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

Stem definition	Drug id	CAS RN
antiarrhythmics, propafenone derivatives	2291	54063-53-5

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: propafenone propafenone hydrochloride polfenon (RS)-Propafenone propafenone HCl	An antiarrhythmia agent that is particularly effective in ventricular arrhythmias. It also has weak beta-blocking activity. Molecular weight: 341.45 Formula: C21H27NO3 CLOGP: 3.64 LIPINSKI: 0 HAC: 4 HDO: 2 TPSA: 58.56 ALOGS: -4.65 ROTB: 11 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

propafenone
propafenone hydrochloride
polfenon
(RS)-Propafenone
propafenone HCl

An antiarrhythmia agent that is particularly effective in ventricular arrhythmias. It also has weak beta-blocking activity.

Molecular weight: 341.45
Formula: C21H27NO3
CLOGP: 3.64
LIPINSKI: 0
HAC: 4
HDO: 2
TPSA: 58.56
ALOGS: -4.65
ROTB: 11

Status: OFP

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

Drug dosage:

Dose	Unit	Route
0.30	g	O
0.30	g	P

ADMET properties:

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Property	Value	Reference
Vd (Volume of distribution)	2.20 L/kg	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	2.10 hours	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
CL (Clearance)	16 mL/min/kg	Lombardo F, Berellini G, Obach RS
BA (Bioavailability)	12 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
EoM (Fraction excreted unchanged in urine)	0.50 %	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	0.09 mg/mL	Benet LZ, Broccatelli F, Oprea TI
fu (Fraction unbound in plasma)	0.04 %	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
Nov. 27, 1989	FDA	GLAXOSMITHKLINE LLC

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
Atrial fibrillation	215.03	17.39	153	8218	116483	63364168
Electrocardiogram QRS complex prolonged	179.82	17.39	55	8316	5883	63474768
Drug interaction	162.11	17.39	174	8197	228957	63251694
Bradycardia	141.57	17.39	99	8272	73128	63407523
Sinus bradycardia	111.82	17.39	49	8322	14502	63466149
Arrhythmia	84.16	17.39	56	8315	38084	63442567
Completed suicide	68.52	17.39	90	8281	145583	63335068
Cardiac arrest	64.69	17.39	70	8301	92475	63388176
Toxicity to various agents	60.46	17.39	113	8258	247137	63233514
Enzyme induction	54.05	17.39	9	8362	53	63480598

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FDA Adverse Event Reporting System (Male)

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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
Electrocardiogram QRS complex prolonged	263.33	18.25	73	5219	4821	34946818
Bradycardia	135.78	18.25	103	5189	75315	34876324
Electrocardiogram PR prolongation	105.64	18.25	25	5267	870	34950769
Atrial fibrillation	91.17	18.25	102	5190	122291	34829348
Drug interaction	73.30	18.25	126	5166	225820	34725819
Palpitations	59.70	18.25	49	5243	39937	34911702
Facial asymmetry	58.87	18.25	13	5279	330	34951309
Ventricular tachycardia	56.01	18.25	40	5252	26539	34925100
Accidental exposure to product by child	40.07	18.25	13	5279	1463	34950176
Neonatal pneumonia	39.79	18.25	8	5284	127	34951512

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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
Electrocardiogram QRS complex prolonged	431.01	16.03	129	12464	10704	79721091
Bradycardia	236.46	16.03	185	12408	135372	79596423
Atrial fibrillation	218.77	16.03	208	12385	197678	79534117
Drug interaction	208.77	16.03	290	12303	414893	79316902
Sinus bradycardia	106.79	16.03	60	12533	25187	79706608
Electrocardiogram PR prolongation	99.70	16.03	27	12566	1556	79730239
Arrhythmia	92.57	16.03	77	12516	61195	79670600
Ventricular tachycardia	81.19	16.03	61	12532	41874	79689921
Completed suicide	80.13	16.03	141	12452	245626	79486169
Palpitations	79.61	16.03	99	12494	126511	79605284

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	C01BC03	CARDIOVASCULAR SYSTEM CARDIAC THERAPY ANTIARRHYTHMICS, CLASS I AND III Antiarrhythmics, class Ic
CHEBI has role	CHEBI:38070	antiarrhythmic agent
FDA EPC	N0000175426	Antiarrhythmic
MeSH PA	D000889	Anti-Arrhythmia Agents
MeSH PA	D002317	Cardiovascular Agents
MeSH PA	D049990	Membrane Transport Modulators
MeSH PA	D026941	Sodium Channel Blockers
MeSH PA	D061567	Voltage-Gated Sodium Channel Blockers

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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
Atrial fibrillation	indication	49436004	DOID:0060224
Paroxysmal supraventricular tachycardia	indication	67198005
Paroxysmal atrial fibrillation	indication	282825002
Paroxysmal atrial flutter	indication	427665004
Life-Threatening Ventricular Tachycardia	indication
Cardioversion of Atrial Fibrillation	off-label use
Bronchospasm	contraindication	4386001
Bundle branch block	contraindication	6374002
Hyperkalemia	contraindication	14140009
Agranulocytosis	contraindication	17182001	DOID:12987

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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	9.15	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
Sodium channel protein type 5 subunit alpha	Ion channel	Q14524	SCN5A_HUMAN	BLOCKER	IC50	5.48	CHEMBL	CHEMBL
Beta-1 adrenergic receptor	GPCR	P08588	ADRB1_HUMAN	ANTAGONIST	Ki	6.69	DRUG MATRIX	CHEMBL
Sodium channel subunit beta-1	Ion channel	Q07699	SCN1B_HUMAN				WOMBAT-PK
Sodium channel subunit beta-2	Ion channel	O60939	SCN2B_HUMAN				WOMBAT-PK
Sodium channel subunit beta-3	Ion channel	Q9NY72	SCN3B_HUMAN				WOMBAT-PK
Sodium channel subunit beta-4	Ion channel	Q8IWT1	SCN4B_HUMAN				WOMBAT-PK
Sigma non-opioid intracellular receptor 1	Membrane receptor	Q99720	SGMR1_HUMAN		Ki	5.96	DRUG MATRIX
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		IC50	6.10	WOMBAT-PK
Multidrug resistance protein 1	Transporter	P08183	MDR1_HUMAN		ED50	7.06	WOMBAT-PK
Sodium-dependent noradrenaline transporter	Transporter	P23975	SC6A2_HUMAN		Ki	5.52	DRUG MATRIX

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External reference:

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ID	Source
003525	NDDF
004487	NDDF
108501006	SNOMEDCT_US
203135	RXNORM
2561	IUPHAR_LIGAND_ID
3312	INN_ID
34183-22-7	SECONDARY_CAS_RN
372910007	SNOMEDCT_US
4019487	VANDF
4019911	VUID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Propafenone	HUMAN PRESCRIPTION DRUG LABEL	1	21695-814	CAPSULE, EXTENDED RELEASE	325 mg	ORAL	ANDA	21 sections
Propafenone HCl	HUMAN PRESCRIPTION DRUG LABEL	1	0591-0582	TABLET, FILM COATED	150 mg	ORAL	ANDA	29 sections
Propafenone HCl	HUMAN PRESCRIPTION DRUG LABEL	1	0591-0583	TABLET, FILM COATED	225 mg	ORAL	ANDA	29 sections
Propafenone Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0591-2285	CAPSULE, EXTENDED RELEASE	225 mg	ORAL	ANDA	29 sections
Propafenone Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0591-2286	CAPSULE, EXTENDED RELEASE	325 mg	ORAL	ANDA	29 sections
Propafenone Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0591-2287	CAPSULE, EXTENDED RELEASE	425 mg	ORAL	ANDA	29 sections
Propafenone Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0603-5448	TABLET, FILM COATED	150 mg	ORAL	ANDA	29 sections
Propafenone Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0603-5448	TABLET, FILM COATED	150 mg	ORAL	ANDA	29 sections
Propafenone Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0603-5449	TABLET, FILM COATED	225 mg	ORAL	ANDA	29 sections
Propafenone Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0603-5449	TABLET, FILM COATED	225 mg	ORAL	ANDA	29 sections

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