Cardosal: instructions for use, analogues, price and reviews from doctors

Compound

One tablet of Cardosal 40 contains 40 mg of medoxomil olmesartan.
One tablet of Cardosal 20 contains 20 mg of medoxomil olmesartan.

One tablet of Cardosal 10 contains 10 mg of medoxomil olmesartan.

Additional substances: hyprolose, microcrystalline cellulose, lactose monohydrate, magnesium stearate.

Shell composition: hypromellose, talc, titanium dioxide.

Cardosal® 40

Olmesartan medoxomil, the active substance of the drug Cardosal 40, is a powerful specific antagonist of angiotensin II receptors (type AT1).

Angiotensin II is the primary vasoactive hormone of the renin-angiotensin-aldosterone system and plays a significant role in the pathophysiology of arterial hypertension by acting on AT1 receptors. It is assumed that olmesartan medoxomil blocks all AT1 receptor-mediated actions of angiotensin II, regardless of the source and route of angiotensin II synthesis. The specific antagonism of olmesartan medoxomil towards angiotensin II receptors (AT1 type) leads to an increase in the activity of renin, angiotensin I and II in the blood plasma, and also helps to reduce the plasma concentration of aldosterone.

In arterial hypertension, olmesartan medoxomil causes a dose-dependent, prolonged decrease in blood pressure (BP). There is no data on the development of arterial hypotension after taking the first dose of the drug, tachyphylaxis during long-term treatment or withdrawal syndrome (a sharp increase in blood pressure after discontinuation of the drug).

Taking olmesartan medoxomil once a day provides an effective and uniform reduction in blood pressure over 24 hours, and the effect after a single dose is similar to the effect of taking the drug 2 times a day at the same daily dose.

The antihypertensive effect of olmesartan medoxomil usually develops within 2 weeks, and the maximum effect develops approximately 8 weeks after the start of therapy.

The effect of olmesartan medoxomil on mortality and complication rates has not been established.

The ROADMAP trial, a randomized trial of 4447 patients with type 2 diabetes mellitus, normoalbuminuria, and at least one additional cardiovascular risk factor, assessed the ability of olmesartan medoxomil to prolong the time to onset of microalbuminuria. During the study period (median follow-up of 3.2 years), patients received olmesartan medoxomil or placebo in addition to other antihypertensive agents other than angiotensin-converting enzyme (ACE) inhibitors or other angiotensin II receptor antagonists.

The study demonstrated a significant reduction in the risk of the primary endpoint (time to onset of microalbuminuria) in favor of olmesartan medoxomil. After adjusting for differences in BP using double-blind prespecified parameters, the risk reduction was 17% (relative risk (RR) 0.834; 95% confidence interval (CI): 0.681 to 1.021; p = 0.0789) for systolic BP (SBP) adjusted for area under the curve (AUC) and 18% (RR 0.823; 95% CI: 0.672 - 1.008; p = 0.0596) for diastolic blood pressure (DBP) adjusted for AUC in favor of olmesartan medoxomil. Microalbuminuria developed in 8.2% of patients in the olmesartan medoxomil group (178 of 2160 patients) and 9.8% in the placebo group (210 of 2139 patients).

Cardiovascular events (secondary endpoints) were reported in 96 patients (4.3%) receiving olmesartan medoxomil and in 94 patients (4.2%) receiving placebo. Cardiovascular mortality was higher in the olmesartan medoxomil group compared with the placebo group (15 (0.7%) and 3 (0.1%) patients, respectively). At the same time, in the olmesartan medocomil group and the placebo group, a similar incidence of non-fatal stroke was observed (in 14 (0.6%) and 8 (0.4%) patients, respectively), non-fatal myocardial infarction (in 17 (0.8%) and 26 (1.2%) patients, respectively) and mortality from non-cardiovascular causes (in 11 (0.5%) and 12 (0.5%) patients, respectively). Overall mortality was numerically higher in the olmesartan medoxomil group than in the placebo group (in 26 (1.2%) and 15 (0.7%) patients, respectively), which was mainly due to a higher number of fatal cardiovascular events.

The randomized ORIENT trial, conducted in Japan and China, examined the effects of olmesartan medoxomil on renal and cardiovascular outcomes in 577 patients with type 2 diabetes mellitus and advanced nephropathy. During the study (median follow-up of 3.1 years), patients received olmesartan medoxomil or placebo in addition to other antihypertensive drugs, including ACE inhibitors.

The composite cardiovascular endpoint included: death from cardiovascular causes in 10 (3.5%) patients in the olmesartan medoxomil group and in 3 (1.1%) patients in the placebo group); total mortality (19 (6.7%) cases in the olmesartan medoxomil group and 20 (7.0%) cases in the placebo group), non-fatal stroke (8 (2.8%) cases in the olmesartan medoxomil group and 11 (3.9 %) cases in the placebo group), non-fatal myocardial infarction (3 (1.1%) cases in the olmesartan medoxomil group and 7 (2.5%) cases in the placebo group).

Children and teenagers

The antihypertensive effect of olmesartan medoxomil in children and adolescents was analyzed in a randomized, double-blind, placebo-controlled study involving 302 patients aged 6 to 17 years. The study group consisted of black patients (112 people) and a racially mixed group (190 patients, 38 of whom were black). The etiology of arterial hypertension was predominantly primary (87% of the group consisting of patients of the Negroid race and 67% of the “mixed” group).

Patients weighing 20 to <35 kg were randomized to receive olmesartan medoxomil 2.5 mg (low dose) or 20 mg (high dose) once daily, and patients weighing ≥35 kg were randomized into groups receiving olmesartan medoxomil at doses of 5 mg (low dose) or 40 mg (high dose) once daily. At a dose adjusted according to body weight, olmesartan medoxomil significantly reduced both systolic and diastolic blood pressure. At both low and high doses of olmesartan, medoxomil significantly reduced systolic blood pressure by 6.6 and 11.9 mmHg, respectively. Art. (from the initial level). This effect was also observed during the 2-week randomized withdrawal phase, with both mean systolic and diastolic blood pressure showing statistically significant increases in the placebo group compared with the olmesartan medoxomil group. In children and adolescents, treatment was effective for both primary and secondary arterial hypertension. As in adult patients, blood pressure in black patients decreased to a lesser extent.

In the same study, 59 patients aged 1 to 5 years weighing ≥ 5 kg received 0.3 mg/kg olmesartan medoxomil once daily for three weeks in the open-label phase of the study and were then randomized in the double-blind phase of the study. into groups receiving either olmesartan medoxomil or placebo. At the end of the 2-week withdrawal phase, the mean systolic/diastolic blood pressure at the nadir was 3/3 mm Hg. Art. lower in the olmesartan medoxomil group; this difference in blood pressure was not statistically significant (95% CI: 2-7/1-7).

Pharmacodynamics and pharmacokinetics

Pharmacodynamics

An angiotensin type 2 receptor blocker , which is a hormone and plays a major role in the development of arterial hypertension .

Olmesartan presumably inhibits the effects of angiotensin II type by blocking the corresponding receptors.

In arterial hypertension it causes a dose-dependent long-term decrease in pressure. There is no evidence of the occurrence of arterial hypotension, tachycardia (during long-term treatment) or withdrawal syndrome after taking the drug.

Taking olmesartan once a day provides a gentle and effective reduction in blood pressure throughout the day. The hypotensive effect develops after two weeks, and the greatest effect occurs approximately two months after the start of treatment.

Pharmacokinetics

The active substance is a prodrug. In the mucous membrane of the digestive tract, under the action of enzymes , it quickly turns into an active metabolite . Olmesartan medoxomil the blood in its original form . Bioavailability is approximately 25.6%. The highest concentration in the blood is achieved on average two hours after oral administration. Food intake does not affect bioavailability.

Binds to plasma proteins by 99.7%. The connection with blood cells is weak. 40% of the drug is excreted by the kidneys, another 60% - with bile. The half-life is 11-14 hours.

Cardosal® 20

Olmesartan medoxomil, the active ingredient of Cardosal® 20, is a potent specific antagonist of angiotensin II receptors (type AT1).

The antihypertensive effect of olmesartan medoxomil usually develops within 2 weeks, and the maximum effect develops approximately 8 weeks after the start of therapy.

The effect of olmesartan medoxomil on mortality and complication rates has not been established.

The ROADMAP trial, a randomized trial of 4447 patients with type 2 diabetes mellitus, normoalbuinuria, and at least one additional cardiovascular risk factor, assessed the ability of olmesartan medoxomil to prolong the time to onset of microalbuminuria.

During the study period (median follow-up of 3.2 years), patients received olmesartan medoxomil or placebo in addition to other antihypertensive agents other than angiotensin-converting enzyme (ACE) inhibitors or other angiotensin II receptor antagonists.

The study demonstrated a significant reduction in the risk of the primary endpoint (time to onset of microalbuminuria) in favor of olmesartan medoxomil. After adjustment for differences in BP using prespecified parameters for double-blind design, the risk reduction was 17% (relative risk (RR) 0.8 [34; 95% confidence interval (CI): 0.681 - 1.021; p = 0.0789 ) for systolic blood pressure (SBP) adjusted for area under the curve (AUC) and 18% (RR 0.823; 95% CI: 0.672 - 1.008; p = 0.0596) for diastolic blood pressure (DBP) adjusted for AUC in the benefits of olmesartan medoxomil. Microalbuminuria developed in 8.2% of patients in the olmesartan medoxomil group (178 of 2160 patients) and 9.8% in the placebo group (210 of 2139 patients).

The primary composite endpoint (time to first event: doubling of plasma creatinine concentration, development of end-stage chronic kidney disease, death from all causes) was recorded in 116 patients in the olmesartan medoxomil group (41.1%) and in 129 patients in the placebo group (45.4%) (RR 0.97; 95% CI: 0.75-1.24; p = 0.791). The secondary composite cardiovascular endpoint was recorded in 40 patients in the olmesartan medoxomil group (14.2%) and in 53 patients in the placebo group (18.7%). The composite cardiovascular endpoint included: death from cardiovascular causes in 10 (3.5%) patients in the olmesartan medoxomil group and in 3 (1.1%) patients in the placebo group; total mortality (19 (6.7%) cases in the olmesartan medoxomil group and 20 (7.0%) cases in the placebo group), non-fatal stroke (8 (2.8%) cases in the olmesartan medoxomil group and 11 (3.9 %) cases in the placebo group), non-fatal myocardial infarction (3 (1.1%) cases in the olmesartan medoxomil group and 7 (2.5%) cases in the placebo group).

Children and teenagers

Patients weighing 20 to <35 kg were randomized to receive olmesartan medoxomil 2.5 mg (low dose) or mg (high dose) once daily, and patients weighing ≥ 35 kg were randomized to receive olmesartan medoxomil 2.5 mg (low dose) or mg (high dose) once daily. groups receiving olmesartan medoxomil at doses of 5 mg (low dose) or 40 mg (high dose) once daily. At a dose adjusted according to body weight, olmesartan medoxomil significantly reduced both systolic and diastolic blood pressure. At both low and high doses of olmesartan, medoxomil significantly reduced systolic blood pressure by 6.6 and 11.9 mmHg, respectively. Art. (from the initial level). This effect was also observed during the 2-week randomized withdrawal phase, with both mean systolic and diastolic blood pressure showing statistically significant increases in the placebo group compared with the olmesartan medoxomil group. In children and adolescents, treatment was effective for both primary and secondary arterial hypertension. As in adult patients, blood pressure in black patients decreased to a lesser extent.

Contraindications

Renal failure , a condition after a kidney transplant.
Obstruction of the biliary tract.
Lactase deficiency , malabsorption or galactosemia.
Age less than 18 years.
Pregnancy and lactation .
Hypersensitivity to the components of the drug.

It is recommended to use the drug with caution in the following diseases and conditions:

obstructive hypertrophic cardiomyopathy;
heart valve stenosis
primary aldosteronism;
mild renal failure
hyperkalemia or hyponatremia;
chronic cardiac failure;
cardiac ischemia;
bilateral renal artery stenosis
cerebrovascular disorders;
decreased volume of circulating fluid due to diet , vomiting or diarrhea;
liver dysfunction;
elderly age;
combined use with diuretics.

Side effects

Hematopoietic reactions: thrombocytopenia.
Reactions from nervous activity: dizziness , headache .
Reactions from breathing: cough, rhinitis, pharyngitis, bronchitis.
Digestive reactions: nausea, diarrhea, dyspepsia , abdominal pain, gastroenteritis , vomiting.
Skin reactions: itching , skin rash, allergic dermatitis, Quincke's edema, urticaria.
Reactions from the musculoskeletal system: pain in bones and joints, arthritis, back pain, cramps .
Reactions from the genitourinary tract: genitourinary tract infections, hematuria, acute renal failure.
Reactions from laboratory tests: increased levels of urea and creatinine in the blood, increased levels of liver enzymes.
Circulatory reactions: tachycardia, angina , decreased blood pressure.
Metabolic reactions: increased creatine phosphokinase levels, hyperuricemia, hypertriglyceridemia, hyperkalemia.
General reactions: flu-like symptoms, chest pain, asthenia , peripheral edema, malaise, fatigue, drowsiness .

Instructions for use of Cardosal (Method and dosage)

Instructions for use of Cardosal prescribe taking the drug orally every day at the same time, once a day.

The recommended initial dose is 10 mg once daily. If the blood pressure reduction is not sufficient when taking 10 mg per day, it can be increased to 20 mg per day. If additional pressure reduction is required, the dosage is increased to a maximum of 40 mg per day or a diuretic (for example, hydrochlorothiazide ).

The highest daily dose is 40 mg.

Cardosal® 10

Olmesartan medoxomil, the active ingredient of Cardosal® 10, is a potent specific antagonist of angiotensin II receptors (type AT1).

Angiotensin II is the primary vasoactive hormone of the renin-angiotensin-aldosterone system and plays a significant role in the pathophysiology of arterial hypertension by acting on AT1 receptors. Olmesartan medoxomil is expected to block all AT1 receptor-mediated actions of angiotensin II, regardless of the source and route of angiotensin II synthesis. The specific antagonism of olmesartan medoxomil towards angiotensin II receptors (AT1 type) leads to an increase in the activity of renin, angiotensin I and II in the blood plasma, and also helps to reduce the plasma concentration of aldosterone.

The antihypertensive effect of olmesartan medoxomil usually develops within 2 weeks, and the maximum effect develops approximately 8 weeks after the start of therapy.

The effect of olmesartan medoxomil on mortality and complication rates has not been established. The ROADMAP trial, a randomized trial of 4447 patients with type 2 diabetes mellitus, normoalbuminuria, and at least one additional cardiovascular risk factor, assessed the ability of olmesartan medoxomil to prolong the time to onset of microalbuminuria. During the study period (median follow-up of 3.2 years), patients received olmesartan medoxomil or placebo in addition to other antihypertensive agents other than angiotensin-converting enzyme (ACE) inhibitors or other angiotensin II receptor antagonists.

The secondary composite cardiovascular endpoint was recorded in 40 patients in the olmesartan medoxomil group (14.2%) and in 53 patients in the placebo group (18.7%).

The composite cardiovascular endpoint included: death from cardiovascular causes in 10 (3.5%) patients in the olmesartan medoxomil group and in 3 (1.1%) patients in the placebo group; total mortality (19 (6.7%) cases in the olmesartan medoxomil group and 20 (7.0%) cases in the placebo group), non-fatal stroke (8 (2.8%) cases in the olmesartan medoxomil group and 11 (3.9 %) cases in the placebo group), non-fatal myocardial infarction (3 (1.1%) cases in the olmesartan medoxomil group and 7 (2.5%) cases in the placebo group).

Children and teenagers

In children and adolescents, treatment was effective for both primary and secondary arterial hypertension. As in adult patients, blood pressure in black patients decreased to a lesser extent.

Interaction

Concomitant use with potassium supplements, potassium-sparing diuretics or other drugs that can increase potassium in the blood is not recommended.

The antihypertensive effect of treatment with olmesartan is enhanced when used in combination with other antihypertensive drugs.

Nonsteroidal anti-inflammatory drugs, cyclooxygenase type 2 inhibitors, and angiotensin type 2 receptor blockers may interact synergistically to inhibit glomerular filtration. In this case, there is a possibility of acute renal failure . To avoid such phenomena, it is recommended to monitor kidney function at the beginning of therapy, as well as timely intake of a sufficient volume of fluid.

When used together with antacids , a moderate decrease in the bioavailability of olmesartan is possible.

The use of olmesartan together with lithium preparations is dangerous due to an increase in the concentration of the latter in the blood.

Interactions of the drug Cardosal

When used with other antihypertensive drugs, the effect of olmesartan medoxomil may be enhanced. When olmesartan medoxomil is used simultaneously with NSAIDs, its antihypertensive effect may be reduced and there may be a risk of acute renal failure. After therapy with antacids (magnesium-aluminum hydroxide), a decrease in the bioavailability of olmesartan medoxomil was noted. The combined use of warfarin and digoxin does not change the pharmacokinetics of olmesartan. It is not recommended to use olmesartan medoxomil with lithium preparations due to the increased toxicity of the latter. Due to the possibility of developing hyperkalemia, it is not recommended to use olmesartan medoxomil with potassium-sparing diuretics, drugs containing potassium, or with other drugs that can lead to an increase in serum potassium levels (for example, heparin). When using olmesartan medoxomil with pravastatin, no clinically significant interactions were observed. The interactions of olmesartan medoxomil with drugs that are metabolized by the cytochrome P450 enzyme have not been determined.

special instructions

When using the drug in people with impaired renal function, it is recommended to regularly monitor potassium and creatinine in the blood.

It should be remembered that an excessive decrease in pressure in patients with coronary artery disease or cerebrovascular changes can cause heart attack or stroke .

When driving a vehicle during treatment with this drug, you should be careful.

Cardosal's analogs

Level 4 ATC code matches:
Telmisartan

Irbesartan

Presartan

Nortivan

Candesartan

Kozaar

Aprovel

Teveten

Blocktran

Valsartan

Losartan

Atakand

Diovan

Valsacor

Mikardis

Vazar

Valz

Lorista

Lozap

Complete analogues of Cardosal: Olimestra, Olmesar.

Cardosal price, where to buy

In Russia, the price of Cardosal 10 No. 28 is 460-570 rubles, the price of Cardosal 20 No. 28 is 505-660 rubles, and Cardosal 40 with the same number is 670-715 rubles.

In Ukraine, prices for the drug in the same release forms are close to 248, 328 and 374 hryvnia, respectively.

Online pharmacies in RussiaRussia
Online pharmacies in UkraineUkraine

ZdravCity

Cardosal tablets p.p.o.
10 mg 28 pcs. Daichi Sankyo Europe GmbH RUR 590 order
Cardosal tablets p.p.o. 40 mg 28 pcs. Daichi Sankyo Europe GmbH
RUB 831 order
Cardosal Plus tablets p.p.o. 12.5 mg+20 mg 28 pcs. Daichi Sankyo Europe GmbH
RUR 792 order
Cardosal tablets p.p.o. 20 mg 28 pcs. Daichi Sankyo Europe GmbH
RUR 759 order
Read also: How to normalize eye pressure for an adult?

Pharmacy Dialogue

Cardosal (tab.p/vol.10mg No. 28)Berlin-Chemie AG/Menarini
RUR 583 order
Cardosal (tablet p/o 20 mg No. 28)Berlin-Chemie AG/Menarini
RUR 734 order
Cardosal plus (tab. p.pl/vol. 12.5 mg + 20 mg No. 28) Daiichi Sankyo
RUR 771 order
Cardosal (tab.p/vol.40mg No. 28)Berlin-Chemie AG/Menarini
RUB 823 order

Pharmacy24

Cardosal plus 20/12.5 No. 28 tablets Daichie Sankio Europe GmbH/Berlin Chemie AG (Menarini Group), Nimechchina/Nimechchina
380 UAH.order
Cardosal 40 mg No. 28 tablets Berlin Chemi AG, /Daichi Sankio Europe GmbH/Labor.Menarini S.A., Nimechchina
427 UAH. order
Cardosal plus 20/25 No. 28 tablets Berlin Chemi AG, Nimechchina
380 UAH. order
Cardosal 20 mg No. 28 tablets Berlin Chemi AG, /Daichi Sankio Europe GmbH/Labor.Menarini S.A., Nimechchina
388 UAH order
Cardosal 10 mg N28 tablets Berlin Chemi AG, /Daichi Sankio Europe GmbH/Labor.Menarini S.A., Nimechchina
312 UAH. order

Newspaper "News of Medicine and Pharmacy" Cardiology (368) 2011 (thematic issue)

General view of sartans

Now we can confidently talk about a significant expansion of the use of sartans in the world practice of treating internal diseases over the past decade.
Having antihypertensive efficacy comparable to angiotensin-converting enzyme inhibitors (ACEIs), organoprotective properties, a favorable effect on prognosis and proven safety, sartans show placebo-like tolerability. These valuable properties determine a clear transformation of the views of practicing doctors around the world (Europe, USA, Japan) in the place of sartans: instead of being used primarily for intolerance to ACEIs, they are increasingly used on an equal basis with ACEIs or even ahead of ACEIs. The latter concerns primarily two indications: 1) uncomplicated arterial hypertension (AH) and 2) chronic kidney disease (CKD) against the background of type 2 diabetes mellitus (DM2). For hypertension sartans:

- constitute one of the basic classes of antihypertensive drugs;

— over the past 7–8 years they have shown continuous rapid growth in foreign appointment statistics;

- are constantly included in more and more new fixed combinations of antihypertensive drugs registered in the world, which directly indicates the popularity of this group of drugs among clinicians.

For CKD on the background of CD-2 sartans:

— recognized as the leading (ahead of ACEI) group of renoprotective drugs by experts of the world’s leading nephrological associations (primarily the National Kidney Foundation, USA, 2010);

— are recommended for use to protect the kidneys, starting from the early stages (microalbuminuria), up to the advanced stages (overt diabetic nephropathy), and further with CKD stages 2–3 and, in some cases, stage 4.

The high safety should be emphasized once again . In the ongoing confrontation with ACE inhibitors (the controversy on both sides is supported by companies producing drugs of both groups, which is clearly not beneficial for patients and leads to a state of uncertainty for practicing doctors), sartans are confidently holding their own. The severity of the discussion is confirmed by its duration and diversity. Only recently has the discussion of the question of whether sartans increase the risk of developing myocardial infarction, which lasted for several years, practically ended (result: they do not increase and even reduce, although to a slightly lesser extent than ACE inhibitors; in this regard, in case of coronary heart disease, sartans still usually used for intolerance to ACE inhibitors). In August 2010, data from a meta-analysis by Sipahi et al. about the possibility of increasing cancer risk due to the use of sartans. In this regard, let us quote a fragment of an editorial from the European Heart Journal, published in 2011 and entitled “Twisting arms to ARBs: the turn of cancer”, by famous European experts with the participation of M. Volpe, LM Ruilope: “...At present At this time, we do not think that the data from the analysis of Sipahi et al. sufficient to warrant a prospective study assessing the causal relationship between sartans (or any individual sartan) and tumor growth... More recently, the Food and Drug Administration (FDA) in a special communication on sartans and cancer (available at website https://www.fda.gov/Drugs/DrugSafety/PostmarketDrugSafetyInformationforPatientsandProviders/ucm218845.htm) does not indicate that sartans increase the risk of cancer... FDA recommends that sartans continue to be used as directed and that patients continue to take them..."

A few words about areas of application of sartans other than hypertension, type 2 diabetes, CKD and coronary heart disease (CHD). Drugs in this group can be quite widely used in post-stroke patients (cerebroprotection, improved prognosis), in people with type 1 diabetes mellitus (various organ protection, including retinoprotection). Noteworthy is the possibility of their use in chronic heart failure (CHF) - both with intolerance to ACEIs and in addition to them. Experts from the world's leading cardiological associations recommend the addition of either sartans or aldosterone antagonists to the treatment of CHF if the clinical manifestations of CHF persist despite the use of ACE inhibitors, diuretics and beta-blockers in titrated doses (attention is drawn to the fact that the use of a “triple” combination, including ACEI, sartan and aldosterone antagonist are not recommended). Sartans are more widely used for CHF in Japan: according to recent registers in this country, up to 50% of patients with CHF take sartans (their share is higher than the share of ACE inhibitors). Noteworthy are the data from the recent Japanese study HF-COSTAR, which showed that the combined use of sartans and statins more significantly improves left ventricular (LV) systolic function and reduces the clinical manifestations of CHF than the isolated use of sartans - this is interpreted as evidence of the synergistic beneficial effects of these groups of drugs for CHF (Y. Maejima et al., 2011).

Olmesartan place. ROADMAP Study

One of the promising representatives of the sartan group is olmesartan (represented in Ukraine by the drug Cardosal). In a number of fairly serious studies, the drug demonstrated a clear but smooth antihypertensive effect, comparable in severity to that of both other sartans and drugs from other basic antihypertensive classes. The antihypertensive effect of olmesartan was stable over time when taken for more than 1 year. Evidence of its organoprotective properties (regression of LV hypertrophy, anti-atherosclerotic effects, reduction of microalbuminuria (MAU), local intravascular anti-inflammatory effects) is presented. Tolerability of olmesartan (as well as sartans in general) is placebo-like. The drug has shown beneficial effects in elderly patients (including those with isolated systolic hypertension). Familiar is the information about the increase in antihypertensive effectiveness when combining olmesartan with hydrochlorothiazide, as well as about the good tolerability of this combination.

In 2011, data from a large-scale ROADMAP study involving olmesartan were published; We consider it important to dwell on the characteristics of the protocol and results of this study. The study was a randomized, double-blind, multicenter study that included 4447 patients with T2DM without microalbuminuria (47% men, mean age 58 years, duration of T2DM ~ 6 years, concomitant ischemic heart disease in 25%, mean glomerular filtration rate (GFR) ) - 85 ml/min). These patients, in addition to standard treatment, received either placebo or olmesartan at a dose of 40 mg/day. To achieve the target blood pressure (BP), which was defined as values less than 130/80 mmHg, other groups of antihypertensive drugs could be used if necessary. The primary endpoint of the study was time to first appearance of MAU. The study lasted up to 4 years. The ROADMAP results were overall very positive for olmesartan. The target blood pressure level was achieved in 80% of patients receiving olmesartan and in 71% of patients receiving placebo; blood pressure levels in the olmesartan group were 3.1/1.9 mmHg. lower than in the placebo group. During the observation period, the incidence of MAU development in the olmesartan group was 23% lower (p = 0.01) than in the placebo group. This beneficial renoprotective effect of the drug did not significantly depend on the initial blood pressure levels, the degree of compensation for type 2 diabetes, or the initial state of renal function. Olmesartan was well tolerated. Taking into account the ROADMAP data, olmesartan became the only sartan that demonstrated renoprotective effects in such a large randomized controlled trial at such an early stage of the development of diabetic nephropathy (previously conducted studies of similar scale RENAAL, IRMA, IDNT included individuals with diabetes who either already had MAU, or overt diabetic nephropathy was present).

Requires a balanced commentary: the slightly higher incidence of fatal cardiovascular complications revealed in the olmesartan group compared to the placebo group (15 patients - 0.7% versus 3 patients - 0.1%), which the study authors associate with an excessive decrease in blood pressure (systolic blood pressure (SBP) - less than 120 mm Hg) in the group of people with initial IHD). In discussing these data, JR Ingelfinger et al. in an editorial published in The New England Journal of Medicine, indicate that "FDA experts, after reviewing the ROADMAP results, did not conclude that olmesartan increases the risk of death... they believe that the beneficial effects of olmesartan in patients with elevated blood pressure are clearly outweigh the potential risks associated with its use...” The data presented are interpreted as further evidence that an excessive decrease in blood pressure in patients with coronary artery disease can have negative consequences (such a conclusion is quite familiar, for example, from the ONTARGET, INVEST, etc. studies; it can also be illustrated by the long-discussed phenomenon in the practice of treating hypertension J-curve). To summarize, we can say that in ROADMAP, olmesartan confirmed high safety and excellent tolerability ; It should be borne in mind that when prescribing antihypertensive drugs (not only sartans, but also other groups) in patients with concomitant ischemic heart disease, an excessive decrease in blood pressure (systolic - less than 120 mm Hg) should be avoided.

Antihypertensive efficacy, renoprotective properties and tolerability of olmesartan (Cardosal) in the ORCHESTR study, Ukraine

Next, we present data from an open prospective study ORCHESTR (OlmesaRtan (Kardosal) for arterial hypertension in patients with type 2 diabetes mellitus and microalbuminuria), which was conducted with the participation of practicing doctors in Donetsk and the region. The purpose of the study was to evaluate the antihypertensive effectiveness, renoprotective properties and tolerability of the drugs Cardosal (olmesartan) and Cardosal plus (fixed combination of olmesartan with hydrochlorothiazide in the ratios of 20/12.5 and 20/25 mg) in patients with hypertension of 1–3 degrees, in parts of which could be type 2 diabetes and/or MAU. Patients who had proteinuria according to a general clinical urine test were excluded from the study; persons with acute coronary syndrome, GFR less than 60 ml/min, with tumor lesions, and CHF of functional classes III–IV were also excluded. The observation mode for patients was outpatient, visits were provided at the beginning of observation, then after 2, 4 and 6 weeks; There were approximately 20 patients for each participating physician.

In all patients, at the beginning of observation and at its completion (after 6 weeks), according to generally accepted methods, the levels of glycemia, total cholesterol, low-density lipoprotein cholesterol, creatinine (with GFR calculation using the Cockroft-Gault formula) were assessed, and MAU levels were also assessed (PHAN, Pliva -Lachema Diagnostica sro).

Antihypertensive therapy in patients included in the study included the initial administration of Cardosal 20 mg/day or Cardosal plus 20/12.5 mg/day - at the discretion of the physician. At visits after 2 and 4 weeks, the dose of drugs was adjusted depending on whether the target blood pressure numbers were achieved (which were defined as levels less than 140/90 mm Hg for people without type 2 diabetes, and if they had it, levels less than 130/80 mmHg.). If necessary, to the above antihypertensive therapy, the doctor could add antihypertensive drugs of other classes (except ACE inhibitors, sartans and thiazide/thiazide-like diuretics). In individuals with high to very high levels of additional cardiovascular risk, inclusion of a statin and aspirin in the treatment program (after blood pressure approaches target values) was recommended in the treatment program, unless there were contraindications or intolerance.

For the study, a simple formalized patient observation chart was developed. Statistical processing was carried out using Microsoft Office, Excel, 2007; Depending on the nature of the data distribution, we used parametric or nonparametric methods. Continuous data are presented as mean and standard deviation (M ± SD); means were compared using Student's t test. Categorical data are presented as percentages (%) and compared using c2 tests and Fisher's exact test. Levels of p < 0.05 were considered statistically significant.

Results of the ORCHESTRA study. The study included 624 patients (255 men and 369 women, mean age 57.7 ± 10.3 years). Age was under 50 years in 22.9%, 51–60 years old in 36.1%, 61–70 years old in 28.6%, 71–80 years old in 11.2%, over 80 years old in 1 .2%. Concomitant hypertension diseases were represented by chronic ischemic heart disease in 61.4%, diabetes mellitus - in 35.1%. Chronic heart failure stage I was in 38.7%, stage IIa - in 17.2%, stage IIb - in 2.1%. Initially, MAU occurred in 238 (38.4%) patients.

All patients included in the study completed a 6-week follow-up period. By the end of this period, the distribution of patients by dosage of the study drug was as follows: Cardosal 20 mg/day was received by 225 (36.1%) patients, Cardosal 40 mg/day - 13 (2.1%) patients, Cardosal plus 20/12, 5 mg/day - 168 (26.9%) and Cardosal plus 20/25 mg/day - 218 (34.9%). In addition to olmesartan medications, patients received: calcium channel blockers - in 137 (21.9%) cases, b-blockers - in 239 (38.3%), other antihypertensive drugs - in 93 (15.9%), statins - in 449 (71.9%), aspirin - in 380 (60.9%) cases.

Olmesartan-based treatment was well tolerated. In none of the observations was there a sharp decrease in blood pressure; in all cases, the decrease in blood pressure was significant and persistent, but very smooth. During the observation period, none of the patients had situations that would be interpreted by the doctor as a manifestation of cardiovascular instability and would require hospitalization. There were no cases of drug withdrawal. In 3 observations during treatment there was nausea, in 4 - headache, in 6 - dizziness (in total - in 13 patients - 2.1%), however, it is difficult to clearly link the occurrence of these effects with taking olmesartan (in all cases these effects were transient).

The antihypertensive effectiveness of the treatment was high. During the observation period, target blood pressure values were achieved in 523 (83.8%) patients. In Fig. Figures 1 and 2 show the dynamics of average values of systolic and diastolic blood pressure (DBP) in the observed patients. As can be seen in Fig. 1 and 2, blood pressure levels showed a stable gradual decrease after 2, 4 and 6 weeks from the start of treatment.

In table Figure 1 shows the dynamics of the studied laboratory parameters at the beginning of observation of patients and at its completion. Commenting on the data in Table. 1, it should be noted the positive dynamics of all studied parameters during the treatment process. These changes in total cholesterol, low-density lipoprotein cholesterol, and glycemia may be due to more frequent use of statins during the study and more careful monitoring of the glycemic profile during follow-up. Statistically significant favorable changes in the levels of creatinine, GFR and MAU are noteworthy, which can be interpreted as a renoprotective effect of treatment (due primarily to olmesartan). It is important to note that out of 238 patients who had MAU at the beginning of observation, by the 6th week of treatment in 63 cases MAU was no longer detected (in 43 of them there was hypertension in combination with T2DM, in 20 - only hypertension).

The presented data allows us to draw the following conclusions :

1. Sartans are one of the harmoniously developing classes of modern medicines, especially widely used in the treatment of hypertension, diabetes mellitus, diabetic nephropathy in type 2 diabetes. This class of drugs is characterized by high safety and placebo-like tolerability.

2. Olmesartan is a new and promising representative of this class. It has high antihypertensive effectiveness, confirmed organoprotective effects. In a recent large-scale randomized controlled trial, ROADMAP, the drug demonstrated a renoprotective effect in patients with T2DM (with a clear reduction in the risk of developing MAU). Olmesartan is the only sartan (and in general among all antihypertensive drugs) that has such a strong evidence base for the earliest renoprotective effect in T2DM (a specially designed study with an early renal primary endpoint).

3. In the domestic prospective open study ORCHESTR, therapy based on olmesartan (drugs Cardosal and Cardosal plus) in patients with hypertension, in some cases with T2DM and/or MAU, demonstrated for 6 weeks:

- good tolerability with a smooth antihypertensive effect and low frequency (2.1%) of side effects;

— high antihypertensive effectiveness with achievement of target blood pressure in 83.8% of cases;

- beneficial effects on total cholesterol and glycemic levels;

- renoprotective effects with a significant decrease in serum creatinine levels, an increase in glomerular filtration rate, and a decrease in microalbuminuria levels. In 43 patients who had MAU at the beginning of the study, MAU was not detected at the end of the study.

4. Taking into account the data from the ORCHESTR study, we can talk about good prospects for the use of the drugs Cardosal (olmesartan) and Cardosal plus (olmesartan with hydrochlorothiazide) in patients with hypertension, as well as with type 2 diabetes, possibly in combination with CKD - olmesartan provides effective control AD has organoprotective potential and is well tolerated.