Roxera, 30 pcs., 20 mg, film-coated tablets

Nosological classification (ICD-10)

• E78.0 Pure hypercholesterolemia
• E78.1 Pure hyperglyceridemia
• E78.2 Mixed hyperlipidemia
• E78.5 Hyperlipidemia, unspecified
• I10 Essential (primary) hypertension
• I15 Secondary hypertension
• I21 Acute myocardial infarction
• I25.9 Chronic ischemic heart disease, unspecified
• I64 Stroke not specified as hemorrhage or infarction
• I70 Atherosclerosis
• Z72.0 Tobacco use
• Z82.4 Family history of coronary heart disease and other diseases of the cardiovascular system

Compound

Description of the dosage form

Tablets, 5 mg: round, biconvex, white film-coated, beveled, stamped “5” on one side*.

Tablets, 10 mg: round, biconvex, white film-coated, chamfered, stamped “10” on one side*.

Tablets 15 mg: round, biconvex, white film-coated, bevelled, stamped “15” on one side*.

Tablets, 20 mg: round, biconvex, white film-coated, beveled*.

Tablets, 30 mg: capsule-shaped, biconvex, white film-coated, scored on both sides*.

Tablets, 40 mg: capsule-shaped, biconvex, white film-coated*.

* On a cross section, two layers are visible, the core is white.

Rocker price

The price of Roxera depends on the dose of the active substance contained in it and the number of tablets in the package.

So, for example, tablets containing rosuvastatin 5 mg can be purchased on average for 295-450 Russian rubles per pack of 30 pieces. A package containing 90 Roxer 5 mg tablets will cost an average of 850-1100 Russian rubles.

The price of Roxera 10 mg is:

• 395-590 Russian rubles for a pack of 30 pieces;
• 1026-1500 Russian rubles per pack of 90 pieces.

The price of Roxera 20 mg is:

• 585-980 Russian rubles for a pack of 30 pieces;
• 1500-2175 Russian rubles per pack of 90 pieces.

• Online pharmacies in RussiaRussia
• Online pharmacies in UkraineUkraine
• Online pharmacies in KazakhstanKazakhstan

ZdravCity

• Roxera tab.
  p/o captivity. 5 mg No. 30 Krka-Rus LLC 417 rub. order
• Roxera tab. p/o captivity. 10mg No. 30Krka-Rus LLC

  RUR 519 order

• Roxera tab. p/o captivity. 5mg No. 90 Krka-Rus LLC

  RUR 923 order

• Roxera tab. p/o captivity. 10 mg No. 90 Krka-Rus LLC

  RUB 1,166 order

• Roxera tablets p.p.o 15 mg 90 pcs. Krka-Rus LLC

  RUB 1,364 order

Pharmacy Dialogue

• Roxera (tablet p/o 15 mg No. 30)KPKA

  680 rub. order

• Roxera (tablet p/o film. 15 mg No. 90)KPKA

  RUB 1,431 order

• Roxera (tablet p/o 10 mg No. 90)KPKA

  RUB 1,216 order

• Roxera (tablet p/o 20 mg No. 90)KPKA

  RUB 1,859 order

• Roxera (tablet p/o 5 mg No. 30)KPKA

  RUR 439 order

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Pharmacy24

• Roxera 40 mg No. 30 tablets KPKA, d.d., Novo mesto, Slovenia
  250 UAH. order
• Roxera 30 mg No. 90 tablets KPKA, d.d., Novo Mesto, Slovenia

  370 UAH. order

• Roxera 10 mg N90 tablets KPKA, d.d., Novo Mesto, Slovenia

  298 UAH order

• Roxera 20 mg No. 30 tablets KPKA, d.d., Novo Mesto, Slovenia

  166 UAH order

• Roxera 15 mg N30 tablets KRKA, Slovenia

  98 UAH order

PaniPharmacy

• Roxera tablets Roxera tablets 10 mg No. 30 Slovenia, KRKA dd Novo Mesto

  134 UAH order

• Roxer table 5mg No.90

  219 UAH. order

• Roxera tablets Roxera tablets. 30 mg No. 90 Slovenia, KRKA dd Novo Mesto

  396 UAH. order

• Roxera tablets Roxera tablets 15 mg No. 30 Slovenia, KRKA dd Novo Mesto

  112 UAH order

• Roxera tablets Roxera tablets 20 mg No. 30 Slovenia, KRKA dd Novo Mesto

  194 UAH order

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Pharmacodynamics

The drug Roxera® is a hypolipidemic agent. The active ingredient of the drug, rosuvastatin, is a selective, competitive inhibitor of HMG-CoA reductase, an enzyme that converts 3-hydroxy-3-methylglutaryl coenzyme A into mevalonic acid, a cholesterol precursor. The main target of rosuvastatin is the liver, where cholesterol (C) synthesis and LDL catabolism occur. Increases the number of hepatic LDL receptors on the cell surface, increasing the uptake and catabolism of LDL, which in turn leads to inhibition of VLDL synthesis, thereby reducing the total amount of LDL and VLDL. Rosuvastatin reduces elevated plasma concentrations of LDL cholesterol (LDL-C), total cholesterol, triglycerides (TG), and increases the concentration of high-density lipoprotein cholesterol (HDL-C). It also reduces the concentration of apolipoprotein B (ApoB), non-HDL-C, VLDL-C, VLDL-TG and increases the concentration of apolipoprotein AI (ApoA-1) in the blood plasma.

Rosuvastatin reduces the ratio of LDL-C/HDL-C, total cholesterol/HDL-C and non-HDL-C/HDL-C and the ApoB/ApoA-1 ratio. The therapeutic effect develops within one week after the start of therapy, after 2 weeks of treatment it reaches 90% of the maximum possible effect. The maximum therapeutic effect is usually achieved by the 4th week of therapy and is maintained with further regular use of the drug.

Clinical effectiveness

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

In 80% of patients with Fredrickson type IIa and IIb hypercholesterolemia (average initial LDL-C concentration of approximately 4.8 mmol/l), while taking rosuvastatin at a dose of 10 mg, the LDL-C concentration reaches values ​​of less than 3 mmol/l. In patients with homozygous familial hypercholesterolemia, rosuvastatin was used in doses of 20–40 mg, with an average reduction of 22%. An additive effect is observed in combination with fenofibrate in relation to TG content and with nicotinic acid in lipid-lowering doses in relation to HDL-C concentration.

pharmachologic effect

The pharmacological action of the drug Roxera is aimed at:

• Suppression of the activity of the microsomal enzyme hydroxymethylglutaryl-CoA reductase , which acts as a catalyst for the rate-limiting early stage of cholesterol .
• Normalization of lipid profile indicators ( hypolipidemic effect ) by reducing the concentration of total cholesterol , triglycerides , lipoproteins the blood , as well as increasing the concentration of lipoproteins .

The medicine belongs to the pharmacological group “ Statins ”.

Pharmacokinetics

Absorption and distribution

Cmax of rosuvastatin in blood plasma is achieved approximately 5 hours after oral administration. Absolute bioavailability is approximately 20%. Metabolized primarily by the liver, which is the main organ that synthesizes cholesterol and metabolizes LDL-C. Vd of rosuvastatin is approximately 134 l. Approximately 90% of rosuvastatin is bound to plasma proteins, mainly albumin.

Metabolism

Subject to limited metabolism (about 10%). Rosuvastatin is a nonspecific substrate of cytochrome P450. The main isoenzyme involved in the metabolism of rosuvastatin is the CYP2C9 isoenzyme. Isoenzymes CYP2C19, CYP3A4, CYP2D6 are involved in metabolism to a lesser extent. The main metabolites identified are N-desmethylrosuvastatin and lactone metabolites. N-desmethyl rosuvastatin is approximately 50% less active than rosuvastatin; the lactone metabolites are pharmacologically inactive. More than 90% of the pharmacological activity of inhibiting plasma HMG-CoA reductase is provided by rosuvastatin, the rest is provided by its metabolites.

Removal

About 90% of the dose of rosuvastatin is excreted unchanged through the intestine (including absorbed and unabsorbed rosuvastatin). The remaining part is excreted by the kidneys. T1/2 from blood plasma is approximately 19 hours (does not change with increasing dose of the drug). The geometric average plasma clearance is 50 l/h (coefficient of variation - 21.7%). As with other HMG-CoA reductase inhibitors, the process of hepatic uptake of rosuvastatin involves a membrane cholesterol transporter, which plays an important role in the hepatic elimination of rosuvastatin.

Linearity

Systemic exposure of rosuvastatin increases in proportion to the dose. Pharmacokinetic parameters do not change with daily use.

Special patient groups

Age and gender. Gender and age do not have a clinically significant effect on the pharmacokinetics of rosuvastatin.

Ethnic groups. Pharmacokinetic studies have shown an approximately twofold increase in the median AUC and Cmax of rosuvastatin in patients of the Mongoloid race (Japanese, Chinese, Filipinos, Vietnamese and Koreans) compared to Caucasians; Indians showed a 1.3-fold increase in median AUC and Cmax. Pharmacokinetic analysis did not reveal clinically significant differences in pharmacokinetics between Caucasian and Negroid races.

Kidney failure. In patients with mild to moderate renal failure, the plasma concentration of rosuvastatin or N-desmethylrosuvastatin does not change significantly. In patients with severe renal failure (Cl creatinine less than 30 ml/min), the concentration of rosuvastatin in the blood plasma is 3 times higher, and the concentration of N-desmethyl rosuvastatin is 9 times higher than in healthy volunteers. The plasma concentration of rosuvastatin in patients on hemodialysis is approximately 50% higher than in healthy volunteers.

Liver failure. In patients with chronic alcoholic liver disease, plasma concentrations of rosuvastatin are moderately increased. Compared with patients with normal liver function, in patients with liver failure (Child-Pugh score 7 or lower), the Cmax and AUC of rosuvastatin are increased by 60 and 5%, respectively; in patients with liver failure (8–9 points on the Child-Pugh scale), these indicators increase by 100 and 21%, respectively. There is no experience with the use of rosuvastatin in patients with liver failure (class C on the Child-Pugh scale - above 9 points).

Genetic polymorphism. HMG-CoA reductase inhibitors, incl. rosuvastatin bind to the transport proteins OATP1B1 (organic anion transport polypeptide involved in the uptake of statins by hepatocytes) and BCRP (efflux transporter). Carriers of the SLCO1B1 (OATP1B1) c.521CC and ABCG2 (BCRP) c.421AA genotypes showed an increase in rosuvastatin exposure (AUC) by 1.6 and 2.4 times, respectively, compared to carriers of the SLCO1B1 c.521TT and ABCG2 c.421CC genotypes.

Indications for Roxera®

primary hypercholesterolemia according to Fredrickson (type IIa) or mixed dyslipidemia (type IIb) as an addition to diet when diet and other non-drug treatment methods are ineffective (for example, exercise, weight loss);

familial homozygous hypercholesterolemia as an addition to diet and other lipid-lowering therapy (eg LDL apheresis) or if such therapy is ineffective;

hypertriglyceridemia (Fredrickson type IV) as an addition to the diet;

to slow the progression of atherosclerosis as an addition to diet in patients who are indicated for therapy to reduce plasma concentrations 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 (age over 50 years for men and over 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: arterial hypertension, low plasma concentration of HDL-C, smoking, early onset of coronary artery disease in the family history).

Indications for use

Rocker shown:

• For the treatment of patients suffering from primary type hypercholesterolemia (including familial hypercholesterolemia type II-A Fredrickson ) or dyslipidemia (type II-b). It is advisable to prescribe the drug when the expected therapeutic effect cannot be achieved by prescribing non-drug treatment methods: diet, correction of the patient’s weight, physical exercise, etc.
• For the treatment of patients diagnosed with familial homozygous hypercholesterolemia . Roxera is prescribed as an addition to therapy, the purpose of which is to lower lipid , as an addition to the diet, and also in cases where previously prescribed treatment does not produce positive results.
• For the treatment of patients diagnosed with atherosclerosis . The drug is used as a supplement to the prescribed diet to slow the progression of the disease, as well as to reduce total cholesterol and low-density lipoprotein cholesterol to the required level.
• As a prophylactic agent to prevent the development of complications of heart and vascular in patients with a predisposition to the development of atherosclerotic vascular lesions .

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 liver transaminases and an increase in the activity of liver transaminases in the blood serum by more than 3 times compared to ULN);

severe renal failure (creatinine Cl less than 30 ml/min);

myopathy;

simultaneous use of cyclosporine;

patients predisposed to the development of myotoxic complications;

pregnancy, breastfeeding period;

use in women of childbearing age who do not use adequate methods of contraception;

lactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome;

age up to 18 years.

Daily dose 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 liver transaminases and an increase in the activity of liver transaminases in the blood serum by more than 3 times compared to ULN);

moderate to severe renal failure (creatinine Cl 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 who do not use adequate methods of contraception;

hypothyroidism;

history of muscle diseases (including family);

history of myotoxicity with the use of other HMG-CoA reductase inhibitors or fibrates;

excessive alcohol consumption;

conditions that can lead to increased concentrations of rosuvastatin in blood plasma;

simultaneous use of fibrates;

lactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome;

patients of the Mongoloid race;

age up to 18 years.

Carefully

Daily dose up to 30 mg. There is a risk of developing myopathy/rhabdomyolysis - renal failure, hypothyroidism, a history of hereditary muscle diseases (including family history) and a previous history of muscle toxicity when using other HMG-CoA reductase inhibitors or fibrates; excessive alcohol consumption; age over 65 years; conditions in which an increase in plasma concentration of rosuvastatin is noted; race (Mongoloid race - Japanese and Chinese); simultaneous use with fibrates; history of liver disease; sepsis; arterial hypotension; major surgery, trauma, severe metabolic, endocrine or electrolyte disturbances or uncontrolled seizures, concomitant use with ezetimibe.

Daily dose is 30 mg or more. Mild renal failure (creatinine Cl more than 60 ml/min); age over 65 years; history of liver disease; sepsis; arterial hypotension; major surgery, trauma, severe metabolic, endocrine or electrolyte disturbances or uncontrolled seizures, concomitant use with ezetimibe.

Reviews about Roxer

Roxer tablets - reviews left on forums by patients taking the drug confirm this fact - are an effective means for lowering cholesterol .

The main advantages of the drug, many of them include a pronounced result, which is observed in a shorter time than when taking drugs similar to Roxera in their pharmacological action.

At the same time, an improvement in the clinical picture often occurs against the background of prescribing an order of magnitude lower dose compared to analogues (for example, Sigmal ).

Use during pregnancy and breastfeeding

Roxera® is contraindicated during pregnancy and lactation.

Women of reproductive age should use adequate methods of contraception.

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

If pregnancy occurs during therapy, use of the drug should be discontinued immediately.

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

Analogues of Roxers

Level 4 ATX code matches:
Akorta

Atomax

Lipitor

Pravastatin

Simvastol

Owencore

Simgal

Tulip

Lovastatin

Liptonorm

Rozulip

Zokor

Rosart

Tevastor

Atorvastatin

Liprimar

Simvastatin

Atoris

Basilip

Rosecard

Analogs of the drug that have the same ATC code, active substance and release form as Roxera are:

• Klyvas 10;
• Klyvas 20;
• Crestor;
• Mertenil;
• Rovics;
• Rosart;
• Rozvator;
• Rosuvastatin Sandoz;
• Rosecard;
• Rozulip;
• Romazik;
• Fastong.

The price of Roxera analogues in Ukraine varies from 65 to 595 hryvnia, on the Russian pharmaceutical market - from 220 to 2100 rubles.

Side effects

Classification of the frequency of side effects: very often - >1/10; often - >1/100, but <1/10; uncommon - >1/1000, but <1/100; rarely - >1/10000, but <1/1000; very rarely - <1/10000, including isolated reports; frequency unknown—cannot be estimated from available data.

Within each group, adverse effects are presented in order of decreasing severity.

The incidence of side effects depends on the dose taken.

From the blood and lymphatic system: frequency unknown - thrombocytopenia.

From the immune system: rarely - hypersensitivity reactions, including angioedema.

From the endocrine system: often - diabetes mellitus type 2.

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

From the respiratory system, chest and mediastinal organs: frequency unknown - cough, shortness of breath.

From the gastrointestinal tract: often - constipation, nausea, abdominal pain; rarely - pancreatitis; frequency unknown - diarrhea.

From the liver and biliary tract: rarely - increased activity of liver transaminases; very rarely - jaundice, hepatitis.

From the skin and subcutaneous tissues: infrequently - itching, skin rash, urticaria; frequency unknown - Stevens-Johnson syndrome.

From the musculoskeletal and connective tissue side: often - myalgia; rarely - myopathy (including myositis) and rhabdomyolysis; very rarely - arthralgia; frequency unknown - immune-mediated necrotizing myopathy.

A dose-dependent increase in CPK activity is observed in a small number of patients taking rosuvastatin. In most cases it is minor, asymptomatic and temporary. If CPK activity increases to more than 5 times the ULN, therapy should be suspended.

From the kidneys and urinary tract: proteinuria is observed in less than 1% of patients receiving a dose of 10-20 mg/day and in about 3% of patients receiving a dose of 40 mg/day. In most cases, proteinuria decreases or disappears during therapy and does not indicate the occurrence of acute or progressive concomitant kidney disease; very rarely - hematuria.

From the genital organs and breast: frequency unknown - gynecomastia.

General disorders and disorders at the injection site: often - asthenia; frequency unknown - peripheral edema.

Laboratory indicators: when using rosuvastatin, an increase in CPK activity, glucose concentration, glycosylated hemoglobin, bilirubin in the blood plasma, GGTP activity, alkaline phosphatase, and changes in the plasma concentration of thyroid hormones were also observed.

The following side effects have been reported with the use of some HMG-CoA reductase inhibitors: depression, sleep disorders, including insomnia and nightmares, sexual dysfunction. Isolated cases of interstitial lung disease have been reported, especially with long-term use of drugs (see "Special Instructions").

Interaction

The effect of the use of other drugs on rosuvastatin

Transport protein inhibitors. Rosuvastatin is a substrate for some transport proteins, in particular OATP1B1 and BCRP. The simultaneous use of drugs that are inhibitors of these transport proteins may be accompanied by an increase in the concentration of rosuvastatin in the blood plasma and an increased risk of developing myopathy (see Table 1, “Dosage and Administration”, “Special Instructions”).

Cyclosporine. With simultaneous use of rosuvastatin and cyclosporine, the AUC of rosuvastatin is on average 7 times higher than the value observed in healthy volunteers (see Table 1). Concomitant use with rosuvastatin does not affect the concentration of cyclosporine in the blood plasma. The use of rosuvastatin is contraindicated in patients taking cyclosporine (see "Contraindications").

HIV protease inhibitors. Concomitant use of HIV protease inhibitors may significantly increase the exposure of rosuvastatin (see Table 1).

The 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 AUC0-24 and Css of rosuvastatin by 2 and 5 times, respectively. Therefore, simultaneous use of rosuvastatin and HIV protease inhibitors is not recommended (see “Dosage and Administration,” Table 1).

Gemfibrozil and other lipid-lowering drugs. The simultaneous use of rosuvastatin and gemfibrozil leads to a 2-fold increase in Cmax and AUC of rosuvastatin in blood plasma (see “Special Instructions”). Based on specific interaction data, a pharmacokinetically significant interaction with fenofibrate is not expected, but a pharmacodynamic interaction is possible. Gemfibrozil, fenofibrate, other fibrates, and lipid-lowering doses of niacin (doses greater than or equivalent to 1 g/day) increased the risk of myopathy when used concomitantly with HMG-CoA reductase inhibitors, possibly due to the fact that they can cause myopathy when used in monotherapy (see “Special Instructions”). 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 (see “Contraindications”, “Dosage and Administration”, “Special Instructions”).

Ezetimibe. The simultaneous use of rosuvastatin at a dose of 10 mg and ezetimibe at a dose of 10 mg was accompanied by an increase in the AUC of rosuvastatin in patients with hypercholesterolemia (see Table 1). A pharmacodynamic interaction between rosuvastatin and ezetimibe, manifested by an increased risk of adverse reactions, cannot be excluded.

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 used 2 hours after taking rosuvastatin. The clinical significance of this interaction has not been studied.

Erythromycin. The simultaneous use of rosuvastatin and erythromycin leads to a decrease in AUC0–t of rosuvastatin by 20% and its Cmax by 30%. This interaction may occur as a result of increased intestinal motility caused by the use of erythromycin.

Cytochrome P450 isoenzymes. The results of in vivo and in vitro studies showed that rosuvastatin is neither an inhibitor nor an inducer of cytochrome P450 isoenzymes. In addition, rosuvastatin is a weak substrate for this isoenzyme system. Therefore, interaction of rosuvastatin with other drugs at the metabolic level involving cytochrome P450 isoenzymes is not expected.

No clinically significant interaction was observed between rosuvastatin, fluconazole (an inhibitor of CYP2C9 and CYP3A4 isoenzymes) and ketoconazole (an inhibitor of CYP2A6 and CYP3A4 isoenzymes).

Interaction with drugs that requires dose adjustment of rosuvastatin (see Table 1)

The dose of rosuvastatin should be adjusted if it is necessary to use it simultaneously with drugs that increase the exposure of rosuvastatin. If an increase in exposure by 2 times or more is expected, the initial dose of rosuvastatin should be 5 mg 1 time per day.

The maximum daily dose of rosuvastatin should also be adjusted so that the expected exposure to rosuvastatin does not exceed that for a dose of 40 mg taken without the simultaneous administration of drugs that interact with rosuvastatin. For example, the maximum daily dose of rosuvastatin when used simultaneously with gemfibrozil is 20 mg (increased exposure by 1.9 times), with ritonavir/atazanavir - 10 mg (increased exposure by 3.1 times).

Table 1

Effect of concomitant therapy on rosuvastatin exposure (AUC, data in descending order) - results of published clinical studies

The effect of rosuvastatin on other drugs

Vitamin K antagonists: As with other HMG-CoA reductase inhibitors, initiating or increasing the dose of rosuvastatin in patients taking concomitant vitamin K antagonists (eg warfarin) may lead to an increase in INR. Discontinuation of rosuvastatin or reduction in its dose may lead to a decrease in MHO. In such cases, MHO monitoring is recommended.

Oral contraceptives/hormone replacement therapy (HRT). The simultaneous use of rosuvastatin and oral contraceptives increases the AUC of ethinyl estradiol and norgestrel by 26 and 34%, respectively. This increase in plasma concentration should be taken into account when selecting the dose of hormonal contraceptives.

There are no pharmacokinetic data on the simultaneous use of rosuvastatin and HRT; 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. A clinically significant interaction between rosuvastatin and digoxin is not expected.

Overdose

Clinical manifestations that may occur when the recommended dose of the drug is exceeded are not described. After a single dose of Roxera at a dose several times greater than the established daily dose, no clinically significant changes in the pharmacokinetics of rosuvastatin were observed.

In case of overdose and the appearance of symptoms of intoxication of the body, symptomatic treatment and, if necessary, a set of supportive measures are prescribed.

It is also recommended to monitor the level of creatine kinase and perform a test to assess liver .

The feasibility of prescribing hemodialysis is considered unlikely.

Directions for use and doses

Inside, do not chew or crush the tablet, swallow it whole with water, can be taken at any time of the day, regardless of meals.

Before starting therapy with Roxera®, the patient should begin to follow a 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 recommendations for 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 Roxera® 1 time per day.

When using the drug simultaneously with gemfibrozil, fibrates, nicotinic acid at a dose of more than 1 g/day, an initial dose of 5 mg is recommended for patients. When choosing the initial dose, you 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 taken into account. 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 additional use of a dose higher than the recommended initial dose for 4 weeks of therapy can only be carried out in patients with severe degree of hypercholesterolemia and a high risk of developing cardiovascular complications (especially in patients with familial hypercholesterolemia) who have not achieved the desired result of therapy when using a dose of 20 mg/day and who will be under medical supervision. Particularly careful monitoring of patients receiving the drug at a dose of 40 mg/day is recommended.

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 when increasing the dose of Roxera®, monitoring of lipid metabolism parameters is necessary (dose adjustment is required if necessary).

Patients with renal failure. No dosage adjustment is required in patients with mild or moderate renal impairment. In patients with severe renal failure (creatinine clearance less than 30 ml/min), the use of Roxera® is contraindicated. The use of the drug in a dose of more than 30 mg/day in patients with moderate to severe renal failure (creatinine clearance less than 60 ml/min) is contraindicated. For patients with moderate renal failure, the recommended initial dose of the drug is 5 mg/day.

Patients with liver failure. Roxera® is contraindicated in patients with active liver disease. There is no experience with the use of the drug in patients with liver failure above 9 points (class C) on the Child-Pugh scale.

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

Ethnic groups. When studying the pharmacokinetic parameters of rosuvastatin in patients belonging to different ethnic groups, an increase in the systemic concentration of rosuvastatin was noted among the Japanese and Chinese. This fact should be taken into account when using the drug Roxera® in these groups of patients. When using doses of 10 and 20 mg/day, the recommended initial dose for patients of the Mongoloid race is 5 mg/day. For patients of the Mongoloid race, the use of Roxera® at a dose of 40 mg is contraindicated.

Genetic polymorphism. Carriers of the SLCO1B1 (OATP1B1) c.521CC and ABCG2 (BCRP) c.421AA genotypes had an increase in rosuvastatin exposure (AUC) compared to carriers of the SLCO1B1 c.521TT and ABCG2 c.421CC genotypes. For patients carrying genotypes c.521CC or c.421AA, the recommended maximum dose of Roxera® is 20 mg once a day.

Patients predisposed to myotoxic complications. The use of Roxera® in a dose of 40 mg is contraindicated in patients predisposed to the development of myotoxic complications. If it is necessary to use doses of 10 and 20 mg/day, the recommended initial dose for this group of patients is 5 mg.

Concomitant therapy. Rosuvastatin binds to various transport proteins (in particular OATP1B1 and BCRP). When using Roxera® with drugs (such as cyclosporine, some human immunodeficiency virus (HIV) protease inhibitors, including a combination of ritonavir with atazanavir, lopinavir and/or tipranavir) that increase the concentration of rosuvastatin in the blood plasma due to interaction with transport proteins, the risk of developing myopathy (including rhabdomyolysis) may increase. In such cases, the possibility of using alternative therapy or temporarily stopping taking Roxera® should be assessed. If it is necessary to use the above drugs, the benefit-risk ratio of concomitant therapy with Roxera® should be assessed and the possibility of reducing its dose should be considered.

Roxer tablets: instructions for use, method of administration and dosage regimen

Before prescribing the drug, the patient is recommended to switch to a standard diet, the purpose of which is to reduce cholesterol . It is necessary to adhere to this diet throughout the entire course of treatment.

The dose is selected individually by the attending physician depending on the purpose of therapy and its effectiveness. The drug can be taken at any time of the day, without being tied to meal times.

The tablet is swallowed whole, without crushing or chewing, and with a sufficient amount of water.

Patients with hypercholesterolemia should start taking the drug with doses equal to 5 or 10 mg of rosuvastatin . The tablets are taken orally, one per day. Moreover, this condition persists both for patients who have not been treated with statins , and for patients who have already undergone treatment with drugs that suppress the activity of hydroxymethylglutaryl-CoA reductase .

cholesterol concentrations , and also assesses the risks of developing cardiovascular complications and side effects.

In cases where this is necessary, the dose may be adjusted to the next level, however, such an adjustment should be made no earlier than 4 weeks after the first prescription.

Considering that adverse reactions are dose-dependent and occur more often when taking 40 mg of rosuvastatin than when taking it in smaller quantities, increasing the daily dose to 30 or 40 mg should be carried out with particular care for:

• patients with severe forms of hypercholesterolemia ;
• patients who are at high risk of developing complications in the function of the heart and vascular system (in particular, if the patient is diagnosed with familial hypercholesterolemia ).

If taking smaller doses of rosuvastatin in these categories of patients did not give the expected result, after prescribing Roxera at a dosage of 30 or 40 mg per day, patients must be constantly monitored by their doctor.

Also, regular monitoring by a doctor is indicated in cases where treatment is started immediately with a dose of 30 or 40 mg.

In accordance with the instructions for use, Roxera 20 mg is indicated as an initial dose for the prevention of heart and vascular diseases in patients who have an increased risk of developing such pathologies.

renal dysfunction do not need to adjust the dose; however, the drug is prescribed to this group of patients with caution.

For renal , when creatinine is within 60 ml/min, treatment begins with a dose of 5 mg. High doses of the drug (30 and 40 mg) are contraindicated.

renal dysfunction are prohibited from prescribing the drug in any dosage.

When Roxera is prescribed to patients with liver pathologies whose Child-Pugh do not exceed 7, there is no increase in systemic exposure to rosuvastatin .

liver dysfunction scores are 8 or 9 on the Child-Pugh scale , systemic exposure is increased. Therefore, before prescribing the drug to such patients, additional testing of renal function is required.

experience in treating patients whose scores exceed 9 points on the Child-Pugh scale .