Nitroglycerin: properties, indications and contraindications, how to use in various forms and cases.

active substance: nitroglycerin with glucose - 10.0 mg, in terms of nitroglycerin - 1.0 mg;

Excipients: sodium chloride - 6.5 mg, potassium dihydrogen phosphate - 0.5 mg, water for injection - up to 1.0 ml.

Once in the systemic circulation, 60% binds to blood plasma proteins. It is highly lipophilic and has a large volume of distribution (3.3-1.2 l/kg). It is quickly metabolized in the liver by glutathione reductase, which acts on organic nitrates, with the formation of di- and mononitrates (only isosorbide-5-mononitrate is active), the final metabolite is glycerol. Excreted by the kidneys in the form of metabolites. The total clearance is 30-78 l/min, the half-life is 1-3 minutes.

Acute myocardial infarction, incl. complicated by acute left ventricular failure;

Severe forms angina pectoris, incl. unstable and post-infarction angina;

Pulmonary edema, acute heart failure, incl. against the background of a hypertensive crisis;

Controlled arterial hypotension during surgical interventions in order to reduce bleeding in the surgical field.

Increased sensitivity to active substance, other organic nitrates or excipients;

Acute disorder blood circulation (shock, vascular collapse);

Cardiogenic shock(if measures are not taken to maintain end-diastolic pressure);

Severe hypotension (systolic blood pressure (BP) below 90 mmHg);

Severe hypovolemia;

Severe anemia;

Hypertrophic obstructive cardiomyopathy;

Constrictive pericarditis;

Cardiac tamponade;

Simultaneous use phosphodiesterase-5 inhibitors (including sildenafil, vardenafil, tadalafil);

Age up to 18 years (efficacy and safety have not been established);

Traumatic brain injury;

Isolated mitral stenosis, aortic stenosis, subaortic stenosis;

Toxic pulmonary edema;

Intracranial hypertension;

Brain hemorrhage.

The drug should be used with extreme caution and under close medical supervision. following cases:

Low filling pressure of the left ventricle, incl. at acute heart attack myocardium (lowering systolic blood pressure below 90 mm Hg should be avoided);

Impaired left ventricular function (for example, with left ventricular failure);

Tendency to orthostatic disorders of vascular regulation;

Increased intraocular pressure, incl. angle-closure glaucoma;

Severe renal and/or liver failure(risk of developing methemoglobinemia);

Thyrotoxicosis;

Diabetes;

Atherosclerosis.

The use of the drug during pregnancy is possible only if the expected benefit to the mother exceeds possible risk for the fetus and/or child, as prescribed by a doctor and careful monitoring of the condition of the pregnant woman and the development of the fetus.

There is information about the penetration of nitrates into breast milk, but the exact content of nitroglycerin in breast milk not determined. A possible risk of developing methemoglobinemia in infants has also been reported. Termination decision breastfeeding or discontinuation/refusal of treatment with the drug should be taken after assessing the benefits of breastfeeding and therapy for the mother.

Treatment should be carried out in a hospital setting with individual selection of the drug infusion rate. The solution is administered through an automatic dispenser or through conventional system for intravenous infusions.

The automatic dispenser allows you to administer even an undiluted 0.1% solution with precise dosing of the injection rate and total dose. Administration through a conventional infusion system ensures that the exact dose is selected by counting the number of drops of fluid being infused.

The following materials are used for intravenous administration of the drug: polyethylene, polypropylene or polytetrafluoroethylene. Infusion materials made from polyvinyl chloride or polyurethane reduce the effectiveness of the drug due to absorption (up to 60%), which must be compensated for by increasing the dose.

The solution quickly degrades in light, so the vials and transfusion system must be shielded with light-proof material. Typically, an infusion solution with a concentration of 100 or 200 mcg/ml is used: the concentrated solution is diluted with 0.9% sodium chloride solution, 5% or 10% dextrose (glucose) solution.

Dilution - see dilution table.

It is recommended to begin treatment with a dose of 0.5-1.0 mg of nitroglycerin per hour (8-16 mcg/min), if necessary, the dose is gradually (every 3-5 minutes) increased (depending on the effect and response of 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).

If at an injection rate of 20 mcg/min it is not obtained therapeutic effect, a further increase in the rate of administration should be 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. Maximum dose is 8 mg of nitroglycerin in tea (133 mcg/min), in in rare cases 10 mg per hour (166 mcg/min).

For severe angina, the dose is 2-8 mg/h (33-133 mcg/min).

At hypertensive crisis with cardiac decompensation under constant monitoring of blood pressure and heart rate (HR), an infusion is performed at a rate of 2-8 mg/h (average 5 mg/h).

Under controlled arterial hypotension Depending on the type of anesthesia and the required level of blood pressure reduction, the dose is 2-10 mcg/kg/min.

Dilution table

*- 0.9% sodium chloride solution or 5% dextrose (glucose) solution can be used as an infusion solution for dilution.

Infusion table

To assess the incidence of adverse events, we used following criteria(according to the World Health Organization classification): very common (≥10% of prescriptions); often (≥1% and<10%); нечасто (≥0,1% и <1%); редко (≥0,01% и <0,1%); очень редко (<0,01%); frequency unknown(insufficient data to estimate the frequency of development).

From the central nervous system: Often - headache; often - drowsiness, dizziness, incl. postural.

From the gastrointestinal tract: infrequently - nausea, vomiting; very rarely - from a burn.

From the cardiovascular system: often -tachycardia, orthostatic hypotension; infrequently - “paradoxical” intensification of angina attacks, collapse (sometimes accompanied by bradyarrhythmia and fainting); transient hypoxemia e the effect of relative redistribution of blood flow into hypoventilated air V eolar areas (in patients with coronary heart disease - can lead to myocardial hypoxia); rarely - cyanosis; frequency unknown -marked decrease in blood pressure, facial skin hyperemia.

For the skin and subcutaneous tissues: infrequently - allergic skin reactions (including rash); frequency unknown - exfoliative dermatitis.

General disorders: often - asthenia.

Others: infrequently- blurred visual perception; rarely - methemoglobinemia.

For organic nitrates, there have been cases of development of a pronounced decrease in blood pressure, accompanied by nausea, vomiting, anxiety, pallor and increased sweating.

Symptoms: a sharp pronounced decrease in blood pressure (less than 90 mm Hg) with orthostatic dysregulation, reflex tachycardia, a feeling of general weakness, dizziness and lethargy, as well as throbbing headache, “hot flashes” and redness of the skin of the face or upper half of the body, nausea, vomiting and diarrhea.

When using the drug in high doses (more than 20 mg/ml), the development of methemoglobinemia, collapse, cyanosis, shortness of breath and tachypnea is possible; increased intracranial pressure with cerebral symptoms is possible.

Treatment: cessation of drug administration, it is necessary to monitor the function of vital organs. When blood pressure decreases, lower the head of the bed and raise the foot end of the bed. As a rule, blood pressure normalizes within 15-20 minutes; after reselecting the infusion rate, you can resume drug administration.

With a pronounced decrease in blood pressure and/or shock, the volume of circulating blood should be increased; in exceptional cases, an infusion of norepinephrine (norepinephrine) and/or dopamine can be given. The use of eninephrine (adrenaline) and related substances is contraindicated.

For methemoglobinemia, depending on the severity, use ascorbic acid in the form of sodium salt intravenously - 0.1-0.15 ml/kg of a 1% solution up to 50 ml; oxygen therapy, artificial ventilation, hemodialysis.

When used simultaneously with other vasodilators, antihypertensive drugs, incl. beta-blockers, blockers of "slow" calcium channels, angiotensin-converting enzyme inhibitors, as well as phosphodiesterase type 5 inhibitors used to treat erectile dysfunction (for example,), procainamide, antipsychotics, tricyclic antidepressants, monoamine oxidase inhibitors (MAOIs), as well as ethanol may increase hypotensive effect.

With simultaneous use of the drug with dihydroergotamine, there may be an increase in the concentration of dihydroergotamine in the blood, which leads to an increase in its hypotensive effect.

With the simultaneous use of heparin and nitroglycerin, the effect of heparin may be weakened. Under the control of blood clotting parameters, the appropriate dose of heparin is selected. After stopping the nitroglycerin infusion, a significant decrease in blood clotting may occur, which may require a reduction in the dose of heparin.

With the simultaneous use of a solution of nitroglycerin and tissue plasminogen activator, a decrease in the concentration in the blood and a decrease in the effectiveness of the latter due to accelerated hepatic clearance have been described.

Sapropterin is a coenzyme of nitric oxide synthetase, which is important to consider due to the increased risk of arterial hypotension when sapropterin is used simultaneously with all vasodilating agents whose action is associated with nitric oxide, including classical nitric oxide donors (for example, sodium nitroprusside, etc. ).

In order to prevent an undesirable decrease in blood pressure, the rate of drug administration should be individually selected, for which it is recommended to monitor blood pressure and heart rate at least 3-4 times per hour throughout the entire duration of drug administration.

When using Nitroglycerin, redistribution of blood flow in the lungs is possible, which Maybe lead to hypoxemia and cause transient myocardial ischemia in patients with coronary heart disease.

After the first signs of intolerance appear, the drug should not be used again.

When treating patients with type 1 diabetes mellitus, it should be taken into account that the solution contains about 5% glucose.

The solution is sterile and does not contain preservatives. in ampoules or vials should be opened under aseptic conditions immediately before use.

If the patient has previously been treated with organic nitrates, for example, isosorbide dinitrate, isosorbide-5 mononitrate, then large doses of Nitroglycerin may be required to achieve the desired hemodynamic effect.

During the treatment period and for some time after, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Concentrate for solution for infusion, 1 mg/ml.

5, 10 ml in ampoules of colorless neutral glass type I with a colored break ring or with a colored dot and a notch or without a break ring, a colored dot and notch. The ampoules can additionally be coated with one, two or three colored rings and/or two-dimensional s th barcode, and/or alphanumeric encoding or without additional color rings, two-dimensional barcode, alphanumeric encoding.

5 ampoules per blister pack made of polyvinyl chloride film and lacquered aluminum foil or polymer film or without foil and without film. Or 5 ampoules are placed in a pre-made mold (gray) made of cardboard with cells for laying ampoules.

1, 2 or 10 blister packs or cardboard boxes, together with instructions for use and a scarifier or ampoule knife, or without a scarifier and ampoule knife, are placed in a cardboard package (pack).

In a place protected from light, at a temperature not exceeding 25 ° C. Do not freeze.

Keep out of the reach of children.

Do not use after the expiration date.

Nitroglycerin is a widely used cardiac drug that helps to quite effectively and quickly eliminate a painful attack of angina pectoris (popularly angina pectoris) of various origins.

The drug has a pronounced antianginal, as well as vasodilator effect, mainly in the area of ​​the coronary vessels of the heart.

Regular use of Nitroglycerin is indicated for patients who have suffered an acute myocardial infarction or suffer from serious diseases of the cardiovascular system (coronary artery disease, cardiosclerosis, heart failure, etc.).

The drug has a very rapid onset of medicinal action, which develops within 30-40 seconds. after sublingual (under the tongue) administration and continues for 3-4 hours.

Main indications for the use of Nitroglycerin:

• complex treatment and prevention of angina pectoris;
• acute form of myocardial infarction;
• biliary colic;
• heart failure;
• acute form of pancreatitis (inflammation of the pancreas);
• intestinal dyskinesia.

Remember: Before starting to use Nitroglycerin, you must consult a cardiologist or therapist!

This cardiac drug is available in the form of tablets for sublingual administration.

How to take Nitroglycerin?

If an attack of angina develops, Nitroglycerin should be taken exclusively sublingually (under the tongue), and the tablet should be kept in the mouth until completely dissolved.

As a rule, a noticeable improvement in general well-being with a decrease in chest pain begins within 2-3 minutes. after taking this heart drug.

If the pain in the heart has not decreased after 5-6 minutes, it is recommended to repeat taking 1 t. Nitroglycerin under the tongue (you are allowed to drink no more than 3 tablets every 5-10 minutes).

Attention: if after taking Nitroglycerin 3 times, 1 t. under the tongue every 5-10 minutes. pain in the heart area has not decreased, then you need to urgently call an ambulance, as this may indicate the possible development of acute myocardial infarction!

Also, you need to remember that when taking Nitroglycerin regularly, you must definitely exclude any consumption of alcoholic beverages.

Contraindications to the use of Nitroglycerin

• hypersensitivity (increased sensitivity of the body to the main active ingredient of the drug);
• age under 18 years;
• shock state;
• arterial hypotension (low blood pressure);
• increased intraocular or intracranial pressure;
• cardiac bradycardia (heart rate less than 50 beats/min.);
• cardiac tamponade;
• angle-closure glaucoma;
• severe head injuries;
• pregnancy and lactation (breastfeeding).

Side effects of Nitroglycerin

• headache or dizziness;
• skin hyperemia (feeling of heat);
• a sharp decrease in blood pressure (hypotension);