Carvedilol Canon pills 6.25mg, 30pcs

Composition

Tablets

Active ingredient:

carvedilol 6.25 mg;

Auxiliary substances:

calcium hydrophosphate dihydrate 70 mg,

hyprolose (hydroxypropylcellulose) 5.3 mg,

croscarmellose sodium (primellose) 4.5 mg,

lactose monohydrate (milk sugar) 93.7 mg,

magnesium stearate 1.5 mg

Pharmacological action

Antihypertensive agent from the group of alpha-and beta-blockers without internal sympathomimetic activity. Blocks α1 -, β1-and β2-adrenergic receptors. As a result of blockade of β1-adrenergic receptors, it moderately reduces the conductivity, strength and heart rate, without causing a sharp bradycardia. As a result of blockade of α1-adrenergic receptors, it causes dilation of peripheral blood vessels. As a result of the blockade of beta-2-adrenergic receptors, the tone of the bronchi, some vessels of the microcirculatory bed, as well as the tone and peristalsis of the intestine can slightly increase.

Pharmacokinetics

After oral use, it is rapidly and almost completely absorbed from the gastrointestinal tract. Cmax in blood plasma is reached within 1 h. Bioavailability is 25%.

Binding to plasma proteins is 98-99%. Vd – about 2 l / kg. Penetrates the placental barrier, is excreted in breast milk. Undergoes the “first pass” effect through the liver. Metabolites have a pronounced antioxidant and adrenoblocking effect.

T1 / 2 – 6-10 hours Plasma clearance – 590 ml/min. It is mainly excreted in the bile.

In patients with impaired liver function, bioavailability may increase by up to 80%.

Indications

• Arterial hypertension.
• IHD: prevention of stable angina attacks.
• Chronic heart failure (as part of combination therapy).

Contraindications

AV block II and III degrees, severe bradycardia, decompensated heart failure, shock, bronchial asthma, chronic lung diseases with a history of bronchial obstructive syndrome, liver failure, pregnancy, lactation, hypersensitivity to carvedilol.

Side effects

Blood and lymphatic system disorders Rarely: thrombocytopenia. Very rare: leukopenia.

Endocrine system disorders Often: in patients with pre-existing diabetes mellitus-hyperglycemia or hypoglycemia, violation of glycemic control. The presence of beta-blocking properties in the drug does not exclude the possibility of manifestation of latent diabetes mellitus, decompensation of existing diabetes mellitus, or suppression of the contrinsular system.

Metabolic and nutritional disorders often: weight gain, hypercholesterolemia.

Nervous system disorders often: dizziness, headache (usually mild and occurring more often at the beginning of treatment), asthenia (including increased fatigue), depression. Rare: changes in mood/thinking, sleep disorders, paresthesia, loss of consciousness.

Visual disturbances Often: eye irritation, reduced tear production (pay attention when using contact lenses). Very rare: visual impairment.

Disorders of the cardiovascular system are very common: orthostatic hypotension. Common: bradycardia. Rarely: impaired cardiac conduction, worsening of angina pectoris, worsening of the clinical picture of heart failure (especially with increasing dose), marked decrease in blood pressure, palpitation, fainting, cold hands and feet, fluid retention, hypervolemia, edema (including generalized, peripheral, position-dependent, perineal edema, edema of the lower extremities). Very rare: syncopal conditions (including presyncopal), occlusive disorders of peripheral blood circulation, exacerbation of intermittent claudication syndrome and Raynaud’s syndrome.

Respiratory, thoracic and mediastinal disorders Rarely: bronchospasm and shortness of breath in predisposed patients, nasal congestion. Very rare: sneezing.

Disorders of the gastrointestinal tract Often: nausea, diarrhea, abdominal pain, dryness of the oral mucosa. Rare: vomiting, decreased appetite, flatulence, constipation. Very rare: increased activity of “hepatic” transaminases-alanine aminotransferase (ALT), aspartate aminotransferase (AST) and gamma-glutamyltransferase (GGT).

Skin and subcutaneous tissue disorders are very rare: exacerbation of psoriasis, exfoliative dermatitis, alopecia.

Musculoskeletal and connective tissue disorders: myasthenia gravis, muscle, bone, and spine pain.

Renal and urinary tract disorders Rarely: impaired urination, cases of urinary incontinence in women, reversible after discontinuation of the drug. Very rare: renal insufficiency and impaired renal function in patients with diffuse vasculitis and / or impaired renal function, edema.

Disorders of the genitals and mammary gland often: reduced potency.

General disorders and disorders at the injection site often: general weakness. Infrequently: hypersensitivity reaction (pruritus, rash, urticaria). Very rare: “hot flashes” of blood to the skin of the face, flu-like syndrome.

Adverse reactions in patients with chronic heart failure

Nervous system disorders are very common: dizziness, headache (usually mild and occurring at the beginning of treatment), asthenia (including increased fatigue), depression.

Disorders of the cardiovascular system often: bradycardia, postural hypotension, marked decrease in blood pressure, edema (including generalized, peripheral, depending on the body position, perineal edema, edema of the lower extremities, hypervolemia, fluid retention). Infrequently: syncopal conditions (including presyncopal), atrioventricular block and heart failure during the period of increasing the dose.

Disorders of the gastrointestinal tract Often: nausea, diarrhea, vomiting.

Blood and lymphatic system disorders Rarely: thrombocytopenia. Very rare: leukopenia.

Metabolic and nutritional disorders Often: weight gain, hypercholesterolemia; in patients with pre – existing diabetes mellitus-hyperglycemia or hypoglycemia, impaired carbohydrate metabolism.

Other disorders often: visual disturbances. Rare: renal insufficiency and impaired renal function in patients with diffuse vasculitis and / or impaired renal function.

Interaction

With simultaneous use of carvedilol and digoxin, the concentration of the latter increases by about 15%. At the beginning of carvedilol therapy, when selecting its dose or discontinuing the drug, it is recommended to regularly monitor the concentration of digoxin in the blood plasma. However, combination therapy with carvedilol and digoxin may lead to an additional slowing of atrioventricular conduction.

Due to pronounced individual fluctuations in the concentration of cyclosporine, careful monitoring of its concentration is recommended after starting carvedilol therapy and, if necessary, appropriate adjustment of the daily dose of cyclosporine. In the case of intravenous 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 increase the hypoglycemic effect of insulin or oral hypoglycemic agents. When taken together, regular monitoring of blood glucose concentration is recommended.

Patients taking carvedilol concomitantly with drugs that reduce the content of catecholamines (for example, reserpine and monoamine oxidase inhibitors) should be closely monitored due to the risk of 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 increasing the beta-blocking effect. However, amiodarone may increase the risk of impaired AV conduction.

Concomitant use of carvedilol with clonidine may potentiate the antihypertensive and bradycardic effects. If you plan to stop combination therapy with these drugs, you should first cancel carvedilol, and after a few days – clonidine, gradually reducing its dose.

Concomitant use of slow calcium channel blockers (BCCs) such as verapamil, diltiazem and carvedilol may increase the risk of atrioventricular conduction disorders. use of carvedilol together with BMCC is recommended to be carried out under the control of ECG and blood pressure.

Carvedilol may increase the effect of other concomitant antihypertensive agents (for example, alpha% ^% 1-blockers) or drugs that cause arterial hypotension as a side effect. for general anesthesia, the negative inotropic and hypotensive effect of carvedilol is enhanced.

Nonsteroidal anti-inflammatory drugs (NSAIDs) reduce the antihypertensive effect of carvedilol.

Bronchodilators (beta-adrenergic agonists). Since non-cardioselective beta-blockers prevent the bronchodilating effect of bronchodilators that are beta-adrenergic stimulants, careful monitoring of patients receiving these drugs is necessary.

How to take it, course of use and dosage

Inside, regardless of food intake, with a sufficient amount of liquid.

– Arterial hypertension

The recommended initial dose is 6.25-12.5 mg (1 tablet of 6.25 mg or 1/2 tablet of 12.5 mg – 1 tablet of 12.5) once a day for the first 2 days of therapy, then 25 mg once a day. If necessary, in the future, the dose can be increased at intervals of at least 2 weeks, bringing up to the maximum recommended dose of 50 mg once a day (or divided into 2 doses).

Coronary heart disease

The recommended starting dose is 12.5 mg twice daily for the first 2 days, followed by 25 mg twice daily. If the antianginal effect is insufficient, the dose can be increased at intervals of at least 2 weeks, bringing it to the highest 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 starting dose is 3.125 mg (1/2 tablet of 6.25 mg) 2 times a day for 2 weeks. With good tolerability, 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 the maximum dose that is well tolerated by the patient. The recommended maximum dose is 25 mg twice daily for all patients with severe chronic heart failure and for patients with mild to moderate chronic heart failure with a patient’s body weight of less than 85 kg. In patients with mild to moderate chronic heart failure and a body weight of more than 85 kg, the recommended maximum dose is 50 mg 2 times a day.

Before each dose increase, a doctor’s examination is necessary to detect a possible increase in symptoms of chronic heart failure or vasodilation. If there is a transient increase in symptoms of chronic heart failure or fluid retention in the body, the dose of diuretics should be increased, although sometimes it is necessary to reduce the dose of the drug or temporarily cancel it.

Symptoms of vasodilation can be eliminated by reducing the dose of diuretics. If symptoms persist, you can reduce the dose of an ACE inhibitor (if the patient is taking it), and then, if necessary, reduce the dose of Carvedilol Canon. In this situation, the dose of Carvedilol Canon should not be increased until the symptoms of worsening chronic heart failure or 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 recommendations given above.

If treatment with Carvedilol Canon is interrupted for more than 2 weeks, then its repeated use should be resumed with a dose of 3.125 mg (1/2 tablet of 6.25 mg) 2 times a day, then the dose is selected in accordance with the above recommendations.

Dosage for special patient groups

Impaired renal function

In patients with moderate to severe renal insufficiency, no dose adjustment of Carvedilol Canon is required.

Impaired liver function

Carvedilol Canon is contraindicated in patients with clinical manifestations of impaired liver function (see the section “Contraindications”).

Elderly patients

There are no data that would dictate the need for dose adjustment.

Overdose

Symptoms: marked decrease in blood pressure, bradycardia, heart failure, cardiogenic shock, cardiac arrest; possible respiratory disorders, bronchospasm, vomiting, confusion and generalized convulsions.

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 events::- lay the patient on his back with his legs raised;- with severe bradycardia – atropine 0.5-2 mg intravenously; – to maintain cardiovascular activity-glucagon 1-10 mg intravenously jet, then 2-5 mg per hour in the form of a long infusion; – sympathomimetics (dobutamine, isoprenaline, orciprenaline or epinephrine (epinephrine)) in different doses, depending on body weight and response to treatment. If the clinical picture of an overdose is dominated by a pronounced decrease in blood pressure, norepinephrine (norepinephrine) is administered; it is prescribed in conditions of continuous monitoring of blood circulation parameters. In treatment-resistant bradycardia, the use of an artificial pacemaker is indicated. With bronchospasm, beta-adrenomimetics are administered in the form of an aerosol (if ineffective, intravenously) or aminophylline intravenously. For convulsions, diazepam or clonazepam is slowly administered intravenously. Since severe overdose with shock symptoms 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 and should be continued until the patient’s clinical condition stabilizes.

Special instructions

Chronic heart failure.

Patients with chronic heart failure may experience increased symptoms of chronic heart failure or fluid retention during the dose adjustment period. If such symptoms occur, it is necessary to increase the dose of diuretics and not increase the dose of the drug until the hemodynamic parameters stabilize. Sometimes it is necessary to reduce the dose of Carvedilol Canon or, in rare cases, temporarily discontinue the drug. Such episodes do not prevent further correct selection of the dose of Carvedilol Canon.

Carvedilol Canon is used with caution in combination with cardiac glycosides (excessive slowing of AV conduction is possible).

At the beginning of therapy with Carvedilol Canon or with an increase in the dose of the drug, patients, especially the elderly, may experience an excessive decrease in blood pressure, mainly during the transition from the “lying” position to the “standing”position. It is necessary to adjust the dose of the drug.

Kidney function in chronic heart failure.

When Carvedilol Canon was prescribed to patients with chronic heart failure and low blood pressure (systolic blood pressure less than 100 mm Hg), coronary heart disease, diffuse vascular changes and/or renal failure, reversible deterioration of renal function was noted. 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 do not receive oral or inhaled anti-asthmatic drugs, Carvedilol Canon is prescribed only if the possible benefits of its use outweigh the potential risk. If there is an initial predisposition to bronchospastic syndrome when taking Carvedilol Canon, shortness of breath may develop as a result of increased airway resistance. These patients should be carefully monitored at the beginning of Carvedilol Canon use and when increasing the dose, reducing the dose of the drug when the initial signs of bronchospasm appear.

Diabetes mellitus.

Caution should be exercised when prescribing the drug to patients with diabetes mellitus, as it may mask or reduce the symptoms of hypoglycemia (especially tachycardia). In patients with chronic heart failure and diabetes mellitus, the use of Carvedilol Canon may be accompanied by impaired glycemic control.

Peripheral vascular diseases.

Caution should be exercised when prescribing Carvedilol Canon to patients with peripheral vascular diseases, including Raynaud’s syndrome, since beta-blockers can 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 procedures.

Caution is required in patients undergoing surgery under general anesthesia, due to the possibility of combining the negative effects of carvedilol and general anesthesia agents.

Bradycardia.

Carvedilol Canon can cause bradycardia. If the heart rate is reduced to less than 55 beats / min, the dose of the drug should be reduced.

Hypersensitivity.

Caution should be exercised when prescribing Carvedilol Canon to patients with a history of severe hypersensitivity reactions or undergoing desensitization, since beta-blockers can increase sensitivity to allergens and the severity of anaphylactic reactions.

Psoriasis.

In patients with a history of psoriasis occurrence or exacerbation when using beta-blockers, Carvedilol Canon should be prescribed only after a thorough analysis of the possible benefits and risks. Pheochromocytoma.

Patients with pheochromocytoma should be prescribed an alpha-blocker before starting any beta-blocker. Although carvedilol has both beta-and alpha-blocking properties, there is no experience of its use in such patients, so it should be prescribed with caution to patients with suspected pheochromocytoma.

Prinzmetal angina pectoris.

Non-selective beta-blockers may cause pain in patients with Prinzmetal angina. There is no experience in prescribing carvedilol to these patients.Although its alpha-blocking properties may prevent such symptoms, Carvedilol Canon should be prescribed with caution in such cases.

Contact lenses.

Patients who use contact lenses should be aware of the possibility of reducing the amount of tear fluid.

Withdrawal syndrome.

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 coronary heart disease. If it is necessary to perform surgical intervention using general anesthesia, it is necessary to warn the anesthesiologist about previous therapy with Carvedilol Canon.

During the treatment period, alcohol consumption is excluded.

Influence on the ability to drive vehicles and mechanisms:

Caution should be exercised when driving vehicles and engaging in potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions, due to the fact that dizziness may develop.

Active ingredient

Carvedilol

Conditions of release from pharmacies

By prescription

Dosage form

Tablets