2010/12/17

Berlipril

Release form, composition and packing  Berlipril

Berlipril ® 5 Tablets are round, flat, almost white, with beveled edge and a risk to the division on one side. 1 tab. Enalapril Maleate 5 mg. Other ingredients: gelatin, lactose monohydrate, magnesium stearate, magnesium carbonate, basic, colloidal silicon dioxide, sodium carboxymethyl starch.

Berlipril ® 10

The tablets are round, Valium, light brown, with a notch for the division on the one hand, there may be blotches of white. 1 tab. enalapril 10 mg. Excipients: lactose monohydrate, magnesium carbonate light, gelatin, sodium carboxymethyl starch, magnesium stearate, iron oxide brown (E172).

Berlipril ® 20

The tablets are round, Valium, pale pink, with a notch for the division on one side, there may be blotches of white. 1 tab. enalapril 20 mg. Excipients: lactose monohydrate, magnesium carbonate light, gelatin, sodium carboxymethyl starch, magnesium stearate, iron oxide red (E172). Clinico-pharmacological group: ACE inhibitor.

Pharmacological action

ACE inhibitor, an antihypertensive drug. Enalapril is a prodrug: as a result of its hydrolysis formed enalaprilat, which inhibits ACE.

The mechanism of action of the drug is associated with a decrease in formation of angiotensin II from angiotensin I, which reduces the release of aldosterone. In this case falls PR, systolic and diastolic blood pressure, fasting and preload on the myocardium.

The drug reduces the decay of bradykinin, increased prostaglandin synthesis. Enalaprilat widens arteries more than veins, and the reflex heart rate increase is not observed. Strengthens the coronary and renal blood flow. Antihypertensive effect is more pronounced at high levels of plasma renin blood than with normal or reduced its level.

BP 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 and on a background of reduced blood pressure. With prolonged use decreases left ventricular hypertrophy and myocardial muscle cells of the arteries of resistive type.

Use of the drug prevents the progression of heart failure and slowing the development of dilatation of the left ventricle. Improves blood flow to ischemic myocardium, reduce platelet aggregation. The timing of antihypertensive action by ingestion - 1 hour, its maximum is observed after 4-6 h, the effect persists for 24 hours in some patients to achieve optimal blood pressure level needed treatment for several weeks. Heart failure significant clinical effect observed in long-term treatment - 6 months or more.

Pharmacokinetics

Suction

If ingestion is absorbed 60% of the drug. Food intake did not affect the absorption of enalapril.

Distribution

Plasma protein binding is 50%. Cmax plasma levels reached after 1 hour, enalaprilat - 3-4 pm enalaprilat easily passes through gistogematicheskie barriers, eliminating the BBB, a small number of crosses the placental barrier and into breast milk.

Metabolism

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%.

Breeding

T1 / 2 enalaprilat - about 11 hours is excreted primarily by the kidneys - 60% (20% - in the form of enalapril and 40% - in the form of enalaprilat), through the intestines - 33% (6% - in the form of enalapril and 27% - in as enalaprilat). Removed during dialysis (rate 62 ml / min) and peritoneal dialysis.

Statement
hypertension (including renovascular);
Chronic heart failure (as part of combination therapy);
asymptomatic left ventricular dysfunction after myocardial infarction (as part of combination therapy).

Dosing regimen

Berlipril are inside, regardless of the meal. In monotherapy of hypertension the initial dose is 5 mg 1 time per day. In the absence of clinical effect in 1-2 weeks. increase the dose of 5 mg. After first taking the drug, 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 can be increased to 40 mg / day in 2 divided doses. 2-3 weeks. go to the maintenance dose of 10-40 mg / day, divided by 1-2 reception.

With moderate hypertension average daily dose is 10 mg. The maximum daily dose is 40 mg. In the case of the appointment Berliprila patients while receiving diuretics, diuretic therapy should be discontinued 2-3 days prior to the appointment Berliprila. If this is not possible that the initial dose should be 2.5 mg / day.

Patients with hyponatremia (sodium ion concentration in the blood serum of less than 130 mg / dL), or the content of serum creatinine over 0.14 mmol / l initial dose Berliprila - 2.5 mg 1 time per day. When renovascular hypertension the initial dose - 2.5-5 mg / day. The maximum daily dose - 20 mg. In chronic heart failure the initial dose - 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 magnitude of BP, but not higher than 40 mg / day once or 2 admission. In patients with low systolic blood pressure (less than 110 mm Hg), therapy should begin with a dose of 1.25 mg. Titration should be carried out for 2-4 weeks. or in a shorter time. The average maintenance dose - 5-20 mg / day for 1-2 reception.

Elderly patients often had more pronounced hypotensive effect and lengthening the time of the drug, which is associated with a decrease in clearance rate enalaprilat, so the recommended initial dose is 1.25 mg. Asymptomatic left ventricular dysfunction drug is prescribed to 2.5 mg 2 times a day. Dose is selected taking into account the tolerance to 20 mg / day and share it on 2 receptions.

In chronic renal failure, accumulation of the drug comes with a decrease in the filtration rate of less than 10 ml / min. With CC 80-30 ml / min dose Berliprila typically 5-10 mg / day, with CC 30.10 ml / min - 2.5-5 mg / day, with CC <10 ml / min - 1.25-2.5 mg / day only during dialysis.

Duration of treatment depends on the effectiveness of therapy. With too pronounced decrease in blood pressure dose gradually. The drug used in monotherapy and in combination with other antihypertensive drugs.

Side effect
Cardio-vascular system: hypotension, orthostatic collapse, rarely - chest pain, angina, myocardial infarction (commonly associated with a marked decrease in blood pressure), arrhythmias (atrial Braden or tachycardia, atrial fibrillation), tachycardia, thromboembolism branches of the pulmonary artery pain in the heart swoon.
CNS and peripheral nervous system: dizziness, headache, fatigue, insomnia, anxiety, confusion, fatigue, drowsiness (2.3%), rarely at a reception in high doses - nervousness, depression, paresthesia.
From the sensory organs: very rarely - vestibular disorders, hearing and vision, tinnitus.
From the digestive system: dry mouth, anorexia, nausea, vomiting, constipation, diarrhea, rarely - abdominal pain, ileus, pancreatitis, abnormal liver function and bile ducts, hepatitis, jaundice.
With the respiratory system: non-productive dry cough, interstitial pneumonitis, bronchospasm, dyspnea, rhinorrhea, sore throat. Allergic reactions: skin rash, angioedema face, lips, tongue, glottis and / or throat, limbs, dysphonia, polymorphic erythema, exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis, pemphigus, pruritus, urticaria, photosensitivity, serositis, vasculitis, myositis, arthralgia, arthritis, stomatitis, glossitis.
From the laboratory parameters: hypercreatininemia, elevated levels of urea, elevated liver transaminases, hyperbilirubinemia, hyperkalemia, hyponatremia, in some cases - reduced hematocrit and hemoglobin, increased sedimentation rate, thrombocytopenia, neutropenia, agranulocytosis (in patients with autoimmune diseases), eosinophilia.
With the urinary system: Renal proteinuria.

Other: alopecia, decreased libido, hot flashes.

The drug is generally well tolerated and in most cases does not cause adverse reactions requiring withdrawal of therapy.

Contraindications
angioedema associated with ACE inhibitors, a history;
porphyria;
pregnancy;
Lactation (breastfeeding);
childhood and adolescence to 18 years;
increased sensitivity to enalapril and other ACE inhibitors.

Precautions should be appointed Berlipril in primary hyperaldosteronism, bilateral renal artery stenosis, stenosis of the artery a single kidney, hyperkalemia, condition after kidney transplantation, aortic stenosis, mitral stenosis with impaired hemodynamics, idiopathic hypertrophic subaortalnom stenosis, connective tissue diseases, ischemic heart disease, cerebrovascular disease, diabetes diabetes, renal disease (proteinuria greater than 1 g / d), liver failure, while the reception with immunosuppressants and saluretics elderly patients (over 65).

Pregnancy and lactation

The drug is contraindicated during pregnancy and lactation (breastfeeding).

Use in hepatic dysfunction

Precautions should be appointed Berlipril in hepatic failure.