Vedicardol tabs 12.5mg #30

Instruction for use for Vedicardol

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Vedicardol is an alpha and beta blocker.

Release form and composition

Dosage form - tablets: flat-cylindrical, almost white or white, marbling is allowed, with a chamfer (in a cardboard box 3 cell contour packs of 10 tablets and instructions for using Vedicardol).
Composition of 1 tablet:
    active substance: carvedilol - 6.25; 12.5 or 25 mg;
    auxiliary components: crospovidone, calcium stearate, lactose monohydrate, talc, microcrystalline cellulose.

Pharmacodynamics

The active ingredient in the drug - carvedilol - is an alpha and beta blocker. Blocks α1-, β1- and β2-adrenergic receptors. It has antiarrhythmic, antianginal and vasodilating effects.
Carvedilol is a racemic mixture of R (+) and S (-) - stereoisomers with the same alpha-adrenergic blocking properties.
The beta-adrenergic blocking activity of Vedicardol is non-selective and is due to the levorotatory S (-) stereoisomer.
The vasodilating effect of carvedilol is mainly due to the blockade of α1-adrenergic receptors. Due to vasodilation, the total peripheral vascular resistance decreases.
Carvedilol has membrane-stabilizing properties, but does not show its own sympathomimetic activity.
Vasodilation in combination with a blockade of β-adrenergic receptors leads to a decrease in renal vascular resistance in kidney disease and arterial hypertension. In this case, there is no significant effect on the glomerular filtration rate, renal plasma flow and electrolyte excretion. Peripheral blood flow persists, therefore, patients rarely develop cold feet and hands, often occurring while taking beta-blockers.
Carvedilol lowers heart rate slightly. With ischemic heart disease (CHD), it has an antianginal effect. Reduces pre- and afterload on the heart. Does not significantly affect lipid metabolism, plasma content of magnesium, sodium and potassium ions.
In the case of functional impairment of the left ventricle and / or heart failure, the substance has a positive effect on hemodynamic parameters, improves the ejection fraction and the size of the left ventricle.
Vedicardol improves left ventricular function, relieves symptoms, reduces hospital admissions and mortality rates in patients with chronic heart failure, both ischemic and non-ischemic.
The effects of carvedilol are dose-dependent.

Pharmacokinetics

When administered orally, carvedilol is rapidly and almost completely absorbed from the gastrointestinal tract. The maximum plasma concentration (Cmax) of 5–99 μg / ml reaches after 1–1.5 hours.
The absolute bioavailability is 25–35%: for the S (-) - stereoisomer ~ 15%, for the R (+) - stereoisomer ~ 31%.
The degree of binding to plasma proteins is 98–99%, mainly due to the R (+) - stereoisomer that binds to albumin. The volume of distribution is approximately 2 l / kg.
Carvedilol is characterized by a first pass effect through the liver. It is metabolized with the participation of cytochrome P450 isoenzymes, such as CYP1A2, CYP2C19, CYP2C9, CYP2E1, CYP2D6 and CYP3A4. As a result, by demethylation and hydroxylation, three active metabolites are formed, which have a pronounced beta-adrenergic blocking effect. The main metabolite is 4'-hydroxyphenyl-carvedilol, which is 13 times more active than carvedilol, despite the fact that its plasma concentration is 10% of that of carvedilol in plasma.
Plasma clearance - 500-700 ml / min. It is excreted mainly with bile through the intestines. Up to 2% is excreted in the kidneys. The half-life is 6-10 hours.
Carvedilol crosses the placental barrier and into breast milk.
Pharmacokinetics in special groups:
    elderly and senile age: significant differences in pharmacokinetic parameters are not observed, and the tolerance of Vedicardol does not change;
    functional impairment of the kidneys: carvedilol does not violate the intensity of renal blood flow, does not change the glomerular filtration rate. With arterial hypertension and concomitant impairment of renal function, the pharmacokinetic parameters of the drug do not change. In patients with renal insufficiency, the renal excretion of unchanged carvedilol decreases, but the changes in pharmacokinetics are not significant. Carvedilol is widely used for the treatment of renovascular arterial hypertension, including in patients with chronic renal failure, patients on hemodialysis or undergoing kidney transplantation. Vedicardol promotes a gradual decrease in blood pressure (BP) in the periods between dialysis and on the days of dialysis, while the severity of the antihypertensive effect is comparable to that in healthy volunteers. Carvedilol is not excreted by dialysis (probably due to its high binding to plasma proteins);
    functional disorder of the liver: the bioavailability of the drug increases significantly (up to 80%), therefore the use of Vedicardol is contraindicated;
    heart failure: the clearance of R (+) and S (-) - stereoisomers of carvedilol is significantly reduced, but their pharmacokinetics does not change significantly;
    diabetes mellitus: in patients with arterial hypertension and type 2 diabetes mellitus, carvedilol does not affect blood glucose (both after meals and on an empty stomach), the level of glycated hemoglobin and the therapeutic efficacy of the hypoglycemic agent used. Some studies have shown that Vedicardol does not decrease glucose tolerance. In patients with arterial hypertension and insulin resistance (syndrome X), but without diabetes mellitus, carvedilol increases insulin sensitivity. Similar results were obtained in a study of patients with arterial hypertension and type 2 diabetes mellitus.

Indications for use

    arterial hypertension (as a monopreparation or in combination with diuretics);
    chronic heart failure (as part of complex therapy);
    ischemic heart disease - to prevent attacks of stable angina pectoris.

Contraindications

Absolute:
    metabolic acidosis;
    terminal stage of peripheral vascular occlusive disease;
    Prinzmetal's angina;
    atrioventricular (AV) blockade of the II-III degree (except for patients with an artificial pacemaker);
    chronic heart failure in the stage of decompensation, requiring intravenous administration of inotropic drugs;
    acute heart failure;
    cardiogenic shock;
    sick sinus syndrome;
    bradycardia (less than 60 beats / min);
    severe arterial hypotension (systolic blood pressure less than 85 mm Hg. Art.);
    bronchial asthma;
    severe form of chronic obstructive pulmonary disease;
    pheochromocytoma (without the simultaneous use of alpha-blockers);
    liver failure;
    lactose intolerance, lactase deficiency, glucose / galactose malabsorption syndrome;
    age up to 18 years;
    period of breastfeeding;
    concomitant use of diltiazem or verapamil;
    hypersensitivity to any component of the drug.
Relative (Vedicardol is used with caution only if the benefits are higher than the risks):
    renal failure;
    a history of bronchospasm;
    chronic obstructive pulmonary disease;
    peripheral vascular occlusive disease;
    AV block I degree;
    myasthenia gravis;
    pheochromocytoma (with the simultaneous use of alpha-blockers);
    thyrotoxicosis;
    hypoglycemia;
    diabetes;
    psoriasis;
    depression;
    major surgery or general anesthesia;
    period of pregnancy;
    simultaneous use of MAO (monoamine oxidase) inhibitors.

Instructions for use: method and dosage

The tablets are taken orally with the required amount of water. Meal time does not matter.
With arterial hypertension, treatment begins with a daily dose of 12.5 mg in 1 dose. After 2 days, it is increased to 25 mg once a day. If the effect is insufficient, the dose is continued to be gradually increased at minimum intervals of 2 weeks. The maximum permissible daily dose is 50 mg per day for 1 or 2 doses.
With angina pectoris and coronary heart disease, the recommended dose in the first 2 days is 12.5 mg 2 times a day, then 25 mg 2 times a day. In cases of insufficient antianginal effect, an increase in the daily dose is possible after 2 weeks. The highest daily dose for this category of patients is 100 mg in 2 divided doses.
In chronic heart failure, the dose is selected by the doctor individually for each patient. Vedicardol is prescribed in addition to cardiac glycosides, diuretics, and angiotensin-converting enzyme (ACE) inhibitors. Within 2-3 hours after the first dose and the first dose increase, the patient requires careful medical supervision. It is recommended to start treatment with a dose of 3.125 mg (½ Vedicardol 6.25 mg tablet) 2 times a day. In order to avoid the development of orthostatic hypotension, it is advisable to take the drug with meals. In case of insufficient therapeutic effect, but provided that the therapy is well tolerated, at intervals of at least 2 weeks, a single dose can be increased: first, Vedicardol 6.25 mg, then 12.5 mg, then up to 25 mg while maintaining the frequency of administration 2 times per day. The maximum recommended doses: patients weighing <85 kg - 25 mg 2 times a day; patients weighing> 85 mg - 50 mg 2 times a day.
In severe chronic heart failure, the highest dose is 25 mg 2 times a day, regardless of body weight. Before each dose increase, the patient is examined for the absence of symptoms of an increase in chronic heart failure or the development of vasodilation. In case of fluid retention or a transient increase in chronic heart failure, the dose of the diuretic is increased or Vedicardol is temporarily canceled. With symptoms of vasodilation, reduce the dose of the diuretic. If signs of chronic heart failure persist, reduce the dose of the ACE inhibitor (in patients who receive it), then, if necessary, reduce the dose of Vedicardol. Do not increase the dose of carvedilol until the symptoms of arterial hypotension or chronic heart failure stabilize.
If the next dose is missed, the pill should be taken as soon as the patient remembers it, only if the time for the next dose is not approaching. Do not double the dose.
The end of therapy is carried out gradually - within 1–2 weeks.
If the use of Vedicardol is interrupted for more than 2 weeks, you should resume taking the drug with the minimum dose and gradually increase it.
For elderly patients and patients with moderate renal insufficiency, the therapy regimen is not adjusted.

Side effects

Against the background of drug therapy, the following side effects may occur (according to the frequency of development, they are classified as follows: very often -> 1/10, often - from> 1/100 to <1/10, infrequently - from> 1/1000 to <1/100 , rarely - from> 1/10 000 to <1/1000, very rarely - <1/10 000, including individual messages):
    laboratory parameters: often - hypercholesterolemia, hyperglycemia, hypoglycemia;
    on the part of the cardiovascular system: very often - orthostatic hypotension; often - AV block II – III degree, bradycardia; rarely - a pronounced decrease in blood pressure, angina pectoris, peripheral edema (including generalized, edema of the lower extremities / perineum), presyncopal and syncope states, exacerbation of the course of chronic heart failure (in the period of increasing doses), peripheral circulatory disorders manifested by cold extremities, exacerbation Raynaud's syndrome and intermittent claudication syndrome;
    from the central and peripheral nervous system: often - headache (especially at the beginning of taking Vedicardol and when changing the dose), dizziness, weakness; rarely - asthenic conditions (including increased fatigue), sleep disturbances, mood lability, depression, paresthesia;
    from the side of metabolism: often - decompensation of already existing diabetes mellitus, suppression of the contrainsular system, manifestation of latent diabetes mellitus, increase in body weight;
    from the digestive system: often - diarrhea, abdominal pain, nausea; rarely - vomiting, constipation; very rarely - increased activity of hepatic transaminases;
    from the urinary system: rarely - urination disorder; very rarely - urinary incontinence in women (reversible after discontinuation of Vedicardol), severe renal dysfunction; in patients with impaired renal function and / or diffuse vasculitis - further deterioration of renal function, renal failure;
    from the respiratory system: rarely - shortness of breath, nasal congestion, bronchospasm (in predisposed patients);
    from the reproductive system: infrequently - decreased potency;
    on the part of the hematopoietic organs: rarely - thrombocytopenia; very rarely - leukopenia;
    on the part of the skin: infrequently - rash, skin itching, urticaria, dermatitis;
    on the part of the organ of vision: often - eye irritation, reduced tearing, visual impairment;
    others: rarely - dryness of the oral mucosa, sneezing; very rarely - pain in the limbs, exacerbation of the course of psoriasis, flu-like syndrome.

Overdose

An overdose of Vedicardol can manifest itself as an excessive decrease in blood pressure (accompanied by dizziness or fainting), severe bradycardia (<50 beats / min), bronchospasm, shortness of breath, vomiting. In severe cases, the following disorders are possible: confusion, respiratory failure, generalized convulsions, conduction disturbances, heart failure, cardiogenic shock, cardiac arrest.
After taking a dose significantly higher than the recommended one, the patient should undergo gastric lavage and take an adsorbent. Further, symptomatic treatment is carried out, which is accompanied by monitoring and maintaining the vital functions of the body. If required, the patient is admitted to the intensive care unit.
Recommended treatment for overdose depending on symptoms:
    the predominance of a pronounced decrease in blood pressure: the introduction of a sympathomimetic (epinephrine, norepinephrine, adrenaline, norepinephrine or dobutamine) is shown under continuous monitoring of blood circulation parameters;
    severe bradycardia: intravenous (intravenous) administration of an m-anticholinergic antagonist (for example, atropine at a dose of 0.5–2 mg) is recommended;
    treatment-resistant bradycardia: an artificial pacemaker may be needed;
    convulsions: diazepam is slowly administered intravenously;
    bronchospasm: requires the appointment of aminophylline in / in or beta-adrenomimetic in the form of an aerosol, if the aerosol form is ineffective, it is required for intravenous administration.
For patients with severe overdose accompanied by shock, maintenance therapy is carried out for a long time, since the half-life of carvedilol and the excretion of Vedicardol from the depot may increase.

Special instructions

The drug is used for a long time and is not canceled abruptly, especially during the treatment of coronary artery disease, since the patient's condition may worsen. If it is necessary to stop treatment, the dose of Vedicardol is gradually reduced over 1–2 weeks.
At the initial stage of therapy and with an increase in the dose of Vedicardol, especially in the elderly, an excessive decrease in blood pressure is possible, more often during standing up. In this case, dose adjustment is required.
During the period of dose selection in patients with chronic heart failure, an increase in symptoms of the disease and the appearance of peripheral edema are possible. In this case, further increase in the dose of Vedicardol is prohibited. An increase in the dose of diuretics is required until the hemodynamic parameters stabilize. Sometimes it is necessary to reduce the dose of carvedilol, in rare cases it is temporarily canceled. This does not interfere with further correct selection of the dose.
Sometimes, during therapy, bradycardia develops. If the heart rate decreases below 60 beats / min, reduce the dose of Vedicardol or cancel the drug.
Carvedilol is able to mask the symptoms of hypoglycemia, especially tachycardia, and reduce the symptoms of thyrotoxicosis, therefore, it should be used with caution in patients with endocrine disorders.
Beta-blockers can increase the symptoms of arterial insufficiency, which should be considered when treating patients with peripheral vascular disease, including Raynaud's syndrome.
In patients with coronary artery disease and diffuse peripheral vascular disease and / or renal failure, in patients with chronic heart failure and arterial hypotension (systolic blood pressure less than 100 mm Hg), a reversible deterioration of renal function is possible. In these cases, the dose of Vedicardol is selected in accordance with the functional state of the kidneys.
With the simultaneous use of phenylalkylamine derivatives (verapamil) or benzodiazepine (diltiazem), class I antiarrhythmics or slow calcium channel blockers, it is necessary to constantly monitor blood pressure and electrocardiogram.
Patients with pheochromocytoma can be prescribed Vedicardol only if alpha-blockers are used simultaneously.
If surgery is necessary using general anesthesia, the patient should inform the anesthesiologist about taking carvedilol.
Patients with chronic obstructive pulmonary disease, if they are not taking oral or inhaled beta2-adrenomimetics, Vedicardol should be prescribed only after a careful assessment of the benefits and risks. If there is a predisposition to the development of bronchospastic syndrome, the drug may cause shortness of breath. At the beginning of treatment and when the dose is increased, such patients should be under close medical supervision. If symptoms of bronchospasm appear, the dose should be reduced.
With caution, Vedicardol should be used to treat patients with a history of severe hypersensitivity reactions and patients undergoing a course of desensitization, since carvedilol can increase a person's sensitivity to allergens and, as a result, increase the severity of anaphylactic reactions.
Vedicardol is able to reduce the secretion of tear fluid, which should be taken into account by people wearing contact lenses.
During therapy, it is strongly recommended to refrain from drinking alcoholic beverages.

Influence on the ability to drive vehicles and complex mechanisms

At the beginning of taking Vedicardol and during the period of increasing its dose, patients should be careful when engaging in activities with potentially dangerous consequences, including driving a car.

Application during pregnancy and lactation

By decreasing placental blood flow, carvedilol can have a negative effect on the development of the embryo, cause hypoglycemia, bradycardia and arterial hypotension in the fetus, lead to premature birth or intrauterine fetal death. For this reason, Vedicardol is contraindicated during pregnancy, except in cases of urgent need, when the benefits for the woman are definitely higher than the possible risks.
Carvedilol passes into breast milk, so it is contraindicated to take Vedicardol during lactation, or breastfeeding should be stopped.

Childhood use

Vedicardol is not used in pediatrics, as there is no evidence of the safety and efficacy of its use in patients under the age of 18 years.

With impaired renal function

In renal failure, Vedicardol is used with caution.

For violations of liver function

The drug is contraindicated in severe liver dysfunction.

Use in the elderly

At the stage of selecting and increasing the dose in elderly patients, an excessive decrease in blood pressure is possible, especially when standing up. In this case, it is recommended to adjust the Vedicardol dose.

Drug interactions

Carvedilol has the following effect on concurrently used drugs:
    potentiates the action of other antihypertensive drugs and drugs with antihypertensive effects (for example, nitrates);
    increases the concentration of digoxin in the blood, which may lead to an increase in the AV conduction time;
    enhances the effect of insulin and oral hypoglycemic agents, including sulfonylurea derivatives, can mask the symptoms of hypoglycemia, especially tachycardia (requires intensive control of blood glucose levels);
    increases the content of cyclosporine in the blood (dose adjustment is required);
    prevents the bronchodilator effect of bronchodilators, which are β-adrenoreceptor agonists.
Potential effects of other drugs on carvedilol:
    non-steroidal anti-inflammatory drugs and inducers of microsomal oxidation (phenobarbital, rifampicin): reduce its antihypertensive effect;
    inhibitors of microsomal oxidation (cimetidine): enhance its hypotensive effect;
    ergotamine: enhances induced vasoconstriction;
    general anesthetics: potentiate its antihypertensive effect and inotropic effect;
    clonidine: it can increase its hypotensive and negative chronotropic effects (if it is necessary to stop the combination therapy, carvedilol should be canceled first, after a few days - clonidine, gradually reducing the dose);
    fluoxetine: inhibits its metabolism and causes the accumulation of carvedilol, which may increase the cardiodepressive effect (including the development of bradycardia), this effect persists even a few days after the discontinuation of fluoxetine;
    drugs that increase the content of catecholamines (for example, reserpine and MAO inhibitors): increase the risk of developing arterial hypotension and severe bradycardia;
    antiarrhythmics (especially class I) and blockers of slow calcium channels (such as verapamil and diltiazem): increase the likelihood of a violation of AV conduction, may contribute to the occurrence of severe arterial hypotension and heart failure (it is contraindicated to prescribe verapamil or diltiazem i / v simultaneously with carvedilol);
    amiodarone: reduces the clearance of the S (-) - stereoisomer of carvedilol in patients with heart failure, which is accompanied by the risk of increased beta-adrenergic blocking action.

Terms and conditions of storage

Store at a temperature not exceeding 25 ° C, protected from light, dry and out of reach of children.
The shelf life is 3 years.

Reviews about Vedicardol

There are practically no reviews of Vedicardol on specialized forums and sites. The drug contains carvedilol as an active ingredient, which is a part of many medicines. Patients assess it mainly positively: the drug is good at reducing high blood pressure, stabilizes the condition in coronary heart disease and chronic heart failure.

Terms of sell

You don't need a prescription to buy Vedicardol.