Coronal, pills 5mg, 100pcs

Composition

of 1 tab. :  bisoprolol fumarate – 5 mg

Auxiliary substances:

microcrystalline cellulose-133 mg,

corn starch-7.5 mg,

sodium lauryl sulfate-1 mg,

colloidal silicon dioxide-2 mg,

magnesium stearate-1.5 mg.

Composition of the film shell:

hypromellose – 6.4 mg,

macrogol 400-1.28 mg,

titanium dioxide (E 171) – 2.3 mg,

iron oxide yellow dye (E 172) – 20 mcg.

Pharmacological action

Selective beta_-1-adrenoblocker. Reduces the activity of plasma renin, reduces the need for myocardial oxygen, reduces heart rate (at rest and during exercise). It has antihypertensive, antiarrhythmic and antianginal effects. Blocking the beta-₁-adrenergic receptors of the heart in low doses, it reduces the catecholamine-stimulated formation of cAMP from ATP, reduces the intracellular flow of calcium ions, has a negative chrono -, dromo -, batmo-and inotropic effect (reduces heart rate, inhibits conduction and excitability, reduces myocardial contractility). When the dose is increased, it has a beta_-2-adrenoblocking effect.

OPSS at the beginning of the drug use, in the first 24 hours after oral use, increases (as a result of a reciprocal increase in the activity of α-adrenergic receptors and elimination of stimulation of β2-adrenergic receptors), which returns to its original value after 1-3 days, and decreases with prolonged use.

The antihypertensive effect is associated with a decrease in the minute blood volume, sympathetic stimulation of peripheral vessels, a decrease in the activity of RAAS (which is more important for patients with initial hypersecretion of renin) and the central nervous system, restoration of the sensitivity of the aortic arch baroreceptors (there is no increase in their activity in response to a decrease in blood pressure) and, as a result, a decrease in peripheral sympathetic influences. With arterial hypertension, the hypotensive effect develops in 2-5 days, and a stable effect-in 1-2 months.

The antianginal effect is due to a decrease in the myocardial oxygen demand as a result of a decrease in heart rate and contractility, an elongation of the diastole, an improvement in myocardial perfusion, and a decrease in myocardial sensitivity to the effects of sympathetic innervation. Reduces the number and severity of angina attacks and increases exercise tolerance. By increasing the final diastolic pressure in the left ventricle and increasing the stretching of the muscle fibers of the ventricles, oxygen demand may increase, especially in patients with chronic heart failure.

The antiarrhythmic effect is due to the elimination of arrhythmogenic factors (tachycardia, increased activity of the sympathetic nervous system, increased cAMP content, arterial hypertension), a decrease in the rate of spontaneous excitation of sinus and ectopic pacemakers, and a slowdown in AV conduction (mainly in the antegrade and, to a lesser extent, in the retrograde directions through the AV node) and conduction along additional pathways.

When used in medium therapeutic doses, unlike non-selective beta-blockers, it has a less pronounced effect on the organs containing beta_-2-adrenergic receptors (pancreas, skeletal muscles, smooth muscles of peripheral arteries, bronchi and uterus) and on carbohydrate metabolism, does not cause sodium ion retention in the body. When used in high doses (200 mg or more), it has a blocking effect on both subtypes of beta-adrenergic receptors, mainly in the bronchi and vascular smooth muscles.

Indications

-arterial hypertension—

– IHD: prevention of angina attacks.

Use during pregnancy and lactation

During pregnancy, Coronal is prescribed only for strict indications if the intended benefit to the mother exceeds the potential risk to the fetus.

72 hours before delivery, Coronal should be discontinued due to the possible development of bradycardia, hypotension, hypoglycemia and respiratory depression in the fetus/newborn.

If taking the drug Coronal is necessary during lactation, breastfeeding should be discontinued.

When taking bisoprolol during pregnancy, the fetus may have intrauterine growth retardation, hypoglycemia, and bradycardia.

Contraindications

— shock (including cardiogenic);

acute heart failure;

— chronic heart failure in the stage of decompensation;

— AV-block II and III degree (without an artificial pacemaker);

— sinoatrial block;

— SSSU;

— bradycardia;

— cardiomegaly (without signs of heart failure);

— arterial hypotension (systolic blood pressure below 100 mm Hg. St., especially in myocardial infarction);

— bronchial asthma and chronic obstructive pulmonary disease in the anamnesis;

— simultaneous reception of MAO inhibitors (except MAO inhibitors type);

— concomitant use floctafenine and sultopride;

— late stages of peripheral circulatory disorders;

— Raynaud’s disease;

— lactation period;

— age under 18 years (effectiveness and safety not established);

— hypersensitivity to the medication and other beta-blockers.

With caution, the drug should be prescribed for hepatic insufficiency, renal insufficiency (creatinine clearance less than 20 ml/min), metabolic acidosis, pheochromocytoma (with concomitant use of alpha-blockers), diabetes mellitus in the decompensation stage, AV block I degree, Prinzmetal angina pectoris, restrictive cardiomyopathy, congenital heart defects or heart valve defects with severe hemodynamic disorders, chronic heart failure with severe hemodynamic disorders. heart attack within the last 3 months, psoriasis, depression (including in the anamnesis), severe allergic reactions in the anamnesis, during pregnancy, with a strict diet, desensitizing immunotherapy with allergens and allergen extracts, as well as in elderly patients.

Side effects

The frequency of occurrence of side effects is determined as follows: very common (≥1/10), common (≥1/100 and

From the central nervous system:  infrequently – increased fatigue, asthenia, dizziness, headache, drowsiness or insomnia, depression; rarely-hallucinations, nightmares, convulsions.

From the side of the senses:  rarely-visual impairment, decreased lacrimal fluid secretion, dry and painful eyes, hearing impairment; very rarely – conjunctivitis.

From the cardiovascular system:  very often-sinus bradycardia; often-a decrease in blood pressure, angiospasm (increased peripheral circulatory disorders, cold of the lower extremities, paresthesia); infrequently – violation of AV conduction, orthostatic hypotension, decompensation of chronic heart failure, peripheral edema.

From the digestive system:  often – dryness of the oral mucosa, nausea, vomiting, diarrhea, constipation; rarely-hepatitis, increased activity of hepatic transaminases.

Respiratory system disorders:  infrequently-difficulty breathing when prescribed in high doses (loss of selectivity) and/or in predisposed patients – laryngo – and bronchospasm; rarely – nasal congestion, allergic rhinitis.

From the endocrine system:  rarely – hyperglycemia (in patients with type 2 diabetes mellitus), hypoglycemia (in patients receiving insulin).

Allergic reactions:  rarely – skin pruritus, rash, urticaria.

From the side of the skin:  rarely-increased sweating, hyperemia of the skin; very rarely-psoriasis-like skin reactions, exacerbation of psoriasis symptoms, alopecia.

Musculoskeletal disorders:  infrequently – muscle weakness, cramps in the calf muscles, arthralgia.

From the side of hematopoietic organs:  in some cases – thrombocytopenia, agranulocytosis.

Other services:  very rarely-violation of potency; rarely-hypertriglyceridemia, “withdrawal” syndrome (increased angina attacks, increased blood pressure).

Interaction

Allergens used for immunotherapy or allergen extracts for skin tests increase the risk of severe systemic allergic reactions or anaphylaxis in patients receiving bisoprolol.

When used concomitantly with Coronal, iodine-containing radiopaque drugs for intravenous use increase the risk of anaphylactic reactions.

When used concomitantly with Coronal phenytoin for intravenous use, drugs for inhaled general anesthesia (hydrocarbon derivatives) increase the severity of cardiodepressive effects and the likelihood of lowering blood pressure.

When used concomitantly, Coronal changes the effectiveness of insulin and oral hypoglycemic drugs, masks the symptoms of developing hypoglycemia (tachycardia, increased blood pressure).

When used concomitantly, Coronal reduces the clearance of lidocaine and xanthines (except diphylline) and increases their plasma concentrations, especially in patients with an initially increased clearance of theophylline under the influence of smoking.

NSAIDs (by delaying sodium ions and blocking prostaglandin synthesis by the kidneys), corticosteroids and estrogens (by delaying sodium ions) weaken the antihypertensive effect of Coronal.

When used concomitantly with Coronal, cardiac glycosides, methyldopa, reserpine and guanfacine, slow calcium channel blockers (verapamil, diltiazem), amiodarone and other antiarrhythmic drugs increase the risk of developing or exacerbating bradycardia, AV block, cardiac arrest and heart failure.

When used concomitantly with Coronal, nifedipine can lead to a significant decrease in blood pressure.

When used concomitantly with Coronal, diuretics, clonidine, sympatholytics, hydralazine and other antihypertensive drugs can lead to an excessive decrease in blood pressure.

Coronal prolongs the effect of non-depolarizing muscle relaxants and the anticoagulant effect of coumarins.

When used concomitantly with Coronal, tricyclic and tetracyclic antidepressants, antipsychotic drugs (neuroleptics), ethanol, sedatives and hypnotic drugs increase central nervous system depression, can provoke cardiac arrhythmias, bradycardia and orthostatic hypotension.

Concomitant use of Coronal with MAO inhibitors is not recommended due to a significant increase in the antihypertensive effect, a break in treatment between taking MAO inhibitors and Coronal should be at least 14 days.

When used concomitantly with Coronal, non-hydrogenated ergot alkaloids and ergotamine increase the risk of developing peripheral circulatory disorders.

When used concomitantly with Coronal, sulfasalazine increases the concentration of bisoprolol in plasma.

When used concomitantly with Coronal, rifampicin shortens the T 1/2 of bisoprolol.

There is a potential danger of an additive effect with the development of hypotension and / or significant bradycardia, when combined with beta-blockers for topical use (eye drops).

There is a decrease in the antihypertensive effect of the drug against the background of the use of epinephrine and norepinephrine.

The probability of violations of automatism, conduction and contractility of the heart increases (mutually) against the background of therapy with quinidine drugs (mefloquine, chloroquine).

In case of shock or hypotension caused by floctafenin, when used together, it is possible to reduce compensatory cardiovascular reactions.

When used concomitantly with baclofen or amifostine, an increase in antihypertensive effect is also noted.

How to take, course of use and dosage

For arterial hypertension and CHD (prevention of stable angina attacks) the initial dose is 2.5-5 mg 1 time/day. If necessary, the dose is increased to 10 mg 1 time/day. The maximum daily dose is 20 mg.

In patients with impaired renal function with creatinine clearance < 20 ml/min or with severe hepatic impairment, the maximum daily dose is 10 mg.

No dose adjustment is required in elderly patients.

Tablets should be taken orally, in the morning on an empty stomach, without chewing, with a small amount of liquid.

Overdose

Symptoms: arrhythmia, ventricular extrasystole, severe bradycardia, AV block, decreased blood pressure, acute heart failure, acrocyanosis, difficulty breathing, bronchospasm, dizziness, fainting, convulsions.

Treatment: it is necessary to wash the stomach and prescribe adsorbent drugs. Symptomatic therapy is carried out: if AV block develops, intravenous use of 1-2 mg of atropine, epinephrine or a temporary pacemaker; with ventricular extrasystole, intravenous lidocaine (Class I A drugs are not used); with a decrease in blood pressure, the patient should be in the Trendelenburg position; in the absence of symptoms of pulmonary edema, intravenous plasma-substituting solutions; if ineffective, use of epinephrine, dopamine, dobutamine (to maintain chrono – and intravenous inotropic effect and elimination of a pronounced decrease in blood pressure); in heart failure – cardiac glycosides, diuretics, glucagon; in convulsions – IV diazepam; in bronchospasm – beta – 2 – adrenostimulants by inhalation.

Special instructions

When prescribing Coronal, you should regularly monitor your heart rate and blood pressure (at the beginning of treatment – daily, then – 1 time in 3-4 months), conduct an ECG, and determine the blood glucose level in patients with diabetes mellitus (1 time in 4-5 months). In elderly patients, it is recommended to monitor renal function (1 time in 4-5 months).

The patient should be trained in the method of calculating heart rate and instructed about the need for medical consultation if the heart rate is less than 50 beats/min.

Before starting treatment, it is recommended to conduct a study of the function of external respiration in patients with a burdened bronchopulmonary history.

It should be taken into account that beta-blockers are ineffective in approximately 20% of patients with angina pectoris due to severe coronary atherosclerosis with a low ischemic threshold (heart rate less than 100 beats/min) and an increased end diastolic volume of the left ventricle, which disrupts subendocardial blood flow.

In smoking patients, the effectiveness of beta-blockers decreases.

Patients who use contact lenses should take into account that during treatment, there may be a decrease in the production of tear fluid.

When using Coronal in patients with pheochromocytoma, there is a risk of developing paradoxical arterial hypertension (if an effective alpha-adrenoblockade is not achieved beforehand).

Bisoprolol may mask certain clinical signs of thyrotoxicosis (for example, tachycardia). Abrupt withdrawal of Coronal in patients with thyrotoxicosis is contraindicated, since it can increase the symptoms of the disease.

In diabetes mellitus, bisoprolol can mask tachycardia caused by hypoglycemia. Unlike non-selective beta-blockers, it practically does not increase insulin-induced hypoglycemia and does not delay the restoration of blood glucose concentration to normal levels.

When used concomitantly with clonidine, the latter may be discontinued only a few days after discontinuation of Coronal.

It is possible to increase the severity of the hypersensitivity reaction and the lack of effect from conventional doses of epinephrine against the background of a burdened allergic history.

If elective surgical treatment is necessary, the drug is withdrawn 48 hours before the start of general anesthesia. If the patient took the drug before surgery, he should choose a drug for general anesthesia with minimal negative inotropic effect.

Reciprocal activation of the vagus nerve can be eliminated by intravenous use of atropine (1-2 mg).

Drugs that reduce the supply of catecholamines (including reserpine) can increase the effect of beta-blockers, so patients taking such combinations of drugs should be constantly monitored by a doctor for a pronounced decrease in blood pressure or bradycardia.

Patients with concomitant bronchospastic diseases can be prescribed cardioselective adrenoblockers in case of intolerance and / or ineffectiveness of other antihypertensive drugs. Overdose is dangerous for the development of bronchospasm.

If elderly patients develop increasing bradycardia (less than 50 beats / min), a marked decrease in blood pressure (systolic blood pressure below 100 mm Hg), AV-blockade, the dose should be reduced or treatment should be discontinued.

It is recommended to stop therapy if depression develops.

The drug should be discontinued before testing the content of catecholamines, normetanephrine, vanillinmindalic acid, and anti-nuclearbody titers in the blood and urine.

Do not abruptly interrupt treatment due to the risk of developing severe arrhythmias and myocardial infarction. Withdrawal is carried out gradually, reducing the dose for 2 weeks or more (the dose is reduced by 25% in 3-4 days).

Use in pediatrics

The use of Coronal in children and adolescents under 18 years of age is contraindicated, as efficacy and safety have not been established.

Influence on the ability to drive motor vehicles and manage mechanisms

During the treatment period, care should be taken when driving vehicles and engaging in other potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.

Form of production

Pills.

Storage conditions

The drug should be stored out of the reach of children at a temperature not exceeding 25°C.

Shelf

life is 3 years.

Active ingredient

Bisoprolol

Conditions of release from pharmacies

By prescription

Dosage form

Tablets