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

Excipients: lactose (milk sugar), potato starch, microcrystalline cellulose, povidone (low molecular weight medical polyvinylpyrrolidone 12600 ± 2700), magnesium stearate, magnesium hydrosilicate (talc).

Description:

Tablets white or white with a creamy shade of color with a characteristic odor, flat-cylindrical with a bevel. Light marble is allowed.

Pharmacotherapeutic group:Angiotensin converting enzyme inhibitor

ATX: & nbsp

C.09.A.A.01 Captopril

Pharmacodynamics:

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 into angiotensin II and eliminates its vasoconstrictive effect.

As a result of a decrease in angiotensin II concentration, a secondary increase in plasma renin activity occurs due to 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), wedging pressure in the pulmonary capillaries (preload) and resistance in the 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 the absorption by 30-40%. Communication with blood proteins, mainly with albumins, is 25-30%. Poorly penetrates the blood-brain barrier and placental barrier (less than 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:

- Pincreased sensitivity to captopril and other ACE inhibitors;

- angioedema (history of therapy with ACE inhibitors or hereditary);

- severe violations of the liver and / or kidney function;

- bilateral stenosis of the renal arteries;

- stenosis of the artery of a single kidney with progressive azotemia;

- condition after kidney transplantation;

- hyperkalemia;

- stenosis of the aortic or other obstructions to outflow of blood from the left ventricle of the heart;

- pregnancy and lactation;

- age to 18 years (efficacy and safety not established).

Carefully:

Primary hyperaldosteronism, ischemic heart disease, cerebrovascular diseases, severe autoimmune diseases of connective tissue (including systemic lupus erythematosus, scleroderma), oppression of bone marrow hematopoiesis (risk of neutropenia and agranulocytosis), cerebral ischemia, diabetes mellitus (increased risk of hyperkalemia), sick,hemodialysis-based diets with sodium restriction; conditions, 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. 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 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 hypertension, the usual maintenance dose is 25 mg twice 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 is prescribed 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 per 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 dose of the drug is selected individually, therapy is recommended to start with a dose of 6.25 mg 2 times a day and, if possible, maintain it at this level.

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

Side effects:

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

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

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

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

Co hematopoiesis side: neutropenia, anemia, thrombocytopenia, agranulocytosis.

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

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

Co the sides of the digestive system: nausea, decreased appetite, dry mouth, dyspnoea, stomatitis, gingival hyperplasia, diarrhea, abdominal pain,an increase in the activity of liver enzymes, signs of hepatocellular injury, cholestasis (in rare cases), hepatitis, hyperbilirubinemia.

Overdose:

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

Treatment: give the patient a position with raised lower limbs; introduction of an isotonic solution of sodium chloride 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), beta-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 (azathioprine, cyclophosphamide 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.

In patients with chronic renal insufficiency apply under careful 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 tissue diseases, 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, blood leukocyte counts should be monitored every 2 weeks during the first 3 months of captopril therapy, then every 2 months. If the number of white blood cells is less than 1 thousand / μl, the drug intake terminate.

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 to patients with stenosis of the renal arteries, tk. 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 host potassium-sparing diuretics, potassium supplements, and drugs that increase in blood potassium levels (e.g., heparin) the risk of 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 treatment, care must be taken when driving and occupation of other potentially hazardous activities that require high concentration and psychomotor speed reactions (dizziness, especially after receiving the starting dose).

Form release / dosage:

Tablets of 25 mg.

Packaging:

For 20, 30, 40 tablets in a can of orange glass or in a polymer can.

For 10 tablets in a contour mesh or contour non-jawed packaging.

One bank, 2, 3 or 4 contour packs together with the instruction for use are placed in a cardboard box.

Storage conditions:

In a dry place, protected from light, out of reach of children, at a temperature not exceeding 25 ° C.

Shelf life:

2 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:P N000732 / 01

Date of registration:09.04.2008

Expiration Date:Unlimited

The owner of the registration certificate:BIOSINTEZ, PAO BIOSINTEZ, PAO Russia

Manufacturer: & nbsp

BIOSINTEZ, PAO Russia

Representation: & nbspBIOSINTEZ JSC BIOSINTEZ JSC Russia

Information update date: & nbsp06.12.2017

Illustrated instructions

Instructions

Captopril (Captopril)