Composition, form of production and packaging
Tablets of prolonged action of white color, round, on the one hand flat, with a facet and a risk, with engraving "IR" over risk and "20" - under risk; on the other hand convex, with engraving "SCHWARZ PHARMA".
1 tab.
isosorbide dinitrate 20 mg
Excipients: lactose monohydrate, magnesium stearate, polyvinyl acetate, talc.
10 pieces. - packings cellular planimetric (2) - packs cardboard.
10 pieces. - packings cellular planimetric (5) - packs cardboard.
Tablets of prolonged action of white color, round, on the one hand flat, with a facet and a risk, with engraving "IR" above risk and "40" - under risk; on the other hand convex, with engraving "SCHWARZ PHARMA".
1 tab.
isosorbide dinitrate 40 mg
Excipients: lactose monohydrate, talc, magnesium stearate, polyvinyl acetate, potato starch.
10 pieces. - packings cellular planimetric (2) - packs cardboard.
10 pieces. - packings cellular planimetric (5) - packs cardboard.
Tablets of prolonged action of white color, round, on the one hand flat, with a facet and a risk, with engraving "IR" above the risk and "60" - under the risk; on the other hand convex, with engraving "SCHWARZ PHARMA".
1 tab.
isosorbide dinitrate 60 mg
Excipients: lactose monohydrate, talc, magnesium stearate, polyvinyl acetate, potato starch.
10 pieces. - packings cellular planimetric (2) - packs cardboard.
10 pieces. - packings cellular planimetric (5) - packs cardboard.
Capsules of prolonged action hard gelatinous, size 1, light brown in color; the contents of the capsules are white to white granules with a yellow shade of color, odorless or almost odorless.
1 caps.
isosorbide dinitrate 120 mg
Excipients: lactose, sugar balls, poly (O-ethyl) cellulose, talc, shellac.
10 pieces. - packings cellular planimetric (2) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.
The product description was approved by the manufacturer for the 2009 print edition.
PHARMACHOLOGIC EFFECT
Antianginal drug, organic nitrate.
Isosorbide dinitrate causes relaxation of the smooth muscle wall of the vessels, thus inducing vasodilation. Isosorbide dinitrate acts as a peripheral vasodilator, affecting both arteries and veins. These effects contribute to the deposition of venous blood and a decrease in venous return to the heart, reducing the end-diastolic pressure and volume of the left ventricle (reduce preload).
The drug is characterized by a combination of rapid onset of effect with duration of action.
Advantages of the drug are determined by the fact that the active substance contained in tablets and capsules of prolonged action, quickly enters the bloodstream. As a result, the drug provides a rapid onset of the effect in the treatment of angina and permanently retains its protective effect.
The beginning of the drug is observed after 15-30 minutes.
PHARMACOKINETICS
Capsules after ingestion dissolve in the stomach for several minutes. The contents of the active substance granules are released gradually over several hours.
Suction and distribution
After ingestion of isosorbide, dinitrate is rapidly absorbed. Bioavailability - 22% (effect of "first passage" through the liver). C max is reached 15 minutes -1-2 hours.
Binding to blood plasma proteins - 30%.
Metabolism and excretion
T 1/2 is 12 hours.
Metabolised in the liver with the formation of active metabolites - isosorbide-5-mononitrate (T 1/2 is 4-6 h) and isosorbide-2-mononitrate (T 1/2 - 1.5-2 h). It is excreted in urine (almost completely in the form of metabolites).
INDICATIONS
- Prolonged treatment of IHD: prevention of angina attacks;
- Chronic heart failure (as part of a combination therapy with cardiac glycosides, ACE inhibitors and / or diuretics);
- secondary prevention of myocardial infarction and treatment with persistent angina pectoris (as part of combination therapy) for prolonged-release tablets.
DOSING MODE
Tablets of prolonged action of 20 mg appoint 1 tab. 2 times / day. With increasing requirements for the drug, the dose can be increased to 1 tablet. 3 times / day.
Tablets of prolonged action of 40 mg at the beginning of treatment appoint 1 tab. 1 time / day or 1/2 tablet. 2 times / day. If the therapeutic effect is insufficient, the dose can be increased to 1 tab. 2 times / day. The second tablet should be taken no later than 8 hours after the first.
Tablets of prolonged action of 60 mg at the beginning of treatment appoint 1 tab. 1 time / day. If necessary, the dose can be increased to 1 tab. 2 times / day. The second tablet should be taken no later than 8 hours after the first.
The drug in the form of prolonged-action capsules is prescribed for 120 mg 1 time / day.
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. The drug is intended for long-term use, and without consulting a physician, it should not be abruptly discontinued.
The drug is taken inside regardless of food intake, without chewing and squeezed with a small amount of liquid. In order to divide the tablet in half, it should be placed on a hard surface with a line of fracture upwards and press with your thumb on the tablet. It can easily be divided into two halves.
SIDE EFFECT
From the side of the cardiovascular system: at the beginning of the treatment, headache ("nitrate" headache), which, as a rule, disappears in a few days with the further application of the drug may develop. Sometimes, with the first application or with an increase in the dose of the drug, there is a marked decrease in blood pressure, especially when the patient rises from the bed, which can be accompanied by tachycardia (paradoxical bradycardia is possible), retardation, and dizziness and a sense of weakness. In rare cases with a marked decrease in blood pressure, there may be an increase in the symptoms of angina pectoris (a paradoxical increase in angina attacks). Very rarely observed are collapoid states, sometimes with bradycardia and sudden loss of consciousness (syncope).
From the digestive system: rarely - nausea, vomiting, dry mouth, belching, abdominal pain.
From the side of the central nervous system: stiffness, drowsiness, blurred vision, decreased ability to rapid mental and motor reactions (especially at the beginning of treatment); rarely - ischemia of the brain.
Allergic reactions: skin rash.
Other: development of tolerance (including cross-over to other nitrates), exfoliative dermatitis, skin hyperemia.
CONTRAINDICATIONS
- Acute myocardial infarction with severe arterial hypotension;
- acute vascular insufficiency (shock, vascular collapse);
- severe arterial hypotension (systolic pressure less than 90 mm Hg);
- closed angle glaucoma with high intraocular pressure;
- craniocerebral trauma;
severe aortic and / or mitral stenosis;
- hypovolemia;
- hemorrhagic stroke;
- children and adolescents under 18 years of age (efficacy and safety of use not established);
- simultaneous administration of phosphodiesterase type 5 inhibitors (such as sildenafil, vardenafil or tadalafil), as they potentiate the hypotensive effect of nitrates;
- hypersensitivity to nitrates.
Relative contraindications
- cardiac tamponade;
- hypertrophic obstructive cardiomyopathy (possibly an increase in angina attacks);
- severe anemia;
- constrictive pericarditis;
- Hemorrhage in the brain;
- toxic pulmonary edema.
With caution and with careful medical supervision, the drug should be prescribed with a tendency to disturbances in blood circulation regulation due to low blood pressure (orthostatic disorders of blood circulation regulation), diseases accompanied by increased intracranial pressure, severe hepatic insufficiency (risk of methaemoglobinaemia), severe renal failure, hyperthyroidism , increased peristalsis of the gastrointestinal tract, malabsorption syndrome, elderly patients.
PREGNANCY AND LACTATION
During pregnancy and lactation, cardiac use is possible only if the intended benefit to the mother exceeds the possible risk to the fetus and / or the child.
APPLICATION FOR FUNCTIONS OF THE LIVER
With caution appoint a drug with severe renal failure.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
With caution appoint the drug with severe hepatic insufficiency (risk of development of methaemoglobinaemia).
SPECIAL INSTRUCTIONS
Cardiac is not used to stop angina attacks.
In the period of treatment, control of blood pressure and heart rate is necessary.
With constant continuous treatment with Cardicet in high doses, the development of tolerance is possible, as well as the appearance of cross tolerance to other drugs of the nitrate group. To prevent a decrease in the effectiveness of the drug, you should avoid its constant use in high doses.
When Cardistet is taken in patients with primary lung diseases, temporary hypoxemia may occur due to the relative redistribution of blood flow to the hypoventilation alveolar zones. In patients with IHD, this can lead to transient myocardial ischemia.
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.
To prevent the increase in angina attacks, sharp abolition should be avoided.
Against the background of cardiac treatment in the event of an attack of angina pectoris for its arresting it is necessary to additionally apply high-speed nitrates.
To prevent undesirable BP reduction, you should individually select the dose of the drug.
Against the background of treatment, it is possible to reduce blood pressure and the appearance of dizziness during a sharp transition to a vertical position from the "lying" or "sitting" position, with the use of ethanol, physical exercises and hot weather, as well as increased angina with a sharp decrease in blood pressure, ischemia right up to myocardial infarction and sudden death (paradoxical "nitrate reactions").
The severity of the headache on the background of cardiac therapy can be reduced by reducing its dose and / or concurrent intake of menthol-containing drugs (validol).
With frequent use without intervals free from use, habituation that requires a dose increase may develop.
In order to prevent the occurrence of tolerance, it is recommended to observe a daily, preferably nocturnal, "no-nite interval" for 8-12 hours. In most patients, such therapy is more effective than continuous treatment.
If on the background of taking the drug blurred vision or dry mouth is retained or expressed strongly, treatment should be discontinued.
During the treatment with the drug should be excluded from drinking alcohol.
Impact on the ability to drive vehicles and manage mechanisms
During cardiac therapy, it is necessary to refrain from driving motor vehicles and practicing potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.
OVERDOSE
Symptoms: marked decrease in blood pressure, collapse, fainting, headache, dizziness, palpitations, visual disturbances, skin hyperemia, nausea, vomiting, diarrhea, methemoglobinemia (cyanosis, anoxia), hyperpnoea, dyspnoea, bradycardia, perspiration, craniocerebral hypertension, paralysis, coma.
Treatment: gastric lavage; at methemoglobinemia - in / in 1% solution of methylene blue 1-2 mg / kg of body weight. Symptomatic therapy (epinephrine and related compounds are ineffective).
DRUG INTERACTION
It is possible to intensify the hypotensive effect of CardiKet with simultaneous reception with other vasodilators (vasodilators), antihypertensive drugs, beta-blockers, slow calcium channel blockers, phosphodiesterase 5 inhibitors used to treat erectile dysfunction, neuroleptics and tricyclic antidepressants, novocainamide, quinidine, and ethanol.
The simultaneous use of Cardiqet with dihydroergotamine may lead to an increase in the concentration of dihydroergotamine in the blood and, thus, enhance its hypotensive effect.
With the simultaneous use of sympathomimetic agents, alpha-blockers, it is possible to reduce the antianginal effect of the Cardicet drug.
The combination of amiodarone and other medications such as propranolol, slow calcium channel blockers (verapamil, nifedipine) and Cardiqet is rational for the treatment of IHD.
The combined use of acetylsalicylic acid and Cardicet improves coronary circulation.
With the combined use of Cardiket with m-holinoblokatorami (atropine) the probability of increasing intraocular pressure increases.
Adsorbents, astringents and enveloping agents reduce the absorption of Cardiac in the digestive tract.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
List B. The drug should be stored out of reach of children at a temperature of no higher than 25 В° C. Shelf life - 5 years.
