OralTherapeutic flag

Propafenone

CAS 54063-53-5

Propafenone (CAS 54063-53-5) is a Phase 4 pharmaceutical compound with 32 bioactivity targets and 107 adverse event associations.

SOURCE NLM DailyMed

Label records

SOURCE EMBL-EBI ChEMBL

Bioactivity

SOURCE DrugCentral

Adverse signals

107

SOURCE IUPHAR/BPS

PubMed IDs

SOURCE EMBL-EBI ChEMBL B25820EEF0F0

Compound Identity

Matched identifiers and naming fields for the pharmaceutical compound record.

Primary Name

Propafenone

CAS Number

54063-53-5

UNII

68IQX3T69U

InChIKey

JWHAUXFOSRPERK-UHFFFAOYSA-N

ChEMBL ID

CHEMBL631

Molecule Type

Small molecule

Source Match

EMBL-EBI ChEMBL (INCHIKEY)

Synonyms and normalized names

PROPAFENONE HYDROCHLORIDERythmol

black box warningnatural productoraltherapeutic flag

SOURCE EMBL-EBI ChEMBL B25820EEF0F0

Clinical Development Phase

Highest clinical development phase rendered from the matched compound identifier rows.

Phase 4 (Approved)

Approved or marketed human pharmaceutical use is represented in the source phase field.

ChEMBL CHEMBL631 | Small molecule

SOURCE EMBL-EBI ChEMBL 38 bioactivity rows

Bioactivity & Target Interactions

Target-level activity records with assay counts, activity type, and measured value where present.

Target	Activity	Value	Assays	Organism
-	AC50	24288.365060240965 nM	83	-
-	IC50	11548.745272727272 nM	54	-
-	Potency	11391.49705882353 nM	23	-
-	Ki	1179.4117647058824 nM	17	-
-	EC50	5315.8730000000005 nM	10	-
Beta-1 adrenergic receptor GPCR	Ki	6.688	-	Homo sapiens
Beta-2 adrenergic receptor GPCR	Ki	7.444	-	Homo sapiens
Sodium channel protein type 5 subunit alpha Ion channel	IC50	5.48	-	Homo sapiens
Sodium channel subunit beta-1 Ion channel	-	-	-	Homo sapiens
Sodium channel subunit beta-2 Ion channel	-	-	-	Homo sapiens
Sodium channel subunit beta-3 Ion channel	-	-	-	Homo sapiens
Sodium channel subunit beta-4 Ion channel	-	-	-	Homo sapiens
Sigma non-opioid intracellular receptor 1 Membrane receptor	Ki	5.96	-	Homo sapiens
Potassium voltage-gated channel subfamily H member 2 Ion channel	IC50	6.097	-	Homo sapiens
Multidrug resistance protein 1 Transporter	ED50	7.056	-	Homo sapiens
Sodium-dependent noradrenaline transporter Transporter	Ki	5.524	-	Homo sapiens
5-hydroxytryptamine receptor 1A GPCR	Ki	6.029	-	Homo sapiens
5-hydroxytryptamine receptor 2A GPCR	Ki	6.728	-	Homo sapiens
5-hydroxytryptamine receptor 2B GPCR	Ki	7.237	-	Homo sapiens
5-hydroxytryptamine receptor 2C GPCR	Ki	6.697	-	Homo sapiens
5-hydroxytryptamine receptor 6 GPCR	Ki	6.063	-	Homo sapiens
Aldehyde oxidase Enzyme	IC50	5.602	-	Homo sapiens
Beta-3 adrenergic receptor GPCR	Ki	6.498	-	Homo sapiens
Sodium-dependent dopamine transporter Transporter	Ki	5.829	-	Homo sapiens
Cytochrome P450 2D6 Enzyme	IC50	5.337	-	Homo sapiens
Alpha-1D adrenergic receptor GPCR	Ki	5.604	-	Homo sapiens
Cytochrome P450 1A2 Enzyme	IC50	5.483	-	Homo sapiens
Potassium channel subfamily K member 2 Ion channel	IC50	5.12	-	Homo sapiens
Potassium voltage-gated channel subfamily A member 5 Ion channel	IC50	4.4	-	Homo sapiens
Potassium channel subfamily K member 3 Ion channel	IC50	5.29	-	Homo sapiens
Solute carrier family 22 member 1 Transporter	IC50	4.95	-	Homo sapiens
Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4 Ion channel	IC50	4.845	-	Homo sapiens
Alpha-1B adrenergic receptor GPCR	Ki	5.849	-	Rattus norvegicus
Alpha-1A adrenergic receptor GPCR	IC50	5.21	-	Rattus norvegicus
5-hydroxytryptamine receptor 1A GPCR	IC50	5.79	-	Rattus norvegicus
Solute carrier family 22 member 2 Transporter	IC50	4.602	-	Homo sapiens
Sulfonylurea receptor 2, Kir6.2 Ion channel	IC50	5.66	-	Homo sapiens
Nuclear receptor subfamily 2 group E member 1 Nuclear hormone receptor	EC50	4.33	-	Homo sapiens

SOURCE DrugCentral 80 associations

Adverse Event Associations

DrugCentral / FAERS disproportionality signal rows matched to this compound.

Reaction PT	Drug AE	LLR	MedDRA
Electrocardiogram QRS complex prolonged	149	513.414	10014380
Atrial fibrillation	270	307.9	10003658
Bradycardia	215	288.633	10006093
Drug interaction	323	236.891	10013710
Arrhythmia	106	138.542	10003119
Toxicity to various agents	245	128.036	10070863
Sinus bradycardia	69	127.798	10040741
Cardiac arrest	145	118.106	10007515
Ventricular tachycardia	75	108.264	10047302
Electrocardiogram PR prolongation	29	106.795	10053657
Syncope	136	91.301	10042772
Palpitations	115	91.031	10033557
Completed suicide	146	91.014	10010144
Atrial flutter	52	87.135	10003662
Hypotension	209	77.549	10021097
Atrioventricular block first degree	36	69.006	10003674
Intentional overdose	89	68.528	10022523
Dizziness	236	65.891	10013573
Nodal arrhythmia	20	61.639	10029458
Generalised tonic-clonic seizure	55	60.972	10018100
Loss of consciousness	106	56.816	10024855
Electrocardiogram QT prolonged	73	54.237	10014387
Asthenia	212	51.585	10003549
Enzyme induction	10	50.858	10048652
Presyncope	50	50.276	10036653
Brugada syndrome	15	49.914	10059027
Heart rate irregular	44	47.207	10019304
Ventricular arrhythmia	25	46.717	10047281
Facial asymmetry	14	45.193	10068737
Bundle branch block right	26	43.687	10006582
International normalised ratio increased	61	41.856	10022595
Retro-orbital neoplasm	8	41.453	10038956
Electrocardiogram abnormal	29	41.34	10014363
Pain	55	39.769	10033371
Supraventricular tachycardia	32	39.313	10042604
Atrioventricular block	26	37.65	10003671
Neonatal pneumonia	9	37.537	10053584
Conduction disorder	16	37.03	10010276
Rheumatoid arthritis	3	36.929	10039073
Cardiogenic shock	39	35.342	10007625
Suicide attempt	59	35.297	10042464
Bradyarrhythmia	16	35.174	10049765
Haematuria	53	34.916	10018867
Drug level increased	39	34.728	10013722
Neonatal hypotension	9	34.308	10049223
Atrioventricular block complete	25	33.031	10003673
Sinus arrest	14	30.619	10040738
Accidental exposure to product by child	13	30.221	10073318
Bundle branch block left	21	30.196	10006580
Off label use	95	29.723	10053762

Association rows are source-linked signal records, not incidence rates or clinical causality claims.

SOURCE IUPHAR/BPS 3 interactions

IUPHAR Ligand-Target Data

Curated ligand-target interaction rows with action, affinity, and literature identifiers.

Target	Action	Affinity	PubMed
β 1 -adrenoceptor ADRB1	Antagonist	6.699999809265137 pKi	-
K v 1.5 KCNA5	Channel blocker	4.400000095367432 pIC50	9846634
β 2 -adrenoceptor ADRB2	Antagonist	7.440000057220459 pKi	-

SOURCE PharmGKB 8 phenotype rows

Pharmacogenomics

Drug-gene phenotype annotations and evidence levels from PharmGKB-mapped rows.

CYP2D6 (PA128) CYP2D6*1, CYP2D6*10

CYP2D6 *10/*10 is associated with increased response to propafenone in people with Arrhythmias, Cardiac as compared to CYP2D6 *1/*1.

Evidence: -; PMID 12421483

CYP2D6 (PA128) CYP2D6*1, CYP2D6*10

CYP2D6 *10/*10 is associated with increased concentrations of propafenone in people with Arrhythmias, Cardiac as compared to CYP2D6 *1/*1.

Evidence: -; PMID 12421483

CYP2D6 (PA128) CYP2D6*1, CYP2D6*2, CYP2D6*5, CYP2D6*10, CYP2D6*36

CYP2D6 *1/*5 + *2/*36 + *5/*10 + *5/*5 (assigned as poor metabolizers phenotype) is associated with increased concentrations of propafenone in people with Tachycardia as compared to CYP2D6 *1/*1 + *1/*2 + *2/*2 + *1/*10 + *2/*10 + *10/*10 (assigned as intermediate metabolizer and normal metabolizer phenotype) .

Evidence: -; PMID 33203295

CYP2D6 (PA128) CYP2D6*1, CYP2D6*10

CYP2D6 *10/*10 is associated with decreased metabolism, elevated plasma concentration and better efficacy of propafenone in Chinese patients with ventricular arrhythmia when treated with propafenone in people with Arrhythmias, Cardiac as compared to CYP2D6 *1/*1.

Evidence: -; PMID 12421483

CYP2D6 (PA128) CYP2D6*1, CYP2D6*10

CYP2D6 *10/*10 is associated with decreased metabolism of propafenone in healthy individuals as compared to CYP2D6 *1/*10 + *1/*1.

Evidence: -; PMID 14653957

SCN5A (PA304) rs41261344

Allele T is associated with increased likelihood of Brugada syndrome when treated with propafenone in men with Atrial Fibrillation as compared to allele C.

Evidence: -; PMID 30984031

CYP2D6 CYP2D6*1, CYP2D6*2, CYP2D6*5, CYP2D6*10, CYP2D6*36

Cardiac rhythm disease;Tachycardia

Evidence: 1A; PMID 3

CYP2D6 CYP2D6*1, CYP2D6*10

Cardiac rhythm disease

Evidence: 3; PMID 1

SOURCE NLM RxNorm 5 name rows

Drug Names / RxNorm

Normalized drug-name vocabulary rows, RxCUIs, and source abbreviations.

Name	RxCUI	Type	Source
PROPAFENONE	8754	SU	MTHSPL
PROPAFENONE HYDROCHLORIDE	203135	SU	MTHSPL
propafenone	8754	IN	RXNORM
Rythmol	82079	BN	RXNORM
propafenone hydrochloride	203135	PIN	RXNORM

SOURCE SIDER 80 side-effect rows

Side Effects

SIDER side-effect terms mapped to the drug or same-CAS compound identity.

Side Effect	Drug Name	MedDRA Type	Concept ID
Abdominal distension	propafenone	LLT	C0000731
Abdominal distension	propafenone	PT	C0000731
Abdominal pain	propafenone	LLT	C0000737
Abdominal pain	propafenone	PT	C0000737
Abnormal dreams	propafenone	LLT	C0234458
Abnormal dreams	propafenone	PT	C0234458
Abnormal vision	propafenone	LLT	C3665386
Agranulocytosis	propafenone	LLT	C0001824
Agranulocytosis	propafenone	PT	C0001824
Alanine aminotransferase increased	propafenone	LLT	C0151905
Alanine aminotransferase increased	propafenone	PT	C0151905
Alopecia	propafenone	LLT	C0002170
Alopecia	propafenone	PT	C0002170
Amnesia	propafenone	LLT	C0002622
Amnesia	propafenone	PT	C0002622
Amnesia	propafenone	PT	C0002622
Anaemia	propafenone	LLT	C0002871
Anaemia	propafenone	PT	C0002871
Angina pectoris	propafenone	LLT	C0002962
Angina pectoris	propafenone	PT	C0002962
Angina pectoris	propafenone	PT	C0002962
Angina unstable	propafenone	LLT	C0002965
Angina unstable	propafenone	PT	C0002965
Angiopathy	propafenone	LLT	C0042373
Angiopathy	propafenone	PT	C0042373
Anorexia	propafenone	LLT	C0003123
Antinuclear antibody positive	propafenone	LLT	C0151480
Antinuclear antibody positive	propafenone	PT	C0151480
Anxiety	propafenone	LLT	C0003467
Anxiety	propafenone	PT	C0003467
Apnoea	propafenone	LLT	C0003578
Apnoea	propafenone	PT	C0003578
Arrhythmia	propafenone	LLT	C0003811
Arrhythmia	propafenone	PT	C0003811
Arrhythmia	propafenone	PT	C0003811
Arrhythmia supraventricular	propafenone	PT	C0428974
Arthritis	propafenone	LLT	C0003864
Arthritis	propafenone	PT	C0003864
Arthropathy	propafenone	LLT	C0022408
Arthropathy	propafenone	PT	C0022408
Aspartate aminotransferase increased	propafenone	LLT	C0151904
Aspartate aminotransferase increased	propafenone	PT	C0151904
Asthenia	propafenone	LLT	C0004093
Asthenia	propafenone	PT	C0004093
Asthenia	propafenone	PT	C0004093
Ataxia	propafenone	LLT	C0004134
Ataxia	propafenone	PT	C0004134
Atelectasis	propafenone	LLT	C0004144
Atelectasis	propafenone	PT	C0004144
Atrial arrhythmia	propafenone	LLT	C0085611
Atrial fibrillation	propafenone	LLT	C0004238
Atrial fibrillation	propafenone	PT	C0004238
Atrial fibrillation	propafenone	PT	C0004238
Atrial flutter	propafenone	LLT	C0004239
Atrial flutter	propafenone	PT	C0004239
Atrial hypertrophy	propafenone	LLT	C0340278
Atrial hypertrophy	propafenone	PT	C0340278
Atrioventricular block	propafenone	LLT	C0004245
Atrioventricular block	propafenone	PT	C0004245
Atrioventricular block	propafenone	PT	C0004245
Atrioventricular block first degree	propafenone	LLT	C0085614
Atrioventricular block first degree	propafenone	PT	C0085614
Atrioventricular block second degree	propafenone	LLT	C0264906
Atrioventricular block second degree	propafenone	PT	C0264906
Atrioventricular dissociation	propafenone	LLT	C0004331
Atrioventricular dissociation	propafenone	PT	C0004331
Bleeding time prolonged	propafenone	LLT	C0151529
Bleeding time prolonged	propafenone	PT	C0151529
Blister	propafenone	LLT	C0005758
Blister	propafenone	PT	C0005758
Block heart	propafenone	LLT	C0018794
Blood alkaline phosphatase increased	propafenone	LLT	C0852911
Blood alkaline phosphatase increased	propafenone	PT	C0852911
Blood and lymphatic system disorders	propafenone	-	C0851353
Blood bilirubin increased	propafenone	LLT	C0311468
Blood bilirubin increased	propafenone	PT	C0311468
Blood creatinine increased	propafenone	LLT	C0235431
Blood creatinine increased	propafenone	PT	C0235431
Blood disorder	propafenone	LLT	C0018939
Blood disorder	propafenone	PT	C0018939

SOURCE Rendered pharma page rows FAQPage JSON-LD

Frequently Asked Questions

Short answers generated only from the same visible source-linked rows on this page.

What is Propafenone used for in pharmaceutical contexts?

Propafenone (CAS 54063-53-5) is rendered as a pharmaceutical compound from the matched source rows; no DailyMed product-name rows are present in this page query.

What are the known adverse events for Propafenone?

Propafenone has 107 DrugCentral/FAERS adverse event associations. Rendered reaction terms include Electrocardiogram QRS complex prolonged, Atrial fibrillation, Bradycardia, Drug interaction, Arrhythmia. Signal rows are source-linked records and should not be read as incidence rates or causality conclusions.

Is Propafenone also used in cosmetics?

No same-CAS cosmetics profile is rendered from the ingredients-table cross-reference for Propafenone.

What clinical phase is Propafenone in?

Propafenone is rendered with ChEMBL max phase 4 (approved).

What bioactivity targets are documented for Propafenone?

Propafenone has 38 bioactivity rows in this page query. Rendered target entries include Beta-1 adrenergic receptor, Beta-2 adrenergic receptor, Sodium channel protein type 5 subunit alpha, Sodium channel subunit beta-1, Sodium channel subunit beta-2.