Roxera pills 10mg №90

Packaging

90 pcs.

Indications and usage

• Fredrickson primary hypercholesterolemia (type IIa) or mixed dyslipidemia (type IIb) as a supplement to the diet with ineffective diet and other non-pharmacological treatments (for example, exercise, weight loss);
• familial homozygous hypercholesterolemia as an adjunct to diet and other lipid-lowering therapy (for example, LDL-apheresis) or if such therapy is not effective;
• hypertriglyceridemia (type IV according to Fredrickson) as an addition to the diet;
• to slow the progression of atherosclerosis as a supplement to the diet in patients who have been shown therapy to reduce the plasma concentration of cholesterol and LDL-C;
• primary prevention of major cardiovascular complications (stroke, myocardial infarction, arterial revascularization) in adult patients without clinical signs of coronary heart disease (CHD), but with an increased risk of its development (women older than 50 years for men and older than 60 years for women, increased plasma concentration of C-reactive protein (≥2 g / l) in the presence of at least one of the additional risk factors, such as: hypertension, low plasma concentration of HDL-C, smoking, early onset of CHD in family m anamnesis).

Contraindications

• Daily dose up to 30 mg
• hypersensitivity to Rosuvastatin or any of the components of the drug;
• liver diseases in the active phase (including a persistent increase in the activity of hepatic transaminases and an increase in the activity of hepatic transaminases in the blood serum by more than 3 times as compared with VGN);
• severe renal impairment (Cl creatinine less than 30 ml / min);
• myopathy;
• simultaneous administration of cyclosporine;
• patients predisposed to the development of myotoxic complications;
• pregnancy, breastfeeding period;
• use in women of childbearing age, not using adequate methods of contraception;
• lactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome;
• age up to 18 years.
• Daily dose of 30 mg or more
• hypersensitivity to rosuvastatin or any of the components of the drug;
• liver diseases in the active phase (including a persistent increase in the activity of hepatic transaminases and an increase in the activity of hepatic transaminases in the blood serum by more than 3 times as compared with VGN);
• moderate to severe renal failure (Cl creatinine less than 60 ml / min);
• myopathy;
• simultaneous use of cyclosporine;
• patients predisposed to the development of myotoxic complications;
• pregnancy, breastfeeding period;
• use in women of childbearing age, not using adequate methods of contraception;
• hypothyroidism;
• diseases of the muscles in history (including in the family);
• myotoxicity with the use of other inhibitors of HMG-CoA reductase or fibrates in history;
• excessive drinking;
• conditions that can lead to increased plasma concentrations of rosuvastatin;
• simultaneous use of fibrates;
• lactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome;
• Mongoloid patients;
• age up to 18 years.
• Carefully
• Daily dose up to 30 mg
• There is a risk of myopathy / rhabdomyolysis - renal failure, hypothyroidism, hereditary muscle diseases in history (including family) and a previous history of muscle toxicity when using other HMG-CoA reductase inhibitors or fibrates; excessive drinking; age over 65; conditions in which there is an increase in the plasma concentration of rosuvastatin; race (Mongoloid race - Japanese and Chinese); simultaneous use with fibrates; history of liver disease; sepsis; hypotension; extensive surgical intervention, trauma, severe metabolic, endocrine or electrolyte disturbances or uncontrolled seizures, simultaneous use with ezetimibe.
• Daily dose of 30 mg or more
• Renal failure mild severity (Cl creatinine more than 60 ml / min); age over 65; history of liver disease; sepsis; hypotension; extensive surgical intervention, trauma, severe metabolic, endocrine or electrolyte disturbances or uncontrolled seizures, simultaneous use with ezetimibe.

Pregnancy and breastfeeding

Roxera is contraindicated in pregnancy and lactation.

Women of reproductive age should use adequate methods of contraception.

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

In the event of pregnancy in the course of therapy, the use of the drug should be immediately discontinued.

There is no data on the release of rosuvastatin with breast milk (it is known that other HMG-CoA reductase inhibitors can be excreted in breast milk), therefore, during the period of breastfeeding, the use of the drug should be stopped.

Dosage and administration

Inside Do not chew a pill or grind it; swallow it whole with water, it can be taken at any time of the day, regardless of the meal.

Before starting therapy with Roxer, the patient should begin to follow the standard cholesterol-lowering diet and continue to follow it during treatment. The dose of the drug should be selected individually, depending on the goals of therapy and the therapeutic response to treatment, taking into account the recommendations on target plasma lipid concentrations.

The recommended initial dose for patients starting to take the drug, or for patients transferred from taking other HMG-CoA reductase inhibitors, should be 5 or 10 mg of Roxer's preparation 1 time per day.

With simultaneous use of the drug with gemfibrozil, fibrates, nicotinic acid in a dose of more than 1 g / day, an initial dose of 5 mg is recommended for patients. When choosing the initial dose, one should be guided by the individual concentration of cholesterol in the blood plasma and take into account the possible risk of developing cardiovascular complications; the potential risk of side effects must also be considered. If necessary, the dose can be increased after 4 weeks.

Due to the possible development of side effects when using a dose of 40 mg / day, compared with lower doses of the drug, increasing the dose to 40 mg / day after an additional dose of the dose above the recommended initial dose during 4 weeks of therapy can be carried out only in patients with severe degree of hypercholesterolemia and a high risk of cardiovascular complications (especially in patients with familial hypercholesterolemia) who have not achieved the desired result of therapy with a dose of 20 mg / day and which will be oditsya under the supervision of a physician. It is recommended especially careful monitoring of patients receiving the drug at a dose of 40 mg / day.

It is not recommended to use a dose of 40 mg / day in patients who have not previously consulted a doctor. After 2–4 weeks of therapy and / or with an increase in the dose of Roxer's drug, monitoring of lipid metabolism indices is necessary (if necessary, dose adjustment is required).

Patients with renal failure.In patients with mild to moderate renal insufficiency, dose adjustment is not required. In patients with severe renal insufficiency (Cl creatinine less than 30 ml / min), the use of Roxer is contraindicated. Use of the drug in a dose of more than 30 mg / day in patients with moderate to severe renal insufficiency (Cl creatinine less than 60 ml / min) is contraindicated. For patients with moderate renal insufficiency, the recommended initial dose of the drug is 5 mg / day.

Patients with liver failure.Roxera is contraindicated in patients with liver disease in the active phase. Experience with the use of the drug in patients with liver failure above 9 points (class C) on the Child-Pugh scale is absent.

Use in elderly patients.Patients over the age of 65 are advised to start using the drug with a dose of 5 mg / day.

Special populations

When studying the pharmacokinetic parameters of rosuvastatin in patients belonging to different ethnic groups, an increase in the systemic concentration of rosuvastatin among Japanese and Chinese was observed. This fact should be taken into account when using Roxer's drug in this group of patients. At doses of 10 and 20 mg / day, the recommended initial dose for patients of the Mongoloid race is 5 mg / day. The use of the drug in a dose of 40 mg is contraindicated for patients of the Mongoloid race.

Patients predisposed to myotoxic complications.The use of the drug at a dose of 40 mg in patients predisposed to the development of myotoxic complications is contraindicated. If necessary, the use of doses of 10 and 20 mg / day, the recommended initial dose for this group of patients is 5 mg. When used with gemfibrozil, the dose of Roxer should not exceed 10 mg / day.

Classification of the incidence of side effects: very often -> 1/10; often -> 1/100, but <1/10; infrequently -> 1/1000, but <1/100; rarely> 1/10000, but <1/1000; very rarely - <1/10000, including individual messages.

The frequency of side effects depends on the dose taken.

On the part of the immune system:rarely, hypersensitivity reactions, including angioedema.

From the side of the central nervous system:often - headache, dizziness; very rarely - polyneuropathy , loss of memory.

From the digestive system: often - constipation, nausea, abdominal pain; rarely - pancreatitis, increased activity of hepatic transaminases; very rarely - jaundice, hepatitis, diarrhea.

From the skin: infrequently - pruritus, rash, urticaria; very rarely - Stevens-Johnson syndrome.

From the musculoskeletal and connective tissue: often myalgia; rarely, myopathy (including myositis) and rhabdomyolysis; very rarely - arthralgia.

A dose-dependent increase in the activity of creatine phosphokinase (CPK) is observed in a small number of patients taking rosuvastatin. In most cases, it is minor, asymptomatic and temporary. In the case of increased activity of CPK more than 5 times higher than VGN, therapy should be suspended.

From the urinary system:often - proteinuria (less than 1% of patients receiving a dose of 10–20 mg / day and about 3% of patients receiving a dose of 40 mg / day). In most cases, proteinuria decreases or disappears during therapy and does not mean the onset of acute or progressive concomitant kidney disease; very rarely - hematuria.

General violations:often - asthenia.

Laboratory values: increased CPK activity, glucose, bilirubin concentration, GGTP, alkaline phosphate activity, change in plasma concentration of thyroid hormones.

Cyclosporine. With the simultaneous use of rosuvastatin and cyclosporine, Rosuvastatin AUC is on average 7 times higher than the value observed in healthy volunteers. The plasma concentration of rosuvastatin is increased 11 times. Simultaneous use with rosuvastatin does not affect the concentration of cyclosporine in the blood plasma.

Indirect anticoagulants. As in the case of other HMG-CoA reductase inhibitors, the initiation of rosuvastatin therapy or an increase in its dose in patients taking both indirect anticoagulants (for example, warfarin) can lead to an increase in MHO. Canceling rosuvastatin or reducing its dose may lead to a decrease in MHO. In such cases, monitoring of the MHO is recommended.

Ezetimibe.The simultaneous use of rosuvastatin and ezetimiba is not accompanied by a change in AUC or C_max both drugs. However, the pharmacodynamic interaction between rosuvastatin and ezetimibe cannot be excluded, which is manifested by an increase in the risk of the development of undesirable muscle reactions.

Gemfibrozil and other lipid-lowering drugs.The simultaneous use of rosuvastatin and gemfibrozil leads to an increase in C_max and Rosuvastatin AUC 2 times. Gemfibrozil, fenofibrate, other fibrates and lipid-lowering doses of nicotinic acid (higher doses or equivalent 1 g / day) increased the risk of myopathy while being used with HMG-CoA reductase inhibitors (possibly due to the fact that they can cause myopathy and monotherapy use). The simultaneous use of fibrates and rosuvastatin in a daily dose of 30 mg is contraindicated. In such patients, therapy should begin with a dose of 5 mg / day.

HIV protease inhibitors.The simultaneous use of HIV protease inhibitors can significantly increase the plasma concentration of rosuvastatin. The simultaneous use of 20 mg of rozuvastatin and a combination of two HIV protease inhibitors (400 mg of lopinavir / 100 mg of ritonavir) is accompanied by an increase in the equilibrium AUC_0–24 and C_max Rosuvastatin 2 and 5 times, respectively.

Antacids.The simultaneous use of rosuvastatin and antacids containing aluminum and Magnesium hydroxide, reduces the plasma concentration of rosuvastatin by about 50%. This effect is less pronounced if antacids are applied 2 hours after taking rosuvastatin.

Erythromycin. The simultaneous use of rosuvastatin and Erythromycin leads to a decrease in AUC_{0 – t} Rosuvastatin by 20% and its C_max by 30%. Such an interaction may occur as a result of increased intestinal motility caused by the use of erythromycin.

Hormonal contraceptives / hormone replacement therapy. The simultaneous use of rosuvastatin and hormonal contraceptives increases the AUC of ethinyl estradiol and norgestrel by 26% and 34%, respectively. Such an increase in plasma concentration should be taken into account when selecting a dose of hormonal contraceptives.

Pharmacokinetic data on the simultaneous use of rozuvastatin and hormone replacement therapy are not available, 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 drugs.No clinically significant interaction of rosuvastatin with Digoxin is expected.

Isoenzymes of cytochrome P450. Rosuvastatin is neither an inhibitor nor an inducer of cytochrome P450. In addition, rosuvastatin is a weak substrate for this system of isoenzymes.

No clinically significant interaction between rosuvastatin and Fluconazole (an inhibitor of isoenzymes CYP2C9 and CYP3A4) and Ketoconazole (an inhibitor of isoenzymes CYP2A6 and CYP3A4) was noted. The simultaneous use of rosuvastatin and itraconazole (inhibitor of CYP3A4 isoenzyme) increases the AUC of rosuvastatin by 28%, which is clinically insignificant. Thus, interactions associated with cytochrome P450 are not expected.

At a temperature not higher than 30 ° C.