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
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Bocci G, Oprea TI, Benet LZ
CL (Clearance) 2.38 mL/min/kg Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K
Vd (Volume of distribution) 0.71 L/kg Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K

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 52.93 45.16 14 209 34806 63453993

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 95.52 14.76 91 13057 36197 34907586
Reversible airways obstruction 83.46 14.76 22 13126 467 34943316
Interstitial lung disease 52.93 14.76 91 13057 65191 34878592
Granulomatous rosacea 51.91 14.76 12 13136 144 34943639
Orthostatic hypotension 44.87 14.76 52 13096 25867 34917916
Retrograde ejaculation 44.11 14.76 13 13135 420 34943363
Mucosal dryness 39.94 14.76 16 13132 1315 34942468
Cerebral infarction 39.25 14.76 50 13098 27405 34916378
Ejaculation failure 36.12 14.76 13 13135 796 34942987
Left atrial dilatation 33.71 14.76 16 13132 1980 34941803
Toxicity to various agents 33.18 14.76 17 13131 200345 34743438
Histamine level increased 33.07 14.76 7 13141 54 34943729
Haematocrit increased 32.84 14.76 16 13132 2097 34941686
Cerebellar ischaemia 32.65 14.76 8 13140 125 34943658
Acute kidney injury 32.05 14.76 210 12938 304778 34639005
Hypoparathyroidism 31.89 14.76 11 13137 594 34943189
Pemphigoid 31.27 14.76 26 13122 8640 34935143
Hyponatraemia 30.67 14.76 84 13064 82607 34861176
Cerebral haematoma 30.63 14.76 20 13128 4595 34939188
Face oedema 28.61 14.76 28 13120 11488 34932295
Fall 28.58 14.76 151 12997 202734 34741049
Acute lung injury 28.27 14.76 13 13135 1497 34942286
Presyncope 26.12 14.76 34 13114 19025 34924758
Haemoglobin increased 25.68 14.76 16 13132 3393 34940390
Linear IgA disease 24.34 14.76 12 13136 1614 34942169
Tryptase increased 23.64 14.76 7 13141 230 34943553
Loss of consciousness 23.10 14.76 76 13072 82591 34861192
Tongue oedema 22.40 14.76 14 13134 2983 34940800
Haematuria 21.77 14.76 54 13094 50012 34893771
Subdural haematoma 21.37 14.76 32 13116 20389 34923394
Hypoproteinaemia 20.90 14.76 12 13136 2192 34941591
Neuropathy vitamin B6 deficiency 20.66 14.76 3 13145 0 34943783
Lymphopenia 20.63 14.76 28 13120 16307 34927476
Neutrophil percentage decreased 20.55 14.76 7 13141 364 34943419
Hepatic function abnormal 20.51 14.76 49 13099 44314 34899469
Angle closure glaucoma 20.33 14.76 9 13139 948 34942835
Acquired haemophilia 19.87 14.76 9 13139 1001 34942782
Erectile dysfunction 19.71 14.76 31 13117 20606 34923177
Band neutrophil percentage increased 18.97 14.76 5 13143 106 34943677
Lactic acidosis 18.96 14.76 41 13107 34731 34909052
Blood triglycerides decreased 18.88 14.76 5 13143 108 34943675
Syncope 18.71 14.76 76 13072 91375 34852408
Atrioventricular block complete 18.35 14.76 20 13128 9299 34934484
Rash vesicular 18.35 14.76 12 13136 2765 34941018
Bradycardia 18.15 14.76 66 13082 75352 34868431
Arrhythmia 18.14 14.76 41 13107 35767 34908016
Mucocutaneous disorder 18.11 14.76 5 13143 127 34943656
Pneumonia aspiration 18.01 14.76 45 13103 41858 34901925
Eosinophil percentage increased 17.79 14.76 7 13141 549 34943234
Altered state of consciousness 17.34 14.76 31 13117 22862 34920921
Cardiac failure 17.24 14.76 74 13074 91174 34852609
Hepatocellular injury 16.73 14.76 30 13118 22181 34921602
Cystitis interstitial 16.72 14.76 5 13143 170 34943613
Agranulocytosis 16.46 14.76 31 13117 23790 34919993
Decreased appetite 16.45 14.76 113 13035 166279 34777504
Platelet count decreased 16.06 14.76 88 13060 119629 34824154
Anaemia 15.69 14.76 145 13003 233190 34710593
Tricuspid valve disease 15.66 14.76 5 13143 212 34943571
Eosinophilia 15.55 14.76 32 13116 26190 34917593
Multiple drug therapy 15.44 14.76 6 13142 455 34943328
Psychological trauma 15.42 14.76 5 13143 223 34943560
Prostatic specific antigen increased 15.35 14.76 23 13125 14657 34929126
Skin disorder 15.28 14.76 22 13126 13533 34930250
Adenocarcinoma gastric 15.25 14.76 8 13140 1225 34942558
Dysuria 14.78 14.76 32 13116 27120 34916663

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 93.95 14.67 73 11659 56557 79676099
Reversible airways obstruction 75.66 14.67 23 11709 2153 79730503
Acute kidney injury 72.44 14.67 203 11529 519201 79213455
Interstitial lung disease 69.13 14.67 84 11648 112516 79620140
Granulomatous rosacea 59.25 14.67 12 11720 204 79732452
Retrograde ejaculation 54.73 14.67 12 11720 303 79732353
Cerebral infarction 49.27 14.67 46 11686 45630 79687026
Hyponatraemia 45.07 14.67 88 11644 177760 79554896
Orthostatic hypotension 43.03 14.67 47 11685 56117 79676539
Left atrial dilatation 41.13 14.67 16 11716 3137 79729519
Mucosal dryness 39.25 14.67 16 11716 3543 79729113
Haematuria 38.45 14.67 49 11683 68787 79663869
Haematocrit increased 37.31 14.67 16 11716 4018 79728638
Histamine level increased 35.90 14.67 7 11725 97 79732559
Pemphigoid 35.05 14.67 24 11708 15291 79717365
Subdural haematoma 32.64 14.67 31 11701 31403 79701253
Cerebral haematoma 32.41 14.67 18 11714 7924 79724732
Acute lung injury 31.01 14.67 13 11719 3087 79729569
Haemoglobin increased 30.92 14.67 16 11716 6116 79726540
Presyncope 30.82 14.67 34 11698 41020 79691636
Pain 30.78 14.67 35 11697 703767 79028889
Drug hypersensitivity 30.46 14.67 4 11728 298912 79433744
Prostatic specific antigen increased 30.43 14.67 19 11713 10367 79722289
Cardiac failure 30.34 14.67 69 11663 154773 79577883
Bradycardia 29.49 14.67 63 11669 135494 79597162
Anaemia 29.11 14.67 136 11596 444879 79287777
Psychological trauma 28.99 14.67 10 11722 1396 79731260
Face oedema 27.80 14.67 27 11705 28109 79704547
Toxicity to various agents 27.28 14.67 14 11718 421526 79311130
Pneumonia aspiration 25.94 14.67 40 11692 66927 79665729
Decreased appetite 25.65 14.67 109 11623 342309 79390347
Platelet count decreased 24.98 14.67 74 11658 194590 79538066
Lactic acidosis 24.46 14.67 40 11692 70319 79662337
Linear IgA disease 24.37 14.67 11 11721 3121 79729535
Haematoma 24.30 14.67 34 11698 52161 79680495
Prostate cancer 24.02 14.67 27 11705 33241 79699415
Alopecia 23.79 14.67 3 11729 231352 79501304
Neuropathy vitamin B6 deficiency 23.47 14.67 3 11729 0 79732656
Hypoparathyroidism 23.38 14.67 8 11724 1090 79731566
Hepatic function abnormal 23.33 14.67 40 11692 73067 79659589
Tryptase increased 23.12 14.67 7 11725 646 79732010
Acquired haemophilia 22.48 14.67 9 11723 1902 79730754
Hyperkalaemia 22.42 14.67 51 11681 114347 79618309
Lymphopenia 22.41 14.67 25 11707 30532 79702124
Erectile dysfunction 22.36 14.67 18 11714 14646 79718010
Fall 22.26 14.67 135 11597 487494 79245162
Mucocutaneous disorder 22.14 14.67 5 11727 145 79732511
Agranulocytosis 21.96 14.67 30 11702 45000 79687656
Hypoproteinaemia 21.68 14.67 11 11721 4035 79728621
Arrhythmia 21.52 14.67 35 11697 61237 79671419
Benign prostatic hyperplasia 21.51 14.67 16 11716 11596 79721060
Neutrophil percentage decreased 21.31 14.67 7 11725 842 79731814
Joint swelling 21.16 14.67 8 11724 288638 79444018
Rheumatoid arthritis 20.73 14.67 3 11729 208467 79524189
Hepatocellular injury 20.68 14.67 30 11702 47563 79685093
Atrioventricular block complete 20.40 14.67 18 11714 16592 79716064
Eosinophilia 20.31 14.67 29 11703 45316 79687340
Rhabdomyolysis 20.23 14.67 46 11686 103085 79629571
Blood triglycerides decreased 19.99 14.67 5 11727 226 79732430
Cerebellar ischaemia 19.84 14.67 5 11727 233 79732423
Drug ineffective 19.77 14.67 87 11645 1080826 78651830
Neutrophil count decreased 19.66 14.67 43 11689 93916 79638740
Altered state of consciousness 19.59 14.67 28 11704 43794 79688862
Sinusitis 19.01 14.67 3 11729 195498 79537158
Thrombocytopenia 18.74 14.67 83 11649 265176 79467480
Hypokalaemia 18.70 14.67 55 11677 143985 79588671
Angle closure glaucoma 18.65 14.67 9 11723 2967 79729689
Tongue oedema 18.32 14.67 12 11720 7105 79725551
Atrial fibrillation 18.02 14.67 67 11665 197819 79534837
Acidosis 17.73 14.67 18 11714 19744 79712912
Rash vesicular 17.73 14.67 11 11721 5934 79726722
Arthralgia 17.67 14.67 36 11696 571767 79160889
Hypovolaemia 17.52 14.67 17 11715 17674 79714982
Syncope 17.39 14.67 62 11670 179387 79553269
Eosinophil percentage increased 17.34 14.67 7 11725 1511 79731145
Band neutrophil percentage increased 16.93 14.67 5 11727 424 79732232
Tricuspid valve disease 16.89 14.67 5 11727 427 79732229
Impaired quality of life 16.50 14.67 15 11717 14371 79718285
Adenocarcinoma gastric 16.34 14.67 7 11725 1754 79730902
Pneumonia bacterial 16.25 14.67 17 11715 19314 79713342
Peripheral swelling 15.93 14.67 10 11722 269607 79463049
Dermatitis exfoliative 15.89 14.67 13 11719 10816 79721840
Bladder tamponade 15.34 14.67 5 11727 587 79732069
Prostatic pain 15.23 14.67 3 11729 44 79732612
Wrong patient received product 14.94 14.67 9 11723 4609 79728047
Squamous cell carcinoma of skin 14.87 14.67 14 11718 14019 79718637
Parapsoriasis 14.79 14.67 4 11728 246 79732410

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 46708-405 CAPSULE 4 mg ORAL ANDA 25 sections
Silodosin Human Prescription Drug Label 1 46708-406 CAPSULE 8 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