Izocet spray 15 ml. 300 doses

Description

Izocet spray Composition
active substance: isosorbide dinitrate;

1 dose (1 press on the nebulizer) is 0.05 ml of a solution containing 1.25 mg of isosorbide dinitrate;

1 bottle with 15 ml (12.7 g) of solution contains 375 mg of isosorbide dinitrate;

excipients: ethanol, macrogol 400.

Izocet spray Dosage form
Oromucous spray.

Basic physical and chemical properties: transparent, colorless, mobile solution.

Izocet spray Pharmacotherapeutic group
Vasodilators used in cardiology. Organic nitrates. ATX code C01D A08.

Pharmacodynamics
Isosorbide dinitrate causes relaxation of vascular smooth muscles, leading to vasodilation. this relaxes both peripheral arteries and veins. this effect promotes venous “POOLING” of blood and reduces venous return to the heart; thus, ventricular end-diastolic pressure and volume (preload) are reduced. the effect on arteries, and when high doses are used, on arterioles, leads to a decrease in systemic vascular resistance (afterload). this, in turn, makes it easier for the heart.

The effect on both pre- and afterload leads to a further decrease in heart oxygen consumption.

Isosorbide dinitrate also causes a redistribution of blood flow in the subendocardial parts of the heart if coronary circulation is partially obstructed by atherosclerotic lesions. This effect is probably due to the selective dilatation of large coronary vessels. Dilation of collateral arteries caused by nitrates can improve post-stenotic myocardial perfusion. In addition, nitrates counteract the occurrence and eliminate coronary spasm.

In patients with congestive heart failure, nitrates improve hemodynamics at rest and during exercise. This beneficial effect is achieved through a number of pathogenetic mechanisms, including improved valve regurgitation (due to a decrease in the ventricle) and a decrease in myocardial oxygen demand.

Due to a decrease in oxygen demand and an increase in its intake, nitrates limit myocardial damage during a heart attack. Thus, the use of isosorbide dinitrate may be beneficial for patients with myocardial infarction.

Effects on other organ systems include relaxation of the muscles of the bronchi as well as the muscles of the gastrointestinal tract, biliary tract, and urinary tract. There are also reports of relaxation of the smooth muscles of the uterus.

Mechanism of action

Like all organic nitrates, isosorbide dinitrate acts as a donor of nitric oxide (NO). Nitric oxide causes relaxation of vascular smooth muscles by stimulating guanylyl cyclase and further increasing the concentration of intracellular cGMP. Thus, cGMP-dependent protein kinase is stimulated, and as a result, the phosphorylation of proteins in the smooth muscle cell is altered. This, in turn, causes dephosphorylation of myosin light chains and a decrease in contractility.

Pharmacokinetics
After injection into the oral cavity, the active substance isosorbide dinitrate is absorbed very quickly. The action of the drug begins within 1-3 minutes after application, C max in blood plasma is achieved within 3-6 minutes. T ½ is 30-60 minutes. Within 90-120 minutes, the concentration in the blood plasma returns to the initial level. Isosorbide dinitrate is metabolized to form isosorbide-2-mononitrate and isosorbide-5-mononitrate with T ½, which are 1.5-2 hours and 4-6 hours, respectively. Both metabolites are inactive.

When isosorbide is used in the oral cavity, dinitrate undergoes rapid metabolism in the liver, due to which a significantly higher bioavailability is achieved – 60-100% (with oral administration – 15-30%).

Indications
Assign:

for the prevention and treatment of angina attacks;
with acute myocardial infarction;
with acute left ventricular heart failure.
Contraindications
The drug is contraindicated in:

hypersensitivity to isosorbide dinitrate, other nitrate compounds or other components of the drug;
acute vascular insufficiency (shock, vascular collapse);
cardiogenic shock, if it is impossible to correct the end diastolic pressure of the left ventricle with the help of appropriate measures;
severe hypotension (systolic blood pressure 90 mm Hg);
hypertrophic obstructive cardiomyopathy;
hemodynamic;
tamponade.
During therapy with nitrates, phosphodiesterase inhibitors (for example, sildenafil – see Interaction with other medicinal products) should not be used.