alfuzosin indications/contra

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

Drug dosage:

DoseUnitRoute
7.50 mg O

Approvals:

DateAgencyCompanyOrphan
June 12, 2003 FDA COVIS PHARMA SARL

FDA Adverse Event Reporting System

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MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Hypotension 319.32 41.20 109 948 49405 3335397
Syncope 256.43 41.20 79 978 25554 3359248
Dizziness 165.91 41.20 77 980 76435 3308367
Fall 155.22 41.20 68 989 58815 3325987
Orthostatic hypotension 121.14 41.20 31 1026 5005 3379797
Loss of consciousness 81.86 41.20 35 1022 28112 3356690
Thrombocytopenia 80.53 41.20 37 1020 35231 3349571
Agranulocytosis 77.23 41.20 22 1035 5290 3379512
Presyncope 73.07 41.20 21 1036 5210 3379592
Hepatitis 64.35 41.20 22 1035 9603 3375199
Urinary retention 61.32 41.20 20 1037 7552 3377250
Soft tissue mass 60.20 41.20 9 1048 80 3384722
Cholestasis 59.51 41.20 18 1039 5319 3379483
Hepatocellular injury 58.49 41.20 17 1040 4378 3380424
On and off phenomenon 58.46 41.20 10 1047 220 3384582
Eosinophilia 56.76 41.20 17 1040 4856 3379946
Illusion 53.85 41.20 10 1047 355 3384447
Stool analysis abnormal 53.03 41.20 8 1049 76 3384726
Malaise 51.68 41.20 34 1023 65143 3319659
Neutropenia 49.11 41.20 26 1031 33360 3351442
Confusional state 45.95 41.20 26 1031 37972 3346830
Nasal discomfort 45.03 41.20 10 1047 874 3383928
Acute kidney injury 44.48 41.20 28 1029 49655 3335147

Pharmacologic Action:

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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
FDA EPC N0000175553 alpha-Adrenergic Blocker
MeSH PA D018663 Adrenergic Agents
MeSH PA D058668 Adrenergic alpha-1 Receptor Antagonists
MeSH PA D000317 Adrenergic alpha-Antagonists
MeSH PA D018674 Adrenergic Antagonists
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D064804 Urological Agents
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:35674 antihypertensive agent
CHEBI has role CHEBI:37890 alpha-adrenergic antagonist

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
Benign prostatic hyperplasia indication 266569009 DOID:2883
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

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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:

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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:

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IDSource
DB00346 DRUGBANK_ID
4021396 VUID
N0000148814 NUI
C0051150 UMLSCUI
7109 IUPHAR_LIGAND_ID
D01692 KEGG_DRUG
75046A1XTN UNII
81403-68-1 SECONDARY_CAS_RN
CHEMBL709 ChEMBL_ID
N0000148814 NDFRT
N0000010340 NDFRT
005431 NDDF
17300 RXNORM
d04797 MMSL
349912006 SNOMEDCT_US
395954002 SNOMEDCT_US
4021396 VANDF
5357 INN_ID
2092 PUBCHEM_CID
CHEMBL1723 ChEMBL_ID
C047638 MESH_SUPPLEMENTAL_RECORD_UI
CHEBI:51141 CHEBI

Pharmaceutical products:

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ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
Alfuzosin Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0378-5005 TABLET, EXTENDED RELEASE 10 mg ORAL ANDA 17 sections
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 42291-110 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 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 69189-0304 TABLET 10 mg ORAL ANDA 17 sections
Alfuzosin hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 76282-302 TABLET, EXTENDED RELEASE 10 mg ORAL ANDA 16 sections