Instruction for Cardosal
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Cardosal is an antihypertensive drug, angiotensin II receptor antagonist.
Release form and composition
The drug is produced in the form of film-coated tablets: round, biconvex, white, on one side with an imprint "C14", with a specific subtle odor (14 pcs. In blisters, in a cardboard box 1, 2, 4 or 7 blisters together with instructions for use of Cardosal).
Composition for one tablet:
active ingredient: olmesartan medoxomil - 20 mg;
auxiliary components: hyprolosis with a low degree of substitution, hyprolosis with a viscosity of 6–10 mPa × s, lactose monohydrate, magnesium stearate, microcrystalline cellulose;
film shell: talc, titanium dioxide, hypromellose with a viscosity of 5 mPa s.
Olmesartan medoxomil is a potent specific antagonist of angiotensin II receptors (AT1 receptors). Angiotensin II is the primary vasoactive hormone of the RAAS (renin-angiotensin-aldosterone system). Due to its effect on AT1 receptors, it plays an important role in the mechanism of arterial hypertension. It is assumed that olmesartan medoxomil blocks all actions of the hormone angiotensin II, which are mediated by AT1 receptors, regardless of the synthesis route and source of origin of angiotensin II. Due to the specific antagonism of the drug in relation to the AT1 receptors of angiotensin II, the activity of renin, angiotensin I and angiotensin II in plasma increases, and the plasma concentration of aldosterone also decreases.
In patients with arterial hypertension under the influence of Cardosal, a prolonged dose-dependent decrease in blood pressure is observed. There is no evidence that hypotension develops after the first dose. There is also no evidence of the occurrence of tachyphylaxis during long-term therapy or the withdrawal syndrome after discontinuation of treatment (manifested by a sharp increase in blood pressure).
As a result of taking olmesartan once a day, a mild and effective decrease in blood pressure is provided for 24 hours, and the effectiveness of a single dose is similar to the effect of the drug when taken twice a day at the same daily dose.
The antihypertensive effect of Cardosal usually develops after 2 weeks, and approximately 8 weeks after the start of treatment, the maximum antihypertensive effect is observed.
Olmesartan medoxomil is a prodrug that, under the action of intestinal enzymes and during absorption from the gastrointestinal tract, in the portal blood, is converted into olmesartan (an active metabolite). In blood plasma and / or feces, unchanged olmesartan medoxomil or olmesartan with an intact site of medoxomil is absent. On average, the bioavailability of olmesartan is 25.6%.
The maximum plasma concentration of the active metabolite is reached approximately 2 hours after ingestion of the drug and increases almost linearly with an increase in a single dose of Cardosal to 80 mg. Food intake practically does not affect the bioavailability of the active substance, so the drug can be taken at any time, regardless of the time of the meal.
Up to 99.7% of olmesartan binds to plasma proteins, while the shift in this indicator when interacting with other simultaneously used drugs and substances with a high degree of binding to blood plasma proteins is insignificant (this fact is confirmed by the absence of clinically significant interaction with warfarin). Olmesartan hardly binds to blood cells. After its intravenous administration, the average volume of distribution is 16 to 29 liters.
Plasma clearance is typically 1.3 L / h (19% coefficient of variation). It is quite low compared to the blood flow in the liver, which is 90 l / h.
Olmesartan is excreted by the kidneys (about 40% of the absorbed substance) and through the hepatobiliary system (about 60%). There are no other metabolites other than olmesartan. The enterohepatic recirculation of the active metabolite is minimal. Since the main part of the drug is excreted through the liver, it is contraindicated in patients with obstruction of the biliary tract.
After repeated oral administration, T1 / 2 of olmesartan is 10 to 15 hours. Already after taking the first few doses of Cardosal, an equilibrium state is achieved. After 14 days of daily use, no further accumulation of olmesartan is observed. Clearance in the kidneys averages 0.5–0.7 l / h and does not depend on the dose taken.
The pharmacokinetics of olmesartan in patients of different sex does not have clinically significant differences.
In renal failure, AUC (area under the concentration-time curve) increases by 62, 82 and 179% in patients with mild, moderate and severe renal failure, respectively (when compared with the same indicator in healthy volunteers).
In individuals with mild and moderate hepatic impairment, after a single oral administration of the drug, the AUC of olmesartan increased by 6% and 65%, respectively. After repeated administration of Cardosal, 20 AUC of olmesartan in patients with moderate hepatic insufficiency is 65% higher than in healthy volunteers. The mean values of the maximum plasma concentration in healthy people and patients with hepatic insufficiency were similar. The pharmacokinetic parameters of the drug in persons with severe hepatic impairment have not been studied.
In elderly and senile age (65 years and older) in patients with arterial hypertension, upon reaching an equilibrium state, the AUC of olmesartan increased by 35% (in persons aged 65-75 years) and by 44% (in patients older than 75 years), according to compared with younger patients. Perhaps these differences were due to age-related decline in renal function.
Indications for use
Cardosal is used to treat essential (primary) hypertension.
severe renal failure (creatinine clearance is less than 20 ml / min);
severe liver failure (more than 9 points on the Child-Pugh scale);
condition after kidney transplantation (since there is no experience of clinical use of the drug after kidney transplantation);
obstruction of the biliary tract;
lactase deficiency, hereditary galactose intolerance, glucose-galactose malabsorption (since the tablets contain lactose);
joint administration with aliskiren and aliskiren-containing drugs in patients with diabetes mellitus and / or patients with impaired renal function (creatinine clearance less than 60 ml / min);
period of pregnancy and lactation;
children and adolescents up to 18 years old;
hypersensitivity to the active substance or auxiliary components of the drug.
Relative (Cardosal is used with caution):
mild and moderate renal failure (creatinine clearance value more than 20 ml / min);
moderate hepatic impairment (less than 9 points on the Child-Pugh scale);
chronic heart failure;
Ischemic heart disease (ischemic heart disease);
mitral or aortic valve stenosis;
bilateral stenosis of the renal arteries or stenosis of the renal artery of a single kidney (vasorenal hypertension);
hypertrophic obstructive cardiomyopathy;
hyponatremia and / or hyperkalemia (due to the risk of arterial hypotension, dehydration and renal failure);
conditions leading to a decrease in the volume of circulating blood (for example, vomiting and diarrhea);
adherence to a diet with a limited content of table salt;
Connes syndrome (primary aldosteronism);
simultaneous use with lithium preparations and diuretics;
advanced age (patients over 65 years old).
Cardosal, instructions for use: method and dosage
Cardosal is taken orally, regardless of meal time. The tablet should not be chewed, but should be swallowed whole with plenty of water or other liquid. The drug is taken once a day, preferably at the same time.
The initial dose is 10 mg once a day. If the desired reduction in blood pressure has not been achieved, the dose can be increased to 20 mg per day. In the future, if necessary, the daily dose is increased to 40 mg. To select a dose, you can use different dosages of the drug (Cardosal 10, Cardosal or Cardosal 40).
The maximum dose is 40 mg per day.
Patients over the age of 65 should be treated with careful blood pressure monitoring.
With mild to moderate renal failure (creatinine clearance from 20 to 60 ml / min), the maximum daily dose of the drug is 20 mg (in patients with severe renal failure, olmesartan medoxomil is not used).
For patients with mild hepatic impairment, the drug is prescribed in usual doses. With moderate hepatic impairment, the initial daily dose is 10 mg, the maximum is 20 mg. In the case of simultaneous use with diuretics and / or other antihypertensive drugs in patients with hepatic insufficiency, it is necessary to monitor renal function and blood pressure. In severe hepatic impairment, Cardosal is contraindicated.
gastrointestinal tract: often - dyspeptic disorders, nausea, gastroenteritis, diarrhea, abdominal pain; infrequently - vomiting;
metabolism and nutrition: often - an increase in the plasma concentration of triglycerides and uric acid; rarely - an increase in the content of potassium in the blood;
cardiovascular system: infrequently - angina pectoris; rarely - a significant decrease in blood pressure;
respiratory system: often - rhinitis, pharyngitis, cough, bronchitis;
nervous system and sensory organs: often - headache, dizziness; infrequently - vertigo;
urinary system: often - urinary tract infections, an increase in the number of red blood cells in the urine; rarely - renal failure, including acute;
lymphatic system and blood: infrequently - thrombocytopenia;
musculoskeletal system: often - arthritis, bone and back pain; infrequently - muscle pain; rarely - muscle cramps;
skin and subcutaneous fat: infrequently - allergic dermatitis, skin rash, exanthema, itching, urticaria; rarely - Quincke's edema;
immune system: infrequently - anaphylactic and anaphylactoid reactions;
indicators of laboratory tests: often - an increase in the activity of liver enzymes, an increase in the content of urea and creatine phosphokinase in the blood; rarely - an increase in the plasma concentration of creatinine;
other reactions: often - flu-like symptoms, chest pain, weakness, peripheral edema; infrequently - malaise, asthenia, swelling of the face; rarely - a feeling of drowsiness; isolated cases - rhabdomyolysis.
Data on overdose of Cardosal are very limited. The main symptom is a marked decrease in blood pressure.
The patient should be laid in a horizontal position (on his back), slightly lifting his legs. It is recommended to flush the stomach and / or give the patient activated charcoal. Further treatment should be aimed at replenishing the circulating blood volume and correcting violations of the water-electrolyte balance. The effectiveness of dialysis to eliminate olmesartan has not been studied.
Before starting therapy with Cardosal, it is necessary to eliminate factors that contribute to an additional decrease in blood pressure (intensive diuretic treatment, vomiting, diarrhea, limited consumption of table salt).
In some patients, renal function and vascular tone depend on the activity of the RAAS to a greater extent than in others (for example, in severe chronic heart failure or renal artery stenosis). In such patients, concomitant use of other drugs that affect the RAAS can lead to the development of oliguria, azotemia, acute arterial hypotension, or acute renal failure (rarely).
With the use of angiotensin II receptor antagonists, the possibility of a similar therapeutic effect cannot be excluded.
In patients with vasorenal hypertension who receive drugs that affect the RAAS, the risk of renal failure and severe arterial hypotension is increased.
In case of impaired renal function during treatment with Cardosal, it is recommended to periodically monitor the level of creatinine and the content of potassium in the blood plasma.
Hyperkalemia, sometimes associated with treatment with angiotensin II receptor antagonists or angiotensin converting enzyme (ACE) inhibitors, can be fatal. The risk of its occurrence increases with renal failure, dehydration, metabolic acidosis, diabetes mellitus, acute decompensation of cardiac activity, conditions that are accompanied by massive cell lysis (extensive trauma, rhabdomyolysis, acute limb ischemia), when used together with drugs that increase the plasma potassium concentration, as well as in old age.
The appointment of Cardosal simultaneously with other drugs that affect the RAAS is possible only after a careful assessment of the balance of benefits and risks of this combination. Consideration of other treatment options is recommended.
In patients of the Negroid race, the effectiveness of therapy with olmesartan medoxomil is slightly lower than in other races, which, apparently, is due to the greater prevalence of low plasma renin activity in this population.
An excessive decrease in blood pressure in patients with cerebrovascular insufficiency or ischemic heart disease can lead to stroke or myocardial infarction.
Influence on the ability to drive vehicles and complex mechanisms
During the period of treatment with Cardosal, adverse reactions such as weakness and drowsiness may occur, therefore, when driving a car or other vehicles, as well as while engaging in other potentially hazardous activities, care must be taken.
Application during pregnancy and lactation
There is no experience of using the drug in pregnant women. However, it is known that drugs that directly affect the RAAS have a severe teratogenic effect, therefore Cardosal is contraindicated during pregnancy. If pregnancy occurs during treatment with the drug, it should be immediately canceled and another, alternative therapy should be prescribed.
For women planning pregnancy, it is advisable to select antihypertensive drugs from other groups, the safety of which during pregnancy has been proven by relevant studies. The exception is when the use of angiotensin II receptor antagonists is vital.
Pregnant women who have taken angiotensin II receptor antagonists in the II and III trimesters should undergo an ultrasound examination of the fetus to assess the ossification of the skull bones and kidney function. Newborns whose mothers took drugs of this group should be examined for possible impairment of renal function and the development of arterial hypotension.
It is not known whether the drug is secreted in human breast milk. There are reliable data on the penetration of olmesartan into the breast milk of rats. Therefore, during lactation, Cardosal is contraindicated.
In patients under 18 years of age, Cardosal is not used due to the lack of data on the efficacy and safety of olmesartan medoxomil in childhood.
With impaired renal function
Olmesartan medoxomil is contraindicated in severe renal impairment (creatinine clearance less than 20 ml / min). With a creatinine clearance of 20 to 60 ml / min, Cardosal is used with caution.
For violations of liver function
Cardosal is contraindicated in patients with severe hepatic impairment and obstruction of the biliary tract.
Use in the elderly
In patients aged 65 years and older, Cardosal is used with caution.
Cardosal is not recommended to be taken simultaneously with potassium preparations, potassium-containing salt substitutes, potassium-sparing diuretics and other drugs that increase the plasma concentration of potassium (for example, immunosuppressants, selective cyclooxygenase-2 inhibitors, heparin, ACE inhibitors, etc.), as this can lead to hyperkalemia. ...
The antihypertensive effect of olmesartan is usually enhanced when used together with other drugs to lower blood pressure.
Cyclooxygenase-2 inhibitors, non-steroidal anti-inflammatory drugs (including acetylsalicylic acid in doses of more than 3 g per day) and angiotensin II receptor antagonists are able to synergize and reduce glomerular filtration. In the case of a combination of olmesartan with non-steroidal anti-inflammatory drugs, the likelihood of acute renal failure increases, therefore, at the beginning of joint therapy, it is recommended to monitor renal function and consume a sufficient amount of fluid. In addition, with simultaneous use, it is possible to reduce the antihypertensive activity of angiotensin II receptor antagonists and partially lose their therapeutic effect.
Co-administration with lithium preparations is not recommended (due to a possible reversible increase in the serum concentration of lithium and an increase in its toxicity).
Antacids (magnesium hydroxide and aluminum hydroxide) may moderately reduce the bioavailability of olmesartan.
Cardosal should not be used simultaneously with aliskiren, aliskiren-containing drugs and ACE inhibitors, since with a double blockade of the RAAS, the incidence of hyperkalemia, arterial hypotension and a decrease in renal function is higher than in the case of therapy with only one drug from the listed drugs.
Aliskiren-containing drugs should not be combined with olmesartan medoxomil in patients with renal failure and diabetes mellitus. Patients with diabetic nephropathy should not be simultaneously prescribed ACE inhibitors.
There was no clinically significant interaction with digoxin, pravastatin, warfarin and hydrochlorothiazide.
Terms and conditions of storage
Keep out of the reach of children. Store in a dark place at a temperature not exceeding 30 ° C.
The shelf life of the drug is 3 years.
Reviews about Cardosal
There are not many reviews of Cardosal. Patients note that the drug reduces and stabilizes blood pressure well, and is suitable for long-term use. The tablets are convenient to take (a sufficient single dose per day).
The main disadvantage, according to doctors and patients, is the frequent occurrence of side effects, including persistent weakness and chest pain.
Terms of sell
You don't need a prescription to buy Cardosal.