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

Stem definition	Drug id	CAS RN
antihypertensives, hydrazinephthalazine derivatives	1384	86-54-4

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: hydralazine hydralazine hydrochloride hydralazine HCl	A direct-acting vasodilator that is used as an antihypertensive agent. Molecular weight: 160.18 Formula: C8H8N4 CLOGP: 1.17 LIPINSKI: 0 HAC: 4 HDO: 2 TPSA: 63.83 ALOGS: -1.78 ROTB: 1 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

hydralazine
hydralazine hydrochloride
hydralazine HCl

A direct-acting vasodilator that is used as an antihypertensive agent.

Molecular weight: 160.18
Formula: C8H8N4
CLOGP: 1.17
LIPINSKI: 0
HAC: 4
HDO: 2
TPSA: 63.83
ALOGS: -1.78
ROTB: 1

Status: OFP

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

Drug dosage:

Dose	Unit	Route
0.10	g	O

ADMET properties:

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Property	Value	Reference
CL (Clearance)	85 mL/min/kg	Lombardo F, Berellini G, Obach RS
EoM (Fraction excreted unchanged in urine)	8 %	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	44.20 mg/mL	Benet LZ, Broccatelli F, Oprea TI
BA (Bioavailability)	23 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
MRTD (Maximum Recommended Therapeutic Daily Dose)	20.79 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
Vd (Volume of distribution)	1.50 L/kg	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	1 hours	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
fu (Fraction unbound in plasma)	0.12 %	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
Jan. 15, 1953	FDA

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
Anti-neutrophil cytoplasmic antibody positive vasculitis	1831.05	12.44	387	27378	2512	63458745
Glomerulonephritis rapidly progressive	532.62	12.44	116	27649	879	63460378
Pulmonary renal syndrome	382.27	12.44	77	27688	377	63460880
Cardiac failure congestive	353.07	12.44	305	27460	92128	63369129
Gastrointestinal tract mucosal pigmentation	223.18	12.44	52	27713	550	63460707
Glomerulonephritis	222.54	12.44	65	27700	1741	63459516
Lupus-like syndrome	196.52	12.44	107	27658	15188	63446069
Pulmonary alveolar haemorrhage	183.11	12.44	71	27694	4597	63456660
Acute kidney injury	158.52	12.44	353	27412	263062	63198195
Vasculitis	146.13	12.44	94	27671	18115	63443142

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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
Anti-neutrophil cytoplasmic antibody positive vasculitis	909.88	12.72	187	19913	742	34936089
Lupus-like syndrome	275.33	12.72	90	20010	2666	34934165
Gastrointestinal tract mucosal pigmentation	262.04	12.72	60	20040	430	34936401
Glomerulonephritis rapidly progressive	259.73	12.72	63	20037	595	34936236
Cardiac failure congestive	239.21	12.72	266	19834	83004	34853827
Pulmonary renal syndrome	215.70	12.72	43	20057	140	34936691
Device interaction	96.31	12.72	28	20072	554	34936277
Acute kidney injury	91.06	12.72	381	19719	304607	34632224
Chronic kidney disease	85.85	12.72	112	19988	41098	34895733
Pulmonary alveolar haemorrhage	74.38	12.72	49	20051	7463	34929368

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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
Anti-neutrophil cytoplasmic antibody positive vasculitis	2750.90	11.49	582	40391	3147	79700268
Glomerulonephritis rapidly progressive	737.87	11.49	171	40802	1477	79701938
Cardiac failure congestive	585.27	11.49	525	40448	141877	79561538
Pulmonary renal syndrome	576.68	11.49	118	40855	522	79702893
Gastrointestinal tract mucosal pigmentation	486.28	11.49	112	40861	938	79702477
Lupus-like syndrome	464.67	11.49	197	40776	13660	79689755
Pulmonary alveolar haemorrhage	244.81	11.49	119	40854	11338	79692077
Glomerulonephritis	242.36	11.49	84	40889	3349	79700066
Acute kidney injury	230.70	11.49	686	40287	518718	79184697
Vasculitis	192.75	11.49	134	40839	24968	79678447

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	C02DB02	CARDIOVASCULAR SYSTEM ANTIHYPERTENSIVES ARTERIOLAR SMOOTH MUSCLE, AGENTS ACTING ON Hydrazinophthalazine derivatives
ATC	C02LG02	CARDIOVASCULAR SYSTEM ANTIHYPERTENSIVES ANTIHYPERTENSIVES AND DIURETICS IN COMBINATION Hydrazinophthalazine derivatives and diuretics
CHEBI has role	CHEBI:35620	vasodilator agents
CHEBI has role	CHEBI:35674	antihypertensive drugs
FDA EPC	N0000175564	Arteriolar Vasodilator
FDA PE	N0000175379	Arteriolar Vasodilation
MeSH PA	D000959	Antihypertensive Agents
MeSH PA	D002317	Cardiovascular Agents
MeSH PA	D014665	Vasodilator 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
Chronic heart failure	indication	48447003
Anuria	contraindication	2472002	DOID:2983
Suicidal thoughts	contraindication	6471006
Peptic ulcer	contraindication	13200003	DOID:750
Hypercholesterolemia	contraindication	13644009
Chronic disease of respiratory system	contraindication	17097001
Secondary angle-closure glaucoma	contraindication	21571006
Myocardial infarction	contraindication	22298006	DOID:5844
Electroconvulsive therapy	contraindication	23835007

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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	6.81	Basic
pKa2	3.26	Basic
pKa3	2.62	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
Ryanodine receptor 2	Ion channel	Q92736	RYR2_HUMAN	BLOCKER			SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
Voltage-dependent L-type calcium channel subunit alpha-1C	Ion channel	Q13936	CAC1C_HUMAN				WOMBAT-PK
DNA (cytosine-5)-methyltransferase 1	Enzyme	P26358	DNMT1_HUMAN				WOMBAT-PK
DNA (cytosine-5)-methyltransferase 3A	Enzyme	Q9Y6K1	DNM3A_HUMAN				WOMBAT-PK
DNA (cytosine-5)-methyltransferase 3B	Enzyme	Q9UBC3	DNM3B_HUMAN				WOMBAT-PK
Aspartate aminotransferase, cytoplasmic	Enzyme	P17174	AATC_HUMAN		Ki	4.83	CHEMBL
Aldehyde oxidase	Enzyme	Q06278	AOXA_HUMAN		IC50	5.41	CHEMBL
Myeloperoxidase	Enzyme	P05164	PERM_HUMAN		IC50	6.05	CHEMBL
Arachidonate 15-lipoxygenase	Enzyme		LOX15_RABIT		IC50	5.44	DRUG MATRIX
Acetylcholinesterase	Enzyme		ACES_ELEEL		Ki	5.15	CHEMBL

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External reference:

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ID	Source
HLZ	PDB_CHEM_ID
000632	NDDF
004489	NDDF
1	INN_ID
22696000	SNOMEDCT_US
26NAK24LS8	UNII
28662003	SNOMEDCT_US
304-20-1	SECONDARY_CAS_RN
3637	PUBCHEM_CID
387125005	SNOMEDCT_US

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
HYDRALAZINE HYDROCHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	0404-9875	INJECTION	20 mg	INTRAVENOUS	ANDA	12 sections
HYDRALAZINE HYDROCHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	0404-9875	INJECTION	20 mg	INTRAVENOUS	ANDA	12 sections
HYDRALAZINE HYDROCHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	0404-9986	INJECTION	20 mg	INTRAVENOUS	ANDA	11 sections
HYDRALAZINE HYDROCHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	0404-9986	INJECTION	20 mg	INTRAVENOUS	ANDA	11 sections
HYDRALAZINE HYDROCHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	0404-9994	INJECTION, SOLUTION	20 mg	INTRAMUSCULAR	ANDA	12 sections
Hydralazine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0517-0901	INJECTION, SOLUTION	20 mg	INTRAMUSCULAR	ANDA	19 sections
Hydralazine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0615-7973	TABLET	100 mg	ORAL	ANDA	9 sections
Hydralazine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0615-7973	TABLET	100 mg	ORAL	ANDA	9 sections
HydrALAZINE hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0641-6231	INJECTION, SOLUTION	20 mg	INTRAMUSCULAR	ANDA	18 sections
Hydralazine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0904-6440	TABLET, FILM COATED	10 mg	ORAL	ANDA	10 sections

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