Identification

Name
Alfuzosin
Accession Number
DB00346  (APRD00490)
Type
Small Molecule
Groups
Approved, 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 IDs
SL 77499-10
Product Ingredients
IngredientUNIICASInChI Key
Alfuzosin Hydrochloride75046A1XTN81403-68-1YTNKWDJILNVLGX-UHFFFAOYSA-N
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
AlfuzosinTablet, extended release10 mgOralSivem Pharmaceuticals Ulc2015-11-25Not applicableCanada
AlfuzosinTablet, extended release10 mgOralPro Doc Limitee2013-11-21Not applicableCanada
Sandoz AlfuzosinTablet, extended release10 mgOralSandoz Canada Incorporated2008-08-28Not applicableCanada
UroxatralTablet, extended release10 mg/1OralConcordia Pharmaceuticals, Inc2013-06-03Not applicableUs
UroxatralTablet, extended release10 mg/1OralPhysicians Total Care, Inc.2004-06-22Not applicableUs54868 504620180907 15195 1m0apxe
UroxatralTablet, extended release10 mg/1OralSanofi Aventis2009-06-052015-09-30Us00024 4200 10 nlmimage10 27201390
UroxatralTablet, extended release10 mg/1OralStat Rx USA2009-06-05Not applicableUs
UroxatralTablet, extended release10 mg/1OralCovis Pharmaceuticals, Inc.2013-06-032016-04-30Us
XatralTablet, extended release10 mgOralSanofi Aventis2002-02-21Not applicableCanada
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Alfuzosin HydrochlorideTablet, extended release10 mg/1OralPhysicians Total Care, Inc.2012-02-22Not applicableUs54868 632920180907 15195 1iptl9z
Alfuzosin HydrochlorideTablet, extended release10 mg/1OralGolden State Medical Supply2011-12-152015-12-31Us
Alfuzosin HydrochlorideTablet, extended release10 mg/1OralAphena Pharma Solutions Tennessee, Inc.2011-08-09Not applicableUs
Alfuzosin HydrochlorideTablet, extended release10 mg/1OralTorrent Pharmaceuticals Limited2011-07-18Not applicableUs13668 02120180913 8702 1118ud2
Alfuzosin HydrochlorideTablet, extended release10 mg/1OralApotex Corporation2011-07-18Not applicableUs60505 2850 01 nlmimage10 30441840
Alfuzosin HydrochlorideTablet10 mg/1OralWockhardt2012-08-15Not applicableUs
Alfuzosin HydrochlorideTablet, extended release10 mg/1OralSun Pharma Global FZE2011-11-22Not applicableUs47335 0956 18 nlmimage10 ac12d656
Alfuzosin hydrochlorideTablet, extended release10 mg/1OralExelan Pharmaceuticals, Inc.2012-10-02Not applicableUs
Alfuzosin HydrochlorideTablet, extended release10 mg/1OralMylan Pharmaceuticals2011-08-09Not applicableUs
Alfuzosin hydrochlorideTablet, extended release10 mg/1OralAphena Pharma Solutions Tennessee, Inc.2012-10-02Not applicableUs
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)
Categories
UNII
90347YTW5F
CAS number
81403-80-7
Weight
Average: 389.4488
Monoisotopic: 389.206304377
Chemical Formula
C19H27N5O4
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=C(OC)C=C2C(N)=NC(=NC2=C1)N(C)CCCNC(=O)C1CCCO1

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
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.

TargetActionsOrganism
AAlpha-1A adrenergic receptor
antagonist
Human
AAlpha-1B adrenergic receptor
antagonist
Human
AAlpha-1D adrenergic receptor
antagonist
Human
UPotassium voltage-gated channel subfamily H member 2
inhibitor
Human
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
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
DrugInteraction
(R)-warfarinThe metabolism of (R)-warfarin can be decreased when combined with Alfuzosin.
(S)-WarfarinThe metabolism of (S)-Warfarin can be decreased when combined with Alfuzosin.
16-BromoepiandrosteroneThe metabolism of 16-Bromoepiandrosterone can be decreased when combined with Alfuzosin.
3,5-diiodothyropropionic acidThe metabolism of 3,5-diiodothyropropionic acid can be decreased when combined with Alfuzosin.
4-hydroxycoumarinThe metabolism of 4-hydroxycoumarin can be decreased when combined with Alfuzosin.
4-MethoxyamphetamineThe therapeutic efficacy of 4-Methoxyamphetamine can be decreased when used in combination with Alfuzosin.
5-androstenedioneThe metabolism of 5-androstenedione can be decreased when combined with Alfuzosin.
6-Deoxyerythronolide BThe metabolism of Alfuzosin can be decreased when combined with 6-Deoxyerythronolide B.
6-O-benzylguanineThe metabolism of 6-O-benzylguanine can be decreased when combined with Alfuzosin.
AbediterolThe therapeutic efficacy of Abediterol can be decreased when used in combination with Alfuzosin.
Food Interactions
  • Take after a meal (always the same meal), product bioavailability is reduced when taken on an empty stomach.

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
Human Metabolome Database
HMDB0014490
KEGG Drug
D01692
PubChem Compound
2092
PubChem Substance
46508512
ChemSpider
2008
BindingDB
50033110
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
ATC Codes
G04CA51 — Alfuzosin and finasterideG04CA01 — Alfuzosin
AHFS Codes
  • 12:16.04.12 — Selective Alfa-1-adrenergic Blocking Agents
FDA label
Download (72.9 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedTreatmentHealthy Volunteers1
2CompletedTreatmentAcute Urinary Retention1
2CompletedTreatmentBenign Prostatic Hyperplasia (BPH)1
2CompletedTreatmentOccasional Constipation1
2, 3TerminatedTreatmentBladder Dysfunction / Disseminated Sclerosis1
3CompletedNot AvailableUreteral Stent Discomfort1
3CompletedPreventionBenign Prostatic Hypertrophy (BPH) / Prostatic Hyperplasia / Urinary Retention1
3CompletedTreatmentAcute Urinary Retention / Prostatic Hyperplasia1
3CompletedTreatmentBenign Prostatic Hyperplasia (BPH)1
3CompletedTreatmentErectile Dysfunction (ED) / Lower Urinary Tract Symptoms (LUTS)1
3CompletedTreatmentHydronephrosis / Neurogenic Bladder Dysfunction1
3CompletedTreatmentNeurogenic Urinary Bladder1
3CompletedTreatmentProstatic Hyperplasia1
3CompletedTreatmentProstatitis1
3CompletedTreatmentUrinary Bladder Neurogenic1
3TerminatedTreatmentBenign Prostatic Hyperplasia (BPH)1
3TerminatedTreatmentProstatic Hyperplasia1
3TerminatedTreatmentUrinary Retention1
3Unknown StatusTreatmentRenal Stones1
3WithdrawnTreatmentUrinary Calculi1
4CompletedTreatmentBPH/LUTS/Sexual Functions1
4CompletedTreatmentBenign Prostatic Hyperplasia (BPH)1
4CompletedTreatmentBenign Prostatic Hyperplasia (BPH) / Lower Urinary Tract Symptoms (LUTS)1
4CompletedTreatmentBenign Prostatic Hypertrophy (BPH)1
4CompletedTreatmentProstatic Diseases1
4CompletedTreatmentProstatic Hyperplasia4
4Unknown StatusTreatmentRenal Colic1
4WithdrawnTreatmentBenign Prostatic Hyperplasia (BPH)1
Not AvailableCompletedTreatmentBenign Prostatic Hyperplasia (BPH) / Benign Prostatic Hypertrophy With Outflow Obstruction1
Not AvailableCompletedTreatmentProstatic Diseases1
Not AvailableUnknown StatusTreatmentBenign Prostatic Hypertrophy (BPH) / Erectile Dysfunction (ED)1
Not AvailableWithdrawnTreatmentRenal Stones1

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 releaseOral10 mg/1
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)
US4661491No1994-01-182011-01-18Us
CA2264250No2005-07-052017-08-22Canada
US6149940Yes1998-02-222018-02-22Us

Properties

State
Solid
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 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

Taxonomy

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
Quinazolinamine / Anisole / Dialkylarylamine / Alkyl aryl ether / Aminopyrimidine / Pyrimidine / Imidolactam / Benzenoid / Heteroaromatic compound / Tetrahydrofuran
show 15 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
monocarboxylic acid amide, tetrahydrofuranol, quinazolines (CHEBI:51141)

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) prot...
Gene Name
ADRA1A
Uniprot ID
P35348
Uniprot Name
Alpha-1A adrenergic receptor
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) prot...
Gene Name
ADRA1B
Uniprot ID
P35368
Uniprot Name
Alpha-1B adrenergic receptor
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
Uniprot Name
Alpha-1D adrenergic receptor
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
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
  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 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. [PubMed:15555475]

Drug created on June 13, 2005 07:24 / Updated on September 22, 2018 22:21