Cardicet® (Cardiket® )

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceIsosorbide dinitrateIsosorbide dinitrate
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    • Dosage form: & nbspsustained-release tablets
    Composition:
    1 tablet of prolonged action contains:
    Active substance: isosorbide dinitrate 20.00 mg / 40.00 mg / 60.00 mg (use 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 are white in color, odorless. On the one hand, flat, with a facet and risk and engraving over the risk - "IR", at risk - "20" (for tablets 20 mg), "40" (for tablets 40 mg), "60" (for tablets 60 mg) ; on the other hand - convex with engraving "SCHWARZ PHARMA".
    Pharmacotherapeutic group:vasodilator - nitrate
    ATX: & nbsp

    C.05.A.E.02   Isosorbide dinitrate

    C.01.D.A.08   Isosorbide dinitrate

    Pharmacodynamics:
    Isosorbide dinitrate is a peripheral vasodilator with a predominant effect on 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, which results in an increase in the level of cyclic guanosine monophosphate (cGMP) (mediator of vasodilation). The latter stimulates cGMP-dependent protein kinase, which disrupts the phospholysis of some smooth muscle cell proteins, including the light chain of myosin, which ultimately reduces contractility and subsequently leads to relaxation of smooth muscle vessels.
    It 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 an increase (albeit to a lesser extent) of arterial vessels, which is accompanied by a decrease in blood pressure (BP), a decrease in the total peripheral resistance of the vessels (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. Reducing oxygen consumption by myocardium and improving oxygen delivery to ischemic areas, reduce the area of ​​myocardial damage.
    Improves hemodynamics in patients with chronic heart failure, both at rest and during physical exertion.
    Reduces the flow of blood to the right atrium, helps reduce pressure in a small circle of circulation and regression of symptoms with pulmonary edema.
    It dilates the vessels of the brain, the dura mater, which can be accompanied by a headache.
    It also relaxes the smooth muscles of the bronchi, gastrointestinal tract, bile and urinary tract.
    Like other nitrates, cross tolerance is developing. After cancellation (interruption in treatment) sensitivity to it is quickly restored. In order to prevent the occurrence of tolerance, it is recommended to observe a daily, preferably nocturnal, "no-nit interval" for 8-12 hours.In most patients, such therapy is more effective than continuous treatment.
    Pharmacokinetics:When taken orally isosorbide dinitrate quickly absorbed. The relative bioavailability for forms of prolonged action of isosorbide dinitrate in comparison with conventional tablets is more than 80% when taken orally. The onset of action - after 15-30 minutes, the maximum concentration of the substance in the blood plasma is reached after 15 minutes - 1 - 2 hours. Metabolised in the liver with the formation of active metabolites of isosorbide-5-mononitrate (half-life (T 1/2) is 4-6 hours) and isosorbide-2-mononitrate (half-life (T1 / 2) - 1,5-2 hours). It is excreted by the kidneys (mainly in the form of metabolites).
    Indications:
    - Long-term treatment of coronary heart disease (prevention of angina attacks).
    - Secondary prevention of myocardial infarction and treatment with persistent angina pectoris (as part of combination therapy).
    - Long-term treatment of severe chronic heart failure (as part of a combination therapy with cardiac glycosides, diuretics, angiotensin-converting enzyme (ACE) inhibitors).

    Contraindications:
    - Hypersensitivity to isosorbide dinitrate, other nitrates or auxiliaries.
    - 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, severe mitral stenosis.
    - Simultaneous administration of inhibitors of phosphodiesterase-5 (including sildenafil, vardenafin, tadalafil).
    - Age to 18 years (effectiveness and safety not established).
    - Because of the presence of lactose, patients with congenital intolerance to galactose or impaired absorption, glucose and galactose should not take this drug.

    Carefully:low filling pressure of the left ventricle, including acute myocardial infarction, left ventricular dysfunction (eg, left ventricular failure); aortic and / or mitral stenosis of mild to moderate; diseases,accompanied by increased intracranial pressure (until now, increased intracranial pressure was observed only after intravenous injection of nitroglycerin in high doses); cerebral hemorrhage, increased intraocular pressure, incl. closed angle glaucoma, a tendency to orthostatic disorders of vascular regulation, severe renal and / or hepatic insufficiency, hypothyroidism, inadequate and inadequate nutrition; pregnancy, lactation.
    Pregnancy and lactation:Clinical studies of the use of Cardicet® in pregnant women have not been conducted. Use during pregnancy is only possible if the intended benefit to the mother exceeds the possible risk to the fetus and / or the child. In this case, careful monitoring of the condition of the pregnant woman and fetal development 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. Also, a possible risk of developing methaemoglobinemia in infants has been reported, so taking the drug during breastfeeding should be done with caution.

    Use in children
    Until now, there is no experience of treating children with this drug.

    Application in elderly patients
    Information on the need for dosage adjustment in elderly patients is lacking.
    Dosing and Administration:
    Tablets of prolonged action can not be divided!
    The drug should be taken orally, without chewing and washing down with a small amount of liquid, regardless of the time of ingestion.
    Unless otherwise specified:
    Kardiket® tablets prolonged action 20 mg: 1 tablet 2 times a day. To maintain therapeutic effect the second tablet should be taken 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.

    Cardiac tablets prolonged action 40 mg: at the beginning of treatment - 1 tablet 1 time per day. If the therapeutic effect is insufficient, the dose can be increased to 1 tablet 2 times a day. To maintain therapeutic effect at a dosage twice a day, the second tablet should be taken no later than 6-8 hours after the first.

    Kardiket® tablets prolonged action 60 mg: at the beginning of treatment - 1 tablet 1 time per day. If necessary, the dose can be increased to 1 tablet 2 times a day.To maintain therapeutic effect at a dosage twice a day, the second tablet should be taken no later than 6-8 hours after the first. Treatment should be started with the lowest doses and slowly increase the dose to the maximum effective dose. The decision on the duration of treatment is made by the doctor. This drug is intended for long-term use, and without consulting a physician, it should not be abruptly discontinued.

    Side effects:
    Possible side effects are given below for the body systems and the incidence rate: 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), the frequency is unknown.
    From the central nervous system Very often: headache. Often: drowsiness, slight dizziness.
    From the side of the cardiac system Often: tachycardia.
    Infrequently: the "paradoxical" intensification of angina attacks.
    From the side of the vascular system: Often: orthostatic hypotension.
    Infrequently: collapse (sometimes accompanied by bradyarrhythmia and syncope).
    Frequency unknown: hypotension.
    From the gastrointestinal tract
    Infrequent: nausea, vomiting.
    Very rarely: heartburn.
    Disturbances from the skin and subcutaneous tissues
    Infrequent: skin allergic reactions (including rash), "hot flashes" of blood to the skin of the face.
    Very rarely: angioedema, Stevens-Johnson syndrome. The frequency is unknown: exfoliative dermatitis.
    General violations and violations at the site of introduction Often: asthenia.
    Other: development of tolerance (including cross-over to other nitrates). To prevent the development of tolerance, continuous intake of high doses of the drug should be avoided.
    For organic nitrates, there have been cases of development of severe hypotension accompanied by nausea, vomiting, anxiety, pallor and increased sweating.
    Prolonged use of the drug may cause transient hypoxemia due to the relative redistribution of blood flow to hypoventilation alveolar sites (in patients with coronary heart disease - may lead to myocardial hypoxia).
    Overdose:
    Symptoms: marked reduction in arterial pressure with orthostatic vasodilation, reflex tachycardia and headache.There may appear pallor, increased sweating, "threadlike" pulse, weakness, dizziness, incl. postural, skin hyperemia, nausea, vomiting, diarrhea. In high doses (more than 20 mg / kg body weight), the appearance of methemoglobinemia, cyanosis, tachypnea, dyspnoea due to the formation of nitrite ions due to the metabolism of isosorbide mononitrate, it is also possible the appearance of anxiety, loss of consciousness and cardiac arrest. It is not excluded that these symptoms can 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 you have symptoms of an overdose, you must stop taking the medication, rinse your stomach, take Activated carbon.
    If there is a pronounced decrease in blood pressure and / or a shock condition, give the patient a horizontal position with raised legs and take measures to replenish the volume of circulating blood (BCC); In exceptional cases, norepinephrine (noradrenaline) and / or dopamine may be used to improve blood circulation.The introduction 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 1% solution up to 50 ml.
    2. Oxygenotherapy, hemodialysis, exchange blood transfusion.
    Interaction:
    When combined with amiodarone, propranolol, blockers of "slow" calcium channels (verapamil, nifedipine, etc.), it is possible to increase the antianginal effect. Under the influence of beta adrenostimulants, alpha-adrenoblbkatorov possible decrease in the expression of antianginal effect (tachycardia and excessive decrease in blood pressure). Barbiturates accelerate metabolism and reduce the concentration of isosorbide mononitrate in the blood. Reduces the effect of vasopressors.

    M-holinoblokatory, incl. atropine (and other drugs with m-holinoblokiruyuschim effect) increases the likelihood of increased intraocular pressure when used with nitrates. Nitro compounds can reduce the therapeutic effect of norepinephrine (noradrenaline).

    Barbiturates accelerate metabolism and reduce the concentration reduce the concentration of nitrocompounds in the blood plasma. The use of isosorbide dinitrate with antihypertensive agents (for example, beta-adrenoblockers, diuretics, blockers of "slow"
    calcium channel blockers, angiotensin converting enzyme inhibitors), neuroleptics, tricyclic antidepressants, ethanol and ethanol containing agents can lead to an increase in the hypotensive effect of isosorbide dinitrate. Simultaneous reception Kardiket® drug and phosphodiesterase-5 inhibitors (including sildenafil, tadalafil, vardenafil) is contraindicated
    in view of the possibility of intensifying the hypotensive effect of the drug. With simultaneous application with dihydroergotamine, an increase in the concentration and increase in the action of dihydroergotamine is possible. Adsorbents, astringents and enveloping agents reduce the absorption of the drug in the gastrointestinal tract.
    It is advisable to use caution while using sapropterine-containing medicines (sapropterine - cofactor of nitric oxide synthase) with all vasodilating agents, the realization of pharmacological action of which is associated with nitric oxide (N0), including classical NO donators (for example, nitroglycerine, isosorbide dinitrate, isosorbide mononitrate) and others.
    Special instructions:
    Precautions for use
    Kardiket® in the form of a sustained-release tablet does not apply to the relief of angina attacks.
    In case of acute myocardial infarction or acute heart failure, the drug should be used only under condition of careful clinical observation of the patient. Breaks in therapy with Cardicet® for the intake of phosphodiesterase-5 inhibitors are not allowed, as the risk of developing angina attacks and withdrawal can increase. In the event of an attack of angina for arresting an attack, rapid-acting nitrates should be additionally applied.
    Against the background of treatment, it is possible to reduce blood pressure and the appearance of dizziness during a sharp transition from the "lying" or "sitting" position to the standing position, with alcohol, exercise and hot weather, and possibly increased angina with a sharp decrease in blood pressure, development ischemia up to myocardial infarction and sudden death (paradoxical "nitrate reactions").
    With prolonged use of Cardidetic®, it is possible to develop tolerance, therefore it is recommended to cancel for 24 to 48 hours or after 3-6 weeks of regular medication taking a break for 3-5 days,replacing at this time the drug Cardicet® with other antianginal drugs.

    Effect on the ability to drive transp. cf. and fur:Isosorbide dinitrate can reduce the ability to drive vehicles and engage in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions. Therefore, it is recommended to use caution when driving vehicles and engaging in other potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.
    Form release / dosage:Long-acting tablets 20 mg, 40 mg, 60 mg.
    Packaging:10 tablets in a blister of polypropylene foil, or transparent polypropylene foil and aluminum foil, or a polyvinyl chloride film and aluminum foil. For 2 or 5 blisters together with instructions for use in a cardboard bundle.
    Storage conditions:At a temperature of no higher than 25 ° C.
    Keep out of the reach of children.
    Shelf life:
    5 years.
    Do not use the drug after the expiration date.
    Terms of leave from pharmacies:On prescription
    Registration number:П N013273 / 01
    Date of registration:19.09.2011
    The owner of the registration certificate:YUSB Pharma GmbHYUSB Pharma GmbH Germany
    Manufacturer: & nbsp
    Representation: & nbspYUSB FARMA LLC YUSB FARMA LLC Russia
    Information update date: & nbsp30.05.2013
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