Carvedilol - instructions for use, reviews, analogs and formulations (tablets 12.5 mg and 25 mg) of the drug for the treatment of heart failure and depression in adults, children and pregnancy

In this article, you can read the instructions for using the drug Carvedilol. Presented are reviews of visitors to the site - consumers of this medication, as well as opinions of doctors specialists on the use of Carvedilol in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of Carvedilol in the presence of existing structural analogues. Use to treat heart failure and reduce blood pressure in adults, children, as well as during pregnancy and lactation.

Carvedilol - alpha and beta-adrenoblocker without internal sympathomimetic activity.

It blocks alpha1, beta1 and beta2-adrenergic receptors. Has vasodilating, antianginal and antiarrhythmic action.

The vasodilating effect is mainly related to the blockade of alpha 1-adrenergic receptors. Thanks to vasodilation reduces OPSS. It has membrane-stabilizing properties. The combination of vasodilation and blockade of beta-adrenoreceptors leads to the following effects: in patients with arterial hypertension, a decrease in blood pressure is not accompanied by an increase in OPSS, peripheral blood flow (in contrast to beta-blockers) does not decrease. The heart rate decreases slightly.

In patients with IHD, it has an antianginal effect. Reduces pre- and postnagruzku on the heart. It has no pronounced effect on the lipid metabolism and the content of potassium, sodium, and magnesium in the blood plasma. In patients with impaired left ventricular function or circulatory failure, it has a beneficial effect on hemodynamic parameters and improves the ejection fraction and the size of the left ventricle. It has an antioxidant effect, eliminating free oxygen radicals.

Composition

Carvedilol + excipients.

Pharmacokinetics

After intake of carvedilol quickly and almost completely absorbed from the digestive tract. Bioavailability is 25% (due to the high degree of metabolism in the liver). Concentration in the blood plasma is proportional to the dose taken. The intake of food slows the absorption of carvedilol, without affecting its bioavailability. Binding to plasma proteins is almost complete - 98-99%. Penetrates through the placental barrier, excreted in breast milk. Metabolized with the formation of metabolites that have a high ability to block beta-adrenergic receptors. It is excreted mainly with bile.

Indications

• arterial hypertension (as a mono- or combination therapy);
• stable angina;
• chronic heart failure (as part of combination therapy).

Forms of release

Tablets 12.5 mg and 25 mg.

Instructions for use and dosage

The dosage regimen is set individually.

The drug is taken orally, regardless of food intake.

With hypertension for the first 7-14 days, the recommended initial dose is 12.5 mg per day (1 tablet) in the morning after breakfast. The dose can be divided into 2 divided doses of 6.25 mg of Carvedilol (1/2 tablets of 12.5 mg).Next, the drug is prescribed in a dose of 25 mg (1 tablet 25 mg) in 1 morning, or divided into 2 divided doses of 12.5 mg (1 tablet 12.5 mg). If necessary, after 14 days, it is possible to increase the dose once more.

With stable angina, the initial dose of Carvedilol is 12.5 mg (1 tablet 12.5 mg) 2 times a day. After 7-14 days the dose can be increased to 25 mg (1 tablet 25 mg) 2 times a day. With insufficient effectiveness and good tolerability after 14 days and the dose of Carvedilol can be further increased. The daily dose of Carvedilol in angina pectoris should not exceed 50 mg (2 tablets of 25 mg), administered twice a day.

For patients over the age of 70, the daily dose of Carvedilol should not exceed 25 mg (1 tablet 25 mg) twice daily.

If the drug is withdrawn, the dose reduction should be carried out gradually within 1-2 weeks.

If you miss a regular dose, the drug should be taken as soon as possible. However, if it's time for the next appointment, then you need to take only one single dose (without doubling).

At a break in taking the drug for more than 2 weeks, it is necessary to resume treatment with the lowest doses of Carvedilol.

With chronic heart failure, the dose is selected individually, under the careful supervision of a doctor. The recommended initial dose is 3.125 mg twice a day for 2 weeks.With good tolerance, the dose is increased at intervals of at least 2 weeks to 6.25 mg twice a day, then 12.5 mg twice a day and then to 25 mg twice a day. The dose should be increased to the maximum, which 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.

Side effect

• headache;
• dizziness;
• muscle weakness (often at the beginning of treatment);
• sleep disorders;
• depression;
• bradycardia;
• orthostatic hypotension;
• angina pectoris;
• AV blockade;
• violations of peripheral circulation;
• intermittent claudication;
• progression of heart failure;
• dry mouth;
• nausea, vomiting;
• abdominal pain;
• diarrhea;
• constipation;
• thrombocytopenia, leukopenia;
• severe renal dysfunction;
• edema;
• skin reactions (exanthema, urticaria, pruritus, rash);
• exacerbation of psoriasis;
• sneeze;
• nasal congestion;
• bronchospasm;
• shortness of breath (in predisposed patients);
• influenza-like syndrome;
• pain in the limbs;
• reduction of lacrimation;
• increase in body weight.

Contraindications

• severe hepatic impairment;
• pronounced bradycardia (heart rate less than 50 beats per minute);
• syndrome of weakness of the sinus node (SSSU);
• AV-blockade 2 and 3 degrees (except for patients with an artificial pacemaker);
• chronic heart failure in the stage of decompensation;
• acute heart failure;
• cardiogenic shock;
• arterial hypotension (systolic blood pressure less than 85 mm Hg);
• pregnancy;
• lactation (breastfeeding);
• children and adolescents under 18;
• hypersensitivity to carvedilol and other components of the drug.

Application in pregnancy and lactation

The drug is contraindicated for use in pregnancy and lactation (breastfeeding).

Application in elderly patients

For patients over the age of 70, the daily dose of Carvedilol should not exceed 25 mg (1 tablet 25 mg) twice daily.

Use in children

The drug is contraindicated in children and adolescents under 18 years. The safety and efficacy of carvedilol in children and adolescents under the age of 18 years have not been established.

special instructions

Caution should be given to patients with bronchospastic syndrome, chronic bronchitis, emphysema.

At the beginning of treatment with Carvedilol and with increasing the dose of the drug, a sharp decrease in blood pressure and orthostatic reactions are possible. Dizziness may occur up to fainting, especially in elderly patients, with heart failure, with combined antihypertensive therapy or with diuretics.

The drug is not recommended for use in patients with low blood pressure.

Treatment with carvedilol should not be abruptly discontinued, especially in patients with angina pectoris. this can lead to a worsening of the condition. Dose reduction should be gradual within 1-2 weeks.

During the period of carvedilol administration, renal function in patients with renal insufficiency, ischemic heart disease, peripheral vascular disease, arterial hypotension and / or heart failure should be monitored. If the kidney function worsens, the drug should be discarded.

The appointment of beta-blockers to patients with peripheral vascular disease,with psoriasis and anaphylactic reactions in the anamnesis may lead to a worsening of the course of the disease, and with Prinzmetal angina pectoris may provoke the appearance of chest pains. In addition, the use of carvedilol may reduce the sensitivity of allergic tests.

The purpose of the drug may mask the symptoms of thyrotoxicosis and the early symptoms of hyperglycemia. With diabetes, regular monitoring of blood glucose levels and, if necessary, correction of hypoglycemic therapy are recommended.

With the use of Carvedilol with caution should be conducted general anesthesia using drugs with a negative inotropic effect (ether, cyclopropane, trichlorethylene). The patient should inform the doctor about taking Carvedilol. Before extensive surgical interventions, gradual withdrawal is recommended.

Care should be taken when using the drug in case of severe metabolic acidosis.

When using the drug in patients with pheochromocytoma before the start of therapy, alpha-blockers are prescribed.

Avoid using the drug when wearing contact lenses due to reduced tearing.

During the period of drug use, alcohol should be avoided.

It should be borne in mind that if you need to cancel combination therapy with carvedilol and clonidine, Carvedilol should be canceled first, a few days before the gradual decrease in the dose of clonidine.

Impact on the ability to drive vehicles and manage mechanisms

It should be borne in mind that at the beginning of treatment and with increasing doses of Carvedilol, blood pressure can be excessively reduced, causing dizziness. Therefore, during the treatment period, patients should refrain from engaging in potentially hazardous activities requiring increased attention and speed of psychomotor reactions.

Drug Interactions

On the background of Carvedilol therapy, diltiazem and Verapamil can not be administered IV because of a possible pronounced decrease in heart rate and a pronounced decrease in blood pressure.

Some antiarrhythmic drugs, narcosis drugs, antihypertensive drugs, antianginal drugs, other beta-blockers (including those used in the form of eye drops), MAO inhibitors, sympatholytics (reserpine) and cardiac glycosides can enhance the effect of Carvedilol. With a simultaneous appointment with Carvedilol, doses of these drugs should be selected with caution.

When applied simultaneously with inducers of liver enzymes (for example, with rifampicin, phenobarbital), the concentration of carvedilol in the blood plasma may decrease, and when combined with inhibitors of hepatic enzymes (eg, cimetidine), the carvedilol concentration in the plasma may increase.

With the simultaneous use of carvedilol may increase the concentration of Digoxin in the blood plasma.

Simultaneous administration of carvedilol with ergot alkaloids worsens the peripheral circulation.

Carvedilol can enhance the effect of hypoglycemic drugs and mask the manifestations of hypoglycemia (it is recommended to regularly monitor blood glucose levels).

Analogues of the drug Carvedilol

Structural analogs for the active substance:

• Acridilol;
• Bagolol;
• Vedicardol;
• Dilatrend;
• Carvedigamma;
• Carvedilol Zentiva;
• Carvedilol Canon;
• Carvedilol Sandoz;
• Carvedilol Stade;
• Carvedilol Teva;
• Carvenal;
• Carvetrend;
• Carvydil;
• Kardivas;
• Coriol;
• Credex;
• Rekardium;
• Talliton.

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