Ramipril is rapidly absorbed in the gastrointestinal tract and is hydrolyzed in the liver to form the active metabolite ramiprilat. Ramiprilat durabolin injection side effects is a long-acting ACE inhibitor -. An enzyme catalyzing the conversion of angiotensin I into angiotensin II
Ramipril causes a decrease in angiotensin II in plasma renin activity increase and decrease in aldosterone release.
Suppresses kininase II level, prevents the breakdown of bradykinin, it enhances the synthesis of prostaglandins. Under the effect of ramipril expanding peripheral vessels and decreasing total peripheral vascular resistance (SVR). Hypertension has a hypotensive effect in the position of the patient “lying” and “standing”. Reduces peripheral vascular resistance (afterload), wedge pressure in the pulmonary capillaries without a compensatory increase in heart rate ( hR). Enhances coronary and renal blood flow without affecting glomerular filtration rate. Getting the hypotensive effect in 1-2 hours after oral administration, the maximum effect develops within 3-6 hours after ingestion. Action is maintained for at least 24 hours. Chronic heart failure and heart failure due to acute myocardial infarction Ramipril reduces peripheral vascular resistance and, ultimately, the blood pressure. It increases cardiac output and exercise tolerance. With prolonged use promotes regression of myocardial hypertrophy in patients with heart failure I and II class NYHA functional classification, improve blood flow to ischemic myocardium. Ramipril improves survival in patients with symptoms of transient or chronic heart failure after myocardial infarction. It has a cardioprotective effect, prevents coronary ischemic episodes, reduces the likelihood of myocardial infarction and reduces the duration of hospitalization. Diabetic and nondiabetic nephropathy in patients with diabetic and non-diabetic nephropathy, durabolin injection side effects ramipril slows the rate of progression of renal failure and the onset of end-stage renal failure and, thereby, reduces the the need for hemodialysis or kidney transplantation. In the initial stages of diabetic and nondiabetic nephropathy ramipril reduces the severity of proteinuria. Patients with high risk of cardiovascular disease due to vascular lesions (diagnosed coronary heart disease (CHD), obliterative peripheral arterial disease or a stroke disorder), diabetes with at least one additional risk factor (microalbuminuria, hypertension, elevated plasma concentrations of total cholesterol (TC), a decrease of plasma high density lipoprotein cholesterol concentration (HDL-C), smoking) joining ramipril to standard therapy significantly reduces the incidence of myocardial infarction, stroke and death from cardiovascular -sosudistyh reasons. Pharmacokinetics Ramipril is rapidly absorbed in the gastrointestinal tract after ingestion. The absorption is independent of food intake. After absorption ramipril is rapidly and almost completely converted to the active metabolite ramiprilat by the enzyme liver esterase. Ramiprilat about 6 times stronger inhibits ACE than ramipril. Other pharmacologically inactive metabolites are also found. In patients with impaired renal function the transformation of ramipril into ramiprilat is slowed down due to the relatively short period of esterase, so the level of ramipril plasma from these patients increased. The maximum concentration of ramipril plasma levels achieved within one hour after administration, ramiprilata -. for 2-4 hours after taking the drug bioavailability of ramipril is 60%. Communication to plasma proteins up to 73% for ramipril and 56% for ramiprilat. Upon receiving 5 mg ramipril renal clearance of 10-55 ml / min, extrarenal clearance reaches 750 ml / min. For ramiprilat these figures are 70-120 ml / min and 140 ml / min, respectively. Ramipril and ramiprilat is mainly excreted by the kidneys (40-60%). In case of violation of renal excretion is slowing. The half-life period ramiprilata long-term use in a dose of 5-10 mg once per day is 13-17 hours.
• chronic heart failure (in combination therapy);
• diabetic or non-diabetic nephropathy, preclinical and symptomatic stage, including those with severe proteinuria, especially when combined with hypertension and the presence of microalbuminuria;
• reduction of infarct risk infarction, stroke or cardiovascular death in patients at high risk of cardiovascular disease:
– in patients with documented coronary artery disease, myocardial infarction with or without including patients undergoing percutaneous transluminal coronary angioplasty, coronary artery bypass grafting;
– in patients with stroke history;
– in patients with peripheral arterial occlusive disease;
– in patients with diabetes mellitus with at least one additional risk factor durabolin injection side effects (microalbuminuria, hypertension, elevated plasma concentrations of OX, reduced plasma concentrations of HDL-C, smoking);
• heart failure which has developed during the first few days (from day 2 to 9) after an acute myocardial infarction.
• Hypersensitivity to ramipril, other ACE inhibitors or auxiliary components of the drug;
• hereditary angioedema or idiopathic angioedema (including appointment of ACE inhibitors in history);
• hemodynamically significant renal artery stenosis (bilateral or unilateral in the case of a solitary kidney) ;
• cardiogenic shock;
• primary hyperaldosteronism;
• severe hypotension (systolic blood pressure less than 90 mmHg..) or a condition with unstable hemodynamics;
• the age of 18 years (effectiveness and safety have not been studied);
• severe renal impairment (creatinine clearance (CC) of less than 20 mL / min / 1.73 m²);
• severe hepatic insufficiency (no clinical experience);
• hemodialysis or hemofiltration with certain membrane with negatively charged surface (vysokoprotochnyh membrane of polyacrylonitrile (risk of hypersensitivity reactions);
• apheresis LDL with dextran sulfate (risk of hypersensitivity reactions);
• the use in the acute phase of myocardial infarction: severe chronic heart failure (CHF) (IV NYHA functional class classification ), unstable angina, life-threatening ventricular disorders, “pulmonary” heart rhythm heart;
• as in the case with other ACE inhibitors, is contraindicated concomitant use of ramipril and products containing aliskiren in patients with diabetes mellitus or moderate to severe renal insufficiency ( CC less than 60 ml / min / 1.73 m²);
• concurrent use with angiotensin II receptor antagonists in patients with diabetic nephropathy;
• nephropathy, treatment which is conducted corticosteroids, non-steroidal anti-inflammatory drugs (NSAIDs), immunomodulators and / or other cytotoxic drugs ( clinical experience is insufficient);
• hemodynamically significant aortic or mitral stenosis (risk of excessive reduction of blood pressure followed durabolin injection side effects by impaired renal function (creatinine clearance 20 mL / min / 1.73 m²)), hypertrophic obstructive cardiomyopathy.
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