Possibilities of bisoprolol in the treatment of cardiovascular diseases


Pharmacological properties of the drug Bisoprolol-ratiopharm

Selective β1-adrenergic receptor blocker without BCA. Blocks β1-adrenergic receptors and reduces the effect of catecholamines on them. It has a hypotensive and antianginal effect. The hypotensive effect is due to a decrease in IOC, a decrease in sympathetic stimulation of peripheral vessels and inhibition of renin release by the kidneys. The antianginal effect is due to the blockade of β1-adrenergic receptors, which leads to a decrease in heart function due to negative chronotropic and inotropic effects. Thus, bisoprolol (INN - bisoprololum) eliminates or reduces the severity of symptoms of myocardial ischemia. Bisoprolol is almost completely (up to 90%) absorbed from the gastrointestinal tract. The effect of primary passage through the liver is very slight, due to which the drug has high bioavailability - about 90%. The half-life is 10–12 hours, which provides a therapeutic effect for 24 hours when taken once a day. More than 95% of the active substance is excreted by the kidneys, 50% unchanged. Active metabolites are not formed in the human body.

Concor and alcohol

Drinking alcohol with Concor

It is known that when drinking alcohol, blood vessels dilate for a short time, that is, the heartbeat accelerates. True, after a short amount of time the opposite happens - vasospasm. And a sharp rise in blood pressure is not the most pleasant, but also not the most dangerous, thing that can await a patient taking Concor. The instructions directly state that Concor and alcohol are incompatible. The central nervous system is depressed, and the patient’s psychomotor abilities deteriorate. Also, do not forget that the medicine and alcohol will be excreted through one excretory system - the kidneys. This can lead to organ damage, and in some cases functional impairment may develop. Internal bleeding may begin, a hypertensive crisis, pulmonary edema, and vascular collapse may begin. But the worst result of taking Concor and alcohol together is death.

Therefore, doctors strongly recommend that you stop drinking alcohol while taking Concor.

Use of the drug Bisoprolol-ratiopharm

Orally, therapeutic dose - 5-10 mg 1 time per day, maximum daily dose - 20 mg. In patients with impaired renal or liver function (creatinine clearance less than 20 ml/min), the dose of Bisoprolol-ratiopharm should not exceed 10 mg 1 time per day (this dose can be divided into two). In elderly patients, no dose adjustment is required. It is recommended to start using the drug with the lowest possible dose. When discontinuing the drug, the dose is reduced gradually (by half the dose daily).

Concor during pregnancy

Reception during pregnancy is limited

Expectant mothers should be extremely careful when choosing certain medications. In the case of Concor, you can take it only if the benefit to the mother’s body is greater than the damage. Concor should not be taken during lactation, since the baby receives bisoprolol and auxiliary components through breast milk. If discontinuation of the drug is not possible, then breastfeeding should be discontinued.

Contraindications to the use of the drug Bisoprolol-ratiopharm

Hypersensitivity to bisoprolol or other components of the drug, chronic heart failure in the decompensation phase, cardiogenic shock, AV blockade II–III degree, sick sinus syndrome, sinoatrial block II degree, bradycardia (heart rate ≤50 beats/min), tendency to bronchospasms (BA, obstructive airway diseases), arterial hypotension (systolic blood pressure ≤90 mm Hg), late stages of peripheral circulatory disorders, simultaneous use of MAO inhibitors (except MAO-B), age up to 12 years.

Side effects of the drug Bisoprolol-ratiopharm

From the cardiovascular system: bradycardia, arterial hypotension (including orthostatic hypotension), rarely - slowing of AV conduction or strengthening of existing AV blockade, arrhythmias, appearance/intensification of manifestations of heart failure with worsening peripheral circulation, the course of Raynaud's disease, with worsening of existing intermittent claudication. From the side of the central nervous system: increased fatigue, unmotivated weakness, dizziness, headache, rarely - anxiety, irritability, sleep disturbance, depression, confusion (especially in elderly patients), vivid dreams, depressed state. From the gastrointestinal tract: nausea, vomiting, diarrhea, abdominal pain, constipation, increased levels of liver enzymes (AST, ALT), hepatitis. From the respiratory system: rhinitis, shortness of breath, bronchospasm (especially in patients with asthma or a history of obstructive bronchial diseases); Skin reactions: rash. From the hearing organs: hearing loss. From the organs of vision: dry eyes, eye pain, conjunctivitis. Metabolic disorders: increased TG levels, hypoglycemia. In patients with a latent form of diabetes mellitus or manifestations of this disease, it is possible to reduce glucose tolerance and mask the manifestations of hypoglycemia. There have been reports of increased symptoms of psoriasis or the development of a psoriasis-like rash. In isolated cases, during treatment with beta-adrenergic receptor blockers, the following were observed: alopecia, tinnitus, weight gain, emotional lability, temporary memory loss, allergic rhinitis, hypersensitivity reactions, autoimmune disorders such as systemic lupus, decreased sexual function, dysuria, taste disturbance , nonspecific disorders - muscle weakness, cramps, pain in muscles and joints.

Special instructions for the use of the drug Bisoprolol-ratiopharm

Use with caution in patients with first degree AV block, cardiac and peripheral circulatory disorders, including Raynaud's disease and metabolic acidosis. β-adrenergic blockers may provoke or increase the frequency and duration of attacks of vasospastic angina/Prinzmetal angina. It is not recommended to prescribe the drug to patients with COPD or, if necessary, use it in lower doses (initial dose - 2.5 mg / day) in combination with bronchodilators. The drug should be used with caution in patients with diabetes mellitus with significant fluctuations in glycemic levels and metabolic acidosis. For the treatment of patients with severe pheochromocytoma, the drug is used only in combination with β-adrenergic receptor blockers. Bisoprolol-ratiopharm may mask the symptoms of thyrotoxicosis or hypoglycemia. At heart rate ≤50–55 beats/min per 1 min, the dose of the drug should be reduced. In congestive heart failure, it is necessary to evaluate the benefit/risk ratio due to possible inhibition of myocardial contractility. Treatment begins with a minimum dose of 2.5 mg. Bisoprolol-ratiopharm should be used with caution in patients with psoriasis, including a history of psoriasis. The drug may increase sensitivity to allergens and the severity of allergic reactions. In patients with coronary artery disease, sudden withdrawal of the drug may develop withdrawal syndrome. Therefore, drug withdrawal and dose reduction should be done gradually. Each tablet contains approximately 130 mg of lactose, each recommended dose contains 130–260 mg of lactose, which should be advised in patients with galactosemia or glucose/galactose malabsorption syndrome. The drug gives a positive result during doping control. During pregnancy, the use of the drug is possible only after a thorough assessment of the benefit/risk ratio for the mother and fetus. Given the lack of information regarding the content of the drug in breast milk, its use during breastfeeding is not recommended. The drug should not be prescribed to children under 12 years of age due to lack of experience in use. The drug does not affect the ability to drive vehicles or operate other machinery, but due to possible individual reactions, caution should be exercised when using the drug (especially at the beginning of treatment).

Analogs

When choosing analogues, it is important to understand that each of them has its own indications for use, side effects, contraindications, active substances, etc. It is important to consult a doctor and not change the drug yourself.

Which is better: Concor, Bisoprolol, Coronal?

All of these drugs contain the same active substance - bisoprolol. They have similar contraindications and indications for use.

Bisoprolol is used to treat arterial hypertension, tachycardic heart rhythm disorders, ischemia, heart failure and various forms of arrhythmia. It is considered antihypertensive and lowers blood pressure. Patients whose blood pressure is 90 mm or lower (hypotension) are prohibited from taking Bisoprolol. It is easier to tolerate by patients and there is less risk of complications when taking it. This applies to diabetes mellitus, respiratory tract diseases, and hypotension.

Coronal is a generic drug Concor, that is, it has the same spectrum of pharmacological action as the original drug, but differs in strength. Coronal also reduces pain and blood pressure, improves blood supply to the heart muscle, and normalizes heart rhythm. But Coronal does not have such a noticeable effect on the patient’s heart rate.

Which is better: Concor, Betalok Zok, Betalok or Egilok?

The active ingredient in the drugs Betalok ZOK, Betalok and Egilok is the same - metoprolol.

The effectiveness of Concor and Betaloc ZOK in reducing blood pressure and stopping attacks of tachycardia is the same. The duration of the therapeutic effect lasts more than a day. But only a cardiologist has the right to prescribe Concor or Betaloc ZOK, having studied the risk factors, medical history and individual sensitivity of the patient to the components of the drug.

Betaloc is a medicine for hypertension, angina and heart failure. Today it is considered obsolete. He was replaced by Betalok ZOK.

Egilok, like Concor, is effective for high blood pressure, but since the active components are different, there are differences. Compared to Concor, Egilok acts very quickly (15-20 minutes after taking the tablet), but this means that the duration of the therapeutic effect is not so long. The drug should be taken two to three times a day during or after meals.

Which is better: Concor, Nebivolol or Nebilet?

The drugs have a positive effect on the heart with high blood pressure, chronic heart failure, ischemia, tachycardia, but Nebilet and its almost complete analogue Nebivolol are based on the active component - nebivolol, which is capable of dilating peripheral vessels and reducing cardiac output. This adds to its effectiveness as an antihypertensive agent.

The active substance nebivolol promotes the production of nitric oxide, which relaxes blood vessels for a longer period. Unlike Concor, it does not contribute to the patient’s weight gain. Since nebivolol dilates blood vessels, it acts faster, but the effect does not last long.

Nebilet and differing from it solely in the degree of purification and, accordingly, in price, Nebivolol is also used for hypertension and coronary heart disease. But it is contraindicated in patients with low blood pressure, cardiogenic shock, severe heart failure, diseases of the respiratory system and liver. Not for use by children, pregnant and lactating women. Treatment should not be started if you have diabetes, thyroid dysfunction, psoriasis or in old age. Concor is safer for the elderly, children and patients with breathing problems.

Concor or Sotahexal

The active ingredient in Sotahexal, sotalol hydrochloride, copes well with arrhythmia and lowers blood pressure. Contraindicated for use in patients with hypotension.

Sotahexal can cause side effects in the form of bronchospasms, disorders of carbohydrate and lipid metabolism.

Concor, compared to Sotahexal, is easier to tolerate and more effective for patients suffering from chronic heart failure. Also, Concor has a lower risk of complications. This applies to diabetes mellitus (Sotahexal increases hypoglycemia), respiratory diseases, and hypotension. But Sotahexal is more often prescribed for arrhythmic disorders.

Concor or Anaprilin

Anaprilin is a “veteran” of beta-blockers. Time-tested drug. However, since it affects not only the adrenergic receptors of the heart muscle, side effects and dangerous complications develop much more often when taking anaprilin. Therefore, cardiologists advise using new generation beta-blockers, for example, Concor.

Take care of your heart and blood vessels.

Be healthy!

Interactions of the drug Bisoprolol-ratiopharm

Combinations (due to the possibility of decreased activity) with floctafenine, sultopride, and MAO inhibitors (except MAO-B) are contraindicated. Allergens used for immunotherapy, allergen extracts for skin testing in combination with β-adrenergic receptor blockers can provoke the development of severe systemic allergic reactions. Combinations of bisoprolol with calcium antagonists (verapamil, diltiazem, bepridil) are not recommended/require special caution due to an increased negative effect on myocardial inotropic function, AV conductivity, and blood pressure. Drugs containing clonidine, reserpine, alpha-methyldopa should not be prescribed simultaneously with bisoprolol due to a possible slowdown in heart rate. Clonidine, digitalis, guanfacine can inhibit AV conduction. If combination therapy of bisoprolol with clonidine is discontinued, then after stopping clonidine, treatment with bisoprolol should be continued for several more days, ensuring medical monitoring of the patient's condition. Combinations requiring caution: class I antiarrhythmic drugs (eg disopyramide, quinidine, lidocaine, diphenine, propafenone); class III antiarrhythmic drugs (amiodarone, sotalol); calcium antagonists (dihydropyridine derivatives) - due to an increased risk of arterial hypotension and heart failure. The effect of insulin and oral hypoglycemic drugs may be enhanced when used simultaneously with bisoprolol. Cardiac glycosides: decrease in heart rate, prolongation of AV conduction. Baclofen: increased antihypertensive activity. Contrast agents containing iodine: β-adrenergic blockers may increase the risk of anaphylactic reactions. Drugs that block prostaglandin synthesis (in particular NSAIDs): decreased antihypertensive effect. Ergotamine derivatives: exacerbation of peripheral circulatory disorders. Sympathomimetic agents: combination with bisoprolol may reduce the effects of both drugs. Tricyclic antidepressants, barbiturates, phenothiazines, other antihypertensive drugs: enhance the effect of lowering blood pressure. Antihypertensive drugs (diuretics, ACE inhibitors, β-adrenergic receptor blockers) and nitrates potentiate the antihypertensive effect of bisoprolol. Corticosteroids: the antihypertensive effect may be reduced due to water and sodium retention. Inhalation anesthetics and hydrocarbon derivatives (chloroform, cyclopropane, halothane, methoxyfuran, etc.) when used simultaneously with β-adrenergic receptor blockers increase the risk of inhibition of myocardial function and the development of hypotensive reactions. The effect of depolarizing blockers of neuromuscular transmission can be enhanced and prolonged by the influence of beta-adrenergic receptor blockers. Cimetidine may reduce the clearance of β-adrenergic blockers that are metabolized in the liver and accordingly increase their bioavailability. The simultaneous use of rifampicin slightly accelerates the metabolism of bisoprolol, but in this situation there is no need to adjust the dose of the drug. Xanthines (aminophylline, theophylline) may mutually reduce the therapeutic effects when combined with beta-adrenergic receptor blockers.

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