Indications
Arterial hypertension, angina pectoris, post-infarction period, arrhythmias, chronic heart failure (moderate, stable without exacerbation during the last 6 weeks).
$16.00
Active ingredient: | |
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Dosage form: | |
Indications for use: |
Arterial hypertension, angina pectoris, post-infarction period, arrhythmias, chronic heart failure (moderate, stable without exacerbation during the last 6 weeks).
Hypersensitivity, sinus bradycardia (less than 45-50 beats/min), sinus node weakness syndrome, sinoatrial and AV block II–III degrees, cardiogenic shock, acute and refractory to treatment severe heart failure, acute myocardial infarction, hypotension (sBP below 90 mm Hg), severe obstructive respiratory failure, pregnancy, breast-feeding.
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.
1 tablet contains:
Active ingredient:
bisoprolol fumarate 2.5 mg
excipients:
lactose monohydrate – 68.15 mg,
microcrystalline cellulose-16 mg,
magnesium stearate-0.35 mg,
crospovidone-3 mg
Selective beta-1-adrenoblocker without internal sympathomimetic activity, does not have membrane-stabilizing activity. Reduces the activity of plasma renin, reduces the need for myocardial oxygen, reduces heart rate (at rest and during exercise) and cardiac output, while the stroke volume does not significantly decrease. Inhibits AV conduction. It has antianginal and antihypertensive effects. In high doses (200 mg or more) it can cause blockade of beta-2-adrenergic receptors mainly in the bronchi and in 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 (which is more important 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 the myocardial oxygen demand as a result of a decrease in heart rate and contractility, an elongation of the 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 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 through the AV node) and along additional pathways.
Pharmacokinetics
Absorption – 80-90%, food intake does not affect absorption.
Cmax in blood plasma is reached in 2-4 hours. Binding to plasma proteins is 26-33%. Bisoprolol penetrates the BBB and placental barrier to a small extent; it is excreted in breast milk.
It is metabolized in the liver.
T1/2 – 9-12 hours. Excreted by the kidneys-50% unchanged, less than 2% – with bile.
Arterial hypertension, angina pectoris, post-infarction period, arrhythmias, chronic heart failure (moderate, stable without exacerbation during the last 6 weeks).
Hypersensitivity, sinus bradycardia (less than 45-50 beats/min), sinus node weakness syndrome, sinoatrial and AV block II–III degrees, cardiogenic shock, acute and refractory to treatment severe heart failure, acute myocardial infarction, hypotension (sBP below 90 mm Hg), severe obstructive respiratory failure, pregnancy, breast-feeding.
The frequency of side effects is indicated when prescribing doses not exceeding 40 mg.
From the nervous system and sensory organs: dizziness (3.5%), insomnia (2.5%), asthenia (1.5%), hypesthesia (1.5%), depression (0.2%), drowsiness, anxiety, paresthesia (feeling of cold in the extremities), hallucinations, impaired thinking, concentration, orientation in time and space, balance, emotional lability, tinnitus, conjunctivitis, visual disturbances, decreased secretion of tear fluid, convulsions.
From the cardiovascular system and blood (hematopoiesis, hemostasis): bradycardia (0.5%), arrhythmia, palpitation, AV block, hypotension, heart failure, microcirculation disorders in the myocardium and extremities, intermittent claudication, vasculitis, agranulocytosis, thrombocytopenia, thrombocytopenic purpura.
Gastrointestinal disorders: diarrhea (3.5%), nausea (2.2%), vomiting (1.5%), dry mouth (1.3%), dyspeptic symptoms, constipation, ischemic colitis, mesenteric artery thrombosis.
From the respiratory system: cough (2.5%), shortness of breath (1.5%), broncho – and laryngospasm, pharyngitis (2.2%), rhinitis (4%), sinusitis (2.2%), respiratory tract infections (5%), respiratory distress syndrome.
From the genitourinary system: peripheral edema (3%), decreased libido, impotence, Peyronie’s disease, cystitis, renal colic.
Skin disorders: rash, acne, eczema-like reactions, prurigo, redness of the skin, hyperhidrosis, dermatitis, alopecia.
From the side of metabolism: increased concentration of liver enzymes (AST, ALT), hyperglycemia or increased glucose tolerance, hyperuricemia, changes in the concentration of potassium in the blood.
Other: pain syndrome (headache-10.9%, arthralgia-2.7%, myalgia, abdominal pain, chest pain — 1.5%, eyes, ears), weight gain.
With simultaneous use of antacids and antidiarrheal agents, it is possible to reduce the absorption of beta-blockers. With simultaneous use of antiarrhythmic drugs, a sharp decrease in blood pressure, a decrease in heart rate, the development of arrhythmia and/or heart failure may occur. With the simultaneous use of antihypertensive agents, the antihypertensive effect may increase. With simultaneous use of cardiac glycosides, conduction disturbances may occur. With the simultaneous use of sympathomimetics (including those included in cough remedies, nasal drops, eye drops), the effectiveness of bisoprolol decreases. With the simultaneous use of verapamil, diltiazem, a sharp decrease in blood pressure, a decrease in heart rate, the development of arrhythmia and/or heart failure is possible. With the simultaneous use of guanfacine, severe bradycardia and conduction disturbances are possible. With simultaneous use of insulin, hypogligemic agents for oral use, the effect of insulin or other hypogligemic agents increases (regular monitoring of blood glucose levels is necessary). With the simultaneous use of clonidine, severe bradycardia, arterial hypotension, and conduction disorders are possible. In case of sudden withdrawal of clonidine in patients receiving bisoprolol, a sharp increase in blood pressure may occur. 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, alpha-methyldopa, severe bradycardia is possible. With simultaneous use of rifampicin, a slight decrease in T1/2 bisoprolol is possible. Concomitant use of ergotamine derivatives (including drugs for the treatment of migraines containing ergotamine) increases the symptoms of peripheral circulatory disorders.
The dosage regimen is individual.
For oral use, the daily dose is 2.5-10 mg, the frequency of use is 1 time/day.
The maximum daily dose is 10 mg.
Consideration should be given to the possibility of masking the symptoms of hypoglycemia and thyrotoxicosis during treatment.
It is possible to increase the severity of hypersensitivity reactions and the lack of effect from conventional doses of epinephrine against the background of a burdened allergic history.
In severe hepatic impairment, acute renal failure (creatinine clearance less than 20 ml/min), patients undergoing hemo – or peritoneal dialysis, the dose should be reduced. When pheochromocytoma should not be prescribed without additional use of alpha-blockers.
Bisoprolol reduces compensatory cardiovascular reactions in response to the use of general anesthetics and iodine-containing contrast agents.
It is necessary to cancel the drug 48 hours before anesthesia or choose an anesthetic with the least negative inotropic effect.
Treatment should be discontinued gradually, over a period of approximately 2 weeks (withdrawal syndrome is possible).
Use with caution when working for drivers of vehicles and people whose profession is associated with increased concentration of attention.
It is necessary to exclude the use of alcoholic beverages during treatment (risk of orthostatic hypotension).
Tablets
Store in a dry place, protected from light, at a temperature not exceeding 25 °C.
Bisoprolol
By prescription
Tablets
For adults as directed by your doctor
Heart Failure, Hypertension, Arrhythmia
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