Nitroglycerin capsules route of administration. Nitroglycerin is an effective vasodilator, indications for use, side effects and reviews

In this article you can find instructions for use medicinal product Nitroglycerine. Feedback from site visitors - consumers - is presented of this medicine, as well as the opinions of specialist doctors on the use of Nitroglycerin in their practice. We kindly ask you to actively add your reviews about the drug: whether the medicine helped or did not help get rid of the disease, what complications were observed and side effects, perhaps not stated by the manufacturer in the annotation. Analogues of Nitroglycerin in the presence of existing structural analogues. Use for the treatment and prevention of angina attacks and myocardial infarction in adults, children, as well as during pregnancy and lactation.

Nitroglycerine- peripheral vasodilator with a predominant effect on venous vessels. Antianginal agent. The mechanism of action is related to the release active substance nitric oxide in vascular smooth muscle. Nitric oxide causes activation of guanylate cyclase and increases cGMP levels, which ultimately leads to smooth muscle relaxation. Under the influence of glyceryl trinitrate ( active substance drug Nitroglycerin) arterioles and precapillary sphincters relax to a lesser extent than large arteries and veins. This is partly due to reflex reactions, as well as the less intense formation of nitric oxide from active substance molecules in the walls of arterioles.

The effect of glyceryl trinitrate 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 (decreased peripheral vascular resistance). Promotes the redistribution of coronary blood flow into ischemic subendocardial areas of the myocardium. Increases exercise tolerance in patients with coronary disease heart disease (CHD), angina pectoris. In heart failure, it helps to unload the myocardium mainly by reducing preload. Reduces pressure in the pulmonary circulation.

Pharmacokinetics

After oral administration, it is absorbed from the gastrointestinal tract and undergoes a “first pass” effect through the liver. When administered sublingually, this effect is absent, and therapeutic concentrations in the blood plasma are achieved within a few minutes. Metabolized in the liver with the participation of nitrate reductase. Of the metabolites of glyceryl trinitrate, dinitro derivatives can cause pronounced vasodilation; perhaps they are the ones who determine therapeutic effect glyceryl trinitrate when taken orally. It is excreted primarily by the kidneys.

Indications

For sublingual and buccal use:

as an emergency aid for acute heart attack myocardium and acute left ventricular failure at the prehospital stage.

For oral administration:

relief and prevention of angina attacks;
rehabilitation treatment after myocardial infarction.

For intravenous administration:

acute myocardial infarction, incl. complicated by acute left ventricular failure;
unstable angina;
pulmonary edema.

For cutaneous use:

prevention of angina attacks.

Release forms

Tablets under the tongue 0.5 mg.

Sublingual capsules 0.5 mg.

Sublingual dosed spray or aerosol.

Solution for intravenous administration (injections in injection ampoules).

Film-coated tablets, prolonged release 5.2 mg.

Instructions for use and dosage

Intravenously (must be diluted in 5% glucose solution or isotonic solution to a final concentration of 50 or 100 mcg/ml): 0.005 mg/min, the dose is increased by 0.005 mg/min every 3-5 minutes. until an effect is obtained or a rate of 0.02 mg/min is achieved (if ineffective, a further increase of 0.01 mg/min).

Sublingual: tablets - 0.15-0.5 mg per dose, if necessary, again after 5 minutes; aerosol - to relieve an attack of angina - 1-2 doses under the tongue, pressing the dosing valve (can be repeated, but no more than 3 doses within 15 minutes). In case of development of acute left ventricular failure, it is possible to use 4 or more doses over a short period.

Transdermal: stick on each time new site skin and leave for 12-14 hours, after which it is removed to provide a break of 10-12 hours to prevent the development of tolerance.

Orally: tablets and capsules are taken without chewing or breaking, 2-4 times a day before meals, preferably 30 minutes before. before physical activity, single dose is 5-13 mg; due to poor bioavailability, a single dose may increase to 19.5 mg.

Subbuccally: the tablet is placed on the oral mucosa (behind the cheek) and held until completely absorbed: 2 mg 3 times a day.

Side effect

dizziness;
headache;
tachycardia;
hyperemia of the skin;
feeling of heat;
arterial hypotension;
collapse;
cyanosis;
nausea, vomiting;
anxiety;
psychotic reactions;
skin rash;
burning and redness of the skin.

Contraindications

collapse;
arterial hypotension (systolic blood pressure<100 мм. рт.ст., диастолическое АД<60 мм. рт.ст.);
acute myocardial infarction with severe arterial hypotension;
hypertrophic obstructive cardiomyopathy;
constrictive pericarditis;
cardiac tamponade;
toxic pulmonary edema;
increased intracranial pressure (including with hemorrhagic stroke, after a recent head injury);
angle-closure glaucoma with high intraocular pressure;
increased sensitivity to nitrates.

Use during pregnancy and breastfeeding

The use of Nitroglycerin during pregnancy and lactation (breastfeeding) is possible only in cases where the expected benefit to the mother outweighs the potential risk to the fetus or infant.

special instructions

Use with caution in patients with severe cerebral atherosclerosis, cerebrovascular accidents, with a tendency to orthostatic hypotension, with severe anemia, in elderly patients, as well as with hypovolemia and severe impairment of liver and kidney function (parenterally).

With prolonged use, tolerance to the effects of nitrates may develop. To prevent the occurrence of tolerance, it is recommended to observe a 10-12 hour break in their use during each 24-hour cycle.

If an attack of angina occurs with cutaneous use of glyceryl trinitrate, it should be stopped by taking glyceryl trinitrate under the tongue.

During the treatment period, avoid drinking alcohol.

Impact on the ability to drive vehicles and operate machinery

Nitroglycerin may reduce the speed of psychomotor reactions, which should be taken into account when driving vehicles or engaging in other potentially hazardous activities.

Drug interactions

When used simultaneously with vasodilators, ACE inhibitors, calcium channel blockers, beta-blockers, diuretics, tricyclic antidepressants, MAO inhibitors, ethanol (alcohol), ethanol-containing drugs, the hypotensive effect of glyceryl trinitrate may be enhanced.

When used simultaneously with beta-blockers and calcium channel blockers, the antianginal effect is enhanced.

When used simultaneously with sympathomimetics, it is possible to reduce the antianginal effect of glyceryl trinitrate, which, in turn, can reduce the pressor effect of sympathomimetics (as a result, arterial hypotension is possible).

With the simultaneous use of drugs with anticholinergic activity (including tricyclic antidepressants, disopyramide), hyposalivation and dry mouth develop.

There is limited evidence that acetylsalicylic acid, used as an analgesic, increases plasma concentrations of glyceryl trinitrate. This may be accompanied by increased hypotensive effect and headaches.

A number of studies have observed a decrease in the vasodilating effect of glyceryl trinitrate during long-term therapy with acetylsalicylic acid.

It is believed that it is possible to enhance the antiplatelet effect of acetylsalicylic acid with the use of Nitroglycerin.

When used simultaneously with glyceryl trinitrate, the effect of acetylcholine, histamine, and norepinephrine decreases.

Against the background of intravenous administration of Nitroglycerin, the anticoagulant effect of heparin may be reduced.

With simultaneous use, it is possible to increase the bioavailability of dihydroergotamine and reduce the antianginal effect of glyceryl trinitrate.

When used simultaneously with novocainamide, the hypotensive effect and the development of collapse may be enhanced.

When used simultaneously with rizatriptan, sumatriptan, the risk of developing coronary artery spasm increases; with sildenafil (Viagra) - the risk of developing severe arterial hypotension and myocardial infarction; with quinidine - orthostatic collapse is possible; with ethanol (alcohol) - severe weakness and dizziness.

Analogues of the drug Nitroglycerin

Structural analogues of the active substance:

Gluconite;
Deposit 10;
Nirmin;
Nit-ret;
Nitradisk;
Nitro;
Nitro Mac Ampoules;
Nitro McRetard;
Nitro Pol infusion;
Nitro-dur;
Nitro-Nick tablets;
Nitroglycerin microgranules;
Nitroglycerin Nycomed;
Nitroglycerin forte;
Nitrogranulonga film-coated tablets;
Nitroject;
Nitrocor;
Nitrolingual-Aerosol;
Nitrolong;
Nitromint;
Nitrong forte;
Nitrong;
Nitropercutene TTC;
Nitrospray;
Nitrospray-ICN;
Nitrosprint;
Perlinganite;
Sustak mite;
Sustak forte;
Sustonite;
Trinitrolong.

If there are no analogues of the drug for the active substance, you can follow the links below to the diseases for which the corresponding drug helps, and look at the available analogues for the therapeutic effect.

Why is Nitroglycerin prescribed?

Nitroglycerin is a well-known medicine that can effectively resist heart disease. It is qualified to prevent the development of angina pectoris and its harmful consequences. The drug has a number of advantages. Let's look at what pharmaceuticals help with and why they are prescribed by doctors.

Form of production and composition

Tableted. Sublingual administration. The tablets are white or yellowish in color. An integral component is nitroglycerin itself and other auxiliary elements, in particular lactose, macrogol, crospovidone and povidone;
Solution. Contained in ampoules. In addition to the active element, it contains potassium dihydrogen phosphate, sodium chloride, dextrose and water;
Sublingual spray. It is a colorless liquid in bottles with a dispenser pump. Additional component – 95% ethanol;

Also on sale are drops under the tongue, a concentrate for the preparation of a solution administered intravenously.

Action of the medication

The action of the active component is carried out by increasing the concentration of guanosine monophosphatases, preventing calcium ions from entering the smooth muscle environment. The blood vessels also dilate, reducing venous outflow into the heart muscle, preventing a large circle of blood flow. It has a beneficial effect on blood vessels and inhibits pain syndromes.

The tablets act for up to 1.5 minutes after use. The effect lasts up to half an hour. They are absorbed in the shortest possible time and fully enter the circulatory system.

After using the spray, the maximum concentration in the body is reached in four minutes. Bioavailability is one hundred percent. This is due to the fact that hepatic degradation of the drug is prevented. Connection with blood proteins – 60%. Excreted by the renal system.

Indications for use

Taking Nitroglycerin is indicated in the following cases:

Presence of angina attacks;
Biliary tract disorder;
Pathologies of the retinal artery;
Left ventricular failure.

Contraindications

Nitrate intolerance;
Severe heart pathologies - tamponade;
Increased intracranial pressure;
Rupture of cerebral vessels;
Angle-closure glaucoma;
Release of thyroid hormones into the blood;
Previous head injuries;
Toxic pulmonary edema;
Anemia;
Minor age;
Reduced blood pressure level.

Persons with kidney and liver problems should definitely consult with a specialist regarding the advisability of treatment. Otherwise, an incorrect therapeutic regimen can lead to extremely negative consequences.

Use during pregnancy and lactation period

In preparing a woman for the process of childbirth, her body endures excessive stress. This is especially true for the heart and blood vessels. This increases the volume of blood, part of which is supplied to the fetus. Heart rate increases accordingly.

If you experience pain in the sternum and suspect heart problems, you should immediately contact a doctor. Such symptoms, which at first glance seem harmless, are in fact often harbingers of serious illnesses that require prompt treatment.

The drug can be taken during pregnancy, but only when the benefits to the mother are truly greater than the potential risks to the fetus. As for nursing mothers, this process should be stopped for a while.

Key points of the treatment process

Do not allow the solution to come into contact with the body. During suction, headache may occur;
It is not uncommon for addiction to the product to occur;
There is a slowdown in the reaction. This indicates the need to refuse potentially dangerous work, operating complex machinery and vehicles;
During the fight against an attack of severe chest pain, it is forbidden to chew the pill. This will cause excessive entry of active substances into the circulatory system;
Alcohol is strictly prohibited during therapy.

Side effects

As a rule, the drug is usually tolerated without problems, but a number of bad phenomena cannot be ruled out.

Migraines, problems with the vestibular system, low blood pressure, weak condition, and visual disturbances are allowed.

From the gastrointestinal tract, vomiting, diarrhea, and a feeling of dry mouth are possible.

Sometimes there are skin rashes, characterized as allergies and other equally pleasant phenomena - fever, angina exacerbations. In the worst case, the patient can suffer a heart attack, leading to death.

How to take the medicine

Instructions for use:

Sublingual pills should be kept until completely dissolved. Ingesting them is prohibited. After the onset of pain, 0.5 to 1 mg is used. When pronounced syndromes cease, resorption can be stopped.

The absence of a positive effect suggests an increase in dosage by 0.5 mg. If there is no improvement in the condition, you should urgently seek medical help.

The spray is applied under the tongue. To achieve a sufficient therapeutic effect, 1–2 doses are required by pressing the dosing pump.

The amount of solution injected into the body is determined by the attending doctor.

Consequences of overdose

The patient experiences severe pain in the head, decreased blood pressure, destabilized heart rate, dizziness, diarrhea, nausea, feeling hot and the desire to sleep.

The large dose size is from 20 mg. This amount can cause orthostatic collapse and even coma in the patient, followed by death.

Mild forms of overdose are treated by moving the person to a horizontal position. The patient's legs are raised. In a worse situation, general methods of overcoming shock and intoxication are used.

Compatibility with other medications

Salicylates. Promote a multiple increase in the level of nitroglycerin in the blood;
Barbiturates. Accelerates the metabolic processes of nitroglycerin;
Heparin. Reduces effectiveness;
The effect of the medication is enhanced by the concomitant use of antihypertensive and antiadrenergic medications, as well as sildanefil;
Taking acetylcysteine (N), ACE inhibitors, increases antianginal activity;
Alpha adrenergic agonists, anticholinergics, histamines, pituitrins, corticosteroids reduce the effect of the pharmaceutical product in question.

How much does Nitroglycerin cost - price at the pharmacy

It is an affordable medicine for almost everyone. The price ranges from 18 to 519 rubles (depending on the release format). Sale - by prescription from doctors from the appropriate institution. Cost information was taken from some of the most famous Russian online pharmacies.

Nitroglycerin analogues

Perlinganite

A decent generic in the form of a solution. Overcomes various types of angina, the consequences of acute myocardial infarction, hypertensive crisis.

Prohibited in case of acute circulatory problems, obvious hypotension, cardiogenic shock.

It is administered intravenously using an infusion syringe pump. The doctor selects the dose using an individual approach. On average it ranges from 0.75 to 10 mg. Depends on the severity of the disease.

Nitromint

Used to relieve and prevent the development of symptoms of angina pectoris. Helps against acute left ventricular failure, but only with the use of additional pharmaceuticals.

Not indicated for patients in shock, with a clearly harmful reaction to the composition and under 18 years of age. You need to be especially careful in cases of problems with blood circulation, including hemorrhagic hemorrhage in the brain, problems with blood pressure, pathologies of the liver and kidneys, and angle-closure glaucoma.

The medicine is sprayed under the tongue. 1-2 doses are enough - 400 or 800 mcg, respectively. Therapy must be carried out in a sitting position, holding your breath. After applying the drug, the patient closes the oral cavity for several seconds. In some situations, re-use is allowed. Insufficient beneficial effect allows repeated use of a similar dose after 10 minutes.

Nitrospray

It shows itself well in the fight against cardiac pain syndrome, does not allow them to develop, and is indicated for acute heart attack.

It is not prescribed for hypersensitive patients with severe hypotension, cardiomyopathy, stroke with vascular rupture, head injuries, pulmonary edema and angle-closure glaucoma.

Apply under the tongue. To combat the main indications, one or two doses are enough. Maximum – four (1.6 mg). Per day up to 6.4 mg.

Nitrosorbide

Sold in the form of tablets and solution. The latter is intended for intravenous administration. Qualitatively resists angina attacks, and is also prescribed in the post-infarction state.

Nitrosorbide is not allowed for people after a head injury, low blood pressure, or stroke.

The minimum dose is 10 mg, divided into 4-5 doses over 24 hours. To increase the effect, 60–120 mg per day can be used. It differs from all the listed sublingual analogues in that the tablet can be chewed, which will bring the therapeutic effect even faster. Its period will be determined by a qualified doctor. After achieving a favorable clinical picture and proper dynamics, therapy should be stopped in stages.

Nitrogranulong

Prevents and relieves angina-type pain. Competent in the recovery of a patient after suffering a myocardial infarction of any form. Produced in the form of tablets and solution. The last medicinal type is used for acute manifestations of the listed ailments - it is administered intravenously.

Not intended for the treatment of minors with excessive intraocular pressure, liver and kidney disease. Pregnant women and breastfeeding babies should refuse.

The total period of resistance to these ailments depends on the immediate dynamics of the therapeutic period. The right to establish a clear scheme and rules is established by the doctor.

Dikor Long

Provides qualified assistance for chest pain and during post-infarction rehabilitation. It dilates blood vessels well, relieves the heart, which allows it to adequately saturate its system with oxygen.

It will not help people with low blood pressure and high intracranial, cerebral hemorrhage, or head injury.

Therapeutic rules are set by doctors.

Nitrocor

The simplest substitute is in the form of pills. The main indication is angina pectoris.

Not allowed for people with glaucoma, obvious intracranial pressure, impaired cerebral blood flow and cerebral atherosclerosis.

0.15-0.5 mg tablets are placed under the tongue. Let's say it happens again in 5 minutes.

Diseases of the cardiovascular system are a common occurrence in the modern world, where people lead a sedentary lifestyle, often find themselves in stressful situations and have bad habits. The drug Nitroglycerin can come to the aid of a person with heart disease. This article will tell you how Nitroglycerin works, what its types are and indications for use.

Action of Nitroglycerin

The drug Nitroglycerine (English – Nitroglycerine) is a synthetic substance that quickly dilates blood vessels, stopping ischemic attacks in the myocardium. The main effect of Nitroglycerin is short-term prevention of angina pectoris and relief from pain. The medication has the following effects on the cardiovascular system:

decreased venous return of blood to the heart;
distribution of blood flow in the myocardium;
improving the contractile function of the heart muscle;
decreased myocardial oxygen demand;
relaxation of the smooth muscles of the heart walls.

Nitroglycerin - indications

The drug Nitroglycerin is mainly used in cardiology. In pharmacies you can find this medication in the form of tablets, capsules, ampoules, spray, solution and ointment. To find out in what cases Nitroglycerin is taken, and in which type, you should definitely consult a doctor and carefully read the section of the instructions “Nitroglycerin - indications for use”.

Main indications for the use of nitroglycerin:

Nitroglycerin – tablets

Capsules and tablets contain 0.5 mg of the substance. Nitroglycerin tablets are taken subbucally (in the cheek), and capsules are taken sublingually (under the tongue). There is no need to chew or break the tablet; it is placed on the mucous membrane of the mouth and remains there until completely dissolved. The tablets are used up to four times a day, half an hour before meals. A single dose can reach 19.5 g, since the penetration of the substance into the body in this form is complicated.

Nitroglycerin – spray

The medication in aerosol form has a faster effect than tablets or solution. Nitroglycerin spray is used by spraying in the mouth under the tongue. One spray can contains 250 doses (30 g) or 100 doses (12 g). To stop an attack of angina, 1-2 doses are enough. It is impossible to increase the norm by 3-4 doses of aerosol in 15 minutes. The main indication for the use of the spray is painful spasms of the heart muscle.

Nitroglycerin ointment

Nitroglycerin in the form of ointment has no indications for use in cardiology. Nitroglycerin ointment 0.2% is used in medicine in proctology for the treatment of hemorrhoids and anal fissures. Nitroglycerin ointment, when applied topically, dilates blood vessels, improving blood circulation and promoting tissue regeneration. The drug has the property of reducing combat sensations and healing fissures in the anorectal area.

Nitroglycerin in ampoules

The use of nitroglycerin in ampoules is carried out by intravenous administration through a dropper. The duration of administration and dose of the liquid substance must be correctly calculated by the doctor; doing this on your own is dangerous. For intravenous use, the ampoule should be diluted in an isotonic solution or a five percent glucose solution to a concentration of 50 or 100 mcg/ml. Indications for the use of nitroglycerin ampoules are acute myocardial infarction, severe forms of angina.

Instructions for use

To find out how to drink nitroglycerin, you should consult your doctor and read the instructions for use of the drug. The type of medication, method of administration and dosage are prescribed individually for each patient, based on his medical history. Instructions for the use of nitroglycerin should be familiar to every person suffering from angina or cardiac ischemia.

In case of an angina attack, you should put the whole tablet or half of it under your tongue. There is no need to chew or swallow the medicine - just keep it under your tongue. The pain should disappear after one to three minutes. If the pain has passed, the remaining tablets should be spat out, and if relief does not occur, put another capsule under the tongue. If two tablets do not help, consult a doctor immediately.

Dosage

To find out how to take nitroglycerin for the heart, you should definitely contact a medical facility. The dosage of nitroglycerin is determined by the doctor, taking into account the characteristics and indications of the disease, the physiological parameters of the patient and the nature of the pain. Excessive use of the drug, taking the drug without indications for use, or exceeding the recommended dose can cause an overdose.

Consequences of overdose:

decreased blood pressure (blood pressure);
dizziness, migraine;
weakness and body aches;
increased temperature and intracranial pressure;
nausea, stomach cramps.

Side effects

Before taking the medicine, you should find out what nitroglycerin is for and what complications it can create. Before using the product, be sure to read its composition and information about expiration dates. The body's intolerance to this drug can provoke the following side effects of nitroglycerin:

For the sensory organs and nervous system: headache, weakness, dizziness, blurred vision, motor restlessness, feeling of fullness in the head, psychotic reactions, exacerbation of glaucoma.
For the cardiovascular and circulatory systems: hypotension, flushing, methemoglobinemia, collapse.
For the gastrointestinal tract: nausea, diarrhea, vomiting, dry mouth.
For the skin: skin redness, hyperemia, cyanosis.
Allergic reactions: contact dermatitis, burning and itching.
Other: feeling of heat, hypothermia, paradoxical phenomena - angina attack, development of tolerance, myocardial infarction up to sudden death.

Contraindications

The use of the medication is prohibited during pregnancy, for children and for mothers nursing a child. Other contraindications for nitroglycerin:

cerebral ischemia;
low blood pressure;
hemorrhagic stroke;
high intracranial pressure;
vascular collapse or shock;
cardiac tamponade;
angle-closure glaucoma;
toxic pulmonary edema;
hyperthyroidism;
bradycardia;
severe anemia;
cerebral hemorrhage;
acute vascular insufficiency;
intolerance to nitroglycerin or other nitrates.

Nitroglycerin price

The drug Nitroglycerin is an indispensable remedy for people suffering from cardiovascular diseases. The medicine is relatively inexpensive, and you can find it in almost every pharmacy, since it is one of the essential medicines. Find out how the price of Nitroglycerin 500 mcg tablets differs in different pharmacies in Moscow in the table below.

“Nitroglycerin” is a medication containing a nitric acid compound and a glycerol ester. For 150 years, the medicine has been widely used to quickly relieve heart pain. A wide range of indications for the use of Nitroglycerin allows the drug to be used for the treatment of cardiac patients. Its widespread use is due to its vasodilating and antispasmodic properties. But before using Nitroglycerin, it is recommended to carefully read its instructions for use. It will make it possible to find out what Nitroglycerin helps with, in what cases it is contraindicated, and what is the mechanism of action of Nitroglycerin.

“Nitroglycerin” is a drug belonging to the group of nitrates and has a venodelatating effect. The mechanism of action of Nitroglycerin is as follows:

It is due to the nitrogen included in the structure of the drug, which, in combination with oxygen, creates a new chemical substance - nitric oxide.
It is a natural relaxer of the endothelial layer of blood vessels due to the activation of the guanylate cyclase system. Due to an increase in cGMP, smooth muscle structures expand, especially venous fibers. At the same time, under the influence of the drug, the muscles of the gastrointestinal tract, bronchi, bile ducts and urinary tract relax. Intravenous administration allows the peripheral veins to dilate, which reduces cardiac overload.

As a result of vasodilation in the right atrium, blood flow decreases, pressure in the pulmonary circulation decreases, as a result of which the symptoms of pulmonary edema become less acute. In an area with reduced blood supply, blood flow is redistributed, the pressure in the chambers is normalized, tension and stress on the heart are relieved, this reduces the need for oxygen in the myocardium. The drug inhibits the negative effect on the sympathetic fibers of blood vessels, which helps relieve pain. Due to the use of the medicine, the cerebral vessels also dilate, so sometimes a headache occurs after taking it.

Due to its ability to relieve the tone of the walls of the coronary vessels and expand their lumen, the drug is prescribed to people with various heart diseases to relieve manifestations of angina of any type, relieve pain, and improve condition after a heart attack.

Existing forms of release

The rate of absorption and activity of the drug is determined by the form of the drug and the option of its use. "Nitroglycerin" release form:

When taken sublingually (under the tongue) in tablet forms or capsules, the drug is completely absorbed. Its effect is felt within a minute to a minute and a half after dissolution in the oral cavity, the duration of exposure is about half an hour. Bioavailability – 100%. After 5 minutes, the active substance, having reached its maximum concentration in the blood plasma, binds to proteins by 60%.
When tablets coated for prolonged action are ingested, the substance passes through the digestive system and is absorbed into the blood in the small intestine. It begins to act half an hour after swallowing, bioavailability is no more than 10%.
“Nitroglycerin” spray, after spraying onto the mucous membrane under the tongue, is quickly and completely absorbed, the medicine appears in the bloodstream almost immediately, and accumulates in the plasma to the maximum after 4 minutes. When excreted by the kidneys, less than 1% of the ingested volume leaves the body.
The film for gluing to the gums stops the attack in a minute - one and a half.
The concentrated injection liquid is injected directly into a vein.
The ointment is used externally (also for the treatment of hemorrhoids). The effect is observed after a quarter of an hour, a maximum of an hour. The drug is effective for up to 5 hours.
The transdermal system is represented by a multilayer patch. The use of Nitroglycerin through the skin ensures a constant release of the drug. The gradual entry of the active component into the blood vessels of the dermis ensures its presence in the vascular bed in a stable concentration for the entire period while the patch is on the skin. The dose depends on the size of the area that the patch covers. The result after gluing appears after half an hour (the maximum period reaches 3 hours), the effect of “Nitroglycerin” lasts up to 10 hours.

The drug is metabolized in the liver and excreted from the body by the kidneys. When taking Nitroglycerin, it is important to remember that its long-term use, especially prolonged forms, forms tolerance (resistance) to the component. The result is a decrease in productivity. Therefore, while taking the medicine, the doctor recommends pausing its use for 8 to 12 hours.

Indications

Indications for the use of Nitroglycerin include:

prevention and treatment of angina attacks;
myocardial infarction and post-infarction period;
blockage of the retinal artery;
bile duct dyskinesia;
acute pancreatic failure accompanied by pulmonary edema.

The drug is used during surgery to prevent blood loss.

Reception rules

"Nitroglycerin" instructions contain the following information on the rules of administration:

Tablet forms

How to take the capsule or tablet sublingually? At the moment when heart pain appears, the drug is placed under the tongue in a dosage of 0.5 to 1 mg. If the pain does not go away, it is allowed to use another 0.5 mg after 5 minutes. It is permissible to take a second dose after half an hour. If a positive result occurs, if the tablet has not yet dissolved, it must be removed from the mouth. How many tablets are allowed to be taken once? No more than 3 pieces are used per attack. If there is no effect, a heart attack most likely developed. Urgent medical attention is required.

When heart pain occurs frequently, the doctor prescribes a long-acting medication for preventive purposes. "Retard" is available in tablets of 2.6 mg. Nitroglycerin is taken at least 3 times a day. In severe cases, the dosage is doubled. But if an attack develops, you can additionally take one tablet under the tongue. Nitroglycerin extended-release should be swallowed, so its effect occurs later, since part of the active component is inactivated in the liver. Medications are indicated to prevent an attack before emotional or physical stress.

"Nitroglycerin" aerosol

Available in cans for sublingual use. The convenient form allows you to quickly administer the required dose to eliminate an attack of angina and in the event of the development of pulmonary edema. The nitrospray is administered according to the instructions for use: sitting, shaking the can, and spraying the drug into the mouth with one or two presses of the dispenser. In this case, you need to hold your breath; you don’t need to swallow right away. During severe heart pain, nitrospray is also used. The instructions allow you to use up to 3 clicks at intervals of 5 minutes. For pulmonary edema, the maximum volume is 4 doses. The medicine can be used in one dose for prevention before stress or physical activity in 5 minutes.

Film

The composition of "Nitroglycerin" from a biosoluble polymer ("Trinitrolong") is as follows: 1 - 2 mg of the active ingredient. The film is glued to the mucous membrane of the upper gum. After painful sensations appear, press it with your fingers for a few seconds. To increase the suction speed, you can run your tongue over it a couple of times, being careful not to move it from its place. When the pain has passed and the film has not dissolved, it is removed. If the effect does not occur within 5 minutes, you are allowed to use the medicine again. After twice unsuccessful use, immediate medical attention is required.

Drops

The drops are a 1% solution of nitroglycerin in alcohol. They are used sublingually for pain relief. One or two drops are applied to a piece of sugar, it is placed in the mouth and dissolved until dissolved.

Ointment

How to use ointment with nitroglycerin? Initially, for cutaneous use, the permissible volume of the product is 2.5 cm column. If the dosage is insufficient, it is gradually doubled; it is permissible to apply up to 10 cm per day. The ointment is squeezed onto dosage paper and applied to the skin without hair.

Intravenously

Nitroglycerin is administered intravenously, individually selecting the rate at which the solution enters the blood. For this, a special dispenser or dropper is used. In the latter case, drops are counted. The initial injection rate is 5 mcg/min. Subsequently, after 3–5 minutes it is increased. The figure will depend on the body’s reaction – blood pressure and heart rate. The duration of treatment is usually up to 3 days. If necessary, administration is resumed.

Interaction

At an appointment with a cardiologist, it is important to tell about all the medications you are taking to avoid unwanted reactions:

The use of Nitroglycerin in parallel with vasodilators, some types of antidepressants, anti-arrhythmia tablets, diuretics or blood pressure medications and beta blockers enhances the hypotensive effect.
When taken simultaneously with salicylates, the concentration of the drug increases.
When administered intravenously, the drug reduces the effect of Heparin.

Nitroglycerin should not be used together with alcohol, as the risk of developing hypotension increases. Moreover, any heart disease requires abstinence from alcohol-containing drinks, since the product negatively affects the condition and functioning of the organ. The air temperature should also be taken into account: in the warm season, in hot weather, a sharp decrease in pressure is also possible.

Contraindications

Has "Nitroglycerin" and contraindications. The drug is not prescribed in the following cases:

with nitrate intolerance;
with hypotension;
with galactosemia;
with pericardial tamponade;
with adhesive pericarditis;
while taking phosphodiesterase inhibitors.

Use with extreme caution when:

increased ocular and intracranial pressure;
tendency to hypotension;
congestion in the right ventricle of the heart;
low hemoglobin;
hyperthyroidism;
severe kidney and liver diseases;
heart valve defects.

Nitroglycerin is not prescribed during pregnancy and lactation, or for young people under 18 years of age.

Side effects

Side effects after consuming Nitroglycerin include:

The nervous system is bothered by dizziness, incoming headaches, a feeling of fullness inside the head, weakness, and the development of paradoxical effects.
The heart and blood vessels can respond with flushes to the surface of the skin, hypotension, and palpitations.
The digestive organs react with nausea, dry mouth, sometimes vomiting, and diarrhea.
The allergy is expressed by itching; when using cutaneous forms, contact dermatitis cannot be ruled out.

With glaucoma, vision loss and worsening of the disease are possible.

Overdose of Nitroglycerin

You can get an excess dose of the drug by taking it in any form, and the onset of collapse is noted. The condition is characterized by a sharp decrease in blood pressure when standing up. An overdose of Nitroglycerin also manifests itself:

increasing weakness;
decreased blood pressure;
an increase in methemoglobin in the blood;
shortness of breath and burning in the throat;
swelling of the skin;
development of cyanosis (appearance of blue areas on the skin);
hypothermia;
ischemia, the development of a heart attack with sudden death cannot be ruled out.

The drug is classified as a toxic substance, as absorption through the mucous surface occurs quickly. The amount of medication that can cause Nitroglycerin poisoning ranges from 25 to 75 mg.

Lethal dose of Nitroglycerin

The drug “Nitroglycerin” also has a lethal dose, because this chemical actively affects the body. These indicators are individual for each person. Severe poisoning develops if you drink 100–150 mg/kg, and death is possible. When 210 mg/kg is taken orally, death occurs within 2 minutes. There have been situations where the death of a patient occurred when taking the recommended dose, but the interval between doses was not observed.

Any form of “Nitroglycerin” requires a doctor’s prescription in a strictly specified dosage. Take the drug on your own if your doctor has recommended its use during attacks or as a preventative measure. If the effect of Nitroglycerin does not appear, call an ambulance.

Nitroglycerin is a peripheral vasodilator used primarily for coronary heart disease to relieve attacks of angina. Nitrates (nitroglycerin), along with calcium antagonists and *-adrenergic blockers, belong to the group of so-called antianginal drugs that level out the disturbed balance between the need of the heart muscle for oxygen and its transportation, while nitrates best meet the target requirements. Nitroglycerin has been used for more than a century, and there have long been no secrets in its mechanism of action. This drug (as well as other nitrates) is a donor of NO - nitric oxide, which relaxes the smooth muscle walls of blood vessels by increasing the content of cGMP. In a clinical sense, this is very beneficial. Thus, due to the dilation of the veins of the lower extremities, more blood remains there, which reduces the preload on the heart and diastolic blood pressure. At the same time, nitroglycerin relieves spasm of the coronary arteries, increases peripheral blood flow, “forces” the myocardium to share blood with its ischemic areas and dilates the resistive vessels that are most resistant to blood flow, which leads to a decrease in afterload on the heart. Thus, nitroglycerin reduces oxygen deficiency in two ways: it reduces the work of the heart while simultaneously increasing blood flow in it.

Despite its venerable age, nitroglycerin remains to this day an unrivaled remedy for relieving angina attacks. A nitroglycerin tablet under the tongue becomes an integral part of the lives of people suffering from this characteristic manifestation of coronary heart disease.

Taking nitroglycerin obliges the patient to comply with pharmacological discipline, in other words, certain rules with which the doctor must first familiarize him.

Nitroglycerin is available in several forms: capsules and sublingual tablets, incl. prolonged action, sublingual spray, solution for intravenous administration. It belongs to a group of drugs that cannot be abruptly discontinued due to rebound syndrome. In the case of nitroglycerin, it will manifest itself by increasing the frequency of angina attacks. Some changes in the patient's usual state are associated with taking nitroglycerin: a pronounced decrease in blood pressure and the appearance of dizziness when standing up suddenly, drinking alcohol and physical activity (especially in hot weather conditions) are possible. Nitroglycerin is characterized by the development of a phenomenon called tolerance, when, with long-term use, an increase in the dosage of the drug is required to achieve the desired therapeutic effect. It is often recommended to mitigate headaches accompanying the drug by simultaneous administration of validol or by reducing the dose. If side effects are severe (blurred vision, hyposalivation), nitroglycerin should be discontinued. Nitroglycerin spray contains alcohol, so when prescribing this dosage form, special caution should be exercised in relation to persons with central nervous system diseases.

Pharmacology

Peripheral vasodilator with a predominant effect on venous vessels. Antianginal agent. The mechanism of action is associated with the release of the active substance nitric oxide in the smooth muscles of blood vessels. Nitric oxide causes activation of guanylate cyclase and increases cGMP levels, which ultimately leads to smooth muscle relaxation. Under the influence of glyceryl trinitrate, arterioles and precapillary sphincters relax to a lesser extent than large arteries and veins. This is partly due to reflex reactions, as well as the less intense formation of nitric oxide from active substance molecules in the walls of arterioles.

The effect of nitroglycerin (glyceryl trinitrate) 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 (decreased OPSS). Promotes the redistribution of coronary blood flow into ischemic subendocardial areas of the myocardium. Increases exercise tolerance in patients with coronary artery disease and angina pectoris. In heart failure, it helps to unload the myocardium mainly by reducing preload. Reduces pressure in the pulmonary circulation.

Pharmacokinetics

After oral administration, it is absorbed from the gastrointestinal tract and undergoes a “first pass” effect through the liver. When administered sublingually, this effect is absent, and therapeutic concentrations in the blood plasma are achieved within a few minutes. Metabolized in the liver with the participation of nitrate reductase. Of the nitroglycerin metabolites, dinitro derivatives can cause pronounced vasodilation; perhaps they determine the therapeutic effect of nitroglycerin (glyceryl trinitrate) when taken orally.

Plasma protein binding is 60%. T1/2 after oral administration - 4 hours, with sublingual administration - 20 minutes, after intravenous administration - 1-4 minutes. It is excreted primarily by the kidneys.

Release form

10 ml - ampoules (10) - cardboard packs.

Dosage

Use sublingually, buccally, orally, cutaneously, intravenously. The dose and treatment regimen are set individually, depending on the indications, the specific clinical situation, and the dosage form used.

Interaction

When used simultaneously with vasodilators, ACE inhibitors, calcium channel blockers, beta-blockers, diuretics, tricyclic antidepressants, MAO inhibitors, ethanol, ethanol-containing drugs, the hypotensive effect of glyceryl trinitrate may be enhanced.

When used simultaneously with beta-blockers and calcium channel blockers, the antianginal effect is enhanced.

With the simultaneous use of drugs with anticholinergic activity (including tricyclic antidepressants, disopyramide), hyposalivation and dry mouth develop.

There is limited evidence that acetylsalicylic acid, used as an analgesic, increases the concentration of nitroglycerin (glyceryl trinitrate) in the blood plasma. This may be accompanied by increased hypotensive effect and headaches.

A number of studies have observed a decrease in the vasodilating effect of nitroglycerin (glyceryl trinitrate) during long-term therapy with acetylsalicylic acid.

It is believed that it is possible to enhance the antiplatelet effect of acetylsalicylic acid with the use of nitroglycerin (glyceryl trinitrate).

When used simultaneously with nitroglycerin, the effect of acetylcholine, histamine, and norepinephrine decreases.

Against the background of intravenous administration of nitroglycerin, the anticoagulant effect of heparin may be reduced.

With simultaneous use, it is possible to increase the bioavailability of dihydroergotamine and reduce the antianginal effect of nitroglycerin (glyceryl trinitrate).

When used simultaneously with novocainamide, the hypotensive effect and the development of collapse may be enhanced.

When used simultaneously with rizatriptan, sumatriptan, the risk of developing coronary artery spasm increases; with sildenafil - the risk of developing severe arterial hypotension and myocardial infarction; with quinidine - orthostatic collapse is possible; with ethanol - severe weakness and dizziness.

Side effects

From the cardiovascular system: dizziness, headache, tachycardia, skin hyperemia, feeling of heat, arterial hypotension; rarely (especially with overdose) - collapse, cyanosis.

From the digestive system: nausea, vomiting.

From the side of the central nervous system: rarely (especially in case of overdose) - anxiety, psychotic reactions.

Allergic reactions: rarely - skin rash, itching.

Local reactions: mild itching, burning, redness of the skin.

Other: methemoglobinemia.

Indications

For sublingual and buccal use: relief and prevention of angina attacks; as an emergency medicine for acute myocardial infarction and acute left ventricular failure at the prehospital stage.

For oral administration: relief and prevention of angina attacks, rehabilitation treatment after myocardial infarction.

For intravenous administration: acute myocardial infarction, incl. complicated by acute left ventricular failure; unstable angina; pulmonary edema.

For cutaneous use: prevention of angina attacks.

Contraindications

Shock, collapse, arterial hypotension (systolic blood pressure<100 мм рт.ст., диастолическое АД<60 мм рт.ст.), острый инфаркт миокарда с выраженной артериальной гипотензией, гипертрофическая обструктивная кардиомиопатия, констриктивный перикардит, тампонада сердца, токсический отек легких, повышение внутричерепного давления (в т.ч. при геморрагическом инсульте, после недавно перенесенной травмы головы), закрытоугольная глаукома с высоким внутриглазным давлением, повышенная чувствительность к нитратам.

Features of application

Use during pregnancy and breastfeeding

The use of nitroglycerin (glyceryl trinitrate) during pregnancy and lactation (breastfeeding) is possible only in cases where the expected benefit to the mother outweighs the potential risk to the fetus or infant.

Use for liver dysfunction

Use with caution in cases of severe liver dysfunction (parenterally).

Use for renal impairment

Use with caution in cases of severe renal impairment (parenteral).

special instructions

With prolonged use, tolerance to the effects of nitrates may develop. To prevent the occurrence of tolerance, it is recommended to observe a 10-12 hour break in their use during each 24-hour cycle.

If an attack of angina occurs during cutaneous use of nitroglycerin (glyceryl trinitrate), it should be stopped by taking glyceryl trinitrate under the tongue.

During the treatment period, avoid drinking alcohol.

Impact on the ability to drive vehicles and operate machinery

Glyceryl trinitrate may reduce the speed of psychomotor reactions, which should be taken into account when driving vehicles or engaging in other potentially hazardous activities.