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
ACE inhibitor. It is a prodrug, from which the active metabolite ramiprilate is formed in the body. It is believed that 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 is a potent vasoconstrictor. 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 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.
In patients with signs of chronic heart failure after myocardial infarction, ramipril reduces the risk of sudden death, the progression of heart failure to severe / resistant failure, and reduces the number of hospitalizations for heart failure.
It is known that ramipril significantly reduces the incidence of myocardial infarction, stroke, and cardiovascular death in patients with increased cardiovascular risk due to vascular disease (CHD, stroke or peripheral vascular disease) or diabetes mellitus, which have at least one additional risk factor (microalbuminuria , hypertension, increased total cholesterol, low HDL, smoking). Reduces the overall mortality and need for revascularization procedures, slows the onset and progression of chronic heart failure. As in patients with diabetes mellitus, and without it, ramipril significantly reduces the existing microalbuminuria and the risk of developing nephropathy. These effects are observed in patients with both elevated and normal BP.
The hypotensive effect of ramipril develops after about 1-2 hours, reaches a maximum within 3-6 hours, lasts at least 24 hours.
PHARMACOKINETICS
When ingested absorption is 50-60%, food does not affect the degree of absorption, but slows absorption. C max is achieved in 2-4 hours. In the liver it is metabolized to form an active metabolite of ramiprilate (6 times more active inhibits ACE than ramipril), inactive diketopiperazine and glucuronize. All metabolites formed, with the exception of ramiprilate, have no pharmacological activity. Binding to plasma proteins for ramipril - 73%, ramiprilata - 56%. Bioavailability after oral administration of 2.5-5 mg of ramipril - 15-28%; for ramiprilate - 45%. After a daily intake of ramipril at a dose of 5 mg / day, the steady concentration of ramiprilate in plasma is reached by day 4.
T 1/2 for ramipril - 5.1 hours; in the distribution and elimination phase, the drop in the concentration of ramiprilata in the blood serum occurs with T 1/2 - 3 hours, followed by a transition phase with T 1/2 - 15 hours, and a long final phase with very low plasma ramiprilate concentrations and T 1/2 - 4-5 days. T 1/2 increases with chronic renal failure. V d of ramipril - 90 liters, ramiprilata - 500 liters. The kidneys excrete 60%, through the intestines - 40% (mainly in the form of metabolites). If renal function is impaired, excretion of ramipril and its metabolites slows in proportion to the decrease in QC; when the liver function is impaired, the conversion into ramiprilat is slowed down; with heart failure, the concentration of ramiprilate increases 1.5-1.8 times.
INDICATIONS
Arterial hypertension; chronic heart failure; heart failure, developed in the first few days after an acute myocardial infarction; diabetic and nondiabetic nephropathy;reduction in the risk of myocardial infarction, stroke, and cardiovascular mortality in patients with high cardiovascular risk, including patients with confirmed coronary artery disease (with or without a history of heart attack), patients undergoing percutaneous transluminal coronary angioplasty, coronary artery bypass grafting, with stroke in history and patients with occlusive lesions of peripheral arteries.
DOSING MODE
Is taken internally. The initial dose is 1.25-2.5 mg 1-2 times / day. If necessary, a gradual increase in the dose is possible. The maintenance dose is set individually, depending on the indications for use and the effectiveness of the treatment.
SIDE EFFECT
From the side of the cardiovascular system: arterial hypotension; rarely - pain in the chest, tachycardia.
From the side of the central nervous system: dizziness, weakness, headache; rarely - sleep disorders, mood.
On the part of the digestive system: diarrhea, constipation, loss of appetite; rarely - stomatitis, abdominal pain, pancreatitis, cholestatic jaundice.
On the part of the respiratory system: dry cough, bronchitis, sinusitis.
From the urinary system: rarely - proteinuria, increasing the concentration of creatinine and urea in the blood (mainly in patients with impaired renal function).
From the hemopoietic system: rarely - neutropenia, agranulocytosis, thrombocytopenia, anemia.
On the part of laboratory indicators: hypokalemia, hyponatremia.
Allergic reactions: skin rash, angioedema and other hypersensitivity reactions.
Other: rarely - muscle spasms, impotence, alopecia.
CONTRAINDICATIONS
Severe renal and hepatic dysfunction, bilateral stenosis of the renal arteries or stenosis of the artery of a single kidney; condition after kidney transplantation; primary hyperaldosteronism, hyperkalemia, stenosis of the aortic aorta, pregnancy, lactation (breastfeeding), children and adolescents under 18 years of age, hypersensitivity to ramipril and other ACE inhibitors.
PREGNANCY AND LACTATION
Ramipril is contraindicated in pregnancy and lactation (breastfeeding).
APPLICATION FOR FUNCTIONS OF THE LIVER
Contraindicated in severe violations of kidney function, condition after kidney transplantation. In patients with concomitant renal dysfunction, doses are individually selected in accordance with the values ​​of CK. Before starting treatment, all patients need to conduct a study of kidney function.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Contraindicated in severe violations of liver function.
APPLICATION FOR CHILDREN
Contraindicated in children and adolescents under 18 years.
SPECIAL INSTRUCTIONS
In patients with concomitant renal dysfunction, doses are individually selected in accordance with the values ​​of CK. Before starting treatment, all patients need to conduct a study of kidney function. In the process of treatment with ramipril, kidney function, electrolyte blood composition, hepatic enzymes in the blood, and peripheral blood patterns are regularly monitored (especially in patients with diffuse connective tissue diseases, in patients receiving immunosuppressants, allopurinol). Patients who have a deficiency of fluid and / or sodium before treatment should be corrected water-electrolyte disorders. During treatment with ramipril, hemodialysis can not be performed using polyacrylonitrile membranes (the risk of anaphylactic reactions is increased).
DRUG INTERACTION
With the simultaneous use of potassium-sparing diuretics (including spironolactone, triamterene, amiloride), potassium preparations, salt substitutes and dietary supplements containing potassium, hyperkalaemia may develop (especially in patients with renal dysfunction), 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 with NSAIDs, it is possible to reduce the hypotensive effect of ramipril, impaired renal function.
When used simultaneously with "loop" or thiazide diuretics, the antihypertensive effect is enhanced. Severe arterial hypotension, especially after taking the first dose of a diuretic, appears to be due to hypovolemia, which leads to a transient increase in the hypotensive effect of ramipril. There is a risk of hypokalemia. Increased risk of impaired renal function.
With simultaneous use with drugs that have an antihypertensive effect, it is possible to intensify the hypotensive effect.
When used simultaneously with insulin, hypoglycemic agents, sulfonylurea derivatives, metformin, hypoglycemia may develop.
When used simultaneously with allopurinol, cystostatics, immunosuppressants, procainamide, an increased risk of developing leukopenia is possible.
With the simultaneous use of lithium carbonate, an increase in the concentration of lithium in the blood serum is possible.
TERMS AND CONDITIONS OF STORAGE
[MSK] 01.04 in the RK is not registered.
