Iso-Mik 5 mg tablets №50

Iso-Mik instructions for use

Composition

active ingredient: isosorbide dinitrate; 1 tablet contains isosorbide dinitrate 5 mg;
auxiliary substances: corn starch, lactose monohydrate, sorbitol (E 420) magnesium stearate.

Dosage form

Tablets sublingual.

Pharmacological group

Means that affect the cardiovascular system. Vasodilators used in cardiology. Organic nitrates. The code of automatic telephone exchange С01D А08.

Indications

Cupping and prevention of angina attacks.

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

Contraindications

• Hypersensitivity to the drug components
• severe arterial hypotension (systolic blood pressure is less than 90 mm Hg, diastolic blood pressure is 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, craniocerebral injury);
• glaucoma with high intraocular pressure;
• bleeding, hypovolemia (isosorbide dinitrate, reducing venous return, can provoke fainting)
• primary pulmonary diseases (because of the risk of hypoxemia, which can be caused by redistribution of blood flow in the hyperventilation zone), pulmonary heart,
• severe anemia
• acute myocardial infarction with low ventricular filling pressure;
• severe violations of the liver and / or kidney function, hyperthyroidism
• simultaneous use of phosphodiesterase inhibitors, for example sildenafil, tadalafil, vardenafil.

Dosing and Administration

Iso-Meek 5 mg is applied sublingually (under the tongue). The single dose is 5-10 mg.

To stop an attack of angina or before the expected emotional and physical stress, which usually causes an attack, put one tablet under the tongue and hold in the mouth until it dissolves. If necessary, you can repeat the drug in 10-15 minutes.

Adverse Reactions

From the side of the cardiovascular system: reflex tachycardia is possible, short-term hyperemia of the face, arterial hypotension in some cases - increased angina attacks, bradycardia, cardiac rhythm and syncope, alveolar hypoventilation followed by hypoxemia and risk of hypoxia / myocardial infarction in patients with ischemic heart disease.

On the part of the digestive system: nausea, vomiting, the appearance of a feeling of mild burning tongue, dry mouth, heartburn, constipation.

From the nervous system: dizziness, drowsiness, headache (with constant treatment usually disappears in 1-2 weeks after the start of therapy), collapse, hemorrhage in the pituitary gland in patients with undiagnosed pituitary tumor.

Allergic reactions: skin rash, itching, pale skin, Stevens-Johnson syndrome, and Quincke's edema.

From the side of the organ of vision: blurred vision, glaucoma. Cases of visual hallucinations, narrowing of the field of vision were reported.

General disorders: sweating, weakness, hot flashes, peripheral edema, hematologic side effects, including methemoglobinemia, isosorbide dinitrate-induced hemolytic anemia in a patient with concomitant insufficiency of glucose-6-phosphate dehydrogenase.

The cases of tolerance development to isosorbide dinitrate, as well as cross tolerance to other nitrates have been described.

Long-term use of high doses and / or a reduction in the interval between doses may lead to a decrease or even a loss of the effect of the drug.

There have been reports of a significant increase in renin and aldosterone levels in blood plasma associated with a decrease in glomerular filtration rate and clearance of osmotically free water in patients with cirrhosis, especially with ascites.

Overdose

Symptoms: pallor, increased sweating, weak pulse filling, hyperthermia, diarrhea, reflex tachycardia, headache, fits of weakness, dizziness, palpitations, nausea, vomiting, arterial hypotension, numbness.

It is possible the formation of methemoglobin, which is accompanied by tachypnea, a sense of anxiety, loss of consciousness, cardiac arrest.

With excessive doses, it is possible to increase intracranial pressure with the appearance of cerebral symptoms, including by the court.

Treatment: with arterial hypotension the patient should be given a horizontal position with raised lower limbs. If blood pressure is not normalized, the volume of circulating blood is corrected, in severe cases, dopamine and sympathomimetics are indicated. The use of epinephrine (adrenaline) is contraindicated.

With methemoglobinemia depending on the severity of the condition, antidotes can be used: vitamin C (1 g orally), methylene blue (up to 50 ml 1% solution intravenously), toluidine blue (first 2-4 mg / kg body weight intravenously, then - depending of the severity of the condition), as well as oxygen therapy, transfusion therapy, hemodialysis.

Use during pregnancy and lactation

Data on the safety of isosorbide dinitrate during pregnancy is not enough. In the first trimester of pregnancy, the use of the drug is contraindicated. In the II-III trimesters of pregnancy, the drug should only be used taking into account the relationship expected benefit for the mother / potential risk to the fetus.

If you need to use the drug during breastfeeding, breastfeeding should be discontinued.

Children

Experience of use in children is absent.

Application features

Use with caution for the treatment of patients with circulatory disorders, with aortic and / or mitral stenosis; patients prone to orthostatic hypotension; patients with symptoms of ischemia in various vascular beds, which occur against a background of lowering blood pressure. During the treatment period, especially in the case of a gradual increase in the dose, control of blood pressure and heart rate is necessary. Frequent administration of high doses can cause "nitrate" tolerance to isosorbide dinitrate or cross-tolerance to other nitrates. To overcome the tolerance to isosorbide dinitrate (if possible - the abolition of nitrates), it is recommended not to increase the frequency or dose of the drug, and to refrain from taking it for 16-24 hours, replacing it for this time with other antianginal drugs, and then continue treatment as monotherapy in conventional doses or in combination with other drugs. (It is recommended to take breaks with regular administration of the drug after 4-6 weeks.) The onset of "nitrate" headache at the beginning of treatment can be prevented by a gradual increase in the dose or by the appointment of Validol and non-narcotic analgesics (acetylsalicylic acid, paracetamol, analgin). During treatment should refrain from drinking alcohol.

The drug should be administered with caution to patients with hypothyroidism, hypothermia, malnutrition, concomitant diseases and other medications.

To cancel the drug should be gradually reducing the dose. To prevent arterial hypotension and "nitrate" headache, treatment should be started with a minimal dose. Treatment with the drug may cause the development of orthostatic reactions, often occur with the simultaneous use of alcohol or other vasodilators. In patients with a deficiency of glucose-6-phosphate dehydrogenase, the development of acute hemolysis (favism) with the use of isosorbide dinitrate is possible.

The intake of isosorbide dinitrate can affect the results of colorimetric determination of cholesterol.

The ability to influence the reaction rate when driving vehicles or other mechanisms

During the period of treatment, it is not recommended to drive vehicles and engage in other potentially hazardous activities, since regular application of dinitrate isosorbide reduces the ability to concentrate and the speed of psychomotor reactions.

Interaction with other drugs and other interactions

Hypotensive drugs (eg, beta-blockers, ACE inhibitors, calcium antagonists, vasodilators), phenothiazines, other nitrates / nitrites, quinidine, novocainamide, cyclic antidepressants, MAO inhibitors, narcotic analgesics- potentiation of hypotensive action of isosorbide dinitrate, orthostatic collapse possible.

Dysopyramide - may reduce the effectiveness of isosorbide dinitrate.

Heparin - it is possible to reduce its anticoagulant effect.

Hydralazine - improves cardiac output in heart failure when combined with isosorbide dinitrate.

Atropine and other drugs that have M-cholinolytic action (eg etatsizin, etmozin) - it is possible to reduce the vasodilating action of isosorbide dinitrate and increase intraocular pressure.

Donators of sulfhydryl groups (captopril, acetylcysteine, unitiol) restore reduced sensitivity to the drug.

Inhibitors of phosphodiesterase (sildenafil) - use with nitrates is prohibited for the possible development of uncontrolled arterial hypotension.

Sympathomimetics (epinephrine, ephedrine, norepinephrine, histamine, acetylcholine, naphthysine, mezaton, isadrine, etc. Antihypertensive drugs) - it is possible to reduce the antianginal effect of isosorbide dinitrate.

Pharmacological properties

Pharmacodynamics.

Peripheral vasodilator with predominant effect on venous vessels. Antianginal remedy. The mechanism of action is associated with the release of the active substance - nitric oxide. In smooth muscle vessels, nitric oxide activates guanylate cyclase and increases the level of cyclic 3 ¢, 5 ¢ -guanosine monophosphate, which leads to relaxation of smooth muscles. Under the influence of isosorbide dinitrate, arterioles and precapillary sphincters relax less than large arteries and veins. The effect of isosorbide dinitrate is mainly due to a decrease in the demand for myocardium in oxygen due to a reduction in preload (peripheral veins and a decrease in the flow of blood to the right atrium) and postnagruzki (a decrease in the total peripheral vascular resistance), as well as with direct coronary dilatation.Isosorbide dinitrate promotes redistribution of coronary blood flow in the area with reduced blood supply. Increases tolerance to physical activity in patients with ischemic heart disease, angina pectoris. With heart failure, the drug helps to relieve the myocardium by reducing the preload, reduces pressure in the small circle of the circulation.

Pharmacokinetics.

With sublingual application of isosorbide, dinitrate is rapidly absorbed and exhibits a hemodynamic and antianginal effect in 2-5 minutes (i.e., cupping of an attack of angina occurs after 2-5 minutes after application, which is due to the peculiarities of production of the sublingual form of the drug). The maximum concentration in the blood plasma is reached after 5-6 minutes. The maximum effect of tablets of isosorbide dinitrate in sublingual administration occurs in the 10-15 minute. The duration of the therapeutic effect of the drug is 60-120 minutes. The drug is short-acting.Isosorbide dinitrate is metabolized to form an active metabolite of isosorbide-5-mononitrate, the half-life of which is 5:00, 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 1:00. From 80 to 100% of the taken single dose is excreted in the urine within 24 hours, mainly in the form of metabolites. Of particular importance is this form in patients with low systemic bioavailability of tablets of isosorbide dinitrate when ingested.

Basic physical and chemical properties

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

Shelf life

4 years. Do not use after the expiration date stated on the package.

Storage conditions

Store at a temperature of no higher than 30 0 C in the original packaging. Keep out of the reach of children.

Packaging

50 tablets in a jar in a pack of cardboard.

Category of leave

On prescription.