Carvedilol Canon pills 25mg, 30pcs

Composition

Tablets

Active ingredient:

carvedilol 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

Disorders of the blood and lymphatic system

Rare: 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) 1 time a day for the first 2 days of therapy, then 25 mg 1 time a day. If necessary, in the future, the dose can be incrAlthough 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