Captopril, tablets 25 mg 40 pcs

Captopril

Indications

arterial hypertension (including renovascular);
chronic heart failure (as part of combination therapy).

Pharmacological effect

Pharmacotherapeutic group: ACE blocker

Pharmacological action

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 to angiotensin II and eliminates its vasoconstrictor effect.

As a result of a decrease in the concentration of angiotensin II, a secondary increase in plasma renin activity occurs due to the elimination of negative feedback during the release of renin and a direct decrease in aldosterone secretion. Due to its vasodilatory effect, it reduces total peripheral vascular resistance (afterload), wedge pressure in the pulmonary capillaries (preload) and resistance in the pulmonary vessels; increases cardiac output and exercise tolerance. Does not affect lipid metabolism.

Causes a decrease in bradykinin degradation (one of the effects of ACE) and an increase in Pg synthesis.

The hypotensive effect does not depend on the activity of plasma renin; a decrease in blood pressure is observed at normal and even reduced concentrations of the hormone, which is due to the effect on the tissue RAAS. Increases coronary and renal blood flow.

With long-term use, it reduces the severity of hypertrophy of the myocardium and the walls of resistive arteries. Improves blood supply to ischemic myocardium.

Reduces platelet aggregation.

Pharmacokinetics

Suction and distribution

After oral administration, at least 75% of the drug is rapidly absorbed and Cmax is observed in the blood after 50 minutes.

Protein binding, mainly albumin, is 25-30%.

Metabolism and excretion

Captopril is metabolized in the liver.

T1/2 is about 3 hours. More than 95% of the drug is excreted in the urine, of which 40-50% is unchanged, the rest is excreted in the form of metabolites. The duration of action of the drug is about 5 hours.

Special instructions

Before starting, as well as regularly during treatment with captopril, kidney function should be monitored.

For chronic heart failure, the drug is used subject to careful medical supervision.

Captopril is prescribed with extreme caution to patients with diffuse connective tissue diseases or systemic vasculitis; patients receiving immunosuppressants, especially those with impaired renal function (risk of developing serious infections that cannot be treated with antibiotics). In such cases, peripheral blood patterns should be monitored before starting captopril, every 2 weeks during the first 3 months of therapy, and periodically during the subsequent treatment period.

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

Use with caution in patients with a history of kidney disease, as the risk of developing proteinuria increases. In such cases, the amount of protein in the urine should be monitored monthly during the first 9 months of treatment with captopril. If the level of protein in the urine exceeds 1 g/day, it is necessary to decide on the advisability of further use of the drug. Captopril should be prescribed with caution to patients with renal artery stenosis, because there is a risk of developing renal dysfunction; if the level of urea or creatinine in the blood increases, it may be necessary to reduce the dose of captopril or discontinue the drug.

When performing hemodialysis in patients receiving captopril, the use of high permeability dialysis membranes (including AN69) should be avoided, because this increases the risk of developing anaphylactoid reactions.

The likelihood of developing arterial hypotension during treatment can be reduced if you stop using diuretics or significantly reduce their dose 4-7 days before starting captopril treatment.

If symptomatic arterial hypotension occurs after taking captopril, the patient should take a horizontal position with legs elevated.

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

If angioedema develops, the drug is discontinued and careful medical observation is carried out. If the swelling is localized on the face, special treatment is usually not required (antihistamines can be used to reduce the severity of symptoms); in the event that the swelling spreads to the tongue, pharynx or larynx and there is a threat of developing airway obstruction, epinephrine (adrenaline) should be immediately administered subcutaneously (0.5 ml in a dilution of 1:1000).

Impact on the ability to drive vehicles and machinery

During treatment with captopril, it is necessary to refrain from driving vehicles and engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions, because Dizziness may occur, especially after taking the initial dose.

Active ingredient

Captopril

Composition

Active substance: captopril

Contraindications

angioedema, incl. hereditary, history (including history after use of other ACE inhibitors);
severe renal dysfunction, azotemia, hyperkalemia, bilateral renal artery stenosis or stenosis of a single kidney with progressive azotemia, condition after kidney transplantation, primary hyperaldosteronism;
stenosis of the aortic mouth, mitral stenosis, the presence of other obstacles to the outflow of blood from the left ventricle of the heart;
severe liver dysfunction;
arterial hypotension;
cardiogenic shock;
pregnancy and lactation;
age under 18 years (efficacy and safety have not been established).
hypersensitivity to captopril and other ACE inhibitors.

Use with caution: severe autoimmune diseases (including systemic lupus erythematosus, scleroderma), inhibition of bone marrow circulation (risk of developing neutropenia and agranulocytosis), cerebral ischemia, diabetes mellitus (increased risk of developing hyperkalemia), patients on hemodialysis, sodium-restricted diet, coronary heart disease, conditions accompanied by a decrease in blood volume (including diarrhea, vomiting), old age.

Side Effects

From the cardiovascular system: marked decrease in blood pressure, tachycardia, orthostatic hypotension, peripheral edema.

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

From the hematopoietic system: rarely – neutropenia, anemia, thrombocytopenia, agranulocytosis.

From the central nervous system: dizziness, headache, ataxia, paresthesia, drowsiness, blurred vision, fatigue, asthenia.

From the respiratory system: dry cough that goes away after discontinuation of the drug, bronchospasm, pulmonary edema.

Allergic and immunopathological reactions: angioedema of the extremities, face, lips, mucous membranes, tongue, pharynx and larynx, as well as intestinal edema (very rare), serum sickness, lymphadenopathy, in rare cases – the appearance of antinuclear antibodies in the blood.

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

From the gastrointestinal tract, liver, pancreas: impaired taste, dry mouth, stomatitis, nausea, decreased appetite, rarely – diarrhea, abdominal pain, increased activity of liver transaminases, hyperbilirubinemia, hepatitis.

Laboratory indicators: hyperkalemia, hyponatremia, acidosis. Cases of hypoglycemia have been reported in patients with diabetes mellitus who took insulin and oral hypoglycemic drugs.

Other: paresthesia.

Interaction

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

When captopril is used concomitantly with indomethacin (and possibly with other NSAIDs), a decrease in the hypotensive effect may be observed.

The hypotensive effect of captopril can be reduced by estrogens (Na+ retention).

The hypotensive effect of captopril may be delayed when administered to patients receiving clonidine.

Concomitant use with potassium-sparing diuretics or potassium supplements may lead to hyperkalemia.

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

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, cyclophosphacine or azathioprine) increases the risk of developing hematological disorders.

With the simultaneous use of ACE inhibitors and gold preparations (sodium aurothiomalate), a symptom complex has been described, including facial flushing, nausea, vomiting and decreased blood pressure.

The simultaneous use of insulin and oral hypoglycemic drugs increases the risk of developing hypoglycemia.

Overdose

Symptoms: pronounced decrease in blood pressure, up to collapse, myocardial infarction, acute cerebrovascular accident, thromboembolic complications.

Treatment: place the patient with the lower limbs elevated; measures aimed at restoring blood pressure (increasing blood volume, including intravenous infusion of saline), symptomatic therapy. Hemodialysis may be used; peritoneal dialysis is ineffective.

Manufacturer

Pharmacor Production, Russia