ISOKET CONCENTRATE FOR THE SOLUTION OF AMPOULE 1 MG/ML 10 ML

Mechanism of action

Peripheral vasodilator with a predominant effect on the venous vessels. Antianginal agent. The mechanism of action is associated with the release of the active substance nitric oxide in the smooth muscles of the blood vessels. Nitric oxide causes activation of guanylate cyclase and increases the level of cGMP, which ultimately leads to relaxation of vascular smooth muscle. The action of isosorbide dinitrate is mainly associated with a decrease in myocardial oxygen demand due to a decrease in preload (dilation of peripheral veins and a decrease in blood flow to the right atrium) and afterload (decrease in OPS), as well as direct coronary dilating. It promotes the redistribution of coronary blood flow in the ischemic areas.
Increases exercise tolerance in patients with coronary artery disease. In heart failure, it helps to relieve the myocardium by reducing preload. Reduces pressure in the pulmonary circulation.
The action of the drug begins immediately after application of the aerosol.

Each time you press the sprayer an equal amount of solution is sprayed in the form of tiny droplets in the mouth. Isosorbide dinitrate easily penetrates through the mucous membrane of the mouth and very quickly (after a few seconds) enters the bloodstream.

Indications and usage

- relief of angina attacks;
- prevention of strokes (for example, the use of the drug before exercise or emotional stress);
- acute myocardial infarction;
- acute left ventricular failure.

For relieving angina pectoris or for the prevention of its occurrence (before physical or emotional stress) The aerosol is sprayed in the oral cavity 1-3 times (at a dose of 1.25-3.75 mg) with an interval of 30 seconds between injections. The maximum single dose is 3.75 mg (3 injections), the excess of which is possible only in exceptional cases.
At acute myocardial infarction and acute heart failure Start with a single dose of 1.25-3.75 mg (1-3 injections) under strict control of blood pressure.If there is no effect for 5 minutes, the injection can be repeated (with careful medical control). If the improvement does not occur within 10 minutes, another application of the aerosol is possible during blood pressure monitoring.
Aerosol application rules
Isoket in the form of an aerosol is sprayed into the oral cavity. Do not inhale the solution.
When applying the bottle, you need to bring it to your mouth, then take a deep breath and hold your breath, then inject the solution (with a slight burning sensation on the tongue), close your mouth and breathe through your nose for about 30 seconds.
When applying the spray bottle should be held vertically spray up.
When you first use and with a break in the use of the drug (more than a day) should check the operation of the sprayer.

Adverse reactions

Cardiovascular: It is possible (at the first use or when the dose is increased) a decrease in blood pressure, orthostatic hypotension (with reflex tachycardia, lethargy, as well as dizziness and a feeling of weakness), "nitrate" headaches (arising at the beginning of treatment and disappearing, usually with further use of the drug ); rarely, increased symptoms of angina (with a marked decrease in blood pressure); in rare cases, collaptoid states, sometimes with bradycardia and syncope.
Gastrointestinal: rarely - nausea, vomiting.
Dermatologic: rarely - redness of the skin; in some cases - exfoliative dermatitis.
Allergic reactions: rarely a skin rash.

Contraindications

- vascular collapse;
- severe arterial hypotension (systolic blood pressure below 90 mm Hg);
- cardiogenic shock (if it is impossible to correct the end-diastolic pressure of the left ventricle using intra-aortic contraception or drugs with a positive inotropic effect);
- simultaneous administration of phosphodiesterase-5 inhibitors (for example, sildenafil).
- hypersensitivity to the drug or other nitrates.
Isoket spray can not be used in the event of an angina attack while using the phosphodiesterase-5 inhibitor (sildenafil).

Pregnancy and breastfeeding

During pregnancy and lactation, the drug is prescribed only in cases where the intended benefit to the mother outweighs the potential risk to the fetus or child due to the lack of sufficient clinical experience of its use during these periods.

Special notes

With caution and under close medical supervision, the drug is used in acute myocardial infarction with a reduced ventricular filling pressure (a decrease in systolic blood pressure below 90 mm Hg should be avoided); with hypertrophic obstructive cardiomyopathy, constrictive pericarditis, cardiac tamponade, with aortic or mitral stenosis; with diseases accompanied by increased intracranial pressure; in patients with a tendency to orthostatic reactions.
When using the drug should be borne in mind that the composition of the aerosol includes 85 vol.% Ethanol.
In appointing the drug should take into account the possibility of drug interaction, even at the very beginning of the use of Isoketa.
Avoid contact with the aerosol.
Isoket spray does not contain freon, harmless to the environment.
On the label of the bottle, below, there is an arrow. When the liquid level in the vial reaches the upper edge of the arrow, the next vial of aerosol must be purchased. Further use of such a vial is possible as long as the tip of the suction tube is still immersed in the liquid with a slight tilt. Transparent bottle allows you to notice the need for replacement.
Influence on ability to drive motor transport and control mechanisms
The question of the possibility of practicing potentially hazardous activities should be resolved only after evaluating the patient's individual response to the drug. This is especially important to consider at the beginning of treatment, with increasing doses and changing the drug, as well as the simultaneous use of alcohol.

Overdosage

Symptoms: may increase the described side effects.
Treatment: if necessary, conduct symptomatic therapy.

Drug Interactions

With simultaneous use with phosphodiesterase-5 inhibitors (for example, sildenafil), hypotensive effect may be enhanced (this combination is contraindicated.)
It is possible to enhance the hypotensive action of Izoket aerosol, while using it with other peripheral vasodilators, antihypertensive drugs, beta-blockers, Calcium channel blockers, neuroleptics and tricyclic antidepressants, as well as ethanol.
The simultaneous use of Izoketa aerosol with dihydroergotamine can lead to an increase in the concentration of dihydroergotamine in the blood and, thus, to enhance its action.

The aerosol form of izoket should be kept out of the reach of children at room temperature.