Bicard

Bicard is a highly selective β1-adrenoblocker with cardiotropic activity and an effect on hemodynamic values.

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Indications Bicarda

It is used for the following painful conditions:

• increased blood pressure;
• angina pectoris, which may be stable or unstable;
• prevention of development of secondary coronary heart disease;
• cardiac insufficiency;
• symptomatic therapy for migraines, thyrotoxicosis;
• perioperative reduction in the likelihood of cardiac-related mortality.

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Release form

The drug is produced in tablets of 5 or 10 mg, in the amount of 10 pieces inside blister packs. There are 3 such packs in a box.

Pharmacodynamics

Bisoprolol mainly affects cardiac β1-adrenergic endings. The drug is synthesized with the endings and prevents their interaction with catecholamines, which leads to inhibition of cAMP binding processes. Such changes destroy the processes occurring inside the membrane Ca channels and change the Ca level inside the cells of the conduction system. This leads to a decrease in heart rate, suppression of impulse conduction through the bundle of Kent with the AV node, and at the same time weakens nodal automatism. When conduction processes are suppressed, an antiarrhythmic effect develops. The absence of calcium ions inside cardiomyocytes causes the destruction of the interaction of myosin with actin, due to which the force of heart contractions decreases.

A reduced heart rate and a weakening of the intensity of this process reduce the oxygen demand of myocardial fibers, resulting in an antianginal effect and an increase in the level of myocardial perfusion.

Bisoprolol can normalize the walls of lysosomes and cells, and slow down the aggregation of blood platelets. The drug blocks the activity of β1-adrenoreceptors inside the kidneys, resulting in a decrease in angiotensin 2 with renin. In combination with a decrease in heart rate and contraction intensity, such effects lead to a persistent decrease in blood pressure.

Bicard affects the processes of restructuring the baroreflex reactions of the aortic arch and carotid sinus, and at the same time enhances the release of vasodilator components (PNP with PG and nitric oxide).

Bisoprolol does not have an effect on β2-adrenoreceptors, due to which the severity and frequency of its negative manifestations are reduced - this is the reason for the good tolerability of the drug. In large doses, the drug can affect the activity of β1-, as well as β2-adrenoreceptors.

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Pharmacokinetics

The drug has good absorption from the gastrointestinal tract. Blood values of Cmax are recorded after 1-3 hours.

Synthesis of the substance with blood albumin is 30%. The component bisoprolol can pass through the placenta and the BBB, and is also excreted in small quantities with breast milk.

The half-life of the element is up to 12 hours, and the duration of circulation and medicinal effect is up to 24 hours.

Since bisoprolol is an amphophilic component, the drug is excreted in 2 equally effective ways - about 50% is eliminated through the liver, and another 50% is excreted by the kidneys in the form of active metabolic products (thus having a balanced clearance). Due to this, the drug can be used with equal success in cases of kidney or liver problems, without the need to adjust the dose of the drug.

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Dosing and administration

The medicine should be taken orally. It is recommended to take a tablet once a day, preferably in the morning. The medicine should be washed down with plain water, without biting or chewing the tablet. The medicine can be taken without reference to food intake.

The initial dose of the medicine is 5 mg taken once a day. The dosage of the medicine can be gradually increased (weekly by 5 mg). Sometimes the initial dose is 10 mg. Increasing the dose can cause negative symptoms to develop - in this case, you need to return to the previous dose. The maximum permissible daily dose is 20 mg taken once a day.

If a patient suffers from chronic renal failure in a severe form, he can take no more than 10 mg of the substance per day.

The treatment cycle should continue for a long time.

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Use Bicarda during pregnancy

The drug should not be prescribed to pregnant or breastfeeding women. The drug may slow down intrauterine development, suppress the respiratory center in the fetus, and then after birth cause severe hypoglycemic conditions in the newborn baby (during the first 3 days of life).

Contraindications

Among the contraindications:

• signs of AV or sinoatrial block of 2-3 degree severity;
• heart rate values below 50 beats/minute;
• SSSU;
• low systolic pressure (less than 90 mmHg);
• severe peripheral blood flow disorders;
• COPD or bronchial asthma;
• psoriasis or pheochromocytoma;
• use together with MAOIs.

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Side effects Bicarda

Bisoprolol has a good drug safety profile. Side effects after its use develop quite rarely.

The drug may cause CNS disorders, including dizziness, asthenic symptoms and headaches that occur at the initial stage of treatment. In addition, depression, sleep disorders or paresthesia may develop; hallucinations have been reported sporadically. Such disorders disappear on their own after 10-14 days from the start of therapy.

Visual disturbances may occur – conjunctivitis, decreased lacrimation and visual impairment.

Negative signs in the work of the cardiovascular system may be observed - a decrease in blood pressure or heart rate, disturbance of the blockade and rhythm processes, heart failure accompanied by symptoms of peripheral edema, and temporary intermittent claudication at the initial stage of drug use.

Occasionally, respiratory system dysfunctions such as bronchial spasms occur.

The appearance of stool disorders, dyspeptic symptoms and an increase in the activity of liver transaminases are noted; hepatitis may appear.

Occasionally, the development of muscle weakness, arthralgia or cramps is recorded.

Treatment may provoke the appearance of signs of allergy - in these cases it is necessary to stop using Bicard.

In diabetics, the drug may cause hypoglycemic symptoms; in non-diabetics, increased TG levels and impaired glucose tolerance have been reported rarely.

In men, the use of bisprool may cause problems with erectile function or the development of alopecia.

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Overdose

When the drug is administered in large doses, disturbances in heart rhythm, symptoms of bradycardia, bronchial spasms, seizures, fainting and signs of heart failure occur, and in addition, blood pressure decreases.

To eliminate these disorders, gastric lavage and sorbent administration are performed. When the blood pressure and bradycardia levels decrease, 1.5-2 mg of atropine, as well as dopamine and epinephrine, are administered intravenously.

When heart failure occurs, diuretics, glucagon and CG are used.

In case of development of bronchial spasms, inhalations of β2-adrenergic agents are performed.

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Interactions with other drugs

Bisoprolol interacts with antihypertensive medications, exhibiting synergism; as a result, their therapeutic properties are enhanced.

The development of severe bradycardia is observed in the case of a combination of the drug with clonidine, reserpine, as well as α-methyldopa or guanfacine.

Concomitant use with guanfacine, clonidine or digitalis medications leads to conduction disturbances and the development of AV block.

Sympathomimetics weaken the therapeutic properties of bisoprolol.

Drugs that block Ca channels (dihydropyridine derivatives), as well as nifedipine, lead to a strong decrease in blood pressure values.

Diltiazem with verapamil and antiarrhythmic drugs when used together with Bicard lead to a decrease in blood pressure, the development of a persistent form of bradycardia, heart rhythm disorders, reaching heart failure along with cardiac arrest.

Ergotamine derivatives, combined with the drug, increase the signs of peripheral blood flow disorders.

Rifampicin reduces the half-life of bisoprolol, but this fact is not clinically significant.

The drug destroys the effectiveness of glycemic control processes in diabetics.

NSAIDs reduce the antihypertensive activity of the drug.

The drug increases the half-life of coumarin anticoagulants and muscle relaxants.

Sleeping pills and sedatives, antidepressants, ethyl alcohol and neuroleptics significantly suppress the functioning of the central nervous system when combined with medication.

MAOIs disrupt the metabolic processes of Bicard, which increases the severity of its negative manifestations. The interval between the use of the drug and MAOIs should be at least 14 days.

Sulfasalazine, when combined with the drug, increases the plasma Cmax values of the former.

Iodine-containing radiocontrast agents, if administered during the use of bisoprolol, may rarely lead to severe anaphylactic symptoms.

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Storage conditions

Bicard must be kept at temperatures around 25°C.

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Shelf life

Bicard can be used within 24 months from the date of manufacture of the pharmaceutical product.

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Application for children

There is no information regarding the safety and medicinal efficacy of Bicard when used in pediatrics, which is why it is not prescribed to children.

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Analogues

Analogues of the drug are Bisoprolol, Bisogamma, Aritel with Concor, Niperten and Coronal with Aritel Cor, and also Bidop and Biprolol.

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