From this article you will learn: what are ACE inhibitors( abbreviated as ACE), how do they reduce blood pressure? Than similar and than differ from each other medicines. List of popular drugs, indications for use, mechanism of action, side effects and contraindications to ACE inhibitors.
Contents of the article:
- The difference between ACE inhibitors
- List of popular drugs
- Indications for use
- Mechanism of action
- Side effects of
- Contraindications to the use of
ACE inhibitors are called a group of drugs that block a chemical contributing to vasoconstriction and pressure increase.
Human kidneys produce a specific enzyme, renin, from which a chain of chemical transformations begins, leading to the appearance in tissues and blood plasma of a substance called "angiotensin converting enzyme", or angiotensin. What is angiotensin? It is an enzyme that has the property of narrowing the vascular walls, thereby increasing blood flow and pressure. At the same time, its increase in blood provokes the production of adrenal glands by other hormones that retard sodium ions in tissues, increase vasospasm, provoke heartbeat, increase the amount of fluid in the body. It turns out a vicious circle of chemical transformations, as a result of which arterial hypertension becomes stable and contributes to damage to the vascular walls, the development of chronic cardiac and renal insufficiency.
The ACE inhibitor( ACE inhibitor) interrupts this chain of reactions by blocking it during the transformation stage into an angiotensin-converting enzyme. Simultaneously, it promotes the accumulation of another substance( bradykinin), which prevents the development of pathological cellular reactions in cardiovascular and renal failure( intensive division, growth and death of myocardial cells, kidneys, vascular walls).Therefore, ACE inhibitors are used not only to treat arterial hypertension, but also for the prevention of cardiac and renal failure, myocardial infarction, stroke.
ACE inhibitors are one of the most effective antihypertensive drugs. Unlike other drugs that dilate blood vessels, they prevent vascular spasm and act milder.
ACE inhibitors are prescribed by a physician-therapist, based on the symptoms of hypertension and concomitant diseases. Do not recommend taking and setting a daily dose yourself.
Than ACE inhibitors differ from each other
ACE inhibitors have similar indications and contraindications, the mechanism of action, side effects, but differ from each other:
- is the starting substance in the drug base( the active part of the molecule( the group) that determines the duration of action plays a decisive role);
- activity of the drug( the substance is active, or it needs additional conditions to start work, as far as it is available for absorption);
- excretion methods( which is important for patients with severe liver and kidney diseases).
Starting substance
The starting substance affects the duration of the drug in the body, with the appointment it allows you to choose the dosage and determine the time interval through which you need to repeat the reception.
| Active group of | ACE inhibitor | action mechanism Mechanism of action | |
|---|---|---|---|
| With sulfhydryl group( 1st generation) | Zofenopril, captopril, pivalo pril | Sulphydryl group enhances the effect of ACE inhibitors, but easily oxidizes, therefore a short time occurs | |
| With carboxyl group( 2 generations) | Lisinopril, enalapril, ramipril, perindopril | Action time is medium, differ in high ability to penetrate into tissues | |
| With phosphinyl group( 3 generations) | Ceronapril, fosinopril | Dystvuyut long time, have high ability to penetrate and accumulate in tissues |
Ramipril available in a dosage of 2.5 mg, 5 mg and 10 mg activity mechanism plays a decisive role in the conversion of the chemical active:
| ACE inhibitors | Activity of the drug |
|---|---|
| Preparations of the 1st class( captopril) | Fat-soluble, enter the body in active form, transform into the liver, appear in an altered form, penetrate well through cell barriers( bioavailable) |
| Fasinopril | Fat-soluble,are activated as a result of chemical reactions in the kidneys or liver, are removed in a modified form, bioavailable |
| Preparations of the 3rd class( lisinopril, ceronapril) | Water-soluble, enter the body in active form,in the liver are not transformed, are released unchanged, bioavailable to a lesser extent. |
Lisinopril is released at a dosage of 5, 10 and 20 mg. Methods of elimination
There are several ways to remove ACE from the body:
- Drugs that are excreted by the kidneys( captopril, lisinopril).
- The most part is excreted by the kidneys( 60%), the rest - by the liver( perindopril, enalapril).
- Equally excreted by the kidneys and liver( fosinopril, ramipril).
- Most of the liver( 60%, trandolapril).
This allows you to select and prescribe medication for patients with severe kidney or liver disease.
Due to the fact that generations and classes of drugs do not coincide, the mechanisms of action( pharmacokinetics) may differ insignificantly from agents from the same series( for example, with the sulfhydryl group).Typically, these differences are specified in the instructions and contain information on the effect of food on absorption( before meals, after), the methods of excretion, the time during which the substance is retained in plasma and tissues, half-lives and decay( transformation into an inactive species), etc. Information is important to a specialist for the proper administration of a medicine.
The list of popular ACEIs
The list of drugs includes a list of the most common drugs and their absolute counterparts.
| Generation | international drug name | Trade name( absolute analogs) |
|---|---|---|
| 1 generation( sulfhydryl group) | Captopril | Katopil, hood, blokordil, angiopril |
| Benazepril | Benzapril | |
| Zofenopril | Zokardis | |
| 2 generation drugs, ACE inhibitors( with the carboxyl group) | Enalapril | Vasolapril, enalacor, enam, renipril, renitek, enap, invol, corandil, berlipril, bapopril, myopril |
| Perindopril | Pre -arium, perinpress, paravevel, giernika, stopress, arentopres | |
| Ramipril | Dilaprel, vazolong, peers, korpril, ramepress, Hart, tritatse, amprilan | |
| Lisinopril | Diroton, diropress, irumed, liten, irumed, sinopril, Dapril, lizigamma, prinivil | |
| Cilazapril | Prilazid, inhibeys | |
| moexipril | Moeks | |
| Trandolapril | Gopten | |
| Spirapril | Quadropril | |
| Quinapril | Akkupro | |
| 3 generation( phosphinyl group) | Fosinopril | Fozinap, fozikard, monopril, fozinotek |
| ceronapril |
FaThe pharmaceutical industry produces combined medications: ACE inhibitors in combination with other substances( with diuretics - kaptopres).
Enap H is a combined preparation. In the composition contains enalapril and potassium-sparing diuretic( hydrochlorothiazide) Indications for use
In addition to the pronounced hypotensive effect, ACE inhibitors have some additional qualities: they positively influence the cells of the vascular walls and myocardial tissues, prevent their degeneration and mass death. Therefore, they are used for the treatment of hypertension and the prevention of concomitant pathologies:
- acute or transferred myocardial infarction;
- ischemic stroke;
- chronic renal failure;
- chronic cardiovascular failure;
- ischemic disease;
- diabetic nephropathy( kidney damage in diabetes mellitus);
- reduced myocardial contractility;
- peripheral vascular pathology( obliterating atherosclerosis of the extremities).
ACE inhibitors are widely used in the treatment of ischemic stroke In the presence of a complex of diseases from the list, ACE inhibitors remain the preferred drugs for a long time, they have many advantages over other antihypertensive agents.
With constant use, they:
- significantly reduce the risk of cardiovascular complications in the presence of hypertension( myocardial infarction)( 89%), against hypertension and diabetes( 42%);
- are capable of inducing the reverse development of hypertrophy( increasing the thickness of the walls) of the left ventricle and preventing the dilatation of the walls( dilatation) of the heart chambers;
- in appointments with diuretics do not need to control the level and apply potassium preparations, since this indicator remains normal;
- increase the glomerular filtration rate against a background of renal failure( 42-46%);
- mediate rhythm regulation and anti-ischemic action.
The physician can prescribe ACE inhibitors in combination with diuretics( diuretics), beta blockers, or other medications to achieve a more pronounced effect.
Mechanism of action
Action for persistent hypertension( arterial hypertension)
Drugs block the conversion of angiotensin, which has a pronounced vasoconstrictive effect. The effect extends to plasma and tissue enzymes, so it provides a mild and prolonged hypotensive effect.
This is the main mechanism of action. Next, you will learn about the additional effects of ACE inhibitors in different pathologies.
Action for cardiovascular failure, IHD, myocardial infarction,
stroke. Due to lowering of angiotensin level, the amount of another substance( bradykinin) that prevents pathological division, growth, degeneration and mass death of cardiac muscle cells and vascular walls due to oxygen starvation. With the regular administration of ACE inhibition significantly slows down the process of thickening of the myocardium and vessels, expansion of the heart chambers that appear against the background of persistent hypertension.
In renal failure, kidney damage in diabetes mellitus
, ACE inhibits the production of specific adrenal enzymes that inhibit sodium ions and water indirectly. They help to reduce edema, restore the inner layer( endothelium) of the vessels of the renal glomeruli, reduce renal filtration of the protein( proteinuria) and pressure in the glomeruli.
In atherosclerosis( due to hypercholesterolemia) and increased coagulation of blood
Because of the ability of ACE inhibitors to release nitric oxide, clotting of platelets is reduced in the blood plasma and the level of fibrins( proteins participating in the formation of thrombus) is normalized. Because of the ability to suppress the production of adrenal hormones, which increase the level of "bad" cholesterol in the blood, the drugs have antisclerotic effect.
Side effects of
ACE inhibitors rarely cause side effects, they usually tolerate them quite well. However, there are a number of symptoms and conditions, when you need to consult a doctor and replace ACE inhibitors with other drugs.
| Side effect | Description | |
|---|---|---|
| Appearance of dry cough | Regardless of the dose, a dry, painful cough in 20% of patients( passes 4-5 days after cancellation) | |
| Allergy | Skin manifestations of an allergic reaction in the form of rash, hives, itching, redness, swellingQuincke( 0.2%) | |
| electrolyte imbalance Hyperkalemia with potassium-sparing diuretics( increase in the amount of potassium) | ||
| Effect on the liver | Development of cholestasis( congestion of bile in the gallbladder) | |
| Arterieshypotension | weakness, weakness, decrease in blood pressure, which is regulated by dose reduction, cancellation of diuretics | |
| Dyspepsia | Nausea, vomiting, diarrhea | |
| Kidney disorders | Increased creatinine in blood, glucose level in urine, acute renal failure( kidneys can refuse in the elderlypeople with heart failure) | |
| Taste distortion | Decreased sensitivity or total loss of taste | |
| Change in blood formula | Increased amount of neutrophils |
Contraindications to
| Contraindicated in ACE inhibitors for patients with concomitant pathologies | Do not prescribe medicines |
|---|---|
| Stenosis( constriction of the aorta)( a large vessel from which blood enters the large circulatory system from the left ventricle of the heart) | In pregnancy, they can provoke lack of amniotic fluid, growth retardation,abnormal formation of the bones of the skull, lungs and fetal death |
| Stenosis of the renal arteries | During breastfeeding the baby |
| Severe renal insufficiencymore than 300 μmol / l) | With individual intolerance |
| Severe arterial hypotension | |
| Increased potassium level in the blood( more than 5.5 mmol / l) |
It is not recommended to use ACE inhibitors in combination with drugs that suppress immunity, as well as cell growth and division,since the number of leukocytes in the blood can decrease to a critical level.
