Rosart
Effect on kidney function
In patients receiving high doses of rosuvastatin (mainly 40 mg), tubular proteinuria was observed during urine dipstick analysis, which in most cases was transient. This proteinuria did not indicate acute kidney disease or progression of kidney disease. The incidence of post-marketing reports of serious renal adverse reactions was higher in patients receiving rosuvastatin 40 mg.
When using the drug Rozart at a dose of 40 mg, it is recommended to monitor kidney function indicators during treatment.
Effect on the musculoskeletal system
Myalgia, myopathy and, in rare cases, rhabdomyolysis have been reported with all doses of rosuvastatin, and particularly with doses greater than 20 mg. In very rare cases, rhabdomyolysis has been reported while taking HMG-CoA reductase inhibitors and ezetimibe. In this case, a pharmacodynamic interaction cannot be excluded, so caution should be exercised when taking them together. As with other HMG-CoA reductase inhibitors, the incidence of post-marketing reports of rhabdomyolysis associated with rosuvastatin was higher with the 40 mg dose.
Determination of creatine phosphokinase
Determination of CPK activity should not be carried out after intense physical activity or in the presence of other possible reasons for an increase in its activity, which may lead to incorrect interpretation of the results obtained. If the initial CPK activity is significantly increased, a repeat measurement should be taken after 5-7 days; therapy should not be started if a repeat test confirms the initial CPK activity (5 times higher than normal).
Before starting therapy
Caution should be exercised when prescribing Rozart, as well as when prescribing other HMG-CoA reductase inhibitors, to patients with existing risk factors for the development of myopathy/rhabdomyolysis (see section Caution).
It is necessary to consider the balance between the expected benefit of therapy and the potential risk and conduct clinical monitoring throughout the course of treatment. If the initial activity of CPK is significantly increased (5 times higher than the ULN), then treatment with the drug should not be started.
During treatment
The patient should be informed to immediately report to the doctor the unexpected onset of muscle pain, muscle weakness or cramps, especially in combination with malaise and fever. In such patients, CPK activity should be determined. Therapy should be discontinued if CPK activity is significantly increased (more than 5 times the ULN) or if muscle symptoms are severe and cause daily discomfort (even if CPK activity is 5 times less than the ULN). If symptoms disappear and CPK activity returns to normal, re-prescribing Rozart or other HMG-CoA reductase inhibitors in lower doses should be considered with careful monitoring of the patient. Routine monitoring of CPK activity in the absence of symptoms is impractical. Very rare cases of immune-mediated necrotizing myopathy have been reported with clinical manifestations of persistent proximal muscle weakness and increased serum CPK activity during treatment or discontinuation of statins, including rosuvastatin. There were no signs of increased effects on skeletal muscles when taking rosuvastatin and concomitant therapy. However, an increase in the number of cases of myositis and myopathy has been reported in patients taking other HMG-CoA reductase inhibitors in combination with fibric acid derivatives (including gemfibrozil), cyclosporine, nicotinic acid in lipid-lowering doses > 1 g / day, azole antifungals, inhibitors proteases and macrolide antibiotics. Gemfibrozil increases the risk of developing myopathy when taken concomitantly with certain HMG-CoA reductase inhibitors, therefore the simultaneous use of gemfibrozil and rosuvastatin is not recommended. The ratio of expected benefits and potential risks should be carefully weighed when using the drug Rozart together with fibrates or nicotinic acid in lipid-lowering doses > 1 g / day. Taking the drug Rozart at a dose of 40 mg simultaneously with fibrates is contraindicated (see sections Interaction with other drugs and Contraindications
). During treatment, especially during the period of dose adjustment of the drug Rozart, the lipid profile should be monitored every 2-4 weeks and, according to it, the dose of the drug should be changed if necessary. Rosart should not be taken by patients with acute and severe symptoms of myopathy or with risk factors predisposing to the development of renal dysfunction and secondary rhabdomyolysis (for example, sepsis, arterial hypotension, major surgical interventions, trauma, severe metabolic disorders, severe endocrine disorders and severe disturbances in water and electrolyte balance, uncontrolled seizures).
Effect on liver function
Like other HMG-CoA reductase inhibitors, rosuvastatin should be used with caution in patients who abuse alcohol and/or have a history of liver disease. It is recommended to determine liver function indicators before starting therapy and 3 months after starting therapy. Taking Rozart should be stopped or the dose reduced if the level of hepatic transaminase activity in the blood serum is 3 times higher than the ULN. In patients with hypercholesterolemia due to hypothyroidism or nephrotic syndrome, treatment of underlying diseases should be carried out before starting treatment with Rozart. During post-marketing surveillance of rosuvastatin, the frequency of reports of the development of serious liver dysfunction (expressed mainly in increased activity of hepatic transaminases) was higher when taking a dose of 40 mg.
Ethnic groups
During pharmacokinetic studies among patients of the Mongoloid race compared with Caucasians, an increase in the systemic concentration of rosuvastatin was noted (see section Dosage and Administration and Pharmacokinetics
).
HIV protease inhibitors
During co-administration of rosuvastatin and a combination of various HIV protease inhibitors with ritonavir, an increase in the systemic concentration of rosuvastatin is observed. The decrease in blood lipid concentrations should be carefully assessed, and the possible increase in rosuvastatin in the blood plasma should also be taken into account at the beginning of treatment and during the period of increasing the dose of the drug Rozart in patients with HIV taking HIV protease inhibitors. Concomitant use of HIV protease inhibitors is not recommended without dosage adjustment of rosuvastatin (see Dosage and Administration and Interactions with other medicinal products
).
Interstitial lung disease
Isolated cases of interstitial lung disease have been reported with the use of certain HMG-CoA reductase inhibitors, especially over long periods of time. Manifestations of the disease may include shortness of breath, non-productive cough and deterioration in general health (weakness, weight loss and fever). If interstitial lung disease is suspected, therapy with HMG-CoA reductase inhibitors should be discontinued.
Diabetes mellitus type II
Some evidence suggests that HMG-CoA reductase inhibitors increase blood glucose concentrations and increase the likelihood of developing type 2 diabetes in some patients. However, this risk is outweighed by the ability of HMG-CoA reductase inhibitors to reduce the risk of vascular complications, so this fact is not a reason to interrupt treatment with rosuvastatin. It is necessary to establish clinical observation and conduct a biochemical blood test according to national standards in patients at risk of developing hyperglycemia (blood glucose concentration 5.6-6.9 mmol/l, body mass index > 30 kg/m2, triglyceridemia, arterial hypertension). One study of rosuvastatin reported an overall incidence of diabetes mellitus of 2.8% in the rosuvastatin group and 2.3% in the placebo group, primarily in patients with fasting glucose 5.6 to 6.9 mmol/L.
Lactose intolerance
The drug Rozart should not be taken by patients with lactose intolerance, lactase deficiency and glucose-galactose malabsorption, since it contains lactose monohydrate.
Mechanism of action
The active substance selectively and competitively inhibits 3-hydroxy-3-methylglutaryl-coenzyme A reductase, an enzyme involved in the synthesis of cholesterol precursor. Rosart tablets act in the liver, increasing the number of LDL receptors in its cells and suppressing the formation of VLDL. Low and very low density lipoproteins (LDL and VLDL, respectively) are the main atherogenic fractions of blood lipids. Their increase significantly increases the risk of developing atherosclerosis and its complications from the cardiovascular system.
Under the influence of rosuvastatin, the content of HDL in the body increases - high-density lipoproteins, which have anti-atherogenic properties and transfer excess “bad” cholesterol back to the liver for their further elimination.
The maximum concentration of the active substance in the body is determined 5 hours after taking the medicine orally. Metabolites of the drug are excreted from the body in feces and urine. The pharmacokinetic properties of the drug do not change with repeated administration.
In Mongoloid patients, the bioavailability and maximum concentration of statins is doubled compared to European patients, and in Indians - by 1.3 times.
Features of application and interaction
Creatine kinase levels should be monitored during statin therapy. If its level is increased more than 5 times, use of the medicine should be discontinued. In patients taking rosuvastatin in maximum dosages, the condition of the kidneys and liver should be regularly monitored. If you are at high risk of developing diabetes, your blood glucose levels should be monitored.
Cyclosporine, protease inhibitors, gemfibrozil, ezetimibe increase the bioavailability of rosuvastatin. The simultaneous use of these drugs is prohibited. Antacids and erythromycin reduce the bioavailability and maximum concentration of the drug Rozart.
Note!
The description of the drug Rozart on this page is a simplified author’s version of the apteka911 website, created on the basis of the instructions for use.
Before purchasing or using the drug, you should consult your doctor and read the manufacturer's original instructions (attached to each package of the drug). Information about the drug is provided for informational purposes only and should not be used as a guide to self-medication. Only a doctor can decide to prescribe the drug, as well as determine the dose and methods of its use.
Dosage regimen
Therapy begins with a lipid-lowering diet. It is observed throughout the entire therapy. Doses of the medication are selected individually in accordance with the instructions, the purpose of treatment and concomitant diseases.
Rosart is taken without connection with food. A clinically significant effect occurs 7 days after starting to take the medicine, the maximum effect occurs by the end of the first month.
Treatment of hypercholesterolemia begins with the appointment of Rozart 10 or 5 mg/day orally, regardless of whether the patient has previously received statins. The product is used once in the morning, afternoon or evening.
If it is necessary to increase the therapeutic dose, this can be done no earlier than 28 days from the start of treatment. It is permissible to increase the dose to 40 mg of rosuvastatin only in case of extremely severe pathology and when low dosages have not brought any effect. The maximum dose (40 mg) causes the development of adverse reactions more often than medium and low doses. The dose can be increased only as prescribed by the attending physician and under his supervision.
With a high total cardiovascular risk, Rozart is taken 20 mg per day.
People over 70 years of age are prescribed Rozart at a dosage of 5 mg. The same dose is the starting daily dose for patients of the Mongoloid race, and the maximum dosage (40 mg) is prohibited in these cases. The same applies to people with a tendency to myopathies and rhabdomyolysis.
Children
Only a doctor can prescribe Rosart to a child. The drug is used in children over 10 years of age (boys at a stage of development above Tanner II and girls who have menstruated for less than a year). The starting dose of the drug is 5 mg/day, the therapeutic dose usually does not exceed 20 mg/day. Dose limits do not apply to children.
Treatment begins with diet. Increasing the dose is possible no earlier than 28 days from the start of treatment.
Indications for use
Primary hypercholesterolemia (including familial heterozygous) or mixed dyslipidemia. The drug is used as part of a general treatment regimen when nonspecific methods of combating hyperlipidemia (diet and exercise) are not enough to achieve a clinical effect.
Rosuvastatin is also used in patients with homozygous familial hypercholesterolemia in cases where diet or extracorporeal blood lipid purification procedures are ineffective.
The attending physician may prescribe Rosart to patients with an increased total cardiovascular risk. You can buy it as one of the means of correcting the condition.
Contraindications
The drug should not be used in patients with the following conditions:
- hypersensitivity to the active or auxiliary components of the drug;
- liver pathology and increased liver tests (including idiopathic) when they increase 3 times compared to the norm;
- severe renal failure with creatinine clearance <30 ml/min;
- muscle pathology;
- lactose intolerance and lactase deficiency;
- period of pregnancy and breastfeeding;
- age up to 10 years;
- concomitant treatment with cyclosporine.
Rosuvastatin should also not be taken by women of reproductive age unless they are protected from pregnancy by reliable methods. If pregnancy occurs during treatment, statins should be stopped immediately. It is recommended to avoid breastfeeding during drug therapy.
Patients with a tendency to muscle pathology and myolysis are prohibited from taking the drug at a dosage of 40 mg. Risk factors that increase the likelihood of developing myopathy/rhabdomyolysis include:
- moderate renal failure;
- hypofunction of the thyroid gland;
- history of muscle pathology (including family);
- history of myotoxicity reactions caused by statins or fibrates;
- addiction to alcohol;
- belonging to the Mongoloid race;
- concomitant treatment with fibrates;
- the presence of conditions that can increase the content of the active substance in the blood.
The use of rosuvastatin at a dosage of 40 mg is also prohibited for patients of the Mongoloid race.
Popular questions about Rosart
What does Roseart treat?
Roseart is used to treat hypercholesterolemia and other dyslipidemias.
How much to drink Roseart?
The duration of treatment is determined by the doctor. The timing of therapy depends on its purpose and effectiveness. The first clinically significant effect from the use of Rozart and its analogues occurs after a week of use, the maximum - after a month.
What is Roseart for?
Rozart is used to reduce the content of atherogenic lipid fractions (LDL and VLDL) in the blood.
How much does rosuvastatin cost?
The current cost of the drug Rozart can be found on the pharmacy 911 website.
