Carveland tablets 12.5mg №10×3

NameKarveland tabl. The main active ingredient carvedilol Release form tablets Dosage 12.5 mg Pharmacological properties Pharmacodynamics Carveland has a combined non-selective a1-, b1-, b2-blocking and antioxidant effect. Its vasodilatory effect is mediated primarily through selective blockade of a1 receptors. Karveland reduces the activity of the renin-angiotensin-aldosterone system, reducing the release of renin, so fluid retention (characteristic of selective alpha-blockers) rarely occurs. Karveland does not have its own sympathomimetic activity, it has membrane stabilizing properties. Carveland is a powerful antioxidant that eliminates free oxygen radicals. The combination of vasodilation and b-blockade when using carveland has the following effect: in patients with arterial hypertension, the decrease in blood pressure is not accompanied by a simultaneous increase in total peripheral vascular resistance, which is observed when taking b-blockers; the heart rate decreases slightly; renal blood flow and kidney function are preserved. Peripheral blood flow does not change, so cold extremities (often occurring during treatment with conventional b-blockers) are rarely observed. In patients with coronary heart disease, Carveland has an anti-ischemic and antianginal effect, which persists with long-term use. Hemodynamic studies after a single administration of the drug showed that carveland reduces pre- and afterload. In patients with impaired left ventricular function or circulatory insufficiency, carveland favorably affects hemodynamic parameters, increases ejection fraction and reduces the size of the left ventricle. When taking the drug, the ratio of high-density lipoproteins to low-density lipoproteins remains normal, the concentration of electrolytes in the serum does not change. Pharmacokinetics After oral administration, Carveland is rapidly absorbed. The maximum serum concentration is reached after about 1 hour. The absolute bioavailability of carveland in humans is approximately 25%. Eating does not affect bioavailability. In case of impaired liver function, bioavailability increases by 80% due to a decrease in the effect of the first passage through the liver. With long-term therapy, cumulation of carveland is not observed. The half-life of carveland is 6-10 hours, plasma clearance is about 590 ml / min. Excretion occurs mainly with bile. A small part of the dose is excreted through the kidneys in the form of various metabolites. Indications for use Arterial hypertension. Essential hypertension (in monotherapy – or in combination with other antihypertensive agents, for example, blockers of “slow” calcium channels or diuretics). Ischemic heart disease (including in patients with unstable angina and painless myocardial ischemia). Chronic heart failure. Treatment of stable and symptomatic mild, moderate and severe chronic heart failure (FC II-IV according to the New York Heart Association, NYHA) of ischemic or non-ischemic origin in combination with hypotensin-converting enzyme (ACE) inhibitors and diuretics, with or without cardiac glycosides (standard therapy), in the absence of contraindications. Dosing and Administration Carveland tablets should be swallowed with a sufficient amount of liquid. It is not necessary to associate the drug with food intake, however, in patients with circulatory insufficiency, it is preferable to prescribe it during meals (to slow down the rate of absorption and reduce the risk of orthostatic reactions). Essential hypertension The recommended starting dose is 12.5 mg once daily for the first 2 days, followed by 25 mg once daily. If necessary, the dose can be increased at intervals of no more than two weeks, reaching the highest recommended dose of 50 mg once a day (or divided into two doses). Ischemic heart disease The recommended starting dose is 12.5 mg twice daily. If necessary, the dose can subsequently be increased at intervals of at least two weeks, leading up to the highest daily dose of 100 mg, divided into two doses. For elderly patients, the highest daily dose is 50 mg divided into 2 doses. Chronic heart failure The dose is selected individually, careful medical supervision is necessary. In patients receiving cardiac glycosides, diuretics and ACE inhibitors, their doses should be adjusted before starting treatment with carveland. Dosing in Special Populations Renal Impairment Existing pharmacokinetic data in patients with varying degrees of renal impairment (including renal insufficiency) suggest that no dose adjustment of carveland is required in patients with moderate to severe renal insufficiency. Impaired liver function Carveland is contraindicated in patients with clinical manifestations of hepatic dysfunction (see section “Contraindications”). Elderly patients There are no data on the need for dose adjustment. If treatment with carveland is interrupted for more than 1 week, then its administration is resumed at a lower dose, and then increased in accordance with the recommendations above. If treatment with Carveland is interrupted for more than 2 weeks, then 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. Carveland treatment is usually carried out for a long time. Like other b-blockers, it should not be discontinued abruptly, especially in patients with coronary artery disease. The drug should be discontinued gradually (within 1-2 weeks), reducing its dose by half every 3 days. Precautions Chronic heart failure In patients with chronic heart failure during the period of carvedilol dose selection, there may be an increase in symptoms of chronic heart failure or fluid retention. If such symptoms occur, it is necessary to increase the dose of diuretics and not increase the dose of carvedilol until hemodynamic parameters stabilize. Sometimes it is necessary to reduce the dose of carvedilol, or, in rare cases, stop the drug temporarily. Carvedilol is used with caution in combination with cardiac glycosides (possibly excessive slowing of AV conduction). When Karveland was prescribed to patients with chronic heart failure and low blood pressure (systolic blood pressure less than 100 mm Hg), coronary heart disease and diffuse vascular changes and / or renal failure, a reversible deterioration in renal function was noted. The dose of the drug is adjusted depending on the functional state of the kidneys. Chronic obstructive pulmonary disease (COPD) In patients with COPD (including bronchospastic syndrome) who are not receiving oral or inhaled anti-asthma drugs, Karveland is prescribed only if the possible benefits of its use outweigh the potential risk. If there is an initial predisposition to bronchospastic syndrome when taking Carveland, shortness of breath may develop as a result of increased airway resistance. Carveland should be carefully observed at the start of treatment and when increasing the dose of the drug, reducing the dose of the drug at the onset of initial signs of bronchospasm. 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 mellitus, the use of Karveland may be accompanied by decompensation of carbohydrate metabolism. Diseases of the peripheral vessels. It should be used with caution in patients with peripheral vascular disease (including Raynaud’s syndrome), since beta-blockers may increase the symptoms of arterial insufficiency. thyrotoxicosis. Like other beta-blockers, Karveland may reduce the symptoms of thyrotoxicosis. General anesthesia and major surgery. Caution is required in patients undergoing surgery under general anesthesia due to the potential for additive adverse effects of Carveland and anesthetics. Bradycardia. Karveland can cause bradycardia when the heart rate falls below 55 bpm. The dose of Carveland should be reduced. Increased sensitivity. Caution should be exercised when prescribing Carveland to patients with a history of severe hypersensitivity reactions or undergoing desensitization, as beta-blockers may increase sensitivity to allergens and the severity of anaphylactic reactions. Psoriasis. Patients with a history of the onset or exacerbation of psoriasis when using beta-blockers, Karveland can only be prescribed after a thorough analysis of the possible benefits and risks. Simultaneous reception of “slow” calcium channel blockers (BMCC). ECG and blood pressure should be measured regularly in patients who are simultaneously taking BMCCs such as verapamil or diltiazem, as well as other antiarrhythmic drugs. Pheochromocytoma. Patients with pheochromocytoma should be given an alpha-blocker before starting any beta-blocker. Although Carveland 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’s angina. Non-selective beta-blockers can provoke pain in patients with Prinzmetal’s angina. There is no experience of prescribing Carveland in these patients. Although its alpha-adrenergic blocking properties may prevent such symptoms, Karveland should be used with caution in such cases. Contact lenses. Persons using contact lenses should be aware of the possibility of reducing the amount of tear fluid. withdrawal syndrome. Treatment with Carveland is long-term. 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. If it is necessary to perform a surgical intervention using general anesthesia, it is necessary to warn the anesthesiologist about previous therapy with Karveland. During the period of treatment, the use of alcohol is excluded. Pregnancy and lactation. Beta-blockers reduce placental perfusion, which can lead to fetal death and preterm birth. In addition, adverse effects (eg, hypoglycemia and bradycardia, cardiac and pulmonary complications) may occur in the fetus and newborn. Carveland should only be used during pregnancy if the possible benefits outweigh the potential risk to the woman and fetus. Karveland and its metabolites are excreted in breast milk, therefore, if it is necessary to prescribe the drug during lactation, the issue of stopping breastfeeding should be considered. Interaction with other drugs Pharmacokinetic interaction Since Karveland is both a substrate and an inhibitor of P-glycoprotein, when taken simultaneously with drugs transported by P-glycoprotein, the bioavailability of the latter may increase. In addition, the bioavailability of Carveland may be altered by inducers or inhibitors of P glycoprotein. Inhibitors and inducers of CYP2D6 and CYP2C9 may stereoselectively alter the systemic and/or presystemic metabolism of carvedilol, leading to an increase or decrease in plasma concentrations of the R and S stereoisomers of carvedilol. Some examples of such interactions observed in patients or healthy volunteers are listed below, but this list is not exhaustive. Digoxin. Digoxin concentrations increase by approximately 15% when Carveland and digoxin are taken concomitantly. At the beginning of therapy with Carveland, when selecting its dose or discontinuing the drug, regular monitoring of the concentration of digoxin in the blood plasma is recommended. Cyclosporine. When prescribing Carveland to kidney transplant patients who developed chronic vascular graft rejection, there was a moderate increase in the average minimum concentrations of cyclosporine. To maintain cyclosporine concentrations within the therapeutic range, approximately 30% of patients had to reduce the dose of cyclosporine (by an average of 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 the start of therapy with Carveland and, if necessary, an appropriate correction of the daily dose of cyclosporine is recommended. With intravenous administration of cyclosporine, no interaction with Karveland is expected. Rifampicin. In a study of 12 healthy volunteers, rifampicin reduced plasma concentrations of Carveland, most likely by induction of P-glycoprotein, leading to a decrease in intestinal absorption of Carveland and its antihypertensive effect. Amiodarone. In patients with heart failure, amiodarone reduced the clearance of the S stereoisomer of Carveland by inhibiting CYP2C9. The mean concentration of the R stereoisomer of Carveland did not change. Therefore, due to an increase in the concentration of the S stereoisomer of Karveland, there may be a risk of an increase in beta-adrenergic blocking action. fluoxetine. In a randomized, cross-over design study in 10 patients with heart failure, co-administration of fluoxetine (an inhibitor of CYP2D6) resulted in stereoselective inhibition of Carveland’s metabolism, with a 77% increase in mean R(+) AUC. However, there was no difference in side effects, blood pressure or heart rate between the two groups. Pharmacodynamic interactions Insulin or oral hypoglycemic agents. Drugs with beta-adrenergic blocking properties may enhance the hypoglycemic effect of insulin or oral hypoglycemic agents. Symptoms of hypoglycemia, especially tachycardia, may be masked or subsided. Patients receiving insulin or oral hypoglycemic agents are advised to regularly monitor their blood glucose levels. Drugs that reduce the content of catecholamines. Patients taking concomitant beta-adrenergic blocking agents and catecholamine-lowering agents (eg, reserpine and monoamine oxidase inhibitors) should be closely monitored due to the risk of arterial hypotension and / or severe bradycardia. Digoxin. Combination therapy of drugs with beta-adrenergic blocking properties and digoxin can lead to an additional slowdown in atrioventricular conduction. Verapamil, diltiazem and other antiarrhythmic drugs. When taken simultaneously with Karveland, the risk of impaired atrioventricular conduction may increase. Clonidine. Simultaneous administration of clonidine with drugs with beta-adrenergic blocking properties can potentiate the antihypertensive and bradycardic effect. If you plan to stop combination therapy with a drug with beta-blocking properties and clonidine, the beta-blocker should be canceled first, and after a few days clonidine can be canceled by gradually reducing its dose. Blockers of “slow” calcium channels (BMCC). With the simultaneous appointment of Karveland and diltiazem, isolated cases of conduction disturbances were noted (rarely – with violations of hemodynamic parameters). As in the case of other drugs with beta-adrenergic blocking properties, the appointment of Karveland together with BMCC such as verapamil or diltiazem is recommended under the control of ECG and blood pressure. Antihypertensive agents. As with other drugs with beta-blocking activity, Karveland may increase the effect of other concomitantly taken antihypertensive drugs (for example, alpha1-blockers) or drugs that have a hypotensive effect as a side effect. Means for general anesthesia. Careful monitoring of vital signs during general anesthesia should be carried out due to the possibility of a synergistic negative inotropic effect of Carvedilol and general anesthesia agents. Non-steroidal anti-inflammatory drugs (NSAIDs). The combined use of NSAIDs and beta-blockers can lead to an increase in blood pressure and a decrease in blood pressure control. Vasodilators (beta-adrenergic agonists). Since non-cardioselective beta-blockers interfere with the bronchodilator effect of bronchodilators, which are beta-adrenergic stimulants, careful monitoring of patients receiving these drugs is necessary. Contraindications Hypersensitivity to Carveland or any component of the drug, acute heart failure, decompensated heart failure (class IV NYHA), requiring intravenous administration of drugs, atrioventricular block II and III degree, severe bradycardia less than 50 beats / min, sick sinus syndrome (incl. h. sinotrial blockade), severe arterial hypotension (systolic blood pressure less than 85 mm Hg. Art.), cardiogenic shock, chronic lung disease with a bronchospastic component, bronchial asthma, clinically pronounced liver damage, pregnancy, lactation, age up to 18 years. Composition Active ingredient: carvedilol – 6.25 mg, 12.5 mg or 25 mg. Excipients: lactose monohydrate, sucrose, povidone K-30, crospovidone, anhydrous colloidal silicon dioxide, magnesium stearate, iron oxide (yellow) E 172 (dosages 12.5 mg and 25 mg), iron oxide (red) E 172 (dosage 25 mg). Overdose Symptoms: marked decrease in blood pressure, bradycardia, heart failure, cardiogenic shock, cardiac arrest; possible respiratory failure, bronchospasm, vomiting, confusion and generalized convulsions. Treatment: in addition to general measures, it is necessary to monitor and correct vital signs, if necessary, in the intensive care unit. You can use the following measures: a) put the patient on his back b) with severe bradycardia – atropine 0.5-2 mg intravenously; c) to maintain cardiovascular activity – glucagon 1-10 mg intravenously by stream, then 2-5 mg per hour as a long-term infusion; d) sympathomimetics (dobutamine, isoprenaline, orciprenaline or adrenaline) in various doses, depending on body weight and therapeutic efficacy. If it is necessary to administer drugs with a positive inotropic effect, phosphodiesterase inhibitors are prescribed. If arterial hypotension dominates in the clinical picture of an overdose, norepinephrine is administered; it is prescribed under conditions of continuous monitoring of blood circulation parameters. With treatment-resistant bradycardia, the use of an artificial pacemaker is indicated. With bronchospasm, beta-adrenergic agonists are administered in the form of an aerosol (if ineffective, intravenously) or aminophylline intravenously. For convulsions, diazepam or clonazepam is slowly injected intravenously. Since severe overdose with symptoms of shock may prolong the half-life of carveland and remove the drug from the depot, it is necessary to continue maintenance therapy for a sufficiently 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. Side effects Central nervous system: dizziness, headaches and weakness, asthenia (including fatigue), especially at the beginning of treatment, rarely – depression, sleep disturbances, paresthesia. Cardiovascular system: bradycardia, orthostatic hypotension, postural hypotension, pronounced decrease in blood pressure, edema (including generalized, peripheral, depending on body position, perineal edema, edema of the lower extremities, hypervolemia, fluid retention), rarely – fainting (in the beginning of treatment), syncopal conditions (including presyncopal), atrioventricular blockade and heart failure during the period of increasing the dose, peripheral circulatory disorders (cold extremities, exacerbation of the “intermittent” claudication syndrome and Raynaud’s syndrome),. Respiratory organs: bronchospasm and shortness of breath in predisposed patients, rarely – nasal congestion. Gastrointestinal: dyspeptic disorders (including nausea, abdominal pain, diarrhea, vomiting) rarely – constipation, changes in liver transaminase activity. Hematopoietic system: rarely: thrombocytopenia. Individual cases of leukopenia. Metabolic disorders: weight gain hypercholesterolemia; in patients with pre-existing diabetes mellitus – hyperglycemia or hypoglycemia, decompensation of carbohydrate metabolism. Skin: skin reactions (allergic rash, dermatitis, urticaria and itching). Urinary system: rarely – renal failure and impaired renal function in patients with diffuse vasculitis and / or impaired renal function, dysuria. Organs of vision: blurred vision, decreased lacrimation. Other: pain in the limbs, dry mouth, impotence. Storage conditionsKeep in a place protected from light at a temperature not exceeding 25°C. Keep out of the reach of children. Buy Karveland tablets 12.5 mg No. 10×3 Price for Karveland tablets 12.5 mg No. 10×3