Nitrosorbidum

General characteristics. Structure:

International and chemical names: isosorbide dinitrate; 1,4,3,6-diangidro-D-sorbite dinitrate; main physical and chemical properties: tablets of white color of a ploskotsilindrichesky form with a facet; structure: one tablet contains isosorbide of dinitrate divorced, in terms of 100% of isosorbide dinitrate-0,01 of; excipients: tabletoza-80, кросповидон NF, calcium stearate.

Pharmacological properties:

Nitrosorbidum is a peripheral vasodilator among groups of organic nitrates, anti-anginal means for oral administration. The mechanism of a ddeystviye is connected with release of nitrogen oxide in unstriated muscles of vessels, guanylate cyclase activation, increase in the tsGMF level of vessels, decrease of the activity of a protein kinase that leads to relaxation of unstriated muscles (preferential veins), a short-term lowering of arterial pressure, decrease before / and after loads of a myocardium and need of a myocardium for oxygen. Vsledvstvy dilatations of capillaries blood supply and providing a myocardium with oxygen improves, the heart rhythm can accelerate reflex. Pharmacokinetics. Unlike nitroglycerine Nitrosorbidum is soaked up slowly, has effect of the first passing through a liver. At intake in the form of tablets the beginning of action of Nitrosorbidum is noted in 30-50 min. The maximum effect is observed in 1,5-2 h, the general duration of action makes 4-6 h and more. Bioavailability of 20-25%, volume of distribution of 470 l, nearly 30% of drug it is connected with proteins, the elimination half-life makes 1,2-1,8 h. Drug is metabolized in a liver by subinfluence of glutathione S-transferase with formation of active metabolites 2 and 5 isosorbides of mononitrates. It Vivoditsya by kidneys and through intestines.

Indications to use:

Nitrosorbidum is appointed as anti-anginal means for the prevention of attacks of stenocardia and their treatment, for recovery treatment after a myocardial infarction. Nitrosorbidum is applied also as a peripheral vazodilatator at severe forms of heart failure. Sometimes appoint at the endarteritis and other diseases which are followed by vasomotor spasms.

Route of administration and doses:

Adults accept Nitrosorbidum inside in 30 minutes prior to food on 5-10 mg 3-4 times a day. In some cases according to indications single doses raise to 20-30 mg. At severe forms of heart failure appoint 2 tablets (20 mg) each 4-5 hours. In the form of the usual tablets applied sublingual, drug, as well as nitroglycerine, can stop a stenocardia attack, but much more slowly.

Features of use:

With care apply isosorbide dinitrate at patients with disturbance of mozkovy blood circulation, with an aortal or mitral stenosis, at the patients inclined to orthostatic hypotension, at people of advanced age. During treatment, especially in cases of gradual increase in a dose, control of the ABP and ChSS is necessary. During treatment alcohol intake is not allowed, it is not recommended to manage vehicles, to be engaged in other potentially dangerous types of activity as at regular use of isosorbide dinitrate reduces ability of concentration of attention and speed of psychomotor reactions.

Side effects:

At use of Nitrosorbidum the headache, dizziness, nausea, drowsiness, a hyperemia of integuments, orthostatic hypotension, reflex tachycardia, in isolated cases bradycardia, a collapse, strengthening of stenocardia which pass at reduction of a dose are possible. At prolonged use of Nitrosorbidum tolerance can develop: for its prevention it is recommended to take after 3-6 weeks of regular reception of tablets a break for 3-5 days, having replaced with this time Nitrosorbidum with other anti-anginal means.

Interaction with other medicines:

Simultaneous use of vazodilatator, blockers of calcium channels, beta adrenoblockers, tricyclic antidepressants, neuroleptics, alcohol intake can strengthen hypotensive effect of isosorbide of dinitrate.

Contraindications:

Use of Nitrosorbidum is contraindicated at a stroke (including a hemorrhagic stroke), at a craniocereberal injury, shock, a collapse, the suspended sensitivity to nitrates, a concomitant use with the sildenafily, increased intracranial pressure, the acute period of a myocardial infarction, the expressed hypotension (systolic the ABP less than 100 mm of mercury. diastolichky - a mensha of 60 mm of mercury.), a closed-angle form of glaucoma with the high intraocular pressure (at an open angle glaucoma Nitrosorbidum is not contraindicated). Dinitrate isosorbide use during pregnancy and a lactation is possible only in that case when the expected advantage for mother exceeds potential risk for a fruit or the child.

Overdose:

Depending on extent of overdose hypotension, tachycardia, dizziness, drowsiness, a headache, nausea, vomiting, a diarrhea are observed. It is necessary to wash out a stomach, to give to the patient horizontal position. At the expressed arterial hypotension administration of blood substitutes, noradrenaline or dopamine is possible. At emergence of a methemoglobinemia hemotransfusion, intravenous administration of 10-20 ml of 1% of solution methylene blue is possible.

Storage conditions:

To store in unavailable from children, the dry, cool, protected from light place. A period of validity - 2 years.

Issue conditions:

According to the recipe

Packaging:

On 10 or 20 tablets in planimetric yachetskovy packagings. On the 2nd blister strip packagings No. 20 or on the 4th blister strip packagings No. 10 in a pack.