Dicor Long 60 mg tablets # 50

Author Ольга Кияница

2017-05-11

Amount in a package -
Product form Pills
Manufacturer Microhim Ltd. (Ukraine, Rubezhnoye)
Registration certificate UA/11012/01/03
The main medicament -
morion code 141583

Dicor Long (DICOR long) user manual

Composition

active ingredient: i sosorbide dinitrate; 1 tablet contains 20 mg or 40 mg, or 60 mg isosorbide dinitrate;
auxiliary substances: lactose monohydrate, starch corn cellulose microcrystalline polyacrylate dispersion; methacrylate copolymer dispersion; crospovidone; povidone, hypromellose; hydroxypropyl cellulose; silicon dioxide colloidal magnesium stearate titanium dioxide (E 171) talc sodium lauryl sulfate.

Dosage form

Long-acting tablets.

Basic physical and chemical properties:

white tablets with a biconvex smooth surface, covered with a film membrane, through which the contours of the granules can be seen.

Pharmacological group

Vasodilators used in cardiology. ATC code C01D A08.

Pharmacological properties

Pharmacodynamics.

Like all organic nitrates, isosorbide dinitrate (ISDN) acts as a donor of nitric oxide (NO). NO leads to relaxation of smooth muscle vessels by stimulating guanylate cyclase and further increasing the concentration of intracellular cyclic guanylate monophosphate (cGMP). Thus, the (cGMP) -dependent protein kinase is stimulated, and as a result, the phosphorylation of various proteins in the smooth muscle cell changes. In turn, this leads to dephosphorylation of light chains of myosin and a decrease in contractility.

ISDN causes relaxation of the smooth muscles of the vessels, which leads to vasodilation. The expansion of veins promotes the venous "deposition" of blood and reduces the venous return to the heart; thus reducing ventricular end-diastolic pressure and volume (preload).

Action on the arteries, and at higher doses - on the arterioles leads to a decrease in systemic vascular resistance (afterload). This, in turn, improves the function of the heart.

The effect on preload as well as afterload causes a decrease in heart oxygen consumption.

In addition, ISDN causes a redistribution of blood flow to the subendocardial heart in an atherosclerotic lesion. The latter effect may be due to the selective dilatation of large coronary vessels. Dilation of collateral arteries, caused by nitrates, can improve myocardial perfusion with vessel stenosis. In addition, nitrates counteract the appearance and eliminate coronary spasms.

In patients with congestive heart failure, nitrates improve hemodynamics at rest and with exercise.

Pharmacokinetics.

In the digestive tract, ISDN is released from the sustained-release tablet slowly, for several hours. Absorption of the active substance is high. Bioavailability - 22% (effect of the first passage through the liver). Therapeutic concentration is achieved after 30 minutes, the maximum concentration (C max) is 1:00. Binding to blood plasma proteins - 30%. The elimination half-life is 12:00. ISDN is metabolized in the liver to form isosorbide-2-mononitrate (T 1/2 - 1.5-2 hours) and isosorbide-5-mononitrate (T 1/2 - 4-6 hours). Both metabolites are pharmacologically active. It is excreted by the kidneys (mainly in the form of metabolites).

Indications

Treatment and prevention of angina pectoris (including after myocardial infarction);
treatment of severe chronic heart failure in combination with glycosides, diuretics, ACE inhibitors.

Contraindications

The drug is contraindicated in:

  • hypersensitivity to isosorbide dinitrate, other nitrate compounds or other components of the drug
  • acute vascular insufficiency (shock, vascular collapse)
  • cardiogenic shock, with the impossibility of correcting the final diastolic pressure of the left ventricle with the help of appropriate measures;
  • severe hypotension (systolic blood pressure (BP) below 90 mm Hg)
  • hypertrophic obstructive cardiomyopathy;
  • constrictive pericarditis;
  • cardiac tamponade;
  • severe anemia
  • increased intracranial pressure (including those with craniocerebral trauma, hemorrhagic stroke), since venodilatation can lead to its further increase;
  • bleeding, severe hypovolemia (isosorbide dinitrate, reducing venous return, may provoke syncope)
  • aortic stenosis, mitral stenosis;
  • angle-closure glaucoma;
  • severe violations of the liver and / or kidney function, hyperthyroidism
  • hypothermia;
  • acute myocardial infarction with low filling pressure.

During therapy with nitrates, phosphodiesterase inhibitors (eg sildenafil, see "Interaction with other drugs and other interactions") should not be used.

Interaction with other drugs and other interactions

The hypotensive effect of the drug may be enhanced with simultaneous use with other vasodilators such as beta-blockers, calcium channel blockers, vasodilators with ethanol, neuroleptics and tricyclic antidepressants.

Inhibitors of phosphodiesterase (sildenafil, tadalafil, vardenafil) - the simultaneous use of isosorbide dinitrate with these drugs is contraindicated, since the use of isosorbide dinitrate contraindicated treatment of erectile dysfunction with these drugs, as there is a potential danger of uncontrolled arterial hypotension, life-threatening cardiovascular complications. If necessary, phosphodiesterase inhibitors should be taken no earlier than 72 hours after taking nitrates.

ACE inhibitors, phenothiazines, other nitrates / nitrites, quinidine, novocainamide, MAO inhibitors, narcotic analgesics-potentiating the hypotensive effect of isosorbide dinitrate, possibly the development of orthostatic collapse.

Dysopyramide - may reduce the effectiveness of isosorbide dinitrate.

Dihydroergotamine - the concentration of dihydroergotamine in the blood can increase, which leads to an increase in its hypertensive effect.

Norepinephrine, acetylcholine, histamine - the weakening of their effects when used with nitrates, since isosorbide dinitrate can be their physiological antagonist.

Heparin - it is possible to reduce its anticoagulant effect.

Alcohol - heavy disulfide-alcoholic reactions are possible, incl. severe hypotension, collapse.

With the simultaneous use of sympathomimetics (epinephrine, ephedrine, norepinephrine, naphthyzine, mezaton, and isadrine), the antianginal effect of isosorbide dinitrate may be reduced.

Application features

The drug can be used with caution and with careful observation of the doctor:

  • if left ventricular function is disrupted (left ventricular failure), systolic blood pressure lower than 90 mm Hg should be avoided. at .;
  • with orthostatic hypotension;
  • in case of anemia
  • at surgical interventions;
  • when using the drug, tolerance to other drugs that contain nitrates may develop;
  • with hypoxemia, which can be caused by the redistribution of blood flow in the hyperventilation zone in lung diseases.

The drug should not be used to eliminate acute attacks of angina pectoris.

The drug should be administered with caution to patients with a tendency to orthostatic reactions, hypothyroidism, malnutrition, as well as elderly patients, given the age-related changes in liver, kidney and heart function, concomitant diseases and other medications.

The intake of isosorbide dinitrate can affect the results of calorimetric determination of cholesterol.

Avoid alcohol during treatment with the drug.

Patients should be warned that the antianginal effect of isosorbide dinitrate is closely related to its dosage regimen, so the proposed dosage schedule should be carefully observed.

During treatment, especially with a gradual increase in the dose, it is necessary to control blood pressure and heart rate.

The development of tolerance (decreased effectiveness), as well as cross-tolerance to other drugs of the nitrate type (decrease in effect, if the patient before taking another nitrate) is described. To prevent a decrease or loss of the effect, prolonged intake of large doses (120 mg per day) should be avoided.

Patients on maintenance therapy should be informed that they should not take drugs containing phosphodiesterase inhibitors (eg sildenafil, tadalafil, vardenafil), because of the risk of developing uncontrolled arterial hypotension.

Due to the fact that the preparation contains lactose, it can not be administered to patients with rare genetic diseases such as galactose intolerance, hereditary lactase-deficiency Lappa, glucose-galactose malabsorption.

Due to the fact that the preparation contains sucrose, the drug should not be administered to patients with rare genetic diseases like fructose intolerance, impaired absorption of glucose and galactose (glucose-galactose malabsorption), sucrose isomaltase deficiency.

Use during pregnancy or lactation

Data on the safety of isosorbide dinitrate during pregnancy is not enough. In the first trimester of pregnancy, the use of the drug is contraindicated. In the II-III trimesters of pregnancy, the drug can be used only taking into account the ratio "expected benefit for the mother / risk to the fetus."

If necessary, breast-feeding should be discontinued.

The ability to influence the reaction rate when driving vehicles or other mechanisms

The drug can affect the reaction rate when driving vehicles or working with mechanisms.

Dosing and Administration

In the absence of other recommendations, the drug should be used regardless of food intake, without chewing, squeezed with enough water.

Dicor long 20 mg 1 tablet 2 times a day. The second / next dose should be taken no earlier than 6-8 hours after taking the first dose. With increased demand for nitrates, the daily dose can be increased to 1 tablet 3 times a day, with an interval of 6:00.

Dicor long 40 mg 1 tablet once a day. With increased demand for nitro drugs, the daily dose can be increased to 1 tablet 2 times a day. The second / next dose should be taken no earlier than 6-8 hours after the first dose.

Dicor long 60 mg 1 tablet once a day. With increased demand for nitrates, the daily dose can be increased to 1 tablet 2 times a day. The second / next dose should be taken no earlier than 6-8 hours after taking the first dose.

Treatment should begin with small doses, gradually increasing the dose to the required. The maximum daily dose is 120 mg. The duration of treatment is determined individually. The drug is intended for long-term use, which can not be abruptly discontinued.

There is no evidence that it is necessary to change the dosage for elderly patients.

Children

Do not use it for children.

Overdose

Symptoms:

  • decrease in blood pressure ≤ 90 mm Hg. at .;
  • pallor;
  • increased sweating;
  • low pulse filling
  • tachycardia
  • dizziness (including orthostatic reactions when the position of the body changes)
  • headache;
  • weakness,
  • nausea
  • vomiting
  • diarrhea
  • relative to patients taking other nitrates, reported cases of methaemoglobinaemia. During the biotransformation of isosorbide dinitrate, nitrite ions are released that can induce methemoglobinemia and cyanosis, followed by tachypnea, a sense of anxiety, loss of consciousness, and cardiac arrest. It is impossible to exclude the possibility of this side reaction in case of an overdose of isosorbide dinitrate;
  • excessive doses can increase intracranial pressure, sometimes causes cerebral symptoms.

General activities:

  • stop the drug
  • general measures used in the case of nitrate-induced hypotension:
  • provide the patient a horizontal position with the head down while the head is low;
  • ensure the supply of oxygen;
  • increase circulating volume;
  • conduct a special anti-shock therapy (the patient must be in the intensive care unit).

Special events.
There is no specific antagonist of the vasodilator effect of isosorbide dinitrate. Since arterial hypotension, developing in case of overdose, is the result of venodilation and arterial hypovolemia, therapy should be aimed at increasing the volume of circulating blood (see "General measures"). Sometimes it is enough to give the patient a horizontal position.Sometimes it is necessary to make an infusion of 0.9% solution of sodium chloride (or similar) solution. The use of epinephrine in this situation is not recommended (the harmful effect over the positive predominates).

Treatment of methemoglobinemia:

  • Restorative therapy with vitamin C, methylene blue or toluidine blue to choose from;
  • the use of oxygen (if necessary);
  • artificial ventilation, blood replacement (if necessary).
  • hemodialysis (if necessary).

Resuscitative measures:

  • In the event of signs of stopping breathing or circulation, immediate resuscitation should be taken.

Adverse Reactions

From the cardiovascular system: peripheral edema (usually in patients with left ventricular failure) short-term hyperemia of the face; arterial hypertension and / or orthostatic hypotension bradycardia heart rhythm disturbances; reflex tachycardia at the first application or with an increase in the dose there is a decrease in blood pressure and / or with a change in body position, sometimes, with a significant decrease in blood pressure, there may be an increase in the symptoms of angina pectoris; may develop collapse (which is sometimes accompanied by bradyarrhythmia (slow heartbeat) and short-term loss of consciousness (syncope) .Throughout therapy, the drug may experience temporary hypoxemia due to a relative redistribution of blood flow to the alveolar zones with hypoventilation.In patients with coronary heart disease this may lead to a temporary hypoxia of the myocardium.

From the side of the digestive tract: nausea vomiting heartburn; constipation, a feeling of mild burning tongue, dry mouth.

General disorders: sensation of weakness.

From the side of the nervous system: hemorrhage in the pituitary gland in patients with undiagnosed pituitary tumor headache; dizziness drowsiness sensation of fever; "Nitrate" headache at the beginning of treatment, which usually gradually decreases / disappears with further administration of the drug, but can be strong and stable.

From the skin and subcutaneous tissue: redness of the skin and allergic reactions, including rash, itching, angioedema, pale skin; in some cases there is exfoliative dermatitis Stevens-Johnson syndrome.

From the side of the organ of vision: blurred vision; glaucoma; cases of visual hallucinations; narrowing of the field of view.

Common violations: hot flashes; sweating; hyperhidrosis; hematological side effects, including methemoglobinemia;cases of isosorbide dinitratin-induction and hemolytic anemia in patients with concomitant insufficiency of glucose-6-phosphate dehydrogenase.

The cases of tolerance development to isosorbide dinitrate, as well as cross tolerance to other nitrates have been described.

Long-term use of high doses and / or a reduction in the interval between doses may lead to a decrease or even a loss of the effect of the drug.

There have been reports of a significant increase in renin and aldosterone levels in blood plasma associated with a decrease in glomerular filtration rate and clearance of osmotically free water in patients with cirrhosis, especially with ascites.

Shelf life

3 years.

Storage conditions

Store at a temperature of no higher than 30 ° C in the original packaging. Keep out of the reach of children.

Packaging

50 tablets in a plastic can in a pack of cardboard.

Or 50 tablets (10x5) in blisters in a pack of cardboard.

Category of leave

On prescription.


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