cilazapril 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| angiotensin-converting enzyme inhibitors | 641 | 88768-40-5 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
One of the ANGIOTENSIN-CONVERTING ENZYME INHIBITORS (ACE inhibitors) used for hypertension. It is a prodrug that is hydrolyzed after absorption to its main metabolite cilazaprilat.
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 2.50 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 1 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 0 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 0.34 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 60 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Approvals:
None
FDA Adverse Event Reporting System (Female)
| 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 |
|---|---|---|---|---|---|---|
| Labile hypertension | 131.08 | 35.12 | 18 | 586 | 468 | 63487950 |
| Labelled drug-drug interaction medication error | 66.55 | 35.12 | 17 | 587 | 13382 | 63475036 |
| Tinnitus | 66.35 | 35.12 | 21 | 583 | 35607 | 63452811 |
| Myalgia | 51.98 | 35.12 | 26 | 578 | 146503 | 63341915 |
| Chest pain | 42.53 | 35.12 | 26 | 578 | 215933 | 63272485 |
| Muscle spasms | 39.14 | 35.12 | 22 | 582 | 156128 | 63332290 |
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 |
|---|---|---|---|---|---|---|
| Antiacetylcholine receptor antibody positive | 62.05 | 32.66 | 8 | 674 | 57 | 34956192 |
| Pacemaker generated rhythm | 61.45 | 32.66 | 8 | 674 | 62 | 34956187 |
| Heart rate abnormal | 35.37 | 32.66 | 8 | 674 | 1823 | 34954426 |
| Heart rate increased | 33.97 | 32.66 | 17 | 665 | 46326 | 34909923 |
FDA Adverse Event Reporting System (Geriatric)
| 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 |
|---|---|---|---|---|---|---|
| Labile hypertension | 119.30 | 34.88 | 18 | 1264 | 531 | 79742575 |
| Pacemaker generated rhythm | 62.64 | 34.88 | 8 | 1274 | 65 | 79743041 |
| Antiacetylcholine receptor antibody positive | 62.22 | 34.88 | 8 | 1274 | 69 | 79743037 |
| Tinnitus | 50.92 | 34.88 | 21 | 1261 | 44312 | 79698794 |
| Labelled drug-drug interaction medication error | 45.50 | 34.88 | 17 | 1265 | 27633 | 79715473 |
| Myalgia | 35.68 | 34.88 | 27 | 1255 | 185614 | 79557492 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | C09AA08 | CARDIOVASCULAR SYSTEM AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM ACE INHIBITORS, PLAIN ACE inhibitors, plain |
| ATC | C09BA08 | 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 |
| 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 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 1.93 | acidic |
| pKa2 | 7.61 | Basic |
| pKa3 | 3.71 | 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 | 8.70 | WOMBAT-PK | SCIENTIFIC LITERATURE |
External reference:
| ID | Source |
|---|---|
| 4025239 | VUID |
| N0000171771 | NUI |
| D01069 | KEGG_DRUG |
| 152491 | RXNORM |
| 4025239 | VANDF |
| C0055723 | UMLSCUI |
| CHEBI:145568 | CHEBI |
| CHEMBL515606 | ChEMBL_ID |
| D017315 | MESH_DESCRIPTOR_UI |
| DB01340 | DRUGBANK_ID |
| 56330 | PUBCHEM_CID |
| 6459 | IUPHAR_LIGAND_ID |
| C045980 | MESH_SUPPLEMENTAL_RECORD_UI |
| 19KW7PI29F | UNII |
| DB15565 | DRUGBANK_ID |
| 003950 | NDDF |
| 1268982005 | SNOMEDCT_US |
| 318913001 | SNOMEDCT_US |
| 395947008 | SNOMEDCT_US |
| 725786001 | SNOMEDCT_US |
| C0055724 | UMLSCUI |
| CHEMBL2104578 | ChEMBL_ID |
| 5675 | INN_ID |
| 5811 | INN_ID |
| 92077-78-6 | SECONDARY_CAS_RN |
| 90139-06-3 | SECONDARY_CAS_RN |
| 64766 | PUBCHEM_CID |
| 6461 | IUPHAR_LIGAND_ID |
| WBL76FH528 | UNII |
Pharmaceutical products:
None