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celiprolol 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| beta-adrenoreceptor antagonists | 569 | 56980-93-9 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A cardioselective beta-1 adrenergic antagonist that has intrinsic symopathomimetic activity. It is used in the management of ANGINA PECTORIS and HYPERTENSION.
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.20 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 3 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 151 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 20 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 22.59 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 50 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | -0.062 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 31.550 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 0.579 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 1.432 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 80.800 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 74.210 | % | High | 1 |
| herg | hERG pIC50 | 4.334 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 1.050 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 2.871 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 79.740 | % | High | 1 |
| kinase-safety-class | ACVR2A,ACVR2B,ACVRL1,AKT1,AKT2,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,DDR1,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,GSK3B,IGF1R,IKBKB,ITK,JAK1,JAK2,JAK3,MAP2K6,MAP3K21,MAP3K7,MAPK12,MAPK7,MAPK9,MAPKAPK2,MET,MTOR,NTRK2,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PLK1,PLK2,PLK3,PLK4,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK,ZAP70 | 58 | |||
| kinase-selectivity-class | AXL,BRAF,GRK2,PDK4,STK33,TEK | 6 | |||
| mdck-mdr1-bcrp-efflux | MDCK-MDR1-BCRP efflux ratio | 4.276 | High | 1 | |
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 5.058 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 4.018 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 77.130 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 6.039 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 88.190 | % | High | 1 |
| rat-kpuu-brain | Rat brain Kpuu | 0.005 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 1.524 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 84.720 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 81.330 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 937.562 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 1, 1982 | YEAR INTRODUCED |
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 |
|---|---|---|---|---|---|---|
| Pemphigoid | 60.87 | 42.41 | 15 | 956 | 9011 | 90618465 |
| Acute kidney injury | 52.59 | 42.41 | 36 | 935 | 320351 | 90307125 |
| Prevertebral soft tissue swelling of cervical space | 51.01 | 42.41 | 6 | 965 | 36 | 90627440 |
| Bradycardia | 49.49 | 42.41 | 22 | 949 | 83825 | 90543651 |
| Hyponatraemia | 48.24 | 42.41 | 25 | 946 | 133513 | 90493963 |
| Eosinophilia | 47.76 | 42.41 | 16 | 955 | 28517 | 90598959 |
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 |
|---|---|---|---|---|---|---|
| Nipple inflammation | 83.91 | 53.89 | 10 | 560 | 53 | 42620712 |
| Nipple disorder | 71.13 | 53.89 | 10 | 560 | 216 | 42620549 |
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 |
|---|---|---|---|---|---|---|
| Nipple inflammation | 82.94 | 34.51 | 10 | 1690 | 50 | 110587549 |
| Acute kidney injury | 70.81 | 34.51 | 66 | 1634 | 635364 | 109952235 |
| Bradycardia | 69.88 | 34.51 | 38 | 1662 | 155479 | 110432120 |
| Nipple disorder | 64.15 | 34.51 | 10 | 1690 | 383 | 110587216 |
| Interstitial lung disease | 48.92 | 34.51 | 29 | 1671 | 139305 | 110448294 |
| Prevertebral soft tissue swelling of cervical space | 48.83 | 34.51 | 6 | 1694 | 36 | 110587563 |
| Pemphigoid | 43.90 | 34.51 | 15 | 1685 | 19692 | 110567907 |
| Hepatocellular injury | 42.58 | 34.51 | 19 | 1681 | 50623 | 110536976 |
| Hyponatraemia | 41.59 | 34.51 | 31 | 1669 | 217622 | 110369977 |
| Eosinophilia | 37.09 | 34.51 | 18 | 1682 | 57918 | 110529681 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | C07AB08 | CARDIOVASCULAR SYSTEM BETA BLOCKING AGENTS BETA BLOCKING AGENTS Beta blocking agents, selective |
| MeSH PA | D000319 | Adrenergic beta-Antagonists |
| MeSH PA | D000889 | Anti-Arrhythmia Agents |
| MeSH PA | D000959 | Antihypertensive Agents |
| MeSH PA | D002317 | Cardiovascular Agents |
| MeSH PA | D013566 | Sympathomimetics |
| MeSH PA | D014665 | Vasodilator Agents |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018663 | Adrenergic Agents |
| MeSH PA | D018674 | Adrenergic Antagonists |
| MeSH PA | D058671 | Adrenergic beta-1 Receptor Antagonists |
| CHEBI has role | CHEBI:35554 | cardiovascular drug |
Related Drugs by ATC class:
C07AB Beta blocking agents, selective 13 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Hypertensive disorder | indication | 38341003 | DOID:10763 |
| Angina pectoris | indication | 194828000 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 13.38 | acidic |
| pKa2 | 9.31 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Beta-1 adrenergic receptor | GPCR | ANTAGONIST | Ki | 8.10 | WOMBAT-PK | SCIENTIFIC LITERATURE | |||
| Beta-2 adrenergic receptor | GPCR | AGONIST | Ki | 6.80 | WOMBAT-PK | ||||
| 5-hydroxytryptamine receptor 1A | GPCR | Ki | 5.05 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4025238 | VUID |
| N0000171770 | NUI |
| D01741 | KEGG_DRUG |
| 203145 | RXNORM |
| C0055021 | UMLSCUI |
| CHEBI:748072 | CHEBI |
| CHEMBL27810 | ChEMBL_ID |
| DB04846 | DRUGBANK_ID |
| CHEMBL1742424 | ChEMBL_ID |
| D017272 | MESH_DESCRIPTOR_UI |
| 2663 | PUBCHEM_CID |
| 9064 | IUPHAR_LIGAND_ID |
| 3979 | INN_ID |
| 57470-78-7 | SECONDARY_CAS_RN |
| DRB57K47QC | UNII |
| 003948 | NDDF |
| 003949 | NDDF |
| 349901006 | SNOMEDCT_US |
| 395874008 | SNOMEDCT_US |
| 395960002 | SNOMEDCT_US |
| 4025238 | VANDF |
| DRB57K47QC | INXIGHT DRUGS |
Pharmaceutical products:
None