Bisoprolol
The effectiveness and tolerability of bisoprolol may be affected by concomitant use of other medications. This interaction can also occur when two drugs are taken within a short period of time. The doctor must be informed about taking other medications, even if taken without a doctor's prescription (i.e., over-the-counter drugs).
Combinations not recommended
Treatment of CHF
Class I antiarrhythmic drugs (for example, quinidine, disopyramide, lidocaine, phenytoin; flecainide, propafenone), when used simultaneously with bisoprolol, can reduce AV conduction and myocardial contractility.
All indications for use of the drug Bisoprolol
Blockers of “slow” calcium channels (SCBC) such as verapamil and, to a lesser extent, diltiazem, when used simultaneously with bisoprolol, can lead to a decrease in myocardial contractility and impaired AV conduction. In particular, intravenous administration of verapamil to patients taking beta-blockers can lead to severe arterial hypotension and impaired AV conduction.
Centrally acting antihypertensives (such as clonidine, methyldopa, moxonidine, rilmenidine) can lead to a decrease in heart rate and cardiac output, as well as vasodilation due to a decrease in central sympathetic tone. Abrupt withdrawal, especially before discontinuation of beta-blockers, may increase the risk of developing “rebound” arterial hypertension.
Combinations requiring special caution
Treatment of arterial hypertension and angina pectoris
Class I antiarrhythmic drugs (for example, quinidine, disopyramide, lidocaine, phenytoin; flecainide, propafenone), when used simultaneously with bisoprolol, can reduce AV conduction and myocardial contractility.
All indications for use of the drug Bisoprolol
BMCC dihydropyridine derivatives (for example, nifedipine, felodipine, amlodipine) when used simultaneously with bisoprolol may increase the risk of arterial hypotension. In patients with CHF, the risk of subsequent deterioration in cardiac contractility cannot be excluded. Class III antiarrhythmic drugs (eg, amiodarone) may worsen AV conduction disturbances.
The effect of beta-blockers for topical use (for example, eye drops for the treatment of glaucoma) may enhance the systemic effects of bisoprolol (lowering blood pressure, lowering heart rate).
Parasympathomimetics, when used simultaneously with bisoprolol, may enhance AV conduction disturbances and increase the risk of developing bradycardia.
The hypoglycemic effect of insulin or oral hypoglycemic agents may be enhanced. Signs of hypoglycemia - in particular tachycardia - may be masked or suppressed. Such interactions are more likely when using non-selective beta-blockers.
Agents for general anesthesia may increase the risk of cardiodepressive effects, leading to arterial hypotension (see section "Special Instructions").
Cardiac glycosides, when used simultaneously with bisoprolol, can lead to an increase in impulse conduction time, and thus to the development of bradycardia.
Nonsteroidal anti-inflammatory drugs (NSAIDs) may reduce the antihypertensive effect of bisoprolol.
The simultaneous use of Bisoprolol with beta-agonists (for example, isoprenaline, dobutamine) may lead to a decrease in the effect of both drugs.
The combination of bisoprolol with adrenergic agonists that affect beta and alpha adrenergic receptors (for example, norepinephrine, epinephrine) may enhance the vasoconstrictor effects of these drugs that occur with the participation of alpha adrenergic receptors, leading to an increase in blood pressure. Such interactions are more likely when using non-selective beta-blockers.
Antihypertensive drugs, as well as other drugs with a possible antihypertensive effect (for example, tricyclic antidepressants, barbiturates, phenothiazines) may enhance the antihypertensive effect of bisoprolol.
Mefloquine, when used simultaneously with bisoprolol, may increase the risk of bradycardia.
MAO inhibitors (except MAO B inhibitors) may enhance the antihypertensive effect of beta-blockers. Concomitant use may also lead to the development of a hypertensive crisis.
Allergens used for immunotherapy or allergen extracts used in skin testing increase the risk of anaphylactic reactions.
The clearance of lidocaine and xanthines (except theophylline) may be reduced due to a possible increase in their concentration in the blood plasma, especially in patients with an initially increased clearance of theophylline under the influence of smoking.
The effect of non-depolarizing muscle relaxants and the anticoagulant effect of coumarins may be prolonged during treatment with bisoprolol.
When used simultaneously with rifampicin, a slight decrease in the half-life of bisoprolol is possible due to the induction of hepatic isoenzymes of cytochrome P450 by rifampicin. Usually no dose adjustment is required.
Non-hydrogenated ergot alkaloids and ergotamine increase the risk of developing peripheral circulatory disorders.
Sulfasalazine increases the concentration of bisoprolol in the blood plasma.
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.
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).
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).
