Nitroglycerin method of application. Indications for use and side effects when taking nitroglycerin

Dosage form:  sublingual tablets Compound:

1 tablet contains:

active substance: nitroglycerin diluted 10% (lactose) in terms of nitroglycerin - 0.5 mg;

Excipients: microcrystalline cellulose - 2.0 mg, potato starch - 4.0 mg, low molecular weight medical polyvinylpyrrolidone - 2.0 mg, colloidal silicon dioxide (aerosil) - 1.0 mg, magnesium stearate - 0.8 mg, aspartame -1.6 mg, crospovidone - 12.0 mg, milk sugar (lactose) - a sufficient amount to obtain a tablet weighing 80.0 mg.

Description:

Tablets are white or white with a creamy or grayish tint, flat-cylindrical, with a chamfer.

Pharmacotherapeutic group:Vasodilating agent - nitrate ATX:  

C.01.D.A.02 Nitroglycerin

Pharmacodynamics:

Venodilator from the group of nitrates. 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. An increase in the concentration of cyclic guanosine monophosphate leads to relaxation of smooth muscle fibers, mainly venules and veins.

It has antianginal and antispasmodic effect, relaxes the smooth muscles of the vascular walls, bronchi, gastrointestinal tract, biliary tract, ureters. Reduces blood flow to the right atrium, helps to reduce pressure in the pulmonary circulation and regression of symptoms in edema of preload, afterload and tension of the walls of the ventricles 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 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 antianginal effect lasts from 30 minutes to 60 minutes.

Pharmacokinetics:

It is quickly and completely absorbed from the surface of the mucous membranes of the oral cavity. When taken under the tongue, the effect of "primary passage" through the liver is excluded. When taking 1 tablet under the tongue, bioavailability is approximately 100%, the time to reach the maximum concentration in the blood is 5 minutes. Has a very large volume of distribution. Communication with blood plasma proteins - 60%. 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. Excreted by the kidneys as metabolites. The total clearance is 25-30 l / min, the half-life is 4-5 minutes.

Indications: Relief of seizures angina pectoris, short-term prevention of angina attacks before physical exertion or emotional stress. Contraindications:

Hypersensitivity to the components of the drug, other nitrates; hypotension with low systolic blood pressure (below 90 mmHg) (may aggravate the condition by causing paradoxical bradycardia and angina attacks), hypertrophic obstructive cardiomyopathy (may increase angina attacks), severe aortic / subaortic stenosis or mitral stenosis, constrictive pericarditis , cardiac tamponade; severe hypovolemia, head injury, conditions with increased intracranial pressure (eg, cerebral hemorrhage; an increase in intracranial pressure has been noted with high doses of nitroglycerin), shock, collapse; simultaneous administration of phosphodiesterase-5 inhibitors (,); severe anemia, phenylketonuria (the drug contains aspartame), lactose intolerance, lactase deficiency, glucose-galactose malabsorption, age up to 18 years.

Carefully:

hemorrhagic stroke; intracranial hypertension; acute myocardial infarction with low filling pressure of the left ventricle (risk of lowering blood pressure and tachycardia, which can increase ischemia), chronic heart failure with low filling pressure of the left ventricle; mild aortic/subaortic stenosis or mitral stenosis; angle-closure glaucoma (risk of increased intraocular pressure); thyrotoxicosis; severe renal failure; liver failure (risk of developing methemoglobinemia); diabetes.

Pregnancy and lactation:

Use during pregnancy is possible only in cases where the expected benefit to the mother outweighs the potential risk to the fetus.

At the time of treatment should be discontinued. lactation.

Dosage and administration:

With angina pectoris (immediately after the onset of anginal pain), place 1 tablet under the tongue until completely resorbed. In some patients with stable angina, the effect comes from a lower dose, so if the pain passes quickly, it is recommended to spit out the rest of the tablet, which has not completely resolved. Usually the effect appears after 0.5-2 minutes, in some cases - 4-5 minutes. In the absence of antianginal action during the first 5 minutes, another tablet should be taken.

The maximum daily dose is 3 mg (6 tablets), but in some cases, depending on the clinical situation, it may be higher.

In the absence of a therapeutic effect after taking 2-3 tablets, it is urgent to call a doctor (the likelihood of developing a myocardial infarction).

The action of nitroglycerin lasts for 30-60 minutes.

When taken under the tongue, tolerance to nitroglycerin rarely develops, but in some patients the dose of the drug has to be gradually increased, bringing it up to 2-3 tablets.

Side effects:

From the side of the cardiovascular system: flushes to the face, palpitations, tachycardia, lowering blood pressure; rarely - orthostatic collapse, cyanosis.

From the side of the central and peripheral nervous system and sensory organs:"nitrate" headache, dizziness, feeling of fullness of the head, weakness; rarely (especially with an overdose) - anxiety, psychotic reactions, lethargy, disorientation.

From the side of the organs of vision: blurred vision, exacerbation of angle-closure glaucoma.

From the digestive system: dryness of the oral mucosa, nausea, vomiting, abdominal pain.

Allergic reactions: rarely - skin rash, itching.

Others: hypothermia, hyperemia of the skin, sensation of heat; rarely - methemoglobinemia.

Overdose:

Symptoms: lowering blood pressure (below 90 mm Hg) with orthostatic dysregulation, reflex tachycardia, headache; asthenia, dizziness, increased drowsiness, feeling of heat, nausea, vomiting may develop; when using high doses - collapse, cyanosis, methemoglobinemia, dyspnea and tachypnea.

Treatment: transfer of the patient to a horizontal position with raising the legs higher head (to increase venous return to the heart), gastric lavage(if with a little time has passed since the moment of ingestion); in severe cases - the use of plasma substitutes, intravenous administration of agonistsα -adrenergic receptors ().

The introduction of epinephrine as a cardiotonic agent should be avoided due to the possibility of enhancing a shock-like reaction.

To eliminate methemoglobinemia, depending on the severity, ascorbic acid is prescribed orally (1 g) or, in the form of sodium salt intravenously, 1% solution of methylthioninium chloride (methylene blue) at a dose of 1-2 mg / kg (up to 50 ml), oxygen therapy ; hemodialysis, blood transfusion.

It is recommended to monitor the concentration of methemoglobin in the blood. Interaction:

Simultaneous use with vasodilators, antihypertensive drugs, angiotensin-converting enzyme inhibitors, beta-blockers, slow calcium channel blockers, procainamide, tricyclic antidepressants, monoamine oxidase inhibitors, diuretics, ethanol enhances the hypotensive effect of nitroglycerin.

A synthetic analogue of the natural coenzyme of nitric oxide synthase, when used simultaneously with nitroglycerin, increases the risk of arterial hypotension.

When taken simultaneously with sildenafil, as well as with other phosphodiesterase-5 inhibitors (, ), a sharp decrease in blood pressure may occur.

With simultaneous use with beta-blockers and blockers of "slow" calcium channels, the antianginal effect of nitroglycerin increases.

With simultaneous use with sympathomimetics, it is possible to reduce the antianginal effect of nitroglycerin and reduce the pressor effect of sympathomimetics, which increases the risk of arterial hypotension.

Against the background of simultaneous administration with quinidine, procainamide, orthostatic collapse may occur.

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

The simultaneous use of nitroglycerin and heparin reduces the effectiveness of the latter, which may require an increase in the dose of heparin (after discontinuation of the drug, a decrease in the dose of heparin may be required).

Simultaneous use with acetylsalicylic acid leads to an increase in the maximum concentration of nitroglycerin andAUC(area under the concentration-time pharmacokinetic curve).

With the simultaneous use of nitroglycerin with rizatriptan or sumatriptan, the risk of developing coronary artery spasm increases, with agents with anticholinergic activity (tricyclic antidepressants, disopyramide), hyposalivation and dry mouth develop.

Nitroglycerin reduces the effectiveness of acetylcholine, histamine, norepinephrine.

Special instructions:

The tablet should not be chewed, as an excess amount of the active substance may enter the systemic circulation through the mucous membrane of the oral cavity.

When a headache or migraine occurs, improvement is achieved by using validol or sublingual menthol drops. Often, only the first doses are poorly tolerated, then the side effects subside.

In acute myocardial infarction or acute heart failure, it should be used only under the condition of careful clinical monitoring of the patient with hemodynamic control.

When 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 in hot weather, as well as increased angina pectoris with a sharp decrease in blood pressure, ischemia up to myocardial infarction (paradoxical nitrate reactions).

During the treatment period, alcohol is not allowed.

To reduce the risk of side effects, care must be taken when used simultaneously with drugs that have pronounced antihypertensive and vasodilating properties; stop drinking alcohol, limit stay in rooms with high ambient temperature (bath, sauna, hot shower), avoid taking several tablets at the same time or sequentially for a short period of time after the first dose.

The risk of developing methemoglobinemia, manifested by cyanosis and the appearance of a brown hue of the blood, increases with prolonged uncontrolled intake of nitroglycerin, taking high doses of the drug by patients with liver failure. In the case of the development of methemoglobinemia, it is urgent to cancel and apply an antidote. If further use of nitrates is necessary, control over the content of methemoglobin is mandatory.

Uncontrolled use of the drug can lead to the development of tolerance, expressed in a decrease in the duration and severity of the effect and the need increasing the dose to achieve a therapeutic effect. After a break in treatmentsensitivity to nitrates is restored. In order to prevent the development of tolerance, it is recommended to observe the daily interval between nitrate intakes (8-12 hours).

1 tablet of Nitroglycerin contains 0.005 XE (bread units), the maximum daily dose is 0.03 XE.

Influence on the ability to drive transport. cf. and fur.:

During the period of treatment, it is necessary to refrain from driving vehicles and engaging in potentially hazardous activities that require an increased concentration of attention and speed of psychomotor reactions.

Release form / dosage:sublingual tablets, 0.5 mg.
Package:

20 tablets in a blister pack made of polyvinyl chloride film and aluminum foil.

40 tablets in glass jars, or in plastic containers for medicines, or in polymer jars.

One blister pack, or one jar, or one container, together with instructions for medical use, is placed in a cardboard pack.

Storage conditions:

Store in a dry, dark place at a temperature of 15 to 25 °C.

Keep out of the reach of children. Best before date:

Do not use after the expiry date stated on the package.

Conditions for dispensing from pharmacies: Over the counter Registration number: LS-002381 Date of registration: 10.10.2011 / 05.02.2018 Expiration date: Perpetual Registration certificate holder:HEALTH PHARMACEUTICAL COMPANY, LLC Ukraine Manufacturer:   Information update date:   12.07.2018 Illustrated Instructions

The use of nitroglycerin.

Ischemic heart disease (CHD): exertional angina (treatment, prevention), unstable angina, Prinzmetal's angina, spasm of the coronary arteries during coronary angiography, acute coronary syndrome, acute myocardial infarction, acute left ventricular failure, chronic heart failure.

It is used to relieve an angio attack-attack of angina pectoris

Nitroglycerine

Contraindications to the use of nitroglycerin.

Severe hypotension, shock, collapse, myocardial infarction with low end-diastolic pressure in the left ventricle and / or severe hypotension (system BP below 100 mm Hg) or collapse, right ventricular infarction, bradycardia less than 50 bpm , primary pulmonary hypertension, cerebral hemorrhage, head trauma, increased intracranial pressure, cerebral ischemia, cardiac tamponade, toxic pulmonary edema, severe aortic stenosis, conditions accompanied by a decrease in end-diastolic pressure in the left ventricle (isolated mitral stenosis, constrictive pericarditis), angle-closure glaucoma, pregnancy, breastfeeding.

Restrictions on the use of nitroglycerin.

Severe cerebral atherosclerosis, anemia, hypertrophic cardiomyopathy (idiopathic hypertrophic subaortic stenosis), advanced age, severe liver and kidney dysfunction, hyperthyroidism. During the period of taking the drug, avoid drinking alcohol.

Side effects when using nitroglycerin.

From the nervous system and sensory organs: headache, dizziness, feeling of fullness of the head, weakness, restlessness, psychotic reactions, blurred vision, exacerbation of glaucoma.
From the side of the cardiovascular system and blood (hematopoiesis, hemostasis): flushing of the face, tachycardia, hypotension, collapse.
From the digestive tract: dry mouth, nausea, vomiting, diarrhea.
On the part of the skin: cyanosis, skin hyperemia.
Allergic reactions: itching and burning, rash.
Other: irritability, visual disturbances, paradoxical reactions.

An overdose of nitroglycerin.

Symptoms: headache, dizziness, feeling of strong pressure in the head, palpitations, nausea and vomiting, cyanosis of the lips, nails or palms, shortness of breath, hypotension, weak rapid pulse, fever, increased intracranial pressure (brain symptoms up to the development of convulsions and coma ), methemoglobinemia.

Treatment of an overdose with nitroglycerin: transferring the patient to a horizontal position (raising the legs above head level to increase venous return to the heart), gastric lavage (if a little time has passed since ingestion), plasma substitutes. To eliminate methemoglobinemia, use oxygen under pressure or a 1% solution of methylthioninium chloride (Methylene blue) at a dose of 1–2 mg/kg, i.v. It is recommended to monitor the concentration of methemoglobin in the blood.

Method of application and dose.

In / in: (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 speed of 0 is reached 02 mg/min (with inefficiency - further increase by 0.01 mg/min).
Sublingual:
nitroglycerin tablets - 0.15-0.5 mg per dose, if necessary, again after 5 minutes; aerosol - for stopping an attack of angina pectoris - 1-2 doses under the tongue by pressing the dosing valve (can be repeated, but not more than 3 doses within 15 minutes). In the case of acute left ventricular failure, 4 or more doses may be used in a short period.
Transdermally:
stick each time on a new skin area and leave for 12–14 hours, after which they are removed to provide a break of 10–12 hours to prevent the development of tolerance.
Inside:
tablets and capsules are taken without chewing or breaking, 2-4 times a day before meals, preferably 30 minutes before exercise, a single dose is 5-13 mg; due to poor bioavailability, a single dose may increase to 19.5 mg.
Subbuccal:
the tablet is placed on the mucous membrane of the oral cavity (behind the cheek) and kept until completely absorbed: 2 mg 3 times a day.

Precautions: In the acute period of myocardial infarction and with the development of acute heart failure, it is prescribed under strict control of hemodynamics. With caution, nitroglycerin is used for aortic and mitral stenosis, in patients with hypovolemia and reduced system. BP (less than 100 mm Hg). With prolonged uncontrolled intake of nitroglycerin, the appointment of high doses to patients with liver failure and children, the risk of methemoglobinemia, manifested by cyanosis and the appearance of a brown tint in the blood, increases. 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.

It is not recommended to take nitroglycerin while drinking alcohol, in rooms with a high ambient temperature, as well as taking several tablets at the same time or sequentially in a short period of time at the first dose.

Do not chew tablets nitroglycerin and capsules in order to stop an angina attack, tk. 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.

Uncontrolled reception nitroglycerin may lead to the development of tolerance, 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 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.

Hypertension leads to the development of myocardial ischemia.

Arterial hypertension (high blood pressure) is a strong catalyst in the development of angina. With high blood pressure, deposits form on the inner walls of the vessels, which narrow the lumen of the vessel, worsening blood flow - oxygen starvation of the body tissues occurs.

When blood circulation is disturbed in the vascular system that feeds the myocardium, anginal attacks occur - myocardial ischemia occurs, angina pectoris develops. There is an imbalance between the need of the myocardium (heart) for oxygen and its delivery, which is provided by the coronary blood flow.

Uncontrolled attacks of angina pectoris (the course of an attack without taking antianginal drugs, without medical assistance) may be the cause myocardial infarction.


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Nitroglycerin has a very fast effect, so it is indispensable in case of sudden attacks of angina pectoris. It dilates blood vessels, including coronary ones, and eliminates pain. In its pure form, this substance is not used for treatment due to explosiveness.

Nitroglycerin was discovered 170 years ago, but then it was not used for therapeutic purposes. There was a proposal to use it as a homeopathic remedy for migraine due to short-term headache attacks after taking the drug, but this idea did not catch on.

Interestingly, Alfred Nobel himself became interested in a new substance and even patented his own method of making explosives from it, having found the possibility of properly handling it. As a result, the industrial production of nitroglycerin as an explosive was started, but Nobel himself denied its antianginal effect, although he suffered from attacks of pain in the heart.

Only after almost 30 years, thanks to the efforts of the medical practitioner W. Merrell, nitroglycerin began to be used as a drug. Merrell not only traced the features of its action and summarized them in his article, but also determined the optimal dosage by dissolving an alcohol solution of the drug in ordinary water. A year later, a solid form of nitroglycerin appeared - the drug was mixed with chocolate, which gave it excellent digestibility.

Since the beginning of the last century, nitroglycerin as a drug began to be produced on an industrial scale, thanks to which angina patients received an excellent inexpensive remedy for attacks of pain in the heart.

Nitroglycerin is considered an organic nitrate, so it would be foolish to deny the possibility of its negative and even toxic effects in large doses. The effect of intoxication and addiction was pronounced in workers of pharmaceutical industries. This prompted scientists to further research, because they had to determine exactly how the substance works in the body, what are its side effects and how to use it correctly.

By the end of the twentieth century, the mechanism of action of nitroglycerin was revealed - scientists found that the drug owes its vasodilating effect to nitric oxide. For establishing the mechanism of action of nitroglycerin, the researchers received the Nobel Prize.

For more than 150 years since its discovery, nitroglycerin has not lost its relevance. On the contrary, it continues to be one of the main means of stopping episodes of angina pectoris due to its rapid action and proven high efficiency.

Pharmacological properties of nitroglycerin

Patients suffering from a variety of cardiac pathologies know that nitroglycerin helps to quickly and effectively relieve heart pain, relieve an angina attack, improve the condition after a heart attack, so it usually prescribed for angina pectoris, regardless of its variety.

Nitroglycerin owes its ability to dilate blood vessels to its constituent nitrogen, which, when released and combined with oxygen, is converted into NO - nitric oxide, a compound that normally promotes relaxation of the vascular walls due to the activation of guanylate cyclase.

An increase in the content of guanylate cyclase causes relaxation of muscle fibers in the vascular walls, their removal, as well as relaxation of the muscles of the bronchi, digestive system, ureters, and bile ducts.

Expansion of peripheral venous vessels with intravenous use of nitroglycerin reduces the blood load on the heart. Reduced blood flow through the vena cava causes a decrease in pressure in the right heart and pulmonary circulation, so pulmonary edema is considered one of the indications for the use of nitroglycerin.

In conditions of a reduced load on the heart, a decrease in its filling with blood and pressure in the chambers, the need for oxygen in the heart muscle also decreases, due to which an analgesic effect is achieved in angina pectoris.

The vasodilating effect of nitroglycerin allows it to stop heart pain, but side effects are also associated with it.. For example, dilatation (expansion) of cerebral vessels causes headaches, dizziness, and even loss of consciousness after taking the drug.

With prolonged use of prolonged forms of nitroglycerin, the formation of drug resistance is possible and, as a result, a decrease in the effectiveness of the drug. To prevent this, experts recommend taking breaks for 8-12 hours between taking the drug.

The rate of action of nitroglycerin depends on the form in which the patient consumes it. When taking the drug under the tongue, the analgesic effect is noticeable after a minute and a half and lasts up to 5 hours. The action of the ointment comes a little later - after 15 minutes, maximum - an hour from the moment of administration, the action lasts 3-4 hours.

There are special patches with nitroglycerin that are fixed on the skin and provide a gradual effect of the drug over a long period of time. During the day, about a fifth of nitroglycerin is absorbed into the blood from such a patch. The amount of medicine obtained from the patch depends on its area.

It is believed that nitroglycerin enters the bloodstream most quickly through the mucous membranes and skin, as well as intravenously, oral bioavailability is significantly inferior to transdermal and buccal forms of the drug, since most of it passes through the liver and is destroyed there.

The sublingual route of administration of nitroglycerin is considered attractive - under the tongue, when the entire dose of the drug is absorbed directly into the bloodstream, and after five minutes its amount in the blood becomes maximum. Metabolism of nitroglycerin occurs in the liver, where it breaks down to end products excreted by the kidneys.

Indications and contraindications for the appointment of nitroglycerin

Nitroglycerin is used very widely. Almost every elderly patient suffering from periodic pain in the heart, has with him a tablet or spray of this drug, which can be taken as soon as an attack is felt. The effect comes very quickly, the pain is removed, the work of the heart is getting better. The main reason for the use of nitroglycerin is coronary heart disease. The drug is used for:

  • Paroxysms of angina pectoris (pain in the heart) and for their prevention;
  • Recovery in the postinfarction period.

Intravenous administration of nitroglycerin is necessary in the case of:

  1. Acute;
  2. Angina resistant to other types of treatment;
  3. Postinfarction and unstable angina;
  4. Acute left ventricular failure with pulmonary edema;
  5. Controlled hypotension, which is adjusted during surgical interventions to reduce blood loss;
  6. Thrombosis of the central retinal artery.

In addition to cardiac pathology, indications for the use of nitroglycerin can be acute pancreatitis, attacks of biliary colic, esophageal and intestinal dyskinesia, gallbladder motility disorders.

There are also contraindications to taking nitroglycerin. Among them:

  • Individual intolerance;
  • Simultaneous administration of phosphodiesterase inhibitors (sildenafil);
  • heavy;
  • Intolerance to lactose, galactose caused by hereditary causes;
  • Sticky.

Prescribe nitroglycerin with caution should:

  1. Patients with increased and intraocular pressure;
  2. With congestion, when the pressure in the left ventricle is very low;
  3. At ;
  4. Hyperthyroidism;
  5. Pathology of the liver and kidneys;
  6. Tendency to hypotension.

It is better to refrain from taking nitroglycerin for pregnant women and nursing mothers. The safety of its use in children and adolescents has not been established, so nitroglycerin is not usually used before the age of 18.

The listed contraindications apply to all dosage forms of nitroglycerin. In addition, prolonged preparations are contraindicated in people with increased intestinal and gastric motility and malabsorption, and intravenous administration of nitroglycerin is prohibited in case of severe shock, pericardial hemotamponade and pericarditis, toxic pulmonary edema.

Instructions for the use of nitroglycerin carry a large amount of information regarding not only the mechanism of action, but also possible adverse reactions, complications during treatment, drug interactions that the patient should be aware of, therefore, after prescribing this medication, it is better to immediately read the instructions and follow the recommendations of your doctor. doctor.

Adverse reactions from the use of nitroglycerin occur on the part of the cardiovascular, nervous system, and digestive organs. Often, while taking nitroglycerin, patients complain of the appearance of dizziness, headaches, tachycardia, which is associated with rapid vasodilation. These effects develop most frequently and usually resolve within 10-20 minutes of ingestion. To restore the blood supply to the cerebral vessels and eliminate headaches, it is better to take a horizontal position, lowering your head and slightly raising your legs. Nausea, dry mouth, dyspeptic disorders are less common.

With an overdose of the drug, symptoms from the nervous system appear: the patient is excited, disoriented, may be inhibited, in rare cases it comes to psychosis. Severe intoxication with nitroglycerin is accompanied by collapse, cyanosis of the skin, respiratory disorders, methemoglobin appears in the blood, provoking hypoxia.

The likelihood of such effects dictates the need for strict adherence to the prescribed dosage and regimen for the use of nitroglycerin. Very rare, but still not excluded, allergic reactions and local negative manifestations - itching, burning, redness of the skin, dermatitis.

If adverse reactions have developed with intravenous infusions, then they are immediately stopped. In the case of using skin products, they should be removed (ointments, patches). Given the expansion of cerebral vessels and possible fainting, the patient is laid with raised legs and slightly lowered head. Usually normal blood pressure is restored within 15-20 minutes.

With methemoglobinemia caused by an overdose of nitroglycerin, ascorbic acid, oxygen therapy are indicated; in acute renal failure against this background, hemodialysis is necessary. In rare cases, doctors are forced to resort to blood transfusions.

Dosage forms and features of taking nitroglycerin

Nitroglycerin can be administered intravenously or in the form of tablets, spray, patches. For intravenous administration, a solution of the drug is used. It is considered very effective to administer the drug through the skin or mucous membrane of the gums. To do this, use drops, tablets, spray, which are taken under the tongue.

Nitroglycerin should be taken as soon as pain appears, or even as a preventive measure if the patient is going to exercise or perform activities that provoke pain in the heart. In the first case, the number of tablets can reach up to three, in the second it is usually enough to take one single one. The onset of the effect is judged by the reduction and disappearance of pain, control of blood pressure and pulse is mandatory.

The modern pharmacological market offers a wide selection of both forms and names of nitrate-containing drugs. Analogues of conventional nitroglycerin in tablets - nitrocardin, nitrocor, prolonged action nitrates - sustak mite, sustak forte, nitrogranulong. A common aerosol containing nitroglycerin is nitromint, a spray is called nitrospray, plates for buccal use are trinitrolong, patches are deponit 10 and nitropercuten TTS.

To absorb the drug through the vessels of the skin, a special patch impregnated with nitroglycerin is prescribed. Tablets can be sublingual, acting fairly quickly, but prolonged forms are also available, designed for a long-term effect.

Dosage, dosage form and regimen are determined by the pathology for which the cardiologist prescribes nitroglycerin - angina pectoris, heart attack, hypertensive crisis, etc.

taking nitroglycerin under the tongue

With an attack of heart pain, take a tablet or capsule of nitroglycerin under the tongue until it dissolves, the average dose for a pain attack is 0.5-1 milligram. If the first tablet does not work, the next one is recommended to be taken no earlier than half an hour later. If the pain has passed, and the tablet is still not absorbed, it can and even needs to be removed from the oral cavity.

In most patients, the pain is removed already in the first few minutes after taking nitroglycerin, but if after 5 minutes the heart still hurts, then you can add half a milligram of the drug more. The maximum number of tablets per attack is up to three. If they do not work, you need to immediately call an ambulance, because the pain may indicate a myocardial infarction.

With frequently recurring episodes of angina pectoris, it is more expedient to prescribe prolonged forms of nitroglycerin, but if an acute attack develops against this background, then the patient needs to additionally take nitroglycerin under the tongue.

Nitrates for prophylactic purposes are prescribed in the form of long-acting tablets (prolonged). They are taken orally with water, before meals. The dosage of nitroglycerin is 2.9 mg, up to two tablets per dose, the frequency of use is 3-4 times a day. In severe pathology, the dosage of the drug can be increased to 5.2 mg.

Long-acting nitrates act more slowly, most of them are inactivated in the liver, so the effectiveness is lower than that of "sublingual" drugs. With regular use, the maximum number of tablets per dose should not be more than two.

Films or drops that penetrate the oral mucosa are much more effective. Drops are instilled under the tongue, the film is glued to the gum. These funds are indicated both for the elimination of a painful attack and for the prevention of angina pectoris (during physical activity, for example).

Transdermal patches with nitroglycerin provide a uniform and long-term flow of the drug into the bloodstream through the skin. They are indicated for patients with chronic circulatory failure, after a heart attack. It is advisable to start treatment with them in a hospital setting, and when the maximum effective dose is reached, the patient is sent home.

In addition to patches, the penetration of the drug through the skin is achieved by using an ointment, which is applied to an area of ​​\u200b\u200bthe body devoid of hair and the possibility of friction with clothing.

nitroglycerin spray

Spray and aerosols are popular and convenient forms of nitroglycerin administration. They are used for attacks of pain in the heart, as well as for incipient or developed pulmonary edema. In the sitting position, the patient needs to make 1-2 clicks on the vial dispenser, while holding his breath. After the drug enters the oral cavity, the effect occurs within a few minutes.

The maximum dose of a spray or aerosol for a painful attack is 3 clicks, for pulmonary edema - up to four. To prevent an attack of pain before exercise, the patient can take a single dose of the drug.

Intravenous administration of nitroglycerin is indicated for myocardial infarction and other severe forms of coronary heart disease. It is important to carefully calculate the rate of administration of the drug, otherwise side effects cannot be avoided. In the case of using a special dispenser, it is possible to use even undiluted nitroglycerin, because the device itself will calculate at what intervals and in what quantity it should be administered to the patient. When using a conventional dropper, the doctor calculates the number of drops per unit of time.

Treatment by intravenous infusion can be carried out for 2-3 days, it is not forbidden to re-administer nitroglycerin if necessary. During the introduction, the doctor must monitor the level of blood pressure in order to prevent severe hypotension.

Often, nitroglycerin is taken not only for angina attacks, but also for high blood pressure. in combination with others. This is especially justified with chest pain and against the background. The dosage of the drug is the same as for angina pectoris - up to three tablets with an interval of 5-10 minutes. If the pain does not go away, the pressure continues to remain high, it is necessary to immediately call an ambulance team.

Precautionary measures

A patient who is indicated for nitroglycerin tells the attending physician in detail about all the drugs he takes in order to avoid unwanted interactions. Simultaneous administration of nitroglycerin and other vasodilators, some groups of antidepressants, increases the hypotensive effect of nitroglycerin.

Nitroglycerin and alcohol are also incompatible things due to the risk of severe hypotension, therefore, the use of any alcohol-containing beverages must be categorically abandoned, especially since heart problems, which serve as an indication for taking nitroglycerin, in themselves do not go well with drinking alcohol.

Hot rooms and high ambient temperatures contribute to the expansion of peripheral vessels, so taking nitroglycerin in such conditions may be accompanied by hypotension.

Tableted nitroglycerin does not need to be chewed, since the sudden penetration into the bloodstream at once of the entire dose can provoke a severe headache. To prevent this effect, you can take simultaneously validol, menthol under the tongue.

Patients with acute cardiac pathology usually need the introduction of heparin. In this case, it is worth remembering that nitroglycerin reduces the blood-thinning effect of heparin, therefore, if the doctor is forced to prescribe them at the same time, he will strictly control hemostasis.

Preparations of nitroglycerin in the form of buccal plates should not be used in case of stomatitis, periodontitis, the presence of removable dentures, as these circumstances complicate the absorption of the active substance.

Uncontrolled, long-term use of nitrates without interruption creates the prerequisites for the formation of drug resistance. It is especially likely when using a patch or ointment, when the drug is actually present in the blood all the time. Drug resistance makes treatment ineffective, requiring an increase in the dose of the drug taken. To avoid such negative moments, doctors recommend taking breaks every day - removing the patch at night, for example.

It is worth recalling once again that nitroglycerin in any form should be prescribed by a specialist, it can be taken on its own only if an accurate diagnosis and cause of chest pain is established, and a cardiologist or therapist has already prescribed a specific dosage and dosage form. At the same time, each patient is warned about the maximum amount of the drug at a time, upon reaching which, if there is no effect, you should immediately call a doctor.

Video: nitroglycerin in the program “Live Healthy”

Video: what is the danger of nitroglycerin

An old friend is better than two new ones. This saying perfectly illustrates the purpose of Nitroglycerin. Despite the development of pharmacology, this drug remains the leading one in the treatment. So, let's talk about the indications for the use of Nitroglycerin, dosage, prices in pharmacies, instructions and reviews about the medicine.

Features of the drug

Nitroglycerin has a rich history and has been used for a long time. The drug dilates blood vessels, mainly of the brain and coronary, and also relaxes the muscles of the gastrointestinal tract, biliary tract and some other organs. Nitroglycerin also reduces venous blood return, reduces myocardial oxygen demand.

Compound

The main active ingredient of the drug is nitroglycerin, and one tablet contains 0.5 mg. The remaining substances contained are auxiliary:

  1. crospovidone CL;
  2. macrogol 6000;
  3. lactose;
  4. povidone 25;

The tablet contains no other substances. The next section will tell about the release forms, as well as the prices for spray, tablets and other forms of Nitroglycerin.

Dosage forms

Today in pharmacies you can find Nitroglycerin in various forms. For ease of perception, they are all placed in the table:

FormQty
active ingredient in mg/l and mg
Approximate price, rub.
Concentrate for solution for injection1 20
Spray0,4 100
Films1 and 2no data
Drops (under the tongue)10 50
Capsules (under the tongue)0.5 and 130
Tablets (under the tongue)0,5 50
Prolonged release tablets2,6 80
Aerosol0,4 80
Therapeutic system transdermal37,4 1900

pharmachologic effect

Nitroglycerin has a vasodilating peripheral, that is, a vasodilating effect. Let's now talk about the mechanism of action of Nitroglycerin.

Pharmacodynamics

Nitroglycerin is a vasodilator that specifically affects the veins. For the most part, the work of the drug is based on the reduction of preload and afterload, which reduces the need for oxygen in the myocardium. Nitroglycerin also inhibits the effect on sympathetic vascular tone, which inhibits the formation of pain. Another effect of the drug is based on the expansion of the meningeal vessels, which can lead to headaches.

When applied under the tongue, an angina attack stops within 5 minutes, and the hemodynamic effect persists for an hour.

The duration of action of Nitroglycerin will be discussed below.

Pharmacokinetics

The advantage of Nitroglycerin is that it is completely absorbed by the body from the mucous membranes.

  • When taking sublingual forms, the drug immediately enters the bloodstream.
  • When taken under the tongue at a minimum dosage of 0.5 mg, bioavailability reaches 100%, and Cmax can be determined after 5 minutes.

Studies show that the protein binding of nitroglycerin reaches 60%.

Indications

Various forms may have extended indications, however, in most cases they are limited to the relief of angina attacks. Nitroglycerin can also be prescribed for dyskinesia of the biliary tract and retinal artery, left ventricular failure, for example, with.

It is strictly forbidden to give Nitroglycerin to children. During pregnancy, taking the drug is possible only if the intended benefit outweighs the risk to the fetus. Nitroglycerin has been rated fetal exposure category C by the FDA. The tablets should not be taken while breastfeeding.

Instructions for use

The instruction largely depends on the dosage form of the drug. At this time, tablets and capsules are most often used, less often - an alcohol solution, each of the products is sublingual:

  • Solution 1%. 1-2 cap. under the tongue or 2-3 drops. on a piece of sugar and also under the tongue until completely absorbed. The highest dose of Nitroglycerin - 4 drops. (one-time) and 16 cap. (daily).
  • Pills. Half or a whole under the tongue, hold until dissolved. The highest dose is 1.5 tab. (one-time) and 6 tab. (daily).
  • Capsules. 1 under the tongue, you can pre-bite to accelerate the effect of taking Nitroglycerin.

Taking the drug depends on the appearance and strength of angina attacks, that is, take it with each attack. When stopping seizures, long-acting tablets are often prescribed.

Intravenous nitroglycerin is prescribed during an ambulance. Preliminary give 1-2 tab. under the tongue every 10 minutes.

Elena Malysheva in her video talks about the features of the correct intake of Nitroglycerin:

Contraindications

Nitroglycerin is contraindicated in people with:

  1. hypersensitivity to nitrates;
    • Nitroglycerin does not affect the absorption of drugs into the blood, however, it is recommended to stop drinking Viagra while taking it.
    • With caution, take Nitroglycerin with renal and hepatic insufficiency, since there is a high risk of developing methemoglobinemia.

    Side effects of Nitroglycerin

    The most common side effects that occur when taking Nitroglycerin are dizziness, pain in the abdomen and head, and. Also, side effects include:

    1. hyperemia of the skin;
    2. temperature increase;
    3. nausea;
    4. vomiting;
    5. anxiety;
    6. inhibition of reactions;
    7. disorientation;
    8. allergic reactions;

    Extremely rarely, with an overdose, orthostatic collapse and cyanosis may occur.

    special instructions

    As with other nitrates, long-term use of nitroglycerin causes resistance to its action, which leads to the need to increase the dosage or frequency of administration. This requires careful monitoring of doses, their variable increase and periodic withdrawal.

    Nitroglycerin is a drug that contains an ester of glycerol and a nitric acid compound. For 150 years, this drug has been used to quickly get rid of pain in the heart.

    A wide range of indications allows the use of this drug for the treatment of cardiac patients. Nitroglycerin has antispasmodic and vasodilating properties. According to numerous reviews, this effective drug has a low price, so everyone can afford it.

    In contact with

    The composition of Nitroglycerin and the principle of action

    Release the drug in three dosage forms:

    • pills;
    • spray;
    • patches.

    The composition of Nitroglycerin tablets includes the active ingredient nitroglycerin, as well as additional components: crospovidone CL, lactose, povidone 25, macrogol 6000.

    The solution consists of the active component of nitroglycerin and such additional components as dextrose, sodium chloride, potassium dihydrogen phosphate, water for injection.

    The composition of the spray includes the active component nitroglycerin and an additional component ethanol 95%.

    Medicines such as nitroglycerin The mechanism of action is as follows:

    Indications and contraindications for use

    Nitroglycerin is a very popular drug., which is often used by older people suffering from periodic pain in the heart. It must be taken immediately when an attack occurs. As evidenced by numerous reviews, the effect is observed almost immediately, the pain is removed and the work of the heart is improved. Ischemic heart disease most often causes the appointment of Nitroglycerin.

    Indications for the use of this drug are also:

    • paroxysmal angina (pain in the heart);
    • recovery after a heart attack.

    According to the instructions for use, Nitroglycerin is administered intravenously in the following cases:

    • acute myocardial infarction;
    • thrombosis of the central retinal artery;
    • angina resistant to other treatments;
    • acute left ventricular failure with pulmonary edema;
    • postinfarction and unstable angina.

    In addition to heart disease, the drug is indicated for acute pancreatitis, dysmotility of the gallbladder, dyskinesia of the intestine and esophagus, during attacks of biliary colic.

    The instructions for use list contraindications to the use of nitroglycerin. These include:

    • individual intolerance;
    • severe hypotension;
    • adhesive pericarditis;
    • hemotamponade of the heart;
    • intolerance to galactose, lactose, which is caused by hereditary causes.

    Nitroglycerin should be taken with caution in the following cases:

    The use of nitroglycerin should be avoided pregnant and lactating women. Since its safety for children and adolescents has not been established, the drug is not prescribed to patients under 18 years of age.

    All of these contraindications apply to all dosage forms of Nitroglycerin. In addition, prolonged drugs are prohibited for people who have increased intestinal and gastric motility and absorption disorders, and intravenous administration of the drug is contraindicated in severe atherosclerosis, traumatic brain injury, toxic pulmonary edema, pericardial hemotamponade, and shocks.

    The instructions for use contain a large amount of information, which concerns not only the mechanism of action, but also possible side effects, complications, and drug interactions.

    Side effects

    In numerous reviews of this drug, it is noted that it has side effects on the part of the digestive system, the nervous, and the cardiovascular system. Quite often, patients taking Nitroglycerin complain of headaches, dizziness, tachycardia, and this is due to the rapid expansion of blood vessels. Such side effects develop most often and disappear after 10 to 20 minutes. To get rid of a headache and restore the blood supply to the cerebral vessels, you should take a horizontal position, lower your head, and slightly raise your legs.

    Much less often side effects are dry mouth, nausea, dyspeptic disorders. In case of an overdose, symptoms from the nervous system may appear: the patient is disoriented, agitated or inhibited, sometimes psychosis occurs. Severe intoxication with the drug is accompanied by respiratory disorders, cyanosis of the skin, collapse, methemoglobin is found in the blood, which provokes hypoxia. Very rarely, local negative manifestations and allergic reactions occur - burning, itching, dermatitis, redness of the skin.

    If side effects have developed with intravenous infusions, then they are immediately stopped. Given that the cerebral vessels have expanded and fainting may occur, the patient is placed with his head slightly lowered and his legs raised. Blood pressure is usually restored after 15 to 20 minutes.

    With methemoglobinemia, which develops as a result of an overdose of Nitroglycerin, oxygen therapy, ascorbic acid are indicated. Very rarely, doctors resort to blood transfusions.

    Features of taking dosage forms

    Nitroglycerin is prescribed both intravenously and in the form of tablets, sprays, patches. It is necessary to take the drug immediately when pain occurs. The fact that the remedy has worked is judged by the disappearance of pain and blood pressure and pulse are necessarily measured.

    Pills

    If you have a heart attack, then the tablet is placed under the tongue until it dissolves. The usual dose is 0.5 - 1 mg. If the pain has not gone away, then after 5 minutes it is allowed to take another 0.5 mg. A second dose is recommended after 30 minutes. If a positive result has come, and the tablet has not had time to dissolve, it must be removed from the mouth. With one attack, it is allowed to take no more than 3 pieces. If the effect is not observed, then, most likely, a heart attack has developed and an urgent need to seek medical help.

    For prophylactic purposes, Nitroglycerin is prescribed in the form of long-acting tablets. They should be taken orally before meals. The dosage of the drug in this case is 2.9 mg and you need to take the tablets 3-4 times a day. In severe pathology, the dosage can be increased to 5.2 mg.

    plasters

    Transdermal patches with nitroglycerin guarantee a long and uniform flow of the drug into the bloodstream through the skin. They are intended for patients with circulatory failure that developed after a heart attack. It is advisable to start treatment with patches in a hospital setting, and when the maximum dose is reached, the patient is sent home.

    Spray

    This is a very popular and convenient form of Nitroglycerin. The spray is intended for attacks of pain in the heart, as well as for incipient pulmonary edema. The patient in a sitting position should hold his breath and press the vial dispenser 1-2 times. The effect comes in a few minutes. With pain syndrome, the maximum dose of the spray is three clicks, and with pulmonary edema - four.

    Intravenous administration

    This way indicated for myocardial infarction, as well as in other severe forms of coronary heart disease. It is necessary to correctly calculate the rate of administration of the drug, as side effects may occur. If a special dispenser is used, then even undiluted nitroglycerin can be used, because the device itself will calculate how much and at what intervals to administer it to the patient. When using a dropper, the doctor calculates the number of drops per unit time.

    Treatment with intravenous administration should be carried out within 2 to 3 days. If there is such a need, then you can re-enter the medicine. To avoid severe hypotension, the doctor must monitor the level of blood pressure during the administration of Nitroglycerin.

    Analogues and price

    If the pharmacy does not have Nitroglycerin or, as prescribed by a doctor, it is allowed to use a drug that is similar in composition and pharmacological effect . Analogues of Nitroglycerin also qualitatively relieve an acute condition and help in the long-term treatment of pathology. These include:

    • Nitrocore;
    • Nitrogranulong;
    • Dikor Long;
    • Isodinit.

    The price of Nitroglycerin tablets is affordable for everyone and is about 40 rubles. But Nitroglycerin in ampoules for intravenous administration is much more expensive and averages 420 rubles.