Crestor tablets 20mg, No. 28

primary Fredrickson hypercholesterolemia (type IIa, including familial heterozygous hypercholesterolemia) or mixed hypercholesterolemia (type IIb) as an adjunct to diet when diet and other non-drug treatments (eg exercise, weight loss) are insufficient;

familial homozygous hypercholesterolemia as an adjunct to diet and other lipid-lowering therapy (eg LDL apheresis) or in cases where such therapy is not effective enough;

hypertriglyceridemia (Fredrickson type IV) as an adjunct to diet;

slowing the progression of atherosclerosis, as an addition to the diet in patients who are indicated for therapy to reduce the concentration of total cholesterol and LDL-C;

primary prevention of major cardiovascular complications (stroke, heart attack, arterial revascularization) in adult patients without clinical signs of coronary heart disease, but with an increased risk of its development (age over 50 for men and over 60 for women, increased concentration of C-reactive protein (?2 mg / L) in the presence of at least one of the additional risk factors, such as arterial hypertension, low concentration of HDL-C, smoking, family history of early onset of coronary heart disease).

Inside, without chewing or crushing the tablet, swallowing it whole with water. The drug can be prescribed at any time of the day, regardless of food intake.

Before starting therapy with CrestorЃ, the patient should begin to follow a standard cholesterol-lowering diet and continue to follow it during treatment. The dose of the drug should be selected individually, depending on the goals of therapy and the therapeutic response to treatment, taking into account the current recommendations for the target lipid concentration.

The recommended starting dose for patients starting to take the drug, or for patients transferred from taking other HMG-CoA reductase inhibitors, should be 5 or 10 mg of CrestorЃ once a day. When choosing an initial dose, one should be guided by the individual concentration of cholesterol and take into account the possible risk of cardiovascular complications, and it is also necessary to assess the potential risk of side effects. If necessary, the dose can be increased to a larger one after 4 weeks (see 'Pharmacodynamics').

In connection with the possible development of side effects when taking a dose of 40 mg, compared with lower doses of the drug (see 'Side Effects'), increasing the dose to 40 mg, after taking an additional dose above the recommended initial dose for 4 weeks of therapy, may carried out only in patients with severe hypercholesterolemia and a high risk of cardiovascular complications (especially in patients with familial hypercholesterolemia), who did not achieve the desired result of therapy when taking a dose of 20 mg, and who will be under the supervision of a specialist (see Special instructions'). Particularly careful monitoring of patients receiving the drug at a dose of 40 mg is recommended.

It is not recommended to prescribe a dose of 40 mg to patients who have not previously consulted a doctor. After 2Ц4 weeks of therapy and / or with an increase in the dose of CrestorЃ, it is necessary to monitor lipid metabolism (if necessary, dose adjustment is required).

Elderly patients. No dose adjustment required.

Patients with renal impairment. No dose adjustment is required in patients with mild to moderate renal impairment. In patients with severe renal insufficiency (Cl creatinine less than 30 ml / min), the use of CrestorЃ is contraindicated. The use of the drug at a dose of 40 mg is contraindicated in patients with moderate renal impairment (Cl creatinine 30-60 ml / min) (see 'Special instructions', 'Pharmacodynamics'). For patients with moderate renal impairment, an initial dose of 5 mg is recommended.

Patients with hepatic impairment. CrestorЃ is contraindicated in patients with active liver disease (see 'Contraindications').

Special populations

Ethnic groups. When studying the pharmacokinetic parameters of rosuvastatin in patients belonging to different ethnic groups, an increase in the systemic concentration of rosuvastatin in the Japanese and Chinese was noted (see 'Special instructions'). This fact should be taken into account when prescribing CrestorЃ to these groups of patients. When prescribing doses of 10 and 20 mg, the recommended starting dose for patients of the Mongoloid race is 5 mg. The appointment of the drug in a dose of 40 mg is contraindicated in patients of the Mongoloid race (see 'Contraindications').

Patients predisposed to myopathy. The appointment of the drug at a dose of 40 mg is contraindicated in patients with factors that may indicate a predisposition to the development of myopathy (see 'Contraindications'). When prescribing doses of 10 and 20 mg, the recommended initial dose for this group of patients is 5 mg (see 'Contraindications').

Film-coated tablets

active substance: rosuvastatin

Tablets, 5, 10 and 20 mg:

hypersensitivity to rosuvastatin or any of the components of the drug;

liver disease in the active phase, including a persistent increase in serum transaminase activity and any increase in serum transaminase activity (more than 3 times compared with VGN);

severe renal dysfunction (Cl creatinine less than 30 ml / min);

myopathy;

concomitant use of cyclosporine;

in women: pregnancy, lactation, lack of adequate contraceptive methods;

patients prone to the development of myotoxic complications;

lactose intolerance, lactase deficiency or glucose-galactose malabsorption (the drug contains lactose).

Tablets, 40 mg:

hypersensitivity to rosuvastatin or any of the components of the drug;

concomitant use of cyclosporine;

in women: pregnancy, lactation, lack of adequate contraceptive methods;

liver disease in the active phase, including a persistent increase in serum transaminase activity and any increase in serum transaminase activity (more than 3 times compared with VGN);

patients with risk factors for the development of myopathy / rhabdomyolysis, namely:

- Renal failure of moderate severity (Cl creatinine less than 60 ml / min);

- hypothyroidism;

- personal or family history of muscle disease;

- myotoxicity while taking other inhibitors of HMG-CoA reductase or fibrates in history;

excessive alcohol consumption;

conditions that can lead to an increase in the plasma concentration of rosuvastatin;

simultaneous reception of fibrates;

patients of the Asian race;

lactose intolerance, lactase deficiency or glucose-galactose malabsorption (the drug contains lactose).

Carefully

Tablets, 10 and 20 mg: risk of myopathy / rhabdomyolysis - renal failure, hypothyroidism, personal or family history of hereditary muscle diseases and a previous history of muscle toxicity when using other HMG-CoA reductase inhibitors or fibrates; excessive alcohol consumption; age over 65; conditions in which an increase in the plasma concentration of rosuvastatin is noted; race (Asian race); simultaneous appointment with fibrates (see 'Pharmacokinetics'); history of liver disease; sepsis; arterial hypotension; major surgery, trauma, severe metabolic, endocrine, or electrolyte disturbances, or uncontrolled seizures.

Tablets, 40 mg: renal failure of mild severity (Cl creatinine more than 60 ml / min); age over 65; history of liver disease; sepsis; arterial hypotension; major surgery, trauma, severe metabolic, endocrine, or electrolyte disturbances, or uncontrolled seizures.

Application in pediatric practice

The efficacy and safety of the drug in children under 18 years of age has not been established. The experience of using the drug in pediatric practice is limited to a small number of children (8 years and older) with familial homozygous hypercholesterolemia. Currently, it is not recommended to use CrestorЃ in children under 18 years of age.

Patients with hepatic impairment

There are no data or experience of using the drug in patients with a score above 9 on the Child-Pugh scale (see 'Pharmacodynamics', 'Special instructions').

Crestor inhibits HMG-CoA reductase, an enzyme that controls the production of mevalonate, a precursor of cholesterol. Rosuvastatin works in the liver, one of the main target organs. Statin reduces the amount of low and very low density lipoproteins by suppressing their synthesis, as well as the production of additional HDL for the uptake and catabolism of LDL. As a result, the level of total cholesterol, LDL and triglycerides decreases. At the same time, the concentration of HDL increases. Rosuvastatin is effective for hypercholesterolemia with or without hypertriglyceridemia for Crestor patients of any gender, age and race. The effect of the use of Crestor, judging by the reviews of the research participants, is observed by the end of the first week of the course, but the maximum result (over 90%) can be seen only after 2-4 weeks of regular use. Unlike some analogues,Crestor has a minimal negative effect on the liver. It is used in combination with a low-cholesterol diet and other cholesterol-lowering medications.

Pharmacokinetics: -
Absorption. The highest content of statin in blood plasma is observed 5 hours after internal use. The bioavailability of the drug is up to 20%.
-Distribution. The crestor mainly captures the liver - the main organ where cholesterol is produced and LDL is cleared. Its distribution volume is 134 liters. Up to 90% of drugs bind blood proteins, mainly albumin.
-Crestor's metabolism is insignificant (up to 10%). The share of rosuvastatin accounts for over 90% of the activity of a circulating inhibitor of HMG-CoA reductase.
- Withdrawal. The body removes up to 90% of the drug Crestor from the intestines with feces, the remains are removed with urine. The half-life does not depend on the dosage and is 19 hours.
-Special categories of patients. Age or gender does not affect statin pharmacokinetics. There were no clinically significant differences between the representatives of the European and Negroid races, while among the inhabitants of the Asian continent (Chinese, Japanese, Vietnamese, Filipinos) AUC and C max were twice as high. Pharmacokinetic parameters in children with heterozygous familial hypercholesterolemia have not been fully determined. There were no changes in statin levels in patients with mild to moderate renal failure. In severe cases, the content of rosuvastatin in the plasma increased 3 times, the metabolite - 9 times compared with the control group of healthy volunteers. When examining patients with liver pathologies, no changes were detected during treatment with rosuvastatin in individuals whose condition was assessed up to 7 points on the Child-Pugh scale.The experience of Krestor's treatment of patients with severe forms is not reflected.

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