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

Stem definition	Drug id	CAS RN
vasodilators	2796	34661-75-1

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: urapidil ebrantil eupressyl mediatensyl uraprene uropidil urapidil hydrochloride urapidil HCl	Molecular weight: 387.48 Formula: C20H29N5O3 CLOGP: 2.25 LIPINSKI: 0 HAC: 8 HDO: 1 TPSA: 68.36 ALOGS: -2.86 ROTB: 7

Molecule

Description

Molfile Inchi Smiles

Synonyms:

urapidil
ebrantil
eupressyl
mediatensyl
uraprene
uropidil
urapidil hydrochloride
urapidil HCl

Molecular weight: 387.48
Formula: C20H29N5O3
CLOGP: 2.25
LIPINSKI: 0
HAC: 8
HDO: 1
TPSA: 68.36
ALOGS: -2.86
ROTB: 7

Drug dosage:

Dose	Unit	Route
0.12	g	O
50	mg	P

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	78 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
MRTD (Maximum Recommended Therapeutic Daily Dose)	6.64 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
t_half (Half-life)	3.50 hours	Lombardo F, Berellini G, Obach RS
CL (Clearance)	3.10 mL/min/kg	Lombardo F, Berellini G, Obach RS
S (Water solubility)	19 mg/mL	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	15 %	Benet LZ, Broccatelli F, Oprea TI
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
Vd (Volume of distribution)	0.75 L/kg	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
Jan. 1, 1981	YEAR INTRODUCED

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
Acute kidney injury	221.75	25.47	187	5650	263228	63219957
Hyponatraemia	143.00	25.47	102	5735	111798	63371387
Hyperkalaemia	139.23	25.47	77	5760	54126	63429059
Product prescribing error	98.05	25.47	48	5789	26241	63456944
Bradycardia	87.14	25.47	64	5773	73163	63410022
Mixed liver injury	64.78	25.47	22	5815	4713	63478472
Product monitoring error	61.85	25.47	21	5816	4495	63478690
Fall	58.51	25.47	118	5719	392216	63090969
Anaemia	58.46	25.47	100	5737	293330	63189855
Shock haemorrhagic	52.24	25.47	23	5814	9872	63473313

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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
Acute kidney injury	139.15	21.56	208	5579	304780	34646364
Toxic epidermal necrolysis	118.63	21.56	62	5725	21584	34929560
Coma	67.95	21.56	58	5729	45620	34905524
Rash maculo-papular	61.42	21.56	45	5742	28406	34922738
Hepatic cytolysis	61.29	21.56	35	5752	14461	34936683
Ureteric compression	60.33	21.56	13	5774	267	34950877
Eosinophilia	55.52	21.56	41	5746	26181	34924963
General physical health deterioration	50.35	21.56	82	5705	128187	34822957
Drug reaction with eosinophilia and systemic symptoms	49.23	21.56	42	5745	32970	34918174
Hyperkalaemia	49.23	21.56	59	5728	69330	34881814

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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
Acute kidney injury	334.25	20.42	390	11057	519014	79213927
Hyperkalaemia	162.22	20.42	133	11314	114265	79618676
Hyponatraemia	112.56	20.42	133	11314	177715	79555226
Toxic epidermal necrolysis	106.44	20.42	71	11376	44510	79688431
Bradycardia	93.47	20.42	106	11341	135451	79597490
Product prescribing error	89.62	20.42	64	11383	44749	79688192
Rash maculo-papular	87.46	20.42	69	11378	56009	79676932
General physical health deterioration	86.16	20.42	147	11300	275091	79457850
Anaemia	85.01	20.42	193	11254	444822	79288119
Shock haemorrhagic	76.20	20.42	43	11404	20017	79712924

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	C02CA06	CARDIOVASCULAR SYSTEM ANTIHYPERTENSIVES ANTIADRENERGIC AGENTS, PERIPHERALLY ACTING Alpha-adrenoreceptor 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	D000959	Antihypertensive Agents
MeSH PA	D002317	Cardiovascular Agents
MeSH PA	D018377	Neurotransmitter Agents
MeSH PA	D018490	Serotonin Agents
MeSH PA	D017366	Serotonin Receptor Agonists

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

Disease	Relation	SNOMED_ID	DOID
Hypertensive emergency	indication	132721000119104

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	6.85	Basic
pKa2	2.48	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	8.85	WOMBAT-PK	KEGG DRUG
Alpha-1D adrenergic receptor	GPCR	P25100	ADA1D_HUMAN	ANTAGONIST	Ki	7.90	WOMBAT-PK	KEGG DRUG
Alpha-1B adrenergic receptor	GPCR	P35368	ADA1B_HUMAN	ANTAGONIST	Ki	7.10	WOMBAT-PK	KEGG DRUG
5-hydroxytryptamine receptor 1A	GPCR	P08908	5HT1A_HUMAN		Ki	9.46	WOMBAT-PK

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External reference:

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ID	Source
005866	NDDF
005867	NDDF
3169	INN_ID
39230	RXNORM
5639	PUBCHEM_CID
64887-14-5	SECONDARY_CAS_RN
698807007	SNOMEDCT_US
734449004	SNOMEDCT_US
A78GF17HJS	UNII
C0077857	UMLSCUI

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Pharmaceutical products:

None