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

Stem definition	Drug id	CAS RN
antihypertensive substances, prazosin derivatives	2562	106133-20-4

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: tamsulosin tamsulosin hydrochloride tamsulosin HCl LY-253352	A sulfonamide derivative and adrenergic alpha-1 receptor antagonist that is used to relieve symptoms of urinary obstruction caused by BENIGN PROSTATIC HYPERPLASIA. Molecular weight: 408.51 Formula: C20H28N2O5S CLOGP: 2.17 LIPINSKI: 0 HAC: 7 HDO: 2 TPSA: 99.88 ALOGS: -4.79 ROTB: 11 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

tamsulosin
tamsulosin hydrochloride
tamsulosin HCl
LY-253352

A sulfonamide derivative and adrenergic alpha-1 receptor antagonist that is used to relieve symptoms of urinary obstruction caused by BENIGN PROSTATIC HYPERPLASIA.

Molecular weight: 408.51
Formula: C20H28N2O5S
CLOGP: 2.17
LIPINSKI: 0
HAC: 7
HDO: 2
TPSA: 99.88
ALOGS: -4.79
ROTB: 11

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
0.40	mg	O

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	99 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
EoM (Fraction excreted unchanged in urine)	8.70 %	Benet LZ, Broccatelli F, Oprea TI
t_half (Half-life)	6.80 hours	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
CL (Clearance)	0.62 mL/min/kg	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	0.21 L/kg	Lombardo F, Berellini G, Obach RS
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.03 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
fu (Fraction unbound in plasma)	0.01 %	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
April 15, 1997	FDA	BOEHRINGER INGELHEIM

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
Nephrolithiasis	187.74	14.56	101	9254	41883	63437784
Urinary tract infection	93.09	14.56	151	9204	264533	63215134
Multiple sclerosis relapse	72.86	14.56	59	9296	48419	63431248
Urinary retention	58.94	14.56	43	9312	30258	63449409
Residual urine volume increased	40.09	14.56	7	9348	50	63479617
Renal colic	36.31	14.56	12	9343	1469	63478198
Ligament pain	36.14	14.56	8	9347	211	63479456
Multiple sclerosis	35.20	14.56	29	9326	24343	63455324
Drug ineffective	33.33	14.56	65	9290	1044700	62434967
Respiratory tract inflammation	32.64	14.56	9	9346	595	63479072

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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
Iris disorder	728.36	10.84	197	173564	168	34783002
Fall	382.12	10.84	2002	171759	200883	34582287
Dizziness	378.94	10.84	2108	171653	216413	34566757
Urinary retention	337.63	10.84	629	173132	35659	34747511
Orthostatic hypotension	277.88	10.84	478	173283	25441	34757729
Drug abuse	264.04	10.84	82	173679	99014	34684156
Cataract operation complication	246.14	10.84	71	173690	95	34783075
Syncope	235.96	10.84	990	172771	90461	34692709
Toxicity to various agents	230.25	10.84	402	173359	199960	34583210
Iridocele	223.66	10.84	57	173704	27	34783143

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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
Iris disorder	538.91	10.13	128	150187	245	79593828
Urinary retention	472.31	10.13	558	149757	56072	79538001
Syncope	356.12	10.13	936	149379	178513	79415560
Benign prostatic hyperplasia	330.67	10.13	229	150086	11383	79582690
Fall	315.40	10.13	1776	148539	485853	79108220
Drug ineffective	280.84	10.13	1071	149244	1079842	78514231
Haematuria	278.08	10.13	480	149835	68356	79525717
Dizziness	268.21	10.13	1803	148512	524638	79069435
Orthostatic hypotension	266.37	10.13	421	149894	55743	79538330
Atrial fibrillation	254.38	10.13	886	149429	197000	79397073

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	G04CA02	GENITO URINARY SYSTEM AND SEX HORMONES UROLOGICALS DRUGS USED IN BENIGN PROSTATIC HYPERTROPHY Alpha-adrenoreceptor antagonists
ATC	G04CA52	GENITO URINARY SYSTEM AND SEX HORMONES UROLOGICALS DRUGS USED IN BENIGN PROSTATIC HYPERTROPHY Alpha-adrenoreceptor antagonists
ATC	G04CA53	GENITO URINARY SYSTEM AND SEX HORMONES UROLOGICALS DRUGS USED IN BENIGN PROSTATIC HYPERTROPHY Alpha-adrenoreceptor antagonists
ATC	G04CA54	GENITO URINARY SYSTEM AND SEX HORMONES UROLOGICALS DRUGS USED IN BENIGN PROSTATIC HYPERTROPHY Alpha-adrenoreceptor antagonists
CHEBI has role	CHEBI:35610	antineoplastic agents
CHEBI has role	CHEBI:37890	alpha-adrenergic receptor blockaders
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

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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
Priapism	contraindication	6273006	DOID:9286
Orthostatic hypotension	contraindication	28651003
Oligozoospermia	contraindication	88311004
Cataract surgery	contraindication	110473004
Disease of liver	contraindication	235856003	DOID:409
Syncope	contraindication	271594007
Pregnancy, function	contraindication	289908002
Dizziness	contraindication	404640003
Breastfeeding (mother)	contraindication	413712001

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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	9.71	acidic
pKa2	8.16	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	Type	Activity value (-log[M])	Bioact source
D(2) dopamine receptor	GPCR	P14416	DRD2_HUMAN	Ki	7.89	CHEMBL
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN	Ki	7.87	CHEMBL
5-hydroxytryptamine receptor 1A	GPCR	P08908	5HT1A_HUMAN	Ki	9.10	CHEMBL
5-hydroxytryptamine receptor 7	GPCR	P34969	5HT7R_HUMAN	Ki	7.08	CHEMBL
Alpha-1A adrenergic receptor	GPCR	P35348	ADA1A_HUMAN	Ki	10.54	CHEMBL
D(3) dopamine receptor	GPCR	P35462	DRD3_HUMAN	Ki	9.55	CHEMBL
Alpha-2C adrenergic receptor	GPCR	P18825	ADA2C_HUMAN	Ki	8.10	CHEMBL
Alpha-1D adrenergic receptor	GPCR	P25100	ADA1D_HUMAN	Ki	10.24	CHEMBL
Alpha-1B adrenergic receptor	GPCR	P35368	ADA1B_HUMAN	Ki	9.21	CHEMBL
Alpha-1A adrenergic receptor	GPCR		ADA1A_RAT	Ki	10.52	CHEMBL

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External reference:

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ID	Source
JGX	PDB_CHEM_ID
006115	NDDF
006116	NDDF
106463-17-6	SECONDARY_CAS_RN
108559004	SNOMEDCT_US
108560009	SNOMEDCT_US
129211	PUBCHEM_CID
171693	MMSL
20642	MMSL
236495	RXNORM

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Dutasteride and Tamsulosin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	2	10370-280	CAPSULE	0.40 mg	ORAL	ANDA	28 sections
Dutasteride and Tamsulosin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	2	10370-280	CAPSULE	0.40 mg	ORAL	ANDA	28 sections
FLOMAX	HUMAN PRESCRIPTION DRUG LABEL	1	0024-5837	CAPSULE	0.40 mg	ORAL	NDA	30 sections
FLOMAX	HUMAN PRESCRIPTION DRUG LABEL	1	0024-5837	CAPSULE	0.40 mg	ORAL	NDA	30 sections
FLOMAX	HUMAN PRESCRIPTION DRUG LABEL	1	16590-489	CAPSULE	0.40 mg	ORAL	NDA	28 sections
JALYN	HUMAN PRESCRIPTION DRUG LABEL	2	0173-0809	CAPSULE	0.40 mg	ORAL	NDA	29 sections
JALYN	HUMAN PRESCRIPTION DRUG LABEL	2	0173-0809	CAPSULE	0.40 mg	ORAL	NDA	29 sections
Tamsulosin hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0228-2996	CAPSULE	0.40 mg	ORAL	ANDA	19 sections
Tamsulosin hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0228-2996	CAPSULE	0.40 mg	ORAL	ANDA	19 sections
Tamsulosin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0615-7995	CAPSULE	0.40 mg	ORAL	ANDA	26 sections

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