Effective pills to relieve heart pain

The main indications for the use of tablets for heart pain are the relief of attacks and intensification of pain syndrome of anginal etiology in such cardiac diseases as angina pectoris (including against the background of coronary insufficiency), ischemic heart disease, myocardial infarction.

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Indications for the use of tablets for heart pain

Sublingual tablets of Validol or Molsidomine help relieve pain during an attack of angina, and they are effective in cases of cardiovascular insufficiency, supraventricular tachycardia and cardiac atrial fibrillation. Moreover, Molsidomine can replace Nitroglycerin in case of individual intolerance to the latter.

Tablets for heart pain of the adrenaline cardioblocker group are prescribed for angina with spasms of small coronary vessels, tachycardia and extrasystole. And for myocardial ischemia, antiarrhythmic drugs of the nitrate group, calcium channel blockers and beta-blockers are necessary. Nitrates relieve vascular spasm and promote their expansion. And although blockers do not relieve pain directly, the consequences of their biochemical and physiological effects allow to relieve oxygen starvation of the heart muscle, reduce the heart rate (which is caused by excess adrenaline) and thereby relieve pain.

In cardiology, indications for the use of tablets for heart pain include a wide range of pathologies. Doctors classify drugs of these groups as antianginal and use them in the treatment of concomitant and stable angina, in the complex therapy of chronic heart failure, and also to normalize heart function after myocardial infarction.

Pharmacodynamics of tablets for heart pain

The mechanism of action of the sedative tablets Validol is due to non-specific reflex vasodilation, which occurs in response to local irritation of the receptors of the oral mucosa by menthol, which is part of its composition, dissolved in the menthol ester of 3-methylbutanoic (isovalerianic) acid. As a result of irritation of the nerve endings, the synthesis of neuropeptides and hormones responsible for vascular tone and inhibition of pain transmission increases in the body.

Pharmacodynamics of Molsidomine heart pain tablets is provided by its active substance, ethyl ester of N-carboxy-3-morpholino-sydnonimine, which reduces tension in cardiac venules and reduces venous blood flow to the heart. Due to this, blood filling of the left ventricle and overall myocardial tone are reduced.

All nitrate-based heart pain pills act on the vascular system of the entire body and dilate the heart vessels in a matter of minutes. The biochemical mechanism of this reaction has not been fully elucidated.

The drugs of this group help to reduce the tension of the walls of the coronary vessels and increase the blood flow to the myocardial tissues (which reduces their need for oxygen) - with a simultaneous reduction in the flow of venous blood (which reduces the pressure in the right atrium). Thus, a kind of redistribution of blood flow in the vessels of the heart occurs with the activation of arteriovenous blood supply to pathologically altered areas of the myocardium.

The increase in the contractile force of the myocardium under the influence of cardiac glycosides is explained by the increase in electrical activity (membrane action potential) of muscle tissue cells (cardiomycetes), in the cytoplasm of which Na ions accumulate and the level of Ca ions increases. In addition, the cardiac conduction system (CCS), in particular, the atrioventricular node in the interatrial septum, begins to transmit excitation to the muscle fibers of the myocardium more slowly, which reduces the heart rate.

The pharmacodynamics of beta-blockers used in cardiology is associated with a decrease in the effect of neurotransmitters adrenaline and noradrenaline on their specific receptors in the heart muscle. This is ensured by the active substance metoprolol tartrate, and due to it, the synthesis of cyclic adenosine monophosphate (cAMP) and the level of calcium ions in the cells of the myocardium are reduced. The result of all biochemical changes is a decrease in the intensity of heart contractions, stabilization of vascular tone (and arterial pressure), as well as sufficient oxygen supply to the myocardial cells.

The principle of action of calcium channel blockers of the sinoatrial and atrioventricular nodes is to neutralize the contractile effect of calcium ions on the walls of myocardial blood vessels. As a result, coronary vessel spasm ceases, and muscle fibers do not experience oxygen deficiency. This has a positive effect on the mechanics of the heart: the normal rhythm of its contractions is restored.

Pharmacokinetics of tablets for heart pain

Nitroglycerin and all drugs of the nitrate group, when administered sublingually, immediately enter the bloodstream, so these tablets for heart pain act very quickly - in 1.5-2 minutes.

The pharmacokinetics of cardiac glycosides – digoxin – is characterized by rapid absorption in the gastrointestinal tract, accumulation in muscle tissues and average bioavailability within 65-75% of the dose taken. The maximum level of the active substance of the drugs in the blood is achieved within 90 minutes from the moment of administration. 20% of the glycosides are metabolized in the liver, and the rest are excreted from the body in their original form; the half-life is 1.5-3 days.

The active substance of Metoprolol and other cardiac beta-blockers (metoprolol tartrate) is adsorbed in the digestive tract by 90%, but its bioavailability does not exceed 50%. The maximum concentration of the active substance is determined in the blood plasma after a maximum of 120 minutes after oral administration. Biotransformation occurs in the liver, metabolites are completely excreted in the urine after 7-10 hours.

Pharmacokinetics of Verapamil tablets for heart pain: adsorbed in the digestive tract and bound to plasma proteins; the highest concentration of verapamil hydrochloride in plasma is achieved 60-100 minutes after oral administration. Bioavailability does not exceed 35%; undergoes metabolism in the liver; excreted by the kidneys and through the intestines.

Names of pills for heart pain

Depending on the nature of the therapeutic effect, cardiac pain relief drugs are divided into peripheral vasodilators (including nitrates), cardiac glycosides, selective beta-blockers and calcium channel blockers.

Vasodilators include Validol (Corvalment), Molsidomine (Corvaton, Sidnofarm), as well as a large group of glycerol-esterified nitric acid salts (nitrates) and their derivatives.

Names of nitrate-based tablets for heart pain: Nitroglycerin (Nitromint, Nitrocor, Nitrocardiol, Sustak); derivatives of nitroglycerin mononitrate isosorbide (Monizid, Monosan, Olikard, Pentrol, Pentacard) and isosorbide dinitrate (Isacardin, Cardiket, Cardonit, Cardix); as well as Pentaerythritol tetrat (Pentral, Pentrit, Nitropentor, Vasocor, Vasodilatol, Erinit, etc.) - based on tetranitropentaerythritol.

The group of cardiac glycosides (cardiotonic agents) includes tablet preparations based on the digitalis glycoside digoxin: Digoxin, Gitoxin, Digicor, Izolanid, Celanid, Medilazide, Medigoxin, Methyldigoxin, Acetyldigoxin beta and other trade names.

The group of selective cardiac β1-adrenergic blockers is represented by such drugs as Metoprolol (Vazokardin, Corvitol, Lopressor, Betalok, Serdol Egalok).

Verapamil hydrochloride tablets Verapamil (Veracard, Lekoptin, Finoptin), as well as tablets based on benzothiazepine derivatives Diltiazem (Angisem, Ditriin, Diazem, Diacordin, Cardil and other trade names) are part of a fairly large pharmacological group of cardioselective calcium channel blockers.

Method of administration and dosage

The method of administration of Validol, Molsidomine and Nitroglycerin is sublingual (i.e. under the tongue). A separate recommendation regarding the dose of Nitroglycerin: if there is no effect on relieving the pain accompanying an attack of angina after the first dose of the drug (1-2 tablets of 0.5 mg), it should be taken again only after five minutes - not earlier.

Molsidomine can be taken orally, half or a whole tablet, 2-3 times a day (after meals), but the therapeutic effect appears after 20-25 minutes, that is, 2-3 times longer than with the sublingual method.

Doses of cardiac glycosides and calcium channel blockers are determined strictly individually - based on the results of a cardiological examination. The standard single dose of Digoxin is 0.25 mg, and the daily dose should not exceed 1.25 mg. And Verapamil tablets are recommended to be taken in a volume of 160-480 mg during the day; the course of treatment can last from 2 to 24 months.

Metoprolol is prescribed at 50 mg 2-4 times a day (depending on the patient's condition), the tablet should be swallowed whole during or immediately after a meal.

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Contraindications for use

The following contraindications for use are noted:

• Validol: complication of myocardial infarction in the form of cardiogenic shock, severe form of arterial hypotension.
• Nitroglycerin (and all nitrates): shock, increased intracranial pressure and impaired cerebral circulation, low blood pressure, glaucoma (closed-angle).
• Cardiac glycosides: tachycardia-bradycardia syndrome with weakness or dysfunction of the sinus node, atrioventricular block (1-2 degrees), ventricular arrhythmia, hypertrophic changes in the myocardium, stenosis of the aorta or mitral valve.

Metoprolol and other cardiac beta-blockers: acute myocardial infarction, sinoatrial or atrioventricular node block, heart failure (acute or chronic), decreased heart rate below 60 beats per minute, low blood pressure, peripheral circulatory problems (endarteritis, thrombophlebitis). As well as chronic obstructive bronchitis and bronchial asthma.

Calcium channel blockers (Verapamil, etc.) are contraindicated for use in cases of low blood pressure and decreased heart rate.

The use of heart pain pills during pregnancy is prohibited. Validol is contraindicated in the first trimester of pregnancy.

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Side effects

Vasodilators and heart pain-reducing tablets Validol and Molsidomine have side effects in the form of headache and decreased blood pressure. The most common adverse effects when using Nitroglycerin include: pulsating headache and dizziness; a feeling of heat in the upper body, flushing of the skin on the face and general hyperhidrosis; increased heart rate; a significant decrease in blood pressure.

Loss of appetite, nausea, vomiting, and headache may accompany the use (especially frequent) of cardiac glycosides.

The use of cardiac adrenaline receptor blockers (Metoprolol, etc.) can cause side effects such as sinus arrhythmia, shortness of breath, arterial hypotension, swelling of soft tissues of the extremities, dyspepsia, increased blood sugar levels, etc.

In addition to the side effects characteristic of Nitroglycerin and nitrates, the list of side effects of drugs that block calcium channels in the cardiac conduction system also includes a feeling of dry mouth, nausea and vomiting, intestinal problems, increased liver transaminases, paresthesia of the extremities, sleep disorders, depression and mental disorders.

Overdose

It should be borne in mind that an overdose of Nitroglycerin can lead not only to increased manifestation of side effects, but also to collapse.

As noted in the instructions, the symptoms of an obvious overdose of cardiac glycosides (glycoside intoxication) are expressed in the exacerbation of side effects, which are accompanied by heart rhythm disturbances, ventricular fibrillation, muscle weakness, impaired vision and color perception, euphoria and a state of psychosis. In such a situation, the intake of drugs is stopped, a laxative (saline) is given and symptomatic treatment of cardiac manifestations is carried out.

Exceeding the prescribed dosage of Metoprolol causes a drop in blood pressure, convulsions, cyanosis of the mucous membranes, a state of acute heart failure up to cardiogenic shock and cardiac arrest. In such cases, emergency medical care is required with gastric lavage and intravenous administration of appropriate drugs.

Overdose of Verapamil may also result in decreased heart rate and blood pressure, atrial and ventricular block, and loss of consciousness. The condition may require cardiac pacing.

Interactions with other drugs

The simultaneous use of Nitroglycerin with beta-adrenergic receptor blockers, vasodilators, diuretics, Aspirin and alcohol tinctures enhances the reduction in blood pressure. The anti-anginal effect is enhanced by a combination with beta-adrenergic blockers and calcium channel blockers.

Features of interaction with other cardiac glycoside drugs:

• enhancing changes in myocardial contraction in combination with B vitamins,
• reduction of heart rate in combination with sleeping pills, magnesium sulfate and local anesthetics,
• improvement of hemodynamics with simultaneous administration of curantil,
• increased blood clotting when combined with aminazine and heparin.

Interaction of cardiac beta-blockers (Metoprolol, etc.): it is prohibited to use together with Nitroglycerin, barbiturates, diuretics and alcohol-containing products; the effect of antihypertensive drugs is enhanced; with the combined use of cardiac glycosides, there is an excessive decrease in heart rate and a slowdown in the work of the cardiac conduction system.

Interaction of calcium channel blockers (Verapamil hydrochloride) with other drugs:

• enhance the blockade of the sinoatrial and atrioventricular nodes when combined with beta-blockers,
• enhances the effect of drugs to lower blood pressure and relieve muscle spasms,
• The effect of Verapamil is potentiated by the simultaneous use of neuroleptics and antidepressants.

Storage conditions

According to the instructions, Nitroglycerin should be stored in a dark place, protected from possible contact with fire, at a moderate temperature (+18-20°C). The remaining tablets for heart pain are stored in a dark place, at a temperature not exceeding +25°C.

The expiration date of the drugs is indicated on the packaging, which also contains information about the date of manufacture.