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

Stem definition	Drug id	CAS RN
beta-adrenoreceptor antagonists	2176	13523-86-9

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: pindolol betapindol pinbetol prinodolol dl-Pindolol durapindol LB-46	A moderately lipophilic beta blocker (ADRENERGIC BETA-ANTAGONISTS). It is non-cardioselective and has intrinsic sympathomimetic actions, but little membrane-stabilizing activity. (From Martindale, The Extra Pharmocopoeia, 30th ed, p638) Molecular weight: 248.33 Formula: C14H20N2O2 CLOGP: 1.67 LIPINSKI: 0 HAC: 4 HDO: 3 TPSA: 57.28 ALOGS: -2.46 ROTB: 6 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

pindolol
betapindol
pinbetol
prinodolol
dl-Pindolol
durapindol
LB-46

A moderately lipophilic beta blocker (ADRENERGIC BETA-ANTAGONISTS). It is non-cardioselective and has intrinsic sympathomimetic actions, but little membrane-stabilizing activity. (From Martindale, The Extra Pharmocopoeia, 30th ed, p638)

Molecular weight: 248.33
Formula: C14H20N2O2
CLOGP: 1.67
LIPINSKI: 0
HAC: 4
HDO: 3
TPSA: 57.28
ALOGS: -2.46
ROTB: 6

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
15	mg	O
15	mg	P

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	88 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
CL (Clearance)	7.70 mL/min/kg	Lombardo F, Berellini G, Obach RS
EoM (Fraction excreted unchanged in urine)	54 %	Hosey CM, Chan R, Benet LZ
MRTD (Maximum Recommended Therapeutic Daily Dose)	4.03 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
t_half (Half-life)	2.20 hours	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	1.20 L/kg	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Hosey CM, Chan R, Benet LZ
S (Water solubility)	0.86 mg/mL	Bocci G, Oprea TI, Benet LZ
fu (Fraction unbound in plasma)	0.58 %	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
Sept. 3, 1982	FDA

FDA Adverse Event Reporting System (Female)

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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
Atrioventricular block complete	112.42	36.50	24	618	8227	63480153
Oesophagitis	63.59	36.50	17	625	14991	63473389
Neutrophil count abnormal	54.35	36.50	11	631	2881	63485499
Rhabdomyolysis	53.07	36.50	19	623	43932	63444448
White blood cell count abnormal	51.15	36.50	12	630	6230	63482150
Urinary tract infection	48.25	36.50	31	611	264653	63223727
Haemoglobin abnormal	48.16	36.50	11	631	5077	63483303
Hypertension	44.30	36.50	30	612	279273	63209107
Drug interaction	37.19	36.50	25	617	229106	63259274

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FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

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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
Atrioventricular block complete	98.53	27.36	24	691	16586	79727087
Hypertension	40.56	27.36	29	686	330963	79412710
Rhabdomyolysis	39.59	27.36	19	696	103112	79640561
Chromaturia	31.82	27.36	11	704	25735	79717938

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	C07AA03	CARDIOVASCULAR SYSTEM BETA BLOCKING AGENTS BETA BLOCKING AGENTS Beta blocking agents, non-selective
ATC	C07CA03	CARDIOVASCULAR SYSTEM BETA BLOCKING AGENTS BETA BLOCKING AGENTS AND OTHER DIURETICS Beta blocking agents, non-selective, and other diuretics
CHEBI has role	CHEBI:35530	beta-adrenergic blockers
CHEBI has role	CHEBI:35620	vasodilator agents
CHEBI has role	CHEBI:35674	antihypertensive drugs
CHEBI has role	CHEBI:39456	antiglaucoma agent
CHEBI has role	CHEBI:48279	serotonin antagonists
FDA EPC	N0000175556	beta-Adrenergic Blocker
FDA MoA	N0000000161	Adrenergic beta-Antagonists
MeSH PA	D018663	Adrenergic Agents

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Drug Use | Suggest Off label Use Form| |View source of the data|

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Disease	Relation	SNOMED_ID	DOID
Hypertensive disorder	indication	38341003	DOID:10763
Angina pectoris	off-label use	194828000
Bronchospasm	contraindication	4386001
Complete atrioventricular block	contraindication	27885002
Depressive disorder	contraindication	35489007
Anaphylaxis	contraindication	39579001
Sinus bradycardia	contraindication	49710005
Diabetes mellitus	contraindication	73211009	DOID:9351
Pulmonary emphysema	contraindication	87433001
Cardiogenic shock	contraindication	89138009

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	13.41	acidic
pKa2	9.19	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Beta-1 adrenergic receptor	GPCR	P08588	ADRB1_HUMAN	PARTIAL AGONIST	Ki	9.40	WOMBAT-PK	CHEMBL
Beta-2 adrenergic receptor	GPCR	P07550	ADRB2_HUMAN	PARTIAL AGONIST	Ki	9	WOMBAT-PK	CHEMBL
5-hydroxytryptamine receptor 1A	GPCR	P08908	5HT1A_HUMAN		Ki	8.10	WOMBAT-PK
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN	AGONIST	Ki	5	IUPHAR
5-hydroxytryptamine receptor 2B	GPCR	P41595	5HT2B_HUMAN	AGONIST	Ki	5.70	IUPHAR
5-hydroxytryptamine receptor 2C	GPCR	P28335	5HT2C_HUMAN		Ki	4.27	CHEMBL
Beta-3 adrenergic receptor	GPCR	P13945	ADRB3_HUMAN		Kd	6.78	CHEMBL
5-hydroxytryptamine receptor 1B	GPCR	P28222	5HT1B_HUMAN		Ki	7.10	WOMBAT-PK
5-hydroxytryptamine receptor 1D	GPCR	P28221	5HT1D_HUMAN		Ki	5.21	PDSP
5-hydroxytryptamine receptor 1B	GPCR		5HT1B_RAT		Ki	7.10	CHEMBL

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External reference:

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ID	Source
001857	NDDF
1482	MMSL
18381001	SNOMEDCT_US
2698	INN_ID
387102009	SNOMEDCT_US
4018760	VUID
4018760	VANDF
4828	PUBCHEM_CID
5302	MMSL
8332	RXNORM

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Pindolol	HUMAN PRESCRIPTION DRUG LABEL	1	0378-0052	TABLET	5 mg	ORAL	ANDA	21 sections
Pindolol	HUMAN PRESCRIPTION DRUG LABEL	1	0378-0052	TABLET	5 mg	ORAL	ANDA	21 sections
Pindolol	HUMAN PRESCRIPTION DRUG LABEL	1	0378-0127	TABLET	10 mg	ORAL	ANDA	21 sections
Pindolol	HUMAN PRESCRIPTION DRUG LABEL	1	0378-0127	TABLET	10 mg	ORAL	ANDA	21 sections
Pindolol	HUMAN PRESCRIPTION DRUG LABEL	1	10135-743	TABLET	5 mg	ORAL	ANDA	19 sections
Pindolol	HUMAN PRESCRIPTION DRUG LABEL	1	10135-743	TABLET	5 mg	ORAL	ANDA	19 sections
Pindolol	HUMAN PRESCRIPTION DRUG LABEL	1	10135-744	TABLET	10 mg	ORAL	ANDA	19 sections
Pindolol	HUMAN PRESCRIPTION DRUG LABEL	1	10135-744	TABLET	10 mg	ORAL	ANDA	19 sections
Pindolol	HUMAN PRESCRIPTION DRUG LABEL	1	29033-028	TABLET	5 mg	ORAL	ANDA	14 sections
Pindolol	HUMAN PRESCRIPTION DRUG LABEL	1	29033-029	TABLET	10 mg	ORAL	ANDA	14 sections

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