Description of the active substance:
This information is a reference and it is not enough that the drug has been prescribed by a doctor ..
Peripheral vasodilator with 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, 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 action of nitroglycerin (glyceryl trinitrate) is mainly due to a decrease in the demand for myocardium in oxygen due to a reduction 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 exercise tolerance in patients with IHD, angina pectoris. With heart failure, it helps to relieve the myocardium mainly by reducing preload. Reduces pressure in a small circle of blood circulation.
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. From the metabolites of nitroglycerin, dinitroderivatives can cause pronounced vasodilation; probably, they determine the therapeutic effect of nitroglycerin (glyceryl trinitrate) when ingested.
The binding to plasma proteins is 60%. T 1/2 after ingestion - 4 hours, with sublingual application - 20 minutes, after intravenous administration - 1-4 minutes. It is excreted mainly by the kidneys.
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.
Apply sublingually, buccally, inwardly, dermally, intravenously drip. The dose and treatment regimen is set individually, depending on the indications, the specific clinical situation, the dosage form used.
From the cardiovascular system: dizziness, headache, tachycardia, skin flushing, fever, arterial hypotension; rarely (especially with an overdose) - collapse, cyanosis.
From the digestive system: nausea, vomiting.
From the side of the central nervous system: rarely (especially with an overdose) - anxiety, psychotic reactions.
Allergic reactions: rarely - skin rash, itching.
Local reactions: mild itching, burning, redness of the skin.
Shock, collapse, arterial hypotension (systolic blood pressure <100 mmHg, diastolic BP <60 mmHg), acute myocardial infarction with severe arterial hypotension, hypertrophic obstructive cardiomyopathy, constrictive pericarditis, cardiac tamponade, toxic pulmonary edema, increased intracranial pressure (including with hemorrhagic stroke, after a recent head injury), angle-closure glaucoma with high intraocular pressure, increased sensitivity to nitrates.
PREGNANCY AND LACTATION
The use of nitroglycerin (glyceryl trinitrate) 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.
APPLICATION FOR FUNCTIONS OF THE LIVER
With caution apply for severe impairment of kidney function (parenteral).
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
With caution apply for severe violations of the liver (parenteral).
APPLICATION IN ELDERLY PATIENTS
Use with caution in elderly patients.
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 a nasal application of nitroglycerin (glyceryl 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
Glyceryl trinitrate can reduce the speed of psychomotor reactions, which should be taken into account when driving vehicles or engaging in other potentially hazardous activities.
With simultaneous use with vasodilators, ACE inhibitors, calcium channel blockers, beta-adrenoblockers, diuretics, tricyclic antidepressants, MAO inhibitors, ethanol, 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 nitroglycerin (glyceryl trinitrate) in blood plasma. This may be accompanied by increased hypotensive effect and headaches.
In a number of studies, a decrease in the vasodilating effect of nitroglycerin (glyceryl trinitrate) was observed against long-term therapy with acetylsalicylic acid.
It is believed that it is possible to increase the antiplatelet effect of acetylsalicylic acid against the background of nitroglycerin (glyceryl trinitrate).
At simultaneous application with nitroglycerin decreases action of acetylcholine, histamine, norepinephrine.
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 nitroglycerin (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 coronary artery spasm; with sildenafil - the risk of severe arterial hypotension and myocardial infarction; with quinidine - orthostatic collapse possible; with ethanol - a sharp weakness and dizziness.