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

Tablets are white or white with a creamy shade of color with a characteristic odor, biconvex with a risk on one side. Light marble is allowed. In appearance, must comply with the requirements of GF XI, issue. 2, p. 154.

Pharmacotherapeutic group:ACE inhibitor

ATX: & nbsp

C.09.A.A.01 Captopril

Pharmacodynamics:Angiotensin-converting enzyme (ACE) inhibitor. 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. Promotes content reduction Na+ in patients with 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 duringseveral weeks.

Pharmacokinetics:

Absorption - fast, reaches 75% (eating intake reduces absorption by 30-40%). Bioavailability - 35-40% (the effect of "first passage" through the liver). The connection with blood plasma proteins (mainly with albumins) is 25-30%. The maximum concentration in blood plasma (114 ng / ml) with oral intake is achieved after 30-90 minutes. 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 is 3 hours. It is 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 intake, 38% of unchanged captopril and 28% of metabolites are contained in the urine, in 6 hours only in the form of metabolites; in daily urine - 38% of unchanged captopril and 62% - in the form of metabolites. Half-life with impaired renal function is 3.5-32 hours. Cumulates in chronic kidney failure.

Indications:

Arterial hypertension, includingRenovascular; chronic heart failure (as part of complex 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:

Hypersensitivity to the drug and other ACE inhibitors, angioedema (against the backdrop of the use of ACE inhibitors, including in the anamnesis); severe renal or hepatic impairment; hyperkalemia; bilateral stenosis of the renal arteries or stenosis of the artery of a single kidney with progressive azotemia; condition after kidney transplantation; stenosis of the aortic orifice and similar obstructive changes that hinder the outflow of blood; pregnancy, lactation; age to 18 years.

Carefully:

Severe autoimmune diseases (especially SLE or scleroderma), oppression of bone marrow hematopoiesis (risk of neutropenia and agranulocytosis), cerebral ischemia, diabetes mellitus (increased risk of hyperkalemia); patients on hemodialysis; diet with sodium restriction; primary hyperaldosteronism; cardiac ischemia;conditions, accompanied by a decrease in the volume of circulating blood (including diarrhea, vomiting); elderly age.

Dosing and Administration:

Captopril-STI is administered orally 1 hour before meals. The dosage regimen is set individually.

With arterial hypertension, treatment is prescribed with the lowest effective dose of 12.5 mg twice 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 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.

If heart failure is prescribed together with diuretics and / or in combination with digitalis preparations (in order to avoid initial excessive reduction of blood pressure, prior to the appointment of Captopril-STI 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 to 25 mg 3 times a day. The maximum daily dose is 150 mg.

In cases of violations of left ventricular function after a myocardial infarction in patients in a clinically stable state, the use of Captopril-STI 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 drug tolerability). 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 a maximum daily dose of 150 mg should be based on tolerability of patients with Captopril-STI.

With diabetic nephropathy, Captopril-STI 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 renal dysfunction (KK - not less than 30 ml / min / 1.73 m 2) Captopril-STI can be administered at a dose of 75-100 mg / day. With a more severe degree of renal dysfunction (CC - less than 30 ml / min / 1.73 square meters), the initial dose should not exceed 12.5 mg / day; In the future, if necessary, the dose of Captopril-STI is gradually increased after sufficiently long intervals of time, but use a daily dose of the drug less than in the case of arterial hypertension.

If necessary, additionally prescribed loop diuretics, and not diuretics thiazide series.

Side effects:

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

From the nervous system: dizziness, headache, fatigue, asthenia, paresthesia.

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

From the urinary system: proteinuria, impaired renal function (increased levels of urea and creatinine in the blood).

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

From the digestive system: decreased appetite, taste, mouth dryness, stomatitis, nausea, abdominal pain, dyspepsia, constipation or diarrhea, increased activity of "liver" transaminases, hyperbilirubinemia, signs of hepatocellular damage (hepatitis) and cholestasis (in rare cases); pancreatitis (in isolated cases).

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

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

Other: general weakness.

Overdose:

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

Treatment: to lay the patient with raised lower limbs; take measures aimed at restoring blood pressure (increasing the volume of circulating blood,including intravenous infusion of physiological saline), symptomatic therapy.

Possible use of hemodialysis; peritoneal dialysis is not effective.

Interaction:

Captopril 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 (delay Na+ and decreased synthesis of prostaglandin).

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

Combined application with potassium-sparing diuretics, potassium preparations, cyclosporin, potassium supplements, salt substitutes (contain significant amounts of K⁺) increases the risk of hyperkalemia.

Slows the excretion of lithium preparations.

When combined with procainamide, allopurinol, flecainide, the risk of developing an immunosuppressive effect is increased.

Probenecid slows the excretion of captopril with urine.

Clonidine reduces the severity of the hypotensive effect.

Immunosuppressants (azathioprine or cyclophosphamide) increase the risk of hematological disorders.

Special instructions:

Before the start, and also regularly during the treatment with Captopril-STI, kidney function should be monitored. Patients with chronic heart failure are treated under close medical supervision.

Against a background of prolonged use of Captopril-STI in about 20% of patients, an increase in urea and serum creatinine by more than 20% is observed, 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-STI expressed arterial hypotension is observed only in rare cases. The likelihood of developing arterial hypotension increases with a deficiency of fluid and salts (for example, after intensive treatment with diuretics), in patients with heart failure or who are on dialysis.

The possibility of a sharp decrease 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 admission),or by the appointment of Captopril-STI at the start of treatment in small doses (6.25-12.5 mg / day).

In the first 3 months of therapy, the number of blood leukocytes is monitored monthly, 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.

In some cases, against the background of the use of ACE inhibitors, incl. Captopril-STI, an increase in the concentration of K + in serum is observed. The risk of hyperkalemia in the use of captopril is increased in patients with renal insufficiency and diabetes mellitus, as well as taking potassium-sparing diuretics, potassium preparations or other drugs that cause an increase in the concentration of K + in the blood (eg, heparin). You should avoid the simultaneous use of potassium-sparing diuretics and potassium preparations.

When hemodialysis in patients receiving Captopril-STI, the use of dialysis membranes with high permeability (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-STI, a false positive reaction may be observed when analyzing urine for acetone.

Be wary appoint patients who are on malosolevoy or salt-free diet (increased risk of arterial hypotension).

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

Form release / dosage:

Tablets of 25 and 50 mg.

Packaging:

For 10 tablets in a contour mesh package (blister) or 20, 30, 40, 50 or 60 tablets in a can of polymer or a bottle of polymer.

By 2, 3, 4, 5 or 6 blisters or a jar or bottle together with the instruction for use is placed in a cardboard box.

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:

3 years.

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

Terms of leave from pharmacies:On prescription

Registration number:P N002904 / 01

Date of registration:14.01.2009 / 24.06.2010

Expiration Date:Unlimited

The owner of the registration certificate:AVVA RUS, OJSC AVVA RUS, OJSC Russia

Manufacturer: & nbsp

AVVA RUS, OJSC Russia

Representation: & nbspAVVA ENG JSC AVVA ENG JSC Russia

Information update date: & nbsp07.12.2017

Illustrated instructions

Instructions

Captopril-STI (Captopril-STI)