Bisoprolol

Bisoprolol is a selective (cardioselective) beta-1 blocker with antihypertensive, antiarrhythmic and antianginal effects. The drug reduces the need for oxygen in the heart muscle, slows the heart rate, and “disarms” renin circulating in the blood plasma. Good tolerance by patients, high efficiency and the ability to prevent the development of a number of negative consequences of arterial hypertension have elevated beta blockers to the rank of permanent participants in the “battle” against cardiovascular diseases, which is waged today with varying success in modern cardiology. The discovery of subtypes of beta-1 and beta-2 adrenergic receptors at the end of the 60s of the last century prompted scientists to think about selective blockade of the former, because It is they, interacting with catecholamines, that create a favorable background for moving the tonometer needle beyond the WHO-recommended borderline readings of “140/90”. Selectivity (or cardioselectivity) has little effect on the hypotensive and antianginal effects of beta-blockers, while reducing the likelihood of a number of unpleasant side effects associated with stimulation of beta-2 adrenergic receptors (for example, bronchospasm or peripheral vasoconstriction).

Among all beta blockers known today, bisoprolol is endowed with the greatest selectivity and effectiveness. The antihypertensive effect of bisoprolol is comparable to that of calcium channel blockers and angiotensin-converting enzyme inhibitors. Distinctive features of this drug are also high (about 90%) bioavailability, long elimination period and “elusiveness” for proteins, with which no more than 30% of the active substance of the drug binds.

Moreover, these purely positive qualities of bisoprolol are characteristic of it regardless of the dose, which makes it possible to reduce the frequency of administration to a minimum - once a day. Having the advantages of both lipophilic (high absorption rate) and hydrophilic (long elimination time, insignificant biotransformations after the first passage through the liver) beta blockers, bisoprolol can be used in patients with liver and kidney diseases without changing the dose. As already mentioned, bisoprolol has the highest degree of cardioselectivity and only minimally affects beta-2 adrenergic receptors. This allows the drug to be prescribed to patients with chronic bronchial obstruction, bronchial asthma and atherosclerosis of peripheral vessels. Bisoprolol does not interfere with the processes of carbohydrate and lipid metabolism, and therefore does not cause increased insulin resistance. Regular and long-term use of bisoprolol for arterial hypertension, angina pectoris, chronic heart failure allows not only to curb “unleashed” blood pressure, reduce the frequency of angina manifestations, prevent or stop the progression of heart failure, but also significantly reduce the development of severe cardiovascular complications, thereby improving health prognosis patient and increasing his life expectancy.

Contraindications

Hypersensitivity to bisoprolol or other components of the drug; acute heart failure or decompensated heart failure that requires inotropic therapy; cardiogenic shock; AV blockade of the 2nd and 3rd degrees (with the exception of that in patients with an artificial pacemaker); sick sinus syndrome; sinoatrial block; symptomatic bradycardia; symptomatic arterial hypotension; severe asthma or severe chronic obstructive pulmonary disease; late stages of peripheral circulatory disorders or Raynaud's disease; metabolic acidosis; untreated pheochromocytoma.

Side effects

On the part of the immune system: the appearance of antinuclear antibodies with specific clinical symptoms such as lupus-like syndrome, which disappeared after cessation of treatment.

From the psyche: sleep disturbance, depression, nightmares, hallucinations.

Metabolic disorders: increased TG levels in the blood, hypoglycemia.

From the nervous system: increased fatigue, exhaustion, dizziness*, headache*, loss of consciousness.

On the part of the organ of vision: decreased tear production (should be taken into account when wearing contact lenses), conjunctivitis.

On the part of the hearing organ: hearing loss.

From the heart: bradycardia, impaired AV conduction, appearance/intensification of signs of heart failure.

Vascular: a feeling of coldness or numbness of the extremities, arterial hypotension (especially in patients with heart failure), worsening of Raynaud's disease, worsening of existing intermittent claudication, orthostatic hypotension.

From the respiratory system: bronchospasm in patients with a history of asthma or COPD, allergic rhinitis.

From the digestive system: nausea, vomiting, diarrhea, abdominal pain, constipation.

From the liver: increased levels of liver enzymes (ALAT, AST) in the blood plasma, hepatitis.

From the skin and subcutaneous tissue: hypersensitivity reactions, including itching, redness, rash, hot flashes, increased sweating, hair loss, β-adrenergic receptor blockers can cause or worsen psoriasis, psoriatic rashes.

From the musculoskeletal system: muscle weakness, cramps, arthropathy.

From the reproductive system: impaired potency.

General disorders: increased fatigue*, asthenia.

Laboratory tests: increased levels of TG, liver enzymes (ALAT, AST)*.

*Applies only to patients with hypertension or coronary artery disease. These symptoms usually occur at the beginning of therapy, are mild and disappear within the first 1–2 weeks.

In case of side effects or undesirable reactions, you must immediately inform your doctor.

special instructions

At the beginning of treatment with bisoprolol, it is necessary to ensure regular monitoring of the patient's condition, especially for elderly people.

Treatment of stable chronic heart failure with bisoprolol should begin with a titration phase.

In patients with coronary artery disease, treatment should not be stopped suddenly unless necessary, as this may lead to transient worsening of the condition. Initiation and cessation of treatment with bisoprolol requires regular monitoring.

Currently, there is not enough therapeutic experience in the treatment of heart failure in patients with the following diseases and pathological conditions: diabetes mellitus type I (insulin-dependent), severe renal dysfunction, severe liver dysfunction, restrictive cardiomyopathy, congenital heart defects, hemodynamically significant acquired valvular heart defects , myocardial infarction within the last 3 months.

The drug should be used with caution in combination with amiodarone, given the risk of developing contractile contractility and cardiac conduction disturbances (inhibition of compensatory sympathetic reactions).

In general, it is not recommended to prescribe bisoprolol in combination with calcium antagonists of the verapamil or diltiazem type and with centrally acting antihypertensive drugs.

The drug should be used with caution in patients with the following conditions:

bronchospasm (BA, obstructive airway diseases);
diabetes mellitus with significant fluctuations in blood glucose levels due to the possibility of masking the symptoms of hypoglycemia (tachycardia, palpitations, increased sweating);
strict diet;
carrying out desensitization. Like other beta-adrenergic blockers, bisoprolol may increase sensitivity to allergens and increase the severity of anaphylactic reactions. In such cases, treatment with epinephrine does not always provide a positive therapeutic effect;
I degree blockade;
Prinzmetal's angina;
obliterating diseases of peripheral arteries (at the beginning of therapy, complaints may increase);
general anesthesia.

It is imperative to warn the anesthesiologist about taking β-adrenergic receptor blockers. In patients undergoing general anesthesia, the use of β-adrenergic blockers reduces the incidence of arrhythmia and myocardial ischemia during induction of anesthesia, intubation and the postoperative period. It is recommended to continue the use of β-adrenergic blockers during the perioperative period. It is imperative to warn the anesthesiologist about taking β-adrenergic receptor blockers, since the doctor must take into account the potential interaction with other drugs, which can lead to bradyarrhythmia, reflex tachycardia and a decrease in the ability of the reflex mechanism to compensate for blood loss. If bisoprolol is discontinued before surgery, the dose should be gradually reduced and the drug should be stopped 48 hours before general anesthesia.

Combinations of bisoprolol with calcium antagonists of the verapamil or diltiazem group, class I antiarrhythmic drugs and centrally acting antihypertensive drugs are not recommended (see INTERACTIONS).

Although cardioselective β-blockers (β1) have less effect on pulmonary function than non-selective β-blockers, their use, like all β-blockers, should be avoided in obstructive airway disease unless there is compelling reason for therapy. If necessary, bisoprolol should be used with caution. In patients with obstructive airway diseases, treatment with bisoprolol should be started at the lowest possible dose and patients should be monitored for the occurrence of new symptoms (such as shortness of breath, exercise intolerance, cough).

For asthma or other chronic obstructive pulmonary diseases that may cause symptoms, concomitant therapy with bronchodilators is indicated. In some cases, while taking the drug, patients with asthma may require higher doses of β2-sympathomimetics due to increased respiratory tract resistance.

For patients with psoriasis (including those with a history), beta-adrenergic receptor blockers (for example bisoprolol) should be prescribed after a careful benefit/risk balance.

Patients with pheochromocytoma should be prescribed bisoprolol only after prescribing therapy with α-adrenergic receptor blockers.

Symptoms of thyrotoxicosis may be masked while taking the drug.

When using bisoprolol, a positive result may be observed during doping control.

Use during pregnancy or breastfeeding. The use of bisoprolol in pregnant women is possible only if absolutely necessary after assessing the balance of benefits and risks for the mother and fetus. In general, beta-blockers reduce blood flow to the placenta and may affect fetal development. If treatment with a β-adrenergic blocker is necessary, it is desirable that it be a β1-selective β-adrenergic blocker. It is necessary to control the blood flow in the placenta and uterus. After birth, the newborn should be closely monitored. Symptoms of hypoglycemia and bradycardia can be expected within the first 3 days. There is no data on the penetration of bisoprolol into breast milk. Therefore, taking the drug is not recommended during breastfeeding.

The ability to influence reaction speed when driving vehicles or other mechanisms. In some cases, at the beginning of treatment, when changing the drug, as well as when interacting with alcohol, the ability to drive a car and other mechanisms may be reduced.

Note!

Description of the drug Bisoprolol-Teva table. 5mg No. 30 on this page is a simplified author’s version of the apteka911 website, created on the basis of the instructions for use.
Before purchasing or using the drug, you should consult your doctor and read the manufacturer's original instructions (attached to each package of the drug). Information about the drug is provided for informational purposes only and should not be used as a guide to self-medication. Only a doctor can decide to prescribe the drug, as well as determine the dose and methods of its use.

Overdose

Symptoms: bradycardia, arterial hypotension, acute heart failure, bronchospasm, hypoglycemia. There is wide variability in individual sensitivity to a single high dose of bisoprolol; patients with heart failure may be more sensitive to the drug.

In case of overdose, consult a doctor immediately.

In cases of overdose, cases of third degree AV block and dizziness have also been reported.

Treatment: stop taking the drug and carry out supportive and symptomatic treatment. There is limited evidence that bisoprolol is difficult to dialyze.

If necessary, monitoring of respiratory function should be provided; artificial respiration may be indicated.

For bronchospasm: bronchodilators (eg isoprenaline) or β2-adrenergic agonists and/or aminophylline.

For AV blockade of II and III degrees: infusion of isoprenaline; if necessary, cardiac stimulation.

Deterioration of heart failure: intravenous administration of diuretics, vasodilators.

For bradycardia: intravenous administration of atropine. If there is no response, isoprenaline or another drug with a positive chronotropic effect should be administered with caution. In exceptional cases, introduce an artificial pacemaker.

For arterial hypotension: taking vasoconstrictors and plasma expanders, intravenous administration of glucagon.

For hypoglycemia: intravenous administration of glucose.