2010/06/23

Bagopril

Composition, structure and packing.

Tablets are white, round, biconvex, with the inscription "GLI 2.5" on one side and the logo of the company - to another.

1 tab.

enalapril maleate 2.5 mg.

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

1 tab.

enalapril 5 mg.

Tablets are white, round, biconvex, with a Phillips scored on one side, a segment of a circle marking "G", "L", "I" and "10", on the other side - the corporate logo.

1 tab.

enalapril 10 mg.

Tablets are white, round, biconvex, with a Phillips scored on one side, a segment of a circle marking "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 - antihypertensive drug, its mechanism of action is associated with a decrease in formation of angiotensin I angiotensin II, a decrease of which leads to a direct decrease in the allocation of aldosterone. This decreases total peripheral vascular resistance, systolic and diastolic blood pressure, post-and preload on the myocardium.

Extends the artery to a greater extent than the veins, and the reflex increase in heart rate is noted.

Reduces degradation of bradykinin, increases prostaglandin synthesis.

The hypotensive effect is more pronounced at high levels of plasma renin blood than normal or reduced its level.

Reducing blood pressure 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, the reduction of pressure.

Enhances coronary and renal blood flow.

Prolonged use of reduced left ventricular hypertrophy of the myocardium and myocytes of the walls of arteries resistant type, prevents the progression of heart failure and slowing the growth of dilatation of the left ventricle.

Improves blood flow to ischemic myocardium.

Reduces platelet aggregation.

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

Time of onset of the hypotensive effect when administered - 1 hour, reaches a maximum after 4-6 hours and up to 24 hours. Some patients to achieve optimal blood pressure level needed therapy for several weeks.

In heart failure, significant clinical effect observed with prolonged use - 6 months or more.

Pharmacokinetics

After ingestion is absorbed 60% of the drug. Eating does not affect the absorption of enalapril. Enalapril to 50% bound to plasma proteins of blood. Enalapril is rapidly metabolized in the liver with the formation of the active metabolite enalaprilata, which is more active ACE inhibitor than enalapril. Bioavailability 40%. The maximum concentration of enalapril in plasma is reached after 1 hour, enalaprilata - 3-4 hours. Enalaprilat easily passes through histohematogenous barriers, except the blood-brain, a small number of crosses the placenta and into breast milk. The half enalaprilata about 11 hours. Enalapril is derived primarily (60%) through the kidneys (20% as enalapril and 40% in the form of enalaprilata), through the intestines - 33% (6% as enalapril and 27% in the form of enalaprilata). 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 (in a combination therapy).

Dosage regimen

Bagopril appointed interior, regardless of meal times.

When 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 stable blood pressure.

If necessary, and quite well tolerated, the dose may be increased to 40 mg per day for 1-2 reception. After 2-3 weeks go on supporting dose equal to 10 - 40 mg per day, divided into 1 -2 reception.

In the 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 application Bagoprila. If not, then 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 a day.

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

The maximum daily dose is 20 mg.

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

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

Selection of the dose should be conducted within 2-4 weeks or when necessary and possible in a shorter time.

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

Older people often more pronounced hypotensive effect, and lengthening the duration 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 enalapril cumulation occurs at lower filtration 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 30-10 ml / min - 2,5 -, 5 mg / day, with the spacecraft at least 10 ml / min - 1,25-2.5 mg / day only in the days of dialysis.

Duration of treatment depends on the effectiveness of therapy. If you are too marked reduction in blood pressure Bagoprila dose gradually. The drug is used as a monotherapy and in combination with other antihypertensive therapy.

Side effect

Since the cardiovascular system: the excessive lowering of blood pressure, Orthostatic hypotension, rarely - retrosternal pain, angina, myocardial infarction (usually associated with a marked decrease in blood pressure), arrhythmia (atrial brady-or tachycardia, atrial fibrillation), heart rate, thromboembolism of the branches pulmonary artery, pain in the heart, syncope.

On the part of the nervous system: dizziness, headache, anxiety, confusion, fatigue, sleepiness (2-3%), very rarely in the application of high doses indicated nervousness, depression, paresthesia.

From the senses: a violation of the vestibular apparatus, hearing and vision, tinnitus.

On the part of the digestive tract: dry mouth, anorexia, diarrhea disorders (nausea, diarrhea or constipation, vomiting, abdominal pain), intestinal obstruction, pancreatitis, abnormal liver function and bile flow, hepatitis, jaundice.

On the part of the respiratory system: non-productive dry cough, interstitial pneumonitis, bronchospasm, dyspnea, rhinorrhea, sore throat.

Allergic reactions: skin rash, angioedema face, extremities, lips, tongue, glottis and / or throat, hoarseness, 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, increased activity of "liver" transaminases, hyperbilirubinemia, hyperkalemia, hyponatremia.

There have, in some cases, the reduction of hematocrit and hemoglobin, increased erythrocyte sedimentation rate, thrombocytopenia, neutropenia, agranulocytosis (in patients with autoimmune disease), eosinophilia.

On the part of the urinary system: renal dysfunction, proteinuria.

Other side effects: alopecia, decreased libido, flushing.

Contraindications
Hypersensitivity to enalapril and other angiotensin converting enzyme (ACE)
a history of angioedema related to treatment with ACE inhibitors, porphyria, pregnancy, lactation, at the age of 18 years.

Precautions should be used enalapril in primary aldosteronizme, bilateral renal artery stenosis, stenosis of the artery of a sole kidney, hyperkalemia, a condition after kidney transplantation, aortic stenosis, mitral stenosis (with hemodynamic disorders), idiopathic hypertrophic subaortalnom stenosis, systemic connective tissue disease, coronary heart disease , cerebrovascular diseases, diabetes, renal disease (proteinuria over 1 g / day), hepatic failure, patients adhering to a diet with restriction of salt, or are on hemodialysis, while the reception with immunosuppressants and saluretikami in the elderly (65 years) .

Cautions

Be careful when you use of the drug to patients with low blood volume (due to diuretic therapy, while limiting salt intake, conducting dialysis, diarrhea or vomiting) increased risk of sudden and significant decrease in blood pressure after the application of even the initial dose of ACE inhibitor.

Transitory hypotension is not a contraindication for the continuation of drug treatment after stabilization of blood pressure, reduce the dose or cancel the drug. With the development of excessive loss of blood pressure patient is transferred to a horizontal position with a low headboard, you need to enter plazmozameschayuschie saline and drugs.

Application vysokoprotochnyh dialysis membranes increases the risk of an anaphylactic reaction. Correction of dosage regimen in the days free from dialysis, should be carried out depending on the level of blood pressure. Before and after treatment with ACE inhibitors is necessary to monitor blood pressure, blood parameters (hemoglobin, potassium, creatinine, urea, the activity of "liver" enzymes), protein in the urine. One should carefully monitor patients with severe heart failure, coronary heart disease and cerebrovascular disease, in which a sharp decline in blood pressure can lead to myocardial infarction, stroke or renal dysfunction.

The sudden cancellation of treatment does not lead to a syndrome of "abolition" (a rapid rise in blood pressure).

In patients with an indication of a history of angioedema, have an increased risk of developing it while taking ACE inhibitors. For newborns and infants, who were in utero effects of ACE inhibitors, should be closely monitored for early detection of significant decrease in blood pressure, oliguria, hyperkalaemia and neurological disorders, possible due to the reduction of renal and cerebral blood flow with a decrease in blood pressure caused by ACE inhibitors.

If oliguria need to maintain blood pressure and renal perfusion through the introduction of appropriate fluids and vasoconstrictor agent.

In patients with decreased renal function should be reduced a single dose or increase the intervals between doses of the drug. Before examining the function of parathyroid glands enalapril should be abolished.

During the period of treatment is not recommended to drink alcoholic beverages, since alcohol increases the hypotensive effect of the drug.

During the period of treatment should refrain from driving motor vehicles and classes of potentially hazardous activities that require high concentration and quickness of psychomotor reactions as dizziness, especially after the initial dose of ACE inhibitor in patients taking diuretic drugs.

Caution must be exercised when performing physical exercise in hot weather (risk of dehydration and excessive loss of blood pressure due to reduced blood volume).

Before surgery (including dental) must notify the surgeon / anesthesiologist on the use of ACE inhibitors.

Overdose

Symptoms: marked reduction in blood pressure until the development of collapse, myocardial infarction, acute ischemic or thromboembolic complications, convulsions, catatonia.

Treatment: bolnogo transferred to a horizontal position with a low headboard. In mild cases shown a gastric lavage and ingestion of saline. In more severe cases, the recommended measures aimed at stabilizing blood pressure: intravenous injection of saline, plasma substitutes and, if necessary - angiotensin II. Perhaps the use of hemodialysis.

Drug Interactions

In case of simultaneous appointment of enalapril with nonsteroidal anti-inflammatory drugs may reduce the hypotensive effect. Use of the drug with potassium-sparing diuretics (spironolactone, triamterene, amiloride) may lead to hyperkalaemia, with lithium salts - to slow the elimination of lithium in blood plasma (indicated by monitoring the concentration of lithium in blood plasma).

Simultaneous reception of enalapril with antipyretic and analgesic drugs may reduce the effectiveness of enalapril. Enalapril reduces the effect of drugs containing theophylline.

Hypotensive effect of enalapril reinforce diuretics, beta-blockers, methyldopa, nitrates, blockers of slow calcium channels, hydralazine, prazozina.

Immunosuppressants, allopurinol, cytostatics reinforce gematotoksichnost.

Drugs that cause bone marrow suppression, increase the risk of neutropenia and / or agranulocytosis until death.

Terms and Conditions of storage

In a dry, protected from light and the reach of children, at up to 25 ° C.

Shelf life 2 years.