Captopril Ozone pills 50mg N40
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Description
The drug Captopril has a hypotensive, vasodilating, natriureticheskoe, cardioprotective effect. Appointed as part of complex therapy for cardiovascular diseases.
Active ingredients
Captopril
Release form
Pills
Composition
Captopril, microcrystalline cellulose, milk sugar, corn or potato starch, polyvinylpyrrolidone, magnesium steric acid.
Pharmacological effect
Angiotensin-converting enzyme inhibitor. Reduces the formation of angiotensin II from angiotensin I. Reducing the content of angiotensin II leads to a direct reduction in the release of aldosterone. This reduces the total peripheral vascular resistance, blood pressure, post- and preload on the heart. Expands arteries to a greater extent than veins. It causes a decrease in the degradation of bradykinin (one of the effects of ACE) and an increase in the synthesis of prostagdandin. The hypotensive effect does not depend on plasma renin activity, a decrease in blood pressure is noted at normal and even reduced levels of the hormone, which is caused by the effect on tissue renin-angiotensin systems. Enhances coronary and renal blood flow. With prolonged use reduces the severity of myocardial hypertrophy and the walls of resistive-type arteries. Improves blood supply to ischemic myocardium. Reduces platelet aggregation. Helps reduce the content of Na + in patients with heart failure. In large doses (500 mg / day) it exhibits angioprotective properties in relation to the vessels of the microvasculature and helps slow the progression of chronic renal failure in diabetic nephroangiopathy. A decrease in blood pressure, in contrast to direct vasodilators (hydralazine, minoxidil, etc.), is not accompanied by reflex tachycardia and leads to a decrease in myocardial oxygen demand. With heart failure in an adequate dose does not affect the amount of blood pressure. The maximum decrease in blood pressure after oral administration is observed after 60-90 minutes. The duration of the hypotensive effect is dose-dependent and reaches optimal values within a few weeks.
Pharmacokinetics
Absorption - fast, reaches 75% (food intake reduces by 30-40%), bioavailability - 35-40% (effect of "first passing" through the liver). Communication with plasma proteins (mainly with albumin) - 25-30%, the maximum concentration in the blood plasma (114 ng / ml) when taken orally - 30-90 minutes. Through the blood-brain barrier and the placental barrier penetrates poorly (less than 1%). Metabolized in the liver with the formation of disulfide dimer captopril and captopril-cysteine disulfide. Metabolites are pharmacologically inactive. The half-life is 3 hours. 95% is excreted by the kidneys (40-50% unchanged), the rest is in the form of metabolites. It is secreted with mother's milk. 4 hours after a single ingestion, the urine contains 38% unchanged captopril and 28% in the form of metabolites, after 6 hours - only as metabolites, in daily urine - 38% unchanged captopril and 62% - in the form of metabolites. The elimination half-life in case of impaired renal function is 3.5-32 hours. It accumulates in cases of chronic renal failure.
Indications
Arterial hypertension, incl. Renovascular, chronic heart failure (as part of complex therapy), left ventricular dysfunction after myocardial infarction with a clinically stable condition, diabetic nephropathy with diabetes mellitus type I (with albuminuria more than 30 mg / day).
Contraindications
Hypersensitivity to the drug and other ACE inhibitors, angioedema (with the use of ACE inhibitors, including a history), marked impaired renal or liver function, hyperkalemia, bilateral renal artery stenosis or arterial stenosis of the only kidney with progressive azotemia, post-transplant condition kidneys, stenosis of the mouth of the aorta, and similar changes that impede the outflow of blood, pregnancy, lactation, age up to 18 years.
Use during pregnancy and lactation
Contraindicated.
Dosage and administration
Captopril is prescribed orally for 1 hour before meals. Dosing regimen set individually.
Side effects
Since the cardiovascular system: tachycardia, lowering blood pressure, orthostatic hypotension, peripheral edema. From the nervous system: dizziness, headache, tired feeling, asthenia, paresthesia. On the part of the respiratory system: dry cough, pulmonary edema, bronchospasm. On the part of the urinary system: proteinuria, impaired renal function (increased levels of urea and creatinine in the blood).From the side of water-electrolyte metabolism: hyperkalemia, hyponatremia (most often with salt-free diet and simultaneous diuretic intake), proteinuria, elevated blood urea nitrogen, creatinine, acidosis. From the side of blood-forming organs: neutropenia, anemia, thrombocytopenia, agranulocytosis. Allergic reactions: angioedema, flushing of blood to the skin of the face, fever, skin rash (maculopapular, less often vesicular or bullous nature), pruritus, photosensitivity, bronchospasm, serum sickness, lymphadenopathy, in rare cases - the appearance of anti-nuclear antibodies in the blood. On the part of the gastrointestinal tract: a violation of taste, loss of appetite, stomatitis, dyspeptic symptoms, nausea, abdominal pain, constipation or diarrhea, increased activity of liver transaminases, hyperbilirubinemia, signs of hepatocellular damage (hepatitis) and cholestasis (in rare cases) , pancreatitis (in isolated cases). Other: general weakness, swelling of the legs.
Overdose
Symptoms: marked reduction in blood pressure, up to collapse, myocardial infarction, acute cerebrovascular accident, thromboembolic complications. Treatment: put the patient with raised lower limbs, measures aimed at restoring blood pressure (an increase in circulating blood volume, including a / v infusion of saline), symptomatic therapy. Perhaps the use of hemodialysis, peritoneal dialysis is ineffective.
Interaction with other drugs
Increases the concentration of digoxin in the blood plasma by 15-20%. Increases the bioavailability of propranolol. Cimetidine, slowing metabolism in the liver, increases the concentration of captopril in the blood plasma. The antihypertensive effect is weakened by NSAIDs, especially against the background of low concentrations of renin, and estrogens. The combination with thiazide diuretics, vasodilators (minoxidil), verapamil, beta-blockers, tricyclic antidepressants, ethanol enhances the hypotensive effect. Combined use with potassium-sparing diuretics, potassium preparations, cyclosporine, low salt milk (may contain K + up to 60 mmol / l), potassium supplements, salt substitutes (contain significant amounts of K +) increases the risk of hyperkalemia. Slows down the excretion of drugs lithium. Clonidine reduces the severity of the hypotensive effect.When prescribing captopril in the presence of allopurinol or procainamide, increases the risk of developing Stevens-Johnson syndrome and immunosuppressive action. The use of captopril in patients taking immunosuppressants (for example, azathioprine or cyclophosphamide) increases the risk of hematological disorders.
special instructions
Before starting, and regularly in the process of treatment with captopril, renal function should be monitored. In patients with chronic heart failure, it is used under close medical supervision. Against the background of long-term use of captopril, approximately 20% of patients have a stable increase in urea and serum creatinine by more than 20% compared with the norm or baseline value. Less than 5% of patients, especially in severe nephropathies, require discontinuation of treatment due to an increase in creatinine concentration. In patients with arterial hypertension, when captopril is used, severe hypotension is observed only in rare cases, the likelihood of developing this condition is increased when there is a shortage of fluid and salt loss (for example, after intensive diuretic therapy), in patients with heart failure or dialysis. In the case of the development of angioedema, the drug is canceled and thorough medical observation and symptomatic therapy are carried out. When taking captopril, a false-positive reaction may be observed when urine analyzes acetone. With caution prescribed to patients on a low-salt or salt-free diet (increased risk of arterial hypotension) and hyperkalemia.