doxazosin indications/contra

Stem definitionDrug idCAS RN
antihypertensive substances, prazosin derivatives 954 74191-85-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • doxazosin
  • doxazosin mesylate
  • doxazosine
  • doxazosin mesilate
A prazosin-related compound that is a selective alpha-1-adrenergic blocker.
  • Molecular weight: 451.48
  • Formula: C23H25N5O5
  • CLOGP: 3.53
  • LIPINSKI: 0
  • HAC: 10
  • HDO: 1
  • TPSA: 112.27
  • ALOGS: -2.76
  • ROTB: 4

Drug dosage:

DoseUnitRoute
4 mg O

Approvals:

DateAgencyCompanyOrphan
Nov. 2, 1990 FDA PFIZER

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 841.74 33.48 263 1705 49251 3334640
Syncope 477.06 33.48 147 1821 25486 3358405
Orthostatic hypotension 413.77 33.48 94 1874 4942 3378949
Acute kidney injury 277.05 33.48 117 1851 49566 3334325
Drug interaction 266.79 33.48 112 1856 46700 3337191
Bradycardia 236.15 33.48 78 1890 16591 3367300
Dizziness 234.60 33.48 119 1849 76393 3307498
Loss of consciousness 206.81 33.48 81 1887 28066 3355825
Overdose 192.05 33.48 81 1887 33897 3349994
Fall 178.25 33.48 91 1877 58792 3325099
Urinary incontinence 143.36 33.48 42 1926 5970 3377921
Presyncope 140.08 33.48 40 1928 5191 3378700
Dyspnoea 138.22 33.48 94 1874 102840 3281051
Hypertensive crisis 130.66 33.48 34 1934 3113 3380778
Completed suicide 129.73 33.48 60 1908 31054 3352837
Floppy iris syndrome 117.31 33.48 19 1949 150 3383741
Toxicity to various agents 117.26 33.48 64 1904 46990 3336901
Circulatory collapse 112.90 33.48 35 1933 6014 3377877
Blood lactic acid increased 109.72 33.48 25 1943 1308 3382583
Hypertension 106.08 33.48 56 1912 38410 3345481
Asthenia 104.92 33.48 67 1901 65598 3318293
Pulmonary oedema 104.07 33.48 39 1929 11872 3372019
Cardiomegaly 102.01 33.48 30 1938 4308 3379583
Renal failure 99.51 33.48 51 1917 32889 3351002
Drug hypersensitivity 95.67 33.48 51 1917 35629 3348262
Joint swelling 93.81 33.48 40 1928 17017 3366874
Blood pressure inadequately controlled 92.36 33.48 22 1946 1398 3382493
Nocturia 89.29 33.48 22 1946 1612 3382279
Drug ineffective 88.91 33.48 76 1892 116014 3267877
Hyperkalaemia 87.91 33.48 34 1934 11260 3372631

Pharmacologic Action:

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SourceCodeDescription
ATC C02CA04 CARDIOVASCULAR SYSTEM
ANTIHYPERTENSIVES
ANTIADRENERGIC AGENTS, PERIPHERALLY ACTING
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 D000959 Antihypertensive Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D018377 Neurotransmitter Agents
CHEBI has role CHEBI:35674 antihypertensive agent
CHEBI has role CHEBI:37890 alpha-adrenergic antagonist
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:35620 vasodilator agent
CHEBI has role CHEBI:59844 antihyperplasia drug

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
Hypertensive disorder indication 38341003 DOID:10763
Benign prostatic hyperplasia indication 266569009 DOID:2883
Priapism contraindication 6273006 DOID:9286
Stenosis of intestine contraindication 23065003
Orthostatic hypotension contraindication 28651003
Low blood pressure contraindication 45007003
Hepatic failure contraindication 59927004
Chronic idiopathic constipation contraindication 82934008
Cataract surgery contraindication 110473004
Disease of liver contraindication 235856003 DOID:409
Pyloric obstruction contraindication 244815007 DOID:3122
Syncope contraindication 271594007
Intraoperative floppy iris syndrome contraindication 418801006

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation levelDissociation constantType (acidic/basic)
pKa1 7.22 Basic
pKa2 0.72 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 8.85 WOMBAT-PK CHEMBL
Alpha-1A adrenergic receptor GPCR ANTAGONIST Ki 8.80 WOMBAT-PK CHEMBL
Alpha-1B adrenergic receptor GPCR ANTAGONIST Ki 9.10 WOMBAT-PK CHEMBL
5-hydroxytryptamine receptor 2B GPCR Ki 6.63 DRUG MATRIX
5-hydroxytryptamine receptor 2C GPCR Ki 6.55 DRUG MATRIX
Sodium-dependent dopamine transporter Transporter Ki 6.83 DRUG MATRIX
Interstitial collagenase Enzyme IC50 5.24 DRUG MATRIX
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 6.23 WOMBAT-PK
Multidrug resistance protein 1 Transporter Ki 5 WOMBAT-PK
Alpha-2A adrenergic receptor GPCR Ki 6.14 CHEMBL
Alpha-2C adrenergic receptor GPCR Ki 6.55 CHEMBL
Beta-2 adrenergic receptor GPCR Ki 5.72 DRUG MATRIX
Sodium-dependent serotonin transporter Transporter Ki 5.85 DRUG MATRIX
5-hydroxytryptamine receptor 4 GPCR Ki 6.90 DRUG MATRIX
Alpha-1B adrenergic receptor GPCR Ki 9.38 DRUG MATRIX
Alpha-1A adrenergic receptor GPCR IC50 8.81 CHEMBL

External reference:

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IDSource
4019735 VUID
N0000147827 NUI
C0114873 UMLSCUI
7170 IUPHAR_LIGAND_ID
D00608 KEGG_DRUG
DB00590 DRUGBANK_ID
CHEMBL707 ChEMBL_ID
4019735 VANDF
N0000147827 NDFRT
N0000007318 NDFRT
004493 NDDF
49276 RXNORM
108556006 SNOMEDCT_US
372508002 SNOMEDCT_US
d00726 MMSL
86P6PQK0MU UNII
77883-43-3 SECONDARY_CAS_RN
3157 PUBCHEM_CID
CHEMBL1200561 ChEMBL_ID
5143 INN_ID
D017292 MESH_DESCRIPTOR_UI
CHEBI:4708 CHEBI

Pharmaceutical products:

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ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
Cardura HUMAN PRESCRIPTION DRUG LABEL 1 0049-2710 TABLET, MULTILAYER, EXTENDED RELEASE 4 mg ORAL NDA 19 sections
Cardura HUMAN PRESCRIPTION DRUG LABEL 1 0049-2720 TABLET, MULTILAYER, EXTENDED RELEASE 8 mg ORAL NDA 19 sections
Cardura HUMAN PRESCRIPTION DRUG LABEL 1 0049-2750 TABLET 1 mg ORAL NDA 18 sections
Cardura HUMAN PRESCRIPTION DRUG LABEL 1 0049-2760 TABLET 2 mg ORAL NDA 18 sections
Cardura HUMAN PRESCRIPTION DRUG LABEL 1 0049-2770 TABLET 4 mg ORAL NDA 18 sections
Cardura HUMAN PRESCRIPTION DRUG LABEL 1 0049-2780 TABLET 8 mg ORAL NDA 18 sections
Doxazosin HUMAN PRESCRIPTION DRUG LABEL 1 0093-2067 TABLET 8 mg ORAL ANDA 17 sections
Doxazosin HUMAN PRESCRIPTION DRUG LABEL 1 0093-2068 TABLET 4 mg ORAL ANDA 17 sections
Doxazosin HUMAN PRESCRIPTION DRUG LABEL 1 0093-2069 TABLET 2 mg ORAL ANDA 17 sections
Doxazosin HUMAN PRESCRIPTION DRUG LABEL 1 0093-2070 TABLET 1 mg ORAL ANDA 17 sections
Doxazosin HUMAN PRESCRIPTION DRUG LABEL 1 0378-4021 TABLET 1 mg ORAL ANDA 17 sections
Doxazosin HUMAN PRESCRIPTION DRUG LABEL 1 0378-4022 TABLET 2 mg ORAL ANDA 17 sections
Doxazosin HUMAN PRESCRIPTION DRUG LABEL 1 0378-4024 TABLET 4 mg ORAL ANDA 17 sections
Doxazosin HUMAN PRESCRIPTION DRUG LABEL 1 0378-4028 TABLET 8 mg ORAL ANDA 17 sections
Doxazosin HUMAN PRESCRIPTION DRUG LABEL 1 0615-5536 TABLET 1 mg ORAL ANDA 13 sections
Doxazosin HUMAN PRESCRIPTION DRUG LABEL 1 0615-5537 TABLET 8 mg ORAL ANDA 13 sections
Doxazosin HUMAN PRESCRIPTION DRUG LABEL 1 0615-6570 TABLET 2 mg ORAL ANDA 13 sections
Doxazosin HUMAN PRESCRIPTION DRUG LABEL 1 0615-6571 TABLET 4 mg ORAL ANDA 13 sections
Doxazosin HUMAN PRESCRIPTION DRUG LABEL 1 0904-5522 TABLET 1 mg ORAL ANDA 17 sections
Doxazosin HUMAN PRESCRIPTION DRUG LABEL 1 0904-5523 TABLET 2 mg ORAL ANDA 17 sections
Doxazosin HUMAN PRESCRIPTION DRUG LABEL 1 0904-5524 TABLET 4 mg ORAL ANDA 17 sections
Doxazosin HUMAN PRESCRIPTION DRUG LABEL 1 0904-5525 TABLET 8 mg ORAL ANDA 17 sections
Doxazosin Mesylate HUMAN PRESCRIPTION DRUG LABEL 1 0904-6140 TABLET 1 mg ORAL ANDA 13 sections
Doxazosin Mesylate HUMAN PRESCRIPTION DRUG LABEL 1 0904-6141 TABLET 2 mg ORAL ANDA 13 sections
Doxazosin Mesylate HUMAN PRESCRIPTION DRUG LABEL 1 0904-6142 TABLET 4 mg ORAL ANDA 13 sections
Doxazosin Mesylate HUMAN PRESCRIPTION DRUG LABEL 1 0904-6143 TABLET 8 mg ORAL ANDA 13 sections
Doxazosin Mesylate HUMAN PRESCRIPTION DRUG LABEL 1 10544-292 TABLET 4 mg ORAL ANDA 12 sections
Doxazosin Mesylate HUMAN PRESCRIPTION DRUG LABEL 1 10544-629 TABLET 1 mg ORAL ANDA 12 sections
Doxazosin HUMAN PRESCRIPTION DRUG LABEL 1 16590-274 TABLET 4 mg ORAL ANDA 12 sections
Doxazosin HUMAN PRESCRIPTION DRUG LABEL 1 16729-211 TABLET 1 mg ORAL ANDA 17 sections