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 into angiotensin II and eliminates its vasoconstrictive effect.

As a result of a decrease in the concentration of angiotensin II, a secondary increase in renin plasma activity occurs by eliminating the negative feedback during the release of renin and directly reducing the secretion of aldosterone.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, the maximum concentration is observed in the blood after 50 minutes. The binding with proteins, mainly albumin, is 25-30%. Captopril metabolized in the liver with the formation of disulfide dimer captopril and captopril-cysteine disulfide. Metabolites are pharmacologically inactive. The half-life is about 3 hours. The half-life for chronic renal failure is 3.5-32 hours. Cumulates in chronic kidney failure. More than 95% of the drug is excreted in the urine, 40-50% of which is unchanged, the rest is metabolized. The duration of the drug is about 5 hours.

Indications:

- Ahyperthermia (including renovascular);

- chronic heart failure (as part of combination therapy).

Contraindications:

- Hypersensitivity to captopril and other ACE inhibitors;

- angioedema in history (including in anamnesis after use of other ACE inhibitors);

- severe renal dysfunction, azotemia, hyperkalemia, bilateral stenosis of the renal arteries or stenosis of a single kidney with progressive azotemia, condition after kidney transplantation, primary hyperaldosteronism;

- stenosis of the aortic aorta, mitral stenosis, presence of other obstructions to outflow of blood from the left ventricle of the heart;

- severe liver dysfunction;

- arterial hypotension;

- cardiogenic shock;

- pregnancy and lactation;

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

Carefully:

Severe autoimmune diseases (including systemic lupus erythematosus, scleroderma), suppression of bone marrow circulation (risk of developing neutropenia and agranulocytosis), cerebral ischemia, diabetes mellitus (increased risk of hyperkalemia), patients on hemodialysis, diet with sodium restriction, ischemic heart disease, conditions accompanied by a decrease in the volume of circulating blood (including diarrhea, vomiting), and advanced age.

Dosing and Administration:

Captopril is prescribed an hour before meals.The dosage regimen is set individually.

With arterial hypertensionand the drug is prescribed in an initial dose of 25 mg twice a day. 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.

For the treatment of chronic heart failure captopril appoint in those cases when the use of diuretics does not provide an adequate effect. The initial daily dose is 6.25 mg 3 times a day, if necessary, increase the dose with an interval of at least 2 weeks. The average maintenance dose is 25 mg 2-3 times a day. In the future, if necessary, the dose gradually (with an interval of at least 2 weeks) is increased. 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 be no more than 12.5 - 25 mg / day; Further, if necessary, with sufficiently long intervals, the dose of captopril is gradually increased, but a smaller, than usual, daily dose of the drug is used.

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

Side effects:

Co cardiovascular system: a marked decrease in blood pressure, tachycardia, orthostatic hypotension, peripheral edema.

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

Co side of water-electrolyte and acid-base balance: hyperkalemia, acidosis.

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

Co the central nervous system: dizziness, headache, fatigue, asthenia, ataxia, drowsiness, impaired vision.

Co of the respiratory system: "dry" cough, which occurs after withdrawal of the drug, bronchospasm, pulmonary edema.

Allergic and immunopathological reactions: angioedema, serum sickness, lymphadenopathy, in rare cases - the appearance of antinuclear antibodies in the blood.

Dermatological reactions: a rash, usually maculopapular, less often vesicular or bullous, itching, increased photosensitivity.

From the gastrointestinal tract, liver, pancreas: loss of taste, dry mouth, stomatitis, nausea, decreased appetite, rarely - diarrhea, abdominal pain, increased activity of liver enzymes, signs of hepatocellular injury and cholestasis (in rare cases).

Other: paresthesia.

Overdose:

Symptoms: a marked decrease in blood pressure, including collapse, myocardial infarction, acute cerebrovascular accident, thromboembolic complications.

Treatment: lay the patient with raised lower limbs; measures aimed at restoring blood pressure (increase in the volume of circulating blood, including intravenous infusion of physiological solution), symptomatic therapy. Possible use of hemodialysis; peritoneal hemodialysis - ineffective.

Interaction:

Diuretics and vasodilators (for example, minoxidil) potentiate the hypotensive effect of captopril.

With the combined use of captopril with indomethacin (and, possibly, with other nonsteroidal anti-inflammatory drugs), hypotensive action may decrease.

The hypotensive effect of captopril can be slowed down when administered to patients receiving clonidine.

Simultaneous use with potassium-sparing diuretics or with potassium preparations 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 (for example, cyclophosphamide or azathioprine), increases the risk of hematological disorders.

Special instructions:

Before the beginning, and also regularly during the treatment with the drug captopril kidney function should be monitored.

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

With extreme caution appoint captopril patients with diffuse connective tissue diseases or systemic vasculitis; patients receiving immunosuppressants, especially in the presence of violations of kidney function (the risk of serious infections that are not amenable to antibiotic therapy). In such cases, monitor the pattern of peripheral blood before using captopril, every 2 weeks for the first 3 months of therapy, and periodically - in the subsequent treatment period.

The drug is used with caution on the background of treatment with allopurinol or procainamide, as well as against the background of treatment with immunosuppressants (including, azathioprine, cyclophosphamide), especially in patients with impaired renal function.

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; In the case of increased levels of urea or creatinine in the blood, a reduction in the dose of captopril or withdrawal of the drug may be required. The likelihood of developing arterial hypotension in the course of treatment can be reduced if stopping the use of diuretics or significantly reducing their dose 4 to 7 days before the start of treatment with captopril.

In the case of symptomatic arterial hypotension after taking captopril, the patient should take a horizontal position with raised legs.

In the case of severe arterial hypotension, a positive effect is observed with intravenous administration of an isotonic sodium chloride solution.

In the case of angioedema, the drug is withdrawn and carefully monitored. If the edema is localized on the face, special treatment is usually not required (to reduce the severity of symptoms can be used antihistamines); in that case,if swelling spreads to the tongue, throat or larynx and there is a threat of developing airway obstruction, adrenaline should be injected immediately (INN epinephrine) subcutaneously (0.5 ml diluted 1:1000).

Form release / dosage:

Tablets 25 mg.

Packaging:

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

For 10, 20, 30, 40, 50 or 100 tablets into a polymer container for medicines or a vial of glass with screwed plastic or aluminum caps.

One container (vial) or 1, 2, 4, 6, 8 or 10 out-of-round cell packs, together with the instruction for use, is placed in a pack of cardboard.

For 10 or 20 containers (bottles) or 20, 40, 60, 80 and 100 contour mesh packages, together with the corresponding number of instructions for use, are placed in a cardboard box (for hospitals).

Storage conditions:

In a dry, protected from light place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use the product after the date shown on the package.

Terms of leave from pharmacies:On prescription

Registration number:P N001695 / 01

Date of registration:12.11.2007 / 23.10.2014

Expiration Date:Unlimited

The owner of the registration certificate:OZONE, LLC OZONE, LLC Russia

Manufacturer: & nbsp

OZONE, LLC Russia

Representation: & nbspOZONE LLC OZONE LLC Russia

Information update date: & nbsp06.12.2017

Illustrated instructions

Instructions

Captopril (Captopril)