The effects of antianginal drugs, especially arylalkylamines and structurally related derivatives, on 3H-batrachotoxinin-A 20-alpha-benzoate (3H-BTX-B) binding and on 3H-tetracaine binding were studied on rat synaptosomal and heart membrane preparations. The effect of the same drugs on the Na+ influx induced by protoveratrine B was studied on the rat synaptosomal preparation. Antianginal drugs tested inhibited 3H-BTX-B binding in rat synaptosomes, arylalkylamine derivatives being the most potent: IC50 values were 27 nM for flunarizine, 32 nM for prenylamine, 79 nM for cinnarizine. Similarly, these drugs were the most potent when tested in cardiac membrane preparations. All the drugs tested were very weak inhibitors of 3H-tetracaine binding (IC50 ranging from 0.01 mM to more than 1 mM) except for guanabenz, which was more potent (IC50:0.3 microM on the synaptosomal preparation). The various drugs tested inhibited the 22Na+ influx induced by protoveratrine B, with IC50 values ranging from 15 microM (prenylamine) to 110 microM (verapamil), with the exception of nifedipine which had an IC50 of more than 0.1 mM. The inhibition of 22Na+ influx correlated well with the inhibition of 3H-BTX-B binding. These findings suggest that some antianginal drugs, especially the arylalkylamines may have, in addition to their calcium antagonist activity, direct effects on sodium channels.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1007/BF00177720 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Bridging the Gender Gap in Cardiovascular Medicine: Addressing Drug Intolerances and Personalized Care for Women with Angina/Ischemia with Non-Obstructive Coronary Artery Disease.
J Cardiovasc Dev Dis
November 2024
Robert Bosch Krankenhaus, Department of Cardiology and Angiology, Auerbachstr. 110, 70376 Stuttgart, Germany.
Gender medicine has increasingly underscored the necessity of addressing sex-based differences in disease prevalence and management, particularly within cardiovascular conditions and drug intolerance. Women often present cardiovascular diseases distinctively from men, with a higher prevalence of non-obstructive coronary artery disease and varied ischemic manifestations, such as coronary microvascular dysfunction and epicardial or microvascular coronary spasm. This disparity is further exacerbated by elevated drug intolerance rates among women, influenced by hormonal, genetic, and psychosocial factors.
View Article and Find Full Text PDFStable Angina Pectoris: A Review of Pathophysiology, Diagnosis, and Its Management.
J Assoc Physicians India
November 2024
Director, Department of Medical Affairs, Dr Reddy's Laboratories Ltd., Ameerpet, Hyderabad, Telangana, India.
Article Synopsis
- India faces a growing epidemic of cardiovascular diseases, particularly coronary artery disease, due to rapid urbanization and globalization, with over 7 million deaths annually from CAD.
- Key challenges in low- and middle-income countries include a lack of awareness about risk factors, healthcare access, and affordability of treatment.
- Effective management of angina pectoris involves collaboration among patients and healthcare providers and utilizes both first-line (like CCBs and β-blockers) and second-line antianginal medications to improve patient outcomes.
New insights on pharmacological and therapeutic potentials of trimetazidine beyond anti-anginal drug: A comprehensive review.
Eur J Pharmacol
December 2024
Department of Pharmacology, Therapeutics & Toxicology, Faculty of Basic Medical Sciences, College of Medicine, University of Lagos, Idi-Araba, P.M.B. 12003, Lagos, Nigeria. Electronic address:
Trimetazidine (TMZ) is a beneficial and well-tolerable anti-anginal drug which has protective action towards ischemia and reperfusion injury. TMZ performs its anti-ischemic effect by modifying cardiac metabolism without shifting the hemodynamic functions, so it represents an outstanding complementary perspective to the general angina treatment. TMZ possesses a positive impact on the inflammatory profile, and also endothelial function furthermore displays various benefits through minimising the number, as well as the intensity of angina strikes and ameliorating the clinical indication and symptoms of myocardium ischemia.
View Article and Find Full Text PDF"Emerging clinical approaches in diabetic cardiomyopathy: insights from clinical trials and future directions".
Acta Diabetol
January 2025
Department of Clinical Research, Hindu Mission Hospital, Tambaram, Chennai, 600045, Tamil Nadu, India.
Aim: We aim to explore the potential of diverse treatments, including perhexiline, calcium channel blockers, anti-hypertensives, PDE5 inhibitors, anti-anginal drugs, aldose reductase inhibitors, and SGLT-2 inhibitors, supported by clinical evidence. Additionally, this review seeks to identify novel therapeutic targets and future avenues for improving cardiovascular outcomes in diabetic populations.
Method: We performed a comprehensive literature review of English-language studies across multiple electronic databases, such as PubMed, ScienceDirect, Scopus, and Google Scholar, focusing on clinical trials.
The Role of Ranolazine in the Treatment of Ventricular Tachycardia and Atrial Fibrillation: A Narrative Review of the Clinical Evidence.
Biomedicines
July 2024
1st Department of Medicine, Medical School, University of Pécs, Ifjúság útja 13, H-7624 Pécs, Hungary.
Cardiac arrhythmias are among the leading causes of morbidity and mortality worldwide. While antiarrhythmic drugs traditionally represent the first-line management strategy, their use is often limited by profound proarrhythmic effects. Several studies, including randomized control trials (RCTs), have demonstrated the antiarrhythmic efficacy of ranolazine, which is registered as an antianginal agent, while also establishing its safety profile.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!