Description
Release form
Tablets
Pharmacological action
Selective beta1-blocker without internal sympathomimetic activity, 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 significantly decrease. Inhibits AV conduction. It has antianginal and hypotensive effects. In high doses (200 mg or more), it can cause blockade and 2-adrenoreceptors mainly in the bronchi and in the smooth muscles of blood vessels.
The antihypertensive 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 (more important for patients with initial renal hypersecretion), restoration of sensitivity in response to a decrease in blood pressure and effects on the central nervous system.
The antianginal effect is due to a decrease in myocardial oxygen demand as a result of decreased heart rate and reduced contractility, lengthening of diastole, and improved myocardial perfusion.
Antiarrhythmic effect is due to the elimination of arrhythmogenic factors (tachycardia, increased activity of the sympathetic nervous system, increased content of cAMP, arterial hypertension), a decrease in the rate of spontaneous excitation of sinus and ectopic pacemakers, and a slowdown in AV conduction (mainly in antegrade and, to a lesser extent, in retrograde directions through the AV node) and along additional paths.
Pharmacokinetics
Absorption – 80-90%, food intake does not affect absorption.
Cmax in plasma is reached after 2-4 hours. Binding to plasma proteins – 26-33%. Bisoprolol to a small extent crosses the BBB and the placental barrier is excreted in breast milk.
Metabolized in the liver.
T1 / 2 – 9-12 hours. It is excreted by the kidneys – 50% unchanged, less than 2% – with bile.
Indications
Arterial hypertension, angina pectoris, post-infarction period, arrhythmias, chronic heart failure (moderate, stable without exacerbation during the last 6 weeks).
Contraindications
Hypersensitivity, concomitant use with tizanidine (risk of pronounced decrease in blood pressure, drowsiness), age up to 18 years (until the completion of the skeleton formation process, sinoatrial and AV block II III degree, cardiogenic shock, acute and refractory treatment of severe heart failure, acute myocardial infarction, arterial hypotension (SBP below 90 mm Hg), severe obstructive respiratory failure, pregnancy, breast-feeding.
Use during pregnancy and lactation
It is possible if the expected effect of therapy in the mother outweighs the potential risk to the fetus and the baby (there were no adequate and strictly controlled studies of the safety of pregnant and lactating women) .
Since there is a risk of developing bradycardia, hypotension, hypoglycemia, and respiratory distress (neonatal asphyxia) in newborns, treatment with bisoprolol fumarate should be discontinued 48 ² 72 hours before delivery.
If this is not possible, the newborn should be under close medical supervision for 48 ² 72 hours after birth.
The secretion of bisoprolol fumarate with breast milk has not been studied, but since it is secreted into breast milk in rats (less than 2%), infants should be under medical supervision.
FDA category of effect on the fetus is C.
Special instructions
The possibility of masking the symptoms of hypoglycemia and thyrotoxicosis during treatment should be considered.
It is possible to increase the severity of hypersensitivity reactions and the lack of effect of the usual doses of adrenaline against the background of a burdened allergic history.
In severe hepatic impairment, acute renal failure (creatinine Cl less than 20 ml / min), patients undergoing hemo- or peritoneal dialysis, the dose must be reduced.
With pheochromocytoma should not be prescribed without additional administration of alpha-blockers.
Bisoprolol reduces compensatory cardiovascular reactions in response to the use of general anesthetics and iodine-containing contrast agents.
You must cancel the drug 48 hours before anesthesia or choose an anesthetic with the least negative inotropic effect.
Treatment should be discontinued gradually, for approximately 2 weeks (withdrawal syndrome is possible).
Use with caution while 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).
Composition of
1 tablet contains:
active substance:
bisoprolol fumarate 2.5 mg
excipients:
lactose monohydrate – 68.15 mg,
microcrystalline cellulose – 16 mg,
mgpc 3 mg srlcp
Dosage and administration
Dosage regimen is individual.
For oral administration, the daily dose is 2.5-10 mg, the frequency of administration is 1 time / day.
The maximum daily dose is 10 mg.
Side effects
The frequency of side effects is indicated with doses not exceeding 40 mg.
From the side of 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 cold in the limbs), hallucinations, impaired thinking, concentration, orientation in time and space, balance, emotional lability, tinnitus, conjunctivitis, visual disturbances, decreased secretion of lacrimal fluid, convulsions.
From the cardiovascular system and blood (hematopoiesis, hemostasis): bradycardia (0.5%), arrhythmia, palpitations, AV block, hypotension, heart failure, impaired microcirculation in the myocardium and limbs, intermittent claudication, vasculitis, agranulocytosis, thrombocytopenia thrombocytopenic purpura.
From the digestive tract: diarrhea (3.5%), nausea (2.2%), vomiting (1.5%), dry mouth (1.3%), dyspeptic symptoms, constipation, ischemic colitis, mesenteric thrombosis arteries.
From the respiratory system: cough (2.5%), shortness of breath (1, 5%), bronchial 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.
From the skin: 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, a change in the concentration of potassium in the blood.
Other: pain (headache – 10.9%, arthralgia – 2.7%, myalgia, pain in the abdomen, chest – 1.5%, eyes, ears), weight gain.
Drug Interactions
With the simultaneous use of antacids and antidiarrheal drugs, it is possible to reduce the absorption of beta-blockers.
With the simultaneous use of antiarrhythmic drugs, a sharp decrease in blood pressure, a decrease in heart rate, the development of arrhythmia and / or heart failure are possible.
With the simultaneous use of antihypertensive drugs, it is possible to increase the antihypertensive effect.
Concomitant conduction disturbances with the simultaneous use of cardiac glycosides.
With the simultaneous use of sympathomimetics (including those included in cough, nose drops, and 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.
With the simultaneous use of guanfacine, severe bradycardia and conduction disturbances are possible.
With the simultaneous use of insulin, hypoglycemic agents for oral administration, the action of insulin or other hypoglycemic agents is enhanced (regular monitoring of blood glucose levels is necessary).
With the simultaneous use of clonidine, severe bradycardia, arterial hypotension, and conduction disturbances are possible.
In the 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, alpha-methyldopa possible severe bradycardia.
With the simultaneous use of rifampicin, a slight decrease in T1 / 2 of bisoprolol is possible.
With the simultaneous use of ergotamine derivatives (including agents for the treatment of migraine containing ergotamine), symptoms of peripheral circulation disturbance are aggravated.
Storage conditions
In a dry, dark place at a temperature of no higher than 25 ° C.
Deystvuyuschee substances
bisoprolol
dosage form
tablets
appointment
Dlya vzrosl h in naznacheniyu Vracha
Gedeon Richter-Rus Vengriya
