Rosuvastatin-Vertex, 10 mg 90 pcs

Directions for use

Orally, do not chew or crush the tablet, swallow it whole with water. The drug may be administered at any time of the day regardless of the time of meals.

Prior to therapy with Rosavastatin the patient should start a standard hypocholesterolemic diet and continue it during treatment.

The dose of the drug should be adjusted individually depending on the goals of therapy and the therapeutic response to treatment, taking into account current recommendations for target lipid concentrations. The recommended starting dose for patients starting to take the drug or for patients transferred from other HMG-CoA reductase inhibitors should be 5 or 10 mg of Rosuvastatin once daily. When choosing the initial dose, individual cholesterol content should be guided and possible risk of cardiovascular complications should be taken into account, as well as the potential risk of side effects should be assessed. If necessary, the dose may be increased to a larger dose in 4 weeks .

In connection with the possible development of side effects when taking a dose of 40 mg, compared with lower doses of the drug (see Due to the possible development of side effects of the 40 mg dose compared to lower doses of the drug (see “Side effects”), the dose increase to 40 mg, after an additional dose above the recommended initial dose for 4 weeks of therapy, may be conducted only in patients with severe hypercholesterolemia and with a high risk of cardiovascular complications (especially in patients with familial hypercholesterolemia), in whom the desired therapy result was not achieved while taking the 20 mg dose and who will be under the supervision of a specialist.

Especially close monitoring of patients receiving the drug at the 40 mg dose is recommended. It is not recommended to prescribe the 40 mg dose to patients who have not previously seen a physician. After 2-4 weeks of therapy and/or if the dose of Rosuvastatin is increased, lipid metabolism should be monitored (if necessary, a dose adjustment is required). The use of the drug in a higher dose than 40 mg is not justified in connection with the increase in the side effects and in most cases is not recommended. Older patients No dose adjustment is required.

Patients with renal impairment :
In patients with renal impairment of mild to moderate severity no dose adjustment is required. In patients with severe renal failure (CKD less than 30 ml/min) the drug Rosuvastatin is contraindicated. The use of the preparation in dose of 40 mg is contraindicated in patients with moderate renal impairment (CKD 30-60 ml/min).

Patients with hepatic impairment : Rosuvastatin is contraindicated in patients with active liver disease Special populations. Ethnic groups When studying pharmacokinetic parameters of rosuvastatin in patients belonging to different ethnic groups, an increase in systemic concentration of rosuvastatin among Japanese and Chinese was noted (see section “Cautionary Note”). This fact should be considered when prescribing Rosuvastatin to these groups of patients.

When prescribing doses of 10 and 20 mg the recommended starting dose for mongoloid patients is 5 mg. Administration of the drug in a dose of 40 mg is contraindicated in patients of mongoloid race (see section “Contraindications”). Genetic polymorphisms Carriers of SLCO1B1 (OATP1B1) c.521CC and ABCG2 (BCRP) c.421AA had increased exposure (AUC) to rosuvastatin compared to carriers of SLCO1B1 c.521TT and ABCG2 c.421CC genotypes. For patients-carriers of c.521CC or c.421AA genotypes the recommended maximum dose of the drug Rosuvastatin is 20 mg once daily.

Patients predisposed to myopathy Administration of the drug in dose of 40 mg is contraindicated in patients with factors that may indicate predisposition to myopathy. When prescribing doses of 10 and 20 mg, the recommended starting dose for this group of patients is 5 mg Concomitant therapy Rosuvastatin binds to various transport proteins (in particular to OATP1B1 and BCRP).

When co-administration of Rosuvastatin with drugs (such as cyclosporine, some HIV protease inhibitors, including the combination of ritonavir with atazanavir, lopinavir and/or tipranavir) that increase the plasma concentration of Rosuvastatin due to interaction with transport proteins, the risk of myopathy (including rhabdomyolysis) may increase.br>
In such cases, the possibility of prescribing alternative therapy or temporary discontinuation of Rosuvastatin should be assessed. If the use of the above drugs is necessary, the benefit-risk ratio of concomitant therapy with Rosuvastatin should be assessed and the possibility of reducing its dose should be considered

Special Instructions

Impaired renal function. In patients receiving high doses of rosuvastatin (in particular, 40 mg/day), tubular proteinuria was observed, which was detected using test strips and in most cases was intermittent or transient. Such proteinuria is not indicative of acute disease or progression of concomitant renal disease.

The incidence of serious renal dysfunction observed in the post-marketing study of rosuvastatin was higher with the 40 mg/day dose. In patients taking the drug at a dose of 30 or 40 mg/day, it is recommended to monitor renal function parameters during treatment (at least once every 3 months). Effect on the musculoskeletal system.

When using rosuvastatin at all doses, but especially at doses exceeding 20 mg/day, the following effects on the musculoskeletal system have been reported: myalgia, myopathy, in rare cases rhabdomyolysis. Very rare cases of rhabdomyolysis have been reported with concomitant use of HMG-CoA reductase inhibitors and ezetimibe. Such combination should be used with caution because pharmacodynamic interaction cannot be excluded. As in case of other HMG-CoA reductase inhibitors, the incidence of rhabdomyolysis in post-marketing use of rosuvastatin is higher when using 40 mg/day

determination of CPK activity. CPK activity should not be determined after strenuous physical activity and in the presence of other possible causes of increase in its activity; it may lead to misinterpretation of the obtained results. If the baseline CPK activity is significantly elevated (5 times the ULN), a repeat analysis should be performed after 5-7 days. The therapy should not be started if the results of the repeated test confirm the initial high activity of CPK (more than 5 times the ULN). Before therapy Depending on the daily dose in patients with existing risk factors for myopathy/rhabdomyolysis, rosuvastatin is either contraindicated or should be administered with caution (see “Contraindications”, “Limitations of use”).

Such factors include: impaired renal function; hypothyroidism; muscle diseases in anamnesis (including family history ofincluding familial); myotoxic phenomena when taking other HMG-CoA reductase inhibitors or fibrates in the history; excessive use of alcohol; age over 65 years; conditions in which plasma concentrations of rosuvastatin may increase; concomitant use of fibrates. In such patients, it is necessary to assess the risk and possible benefit of therapy. Clinical monitoring is also recommended. If baseline CPK activity is more than 5-fold higher compared to IGN, therapy with rosuvastatin should not be started.

During therapy with rosuvastatin, patients should be informed about the need to seek immediate medical attention in case of sudden onset of muscle pain, muscle weakness or cramps, especially in combination with malaise and fever. In such patients, CPK activity should be determined. The therapy should be stopped if CPK activity is significantly increased (more than 5 times of IGN) or muscle symptoms are severe and cause daily discomfort (even if CPK activity is not more than 5 times of IGN).

If symptoms disappear and CPK activity returns to normal, resumption of rosuvastatin or other HMG-CoA reductase inhibitors at lower doses with close medical supervision should be considered. Monitoring of CPK activity in the absence of symptoms is unnecessary. Very rare cases of immune-mediated necrotizing myopathy with clinical manifestations in the form of persistent weakness of proximal muscles and increased serum CPK activity during therapy or upon discontinuation of HMG-CoA reductase inhibitors, including rosuvastatin, have been reported. Additional muscular and nervous system studies, serological studies, as well as therapy with immunosuppressive agents may be required. No evidence of increased skeletal muscle effects with rosuvastatin and concomitant therapy has been noted. However, an increase in myositis and myopathy has been reported in patients taking other HMG-CoA reductase inhibitors in combination with fibric acid derivatives (e.g. gemfibrozil), cyclosporine, nicotinic acid at lipid-lowering doses (over 1 g/day), antifungal agents – azole derivatives, HIV protease inhibitors and macrolide antibiotics. When concomitant use with some HMG-CoA reductase inhibitors, gemfibrozil increases the risk of myopathy. Thus, concomitant use of rosuvastatin and gemfibrozil is not recommended. The benefits of further changes in plasma lipid concentrations when combining this drug with fibrates or nicotinic acid in lipid-lowering doses should be carefully weighed against the possible risk. Rosuvastatin at a dose of 30 mg/day is contraindicated for combined therapy with fibrates.

Due to the increased risk of rhabdomyolysis, rosuvastatin should not be used in patients with acute conditions that may lead to myopathy or conditions predisposing to the development of renal failure (eg, sepsis, arterial hypotension, extensive surgery, trauma, severe metabolic, endocrine and electrolyte disorders or uncontrolled seizures). Liver. Depending on the daily dose, rosuvastatin is contraindicated or should be used with caution in patients with excessive alcohol consumption and/or with a history of liver disease (see “Contraindications”, “Limitations on use”).

It is recommended to determine liver function tests before therapy and 3 months after therapy start. Rosuvastatin should be discontinued or the dose of this drug should be reduced if hepatic serum transaminase activity is 3 times higher than BHN. Patients with hypercholesterolemia due to hypothyroidism or nephrotic syndrome should be treated for underlying diseases before treatment with rosuvastatin. Ethnic peculiarities.

During pharmacokinetic studies, increased plasma concentration of rosuvastatin was observed in mongoloid race compared to Caucasoid race. Interstitial lung disease. When using some HMG-CoA reductase inhibitors, especially for a long time, sporadic cases of interstitial lung disease have been reported.

The manifestations of the disease may include dyspnea, non-productive cough and deterioration of general well-being (weakness, weight loss and fever). If interstitial lung disease is suspected, therapy with HMG-CoA reductase inhibitors should be discontinued. Type 2 diabetes mellitus. In patients with glucose concentrations between 5.6 and 6.9 mmol/L, therapy with rosuvastatin has been associated with an increased risk of developing type 2 diabetes mellitus. Influence on the ability to drive a car or perform work requiring increased speed of physical and mental reactions.

Studies on the effect of rosuvastatin on the ability to drive vehicles and work with mechanisms have not been conducted. Nevertheless, taking into account the possibility of development of dizziness and other side effects, caution should be exercised when driving vehicles and operating other mechanisms that require high concentration and quick psychomotor reactions.

Contraindications

Daily dose up to 30 mg:
hypersensitivity to rosuvastatin; liver diseases in active phase (including persistent increase of hepatic transaminases activity and increase of hepatic transaminases activity in serum more than 3 times as compared to CHF); severe renal insufficiency (creatinine cl .

Daily dose 30 mg and more: Hypersensitivity to rosuvastatin; active hepatic diseases (including steady increase of hepatic transaminases activity and increase of hepatic transaminases activity in serum more than 3 times as compared to IGN); moderate to severe renal insufficiency (creatinine Cl).

Side effects

Side effects observed during administration of rosuvastatin are usually insignificant and pass on their own.

As with other HMG-CoA reductase inhibitors, the incidence of side effects is mainly dose-dependent. Classification of the frequency of side effects by WHO: very common (≥1/10); common (≥1/100,

Blood and lymphatic system disorders: frequency is unknown – thrombocytopenia.

Immune system: rare – hypersensitivity reactions, including angioedema.

Endocrine system: often – diabetes mellitus type 2.

The nervous system: frequently – headache, dizziness, very rarely – loss or reduction of memory; frequency is unknown – peripheral neuropathy.

Respiratory system, chest and mediastinal organs: frequency unknown – cough, shortness of breath.

The digestive system: frequently – constipation, nausea, abdominal pain, rarely – pancreatitis, very rare – jaundice, hepatitis, the frequency is unknown – diarrhea. When using rosuvastatin, a dose-dependent increase in plasma hepatic transaminase activity is observed in a small number of patients. In most cases it is insignificant, asymptomatic and temporary.

Skin and subcutaneous tissue: infrequent – skin itching, skin rash, urticaria, the frequency is unknown – Stevens-Johnson syndrome.

Musculoskeletal and connective tissue: common – myalgia, rare – myopathy (including myositis), rhabdomyolysis (with or without acute renal failure), very rare – arthralgia, frequency unknown – immune mediated necrotizing myopathy. A dose-dependent increase in plasma CPK activity has been observed in a small number of patients taking rosuvastatin. In most cases, it is insignificant, asymptomatic and temporary. In case of an increase in plasma CPK activity of more than 5 times the ULN the therapy should be suspended.

Renal and urinary tract disorders: proteinuria may be detected in patients receiving rosuvastatin therapy. Changes in the amount of protein in the urine (from no or trace amounts to ++ or more) are observed in less than 1% of patients receiving 10-20 mg rosuvastatin and in about 3% of patients receiving a dose of 40 mg/day. Little change in urinary protein counts has been observed with the 20 mg dose. In most cases proteinuria decreases or disappears during therapy and does not indicate the occurrence of acute or progression of existing renal disease; very rarely – hematuria.

Genital and mammary glands: frequency is unknown – gynecomastia.

General disorders and disorders at the injection site: frequently – asthenic syndrome; frequently unknown – peripheral edema. Laboratory parameters: hyperglycemia, increased concentration of bilirubin in blood plasma, GGTP activity, alkaline phosphatase in blood plasma, changes in serum concentration of thyroid hormones.

When using some HMG-CoA reductase inhibitors (statins) the following side effects have been reported: depression, sleep disorders, including insomnia and nightmares, sexual dysfunction, increased concentration of glycosylated hemoglobin. Single cases of interstitial lung disease have been reported, especially with long-term use of these drugs

Overdose

Symptoms: the clinical picture of overdose is not described.

Pregnancy use

Rosuvastatin is contraindicated in pregnancy and lactation. Women of reproductive age should use adequate methods of contraception.

Since Chs and substances synthesized from Chs are important for fetal development, the potential risk of HMG-CoA reductase inhibition for the fetus exceeds the benefit of using rosuvastatin in pregnancy. In case of pregnancy during therapy the use of the drug should be immediately discontinued.

There are no data on excretion of rosuvastatin with breast milk (it is known that other HMG-CoA reductase inhibitors can be excreted with breast milk), therefore during breast-feeding the drug should be discontinued. Fetal category of action according to FDA is X.

Similarities

Mertenil, Crestor, Rosulip, Rosucard, Rosart, Rosuvastatin, Rosistarque, Roxera, Suvardio, Rosuvastatin NW, Cardiolip