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

The mechanism of antihypertensive action is associated with competitive inhibition of ACE activity, which leads to a decrease in the rate of conversion of angiotensin I in angiotensin II and eliminates its vasoconstrictive effect.

As a result of a decrease in angiotensin concentration II there is a secondary increase in plasma renin activity due to the elimination of negative feedback during the release of renin and a direct decrease in aldosterone secretion. Due to the vasodilator effect, reduces the overall peripheral vascular resistance (afterload), the pressure of wedging in the pulmonary capillaries (preload) and resistance in pulmonary vessels; increases the minute volume of the heart and tolerance to the load. Does not affect lipid metabolism.

Pharmacokinetics:After ingestion, at least 75% of the drug is rapidly absorbed, and the maximum concentration is observed in the blood after 30-90 minutes. Simultaneous food intake reduces intake by 30-40%. The connection with blood plasma proteins, mainly with albumins, is 25-30%. Poorly penetrates through the blood-brain and placental barrier (1%). Metabolised in the liver. More than 95% of captopril is excreted by the kidneys, 40-50% of which are unchanged, the rest is in the form of metabolites. Half-life is 3 hours, with chronic renal failure may increase to 32 hours. It is secreted with mother's milk.

Indications:

Arterial hypertension (including renovascular).

Chronic heart failure (as part of combination therapy).

Contraindications:

Hypersensitivity to captopril and other ACE inhibitors, angioedema (history of therapy with ACE inhibitors or hereditary), severe liver and / or kidney dysfunction, hyperkalemia, stenosis of the aortic or other obstructions to outflow from the left ventricle of the heart, bilateral stenosis renal arteries, arterial stenosis of a single kidney with progressive azotemia, condition after kidney transplantation, pregnancy and lactation, age under 18 (efficacy and safety not established Lena).

Carefully:

Primary aldosteronism, coronary heart disease, cerebrovascular disease, severe autoimmune connective tissue disease (including systemic lupus erythematosus, scleroderma), inhibition of bone marrow hematopoiesis (the risk of neutropenia and agranulocytosis), cerebral ischemia, diabetes (increased risk of hyperkalemia) patients who are on hemodialysis, a diet with sodium restriction; state,accompanied by a decrease in the volume of circulating blood (including diarrhea, vomiting), advanced age (dose adjustment is required).

Dosing and Administration:

Captopril is administered orally 1 hour before meals. Dosage regimen is set by the doctor.

With arterial hypertension the drug is prescribed in an initial dose of 12.5 mg twice a day. If necessary, the dose gradually (with an interval of 2-4 weeks) is increased to achieve the optimal effect. With a mild or moderate degree of arterial hypertension, the usual maintenance dose is 25 mg 2 times a day; the maximum dose is 50 mg twice a day. With a severe degree of hypertension, the maximum dose is 50 mg 3 times a day. The maximum daily dose is 150 mg.

For the treatment of chronic heart failure captopril prescribe as part of a combination therapy (including together with diuretics and / or with digitalis preparations). The initial dose is 6.25 mg 3 times a day. In the future, if necessary (with intervals of at least 2 weeks) the dose is gradually increased. The average maintenance dose is 25 mg 2-3 times a day. The maximum dose is 150 mg / day.

Patients with impaired renal function with a moderate degree of renal dysfunction (creatinine clearance (CK) of at least 30 ml / min / 1.73 m²) captopril can be prescribed in 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 per day; In the future, if necessary, the dose of captopril is increased, with sufficiently long intervals, but use less than the recommended daily dose.

In old age the dose of the drug is selected individually, it is recommended to start therapy with a dose of 6.25 mg twice a day and, if possible, maintain it at this level.

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

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

From the side of the water-electrolyte and acid-base state: hyperkalemia, acidosis.

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

From the respiratory system: dry cough usually occurring after withdrawal of the drug, bronchospasm, pulmonary edema.

Allergic and immunopathological reactions: angioedema limbs, face, lips, mucous membranes of the tongue, pharynx and larynx, "tides" of blood to the skin of the face, rash (maculopapular nature, less often vesicular or bullous character), itching, increased photosensitivity, serum sickness, lymphadenopathy, in rare cases antinuclear antibodies in the blood.

From the side of the digestive tract: nausea, decreased appetite, dry mouth, taste disorders, stomatitis, gingival hyperplasia, diarrhea, abdominal pain, increased activity of liver enzymes, signs of hepatocellular injury, cholestasis (in rare cases), hepatitis, hyperbilirubinemia.

Overdose:Symptoms: a marked decrease in blood pressure, myocardial infarction, acute violation of cerebral circulation, thromboembolic complications.

Treatment: give patient position with raised lower limbs; introductionisotonic sodium chloride solution or other plasma-substituting solutions, hemodialysis, symptomatic therapy.

Interaction:

Increases the concentration of digoxin in the blood plasma. Increases the bioavailability of propranolol.

Cimetidine increases the concentration of captopril in the blood plasma.

Diuretics and vasodilators (for example, minoxidil), B-adrenoblockers, blockers of "slow" calcium channels, tricyclic antidepressants, ethanol increase the hypotensive effect of captopril.

Non-steroidal anti-inflammatory drugs and clonidine reduce the hypotensive effect of captopril.

Simultaneous use with potassium-sparing diuretics, potassium preparations, cyclosporine can lead to hyperkalemia.

With the simultaneous use of lithium salts, it is possible to increase the concentration of lithium in the blood serum.

The use of captopril in patients taking allopurinol or procainamide, increases the risk of developing neutropenia and / or Stevens-Johnson syndrome.

The use of captopril in patients taking immunosuppressants (cyclophosphacin, azathioprine and others) increases the risk of hematological abnormalities.

Special instructions:

Before the beginning, and also regularly during the treatment with the drug Captopril kidney function should be monitored. Patients with chronic renal failure are used under close medical supervision.

In patients with hypertension, the likelihood of developing severe arterial hypotension with captopril increases with a deficiency of fluid and salts, for example, with intensive treatment with diuretics, using a low and salt-free diet. The possibility of a sharp decrease in blood pressure is reduced to a minimum with a preliminary (for 4-7 days) cancellation of the diuretic or a decrease in its dose.

In chronic heart failure, the drug is used under conditions of careful medical supervision.

With extreme caution appoint captopril patients with autoimmune diseases (diffuse connective diseases tissue, systemic vasculitis), patients receiving allopurinol, procainamide, immunosuppressants, especially in the presence of violations of kidney function (the risk of serious infections that can not be treated with antibiotics).In such cases, the blood leukocyte count should be monitored every 2 weeks during the first 3 months of therapy captopril, then - every 2 months. If the number of white blood cells is less than 1 thousand / mm3, the drug is stopped.

Caution is used in patients with a history of kidney disease, as the risk of developing proteinuria increases. In such cases, during the first 9 months of treatment with captopril, the amount of protein in the urine should be monitored on a monthly basis. If the level of protein in the urine exceeds 1 g / day, it is necessary to decide whether further use of the drug is advisable. With caution appoint captopril patients with stenosis of the renal arteries; there is a risk of kidney dysfunction; If urea and / or creatinine levels increase, a reduction in the dose of captopril or drug withdrawal may be required.

In patients with renal insufficiency and diabetes, as well as taking potassium-sparing diuretics., Potassium preparations, and drugs that raise the level of potassium in the blood (eg, heparin), there is a risk of developing hyperkalemia.You should avoid the simultaneous use of potassium-sparing diuretics and potassium preparations.

When conducting hemodialysis in patients receiving captopril, the use of dialysis membranes with high permeability should be avoided, since in such cases the risk of developing anaphylactoid reactions increases.

When taking captopril, a false positive reaction may be observed when analyzing urine for acetone.

Effect on the ability to drive transp. cf. and fur:

During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities requiring increased attention and speed of psychomotor reactions (possibly dizziness, especially after taking the initial dose).

Form release / dosage:

Tablets of 25 mg and 50 mg.

Packaging:For 10 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

For 2 or 4 contour packagings together with the instructions for use are placed in a pack of cardboard.

Storage conditions:

In the dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:

4 years.

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

Terms of leave from pharmacies:On prescription

Registration number:P N000488 / 01

Date of registration:21.07.2008 / 18.05.2012

Expiration Date:Unlimited

The owner of the registration certificate:VALENTA PHARM, PAO VALENTA PHARM, PAO Russia

Manufacturer: & nbsp

VALENTA PHARMACEUTICS, JSC Russia

Representation: & nbspVALENTA PHARM, PAO VALENTA PHARM, PAO Russia

Information update date: & nbsp06.12.2017

Illustrated instructions

Instructions

Captopril (Captopril)