DILATREND PILLS 12.5 MG

Active ingredient and dosage form

Tablets: 1 pill contains Carvedilol - 6.25 mg, 12.5 mg or 25 mg;
30, 50 or 100 pills in a carton box.

П №015353 / 01

Alpha and beta blocker

Carvedilol is a multifunctional adrenoreceptor blocker with beta1, beta2, and alpha1 adrenoceptor blocking properties. Carvedilol has an organ-protective effect. It is a powerful antioxidant that eliminates free oxygen radicals, has antiproliferative effects against smooth muscle cells of the walls of blood vessels.
Carvedilol has no internal sympathomimetic activity and, like propranolol, has membrane stabilizing properties. By blocking beta-adrenoreceptors, it reduces the activity of the renin-angiotensin-aldosterone system, reducing the release of renin, therefore fluid retention (characteristic of selective alpha-adrenoblocktrakers) rarely occurs.
Selectively blocking a1adrenoreceptors, carvedilol reduces total peripheral vascular resistance.
Carvedilol does not adversely affect the lipid profile, maintaining a normal ratio of lipoproteins with a height of density to low density lipoprotein (HDL / LDL).

Arterial hypertension. In patients with arterial hypertension, carvedilol lowers blood pressure caused by combined blockade of b-and a-adrenoreceptors. A decrease in blood pressure is not accompanied by a simultaneous increase in total peripheral vascular resistance, which is observed when taking selective beta-blockers. Heart rate decreases slightly. Renal blood flow and renal function in patients with arterial hypertension remain. It was shown that carvedilol does not alter the stroke volume and decreases the total peripheral vascular resistance; does not violate the blood supply to the organs and peripheral blood flow, including the skeletal muscles, forearms, lower limbs, skin, brain, and carotid artery. Cooling of the limbs and early onset of fatigue during physical exertion are rarely observed. The hypotensive effect of carvedilol in hypertension persists for a long time.
Coronary heart disease. In patients with ischemic heart disease, carvedilol has anti-ischemic and antianginal effects, which persist during long-term therapy. Carvedilol significantly reduces the oxygen demand of the myocardium and the activity of the sympathoadrenal system. It also reduces the preload (pulmonary arrest pressure and pulmonary capillary pressure) and the afterload (total peripheral vascular resistance).
Chronic heart failure . Recent clinical studies, including Copernicus, have shown that carvedilol is effective and well tolerated by patients with chronic heart failure of any severity, reducing their mortality.

Carvedilol significantly reduces overall mortality and the need for cardiovascular hospitalization. It also increases the ejection fraction and reduces symptoms in patients with chronic heart failure of ischemic and non-ischemic genesis. The effects of carvedilol are dose-dependent.

Indications and usage

Arterial hypertension. Dilatrend is indicated mainly for essential hypertension (as monotherapy or combination therapy with other antihypertensive drugs, for example, blockers of “slow” Calcium channels or diuretics).
Coronary heart disease (including in patients with unstable angina and painless myocardial ischemia).
Chronic heart failure. Dilatrend is indicated for the treatment of clinically manifested mild, moderate and severe chronic heart failure of ischemic or non-ischemic genesis, for reducing the number of complications (hospitalization for cardiovascular causes) and mortality, as well as improving health and slowing progression of the disease when used in combination with inhibitors ACE, diuretics, and sometimes digitalis preparations (standard therapy).Dilatrend can be prescribed both in addition to standard therapy and to patients who do not receive digitalis, vasodilators, or nitrates.

Contraindications

Hypersensitivity to carvedilol or any component of the drug, acute heart failure, clinically significant impaired liver function, breastfeeding period.
Like other beta-blockers, Dilatrend should not be prescribed to patients with atrioventricular block II and III (unless a permanent pacemaker is installed), severe bradycardia (less than 50 beats / min), sick sinus syndrome, severe arterial hypotension (systolic blood pressure less than 85 mm Hg.), cardiogenic shock, anamnestic indications of bronchospasm and bronchial asthma. With caution, use the drug for emphysema, depression, myasthenia, pregnancy.

Dosage and administration

The drug is taken orally with a sufficient amount of liquid.

Dilatrend treatment is carried out for a long time. It should not be stopped abruptly, it is necessary to gradually reduce the dose of the drug at weekly intervals. This is especially important in patients with ischemic heart disease.
Essential hypertension. The recommended initial dose is 12.5 mg once a day for the first 2 days, then 25 mg once a day. If necessary, further dose can be increased at intervals of at least 2 weeks, bringing to the highest recommended dose of 50 mg once a day (or divided into two doses).
Coronary heart disease. The recommended initial dose is 12.5 mg twice a day for the first 2 days, then 25 mg twice a day. If necessary, subsequently, the dose can be increased at intervals of at least two weeks, bringing to the highest daily dose of 100 mg, divided into two doses.
Chronic heart failure. The dose is selected individually, under the close supervision of a doctor. In patients receiving digitalis, diuretics and ACE inhibitors, their doses should be stabilized before the start of treatment with Dilatrend. The recommended starting dose is 3.125 mg twice a day for two weeks. With good tolerance, the dose is increased at intervals of at least two weeks, to 6.25 mg twice a day, then to 12.5 mg twice a day, then to 25 mg twice a day. The dose should be increased to the maximum, which is well tolerated by patients. The recommended maximum dose is 25 mg 2 times a day for all patients with severe chronic heart failure and for patients with mild and moderate degrees of chronic heart failure with a body weight less than 85 kg. In patients with mild and moderate chronic heart failure and weighing more than 85 kg, the recommended maximum dose is 50 mg twice a day. Before each increase in dose, the physician should examine the patient to identify a possible increase in symptoms of heart failure or vasodilation. With a transient increase in symptoms of heart failure or fluid retention, the dose of diuretics should be increased, although sometimes it is necessary to reduce the dose of Dilatrend or temporarily cancel it.

If treatment with Dilatrend is interrupted for more than 1 week, then its administration is resumed at a lower dose, and then increased in accordance with the above recommendations. If treatment with Dilatrend is interrupted for more than 2 weeks, it should be resumed at a dose of 3.125 mg twice a day, then the dose should be adjusted in accordance with the above recommendations.

Symptoms of vasodilation can be eliminated by reducing the dose of diuretics. If the symptoms persist, you can reduce the dose of the ACE inhibitor (if the patient takes it), and then, if necessary, the dose of Dilatrend. In this situation, you should not increase the dose of Dilatrend until the symptoms of increasing heart failure or arterial hypotension stabilize. Doses in special groups of patients

Existing data on pharmacokinetics in patients with varying degrees of renal dysfunction (including renal insufficiency) suggest that patients with moderate and severe renal insufficiency do not require Dilatrend dose adjustment.
Liver dysfunction. Dilatrend is contraindicated in patients with clinical manifestations of abnormal liver function (see "Contraindications").
Patients of advanced age. Data that would dictate the need for dose adjustment are not available.

Adverse events in patients receiving treatment for hypertension and coronary heart disease
The nature of Dilatrend's side effects in the treatment of arterial hypertension and long-term treatment of coronary heart disease is similar to that in heart failure, but their frequency is somewhat less.
The following adverse events were observed in clinical studies in patients with arterial hypertension and ischemic heart disease.
Central nervous system. Frequent: dizziness, headache and general weakness, usually mild and occurring, in particular, at the beginning of treatment. Infrequent: decrease in mood, sleep disorders, paresthesias.
The cardiovascular system. Frequent: bradycardia, postural hypotension, syncopal states, especially at the beginning of therapy. Infrequent: peripheral circulatory disorders (cooling of limbs, exacerbation of intermittent claudication and Raynaud's syndrome), atrioventricular blockade of angina (chest pain), symptoms of heart failure and peripheral edema.
Respiratory system. Frequent: bronchospasm and shortness of breath in predisposed patients. Rare: nasal congestion.
Gastrointestinal tract. Frequent: dyspeptic disorders (including nausea, abdominal pain, diarrhea). Infrequent: constipation, vomiting.
The skin. Infrequent: skin reactions (allergic rash, dermatitis, urticaria, and itching).
Laboratory indicators. Individual cases of increased activity of liver transaminases - alanine aminotransferase (ALT), aspartate aminotransferase (ACT) and gamma glutamyltransferase, thrombotic cytopenia and leukopenia.
Other Frequent: pain in the limbs, reduction of tearing and eye irritation.Infrequent: decrease in a potentiality, a vision disorder. Rare: dry mouth and urination disorders.

Isolated cases of allergic skin reactions (rash, urticaria, pruritus, rash), exacerbation of psoriatic lesions, sneezing, nasal congestion, bronchospasm, shortness of breath (in predisposed patients). Selected cases of influenza-like syndrome.
The presence of beta-adrenergic blocking properties of the drug does not exclude the possibility of latent diabetes mellitus manifestation, worsening of the compensation of the already existing diabetes mellitus or suppression of the contrainsular system.

Symptoms: pronounced decrease in blood pressure, bradycardia, heart failure, cardiogenic shock, cardiac arrest; respiratory disorders, bronchospasm, vomiting, confusion, and generalized convulsions are possible.
Treatment: in addition to general measures, it is necessary to monitor and correct vital indicators, and if necessary, in the intensive care unit. You can use the following activities:
a) put the patient on his back
b) with severe bradycardia, atropine 0.5-2 mg intravenously;
c) for the maintenance of cardiovascular activity - glucagon 1-10 mg intravenously in a stream, then 2-5 mg per hour in the form of a long-term infusion;
d) sympathomimetics (dobutamine, isoprenaline, orciprenaline or epinephrine) in various doses, depending on body weight and therapeutic efficacy.If necessary, the introduction of drugs with a positive inotropic effect, phosphodiesterase inhibitors are prescribed. If hypotension dominates the clinical picture of an overdose, norepinephrine is administered; it is prescribed in conditions of continuous monitoring of blood circulation parameters.

In case of treatment-resistant bradycardia, the use of an artificial pacemaker is indicated.

In case of bronchospasm, beta-adrenomimetics are administered in the form of an aerosol (if it is ineffective, intravenously) or aminophylline is administered intravenously. For convulsions, diazepam or clonazepam is slowly injected intravenously. Since severe overdose with symptomatic shock may prolong the half-life of carvedilol and remove the drug from the depot, it is necessary to continue maintenance therapy for a long time. The duration of maintenance / detoxification therapy depends on the severity of the overdose, it should be continued until the patient’s condition stabilizes.

Digoxin. With the simultaneous use of carvedilol and Digoxin , the concentration of digoxin increases by about 15%. At the beginning of therapy with carvedilol, with the selection of its dose or withdrawal of the drug, regular monitoring of the concentration of digoxin in the blood plasma is recommended.
Insulin or oral hypoglycemic agents. Drugs with beta-adrenergic blocking properties may enhance the hypoglycemic effect of insulin or oral glucose-lowering agents. Symptoms of hypoglycemia, especially tachycardia, may be masked or weakened. Patients receiving insulin or oral hypoglycemic drugs are recommended regular monitoring of blood glucose.
Inductors or inhibitors of hepatic metabolism. Rifampicin reduces plasma concentrations of carvedilol by about 70%.
Drugs that reduce the content of catecholamines. Patients who are taking drugs with beta-adrenergic blocking properties, and drugs that reduce the content of catecholamines (for example, reserpine and monoamine oxidase inhibitors) should be closely monitored for the risk of arterial hypotension and / or severe bradycardia.
Cyclosporine. When carvedilol was prescribed to patients who underwent a kidney transplant, who developed chronic vascular graft rejection, moderately increased mean minimum concentrations of cyclosporine were observed. patients dose adjustment is not needed. Due to the pronounced individual fluctuations in the required daily dose of cyclosporine, careful monitoring of the concentration of cyclosporine after initiation of carvedilol therapy and, if necessary, appropriate correction of the daily dose of cyclosporine is recommended. Verapamil diltiazem and other antiarrhythmic drugs (propranolol, amiodarone).Simultaneous administration with carvedilol may increase the risk of atrioventricular conduction disturbance.
Clonidine. Simultaneous administration of clonidine with drugs with beta-blocking properties may potentiate antihypertensive and heart rate-reducing effects. If you plan to stop the combination therapy with beta-adreno-blocking properties and clonidine, first you should cancel the beta-blocker, and after a few days you can cancel the clonidine, gradually reducing its dose.
Slow calcium channel blockers. With the simultaneous appointment of carvedilol and diltiazem, there were isolated cases of conduction disturbances (rarely with impaired hemodynamic parameters). As in the case of other drugs with beta-adrenergic blocking properties, carvedilol should be prescribed with blockers of “slow” calcium channels like Verapamil or diltiazem under ECG and blood pressure monitoring.

Like other drugs with beta-adrenergic blocking activity, carvedilol may enhance the effects of other concomitant antihypertensive drugs (for example, u -blockers) or drugs that have a hypotensive effect as a side effect.
Particular attention should be paid when conducting general anesthesia to the possibility of a synergistic negative inotropic effect of carvedilol and some anesthetics.

Chronic heart failure. In patients with chronic heart failure during the selection period of Dilatrend, there may be an increase in the symptoms of heart failure or fluid retention. In case of such symptoms, it is necessary to increase the dose of diuretics and not to increase the dose of Dilatrend until the patient's condition stabilizes. Sometimes it is necessary to reduce the dose of Dilatrend or, in rare cases, temporarily cancel the drug. Such episodes do not interfere with further proper selection of the Dilatrend dose. Dilatrend is used with caution in combination with cardiac glycosides (excessive retardation of atrioventricular conductivity is possible).
Kidney function in chronic heart failure. When Dilatrend was prescribed, patients with chronic heart failure and low blood pressure (systolic blood pressure <100 mmHg), coronary heart disease and diffuse vascular changes and / or renal failure showed a reversible deterioration in renal function. The dose of the drug regulate depending on the functional state of the kidneys.
Chronic obstructive pulmonary disease. Patients with chronic obstructive pulmonary diseases (including bronchospastic syndrome) who do not receive oral or inhalation anti-asthma drugs are given Dilatrend only if the possible benefits of its use outweigh the potential risk.If there is an initial propensity for the bronchospastic syndrome when taking Dilatrend as a result of an increase in airway resistance, respiratory distress syndrome may develop. At the beginning of the reception and with an increase in the dose of Dilatrend of these patients, it is necessary to observe it, reducing the dose of the drug when the initial signs of bronchospasm appear
Diabetes. With caution, the drug is prescribed to patients with diabetes mellitus, since it can mask or alleviate the symptoms of hypoglycemia (especially tachycardia). In patients with heart failure and diabetes, the use of Dilatrend may be accompanied by decompensation of carbohydrate metabolism.
Peripheral vascular disease. Caution is needed when prescribing Dilatrend to patients with peripheral vascular diseases (including Raynaud's syndrome), since beta-blockers may increase the symptoms of arterial insufficiency.
Thyrotoxicosis. Like other beta-blockers, Dilatrend may reduce the severity of thyrotoxicosis symptoms.
General anesthesia and major surgery. Caution is required in patients undergoing surgery under general anesthesia because of the possibility of summing up the negative effects of Dilatrend and anesthetics.
Bradycardia. Dilatrend can cause bradycardia, with a decrease in heart rate below 55 beats per minute, the dose of Dilatrend should be reduced.
Hypersensitivity. Care must be taken when prescribing Dilatrend to individuals with anamnestic indications of severe hypersensitivity reactions or undergoing desensitization, since beta-blockers may increase sensitivity to allergens and severity of Anaphylactic reactions .
Psoriasis. Patients with anamnestic indications for the occurrence or worsening of psoriasis when using beta-blockers, Dilatrend can be assigned only after a careful analysis of the possible benefits and risks.
Simultaneous reception of blockers of "slow" calcium channels. In patients who simultaneously take blockers of "slow" calcium channels such as verapamil or diltiazem, as well as other antiarrhythmic drugs, it is necessary to regularly monitor ECG and blood pressure.
Pheochromocytoma. Patients with pheochromocytoma prior to the use of any beta-blocker, you must assign an alfz-blocker. Although Dilatrend has both beta and alpha-adrenergic blocking properties, there is no experience with its use in such patients, so it should be prescribed with caution in patients with suspected pheochromocytoma.
Printsmetal angina Non-selective beta-blockers can provoke pain in patients with Prinzmetal angina. Experience Dilatrend destination these patients do not. Although its alpha-adrenergic blocking properties can prevent similar symptoms, carvedilol should be administered with caution in such cases. Elderly age: use with caution.
Contact lenses. Persons using contact lenses should be aware of the possibility of reducing the amount of tear fluid.
Cancellation syndrome. Dilatrend treatment cannot be interrupted abruptly, especially in patients with coronary heart disease. Cancel Dilatrend should be gradual (within 2 weeks). When stored in the light may change the color of the tablets.
If it is necessary to perform a surgical intervention using anesthesia, it is necessary to warn the anesthesiologist about the previous treatment with Dilatrend. During treatment, the use of ethanol is excluded.
Pregnancy and lactation period. Beta-blockers reduce perfusion of the placenta, which can lead to fetal death and premature labor. In addition, adverse events can occur in the fetus and newborn (in particular, hypoglycemia and bradycardia, complications of the heart and lungs). Studies on animals did not reveal his teratogenicity. There is not enough experience with Dilatrend in pregnant women. Carvedilol can be prescribed during pregnancy only if the possible benefits of its use exceed the potential risk to the woman and the fetus.
In animals, carvedilol and its metabolites enter breast milk. Data on the excretion of the drug with human milk is not, therefore, it should not be used during lactation. Influence on ability to driving of vehicles and work with cars and mechanisms.Studies on the effect of Dilatrend on the ability to drive vehicles or work with machines and mechanisms were not conducted. Due to individual reactions to the drug (for example, dizziness, general weakness) it can be disturbed (especially at the beginning of treatment, when the dosage is changed, and also in the case of simultaneous alcohol intake).

Store at a temperature not exceeding 30 ° C, protected from light.
Keep out of the reach of children.
Since the color of the pills changes when exposed to light, it is recommended to store them in closed boxes.

Dilatrend