In many home medicine kits, a drug such as Nitroglycerin can be found as a heart remedy. The pharmacological group of this medicine is named after the chemical element - nitrogen. Rather, its compounds with glycerol ester. About how this substance works, in which cases the drug is prescribed for use, the pharmacological forms produced, contraindications and side effects of Nitroglycerin will be described below.
Nitrogen and bioprocesses
Cardiovascular disease persecutes people of different sex and age. Unfortunately, even young people suffer from insufficiency in the functionality of the heart. and already traditionally drugs with nitroglycerin are considered almost the main helpers in such health problems as angina pectoris, palpitations, pain in the heart. Why do preparations based on nitrogen and nitroglycerin in particular help to cope with rather serious pathological processes?
Nitrogen is the most common substance in the atmosphere of our planet - its concentration is 80% in the air that all living things breathe. It is not surprising that this chemical element, or rather, its compounds are so important for good human health. Compounds and nitrogen derivatives are part of amino acids, vitamins, nucleotides, neurotransmitters, hormones, hemoglobin and other biologically significant substances produced in humans or animals. Compounds of the seventh chemical element of the Periodic Table of D. I. Mendeleev carry out very significant functions. It:
- building material of biologically significant components;
- hemoglobin vehicle for oxygen transfer through tissues and organs;
- excellent vasodilator.
It is noteworthy that nitrogen does not need nitrogen in its pure form, but its derivatives and compounds are vital components. But in addition to the implementation of indispensable functionality inside tissues and organs, nitrogen compounds are also used as medications. Such a medicine is Nitroglycerin, the trade name of which is given by its active component.
Pharmacological group
Painful sensations in the region of the heart, heart failure, and other ailments that serve as a sign of serious disorders in the body may appear suddenly or be expected by the established diagnosis. No one is safe from the appearance of such problems, especially people of middle and older age. For many of them, it becomes a vital necessity to always have the drug Nitroglycerin at hand. The pharmacological group of this medicine is determined by its main component - "Nitrates and nitrate-like agents." They are widely used as antianginal drugs that help a person suffering from coronary heart disease due to the ability of nitrates to increase the amount of nitric oxide acting as an endothelial relaxer.
Substance features
Treatment with Nitroglycerin, like any other drug, should be carried out only on the recommendation of a specialist who observes the patient. After all, the active substance in the drug is quite unusual for medicine. Nitroglycerin, in addition to its vasodilating properties, has another feature - it is an explosive. Naturally, it is not able to explode when taken orally as a medicine, but under certain conditions it is nitroglycerin that acts as the main constituent of dynamite.
At its core, nitroglycerin is a glycerol ester in tandem with nitric acid. Under ordinary conditions, it is similar in consistency to liquid oil, has no color, that is, is completely transparent, and has the properties of a liquid prone to overcooling, not volatile. Its pyrotechnic properties are widely used in certain human activities. Nitroglycerin was also widely used in medicine, because Nitroglycerin is a drug that can be found in almost any home medicine cabinet as a cardiac, vasodilator.
In what forms is the medicine available?
Many drugs with the same name can be seen in pharmacies in different dosage forms, with different contents of active ingredients. This is noted by both specialists and patients as a huge plus, because in each specific situation the patient needs to use this or that drug in not only a different physical form, but also a different amount of working substance.
For the antianginal drug Nitroglycerin, the release form and dosage will be as follows:
- sublingual, that is, sublingual tablets, each containing 0.5 mg of the active substance, packaged in blisters, boxes or plastic jars;
- solution for infusion, in which 5% of the composition of the drug;
- an oil solution of nitroglycerin in gelatin capsules - 0.5 mg of the working component;
- sublingual spray, in a single injection dose contains 0.4 mg of nitroglycerin;
- films for gluing on the gum in two versions - 1 or 2 mg of the working substance.
In what form to use this medicine, the attending physician must decide with the patient, choosing the optimal form and dosage.
How do nitrogen compounds work?
Very often people hear that with heart pain it is best to take a tablet with nitroglycerin. And therefore the question: "What helps" Nitroglycerin "(tablets)?" arises by itself. First you need to find out how this substance works, and therefore medicines based on it.
In medical practice, nitrate-containing drugs are used as vaso-and coronary dilators and antianginal agents. This action is due to the work of nitroglycerin, which, undergoing biochemical processes in the human body, potentiates the activation of guanylate cyclase and an increase in the content of cyclic guanosine monophosphate in smooth muscle cells by increasing the number of free radicals of nitric oxide (NO). As a result of the work of nitroglycerin metabolites, mainly venous vessels expand, which contributes to the deposition (accumulation) of blood in the venous system and a decrease in venous return. This, in turn, allows to reduce the preload of the heart and the final diastolic fullness of the left ventricle.
Also, nitroglycerin performs systemic arterial vasodilation, that is, it expands large arteries, which is accompanied by a decrease in the total peripheral vascular resistance and blood pressure - the so-called afterload. Reducing pre- and afterload on the heart can significantly reduce the need for myocardium in oxygen.
This medicinal substance performs the following functionality:
- reduces venous pressure - central;
- slightly increases the heart rate;
- lowers the pressure of jamming created in pulmonary capillaries;
- reduces the resistance of coronary arteries.
Nitroglycerin for pain in the heart is able to normalize cardiac blood flow in cases not associated with an excessive decrease in systemic blood pressure, as well as a significant increase in heart rate. In this case, the effect of the drug can provoke a deterioration in coronary blood flow.
The effect of nitroglycerin on coronary blood flow is carried out through:
- expansion of large epicardial parts of the coronary arteries;
- increase in pressure gradient at the site of atherosclerotic narrowing of the coronary vessel;
- ensuring perfusion even in the case of almost subtotal stenosis;
- collateral activation;
- differentiation of coronary blood flow in favor of ischemic areas, especially subendocardial departments.
As an aid during ischemic hypokinesia of some sections of the myocardium, the drug restores local contractility. It also inhibits the pathological rigidity of the myocardium, which helps prevent the development of fatal arrhythmias accompanying myocardial infarction. Preparations with nitroglycerin weaken postinfarction remodeling of the left ventricle. they also reduce the ability to aggregate platelets and their adhesion to the vascular endothelium. Nitroglycerin increases the threshold for the development of myocardial ischemia.
For patients with a diagnosed heart failure and angina pectoris, as well as potentially having these health problems, nitro compounds can increase cardiac output and increase exercise tolerance. Nitroglycerin helps reduce the severity and frequency of attacks of coronary heart disease and significantly reduces the amount of mitral regurgitation.
The drug Nitroglycerin, whose pharmacological group is defined as a vasodilator, inhibits the sympathetic tone of blood vessels by inhibiting the vascular component of the formation of pain. He also takes an active part in electrolyte metabolic and energy processes due to the normalization of the ratio of oxidized and reduced forms of nicotinamide coenzymes, the activity of NAD-dependent dehydrogenases. The drug at the nitro compound helps release catecholamines in the brain and heart, has an indirect sympathomimetic effect on the myocardium, modulates the conformation of the troponin-tropomyosin complex.
In addition to the positive effect of nitroglycerin, its negative effects have been identified that can occur under certain circumstances:
- activates the transition of hemoglobin to methemoglobin;
- deterioration of oxygen transport;
- the appearance of a headache against the background of the expansion of meningeal vessels;
- relaxes the smooth muscles of the intestines, bronchi, stomach, esophagus, bile ducts, as well as the organs of the genitourinary tract, which can cause changes in the functionality of these organs.
Such an extensive effect of Nitroglycerin is due to the presence of a nitrogen element in its composition, which plays a significant role in many biological processes.
What is the path of the drug in the human body?
Quite often found in many home medicine chests, the drug is Nitroglycerin. The pharmacological group of this drug is vasodilators, antianginal drugs and coronary dilators. This substance is available in a fairly wide range of dosage forms, which allows each patient to choose the right one.
The drug is very quickly and completely absorbed into the bloodstream through the mucous membranes or skin. When taking the drug orally, nitroglycerin gets the effect of the first passage, as a result of which it is largely destroyed, undergoing biotransformation in the liver. In smooth muscle cells, metabolites form NO.
The use of the drug sublingual, in the form of a spray on the mucous membranes of the mouth, gum patches or in the form of injections, allows the active substance to be delivered immediately to the systemic circulation, which deprives it of hepatic degradation and retains a large amount of active substance.
Metabolic processes this drug component passes twice:
- di- and mononitrates;
- glycerol.
Sublingual administration of the drug gives the maximum concentration of the main metabolites, and this is about 0.3 ng / ml, in 2-2.5 minutes. The half-life of nitroglycerin will be from 1 to 4 minutes, and metabolites - 7 minutes.
If you use the medicine in the form of an aerosol sprayed into the oral cavity, then the maximum concentration of its metabolites will be about 15 ng / ml in almost 5 minutes. In this case, the relative bioavailability is quite large - 76%, and the half-life is significantly increased - 20 minutes.
The smallest bioavailability of the drug is recorded when taken orally - only 10-15%. The maximum concentration of C max metabolites is 0.1-0.2 ng / ml and is achieved half an hour after taking the drug by mouth - orally. The elimination half-life designated by T 1/2 , metabolites is fixed in 4 hours.
Intravenous administration of nitroglycerin gives a half-life of T 1/2 of 1-3 minutes, and the total total clearance is 30–78 l / min. If the patient suffers from heart failure, then the above indicators change towards prolongation.
Nitroglycerin binds to plasma blood proteins by 60%. Metabolites are excreted mainly in the urine through the kidneys, although some of them are excreted by the lungs along with exhaled air.
With angina pectoris, it is preferable to use sublingual and buccal forms of the drug. In this case, the attack stops after 1.5 minutes. In this case, the hemodynamic effect lasts up to 30 minutes, and the anti-ischemic effect of the drug lasts up to 5 hours.
Small doses of the drug in 2.5 mg of the working substance make it possible to obtain a hemodynamic effect for half an hour, but large doses, called forts in pharmacology, give a long-lasting effect - up to 5-6 hours. The use of external agents with nitroglycerin allows you to provide antianginal action after 15-60 minutes and its 3-4 hour duration. Transdermal forms act in half an hour and keep it up to about 10 hours.
In what cases is a medicine prescribed?
Antianginal drugs of the nitrate group, and this is primarily nitroglycerin in various pharmaceutical forms, have a fairly extensive list of recommendations for use:
- arterial hypotension controlled during surgical procedures;
- vasospastic angina pectoris, the so-called Prinzmetal angina pectoris ;
- esophagus dyskinesia;
- biliary colic;
- unstable angina pectoris;
- occlusion (sudden closure) of the central artery of the eye retina;
- acute left ventricular failure as a symptom of cardiac asthma, interstitial and alveolar pulmonary edema ;
- acute myocardial infarction;
- acute stage coronary syndrome;
- acute pancreatitis;
- heart failure;
- coronary artery spasm during coronary angiography;
- spastic intestinal dyskinesia;
- chronic angina pectoris;
- functional cholecystopathy.
The action of Nitroglycerin also helps to prevent hypertensive reactions during skin incisions, sternotomy, endotracheal intubation.
If the drug can not be taken?
One of the demanded "heart" means in pharmacies is Nitroglycerin. Its price makes it affordable for all segments of the population. But you can not use it without the recommendation of a specialist. As with any other drug, Nitroglycerin has its own contraindications. It:
- bradycardia, with a fixed heart rate of less than 50 beats in one minute;
- increased intracranial pressure;
- hypersensitivity to the active substance or other components of the dosage form;
- primary pulmonary hypertension;
- hypotension pronounced;
- angle-closure glaucoma;
- myocardial infarction with a low final diastolic pressure in the left ventricle and / or with severe hypotension - with blood pressure below 90 mm Hg;
- right ventricular infarction;
- collapse;
- cerebral hemorrhage;
- toxic pulmonary edema;
- severe aortic stenosis;
- cardiac tamponade;
- head injury;
- cerebral ischemia.
Also, this drug in any form is contraindicated in conditions accompanied by a decrease in the final diastolic pressure in the left ventricle.
Medication and special periods in a woman’s life
Many believe that Nitroglycerin for pain in the heart can be taken anyway. But you can’t do this at certain times in a woman’s life - this is pregnancy and breastfeeding. It is advisable that the woman be under the supervision of a doctor for the entire gestation period. Pain in the heart is an indicator for a thorough diagnosis. Nitroglycerin during pregnancy can be taken only in situations where the health benefits of the mother are much higher than the risk to the fetus. Only a specialist can assess a specific situation and prescribe a medicine for a woman expecting a baby’s birth. If the intake of "Nitroglycerin" is recommended for a woman during lactation, then the transfer of a newborn baby to artificial feeding should be considered.
Unwanted action
The drug that helps relieve heart pain is Nitroglycerin. Side effects when it is used in the treatment of certain diseases or conditions do not occur so often. Among these undesirable effects are observed:
- hyperemia of the skin;
- hypotension, including orthostatic form;
- hypothermia;
- headache;
- dizziness;
- motor anxiety;
- allergic contact dermatitis;
- diarrhea;
- fever and flushing;
- burning;
- itching
- collapse;
- methemoglobinemia;
- visual impairment (fuzziness);
- exacerbation of glaucoma;
- psychotic reactions;
- vomiting
- palpitations
- dry mouth
- nausea;
- fatigue;
- cyanosis.
Side effects of Nitroglycerin are rare, even less so-called paradoxical effects are recorded when the effect of the drug has the opposite of the expected result. This can be an attack of angina pectoris, coronary heart disease up to the development of myocardial infarction and sudden death, the development of the body's immunity to the action of the drug based on the nitro compound.
Along with other medicines
How to take "Nitroglycerin" in a specific dosage form, the doctor should tell the patient. He must take into account the possible combined effect of drugs that the patient is taking.
So, if the patient takes salicylates, then such a comprehensive treatment will lead to an increase in the level of nitroglycerin in the blood plasma. Barbiturates activate the metabolic breakdown of nitroglycerin.
The substance itself nitroglycerin inhibits the pressor action of adrenergic agonists, provokes a decrease in the activity of heparin with intravenous administration.
If this drug is prescribed for use in conjunction with antihypertensive, antiadrenergic drugs, vasodilators, calcium antagonists, tricyclic antidepressants, MAO inhibitors, with sildenafil citrate, ethanol, quinidine and novocainamide, it should be taken into account that the hypotensive and systemic vasodilates will be significantly enhanced. Antianginal activity of drugs increases with the combined use of nitroglycerin and methionine, N-acetylcysteine, ACE inhibitors and salicylates. But alpha-adrenergic agonists, histamine, dihydroergotamine, corticosteroids, m-anticholinergics, pituitrin, stimulants of the central nervous system and autonomic ganglia, as well as organic poisons - snake and bee, and excessive insolation reduce vasodilator and antianginal effects.
Excess drug
How to take "Nitroglycerin"? In accordance with the appointment of the attending physician, without violating the dosage and regimen. But if for any reason the drug was taken in excess, then this can manifest itself as follows:
- hypotension;
- dizziness and / or headache;
- methemoglobinemia;
- unusual breakdown, weakness;
- fainting or fainting;
- dyspnea;
- feeling of intense pressure in the head;
- increased sweating;
- vomiting
- palpitations
- nausea;
- increase in body temperature;
- the pulse is weak, rapid;
- increased intracranial pressure, accompanied by cerebral symptoms up to the development of seizures and coma);
- cyanosis (blueing) of the lips, palms, nails;
- a fever - heat or chills.
Nitroglycerin does not have a specific antidote. Therefore, with an overdose of the drug, the following measures must be taken:
- to put the patient on a flat surface, raising his legs above the head to strengthen the venous return to the heart;
- if very little time has passed from the moment of taking the excess dose of the drug, then the stomach should be washed;
- use plasma substitutes and alpha-adrenergic agonists, for example, phenylephrine;
- take into account that it is impossible to use epinephrine as a cardiotonic agent, since an increase in the shock-like reaction is possible.
If the patient shows signs of methemoglobinemia, it is necessary to use oxygen under pressure or to inject intravenously 1% methylene blue solution at the rate of 1-2 mg of the drug per 1 kilogram of the patient’s body weight. Blood methemoglobin concentration should be monitored.
Features of nitroglycerin therapy
"Nitroglycerin" in case of heart attack in the inhabitants is considered a necessary medicine. But its use requires careful monitoring of the hemodynamics of the patient.
This drug is used with caution in therapy for aortic and mitral stenosis, as well as in patients with hypovolemia and significantly reduced, less than 90 mm Hg. systolic blood pressure. If the patient has hypertrophic cardiomyopathy, then nitroglycerin can provoke an increase and / or aggravation of angina attacks.
Capsules and tablets of the drug "Nitroglycerin" can not be cracked or chewed. They are taken sublingually, that is, placed under the tongue until completely resorbed. If the effect comes faster. than the drug is completely dissolved, its residues must be removed.
The buccal use of nitroglycerin is undesirable for patients suffering from gingivitis, aphthous stomatitis, periodontal and root system diseases, as well as with removable upper dentures.
Preparations with nitroglycerin should be taken only on the recommendation and under the supervision of a specialist, otherwise the development of tolerance to the active substance can be provoked. If the patient is prescribed prolonged forms of drugs, it is important to ensure interruptions in admission during the day, providing periods of the day free from the action of the drug, it is most convenient to determine this period of time at night. But at the same time, with such a regimen of the drug, there is a risk of developing withdrawal syndrome, which can become an impetus for the activation of an angina attack.
How to purchase and store medicine "for the heart"?
One of the popular heart remedies that can relieve pain in angina pectoris is Nitroglycerin. Its price is the most affordable - for a package of 40 tablets you will have to pay about 40-50 rubles. A bottle of spray costs about 100 rubles.
Such drugs are sold without a doctor’s prescription, but they should be taken only as directed by a specialist.
For the drug Nitroglycerin, the pharmacological group is defined as a coronary dilating and antianginal drug. It helps to cope with pain caused by disorders in the cardiovascular system. Only a specialist is entitled to recommend it after a thorough examination and diagnosis.