Noliprel A coated pills 2.5 mg + 0.625 mg N30
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Active ingredients
Indapamide + Perindopril
Release form
Pills
Composition
Perindopril arginine 2.5 mg; which corresponds to the content of perindopril 1.6975 mg; indapamide 0.625 mg; excipients: lactose monohydrate - 74.455 mg, magnesium stearate - 450 μg, maltodextrin - 9 mg, silicon dioxide anhydrous colloidal dioxide - 270 μg, sodium carboxymethyl starch (type a) - 2.7 mg; the composition of the film shell: macrogol 6000 - 87 mcg, premix for the film shell of white color sepifilm 37781 rbc (glycerol - 4.5%, hypromellose - 74.8%, macrogol 6000 - 1.8%, magnesium stearate - 4.5%, titanium dioxide (e171) - 14.4% ) - 2.913 mg.
Pharmacological effect
Combined preparation containing perindopril arginine and indapamide. The pharmacological properties of the drug Noliprel A combine the individual properties of each of the components. Mechanism of action; Noliprel A; The combination of perindopril and indapamide enhances the antihypertensive effect of each of them.; Perindopril; Perindopril is an inhibitor of the enzyme that converts angiotensin I to angiotensin II (ACE inhibitor) . ACE, or kininase II, is exopeptidase, which carries out both the conversion of angiotensin I into a vasoconstrictor substance angiotensin II, and the destruction of bradykinin, which has a vasodilator, to an inactive heptapeptide. As a result, perindopril reduces the secretion of aldosterone; by the principle of negative feedback increases the activity of renin in the blood plasma; with long-term use reduces the OPSS, which is mainly due to the effect on the vessels in the muscles and kidneys. These effects are not accompanied by the retention of sodium ions and fluids or the development of reflex tachycardia.; Perindopril normalizes myocardial function, reducing preload and afterload.; When studying hemodynamic parameters in patients with chronic heart failure (CHF), a decrease in filling pressure in the left and right ventricles of the heart was found , decrease in OPSS, increase in cardiac output, increase in muscle peripheral blood flow.; Indapamide; Indapamide belongs to the sulfonamide group, according to its pharmacological properties Isocost to the thiazide diuretics. Indapamide inhibits the reabsorption of sodium ions in the cortical segment of the loop of Henle, which leads to an increase in kidney excretion of sodium ions, chlorine and to a lesser extent potassium and magnesium ions, thereby increasing diuresis and reducing blood pressure.; Antihypertensive effect; Noliprel A; Noliprel A has a dose-dependent antihypertensive action, both on diastolic and systolic blood pressure in both standing and lying.The antihypertensive effect persists for 24 hours. A stable therapeutic effect develops in less than 1 month from the start of therapy and is not accompanied by tachyphylaxis. Termination of treatment does not cause withdrawal.; Noliprel A reduces the degree of left ventricular hypertrophy (GTLZH), improves the elasticity of the arteries, reduces OPSS, does not affect lipid metabolism (total cholesterol, HDL cholesterol and LDL cholesterol, triglycerides); indapamide on GTLZH in comparison with enalapril. In patients with arterial hypertension and GTLV who received perindopril erbumin 2 mg (equivalent to 2.5 mg perindopril arginine) / indapamide 0.625 mg or enalapril at a dose of 10 mg 1 time / day, and with an increase in perindopril erbumine dose to 8 mg (equivalent to 10 mg perindopril arginine) and indapamide up to 2.5 mg, or enalapril up to 40 mg 1 time / day, there was a more significant decrease in the left ventricular mass index (LVMI) in the perindopril / indapamide group compared with the enalapril group. At the same time, the most significant effect on LVMI is observed when perindopril erbumine 8 mg / indapamide 2.5 mg is used. Also, a more pronounced antihypertensive effect was observed on the background of combined therapy with perindopril and indapamide compared with enalapril. In patients with diabetes type 2 (mean age 66 years, BMI 28 kg / m2, glycated hemoglobin (HbA1c) 7.5%, BP 145/81 mm Hg.) The effect of the fixed perindopril / indapamide combination on the main micro- and macrovascular complications was studied in addition to Drug therapy of glycemic control and intensive glycemic control (IHC) strategies (target HbA1c <6.5%); 83% of patients had arterial hypertension, 32% and 10% had macro- and microvascular complications, and 27% had microalbuminuria. The majority of patients at the time of inclusion in the study received hypoglycemic therapy, 90% of patients received hypoglycemic agents for oral administration (47% of patients - in monotherapy, 46% - therapy with two drugs, 7% - therapy with three drugs). 1% of patients received insulin therapy, 9% - only diet therapy.; Sulfonylurea derivatives were taken by 72% of patients, 61% by metformin. As a concomitant treatment, 75% of patients received antihypertensive drugs,35% of patients - hypolipidemic agents (mainly HMG-CoA reductase inhibitors (statins) - 28%), acetylsalicylic acid as an antiplatelet agent and other antiplatelet agents (47%) .; After 6 weeks of the introductory period, during which patients received perindopril / indapamide therapy, they were distributed to the standard glycemic control group or to the IHC group (Diabeton MB with the possibility of increasing the dose to a maximum of 120 mg / day or adding another hypoglycemic agent); In the IHC group (average Observation 4.8 years, mean HbA1c 6.5%) compared with the standard control group (average HbA1c 7.3%) showed a significant decrease of 10% in the relative risk of the combined frequency of macro- and microvascular complications. The advantage was achieved due to a significant reduction in the relative risk: microvascular complications by 14%, the occurrence and progression of nephropathy by 21%, microalbuminuria by 9%, macroalbuminuria by 30% and the development of kidney complications by 11%. The benefits of antihypertensive therapy did not depend on of properties achieved on the background of GCI.; Perindopril; Perindopril is effective in the treatment of hypertension of any severity.; The antihypertensive effect of the drug reaches a maximum after 4-6 hours after a single ingestion and persists for 24 hours (about 80%) residual inhibition of ACE.; Perindopril has an antihypertensive effect in patients with both low and normal renin activity in the blood plasma.; Simultaneous administration of thiazide diuretics by increasing There is a pronounced antihypertensive effect. In addition, the combination of an ACE inhibitor and a thiazide diuretic also reduces the risk of hypokalemia while taking diuretics.; Double blockade of the RAAS; There are data from clinical studies of combination therapy with the use of an ACE inhibitor with angiotensin II receptor; participation of patients with a history of cardiovascular or cerebrovascular disease, or diabetes mellitus type 2, accompanied by confirmed lesion of the target organ,and studies involving patients with type 2 diabetes mellitus and diabetic nephropathy. These studies did not reveal in patients receiving combination therapy a significant positive effect on the occurrence of renal and / or cardiovascular events and on mortality rates, while the risk of developing hyperkalemia , acute renal failure and / or hypotension increased compared with patients receiving monotherapy.; Taking into account similar intragroup pharmacodynamic ACE inhibitors and ARA II, these results can be expected for the interaction of any other drugs, representatives of the classes of ACE inhibitors and ARA II. Therefore, ACE inhibitors and ARA II should not be used simultaneously in patients with diabetic nephropathy. effects of adding aliskiren to standard therapy with an ACE inhibitor or ARA II in patients with type 2 diabetes mellitus and chronic kidney disease or cardiovascular disease, or with f of these diseases. The study was terminated early due to an increased risk of adverse outcomes. Cardiovascular death and stroke occurred more frequently in the group of patients receiving aliskiren compared with the placebo group. Also, adverse events and serious adverse events of particular interest (hyperkalemia, hypotension and renal dysfunction) were recorded more often in the aliskiren group than in the placebo group.; Indapamide; indapamide is associated with an improvement in the elastic properties of large arteries, a decrease in OPSS.; Indapamide reduces GTLV, does not affect the concentration of lipids in the blood plasma: t riglycerides, total cholesterol, LDL, HDL; carbohydrate metabolism (including in patients with concomitant diabetes).
Pharmacokinetics
The combination of perindopril and indapamide does not change their pharmacokinetic characteristics compared with the separate intake of these drugs.; Perindopril; Absorption and metabolism; After oral administration, perindopril is rapidly absorbed. Bioavailability is 65-70%.Approximately 20% of the total amount of absorbed perindopril is converted to the active metabolite of perindopril. Cmax of perindoprilat in blood plasma is reached after 3-4 hours. When taking the drug during a meal, the conversion of perindopril to perindoprilat decreases (this effect does not have significant clinical significance) .; Distribution and elimination; in blood plasma. The dissociation of perindoprilat associated with ACE is slowed down. As a result, the “effective” T1 / 2 is 25 hours. Reappointment of perindopril does not lead to its cumulation, and T1 / 2 of perindoprilat upon repeated administration corresponds to the period of its activity, thus, the equilibrium state is reached after 4 days; . T1 / 2 perindoprilat makes 3-5 hours; Pharmacokinetics in special clinical cases; Removal of perindoprilat slows down in elderly patients, as well as in patients with renal insufficiency and heart failure.; Perindoprilat clearance in dialysis is 70 ml / min; Pharmacokinetics Perindopril varies in patients with cirrhosis of the liver: hepatic clearance of perindopril is reduced by 2 times. However, the amount of perindoprilat formed does not change, so dose adjustment is not required.; Perindopril crosses the placental barrier.; Indapamide; Absorption; Indapamide is rapidly and completely absorbed from the gastrointestinal tract. Cmax in blood plasma is achieved after 1 h after ingestion.; Distribution; Binding to plasma proteins - 79%; Repeated administration of the drug does not lead to its cumulation in the body.; Elimination; T1 / 2 is 14-24 h (average 19 h. Excreted mainly by the kidneys (70% of the administered dose) and through the intestine (22%) in the form of inactive metabolites.; Pharmacokinetics in special clinical cases; Pharmacokinetics of indapamide does not change in patients with renal insufficiency.
Indications
- essential hypertension ;; - in patients with arterial hypertension and type 2 diabetes to reduce the risk of microvascular complications (from the kidneys) and macrovascular complications from cardiovascular diseases.
Contraindications
- hypersensitivity to perindopril and other ACE inhibitors, to indapamide and other sulfonamides, as well as to other auxiliary components of the drug ;; - angioedema in the history (including while taking other ACE inhibitors) (seesection "Special instructions") ;; - hereditary / idiopathic angioedema ;; - severe renal failure (CC <30 ml / min) ;; - hypokalemia ;; - bilateral renal artery stenosis or the presence of one functioning kidney ;; - severe hepatic failure (including with encephalopathy) ;; - simultaneous use of drugs that extend the QT interval ;; - simultaneous use with antiarrhythmic drugs that can cause arrhythmia like pirouette (see the section "Drug Interactions") ;; - simultaneous use with aliskiren containing reparations in patients with diabetes mellitus or impaired renal function (GFR less than 60 ml / min / 1.73 m2 of body surface area) (see the sections "Pharmacological action" and "Drug interaction") ;; - pregnancy ;; - breastfeeding period ;; - age up to 18 years (efficacy and safety have not been established) ;; - presence of lactase deficiency, galactosemia or glucose-galactose malabsorption syndrome (the preparation contains lactose) .; Due to the lack of sufficient clinical experience, Noliprel A should not be used in patients with untreated oh decompensated heart failure and in patients on hemodialysis;. The caution (see. sections "Special Instructions" and "Drug Interactions") should be prescribed a drug for systemic diseases of the connective tissue (including systemic lupus erythematosus, scleroderma), therapy with immunosuppressants (risk of developing neutropenia, agranulocytosis), therapy with lithium preparations, bone marrow inhibition, reduced bcc (diuretic intake, salt-free diet, vomiting, diarrhea, hemodialysis), angina pectoris, cerebrovascular diseases, renovascular hypertension, diabetes mellitus, chronic heart failure (IV To the NYHA classification), liver failure, hyperuricemia (especially accompanied urate gout and nephrolithiasis), lability AD; conducting hemodialysis using high-flow membranes, desensitization, before the procedure of LDL apheresis; in condition after kidney transplantation; aortic valve stenosis / hypertrophic obstructive cardiomyopathy; under anesthesia; atherosclerosis; as well as elderly patients; Negroid patients (less pronounced effect of the application); athletes (possible positive reaction with doping control).
Dosage and administration
Assign inside, preferably in the morning, before meals.; In essential hypertension, 1 tab.drug Noliprel A 1 time / day. If possible, the drug start with the selection of doses of single-component drugs. In the case of clinical need, you can consider the possibility of prescribing combination therapy with Noliprel A immediately after monotherapy.; Patients with hypertension and type 2 diabetes to reduce the risk of developing microvascular complications (from the kidneys) and macrovascular complications from cardiovascular diseases, 1 tab . Noliprel A 1 time / day. After 3 months of therapy, subject to good tolerability, it is possible to increase the dose to 2 tab. Noliprel A 1 time / day (or 1 tab. Noliprel A forte 1 time / day); Elderly patients should begin therapy after monitoring kidney function and blood pressure.; The drug is contraindicated in patients with severe renal failure (CC <30 ml / min ). For patients with moderately severe renal insufficiency (CK 30-60 ml / min), it is recommended to begin therapy with the necessary doses of drugs (as monotherapy) that are part of Noliprel A. Patients with CC> 60 ml / min do not need dose adjustment. The therapy requires regular monitoring of creatinine and potassium in the blood plasma.; The drug is contraindicated in patients with severe liver failure. With moderately severe liver failure, dose adjustment is not required.; Noliprel A should not be given to children and adolescents under the age of 18 years because of the lack of data on the efficacy and safety of using the drug in patients of this age group.