Dilatrend pills 25 mg 30 pcs
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Active ingredients
Carvedilol
Release form
Pills
Composition
Active ingredient: Carvedilol (Carvedilol) Concentration of active ingredient (mg): 25
Pharmacological effect
The instruction for medical use of the drug was introduced by order of the Federal Service for Supervision in Healthcare and Social Development of October 21, 2005 No. 56. Carvedilol is an α1-, β1, and β2-adrenoreceptor blocker, has an organoprotective effect, is a powerful antioxidant that eliminates free oxygen radicals, possesses antiproliferative action against smooth muscle cells of vascular walls. Carvedilol is a racemic mixture of R (+) and S (-) stereoisomers, each of which has the same a-adrenergic blocking and antioxidant properties. The beta-adrenergic blocking effect of carvedilol is non-selective in nature and is due to the levorotatory S (-) stereoisomer. 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, so fluid retention (characteristic of selective alpha-adrenoblokatolorov) rarely occurs. Selectively blocking α1-adrenoreceptors, carvedilol reduces total peripheral vascular resistance. effects on the lipid profile, while maintaining a normal ratio of high and low density lipoproteins (HDL / LDL). EfficacyArterial hypertension. In patients with arterial hypertension, carvedilol reduces arterial pressure (BP) due to the combined blockade of β- and α1-adrenergic receptors. Reduction in blood pressure is not accompanied by a simultaneous increase in total peripheral vascular resistance, which is observed when taking non-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 organs and peripheral blood flow, including skeletal muscles, forearms, lower limbs, skin, brain, and carotid artery. Cooling of the limbs and fatigue during exercise are rare.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 (an increase in the total duration of exercise, the time until depression of the ST segment is 1 mm deep, and the time until an angina attack occurs), which is maintained during prolonged therapy. Carvedilol significantly reduces the oxygen demand of the myocardium and the activity of the sympathoadrenal system. Also reduces preload (pulmonary arrest pressure and pulmonary capillary pressure) and afterload (total peripheral vascular resistance). Chronic heart failure. Carvedilol reduces mortality in patients with chronic heart failure of any stage and functional class and is well tolerated (COPERNICUS, COMET studies). Carvedilol significantly reduces the need for cardiovascular hospitalization, it increases the ejection fraction and reduces symptoms in patients with chronic ischemic heart failure and non-ischemic genesis. The effects of carvedilol are dose-dependent.
Pharmacokinetics
AbsorptionAfter ingestion, carvedilol is rapidly absorbed. The maximum plasma concentration (Cmax) is reached in approximately 1 hour. The absolute bioavailability of carvedilol is approximately 25%. Distribution Carvedilol is highly lipophilic. About 98-99% of carvedilol binds to plasma proteins. Its volume of distribution is approximately 2 l / kg. MetabolismCarvedilol undergoes biotransformation in the liver with the formation of a number of metabolites - 60-75% of the absorbed drug is metabolized during the first “passage” through the liver. The existence of the enterohepatic circulation of the initial substance is shown. As a result of demethylation and hydroxylation of the phenol ring, 3 metabolites are formed (their concentration is 10 times lower than the concentration of the initial substance) with beta-adrenergic blocking activity (in a 4'-hydroxyphenol metabolite it is about 13 times stronger than carvedilol itself). 3 active metabolites have weaker vasodilating properties than carvedilol.Two of the hydroxycarbazole metabolites of carvedilol are extremely powerful antioxidants, and their activity in this regard is 30-80 times higher than that of carvedilol. Introduction The half-life of carvedilol is about 6 hours, the plasma clearance is about 500-700 ml / min. Excretion occurs mainly in the feces, the main route of excretion is through bile. A small part of the dose is excreted through the kidneys in the form of various metabolites. Pharmacokinetics in special groups of patients Patients with impaired renal function. With long-term carvedilol therapy, the intensity of the renal blood flow is maintained, the glomerular filtration does not change. In patients with arterial hypertension with renal insufficiency, the area under the concentration-time curve, the half-life and maximum plasma concentrations do not change. Renal excretion of unchanged drug in patients with renal insufficiency is reduced, however, changes in pharmacokinetic parameters are moderately expressed. Carvedilol is an effective drug for treating patients with arterial hypertension of renal origin (“renal hypertension”), including in patients with chronic renal failure, as well as in patients on hemodialysis or after a kidney transplant. Carvedilol causes a gradual decrease in blood pressure both on the day of dialysis and on days without dialysis, and its hypotensive effect is comparable to that in patients with normal renal function. Carvedilol is not excreted during dialysis because it does not cross the dialysis membrane, probably due to its strong binding to plasma proteins. Patients with impaired liver function. In patients with cirrhosis of the liver, the systemic bioavailability of the drug is increased by 80% due to a decrease in the severity of metabolism during the first “passage” through the liver. Therefore, carvedilol is contraindicated in patients with clinically manifestly impaired liver function (see “Contraindications”). Patients of elderly and old age. Age does not affect the pharmacokinetics and tolerability of carvedilol in patients with arterial hypertension. Children. Data on the pharmacokinetics of the drug in patients under 18 years of age are currently limited. Patients with diabetes.In patients with type 2 (insulin-independent) diabetes mellitus and arterial hypertension, carvedilol did not affect the fasting blood glucose concentration after eating, the level of glycated hemoglobin (HbA1), or the dose of hypoglycemic drugs. In some clinical studies, it has been shown that carvedilol does not cause changes in glucose tolerance test scores of non-insulin dependent diabetes mellitus. In patients with arterial hypertension without diabetes mellitus, who had insulin resistance (Syndrome X), carvedilol improves insulin sensitivity. Similar results were obtained in patients with arterial hypertension and type 2 diabetes mellitus (non-insulin-dependent).
Indications
Essential hypertension (in monotherapy or in combination with other antihypertensive drugs, such as “slow” calcium channel blockers or diuretics). Ischemic heart disease (including in patients with unstable angina and painless myocardial ischemia). Treatment of stable and symptomatic mild, moderate and severe chronic heart failure (NYHA classification II-IV functional class) of ischemic or non-ischemic genesis in combination with angiotensin-converting enzyme inhibitors (ACE) and diuretics, with or without cardiac glycosides (standard therapy), in the absence of contraindications.
Contraindications
Hypersensitivity to carvedilol or any component of the drug; acute and chronic heart failure in the decompensation stage, requiring intravenous administration of inotropic drugs; clinically significant impaired liver function; age up to 18 years (efficacy and safety of the drug Dilatrend not installed); atrioventricular block II and III degree (except for patients with an artificial pacemaker); severe bradycardia (heart rate less than 50 beats / min); sick sinus syndrome (including sinoauricular block); severe arterial hypotension (systolic blood pressure less than 85 mm Hg. Art.); cardiogenic shock; anamnestic indications of bronchospasm and bronchial asthma; lactose intolerance, lactase deficiency, fructose intolerance, glucose / galactose absorption disorder syndrome, sucrase / isomaltase deficiency (the product contains sucrose); pheochromocytoma (without simultaneous use of alpha-blockers).
Precautionary measures
Do not exceed the recommended dose. With caution, the drug is used in chronic obstructive pulmonary disease (COPD), depression, myasthenia, hypoglycemia, grade I AV-blockade, thyrotoxicosis, with extensive surgical interventions and general anesthesia, Prinzmetal angina, diabetes, occlusive diseases, peripherals , pheochromocytoma, renal failure, psoriasis.
Use during pregnancy and lactation
Beta-blockers reduce placental blood flow, which can lead to fetal death and premature birth. In addition, unwanted reactions may 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. Pregnant women do not have sufficient experience with Dilatrend. Carvedilol is contraindicated in pregnancy, unless the possible benefits of its use exceed the potential risk to the woman and the fetus. In animals, carvedilol and its metabolites pass into breast milk. Data on the excretion of the drug with human milk is not, therefore, it should not be used during lactation.
Dosage and administration
Inside, drinking plenty of fluids. Essential hypertension The recommended initial dose is 12. 5 mg 1 time per day for the first 2 days of treatment, then 25 mg 1 time per day. If necessary, further dose can be increased at intervals of at least 2 weeks, bringing to the maximum recommended dose of 50 mg 1 time per day (or divided into 2 doses). Ischemic heart disease. The recommended initial dose is 12. 5 mg 2 times a day for the first 2 days, then 25 mg 2 times a day. If necessary, subsequently, the dose can be increased at intervals of at least 2 weeks, bringing to a maximum daily dose of 100 mg divided into 2 doses. Chronic heart failure. The dose is selected individually, it is necessary to carefully monitor the doctor. In patients receiving cardiac glycosides, diuretics, and ACE inhibitors, their doses should be adjusted prior to treatment with Dilatrend. The recommended initial dose is 3. 125 mg (1/2 pills of 6. 25 mg) 2 times a day for 2 weeks.With good tolerance, the dose is increased at intervals of at least 2 weeks to 6. 25 mg 2 times a day, then up to 12. 5 mg 2 times a day, then up to 25 mg 2 times a day. The dose should be increased to a maximum dose that is well tolerated by the patient. 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 patient's 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 2 times a day.
Side effects
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 the extremities, 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 hepatic transaminases - alanine aminotransferase (ALT), aspartate aminotransferase (ACT) and gamma-glutamyltransferase, thrombocytopenia 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.
Overdose
Symptoms: marked reduction 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 signs, and if necessary, in the intensive care unit.The following measures can be used: a) put the patient on his back (with raised legs) b) with severe bradycardia - atropine at 0.5-2 mg IV, c) to maintain cardiovascular activity - glucagon at 1-10 mg IV spray, then 2-5 mg per hour in the form of a long-term infusion; d) sympathomimetics (dobutamine, isoprenaline, ortsiprenalin or epinephrine (adrenaline) in various doses, depending on body weight and therapeutic efficacy. If necessary, the administration of drugs with positive inotropic action prescribed phosphodia inhibitors steraz. If arterial hypotension dominates in the clinical picture of an overdose, norepinephrine (norepinephrine) is administered; it is prescribed under continuous monitoring of blood circulation indicators. An artificial pacemaker is indicated for treatment-resistant bradycardia. w / w) or aminophylline w / w.When convulsions w / w, diazepam or clonazepam is slowly injected. As a severe overdose with symptoms of shock, prolongation is possible. The half-life of carvedilol and excretion of the drug from the depot, it is necessary to continue maintenance therapy for quite 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.
Interaction with other drugs
Digoxin. When co-administered with carvedilol and digoxin, the concentration of digoxin increases by about 15%. Both digoxin and carvedilol slow down atrioventricular conductivity. 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 drugs. Preparations with beta-adrenoblokiruyuschim properties can enhance the hypoglycemic effect of insulin or oral hypoglycemic 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. Inducers or inhibitors of hepatic metabolism.Rifampicin reduces plasma concentrations of carvedilol by about 70%. Cimetidine increases the area under the concentration-time curve by about 30%, but does not change Cmax. Caution may be required in patients receiving inducers of polyfunctional oxidases, for example, rifampicin (a decrease in plasma concentrations of carvedilol), as well as inhibitors of polyfunctional oxidases, for example, cimetidine (increases in plasma concentrations of carvedilol). However, given the relatively insignificant effect of cimetidine on the concentration of carvedilol, the probability of any clinically significant interactions is minimal. Preparations 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 carefully monitored due to the risk of arterial hypotension and / or severe bradycardia. Cyclosporin. When carvedilol was prescribed to patients who underwent a kidney transplant, who developed chronic vascular graft rejection, a moderate increase in mean minimum concentrations of cyclosporine was noted. In order to maintain the concentration of cyclosporine in the therapeutic range, approximately 30% of patients had to reduce the dose of cyclosporine (on average by 20%), the rest of the patients did not need dose adjustment. Due to the pronounced individual fluctuations in the required daily dose of cyclosporine, careful monitoring of the concentration of cyclosporine after starting carvedilol therapy and, if necessary, appropriate correction of the daily dose of cyclosporine is recommended. Verapamil, diltiazem and other antiarrhythmic drugs (propranolol, amiodarone). Simultaneous use 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-adrenergic blocking properties and clonidine, first you should cancel the beta-blocker, and after a few days you can cancel clonidine, gradually reducing its dose. Blockers of “slow” calcium channels. 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 together with blockers of “slow” calcium channels like verapamil or diltiazem under ECG and BP control. simultaneously taken antihypertensive agents (for example, α1-blockers) or drugs that have a hypotensive effect as a side effect. It prevents the increase in blood pressure, calling Vai introduction of α1-adrenoceptor agonist - phenylephrine, but does not affect the increase in blood pressure caused by angiotensin II.Osoboe attention should be paid during general anesthesia, the possibility of synergistic negative inotropic effects of carvedilol and some anesthetics.
special instructions
Chronic heart failure. In patients with chronic heart failure, during the period of Dilatrend dose selection, there may be an increase in symptoms of heart failure or fluid retention. In the event 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 (possibly excessive slowing of AV conduction). Renal function in chronic heart failure. When Dilatrend is prescribed to patients with chronic heart failure and low blood pressure (systolic BP less than 100 mm Hg), ischemic disease heart and diffuse changes of blood vessels and / or renal failure was observed reversible deterioration of renal function. The dose of the drug is regulated depending on the functional state of the kidneys. Chronic obstructive pulmonary disease (COPD). Patients with chronic obstructive pulmonary diseases (including those with bronchospastic syndrome) who do not receive oral or inhalation anti-asthma drugs are prescribed 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 Dilatrend dose of these patients, it is necessary to carefully observe, reducing the dose of the drug when the initial signs of bronchospasm appear. Diabetes mellitus. 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 diseases. Caution is needed when prescribing Dilatrend in 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 surgical procedures. Caution is required in patients undergoing surgery under general anesthesia, due to 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. Increased sensitivity. 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 the severity of anaphylactic reactions. Psoriasis. Patients with anamnestic indications for the occurrence or exacerbation of psoriasis when using beta-blockers, Dilatrend can be assigned only after careful analysis of 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 the ECG and BP. Feochromocytoma.Patients with pheochromocytoma prior to the use of any beta-blocker must be assigned an alpha 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 used with caution in patients with suspected pheochromocytoma. Prinzmetal angina pectoris. 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 prescribed in such cases 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 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 coronary heart disease. When stored in the light, the pills may change color. If surgery is necessary with general anesthesia, the anesthesiologist should be warned about prior Dilatrend therapy. During treatment, ethanol use is excluded. and work with machines 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). It should be carefully prescribed to patients whose work requires a quick psychomotor reaction.