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Roxer - instructions for use, reviews, analogs and formulations (tablets 5 mg, 10 mg, 15 mg, 20 mg, 30 mg and 40 mg) of statin drug for lowering cholesterol and preventing infarction in adults, children and pregnancy

Roxer - instructions for use, reviews, analogs and formulations (tablets 5 mg, 10 mg, 15 mg, 20 mg, 30 mg and 40 mg) of statin drug for lowering cholesterol and preventing infarction in adults, children and pregnancy

In this article, you can read the instructions for using the drug Roxer. Presented are reviews of visitors to the site - consumers of this medication, as well as opinions of doctors specialists on the use of statin Roxer in their practice. 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. Analogues of the Rockers in the presence of existing structural analogs. Use to reduce cholesterol and prevent heart attack and stroke in adults, children, as well as during pregnancy and lactation.

 

Roxer - a hypolipidemic drug. The active substance of the drug, rosuvastatin, is a selective, competitive inhibitor of HMG-CoA reductase, an enzyme that converts 3-hydroxy-3-methylglutarylcoenzyme A into mevalonic acid, the precursor of cholesterol. The main target of the action of Rosuvastatin is the liver, where there is a synthesis of cholesterol (Xs) and catabolism of low density lipoproteins (LDL). Increases the number of hepatic receptors for LDL on the surface of cells, increasing the uptake and catabolism of LDL, which in turn leads to inhibition of the synthesis of very low density lipoproteins (VLDL), thereby reducing the total number of LDL and VLDL.

 

Rosuvastatin reduces elevated plasma concentrations of LDL cholesterol (Xc-LDL), total cholesterol, triglycerides (TG), increases the concentration of high-density lipoprotein cholesterol (HDL-C). It also reduces the concentration of apolipoprotein B (ApoB), Xc-non-HDL, Xc-VLDL, TG-VLDL and increases the concentration of apolipoprotein A-1 in blood plasma. Rosuvastatin reduces the ratio of Xc-LDL / Xc-HDL, total Xc / Xc-HDL and Xc-non-HDL / Xc-HDL and the ApoB / ApoA-1 ratio.

 

The therapeutic effect develops within one week after the initiation of therapy, after 2 weeks of treatment it reaches 90% of the maximum possible effect. The maximum therapeutic effect is usually achieved by week 4 of therapy and is maintained with further regular administration of the drug.

 

Clinical efficacy

 

Rosuvastatin is effective in adult patients with hypercholesterolemia with or without accompanying hypertriglyceridemia, regardless of race, gender or age, incl. in patients with diabetes mellitus or familial hypercholesterolemia.

 

In 80% of patients with Fredrickson-type 2a and 2b hypercholesterolemia (mean baseline LDL-C concentration of approximately 4.8 mmol / L), with rosuvastatin 10 mg, the concentration of LDL-C is lower than 3 mmol / L.

 

In patients with homozygous familial hypercholesterolemia, rosuvastatin was used in doses of 20 to 40 mg, with an average decrease of 22%.

 

The additive effect is noted in combination with fenofibrate for TG and nicotinic acid in lipid-lowering doses for the concentration of HDL-C.

 

Composition

 

Calcium rosuvastatin + excipients.

 

Pharmacokinetics

 

Absolute bioavailability is approximately 20%. It is metabolized primarily by the liver, which is the main organ that synthesizes cholesterol and metabolizes LDL-C. Approximately 90% of rosuvastatin binds to blood plasma proteins, mainly albumin. Pharmacokinetic parameters do not change with daily intake. About 90% of the dose of rosuvastatin is excreted unchanged through the intestine (including absorbed and unabsorbed rosuvastatin). The rest is excreted 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) or mixed dyslipidemia (type 2b by Fredrickson) as an adjunct to the diet with ineffectiveness of diet and other non-drug therapies (eg physical exertion, weight loss);
  • family homozygous hypercholesterolemia as an adjunct to diet and other lipid-lowering therapy (eg, LDL-apheresis) or if such therapy is not effective;
  • 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 plasma concentrations of Xc and Xc-LDL;
  • Primary prevention of major cardiovascular complications (stroke, myocardial infarction, arterial revascularization) in adult patients without clinical signs of IHD, but with an increased risk of its development (age over 50 for men and over 60 for women, increased plasma concentration of C-reactive protein (more than 2 g / L) with at least one of additional risk factors, such as hypertension, low plasma concentration of HDL-C, smoking, early onset of CHD in family history).

 

Forms of release

 

Tablets coated with 5 mg, 10 mg, 15 mg, 20 mg, 30 mg and 40 mg.

 

Instructions for use and dosing regimen

 

The drug is taken orally. The tablet can not be chewed or chopped, swallowed whole, washed down with water, it is possible to take it at any time of the day, regardless of food intake.

 

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

 

The recommended initial dose for patients starting to take the drug, or for patients transferred from other HMG-CoA reductase inhibitors, should be 5 or 10 mg once daily.

 

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

 

In connection with the possible development of side effects when applying a dose of 40 mg per day, compared with lower doses of the drug, increasing the dose to 40 mg per day after an additional dose above the recommended initial dose for 4 weeks of therapy,can only be performed in patients with severe hypercholesterolemia and a high risk of developing cardiovascular complications (especially in patients with familial hypercholesterolemia) who did not achieve the desired result of therapy with a dose of 20 mg per day and which will be monitored by a physician . It is recommended especially careful monitoring of patients receiving the drug at a dose of 40 mg per day.

 

Do not use a dose of 40 mg per 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 the drug Roxer, control of the lipid metabolism parameters is necessary (if necessary, dose correction is required).

 

In patients with mild or moderate renal insufficiency, dose adjustment is not required. In patients with severe renal failure (CC less than 30 ml / min), the use of the drug Roxer is contraindicated. The use of the drug at a dose of more than 30 mg per day for patients with moderate and severe renal insufficiency (QC less than 60 ml / min) is contraindicated. Patients with moderate renal insufficiency of the recommended initial dose of the drug is 5 mg per day.

 

The drug of Roxer is contraindicated in patients with liver diseases in the active phase.The experience of using the drug in patients with hepatic insufficiency above 9 points (class C) on the Child-Pugh scale is not available.

 

Patients over the age of 65 years are advised to start using the drug with a dose of 5 mg per day.

 

Side effect

  • hypersensitivity reactions, including angioedema;
  • headache;
  • dizziness;
  • polyneuropathy;
  • memory loss;
  • constipation, diarrhea;
  • nausea;
  • abdominal pain;
  • jaundice;
  • hepatitis;
  • itching;
  • rash;
  • hives;
  • Stevens-Johnson syndrome;
  • myalgia;
  • Myopathy (including myositis) and rhabdomyolysis;
  • arthralgia;
  • proteinuria;
  • hematuria;
  • asthenia;
  • change in plasma concentration of thyroid hormones.

 

Contraindications

 

At a daily dose of up to 30 mg

  • liver diseases in the active phase (including a persistent increase in hepatic transaminase activity and an increase in the activity of hepatic transaminases in the blood serum more than 3-fold compared to IGN);
  • severe renal failure (CC less than 30 ml / min);
  • myopathy;
  • simultaneous administration of cyclosporine;
  • patients who are predisposed to the development of myotoxic complications;
  • pregnancy;
  • the period of breastfeeding;
  • use in women of childbearing age who do not use adequate methods of contraception;
  • lactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome;
  • age to 18 years;
  • increased sensitivity to rosuvastatin or any of the components of the drug.

 

At a daily dose of 30 mg and more

  • liver diseases in the active phase (including a persistent increase in hepatic transaminase activity and an increase in the activity of hepatic transaminases in the blood serum more than 3-fold compared to IGN);
  • renal insufficiency of moderate and severe degree (CC less than 60 ml / min);
  • myopathy;
  • simultaneous application of cyclosporine;
  • patients who are predisposed to the development of myotoxic complications;
  • pregnancy;
  • the period of breastfeeding;
  • use in women of childbearing age not using adequate methods of contraception;
  • hypothyroidism;
  • muscle diseases in the anamnesis (including in the family);
  • myotoxicity with other inhibitors of HMG-CoA reductase or fibrates in history;
  • excessive use of alcohol;
  • conditions that may lead to an increase in the concentration of rosuvastatin in the blood plasma;
  • simultaneous application of fibrates;
  • lactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome;
  • patients of the Mongoloid race;
  • age to 18 years;
  • increased sensitivity to rosuvastatin or any of the components of the drug.

 

Application in pregnancy and lactation

 

The drug of Roxer is contraindicated in pregnancy and lactation.

 

Women of reproductive age should apply 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 inhibitors for the fetus outweigh the benefits of the use of the drug during pregnancy.

 

In the case of pregnancy in the process of therapy, the drug should be discontinued immediately.

 

The data on the allocation of rosuvastatin with breast milk are absent (it is known that other inhibitors of HMG-CoA reductase can be allocated to breast milk), so the period of use of the drug breast feeding must be stopped.

 

Use in children

 

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

 

Application in elderly patients

 

Patients over the age of 65 years are advised to start using the drug with a dose of 5 mg per day.

 

special instructions

 

Impaired renal function

 

In patients receiving high doses of rosuvastatin (in particular, 40 mg per day) tubular proteinuria was observed, which was detected with the help of test strips and in most cases was periodic or short-term. Such proteinuria does not indicate an acute or progressive comorbid kidney disease. The frequency of serious renal dysfunction, noted in the post-marketing study of rosuvastatin, is higher with a dose of 40 mg per day. In patients taking the drug Roxer in a dose of 30 or 40 mg per day, it is recommended to monitor the indicators of kidney function during treatment (at least every 3 months).

 

Influence on the musculoskeletal system

 

When rosuvastatin was used in all doses, but in particular at doses exceeding 20 mg per day, the following effects on the musculoskeletal system were reported: myalgia, myopathy, in rare cases rhabdomyolysis. Very rare cases of rhabdomyolysis with simultaneous application of HMG-CoA reductase inhibitors and ezetimibe have been noted.This combination should be used with caution, because it is impossible to exclude pharmacodynamic interaction.

 

As with the use of other inhibitors of HMG-CoA reductase, the frequency of rhabdomyolysis in the post-marketing application of the drug Roxer is higher with a dose of 40 mg per day.

 

Determination of CKK activity

 

The activity of CK can not be determined after intensive physical exertion and in the presence of other possible causes of an increase in its activity; this can lead to incorrect interpretation of the results. In case the initial activity of CK is significantly exceeded (5 times higher than ULN), after 5-7 days, a second analysis should be carried out. You can not start therapy if the results of the repeated analysis confirm the initial high activity of CK (more than 5-fold excess of UGN).

 

Before starting therapy

 

Depending on the daily dose, the Roxer preparation should be administered with caution to patients with existing risk factors for myopathy / rhabdomyolysis or the use of the drug is contraindicated. Such factors include:

  • impaired renal function;
  • hypothyroidism;
  • muscle diseases in the anamnesis (including in the family);
  • myotoxic effects when taking other inhibitors of HMG-CoA reductase or fibrates in anamnesis;
  • excessive use of alcohol;
  • age over 65;
  • conditions in which the concentration of rosuvastatin in the blood plasma may increase;
  • simultaneous application of fibrates.

 

These patients need to assess the risk and possible benefits of therapy. Clinical monitoring is also recommended. If the initial activity of CK is more than 5 times higher than that of VGN, therapy with Roxer can not be started.

 

During the period of drug therapy

 

The patient should be informed of the need to report immediately to the doctor in the event of an 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 CKK is significantly increased (more than 5 times compared with IGN) or if the symptoms from the muscles are pronounced and cause daily discomfort (even if the CKK activity is not more than 5 times higher than the IGN). If the symptoms disappear and CPK activity returns to normal,should consider resuming the use of the drug Roxer or other inhibitors of HMG-CoA reductase in smaller doses with careful medical supervision. Control of the activity of CKK in the absence of symptoms is inexpedient.

 

Signs of increased effects on skeletal muscle with rosuvastatin and concomitant therapy were not noted. However, an increase in the number of cases of myositis and myopathy in patients taking other HMG-CoA reductase inhibitors in combination with fibrolic acid derivatives (for example, gemfibrozil), cyclosporine, nicotinic acid in lipid lowering doses (more than 1 g per day), antifungal agents - derivatives of azole, HIV protease inhibitors and macrolide antibiotics.

 

When used simultaneously with certain HMG-CoA reductase inhibitors, gemfibrozil increases the risk of myopathy. Thus, the simultaneous use of the drug Roxer and gemfibrozil is not recommended (in doses less than 30 mg per day). The benefits of further changes in plasma lipid concentration when combined with the use of the Roxer preparation with fibrates or nicotinic acid in lipid lowering doses should be carefully weighed taking into account the possible risk.Rosuvastatin in a dose of 30 mg per day or more is contraindicated for combination therapy with fibrates.

 

Due to the increased risk of rhabdomyolysis, Roxer 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 surgical interventions, trauma, severe metabolic, endocrine and electrolyte disorders or uncontrolled convulsions).

 

Liver

 

Depending on the daily dose, the Roxer preparation should be used with caution in patients with excessive alcohol use and / or having a history of liver disease or its use is contraindicated.

 

It is recommended to carry out the determination of functional liver samples before the start of therapy and 3 months after the beginning of therapy. The use of the drug Roxer should stop or reduce the dose of the drug if the activity of hepatic transaminases in the serum is 3 times higher than VGN.

 

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

 

Ethnic Features

 

In the course of pharmacokinetic studies, an increase in the plasma concentration of rosuvastatin was observed in Mongoloids compared with Caucasians.

 

The preparation of Roxer contains lactose, and therefore it should not be used for patients with lactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome.

 

Impact on the ability to drive vehicles and manage mechanisms

 

Studies to study the effect of the drug Roxer on the ability to drive vehicles and work with mechanisms were not conducted. Nevertheless, considering the possibility of developing dizziness and other side effects, care must be taken when driving vehicles and other mechanisms that require a high concentration of attention and speed of psychomotor reactions.

 

Drug Interactions

 

Cyclosporin

 

With simultaneous application of rosuvastatin and cyclosporine, rosuvastatin AUC is on average 7 times higher than that seen in healthy volunteers. The plasma concentration of rosuvastatin rises 11 times.

 

Simultaneous use with rosuvastatin does not affect the concentration of cyclosporine in the blood plasma.

 

Indirect anticoagulants

 

As with other HMG-CoA reductase inhibitors, initiating therapy with Roxer or increasing its dose in patients taking concomitantly indirect anticoagulants (eg, warfarin) may result in an increase in MHO. Removing rosuvastatin or reducing its dose may result in a decrease in MHO. In such cases, MHO monitoring is recommended.

 

Ezetimibe

 

The simultaneous use of rosuvastatin and ezetimibe is not accompanied by a change in the AUC or C max of both drugs. However, it is impossible to exclude the pharmacodynamic interaction between rosuvastatin and ezetimibe, which is manifested by an increased risk of developing unwanted reactions from the muscles.

 

Gemfibrozil and other lipid-lowering agents

 

The simultaneous use of rosuvastatin and gemfibrozil leads to an increase in Cmax and AUC of rosuvastatin by a factor of 2. Gemfibrozil, fenofibrate, other fibrates and lipid-lowering doses of nicotinic acid (doses greater than or equivalent to 1 g per day) increased the risk of myopathy with concomitant use with HMG-CoA reductase inhibitors (possibly due to the fact that they can cause myopathy and when applied in monotherapy).

 

Simultaneous application of fibrates and Roxers in a daily dose of 30 mg is contraindicated. In such patients, therapy should begin with a dose of 5 mg per day.

 

HIV protease inhibitors

 

Simultaneous use of HIV protease inhibitors can significantly increase the plasma concentration of rosuvastatin. Simultaneous use of 20 mg of rosuvastatin 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 hours) and Cmax of rosuvastatin by 2 and 5 times, respectively.

 

Antacids

 

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.

 

Erythromycin

 

Simultaneous application of rosuvastatin and Erythromycin leads to a decrease in AUC (0-t) rosuvastatin by 20% and its Cmax by 30%. Such interaction can arise as a result of increased intestinal motility caused by the use of erythromycin.

 

Hormonal contraceptives - hormone replacement therapy (HRT)

 

The simultaneous use of rosuvastatin and hormonal contraceptives increases the AUC of ethinylestradiol 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 rosuvastatin and hormone replacement therapy are not available, therefore, it is impossible to exclude a similar effect when using this combination. However, this combination was widely used during clinical trials and was well tolerated by patients.

 

Digoxin

 

Clinically significant interaction of Roxera with Digoxin is not expected.

 

Isozymes of cytochrome P450

 

Rosuvastatin is neither an inhibitor nor an inducer of cytochrome P450. In addition, rosuvastatin is a weak substrate for this isoenzyme system. Clinically significant interactions between rosuvastatin and Fluconazole (inhibitor of isoenzymes CYP2C9 and CYP3A4) and Ketoconazole (inhibitor of isoenzymes CYP2A6 and CYP3A4) were not observed. The simultaneous use of rosuvastatin and Itraconazole (an inhibitor of the isoenzyme CYP3A4) increases the aUC of rosuvastatin by 28%which is clinically insignificant. Thus, no interaction is expected with cytochrome P450.

 

Analogues of the drug Roxer

 

Structural analogs for the active substance:

  • Akorta;
  • The Cross;
  • Mertenil;
  • Rosart;
  • Rosystark;
  • Rosuvastatin;
  • Rosewood;
  • Rosulip;
  • Rustor;
  • Tevastor.

 

Analogues for the pharmacological group (statins):

  • Aktalipid;
  • Anistat;
  • Apexstatin;
  • Atherostat;
  • Atokord;
  • Atomax;
  • Ator;
  • Atorvastatin;
  • Atorvox;
  • Atoris;
  • The Vasator;
  • Vazilip;
  • Zocor;
  • Zokor forte;
  • Zorstat;
  • Cardiostatin;
  • The Cross;
  • Leskol;
  • Lipobay;
  • Lipon;
  • Lipostat;
  • Lipofford;
  • Liprimar;
  • Liptonorm;
  • Lovacor;
  • Lovastatin;
  • Lovasterol;
  • Mertenil;
  • Novostat;
  • Pravastatin;
  • Rovacor;
  • Rosart;
  • Rosuvastatin;
  • Rosewood;
  • Rosulip;
  • Rustor;
  • Simvard;
  • Simvakol;
  • Simvastatin;
  • Simvastol;
  • Simgal;
  • Simlo;
  • Sinquard;
  • Tevastor;
  • Torvazine;
  • Torvacard;
  • Torvalip;
  • Torvas;
  • Tulip;
  • Holvasim;
  • Holletar.

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