Izacardin
Izakardin: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Conditions for dispensing pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Isacardin
ATX code: C01DA08
Active ingredient: isosorbide dinitrate (Isosorbide dinitrate)
Producer: NPF Mikrokhim, LLC (Ukraine), OZON, LLC (Russia), FKP Armavir biofactory (Russia)
Description and photo update: 2019-11-07
Prices in pharmacies: from 247 rubles.
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Isacardine is a peripheral vasodilator with antianginal effects.
Release form and composition
- concentrate for the preparation of a solution for infusion: colorless transparent liquid (10 ml in an ampoule made of transparent / light-shielding glass with or without a ring or break point, in a polymer blister strip packaging 5 ampoules, in a cardboard box 2 contour packs; for ampoules without a ring / dot breaks are applied with scarifiers or ampoule knives);
- dosed sublingual spray: colorless or pale yellow, transparent, with an alcoholic odor [15 ml (300 doses) in a brown glass bottle equipped with a mechanical dosing pump with a spray, in a cardboard box 1 bottle with a safety cap].
Each pack also contains instructions for the use of Izakardin.
1 ml of concentrate contains:
- active substance: aqueous isosorbide dinitrate (calculated as 100% isosorbide dinitrate) - 1 mg;
- additional components: sodium chloride, water for injection.
1 spray dose contains:
- active substance: aqueous isosorbide dinitrate (in terms of 100% isosorbide dinitrate) - 1.25 mg;
- additional components: ethanol 96%, macrogol 400 (polyethylene oxide 400).
Pharmacological properties
Pharmacodynamics
Isacardine is a peripheral vasodilator that mainly affects the venous vessels. Possesses antianginal action, provides hypotensive effect. The mechanism of action of the drug consists in the release of nitric oxide (endothelial relaxing factor) in the endothelium of the vascular walls, which initiates the activation of the intracellular enzyme guanylate cyclase, resulting in an increase in guanosine monophosphate (cGMP), a mediator of vasodilation, and as a result, relaxation of vascular smooth muscles.
By reducing the level of preload (reducing the end-diastolic volume of the left ventricle and reducing the systolic tension of its walls) isosorbide dinitrate helps to reduce the oxygen demand of the heart muscle. The active substance exhibits a coronary dilating effect, peripheral veins and arteries are exposed to the influence of Isacardin. Due to the relaxation of the veins, there is a decrease in venous return to the heart (preload), which helps to reduce the filling pressure of the left ventricle. To a lesser extent, the expansion of the arteries is also recorded, while there is a decrease in blood pressure (BP), a decrease in total peripheral vascular resistance (OPSR) - afterload.
By reducing pre- and afterload, there is a decrease in myocardial oxygen consumption. As a result of improved oxygen delivery to ischemic areas, the zone of damage to the heart muscle decreases. Isacardine also helps to relax the smooth muscles of the bronchi, gastrointestinal tract (GIT), bile and urinary tract.
Due to the action of isosorbide dinitrate, blood flow to the right atrium decreases, the pressure in the pulmonary circulation, and also with pulmonary edema, regression of symptoms is noted. In the area with low blood circulation, Isacardine helps to regulate coronary blood flow. Leads to increased exercise tolerance in patients with coronary heart disease (CHD), angina pectoris.
By expanding the vessels of the brain, dura mater, the drug can provoke the appearance of a headache.
To Izakardin, as well as to other drugs from the nitrate group, cross-tolerance occurs, however, after a break in therapy or withdrawal of the drug, sensitivity to it is quickly restored.
After spraying the spray on the oral mucosa, its effect appears after 30 seconds and lasts 15–120 minutes.
Pharmacokinetics
Concentrate for the preparation of solution for infusion Isacardin in ampoules is used intravenously (i / v), therefore the drug does not undergo the effect of primary passage through the liver. The metabolic transformation of isosorbide dinitrate occurs with the participation of the glutathione-S-transferase enzyme system.
When using the product in the form of a sublingual spray, high absorption is recorded. Bioavailability through the oral mucosa - 60%. It binds to plasma proteins by 30%.
The half-life (T ½) of the active substance with intravenous administration is 10 minutes, with sublingual administration - 60 minutes. The active metabolites formed as a result of biotransformation - isosorbide-5-nitrate and isosorbide-2-nitrate - have T ½ from 4 to 6 and from 1.5 to 2 hours (when using a spray - 2.5 hours), respectively. The agent is excreted by the kidneys almost completely in the form of metabolites.
Indications for use
Concentrate for solution for infusion
- relief of a prolonged attack of angina pectoris, including in the case of unstable or vasospastic angina pectoris;
- acute left ventricular failure;
- acute myocardial infarction;
- control of blood pressure when it rises before and during surgery, especially in cardiovascular surgery.
Sublingual metered spray
- relief of angina attacks;
- acute left ventricular failure;
- acute myocardial infarction;
- prevention of angina attacks, including before physical / emotional stress.
Contraindications
Absolute:
- acute vascular insufficiency (vascular collapse);
- acute circulatory disorders, including shock, collapse (for concentrate);
- cardiogenic shock (if it is impossible to correct the end-diastolic pressure of the left ventricle using intra-aortic counterpulsation or drugs with a positive inotropic effect);
- severe arterial hypotension [systolic blood pressure (SBP) below 90 mm Hg. Art., diastolic blood pressure (DBP) below 60 mm Hg. Art.];
- hypertrophic obstructive cardiomyopathy;
- cardiac tamponade;
- constrictive pericarditis;
- severe aortic and subaortic stenosis, mitral stenosis;
- severe hypovolemia;
- severe anemia;
- deficiency of glucose-6-phosphate dehydrogenase (for spray);
- traumatic brain injury (for concentrate), cerebral hemorrhage;
- increased intraocular pressure (IOP), including angle-closure glaucoma (for concentrate);
- combined use with a soluble guanylate cyclase stimulator - riociguat (the risk of arterial hypotension is aggravated);
- combination therapy with phosphodiesterase type 5 inhibitors (PDE-5) (including vardenafil, sildenafil, udenafil, tadalafil), since they enhance the antihypertensive effect of nitrates;
- age up to 18 years;
- lactation period (if necessary, emergency use is allowed to use Izakardin in the form of a spray);
- hypersensitivity to any component of the drug or other organic nitrates.
Relative (use Isacardine with caution):
- low filling pressure of the left ventricle, including in acute myocardial infarction, dysfunction of the left ventricle, for example, in left ventricular failure (it is required to prevent a decrease in systolic blood pressure of less than 90 mm Hg);
- tendency to orthostatic hypotension (orthostatic dysregulation of blood circulation);
- mild / moderate aortic and / or mitral stenosis;
- diseases occurring with an increase in intracranial pressure (ICP), including hemorrhagic stroke, traumatic brain injury (until now, an increase in ICP was recorded only after intracranial infusion of nitroglycerin in large doses);
- severe renal and / or liver failure;
- angle-closure glaucoma (due to the risk of increased IOP) (for spray);
- hypothyroidism;
- old age (for spray);
- insufficient or inadequate nutrition;
- pregnancy.
Izakardin, instructions for use: method and dosage
Concentrate for solution for infusion
The drug must be injected slowly.
The attending physician sets the dosage regimen individually, based on the hemodynamic parameters and the clinical condition of the patient.
The recommended initial dose is 1–2 mg / h, taking into account the patient's response and subject to monitoring of urine output, blood pressure, heart rate (HR) and electrocardiogram (ECG). The maximum dose is 8-10 mg / hour, the average dose is about 7.5 mg / hour. In patients who previously received organic nitrates, such as nitroglycerin, isosorbide-5-mononitrate, isosorbide dinitrate, to achieve the required hemodynamic effect, it is allowed to use higher doses of Isacardine.
In the presence of heart failure, as a rule, it is necessary to prescribe higher doses, in some cases reaching 50 mg / hour.
The concentrate must be infused in a diluted form intravenously using automatic infusion systems, or undiluted through the use of a syringe infusion pump, in a hospital setting, with constant monitoring of the parameters of the cardiovascular system.
Isacardine in ampoules can be combined with the following infusion solutions: sodium chloride solution 0.9%, dextrose (glucose) solution 5-30%, Ringer's solution, solutions containing albumin. In the case of combined use with other infusion solutions, it is required to take into account the manufacturer's information on compatibility, side effects and contraindications of these funds.
To prepare 500 ml of a solution for infusion at a concentration of 0.1 mg / ml (0.01%), 5 ampoules of 10 ml (50 ml) of concentrate are required; for 500 ml of solution for infusion at a concentration of 0.2 mg / ml (0.02%) - 10 ampoules of 10 ml (100 ml) of Isakardin concentrate.
Given the clinical picture, hemodynamic and ECG parameters, the course of treatment can be continued up to 3 days or more.
Sublingual metered spray
Isacardine spray is used sublingually.
The drug is administered by spraying on the oral mucosa, under the tongue. The drug should not be inhaled.
To take Isacardin, you need to bring the spray bottle close to your mouth, holding it vertically with the spray up. After taking a deep breath and holding your breath, you need to press the sprayer, injecting the solution into the oral cavity. During the injection, a slight burning sensation of the tongue may occur. After administration of the drug, you should close your mouth and breathe through your nose for about 30 seconds.
Recommended dosage regimen depending on indications:
- relief of an attack of angina pectoris, prevention of attacks of angina pectoris, including before physical / emotional stress: Isakardine is administered 1-3 times with an interval between injections of 30 seconds against the background of holding the breath; to stop an attack, increasing a single dose over 3 injections is allowed only as directed by a doctor;
- acute left ventricular failure, acute myocardial infarction (under medical supervision): it is necessary to carry out treatment against the background of monitoring blood pressure and heart rate; therapy should be started with 1-3 injections with 30-second breaks between them; after 5 minutes, in the absence of a positive effect, it is allowed to carry out another 1 injection, and if after 10 minutes there is no improvement, another 1 injection.
Before the first use of Isakardin spray or during a break in treatment for more than a day, press the sprayer 2-3 times until the first drops of the solution are released.
It is necessary to beware of getting the drug in the eyes.
Side effects
Adverse reactions that occurred during therapy with Isacardine (criteria for assessing the incidence: very often - ≥ 10%; often - from ≥ 1% to <10%; infrequently - from ≥ 0.1% to <1%; rarely - from ≥ 0, 01% to <0.1%; extremely rare - <0.01%; with an unknown frequency - according to reports, it is not possible to establish the frequency of occurrence of adverse reactions):
- cardiovascular system: often - orthostatic hypotension, tachycardia (for a spray - reflex); infrequently - paradoxical intensification of angina attacks, collapse (sometimes accompanied by bradyarrhythmia and fainting), transient hypoxemia as a result of a relative redistribution of blood flow to hypoventilated alveolar areas (in patients with coronary artery disease, it can cause myocardial hypoxia); with an unknown frequency - a pronounced decrease in blood pressure with a possible concomitant appearance of pallor, increased sweating, nausea, vomiting, anxiety;
- central nervous system: very often - headaches (nitrate headaches) at the beginning of the course, as a rule, passing with further use of the drug; often - drowsiness, light dizziness, in addition to the spray - blurred visual perception; with an unknown frequency (for a spray) - lethargy (mainly at the beginning of therapy), cerebral ischemia;
- skin and subcutaneous tissues: infrequently - skin flushing, allergic skin reactions (including skin rash); extremely rare - Stevens-Johnson syndrome, angioedema; with an unknown frequency - exfoliative dermatitis;
- digestive system: often (for spray) - burning of the tongue; infrequently - vomiting, nausea; extremely rare - heartburn; with an unknown frequency (for a spray) - dryness of the oral mucosa;
- others: often - asthenia; possible tolerance, including cross, to other nitrates (to prevent the development of this effect, you must avoid the course use of high doses of isosorbide dinitrate).
Overdose
Symptoms of an overdose of Isacardine may include the following reactions: a significant decrease in blood pressure (less than 90 mm Hg), increased sweating, pallor, threadlike pulse, postural dizziness, tachycardia, asthenia, throbbing headache, fainting, vomiting, nausea, diarrhea. When using the drug in large doses (more than 20 mg / kg), as a result of the formation of nitrite ions due to the metabolic transformation of isosorbide mononitrate, methemoglobinemia, dyspnea, and tachypnea may develop. Anxiety, loss of consciousness and cardiac arrest associated with an overdose of the drug can also be recorded. With the introduction of excessively large doses, an increase in ICP is possible, causing such cerebral symptoms as headache, drowsiness, and dizziness. In the case of chronic overdose, an increase in methemoglobin is observed.
With the development of the above symptoms, it is necessary to stop the administration of Isacardine and give the patient a horizontal position with raised legs. If there is a significant decrease in blood pressure and / or a state of shock, measures are prescribed to replenish the BCC (circulating blood volume). In order to improve blood circulation in exceptional cases, it is possible to carry out an infusion of norepinephrine (norepinephrine) and / or dopamine. The use of adrenaline (epinephrine) and related compounds is contraindicated!
In the event of methemoglobinemia, ascorbic acid is prescribed: orally at a dose of 1 g or in the form of sodium salt intravenously at a dose of 0.1–0.15 ml / kg of a 1% solution (no more than 50 ml). Oxygen therapy, artificial lung ventilation (ALV), hemodialysis are performed.
special instructions
During treatment, it is necessary to monitor blood pressure and heart rate, as well as indicators of other vital organs.
Therapy with Isacardine should not be carried out in patients who have previously received PDE-5 inhibitors (tadalafil, sildenafil, udenafil, vardenafil).
The solution concentrate for infusion is not reusable. The concentrate is sterile, it does not contain preservatives and must be applied immediately after opening the ampoule. The prepared solution for infusion must be administered within 24 hours after dilution.
Since the concentrate is a supersaturated solution, crystallization of the substance can occur when used undiluted. Although under normal conditions this reaction does not affect the activity of the agent, it is not recommended to use the concentrate in ampoules if crystallization is observed.
For intravenous infusion of the solution, blood transfusion systems made of polypropylene, polytetrafluoroethylene (PTFE) and polyethylene (PE) are used. Infusion materials made of polyurethane or polyvinyl chloride (PVC), due to the adsorption of the active substance, weaken the effect of Isacardine, because of this, an increase in the dose may be required. In the case where polyurethane and / or PVC materials are used, the level of isosorbide dinitrate should be monitored and, if necessary, the dose adjusted.
Patients on a sodium-restricted diet should remember that 1 ml of the concentrate contains 0.15 mmol (3.54 mg) sodium.
Avoid abrupt cessation of therapy with Isacardine in the form of a dosed sublingual spray, the dose of the drug should be reduced gradually. The use of high doses of the spray and its frequent use can lead to the development of tolerance. In this case, it is recommended to cancel the drug treatment for 24-48 hours, or after 3-6 weeks of regular use, take a break in admission for 3-5 days and take another antianginal agent during this period.
Patients with acute myocardial infarction with reduced ventricular filling pressure require particularly careful medical supervision.
Sublingual spray contains approximately 85% ethanol. During therapy, you should stop drinking ethanol-containing drinks.
Influence on the ability to drive vehicles and complex mechanisms
During the period of using Izakardin, special care must be taken when driving vehicles and controlling other complex moving mechanisms due to the possible development of drowsiness and dizziness during therapy with the drug.
Application during pregnancy and lactation
There is no information on the effect of Isacardine on human fertility. Adequate and well-controlled studies of the safety of isosorbide dinitrate treatment have not been conducted. In preclinical reproductive studies using animals with the introduction of the active substance in doses reaching the level of maternal toxicity, no signs of a negative effect of the drug on the fetus were found.
Due to the fact that in the process of animal studies it is not always possible to reproduce the effect of the drug on humans, for safety reasons, Isakardin can be used by pregnant women strictly according to the doctor's prescription and under his supervision, after a careful assessment of the expected benefits of treatment for the mother and the possible threat to the health of the fetus.
It is known that nitrates can be excreted in human milk, but the exact concentration of isosorbide dinitrate in breast milk has not been established. There is also data on the potential risk of methemoglobinemia in infants, therefore, if it is necessary to use Isacardine during lactation, it is necessary to stop breastfeeding.
In the case when a nursing woman needs to administer the spray as an emergency drug, for example, in order to stop an attack of angina pectoris, the child should be monitored for possible adverse reactions.
Pediatric use
For patients under 18 years of age, the use of Isacardine is contraindicated, since the effectiveness and safety of its use in patients of this age group have not been established.
With impaired renal function
In the presence of severe renal failure, drug treatment should be carried out with caution.
For violations of liver function
In the presence of severe hepatic impairment, therapy with Isacardine should be carried out with caution due to the aggravated risk of methemoglobinemia.
Use in the elderly
Elderly patients Izacardine in the form of a spray should be prescribed with caution. There are no data on the need to change the dose of the drug in the form of a concentrate in patients of this age category.
Drug interactions
- vasodilators - vasodilators; antihypertensive drugs - diuretics, β-blockers, angiotensin-converting enzyme inhibitors (ACE inhibitors), slow calcium channel blockers (BMCC); tricyclic antidepressants, antipsychotics - neuroleptics; quinidine, procainamide, ethanol and ethanol-containing drugs: increased antihypertensive effect;
- sapropterin: the threat of arterial hypotension is aggravated, since this substance is a coenzyme of nitric oxide synthetase and enhances the production of an additional amount of the latter;
- nifedipine, verapamil and other BMCC, propranolol, amiodarone: the antianginal effect is enhanced;
- heparin: its anticoagulant effect is weakened against the background of intravenous infusion of isosorbide dinitrate;
- dihydroergotamine: it is possible to increase its concentration and potentiate the hypotensive effect;
- α-blockers, sympathomimetics: the severity of antianginal action decreases (a significant decrease in blood pressure, causing a decrease in coronary perfusion);
- norepinephrine (norepinephrine): its therapeutic effect is weakened;
- barbiturates: metabolic transformation is accelerated, and the plasma level of nitro compounds in the blood decreases;
- atropine and other m-anticholinergics: the risk of increased IOP increases.
Analogs
Isakardin's analogs are Kardiket, Isoket, Dinisorb, Nitrosorbid, etc.
Terms and conditions of storage
Store in places inaccessible to children, away from fire (spray), at a temperature not exceeding 25 ° C - for concentrate, 30 ° C - for spray.
The shelf life of the concentrate is 3 years, the spray is 4 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Izacardin
Reviews of Isacardine on medical sites are mostly good. Most often, patients use the drug in the form of a metered-dose sublingual spray and characterize it as an effective remedy for the relief and prevention of angina attacks. To prevent an attack (including before physical activity), according to most reviews, one injection of Isakardine is sufficient, and sometimes two or three doses of spray are required to relieve chest pain.
Patients note that the drug is well tolerated, however, some reviews indicate the development of dizziness and drowsiness after its administration.
Price for Isacardine in pharmacies
The price for Isacardin can be:
- concentrate for preparation of solution for infusion (1 mg / ml): 650-800 rubles. per package containing 10 ampoules of 10 ml;
- dosed sublingual spray (1.25 mg / dose): 220–250 rubles. per bottle of 15 ml.
Izakardin: prices in online pharmacies
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Drug name Price Pharmacy |
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Izakardin 1.25 mg / dose sublingual spray dosed 15 ml 1 pc. 247 r Buy |
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Izakardin 1 mg / ml concentrate for preparation of solution for infusion 10 ml 10 pcs. 727 RUB Buy |
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Isakardin conc. for prig solution for inf. 1mg / ml 10ml 10 pcs. 742 RUB Buy |
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
