benazepril indications/contra

Stem definitionDrug idCAS RN
angiotensin-converting enzyme inhibitors 299 86541-75-5

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • benazepril
  • cibacen
  • benazepril hydrochloride
  • benazepril HCl
prodrug of benazeprilat inhibit angiotensin-converting enzyme (ACE) and results in decreased plasma angiotensin II, which leads to decreased vasopressor activity and to decreased aldosterone secretion
  • Molecular weight: 424.50
  • Formula: C24H28N2O5
  • CLOGP: 1.82
  • LIPINSKI: 0
  • HAC: 7
  • HDO: 2
  • TPSA: 95.94
  • ALOGS: -4.61
  • ROTB: 10

Drug dosage:

DoseUnitRoute
7.50 mg O

Approvals:

DateAgencyCompanyOrphan
June 25, 1991 FDA US PHARMS HOLDINGS I

FDA Adverse Event Reporting System

scroll-->
MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Angioedema 1046.84 36.02 226 1108 14909 3369616
Completed suicide 355.52 36.02 112 1222 31002 3353523
Swollen tongue 293.49 36.02 70 1264 6773 3377752
Cough 218.05 36.02 83 1251 39775 3344750
Drug hypersensitivity 204.79 36.02 77 1257 35603 3348922
Dizziness 190.16 36.02 91 1243 76421 3308104
Hypotension 180.33 36.02 77 1257 49437 3335088
Blood pressure inadequately controlled 158.88 36.02 32 1302 1388 3383137
Swelling face 145.73 36.02 45 1289 11371 3373154
Blood creatinine increased 135.41 36.02 50 1284 21768 3362757
Acute kidney injury 119.50 36.02 58 1276 49625 3334900
Dyspnoea 119.20 36.02 74 1260 102860 3281665
Blood pressure increased 109.25 36.02 43 1291 22187 3362338
Toxicity to various agents 107.30 36.02 53 1281 47001 3337524
Oedema peripheral 103.77 36.02 47 1287 34314 3350211
Hyperkalaemia 97.01 36.02 33 1301 11261 3373264
Lip swelling 89.78 36.02 27 1307 6204 3378321
Asthenia 85.41 36.02 51 1283 65614 3318911
Palpitations 83.57 36.02 34 1300 19049 3365476
Concomitant disease progression 75.97 36.02 16 1318 861 3383664
Nausea 74.66 36.02 61 1273 129584 3254941
Hypertension 72.02 36.02 38 1296 38428 3346097
Oropharyngeal swelling 69.87 36.02 13 1321 367 3384158
Product quality issue 66.40 36.02 32 1302 26703 3357822
Dysphagia 65.96 36.02 29 1305 19622 3364903
Headache 62.97 36.02 48 1286 91932 3292593
Overdose 61.96 36.02 33 1301 33945 3350580
Drug ineffective 59.21 36.02 51 1283 116039 3268486
Blood pressure decreased 58.28 36.02 24 1310 13812 3370713
Renal failure 54.49 36.02 30 1304 32910 3351615

Pharmacologic Action:

scroll-->
SourceCodeDescription
ATC C09AA07 CARDIOVASCULAR SYSTEM
AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
ACE INHIBITORS, PLAIN
ACE inhibitors, plain
ATC C09BA07 CARDIOVASCULAR SYSTEM
AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
ACE INHIBITORS, COMBINATIONS
ACE inhibitors and diuretics
FDA EPC N0000175562 Angiotensin Converting Enzyme Inhibitor
FDA PE N0000178477 Decreased Blood Pressure
MeSH PA D000806 Angiotensin-Converting Enzyme Inhibitors
MeSH PA D000959 Antihypertensive Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D011480 Protease Inhibitors
CHEBI has role CHEBI:35457 EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor
CHEBI has role CHEBI:50266 prodrug

Drug Use (View source of the data)

scroll-->
DiseaseRelationSNOMED_IDDOID
Hypertensive disorder indication 38341003 DOID:10763
Anuria contraindication 2472002 DOID:2983
Hypercholesterolemia contraindication 13644009
Hyperkalemia contraindication 14140009
Jaundice contraindication 18165001
Secondary angle-closure glaucoma contraindication 21571006
Hypovolemia contraindication 28560003
Dehydration contraindication 34095006
Hyperuricemia contraindication 35885006 DOID:1920
Angioedema contraindication 41291007 DOID:1558
Hypokalemia contraindication 43339004
Low blood pressure contraindication 45007003
Systemic lupus erythematosus contraindication 55464009 DOID:9074
Sympathectomy contraindication 57071006
Hepatic failure contraindication 59927004
Hypercalcemia contraindication 66931009 DOID:12678
Hyperparathyroidism contraindication 66999008 DOID:13543
Hypochloremic alkalosis contraindication 70134007
Hepatic coma contraindication 72836002 DOID:12550
Diabetes mellitus contraindication 73211009 DOID:9351
Chronic idiopathic constipation contraindication 82934008
Hereditary angioneurotic edema contraindication 82966003 DOID:14735
Hyponatremia contraindication 89627008
Gout contraindication 90560007 DOID:13189
Kidney disease contraindication 90708001 DOID:2527
Disorder of connective tissue contraindication 105969002 DOID:65
Liver function tests abnormal contraindication 166603001
Hypomagnesemia contraindication 190855004
Acute pancreatitis contraindication 197456007 DOID:2913
Disease of liver contraindication 235856003 DOID:409
Neonatal hyperbilirubinemia contraindication 281610001
Pregnancy, function contraindication 289908002
Renal artery stenosis contraindication 302233006
Neutropenic disorder contraindication 303011007 DOID:1227
Bone marrow depression contraindication 307762000
Azotemia contraindication 445009001
Head and Neck Angioedema contraindication
Hemodialysis with High-Flux Membrane contraindication
Intestinal Angioedema contraindication
Severe Aortic Valve Stenosis contraindication
Chronic heart failure off-label use 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
Hypertension due to Scleroderma off-label use

Acid dissociation constants calculated using MoKa v3.0.0

scroll-->
Dissociation levelDissociation constantType (acidic/basic)
pKa1 2.9 acidic
pKa2 5.34 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

scroll-->
TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Angiotensin-converting enzyme Enzyme INHIBITOR IC50 6.51 WOMBAT-PK CHEMBL
Angiotensin-converting enzyme Enzyme IC50 8.70 CHEMBL
Angiotensin-converting enzyme Enzyme IC50 8.77 CHEMBL

External reference:

scroll-->
IDSource
DB00542 DRUGBANK_ID
4020817 VUID
N0000148336 NUI
C0053091 UMLSCUI
6374 IUPHAR_LIGAND_ID
D00620 KEGG_DRUG
CHEMBL838 ChEMBL_ID
4020817 VANDF
N0000006630 NDFRT
N0000148336 NDFRT
003597 NDDF
d00730 MMSL
18867 RXNORM
108572003 SNOMEDCT_US
372511001 SNOMEDCT_US
5362124 PUBCHEM_CID
CHEMBL1694 ChEMBL_ID
CHEMBL1192519 ChEMBL_ID
C052133 MESH_SUPPLEMENTAL_RECORD_UI
C044946 MESH_SUPPLEMENTAL_RECORD_UI
JRM708L703 UNII
6128 INN_ID
86541-78-8 SECONDARY_CAS_RN
CHEBI:3011 CHEBI

Pharmaceutical products:

scroll-->
ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
Lotrel HUMAN PRESCRIPTION DRUG LABEL 2 0078-0364 CAPSULE 20 mg ORAL NDA 19 sections
Lotrel HUMAN PRESCRIPTION DRUG LABEL 2 0078-0379 CAPSULE 40 mg ORAL NDA 19 sections
Lotrel HUMAN PRESCRIPTION DRUG LABEL 2 0078-0384 CAPSULE 40 mg ORAL NDA 19 sections
Lotrel HUMAN PRESCRIPTION DRUG LABEL 2 0078-0404 CAPSULE 10 mg ORAL NDA 19 sections
Lotrel HUMAN PRESCRIPTION DRUG LABEL 2 0078-0405 CAPSULE 10 mg ORAL NDA 19 sections
Lotrel HUMAN PRESCRIPTION DRUG LABEL 2 0078-0406 CAPSULE 20 mg ORAL NDA 19 sections
Benazepril Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0093-5124 TABLET, COATED 5 mg ORAL ANDA 17 sections
Benazepril Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0093-5125 TABLET, COATED 10 mg ORAL ANDA 17 sections
Benazepril Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0093-5126 TABLET, COATED 20 mg ORAL ANDA 17 sections
Benazepril Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0093-5127 TABLET, COATED 40 mg ORAL ANDA 17 sections
Amlodipine and Benazepril Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 2 0093-7370 CAPSULE 10 mg ORAL ANDA 18 sections
Amlodipine and Benazepril Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 2 0093-7371 CAPSULE 10 mg ORAL ANDA 18 sections
Amlodipine and Benazepril Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 2 0093-7372 CAPSULE 20 mg ORAL ANDA 18 sections
Amlodipine and Benazepril Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 2 0093-7373 CAPSULE 20 mg ORAL ANDA 18 sections
Amlodipine and Benazepril Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 2 0093-7670 CAPSULE 40 mg ORAL ANDA 18 sections
Amlodipine and Benazepril Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 2 0093-7671 CAPSULE 40 mg ORAL ANDA 18 sections
Benazepril Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0185-0048 TABLET, FILM COATED 40 mg ORAL ANDA 17 sections
Benazepril Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0185-0053 TABLET, FILM COATED 10 mg ORAL ANDA 17 sections
Benazepril Hydrochloride and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 0185-0211 TABLET, FILM COATED 20 mg ORAL ANDA 13 sections
Benazepril Hydrochloride and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 0185-0236 TABLET, FILM COATED 5 mg ORAL ANDA 13 sections
Benazepril Hydrochloride and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 0185-0277 TABLET, FILM COATED 20 mg ORAL ANDA 13 sections
Benazepril Hydrochloride and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 0185-0325 TABLET, FILM COATED 10 mg ORAL ANDA 13 sections
Benazepril Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0185-0505 TABLET, FILM COATED 5 mg ORAL ANDA 17 sections
Benazepril Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0185-0820 TABLET, FILM COATED 20 mg ORAL ANDA 17 sections
Benazepril Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0378-0441 TABLET, FILM COATED 5 mg ORAL ANDA 17 sections
Benazepril Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0378-0443 TABLET, FILM COATED 10 mg ORAL ANDA 17 sections
Benazepril Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0378-0444 TABLET, FILM COATED 20 mg ORAL ANDA 17 sections
Benazepril Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0378-0447 TABLET, FILM COATED 40 mg ORAL ANDA 17 sections
Benazepril Hydrochloride and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 0378-4725 TABLET, FILM COATED 5 mg ORAL ANDA 13 sections
Benazepril Hydrochloride and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 0378-4735 TABLET, FILM COATED 10 mg ORAL ANDA 13 sections