Index of drugs

Prophylaxis and symptomatic treatment of ischemic heart disease. Myocardial infarction.

1 dose of aerosol contains 1.25 mg of isosorbide diazotate. The preparation contains: propylene glycol, anhydrous ethanol.

A drug that widens blood vessels from the group of organic nitrates. The mechanism of action is to provide exogenous nitric oxide to endothelial cells and smooth muscle, which causes vasodilatation. Isosorbide dinitrate, after penetration into the smooth muscle cell, is reduced to NO. Nitric oxide, when combined with the sulfhydryl group, forms a S-nitroso-reagent reacting with guanylate cyclase to form cGMP, which causes vasodilatation. The preparation strongly expands venous and arterial vessels, including coronary arteries. It reduces the inflow of blood to the heart (reduction of preload), reduces the volume and pressure of late tachycardia in the chambers and the pulmonary wedge pressure. The impact on arteries is lower, resulting in a decrease in systemic peripheral resistance and afterload. The reduction of both of these loads leads to a reduction in the oxygen consumption of the heart. The result of these actions is the resolution of coronary pain. After administration to the oral mucosa, the effect of the drug occurs after 1 min and lasts up to 2 h. The variation of the therapeutic effect may depend on the time of administration of the preparation. After administration of the drug in the form of an oral spray, the absorption is very good and almost immediate. Biological availability is on average 40-60%. The maximum concentration is reached after 10-15 minutes. Plasma protein binding reaches 28%. Administration of the drug in the form of an aerosol can significantly reduce the first-pass effect (hepatic metabolism). Biological T_0,5 is about 1 hour.

Hypersensitivity to isosorbide dinitrate, other nitrates, nitrites or any of the excipients. Glaucoma with a narrow angle of perception. acute myocardial infarction with low left ventricular filling pressure (including a fresh myocardial infarction). Hypertrophic cardiomyopathy with narrowing of the outflow path. Clenching pericarditis. Tamponada heart. Acute circulatory failure (shock, vascular collapse). Very low blood pressure (systolic pressure below 90 mmHg). Head injury and cerebral hemorrhage. Severe anemia. Hypovolemia. Concomitant use of phosphodiesterase 5 inhibitors, e.g. sildenafil.

The preparation should be used with caution in patients with hypothyroidism, hypothermia, malnourished patients and patients with severe liver or kidney disease. Special care should be taken in patients with low ventricular filling pressure, aortic or bifurcated valve stenosis and patients with diseases in which there is elevated intracranial pressure - in these patients the preparation should only be used under medical supervision. In patients with glaucoma without obstruction, the preparation can only be used with caution and under the supervision of a physician. Sometimes after taking the preparation (especially in the standing position and in people susceptible to wax) a significant reduction in blood pressure or loss of consciousness may occur - the preparation should be administered particularly carefully to patients with circulatory disorders, orthostatic hypotension, hypotension of other origin, hypovolaemia (eg during treatment with diuretics) or with low systolic pressure. Paradoxically, the drop in pressure after administration of nitrates may be accompanied by bradycardia and aggravation of angina pectoris. Chronic, continuous use of the drug may lead to the weakening or even elimination of its therapeutic effect - it is necessary to keep the daily use of the preparation (preferably nocturnal) lasting at least 8-10 h. During the use of the preparation temporary hypoxia may occur due to the relative redistribution of blood flow to hypoventilation area of ​​alveoli. Especially in patients with coronary artery disease may lead to myocardial ischemia.The preparation contains propylene glycol - its accidental application on the skin may cause irritation. Immediately wash the irritated area of ​​the skin due to the risk of absorbing the solution and the possibility of side effects. The product contains small amounts of ethanol - less than 100 mg per dose.

Pregnancy is not an absolute contraindication to the use of the drug. The preparation can be used during pregnancy only if the expected benefit to the mother outweighs the potential risk to the fetus. Due to the lack of data on the penetration of the drug into milk, special care should be taken during breastfeeding.

Very common: transient headaches (in about 40% of patients, most of them disappear after a few days of treatment, 10% of patients require discontinuation of the preparation). Common: reflexive acceleration of heart rate, dizziness, drowsiness in standing position, drowsiness, low blood pressure in standing position, weakness. Uncommon: significant decrease in blood pressure (may lead to worsening of ischemic heart disease), nausea, vomiting, allergic skin reactions (eg rash), redness of the skin (mainly the face), fainting (sometimes with simultaneous release of the heart rhythm and loss of consciousness) . Very rare: methaemoglobinaemia (after long-term use of very high doses), heartburn, angioneurotic edema, Stevens-Johnson syndrome. Frequency unknown: exfoliative dermatitis, burning of the tongue at the site of administration. Two cases of haemolysis have been described in patients with G-6-PD deficiency. In response to a significant reduction in blood pressure, nausea, vomiting, anxiety, pallor and excessive sweating may occur.

Therapeutically: 1 dose (1.25 mg) is usually used in a coronary pain attack; if after 2-5 minutes the pain persists, the second dose can be used. A maximum of three doses can be given at once. The administration of the preparation can be repeated every 2-3 hours. Prophylactically: 1 dose for 5 minutes before the expected occurrence of coronary pain (in case of coronary pain in typical situations for a given patient). It is recommended that the patient taking the medicine for the first time in his life do so while sitting.