Coronal, 5 mg 100 pcs

A selective beta₁-adrenoblocker. Reduces plasma renin activity, reduces myocardial oxygen demand, reduces HR (at rest and under load). It has antihypertensive, antiarrhythmic and antianginal effects. In low doses it blocks β₁-adrenoceptors of heart, reduces catecholamine-stimulated formation of cAMP from ATP, decreases intracellular calcium ion current, produces negative chrono-, dromo-, batmo- and inotropic effect (decreases heart rate, inhibits conduction and excitability, reduces myocardial contractility). With increasing dose has beta₂-adrenoblocking effect.

The HRP at the beginning of the drug administration, in the first 24 hours after oral administration, increases (as a result of reciprocal increase of α-adrenoreceptor activity and elimination of β₂-adrenoreceptor stimulation) which returns to baseline after 1-3 days, and decreases with prolonged administration.

The antihypertensive effect is associated with the reduction of the minute blood volume, sympathetic stimulation of peripheral vessels, reduction of the RAAS activity (of greater importance for patients with initial renin hypersecretion) and CNS, restoration of aortic arch baroreceptors sensitivity (their activity in response to BP decrease is not increased) and finally reduction of peripheral sympathetic effects. In arterial hypertension hypotensive effect develops in 2-5 days, stable effect – in 1-2 months.

The antianginal effect is caused by decrease of myocardial oxygen demand as a result of HR shortening and decrease of contractility, prolongation of diastole, improvement of myocardial perfusion and decrease of myocardial sensitivity to sympathetic innervation. It reduces the number and severity of angina attacks and increases exercise tolerance. By increasing left ventricular end-diastolic pressure and increasing ventricular muscle fiber stretch, oxygen demand may increase, especially in patients with chronic heart failure.

. Antiarrhythmic action is caused by the removal of arrhythmogenic factors (tachycardia, increased activity of the sympathetic nervous system, increased content of CAMF, arterial hypertension), the decrease of spontaneous excitation rate of sinus and ectopic pacemakers and slowing of AV conduction (mainly in antegrade and, to a lesser extent, in retrograde direction through AV node) and conduction through additional pathways.

When used in medium therapeutic doses, unlike non-selective beta-adrenoblockers, it has less pronounced effect on organs containing β₂-adrenoreceptors (pancreas, skeletal muscles, smooth muscles of peripheral arteries, bronchi and uterus) and on carbohydrate metabolism, does not cause retention of sodium ions in the body. When used in high doses (200 mg and more) it has a blocking effect on both subtypes of β-adrenoreceptors, mainly in the bronchi and vascular smooth muscle.

Indications

– arterial hypertension;

– CHD: prevention of angina attacks.

Active ingredient

How to take, the dosage

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

In patients with impaired renal function at CKR < 20 ml/min or with significant hepatic impairment, the maximum daily dose is 10 mg.

Dose adjustment is not required in elderly patients.

The tablets should be taken orally, in the morning on an empty stomach, without chewing, with some fluids.

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.

In concomitant use with Coronal, iodine-containing intravenous radiopaque drugs increase the risk of anaphylactic reactions.

Concomitant use of IV phenytoin, drugs for inhalation general anesthesia (hydrocarbon derivatives) increases the severity of cardiodepressive effects and the likelihood of BP reduction with Coronal.

In concomitant use, Coronal alters the effectiveness of insulin and oral hypoglycemic drugs and masks the symptoms of developing hypoglycemia (tachycardia, increased BP).

Concomitant use of Coronal decreases clearance of lidocaine and xanthines (except diphylline) and increases their plasma concentrations, especially in patients with initially increased clearance of theophylline under the influence of smoking.

The NSAIDs (due to retention of sodium ions and blockade of prostaglandin synthesis by the kidneys), GCS and estrogens (due to retention of 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 worsening bradycardia, AV blockade, heart failure and heart failure.

When used concomitantly with Coronal, nifedipine may lead to a significant decrease in BP.

Diuretics, clonidine, sympatholytics, hydralazine and other hypotensive drugs may cause excessive BP reduction when used concomitantly with Coronal.

Coronal prolongs the effects of nondepolarizing myorelaxants and the anticoagulant effect of coumarins.

When used concomitantly with Coronal, tricyclic and tetracyclic antidepressants, antipsychotic drugs (neuroleptics), ethanol, sedatives and sleeping pills increase CNS depression and may provoke cardiac rhythm disturbances, bradycardia and orthostatic hypotension.

The concomitant use of Coronal with MAO inhibitors is not recommended due to the significant increase in hypotensive effect; a break in treatment between MAO inhibitors and Coronal should be at least 14 days.

When used concomitantly with Coronal, nonhydrogenated ergot alkaloids, ergotamine increase the risk of peripheral circulatory disorders.

Sulfasalazine increases the plasma concentration of bisoprolol when used concomitantly with Coronal.

In concomitant use with Coronal, rifampicin shortens the T1/2 of bisoprolol.

There is a potential risk of additive effects with the development of hypotension and/or significant bradycardia when used together with beta-adrenoblockers for topical use (eye drops).

A decreased antihypertensive effect of the drug has been noted with the use of adrenaline and noradrenaline.

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

In case of shock or arterial hypotension due to floktafenin, a decrease in compensatory cardiovascular responses is possible with concomitant use.

Concomitant use with baclofen or amifostine also shows increased antihypertensive effects.

Special Instructions

When prescribing Coronal, HR and BP should be monitored regularly (daily at the beginning of treatment, then once every 3-4 months), ECG should be performed, blood glucose levels should be determined in diabetic patients (once every 4-5 months). In elderly patients it is recommended to control kidney function (once every 4-5 months).

The patient should be trained on how to calculate heart rate and instructed to consult a physician if the heart rate is less than 50 bpm.

Physicians with a history of bronchopulmonary problems should have an external respiratory function study before starting treatment.

It should be considered that beta-adrenoblockers are ineffective in approximately 20% of angina patients because of severe coronary atherosclerosis with low threshold of ischemia (HR less than 100 bpm) and increased left ventricular end-diastolic volume, which impairs subendocardial blood flow.

In patients who smoke, the effectiveness of beta-adrenoblockers is reduced.

Patients who wear contact lenses should be aware that the treatment may decrease tear fluid production.

When using Coronal in patients with pheochromocytoma, there is a risk of paradoxical arterial hypertension (unless effective alpha-adrenoblockade has first been achieved).

Bisoprolol may mask certain clinical signs of thyrotoxicosis (e.g., tachycardia). Abrupt withdrawal of Coronal in patients with thyrotoxicosis is contraindicated because it may exacerbate the symptoms of the disease.

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

If used concomitantly with clonidine, the latter can be discontinued only after several days of withdrawal of Coronal.

The severity of hypersensitivity reactions and lack of effect of usual doses of epinephrine with a history of allergy may increase.

If planned surgical treatment is necessary, the drug should be withdrawn 48 hours before the start of general anesthesia. If the patient has taken the drug prior to surgery, the drug for general anesthesia should be selected with minimal negative inotropic effect.

The reciprocal activation of the vagus nerve can be eliminated by IV administration of atropine (1-2 mg).

Drugs that reduce catecholamine stores (including reserpine) can potentiate the effects of beta-adrenoblockers, so patients taking these combinations of drugs should be kept under constant medical supervision for signs of marked BP lowering or bradycardia.

Patients with concomitant bronchospastic disorders may be prescribed cardioselective adrenoblockers if other hypotensive medications are intolerant and/or ineffective. Overdose is dangerous with the development of bronchospasm.

In case of increasing bradycardia (less than 50 bpm), marked BP decrease (systolic BP below 100 mmHg), AV-blockade in elderly patients the dose should be reduced or the treatment should be stopped.

It is recommended that therapy be discontinued if depression develops.

The drug should be discontinued before blood and urine catecholamine, normetanephrine, vanillylindalic acid, and antinuclear antibody titers are investigated.

The treatment should not be abruptly interrupted because of the risk of severe arrhythmias and myocardial infarction. Withdrawal is done gradually, reducing the dose over 2 weeks or more (the dose is reduced by 25% every 3 to 4 days).

Pediatric use

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

Impact on driving and operating machinery

When using the drug, caution must be exercised while driving vehicles and engaging in other potentially dangerous activities requiring increased concentration and quick psychomotor reactions.

Contraindications

– shock (including.

– acute heart failure;

– decompensated chronic heart failure;

– AV-blockade of II and III degree (without artificial pacemaker);

– sinoatrial block;

– SSRI;

– marked bradycardia;

– cardiomegaly (without signs of heart failure);

– arterial hypotension (systolic BP below 100 mm Hg.systolic BP below 100 mm Hg, especially in myocardial infarction);

– a history of bronchial asthma and chronic obstructive pulmonary disease;

– concomitant use of MAO inhibitors (except MAO type B inhibitors);

– concomitant use of floktafenine and sultopride;

– advanced peripheral circulatory disorders;

– Raynaud’s disease;

– lactation;

– age less than 18 years (efficacy and safety have not been established);

– hypersensitivity to the components of the drug and other beta-adrenoblockers.

. The preparation should be used with caution in patients with hepatic insufficiency, renal insufficiency (CK less than 20 ml/min), metabolic acidosis, pheochromocytoma (concomitant use of alpha-adrenoblockers), decompensated diabetes mellitus, 1st degree AV-blockade, Prinzmetal’s angina, restrictive cardiomyopathy, congenital heart disease or heart valve defects with significant hemodynamic disturbances, chronic heart failure with myocardial infarction within the last 3 months, psoriasis, depression (incl.

In case of severe allergic reactions in anamnesis, pregnancy, strict diet, desensitizing immunotherapy with allergens and allergen extracts, as well as elderly patients.

Side effects

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

CNS disorders: infrequent – fatigue, asthenia, dizziness, headache, somnolence or insomnia, depression; rare – hallucinations, nightmares, seizures.

Sensory organs: rare – visual impairment, decreased tear fluid secretion, dry and painful eyes, hearing impairment; very rare – conjunctivitis.

Cardiovascular system: very common – sinus bradycardia; common – decrease of BP, angiospasm manifestation (increase of peripheral circulation disturbance, cooling of lower extremities, paresthesia); infrequent – AV conduction disturbance, orthostatic hypotension, decompensation of chronic heart failure, peripheral edema.

Digestive system disorders: frequently – dry mouth, nausea, vomiting, diarrhea, constipation; rarely – hepatitis, increased liver transaminase activity.

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

Endocrine system: rarely – hyperglycemia (in patients with type 2 diabetes), hypoglycemia (in patients receiving insulin).

Allergic reactions: rare – skin itching, rash, urticaria.

Skin disorders: rare – increased sweating, skin hyperemia; very rare – psoriasis-like skin reactions, exacerbation of psoriasis symptoms, alopecia.

Muscular system disorders: infrequent – muscle weakness, cramps of the calves, arthralgia.

Hematopoietic system: in rare cases – thrombocytopenia, agranulocytosis.

Others: very rarely – potency disorder, rarely – hypertriglyceridemia, withdrawal syndrome (increased angina pectoris attacks, increased BP).

Overdose

Symptoms: arrhythmia, ventricular extrasystole, marked bradycardia, AV-blockade, decreased BP, acute heart failure, acrocyanosis, difficulty breathing, bronchospasm, dizziness, fainting, seizures.

Treatment: it is necessary to flush the stomach and prescribe adsorptive drugs. Symptomatic therapy is carried out: if AV blockade has developed – IV injection of 1-2 mg of atropine, epinephrine or placement of a temporary pacemaker; if ventricular extrasystole – IV lidocaine (Class I A drugs are not used); if BP decreases, the patient should be in Trendelenburg position; if there are no symptoms of pulmonary edema – IV plasma exchange solutions, if ineffective – injection of epinephrine, dopamine, dobutamine (to maintain chrono- and inotropic action and to eliminate marked BP decrease); in heart failure – cardiac glycosides, diuretics, glucagon; in convulsions – IV diazepam; in bronchospasm – beta2-adreno stimulants inhaled.

Pregnancy use

In pregnancy, Coronal is prescribed only under strict indications if the estimated 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 Coronal is required during lactation, breastfeeding should be stopped.

Bisoprolol administration during pregnancy may cause intrauterine growth retardation, hypoglycemia, and bradycardia in the fetus.

Similarities