Bicard

Bikard is a highly selective β1-adrenoblocker with cardiotropic activity and acting on hemodynamic values.

[1],

Indications It's over

It is used for the following conditions:

• increased blood pressure;
• angina, having a stable or unstable nature;
• prevention of the development of secondary ischemic heart disease;
• heart failure;
• symptomatic therapy for migraines, thyrotoxicosis;
• perioperative reduction in the probability of death due to cardiac factors.

[2], [3]

Release form

The release of drugs produced in tablets with a volume of 5 or 10 mg, in the amount of 10 pieces inside the cellular packaging. In the box - 3 such packages.

Pharmacodynamics

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

Reduced HR and a decrease in the intensity of this process reduce the oxygen demand of myocardial fibers, resulting in an antianginal effect and an increase in myocardial perfusion.

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

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

Bisoprolol does not have an effect on β2-adrenoreceptors, because of which the severity and frequency of its negative manifestations decreases - this is the reason for the good tolerance of the drug. In large portions, the drug can affect the activity of β1-, as well as β2-adrenergic receptors.

[4], [5], [6], [7], [8], [9], [10], [11]

Pharmacokinetics

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

Synthesis of a substance with blood albumin is 30%. The bisoprolol component can pass through the placenta and the BBB, and is also excreted in small amounts with mother's milk.

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

Since bisoprolol is an amphophilic component, the drug is excreted in two 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 (possessing, thus, a balanced clearance). Due to this, the drug can be used with equal success in case of problems with the work of the kidneys or liver, without the need to adjust the dose of drugs.

[12], [13], [14], [15], [16], [17], [18], [19]

Dosing and administration

The medicine must be taken orally. It is recommended to take a pill once a day, preferably in the morning. It is required to wash down a preparation with usual water, without getting through and not chewing a tablet. You can take drugs without reference to the use of food.

The initial dose of the medication is 5 mg with a single dose per day. You can gradually increase the dosage of the drug (weekly 5 mg). At times, the size of the initial portion is 10 mg. An increase in a portion of the dose may cause the development of negative symptoms - in this case, you need to return to the previous dosage. The maximum allowable daily dose is 20 mg, which are taken 1-fold.

If the patient is ill with chronic kidney disease, which has a severe form of severity, it can take no more than 10 mg of a substance per day.

The treatment cycle should last a long time.

[27], [28]

Use It's over during pregnancy

Do not prescribe medication to pregnant or lactating women. The medication can lead to a slowdown of intrauterine development, suppress the respiratory center in the fetus, and then after birth cause severe hypoglycemic states in the newborn baby (during the first 3 days of life).

Contraindications

Among the contraindications:

• signs of AB - or sinoatrial blockade, with 2-3 degree of severity;
• HR values below 50 beats / minute;
• SSSU;
• low systolic pressure (less than 90 mm Hg);
• severe peripheral blood flow disorders;
• COPD or BA;
• psoriasis or pheochromocytoma;
• use with IMAO.

[20], [21], [22], [23]

Side effects It's over

Bisoprolol has a good medical safety profile. Adverse symptoms after its use are quite rare.

The drug can cause disturbances in the work of the central nervous system, including dizziness, asthenic symptoms and headaches that occur at the initial stage of treatment. In addition, depression, sleep disorder or paresthesia may develop; a single report of hallucinations. Such violations disappear on their own after 10-14 days have passed since the start of therapy.

Perhaps the appearance of visual disorders - conjunctivitis, reduction of tearing and visual impairment.

Negative symptoms in the work of the cardiovascular system can be noted - a decrease in the level of blood pressure or heart rate indicators, a disorder 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, there are disorders of the respiratory system, such as bronchial spasms.

The occurrence of stool disorders, dyspeptic symptoms and an increase in liver transaminase activity is noted; hepatitis may appear.

The development of muscle weakness, arthralgia, or seizures is rarely recorded.

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

In diabetics, medication can lead to the development of symptoms of hypoglycemia; in people who do not have diabetes, occasionally an increase in the level of TG and impaired glucose tolerance were recorded.

In men, as a result of the use of bisprolol, problems with erectile function may occur or alopecia may develop.

[24], [25], [26]

Overdose

With the introduction of the drug in large portions, heart rhythm disorders, symptoms of bradycardia, bronchial spasms, seizures, fainting and signs of heart failure appear, and in addition the BP index decreases.

To eliminate these disorders, gastric lavage and the appointment of sorbents are carried out. With a decrease in blood pressure and bradycardia, intravenous administration of 1.5-2 mg of atropine, as well as dopamine and epinephrine, is performed.

When manifested CHF use diuretic drugs, glucagon and SG.

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

[29], [30],

Interactions with other drugs

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

The development of bradycardia of a pronounced nature is noted in the case of a combination of the drug with clonidine, reserpine, and also α-methyldopa or guanfacine.

Simultaneous use with guanfacine, clonidine or digitalis drugs leads to disorders of the conduction process and the development of AV-blockade.

Sympathomimetics weaken the therapeutic properties of bisoprolol.

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

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

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

Rifampicin reduces the half-life of bisoprolol, but this fact does not have clinical significance.

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 antipsychotics significantly inhibit the work of the central nervous system when they are combined with the medication.

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

Sulfasalazine combined with the drug increases plasma Cmax values of the first.

Radiopaque medications containing iodine, if administered during the period of use of bisoprolol, can rarely lead to the appearance of severe anaphylaxis symptoms.

[31], [32], [33], [34], [35], [36], [37]

Storage conditions

Bikard must be maintained at temperature values within the mark of 25 ° C.

[38], [39], [40]

Shelf life

Bikard can be applied within 24 months from the moment of production of pharmaceutical means.

[41]

Application for children

Information regarding the safety and drug efficacy of Bicard when used in pediatrics is absent, because of what it is not prescribed to children.

[42], [43]

Analogs

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

[44], [45], [46]