Izo-Mik concentrate for infusions ampoules 0.1% 10 ml. №10

Description

Izo-Mik ampoules Storage
active substance: isosorbide dinitrate;

1 ml of concentrate contains isosorbide dinitrate 1 mg;

Excipients: sodium chloride, water for injections.

Izo-Mik ampoules Dosage form
Concentrate for solution for infusion.

Basic physical and chemical properties: transparent colorless liquid.

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

Pharmacological properties

Pharmacodynamics.

Isosorbide dinitrate is an antianginal agent, a vasodilator that acts mainly on venous vessels and also relaxes arteries. This reduces the amount of venous return to the heart; this reduces ventricular end-diastolic pressure and volume (preload). The effect on the arteries, and at higher doses – on the arterioles, leads to a decrease in systemic vascular resistance (afterload). This, in turn, facilitates the work of the heart. The effect on both preload and postload further reduces the heart’s need for oxygen. In addition, isosorbide dinitrate causes redistribution of blood flow to the subendocardial parts of the heart if coronary circulation is partially complicated by atherosclerotic lesions. This effect may be due to selective dilatation of large coronary vessels. Dilatation of collateral arteries caused by nitrates can improve perfusion of ischemic areas.

In patients with congestive heart failure, nitrates improve hemodynamics at rest and during exercise. This positive effect includes several mechanisms, including improved valvular regurgitation (by reducing ventricular dilatation) and reduced myocardial oxygen consumption. By reducing the need for oxygen and increasing its supply, the area of ​​myocardial infarction is reduced. Thus, isosorbide dinitrate may be useful for patients with myocardial infarction.

Effects on other organ systems include relaxation of the bronchial muscles, the muscles of the gastrointestinal tract, and the muscles of the biliary and urinary tracts. There are reports of the effect of relaxing the smooth muscles of the uterus.

Mechanism of action

Isosorbide dinitrate acts as a nitric oxide (NO) donor, leading to vascular smooth muscle relaxation by stimulating guanylyl cyclase and subsequently increasing the concentration of cyclic guanosyl monophosphate (cGMP); the latter is considered a mediator of relaxation. CGMP-dependent protein kinase is thus stimulated, resulting in altered phosphorylation of various proteins in smooth muscle cells. This ultimately leads to dephosphorylation of the myosin light chain and reduced contractility.

Pharmacokinetics.

The half-life of isosorbide dinitrate after intravenous infusion is 10 minutes. Isosorbide dinitrate is metabolized in the liver to form isosorbide-2-mononitrate and isosorbide-5-mononitrate with half-lives of 1.5–2 hours and 4–6 hours, respectively. Both metabolites are pharmacologically active. The bioavailability of the isosorbide dinitrate solution is 100%, as with all drugs administered intravenously.

Indication

Symptomatic treatment of unstable angina in addition to standard therapy, long-term therapy of vasospastic angina (Princemetal angina);
acute left ventricular heart failure of various etiologies (weakness of the heart muscle with dysfunction of the left ventricle);
acute myocardial infarction.

Contraindication

Hypersensitivity to isosorbide dinitrate, other nitrate compounds or other components of the drug;
acute circulatory failure (shock, collapse);
cardiogenic shock (except in cases when the final diastolic pressure of the left ventricle is maintained at a sufficient level due to appropriate measures);
hypertrophic obstructive cardiomyopathy;
constrictive pericarditis;
cardiac tamponade;
severe arterial hypotension (systolic blood pressure below 90 mm Hg);
severe hypovolemia;
severe anemia;
the drug should not be used during therapy with phosphodiesterase-5 inhibitors (eg sildenafil, vardenafil, tadalafil). See sections “Features of use” and “Interaction with other drugs and other types of interactions”;
soluble guanylate cyclase stimulant riociguate should not be used during nitrate therapy (see Interaction with other medicinal products and other forms of interaction);
hemorrhagic stroke;
head injury;
diseases accompanied by an increase in intracranial pressure (however, until now, an additional increase in intracranial pressure was observed only after intravenous administration of high doses of glyceryl trinitrate);
aortic and / or mitral stenosis;
angle-closure glaucoma;
hypothermia.