Isacardin® (Isacardin)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceIsosorbide dinitrateIsosorbide dinitrate
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    • Dosage form: & nbspspray sublingual dosed.
    Composition:Composition per 1 bottle (300 doses): active substance isosorbide dinitrate aqueous in the 100% isosorbide dinitrate - 0.375 g (1 dose contains 1.25 mg isosorbide dinitrate); Excipients: Macrogol-400 (polyethylene oxide-400) 1.8 g, ethanol 96% to 15 ml.
    Description:Transparent colorless or yellowish liquid with an alcohol smell.
    Pharmacotherapeutic group:Vasodilators from the group of organic nitrates
    ATX: & nbsp

    C.05.A.E.02   Isosorbide dinitrate

    C.01.D.A.08   Isosorbide dinitrate

    Pharmacodynamics:
    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 (BP), a decrease in the total peripheral vascular resistance (postload).
    Decrease in pre- and postnagruzki leads to a decrease in oxygen consumption by the myocardium. Improving the delivery of oxygen to the ischemic sites, reduces the zone-damage to the myocardium. 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 (CHD), 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 oral mucosa, the effect manifests itself after 30 seconds and lasts 15 to 120 minutes.
    Pharmacokinetics:
    Absorption is high. Bioavailability through oral mucosa - 60%. Connection with blood plasma proteins - 30%. The half-life (T1 / 2) is 60 minutes. Metabolized in the liver to two active metabolites:
    isosorbide-5-mononitrate, whose fraction is 75 to 85%, the half-life is 5 hours and isosorbide-2-mononitrate,
    which is 15-25% with a half-life of 2.5 hours. The drug is excreted by the kidneys (almost completely in the form of metabolites).
    Indications:
    - Cessation of angina attacks;
    - prevention of angina attacks (including before physical exertion);
    - acute myocardial infarction (including complicated by acute left ventricular failure);
    - a condition after the transferred myocardial infarction.
    Contraindications:
    - Hypersensitivity to nitrates or other components of the drug;
    - acute circulatory disturbance (shock, collapse);
    - severe arterial hypotension (systolic blood pressure below 90 mmHg, diastolic blood pressure below 60 mmHg);
    - severe hypovolemia;
    - cardiogenic shock if it is not possible 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 and cardiac tamponade;
    - severe aortic, subaortic and mitral stenosis;
    - cerebral hemorrhage;
    - severe anemia;
    - simultaneous administration of inhibitors of phosphodiesterase-5 (including, sildenafil, vardenafil, tadalafil) (risk of pronounced blood pressure lowering);
    - patients under 18 years of age (efficacy and safety not established).
    Carefully:
    The drug should be used 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 that are accompanied by increased intracranial pressure (including hemorrhagic stroke, craniocerebral trauma,
    cerebral trauma);
    - with severe renal failure, liver failure (risk of development of methemoglobinemia);
    - with hyperthyroidism;
    - with a closed-angle form of glaucoma;
    - in the elderly;
    - inadequate and inadequate nutrition.
    Pregnancy and lactation:
    Use of Isacardin® Spray in pregnancy is possible only 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 you need an emergency drug Isakardine spray, for example, to stop an attack of angina, you need to establish observation of the child for possible side effects.
    Dosing and Administration:
    Isakardine ® spray is used to spray on the oral mucosa, under the tongue.

    The solution should not be inhaled.Bring the spray close to the mouth and, pressing on the nebulizer, inject the solution into the oral cavity:
    - take a deep breath;
    - hold your breath;
    - inject the solution into the mouth (there may be 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.
    For relief of angina or to physical or emotional stress, which may cause an attack, it is necessary to inject the spray in the mouth 1-3 times with an interval of 30 seconds between injections to background respiration delay. A single dose of 3 injections for an arrest of an attack can be increased only on the recommendation of a doctor. In acute myocardial infarction, and congestive heart failure treatment is performed under the control of blood pressure, heart rate (HR) and a doctor's supervision, start with 1-3-spraying, with 30 second intervals between-spraying; in the absence of effect after 5 minutes, you can repeat 1 injection; if no improvement occurs, after 10 minutes repeat 1 injection again. When using Isacardin Spray for the first time, or if it takes more than a day to break, you should press the spray gun several timesthe appearance of the first drops of the solution. When using the spray bottle, keep it upright with a spray gun. Avoid contact with eyes.
    Side effects:The frequency of side effects is given according to the World Health Organization (WHO) classification: very often more than 1/10, often more than 1/100 and less than 1/10, infrequently more than 1/1000 and less than 1/100, rarely more than 1 / 10000 and less than 1/1000, very rarely - less than 1/10000, the frequency is unknown (according to available data, it is not possible to determine the frequency of development).
    From the central nervous system: very often - headache; often - dizziness, drowsiness, 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, including cross-over to other nitrates.
    Overdose:
    Symptoms: a marked decrease in blood pressure (less than 90 mm Hg), pallor, increased sweating, "threadlike" pulse, tachycardia, dizziness, headache, weakness, fainting, nausea, vomiting, diarrhea, methemoglobinemia (accompanied by tachypnea, anxiety, loss of consciousness , cardiac arrest). When using high doses of isosorbide dinitrate, 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 the circulating blood volume (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 the sodium salt intravenously 0.1-0.15 ml / kg 1% solution (up to 50 ml), oxygen therapy, mechanical ventilation, hemodialysis.
    Interaction:It is possible to intensify the hypotensive effect of the preparation Isachardine ® spray with simultaneous reception with other vasodilators (vasodilators), antihypertensive drugs, beta-blockers, slow calcium channel blockers, antipsychotic drugs (antipsychotics) and tricyclic antidepressants, in combination with ethanol, when using phosphodiesterase-5 inhibitors (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, etc.), it is possible to increase the antianginal effect. 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.
    Special instructions: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 may cause tolerance development, in this case it is recommended to cancel for 24 to 48 hours, or after 3-6 weeks of regular admission, to take a break for 3-5 days, replacing the preparation of Isacardin ® spray with other antianginal drugs at 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 Isacardin ® spray should be excluded from the use of ethanol (alcohol).
    Effect on the ability to drive transp. cf. and fur:When using the drug Isacardin Spray, care must be taken when driving vehicles and mechanisms (risk of dizziness).
    Form release / dosage:
    Spray sublingual dosage 1.25 mg / dose.
    Packaging:For 15 ml (300 doses) in bottles of brown glass. Vials are supplied with a mechanical dosing pump with a nebulizer. Each bottle is glued with a self-adhesive label. Each bottle together with a nebulizer, safety cap and instruction (leaflet) is placed in a pack of cardboard.
    Storage conditions:At a temperature of no higher than 30 ° C, away from fire. Keep out of the reach of children.
    Shelf life:4 years. Do not use after expiry date.
    Terms of leave from pharmacies:On prescription
    Registration number:LP-000348
    Date of registration:22.02.2011
    Manufacturer: & nbsp
    Information update date: & nbsp05.09.2013
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