Roxera refers to lipid-lowering drugs, the main active ingredient of which is rosuvastatin.
It is a competitive selective inhibitor of the enzyme reductase, which converts methylglutaryl coenzyme into mevalonic acid (direct precursor of cholesterol). The therapeutic effect on the background of taking the medicine Roxer develops within 7 days after the start of use. Maximum - after 1 month of regular use and maintained throughout the entire course of treatment.
The maximum concentration of the active substance in the blood is observed 5 hours after administration. The half-life is 20 hours and does not change when using high therapeutic dosages. Rosuvastatin - 90% of the dose - is excreted in an unchanged state with feces. The rest is through the urinary system.
Clinical and pharmacological group
Terms of sale from pharmacies
You can buy by prescription.
How much does Roxer in pharmacies? The approximate price for Roxer is:
- 5 mg (in a package of 30 or 90 pieces): 365-420 or 835-925 rubles;
- 10 mg (in a package of 30 or 90 pieces): 480-580 or 1050-1175 rubles;
- 15 mg (in a package of 30, 60 or 90 pieces): 565-635, 1260-1360 or 1360-1395 rubles;
- 20 mg (in a package of 20, 30, 60 or 90 pieces): 760, 700-780, 1680-1710 or 1720 rubles.
Composition and release form
The drug is available in dosage form tablets for oral administration (oral administration). They have a round shape, a biconvex surface and white color.
- The active ingredient in the composition of 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.
The tablets are packaged in a blister of 10 pieces. The carton pack contains 3 or 9 blisters and instructions for use of the drug.
Pharmacological action of the drug Roxera is aimed at:
- Suppression of the activity of the microsomal hydroxymethylglutaryl-CoA reductase enzyme, which acts as a catalyst for the limiting early stage of cholesterol synthesis.
- Normalization of lipid profile (lipid-lowering effect) by reducing the concentration of total cholesterol, triglycerides, low-density lipoprotein in the blood, as well as increasing the concentration of high-density lipoprotein.
The drug belongs to the statins pharmacological group.
Indications for use
The indications for the use of the drug are:
- The development of atherosclerosis in patients who are prescribed therapy for reducing plasma concentrations of Xc and Xc-LDL;
- Mixed dyslipidemia or primary hypercholesterolemia (as a supplement to the diet with the ineffectiveness of non-drug therapies - weight loss, exercise, etc.);
- Familial homozygous hypercholesterolemia (as a supplement to the previous treatment method);
- Type IV hypertriglyceridemia (as a supplement to the diet);
- Primary prevention of heart disease (arterial revascularization, myocardial infarction, stroke) in patients with a predisposition to coronary heart disease, as well as in the elderly.
Before prescribing the drug, the patient must begin to follow the standard cholesterol-lowering diet and not disturb it during the treatment period.
Contraindications for the use of the drug to 30 ml / day:
- pregnancy and lactation;
- women of childbearing age who do not use effective methods of contraception;
- lactose intolerance, glucose-galactose malabsorption syndrome, lack of lactase;
- liver disease in an active form, including the excess of the rate of hepatic transaminases in the blood plasma by more than 3 times in relation to VGN;
- severe renal failure;
- history of myotoxic complications;
- simultaneous therapy with cyclosporine;
- age up to 18 years;
- hypersensitivity to the drug.
Indications for applying a dose of more than 30 mg / day:
- muscular diseases in history;
- myotoxicity when taking fibrates or HMG-CoA reductase inhibitors in history;
- synchronous use of fibrates;
- alcohol consumption;
- liver disease in the active phase and excess accumulation of transaminases in the blood more than 3 times;
- renal failure, including acute;
- simultaneous use of cyclosporine;
- history of myotoxic complications;
- pregnancy and lactation;
- the child-bearing age of women who do not use reliable contraceptive methods;
- lactase deficiency, lactose intolerance, glucose-galactose malabsorption syndrome;
- 18 years old;
- hypersensitivity to the drug;
- representatives of the Mongoloid race.
The drug should be used with extreme caution in patients over 65 years of age who suffer from arterial hypotension, sepsis who have suffered injuries, surgery and disorders of the metabolic, endocrine and electrolyte processes, as well as in the presence of uncontrolled seizures and simultaneous use of ezetimibe.
Appointment during pregnancy and lactation
Take Roxer tablets during pregnancy and lactation is contraindicated.
In the event of pregnancy, the drug is canceled.
Women in reproductive age are recommended to use adequate contraceptive protection.
Dosage and method of use
As indicated in the instructions for use Roxer taken orally. The tablet should not be chewed or crushed, swallowed whole, washed down with water, can be taken at any time of the day, regardless of the meal.
- Before starting therapy with Roxer, the patient should begin to follow the standard cholesterol-lowering diet and continue to follow it during treatment. The dose of the drug should be chosen individually depending on the goals of therapy and the therapeutic response to treatment, taking into account national recommendations on target plasma lipid concentrations.
- The recommended initial dose for patients starting to take the drug, or for patients transferred from taking other HMG-CoA reductase inhibitors, should be 5 or 10 mg 1 time / day.
- With simultaneous use of the drug with gemfibrozil, fibrates, nicotinic acid in a dose of more than 1 g / day, patients are recommended an initial dose of 5 mg. When choosing the initial dose, one should be guided by the individual concentration of cholesterol in the blood plasma and take into account the possible risk of developing cardiovascular complications; The potential risk of side effects must also be considered. If necessary, the dose may be increased after 4 weeks.
- Due to the possible development of side effects when applying a dose of 40 mg / day, compared with lower doses of the drug, increasing the dose to 40 mg / day after additional use of the dose above the recommended initial dose during 4 weeks of therapy can only be carried out patients with severe hypercholesterolemia and with a high risk of developing cardiovascular complications (especially in patients with familial hypercholesterolemia) who have not achieved the desired result of therapy with a dose of 20 mg / day and who will be under the supervision of a physician. 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 with an increase in the dose of Roxer's drug, monitoring of lipid metabolism indices is necessary (dose adjustment is required if necessary).
In case of impaired renal function
In patients with renal insufficiency, mild or moderate severity of dose adjustment is not required. In patients with severe renal insufficiency (CK less than 30 ml / min), use of Roxera is contraindicated. The use of the drug in a dose of more than 30 mg / day is contraindicated in patients with moderate to severe renal failure (CC less than 60 ml / min). For patients with moderate renal insufficiency, the recommended initial dose of the drug is 5 mg / day.
With abnormal liver function
Roxera is contraindicated in patients with liver disease in the active phase. The experience of using the drug in patients with hepatic insufficiency is higher than 9 points (class C) on the Childe-Pugh scale is absent.
Adverse reactions, the development of which may occur during the period of therapy (> 10% - very often;> 1% and 0.1% and 0.01% and <0.1% - rarely; <0.01% - very rarely; with uncertain frequency - in cases when it is impossible to determine the frequency of occurrence of a violation from the available data):
- urinary tract and kidneys: proteinuria (as a rule, its symptoms in the process of treatment diminish or disappear, 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, immuno-mediated necrotizing myopathy; in a small number of patients - a dose-dependent increase in plasma creatine phosphokinase activity (as a rule, short-term, insignificant, asymptomatic), in cases of significant increase - more than 5 times in comparison with VGN therapy stop;
- immune system: rarely - hypersensitivity reactions, including angioedema;
- lymphatic system and blood: with an uncertain frequency - thrombocytopenia;
- endocrine system: often - insulin-independent diabetes;
- respiratory system: with uncertain frequency - shortness of breath, cough;
- subcutaneous tissue and skin: infrequently - skin rash / itching, urticaria; with indefinite frequency - Stevens-Johnson syndrome;
- nervous system: often - dizziness, headache; very rarely - memory impairment / loss; with uncertain frequency - peripheral neuropathy;
- digestive system: often - abdominal pain, nausea, constipation; rarely - inflammation of the pancreas; very rarely - hepatitis, jaundice; with uncertain frequency - diarrhea; in some cases, a dose-dependent increase in the activity of hepatic transaminases in the blood plasma (as a rule, short-term, insignificant, asymptomatic);
- genitals and mammary gland: with unknown frequency - gynecomastia;
- laboratory indicators: hyperglycemia, changes in the serum concentration of thyroid hormones, increased plasma concentrations of bilirubin in the blood, the activity of gamma-glutamyltransferase, alkaline phosphatase in the blood plasma;
- common disorders: often - asthenic syndrome; with unknown frequency - peripheral edema.
There is evidence of the development of the following disorders on the background of the use of certain inhibitors of HMG-CoA reductase (statins): impaired sexual function and sleep, depression, increased concentrations of glycosylated hemoglobin; in rare cases - diffuse parenchymal lung diseases, especially when conducting a long course of therapy.
A single dose of several daily doses of Roxer's tablets is not displayed on the pharmacokinetics of the active substance and does not lead to an overdose. Receiving higher doses may be accompanied by the appearance or increase of negative side effects.
In this case, washing the stomach, intestines, receiving intestinal sorbents (activated carbon), and symptomatic therapy is carried out, which is associated with the absence of a specific antidote.
Patients who received Roxer in high doses (for example, 40 mg per day) had tubular proteinuria, which was detected using test strips. As a rule, it is periodic or short-lived. Such proteinuria does not indicate an acute illness or progression of concomitant kidney disease. Patients taking Roxer at a daily dose of 30 or 40 mg are recommended to monitor the indicators of renal function during treatment. Studies should be conducted at least once every 3 months.
In cases of receiving rosuvastatin in all doses, but in particular exceeding 20 mg per day, the following effects on the musculoskeletal system were reported: myopathy, myalgia, and 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 prescribed with caution. The incidence of rhabdomyolysis in post-registration studies was higher with a dose of 40 mg per day.
If, before the administration of the Roxera, the activity of creatine phosphokinase is significantly exceeded (VGN excess is 5 times), it is recommended to re-measure after 5-7 days. When confirming the indicators, therapy is not started. It is necessary to take into account that in order to avoid distortion of the results, this indicator cannot be determined after increased physical exertion or if there are other possible reasons for its increase.
In patients with a glucose concentration in the range of 5.6-6.9 mmol / l, the use of Roxera was associated with an increased risk of insulin-independent diabetes.
In the presence of factors that increase the likelihood of myopathy and rhabdomyolysis, the drug should be administered with caution.
In cases of sudden spasms, muscle pain, muscle weakness, especially if they are accompanied by fever and malaise, you should consult a doctor.
When hypercholesterolemia is associated with hypothyroidism, nephrotic syndrome, before the start of taking Roxera, the main disease should be treated.
Interaction with other drugs
Statin "Roster" is not used during treatment with cephalosporin-type antibiotics. While taking anticoagulants, rosuvastatin may contribute to an increase in prothrombin time.
With simultaneous treatment with the anti-lipid agent "Ezetimib", other fibrates are extremely high risk of developing myopathy. Rosuvastatin does not interact with cytochrome P450.
Drugs used to treat HIV increase the availability of rosuvastatin. Therefore, effective dosages should be reviewed.
Acceptance of antacid agents based on aluminum and magnesium salts, erythromycin reduces the absorbability of the active substances "Roxer" by 20-50%. This effect does not appear if the antacid is taken 2 hours after the use of rosuvastatin.
When taken simultaneously with the drugs of the fibrates group, chemical interaction with the active component of the Roxer does not occur. But since these agents have a similar effect, the risk of myopathy development increases.
Rosuvastatin, when taken with hormonal contraceptives, increases the concentration of ethinyl estradiol and norgestrel blood. However, there is no data on the negative effect of a statin on hormone replacement therapy.
The antimycotic "Intraconazole" increases the absorption of rosuvastatin, but the administration of "Fluconazole" and "Ketoconazole" does not affect the distribution of the active ingredient "Roxera".
We offer you to read the reviews of people who used the drug Roxer:
- Anton. An effective drug, cheaper than Cresto 2 times and no worse. active substances too. In 2 months, total cholesterol went down from 6 to 4. There is more good cholesterol, less bad.In general, I will drink for life as prescribed by the doctor.
- Oksana. This is a very good lipid-lowering drug, it acts very quickly and effectively. After taking for 1 month, the result is already visible, cholesterol is reduced, atherosclerotic plaques are reduced, the risk of cardiovascular diseases is reduced. Convenient reception, 1 time per day. Price and quality are excellent, this drug can be trusted. Side effects are not observed.
Structural analogues of the active substance:
Before buying an analogue, consult your doctor.
Shelf life and storage conditions
The shelf life of tablets is 2 years from the date of their manufacture. The drug must be stored in the original intact original packaging, dark, dry, out of the reach of children at air temperature not higher than + 30 ° C.