BISOPROLOL PILLS 10MG
BISOPROLOL PILLS 10MG - 50 TABS
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1 pill 2.5 mg
Active ingredient: bisoprolol fumarat 2.5 mg.
1 pill 5.0 mg
Active substances: bisoprolol fumarate 5.0 mg.
1 pill 10.0 mg
Active substances: bisoprolol fumarate 5.0 mg.
Mechanism of action
Bisoprolol is a selective β1-adrenoblocker, without its own sympathomimetic activity, does not have a membrane stabilizing effect. As with other β1-blockers, the mechanism of action in hypertension is unclear. At the same time, it is known that bisoprolol reduces renin activity in blood plasma, decreases myocardial oxygen demand, and reduces heart rate (HR). It has antihypertensive, antiarrhythmic and antianginal effects.
By blocking the β1-adrenoreceptors of the heart in low doses, it reduces catecholamine-stimulated formation of cyclic adenosine monophosphate (cAMP) from adenosine triphosphate (ATP), reduces the intracellular current of Calcium ions, inhibits all heart functions, reduces atrioventricular (AV) conductivity and excitability. When the therapeutic dose is exceeded, it has a β2-adrenergic blocking effect.General peripheral vascular resistance at the beginning of the drug, increases in the first 24 hours (as a result of the reciprocal increase in the activity of α-adrenoreceptors and the removal of stimulation of β2-adrenoreceptors), after 1-3 days it returns to its original value, and with prolonged use it decreases.
The antihypertensive effect is associated with a decrease in the minute volume of blood, sympathetic stimulation of peripheral vessels, a decrease in the activity of the sympathoadrenal system (SAS) (important for patients with initial renin hypersecretion), the restoration of sensitivity in response to a decrease in arterial pressure (BP) and the effect on the central nervous system.
In case of arterial hypertension, the effect develops in 2-5 days, a stable effect is noted in 1-2 months.
The antianginal effect is due to a decrease in myocardial oxygen demand as a result of a decrease in contractility and other myocardial functions, a prolongation of diastole, and an improvement in myocardial perfusion. By increasing the end-diastolic pressure in the left ventricle and increasing the stretching of the muscle fibers of the ventricles, oxygen demand may increase, especially in patients with chronic heart failure (CHF).
When used in moderate therapeutic doses, in contrast to non-selective β-blockers, it has a less pronounced effect on organs containing β2-adrenoreceptors (pancreas, skeletal muscles,smooth muscles of peripheral arteries, bronchi and uterus) and carbohydrate metabolism; does not cause the delay of sodium ions in the body; the severity of atherogenic action does not differ from that of propranolol.
Indications and usage
- arterial hypertension;
- Ischemic heart disease: prevention of angina attacks;
- chronic heart failure.
- hypersensitivity to bisoprolol, other components of the drug and to other β-blockers,
- acute heart failure or CHF in the decompensation stage, requiring inotropic therapy,
- shock (including cardiogenic),
- pulmonary edema,
- atrioventricular block (AV) block II-III degree, without pacemaker,
- sinoatrial blockade,
- sick sinus syndrome,
- bradycardia (heart rate less than 60 beats / min.),
- severe hypotension (systolic blood pressure (BP) 100 mm Hg),
- severe forms of asthma and chronic obstructive pulmonary disease (COPD) in history,
- pronounced disorders of the peripheral circulation, Raynaud's syndrome,
- metabolic acidosis,
- pheochromocytoma (without the simultaneous use of α-blockers),
- simultaneous administration of monoamine oxidase inhibitors (MAO) (with the exception of MAO type B inhibitors),
- age up to 18 years (efficiency and safety have not been established),
- lactose intolerance, lactase deficiency or glucose-galactose malabsorption syndrome.
Dosage and administration
The drug Bisoprolol is taken orally, in the morning on an empty stomach, once, without chewing, with a small amount of liquid. pills should not be chewed or powdered.
Treatment of hypertension and angina pectoris
In all cases, the dosage regimen and dosage are selected by the doctor for each patient individually, in particular, taking into account the heart rate and therapeutic response.
In hypertension and ischemic heart disease, the initial dose is usually 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 / day. It is possible to divide the daily dose into 2 doses.
Treatment of stable chronic heart failure
The standard treatment regimen for CHF includes the use of angiotensin converting enzyme (ACE) inhibitors or angiotensin II receptor antagonists (in case of intolerance to ACE inhibitors), β-blockers, diuretics, and, optionally, cardiac glycosides. The initiation of treatment of CHF with the drug Bisoprolol requires the obligatory carrying out of a special phase of titration and regular medical monitoring.
A prerequisite for treatment with bisoprolol is stable chronic heart failure with no signs of exacerbation.
Treatment of CHF with the drug Bisoprolol begins in accordance with the following titration scheme.This may require individual adaptation depending on how well the patient tolerates the prescribed dose, that is, the dose can be increased only if the previous dose was well tolerated.
The recommended starting dose is 1.25 mg (1/2 pills of 2.5 mg) once a day. Depending on the individual tolerance, the dose should be gradually increased to 2.5 mg, 3.75 mg (1½ pills of 2.5 mg), 7.5 mg (3 pills of 2.5 mg) and 10 mg once a day. Each subsequent increase in dose should be carried out no less than two weeks.
If an increase in the dose is poorly tolerated by the patient, a dose reduction is possible. The maximum recommended dose for CHF is 10 mg of the drug Bisoprolol 1 time per day.
During titration, regular monitoring of blood pressure, heart rate and degree of CHF symptoms is recommended. The aggravation of the symptoms of CHF is possible from the first day of using the drug.
If the patient does not tolerate the maximum recommended dose of the drug, a gradual dose reduction is possible.
During the titration phase or after it, a temporary worsening in the course of CHF, hypotension or bradycardia may occur. In this case, it is recommended, first of all, to adjust the doses of drugs associated therapy. It may also require a temporary reduction in the dose of the drug Bisoprolol or its cancellation.
After the patient's condition has stabilized, a dose titration should be repeated, or the treatment should be continued.
Special patient groups
Impaired renal or hepatic function:
- In case of a mild or moderately impaired liver or kidney function, it is usually not necessary to adjust the dose.
- With pronounced impaired renal function (CC less than 20 ml / min) and in patients with severe liver diseases, the maximum daily dose is 10 mg. Increasing the dose in such patients should be carried out with extreme caution.
To date, insufficient data on the use of the drug Bisoprolol in patients with CHF associated with type 1 diabetes, severe impaired renal function and / or liver, restrictive cardiomyopathy, congenital heart disease or valvular heart disease with severe hemodynamic disorders. Also, until now there has not been obtained sufficient data on patients with chronic heart failure with myocardial infarction in the last 3 months.