silodosin 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: 2.97
  • 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 ┬ÁM/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 50.05 44.55 8 15 5113 2352949

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
Granulomatous rosacea 96.30 36.63 11 466 3 1746301
Loss of consciousness 73.59 36.63 27 450 14848 1731456
Hyponatraemia 58.33 36.63 20 457 8980 1737324
Orthostatic hypotension 58.29 36.63 16 461 3415 1742889
Fall 54.72 36.63 26 451 27188 1719116
Histamine level increased 47.03 36.63 6 471 13 1746291
Syncope 46.04 36.63 19 458 14150 1732154
Rash vesicular 45.40 36.63 9 468 459 1745845
Eosinophilia 44.29 36.63 13 464 3514 1742790
Dizziness 40.60 36.63 23 454 34338 1711966
Tryptase increased 39.29 36.63 6 471 63 1746241

Pharmacologic Action:

SourceCodeDescription
ATC G04CA04 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
MeSH PA D064804 Urological Agents

Drug Use (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

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
Alpha-1D adrenergic receptor GPCR ANTAGONIST Ki 8.70 IUPHAR
Alpha-1B adrenergic receptor GPCR ANTAGONIST Ki 7.70 IUPHAR
Multidrug resistance protein 1 Transporter WOMBAT-PK

External reference:

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

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
RAPAFLO HUMAN PRESCRIPTION DRUG LABEL 1 0023-6142 CAPSULE 8 mg ORAL NDA 16 sections
RAPAFLO HUMAN PRESCRIPTION DRUG LABEL 1 0023-6147 CAPSULE 4 mg ORAL NDA 16 sections
Silodosin HUMAN PRESCRIPTION DRUG LABEL 1 0781-2623 CAPSULE, GELATIN COATED 4 mg ORAL ANDA 16 sections
Silodosin HUMAN PRESCRIPTION DRUG LABEL 1 0781-2624 CAPSULE, GELATIN COATED 8 mg ORAL ANDA 16 sections
Silodosin HUMAN PRESCRIPTION DRUG LABEL 1 27241-144 CAPSULE 4 mg ORAL ANDA 16 sections
Silodosin HUMAN PRESCRIPTION DRUG LABEL 1 27241-145 CAPSULE 8 mg ORAL ANDA 16 sections
Silodosin HUMAN PRESCRIPTION DRUG LABEL 1 31722-635 CAPSULE 4 mg ORAL ANDA 16 sections
Silodosin HUMAN PRESCRIPTION DRUG LABEL 1 31722-636 CAPSULE 8 mg ORAL ANDA 16 sections
Silodosin HUMAN PRESCRIPTION DRUG LABEL 1 33342-384 CAPSULE 4 mg ORAL ANDA 17 sections
Silodosin HUMAN PRESCRIPTION DRUG LABEL 1 33342-385 CAPSULE 8 mg ORAL ANDA 17 sections
Silodosin HUMAN PRESCRIPTION DRUG LABEL 1 46708-405 CAPSULE 4 mg ORAL ANDA 17 sections
Silodosin HUMAN PRESCRIPTION DRUG LABEL 1 46708-406 CAPSULE 8 mg ORAL ANDA 17 sections
RAPAFLO HUMAN PRESCRIPTION DRUG LABEL 1 52544-151 CAPSULE 4 mg ORAL NDA 16 sections
RAPAFLO HUMAN PRESCRIPTION DRUG LABEL 1 52544-152 CAPSULE 8 mg ORAL NDA 16 sections
RAPAFLO HUMAN PRESCRIPTION DRUG LABEL 1 54868-6173 CAPSULE 8 mg ORAL NDA 16 sections
SILODOSIN HUMAN PRESCRIPTION DRUG LABEL 1 59651-095 CAPSULE 4 mg ORAL ANDA 17 sections
SILODOSIN HUMAN PRESCRIPTION DRUG LABEL 1 59651-096 CAPSULE 8 mg ORAL ANDA 17 sections
Silodosin HUMAN PRESCRIPTION DRUG LABEL 1 62332-405 CAPSULE 4 mg ORAL ANDA 17 sections
Silodosin HUMAN PRESCRIPTION DRUG LABEL 1 62332-406 CAPSULE 8 mg ORAL ANDA 17 sections
Silodosin HUMAN PRESCRIPTION DRUG LABEL 1 68180-740 CAPSULE 4 mg ORAL ANDA 16 sections
Silodosin HUMAN PRESCRIPTION DRUG LABEL 1 68180-741 CAPSULE 8 mg ORAL ANDA 16 sections
Silodosin HUMAN PRESCRIPTION DRUG LABEL 1 69238-1420 CAPSULE 8 mg ORAL ANDA 16 sections
Silodosin HUMAN PRESCRIPTION DRUG LABEL 1 69238-1421 CAPSULE 4 mg ORAL ANDA 16 sections
SILODOSIN HUMAN PRESCRIPTION DRUG LABEL 1 69539-052 CAPSULE 4 mg ORAL ANDA 16 sections
SILODOSIN HUMAN PRESCRIPTION DRUG LABEL 1 69539-053 CAPSULE 8 mg ORAL ANDA 16 sections
SILODOSIN HUMAN PRESCRIPTION DRUG LABEL 1 72205-009 CAPSULE 4 mg ORAL ANDA 16 sections
SILODOSIN HUMAN PRESCRIPTION DRUG LABEL 1 72205-010 CAPSULE 8 mg ORAL ANDA 16 sections