Universal reference book for medicines
Name of the preparation: ISOOKET В® (ISOKET)

Active substance: isosorbide dinitrate

Type: Peripheral vasodilator.
Antianginal drug
Manufacturer: SCHWARZ PHARMA (Germany) manufactured by COLEP CCL LAUPHEIM (Germany)
Composition, form of production and packaging
Spray dosed
in the form of a transparent colorless solution with the smell of alcohol.

1 injection (1 dose)

isosorbide dinitrate 1.25 mg

Excipients: Macrogol 400, ethanol 100%.

15 ml (300 doses) - vials of dark glass with dosing device (1) - packs cardboard.


The product description was approved by the manufacturer for the 2009 print edition.


Peripheral vasodilator with predominant effect on venous vessels.
Stimulates the formation of nitric oxide (endothelial relaxing factor) in the vascular endothelium, which causes activation of intracellular guanylate cyclase, resulting in an increase in cGMP (mediator of vasodilation). Reduces the need for myocardium in oxygen by reducing preload (reduces the final diastolic volume of the left ventricle and reduces the systolic tension of its walls). Possesses coronary dilatation.
Reduces the flow of blood to the right atrium, helps reduce pressure in a small circle of circulation and regression of symptoms with pulmonary edema.
Promotes redistribution of coronary blood flow in the area with reduced blood circulation. Increases tolerance to physical activity in patients with coronary heart disease (including angina pectoris).
It dilates the vessels of the brain, the dura mater, which can be accompanied by a headache.

Like other nitrates, cross tolerance is developing.
After cancellation (interruption in treatment) sensitivity to it is quickly restored.
After spraying on the mucous membrane of the oral cavity, the effect manifests itself after 30 seconds and lasts 15-120 minutes.



Absorption is high.
Bioavailability is 60%.

Binding to blood plasma proteins - 30%.

Metabolism and excretion

It is metabolized in the liver with the formation of 2 active metabolites: isosorbide-5-mononitrate, whose fraction is 75-85%, T 1/2 - 5 h, and isosorbide-2-mononitrate, 15-25%, with T 1/2 - 2.5 h.

T 1/2 isosorbide dinitrate is 60 minutes.
It is excreted in the urine almost completely in the form of metabolites.

- relief of angina attacks;

- prevention of angina attacks;

- Acute myocardial infarction (including complicated by acute left ventricular failure);

- a condition after the transferred myocardial infarction.


To stop an angina attack or before a physical or emotional load that can cause an attack, the drug should be injected into the mouth 1-3 times with an interval of 30 seconds between injections against the background of a delay in breathing.
A single dose (3 injections) to stop an attack can be increased only on the advice of a doctor.
In acute myocardial infarction and acute heart failure, 1-3 injections are administered under the control of blood pressure and heart rate.
If there is no effect for 5 minutes, you can repeat the injection under the supervision of a doctor. If the improvement does not occur within 10 minutes, you can repeat the use of Isoket under the control of blood pressure.
Terms of use

Aerosol should not be inhaled.
It is necessary to bring the dosing device (sprayer) close to the mouth, then take a deep breath, hold your breath and, by pressing the sprayer, inject the aerosol into the mouth (and there may be a slight burning sensation of the tongue). Then you should close your mouth and breathe through your nose for about 30 seconds.
At the first application of the drug, and after more than 24 hours after the last use of the Isoquette, the first pressing of the spray gun should direct the jet into the air (continuously and until the end, push the sprayer and release again).
When using the bottle, hold it vertically, with the spray gun facing upwards.

On the part of the cardiovascular system: with the first application or with increasing doses, it is possible to reduce blood pressure, the development of orthostatic hypotension, which can be accompanied by a reflex increase in heart rate, inhibition, as well as dizziness and a sense of weakness.
At the beginning of treatment, headaches may also appear ("nitrate" headaches), which, as a rule, disappear with further use of the drug.
Rarely with a marked decrease in blood pressure, there may be an increase in symptoms of angina pectoris (paradoxical nitrate reaction) and collapse.

In some cases, there are collapoid conditions, sometimes with bradycardia and syncope (fits of consciousness, dizziness, associated with a disorder of cerebral circulation as a result of cardiac arrhythmias, primarily due to a significant loss of it).

On the part of the digestive system: there may be a sensation of slight burning of the tongue, dry mouth;
rarely - nausea, vomiting.
From the side of the central nervous system and peripheral nervous system: stiffness, drowsiness, blurred vision, decreased ability to rapid mental and motor reactions (especially at the beginning of treatment);
rarely - ischemia of the brain.
Other: rarely - redness of the face, fever, allergic skin reactions;
in some cases - exfoliative dermatitis, the development of tolerance (including cross-over to other nitrates).

acute vascular insufficiency;

- severe arterial hypotension (systolic blood pressure below 90 mm Hg, diastolic blood pressure below 60 mm Hg);

- cardiogenic shock (if it is impossible to correct the final diastolic pressure of the left ventricle with intra-aortic counterpulsation or preparations with a positive inotropic effect);

- deficiency of glucose-6-phosphate dehydrogenase;

- the closed-angle form of glaucoma;

- hyperthyroidism;

- children and adolescents under 18 years of age (efficacy and safety not established);

- simultaneous administration with inhibitors of phosphodiesterase type 5 (eg, sildenafil), t.
in this case, an increase in the hypotensive effect of the drug is possible;
- hypersensitivity to nitrate compounds or other components of the drug.

With caution and under the supervision of a doctor, the drug should be used for acute myocardial infarction with a reduced ventricular filling pressure.

Caution should be given to the preparation with hypertrophic obstructive cardiomyopathy, constrictive pericarditis, cardiac tamponade, aortic and / or mitral stenosis, propensity to orthostatic reactions, with diseases accompanied by increased intracranial pressure (including hemorrhagic stroke, traumatic brain injury) , renal insufficiency of a serious degree, hepatic insufficiency (since the risk of development of methemoglobinemia increases), in elderly patients.


During pregnancy and during the period of breastfeeding, the use of Isoket is possible only in cases where the expected benefit for the mother considerably exceeds the possible risk for the fetus or the child.

In experimental studies, no damaging effects on the fetus have been identified.


With caution should prescribe the drug in severe kidney failure.


With caution should prescribe the drug for liver failure.


During the period of Isoket application, it is necessary to monitor blood pressure and heart rate.

It should be avoided abrupt withdrawal of the drug, the drug is canceled gradually.

It should be borne in mind that the frequent administration and use of the drug in high doses can cause the development of tolerance.
In this case, it is recommended to cancel the drug for 24-48 h, or after 3-6 weeks of regular admission to take a break for 3-5 days, replacing the time of Isoket with other antianginal drugs.
It should be taken into account that the preparation contains about 85% ethanol.
Therefore, during the treatment with Izoket, alcohol consumption should be excluded.
Avoid contact with the eyes.

Each time the spray is pressed, an equal amount of solution is sprayed in the form of minute droplets.
It easily penetrates the mucous membrane of the mouth and in a few seconds falls into the bloodstream.
Isoket does not contain freon, is environmentally friendly.
The bottle is transparent, which makes it possible to notice the need for a replacement in time.
Impact on the ability to drive vehicles and manage mechanisms

The characteristics of an individual response to a drug may lead to a disruption in the ability to drive vehicles or other mechanisms.
This effect is greatly enhanced at the beginning of treatment, with increasing doses and changing the drug, as well as when combined with the intake of alcohol.

Symptoms: collapse, fainting, headache, dizziness, palpitation, visual disturbances, hyperthermia, convulsions, skin hyperemia, increased sweating, nausea, vomiting, diarrhea, methemoglobinemia (cyanosis, dyspnoea), bradycardia, increased intracranial pressure, paralysis, coma.

Treatment: with methemoglobinemia - iv injection of 1% methylene blue at a dose of 1-2 mg / kg;
In severe arterial hypotension, phenylephrine (mezaton), epinephrine (adrenaline) and related compounds are contraindicated.

With the simultaneous use of Isoket with other vasodilators (vasodilators), antihypertensive drugs, beta adrenoblockers, slow calcium channel blockers, neuroleptics, tricyclic antidepressants, ethanol, novocaineamide, quinidine, phosphodiesterase inhibitors, hypotensive effect may be enhanced.

When the combination of Isoket with amiodarone, propranolol, slow calcium channel blockers (verapamil, nifedipine), an antianginal effect is possible.

With the simultaneous use of Isoket with sympathomimetics, alpha-adrenoblockers (dihydroergotamine), the severity of antianginal action can be reduced (due to a pronounced decrease in blood pressure, and as a consequence, coronary perfusion).

With the combined use of Isocet with m-holinoblokatorami (atropine) the probability of increasing intracranial pressure increases.

It should be borne in mind that the data also apply to cases when the drug was taken recently.


The drug is released by prescription.


The drug should be stored out of reach of children at a temperature of no higher than 25 В° C.
Shelf life - 5 years.
It is necessary to periodically check the operation of the sprayer (especially with a long break in its use).
The label of the bottle below shows an arrow. When the level of the liquid in the vial reaches the upper edge of the arrow, you need to purchase the next spray bottle. Further use of such a vial is possible until, with slight inclination, the tip of the suction tube is still immersed in the liquid.
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