Rosuvastatin pills 10mg №30

Adverse Effects

The classification of the incidence of side effects is as follows: very often (> 1/10); often (from> 1/100 to <1/10); infrequently (from> 1/1000 to <1/100); rarely (from> 1/10 000 to <1/1000); very rarely (from <1/10 000, including individual messages); unspecified frequency (frequency cannot be calculated from available data).

The frequency of side effects depends on the dose of the drug.

From the side of the central nervous system: often - headache, dizziness, asthenic syndrome; very rarely - polyneuropathy, loss of memory.

Gastrointestinal: often - constipation, nausea, abdominal pain; rarely - pancreatitis; very rarely - jaundice, hepatitis; unspecified frequency - diarrhea.

Respiratory: unspecified frequency - cough, shortness of breath.

Musculoskeletal system: often myalgia; rarely, myopathy (including myositis), rhabdomyolysis with or without acute renal failure; very rarely - arthralgia.

Urogenital: proteinuria (less than 1% of cases - for doses of 10 mg and 20 mg, 3% of cases - for a dose of 40 mg); unspecified frequency - peripheral edema; very rarely - hematuria.

On the part of the endocrine system: type 2 diabetes.

Allergic reactions: rarely, hypersensitivity reactions, including angioedema; infrequently - pruritus, rash, urticaria; unspecified frequency - Stevens-Johnson syndrome.

From the laboratory indicators: a transient dose-dependent increase in the activity of CPK (with an increase in the activity of CPK by more than 5 times compared with VGN, therapy should be temporarily suspended); reversible transient dose-dependent increase in liver transaminases; an increase in the concentration of glucose, bilirubin, the activity of GGT, ALP, a change in the concentration of thyroid hormones.

When using some HMG-CoA reductase inhibitors (statins), the following side effects have been reported: depression, sleep disorders, including insomnia and nightmares, sexual dysfunction. It was reported on isolated cases of interstitial lung disease, especially with prolonged use of drugs.

Contraindications

For pills of 10 mg and 20 mg

- liver diseases in the active phase, including a persistent increase in serum transaminase activity and any increase in serum transaminase activity (more than 3 times as compared with VGN);

- severe renal dysfunction (CC less than 30 ml / min);

- myopathy;

- simultaneous use of cyclosporine;

- in women: pregnancy, lactation, lack of adequate methods of contraception;

- to patients predisposed to the development of myotoxic complications;

- children's and teenage age up to 18 years;

- Hypersensitivity to Rosuvastatin or any of the components of the drug.

For 40 mg tablets

- simultaneous administration of cyclosporine;

- in women: pregnancy, lactation, lack of adequate methods of contraception;

- liver diseases in the active phase, including a persistent increase in serum transaminase activity and any increase in serum transaminase activity (more than 3 times as compared with VGN);

- Hypersensitivity to rosuvastatin or any of the components of the drug.

Patients with risk factors for myopathy / rhabdomyolysis, namely:

- renal failure of moderate severity (CC less than 60 ml / min);

- hypothyroidism;

- an indication in personal or family history of muscular diseases;

- myotoxicity against the background of the use of other inhibitors of HMG-CoA reductase or fibrates in history;

- excessive use of alcohol;

- conditions that can lead to an increase in the plasma concentration of rosuvastatin;

- simultaneous use of fibrates;

- patients of the Asian race;

- children's and teenage age up to 18 years.

Carefully

For pills of 10 mg and 20 mg

The risk of myopathy / rhabdomyolysis is renal failure, hypothyroidism, an indication in the family or personal history of hereditary muscular diseases and myotoxicity when using other HMG-CoA reductase inhibitors or fibrates; alcohol addiction; age over 65; conditions in which there is an increase in the plasma concentration of rosuvastatin; race (Asian race - Japanese and Chinese); simultaneous use with fibrates; history of liver disease; sepsis; hypotension; extensive surgical intervention, trauma, severe metabolic, endocrine or electrolyte disturbances, or uncontrolled convulsive seizures.

For 40 mg tablets

Renal failure is easy to degree (CC more than 60 ml / min); age over 65; history of liver disease; sepsis; hypotension; extensive surgical intervention, trauma, severe metabolic, endocrine or electrolyte disturbances, or uncontrolled convulsive seizures.

Patients with liver failure

Data or experience of the drug in patients with a score above 9 on the Child-Pugh scale is absent.

Rosuvastatin 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 inhibition of HMG-CoA reductase exceeds the benefits of using the drug during pregnancy.

If pregnancy is diagnosed during therapy, the drug should be stopped immediately.

Data regarding the allocation of rosuvastatin with breast milk are not available, therefore, during lactation, the drug should be stopped.

Precautions should be prescribed to patients with a history of liver disease.

The use of the drug in patients with liver diseases in the active phase, including a persistent increase in serum transaminase activity and any increase in serum transaminase activity (more than 3 times compared to VGN) is contraindicated.

Data or experience of the drug in patients with a score above 9 on the Child-Pugh scale is absent.

Precautions should be prescribed the drug in a dose of 10 mg and 20 mg in patients with renal insufficiency; at a dose of 40 mg - in patients with mild severity of renal failure (CC more than 60 ml / min).

The use of the drug in a dose of 10 mg and 20 mg in patients with severe impaired renal function (CC less than 30 ml / min) is contraindicated.

The use of the drug at a dose of 40 mg in patients with moderately severe renal failure (CC less than 60 ml / min) is contraindicated.

Use in children

The use of the drug in children and adolescents under the age of 18 years is contraindicated.

With the sameness, the drug should be prescribed to patients older than 65 years.

Prior to the initiation of therapy and throughout the entire period of treatment, the patient should observe a standard lipid-lowering diet. During treatment, a lipid profile should be monitored every 2–4 weeks and according to the results, if necessary, adjust the dose of the drug.

With the use of rosuvastatin in all doses, and especially at a dose in excess of 20 mg, short-term proteinuria can be observed. In patients taking the drug in a dose of 40 mg, it is recommended to monitor indicators of renal function.

In patients taking rosuvastatin in a dose exceeding 20 mg, myalgia, myopathy may occur, rarely rhabdomyolysis. Determination of CPK activity should not be carried out after intense physical exertion or in the presence of other possible reasons for increasing CPK, which may lead to a misinterpretation of the obtained results. With an increase in CPK 5 times higher than WGN after 5-7 days should be repeated measurement. It is not necessary to begin therapy if the repeated test confirms the initial increased activity of CPK more than 5 times in comparison with VGN.

In patients at risk of developing myopathy / rhabdomyolysis, it is necessary to consider the ratio of risk and possible benefit of therapy and to conduct clinical observation throughout the course of treatment.

The patient should be informed of the need to immediately inform the doctor in cases of sudden onset of muscle pain, muscle weakness or spasms, especially when combined with indisposition and fever. In such patients, the activity of CPK should be monitored. Therapy should be discontinued if the activity of CPK is increased by more than 5 times as compared with VGN, or if the muscle symptoms are pronounced and cause daily discomfort (even if the activity of CPK is 5 times less as compared to VGN). If the symptoms disappear and the activity of CPK returns to normal, consideration should be given to the repeated use of the drug or other HMG-CoA reductase inhibitors in smaller doses under close medical supervision. Routine monitoring of CPK in the absence of rhabdomyolysis symptoms is not advisable.

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 in lipid-lowering doses, antifungal drugs from the azole group, HIV protease inhibitors and antibiotics macrolides. Gemfibrozil increases the risk of myopathy when used in combination with some HMG-CoA reductase inhibitors.Thus, the simultaneous use of rosuvastatin and gemfibrozil is not recommended. Care should be taken to weigh the balance between risk and potential benefit when rosuvastatin is used together with fibrate or nicotinic acid in lipid-lowering doses.

It is recommended to carry out the determination of indicators of liver function before the start of therapy and 3 months after the start of therapy. If the activity of hepatic transaminases in serum is 3 times higher than VGN, the dose should be reduced or discontinued.

With a combination of hypercholesterolemia and hypothyroidism or nephrotic syndrome, the treatment of major diseases should be carried out before starting treatment with rosuvastatin.

An increase in the plasma concentration of rosuvastatin was noted in patients of the Asian race as compared with patients of the Caucasian race.

In patients with a blood glucose concentration of 5.6 to 6.9 mmol / l, rosuvastatin therapy was associated with an increased risk of developing type 2 diabetes.

Women of reproductive age should use adequate methods of contraception.

Influence on ability to drive motor transport and control mechanisms

During treatment, dizziness and weakness may occur, so care must be taken when driving and engaging in other potentially hazardous activities that require increased concentration and psychomotor speed.

When several daily doses are taken simultaneously, the pharmacokinetic parameters of rosuvastatin do not change.

Treatment: symptomatic therapy; control of liver function and CPK activity is necessary; there is no specific antidote, hemodialysis is ineffective.

With the simultaneous use of rosuvastatin and cyclosporine, AUC of rosuvastatin is on average 7 times higher than that observed in healthy volunteers. Combined use with rosuvastatin increases C_max in blood plasma 11 times. It does not affect the plasma concentration of cyclosporine.

Initiation of rosuvastatin therapy or an increase in the dose of the drug in patients receiving vitamin K antagonists (for example, warfarin) at the same time can lead to an increase in prothrombin time (INR).Canceling rosuvastatin or reducing the dose of a drug can lead to a decrease in INR (it is recommended to control INR).

The combined use of rosuvastatin and gemfibrozil leads to an increase of 2 times C_max and Rosuvastatin AUC. Based on data on specific interactions, pharmacokinetically significant interactions with fenofibrates are not expected, pharmacodynamic interactions are possible.

Gemfibrozil, fenofibrate, other fibrates and lipid-lowering doses of nicotinic acid (large doses or equivalent 1 g / day) increase the risk of myopathy when used simultaneously with HMG-CoA reductase inhibitors, possibly due to the fact that they can cause myopathy and when used as monotherapy. 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 the drug of 5 mg (1/2 tab. 10 mg).

The simultaneous use of rosuvastatin and ezetimiba was not accompanied by a change in AUC and C_max both drugs.

Despite the fact that the exact mechanism of interaction is unknown, the combined use of HIV protease inhibitors can lead to a significant increase in the exposure of rosuvastatin. A pharmacokinetic study on the simultaneous use of rozuvastatin at a dose of 20 mg with a combination preparation containing two HIV protease inhibitors (400 mg of lopinavir / 100 mg of ritonavir) in healthy volunteers resulted in an approximately twofold and fivefold increase in AUC_(0-24) and C_max Rosuvastatin, respectively. Therefore, the simultaneous use of rosuvastatin and HIV protease inhibitors in the treatment of patients with HIV is not recommended.

The simultaneous use of rosuvastatin and suspensions of 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.

The simultaneous use of rosuvastatin and Erythromycin leads to a decrease in the AUC of rosuvastatin by 20% and C_max by 30%. Such an interaction may occur as a result of increased intestinal motility caused by taking erythromycin.

The simultaneous use of rosuvastatin and oral contraceptives increases the AUC of ethinyl estradiol and AUC of norgestrel by 26% and 34%, respectively. Such an increase in plasma concentration should be taken into account when selecting the dose of oral contraceptives. Pharmacokinetic data on the simultaneous use of rosuvastatin and hormone replacement therapy are not available, therefore, a similar effect cannot be excluded when using this combination.

No clinically significant interaction of rosuvastatin with Digoxin is expected.

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 non-core substrate for these isoenzymes. There was no clinically significant interaction between rosuvastatin and Fluconazole (an inhibitor of CYP2C9 and CYP3A4 isoenzymes) and Ketoconazole (an inhibitor of CYP2A6 and CYP3A4 isoenzymes). The combined use of rosuvastatin and itraconazole (an inhibitor of the isoenzyme CYP3A4) increases the AUC of rosuvastatin by 28% (clinically insignificant). Thus, interactions associated with metabolism through the cytochrome P450 system are not expected.

Pharmacy sales terms

The drug is available on prescription.

Terms and conditions of storage

The drug should be stored out of the reach of children, dry, protected from light, at a temperature not exceeding 25 ° C.