Nitroglycerin - instructions for use, reviews, analogs and formulations (tablets and capsules of sublingual 0,5 mg, spray or aerosol, injections in ampoules) for the treatment of angina in adults, children and pregnancy

In this article, you can read the instructions for using the drug Nitroglycerine. Comments of visitors of the site - consumers of this medication, as well as opinions of doctors of specialists on the use of Nitroglycerin in their practice are presented. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of Nitroglycerin in the presence of existing structural analogues.Use to treat and prevent attacks of angina and myocardial infarction in adults, children, as well as during pregnancy and lactation.

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

The effect of glycerol trinitrate is mainly due to the decrease in the demand for myocardium in oxygen due to a decrease in preload (the expansion of peripheral veins and a decrease in the flow of blood to the right atrium) and postnagruzki (reduction in OPSS). Promotes the redistribution of coronary blood flow to the ischemic subendocardial areas of the myocardium.Increases tolerance to physical activity in patients with coronary heart disease (CHD), angina pectoris. With heart failure, it helps to relieve the myocardium mainly by reducing preload. Reduces pressure in a small circle of blood circulation.

Pharmacokinetics

After oral intake absorbed from the gastrointestinal tract, is subjected to the effect of "first passage" through the liver. With sublingual application, this effect is absent, and the therapeutic concentration in the blood plasma is reached within a few minutes. Metabolised in the liver with the participation of nitrate reductase. Of the metabolites of glycerol trinitrate, dinitroderivatives can cause pronounced vasodilation; probably, they determine the therapeutic effect of glycerol trinitrate when taken orally. It is excreted mainly by the kidneys.

Indications

For sublingual and buccal use:

• cupping and prevention of angina attacks;
• as an emergency aid for acute myocardial infarction and acute left ventricular failure at the prehospital stage.

For oral administration:

• cupping and prevention of angina attacks;
• restorative treatment after myocardial infarction.

For intravenous administration:

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

For dermal application:

• prevention of angina attacks.

Forms of release

Tablets under the tongue of 0.5 mg.

Capsules sublingual 0,5 mg.

Spray or aerosol dosed sublingual.

Solution for intravenous administration (injections in ampoules for injection).

Tablets, coated with a shell, prolonged action 5.2 mg.

Instructions for use and dosage

Intravenously (it is necessary to dilute in a 5% solution of glucose or isotonic solution to a final concentration of 50 or 100 μg / ml): 0,005 mg / min, increase the dose by 0,005 mg / min every 3-5 minutes. to obtain an effect or to achieve a rate of 0.02 mg / min (with inefficiency - further increase by 0.01 mg / min).

Sublingually: tablets - 0,15-0,5 mg per reception, if necessary, again after 5 minutes; aerosol - to stop an attack of angina pectoris - 1-2 doses under the tongue, pressing the dosing valve (can be repeated, but not more than 3 doses for 15 min). In the case of acute left ventricular failure, 4 or more doses can be used for a short period.

Transdermally: they are glued each time to a new area of ​​the skin and left for 12-14 hours, after which they are removed to provide a break for 10-12 hours to prevent the development of tolerance.

Inside: pills and capsules are not chewed and not breaking, 2-4 times a day before meals, preferably 30 minutes. before exercise, a single dose of 5-13 mg; due to poor bioavailability, a single dose can increase to 19.5 mg.

Sub-buccal: the tablet is placed on the mucous membrane of the mouth (behind the cheek) and kept until complete resorption: 2 mg 3 times a day.

Side effect

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

Contraindications

• shock;
• collapse;
• arterial hypotension (systolic blood pressure <100 mmHg, diastolic blood pressure <60 mmHg);
• acute myocardial infarction with severe arterial hypotension;
• hypertrophic obstructive cardiomyopathy;
• constrictive pericarditis;
• cardiac tamponade;
• toxic pulmonary edema;
• increased intracranial pressure (incl.with a hemorrhagic stroke, after a recent head injury);
• closed angle glaucoma with high intraocular pressure;
• hypersensitivity to nitrates.

Application in pregnancy and lactation

The use of nitroglycerin during pregnancy and lactation (breastfeeding) is possible only in cases where the intended use for the mother exceeds the potential risk to the fetus or baby.

special instructions

They are used with caution in patients with severe cerebral atherosclerosis, cerebral blood flow disorders, orthostatic hypotension, severe anemia, elderly patients, hypovolemia and marked violations of liver and kidney function (parenteral).

With long-term use, the development of tolerance to the action of nitrates is possible. 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 the epicutaneous application of glycerol trinitrate causes an attack of angina pectoris, it should be quenched by the ingestion of glycerol trinitrate under the tongue.

During the treatment period, do not drink alcohol.

Impact on the ability to drive vehicles and manage mechanisms

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

Drug Interactions

With simultaneous use with vasodilators, ACE inhibitors, calcium channel blockers, beta-adrenoblockers, diuretics, tricyclic antidepressants, MAO inhibitors, ethanol (alcohol), ethanol-containing drugs, the hypotensive effect of glyceryl trinitrate may be increased.

With simultaneous use with beta-blockers, calcium channel blockers, antianginal action is intensified.

With simultaneous use with sympathomimetics, it is possible to reduce the antianginal effect of glycerol trinitrate, which, in turn, can reduce the pressor effect of sympathomimetics (as a result, hypotension is possible).

With the simultaneous use of drugs that have anticholinergic activity (including tricyclic antidepressants, disopyramide), hypoxalization, dry mouth develops.

There is limited evidence that Acetylsalicylic acid used as an analgesic agent increases the concentration of glycerol trinitrate in the blood plasma. This may be accompanied by increased hypotensive effect and headaches.

In a number of studies, there was a decrease in the vasodilating effect of glycerol trinitrate on the background of prolonged therapy with acetylsalicylic acid.

It is believed that it is possible to increase the antiaggregant effect of acetylsalicylic acid against the background of Nitroglycerin.

At simultaneous application with with glycerol trinitrate the action of acetylcholine, histamine, norepinephrine decreases.

Against the background of intravenous administration of Nitroglycerin, a decrease in the anticoagulant effect of Heparin is possible.

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

With simultaneous use with novocainamide, hypotensive effect and the development of collapse are possible.

With simultaneous use with rizatriptanum, Sumatriptan increases the risk of developing spasmcoronary arteries; with Sildenafil (Viagra) - the risk of severe arterial hypotension and myocardial infarction; with quinidine - orthostatic collapse possible; with ethanol (alcohol) - a sharp weakness and dizziness.

Analogues of the drug Nitroglycerin

Structural analogs for the active substance:

• Gluconite;
• Deposits 10;
• Nirmine;
• Nit-ret;
• Nitradisk;
• Nitro;
• Nitro Mac Ampoules;
• Nitro Mac Retard;
• Nitro Paul infuz;
• Nitro-dur;
• Nitro-Nick tablets;
• Nitroglycerin microgranules;
• Nitroglycerine Nycomed;
• Nitroglycerin forte;
• Nitrogranulong tablets coated;
• Nitrodzhekt;
• Nitrocore;
• Nitrorolling-Aerosol;
• Nitrolong;
• Nitromint;
• Nitroung forte;
• Nitrogen;
• Nitroperpecten TTS;
• Nitrospray;
• Nitrospray-ICN;
• Nitrosprint;
• Perlingant;
• Sustak mite;
• Sustak forte;
• Sustonite;
• Trinitrolong.

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