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

Stem definition	Drug id	CAS RN
beta-adrenoreceptor antagonists	569	56980-93-9

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: celiprolol DL-Celiprolol selectol celiprolol hydrochloride celiprolol HCl celiprolol monohydrochloride	A cardioselective beta-1 adrenergic antagonist that has intrinsic symopathomimetic activity. It is used in the management of ANGINA PECTORIS and HYPERTENSION. Molecular weight: 379.50 Formula: C20H33N3O4 CLOGP: 1.86 LIPINSKI: 0 HAC: 7 HDO: 3 TPSA: 90.90 ALOGS: -3.34 ROTB: 10

Molecule

Description

Molfile Inchi Smiles

Synonyms:

celiprolol
DL-Celiprolol
selectol
celiprolol hydrochloride
celiprolol HCl
celiprolol monohydrochloride

A cardioselective beta-1 adrenergic antagonist that has intrinsic symopathomimetic activity. It is used in the management of ANGINA PECTORIS and HYPERTENSION.

Molecular weight: 379.50
Formula: C20H33N3O4
CLOGP: 1.86
LIPINSKI: 0
HAC: 7
HDO: 3
TPSA: 90.90
ALOGS: -3.34
ROTB: 10

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)	40 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

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	55.67	39.38	14	834	7330	63480844
Prevertebral soft tissue swelling of cervical space	49.69	39.38	6	842	36	63488138
Eosinophilia	47.87	39.38	16	832	22740	63465434
Hyponatraemia	44.43	39.38	24	824	111876	63376298
Lactic acidosis	43.24	39.38	17	831	38270	63449904

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	83.92	50.88	10	458	53	34956410
Nipple disorder	71.88	50.88	10	458	200	34956263
Breast pain	52.72	50.88	10	458	1418	34955045

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	81.18	37.08	10	1453	50	79742875
Nipple disorder	68.47	37.08	10	1453	204	79742721
Acute kidney injury	53.46	37.08	56	1407	519348	79223577
Prevertebral soft tissue swelling of cervical space	47.77	37.08	6	1457	36	79742889
Pemphigoid	41.07	37.08	14	1449	15301	79727624
Hepatocellular injury	40.51	37.08	19	1444	47574	79695351
Hyponatraemia	40.07	37.08	30	1433	177818	79565107
Eosinophilia	38.27	37.08	18	1445	45327	79697598
Bradycardia	37.70	37.08	26	1437	135531	79607394

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	D018663	Adrenergic Agents
MeSH PA	D018674	Adrenergic Antagonists
MeSH PA	D058671	Adrenergic beta-1 Receptor Antagonists
MeSH PA	D000319	Adrenergic beta-Antagonists
MeSH PA	D000889	Anti-Arrhythmia Agents
MeSH PA	D000959	Antihypertensive Agents
MeSH PA	D002317	Cardiovascular Agents
MeSH PA	D018377	Neurotransmitter Agents
MeSH PA	D018373	Peripheral Nervous System Agents
MeSH PA	D013566	Sympathomimetics
MeSH PA	D014665	Vasodilator Agents

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])	Bioact source	MoA source
Beta-1 adrenergic receptor	GPCR	P08588	ADRB1_HUMAN	ANTAGONIST	Ki	8.10	WOMBAT-PK	SCIENTIFIC LITERATURE
Beta-2 adrenergic receptor	GPCR	P07550	ADRB2_HUMAN	AGONIST	Ki	6.80	WOMBAT-PK
5-hydroxytryptamine receptor 1A	GPCR		5HT1A_RAT		Ki	5.05	CHEMBL

External reference:

ID	Source
4025238	VUID
N0000171770	NUI
D01741	KEGG_DRUG
203145	RXNORM
C0055021	UMLSCUI
CHEBI:94461	CHEBI
CHEMBL27810	ChEMBL_ID
DB04846	DRUGBANK_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
CHEMBL1742424	ChEMBL_ID
4025238	VANDF

Pharmaceutical products:

None