Carvedilol, pills 25mg, 30pcs

Composition

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

Pharmacological action

Carvedilol has a combined non-selective β1 -, β2– and_α1-adrenoblocking effect. The drug does not have its own sympathomimetic activity, it 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 by blocking the beta-adrenergic receptors of the kidneys, causing a decrease in plasma renin activity. By blocking alpha-adrenergic receptors, the drug can cause peripheral vascular dilation, thereby reducing systemic vascular resistance. The combination of beta-adrenergic blockade and vasodilation has the following effects: in patients with arterial hypertension – a decrease in blood pressure; in patients with CHD-anti-ischemic and anti-anginal effects; in patients with left ventricular dysfunction and circulatory insufficiency – a favorable effect on hemodynamic parameters, increases the ejection fraction of the left ventricle and reduces its size.

Indications

• arterial hypertension (in monotherapy and in combination with diuretics);
• chronic heart failure (in combination therapy);
• IHD: stable angina pectoris.

Contraindications

• acute and decompensated chronic heart failure, requiring I/V use of inotropic agents;
• severe hepatic impairment;
• AV-block II-III degree;
• bradycardia (less than 50 beats/min);
• the syndrome of weakness of the sinus node;
• hypotension (systolic blood pressure less than 85 mm Hg. calendar);
• cardiogenic shock;
• bronchial asthma;
• chronic obstructive pulmonary disease;
• age to 18 years (efficacy and safety not established);
• hypersensitivity to carvedilol or other components of the drug.

With caution:  Bronchospastic syndrome, chronic bronchitis, emphysema of the lungs, Prinzmetal angina, thyrotoxicosis, occlusive diseases of peripheral vessels, pheochromocytoma, psoriasis, renal failure, AV block I degree, extensive surgery 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 (more often at the beginning of treatment), increased fatigue, depression, sleep disorders, paresthesia.

From the cardiovascular system:  bradycardia, orthostatic hypotension, AV block II – III st., rarely-violation of peripheral blood circulation, progression of heart failure (in the period of increased doses), edema of the lower extremities, angina pectoris, a pronounced 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.

From the side of metabolism:  increase in body weight, violation of carbohydrate metabolism.

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

Respiratory system disorders:  dyspnea and bronchospasm (in predisposed patients).

Other services:  visual impairment, decreased tear production, flu – like syndrome, sneezing, myalgia, arthralgia, pain in the extremities, intermittent claudication; rarely-impaired urination, impaired kidney function.

Interaction

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

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

With simultaneous use of carvedilol and digoxin, the concentration of the latter increases and the time of atrioventricular conduction may increase.

Carvedilol can potentiate the effects of insulin and oral hypoglycemic agents, while the symptoms of hypoglycemia (especially tachycardia) can be masked, so regular monitoring of blood sugar levels is recommended in diabetic patients.

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 hypotension and severe bradycardia.

Concomitant use of cyclosporine increases the concentration of the latter (correction of the daily dose of cyclosporine is recommended).

Concomitant use of clonidine may potentiate the antihypertensive and heart rate-reducing effects of carvedilol.

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

How to take, course of use and dosage

Inside, regardless of food intake.

To ensure the following dosage regimen, it is possible to use Carvedilol in the dosage form of a 6.25 mg tablet.

Arterial hypertension

The initial dose is 6.25-12.5 mg 1 time / day in the first two days of treatment. Then – 25 mg 1 time/day. If the antihypertensive effect is insufficient, the dose can be increased 2-fold after 2 weeks of therapy. The maximum recommended dose of the drug is 50 mg 1 time/day (possibly divided into 2 doses).

Coronary heart disease

The initial dose is 12.5 mg twice daily for the first two days of treatment. Then-25 mg 2 times/day. If the antianginal effect is insufficient, the dose can be increased 2-fold after 2 weeks of therapy. The maximum recommended daily dose of the drug is 100 mg, divided into 2 doses.

Chronic heart failure

The dose is selected individually, under the careful supervision of a doctor. The recommended starting dose is 3.125 mg twice daily for 2 weeks. With good tolerability, the dose is increased at intervals of at least 2 weeks to 6.25 mg 2 times/day, then to 12.5 mg 2 times/day, then to 25 mg 2 times/day. The dose should be increased to the maximum, which is well tolerated by patients. In patients with a body weight of less than 85 kg, the target dose is 50 mg / day; in patients with a body weight of more than 85 kg, the target dose is 75-100 mg/day.

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 disorders, confusion, and conduction disorders are possible.

Treatment:  it is necessary to monitor and correct vital signs, if necessary – in the intensive care unit. Treatment is symptomatic. Intravenous use of m-holinoblokatorov (atropine), adrenomimetics (epinephrine, norepinephrine) is advisable.

Special instructions

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

At the beginning of carvedilol therapy or when increasing the dose of the drug, patients, especially the elderly, may experience an excessive decrease in blood pressure, mainly when getting up. It is necessary to adjust the dose of the drug. In patients with chronic heart failure, when selecting the dose, it is possible to increase the symptoms of heart failure, the appearance of edema. At the same time, the dose of carvedilol should not be increased, it is recommended to prescribe large doses of diuretics until the patient’s condition stabilizes.

It is recommended to constantly monitor the electrocardiogram and blood pressure while prescribing carvedilol and slow calcium channel blockers, phenylalkylamine derivatives (verapamil) and benzodiazepine (diltiazem), as well as Class I antiarrhythmics.

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

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

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 using ethanol during treatment.

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

Patients who wear contact lenses should be aware that the drug may cause a decrease in lacrimation.

Influence on the ability to drive motor vehicles and manage mechanisms

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 related to the need for high concentration of attention and rapid psychomotor reactions.

Storage conditions

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

Shelf life

2 years

Active ingredient

Carvedilol

Conditions of release from pharmacies

By prescription

Dosage form

tablets