Nitroglycerine

Nitroglycerine – the vasodilating drug used for stopping of attacks of stenocardia.

Form of release and structure

Nitroglycerine is produced in the following dosage forms:

• Tablets are hypoglossal: almost white or white, ploskotsilindrichesky, with a rough surface (on 40 tablets in the polymeric test tube which is densely corked by a polymeric stopper on 1 test tube in a cardboard pack);
• Spray hypoglossal dosed: colourless, transparent (in bottles or cylinders on 200 doses (10 ml), on 1 bottle or a cylinder in a cardboard pack complete with the dosing mechanical pump);
• Concentrate for preparation of solution for infusions: colourless, transparent (in ampoules on 2, 5 or 10 ml, on 5 ampoules in blister strip packagings, on 1, 2 or 10 packagings in a cardboard pack).

Hypoglossal is a part of 1 tablet:

• Active agent: nitroglycerine – 0,5 mg (in terms of 100% substance);
• Auxiliary components: sugar (sucrose) – 7,9 mg, glucose (dextrose) – 9,3 mg, potato starch – 9,3 mg.

Hypoglossal is a part of 1 dose of spray:

• Active agent: nitroglycerine – 0,4 mg;
• Auxiliary components: 95% ethanol (in the form of 1% of solution).

For preparation of infusion solution is a part of 1 ml of a concentrate:

• Active agent: nitroglycerine – 1 mg;
• Auxiliary components: a dextrose, sodium chloride, dihydropotassium phosphate, water for injections.

Indications to use

• Stenocardia (stopping and short prevention of attacks of stenocardia before emotional pressure or an exercise stress);
• Acute myocardial infarction, including (infusion solution) complicated by an acute left ventricular failure;
• Fluid lungs (infusion solution);
• Unstable stenocardia (infusion solution).

Contraindications

Absolute:

• Collapse;
• Age up to 18 years (efficiency and safety of use of Nitroglycerine for this age group of patients are not established);
• Hypersensitivity to drug components.

Depending on a dosage form, additional absolute contraindications to use of Nitroglycerine are the following diseases / states:

• Glyukozo-galaktozny malabsorption (tablets hypoglossal);
• Shock (hypoglossal spray and tablets);
• Cardiogenic shock, except cases of holding actions for maintenance of end diastolic pressure (spray hypoglossal);
• Heavy arterial hypotension with a systolic arterial pressure below 90 mm of mercury. (spray hypoglossal);
• Chronic cardial compression (spray hypoglossal);
• The stenocardia connected with a hypertrophic subaortic stenosis (spray hypoglossal);
• Acute myocardial infarction and chronic heart failure with the low filling pressure of a left ventricle (spray hypoglossal);
• Pericardium tamponade (spray hypoglossal);
• Any states connected with increase in intracranial pressure (spray hypoglossal);
• Heavy stenosis of the mitral and/or aortal valve, primary pulmonary hypertensia (spray hypoglossal);
• Simultaneous use with phosphodiesterase-5 inhibitors, including vardenafit, sildenafit, tadalafit (tablets and spray hypoglossal).

Relative (Nitroglycerine should be applied with care after ratio assessment advantage/risk):

• Hemorrhagic stroke;
• Heavy anemia;
• Thyrotoxicosis;
• Heavy renal failure;
• Closed-angle glaucoma;
• The head injuries postponed in recent time;
• Intracranial hypertensia;
• Cardiac tamponade (tablets hypoglossal and infusion solution);
• Liver failure (tablets hypoglossal and infusion solution), heavy liver failure (spray hypoglossal);
• Arterial hypotension with low systolic pressure – is less than 90 mm of mercury. (tablets hypoglossal and infusion solution);
• Orthostatic hypotension and tendency to development of orthostatic hypotension (spray hypoglossal);
• Alcohol abuse (spray hypoglossal);
• Epilepsy (spray hypoglossal);
• Migraine (spray hypoglossal);
• Chronic cardial compression (tablets hypoglossal and infusion solution);
• The isolated mitral stenosis (tablets hypoglossal and infusion solution);
• Hypertrophic cardiomyopathy (tablets hypoglossal and infusion solution);
• Toxic fluid lungs (infusion solution);
• Idiopathic hypertrophic subaortal stenosis (tablets hypoglossal), aortal stenosis (infusion solution);
• Acute myocardial infarction, chronic heart failure with the low pressure of filling of a left ventricle (a tablet hypoglossal and infusion solution);
• Uncontrollable hypovolemia with a normal or low pulmonary pressure at patients with heart failure (infusion solution);
• Shock, including cardiogenic, except cases with rather high pressure of filling of a left ventricle, including provided with medicines with positive inotropic action or intra aortal counterpulsation (infusion solution);
• Hematencephalon (infusion solution);
• The expressed cerebral atherosclerosis (infusion solution);
• Pregnancy and the period of a lactation (for all forms of drug);
• Advanced age (infusion solution).

Route of administration and dosage

Tablets are hypoglossal

For the prevention of complications Nitroglycerine is recommended to be accepted on doctor's orders.

Drug is accepted (sublingual) under language, holding a tablet in a mouth to a full rassasyvaniye, not swallowing.

Nitroglycerine needs to be accepted at once at emergence of the first signs of development of an attack of stenocardia or before an estimated exercise stress or emotional pressure. A single dose – 1 tablet. At stable stenocardia the effect can occur and from a smaller dose, in this case the tablet rest which did not manage to resolve, is recommended to be spat out. In most cases (at 75% of patients) improvement is noted for the first 3 minutes of use of Nitroglycerine.

If within 5 minutes the attack of stenocardia is not stopped, it is necessary to take 1 more pill.

In cases of lack of therapeutic effect after reception of 2 tablets it is necessary to see a doctor immediately.

Spray hypoglossal

Enter on or under language, it is more preferable – in a sitting position, at breath holding. After a vspryskivaniye spray is not swallowed at once, and held, having closed a mouth for several seconds.

In order to avoid complications Nitroglycerine should be applied on doctor's orders.

At emergence of the first signs of an attack of stenocardia enter 1-2 doses of spray (depending on weight). Introduction of 1 more dose, but no more than 3 doses (1,2 mg) within 15 minutes is in case of need possible.

If after use of 3 doses for 15 minutes the state did not improve, it is necessary to consult with the doctor.

The maximum single dose – 3 doses of spray.

With the preventive purpose appoint on 1 dose in 5-10 minutes prior to estimated loading or a stress.

Before use packaging with spray should not be stirred up. When spraying the bottle needs to be held vertically.

Infusion solution

Speed of intravenous administration of Nitroglycerine is selected individually, considering the arterial pressure, heart rate, the central venous pressure, an ECG and other indicators. Solution should be entered through инфузомат or the automatic doser, allowing to dose precisely it and to control an introduction rhythm.

Administration of Nitroglycerine by means of usual system for transfusion of liquids provides dosage accuracy in the way with calculation of number of drops of the poured liquid. Before introduction previously Solution Nitroglycerini is parted in 0,9% solution of sodium chloride or 5% solution of glucose (dextrose) to concentration of 0,01%. It is not necessary to apply other solvents.

It is reasonable to use glass and polyethylene tubes as active agent on walls of tubes from polyvinylchloride is absorbed (losses can make 40-80%). Solution Nitroglycerini quickly collapses on light therefore the system for transfusion and bottles needs to be shielded lightproof material. Storage of solution in the opened ampoule is not allowed.

Initial rate of administering of solution makes 0,5-1 mg an hour, the maximum speed – 8-10 mg an hour.

The recommended concentration and rate of administering of Nitroglycerine make: 1 mg/h (0,0166 mg/min.) – 24 mg a day via the automatic doser (volume of solution of 1 mg/ml) or 240 mg a day through system for intravenous administration (volume of solution of 0,1 mg/ml); rate of administering – 3-4 drops one minute (1 ml corresponds to 20 drops).

Duration of therapy is defined by clinical indications and can vary from several hours to 2-3 days.

Side effects

• Central nervous system: weakness; seldom – psychotic reactions, uneasiness, a disorientation, block;
• Alimentary system: dryness of a mucous membrane of an oral cavity; seldom – vomiting, nausea, abdominal pain;
• Cardiovascular system: headache, dizziness, heat, tachycardia, lowering of arterial pressure; seldom (in particular at overdose) – cyanosis, an orthostatic collapse, strengthening of symptoms of stenocardia (paradoxical reaction to nitrates); sometimes – a collapse with a loss of consciousness and a bradyarrhythmia;
• Local reactions: burning under language, a dermahemia;
• Allergic reactions: seldom – an itch, skin rash, exfoliative dermatitis;
• Others: seldom – a hypothermia, a sight illegibility, a methemoglobinemia.

Special instructions

It is not necessary to exceed the therapeutic doses specified in the instruction.

Hypoglossal Nitroglitserina contains in 1 tablet ^2,65Ch10-3 GU (grain units).

During therapy perhaps considerable lowering of arterial pressure and development of dizziness upon sharp transition to vertical position from a prone position or sitting, and also in hot weather, during the performing of physical exercises or alcohol intake.

At preservation or considerable expressiveness of an illegibility of sight or dryness of a mucous membrane of an oral cavity treatment needs to be interrupted.

As well as to other organic nitrates, to Nitroglitserin at frequent use accustoming can develop (in this case increase in a dosage will be required).

Expressiveness of a headache during therapy can be reduced by reduction of a dose of drug and/or a concomitant use of validol.

At frequent attacks of stenocardia it is recommended to apply the prolonged medicines of a nitroglyceric row.

During Nitroglycerine use the use of alcoholic beverages is strictly forbidden.

Alcohol is a part of spray hypoglossal that is important for the feeding and pregnant women, patients with functional disturbances of a liver, epilepsy, craniocereberal injuries and other diseases of the central nervous system, and also at an alcohol abuse.

Glucose (dextrose) is a part of infusion solution that patients need to consider with a diabetes mellitus.

At an acute heart failure or an acute myocardial infarction Nitroglycerine should be applied only on condition of careful clinical observation of a condition of patients.

Not to allow increase of attacks of stenocardia it is recommended to avoid sharp drug withdrawal.

For prevention of undesirable lowering of arterial pressure rate of administering of infusion solution of Nitroglycerine needs to be selected individually. Lowering of arterial pressure can be observed not only at selection of rate of administering of solution, but also later, against the background of originally stabilized arterial pressure (control it is necessary to carry out at least 3-4 times an hour throughout all time of infusion).

Undergoing earlier treatment by organic nitrates (isosorbide-5-mononitrate, dinitrate isosorbide) higher dose for obtaining desired hemodynamic effect can be required by patients.

During use of Nitroglycerine it is necessary to be careful at control of motor transport and performance of potentially dangerous types of the works demanding the increased concentration of attention and bystry psychomotor reactions.

Medicinal interaction

At simultaneous use of Nitroglycerine with some medicines there can be following effects:

• Vazodilatatora, antihypertensives, inhibitors of an angiotensin-converting enzyme, inhibitors fosfoyodiyoesterazy-5, blockers of "slow" calcium channels, tricyclic antidepressants, ethanol, diuretics, beta adrenoblockers, monoamine oxidase inhibitors, procaineamide: strengthening of hypotensive effect of nitroglycerine;
• Digidroergotamin: increase in its content in blood and increase in arterial pressure;
• Heparin: decrease in its efficiency;
• Acetylsalicylic acid: increase in level of nitroglycerine in blood and strengthening of its action.

Terms and storage conditions

To store in protected from light, the place, unavailable to children.

Period of validity:

• Tablets are hypoglossal: 2 years at a temperature up to 25 °C;
• Spray hypoglossal: 2 years at a temperature up to 15 °C;
• Concentrate for preparation of solution for infusions: 3 years at a temperature of 5-25 °C.