Carvedilol, pills 12.5mg, 30pcs

Composition

1 tablet contains: Active ingredient: carvedilol 12.5 mg

Pharmacological action

Pharmacodynamics

Carvedilol blocks alpha-1 -, beta – 1-and beta-2-adrenergic receptors. It has vasodilating, antianginal and antiarrhythmic effects. The vasodilating effect is mainly associated with the blockade of alpha-1 receptors. Vasodilation reduces total peripheral vascular resistance (OPSS). It does not have its own sympathomimetic activity and has membrane-stabilizing properties. The combination of vasodilation and beta-adrenergic blockade leads to the following effects: in patients with arterial hypertension, a decrease in blood pressure (BP) is not accompanied by an increase in OPSS, and peripheral blood flow does not decrease (unlike beta-blockers). Heart rate decreases slightly. In patients with CHD, it has an antianginal effect. Reduces pre-and post-stress on the heart. It does not have a pronounced effect on lipid metabolism and the content of potassium, sodium, and magnesium in blood plasma. In patients with impaired left ventricular function or circulatory insufficiency, it has a positive effect on hemodynamic parameters and improves the ejection fraction and size of the left ventricle. It has an antioxidant effect, eliminating free oxygen radicals.

Pharmacokinetics

Carvedilol is rapidly and almost completely absorbed after oral use from the gastrointestinal tract. It binds almost completely to plasma proteins (98-99%). The concentration in the blood plasma is proportional to the dose taken. Bioavailability is about 25% due to the high degree of metabolism in the liver. In this case, metabolites are formed that have a high ability to block beta-adrenergic receptors. The maximum concentration in the blood plasma is reached after 1 hour. The elimination half-life is 6-10 hours.

In elderly patients, the concentration of carvedilol in the blood plasma is approximately 50% higher than in young patients. It is mainly excreted in the bile. In patients with impaired liver function, bioavailability may increase up to 80%. Penetrates the placental barrier, is excreted in breast milk. Food slows down the absorption of the drug, but does not affect its bioavailability.

Indications

• Arterial hypertension (in monotherapy and in combination with diuretics)
• Chronic heart failure (as part of combination therapy)
• Coronary heart disease: stable angina pectoris.

Contraindications

• Hypersensitivity to carvedilol or other components of the drug,
• acute and chronic decompensated heart failure
• requiring intravenous inotropic funds,
• severe liver failure,
• atrioventricular block II to III century,
• bradycardia (less than 50 beats/min),
• the syndrome of weakness of the sinus node,
• hypotension (systolic blood pressure less than 85 mm Hg. Hg),
• cardiogenic shock,
• bronchial asthma,
• chronic obstructive pulmonary disease,
• age to 18 years (efficacy and safety not established).

With caution: Bronchospastic syndrome, chronic bronchitis, emphysema of the lungs, Prinz Metal angina, thyrotoxicosis, occlusive diseases of peripheral vessels, pheochromocytoma, psoriasis, renal failure, atrioventricular block I degree, extensive surgery and general anesthesia, diabetes mellitus, hypoglycemia, depression, myasthenia gravis.

Side effects

From the central nervous system: headache, dizziness, syncopal states, muscle weakness (more often at the beginning of treatment), sleep disorders, depression, paresthesia.

From the cardiovascular system: bradycardia, orthostatic hypotension, angina pectoris, atrioventricular block, rarely – “intermittent” claudication, violation

of peripheral blood circulation, progression of heart failure.

From the gastrointestinal tract: dry mouth, nausea, abdominal pain, diarrhea or constipation, vomiting, increased activity of “liver” transaminases.

Hematopoietic disorders: thrombocytopenia, leukopenia.

From the urinary system: severe renal impairment, edema.

Allergic reactions: skin allergic reactions (exanthema, urticaria, pruritus, rashes), exacerbation of psoriatic rashes, sneezing, nasal congestion, bronchospasm, shortness of breath (in predisposed patients).

Others: flu-like syndrome, pain in the extremities, decreased tear production, weight gain.

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, monoaminooxidase 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. Strictly follow your doctor’s instructions. Without prior consultation with your doctor, you should not stop Carvedilol treatment or change its dosage. If it is necessary to cancel the drug, the dose reduction should occur gradually over 1 to 2 weeks. If there is no therapeutic effect from treatment or if the condition worsens, consult your doctor.

Arterial hypertension. The dose is selected individually. For the first 7-14 days, the recommended dose of Carvedilol is 12.5 mg (1 tablet of 12.5 mg), taken in the morning after breakfast. The dose can be divided into two doses of 6.25 mg of Carvedilol (1/2 tablet of 12.5 mg). Further treatment should be given with Carvedilol at a dose of 25 mg (1 tablet of 25 mg) in the morning or divided into two doses of 12.5 mg of the drug (1 tablet of 12.5 mg). If necessary, the doctor may increase the dose again after 14 days. Take this medicine after a meal with a small amount of liquid.

Stable angina pectoris. The initial dose of Carvedilol is 12.5 mg (1 tablet of 12.5 mg) twice a day. After 7-14 days, under the supervision of a doctor, the dose of Carvedilol can be increased to 25 mg (1 tablet of 25 mg) twice a day. After 14 days, if there is insufficient efficacy and good tolerability, the dose of Carvedilol can be further increased.

The total daily dose of Carvedilol for angina pectoris should not exceed 50 mg of the drug (2 tablets of 25 mg), prescribed 2 times a day. If you are over 70 years of age, then the daily dose of Carvedilol should not exceed 25 mg (1 tablet of 25 mg) twice a day. If you have missed the next dose, then you should take the drug as soon as possible. However, if the time for the next dose is already approaching, then you should only take it, without doubling it. You should take the drug regularly. If you have not taken the drug for more than 2 weeks, you should resume treatment with the lowest 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 a day, then l2.5 mg 2 times a day, then to 25 mg 2 times a day. The dose should be increased to the maximum that is well tolerated by the patient. In patients with a body weight of less than 85 kg, the target dose is 50 mg per day; in patients with a body weight of more than 85 kg, the target dose is 75-100 mg per day.

If treatment is interrupted for more than 2 weeks, then its resumption begins with a dose of 3.125 mg 2 times a day, followed by an increase in the dose.

Overdose

Symptoms: low 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, especially 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.

Continuous monitoring of the electrocardiogram and blood pressure is recommended with simultaneous use of carvedilol and slow calcium channel blockers, phenylalkylamine derivatives (verapamil) and benzodiazepine (diltiazem), as well as with Class I antiarrhythmics. It is recommended to monitor renal function in patients with chronic renal insufficiency, 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. 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.

Form of production

Tablets

Storage conditions

Store in a dry place, protected from light, at a temperature not exceeding 25° C.

Shelf

life is 3 years.

Active ingredient

Carvedilol

Conditions of release from pharmacies

By prescription

Dosage form

Tablets