Nitroglycerin - instructions for use, dose, side effects, contraindications

Peripheral vasodilator with predominant effect on venous vessels. 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. Increasing the concentration of cGMP leads to a 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 (IV) injection causes a rapid decrease in preload on the heart due to the expansion of peripheral veins.

Reduces the flow of blood to the right atrium, helps to reduce pressure in the "small" circle of blood circulation and regression of symptoms when swelling of the lungs, reduces afterload, the need for myocardium in oxygen (due to reduced preload, afterload and ventricular wall tension due to a decrease in heart volume). 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. It causes the expansion of meningeal vessels, which explains the headache when it is used.

The effect develops 1-2 minutes after the start of the infusion.

Pharmacokinetics:

Getting into the systemic bloodstream, 60% binds to blood plasma proteins. It is highly lipophilic and has a large volume of distribution (3.3-1.2 l / kg).

Rapidly metabolized in the liver by glutathione reductase, which affects organic nitrates, with the formation of di- and mononitrates, the final metabolite is glycerol. It is excreted by the kidneys in the form of metabolites. The total ground clearance is 30-78 l / min, the half-life is -1-4 min.In addition, the metabolism of nitroglycerin in erythrocytes is mediated by enzymatic reactions that occur with the participation of sulfhydryl radicals, as well as in interaction with reduced hemoglobin.

Indications:

Acute myocardial infarction (including complications of acute left ventricular failure); unstable angina; controlled arterial hypotension during surgical interventions to reduce bleeding in the operating theater.

Contraindications:

Hypersensitivity to the drug and other nitro compounds, shock, collapse, age 18 years (effectiveness and safety has not been established).

Carefully:

Craniocerebral hypertension, cardiac tamponade, toxic lung edema, hemorrhagic stroke, isolated mitral stenosis, aortic stenosis, hypertrophic obstructive cardiomyopathy, constrictive pericarditis (state accompanied by a pressure decrease in the filling of the left ventricle), hypovolemia, hypotension with a low systolic blood pressure (can aggravate the condition, causing a paradoxical bradycardia and angina), glaucoma, pregnancy, lactation, recent cerebral trauma, severe cerebral atherosclerosis, severe renal failure (risk of methaemoglobinaemia), thyrotoxicosis, severe anemia, hepatic insufficiency, elderly age.

Dosing and Administration:

Intravenously, drip. The introduction should be carried out with an individual selection of the rate of administration of the drug.

Nitroglycerin concentrate 1% is diluted in 0.9% sodium chloride solution to a concentration that is 0.01%. This solution contains 100 μg (0.1 mg) of nitroglycerin in 1 ml. The initial rate of administration of a 0.01% solution of nitroglycerin is 25 μg / min (1 ml of 0.01% solution over 4 minutes).

The rate of administration is adjusted depending on the therapeutic effect and the response of systolic blood pressure, which can be reduced by 10-25% of the initial, but should not be less than 90 mm Hg.

In the absence of effect and the acceptable level of AD, the rate of administration is increased by 25 μg / min every 15-20 minutes. That is, after the first increase in the rate of administration, the patient receives 2 ml of a 0.01% solution of nitroglycerin in 4 minutes, then 3 ml in 4 minutes and then 4 ml in 4 minutes. To achieve the optimal effect, the rate of administration of a 0.01% solution of nitroglycerin usually does not exceed 100 μg / min. (1 ml of solution per 1 minute).

In the absence of the effect of smaller doses and the acceptable level of AD, the rate of administration can reach 300 μg / min (3 ml of 0.01% solution).

Further increase in the rate of administration is impractical.

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

Nitroglycerin for intravenous administration may be re-administered, if necessary, under the control of blood pressure, at any time intervals.

Side effects:

From the cardiovascular system: decrease in blood pressure (below 90 mm Hg), dizziness, nitrate headache, tachycardia, skin hyperemia, fever, palpitation; rarely (especially with an overdose) - orthostatic collapse, cyanosis, methemoglobinemia.

From the gastrointestinal tract: dry mouth, nausea, vomiting, abdominal pain.

From the central nervous system: rarely (especially with an overdose) - anxiety, psychotic reactions, inhibition, disorientation, blurred vision, dizziness, general weakness.

Possible allergic reactions, hypothermia.

Overdose:

Symptoms: marked decrease in blood pressure (below 90 mm Hg) with orthostatic dissolution, reflex tachycardia, headache,dizziness, increased drowsiness, a feeling of heat, nausea, vomiting; when using high doses (more than 20 mg / kg) - collapse, cyanosis, methemoglobinemia, dyspnea and tachypnea.

Treatment: discontinue further administration of the drug. It is necessary to lower the head of the bed and raise the patient's legs. As a rule, blood pressure is normalized within 15-20 minutes after stopping the introduction of nitroglycerin, then you can continue the introduction, after re-selection of the infusion rate.

To correct blood pressure, it is possible to use phenylephrine and other vasoconstrictors.

Depending on the degree of severity, the following antidotes are suggested in the case of methemoglobinemia:

1. Vitamin C: 1 g orally or as sodium salt intravenously

2. Methylthioninium chloride (methylene blue): up to 50 ml of 1% solution of methylene blue intravenously

3. Oxygenotherapy, hemodialysis, exchange blood transfusion.

Interaction:

Simultaneous use with vasodilators, antihypertensives, angiotensin converting enzyme (ACE) inhibitors, beta-blockers, slow calcium channel blockers, novocainamide, tricyclic antidepressants, monoamine oxidase inhibitors (MAO), phosphodiesterase inhibitors, and also ethanol enhances the hypotensive effect.

The appointment with dihydroergotamine can lead to an increase in its content in the blood and lead to an increase in blood pressure (increasing the bioavailability of dihydroergotamine).

Simultaneous administration of nitroglycerin and heparin reduces the effectiveness of the latter (after drug cancellation, there may be a significant reduction in blood coagulability, which may require a reduction in the dose of heparin).

Simultaneous use with sapropterin can lead to an increased risk of arterial hypotension due to additional activation of nitric oxide synthesis.

Special instructions:

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

To prevent undesirable reduction in blood pressure should be individually and methodically correct (see above) to select the rate of administration of the drug.

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

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

Severity of headache against the background of taking nitroglycerin can be reduced by lowering its dose and / or concurrent administration of Validol.

If blurred vision or dry mouth is retained or severely expressed, treatment should be discontinued.

Form release / dosage:

Concentrate for solution for infusion, 10 mg / ml.

Packaging:

When produced at OOO "Experimental Plant" GNTSLS ", Ukraine

2 ml in ampoules.

For 10 ampoules together with the instruction for use and scarifier ampoule or disk cutting ceramic in a pack of cardboard.

5 ml in ampoules.

For 5 or 10 ampoules together with the instruction for use and scarifier ampoule or disk cutting ceramic in a pack of cardboard.

If there are fracture rings or break points on the ampoule, the ampoule scarifier or ceramic cutting disc is not put into the pack.

When produced at OOO "Pharmaceutical Company" Health ", Ukraine

2 ml in ampoules.

For 10 ampoules together with the instruction for use and scarifier ampoule or disk cutting ceramic in a pack of cardboard.

5 ml in ampoules.

For 5 or 10 ampoules together with the instruction for use and scarifier ampoule or disk cutting ceramic in a pack of cardboard.

If there are fracture rings or points and incisions on the ampoule, the ampoule scarifier or ceramic cutting disc is not inserted into the pack.

Storage conditions:

Store in a dark place, away from fire, at a temperature of 8 to 15 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

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

Terms of leave from pharmacies:On prescription

Registration number:LSR-008037/08

Date of registration:10.10.2008 / 20.04.2015

The owner of the registration certificate:EXPERIMENTAL FACTORY ГНЦЛС, ООО EXPERIMENTAL FACTORY ГНЦЛС, ООО Ukraine

Manufacturer: & nbsp

EXPERIMENTAL FACTORY ГНЦЛС, ООО Ukraine

HEALTH PHARMACEUTICAL COMPANY, LTD. Ukraine

Information update date: & nbsp11.03.2016

Illustrated instructions

Instructions

Nitroglycerine (Nitroglycerin)