Coronal - instructions for use, dose, side effects, contraindications

	5 mg	10 mg
Active substance:
Bisoprolol fumarate	5.0 mg	10.0 mg
Excipients:
Core:
Microcrystalline cellulose	133.0 mg	128.0 mg
Corn starch	7.50 mg	7.50 mg
Sodium lauryl sulfate	1.0 mg	1.0 mg
Silica colloidal dioxide	2.0 mg	2.0 mg
Magnesium stearate	1.50 mg	1.50 mg
Film sheath:
Hypromellose	6.40 mg	6.40 mg
Macrogol 400	1.28 mg	1.28 mg
Titanium dioxide	2.30 mg	2.30 mg
Dye-iron oxide yellow (E172)	0.02 mg	-
Dye-iron oxide red (E172)	-	0.02 mg

Description:

Tablets 5 mg: round, biconcave, light yellow color pills with a risk, covered with a film membrane.

Tablets 10 mg: round, biconcave, light pink color pills with a risk, film-coated.

Pharmacotherapeutic group:beta1-blocker selective

ATX: & nbsp

C.07.A.B Selective beta-blockers

C.07.A.B.07 Bisoprolol

Pharmacodynamics:

Selective beta₁-adrenoceptor without its own sympathomimetic activity, does not possess membrane-stabilizing action. Reduces the activity of plasma renin, reduces the need for myocardium in oxygen, reduces the heart rate (heart rate) (at rest and with exercise). Has antihypertensive, antiarrhythmic and anti-anginal action. Blocking in low doses beta₁-cardiac adenosine monophosphate (cAMP) from adenosine triphosphate (ATP), reduces the intracellular current of calcium ions, has a negative chrono-, dromo-, batmo- and inotropic effect (it cuts the heart rate, inhibits conduction and excitability, reduces contractility myocardium).

With an increase in the dose of beta₂-adrenoblocking action.

The total peripheral vascular resistance (OPSS) at the beginning of the drug, in the first 24 hours after ingestion, increases (as a result of the reciprocal increase in the activity of alpha-adrenergic receptors and the removal of stimulation beta₂-adrenoreceptors), returns to the initial value in 1-3 days, and decreases with long-term administration.

Antihypertensive action is associated with a decrease in the minute volume of blood, sympathetic stimulation of peripheral vessels, a decrease in the activity of the renin-angiotensin-aldosterone system (important for patients with initial hypersecretion of renin) and central nervous system (CNS), restoration of the sensitivity of the aortic arch baroreceptors in response to a decrease in blood pressure (BP)) and, in the end,reduction of peripheral sympathetic influences. With arterial hypertension, the effect occurs after 2-5 days, a stable effect - after 1-2 months.

Antianginal effect is caused by a decrease in myocardial oxygen demand as a result of a decrease in the heart rate, a decrease in contractility, diastole lengthening, improved myocardial perfusion, and a decrease in myocardial sensitivity to sympathetic innervation. Reduces the number and severity of angina attacks and increases the tolerance of exercise. By increasing the end diastolic pressure in the left ventricle and increasing the stretching of the muscle fibers of the ventricles, it can increase the need for oxygen, especially in patients with chronic heart failure (CHF).

Antiarrhythmic effect is due to elimination of arrhythmogenic factors (tachycardia, increased activity of the sympathetic nervous system, increased content of cyclic adenosine monophosphate, arterial hypertension), a decrease in the rate of spontaneous excitation of sinus and ectopic pacemakers and slowing of atrioventricular (AV) conduct (mainly in antegrade and, to a lesser extent, in the retrograde direction through AV node) and on additional paths.

When used in secondary therapeutic doses, in contrast to non-selective beta-blockers, has a less pronounced effect on organs containing beta₂-adrenoceptors (pancreas, skeletal muscles, smooth muscles of peripheral arteries, bronchi and uterus) and on carbohydrate metabolism, does not cause delay of sodium ions (Na⁺) in organism; the severity of atherogenic action does not differ from that of propranolol. When used in large doses (200 mg and more) has a blocking effect on both subtypes of beta adrenoreceptors, mainly in the bronchi and smooth muscles of the vessels.

Pharmacokinetics:

Absorption - 80-90%, food intake does not affect absorption. The maximum concentration in the blood plasma is observed after 1-3 h, the connection with blood plasma proteins is about 30%. The permeability of the blood-brain barrier and the placental barrier - low secretion breast milk - low.

Metabolized in the liver with the formation of inactive metabolites, half-life of 10-12 hours.About 98% is excreted by the kidneys, 50% of them are excreted unchanged, less than 2% with bile.

Indications:

- Ahyperthermia;

- ischemic heart disease: prevention of angina attacks.

Contraindications:

Hypersensitivity to the components of the drug and other beta-blockers, shock (including cardiogenic), acute heart failure, chronic heart failure in the stage of decompensation, AV blockade II-III degree (without artificial pacemaker), sinoatrial block, sinus node weakness syndrome, severe bradycardia, cardiomegaly (no signs of heart failure), arterial hypotension (systolic blood pressure less than 100 mmHg, especially with myocardial infarction); The bronchial asthma and chronic obstructive pulmonary disease in the anamnesis; simultaneous administration of monoamine oxidase inhibitors (MAO) (with the exception of MAO type B inhibitors), concomitant use of floktaphenin and sultopride, late stages of peripheral circulation, Raynaud's disease, lactation, age under 18 years (efficacy and safety not established).

Carefully:

Hepatic failure, renal insufficiency (creatinine clearance less than 20 ml / min), metabolic acidosis, pheochromocytoma (with concomitant use of alpha-blockers), diabetes mellitus in decompensation stage, atrioventricular blockade of I degree, angina prinzmetal, restrictive cardiomyopathy, congenital heart defects or heart valve defects with severe hemodynamic disorders, chronic cardiac insufficiency with myocardial infarction during the last 3 months, psoriasis, depression (including history), severe allergic reactions in the history, pregnancy, elderly age t, a strict diet, carrying out desensitizing immunotherapy with allergens and allergen extracts.

Pregnancy and lactation:

In pregnancy, CORONAL is prescribed only according to strict indications, if the intended benefit to the mother exceeds the potential risk to the fetus. 72 hours prior to delivery, the CORONAL drug should be discontinued due to possible fetal / newborn bradycardia, arterial hypotension, hypoglycemia, and respiratory depression.

If taking CORONAL is necessary during lactation, breastfeeding should be discontinued.

Dosing and Administration:

CORONAL ® is taken orally, in the morning on an empty stomach, without chewing, with a small amount of liquid.

With arterial hypertension and ischemic heart disease (prevention of attacks of stable angina) the initial dose is 2.5-5 mg once a day. If necessary, increase the dose to 10 mg once a day. The maximum daily dose is 20 mg / day.

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

Dose adjustments in elderly patients are not required.

Side effects:

Frequency: very often (more than or equal to 1/10); often (more than 1/100, less than 1/10); infrequently (more than 1/1000, less than 1/100); rarely (more than 1/10000, less than 1/1000); very rarely (less than 1/10000, including individual messages).

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

From the sense organs: rarely - visual impairment, a decrease in the secretion of tear fluid, dryness and soreness of the eyes,hearing impairment; very rarely - conjunctivitis.

Co cardiovascular system: very often - a sinus bradycardia; often - decrease in arterial pressure, manifestation of angiospasm (increased peripheral circulatory disturbances, coldness of the lower limbs, paresthesia); infrequently - violation of atrioventricular 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.

From the respiratory system: infrequent breathing difficulties when prescribing in high doses (loss of selectivity) and / or in predisposed patients - laryngo- and bronchospasm; rarely - stuffy nose, allergic rhinitis.

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

Allergic reactions: rarely - skin itching, rash, hives.

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

From the musculoskeletal system: infrequently - muscle weakness, cramps in the calf muscles, arthralgia.

Laboratory indicators: rarely - increased activity of "hepatic" transaminases, hypertriglyceridemia; in some cases - thrombocytopenia, agranulocytosis.

Influence on the fetus: intrauterine growth retardation, hypoglycemia, bradycardia.

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

Overdose:

Symptoms: arrhythmia, ventricular ekstrasistoliya, pronounced bradycardia, AV blockade, marked decrease in arterial pressure, acute heart failure, acrocyanosis, difficulty breathing, bronchospasm, dizziness, fainting, convulsions.

Treatment: gastric lavage and administration of absorbent drugs; symptomatic therapy: with developed AV blockade - intravenous (intravenous) 1-2 mg of atropine, epinephrine or temporary cardiac pacemaker; with ventricular extrasystole - lidocaine (preparations Ia of a class are not applied); with a decrease in blood pressure - the patient should be in the Trendelenburg position; if there are no signs of pulmonary edema - intravenously plasmo-replacing solutions, with inefficiency - the introduction of epinephrine, dopamine,dobutamine (to maintain chronotropic and inotropic action and to eliminate the pronounced decrease in blood pressure); with heart failure - cardiac glycosides, diuretics, glucagon; with convulsions - intravenously diazepam; with bronchospasm - beta₂-adrenostimulators inhalation.

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.

Iodine-containing radiopaque drugs for intravenous administration increase the risk of developing anaphylactic reactions.

Phenytoin with intravenous administration, drugs for inhalation anesthesia (derivatives of hydrocarbons) increase the severity of cardiodepressive action and the likelihood of lowering blood pressure.

Changes the effectiveness of insulin and hypoglycemic agents for oral administration, masks the symptoms of developing hypoglycemia (tachycardia, increased blood pressure).

Reduces the clearance of lidocaine and xanthines (except diphylline) and increases their concentration in the plasma, especially in patients with initially elevated clearance of theophylline under the influence of smoking.

Antihypertensive effects weaken non-steroidal anti-inflammatory drugs (sodium ion retention (Na⁺) and blockade of prostaglandin synthesis by the kidneys), glucocorticosteroids and estrogens (sodium ion retention).

Cardiac glycosides, methyldopa, reserpine and guanfacine, blockers of "slow" calcium channels (verapamil, diltiazem), amiodarone and other antiarrhythmic drugs increase the risk of developing or worsening bradycardia, AV blockade, cardiac arrest and heart failure.

Nifedipine can lead to a significant reduction in blood pressure.

Diuretics, clonidine, sympatholytics, hydralazine and other antihypertensive drugs can lead to excessive lowering of blood pressure.

Lengthens the effect of nondepolarizing muscle relaxants and increases the anticoagulant effect of coumarins.

Tri- and tetracyclic antidepressants, antipsychotics (antipsychotics, including sultopride), ethanol, sedative and hypnotic drugs increase the inhibition of the central nervous system, can cause heart rhythm disturbances, bradycardia and orthostatic hypotension.

It is not recommended simultaneous use with monoamine oxidase inhibitors due to a significant increase in antihypertensive action, a break in treatment between taking monoamine oxidase inhibitors and bisoprolol should be at least 14 days.

Unhydrated ergot alkaloids increase the risk of peripheral circulatory disorders.

Ergotamine increases the risk of peripheral circulatory disorders; sulfasalazine increases the concentration of bisoprolol in plasma; rifampicin shortens the half-life of the drug.

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

A decrease in the antihypertensive effect of the drug against the background of the use of adrenaline and norepinephrine is noted.

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 the case of shock or arterial hypotension caused by floktaphenin, when combined, it is possible to reduce compensatory cardiovascular reactions.

With simultaneous use with baclofen or amifostine also increased antihypertensive effect.

Special instructions:

The use of CORONAL in children under 18 years old is contraindicated, since efficacy and safety have not been established.

Control of patients taking CORONAL should include measurement of heart rate and blood pressure (at the beginning of treatment - every day, then once every 3-4 months), conducting an electrocardiogram, determining the concentration of glucose in the blood in patients with diabetes mellitus (1 every 4 -5 months). In elderly patients it is recommended to follow the function of the kidneys (once every 4-5 months).

The patient should be taught how to calculate the heart rate and instructed about the need for medical advice at a heart rate of less than 50 beats per minute.

Before the start of treatment, it is recommended to perform an external respiration function in patients with a history of bronchopulmonary anamnesis.

Approximately in 20% of patients with angina pectoris beta-adrenoblockers are ineffective. The main causes are severe coronary atherosclerosis with a low threshold of ischemia (heart rate less than 100 beats per minute) and an increased end-diastolic volume of the left ventricle that disrupts the subendocardial blood flow.

In "smokers" the effectiveness of beta-blockers is lower.

Patients who use contact lenses should take into account that, on the background of treatment, tear fluid production can be reduced.

When used in patients with pheochroctomy, there is a risk of developing paradoxical arterial hypertension (unless an effective alpha-adrenoblockade has been previously achieved).

With thyrotoxicosis bisoprolol can mask certain clinical signs of tretoothicosis (eg, tachycardia). Abrupt withdrawal in patients with thyrotoxicosis is contraindicated, since it can strengthen symptoms.

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

With the simultaneous administration of clonidine, his reception may be terminated only a few days after the CORONAL drug is discontinued.

It is possible to increase the severity of the reaction of hypersensitivity and the lack of effect from the usual doses of epinephrine against the background of a burdened allergological anamnesis.If it is necessary to conduct routine surgical treatment, the drug can be withdrawn 48 hours before the start of the general anesthesia. If the patient has taken the drug before the operation, he should choose a medicine for general anesthesia with a minimum negative inotropic effect.

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

Drugs that reduce the reserves of catecholamines (including, reserpine), can enhance the action of beta-blockers, so patients who take such combinations of drugs should be under constant medical supervision to detect a marked decrease in blood pressure or bradycardia.

Patients with bronchospastic diseases can be prescribed cardioselective beta-blockers in case of intolerance and / or ineffectiveness of other antihypertensive medications. Overdosing is dangerous by the development of bronchospasm.

In the case of an increased bradycardia (less than 50 beats / min) in elderly patients, a marked decrease in blood pressure (systolic blood pressure below 100 mm Hg) AV blockade, it is necessary to reduce the dose or stop treatment.

It is recommended to stop therapy with the development of depression.

The drug should be withdrawn before the study of blood and urine levels of catecholamines, normetanephrine and vanillin-mandelic acid; titers of antinuclear antibodies.

Features of the drug during the first admission or when it is canceled

You can not abruptly interrupt treatment because of the danger of developing the syndrome of "withdrawal" (severe arrhythmias and myocardial infarction). Abolition is carried out gradually, reducing the dose for 2 weeks or more (reduce the dose by 25% in 3-4 days).

Effect on the ability to drive transp. cf. and fur:

During the treatment period, care must be taken when driving a vehicle and engaging in other potentially hazardous activities that require a high concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Tablets, film-coated, 5 mg and 10 mg.

Packaging:

For 10 or 15 tablets in a blister pack of PVC/PE/PVDC-AL or in a blister of Al / Al.

For 1, 3, 6 or 10 blisters of 10 tablets or 2 or 4 blisters of 15 tablets, together with the instructions for use are placed in a cardboard box.

Storage conditions:

At a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years

The drug should not be used after the expiry date indicated on the package.

Terms of leave from pharmacies:On prescription

Registration number:LS-000943

Date of registration:04.04.2011

The owner of the registration certificate:Zentiva as.Zentiva as. Czech Republic

Manufacturer: & nbsp

ZENTIVA, a.s. Czech Republic

Representation: & nbspZENTIVA PHARMA, LLCZENTIVA PHARMA, LLC

Information update date: & nbsp26.11.2015

Illustrated instructions

Instructions

Coronal (Coronal)