Rozukard - instructions for use, reviews, analogs and formulations (tablets 10 mg, 20 mg and 40 mg statin) of the drug for the treatment of hypercholesterolemia and lowering cholesterol levels in adults, children and pregnancy. Composition

In this article, you can read the instructions for using the drug Rosacard. Comments of visitors of the site - consumers of this medication, as well as opinions of doctors specialists on the use of statin Rosukard in their practice are presented. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Rosukard analogues in the presence of existing structural analogues.Use to treat hypercholesterolemia and lower blood cholesterol levels in adults, children, as well as in pregnancy and lactation. Composition of the preparation.

Rosacard - a hypolipidemic drug from the group of statins. A selective competitive inhibitor of HMG-CoA reductase, an enzyme that converts HMG-CoA to mevalonate, a cholesterol precursor (Xc).

Increases the number of LDL receptors on the surface of hepatocytes, which leads to increased capture and catabolism of LDL, inhibition of VLDL synthesis, reducing the total concentration of LDL and VLDL. Reduces the concentration of high-density cholesterol-non-lipoprotein cholesterol (Xc-non-HDL), X-VLDL, total cholesterol, TG, TG-VLDL, apolipoprotein B (ApoB), reduces the ratio of Xc-LDL / Xc-HDL - HDL, Xc-non-HDL / XC-HDL, Apov / apolipoprotein A-1 (ApoA-1), increases the concentrations of Xc-HDL and ApoA-1.

The hypolipidemic effect is directly proportional to the magnitude of the prescribed dose. The therapeutic effect appears within 1 week after the initiation of therapy, after 2 weeks reaches 90% of the maximum, reaches a maximum at 4 weeks, and then remains constant.The drug is effective in adult patients with hypercholesterolemia with or without hypertriglyceridemia (regardless of race, gender or age), incl. in patients with diabetes mellitus and familial hypercholesterolemia. In 80% of patients with hypercholesterolemia 2a and 2b type (Fredrickson classification) with an average initial concentration of LDL-C around 4.8 mmol / l, the concentration of LDL-C is lower than 3 mmol / L when taken at a dose of 10 mg. In patients with homozygous familial hypercholesterolemia who receive the drug at a dose of 20 mg and 40 mg, the average decrease in the concentration of LDL-C is 22%.

The additive effect is noted in combination with fenofibrate (in terms of reducing the concentration of TG and with nicotinic acid in lipid lowering doses (at least 1 g per day) (for reducing the concentration of HDL-C).

Composition

Calcium Rosuvastatin + excipients.

Pharmacokinetics

Absolute bioavailability is approximately 20%. The systemic exposure of rosuvastatin increases in proportion to the dose. Pharmacokinetic parameters do not change with daily intake. Binding to plasma proteins (predominantly with albumin) is approximately 90%.Rosuvastatin is absorbed mainly by the liver, which is the main site for the synthesis of Xc and the metabolism of LDL-C. Penetrates through the placental barrier.

Biotransformed in the liver to a small extent (about 10%), being a non-core substrate for cytochrome P450 isoenzymes. As with other HMG-CoA reductase inhibitors, a specific membrane transporter-a polypeptide transporting an organic anion (AATP) 1B1, which plays an important role in its hepatic elimination-is involved in the hepatic capture process. The main isoenzyme involved in the metabolism of rosuvastatin is the isoenzyme CYP2C9. Isozymes CYP2C19, CYP3A4 and CYP2D6 are less involved in metabolism.

The main metabolites of rosuvastatin are N-dysmethyl and lactone metabolites. N-dimethyl is about 50% less active than rosuvastatin; lactone metabolites are pharmacologically inactive. More than 90% of the pharmacological activity of inhibiting the circulating HMG-CoA reductase is provided by rosuvastatin, the rest - by its metabolites.

About 90% of the dose of rosuvastatin is excreted unchanged through the intestine, the rest - by the kidneys.

Sex and age do not have a clinically significant effect on the pharmacokinetics of rosuvastatin.

Indications

• Primary hypercholesterolemia (type 2a by Fredrickson), including heterozygous hereditary hypercholesterolemia or mixed (combined) hypercholesterolemia (type 2b by Fredrickson), as a supplement to diet and other non-medicamentous measures (physical activity and weight loss) with ineffectiveness of diet and non-drug measures;
• homozygous form of hereditary hypercholesterolemia with insufficient effectiveness of diet therapy and other treatments aimed at lowering lipid levels (eg, LDL apheresis), or if such treatments are not suitable for the patient;
• hypertriglyceridemia (type 4 by Fredrickson) - as a supplement to the diet;
• to slow the progression of atherosclerosis - as a supplement to the diet in patients who are shown therapy to reduce the concentration of total Xc and Xc-LDL;
• prevention of major cardiovascular complications (stroke, heart attack, arterial revascularization) in adult patients without clinical signs of coronary artery disease,but with an increased risk of developing it (age over 50 for men and over 60 for women, increased concentration of C-reactive protein (more than 2 mg / L), with at least one of additional risk factors such as hypertension, low concentration of HDL-C, smoking, family history of early onset of CHD).

Forms of release

Tablets coated with 10 mg, 20 mg and 40 mg.

Instructions for use and dosage

The drug is taken orally. Tablets should be swallowed whole, without chewing and grinding, with water, at any time of the day, regardless of food intake.

Before starting therapy with Rosacard, the patient should begin to follow the standard lipid-lowering diet and continue to observe it during treatment.

The dose of the drug should be selected individually depending on the indications and therapeutic response, taking into account the current generally accepted recommendations for target levels of lipids.

The recommended initial dose of the drug Rosucard for patients starting to take the drug, or for patients transferred from other HMG-CoA reductase inhibitors, is 5 or 10 mg 1 time per day.If you need to take the drug at a dose of 5 mg, you should divide the 10 mg tablet into two parts according to the risk.

When choosing the initial dose should be guided by the content of cholesterol in the patient and take into account the risk of cardiovascular complications, as well as the potential risk of side effects. If necessary, after 4 weeks, the dose of the drug may be increased.

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

In patients with hepatic insufficiency with values ​​below 7 on the Child-Pugh scale, dose adjustment of the Rosicard is not required.

In patients with mild renal insufficiency, correction of the dose of the drug Rosukard is not required; an initial dose of 5 mg per day is recommended.In patients with moderate renal insufficiency (KK 30-60 ml / min), the use of the drug Rosukard at a dose of 40 mg per day is contraindicated. In patients with renal insufficiency (CC less than 30 ml / min), a severe degree of use of the drug Rosukard is contraindicated.

In patients older than 65 years, dose adjustment is not required.

In patients with a predisposition to myopathy, the use of the drug Rosukard in a dose of 40 mg per day is contraindicated. When prescribing the drug at doses of 10 mg and 20 mg per day, the recommended initial dose for this group of patients is 5 mg per day.

When studying the pharmacokinetic parameters of rosuvastatin, there was an increase in the systemic concentration of the drug in representatives of the Mongoloid race. This fact should be taken into account when prescribing the drug Rosukard to patients of the Mongoloid race. When prescribing the drug at doses of 10 mg and 20 mg, the recommended initial dose for this group of patients is 5 mg per day. The use of the drug Rosukard in a dose of 40 mg per day in representatives of the Mongoloid race is contraindicated.

When appointing the drug Rosukard with gemfibrozilom dose should not exceed 10 mg per day.

Side effect

• thrombocytopenia;
• headache;
• dizziness;
• peripheral neuropathy;
• decreased memory;
• sleep disorders, including insomnia and nightmares;
• depression;
• nausea, vomiting;
• constipation, diarrhea;
• abdominal pain;
• pancreatitis;
• hepatitis;
• jaundice;
• cough;
• type 2 diabetes mellitus;
• myalgia;
• myopathy (including myositis);
• rhabdomyolysis (in patients treated at doses greater than 20 mg per day);
• arthralgia;
• tendonitis, possibly with a rupture of tendons;
• immuno-mediated necrotizing myopathy;
• itching;
• hives;
• rash;
• hypersensitivity reactions, including angioedema;
• Stevens-Johnson syndrome;
• proteinuria (with a frequency of more than 3% in patients receiving the drug at a dose of 40 mg), decreasing during therapy and not associated with the onset of kidney disease;
• urinary tract infections;
• hematuria;
• gynecomastia;
• transient increase in AST and ALT activity;
• asthenia;
• peripheral edema;
• increase in glucose concentration, bilirubin.

Contraindications

For tablets 10 and 20 mg

• liver disease in the active phase, or a steady increase in hepatic transaminase activity in the serum (more than 3 times overcompared with UGN) of unknown origin;
• hepatic failure (severity from 7 to 9 on the Child-Pugh scale);
• increase in the concentration of CK in the blood more than 5 times compared with VGN;
• hereditary diseases such as lactose intolerance, lactase deficiency or glucose-galactose malabsorption (due to the presence of lactose in the composition);
• severe renal dysfunction (KK less than 30 ml / min);
• myopathy;
• patients who are predisposed to the development of myotoxic complications;
• simultaneous administration of cyclosporine;
• joint application with HIV protease inhibitors;
• women of reproductive age who do not use adequate methods of contraception;
• pregnancy;
• lactation period (breastfeeding);
• age under 18 years (effectiveness and safety not established);
• hypersensitivity to the components of the drug.

For tablets 40 mg (supplement to contraindications for tablets 10 and 20 mg)

The presence of the following risk factors for the development of myopathy / rhabdomyolysis:

• myotoxicity against the background of the use of other inhibitors of HMG-CoA reductase or fibrates in the anamnesis;
• hypothyroidism;
• renal failure of moderate severity (CK 30-60 ml / min);
• excessive use of alcohol;
• conditions that may lead to an increase in the plasma concentration of rosuvastatin;
• simultaneous reception of fibrates.

Notes on muscle diseases in a family history.

Application in pregnancy and lactation

Rozukard contraindicated in pregnancy and lactation (breastfeeding).

The use of the drug Rosukard in women of reproductive age is possible only if reliable methods of contraception are used and if the patient is informed of the possible risk of treatment for the fetus.

Because cholesterol and substances synthesized from cholesterol are important for fetal development, the potential risk of inhibiting HMG-CoA reductase exceeds the benefit of using the drug during pregnancy. In case of diagnosing pregnancy during the drug treatment, taking Rosukard should be stopped immediately, and the patient should be warned about the potential risk to the fetus.

If it is necessary to use the drug during lactation, taking into account the possibility of undesirable phenomena in infants, it is necessary to solve the problem of stopping breastfeeding.

Use in children

Contraindicated in children and adolescents under the age of 18 years.

special instructions

During treatment, especially during the dose adjustment period of the drug Rosukard, every 2-4 weeks, it is necessary to monitor the lipid profile and, if necessary, change the dose of the drug.

It is recommended to carry out the determination of liver function indices before the start of therapy and 3 months after the start of therapy. Use of the drug Rosukard should stop or reduce the dose, if the level of activity of hepatic transaminases in the serum is 3 times higher than VGN.

When using the drug Rosukard in a dose of 40 mg is recommended to monitor the indicators of kidney function.

In patients with hypercholesterolemia due to hypothyroidism or nephrotic syndrome, treatment of underlying diseases should be performed prior to the initiation of Rosucard treatment.

In patients with existing risk factors for rhabdomyolysis, it is necessary to consider the relationship between expected benefit and potential risk and to conduct clinical follow-up throughout the course of treatment.

The patient should be informed of the need to report immediately to the doctor about cases of unexpected occurrence of muscle pain, muscle weakness or spasms,especially in combination with malaise and fever. In such patients, the activity of CK should be determined. Therapy should be discontinued if the activity of the CK is significantly increased (more than 5 times compared with the VGN) or if the muscle symptoms are pronounced and cause daily discomfort. If symptoms disappear and CPK activity returns to normal, consideration should be given to re-administering Rosacard or other HMG-CoA reductase inhibitors in smaller doses, with careful monitoring of the patient.

Determination of CKK activity should not be performed after intensive physical exertion or in the presence of other possible causes of increased activity of CK, which may lead to incorrect interpretation of the results. If the initial activity of CK is significantly increased, then after 5-7 days a second measurement should be carried out; Do not start therapy if a second test confirms the initial activity of CK (5-fold higher than normal).

Routine monitoring of the activity of CKK in the absence of symptoms is inexpedient.

An increase in the incidence of myositis and myopathy in patients was reported,Taking other inhibitors of HMG-CoA reductase in combination with fibrates (including gemfibrozil), cyclosporine, nicotinic acid, antifungal agents from the azole group, protease inhibitors and antibiotics from the macrolide group. We should carefully weigh the ratio of expected benefits and potential risks with the simultaneous use of the drug Rosukard and fibrates or nicotinic acid (at least 1 g per day); the simultaneous administration of gemfibrozil is not recommended.

In most cases, proteinuria decreases or disappears during therapy and does not imply the emergence of acute or exacerbation of the existing kidney disease. Evaluation of kidney function should be carried out during a routine examination of patients receiving the drug at a dose of 40 mg.

Preparations of the class of statins can cause an increase in the concentration of glucose in the blood. In some patients at high risk of developing diabetes, such changes can lead to its manifestation, which is an indication for the appointment of hypoglycemic therapy. However, reducing the risk of vascular disease with statin use is greater than the risk of developing diabetes, so this factor should not serve as a basis for abolishing statin treatment.For patients at risk (fasting glucose concentration 5.6-6.9 mmol / L, body mass index (BMI) more than 30 kg / m2, hypertriglyceridemia, history of arterial hypertension), medical supervision should be established and biochemical parameters monitored regularly.

It is not recommended simultaneous administration of rosuvastatin and HIV protease inhibitors.

With prolonged use of rosuvastatin, single cases of interstitial lung disease were reported. If suspected of interstitial lung disease, discontinue therapy with Rosukard.

When studying the pharmacokinetic parameters of rosuvastatin, there was an increase in the systemic concentration of the drug in representatives of the Mongoloid race. This fact should be taken into account when prescribing the drug Rosukard to patients of the Mongoloid race.

Impact on the ability to drive vehicles and manage mechanisms

Patients should be careful when driving vehicles and occupations that require increased concentration and speed of psychomotor reactions (dizziness may occur during therapy).

Drug Interactions

With the simultaneous use of rosuvastatin and cyclosporine, the plasma concentration of cyclosporine does not change, but the effect of rosuvastatin increases (its elimination slows down, AUC increases 7-fold, Cmax-11-fold).

Erythromycin increases intestinal motility, which reduces the effect of rosuvastatin (AUC decreases by 20% and Cmax by 30%).

Patients receiving vitamin K antagonists (eg, warfarin) are advised to monitor MHO, because initiating Rosacard therapy or increasing the dose of the drug may lead to an increase in MHO, and cancellation or reduction of rosuvastatin may lead to a decrease.

The simultaneous use of rosuvastatin and antacids containing aluminum and magnesium hydroxide leads to a decrease in the plasma concentration of rosuvastatin by approximately 50%. This effect is less pronounced if antacids are administered 2 hours after rosuvastatin administration.

The simultaneous use of rosuvastatin and oral contraceptives increases the AUC of ethinylestradiol and AUC of norgestrel by 26% and 34%, respectively, which should be taken into account when selecting a dose of oral contraceptives. Pharmacokinetic data on the simultaneous use of rosuvastatin andhormone replacement therapy are absent, therefore, it is impossible to exclude a similar effect when using this combination.

The results of the studies showed that Rosacard is neither an inhibitor nor an inducer of the action of cytochrome P450 isoenzymes. Rosuvastatin is a non-core substrate for these isoenzymes. There was no clinically significant interaction with such drugs as fluconazole, Ketoconazole and itraconazole, which are metabolized with the participation of cytochrome P450 isoenzymes.

There was no clinically significant interaction between rosuvastatin and digoxin.

There was no clinically significant interaction between rosuvastatin and fenofibrate. Gemfibrozil enhances the effect of rosuvastatin (increases Cmax and AUC by 2 times). Gemfibrozil, other fibrates and nicotinic acid in lipid-lowering doses (at least 1 g per day) increased the risk of myopathy with simultaneous use with other HMG-CoA reductase inhibitors. Perhaps this is due to the fact that they are able to cause myopathy and when used as monotherapy.

The combined use of rosuvastatin and ezetimibe did not result in changes in the AUC or Cmax of both drugs.

The use of HIV protease inhibitors with rosuvastatin can lead to a significant increase in the effect of rosuvastatin. A pharmacokinetic study showed that, when administered jointly in healthy volunteers, rosuvastatin at a dose of 20 mg and a combination of two HIV protease inhibitors (lopinavir 400 mg / ritonavir 100 mg) resulted in approximately a 2- and 5-fold increase in AUC0-24 and Cmax, respectively. Thus, in patients infected with HIV, co-administration of rosuvastatin with HIV protease inhibitors is not recommended.

Analogues of the drug Rosukard

Structural analogs for the active substance:

• Akorta;
• The Cross;
• Mertenil;
• Rosart;
• Rosystark;
• Rosuvastatin;
• Calcium rosuvastatin;
• Rosulip;
• Roxer;
• Tevastor.

Analogues for the pharmacological group (statins):

• Akorta;
• Aktalipid;
• Anistat;
• Atherostat;
• Ator;
• Atorvastatin;
• Atoris;
• Vazilip;
• Zocor;
• The Cross;
• Leskol;
• Lipostat;
• Liprimar;
• Lovacor;
• Lovastatin;
• Mertenil;
• Novostat;
• Pravastatin;
• Rovacor;
• Rosuvastatin;
• Simvard;
• Simvastatin;
• Simlo;
• Tevastor;
• Torvazine;
• Torvacard;
• Tulip;
• Holvasim;
• Holletar.

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