Izo-Mik sublingual tablets 5 mg. №50 vial

Description

Izo-Mik sublingual Storage
active substance: isosorbide dinitrate;

1 tablet contains isosorbide dinitrate 5 mg;

excipients: corn starch; lactose monohydrate; sorbitol (E 420); magnesium stearate.

Izo-Mik sublingual Dosage form
Sublingual tablets.

Basic physical and chemical properties.

Tablets of white color, with a flat surface, with a facet.

Izo-Mik sublingual Pharmacotherapeutic group
Drugs that affect the cardiovascular system. Cardiac drugs. Vasodilators used in cardiology. Organic nitrates. Isosorbide dinitrate. ATX code C01D A08.

Pharmacological properties
Pharmacodynamics.

Peripheral vasodilator with a predominant effect on venous vessels. Antianginal agent. The mechanism of action is associated with the release of the active substance – nitric oxide. In vascular smooth muscle, nitric oxide activates guanylate cyclase and increases the level of cyclic 3 ¢, 5 ¢ -guanosine monophosphate, which causes smooth muscle relaxation. Under the influence of isosorbide dinitrate, arterioles and precapillary sphincters relax to a lesser extent than large arteries and veins. The action of isosorbide dinitrate is mainly related to the reduction of myocardial oxygen demand by reducing preload (dilation of peripheral veins and reduced blood flow to the right atrium) and postload (reduction of total peripheral vascular resistance), as well as direct coronary dilatation. Isosorbide dinitrate promotes redistribution of coronary blood flow in the area with reduced blood supply. Increases exercise tolerance in patients with coronary heart disease, angina. In heart failure, the drug helps to unload the myocardium by reducing preload, reduces the pressure in the small circle of blood circulation.

Pharmacokinetics.

With sublingual administration of isosorbide dinitrate is rapidly absorbed and has a hemodynamic and antianginal effect in 2-5 minutes (ie relief of angina is observed in 2-5 minutes after application, due to the peculiarities of the production of sublingual form of the drug). The maximum concentration of the active substance in plasma is reached in 5-6 minutes. The maximum effect of isosorbide dinitrate tablets when administered sublingually occurs at 10-15 minutes. The duration of therapeutic action of the drug is 60-120 minutes. Short-acting drug. Isosorbide dinitrate is metabolized to form the active metabolite of isosorbide-5-mononitrate, the half-life of which is 5 hours, and isosorbide-2-mononitrate with a half-life of 2.5 hours. The half-life of isosorbide dinitrate with sublingual administration of the drug is 1 hour. 80 to 100% of the administered single dose is excreted in the urine within 24 hours, preferably in the form of metabolites. This form is especially important in patients with low systemic bioavailability of isosorbide dinitrate tablets when taken orally.

Indication
Relief and prevention of angina attacks.

To prevent angina attacks, the drug is used before the expected physical or emotional stress.

Contraindication
Hypersensitivity to the components of the drug;
severe arterial hypotension (systolic blood pressure – less than 90 mm Hg, diastolic blood pressure – less than 60 mm Hg);
acute vascular insufficiency (collapse, shock);
hypertrophic obstructive cardiomyopathy;
constrictive pericarditis;
cardiac tamponade;
toxic pulmonary edema;
conditions accompanied by increased intracranial pressure (including hemorrhagic stroke, traumatic brain injury);
angle-closure glaucoma with high intraocular pressure;
bleeding, hypovolemia (isosorbide dinitrate, reducing venous return, may provoke syncope);
primary lung disease (due to the risk of hypoxemia, which may be caused by redistribution of blood flow in the area of ​​hyperventilation), pulmonary heart;
severe anemia;
acute myocardial infarction with low ventricular filling pressure;
severe liver and / or kidney dysfunction, hyperthyroidism;
concomitant use of phosphodiesterase inhibitors, such as sildenafil, tadalafil, vardenafil.