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Experimental and clinical effects of isradipine relevant to atherosclerosis
F Bernini1, M R Soma, A Corsini
1Institute of Pharmacology and Pharmacognosy, University of Parma, Italy.
Abstract:
A number of studies in experimental animal models have demonstrated the potential direct antiatherosclerotic effects of calcium antagonists. This class of compounds can influence several processes that are involved in the development of atherosclerotic lesions. This action is independent of either blood pressure reduction or hypercholesterolemia. A major problem encountered from the experimental data are the high doses used, which are several times higher than those used in the treatment of humans. One notable exception to this problem is the second-generation calcium antagonist isradipine, which exerts a direct antiatherosclerotic effect in rabbits at doses similar to those used in the clinic. Thus, this review is a summary of the effects and mechanisms of the antiatherosclerotic activity of isradipine.
Insights
Second-generation calcium antagonist isradipine shows direct antiatherosclerotic effects in animal models at clinically relevant doses. This review summarizes its mechanisms against atherosclerosis, independent of blood pressure or cholesterol levels.
Area of Science:
- Pharmacology
- Cardiovascular Research
- Medical Chemistry
Background:
- Calcium antagonists can directly impact atherosclerotic lesion development.
- Their antiatherosclerotic effects are independent of blood pressure reduction or hypercholesterolemia.
- High doses in experimental models limit clinical translation.
Purpose of the Study:
- To review the antiatherosclerotic effects of isradipine.
- To summarize the mechanisms underlying isradipine's activity.
- To highlight isradipine as an exception regarding effective clinical dosing.
Main Methods:
- Review of experimental animal model studies.
- Analysis of isradipine's effects at clinically relevant doses.
- Examination of mechanistic pathways involved in atherosclerosis.
Main Results:
- Isradipine demonstrates direct antiatherosclerotic effects in rabbits.
- These effects occur at doses comparable to human clinical use.
- Isradipine's action is distinct from its effects on blood pressure or cholesterol.
Conclusions:
- Isradipine is a promising agent for direct antiatherosclerotic therapy.
- Its efficacy at clinical doses warrants further investigation.
- Understanding isradipine's mechanisms can inform future atherosclerosis treatment strategies.