Description of the active substance:
This information is a reference and it is not enough that the drug has been prescribed by a doctor ..
PHARMACHOLOGIC EFFECT
Antihypertensive agent, ACE inhibitor. 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 (which has a pronounced vasoconstrictive effect and stimulates the secretion of aldosterone in the adrenal cortex). In addition, captopril, apparently, has an effect on the kinin-kallikrein system, preventing the breakdown of bradykinin. The hypotensive effect does not depend on the plasma renin activity, the decrease in blood pressure is noted with a normal and even decreased concentration of the hormone, which is due to the effect on tissue RAAS. Increases coronary and renal blood flow.
Due to vasodilator effect, reduces OPSS (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. With prolonged use reduces the severity of myocardial hypertrophy of the left ventricle, prevents the progression of heart failure and slows the development of dilatation of the left ventricle. Helps reduce sodium content in patients with chronic heart failure. Expands arteries more than veins. Improves the blood supply of the ischemic myocardium. Reduces the aggregation of platelets.
Reduces the tone of arterioles spreading the glomerulus of the kidneys, improving intra-cerebral hemodynamics, prevents the development of diabetic nephropathy.
PHARMACOKINETICS
After oral administration, at least 75% is rapidly absorbed from the digestive tract. Simultaneous food intake reduces the absorption by 30-40%. C max in blood plasma is achieved after 30-90 min. The binding with proteins, mainly albumin, is 25-30%. Excreted in breast milk. Metabolized in the liver with the formation of disulfide dimer captopril and captopril-cysteine ​​disulfide. Metabolites are pharmacologically inactive.
T 1/2 is less than 3 hours and increases with renal insufficiency (3.5-32 hours). More than 95% is excreted by the kidneys, 40-50% unchanged, the rest - in the form of metabolites.
In chronic renal failure cumulates.
INDICATIONS
Arterial hypertension (including renovascular), chronic heart failure (as part of combination therapy), left ventricular dysfunction after myocardial infarction in patients in a clinically stable state. Diabetic nephropathy in type 1 diabetes mellitus (for albuminuria more than 30 mg / day).
DOSING MODE
When administered orally, the initial dose is 6.25-12.5 mg 2-3 times / day. With insufficient effect, the dose is gradually increased to 25-50 mg 3 times / day. In case of violations of kidney function, the daily dose should be reduced.
The maximum daily dose is 150 mg.
SIDE EFFECT
From the central nervous system and peripheral nervous system: dizziness, headache, fatigue, asthenia, paresthesia.
From the cardiovascular system: orthostatic hypotension; rarely - tachycardia.
On the part of the digestive system: nausea, decreased appetite, a violation of taste; rarely - abdominal pain, diarrhea or constipation, increased activity of hepatic transaminases, hyperbilirubinemia; signs of hepatocellular injury (hepatitis); in some cases - cholestasis; in isolated cases - pancreatitis.
From the hemopoietic system: rarely - neutropenia, anemia, thrombocytopenia; very rarely in patients with autoimmune diseases - agranulocytosis.
From the side of metabolism: hyperkalemia, acidosis.
From the urinary system: proteinuria, impaired renal function (increased concentration of urea and creatinine in the blood).
From the respiratory system: dry cough.
Allergic reactions: skin rash; rarely - Quincke's edema, bronchospasm, serum sickness, lymphadenopathy; in some cases - the appearance of antinuclear antibodies in the blood.
CONTRAINDICATIONS
Pregnancy, lactation, age under 18, hypersensitivity to captopril and other ACE inhibitors.
PREGNANCY AND LACTATION
It should be borne in mind that the use of captopril in the II and III trimesters of pregnancy can cause developmental disorders and fetal death. When pregnancy is established, captopril should be immediately discontinued.
Captopril is excreted in breast milk. If it is necessary to use during the lactation period, the question of stopping breastfeeding should be solved.
APPLICATION FOR FUNCTIONS OF THE LIVER
With caution should be used in the condition after kidney transplantation, kidney failure.
In case of violations of kidney function, the daily dose should be reduced.
It is necessary to avoid simultaneous use of potassium-sparing diuretics and potassium preparations in patients with renal insufficiency.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
With caution should be used for liver failure.
APPLICATION FOR CHILDREN
Contraindicated at the age of 18 years. The use of captopril in children is possible only in the case of ineffectiveness of other drugs.
APPLICATION IN ELDERLY PATIENTS
Caution should be used in elderly patients.
SPECIAL INSTRUCTIONS
It should be used with caution in case of anginaevrotic edema on the background of therapy with ACE inhibitors, hereditary or idiopathic angioedema, with aortic stenosis, cerebrovascular and cardiovascular diseases (including cerebral circulatory insufficiency, coronary heart disease, coronary insufficiency), severe autoimmune diseases of connective tissue (including SLE, scleroderma), with oppression of bone marrow hematopoiesis, diabetes mellitus, hyperkalemia, bilateral stenosis of the renal arteries, ste a single-kidney artery, a condition after kidney transplantation, kidney and / or liver failure, against a background of a diet with sodium restriction, conditions accompanied by a decrease in BCC (including diarrhea, vomiting), in elderly patients.
In patients with chronic heart failure, captopril is used under close medical supervision.
The arterial hypotension arising during surgical intervention on the background of taking captopril is eliminated by replenishing the volume of the liquid.
It should avoid the simultaneous use of potassium-sparing diuretics and potassium preparations, especially in patients with renal insufficiency and diabetes mellitus.
When taking captopril, a false positive reaction may be observed when analyzing urine for acetone.
The use of captopril in children is possible only in the case of ineffectiveness of other drugs.
Impact on the ability to drive vehicles and manage mechanisms
Care must be taken when driving vehicles or doing other work that requires increased attention, because possibly dizziness, especially after the initial dose of captopril.
DRUG INTERACTION
With simultaneous use with immunosuppressants, cytostatics increases the risk of developing leukopenia.
With simultaneous application with potassium-sparing diuretics (including spironolactone, triamterene, amiloride), potassium preparations, salt substitutes and dietary supplements to food containing potassium, it is possible to develop hyperkalemia (especially in patients with impaired renal function) because ACE inhibitors reduce the content of aldosterone, which leads to a delay in potassium in the body against the background of the limitation of the excretion of potassium or its additional intake into the body.
With simultaneous use of ACE inhibitors and NSAIDs, the risk of kidney dysfunction is increased; rarely observed hyperkalemia.
With simultaneous use with "loop" diuretics or thiazide diuretics, severe arterial hypotension is possible, especially after taking the first dose of a diuretic, apparently due to hypovolemia, which leads to a transient enhancement of the antihypertensive effect of captopril. There is a risk of hypokalemia. Increased risk of kidney dysfunction.
With simultaneous use with funds for anesthesia, severe arterial hypotension is possible.
With simultaneous use with azathioprine, the development of anemia is possible, which is due to the inhibition of erythropoietin activity under the influence of ACE inhibitors and azathioprine. There are cases of development of leukopenia, which may be due to the additive inhibition of bone marrow function.
With simultaneous application with allopurinol, the risk of hematological disorders increases; cases of development of severe hypersensitivity reactions, including Stevens-Johnson syndrome, are described.
With the simultaneous use of aluminum hydroxide, magnesium hydroxide, magnesium carbonate, the bioavailability of captopril decreases.
Acetylsalicylic acid in high doses can reduce the antihypertensive effect of captopril. Finally, it is not established whether acetylsalicylic acid reduces the therapeutic efficacy of ACE inhibitors in patients with ischemic heart disease and heart failure. The nature of this interaction depends on the course of the disease. Acetylsalicylic acid, by inhibiting COX and the synthesis of prostaglandins, can cause vasoconstriction, which leads to a reduction in cardiac output and worsening of patients with heart failure receiving ACE inhibitors.
There are reports of an increase in the concentration of digoxin in the blood plasma with the simultaneous use of captopril with digoxin. The risk of developing drug interactions is elevated in patients with impaired renal function.
When used concomitantly with indomethacin, ibuprofen, the antihypertensive effect of captopril is reduced, presumably due to the inhibition of the synthesis of prostaglandins under the influence of NSAIDs (which are believed to play a role in the development of the antihypertensive effect of ACE inhibitors).
With simultaneous use with insulin, hypoglycemic agents, derivatives of sulfonylureas may develop hypoglycemia due to increased tolerance to glucose.
With the simultaneous use of ACE inhibitors and interleukin-3, there is a risk of developing arterial hypotension.
When used simultaneously with interferon alpha-2a or interferon beta, cases of severe granulocytopenia are described.
When switching from clonidine to captopril, the antihypertensive effect of the latter develops gradually. In the case of sudden withdrawal of clonidine in patients receiving captopril, a sharp increase in blood pressure is possible.
With the simultaneous use of lithium carbonate, the concentration of lithium in the serum increases, accompanied by symptoms of intoxication.
With simultaneous use with minoxidil, sodium nitroprusside, the antihypertensive effect is enhanced.
With simultaneous application with orlistatom may reduce the effectiveness of captopril, which can lead to an increase in blood pressure, hypertensive crisis, described the case of cerebral hemorrhage.
With the simultaneous use of ACE inhibitors with pergolide, an increase in the antihypertensive effect is possible.
With simultaneous application with probenecid, the renal clearance of captopril decreases.
With simultaneous use with procainamide, there may be an increased risk of developing leukopenia.
With simultaneous use with trimethoprim, there is a risk of hyperkalemia, especially in patients with impaired renal function.
With simultaneous use with chlorpromazine, there is a risk of developing orthostatic hypotension.
With simultaneous application with cyclosporine there are reports of the development of acute renal failure, oliguria.
It is believed that it is possible to reduce the effectiveness of antihypertensive agents when used simultaneously with erythropoietins.
