Isoquette

We are accustomed to the fact that therapy for many diseases, with the exception of some upper respiratory tract pathologies and skin diseases, is carried out exclusively with the help of tablets, droppers and injections. Therefore, many do not understand how it is possible, for example, to treat the heart with a spray. But in cardiology practice, the use of such forms of the drug is not uncommon. Take, for example, the spray "Isoket", which helps not only to alleviate the condition of patients with serious cardiovascular pathologies, but in some cases, thanks to its enviable speed of action, even save their lives.

[ 1 ], [ 2 ]

Indications Isoquette

Both the Izeket spray and the concentrate of the same name 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, when no stress is needed for attacks to occur, they are recorded even at rest,
• coronary vessel spasms during surgery,
• various types of heart failure,
• pulmonary edema,
• as well as post-infarction conditions.

In this case, the spray "Isoket" is used for the rapid relief of angina attacks, treatment and prevention of myocardial infarction, for the relief of coronary vessel spasms, i.e. when emergency care is required to help prevent the onset of tragic consequences. Its use is permissible both in inpatient treatment and as a constant companion for heart patients.

But the concentrated solution for infusions is used more as an effective therapeutic agent applied in a hospital setting.

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

Release form

Let's start with the fact that Isochet spray is not the only form of release of this drug, and the areas of application of various forms are somewhat different.

Izoket spray is produced in the form of an aerosol. The drug is sprayed under the tongue, and its dose, released when pressing the valve, is strictly standardized. With one injection of the drug, 1.25 mg of isosorbite dinitrate, which is the main active ingredient of the drug, gets on the oral mucosa in combination with auxiliary components: 100% ethanol and mokrogol 400.

A transparent composition with a noticeable alcohol smell in the form of microscopic drops gets on the mucous membrane, where it is quickly absorbed into the blood, which allows the drug to be used as an emergency aid in acute conditions that threaten the patient's life.

The medicinal composition for the aerosol is packaged in transparent bottles, its volume is 15 ml. No other dosage is provided. 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 by assessing the situation only visually.

The bottle with the drug is packed in a cardboard box, which also contains a dispenser designed to spray the medicine onto the mucous membranes.

The absence of freon in the aerosol makes it environmentally friendly.

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

[ 9 ], [ 10 ]

Pharmacodynamics

The drug belongs to the group of peripheral vasodilators. This is the name given to drugs that act on the smooth muscles of blood vessels, promoting their expansion. In doing so, they act primarily 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 muscles. In this way, a decrease in the need of the main heart muscle (myocardium) for oxygen is achieved by weakening the blood flow to the right atrium and reducing the overall resistance of the peripheral vessels (pure physics!), and of course, a vasodilatory effect.

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

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

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

Pharmacokinetics

The drug is highly effective and fast-acting. Even when spraying the spray into the oral cavity, the positive effect is observed after half a minute and lasts up to 2 hours. It is excreted almost completely by the kidneys in the form of metabolites formed when the drug passes through the liver.

With prolonged use of the aerosol, addiction to the drug is observed, although after a short time, sensitivity to it is restored.

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

Dosing and administration

The method of administration and dosage of the drug "Isoket" 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 prescription specifies an aerosol, you need to understand how to use it correctly. Izoket spray is not intended for treating the respiratory tract, which means you do not need 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 spray is brought to the open mouth and, pressing on it, the composition is injected into the area under the tongue, after which the mouth is closed and breathing only through the nose for another half minute.

When handling the aerosol, do not turn the bottle upside down or tilt it, but hold it vertically so that the sprayer remains at the top. Before using a new aerosol, you should test it by releasing the first stream into the air. It is recommended to do the same 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 for different pathologies. The doctor can prescribe a single dose of 1 to 3 injections, which are carried out at intervals of half a minute. You should not increase the dosage on your own; if necessary, the attending physician will do this.

In acute myocardial infarction and heart failure, a repeated injection of a single dose of the drug may be required if the condition is not normalized within 5 minutes. The drug can be taken for the third time after 10 minutes. In this case, it is necessary to constantly monitor blood pressure and pulse.

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

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

To obtain solutions of different concentrations, you will need 500 ml of the above-described dilution solutions and 5 or 10 ampoules of Isochet concentrate (respectively for 0.01% and 0.02% solutions).

The ready solution for infusions must be used within 24 hours. The concentrate in ampoules is sterile, stored without the use of preservatives, and therefore the ampoules must be opened in aseptic conditions, preventing various infections from getting inside.

You should also pay close attention to the material of the drip system. It should not be made of polyvinyl chloride or polyurethane, which reduce the concentration of the active substance due to adsorption (absorption).

The dose of the drug and the rate of its administration are determined individually, taking into account the patient's condition and some indicators of the body's functioning. Treatment should be started with small doses of about 1-2 mg per hour, which are gradually increased to 2-7, and sometimes even to 10 mg per hour.

Treatment of heart failure requires higher doses of the drug, with the average dose being around 7.5 mg per hour, and the maximum sometimes reaching 50 mg per hour.

Infusion therapy using the concentrate "Isochet" can last for 3 or more days. During this time, constant monitoring of hemodynamic parameters and recording of ECT data is carried out.

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

Use Isoquette during pregnancy

Pregnancy is a special period in a woman's life, when the health of the child actually comes to the forefront. The use of Izoket during pregnancy is justified only if there is a danger to the mother's life that exceeds the risk of the drug's negative impact on the fetus. Doctors sometimes prescribe the drug to pregnant women, since animal studies have not shown any harm from the drug to their offspring during intrauterine life. There were no such cases in pregnant women who underwent treatment with the drug.

But caution is caution. After all, this is not the only remedy for angina, and there is almost always an alternative.

Contraindications

No matter how much patients with heart disease would like to quickly and effectively prevent or stop dangerous attacks, the use of the drug "Isoket", like any synthetic drug, is not indicated for everyone. At the same time, contraindications to the use of the drug are due not only to its composition, but also to the forms of release.

Thus, Isochet spray is not approved for use in the treatment of patients with stably low blood pressure (not exceeding 90/60 mm Hg), glucose-6-phosphate dehydrogenase deficiency, closed-angle glaucoma, increased functional activity of the thyroid gland (hyperthyroidism), and acute vascular insufficiency.

It is not permissible to take the spray simultaneously with drugs that suppress the action of the enzyme phosphodiesterase type 5, used for sexual dysfunction in men, since such "neighborhood" contributes to a drop in blood pressure. Even if an attack of angina began shortly after taking such drugs, for example, "Viagra".

Aerosol is also not used in cases of cardiogenic shock that cannot be specifically corrected by reducing diastolic pressure.

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

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

• in case of pericardial tamponade, when, as a result of compression of the heart by fluid accumulated between the layers of the pericardium, the activity of the heart and its hemodynamics are disrupted,
• with obstructive hypertrophic cardiomyopathy (thickening of the walls of the heart ventricles),
• with pericarditis, which is characterized by inflammation of the lining of the heart,
• in primary lung diseases due to the risk of developing hypoxemia (low oxygen content in the blood),
• in ischemic heart disease due to the high probability of developing transient myocardial ischemia,
• damage to the lungs as a result of inhalation of harmful substances (toxic edema),
• with increased intracranial pressure, which is observed as a result of head injuries, hemorrhagic stroke and other pathologies.
• in case of strong sensitivity of the body to nitrate compounds.

The instructions for the drug also note pathologies in which caution should be exercised when undergoing therapy with the drug "Isoket". In relation to the concentrate, such pathologies include acute myocardial infarction with low ventricular filling pressure, aortic or mitral stenosis, and a tendency to orthostatic reactions.

Patients with the above-described pathologies, as well as cardiomyopathy, pericarditis, cardiac tamponade, liver or kidney failure are advised to exercise caution when using the spray. The same applies to elderly patients.

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

Side effects Isoquette

When using the Izoket concentrate, various reactions may be observed from the cardiovascular, immune and digestive systems, and the use of the aerosol may lead to disturbances associated with the functioning of the nervous system.

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

Sometimes mild forms of collapse (acute vascular insufficiency) are diagnosed. Less often, against the background of greatly reduced pressure, exacerbation of angina symptoms and collapse are observed.

The gastrointestinal tract may react to taking Isoket with nausea, leading to vomiting, dry mucous membranes and a burning sensation in the tongue.

Some patients experience the following reactions of the central and peripheral nervous system when using the spray: weakness and drowsiness, stiffness of movement, lethargy, and blurred vision.

Occasionally, reactions such as hyperemia of the skin on the face, as a result of which it acquires a red tint, a feeling of heat, and allergic rashes on the skin are also recorded.

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

Overdose

When using the concentrate for the preparation of an infusion solution in a hospital setting under the supervision of a physician, no cases of overdose were noted. Another matter if this composition is used for transbuccal (behind the cheek) or sublingual (under the tongue) administration with a single dose of 5 to 10 mg and various frequency of administration.

An overdose of Izoket can also occur when using the spray, especially at home, when the patient feels that the drug is not helping effectively enough and decides to increase the dose by using more sprays or more frequent administration.

The symptoms of overdose are quite extensive. These include headaches with dizziness and fainting, increased heart rate, and visual impairment. Also noted is an increase in temperature and, against its background, redness of the skin, increased sweating, convulsions, increased intracranial pressure, digestive disorders in the form of vomiting and diarrhea. In severe cases of overdose, a decrease in pulse (bradycardia), paralysis, and coma are observed.

An increase in the level of methemoglobin (hemoglobin containing iron) while taking the drug can cause the development of methemoglobinemia. Emergency care for this condition includes intravenous administration of a 1% solution of mythene blue at a dosage of 1-2 mg per kilogram of the patient's weight.

In other cases, symptomatic therapy is carried out as prescribed by the doctor.

[ 43 ], [ 44 ], [ 45 ]

Interactions with other drugs

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

The drug has a noticeable hypotensive property. Its use in parallel with some other drugs can reduce the patient's blood pressure to critical values. Such drugs include vasodilators, beta-blockers, alpha-blockers with the active substance dihydroergotamine, calcium channel blockers, drugs that reduce blood pressure, phosphodiesterase type 5 inhibitors, antidepressants and neuroleptics. An identical effect is observed with the simultaneous use of Isoket and Quinidine or Novocainamide.

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

M-anticholinergics also do not “get along” well with Isoket, causing increased intracranial pressure in patients.

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

Storage conditions

The drug for angina, as it is sometimes called "Isoket", then for safe and effective treatment, when purchasing the medicine in a pharmacy network, you need to make sure that its expiration date has not expired, which is indicated on the packaging and on the ampoules or bottle. Although, in principle, such a situation is unlikely, given that this figure is 5 years.

[ 51 ], [ 52 ], [ 53 ]

Special instructions

The drug "Isoket", however, like other cardiac drugs, should not be used without control. Therapy with the drug should be constantly accompanied by measurements of blood pressure and heart rate, urine volume, monitoring of hemodynamic parameters and cardiac cardiogram.

It is not advisable to use the drug for too long, as this will result in a decrease in its effectiveness due to addiction. Doctors recommend using the drug regularly for no longer than 1.5 months, then taking a short break of about 3-5 days, temporarily replacing Izoket with another remedy for angina.

During treatment with Izoket, drinking alcohol is prohibited, although this condition is relevant for any heart disease and its treatment with various drugs. The interaction of the active substance with ethyl alcohol causes a significant decrease in blood pressure.

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

Therapy should be completed by gradually reducing the dosage and frequency of medication administration.

[ 54 ], [ 55 ]

Shelf life

As for the drug for angina, sometimes called "Isoket", for safe and effective treatment, when buying the medicine in a pharmacy network, you need to make sure that its expiration date has not expired, which is indicated on the packaging and on the ampoules or bottle. Although, in principle, such a situation is unlikely, given that this figure is 5 years.

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