In the article, we will consider why Carvedilol tablets help.
This is an alpha and beta blocker that does not have internal sympathomimetic activity and has antiarrhythmic, vasodilating, antianginal effects.
The composition of the drug, pharmacological forms
Why Carvedilol tablets help, is interesting to many.
The drug is available in tablet form. Pills have a cylindrical shape, white. On one side is dividing risk. Tablets of 10 pieces are packed in cell packs of the contour type. Each cardboard pack contains 3 cell packs.
Instructions for use with Carvedilol tablets are available in each pack.
The active substance in the medicine is carvedilol. The dosage of the active component may be 12.5, or 25 mg. Excipients are: croscarmellose sodium, crospovidone, lactose, polyvidone K25, methyl cellulose, sucrose.
Pharmacodynamics, pharmacokinetics of the drug
Carvedilol appears to be a recmic mixture of stereoisomers capable of blocking alpha-1-, beta-1-, beta-2-adrenergic receptors. Each of the stereoisomers is characterized by identical alpha-blocking as well as antioxidant properties. Carvedilol also has a beta-blocking effect, which is not selective. It can be explained by the presence of a levorotatory stereoisomer in the substance.
Carvedilol does not have its own activity of a sympathomimetic nature, it is characterized by membrane-stabilizing properties.
Vasodilating effects are mainly due to blocking of alpha-1-adrenergic receptors. Due to this effect of the drug, a decrease in OPSS is noted. Vasodilation is combined with beta-type adrenergic blockade, which provokes a decrease in blood pressure in patients with arterial hypertension without an increase in OPSS. Moreover, in comparison with beta-blockers, the drug does not cause a slowdown in blood flow in peripheral vessels. There is a slight decrease in heart rate. When using carvedilol in patients suffering from coronary heart disease, an antianginal effect is noted, the preload and afterload on the system of blood vessels and the heart are reduced. The substance does not have a pronounced effect on the level of potassium, sodium, magnesium ions, as well as lipid metabolism in the blood.
According to the instructions for use with Carvedilol tablets, when used by patients suffering from heart failure or left ventricular dysfunctions, the pharmaceutical product is able to normalize the size of the left ventricle, improve the ejection fraction, and have a favorable effect on hemodynamics. In addition, carvedilol is characterized by an antioxidant effect, which is the elimination of oxygen free radicals.
Therapy “Carvedilol” allows you to reduce the number of deaths and reduce the frequency of hospitalizations, eliminate unpleasant symptoms, improve the functionality of the left ventricle in people with chronic heart failure, ischemic and non-ischemic nature. The therapeutic properties of the drug are dose dependent.
When using tablets, carvedilol is rapidly absorbed by the digestive tract. The substance is highly active. The maximum degree of concentration of the main component in the patient’s blood is observed on average one hour after use. The half-elimination period is about 6-10 hours. Carvedilol binds to plasma proteins at 95-98%. The drug is bioavailable at 24-28%. The bioavailability of the main component does not depend on co-administration with food.
Most of the active ingredient is metabolized in the liver through oxidation and conjugation. As a result, certain metabolites are formed. Carvedilol is characterized by a first passage through the liver. Due to metabolism, 3 metabolites are formed, which are characterized by vasodilating properties. They appear to a lesser extent than carvedilol. The metabolites have an antioxidant and adrenergic blocking effect. Carvedilol is excreted mainly through the intestines together with bile, partly in the form of metabolites together with urine.
If patients have dysfunctional renal impairment, the pharmacokinetic properties of the drug do not significantly change. The pharmacokinetics of the drug remains at the same level, regardless of what age the patient is.
The bioavailability of the active component increases to 80% in patients suffering from cirrhosis. This is due to a decrease in metabolic rate due to the initial passage through the liver tissue. The use of carvedilol in severe hepatic dysfunction is not recommended.
The active component is able to penetrate the placental barrier, is determined in the composition of breast milk, through dialysis, it is practically not excreted from the blood plasma.
Indications for the use of a medication
So, from what tablets "Carvedilol" prescribed? The medication is indicated for use with the goal of treating the following conditions:
- Arterial hypertension.
- Chronic heart failure. In this case, the medication is used as an element of a complex effect.
- Stable angina pectoris.
Contraindications to the use of the drug
As the instructions indicate, Carvedilol tablets should not be used if the patient has the following pathological and physiological conditions:
- Increased susceptibility to the components of the drug.
- Lactation period, pregnancy.
- Age to 18 years.
- Cardiogenic shock.
- Arterial hypotension, in which the level of systolic blood pressure drops below 85 mm Hg. Art.
- Acute forms of heart failure.
- 2nd and 3rd degrees of antrioventricular blockade, with the exception of patients who have an artificial pacemaker.
- Decompensated chronic forms of heart failure.
- Weakness of the sinus node.
- Severe forms of bradycardia, in which the heart rate is less than 50 beats / min.
In accordance with the manufacturer's annotation, Cavedilol should be used with caution in the following cases:
- Depression.
- Diabetes.
- Hypoglycemia.
- Myasthenia gravis
- General anesthesia used during extensive surgical interventions.
- Chronical bronchitis.
- Emphysema.
- Bronchospastic syndrome.
- Psoriasis.
- Renal failure.
- Pheochromocytosis.
- Thyrotoxicosis.
- Occlusive pathologies of peripheral vessels.
- Prinzmetal's angina pectoris.
- AV blockade of the first degree.
So, we found out that Carvedilol tablets are from high pressure. These tablets must be taken in strict accordance with the instructions.
Use of the drug, recommended dosages
Tablets should be taken orally, while drinking water in small quantities. The dose of the medicine is calculated by a specialist, based on clinical indications.
The instructions for Carvedilol tablets contain the following general recommendations:
- With stable angina pectoris, therapy is indicated to be started with a double dose of 12.5 mg per day. If the drug is well tolerated by the patient, and the effectiveness is insufficient, the first dose increase of 12.5 mg should be made after 1-2 weeks. A subsequent increase is made after 14 days, without changing the frequency of receptions. A day should be no more than two doses of the drug, the daily dose should not exceed 50 mg.
- In chronic insufficiency, it is recommended to start therapy with a double dose of the initial dose, which is 3.125 mg. The specialist selects the dose strictly individually. For patients who tolerate the drug well, the dose may increase once every two weeks. For 6 weeks, it is brought to 25 mg. Receptions per day should be no more than two. It is recommended that an increase be made to the maximum doses tolerated by the patient. People whose body weight is less than 85 kg are allowed to prescribe 50 mg per day, more than 85 kg - not more than 100 mg.
- For arterial hypertension, it is recommended that tablets be taken from Carvedilol pressure once a day for 12-14 mg, or 6.25 mg twice for 7-14 days. After 1-2 weeks, the daily dosage should be increased to 25 mg.
If the patient interrupts therapy for 2 weeks or more, then it should be resumed according to the recommended schemes from the initial doses.
For elderly patients (over 70 years), the medicine is prescribed twice a day, while the daily dose should not exceed 25 mg.
The drug should be discontinued within 1-2 weeks, gradually reducing the dosage. If the patient misses the appointment, he should take the next dose in the near future. Doubling the dose is not acceptable.
Negative effects of the drug
The following negative effects may develop during the treatment with Carvedilol:
- Peripheral circulatory disorders, progression of heart failure, intermittent claudication, orthostatic hypotension, antrioventricular block, bradycardia, angina pectoris.
- Depression, paresthesia, syncope, sleep disturbances, dizziness, headache, muscle weakness.
- Increased activity of liver enzymes, abdominal pain, constipation, diarrhea, vomiting, dry mouth, nausea.
- Severe renal dysfunction, swelling.
- Thrombocytopenia, leukopenia.
- Shortness of breath, nasal congestion, bronchospasm, exacerbation of psoriasis, urticaria, rash, exanthema, itching, other allergic manifestations, sneezing.
- Decreased lacrimation, weight gain, flu-like syndrome, pain in the limbs.
The occurrence of this negative symptomatology is the basis for drug withdrawal, with their development it is important to seek medical advice.
Overdose
The main symptoms of an overdose are cardiogenic shock, bradycardia, a strong decrease in blood pressure, heart failure, cardiac arrest. In some cases, generalized convulsions, clouding of consciousness, respiratory failure, bronchospasm, and vomiting are observed.
With the onset of intoxication, the patient is hospitalized in intensive care. To eliminate the effects of intoxication, the introduction of sympathomimetics, atropine, glucagon is indicated.
If the main sign of intoxication is arterial hypotension, the patient should be given norepinephrine. With bronchospasm, the use of aerosol beta-adrenergic agonists or intravenous administration of aminophylline is recommended. Elimination of seizures is performed using diazepam.
From what tablets "Carvedilol" is now known.
Interaction with other medicines
Against the background of the use of the medication, intravenous use of verapamil and diltiazem is not allowed, since there is a risk of a decrease in heart rate and a significant decrease in blood pressure.
The effect of carvedilol is enhanced by the parallel use of antispasmodics, monoamine oxidase inhibitors, cardiac glycosides, other beta-blockers, anesthetics, antiarrhythmic drugs, antihypertensive, antianginal drugs.
When used simultaneously with Carvedilol:
- The plasma concentration of digoxin preparations increases.
- Cimetidine and other liver enzyme inhibitors increase the plasma concentration of carvedilol.
- Ergot alkaloids contribute to the deterioration of peripheral circulation.
- Rifampicin, phenobarbital, and other inducers of liver enzymes contribute to a decrease in the plasma concentration of carvedilol.
In addition, Carvedilol is able to enhance the effects of hypoglycemic drugs, mask the symptoms of hypoglycemia.
Analogs of tablets "Carvedilol"
If necessary, Carvedilol can be replaced by Talliton, Coriol, Credex, Carvidil, Kardivas, Carvedilol Sandoz, Carvedilol Zentiva, Carvedilol-Lugal, Carvedilol Hexal, Carvedilol -KV ”,“ Carvedilol Obolenskoye ”,“ Carvedilolom Canon ”,“ Carvedigamma, “Carvidex”, “Carvetrend”, “Vedikardol”, “Dilatrend”, “Aodak-AO”, “Amlodak-AO”, “Anaprilin”, “ Alotendin ”,“ Atram. ”
It is worth noting that each of these medicines has certain contraindications. The possibility of replacing the medicine must be approved by the doctor.
Cost of medicine
The cost of the drug depends on the number of tablets in the package and the manufacturer. The medicine is issued by the companies "Teva", "Canon", "Akrikhin", "Zentiva". The cost of a pharmaceutical product is on average 230 rubles.
What is the price of Carvedilol Canon tablets? The drug from this manufacturer can be purchased for 100 rubles. From 150 rubles costs “Carvedilol Akrikhin”. What are these pills from? All these tools are analogues of each other. And their testimony, respectively, is the same.
Reviews on Carvedilol tablets
Feedback on the experience of using the drug is quite controversial, but many patients note the high effectiveness of the drug. If the specialist has correctly selected the therapeutic regimen that the patient carefully observes, the drug can significantly improve the condition of patients who have had myocardial infarction, and greatly reduce the number of heart attacks. If prolonged remission is observed, the dosage of the drug is gradually reduced.
Patients note that basically the tablets are well tolerated, only in some cases negative symptoms develop. Separately, such a dignity of the drug as accessibility is distinguished - its cost is quite low, almost every patient can purchase it.
We examined how Carvedilol tablets help.