Propafenone

Antiarrhythmic — CARDIOVASCULAR SYSTEM

Key facts

Propafenone is an ofp drug in the Antiarrhythmic class catalogued in DrugCentral. It was first approved by the FDA in 1989. DrugCentral lists 33 molecular targets, including ADRB2, HTR2B and ABCB1. Recorded indications include Atrial fibrillation, Life-Threatening Ventricular Tachycardia, Paroxysmal atrial fibrillation and Paroxysmal atrial flutter.

• Approval status: ofp (first approved 1989 by the FDA).
• Drug class: Antiarrhythmic.
• Molecular targets: ADRB2, HTR2B, ABCB1 and HTR2A (33 listed in DrugCentral).
• Indications: Atrial fibrillation, Life-Threatening Ventricular Tachycardia, Paroxysmal atrial fibrillation, Paroxysmal atrial flutter and Paroxysmal supraventricular tachycardia.
• ATC code: C01BC03 (Antiarrhythmics, class Ic).
• Molecular formula: C21H27NO3; molecular weight 341.45 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (5)

• Atrial fibrillation
• Life-Threatening Ventricular Tachycardia
• Paroxysmal atrial fibrillation
• Paroxysmal atrial flutter
• Paroxysmal supraventricular tachycardia

Off-label uses (1)

• Cardioversion of Atrial Fibrillation

Contraindications (22)

• Agranulocytosis
• Atrioventricular block
• Bradycardia
• Bronchospasm
• Bundle branch block
• Cardiogenic shock
• Chronic heart failure
• Congenital long QT syndrome
• Coronary arteriosclerosis
• Disease of liver
• Hyperkalemia
• Hypokalemia
• Kidney disease
• Low blood pressure
• Myasthenia gravis
• Myocardial infarction
• Myocardial infarction in recovery phase
• Prolonged QT interval
• Severe chronic obstructive pulmonary disease
• Sick sinus syndrome
• Structural disorder of heart
• Torsades de pointes

Mechanism & targets

• Established pharmacologic class: Antiarrhythmic

Molecular targets (33)

Target	Gene	Action	Activity
Beta-2 adrenergic receptor	ADRB2	antagonist	Ki 7.44
5-hydroxytryptamine receptor 2B	HTR2B	unknown	Ki 7.24
Multidrug resistance protein 1	ABCB1	unknown	ED50 7.06
5-hydroxytryptamine receptor 2A	HTR2A	unknown	Ki 6.73
5-hydroxytryptamine receptor 2C	HTR2C	unknown	Ki 6.70
Beta-1 adrenergic receptor	ADRB1	antagonist	Ki 6.69
Beta-3 adrenergic receptor	ADRB3	unknown	Ki 6.50
Potassium voltage-gated channel subfamily H member 2	KCNH2	unknown	IC50 6.10
5-hydroxytryptamine receptor 6	HTR6	unknown	Ki 6.06
5-hydroxytryptamine receptor 1A	HTR1A	unknown	Ki 6.03
Sigma non-opioid intracellular receptor 1	SIGMAR1	unknown	Ki 5.96
Alpha-1B adrenergic receptor	Adra1b	unknown	Ki 5.85
Sodium-dependent dopamine transporter	SLC6A3	unknown	Ki 5.83
5-hydroxytryptamine receptor 1A	Htr1a	unknown	IC50 5.79
Sulfonylurea receptor 2, Kir6.2	ABCC9|KCNJ11	unknown	IC50 5.66
Alpha-1D adrenergic receptor	ADRA1D	unknown	Ki 5.60
Aldehyde oxidase	AOX1	unknown	IC50 5.60
Sodium-dependent noradrenaline transporter	SLC6A2	unknown	Ki 5.52
Cytochrome P450 1A2	CYP1A2	unknown	IC50 5.48
Sodium channel protein type 5 subunit alpha	SCN5A	blocker	IC50 5.48

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
1989-11-27	FDA	—	GLAXOSMITHKLINE LLC

ATC classification

ATC code	Therapeutic hierarchy
C01BC03	CARDIOVASCULAR SYSTEM › CARDIAC THERAPY › ANTIARRHYTHMICS, CLASS I AND III › Antiarrhythmics, class Ic

Pharmacogenomics

Drug-label and guideline annotations from PharmGKB and CPIC.

• FDA label: CYP2D6 · No Clinical PGx
• HCSC label: CYP2D6 · No Clinical PGx
• Swissmedic label: CYP2D6 · Actionable PGx

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Electrocardiogram QRS complex prolonged	492.6
Drug interaction	312.3
Atrial fibrillation	306.8
Bradycardia	276.0
Toxicity to various agents	165.0
Arrhythmia	137.4
Ventricular tachycardia	122.6
Sinus bradycardia	118.9
Cardiac arrest	115.9
Completed suicide	96.0
Electrocardiogram PR prolongation	93.6
Syncope	90.1

Chemical structure

Full physicochemical, ADMET and 3D-structure analysis of Propafenone is on its molecule page.

• Molecular formula: C₂₁H₂₇NO₃
• Molecular weight: 341.45 g/mol
• CAS number: —
• InChIKey: JWHAUXFOSRPERK-UHFFFAOYSA-N
• PubChem CID: 4932

CCCNCC(O)COC1=C(C=CC=C1)C(=O)CCC1=CC=CC=C1

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Propafenone used for?

DrugCentral lists the following indications for Propafenone: Atrial fibrillation, Life-Threatening Ventricular Tachycardia, Paroxysmal atrial fibrillation, Paroxysmal atrial flutter and Paroxysmal supraventricular tachycardia.

How does Propafenone work?

Its molecular targets in DrugCentral include ADRB2 (antagonist), HTR2B, ABCB1 and HTR2A.

When was Propafenone first approved?

Propafenone was first approved by the FDA in 1989.

What drug class does Propafenone belong to?

Propafenone is in the Antiarrhythmic class.

What is the chemical formula of Propafenone?

Propafenone has the molecular formula C21H27NO3 and a molecular weight of 341.45 g/mol.

Sources

• DrugCentral drug card 2291 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1201063 — compound record and bioactivity
• PubChem CID 4932 — chemical identifiers
• DrugBank DB01182 — drug record
• FDA UNII 68IQX3T69U — substance identity
• DailyMed: FDA labels for Propafenone — current prescribing information (label search)
• UniProt P07550 (ADRB2) — target protein
• UniProt P41595 (HTR2B) — target protein
• UniProt P08183 (ABCB1) — target protein
• UniProt P28223 (HTR2A) — target protein
• UniProt P28335 (HTR2C) — target protein
• UniProt P08588 (ADRB1) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral
• PharmGKB / CPIC — pharmacogenomic label annotations

How this page is built: methodology · editorial policy & corrections.