Vasodilator drugs vasodilators use representatives mechanism of action

Vasodilation is a natural reaction of the human body to physical activity, massaging movements or certain chemicals. In the absence of pathology, such a process is necessary for the body to provide tissues with a large amount of energy.

If there is a violation of the normal functioning of the vascular system and the walls of the vessels lose their former elasticity, a significant decrease in lumen can be observed. In this case, the use of vasodilators is necessary.

The use of vasodilators can reduce resistance in blood vessels. The active ingredients of the drugs make the walls of the vessels relax. From this they expand, the lumen increases.

Depending on the properties of a particular medication, the effect may be on small arteries or large vessels. The tool should be selected individually by the attending physician based on the diagnosis and patient characteristics.

The list of peripheral drugs includes:

  1. Nitroglycerin. This is a synthetic drug that has a fast vasodilating effect. The maximum concentration of the active substance in the blood is observed 15 minutes after administration. The action lasts at least an hour. Most often used to stop and prevent attacks of heart failure. Available in the form of sublingual tablets, alcohol solution and capsules. Its use occasionally leads to side effects such as anxiety, headache, tinnitus, and tachycardia. In case of an overdose, it can provoke a sharp drop in blood pressure, slowed breathing, tachycardia. The drug is contraindicated in case of individual intolerance, coronary thrombosis, severe anemia.
  2. Molsidomin. It is used for angina pectoris, acute myocardial infarction, circulatory disorders in a small circle. Available in tablet form. The maximum daily dose is 25 mg. Contraindications to use are hypersensitivity, the first trimester of pregnancy, vascular collapse, cardiogenic shock. In some cases, the use of the drug can provoke the appearance of headaches, slowing down the speed of reactions, nausea, an allergic reaction.
  3. Isosorbide Mononitrate. It is used for spasm of peripheral arteries, hypertension, angina pectoris. Available in the form of tablets and capsules. It can not be used for individual intolerance, glaucoma, acute infarction, pregnancy, liver failure. The maximum allowable dose per day is 80 mg.

Before using the drug, carefully read the attached instructions and consult your doctor.

When it comes to such a large, diverse group of drugs, I want to trust well-proven remedies. You can focus on the following top ten vasodilators with prices:

  1. No-shpa is a drotaverine-based myotropic. It removes any angiospasm, which dilates blood vessels, is quickly absorbed by the body. The drug of choice for painful periods. (Cost from 100 rubles)
  2. Papaverine, a myotropic that relieves spasms of internal organs, practically does not enter the brain, possesses along with vasodilating – sedative properties, in late pregnancy it is recommended for relieving uterine hypertonicity, but is prohibited in glaucoma and atrioventricular block. (from 40 rubles)
  3. Eufillin is the basis of theophylline, the drug is prioritized by bronchospasm, an asthmatic component, it stimulates blood thinning, is not used for arrhythmias, but has proven its effectiveness as a vasodilator for angiospasm. (from 15 rubles)
  4. Duspatalin is the active substance mebeverin, used for intestinal cramps, tablets reduce the ability to concentrate, but well expand the peripheral arteries. (from 550 rubles)
  5. Buscopan – an antispasmodic nootropic based on hyoscine butyl bromide, allergic, can cause anuria. The drug is not recommended for fructose intolerance. (from 350 rubles)
  6. Spazmalgon is a combination agent that demonstrates a vasodilator, anti-inflammatory, analgesic effect. It is forbidden for angina pectoris. (from 110 rubles)
  7. Teotard – theophylline, is indicated for relieving asthma attacks, with pulmonary heart, night apnea. Indirectly reduces blood pressure. Contraindicated in case of hypersensitivity to the drug and with coronary insufficiency. (from 150 rubles)
  8. Dibazole is the active substance of bendazole, it is a myotrop, relaxing the smooth muscles of internal organs, blood vessels, showing a vasodilating effect. Tablets are contraindicated in diabetes. (from 20 rubles)
  9. Cordaflex – the active substance nifedipine, a calcium channel blocker, reduces blood pressure, stimulates coronary blood flow, widening the lumen of blood vessels, the drug is contraindicated in tachycardia. (from 85 rubles)
  10. Diltiazem is a calcium blocker, it is able to correct the rhythm of the heart, it stops myocardial hypoxia due to vasodilation. (from 115 rubles)

To choose the right vasodilator drug, you need to know the cause of the pathology, so you just can not do without a doctor, a clinical and laboratory examination. Today, everyone knows how to count money in their wallet, so exclude waste in a responsible attitude to health.

The mechanism of action of peripheral vasodilators is different, this group includes drugs:

  • blocking alpha adrenergic receptors;
  • calcium ion antagonists;
  • affecting smooth myofibrils of arterioles;
  • converting enzyme inhibitors.

Despite the different mechanism of action, all drugs affect post- and preload of the myocardium. Pharmacodynamic effects are manifested by a decrease in blood flow to the heart due to an increase in the capacity of the venous part of the vascular bed, and minute volume of blood, due to an increase in the capacity of the arterial component of the autonomic vascular system.

The accumulation of cyclic adenosine monophosphate in the cellular tissue of smooth muscles of blood vessels and in blood cells, as well as the inhibition of phosphodiesterase, is the basis of the mechanism of action of Pentoxifylline, a peripheral vasodilator, the intake of which:

  • It improves symptoms in cases of cerebrovascular accident by reducing the overall peripheral resistance and a slight expansion of the coronary vessels. Has a slight vasodilating effect.
  • It inhibits the aggregation of red blood cells and platelets, stimulates fibrinolysis, reduces the concentration of fibrinogen in the blood plasma, improving its viscosity.
  • Disruption of blood flow, with ischemic origin, acute and chronic.
  • Damage to the brain is discirculatory and atherosclerotic.
  • Failure of peripheral blood flow, occurring against the background of inflammatory, as well as atherosclerotic and diabetic processes.
  • As a symptomatic remedy to cure the consequences that arose after cerebrovascular accident.
  • Failure of the middle ear functions of vascular origin, which is accompanied by hearing loss.
  • Violation of blood circulation in the vessels of the eye.
  • Trophic tissue disorders provoked by a malfunction of venous and arterial microcirculation.

According to the instructions for use of “Pentilin” and other drugs that have INN pentoxifylline, they are prohibited for use with:

  • Hypersensitivity to pentoxifylline.
  • Pregnancy.
  • Breastfeeding.
  • Retinal hemorrhage.
  • Heavy bleeding.
  • Acute myocardial infarction.
  • Under the age of eighteen.

Adverse events may occur from:

  • hemostatic system and cardiovascular;
  • subcutaneous fat and skin;
  • Central nervous system;
  • digestive system.

As well as allergic reactions and changes in some laboratory indicators.

“Vinoxin MV” has a selective vasoregulatory effect on cerebral circulation. Due to the intense oxidation of glucose, it establishes the metabolism of the brain. Oxygen supply to neurons is improving. The peripheral resistance of the vessels of the brain is stabilized. In addition, the drug does not adversely affect the liver and kidneys. Doctors recommend Vinoxin MV to normalize cerebral circulation in case of disorders:

  • mental
  • concentration of attention;
  • memory;
  • vision and hearing of vascular origin;
  • cranial post-traumatic;
  • cerebral (after cerebral ischemia);
  • and others.

The duration of the course of treatment and is selected individually by the doctor. Its use is not recommended for pathologies that provoke an increase in intracranial pressure, acute stroke, heart rhythm disturbances, as well as children, pregnant and lactating women. Side effects are minor. Do not increase the dose recommended by the doctor. With prolonged use, monitoring of the liver is necessary.

At present, a large number of drugs with selective action have been developed that are successfully used for the treatment of heart failure, as well as hypertension. The following is a list of vasodilator preparations:

  • “Agapurin.”
  • “Benciclamana Fumarate.”
  • Duzofarm.
  • Complmin.
  • Nicergoline.
  • The Pentagon.
  • “Pentoxifylline.”
  • Pentilin.
  • Pentomere.
  • “Radomin.”
  • “Ralofect.”
  • “Sermion.”
  • “Furazolidone” and others.

Each drug has a different pharmacological effect. For the successful treatment of pathology, it is important to choose the right tool. In order to avoid unpleasant consequences, before using the medicine, you should read the instructions for use and follow all the recommendations of your doctor.

General information

Due to the intake of drugs of this group, blood vessels expand, which reduces both the load on the heart muscle and its oxygen demand. This fact allows you to use them as antianginal agents. Peripheral vasodilators include medications that act on resistive vessels, they are indicated for the treatment of hypertension.

The use of drugs included in this group should be carried out under the supervision of the attending doctor, since they can significantly reduce blood pressure, and worsen the blood supply to the heart.

Features of the use of vasodilators for children

Vasodilation, that is, vasodilation, allows you to achieve the following effect:

  1. Decreased increased tone of the walls of blood vessels.
  2. Increased clearance, which reduces blood circulation and pressure.
  3. Reducing the load on the heart muscle.
  4. Improving the nutrition of tissues and accelerating the process of their recovery in case of damage.

Vasodilators are widely used for heart failure, local tissue necrosis, atherosclerosis. In some cases, they are used to correct high blood pressure.

One of them is balloon vasodilation, that is, the installation of a special spray can in a vessel.

Like any medication, vasodilators have a number of side effects. These include:

  1. Constant feeling of tiredness, weakness, lethargy.
  2. Increased intensity of contraction of the heart muscle.
  3. Bouts of nausea.
  4. Headache.
  5. Dizziness.
  6. Nasal congestion.

Such symptoms most often occur due to individual intolerance to the components of the product or improper use. If such side effects occur, consult a doctor.

The specialist will decide on a change in the drug or dose adjustment.

Vasodilator drugs of this group have a positive effect not only on arteries, but also on small capillaries of the brain. Thanks to this, full blood supply to the body is restored.

The list of vasodilators of this group is headed by:

  1. Hydralazine. The maximum concentration of the drug in the blood is reached 3 hours after administration. Its half-life is about three hours. Once in the liver, the drug is transformed, so for people with an inhibited acetylation process, the recommended dosage is slightly lower than the usual. The maximum daily dose is 400 mg. Among the side effects of such a remedy, tachycardia, swelling, headaches, and discoloration of the skin of the face are noted. Hydralazine is contraindicated in people with lupus erythematosus, gastric ulcer and atherosclerosis of cerebral arteries in advanced form.
  2. Vinpocetine. It copes well with cerebrovascular accident of various etiologies. Helps with impaired hearing and vision. It is produced in the form of tablets, as well as a solution for and injection. The maximum daily dose is 30 mg. The course of treatment with intravenous treatment is no more than two weeks. You can drink tablets for about a month. Side effects may occur, for example, nausea, dry mucous membranes of the mouth, dizziness, heartburn, excessive sweating. The drug is contraindicated in cardiac ischemia, pregnancy, hypersensitivity to the components, as well as significant arrhythmias.
  3. Nicergoline. It is used for chronic disorders of cerebral circulation. Available in tablet form. The maximum daily dose is 30 mg. It must be broken down into three steps. The duration of such therapy is at least two months. Improper administration of the drug leads to symptoms such as sleep disturbance, dizziness, skin itching, and digestive upset. You can not use this medication for people suffering from severe disorders of the liver, severe hypotension, and intolerance to the components of the drug.

It is necessary to choose a drug and its dosage based on the characteristics of the disease and the condition of the patient.

In childhood, such drugs are advisable to use only in the presence of serious pathologies. Most often, doctors prescribe myotropic drugs. These include:

  1. Benzohexonium. The drug is administered intravenously no more than 0,08 mg per 1 kg of a child’s weight.
  2. Papaverine. The maximum daily dose is 0,01 g. It is produced in the form of tablets, suppositories and injection.
  3. Dibazole It is permissible to give the child no more than 5 mg of the drug per day.

Such drugs help improve blood circulation, fight hydrocephalus and diseases of the cardiovascular system.

Before using vasodilators, it is necessary to undergo a medical examination and consult a doctor. Uncontrolled use of such funds can lead to negative consequences.

Venous vasodilators are indicated for overload of the pulmonary circulation, they:

  • reduce pressure in a small circle;
  • reduce diastolic expansion of the left ventricle;
  • reduce the return of venous blood to the heart;
  • reduce myocardial oxygen consumption.

Thus, peripheral vasodilators of this subgroup do not increase cardiac output, but only reduce pressure (pressure) in a small circle of blood circulation. Medicines with a predominant effect on small arteries reduce afterload, while they do not affect pressure in a small circle of blood circulation, that is, the level of preload does not change.

  • “Hydralazine” – with low cardiac output, with severe aortic or mitral regurgitation.
  • “Phentolamine” – in case of catecholamine crisis in individuals with pheochromocytoma.
  • Dihydropyridines – for the treatment of hypertension.

Medications with a simultaneous effect on venules and arterioles affect the pre- and afterload, so they are prescribed for the treatment of acute heart failure. And such a unique combination as “Hydralazine Isosorbide Dinitrate”, used in the treatment of chronic heart failure, within two years of administration helps to reduce the risk of mortality.

Depending on which artery of which area needs to be expanded, a treatment regimen is selected with certain vasodilators.

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For the brain

Group, representativesMaterials
Cerebral Vasodilators: Pentoxifylline, VinpocetineDrugs improve microcirculation, blood supply to the brain, stop hypoxia, expanding cerebral arteries
Calcium Antagonists: Verapamil, Amlodipine, NorvaskTablets correct excess calcium ions in the blood, eliminate hypoxia, normalize blood viscosity, vascular tone, showing vasodilating properties
Nootropics: Phenibut, Piracetam, NoopeptDrugs form resistance to hypoxia, activate the centers of the brain due to the normalization of the nutrition of neurons as a result of vasodilatation of capillaries
For rehabilitation after a stroke: Clopidogrel, CeraxonThe drugs normalize blood circulation, dissolve blood clots, accelerate the regeneration of brain cells, restore concentration due to the ability to expand the lumen of blood vessels, balance metabolism
Group, representativesMaterials
Nitrates: Nitroglycerin, Nitrong, SustakThe drugs stabilize the nutrition of the heart muscle, stop hypoxia, relieve retrosternal discomfort, normalize the heart rhythm, vasodilation serves as a prophylaxis for AMI
Antihypertensives: Atenolol, Renitec, EnalaprilMedicines correct vascular parameters of blood pressure, expanding arteries, relieve arrhythmia, relieve myocardium from oxygen starvation

Stenosis of the arteries of the lower extremities is a consequence of obliterating arteritis or thromboangiitis. An intermittent claudication is considered a sign of the disease: muscle hypoxia with pain that interferes with normal movement.

Group, representativesMaterials
Myotropes: Xanthinol nicotinate, Actovegin, Troxevasin, DetralexDrugs dilate arteries and veins, normalize blood flow
Antispasmodics: No-spa, Papaverine, Baralgetas, SpazmalgonTablets stop vascular spasm, relieve pain, hypoxia, normalize tissue nutrition

Given the basic properties of vasodilators, they are usually prescribed for:

  • arterial hypertension;
  • heart failure of varying severity, of different genesis;
  • intestinal cramps, colic;
  • pathology of the kidneys and urinary system;
  • encephalopathies;
  • VSD;
  • prostatitis;
  • arthrosis;
  • osteochondrosis.

Despite the variety of pharmacological groups and individual characteristics of each drug, there are general contraindications to the appointment:

  • hypotension of any form and stage;
  • children’s age (restrictions from a year to 5-6 years);
  • pregnancy, lactation;
  • CRF;
  • individual intolerance of components;
  • atherosclerotic plaques;
  • thrombosis.

Side effects in case of violation of the rules of admission are:

  • vertigo;
  • feeling unwell;
  • dry mucous membranes;
  • nausea
  • dyspepsia;
  • bleeding.

Separately, it is worth highlighting the symptom of robbery when blood flows through those vessels whose lumen is narrowed, reluctant, easily creating bypass collaterals. Areas that supply blood to damaged vessels remain in a state of shock readiness (they lack nutrition).

Hypertensive crisis, for example, can lead to the use by the body of only detours, while the usual blood supply is ignored, tissue areas are necrotic (AMI, stroke, kidney infarction). Therefore, the importance of vasodilator drugs in stabilizing the pathology is difficult to overestimate.

Classification of drugs

Means for the expansion of blood vessels are numerous, but at the same time the mechanism of their action, the way to adjust vascular tone is strictly individual. The narrowing of arteries and capillaries is the cause of serious deviations in the work of almost all internal organs, which often becomes very life-threatening. After all, the vascular system not only feeds all body tissues, it provides them with oxygen, removes spent metabolites, toxins to the outside.

Tablets (Tanakan, Omaron, Thiocetam) do not directly affect blood vessels, but they improve metabolism, microcirculation, inhibit platelet aggregation, and increase glucose susceptibility.

The drugs stabilize cell membranes, optimize the delivery of oxygen to the brain and nutrients, activate cortical connections (processes in the cortex and hemispheres of the brain)

Read more about new generation neuroprotective drugs and nootropics

Antispasmodic drugs reduce the tone of the muscle wall of blood vessels, expand the lumen of the arteries of the internal organs: No-Shpa, Dibazol, Papaverin.

Medications of the nitrate group (Amylnitrite, Nitroglycerin, Nitranol) reduce venous pressure, reduce the load on the heart, reduce the need for oxygen in the heart muscle, hydrostatic pressure of capillaries, reducing swelling, cardiac output, blood pressure

Calcium channel blockers – dilate the vessels of the heart: Nifedipine, Felodipine, Nicardipine. The drugs block the channels that regulate the ingress of calcium into the cells of blood vessels, the heart, which leads to vasodilation, a decrease in the force of contractions, and a deterioration in the conductivity of pulses to the myocardium.

Plant-based tablets: Bravinton, Cavinton, Vinpocetine, Telektol, Bilobil, Tanakan. The drugs stop vascular spasms of different localization, practically have no contraindications for complications, but still require coordination with a doctor.

The modern classification of peripheral vasodilators is based on the action of the drug and its place of application:

  1. The effect on the vessels – mainly on the arterial vessels, “Hydralazine” and “Phentolamine”, and on the venous – “Prazosin” and nitrates.
  2. Alpha adrenergic receptor blockers – Phentolamine, Droper >

In addition, peripheral vasodilators are divided into:

  • Venous – Molsidomin, Nitroglycerin.
  • Arterial – “Hydralazine”, “Phentolamine” “Minoxidil”.
  • Mixed – “Prazosin”, “Nifedipine”, “Sodium nitroprusside”, “Nitroglycerin” and “Molsidomin”.

By the speed of the onset of the therapeutic effect:

  • Immediate action – “Nitroglycerin”, “Corvaton” with intravenous, under the tongue or local external administration.
  • Slowed down – “Prazosin”, “Isosorbide dinitrate”, “Hydralazine”.

The vasodilator group includes a large list of various drugs. Therefore, their classification is different. If we consider the funds from the point of view of the direction of action, then the following types are distinguished:

  1. Cerebral vasodilators. Such drugs have a direct effect on the vessels of the brain. Thanks to their use, there is a significant improvement in cerebral circulation, which helps to increase mental activity. Indications for the use of such medications are stroke, migraine attacks, vascular atherosclerosis, hypoxia.
  2. Peripheral vasodilators. They are designed to reduce vascular tone in the distal parts of the system. Due to this, the venous inflow to the heart muscle decreases, its functionality improves, and oxygen deficiency in the myocardium decreases.
  3. Mixed. They have a simultaneous effect on the veins and arteries. This leads to a decrease in afterload, an increase in heart rate, as well as a decrease in venous return to the heart.

Different groups of drugs are used for certain diseases. The specific remedy is chosen by the attending physician.

The mechanism of action of drugs with the international nonproprietary name Pentoxifylline

It is a medicine of long (prolonged) action. Pentoxifylline is an active substance that contains 600 mg in one dosage form. Thanks to taking the drug “Vazonit 600”:

  • in places of blood flow failure, microcirculation improves;
  • due to the effect on deformed red blood cells, blood flow improves;
  • erythrocyte membrane elasticity increases;
  • high blood viscosity decreases;
  • platelet adhesion is blocked.

The drug is completely absorbed from the digestive tract. The extended form contributes to the uninterrupted flow of the active substance into the bloodstream. The maximum concentration in the blood is reached after three to four hours and lasts about twelve hours. More than ninety percent of the converted pentoxifylline is excreted by the kidneys.

Mixed drugs

One of the most effective drugs in this group is sodium nitroprusside. It is able to lower the resistance of peripheral vessels and increase venous capacity. This medication is effective only when administered intravenously. It begins to act 5 minutes after administration.

  1. Hypersensitivity.
  2. Intracranial hypertension.
  3. Vitamin B12 deficiency.
  4. Pregnancy.
  5. Glaucoma.
  6. Liver failure.
  7. Renal failure.
  8. Aortic stenosis.

The drug “Agapurin Retard”

The active ingredient of this medicine is also pentoxifylline, which in one tablet is 400 mg. After administration, the active substance is gradually released from the dosage form and evenly enters the bloodstream. In addition to improving microcirculation, the drug has an angioprotective effect. Indications for the appointment of a medication are violations:

  • blood circulation of the eye;
  • cerebral circulation (ischemic);
  • functional sharp inner ear;
  • venous and peripheral arterial blood flow, provoked by diabetes mellitus, atherosclerosis;
  • trophism as a result of varicose ulcerative lesions, frostbite, gangrene;
  • peripheral arterial and venous circulation, proceeding against the background of such processes as infectious, diabetic, atherosclerotic.

And also with angioneuropathy and conditions after a stroke, both hemorrhagic and ischemic.

Individuals with diabetes mellitus often require dose adjustment of antidiabetic agents. Otherwise, the risk of hypoglycemia is high. Take the drug twice a day at the same time, it is well tolerated. Adverse reactions are rare.

Literature

  1. Kharkevich D.A. Pharmacology. M .: GEOTAR MED, 2001.
  2. Belenkov Yu.N., Mareev V.Yu. The principles of rational treatment of heart failure. M .: Consilium Medicum, 2001.
  3. Reference Vidal. Medicines in Russia: A Handbook. – AstraPharmService, 2002.
  4. ACC / AHA Gu>

Higher medical education. 30 years of working experience in practical medicine.

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Editor-in-chief of the Detonic online magazine, cardiologist Yakovenko-Plahotnaya Tatyana. Author of more than 950 scientific articles, including in foreign medical journals. He has been working as a cardiologist in a clinical hospital for over 12 years. He owns modern methods of diagnosis and treatment of cardiovascular diseases and implements them in his professional activities. For example, it uses methods of resuscitation of the heart, decoding of ECG, functional tests, cyclic ergometry and knows echocardiography very well.

For 10 years, she has been an active participant in numerous medical symposia and workshops for doctors - families, therapists and cardiologists. He has many publications on a healthy lifestyle, diagnosis and treatment of heart and vascular diseases.

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