bepridil

Action and Spectrum

Actions and Spectrum: 

Actions: 

bepridil exerts pharmacological effects by inhibiting calcium ion influx into cardiac and smooth muscle cells. It achieves this by blocking specific types of calcium channels, mainly the L-type calcium channels. 

By inhibiting calcium influx into cardiac muscle cells, bepridil reduces the entry of calcium ions during the stagnant phase of the cardiac action potential. This results in a decrease in myocardial contractility, a reduction in the heart rate, and dilation of coronary arteries. These actions help lower the heart’s oxygen demand, making it helpful in treating angina pectoris. 

Spectrum: 

bepridil is used to treat chronic stable angina pectoris (chest pain) in patients with coronary artery disease when other treatments are not sufficient or are contraindicated. 

bepridil is used to manage certain cardiac arrhythmias, including ventricular arrhythmias, where it can help stabilize the heart’s electrical activity. 

Drug Interaction

Adverse Reaction

Frequency not defined 

dizziness 

bradycardia 

edema 

nausea 

dyspnea 

palpitations 

headache 

drowsiness  

QT prolongation 

CHF  

nervousness 

rash 

weakness 

psychiatric disturbances 

insomnia 

tremor 

sexual dysfunction 

GI disturbances 

tinnitus 

rhinitis 

paraesthesia 

blurred vision 

dyspnoea  

diaphoresis 

akathisia 

cough 

flu syndrome 

Black Box Warning

Black Box Warning: 

None 

Contraindication / Caution

Contraindication/Caution: 

Contraindications: 

• Hypersensitivity 
• Long QT-syndrome 
• Concomitant use with QT-prolongers 
• Significant bradycardia 
• Severe Heart Failure 

Cautions: 

• Renal impairment 
• Hepatic impairment 
• Elderly patients 
• Electrolyte imbalance  
• Pregnancy 
• Lactation 

Pregnancy / Lactation

Pregnancy consideration:  

It is contraindicated during pregnancy. 

Breastfeeding warnings:  

No data is available. 

Pregnancy category: 

• Category A: Satisfactory and well-controlled studies show no risk to the fetus in the first or later trimester. 
• Category B: No evidence of risk to the fetus is found in animal reproduction studies, and there are not enough studies on pregnant women. 
• Category C: Adverse effects on the fetus found with evidence in animal reproduction studies and no adequate evidence for a human product; Pregnant women must take care of the potential risks. 
• Category D: There is adequate data with sufficient evidence of human fetal risk from various platforms. However, despite potential dangers may be used only in emergencies for potential benefits. 
• Category X: Drugs listed in this category outweigh the risks over benefits. The drug is not for pregnant women. 
• Category N: No data for the drug under this category is available. 

Pharmacology

Pharmacology: 

bepridil exerts its pharmacological effects by blocking L-type calcium channels in cardiac and smooth muscle cells. These channels are responsible for the entry of calcium ions into the cells during depolarization, which is essential for muscle contraction. 

By inhibiting calcium influx through these channels, bepridil reduces myocardial contractility (the force of the heart’s muscular contractions). This results in decreased oxygen demand by the heart, making it helpful in treating angina pectoris, especially in cases where other treatments are insufficient or contraindicated. 

Pharmacodynamics: 

By inhibiting calcium influx through these channels, bepridil reduces the entry of calcium ions into cardiac muscle cells during the stagnant phase of the cardiac action potential. This leads to a reduction in myocardial contractility (the force of the heart’s muscular contractions), which results in decreased oxygen demand by the heart. 

Pharmacokinetics: 

Absorption 

bepridil is administered orally, typically in the form of tablets or capsules. After oral ingestion, the drug is absorbed from the gastrointestinal tract into the bloodstream. The rate and extent of absorption may vary among individuals. 

Distribution 

bepridil is distributed throughout the body, including the heart and other tissues. Due to its lipophilic nature, it can cross cell membranes and enter various organs and tissues. The drug’s distribution is influenced by blood flow to different tissues and protein binding in the bloodstream. 

Metabolism 

bepridil undergoes extensive metabolism in the liver. The primary metabolic pathway involves cytochrome P450 (CYP) enzymes, particularly CYP3A4. The drug is metabolized into several metabolites, some of which may also have pharmacological activity. 

Elimination and Excretion 

The elimination of bepridil and its metabolites occurs mainly through the kidneys. The drug and its metabolites get excreted in the urine. The elimination half-life of bepridil is relatively long, ranging between 20 to 40 hours. 

Adminstartion

Administration 

bepridil is administered orally, taking the form of tablets or capsules. 

Patient Information Leaflet

Patient information leaflet 

Generic Name:  bepridil 

Why do we use bepridil? 

bepridil was used to manage chronic stable angina pectoris, a condition characterized by chest pain or discomfort by the reduction of blood flow to the heart muscle.

By blocking calcium channels, bepridil reduces the force of the heart’s muscular contractions, lowering the heart’s oxygen demand and relieving chest pain. 

It is also prescribed for treating certain cardiac arrhythmias, particularly those involving irregular heart rhythms. Its action on calcium channels can help stabilize the heart’s electrical activity.