Rosucard 10 mg, 90 film-coated tablets

Pharmacodynamics and pharmacokinetics

Rosucard belongs to the group of statins . It inhibits HMG-CoA reductase , an enzyme that converts HMG-CoA to mevalonate .

In addition, this drug increases the number of LDL receptors on hepatocytes , which increases the intensity of LDL and causes inhibition of VLDL , reducing the total content of VLDL and LDL . The drug reduces the concentration of LDL-C , high-density non-lipoprotein cholesterol , VLDL-C , TG , apolipoprotein B , VLDL-TG , total cholesterol , and also increases the content of ApoA-1 and HDL-C . In addition, it reduces the ratio of ApoB and ApoA-1 , cholesterol-non-HDL and cholesterol-HDL , cholesterol-LDL and cholesterol-HDL , total cholesterol and cholesterol-HDL .

The main effect of Rosucard is directly proportional to the prescribed dosage. The therapeutic effect after the start of treatment is noticeable within a week, after about a month it becomes maximum, and then strengthens and becomes permanent.

The maximum concentration of the main active substance in plasma is established after 5 hours. Absolute bioavailability is 20%. The degree of binding to blood plasma proteins is about 90%.

With regular use, the pharmacokinetics do not change.

is metabolized through the liver. Penetrates well through the placental barrier . The main metabolites are N-dismethyl and lactone metabolites .

The half-life is approximately 19 hours, and it does not change if the dosage of the drug is increased. Plasma clearance on average is 50 l/h. Approximately 90% of the active substance is excreted unchanged through the intestines, the rest through the kidneys.

Gender and age do not affect the pharmacokinetics of Rosucard. However, it depends on race. In Indians, the maximum concentration and mean AUC are approximately 1.3 times higher than in Caucasians. AUC in people of the Mongoloid race is 2 times higher.

Rosucard 10 mg, 90 film-coated tablets

Registration Certificate Holder

SANOFI RUSSIA (Russia)

Dosage form

Medicine - Rosucard®

Description

Film-coated tablets

light pink, oblong, biconvex, with a notch.

1 tab.

rosuvastatin calcium 10.4 mg, which corresponds to the content of rosuvastatin 10 mg

Excipients

: lactose monohydrate - 60 mg, microcrystalline cellulose - 45.4 mg, croscarmellose sodium - 1.2 mg, colloidal silicon dioxide - 0.6 mg, magnesium stearate - 2.4 mg.

Film shell composition:

hypromellose 2910/5 - 2.5 mg, macrogol 6000 - 0.4 mg, titanium dioxide - 0.325 mg, talc - 0.475 mg, red iron oxide dye - 0.013 mg.

10 pieces. - blisters (3) - cardboard packs. 10 pieces. - blisters (6) - cardboard packs. 10 pieces. - blisters (9) - cardboard packs.

Indications

• primary hypercholesterolemia (type IIa according to the Fredrickson classification), including familial heterozygous hypercholesterolemia, or mixed hypercholesterolemia (type IIb) - as an addition to diet when diet and other non-drug treatments (for example, exercise, weight loss) are insufficient;
• familial homozygous hypercholesterolemia - as an adjunct to diet and other lipid-lowering therapy (for example, LDL apheresis), or in cases where such therapy is not effective enough;
• hypertriglyceridemia (type IV according to the Fredrickson classification) - as an addition to the diet;
• to slow 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 cholesterol;
• 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 years for men and over 60 years 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 HDL-C concentration, smoking, family history of early onset ischemic heart disease).

Contraindications for use

For tablets 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 or any increase in serum transaminase activity (more than 3 times compared to ULN);
• severe renal dysfunction (creatinine clearance less than 30 ml/min);
• myopathy;
• simultaneous use of cyclosporine;
• in women - pregnancy, breastfeeding, lack of adequate methods of contraception;
• patients predisposed to the development of myotoxic complications;
• lactose intolerance, lactase deficiency or glucose-galactose malabsorption (the drug contains lactose);
• age under 18 years (efficacy and safety have not been established).

For tablets 40 mg

• hypersensitivity to rosuvastatin or any of the components of the drug;
• simultaneous use of cyclosporine;
• in women - pregnancy, breastfeeding, lack of adequate methods of contraception;
• 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 ULN), patients with risk factors for the development of myopathy/rhabdomyolysis, namely: moderate renal failure (MC) less than 60 ml/min);
• hypothyroidism;
• personal or family history of muscle diseases;
• myotoxicity due to a history of use of other HMG-CoA reductase inhibitors or fibrates.

With caution
For tablets 10 and 20 mg:
with a history of liver disease; sepsis; arterial hypotension; extensive surgical interventions; injuries; severe metabolic, endocrine or water-electrolyte disorders; uncontrollable seizures; for mild to moderate renal failure; hypothyroidism; data on a history of muscle toxicity when using other HMG-CoA reductase inhibitors or fibrates; history of hereditary muscle diseases; conditions in which an increase in the concentration of rosuvastatin in the blood plasma is noted; when used simultaneously with fibrates; when used simultaneously with HIV protease inhibitors; in patients over 65 years of age; in patients of the Mongoloid race; with excessive alcohol consumption.

For 40 mg tablets:

with mild renal failure (creatinine clearance more than 60 ml/min); history of liver diseases; sepsis; arterial hypotension; extensive surgical interventions; injuries; severe metabolic, endocrine or water-electrolyte disorders; uncontrollable seizures; in patients over 65 years of age.

pharmachologic effect

A lipid-lowering drug from the statin group. A selective competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase, an enzyme that converts HMG-CoA into mevalonate, a precursor of cholesterol (Cc).

Increases the number of LDL receptors on the surface of hepatocytes, which leads to increased uptake and catabolism of LDL, inhibition of VLDL synthesis, reducing the total concentration of LDL and VLDL. Reduces the concentrations of LDL-C, high-density non-lipoprotein cholesterol (non-HDL-C), VLDL-C, total cholesterol, TG, VLDL-TG, apolipoprotein B (ApoB), reduces the ratio of LDL-C/HDL-C, total cholesterol/C. -HDL, non-HDL-C/HDL-C, ApoB/apolipoprotein A-1 (ApoA-1), increases the concentrations of HDL-C and ApoA-1.

The lipid-lowering effect is directly proportional to the prescribed dose. The therapeutic effect appears within 1 week after the start of therapy, after 2 weeks it reaches 90% of the maximum, by 4 weeks it reaches a maximum and after that remains constant.

Clinical effectiveness

Effective in adult patients with hypercholesterolemia with or without hypertriglyceridemia (regardless of race, gender or age), incl. in patients with diabetes mellitus and familial hypercholesterolemia. In 80% of patients with hypercholesterolemia type IIa and IIb (according to the Fredrickson classification) with an average initial LDL-C concentration of about 4.8 mmol/l, while taking the drug at a dose of 10 mg, the LDL-C concentration reaches values ​​of less than 3 mmol/l.

In patients with heterozygous familial hypercholesterolemia receiving rosuvastatin at a dose of 20-80 mg/day, positive dynamics of lipid profile indicators are noted.

An additive effect is observed in combination with fenofibrate in relation to the concentration of TG and with nicotinic acid in lipid-lowering doses (more than 1 g/day) in relation to the reduction in the concentration of HDL-C.

Drug interactions

The effect of the use of other drugs on rosuvastatin

Transport protein inhibitors:

rosuvastatin binds to certain transport proteins, in particular OATP1B1 and BCRP. Concomitant use of drugs that are inhibitors of transport proteins may be accompanied by an increase in the concentration of rosuvastatin in the blood plasma and an increased risk of developing myopathy (see table).

Cyclosporine:

with simultaneous use of rosuvastatin and cyclosporine, the AUC of rosuvastatin was on average 7 times higher than the value observed in healthy volunteers (see table). Does not affect plasma concentrations of cyclosporine. Rosucard® is contraindicated in patients taking cyclosporine.

HIV protease inhibitors:

Although the exact mechanism of interaction is unknown, concomitant use of HIV protease inhibitors may lead to a significant increase in rosuvastatin exposure (see table). A pharmacokinetic study of co-administration of rosuvastatin 20 mg and a combination drug containing two HIV protease inhibitors (400 mg lopinavir/100 mg ritonavir) in healthy volunteers resulted in approximately two-fold and five-fold increases in rosuvastatin AUC(0-24) and Cmax, respectively. Therefore, simultaneous use of Rosucard® and HIV protease inhibitors is not recommended (see table).

Gemfibrozil and other lipid-lowering drugs:

The combined use of rosuvastatin and gemfibrozil leads to a 2-fold increase in Cmax and AUC of rosuvastatin. Based on specific interaction data, a pharmacokinetically significant interaction with fenofibrate is not expected, but a pharmacodynamic interaction is possible. Gemfibrozil, fenofibrate, other fibrates and nicotinic acid in lipid-lowering doses (more than 1 g/day) increase the risk of myopathy when used simultaneously with HMG-CoA reductase inhibitors, possibly due to the fact that they can cause myopathy and when used in as monotherapy. When taking the drug simultaneously with gemfibrozil, fibrates, nicotinic acid in lipid-lowering doses, patients are recommended to take an initial dose of Rosucard® 5 mg; taking a dose of 40 mg is contraindicated when co-administered with fibrates.

Fusidic acid:

There have been no specific drug interaction studies between fusidic acid and rosuvastatin, but isolated case reports of rhabdomyolysis have been noted.

Ezetimibe:

simultaneous use of Rosucard® at a dose of 10 mg and ezetimibe at a dose of 10 mg was accompanied by an increase in the AUC of rosuvastatin in patients with hypercholesterolemia (see table). An increased risk of side effects due to the pharmacodynamic interaction between Rosucard® and ezetimibe cannot be excluded.

Antacids:

simultaneous use of rosuvastatin and antacid suspensions containing aluminum or magnesium hydroxide leads to a decrease in the plasma concentration of rosuvastatin by approximately 50%. This effect is less pronounced if antacids are used 2 hours after taking rosuvastatin. The clinical significance of this interaction has not been studied.

Erythromycin:

simultaneous use of rosuvastatin and erythromycin leads to a decrease in AUC of rosuvastatin by 20% and Cmax of rosuvastatin by 30%. This interaction may occur as a result of increased intestinal motility caused by erythromycin.

Isoenzymes of the cytochrome P450 system:

the results of in vivo and in vitro studies showed that rosuvastatin is neither an inhibitor nor an inducer of cytochrome P450 isoenzymes. In addition, rosuvastatin is a weak substrate for these enzymes. Therefore, interaction of rosuvastatin with other drugs at the metabolic level involving cytochrome P450 isoenzymes is not expected. There was no clinically significant interaction between rosuvastatin and fluconazole (inhibitor of CYP2C9 and CYP3A4 isoenzymes) and ketoconazole (inhibitor of CYP2A6 and CYP3A4 isoenzymes).

Interactions with drugs that require dose adjustment of rosuvastatin (see table)

The dose of Rosucard® should be adjusted if it is necessary to use it together with drugs that increase the exposure of rosuvastatin. If an increase in exposure by 2 times or more is expected, the initial dose of Rosucard® should be 5 mg 1 time / day. The maximum daily dose of Rosucard® should also be adjusted so that the expected exposure to rosuvastatin does not exceed that for a dose of 40 mg taken without the simultaneous administration of drugs that interact with rosuvastatin. For example, the maximum daily dose of Rosucard® when used simultaneously with gemfibrozil is 20 mg (increased exposure by 1.9 times), with ritonavir/atazanavir - 10 mg (increased exposure by 3.1 times).

Table. Effect of concomitant therapy on rosuvastatin exposure (AUC, data in descending order) - results of published clinical studies

Concomitant therapy regimen Rosuvastatin regimen Change in rosuvastatin AUC

Cyclosporine 75-200 mg 2 times/day, 6 months 10 mg 1 time/day, 10 days Increase by 7.1 times Atazanavir 300 mg/ritonavir 100 mg 1 time/day, 8 days 10 mg once Increase by 3.1 times Simeprevir 150 mg 1 time/day, 7 days 10 mg once Increased by 2.8 times Lopinavir 400 mg/ritonavir 100 mg 2 times/day, 17 days 20 mg 1 time/day, 7 days Increased by 2.1 times Clopidogrel 300 mg, then 75 mg for 24 hours 20 mg once Increased by 2 times Gemfibrozil 600 mg 2 times/day , 7 days 80 mg once Increase by 1.9 times Eltrombopag 75 mg 1 time / day, 10 days 10 mg once Increase by 1.6 times Darunavir 600 mg / ritonavir 100 mg 2 times / day, 7 days 10 mg 1 time / day, 7 days Increase by 1.5 times Tipranavir 500 mg / ritonavir 200 mg 2 times/day, 11 days 10 mg once 1.4-fold increase Dronedarone 400 mg 2 times/day No data 1.4-fold increase Itraconazole 200 mg 1 time/day, 5 days 10 mg or 80 mg once 1.4-fold increase Ezetimibe 10 mg 1 time/day, 14 days 10 mg 1 time/day, 14 days Increase 1.2 times Fosamprenavir 700 mg/ritonavir 100 mg 2 times/day, 8 days 10 mg once No changes Aleglitazar 0.3 mg, 7 days 40 mg, 7 days No changes Silymarin 140 mg 3 times/day, 5 days 10 mg once No changes Fenofibrate 67 mg 3 times/day, 7 days10 mg, 7 daysNo changesRifampin 450 mg 1 time/day, 7 days20 mg onceNo changesKetoconazole 200 mg 2 times/day, 7 days80 mg onceNo changesFluconazole 200 mg 1 time/day, 11 days80 mg onceNo changesErythromycin 500 mg 4 times/day, 7 days 80 mg once, 28% reduction Baikalin 50 mg 3 times/day, 14 days 20 mg once, 47% reduction

The effect of rosuvastatin on other drugs

Vitamin K antagonists:

Initiating therapy or increasing the dose of Rosucard® in patients receiving concomitant vitamin K antagonists (for example, warfarin) may lead to an increase in the INR. Discontinuation or reduction of the dose of Rosucard® may cause a decrease in INR. In such cases, INR monitoring is recommended.

Oral contraceptives/hormone replacement therapy:

simultaneous use of rosuvastatin and oral contraceptives increases the AUC of ethinyl estradiol and AUC of norgestrel by 26% and 34%, respectively.
This increase in plasma concentration should be taken into account when selecting the dose of oral contraceptives. There are no pharmacokinetic data on the simultaneous use of Rosucard® and hormone replacement therapy; therefore, a similar effect cannot be excluded when using this combination.
However, this combination was widely used during clinical trials and was well tolerated by patients. Other medicines:

No clinically significant interaction between rosuvastatin and digoxin is expected.

Dosage regimen

The drug is taken orally. The tablets should be swallowed whole, without chewing or crushing, with water, at any time of the day, regardless of meals.

Before starting therapy with Rosucard®, the patient should begin to follow a standard lipid-lowering diet and continue to follow it during treatment.

The dose of the drug should be individualized depending on the indication and therapeutic response, taking into account current generally accepted recommendations for target lipid concentrations.

The recommended starting dose of Rosucard® for patients starting to take the drug, or for patients transferred from taking other HMG-CoA reductase inhibitors, is 5 or 10 mg 1 time / day. If it is necessary to take the drug Rosucard® at a dose of 5 mg, the 10 mg tablet should be divided into two parts according to the risk.

When choosing an initial dose, one should be guided by the patient's cholesterol level and take into account the risk of developing cardiovascular complications, and the potential risk of side effects should be assessed. If necessary, after 4 weeks the dose of the drug can be increased.

Due to the possible development of side effects, final titration to a maximum dose of 40 mg should be carried out only in patients with severe hypercholesterolemia and a high risk of cardiovascular complications (especially patients with hereditary hypercholesterolemia) who did not experience symptoms when taking the drug at a dose of 20 mg. the target cholesterol concentration has been achieved. Such patients should be under medical supervision. 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 2-4 weeks of therapy and/or when increasing the dose of the drug Rosucard®, it is necessary to monitor lipid metabolism parameters (if necessary, dose adjustment is required).

In elderly patients over 65 years of age

no dose adjustment is required.

The drug is contraindicated in patients with active liver disease

.

In patients with mild renal failure

no dose adjustment is required;
The recommended initial dose of Rosucard® is 5 mg/day. In patients with moderate renal failure (creatinine clearance 30-60 ml/min),
the use of Rosucard® at a dose of 40 mg/day is contraindicated.
In patients with severe renal failure (creatinine clearance less than 30 ml/min),
the use of Rosucard® is contraindicated.

In patients with a predisposition to myopathy

the use of Rosucard® at a dose of 40 mg/day is contraindicated. When prescribing the drug in doses of 10 mg and 20 mg/day, the recommended initial dose for this group of patients is 5 mg/day.

When studying the pharmacokinetic parameters of rosuvastatin, an increase in the systemic concentration of the drug was noted in representatives of the Mongoloid race

.
This fact should be taken into account when prescribing Rosucard® to patients of the Mongoloid race. When prescribing the drug in doses of 10 mg and 20 mg, the recommended initial dose for this group of patients is 5 mg/day. The use of the drug Rosucard® at a dose of 40 mg/day in representatives of the Mongoloid race is contraindicated. Genetic polymorphism.
Carriers of the SLCO1B1 (OATP1B1) c.521CC and ABCG2 (BCRP) c.421AA genotypes had an increase in rosuvastatin exposure (AUC) compared to carriers of the SLC01B1 c.521TT and ABCG2 c.421CC genotypes. For patients carrying genotypes c.521CC or c.421AA, the recommended maximum dose of Rosucard® is 20 mg/day.

Concomitant therapy.

Rosuvastatin binds to various transport proteins (in particular, OATP1B1 and BCRP). When simultaneous use of the drug Rosucard® with drugs (such as cyclosporine, some HIV protease inhibitors, including a combination of ritonavir with atazanavir, lopinavir and/or tipranavir) that increase the concentration of rosuvastatin in the blood plasma due to interaction with transport proteins, the risk of developing myopathy may increase (including rhabdomyolysis). In such cases, the possibility of prescribing alternative therapy or temporarily stopping the use of Rosucard® should be assessed. If the use of the above drugs is necessary, you should read the instructions for use of the drugs before prescribing them simultaneously with the drug Rosucard®, assess the benefit-risk ratio of concomitant therapy and consider reducing the dose of the drug Rosucard®.

Overdose

When taking several daily doses simultaneously, the pharmacokinetic parameters of rosuvastatin do not change.

Treatment:

There is no specific treatment; symptomatic therapy is carried out to maintain the functions of vital organs and systems. Monitoring of liver function indicators and CPK activity is necessary. Hemodialysis is ineffective.

Side effect

Side effects observed when taking rosuvastatin 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 following is an adverse reaction profile for rosuvastatin based on clinical trial data and extensive post-marketing experience.

Determination of the frequency of adverse reactions (according to the WHO classification): very often (≥1/10), often (from ≥1/100 to <1/10), infrequently (≥1/1000 to <1/100), rarely ( from ≥1/10,000 to <1/1000), very rare (from <1/10,000, including isolated reports), frequency unknown (it is not possible to determine the frequency from the available data).

From the hematopoietic system:

rarely - thrombocytopenia.

From the nervous system:

often - headache, dizziness; very rarely - peripheral neuropathy, memory loss or decline; frequency unknown - sleep disturbances, including insomnia and nightmares.

Mental disorders:

frequency unknown - depression.

From the digestive system:

often - nausea, constipation, abdominal pain; infrequently - vomiting; rarely - pancreatitis; frequency unknown - diarrhea.

From the liver and biliary tract:

rarely - a dose-dependent transient increase in the activity of AST and ALT; very rarely - hepatitis, jaundice.

From the respiratory system:

frequency unknown - cough, dyspnea.

From the musculoskeletal system:

often - myalgia; rarely - myopathy (including myositis), rhabdomyolysis with and without acute renal failure (in patients treated in doses >20 mg/day); very rarely - arthralgia; frequency unknown - immune-mediated necrotizing myopathy.

Allergic reactions:

infrequently - skin itching, urticaria; rarely - hypersensitivity reactions, including angioedema.

From the skin and subcutaneous tissue:

uncommon - rash; frequency unknown - Stevens-Johnson syndrome.

From the urinary system:

often - proteinuria; very rarely - hematuria. Changes in the amount of protein in the urine (from none or trace amounts to ++ or more) are observed in less than 1% of patients receiving a dose of 10-20 mg/day and in approximately 3% of patients receiving 40 mg/day. Proteinuria decreases with therapy and is not associated with kidney disease or urinary tract infection.

From the genital organs and breast:

very rarely - gynecomastia.

Laboratory indicators:

infrequently - a dose-dependent increase in serum CPK activity (in most cases, slight, asymptomatic and temporary). If the activity increases by more than 5 times compared to the ULN, therapy with Rosucard® should be temporarily suspended. Increased concentration of glycosylated hemoglobin in blood plasma.

Other:

often - asthenic syndrome;
frequency unknown - peripheral edema. When using the drug Rosucard®, changes in the following laboratory parameters were observed: increased concentrations of glucose, bilirubin, alkaline phosphatase activity, GGT.
The following adverse events have been reported with the use of some statins: erectile dysfunction, isolated cases of interstitial lung disease (especially with long-term use), type 2 diabetes mellitus, the incidence of which depends on the presence or absence of risk factors (fasting blood glucose concentration 5.6- 6.9 mmol/l, BMI >30 kg/m2, hypertriglyceridemia, history of arterial hypertension).

special instructions

Effect on the kidneys

In patients receiving high doses of rosuvastatin (mainly 40 mg), tubular proteinuria was observed, which in most cases was transient. This 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 parameters during treatment.

Effect on the musculoskeletal system

The following musculoskeletal effects have been reported with rosuvastatin at all doses, and particularly at doses greater than 20 mg: myalgia, myopathy, and in rare cases, rhabdomyolysis.

Determination of CPK activity

Determination of CPK activity should not be carried out after intense physical activity or in the presence of other possible reasons for increased CPK activity, which may lead to incorrect interpretation of the results obtained. If the initial CPK activity is significantly increased (5 times higher than ULN), a repeat measurement should be taken after 5-7 days. Therapy should not be started if a repeat test confirms initial CPK activity (more than 5 times the ULN).

Before starting therapy

When using the drug Rosucard®, as well as when using other HMG-CoA reductase inhibitors, caution should be exercised in patients with existing risk factors for myopathy/rhabdomyolysis. The risk-benefit ratio should be assessed and, if therapy is necessary, clinical monitoring of the patient should be carried out during treatment.

During therapy

The patient should be informed to immediately report to the doctor the unexpected onset of muscle pain, muscle weakness or cramps, especially in combination with malaise and fever. In such patients, CPK activity should be determined. Therapy should be discontinued if CK activity is significantly elevated (more than 5 times the ULN) or if muscle symptoms are severe and cause daily discomfort (even if CK activity is increased less than 5 times the ULN). If symptoms disappear and CPK activity returns to normal, re-prescribing Rosucard® or other HMG-CoA reductase inhibitors in lower doses should be considered 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 weakness of the proximal muscles and increased CPK activity in the blood serum during treatment or upon discontinuation of statins, incl. rosuvastatin. Additional studies of the muscular and nervous system, serological studies, and therapy with immunosuppressive drugs may be required. There were no signs of increased effects on skeletal muscles when taking rosuvastatin and concomitant therapy. However, an increase in the number of cases of myositis and myopathy has been reported in patients taking other HMG-CoA reductase inhibitors in combination with fibric acid derivatives, including gemfibrozil, cyclosporine, nicotinic acid in hypolipidemic doses (more than 1 g / day), azole antifungals, inhibitors HIV proteases and macrolide antibiotics. Gemfibrozil increases the risk of myopathy when used together with certain HMG-CoA reductase inhibitors. Thus, the simultaneous use of Rosucard® and gemfibrozil is not recommended. The risk/benefit ratio should be carefully weighed when using Rosucard® together with fibrates or lipid-lowering doses of nicotinic acid. Taking Rosucard® at a dose of 40 mg together with fibrates is contraindicated. 2-4 weeks after the start of treatment and/or when increasing the dose of the drug Rosucard®, monitoring of lipid metabolism parameters is necessary (if necessary, dose adjustment is required).

Liver

It is recommended to determine liver function indicators before starting therapy and 3 months after starting therapy. Taking Rosucard® should be stopped or the dose reduced if the activity of hepatic transaminases in the blood plasma is 3 times higher than the ULN.

In patients with hypercholesterolemia due to hypothyroidism or nephrotic syndrome, treatment of underlying diseases should be carried out before starting treatment with Rosucard®.

HIV protease inhibitors

Concomitant use of Rosucard® with HIV protease inhibitors is not recommended.

Interstitial lung disease

Isolated cases of interstitial lung disease have been reported with some statins, especially over long periods of use. Manifestations of the disease may include shortness of breath, nonproductive cough and deterioration in general health (weakness, weight loss and fever). If interstitial lung disease is suspected, therapy with Rosucard® should be discontinued.

Diabetes mellitus type 2

Drugs of the statin class can cause an increase in blood glucose concentrations. In some patients at high risk of developing diabetes mellitus, such changes may lead to its manifestation, which is an indication for hypoglycemic therapy. However, the reduction in the risk of vascular diseases while taking statins exceeds the risk of developing diabetes, so this factor should not serve as a basis for discontinuing statin treatment. Patients at risk (fasting blood glucose concentration 5.6-6.9 mmol/l, BMI >30 kg/m2, hypertriglyceridemia, history of arterial hypertension) should be under medical supervision and regularly monitor biochemical parameters.

Lactose

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

Ethnic groups

During pharmacokinetic studies among Chinese and Japanese patients, an increase in systemic concentrations of rosuvastatin was observed compared with values ​​​​obtained among Caucasian patients.
Effect on the ability to drive vehicles and operate machinery
Care should be taken when driving vehicles and doing activities that require increased concentration and speed of psychomotor reactions (dizziness may occur during therapy).

Storage conditions

The drug should be stored in its original packaging out of the reach of children at a temperature not exceeding 25°C.

Best before date

Shelf life: 3 years. Do not use the drug after the expiration date.

Use during pregnancy and breastfeeding

Restrictions during pregnancy - Contraindicated. Restrictions when breastfeeding - Contraindicated.

Rosuvastatin is contraindicated during pregnancy and breastfeeding.

Use of rosuvastatin in women of reproductive age

is possible only if reliable methods of contraception are used and if the patient is informed about the possible risk of treatment to the fetus.

Since cholesterol and substances synthesized from cholesterol are important for fetal development, the potential risk of inhibiting HMG-CoA reductase outweighs the benefit of using the drug during pregnancy. If pregnancy is diagnosed during drug therapy, rosuvastatin should be stopped immediately, and the patient should be warned about the potential risk to the fetus.

If it is necessary to use the drug during lactation, given the possibility of adverse events in infants, breastfeeding should be discontinued.

Use for renal impairment

Restrictions for impaired renal function - With caution.

In patients with severe renal failure (creatinine clearance less than 30 ml/min), the use of Rosucard® is contraindicated.

In patients with moderate renal failure (creatinine clearance 30-60 ml/min), the use of Rosucard® at a dose of 40 mg/day is contraindicated.

In patients with mild renal failure, no dose adjustment is required; The recommended initial dose of Rosucard® is 5 mg/day.

Use for liver dysfunction

Restrictions for liver dysfunction - With caution.

The drug is contraindicated in patients with active liver disease.

The drug should be prescribed with caution if there is a history of liver disease.

Use in elderly patients

Restrictions for elderly patients - Use with caution.

The drug should be prescribed with caution to patients over 65 years of age.

Use in children

Restrictions for children - Contraindicated.

The use of the drug is contraindicated in people under 18 years of age (efficacy and safety have not been established).

Terms of sale

The drug is available with a prescription.

Contacts for inquiries

SANOFI (Unknown)

Representative office of JSC "Sanofi-aventis group" (France) 125009 Moscow, st. Tverskaya, 22 Tel. Fax

Indications for use of Rosucard

Indications for use of Rosucard are as follows:

• primary hypercholesterolemia or mixed dyslipidemia - the drug is used as an addition to the diet if dietary nutrition alone is insufficient;
• the need to slow the development of atherosclerosis - the drug is used as an addition to the diet as part of treatment to reduce the level of total cholesterol and LDL cholesterol to normal levels;
• familial homozygous hypercholesterolemia - the drug is used as an addition to the diet or as a component of lipid-lowering therapy;
• the need to prevent complications in the functioning of the cardiovascular system with an increased risk of atherosclerotic cardiovascular disease - the drug is used as part of therapy.

Nosological classification (ICD-10)

• E78.0 Pure hypercholesterolemia
• E78.1 Pure hyperglyceridemia
• E78.2 Mixed hyperlipidemia
• E78.5 Hyperlipidemia, unspecified
• I10 Essential (primary) hypertension
• I15 Secondary hypertension
• I21 Acute myocardial infarction
• I25.9 Chronic ischemic heart disease, unspecified
• I64 Stroke not specified as hemorrhage or infarction
• I70 Atherosclerosis
• Z72.0 Tobacco use
• Z82.4 Family history of coronary heart disease and other diseases of the cardiovascular system

Contraindications

The medicine should not be used for:

• hypersensitivity to its components;
• severe kidney disease;
• liver diseases in the active phase;
• myopathies;
• pregnancy;
• lactation.

Rosucard is also contraindicated in women of reproductive age who do not use contraception.

The 40 mg dosage should not be taken by people with factors that contribute to the development of myopathy and rhabdomyolysis , namely:

• moderate renal impairment;
• hereditary muscle diseases in an individual or family history ;
• alcoholism;
• hypothyroidism;
• history of myotoxicity provoked - CoA reductase inhibitors or fibrates .

The risk group also includes patients of the Mongoloid race, as well as those taking fibrates . This dosage is also contraindicated in situations that may cause an increase in the content of the drug in the blood plasma.

Use during pregnancy and breastfeeding

The use of Rosucard® in women of reproductive age is possible only if reliable methods of contraception are used and if the patient is informed about the possible risk of treatment to the fetus.

Since cholesterol and substances synthesized from cholesterol are important for fetal development, the potential risk of inhibiting HMG-CoA reductase outweighs the benefit of using the drug during pregnancy.

Rosucard® is contraindicated during pregnancy and lactation. If pregnancy is diagnosed during therapy, the use of the drug Rosucard® should be stopped immediately, and the patient should be warned about the potential risk to the fetus.

If it is necessary to use the drug during lactation, taking into account the possibility of adverse events in infants, the issue of stopping breastfeeding should be decided.

Side effects

Adverse reactions from using the drug may be as follows:

• nervous system: headache , asthenic syndrome , dizziness ;
• respiratory system: cough, dyspnea ;
• musculoskeletal system: myalgia ;
• skin and subcutaneous tissue: peripheral edema , Stevens-Johnson syndrome ;
• laboratory parameters: transient increase in serum CPK depending on the dosage;
• allergic reactions: itching , urticaria , rash;
• digestive system: nausea, pain in the abdomen, constipation , vomiting, diarrhea ;
• endocrine system: diabetes mellitus type II ;
• urinary system: proteinuria , urinary tract infections.

In rare cases peripheral neuropathy , pancreatitis , memory loss, hepatitis , jaundice , myopathy , rhabdomyolysis , angioedema , hematuria , transient increase and ALT activity .

Instructions for use of Rosucard (Method and dosage)

Before the course of Rosucard, the patient must switch to a standard lipid-lowering diet, which must be maintained throughout the entire therapy. Dosages are determined in each case individually depending on the disease and characteristics of the patients.

For those who have been prescribed Rosucard, the instructions for use indicate that it can be taken at any time, before or after meals.

For hypercholesterolemia , the initial dose recommended by experts is 5 or 10 mg orally. Instructions for use of Rosucard include taking it once a day. The choice of initial dosage should take into account individual cholesterol levels, the likelihood of negative reactions, as well as the risk of developing cardiovascular diseases. After 4 weeks it can be changed. At dosages of 40 mg, specialist supervision and adjustment if necessary are required.

For the prevention of cardiovascular diseases, a daily dose of 20 mg is recommended.

For children over 10 years of age with hereditary hypercholesterolemia , the initial dosage is usually 5 mg/day. During treatment, it can be gradually increased, but not exceed 20 mg. Titration is carried out depending on individual tolerance. Before starting the course of the drug, you must follow a standard diet to reduce cholesterol in the body. During treatment with Rosucard, it is also necessary to adhere to this nutritional system.

Elderly patients (over 70 years of age) are usually prescribed a dosage of 5 mg.

For people with mild or moderate renal impairment, 5 mg is prescribed in most cases at the beginning of the course. During treatment, dosages higher than 40 mg should not be used. In cases of severe renal impairment, this medicine is contraindicated.

For patients of the Mongoloid race and those predisposed to myopathy , an initial dosage of 5 mg is recommended. Taking a dose of 40 mg is strictly contraindicated.

Interaction

Cyclosporine in combination with Rosucard increases its AUC by approximately 7 times. Taking more than 5 mg is not recommended.

Gemfibrozil and other lipid-lowering drugs in combination with Rosucard cause an approximately twofold AUC myopathy increases . The maximum dose when combined with Gemfibrozil is 20 mg. When interacting with fibrates, the drug dosage of 40 mg is not allowed, the initial dose is 5 mg.

Interaction of the drug with protease inhibitors may lead to increased exposure to Rosuvastatin. The use of this combination HIV-infected patients is not recommended.

The combination of Erythromycin and Rosucard reduces the AUC of the latter by 20% and the maximum concentration by 30%.

When this drug is combined with lopinavir + ritonavir, AUC levels increase .

Vitamin K antagonists, when interacting with Rosucard, cause an increase in international normalized ratio .

Ezetimibe combined with Rosuvastatin may cause side effects.

Antacid medications with aluminum or magnesium hydroxide reduce the amount of the drug in the body by approximately half. So between taking them you need to take a break of at least 2 hours.

When combining Rosucard with oral contraceptives, patients' condition should be monitored.

Rozucard's analogues

Level 4 ATX code matches:
Akorta

Atomax

Lipitor

Pravastatin

Simvastol

Owencore

Simgal

Tulip

Lovastatin

Liptonorm

Rozulip

Zokor

Rosart

Tevastor

Atorvastatin

Liprimar

Simvastatin

Atoris

Basilip

Roxera

The following analogues of Rosucard are sold in pharmacies:

• Klyvas;
• Mertenil;
• Rosart;
• Rosuvastatin Sandoz;
• Rozulip;
• Crestor;
• Roxera;
• Romazik;
• Rovics;
• Fastong.

All of them are available in tablet form. The price of analogues varies depending on the content of the active substance and the number of plates in the package. In general, most of them cost more. This is why doctors do not often prescribe Rosucard analogues.

Rosecard price

The price of Rozucard is considered very affordable compared to many analogues. The exact cost of the drug depends on the content of the active substance in the tablets. Thus, the price of Rosucard 10 mg in a package with 3 plates is about 500 rubles in Russia or 100 hryvnia in Ukraine. And the price of Rosucard 20 mg in a package with 3 plates is approximately 640 rubles in Russia or 150 hryvnia in Ukraine.

• Online pharmacies in RussiaRussia
• Online pharmacies in UkraineUkraine

ZdravCity

• Rosucard tablets p.p.o.
  20 mg 90 pcs. Zentiva s.s. RUB 1,914 order
• Rosucard tablets p.p.o. 10 mg 90 pcs. Zentiva s.s.

  RUB 1,311 order

• Rosucard tablets p.p.o. 20 mg 30 pcs. Zentiva s.s.

  RUB 863 order

• Rosucard tablets p.p.o. 10 mg 60 pcs. Zentiva s.s.

  RUR 993 order

• Rosucard tablets p.p.o. 10 mg 30 pcs. Zentiva s.s.

  RUB 588 order

Pharmacy Dialogue

• Rosacard tablets 20 mg No. 60Zentiva

  RUB 1,481 order

• Rosacard tablets 40 mg No. 30Zentiva

  1105 rub. order

• Rosacard tablets 10 mg No. 30Zentiva

  RUR 574 order

• Rosacard tablets 40 mg No. 90Zentiva

  RUB 2,759 order

• Rosacard tablets 10 mg No. 60Zentiva

  RUB 1,087 order

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Pharmacy24

• Rosecard 10 mg No. 30 tablets TOV Zentiva, Czech Republic
  139 UAH.order
• Rosecard 20 mg No. 30 tablets TOV Zentiva, Czech Republic

  190 UAH order

• Rosecard 40 mg No. 30 tablets TOV Zentiva, Czech Republic

  340 UAH. order

• Rosacard 20 mg N90 tablets TOV Zentiva, Czech Republic

  506 UAH order

• Rosacard 10 mg N90 tablets TOV Zentiva, Czech Republic

  304 UAH order

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