PROPAFENONE

First approved in 1989

Details

Stereochemistry	RACEMIC
Molecular Formula	C21H27NO3
Molecular Weight	341.444
Optical Activity	( + / - )
Defined Stereocenters	0 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

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

InChI

InChIKey=JWHAUXFOSRPERK-UHFFFAOYSA-N

InChI=1S/C21H27NO3/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

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	( + / - )

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
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.	2003-08	12936703
A novel two-pore domain K+ channel, TRESK, is localized in the spinal cord.	2003-07-25	12754259
Unintentional pediatric overdose of propafenone.	2003-07-05	12841836
Class I or class III agents for atrial fibrillation: are asking the right question?	2003-07	12914611
Risk factors for recurrence of atrial fibrillation in patients undergoing hybrid therapy for antiarrhythmic drug-induced atrial flutter.	2003-07	12831821
[Drug therapy of atrial fibrillation].	2003-06-15	12866149
Amiodarone for pharmacological cardioversion of recent-onset atrial fibrillation.	2003-06	12767548
Effects of acute ischemia, early extrabeats and propafenone on complex activation patterns in intact and ischemic canine hearts.	2003-05-02	12679192
Pharmacologic and nonpharmacologic options to maintain sinus rhythm: guideline-based and new approaches.	2003-03-20	12670640
Old and new antiarrhythmic drugs for converting and maintaining sinus rhythm in atrial fibrillation: comparative efficacy and results of trials.	2003-03-20	12670638
Excitable gap composition in the presence of antiarrhythmic drugs in common human atrial flutter.	2003-03-15	12677279
Effects of a series of dihydroanthracene derivatives on drug efflux in multidrug resistant cancer cells.	2003-03	12667692
Propafenone versus ibutilide for post operative atrial fibrillation following cardiac surgery: neither strategy improves outcomes compared to rate control alone (the PIPAF study).	2003-03	12640352
In silico screening with benzofurane- and benzopyrane-type MDR-modulators.	2003-03	12620414
Left atrial size after cardioversion for atrial fibrillation: effect of external direct current shock.	2003-03	12618736
Effects of propafenone and its main metabolite, 5-hydroxypropafenone, on HERG channels.	2003-03	12618228
Molecular site of action of the antiarrhythmic drug propafenone at the voltage-operated potassium channel Kv2.1.	2003-03	12606761
[Clinical heart arrest after emergency "direct current" cardioversion of atrial flutter].	2003-02-03	12608028
Propafenone hepatotoxicity: report of two new cases.	2003-02	12643615
Oral loading single dose flecainide for pharmacological cardioversion of recent-onset atrial fibrillation.	2003-02	12559528
[Hepatic toxicity of propafenone: a case description].	2003-01-21	12532566
New multidrug resistance reversal agents.	2003-01	12528988
Stereoselectivity in trans-tramadol metabolism and trans-O-demethyltramadol formation in rat liver microsomes.	2003-01	12511234
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
Lopinavir/ritonavir: a review of its use in the management of HIV infection.	2003	12662125
Efficacy and safety of propafenone sustained release in the prophylaxis of symptomatic paroxysmal atrial fibrillation (The European Rythmol/Rytmonorm Atrial Fibrillation Trial [ERAFT] Study).	2002-12-15	12480038
[Role amiodarone in sinus rhythm maintenance after successful cardioversion in patients with chronic non-valvular atrial fibrillation].	2002-12	12687927
Similarity based SAR (SIBAR) as tool for early ADME profiling.	2002-11	12825790
Effect of CYP2D6*10 genotype on propafenone pharmacodynamics in Chinese patients with ventricular arrhythmia.	2002-11	12421483
Human variability in polymorphic CYP2D6 metabolism: is the kinetic default uncertainty factor adequate?	2002-11	12176090
New insights into the mechanisms and management of atrial fibrillation.	2002-10-29	12403742
Exercise-induced bidirectional ventricular tachycardia with alternating right and left bundle branch block-type patterns--a case report.	2002-10-09	12365869
[Recent onset atrial fibrillation at a unit of internal medicine].	2002-10	12405012
Beta-adrenergic stimulation modulates the sodium current block by propafenone in rat ventricular myocardium.	2002-10	12395362
Maintaining stability of sinus rhythm in atrial fibrillation: antiarrhythmic drugs versus ablation.	2002-09	12169239
Long-term clinical significance of frequent and complex ventricular tachyarrhythmias in trained athletes.	2002-08-07	12142109
How to enhance acute outcome of electrical cardioversion by drug therapy: importance of immediate reinitiation of atrial fibrillation.	2002-08	12212706
Congenital junctional ectopic tachycardia in children and adolescents: a 20 year experience based study.	2002-08	12117855
Propafenone-related cholestatic hepatitis in an elderly patient.	2002-07	12189974
[Proarrhythmic effects of propafenone in a woman with hepatopathy: is it always a simple drug in clinical practice?].	2002-07	12187639
Amiodarone reduces procedures and costs related to atrial fibrillation in a controlled clinical trial.	2002-07	12093058
[Antiarrhythmic drugs in atrial fibrillation].	2002-06-15	12187895
[Efficacy and tolerance of propafenone after correction of atrial fibrillation: PEPS pharmaco-epidemiologic study].	2002-06	12138815
Paroxysmal supraventricular tachycardia induced by oral stimulation: a case report and review of swallow-induced dysrhythmias.	2002-05	12113851
[Pharmacological cardioversion of atrial fibrillation with intravenous and oral propafenone].	2002	12552163
Oral mucosal drug delivery: clinical pharmacokinetics and therapeutic applications.	2002	12126458
Impact of stereoselectivity on the pharmacokinetics and pharmacodynamics of antiarrhythmic drugs.	2002	12102640
[Clinical and experimental study of effect of yangxin fumai oral liquid in treating patients with extrasystole].	2001-02	12577393

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 17:59:27 GMT 2025` Edited by `admin` on `Mon Mar 31 17:59:27 GMT 2025`
Record UNII	68IQX3T69U
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

PROPAFENONE

Official Name

English

PROPAFENON HEXAL

Preferred Name

English

PROPAFENONE [MI]

Common Name

English

PROPAFENONE [VANDF]

Common Name

English

Propafenone [WHO-DD]

Common Name

English

propafenone [INN]

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C93038