2010/12/13

Bagopril

Release form, composition and packing Bagopril

Pill white, round, biconvex, with the inscription "GLI 2.5" on one side and company logo - on the other.

1 tab.

Enalapril Maleate 2.5 mg.

Pill white, round, biconvex, with the inscription "GLI" and the numeral "5" under it on one side and company logo - on the other.

1 tab.

Enalapril Maleate 5 mg.

Pill white, round, biconvex, scored with a cross on one side, a segment of a circle notation "G", "L", "I" and "10", on the other side - the corporate logo.

1 tab.

enalapril 10 mg.

Pill white, round, biconvex, scored with a cross on one side, a segment of a circle notation "G", "L", "I" and "20", on the other side - the corporate logo.

1 tab.

enalapril 20 mg.

Excipients: sodium starch glycolate, povidone, microcrystalline cellulose, magnesium stearate, lactose monohydrate.

Pharmacological action

Bagopril - an antihypertensive drug, its mechanism of action is associated with a decrease in formation of angiotensin I angiotensin II, decrease of which leads to a direct reduction of aldosterone release. At the same time decreases the total peripheral vascular resistance, systolic and diastolic blood pressure, fasting and preload on the myocardium.

Expands the artery to a greater extent than the vein, with a reflex increase in heart rate is not marked.

Reduces the degradation of bradykinin, increases prostaglandin synthesis.

Hypotensive effect was more pronounced at high levels of plasma renin blood than normal or reduced its level.

Blood pressure reduction in the therapeutic range has no effect on cerebral blood flow, blood flow in the vessels of the brain is maintained at a sufficient level on the background of reduced pressure.

Strengthens the coronary and renal blood flow.

With prolonged use decreases left ventricular hypertrophy and myocardial muscle cells of the arteries resistant type, prevents the progression of heart failure and slowing the development of dilatation of the left ventricle.

Improves blood flow to ischemic myocardium.

Reduces platelet aggregation.

Has some diuretic effect. Enalapril is a "prodrug": as a result of its hydrolysis formed enalaprilat, which inhibits ACE.

Time of onset of hypotensive effect when taken orally - 1 hour, reaches a maximum after 4-6 h and persists up to 24 hours. In some patients, achieving optimal blood pressure level is required therapy for several weeks.

Heart failure significant clinical effect observed with prolonged use - 6 months or more.

Pharmacokinetics

After oral administration, absorbed 60% of the drug. Food intake did not affect the absorption of enalapril. Enalapril and 50% bound to plasma proteins. Enalapril is rapidly metabolized in the liver with the formation of the active metabolite enalaprilat, which is more active ACE inhibitor than enalapril. Bioavailability 40%. The maximum concentration of enalapril in plasma is reached after 1 hour, enalaprilat - 3-4 hours. Enalaprilat easily passes through gistogematicheskie barriers, except the blood-brain, small amounts cross the placenta and breast milk. Half-life of enalaprilat about 11 hours. Enalapril is derived primarily (60%) through the kidneys (20% as enalapril and 40% as enalaprilat), through the intestines - 33% (6% as enalapril and 27% as enalaprilat). Removed during dialysis (rate 62 ml / min) and peritoneal dialysis.

Statement
Bagopril prescribed for various forms of hypertension, including renovascular hypertension.
The drug is also effective in chronic heart failure (as part of combination therapy).

Dosing regimen

Bagopril appointed interior, regardless of meal times.

In monotherapy of hypertension the initial dose - 5 mg once a day.

In the absence of clinical effect in 1-2 weeks increase the dose of 5 mg.

After receiving the initial dose, patients should be under medical supervision for 2 hours and an additional 1 hour, until it stabilizes blood pressure.

If necessary, and reasonably good tolerability, the dose may be increased to 40 mg / day for 1-2 reception. After 2-3 weeks go to the maintenance dose equal to 10 - 40 mg per day, divided into 1 -2 reception.

With moderate hypertension average daily dose is about 10 mg.

The maximum daily dose - 40 mg.

In fact, if you want to assign Bagopril patients who take diuretics, treatment with diuretics should be discontinued 2-3 days prior to the start of Bagoprila. If it is not possible, the initial dose Bagoprila should be 2.5 mg / day.

Patients with hyponatremia (sodium ion concentration in the serum of less than 130mmol / L) or with increasing concentrations of serum creatinine over 0.14 mmol / L designate Bagopril in an initial dose of 2.5 mg 1 time per day.

When renovascular hypertension the initial dose - 2,5 - 5 mg / day.

The maximum daily dose is 20 mg.

In chronic heart failure the initial dose Bagoprila - 2.5 mg dose, then increase the dose of 2,5 - 5 mg every 3-4 days according to clinical response up to maximum tolerable doses, depending on the values of blood pressure, but not exceeding 40 mg single dose or in 2 divided doses.

In patients with low systolic blood pressure (less than 110 mm Hg), therapy should begin with a dose of 1.25 mg / day.

Titration should be carried out for 2-4 weeks or when necessary and possible in the shortest possible time.

The average maintenance dose - 5 - 20 mg / day for 1 -2 reception.

Older people more often, a more pronounced hypotensive effect and prolonged time of action of enalapril, which is associated with a decrease in clearance rate of the drug, so the recommended initial dose for elderly patients - 1,25 mg / day.

In chronic renal failure, accumulation of enalapril comes with a decrease in filtering of less than 10 ml / min.

When creatinine clearance (CC) 80-30 ml / min dose of enalapril should be 5-10 mg / day, while reducing spacecraft to 10.30 ml / min - 2,5 - 5 mg / day, with CC <10>