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Active ingredients
Rosuvastatin
Release form
Pills
Composition
Active ingredient: Rosuvastatin Concentration of active ingredient (mg): 10 mg
Pharmacological effect
Lipid-lowering, inhibiting gmg-coa-reductase
Indications
Roxer medication is successfully used for hyperlipidemia (type A second), mixed dyslipidemia, familial homozygous hypercholesterolemia and for hypertriglyceridemia in combination with a special diet. For patients with cholesterol plaques, the drug is prescribed to slow the further development of the disease. .
Contraindications
Roxer's medication is strictly forbidden to use for the treatment of patients with allergies to its components, liver diseases during an exacerbation, persistent increase in liver transaminases, severe kidney disorders (with a glomerular filtration rate of less than 30 ml / min), myopathy. The drug is contraindicated for pediatrics When treating women of childbearing age with medication, one should take care of a reliable method of contraception. Treatment with Roxer's pharmaceutical preparation is contraindicated in tsiklosporinom.Naznachenie Roxer than 30 mg / day. contraindicated in hypothyroidism, alcoholism, treatment with fibrates, lactase deficiency, sepsis, hypotension, people over 65 years of age and patients of Mongoloid race.
Precautionary measures
Keep out of the reach of children.
Use during pregnancy and lactation
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 for the fetus exceeds the benefits of using the drug during pregnancy In case of pregnancy in the course of therapy, the use of the drug should be immediately discontinued. There is no data on the release of rosuvastatin with breast milk (iz It is clear that other HMG-CoA reductase inhibitors can be excreted in breast milk), so the use of the drug should be discontinued during breastfeeding.
Dosage and administration
The drug is prescribed strictly according to the results of laboratory blood tests. The recommended initial dose is 5 mg / day. It is necessary to revise the dosage and make the correction no earlier than one month after the application of the minimum dose. The maximum daily dose of Roxer is no more than 40 mg (in case of mild to moderate renal insufficiency - no more than 30 mg / day, and with a predisposition to myotoxic complications 20 mg / day., With simultaneous treatment with hemifibrazil - no more than 10 mg / day.) Roxer's dosage peculiarity is the use of an agent for treating patients of a Mongoloid race (Chinese, Japanese, Mongols, etc.). Clinical studies have shown an increased degree of absorption of the drug, so the dosage of 40 mg / day is strictly contraindicated for them. Tablets should be taken orally, regardless of the time of day, without chewing, washed down with water.
Side effects
Roxer's drug treatment is often accompanied by headache, dizziness, nausea, vomiting, constipation, muscle aches, the presence of protein in the urine, asthenia. Rarely, treatment is accompanied by increased susceptibility to allergens, polyneuropathy, pancreatitis, increased liver transaminases, allergic manifestations (pruritus, rash, urticaria), myopathy and rhabdomyolysis. erythema, joint pain, hematuria.
Overdose
Cases of overdose are not registered.
Interaction with other drugs
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”). Cyclosporin. With the simultaneous use of rosuvastatin and cyclosporine, Rosuvastatin AUC is on average 7 times higher than the value observed in healthy volunteers (see Table 1). Simultaneous use with rosuvastatin does not affect the concentration of cyclosporine in the blood plasma.Rosuvastatin is contraindicated in patients taking cyclosporine (see "Contraindications"). HIV protease inhibitors. The simultaneous use of HIV protease inhibitors can 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 AUC (0-24) and Cmax of rosuvastatin in 2 and 5 times respectively. Therefore, simultaneous administration 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 an increase in Cmax and AUC of rosuvastatin in plasma in 2 times (see. "Special instructions"). Based on data on specific interactions, pharmacokinetically significant interactions with fenofibrate are not expected; pharmacodynamic interactions are possible. Gemfibrozil, fenofibrate, other fibrates and lipid-lowering doses of nicotinic acid (doses large or equivalent to 1 g / day) increased the risk of myopathy with simultaneous use 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). The pharmacodynamic interaction between rosuvastatin and ezetimibe, which is manifested by an increased risk of adverse reactions, cannot be ruled out. Antacids. The simultaneous use of rosuvastatin and antacids containing aluminum and magnesium hydroxide, reduces the plasma concentration of rosuvastatin by about 50%. This effect is less pronounced if antacids are applied 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 AUC (0 – t) of rosuvastatin by 20% and its Cmax by 30%. Such an interaction may occur as a result of increased intestinal motility caused by the use of erythromycin. The cytochrome P450 enzyme.The results of in vivo and in vitro studies have shown that rosuvastatin is neither an inhibitor nor an inducer of cytochrome P450 isoenzymes. In addition, rosuvastatin is a weak substrate for this system of isoenzymes. Therefore, the interaction of rosuvastatin with other drugs at the metabolic level with the participation of cytochrome P450 isoenzymes is not expected. The clinically significant interaction between rosuvastatin, fluconazole (an inhibitor of isoenzymes CYP2C9 and CYP3A4) and ketoconazole (an inhibitor of isoenzymes CYP2C9 and CYP3A4) and a radionuclide (CYP2A6 and CYP3A4 isoenzymes) and a ketoconazole (CYP2A6 isoenzymes inhibitor) and a CYP3A4 inhibitor, did not notice that a non-interaction of cytochrome P450 Research on the interaction of rosuvastatin and fusidic acid was not conducted. As with other statins, post-marketing reports of cases of rhabdomyolysis with rosuvastatin and fusidic acid were obtained. It is necessary to closely monitor patients. If necessary, it is possible to temporarily stop taking rosuvastatin. Interaction with drugs, which requires dose adjustment of rosuvastatin (see Table 1) The dose of Roxer should be adjusted if necessary to use it simultaneously with drugs that increase the exposure of rosuvastatin. If exposure is expected to increase by 2 times or more, the initial dose of rosuvastatin should be 5 mg 1 time per day. Also, the maximum daily dose of rosuvastatin should be adjusted so that the expected exposure of rosuvastatin does not exceed that for a dose of 40 mg taken without co-administration of drugs that interact with Rosuvastatin. For example, the maximum daily dose of rosuvastatin with simultaneous use with gemfibrozil is 20 mg (1.9 times increase in exposure), with ritonavir / atazanavir - 10 mg (3.1 times increase in exposure). Effect of the use of rosuvastatin on other drugs Vitamin K antagonists. How and in the case of other HMG-CoA reductase inhibitors, the initiation of rosuvastatin therapy or an increase in its dose in patients taking vitamin K antagonists at the same time (for example, warfarin) may lead to an increase in MHO. Canceling rosuvastatin or reducing its dose may lead to a decrease in MHO. In such cases, monitoring of MHO is recommended. Contraceptives for oral / 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.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 HRT are absent, 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. Clinically significant interaction of rosuvastatin with digoxin is not expected.special instructions
Impaired renal function. In patients who received high doses of rosuvastatin (in particular 40 mg / day), tubular proteinuria was observed, which was detected using test strips and in most cases was periodic or short-term. This proteinuria does not indicate an acute illness or progression of concomitant kidney disease. The frequency of serious impairment of kidney function, noted in the post-marketing study of rosuvastatin, is higher with a dose of 40 mg / day. In patients taking Roxer’s drug in a dose of 30 or 40 mg / day, it is recommended to monitor renal function indicators during treatment (at least once every 3 months). Effect on the musculoskeletal system. When rosuvastatin was used in all doses, but especially in doses exceeding 20 mg / day, the following effects on the musculoskeletal system were reported: myalgia, myopathy, in rare cases rhabdomyolysis. Very rare cases of rhabdomyolysis with simultaneous use of HMG-CoA reductase inhibitors and ezetimiba have been noted. This combination should be used with caution, since pharmacodynamic interactions cannot be excluded. As in the case of other HMG-CoA reductase inhibitors, the frequency of rhabdomyolysis with postmarketing use of the drug Roxer is higher with a dose of 40 mg / day. Determination of CPK activity. The activity of CPK cannot be determined after intense physical exertion and in the presence of other possible reasons for the increase in its activity; This may lead to misinterpretation of the results. If the initial activity of CPK is significantly exceeded (5 times higher than VGN), after 5-7 days, a repeated analysis should be carried out.Do not start therapy if the results of re-analysis confirm the initial high activity of CPK (more than 5-fold excess of VGN). Before starting therapy, depending on the daily dose, Roxera should be administered with caution to patients with myopathy / rhabdomyolysis risk factors or use of the drug is contraindicated (see "Contraindications" and "With caution"). These factors include: - renal dysfunction; - hypothyroidism; - muscle diseases in history (including family); - myotoxic effects taking other HMG-CoA reductase inhibitors or a history of fibrates; - excessive alcohol consumption; - age over 65 years; - conditions in which plasma concentrations of rosuvastatin may increase; - simultaneous use of fibrates. In such patients, it is necessary to evaluate the risk and possible benefit of therapy. Clinical monitoring is also recommended. If the initial activity of CPK is more than 5 times higher than that of VGN, Roxer's drug therapy cannot be started. During the drug therapy period, the patient should be informed about the need to immediately consult a doctor if muscle pain, muscle weakness or spasms occur unexpectedly, especially in combination with malaise and fever. In such patients, the activity of CPK should be determined. Therapy should be discontinued if the activity of CPK is significantly increased (more than 5 times compared with VGN) or if the symptoms of the muscles are pronounced and cause daily discomfort (even if the activity of KFK is not more than 5 times higher than VGN). If the symptoms disappear and the activity of CPK returns to normal, consideration should be given to resuming the use of Roxer or other HMG-CoA reductase inhibitors in smaller doses with careful medical observation. Control of CPK activity in the absence of symptoms is impractical. Very rare cases of immune-mediated necrotizing myopathy with clinical manifestations in the form of persistent proximal muscle weakness and increased serum CPK activity during therapy or when discontinuing the use of HMG-CoA reductase inhibitors are noted, including Rosuvastatin. Additional studies of the muscular and nervous systems, serological studies, and therapy with immunosuppressive agents may be required. There are no signs of an increase in the effect on skeletal muscles when taking rosuvastatin and concomitant therapy.However, an increase in the incidence of myositis and myopathy was reported in patients taking other HMG-CoA reductase inhibitors in combination with fibric acid derivatives (for example gemfibrozil), cyclosporine, nicotinic acid in lipid-lowering doses (more than 1 g / day), antifungal agents 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. The advantages of further changes in plasma lipid concentrations with the combined use of Roxer's drug with fibrates or nicotinic acid in lipid-lowering doses should be carefully weighed, taking into account the possible risk. The drug Roxer at a dose of 30 mg / day 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 can lead to myopathy or conditions that predispose to the development of renal failure (for example, sepsis, arterial hypotension , extensive surgery, trauma, severe metabolic, endocrine and electrolyte disturbances or uncontrolled seizures). Liver. Depending on the daily dose, Roxera should be used with caution in patients with excessive alcohol consumption and / or having a history of liver disease or its use is contraindicated (see "Contraindications" and "With caution"). It is recommended to carry out the determination of functional liver samples before the start of therapy and 3 months after its start. Use of Roxer should stop or reduce the dose of the drug, if the activity of hepatic transaminases in serum is 3 times higher than VGN.Patients with hypercholesterolemia due to hypothyroidism or nephrotic syndrome should be treated before basic treatment with Roxer. Ethnic features. In the course of pharmacokinetic studies, an increase in plasma concentration of rosuvastatin was observed in representatives of the Mongoloid race as compared with representatives of the Caucasian race. Roxer's preparation contains lactose, and therefore it should not be used in patients with lactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome. .With the use of some HMG-CoA reductase inhibitors, especially for a long time, isolated cases of interstitial lung disease have been reported. Manifestations of the disease can be shortness of breath, unproductive cough and worsening of general well-being (weakness, weight loss and fever). If interstitial lung disease is suspected, treatment with HMG-CoA reductase inhibitors should be discontinued. Type 2 diabetes mellitus on the ability to drive a car or perform work that require increased speed of physical and mental reactions. Studies on the effect of the drug Roxera on the ability to drive and work with the mechanisms were not conducted. Nevertheless, given the possibility of dizziness and other side effects, care must be taken when driving vehicles and other mechanisms that require increased concentration and psychomotor speed.