Side effect of nitroglycerin is dilation of the coronary arteries. What Nitroglycerin helps with: effect on the heart and blood vessels, indications, contraindications and side effects. Cautions for use

Nitroglycerin is a drug from the group of organic nitrates, primarily a venous dilator. Nitrates are capable of releasing nitric oxide from their molecule, which is a natural endothelial relaxing factor - a mediator of direct activation of guanylate cyclase. An increase in cGMP concentration leads to relaxation of smooth muscle fibers, mainly venules and veins. It has an antianginal and antispasmodic effect, relaxes the smooth muscle cells of the walls of blood vessels, bronchi, digestive tract, biliary tract and ureters. When administered intravenously, it causes a decrease in preload on the heart due to the expansion of peripheral veins. Reduces blood flow to the right atrium, helps reduce pressure in the pulmonary circulation and regression of symptoms in pulmonary edema, reduces afterload, myocardial oxygen demand (by reducing preload, afterload and tension of the ventricular walls due to a decrease in heart volume). Promotes redistribution of coronary blood flow in areas with reduced blood circulation. Has a central inhibitory effect on sympathetic tone vessels, inhibiting the vascular component of formation pain syndrome. Causes dilation of meningeal vessels, which explains the appearance of a specific “nitrate” headache. For prolonged or frequent use long-acting nitrates may develop tolerance. After a break in treatment, sensitivity to nitrates is restored. In order to prevent the development of tolerance, it is recommended to maintain a daily interval in taking nitrates (8-12 hours), preferably at night. For most patients, this therapy is more effective than continuous treatment. When using sublingual forms, an attack of angina is stopped after 1.5 minutes, the hemodynamic and antianginal effect lasts up to 30 minutes. Retard tablets can prevent the development of angina attacks.
Nitroglycerin is quickly and completely absorbed from the surface of the mucous membranes and through the skin. When taken orally, bioavailability is no more than 10% compared to nitroglycerin administered sublingually (first pass effect through the liver). With sublingual, buccal and intravenous administration, first-pass metabolism is excluded, and the active substance enters directly into the systemic circulation. When taken sublingually at a dose of 0.5 mg, the bioavailability is almost 100%, the maximum concentration in the blood plasma is observed after 5 minutes. Up to 60% of nitroglycerin binds to blood plasma proteins. It is quickly metabolized with the participation of nitrate reductase, with the formation of di- and mononitrates (only isosorbide-5-mononitrate is active), the final metabolite is glycerol. Excreted in the urine in the form of metabolites. The total clearance is 25-30 l/min, the half-life is 4-5 minutes. With intravenous administration, the half-life is 1-3 minutes, the total clearance is 30-78 l/min. The active substance is rapidly metabolized in the liver by glutathione reductase, which acts on organic nitrates. In addition, nitroglycerin is metabolized in erythrocytes using enzymatic reactions that occur with the participation of sulfhydryl radicals, as well as through interaction with reduced hemoglobin.

Indications for use of the drug Nitroglycerin

IHD - angina pectoris, including in the post-infarction period; for intravenous administration - acute period myocardial infarction (including complicated by acute left ventricular failure), unstable and post-infarction angina, pulmonary edema, controlled arterial hypotension during surgery to reduce bleeding in the surgical field, occlusion of the central retinal artery.

Use of the drug Nitroglycerin

Inside, sublingually, intravenously. Elimination of angina pectoris. Sublingually (the tablet or capsule with the solution is kept under the tongue until completely absorbed, without swallowing), immediately after the onset of pain - 0.5-1 mg per dose. If necessary, to achieve a faster effect, the capsule should be bitten immediately; the capsule can be repeated after 30-40 minutes. Typically, the antianginal effect appears within 0.5-2 minutes, in some cases within 4-5 minutes. If there is no antianginal effect within the first 5 minutes, another 0.5 mg of nitroglycerin should be prescribed. With absence therapeutic effect after 2-3 doses, the likelihood of developing myocardial infarction should be taken into account.
When using a 1% nitroglycerin solution to relieve an attack, 2-3 drops of the solution are applied to a small piece of sugar and kept in the mouth without swallowing until it is completely absorbed. Duration of action after sublingual administration is about 45 minutes.
At frequent attacks For angina pectoris, it is advisable to prescribe prolonged forms of nitrates. If an attack of angina develops during treatment with prolonged forms of nitrates, for relief acute attack it is necessary to take nitroglycerin sublingually. Tolerance to sublingual forms of nitroglycerin develops infrequently, however, when it develops in some patients, the dose must be gradually increased, bringing it to 2-3 tablets.
Long-acting nitroglycerin, intended for the prevention of angina pectoris, is taken orally with water before meals. In mild cases - 0.0029-0.0058 g 2-3 times a day. In more severe cases- 0.0052-0.01 g 2-3 times a day. Maximum daily dose- 0.0348 g. Due to the fact that the bioavailability of nitroglycerin from retard tablets is low, it is recommended, if well tolerated, to take 1-3 tablets at a time regularly 3-4 times a day or periodically - 30-40 minutes before the expected physical activity . If the therapeutic effect is insufficient, the dose can be gradually increased (but not more than 2 tablets per dose), and after the onset of a therapeutic effect, it can be reduced.
Aerosol for sublingual use: to relieve an attack of angina - 0.4-0.8 mg, pressing the dosing valve, preferably in a sitting position, while holding your breath at intervals of 30 s; After this, you should close your mouth for a few seconds. If necessary, repeat administration, but not more than 1.2 mg over 15 minutes. To prevent an attack - 0.4 mg 5-10 minutes before exercise. In case of acute left ventricular failure, developing pulmonary edema - 1.6 mg or more in a short period of time.
Treatment with nitroglycerin for intravenous administration should be carried out by individually setting the rate of administration of the solution. Enter through automatic dispenser or through a regular IV system. When using a polyvinyl chloride tube system, the active substance is absorbed and losses on the tube walls are up to 60% (it is advisable to use polyethylene and glass tubes). The solution is quickly destroyed in the light, so the bottles and transfusion system must be shielded with light-proof material. Usually used infusion solution with a concentration of 100 µg/ml: concentrated solution diluted with 0.9% sodium chloride solution or 5% dextrose solution and administered intravenously at an initial rate of 5 mcg/min. The rate of administration can be increased every 3-5 minutes by 5 mcg/min (depending on the effect, heart rate, central venous pressure and systolic blood pressure, which can be reduced by 10-25% of the original, but should not be lower than 90 mm Hg. Art.). If the therapeutic effect is not achieved at an injection rate of 20 mcg/min, the injection rate can be increased by 10-20 mcg/min. If a response occurs (in particular, a decrease in blood pressure), a further increase in the infusion rate is not carried out or is carried out at longer intervals. For achievement good effect the rate of administration of 0.01% nitroglycerin solution usually does not exceed 100 mcg/min (1 ml/min). If there is no effect due to the use of nitroglycerin in lower doses and with acceptable level The blood pressure rate of administration of a 0.01% solution can reach 300-400 mcg/min (3-4 ml/min). A further increase in the infusion rate is not advisable. The duration of use is determined clinical indications and can be 2-3 days.

Contraindications to the use of the drug Nitroglycerin

Increased sensitivity to nitroglycerin; for intravenous administration (relative contraindications) - , traumatic brain injury, increased intracranial pressure, cardiac tamponade, constrictive pericarditis, hypovolemia (must be corrected before using nitroglycerin).

Side effects of the drug Nitroglycerin

dizziness, “nitrate” headache, tachycardia, skin flushing, feeling of heat, decreased blood pressure; rarely (mainly in case of overdose) - orthostatic collapse, cyanosis; feeling of dry mouth, nausea, vomiting, abdominal pain; rarely (mainly in case of overdose) - anxiety, psychotic reactions, lethargy, disorientation; rarely - allergic reactions (itchy skin, rash); local reactions during transdermal use: hyperemia and itching of the skin, burning, allergic contact dermatitis; blurred vision, general weakness, hypothermia, methemoglobinemia.

Special instructions for the use of the drug Nitroglycerin

Use with caution, given possible risk, with a recent traumatic brain injury, acute myocardial infarction (risk of decreased blood pressure and tachycardia, which can increase ischemia), glaucoma (risk of increased intraocular pressure), severe anemia, hyperthyroidism, arterial hypotension with low systolic blood pressure (may aggravate the condition, causing paradoxical bradycardia and angina attacks), hypertrophic cardiomyopathy (possible increased frequency of angina attacks), severe renal failure, liver failure(risk of developing methemoglobinemia), during pregnancy and lactation, in children.
In acute myocardial infarction or acute heart failure, it should be used only under the condition of careful clinical observation and monitoring of hemodynamic parameters. To prevent an increase in angina attacks, abrupt withdrawal should be avoided.
During the treatment period, it is necessary to refrain from driving vehicles and engaging in potentially hazardous activities that require increased concentration attention and speed of psychomotor reactions.
While taking nitroglycerin, there may be a significant decrease in blood pressure and the appearance of dizziness when suddenly moving to a vertical position from a lying or sitting position; when drinking ethanol, performing physical exercise and in hot weather. It is also possible that angina may worsen with sharp decline Blood pressure, ischemia up to myocardial infarction and sudden death. With frequent use without intervals, tolerance to nitrates may develop, requiring an increase in dose. The severity of headaches while taking nitroglycerin can be reduced by reducing the dose of nitroglycerin and/or simultaneously taking validol.

Drug interactions Nitroglycerin

Simultaneous use with vasodilators, antihypertensive drugs, ACE inhibitors, β-adrenergic receptor blockers, calcium antagonists, procainamide, tricyclic antidepressants, MAO inhibitors, phosphodiesterase inhibitors, and ethanol enhance the hypotensive effect of nitroglycerin. Prescription with dihydroergotamine can lead to an increase in its content in the blood and an increase in blood pressure (increased bioavailability of dihydroergotamine). Nitroglycerin should be combined with heparin with caution.

Nitroglycerin drug overdose, symptoms and treatment

Manifested by a decrease in blood pressure (below 90 mm Hg), orthostatic reactions, reflex tachycardia, headache, dizziness, drowsiness, feeling of heat, nausea, vomiting, with a significant overdose (more than 20 mg/kg) - collapse, cyanosis, methemoglobinemia, dyspnea and tachypnea. If symptoms of overdose develop, stop further administration and remove the patch. The head end of the bed should be lowered and the patient's legs should be raised. As a rule, blood pressure normalizes within 15-20 minutes after stopping the administration of nitroglycerin, then administration can be continued after re-establishing the infusion rate. To correct blood pressure, it is possible to use phenylephrine, epinephrine and other vasoconstrictors. For methemoglobinemia, depending on the severity, it is prescribed ascorbic acid 1 g orally or in form sodium salt i.v.; IV methylene blue 0.1-0.15 ml/kg 1% solution (up to 50 ml), oxygen therapy, hemodialysis, exchange blood transfusion.

List of pharmacies where you can buy Nitroglycerin:

  • Saint Petersburg

Nitroglycerin: instructions for use and reviews

Latin name: Nitroglycerin

ATX code: C01DA02

Active substance: nitroglycerin

Manufacturer: NPF "Microkhim", LLC "Experimental plant GNTsLS" (Ukraine), LLC "Ozon", LLC "Lumi", LLC "Pharmamed", Medical-technological holding "MTX", "Samaramedprom", CJSC "Binnopharm", JSC "Biomed" named after. I. I. Mechnikova”, “Medisorb” (Russia)

Updating the description and photo: 16.08.2019

Nitroglycerin – vasodilator, used to relieve attacks of angina pectoris.

Release form and composition

Nitroglycerin is available in the following dosage forms:

  • Sublingual tablets: almost white or white, flat-cylindrical, with a rough surface (40 tablets in a polymer tube tightly sealed with a polymer stopper, 1 tube in a cardboard box);
  • Sublingual dosed spray: colorless, transparent (in bottles or cylinders of 200 doses (10 ml), 1 bottle or cylinder in a cardboard box complete with a mechanical dosing pump);
  • Concentrate for the preparation of solution for infusion: colorless, transparent (in ampoules of 2, 5 or 10 ml, 5 ampoules in blister packs, 1, 2 or 10 packs in a cardboard box).

The composition of 1 sublingual tablet includes:

  • Active substance: nitroglycerin – 0.5 mg (based on 100% substance);
  • Auxiliary components: sugar (sucrose) - 7.9 mg, glucose (dextrose) - 9.3 mg, potato starch - 9.3 mg.

The composition of 1 dose of sublingual spray includes:

  • Active substance: nitroglycerin – 0.4 mg;
  • Auxiliary components: 95% ethanol (in the form of a 1% solution).

Contains 1 ml of concentrate for preparation infusion solution includes:

  • Active substance: nitroglycerin – 1 mg;
  • Auxiliary components: dextrose, sodium chloride, potassium dihydrogen phosphate, water for injection.

Pharmacological properties

Pharmacodynamics

Nitroglycerin is a peripheral vasodilator, preferentially affecting the venous vessels. Its effect is mainly due to a decrease in myocardial oxygen demand due to a decrease in preload (decreased blood flow to the right atrium and dilation of peripheral venous vessels) and afterload (decreased total peripheral vascular resistance).

Nitroglycerin is capable of releasing nitric oxide from its molecule, which is a natural endothelial relaxing factor. The compound increases the concentration of cyclic guanosine monophosphatase inside the cell, which prevents the penetration of calcium ions into smooth muscle cells and provokes their relaxation. Relaxation of the smooth muscles of the vascular wall leads to vasodilation, which reduces the load on the heart and the myocardium’s need for oxygen. Extension coronary vessels helps improve coronary blood flow and its redistribution to areas characterized by reduced blood circulation, which stimulates the transport of oxygen to the myocardium.

A decrease in venous return causes a decrease in pressure in the pulmonary circulation and filling pressure, improvement in blood supply to the subendocardial layers and regression of symptoms characteristic of pulmonary edema. Nitroglycerin is characterized by a central inhibitory effect on the sympathetic tone of blood vessels and suppression of the vascular component responsible for the formation of pain. It also provokes dilation of the meningeal vessels, which causes headaches after taking it, and relaxes the smooth muscle cells of the bronchi, small and large intestines, esophagus, and their sphincters, bile ducts, gallbladder, urinary tract.

The use of sublingual forms usually allows you to stop an attack of angina within 1.5 minutes after oral administration, and the antianginal effect lasts for 30–60 minutes.

Pharmacokinetics

Nitroglycerin is quickly and almost completely absorbed from the surface of the mucous membranes oral cavity. When taken sublingually, it immediately penetrates the systemic bloodstream. The bioavailability of the drug is 100%, since primary hepatic degradation of the substance is excluded. Maximum concentration nitroglycerin in blood plasma is determined after 4-5 minutes. The substance is metabolized quite quickly with the participation of nitrate reductase. In this case, mono- and dinitrates are formed. Only isosorbide-5-mononitrate demonstrates pharmacological activity. The final metabolite is glycerol.

The drug has a very large volume of distribution (1.2‒3.3 l/kg). The degree of binding to plasma proteins is 60%. Nitroglycerin is excreted in the urine in the form of metabolites (less than 1% of the dose taken is excreted unchanged), the total clearance is 25–30 l/min (with infusion administration - up to 78 l/min). After oral sublingual administration of the drug, the half-life from blood plasma varies from 2.5 to 4.4 minutes (with infusion administration - from 1 to 3 minutes). Circulating nitroglycerin binds tightly to red blood cells and accumulates in the walls of blood vessels.

Indications for use

Indications for the use of Nitroglycerin are:

  • Angina pectoris (relief and short-term prevention of angina attacks before emotional stress or physical activity);
  • Acute myocardial infarction, including complicated by acute left ventricular failure (infusion solution);
  • Pulmonary edema (infusion solution);
  • Unstable angina (infusion solution).

Contraindications

Absolute:

  • Collapse;
  • Age up to 18 years (efficacy and safety of using Nitroglycerin for this age group patients not identified);
  • Hypersensitivity to the components of the drug.

Depending on the dosage form, additional absolute contraindications The following diseases/conditions are suitable for the use of Nitroglycerin:

  • Glucose-galactose malabsorption (sublingual tablets);
  • Shock (sublingual spray and tablets);
  • Cardiogenic shock, except in cases of measures to maintain end-diastolic pressure (sublingual spray);
  • Severe hypotension with systolic blood pressure below 90 mm Hg. Art. (spray sublingual);
  • Constrictive pericarditis (sublingual spray);
  • Angina associated with hypertrophic obstructive cardiomyopathy (sublingual spray);
  • Acute myocardial infarction and chronic heart failure with low left ventricular filling pressure (sublingual spray);
  • Pericardial tamponade (sublingual spray);
  • Any conditions associated with increased intracranial pressure (sublingual spray);
  • Severe mitral stenosis and/or aortic valve, primary pulmonary hypertension (sublingual spray);
  • Concomitant use with phosphodiesterase-5 inhibitors, including vardenafil, sildenafil, tadalafil (sublingual tablets and spray).

According to the instructions, Nitroglycerin should be used with caution after assessing the benefit/risk ratio:

  • Hemorrhagic stroke;
  • Severe anemia;
  • Thyrotoxicosis;
  • Severe renal failure;
  • Angle-closure glaucoma;
  • Recent head injuries;
  • Intracranial hypertension;
  • Cardiac tamponade (sublingual tablets and infusion solution);
  • Liver failure (sublingual tablets and infusion solution), severe liver failure (sublingual spray);
  • Arterial hypotension with low systolic pressure - less than 90 mm Hg. Art. (sublingual tablets and infusion solution);
  • Orthostatic hypotension and tendency to develop orthostatic hypotension(spray sublingual);
  • Alcohol abuse (sublingual spray);
  • Epilepsy (sublingual spray);
  • Migraine (sublingual spray);
  • Constrictive pericarditis (sublingual tablets and infusion solution);
  • Isolated mitral stenosis (sublingual tablets and infusion solution);
  • Hypertrophic cardiomyopathy (sublingual tablets and infusion solution);
  • Toxic pulmonary edema (infusion solution);
  • Idiopathic hypertrophic sub aortic stenosis(sublingual tablets), aortic stenosis (infusion solution);
  • Acute myocardial infarction, chronic heart failure with low left ventricular filling pressure (sublingual tablets and infusion solution);
  • Uncontrolled hypovolemia with normal or low blood pressure pulmonary artery in patients with heart failure (infusion solution);
  • Shock, including cardiogenic, except in cases of sufficient high pressure filling the left ventricle, incl. provided with drugs with a positive inotropic effect or intra-aortic counterpulsation (infusion solution);
  • Cerebral hemorrhage (infusion solution);
  • Expressed cerebral atherosclerosis(infusion solution);
  • Pregnancy and lactation (for all forms of the drug);
  • Old age (infusion solution).

Instructions for use of Nitroglycerin: method and dosage

Sublingual tablets

To prevent complications, Nitroglycerin is recommended to be taken as prescribed by a doctor.

Nitroglycerin tablets are taken (sublingually) under the tongue, held in the mouth until completely dissolved, without swallowing.

Nitroglycerin should be taken immediately when the first signs of an angina attack appear or before expected physical activity or emotional stress. Single dose– 1 tablet. In case of stable angina pectoris, the effect may occur with a smaller dose; in this case, it is recommended to spit out the remaining tablet that has not had time to dissolve. In most cases (75% of patients), improvement is noted within the first 3 minutes of using Nitroglycerin.

If the angina attack is not stopped within 5 minutes, you should take 1 more tablet.

If there is no therapeutic effect after taking 2 Nitroglycerin tablets, you should immediately consult a doctor.

Spray sublingual

Injected on or under the tongue, preferably in a sitting position, while holding your breath. After spraying, the spray is not swallowed immediately, but is held by closing the mouth for a few seconds.

To avoid complications, Nitroglycerin should be used as prescribed by a doctor.

When the first signs of an angina attack appear, 1-2 doses of the spray are administered (depending on the severity). If necessary, it is possible to administer 1 more dose, but not more than 3 doses (1.2 mg) within 15 minutes.

If after using 3 doses over 15 minutes the condition does not improve, you should consult your doctor.

The maximum single dose is 3 doses of spray.

If the indication for the use of Nitroglycerin is the prevention of angina attacks, the drug is used 1 dose 5-10 minutes before the expected load or stress.

The spray package should not be shaken before use. When spraying, the bottle must be held vertically.

Infusion solution

The rate of intravenous administration of Nitroglycerin is selected individually, taking into account blood pressure, heart rate, central venous pressure, ECG and other indicators. The solution should be administered through an infusion pump or automatic dispenser, allowing for precise dosing and control of the rhythm of administration.

Administration of Nitroglycerin using a conventional fluid transfusion system ensures dosage accuracy by counting the number of drops of fluid being transfused. Before administration, the Nitroglycerin solution is first diluted in a 0.9% sodium chloride solution or a 5% glucose (dextrose) solution to a concentration of 0.01%. No other solvents should be used.

It is advisable to use glass and polyethylene tubes, since the active substance is absorbed on the walls of polyvinyl chloride tubes (losses can be 40-80%). Nitroglycerin solution is quickly destroyed in light, so the transfusion system and bottles must be shielded with light-proof material. Storing the solution in an opened ampoule is not allowed.

The initial rate of administration of the solution is 0.5-1 mg per hour, maximum speed– 8-10 mg per hour.

Recommended concentrations and rates of administration of Nitroglycerin are: 1 mg/h (0.0166 mg/min) - 24 mg per day via an automatic dispenser (solution volume 1 mg/ml) or 240 mg per day via an intravenous system (solution volume 0 .1 mg/ml); injection rate – 3-4 drops per minute (1 ml corresponds to 20 drops).

The duration of therapy is determined by clinical indications and can vary from several hours to 2-3 days.

Side effects

  • Central nervous system: weakness; rarely – psychotic reactions, anxiety, disorientation, lethargy;
  • Digestive system: dryness of the oral mucosa; rarely – vomiting, nausea, abdominal pain;
  • The cardiovascular system: headache, dizziness, fever, tachycardia, decrease blood pressure; rarely (especially in case of overdose) - cyanosis, orthostatic collapse, increased symptoms of angina pectoris (paradoxical reaction to nitrates); sometimes - collapse with loss of consciousness and bradyarrhythmia;
  • Local reactions: burning sensation under the tongue, skin hyperemia;
  • Allergic reactions: rarely – itching, skin rash, exfoliative dermatitis;
  • Other: rarely - hypothermia, blurred vision, methemoglobinemia.

Overdose

Symptoms of an overdose of Nitroglycerin are: nausea, vomiting, increased drowsiness, severe weakness, asthenia, severe dizziness, headache, seizures, feeling of heat, shortness of breath, reflex tachycardia, decreased blood pressure (below 90 mm Hg), accompanied by orthostatic dysregulation. Taking the drug in high doses (more than 20 mg/kg) can lead to the development of tachypnea, dyspnea, cyanosis, collapse, and methemoglobinemia.

If signs of overdose occur, you should immediately put the patient in a horizontal position, raising his legs, and also seek medical help.

special instructions

The therapeutic doses indicated in the instructions should not be exceeded.

1 tablet of sublingual Nitroglycerin contains 2.65×10 -3 XE (bread units).

During therapy, a significant decrease in blood pressure and the development of dizziness are possible with a sudden transition to a vertical position from a lying or sitting position, as well as in hot weather, when doing physical exercise or drinking alcohol.

If blurred vision or dryness of the oral mucosa persists or becomes significant, treatment should be interrupted.

According to the instructions, Nitroglycerin, like other organic nitrates, can be addictive (in this case, an increase in dosage will be required).

The severity of headache during therapy can be reduced by reducing the dose of the drug and/or simultaneous administration of validol.

While using Nitroglycerin, use alcoholic drinks strictly prohibited.

The sublingual spray contains alcohol, which is important for nursing and pregnant women, patients with functional disorders liver, epilepsy, traumatic brain injury and other diseases of the central nervous system, as well as alcohol abuse.

The infusion solution contains glucose (dextrose), which should be taken into account in patients with diabetes.

In acute heart failure or acute myocardial infarction, Nitroglycerin should be used only under the condition of careful clinical monitoring of the patient's condition.

To prevent an increase in angina attacks, it is recommended to avoid abrupt withdrawal of the drug.

To prevent an unwanted decrease in blood pressure, the rate of administration of the Nitroglycerin infusion solution must be selected individually. A decrease in blood pressure can be observed not only when selecting the rate of solution administration, but also later, against the background of initially stabilized blood pressure (monitoring should be carried out at least 3-4 times per hour throughout the entire infusion time).

Patients previously treated with organic nitrates (isosorbide-5-mononitrate, isosorbide dinitrate) may require a higher dose to obtain the desired hemodynamic effect.

When using Nitroglycerin, care must be taken when driving vehicles and performing potentially dangerous species work that requires increased concentration and quick psychomotor reactions.

Drug interactions

When nitroglycerin is used simultaneously with certain medications, the following effects may occur:

  • Vasodilators, antihypertensives, angiotensin-converting enzyme inhibitors, phosphodiesterase-5 inhibitors, slow blockers calcium channels, tricyclic antidepressants, ethanol, diuretics, beta-blockers, monoamine oxidase inhibitors, procainamide: increased hypotensive effect of nitroglycerin;
    • Sublingual tablets: 2 years at temperatures up to 25 °C;
    • Sublingual spray: 2 years at temperatures up to 15 °C;
    • Concentrate for the preparation of solution for infusion: 3 years at a temperature of 5-25 °C.

Nitroglycerin is medicinal product synthetic origin, which is used in cardiology. Available in the form of an alcohol solution, sublingual tablets and capsules.

Pharmacological action of Nitroglycerin

According to the instructions, the active ingredient of the drug is nitroglycerin.

The drug is a peripheral vasodilator that affects the venous vessels. Nitroglycerin produces nitric oxide, which leads to activation of guanylate cyclase and an increase in the content of cyclic guanosine monophosphate (cGMP) in smooth muscle cells. In accordance with the instructions, Nitroglycerin promotes nonspecific relaxation of vascular smooth muscles, mostly venous, which is accompanied by the deposition of blood in the venous system.

When using Nitroglycerin, there is a decrease in cardiac preload and end-diastolic filling of the left ventricle. General systemic arterial dilatation, mainly of large vessels, reduces afterload.

This medication reduces the myocardium's need for oxygen and normalizes the functioning of systemic blood flow.

When using Nitroglycerin, relaxation of the smooth muscles of the bile ducts, bronchi, intestines, stomach, esophagus, and genitourinary system is observed.

Nitroglycerin is quickly and completely absorbed into the systemic circulation. The period of complete elimination of the drug is 8 hours. It is excreted from the body in the form of metabolites through the kidneys.

Indications for use of Nitroglycerin

Indications for Nitroglycerin are angina attacks, left ventricular failure, myocardial infarction.

IN individual cases the medicine is used to treat biliary dyskinesia. In some cases, it is prescribed for therapy of the central retinal artery.

Directions for use and dosage

Nitroglycerin in the form of an alcohol solution is applied directly to the tongue, 1-2 drops, or moistened with a small piece of sugar and kept under the tongue until it is completely absorbed. The maximum single dose of Nitroglycerin under the tongue is 4 drops, the daily dose is 16 drops.

According to indications, Nitroglycerin tablets are taken sublingually, immediately after pain occurs, without swallowing. A single dose of Nitroglycerin tablets for adults is 1-2 pcs. The maximum daily dose is 6 tablets.

The rules for taking capsules correspond to the rules for taking tablets. To speed up the therapeutic effect, the capsule can be crushed with your teeth.

The duration and frequency of use of Nitroglycerin depend on the intensity and frequency of angina attacks.

If there is no effect within 5 minutes after taking the medicine, you need to take 1 more tablet. If there is no effect after taking 2-3 tablets, you should immediately call an ambulance.

Side effects

When using Nitroglycerin, headaches, tachycardia, tinnitus, fever, decreased blood pressure, dry mouth, abdominal pain, nausea, and vomiting may occur.

Contraindications

According to the instructions, Nitroglycerin is not prescribed to people who have:

  • Arterial hypotension;
  • Circulatory disorders of the brain;
  • Hyperthyroidism;
  • Angle-closure form of glaucoma, accompanied by increased intraocular pressure;
  • Idiopathic hypertrophic subaortic stenosis;
  • Head injuries;
  • Hemorrhagic stroke;
  • Severe anemia;
  • Subarachnoid hemorrhage;
  • Collapse;
  • Heart failure;
  • Uncontrolled hypovolemia;
  • Constrictive pericarditis;
  • Isolated mitral stenosis;
  • Cardiac tamponade;
  • Cranial hypertension.

Contraindications to Nitroglycerin also include age under 18 years, pregnancy, and lactation.

Take the medicine with caution in case of liver failure and severe renal failure.

Overdose

An overdose of Nitroglycerin may result in a decrease in blood pressure, reflex tachycardia, and asthenia.

Symptoms of an overdose of Nitroglycerin also include dizziness, cyanosis, dyspnea, methemoglobinemia, tachypnea.

Additional Information

Uncontrolled use of Nitroglycerin can cause the development of tolerance to the drug.

The medicine affects the speed of psychomotor reactions, so during therapy it is recommended to refrain from driving heavy machinery and vehicles.

According to the instructions, Nitroglycerin must be stored in a cool place out of reach of children.

Shelf life – 2 years.

Nitroglycerin is available from pharmacies over the counter.

Each tablet contains: nitroglycerin (in the form of nitroglycerin with glucose) - 0.5 mg;

Excipients: potato starch, microcrystalline cellulose, colloidal anhydrous silicon dioxide, calcium stearate, lactose monohydrate.

Pharmacotherapeutic group

Peripheral vasodilators used in the treatment of heart disease. Organic nitrates.

Indications for use

Relief and short-term prevention of angina attacks.

Directions for use and doses

The dose and treatment regimen are determined by the attending physician individually, depending on the patient’s sensitivity to nitroglycerin preparations, indications, and the specific clinical situation. The drug should be used with caution when pronounced violations liver and/or kidney functions.

The usual dose of the drug for angina pectoris is 1 tablet under the tongue, in many patients with stable angina the effect occurs with a smaller dose (1/2-1/3 tablets), therefore, if the pain goes away quickly, it is recommended to spit out the remainder of the tablet that has not had time to dissolve. Typically, the antianginal effect appears within 0.5-2 minutes; 75% of patients note improvement within the first 3 minutes; and another 15% - within 4-5 minutes. If there is no therapeutic effect within the first 5 minutes, you must take another tablet of the drug. If there is no therapeutic effect after 2-3 doses, you must call a doctor (the likelihood of developing a myocardial infarction). The duration of action of nitroglycerin is about 45 minutes.

Tolerance to sublingual forms of nitroglycerin rarely develops; however, if it occurs in some patients, the dose of the drug must be gradually increased, bringing it to 2-3 tablets.

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Side effect

From the side of the central nervous system: blurred vision, headache (especially at the beginning of treatment, with long-term therapy decreases), dizziness and feeling of weakness, restlessness, fainting, drowsiness, cerebral ischemia.

From the outsidecardiovascularsystems: arterial hypotension, facial flushing, tachycardia, bradycardia, vascular collapse. Sometimes, with a sudden decrease in blood pressure, an increase in the symptoms of angina pectoris may be observed (paradoxical “nitrate reactions”).

From the digestive tract: a slight burning sensation in the mouth, rarely - nausea, vomiting, heartburn.

WITHon the side of the hematopoietic system: rarely - methemoglobinemia, cyanosis.

Others: allergic reactions are possible; rarely - exfoliative dermatitis, increased intraocular pressure; with long-term use of the drug in high doses - drug withdrawal syndrome; development of tolerance.

Contraindications

Increased sensitivity to active substance, other nitrates, or any of excipients; arterial hypotension (systolic pressure less than 90 mm Hg); vascular collapse; closed-angle form of glaucoma; shock; acute heart attack myocardium with low filling pressure of the left ventricle; toxic edema lungs; hemorrhagic stroke; conditions accompanied by a decrease in left ventricular filling pressure (isolated mitral stenosis, constrictive pericarditis); hypertrophic cardiomyopathy; simultaneous use with phosphodiesterase inhibitors (for example, sildenafil, vardenafil, tadalafil); anemia, increased intracranial pressure (including after a traumatic brain injury), bradycardia, cardiac tamponade, aortic stenosis.”

Pregnancy, breastfeeding, childhood.

Overdose

Symptoms: severe arterial hypotension, tachycardia, collapse, cyanosis, methemoglobinemia.

Treatment: in case of collapse, the patient should take a horizontal position with his legs raised up. For methemoglobinemia, intravenous administration of methylene blue is indicated (on average 0.1-0.15 ml of 1% solution per 1 kg of body weight). In severe cases, plasma substitutes, sympathomimetics, and oxygen are prescribed.

Precautions and application features

Before using the drug for the first time, you should consult your doctor!

While taking the drug, there may be a significant decrease in blood pressure, dizziness may occur during a sudden transition to a vertical position from a “lying” or “sitting” position, when drinking alcohol, doing physical exercise and in hot weather.

With frequent use, nitroglycerin may become addictive, requiring increased dosage.

The severity of headache while taking the drug can be reduced by reducing its dose and/or simultaneous administration of validol.

During the treatment period, alcohol consumption is not allowed.

Use with caution in case of cerebrovascular pathology, serious illnesses liver or kidneys, hypothyroidism, hypoxemia, recent myocardial infarction, primary pulmonary hypertension, migraine, tendency to develop orthostatic hypotension, malnutrition, deficiency of methemoglobin reductase, glucose-6-phosphate dehydrogenase.

To prevent hypotension, it is recommended to take nitroglycerin while lying down or sitting. Taking nitroglycerin in a standing position can not only contribute to fainting, but also weaken the antianginal effect and develop the “steal” syndrome (increased myocardial ischemia), especially in patients with widespread atherosclerosis of the coronary vessels.

If the symptoms of angina pectoris do not go away after taking three doses of the drug, the patient should immediately consult a doctor.

In order to prevent the development of tolerance, it is recommended to maintain a daily interval between taking nitrates (8-12 hours). If tolerance develops, you should temporarily stop taking the drug (for several days) and replace it with antianginal drugs of other pharmacotherapeutic groups.

The storage conditions of the drug should be strictly observed. If the integrity of the packaging or storage conditions is violated, the effectiveness of the drug may decrease.

Features of use in elderly patients

When nitrates are used in older people, the risk of developing such adverse reactions such as hypotension and syncope. This category of patients is recommended to take the drug with caution, if possible, in a sitting or lying position.”

Use in children

The drug is contraindicated in children due to the lack of data on effectiveness and safety.

Use during pregnancy and breastfeeding

Safety of use during pregnancy and lactation has not been proven. During pregnancy and breastfeeding, taking the drug is possible only if the expected benefit to the mother outweighs the possible risk to the fetus or child.

Effect of the drug on the abilitydrive a car and operate machinerymami

When driving a vehicle or operating machinery that requires increased attention, it should be remembered that taking the drug may lead to a decrease in the reaction rate.

Interaction with other drugs

The hypotensive effect of the drug may be excessive in case of uncontrolled simultaneous administration antihypertensive drugs, tricyclic antidepressants, alcohol, diuretics, beta-blockers, monoamine oxidase inhibitors (MAO). Nitroglycerin should be taken with procainamide with caution, as the hypotensive effect may be enhanced and collapse may develop.

Concomitant use of nitroglycerin with phosphodiesterase type 5 inhibitors, which are used to treat erectile dysfunction or pulmonary hypertension, is strictly contraindicated due to the risk of severe hypotension. The use of nitroglycerin is possible no earlier than 24 hours after taking drugs containing sildenafil and vardenafil, no earlier than 48 hours after taking drugs containing tadalafil.

The drug has been quickly and effectively making life easier for patients with heart disease for the second century. But the study and creation of all kinds pharmacological forms continues. Behind for a long time scientists and doctors have discovered many beneficial properties and found out what nitroglycerin helps with by affecting the vascular system.

How does nitroglycerin work?

The mechanism of action of nitroglycerin has been no longer a mystery since the end of the twentieth century. The scientists who discovered it were awarded Nobel Prize. The medicine has a relaxing effect on the smooth muscle layer of the vascular wall, due to which the lumen of the vessel becomes wider.

The reason for this is nitrogen released from nitroglycerin. It reacts with free oxygen and forms nitric oxide, which activates a special substance - guanylate cyclase, which is responsible in the body for relaxing smooth muscles.

Nitroglycerin - what does the drug help with?

Smooth muscle fibers are located not only in blood vessels. They also contain the walls of the intestines, bronchi, ureters, bile and pancreatic ducts. Using nitroglycerin, you can relieve spasm of these anatomical formations.

  • The cardiovascular system. The main and most commonly used “target” of nitroglycerin.
    • By dilating the coronary arteries, the drug increases the flow of oxygen-rich blood to the heart muscle. As a result, angina pain is relieved.
    • Dilatation of venous vessels, especially with intravenous administration medications, reduces venous return to the heart, “unloading” its right sections. The result is a reduction in congestion and prevention of pulmonary edema. In addition, with a decrease in the volume of blood load on the heart, its need for oxygen is correspondingly reduced, which also has an analgesic effect in angina pectoris.
    • The drug is used for surgical interventions for controlled hypotension.
    • The rehabilitation period after a heart attack is also not complete without this drug.
    • Hypertension, accompanied by crises with heart pain and shortness of breath, is also an indication for the use of nitroglycerin.
  • Bile and pancreatic ducts. Nitroglycerin relieves spasm of the duct walls in biliary colic, gallbladder dyskinesia or acute pancreatitis.
  • Gastrointestinal tract. The drug relieves pain due to colic and dyskinesia.
  • Urinary ducts. By relaxing the walls of the ureter, nitroglycerin relieves pain in renal colic.

Side effect

The wonderful property of the drug to relax smooth muscles can cause and unpleasant consequences. The reason is rapid dilation of blood vessels, a drop in blood pressure

  • Headache, possible fainting.
  • Cardiopalmus.
  • Nausea, dyspepsia, feeling of dry mouth.

An overdose may cause nervousness, disorientation, or lethargy. In case of severe intoxication, collapse and breathing problems occur, which requires immediate medical attention.

At fainting caused by taking nitroglycerin, the drug should be stopped entering the body, the patient should be placed with his legs elevated and his head slightly lowered. Normalization of blood pressure usually occurs within 20 minutes.

Admission rules

For more than a hundred years, the pharmaceutical industry has produced a wide variety of forms of the drug. The most popular and effective are sublingual and buccal. Intravenous and cutaneous, as well as prolonged forms are also produced.

How to take nitroglycerin tablets under the tongue

Sublingual tablets 0.5 mg. They should be taken to relieve angina pain. Fast acting drug.

Admission rules. If you experience an attack of angina-type pain, you should stop the exercise during which it occurred, sit down and put 1 tablet of nitroglycerin under your tongue. The patient will feel the effect within 1-3 minutes. Duration – up to 10 minutes. If it doesn’t help, you can take a second tablet 5 minutes after the first, and a third after another 5 minutes. Lack of pain relief within 15 minutes when taking 3 tablets is a reason to seek treatment medical care, since myocardial infarction may develop.

The storage conditions for tablets should be observed:

  • in an open package (glass tube), nitroglycerin remains active for no more than two months;
  • plastic packaging for nitroglycerin is not suitable; after three days of storage it loses 80% of its effectiveness;
  • the glass tube must be closed with a rubber stopper, without cotton wool, which absorbs nitroglycerin;
  • Unopened packaging loses 32% of activity within a week.

Side effects most often include headaches, a feeling of fullness, tinnitus, and facial flushing. Possible dizziness and hypotension. This is due to the expansion of venous vessels in the head and difficulty in venous outflow.

To reduce side effects, you can take half a nitroglycerin tablet, adding validol or menthol, which helps improve venous outflow from the cranial cavity.

Other forms of nitroglycerin that have a quick effect

Not only tablets can be taken under the tongue. They also release alcohol solution nitroglycerin, oil solution in gelatin capsules, spray and aerosol, plates glued to the gums

  • Alcohol solution. Drop 4 drops of solution onto a piece of sugar (2-3 is enough for some patients) and place it under the tongue. Just as with sublingual tablets, three doses within 15 minutes are allowed if there is no desired effect.
  • Gelatin capsules with oil solution. Application involves placing a capsule previously crushed by the teeth under the tongue.
  • Inhalation forms. Spray and aerosol release 0.4 and 0.2 mg of nitroglycerin with 1 spray. One sublingual tablet corresponds to 2-4 valve presses. The spray effect occurs faster and lasts up to 20 minutes. The drug has proven itself well in pulmonary edema and cardiac asthma. The drug is sprayed into the mouth while holding your breath. When inhaling the aerosol, bronchospasm may develop.

  • Plates on the gums. Contains 4, 2 or 1 mg of nitroglycerin. Polymer plates are glued to the gums upper jaw in the area of ​​canines and small molars. The effect occurs within 1 or 2 minutes, and lasts the entire period of resorption of the plate. It is individual and depending on this the dose of the drug is selected. If resorption occurs within an hour and a half, a plate containing 1 mg of the drug is prescribed, 2-3 hours - twice as much, 4-6 hours - 4 mg. If the load painful, stopped earlier, it makes sense to remove the record. If you need to increase the supply of nitroglycerin, you need to lick the plate two or three times.

Contraindications to taking nitroglycerin

Taking nitroglycerin may worsen the condition of patients with

  • increased intracranial pressure;
  • cerebral hemorrhage;
  • allergies to nitrates;
  • hypotension below 100/60 mmHg. Art.;
  • hypovolemia CVP less than 4-5 mm Hg. Art.;
  • angle-closure glaucoma with high intraocular pressure;
  • pregnancy, lactation;
  • hypertrophic cardiomyopathy;
  • severe renal and liver failure;
  • thyrotoxicosis.

The use of nitroglycerin, as well as others medicines, must be agreed with the attending physician after thorough examination and establishing an accurate diagnosis.

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