Cardiket tablets of prolonged action 20mg, No. 50

• Long-term treatment of coronary heart disease (prevention of angina attacks).

• Secondary prevention of myocardial infarction and treatment for persistent angina pectoris (as part of combination therapy).

• Long-term treatment of severe chronic heart failure (as part of combination therapy with cardiac glycosides, diuretics, angiotensin-converting enzyme (ACE) inhibitors).

Prolonged-release tablets cannot be divided!
The drug should be taken orally without chewing and drinking a small amount of liquid, regardless of the time of the meal. Unless otherwise prescribed:
KardiketЃ tablets of prolonged action 20 mg: 1 tablet 2 times a day. To maintain the therapeutic effect, take the second pill no later than 6-8 hours after the first. If the therapeutic effect is insufficient, the dose can be increased to 1 tablet 3 times a day, one tablet every 6 hours.
CardiketЃ tablets of prolonged action 40 mg: at the beginning of treatment - 1 tablet once a day. If the therapeutic effect is insufficient, the dose can be increased to 1 tablet 2 times a day. To maintain the therapeutic effect at a dosage twice a day, take the second pill no later than 6-8 hours after the first. CardiketЃ tablets of prolonged action 60 mg: at the beginning of treatment - 1 tablet once a day. If necessary, the dose can be increased to 1 tablet 2 times a day. To maintain the therapeutic effect at a dosage twice a day, take the second pill no later than 6-8 hours after the first.
Cardiket tablets of prolonged action 40 mg: at the beginning of treatment - 1 tablet once a day. If the therapeutic effect is insufficient, the dose can be increased to 1 tablet 2 times a day. To maintain the therapeutic effect at a dosage twice a day, take the second pill no later than 6-8 hours after the first.
CardiketЃ extended-release tablets 60 mg: at the beginning of treatment - 1 tablet once a day. If necessary, the dose can be increased to 1 tablet 2 times a day. To maintain the therapeutic effect at a dosage twice a day, take the second pill no later than 6-8 hours after the first.
Treatment should be started with the lowest dose and slowly increased to the most effective dose. The doctor decides on the duration of treatment. This medicinal product is intended for long-term use and should not be stopped abruptly without consulting a doctor.

1 prolonged-release tablet contains:
active substance: isosorbide dinitrate 20.00 mg;
auxiliary substances : lactose monohydrate 157.95 mg, talc 55.00 mg, magnesium stearate 2.05 mg, polyvinyl acetate 15.00 mg.

• Hypersensitivity to isosorbide dinitrate, other nitrates or excipients.

• Acute circulatory disorder (shock, collapse)

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

• Hypertrophic obstructive cardiomyopathy.

• Constructive pericarditis.

• Cardiac tamponade.

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

• Severe hypovolemia.

• Severe anemia.

• Severe aortic and subaortic stenosis, severe mitral stenosis.

• Concomitant use of phosphodiesterase-5 inhibitors (including sildenafil, vardenafin, tadalafil).

• Age up to 18 years (efficacy and safety have not been established).

• Due to the presence of lactose, patients with congenital galactose intolerance or malabsorption of glucose and galactose should not take this drug.

With caution,
low filling pressure of the left ventricle, including in acute myocardial infarction, impaired left ventricular function (for example, with left ventricular failure); mild to moderate aortic and / or mitral stenosis; diseases accompanied by increased intracranial pressure (until now, an increase in intracranial pressure was observed only after intravenous administration of nitroglycerin in high doses); cerebral hemorrhage, increased intraocular pressure, incl. angle-closure glaucoma, a tendency to orthostatic disorders of vascular regulation, severe renal and / or hepatic failure. hypothyroidism, malnutrition and malnutrition; pregnancy, lactation period.

Trade name of the drug:

CardiketЃ

International non-proprietary name:

isosorbide dinitrate

Dosage form:

extended-release tablets

Composition:

1 prolonged-release tablet contains:
active substance: isosorbide dinitrate 20.00 mg / 40.00 mg / 60.00 mg (use a mixture (trituration) of isosorbide dinitrate and lactose monohydrate 40/60).
excipients : lactose monohydrate 157.95 mg / 162.70 mg / 250.70 mg, talc 55.00 mg / 45.00 mg / 72.715 mg, magnesium stearate 2.05 mg / 2.08 mg / 2.515 mg, polyvinyl acetate 15.00 mg / 9.00 mg / 12.00 mg, potato starch - / 1.22 mg / 2.07 mg.

Description:

Round tablets of white color, odorless. On the one hand they are flat, with a chamfer and a notch and engraving above the line - 'IR', under the line - '20' (for 20 mg tablets), '40' (for 40 mg tablets), '60' (for 60 mg tablets) ; on the other hand - convex with engraving 'SCHWARZ PHARMA'.

Pharmacotherapeutic group:

vasodilating agent - nitrate.

ATX code:

C01DA08

Pharmacological properties

Pharmacodynamics
Isosorbide dinitrate is a peripheral vasodilator with a predominant effect on venous vessels. It has an antianginal effect, causes a hypotensive effect. The mechanism of action is associated with the release of nitric oxide (an endothelial relaxing factor) in the vascular endothelium, which causes the activation of intracellular guanylate cyclase, resulting in an increase in the level of cyclic guanosine monophosphate (cGMP) (a mediator of vasodilation). The latter stimulates cGMP-dependent protein kinase, which disrupts the phospholation of certain proteins of smooth muscle cells, including the myosin light chain, which ultimately reduces contractility and subsequently leads to relaxation of vascular smooth muscle.
Acts on peripheral arteries and veins. Relaxation of the veins leads to a decrease in venous return to the heart (preload), which decreases the filling pressure of the left ventricle. There also occurs (albeit to a lesser extent) the expansion of arterial vessels, which is accompanied by a decrease in blood pressure (BP), a decrease in the total peripheral vascular resistance (afterload).
A decrease in pre- and afterload leads to a decrease in oxygen consumption by the myocardium.
Promotes redistribution of coronary blood flow in favor of subendocardial zones, especially in atherosclerosis of coronary arteries (mainly large). Vasodilation of collateral arteries can improve myocardial blood supply. By reducing oxygen consumption by the myocardium and improving oxygen delivery to ischemic areas, they reduce the zone of myocardial damage.
Improves hemodynamics in patients with chronic heart failure, both at rest and during exercise.
Reduces blood flow to the right atrium, helps to reduce pressure in the pulmonary circulation and regression of symptoms in pulmonary edema.
Expands the vessels of the brain, dura mater, which may be accompanied by a headache.
It also relaxes the smooth muscles of the bronchi, gastrointestinal tract, bile and urinary tract.
As with other nitrates, cross-tolerance develops. After cancellation (a break in treatment), sensitivity to it quickly recovers. In order to prevent the onset of tolerance, it is recommended to observe a daily, preferably nightly, 'nitrate-free interval' for 8-12 hours. For most patients, this therapy is more effective than continuous treatment.

Pharmacokinetics
After oral administration of isosorbide, dinitrate is rapidly absorbed. The relative bioavailability for the sustained-release forms of isosorbide dinitrate compared to conventional tablets is more than 80% when taken orally. The action is started - after 15-30 minutes, the maximum concentration of the substance in the blood plasma is reached after 15 minutes - 1 - 2 hours. It is metabolized in the liver with the formation of active metabolites isosorbide-5-mononitrate (half-life (T?) Is 4-6 hours) and isosorbide-2-mononitrate (half-life (T?) - 1.5-2 hours). It is excreted by the kidneys (mainly in the form of metabolites).

Indications for use

• Long-term treatment of coronary heart disease (prevention of angina attacks).

• Secondary prevention of myocardial infarction and treatment for persistent angina pectoris (as part of combination therapy).

• Long-term treatment of severe chronic heart failure (as part of combination therapy with cardiac glycosides, diuretics, angiotensin-converting enzyme (ACE) inhibitors).

Contraindications

• Hypersensitivity to isosorbide dinitrate, other nitrates or excipients.

• Acute circulatory disorder (shock, collapse)

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

• Hypertrophic obstructive cardiomyopathy.

• Constructive pericarditis.

• Cardiac tamponade.

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

• Severe hypovolemia.

• Severe anemia.

• Severe aortic and subaortic stenosis, severe mitral stenosis.

• Concomitant use of phosphodiesterase-5 inhibitors (including sildenafil, vardenafin, tadalafil).

• Age up to 18 years (efficacy and safety have not been established).

• Due to the presence of lactose, patients with congenital galactose intolerance or malabsorption of glucose and galactose should not take this drug.

With caution,
low filling pressure of the left ventricle, including in acute myocardial infarction, impaired left ventricular function (for example, with left ventricular failure); mild to moderate aortic and / or mitral stenosis; diseases accompanied by increased intracranial pressure (until now, an increase in intracranial pressure was observed only after intravenous administration of nitroglycerin in high doses); cerebral hemorrhage, increased intraocular pressure, incl. angle-closure glaucoma, a tendency to orthostatic disorders of vascular regulation, severe renal and / or hepatic failure. hypothyroidism, malnutrition and malnutrition; pregnancy, lactation period.

Precautions for use

KardiketЃ in the dosage form of a prolonged-release tablet is not used to relieve angina attacks.
In acute myocardial infarction or acute heart failure, the drug should be used only under the condition of careful clinical observation of the patient. Interruptions in therapy with KardiketЃ for taking phosphodiesterase-5 inhibitors are not permissible, since the risk of angina attacks and withdrawal syndrome increases. In the event of an attack of angina pectoris, fast-acting nitrates should be additionally used to stop the attack.
During treatment, a decrease in blood pressure and the appearance of dizziness may occur with a sharp transition from a 'lying' or 'sitting' position to a 'standing' position, while drinking alcohol, during exercise and hot weather, and it is also possible to increase angina pectoris with a sharp decrease in blood pressure, the development ischemia up to myocardial infarction and sudden death (paradoxical 'nitrate reactions').
With prolonged use of the drug KardiketЃ, the development of tolerance is possible, and therefore, it is recommended to cancel for 24 - 48 hours or after 3-6 weeks of regular intake of the drug, take a break for 3-5 days, replacing the intake of the drug KardiketЃ with other antianginal drugs. ...

Method of administration and dosage

Prolonged-release tablets cannot be divided!
The drug should be taken orally without chewing and drinking a small amount of liquid, regardless of the time of the meal. Unless otherwise prescribed:
KardiketЃ tablets of prolonged action 20 mg: 1 tablet 2 times a day. To maintain the therapeutic effect, take the second pill no later than 6-8 hours after the first. If the therapeutic effect is insufficient, the dose can be increased to 1 tablet 3 times a day, one tablet every 6 hours.
CardiketЃ tablets of prolonged action 40 mg: at the beginning of treatment - 1 tablet once a day. If the therapeutic effect is insufficient, the dose can be increased to 1 tablet 2 times a day. To maintain the therapeutic effect at a dosage twice a day, take the second pill no later than 6-8 hours after the first. CardiketЃ tablets of prolonged action 60 mg: at the beginning of treatment - 1 tablet once a day. If necessary, the dose can be increased to 1 tablet 2 times a day. To maintain the therapeutic effect at a dosage twice a day, take the second pill no later than 6-8 hours after the first.
Cardiket tablets of prolonged action 40 mg: at the beginning of treatment - 1 tablet once a day. If the therapeutic effect is insufficient, the dose can be increased to 1 tablet 2 times a day. To maintain the therapeutic effect at a dosage twice a day, take the second pill no later than 6-8 hours after the first.
CardiketЃ extended-release tablets 60 mg: at the beginning of treatment - 1 tablet once a day. If necessary, the dose can be increased to 1 tablet 2 times a day. To maintain the therapeutic effect at a dosage twice a day, take the second pill no later than 6-8 hours after the first.
Treatment should be started with the lowest dose and slowly increased to the most effective dose. The doctor decides on the duration of treatment. This medicinal product is intended for long-term use and should not be stopped abruptly without consulting a doctor.

Overdose

Symptoms : severe decrease in blood pressure with orthostatic vasodilation, reflex tachycardia and headache. There may be pallor, increased sweating, 'threadlike' pulse, weakness, dizziness, incl. postural, skin flushing, nausea, vomiting, diarrhea. At high doses (more than 20 mg / kg of body weight), the appearance of methemoglobinemia, cyanosis, tachypnea, dyspnea due to the formation of nitrithions due to the metabolism of isosorbide mononitrate should be expected, anxiety, loss of consciousness and cardiac arrest are also possible. It is possible that these symptoms may be caused by an overdose of isosorbide dinitrate. At very high doses of the drug, intracranial pressure may increase with cerebral symptoms. In chronic overdose, an increase in methemoglobin is detected.
Treatment : if symptoms of an overdose appear, the drug should be discontinued, the stomach should be rinsed, and activated charcoal should be taken.
With a pronounced decrease in blood pressure and / or a state of shock - give the patient a horizontal position with raised legs and take measures to replenish the circulating blood volume (BCC); in exceptional cases, norepinephrine (norepinephrine) and / or dopamine infusions can be used to improve blood circulation. Administration of epinephrine (adrenaline) and related compounds is contraindicated.
With methemoglobinemia:
1. Ascorbic acid - 1 g inside or in the form of sodium salt intravenously - 0.1 - 0.15 ml / kg of 1% solution up to 50 ml.
2. Oxygen therapy, hemodialysis, exchange blood transfusion.

Side effect

Possible side effects are listed below by 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 1/10 000), the frequency is unknown.
From the side of the central nervous system
Very often: headache.
Often: drowsiness, light dizziness.
From the side of the cardiac system
Often: tachycardia.
Infrequently: 'paradoxical' intensification of angina attacks.
On the part of the vascular system :
Often: orthostatic hypotension.
Uncommon: collapse (sometimes accompanied by bradyarrhythmia and fainting).
Frequency unknown - hypotension.
From the gastrointestinal tract
Uncommon: nausea, vomiting.
Very rare: heartburn.
Violations of the skin and subcutaneous tissues
Uncommon, skin allergic reactions (including rash), 'flushes' of blood to the skin of the face.
Very rare: angioedema, Stevens-Johnson syndrome.
Frequency not known: exfoliative dermatitis.
General disorders and disorders at the injection site
Often: asthenia.
Others: development of tolerance (including cross-tolerance to other nitrates).
To prevent the development of tolerance, continuous high doses of the drug should be avoided.
For organic nitrates, cases of severe hypotension were noted, accompanied by nausea, vomiting, anxiety, pallor and increased sweating.
Long-term use of the drug can cause transient hypoxemia due to a relative redistribution of blood flow to hypoventilated alveolar areas (in patients with coronary heart disease, it can lead to myocardial hypoxia).

Interaction with other medicinal products

When combined with amiodarone, propranolol, blockers of 'slow' calcium channels (verapamil, nifedipine, etc.), an increase in the antianginal effect is possible.
Under the influence of beta-adrenostimulants, alpha-blockers, it is possible to reduce the severity of the antianginal effect (tachycardia and an excessive decrease in blood pressure). Barbiturates accelerate metabolism and reduce the concentration of isosorbide mononitrate in the blood. Reduces the effect of vasopressors.
M-anticholinergics, incl. atropine (and other drugs with m-anticholinergic effect) increases the likelihood of increased intraocular pressure when used with nitrates. Nitro compounds can reduce the therapeutic effect of norepinephrine (norepinephrine).
Barbiturates accelerate metabolism and reduce the concentration of nitro compounds in blood plasma.
The use of isosorbide dinitrate with antihypertensive drugs (for example, beta-blockers, diuretics, blockers of 'slow' calcium channels, angiotensin-converting enzyme inhibitors), antipsychotics, tricyclic antidepressants, ethanol and ethanol-containing drugs can lead to increased hypotensive action.
Simultaneous administration of the drug KardiketЃ and phosphodiesterase-5 inhibitors (including sildenafil, tadalafil, vardenafil) is contraindicated due to the possibility of increasing the hypotensive effect of the drug.
With simultaneous use with dihydroergotamine, it is possible to increase the concentration and enhance the effect of dihydroergotamine.
Adsorbents, astringents and coating agents reduce the absorption of the drug in the gastrointestinal tract.
It is recommended to be careful with the simultaneous use of sapropterin-containing drugs (sapropterin is a cofactor of nitric oxide synthase) with all vasodilating agents whose pharmacological action is associated with nitric oxide (NO), including classic NO donors (for example, nitroglycerin, isosorbide dinitrate, isosorbide mononitrate) and others.

Application during pregnancy and during breastfeeding

Clinical studies of the use of the drug KardiketЃ in pregnant women have not been conducted. Use during pregnancy is possible only if the intended benefit to the mother outweighs the possible risk to the fetus and / or child. At the same time, careful monitoring of the condition of the pregnant woman and the development of the fetus is carried out.
There is information about the penetration of nitrates into breast milk, but the exact content of isosorbide dinitrate and its metabolites in breast milk has not been determined. It has also been reported about the possible risk of developing methemoglobinemia in infants, so taking the drug during breastfeeding should be done with caution.
Application in children
There is still no experience of treating children with this drug.
Use in elderly patients
There is no information on the need for dosage adjustments in elderly patients.

Influence on the ability to drive vehicles and mechanisms

Isosorbide dinitrate can reduce the ability to drive vehicles and engage in other potentially hazardous activities that require increased concentration and psychomotor speed. Therefore, it is recommended to be careful when driving vehicles and engaging in other potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions.

Release form

Extended release tablets 20 mg, 40 mg, 60 mg. 10 tablets in a blister made of polypropylene foil, or transparent polypropylene foil and aluminum foil, or polyvinyl chloride film and aluminum foil. 2 or 5 blisters with instructions for use in a cardboard box.

Storage conditions

At a temperature not higher than 25 ? C.
Keep out of the reach of children.

Shelf life

Shelf life is 5 years.
Do not use the drug after the expiration date.

Vacation conditions

On prescription.