Isacardin, 1.25 mg/dose 300 doses 15 ml

Peripheral vasodilator with predominant effect on venous vessels. It stimulates the formation of nitric oxide (endothelial relaxing factor) in the vascular endothelium, causing activation of intracellular guanylate cyclase, the consequence of which is an increase of cyclic guanosine monophosphate (cGMP), mediator of vasodilation.

Limits myocardial oxygen demand by reducing preload (decreases left ventricular end-diastolic volume (EDV) and reduces systolic wall tension). It has coronary dilator effect. It acts on peripheral arteries and veins. Relaxation of the veins leads to a decrease in venous return to the heart (preload), which reduces the filling pressure of the left ventricle. There is also (although to a lesser extent) dilation of arterial vessels, which is accompanied by a decrease in BP, a decrease in PPS (post-load).

The decrease in pre- and post-load leads to a decrease in myocardial oxygen consumption. By improving oxygen delivery to ischemic areas, it reduces the area of myocardial damage. Reduces blood flow to the right atrium, reduces pressure in the small circle of circulation and regresses the symptoms of pulmonary edema. It promotes redistribution of coronary blood flow in favor of subendocardial zones, especially in atherosclerosis of coronary arteries (mainly large ones). Vasodilatation of collateral arteries may improve the blood supply to the myocardium. Increases exercise tolerance in patients with CHD, angina pectoris.

Limiting myocardial oxygen consumption and improving oxygen delivery to ischemic areas, reduces the area of myocardial damage, also relaxes the smooth muscles of the bronchi, gastrointestinal tract, biliary and urinary tract.

Dilates cerebral vessels, dura mater, which may be accompanied by headache. As with other nitrates, cross-tolerance develops.

After withdrawal (interruption of treatment), sensitivity to it is quickly restored. After spraying on the oral mucosa, the effect is evident in 30 seconds and lasts 15-120 minutes.

Pharmacokinetics

The absorption is high. Bioavailability through the oral mucosa is 60%. Blood plasma protein binding – 30%. T_1/2 is 60 min. It is metabolized in the liver to two active metabolites – isosorbide-5-monononitrate, which is 75-85%, T_1/2 is 5 h and isosorbide-2-monononitrate, which is 15-25% with T_1/2 2.5 h.

The drug is excreted by the kidneys (almost completely as metabolites).

Indications

Active ingredient

Composition

How to take, the dosage

The drug Isacardin® sublingual dosage spray is used for spraying on the mucosa of the mouth, under the tongue. The solution should not be inhaled. Bring the spray close to the mouth and press the atomizer to inject the solution into the oral cavity:

– take a deep breath;

– hold your breath;

– squirt the solution in your mouth (you might have a mild burning sensation on your tongue);

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

One dose of this medicine contains 1.25 mg isosorbide dinitrate.

To relieve an attack of angina or before physical or emotional exertion that may cause an attack, the spray should be injected by mouth 1-3 times with 30 seconds between injections while holding your breath. The single dose of 3 injections to end a seizure should only be increased on the advice of the physician.

In acute myocardial infarction and acute heart failure, therapy should be started under control of BP, HR and under medical supervision, starting with 1-3 injections with 30-second intervals between injections; if there is no effect, 1 injection may be repeated after 5 min; if there is no improvement, 1 injection should be repeated after 10 min again. When using Isacardin® Spray for the first time or if there is a break in use for more than 24 hours, press the sprayer several times until the first drops of solution appear. During use the spray bottle should be held vertically with the atomizer upwards. Avoid getting the spray in the eyes.

Interaction

The hypotensive effect of the drug Isacardin® may be increased Hypodiazeptic spray when taken simultaneously with other vasodilators (vasodilators), hypotensive drugs, beta-adrenoblockers, BCCs, antipsychotics (neuroleptics) and tricyclic antidepressants, in combination with ethanol, as well as – when using FDE-5 inhibitors (incl.

In concomitant use with procainamide, quinidine it is also possible to increase the hypotensive effect.

When combining with amiodarone, propranolol, BCCs (verapamil, nifedipine, etc.) may increase the antianginal effect.

The concomitant use of isosorbide dinitrate with dihydroergotamine may lead to increased plasma concentrations of the latter and thus enhance its hypertensive effect.

Concomitant use with m-cholinoblockers (atropine) increases the possibility of IOP elevation.

Nitro compounds may decrease the therapeutic effect of norepinephrine (noradrenaline).

Barbiturates accelerate metabolism and decrease plasma concentrations of nitro compounds.

Special Instructions

A BP and HR should be monitored during therapy. Abrupt withdrawal of the drug should be avoided; the dose should be reduced gradually. Frequent prescribing and high doses may cause the development of tolerance, in which case it is recommended to cancel for 24-48 hours, or after 3-6 weeks of regular use to make a break for 3-5 days, replacing for this time the drug Isacardin ®, sublingual dosed spray with other antianginal agents. Particularly careful medical supervision is necessary in acute myocardial infarction with reduced ventricular filling pressure. The solution contains about 85% of ethanol. During treatment with the drug Isacardin® Sublingual dosage spray the use of ethanol (alcohol) should be avoided.

Impact on the ability to drive vehicles and other mechanisms. When using the drug Isacardin®, sublingual dosage spray, caution must be exercised while driving vehicles and operating machinery (risk of dizziness).

Contraindications

– acute circulatory disturbance (shock, collapse);

– severe arterial hypotension (systolic BP below 90 mm Hg, diastolic BP below 60 mmHg.

– severe hypovolemia;

– cardiogenic shock if end-diastolic left ventricular pressure cannot be corrected by intra-aortic counterpulsation or drugs with positive inotropic action; – hypertrophic obstructive cardiomyopathy, constrictive pericarditis, cardiac tamponade;

– severe aortic, subaortic and mitral stenosis;

– cerebral hemorrhage;

– severe anemia;

– concomitant use of FDE5 inhibitors (including sildenafilsildenafil, vardenafil, tadalafil- risk of significant BP decrease;

– age less than 18 years (efficacy and safety not established);

– hypersensitivity to nitrates or other drug components.

With caution:

– in low left ventricular filling pressure, including In acute myocardial infarction;

– with aortic or mitral stenosis;

– with a tendency to orthostatic reactions (a sharp decrease in BP with changes in body position);

– with conditions accompanied by increased intracranial pressure (including

– In diseases accompanied by increased intracranial pressure (including hemorrhagic stroke, craniocerebral trauma);

– In patients with hepatic insufficiency (risk of methemoglobinemia);

– In patients with severe renal failurep>- in hyperthyroidism;

– in closed-angle glaucoma;

– in the elderly;

– in poor and inadequate nutrition;

– toxic pulmonary edema.

Side effects

Possible side effects are listed below by body system and frequency of occurrence: very common (more than 1/10); common (more than 1/100 and less than 1/10); infrequent (more than 1/1000 and less than 1/100), rare (more than 1/10000 and less than 1/1000); very rare (less than 1/10000), frequency is unknown (according to available data it is impossible to determine the frequency of development).

CNS disorders: very common – headache; common – dizziness, somnolence, blurred vision.

Systemic system disorders: frequent – orthostatic hypotension, reflex tachycardia; infrequent – paradoxical worsening of angina attacks, collapse (accompanied by bradyarrhythmia and fainting), transient hypoxemia due to relative redistribution of blood flow to hypoventilated alveolar areas (in patients with CHD can lead to myocardial hypoxia).

Digestive system disorders: frequently – tongue burning; infrequently – nausea, vomiting; very rarely – heartburn.

Skin disorders: infrequent – skin allergic reactions (including skin rash), flushing of blood to the skin of the face; very rare – angioedema, Stevens-Johnson syndrome; frequency unknown – exfoliative dermatitis.

Others: frequent – asthenia. Possible development of tolerance, including cross-tolerance to other nitrates.

Overdose

Symptoms: marked BP decrease (less than 90 mm Hg), pallor, increased sweating, thready pulse, tachycardia, dizziness, headache, weakness, fainting, nausea, vomiting, diarrhea, methemoglobinemia (accompanied by tachypnea, anxiety, loss of consciousness, cardiac arrest).The use of high doses of the drug may cause increase in IOP,

Treatment: in mild cases, transfer the patient to the supine position with the legs elevated or the head end of the bed lowered; in more severe cases, with a marked decrease in BP, replenishment of the BCC, administration of norepinephrine or vasoconstrictors (vasoconstrictors) such as phenylephrine, dopamine (use of epinephrine is not recommended); in case of methemoglobinemia – ascorbic acid – 1 g orally or in the form of sodium salt – IV 0.1-0.15 ml/kg 1% solution (up to 50 ml), oxygen therapy, AVI, hemodialysis.

Pregnancy use

Pregnant use of the drug Isacardin® sublingual dosage spray is possible only when the expected benefits exceed the potential risk to the fetus and child, and should be conducted under medical supervision. If it is necessary to use isosorbide dinitrate during breastfeeding, breastfeeding should be stopped because there are data on penetration of nitrates into the breast milk. If there is a need for emergency administration of Isacardin® sublingual dosage spray, e.g. to relieve an attack of angina pectoris, the child should be monitored for possible side effects.

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