Isoket

We are used to the fact that the therapy of many diseases, with the exception of certain pathologies of the upper respiratory tract and skin diseases, is carried out exclusively with the help of tablets, droppers and injections. Therefore, many people do not understand how you can, for example, treat your heart with a spray. But in the cardiological practice of using such forms of the drug is not uncommon. Take at least a spray "Izoket", which helps not only to alleviate the condition of patients with serious cardiovascular pathologies, but in some cases, thanks to an enviable speed, even save their lives.

[1], [2]

Indications Isoket

And spray "Izeket", and eponymous concentrate are used to treat certain cardiovascular pathologies, which include:

• acute left ventricular failure,
• acute stage of myocardial infarction, including, if the situation is complicated by acute left ventricular failure,
• unstable angina, which is the most dangerous exacerbation of coronary heart disease and often leads to myocardial infarction,
• a rare type of angina pectoris, when for the appearance of seizures the load is not needed, they are fixed even in a state of rest,
• spasms of the coronary vessels during surgical intervention,
• various types of heart failure,
• pulmonary edema,
• as well as post-infarction states.

In this case, the spray "Izoket" is used for rapid relief of angina attacks, treatment and prevention of myocardial infarction, for the removal of spasms of the coronary vessels, i.e. When urgent help is needed, helping to prevent the onset of tragic consequences. Its use is permissible both in conditions of inpatient treatment, and as a constant companion of cardiac patients.

But a solution-concentrate for infusions is used more as an effective therapeutic agent used in a hospital.

[3], [4], [5], [6], [7], [8]

Release form

To begin with, the spray "Izoket" is not the only form of release of this drug, and the areas of application of various forms are somewhat different.

The spray "Izoket" is produced in the form of an aerosol. Spraying of the drug is carried out under the tongue, while its dose, released when the valve is pressed, is strictly normalized. When one drug is injected into the oral mucosa, 1.25 mg of isosorbide dinitrate, the main active ingredient of the drug, is ingested in combination with the auxiliary components: 100% ethanol and a wethead 400.

Transparent composition with a tangible alcohol smell in the form of microscopic drops falls on the mucosa, where it is absorbed into the blood in a short time, which allows using the medicine as an ambulance in acute conditions that threaten the patient's life.

The medicinal composition for aerosol is packed in transparent bottles, its volume is 15 ml. There is no other dosage. Each bottle is designed for the same number of doses - 300, which allows you to clearly control the consumption of the drug, which is not easy to do, assessing the situation only visually.

The bottle with the drug is packed in a cardboard box, where the dispenser is also placed, intended for spraying the drug onto the mucous membranes.

The lack of freon in the composition of the aerosol makes it environmentally safe.

Another form of release of the drug is concentrate, which is used to fill the droppers. It is packaged in ampoules of 10 ml, which in turn are placed in cardboard containers of 10 pieces. In one ampoule of the drug contains 10 mg of active ingredient, supplemented with water, as well as sodium chloride and sodium hydroxide. 

[9], [10]

Pharmacodynamics

The drug belongs to the group of peripheral vasodilators. So called medicines, which, acting on the smooth muscles of blood vessels, contribute to their expansion. In this case, they act mainly on small blood vessels (arterioles and venules).

The mechanism of action of isosorbide dinitrate is based on the release of the active component of nitric oxide in the walls of blood vessels, which leads to relaxation of the vascular musculature. Thus, the need of the main cardiac muscle (myocardium) in oxygen is reduced due to the weakening of the blood flow to the right atrium and a reduction in the overall resistance of the peripheral vessels (pure physics!), And of course the vasodilator action itself.

The drug is able to redistribute coronary blood flow in the area with reduced blood circulation. It increases the endurance of patients with ischemic heart disease and angina pectoris. In the case of heart failure, "Izoket" facilitates the work of the heart by expanding the vessels and reducing the flow of blood to the right atrium.

Under the action of the drug, pressure decreases on the way from the heart to the lungs and back (a small circle of blood circulation), which prevents the violation of blood flow and gas exchange in the lungs, as well as functional changes in the work of the right heart ventricle.

[11], [12], [13], [14], [15], [16], [17]

Pharmacokinetics

The drug has a high efficiency and speed. Even when spraying the spray into the oral cavity, a positive effect is observed after half a minute and lasts up to 2 hours. It is excreted practically in its entirety with the help of kidneys in the form of metabolites formed during the passage of the medicinal composition through the liver.

When the aerosol is used for a long time, the drug becomes addictive, although after a short time the sensitivity to it is restored.

[18], [19], [20], [21], [22], [23], [24]

Dosing and administration

The method of application and dose of the drug "Izoket" is determined by the attending physician. He also decides which form of release of the drug will be more effective in each specific case.

If the aerosol is indicated in the application, you need to understand how to use it correctly. The spray "Izoket" is not intended for the treatment of the respiratory tract, and therefore it is not necessary to inhale the composition. On the contrary, you need to take a deep breath and hold your breath for a while. At this time, the aerosol dispenser is brought to the open mouth and, pressing it, the composition is injected into the area under the tongue, after which the mouth is closed and another half a minute breathe only through the nose.

When manipulating the aerosol, the vial is not turned over or tilted, but kept vertically, so that the nebulizer remains at the top. Before you start using a new aerosol, you should test it by letting the first jet into the air. The same is recommended if the aerosol has not been used for a long time.

As for the dosage of the drug in the form of a spray, it does not differ significantly with different pathologies. The doctor can prescribe a single dose of 1 to 3 injections, which are carried out with an interval of half a minute. Independently to increase the dosage is not necessary, if there is a need, it will make the attending physician.

In the acute course of myocardial infarction and heart failure, it may be necessary to re-inject a single dose of the drug if no normalization of the condition occurs within 5 minutes. The third time the drug can be repeated after 10 minutes. It is necessary to constantly monitor the indications of blood pressure and pulse.

The use of a solution of the drug in ampoule form, intended for filling the droppers with infusion therapy, is advisable in a hospital where it is possible to constantly monitor the pulse and BP indicators, and if necessary, hemodynamic indicators, or in ambulances.

Concentrate from ampoules is not used in pure form, it is diluted in saline solution or glucose solution (from 5 to 30%) to a concentration of 100 mg / ml (0.01%) or 200 mg / ml (0.02%). For dilution, Ringer's solution and other solutions containing albumin can also be used.

To obtain solutions of different concentrations, 500 ml of the above dilution solutions and 5 or 10 ampoules of Isoket concentrate (0.01% and 0.02% solutions respectively) will be needed.

Ready-made solution for infusion should be used within a day. The concentrate in the ampoules is sterile, the use of preservatives is stored, and therefore it is necessary to open the ampoules in aseptic conditions, preventing the ingress of various infections.

Care must be taken also to the material of the dropper system. It should not be made of polyvinyl chloride and polyurethane, which reduce the concentration of the active substance due to adsorption (absorption).

The dose of the drug and the speed of its administration are determined individually, taking into account the patient's condition and some parameters of the organism's functioning. Treatment should be started with small doses of the order of 1-2 mg per hour, which gradually bring up to 2-7, and sometimes even up to 10 mg per hour.

Heart failure therapy requires increased doses of medication, with an average dose of about 7.5 mg per hour, and the maximum sometimes reaches 50 mg per hour.

Infusion therapy with the help of "Isoket" concentrate can last 3 or more days. At the same time, constant monitoring of hemodynamic parameters and recording of ECT data are carried out.

[35], [36], [37], [38], [39], [40], [41], [42]

Use Isoket during pregnancy

Pregnancy is a special period in a woman's life, when the child's health actually comes to the fore. The use of "Izoket" during pregnancy is justified only if there is a danger to the life of the mother, exceeding the risk of a negative effect of the drug on the fetus. Doctors sometimes prescribe the drug to pregnant women, since animal studies have shown no harm from the medication for their young in the period of intrauterine life. They were not observed in the case of pregnant women who underwent treatment with the drug.

But caution is caution. In the end, this is not the only remedy for angina, you can almost always find an alternative.

Contraindications

No matter how much patients want to quickly and effectively prevent or kill dangerous seizures, the use of Isoket, as well as any synthetic drug, has not been shown to everyone. In this contraindication to the use of the drug is due not only to its composition, but also to the forms of release.

So the spray "Izoket" is inadmissible for use in patients with stable low blood pressure (not exceeding 90/60 mm Hg), deficiency of glucose-6-phosphate dehydrogenase, closed-angle glaucoma, increased thyroid functional activity (hyperthyroidism), acute cardiovascular insufficiency.

It is not permissible to simultaneously take a spray and drugs that suppress the action of the enzyme phosphodiesterase type 5, used for sexual disorders in men, because this "neighborhood" contributes to a drop in blood pressure. Even if the attack of angina began a short time after taking such drugs, for example, "Viagra."

Do not use aerosol in the case of cardiogenic shock, not amenable to special correction by reducing diastolic pressure.

The drug is not used in pediatric practice, so the question of its safety in the treatment of patients under the age of 18 remains open. And, of course, an obstacle to taking the drug is hypersensitivity to its components.

The use of concentrate for infusions, in addition to the above conditions, is limited in such cases:

• with a tamponade of the pericardial cavity, when, as a result of the compression of the heart, the fluid accumulated between the pericardial sheets disrupts the activity of the heart, its hemodynamics,
• with obstructive hypertrophic cardiomyopathy (thickening of the walls of the cardiac ventricles),
• with pericarditis, which is characterized by inflammation of the membranes of the heart,
• in primary lung diseases due to the danger of developing hypoxemia (low oxygen in the blood),
• with ischemic heart disease due to the high probability of development of transistor ischemia of the myocardium,
• damage to lungs as a result of inhalation of harmful substances (toxic edema),
• at the raised intracranial pressure which is observed as a result of traumas of a head, at a hemorrhagic stroke and other pathologies.
• with a strong sensitivity of the organism to nitrate compounds.

In the instructions to the preparation, pathologies are also noted, in which care should be taken when undergoing Isoket therapy. Concentrate to such pathologies include acute myocardial infarction with low ventricular filling pressure, aortic or mitral stenosis, propensity to orthostatic reactions.

Caution when using the spray is advised to comply with patients with the above pathologies, as well as with cardiomyopathy, pericarditis, cardiac tamponade, liver or kidney failure. The same applies to elderly patients.

[25], [26], [27], [28], [29]

Side effects Isoket

When using the "Isoket" concentrate, various reactions can be observed from the cardiovascular, immune and digestive systems, and the use of aerosol can lead to disorders related to the work of the nervous system.

The first use of the drug can cause a decrease in blood pressure. Similar symptoms are observed with an increase in the dose of the drug. A person can feel severe vertigo up to a clouding of consciousness, weakness and increased heart rate during sudden movements (orthostatic hypotension).

Sometimes light forms of collapse (acute vascular insufficiency) are diagnosed. More rarely, against a background of greatly reduced pressure, there is an exacerbation of symptoms of angina and collapse.

The gastrointestinal tract for taking Izote can react with nausea, reaching vomiting, dry mucous membranes and burning tongue.

In some patients, when using a spray, the following reactions of the central and peripheral nervous system are observed: weakness and drowsiness, stiffness of movement, inhibition, impaired vision.

Occasionally, such reactions as hyperemia of the skin on the face are fixed, as a result of which it acquires a red shade, a feeling of heat, allergic skin rashes.

[30], [31], [32], [33], [34]

Overdose

When using a concentrate for the preparation of an infusion solution in a hospital environment under the supervision of a doctor, there were no cases of overdose. Another thing is if this compound is used for buccal (per cheek) or sublingual (under the tongue) administration with a single dose of 5 to 10 mg and a different frequency of administration.

An overdose of the drug "Isoket" can be observed even with the use of a spray, especially at home, when the patient feels that the drug is not helping effectively, and he decides to increase the dose with more injections or multiple reception.

Symptoms of overdose are quite extensive. These are headaches with dizziness and fainting, and increased heart rate, and impaired vision. There is also an increase in temperature and against it the redness of the skin, increased sweating, seizures, increased intracranial pressure, digestive disorders in the form of vomiting and diarrhea. In severe cases of overdose, there is a decrease in the pulse (bradycardia), paralysis and coma.

An increase in the level of methemoglobin (hemoglobin with iron content) on the background of taking the drug may cause the development of methemoglobinemia. An ambulance in this condition includes intravenous administration of a 1% solution of myelene blue at a dosage of 1-2 mg per kilogram of the patient's weight.

In other cases, symptomatic therapy is indicated, as indicated by the doctor.

[43], [44], [45]

Interactions with other drugs

Taking into account the drug interaction "Izoket" with other drugs will help make the treatment not only safe, but in some cases more effective.

The drug has a noticeable hypotensive effect. Using it in parallel with some other drugs can reduce the patient's pressure to critical levels. These drugs include vasodilators, beta-adrenoblockers, alpha-adrenoblockers with the active substance dihydroergotamine, calcium channel blockers, blood pressure lowering drugs, type 5 phosphodiesterase inhibitors, antidepressants and antipsychotics. An identical action is observed with simultaneous reception of "Izoke" and "Quinidine" or "Novokainamid."

But "Verapamil", "Nifedipine", "Amiodarone" and "Propranolol" are able to enhance the antianginal effect of the drug "Izoket", thereby increasing its effectiveness. While alpha-adrenoblockers and sympathomimetics reduce its effect, aimed at relieving angina attacks.

M-holinoblokatory also badly "get along" with "Izoket", causing patients to increase intracranial pressure.

[46], [47], [48], [49], [50]

Storage conditions

The drug for angina pectoris, sometimes called Isoket, for safe and effective treatment, when purchasing medicine in the pharmacy network, you need to ensure that it does not expire, which is indicated on the package, and on the ampoules or vial. Although, in principle, this situation is unlikely, given that this figure is 5 years.

[51], [52], [53],

Special instructions

The drug "Izoket", however, like other cardiac drugs, can not be used uncontrollably. The drug therapy should be constantly accompanied by measurements of blood pressure and heart rate, volume of urine, control of hemodynamic parameters and cardiogram of the heart.

It is not advisable to use the drug for too long, because as a result, its effectiveness is reduced due to habituation. Doctors recommend using the medicine on a regular basis for no longer than 1.5 months, then taking a short break for 3-5 days, temporarily replacing "Izoket" with another remedy for angina pectoris.

During treatment with the drug "Izoket" is prohibited the use of alcoholic beverages, although this condition is relevant in all diseases of the heart and their treatment with various medications. The interaction of the active substance with ethyl alcohol causes a significant decrease in blood pressure.

It is also not recommended at this time to drive a car or perform tasks that require increased attention. This is due to side effects of the drug, which can cause drowsiness, impaired perception, affect the reaction rate.

Complete therapy should be gradually reducing the dosage and frequency of medication.

[54], [55]

Shelf life

As for the drug itself from angina pectoris, as Isoket is sometimes called, for safe and effective treatment, when purchasing a medicine in the pharmacy network, you need to ensure that it does not expire, which is indicated on the package, ampoules or vial. Although, in principle, this situation is unlikely, given that this figure is 5 years.

[56], [57], [58], [59]