Expiration date: 03/2025

Composition

1 tablet contains:

active substance: rosuvastatin 5, 10, 20 or 40 mg

excipients: cellulose microcrystalline, crospovidone, calcium hydrogen phosphate dihydrate, lactose monohydrate, magnesium stearate,

film coating: Opadry pink II 33G240007 (hypromellose-2910, titanium dioxide, lactose monohydrate, macrogol-3350, triacetin, dye Carmine red)

Pharmacological action

Rosart - lipid-lowering drugs from the group of statins. Selective competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme a (HMG-COA) reductase – the enzyme that transforms HMG-COA to mevalonate, a precursor of cholesterol.

Increases the number of receptors of low density lipoproteins (LDL) on the surface of hepatocytes, which leads to increased capture and catabolism of LDL, inhibition of synthesis of very low density lipoproteins (VLDL), reducing the total number of LDL and VLDL. Lowers high cholesterol-LDL, cholesterol-lipoproteinov high density (nelup), cholesterol-VLDL, total cholesterol, triglycerides (TG), TG-VLDL, apolipoprotein b (Apob), reduces the ratio of LDL cholesterol/HDL-cholesterol, total cholesterol/HDL-cholesterol, cholesterol-elpvp/cholesterol-HDL, Apob/apolipoprotein A-I (Apoa-I), increases the concentration of HDL-cholesterol, the level of Apoa-I.

Hypolipidemic action directly proportional to the administered dose. The therapeutic effect appears within 1 week after the start of therapy, after 2 weeks achieves 90% of maximum, for 4 weeks reaches a maximum and then remains constant. 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 IIa and IIb hypercholesterolemia (Fredrickson classification) with an average baseline LDL cholesterol of about 4.8 mmol/l in patients receiving the drug in a dose of 10 mg LDL cholesterol reaches values of less than 3 mmol/l in patients with homozygous familial hypercholesterolemia taking the drug at a dose of 20 mg and 40 mg, the mean reduction of LDL cholesterol of 22 percent.

The additive effect observed in combination with fenofibrate (to reduce the concentration of triglycerides (TG) and nicotinic acid in lipidemias doses (to reduce the concentration of cholesterol-HDL).

Testimony

Primary hypercholesterolemia (type IIA according to Fredrickson), including heterozygous inherited hypercholesterolemia) or mixed (combined) hyperlipidemia (type IIb according to Frederickson), as an adjunct to diet and other non-pharmacological interventions (physical activity and weight loss),

The homozygous form of familial hypercholesterolemia with the ineffectiveness of diet and other treatments aimed at reducing the level of lipids (e.g., LDL apheresis) or if such treatments are not suitable for the patient.

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

For slowing the progression of atherosclerosis as an adjunct to diet in patients who have shown therapy for reducing the concentration of total cholesterol and LDL cholesterol.

Prevention of major cardiovascular complications (stroke, infarction, arterial revascularization) in adults without clinical signs of coronary heart disease (CHD), but with an increased risk of its development (age older than 50 years for men and over 60 for women, increased concentration of C-reactive protein (? 2 mg/l) in the presence of at least one of additional risk factors such as hypertension, low concentration of HDL-cholesterol, Smoking, family history of early CHD).

Contraindications

• Hypersensitivity to rosuvastatin or other components of the drug,
  
• Liver disease in the active phase, including a persistent increase in serum activity of "liver" transaminases (more than 3 times compared with the upper limit of normal (ULN)) of unknown origin,
  
• Expressed by the human kidney (KK less 30 ml/min),
  
• Myopathy,
  
• Concurrent administration of cyclosporine,
  
• Women of reproductive age not using adequate contraceptive methods 
  
• Pregnancy and lactation,
  
• The age of 18 years (efficacy and safety not established),
  
• Lactose intolerance, lactase deficiency, glucose-galactose malabsorption (the drug contains lactose monohydrate).
  
• With caution:
  

The presence of risk factors for myopathy and/or rhabdomyolysis - renal insufficiency (QC more 30 ml/min), hypothyroidism, personal or family history of hereditary muscular diseases and previous history of myotoxicity the use of other inhibitors of HMG-COA reductase inhibitors or fibrates, excessive alcohol use, age older than 70 years, a condition in which increased plasma concentrations of rosuvastatin, race (Mongoloid race), concurrent use with fibrates, liver diseases in history, sepsis, arterial hypotension, extensive surgical interventions, injuries, severe metabolic, endocrine or electrolyte disorders or uncontrolled epilepsy.

Application of pregnancy and breastfeeding

Rosart, the drug is contraindicated in pregnancy and lactation.

The use of the drug Rosart  in women of reproductive age is possible only if you use reliable methods of contraception, and if the patient informed about the possible risk of treatment for the fetus.

Because cholesterol and cholesterol substances, synthesized from cholesterol important for the development of the fetus, the potential risk of inhibition of HMG-COA reductase is greater than the benefit derived from the use of the drug during pregnancy. In the case of confirmation of pregnancy in the process of drug therapy Rosart, the drug should be immediately discontinued and the patient advised of the potential risk to the fetus.

Data concerning the allocation of rosuvastatin in breast milk is not available, so if you need the use of the drug during lactation because of the possibility of adverse events in infants should solve the issue of termination of breastfeeding.

Method of application and doses

Inside, without chewing or crushing, swallowed whole with water at any time of the day regardless of the meal.

Before the start of drug therapy Rosart, the patient must begin to comply with the standard hypolipidemic diet and continue to observe her during treatment. The dose should be selected individually depending on indications and therapeutic response, taking into account current generally accepted guidelines for target levels of lipids. The recommended initial dose of the drug Rosart for patients who start taking the drug or for patients transferred from the reception of other inhibitors of HMG-COA reductase is 5 or 10 mg 1 times/day. When selecting the starting dose should be guided by the content of cholesterol in a patient and to take into account the risk of developing cardiovascular complications, and to assess the potential risk of side effects. If necessary, after 4 weeks the dose can be increased.

In connection with the possible development of side effects when taking doses of 40 mg compared with lower doses of the drug (see section "Side effects"), a final titration to the maximum dose of 40 mg should only be performed in patients with severe hypercholesterolemia and high risk of cardiovascular complications (especially in patients with hereditary hypercholesterolemia), which in the dose of 20 mg was not achieved the target cholesterol level, and who will be under medical supervision.

Especially advised careful monitoring of patients receiving the drug in a dose of 40 mg After 2-4 weeks of therapy and/or increase in dosage necessary to control lipid metabolism.

In elderly patients dose adjustment is not required.

In patients with hepatic impairment of child-Pugh below 7 points correction dose is not required. Patients with values of 8 and 9 points on a scale child-Pugh should be a preliminary assessment of kidney function. Experience with the use of rosuvastatin in patients with hepatic impairment than 9 points on a scale child-Pugh missing.

In renal insufficiency, mild or moderate severity dose adjustment is not required. It is recommended that the initial dose of 5 mg for patients with renal failure of moderate severity (KK less 60 ml/min). Patients with renal insufficiency medium severity (QC less than 30-60 ml/min) the drug at a dose of 40 mg is contraindicated. The drug Rosart contraindicated at any dose patients with severe renal failure (KK less 30 ml/min).

Ethnic groups

Patients of Asian race may increase systemic concentrations of rosuvastatin. When assigning doses 10 and 20 mg initial recommended dose for patients of Asian origin is 5 mg. the drug is administered at a dose of 40 mg such patients is contraindicated.

Patients predisposed to the development of myopathy

When assigning doses 10 and 20 mg initial recommended dose for these patients is 5 mg. the drug is administered at a dose of 40 mg in these patients is contraindicated.

Side effects

From the Central nervous system: often – headache, dizziness, asthenic syndrome, rarely – depression, anxiety, insomnia, paraesthesia, rarely peripheral neuropathy, memory loss.

From the digestive system: often – nausea, constipation, abdominal pain, rarely – vomiting, diarrhea, flatulence, rarely - pancreatitis, very rarely – hepatitis, jaundice.

The respiratory system: often – pharyngitis, rarely – rhinitis, sinusitis, asthma, bronchitis, cough, dyspnoea, pneumonia.

From the side of cardiovascular system: rarely – angina, high blood pressure, palpitations, vasodilation.

From the endocrine system: often – sugar diabetes. (In the JUPITER study, the reported overall frequency 2.8% in rosuvastatin group and 2.3% in the placebo group, mostly in patients with fasting glucose 5.6 to 6.9 mmol/L.)

From the side of musculoskeletal system: often – myalgia, rarely – arthralgia, myopathy (including myositis), rhabdomyolysis, back pain, hypertonia, pathological fracture of the extremities, a very rare immune-mediated necrotizing myopathy.

Allergic reactions: rare – skin itching, rash, hives, rarely – angioedema.

Skin and subcutaneous tissue: frequency unknown - Stevens-Johnson syndrome.

From the urinary system: often – proteinuria (mostly in patients receiving a dose of 40 mg), decreasing in the process of therapy and not associated with the occurrence of kidney disease, urinary tract infection, rarely – peripheral edema, abdominal pain, rarely - hematuria.

Laboratory parameters: rare – transient dose-dependent increase in the activity of serum creatine phosphokinase (CPK), while increasing more than 5 times compared with CAH therapy should be temporarily suspended rare – tranzithornoe increase in aspartate aminotransferase and alanine aminotransferase.

Other: often – back pain, nasopharyngitis, rarely reduced potency. 

As the use of other inhibitors of HMG-COA reductase, the frequency of occurrence is dose dependent in nature, side effects are usually expressed slightly and are themselves.

Special instructions

During treatment, especially during dose adjustment of the drug Rosart, every 2-4 weeks should monitor the lipid profile and according to it if you need to change the dose.

Recommended definition of indicators of liver function before therapy and 3 months after initiation of therapy. The drug Rosart should stop or reduce the dose of the drug, if the level of activity of “hepatic” transaminases in serum in 3 times the VGN.

In applying the drug Rosart at a dose of 40 mg is recommended to monitor indicators of kidney function.

In patients with hypercholesterolemia due to hypothyroidism or nefroticski syndrome therapy major diseases should be carried out before the start of drug treatment Rosart.

In patients with existing risk factors for rhabdomyolysis it is necessary to consider the ratio of expected benefits and potential risks and conduct clinical observation throughout the entire course of treatment.

Should inform the patient about the need for an immediate message to the doctor about the cases of sudden occurrence of muscle pain, muscle weakness or cramps, especially in combination with malaise and fever. These patients should determine the level of CPK. Therapy should be discontinued if the CPK level increased significantly (more than 5 times compared with CAH), or if muscle symptoms are pronounced and cause daily discomfort. If the symptoms disappear and the CPK level returned to normal, you should consider re-administering the drug Rosart or other inhibitors of HMG-COA reductase in smaller doses with careful monitoring of the patient.

The definition of CPK should not be after intense exercise or if there are other possible reasons for the increase in ck, which may lead to misinterpretation of the results. If the baseline CPK is significantly elevated, 5-7 days should be a re – measurement should not start therapy if the second test confirms the initial level of CPK (in 5 times above normal).

Routine monitoring of CPK in the absence of symptoms is inappropriate.

There is a reported increase in the incidence of myositis and myopathy in patients taking other inhibitors of HMG-COA reductase inhibitor in combination with fibrin acid derivatives (including gemfibrozil), cyclosporine, nicotinic acid, azole antifungals, protease inhibitors and macrolide antibiotics. You should carefully weigh the ratio of expected benefits and potential risks in a joint application of the drug Rosart and fibrates or Niacin are not recommended co-administration of gemfibrozil.

In most cases, proteinuria decreases or disappears during therapy and does not mean the occurrence of acute or exacerbation of existing kidney problems. Assessment of renal function should be performed during routine evaluation of patients receiving a dose of 40 mg.

Women of childbearing age should use adequate methods of contraception. Because cholesterol and cholesterol substances, synthesized from cholesterol important for the development of the fetus, the potential risk of inhibition of HMG-COA reductase is greater than the benefit derived from the use of the drug during pregnancy. In case of pregnancy during therapy, the drug should be immediately discontinued. Data concerning the allocation of rosuvastatin with milk women, so breast-feeding should be discontinued.

Not recommended joint appointment of rosuvastatin and inhibitors of HIV protease.

Effects on ability to drive vehicles and mechanisms.

When you drive vehicles and activities potentially hazardous activities patients should be aware that during the treatment may occur dizziness.

Overdose

Treatment: there is no specific treatment, symptomatic therapy is carried out under the monitoring of liver function and activity of KFK. Hemodialysis is ineffective.

Storage conditions

Does not require special storage conditions. Keep out of reach of children!

Shelf life

30 months.