenoceptors and uroselectivity. Prostate. 1997 Feb 15;30(3):202-15. [Article]
  3. 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. [Article]
  4. 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. [Article]
  5. McVary KT: BPH: epidemiology and comorbidities. Am J Manag Care. 2006 Apr;12(5 Suppl):S122-8. [Article]
  6. 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. [Article]
  7. 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. [Article]
Kind
Protein group
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...

Components:
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. [Article]
  2. 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. [Article]
  3. FDA Approved Drug Products: Alfuzosin Extended Release Tablets [Link]

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
  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. [Article]
  2. FDA Approved Drug Products: Alfuzosin Extended Release Tablets [Link]

Carriers

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Binder
General Function
Toxic substance binding
Specific Function
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
Gene Name
ALB
Uniprot ID
P02768
Uniprot Name
Serum albumin
Molecular Weight
69365.94 Da
References
  1. Medicines UK: Alfuzosin hydrochloride tablets [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Binder
General Function
Not Available
Specific Function
Functions as transport protein in the blood stream. Binds various ligands in the interior of its beta-barrel domain. Also binds synthetic drugs and influences their distribution and availability in...
Gene Name
ORM1
Uniprot ID
P02763
Uniprot Name
Alpha-1-acid glycoprotein 1
Molecular Weight
23511.38 Da
References
  1. Medicines UK: Alfuzosin hydrochloride tablets [Link]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. Zhao R, Raub TJ, Sawada GA, Kasper SC, Bacon JA, Bridges AS, Pollack GM: Breast cancer resistance protein interacts with various compounds in vitro, but plays a minor role in substrate efflux at the blood-brain barrier. Drug Metab Dispos. 2009 Jun;37(6):1251-8. doi: 10.1124/dmd.108.025064. Epub 2009 Mar 9. [Article]

Drug created on June 13, 2005 13:24 / Updated on September 28, 2021 07:54