The list of demanded cardiological drugs for a long time includes "Carvedilol". Reviews of experts characterize it as a quality tool for the treatment of 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 Carvedilol generics. Each of them has its own characteristics of the release and creation of therapeutic concentrations in the blood. Although in general they cope with their task.
Since all Carvedilol analogues have the same valuable properties, there is no actual importance in which one should be chosen for treatment. Although, as bioequivalence studies show, more expensive and more generic and the original drug have a fuller and milder effect. Therefore, the aim of this review is to highlight the highest quality analogues with high therapeutic value.
Systemic characteristics of the drug
As therapeutic drugs "Carvedilol", analogues and its generics have already proven their effectiveness. The drug substance itself belongs to the class of adrenergic blockers of mixed action. They inhibit two types of adrenaline and noradrenaline 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. By inhibiting them, the drug provokes the development of several therapeutic effects.
Among drugs of the class of adrenergic blocking agents, the drug “Carvedilol” has no analogues. There are only similar substances on the mechanisms of action. In particular, the closest drug is Nebivolol, which also has a unique effect. There are simpler class analogues. They are represented by cardioselective, that is, selective in relation to the first type of beta-adrenergic receptors, Metoprolol and Bisoprolol.
Compared to Metoprolol, Carvedilol is more selective for beta receptors, showing an affinity for cardiac beta adrenoreceptors almost similar to Bisoprolol. At the same time, Carvedilol is also a powerful antioxidant. This effect is extremely important for the remodeling of 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.
Pharmacodynamics "Carvedilol"
The modern medicine "Carvedilol" due to the effects of blockade of beta-adrenergic receptors of type I has the following effects:
- reduces myocardial contractility, reducing the need for heart muscle in nutrition and oxygen (antianginal effect);
- 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;
- able to dilate the vessels of the peripheral bed.
The latter effect positively characterizes Carvedilol. Reviews of the chronic use of the drug indicate the presence of blockade effects of adrenoreceptor alpha-one subtype. They are located in peripheral, that is, muscular vessels. Their blockade leads to the expansion of small arteries. This provokes a drop in total peripheral hydrodynamic resistance, leading to a decrease in blood pressure and an improvement in muscle nutrition.
A similar effect is exerted by Carvedilol, analogues and its generics, not only in skeletal muscle, but also in the heart. This leaves it possible to apply it in case of chronic heart failure provoked by chronic ischemia (CHD). And since Carvedilol is a selective beta 1-blocker with some affinity for alpha1 receptors and antioxidant properties, its use is as wide as possible.
The use of "Carvedilol"
Since the pharmacodynamic characteristics of the drug favorably characterize Carvedilol, reviews of its use should either confirm these findings or refute erroneous judgments. The positive effects of the drug have already been proven, therefore, none of the facts is subject to refutation. For this reason, "Carvedilol" is suitable as a drug necessary in the following clinical situations:
- coronary heart disease;
- chronic heart failure;
- tachyarrhythmias;
- angina pectoris, acute myocardial infarction, unstable angina pectoris;
- arterial hypertension.
Indications
The drug "Carvedilol" testimony follows from its pharmacodynamic characteristics. Due to a decrease in blood pressure, a decrease in pre- and afterload on the myocardium, as well as due to the antiarrhythmic effect, the drug can be used in case of the following diseases:
- arterial hypertension II and III degree as part of a combined balanced treatment;
- arterial hypertension of the I degree with high cardiovascular risk in the form of monotherapy;
- with tachyarrhythmias: a constant form of atrial fibrillation, with frequent supraventricular extrasystoles;
- with coronary heart disease with acute manifestations (unstable angina or myocardial infarction);
- with coronary heart disease outside of acute manifestations (angina pectoris, progressive angina pectoris);
- chronic heart failure, starting from the HIIA stage according to Vasilenko-Strazhesko, or FC III according to NYHA as part of a balanced combination treatment;
- with symptomatic arterial hypertension and sinus tachycardia associated with hyperthyroidism or pheochromocytoma.
Available analogues of the drug "Carvedilol" also differ in the presence of these indications. They are used for the most common cardiac diseases, that is, for coronary heart disease and heart failure. Also, the drug has an even wider scope. This is essential arterial hypertension, although symptomatic, triggered 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" cannot be used in clinical practice in the presence of the following conditions:
- bronchial asthma, COPD due to an increased risk of bronchospasm;
- it is forbidden to take "Carvedilol" with a heart rate of less than 50 per minute due to the risk of fatal bradycardia;
- it is forbidden to prescribe and use "Carvedilol" in case of arrhythmias (SA-blockade, AV-blockade of the 2nd and 3rd degree), unless a regular pacemaker is installed;
- the administration of the drug in severe liver failure is unacceptable;
- it is forbidden to use the drug in heart failure with functional class IV according to NYHA (HIII according to Vasilenko-Strazhesko) due to inhibition of contractile ability of a decompensated heart;
- "Carvedilol" is prohibited during pregnancy, lactation, in children under 18 years of age;
- it is unacceptable to use the drug in case of an allergic reaction to its active substance or component of the dosage form;
- the drug is not used for cardiogenic shock with SBP less than 85 mm RT. Art.
Despite the fact that Carvedilol reviews are characterized as a high-quality and relatively safe drug, these recommendations should be followed. They are designed to protect the patient and specialist from undesirable situations. Therefore, these contraindications are absolute and cannot be ignored due to the high risk of fatal disorders 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 studies. Among the side effects, the most common, occurring with a frequency of 1 to 10%, are the following:
- on the part of the PNS and central nervous system, headaches, dizziness, muscle weakness, sleep disturbances, parasthesia as manifestations of idiosyncrasy are possible;
- cardiovascular effects (transient or persistent bradycardia or AV block, orthostatic hypotension, less often lameness due to impaired blood supply to muscles with obliterating atherosclerosis);
- respiratory organs: manifestations of shortness of breath, nasal congestion are possible , and bronchospasm is possible with bronchial hyperreactivity or obstructive disease;
- side effects from the digestive system are manifested by abdominal pains, nausea, dry mouth, diarrhea, and constipation or vomiting is extremely rare, liver transaminases may increase;
- the hematopoietic system rarely reacts with thrombocytopenia or leukopenia;
- eczema, pruritus, exacerbation of psoriasis are possible, and anaphylactoid reactions can be extremely rare.
Also, since Carvedilol is a substance alien to the body, the development of a general toxic reaction is possible. It manifests itself as a flu-like syndrome with the development of pain in the limbs, dry eyes, and irritation of urination. In this regard, Carvedilol has much more side effects than Metoprolol, although the first is superior in clinical efficacy to the second.
Features of long-term use of "Carvedilol"
The main dosage forms for the release of the drug are capsules and tablets. "Carvedilol" is taken once in case of arterial hypertension and twice in case of 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 heart failure, coronary heart disease or tachyarrhythmia, it is recommended to use 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 arrhythmias or to prolong life in heart failure. This feature of the drug, taken in combination with diuretics and ACE inhibitors, prolongs life. Moreover, with CHF, Carvedilol tablets are much better tolerated than Bisoprolol. Although treatment requires refraining from driving and engaging in potentially hazardous activities, controlling machinery.
Standard release forms
The drug "Carvedilol" price is not a determining criterion for selection. It is much more effective to choose the right dosage form for a particular patient. Most often, three types of dosages of the drug are distributed in the domestic and western pharmacy chains. These are 25 mg, 12.5 and 6.25 mg. Tablets are packed in blisters or in plastic containers. Medications are taken before meals, but if a dose activity reduction is required, then with meals.
Generics
Generics are those preparations that contain "Carvedilol" in a specific dosage form that meets the requirements of bioequivalence in comparison with the original drug. And now in the domestic pharmacy market there are a lot of generics, divided into three categories according to their value:
- with a high price ("Dilatrend", "Coriol", "Carvedilol Sandoz");
- with an average price (Carveland, Carvedilol Zentiva, Carvedilol Teva);
- with a low price (Carvedilol-MIK, Carvedilol Belmed, Karvetrend, Carvenal, 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. The price for Coriol is 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, "Karvetrend" - 170-290 rubles.
For the drug "Carvedilol" the price is not an indicator of quality, although it is higher for the medicine of a reputable manufacturer. In the clinic, there are few significant differences between expensive imported drugs and domestic, more affordable analogues. Often, clinicians are only concerned about the mismatch of the dosage form to the original. Therefore, you should choose a generic capsule, which will significantly reduce its gastrotoxicity.
Otherwise, cheap analogues exhibit the same clinical activity and are effective for the treatment of heart diseases and arterial hypertension. However, if the patient previously took a certain generic, then it should be left further. Since he is used 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 its balance. Then it will be subjectively noted that the drug substance does not work or does not work as we would like.
Class analogues
Class analogues that most fully meet the therapeutic requirements make up Carvedilola in a number of indications. In particular, for hypertension, either Bisoprolol or Nebivolol should be selected. The latter, due to its high cost, cannot be used by most patients, although it is a successful drug. If all cardioselective beta-blockers are located, then their therapeutic value increases in the series: “Bisoprolol”, “Metoprolol”, “Carvedilol”, “Nebivolol”.
"Nebivolol" is considered the best drug for the treatment of hypertension, and "Carvedilol" - for the treatment of heart failure. None of the other medicinal substances has as many beneficial effects on the course of chronic heart failure as Carvedilol. For this reason, in combination with a diuretic and an ACE inhibitor, it is able to prolong a person's life.
Carvedilol is an effective antiarrhythmic through which it is possible to conveniently control the AV node. This is important for atrial fibrillation, when the ability to restore rhythm and maintain it is not available. Also, with atrial fibrillation, Carvedilol is prescribed for rhythm control during the preparation of the patient for electropulse therapy.