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Carvedilol

Obolensky OP
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2019-09-19
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Clinical Pharmacology

Carvedilol - alpha and beta adrenergic blocking drug with hypotensive, antioxidant and antianginal effect.

Has a combined non-selective beta-blocking, alpha1-blocking and antioxidant effects. The vasodilating effect is mainly associated with blockade of alpha1 receptors. Due to vasodilation, it reduces TPR. It has no intrinsic sympathomimetic activity and, like propranolol, has a membrane stabilizing effect.

Powerful antioxidant, eliminates free oxygen radicals. The combination of the vasodilating action and beta-blocking properties of carvedilol leads to the fact that in patients with arterial hypertension, a decrease in blood pressure is not accompanied by a simultaneous increase in OPSS, which is noted when taking beta-blockers. The heart rate decreases slightly, renal blood flow and renal function are preserved. Since peripheral blood flow persists, coldness of the extremities is very rare, in contrast to patients who are treated with beta-blockers.

The antihypertensive effect develops rapidly - 2-3 hours after a single dose and lasts for 24 hours. With prolonged treatment, the maximum effect is observed after 3-4 weeks. In patients with ischemic heart disease, carvedilol has anti-ischemic and antianginal effects. Reduces pre- and afterload on the heart. Does not have a pronounced effect on lipid metabolism and the content of potassium, sodium and magnesium ions in plasma. In patients with impaired left ventricular function and / or circulatory failure, the alpha1-adrenergic blocking action of carvedilol leads to the expansion of arterial and, to a lesser extent, venous vessels; carvedilol has a beneficial effect on hemodynamic parameters: it increases the ejection function of the left ventricle and reduces its size.

Carvedilol has a beneficial effect on heart hemodynamics and left ventricular ejection fraction both in dilated cardiomyopathy and in ischemic heart failure. With heart failure, end-systolic and end-diastolic volume decreases, as well as peripheral and pulmonary vascular resistance. The ejection fraction and cardiac index do not change during normal heart function.

It has been established that with additional prescription against the background of cardiac glycosides, ACE inhibitors and diuretics, carvedilol reduces the mortality rate, slows down the progression of the disease and improves the general condition of the patient, regardless of the severity of the disease. The effect of carvedilol is more pronounced in patients with tachycardia (heart rate more than 82 bpm) and low ejection fraction (less than 23%).

During treatment with carvedilol, the ratio of HDL / LDL cholesterol does not change.

Carvedilol is marketed under different brands and generic names, and comes in different dosage forms:

Brand nameManufacturerCountryDosage form
Carvedilol Obolensky OP Russia pills
Carvedilol Canonpharma Russia pills
Carvedilol-zentiva Zentiva KS Czech pills
Carvedilol Vertex Russia pills
Dilatrend Hoffmann la roch Switzerland pills
Carvedilol-teva Teva Israel pills
Carvedilol-Sandoz Sandoz Switzerland pills
Vedicardol Synthesis AKOMP Russia pills
Carvedilol Makiz-Pharma Russia pills

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Carvedilol

Dosage and Administration

Inside, regardless of the meal.
- Arterial hypertension
The recommended initial dose is 6.25 - 12.5 mg (1 tablet 6.25 mg or 1/2 pills 12.5 mg - 1 tablet 12.5) once a day during the first 2 days of therapy, then on 25 mg once a day. If necessary, further dose can be increased at intervals of at least 2 weeks, bringing to the maximum recommended dose of 50 mg 1 time per day (or divided into 2 doses).
Coronary heart disease
The recommended initial dose is 12.5 mg 2 times a day for the first 2 days, then 25 mg 2 times a day. If the antianginal effect is insufficient, the dose can be increased at intervals of at least 2 weeks, bringing to a higher daily dose of 100 mg divided into 2 doses.
- Chronic heart failure
The dose is selected individually, it is necessary to carefully monitor the doctor. In patients receiving cardiac glycosides, diuretics, and ACE inhibitors, their doses should be adjusted before starting treatment with Carvedilol Canon.
The recommended initial dose is 3.125 mg (1/2 pills of 6.25 mg) 2 times a day for 2 weeks. With good tolerance, the dose is increased at intervals of at least 2 weeks to 6.25 mg 2 times a day, then to 12.5 mg 2 times a day, then to 25 mg 2 times a day. The dose should be increased to a maximum dose that is well tolerated by the patient. The recommended maximum dose is 25 mg 2 times a day for all patients with severe chronic heart failure and for patients with mild and moderate degrees of chronic heart failure with a patient's body weight less than 85 kg. In patients with mild and moderate chronic heart failure and weighing more than 85 kg, the recommended maximum dose is 50 mg 2 times a day.
Before each increase in dose, an examination by a physician is necessary to identify the possible increase in symptoms of chronic heart failure or vasodilation. When a transient increase in symptoms of chronic heart failure or fluid retention in the body should increase the dose of diuretics, although sometimes you have to reduce the dose of the drug or temporarily cancel it.
Symptoms of vasodilation can be eliminated by reducing the dose of diuretics. If the symptoms persist, you can reduce the dose of the ACE inhibitor (if the patient is taking it), and then, if necessary, reduce the dose of the drug Carvedilol Canon. In such a situation, the dose of carvedilol canon should not be increased until the symptoms of exacerbated chronic heart failure or arterial hypotension improve.
If treatment with Carvedilol Canon is interrupted for more than 1 week, then its use is resumed at a lower dose, and then increased in accordance with the above recommendations.
If treatment with Carvedilol Canon is interrupted for more than 2 weeks, then its reappointment should be resumed from a dose of 3.125 mg (1/2 pills of 6.25 mg) 2 times a day, then the dose should be adjusted in accordance with the above recommendations.
Dosing in special patient groups
Renal dysfunction
In patients with moderate and severe renal failure, dose adjustment of the drug Carvedilol Canon is not required.
Liver dysfunction
Carvedilol Canon is contraindicated in patients with clinical manifestations of abnormal liver function (see section "Contraindications").
Elderly patients
Data that would dictate the need for dose adjustment are not available.

Adverse reactions

WHO classification of the incidence of side effects:
very often - ≥1 / 10 appointments (> 10%)
often from ≥1 / 100 to 1% and infrequently from ≥1 / 1000 to 0.1% and rarely from ≥1 / 10,000 to 0.01% and very rarely - The frequency of some undesirable effects such as dizziness, hypotension, bradycardia visual impairment is proportional to the size of the dose and often develops in patients with CHF. If serious adverse effects develop, treatment of the drug should be discontinued.
Violations of the blood and lymphatic system
Rarely: thrombocytopenia.
Very rare: leukopenia.
Endocrine Disorders
Often: in patients with existing diabetes mellitus - hyperglycemia or hypoglycemia, impaired glycemic control.
The presence of beta-adrenergic blocking properties of the drug does not exclude the possibility of latent diabetes mellitus manifestation, decompensation of already existing diabetes mellitus or suppression of the backsynular system.
Metabolic and nutritional disorders
Often: weight gain, hypercholesterolemia.
Nervous system disorders
Often: dizziness, headache (usually light and more common at the beginning of treatment), asthenia (including fatigue), depression.
Seldom: mood / thinking changes, sleep disturbance, paresthesia, loss of consciousness.
Violations by the organ of vision
Often: eye irritation, reduced tearing (pay attention when using contact lenses).
Very rare: visual impairment.
Violations of the cardiovascular system
Very often: orthostatic hypotension.
Often: bradycardia.
Rarely: impaired cardiac conduction, aggravation of angina, worsening of the clinical picture of heart failure (especially with increasing doses), pronounced decrease in blood pressure, heartbeat, fainting, cooling hands and feet, fluid retention, hypervolemia, edema (including generalized, peripheral, depending on body position, edema of the perineum, edema of the lower extremities).
Very rarely: syncopal states (including presyncopal), occlusive disorders of the peripheral circulation, exacerbation of the syndrome of "intermittent" claudication and Raynaud's syndrome.
Disorders of the respiratory system, organs of the chest and mediastinum
Rarely: bronchospasm and shortness of breath in predisposed patients, nasal congestion.
Very rarely: sneezing.
Disorders of the gastrointestinal tract
Often: nausea, diarrhea, abdominal pain, dryness of the oral mucosa.
Seldom: vomiting, loss of appetite, flatulence, constipation.
Very rarely: increased activity of liver transaminases - alanine aminotransferase (ALT), aspartate aminotransferase (AST) and gamma glutamyltransferase (GGT).
Violations of the skin and subcutaneous tissue
Very seldom: exacerbation of the course of psoriasis, exfoliative dermatitis, alopecia.
Disorders of the musculoskeletal and connective tissue
Rarely: male, pain in muscles, bones, spine.
Kidney and urinary tract disorders
Rarely: urination disorders, incontinence in women, reversible after discontinuation of the drug.
Very rare: renal failure and impaired renal function in patients with diffuse vasculitis and / or impaired renal function, edema.
Disorders of the genitals and breast
Infrequently: decrease in a potentiality.
General disorders and disorders at the site of administration
Often: general weakness.
Infrequently: hypersensitivity reaction (itchy skin, rash, urticaria).
Very rarely: "flushes" of blood to the skin of the face, flu-like syndrome.
Adverse reactions in patients with chronic heart failure
Nervous system disorders
Very often: dizziness, headache (usually light and arising at the beginning of treatment), asthenia (including fatigue), depression.
Violations of the cardiovascular system
Often: bradycardia, postural hypotension, marked reduction in blood pressure, edema (including generalized, peripheral, depending on body position, perineal edema, lower limb edema, hypervolemia, fluid retention).
Infrequently: syncopal states (including presinkopalnye), atrioventricular block and heart failure in the period of increasing doses.
Disorders of the gastrointestinal tract
Often: nausea, diarrhea, vomiting.
Violations of the blood and lymphatic system
Rarely: thrombocytopenia.
Very rare: leukopenia.
Metabolic and nutritional disorders
Often: weight gain, hypercholesterolemia; in patients with existing diabetes mellitus - hyperglycemia or hypoglycemia, a violation of carbohydrate metabolism.
Other violations
Often: visual impairment.
Rarely: renal failure and impaired renal function in patients with diffuse vasculitis and / or impaired renal function.

Contraindications

- Hypersensitivity to carvedilol or any component of the drug;
- acute and chronic heart failure in the decompensation stage, requiring intravenous administration of inotropic drugs;
- severe liver failure;
- atrioventricular block II and III degree (except for patients with an artificial pacemaker);
- severe bradycardia (heart rate less than 50 beats / min);
- sick sinus syndrome (including sinoauricular blockade);
- severe hypotension (systolic blood pressure less than 85 mm Hg. Art.);
- cardiogenic shock;
- severe forms of bronchial asthma or bronchospasm (in history);
- pheochromocytoma (without the simultaneous use of alpha-blockers);
- lactose intolerance, lactase deficiency, glucose-galactose malabsorption;
- terminal stage of occlusive peripheral vascular disease;
- age up to 18 years (efficacy and safety have not been established).
Carefully:
With caution, the drug is used for aggravated allergic history, chronic obstructive pulmonary disease (CAPD) patients, depression, myasthenia, hypoglycemia, atrioventricular blockade of the first degree, thyrotoxicosis, with extensive surgical interventions and general anesthesia, Princarmela syndrome, anesthesia, angina, stenocardia, Pristmetocosis, with extensive surgical interventions and general anesthesia, Pristroeksikoze, with extensive surgical interventions and general anesthesia, Princarmela, octomezia, with extensive surgical interventions and general anesthesia, with Pristinocardia, Pristmetosis, with extensive surgical interventions and general anesthesia, Pristroeksikoze, with extensive surgical interventions and conducting general anesthesia, Pristrokoksikoze, with extensive surgical interventions and general anesthesia, Princarmela syndrome, Ithromyopathy, with extensive surgical interventions and general anesthesia, with Pristinocardia Chytotoxicosis; with suspected pheochromocytoma, renal failure, psoriasis.

Drug interactions

At the same time taking carvedilola and digoxin, the concentration of the latter increases by about 15%. At the beginning of carvedilol therapy, when selecting its dose or discontinuation of the drug, regular monitoring of the concentration of digoxin in the blood plasma is recommended. At the same time, combination therapy with carvedilol and digoxin may lead to an additional slowdown of atrioventricular conductivity.
In connection with pronounced individual fluctuations in the concentration of cyclosporine, careful monitoring of its concentration is recommended after initiating carvedilol therapy and, if necessary, a corresponding adjustment in the daily dose of cyclosporine. In the case of intravenous administration of cyclosporine, no interaction with carvedilol is expected.
Rifampicin reduces plasma concentrations of carvedilol, leading to a decrease in its antihypertensive effect.
Fluoxetine, ketoconazole, cimetidine, haloperidol enhance the hypotensive effect of carvedilol.
Carvedilol may enhance the hypoglycemic effect of insulin or hypoglycemic agents for oral administration. When taken together, it is recommended to regularly monitor blood glucose concentrations.
Patients taking both carvedilol and catecholamine-lowering drugs (for example, reserpine and monoamine oxidase inhibitors) should be closely monitored for the risk of arterial hypotension and / or severe bradycardia.
In patients with heart failure, concomitant use of carvedilol with amiodarone or other antiarrhythmic agents is associated with the risk of an increase in beta-adrenoceptor blocking action. However, amiodarone may increase the risk of AV conduction disturbances.
The simultaneous use of carvedilol with clonidine can potentiate the antihypertensive and bradycarditis effect.If it is planned to discontinue the combination therapy with these drugs, carvedilol should be abolished first, and clonidine after a few days, gradually reducing its dose.
Simultaneous administration of blockers of “slow” calcium channels (BCCA) of the verapamil type, diltiazem with carvedilol may increase the risk of atrioventricular conduction disturbance. It is recommended that carvedilol should be prescribed with BMCC under the control of ECG and blood pressure.
Carvedilol may enhance the effects of other concomitant antihypertensive drugs (for example, alpha1-blockers) or drugs that cause hypotension as a side effect.
for general anesthesia, the negative inotropic and hypotensive effect of carvedilol is enhanced.
Non-steroidal anti-inflammatory drugs (NSAIDs) reduce the antihypertensive effect of carvedilol.
Bronchodilators (beta-adrenoreceptor agonists). Since non-cardio selective beta-blockers interfere with the bronchodilating effect of bronchodilators, which are beta-adrenoreceptor stimulants, careful monitoring of patients receiving these drugs is necessary.

Special instructions

Chronic heart failure.
In patients with chronic heart failure during the selection of the dose of the drug may be an increase in symptoms of chronic heart failure or fluid retention. If such symptoms occur, it is necessary to increase the dose of diuretics and not to increase the dose of the drug until the hemodynamic parameters stabilize. Sometimes it is necessary to reduce the dose of the drug Carvedilol Canon or, in rare cases, temporarily cancel the drug. Such episodes do not impede the further proper selection of the dose of the drug Carvedilol Canon.
Carvedilol Canon is used with caution in combination with cardiac glycosides (excessive AV conduction may be slowed down).
At the beginning of therapy with Carvedilol Canon or with an increase in the dose of the drug in patients, especially the elderly, there may be an excessive decrease in blood pressure, predominantly when going from a “lying” to a “standing” position. Correction of the dose of the drug.
Kidney function in chronic heart failure.
Carvedilol canon was prescribed to patients with chronic heart failure and low blood pressure (systolic blood pressure less than 100 mmHg), coronary heart disease and diffuse vascular changes and / or renal insufficiency showed a reversible deterioration in renal function. The dose of the drug is selected depending on the functional state of the kidneys.
It is recommended to monitor renal function in patients with chronic renal failure, arterial hypotension and chronic heart failure.
COPD
Patients with COPD, including those with bronchospastic syndrome who are not receiving oral or inhaled anti-asthma drugs, are prescribed Carvedilol Canon only if the possible benefits of its use outweigh the potential risk. If there is an initial predisposition to the bronchospastic syndrome, while taking Carvedilol Canon, as a result of an increase in airway resistance, shortness of breath may develop. At the beginning of the reception and with an increase in the dose of the drug Carvedilol Canon, these patients should be carefully observed, reducing the dose of the drug when the initial signs of bronchospasm appear.
Diabetes.
With caution, the drug is prescribed to patients with diabetes mellitus, since it can mask or alleviate the symptoms of hypoglycemia (especially tachycardia). In patients with chronic heart failure and diabetes, use of the drug Carvedilol Canon can be accompanied by impaired glycemic control.
Peripheral vascular disease.
Caution is needed when prescribing Carvedilol Canon for patients with peripheral vascular diseases, including Raynaud's syndrome, since beta-blockers may increase the symptoms of arterial insufficiency.
Thyrotoxicosis.
Like other beta-blockers, Carvedilol Canon can reduce the severity of thyrotoxicosis symptoms.
General anesthesia and extensive surgical interventions.
Caution is required in patients undergoing surgery under general anesthesia because of the possibility of the summation of the negative effects of carvedilol and agents for general anesthesia.
Bradycardia.
Carvedilol Canon can cause bradycardia. When reducing heart rate less than 55 beats / min, the dose of the drug should be reduced.
Hypersensitivity.
Care must be taken when prescribing Carvedilol Canon to patients with anamnestic indications of severe hypersensitivity reactions or undergoing desensitization, as beta-blockers may increase sensitivity to allergens and the severity of anaphylactic reactions.
Psoriasis.
Patients with anamnestic indications of the occurrence or aggravation of the course of psoriasis with the use of beta-blockers, carvedilol canon can only be prescribed after a careful analysis of the possible benefits and risks.
Pheochromocytoma.
Patients with pheochromocytoma prior to the use of any beta-blocker must be assigned an alpha blocker. Although carvedilol has both beta and alpha-adrenergic blocking properties, such patients have no experience with it, so it should be prescribed with caution to patients with suspected pheochromocytoma.
Angina Prinzmetala.
Non-selective beta-blockers can cause pain in patients with Prinzmetal angina. Experience patients carvedilola no these patients. Although its alpha-adrenergic blocking properties can prevent similar symptoms, Carvedilol Canon should be prescribed in such cases with caution.
Contact lenses.
Patients using contact lenses should be aware of the possibility of reducing the amount of tear fluid.
The syndrome of "cancel".
Treatment with carvedilol canon is carried out for a long time. It should not be stopped abruptly, it is necessary to gradually reduce the dose of the drug at intervals of 1-2 weeks. This is especially important in patients with ischemic heart disease.
If it is necessary to perform a surgical procedure with the use of general anesthesia, it is necessary to warn the anesthesiologist about the previous therapy with Carvedilol Canon.
During treatment, alcohol is excluded.
Influence on the ability to drive vehicles and mechanisms:
Care must be taken when driving vehicles and occupations of potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions, due to the fact that dizziness may develop.

Overdosage

Symptoms: marked reduction in blood pressure, bradycardia, heart failure, cardiogenic shock, cardiac arrest; respiratory disorders, bronchospasm, vomiting, confusion, and generalized convulsions are possible.
Treatment: in addition to general measures, it is necessary to monitor and correct vital signs, if necessary in the intensive care unit. You can use the following activities:
- Lay the patient on his back with raised legs;
- with severe bradycardia - atropine 0.5-2 mg intravenously;
- for maintenance of cardiovascular activity - glucagon 1-10 mg intravenously in a stream, then 2-5 mg per hour in the form of a long-term infusion;
- sympathomimetics (dobutamine, isoprenaline, orciprenaline or epinephrine (adrenaline)) in various doses, depending on body weight and the response to the treatment.
If a marked reduction in blood pressure dominates in the clinical picture of overdose, norepinephrine (norepinephrine) is administered; it is prescribed under conditions of continuous monitoring of blood circulation parameters. In case of treatment-resistant bradycardia, the use of an artificial pacemaker is indicated. In case of bronchospasm, beta-adrenomimetics are administered in the form of an aerosol (with intravenous inefficiency) or aminophylline intravenously. For convulsions, diazepam or clonazepam is slowly administered intravenously. Since severe overdose with symptomatic shock may prolong the half-life of carvedilol and remove the drug from the depot, it is necessary to continue maintenance therapy for a sufficiently long time. The duration of maintenance / detoxification therapy depends on the severity of the overdose, it should be continued until the patient’s clinical condition stabilizes.

  • Brand name: Carvedilol
  • Active ingredient: Carvedilol
  • Manufacturer: Obolensky OP
  • Country of Origin: Russia

Studies and clinical trials of Carvedilol (Click to expand)

  1. Carvedilol-induced myoclonus
  2. Saturable Enantioselective First-pass Effect for Carvedilol after High Oral Racemate Doses in Rats
  3. Carvedilol Stereopharmacokinetics in Rats: Affinities to Blood Constituents and Tissues
  4. Stereoselective analysis of carvedilol in human plasma and urine using HPLC after chiral derivatization
  5. Determination of trace carvedilol by solid substrate–room temperature phosphorimetry, based on its activating effect on hypochlorite-oxidizing amaranth using sodium dodecyl benzene sulphonate as sensitizer
  6. Enantioselective bioanalysis of beta-blocking agents: Focus on atenolol, betaxolol, carvedilol, metoprolol, pindolol, propranolol and sotalol
  7. Structural determination of glucuronide conjugates and a carbamoyl glucuronide conjugate of carvedilol: Use of acetylation reactions as an aid to determine positions of glucuronidation
  8. ChemInform Abstract: A Facile Synthesis of Carvedilol, β-Adrenergic Blocking Agent, via a Key 5-Substituted-2-oxazolidinone Intermediate.
  9. ChemInform Abstract: Synthesis of Active Metabolites of Carvedilol, an Antihypertensive Drug.
  10. Stereoselective effects of (R)- and (S)-carvedilol in humans
  11. The interaction of the enantiomers of carvedilol with α1- and β1-adrenoceptors
  12. Stereoselective disposition and tissue distribution of carvedilol enantiomers in rats
  13. Rats with portacaval shunt as a potential experimental pharmacokinetic model for liver cirrhosis: Application to carvedilol stereopharmacokinetics
  14. Mechanism of carvedilol-induced block of delayed rectifier K+ current in the NG108-15 neuronal cell line
  15. Electrochemical Behavior of Carvedilol and Its Adsorptive Stripping Determination in Dosage Forms and Biological Fluids
  16. Randomized comparison of long-term carvedilol and propranolol administration in the treatment of portal hypertension in cirrhosis
  17. Randomized controlled trial of carvedilol versus variceal band ligation for the prevention of the first variceal bleed
  18. Carvedilol versus variceal band ligation for prevention of the first variceal bleed
  19. Carvedilol for portal hypertension in patients with cirrhosis
  20. Carvedilol, a new nonselective beta-blocker with intrinsic anti-alpha1-adrenergic activity, has a greater portal hypotensive effect than propranolol in patients with cirrhosis
  21. Carvedilol—A new nonselective beta blocker
  22. Theoretical Parameters to Characterize Antioxidants. Part 2. The cases of melatonin and carvedilol
  23. Synthesis of the enantiomers and three racemic metabolites of carvedilol labeled to high specific activity with tritium

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