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

Stem definition	Drug id	CAS RN
	4151	160970-54-7

Description:

Molecule	Description
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

Molecule

Description

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:

Dose	Unit	Route
8	mg	O

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	32 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
t_half (Half-life)	3.60 hours	Lombardo F, Berellini G, Obach RS
CL (Clearance)	2.80 mL/min/kg	Lombardo F, Berellini G, Obach RS
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
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Bocci G, Oprea TI, Benet LZ
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
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.23 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
fu (Fraction unbound in plasma)	0.05 %	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
Jan. 29, 2010	EMA
Oct. 8, 2008	FDA	ACTAVIS LABS UT INC

FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Haematoma	52.93	45.16	14	209	34806	63453993

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	G04CA04	GENITO URINARY SYSTEM AND SEX HORMONES UROLOGICALS DRUGS USED IN BENIGN PROSTATIC HYPERTROPHY Alpha-adrenoreceptor antagonists
FDA EPC	N0000175553	alpha-Adrenergic Blocker
FDA MoA	N0000000099	Adrenergic alpha-Antagonists
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

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

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Disease	Relation	SNOMED_ID	DOID
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

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (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:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Alpha-1A adrenergic receptor	GPCR	P35348	ADA1A_HUMAN	ANTAGONIST	Ki	10.44	CHEMBL	CHEMBL
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		IC50	5.09	CHEMBL
Multidrug resistance protein 1	Transporter	P08183	MDR1_HUMAN				WOMBAT-PK
Alpha-1D adrenergic receptor	GPCR	P25100	ADA1D_HUMAN	ANTAGONIST	Ki	8.70	IUPHAR
Alpha-1B adrenergic receptor	GPCR	P35368	ADA1B_HUMAN	ANTAGONIST	Ki	7.70	IUPHAR
Alpha-1A adrenergic receptor	GPCR		ADA1A_RAT		IC50	9.10	CHEMBL

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External reference:

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ID	Source
012969	NDDF
159000	MMSL
26009	MMSL
299655	MMSL
4028100	VUID
4028100	VANDF
441605002	SNOMEDCT_US
442042006	SNOMEDCT_US
493	IUPHAR_LIGAND_ID
5312125	PUBCHEM_CID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
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
RAPAFLO	HUMAN PRESCRIPTION DRUG LABEL	1	54868-6173	CAPSULE	8 mg	ORAL	NDA	24 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

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