Concor, pills 10mg 30pcs

Composition

1 tablet contains:

Active ingredient:

bisoprolol fumarate 10 mg;

Auxiliary substances:  

colloidal silicon dioxide,

magnesium stearate,

crospovidone,

microcrystalline cellulose,

corn starch,

calcium hydrophosphate,

dimethicone 100,

macrogol 400,

iron oxide,

titanium oxide,

methylhydroxypropylcellulose.

Pharmacological action

Concor – antiarrhythmic, antihypertensive, antianginal.

Pharmacodynamics

Selective β_-1-adrenoblocker, without its own sympathomimetic activity, does not have a membrane-stabilizing effect. It has only a slight affinity for β2-adrenergic receptors of the smooth muscles of the bronchi and blood vessels, as well as for β2-adrenergic receptors involved in the regulation of metabolism. Therefore, bisoprolol generally does not affect the resistance of the respiratory tract and metabolic processes in which β2-adrenergic receptors are involved.

The selective effect of the drug on β1-adrenergic receptors remains beyond the therapeutic range.

Bisoprolol does not have a pronounced negative inotropic effect. The maximum effect of the drug is achieved 3-4 hours after ingestion. Even when bisoprolol is prescribed once a day, its therapeutic effect persists for 24 hours due to a 10-12-hour T_1/2 from blood plasma. As a rule, the maximum reduction is Blood pressure is reached 2 weeks after the start of treatment.

Bisoprolol reduces the activity of the sympathoadrenal system (SAS) by blocking the beta_-1-adrenergic receptors of the heart.

A single oral dose of bisoprolol reduces heart rate, reduces stroke volume, and consequently reduces ejection fraction and myocardial oxygen demand in patients with CHD without signs of CHF. With long-term therapy, the initially increased OPSS decreases. A decrease in the activity of renin in blood plasma is considered as one of the components of the antihypertensive effect of beta-blockers.

Pharmacokinetics

Suction. Bisoprolol is almost completely (>90%) absorbed from the gastrointestinal tract. Its bioavailability due to insignificant metabolism at the first passage through the liver (at about 10%) is about 90% after oral use. Food intake does not affect bioavailability. Bisoprolol demonstrates linear kinetics, and its plasma concentrations are proportional to the dose taken in the range from 5 to 20 mg. Cmax in blood plasma is reached after 2-3 hours.

Distribution. Bisoprolol is distributed fairly widely. V_d — 3.5 l / kg. Binding to plasma proteins reaches approximately 30%.

Metabolism. It is metabolized by the oxidative pathway without subsequent conjugation. All metabolites are polar (water-soluble) and excreted by the kidneys. The main metabolites found in blood plasma and urine do not show pharmacological activity. Data obtained from experiments with human liver microsomes in vitro show that bisoprolol is primarily metabolized by the CYP3A4 isoenzyme (about 95%), and the CYP2D6 isoenzyme plays only a minor role.

Output. The clearance of bisoprolol is determined by the balance between renal excretion unchanged (about 50%) and liver metabolism (about 50%) to metabolites that are then also excreted by the kidneys. The total ground clearance is 15 l/h. T_1/2 — 10-12 hours.

There is no information on the pharmacokinetics of bisoprolol in patients with CHF and concomitant hepatic or renal impairment.

Indications

Arterial hypertension, CHD, heart failure

Contraindications

• hypersensitivity to bisoprolol or any of the excipients (see “Composition”);
• acute heart failure, chronic heart failure decompensation requiring inotropic therapy;
• cardiogenic shock;
• AV blockade II and III degree, without pacemaker;
• the syndrome of weakness of the sinus node;
• sinoatrial block;
• bradycardia (heart rate <60 beats/min);
• severe hypotension (SBP <100 mm Hg. calendar);
• severe forms of bronchial asthma or chronic obstructive pulmonary disease;
• expressed by human peripheral blood circulation or Raynaud’s syndrome;
• pheochromocytoma (without the simultaneous application of α-blockers);
• metabolic acidosis;
• the age of 18 (there are insufficient data on efficacy and safety in this age group).

With caution:  desensitizing therapy, Prinzmetal angina, hyperthyroidism, type I diabetes mellitus and diabetes mellitus with significant fluctuations in blood glucose concentration, grade I AV blockage, severe renal failure (creatinine clearance

Side effects

From the central nervous system and peripheral nervous system:  possible (especially at the beginning of the course of treatment) feeling of fatigue, dizziness, headache, sleep disturbance, depression; rarely-hallucinations. Usually, these phenomena are mild and usually disappear within 1-2 weeks.

From the side of the visual organ:  rarely-visual impairment, reduced tear production (should be considered when wearing contact lenses), conjunctivitis.

From the cardiovascular system:  in some cases, orthostatic hypotension, bradycardia, impaired AV conduction, decompensation of heart failure with the development of peripheral edema; paresthesia and a feeling of cold in the extremities are possible. At the beginning of treatment, the condition may worsen in patients with intermittent claudication or with Raynaud’s syndrome.

Respiratory system disorders:  rarely-shortness of breath (in patients with a tendency to bronchospasm, including bronchitis with bronchoobstructive syndrome).

From the digestive system:  in some cases-diarrhea, constipation, nausea, abdominal pain, increased activity of liver enzymes in blood plasma (AST, ALT), hepatitis.

Musculoskeletal disorders:  in some cases-muscle weakness, muscle cramps, arthropathy with damage to one or more joints (mono – or polyarthritis).

From the endocrine system:  reduced glucose tolerance (in latent diabetes mellitus) and masked signs of hypoglycemia; in some cases, an increase in blood triglycerides.

From the side of the reproductive system:  in some cases – violation of potency.

Dermatological reactions:  itching is possible; rarely-redness of the skin, increased sweating, rash.

Interaction

Concor may increase the effect of antihypertensive drugs when used concomitantly.

Concor and reserpine, alpha-methyldopa, clonidine, digitalis preparations or guanfacine may cause a sharp decrease in heart rate.

With the simultaneous use of Concor and clonidine, digitalis preparations, as well as guanfacine, conduction disturbances are also possible.

Concor and sympathomimetics (including those contained in cough suppressants, nasal drops and eye drops) may reduce the effect of bisoprolol.

Concomitant use of nifedipine and other calcium channel blockers – dihydropyridine derivatives-may enhance the antihypertensive effect of Concor.

Concor and verapamil, or diltiazem and other antiarrhythmic drugs may cause a sharp decrease in blood pressure, a decrease in heart rate, and the development of arrhythmia and/or heart failure (careful medical supervision is required). Calcium channel blockers and antiarrhythmic drugs should not be administered intravenously during Concor therapy.

When Concor and clonidine are used simultaneously, the latter can only be discontinued if Concor has been discontinued several days before, due to the risk of an excessive increase in blood pressure.

Concomitant use of ergotamine derivatives (including ergotamine-containing drugs for the treatment of migraines) and Concor may increase peripheral circulatory disorders.

Concor and rifampicin concomitantly may cause a slight decrease in T1 / 2 bisoprolol (an increase in the Concor dose is usually not required).

Concomitant use of Concor and insulin or oral hypoglycemic agents may increase the hypoglycemic effect. Symptoms of hypoglycemia are masked or mitigated (regular monitoring of blood glucose levels is necessary).

How to take it, course of use and dosage

The drug is taken orally once a day. Tablets should be taken with a small amount of liquid in the morning before breakfast, during or after it. Tablets should not be chewed or ground into powder.

Arterial hypertension and angina pectoris

The dose is selected individually, primarily taking into account the patient’s heart rate and condition.

As a rule, the initial dose is 5 mg once a day. If necessary, the dose can be increased to 10 mg 1 time/day. In the treatment of arterial hypertension and angina pectoris, the maximum recommended dose is 20 mg once a day.

Chronic heart failure

The standard treatment regimen for chronic heart failure includes the use of ACE inhibitors or angiotensin II receptor antagonists (in case of intolerance to ACE inhibitors), beta-blockers, diuretics and, optionally, cardiac glycosides. At the beginning of treatment of chronic heart failure with Concor®, a special titration phase is required under regular medical supervision.

A prerequisite for treatment with Concor® is stable chronic heart failure without signs of exacerbation.

Concor® treatment begins according to the following titration schedule. However, individual adjustment may be required depending on how well the patient tolerates the prescribed dose, i. e. the dose can only be increased if the previous dose was well tolerated.

To ensure an appropriate titration process at the initial stages of treatment, it is recommended to use bisoprolol in the dosage form of 2.5 mg tablets.

The recommended starting dose is 1.25 mg 1 time/day. Depending on individual tolerance, the dose should be gradually increased to 2.5 mg,3.75 mg,5 mg,7.5 mg and 10 mg 1 time/day. Each subsequent dose increase should be carried out at least 2 weeks later. If an increase in the dose of the drug is poorly tolerated by the patient, then a reduction in the dose is possible.

The maximum recommended dose in the treatment of chronic heart failure is 10 mg 1 time/day.

During titration, regular monitoring of blood pressure, heart rate, and the severity of symptoms of chronic heart failure is recommended. Aggravation of the symptoms of the course of chronic heart failure is possible from the first day of using the drug.

If the patient does not tolerate the maximum recommended dose of the drug, then the possibility of gradually reducing the dose should be considered.

During or after the titration phase, the course of chronic heart failure, hypotension, or bradycardia may temporarily worsen. In this case, it is recommended, first of all, to adjust the doses of concomitant therapy. It may also be necessary to temporarily reduce the dose of Concor® or cancel it. After the patient’s condition stabilizes, the dose should be re-titrated or the treatment should be continued.

Duration of treatment for all indications

Concor® treatment is usually long-term.

Special patient groups

Patients with mild or moderate hepatic or renal impairment, as well as elderly patients, usually do not need to adjust the dosage regimen.

In patients with severe renal impairment (creatinine clearance less than 20 ml / min) and in patients with severe liver diseases, the maximum daily dose is 10 mg. Increasing the dose in such patients should be carried out with extreme caution.

Elderly patients do not need to adjust the dose.

Since there is insufficient data on the use of Concor® in children, it is not recommended to prescribe the drug to children under 18 years of age.

To date, there are insufficient data on the use of Concor® in patients with chronic heart failure in combination with type 1 diabetes mellitus, severe renal and/or liver dysfunction, restrictive cardiomyopathy, congenital heart defects or heart valve disease with severe hemodynamic disorders. Also, until now, insufficient data have been obtained on patients with chronic heart failure with myocardial infarction in the last 3 months.

Overdose

Symptoms: The most common symptoms are AV block, severe bradycardia, severe BP reduction, bronchospasm, acute heart failure, and hypoglycemia. Sensitivity to a single high dose of bisoprolol varies greatly among individual patients and is likely to be high in patients with chronic heart failure.

Treatment: if an overdose occurs, first of all, it is necessary to stop taking the drug and start supportive symptomatic therapy.

With severe bradycardia-IV use of atropine. If the effect is insufficient, then with caution you can enter a drug that has a positive chronotropic effect. Sometimes it may be necessary to temporarily install an artificial pacemaker.

With a pronounced decrease in blood pressure, intravenous use of plasma – substituting solutions and vasopressors is recommended.

With AV blockade-constant clinical monitoring, the appointment of beta-adrenomimetics, such as epinephrine. If necessary, an artificial pacemaker can be installed.

In case of exacerbation of the course of chronic heart failure-intravenous use of diuretics, drugs with a positive inotropic effect, as well as vasodilators.

With bronchospasm-the appointment of bronchodilators, including beta-2-adrenomimetics and / or aminophylline.

With hypoglycemia-intravenous use of dextrose (glucose).

Special instructions

Caution should be exercised in the treatment of patients with diabetes mellitus with significant fluctuations in blood glucose, since the symptoms of hypoglycemia can be masked; in the treatment of patients who adhere to a strict diet; in the treatment of patients with metabolic acidosis; in patients with a history of severe hypersensitivity reactions; in desensitizing therapy; in AV block I degree; in angiospastic angina pectoris (Prinzmetal angina pectoris).

In some cases, the use of beta-blockers (including Concor) can cause the development or worsening of the course of psoriasis or lead to the appearance of psoriatic rashes on the skin.

Against the background of taking beta-blockers, more severe forms of hypersensitivity reactions may occur.

When treated with beta-blockers, in some cases there is hair loss, hearing loss or tinnitus, weight gain, mood changes, short-term memory loss, allergic rhinitis.

Before performing surgery, you should inform the anesthesiologist about taking Concor.

Use in pediatrics

Concor should not be prescribed to children due to the lack of clinical experience of using the drug in this category of patients.

Influence on the ability to drive motor vehicles and manage mechanisms

The question of the possibility of engaging in potentially dangerous activities that require increased attention and speed of psychomotor reactions should be resolved only after evaluating the individual patient’s response to the drug (especially at the beginning of treatment or with simultaneous use of alcohol or ethanol-containing drugs).

Form of production

Tablets

Storage conditions

The drug should be kept out of the reach of children.

Shelf life

5 years

Active ingredient

Bisoprolol

Conditions of release from pharmacies

By prescription

Dosage form

Tablets