Rosucard 20mg pills №90

Release form

Film Coated Tablets

Composition

Each pill film coated contains:
active substance:
Rosuvastatin - 20,000 mg;
Excipients:
core: lactose monohydrate - 240,000 mg, microcrystalline cellulose - 181,600 mg, croscarmellose sodium - 4,800 mg, colloidal silicon dioxide - 2,400 mg, Magnesium stearate - 9,600 mg;
film cover: hypromellose 2910/5 - 10,000 mg, macrogol 6000 - 1,600 mg, titanium dioxide - 1,300 mg, talc - 1,900 mg, iron dye red oxide - 0.200 mg.

Packaging

90 pcs.

pharmachologic effect

Rosucard is a lipid-lowering agent from the group of statins. Selective competitive inhibitor of Z-hydroxy-Z-methylglutaryl coenzyme A (HMG-CoA) -reductase - an enzyme that converts HMG-CoA to mevalonate, a precursor of cholesterol (CH).
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 concentration of LDL and VLDL. Decreases concentrations of cholesterol-cholesterol-cholesterol-cholesterol, high-density non-lipoprotein cholesterol (cholesterol-LDLP), cholesterol cholesterol, total cholesterol cholesterol, total cholesterol cholesterol, triglycerides (TG), cholesterol cholesterol, apolipoprotein B (ApoV), lowers cholesterol-LDL / cholesterol-LDL-cholesterol, apolipoprotein B (ApoV) Cholesterol / cholesterol-HDL, cholesterol-HDL-cholesterol / cholesterol-HDL, apoB / apolipoprotein A-1 (apoA-I), increases the concentration of cholesterol-HDL and apoA-I.
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 initial concentration of LDL-C of about 4.8 mmol / l while receiving the drug at a dose of 10 mg, the concentration of LDL-C makes up 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 decrease in the concentration of LDL-C is 22%.
The additive effect is observed in combination with fenofibrate (in relation to reducing the concentration of TG and with nicotinic acid in lipid-lowering doses (at least 1 g / day) (in relation to reducing the concentration of HDL-C).

Indications

• Primary hypercholesterolemia (type IIa according to Fredrickson), including heterozygous hereditary hypercholesterolemia or mixed (combined) hypercholesterolemia (type II according to Fredrickson), as a supplement to diet and other non-drug measures (exercise and weight loss) while not using a healthy diet.
• Homozygous form of hereditary hypercholesterolemia and with insufficient effectiveness of diet therapy and other types of treatment aimed at reducing the level of lipids (for example, LDL apheresis),or if such treatments 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 cholesterol - LDL.
• 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 concentrations of HDL-C, smoking, family history of early onset of CHD).

Contraindications

• Presence of the following risk factors for myopathy / rhabdomyolysis:
  1. Myotoxicity while taking other HMG-CoA reductase inhibitors or a history of fibrates;
  2. Hypothyroidism;
  3. Renal failure of moderate severity (CC 30 - 60 ml / min);
  4. Excessive alcohol consumption;
  5. States that can lead to an increase in the plasma concentration of rosuvastatin;
  6. Simultaneous intake of fibrates;
• Patients of the Mongoloid race;
• Family history of muscular diseases.

Use during pregnancy and lactation

The use of the drug Rosukard in women of reproductive age is possible only in the case of using reliable methods of contraception and if the patient is informed about 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. Rosucardum is contraindicated during pregnancy and lactation. If pregnancy is diagnosed during the course of drug therapy, Rosukard should be discontinued immediately and the patient warned of the potential risk to the fetus.
If necessary, the use of the drug during lactation, given the possibility of adverse events in infants, should decide on the termination of breastfeeding.

Dosage and administration

Inside, without chewing and chopping, swallow whole with water, at any time of the day, regardless of the meal.
Before starting therapy with roscard, 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. If necessary, taking the drug in a dose of 5 mg should be divided into a pill of 10 mg into two parts according to the risk.
The recommended initial dose of Rosucard for patients starting the drug or for patients transferred from taking other HMG-CoA reductase inhibitors is 5 or 10 mg 1 time per 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, final titration to the maximum dose of 40 mg should be carried out only in patients with severe hypercholesterolemia and high risk of cardiovascular complications (especially in patients with hereditary hypercholesterolemia) in which the target level of cholesterol was not reached when taking a dose of 20 mg, and which will be under medical supervision.
Patients with liver failure
In patients with hepatic insufficiency with Child-Pugh scores of less than 7, no dose adjustment is required for Rosucardia.
Patients with renal failure
In patients with renal failure, mild dose adjustment is not required. An initial dose of roscarda is recommended - 5 mg per day.
In patients with severe renal insufficiency (CC less than 30 ml / min), use of roscardum is contraindicated.
In patients with moderately severe renal failure (CK 30–60 ml / min), the use of roscard at a dose of 40 mg per day is contraindicated.
Special populations. Elderly patients
Patients over 65 years of age do not require dose adjustment.
Patients with a predisposition to myopathy
The use of Rosucard at a dose of 40 mg per day is contraindicated in patients with a predisposition to myopathy. When prescribing doses of 10 mg and 20 mg per day, the recommended initial dose of roscard for this group of patients is 5 mg per day.
Ethnic groups
In the study of the pharmacokinetic parameters of rosuvastatin, an increase in the systemic concentration of the drug among representatives of the Mongoloid race was noted. This fact should be taken into account in the appointment of Rosukard to patients of the Mongoloid race. When prescribing doses of 10 and 20 mg, the recommended initial dose of roscard for this group of patients is 5 mg per day. The use of roscard in a dose of 40 mg per day is not recommended for representatives of the Mongoloid race.

When prescribing rosucard with gemfibrozil, the dose should not exceed 10 mg per day.

Side effects

The frequency of adverse reactions was determined according to the following gradation (classification of the World Health Organization):

• very often - more than 1/10,
• often from more than 1/100 to less than 1/10,
• infrequently - from more than 1/1000 to less than 1/100,
• rarely from more than 1/10000 to less than 1/1000,
• very seldom - from less than 1/10000, including individual messages.
• not specified frequency.

From the side of the central nervous system: often - headache, dizziness, asthenic syndrome; very rarely - peripheral neuropathy, loss of memory.
From the digestive system: often - nausea, constipation, abdominal pain; infrequently - vomiting; rarely - pancreatitis; very rarely - hepatitis, jaundice; unspecified frequency - diarrhea.
On the part of the respiratory system: infrequently - cough, dyspnea.
On the part of the endocrine system: often - type 2 diabetes.
From the musculoskeletal system: often myalgia; very rarely - arthralgia; rarely - myopathy (including myositis), rhabdomyolysis.
Allergic reactions: infrequently - pruritus, urticaria, rash; rarely - angioedema.
Skin and subcutaneous tissue: unspecified frequency - Stevens-Johnson syndrome, peripheral edema.
From the urinary system: often - proteinuria (with a frequency of more than 3% 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; 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 the upper limit of the norm, therapy should be temporarily suspended; rarely, a transient increase in the activity of aspartate aminotransferase and alanine aminotransferase.
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.
When using Rozukard, changes in the following laboratory parameters were noted: increase in the concentration of glucose, bilirubin, alkaline phosphatase activity, gamma-glutamyltransferase.
When using other statins, the following side effects were reported: depression, insomnia, decreased potency.
With prolonged use of rosuvastatin, isolated cases of interstitial lung disease have been reported.

Drug interaction

The simultaneous use of rosuvastatin and cyclosporine does not affect the plasma concentration of cyclosporin, but the effect of rosuvastatin is enhanced (its excretion is slowed down, the AUC increases 7 times, C_max - 11 times).
Erythromycin increases intestinal motility, which leads to a decrease in the effect of rosuvastatin (AUC decreases by 20% and C_max by 30%).
In patients receiving vitamin K antagonists (for example, warfarin), monitoring of the international normalized ratio (INR) is recommended, since initiating rosuvastatin therapy or increasing the dose of the drug can lead to an increase in INO, and withdrawal of rosuvastatin can reduce it. Gemfibrozil enhances the effect of rosuvastatin (increases C_max and AUC 2 times). 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 simultaneous use of rosuvastatin and oral contraceptives increases the AUC of ethinyl estradiol and AUC of norgestrel by 26% and 34%, respectively, which should be considered 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.
Studies have shown that rosuvastatin is neither an inhibitor nor an inducer of the action of cytochrome P450 isoenzymes. Rosuvastatin is a non-core substrate for these isoenzymes. There was no clinically significant interaction with drugs such as Fluconazole , Ketoconazole and itraconazole, associated with the metabolism of the cytochrome P450 system.
No clinically significant interaction of rosuvastatin with Digoxin or fenofibrate, Gemfibrozil, other fibrates and lipid-lowering doses of nicotinic acid (at least 1 g / day) increased the risk of myopathy, while being used with other HMG-CoA reductase inhibitors. Perhaps due to the fact that they can cause myopathy and when used as monotherapy.
The combined use of rosuvastatin and ezetimiba did not lead to changes in AUC or C_max both drugs.
The use of HIV protease inhibitors (human immunodeficiency virus) with rosuvastatin can lead to a significant increase in the effect of rosuvastatin. A pharmacokinetic study of co-administration of 20 mg of rozuvastatin with healthy volunteers and a combination of two HIV protease inhibitors (400 mg of lopinavir / 100 mg of ritonavir) resulted in an approximately two and fivefold increase in AUC (0-24) and C_max, respectively.Thus, in patients infected with HIV, co-administration of rosuvastatin with HIV protease inhibitors is not recommended.

Overdose

With simultaneous administration of several daily doses, the pharmacokinetic parameters of rosuvastatin do not change.
Treatment: There is no specific treatment, symptomatic therapy is carried out to maintain the functions of vital organs and systems. Monitoring of liver function and CPK activity is necessary. Hemodialysis is ineffective.

Storage conditions

At a temperature not higher than 25^oC in original packaging.