Nitroglycerine (Nitroglycerin)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
Read on
Similar drugsTo uncover
Dosage form: & nbspconcentrate for solution for infusion
Composition:

In 1 ml of the drug contains:

of the active substance: nitroglycerin with glucose 10 mg (contains active ingredient: nitroglycerin 1 mg; excipient: glucose (dextrose) up to 10 mg);

Excipients: sodium chloride, potassium dihydrogen phosphate, water for injection.

Description:

A clear, colorless liquid.

Pharmacotherapeutic group:Vasodilating agent - nitrate
ATX: & nbsp
  • Nitroglycerine
    • Pharmacodynamics:

    Venodilating agent from the group of nitrates. Nitrates are able to release from their molecule nitric oxide, which is a natural endothelial relaxing factor - a mediator of the direct activation of guanylate cyclase. An increase in the concentration of cyclic guanosine monophosphate results in the relaxation of smooth muscle fibers (mainly venules and veins). Has antianginal and spasmolytic effect, relaxes the smooth muscles of the vascular walls, bronchi, gastrointestinal tract, bile ducts, ureters. With intravenous administration, a rapid decrease in preload on the heart is caused by the widening of the peripheral veins.

    Reduces the flow of blood to the right atrium, helps reduce pressure in the "small" circle of blood circulation and regressionsymptoms in swelling of the lungs, reduces postnagruzku, the need for myocardium in oxygen (due to reduced preload, postnagruzki and stress of the walls of the ventricles due to a decrease in the volume of the heart). Promotes redistribution of coronary blood flow in the area with reduced blood circulation.

    Has a central inhibitory effect on sympathetic vascular tone, inhibiting the vascular component of the pain syndrome.

    Causes the expansion of cerebral vessels, which explains the headache when it is used.

    With the prolonged or frequent use of long-acting nitrates, there is a development of tolerance to the drug (weakening of the therapeutic effect). After a break, the sensitivity is restored. In order to prevent the occurrence of tolerance, it is recommended to observe a daily, preferably nocturnal, "no-nite interval" for 8-12 hours. In most patients, such therapy is more effective than continuous treatment.

    Pharmacokinetics:

    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 glycerin.It is excreted by the kidneys in the form of metabolites. The total ground clearance is 25-30 l / min.

    With intravenous administration, the elimination half-life is 1-3 min, the total clearance is 30-78 l / min.

    Indications:

    Acute myocardial infarction (including complicated by acute left ventricular failure); unstable and postinfarction angina; pulmonary edema; controlled hypotension during surgical interventions to reduce bleeding in the operating theater.

    Contraindications:

    Increased sensitivity to nitroglycerin and other organic nitrates, isolated mitral stenosis, aortic stenosis, subaortal stenosis, cardiogenic shock, toxic pulmonary edema, acute circulatory disturbance (shock, vascular collapse), hypovolemia, severe arterial hypotension (systolic blood pressure <90 mm Hg. ), cardiac tamponade, constrictive pericarditis, diseases that occur with increased intracranial pressure, cerebral hemorrhage, severe anemia, age 18 years (efficacy and safety are not installed).

    In connection with a significant hypotensive effect and pronounced side effects (syncope, myocardial infarction),drugs for the treatment of erectile dysfunction (phosphodiesterase inhibitors) should not be used against the background of therapy with nitroglycerin group drugs.

    Carefully:

    Hypertrophic obstructive cardiomyopathy, atherosclerosis, acute myocardial infarction with low left ventricular filling pressure, recently suffered head trauma, angle-closure glaucoma, severe renal failure, hepatic insufficiency (risk of methaemoglobinaemia), thyrotoxicosis, diabetes mellitus.

    Pregnancy and lactation:

    The use of nitroglycerin during pregnancy and during breastfeeding is possible if the potential benefit of treatment for the mother exceeds the risk to the fetus or the baby.

    Dosing and Administration:

    Intravenous injection of nitroglycerin should be carried out with an individual selection of the rate of administration of the drug.

    The solution is administered via an automatic dispenser or via a conventional intravenous infusion system. Automatic dispenser allows introduce even undiluted 0.1% solution with precise dosing of the rhythm of administration and total dose.

    Introduction through a conventional system for transfusion of fluids provides the choice of an accurate dose by counting the number of drops.When using a system of PVC tubes, the active substance is absorbed and losses on the walls of the tubes are up to 60% (it is advisable to use polyethylene and glass tubes). The solution is rapidly destroyed in the light, therefore the vials and the transfusion system must be screened with a lightproof material.

    Usually, an infusion solution with a concentration of 100 μg / ml is used: the concentrated solution is diluted with 0.9% sodium chloride solution or 5% dextrose solution (do not use other solvents).

    The solution is intravenously dripped, with an initial rate of 5 μg / min.

    The rate of administration can be increased every 3-5 minutes by 5 μg / min (depending on the therapeutic effect, heart rate, central venous pressure and systolic blood pressure, which can be reduced by 10-25% of the initial, but should not be lower 90 mmHg).

    If no therapeutic effect is obtained at a rate of 20 μg / min, a further increase in the rate of administration should be 10-20 μg / min.

    When there is a response (in particular, lowering blood pressure), further increase in the rate of infusion is not performed or carried out at longer intervals.

    To achieve a good effect, the rate of administration of a 0.01% solution of nitroglycerin usually does not exceed 100 μg / min (1 ml / min).

    In the absence of effect from smaller doses and an acceptable level of arterial pressure, the introduction rate of 0.01% solution may reach 300 μg / min (3 ml / min). Further increase in speed is impractical.

    The duration of treatment is determined by clinical indications and can be 2-3 days.

    Nitroglycerin for intravenous administration can be re-introduced, if necessary, at any time intervals.

    Side effects:

    From the cardiovascular system: tachycardia, skin hyperemia, fever, lower blood pressure, palpitations, unpleasant sensations behind the sternum; orthostatic collapse, cyanosis.

    With a marked decrease in blood pressure, a paradoxical bradycardia and an increase in symptoms of angina may occur.

    From the gastrointestinal tract: dryness of the oral mucosa, nausea, vomiting, abdominal pain.

    From the central nervous system: dizziness, headache, anxiety, psychotic reactions, inhibition, disorientation, fainting.

    Allergic reactions: skin rash, itching.

    Local reactions: skin hyperemia, skin itching, burning, allergic contact dermatitis.

    Other: blurred vision, weakness, hypothermia, methemoglobinemia.

    Overdose:

    Symptoms: marked decrease in blood pressure (below 90 mm Hg) with orthostatic dysregulation, reflex tachycardia, headache; may develop asthenia, dizziness, increased drowsiness, a feeling of heat, nausea, vomiting; when used in high doses (more than 20 mg / kg) - collapse, cyanosis, methemoglobinemia, dyspnea and tachypnea; at very high doses, an increase in intracranial pressure is possible.

    Treatment: with intravenous administration - stop further administration. It is necessary to lower the head end of the bed and raise the patient's legs. As a rule, the blood pressure is normalized within 15-20 minutes after the cessation of nitroglycerin administration, then you can continue the injection after re-selection of the infusion rate. To correct blood pressure, it is possible to use phenylephrine and other vasoconstrictors.

    At a methemoglobinemia, depending on a degree of gravity, are appointed or nominated: ascorbic acid - 1 g inside or intravenously (in the form of sodium salt); oxygen therapy, hemodialysis, exchange blood transfusion.

    Interaction:

    Simultaneous use of nitroglycerin with vasodilators, hypotensive drugs, andMr.angiotensin-converting enzyme (ACE), beta-blockers, blockers of "slow" calcium channels, procainamide, tricyclic antidepressants, monoamine oxidase inhibitors, diuretics, and also ethanol enhances the hypotensive effect.

    With simultaneous admission with sildenafil, as well as with other inhibitors of phosphodiesterase, a sharp drop in blood pressure may occur.

    The 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).

    Against the background of quinidine and procainamide, orthostatic collapse may occur.

    Simultaneous administration of nitroglycerin and heparin reduces the effectiveness of the latter (after drug cancellation, a reduction in the dose of heparin may be required).

    Special instructions:

    In acute myocardial infarction or acute heart failure should be used only under the condition of careful monitoring of the patient.

    To prevent the increase in angina attacks, sharp abolition should be avoided. To prevent undesirable reduction in blood pressure, it is necessary to select the rate of administration of the drug individually and methodically correctly (see above).

    Reduction of blood pressure can be observed not only during the selection of the rate of nitroglycerin, but also later, against the background of initially stabilized blood pressure. Therefore, control over blood pressure should be carried out at least 3-4 times per hour during the entire infusion of nitroglycerin.

    Perhaps the development of tolerance to nitroglycerin, as well as the development of group tolerance to nitrates (a decrease in the effectiveness of the drug with previous therapy with other nitrates).

    Patients previously treated with organic nitrates (isosorbide dinitrate, isosorbide-5-mononitrate) may need a higher dose to produce the desired hemodynamic effect.

    The solution for intravenous administration contains dextrose, which must be taken into account when used in patients with diabetes mellitus.

    Effect on the ability to drive transp. cf. and fur:

    During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

    Form release / dosage:Concentrate for the preparation of a solution for infusions 1 mg / ml.
    Packaging:

    In ampoules of 10 ml.

    For 10 ampoules with instructions for use, a vial ampoule or scarifier ampullum in a pack of cardboard.

    5 ampoules in the outline of the cell. 2 contour packs with instructions for use, ampoule or ampoule with a knife in a pack of cardboard.

    When packaging ampoules that have a break ring or an opening point, the ampoule knife or the ampoule scapegrator is not put in.

    5 ampoules in a cassette outline package. 2 cassette contour packs with instructions for use in a pack of cardboard.

    Storage conditions:

    In a cool, dark place away from the fire.

    Do not store the solution in an opened ampoule.

    Keep out of the reach of children.

    Shelf life:

    2 years.

    Do not use after the expiration date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:LS-002352
    Date of registration:08.02.2012 / 28.01.2015
    Expiration Date:Unlimited
    The owner of the registration certificate:MICROGEN FGUP Scientific and Production Association MICROGEN FGUP Scientific and Production Association Russia
    Manufacturer: & nbsp
    Representation: & nbspMICROGEN FGUP Scientific and Production Association MICROGEN FGUP Scientific and Production Association Russia
    Information update date: & nbsp22.06.2018
    Illustrated instructions
      Instructions
      Up