Carvedilol: reviews. Instructions for use, analogues, price

In the list of popular cardiological drugs "Carvedilol" has been included for a long time. The responses of specialists characterize it as a qualitative treatment for heart failure and control of the AV-node during atrial fibrillation. It can also be widely used for the treatment of hypertension, which makes it a very valuable drug. For this reason, many pharmacological companies synthesize and sell generics "Carvedilola." Each of them has its own peculiarities of releasing and creating therapeutic concentrations in the blood. Although in general they cope with their task.

Since all the drugs "Carvedilol" analogs have the same valuable properties, there is no actual importance in which of them should be chosen for treatment. Although, as studies of bioequivalence show, a more complete and mild effect is produced by more expensive generics and the original drug. Therefore, the purpose of this review is to identify the most high-quality analogues with high therapeutic value.

System characteristic of the medicinal product

As therapeutic preparations "Carvedilol", analogues and its generics have already proved their effectiveness. The medicinal substance itself belongs to the class of adrenoblockers of mixed action. They inhibit two types of adrenaline and norepinephrine receptors: beta and alpha receptors of the first type. The former are located in the heart, and the latter - in the vessels of the muscles. Inhibiting them, the drug provokes the development of several therapeutic effects.

There are no analogues among drugs of the adrenoblocker class in the drug "Carvedilol". There are only similar substances in the mechanisms of action. In particular, the closest drug is Nebivolol, which also has a unique effect. There are also simpler class analogues. They are represented by cardioselective, that is selective for beta-adrenoreceptors of the first type, Metoprolol and Bisoprolol.

In comparison with "Metoprolol", "Carvedilol" is more selective to beta-receptors, showing an affinity for cardiac beta-adrenoceptors almost similar to "Bisoprolol". Carvedilol is also a powerful antioxidant. This effect is extremely important for remodeling the vascular wall, already affected by the processes of atherosclerosis. In importance, this auxiliary property of the drug is inferior to the unique feature of Nebivolol. It causes the activation of nitrogen-dependent endothelial factors, and therefore is able to prevent atherosclerotic lesions of the arteries.

Farmakodinamika "Carvedilola"

Modern medicine "Carvedilol" due to the effects of blockade of beta-adrenoreceptors type I has the following effects:

• Reduces myocardial contractility, reducing the need for cardiac muscle in nutrition and oxygen (antianginal action);
• Is able to inhibit automatism and conduction (antiarrhythmic action);
• Suppresses the renin-angiotensin system of the body (antihypertensive effect);
• Reduces the fraction of cardiac output, reducing the level of systolic blood pressure;
• It is able to expand the vessels of the peripheral channel.

The latter effect positively characterizes "Carvedilol". Reviews of the chronic use of the drug indicate the presence of blockade effects of adrenoreceptors alpha-one subtype. They are located in the peripheral, that is, the muscular vessels. Their blockade leads to the expansion of small arteries. This causes a drop in the overall peripheral hydrodynamic resistance, leading to a decrease in blood pressure and an improvement in muscle nutrition.

Similar action has "Carvedilol", analogs and its generics, not only in skeletal muscles, but also in the heart. This leaves the possibility to use it for chronic heart failure, provoked by chronic ischemia (IHD). And because "Carvedilol" is a selective beta-1-blocker with some tropism for alpha-1 receptors and antioxidant properties, its application is maximally wide.

Application of "Carvedilol"

Since the pharmacodynamic features of the drug favorably characterize "Carvedilol", feedback about its use should either confirm these findings, or refute erroneous judgments. The positive effects of the medication have already been proven, therefore, none of the facts can be refuted. For this reason, "Carvedilol" is suitable as a drug required in the following clinical situations:

• Ischemic cardiac disease;
• Chronic heart failure;
• Tachyarrhythmias;
• Angina pectoris, acute myocardial infarction, unstable angina;
• Arterial hypertension.

Indications

The drug "Carvedilol" testimony follows from its pharmacodynamic features. Because of lowering blood pressure, reducing pre- and post-loading on the myocardium, and also because of antiarrhythmic effect, the drug can be used in the following cases:

• Arterial hypertension II and III degree in the combined balanced treatment;
• Arterial hypertension I degree with a high cardiovascular risk in the form of monotherapy;
• With tachyarrhythmias: constant form of atrial fibrillation, with frequent supraventricular extrasystole;
• With ischemic heart disease with acute manifestations (stenocardia unstable or myocardial infarction);
• With IHD outside of acute manifestations (angina of tension, progressive angina);
• Chronic heart failure, starting from the HIIA stage according to Vasilenko-Strazhesko, or NYHA FC III in a balanced combination treatment;
• With symptomatic arterial hypertension and sinus tachycardia associated with hyperthyroidism or pheochromocytoma.

Analogues available in the drug "Carvedilol" also differ in the presence of these indications. They are used in the most frequent cardiac diseases, that is, with IHD and CHF. Also, the drug has an even wider scope of application. This is an essential hypertension, although symptomatic, provoked by hyperthyroidism or pheochromocytoma, is also effectively controlled by beta-blockers.

Contraindications

Despite a wider therapeutic profile than selective beta-1-blockers, the drug has contraindications that limit its use. "Carvedilol" can not be used in clinical practice in the presence of the following conditions:

• Bronchial asthma, COPD due to increased risk of bronchospasm;
• It is forbidden to take carvedilol at a heart rate of less than 50 per minute because of the risk of fatal bradycardia;
• It is forbidden to prescribe and apply "Carvedilol" in arrhythmias (CA-blockade, AV blockade of 2 nd and 3 rd degree), if a permanent pacemaker is not installed;
• It is unacceptable to prescribe the drug with severe hepatic insufficiency;
• It is forbidden to apply the drug in CHF with functional class IV according to NYHA (HIII according to Vasilenko-Strazhesko) due to oppression of the contractility of the decompensated heart;
• "Carvedilol" is prohibited in pregnancy, lactation, in children under 18 years of age;
• It is inadmissible to apply the drug in case of an allergic reaction to its active ingredient or a component of the dosage form;
• The drug is not used in cardiogenic shock with SBP less than 85 mm Hg. Art.

Despite the fact that "Carvedilol" reviews characterize as a quality and relatively safe drug, you should follow these recommendations. They are designed to protect the patient and the specialist from unwanted situations. Therefore, these contraindications are absolute and can not be ignored because of the high risk of fatal disturbances in the vital activity of the body.

Side effects

To assess the side effects of the drug "Carvedilol" reviews are not indicative. Patients are subjective in assessing clinical and side effects. Therefore, it is more rational to rely on statistical research. Among the side effects, the most frequent, manifested with a frequency of 1 to 10%, are the following:

• From the side of the PNS and the central nervous system, it is possible to develop headaches, dizziness, muscle weakness, sleep disorders, parasthesias as manifestations of idiosyncrasy;
• Cardiovascular effects (transient or persistent bradycardia or AV blockade, orthostatic hypotension, less frequent lameness due to impaired blood supply to muscles with obliterating atherosclerosis);
• Respiratory organs: manifestations of dyspnea, nasal congestion, and bronchial hyperreactivity or obstructive disease, bronchospasm are possible;
• Side effects from the digestive system are manifested by abdominal pain, nausea, dry mouth, diarrhea, and rarely there is constipation or vomiting, liver transaminases may increase;
• The hematopoiesis system rarely responds to thrombocytopenia or leukopenia;
• Possible eczema, pruritus, exacerbation of psoriasis, and rarely anaphylactoid reactions can occur.

Also, since "Carvedilol" is a foreign substance for the body, it is possible to develop a general toxic reaction. It manifests itself as a flu-like syndrome with the development of pain in the limbs, dry eyes, irritation of urination. In this regard, "Karvedilol" has many more side effects than "Metoprolol", although the clinical efficiency of the first exceeds the second.

Features of the long-term use of "Carvedilol"

The main dosage forms of the drug are capsules and tablets. "Carvedilol" is taken once in the case of hypertension and twice with IHD, CHF, or arrhythmia. The initial dose is 6.25 mg once a day, which is suitable for the treatment of hypertension. In the treatment of CHF, IHD or tachyarrhythmias, it is recommended to apply an initial dose of 6.25 twice a day. Then, by titration, the daily dose is adjusted to 25-50 mg.

The drug is used whenever possible and in case of good individual tolerance. It is needed to control arrhythmia or to prolong life in CHF. This feature of the drug taken in combination with diuretics and ACE inhibitors prolongs life. And with CHF tablets "Carvedilol" are transferred much better than "Bisoprolol." Although treatment requires refraining from driving and engaging in potentially dangerous activities, management mechanisms.

Standard Release Forms

The drug "Carvedilol" price is not the determining criterion for choice. It is much more effective to choose a successful dosage form for a particular patient. The most common in the domestic and Western pharmacy network are three types of dosage medication. This is 25 mg, 12.5 and 6.25 mg. The tablets are packed in blisters or in polymeric containers. Medications are taken before meals, if a decrease in dose activity is required, then during meals.

Generics

Generics are those drugs that contain "Carvedilol" in a certain dosage form that meets the requirements of bioequivalence in comparison with the original drug. And now in the domestic pharmacy market there is a mass of generics, divided into three categories according to their value:

• With a high price (Dilatrend, Coriol, Carvedilol Sandoz);
• With an average price (Carvelend, Carvedilol Zentiva, Carvedilol Teva);
• With a low price (Karvedilol-MIK, Karvedilol Belmed, Karvetrend, Karvenal, Vedicardol).

The cost of "Dilatrend" is 450-750 rubles, depending on the dosage: 6.25 mg - cheaper than 25 mg. A similar trend is naturally observed in the case of other drugs. On the "Coriol" the price of 250-500 rubles, for "Carvedilol Sandoz" 300-550 rubles, for "Carvedilol Zentiva" - 250-400 rubles. "Carvedilol Teva" costs 200-300 rubles, "Carveland" - 170-330 rubles, "Carvedilol Belmed" - 150-250, "Carvetrend" - 170-290 rubles.

For the drug "Carvedilol" the price is not an indicator of quality, although it is higher for a medicine of a reputable manufacturer. In the clinic, there are few significant differences between expensive imported drugs and domestic, more accessible analogues. Often, clinicians are concerned only with the discrepancy between the dosage form and the original. Therefore, you should choose a generic in capsules, which will significantly reduce its gastrotoxicity.

In other respects, cheap analogs exhibit the same clinical activity and are effective for the treatment of heart diseases and arterial hypertension. However, if the patient has previously taken a certain generic, then he should be left on. Since he was accustomed to the peculiarities of the dosage form and the dynamics of the increase in the plasma concentration of the active substance, the replacement of the drug will shift his balance. Then it will be subjectively noted that the drug does not work or does not work as it would be desirable.

Class analogues

Class analogues, most fully meet the therapeutic requirements, constitute "Carvedilol" competition in a number of indications. In particular, with hypertension, you should choose either "Bisoprolol" or "Nebivolol". The latter, because of its high cost, can not be used by most patients, although it is a successful drug. If all cardioselective beta-blockers are located, their therapeutic value increases in a number: "Bisoprolol", "Metoprolol", "Carvedilol", "Nebivolol".

"Nebivolol" is considered the best drug for the treatment of hypertension, and "Carvedilol" - for the therapy of CHF. None of the other drugs has so many beneficial effects on the course of chronic heart failure, like Carvedilol. For this reason, in combination with a diuretic and an ACE inhibitor, it is able to prolong human life.

"Carvedilol" is an effective antiarrhythmic, by means of which it is possible to conveniently control the conduct on the AV node. This is important for atrial fibrillation, when the possibility of restoring rhythm and maintaining it is not available. Also, with atrial fibrillation, "Carvedilol" is assigned to control the rhythm during the preparation of the patient for electropulse therapy.