Composition, form of production and packaging
Concentrate for the preparation of solution for infusions is transparent, colorless.
1 ml of 1 amp.
isosorbide dinitrate 1 mg 10 mg
Excipients: sodium chloride - 9 mg, water d / and - up to 1 ml.
10 ml - glass ampoules with a ring of a break (5) - packages cellular contour polymeric (2) - packs cardboard.
10 ml - glass ampoules with a break point (5) - packings of cellular contour polymeric (2) - packs cardboard.
10 ml - glass ampoules without break ring (5) with ampoule knife or scarifier - packings, cellular polymer contouring (2) - cardboard packs.
10 ml - glass ampoules without a break point (5) with a knife ampoule or scarifier - packings of cellular contour polymeric (2) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2015.
PHARMACHOLOGIC EFFECT
Peripheral vasodilator, mainly affecting the 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 guanylate cyclase, resulting in an increase in the content of cGMP (mediator of vasodilation), which ultimately leads to relaxation of smooth muscle 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. 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. 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 both at rest and during physical activity.
By reducing myocardial oxygen consumption and improving the oxygen delivery to the ischemic areas, it reduces the area of ​​myocardium damage, also relaxes the smooth muscles of the bronchi, gastrointestinal tract, bile and urinary tract.
PHARMACOKINETICS
Since the solution of Isacardinum is applied iv, 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 T 1/2 from 1.5 to 2 hours or from 4 to 6 hours, respectively. T 1/2 isosorbide dinitrate, administered iv, is 10 minutes.
INDICATIONS
- arresting a prolonged attack of angina (including unstable or vasospastic angina);
acute myocardial infarction;
acute left ventricular failure;
- control of blood pressure at its increase before and during surgical operations, especially in cardiovascular surgery.
DOSING MODE
The dosage regimen is set individually according to the patient's clinical condition and hemodynamic parameters.
Enter in / in slowly. The recommended starting dose is 1-2 mg / h depending on the response of the patient (under condition of monitoring of blood pressure, heart rate, ECG and diuresis). The maximum dose of the drug is 8-10 mg / h. For patients with heart failure, as a rule, higher doses are required - in some cases up to 50 mg / h. The average dose is approximately 7.5 mg / h.
Patients who used to take organic nitrates (for example, isosorbide dinitrate, isosorbide-5-mononitrate) can inject higher doses of Isacardin В® to achieve the desired hemodynamic effect.
The concentration of Isacardin В® 1 mg / ml should be administered in dissolved form by IV 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 Ојg / ml (0.01%) - 50 ml of Isacardin В® concentrate 1 mg / ml (5 ampoules of 10 ml), dilute in 450 ml of 0.9% sodium chloride solution.
To prepare a solution with a concentration of 200 Ојg / ml (0.02%) - 100 ml of Isacardin В® concentrate 1 mg / ml (10 ampoules of 10 ml), dilute in 400 ml of 0.9% sodium chloride solution.
Dose calculation table
Dose 0.01% solution 0.02% solution
mg / h ml / h drop / min ml / h drop / 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
6 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 EFFECT
Possible side effects are given below for body systems and frequency of occurrence: very often (> 1/10), often (> 1/100 and <1/10), infrequently (> 1/1000 and <1/100), rarely (> 1/10 000 and <1/1000), very rarely (<1/10 000, including individual messages).
From the cardiovascular system: often - tachycardia, orthostatic hypotension; infrequently, the paradoxical intensification of angina attacks, collapse (sometimes accompanied by bradyarrhythmia and syncope), transient hypoxemia due to relative redistribution of blood flow to hypoventilated alveolar sites (in patients with ischemic heart disease - may lead to myocardial hypoxia).
From the side of the digestive system: infrequently - nausea, vomiting; very rarely - heartburn.
From the side of the central nervous system: very often - headache; often - drowsiness, dizziness.
From the skin and subcutaneous tissues: infrequently - skin allergic reactions (including rashes), hyperemia of the facial skin; very rarely - angioedema, Stevens-Johnson syndrome; frequency unknown - exfoliative dermatitis.
General disorders: often - asthenia.
CONTRAINDICATIONS
- 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;
- an angle-closure glaucoma;
- simultaneous reception of PDE5 inhibitors (including sildenafil, vardenafil in the previous 24 hours, tadalafil in the previous 48 hours and more);
- age under 18 years (effectiveness and safety not established);
- hypersensitivity to the components of the drug;
- Hypersensitivity to other nitrocompounds.
Carefully:
- low filling pressure of the left ventricle, incl. with 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 insufficiency;
severe hepatic impairment;
- hypothyroidism;
- Inadequate and malnutrition;
- Pregnancy;
lactation period.
PREGNANCY AND LACTATION
The use of Isacardin В® during pregnancy and lactation is possible only if the intended benefit to the mother exceeds the risk to the fetus and / or the child.
APPLICATION FOR FUNCTIONS OF THE LIVER
With caution: severe renal failure.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
With caution: severe hepatic impairment.
APPLICATION FOR CHILDREN
Contraindicated at the age of 18 years (efficacy and safety not established).
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. The prepared working solution of the preparation Izacardin В® 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!
OVERDOSE
Symptoms: a decrease in blood pressure of less than 90 mm Hg, paleness, increased sweating, threadlike pulse, tachycardia, postural dizziness, throbbing headache, weakness, dizziness, nausea, vomiting, diarrhea, methemoglobinemia, cyanosis, followed by development of tachypnea, 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, BCC compensation should be made. In exceptional cases, norepinephrine (noradrenaline) and / or dopamine can be administered to maintain blood circulation.
The introduction of epinephrine (adrenaline) and related compounds is contraindicated!
With methemoglobinemia, depending on the degree of severity, intravenous ascorbic acid is administered in the form of a sodium salt; oxygen therapy, hemodialysis, exchange blood transfusion.
DRUG INTERACTION
It is possible to intensify the hypotensive effect when using isosorbide dinitrate with:
- antihypertensive agents (for example, beta-adrenoblockers, diuretics, slow calcium channel blockers, ACE inhibitors);
- vasodilators (vasodilators);
- antipsychotic drugs (neuroleptics);
- Tricyclic antidepressants;
- ethanol and ethanol-containing products.
With simultaneous administration of the drug and PDE5 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 IV introduction weakens the anticoagulant effect of heparin.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored in a place protected from light, inaccessible to children, at a temperature of no higher than 25 В° C. Shelf life - 3 years.
