Rosart pills 10 mg №90

Packaging

90 pcs.

Mechanism of action

Rosart is a lipid-lowering agent from the group of statins. Selective competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) - reductase - an enzyme that converts HMG-CoA to mevalonate, a precursor of cholesterol.

Increases the number of low density lipoprotein receptors (LDL) on the surface of hepatocytes, which leads to increased uptake and catabolism of LDL, inhibition of the synthesis of very low density lipoproteins (VLDL), reducing the total number of LDL and VLDL. Reduces high LDL-cholesterol, high density-nelipoproteinov cholesterol (neLPVP), VLDL cholesterol, total cholesterol, triglycerides (TG) TG-VLDL, apolipoprotein B (apoB), reduces the ratio of LDL cholesterol / cholesterol, HDL, total cholesterol / HDL-cholesterol-cholesterol-HDL-cholesterol / HDL-cholesterol, ApoV / Apolipoprotein AI (ApoA-I), increases the concentration of HDL-cholesterol, ApoA-I level.

Lipid-lowering action is directly proportional to the size of the prescribed dose. The therapeutic effect appears within 1 week after the start of therapy, after 2 weeks reaches 90% of the maximum, reaches a maximum by 4 weeks and remains constant after that. Effective in adult patients with hypercholesterolemia with or without hypertriglyceridemia (regardless of race, gender or age), including patients with diabetes and familial hypercholesterolemia. In 80% of patients with hypercholesterolemia IIa and IIb type (Fredrickson classification) with an average baseline LDL cholesterol-level of about 4.8 mmol / l while receiving the drug at a dose of 10 mg, the level of cholesterol-LDL reaches less than 3 mmol / l.In patients with homozygous familial hypercholesterolemia, taking the drug at a dose of 20 mg and 40 mg, the average reduction in LDL cholesterol is 22%.

An additive effect is observed in combination with fenofibrate (in relation to lowering the concentration of triglycerides (TG) and nicotinic acid in lipid-lowering doses (in relation to lowering the concentration of HDL cholesterol).

Indications and usage

• Primary hypercholesterolemia (type IIa according to Fredrickson), including heterozygous hereditary hypercholesterolemia or mixed (combined) hyperlipidemia (type IIb according to Fredrickson), as a supplement to diet and other non-drug measures (exercise and weight loss);
• Homozygous form of hereditary hypercholesterolemia with insufficient efficacy of diet therapy and other types of treatment aimed at reducing the level of lipids (for example, LDL-apheresis) or if such types of treatment are not suitable for the patient.
• Hypertriglyceridemia (type IV by Fredrickson) as a supplement to the diet.
• To slow the progression of atherosclerosis as a supplement to the diet in patients who have been shown therapy to reduce the concentration of total cholesterol and LDL cholesterol.
• Prevention of major cardiovascular complications (stroke, heart attack, 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, elevated concentration C -reactive protein (≥ 2 mg / l) in the presence of at least one of the additional risk factors such as hypertension, low concentration of HDL cholesterol, smoking, a family history of early onset of CHD).

• Hypersensitivity to Rosuvastatin or other components of the drug;
• Liver diseases in the active phase, including a persistent increase in serum activity of “liver” transaminases (more than 3 times compared with the upper limit of normal (VGN)) of unclear genesis;
• Severe renal dysfunction (CC less than 30 ml / min);
• Myopathy;
• Simultaneous administration of cyclosporine;
• Women of reproductive age who do not use adequate methods of contraception;
• Pregnancy and lactation;
• Age up to 18 years (efficacy and safety have not been established);
• Lactose intolerance, lactase deficiency, glucose-galactose malabsorption (the product contains lactose monohydrate).

Carefully:
The presence of risk factors for myopathy and / or rhabdomyolysis - renal failure (QA more than 30 ml / min), hypothyroidism, personal or family history of hereditary muscular diseases and previous history of myotoxicity with the use of other HMG-CoA reductase inhibitors or fibrates; excessive drinking, age over 70 years; conditions in which there is an increase in the plasma concentration of rosuvastatin; race (Mongoloid race), simultaneous use with fibrates, history of liver disease, sepsis, hypotension, extensive surgical intervention, trauma, severe metabolic, endocrine or electrolyte disturbances or uncontrolled epilepsy.

Pregnancy and Breastfeeding

Rosart drug is contraindicated during pregnancy and lactation.

Use of Rosart in women of reproductive age is possible only if reliable contraceptive methods are used and if the patient is informed of the possible risk of treatment for the fetus.

Since cholesterol and substances synthesized from cholesterol are important for fetal development, the potential risk of inhibition of HMG-CoA reductase exceeds the benefits of using the drug during pregnancy. If pregnancy is diagnosed during the course of therapy with Rosart, the drug should be immediately discontinued and patients should be warned of the potential risk to the fetus.

Data on the allocation of rosuvastatin with breast milk are not available, so if you need to use the drug during lactation, given the possibility of adverse events in infants, it is necessary to decide on the termination of breastfeeding.

Dosage and Administration

The drug should be taken orally, without chewing and chopping, swallow whole with water, at any time of the day, regardless of the meal.

Before starting therapy with Rozart, the patient should begin to follow a standard lipid-lowering diet and continue to follow it during treatment.The dose of the drug should be selected individually depending on the indications and therapeutic response, taking into account the current generally accepted recommendations for target lipid levels. The recommended initial dose of Rosart for patients starting the drug or for patients transferred from receiving other HMG-CoA reductase inhibitors is 5 or 10 mg 1 time / day. When choosing the initial dose, one should be guided by the patient’s cholesterol content and take into account the risk of cardiovascular complications, and the potential risk of side effects should be assessed. If necessary, after 4 weeks, the dose may be increased.

Due to the possible development of side effects when taking a dose of 40 mg compared with lower doses of the drug (see the “Side Effects” section), the final titration to the maximum dose of 40 mg should be carried out only in patients with severe hypercholesterolemia and a high risk of cardiovascular disease. vascular complications (especially in patients with hereditary hypercholesterolemia), in whom the target cholesterol level was not reached at the 20 mg dose, and which will be under medical supervision.

Especially careful monitoring of patients receiving the drug at a dose of 40 mg is recommended. After 2-4 weeks of therapy and / or increasing the dose of the drug, control of lipid metabolism indicators is necessary.

In elderly patients dose adjustment is not required.

In patients with hepatic impairment on the Child-Pugh scale below 7 points, dose adjustment is not required. Patients with a score of 8 and 9 on the Child-Pugh scale should have a preliminary assessment of renal function. The experience of using rosuvastatin in patients with hepatic impairment is higher than 9 on the Child-Pugh scale.

In renal failure, mild or moderate dosage adjustment is not required. An initial dose of 5 mg is recommended for patients with moderately severe renal insufficiency (CC less than 60 ml / min). For patients with moderate renal insufficiency (CC less than 30-60 ml / min), the administration of the drug in a dose of 40 mg is contraindicated. Acceptance of Rosart is contraindicated in all doses in patients with severe renal failure (CC less than 30 ml / min).

Ethnic groups
Patients of the Asian race may have increased systemic concentrations of rosuvastatin.When prescribing doses of 10 and 20 mg, the initial recommended dose for Asian patients is 5 mg. The use of the drug in a dose of 40 mg is contraindicated in such patients.

Patients predisposed to the development of myopathy
When prescribing doses of 10 and 20 mg, the initial recommended dose for these patients is 5 mg. The use of the drug in a dose of 40 mg in these patients is contraindicated.

From the side of the central nervous system: often - headache, dizziness, asthenic syndrome; infrequently - depression, anxiety, insomnia, paresthesias; very rarely - peripheral neuropathy, loss of memory.

From the digestive system: often - nausea, constipation, abdominal pain; infrequently - vomiting, diarrhea, flatulence; rarely - pancreatitis; very rarely - hepatitis, jaundice.

On the part of the respiratory system: often - pharyngitis; infrequently - rhinitis, sinusitis, bronchial asthma, bronchitis, cough, dyspnea, pneumonia.

Since the cardiovascular system: infrequently - angina, increased blood pressure, palpitations, vasodilation.

On the part of the endocrine system: often - diabetes mellitus1. (In the JUPITER study, the overall incidence was 2.8% in the rosuvastatin group and 2.3% in the placebo group mainly in patients with fasting glucose 5.6 - 6.9 mmol / l.)

From the musculoskeletal system: often myalgia; rarely, arthralgia; myopathy (including myositis), rhabdomyolysis, back pain, muscle hypertonus, pathological fracture of the limbs; very rarely, immune-mediated necrotizing myopathy.

Allergic reactions: infrequently - pruritus, rash, urticaria; rarely - angioedema.

Skin and subcutaneous tissue: frequency is unknown - Stevens-Johnson syndrome.

From the urinary system: often - proteinuria (mainly in patients receiving a dose of 40 mg), decreasing in the course of therapy and not associated with the occurrence of kidney disease, urinary tract infection; infrequently - peripheral edema, abdominal pain; very rarely - hematuria.

Laboratory values: infrequently - a transient dose-dependent increase in the activity of serum creatine phosphokinase (CPK), with an increase of more than 5 times compared with VGN therapy should be temporarily suspended; rarely, a transient increase in the activity of aspartate aminotransferase and alanine aminotransferase.

Other: often - back pain, rhinopharyngitis; rarely - reduced potency.
As with the use of other inhibitors of HMG-CoA reductase, the frequency of occurrence is dose-dependent in nature, side effects are usually expressed slightly and pass on their own.

During treatment, especially during the dose adjustment period of Rosart, every 2–4 weeks the lipid profile should be monitored and, according to it, the dose of the drug should be changed if necessary.

It is recommended to determine the indicators of liver function before the start of therapy and 3 months after the start of therapy. Taking Rosart should be stopped or reduced in dose if the level of activity of “liver” transaminases in serum is 3 times higher than VGN.

When using the drug ROSART at a dose of 40 mg, it is recommended to monitor indicators of renal function.

In patients with hypercholesterolemia due to hypothyroidism or nephrotic syndrome, treatment of major diseases should be carried out before starting treatment with Rosart.

In patients with existing risk factors for rhabdomyolysis, it is necessary to consider the ratio of the expected benefit to potential risk and conduct clinical observation throughout the course of treatment.

The patient should be informed of the need to immediately report to the doctor about cases of sudden onset of muscle pain, muscle weakness or spasms, especially in combination with indisposition and fever. In such patients, the level of CPK should be determined. Therapy should be discontinued if the level of CPK is significantly increased (more than 5 times compared with VGN) or if the muscle symptoms are pronounced and cause daily discomfort. If the symptoms disappear and the CK level returns to normal, consideration should be given to reappointment of Rosart or other HMG-CoA reductase inhibitors in smaller doses with careful monitoring of the patient.

The definition of CPK should not be carried out after intense physical exertion or if there are other possible causes for an increase in CPK, which can lead to a misinterpretation of the results obtained. If the initial level of CPK is significantly increased, after 5-7 days it is necessary to re-measure - do not start therapy if the repeated test confirms the initial level of CPK (5 times higher than the norm).

Routine monitoring of CPK in the absence of symptoms is not appropriate.

An increase in the incidence of myositis and myopathy was reported in patients taking other HMG-CoA reductase inhibitors in combination with fibrin acid derivatives (including gemfibrozil), cyclosporine, nicotinic acid, azole antifungal drugs, protease inhibitors and macrolide antibiotics. It is necessary to carefully weigh the ratio of the expected benefit and potential risk in the joint use of the drug Rozart and fibrates or niacin, the simultaneous administration of gemfibrozil is not recommended.

In most cases, proteinuria diminishes or disappears during therapy and does not mean the occurrence of acute or exacerbation of an existing kidney disease. Evaluation of renal function should be carried out during routine examination of patients receiving a dose of 40 mg.

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 inhibition of HMG-CoA reductase exceeds the benefits of using the drug during pregnancy. In the event of pregnancy during therapy, the drug should be immediately discontinued. Data on the allocation of rosuvastatin with milk of women are not available, so breastfeeding should be stopped.

Co-administration of rosuvastatin and HIV protease inhibitors is not recommended.

Influence on ability to drive vehicles and mechanisms.
When driving and practicing potentially hazardous activities, patients should take into account that dizziness may occur during therapy.

Treatment: There is no specific treatment, symptomatic therapy is carried out under the control of liver function and CPK activity. Hemodialysis is ineffective.

Does not require special storage conditions. Keep out of the reach of children!