Index of drugs

Primary hypercholesterolemia in adults, adolescents and children aged 10 years or older (type IIa, with the exception of familial heterozygous hypercholesterolemia) or mixed dyslipidemia (type IIb) as complementary treatment to the diet when using diet and other non-pharmacological treatments (eg physical exercise) , weight loss) is insufficient. Familial homozygous hypercholesterolemia as adjuvant therapy to diet and other lipid-lowering treatments (e.g., LDL apheresis) or if other treatments are inappropriate. Prevention of major cardiovascular events in patients at high risk of this event for the first time, together with activities aimed at reducing other risk factors.

1 tabl powl. contains 5 mg, 10 mg, 20 mg or 40 mg of Rosuvastatin in the form of a Calcium salt; tablets contain lactose.

Rosuvastatin is a selective and competitive inhibitor of HMG-CoA reductase, an enzyme that determines the rate of conversion of 3-hydroxy-3-methylglutaryl-coenzyme A to mevalonate, a precursor to cholesterol. Rosuvastatin increases the number of receptors for LDL on the surface of liver cells, which facilitates the capture and catabolism of LDL, inhibits the production of VLDL in the liver, leading to a reduction in the total amount of LDL and VLDL. After oral administration, rosuvastatin reaches C_max after about 5 hours. Absolute bioavailability is about 20%. It binds to plasma proteins, mainly to albumin, in about 90%. It is metabolized to a small extent (10%). About 90% of rosuvastatin is excreted unchanged with faeces (both absorbed and unabsorbed). The remaining part is excreted in the urine, about 5% in unchanged form. T_0,5 in the elimination phase, it is about 19 hours.

Hypersensitivity to rosuvastatin or other components of the preparation. Active liver disease, including unexplained, persistently elevated serum transaminase activity and more than 3-fold increase above the upper limit of normal (ULN) activity of one of them. Severe renal impairment (creatinine clearance <30 ml / min). Myopathy. Simultaneous treatment with cyclosporin. Pregnancy. Breastfeeding period. Women of childbearing potential not using effective methods of contraception. In addition, the 40 mg dose is contraindicated in patients with predisposing factors for myopathy or rhabdomyolysis; they include: moderate renal impairment (creatinine clearance <60 ml / min), hypothyroidism, genetically determined muscular disease in a patient or members of his family, signs of muscle damage after using another HMG-CoA reductase inhibitor or a fibrate drug, alcohol abuse, situations in which blood levels may increase, Asian origin, concomitant use of fibrates.

Rosuvastatin should be used with caution in patients with predisposing factors for myopathy or rhabdomyolysis such as: renal dysfunction, hypothyroidism, genetically determined muscular disease in a patient or members of his family, signs of muscle damage after using another HMG-CoA reductase inhibitor or fibrates , alcohol abuse, age> 70 years, situations where blood levels may rise (eg in Asian patients with rosuvastatin exposure increased). The risk of myopathy may also be increased when rosuvastatin is co-administered with: gemfibrozil (do not use together), other fibrin derivatives (use caution, do not use together in rosuvastatin 40 mg patients), nicotinic acid, ezetimibe (caution), inhibitors proteases (do not use together), cyclosporin (do not use together). In groups of patients with an increased risk of myopathy, the risk and possible benefits of treatment should be considered, and the patient should be monitored during treatment.Before initiating rosuvastatin therapy, creatine kinase (CK) should be measured; if it is significantly increased (> 5 x ULN), follow-up should be carried out after 5-7 days. Treatment should not be initiated if the control CK> 5 x ULN. If you experience unexplained muscle pain, muscle weakness or muscle cramps during rosuvastatin treatment, especially if you feel unwell or have a fever, test for CK; treatment should be discontinued if the CK activity is significantly increased (> 5 times ULN) or if the muscle symptoms are severe and cause discomfort during daily activities (even if the CK activity ≤5 times ULN). After the clinical symptoms have resolved and CK levels are reduced to normal, re-application of the product or other HMG-CoA inhibitor at the lowest dose may be considered, with close observation of the patient. If the patient does not have clinical symptoms, routine CK activity monitoring is not necessary. Do not use the product if you have severe, severe symptoms suggestive of myopathy or predisposing to secondary renal failure as a result of rhabdomyolysis (eg sepsis, hypotension, extensive surgery, trauma, severe metabolic, endocrine and electrolyte or uncontrolled convulsions) . The drug should be used with caution in patients who are abusing alcohol and / or have a history of liver disease. It is recommended that liver function tests be performed before treatment and 3 months after its initiation. The drug should be discontinued or the dose reduced if the aminotransferase activity is more than 3-fold greater than ULN. In patients with secondary hypercholesterolaemia caused by hypothyroidism or nephrotic syndrome, appropriate treatment of the underlying disease should be initiated prior to treatment initiation. Due to the increased risk of proteinuria, patients undergoing 40 mg should be considered for monitoring renal function during routine follow-up visits. If the patient is suspected of developing interstitial lung disease (manifested by dyspnoea, dry cough, general deterioration of health - fatigue, weight loss, fever), statin therapy should be discontinued. Statins can cause an increase in blood Glucose and in some patients at risk for developing diabetes can cause hyperglycaemia, which requires proper diabetes care. However, this risk should not be a reason for discontinuation of statin therapy, because the benefits of reducing the risk of vascular disorders due to the use of statins are greater. Patients at risk (with a fasting glucose level of 5.6-6.9 mmol / l, BMI> 30 kg / m², increased triglycerides, hypertension) should be monitored both clinically and biochemically in accordance with national guidelines. Experience regarding the use of rosuvastatin in children <10 years of age is limited to a small number of patients (between 8 and 10 years of age) with familial homozygous hypercholesterolemia, therefore the drug is not recommended for use in children <10 years of age. Due to the lactose content, the drug should not be used in patients with rare hereditary galactose intolerance, lactase deficiency (Lapp type) or malabsorption of glucose-galactose.

Use during pregnancy and breast-feeding is contraindicated. Patients of childbearing age should use effective methods of contraception.

Common: diabetes (prevalence depending on risk factors: fasting glucose level ≥5,6 mmol / l, BMI> 30 kg / m², increased triglyceride levels, history of hypertension), headache and dizziness, constipation, nausea, abdominal pain, muscle pain, weakness. Uncommon: pruritus, rash, urticaria. Rare: thrombocytopenia, hypersensitivity reactions (including angioneurotic edema), pancreatitis, increased hepatic transaminases, myopathy (including myositis) and rhabdomyolysis. Very rare: polyneuropathy, memory loss, jaundice, hepatitis, arthralgia, hematuria, gynecomastia. Frequency unknown: depression, sleep disorders (including insomnia and nightmares), cough, dyspnoea, diarrhea, Stevens-Johnson syndrome, edema.Rosacea has been observed in rosuvastatin-treated patients (mainly of tubular origin, particularly in patients treated with high doses, and no evidence of proteinuria prior to the onset of acute or progressive kidney disease); increase in creatine kinase activity. For some statins, the following side effects have been reported: sexual dysfunction, interstitial lung disease (especially during long-term use), tendon disorders (in some cases complicated by tendon rupture). The incidence of rhabdomyolysis, severe adverse reactions from the kidneys and liver is higher after a dose of 40 mg. In children and adolescents, an increase in CK> 10 x ULN and muscle symptoms were observed more frequently than in adult patients.

Orally. Dosage should be determined individually, in accordance with current recommendations, depending on the purpose of therapy and patient's response to treatment. Before and during treatment, the patient should use a diet to reduce cholesterol.Treatment of hypercholesterolemia: initially 5-10 mg once daily, both in patients who have not been previously treated with other statin drugs, as well as in those treated with other HMG-CoA reductase inhibitors. If necessary, the dose may be increased after 4 weeks of treatment. Due to the increased incidence of side effects after administration of the 40 mg dose, this dose may only be considered in patients with severe hypercholesterolaemia (with the exception of familial heterozygous hypercholesterolaemia) who are at high risk of developing cardiovascular disease (especially patients with familial homozygous hypercholesterolemia) in which the expected goal of treatment has not been achieved after 20 mg. Treatment with a 40 mg dose should be carried out under the supervision of a specialist.Prevention of cardiovascular events20 mg daily.Special groups of patients. In the elderly (> 70 years), in patients with moderate renal impairment (creatinine clearance <60 ml / min), in patients with predisposing factors for myopathy and Asian patients, the recommended starting dose is 5 mg.Children: use of the drug in children should be carried out by a specialist; drug is not recommended for use in children <10 years.
The preparation can be taken at any time of the day, with or without food.