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Archive » 1993 » 1 » | Archive » Medical field » Fields » Pharmacology and Experimental Toxicology »

The pharmacology of calcium antagonists

 
Abstract:

This post is also available in: enEnglish slSlovenščina (Slovenian)

Calcium antagonists constitute a chemically 
and pharmacologically diverse group of drugs. Chemically, at least four major types of calcium antagonists can 
be distinguished; they include phenylalkylamines, dihydropyridines, benzothiazepines and piperazines. As a
group they share the common property of slowing the 
transmembrane entry of calcium ions through either 
voltage-activated, or (probably) receptor operated, ion
 selective channels. They differ from one another also in 
terms of their tissue specificity and selectivity. Different
 types (L, T, N) of calcium channels have been identified 
and their distribution in different tissues is specific. The 
molecular properties and the differential binding characteristics of the subgroups of calcium antagonists have
 been defined. At least one of calcium antagonists, diltiazem, has an intracellular action. All calcium antagonists
 share the ability to dilate blood vessels, but there is a 
marked difference in potency and selectivity, even within 
individual subgroups. The dihydropyridines are relatively 
selective antagonists of vascular smooth muscle cell 
calcium uptake. Their ability to inhibit myogenic vascular
 tone contributes to their predominant in vivo effect on
 vascular beds characterized by a relatively high myogenic
 tone, such as the coronary and skeletal muscle beds. Additional mechanisms contributing to the antihypertensive action of dihydropyridines include interference with 
neural control of circulation, as well as intrarenal actions 
to promote electrolyte and water excretion. In myocardium, the tissue protecting effects of calcium antagonists,
 especially the dihydropyridine-based group, in the presence of hypertension involve not only reduction of hypertrophy, but they also reduce ischemia-induced injury and
 the incidence of damage due to lipid peroxidation. Other 
possible therapeutic uses of calcium antagonist include
 prevention of atherogenic changes, treatment and prevention of acute asthma, prevention of consequences of
 cerebral ischemia and vasospasm, anticonvulsant therapy, prophylactic therapy of migraine, attenuation of acute 
renal failure and slowing of the progression of chronic 
renal failure, uterine relaxation, and treatment of some 
gastrointestinal disorders.

Authors:
Budihna Metka V

Keywords:
calcium channel blockers - pharmacology

Cite as:
Med Razgl. 1993; 32: 65–86.
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