Masteron steroids – selective non-peptidic renin inhibitor structure having marked activity. Kidney renin secretion and activation of the renin-angiotensin-aldosterone system occurs with a decrease in blood volume and renal blood flow through a feedback mechanism. Renin acts on angiotensinogen to form the inactive decapeptide – angiotensin 1 , via which the angiotensin converting enzyme and partly without its participation is converted into the active octapeptide angiotensin. It is a potent vasoconstrictor stimulates the release of catecholamines from the adrenal medulla and presynaptic nerve terminals and enhances the secretion of aldosterone and sodium reabsorption, which ultimately leads to increased blood pressure.
Long-term increase in the concentration stimulates the production of mediators of inflammation and fibrosis, leading to end-organ damage.
When the plasma concentrations observed decrease renin secretion by the mechanism of negative feedback.
All drugs inhibiting (including renin inhibitors) inhibit the negative feedback, causing a compensatory increase renin concentration in blood plasma, the treatment with inhibitors and and antagonists of angiotensin leads to an increase in plasma renin activity, but in the treatment of aliskiren negative feedback effects are neutralized, resulting in plasma renin activity (hypertensive patients by an average of 50-80%), aT I and is reduced as aliskiren monotherapy or when combined with other antihypertensive agents . Increased renin plasma activity is directly related to an increased risk of cardiovascular disease in patients with normal blood pressure and patients with arterial hypertension (.
In patients with hypertension drug Rasilez when used at a dose of 150 or 300 mg 1 time a day marked dose-dependent prolonged decline in both systolic and diastolic blood pressure within 24 hours, including the early morning hours. The ratio of the residual effect of the drug to the maximum or target for diastolic blood pressure is 98%. After 2 weeks of regular ingestion is marked reduction of blood pressure to a maximum of 8590%, the hypotensive effect is maintained at the level reached in the course of long-term (up to 1 year) use. After stopping treatment with Rasilez observed a gradual return of blood pressure to baseline levels within a few weeks, without the development of the syndrome of “cancellation” and increase renin plasma activity.
After 4 weeks from the date of withdrawal of the drug Rasilez blood pressure is significantly lower in comparison with placebo.
Using the drug for the first time is not observed hypotensive response (the effect of “first dose”) and a reflex increase in heart rate (HR) in response to vasodilation.
Rasnleza When applied in monotherapy or in masteron steroids combination with other antihypertensive agents excessive blood pressure reduction observed in 0.1% and 1%, respectively.
Monotherapy Rasnlezom with concomitant diabetes mellitus can achieve efficient and safe lowering of blood pressure. In patients with diabetes mellitus concomitant use Rasilez preparation in combination with ramipril results in a greater reduction in blood pressure compared to that of monotherapy to each drug separately.
In patients with hypertension, obesity, and poor control of blood pressure hydrochlorothiazide monotherapy additional use of the drug Rasilez lowers blood pressure, comparable to hydrochlorothiazide combination with irbesartan or amlodipine.
Antihypertensive effect of the drug does not depend on age, sex, race, and body mass index.
In patients with existing (or history), hypertension and compensated chronic heart failure , a stable flow, receiving standard therapy in connection with chronic heart failure ( inhibitors or angiotensin II of, beta-blockers and one third of patients – aldosterone antagonists), the inclusion of a standard Rasilez drug therapy at a dose of 150 mg / day. well tolerated. The level of brain natrnyureticheskogo peptide is reduced by 25% in the group of patients receiving Rasilez compared with the placebo group.
In patients with hypertension, type 2 diabetes and nephropathy treated with losartan in a dosage of 100 mg and optimized antihypertensive concomitant therapy, addition drug at a dose of 300 mg / day. leads to clinically significant reduction ratio kreatnnin-albumin in the urine by 20% in comparison with placebo, i.e. with 58 mg / mmol to 46 mg / mmol. The percentage of patients with a reduction ratio of albumin in the urine creatinine of at least 50% from baseline is 24.7% and 12.5% in masteron steroids the placebo group and respectively Rasileza. linda durbesson before and after