Biprol - instructions for use, analogs, reviews and release forms (tablets 2.5 mg, 5 mg and 10 mg plus in combination with a diuretic) drug for the treatment of angina and lowering pressure in adults, children and pregnancy. Composition

In this article, you can read the instructions for using the drug Biprol. Comments of visitors of the site - consumers of this medication, as well as opinions of doctors of specialists on the use of Biprol in their practice are presented. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of Biprol in the presence of existing structural analogues. Use for the treatment of angina pectoris, hypertension and depression in adults, children, as well as in pregnancy and lactation.Composition of the preparation.

Biprol - selective beta-1-blocker without internal sympathomimetic activity, does not possess membrane-stabilizing properties.

Reduces the activity of plasma renin, reduces the need for myocardium in oxygen, reduces heart rate at rest and with exercise. Has antihypertensive, antiarrhythmic and antianginal action. When used in low doses, it blocks beta 1-adrenoreceptors of the heart, reduces catecholamine-stimulated cAMP formation from ATP, reduces the intracellular current of calcium ions, has a negative chrono-, dromo-, batmo- and inotropic effect, inhibits conduction and excitability, and reduces myocardial contractility.

When used in high doses has beta2-adrenoblocking effect.

OPSS at the beginning of the drug (in the first 24 hours) increases (as a result of the reciprocal increase in the activity of alpha-adrenoreceptors and removal of stimulation of beta2-adrenoreceptors), then in 1-3 days it returns to the initial, and with prolonged use of the drug - decreases.

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-aldosterone system (is of great importance for patients with initial hypersecretion of renin), restoration of sensitivity in response to a decrease in blood pressure and influence on the CNS. With arterial hypertension, the initial effect occurs after 2-5 days, stable after 1-2 months.

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, diastole lengthening, and improvement in myocardial perfusion. By increasing the end diastolic pressure in the left ventricle and increasing the stretching of the muscle fibers, the ventricles can increase the demand for myocardium in oxygen, especially in patients with chronic heart failure.

The antiarrhythmic effect is caused by 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 slowing of AV conduction (mainly in antegrade and, to a lesser extent, in retrograde directions via the AV node) and by additional paths.

When used at average therapeutic doses, in contrast to non-selective beta-blockers, it exerts a less pronounced effect on organs containing beta2-adrenoreceptors (pancreas, skeletal muscles, smooth muscle of peripheral arteries, bronchi and uterus) and on carbohydrate metabolism, does not cause delay sodium ions in the body; the severity of atherogenic action does not differ from that of propranolol. When used in high doses (200 mg or more) has a blocking effect on both subtypes of beta adrenoreceptors, mainly in the bronchi and smooth muscles of the vessels.

Hydrochlorothiazide (as part of Biprol Plus) is a thiazide diuretic (diuretic). Reduces the reabsorption of sodium ions in the cortical segment of the Henley loop, without affecting its area passing through the medulla of the kidney. It blocks carbonic anhydrase in the proximal part of the convoluted renal tubules, enhances the excretion of potassium ions, hydrocarbonates and phosphates by the kidneys. Virtually does not affect the acid-base state. Increases the excretion of magnesium ions by the kidneys; It detains calcium ions in the body and inhibits the excretion of urates.The diuretic effect develops after 1-2 hours, reaches a maximum after 4 hours, the duration of the antihypertensive effect persists for a day. The diuretic effect decreases with a decrease in the glomerular filtration rate and stops at a value of less than 30 ml / min.

Composition

Bisoprolol fumarate + excipients.

Bisoprolol fumarate + hydrochlorothiazide + excipients.

Pharmacokinetics

Bisoprolol

Absorption does not depend on food intake. After ingestion, absorption from the gastrointestinal tract (GIT) is 80-90%. Moderately soluble in lipids, poorly penetrates the blood-brain and placental barrier, excreted in breast milk (about 1%). Metabolised in the liver. It is produced in two equivalent ways: approximately 50% of the dose of Bisoprolol is excreted by the kidneys in an unchanged form and only 1-2% by the intestine.

Hydrochlorothiazide

When ingested quickly absorbed, but incomplete, 80% absorption, communication with plasma proteins 64%. Bioavailability of hydrochlorothiazide from 60 to 80%. It penetrates the placental barrier and is excreted into breast milk. It is not metabolized. It is excreted by the kidneys mainly (more than 95%) unchanged through glomerular filtration and active tubular secretion.

Indications

• arterial hypertension;
• IHD: prevention of angina attacks.

Forms of release

Tablets coated with 2.5 mg, 5 mg and 10 mg.

Instructions for use and dosage

Biprol

Is taken orally, in the morning, on an empty stomach, the tablets are not chewed.

The drug is prescribed in a dose of 5 mg 1 time per day. If necessary, increase the dose to 10 mg once a day. The maximum daily dose is 20 mg.

In patients with impaired renal function with QC less than 20 ml / min or with severe impairment of liver function, the maximum daily dose is 10 mg.

Biprol Plus

Inside, in the morning (during a meal), not liquid with a small amount of liquid 1 time per day.

The dose of the drug is selected individually.

The initial dose of Biprol plus is 1 tablet 5 / 12.5 (containing 5 mg of bisoprolol and 12.5 mg of hydrochlorothiazide) once a day. If the therapeutic effect is inadequate, the dose can be increased to a maximum daily dose of 10/25 - 1 tablet of Biprol Plus (containing 10 mg of bisoprolol and 25 mg of hydrochlorothiazide).

In the elderly, dose adjustment is not required. It is recommended to start with the lowest possible dose.

Patients with renal insufficiency (QC greater than 30 ml / minute), as well as mild to moderate hepatic insufficiency, dose adjustment is not required.

Side effect

• increased fatigue;
• dizziness;
• headache, which especially often occur at the beginning of treatment, are mild and pass during the first 1-2 weeks of treatment;
• sleep disturbance;
• depression;
• convulsions;
• hallucinations;
• bradycardia;
• violation of AV conductivity;
• exacerbation of chronic heart failure;
• ventricular extrasystole;
• sensation of cold and numbness of limbs;
• orthostatic hypotension;
• pain in the chest;
• bronchospasm in patients with bronchial asthma and bronchospasm (in the anamnesis);
• nausea, vomiting;
• diarrhea, constipation;
• dryness of the oral mucosa;
• loss of appetite;
• discomfort in the gastrointestinal tract;
• muscle weakness;
• cramps in the calf muscles;
• arthralgia;
• hearing and vision impairment;
• decreased lacrimal gland production (it is necessary to consider patients who use contact lenses);
• conjunctivitis;
• violation of potency;
• leukopenia, thrombocytopenia, agranulocytosis;
• itching;
• rash;
• redness of facial skin;
• allergic rhinitis;
• increased sweating;
• possibly exacerbation of psoriasis, alopecia, discoid and red lupus;
• increased activity of liver enzymes (alanine aminotransferase, aspartate aminotransferase);
• hepatitis;
• jaundice.

Contraindications

• severe forms of bronchial asthma;
• chronic obstructive pulmonary disease;
• cardiogenic shock;
• syndrome of weakness of the sinus node (including sinoatrial blockade);
• atrioventricular blockade of 2 and 3 degrees without an artificial pacemaker;
• pronounced bradycardia (heart rate less than 60 beats per minute);
• pheochromocytoma (without simultaneous use of alpha-1 adrenoblockers);
• late stages of peripheral circulatory disorders (including Raynaud's syndrome);
• severe arterial hypotension (systolic blood pressure less than 90 mm Hg);
• refractory hypokalemia, hyponatremia, hypercalcemia;
• metabolic acidosis;
• dehydration;
• acute renal insufficiency;
• chronic renal failure (creatinine clearance (CK) less than 30 ml / min);
• simultaneous application with floktaphenin, sultopride;
• simultaneous administration of monoamine oxidase inhibitors (MAO) (with the exception of MAO type B inhibitors);
• age under 18 years (effectiveness and safety not established);
• severe hepatic insufficiency (including hepatic precoma and coma);
• gout;
• hypersensitivity to bisoprolol, hydrochlorothiazide and other derivatives of sulfonamide, as well as to other components of the drug.

Application in pregnancy and lactation

The use of Biprol during pregnancy and lactation is possible if the benefit to the mother exceeds the risk of side effects in the fetus and the baby.

The use of Biprol Plus during pregnancy and lactation is contraindicated.

Use in children

Contraindicated in children and adolescents under the age of 18 years (efficacy and safety not established).

Application in elderly patients

With caution appoint the drug to elderly patients.

special instructions

Control of the condition of patients taking Biprol should include a measurement of heart rate and blood pressure (at the beginning of treatment - every day, then once every 3-4 months), ECG, blood glucose in diabetic patients (once every 4-5 months). In elderly patients it is recommended to monitor the kidney function (1 time in 4-5 months).

Before the start of treatment, it is recommended to perform a study of the function of external respiration in patients with respiratory diseases in the anamnesis.

It is necessary to teach the patient how to calculate heart rate and instruct about the need for medical consultation at heart rate less than 50 beats per minute.

Approximately in 20% of patients with angina pectoris beta-blockers are ineffective. The main causes are severe coronary atherosclerosis with a low threshold of ischemia (heart rate less than 100 beats per minute) and an increased end-diastolic volume of the left ventricle, which breaks the subendocardial blood flow.

In smoking patients, the effectiveness of beta-blockers is lower.

Patients using contact lenses should take into account that a reduction in tear fluid production is possible against the background of treatment.

When used in patients with pheochromocytoma, there is a risk of developing paradoxical arterial hypertension (unless an effective blockade of alpha-adrenergic receptors is previously achieved).

With thyrotoxicosis, Biprol can mask certain clinical signs of thyrotoxicosis (for example, tachycardia). Sharp abolition in patients with thyrotoxicosis is contraindicated, since in this case, it is possible to increase symptoms.

With diabetes, the drug can mask tachycardia caused by hypoglycemia.Unlike nonselective beta-blockers, it does not actually increase insulin-induced hypoglycemia and does not delay the restoration of blood glucose to normal levels.

With the simultaneous administration of clonidine, his admission can be stopped only a few days after the cancellation of Biprol.

It is possible to increase the severity of the hypersensitivity reaction and the lack of effect on the usual doses of epinephrine in patients with a history of allergic anamnesis.

If it is necessary to conduct routine surgical treatment, the drug can be withdrawn 48 hours before the start of the general anesthesia. If the patient took the drug before the operation, he should choose a medicine for general anesthesia with a minimum negative inotropic effect.

Reciprocal activation of the vagus nerve can be eliminated by intravenous administration of atropine (1-2 mg).

Drugs that reduce the reserves of catecholamines (including reserpine) can enhance the action of beta-blockers, so patients taking such combinations of drugs should be under constant medical supervision to detect a pronounced lowering of blood pressure or bradycardia.

Patients with bronchospastic states or diseases can be prescribed cardioselective adrenoblockers in case of intolerance and / or inefficiency of other antihypertensive drugs. Overdosing is dangerous by the development of bronchospasm.

If older bradycardia (less than 50 beats per minute), a marked decrease in blood pressure (systolic blood pressure below 100 mm Hg), AV blockade should be reduced or treatment should be stopped in patients with advanced age.

It is recommended to stop therapy with the development of depression.

Do not abruptly interrupt treatment because of the risk of developing severe arrhythmias and myocardial infarction. Cancellation is carried out gradually, reducing the dose for 2 weeks or more (by 25% in 3-4 days).

The drug should be discontinued before the study of blood and urine levels of catecholamines, normetanephrine and vanillin-mandelic acid; titers of antinuclear antibodies.

Impact on the ability to drive vehicles and manage mechanisms

During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Drug Interactions

Biprol treatment with allergens used for immunotherapy, or allergen extracts for skin tests increases the risk of severe systemic allergic reactions or anaphylaxis.

With the simultaneous use with bisoprolol iodine-containing radiocontrast drugs for intravenous administration, the risk of anaphylactic reactions increases.

With simultaneous appointment with bisoprolol phenytoin for intravenous administration, medicines for inhalation of general anesthesia (derivatives of hydrocarbons) increase the severity of cardiodepressive action and the likelihood of lowering blood pressure.

With simultaneous use of bisoprolol changes the effectiveness of insulin and oral hypoglycemic drugs, masks the symptoms of developing hypoglycemia (tachycardia, increased blood pressure).

With simultaneous use of bisoprolol reduces the clearance of Lidocaine and xanthines (except for diphylline) and increases their concentration in the plasma, especially in patients with initially elevated clearance of theophylline under the influence of smoking.

The hypotensive effect of bisoprolol reduces non-steroidal anti-inflammatory drugs (NSAIDs), glucocorticosteroids (GCS), and estrogens (Na ion retention).

With simultaneous use of cardiac glycosides, methyldopa, reserpine and guanfacine, calcium channel blockers (verapamil, diltiazem), amiodorone and other antiarrhythmic drugs increase the risk of developing or aggravating bradycardia, AV blockade, cardiac arrest and heart failure.

With simultaneous application with bisoprolol, Nifedipine can lead to a significant reduction in blood pressure.

With simultaneous use with bisoprolol, diuretics, clonidine, sympatholytics, hydralazine and other antihypertensive drugs can lead to excessive blood pressure lowering.

Bisoprolol extends the action of nondepolarizing muscle relaxants and the anticoagulant effect of coumarins.

Tri- and tetracyclic antidepressants, antipsychotic drugs (antipsychotics), ethanol (alcohol), sedative and hypnotic drugs increase the inhibitory effect of bisoprolol on the central nervous system.

It is not recommended simultaneous use of bisoprolol with MAO inhibitors due to a significant increase in antihypertensive action(the interval between taking MAO inhibitors and bisoprolol should be at least 14 days).

With simultaneous application with bisoprolol, unhydrated ergot alkaloids, ergotamine increase the risk of peripheral circulatory disorders.

With simultaneous application of Sulfasalazine increases the concentration of bisoprolol in plasma.

Analogues of the drug Biprol

Structural analogs for the active substance:

• Aritel;
• Aritel Cor;
• Bidop;
• Bidop Kor;
• Biol;
• Bisogamma;
• Bisocardium;
• Bisomore;
• Bisoprolol;
• Bisoprolol hemifumarate;
• Bisoprolol fumarate;
• Concor;
• Concor Cor;
• Corbis;
• Cordinorm;
• Coronale;
• Niperten;
• Thyrez.

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