ACE inhibitors
This information is not intended for purposes of treatment without physician.
Description of the pharmacological group
The medicines, which reduce activity RAAS, ACE inhibitors
Reninangiotensin-aldosterone system considers as the circulatory neuroendocrine system, which plays extremely important role in the regulation system AD and water balance. The normally functioning system RAAS can be considered as the system, which plays the role “of first aid” in the organism with the hemorrhages, sharp drop AD and so forth however the hyper-activity of this system entails the development of such severe illnesses as hypertonic disease, chronic heart insufficiency, disturbance of the function of kidneys.
Creation and putting into clinical practice of the medicines, which suppress the activity of the angiotensin-converting enzyme, made it possible to block not only the activity of circulatory RAAS, but also to render the essential organic protective effect, caused by the oppression of the hyper-activity of local (woven) RAAS.
These medicines were called ACE inhibitors. The history of the creation of ACE inhibitors is sufficiently interesting. In 1965, a brazilian biologist S. Ferreira isolated from the poison of the rattlesnake of bothrops of jararaca the connection, which possesses the ability to block the transformation of angiotensin of the I into angiotensin II, which was called name bradykinetic factor. In 1975, the employees of the American pharmaceutical firm "Bristol-Myerts Squibb" D. Cushman and M. Ondetti synthesized the first ACE inhibitor ACE - Captopril.
At present in the wide clinical practice is inculcated the sufficiently large number of highly effective ACE inhibitors, which subdivide into the ACE inhibitors of the first generation - Captopril (sin.: Capoten) and the second generation - fosinopril (sin.: monopril), Coversyl (sin.: prestarium, perindopril), Enalapril (sin.: renitek, ENAP, Vasotec) and other
Preparation Captopril, which relates to the ACE inhibitors of the I generation, acts for 5 -6 h, whereas the ACE inhibitors of the II generation act 24 h and more. The majorities of the ACE inhibitors of the II generation relate to the group of “prodrugs”, i.e., they are not biologically active, but they are metabolized in the liver to the biologically active substances. Thus, for instance, enalapril is not biologically active, but it is metabolized in the liver to biologically active Enalapril (Vasotec), and which has the properties of AMF inhibitors.
Suppressing activity ACE, its inhibitors block formation in the organism of angiotensin of the II and thus renders the vaso-dilating action, they prevent the delay of sodium ions of Na+ and water in the organism, decrease the volume of circulant and the general peripheral resistance of vessels, which entails the normalization of level AD. In parallel with this occurs the blockade of local RAAS, which is clinically manifested by the decrease of the hypertrophy of heart muscle and vascular wall, by the normalization of the functional activity of kidneys and so forth
The suppression of the activity of the angiotensin-converting enzyme is also accompanied by the normalization of the functional activity of kallikrein-kinin system, which also contributes to the vaso-dilation of vascular channel, including to an improvement in the coronary blood flow.
In the clinical practice the ACE inhibitors in essence use for treating of hypertonic disease, chronic heart insufficiency. There are data about the high efficiency of ACE inhibitors in the complex therapy coronary heart disease, including of sharp myocardial infarction.
Besides the ACE inhibitors are at present in the clinical practice inculcated the blockers of AT1- receptors - Losartan (sin.: Cozaar) and by others preventing interaction of angiotensin of the II with AT1- receptors, of medicines of this group they block the realization of the effects, caused by the hyper-activity of both the circulatory, and woven RAAS, they suppress vasoconstriction, they contribute to the decrease of ion concentration of sodium of Na+ in the plasma of the blood, they possess diuretic activity, decrease the hypertrophy of myocardium and vascular wall.
However, in contrast to the ACE inhibitors they do not restore the activity of kallikrein-kinin system, since they do not influence the level of angiotensin of the II in the plasma blood.
In the clinical practice the antagonists of AT1- receptors use from the same indications, as ACE inhibitors. These medicines act prolongedly; therefore them use 1 2 times in a 24 hour period.
ACE inhibitors are used to treat diseases of the vessels of the brain and peripheral vessels