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

Active ingredient

Composition

How to take, the dosage

Overly, regardless of meals.

The dosage regimen below can be achieved by using Carvedilol in the dosage form of 6.25 mg tablets.

Arterial hypertension

The initial dose is 6.25-12.5 mg once daily for the first two days of treatment. Thereafter, 25 mg once daily. In case of insufficient antihypertensive effect after 2 weeks of therapy, the dose may be doubled. The maximum recommended dose is 50 mg once daily (possibly divided into two doses).

Ischemic heart disease

The starting dose is 12.5 mg 2 times daily for the first two days of therapy. Thereafter, 25 mg 2 times daily. In case of insufficient antianginal effect after 2 weeks of therapy, the dose may be doubled. The maximum recommended daily dose of the drug is 100 mg divided into two doses.

Chronic heart failure

The dose is adjusted individually under close medical supervision. The recommended starting dose is 3.125 mg 2 times daily for 2 weeks. If well tolerated, 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 dose that is well tolerated by the patient. In patients weighing less than 85 kg, the target dose is 50 mg/day; in patients weighing more than 85 kg, the target dose is 75-100 mg/day.

Interaction

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

In concomitant use of Carvedilol and diltiazem, cardiac conduction abnormalities and hemodynamic disorders may develop.

The concomitant use of carvedilol and digoxin increases the concentration of the latter and may prolong atrioventricular conduction time.

Carvedilol may potentiate the effects of insulin and oral hypoglycemic agents, and the symptoms of hypoglycemia (especially tachycardia) may mask, therefore regular monitoring of blood sugar level is recommended in diabetic patients.

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

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

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

The concomitant administration of clonidine may potentiate the antihypertensive and heart rhythm-relieving effects of carvedilol.

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

Special Instructions

The therapy should be prolonged and should not be stopped abruptly, especially in patients with coronary heart disease, as this may worsen the course of the underlying disease. If necessary, reduction of the drug dose should be gradual, over 1-2 weeks.

At the beginning of therapy with carvedilol or when increasing the dose of the drug, patients, especially elderly patients, may have an excessive decrease in blood pressure, mainly when standing up. Correction of the drug dose is necessary. In patients with chronic heart failure when adjusting the dose, an increase in symptoms of heart failure and edema may occur. In this case the dose of carvedilol should not be increased, it is recommended to prescribe high doses of diuretics until the patient’s condition stabilizes.

Continuous monitoring of electrocardiogram and blood pressure is recommended with simultaneous administration of carvedilol and slow calcium channel blockers, phenylalkylamine derivatives (verapamil) and benzodiazepine (diltiazem), and also with class I antiarrhythmic agents.

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

If surgery is performed using general anesthesia, the anesthesiologist should be advised of prior therapy with Carvedilol.

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

At the time of treatment, avoid the use of ethanol.

Patients with pheochromocytoma should be prescribed alpha-adrenoblockers before therapy.

Patients who wear contact lenses should be aware that the drug may cause decreased tear production.

Impact on driving and operating machinery

It is not recommended to drive at the beginning of therapy and when increasing the dose of Carvedilol. Other activities requiring high concentration and quick psychomotor reactions should be refrained from.

Contraindications

Side effects

Central nervous system disorders: dizziness, headache (usually not severe and at the beginning of treatment), loss of consciousness, myasthenia gravis (more often at the beginning of treatment), increased fatigue, depression, sleep disorders, paresthesias.

Cardiovascular system: bradycardia, orthostatic hypotension, AV blockade II – III degree, rarely – peripheral circulatory disorders, progression of heart failure (during increasing
doses), edema of lower limbs, angina pectoris, marked BP reduction.

Digestive system disorders: dry mouth, nausea, diarrhea or constipation, vomiting, abdominal pain, loss of appetite, increased liver transaminase activity.

Hematopoietic system disorders: rare – thrombocytopenia, leukopenia.

Metabolism disorders: weight gain, disorder of carbohydrate metabolism.

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

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

Others: visual disturbances, decreased tear production, flu-like syndrome, sneezing, myalgia, arthralgia, pain in the extremities, claudication; rarely – disorders of urination and renal function.

Overdose

Symptoms: decreased BP (accompanied by dizziness or fainting), bradycardia. Dyspnea due to bronchospasm and vomiting may occur. In severe cases, cardiogenic shock, respiratory distress, confusion, and conduction disorders may occur.

Treatment: monitoring and correction of vital signs should be carried out, if necessary – in the intensive care unit. Treatment is symptomatic. Intravenous use of m-cholinoblockers (atropine), adrenomimetics (epinephrine, norepinephrine) is advisable.