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

Stem definition	Drug id	CAS RN
angiotensin-converting enzyme inhibitors	2340	85441-61-8

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: quinapril ectren koretic quinapril hydrochloride quinapril HCl	A tetrahydroisoquinoline derivative and ANGIOTENSIN CONVERTING ENZYME inhibitor that is used in the treatment of HYPERTENSION and HEART FAILURE. Molecular weight: 438.52 Formula: C25H30N2O5 CLOGP: 1.74 LIPINSKI: 0 HAC: 7 HDO: 2 TPSA: 95.94 ALOGS: -4.71 ROTB: 10 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

quinapril
ectren
koretic
quinapril hydrochloride
quinapril HCl

A tetrahydroisoquinoline derivative and ANGIOTENSIN CONVERTING ENZYME inhibitor that is used in the treatment of HYPERTENSION and HEART FAILURE.

Molecular weight: 438.52
Formula: C25H30N2O5
CLOGP: 1.74
LIPINSKI: 0
HAC: 7
HDO: 2
TPSA: 95.94
ALOGS: -4.71
ROTB: 10

Status: OFP

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

Drug dosage:

Dose	Unit	Route
15	mg	O
15	mg	P

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	60 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
EoM (Fraction excreted unchanged in urine)	3.10 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	2.61 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Bocci G, Oprea TI, Benet LZ
S (Water solubility)	0.00 mg/mL	Benet LZ, Broccatelli F, Oprea TI

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Approvals:

Date	Agency	Company	Orphan
Nov. 19, 1991	FDA	PFIZER PHARMS

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
Sedation complication	1059.87	16.07	307	16470	13515	63458730
Orthostatic hypotension	1029.54	16.07	379	16398	35781	63436464
Creatinine renal clearance decreased	1026.90	16.07	311	16466	15997	63456248
Sedation	952.85	16.07	365	16412	38444	63433801
Cognitive disorder	876.65	16.07	381	16396	55434	63416811
Blood calcium decreased	871.50	16.07	309	16468	26142	63446103
Balance disorder	746.47	16.07	388	16389	84034	63388211
Depressed level of consciousness	655.81	16.07	322	16455	61756	63410489
Constipation	448.83	16.07	412	16365	224531	63247714
Mobility decreased	428.14	16.07	310	16467	120849	63351396

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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
Myocardial infarction	124.30	14.59	157	9174	120928	34826672
Coronary artery disease	118.14	14.59	100	9231	48205	34899395
Cardiac failure congestive	101.71	14.59	118	9213	83152	34864448
Blood mercury abnormal	101.26	14.59	21	9310	213	34947387
5-hydroxyindolacetic acid in urine increased	99.30	14.59	21	9310	236	34947364
Low density lipoprotein decreased	72.45	14.59	22	9309	1121	34946479
Expired product administered	62.61	14.59	26	9305	3315	34944285
Head titubation	58.89	14.59	15	9316	396	34947204
Hepatic neoplasm	56.91	14.59	21	9310	1956	34945644
Blood glucose increased	55.21	14.59	78	9253	66640	34880960

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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
Sedation complication	1100.37	13.97	330	22144	15339	79706575
Creatinine renal clearance decreased	996.45	13.97	320	22154	18682	79703232
Orthostatic hypotension	885.10	13.97	392	22082	55772	79666142
Sedation	849.33	13.97	372	22102	51523	79670391
Blood calcium decreased	845.82	13.97	323	22151	31496	79690418
Cognitive disorder	803.01	13.97	392	22082	69534	79652380
Balance disorder	691.31	13.97	398	22076	98459	79623455
Depressed level of consciousness	522.46	13.97	330	22144	96322	79625592
Mobility decreased	468.21	13.97	337	22137	121838	79600076
Constipation	356.68	13.97	418	22056	282632	79439282

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	C09AA06	CARDIOVASCULAR SYSTEM AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM ACE INHIBITORS, PLAIN ACE inhibitors, plain
ATC	C09BA06	CARDIOVASCULAR SYSTEM AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM ACE INHIBITORS, COMBINATIONS ACE inhibitors and diuretics
CHEBI has role	CHEBI:35457	ACE inhibitor
CHEBI has role	CHEBI:35674	antihypertensive drugs
CHEBI has role	CHEBI:50266	Prodrugs
CHEBI has role	CHEBI:35620	vasodilator agents
FDA EPC	N0000175562	Angiotensin Converting Enzyme Inhibitor
FDA MoA	N0000000181	Angiotensin-converting Enzyme Inhibitors
MeSH PA	D000806	Angiotensin-Converting Enzyme Inhibitors
MeSH PA	D000959	Antihypertensive 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
Atrial fibrillation	off-label use	49436004	DOID:0060224
Diabetic renal disease	off-label use	127013003
Acute scleroderma renal crisis	off-label use	236503001
Diastolic heart failure	off-label use	418304008	DOID:9775
Nondiabetic Proteinuric Nephropathy	off-label use
Anuria	contraindication	2472002	DOID:2983
Hypercholesterolemia	contraindication	13644009
Hyperkalemia	contraindication	14140009

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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	2.96	acidic
pKa2	5.72	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])	Mechanism action	Bioact source	MoA source
Angiotensin-converting enzyme	Enzyme	P12821	ACE_HUMAN	INHIBITOR	IC50	8.08		CHEMBL	CHEMBL
Angiotensin-converting enzyme	Enzyme		ACE_RABIT		IC50	5.40		DRUG MATRIX

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External reference:

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ID	Source
003612	NDDF
003613	NDDF
107994	PUBCHEM_CID
108578004	SNOMEDCT_US
1546359	RXNORM
34SSX5LDE5	UNII
386874003	SNOMEDCT_US
386875002	SNOMEDCT_US
4020379	VANDF
4020549	VUID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Accupril	HUMAN PRESCRIPTION DRUG LABEL	1	0071-0527	TABLET, FILM COATED	5 mg	ORAL	NDA	25 sections
Accupril	HUMAN PRESCRIPTION DRUG LABEL	1	0071-0527	TABLET, FILM COATED	5 mg	ORAL	NDA	25 sections
Accupril	HUMAN PRESCRIPTION DRUG LABEL	1	0071-0527	TABLET, FILM COATED	5 mg	ORAL	NDA	25 sections
Accupril	HUMAN PRESCRIPTION DRUG LABEL	1	0071-0530	TABLET, FILM COATED	10 mg	ORAL	NDA	25 sections
Accupril	HUMAN PRESCRIPTION DRUG LABEL	1	0071-0530	TABLET, FILM COATED	10 mg	ORAL	NDA	25 sections
Accupril	HUMAN PRESCRIPTION DRUG LABEL	1	0071-0530	TABLET, FILM COATED	10 mg	ORAL	NDA	25 sections
Accupril	HUMAN PRESCRIPTION DRUG LABEL	1	0071-0532	TABLET, FILM COATED	20 mg	ORAL	NDA	25 sections
Accupril	HUMAN PRESCRIPTION DRUG LABEL	1	0071-0532	TABLET, FILM COATED	20 mg	ORAL	NDA	25 sections
Accupril	HUMAN PRESCRIPTION DRUG LABEL	1	0071-0532	TABLET, FILM COATED	20 mg	ORAL	NDA	25 sections
Accupril	HUMAN PRESCRIPTION DRUG LABEL	1	0071-0535	TABLET, FILM COATED	40 mg	ORAL	NDA	25 sections

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