Bisoprolol, 30 pcs., 5 mg, film-coated tablets
The effectiveness and tolerability of bisoprolol may be affected by the simultaneous use of other drugs. This interaction can also occur when two drugs are taken within a short period of time.
The doctor must be informed about the use of other medications, even if they are used without a doctor’s prescription (that is, over-the-counter drugs).
Combinations not recommended
Class I antiarrhythmic drugs (for example, quinidine, disopyramide, lidocaine, phenytoin, flecainide, propafenone), when used simultaneously with bisoprolol, can reduce AV conduction and myocardial contractility.
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 symptoms of 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
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 (for example, amiodarone), when used simultaneously with bisoprolol, may increase 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 an interaction is more likely when using non-selective beta-blockers.
General anesthesia products
Can increase the risk of cardiodepressive effects, leading to arterial hypotension (see section "Special Instructions").
Cardiac glycosides
When used simultaneously with bisoprolol, they 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 alpha and beta 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.
When bisoprolol is combined with norepinephrine and epinephrine, aggravation of intermittent claudication may occur.
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.
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.
Tricyclic and tetracyclic antidepressants, antipsychotics (neuroleptics), ethanol, sedatives and hypnotics increase depression of the central nervous system.
Diuretics, sympatholytics, hydralazine and other antihypertensive drugs can lead to an excessive decrease in blood pressure.
The effect of non-depolarizing muscle relaxants and the anticoagulant effect of coumarins may be prolonged during treatment with bisoprolol.
Mefloquine
When used simultaneously with bisoprolol, it can increase the risk of developing 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. The break between taking MAO inhibitors and bisoprolol should be at least 14 days.
Rifampicin
There may be a slight decrease in the half-life of bisoprolol due to the induction of hepatic isoenzymes of cytochrome P450 by rifampicin. Usually no dose adjustment is required.
Ergotamine derivatives
Non-hydrogenated ergot alkaloids increase the risk of developing peripheral circulatory disorders. Ergotamine increases the risk of developing peripheral circulatory disorders.
Sulfasalazine increases the concentration of bisoprolol in the blood plasma.
Bisoprolol 5 mg, 30 film-coated tablets
Registration Certificate Holder
RAFARMA (Russia)
Dosage form
Medicine - Bisoprolol (Bisoprolol)
Description
Film-coated tablets
from yellow to dark yellow, round, biconvex, scored and chamfered; On a cross section, the kernel is white to yellowish-white.
1 tab.
bisoprolol fumarate 5 mg
Excipients
: microcrystalline cellulose - 91 mg, corn starch - 43.7 mg, croscarmellose sodium - 2.9 mg, magnesium stearate - 1.5 mg, colloidal silicon dioxide - 1.4 mg.
Film shell composition:
opadry II yellow - 4.5 mg, including polyvinyl alcohol - 1.8 mg, macrogol - 0.909 mg, titanium dioxide - 0.877 mg, talc - 0.666 mg, iron dye yellow oxide - 0.2475 mg, iron oxide black - 0.0005 mg.
10 pieces. — contour cellular packaging (aluminum/PVC) (3) — cardboard packs. 10 pieces. — cellular contour packages (aluminum/PVC) (5) — cardboard packs. 10 pieces. — contour cellular packaging (aluminum/PVC) (10) — cardboard packs. 100 pieces. — polymer jars (1) — cardboard packs.
Indications
Arterial hypertension, prevention of angina attacks, chronic heart failure.
Contraindications for use
Acute heart failure, chronic heart failure in the stage of decompensation, cardiogenic shock, collapse, AV block of II and III degrees (without a pacemaker), SSSU; sinoatrial blockade, severe bradycardia (heart rate <50 beats/min), Prinzmetal's angina, marked decrease in blood pressure (systolic blood pressure <90 mm Hg), history of severe forms of bronchial asthma and COPD, late stages of peripheral circulatory disorders, Raynaud's disease , pheochromocytoma (without simultaneous use of alpha-blockers), metabolic acidosis, simultaneous use of MAO inhibitors (except for MAO type B inhibitors), children and adolescents under 18 years of age, hypersensitivity to bisoprolol and other beta-blockers.
pharmachologic effect
A selective beta1-blocker without internal sympathomimetic activity and does not have membrane stabilizing activity. Reduces plasma renin activity, reduces myocardial oxygen demand, reduces heart rate (at rest and during exercise) and cardiac output, while stroke volume does not decrease significantly. Inhibits AV conduction. Has antianginal and hypotensive effects. In high doses (200 mg or more) it can cause blockade of β2-adrenergic receptors, mainly in the bronchi and vascular smooth muscles.
The hypotensive effect is associated with a decrease in minute blood volume, sympathetic stimulation of peripheral vessels, a decrease in the activity of the renin-angiotensin system (of greater importance for patients with initial hypersecretion of renin), restoration of sensitivity in response to a decrease in blood pressure and an effect on the central nervous system.
The antianginal effect is due to a decrease in myocardial oxygen demand as a result of a decrease in heart rate and decreased contractility, prolongation of diastole, and improved myocardial perfusion.
The antiarrhythmic effect is due to the elimination of arrhythmogenic factors (tachycardia, increased activity of the sympathetic nervous system, increased cAMP content, arterial hypertension), a decrease in the rate of spontaneous excitation of sinus and ectopic pacemakers and a slowdown in AV conduction (mainly in the antegrade and, to a lesser extent, in the retrograde directions via the AV node) and along additional paths.
Drug interactions
With the simultaneous use of antacids and antidiarrheals, the absorption of beta-blockers may be reduced.
With the simultaneous use of antiarrhythmic drugs, a sharp decrease in blood pressure, a decrease in heart rate, and the development of arrhythmia and/or heart failure are possible.
With the simultaneous use of antihypertensive drugs, the antihypertensive effect may be enhanced.
With the simultaneous use of cardiac glycosides, conduction disturbances are possible.
With the simultaneous use of sympathomimetics (including those included in cough suppressants, nasal drops, eye drops), the effectiveness of bisoprolol decreases.
With the simultaneous use of verapamil and diltiazem, a sharp decrease in blood pressure, a decrease in heart rate, and the development of arrhythmia and/or heart failure are possible.
With simultaneous use of guanfacine, severe bradycardia and conduction disturbances are possible.
With the simultaneous use of insulin and hypoglycemic agents for oral administration, the effect of insulin or other hypoglycemic agents is enhanced (regular monitoring of plasma glucose levels is necessary).
With simultaneous use of clonidine, severe bradycardia, arterial hypotension, and conduction disturbances are possible.
In case of sudden withdrawal of clonidine in patients receiving bisoprolol, a sharp increase in blood pressure is possible.
With the simultaneous use of nifedipine, other calcium channel blockers, dihydropyridine derivatives, the antihypertensive effect of bisoprolol is enhanced.
With the simultaneous use of reserpine and alpha-methyldopa, severe bradycardia is possible.
With simultaneous use of rifampicin, a slight decrease in T1/2 of bisoprolol is possible.
With the simultaneous use of ergotamine derivatives (including drugs for the treatment of migraines containing ergotamine), symptoms of peripheral circulatory disorders increase.
Dosage regimen
Individual. For oral administration, the daily dose is 2.5-10 mg, the frequency of administration is 1 time / day. Maximum daily dose
- 10 mg.
Side effect
From the nervous system:
weakness, fatigue, dizziness, headache, sleep disorders, mental disorders (depression, rarely hallucinations), feeling of cold and paresthesia in the extremities.
From the cardiovascular system:
orthostatic hypotension, bradycardia, impaired AV conduction, the appearance of symptoms of heart failure, worsening intermittent claudication and the main clinical symptoms of Raynaud's syndrome.
From the side of the organ of vision:
decreased secretion of tear fluid, conjunctivitis.
From the digestive system:
diarrhea, constipation, nausea, abdominal pain.
From the musculoskeletal system:
muscle weakness, muscle cramps.
For the skin and subcutaneous tissues:
skin itching;
in some cases - increased manifestations of psoriasis, the appearance of psoriasis-like rashes. From the respiratory system:
in predisposed patients, symptoms of bronchial obstruction may appear.
Other:
sweating, hot flashes, impaired potency, decreased glucose tolerance in patients with diabetes, allergic reactions.
special instructions
Use with caution for psoriasis and when there is a family history of psoriasis, diabetes mellitus in the decompensation phase, or with a predisposition to allergic reactions. In case of pheochromocytoma, the use of bisoprolol is possible only after taking alpha-blockers. Avoid abrupt withdrawal of bisoprolol; the course of treatment should be completed slowly with a gradual reduction in dose. Before surgery, the anesthesiologist should be informed about treatment with bisoprolol.
Bisoprolol at a dose of more than 10 mg/day should be used only in exceptional cases.
This dose should not be exceeded in case of renal failure (creatinine clearance less than 20 ml/min) and severe liver dysfunction.
During the treatment period, avoid drinking alcohol.
Effect on the ability to drive vehicles and operate machinery.
Use with caution in patients whose activities require concentration and high speed of psychomotor reactions.
Use during pregnancy and breastfeeding
Restrictions during pregnancy - Contraindicated. Restrictions when breastfeeding - Contraindicated.
Use during pregnancy and lactation is not recommended and is possible only in cases where the expected benefit to the mother outweighs the potential risk of side effects in the fetus and child.
In exceptional cases of use during pregnancy, bisoprolol should be discontinued 72 hours before the expected due date due to the possibility of bradycardia, arterial hypotension, hypoglycemia and respiratory depression in the newborn. If discontinuation is not possible, then the condition of the newborn must be carefully monitored for 72 hours after birth.
If it is necessary to use bisoprolol during lactation, breastfeeding should be stopped.
Use for renal impairment
Restrictions for impaired renal function - With caution. Do not exceed the dose of 10 mg/day in case of renal failure (creatinine clearance less than 20 ml/min).
Use for liver dysfunction
Restrictions for liver dysfunction - With caution.
The dose should not exceed 10 mg/day in case of severe liver dysfunction.
Use in children
Restrictions for children - Contraindicated. Use in children is not recommended.
