Isacardin - instructions for use, doses, side effects, contraindications

Active substanceIsosorbide dinitrateIsosorbide dinitrate

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UPDATE OF PFC, CJSC Russia

Dosage form: & nbspconcentrate for solution for infusion

Composition:

Composition per ml:

active substance: isosorbide dinitrate aqueous in the recalculation of 100% isosorbide dinitrate -1 mg;

Excipients: sodium chloride 9 mg, water for injection up to 1 ml.

Description:clear colorless liquid

Pharmacotherapeutic group:vasodilator - nitrate

ATX: & nbsp

C.05.A.E.02 Isosorbide dinitrate

C.01.D.A.08 Isosorbide dinitrate

Pharmacodynamics:

Izakardine is a peripheral vasodilator that primarily affects venous vessels. Has an antianginal effect, causes an antihypertensive effect. The mechanism of action is associated with the release of nitric oxide (endothelial relaxing factor) in the vascular endothelium, which causes activation of intracellular anilate cyclase, which results in an increase in the content,cyclic guanosine monophosphate (cGMP) (a mediator of vasodilation), which ultimately leads to relaxation of the smooth muscles of the vessels.

Isosorbide dinitrate 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 (LV). 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. Promotes redistribution of coronary blood flow in favor of subendocardial zones, especially in coronary artery atherosclerosis (mostly large). Vasodilation of the collateral arteries can improve the blood supply of the myocardium. Copes coronary spasm; improves hemodynamics in patients with chronic heart failure (CHF) both at rest and during physical exertion.

By reducing myocardial oxygen consumption and improving oxygen delivery to ischemic sites, reduce the area of myocardium damage,relaxes also the smooth muscles of the bronchi, the gastrointestinal tract (GIT), the biliary and urinary tract.

Pharmacokinetics:

Since the solution of Isacardin is administered intravenously, there is no effect of "first passage" through the liver.

Isosorbide dinitrate is metabolized by the participation of the glutathione-S-transferase enzyme system. The active metabolites formed during the cleavage of the nitro group, isosorbide-2-nitrate and isosorbide-5-nitrate, have a half-life of 1.5 to 2 hours or 4 to 6 hours, respectively. The half-life of isosorbide dinitrate, administered intravenously, is 10 minutes.

Indications:

- Kupirovanie a prolonged attack of angina pectoris (including unstable or vasospastic angina);

- Acute myocardial infarction,

- Acute left ventricular failure (LV) insufficiency

- Control of blood pressure when it is raised before and during surgery, especially in cardiovascular surgery.

Contraindications:

- Hypersensitivity to isosorbide dinitrate, other nitro compounds or excipients.

- Acute circulatory disturbance (shock, collapse).

- Cardiogenic shock (if no measures are taken to maintain the end diastolic pressure).

- Hypertrophic obstructive cardiomyopathy.

- Constrictive pericarditis.

- Cardiac tamponade.

- Severe arterial hypotension (systolic blood pressure below 90 mm Hg).

- Severe hypovolemia.

- Severe anemia.

- Severe aortic and subaortic stenosis, mitral stenosis.

- Hemorrhage in the brain.

- Closed-angle glaucoma.

- Simultaneous administration of inhibitors of phosphodiesterase-5 (including sildenafil, vardenafil in the previous 24 hours, tadalafil in the previous 48 hours and more).

- Age to 18 years (effectiveness and safety not established).

Carefully:

- low filling pressure of the left ventricle, including acute myocardial infarction, left ventricular dysfunction (eg, left ventricular failure);

- aortic and / or mitral stenosis;

- diseases accompanied by increased intracranial pressure (until now, increased intracranial pressure was observed only after intravenous injection of nitroglycerin in high doses);

- propensity to orthostatic hypotension;

- severe renal and / or hepatic insufficiency,

- hypothyroidism,

- inadequate and malnutrition;

- pregnancy and lactation.

Pregnancy and lactation:Use of Isacardin during pregnancy and lactation is possible only if the intended benefit to the mother exceeds the risk to the fetus and / or the baby.

Dosing and Administration:

The dosage regimen is set individually according to the patient's clinical condition and hemodynamic parameters.

Enter intravenously slowly. The recommended starting dose is 1-2 mg / h depending on the patient's response (under condition of monitoring of blood pressure, heart rate: abbreviations (heart rate), electrocardiogram (ECG) and diuresis). The maximum dose of the drug is 8-10 mg / hour. For patients with heart failure, like. usually, higher doses are required - in some cases up to 50 mg / h. The average dose is approximately 7.5 mg / hour.

Patients who used to take organic nitrates (for example, isosorbide dinitrate, isosorbide-5-mononitrate), higher doses of Isacardin may be administered to achieve the desired hemodynamic effect.

Isucardine concentrate 1 mg / ml should be administered in a dissolved form intravenously with the help of automatic infusion systems (or as a last resort in the form of drop infusion) in hospital conditions under constant monitoring of cardiovascular system parameters.

To prepare a solution with a concentration of 100 μg / ml (0.01%) - 50 ml of Isacardin concentrate 1 mg / ml (5 ampoules of 10 ml), dilute in 0,9% sodium chloride solution in 450 ml;

To prepare a solution with a concentration of 200 μg / ml (0.02%) - 100 ml of Isacardine concentrate 1 mg / ml (10 ampoules per 10 ml), dilute in 400 ml of 0.9% sodium chloride solution.

Dose	0.01% solution		0.02% solution
mg / hour	ml / hour	"drops / min	ml / hour	drops / min
1	10	3-4	5	1-2
2	20	7	10	3
3	30	10	15	5
4	40	13	20	7
5	50	17	25	8
b	60	20	30	10
7	70	23	35	12
8	80	27	40	13
9	90	30	45	15
10	100	33	50	17

1 ml corresponds to 20 drops.

Depending on the clinical picture, the parameters of hemodynamics and ECG treatment can be continued up to 3 days or longer.

Side effects:

Possible side effects are given below for the body systems and frequency of occurrence: 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), including individual messages.

From the side of the cardiovascular system

Often: tachycardia, orthostatic hypotension.

Infrequently "paradoxical" amplification strokes, collapse (sometimes accompanied by bradyarrhythmia and syncope); transient hypoxemia due to a relative redistribution of the blood flow in gipoventiliruemye alveolar areas (in patients with coronary artery disease, heart can lead to myocardial hypoxia).

From the gastrointestinal tract

Infrequent: nausea, vomiting.

Very rarely: heartburn.

From the central nervous system

Very often: headache.

Often: drowsiness, dizziness.

From the skin and subcutaneous tissues

Uncommon: allergic skin reactions (including rash), flushing of the skin. Very rarely: angioedema, Stevens-Johnson syndrome. The frequency is unknown: exfoliative dermatitis.

General disorders

Often: asthenia.

Overdose:

Symptoms: decrease in blood pressure less than 90 mm Hg, paleness, increased sweating, threadlike pulse, tachycardia, postural dizziness, throbbing headache, weakness, dizziness, nausea, vomiting, diarrhea, methaemoglobinaemia, cyanosis, followed by development of tachypnea, feelings of anxiety, loss of consciousness and heart failure.

The use of high doses of the drug may cause an increase in intracranial pressure, which can cause cerebral symptoms. .

Treatment: discontinue further administration of the drug. It is necessary to lower the head of the bed and raise the patient's legs. As a rule, blood pressure is normalized within 15-20 minutes after discontinuation of the drug administration.

In the case of severe arterial hypotension, the volume of circulating blood should be compensated. In exceptional cases, to maintain circulation, norepinephrine (norepinephrine) and / or dopamine.

The introduction of epinephrine (adrenaline) and related compounds is contraindicated!

At a methemoglobinemia depending on a degree of gravity are appointed or nominated - intravenously ascorbic acid in the form of a sodium salt; oxygen therapy, hemodialysis, exchange blood transfusion.

Interaction:

It is possible to intensify the hypotensive effect when using isosorbide dinitrate with:

- antihypertensive agents (eg, beta-adrenergic blockers, diuretics, blockers of "slow", calcium channels, angiotensin-converting enzyme inhibitors);

- vasodilators (vasodilators),

- antipsychotic drugs (neuroleptics),

- tricyclic antidepressants,

- ethanol and ethanol-containing products.

With the simultaneous administration of the drug and phosphodiesterase-5 inhibitors (including sildenafil, tadalafil, vardenafil), potentiation of hypotensive action is possible.

With simultaneous application with dihydroergotamine, an increase in concentration and an increase in its hypotensive effect are possible.

Isosorbide dinitrate with intravenous administration weakens the anticoagulant effect of heparin.

Special instructions:

During treatment, the following parameters of the cardiovascular system should be monitored: blood pressure (not lower than 100 mm Hg); ECG monitoring; heart rate; volume of urination (catheter).

Infusion materials made of polyvinyl chloride or polyurethane cause the loss of the active component as a result of adsorption, which must be compensated for by increasing the dose. Prepared a working solution of the drug Isacardin should be protected from exposure to intense light.

In case of precipitation of crystals (turbidity), the drug should not be used. The solution should be used within 24 hours after breeding!

Form release / dosage:

Concentrate for the preparation of a solution for infusions 1 mg / ml.

Packaging:

For 10 ml in ampoules of light-protective or transparent glass with a color ring of the fracture or without. 5 ampoules in a cassette made of polyethylene terephthalate. 2 cassettes together with instructions for medical use in a pack of cardboard. In addition, ampoule knives or scarifiers are placed in bundles with ampoules without a colored ring of the break.

Storage conditions:In the dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:3 years. Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:PL-000326

Date of registration:22.02.2011

Manufacturer: & nbsp

FARMAK, JSC Ukraine

Information update date: & nbsp31.07.2013

Illustrated instructions

Instructions

Isacardin® (Izakardin)