Iso-mik

A drug for the treatment of diseases of the cardiovascular system. Consider the indications for its use, side effects, dosage and other pharmacological features. International name Isom-micro: isosorbide dinitrate -1,4 3,6-diandrosorbitol-2,5 dinitrate. It is part of the pharmacological group of drugs that improve the blood supply and metabolism of the myocardium. Antianginal drug with the active substance - isosorbide dinitrate, belongs to the group of organic nitrates. Stimulates the relaxation of the smooth muscle vascular layer, which causes a decrease in peripheral resistance and the flow of blood to the right atrium. Antianginal effect is due to increased lumen of coronary vessels and redistribution of coronary blood flow in favor of ischemic sites.

Indications of the iso-mik

The drug is used for medical purposes and has such indications for use:

• Unstable angina
• Acute heart attack
• Acute left ventricular failure
• Vasospastic angina (Prinzmetal)

Tablets and spray are used to prevent attacks of angina pectoris in patients with ischemia of the heart. They are effective in chronic heart failure and a pronounced syndrome of pulmonary hypertension.

Parenteral forms of Iso-mics are prescribed for patients with acute conditions: acute myocardial infarction, acute left ventricular failure, pre-infarction, unstable angina.

[1]

Release form

Iso-mik has several forms of release, consider each of them:

• Spray

It is produced in bottles of dark glass of 15 ml each. The sublingual aerosol contains 375 mg of isosorbide dinitrate.

• Ampoules

Concentrate for solution for infusion. Available in ampoules of 2 ml or in bottles of 5 ml. In one cardboard pack 10 ampoules or 5 bottles. 1 ml of the drug contains 10 mg of isosorbide dinitrate.

• Injection

Ampoules of dark glass 10 ml each, in the package 10 ampoules. 1 ampoule solution contains 10 mg isosorbide dinitrate.

• Tablets sublingual

Capsules in polymer bottles, 50 pieces each. The tablets are released at a dosage of 5, 10 and 20 mg isosorbide dinitrate. As auxiliary substances: sorbitol and sugar.

[2], [3], [4]

Pharmacodynamics

Isosorbide dinitrate is the active ingredient Iso-mik. Pharmacodynamics of the drug is associated with the release of active components of nitric oxide in the smooth muscles of the vascular system. Nitric oxide increases the level of cyclic 3,5 guanosine monophosphate and promotes the activation of guanylate cyclase. This helps to relax the smooth muscles. Under the influence of the active substance, precapillary sphincters and arterioles relax much less unlike veins and large arteries.

Isosorbide dinitrate is a peripheral dilator that acts on venous vessels. It reduces myocardial oxygen demand by expanding peripheral veins and reducing inflow to the right atrium before exercise, reduces overall peripheral vascular resistance after exercise.

The active substance redistributes coronary blood flow in the area with reduced blood supply. Increases tolerance to physical exertion in ischemic disease and angina pectoris. Unloads the myocardium in case of heart failure due to before the load, and also reduces the pressure in the small circle of the circulation.

[5], [6], [7], [8]

Pharmacokinetics

When applying sublingual forms of Iso-Mik (spray, tablets), the therapeutic effect occurs within 2-5 minutes and lasts up to 1-2 hours. Pharmacokinetics indicates the achievement of maximum plasma concentrations within 5-6 minutes. With parenteral administration, the effect occurs within 1-2 minutes after infusion. Oral forms are characterized by a prolonged therapeutic effect of 4-5 hours. The maximum plasma concentration is reached within 2 hours, bioavailability of 22% (at the first passage through the liver).

Isosorbide dinitrate is metabolized in the body and forms two active metabolites. They are withdrawn within 5 and 2.5 hours. Isosorbide dinitrate is withdrawn within 1-5 hours regardless of the method of administration. With a long course of treatment, the elimination half-life increases. During the day with the help of the kidneys, 80-100% of the dose taken is excreted.

[9], [10], [11]

Dosing and administration

Depending on the medical indications and the form of release, the patient is prescribed a method of administration and dose of Iso-mik.

• Sublingual tablets are taken before the expected emotional or physical exertion. Dragee is kept under the tongue until completely dissolved or chewed. Recommended dosage: 1-2 pcs. 3-4 times a day, the duration of treatment is selected by a doctor.
• Tablets for oral intake are washed down with clean drinking water, without chewing. As a rule, prescribe 10-20 mg of medication 2-3 times a day, the maximum dosage of 120 mg isosorbide dinitrate per day. Between receptions it is necessary to observe a time interval of 4 hours.
• Solution for injection dissolve in the infusion solution and injected intravenously drip. To do this, use 400 ml of isotonic sodium chloride solution and 50-100 ml of solution for injection of Iso-mic. Dosage and duration of treatment are individual for each patient.
• Concentrate for the preparation of the infusion solution used immediately after dilution and injected intravenously drip. The dose and duration of therapy depend on the patient's condition. It requires control over blood pressure, heart rate, ECG and diuresis.
• Spray sublingual sprayed under the tongue. When injecting it is necessary to hold your breath and breathe through your nose. Between aerosol sprays should be a time interval of 30 seconds. For treatment appoint 1-2 injections 3-4 times a day.

With prolonged therapy, it is necessary to take weekly breaks every 4-6 weeks of use, regardless of the form of release of the drug.

[15], [16]

Use of the iso-mik during pregnancy

The drug iso-mik is not recommended for use during pregnancy and lactation. The purpose of the drug in this period may be associated with life indications. But in this case, it is necessary to consider the possibility of developing pathological reactions in the fetus.

In pediatric practice, the medication is not used because of the lack of reliable data on the safety of its use.

Contraindications

Iso-mik has contraindications to the use, which are based on the individual reaction of the organism to the active substance. Medication is not prescribed in such cases:

• Acute vascular insufficiency
• Severe arterial hypotension
• Cardiac tamponade
• Constrictive pericarditis
• Hypertrophic obstructive cardiomyopathy
• Cardiogenic shock
• Severe form of anemia
• Closed-angle glaucoma
• Toxic pulmonary edema and hyperthyroidism
• Craniocerebral trauma
• Hemorrhagic stroke

Parenteral forms are not used for severe anemia, severe impairment of kidney and liver function. With special care, the drug is prescribed for patients with acute myocardial infarction under reduced pressure, cerebral circulatory disorders, increased intracranial pressure, aortic or mitral stenosis.

[12]

Side effects of the iso-mik

During the application of Iso-mik, some patients may develop side effects. Undesirable reactions are due to the active component - isosorbide dinitrate:

• Cardiovascular system: hyperemia of the face and upper body, attacks of stenocardia, short-term hypoxemia, lowering of arterial pressure, reflex tachycardia, collapse.
• Gastrointestinal tract: dry mouth, nausea and vomiting, burning and tingling in the mouth, heartburn, relaxation of the sphincter.
• Central nervous system: weakness, sleep problems, decreased visual acuity, headaches and dizziness, brain ischemia.

In addition, skin allergic reactions (itching, burning, redness), tolerance to nitrates are possible. When using Isom-micro, it is not recommended to engage in work that requires increased attention and to manage potentially unsafe mechanisms. This is due to the fact that the drug can cause dizziness, decreased visual acuity.

[13], [14]

Overdose

High doses of medication can lead to the development of an overdose. Most often these are signs of arterial hypotension and reflex tachycardia. Overdose can trigger methaemoglobinemia, severe headaches, nausea, heart palpitations.

• With a sharp decrease in blood pressure, it is necessary to introduce an isotonic solution of sodium chloride. This will help restore the volume of circulating blood.
• In severe hypotension, Noradrenaline, Dopamine is used.
• With methemoglobinemia, 1 g of ascorbic acid, oxygen therapy and intravenous administration of 50 ml of 1% methylene blue solution are taken orally.

Since there is no specific antidote, symptomatic therapy and actions aimed at maintaining the normal functioning of the cardiovascular system are indicated. 

[17], [18], [19], [20]

Interactions with other drugs

Iso-mik can be used in complex therapy of diseases of the cardiovascular system. Interaction with other drugs is possible with the appropriate medical appointment.

• The drug can increase the toxicity of dihydroergotamine and increase its plasma concentrations.
• Contraindicated combine with sildenafil and nitrates.
• Reduces the effectiveness of heparin and myotic drugs.
• When used with sympathomimetics, the antianginal effect decreases.
• Hypotensive and vasodilating agents, beta-adrenergic blockers and calcium channel blockers, tricyclic antidepressants, neuroleptics, ethyl alcohol and other medicines increase the hypotensive properties of isosorbide dinitrate.

When using solutions for intravenous administration, it is not recommended to use infusion systems made of polyvinyl chloride or polyurethane. Systems of glass, polyethylene, polytetrafluoroethylene are allowed.

[21], [22], [23], [24], [25], [26], [27]

Storage conditions

All forms of Izo-Mik release should be kept in their original packaging, away from open fire, protected from moisture and sunlight. The recommended storage temperature should not exceed 25 ° C.

[28]

Shelf life

Iso-mik in the form of a sublingual spray has a shelf life of 48 months from the date of manufacture. Solution for injection, concentrate for solution for infusion and tablets can be used for 36 months. At the end of this period, the medicine must not be used and must be disposed of.

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