The drug nitroglycerin. Nitroglycerin: properties, indications and contraindications, how to use in various forms and cases. Video: nitroglycerin in the “Live Healthy” program

Formula: C3H5N3O9, chemical name: 1,2,3-Propanetriol trinitrate.
Pharmacological group: organotropic drugs / cardiovascular drugs / nitrates and nitrate-like drugs.
Pharmachologic effect: vasodilator, antianginal, coronary dilatant.

Pharmacological properties

Nitroglycerin increases the concentration of the free radical nitric oxide (NO), which activates guanylate cyclase and increases the level of cGMP (which controls the dephosphorylation of myosin light chains) in vascular smooth muscle cells. Nitroglycerin mainly dilates venous vessels, reduces preload (venous return of blood) to the heart and end-diastolic filling of the left ventricle, and deposits blood in the venous system. Systemic dilation of arterial vessels (mainly large arteries) is accompanied by a decrease in blood pressure and total peripheral vascular resistance, that is, afterload. A decrease in post- and preload on the heart leads to a decrease in the oxygen demand of the myocardium; reduces elevated pulmonary capillary wedge pressure and central venous pressure; slightly increases heart rate (reflexively, in response to a decrease in stroke volume and systemic blood pressure, tachycardia is more pronounced with an upright body position), improves cardiac blood flow (except in cases of a significant increase in heart rate or a strong decrease in systemic blood pressure, when deterioration of coronary arterial blood pressure is possible blood flow) and weakens the resistance of the coronary arteries.
Nitroglycerin increases the pressure gradient in the area of ​​atherosclerotic stenosis of the coronary vessels, expands the large epicardial sections of the coronary arteries, provides blood supply even with subtotal stenosis, and includes collaterals, including by reducing the resistance to blood flow through them.
Nitroglycerin redistributes coronary blood flow in favor of ischemic areas (including subendocardial sections). In the presence of ischemic hypokinesia in certain areas of the myocardium, it helps restore local contractility. Nitroglycerin during myocardial infarction prevents the development of fatal arrhythmias and eliminates pathological stiffness of the myocardium.
Nitroglycerin reduces post-infarction left ventricular remodeling. Effectively inhibits platelet adhesion to the vascular endothelium and their aggregation. Nitroglycerin increases the threshold for the development of myocardial ischemia. In patients with angina pectoris and heart failure, it increases exercise tolerance, cardiac output, and reduces the frequency and severity of attacks. Significantly reduces the volume of mitral regurgitation. Nitroglycerin has a central inhibitory effect on the sympathetic tone of blood vessels, thereby inhibiting the vascular part of the formation of pain. Nitroglycerin normalizes energy processes and electrolyte metabolism - the activity of NAD-dependent dehydrogenases, the ratio of reduced and oxidized forms of nicotinamide coenzymes. Promotes the release of catecholamines in the heart and brain, has an indirect sympathomimetic effect on the myocardium, and changes the conformation of the troponin-tropomyosin complex.
Nitroglycerin can impair oxygen transport by promoting the conversion of hemoglobin to methemoglobin. Nitroglycerin dilates the meningeal vessels, which is accompanied by headaches. Nitroglycerin relaxes the smooth muscles of the esophagus, bile ducts, stomach, intestines, bronchi, and genitourinary tract.
Nitroglycerin is absorbed quite completely and quickly through the skin and from the surface of mucous membranes. When taken orally, it is largely destroyed in the liver, and then biotransformed in smooth muscle cells to form NO. With intravenous, subbuccal, sublingual use, “primary” hepatic degradation is excluded. The primary metabolites of nitroglycerin are mono- and dinitrates, the final metabolite is glycerol. When administered into the oral cavity in the form of an aerosol, the maximum concentration of metabolites is reached after 5.3 minutes (14.6 ng/ml), the relative bioavailability is 76%, and the half-life is 20 minutes. With sublingual administration, the maximum concentration of the main metabolites is reached by 120–150 seconds (0.2–0.3 ng/ml), the half-life of nitroglycerin is 1–4.4 minutes, of metabolites - 7 minutes, clearance is 0.3–1, 0 l/kg/min, volume of distribution 3 l/kg. When taking 6.4 mg of the drug orally, the maximum concentration of metabolites is reached after 20–60 minutes (0.1–0.2 ng/ml), the relative bioavailability is 10–15%, and the half-life of metabolites is 4 hours. With intravenous administration, the half-life is 1–3 minutes, the total clearance is 30–78 l/min; in heart failure, these indicators correspondingly decrease to 12 s−1.9 minutes and 3.6–13.8 l/min. In plasma, nitroglycerin is 60% protein bound. Nitroglycerin metabolites are mainly excreted through the kidneys, some with exhaled air from the lungs. When using buccal and sublingual forms, an attack of angina is stopped after 1.5 minutes, and the anti-ischemic and hemodynamic effects last up to 5 hours and 30 minutes, respectively. When taking small doses (2.5 mg), the hemodynamic effect lasts up to 30 minutes, large doses (Forte) - up to 5–6 hours (with large doses, hemodynamic effects appear after 2–5 minutes, and antianginal effects after 20–45 minutes). When applying the ointment, the development of antianginal effects occurs within 15–60 minutes and lasts 3–4 hours. The effects of transdermal forms occur within 0.5–3 hours and last up to 8–10 hours.

Indications

Coronary heart disease: angina pectoris (prevention, therapy), unstable angina, vasospastic angina (Prinzmetal), acute coronary syndrome, coronary artery spasm during coronary angiography, acute left ventricular failure (alveolar and interstitial pulmonary edema, cardiac asthma), acute infarction myocardium; controlled arterial hypotension during surgical procedures; chronic heart failure; prevention of hypertensive reactions during skin incisions, endotracheal intubation, sternotomy; esophageal dyskinesia; occlusion of the central retinal artery; functional cholecystopathy; biliary colic; acute pancreatitis; spastic intestinal dyskinesia.

Method of administration of nitroglycerin and dose

Sublingual (under the tongue): tablets per dose 0.15–0.5 mg, after 5 minutes, if necessary, take again; aerosol - to relieve an attack of angina - 1-2 doses under the tongue, pressing the dosing valve (you can repeat the dose, but no more than 3 doses in 15 minutes). With the development of acute left ventricular failure, it is possible to use 4 or more doses over a short period. Intravenously (diluted in isotonic saline or 5% glucose solution to a final concentration of 100 or 50 mcg/ml): 0.005 mg/min, dose increased by 0.005 mg/min every 3–5 minutes until a rate of 0.02 mg/min is reached (at ineffectiveness - further increase by 0.01 mg/min) or obtaining an effect. Orally: capsules and tablets are taken without breaking or chewing, before meals 2–4 times a day, preferably half an hour before physical activity, a single dose is 5–13 mg, but due to poor bioavailability it can increase to 19.5 mg. Transdermal: Each time I apply it to a new area of ​​skin and leave it on for 12–14 hours, after which I remove it for 10–12 hours to prevent the development of tolerance.
Subbuccal: The tablet is placed on the mucous membrane of the oral cavity (behind the cheek) and kept there until complete resorption: 3 times a day, 2 mg.
With the development of acute heart failure and in the acute period of myocardial infarction, nitroglycerin is prescribed only under strict control of hemodynamic status. Use nitroglycerin with caution in mitral and aortic stenosis, in patients with low systolic blood pressure (less than 90 mm Hg) and hypovolemia. In hypertrophic cardiomyopathy, taking nitroglycerin can lead to worsening and/or increased frequency of angina attacks. With prolonged uncontrolled use of nitroglycerin, prescribing high doses to children and patients with liver failure, the possibility of developing methemoglobinemia increases, which is manifested by the appearance of a brown tint in the blood and cyanosis. In such cases, it is necessary to urgently discontinue nitroglycerin and introduce an antidote - methylene blue (methylthioninium chloride). If there is a further need to use nitrates, then mandatory monitoring of the level of methemoglobin in the blood or replacement of nitrates with sydnonimines is necessary. To reduce the possibility of developing adverse reactions, caution must be exercised when using nitroglycerin together with drugs that have pronounced vasodilating and hypotensive properties; It is not recommended to take nitroglycerin in rooms with high ambient temperatures (sauna, steam bath, hot shower), while drinking alcohol, as well as using several tablets simultaneously or sequentially within a short period of time after the first dose. You should not chew capsules and tablets in order to relieve angina pectoris, since a large amount of the drug can enter the systemic circulation from the destroyed microcapsules through the oral mucosa. If you experience a headache or other unpleasant sensations in the head area, improvement can be achieved by taking sublingual drops of menthol or validol. Often only the first doses are poorly tolerated, then adverse reactions decrease. When using nitroglycerin with heparin together, it is necessary to increase the dose of heparin and at the same time strictly monitor the partially activated thromboplastin time. Use nitroglycerin with caution in elderly patients. Do not prescribe buccal forms of nitroglycerin to patients with gingivitis, aphthous stomatitis, diseases of the root system of the teeth and periodontium, and removable upper dentures. Uncontrolled use of nitroglycerin can lead to tolerance, which is expressed in a decrease in the duration and severity of effects with regular use or the need to increase the dose to achieve the same effects. With regular use of prolonged forms of nitroglycerin, especially ointments and patches, the drug is in the blood almost all the time, so the possibility of tolerance increases greatly. To prevent the development of resistance, co-administration of ACE inhibitors, calcium antagonists or diuretics or intermittent administration of nitroglycerin throughout the day is necessary.
Transdermal forms of nitroglycerin must be removed from the body at night so that there is a period free from the action of the drug. But at the same time, it is necessary to beware of the appearance of withdrawal syndrome, which is associated with a sharp cessation of the drug entering the body and is manifested by the sudden development of angina attacks. When administered intravenously, tachyphylaxis may occur; this requires an increase in the dosage of the drug. By the dynamics of pressure in the right atrium one can judge the degree of tolerance. When approaching 25% of the tolerance index, it is necessary to stop administering the solution. The appearance of tolerance during intravenous administration can be simulated by a decrease in the content of nitroglycerin in the solution due to its destruction under direct exposure to light rays, violation of the administration technique or its absorption on the walls of the plastic infusion system. It is necessary to use systems made of polyethylene, chemically pure glass, nylon, silicone, and Teflon. Do not use hydraulic lines that are too long. When administering nitroglycerin intravenously, it must be taken into account that after discontinuation of infusions and when transferring the patient to other forms of administration, an insufficient dose or withdrawal syndrome may occur, while an increase in the frequency of complications in the acute period of myocardial infarction is possible - an increase in the phenomena of circulatory failure, an increase in angina attacks, the formation of acute cardiac aneurysms, recurrence of myocardial infarction, increased incidence of myocardial ruptures.

Contraindications for use

Hypersensitivity, collapse, severe hypotension, myocardial infarction with severe hypotension (systolic blood pressure less than 90 mm Hg) and/or low end-diastolic pressure in the left ventricle or collapse, bradycardia less than 50 beats/min, right ventricular infarction, primary pulmonary hypertension, head injury, cerebral hemorrhage, increased intracranial pressure, cardiac tamponade, cerebral ischemia, toxic pulmonary edema, conditions that are accompanied by a decrease in end-diastolic pressure in the left ventricle (constrictive pericarditis, isolated mitral stenosis); severe aortic stenosis, angle-closure glaucoma, breastfeeding, pregnancy.

Restrictions on use

Hypertrophic cardiomyopathy (hypertrophic idiopathic subaortic stenosis), anemia, severe impairment of the functional state of the kidneys and liver, old age, hyperthyroidism.

Use during pregnancy and breastfeeding

The use of nitroglycerin during pregnancy is possible only when the expected benefit to the mother is higher than the possible risk to the fetus. During nitroglycerin therapy, breastfeeding should be stopped.

Side effects of nitroglycerin

Sense organs and nervous system: headache, feeling of fullness in the head, dizziness, weakness, psychotic reactions, motor restlessness, exacerbation of glaucoma, blurred vision; circulatory system and blood: palpitations, flushing, collapse, hypotension (including orthostatic), methemoglobinemia; digestive system: dry mouth, nausea, diarrhea, vomiting; skin: skin hyperemia, cyanosis; allergic reactions: burning and itching, allergic contact dermatitis (when using transdermal forms); others: development of tolerance to nitroglycerin, sensation of heat, hypothermia, paradoxical effects - an attack of angina, ischemia up to myocardial infarction and sudden death.

Interaction of nitroglycerin with other substances

Salicylates increase plasma nitroglycerin levels; Barbiturates accelerate the metabolism of nitroglycerin. Nitroglycerin reduces the anticoagulant effects of heparin (when administered intravenously) and the pressor effect of adrenergic agonists. Antiadrenergic and antihypertensive drugs, sildenafil citrate, vasodilators, calcium antagonists, MAO inhibitors, tricyclic antidepressants, ethanol, procainamide and quinidine enhance the systemic vasodilating and hypotensive effects of nitroglycerin. Methionine, ACE inhibitors, N-acetylcysteine ​​and salicylates increase the antianginal activity of nitroglycerin. Unithiol restores reduced sensitivity to nitroglycerin. Dihydroergotamine, alpha-adrenergic agonists, m-anticholinergics, histamine, corticosteroids, pituitrin, stimulants of the autonomic ganglia and central nervous system, snake and bee venoms, excessive insolation reduce the antianginal and vasodilatory effects of nitroglycerin.

Overdose

In case of an overdose of nitroglycerin, the following may occur: headache, a feeling of strong pressure in the head, dizziness, unusual weakness or fatigue, chills or a feeling of heat, fainting, increased sweating, nausea and vomiting, palpitations, cyanosis of the lips, palms or nails, hypotension, shortness of breath, mild rapid pulse, hyperthermia, increased intracranial pressure (development of cerebral symptoms up to the appearance of coma and seizures), methemoglobinemia. It is necessary: ​​transfer the patient to a horizontal position (to increase venous return to the heart, the legs are raised above the level of the head), if little time has passed since ingestion, then gastric lavage; plasma expanders, intravenous administration of alpha-adrenergic receptor agonists (for example, phenylephrine). The use of epinephrine as a cardiotonic agent should be avoided due to increased shock-like reactions. To eliminate methemoglobinemia, a 1% solution of methylthioninium chloride (methylene blue) or oxygen under pressure is used intravenously at a dose of 1–2 mg/kg. Monitoring of methemoglobin levels in the blood is necessary.

Nitroglycerin is a peripheral vasodilator; it has a direct effect on blood vessels and promotes their dilation. It is one of the most popular drugs used in cardiology. Available in various forms, each of which requires a special approach to use.

Nitroglycerin is a Russian drug based on the medicinal component of the same name - nitroglycerin, which is used in the prevention and treatment of disorders of the cardiovascular system. INN identical – Nitroglycerin. The name of the drug in Latin is Nitroglycerinum. Belongs to the group of nitrates and nitrate-like drugs, has antianginal and vasodilating properties, primarily affects venous vessels.

Pharmacodynamics, pharmacokinetics

The action of the drug is aimed at releasing a component in the smooth muscle tissue of blood vessels, such as nitric oxide. The substance promotes the activation of guanylate cyclase and an increase in the level of cyclic guanosine monophosphate, resulting in relaxation of the cellular structures of vascular smooth muscles. Under the influence of the drug, precapillary sphincters and arterioles relax to a lesser extent (compared to large veins and arteries).

The action of the drug is aimed at reducing the need for myocardium to absorb oxygen. This occurs due to a decrease in pre- and afterload (decrease in vascular peripheral resistance, dilation of veins, decrease in blood flow to the right atrium). The coronary blood flow is distributed in areas of the myocardium susceptible to ischemia.

Nitroglycerin therapy helps increase tolerance to active physical activity in patients diagnosed with angina pectoris and coronary artery disease. In case of heart failure, it helps to ease and relieve the work of the myocardium. In the pulmonary circulation it helps reduce blood pressure.

The therapeutic effect is felt after a couple of minutes. Pharmacokinetics is quite complex and mainly depends on the characteristics of the pathology and the patient’s body. The drug is quickly absorbed from the surface of the oral mucosa and after five minutes is already detected in the blood.

Average price for the drug in Moscow, depending on the form of release

The composition of the drug depends on the form of release:

  1. Tablets, capsules. The base is nitroglycerin (0.5 mg), as well as additional components: magnesium stearate, lactose monohydrate, crospovidone, starch, sugar.
  2. Solution in ampoules. 1 ml of the drug contains 10 mg of nitroglycerin and ethanol.
  3. Ointment. The composition contains nitroglycerin and lanolin (vaseline base).
  4. Spray. The composition of the colorless liquid is based on nitroglycerin in a dosage of 400 mcg, 1% ethanol solution.

The approximate cost of Nitroglycerin, depending on the form of release and dosage in Moscow, is presented in the table (Table 1).

Table 1 - Cost of Nitroglycerin

As can be seen from the table, the cost of the drug, regardless of the release form, is quite acceptable. It is also worth noting that the prices presented are the average for Moscow. In the regions you can purchase Nitroglycerin at an even more attractive price.

Instructions for use of the drug for heart pathologies

The attending physician decides in what form the drug should be taken. It is important to pay attention to the features of the use of Nitroglycerin, depending on the types of its release.

Indications and restrictions

The drug is prescribed for the following acute conditions:

  • ischemia;
  • angina pectoris;
  • arterial spasms;
  • coronary syndrome;
  • myocardial infarction;
  • left ventricular failure (due to cardiac asthma, alveolar or interstitial pulmonary edema).

Indications may also be a chronic course:

  • heart failure;
  • sternotomy;
  • angina pectoris.

Contraindications for use:

Sublingual tablets

Tablets are prescribed to relieve attacks of angina pectoris, blockage of the central artery, heart attack, left ventricular failure. To relieve an acute condition, one tablet is prescribed once (or half a tablet, depending on the patient’s condition and tolerability of the drug).

The drug is taken sublingually (under the tongue), it must be kept in the mouth until the drug is completely absorbed.

Do not bite or swallow the tablet! If the effect of using the drug occurs before the tablet is completely absorbed, then the remaining part should be spat out.

If after taking the first tablet the effect is insufficient, then the next tablet can be taken no earlier than five minutes after the first. You can take no more than three tablets at a time; if this is not enough, you need to call your doctor or an ambulance, as this may be a myocardial infarction.

The tablet is effective for half an hour; if this is not enough, then special prolonged forms of nitrates are prescribed. Addiction to Nitroglycerin develops extremely rarely, but if it occurs, the dosage of the drug is increased to two or three tablets.

Capsules

This form is prescribed in the same cases as the tablet form. The capsule must be taken sublingually and dissolved until it is completely dissolved. Single dose – one or two capsules. The dosage may be reduced depending on the patient’s condition (the treatment procedure is similar, only the capsule must not be completely dissolved, but spat out when about half remains).

The daily amount of the drug is prescribed by a doctor, but should not exceed 6 capsules. In exceptional cases, it is possible to prescribe capsules orally with plenty of water (one capsule no more than 3 times a day).

The therapeutic effect is achieved fairly quickly, in most cases within a minute. In rare cases, the process takes longer - up to 3 or even 5 minutes. If after this time the effect is weak, it is recommended to take another capsule or two. Lack of results is a reason to urgently call a doctor.

How to apply the spray?

Prescribed for the prevention and elimination of angina pectoris. At the first manifestations of attacks, it is necessary to introduce a dosage of Nitroglycerin: shake the bottle, place the valve under the tongue, make 1-2 presses on the dispenser.

At the moment of injection, you must hold your breath for 20-30 seconds. Then close your mouth and wait a few seconds. If necessary, the doctor prescribes an increased dosage - the procedure must be repeated 1-2 times, with an interval of 5 minutes. A single dosage should not exceed 3 injections.

The advantages of using this form of the drug:

  • the effect occurs much faster than when taking tablets or capsules;
  • The spray contains menthol, which reduces the severity of side symptoms (nausea, dizziness), as well as enhances the effect of nitroglycerin;
  • the price is also quite affordable for a wide range of consumers.

Nitroglycerin ointment

Refers to local vasodilating and blood circulation-normalizing drugs. Used in proctology and urology. Eliminates painful sensations due to the development of anal fissures and hemorrhoids, prescribed in the complex therapy of erectile dysfunction and increasing potency.

In proctology it is used externally. A small amount of ointment is applied directly to the anal area. Processed 2 to 4 times a day. The optimal duration of therapy is a month.

In urology, the drug of this form is also used externally. Apply the ointment in a thin layer to the genital organ, using soft, massaging movements, while avoiding getting the product on the foreskin. It is recommended to use the product no more than once a day, shortly before expected sexual intercourse.

Nitroglycerin in ampoules

Nitroglycerin solution for intravenous administration is prescribed for severe, prolonged pain of ischemic origin. It is also used for heart failure and pulmonary edema due to myocardial infarction and arterial hypertension.

To prepare the solution, it is necessary to dilute the ampoule containing Nitroglycerin with a 5% glucose solution. You should get a concentrated solution of 100 µg/ml. It is important to note that intravenous administration of the solution should only be done in a hospital. The frequency of drug administration is controlled by a doctor and is determined strictly on an individual basis. The dosage of the drug and the rate of administration are presented in the table (Table 2).

Some features of the use of the drug

Before using Nitroglycerin, you need to familiarize yourself with the features of its use and effect on the body in various pathologies.

For blood pressure disorders

Nitroglycerin is not a specialized drug for lowering or increasing blood pressure, since its main purpose is to relieve attacks of angina. However, it does affect blood pressure levels. The drug acts almost instantly, within 1-3 minutes, helps to expand the lumen of blood vessels, relieves spasms of smooth muscles. In addition, blood pressure decreases.

Despite this fact, the use of Nitroglycerin as monotherapy for high blood pressure is not recommended. Doctors claim that this fact (a decrease in blood pressure while taking the drug) is a side effect.

Normalization of potency

As we have already found out, Nitroglycerin helps to dilate blood vessels and normalize blood circulation. It is precisely these properties of the drug that urologists took note of. After applying nitroglycerin ointment to the flesh of the genital organ, it is quickly absorbed, then its effect on the circulatory system is activated. This effect is actively used to increase potency.

According to numerous reviews, nitroglycerin-based ointment has an active effect on increasing sexual desire in men, eliminates signs of erectile dysfunction, is used in the complex treatment of impotence and has positive results. Despite all the benefits of Nitroglycerin, it is strictly unacceptable to use it for self-medication. Consultation with a specialist is necessary.

Possible side effects, precautions.

During therapy, side effects may occur:


The most dangerous adverse reaction is heart attack and sudden death. To avoid dangerous consequences, you must avoid self-medication with the use of Nitroglycerin and strictly adhere to the dosage prescribed by your doctor. It is also necessary to carefully listen to your well-being during the treatment period. If your health condition worsens, you should stop taking the drug and consult a doctor immediately.

Overdose

This condition manifests itself in this way:

  • a sharp decrease in blood pressure;
  • reflex tachycardia;
  • excruciating temporal pain and dizziness;
  • asthenia;
  • daytime sleepiness;
  • vomit;
  • state of shock.

Help in case of overdose:


It is also possible to prescribe hemodialysis, oxygen therapy, and blood transfusions.

Compatibility with alcohol

The main rule during drug therapy is abstinence from consuming alcoholic beverages. This combination is especially dangerous for drugs intended to eliminate problems with the heart and blood vessels. The consequences can be extremely severe:


In case of pathologies of the heart and blood vessels, drinking alcohol is generally contraindicated. And its combination with a powerful medicine can even lead to death.

Similar drugs: which is better and cheaper?

Drugs intended for the prevention and treatment of cardiovascular pathologies are produced by pharmaceutical companies in a wide range. Among them you can find drugs with similar indications and effects.

Generics of Nitroglycerin include: Nitrocor, Nitromint, Nitrospray; analogues in terms of their effect include Validol, Corvalment. In order to understand which of the drugs has a more affordable price and the most effective therapeutic effect, you need to familiarize yourself with each of them in more detail.

The drug contains the substance nitroglycerin. Intended for the treatment of various forms of angina pectoris. Contraindicated in glaucoma, severe traumatic brain injury, severe hypertension, and cerebrovascular accidents. During pregnancy and breastfeeding, it can be prescribed at the discretion of the attending physician, but in a minimal dosage and under the supervision of a specialist.

Available in the form of sublingual tablets. Prescribed as a tablet for a single dose. The tablet must be taken sublingually and dissolved until it is completely dissolved.

The daily dosage is set by the doctor individually for each patient. In rare cases, up to 4 tablets are prescribed for a single dose (each tablet must be dissolved at intervals of 5 minutes).

If you compare Nitrocor with Nitroglycerin, you can note that the original has a wider scope of application. However, the analogue causes significantly fewer side effects. As for the cost, Nitrocor is a more expensive drug compared to a similar dosage form of Nitroglycerin. The approximate cost for 40 Nitrocor tablets containing 0.5 mg of nitroglycerin is about 65 rubles.

Based on nitroglycerin, another drug is produced in aerosol form -. In addition to the main active ingredient, it contains auxiliary components - propylene glycol and ethanol. Belongs to the group of peripheral vasodilators, prescribed for angina pectoris and acute left ventricular failure.

Contraindicated in young people under 18 years of age, with hemorrhagic stroke, anemia, thyroid disorders, glaucoma. Pregnant and lactating women are prescribed in exceptional cases, at the discretion of the doctor.

Before use, the aerosol can must be shaken thoroughly, then by pressing the dispenser, make 2 injections under the tongue. As prescribed by the doctor, the single dosage can be increased, but a new injection of the drug can be done no earlier than after 10 minutes.

Price – about 180 rubles per 10 ml. It is worth noting that this cost is almost twice that of Nitroglycerin in a similar release form. Also, the original (compared to the generic) has a wider scope of use.

- another antianginal medicine based on nitroglycerin. Allows you to dilate arteries and veins, reduce pre- and afterload, and is prescribed for the prevention and relief of angina pectoris, in acute forms of heart attack and left ventricular failure.

Contraindicated in cases of hypotension (pressure readings below 90 mm Hg), hypertrophic cardiomyopathy, hemorrhagic stroke, toxic pulmonary edema, glaucoma. It is not recommended to use the drug during pregnancy and breastfeeding.

Available in spray form. The medicine must be sprayed under the tongue; a single press is sufficient. The frequency of daily use of the drug is determined by the doctor, but should not exceed 16 injections.

10 ml of the drug can be purchased for about 140 rubles. In terms of cost, the analogue is higher than the original; according to other criteria, both drugs are generally identical.

Unlike the drugs presented above, it does not contain nitroglycerin. The composition includes menthol, a solution of which is prepared in isovaleric acid. It has a sedative effect, dilates blood vessels, and can eliminate headaches.

However, it is not used as a treatment for coronary heart disease. It can be prescribed as a remedy to relieve mild attacks of angina pectoris. Well tolerated, the only contraindications include intolerance to the composition.

Directions for use: The tablet must be placed under the tongue and dissolved until completely dissolved. The procedure can be repeated no more than 5 times a day. The approximate cost for 20 tablets of 60 mg is 55 rubles.

Validol is quite difficult to compare with the effect of Nitroglycerin, since the former has a rather weak effect on the functioning of the cardiovascular system and is more often prescribed as a prophylaxis or relief of minor attacks.

The composition is absolutely similar to Validol, it contains a menthol solution. Promotes the expansion of coronary vessels, the antianginal effect of the drug is weakly expressed. Prescribed for mild attacks of angina pectoris, for problems in the psycho-emotional state, and helps with motion sickness. Contraindicated only in case of hypersensitivity to menthol.

Available in the form of capsules that must be taken sublingually. It is recommended to first bite the capsule with your teeth, this will speed up the effect of the medicine. Daily dosage – no more than 3 capsules.

A package of capsules can be purchased for about 50 rubles. Despite the affordable cost, the effect of the medication is weak in eliminating acute pathologies of the heart and blood vessels. More suitable for carrying out preventive measures and relieving angina attacks.

Nitroglycerin tablets sublingual contain an active ingredient nitroglycerine and additional components: lactose, crospovidone CL, macrogol 6000, povidone 25.

Nitroglycerin solution contains active ingredient nitroglycerine and additional components: potassium dihydrogen phosphate, sodium chloride, water for injection.

Spray Nitroglycerin contains an active ingredient nitroglycerine , and also as an additional component ethanol 95%.

Release form

Available in the form tablets, which are taken sublingually. The tablets are white or white with a yellowish tint. The tablet may be rough in appearance. Contained in polymer containers or in blister packs. In packs from 10 to 100 pieces.

Also available Nitroglycerin solution 1% in ampoules of 5 ml and 1% solution of nitroglycerin in oil in capsules.

Nitroglycerin sublingual spray– a clear, colorless liquid, contained in 10 ml bottles, the kit also includes a mechanical dosing pump.

There are also other forms of release of the drug - sublingual drops, a concentrate for preparing a solution for administering the substance nitroglycerin intravenously, films on the gums.

pharmachologic effect

Nitroglycerin is a nitrogen-containing organic compound that primarily has venodilating effect .

Nitroglycerin formula: C3H5N3O9.

Pharmacological group of the drug: nitrates and nitrate-like agents.

The reaction to produce the substance nitroglycerin is described in chemistry textbooks. Nitroglycerin is an explosive substance, but the drug contains a very low concentration of it.

The substance acts due to the release of nitric oxide from the molecule, which is a natural endothelial relaxing factor. The mechanism of action of nitroglycerin is as follows: under the influence of nitric oxide inside the cells, the concentration of cyclic guanosine monophosphatases As a result, a barrier is formed for calcium ions to enter smooth muscle cells. At the same time, smooth muscle cells relax, blood vessels dilate, which reduces venous return to the heart and the resistance of the systemic circulation, that is, preload and afterload. As a result, the myocardium's need for oxygen decreases.

Due to the expansion of the coronary vessels, coronary blood flow is activated, redistributing to areas where blood circulation is reduced. This helps improve oxygen delivery to the myocardium.

After reducing venous return, filling pressure decreases, blood flow in the subendocardial layers improves, pressure in the pulmonary circulation decreases, and regression of symptoms in patients with pulmonary diseases decreases.

Wikipedia indicates that nitroglycerin has a central inhibitory effect on the sympathetic tone of blood vessels, while inhibiting the vascular component of the formation of pain. Under the influence of nitroglycerin, smooth muscle cells of the bronchi, gallbladder, urinary tract, esophagus, bile ducts, and intestines relax.

Pharmacokinetics and pharmacodynamics

Nitroglycerin, when applied sublingually, begins to act 1-1.5 minutes after application. The effect lasts for approximately thirty minutes. Absorbed quickly and completely from the surface of the mucous membranes. Immediately enters the systemic circulation. If the drug is used in a dose of 0.5 mg, its bioavailability is 100%, and the maximum plasma concentration is observed after 5 minutes. The distribution volume is very large. The connection with plasma proteins is 60%.

When taking the spray, it is quickly and completely absorbed. The maximum plasma concentration is observed after 4 minutes. passes quickly, with participation nitrate reductase . In this case, di- and mononitrates are formed, the final result is . Excreted through the kidneys. Less than 1% of the dose taken is excreted unchanged. The half-life when taken sublingually is 2.5-4.4 minutes.

Nitroglycerin accumulates in the walls of blood vessels and binds tightly to .

Indications for use of Nitroglycerin

There are the following indications for the use of Nitroglycerin:

  • to eliminate seizures ;
  • at ;
  • at embolism central retinal artery;
  • at left ventricular failure (reception is indicated for ).

Contraindications

The drug should not be used by people who have the following diseases and body conditions:

  • high sensitivity of the body to nitrates;
  • hypertension cranial;
  • constrictive pericarditis (if there is a decrease in left ventricular filling pressure);
  • hypovolemia uncontrolled;
  • isolated mitral stenosis ;
  • heart failure ( under conditions of low or normal pressure in the pulmonary artery);
  • hemorrhagic;
  • collapse ;
  • subarachnoid hemorrhage ;
  • head injury recently suffered by the patient;
  • pulmonary edema toxic;
  • idiopathic hypertrophic subaortic stenosis ;
  • (closed-angle form) under conditions of high intraocular pressure;
  • severe anemia ;
  • patient age under 18 years;
  • shock ;
  • cerebrovascular accident;
  • arterial hypotension ;
  • while taking the drug Sildenafil ( );
  • and natural.

Before taking the drug in tablets or other forms, please note that patients with severe and severe liver failure Nitroglycerin for the heart is prescribed with caution.

Side effects

During the use of Nitroglycerin, patients often develop a transient, sensation may occur, and sometimes the readings decrease. (this symptom most often develops if a person is in an upright position).

If an overdose of tablets and other forms of the drug occurs, the patient may develop orthostatic collapse , in this condition, the patient’s blood pressure drops sharply when a person moves from a horizontal position to a vertical one.

Thus, it should be borne in mind that such a medicine may cause the following side effects:

  • Nervous system, sensory organs: headache, feeling of fullness in the head, , feeling of weakness, motor restlessness, deterioration in vision clarity, psychotic manifestations, exacerbation of glaucoma.
  • Heart and blood vessels hematopoietic system: feeling of flushing to the face, hypotension, palpitations, methemoglobinemia, collapse.
  • Digestive system: vomiting, nausea, , the appearance of dry mouth.
  • Skin : skin hyperemia, cyanosis.
  • Allergy : burning sensation, contact (if transdermal forms are used).
  • Other manifestations: sensation of heat, development of paradoxical effects - , angina attack , possible development myocardial infarction with sudden death.

Instructions for use of Nitroglycerin (Method and dosage)

In modern medicine, the use of an alcohol solution of nitroglycerin sublingually is used in rare cases. The solution is applied under the tongue - 2-3 drops or dripped onto a piece of sugar.

Nitroglycerin tablets, instructions for use

The tablets are used sublingually - kept under the tongue until completely absorbed, but the tablet should not be swallowed. The tablet should be taken immediately after the development of pain, 0.5-1 mg per dose. Often patients with stable angina note the onset of effect even after using smaller doses (1/2-1/3 table). Therefore, if the pain goes away quickly, you don’t have to dissolve the rest of the tablet. As a rule, after resorption of the tablet, the effect appears within 0.5-2 minutes; some patients note an improvement in their condition within 3-4 minutes.

If the antianginal effect is absent during the first 5 minutes, you should also take 0.5 mg of the drug. If there is no effect even after taking two tablets, you should immediately consult a doctor. After sublingual administration, the effect of Nitroglycerin continues for 45 minutes.

In rare cases, tolerance to Nitroglycerin (its sublingual forms) may develop, in which case the patient gradually increases the dose - up to 2-3 tablets.

Nitroglycerin spray, instructions for use

The use of a spray to prevent an attack of angina involves the use of 1-2 doses under the tongue. To receive one dose, you need to press the dosing valve. Do not use more than 3 doses within 15 minutes. If the patient has developed acute left ventricular failure, 4 or more doses may be administered over a short period.

It is important to monitor the effectiveness of treatment, adjust doses, and, in case of prolonged use, replace them with medications from other groups.

Overdose

In case of an overdose of the drug, the patient may develop a headache, blood pressure also decreases, and a reflex , orthostatic hypotension , dizziness , vomiting and , redness of the face, asthenia , feeling of heat, intense.

It should be remembered that taking very high doses of the drug (i.e. more than 20 mg/kg) can lead to cyanosis , methemoglobinemia , tachypnea , dyspnea , orthostatic collapse . If a serious overdose occurs, death is also possible. Death from an overdose of Nitroglycerin can occur if prompt assistance is not provided to a patient who has taken an excessive dose of the drug. In this case, after a few hours it may occur , and later – death.

If a slight overdose has occurred, you need to transfer the person to a lying position, making sure that his legs are elevated. If a severe overdose is noted, the use of general methods of shock and body therapy is practiced. In particular, they replenish the volume of circulating blood, prescribe Norepinephrine, . Contraindicated for use .

If the patient has developed methemoglobinemia, it is practiced to take it in the form of sodium salt, taken orally or intravenously. Appointed oxygen therapy, blood transfusion.

It should also be noted that the risk of serious consequences increases when taking Nitroglycerin after drinking alcohol. The lethal dose of Nitroglycerin and alcohol has not been determined, but with such a combination in any dose, the risk of serious consequences increases sharply.

Interaction

The medicine may interact with other drugs, so Nitroglycerin should be taken with caution in the following combinations:

  • With simultaneous administration of salicylates, the level of nitroglycerin in plasma increases.
  • When taken simultaneously barbiturates the metabolism of nitroglycerin is activated. If Nitroglycerin is taken simultaneously with adrenomimetics , their pressor effect will decrease.
  • Nitroglycerin reduces the anticoagulant effect (when administered intravenously).
  • The hypotensive and systemic vasodilating effect of Nitroglycerin is enhanced by simultaneous administration antiadrenergic, hypotensive medications, as well as

    Storage conditions

    It must be protected from moisture and stored at a temperature of no more than 25 °C.

    Best before date

    The shelf life of nitroglycerin is 2 years.

    special instructions

    It is necessary to ensure that the Nitroglycerin solution does not come into contact with the skin, as it can be absorbed and lead to the development of a headache.

    You should consider not only what the tablets are used for, but also their side effects. In particular, it should be remembered that when taking them, blood pressure can sharply decrease and manifest itself dizziness . These symptoms are most pronounced when drinking alcohol, during hot periods and during physical activity.

    Over time, the patient may become accustomed to the drug, so an increase in dose may be required. If while taking the drug develops headache , this symptom can be reduced by reducing the dose of the medicine or taking it at the same time.

    When taken, the reaction may slow down, so at this time you should not drive or work with precise and dangerous mechanisms.

    To reduce the risk of side effects, you should not take the drug simultaneously with drugs that have a hypotensive and vasodilating effect.

    In order to relieve an attack of angina, do not chew the tablet to prevent excess amounts of the active substance from entering the bloodstream.

    Synonyms

    Angiolingual , Nitroglycerol , Anginin , Anhibid , Anguished , Glyceryl trinitrate , Angorin , Nitrangine , Myoglycerin , Nitrocardiol , Nitromint , Nitroglin , Nitrostat , Nitrozell , Trinitroglierol , Trinitrine , Trinitrol .

    Analogs

    Level 4 ATX code matches:

    Drug analogues are drugs Nirmin , Nit-ret , Nitradisk , Nitrosorbide , aerosol, etc. Before changing the medicine, you should always consult your doctor.

    For children

    The use of Nitroglycerin for the treatment of children is not practiced.

    With alcohol

    You should not take alcohol at the same time as Nitroglycerin, as the risk of serious side effects increases.

    During pregnancy and lactation

    Contraindicated during natural feeding. Can be taken only for health reasons.

Diseases of the cardiovascular system affect most of the world's population. To eliminate the symptoms of such diseases, it is recommended to use the most effective drugs, of which nitroglycerin is the drug of choice.

The medicinal group to which the drug belongs is antianginal drugs. This means that it reduces or completely eliminates attacks of pain that occur with heart pathologies.

pharmachologic effect

It is a peripheral vasodilator. It causes relaxation of peripheral vessels, mainly valve veins. It reduces the heart's need for O2 oxygen by relaxing the tone of the venous vessels, which reduces the flow of blood to the right side of the heart, and also eliminates high peripheral vascular resistance - total peripheral vascular resistance.

The main component is nitric oxide. It represents a factor that relaxes endothelial structures. Nitric oxide increases the amount of cyclic guanosine monophosphate inside cell membranes, causing the formation of an obstacle to the passage of calcium ions into cardiomyocytes. Calcium ions cause narrowing of the walls of blood vessels. Due to the fact that they do not accumulate inside the cell, the smooth muscle layer of the vascular wall relaxes, the vascular walls do not narrow, and the high level of oxygen demand of the myocardium (muscle layer) disappears.

Dilated vessels of the central sections - coronary arteries and veins improve their own blood flow, the metabolic redistribution function of oxygen ions that saturate the myocardium.

A decrease in the flow of venous blood causes the development of minimal pressure in the pulmonary circulation. The level of pressure in systole drops, and the symptoms of pulmonary failure regress.

The drug also acts on the sympathetic part of the nervous system, suppressing the action of its main components that cause a painful (angiotic) attack.

Nitroglycerin can dilate the vessels of the meningeal (brain) membrane, causing headache, which is a common side effect. The drug relaxes the muscle walls of the bronchial and intestinal tissues, esophageal sphincters, biliary and urinary tract structures.

Positive effects of the drug:

  1. Reduced cardiac workload.
  2. Reduced pressure.
  3. Vasodilation.
  4. Redistribution of blood flow to ischemic areas.
  5. Reduction of angiotic attacks.
  6. Increasing the ability to exercise during angina pectoris (angina pectoris).
  7. Relaxation of the walls of organs and their muscles.

Release form

Nitroglycerin is available in the following forms:

  • tableted;
  • infusion;
  • spray.

In some countries it is available as:

  • patch;
  • sublingual drops;
  • gingival films.

The main components are nitric oxide and glycerin, and additional components are lactose, sodium chloride and other chemical compounds.

Instructions for use

Indicated for the treatment of angina pectoris, relief of angiosis (pain) syndromes, myocardial infarction and unstable angina.

In some cases, drugs can be used to treat pathological conditions of the digestive tract(because it relaxes the smooth muscle layers of the intestinal walls), with pancreatitis, biliary colic and biliary dyskinesia.


During an angina attack, take one tablet sublingually. If its effectiveness is too low, then the next one is taken only after 5-10 minutes. If the pain syndrome has been relieved, but the tablet has not completely dissolved, then it must be removed from the mouth. A maximum of 3 tablets can be used during an attack. If there is no effect from 3 tablets, you should urgently call emergency help. The effect of the tablet form of the drug is absent in case of angina pectoris and acute myocardial infarction.

Before physical activity, you also need to take 1 tablet of nitroglycerin.

The use of a prolonged-release drug is recommended as a preventive measure for angina pectoris. They use sustak-forte and nitrong.

Important!

The solution for intravenous infusion is administered only in a cardiology department for decompensated vascular and cardiac pathologies in combination with a serious complication - acute functional ventricular failure.

The drug is diluted in an isotonic sodium chloride solution and administered dropwise.

The spray is used to stop angina attacks. You need to take the dispenser with the medicine, press it 2 times, spray it into your mouth. You need to hold your breath. There is no need to swallow the dissolved mass immediately. You need to wait 5-10 seconds. The effect of the drug occurs within 1.5-2 minutes. In case of angina pectoris, you can press the maximum 3 times, in case of ventricular failure - 4 times.

Contraindications

For treatment with the drug, it is important to exclude those conditions in which nitroglycerin is contraindicated. If this rule is not followed, the patient's condition may worsen and complications may arise that can lead to death.

Important!

The use of nitroglycerin in children is not indicated, since there is insufficient data indicating the effectiveness and safe use of the drug.

Some dosage forms are not recommended for use in pathologies of the cardiovascular system.

Disease Release form that cannot be used
Pathological indigestibility of glucose and galactose
Shock
Taking phosphodiesterase inhibitors (Viagra)
Pills
Shock states (+ cardiogenic)
Hypotonic crises (systolic less than 89 mmHg)
Ventricular hypertrophy
Adhesive pericarditis
Cardiac tamponade due to pericarditis
Decompensated narrowing of the mitral and aortic orifices
Intracranial pressure
Acute myocardial infarction
Sublingual spray
Narrowing of the aortic valve opening
Toxic left ventricular failure
Adhesive pericarditis
Isolated narrowing of the bicuspid valve opening
Intracranial hemorrhage
Atherosclerosis of cerebral (brain) vessels
Hypovolemic shock
Injection

Nitroglycerin should be used with caution in the following conditions:

  • strokes;
  • anemic syndrome;
  • hypothyroidism and hyperthyroidism;
  • decompensated kidney failure;
  • decompensated liver failure;
  • epilepsy;
  • head injuries;
  • arrhythmias.

Pregnancy

During pregnancy and breastfeeding Nitroglycerin is not indicated. It is prescribed only in cases where the productivity and effectiveness of treatment is high, and the threat of intrauterine pathologies of the fetus is absent or minimal. After a full examination and consultation with specialists, nitroglycerin is recommended to eliminate angiotic attacks.

Alcohol

Alcohol and nitroglycerin are incompatible things. When taking the drug in combination with alcoholic beverages, cardiogenic shock may occur (sharply decreased blood pressure, fainting). Therefore, it is necessary to completely eliminate alcohol consumption so that an urgent state does not develop.

Kidneys and liver

Nitroglycerin, when taken orally, passes through the esophagus, stomach, and intestines, spreading through the bloodstream. The highest concentration appears after 3-6 minutes. Breaking down into metabolites in the liver, the final breakdown product is glycerol. The drug is excreted by the kidneys.

For pathologies of the liver and kidneys in decompensated stages, the use of nitroglycerin should be avoided. This is due to the fact that if these organs are dysfunctional, the drug will not be metabolized and eliminated completely from the body. This can cause severe heart failure, dizziness and headache. The drug will lose its effectiveness and cause harm to the body.

Dosage: how to take

The effect of nitroglycerin, when used sublingually, begins to appear 1-2 minutes after administration. The duration of the effect is 20-30 minutes.

Depending on the form of release, nitroglycerin has different indications for use.

In the table we will consider how it is used in therapeutic practice. Dosages of the drug are prescribed individually by the attending physician.

Release form Disease Directions for use and dosage
Pills Angina pectoris, angina attack and its prevention 1 tablet (0.5 mg) under the tongue to eliminate an attack.
As a permanent therapy for angina pectoris, 1 tablet orally 1 time per day.
Solution for infusion Uncomplicated myocardial infarction, acute form;
necrosis of the heart muscle complicated by left ventricular failure;
unstable angina (angina at rest, Prinzmetal);
thrombosis of the central vessels of the retina;
Hypotension during surgical operations to reduce blood loss and prevent the development of severe anemia.
Intravenous drip administration of a 1% solution of nitroglycerin in 100 ml of isotonic sodium chloride solution.
Spray Angina pectoris It is used under the tongue to relieve an angioedema attack.

Side effects

Undesirable effects may occur when using nitroglycerin. The use of the drug can provoke the development of:

  1. Redness of the skin.
  2. Depression, fatigue.
  3. Transient headaches.
  4. Visual impairment in the form of midges in front of the eyes or flashes of light.
  5. Hyperhidrosis.
  6. Nausea, gag reflex.
  7. Tachycardia.
  8. Skin rashes.

Overdose: how to prevent it

Repeated intake of more than 3 nitroglycerin tablets within 15-20 minutes can lead to an overdose of the drug. Taking 3 nitroglycerin tablets at a time is unacceptable. The first signs appear after taking 4 tablets over 10 minutes (20 mc/kg). When the drug concentration in the blood exceeds 100 mg/kg, death occurs.

When taking the drug parenterally, the risk of overdose is minimal, because the rate of administration and dosage are carefully selected by a specialist.

Clinical symptoms of overdose are:

  • fainting;
  • a sharp drop in pressure;
  • tachycardia (due to increased tone of the sympathetic nervous system);
  • dizziness;
  • feeling of tide;
  • dyspeptic disorders;
  • paleness of the skin;
  • disorientation;
  • maladjustment;
  • anxiety;
  • general weakness;
  • lack of air;
  • chest tightness.

If an overdose occurs, it is necessary to urgently exclude the use of the drug. Place the patient in a certain position so that the legs are higher than the head.

It is prohibited to perform gastric lavage and the use of enterosorbents due to the fact that nitroglycerin is used sublingually (that is, it is absorbed into the systemic bloodstream without passing through the digestive tract).

There is no specific antidote therapy for nitroglycerin.

Important!

Long-term constant use of Nitroglycerin spray and patches can be addictive due to the fact that it is constantly in the bloodstream. In order to avoid this, you need to skip days of application. The patch can be applied after 1 day, and the spray can be used only to stop an attack if it has already happened.

Complications arising from overdose:

  1. Shock states.
  2. Loss of blood circulation in the brain.
  3. Toxic left ventricular failure.
  4. Kidney failure.
  5. Liver failure.

Analogs and prices

Nitroglycerin belongs to the group of nitrates. They are divided into:

  • short-acting - nitroglycerin itself,
  • long-acting - isosorbide dinitrate, mononitrate, etc.

A feature and important difference of nitroglycerin is the rapid development of its maximum effect. The cost of nitroglycerin ranges from 12 rubles to 700 rubles.

Analogues of nitroglycerin are long-acting drugs from the nitroglycerin group.

Other analogues are nitrocor, nitro-time, nitropentone and others.

Important!

It is prohibited to independently change the drug prescribed by the doctor!

Table of current prices for the drug Nitroglycerin in online pharmacies. The last data update was 10/21/2019 00:00.

56.00 rub. RUSSIA

Combination with other drugs

The drug can be combined with other drugs.

When angina pectoris is combined with arterial hypertension, nitroglycerin is combined with antihypertensive drugs - diuretics (), B-blockers (Bisoprolol), ACE inhibitors (Captopril). The combination of these drugs causes a persistent hypotensive effect.

Treatment of angina pectoris is complex. In addition to taking nitroglycerin, other drugs from the antianginal group are used - B-blockers (Bisoprolol) and calcium channel blockers (). This therapy is used for exertional angina with functional classes 3 and 4. With such angina pectoris, shortness of breath and anginal attacks occur with moderate or minor physical activity.

Also, for severe dangerous types of angina and AMI, antiplatelet agents (Cardiomagnyl) and anticoagulants (Heparin) are used.

Dispensing conditions in pharmacies

Dispensed in a pharmacy without a doctor's prescription. Before taking nitroglycerin, there should be a mandatory consultation with a cardiologist.

Shelf life

The shelf life is 3 years. Use after the expiration date is prohibited.

Nitroglycerin is an antianginal agent, nitrate with vasodilating peripheral action.

Release form and composition

Dosage forms of Nitroglycerin:

  • Sublingual tablets: with a flat surface, white or almost white, with a chamfer and a score (10 or 20 pieces in a blister pack, in a cardboard pack of 1, 2, 3, 4, 5, 6, 8 or 10 packs; 10, 20, 30, 40, 50 or 100 pieces in a polymer container, 1 container in a cardboard pack);
  • Concentrate for preparing a solution for infusion: transparent colorless solution (2, 5 or 10 ml in an ampoule, 5 ampoules in a blister pack, 1, 2 or 10 packs in a cardboard box);
  • Sublingual dosed spray: transparent colorless liquid (10 ml (200 doses) in a bottle with a mechanical dosing pump, 1 bottle in a cardboard box; 10 ml (200 doses) in a bottle with a mechanical dosing pump, 1 bottle in a cardboard box).

The active ingredient is nitroglycerin, the content depends on the form of release:

  • Tablets: 0.5 mg/1 piece;
  • Concentrate for solution: 1 mg/1 ml;
  • Spray: 0.4 mg/1 dose.

Additional components:

  • Tablets: macrogol 6000, povidone 25, lactose, crospovidone CL;
  • Concentrate for solution: potassium dihydrogen phosphate, sodium chloride, dextrose, water for injection;
  • Spray: ethanol 95% (as a 1% solution).

Indications for use

Nitroglycerin taken sublingually (tablets, spray) is recommended for the relief and prevention of angina attacks (including the period before physical activity).

When administered intravenously, the indications for use of the drug are:

  • Unstable angina;
  • Acute myocardial infarction (including complicated by acute left ventricular failure);
  • Pulmonary edema;
  • Angina pectoris (relief of attacks).

Contraindications

  • Cardiac tamponade;
  • Cranial hypertension;
  • Toxic pulmonary edema;
  • Isolated mitral stenosis;
  • Collapse;
  • Constrictive pericarditis;
  • Acute myocardial infarction;
  • Heart failure with normal or low pulmonary artery pressure;
  • Hypotension with low systolic blood pressure;
  • Uncontrolled hypovolemia;
  • Hemorrhagic stroke;
  • Recent head injury;
  • Subarachnoid hemorrhage;
  • Cerebrovascular accident;
  • Angle-closure form of glaucoma;
  • Idiopathic hypertrophic subaortic stenosis;
  • Hyperthyroidism;
  • Severe anemia;
  • Concomitant use of phosphodiesterase inhibitors (including sildenafil, vardenafil, tadalafil, etc.);
  • Age up to 18 years;
  • Hypersensitivity to the components of the drug and other nitrates.

During pregnancy and breastfeeding, use of the product is permissible only for health reasons.

Directions for use and dosage

Sublingual tablets

The tablet should be kept under the tongue until it is completely dissolved, without swallowing.

Immediately after feeling pain, it is recommended to take 0.5-1 mg (1-2 tablets) per dose. In many cases, patients with stable angina note a positive effect even after taking smaller doses (1/2 - 1/3 tablet). If the pain quickly disappears, it is recommended to spit out the rest of the tablet that has not had time to dissolve. As a rule, the antianginal effect is observed after 0.5-2 minutes, and improvement in the majority of patients occurs within the first 3 minutes. If the antianginal effect is not observed within the first 5 minutes, another 0.5 mg of the drug (1 tablet) should be taken. If there is no therapeutic effect when taking 1-1.5 mg (2-3 tablets), you should immediately seek medical help. After using the tablets, the duration of the effect of nitroglycerin is about 45 minutes. Sometimes the development of tolerance to the sublingual form of the drug may occur; when observed, a gradual increase in the dose is required to 2-3 tablets per dose.

Concentrate for the preparation of solution for infusion

Intravenous infusion is carried out with individual selection of the rate of administration of the drug. It is recommended to administer the solution through an infusion pump or automatic dispenser, allowing administration with precise control of its speed and total dose. When using an automatic dispenser, infusions can be carried out even with an undiluted 0.1% solution with precise dosing of the administration rhythm and total dose.

When using a conventional intravenous infusion system, it is recommended to dilute the concentrate with a 5% dextrose (glucose) solution or 0.9% sodium chloride solution (other solvents cannot be used) to obtain a product with a 0.01% concentration of nitroglycerin. The dosage upon administration is selected individually depending on heart rate, blood pressure, electrocardiogram and other indicators.

Drip injections are carried out at an initial rate of 0.5-1 mg/h, with a maximum injection rate of 8-10 mg/h, the duration of therapy varies from 2-3 hours to 2-3 days.

Storage of the solution in an opened ampoule is not permitted. Since the drug is quickly destroyed in light, the transfusion system and bottles must be shielded with light-proof material.

Spray sublingual

Nitroglycerin is administered by pressing the dosing valve (each valve press corresponds to 1 dose) and applying the solution to or under the tongue while holding your breath at intervals of 30 seconds. The packaging must be held vertically, straight in front of you. After taking the spray, your mouth should be closed for 2-3 seconds.

The drug is recommended to be taken at the first sign of an angina attack, at a dose of 0.4-0.8 mg (1-2 doses), while it is advisable for the patient to be in a “sitting” position. If there is no desired effect within 15 minutes, repeated administration is possible at 5-minute intervals, but not more than 1.2 mg (3 doses).

If after using the maximum allowable 3 doses within 15 minutes there is no improvement in the condition, you should consult a doctor.

Do not shake the bottle before taking. The product should not be swallowed immediately.

Side effects

  • Cardiovascular system: fever, skin flushing, dizziness, tachycardia, “nitrate” headache, palpitations, decreased blood pressure; rarely – cyanosis, orthostatic collapse (especially with overdose);
  • Gastrointestinal tract: abdominal pain, nausea, dry mouth, vomiting;
  • Nervous system: rarely (especially in case of overdose) - lethargy, dizziness and feeling of weakness, psychotic reactions, anxiety, disorientation;
  • Allergic reactions: rarely – itching, skin rash;
  • Other: blurred vision, hypothermia, methemoglobinemia (for concentrate).

Symptoms of overdose include: marked decrease in blood pressure with orthostatic dysregulation, headache, reflex tachycardia, vomiting, diarrhea, nausea, dizziness, asthenia, feeling of heat, increased drowsiness; when using high doses (>20 mg/kg) – cyanosis, collapse, dyspnea, methemoglobinemia, tachypnea.

special instructions

Drinking alcohol during therapy is prohibited.

In case of severe blurred vision or dry mouth, you should stop taking nitroglycerin.

When using the drug, a significant decrease in blood pressure and dizziness may be observed in the event of a rapid transition from a “sitting” or “lying” position to an upright position, performing physical exercise, as well as when drinking alcohol.

Reducing the dose of the drug or simultaneous use of validol can help reduce the severity of headaches that occur during treatment.

Patients with diabetes mellitus should remember that the solution for intravenous administration contains dextrose.

It is necessary to avoid abrupt withdrawal of the drug due to the threat of increased frequency of angina attacks.

The spray must not be inhaled!

Drug interactions

It must be taken into account that when combined with nitroglycerin, blockers of “slow” calcium channels, beta-blockers, angiotensin-converting enzyme inhibitors, antihypertensives, vasodilators, procainamide, monoamine oxidase inhibitors, tricyclic antidepressants, phosphodiesterase inhibitors and ethanol aggravate the hypotensive effect.

The drug reduces the effectiveness of heparin and increases the concentration of dihydroergotamine in the blood (increasing its bioavailability), which can lead to increased blood pressure.

Nitroglycerin spray activates the excretion of vanillylmandelic acid and catecholamines in the urine.

Terms and conditions of storage

Store in a place protected from light, out of reach of children; concentrate for the preparation of solution for infusion - at a temperature from 5 ° C to 25 ° C; sublingual tablets – no higher than 25 °C; sublingual spray – no higher than 15 °C.

Best before date:

Concentrate – 3 years;

Tablets – 2.5 years;