Bisoprolol

Brand Chanelle Medical

In stock 1429 Items

Available since: 2019-09-19

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Clinical Pharmacology

Selective beta₁-adrenergic blocker without internal sympathomimetic activity, does not possess membrane stabilizing activity. It reduces plasma renin activity, reduces myocardial oxygen demand, reduces heart rate (at rest and under load) and cardiac output, while the stroke volume does not significantly decrease. Inhibits AV conductivity. It has antianginal and hypotensive effects. In high doses (200 mg or more) can cause blockade and β₂-adrenoreceptors mainly in the bronchi and vascular smooth muscle.

The hypotensive effect is associated with a decrease in the minute volume of blood, sympathetic stimulation of peripheral vessels, a decrease in the activity of the renin-angiotensin system (important for patients with initial renin hypersecretion), the restoration of sensitivity in response to a decrease in blood pressure and an effect on the CNS.

The antianginal effect is due to a decrease in myocardial oxygen demand as a result of a decrease in heart rate and a decrease in contractility, a prolongation of diastole, and an improvement in myocardial perfusion.

The antiarrhythmic effect is due to the elimination of arrhythmogenic factors (tachycardia, increased activity of the sympathetic nervous system, increased cAMP, 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 retrograde directions through the AV node) and along additional paths.

Pharmacokinetics

Indications

Arterial hypertension, angina pectoris, post-infarction period, arrhythmias, chronic heart failure (moderately severe, stable without exacerbation during the last 6 weeks).

Composition

1 tablet contains:
active substance: bisoprolol fumarate 2.5 mg
Excipients: lactose monohydrate - 68.15 mg, microcrystalline cellulose - 16 mg, magnesium stearate - 0.35 mg, crospovidone - 3 mg.

Bisoprolol is marketed under different brands and generic names, and comes in different dosage forms:

Brand name	Manufacturer	Country	Dosage form
Cordinorm	Chanelle Medical	Ireland	pills
Biprol	Makiz-Pharma	Russia	pills
Bisoprolol	Izvarino Pharma	Russia	pills
Biol	S.I.F.I. S.p.A	Italy	pills
Aritel	Canonpharma	Russia	pills
Biprol	Hemofarm	Serbia	pills
Bidop	Gedeon Richter	Hungary	pills
Bisoprolol	Vertex	Russia	pills
Bisoprolol-SZ	North Star	Russia	pills
Coronal	Saneka Pharmaceuticals a.s	Czech	pills
Niperten	Krka dd Novo mesto AO	Slovenia	pills
Biol	Sandoz	Switzerland	pills
Cordinorm	Catalent Germani Schorndorf GmbH	Germany	pills
Bisoprolol-teva	Teva	Israel	pills
Bisogamma	Verwag Pharma	Germany	pills

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Dosage and Administration

Biprol drug is taken orally, in the morning, 1 time per day with a small amount of liquid, before breakfast, during or after it. pills should not be chewed or powdered. In all cases, the reception and dose regimen is selected by the doctor for each patient individually, in particular, taking into account the heart rate and the patient's condition.
In case of arterial hypertension and ischemic heart disease, the drug is prescribed 5 mg 1 time per day. If necessary, increase the dose to 10 mg 1 time per day. In the treatment of hypertension and angina, the maximum daily dose is 20 mg 1 time per day.
For patients with severe impaired renal function (creatinine clearance less than 20 ml / min) or with severe impaired liver function, the maximum daily dose is 10 mg 1 time per day. Increasing the dose in these patients should be carried out with extreme caution.
Elderly patients dose adjustment is not required.

Adverse reactions

The frequency of the side effects listed below is indicated in accordance with the WHO classification: very often - more than 10%; often more than 1% and less than 10%; infrequently - more than 0.1% or less
one%; rarely more than 0.01% and less than 0.1%; very rarely - less than 0.01%, including some cases.
From the central and peripheral nervous system: often - increased fatigue, asthenia, dizziness, headache. Usually these phenomena develop at the beginning of treatment, as a rule, are expressed slightly and disappear within 1-2 weeks; infrequently - sleep disturbances, depression; rarely - nightmares, hallucinations, loss of consciousness.
Since the cardiovascular system: very often - bradycardia, palpitations; often - marked reduction in blood pressure (especially in patients with CHF), manifestations of angiospasm (increased disturbance of the peripheral circulation, feeling cold in the extremities (paresthesia); rarely - impaired AV conduction (up to the development of complete transverse blockade and cardiac arrest), arrhythmias, aggravation
chronic heart failure with the development of peripheral edema (swelling of the ankles, feet) and shortness of breath, orthostatic hypotension, chest pain.
On the part of the digestive system: often - nausea, vomiting, diarrhea, abdominal pain,
constipation, dryness of the oral mucosa; rarely, hepatitis, increased activity of liver transaminases (alanine aminotransferase, aspartate aminotransferase), increased bilirubin concentration.
On the part of the respiratory system: infrequently - laryngo- and bronchospasm in patients with
bronchial asthma or obstructive airway diseases; seldom -
allergic rhinitis, nasal congestion.
On the part of the musculoskeletal system: infrequently - muscular weakness, cramps in the calf muscles, arthralgia.
On the part of the senses: rarely - impaired vision, reduction of tearing (should be considered when wearing contact lenses), hearing loss, change in taste;
very rarely - dry and sore eyes, conjunctivitis.
For the skin: rarely - increased sweating, psoriasis-like skin reactions; very rarely - alopecia, exacerbation of the course of psoriasis.
On the part of the endocrine system: rarely - hypoglycemia.
From the genitourinary system: rarely - a violation of potency, weakening of libido.
On the part of the immune system: rarely - the appearance of antinuclear antibodies with unusual clinical symptoms of lupus-like syndrome, which disappear after the end of treatment.
Allergic reactions: rarely - skin hyperemia, pruritus, skin rash, urticaria.
Laboratory indicators: rarely - hypertriglyceridemia; very rarely - thrombocytopenia, agranulocytosis, leukopenia.
Other: rarely - the syndrome of "cancel" (increased angina attacks, increased blood pressure).

Contraindications

Hypersensitivity to bisoprolol, other components of the drug and other beta-blockers; shock (including cardiogenic); pulmonary edema; acute heart failure or CHF in the decompensation stage, requiring inotropic therapy; AV block II-III degree, without pacemaker; sinoatrial blockade; sick sinus syndrome; bradycardia (heart rate less than 60 beats / min); Prinzmetal angina pectoris; cardiomegaly (without signs of heart failure); severe hypotension (systolic blood pressure less than 100 mm Hg), especially with myocardial infarction; severe bronchial asthma and chronic obstructive pulmonary disease (COPD) in history; simultaneous use of phloctafenin, luprid, monoamine oxidase inhibitors (MAO), with the exception of MAO type B; simultaneous intravenous administration of verapamil or diltiazem; severe peripheral circulatory disorders, Raynaud's syndrome; pheochromocytoma (without the simultaneous use of alpha-blockers); metabolic acidosis; age up to 18 years (efficacy and safety have not been established).
Lactase deficiency, lactose intolerance, lactose / isomaltose malabsorption syndrome (lactose is part of the drug).
Carefully
Severe liver failure, severe renal insufficiency (creatinine clearance less than 20 ml / min), myasthenia, thyrotoxicosis, diabetes mellitus (can mask the symptoms of hypoglycemia), burdened allergy history, AV block I degree, depression (including history), psoriasis, bronchial asthma, COPD, impaired peripheral circulation, strict diet.

Drug interactions

Floctafenin. In the case of shock or hypotension caused by floctafenin, beta-blockers cause a decrease in compensatory cardiovascular reactions (combined use is contraindicated).
Sultopride Due to the additive effect may develop severe bradycardia (combined use is contraindicated).
MAO inhibitors. It is not recommended simultaneous use (with the exception of MAO type B), since there is a high probability of a significant increase in the antihypertensive effect. A break in treatment between taking MAO inhibitors and bisoprolol should be at least 14 days.
Slow calcium channel blockers (diltiazem and verapamil). This combination should be avoided. During the period of treatment with Biprol, intravenous administration of verapamil or diltiazem, other antiarrhythmic drugs is contraindicated. Due to the synergism of the action, a sharp decrease in blood pressure, automatism disorders (severe bradycardia, sinus node arrest), AV conduction disorders, heart failure are possible. If necessary, the appointment of such a combination requires careful clinical and electrocardiographic observation of patients, especially the elderly and at the beginning of treatment.
Class I antiarrhythmic drugs (for example, quinidine, disopyramide, lidocaine, phenytoin; flecainide, propafenone) with simultaneous use may decrease
AV conductivity and myocardial contractility (combination with bisoprolol should be avoided).
Class III antiarrhythmic drugs (for example, amiodarone). When combined with bisoprolol may be a violation of contractility, automatism and conduction due to inhibition of sympathetic compensatory mechanisms (this combination should be avoided).
Antihypertensive agents of central action (clonidine, apraclonidine, alpha-methyldopa, guanfantsin, moxonidine, rilmenidine). When combined, increasing the risk of developing severe bradycardia, stopping the sinus node, AV conduction disturbances, a sharp decrease in blood pressure, heart failure (synergistic effect).This combination should be avoided. If necessary, careful clinical and electrocardiographic monitoring is required, especially in elderly patients and at the beginning of treatment. A significant increase in blood pressure during the abrupt cancellation of the antihypertensive drug of central action
Cardiac glycosides. Decrease in heart rate, conduction disturbance.
Beta-blockers for local use (for example, eye drops for the treatment of glaucoma) can enhance the systemic effect of bisoprolol (lower blood pressure, decrease the heart rate).
Calcium channel blockers (eg, nifedipine). Excessive lowering of blood pressure is possible.
Parasympathomimetics. When combined, the risk of developing bradycardia.
Meflokhin. Combined use with bisoprolol increases the risk of developing bradycardia (additive effect).
Phenytoin when administered intravenously, drugs for inhalation general anesthesia (derivatives of hydrocarbons) increase the severity of the cardiodepressant action and the likelihood of lowering blood pressure.
Simultaneous use with beta-adrenomimetics (for example, isoprenaline, dobutamine) can lead to a decrease in the effect of both drugs.
The combination of bisoprolol with adrenergic drugs that affect beta and alpha adrenergic receptors (for example, norepinephrine, epinephrine) can enhance the vasoconstrictor effect of these agents, which occurs with the participation of alpha adrenoreceptors, leading to an increase in blood pressure. Such interactions are more likely when using non-selective beta-blockers.
Bisoprolol can change the effectiveness of insulin and hypoglycemic agents for oral administration, to mask the symptoms of developing hypoglycemia (tachycardia, high blood pressure).
Bisoprolol reduces the clearance of lidocaine and xanthines (except difillin) and increases their plasma concentration, especially in patients with initially elevated clearance of theophylline under the influence of smoking.
The antihypertensive effect is weakened by nonsteroidal anti-inflammatory drugs (sodium ion retention and prostaglandin synthesis blockade by the kidneys), glucocorticosteroids and estrogens (sodium ion retention).
Diuretics, sympatholytics, hydralazine and other antihypertensive drugs. Risk of excessive blood pressure reduction.
Bisoprolol prolongs the action of non-depolarizing muscle relaxants and the anticoagulant effect of coumarins.
Tri- and tetracyclic antidepressants, antipsychotic drugs (neuroleptics), ethanol, sedatives and hypnotics drugs - when used together with bisoprolol, increased inhibition of the central nervous system.
Unhydrogenated ergot alkaloids increase the risk of developing peripheral circulatory disorders.
Ergotamine increases the risk of developing impaired peripheral circulation.
Sulfasalazine increases plasma concentration of bisoprolol.
Rifampicin reduces the half-life of bisoprolol.
Allergens used for immunotherapy or allergen extracts for skin tests increase the risk of severe systemic allergic reactions or anaphylaxis in patients receiving bisoprolol.
Iodine radiopaque diagnostic tools for intravenous administration increase the risk of anaphylactic reactions.

Special instructions

Drug treatment is usually long-term.
Before starting treatment, it is recommended to conduct a study of respiratory function in patients with a burdened bronchopulmonary history. Bisoprolol can be prescribed to patients with bronchospastic diseases in case of intolerance and / or ineffectiveness of other antihypertensive drugs, and the dose of the drug should be strictly monitored.Overdose is dangerous for the development of bronchospasm.
Monitoring of patients taking bisoprolol should include monitoring of heart rate, blood pressure (at the beginning of treatment - daily, then once every 3-4 months), electrocardiogram, plasma glucose concentration in patients with diabetes mellitus (1 time in 4 -5 months). In elderly patients, it is recommended to monitor renal function (1 time in 4-5 months). The patient should be trained in the method of counting the heart rate and instructed on the need for medical advice while reducing it to less than 60 beats / min.
In approximately 20% of patients with angina pectoris, beta-blockers are ineffective. The main causes are severe coronary atherosclerosis with a low ischemic threshold (heart rate less than 100 beats / min) and an increase in the end-diastolic volume of the left ventricle, which violates the subendocardial blood flow. In smokers, the effectiveness of beta-blockers is lower.
Patients using contact lenses should take into account that a decrease in the production of tear fluid is possible during treatment.
When used in patients with pheochromocytoma, there is a risk of development of paradoxical arterial hypertension (unless effective alpha adrenoblockade has been previously achieved).
With thyrotoxicosis, bisoprolol may mask certain clinical signs of thyrotoxicosis (for example, tachycardia). Abrupt cancellation in patients with thyrotoxicosis is contraindicated, as it can enhance symptoms.
In case of diabetes mellitus it may mask tachycardia caused by hypoglycemia. Unlike non-selective beta-adrenergic blockers, it practically does not increase insulin-induced hypoglycemia and does not delay the restoration of glucose concentration in the blood to normal levels.
With simultaneous use of clonidine, its reception can be terminated only a few days after the cancellation of bisoprolol.
Perhaps an increase in the severity of hypersensitivity reactions and the lack of effect from the usual doses of epinephrine on the background of aggravated allergic history.
In the case of the need for a planned surgical intervention cancellation
The preparation is carried out 48 hours before the start of general anesthesia. If the patient has taken the drug before surgery, he should choose a drug for general anesthesia with minimal negative inotropic effect.
Reciprocal activation of the vagus nerve can be eliminated by intravenous administration of atropine (1-2 mg).
Drugs that reduce catecholamine reserves (for example, reserpine) can enhance the effect of beta-blockers, so patients taking such combinations of drugs should be under constant medical supervision to detect arterial hypotension or bradycardia.
In the case of elderly patients, increasing bradycardia (less than 60 beats / min), arterial hypotension (systolic blood pressure below 100 mm Hg), AV blockade, bronchospasm, ventricular arrhythmias, severe liver dysfunction and stop treatment.
You can not abruptly interrupt treatment with bisoprolol because of the risk of developing severe arrhythmias and myocardial infarction. Cancellation is carried out gradually, reducing the dose for 2 weeks or more (the dose is reduced by 25% in 3-4 days).
It is recommended to stop therapy (with a gradual decrease in dose) with the development of depression caused by taking the drug. The drug should be discontinued before the study of the content in the blood and urine of catecholamines, normetanephrine and vanillimndalnoy acid titer of antinuclear antibodies.
Influence on ability to drive vehicles and work with mechanisms
During the period of treatment, care must be taken when driving and performing other potentially hazardous activities that require high concentration of attention and psychomotor speed.

Overdosage

Symptoms: arrhythmia, ventricular extrasystole, severe bradycardia, AV block, marked reduction in blood pressure, acute heart failure, hypoglycemia, acrocyanosis, difficulty breathing, bronchospasm, dizziness, fainting, seizures.
Treatment: gastric lavage, the appointment of adsorbing agents, symptomatic therapy. In severe bradycardia, intravenous atropine. If the effect is insufficient, with caution you can enter a tool that has a positive chronotropic effect. Sometimes it may require a temporary setting of an artificial pacemaker.
With advanced AV blockade, intravenous administration of 1-2 mg of atropine, epinephrine, or the installation of a temporary pacemaker.
For ventricular extrasystoles - lidocaine (class IA drugs are not used). With a marked decrease in blood pressure, the patient should be moved to the Trendelenburg position; if there are no signs of pulmonary edema, intravenous administration of plasma-substituting solutions, with their ineffectiveness, administration of epinephrine, dopamine, dobutamine (to maintain chronotropic and inotropic action and eliminate marked reduction in blood pressure).
For hypoglycemia, intravenous administration of a dextrose (glucose) solution may be indicated. In heart failure - cardiac glycosides, diuretics. When convulsions - intravenous diazepam. When bronchospasm is inhaled beta2-adrenergic mimetics.