Nitro

General characteristics. Structure:

Active ingredient: 5,0 mg of nitroglycerine in 1 ml of solution.

Excipients: ethanol of 96%, propylene glycol for parenteral use, water for injections.

Vazodilatator from group of organic nitrates. Along with decrease in resistance of coronary and peripheral vessels nitroglycerine reduces venous return of blood to heart, promotes redistribution of a blood-groove in a myocardium in favor of the center of ischemia and to reduction at a heart attack of a myocardium of the centers of ischemic defeat, strengthens inotropic function of a myocardium. As well as other organic nitrates, nitroglycerine improves metabolic processes in a myocardium, reduces the need of a myocardium for oxygen.

Pharmacological properties:

Pharmacodynamics. A peripheral vazodilatator with preferential influence on venous vessels. Anti-anginal means. The mechanism of action is connected with release of active agent of nitrogen oxide in smooth muscles of vessels. Nitrogen oxide causes activation of guanylate cyclase and increases the tsGMF level that, eventually, leads to relaxation of an unstriated muscle. Under the influence of glyceryl of trinitrate of an arteriole and precapillary sphincters relax to a lesser extent, than large arteries and veins. It is partially caused by reflex reactions, and also less intensive formation of nitrogen oxide from molecules of active agent in walls of arterioles.

Effect of nitroglycerine (trinitrate glyceryl) is connected mainly with reduction of need of a myocardium for oxygen due to reduction of preloading (expansion of peripheral veins and reduction of inflow of blood to the right auricle) and afterloads (reduction of OPSS). Promotes redistribution of a coronary blood-groove to ischemic subendocardial areas of a myocardium. Increases tolerance to an exercise stress at patients with an ischemic heart disease, stenocardia. At heart failure promotes unloading of a myocardium mainly due to reduction of preloading. Reduces pressure in a small circle of blood circulation.

Pharmacokinetics. After intake it is absorbed from a GIT, is exposed to effect of "the first passing" through a liver. At sublingual use the specified effect is absent, and therapeutic concentration in a blood plasma is reached within several minutes. It is metabolized in a liver with the participation of nitrate reductase. From nitroglycerine metabolites dinitroderivatives can cause the expressed vazodilatation; perhaps, they define therapeutic effect of nitroglycerine (trinitrate glyceryl) at intake.

Linkng with proteins of plasma makes 60%. T1/2 after intake is 4 h, at sublingual use - 20 min., later in/in introductions - 1-4 min. It is removed preferential by kidneys.

Indications to use:

The acute myocardial infarction including complicated by an acute left ventricular failure. Stenocardia, including unstable and postinfarction. Fluid lungs. Hypertensia in connection with surgical intervention on open heart and other surgeries; induction of controlled hypotension in case of surgical interventions.

Route of administration and doses:

Only for intravenous use!
The mode of dosing is set individually depending on a condition of the patient and a pokazateleygemodinamika.

During infusion it is necessary to carry out constant control of the systolic and diastolic ABP, the heart rate (HR), an ECG, minute volume of heart, and also (whenever possible) systolic and diastolic pressure in a pulmonary artery, jamming pressure in pulmonary capillaries.

Usually use the infusion solution containing 100 mkg/ml of nitroglycerine. Such solution prepares by cultivation of 5 ampoules of the Nitro concentrate for infusions (=50 mg of nitroglycerine) in 500 ml of 0,9% isotonic solution, 5% solution of a dextrose (glucose) or normal glyukozosolevy saline solution for obtaining concentration of solution of 0,1 mg/ml (it is not necessary to apply in a combination with other medicines). It is possible to use more strong solution, but it is not recommended to exceed concentration of 400 mkg/ml.

Glycerin trinitrate is adsorbed by plastic. Therefore when mixing infusion solution следуетприменять glass bottles.

Intravenous administration is begun slowly with a speed of 10-20 mkg/min. Then rate of administering can be increased by 10–20 mkg/min. with 5-10-minute intervals depending on reaction of the patient. The good therapeutic effect is usually reached at rate of administering of 50-100 mkg/min. The maximum rate of administering makes 400 mkg/min. Duration of administration of drug depends on dynamics of clinical symptoms and indicators of a hemodynamics and can make from several hours to 3 days.

At long introduction of high doses in 8–24 hours tolerance develops and increase in a dose can be required. At intravenous administration of the drug Nitro the expressed hemodynamic effects are observed. Therefore drug is used only in stationary conditions and demands constant control of function of cardiovascular system. Systolic the ABP more than should not decrease by 10–15 mm of mercury. at patients with the normal ABP, no more than on 5 mm of mercury. at patients with arterial hypotension or inclined to it, ChSS should not increase more than on 5 уд. / mines if in the same time the clinical picture accurately improves.

As the withdrawal (a phenomenon of "ricochet") is not excluded, it is not recommended to stop sharply administration of the drug Nitro, and it is necessary to reduce a dose slowly.

Features of use:

Purpose of drug the patient with anemia, a hypertrophic subaortic stenosis, an aortal or mitral stenosis, with a pulmonary heart; with an acute myocardial infarction, in the presence of a renal/liver failure, at the expressed anemia, to patients of advanced age, with a hemorrhagic stroke / a craniocereberal injury in the anamnesis it has to be carried out with care.

Information on use of drug during the periods of pregnancy and a lactation is limited therefore it should be applied only in that case when the expected result exceeds possible harm for the fruit/newborn. In these cases the lowest dose has to be used.

Side effects:

From cardiovascular system: dizziness, headache, tachycardia, hyperemia of integuments, feeling of heat, arterial hypotension; seldom (especially at overdose) - a collapse, cyanosis.

From the alimentary system: nausea, vomiting.

From TsNS: seldom (especially at overdose) - concern, psychotic reactions.

Allergic reactions: seldom - skin rash, an itch.

Local reactions: slight itch, burning, erubescence.

Others: methemoglobinemia.

Interaction with other medicines:

At simultaneous use with other vazodilatator, APF inhibitors, blockers of "slow" calcium channels, beta adrenoblockers, diuretics, tricyclic antidepressants, MAO inhibitors and inhibitors of phosphodiesterase, ethanol and etanolsoderzhashchy drugs hypotensive effect of nitroglycerine amplifies. Introduction of higher doses Nitro can be required by the patients who were earlier receiving therapy by organic nitrates for achievement of desirable hemodynamic effect.

Alcohol can cause development of hypotension and feeling of weakness at therapy by nitroglycerine.

The combination to dihydroergotamine is irrational as can lead to increase in bioavailability of the last, increasing risk of a digidroergotaminindutsirovanny coronary spasm.

Combined use of heparin and nitroglycerine leads to weakening of effect of heparin. At regular control of parameters of a blood coagulation the dose of heparin has to be respectively picked up. After drug withdrawal perhaps essential decrease in indicators of coagulability of blood which can demand a heparin dose decline.

Sildenafil increases hypotensive effect of nitroglycerine.

Simultaneous use of nitroglycerine and drugs-inhibitors of phosphodiesterase contraindicated.

Contraindications:

Hypersensitivity to a glitseriltrinitrat and other nitro compounds; the expressed arterial hypotension (systolic pressure <90 mm hg); uncontrollable hypovolemia; the increased intracranial pressure; chronic cardial compression; hypertrophic subaortic stenosis; cardiac tamponade; toxic fluid lungs; closed-angle glaucoma with high intraocular pressure.

Sildenafil. The concomitant use of inhibitor of phosphodiesterase of type 5 – a sildenafil as sildenafit exponentiates hypotensive effect of nitrates (the break between receptions has to make not less than 48 h).

Overdose:

Symptoms: the expressed lowering of arterial pressure with orthostatic dysregulation, reflex tachycardia and a headache. There can be an adynamy, dizziness, the increased drowsiness, feeling of heat, nausea, vomiting. At use of high doses (more than 1-2 mg/kg of body weight) the methemoglobinemia, cyanosis, диспноэ and a tachypnea can develop.

Treatment: at the expressed decrease in the ABP and/or the patient in state of shock it is necessary to enter liquid. In exceptional cases for improvement of blood circulation it is possible to enter noradrenaline (Norepinephrinum) and/or a dopamine. Administration of adrenaline (Epinephrinum) and related connections contraindicated. Depending on severity in cases of a methemoglobinemia below-mentioned antidotes are applied.

1. Vitamin C: 1 g in or in the form of sodium salt intravenously.
2. Methylene blue: to 50 ml of 1% of solution intravenously.
3. Oxygenotherapy, hemodialysis, exchange hemotransfusion.

Storage conditions:

To store at the room temperature (15–25 °C) in the place, unavailable to children. Solution has to be used right after cultivation!

Issue conditions:

According to the recipe

Packaging:

5 ampoules on 2 ml in a cardboard box.