Add to favorites

Heart medicine nitroglycerin. Instructions for use and dosage

Disease class

Angina pectoris [angina pectoris]
Acute myocardial infarction
Congestive heart failure
Left ventricular failure

Clinical and pharmacological group

Not specified. See instructions

Pharmacological action

Antianginal
Vasodilator (vasodilating)
Coronary dilating

Pharmacological group

Nitrates and nitrate-like agents

Capsule Nitroglycerin (Nitroglycerin)

Instructions for the medical use of the drug

Indications for use
Release form
Pharmacodynamics of the drug
Pharmacokinetics of the drug
Contraindications for use
Side effects
Dosage and administration
Overdose
Special instructions for admission
Storage conditions
Best before date

Indications for use

Relief of angina attacks.

Release form

sublingual capsules 0.5 mg; blister pack 20, carton pack 1.2;

Pharmacodynamics

Peripheral vasodilator with a predominant effect on venous vessels. The action of nitroglycerin is mainly associated with a decrease in myocardial oxygen demand due to a decrease in preload (dilation of peripheral veins and a decrease in blood flow to the right atrium) and afterload (decrease in peripheral vascular resistance). It has a central inhibitory effect on sympathetic vascular tone, inhibiting the vascular component of the formation of pain syndrome. Causes the expansion of meningeal vessels, which explains the headache when it is used.

When using sublingual forms, an angina attack usually stops after 1.5 minutes, the hemodynamic and antianginal effect lasts from 30 to 60 minutes.

Pharmacokinetics

Quickly and completely absorbed from the surface of the mucous membranes. When applied sublingually, it immediately enters the systemic circulation. When administered sublingually at a dose of 0.5 mg, bioavailability is 100%, Cmax in blood plasma is determined after 5 minutes. Has a very large volume of distribution. Plasma protein binding - 60%.

Use during pregnancy

During pregnancy and breastfeeding, taking the drug is possible only for health reasons.

Contraindications for use

hypersensitivity to nitrates;

craniocerebral hypertension;

cardiac tamponade;

isolated mitral stenosis;

constrictive pericarditis (conditions accompanied by a decrease in the filling pressure of the left ventricle);

uncontrolled hypovolemia;

heart failure with normal or low pressure in the pulmonary artery;

hemorrhagic stroke;

subarachnoid hemorrhage;

recent head injury

toxic pulmonary edema;

idiopathic hypertrophic subaortic stenosis;

angle-closure glaucoma with high intraocular pressure;

severe anemia;

hyperthyroidism;

age up to 18 years (safety of use has not been established);

violation of cerebral circulation;

arterial hypotension (SBP<90 мм рт.ст.);

concomitant use of sildenafil (Viagra);

pregnancy;

breastfeeding period.

With caution (comparing risk and benefit):

severe renal failure;

liver failure (risk of developing methemoglobinemia).

Side effects

From the side of the cardiovascular system: dizziness, "nitrate" headache, tachycardia, skin flushing, fever, lowering blood pressure; rarely (especially with an overdose) - orthostatic collapse, cyanosis.

From the gastrointestinal tract: dry mouth, nausea, vomiting, abdominal pain.

From the side of the central nervous system: rarely (especially with overdose) - anxiety, psychotic reactions, lethargy, disorientation, blurred vision, headache (especially at the beginning of the course of treatment, decreases with long-term therapy), dizziness and a feeling of weakness. Allergic reactions are possible.

Dosage and administration

The tablet is kept under the tongue until completely resorbed, without swallowing, immediately after the onset of pain - 0.5–1 mg per dose. In many patients with stable angina, the effect also occurs from a lower dose (1/2–1/3 of the table), therefore, if the pain passes quickly, it is recommended to spit out the remainder of the tablet that has not had time to dissolve. Usually, the antianginal effect appears after 0.5-2 minutes; 75% of patients notice an improvement within the first 3 minutes, and another 15% - within 4-5 minutes. In the absence of antianginal action, during the first 5 minutes, you need to take another 1 table. nitroglycerin. In the absence of a therapeutic effect after taking 2-3 tables. you need to call a doctor immediately. The duration of action after sublingual administration is about 45 minutes. With frequent attacks of angina pectoris, it is customary to prescribe prolonged preparations of the nitroglycerin series. Tolerance to sublingual forms of nitroglycerin develops infrequently, however, when it occurs in some patients, the dose of the drug has to be gradually increased, bringing it to 2-3 tables.

Overdose

Symptoms: decrease in blood pressure (<90 мм рт. ст.) с ортостатической дисрегуляцией, рефлекторная тахикардия, головная боль; может развиться астения; головокружение, повышенная сонливость, чувство жара, тошнота, рвота; при применении высоких доз (>20 microns / kg) - collapse, cyanosis, methemoglobinemia, dyspnea and tachypnea.

Treatment: if symptoms of an overdose appear, immediately lay the patient down, raise his legs and urgently call a doctor.

Interactions with other drugs

Simultaneous use with vasodilators, antihypertensives, ACE inhibitors, beta-blockers, CCBs, procainamide, tricyclic antidepressants, MAO inhibitors, phosphodiesterase inhibitors, and ethanol enhances the hypotensive effect.

Appointment with dihydroergotamine can lead to an increase in its content in the blood and an increase in blood pressure (due to an increase in the bioavailability of dihydroergotamine).

The simultaneous appointment of nitroglycerin and heparin reduces the effectiveness of the latter (after discontinuation of the drug, a significant decrease in blood clotting is possible, which may require a decrease in the dose of heparin).

Precautions for use

In the acute period of myocardial infarction and with the development of acute heart failure, it is prescribed under strict control of hemodynamics. Use with caution in aortic and mitral stenosis, in patients with hypovolemia and low SBP (less than 90 mm Hg). In hypertrophic cardiomyopathy, it can cause an increase in and / or worsening of angina attacks. With prolonged uncontrolled intake of nitroglycerin, the appointment of high doses to patients with liver failure and children increases the risk of methemoglobinemia, manifested by cyanosis and the appearance of a brown tint in the blood. In cases of development of methemoglobinemia, the drug must be urgently canceled and an antidote - methylthioninium chloride (Methylene blue) administered. If it is necessary to continue the use of nitrates, it is necessary to control the content of methemoglobin in the blood or replace nitrates with sydnonimines.

To reduce the risk of side effects, care must be taken when taken simultaneously with drugs that have pronounced antihypertensive and vasodilating properties; it is not recommended to take the drug while drinking alcohol, in rooms with a high ambient temperature (bath, sauna, hot shower), as well as taking several tablets at the same time or sequentially in a short period of time at the first dose.

You can not chew tablets and capsules in order to stop an angina attack, because. an excess amount of the drug from the destroyed microcapsules through the oral mucosa can enter the systemic circulation. With the appearance of a headache and other unpleasant sensations in the head area, improvement is achieved by prescribing validol or menthol drops sublingually. Often, only the first doses are poorly tolerated, then the side effects subside.

With simultaneous use with heparin, it is necessary to increase the dose of heparin and strictly control the partially activated thromboplastin time. Use with caution in elderly patients. It is not recommended to prescribe buccal forms to patients with aphthous stomatitis, gingivitis, periodontal and root system diseases, removable upper dentures.

Uncontrolled intake can lead to the development of tolerance, which is expressed in a decrease in the duration and severity of the effect with regular use or the need to increase the dose to achieve the same effect. With regular use of prolonged forms of nitroglycerin, especially patches and ointments, the drug is almost always present in the blood, so the risk of developing tolerance increases significantly. To prevent the emergence of resistance, intermittent use during the day is necessary, or the joint appointment of calcium antagonists, ACE inhibitors, or diuretics. Transdermal forms of nitroglycerin are recommended to be removed from the body at night, thus leaving a period free from the action of the drug. In this case, one should beware of the development of a withdrawal syndrome associated with a sharp cessation of the intake of nitroglycerin in the body and manifested by the sudden development of angina attacks.

With the on / in the introduction, the development of tachyphylaxis is possible, which requires a change in the dosage towards an increase. The degree of tolerance can be judged by the dynamics of pressure in the right atrium. The approach of the tolerance indicator to 25% requires the cessation of the introduction of the solution. To simulate the development of tolerance during intravenous administration, a decrease in the content of nitroglycerin in solution due to a violation of the technique of administration, destruction of nitroglycerin under direct exposure to light rays, or its absorption on the walls of a plastic infusion system (20–80% when using systems made of polyvinyl chloride, polystyrene-butadiene, cellulose propionate, latex or polyurethane). It is recommended to use systems made of chemically pure glass, polyethylene, nylon, teflon, silicone. It is not recommended to use too long hydraulic lines. With the on / in the introduction of nitroglycerin, it must be borne in mind that after the cessation of infusions and when the patient is transferred to tableted (even long-acting) nitrates, a withdrawal syndrome or an insufficient dose may occur, while an increase in the incidence of complications in the acute period of myocardial infarction is possible - an increase in angina attacks, an increase phenomena of circulatory failure, recurrence of myocardial infarction, the formation of acute aneurysm of the heart, an increase in the frequency of myocardial ruptures.

Special instructions for admission

While taking nitroglycerin, a significant decrease in blood pressure and the appearance of dizziness are possible with a sharp transition to a vertical position from a “lying” or “sitting” position, while drinking alcohol, exercising and hot weather. To nitroglycerin, as well as to all organic nitrates, addiction develops with frequent use, and an increase in dose is required.

When driving vehicles and operating mechanisms that require increased attention, it should be borne in mind that taking nitroglycerin can lead to a decrease in the speed of motor and mental reactions.

The severity of headache while taking nitroglycerin can be reduced by reducing its dose and / or concomitantly taking validol.

Storage conditions

List B.: In a dry, cool, dark place, away from sources of fire. (away from fire).

Best before date

Belonging to ATX-classification:

C Cardiovascular system

C01 Cardiac medicines

C01D Peripheral vasodilators used in the treatment of heart disease

C01DA Organic nitrates

I20 Angina pectoris [angina pectoris]

Composition and form of release

in a blister pack 10 or 20 pcs.; in a cardboard pack 1, 2, 3, 4, 5, 6, 8 or 10 packs or in polymer containers of 10, 20, 30, 40, 50 or 100 pieces; in a pack of cardboard 1 container.

Description of the dosage form

Tablets of white or almost white color with a flat surface, risky and chamfered.

pharmachologic effect

Pharmacological action - peripheral vasodilator.

Pharmacokinetics

Quickly and completely absorbed from the surface of the mucous membranes. When applied sublingually, it immediately enters the systemic circulation. When administered sublingually at a dose of 0.5 mg, bioavailability is 100%, C max in blood plasma is determined after 5 minutes. Has a very large volume of distribution. Plasma protein binding - 60%.

Pharmacodynamics

When using sublingual forms, an angina attack usually stops after 1.5 minutes, the hemodynamic and antianginal effect lasts from 30 to 60 minutes.

Indications

Relief of angina attacks.

Contraindications

hypersensitivity to nitrates;

craniocerebral hypertension;

cardiac tamponade;

isolated mitral stenosis;

constrictive pericarditis (conditions accompanied by a decrease in the filling pressure of the left ventricle);

uncontrolled hypovolemia;

heart failure with normal or low pressure in the pulmonary artery;

hemorrhagic stroke;

subarachnoid hemorrhage;

recent head injury

toxic pulmonary edema;

idiopathic hypertrophic subaortic stenosis;

angle-closure glaucoma with high intraocular pressure;

severe anemia;

hyperthyroidism;

age up to 18 years (safety of use has not been established);

violation of cerebral circulation;

arterial hypotension (SBP<90 мм рт.ст.);

concomitant use of sildenafil (Viagra);

pregnancy;

breastfeeding period.

With caution (comparing risk and benefit):

severe renal failure;

liver failure (risk of developing methemoglobinemia).

Use during pregnancy and lactation

During pregnancy and breastfeeding, taking the drug is possible only for health reasons.

Side effects

From the side of the cardiovascular system: dizziness, "nitrate" headache, tachycardia, skin flushing, fever, lowering blood pressure; rarely (especially with overdose) - orthostatic collapse, cyanosis.

From the gastrointestinal tract: dry mouth, nausea, vomiting, abdominal pain.

From the side of the central nervous system: rarely (especially with overdose) - anxiety, psychotic reactions, lethargy, disorientation, blurred vision, headache (especially at the beginning of the course of treatment, decreases with prolonged therapy), dizziness and a feeling of weakness. Allergic reactions are possible.

Interaction

Appointment with dihydroergotamine can lead to an increase in its content in the blood and an increase in blood pressure (due to an increase in the bioavailability of dihydroergotamine).

Overdose

Treatment: if symptoms of an overdose appear, immediately lay the patient down, raise his legs and urgently call a doctor.

Dosage and administration

The tablet is kept under the tongue until completely resorbed, without swallowing, immediately after the onset of pain - 0.5-1 mg per dose. In many patients with stable angina, the effect also occurs from a lower dose (1 / 2-1 / 3 tablets), therefore, if the pain passes quickly, it is recommended to spit out the remainder of the tablet that has not had time to dissolve. Usually, the antianginal effect appears after 0.5-2 minutes; 75% of patients notice an improvement within the first 3 minutes, and another 15% - within 4-5 minutes. In the absence of antianginal action, during the first 5 minutes, you need to take another 1 table. nitroglycerin. In the absence of a therapeutic effect after taking 2-3 tablets. you need to call a doctor immediately. The duration of action after sublingual administration is about 45 minutes. With frequent attacks of angina pectoris, it is customary to prescribe prolonged preparations of the nitroglycerin series. Tolerance to sublingual forms of nitroglycerin develops infrequently, however, when it occurs in some patients, the dose of the drug has to be gradually increased, bringing it to 2-3 tables.

special instructions

The severity of headache while taking nitroglycerin can be reduced by reducing its dose and / or concomitantly taking validol.

Storage conditions

List B.: In a dry, dark place, at a temperature not exceeding 25 ° C.

Nitroglycerin is one of the most popular drugs often used to relieve angina attacks and ischemic conditions. The drug belongs to the group of antianginal drugs with pronounced vasodilatory effects.

Pharmacological forms

The drug is available in different pharmacological forms, which further increases the degree of demand for this drug:

Nitroglycerin tablets (most often the medicine is placed under the tongue, where the active substance very quickly penetrates into the bloodstream through the mucous membrane and vein);
Nitroglycerin spray (a more modern form that allows you to quickly cut the required amount of active substances);
Preparation for injection in ampoules;
Alcoholic solution with the formula of nitroglycerin;
Films on the gums with nitroglycerin (the main indications for use are with increased pressure and angina attacks).

Pharmacological qualities of the drug

Nitroglycerin, according to the instructions for use, is a peripheral vasodilator. It has a direct effect on the structures of the venous walls. Under the influence of the drug, arterioles relax much less, but large arteries and veins are more loyal to the main active substance.

Nitroglycerin tablets, as stated in the instructions for use, reduces the need for myocardial tissue in oxygen. The redistribution of coronary blood flow unloads the heart. The pressure decreases in the pulmonary circulation.

The main indications for the use of the drug

The main indications for the use of Nitroglycerin:

IUBS (both for treatment and as a prophylactic);
Angina pectoris of vasospastic type;
Unstable angina;
Spasm of the coronary arteries;
Acute coronary syndrome;
Myocardial infarction at any stage of development;
cardiac asthma;
All types of pulmonary edema;
Hypotension, which is amenable to medical control;
Prevention of complications from the cardiovascular system during tracheal intubation;
Severe dyskinesia of the alimentary canal;
Functional cholecystitis at the stage of exacerbation;
Biliary colic.

As you can see, the indications for taking Nitroglycerin are not limited to the effect on the work of the heart and blood vessels. Due to its bright pharmacological qualities, the drug is able to solve a whole range of specific therapeutic problems.

Main contraindications

The widespread use of Nitroglycerin is still not always justified. There are some situations, special pathological conditions, when it is not possible to use a medicinal product:

Individual intolerance to this pharmacological product (basic contraindication, which is found in the list of contraindications for all drugs);
Stroke of hemorrhagic type;
Acute heart failure;
Collapse;
The state of acute anemia;
aortic stenosis;
mitral stenosis;
Hemorrhage in the brain tissue;
Toxic edema of pulmonary structures;
Severe and uncontrolled hypotension;
low levels of blood circulating in the body;
Acute renal failure;
Acute liver failure;
Pregnancy;
Active lactation period;
Closed-angle glaucoma, prone to sharp jumps in blood pressure.

How to take the drug correctly

People with chronic diseases of the cardiovascular system often encounter the drug. In the vast majority of cases, doctors recommend keeping Nitroglycerin near you or at least replenishing your first-aid kit with this medication.

The duties of the attending physician include a detailed consultation of patients: how to take Nitroglycerin in tablets, whether it is worth using Nitroglycerin in the form of a spray, what is the price of these drugs and much more.

In modern practice, alcohol solutions (1%) in the sublingual way are used extremely rarely. More convenient to use tablets and capsules. If it is necessary to use an alcohol solution, 2 drops of Nitroglycerin are dripped under the tongue.

Also, the liquid form of the drug can be combined with regular sugar cubes. Patients "with experience" know how to take Nitroglycerin with sugar - a piece is simply placed under the tongue, like a pill.

Tablets

1 or 1/5 tablets are placed under the tongue and wait until it is completely dissolved. It is impossible to swallow or intensively chew capsules or medicine in tablet form. Otherwise, its therapeutic effect is significantly reduced.

The maximum allowable daily dose of the drug is 16 drops of an alcohol solution on sugar (how to make Nitroglycerin with sugar for sublingual intake has already been discussed above) or 6 tablets.

Side effects

In a number of situations, against the background of malaise and taking Nitroglycerin, some side effects may occur. More details about all negative reactions can be found in the table.

Organs and organ systems	Side effects and specific reactions of the patient's body
Nervous system and sense organs	Severe cephalgia; Feeling of severe discomfort in the cranium, a feeling of "bursting"; severe weakness; Motor restlessness; Unstable emotional state; Blurred vision (temporary); Exacerbation of symptoms characteristic of glaucoma
Heart, vessels, blood	Flushing of the face; Strong heartbeat; severe hypotension; orthostatic collapse
digestive tract	dry mouth; Obsessive feeling of nausea; Vomit; loose stool
Dermis	Severe cyanosis; Hyperemia of the face
allergic status	Itching on the skin; Rash; Allergic dermatitis (if contact forms of the drug were used for the therapeutic regimen)

Overdose: how to prevent

Reviews about Nitroglycerin are mostly positive. The bad experience associated with this drug is usually associated with exceeding the permissible dosage of the drug.

Key symptoms indicating that the patient has taken too much Nitroglycerin and caused an overdose:

Severe collapse in people who are not prone to sudden jumps in blood pressure;
Severe headache, not amenable to relief;
Drowsiness;
feeling of heat; severe vomiting;
Methemoglobinemia;
dyspnea;
Tachypnea.

Medical staff immediately lower the head of the bed, and, on the contrary, raise the patient's legs above head level. The introduction of Nitroglycerin is stopped.

Possible antidotes (only the doctor chooses, assessing the patient's condition):

Vitamin C;
Methylthioninium chloride;
Oxygen therapy.

In severe cases, the patient may require an emergency blood transfusion as well as hemodialysis.

Analogues, alternatives and pricing policy

The price of Nitroglycerin is minimal. Tablets and alcohol form are cheaper. Spray and capsules are more expensive. The most expensive form of the drug is nitroglycerin concentrate.

Analogues of Nitroglycerin are used in cases where the main drug for some reason cannot be used.

Main substitutes:

Angiolingual;
Nitragin;
Nitroglycerol;
Nitrocardiol;
NITrong;
Trinitrol.

About drug combinations

Understanding what Nitroglycerin is used for, you can quickly identify the main "partners" with which you have to combine a vasodilator. Everyone needs to know about special pharmacological combinations.

Barbiturates accelerate the absorption of the active ingredients of Nitroglycerin. Enhance the overall hypotensive effect of ethanol, quinidine, most diuretics, antidepressants, calcium antagonists.

The analgesic effect is enhanced when the vasodilator is combined with methionine, ACE inhibitors, salicylates of all kinds.

Unitiol is a specific drug that can neutralize the therapeutic effect of taking Nitroglycerin.

Corticosteroids, m-anticholinergics, and central nervous system stimulants also negatively affect the strength of the drug.

Nitroglycerin is a means of the group of organic nitrates, mainly a venous dilator. Nitrates are able to release nitric oxide from their molecule, which is a natural endothelial relaxing factor - a mediator of direct activation of guanylate cyclase. Increasing the concentration of cGMP 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 to reduce pressure in the pulmonary circulation and regression of symptoms in pulmonary edema, reduces afterload, myocardial oxygen demand (by reducing preload, afterload and ventricular wall tension due to a decrease in heart volume). Promotes the redistribution of coronary blood flow in areas with reduced blood circulation. It has a central inhibitory effect on sympathetic vascular tone, inhibiting the vascular component of the formation of pain syndrome. Causes expansion of meningeal vessels, which explains the appearance of a specific "nitrate" headache. With prolonged or frequent use of long-acting nitrates, tolerance may develop. After a break in treatment, sensitivity to nitrates is restored. In order to prevent the development of tolerance, it is recommended to observe an interval in taking nitrates daily (8-12 hours), preferably at night. In most patients, this therapy is more effective than continuous treatment. When using sublingual forms, an angina attack stops after 1.5 minutes, the hemodynamic and antianginal effect persists for up to 30 minutes. Retard tablets can prevent the development of angina attacks.
Nitroglycerin is rapidly and completely absorbed from the surface of the mucous membranes and through the skin. When taken orally, the bioavailability is no more than 10% compared with sublingual nitroglycerin (the effect of the primary passage through the liver). With sublingual, buccal and / in the introduction, 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, bioavailability is almost 100%, the maximum plasma concentration is observed after 5 minutes. Up to 60% of nitroglycerin binds to plasma proteins. It is rapidly 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. It is excreted in the urine as metabolites. The total clearance is 25-30 l / min, the half-life is 4-5 minutes. With the on / in the introduction, 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 when interacting with reduced hemoglobin.

Indications for the use of the drug Nitroglycerin

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

The use of the drug Nitroglycerin

Inside, sublingually, in / in. Elimination of angina pectoris. Sublingually (a tablet or capsule with a solution is kept under the tongue until completely resorbed, 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 cracked immediately, the capsule can be repeated after 30-40 minutes. Usually, the antianginal effect appears after 0.5-2 minutes, in some cases - within 4-5 minutes. In the absence of antianginal action during the first 5 minutes, another 0.5 mg of nitroglycerin should be prescribed. In the absence of a therapeutic effect after a 2-3-fold dose, the likelihood of developing a myocardial infarction should be taken into account.
When using 1% nitroglycerin solution to stop an attack, 2-3 drops of the solution are applied to a small piece of sugar and kept in the mouth without swallowing until completely absorbed. The duration of action after sublingual administration is about 45 minutes.
With frequent attacks of angina pectoris, it is advisable to prescribe prolonged forms of nitrates. If an angina attack develops during treatment with prolonged forms of nitrates, sublingual nitroglycerin should be taken to stop an acute attack. Tolerance to sublingual forms of nitroglycerin develops infrequently, however, with its development in some patients, the dose has to be gradually increased, bringing it up 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. The maximum daily dose is 0.0348 g. Due to the fact that the bioavailability of nitroglycerin from retard tablets is low, it is recommended, with good tolerance, to take 1-3 tablets at the same time regularly 3-4 times a day or periodically - 30-40 minutes before expected physical activity. With insufficient therapeutic effect, the dose can be gradually increased (but not more than 2 tablets per 1 dose), and after the onset of the therapeutic effect, reduced.
Aerosol for sublingual use: to stop an attack of angina pectoris - 0.4-0.8 mg by pressing the metering valve, preferably in a sitting position, while holding the breath at intervals of 30 seconds; then close your mouth for a few seconds. If necessary, re-introduction, but not more than 1.2 mg for 15 minutes. To prevent an attack - 0.4 mg 5-10 minutes before exercise. In 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 an automatic dispenser or through a conventional system for intravenous infusion. When using a tube system made of PVC, the active substance is absorbed and the losses on the tube walls are up to 60% (it is advisable to use polyethylene and glass tubes). The solution is rapidly destroyed in the light, so the vials and transfusion system must be shielded with opaque material. Usually, an infusion solution is used with a concentration of 100 μg / ml: a concentrated solution is diluted with 0.9% sodium chloride solution or 5% dextrose solution and injected intravenously at an initial rate of 5 μg / 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 a therapeutic effect is not achieved at an injection rate of 20 μg / min, the injection rate can be increased by 10-20 μg / min. When a response occurs (in particular, a decrease in blood pressure), a further increase in the infusion rate is not carried out or carried out at longer intervals. To achieve a good effect, the rate of administration of 0.01% nitroglycerin solution usually does not exceed 100 mcg / min (1 ml / min). In the absence of an effect due to the use of nitroglycerin at lower doses and at an acceptable level of blood pressure, the rate of administration of 0.01% solution can reach 300-400 mcg / min (3-4 ml / min). Further increase in the rate of infusion is impractical. The duration of use is determined by clinical indications and can be 2-3 days.

Contraindications to the use of the drug Nitroglycerin

Hypersensitivity 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 Nitroglycerin

dizziness, "nitrate" headache, tachycardia, skin flushing, feeling hot, lowering blood pressure; rarely (mainly with an overdose) - orthostatic collapse, cyanosis; feeling of dry mouth, nausea, vomiting, abdominal pain; rarely (mainly with an overdose) - anxiety, psychotic reactions, lethargy, disorientation; rarely - allergic reactions (skin itching, rash); local reactions with transdermal application: 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 the possible risk, with recent traumatic brain injury, acute myocardial infarction (risk of lowering blood pressure and tachycardia, which can increase ischemia), glaucoma (risk of increased intraocular pressure), severe anemia, hyperthyroidism, arterial hypotension with low systolic AD (may aggravate the condition by causing paradoxical bradycardia and angina attacks), hypertrophic cardiomyopathy (possible increase in angina attacks), severe renal failure, liver failure (risk of 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 period of treatment, it is necessary to refrain from driving vehicles and engaging in potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions.
Against the background of taking nitroglycerin, a significant decrease in blood pressure and the appearance of dizziness are possible with a sharp transition to a vertical position from a lying or sitting position; when drinking ethanol, exercising and in hot weather. It is also possible to increase angina pectoris with a sharp decrease in 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 headache while taking nitroglycerin can be reduced by reducing the dose of nitroglycerin and / or simultaneously taking validol.

Drug interactions Nitroglycerin

Simultaneous use with vasodilators, antihypertensives, ACE inhibitors, β-adrenergic blockers, calcium antagonists, procainamide, tricyclic antidepressants, MAO inhibitors, phosphodiesterase inhibitors, and ethanol enhances the hypotensive effect of nitroglycerin. Appointment with dihydroergotamine can lead to an increase in its content in the blood and to an increase in blood pressure (increased bioavailability of dihydroergotamine). Care should be taken when combining nitroglycerin with heparin.

Overdose of the drug Nitroglycerin, symptoms and treatment

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

List of pharmacies where you can buy Nitroglycerin:

St. Petersburg

In 1846, the Italian chemist Sobrero synthesized nitroglycerin as an explosive. Since 1879, nitroglycerin drugs have been used to stop angina attacks.

Nitroglycerine(Nitroglycerin; glyceryl trinitrate) is a colorless thick liquid with strong explosive properties. Nitroglycerin preparations used in medical practice are non-explosive.

Nitroglycerin is well absorbed through the mucous membrane of the oral cavity, gastrointestinal tract; penetrates through intact skin.

Nitroglycerin preparations are highly effective in all forms of angina pectoris.

For the relief of angina attacks sublingually used:

1) capsules with 1% oil solution of nitroglycerin (contain 0.0005 or 0.001 g of nitroglycerin);

2) tablets of nitroglycerin, 0.0005 g;

3) metered spray (one dose - 0.0004 g of nitroglycerin);

4) 1% alcohol solution of nitroglycerin (1-2 drops per piece of sugar).

Nitroglycerin is rapidly absorbed through the oral mucosa and has a resorptive effect that develops in 1-2 minutes and lasts about 30 minutes.

When administered orally, these drugs are ineffective, since the bioavailability of nitroglycerin is extremely low (about 2%).

Preparations of nitroglycerin for the relief of angina attacks should be taken in a sitting position (in the standing position, nitroglycerin can cause dizziness, orthostatic hypotension; in the prone position, the drugs are less effective).

To prevent angina attacks tablets with a higher content of nitroglycerin are used, in particular Sustak-forte, Nitrong tablets (contain, respectively, 0.0064 and 0.0065 g of nitroglycerin), etc. These tablets are administered orally; nitroglycerin is gradually released from the tablets; The action of nitroglycerin begins after 10 minutes and lasts an average of 6 hours.

In addition, a transdermal therapeutic system (TTS) with nitroglycerin is used - a special patch of different sizes, which is glued to a healthy area of \u200b\u200bthe skin (usually in the heart area); 1 cm2 of the patch releases 0.0005 g of nitroglycerin per day, which is absorbed through the skin and begins to act after an average of 30 minutes. After 8–12 hours, the effect of nitroglycerin ceases, as addiction to it develops; the patch is removed. The application of a new patch is possible after 12 hours.

Less often, a dosed 2% nitroglycerin ointment is used, which is applied to a healthy skin surface. The action of nitroglycerin begins in 30-40 minutes and lasts 4-6 hours.

For relief and prevention of angina attacks use polymer plates containing 0.001 or 0.002 g of nitroglycerin (in particular, the drug Trinitrolong).

The patient sticks such a plate to the gum; The action begins after 2 minutes and lasts about 4 hours.

For intravenous drip release solutions of nitroglycerin in ampoules. Intravenous nitroglycerin is administered for severe attacks of angina pectoris, acute myocardial infarction, acute heart failure, pulmonary edema.

Mechanism of action. Nitroglycerin is a myotropic antispasmodic. Relaxes the smooth muscles of the blood vessels, bronchi, intestines, bile ducts, ureters.

The antianginal effect of nitroglycerin is determined by its vasodilating properties. Nitroglycerin dilates venous vessels and, to a lesser extent, arterial ones (it is believed that the activity of enzymes, under the action of which NO is released from nitroglycerin, is higher in venous vessels).

The vasodilating effect of nitroglycerin is due to the fact that during the metabolism of nitroglycerin under the influence of thiol enzymes, nitric oxide (NO) is released, which is identical to the endothelial relaxing factor. NO interacts with thiol compounds (in particular, with glutathione) and forms nitrosothiols, which apparently act as a depot for nitric oxide (NO exists in the free state for 1–2 sec).

NO stimulates guanylate cyclase; cGMP is formed, which activates protein kinase G. Protein kinase G promotes the phosphorylation of phospholamban (a protein in the sarcoplasmic reticulum membrane). At the same time, the activity of phospholamban decreases and its inhibitory effect on the Ca 2+ -ATPase of the sarcoplasmic reticulum membrane decreases. Ca 2+ -ATPase promotes the transition of Ca 2+ ions from the cytoplasm to the sarcoplasmic reticulum; the level of Ca 2+ in the cytoplasm decreases. With a decrease in the concentration of Ca 2+ in the cytoplasm of the smooth muscles of the vessels, they relax, the vessels dilate, since the stimulating effect of the Ca 2+-calmodulin complex on the myosin light chain kinase decreases (Fig. 55).

In addition, cGMP activates K + channels, which leads to hyperpolarization of the cell membrane, prevents the opening of voltage-dependent Ca 2+ channels and contraction of smooth muscle fibers.

Rice. 55. Mechanism of vasodilating action of nitroglycerin.

The antianginal effect of nitroglycerin is explained as follows (Fig. 56):

1) Nitroglycerin dilates venous vessels and reduces venous pressure - the flow of venous blood to the heart decreases (the preload on the heart decreases). As a result, the work of the heart and its need for oxygen decreases. Since with a decrease in blood filling of the chambers of the heart, the tension of its walls decreases, extravasal compression of the coronary vessels decreases and coronary blood flow improves.

2) Nitroglycerin dilates arterial vessels, reduces total peripheral resistance of arterial vessels and blood pressure - afterload on the heart, cardiac output, heart work and its oxygen demand are reduced. Lowering blood pressure is only useful to a certain extent, because in this case, the flow of blood to the coronary vessels is reduced.

3) Nitroglycerin dilates large coronary vessels and improves collateral circulation (increases oxygen delivery). In particular, the collateral vessels that connect the large subepicardial arteries with the arteries of the subendocardium expand (the blood supply to the subendocardium improves).

Rice. 56. Mechanism of antianginal action of nitroglycerin.

The total coronary blood flow (90% determined by the lumen of small coronary vessels) changes little. There is a redistribution of coronary blood in favor of the ischemic area. Unlike sodium nitroprusside, nitroglycerin does not cause steal syndrome.

In addition to angina, nitroglycerin is used (intravenously drip) for acute myocardial infarction, acute left ventricular failure, cardiogenic pulmonary edema. In heart failure, nitroglycerin, by reducing the excessive workload on the heart, increases the stroke volume of the heart.

Side effects of nitroglycerin are associated with its vasodilating effect. So, when it is taken under the tongue, it is possible:

Hyperemia of the face, neck, feeling of heat;

Pulsating headache, sometimes very severe (expansion and pulsation of cerebral vessels);

Decreased blood pressure; may be accompanied by tachycardia, dizziness, tinnitus; possible orthostatic hypotension;

Sweating, restlessness, nausea.

With an overdose of nitroglycerin, vascular collapse (a sharp drop in blood pressure) and fainting, increased intracranial pressure, methemoglobinemia are possible. Do not use nitroglycerin with increased intracranial pressure.

With the systematic use of nitroglycerin, it quickly develops addictive; first of all, side effects, in particular headache, are reduced.

Habituation (tolerance) to nitroglycerin is explained by:

1) temporary depletion of glutathione and other cysteine compounds that are involved in the release of NO from nitroglycerin molecules (tolerance decreases with the appointment of N-acetylcysteine);

2) the formation of a superoxide anion (O 2 ·–), which interacts with NO, forming a peroxynitrite anion (ONOO–).

You can not abruptly stop taking nitroglycerin - it may develop pronounced withdrawal syndrome: angina pectoris attacks increase, myocardial infarction is possible.