Cardosal tablets p / o 40mg, No. 28
Expiration Date: 05/2027
Russian Pharmacy name:
Кардосал таблетки п/о 40мг, №28
essential arterial hypertension
It is recommended to take the drug CardosalЃ inside every day at the same time, regardless of the meal 1 time / day.
The recommended initial dose for adults is 10 mg (1 tab. Drug CardosalЃ 10) 1 time / day. In case of insufficient decrease in blood pressure when taking the drug at a dose of 10 mg / day, the dose of the drug can be increased to 20 mg / day (it is possible to use the drug CardosalЃ 20). If an additional decrease in blood pressure is required, the dose of the drug can be increased to a maximum of 40 mg / day (the use of CardosalЃ 40 is possible) or a diuretic (hydrochlorothiazide) can be additionally prescribed. The maximum daily dose is 40 mg.
Active ingredient: olmesartan medoxomil - 10 mg
Excipients : microcrystalline cellulose - 40 mg, low-substituted hyprolose - 80 mg, lactose monohydrate - 246.4 mg, hyprolose 6-10 mPas - 10 mg, magnesium stearate - 3.6 mg.
The composition of the film shell: hypromellose 5 mPas - 8.64 mg, talc - 1.68 mg, titanium dioxide (E171) - 1.68 mg.
obstruction of the biliary tract;
renal failure (CC less than 20 ml / min), condition after kidney transplantation (no experience of clinical use);
lactase deficiency, galactosemia, or malabsorption syndrome;
pregnancy;
lactation period;
age up to 18 years (efficacy and safety have not been established);
hypersensitivity to the active substance or to any of the excipients that make up the drug.
The drug should be used with caution in the following conditions or diseases:
stenosis of the aortic or mitral valves;
hypertrophic obstructive cardiomyopathy;
primary aldosteronism;
hyperkalemia, hyponatremia (risk of dehydration, arterial hypotension, renal failure);
renal failure (CC more than 20 ml / min);
chronic heart failure;
bilateral stenosis of the renal arteries or stenosis of an artery of a solitary kidney;
Ischemic heart disease;
cerebrovascular diseases;
advanced age (over 65);
impaired liver function;
conditions accompanied by a decrease in BCC (including diarrhea, vomiting), as well as when following a diet with sodium restriction;
simultaneous use with diuretics.
CardosalЃ 10
White film-coated tablets , round, biconvex, with a 'C13' impression on one side, with a subtle specific odor.
Composition:
Active ingredient : olmesartan medoxomil - 10 mg
Excipients : microcrystalline cellulose - 10 mg, low-substituted hyprolose - 20 mg, lactose monohydrate - 61.6 mg, hyprolose 6-10 mPas - 2.5 mg, magnesium stearate - 0.9 mg.
The composition of the film shell: hypromellose 5 mPas - 3.6 mg, talc - 0.7 mg, titanium dioxide (E171) - 0.7 mg.
CardosalЃ 20
White film-coated tablets , round, biconvex, with a 'C14' imprint on one side, with a subtle specific odor.
Composition:
Active ingredient: olmesartan medoxomil - 20 mg
Excipients : microcrystalline cellulose - 20 mg, low-substituted hyprolose - 40 mg, lactose monohydrate - 123.2 mg, hyprolose 6-10 mPas - 5 mg, magnesium stearate - 1.8 mg.
The composition of the film shell: hypromellose 5 mPas - 5.76 mg, talc - 1.12 mg, titanium dioxide (E171) - 1.12 mg.
CardosalЃ 40
White film-coated tablets , oval, biconvex, with a 'C15' impression on one side, with a subtle specific odor.
Composition:
Active ingredient: olmesartan medoxomil - 10 mg
Excipients : microcrystalline cellulose - 40 mg, low-substituted hyprolose - 80 mg, lactose monohydrate - 246.4 mg, hyprolose 6-10 mPas - 10 mg, magnesium stearate - 3.6 mg.
The composition of the film shell: hypromellose 5 mPas - 8.64 mg, talc - 1.68 mg, titanium dioxide (E171) - 1.68 mg.
Clinical and pharmacological group: Angiotensin II receptor antagonist
Pharmaco-therapeutic group: Angiotensin II receptor antagonist
pharmachologic effect
Angiotensin II receptor antagonist (AT1 type). Angiotensin II is the primary vasoactive hormone of the RAAS and plays a significant role in the pathophysiology of hypertension via AT1 receptors. It is assumed that olmesartan blocks all the effects of angiotensin II mediated by AT1 receptors, regardless of the source and route of synthesis of angiotensin II.
With arterial hypertension, olmesartan causes a dose-dependent, prolonged decrease in blood pressure. There is no evidence of the development of arterial hypotension after taking the first dose of the drug, tachycardia during long-term treatment (for CardosalЃ 20 and CardosalЃ 40) and the development of withdrawal syndrome (a sharp increase in blood pressure after drug withdrawal).
Taking olmesartan medoxomil 1 time / day provides an effective and mild decrease in blood pressure within 24 hours, and the effect after a single dose is similar to the effect of taking the drug 2 times / day at the same daily dose.
The antihypertensive effect of olmesartan develops, as a rule, after 2 weeks, and the maximum effect develops approximately 8 weeks after the start of therapy.
Pharmacokinetics
Absorption and distribution
Olmesartan medoxomil is a prodrug. It is rapidly converted to the pharmacologically active metabolite olmesartan by enzymes in the intestinal mucosa and in the portal blood during absorption from the gastrointestinal tract. Olmesartan medoxomil in unchanged form was not detected in blood plasma. The bioavailability of olmesartan averages 25.6%. Cmax of olmesartan in blood plasma, on average, is achieved 2 hours after oral administration of olmesartan medoxomil and increases approximately linearly with an increase in a single dose to 80 mg.
Food intake does not significantly affect the bioavailability of olmesartan, therefore, olmesartan medoxomil can be taken with or without food.
There were no clinically significant differences in the pharmacokinetic parameters of olmesartan depending on gender.
Olmesartan binds to blood plasma proteins (99.7%), but the potential for a clinically significant shift in the amount of protein binding in the interaction of olmesartan with other highly binding and simultaneously used drugs is low (evidence of this is the absence of a clinically significant interaction between olmesartan and warfarin). The connection of olmesartan with blood cells is negligible.
Metabolism and excretion
Total plasma clearance is usually 1.3 L / h (coefficient of variation 19%) and is relatively low compared to hepatic blood flow (approximately 90 L / h). Renal excretion is approximately 40%, with bile - about 60%. Intrahepatic circulation of olmesartan is minimal. Since most of olmesartan is excreted through the liver, its use in patients with biliary obstruction is contraindicated.
T1 / 2 of olmesartan is 10-15 hours after repeated oral administration. A significant effect of therapy is achieved after taking the first few doses of the drug, and after 14 days of repeated use, further cumulation is not observed. Renal clearance is approximately 0.5-0.7 l / h and does not depend on the dose of the drug.
Pharmacokinetics in special clinical situations
In patients with impaired renal function, steady state AUC was increased by approximately 62%, 82% and 179% in the case of mild, moderate and severe renal impairment, respectively, compared with healthy volunteers.
After a single oral administration, the AUC values ??for olmesartan were 6% and 65% higher in patients with mild to moderate liver dysfunction, respectively, compared with healthy volunteers. The unbound fraction of olmesartan 2 hours after taking a dose of the drug in healthy volunteers, in patients with mild and moderate liver dysfunction was 0.26%, 0.34% and 0.41%, respectively.
Indications
essential arterial hypertension
Dosage regimen
It is recommended to take the drug CardosalЃ inside every day at the same time, regardless of the meal 1 time / day.
The recommended initial dose for adults is 10 mg (1 tab. Drug CardosalЃ 10) 1 time / day. In case of insufficient decrease in blood pressure when taking the drug at a dose of 10 mg / day, the dose of the drug can be increased to 20 mg / day (it is possible to use the drug CardosalЃ 20). If an additional decrease in blood pressure is required, the dose of the drug can be increased to a maximum of 40 mg / day (the use of CardosalЃ 40 is possible) or a diuretic (hydrochlorothiazide) can be additionally prescribed. The maximum daily dose is 40 mg.
Side effect
Possible side effects are listed below in descending frequency of occurrence: very common (> 1/10); often (> 1/100 <1/10); sometimes (> 1/1000, <1/100); rarely (> 1/10 000, <1/1000); very rare (<1/10 000), including isolated reports.
From the hematopoietic system: very rarely - thrombocytopenia.
From the side of the central nervous system: sometimes - dizziness; very rarely - headache.
From the respiratory system: often - pharyngitis, rhinitis; very rarely - cough, bronchitis.
From the digestive system: often - diarrhea, dyspepsia, gastroenteritis; very rarely - abdominal pain, nausea, vomiting.
On the part of the skin: very rarely - itchy skin, rash, angioedema, allergic dermatitis, urticaria.
From the musculoskeletal system: often - back pain, bone pain, arthralgia, arthritis; very rarely - muscle cramps, myalgia.
From the urinary system: often - hematuria, urinary tract infection; very rarely - acute renal failure.
On the part of laboratory parameters: very rarely - an increase in the level of creatinine and urea in the blood serum, an increase in the activity of liver enzymes.
From the side of the cardiovascular system: sometimes - angina pectoris, tachycardia; rarely - a marked decrease in blood pressure.
From the side of metabolism: often - an increase in the level of CPK, hypertriglyceridemia, hyperuricemia; rarely, hyperkalemia.
From the side of the body as a whole: often - chest pain, flu-like symptoms, peripheral edema; very rarely - asthenia, fatigue, malaise, drowsiness.
Contraindications for use
obstruction of the biliary tract;
renal failure (CC less than 20 ml / min), condition after kidney transplantation (no experience of clinical use);
lactase deficiency, galactosemia, or malabsorption syndrome;
pregnancy;
lactation period;
age up to 18 years (efficacy and safety have not been established);
hypersensitivity to the active substance or to any of the excipients that make up the drug.
The drug should be used with caution in the following conditions or diseases:
stenosis of the aortic or mitral valves;
hypertrophic obstructive cardiomyopathy;
primary aldosteronism;
hyperkalemia, hyponatremia (risk of dehydration, arterial hypotension, renal failure);
renal failure (CC more than 20 ml / min);
chronic heart failure;
bilateral stenosis of the renal arteries or stenosis of an artery of a solitary kidney;
Ischemic heart disease;
cerebrovascular diseases;
advanced age (over 65);
impaired liver function;
conditions accompanied by a decrease in BCC (including diarrhea, vomiting), as well as when following a diet with sodium restriction;
simultaneous use with diuretics.
Application during pregnancy and lactation
There is no experience with olmesartan medoxomil in pregnant women. However, in view of the existing reports of a severe teratogenic effect of drugs acting directly on the renin-angiotensin system, like any drug of this class, olmesartan is contraindicated during pregnancy. If pregnancy occurs during therapy with CardosalЃ, the drug must be canceled.
There is no data on whether olmesartan is excreted in breast milk, therefore, if it is necessary to use the drug CardosalЃ during lactation, breastfeeding should be discontinued for the period of taking the drug.
Application for violations of liver function
With care: impaired liver function.
Application for impaired renal function
With caution in case of impaired renal function, with CC <20 ml / min - contraindicated.
Use in elderly patients
Contraindicated in old age (over 65 years).
special instructions
Symptomatic arterial hypotension, especially after taking the first dose of the drug, can occur in patients with reduced BCC and / or reduced sodium levels due to intensive diuretic therapy, restriction of salt intake with food during dietary nutrition, and also due to diarrhea or vomiting. These factors should be eliminated before using CardosalЃ.
In patients in whom vascular tone and renal function depend to a large extent on the activity of the RAAS (for example, in patients with severe chronic heart failure or renal impairment, including renal artery stenosis), treatment with other drugs acting on this system is associated with the possibility of developing acute arterial hypotension, azotemia, oliguria, or, in rare cases, acute renal failure. The possibility of a similar effect cannot be excluded with the use of angiotensin II receptor antagonists.
There is an increased risk of severe arterial hypotension and renal failure if a patient with bilateral renal artery stenosis or arterial stenosis of a single functioning kidney is treated with drugs that affect the RAAS.
When using the drug CardosalЃ in patients with impaired renal function, it is recommended to periodically monitor the level of potassium and creatinine in the blood serum. There is no experience with the use of CardosalЃ in patients with recent kidney transplantation or in patients with the last stage of renal dysfunction (for example, CC less than 12 ml / min).
As with other angiotensin II receptor antagonists and ACE inhibitors, hyperkalemia may develop during treatment with CardosalЃ if the patient suffers from impaired renal function and / or chronic heart failure. In patients of this risk group, monitoring of serum potassium levels is recommended.
As with other angiotensin II receptor antagonists, the combination of lithium and CardosalЃ is not recommended.
ак и в случае других антагонистов рецепторов ангиотензина II, у пациентов негроидной расы, страдающих артериальной гипертензией, эффективность терапии препаратом ардосалЃ несколько ниже, чем у пациентов других рас.
ак в случае любого антигипертензивного средства, чрезмерное снижение ј? у пациентов с »Ѕ— или с цереброваскул¤рной недостаточностью может привести к инфаркту миокарда или инсульту.
¬ли¤ние на способность к вождению автотранспорта и управлению механизмами
¬ли¤ние препарата ардосалЃ на способность к вождению автотранспорта и управлению механизмами не изучалось, поэтому в период лечени¤ препаратом ардосалЃ следует соблюдать осторожность при вождении автотранспорта и зан¤ти¤х потенциально опасными видами де¤тельности, требующими повышенной концентрации внимани¤ и быстроты психомоторных реакций (возможны головокружение и слабость).
ѕередозировка
—имптомы: выраженное снижение ј?.
Ћечение: при выраженном снижении ј? рекомендуетс¤ уложить пациента на спину, приподн¤в ноги. –екомендовано промывание желудка и/или прием активированного угл¤, терапи¤, направленна¤ на коррекцию дегидратации и нарушений водно-солевого обмена, восполнение ќ? .
Ћекарственное взаимодействие
Ќе рекомендуетс¤ совместное применение с калийсберегающими диуретиками, препаратами кали¤, заменител¤ми солей, содержащих калий, или другими лекарственными средствами, способными повысить уровень кали¤ в сыворотке крови (например, гепарин), это может привести к повышению уровн¤ кали¤ в сыворотке крови.
јнтигипертензивный эффект от терапии олмесартаном может быть усилен при комбинированном применении с другими гипотензивными средствами.
Ќѕ¬—, включа¤ ацетилсалициловую кислоту в дозах более 3 г/сут, а также ингибиторы ?ќv-2, и антагонисты рецепторов ангиотензина II могут действовать синергично, уменьша¤ гломерул¤рную фильтрацию. ѕри одновременном применении Ќѕ¬ѕ и антагонистов рецепторов ангиотензина II может возникнуть риск развити¤ острой почечной недостаточности, поэтому рекомендуетс¤ контроль функции почек в начале лечени¤, а также регул¤рный прием достаточного количества жидкости. ¬месте с тем, одновременное лечение может уменьшить антигипертензивное действие антагонистов рецепторов ангиотензина II, привод¤ к частичной потере их терапевтической эффективности.
ѕри одновременном применении с антацидами (магни¤ и алюмини¤ гидроксид) возможно умеренное снижение биодоступности олмесартана.
There are reports of a reversible increase in the concentration of lithium in the blood serum and the manifestation of toxicity during the simultaneous use of lithium preparations with ACE inhibitors and angiotensin II receptor antagonists, therefore the use of olmesartan medoxomil in combination with lithium preparations is not recommended . If necessary, the use of appropriate combination therapy is recommended to regularly monitor the level of lithium in the blood serum.
Storage conditions
The drug should be stored out of the reach of children at a temperature not exceeding 30 ? C.
Shelf life
Shelf life is 3 years. Do not use after the expiration date printed on the package.
Terms of sale
The drug is available with a prescription.