enalaprilat 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| angiotensin-converting enzyme inhibitors | 1006 | 76420-72-9 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
The active metabolite of ENALAPRIL and one of the potent, intravenously administered, ANGIOTENSIN-CONVERTING ENZYME INHIBITORS. It is an effective agent for the treatment of essential hypertension and has beneficial hemodynamic effects in heart failure. The drug produces renal vasodilation with an increase in sodium excretion.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 3 | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 60 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 1.91 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 40 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 0.38 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 1.60 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.62 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 39 hours | Lombardo F, Berellini G, Obach RS |
| S (Water solubility) | 14 mg/mL | Bocci G, Oprea TI, Benet LZ |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Feb. 9, 1988 | FDA | BIOVAIL LABS INTL |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
| 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 |
|---|---|---|---|---|---|---|
| Angioedema | 51.24 | 45.89 | 13 | 81 | 37361 | 34919476 |
FDA Adverse Event Reporting System (Geriatric)
None
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| CHEBI has role | CHEBI:35457 | ACE inhibitor |
| CHEBI has role | CHEBI:35674 | antihypertensive drugs |
| 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 |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Hypertensive disorder | indication | 38341003 | DOID:10763 |
| Congestive heart failure | indication | 42343007 | DOID:6000 |
| Asymptomatic left ventricular systolic dysfunction | indication | 698592004 | |
| Angioedema | contraindication | 41291007 | DOID:1558 |
| Hereditary angioneurotic edema | contraindication | 82966003 | DOID:14735 |
| Idiopathic angioedema | contraindication | 402382008 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 2.12 | acidic |
| pKa2 | 3.14 | acidic |
| pKa3 | 8.3 | Basic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Angiotensin-converting enzyme | Enzyme | INHIBITOR | IC50 | 7.50 | IUPHAR | IUPHAR | |||
| Angiotensin-converting enzyme | Enzyme | Ki | 8.85 | CHEMBL | |||||
| Angiotensin-converting enzyme | Enzyme | IC50 | 9.02 | CHEMBL | |||||
| Angiotensin-converting enzyme 2 | Enzyme | Ki | 9.30 | CHEMBL | |||||
| Angiotensin-converting enzyme | Enzyme | IC50 | 7.94 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4019497 | VUID |
| N0000147617 | NUI |
| D03769 | KEGG_DRUG |
| 4019497 | VANDF |
| C0014027 | UMLSCUI |
| CHEBI:4786 | CHEBI |
| EAL | PDB_CHEM_ID |
| CHEMBL577 | ChEMBL_ID |
| CHEMBL3989406 | ChEMBL_ID |
| DB09477 | DRUGBANK_ID |
| D015773 | MESH_DESCRIPTOR_UI |
| 5462501 | PUBCHEM_CID |
| 6332 | IUPHAR_LIGAND_ID |
| 84680-54-6 | SECONDARY_CAS_RN |
| 3829 | RXNORM |
| 37933 | MMSL |
| 4657 | MMSL |
| 004369 | NDDF |
| 007388 | NDDF |
| 414092003 | SNOMEDCT_US |
| 48052001 | SNOMEDCT_US |
| GV0O7ES0R3 | UNII |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Enalaprilat | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0143-9786 | INJECTION | 2.50 mg | INTRAVENOUS | ANDA | 23 sections |
| Enalaprilat | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0143-9786 | INJECTION | 2.50 mg | INTRAVENOUS | ANDA | 23 sections |
| Enalaprilat | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0143-9787 | INJECTION | 1.25 mg | INTRAVENOUS | ANDA | 23 sections |
| Enalaprilat | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0143-9787 | INJECTION | 1.25 mg | INTRAVENOUS | ANDA | 23 sections |
| Enalaprilat | HUMAN PRESCRIPTION DRUG LABEL | 1 | 43598-078 | INJECTION | 1.25 mg | INTRAVENOUS | ANDA | 23 sections |
| Enalaprilat | HUMAN PRESCRIPTION DRUG LABEL | 1 | 43598-169 | INJECTION | 2.50 mg | INTRAVENOUS | ANDA | 23 sections |
| ENALAPRILAT | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51662-1477 | INJECTION | 1.25 mg | INTRAVENOUS | ANDA | 13 sections |