silodosin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
4151 160970-54-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • silodosin
  • urief
  • urorec
  • rapaflo
  • silodyx
  • silodoshin
an alpha(1a)-adrenoceptor-selective antagonist; structure given in first source
  • Molecular weight: 495.54
  • Formula: C25H32F3N3O4
  • CLOGP: 3.16
  • LIPINSKI: 0
  • HAC: 7
  • HDO: 3
  • TPSA: 97.05
  • ALOGS: -4.65
  • ROTB: 14
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
8 mg O

ADMET properties:

PropertyValueReference
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.23 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 32 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
CL (Clearance) 2.80 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.05 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 3.60 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Jan. 29, 2010 EMA
Oct. 8, 2008 FDA ACTAVIS LABS UT INC

FDA Adverse Event Reporting System (Female)

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
Haematoma 56.95 41.11 14 149 32005 56259899

FDA Adverse Event Reporting System (Male)

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
Urinary retention 95.89 14.14 89 12058 33636 31651561
Reversible airways obstruction 60.25 14.14 16 12131 343 31684854
Granulomatous rosacea 51.39 14.14 12 12135 148 31685049
Interstitial lung disease 47.86 14.14 85 12062 61318 31623879
Retrograde ejaculation 46.28 14.14 13 12134 346 31684851
Mucosal dryness 41.59 14.14 16 12131 1159 31684038
Orthostatic hypotension 40.38 14.14 48 12099 24071 31661126
Left atrial dilatation 35.39 14.14 16 12131 1739 31683458
Hyponatraemia 34.77 14.14 83 12064 73716 31611481
Haematocrit increased 34.20 14.14 16 12131 1881 31683316
Histamine level increased 33.17 14.14 7 12140 52 31685145
Acute kidney injury 32.92 14.14 201 11946 279513 31405684
Cerebral infarction 32.89 14.14 45 12102 25932 31659265
Cerebellar ischaemia 32.81 14.14 8 12139 120 31685077
Ejaculation failure 32.75 14.14 12 12135 759 31684438
Hypoparathyroidism 32.51 14.14 11 12136 550 31684647
Pemphigoid 31.91 14.14 26 12121 8245 31676952
Cerebral haematoma 31.19 14.14 20 12127 4375 31680822
Fall 30.16 14.14 146 12001 185943 31499254
Toxicity to various agents 30.16 14.14 16 12131 181471 31503726
Acute lung injury 29.46 14.14 13 12134 1334 31683863
Haemoglobin increased 26.68 14.14 16 12131 3110 31682087
Presyncope 26.58 14.14 33 12114 17295 31667902
Face oedema 24.48 14.14 25 12122 10591 31674606
Tryptase increased 24.21 14.14 7 12140 207 31684990
Tongue oedema 23.55 14.14 14 12133 2679 31682518
Loss of consciousness 23.42 14.14 74 12073 77281 31607916
Subdural haematoma 22.72 14.14 32 12115 18939 31666258
Lactic acidosis 20.84 14.14 41 12106 31896 31653301
Angle closure glaucoma 20.69 14.14 9 12138 892 31684305
Neutrophil percentage decreased 20.68 14.14 7 12140 350 31684847
Neuropathy vitamin B6 deficiency 20.60 14.14 3 12144 0 31685197
Acquired haemophilia 20.14 14.14 9 12138 952 31684245
Lymphopenia 19.94 14.14 26 12121 14303 31670894
Hypoproteinaemia 19.75 14.14 11 12136 1862 31683335
Erectile dysfunction 19.50 14.14 30 12117 19205 31665992
Atrioventricular block complete 19.44 14.14 20 12127 8545 31676652
Rash vesicular 19.18 14.14 12 12135 2515 31682682
Blood triglycerides decreased 19.11 14.14 5 12142 101 31685096
Hepatic function abnormal 19 14.14 46 12101 41176 31644021
Band neutrophil percentage increased 18.88 14.14 5 12142 106 31685091
Agranulocytosis 18.61 14.14 31 12116 21216 31663981
Eosinophil percentage increased 18.22 14.14 7 12140 505 31684692
Mucocutaneous disorder 18.21 14.14 5 12142 122 31685075
Dysuria 18.09 14.14 33 12114 24261 31660936
Bradycardia 18.02 14.14 63 12084 69264 31615933
Eosinophilia 17.84 14.14 32 12115 23221 31661976
Syncope 17.66 14.14 72 12075 85110 31600087
Haematuria 17.54 14.14 48 12099 46266 31638931
Arrhythmia 17.54 14.14 39 12108 33038 31652159
Cardiac failure 17.31 14.14 72 12075 85881 31599316
Hepatocellular injury 16.98 14.14 30 12117 21514 31663683
Cystitis interstitial 16.74 14.14 5 12142 166 31685031
Altered state of consciousness 16.19 14.14 29 12118 21022 31664175
Linear IgA disease 16.00 14.14 9 12138 1553 31683644
Multiple drug therapy 15.78 14.14 6 12141 421 31684776
Tricuspid valve disease 15.57 14.14 5 12142 212 31684985
Benign prostatic hyperplasia 15.51 14.14 22 12125 13103 31672094
Psychological trauma 15.48 14.14 5 12142 216 31684981
Decreased appetite 15.43 14.14 106 12041 153111 31532086
Acidosis 15.34 14.14 19 12128 9927 31675270
Adenocarcinoma gastric 15.26 14.14 8 12139 1200 31683997
Skin disorder 15.13 14.14 21 12126 12260 31672937
Band neutrophil count increased 14.97 14.14 5 12142 240 31684957
Syndesmophyte 14.96 14.14 4 12143 88 31685109
Platelet count decreased 14.62 14.14 82 12065 110353 31574844
Pneumonia aspiration 14.53 14.14 40 12107 38686 31646511
Dermatitis exfoliative 14.44 14.14 15 12132 6477 31678720
Wrong patient received product 14.21 14.14 10 12137 2549 31682648

FDA Adverse Event Reporting System (Geriatric)

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
Urinary retention 92.08 15.64 71 10753 52449 70865171
Acute kidney injury 70.26 15.64 194 10630 474430 70443190
Interstitial lung disease 63.43 15.64 79 10745 104606 70813014
Granulomatous rosacea 58.43 15.64 12 10812 211 70917409
Retrograde ejaculation 57.30 15.64 12 10812 233 70917387
Reversible airways obstruction 55.32 15.64 17 10807 1590 70916030
Hyponatraemia 48.11 15.64 87 10737 160000 70757620
Left atrial dilatation 42.13 15.64 16 10808 2833 70914787
Cerebral infarction 40.73 15.64 41 10783 42968 70874652
Mucosal dryness 40.25 15.64 16 10808 3200 70914420
Haematocrit increased 38.16 15.64 16 10808 3666 70913954
Orthostatic hypotension 37.83 15.64 43 10781 51700 70865920
Histamine level increased 36.65 15.64 7 10817 83 70917537
Pemphigoid 36.18 15.64 24 10800 13998 70903622
Subdural haematoma 33.53 15.64 31 10793 29267 70888353
Cerebral haematoma 33.03 15.64 18 10806 7360 70910260
Haematuria 32.28 15.64 44 10780 63529 70854091
Acute lung injury 31.79 15.64 13 10811 2796 70914824
Haemoglobin increased 31.70 15.64 16 10808 5599 70912021
Presyncope 30.62 15.64 33 10791 37405 70880215
Cardiac failure 29.90 15.64 67 10757 143474 70774146
Benign prostatic hyperplasia 29.70 15.64 19 10805 10424 70907196
Drug hypersensitivity 29.34 15.64 3 10821 262456 70655164
Bradycardia 29.20 15.64 61 10763 124554 70793066
Pain 25.83 15.64 35 10789 628781 70288839
Lactic acidosis 25.73 15.64 40 10784 64984 70852636
Decreased appetite 24.75 15.64 102 10722 304678 70612942
Anaemia 24.57 15.64 124 10700 403299 70514321
Toxicity to various agents 24.44 15.64 14 10810 382158 70535462
Haematoma 23.81 15.64 33 10791 48385 70869235
Hypoparathyroidism 23.72 15.64 8 10816 1006 70916614
Tryptase increased 23.56 15.64 7 10817 584 70917036
Face oedema 23.46 15.64 24 10800 25615 70892005
Neuropathy vitamin B6 deficiency 23.36 15.64 3 10821 0 70917620
Erectile dysfunction 23.02 15.64 18 10806 13544 70904076
Fall 22.63 15.64 130 10694 443966 70473654
Acquired haemophilia 22.41 15.64 9 10815 1848 70915772
Mucocutaneous disorder 22.34 15.64 5 10819 134 70917486
Agranulocytosis 22.15 15.64 29 10795 40269 70877351
Eosinophilia 22.14 15.64 29 10795 40290 70877330
Neutrophil percentage decreased 21.83 15.64 7 10817 752 70916868
Hepatic function abnormal 21.74 15.64 38 10786 67958 70849662
Platelet count decreased 21.59 15.64 68 10756 178154 70739466
Cerebellar ischaemia 21.57 15.64 5 10819 157 70917463
Arrhythmia 21.46 15.64 34 10790 56109 70861511
Atrioventricular block complete 21.25 15.64 18 10806 15145 70902475
Hepatocellular injury 20.57 15.64 30 10794 46061 70871559
Lymphopenia 20.44 15.64 23 10801 27336 70890284
Alopecia 20.39 15.64 3 10821 198487 70719133
Blood triglycerides decreased 20.17 15.64 5 10819 210 70917410
Pneumonia aspiration 20.16 15.64 35 10789 62254 70855366
Prostate cancer 19.62 15.64 24 10800 31139 70886481
Hypoproteinaemia 19.50 15.64 10 10814 3616 70914004
Tongue oedema 19.33 15.64 12 10812 6247 70911373
Angle closure glaucoma 18.92 15.64 9 10815 2770 70914850
Rash vesicular 18.64 15.64 11 10813 5229 70912391
Linear IgA disease 18.49 15.64 9 10815 2915 70914705
Acidosis 18.38 15.64 18 10806 18245 70899375
Hyperkalaemia 18.13 15.64 46 10778 106545 70811075
Joint swelling 18.09 15.64 8 10816 253203 70664417
Rhabdomyolysis 18.06 15.64 43 10781 95717 70821903
Thrombocytopenia 17.83 15.64 78 10746 239032 70678588
Altered state of consciousness 17.79 15.64 26 10798 39996 70877624
Eosinophil percentage increased 17.40 15.64 7 10817 1443 70916177
Neutrophil count decreased 17.38 15.64 39 10785 83517 70834103
Tricuspid valve disease 17.07 15.64 5 10819 397 70917223
Band neutrophil percentage increased 16.91 15.64 5 10819 410 70917210
Arthralgia 16.89 15.64 32 10792 503358 70414262
Hypokalaemia 16.75 15.64 51 10773 131137 70786483
Hypovolaemia 16.54 15.64 16 10808 15977 70901643
Adenocarcinoma gastric 16.19 15.64 7 10817 1729 70915891
Urethral stenosis 16.03 15.64 6 10818 1021 70916599
Pneumonia bacterial 16.00 15.64 16 10808 16625 70900995
Atrial fibrillation 15.98 15.64 63 10761 184285 70733335
Dermatitis exfoliative 15.77 15.64 13 10811 10538 70907082

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC G04CA04 GENITO URINARY SYSTEM AND SEX HORMONES
UROLOGICALS
DRUGS USED IN BENIGN PROSTATIC HYPERTROPHY
Alpha-adrenoreceptor antagonists
FDA MoA N0000000099 Adrenergic alpha-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

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Benign prostatic hyperplasia indication 266569009
Orthostatic hypotension contraindication 28651003
Acute nephropathy contraindication 58574008
Hepatic failure contraindication 59927004
Kidney disease contraindication 90708001 DOID:557
Cataract surgery contraindication 110473004
Intraoperative floppy iris syndrome contraindication 418801006




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 13.41 acidic
pKa2 7.96 Basic
pKa3 4.09 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-1A adrenergic receptor GPCR ANTAGONIST Ki 10.44 CHEMBL CHEMBL
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 5.09 CHEMBL
Multidrug resistance protein 1 Transporter WOMBAT-PK
Alpha-1D adrenergic receptor GPCR ANTAGONIST Ki 8.70 IUPHAR
Alpha-1B adrenergic receptor GPCR ANTAGONIST Ki 7.70 IUPHAR
Alpha-1A adrenergic receptor GPCR IC50 9.10 CHEMBL

External reference:

IDSource
4028100 VUID
N0000177928 NUI
D01965 KEGG_DRUG
4028100 VANDF
C1870115 UMLSCUI
CHEBI:135929 CHEBI
CHEMBL24778 ChEMBL_ID
DB06207 DRUGBANK_ID
C095285 MESH_SUPPLEMENTAL_RECORD_UI
493 IUPHAR_LIGAND_ID
8043 INN_ID
CUZ39LUY82 UNII
5312125 PUBCHEM_CID
720825 RXNORM
159000 MMSL
26009 MMSL
299655 MMSL
d07354 MMSL
012969 NDDF
441605002 SNOMEDCT_US
442042006 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
RAPAFLO HUMAN PRESCRIPTION DRUG LABEL 1 0023-6142 CAPSULE 8 mg ORAL NDA 26 sections
RAPAFLO HUMAN PRESCRIPTION DRUG LABEL 1 0023-6147 CAPSULE 4 mg ORAL NDA 26 sections
Silodosin HUMAN PRESCRIPTION DRUG LABEL 1 0781-2623 CAPSULE, GELATIN COATED 4 mg ORAL ANDA 26 sections
Silodosin HUMAN PRESCRIPTION DRUG LABEL 1 0781-2623 CAPSULE, GELATIN COATED 4 mg ORAL ANDA 26 sections
Silodosin HUMAN PRESCRIPTION DRUG LABEL 1 0781-2624 CAPSULE, GELATIN COATED 8 mg ORAL ANDA 26 sections
Silodosin HUMAN PRESCRIPTION DRUG LABEL 1 0781-2624 CAPSULE, GELATIN COATED 8 mg ORAL ANDA 26 sections
Silodosin Human Prescription Drug Label 1 27241-144 CAPSULE 4 mg ORAL ANDA 25 sections
Silodosin Human Prescription Drug Label 1 27241-145 CAPSULE 8 mg ORAL ANDA 25 sections
Silodosin Human Prescription Drug Label 1 31722-635 CAPSULE 4 mg ORAL ANDA 28 sections
Silodosin Human Prescription Drug Label 1 31722-636 CAPSULE 8 mg ORAL ANDA 28 sections
Silodosin Human Prescription Drug Label 1 33342-384 CAPSULE 4 mg ORAL ANDA 26 sections
Silodosin Human Prescription Drug Label 1 33342-384 CAPSULE 4 mg ORAL ANDA 26 sections
Silodosin Human Prescription Drug Label 1 33342-385 CAPSULE 8 mg ORAL ANDA 26 sections
Silodosin Human Prescription Drug Label 1 33342-385 CAPSULE 8 mg ORAL ANDA 26 sections
Silodosin HUMAN PRESCRIPTION DRUG LABEL 1 42291-777 CAPSULE 4 mg ORAL ANDA 25 sections
Silodosin HUMAN PRESCRIPTION DRUG LABEL 1 42291-778 CAPSULE 8 mg ORAL ANDA 25 sections
Silodosin Human Prescription Drug Label 1 46708-405 CAPSULE 4 mg ORAL ANDA 25 sections
Silodosin Human Prescription Drug Label 1 46708-406 CAPSULE 8 mg ORAL ANDA 25 sections
RAPAFLO HUMAN PRESCRIPTION DRUG LABEL 1 54868-6173 CAPSULE 8 mg ORAL NDA 24 sections
SILODOSIN Human Prescription Drug Label 1 59651-095 CAPSULE 4 mg ORAL ANDA 26 sections
SILODOSIN Human Prescription Drug Label 1 59651-096 CAPSULE 8 mg ORAL ANDA 26 sections
Silodosin HUMAN PRESCRIPTION DRUG LABEL 1 60219-1420 CAPSULE 8 mg ORAL ANDA 25 sections
Silodosin HUMAN PRESCRIPTION DRUG LABEL 1 60219-1421 CAPSULE 4 mg ORAL ANDA 25 sections
Silodosin Human Prescription Drug Label 1 62332-405 CAPSULE 4 mg ORAL ANDA 26 sections
Silodosin Human Prescription Drug Label 1 62332-406 CAPSULE 8 mg ORAL ANDA 26 sections
Silodosin HUMAN PRESCRIPTION DRUG LABEL 1 68180-740 CAPSULE 4 mg ORAL ANDA 24 sections
Silodosin HUMAN PRESCRIPTION DRUG LABEL 1 68180-741 CAPSULE 8 mg ORAL ANDA 24 sections
Silodosin HUMAN PRESCRIPTION DRUG LABEL 1 69238-1420 CAPSULE 8 mg ORAL ANDA 25 sections
Silodosin HUMAN PRESCRIPTION DRUG LABEL 1 69238-1421 CAPSULE 4 mg ORAL ANDA 25 sections
SILODOSIN Human Prescription Drug Label 1 69539-052 CAPSULE 4 mg ORAL ANDA 26 sections