Cardosal 40 - Instructions For Use, Price, Reviews, Analogs Of Tablets

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Cardosal 40

Cardosal 40: instructions for use and reviews

1. 1. Release form and composition
2. 2. Pharmacological properties
3. 3. Indications for use
4. 4. Contraindications
5. 5. Method of application and dosage
6. 6. Side effects
7. 7. Overdose
8. 8. Special instructions
9. 9. Application during pregnancy and lactation
10. 10. Use in childhood
11. 11. In case of impaired renal function
12. 12. For violations of liver function
13. 13. Use in the elderly
14. 14. Drug interactions
15. 15. Analogs
16. 16. Terms and conditions of storage
17. 17. Terms of dispensing from pharmacies
18. 18. Reviews
19. 19. Price in pharmacies

Latin name: Cardosal 40

ATX code: C09CA08

Active ingredient: olmesartan medoxomil (Olmesartani medoxomilum)

Producer: Berlin-Chemie AG (Berlin-Chemie AG) (Germany)

Description and photo update: 2019-12-07

Prices in pharmacies: from 562 rubles.

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Cardosal 40 is an angiotensin II receptor antagonist (ARA II).

Release form and composition

Dosage form - film-coated tablets: biconvex, oval, white, with a subtle specific odor; on one of the sides there is an imprint "C15" (in a cardboard box 1, 2, 4 or 7 blisters containing 14 tablets each, and instructions for use of Cardosal 40).

Composition of 1 tablet:

• active substance: olmesartan medoxomil - 40 mg;
• auxiliary components: magnesium stearate - 3.6 mg; hyprolosis (viscosity from 6 to 10 mPahs) - 10 mg; lactose monohydrate - 264.4 mg; hyprolosis (with a low degree of substitution) - 80 mg; microcrystalline cellulose - 40 mg;
• film shell: hypromellose (viscosity 5 mPahs) - 8.64 mg; talc - 1.68 mg; titanium dioxide (E 171) - 1.68 mg.

Pharmacological properties

Pharmacodynamics

The active substance of Cardosal 40 - olmesartan medoxomil - is a powerful specific ARA II (type AT ₁) intended for oral administration. In turn, angiotensin II is the primary vasoactive hormone of the renin-angiotensin-aldosterone system (RAAS), which plays an important role in the pathophysiology of hypertension by acting on AT ₁ receptors.

There are suggestions that regardless of the source and route of synthesis of angiotensin II, all of its actions mediated by AT ₁ receptors are blocked by olmesartan. Its specific antagonism against angiotensin II (type AT ₁) contributes to a decrease in the plasma concentration of aldosterone, an increase in the activity of angiotensin I / II and renin in the blood plasma.

Against the background of arterial hypertension, taking the drug leads to a dose-dependent long-term decrease in blood pressure (BP).

There is no evidence confirming the occurrence of arterial hypotension after taking the first dose of the drug, the development of tachyphylaxis during the period of prolonged therapy or withdrawal syndrome (a sharp increase in blood pressure after the abolition of Cardosal 40).

The use of the drug once a day provides a mild and effective decrease in blood pressure for 24 hours, and the effect after a single dose is similar to that after taking the drug 2 times a day at the same daily dose.

Usually, after 14 days, the antihypertensive effect of olmesartan develops, and the maximum effect is noted after 56 days from the start of treatment.

Pharmacokinetics

Olmesartan medoxomil is a prodrug. Under the action of enzymes in the intestinal mucosa, as well as in the portal blood during absorption from the gastrointestinal tract, it is rapidly converted into a pharmacologically active metabolite - olmesartan. With an intact fragment of medoxomil or unchanged olmesartan, medoxomil is not detected either in feces or in blood plasma.

On average, the bioavailability of the metabolite is 25.6%, and the maximum concentration in blood plasma is reached after 2 hours after oral administration of the drug and increases approximately linearly with an increase in a single dose to 80 mg. The bioavailability of the metabolite does not depend on food intake, so the drug can be taken regardless of food. The pharmacological parameters of olmesartan do not have clinically significant differences between men and women.

The binding of olmesartan to blood plasma proteins is 99.7%, but the potential for a clinically significant shift in the value of binding to proteins when the metabolite interacts with other highly binding and concomitantly used drugs is low. This is supported by the absence of a clinically significant interaction between olmesartan and warfarin. The connection of the metabolite with blood cells is insignificant. After intravenous administration of the drug, the average volume of distribution is low and ranges from 16 to 29 liters.

Typically, the total plasma clearance is 1.3 L in 1 h (coefficient of variation - 19%) and is relatively low compared to hepatic blood flow (approximately 90 L in 1 h).

Olmesartan is eliminated in two ways. After a single oral administration of a drug labeled with an isotope ¹⁴ C, kidneys were allocated from 10 to 16% of the radioactive substance (represented metabolite), and the rest - the intestine. Taking into account that the systemic bioavailability of the metabolite is 25.6%, it can be concluded that after absorption, it is excreted by approximately 40% through the kidneys, and 60% through the hepatobiliary system. Enterohepatic metabolite recirculation is minimal. Since most of it is excreted by the liver, taking the drug is contraindicated in case of obstruction of the biliary tract.

After repeated oral administration, the half-life of olmesartan varies from 10 to 15 hours. After taking the first few doses of Cardosal 40, an equilibrium state is reached and after 2 weeks of use, no further cumulation is observed.

Regardless of the dose of the drug, renal clearance is approximately 0.5 to 0.7 liters per hour.

Pharmacokinetics in special cases:

• renal failure: the area under the concentration-time curve (AUC) in mild, moderate or severe renal failure at steady state, compared with healthy volunteers, increased by about 62, 82 or 179%, respectively;
• hepatic impairment: AUC values for olmesartan after a single oral dose in mild to moderate hepatic impairment, compared with healthy volunteers, were higher by 6 or 65%, respectively. After 2 hours after taking Cardosal 40, the unbound fraction of the metabolite in healthy volunteers, patients with mild and moderate hepatic insufficiency was 0.26; 0.34 and 0.41%, respectively. The AUC for the metabolite after repeated oral administration in patients with moderate hepatic impairment, compared with healthy volunteers, was 65% higher. The average values of the maximum concentration of olmesartan in blood plasma in hepatic insufficiency are similar to those in healthy volunteers. Pharmacokinetics of the drug in severe hepatic failure has not been studied;
• elderly age: the AUC of the metabolite in an equilibrium state in elderly patients (from 65 to 75 years) and senile (from 75 years) age with arterial hypertension was 35 and ~ 44% higher, respectively, in comparison with younger patients. This may in part be due to age-related declines in kidney function.

Indications for use

Cardosal 40 is prescribed for the treatment of essential hypertension.

Contraindications

Absolute:

• severe liver failure (on the Child-Pugh scale> 9 points);
• severe renal failure (creatinine clearance <20 ml per minute);
• condition after kidney transplantation;
• obstruction of the biliary tract;
• galactose / glucose malabsorption syndrome, lactase deficiency, hereditary galactose intolerance;
• combined treatment with aliskiren and drugs containing aliskiren against the background of impaired renal function (creatinine clearance <60 ml per minute) and / or diabetes mellitus;
• pregnancy;
• lactation period;
• age under 18;
• individual intolerance to the components of the drug.

Relative (Cardosal 40 is prescribed under medical supervision):

• liver failure of moderate severity (on the Child - Pugh scale <9 points);
• renal failure of mild to moderate severity (creatinine clearance> 20 ml in 1 min);
• mitral or aortic valve stenosis;
• primary aldosteronism;
• hypertrophic obstructive cardiomyopathy;
• hypo- and hyperkalemia;
• chronic heart failure;
• renovascular hypertension (stenosis of an artery of a single kidney or bilateral stenosis of the renal arteries);
• cardiac ischemia;
• cerebrovascular diseases;
• conditions that are accompanied by a decrease in circulating blood volume, including vomiting and diarrhea;
• adherence to a diet with limited consumption of table salt;
• combined therapy with diuretics, lithium preparations;
• advanced age (over 65).

Cardosal 40, instructions for use: method and dosage

Tablets Cardosal 40 are taken orally, regardless of food, without chewing, 1 time a day at the same time, washed down with water (in sufficient quantity).

The dosage regimen is selected individually. It is most advisable to prescribe tablets in a suitable dosage - 10, 20 or 40 mg (it is possible to use Cardosal 10, Cardosal 20 or Cardosal 40, respectively).

It is recommended to start therapy with a dose of olmesartan medoxomil - 10 mg once a day. If blood pressure does not decrease enough, the dose can be increased by 2 times, and if necessary, by 4 times. The maximum dose is 40 mg per day.

Therapy in elderly patients (over the age of 65) should be carried out under close control of blood pressure.

In renal failure of mild and moderate severity (creatinine clearance varies from 20 to 60 ml per minute), the maximum dose of the drug is 20 mg per day. The appointment of Cardosal 40 in severe renal failure (creatinine clearance <20 ml / min) is contraindicated.

Correction of the dosage regimen for patients with mild hepatic insufficiency is not carried out. In cases of moderate hepatic insufficiency, therapy begins with a dose of 10 mg per day. The maximum dose is 20 mg per day.

Combined treatment with diuretics and / or other antihypertensive drugs in liver failure is recommended under close monitoring of renal function and blood pressure. In severe hepatic failure and obstruction of the biliary tract, the appointment of the drug is contraindicated.

Side effects

Possible adverse reactions (> 10% - very common;> 1% and 0.1% and 0.01% and <0.1% - rarely; <0.01%, including isolated messages - very rare):

• blood and lymphatic system: infrequently - thrombocytopenia;
• nervous system: often - headache, dizziness;
• organ of hearing and labyrinthine disorders: infrequently - vertigo;
• respiratory system, chest and mediastinal organs: often - cough, bronchitis, rhinitis, pharyngitis;
• digestive tract: often - nausea, abdominal pain, gastroenteritis, dyspepsia, diarrhea; infrequently - vomiting;
• skin and subcutaneous tissues: infrequently - itchy skin / rash, urticaria, allergic dermatitis, exanthema; rarely - angioedema;
• musculoskeletal system: often - arthritis, bone / back pain; infrequently - myalgia; rarely - muscle cramps;
• kidneys and urinary tract: often - urinary tract infection, hematuria; rarely - renal failure, including the acute form;
• cardiovascular system: infrequently - angina pectoris; rarely - a pronounced decrease in blood pressure (in elderly patients, the incidence of arterial hypertension is slightly higher - from rare to infrequent);
• metabolism and nutrition: often - an increase in the concentration of uric acid in the blood, triglycerides in the blood plasma; rarely - an increase in the concentration of potassium in the blood;
• immune system: infrequently - anaphylactic reactions;
• general disorders: often - weakness, flu-like symptoms, peripheral edema, chest pain; infrequently - malaise, asthenia, swelling of the face; rarely - drowsiness;
• other disorders: often - an increase in the concentration of creatine phosphokinase, urea in the blood plasma, an increase in the activity of liver enzymes; rarely - an increase in the concentration of creatinine in the blood plasma; very rarely - rhabdomyolysis (its development was associated with the use of AT-II receptor antagonists).

Overdose

Data on an overdose of olmesartan medoxomil are limited.

The main symptoms: a marked decrease in blood pressure.

Therapy: the patient should be laid in a horizontal position with the lower limbs raised. Recommended gastric lavage and / or the use of activated charcoal, the appointment of treatment aimed at replenishing the volume of circulating blood, correction of dehydration and violations of water and electrolyte metabolism. The use of dialysis to eliminate olmesartan has not been studied.

special instructions

The development of symptomatic arterial hypotension, especially after taking the first dose of the drug, can be observed in patients with low sodium levels (due to vomiting, diarrhea, adherence to a diet with limited salt intake, taking diuretics) or circulating blood volume. These factors must be eliminated before starting therapy with Cardosal 40.

The use of other drugs affecting the RAAS in patients whose renal function and vascular tone are highly dependent on the activity of this system, for example, with impaired renal function (including renal artery stenosis), severe chronic heart failure, is associated with the risk of oliguria, azotemia, arterial hypotension and, in rare cases, acute renal failure. A similar effect can take place when using ARA II.

The likelihood of severe arterial hypotension and renal failure is increased in patients with arterial stenosis of a single functioning kidney or bilateral renal artery stenosis receiving drugs that affect the RAAS.

Treatment with Cardosal 40 for impaired renal function should be carried out under periodic monitoring of the content of creatinine and potassium in the blood plasma. There is no experience with the use of the drug after a recent kidney transplant or in end-stage renal disease (for example, creatinine clearance <12 ml per minute).

Against the background of therapy with ARA II or ACE inhibitors, hyperkalemia may occur, in some cases leading to death. The likelihood of its development increases in the following cases:

• combined treatment with drugs that increase the content of potassium in the blood plasma;
• elderly age;
• renal failure, including the progression of the disease, acute impairment of renal function (for example, with infectious pathologies);
• diabetes;
• dehydration;
• acute decompensation of cardiac activity;
• metabolic acidosis;
• conditions accompanied by massive cell lysis (for example, extensive trauma, rhabdomyolysis, acute limb ischemia).

In patients belonging to this risk group, the content of potassium in the blood plasma should be monitored.

Before prescribing 40 other drugs that affect the RAAS in combination with Cardosal, it is recommended to compare the intended benefits with the potential risks of this combination and consider other therapy options.

Cardosal 40, like other ARA II, is not recommended to be used in combination with products containing lithium.

The therapeutic effect of the drug, like other ARA IIs, in representatives of the Negroid race with arterial hypertension is somewhat lower than in individuals from other populations. This may be due to the greater prevalence of low plasma renin activity in patients belonging to this race.

Excessive lowering of blood pressure with cerebrovascular insufficiency or coronary heart disease while taking pills can cause a stroke or myocardial infarction.

Due to the content of lactose 40 in Cardosal, its use is contraindicated in glucose / galactose malabsorption syndrome, lactase deficiency and hereditary galactose intolerance.

Influence on the ability to drive vehicles and complex mechanisms

Due to the fact that taking Cardosal 40 can lead to the development of weakness and drowsiness, patients during the period of therapy are advised to be careful when driving and conducting potentially hazardous activities.

Application during pregnancy and lactation

Cardosal 40 is not prescribed during pregnancy due to the lack of experience with its use in patients in such cases and the presence of reports of severe teratogenic effects of drugs that directly affect the RAAS. If pregnancy occurs during the period of drug treatment, it is immediately canceled and, if necessary, alternative therapy is prescribed.

When planning a pregnancy, the patient is recommended to transfer to antihypertensive drugs of other groups that are safe to use during this period. An exception are cases when ARA II are prescribed for health reasons.

If the use of ARA II is necessary in the II and III trimesters of pregnancy, it is important to conduct an ultrasound examination to assess the ossification of the skull bones and the function of the fetal kidneys. Newborns whose mothers received ARA II should be monitored for potential renal impairment or hypertension.

Studies conducted have confirmed the ability of olmesartan to penetrate into the breast milk of rats (there are no similar data for humans). If it is necessary to use Cardosal 40 during lactation, breastfeeding is stopped.

Pediatric use

Patients under the age of 18 are not prescribed Cardosal 40.

With impaired renal function

• use is contraindicated: severe renal failure, condition after kidney transplantation;
• application requires medical supervision: stenosis of the artery of a single kidney, bilateral stenosis of the renal arteries (renovascular hypertension).

For violations of liver function

• the appointment is contraindicated: severe liver failure;
• use requires caution: liver failure of moderate severity.

Use in the elderly

For patients over the age of 65, Cardosal 40 is prescribed with caution.

Drug interactions

Possible interactions of olmesartan medoxomil with other drugs / substances:

• salt substitutes containing potassium, potassium preparations, potassium-sparing diuretics, other drugs that increase the level of potassium in the blood plasma [for example, heparin, angiotensin-converting enzyme inhibitors (ACE inhibitors), trimethoprim, immunosuppressants (tacrolimus, cyclosporine, etc.), anti-inflammatory drugs, including selective inhibitors of cyclooxygenase-2]: an increase in the content of potassium in the blood is possible (the use of such combinations is not recommended);
• antihypertensive drugs: the antihypertensive effect of treatment may increase;
• non-steroidal anti-inflammatory drugs, including acetylsalicylic acid in a daily dose of> 3 g, cyclooxygenase-2 inhibitors: in combination with ARA II, they can act synergistically, reducing glomerular filtration, serve to reduce the antihypertensive effect of ARA II and cause a partial loss of their therapeutic efficacy, lead to the risk of developing acute renal failure (it is recommended to take a sufficient amount of fluid, control kidney function at the beginning of therapy);
• antacids (aluminum / magnesium hydroxide): the bioavailability of the drug may moderately decrease.

When combined treatment with lithium preparations with ACE inhibitors and ARA II, a reversible increase in the concentration of lithium in the blood serum and the manifestation of toxicity were reported. In this regard, the use of Cardosal 40 in combination with lithium preparations is not recommended. If the use of such a combination is necessary, the concentration of lithium in the blood serum is regularly monitored.

According to the data of clinical studies, double blockade of the RAAS with the combined use of aliskiren, ARA II or ACE inhibitors is associated with a higher incidence of side effects manifested by a decrease in renal function, including the occurrence of acute renal failure, hyperkalemia and arterial hypotension, compared with the use of only one drug means that have an impact on the RAAS. In this regard, the combination therapy with aliskiren, ARA II or ACE inhibitors is not recommended.

Olmesartan medoxomil is contraindicated to prescribe simultaneously with drugs that include aliskiren in renal failure (glomerular filtration rate <60 ml per minute per 1 m ²) and diabetes mellitus. In diabetic nephropathy, the use of ACE inhibitors and ARA II is not recommended.

If it is necessary to use two drugs that affect the RAAS, the patient must be under close medical supervision. Regular monitoring of plasma electrolytes, blood pressure and renal function is also required.

In vitro studies did not reveal a clinically significant inhibitory effect of olmesartan on isozymes 1A1, 1A2, 2A6, 2C8, 2C9, 2C19, 2D6, 2E1 and ZA4 of human cytochrome P ₄₅₀. In relation to rat cytochrome P _{450, the} inducing effect was zero or minimal. Based on these data, it can be assumed that there are no clinically significant interactions between olmesartan medoxomil and drugs metabolized with the participation of these cytochrome P ₄₅₀ isoenzymes.

Cardosal 40 has no clinically significant effect on the pharmacokinetics and pharmacodynamics of antacids (aluminum / magnesium hydroxide), pravastatin, hydrochlorothiazide, digoxin, and warfarin.

Analogs

The analogues of Cardosal 40 are: Cardosal 10, Olymestra, Cardosal 20.

Terms and conditions of storage

Store in a place protected from light and moisture at temperatures up to 30 ° C. Keep out of the reach of children.

The shelf life is 3 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews for Cardosal 40

According to reviews, Cardosal 40 is a safe and effective drug that stabilizes blood pressure. The drug does not cause side effects with prolonged use.

Price for Cardosal 40 in pharmacies

The approximate price of Cardosal 40 (28 tablets in a package) varies from 685 to 890 rubles.

Cardosal 40: prices in online pharmacies

Drug name Price Pharmacy

Cardosal 40 40 mg film-coated tablets 28 pcs. 562 r Buy

Maria Kulkes Medical journalist About the author

Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!