Vedicardol 6.25 mg №30

Clinico-pharmacological group

Cardiology

Pharmacotherapeutic group

alpha and beta blocker

Tradename

Vedicardol

International non-proprietary name

carvedilol

Dosage Form

pills

Composition

One pill contains: The active substance is Carvedilol : 6.25 mg, 12.5 mg, 25.0 mg. Excipients: milk sugar (lactose), potato starch, low molecular weight polyvinylpyrrolidone (povidone), microcrystalline cellulose, Calcium stearate (calcium stearate), talc.

Pharmacological properties Pharmacodynamics

Carvedilol has a combined non-selective beta-1-, beta-2- and alpha-1- blocking action. The drug does not have its own sympathomimetic activity, has membrane stabilizing properties. Due to the blockade of beta-adrenoreceptors of the heart, blood pressure, cardiac output and heart rate may decrease. Carvedilol inhibits the renin-angiotensin-aldosterone system by blocking the beta-adrenergic receptors of the kidneys, causing a decrease in plasma renin activity. By blocking alpha-adrenoreceptors, the drug can cause expansion of peripheral vessels, thereby reducing systemic vascular resistance. The combination of blockade of beta-adrenergic receptors and vasodilation has the following effects: in patients with arterial hypertension - lowering blood pressure; in patients with ischemic heart disease, anti-ischemic and antianginal effects; in patients with left ventricular dysfunction and circulatory failure - a positive effect on hemodynamic parameters, increases the ejection fraction of the left ventricle and reduces its size.

Pharmacokinetics

Carvedilol is rapidly absorbed from the gastrointestinal tract. It has high lipophilicity. The maximum concentration in the blood is achieved in 1-1.5 hours. The half-life is 6-10 hours. Associated with plasma proteins at 95-99%. Bioavailability of the drug is 24-28%. Food intake does not affect bioavailability.Metabolized in the liver with the formation of a number of active metabolites - 60-75% of the adsorbed drug is metabolized during the first "passage" through the liver. Metabolites have a pronounced antioxidant and adrenergic blocking effect. Removal of the drug from the body occurs through the gastrointestinal tract. In case of impaired renal function, the pharmacokinetic parameters of carvedilol do not change significantly. In patients with impaired liver function, the systemic bioavailability of carvedilol is increased by reducing metabolism during the first “passage” through the liver. With serious violations of the liver, carvedilol is contraindicated. Carvedilol penetrates the placental barrier, is excreted in breast milk.

Indications for use - Arterial hypertension (in monotherapy and combination with diuretics);
- Chronic heart failure (as part of combination therapy);
- Ischemic heart disease: stable angina.

Carefully AV blockade I extent, diabetes mellitus, hypoglycemia, hyperthyroidism, occlusive peripheral vascular disease, Prinzmetal angina, pheochromocytoma (with simultaneous application of alpha-blockers), depression, myasthenia gravis, psoriasis, chronic obstructive pulmonary disease, bronchospasm history, the simultaneous application of inhibitors of monoamine oxidase (MAO), renal failure, extensive surgical interventions and general anesthesia, aggravated allergic history (increased sensitivity to allergens and the severity of Anaphylactic reactions, reduced response to the introduction of epinephrine (adrenaline)), pregnancy.

Contraindications Hypersensitivity to carvedilol or other components of the drug, acute and chronic heart failure (at the stage of decompensation), severe liver failure, atrioventricular block II-III stage, severe bradycardia (less than 50 beats / min), sick sinus syndrome, arterial hypotension ( systolic blood pressure less than 85 mmHg.), cardiogenic shock, chronic obstructive pulmonary disease, age up to 18 years (efficacy and safety have not been established).

Use during pregnancy Controlled studies of the use of carvedilol in pregnant women have not been conducted, therefore, prescribing this category of patients is possible only in cases where the benefit to the mother outweighs the potential risk to the fetus. Breastfeeding is not recommended during treatment with carvedilol.

Dosage and administration

Inside, regardless of the meal, squeezed enough liquid.

With hypertension the initial dose is 12.5 mg once a day during the first 2 days of treatment, then 25 mg once a day, with a possible gradual increase of the dose with an interval of at least 2 weeks. With insufficient severity of the antihypertensive effect after 2 weeks of therapy, the dose may be increased. The maximum recommended daily dose of the drug is 50 mg 1 time per day (possibly divided into 2 doses).

Coronary heart disease: prevention of attacks of stable angina

The initial dose is 12.5 mg 2 times a day for the first 2 days of therapy, then 25 mg 2 times a day. With insufficient severity of antianginal effect after 2 weeks of therapy, the dose may be increased. The maximum recommended daily dose of the drug is 100 mg per day, divided into 2 doses.

In chronic heart failure the dose is selected individually (against the background of selected therapy with cardiac glycosides, diuretics, and angiotensin-converting enzyme (ACE) inhibitors), under close medical supervision. It is necessary to monitor the patient's condition within 2-3 hours after the first dose or after the first increased dose. The recommended initial dose is 3.125 mg (it is possible to use carvedilol in a different dosage of &№189; pills of 6.25 mg with a risk) 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 to 12.5 mg 2 times a day, then to 25 mg 2 times a day. The dose should be increased to the maximum, which is well tolerated by patients. With a body weight less than 85 kg - the maximum dose is 25 mg 2 times a day, with a weight of more than 85 kg - 50 mg 2 times a day. The maximum dose of the drug in patients with severe chronic heart failure is 25 mg 2 times a day, regardless of their body weight.

Before each increase in dose, the physician should examine the patient to identify an increase in symptoms of chronic heart failure or vasodilation.When a transient increase in symptoms of chronic heart failure or fluid retention in the body, you should increase the dose of diuretics or temporarily cancel Vedicardol&№174;. Symptoms of vasodilation can be eliminated by reducing the dose of diuretics. If the symptoms of chronic heart failure persist, you can reduce the dose of an ACE inhibitor (if the patient is taking it), and then, if necessary, a dose of Vedicardol&№174;. Do not increase the dose of the drug Vedicardol^®until the symptoms of chronic heart failure or hypotension stabilize.

Patients with chronic heart failure to prevent orthostatic hypotension are advised to take the drug with meals.

When skipping a dose, the drug should be taken as soon as possible, however, if the time of the next dose is coming, then take it only, without doubling. The abolition of the drug must be made gradually over 1-2 weeks.

If treatment is interrupted for more than 2 weeks, then its renewal begins with a dose of 3.125 mg (carvedilol may be used in another dosage of &№189; pills of 6.25 mg with a risk) 2 times a day, with a subsequent increase in dose.

In patients with moderate renal failure, dose adjustment of the drug Vedicardol^® not required.

Elderly patients dose adjustment of the drug Vedicardol^® not required.

Vedicardol^® contraindicated in patients with clinically significant impairment of liver function (see section "Contraindications").

Side effect

Classification of the incidence of side effects: very often> 1/10; often> 1/100, <1/10; infrequently> 1/1000, <1/100; rarely> 1/10000, <1/1000; very rarely <1/10000, including individual messages.

The frequency of adverse events does not depend on the dose, with the exception of dizziness, visual disturbances and bradycardia.

In patients with chronic heart failure

From the side of the central nervous system: very often - dizziness, headache (especially at the beginning of treatment or when changing doses), asthenia (including increased fatigue), depression.

Since the cardiovascular system: often - bradycardia, postural hypotension, marked reduction in blood pressure, peripheral edema (including generalized, edema of the perineum, lower extremities, fluid retention); infrequently - exacerbation of chronic heart failure (in the period of increasing doses), syncopal states (including presynopal), AV block II-III degree.

From the digestive system: often - nausea, diarrhea, vomiting.

Metabolism: often - weight gain, impaired glycemic control.

From the side of blood-forming organs: rarely thrombocytopenia; very rarely - leukopenia.

From the urinary system: rarely - renal failure and impaired renal function in patients with diffuse vasculitis and / or impaired renal function, severe impairment of renal function.

Laboratory values: often - hypercholesterolemia, hyper- or hypoglycemia in patients with diabetes mellitus.

Other: often - visual impairment.

In patients with arterial hypertension and coronary heart disease

The nature of the side effects of the cardiovascular system in the treatment of hypertension and coronary heart disease is similar to that in chronic heart failure, but their frequency is less.

From the side of the central nervous system: often - dizziness, headache, general weakness (especially at the beginning of treatment or when changing doses); infrequently - mood lability, sleep disturbances, paresthesias.

Since the cardiovascular system: often - postural hypotension, bradycardia; infrequently - development or exacerbation of chronic heart failure, peripheral edema, angina (chest pain), AV block II-III degree, syncopal states (especially at the beginning of therapy), peripheral circulatory disorders (cooling of limbs, aggravation of "intermittent claudication" and Raynaud's syndrome).

From the digestive system: often - dyspeptic disorders (including nausea, abdominal pain, diarrhea); infrequently - constipation, vomiting.

On the part of the respiratory system: often - shortness of breath and bronchospasm (in predisposed patients); rarely nasal congestion.

From the skin: infrequently - pruritus, rash, dermatitis and urticaria.

Metabolism: often - manifestation of latent flowing diabetes, decompensation of existing diabetes mellitus or inhibition of the intrasular system.

From the side of blood-forming organs: very rarely - thrombocytopenia, leukopenia.

From the urinary system: rarely, urinary disturbance, very rarely, urinary incontinence in women, reversible after discontinuation of the drug.

From the genitourinary system: infrequently - a decrease in potency.

Laboratory values: very rarely - increased activity of liver transaminases.

Other: often - pain in the limbs, reduction of tearing and eye irritation; infrequently - visual impairment; rarely, dryness of the oral mucosa; very rarely - flu-like syndrome, sneezing, exacerbation of the course of psoriasis, alopecia.

Storage conditions List B. In a dry, dark place, at a temperature not exceeding 25 ° C. Keep out of the reach of children.

Shelf life 2 years. Do not use after the date indicated on the package.