Nitrospray spray metered for sublingual use 0.4mg / dose, 10ml (200 doses)

- prevention of angina attacks by prophylactic use of the drug before exercise;

- relief of angina attacks;

- Acute left ventricular failure (including acute myocardial infarction).

The drug is recommended to be taken as directed by a doctor in order to avoid complications.

Relief of an attack of angina pectoris

At the first attack of angina pectoris, apply 1 or 2 doses under the tongue. If necessary

can be reapplied at 5 minute intervals. If after taking three doses in

within 15 minutes the attack did not stop, you must immediately consult a doctor.

For prophylactic purposes, 1 dose is used 5-10 minutes before the expected load or stress.

Higher single dose: 4 doses. Highest daily dose: 16 doses.

Rules for taking the drug:

Х sit down if possible

Х remove the protective cap from the cylinder, hold the cylinder upright

Х open your mouth and hold your breath for a few seconds

Х press once on the balloon, directing the stream of the drug under the tongue

Х close your mouth and try not to swallow the drug.

When using for the first time or after a long period of non-use, it is recommended to

by direct application, throw one dose into the air to fill the aerosol chamber.

Nitroglycerin solution 4% - 250 g

(in terms of nitroglycerin) - 10 g

Ethanol - up to 1000 g

(rectified ethyl alcohol)

- hypersensitivity to organic nitrates;

- angle-closure glaucoma;

- severe arterial hypotension;

- increased intracranial pressure due to cerebral hemorrhage or injury;

- simultaneous administration of phosphodiesterase inhibitors;

- age up to 18 years (lack of sufficient clinical data).

Precautions: acute myocardial infarction with low left ventricular filling pressure (risk of low blood pressure and tachycardia, which can increase ischemia), chronic heart failure with low left ventricular filling pressure, severe anemia, thyrotoxicosis, hypertrophic cardiomyopathy (possibly more frequent angina attacks), severe renal failure, liver failure (risk of developing methemoglobinemia).

Trade name of the drug: Nitrosprey

International non-proprietary or group name: nitroglycerin

Dosage form: spray sublingual metered

Composition:

Nitroglycerin solution 4% - 250 g

(in terms of nitroglycerin) - 10 g

Ethanol - up to 1000 g

(rectified ethyl alcohol)

Description: a clear, colorless liquid in a bottle with a mechanical

dosing pump. The determination is carried out immediately after opening the bottle.

Pharmacotherapeutic group: vasodilating agent - nitrate

ATX code: [—01Dј02]

PHARMACOLOGICAL PROPERTIES

Nitroglycerin is an organic nitrogen-containing compound with a predominant venodilating effect.

MECHANISM OF ACTION

The effects of nitroglycerin are due to its ability to release nitric oxide from its molecule, which is a natural endothelial relaxing factor.

Nitric oxide increases the intracellular concentration of cyclic guanosine monophosphatase, which prevents the penetration of calcium ions into smooth muscle cells and causes them to relax.

Relaxation of the smooth muscles of the vascular wall causes vasodilation, which reduces venous return to the heart (preload) and the resistance of the systemic circulation (afterload).

This reduces the work of the heart and myocardial oxygen demand.

Expansion of the coronary vessels improves coronary blood flow and promotes its redistribution in the area with reduced blood circulation, which increases the delivery of oxygen to the myocardium.

A decrease in venous return leads to a decrease in filling pressure, an improvement in blood supply to the subendocardial layers, a decrease in pressure in the pulmonary circulation, and a regression of symptoms in pulmonary edema. Nitroglycerin has a central inhibitory effect on the sympathetic vascular tone, inhibiting the vascular component of the formation of pain syndrome. Nitroglycerin relaxes the smooth muscle cells of the bronchi, urinary tract, gallbladder, bile ducts, esophagus, small and large intestines.

The action begins quickly, the effect develops within 1-1.5 minutes and lasts about 30 minutes.

Pharmacokinetics

Sublingual nitroglycerin is rapidly and completely absorbed from the oral cavity into the systemic circulation.

Bioavailability is 100% with sublingual administration, since УprimaryФ hepatic degradation of the drug is excluded.

The maximum concentration in blood plasma is reached after 4 minutes.

The connection with blood plasma proteins is 60%. It is 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 glycerol.

It is excreted by the kidneys in the form of metabolites.

The total ground clearance is 25-30 l / min. After taking the drug under the tongue, the half-life from blood plasma is 2.5-4.4 minutes. Circulating nitroglycerin is firmly bound to erythrocytes and accumulates in the walls of blood vessels.

The main route of excretion of nitroglycerin is the extraction of metabolites in the urine; less than 1% of the dose is excreted unchanged.

INDICATIONS FOR USE

- prevention of angina attacks by prophylactic use of the drug before exercise;

- relief of angina attacks;

- Acute left ventricular failure (including acute myocardial infarction).

CONTRAINDICATIONS

- hypersensitivity to organic nitrates;

- angle-closure glaucoma;

- severe arterial hypotension;

- increased intracranial pressure due to cerebral hemorrhage or injury;

- simultaneous administration of phosphodiesterase inhibitors;

- age up to 18 years (lack of sufficient clinical data).

Precautions: acute myocardial infarction with low left ventricular filling pressure (risk of low blood pressure and tachycardia, which can increase ischemia), chronic heart failure with low left ventricular filling pressure, severe anemia, thyrotoxicosis, hypertrophic cardiomyopathy (possibly more frequent angina attacks), severe renal failure, liver failure (risk of developing methemoglobinemia).

Pregnancy and lactation

There is no data on the penetration of nitroglycerin into breast milk.

Use during pregnancy and during breastfeeding requires careful

comparison of risk and benefit and should be carried out under strict medical supervision.

DOSAGE AND APPLICATION

The drug is recommended to be taken as directed by a doctor in order to avoid complications.

Relief of an attack of angina pectoris

At the first attack of angina pectoris, apply 1 or 2 doses under the tongue. If necessary

can be reapplied at 5 minute intervals. If after taking three doses in

within 15 minutes the attack did not stop, you must immediately consult a doctor.

For prophylactic purposes, 1 dose is used 5-10 minutes before the expected load or stress.

Higher single dose: 4 doses. Highest daily dose: 16 doses.

Rules for taking the drug:

Х sit down if possible

Х remove the protective cap from the cylinder, hold the cylinder upright

Х open your mouth and hold your breath for a few seconds

Х press once on the balloon, directing the stream of the drug under the tongue

Х close your mouth and try not to swallow the drug.

When using for the first time or after a long period of non-use, it is recommended to

by direct application, throw one dose into the air to fill the aerosol chamber.

SIDE EFFECT

From the side of the cardiovascular system: dizziness, headache, tachycardia, fever, decreased blood pressure; rarely (especially in case of overdose) - orthostatic collapse, cyanosis.

From the digestive system: dry mouth, rarely - nausea, vomiting, abdominal pain.

From the side of the central nervous system: weakness, rarely - anxiety, psychotic reactions, lethargy, disorientation.

Allergic reactions: rarely - skin rash, itching.

Local reactions: flushing of the skin, burning sensation under the tongue.

Others: rarely - blurred vision, hypothermia, methemoglobinemia.

OVERDOSE

Symptoms: headache, decreased blood pressure, orthostatic hypotension, reflex tachycardia, dizziness, facial flushing, vomiting and diarrhea, asthenia, increased drowsiness, feeling hot. Extremely high doses (more than 20 mg / kg) lead to methemoglobinemia, cyanosis, dyspnoea and tachypnea, orthostatic collapse.

Treatment: in mild cases, transferring the patient to a supine position with raised legs.

In severe manifestations of overdose, general methods of treatment of intoxication and shock should be used (replenishment of circulating blood volume, norepinephrine, and / or dopamine, etc.).

The use of epinephrine (adrenaline) is contraindicated.

With the development of methemoglobinemia, the following antidotes and treatment methods can be used:

1. Vitamin C - 1 g as sodium salt or intravenously.

2. Methylene blue intravenously at a dose of up to 50 ml of a 1% solution.

3. Toluidine blue intravenously, first dose 2-4 mg / kg, then 2 mg / kg multiple times.

4. Oxygen therapy, hemodialysis, blood transfusion (exchange).

INTERACTION WITH OTHER DRUGS

Other vasodilators and antihypertensive drugs (beta-blockers, blockers

tori of 'slow' calcium channels), inhibitors of the angiotensin-converting ferhypotensive effect of nitroglycerin.

Nitroglycerin enhances the effect of dihydroergotamine and reduces the effectiveness of heparin.

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

Concomitant use with phosphodiesterase type 5 (PDE 5) inhibitors - sildenafil, tadalafil, vardenafil - may enhance the drug's ability to lower blood pressure.

SPECIAL INSTRUCTIONS

Nitroglycerin enhances the excretion of catecholamines and vanillin mandelic acid in the urine.

Drinking alcoholic beverages while using the drug is strictly prohibited.

Impact on driving and work requiring increased attention

At the beginning of treatment, it is necessary to refrain from driving vehicles and engaging in potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions. In the future, the degree of restrictions is determined individually for each patient.

RELEASE FORM

Spray sublingual dosed 0.4 mg / dose.

10 ml (200 doses) in polypropylene vials equipped with mechanical dosing pumps, nozzles and protective caps.

The bottle, together with the instructions for use, is placed in a cardboard box.

STORAGE CONDITIONS

List B. In the dark place, away from fire, at a temperature not exceeding 30 ? C.

Keep out of the reach of children.

SHELF LIFE

3 years. Do not use after the expiration date indicated on the package.

TERMS OF RELEASE FROM PHARMACIES

Without recipe.

MANUFACTURER / COMPANY ACCEPTING CLAIMS OF CONSUMERS.

JSC 'Pharmstandard-Leksredstva', Russia, 305022, Kursk, st. 2nd Aggregate, 1a / 18.

Tel./Fax: (4712) 34-03-13.