Rosuvastatin-SZ tablets coated. 40 mg, 30 pcs. (rosuvastatin)

Pharmacological action of

Pharmacodynamics:

Rosuvastatin-SZ lowers elevated concentrations of LDL cholesterol (cholesterol-LDL), total cholesterol, triglycerides (TG), increases the concentration of high-density cholesterol-lipoprotein L and Apolipopole, cholesterol-L B (ApoV), cholesterol-free cholesterol, cholesterol-VLDL, TG-VLDL and increases the concentration of apolipoprotein A-I (ApoA-I), reduces the ratio of cholesterol-LDL / cholesterol-HDL, total cholesterol / cholesterol-HDL and cholesterol-non-HDLP / cholesterol-HDL and the ratio of ApoV / ApoA-I.

The therapeutic effect develops within one week after the start of therapy with the drug Rosuvastatin-SZ, after 2 weeks of treatment reaches 90% of the maximum possible effect. The maximum therapeutic effect is usually achieved by the 4th week of therapy and is maintained with regular use of the drug.

Rosuvastatin-SZ is effective in adult patients with hypercholesterolemia with or without hypertriglyceridemia, regardless of race, gender or age, including patients with diabetes mellitus and familial hypercholesterolemia.

In 80% of patients with type IIa and IIb hypercholesterolemia according to Fredrickson (the average initial concentration of LDL-C is about 4.8 mmol / L) while taking the drug at a dose of 10 mg, the concentration of LDL-C reaches less than 3 mmol / L.

In patients with heterozygous familial hypercholesterolemia receiving Rosuvastatin-C3 at a dose of 20-80 mg, a positive dynamics of lipid profile is observed. After titration to a daily dose of 40 mg (12 weeks of therapy), a decrease in the concentration of LDL-C by 53% is noted. In 33% of patients, an LDL-C concentration of less than 3 mmol / L is achieved.

In patients with homozygous familial hypercholesterolemia taking Rosuvastatin-SZ at a dose of 20 mg and 40 mg, the average decrease in the concentration of LDL-C is 22%.

In patients with hypertriglyceridemia with an initial TG concentration of 273 to 817 mg / dl, treated with rosuvastatin-C3 at a dose of 5 mg to 40 mg once a day for 6 weeks, the concentration of TG in the blood plasma was significantly reduced.

The additive effect is observed in combination with fenofibrate in relation to the content of triglycerides and with nicotinic acid in lipid lowering doses in relation to the content of HDL-C (see also the section "Special Instructions").

According to the results of clinical studies, patients with severe hypercholesterolemia and a high risk of cardiovascular disease (CVD) should be prescribed a dose of 40 mg of Rosuvastatin-SZ.

Results from a clinical study (The rationale for using statins for primary prevention: an interventional study evaluating rosuvastatin) showed that rosuvastatin significantly reduced the risk of developing cardiovascular complications.

Pharmacokinetics:

Absorption and distribution of

The maximum concentration of rosuvastatin in blood plasma is reached approximately 5 hours after ingestion. Absolute bioavailability is approximately 20%.

Rosuvastatin is metabolized mainly by the liver, which is the main site of cholesterol synthesis and metabolism of LDL-C. The volume of distribution of rosuvastatin is approximately 134 liters. Approximately 90% of rosuvastatin binds to plasma proteins, mainly albumin.

Metabolism

Undergoes limited metabolism (about 10%). Rosuvastatin is a non-core substrate for metabolism by enzymes of the cytochrome P450 system. The main isoenzyme involved in the metabolism of rosuvastatin is the isoenzyme CYP2C9. The isoenzymes СYР2С19, СЫРЗА4, and CYP2D6 are less involved in metabolism.

The main identified metabolites of rosuvastatin are N-desmethyltrosrosuvastatin and lactone metabolites. N-desmethylrozuvastatin is approximately 50% less active than rosuvastatin, lactone metabolites are pharmacologically inactive. More than 90% of the pharmacological activity in inhibiting circulating HMG-CoA reductase is provided by rosuvastatin, the rest is metabolites.

Excretion of

About 90% of the dose of rosuvastatin is excreted unchanged through the intestines (including absorbed and unabsorbed rosuvastatin). The rest is excreted by the kidneys. The plasma half-life (T1 / 2) is approximately 19 hours. The half-life does not change with an increase in the dose of the drug. The geometric mean plasma clearance is approximately 50 l / h (coefficient of variation 21.7%). As with other HMG-CoA reductase inhibitors, the membrane carrier of cholesterol is involved in the process of “hepatic” uptake of rosuvastatin, playing an important role in the hepatic elimination of rosuvastatin.

Linearity

Systemic exposure of rosuvastatin increases in proportion to dose. Pharmacokinetic parameters do not change with daily use.

Special patient populations

Age and gender

Sex and age do not have a clinically significant effect on the pharmacokinetics of rosuvastatin.

Ethnic groups

Pharmacokinetic studies showed an approximately twofold increase in the median AUC (area under the concentration-time curve) and Cmax (maximum plasma concentration) of rosuvastatin in patients of the Mongoloid race (Japanese, Chinese, Filipinos, Vietnamese and Koreans) compared with Caucasians in Indians showed an increase in the median AUC and Cmax by 1.3 times. Pharmacokinetic analysis did not reveal clinically significant differences in pharmacokinetics among Caucasians and representatives of the Negroid race.

Renal failure

In patients with mild to moderate renal failure, the plasma concentration of rosuvastatin or N-desmethylrose-vastatin does not change significantly. In patients with severe renal failure (creatinine clearance (CC) less than 30 ml / min.), The concentration of rosuvastatin in blood plasma is 3 times higher, and the concentration of N-desmethylrosezuvastatin is 9 times higher than in healthy volunteers. The plasma concentration of rosuvastatin in hemodialysis patients was approximately 50% higher than in healthy volunteers.

Hepatic insufficiency

Patients with various stages of liver failure did not show an increase in the half-life of rosuvastatin in

patients with 7 points or lower on the Child-Pugh scale. Two patients with 8 and 9 points on the Child-Pugh scale showed an increase in half-life by at least 2 times. There is no experience with rosuvastatin in patients with more than 9 Child-Pugh scores.

Indications

Primary Frederickson's hypercholesterolemia (type IIa, including familial heterozygous hypercholesterolemia) or mixed hypercholesterolemia (type IIb) as a supplement to diet, when diet and other non-drug methods of treatment (for example, physical exercises, are insufficient,

Familial homozygous hypercholesterolemia as a supplement to diet and other lipid lowering therapy (e.g., LDL apheresis), or in cases when such therapy is not effective enough.

Hypertriglyceridemia (type IV according to Fredrickson) as a supplement to the diet.

Primary dysbetalipoproteinemia (Frederickson type III) as a supplement to the diet.

To slow the progression of atherosclerosis as a supplement to the diet in patients whotherapy is indicated for lowering the concentration of total cholesterol and cholesterol-LDL.

Primary prevention of major cardiovascular complications (stroke, heart attack, arterial revascularization) in adult patients without clinical signs of coronary artery disease, but with an increased risk of its development (over 50 years old for men and over 60 years old 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

Contraindications

hypersensitivity to rosuvastatin or any of the components of the

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

early pregnancy, maternal pregnancy, concomitant pregnancy adequate methods of contraception

increase in the concentration of creatine phosphokinase (CPK) in the blood by more than 5 times compared with the upper limit of normal

combined use with ibitorami HIV protease

renal failure secondary to severe (CC less than 60 ml / min.)

liver disease in its active phase, including a persistent increase in serum transaminase activity and any increase in serum transaminase activity (more than 3 times compared with the upper limit of normal) for patients with risk factors for myopathy / rhabdomyolysis, namely hypothyroidism

myotoxicity while taking other HMG-CoA inhibitors -reductase or fibrate history of

excessive alcohol consumption

conditions that can lead to increased plasma concentrations of rosuvastatin

concurrent administration of

fibrates myopathy

personal or a family history of

muscle disease in patients of the Mongoloid race

Caution:

mild renal failure (CC> 60 ml / min) over 65 years of history of liver disease sepsis arterial hypotension extensive surgery, injuries, severe metabolic, endocrine or electrolyte disturbances or uncontrolled seizures.

Concomitant use with colchicine and with ezetimibe (see section "Interaction with other drugs").

Use during pregnancy and lactation

Rosuvastatin-SZ is contraindicated in pregnancy and during breastfeeding. Women of reproductive age should use adequate methods of contraception. Since cholesterol and other cholesterol biosynthesis products are important for fetal development, the potential risk of inhibiting HMG-CoA reductase exceeds the benefits of using the drug in pregnant women. In case of pregnancy during treatment, the drug should be stopped immediately.

No data are available on the excretion of rosuvastatin in breast milk, therefore, during the period of breastfeeding, the drug should be discontinued (see section "Contraindications").

Special instructions

Renal effects of

In patients who received high doses of rosuvastatin-C3 (mainly 40 mg), tubular proteinuria was observed, which in most cases was transient. Such proteinuria did not indicate acute kidney disease or progression of kidney disease. In patients taking the drug at a dose of 40 mg, it is recommended to monitor renal function indicators during treatment.

From the musculoskeletal system

When using the drug Rosuvastatin-SZ in all doses and, in particular when taking doses of the drug in excess of 20 mg, the following effects on the musculoskeletal system were reported: myalgia, myopathy, in rare cases, rhabdomyolysis.

Determination of creatine phosphokinase

Determination of CPK activity should not be carried out after intense physical activity or if there are other possible reasons for the increase in CPK activity, which may lead to an incorrect interpretation of the results. If the initial activity of CPK is significantly increased (5 times higher than the upper limit of the norm), a repeated measurement should be carried out after 5-7 days. Therapy should not be started if a repeat test confirms the initial activity of KFK (more than 5 times higher than the upper limit of normal).

Before starting

therapy When prescribing Rosuvastatin-SZ, as with other HMG-CoA reductase inhibitors, caution should be exercised in patients with existing risk factors for myopathy / rhabdomyolysis (see the "Caution" section), it is necessary to consider the ratio of risk and the possible benefits of therapy and conduct clinical observation.

During

therapy, the patient should be informed of the need to immediately inform the doctor of cases of sudden onset of muscle pain, muscle weakness, or cramping, especially in combination with malaise and fever. In such patients, CPK activity should be determined. Therapy should be discontinued if the activity of CPK is significantly increased (more than 5 times compared with the upper limit of the norm) or if the symptoms of the muscles are pronounced and cause daily discomfort (even if CPK activity is 5 times less compared to the upper limit of the norm). If symptoms disappear, and CPK activity returns to normal, consideration should be given to re-prescribing the drug Rosuvastatin-SZ or other HMG-CoA reductase inhibitors in lower doses with careful monitoring of the patient.

Routine monitoring of CPK activity in the absence of symptoms is impractical.

Very rare cases of immune-mediated necrotizing myopathy have been reported with clinical manifestations in the form of persistent proximal muscle weakness and increased serum CPK during treatment or when statins, including rosuvastatin, are stopped. Additional studies of the muscle and nervous system, serological studies, as well as immunosuppressive therapy may be required.

There were no signs of increased effects on skeletal muscle when taking Rosuvastatin-SZ and concomitant therapy. However, an increase in the incidence of myositis and myopathy has been reported in patients taking other HMG-CoA reductase inhibitors in combination with fibric acid derivatives, including gemfibrozil, cyclosporin, nicotinic acid, azole antifungal agents, protease inhibitors and macrolide antibiotics. Gemfibrozil increases the risk of myopathy when used together with certain HMG-CoA reductase inhibitors. Thus, the simultaneous use of the drug Rosuvastatin-SZ and gemfibrozil is not recommended. The ratio of risk and possible benefit should be carefully weighed when the rosuvastatin-SZ drug is combined with fibrates or lipid-lowering doses of nicotinic acid. The use of the drug Rosuvastatin-SZ at a dose of 40 mg together with fibrates is contraindicated (see the sections "Interaction with other drugs" and "Contraindications").

2-4 weeks after the start of treatment and / or with an increase in the dose of the drug Rosuvastatin-SZ, monitoring of lipid metabolism is necessary (dose adjustment is necessary if necessary).

Liver

It is recommended that liver function tests be determined prior to initiation of therapy and 3 months after initiation of therapy. The use of the drug Rosuvastatin-SZ should be discontinued or the dose of the drug should be reduced if the activity of transaminases in the blood serum is 3 times higher than the upper limit of normal.

In patients with hypercholesterolemia due to hypothyroidism or nephrotic syndrome, therapy of the main diseases should be carried out before treatment with Rosuvastatin-SZ.

Special Populations. Ethnic groups

In the course of pharmacokinetic studies among Chinese and Japanese patients, an increase in systemic concentration of rosuvastatin was noted compared with indicators obtained among Caucasoid patients (see sections “Dosage and Administration” and “Pharmacokinetics”).

HIV protease inhibitors

The combined use of the drug with HIV protease inhibitors is not recommended (see sections "Interaction with other medicinal products" and "Contraindications").

Lactose

The drug should not be used in patients with lactase deficiency, galactose intolerance and glucose-galactose malabsorption.

Interstitial pulmonary disease

When using certain statins, especially for a long time, isolated cases of interstitial lung disease have been reported. Manifestations of the disease can include shortness of breath, unproductive cough, and general well-being (weakness, weight loss, and fever). If interstitial pulmonary disease is suspected, statin therapy should be discontinued.

Type 2 diabetes mellitus

In patients with a glucose concentration of 5.6 to 6.9 mmol / L, therapy with Rosuvastatin-S3 was associated with an increased risk of type 2 diabetes.

Influence on the ability to drive vehicles and control mechanisms

No studies have been conducted to study the effect of the drug Rosuvastatin-SZ on the ability to drive a vehicle and use mechanisms. Care must be taken when driving or working, requiring increased concentration of attention and speed of psychomotor reactions (dizziness may occur during therapy).

Composition

Composition (1 tablet, dosage 40 mg): active substance: calcium rosuvastatin in terms of rosuvastatin - 40 mg.

excipients: core - lactose monohydrate (milk sugar) - 55.2 mg calcium hydrogen phosphate dihydrate - 40.0 mg povidone (polyvinylpyrrolidone medium molecular weight) - 13.0 mg croscarmellose sodium (primrose) - 8.3 mg sodium stearylfumarate - 2.5 mg of silicon dioxide colloidal (aerosil) - 1.0 mg microcrystalline cellulose - 90.0 mg

shell - Opadry II (polyvinyl alcohol, partially hydrolyzed - 3.52 mg macrogol (polyethylene glycol) 3350 - 0.988 mg talc - 1, 6 mg titanium dioxide E 171 - 1.5336 mg soya lecithin E 322 - 0.28 mg aluminum varnish indigo carmine dye ove - 0.0048 mg Aluminum Lake Dye azorubin - 0 0408 mg aluminum dye based crimson dye [Ponceau 4R] - 0.0328 mg).

should be intended. Dosage and administration

Inside, do not chew or grind the tablet, swallow whole, washed down with water. The drug can be prescribed at any time of the day, regardless of food intake.

Before starting therapy with Rosuvastatin-C3, the patient should start to follow a standard hypocholesterolemic 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 current recommendations on target lipid concentrations.

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 mg or 10 mg of the drug Rosuvastatin-SZ 1 time per day. When choosing an initial dose, one should be guided by the individual cholesterol content 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 after 4 weeks (see section "Pharmacodynamics").

Due to the possible development of side effects when taking a dose of 40 mg, compared with lower doses of the drug (see section "Side effects"), increasing the dose to 40 mg after an additional dose is higher than the recommended initial dose for 4 weeks of therapy, can be carried out only in patients with severe hypercholesterolemia and a high risk of cardiovascular complications (especially in patients with familial hypercholesterolemia) who have not achieved the desired result of therapy when taking a dose of 20 mg, and who they will be monitored by a specialist (see the section "Special Instructions"). Particularly careful monitoring of patients receiving the drug at a dose of 40 mg is recommended. A dosage of 40 mg is not recommended for patients not previously contacted by a doctor. After 2-4 weeks of therapy and / or with an increase in the dose of the drug Rosuvastatin-SZ, monitoring of lipid metabolism is necessary (dose adjustment is necessary if necessary).

Homozygous hereditary hypercholesterolemia

Recommended starting dose is 20 mg once daily.

Elderly patients

Patients over the age of 65 are advised to start using the drug with a dose of 5 mg once a day.

Patients with renal failure

Dose adjustment is not required in patients with mild or moderate renal failure. In patients with severe renal failure (CC less than 30 ml / min.), The use of the drug Rosuvastatin-SZ is contraindicated. The use of the drug in a dose of 40 mg is contraindicated in patients with moderate impaired renal function (CC 30-60 ml / min.) (See sections "Special Instructions" and "Pharmacodynamics"). For patients with moderate impaired renal function, an initial dose of 5 mg is recommended.

Patients with liver failure

Rosuvastatin-S3 is contraindicated in patients with active liver disease (see section "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 was noted among Japanese and Chinese (see the section "Special Instructions"). This fact should be taken into account when prescribing Rosuvastatin-SZ to these patient groups. When prescribing doses of 10 mg and 20 mg, the recommended initial dose for patients of the Mongoloid race is 5 mg. The administration of the drug in a dose of 40 mg is contraindicated for patients of the Mongoloid race (see section "Contraindications").

Patients predisposed to myopathy

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

Use with concomitant therapy

With the simultaneous use of the drug with gemfibrozil, fibrates, nicotinic acid in a dose of more than 1 g / day, an initial dose of 5 mg is recommended for patients. The dose of the drug Rosuvastatin-SZ should not exceed 10 mg once a day.

Side effects

Side effects observed when taking Rosuvastatin-SZ are usually mild and go away on their own. As with other HMG-CoA reductase inhibitors, the incidence of side effects is primarily dose-dependent.

The frequency of undesirable effects is as follows: often -? 1/100,

From the immune system: rarely - hypersensitivity reactions, including angioedema.

From the endocrine system: often type 2 diabetes.

From the central nervous system: often - headache, dizziness.

From the digestive tract: often - constipation, nausea, abdominal pain rarely - pancreatitis.

From the skin: infrequently - itching, rash, urticaria.

From the musculoskeletal system: often - myalgia rarely - myopathy (including myositis), rhabdomyolysis.

Other: often - asthenic syndrome.

From the urinary system: in patients treated with rosuvastatin-SZ, proteinuria can be detected. Changes in the amount of protein in the urine (from the absence or trace amounts to "++" or more) are observed in less than 1% of patients receiving 10–20 mg of the drug, and in approximately 3% of patients receiving 40 mg of the drug. A slight change in the amount of protein in the urine was observed when taking a dose of 20 mg. In most cases, proteinuria decreases or disappears during therapy and does not mean the occurrence of acute or progression of an existing kidney disease.

From the musculoskeletal system: when using the drug Rosuvastatin-SZ in all doses, and especially when taking doses of the drug in excess of 20 mg, the following reactions from the musculoskeletal system were reported - myalgia, myopathy (including myositis) rarely - rhabdomyolysis with acute renal failure or without it. A dose-dependent increase in CPK activity is observed in a small number of patients taking rosuvastatin. In most cases, it was mild, asymptomatic and temporary. In case of increased activity of CPK (more than 5 times compared with VGN) therapy should be suspended (see. "Special instructions").

From the liver: with the use of rosuvastatin, a dose-dependent increase in the activity of hepatic transaminases is observed in a small number of patients. In most cases, it is insignificant, asymptomatic and temporary.

Laboratory indicators: increased glucose, bilirubin concentration, GGTP activity, alkaline phosphatase, thyroid dysfunction.

Post-marketing application of

From the hematopoietic system: unspecified frequency - thrombocytopenia.

From the digestive tract: very rarely - jaundice, hepatitis rarely - increased activity of hepatic transaminases of unspecified frequency - diarrhea.

From the side of the musculoskeletal system: very rarely - arthralgia of unspecified frequency - immuno-mediated necrotizing myopathy.

From the side of the central nervous system: very rarely - polyneuropathy, memory loss.

From the respiratory system: unspecified frequency - cough, shortness of breath.

From the urinary system: very rarely - hematuria.

From the skin and subcutaneous fat: unspecified frequency - Stevens-Johnson syndrome.

From the reproductive system and breast: unspecified frequency - gynecomastia.

Other: unspecified frequency - peripheral edema.

The following side effects have been reported with some statins: depression, sleep disturbances, including insomnia and nightmares, sexual dysfunction. Isolated cases of interstitial lung disease have been reported, especially with prolonged use of drugs (see "Special Instructions").

Overdose

With the simultaneous administration of several daily doses, the pharmacokinetic parameters of rosuvastatin do not change. There is no specific treatment for an overdose of rosuvastatin. In case of an overdose, symptomatic treatment and measures aimed at maintaining the functions of vital organs and systems are recommended. It is necessary to control liver function and CPK level. Hemodialysis is unlikely to be effective.

Storage conditions

In a dry, dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Expiration

3 years.

Deystvuyuschee substances

rosuvastatin

Form of Treatment

tablets



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