The role of nitrates in the treatment of coronary heart disease at the present stage. Indication for use and dosage of nitrates What drugs are nitrates

Despite the extensive experience in the use of nitrates in clinical practice, the appointment of these drugs is still advisable in cardiac pathology. Modern national guidelines reflect the importance of its use and its analogues for angina pectoris and other forms of coronary heart disease. There is a wide variety of agents within the described group of medicines.

Nitroglycerin is the most common drug used to treat heart attacks.

We are not talking about chemical additives in food products. Among physicians, nitrates are drugs that are used to treat various forms.

Over time, they lost their positions in terms of high predictive value. But until now, it is unlikely that it will be possible to find an alternative to Nitroglycerin or its analogues for stopping an attack at the pre-hospital stage or in the treatment of constantly recurring pain episodes.

According to the classification, the described group of drugs is classified as antianginal. This term means that drugs (nitrates) are aimed at relieving angina pain (angina pectoris).

Today there are many forms, not only in the form of tablets, but also in the form of a spray, plates.

Classification of nitrates

Over time, Nitroglycerin ceased to be the only representative in the presented group of antianginal drugs. There are many analogues, as well as medicines with a similar structure, but in a more convenient form. All this made it necessary to create a classification of nitrates.

There are several subgroups. The main active ingredient is considered the classification criterion. In the treatment of coronary heart disease, in particular, 4 out of 5 subgroups are used.

Nitroglycerin based preparations

Medicines from the nitroglycerin-based group include:

• actually tableted Nitroglycerin, produced in glass vials
• spray Nitrolingval for sublingual use

These are short-acting nitrates.

For the treatment of manifestations of ischemia, intravenous analogs of Nitroglycerin are used. These include Nitropol. Vials of Nitrostat and Perlinganite are also available.

Prolonged representatives of this subgroup are in special demand. Popular products include Nitro in the form of ointments, Nitrong, Trinitrolong, and Sustak.

Means with isosorbide mono - and dinitrate

In addition to drugs based on Nitroglycerin, there are drugs with isosorbide mononitrate, for example, Efoks

Isosorbide mono- and dinitrate is considered a good alternative to nitroglycerin and its analogues. Among the preparations based on these active substances, short-acting and long-term drugs are also produced.

The advantageous advantage is fewer side effects and no need for asymmetric prescription, compliance with the so-called "nitrate-free" interval.

The short-acting agents in these subgroups are a beneficial alternative to the first subgroup nitrates. They are less likely to cause headaches and. Widely used:

• Olikard
• Izodinite
• Efoks

For these funds, there are analogues with an extended period of action.

In the context of specialized cardiology departments, the injectable form of isosorbide dinitrate is popular. But its use also requires monitoring of hemodynamic parameters.

Mechanism of action

When using nitrates, the work of the heart is facilitated by reducing blood flow

Based on the name, it is clear that the described drugs are based on the action of the nitro group - NO 3. Under conditions of blood flow, it turns into nitric oxide, a substance that is a powerful vasodilator.

In other words, the use of nitrates initially leads to an expansion of the vascular lumen, improving blood flow.

Nitric oxide binds to the receptor apparatus of the endothelial lining of veins and arteries. This activates guanylate cyclase, a specific intracellular enzyme.

Its work leads through a whole cascade of complex biochemical transformations to a decrease in the calcium content inside the smooth muscle cell. The result is muscle fiber relaxation.

As a result of a decrease in the tone of the veins, more blood is deposited in them, which means that its flow to the heart is reduced. Thus, when prescribing nitrates, a preload limitation is achieved. The afterload also decreases to a lesser extent - after all, not only the venous trunks expand, but also the arteries with arterioles.

When the blood flow to the chambers of the heart decreases, it becomes much easier to work in this mode. The oxygen demand decreases. And this is what is sought in the treatment of angina pectoris with nitrates and its other forms.

Cardiac blood flow also improves under the influence of nitrates. Nutrition of the ischemic areas of the myocardium again becomes close to full value. The number of collateral (roundabout) blood supply pathways increases, which is important in conditions of chronic ischemia.

Features of the use of nitrates with different duration of action

To avoid pain in the heart with the upcoming load, you can take a drug from the isosorbide group in an hour

The dosage regimen of drugs depends on the purpose of the doctor:

• To relieve acute chest pain, it is enough to take a nitroglycerin tablet or a dose of nitrospray under the tongue. If ineffective, with an interval of five minutes, you need to do the same twice and call an ambulance.
• If the patient wants to protect himself from possible discomfort behind the sternum during the upcoming load or against the background of an expected stressful situation. But then taking Nitroglycerin is impractical because of the short duration of action and the speed of the onset of the effect. The best way out is to take a drug from the isosorbide group an hour before the upcoming event. This will avoid pain and other unpleasant cardiac equivalents.

In the second functional class, the drugs of choice are also long-acting drugs - nitric oxide donors.

It is enough to ensure the effect of the drug for 12 hours. The rest of the time is a nitrate-free interval, the observance of which is important for the prevention of addiction.

Tolerance and Withdrawal Syndrome

It is necessary to observe the nitrate-free interval to reduce the likelihood of addiction to the drug

Like no other means, nitrates develop addiction. This is especially clearly seen with the constant prescription of drugs. In some patients, tolerance is already formed on the 3rd day of treatment, while in others, on the 2nd week.

At first, patients note a pronounced clinical improvement: an increase in exercise tolerance, an improvement in the general condition, an elevation of mood, the ability to endure greater than usual loads and overcome long distances.

But then the drug stops helping the patient, which becomes the reason for self-termination of his intake.

In this case, a second phenomenon occurs - withdrawal syndrome. It consists in a sharp deterioration in the condition. Patients note that against the background of the abolition of nitrate, the condition becomes worse even than what it was before the start of therapy.

It is possible to reduce the likelihood of the formation of addiction to drugs if the so-called nitrate-free interval is observed.

It is about creating a time interval when the effect of nitrates will be minimized. It's easy to follow this rule. The main thing is to pay attention to the duration of the drug's action. The asymmetry of the appointment of nitrates is the key to preventing the development of addiction.

Another possible way to prevent addiction is to prescribe drugs that are donors of sulfhydryl groups. This is, for example, Captopril.

For more information on the use of nitrates, see this video:

The place of nitrates in the treatment of coronary heart disease

With severe shortness of breath against the background of fast walking, the use of nitrates is justified

Treatment of angina pectoris is a complex task. Two principles are used:

1. Improving disease prognosis
2. Improving the quality of life

Nitrates are used to achieve the second goal, as they successfully reduce the severity of clinical symptoms.

Their appointment is justified when a pain syndrome appears behind the sternum or in the case of equivalents of these pains - pronounced against a background of stress or brisk walking.

An individualized approach is used to prescribe the described group of drugs. First, the functional class of angina pectoris is assessed. For functional class 1 and 2, situational intake of nitrates is advisable. Can be used prophylactically before high load.

When functional class 3 is diagnosed, asymmetric reception can be performed, but it is important to observe the nitrate-free gap. Better if it is equal to at least 4-6 hours.

Finally, the appearance of angina pectoris at rest is a reason for appointment on an ongoing basis. It is no longer necessary to observe the nitrate-free interval. We are talking about the 4th functional class of stable angina.

Separately, it should be said about the unstable variants of coronary heart disease. This is progressive angina and. At the prehospital stage, nitroglycerin and its analogs are administered orally. If ineffective, they switch to intravenous drip and very slow administration.

Side effects and contraindications

When using nitrates, a side effect such as headache is very common.

The main undesirable phenomenon that occurs when prescribing Nitroglycerin, Nitrosorbide and other representatives of this group is headache. Some patients report severe discomfort in the occipital or parietal region.

The main cause of the discomfort that occurs is a decrease in the tone of the veins, including the venules of the head and skull. More than usual amount of blood is deposited. This causes the so-called hypertensive syndrome.

The second mechanism for the development of pain is reduction. Severe hypotension occurs, but already at the arteriolar level. It is possible to prevent the development of the described undesirable phenomenon only if nitrates are prescribed at arterial pressure above 120/80 mm Hg.

Hypotension should first be dealt with without medication. It is enough to recommend the patient to take a horizontal position with the legs raised up. If the measures taken are ineffective, inotropic drugs are used.

Nitrates cannot be used for a number of heart conditions. So, among the contraindications is such a pathology as.

Especially dangerous is the appointment of nitrates in the presence of obstruction of the outflow tract of the left ventricle. The use of Nitroglycerin in this clinical situation is fraught with aggravation of symptoms, the appearance of shortness of breath and fainting.

The described drugs are also not indicated for patients with valve pathology. In patients with aortic, for example, severe pain in the retrosternal region and rhythm disturbances appear. Nitrates are also recommended with caution when the left atrioventricular opening is narrowed.

Drug interactions with other drugs

The combined use of nitrates and drugs of the sildenafil groups increases the risk of developing a shock state

A favorable combination is the joint appointment of nitrates and or blockers of slow calcium channels. There is a potentiation of the antianginal effect.

Cardiologists around the world consider this a rational combination. The main thing is that adrenergic blockers and calcium channel blockers are not jointly prescribed.

Of the irrational combinations, the simultaneous administration with drugs of the sildenafil group is considered. These drugs are used in the treatment of pulmonary hypertension and erectile dysfunction (impotence).

Joint use increases the risks of developing a shock state and worsening ischemia, which occurs as a paradoxical reaction.

Hemodynamic parameters should be monitored during joint treatment with antiarrhythmic drugs and nitric oxide donors. Much attention must be paid to the joint appointment of Quinidine or Novocainamide with nitrates.

When treating with nitrates, it is very important to consult a doctor. Self-administration is possible only after his recommendations. After all, there are dangerous side effects, as well as contraindications. The use of drugs in these cases will only aggravate the condition.

Nitrates include three drugs: nitroglycerin, isosorbide dinitrate, isosorbide-5-mononitrate. Sometimes molsidomin is included in the same group. Although it is not structurally nitrate, its mechanism of action is also mediated through nitric oxide and vasodilation.

According to the duration of action, these drugs are divided into:

• short-acting (up to 1 hour);
• moderately prolonged (last 1-6 hours);
• significantly prolonged (from 6 to 24 hours).

Depending on the routes of entry of the drug into the body, the forms of nitrates are distinguished:

• administered into the oral cavity (oral): tablets, aerosols, plates;
• taken by mouth (oral): tablets and capsules;
• injection: solutions for long-term slow intravenous administration.

The following nitrate preparations can be found in pharmacies:

• nitroglycerin: Nitro and Nitro Paul Infusion (for intravenous infusion), Nitroglycerin, Nitrogranulong, Nitrocor, Nitrolong, Nitromint, Nitrong Forte, Nitrosprey, Nitrosprint, Perlinganit, Sustak Forte, Trinitrolong films;
• isosorbide dinitrate: Dinisorb, Isacardin, Isoket, Cardiket, Nitrosorbide;
• isosorbide-5-mononitrate: Monizol, Mono Mac, Mono Rum Retard, Monolong, Monosan, Monochnikwe and Monocinque retard, Olikard 60 Retard, Pectrol, Efoks 20, Efoks Long.

The names with the indications "long", "forte", "retard" refer to drugs with prolonged action.

Molsidomin is sold under the names Korvaton, Sidnopharm and Dilasid.

Mechanism of action

Nitrates cause the arteries of the heart to dilate. This increases the flow of blood to the myocardium and the supply of oxygen to it. As a result, the pain or discomfort behind the breastbone disappears.

In addition, nitrates dilate veins throughout the body. At the same time, they begin to hold more blood. This reduces the amount of blood returning to the heart, thereby reducing the strain on it.

This effect is due to the release of nitric oxide from these compounds, which directly relaxes the vascular wall.

Another property of these drugs is the ability to reduce platelet adhesion (aggregation) and improve blood flow. As a result of such a complex action, the heart tolerates the load much better, and myocardial ischemia occurs with more significant effort.

On average, the antianginal (analgesic) effect of nitrates is stronger than that of drugs in other groups. However, in different patients, the effectiveness and duration of such an effect differ significantly. So, the same dosage of the drug in one patient lasts for 8 hours, while in another - only one hour. Therefore, a gradual slow selection of the dosage and regimen of medication necessary for the patient is important.

Features of the use of nitrates with different duration of action

To relieve an attack of angina pectoris, the most popular remedy is nitroglycerin tablets, which are taken under the tongue. With angina pectoris, they help within 1-3 minutes. If after taking nitroglycerin the pain lasts half an hour or more, then it is most likely cardialgia or thoracalgia (except in cases of myocardial infarction).

If after taking the 1st pill the pain behind the breastbone has not gone away, after 5 minutes you need to take another pill, and if there is no effect after another 5 minutes, take the third. If this does not help, you need to urgently call an ambulance.

To relieve seizures, it is more convenient than tablets to use aerosols Nitrospray, Nitromint. First, nitroglycerin does not fizzle out in cans and does not lose its effectiveness. Secondly, it is easier to use this way. Finally, the smallest aerosol droplets are absorbed faster into the bloodstream than tablet particles.

Trinitrolong plates can not only stop an attack, but also prevent its occurrence for up to 5 hours. Therefore, they can be glued to the gums 15 minutes before the expected load, for example, going to the store.

Plasters with nitroglycerin are convenient:

• they provide a uniform flow of the drug into the bloodstream throughout the day;
• nitroglycerin is absorbed into the blood without entering the liver;
• at night, the patch can be removed, which provides a "nitrate-free window" during which the sensitivity of cells to nitroglycerin is restored.

There are cutaneous forms of isosorbide dinitrate in the form of an aerosol. It is sprayed onto the skin 1-2 times a day, and its effect lasts up to a day. The disadvantage of this form is the rapid "addiction" and reduced effectiveness. Therefore, such dermal aerosols can be used only for unstable angina pectoris in the first few days of the disease.

Isosorbide dinitrate plates of 20 mg should be placed on the gums three times a day, and 40 mg - twice a day. Their action is milder and more gradual than that of tablets.

Of the tablet preparations of isosorbide dinitrate, nitrosorbide is the most common, as well as forms of prolonged action (Cardiket-retard).

Isosorbide-5-mononitrate lasts longer than dinitrate, but its effect is weaker. Therefore, a large dosage is needed. Retard forms are used once a day at a dosage of at least 50 mg.

Tolerance and Withdrawal Syndrome

With a constant level of nitrates in the body, the coronary arteries gradually stop responding to them, and the effect of drugs disappears. The main way to overcome nitrate tolerance is to create a "nitrate-free window", that is, a gap when this drug is not in the blood. For example, conventional tablets for this are prescribed not 4 times a day, but 2-3 times. An important way to prevent tolerance is the use of prolonged forms of isosorbide-5-mononitrate.

Clinics often use "sporadic" nitrates when they are given before planned exercise.

The main hazard associated with intermittent dosing is withdrawal. It occurs when the supply of nitrates abruptly stops. For example, after the end of an intravenous injection or peeling off a skin patch, there may be an increase and increase in attacks of pain behind the sternum.

For the prevention of withdrawal syndrome, it is advisable to use prolonged forms, the reception of which can be prescribed once a day.

Given the high efficiency of this group of drugs, and on the other hand - the phenomena of addiction and withdrawal, nitrates in IHD are prescribed only to those patients who cannot do without them.

Nitrates for ischemic heart disease

With stable angina pectoris, each patient can easily predict whether he will be able to withstand some kind of stress, or it will cause pain. Therefore, with I-II functional classes of angina pectoris, nitrates are prescribed only before exercise to prevent an attack. In this case, ordinary nitrosorbide is used; there is no need to prescribe extended forms.

With frequent attacks corresponding to functional classes III-IV, it is better to prescribe extended isosorbide dinitrate (for example, Cardiket-retard) 2 times a day.

For nighttime symptoms, the appointment of isosorbide-5-mononitrate at a dose of 1–2 times a day is indicated.

With myocardial infarction or an unstable course, a long-term slow intravenous infusion of nitroglycerin is prescribed. At the same time, it is necessary to control the blood pressure level every hour, and when it drops to 110 mm Hg. Art. and lower the rate of administration or temporarily suspend the infusion.

The activity of nitrates increases with their simultaneous use with calcium antagonists (verapamil, diltiazem), beta-blockers, ACE inhibitors.

Side effects and contraindications

Possible side effects:

• development of tolerance;
• headache, dizziness;
• redness of the face;
• increased heart rate;
• decreased pressure, fainting.

Nitrates increase the risk of syncope in patients with hypertrophic cardiomyopathy and severe aortic stenosis. They are contraindicated in such concomitant diseases:

• any form of shock and collapse with a decrease in systolic pressure less than 100 mm Hg, diastolic - less than 60 mm Hg;
• myocardial infarction with a decrease in blood pressure;
• constrictive variant of pericarditis;
• cardiac tamponade;
• pulmonary edema caused by poisonous gases or other toxic substances;
• increased intracranial pressure (hemorrhagic stroke, brain injury);
• angle-closure glaucoma, accompanied by high intraocular pressure;
• individual intolerance.

Pharmacological group - Nitrates and nitrate-like drugs

Subgroup drugs are excluded. Enable

Description

Nitrates are widely used as antianginal agents for various forms of coronary artery disease (angina pectoris, myocardial infarction, etc.). The therapeutic effect of nitrates (nitrovasodilators) is based on the ability of a substrate to increase the content of nitric oxide, which is an endothelial relaxing factor. This factor stimulates guanylate cyclase, increases the content of cyclic guanosine monophosphate inside the cell and, as a result, causes vasodilation. Nitrovasodilators include organic nitrates, as well as sydnoneimines (molsidomin) and other nitric oxide donors (amyl nitrite). The most common in clinical practice are organic nitrates (nitroglycerin, isosorbide dinitrate, isosorbide mononitrate). Recently, not only have been developed new compounds and dosage forms of organic nitrates, incl. prolonged action, but also clarified and expanded the indications for their use, in particular, in heart failure, developed objective methods for assessing their effectiveness and ways to overcome tolerance. Dosage forms of nitrates ensure the penetration of the active substance into the bloodstream through the mucous membrane of the oral cavity (tablets, plates, aerosols), after oral administration (tablets, capsules for oral administration), transdermally, i.e. when applied to the skin (ointments, patches, discs) or used for injections.

The antianginal effect of nitrates is due to the restructuring of hemodynamics associated with the general vascular effect of the drug, relaxation under its influence of smooth muscles of peripheral vessels, especially with its venodilatory effect. Under the influence of nitroglycerin, venous blood flow to the heart decreases, pressure in the right atrium, in the pulmonary artery system decreases, and peripheral vascular resistance decreases. As a result, the myocardium is unloaded, its stress decreases to overcome the resistance of blood ejection, energy costs and oxygen demand are reduced. The ongoing decrease in cardiac tension and coronary action contribute to the restoration of blood flow through the small vessels of the myocardium, improve blood flow in the epicardial coronary arteries. Along with a decrease in ischemia, pain impulses from the ischemic focus gradually disappear and the pain syndrome stops. The action of nitrates is not limited to the effect on the coronary vessels, they cause the expansion of other blood vessels (vessels of the brain, peripheral vessels, vessels of the abdominal cavity). Taking nitrates can modulate fibrinolysis by changing the ratio in plasma between the two main components of this system - tissue plasminogen activator and its inhibitor, which can be both a consequence of changes in hemodynamics and the result of the inhibitory effect of NO on platelet aggregation and adhesion.

In addition to the use of nitrates as drugs of choice for the initial treatment of most patients with angina pectoris (relief and prevention of seizures), their appointment to patients with a variable threshold for the onset of ischemic pain is justified, since they prevent intermittent coronary vasoconstriction in vasospastic angina pectoris. For the purpose of relief and for the prevention of a predicted attack of angina pectoris, dosage forms of nitrates, absorbed in the oral cavity, are often used. Of the drugs taken orally, retarded forms of nitrosorbide and its metabolite are most effective. The main indication for the regular intake of the retarded form of nitrosorbide is resting angina pectoris that often recurs during the day. Occasional administration (mainly 1 time per day) is recommended for the prevention of angina or cardiac asthma attacks that occur at night. For the same purpose, transdermal forms of nitrates can be used. Regular intake of retarded forms of nitrosorbide and 5-mononitrate is indicated for heart failure with impaired left ventricular function and mitral regurgitation, as well as for pulmonary hypertension. The injectable form of nitrates is used to treat patients with unstable angina pectoris, acute myocardial infarction, and severe heart failure.

Due to the significant individual variability of the effect, expressed in a significant fluctuation in the values \u200b\u200bof effective doses of nitrates and the duration of action of the same drug in different patients, modern nitrate treatment programs imply the obligatory use of objective methods for assessing its effectiveness: pharmacodynamic studies with treadmill, paired veloergometry, repeated monitoring Holter ECG, radioisotope methods of myocardial perfusion research, stress echocardiography. Most often, nitrate treatment is monitored by the level of blood pressure, measured at the maximum effect of the drug (after 1 hour), and by the increase in the duration and power of the load during exercise tests, the disappearance of episodes of ST segment depression when monitoring the ECG, as well as by subjective tolerance.

Common side effects of nitrates are headache, usually at the start of treatment, and tachycardia. Reducing the dose, changing the route of administration of the drug or the use of analgesics, menthol or validol in some cases reduce the severity of headache. Another common side effect is postural hypotension, which is manifested by dizziness, weakness, and even short-term loss of consciousness. Methemoglobinemia, as well as severe nitrate poisoning, occur mainly in young children. Some patients with coronary artery disease develop tolerance to nitrates - a condition in which an increase in the dose of nitrates is required to achieve an antianginal or hemodynamic effect. Tolerance is manifested by an increase in the frequency of angina attacks, the appearance of rest angina, and an increase in the need for nitroglycerin. At the same time, the effect of taking various nitrates is perverted or reduced, and the duration of their action is shortened. Tolerance can appear immediately after taking several doses of the drug, and in this case it is referred to as tachyphylaxis. The weakening of the action of nitrates is not associated with increased metabolism in the liver. It is due to the fact that with regular use, their less active metabolites accumulate in the blood, which compete with the main drug for binding sites. In addition, the development of tolerance to nitrates may be associated with the oxidation of sulfhydryl groups located in specific areas of vascular smooth muscles with which nitrates interact, a change in the activity of guanylate cyclase and a decrease in the synthesis of cyclic GMF. The severity of tolerance is directly proportional to the dose and frequency of nitrate intake. With prolonged use of short-acting dosage forms, weakening of their action is not observed. With the regular use of prolonged forms of nitrates and isosorbide dinitrate, especially patches and ointments, the risk of developing tolerance increases significantly. To prevent the development of tolerance, the required minimum dose of the drug should be found, which gives a hemodynamic effect of a certain severity. Methods of intermittent use of nitrates are proposed: the appointment of isosorbide dinitrate not 4, but 2 times a day - in the morning and in the afternoon, so that every day for 8-12 hours, nitrates are absent in the blood. Transdermal forms of nitroglycerin are recommended to be removed from the body at night, creating a drug-free period. In the case of a decrease in the effectiveness of nitrates with forced regular intake, it is recommended to interrupt the treatment for at least 24 hours, allowing the patient only to stop the seizures with short-acting nitroglycerin. However, in this case, the development of a withdrawal syndrome associated with a sharp cessation of the intake of nitroglycerin into the body is possible. This is evidenced by attacks of angina pectoris, often occurring when the intravenous infusion of nitroglycerin is suddenly stopped. It is also recommended to temporarily switch to treatment with molsidomine, prescribe drugs - donors of sulfhydryl groups (S-acetylcysteine, captopril), although there is currently no convincing evidence of the possibility of preventing tachyphylaxis with the help of any means.

Drugs

• First aid kit
• Online store
• About company
• Contacts

• Publisher contacts:
• E-mail:
• Address: Russia, Moscow, st. 5th Magistralnaya, 12.

When citing information materials published on the pages of the site www.rlsnet.ru, a link to the source of information is required.

©. REGISTER OF MEDICINAL PRODUCTS OF RUSSIA ® RLS ®

All rights reserved

Commercial use of materials is not allowed

Information intended for healthcare professionals

Organic nitrates - ATC classification of medicinal products

This section of the site contains information about drugs of the group - C01DA Organic nitrates. Each medicinal product is described in detail by the specialists of the EUROLAB portal.

The Anatomical Therapeutic Chemical Classification (ATC) is an international drug classification system. The Latin name is Anatomical Therapeutic Chemical (ATC). Based on this system, all drugs are divided into groups according to their main therapeutic use. The ATC classification has an understandable hierarchical structure, which makes it easier to find the necessary drugs.

Each medicine has its own pharmacological action. Correctly identifying the right drugs is a fundamental step in successfully treating diseases. In order to avoid undesirable consequences before using certain drugs, consult your doctor and read the instructions for use. Pay particular attention to interactions with other medications and conditions of use during pregnancy.

ATX C01DA Organic nitrates:

Group drugs: Organic nitrates

• Aerosonit (Topical Aerosol)
• Deposit 10 (Plasters (Emplastra))
• Izacardin (Concentrate for solution for infusion)
• Iso Mac retard (capsule)
• Isoket (Spray)
• Isoket (Concentrate for solution for infusion)
• Izolong (Capsule)
• Isomonat (oral tablets)
• Cardiket (Oral tablets)
• Cardix (Capsule)
• Cardix Mono (Capsule)
• Monizid (Oral tablets)
• Monizol (oral tablets)
• Mono Mac (Oral Tablets)
• Mono Mac 50 D (Oral Tablets)
• Mono Mac Depot (Oral Tablets)
• Mono Rum retard (Capsule)
• Monolong (Capsule)
• Mononit (Tablets, oral)
• Mononitroside (Tablets, oral)
• Monosan (Oral tablets)
• Monocinque (Oral tablets)
• Monocinque retard (capsule)
• Nirmin (concentrate for solution for infusion)

• Nitradisc (Transdermal Therapeutic Conduction System)
• Nitro (Concentrate for solution for infusion)
• Nitro Mac (Capsule)
• Nitro Mac (Concentrate for solution for infusion)
• Nitro POL infusion (Concentrate for solution for infusion)
• Nitro-dur (Transdermal Therapeutic System)
• Nitro-Nick (Oral Tablets)
• Nitroglycerin (Capsule)
• Nitroglycerin (Concentrate for solution for infusion)
• Nitroglycerin (Intravenous solution)
• Nitroglycerin (Spray)
• Nitroglycerin (Substance)
• Nitroglycerin (Sublingual Tablets)
• Nitroglycerin (Oral Tablets)
• Nitroglycerin microgranules (Substance)
• Nitroglycerin Nycomed (Sublingual tablets)
• Nitroglycerin with glucose (substance powder)
• Nitroglycerin with lactose (Substance powder)
• Nitroglycerin forte (semi-finished product-granulate)
• Nitrogranulong (Oral Tablets)
• Nitroject (Solution for infusion)
• Nitrocor (oral drops)
• Nitrocor (Capsule)
• Nitrocor (Sublingual tablets)

• Nitrolingval-Aerosol (Aerosol)
• Nitrolong (Capsule)
• Nitromint (Aerosol)
• Nitrong (Oral Tablets)
• Nitrong forte (Tablets, oral)
• Nitroperkuten TTS (Transdermal Therapeutic System)
• Nitrosorbide (Substance powder)
• Nitrosorbide (Tablets, oral)
• Nitrosorbide-Rusfar (Oral tablets)
• Nitrospray (Spray)
• Nitrospray-ICN (Spray)
• Nitrosprint (Spray)
• Pectrol (Tablets, oral)
• Pentacard-10 (Oral tablets)
• Pentacard-20 (Oral tablets)
• Pentacard-40 (Oral tablets)
• Perlinganite (Concentrate for solution for infusion)
• Sorbimon (Tablets)
• Sustak mite (Tablets)
• Sustak forte (Pills)
• Sustonit (Tablets)
• Erinit (Aerosol)
• Efoks 20 (Oral tablets)
• Efoks Long (Capsule)

If you are interested in any other medicines and preparations, their descriptions and instructions for use, synonyms and analogs, information on the composition and form of release, indications for use and side effects, methods of application, dosages and contraindications, notes on the treatment of children with medicine, newborns and pregnant women, the price and reviews of medicines, or if you have any other questions and suggestions - write to us, we will definitely try to help you.

Hot topics

• Hemorrhoid Treatment Important!
• Solving the problems of vaginal discomfort, dryness and itching Important!
• Comprehensive treatment of colds Important!
• Treatment of the back, muscles, joints Important!
• Complex treatment of kidney diseases Important!

Other services:

We are in social networks:

Our partners:

ATX (ATC) - classification of drugs and medical products on the EUROLAB portal.

The EUROLAB ™ trademark and trademark are registered. All rights reserved.

Nitrates: a list of drugs, application features

For more than 100 years, nitrates have opened the list of drugs for the elimination of anginal pain arising from angina pectoris and myocardial infarction, and occupy one of the leading places in cardiological practice. The study of these drugs remains relevant now, since the number of patients with coronary heart disease is constantly increasing from year to year.

In this article, we will acquaint you with the main drugs from the group of organic nitrates, their classification, mechanism of action, forms of release, application features, indications, side effects and contraindications. This information will help you get an idea of \u200b\u200bthe medicines commonly used to treat heart disease and you can ask your PCP if you have any questions.

A bit of history

For the first time, organic nitrates were used to relieve pain in angina pectoris back in 1879. Dr. Murrell published the results of exposure to 1% alcoholic solution of nitroglycerin (glycerol trinitrate) in the Lancet magazine. He first "tested" this drug on himself, and then on his patients. The results of antianginal exposure were positive.

In 1925, capsules with Nitroglycerin entered the practice of cardiologists, and a little later, a liquid alcohol solution and tablets for sublingual administration appeared. However, cardiologists were not satisfied with the short-term effect of this drug, and pharmacological studies aimed at finding such prolonged-acting substances continued. After the 70s, the first such drug was created based on isosorbide dinitrate, and a little later, a new nitrate-containing agent appeared - isosorbide mononitrate.

All of these active components have the same mechanism of action; it consists of a vasodilator and an antianginal component. Thanks to the action of organic nitrates, the smooth muscles of the vessels relax, the coronary vessels expand, and more blood and oxygen are delivered to the myocardium. As a result, the hemodynamic load on the heart and the oxygen demand of the heart muscle are reduced.

Classification

Organic nitrates are divided according to the duration of action:

• short-acting - designed to relieve attacks of anginal pain with angina pectoris or myocardial infarction;
• long-term (or prolonged) action - prescribed for the prevention of angina attacks.

Nitroglycerin preparations

Nitroglycerin is the reference drug among nitrate-containing drugs and is prescribed for both relief and prevention of angina attacks. It can be used as an intravenous infusion for myocardial infarction and acute heart failure.

The active component of these funds is glycerol trinitrate. They are:

• short-acting - Nitroglycerin;
• long-acting - Nitrong, Sustonit, Sustak forte, Nitroderm, Trinitrong, etc.

Ordinary Nitroglycerin begins to take effect in 1-2 minutes and remains active for about 30 minutes. This short-acting drug is used to relieve an attack that has already occurred.

To prevent anginal pain, prolonged nitroglycerin-based drugs are prescribed. After taking them, they begin to act in a minute, and the therapeutic effect lasts for about 6 hours.

Nitroglycerin has a number of side effects that often negatively affect overall health. Over time, they become less pronounced.

Long-term use of drugs based on nitroglycerin can cause addiction, which manifests itself in a decrease in the severity of the therapeutic effect and the duration of action. It is assumed that this tolerance is provoked by the depletion of thiol compounds involved in the metabolism of the active ingredient. For their complete recovery, a free interval of hours is required between taking Nitroglycerin.

Abrupt cessation of taking this and other nitrate-containing drugs can cause withdrawal symptoms, expressed in the occurrence of an attack of angina pectoris. That is why when canceling organic nitrates, the dose should be reduced gradually.

Isosorbide dinitrate preparations

Isosorbide dinitrate is similar in structure to nitroglycerin. With sublingual administration, it begins to act in 2-5 minutes, and when administered orally, in a minute.

The active component of these funds is isosorbitol trinitrate. They are:

• short-acting - Iso poppy, Izoket, Nitrosorbit, Izodinite, etc.;
• long-acting - Iso mac retard, Isoket retard, Cardix, Cardiket, etc.

The duration of action depends on the type and form of release of the drug and can range from 2 to 12 hours.

Isosorbide mononitrate preparations

Isosorbide mononitrate belongs to the main metabolites of isosorbide dinitrate. This substance has greater bioavailability and lasts longer - up to 12 hours or more.

The active component of these funds is isosorbide mononitrate. They are:

• short-acting - Monocinque, Mono mac, Olikard, Isomonat, etc .;
• long-acting - Mono poppy depot, Monocinque retard, Olikard retard, Efoks long, etc.

Side effects of funds based on isosorbite mononitrate and dinitrate are less pronounced than that of Nitroglycerin. With prolonged use, addiction can also develop, and abrupt withdrawal can provoke withdrawal syndrome.

Nitro-like preparations

Their mechanism of action is similar to nitrate-containing agents, and they are also capable of dilating blood vessels in angina pectoris and other heart pathologies. In addition, addiction to such drugs develops to a much lesser extent than to organic nitrates.

Nitrate-like drugs include:

• Sodium nitroprusside;
• Korvaton (Sidnopharm, Molsidomin);
• Nikorandil (Kordinik).

Mechanism of action

The therapeutic effects of organic nitrates are expressed in the expansion of:

• coronary vessels - this process causes an increase in blood circulation along the collaterals and an improvement in the nutrition of ischemic areas of the myocardium;
• arteries - such vasodilation reduces the load on the heart by reducing peripheral resistance;
• veins - this process reduces venous blood flow, reduces the load on the walls of the heart ventricles, improves coronary blood flow.

After entering the body from the nitrate molecule, the NO group is cleaved, which activates guanylate cyclase and thereby causes an increase in the level of cyclic guanosine monophosphate. The accumulation of this substance leads to relaxation of the smooth muscles of the walls of the coronary vessels (along the way, the vessels of the urinary, digestive and respiratory systems also expand). Acting on the brain, organic nitrates cause blocking of the central links of coronary constrictive reflexes and weaken sympathetic control over blood vessels and the heart.

The antianginal effect is provided not only by the expansion of the coronary vessels, but also by the fact that under the influence of the processes occurring in the body, hemodynamic unloading of the myocardium occurs, which causes a weakening of the load on the heart and a decrease in its oxygen requirements. Dilation of arteries leads to a decrease in their resistance to cardiac output, and dilatation of the venous vessels limits the return of venous blood to the heart.

In addition to these effects, nitrates have a positive effect on myocardial nutrition, electrolyte balance, and the activity of respiratory enzymes. They have a beneficial effect on the electrical ability of the heart muscle, preventing the development of arrhythmias, and lowering the pressure in the pulmonary circulation, eliminating left ventricular failure.

Characteristics of dosage forms of organic nitrates

Nitrate preparations are available in different dosage forms:

• tablets and granules for sublingual administration;
• oral tablets;
• solution for intravenous infusion;
• aerosols for sublingual administration;
• plasters, ointments and discs for transdermal use;
• buccal (cheek) plates or tablets.

Sublingual tablets, capsules, granules, or aerosols are short-acting drugs designed to relieve angina attacks. Other forms of these drugs can be prescribed to prevent attacks, treat coronary artery disease and heart failure.

Particular attention is paid to the intake of Nitroglycerin granules. Patients should be reminded that after opening the bottle, they lose their effectiveness after about a day. That is why it is recommended to always monitor the expiration date of the drug used or to carry a new, unopened bottle with you.

As practice shows, aerosol forms of nitrates do not have a particular advantage over sublingual tablets. In addition, their use is currently restrained due to the presence of freon in the can, an environmentally hazardous substance.

When taken under the tongue, the effect of nitroglycerin begins in 1-2 minutes and reaches its maximum in 4-6 minutes. The action of the drug stops after a delay, therefore, in the absence of pain relief after taking the first tablet, it is recommended to take another dose in 3-5 minutes.

Intravenous infusion of nitrates is usually prescribed for patients with unstable angina or myocardial infarction. Infusion of the solution is started at a rate of 5-25 μg / min. Further, the rate of administration begins to increase until the systolic pressure is reduced by% (but not less than 90 mm Hg). Pain relief with this use of the drug usually occurs after 2-5 minutes.

In patients with acute infarction, maintenance infusion is continued for about 10 hours. These organic nitrates include the following drugs:

Nitrate-containing tablets based on nitroglycerin, isosorbide dinitrate and isosorbide mononitrate for oral administration are prolonged (retard) drugs. Part of the administered dose is absorbed from the stomach and begins to act in the first 10 minutes after ingestion, while the other enters the bloodstream more slowly and provides an extension of the therapeutic effect for another 4-6 hours. Such dosage forms are used only for the prevention of angina attacks.

The retard tablets are available in the following doses: 20, 40, 60 and 120 mg. In addition, there are combined nitrate-containing preparations - Nitrodurate containing isosorbitol dinitrate, and Glyceroltrinitrate. The dosage and frequency of administration of such drugs is selected for each patient individually and depends on the severity of angina pectoris.

Transdermal patches (or ointments, discs) with nitrates are used to prevent angina attacks. They begin to act in a minute, and the duration of their effect is from 12 to 24 hours. Now this form of release of organic nitrates has become less popular, since it turned out that these agents are capable of exerting a local irritating effect and do not have stable bioavailability and effectiveness. In addition, they can be not just addictive, but quickly addictive. These forms of nitrates include the following drugs:

Another disadvantage of these funds is their high cost.

Buccal plates and tablets are applied in the form of applications to the gingival mucosa of the upper jaw. They are available in doses of 1, 2 or 4 mg and are designed to relieve angina pain. In addition, these forms of release can be used to prevent recurrent attacks over the next 3-5 hours. Buccal forms have the highest bioavailability. These organic nitrates include the following drugs:

In contrast to these agents, Dinitrosorbilong is available in 40 mg buccal plates and provides a therapeutic effect for 10 hours or more.

Indications for appointment

The main indications for the appointment of organic nitrates are the following conditions:

• exacerbation of ischemic heart disease - to eliminate myocardial ischemia, left ventricular failure and lower blood pressure;
• strong manifestations of ischemic heart disease - are used to eliminate and prevent angina attacks and myocardial ischemia;
• acute heart failure - are prescribed to eliminate congestion in the lungs, pulmonary edema, as well as arterial hypertension and myocardial ischemia;
• chronic heart failure - sometimes used to reduce the burden on the heart;
• arterial hypertension - can be used for urgent pressure reduction.

Contraindications

Taking nitrate-containing drugs may be contraindicated in the following cases:

• collapse (blood pressure less than 90 mm Hg) or shock;
• an attack of myocardial infarction, accompanied by arterial hypotension or shock;
• recent traumatic brain injury;
• increased intracranial pressure;
• acute disorders of cerebral circulation;
• angle-closure glaucoma;
• toxic pulmonary edema;
• severe forms of anemia;
• hypersensitivity, manifested by severe headaches, tachycardia and hypotension.

Nitrates are prescribed with caution to patients with severe manifestations of cerebral atherosclerosis.

The use of organic nitrates during pregnancy and lactation is permissible only if there are strict indications, and their intake can be carried out exclusively under medical supervision. Breastfeeding for the period of admission should be discontinued, since the active components of the drugs penetrate into milk and cause methemoglobinemia and hemodynamic disturbances in the child. According to the results of experiments on sheep, sodium nitroprusside should not be prescribed during pregnancy, since this drug can cause intrauterine fetal death.

Side effects

Taking organic nitrates can have the following side effects:

• headache or throbbing in the head;
• arterial hypotension;
• orthostatic collapse (more often after taking Nitroglycerin);
• tachycardia;
• bradycardia (with intravenous infusion of nitroglycerin);
• redness of the face;
• addictive;
• withdrawal syndrome.

Sodium nitroprusside, in addition to the side effects discussed above, can cause anxiety, nausea, vomiting, chest pain and the accumulation of cyanide, leading to the onset of hypoxia, which is dangerous to health and life.

In more rare cases, when taking organic nitrates, the following undesirable effects are observed:

How to avoid nitrate addiction

So far, the mechanism for reducing tolerance to organic nitrates has not been fully understood, and experts put forward only hypothetical reasons for the occurrence of such a side effect. In addition, the development of addiction is variable in different patients. For example, taking isosorbide dinitrate for a month is accompanied by a complete loss of the antianginal effect in about% of patients, in% this effect is significantly reduced, and in% it remains the same. According to the observations of specialists, more often a decrease in tolerance to nitrate-containing agents occurs when using transdermal forms, and much less often when using buccal tablets and plates.

To reduce or eliminate the addictive effect, it is recommended to take organic nitrates with the obligatory observance of a period free from taking these drugs. According to experts, it is enough to observe the 8-12-hour "nitrate-free" interval for this.

In addition, if possible, you should take breaks in taking nitrate-containing drugs. This interval can be 1-2 weeks. If it is impossible to completely abolish nitrates during this period, the usual drug can be replaced with Corinfar or Sidnopharm (Corvaton).

Interaction with other medicinal products

Taking organic nitrates with some drugs can lead to the development of more pronounced arterial hypotension. These drugs include:

When taking nitrates with some drugs, their vasodilating properties may decrease. These funds include:

• histamine;
• angiotensin;
• carbacholine;
• phenylephrine;
• norepilephrine;
• atropine and other M-anticholinergics;
• central nervous system stimulants;
• glucocorticosteroids.

The joint intake of Phenobarbital and a nitrate-containing drug for oral administration can lead to a significant decrease in the bioavailability of the latter and a decrease in its effectiveness.

Which doctor to contact

Self-administration of nitrates without a doctor's recommendation can lead to a worsening of the patient's condition, a drop in blood pressure, an attack of glaucoma and other adverse consequences. That is why nitrates should be taken only as directed and under the supervision of a therapist or cardiologist.

Help children

Useful information

Contact the specialists

Telephone appointment service for medical specialists in Moscow:

The information is provided for informational purposes only. Do not self-medicate. At the first sign of disease, consult a doctor.

Editorial office address: Moscow, 3rd Frunzenskaya st., 26

17381 0

The first mention of the effectiveness of organic nitrates in angina pectoris dates back to 1867, but the drugs of this group are still widely used in the treatment of cardiac patients. They are indispensable in cases where it is necessary to quickly eliminate myocardial ischemia or acute manifestations of left ventricular heart failure.

Classification

The composition distinguishes propantriol trinitrate (nitroglycerin), isosorbide dinitrate and isosorbide mononitrate.

There are a large number of dosage forms of nitrates:

• for sublingual or aerosol use (nitroglycerin, isosorbide dinitrate);
• for parenteral administration (nitroglycerin, isosorbide dinitrate);
• for gluing on the gums in the form of films (nitroglycerin, isosorbide dinitrate);
• for cutaneous application in the form of plasters, ointments (nitroglycerin, isosorbide dinitrate);
• for oral administration (nitroglycerin, isosorbide dinitrate, isosorbide mononitrate).

Mechanism of action and pharmacological effects

Penetrating into smooth muscle cells, nitrates serve as a source of nitric oxide (NO), which stimulates the activation of guanylate cyclase. As a result, the formation of cGMP increases, which leads to a decrease in the concentration of calcium inside smooth muscle cells and their relaxation. Nitrates act independently of the ability of endothelial cells to produce endogenous nitric oxide.

Nitrates promote the expansion of the coronary arteries and arterioles of sufficiently large diameter. This leads to a decrease in the severity of spastic reactions in the coronary arteries, an improvement in the blood supply to the subendocardial layers of the myocardium, and an increase in collateral blood flow. In addition, nitrates act on the vessels of the systemic circulation, causing the expansion of both peripheral venous vessels that deposit blood and arterioles. Under their influence, the extensibility of large arteries improves. As a result, venous return and SBP in the aorta are reduced. Accordingly, preload, afterload and tension of the walls of the ventricles of the heart decrease, which leads to a decrease in myocardial oxygen demand. Reducing the filling pressure of the ventricles improves the blood supply to the subendocardial layers of the myocardium. These mechanisms underlie the anti-ischemic action of nitrates and their ability to reduce the severity of manifestations of left ventricular heart failure.

The vasodilating effect of nitrates is manifested mainly in the venous vascular bed (sufficiently high doses are required to affect the arterioles). The expansion of the arterioles of the systemic circulation, leading to a decrease in blood pressure, can promote the activation of the sympathetic division of the autonomic nervous system with the occurrence of reflex tachycardia and an increase in myocardial contractility.

There are few long-lived drugs in modern pharmacology that can compete with nitroglycerin, which was discovered in 1847 by the Italian Ascanio Sobrero. True, initially nitroglycerin found no medical use at all - in 1851 Alfred Nobel invented dynamite on its basis, another long-lived substance that is still used in the national economy and in military affairs. Over time, with the development of medicine and pharmacology, nitroglycerin becomes one of the main drugs for the treatment of angina pectoris. And today, nitroglycerin is widely used in the treatment of coronary artery disease, due to its extremely fast and effective action, which makes it to this day the main drug for the relief of angina attacks.

Nitrates are used as antianginal agents for the treatment of unstable and vasospastic angina pectoris. IV dosage forms of nitrates are prescribed for acute myocardial infarction.

Classification of nitrates:

• Trinitrates: nitroglycerin; depot preparations of nitroglycerin.
• Isosorbide dinitrates: nitrosorbide, cardiket, cardiket retard, isoket.
• Isosorbide-5 mononitrates.

Time classification of nitrates:

• short-acting (up to 1 hour) - aerosols of nitroglycerin and isosorbide dinitrate, ensure good preservation of the active substance, provide a quick effect;
• moderately prolonged action (1-6 hours) - tablet preparations of isosorbitol dinitrate (cardiket, cardix, iso-mac retard), begin to act in 10-20 minutes, the duration of the effect is on average 3-4 hours;
• significantly prolonged action (6-24 hours) - retard forms of isosorbide dinitrate and isosorbide-5-mononitrate.

Classification of nitrates by the nature of the dosage form:

• absorbed through the oral mucosa - tablets of nitroglycerin under the tongue, aerosols of nitroglycerin and isosorbide dinitrate, which have a fast and reliable effect;
• for oral administration - various tablets, capsules of isosorbite dinitrate, nitroglycerin, isosorbite mononitrate;
• cutaneous application - nitroglycerin ointments and patches (have lost their clinical significance);
• intravenous administration - ampoules with a solution of nitroglycerin and isosorbide dinitrate (perlinganite 0.1% - 10 ml; isoket 10 ml) are dissolved in 200 ml of glucose, injected intravenously at a rate of 10 drops / min.

The mechanism of action of nitrates consists in the formation of nitric oxide, which has a vasodilating effect. The effect of using nitrates is to dilate the veins and reduce the preload on the heart, thereby reducing myocardial oxygen demand. In addition, nitrates have a direct coronary expanding effect. Increased doses of the drug cause dilatation of the arteries, even larger ones lead to dilatation of arterioles and the development of systemic hypotension.

In patients receiving transdermal dosage forms of nitrates that maintain a uniform concentration throughout the day, addiction (tolerance) to nitrates (tachyphlaxis) may occur. Tachyphlaxis develops especially quickly with intravenous administration - the first signs of tolerance can be observed 10-12 hours after the start of administration. In most cases, nitrate tolerance is lost after drug withdrawal. During the development of tolerance, the load should be reduced, replaced with other antianginal drugs. ACE inhibitors, captopril, can somewhat reduce the development of tolerance to nitrates.

Fundamentals of nitrate therapy

• with angina pectoris of the I functional class (FC), pain occurs only against the background of significant physical exertion: nitrates are prescribed before exercise; nitroglycerin is taken 5 minutes before the load, isosorbide dinitrate preparation - 1 hour;
• with angina pectoris II FC, it is also possible to take nitroglycerin before exercise, with frequent attacks, an extended form of the drug is taken;
• with angina pectoris III FC, drugs are shown with a duration of up to 12 hours (for daytime attacks, the drug is taken in the morning);
• with angina pectoris IV FC, it is necessary to provide an antianginal effect during the day: use forms of isosorbide-5-mononitrate with a duration of 16 hours; it is believed that the absence of the effect of nitrates within 8 hours will prevent the development of tolerance to them.

Contraindications to the appointment of nitrates:

• absolute contraindications: arterial hypotension (blood pressure less than 90/60 mm Hg), hypovolemia, shock, cardiac tamponade, myocardial infarction of the right ventricle, left ventricular failure with low filling pressure, hypersensitivity to nitrates;
• relative contraindications: increased intracranial pressure, hypertrophic cardiomyopathy, severe aortic stenosis, mitral stenosis, tendency to orthostatic arterial hypotension, angle-closure glaucoma;

A classic attack of angina pectoris is stopped by short-acting dosage forms of nitroglycerin and isosorbide dinitrate (a 0.5 mg nitroglycerin tablet under the tongue stops the attack within 1-3 minutes, provided that the factors that provoke the attack itself cease). The maximum effect occurs in 5-6 minutes, the total duration of the drug's action with sublingual administration does not exceed 10-20 minutes. If there is no effect, it is recommended to repeat taking the drug after 5 minutes. To stop an attack of angina pectoris, you can use a short-acting form of nitrosorbide, 10 mg.

The advantage of sublingual nitroglycerin intake is that the active substance is rapidly absorbed through the oral mucosa, bypassing the liver, and immediately entering the systemic circulation.

Patients with exertional angina pectoris, in the event of seizures due to physical exertion, are recommended to take sporadic nitrates (nitrates of short or moderately prolonged action are used) - immediately before exercise.

Patients who have a severe course of the disease (angina attacks occur with little physical exertion or at rest) are prescribed drugs of moderate or significantly prolonged action in order to ensure their antianginal effect during the day.

In the treatment of ischemic heart disease, a withdrawal syndrome is possible (worsening of the condition of patients with a sharp cessation of nitrate intake).

Side effects (most often develop during the first application, due to pronounced dilatation of intracranial veins and difficult outflow of blood from the brain):

• increased intracranial pressure, the appearance of throbbing headaches, a feeling of fullness in the head, tinnitus, facial hyperemia;
• a typical side effect is tachycardia, which is especially pronounced with nitrate monotherapy (tachycardia is leveled by beta-blockers, calcium channel blockers (verapamil, nicardipine, amlodipine, but not nifedipine);
• a rare side effect is bradycardia, which can occur with intravenous administration of nitroglycerin against the background of a pronounced decrease in blood pressure (atropine is used for correction);
• an unstable side effect - increased intraocular pressure;
• heartburn, nausea, vomiting, diarrhea are possible;
• allergic reactions are rarely observed, more often in the form of a skin rash;
• high doses can cause methemoglobinemia;
• aggravation of myocardial ischemia can occur in patients with angina pectoris combined with anemia;
• a sharp decrease in blood pressure, tachycardia, chest pain, nausea, vomiting, anxiety, accumulation of cyanide with the development of deadly hypoxia can cause sodium nitroprusside.

Drug interactions

• nitrates are incompatible with Viagra;
• the ability of nitrates to lower blood pressure is enhanced in combination with vasodilators, narcotic analgesics, and alcohol;
• the hypotensive effect of nitrates is enhanced in combination with vasodilators, antihypertensive drugs, ACE inhibitors, beta-blockers, calcium antagonists, procainamide, tricyclic antidepressants, MAO inhibitors, diuretics, ethanol;
• a sharp decrease in blood pressure can occur when nitrates are combined with sildenafil, other phosphodiesterase inhibitors;
• orthostatic collapse can develop while taking quinidine and novocainamide;
• increased blood pressure - in combination with dihydroergotamine;
• the combination of nitro drugs with heparin can cause a decrease in the effectiveness of the latter, which may require an increase in its dose.

ATTENTION! Information provided by the site website is for reference only. The site administration is not responsible for possible negative consequences in case of taking any medications or procedures without a doctor's prescription!

Nitrates, or nitrovasodilators (NVD), are a group of drugs that have vasodilating properties and differ in chemical structure. They are united by a mechanism of action: as a result of complex chemical transformations, all NVDs are converted into nitric oxide - a substance that is an analogue of the so-called endothelial-dependent relaxing factor. NO activates guanylate cyclase, resulting in the formation of cyclic guanosine monophosphate, which has the ability to relax vascular smooth muscle cells.

Nitrates are used to treat almost all forms of coronary artery disease. The presence of pronounced antianginal and anti-ischemic activity makes it possible to successfully use these drugs for the prevention and relief of seizures in patients with stable exertional angina. When they are taken, exercise tolerance increases significantly, the number of angina attacks decreases.
In general, the antianginal efficacy of nitrates in stable exertional angina is comparable to the efficacy of antianginal drugs of other groups (calcium antagonists, β-blockers). However, it should be noted that the clinical efficacy of nitrates in angina pectoris largely depends on which drug is used, in what dose and dosage form, and also on the scheme of its use.
Nitrates as antianginal drugs are also used to treat unstable angina pectoris, vasospastic angina pectoris. In the form of intravenous dosage forms, nitrates are usually prescribed for acute myocardial infarction (MI), but their effect on the prognosis of this disease has not been proven.
Previously, nitrates were widely used to treat patients with chronic heart failure, but recently they have been almost completely replaced by angiotensin-converting enzyme inhibitors.