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

Description:Transparent, colorless liquid, contained in a vial with a mechanical metering pump. The determination is carried out immediately after opening the vial.

Pharmacotherapeutic group:vasodilator - nitrate

ATX: & nbsp

C.01.D.A.02 Nitroglycerine

Pharmacodynamics:

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 from its molecule nitric oxide, 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 the smooth muscle cells and causes their relaxation.

Relaxation of the smooth muscles of the vascular wall causes vasodilation, which reduces the venous return to the heart (prednaguzka) and resistance to a large range of blood circulation (postload). This reduces the work of the heart and the need for myocardium in oxygen.

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.

Reduction of venous return leads to a decrease in filling pressure, improved blood supply to the subendocardial layers, reduced pressure in the small circulation and regression of symptoms in pulmonary edema.

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

Nitroglycerin relaxes the smooth muscle cells of the bronchi, urinary tract, gall bladder, bile duct, esophagus, small and large intestine. The action begins quickly, the effect develops within 1-1.5 minutes and lasts about 30 minutes.

Pharmacokinetics:

Nitroglycerin for sublingual use is rapidly and completely absorbed from the oral cavity into the systemic bloodstream.Bioavailability is 100% with sublingual admission, as it excludes the "primary" hepatic degradation of the drug. The maximum concentration in the blood plasma is reached after 4 minutes. The connection with plasma proteins is 60%. 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. After taking the drug under the tongue, the elimination half-life from the blood plasma is 2.5-4.4 minutes. Circulating nitroglycerine is firmly connected with erythrocytes and accumulates in the walls of the vessels. The main way to excrete nitroglycerin is the extraction of metabolites with urine; less than 1% of the dose is allocated in unchanged form.

Indications:

- Prevention of angina attacks by prophylactic application of the drug before physical exertion;

- relief of angina attacks;

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

Contraindications:

- Hypersensitivity to organic nitrates;

- the closed-angle form of glaucoma;

- severe arterial hypotension;

- increased intracranial pressure due to hemorrhage in the brain or injury;

- simultaneous administration of phosphodiesterase inhibitors.

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

Carefully:

Acute myocardial infarction with low left ventricular filling pressure (risk of lowering blood pressure and tachycardia that may increase ischemia), chronic heart failure with low left ventricular filling pressure, severe anemia, trihotoxicosis, hypertrophic cardiomyopathy (possibly an increase in angina attacks), severe renal failure, hepatic insufficiency (risk of development of methaemoglobinemia).

Pregnancy and lactation:

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

Application during pregnancy and during breastfeeding requires careful comparison of risk and benefit and should be carried out under strict medical supervision.

Dosing and Administration:

The drug is recommended to take as directed by the doctor to avoid complications.

Stenocardia

At the first attack of angina, apply 1 or 2 doses under the tongue.If necessary, you can apply again with 5-minute intervals. If, after taking three doses for 15 minutes, the attack is not stopped, you should immediately consult a doctor.

For preventive purposes 1 dose is applied 5-10 minutes before the expected load or stress.

The highest single dose: 4 doses. The highest daily dose: 16 doses.

Rules for taking the drug:

- if possible sit down remove the protective cap from the cylinder, keep the cylinder upright;

- open your mouth and hold your breath for a few seconds;

- click once on the balloon, directing the jet of the drug under the tongue;

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

For first use or after prolonged non-use, it is recommended that a single dose be dumped into the air before the direct application to fill the aerosol chamber.

Side effects:

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

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

From the central nervous system: weakness, rarely - anxiety, psychotic reactions, inhibition, disorientation.

Allergic reactions: rarely - skin rash, itching.

Local Reactions: hyperemia of the skin, burning under the tongue

Other: rarely - blurred vision, hypothermia, methemoglobinemia.

Overdose:

Symptoms: headache, lowering of blood pressure, orthostatic hypotension, reflex tachycardia, dizziness, redness of the face, vomiting and diarrhea, asthenia, increased drowsiness, a feeling of heat. Extremely high doses (more than 20 mg / kg) lead to methemoglobinemia, cyanosis, dyspnea and tachypnea, orthostatic collapse.

Treatment: In mild cases, the patient is transferred to a prone position with raised legs. In severe cases of overdose, general methods of treatment of intoxication and shock should be used (replenishment of the volume of circulating blood, norepinephrine and / or dopamine, etc.).

The use of epinephrine (adrenaline) is contraindicated.

When casting methaemoglobinemia, the following antidotes and treatment methods can be used:

1. Vitamin C - 1 g in the form of sodium salt or intravenously.

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

3. Toluidine blue intravenously, the first dose 2-4 mg / kg, then repeatedly 2 mg / kg.

4. Oxygenotherapy, hemodialysis, blood transfusion.

Interaction:

Other vasodilators and anti-hypertensive medications (beta adrenoblockers, slow calcium channel blockers), angiotensin converting enzyme (ACE) inhibitors, antipsychotics, tricyclic antidepressants, monoamine oxidase (MAO) inhibitors, procainamide and ethanol can enhance the hypotensive effect of nitroglycerin.

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

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

Simultaneous reception with inhibitors of phosphodiesterase type 5 (PDE-5) - sildenafil, tadalafil, vardenafil - may increase the ability of the drug to lower blood pressure.

Special instructions:

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

The use of alcoholic beverages during the use of the drug is strictly prohibited.

Effect on the ability to drive transp. cf. and fur:At the beginning of treatment it is necessary to refrain from driving motor vehicles and practicing potentiallydangerous activities that require increased concentration and speed of psychomotor reactions. In the future, the degree of restriction is determined individually for each patient.

Form release / dosage:Spray sublingual dosed, 0.4 mg / dose.

Packaging:

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

The bottle together with the instruction for use is placed in a pack of cardboard.

Storage conditions:

In a place protected from light, away from fire, at a temperature not exceeding 30 ° С.

Keep out of the reach of children.

Shelf life:

3 years.

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

Terms of leave from pharmacies:Without recipe

Registration number:LSR-001698/07

Date of registration:24.07.2007

Expiration Date:Unlimited

The owner of the registration certificate:PHARMSTANDART-FORESTRY, OJSC PHARMSTANDART-FORESTRY, OJSC Russia

Manufacturer: & nbsp

PHARMSTANDART-FORESTRY, OJSC Russia

Information update date: & nbsp04.12.2016

Illustrated instructions

Instructions

Nitrospray (Nitrospray)