Roxer's
Roxera: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Roxera
ATX code: C10AA07
Active ingredient: rosuvastatin (rosuvastatinum)
Manufacturer: KRKA (Slovenia)
Description and photo update: 2018-22-10
Prices in pharmacies: from 250 rubles.
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Roxera is a drug with hypolipidemic action.
Release form and composition
Dosage form Roxera - film-coated tablets: biconvex, white, the core on the cross section is white; 5 mg each - round, with a chamfer, marking "5" on one side, applied by embossing; 10 mg each - round, with a chamfer, marking "10" on one side, applied by embossing; 15 mg each - round, with a chamfer, marking "15" on one side, applied by embossing; 20 mg each - round, chamfered; 30 mg each - capsule form, on both sides with a line; 40 mg - capsule form (in a blister strip of 7 pcs., in a cardboard box 2, 4, 8 or 12 packs; in a blister strip of 10 pcs., in a cardboard box of 1-3, 6 or 9 packs; in blister packs of 14 pcs., in a cardboard box 1, 2, 4 or 6 packages).
The active ingredient in 1 tablet: rosuvastatin - 5, 10, 15, 20, 30 or 40 mg (in the form of rosuvastatin calcium - 5.21; 10.42; g 15.62; 20.83; 31.25 or 41, 66 mg).
Additional components (5/10/15/20/30/40 mg):
- core: lactose - 40/40/60/80/120/160 mg; colloidal silicon dioxide - 0.33 / 0.33 / 0.5 / 0.66 / 0.99 / 1.32 mg; magnesium stearate -1.88 / 1.88 / 2.82 / 3.76 / 5.64 / 7.52 mg; crospovidone - 7.5 / 7.5 / 11.25 / 15 / 22.5 / 30 mg; microcrystalline cellulose - 95.08 / 89.87 / 134.81 / 179.75 / 269.62 / 359.50 mg;
- shell: copolymer of butyl methacrylate, methyl methacrylate and dimethylaminoethyl methacrylate [1: 1: 2] - 1.1 / 1.1 / 1.65 / 2.2 / 3.3 / 4.4 mg; titanium dioxide - 0.5 / 0.5 / 0.75 / 1 / 1.5 / 2 mg; macrogol - 6000 - 0.9 / 0.9 / 1.35 / 1.8 / 2.7 / 3.5 mg; lactose monohydrate - 2/2/3/4/6/8 mg.
Pharmacological properties
Pharmacodynamics
Roxera is a lipid-lowering drug. As an active component, it contains rosuvastatin - a selective, competitive inhibitor of hydroxymethylglutaryl coenzyme A (HMG-CoA) reductase (an enzyme that converts 3-hydroxy-3-methylglutaryl coenzyme A into a cholesterol precursor - mevalonic acid). The action of the drug is directed at the liver, which is associated with the synthesis of cholesterol (CS) and catabolism of low density lipoproteins (LDL).
Thanks to rosuvastatin, the number of hepatic LDL receptors on the cell surface increases, which leads to an increase in the uptake and catabolism of LDL. This, in turn, causes the inhibition of the synthesis of very low density lipoproteins (VLDL) and a decrease in the total number of LDL and VLDL.
Rosuvastatin helps to reduce elevated plasma concentrations of LDL cholesterol (LDL-C), triglycerides (TG), total cholesterol, increase the concentration of high-density lipoprotein cholesterol (HDL-C). The following ratios decrease: cholesterol-LDL / cholesterol-HDL, cholesterol not associated with HDL (cholesterol-non-HDL) / cholesterol-HDL and total cholesterol / cholesterol-HDL, as well as the ratio of ApoV / ApoA-1. In addition, Roxera reduces the concentration of non-HDL-C, apolipoprotein B (ApoB), TG-VLDL, VLDL-C and increases the plasma concentration of apolipoprotein AI in the blood.
The development of the therapeutic effect is observed during the first 7 days of taking the drug, after 14 days of treatment it reaches 90% of the maximum possible. Usually, the maximum therapeutic effect is achieved by the 28th day of treatment, and with regular intake of the drug, it is maintained in the future.
Roxera is effective in adult patients with hypercholesterolemia with / without concomitant hypertriglyceridemia, including patients with familial hypercholesterolemia or diabetes mellitus. Race, gender, or age have no effect on its effectiveness.
In most cases (80%) with hypercholesterolemia IIa and IIb type according to Fredrickson (with an average initial concentration of LDL-C of approximately 4.8 mmol / L) against the background of the use of 10 mg of rosuvastatin, the concentration of LDL-C reaches values less than 3 mmol / L. In homozygous familial hypercholesterolemia, rosuvastatin was administered in doses of 20–40 mg, with an average decrease of 22%.
The additive effect of rosuvastatin is manifested in combination with fenofibrate in relation to the TG content, with nicotinic acid in doses that reduce lipid content in relation to the concentration of HDL-C-C.
Pharmacokinetics
The time to reach the maximum plasma concentration (Cmax) of rosuvastatin in the blood after oral administration is approximately 5 hours. The absolute bioavailability of the substance is ~ 20%. Metabolism occurs mainly in the liver. The volume of distribution is approximately 134 liters. Most of the substance (about 90%) binds to blood plasma proteins, mainly albumin.
Rosuvastatin undergoes limited metabolism (~ 10%). The substance belongs to non-specific substrates of cytochrome P450. The main isoenzyme involved in its metabolism is the CYP2C9 isoenzyme. Involvement of isoenzymes CYP2C19, CYP3A4, CYP2D6 in metabolism occurs to a lesser extent. The main known metabolites are N-desmethylrosuvastatin (the activity is about 2 times lower than that of rosuvastatin) and lactone metabolites (they have no pharmacological activity). Pharmacological activity for inhibition of plasma HMG-CoA reductase is provided mainly due to rosuvastatin (more than 90%).
Approximately 90% of the substance is excreted unchanged through the intestines (including unabsorbed / absorbed rosuvastatin); the rest is by the kidneys. The half-life of a substance from blood plasma is approximately 19 hours (an increase in dose does not affect this indicator). Average geometric plasma clearance - 50 l / h (with a coefficient of variation - 21.7%).
With daily administration, no changes in pharmacokinetic parameters are observed. Systemic exposure increases in proportion to dose.
According to pharmacokinetic studies, in patients of the Mongoloid race (Japanese, Filipinos, Chinese, Koreans and Vietnamese), the median AUC and the maximum concentration of rosuvastatin increase approximately 2 times in comparison with the Caucasian race; for Indians, the coefficient of increase in median AUC and Cmax is 1.3.
In patients with creatinine clearance (CC) less than 30 ml / min, the plasma concentration of rosuvastatin and N-desmethylrosuvastatin in the blood increases significantly.
In chronic alcoholic liver disease, the plasma concentration of rosuvastatin increases moderately. In comparison: patients with normal liver function / patients with hepatic impairment (on the Child-Pugh scale: 7 and below points / 8-9 points) AUC and Cmax of rosuvastatin increase by 5 and 60% / 21 and 100%, respectively. The experience of taking rosuvastatin in patients with liver failure above 9 points is absent.
Indications for use
- primary hypercholesterolemia according to the Fredrickson classification (type IIa, including familial heterozygous hypercholesterolemia) or mixed hypercholesterolemia (type IIb): Roxera is prescribed as an adjunct to diet in cases where diet and other non-drug methods of therapy (for example, exercise, weight loss) are not effective enough;
- familial homozygous hypercholesterolemia: taking Roxera is indicated as an adjunct to diet and other lipid-lowering therapy (for example, LDL apheresis), or in cases where such therapy is not effective enough;
- hypertriglyceridemia (according to Fredrickson's classification - type IV): the drug is prescribed as an addition to the diet;
- atherosclerosis: Roxera is used to slow the progression of the disease as an addition to the diet in patients who are indicated for treatment in order to reduce the plasma concentration of cholesterol and LDL-C;
- cardiovascular complications (stroke, myocardial infarction, arterial revascularization): the drug is indicated for the primary prevention of these complications in adult patients in the absence of clinical signs of coronary heart disease (IHD), but with an increased risk of its occurrence, including the age of 50/60 years (men / women), increased plasma concentration of C-reactive protein (≥ 2 g / L) in the presence of at least one of the additional risk factors - arterial hypertension, low plasma concentration of HDL-C, smoking, family history of early onset of coronary artery disease.
Contraindications
Absolute:
- the active phase of liver diseases, including a steady increase in the activity of hepatic transaminases and the serum activity of hepatic transaminases in the blood more than 3 times compared with VGN (upper limit of the norm);
- renal failure in severe course (CC less than 30 ml / min);
- myopathy;
- combination therapy with cyclosporine;
- syndrome of glucose-galactose malabsorption, lactose intolerance, lactase deficiency;
- the presence of a predisposition to the appearance of myotoxic complications;
- lack of adequate contraceptive protection in women of childbearing age;
- period of pregnancy and lactation;
- age up to 18 years;
- the presence of individual intolerance to the active / additional components of the Roxera.
Additionally, for a dose ≥ 30 mg per day:
- renal failure of moderate and severe degree (CC less than 60 ml / min);
- myotoxicity with the use of other inhibitors of HMG-CoA reductase or fibrates in anamnesis;
- conditions that can lead to an increase in the plasma concentration of rosuvastatin in the blood;
- hypothyroidism;
- burdened history, including family history, of muscle diseases;
- alcohol abuse;
- combination therapy with fibrates;
- belonging to the Mongoloid race.
Relative contraindications for a dose <30 mg per day (conditions and / or diseases, in the presence of which caution and medical supervision are required when prescribing Roxera): alcohol abuse; sepsis; arterial hypotension; the risk of myopathy / rhabdomyolysis, including renal failure, hypothyroidism, aggravated history, including family history of hereditary muscle diseases and a previous history of muscle toxicity with the use of other HMG-CoA reductase inhibitors or fibrates; endocrine system disorders, metabolic / electrolyte disturbances in severe course or uncontrolled seizures; conditions in which there is an increase in the plasma concentration of rosuvastatin; belonging to the Mongoloid race (Chinese, Japanese); trauma, major surgical interventions;a history of indications of liver disease; combination therapy with fibrates, ezetimibe; age from 65 years.
Relative contraindications for a dose of ≥ 30 mg per day (conditions and / or diseases, in the presence of which, when prescribing Roxera, caution and medical supervision are required): renal failure in a mild course (CC more than 60 ml / min); carrying out extensive surgical interventions, trauma; the presence of indications in the history of liver disease; sepsis; arterial hypotension; endocrine system disorders, metabolic / electrolyte disturbances in severe course or uncontrolled seizures; combination therapy with ezetimibe; age from 65 years.
Instructions for use of Roxera: method and dosage
Roxer's tablets are taken orally with water. The tablet should be swallowed without crushing or chewing. Food intake and time of day do not affect the effectiveness of the drug.
Before the course of therapy, it is necessary to begin adherence to the standard cholesterol-lowering diet. During the period of taking the drug, it should be adhered to constantly.
The doctor determines the dosage regimen individually, depending on the goal and the therapeutic response to taking the drug.
Patients starting to take Roxera, as well as when switching from other HMG-CoA reductase inhibitors, are usually prescribed 5 or 10 mg per day.
In cases of combined use with fibrates, gemfibrozil, nicotinic acid in lipid-lowering doses (more than 1000 mg per day), it is recommended to start taking Roxera with 5 mg per day. When choosing an initial dose, the doctor should be guided by the concentration of cholesterol in the patient's blood plasma and take into account the existing or potential risk of adverse reactions (complications) from the cardiovascular system. The dose is increased if necessary after 4 weeks.
Prescription of Roxera at a maximum dose of 40 mg per day is possible only for patients with severe hypercholesterolemia and with a high risk of complications from the cardiovascular system (especially in cases of familial hypercholesterolemia), in whom the desired result was not achieved with the use of 20 mg per day … Therapy should be carried out only under medical supervision.
Taking Roxera at a dose of 40 mg per day in patients who have not previously consulted a doctor is not recommended. After 2-4 weeks of use or with each increase in the dose of the drug, it is necessary to monitor the parameters of lipid metabolism (if necessary, dose adjustment may be required).
The recommended daily dose for patients with moderate renal insufficiency is 5 mg.
The initial dose for patients of the Mongoloid race is 5 mg per day, at a dose of 40 mg Roxer is not prescribed to them.
For patients with c.421AA or c.521CC genotypes, the recommended maximum daily dose is 20 mg once a day.
If there is a predisposition to myotoxic complications, Roxer is not prescribed at a dose of 40 mg per day. If it is necessary to use daily doses of 10 and 20 mg, the recommended initial daily dose is 5 mg.
In the case of combination therapy with drugs, the use of which leads to an increase in the plasma concentration of rosuvastatin in the blood, the risk of myopathy (including rhabdomyolysis) may increase. If it is necessary to prescribe such drugs, it is necessary to assess the likelihood of alternative treatment or temporary interruption of Roxera's intake, as well as the ratio of benefit to risk, and consider the possibility of reducing the dose of the drug.
Side effects
Adverse reactions, the development of which can be observed during the therapy period (> 10% - very often;> 1% and 0.1% and 0.01% and <0.1% - rarely; <0.01% - very rarely; c indefinite frequency - in cases where it is impossible to determine the frequency of occurrence of a violation from the available data):
- immune system: rarely - hypersensitivity reactions, including angioedema;
- lymphatic system and blood: with an uncertain frequency - thrombocytopenia;
- endocrine system: often - non-insulin dependent diabetes;
- respiratory system: with an uncertain frequency - shortness of breath, cough;
- subcutaneous tissue and skin: infrequently - skin rash / itching, urticaria; with an indefinite frequency - Stevens-Johnson syndrome;
- nervous system: often - dizziness, headache; very rarely - memory impairment / loss; with an uncertain frequency - peripheral neuropathy;
- digestive system: often - abdominal pain, nausea, constipation; rarely - inflammation of the pancreas; very rarely - hepatitis, jaundice; with an undefined frequency - diarrhea; in some cases, a dose-dependent increase in the activity of hepatic transaminases in the blood plasma (usually short-term, insignificant, asymptomatic);
- genitals and mammary gland: with an unknown frequency - gynecomastia;
- urinary tract and kidneys: proteinuria (as a rule, its symptoms decrease or disappear during treatment, the appearance of this complication does not mean the development of acute kidney disease or the progression of an existing one); very rarely - hematuria;
- musculoskeletal system, connective tissue: often - myalgia; rarely - myopathy (including myositis), rhabdomyolysis (may occur with acute renal failure); very rarely - arthralgia; with an indefinite frequency - immune-mediated necrotizing myopathy; in a small number of patients - a dose-dependent increase in the activity of creatine phosphokinase in the blood plasma (as a rule, short-term, insignificant, asymptomatic), in cases of a significant increase - more than 5 times in comparison with VGN, therapy is suspended;
- laboratory parameters: hyperglycemia, changes in the serum concentration of thyroid hormones, an increase in the plasma concentration of bilirubin in the blood, the activity of gamma-glutamyltransferase, alkaline phosphatase in the blood plasma;
- general disorders: often - asthenic syndrome; with an unknown frequency - peripheral edema.
There is information about the development of the following disorders against the background of the use of some inhibitors of HMG-CoA reductase (statins): sexual dysfunction and sleep disorders, depression, increased concentration of glycosylated hemoglobin; in isolated cases - diffuse parenchymal diseases of the lungs, especially during a long course of therapy.
Overdose
There is no information on the clinical picture of an overdose. There is no change in the pharmacokinetic parameters of the active substance when taking high doses of Roxera.
Rosuvastatin does not have a specific antidote, hemodialysis is ineffective. In cases of overdose, symptomatic therapy is carried out under the control of liver function and creatine phosphokinase activity.
special instructions
Patients who received high doses of Roxera (for example, 40 mg per day), observed tubular proteinuria, detected using test strips. As a rule, it is periodic or short-lived. Such proteinuria does not indicate acute illness or progression of concomitant kidney disease. Patients taking Roxera in a daily dose of 30 or 40 mg during treatment are recommended to monitor renal function indicators. Research should be carried out at least once every 3 months.
In cases of taking rosuvastatin in all doses, but in particular those exceeding 20 mg per day, there have been reports of the following effects on the musculoskeletal system: myopathy, myalgia, in rare cases, rhabdomyolysis. There is information about very rare cases of rhabdomyolysis with the simultaneous use of Roxera with ezetimibe. This combination should be administered with caution. The incidence of rhabdomyolysis in post-marketing studies was higher with a dose of 40 mg per day.
If, before the appointment of Roxera, the activity of creatine phosphokinase is significantly exceeded (exceeding VGN by 5 times), it is recommended to re-measure it after 5-7 days. When the indicators are confirmed, therapy is not started. It should be taken into account that in order to avoid distortion of the results, it is impossible to determine this indicator after increased physical exertion or in the presence of other possible reasons for its increase.
In patients with glucose concentrations in the range of 5.6–6.9 mmol / L, the use of Roxera was associated with an increased risk of non-insulin dependent diabetes.
In the presence of factors that increase the likelihood of myopathy and rhabdomyolysis, the drug should be prescribed with caution.
In cases of sudden onset of spasms, muscle pain, muscle weakness, especially if they are accompanied by fever and malaise, you should consult a doctor.
In case of hypercholesterolemia associated with hypothyroidism, nephrotic syndrome, before starting to take Roxera, therapy for the underlying disease should be carried out.
Influence on the ability to drive vehicles and complex mechanisms
Patients driving motor vehicles should take into account the likelihood of adverse reactions, including dizziness.
Application during pregnancy and lactation
It is contraindicated to take Roxer's tablets during pregnancy and lactation.
In case of pregnancy, the drug is canceled.
Women of reproductive age are advised to use adequate contraceptive protection.
Pediatric use
According to the instructions, Roxera is not used in pediatric practice in children and adolescents under 18 years of age.
With impaired renal function
In severe renal failure (CC less than 30 ml / min), Roxer is not prescribed.
In case of moderate and severe renal failure (CC less than 60 ml / min), Roxera is used only at a dose of up to 30 mg per day.
The initial dose for moderate renal failure is 5 mg per day.
For violations of liver function
With liver diseases in the active phase, Roxer cannot be used.
Use in the elderly
For patients over 65 years of age, Roxera should be administered with caution.
Drug interactions
- inhibitors of transport proteins: an increase in the plasma concentration of rosuvastatin in the blood and an increased risk of myopathy;
- HIV protease inhibitors: significant increase in rosuvastatin exposure (combination not recommended);
- cyclosporine: a significant increase in the AUC of rosuvastatin (the combination is contraindicated);
- ezetimibe: increased AUC of rosuvastatin in patients with hypercholesterolemia; increasing the likelihood of adverse reactions;
- gemfibrozil and other hypolipidemic agents: a significant increase in the maximum concentration and AUC of rosuvastatin in blood plasma, an increase in the likelihood of myopathy; the combined use of rosuvastatin in a daily dose of 30 mg and fibrates is contraindicated;
- erythromycin: decrease in AUC (0 – t) and Cmax of rosuvastatin;
- antacids containing aluminum and magnesium hydroxide: a significant decrease in the plasma concentration of rosuvastatin (a decrease in the effect can be achieved by observing an interval of 2 hours between taking these drugs);
- fusidic acid: an increase in the likelihood of rhabdomyolysis, which requires close attention to the patient's condition, it may be necessary to temporarily stop taking rosuvastatin;
- vitamin K antagonists: an increase in the international normalized ratio (M HO) at the beginning of the use of rosuvastatin and with an increase in its dose; decrease in MHO when canceling rosuvastatin or reducing its dose (monitoring of this indicator is required);
- oral contraceptives, hormone replacement therapy: an increase in the AUC of ethinyl estradiol and norgestrel (it may be necessary to adjust the doses of these drugs).
In cases of the need for combined use with drugs that lead to an increase in the exposure of rosuvastatin, the dose of Roxera is adjusted.
Analogs
Roxera's analogues are: Rosulip, Krestor, Rustor, Rosart, Reddistatin, Akorta, Mertenil, Lipoprime, Rosuvastatin, Suvardio, Tevastor, Rosistark, Rosufast, Rosucard.
Terms and conditions of storage
Store at temperatures up to 25 ° C. Keep out of the reach of children.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Roxer
According to reviews, Roxera effectively lowers cholesterol levels. It is noted that the drug begins to exert a therapeutic effect faster than other drugs with a similar effect. With good tolerance, long-term therapy is possible. Of the shortcomings, they point to a rather high cost and the development of side effects.
Roxera price in pharmacies
The approximate price for the Roxer is:
- 5 mg (in a package of 30 or 90 pcs.): 365-420 or 835-925 rubles;
- 10 mg (in a package of 30 or 90 pcs.): 480-580 or 1050-1175 rubles;
- 15 mg (in a package of 30, 60 or 90 pcs.): 565-635, 1260-1360 or 1360-1395 rubles;
- 20 mg (in a package of 20, 30, 60 or 90 pcs.): 760, 700-780, 1680-1710 or 1720 rubles.
Roxera: prices in online pharmacies
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Drug name Price Pharmacy |
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Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
