Cardosal® 10 (Cardosal® 10)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceOlmesartan medoxomilOlmesartan medoxomil
Dosage form: & nbspfilm coated tablets.
Composition:1 tablet, film-coated, contains:
Core
Active substance: Olmesartan medoxomil - 10.00 mg;
Excipients: microcrystalline cellulose, giproloza (low-substituted), lactose monohydrate, giproloza (viscosity 6-10 mPa-s), the magnesium stearate. Sheath: titanium dioxide (E 171), talc, Hypromellose (viscosity 5mPas).

Description:white, round, biconvex tablets, film-coated, stamped with "03" on one side, with a barely perceptible characteristic odor.

Pharmacotherapeutic group:angiotensin II receptor antagonist
ATX: & nbsp

C.09.C.A.08   Olmesartan medoxomil

Pharmacodynamics:Olmesartan medoxomil - active substance preparation Kardosal® 10 - is a potent angiotensin II antagonist specific receptors (type for ATP ingestion Angiotensin II is the primary vasoactive hormone of the renin-angiotensin -. Aldosterone system plays a significant role in the pathophysiology of hypertension by acting on receptors ATG.It is assumed that olmesartan blocks all the actions of angiotensin II mediated by AT 1 -receptors, regardless of the source and the pathway of synthesis leads to an increase in the activity of renin, angiotensin I and II in blood plasma, and also helps to reduce the plasma concentration of aldosterone.
In arterial hypertension, olmesartan causes a dose-dependent prolonged decrease in arterial pressure (BP). There is no evidence of the development of arterial hypotension after taking the first dose of the drug, of tachyphylaxis during long-term treatment or of the "withdrawal" syndrome (a sharp increase in BP after drug withdrawal).
Taking olmesartan medoxomil once a day provides an effective and gentle decrease in blood pressure within 24 hours, the effect after a single dose is similar to the effect of taking the drug twice a day in the same daily dose.
The antihypertensive effect of olme-sartan develops, usually after 2 weeks, and the maximum effect develops approximately 8 weeks after the initiation of therapy.
Pharmacokinetics:Absorption and distribution:
Olmesartan medoxomil is a pro med.It quickly turns into pharmacologically active metabolite olmesartan under the action of enzymes in the intestinal mucosa and in portal blood during absorption from the gastrointestinal tract. Olmesartan medoxomil in unmodified form or with an intact fragment of medoxomil is not found in blood plasma and / or feces. The bioavailability of olmesartan is 25.6% on average. The maximum concentration (Stach) of olmesartan in blood plasma is on average 2 hours after taking olmesartan medoxomil by mouth and increases approximately linearly with a single dose increase to 80 mg.
The ingestion of food does not significantly affect the bioavailability of olmesartan, therefore olmesartan medoxomil can be taken regardless of food intake.
Clinically significant differences in pharmacokinetic parameters of olmesartan, depending on gender, are not evident.
Olmesartan binds to blood plasma proteins (99.7%), but the potential for clinically significant protein binding shifts in the interaction of olmesartan with other highly-linked and concomitantly used drugs is low (the absence of a clinically significant interaction between olmesartan and warfarin confirms this).The association of olmesartan with blood cells is negligible. The average volume of distribution after intravenous administration is low (16-29 L).
Metabolism and excretion: the total plasma clearance is usually 1.3 l / h (coefficient of variation -19%) and is relatively low in comparison with hepatic blood flow (approximately 90 l / h).
Elimination of olmesartan is carried out in two ways. After a single oral administration of olmesartan medoxomil labeled with 14C isotope, 10-16% of the radioactive substance was excreted by the kidneys (most within 24 hours after taking olmesartan medoxomil), and the remaining radioactive substance was released through the intestine. Taking into account the systemic bioavailability of 25.6%, it can be calculated that approximately 40% of the absorbed olmesartan is excreted through the kidneys, and about 60% through the hepatobiliary system. The released radioactive substance was represented by olmesartan. No other metabolites were detected. The intestinal and hepatic recirculation of olmesartan is minimal. Since most of the olmesartan is excreted through the liver, its use in patients with bile duct obstruction is contraindicated (see Contraindications section).The half-life of olmesartan is 10-15 hours after repeated ingestion.
A significant effect of therapy is achieved after the first few doses of the drug, and after 14 days of repeated use, further cumulation is not observed. Kidney clearance is approximately 0.5-0.7 l / h and does not depend on the dose of the drug.
In patients with impaired renal function, the area under the concentration-time curve (AUC) in a steady state was increased by approximately 62%, 82% and 179% in the case of mild, moderate and severe renal dysfunction, respectively, compared to healthy volunteers.
After a single oral intake, the AUC values ​​for olmesartan were 6 and 65% higher in patients with mild to moderate liver failure, respectively, compared to healthy volunteers. Unbound olmesartan fraction 2 hours after taking the dose of the drug in healthy volunteers, in patients with mild to moderate degrees of liver function impairment were 0.26, 0.34 and 0.41% respectively.
Indications:

Essential hypertension.

Contraindications:- Hypersensitivity to the active substance or to any of the excipients that make up the preparation (see section Composition);
- Obstruction of the biliary tract;
- renal failure (creatinine clearance less than 20 ml / min), condition after kidney transplantation (no clinical experience);
- pregnancy, lactation period; age under 18 years (effectiveness and safety not established);
- deficiency of lactase, galactosemia or Sindryum is small absorption.

Carefully:- stenosis of the aortic or mitral valves; hypertrophic obstructive cardiomyopathy;
- primary aldosteronism;
- Hyperkalemia, hyponatremia (risk of dehydration, arterial hypotension, renal failure);
- renal failure (QC more than 20 ml / min.);
- Chronic heart failure;
- bilateral stenosis of the renal arteries or stenosis of the artery of a single kidney;
- cardiac ischemia;
- cerebrovascular diseases;
- Older age (over 65 years);
- impaired liver function;
- conditions accompanied by a decrease in the volume of circulating blood (including diarrhea, vomiting), as well as in patients who follow a diet with sodium restriction;
- with simultaneous use with diuretics.
Pregnancy and lactation:The experience of using olmesartan medoxomil in pregnant women is absent. However, in view of the available reports of severe teratogenic effects of drugs acting directly on the renin-angiotensin system, like any medicinal product of this class, olmesartan is contraindicated during pregnancy. In case of pregnancy during treatment with Cardosal® 10, the drug should be discarded.
There is no data whether olmesartan is excreted in breast milk, so if you need Cardosal® 10 during lactation, breastfeeding for the period of taking the drug should be discontinued.
Dosing and Administration:It is recommended to take Cardosal * 10 inside every day at the same time, regardless of food intake.
The recommended initial dose of Cardosal® 10 for adults is 1 tablet (10 mg) once a day. In case of insufficient reduction of 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 (Cardosal * 20 can be used). If it is necessary to further reduce blood pressure, the dose of the drug can be increased to a maximum of 40 mg / day (Cardosal® 40 may be used) or an additional diuretichydrochlorothiazide).The maximum daily dose is 40 mg.
Side effects:Possible side effects are given below on the descending frequency of occurrence: very often (> 1/10); often (> 1/100 <1/10); sometimes (> 1/1000, <1/100); rarely (> 1/10000, <1/1000); very rarely (<1/10000), including individual messages.
From the blood and lymphatic system:
Very rarely: thrombocytopenia.
From the central nervous system:
Sometimes: dizziness.
Very rarely: headache.
From the respiratory system:
Often: pharyngitis, rhinitis.
Very rarely: cough, bronchitis.
From the digestive tract:
Often: diarrhea, indigestion, gastroenteritis.
Very rarely: pain in the abdomen, nausea, vomiting.
From the skin:
Very rarely: itchy skin, rash, angioedema, allergic dermatitis, urticaria.
From the side of 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.
From the laboratory indicators:
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 cardiovascular system:
Rarely: excessive decrease in blood pressure.
Sometimes: stenocardia, tachycardia.
From the side of metabolism:
Often: increased levels of creatine phosphokinase, hypertriglyceridemia, hyperuricemia. Rarely: hyperkalemia.
Other violations
Often: chest pain, flu-like symptoms, peripheral edema.
Very rarely: asthenia, fatigue, malaise, drowsiness.
Overdose:Symptoms: marked decrease in blood pressure.
Treatment: at the expressed depression of a BP it is recommended to lay the patient on a back, having lifted legs. Recommended gastric lavage and / or reception of activated charcoal, therapy aimed at correcting the dehydration and disturbances of water-salt metabolism, replenishment of the volume of circulating blood.
Interaction:It is not recommended to use together with potassium-sparing diuretics, potassium preparations, substitutes for salts containing potassium, or other drugs that can raise the level of potassium in the blood serum (for example, heparin), this can lead to increased serum potassium levels (see Special section instructions).
The anti-hypertensive effect of olmesartan therapy can be enhanced when combined with other antihypertensive agents.
Non-steroidal anti-inflammatory drugs (NSAIDs), including acetylsalicylic acid in doses greater than 3 g / day, as well as cyclooxygenase-2 (COX-2) inhibitors, and angiotensin II receptor antagonists can act synergistically, reducing glomerular filtration. With the simultaneous use of NSAIDs and angiotensin II receptor antagonists, there may be a risk of developing acute renal failure, so it is recommended that kidney function be monitored at the beginning of treatment and that a sufficient amount of fluid is taken regularly. However, simultaneous treatment can reduce the anti-hypertensive effect of angiotensin II receptor antagonists, leading to a partial loss of their therapeutic effectiveness.
When used simultaneously with antacids (magnesium and aluminum hydroxide), a moderate decrease in the bioavailability of olmesartan is possible.
There have been reports of a reversible increase in serum lithium concentration and toxicity during simultaneous use of lithium preparations with angiotensin converting enzyme (ACE) inhibitors and with angiotensin II receptor antagonists, so the use of olmesartan medoxomil in combination with lithium preparations is not recommended (see section Special instructions).If appropriate combination therapy is necessary, regular monitoring of serum lithium levels is recommended.
Special instructions:Symptomatic arterial hypotension, especially after taking the first dose of the drug, may occur in patients with reduced circulating blood volume and / or reduced sodium levels due to intensive diuretic therapy, restricting salt intake from food in dietary nutrition, and also due to diarrhea or vomiting. Corresponding factors should be eliminated before starting the use of Cardosal * 10.
In patients who have vascular tone and kidney function depend to a large extent on the activity of the renin-angiotensin-aldosterone system (for example, in patients with severe chronic heart failure or renal dysfunction, 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 can not be ruled out 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 stenosis of the artery of a single functioning kidney receives therapy with drugs that affect the renin-angiotensin-aldosterone system.
When using Cardosal® 10 in patients with renal dysfunction, periodic monitoring of serum levels of potassium and serum creatinine is recommended. The experience of using Cardosal * 10 in patients with recent kidney transplantation or in patients with the last stage of renal dysfunction (eg, KC less than 12 ml / min) is absent.
As with other angiotensin II receptor antagonists and ACE inhibitors, hyperkalemia may develop in the treatment with Cardosal® 10 if the patient suffers from renal dysfunction and / or chronic heart failure (see Interactions with Other Drugs). Patients at this risk group should be monitored for serum potassium levels.
As in the case of other angiotensin II receptor antagonists,a combination of lithium preparations and Cardosal® 10 preparation is not recommended (see Interactions with Other Drugs).
As in the case of other angiotensin II receptor antagonists, in Negroid patients with hypertension, the effectiveness of Cardosal® 10 treatment is slightly lower than in patients of other races.
As with any anti-hypertensive drug, excessive reduction in blood pressure in patients with coronary heart disease or with cerebrovascular insufficiency can lead to myocardial infarction or stroke.
Effect on the ability to drive transp. cf. and fur:The influence of Cardosal® 10 on the ability to drive vehicles and control mechanisms has not been studied, therefore, during the treatment with Cardosal® 10, caution should be exercised when driving vehicles and practicing potentially dangerous activities requiring increased concentration and speed of psychomotor reactions (dizziness and weakness are possible ).
Form release / dosage:Tablets, film-coated, 10 mg.
Packaging:For 14 tablets in a contour squeeze box (blister) made of laminated film (polyamide / aluminum / PVC) and aluminum foil.
For 1,2, 4 or 7 blisters together with instructions for use in a cardboard bundle.
Storage conditions:Store at temperatures not higher than 300 ° C.
Keep out of the reach of children!
Shelf life:3 years.
Do not use after the expiry date printed on the package.
Terms of leave from pharmacies:On prescription
Registration number:LSR-010758/09
Date of registration:29.12.2009
The owner of the registration certificate:Berlin-Chemie / Menarini Pharma, GmbH Berlin-Chemie / Menarini Pharma, GmbH Germany
Manufacturer: & nbsp
Information update date: & nbsp29.12.2009
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