bisoprolol fumarate 2.5 mg
Pharmacodynamics. Bisoprol - selective blocker of β1-adrenergic receptors. When used in therapeutic doses has no intrinsic sympathomimetic activity and symptomatic membrane stabilizing properties. It has antianginal effects: reduces myocardial oxygen demand by reducing heart rate and cardiac output and decrease blood pressure, increases the myocardial oxygen supply by reducing the diastolic blood pressure and diastolic elongation.
It has a hypotensive effect due to the reduction in cardiac output, inhibition of renin secretion by the kidneys, as well as the impact on the baroreceptors of the aortic arch and carotid sinus. Prolonged use Bisoprola reduced primarily increased peripheral vascular resistance. Agent inhibits activated sympathoadrenal and renin-angiotensin-aldosterone system in patients with chronic heart failure. Bisoprol has very low affinity for the β2-receptors of bronchial smooth muscle and blood vessels, as well as the β2-receptors endocrine system. The drug is only in rare cases can affect bronchial smooth muscle and peripheral arteries, as well as on glucose metabolism. When a single application Bisoprola effect persists for 24 hours.
Pharmacokinetics. After ingestion Bisoprol well absorbed in the gastrointestinal tract. The bioavailability is about 90% and is independent of food intake. C max plasma levels achieved after 1-3 h after administration. Binding to plasma proteins is approximately 30%.
The effect of first passage through the liver is a minor (<10%). Biotransformed in the liver of about 50% of the dose to the formation of inactive metabolites. About 98% excreted by the kidneys, 50% - unchanged, the rest - in the form of metabolites, about 2% of the dose - faeces. T ½ is 10-12 hours.
Ischemic heart disease (angina);
chronic heart failure.
the drug must be taken in the morning is not liquid, regardless of the meal, washed down with a small amount of liquid.
Treatment of hypertension and stable angina
In hypertension and stable angina initial dose of 2.5-5 mg / day, average daily dose - 5.10 mg, the maximum daily dose - 20 mg.
Treatment of chronic heart failure
in chronic heart failure drug prescribed to patients with moderate to severe heart failure with reduced systolic function (ejection fraction ≤35% by echocardiogram data), situated in the stabilization state without exacerbation in the past 6 weeks.
The starting dose is 1.25 mg 1 time per day during the first week (of bisoprolol used drugs, with such a dosing). During the 2nd week of reception administered 2.5 mg / day. During the 3 weeks of the therapeutic dose of 3.75 mg / day (applied bisoprolol preparations, with such a dosing). From the 4th week 8th reception taking 5 mg. Thereafter, the dosage was increased to 7.5 mg (8 th to 12 th week). After 12 weeks of treatment prescribed maximum daily dose - 10 mg. Increasing the dose indicators regulated heart rate, blood pressure, the patient's general condition.
The maximum dose - 10 mg / day.
Bisoprol in patients with chronic heart failure can be combined with an ACE inhibitor, a diuretic and a cardiac glycoside preparations. After beginning treatment with 1.25 mg patient with chronic heart failure should be examined for 4 hours (monitoring of blood pressure, heart rate, conduction abnormalities detection symptoms, increasing the severity of heart failure symptoms); drug overturned if required.
Patients with hepatic and renal failure
for patients with mild and medium dose selection violation liver or kidney functions normally required.
For patients with marked decrease in renal function (creatinine clearance <20 mL / min) and in patients with severe liver function abnormalities daily dose should not exceed 10 mg drug.
Dose picked individually.
The course of treatment lasting and depends on the nature and course of the disease.
The course of treatment should end slowly with a gradual reduction in dose.
You can not stop treatment abruptly!
heart failure decompensation condition;
AV-block II and III degree;
sick sinus syndrome;
expressed sinoatrial block;
symptomatic bradycardia (heart rate <50 beats / min.);
symptomatic hypotension (systolic blood pressure <90 mm Hg..);
severe asthma and other obstructive airway diseases;
later stages peripheral circulatory disorders, Raynaud's disease;
simultaneous MAO inhibitors (except MAO-B inhibitors);
psoriasis (including family history);
During pregnancy and breastfeeding;
hypersensitivity to the drug.
in the dark place at a temperature not higher than 25 ° C.