pilsicainide hydrochloride

Action and Spectrum

Actions and Spectrum: 

Actions: 

• Sodium Channel Blockade: pilsicainde hydrochloride mainly blocks sodium channels in cardiac cells. This slows down the conduction of electrical signals, particularly in the atria. Doing this helps prevent the rapid and disorganized electrical activity of atrial fibrillation and atrial flutter. 
• Rate Control: pilsicainde can indirectly control the heart rate in patients with rapid atrial arrhythmias by slowing the conduction of electrical impulses. 
• Conversion of Arrhythmias: pilsicainde can help convert atrial fibrillation and atrial flutter back to normal sinus rhythm. This is particularly useful for acute episodes of these arrhythmias.

Spectrum: 

pilsicainde hydrochloride is primarily indicated for treating atrial fibrillation and atrial flutter. These arrhythmias involve rapid, irregular electrical activity in the atria, which can lead to compromised cardiac function and an increased risk of stroke due to blood clot formation. pilsicainde’s sodium channel-blocking properties help restore a more organized rhythm and improve cardiac function. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Dizziness 

Headache 

Tremor 

Vomiting 

Confusion 

Amnesia 

Hallucinations 

Ataxia 

Tremor 

Depression 

Black Box Warning

Black Box Warning: 

None 

Contraindication / Caution

Contraindication/Caution: 

Contraindications: 

• Severe Structural Heart Disease 
• Known hypersensitivity 
• Conduction disturbances 
• Bradycardia 

Cautions: 

• Renal impairment  
• Liver impairment 
• Elderly patients 
• Electrolyte imbalance 
• Drug interactions 
• Pregnancy  
• Breastfeeding 

Pregnancy / Lactation

Pregnancy consideration:  

The drug should be avoided during pregnancy. 

Breastfeeding warnings:  

The drug is not indicated during lactation.  

Pregnancy category: 

Category A: Well-controlled and satisfactory studies show no risk to the fetus in the initial or later trimester. 

Category B: There was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 

Category C: There was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    

Category X: Drugs listed in this category outweigh the risks over benefits. Hence, these categories of drugs need to be avoided by pregnant women.    

Category N: No data is available for the drug under this category. 

Pharmacology

Pharmacology:  

pilsicainde belongs to the class Ic antiarrhythmics, which are sodium channel blockers. It exerts its effects on cardiac cells by blocking fast sodium channels, which are responsible for the rapid depolarization phase of the action potential. By inhibiting sodium influx, pilsicainide slows the conduction of electrical impulses through the heart and decreases the excitability of cardiac tissues. 

Pharmacodynamics: 

The effects of pilsicainide on conduction velocity and refractoriness make it effective in treating certain types of arrhythmias, especially those involving rapid and irregular heartbeats originating in the atria. Pilsicainide helps stabilize the heart’s electrical activity and restore a regular rhythm by slowing conduction and prolonging refractoriness. 

Pharmacokinetics: 

Absorption: 

pilsicainde is rapidly absorbed from the gastrointestinal tract after oral administration. 

Distribution:  

Once absorbed, pilsicainide hydrochloride is throughout the body, potentially reaching various tissues. 

Metabolism: 

The drug is primarily metabolized in the liver by cytochrome P450 (CYP) family enzymes, particularly CYP2D6. This metabolism can lead to variations in drug response based on individual genetic differences in CYP2D6 activity. 

Elimination and Excretion: 

pilsicainide and its metabolites are eliminated from the body primarily through renal excretion. Dosage adjustments may be required in patients with impaired renal function. 

Adminstartion

Administration: 

The dosage of pilsicainide hydrochloride based on factors such as the type of arrhythmia being treated, your medical history, and your response to the medication. Dosages can vary widely and are usually tailored to each patient’s needs. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: pilsicainide hydrochloride 

Pronounced as: pil-si-kay-nyd 

Why do we use pilsicainide hydrochloride? 

• Control of Abnormal Heart Rhythms: Atrial fibrillation and atrial flutter are characterized by irregular and often rapid heartbeats. These abnormal rhythms can lead to inefficient pumping of blood and an increased risk of blood clots forming in the heart, potentially leading to stroke or other complications. pilsicainde helps restore a more regular heart rhythm by affecting the heart’s electrical conduction. 
• Sodium Channel Blockade: pilsicainde is a sodium channel blocker, categorized explicitly as a class Ic antiarrhythmic agent. It works by blocking sodium channels in cardiac cells, which slows down the electrical signals traveling through the heart. This action helps prevent the rapid firing of abnormal signals that can cause irregular heart rhythms. 
• Restoring Normal Conduction: By slowing the conduction of electrical signals, pilsicainide can help the heart’s electrical system reset itself, allowing for a more organized and coordinated rhythm. This can improve the heart’s pumping efficiency and reduce arrhythmias symptoms, such as palpitations, shortness of breath, and fatigue. 
• Prolonged Refractoriness: pilsicainde also increases the refractory period of cardiac cells. This means that after a cell has fired an electrical signal (action potential), it takes longer for the cell to be ready for another signal. This can help prevent the heart from entering a rapid and chaotic rhythm.