Carvedilol, tablets 25 mg 30 pcs

Carvedilol has a combined non-selective β ₁ -, β₂– and α₁-adrenoblocking effect. The drug has no sympathomimetic activity of its own and has membrane stabilizing properties. Due to the blockade of the β-adrenoreceptors of the heart, BP, cardiac output and heart rate may decrease. Carvedilol suppresses the renin-angiotensin-aldosterone system by blockade of renal β-adrenoceptors, causing a decrease in plasma renin activity. By blocking α-adrenoreceptors, the drug may cause dilation of peripheral vessels, thereby reducing systemic vascular resistance. The combination of β-adrenoreceptor blockade and vasodilation has the following effects: in patients with arterial hypertension – BP reduction; in patients with CHD – anti-ischemic and antianginal effects; in patients with left ventricular dysfunction and circulatory failure – favorable effects on hemodynamic parameters, increases left ventricular ejection fraction and reduces its size.

Indications

arterial hypertension (in monotherapy and combination with diuretics);
chonic heart failure (as part of combination therapy);
IHD: stable angina.

Pharmacological effect

Carvedilol has a combined non-selective β 1 -, β2- and α1-adrenergic blocking effect. The drug does not have its own sympathomimetic activity, but has membrane-stabilizing properties. Due to the blockade of beta-adrenergic receptors of the heart, blood pressure, cardiac output and heart rate can decrease. Carvedilol suppresses the renin-angiotensin-aldosterone system through blockade of renal β-adrenergic receptors, causing a decrease in plasma renin activity. By blocking α-adrenergic receptors, the drug can cause peripheral vasodilation, thereby reducing systemic vascular resistance. The combination of β-adrenergic receptor blockade and vasodilation has the following effects: in patients with arterial hypertension – a decrease in blood pressure; in patients with coronary artery disease – anti-ischemic and antianginal effects; in patients with left ventricular dysfunction and circulatory failure – has a beneficial effect on hemodynamic parameters, increases the ejection fraction of the left ventricle and reduces its size.

Special instructions

Therapy should be carried out over a long period of time and should not be stopped abruptly, especially in patients with coronary heart disease, as this can lead to a worsening of the underlying disease. If necessary, the dose reduction should be gradual over 1-2 weeks.

At the beginning of therapy with carvedilol or when the dose of the drug is increased in patients, especially elderly patients, an excessive decrease in blood pressure may be observed, mainly when standing up. A dose adjustment of the drug is necessary. In patients with chronic heart failure, when selecting a dose, an increase in symptoms of heart failure and the appearance of edema is possible. In this case, the dose of carvedilol should not be increased; it is recommended to prescribe large doses of diuretics until the patient’s condition is stabilized.

Continuous monitoring of the electrocardiogram and blood pressure is recommended while prescribing carvedilol and slow calcium channel blockers, phenylalkylamine derivatives (verapamil) and benzodiazepine (diltiazem), as well as with class I antiarrhythmic drugs.

It is recommended to monitor renal function in patients with chronic renal failure, arterial hypotension and chronic heart failure.

In case of surgery using general anesthesia, the anesthesiologist should be warned about previous therapy with carvedilol.

Carvedilol does not affect the concentration of glucose in the blood and does not cause changes in the glucose tolerance test in patients with non-insulin-dependent diabetes mellitus.

Avoid drinking ethanol during treatment.

Patients with pheochromocytoma should be prescribed alpha-blockers before starting therapy.

Patients wearing contact lenses should be aware that the drug may cause a decrease in tear production.

Impact on the ability to drive vehicles and operate machinery

It is not recommended to drive a car at the beginning of therapy and when increasing the dose of carvedilol. You should refrain from other activities that require high concentration of attention and rapid psychomotor reactions.

Active ingredient

Carvedilol

Composition

1 tab. carvedilol 25 mg.
Excipients: microcrystalline cellulose, lactose (milk sugar), crospovidone (plasdon XL10), sodium stearyl fumarate.

Contraindications

acute and decompensated chronic heart failure, requiring intravenous administration of inotropic agents;
severe liver failure;
AV blockade II-III stage;
severe bradycardia (less than 50 beats/min);
sick sinus syndrome;
arterial hypotension (systolic blood pressure less than 85 mm Hg);
cardiogenic shock;
bronchial asthma;
chronic obstructive pulmonary disease;
age under 18 years (efficacy and safety have not been established);
hypersensitivity to carvedilol or other components of the drug.

With caution: bronchospastic syndrome, chronic bronchitis, pulmonary emphysema, Prinzmetal’s angina, thyrotoxicosis, occlusive diseases of peripheral vessels, pheochromocytoma, psoriasis, renal failure, AV block of the first degree, extensive surgical interventions and general anesthesia, diabetes mellitus, hypoglycemia, depression, myasthenia gravis.

Side Effects

From the central nervous system: dizziness, headache (usually not severe at the beginning of treatment), loss of consciousness, myasthenia gravis (usually at the beginning of treatment), increased fatigue, depression, sleep disturbance, paresthesia.

From the cardiovascular system: bradycardia, orthostatic hypotension, AV blockade II – III degrees, rarely – peripheral circulatory disorders, progression of heart failure (during the period of increase
doses), edema of the lower extremities, angina pectoris, marked decrease in blood pressure.

From the digestive system: dry mouth, nausea, diarrhea or constipation, vomiting, abdominal pain, loss of appetite, increased activity of liver transaminases.

From the hematopoietic system: rarely – thrombocytopenia, leukopenia.

Metabolism: weight gain, carbohydrate metabolism disorders.

Allergic reactions: allergic skin reactions, exacerbation of psoriasis, nasal congestion.

From the respiratory system: shortness of breath and bronchospasm (in predisposed patients).

Other: blurred vision, decreased lacrimation, flu-like syndrome, sneezing, myalgia, arthralgia, pain in the limbs, intermittent claudication; rarely – urinary disturbances, renal dysfunction.

Interaction

Carvedilol may potentiate the effect of other concomitantly taken antihypertensive drugs or drugs that have a hypotensive effect (nitrates).

When carvedilol and diltiazem are used together, cardiac conduction disturbances and hemodynamic disturbances may develop.

When carvedilol and digoxin are taken simultaneously, the concentration of the latter increases and the atrioventricular conduction time may increase.

Carvedilol may potentiate the effect of insulin and oral hypoglycemic agents, and the symptoms of hypoglycemia (especially tachycardia) may be masked; therefore, regular monitoring of blood sugar levels is recommended in patients with diabetes mellitus.

Inhibitors of microsomal oxidation (cimetidine) enhance, and inducers (phenobarbital, rifampicin) weaken the hypotensive effect of carvedilol.

Drugs that reduce the content of catecholamines (reserpine, monoamine oxidase inhibitors) increase the risk of developing arterial hypotension and severe bradycardia.

With simultaneous use of cyclosporine, the concentration of the latter increases (adjustment of the daily dose of cyclosporine is recommended).

Concomitant administration of clonidine may potentiate the antihypertensive and heart rate-lowering effects of carvedilol.

General anesthetics enhance the negative inotropic and hypotensive effect of carvedilol.

Overdose

Symptoms: decreased blood pressure (accompanied by dizziness or fainting), bradycardia. Shortness of breath may occur due to bronchospasm and vomiting. In severe cases, cardiogenic shock, respiratory failure, confusion, and conduction disturbances are possible.

Treatment: it is necessary to monitor and correct vital signs, if necessary, in the intensive care unit. Treatment is symptomatic. It is advisable to use intravenously m-anticholinergic agents (atropine), adrenergic agonists (epinephrine, norepinephrine).

Storage conditions

List B. Store in a dry place, protected from light, at a temperature not exceeding 25°C. Keep out of the reach of children.

Shelf life

2 years

Manufacturer

Ozon, Russia