alfuzosin Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
antihypertensive substances, prazosin derivatives 115 81403-80-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • alfuzosin
  • alfuzosin hydrochloride
  • xatral
  • SL 77
  • alfuzosin HCl
Alfuzosin is a selective antagonist of post-synaptic alpha1-adrenoreceptors, which are located in the prostate, bladder base, bladder neck, prostatic capsule, and prostatic urethra.
  • Molecular weight: 389.46
  • Formula: C19H27N5O4
  • CLOGP: 2.55
  • LIPINSKI: 0
  • HAC: 9
  • HDO: 2
  • TPSA: 111.83
  • ALOGS: -3.14
  • ROTB: 8

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
7.50 mg O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 11 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.34 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 55 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 1.50 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 5.90 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.14 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 4.80 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
June 12, 2003 FDA COVIS PHARMA SARL

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
ATC G04CA01 GENITO URINARY SYSTEM AND SEX HORMONES
UROLOGICALS
DRUGS USED IN BENIGN PROSTATIC HYPERTROPHY
Alpha-adrenoreceptor antagonists
ATC G04CA51 GENITO URINARY SYSTEM AND SEX HORMONES
UROLOGICALS
DRUGS USED IN BENIGN PROSTATIC HYPERTROPHY
Alpha-adrenoreceptor antagonists
MeSH PA D018663 Adrenergic Agents
MeSH PA D058668 Adrenergic alpha-1 Receptor Antagonists
FDA EPC N0000175553 alpha-Adrenergic Blocker
MeSH PA D000317 Adrenergic alpha-Antagonists
MeSH PA D018674 Adrenergic Antagonists
MeSH PA D018377 Neurotransmitter Agents
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:35674 antihypertensive agent
CHEBI has role CHEBI:37890 alpha-adrenergic antagonist
MeSH PA D064804 Urological Agents

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Benign prostatic hyperplasia indication 266569009
Orthostatic hypotension contraindication 28651003
Torsades de pointes contraindication 31722008
Low blood pressure contraindication 45007003
Acute nephropathy contraindication 58574008
Hepatic failure contraindication 59927004
Cataract surgery contraindication 110473004
Prolonged QT interval contraindication 111975006
Angina pectoris contraindication 194828000
Micturition syncope contraindication 234168001
Disease of liver contraindication 235856003 DOID:409
Intraoperative floppy iris syndrome contraindication 418801006
Congenital long QT syndrome contraindication 442917000
Progressive Angina Pectoris contraindication

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 13.09 acidic
pKa2 7.22 Basic
pKa3 0.97 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Alpha-1D adrenergic receptor GPCR ANTAGONIST Ki 8.44 CHEMBL CHEMBL
Alpha-1A adrenergic receptor GPCR ANTAGONIST Ki 8.09 CHEMBL CHEMBL
Alpha-1B adrenergic receptor GPCR ANTAGONIST Ki 8.55 CHEMBL CHEMBL
Alpha-1A adrenergic receptor GPCR Ki 7.64 CHEMBL
Alpha-1D adrenergic receptor GPCR Ki 8.46 CHEMBL

External reference:

IDSource
4021396 VUID
N0000148814 NUI
C0051150 UMLSCUI
D01692 KEGG_DRUG
75046A1XTN UNII
81403-68-1 SECONDARY_CAS_RN
349912006 SNOMEDCT_US
005431 NDDF
17300 RXNORM
d04797 MMSL
395954002 SNOMEDCT_US
4021396 VANDF
5357 INN_ID
CHEMBL709 ChEMBL_ID
DB00346 DRUGBANK_ID
CHEMBL1723 ChEMBL_ID
CHEBI:51141 CHEBI
7109 IUPHAR_LIGAND_ID
C047638 MESH_SUPPLEMENTAL_RECORD_UI
2092 PUBCHEM_CID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Alfuzosin hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0440-5000 TABLET, EXTENDED RELEASE 10 mg ORAL ANDA 16 sections
ALFUZOSIN HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 13668-021 TABLET, EXTENDED RELEASE 10 mg ORAL ANDA 17 sections
Uroxatral HUMAN PRESCRIPTION DRUG LABEL 1 16590-279 TABLET, EXTENDED RELEASE 10 mg ORAL NDA 11 sections
Alfuzosin hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 29300-155 TABLET, EXTENDED RELEASE 10 mg ORAL ANDA 16 sections
Alfuzosin Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 31722-302 TABLET 10 mg ORAL ANDA 17 sections
Alfuzosin Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 33261-994 TABLET, EXTENDED RELEASE 10 mg ORAL ANDA 18 sections
Alfuzosin Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 43353-746 TABLET, EXTENDED RELEASE 10 mg ORAL ANDA 18 sections
Alfuzosin hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 43353-945 TABLET, EXTENDED RELEASE 10 mg ORAL ANDA 17 sections
Alfuzosin Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 47335-956 TABLET, EXTENDED RELEASE 10 mg ORAL ANDA 18 sections
Uroxatral HUMAN PRESCRIPTION DRUG LABEL 1 54868-5046 TABLET, EXTENDED RELEASE 10 mg ORAL NDA 18 sections
Alfuzosin Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 54868-6329 TABLET, EXTENDED RELEASE 10 mg ORAL ANDA 19 sections
Alfuzosin Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 55648-738 TABLET 10 mg ORAL ANDA 17 sections
Alfuzosin Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 57237-114 TABLET, FILM COATED, EXTENDED RELEASE 10 mg ORAL ANDA 17 sections
Uroxatral HUMAN PRESCRIPTION DRUG LABEL 1 59212-200 TABLET, EXTENDED RELEASE 10 mg ORAL NDA 17 sections
Alfuzosin Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 60505-2850 TABLET, EXTENDED RELEASE 10 mg ORAL ANDA 18 sections
ALFUZOSIN HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 61919-349 TABLET, EXTENDED RELEASE 10 mg ORAL ANDA 18 sections
Alfuzosin hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 63629-7907 TABLET, EXTENDED RELEASE 10 mg ORAL ANDA 17 sections
Alfuzosin Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 64679-738 TABLET 10 mg ORAL ANDA 17 sections
Alfuzosin Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 65862-249 TABLET, FILM COATED, EXTENDED RELEASE 10 mg ORAL ANDA 17 sections
Alfuzosin Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 69097-844 TABLET 10 mg ORAL ANDA 17 sections
Alfuzosin Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 70934-306 TABLET, EXTENDED RELEASE 10 mg ORAL ANDA 18 sections
Alfuzosin hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 76282-302 TABLET, EXTENDED RELEASE 10 mg ORAL ANDA 16 sections