Rosuvastatin-SZ tablets coated. 10 mg, 30 pcs. (rosuvastatin)

release form

tablets

Packing

30 pcs

Pharmacological action

Pharmacotherapeutic group of the drug: lipid-lowering agent - HMG-CoA reductase inhibitor

ATX code: [C10AA07]

Pharmacological properties of

Pharmacodynamics

Mechanism of action of

Rosuvastatin is a selective, competitive inhibitor of HMG-CoA reductase-3 enzyme 3-enzyme, 3 enzyme mevalonic acid, a precursor to cholesterol. The main target of the action of rosuvastatin is the liver, where the synthesis of cholesterol (cholesterol) and the catabolism of low density lipoproteins (LDL) are carried out. Rosuvastatin increases the number of “liver” LDL receptors on the cell surface, increasing the uptake and catabolism of LDL, which in turn leads to inhibition of the synthesis of very low density lipoproteins (VLDL), thereby reducing the total amount of LDL and VLDL.

Pharmacodynamics

Rosuvastatin-SZ reduces elevated concentrations of LDL cholesterol (cholesterol-LDL), total cholesterol, triglycerides (TG), increases the concentration of high-density lipoprotein cholesterol (HDL-cholesterol), and also reduces the concentration of apolipoprotein B non-HDL, cholesterol-VLDL, TG-VLDLP and increases the concentration of apolipoprotein A-I (ApoA-I), reduces the ratio of cholesterol-LDL / cholesterol-HDL, total cholesterol-cholesterol-HDL and cholesterol-HDL / 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) when 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-SZ at a dose of 20-80 mg, there is a positive dynamics in the lipid profile. 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 from 273 to 817 mg / dl, treated with Rosuvastatin-SZ 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. An 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. The results of 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-desmethyltrosluvuvastatin 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 in the case of other HMG-CoA reductase inhibitors, the cholesterol membrane carrier is involved in the process of “hepatic” uptake of rosuvastatin, which plays 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-desmethylrosuvastatin is 9 times higher than that of 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 Fredrickson hypercholesterolemia (type IIa, including familial heterozygous hypercholesterolemia) or mixed hypercholesterolemia (type IIb) as an adjunct to diet, when diet and other non-drug therapies (e.g. physical weight loss) are insufficient.

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

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

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

- To slow the progression of atherosclerosis as a supplement to the diet in patients who are shown 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 artery 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).

Contraindications

For the drug Rosuvastatin-SZ in a daily dose of 5 mg, 10 mg and 20 mg:

- hypersensitivity to rosuvastatin or any of the components of the

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

- children under 18 years old

- liver disease in the active phase, including a persistent increase in serum activity transaminases and any increase in the activity of transaminases in the blood serum (more than 3 times compared with the upper limit of normal)

- severe renal failure (CC less than 30 ml / min.)

- myopathy

- simultaneous Riyem cyclosporine

- in women: pregnancy, period of breastfeeding, the lack of adequate methods of contraception

- an 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 HIV protease inhibitors

- in patients predisposed to the development of myotoxic complications

For rosuvastatin-C3 drug daily dose of 40 mg:

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

- lactose intolerance, lactase deficiency or glucose-galactose malabsorption (the drug contains lactose) s rdlkp - children under 18 years of age

- concomitant use of cyclosporine

- in women: pregnancy, period of breastfeeding, the lack of adequate methods of contraception

- an 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 HIV protease inhibitors

- moderate and severe renal failure (CC less than 60 ml / min. )

- 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 the upper limit of normal) for patients with risk factors Vitality of myopathy / rhabdomyolysis, namely:

- hypothyroidism

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

- excessive alcohol consumption

- condition, which can lead to an increase in the plasma concentration of rosuvastatin

- concomitant use of

fibrates - myopathy

- personal or family history of muscle diseases

- for patients of the Mongoloid race

Caution

For rosuvastatin-10 mg 10 mg daily: The presence of a risk of developing myopathy / rhabdomyolysis - renal failure, hypothyroidism, a personal or family history of hereditary muscle diseases and a previous history of muscle toxicity when using other HMG-Co inhibitors A-reductase or fibrate excessive alcohol consumption age over 65 years of age conditions in which there is an increase in the plasma concentration of rosuvastatin race (Mongoloid race) concurrent administration with fibrates (see section “Pharmacokinetics”) a history of liver disease sepsis arterial hypotension extensive surgery, trauma, severe metabolic, endocrine or electrolyte disturbances or uncontrolled seizures. Concomitant use with colchicine and with ezetimibe (see section "Interaction with other drugs"). For the daily dose of rosuvastatin-SZ 40 mg: Renal insufficiency of mild severity (CC more than 60 ml / min) age over 65 years of liver disease in the history of sepsis arterial hypotension extensive surgery, trauma, severe metabolic, endocrine or electrolyte disturbances or uncontrolled convulsive seizures. Concomitant use with colchicine and with ezetimibe (see section "Interaction with other drugs"). Patients with liver failure There is no data or experience with the use of the drug in patients with more than 9 Child-Pugh scores (see the sections “Pharmacodynamics” and “Special Instructions”).

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. Data on the allocation of rosuvastatin with breast milk are not available, therefore, during the period of breastfeeding, the drug should be discontinued (see section "Contraindications").

Composition

Active ingredient: rosuvastatin calcium in terms of rosuvastatin –10 mg.

Excipients:

core - lactose monohydrate (milk sugar) - 44.3 mg calcium hydrogen phosphate dihydrate - 10.0 mg povidone (polyvinylpyrrolidone medium molecular weight) - 6.0 mg croscarmellose sodium (primellose) - 4.0 mg sodium stearyl fumarate - 1.2 mg of silicon dioxide colloidal dioxide (Aerosil) - 0.5 mg microcrystalline cellulose - 44.0 mg

shell - Opadray II (polyvinyl alcohol, partially hydrolyzed - 1.76 mg macrogol (polyethylene glycol) 3350 - 0.494 mg talc - 0 , 8 mg of titanium dioxide E 171 - 0.7668 mg soy lecithin E 322 - 0.14 mg aluminum varnish per dye-based indigo carmine - 0.0024 mg aluminum varnish-based dye azorubine - 0.0204 mg aluminum varnish-based dye crimson [Ponceau 4R] - 0.0164 mg).

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-S3, the patient should begin 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"). In connection with the possible development of side effects when taking a dose of 40 mg, in comparison 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 only be performed 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 will be under the supervision of a specialist (see 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 who have not previously consulted 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 among Japanese and Chinese was noted (see 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 mainly dose-dependent. The frequency of adverse effects is presented as follows: often (> 1/100, <1/10) infrequently (> 1/1000, <1/100) rarely (> 1/10000, <1/1000) very rarely (<1 / 10000), the frequency is unknown (according to available data, it is not possible to establish the frequency of occurrence), including individual messages.



immune system Rarely: hypersensitivity reactions, including angioedema.

Endocrine system

Often: type 2 diabetes mellitus

From the central nervous system

Often: headache, dizziness

From the digestive tract

Often: constipation, nausea, abdominal pain Rarely: pancreatitis

From the side : skin itch, rash, urticaria

From the musculoskeletal system

Often: myalgia Rarely: myopathy (including myositis), rhabdomyolysis

Other

Often: asthenic syndrome

From the urinary system

Patients treated with rosuvastatin-C3 may have a history of 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 to 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

The following effects on the musculoskeletal system: myalgia, myopathy (including myositis), in rare cases, have been reported with the use of the drug Rosuvastatin-SZ in all doses, and especially when taking doses of the drug in excess of 20 mg cases - rhabdomyolysis with acute renal failure or without it. A dose-dependent increase in the activity of creatine phosphokinase (CPK) 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 the upper limit of normal), therapy should be suspended (see section "Special instructions").

On the part of the liver

When using rosuvastatin, a dose-dependent increase in the activity of “liver” transaminases is observed in a small number of patients. In most cases, it is insignificant, asymptomatic and temporary.

Laboratory indicators

When using the drug Rosuvastatin-SZ, the following changes in laboratory parameters were also observed: an increase in the concentration of glucose, bilirubin, the activity of gamma-glutamyl transpeptidase, alkaline phosphatase, and dysfunction of the thyroid gland.

Post-marketing use of

The following side effects have been reported in the post-marketing use of rosuvastatin-C3:

From the digestive tract

Very rare: jaundice, hepatitis Rarely: increased activity of hepatic transaminases. Frequency unknown: diarrhea, fatal and non-fatal liver failure

From the musculoskeletal system

Very rare: arthralgia. Frequency unknown: Immuno-mediated necrotizing myopathy

From the central nervous system

Very rare: polyneuropathy, forgetfulness, amnesia, memory loss, confusion From the respiratory system Frequency unknown: cough, shortness of breath

From the urinary system

Very rarely: From the skin and subcutaneous fat

Frequency unknown: Stevens-Johnson syndrome From the reproductive system and mammary gland Frequency unknown: gynecoma ment

Other

Frequency unknown: peripheral edema, thrombocytopenia, interstitial lung disease. The following side effects have been reported with some statins: depression, sleep disturbances, including insomnia and nightmares, sexual dysfunction.

Drug interaction

Cyclosporine and gemfibrozil potentiate the effects of rosuvastatin. Antacids, which contain magnesium or aluminum, reduce the plasma concentration of rosuvastatin by about 50% (they should be taken 2 hours after taking rosuvastatin). Erythromycin, by enhancing gastrointestinal motility, reduces the effects of rosuvastatin. Rosuvastatin enhances the effects of oral contraceptives. Gemfibrozil, other fibrates, and nicotinic acid in lipid-lowering doses (approximately 1 g / day) increase the possibility of myopathy when used together with rosuvastatin. Co-administration of rosuvastatin with itraconazole increases 28% of rosuvastatin AUC (clinically insignificant). When used together with rosuvastatin with drugs that reduce the content of endogenous steroid hormones (including cimetidine, ketoconazole, spironolactone), a more pronounced decrease in endogenous steroid hormones is possible.

Overdose

When administered with multiple daily doses, the pharmacokinetic parameters of rosuvastatin do not change. There is no specific treatment for overdose with rosuvastatin. In case of overdose, it is recommended to carry out symptomatic treatment and measures aimed at maintaining the functions of vital organs and systems. Control of liver function and CPF level is required. Hemodialysis is unlikely to be effective.

Storage conditions

Store in a dry, a place protected from light at a temperature of no higher than 30 ° C.

Expiration

3 years. Do not use after the expiry date stated on the packaging.

Deystvuyuschee substances

rosuvastatin

Terms of Pharmacy Leave

Prescription

Northern Star, Russia



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