Rozart, 90 pcs., 10 mg, film-coated tablets
Effect on kidney function.
In patients receiving high doses of rosuvastatin (mainly 40 mg), tubular proteinuria was observed during urine dipstick analysis, which in most cases was transient. This proteinuria did not indicate acute kidney disease or progression of kidney disease. The incidence of post-marketing reports of serious renal adverse reactions was higher in patients receiving rosuvastatin 40 mg.
When using the drug Rozart at a dose of 40 mg, it is recommended to monitor kidney function indicators during treatment.
Effect on the musculoskeletal system.
Myalgia, myopathy and, in rare cases, rhabdomyolysis have been reported with all doses of rosuvastatin, particularly with doses greater than 20 mg. In very rare cases, rhabdomyolysis has been reported while taking HMG-CoA reductase inhibitors and ezetimibe. In this case, a pharmacodynamic interaction cannot be excluded, so caution should be exercised when taking them together. As with other HMG-CoA reductase inhibitors, the incidence of post-marketing reports of rhabdomyolysis associated with rosuvastatin was higher with the 40 mg dose.
Determination of CPK.
Determination of CPK activity should not be carried out after intense physical activity or in the presence of other possible reasons for an increase in its activity, which may lead to incorrect interpretation of the results obtained. If the initial CPK activity is significantly increased, a repeat measurement should be taken after 5-7 days; therapy should not be started if the repeat test confirms the initial CPK activity (5 times higher than normal).
Before starting therapy.
Caution should be exercised when prescribing Rozart, as well as when prescribing other HMG-CoA reductase inhibitors, to patients with existing risk factors for the development of myopathy/rhabdomyolysis (see
Caution
).
It is necessary to consider the balance between the expected benefit of therapy and the potential risk and conduct clinical monitoring throughout the course of treatment. If the initial activity of CPK is significantly increased (5 times higher than the ULN), then treatment with the drug should not be started.
During treatment.
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 CPK activity is significantly increased (more than 5 times compared to ULN) or muscle symptoms are severe and cause daily discomfort (even if CPK activity is 5 times less than ULN).
If symptoms disappear and CPK activity returns to normal, re-prescribing Rozart 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 discontinuation of statins, incl. rosuvastatin. 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 lipid-lowering doses ≥1 g/day, azole antifungals, protease inhibitors and macrolide antibiotics. Gemfibrozil increases the risk of developing myopathy when taken concomitantly with certain HMG-CoA reductase inhibitors, therefore the simultaneous use of gemfibrozil and rosuvastatin is not recommended. The ratio of expected benefits and potential risks should be carefully weighed when using the drug Rozart and fibrates or nicotinic acid in lipid-lowering doses ≥1 g/day together.
Taking the drug Rozart at a dose of 40 mg simultaneously with fibrates is contraindicated (see “Interaction” and “Contraindications”).
During treatment, especially during the period of dose adjustment of the drug Rosart, the lipid profile should be monitored every 2-4 weeks and, according to it, the dose of the drug should be changed if necessary.
Rosart should not be taken by patients with acute and severe symptoms of myopathy or with risk factors predisposing to the development of renal dysfunction and secondary rhabdomyolysis (for example, sepsis, arterial hypotension, major surgical interventions, trauma, severe metabolic disorders, severe endocrine disorders and severe disturbances in water and electrolyte balance, uncontrolled seizures).
Effect on liver function.
Like other HMG-CoA reductase inhibitors, rosuvastatin should be used with caution in patients with alcohol abuse and/or a history of liver disease.
It is recommended to determine liver function indicators before starting therapy and 3 months after starting therapy. Taking Rozart should be stopped or the dose reduced if the level of hepatic transaminase activity in the blood serum 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 Rozart. During post-marketing surveillance of rosuvastatin, the incidence of reports of serious liver dysfunction (expressed primarily as increased liver transaminases) was higher when taking a dose of 40 mg.
Ethnic groups.
During pharmacokinetic studies among patients of the Mongoloid race compared to Caucasians, an increase in the systemic concentration of rosuvastatin was noted (see “Dosage and Administration” and “Pharmacokinetics”).
HIV protease inhibitors.
During co-administration of rosuvastatin and a combination of various HIV protease inhibitors with ritonavir, an increase in the systemic concentration of rosuvastatin is observed. The decrease in blood lipid concentrations should be carefully assessed, and the possible increase in rosuvastatin in the blood plasma should also be taken into account at the beginning of treatment and during the period of increasing the dose of the drug Rozart in patients with HIV taking HIV protease inhibitors. Concomitant use of HIV protease inhibitors is not recommended without dose adjustment of rosuvastatin (see “Dosage and Administration” and “Interaction”).
Interstitial lung disease.
Isolated cases of interstitial lung disease have been reported with the use of certain HMG-CoA reductase inhibitors, especially over long periods of time. Manifestations of the disease may include shortness of breath, non-productive cough and deterioration in general health (weakness, weight loss and fever). If interstitial lung disease is suspected, therapy with HMG-CoA reductase inhibitors should be discontinued.
Diabetes mellitus type 2.
Some evidence suggests that HMG-CoA reductase inhibitors increase blood glucose concentrations and increase the likelihood of developing type 2 diabetes in some patients. However, this risk is outweighed by the ability of HMG-CoA reductase inhibitors to reduce the risk of vascular complications, so this finding is not is a reason to interrupt treatment with rosuvastatin. It is necessary to establish clinical observation and conduct a biochemical blood test according to national standards in patients at risk of developing hyperglycemia (blood glucose concentration 5.6–6.9 mmol/l, body mass index >30 kg/m2, triglyceridemia, arterial hypertension). One study of rosuvastatin reported an overall incidence of diabetes mellitus of 2.8% in the rosuvastatin group and 2.3% in the placebo group, primarily in patients with fasting glucose levels of 5.6–6.9 mmol/L.
Lactose intolerance.
The drug Rozart should not be taken by patients with lactose intolerance, lactase deficiency and glucose-galactose malabsorption, since it contains lactose monohydrate.
Impact on the ability to drive vehicles and machinery.
No studies have been conducted to study the effect of rosuvastatin on the ability to drive vehicles and operate machinery. Patients should be careful when driving vehicles and engaging in potentially hazardous activities, as Dizziness may occur during therapy.
Rosart
Effect on kidney function
In patients receiving high doses of rosuvastatin (mainly 40 mg), tubular proteinuria was observed during urine dipstick analysis, which in most cases was transient. This proteinuria did not indicate acute kidney disease or progression of kidney disease. The incidence of post-marketing reports of serious renal adverse reactions was higher in patients receiving rosuvastatin 40 mg.
When using the drug Rozart at a dose of 40 mg, it is recommended to monitor kidney function indicators during treatment.
Effect on the musculoskeletal system
Myalgia, myopathy and, in rare cases, rhabdomyolysis have been reported with all doses of rosuvastatin, and particularly with doses greater than 20 mg. In very rare cases, rhabdomyolysis has been reported while taking HMG-CoA reductase inhibitors and ezetimibe. In this case, a pharmacodynamic interaction cannot be excluded, so caution should be exercised when taking them together. As with other HMG-CoA reductase inhibitors, the incidence of post-marketing reports of rhabdomyolysis associated with rosuvastatin was higher with the 40 mg dose.
Determination of creatine phosphokinase
Determination of CPK activity should not be carried out after intense physical activity or in the presence of other possible reasons for an increase in its activity, which may lead to incorrect interpretation of the results obtained. If the initial CPK activity is significantly increased, a repeat measurement should be taken after 5-7 days; therapy should not be started if a repeat test confirms the initial CPK activity (5 times higher than normal).
Before starting therapy
Caution should be exercised when prescribing Rozart, as well as when prescribing other HMG-CoA reductase inhibitors, to patients with existing risk factors for the development of myopathy/rhabdomyolysis (see section Caution).
It is necessary to consider the balance between the expected benefit of therapy and the potential risk and conduct clinical monitoring throughout the course of treatment. If the initial activity of CPK is significantly increased (5 times higher than the ULN), then treatment with the drug should not be started.
During treatment
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 CPK activity is significantly increased (more than 5 times the ULN) or if muscle symptoms are severe and cause daily discomfort (even if CPK activity is 5 times less than the ULN). If symptoms disappear and CPK activity returns to normal, re-prescribing Rozart 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 of persistent proximal muscle weakness and increased serum CPK activity during treatment or discontinuation of statins, including rosuvastatin. 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 lipid-lowering doses > 1 g / day, azole antifungals, inhibitors proteases and macrolide antibiotics. Gemfibrozil increases the risk of developing myopathy when taken concomitantly with certain HMG-CoA reductase inhibitors, therefore the simultaneous use of gemfibrozil and rosuvastatin is not recommended. The ratio of expected benefits and potential risks should be carefully weighed when using the drug Rozart together with fibrates or nicotinic acid in lipid-lowering doses > 1 g / day. Taking the drug Rozart at a dose of 40 mg simultaneously with fibrates is contraindicated (see sections Interaction with other drugs and Contraindications
). During treatment, especially during the period of dose adjustment of the drug Rozart, the lipid profile should be monitored every 2-4 weeks and, according to it, the dose of the drug should be changed if necessary. Rosart should not be taken by patients with acute and severe symptoms of myopathy or with risk factors predisposing to the development of renal dysfunction and secondary rhabdomyolysis (for example, sepsis, arterial hypotension, major surgical interventions, trauma, severe metabolic disorders, severe endocrine disorders and severe disturbances in water and electrolyte balance, uncontrolled seizures).
Effect on liver function
Like other HMG-CoA reductase inhibitors, rosuvastatin should be used with caution in patients who abuse alcohol and/or have a history of liver disease. It is recommended to determine liver function indicators before starting therapy and 3 months after starting therapy. Taking Rozart should be stopped or the dose reduced if the level of hepatic transaminase activity in the blood serum 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 Rozart. During post-marketing surveillance of rosuvastatin, the frequency of reports of the development of serious liver dysfunction (expressed mainly in increased activity of hepatic transaminases) was higher when taking a dose of 40 mg.
Ethnic groups
During pharmacokinetic studies among patients of the Mongoloid race compared with Caucasians, an increase in the systemic concentration of rosuvastatin was noted (see section Dosage and Administration and Pharmacokinetics
).
HIV protease inhibitors
During co-administration of rosuvastatin and a combination of various HIV protease inhibitors with ritonavir, an increase in the systemic concentration of rosuvastatin is observed. The decrease in blood lipid concentrations should be carefully assessed, and the possible increase in rosuvastatin in the blood plasma should also be taken into account at the beginning of treatment and during the period of increasing the dose of the drug Rozart in patients with HIV taking HIV protease inhibitors. Concomitant use of HIV protease inhibitors is not recommended without dosage adjustment of rosuvastatin (see Dosage and Administration and Interactions with other medicinal products
).
Interstitial lung disease
Isolated cases of interstitial lung disease have been reported with the use of certain HMG-CoA reductase inhibitors, especially over long periods of time. Manifestations of the disease may include shortness of breath, non-productive cough and deterioration in general health (weakness, weight loss and fever). If interstitial lung disease is suspected, therapy with HMG-CoA reductase inhibitors should be discontinued.
Diabetes mellitus type II
Some evidence suggests that HMG-CoA reductase inhibitors increase blood glucose concentrations and increase the likelihood of developing type 2 diabetes in some patients. However, this risk is outweighed by the ability of HMG-CoA reductase inhibitors to reduce the risk of vascular complications, so this fact is not a reason to interrupt treatment with rosuvastatin. It is necessary to establish clinical observation and conduct a biochemical blood test according to national standards in patients at risk of developing hyperglycemia (blood glucose concentration 5.6-6.9 mmol/l, body mass index > 30 kg/m2, triglyceridemia, arterial hypertension). One study of rosuvastatin reported an overall incidence of diabetes mellitus of 2.8% in the rosuvastatin group and 2.3% in the placebo group, primarily in patients with fasting glucose 5.6 to 6.9 mmol/L.
Lactose intolerance
The drug Rozart should not be taken by patients with lactose intolerance, lactase deficiency and glucose-galactose malabsorption, since it contains lactose monohydrate.
