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Pharmacological properties

olmesartan medoxomil is a potent oral active selective receptor antagonist (type at1) of angiotensin ii. it is believed that it inhibits all the actions of angiotensin ii, which are mediated by the at1 receptor, regardless of the source and route of synthesis of angiotensin ii. selective antagonism of at1 receptors to angiotensin ii leads to an increase in plasma renin levels and angiotensin i and ii concentrations, as well as to a certain decrease in the concentration of aldosterone in blood plasma.

Angiotensin II is the main vasoactive hormone of the renin-angiotensin-aldosterone system (RAAS) and plays an important role in the pathophysiology of hypertension through type 1 receptors (AT1).

Clinical Efficiency and Safety

In hypertension of olmesartan, medoxomil causes a dose-dependent long-term decrease in blood pressure. There is no evidence of arterial hypotension after taking the first dose, tachyphylaxis with prolonged treatment, or the return of hypertension after discontinuation of treatment.

A single daily dose of olmesartan medoxomil provides an effective and mild decrease in blood pressure within 24 hours. A single daily dose of the drug provides the same decrease in blood pressure as when applying its daily dose, divided into 2 doses throughout the day.

With continuous treatment, the maximum decrease in blood pressure is achieved 8 weeks after the start of therapy, although a significant decrease in blood pressure was noted after 2 weeks of treatment. When used with hydrochlorothiazide, an additional decrease in blood pressure is observed, and such concomitant use of drugs is well tolerated.

The effect of olmesartan on mortality and morbidity is still unknown.

In a randomized study of olmesartan and prevention of microalbuminuria in diabetes (ROADMAP study), which involved 4447 patients with type II diabetes, with normal albuminuria and with at least one risk factor for cardiovascular disease, they studied the possibility of delaying the onset of microalbuminuria due to treatment with olmesartan. During the next study, which lasted an average of 3.2 years, patients received olmesartan or placebo in addition to other antihypertensive drugs, except for ACE inhibitors or angiotensin receptor blockers.

According to the criterion of clinical observations of the primary endpoint, the study showed a significant reduction in risk, which was manifested in a reduction in the length of time before the onset of microalbuminuria and was noted mainly with olmesartan. After adjusting for the discrepancy in blood pressure, such a reduction in risk was no longer statistically significant. Microalbuminuria developed in 8.2% (178 of 2160) patients of the olmesartan group and in 9.8% (210 of 2139) of the placebo group.

According to the criteria for clinical observations of secondary endpoints, cases of cardiovascular disorders occurred in 96 (4.3%) patients taking olmesartan, and in 94 (4.2%) patients in the placebo group. The incidence of death due to cardiovascular disease was higher with olmesartan than with placebo [15 patients (0.7%) compared with 3 patients (0.1%)], despite a similar incidence of non-fatal stroke [14 patients (0.6%) compared with 8 patients (0.4%)], non-fatal myocardial infarction [17 patients (0.8%) compared with 26 patients (1.2%)] and death from others not associated with cardiovascular disease, causes [11 patients (0.5%) compared with 12 patients (0.5%)]. With olmesartan, overall mortality increased numerically [26 patients (1.2%) compared with 15 patients (0.7%)], which was mainly the result of a large number of deaths due to cardiovascular disease.

A study of diabetic nephropathy to reduce the incidence of end-stage kidney disease with olmesartan (ORIENT study) examined the effects of olmesartan on renal and cardiovascular outcomes in 577 randomized Japanese and Chinese with type II diabetes, with obvious nephropathy. During the next study, which lasted an average of 3.1 years, patients received olmesartan or placebo in addition to other antihypertensive drugs, including ACE inhibitors.

The primary combined endpoint (the length of time until the first doubling of plasma creatinine concentration, the final stage of kidney disease, death for any reason) was recorded in 116 (41.1%) patients in the olmesartan group and in 129 (45.4%) patients in the group placebo [relative risk 0.97 (95% confidence interval 0.75–1.24); p = 0.791]. A secondary combined endpoint associated with cardiovascular disease was noted in 40 (14.2%) patients who took olmesartan and in 53 (18.7%) placebo patients. This combined endpoint associated with cardiovascular disease included death due to cardiovascular disease in 10 (3.5%) patients taking olmesartan, compared with 3 (1.1%) patients in the placebo group, overall mortality 19 (6.7%) patients compared with 20 (7.0%) patients, non-fatal stroke in 8 (2.8%) patients compared with 11 (3.9%) patients and non-fatal myocardial infarction in 3 (1 , 1%) patients compared with 7 (2.5%) patients, respectively.

Other information. In two large randomized controlled trials: ONTARGET (a global endpoint study for telmisartan alone and when used in combination with ramipril) and VA NEPHRON-D (a diabetes nephropathy study conducted by the U.S. Department of Veterans Affairs) studied the use of a combination of inhibitors ACE with angiotensin II receptor blockers (ARB II).

The ONTARGET study was conducted with patients with a history of cardiovascular or cerebrovascular disease, or type II diabetes mellitus with signs of complications. The VA NEPHRON-D study was performed in patients with type II diabetes mellitus and diabetic nephropathy.

These studies showed that, compared with monotherapy, the use of combined treatment did not lead to a significant positive effect on the consequences and mortality due to renal and / or cardiovascular diseases, but led to an increased risk of hyperkalemia, acute kidney damage and / or arterial hypotension. Given the similar pharmacodynamic properties of ACE inhibitors and ARB II, the findings are valid for other representatives of this category of drugs.

Thus, patients with diabetic nephropathy should not be used together with ACE inhibitors and ARB II.

The ALTITUDE study (a study of aliskiren in type II diabetes using endpoints associated with cardiovascular and renal disease) was devoted to the benefits of adding aliskiren to standard therapy with ACE inhibitors or ARB II in the treatment of patients with type II diabetes and chronic kidney disease cardiovascular disease or with both pathologies. This study was quickly discontinued due to an increased risk of adverse effects. Compared to the placebo group, in patients of the aliskiren group, death due to cardiovascular disease and stroke was quantitatively more frequent, and the corresponding side effects and serious undesirable effects (hyperkalemia, arterial hypotension and impaired renal function) were also recorded more often in patients of the group aliskiren.

Pharmacokinetics Suction and distribution. Olmesartan Medoxomil is a prodrug. It quickly turns into a pharmacologically active metabolite olmesartan under the influence of esterases in the intestinal mucosa and in the portal blood during absorption in the digestive tract.

In the blood plasma or in the excretion products of olmesartan, medoxomil, which did not disintegrate, or the unchanged side chain of the medoxomil group was not detected. The average absolute bioavailability of olmesartan from a tablet dosage form is 25.6%.

Average maximum value (Cmax) plasma olmesartan is reached 2 hours after taking the drug, and the plasma concentration rises almost linearly with an increase in a single oral dose to 80 mg.

Food practically does not affect the bioavailability of olmesartan, so olmesartan medoxomil can be used regardless of food intake.

In the pharmacokinetics of olmesartan, no clinically significant gender difference was noted.

The binding of olmesartan medoxomil to plasma proteins is significant (99.7%), but the potential for a clinically significant shift in the level of protein binding during the interaction of olmesartan with other drugs with a high degree of protein binding is low (which is confirmed by the fact that there is no clinically significant interaction between olmesartan medoxomil and warfarin). The binding of olmesartan to blood cells is negligible. The average volume of distribution after iv administration is small (16–29 L).

Metabolism and excretion. The total plasma clearance, as a rule, was 1.3 l / h (CV, 19%) and was relatively slow compared to blood circulation in the liver (about 90 l / h). After a single dose of olmesartan medoxomil labeled with an isotope 14C, 10–16% of the administered radioactivity was excreted in the urine (the vast majority within 24 hours after the dose was administered), and the remainder of the radioactivity was excreted in the feces. Based on an indicator of systemic availability (25.6%), it can be calculated that absorbed olmesartan is excreted both by the kidneys (approximately 40%) and through the liver and biliary tract (approximately 60%). All deduced radioactivity was identified as olmesartan. No other significant metabolite was detected. The enterohepatic recirculation of olmesartan is minimal. Since a significant portion of olmesartan is excreted through the biliary tract, the use of the drug in patients with biliary tract obstruction is contraindicated.

Final t½ olmesartan was in the range of 10–15 hours after repeated oral administration. A stable state was achieved after taking the first few doses of the drug, and its further accumulation was not observed after 14 days of repeated administration. Renal clearance was approximately 0.5-0.7 l / h and was not dose-dependent.

Pharmacokinetics in special patient groups

Persons of advanced age (from 65 years). In patients with hypertension, the stable AUC value increased by about 35% in elderly patients (65–75 years) and by about 44% in patients aged 75 and over compared with the younger group. This, at least in part, may be associated with an average decrease in renal function in this group of patients.

Impaired renal function. In patients with mild, moderate, or severe renal impairment, AUC in steady state increased by 62, respectively; 82 and 179% compared with the corresponding parameters in healthy volunteers of the control group.

Impaired liver function. After a single oral administration, the AUC of olmesartan in patients with mild or moderate impaired liver function was 6 and 65% higher, respectively, than the corresponding figure in the corresponding healthy volunteers. 2 hours after taking the drug by healthy volunteers and patients with mild to moderate impaired liver function, the unbound fraction of olmesartan was 0.26, respectively; 0.34 and 0.41%. After repeated use in patients with moderate hepatic impairment, the average AUC of olmesartan was 65% higher than in the corresponding healthy volunteers. Average cmax olmesartan was similar in patients with impaired liver function and in healthy volunteers. Evaluation of the use of olmesartan medoxomil in patients with severely impaired liver function was not performed.

Interaction with other drugs.To wheelsetelam (a substance that binds bile acids): the simultaneous use of 40 mg of olmesartan medoxomil and 3750 mg of wheelomelam hydrochloride led to a decrease in Cmax olmesartan by 28% and a decrease in the AUC of olmesartan by 39%. Weak effect (decrease in indicators Cmax and AUC by 4 and 15%, respectively) was noted with the use of olmesartan medoxomil 4 hours before the use of wheel magnam hydrochloride.

T½ olmesartan was reduced by 50–52%, regardless of how it was used - simultaneously with wheel magnam hydrochloride or 4 hours before the use of this drug.


Essential Ag.


Adults the initial daily dose of olmesartan medoxomil is 10 mg once a day. if hell does not decrease enough, the dose is increased to 20 mg once a day. if necessary, the dose of the drug can be increased to a maximum of 40 mg / day or added to the treatment of hydrochlorothiazide. the antihypertensive effect of olmesartan medoxomil is noted, as a rule, within 2 weeks after the start of treatment, and the maximum effect is 8 weeks after the start of therapy. this should be borne in mind when considering changes in the dosage regimen for any patient.

In order to comply with the dosing regimen, it is recommended to use the drug at approximately the same time every day, with or without food intake, for example, during breakfast. Tablets should be washed down with a sufficient amount of liquid (for example, 1 glass of water). The tablet should not be chewed.

Elderly patients (from 65 years). Usually there is no need for dose adjustment for elderly patients (see Patients with impaired renal function). With an increase in the daily dose to a maximum of 40 mg / day, blood pressure should be carefully monitored.

Patients with impaired renal function. The maximum daily dose for patients with mild or moderate renal impairment (creatinine clearance of 20-60 ml / min) is 20 mg, since there is no experience with higher doses for this group of patients. Olmesartan medoxomil is not indicated for severe renal impairment (creatinine clearance of 20 ml / min) due to little experience with its use in these patients.

Impaired liver function. In case of impaired liver function, mild severity dose adjustment is not required. With a moderate degree of violation, the initial dose of olmesartan medoxomil is 10 mg / day, and the maximum is 20 mg / day. With combined use in patients with impaired liver function, diuretics and / or other antihypertensive drugs, it is necessary to carefully monitor the level of blood pressure and kidney function. Olmesartan medoxomil is not indicated for severe hepatic impairment due to lack of sufficient experience. Olmesartan Medoxomil should not be used in patients with bile duct obstruction.


Hypersensitivity to the active substance or to one of the components of the drug. pregnancy or women planning a pregnancy (see use during pregnancy and lactation). bile duct obstruction. concomitant use of olmesartan with drugs containing aliskiren is contraindicated in patients with diabetes mellitus and renal failure (glomerular filtration rate of 60 ml / min / 1.73 m2).

Side effects

Side effects obtained from clinical studies of the drug cardosal, post-marketing studies of the safety of the drug and spontaneous messages are presented in the table. adverse reactions are distributed according to the frequency of occurrence as follows: very often (≥1 / 10); often (≥1 / 100, 1/10); infrequently (≥1 / 1000, 1/100); rarely (≥1 / 10,000, 1/1000); very rarely (1/10 000); frequency is unknown (cannot be estimated from available sources).

Classes of manifestations of disorders and diseases of organ systems according to the classification of MedDRA Adverse reactions Frequency
On the part of the blood system and lymphatic system Thrombocytopenia Infrequently
From the immune system Anaphylactic reaction Infrequently
On the part of metabolism and nutrition Hypertriglyceridemia Often
Hypercholesterolemia Infrequently
Hyperuricemia Often
Hyperkalemia Rarely
From the nervous system Dizziness Often
Headache Often
On the part of the hearing organ Vertigo Infrequently
From the heart Angina pectoris Infrequently
Tachycardia Infrequently
From the vessels Arterial hypotension Rarely
Respiratory, thoracic and mediastinal disorders Bronchitis Often
Pharyngitis Often
Cough Often
Rhinitis Often
From the gastrointestinal tract Gastroenteritis Often
Diarrhea Often
Abdominal pain Often
Nausea Often
Dyspepsia Often
Vomiting Infrequently
Sporiform enteropathy Rarely
On the part of the skin and subcutaneous tissue Exanthema Infrequently
Allergic dermatitis Infrequently
Hives Infrequently
Rash Infrequently
Itching Infrequently
Alopecia Unknown
Angioedema Rarely
From the musculoskeletal system and connective tissue Arthritis Often
Backache Often
Bone pain Often
Myalgia Infrequently
Arthralgia Infrequently
Muscle cramps Rarely
From the kidneys and urinary tract Hematuria Often
Urinary tract infection Often
Arrester Rarely
Impaired renal function Rarely
General violations Pain Often
Chest pain Often
Peripheral edema Often
Flu-like symptoms Often
Fatigue Often
Swelling of the face Infrequently
Asthenia Infrequently
General malaise Infrequently
Lethargic condition Rarely
Change laboratory settings Increased liver enzymes Often
Increased blood urea Often
Increased blood CPK Often
Increased Blood Creatinine Rarely

Isolated cases of rhabdomyolysis associated in time with the use of ARB II have been reported.

Additional information on specific patient groups. In elderly patients, the incidence of arterial hypotension increases slightly - from the category of "rarely" to "infrequently."

special instructions

Decrease in bcc. in patients with reduced BCC and / or hyponatremia due to intensive diuretic therapy, limited salt intake with food, diarrhea or vomiting, symptomatic hypotension may develop, especially after the first dose of the drug. these changes should be adjusted before starting treatment with olmesartan medoxomil.

Other conditions associated with stimulation of RAAS. Patients in whom vascular tone and function are more dependent on RAAS activity, for example, patients with severe congestive heart failure or with pathology of the kidneys, including renal artery stenosis, acute hypotension, azotemia, oliguria, or in rare cases of acute renal failure respond to other drugs that affect this system. The use of angiotensin II receptor antagonists may be accompanied by similar effects.

Vasorenal hypertension. The use of drugs that affect RAAS in patients with bilateral renal artery stenosis of the only kidney that functions is associated with a risk

Tags: Cardosal® [Olmesartan Medoxomil]