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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2014/04/07 10:11:24」(JST)

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Propafenone (/proʊˈpæfɨnoʊn/ proh-PAF-i-nohn; brand name Rythmol SR or Rytmonorm) is a class of anti-arrhythmic medication, which treats illnesses associated with rapid heart beats such as atrial and ventricular arrhythmias.

Mechanism of action

Propafenone works by slowing the influx of sodium ions into the cardiac muscle cells, causing a decrease in excitability of the cells. Propafenone is more selective for cells with a high rate, but also blocks normal cells more than class Ia or Ib. Propafenone differs from the prototypical class Ic antiarrhythmic in that it has additional activity as a beta-adrenergic blocker which can cause bradycardia and bronchospasm.

Metabolism

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.

Side effects

Side effects attributed to propafenone include hypersensitivity reactions, lupus-like syndrome, agranulocytosis, CNS disturbances such as dizziness, lightheadedness, gastrointestinal upset, a metallic taste and bronchospasm. About 20% of patients discontinued the drug due to side effects.

Initiation of therapy

Propafenone generally needs to be started in a hospital setting to assure ECG monitoring of the patient. There are many different dosages of propafenone, depending on clinical presentation of the arrhythmia. The treatment is generally begun with relatively high dosages (450–900 mg/d) decreasing to near 300 mg/d. In most western countries the accepted maximal dosage is 900 mg/d.

For economic and patient convenience reasons, some clinicians are starting certain antiarrhythmic agents in an outpatient setting for some patients. No consensus exists regarding the safety of this practice, and information is needed to determine which agents and which patients are appropriate for outpatient initiation of antiarrhythmic therapy. From a clinical point of view, this drug is used primarily in patients with relatively preserved myocardial function. http://www.ahrq.gov/clinic/epcsums/atrialsum.htm

Contraindications and cautions

Caution should be used in administrating propafenone in individuals with hepatic dysfunction, asthma, CHF, or bradycardia.

Patent issues

The patents for the Rythmol family of products are owned by Reliant Pharmaceuticals, Inc., in Liberty Corner, N.J. Reliant acquired the patents from developer Abbott Laboratories, Inc., in 2003. Rythmol was originally developed in Europe and marketed by Knoll Pharma both in Europe and North America. The product was taken over by Abbott in 2001 when Abbott purchased Knoll.

Reliant Pharmaceuticals filed a federal patent infringement lawsuit against generic drug maker Par Pharmaceuticals, Inc., on December 19, 2006. The lawsuit, filed in the federal district court for Delaware, seeks to prevent Par from manufacturing a generic version of Rythmol. Par is seeking approval to do so from the U.S. Food and Drug Administration.

Reliant's patent for the drug was issued in October, 1997, and it expires in 2014. Par believes the patent is invalid, according to its filing with the FDA.

External links

Rythmol (manufacturer's website)^{[dead link]}
Propafenone (patient information)

UpToDate Contents

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English Journal

Utility of Routine Exercise Testing to Detect Rate-Related QRS Widening in Patients Without Structural Heart Disease on Class Ic Antiarrhythmic Agents (Flecainide and Propafenone).

Vallurupalli S1, Pothineni NV2, Deshmukh A3, Paydak H2.
The American journal of cardiology.Am J Cardiol.2015 Sep 1;116(5):730-2. doi: 10.1016/j.amjcard.2015.05.039. Epub 2015 Jun 3.
Class Ic antiarrhythmic agents are effective in the treatment of various atrial tachyarrhythmias. They are known to cause rate-related QRS widening in the presence of structural heart disease, which can lead to life-threatening arrhythmias. The role of routine exercise electrocardiography in patient
PMID 26100588

Prophylactic lidocaine for myocardial infarction.

Martí-Carvajal AJ1, Simancas-Racines D, Anand V, Bangdiwala S.
The Cochrane database of systematic reviews.Cochrane Database Syst Rev.2015 Aug 21;8:CD008553. doi: 10.1002/14651858.CD008553.pub2.
BACKGROUND: Coronary artery disease is a major public health problem affecting both developed and developing countries. Acute coronary syndromes include unstable angina and myocardial infarction with or without ST-segment elevation (electrocardiogram sector is higher than baseline). Ventricular arrh
PMID 26295202

Factors predisposing to ventricular proarrhythmia during antiarrhythmic drug therapy for atrial fibrillation in patients with structurally normal heart.

Lin CY1, Lin YJ1, Lo LW1, Chen YY2, Chong E3, Chang SL1, Chung FP1, Chao TF1, Hu YF1, Tuan TC1, Liao JN1, Chang Y1, Chien KL4, Chiou CW1, Chen SA5.
Heart rhythm : the official journal of the Heart Rhythm Society.Heart Rhythm.2015 Jul;12(7):1490-500. doi: 10.1016/j.hrthm.2015.04.018. Epub 2015 Apr 15.
BACKGROUND: Ventricular arrhythmia (VA) can occur during propafenone therapy in atrial fibrillation (AF) patients with structurally normal heart.OBJECTIVE: The purpose of this study was to evaluate the incidence and characteristics of propafenone-associated VAs in AF patients with structurally norma
PMID 25889809

Related Pictures

Rythmol, Rythmol SR (propafenone) Drug Rytmonorm (Rythmol) 300 Mg 30 Film Tablets Rythmol :: General Health :: Generics picture alternative for rythmol Logo Reliant 325 Pill - Rythmol SR 325 mg Rythmol oral : Uses, Side Effects Rythmol Oral Tablet Drug Information, Side Rythmol prescription drug /side effects

★リンクテーブル★

リンク元

「プロパフェノン」

Propafenone
Systematic (IUPAC) name
	1-{2-[2-hydroxy-3-(propylamino)propoxy]phenyl}-3-phenylpropan-1-one
Clinical data
Trade names	Rythmol
AHFS/Drugs.com	monograph
MedlinePlus	a698002
Pregnancy cat.	C
Legal status	Prescription only
Routes	Oral
Pharmacokinetic data
Bioavailability	?
Protein binding	97%
Half-life	2-10 hours
Identifiers
CAS number	54063-53-5
ATC code	C01BC03
PubChem	CID 4932
IUPHAR ligand	2561
DrugBank	DB01182
ChemSpider	4763
UNII	68IQX3T69U
KEGG	D08435
ChEMBL	CHEMBL631
Chemical data
Formula	C21H27NO3
Mol. mass	341.444 g/mol
	SMILES O=C(c1ccccc1OCC(O)CNCCC)CCc2ccccc2;
	InChI 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 ; Key:JWHAUXFOSRPERK-UHFFFAOYSA-N ;
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　　[★]

英: propafenone
化: 塩酸プロパフェノン, propafenone hydrochloride
商: ソビラール、プロノン、Rythmol
関: 抗不整脈薬

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Rythmol