Captopril-UBF - instructions for use, dose, side effects, contraindications

Reduces the formation of angiotensin II from angiotensin I. Reduction in angiotensin II leads to a direct reduction in the release of aldosterone. This reduces the overall peripheral vascular resistance, blood pressure, post- and preload on the heart. Expands arteries more than veins.It causes a decrease in the degradation of bradykinin (one of the effects of ACE) and an increase in the synthesis of prostaglandin. The hypotensive effect does not depend on the plasma renin activity, the decrease in arterial pressure is noted at a normal and even lowered level of the hormone, which is due to the effect on tissue renin-angiotensin systems. Strengthens coronary and renal blood flow. With prolonged use reduces the severity of myocardial hypertrophy and the walls of arteries of resistive type. Improves the blood supply of the ischemic myocardium. Reduces the aggregation of platelets. Helps reduce the content of sodium ions (Na+) in patients with chronic heart failure. Reduction of blood pressure in contrast to direct vasodilators (hydralazine, minoxidil, etc.) is not accompanied by reflex tachycardia and leads to a decrease in myocardial oxygen demand. With heart failure in an adequate dose does not affect the value of blood pressure. The maximum decrease in blood pressure after ingestion is observed after 60-90 minutes. The duration of the hypotensive effect is dose-dependent and reaches optimal values within a few weeks.

Pharmacokinetics:

Absorption - Fast, reaches 75% (eating reduces by 30-40%), bioavailability - 35-40% (the effect of "first passage" through the liver). Connection with blood plasma proteins (mainly with albumins) - 25-30%; the maximum concentration in the blood plasma (114 ng / ml) with oral administration - 30-90 min. Through the blood-brain barrier and placental barrier penetrates poorly (less than 1%).

Metabolized in the liver with the formation of disulfide dimer captopril and captopril-cysteine disulfide. Metabolites are pharmacologically inactive. The half-life of - 3 hours excreted by the kidneys 95% (40-50% unchanged), the rest in the form of metabolites.. It is secreted with mother's milk. After 4 hours after a single oral urine contained 38% captopril unchanged and 28% as metabolites through 6h - only as metabolites; in daily urine - 38% of unchanged captopril and 62% - in the form of metabolites. The half-life period for impaired renal function is 3.5-32 hours. Cumulates in chronic renal failure.

Indications:

Arterial hypertension, incl. Renovascular; chronic heart failure (as part ofcomplex therapy); a violation of the function of the left ventricle after a previous myocardial infarction in a clinically stable state; Diabetic nephropathy against type I diabetes mellitus (for albuminuria more than 30 mg / day).

Contraindications:

Increased sensitivity to the drug and other ACE inhibitors, angioedema (in the background of ACE inhibitors, including a history of), expressed impaired renal or hepatic function, hyperkalemia, bilateral renal artery stenosis or artery stenosis only kidneys with progressive azotemia, condition after transplantation kidneys, stenosis of the aortic aorta and similar changes that hinder the outflow of blood, pregnancy, lactation, age 18 years.

Carefully:

Use with caution in severe autoimmune diseases (especially systemic lupus erythematosus or scleroderma), oppression of bone marrow hematopoiesis (risk of developing neutropenia and agranulocytosis), cerebral ischemia, diabetes mellitus (increased risk of hyperkalemia), in patients on hemodialysis, a diet with restriction sodium, primary hyperaldosteronism, ischemic heart disease, conditions,accompanied by a decrease in the volume of circulating blood (including diarrhea, vomiting), in old age.

Dosing and Administration:

Captopril-UBF is administered orally 1 hour before meals. The dosage regimen is set individually. When titrating the dose of the drug captopril according to the declared indications, it is necessary to use captopril in dosage form: tablets of 12.5 mg.

With arterial hypertension, treatment starts with the lowest effective dose of 12.5 mg 2 times a day (rarely with 6.25 mg 2 times a day). Pay attention to the tolerability of the first dose during the first hour. If at the same time arterial hypotension develops, the patient should be transferred to a horizontal position (this reaction to the first dose should not serve as an obstacle to further therapy). If necessary, the dose gradually (with an interval of 2-4 weeks) is increased to achieve the optimal effect. With mild or moderate arterial hypertension, the usual maintenance dose is 25 mg 2 times a day; the maximum dose is 50 mg twice a day. In severe arterial hypertension, the maximum dose is 50 mg 3 times a day. The maximum daily dose is 150 mg.

In elderly patients, the initial dose is 6.25 mg 2 times a day.

When heart failure is prescribed along with diuretics and / or in combination with digitalis preparations (to avoid initial excessive decrease HELL. before the appointment of Captopril-UBF diuretic cancel or reduce the dose). The initial dose is 6.25 mg or 12.5 mg 3 times a day, if necessary, increase the dose gradually (at intervals of not less than 2 weeks) to 25 mg 2-3 times a day. The maximum daily dose is 150 mg.

When violations of left ventricular function after a myocardial infarction in patients in a clinically stable state, the use of Captopril-UBF can begin as early as 3 days after myocardial infarction. The initial dose is 6.25 mg / day, then the daily dose can be increased to 37.5-75 mg for 2-3 doses (depending on the tolerability of the drug). If necessary, the dose is gradually increased to a maximum daily dose of 150 mg / day. With the development of arterial hypotension, a dose reduction may be required. Subsequent attempts to apply the maximum daily dose of 150 mg should be based on tolerability of patients with Captopril-UBF.

When diabetic nephropathy is prescribed in a daily dose of 75-100 mg / day for 2-3 doses.In insulin-dependent diabetes with microalbuminuria (albumin release 30-300 mg per day), the dose of the drug is 50 mg 2 times a day. With a total protein clearance of more than 500 mg per day, the drug is effective at a dose of 25 mg 3 times a day.

With a moderate degree of impaired renal function (creatinine clearance (CK) - at least 30 ml / min / 1.73 m²) Captopril-UBF can be administered at a dose of 75-100 mg / day. With a more pronounced degree of renal dysfunction (CC - less than 30 ml / min / 1.73 m²) the initial dose should not exceed 12.5 mg / day; In the future, if necessary, the dose of Captopril-UBF is gradually increased at sufficiently long intervals, but use a daily dose of the drug that is lower than in the case of arterial hypertension treatment. If necessary, additionally prescribed loop diuretics, and not diuretics thiazide series.

Side effects:

From the side of the cardiovascular system: tachycardia, lowering of arterial pressure, orthostatic hypotension, peripheral edema.

From the central nervous system: dizziness, ataxia, headache, fatigue, asthenia, paresthesia, drowsiness, visual impairment.

From the respiratory system: dry cough, pulmonary edema, bronchospasm.

From the urinary system: impaired renal function.

From the side of water-electrolyte exchange: hyperkalemia, hyponatremia (most often with salt-free diet and simultaneous intake of diuretics), proteinuria, increased urea nitrogen in the blood, creatinine, acidosis.

On the part of the organs of hematopoiesis: neutropenia, anemia, thrombocytopenia, agranulocytosis.

Allergic reactions: angioedema, "hot flashes" to the skin of the face, fever, skin rash (maculopapular, less often vesicular or bullous), itching, photosensitivity, bronchospasm, serum sickness, lymphadenopathy, in rare cases - the appearance of antinuclear antibodies in the blood.

From the digestive system: loss of appetite, dry mouth, stomatitis, dyspepsia, nausea, abdominal pain, constipation or diarrhea, increased activity of "liver" enzymes, hyperbilirubinemia; signs of hepatocellular injury (hepatitis) and cholestasis (in rare cases); pancreatitis (in isolated cases), gingival hyperplasia, intestinal edema.

Other: general weakness, swelling of the legs.

Overdose:

Symptoms: a marked decrease in blood pressure, including collapse, myocardial infarction, acute impairment of cerebral circulation, thromboembolic complications.

Treatment: to lay the patient with raised lower limbs; measures, aimed at restoring blood pressure (increase in the volume of circulating blood, including intravenous infusion of 0.9% sodium chloride solution), symptomatic therapy. Possible use of hemodialysis; peritoneal dialysis - not effective.

Interaction:

Increases the concentration of digoxin in the blood plasma by 15-20%.

Increases the bioavailability of propranolol.

Cimetidine, slowing the metabolism in the liver, increases the concentration of captopril in the blood plasma.

Hypotensive effect weakens non-steroidal anti-inflammatory drugs (NSAIDs) (delay Na+ and decreased synthesis of prostaglandin), especially against a background of low renin concentrations, and estrogens (delay Na+).

Combination with thiazide diuretics, vasodilators (minoxidil), verapamil, beta-adrenoblockers, tricyclic antidepressants, ethanol enhances the hypotensive effect.

Combined use with potassium-sparing diuretics (eg triamterene, spironolactone, amyloride), potassium preparations, cyclosporine, milk with low salt content (can contain K + up to 60 mmol / l), potassium supplements, salt substitutes (contain significant amounts of K +) increases the risk of hyperkalemia.

Slows the excretion of lithium preparations.

When captopril is prescribed against the background of taking allopurinol or procainamide, the risk of developing Stevens-Johnson syndrome and immunosuppressive action is increased. The use of captopril in patients taking immunosuppressants (for example, azathioprine or cyclophosphamide), increases the risk of hematological disorders.

Special instructions:

Before the start, and also regularly during the treatment with Captopril-UBF, kidney function should be monitored. Patients with chronic heart failure are treated under close medical supervision. Against the background of prolonged use of Captopril-UBF, approximately 20% of patients have a stable increase in serum urea and serum creatinine by more than 20%, compared with the norm or the baseline value.Less than 5% of patients, especially in severe nephropathies, require discontinuation of treatment due to increased creatinine concentrations. In patients with arterial hypertension with the use of Captopril-UBF, severe arterial hypotension is observed only in rare cases; the likelihood of developing this condition increases with a loss of fluid and salt loss (for example, after intensive treatment with diuretics), in patients with chronic heart failure or who are on dialysis. The possibility of a sharp drop in blood pressure can be minimized by first canceling (for 4-7 days) a diuretic or increasing the intake of sodium chloride (about a week before the start of the procedure) or by administering captopril at the start of treatment in small doses (6.25- 12.5 mg / day). When therapy in outpatient settings, warn the patient about the possible appearance of symptoms of an infection requiring a follow-up medical examination, a clinical and laboratory examination. In the first 3 months. The therapy monthly controls the number of white blood cells, then - once every 3 months; in patients with autoimmune diseases in the first 3 months - every 2 weeks, then every 2 months.If the number of white blood cells is less than 4000 / mm3, a general blood test is performed, below 1000 / mkl - the drug is stopped. If the first symptoms of a secondary infection occur against a background of myeloid hypoplasia, an extensive blood test should be performed immediately. It is necessary to exclude self-termination of the drug and an independent significant increase in the intensity of physical exertion. In some cases, against the background of the use of ACE inhibitors, incl. captopril, there is an increase in the concentration of potassium in the blood serum. The risk of hyperkalemia when using ACE inhibitors increased in patients with chronic renal insufficiency and diabetes, as well as host potassium-sparing diuretics, potassium supplements or others. Drugs that cause an increase in potassium concentration in the blood (e.g., heparin). You should avoid the simultaneous use of potassium-sparing diuretics and potassium preparations. When hemodialysis in patients receiving Captopril-UBF, the use of dialysis membranes with high permeability should be avoided (for example, AN69), because in such cases the risk of anaphylactoid reactions increases.In case of development of angioedema, the drug is canceled and careful medical supervision and symptomatic therapy are carried out. When taking Captopril-UBF, a false positive reaction can be observed when analyzing urine for acetone.

Be wary appoint patients who are on a low-salt or salt-free diet (an increased risk of arterial hypotension) and hyperkalemia.

Effect on the ability to drive transp. cf. and fur:During the period of treatment it is necessary to refrain from driving motor vehicles and practicing potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions. possibly dizziness, especially after taking the initial dose.

Form release / dosage:

Tablets of 25 mg.

Packaging:

10 tablets per contour cell packaging made of polyvinylchloride film and aluminum foil.

For 10, 20, 30, 40, 50, 60, 100 tablets in cans of polymeric with screw caps.

Each jar or 1, 2, 3, 4, 5 contour mesh packages together with the instruction for use are placed in a pack of cardboard.

Storage conditions:

In a dry, the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-002908/10

Date of registration:07.04.2010

Expiration Date:Unlimited

The owner of the registration certificate:URALBIOFARM, OJSC URALBIOFARM, OJSC Russia

Manufacturer: & nbsp

URALBIOFARM, OJSC Russia

Information update date: & nbsp07.12.2017

Illustrated instructions

Instructions

Captopril-UBF (Captopril-UBF)