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

Stem definition	Drug id	CAS RN
antihypertensive substances, prazosin derivatives	954	74191-85-8

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: doxazosin doxazosin mesylate doxazosine doxazosin mesilate	A prazosin-related compound that is a selective alpha-1-adrenergic blocker. Molecular weight: 451.48 Formula: C23H25N5O5 CLOGP: 3.58 LIPINSKI: 0 HAC: 10 HDO: 1 TPSA: 112.27 ALOGS: -2.76 ROTB: 4 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

doxazosin
doxazosin mesylate
doxazosine
doxazosin mesilate

A prazosin-related compound that is a selective alpha-1-adrenergic blocker.

Molecular weight: 451.48
Formula: C23H25N5O5
CLOGP: 3.58
LIPINSKI: 0
HAC: 10
HDO: 1
TPSA: 112.27
ALOGS: -2.76
ROTB: 4

Status: OFP

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

Drug dosage:

Dose	Unit	Route
4	mg	O

ADMET properties:

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Property	Value	Reference
t_half (Half-life)	10 hours	Lombardo F, Berellini G, Obach RS
CL (Clearance)	1.60 mL/min/kg	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	1.30 L/kg	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
BA (Bioavailability)	0.65 %	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)	0.59 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
fu (Fraction unbound in plasma)	0.02 %	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
Nov. 2, 1990	FDA	PFIZER

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
Hyperkalaemia	153.78	13.22	130	19436	54073	63415383
Hypotension	146.96	13.22	284	19282	272320	63197136
Syncope	123.53	13.22	166	19400	117219	63352237
Hyponatraemia	118.89	13.22	159	19407	111741	63357715
Hypertensive crisis	110.40	13.22	65	19501	15221	63454235
Drug interaction	95.53	13.22	215	19351	228916	63240540
Acute kidney injury	91.28	13.22	230	19336	263185	63206271
Angioedema	69.98	13.22	80	19486	47885	63421571
Drug intolerance	62.78	13.22	10	19556	308651	63160805
Bladder prolapse	62.76	13.22	24	19542	2132	63467324

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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
Syncope	165.07	11.22	324	36654	91127	34828826
Orthostatic hypotension	107.78	11.22	135	36843	25784	34894169
Mycotic allergy	105.54	11.22	35	36943	573	34919380
Off label use	103.22	11.22	179	36799	419345	34500608
Mite allergy	100.61	11.22	35	36943	667	34919286
Spirometry abnormal	99.56	11.22	35	36943	689	34919264
Dust allergy	95.51	11.22	36	36942	870	34919083
Hypertensive crisis	95.44	11.22	77	36901	8674	34911279
Conjunctivitis allergic	93.38	11.22	38	36940	1132	34918821
Asthma	90.38	11.22	162	36816	42494	34877459

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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
Syncope	288.11	11.20	449	49247	179000	79515692
Hypertensive crisis	208.84	11.20	141	49555	20629	79674063
Hyperkalaemia	190.08	11.20	291	49405	114107	79580585
Hypotension	165.95	11.20	626	49070	439691	79255001
Drug interaction	158.69	11.20	593	49103	414590	79280102
Orthostatic hypotension	153.27	11.20	182	49514	55982	79638710
Rectal prolapse	113.93	11.20	45	49651	2133	79692559
Acute kidney injury	108.20	11.20	621	49075	518783	79175909
Off label use	104.35	11.20	260	49436	906955	78787737
Spirometry abnormal	104.01	11.20	34	49662	925	79693767

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	C02CA04	CARDIOVASCULAR SYSTEM ANTIHYPERTENSIVES ANTIADRENERGIC AGENTS, PERIPHERALLY ACTING Alpha-adrenoreceptor antagonists
ATC	G04CA55	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:35620	vasodilator agents
CHEBI has role	CHEBI:35674	antihypertensive drugs
CHEBI has role	CHEBI:37890	alpha-adrenergic receptor blockaders
CHEBI has role	CHEBI:59844	antihyperplasia drugs
FDA EPC	N0000175553	alpha-Adrenergic Blocker
FDA MoA	N0000000099	Adrenergic alpha-Antagonists
MeSH PA	D018663	Adrenergic 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
Hypertensive disorder	indication	38341003	DOID:10763
Benign prostatic hyperplasia	indication	266569009
Priapism	contraindication	6273006	DOID:9286
Stenosis of intestine	contraindication	23065003
Orthostatic hypotension	contraindication	28651003
Low blood pressure	contraindication	45007003
Hepatic failure	contraindication	59927004
Chronic idiopathic constipation	contraindication	82934008
Cataract surgery	contraindication	110473004
Disease of liver	contraindication	235856003	DOID:409

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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	7.22	Basic
pKa2	0.72	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-1D adrenergic receptor	GPCR	P25100	ADA1D_HUMAN	ANTAGONIST	Ki	8.85	WOMBAT-PK	CHEMBL
Alpha-1B adrenergic receptor	GPCR	P35368	ADA1B_HUMAN	ANTAGONIST	Ki	9.10	WOMBAT-PK	CHEMBL
Alpha-1A adrenergic receptor	GPCR	P35348	ADA1A_HUMAN	ANTAGONIST	Ki	8.80	WOMBAT-PK	CHEMBL
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		IC50	6.23	WOMBAT-PK
Multidrug resistance protein 1	Transporter	P08183	MDR1_HUMAN		Ki	5	WOMBAT-PK
Sodium-dependent serotonin transporter	Transporter	P31645	SC6A4_HUMAN		Ki	5.85	DRUG MATRIX
5-hydroxytryptamine receptor 2B	GPCR	P41595	5HT2B_HUMAN		Ki	6.63	DRUG MATRIX
5-hydroxytryptamine receptor 2C	GPCR	P28335	5HT2C_HUMAN		Ki	6.55	DRUG MATRIX
Alpha-2C adrenergic receptor	GPCR	P18825	ADA2C_HUMAN		Ki	6.55	CHEMBL
Sodium-dependent dopamine transporter	Transporter	Q01959	SC6A3_HUMAN		Ki	6.83	DRUG MATRIX

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External reference:

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ID	Source
003561	NDDF
004493	NDDF
108556006	SNOMEDCT_US
108557002	SNOMEDCT_US
3157	PUBCHEM_CID
372508002	SNOMEDCT_US
37806	MMSL
39173	RXNORM
4019565	VANDF
4019735	VUID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Cardura	HUMAN PRESCRIPTION DRUG LABEL	1	0049-2410	TABLET	1 mg	ORAL	NDA	28 sections
Cardura	HUMAN PRESCRIPTION DRUG LABEL	1	0049-2410	TABLET	1 mg	ORAL	NDA	28 sections
Cardura	HUMAN PRESCRIPTION DRUG LABEL	1	0049-2512	TABLET	2 mg	ORAL	NDA	28 sections
Cardura	HUMAN PRESCRIPTION DRUG LABEL	1	0049-2512	TABLET	2 mg	ORAL	NDA	28 sections
Cardura	HUMAN PRESCRIPTION DRUG LABEL	1	0049-2614	TABLET	4 mg	ORAL	NDA	28 sections
Cardura	HUMAN PRESCRIPTION DRUG LABEL	1	0049-2614	TABLET	4 mg	ORAL	NDA	28 sections
Cardura	HUMAN PRESCRIPTION DRUG LABEL	1	0049-2716	TABLET	8 mg	ORAL	NDA	28 sections
Cardura	HUMAN PRESCRIPTION DRUG LABEL	1	0049-2716	TABLET	8 mg	ORAL	NDA	28 sections
Cardura	HUMAN PRESCRIPTION DRUG LABEL	1	0049-2750	TABLET	1 mg	ORAL	NDA	28 sections
Cardura	HUMAN PRESCRIPTION DRUG LABEL	1	0049-2750	TABLET	1 mg	ORAL	NDA	28 sections

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