Table of contents:
- Release form and composition
- Pharmacological properties
- Indications for use
- Instructions for the use of Rosart: method and dosage
- Side effects
- special instructions
- Application during pregnancy and lactation
- Pediatric use
- With impaired renal function
- For violations of liver function
- Use in the elderly
- Drug interactions
- Terms and conditions of storage
- Terms of dispensing from pharmacies
- Reviews about Rosart
- The price of Rosart in pharmacies
- Rosart: prices in online pharmacies
Video: Rosart - Instructions For Use, Price, Reviews, Analogs, Tablets 10 Mg
Rosart: 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: Rozart
ATX code: C10AA07
Active ingredient: rosuvastatin (rosuvastatinum)
Manufacturer: Actavis Ltd (Malta)
Description and photo update: 2018-25-10
Prices in pharmacies: from 275 rubles.
Rosart is a lipid-lowering drug.
Release form and composition
Rosart is available in the form of film-coated tablets: biconvex, one side engraved with "ST 1" - on round white tablets, "ST 2" and "ST 3" - on round pink tablets, "ST 4" - on pink oval-shaped tablets (in blisters: 7 pcs., 4 blisters in a cardboard box; 10 pcs., 3 or 9 blisters in a cardboard box; 14 pcs., 2 or 6 blisters in a cardboard box).
1 tablet contains:
- active substance: rosuvastatin calcium - 5.21 mg, 10.42 mg, 20.84 mg or 41.68 mg, this is equivalent to 5 mg, 10 mg, 20 mg or 40 mg of rosuvastatin, respectively;
- auxiliary components: lactose monohydrate, microcrystalline cellulose (type 102), calcium hydrogen phosphate dihydrate, crospovidone (type A), magnesium stearate;
- composition of the film shell: white tablets - white opadry II 33G28435 (titanium dioxide, hypromellose-2910, lactose monohydrate, triacetin, macrogol-3350), pink tablets - pink opadry II 33G240007 (titanium dioxide, hypromellose-2910, lactose monohydrate, triacetin, macrogol-3350, carmine red dye).
Rosart is a drug from the group of statins with lipid-lowering activity. Its active ingredient, rosuvastatin, is a selective competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMG-CoA reductase), an enzyme that converts HMG-CoA into mevalonate, a precursor of cholesterol.
By increasing the number of low density lipoprotein (LDL) receptors on the surface of hepatocytes, rosuvastatin enhances the uptake and catabolism of LDL, inhibition of the synthesis of very low density lipoproteins (VLDL) and a decrease in the total number of LDL and VLDL. It lowers elevated levels of LDL cholesterol, total cholesterol, triglycerides (TG), VLDL cholesterol, VLDL TG, non-HDL (high density lipoprotein) cholesterol, apolipoprotein B (ApoB). Causes an increase in the concentration of HDL cholesterol and ApoA-I. Reduces the ratio of LDL cholesterol to HDL cholesterol, total cholesterol to HDL cholesterol, non-HDL cholesterol to HDL cholesterol, apolipoprotein B (ApoB) to apolipoprotein AI (ApoA-I).
The lipid-lowering effect of Rosart is in direct proportion to the size of the prescribed dose. The therapeutic effect occurs after the first week of therapy, after two weeks it reaches 90% of the maximum effect, and by the fourth week - 100% and remains constant. Rosuvastatin is indicated for the treatment of hypercholesterolemia without / with hypertriglyceridemia, regardless of gender, age or race of the patient, including patients with diabetes mellitus and familial hypercholesterolemia. The research results showed that against the background of taking Rosart at a dose of 10 mg with hypercholesterolemia IIa and IIb type (Fredrickson classification) with an average baseline LDL cholesterol of 4.8 mmol / L, the concentration of LDL cholesterol reaches values less than 3 mmol / l in 80 % of patients. With homozygous familial hypercholesterolemia, the average decrease in LDL cholesterol levels while taking rosuvastatin at a dose of 20 mg and 40 mg is 22%.
An additive effect is noted in the combination of Rosart with nicotinic acid at a dose of 1000 mg or more per day (in relation to an increase in HDL cholesterol) and fenofibrate (in relation to a decrease in the concentration of TG).
After taking the tablet, C max (maximum concentration) of rosuvastatin in blood plasma is reached after about 5 hours. Its systemic exposure increases in proportion to the dose taken. Absolute bioavailability is about 20%. Pharmacokinetic parameters do not change with daily intake.
Plasma protein binding (mostly with albumin) is approximately 90%. The predominant absorption occurs in the liver. V d (volume of distribution) - 134 liters. The drug crosses the placental barrier.
It is a non-core substrate for isozymes of the cytochrome P 450 system. About 10% of rosuvastatin is biotransformed in the liver. The process of uptake of rosuvastatin in the liver occurs with the participation of a specific membrane transporter - a polypeptide that transports the organic anion (OATP) 1B1 and is significantly involved in its hepatic elimination. CYP2C9 isoenzyme is the main isoenzyme of rosuvastatin metabolism, CYP3A4, CYP2C19 and CYP2D6 to a lesser extent.
The main metabolites of rosuvastatin are the pharmacologically inactive lactone metabolites and N-desmethyl, which is approximately 50% less active than rosuvastatin. Inhibition of circulating HMG-CoA reductase is provided by more than 90% of the pharmacological activity of rosuvastatin, the remaining ~ 10% - by the activity of its metabolites.
Approximately 90% of Rosart's dose is excreted unchanged through the intestines, the remainder is excreted through the kidneys. T 1/2 (half-life) - about 19 hours, with an increase in the dose of the drug, it does not change. Plasma clearance averages 50 l / h.
With mild to moderate severity of renal failure, a significant change in the level of concentration of rosuvastatin in blood plasma or N-desmethyl does not occur. With severe renal failure with creatinine clearance (CC) less than 30 ml / min, the content of rosuvastatin in plasma increases 3 times, N-desmethyl - 9 times. In patients on hemodialysis, the plasma concentration of rosuvastatin increases by about 1/2.
At various stages of liver failure (7 points and lower on the Child - Pugh scale), an increase in T 1/2 was not revealed. A twofold lengthening of T 1/2 of rosuvastatin was observed in patients with hepatic insufficiency at 8 and 9 points on the Child-Pugh scale. With more pronounced violations of liver function, there is no experience with the use of the drug.
The sex and age of the patient do not have a clinically significant effect on the pharmacokinetics of rosuvastatin.
Race influences Rosart's pharmacokinetic parameters. AUC (total concentration) of rosuvastatin in blood plasma in Chinese and Japanese is 2 times higher than in Europeans and North America. C max and AUC in Indians and representatives of the Mongoloid race, on average, increases 1.3 times.
Indications for use
- hypertriglyceridemia (type IV according to Fredrickson) - as an addition to the diet;
- primary hypercholesterolemia (Fredrickson type IIa), including heterozygous hereditary hypercholesterolemia, or combined (mixed) hyperlipidemia (Fredrickson type IIb) - as an adjunct to diet, exercise and weight loss;
- a homozygous form of hereditary hypercholesterolemia in the absence of a sufficient effect from diet and other types of therapy aimed at lowering the level of lipid concentration (including LDL apheresis) or in case of individual intolerance to such treatments;
- primary prevention of cardiovascular complications (heart attack, stroke, arterial revascularization) in adults without clinical signs of coronary heart disease (IHD), but with prerequisites for its development (age for men - over 50 years old and for women - over 60 years old, concentration C -reactive protein 2 mg / l and higher in the presence of at least one of the additional risk factors: arterial hypertension, low HDL cholesterol, early onset of coronary heart disease in a family history, smoking).
In addition, Rosart is prescribed as an adjunct to the diet of patients who are indicated for therapy to lower total cholesterol and LDL cholesterol levels in order to slow the progression of atherosclerosis.
- liver disease in the active phase, including a persistent increase in the serum activity of hepatic transaminases [more than 3 times compared with the upper limit of normal (UHN)];
- concomitant use of cyclosporine;
- lactose intolerance, glucose-galactose malabsorption syndrome, lactase deficiency;
- period of pregnancy;
- age up to 18 years;
- hypersensitivity to the components of the drug.
Also, Rosart should not be taken by women of reproductive age who do not use adequate methods of contraception.
In addition, the drug in a daily dose of 5 mg, 10 mg or 20 mg should not be prescribed for severe renal dysfunction (CC less than 30 ml / min).
Additional contraindications for the use of Rosart at a dose of 40 mg per day:
- belonging to the Mongoloid race;
- myotoxicity against the background of the use of inhibitors of HMG-CoA reductase and fibrates in the anamnesis;
- severe and moderate renal failure (CC less than 60 ml / min);
- conditions that can cause an increase in the plasma concentration of rosuvastatin;
- drinking a lot of alcohol;
- simultaneous reception of fibrates;
- a personal or family history of inherited muscle disorders.
Care should be taken when prescribing any dose of Rosart to patients over the age of 70, with arterial hypotension, a history of liver disease, sepsis, trauma, major surgical operations, uncontrolled epilepsy, severe endocrine, metabolic or water-electrolyte disturbances.
In addition, Rosart in a daily dose of 5 mg, 10 mg or 20 mg is used with caution in the presence of risk factors for the development of rhabdomyolysis and / or myopathy [renal failure (CC more than 30 ml / min), hypothyroidism, personal or family history of hereditary muscle diseases, a history of myotoxicity with the use of other inhibitors of HMG-CoA reductase or fibrates], with excessive alcohol consumption, in patients of the Mongoloid race, in combination with fibrates, in conditions accompanied by an increase in the plasma concentration of rosuvastatin.
When prescribing Rosart in a daily dose of 40 mg, additional caution should be exercised in renal failure (CC is more than 60 ml / min).
Instructions for the use of Rosart: method and dosage
Rosart tablets are taken orally, swallowed whole and washed down with water, regardless of food intake or time of day.
The use of the drug is indicated against the background of adherence to the standard lipid-lowering diet.
The doctor selects the dose of the drug individually, taking into account clinical indications, therapeutic response and generally accepted recommendations for target lipid concentrations.
The recommended starting dose of Rosart is 10 mg or 5 mg once a day, including when switching from taking other HMG-CoA reductase inhibitors. The initial dose depends on the concentration of cholesterol, and the potential risk of developing complications from the cardiovascular system and adverse reactions should also be assessed. If necessary to achieve the desired therapeutic effect, the dose may be increased after 4 weeks.
Due to the risk of developing adverse events when taking a dose of 40 mg, titration to the maximum dose (40 mg) is recommended only in patients with severe hypercholesterolemia and a high risk of cardiovascular complications (especially with hereditary hypercholesterolemia), who, when using a daily dose of 20 mg the target concentration of cholesterol was not achieved. Patients should be provided with regular medical supervision. Monitoring of lipid metabolism parameters should be carried out after 2–4 weeks of therapy.
No dose adjustment is required for mild or moderate renal impairment. With an average degree of renal failure (CC less than 60 ml / min) and in patients over 70 years of age, the initial dose of Rosart should be 5 mg.
With liver failure of 7 points and below on the Child-Pugh scale, dose adjustment is not required; at 8 and 9 points on the Child-Pugh scale, it is necessary to first assess renal function.
With a predisposition to the development of myopathy, the initial dose of Rosart should be 5 mg. Due to the risk of increasing the systemic concentration of rosuvastatin for patients of the Mongoloid race, the initial dose should not exceed 5 mg.
Patients with established specific polymorphism are recommended to use lower daily doses when prescribing the drug.
- from the digestive system: often - abdominal pain, constipation, nausea; rarely - pancreatitis; very rarely - jaundice, hepatitis; frequency not established - diarrhea;
- from the lymphatic system and blood: rarely - thrombocytopenia;
- from the musculoskeletal system: often - myalgia; rarely - rhabdomyolysis, myopathy (including myositis); very rarely - arthralgia; frequency not established - necrotizing myopathy (immune-mediated), tendon lesions, tendon rupture;
- from the nervous system: often - asthenic syndrome, headache, dizziness; very rarely - memory loss, polyneuropathy; frequency not established - peripheral neuropathy, sleep disturbances, insomnia, nightmares, depression;
- from the immune system: infrequently - urticaria, pruritus, rash; rarely - hypersensitivity reactions, angioedema;
- from the respiratory system: the frequency has not been established - shortness of breath, cough, interstitial lung disease;
- on the part of the endocrine system: often - diabetes mellitus (depending on the patient's presence of such risk factors as a history of arterial hypertension, fasting blood glucose 5.6 mmol / l and higher, increased concentration of TG);
- dermatological reactions: frequency not established - Stevens-Johnson syndrome;
- on the part of the mammary gland and genitals: very rarely - gynecomastia;
- from the urinary system: very rarely - hematuria;
- laboratory parameters: rarely - a transient increase in the activity of alanine aminotransferase (ALT) and aspartate aminotransferase (AST);
- others: frequency not established - peripheral edema.
The incidence of side effects is dose-dependent. Against the background of the use of rosuvastatin at a dose of 40 mg, the likelihood of developing pronounced renal dysfunction, rhabdomyolysis, and increased activity of liver enzymes increases.
The symptoms of a rosuvastatin overdose have not been established. A single intake of several daily doses of Rosart does not affect pharmacokinetics.
Treatment: the appointment of symptomatic therapy. It is necessary to monitor the activity of creatine phosphokinase (CPK) and the state of the liver. If necessary, measures are taken to maintain the function of vital organs and systems.
The effectiveness of hemodialysis is unlikely.
The risk of developing myopathy, including rhabdomyolysis, increases with concomitant use of rosuvastatin with the following drugs: cyclosporine, HIV protease inhibitors, including combinations of ritonavir with atazanavir, tipranavir and / or lopinavir. Therefore, you should consider the appointment of alternative therapy, and if necessary, the use of these funds, therapy with rosuvastatin should be temporarily stopped.
When using Rosart at a dose of 40 mg, it is necessary to regularly monitor the indicators of renal function.
When determining the activity of CPK, one should exclude the presence of factors that may impair the reliability of the results, including physical activity. Patients with a significant increase in the initial activity of CPK should be re-examined after 5-7 days. In case of confirmation of a five-fold excess of the norm of CPK activity, the use of the drug is contraindicated.
Special care should be taken when prescribing Rosart to patients with risk factors for the development of myopathy or rhabdomyolysis, carefully assessing the ratio of the expected benefit and potential risk from therapy. This category of patients should be provided with clinical observation throughout the course of treatment. You can not start taking pills with an initial CPK activity 5 times higher than the upper limit of the norm.
The doctor should inform the patient about the possible appearance of muscle pain, malaise, fever, muscle weakness or spasms during therapy, and the need to immediately seek advice from a medical facility. With a significant increase in CPK activity or muscle symptoms, therapy should be discontinued. With the disappearance of symptoms and the restoration of the CPK activity indicator, it is possible to re-prescribe the drug in lower doses.
The lipid profile should be monitored 1-2 times a month and the dose of Rosart should be adjusted taking into account its results.
With a history of liver disease and in patients with alcohol abuse, it is recommended to determine the liver function indicators before starting therapy and after three months of using the drug. If the activity of liver enzymes in the blood serum is 3 times higher than the upper limit of the norm, you should reduce the dose or stop taking Rosart.
Since combinations of HIV protease inhibitors with ritonavir cause an increase in the systemic level of rosuvastatin, a decrease in blood lipid concentration should be carefully evaluated, a possible increase in the concentration of rosuvastatin in blood plasma should be taken into account both at the beginning of treatment and during an increase in the dose of the drug, and appropriate dose adjustment should be made.
Cancellation of Rosart is required if an interstitial lung disease is suspected, the manifestation of which may be shortness of breath, unproductive cough, weakness, weight loss, and fever.
Influence on the ability to drive vehicles and complex mechanisms
Due to the possible development of dizziness, care should be taken when performing potentially hazardous activities, including working with complex machinery and driving.
Application during pregnancy and lactation
According to the instructions, Rosart is contraindicated to use during gestation and breastfeeding.
The appointment of the drug to women of reproductive age should be made only when they use reliable contraceptive methods.
The patient should be informed about the potential risk to the fetus in case of conception during the treatment period.
If necessary, taking Rosart during lactation, breastfeeding should be discontinued.
Due to the lack of information on the safety and efficacy of using Rosart, it is contraindicated to prescribe Rosart to children under the age of 18.
With impaired renal function
It is contraindicated to use Rosart in any dose for severe renal failure with CC less than 30 ml / min, at a dose of 40 mg - with CC from 30 to 60 ml / min.
With mild or moderate renal failure, dose adjustment is not required, the initial dose with QC less than 60 ml / min should be 5 mg.
For violations of liver function
Dose changes of rosuvastatin are not required in case of liver failure of 7 points or lower on the Child-Pugh scale, at 8 and 9 points on the Child-Pugh scale, the appointment should be carried out after a preliminary assessment of renal function.
There is no experience with Rosart in liver failure above 9 points on the Child-Pugh scale.
Use in the elderly
It is recommended to prescribe Rosart with caution to patients over 70 years of age.
The initial dose of the drug is 5 mg, no other dose changes are required.
With the simultaneous use of Rosart:
- drugs that inhibit transport proteins, the substrate of which is rosuvastatin, increase the likelihood of developing myopathy;
- cyclosporine causes a significant increase in the effect of rosuvastatin, increasing its maximum concentration in blood plasma by 11 times;
- erythromycin promotes an increase in C max by 30% and a decrease in the AUC of rosuvastatin by 20%;
- warfarin and other indirect anticoagulants can cause fluctuations in MHO (international normalized ratio, which is used to determine the indicator of the blood coagulation system): at the beginning of use and with an increase in the dose of rosuvastatin - an increase in MHO, and when the dose of rosuvastatin is canceled or reduced, a decrease in the INR is recommended, therefore monitoring is recommended MHO indicator;
- lipid-lowering agents, including gemfibrozil, cause a 2-fold increase in AUC and C max of rosuvastatin;
- antacids containing aluminum and magnesium hydroxide, reduce the plasma concentration of the drug by 2 times;
- oral contraceptives increase the AUC of ethinyl estradiol by 26% and norgestrel by 34%;
- fluconazole, ketoconazole and other drugs that are inhibitors of isoenzymes CYP2A6, CYP3A4 and CYP2C9 do not cause clinically significant interactions;
- ezetimibe (at a dose of 10 mg) in patients with hypercholesterolemia increases the AUC of rosuvastatin (at a dose of 10 mg) by 1.2 times, the development of adverse events is possible;
- inhibitors of HIV proteases can lead to a pronounced increase in exposure to rosuvastatin;
- digoxin does not cause clinically significant interactions.
During the period of application of rosuvastatin, you should consult your doctor if it is necessary to combine it with other drugs.
Rosart's analogues are: Akorta, Aktalipid, Vasilip, Lipostat, Mertenil, Medostatin, Zokor, Simvakol, Rosuvastatin, Krestor, Rosukard, Rozistark, Rosulip, Torvazin, Tevastor, Holetar.
Terms and conditions of storage
Keep out of the reach of children.
Store at temperatures up to 30 ° C.
Shelf life is 2 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Rosart
Reviews about Rosart are mostly positive. Patients point to a quick therapeutic effect, emphasizing that cholesterol decreases well with the beginning of the use of tablets, but regular intake of the drug is necessary to keep its values within the normal range.
Some patients warn that there may be side reactions in the form of itching and rash, lowering blood pressure, headaches and abdominal pain. But in general, they note that Rosart gives minimal side effects in comparison with other similar drugs. For many, the cost of the drug is quite high.
The price of Rosart in pharmacies
Price for Rosart depending on the dosage:
- Rosart 5 mg per pack of 30 tablets - from 400 rubles, 90 tablets - from 1009 rubles;
- Rosart 10 mg per pack of 30 tablets - from 569 rubles, 90 tablets - from 1297 rubles;
- Rosart 20 mg per pack of 30 tablets - from 754 rubles, 90 tablets - from 1954 rubles;
- Rosart 40 mg per pack of 30 tablets - from 1038 rubles, 90 tablets - from 2580 rubles.
Rosart: prices in online pharmacies
Rosart 5 mg film-coated tablets 30 pcs.
Rosart 10 mg film-coated tablets 30 pcs.
Rosart tablets p.o. 5mg 30 pcs.
Rosart 20 mg film-coated tablets 30 pcs.
Rosart 40 mg film-coated tablets 30 pcs.
Rosart 5 mg film-coated tablets 90 pcs.
Rosart 10 mg film-coated tablets 90 pcs.
Rosart tablets p.o. 5mg 90 pcs.
Rosart tablets p.p. 40mg 30 pcs.
Rosart 20 mg film-coated tablets 90 pcs.
Rosart tablets p.p. 10mg 90 pcs.
Rosart tablets p.p. 20mg 90 pcs.
Rosart 40 mg film-coated tablets 90 pcs.
Rosart tablets p.p. 40mg 90 Pcs.
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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!