Nitrosorbidum

General characteristics. Structure:

Active ingredient: 10 mg or 20 mg of isosorbide of dinitrate.

Excipients: sugar (sucrose), potato starch, calcium stearate.

Pharmacological properties:

Pharmacodynamics. A peripheral vazodilatator with preferential influence on venous vessels. Stimulates formation of nitrogen oxide (the endothelial running-down factor) in an endothelium of vessels causing activation of intracellular guanylate cyclase, increase in tsGMF (a vazodilatation mediator) is a consequence of what. Reduces the need of a myocardium for oxygen due to decrease in preloading and an afterload (reduces the final diastolic volume of a left ventricle and reduces the systolic tension of its walls).

Possesses coronarodilator action. Reduces inflow of blood to the right auricle, promotes pressure decrease in a small circle of blood circulation and regression of symptoms at a fluid lungs. Promotes redistribution of a coronary blood-groove in the area with reduced blood circulation. Increases tolerance to an exercise stress at patients with coronary heart disease, stenocardia.

Expands vessels of a brain, a firm meninx that can be followed by a headache. As well as to other nitrates, cross tolerance develops. After cancellation (a break in treatment) sensitivity to it is quickly recovered.

The beginning of action after sublingual reception or chewing – 2-5 min., after intake – 15-40 min. Action duration – 1-2 h and 4-6 h respectively.

Pharmacokinetics. Absorption – high. Bioavailability at intake – 22% (effect of "the first passing" through a liver), at sublingual use – 60%. Time of achievement of the maximum concentration at oral administration – 1 h. Communication with proteins of a blood plasma – 30%. An elimination half-life at oral administration – 4 h. It is metabolized in a liver to 2 active metabolites: (isosorbide-5-mononitrate (75-85%), which elimination half-life – 5 h, and isosorbide-2-mononitrate (15-25%) with an elimination half-life – 2,5 h). It is removed by kidneys (almost completely in the form of metabolites).

Indications to use:

Prevention and treatment of attacks of stenocardia, recovery treatment after a myocardial infarction (as a part of a combination therapy), chronic heart failure (as a part of a combination therapy).

Route of administration and doses:

Drug is appointed inside or sublingual. For prevention of attacks of stenocardia the initial dose of drug inside makes 10 mg of 4-5 times a day. At insufficient efficiency from the 3-5th day of treatment it is possible to increase a dose of drug to 60-120 mg a day.

For stopping of an attack of stenocardia take 1 pill (10 mg) of Nitrosorbidum sublingual (for action acceleration reasonablly to chew a tablet).

As a part of a combination therapy of chronic heart failure appoint 10-20 mg 3-4 times a day. Duration of treatment is defined in each case individually. In case of need drug withdrawal is made gradually.

Features of use:

Use at pregnancy and in the period of a lactation. It is necessary to apply only after careful weighing of a ratio of advantage and risk, connected using drug as experience of use for pregnant women and the feeding women is insufficient. Category of action on the Page fruit.

During treatment by Nitrosorbidum, especially in case of gradual increase in a dose, control of arterial pressure and heart rate is necessary.

Frequent appointment and high doses can cause tolerance development; in this case cancellation on 24-48 h is recommended, or after 3-6 weeks of regular reception to do a break for 3-5 days, having replaced with this time Nitrosorbidum with other anti-anginal means.

During treatment by Nitrosorbidum it is necessary to abstain from driving of motor transport and occupations potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

To avoid sharp drug withdrawal, to reduce a dose gradually. During treatment by drug it is necessary to exclude alcohol intake.

Side effects:

From cardiovascular system: "nitrate" headache, dizziness, dermahemia of the person, feeling of heat, tachycardia, decrease in the ABP. In rare instances – "paradoxical" strengthening of attacks of stenocardia and a collapse.

From digestive tract: nausea, vomiting, emergence of feeling of easy burning of language, dryness in a mouth is possible.

From a nervous system: constraint, drowsiness, a sight illegibility, decline in the ability to bystry mental and motor reactions (especially in an initiation of treatment). In rare instances – brain ischemia.

Allergic reactions: skin rash.

Others: tolerance development (including cross to other nitrates), exfoliative dermatitis.

Interaction with other medicines:

Pharmakodinamicheskoye: under the influence of alpha adrenoblockers (dihydroergotamine, etc.) decrease in expressiveness of anti-anginal effect of Nitrosorbidum is possible (excessive decrease in the ABP and, as a result, coronary perfusion).

Combination of Amiodaronum and other medicines, such as, propranolol, blockers of "slow" calcium channels (verapamil, nifedipine, etc.) and Nitrosorbidum is rational for treatment of coronary heart disease.

The combined use of acetylsalicylic acid and Nitrosorbidum promotes improvement of coronary circulation.

At combined use of Nitrosorbidum with anti-hypertensive means, vazodilatator, antipsychotic means (neuroleptics), tricyclic antidepressants, novokainamidy, ethanol, quinidine, beta adrenoblockers, blockers of "slow" calcium channels and dihydroergotamine strengthening of expressiveness of decrease in the ABP is possible.

At the combined use of Nitrosorbidum with m-holinoblokatorami (atropine, etc.) the probability of increase in intraocular pressure increases. At a concomitant use with sildenafily (Viagra) perhaps expressed lowering of arterial pressure.

Pharmacokinetic: the adsorbents knitting and enveloping means reduce absorption of Nitrosorbidum in digestive tract.

Contraindications:

Hypersensitivity to organic nitrates, a hemorrhagic stroke, the expressed arterial hypotension (systolic the ABP less than 100 mm hg, diastolic the ABP less than 60 mm hg), a collapse, shock, an acute myocardial infarction with the expressed arterial hypotension, the increased intracranial pressure, a toxic fluid lungs, a closed-angle form of glaucoma with high intraocular pressure, a craniocereberal injury, age up to 18 years (efficiency and safety are not established).

With care: a hypertrophic cardiomyopathy (increase of attacks of stenocardia is possible), chronic cardial compression, a cardiac tamponade; an aortal and/or mitral stenosis, the expressed liver failure (risk of development of a methemoglobinemia), the expressed renal failure, a hematencephalon, an acute myocardial infarction (risk of a lowering of arterial pressure and tachycardia which can strengthen ischemia), heavy anemia, a hyperthyroidism, patients with tendency to orthostatic hypotension, elderly patients, the raised digestive tract peristaltics, a sprue.

Overdose:

Symptoms: collapse, faint, headache, dizziness, heart consciousness, visual frustration, dermahemia, perspiration, nausea, vomiting, diarrhea, methemoglobinemia (cyanosis, anoxia), hyperpnea, диспноэ, bradycardia, craniocereberal hypertensia, paralysis, coma.

Treatment: gastric lavage; at a methemoglobinemia – in/in 1% solution of methylene blue, 1-2 mg/kg. Symptomatic therapy (Epinephrinum and related to it connections are ineffective).

Storage conditions:

List B. To store in the dry, cool, protected from light place unavailable to children, far from fire. A period of validity - 3 years. Not to use after the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Tablets on 10 mg and 20 mg. On 10 tablets in planimetric bezjyacheykovy packaging. On 10, 20, 30, 50 tablets in a blister strip packaging. On 30, 50 tablets in a glass jar of dark glass or in bank of polymeric. Each can or 1, 2, 3, 5, 10 planimetric strip or planimetric bezjyacheykovy packagings with the application instruction in a pack.