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QuickView for Propafenone (compound)

Name: Propafenone
PubChem Compound ID: 184821
Description: An antiarrhythmia agent that is particularly effective in ventricular arrhythmias. It also has weak beta-blocking activity. The drug is generally well tolerated.
Molecular formula: C21H28ClNO3
Molecular weight: 377.905 g/mol
Name: Propafenone
Name (isomeric): DB01182
Drug Type: small molecule
Description: An antiarrhythmia agent that is particularly effective in ventricular arrhythmias. It also has weak beta-blocking activity. The drug is generally well tolerated.
Propafenona [INN-Spanish]; Propafenone hydrochloride; Propafenonum [INN-Latin]; Propafenone HCl; Propafenone-HCl
Brand: Rythmol SR, Rythmol
Category: Anti-Arrhythmia Agents
CAS number: 54063-53-5
Indication: Used to prolong the time to recurrence of paroxysmal atrial fibrillation/flutter (PAF) associated with disabling symptoms in patients without structural heart disease. Also used for the treatment of life-threatening documented ventricular arrhythmias, such as sustained ventricular tachycardia.
Propafenone is a Class 1C antiarrhythmic drug with local anesthetic effects, and a direct stabilizing action on myocardial membranes. It is used in the treatment of atrial and ventricular arrhythmias. It works by slowing the influx of sodium ions into the cardiac muscle cells, causing a decrease in excitablity of the cells. Propafenone has local an...
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Mechanism of Action:
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 excit...
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Absorption: Nearly completely absorbed following oral administration (90%). Systemic bioavailability ranges from 5 to 50%, due to significant first-pass metabolism. This wide range in systemic bioavailability is related to two factors: presence of food (food increases bioavailability) and dosage (bioavailability is 3.4% for a 150-mg tablet compared to 10.6% for a 300-mg tablet).
Protein binding: 97%
Biotransformation: Metabolized primarily in the liver where it is rapidly and extensively metabolized to two active metabolites, 5-hydroxypropafenone and N-depropylpropafenone. These metabolites have antiarrhythmic activity comparable to propafenone but are present in concentrations less than 25% of propafenone concentrations.
Route of elimination: Naloxone is metabolized in the liver primarily by glucuronide conjugation with naloxone-3-glucuronide as the major metabolite. After an oral or intravenous dose, about 25 to 40% of the drug is excreted as metabolites in urine within 6 hours.
Half Life: 2-10 hours
Toxicity: Symptoms of propafenone overdose (usually most severe within the first 3 hours) may include convulsions (rarely), heartbeat irregularities, low blood pressure, and sleepiness.
Affected organisms: Humans and other mammals
Food interaction:
Grapefruit and grapefruit juice should be avoided throughout treatment. Grapefruit can increase serum levels of this product.
Always take at the same time in regard to meals.
Drug interaction:
TerbinafineTerbinafine may reduce the metabolism and clearance of Propafenone. Consider alternate therapy or monitor for therapeutic/adverse effects of Propafenone if Terbinafine is initiated, discontinued or dose changed.
DuloxetinePossible increase in the levels of this agent when used with duloxetine
AnisindionePropafenone may increase the anticoagulant effect of anisindione.
MetoprololPropafenone may increase the effect of beta-blocker, metoprolol.
FluoxetineAdditive QTc-prolongation may occur increasing the risk of serious life-threatening arrhythmias. Fluoxetine may also increase the serum concentration of propafenone. Use caution during concomitant therapy and monitor for QTc-prolongation.
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