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=C(C=CC=C1)C(=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 8228	7.6 nM [IC50]
Potassium channel subfamily K member 3 10 Target ID: CHEMBL2321613 Sources: https://www.ncbi.nlm.nih.gov/pubmed/26588045	Inhibitor 8228	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 8228

Conditions

Condition	Modality	Targets	Highest Phase	Product
Atrial fibrillation 131 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/019151s012lbl.pdf	Primary		Approved 8360	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 6.2812802E11
Ventricular arrhythmia 50 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/019151s012lbl.pdf	Primary		Approved 8360	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 6.2812802E11

C_max

Value	Dose	Co-administered	Analyte	Population
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
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

AUC

Value	Dose	Co-administered	Analyte	Population
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
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

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 n = 135 Health Status: unhealthy Condition: atrial fibrillation Age Group: adult Sex: M+F Population Size: 135 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 n = 135 Health Status: unhealthy Condition: atrial fibrillation Age Group: adult Sex: M+F Population Size: 135 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 n = 135 Health Status: unhealthy Condition: atrial fibrillation Age Group: adult Sex: M+F Population Size: 135 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 n = 135 Health Status: unhealthy Condition: atrial fibrillation Age Group: adult Sex: M+F Population Size: 135 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 n = 135 Health Status: unhealthy Condition: atrial fibrillation Age Group: adult Sex: M+F Population Size: 135 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 n = 135 Health Status: unhealthy Condition: atrial fibrillation Age Group: adult Sex: M+F Population Size: 135 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 n = 135 Health Status: unhealthy Condition: atrial fibrillation Age Group: adult Sex: M+F Population Size: 135 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 n = 135 Health Status: unhealthy Condition: atrial fibrillation Age Group: adult Sex: M+F Population Size: 135 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 n = 135 Health Status: unhealthy Condition: atrial fibrillation Age Group: adult Sex: M+F Population Size: 135 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 n = 135 Health Status: unhealthy Condition: atrial fibrillation Age Group: adult Sex: M+F Population Size: 135 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 n = 135 Health Status: unhealthy Condition: atrial fibrillation Age Group: adult Sex: M+F Population Size: 135 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 n = 135 Health Status: unhealthy Condition: atrial fibrillation Age Group: adult Sex: M+F Population Size: 135 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 n = 135 Health Status: unhealthy Condition: atrial fibrillation Age Group: adult Sex: M+F Population Size: 135 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 n = 135 Health Status: unhealthy Condition: atrial fibrillation Age Group: adult Sex: M+F Population Size: 135 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 n = 135 Health Status: unhealthy Condition: atrial fibrillation Age Group: adult Sex: M+F Population Size: 135 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/21-416_Rythmol%20SR_Medr_P1.pdf

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1709		substrate 1193	inhibitor 1599

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
OCT1 506 OCT3 149 OCTN1 29 OCTN2 66 P-gp 1437	CYP1A2 1032 P-gp 1527

Drug as perpetrator

Target	Modality	Activity	Metabolite
OCT1 523	inhibitor 3240 Sources: https://pubmed.ncbi.nlm.nih.gov/21641380/	yes [IC50 1 uM]
P-gp 1626	inhibitor 3240 Sources: https://pubmed.ncbi.nlm.nih.gov/15900513/	yes [IC50 19.9 uM]	5-hydroxypropafenone 2
P-gp 1626	inhibitor 3240 Sources: https://pubmed.ncbi.nlm.nih.gov/15900513/	yes [IC50 21.3 uM]	N-desalkylpropafenone 2
P-gp 1626	inhibitor 3240 Sources: https://pubmed.ncbi.nlm.nih.gov/15900513/	yes [IC50 6.8 uM]
OCTN2 71	inhibitor 3240 Sources: https://pubmed.ncbi.nlm.nih.gov/21641380/ \| https://pubmed.ncbi.nlm.nih.gov/20831193/	yes [Ki 74.2 uM]
OCT3 149	inhibitor 3240 Sources: https://pubmed.ncbi.nlm.nih.gov/21641380/	yes
OCTN1 29	inhibitor 3240 Sources: https://pubmed.ncbi.nlm.nih.gov/21641380/	yes

Drug as victim

Target	Modality	Activity	Metabolite	Clinical evidence
P-gp 1527	substrate 3326 Sources: https://pubmed.ncbi.nlm.nih.gov/15900513/	no
P-gp 1527	substrate 3326 Sources: https://pubmed.ncbi.nlm.nih.gov/15900513/	no	N-desalkylpropafenone 2
P-gp 1527	substrate 3326 Sources: https://pubmed.ncbi.nlm.nih.gov/15900513/	yes	5-hydroxypropafenone 2
CYP1A2 1032	substrate 3326 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 1709	substrate 3326 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 1193	substrate 3326 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 1632	inhibitor 1613 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
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
eMolecules	593585	https://www.emolecules.com/cgi-bin/more?vid=593585

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
Chiral metabolism of propafenone in rat hepatic microsomes treated with two inducers.	2001 Dec	11854911
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
Oral mucosal drug delivery: clinical pharmacokinetics and therapeutic applications.	2002	12126458
Impact of stereoselectivity on the pharmacokinetics and pharmacodynamics of antiarrhythmic drugs.	2002	12102640
Risk of mortality in a cohort of patients newly diagnosed with chronic atrial fibrillation.	2002	11897013
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
Amiodarone reduces procedures and costs related to atrial fibrillation in a controlled clinical trial.	2002 Jul	12093058
Amiodarone: pearl or peril?	2002 Jul	12093050
Inhibition of the current of heterologously expressed HERG potassium channels by flecainide and comparison with quinidine, propafenone and lignocaine.	2002 Jul	12086981
[Efficacy and tolerance of propafenone after correction of atrial fibrillation: PEPS pharmaco-epidemiologic study].	2002 Jun	12138815
Quality of life improves with treatment in the Canadian Trial of Atrial Fibrillation.	2002 Jun	12075253
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
Paroxysmal supraventricular tachycardia induced by oral stimulation: a case report and review of swallow-induced dysrhythmias.	2002 May	12113851
[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
[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
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
Lopinavir/ritonavir: a review of its use in the management of HIV infection.	2003	12662125
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
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
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
[Drug therapy of atrial fibrillation].	2003 Jun 15	12866149
Effects of a series of dihydroanthracene derivatives on drug efflux in multidrug resistant cancer cells.	2003 Mar	12667692
In silico screening with benzofurane- and benzopyrane-type MDR-modulators.	2003 Mar	12620414
Left atrial size after cardioversion for atrial fibrillation: effect of external direct current shock.	2003 Mar	12618736
Molecular site of action of the antiarrhythmic drug propafenone at the voltage-operated potassium channel Kv2.1.	2003 Mar	12606761
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
Old and new antiarrhythmic drugs for converting and maintaining sinus rhythm in atrial fibrillation: comparative efficacy and results of trials.	2003 Mar 20	12670638
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 `Wed Jul 05 23:00:19 UTC 2023` Edited by `admin` on `Wed Jul 05 23:00:19 UTC 2023`
Record UNII	68IQX3T69U
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

PROPAFENONE

Official Name

English

PROPAFENONE [MI]

Common Name

English

PROPAFENON HEXAL

Brand Name

English

PROPAFENONE [INCI]

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