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 JENAHEXAL PHARMA (Germany)
Composition, form of production and packaging
Concentrate for solution for infusion
1 ml 1 amp.

isosorbide dinitrate 1 mg 10 mg

Auxiliary substances: water d /, sodium chloride, sodium hydroxide solution 2M, hydrochloric acid 1M (to pH 5.0-7.0).

10 ml - ampoules (10) - packs of cardboard.


Description of the drug approved by the manufacturer for the printed edition of 2008.


Peripheral vasodilator with predominant effect on venous vessels.
The mechanism of action is associated with the release of the active substance of nitric oxide in the smooth muscles of the vessels. Nitric oxide causes activation of guanylate cyclase and increases the level of cGMP, which leads to relaxation of smooth muscles.Under the influence of isosorbide dinitrate, arterioles and precapillary sphincters relax less than large arteries and veins. This is partly due to reflex reactions, as well as less intense formation of nitric oxide from the molecules of the active substance in the arteriolar walls.
The effect of isosorbide dinitrate is mainly associated with a decrease in the demand for myocardium in oxygen due to a reduction in preload (the expansion of peripheral veins and a decrease in the flow of blood to the right atrium) and postnagruzki (a decrease in OPSS), as well as with a direct coronary expansive action.Isosorbide dinitrate promotes redistribution of coronary blood flow in the area with reduced blood supply, reduces pressure in a small circle of blood circulation.
With heart failure helps discharge the myocardium by reducing preload.

Metabolism and excretion

There is no "first pass" effect through the liver.
It is metabolized outside the liver under the influence of glutathione-S-transferase with the formation of an active metabolite of isosorbide-5-mononitrate, as well as isosorbide-2-mononitrate.
T 1/2 isosorbide-5-mononitrate is 5 hours, isosorbide-2-mononitrate is 2.5 parts. T 1/2 isosorbide dinitrate is about 20 minutes.


- Acute myocardial infarction with left ventricular failure;

acute left ventricular failure;

- heart failure of various etiologies;

unstable angina.


The dose should be selected individually for each patient.
Treatment should begin with low doses, gradually increasing to the necessary.
The initial dose is 2-7 mg / h.
In some cases, the dose can be increased to 10 mg / h.
For patients with heart failure , as a rule, higher doses are required - in some cases up to 50 mg / h.
The average dose is approximately 7.5 mg / h.
The solution is administered in the form of intravenous infusions with the help of automatic infusion systems in hospital conditions under constant monitoring of cardiovascular system parameters.
Depending on the type and severity of the disease, in addition to the usual examination (symptoms, control of blood pressure, heart rate, diuresis), invasive procedures are performed to determine hemodynamic parameters.
For intravenous administration systems of the following materials are used: polyethylene, polypropylene and polytetrafluoroethylene.
Infusion materials made of polyvinyl chloride or polyurethane cause the loss of the active substance as a result of adsorption, which must be compensated for by increasing the dose.
The solution concentrate is sterile, does not contain preservatives.
0.1% solution should be opened under aseptic conditions immediately before use.
Preparation of the solution

To prepare the solution at a concentration of 100 Ојg / ml (0.01%), 50 ml of a 0.1% solution (ie 5 ampules of 10 ml) should be diluted to 500 ml.

To prepare the solution at a concentration of 200 Ојg / ml (0.02%), 100 ml of 0.1% solution (ie 10 ampoules of 10 ml) should be diluted to 500 ml.

Dose calculation table

Solution at a concentration of 100 Ојg / ml Solution at a concentration of 200 Ојg / ml Quantity of active substance

Infusion rate Infusion rate

ml / h drop / min ml / h drop / min mg / h

10 3-4 5 1-2 1

20 7 10 3 2

30 10 15 5 3

40 13 20 7 4

50 17 25 8 5

60 20 30 10 6

70 23 35 12 7

80 27 40 13 8

90 30 45 15 9

100 33 50 17 10

1 ml corresponds to 20 drops.

Depending on the clinical picture, hemodynamic parameters and ECG treatment can be continued up to 3 days or more.


From the side of the cardiovascular system: with the first application or with an increase in the dose of the drug, it is possible to lower blood pressure and / or orthostatic hypotension, which can be accompanied by a reflex increase in the pulse rate, inhibition, and dizziness and a sense of weakness.
At the beginning of treatment, headache ("nitrate" headache), which, as a rule, disappears in a few days with the further application of the drug may appear. In rare cases with a marked decrease in blood pressure, there may be an increase in symptoms of angina pectoris.
In isolated cases, there are collapoid conditions, sometimes with bradycardia and syncope (attacks with mental disturbance, dizziness, related to the disorder of cerebral circulation as a result of cardiac arrhythmias, primarily due to a significant loss of it).

From the digestive system: rarely - nausea, vomiting.

Other: redness of the skin, allergic skin reactions;
in some cases - exfoliative dermatitis.

- acute vascular insufficiency (shock, vascular collapse);

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

- hypertrophic obstructive cardiomyopathy;

- constrictive pericarditis;

- cardiac tamponade;

- 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);

- primary pulmonary diseases (because due to the relative redistribution of blood flow to hypoventilation zones, hypoxemia may occur);

- IHD (since redistribution of blood flow can lead to transient myocardial ischemia);

- toxic pulmonary edema;

- conditions accompanied by increased intracranial pressure (including hemorrhagic stroke, craniocerebral trauma);

- hypersensitivity to nitrate compounds.

With caution should be used in acute myocardial infarction with a reduced pressure filling the left ventricle (this requires a doctor's observation).

Caution should be applied to the drug and the systolic blood pressure lower than 90 mm Hg should be avoided.
with aortic and / or mitral stenosis, propensity to orthostatic reactions, diseases that are accompanied by increased intracranial pressure.

During pregnancy and lactation, the drug should be used very carefully, only in those situations where the expected benefit for the mother significantly exceeds the possible risk to the fetus or child.

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


When using Isoket, the cardiovascular system should be monitored: control of blood pressure (systolic blood pressure not lower than 100 mm Hg), ECG monitoring, heart rate, volume of urination (catheterization of the bladder).

Since a 0.1% Isoket solution is a supersaturated solution, crystallization of the substance can occur.
Despite the fact that under normal conditions this does not affect the activity of the preparation, in the case of crystallization, the solution is not recommended.
It should be taken into account that the ampoule is already inscribed under the blue dot, so additional nipping is not required.


At present, no cases of an overdose of Isoket have been reported.


With the simultaneous use of Isoket with other vasodilators, antihypertensive drugs, beta-blockers, calcium channel blockers, type 5 phosphodiesterase inhibitors used to treat erectile dysfunction (eg sildenafil), neuroleptics, tricyclic antidepressants, and also ethanol, hypotensive actions

With the simultaneous use of Isoket with dihydroergotamine, an increase in the concentration of dihydroergotamine in the blood can be noted, which leads to an increase in its hypotensive effect.


Shelf life - 5 years.
The shelf life of the drug is indicated on a cardboard box and on ampoules. Do not use the drug after the expiration date.
Conditions of leave from pharmacies

The drug is released by prescription.

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