PROPAFENONE HYDROCHLORIDE

First approved in 1989

Details

Stereochemistry	RACEMIC
Molecular Formula	C21H27NO3.ClH
Molecular Weight	377.905
Optical Activity	( + / - )
Defined Stereocenters	0 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

Cl.CCCNCC(O)COC1=CC=CC=C1C(=O)CCC2=CC=CC=C2

InChI

InChIKey=XWIHRGFIPXWGEF-UHFFFAOYSA-N

InChI=1S/C21H27NO3.ClH/c1-2-14-22-15-18(23)16-25-21-11-7-6-10-19(21)20(24)13-12-17-8-4-3-5-9-17;/h3-11,18,22-23H,2,12-16H2,1H3;1H

HIDE SMILES / InChI

Molecular Formula	C21H27NO3
Molecular Weight	341.444
Charge	0
Count

Stereochemistry	RACEMIC
Additional Stereochemistry	No
Defined Stereocenters	0 / 1
E/Z Centers	0
Optical Activity	( + / - )

Molecular Formula	ClH
Molecular Weight	36.461
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/019151s012lbl.pdf
Curator's Comment: description was created based on several sources, including https://www.drugbank.ca/drugs/DB01182 | http://reference.medscape.com/drug/rythmol-propafenone-342307 | https://www.drugs.com/pro/propafenone.html | https://www.ncbi.nlm.nih.gov/pubmed/26588045

Propafenone (brand name Rythmol SR or Rytmonorm) is a class 1C anti-arrhythmic medication, which treats illnesses associated with rapid heartbeats such as atrial and ventricular arrhythmias. The electrophysiological effect of propafenone manifests itself in a reduction of upstroke velocity (Phase 0) of the monophasic action potential. In Purkinje fibers, and to a lesser extent myocardial fibers, propafenone reduces the fast inward current carried by sodium ions, which is responsible for the drugs antiarrhythmic actions. Diastolic excitability threshold is increased and effective refractory period prolonged. Propafenone reduces spontaneous automaticity and depresses triggered activity. At very high concentrations in vitro, propafenone can inhibit the slow inward current carried by calcium but this calcium antagonist effect probably does not contribute to antiarrhythmic efficacy. Propafenone is metabolized primarily in the liver. Because of its short half-life, it requires dosing two or three times daily to maintain steady blood levels. The long-term safety of propafenone is unknown. Because it is structurally similar to another anti-arrhythmic medicine, flecainide, similar cautions should be exercised in its use. Flecainide and propafenone, like other antiarrhythmic drugs, have been shown to increase the occurrence of arrhythmias (5.3% for propafenone, Teva physician prescribing information), primarily in patients with underlying heart disease. However, their use in structurally normal hearts is considered safe.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
Potassium channel subfamily K member 2 6 Target ID: CHEMBL2321615 Sources: https://www.ncbi.nlm.nih.gov/pubmed/26588045	Inhibitor 8504	7.6 nM [IC50]
Potassium channel subfamily K member 3 10 Target ID: CHEMBL2321613 Sources: https://www.ncbi.nlm.nih.gov/pubmed/26588045	Inhibitor 8504	5.1 µM [IC50]
Sodium channel protein type V alpha subunit 49 Target ID: CHEMBL1980 Sources: https://www.ncbi.nlm.nih.gov/pubmed/21955244	Inhibitor 8504

Conditions

Condition	Modality	Targets	Highest Phase	Product
Atrial fibrillation 131 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/019151s012lbl.pdf	Primary		Approved 8583	RYTHMOL Approved Use Propafenone HCl Extended Release Capsules is indicated to prolong the time to recurrence of symptomatic atrial fibrillation (AF) in patients with episodic (most likely paroxysmal or persistent) AF who do not have structural heart disease. Usage Considerations: •The use of propafenone ER capsules in patients with permanent AF or in patients exclusively with atrial flutter or paroxysmal supraventricular tachycardia (PSVT) has not been evaluated. Do not use propafenone ER capsules to control ventricular rate during AF. •Some patients with atrial flutter treated with propafenone have developed 1:1 conduction, producing an increase in ventricular rate. Concomitant treatment with drugs that increase the functional atrioventricular (AV) nodal refractory period is recommended. • The effect of propafenone on mortality has not been determined [see BOXED WARNING Launch Date 1989
Ventricular arrhythmia 50 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/019151s012lbl.pdf	Primary		Approved 8583	RYTHMOL Approved Use Propafenone HCl Extended Release Capsules is indicated to prolong the time to recurrence of symptomatic atrial fibrillation (AF) in patients with episodic (most likely paroxysmal or persistent) AF who do not have structural heart disease. Usage Considerations: •The use of propafenone ER capsules in patients with permanent AF or in patients exclusively with atrial flutter or paroxysmal supraventricular tachycardia (PSVT) has not been evaluated. Do not use propafenone ER capsules to control ventricular rate during AF. •Some patients with atrial flutter treated with propafenone have developed 1:1 conduction, producing an increase in ventricular rate. Concomitant treatment with drugs that increase the functional atrioventricular (AV) nodal refractory period is recommended. • The effect of propafenone on mortality has not been determined [see BOXED WARNING Launch Date 1989

C_max

Value	Dose	Co-administered	Analyte	Population
189.94 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/19402341	150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered:		PROPAFENONE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
314 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/3606933	300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered:		PROPAFENONE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED

AUC

Value	Dose	Co-administered	Analyte	Population
322.43 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/19402341	150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered:		PROPAFENONE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
2900 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/3606933	300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered:		PROPAFENONE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED

T_1/2

Value	Dose	Co-administered	Analyte	Population
3.61 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/3606933	300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered:		PROPAFENONE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED

F_unbound

Value	Dose	Co-administered	Analyte	Population
4.1% EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/2753068			PROPAFENONE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN

Doses

Dose	Population	Adverse events
425 mg 2 times / day multiple, oral Highest studied dose Dose: 425 mg, 2 times / day Route: oral Route: multiple Dose: 425 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/21-416_Rythmol%20SR_Medr_P1.pdf	unhealthy, adult Health Status: unhealthy Age Group: adult Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/21-416_Rythmol%20SR_Medr_P1.pdf	Other AEs: Monocyte count increased, Eosinophil count increased... Other AEs: Monocyte count increased (0.7%) Eosinophil count increased (0.7%) Platelet count decreased (0.7%) Cardiac failure congestive (1.5%) Coronary artery disease NOS (0.7%) Myocardial infarction (0.7%) Abdominal pain NOS (0.7%) Diarrhea NOS (0.7%) Chest pain (1.5%) Pneumonia NOS (0.7%) Urinary tract infection NOS (0.7%) Prothrombin level decreased (0.7%) Headache (0.7%) Syncope (0.7%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/21-416_Rythmol%20SR_Medr_P1.pdf

AEs

AE	Significance	Dose	Population
Abdominal pain NOS	0.7%	425 mg 2 times / day multiple, oral Highest studied dose Dose: 425 mg, 2 times / day Route: oral Route: multiple Dose: 425 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/21-416_Rythmol%20SR_Medr_P1.pdf	unhealthy, adult Health Status: unhealthy Age Group: adult Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/21-416_Rythmol%20SR_Medr_P1.pdf
Coronary artery disease NOS	0.7%	425 mg 2 times / day multiple, oral Highest studied dose Dose: 425 mg, 2 times / day Route: oral Route: multiple Dose: 425 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/21-416_Rythmol%20SR_Medr_P1.pdf	unhealthy, adult Health Status: unhealthy Age Group: adult Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/21-416_Rythmol%20SR_Medr_P1.pdf
Diarrhea NOS	0.7%	425 mg 2 times / day multiple, oral Highest studied dose Dose: 425 mg, 2 times / day Route: oral Route: multiple Dose: 425 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/21-416_Rythmol%20SR_Medr_P1.pdf	unhealthy, adult Health Status: unhealthy Age Group: adult Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/21-416_Rythmol%20SR_Medr_P1.pdf
Eosinophil count increased	0.7%	425 mg 2 times / day multiple, oral Highest studied dose Dose: 425 mg, 2 times / day Route: oral Route: multiple Dose: 425 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/21-416_Rythmol%20SR_Medr_P1.pdf	unhealthy, adult Health Status: unhealthy Age Group: adult Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/21-416_Rythmol%20SR_Medr_P1.pdf
Headache	0.7%	425 mg 2 times / day multiple, oral Highest studied dose Dose: 425 mg, 2 times / day Route: oral Route: multiple Dose: 425 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/21-416_Rythmol%20SR_Medr_P1.pdf	unhealthy, adult Health Status: unhealthy Age Group: adult Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/21-416_Rythmol%20SR_Medr_P1.pdf
Monocyte count increased	0.7%	425 mg 2 times / day multiple, oral Highest studied dose Dose: 425 mg, 2 times / day Route: oral Route: multiple Dose: 425 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/21-416_Rythmol%20SR_Medr_P1.pdf	unhealthy, adult Health Status: unhealthy Age Group: adult Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/21-416_Rythmol%20SR_Medr_P1.pdf
Myocardial infarction	0.7%	425 mg 2 times / day multiple, oral Highest studied dose Dose: 425 mg, 2 times / day Route: oral Route: multiple Dose: 425 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/21-416_Rythmol%20SR_Medr_P1.pdf	unhealthy, adult Health Status: unhealthy Age Group: adult Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/21-416_Rythmol%20SR_Medr_P1.pdf
Platelet count decreased	0.7%	425 mg 2 times / day multiple, oral Highest studied dose Dose: 425 mg, 2 times / day Route: oral Route: multiple Dose: 425 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/21-416_Rythmol%20SR_Medr_P1.pdf	unhealthy, adult Health Status: unhealthy Age Group: adult Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/21-416_Rythmol%20SR_Medr_P1.pdf
Pneumonia NOS	0.7%	425 mg 2 times / day multiple, oral Highest studied dose Dose: 425 mg, 2 times / day Route: oral Route: multiple Dose: 425 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/21-416_Rythmol%20SR_Medr_P1.pdf	unhealthy, adult Health Status: unhealthy Age Group: adult Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/21-416_Rythmol%20SR_Medr_P1.pdf
Prothrombin level decreased	0.7%	425 mg 2 times / day multiple, oral Highest studied dose Dose: 425 mg, 2 times / day Route: oral Route: multiple Dose: 425 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/21-416_Rythmol%20SR_Medr_P1.pdf	unhealthy, adult Health Status: unhealthy Age Group: adult Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/21-416_Rythmol%20SR_Medr_P1.pdf
Syncope	0.7%	425 mg 2 times / day multiple, oral Highest studied dose Dose: 425 mg, 2 times / day Route: oral Route: multiple Dose: 425 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/21-416_Rythmol%20SR_Medr_P1.pdf	unhealthy, adult Health Status: unhealthy Age Group: adult Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/21-416_Rythmol%20SR_Medr_P1.pdf
Urinary tract infection NOS	0.7%	425 mg 2 times / day multiple, oral Highest studied dose Dose: 425 mg, 2 times / day Route: oral Route: multiple Dose: 425 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/21-416_Rythmol%20SR_Medr_P1.pdf	unhealthy, adult Health Status: unhealthy Age Group: adult Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/21-416_Rythmol%20SR_Medr_P1.pdf
Cardiac failure congestive	1.5%	425 mg 2 times / day multiple, oral Highest studied dose Dose: 425 mg, 2 times / day Route: oral Route: multiple Dose: 425 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/21-416_Rythmol%20SR_Medr_P1.pdf	unhealthy, adult Health Status: unhealthy Age Group: adult Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/21-416_Rythmol%20SR_Medr_P1.pdf
Chest pain	1.5%	425 mg 2 times / day multiple, oral Highest studied dose Dose: 425 mg, 2 times / day Route: oral Route: multiple Dose: 425 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/21-416_Rythmol%20SR_Medr_P1.pdf	unhealthy, adult Health Status: unhealthy Age Group: adult Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/21-416_Rythmol%20SR_Medr_P1.pdf

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1946		substrate 1388	inhibitor 2217

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
OCT1 620 OCT3 159 OCTN1 32 OCTN2 71 P-gp 1741	CYP1A2 1197 P-gp 2052

Drug as perpetrator

Target	Modality	Activity	Metabolite
OCT1 656	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/21641380/	yes [IC50 1 uM]
P-gp 1932	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/15900513/	yes [IC50 19.9 uM]	5-hydroxypropafenone 2
P-gp 1932	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/15900513/	yes [IC50 21.3 uM]	N-desalkylpropafenone 2
P-gp 1932	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/15900513/	yes [IC50 6.8 uM]
OCTN2 71	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/21641380/ \| https://pubmed.ncbi.nlm.nih.gov/20831193/	yes [Ki 74.2 uM]
OCT3 161	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/21641380/	yes
OCTN1 32	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/21641380/	yes

Drug as victim

Target	Modality	Activity	Metabolite	Clinical evidence
P-gp 2052	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/15900513/	no
P-gp 2052	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/15900513/	no	N-desalkylpropafenone 2
P-gp 2052	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/15900513/	yes	5-hydroxypropafenone 2
CYP1A2 1197	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/8423765/ \| https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/021416s011lbl.pdf	yes		yes (co-administration study) Comment: amiodarone and tobacco (CYP1A2 inhibitor) can be expected to cause increased plasma levels of propafenone Sources: https://pubmed.ncbi.nlm.nih.gov/8423765/ \| https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/021416s011lbl.pdf
CYP3A4 1946	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/8423765/ \| https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/021416s011lbl.pdf	yes		yes (co-administration study) Comment: ketoconazole, erythromycin, saquinavir, and grapefruit juice for (CYP3A4 inhibitors) can be expected to cause increased plasma levels of propafenone; The combination of CYP3A4 inhibition and either CYP2D6 deficiency or CYP2D6 sinhibition with the simultaneous administration of propafenone may significantly increase the concentration of propafenone and thereby increase the risk of proarrhythmia and other adverse event Sources: https://pubmed.ncbi.nlm.nih.gov/8423765/ \| https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/021416s011lbl.pdf
CYP2D6 1388	substrate 4014 Sources: https://www.ncbi.nlm.nih.gov/books/NBK425391/	yes		yes (pharmacogenomic study) Comment: Multiple studies have found that genetic variants in the CYP2D6 gene influence the plasma drug levels of propafenone Sources: https://www.ncbi.nlm.nih.gov/books/NBK425391/

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 2263	inhibitor 2237 Sources: https://pubmed.ncbi.nlm.nih.gov/12618228/ \| https://pubmed.ncbi.nlm.nih.gov/15308760/ \| https://pubmed.ncbi.nlm.nih.gov/11330342/

Sourcing

Vendor/Aggregator	ID	URL
ChEBI	CHEBI:63619	https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:63619
ChemicalBook	CB2183169	https://www.chemicalbook.com/ChemicalProductProperty_EN_CB2183169
ChemicalBook	CB2854418	https://www.chemicalbook.com/ChemicalProductProperty_EN_CB2854418
eMolecules	593585	https://www.emolecules.com/cgi-bin/more?vid=593585
MolPort	MolPort-002-545-323	https://www.molport.com/shop/molecule-link/MolPort-002-545-323
Selleck Chemicals	Propafenone(Rytmonorm)	http://www.selleckchem.com/products/Propafenone(Rytmonorm).html

PubMed

Title	Date	PubMed
An organic psychosis due to a venlafaxine-propafenone interaction.	2001	11949740
Algorithmic complexity. A new approach of non-linear algorithms for the analysis of atrial signals from multipolar basket catheter.	2001	11889958
[Clinical and experimental study of effect of yangxin fumai oral liquid in treating patients with extrasystole].	2001 Feb	12577393
The effect of propafenone on premature ventricular contractions (PVC): an analysis based on heart rate dependency of PVCs.	2001 Nov	11933920
[Pharmacological cardioversion of atrial fibrillation with intravenous and oral propafenone].	2002	12552163
Risk of mortality in a cohort of patients newly diagnosed with chronic atrial fibrillation.	2002	11897013
Adverse drug events in hospitalized patients treated with cardiovascular drugs and anticoagulants.	2002 Apr-May	12051123
How to enhance acute outcome of electrical cardioversion by drug therapy: importance of immediate reinitiation of atrial fibrillation.	2002 Aug	12212706
Long-term clinical significance of frequent and complex ventricular tachyarrhythmias in trained athletes.	2002 Aug 7	12142109
[Role amiodarone in sinus rhythm maintenance after successful cardioversion in patients with chronic non-valvular atrial fibrillation].	2002 Dec	12687927
Efficacy and safety of propafenone sustained release in the prophylaxis of symptomatic paroxysmal atrial fibrillation (The European Rythmol/Rytmonorm Atrial Fibrillation Trial [ERAFT] Study).	2002 Dec 15	12480038
Evidence for the possible involvement of Ca2+ entry blockade in the relaxation by class I antiarrhythmic drugs in the isolated pig coronary smooth muscle.	2002 Jan	11862334
[Disclosure of "Brugada's syndrome" with intravenous propafenone].	2002 Jan-Mar	11933698
Propafenone-related cholestatic hepatitis in an elderly patient.	2002 Jul	12189974
[Proarrhythmic effects of propafenone in a woman with hepatopathy: is it always a simple drug in clinical practice?].	2002 Jul	12187639
Amiodarone reduces procedures and costs related to atrial fibrillation in a controlled clinical trial.	2002 Jul	12093058
Quality of life improves with treatment in the Canadian Trial of Atrial Fibrillation.	2002 Jun	12075253
[The treatment of postoperative junctional ectopic tachycardia].	2002 Jun	12042148
An evaluation of the strategy of maintenance of sinus rhythm by antiarrhythmic drug therapy after ablation and pacing therapy in patients with paroxysmal atrial fibrillation.	2002 Jun	12042011
Intermittent Brugada syndrome misdiagnosed as acute myocardial infarction and unmasked with propafenone.	2002 Jun	12010935
[Antiarrhythmic drugs in atrial fibrillation].	2002 Jun 15	12187895
Effect of propafenone on the contractile activity of Latissimus dorsi muscle isolated in an organ chamber: experimental study in rats.	2002 Mar	11967585
[Structure and activity relationship of propafenone and alkylesters of 2-and 4-[(3-propylamino-2-hydroxy)-propoxy]-phenylcarbamic acid].	2002 May	12058356
Similarity based SAR (SIBAR) as tool for early ADME profiling.	2002 Nov	12825790
Effect of CYP2D6*10 genotype on propafenone pharmacodynamics in Chinese patients with ventricular arrhythmia.	2002 Nov	12421483
Human variability in polymorphic CYP2D6 metabolism: is the kinetic default uncertainty factor adequate?	2002 Nov	12176090
[Recent onset atrial fibrillation at a unit of internal medicine].	2002 Oct	12405012
Beta-adrenergic stimulation modulates the sodium current block by propafenone in rat ventricular myocardium.	2002 Oct	12395362
New insights into the mechanisms and management of atrial fibrillation.	2002 Oct 29	12403742
[Hepatic toxicity of propafenone: a case description].	2002 Oct-Dec	12532566
Maintaining stability of sinus rhythm in atrial fibrillation: antiarrhythmic drugs versus ablation.	2002 Sep	12169239
Exercise-induced bidirectional ventricular tachycardia with alternating right and left bundle branch block-type patterns--a case report.	2002 Sep-Oct	12365869
Long-term follow-up of sudden cardiac arrest survivors and electrophysiologically guided antiarrhythmic therapy.	2003	12845245
Electrophysiological mapping and histological examinations of the swine atrium with sustained (> or =24 h) atrial fibrillation: a suitable animal model for studying human atrial fibrillation.	2003	12711882
Intracardiac low-energy versus transthoracic high-energy direct-current cardioversion of atrial fibrillation: a randomised comparison.	2003	12711881
High-throughput screening to estimate single or multiple enzymes involved in drug metabolism: microtitre plate assay using a combination of recombinant CYP2D6 and human liver microsomes.	2003 Aug	12936703
Oral loading single dose flecainide for pharmacological cardioversion of recent-onset atrial fibrillation.	2003 Feb	12559528
[Clinical heart arrest after emergency "direct current" cardioversion of atrial flutter].	2003 Feb 3	12608028
New multidrug resistance reversal agents.	2003 Jan	12528988
Stereoselectivity in trans-tramadol metabolism and trans-O-demethyltramadol formation in rat liver microsomes.	2003 Jan	12511234
Class I or class III agents for atrial fibrillation: are asking the right question?	2003 Jul	12914611
Risk factors for recurrence of atrial fibrillation in patients undergoing hybrid therapy for antiarrhythmic drug-induced atrial flutter.	2003 Jul	12831821
A novel two-pore domain K+ channel, TRESK, is localized in the spinal cord.	2003 Jul 25	12754259
Unintentional pediatric overdose of propafenone.	2003 Jul-Aug	12841836
Amiodarone for pharmacological cardioversion of recent-onset atrial fibrillation.	2003 Jun	12767548
[Drug therapy of atrial fibrillation].	2003 Jun 15	12866149
In silico screening with benzofurane- and benzopyrane-type MDR-modulators.	2003 Mar	12620414
Excitable gap composition in the presence of antiarrhythmic drugs in common human atrial flutter.	2003 Mar 15	12677279
Pharmacologic and nonpharmacologic options to maintain sinus rhythm: guideline-based and new approaches.	2003 Mar 20	12670640
Effects of acute ischemia, early extrabeats and propafenone on complex activation patterns in intact and ischemic canine hearts.	2003 May 2	12679192

Patents

Sample Use Guides

In Vivo Use Guide

Initiate therapy with 150 mg given every 8 hours. As needed, uptitrate in 3-4 days to 225-300 mg every 8 hours

Route of Administration: Oral

In Vitro Use Guide

Hela cells were used for activity evaluation. Proliferation percentage was determined by the SRB assay. Cells were incubated with the Propafenone at the concentrations of 0.005-0.2 g/L for 48 h, and the cell proliferation/viability was determined using the survival percentage with the cells treated only with dimethyl sulfoxide (DMSO) at 0.1% as a reference

Substance Class	Chemical Created by `admin` on `Mon Mar 31 19:10:27 GMT 2025` Edited by `admin` on `Mon Mar 31 19:10:27 GMT 2025`
Record UNII	33XCH0HOCD
Record Status	`Validated (UNII)`
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Name

Type

Language

PROPAFENONE HYDROCHLORIDE

Official Name

English

RYTHMOL

Preferred Name

English

Propafenone hydrochloride [WHO-DD]

Common Name

English

PROPAFENONE HYDROCHLORIDE [VANDF]

Common Name

English

1-PROPANONE, 1-(2-(2-HYDROXY-3-(PROPYLAMINO)PROPOXY)PHENYL)-3-PHENYL-, HYDROCHLORIDE

Systematic Name

English

PROPAFENONE HYDROCHLORIDE [JAN]

Common Name

English

PROPAFENONE HYDROCHLORIDE [MART.]

Common Name

English

2'-(2-HYDROXY-3-(PROPYLAMINO)PROPOXY)-3-PHENYLPROPIOPHENONE HYDROCHLORIDE

Systematic Name

English

PROPAFENONE HYDROCHLORIDE [USAN]

Common Name

English

PROPAFENONE HYDROCHLORIDE [MI]

Common Name

English

NSC-758640

Code

English

PROPAFENONE HCL

Common Name

English

RYTHMOL SR

Brand Name

English

PROPAFENONE HYDROCHLORIDE [ORANGE BOOK]

Common Name

English

PROPAFENONE HYDROCHLORIDE [EP MONOGRAPH]

Common Name

English

PROPAFENONE HYDROCHLORIDE [USP-RS]

Common Name

English

PROPAFENONE HYDROCHLORIDE [USP MONOGRAPH]

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C47793