Universal reference book for medicines
Name of the preparation: ISAKARDIN В® (ISACARDIN)

Active substance: isosorbide dinitrate

Type: Peripheral vasodilator.
Antianginal drug
Producer: TECHNOCOM LLC (Group of companies FARMAMED.RF) (Russia) produced by NPF MIKROHIM (Ukraine)
Composition, form of production and packaging
Spray sublingual dosed
transparent, colorless or yellowish in color, with an alcohol smell.

1 dose of 1 fl.

isosorbide dinitrate 1.25 mg 375 mg

Excipients: Macrogol 400 (polyethylene oxide 400) - 1.8 g, ethanol 96% - up to 15 ml.

15 ml (300 doses) - bottles of dark glass (1) with a mechanical dosing pump and a sprayer - packs of cardboard.


Description of the drug approved by the manufacturer for the printed edition of 2015.


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, which results in an increase in cyclic guanosine monophosphate (cGMP), a mediator of vasodilation.Reduces the need for myocardium in oxygen by reducing preload (reduces the end-diastolic volume (BDW) of the left ventricle and reduces the systolic tension of its walls). Possesses coronary dilatation.
It acts on the peripheral arteries and veins.
Relaxation of veins leads to a decrease in venous return to the heart (preload), which reduces the filling pressure of the left ventricle. There is also (though to a lesser extent) an expansion of arterial vessels, which is accompanied by a decrease in blood pressure, a decrease in OPSS (postload).
Decrease in pre- and postnagruzki leads to a decrease in oxygen consumption by the myocardium.
Improving the delivery of oxygen to the ischemic areas, reduces the area of ​​myocardial damage.
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 exercise tolerance in patients with IHD, 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.

Suction and distribution

Absorption is high.
Bioavailability through oral mucosa - 60%. Binding to blood plasma proteins - 30%.
Metabolism and excretion

T 1/2 is 60 minutes.
Metabolised in the liver to two 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) . The drug is excreted by the kidneys (almost completely in the form of metabolites).

- relief of angina attacks;

- prevention of attacks of angina pectoris (including before physical exertion);

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

- a condition after the transferred myocardial infarction.


Isacardin В® spray is used by spraying on the mucosa of the oral cavity, under the tongue.

The solution should not be inhaled.
It is necessary to bring the spray close to the mouth and, pressing on the nebulizer, inject the solution into the oral cavity:
take a deep breath;

- hold the breath;

- inject the solution into the mouth (this may cause a slight burning of the tongue);

- close your mouth and breathe through your nose for about 30 seconds.

One dose of the drug contains 1.25 mg of isosorbide dinitrate.

To stop an attack of angina or before a physical or emotional load that can cause an attack , you need to inject the spray 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 of 3 injections for an arrest of an attack can be increased only on the recommendation of a doctor.
With acute myocardial infarction and acute heart failure, therapy is performed under the control of blood pressure, heart rate and doctor's supervision, starting with 1-3 injections, with a 30 second interval between injections;
in the absence of effect after 5 minutes, you can repeat 1 injection; if no improvement occurs, then after 10 minutes repeat 1 injection again.
When the first use of the preparation of Isacardin В® Spray or with a break in use for more than a day, several times, press the sprayer until the first drops of the solution appear.
When using the spray bottle, keep it upright with a spray gun. Avoid contact with eyes.

The frequency of side effects is given according to WHO classification: very often (> 1/10), often (> 1/100 and <1/10), infrequently (> 1/1000 and <1/100), rarely (> 1/10000 and <1/1000), very rarely (<1/10 000), the frequency is unknown (according to available data, it is not possible to determine the frequency of development).

From the side of the central nervous system: very often - headache;
often - dizziness, drowsiness, weakness, blurred vision.
From the cardiovascular system: often - orthostatic hypotension, reflex tachycardia;
infrequently, the "paradoxical" increase in angina attacks, collapse (accompanied by bradyarrhythmia and syncope), transient hypoxemia due to relative redistribution of blood flow to hypoventilated alveolar areas (in patients with IHD, it can lead to myocardial hypoxia).
From the digestive system: often - burning tongue;
infrequently - nausea, vomiting; very rarely - heartburn.
From the skin: rarely allergic skin reactions (including skin rash), "tides" of blood to the skin of the face;
very rarely - angioedema, Stevens-Johnson syndrome;frequency unknown - exfoliative dermatitis.
Other: often - asthenia.

Perhaps the development of tolerance, incl.
cross-over to other nitrates.

- Acute circulatory disturbance (shock, collapse);

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

- severe hypovolemia;

- 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;

- hypertrophic obstructive cardiomyopathy, constrictive pericarditis, cardiac tamponade;

- severe aortic, subaortic and mitral stenosis;

- Hemorrhage in the brain;

- severe anemia;

- simultaneous reception of PDE5 inhibitors (including sildenafil, vardenafil, tadalafil) - the risk of a pronounced decrease in blood pressure;

- age under 18 years (effectiveness and safety not established);

- Hypersensitivity to nitrates or other components of the drug.

With caution:

- at a low filling pressure of the left ventricle, incl.
with acute myocardial infarction;
- with aortic or mitral stenosis;

- with a tendency to orthostatic reactions (a sharp decrease in blood pressure when the position of the body changes);

- with diseases accompanied by increased intracranial pressure (including hemorrhagic stroke, craniocerebral injury);

- with severe renal failure;

- with hepatic insufficiency (risk of development of methemoglobinemia);

- with hyperthyroidism;

- with angle-closure glaucoma;

- in the elderly;

- inadequate and inadequate nutrition;

- toxic pulmonary edema.


Use of the drug Isachardine В® spray during pregnancy is only possible in cases where the expected benefit exceeds the potential risk to the fetus and the baby, and should be controlled by a doctor.

If it is necessary to use isosorbide dinitrate during breastfeeding, it is recommended to stop breastfeeding, because
there is information about the penetration of nitrates into breast milk.
If an emergency use of the preparation of Isacardin В® Spray is necessary, for example, to stop an attack of angina, it is necessary to establish observation of the child for the development of possible side effects.


Contraindicated in severe renal failure.


Contraindicated in hepatic insufficiency (risk of development of methaemoglobinaemia).


During the therapy, it is necessary to monitor blood pressure and heart rate.
It is necessary to avoid sharp abolition of the drug, to reduce the dose gradually. Frequent prescription and high doses can cause tolerance development, in this case it is recommended to cancel for 24-48 h, or after 3-6 weeks of regular admission to take a break for 3-5 days, replacing the preparation of Isacardin В® spray with other antianginal drugs for this time.
Especially careful medical supervision is necessary for acute myocardial infarction with reduced ventricular filling pressure.

The solution contains about 85% ethanol.
During the period of treatment with the drug Izakardin В® spray should be excluded from the use of ethanol (alcohol).
Impact on the ability to drive vehicles and manage mechanisms

When using Isacardin В® spray, care must be taken when driving vehicles and mechanisms (risk of dizziness).


Symptoms: severe arterial hypotension (systolic blood pressure less than 90 mmHg), pallor, increased sweating, thready pulse, tachycardia, dizziness, headache, weakness, fainting, nausea, vomiting, diarrhea, methemoglobinemia (accompanied by tachypnea, anxiety, loss of consciousness, cardiac arrest).
When used in high doses, intracranial pressure may increase.
Treatment: in mild cases - transfer of the patient to the "lying" position with raised legs or with the head of the bed lowered;
in more serious cases, with a pronounced decrease in blood pressure - replenishment of BCC, the administration of norepinephrine or other vasoconstrictors (vasoconstrictors), for example, phenylephrine, dopamine (epinephrine is not recommended); with methemoglobinemia - ascorbic acid - 1 g inside or in the form of sodium salt iv 0.1-0.15 ml / kg 1% solution (up to 50 ml), oxygen therapy, ventilation, hemodialysis.

It is possible to intensify the hypotensive effect of the preparation Isachardine В® spray with simultaneous reception with other vasodilators (vasodilators), antihypertensives, beta-blockers, slow calcium channel blockers, antipsychotics (antipsychotics) and tricyclic antidepressants, in combination with ethanol, and also with inhibitors PDE5 (including sildenafil, vardenafil, tadalafil).

With simultaneous use with procainamide, quinidine, an increase in the hypotensive effect is also possible.

When combined with amiodoron, propranolol, blockers of slow calcium channels (verapamil, nifedipine and others), the antianginal effect may increase.

Simultaneous application of isosorbide dinitrate with dihydroergotamine can lead to an increase in the concentration in the plasma of the latter and, thus, enhance its hypertensive effect.

When used simultaneously with m-holinoblokatorami (atropine) increases the likelihood of increased intraocular pressure.

Nitro compounds can reduce the therapeutic effect of norepinephrine (noradrenaline).

Barbiturates accelerate metabolism and reduce the concentration of nitro compounds in the blood plasma.


The drug is released by prescription.


The drug should be stored out of reach of children, at a temperature of no higher than 30 В° C, away from the fire.
Shelf life - 4 years.
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