Carvedilol-OBL, tablets 12.5mg 30 pcs

Carvedilol has a combined nonselective β1- β2- and α1-blocking effect. The drug has no sympathomimetic activity of its own and has membrane stabilizing properties.

Blocking the β-adrenoreceptors of the heart may decrease blood pressure, cardiac output and heart rate. Carvedilol suppresses the renin-angiotensin-aldosterone system through blockade of renal β-adrenoceptors, causing a decrease in plasma renin activity.

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 – reduction of blood pressure;

in patients with coronary heart disease – anti-ischemic and antianginal action;

In patients with left ventricular dysfunction and circulatory insufficiency – it has favorable effect on hemodynamic parameters, increases left ventricular ejection fraction and decreases its size.

Indications

Active ingredient

Composition

1 tablet contains:

the active ingredient:

carvedilol 12.5 mg;

auxiliary substances:

sugar (sucrose),

magnesium stearate,

p> potato starch,

hydroxypropyl methylcellulose (hypromellose),

crosscarmellose sodium salt (primellose),

aerosil (colloidal silicon dioxide),

calcium phosphate.

How to take, the dosage

Overly, regardless of meals.

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. If the antihypertensive effect is insufficient, the dose may be doubled after 2 weeks of therapy. The maximum recommended daily dose of the drug 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 treatment. Thereafter, 25 mg 2 times a day. 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 per day divided into two doses.

Chronic heart failure

The dose is adjusted individually, under close medical supervision. The recommended starting dose is 3.125 mg twice daily for 2 weeks. In case of good tolerance, the dose is increased at an interval of at least 2 weeks to 6.25 mg twice a day, then to 12.5 mg twice a day, then to 25 mg twice a day. The dose should be increased to the maximum that is well tolerated by the patient. In patients with body weight less than 85 kg the target dose is 50 mg per day; in patients with body weight over 85 kg the target dose is 75-100 mg per 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.
Concomitant administration of carvedilol and digoxin increases the concentration of the latter and may increase 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 levels 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.

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 cardiac rhythm-relieving effects of carvedilol.
General anesthetics enhance 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 CHD, as this may lead to a worsening of the course of the underlying disease. If necessary, reduction of the drug dose should be gradual, over a period of 1-2 weeks.

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

Periodic ECG and BP should be monitored when Carvedilol OBL is coadministered with slow calcium channel blockers, phenylalkylamine derivatives (verapamil) and benzothiazepine (diltiazem), and 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 under general anesthesia, the anesthesiologist should be advised of prior therapy with Carvedilol-OBL.

Carvedilol-OBL has no effect on blood glucose concentration and does not cause changes in glucose tolerance test in patients with insulin-independent diabetes mellitus.

Ethanol should be avoided during treatment.

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

Patients who wear contact lenses should note 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-OBL. Other activities requiring high concentration and quick psychomotor reactions should be avoided.

Contraindications

With caution: Princetal angina, thyrotoxicosis, peripheral vascular occlusive disease, pheochromocytoma, psoriasis, renal failure, grade I AV blockade, extensive surgery and general anesthesia, diabetes, hypoglycemia, depression, myasthenia.

Side effects

Immune system disorders: very rare – hypersensitivity.

Hematopoietic system: frequent – anemia; rare – thrombocytopenia; very rare – leukopenia.

Nervous system disorders: very frequent – dizziness, headache; infrequent – fainting state, syncope, paresthesias.

An organ of vision: frequent – visual disturbances, decreased lacrimation (dry eyes), eye irritation.

Cardiovascular system disorders: very frequent – heart failure during dose escalation, marked BP reduction; frequent – bradycardia, edema, hypervolemia, fluid retention, orthostatic hypotension, peripheral circulatory disorders (limb coldness, peripheral vascular disease, worsening of intermittent claudication and Raynaud syndrome); infrequent – AV blockade of degree II-III, angina pectoris.

Respiratory system disorders: frequent – shortness of breath, pulmonary edema, asthma in susceptible patients, bronchitis, pneumonia, upper respiratory tract infections; rare – nasal congestion.

Digestive system disorders: frequent – nausea, diarrhea, vomiting, dyspepsia, abdominal pain; infrequent – constipation, dry mouth.

Hepatic and biliary tract disorders: very rare – increased ALT, AST and GGT activity.

Skin and subcutaneous tissue disorders: infrequent – skin reactions (e.g., allergic exanthema, dermatitis, urticaria, pruritus, psoriasis-like and scaly-like skin lesions, alopecia); very rare – erythema multiforme, Stevens-Johnson syndrome and toxic epidermal necrolysis.

Muscular system disorders: frequent – pain in the extremities.

Perior urinary system disorders: frequent – urinary tract infections, urinary disorders, renal failure and renal dysfunction in patients with diffuse vasculitis and/or impaired renal function; very rare – urinary incontinence in women (reversible after drug withdrawal).

Gender and mammary gland disorders: infrequent – erectile dysfunction.

Metabolism and nutrition: frequent – hypercholesterolemia, hyperglycemia or hypoglycemia in patients with diabetes.

General disorders: very frequent – asthenia, increased fatigue; frequent – weight gain.

Dizziness, fainting, headache, and asthenia of usually mild degree occur more frequently at the beginning of therapy with Carvedilol Zentiva.

When the drug is used in patients with chronic heart failure and low BP (systolic BP)

The presence of beta-adrenoblocking properties of the drug does not exclude the possibility of manifestation of latent diabetes mellitus, decompensation of existing diabetes mellitus or suppression of the counterinsulatory system.

Overdose

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

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.

Similarities