Nitrosorbidum

General characteristics. Structure:

Active agent - isosorbide mononitrate diluted 14.3 mg (in terms of 100% substance) (10.0).

Excipients: lactoses monohydrate, potato starch, talc, calcium stearate.

Pharmacological properties:

Pharmacokinetics. Nitrosorbidum is well absorbed at intake. There is a direct dependence of concentration in blood from a dose of the accepted drug.

Nitrosorbidum is not exposed to effect of "the first passing" through a liver in this connection absolute bioavailability after intake makes 100%. At intake it is slowly soaked up from digestive tract, the effect occurs in 20 — 30 minutes and 3,5 — 5 hours proceed. At reception of a tablet of Nitrosorbidum under language the effect occurs in 2 — 5 minutes and lasts for 1 — 2 hours. After denitration or conjugation in a liver Nitrosorbidum is removed with urine preferential in the form of metabolites. T ½-5 h. It is removed by kidneys in the form of glucuronides.

Pharmacodynamics. Nitrosorbidum belongs to organic nitrates of long action. Nitrosorbidum - vazodilatiruyushchy, vasodilating, anti-anginal means. Causes 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 GPVR (general peripheric vascular resistance), and also has direct coronarodilator effect. Promotes redistribution of a coronary blood-groove in the area with reduced blood supply. At use of drug increase in tolerance to an exercise stress at patients with an ischemic heart disease (coronary heart disease), stenocardia is noted. At heart failure drug promotes unloading of a myocardium due to reduction of preloading. Reduces pressure in a small circle of blood circulation.

Indications to use:

- stenocardia (stopping and prevention of attacks)

- chronic heart failure (as a part of a combination therapy)

- pulmonary hypertensia (as a part of a combination therapy)

Route of administration and doses:

Drug should be accepted inside after food, without chewing, washing down with enough water. During the day it is possible to take (according to the recommendation of the doctor) 3 pill. Duration of administration of drug is established by the doctor. If necessary the course of treatment can repeat.

For avoidance of possible sharp falling of arterial pressure at reception of a tablet under language it is necessary to sit down or lay down.

Features of use:

With care apply at a subaortal stenosis, a pericardis and a cardiac tamponade; aortal and/or mitral stenosis; orthostatic hypotension; the diseases which are followed by increase in intracranial pressure.

When using at patients with initially reduced arterial pressure it is necessary to combine with administration of the drugs possessing positive inotropic action. Control of arterial pressure and heart rate, especially in an initiation of treatment is recommended. In an initiation of treatment persons whose activity demands bystry mental and motor reactions need to observe extra care. It is necessary to draw the attention of the patient that side effects amplify against the background of alcohol intake. For prevention of development of accustoming after 3–6 weeks of regular reception it is recommended to do a break for 3–5 days.

In need of cancellation the dose of drug should be reduced gradually, avoiding sharp cancellation.

At reception of too low dose of drug or at the admission of a single dose reception of a double dose of drug is not allowed.

Nitrosorbidum has to be stored in the dry, cool, protected from light place. As drug is explosive, has to be stored far from fire.

Appointment in the II-III trimester of pregnancy is possible only according to strict indications and under constant medical control.

At administration of drug decline in the ability to bystry mental and motor reactions in this connection, it is not recommended to manage the vehicle is possible and to be engaged in other potentially dangerous types of activity.

Side effects:

- passing headache

- nausea, vomiting, emergence of feeling of easy burning of language, dryness of a mucous membrane of an oral cavity is possible

- allergic reactions - (pour) skin manifestations

- lowering of arterial pressure and/or orthostatic arterial hypotension

- collapse, bradyarrhythmia

- tachycardia, dizziness, weakness

- exfoliative dermatitis.

Are possible:

- the considerable lowering of arterial pressure which is followed by strengthening of symptoms of stenocardia

- short-term hyperemia or pallor of integuments

- increase in intraocular pressure

- motive concern

- involuntary urination

- syndrome of "cancellation".

Interaction with other medicines:

At simultaneous use with vazodilatator, tricyclic antidepressants, and also alcohol strengthening of hypotensive effect up to an orthostatic collapse is possible (its early symptoms — dizziness, weakness, etc.). Barbiturates accelerate biotransformation and reduce concentration of Nitrosorbidum in blood.

Therefore it is necessary to follow Regulations of Admission of Nitrosorbidum and with care to combine it with the specified drugs.

Against the background of long reception of Nitrosorbidum reduction of activity of nitroglycerine is possible.

The adsorbents knitting and enveloping means reduce absorption from digestive tract. Anti-hypertensive means (beta adrenoblockers, antagonists of calcium, other vazodilatator), dihydroergotamine, procaineamide, quinidine, tricyclic antidepressants, neuroleptics, a sildenafila citrate strengthen hypotension, sympathomimetics reduce anti-anginal effect, the combination with atropine increases probability of increase in intraocular pressure.

Contraindications:

- hypersensitivity to nitro compounds or one of components

- closed-angle form of glaucoma

- the increased intracranial pressure

- acute disorder of cerebral circulation

- an acute myocardial infarction or heart failure with the low filling pressure of a left ventricle

- the expressed arterial hypotension (systolic arterial pressure less than 90 mm of mercury)

- stenosis of aortal or mitral valves

- cardiogenic shock

- vascular collapse

- hypertrophic subaortic stenosis

- a hemorrhagic stroke or recently postponed head injury

- primary pulmonary hypertensia

- toxic fluid lungs

- anemia

- hyperthyroidism

- deficit глюкозо−6-фосфатдегидрогеназы

- pregnancy (I trimester) and feeding by a breast

- children's age up to 18 years

- simultaneous use of inhibitors of phosphodiesterase 5 of type (sildenafit, vardenafit, tadalafit).

Overdose:

Symptoms: a methemoglobinemia (cyanosis of lips and nails, an anoxia), severe dizziness or a syncope, a collapse, feeling of pressure in the head, weakness, an asthma, bradycardia, the increased body temperature, increase in intracranial pressure, a spasm, nausea, vomiting, diarrhea, диспноэ, visual frustration.

Treatment: a gastric lavage, at a methemoglobinemia — appointment in/in ascorbic acid 1 of in/in, 1% of solution a metiltioniniya (methylene blue) 1-2¼ú/kg (to 50 ml) in/in, an oksinogenoterapiya, a hemodialysis, exchange hemotransfusion, symptomatic therapy.

Storage conditions:

To store in the dry, protected from light place, at a temperature not above 30 °C. To store in the place, unavailable to children!

Issue conditions:

According to the recipe

Packaging:

On 10 tablets in a blister strip packaging from a film of polyvinyl chloride and aluminum foil.

Blister strip packagings place in boxes from a cardboard. Put the approved instructions on a medical use in each box in the state and Russian languages.