Rosuvastatin pills 10mg, 30pcs

Composition

Active ingredient:

rosuvastatin calcium in terms of rosuvastatin -10 mg.

Auxiliary substances:

core – lactose monohydrate (milk sugar) – 44,3 mg;

calcium hydrogen phosphate dihydrate – 10.0 mg;

povidone (polyvinylpyrrolidone middle) – 6.0 mg;

croscarmellose sodium (Primerose) – 4.0 mg;

sodium saariluoma-rat – 1.2 mg;

silicon dioxide colloidal (Aerosil) – 0.5 mg;

cellulose microcrystalline – 44,0 mg;

shell Opadry II (polyvinyl alcohol, partially hydrolyzed – 1,76 mg; macrogol (polyethylene glycol) 3350 – 0,494 mg; talc – 0.8 mg; titanium dioxide E 171 – 0,7668 mg; soy lecithin E 322 – 0,14 mg; aluminum lacquer based on the dye Indigo Carmine – 0,0024 mg; aluminum lacquer dye azorubin – 0,0204 mg; aluminum lacquer dye crimson [Ponceau 4R] – 0,0164 mg).

Pharmacological action

Rosuvastatin is a selective, competitive inhibitor of HMG-CoA reductase, an enzyme that converts 3-hydroxy-3-methylglutaryl coenzyme A to mevalonic acid, a cholesterol precursor.

The main target of rosuvastatin action is the liver, where the synthesis of cholesterol (cholesterol) and catabolism of low-density lipoproteins (LDL) is carried out. Rosuvastatin increases the number of “hepatic” LDL receptors on the cell surface, increasing the uptake and catabolism of LDL, which in turn leads to inhibition of very low-density lipoprotein (VLDL) synthesis, thereby reducing the total amount of LDL and VLDL.

Pharmacodynamics

Rosuvastatin-SZ reduces elevated concentrations of LDL cholesterol (LDL-C), total cholesterol, triglycerides (TG), increases the concentration of high-density lipoprotein cholesterol (HDL – C), and also reduces the concentration of apolipoprotein B (apoB), HDL-C, VLDL-C, TG-VLDL and increases the concentration of apolipoprotein A-I (ApoA-I), reduces the LDL-C/HDL-C ratio, total cholesterol/HDL-C and non-HDL-C/HDL-C ratio, and the apoB/ApoA-I ratio.

The therapeutic effect develops within one week after the start of therapy with Rosuvastatin-SZ, after 2 weeks of treatment it reaches 90% of the maximum possible effect. The maximum therapeutic effect is usually achieved by the 4th week of therapy and is maintained with regular use of the drug.

Rosuvastatin-SZ is effective in adult patients with hypercholesterolemia with or without hypertriglyceridemia, regardless of race, gender or age, including in patients with diabetes mellitus and familial hypercholesterolemia. In 80% of patients with Fredrickson type IIA and IIb hypercholesterolemia (mean baseline LDL-C concentration of about 4.8 mmol/l) against the background of taking the drug at a dose of 10 mg, the concentration of LDL-C reaches values of less than 3 mmol/l.

In patients with heterozygous familial hypercholesterolemia receiving Rosuvastatin – SZ at a dose of 20-80 mg, there is a positive dynamics in the lipid profile indicators. After titration to a daily dose of 40 mg (12 weeks of therapy), the LDL-C concentration decreased by 53%. In 33% of patients, an LDL-C concentration of less than 3 mmol/l is achieved.

In patients with homozygous familial hypercholesterolemia, taking Rosuvastatin – SZ at a dose of 20 mg and 40 mg, the average decrease in LDL-C concentration is 22%. In patients with hypertriglyceridemia with an initial TG concentration of 273 to 817 mg / dl, who received Rosuvastatin-SZ at a dose of 5 mg to 40 mg once a day for 6 weeks, the concentration of TG in blood plasma significantly decreased.

An additive effect is observed in combination with fenofibrate in relation to the content of triglycerides and with nicotinic acid in lipid-lowering doses in relation to the content of HDL-C (see also the section “Special instructions”). According to the results of clinical studies, patients with severe hypercholesterolemia and a high risk of cardiovascular diseases (CVD) should be prescribed a dose of Rosuvastatin-SZ 40 mg. The results of a clinical study (Justification of statin use for primary prevention: an interventional study evaluating rosuvastatin) showed that rosuvastatin significantly reduced the risk of developing cardiovascular complications.

Indications

-Fredrickson’s primary hypercholesterolemia (type IIa, including familial heterozygous hypercholesterolemia) or mixed hypercholesterolemia (type IIb) as a dietary supplement when diet and other non-drug treatments (e. g. exercise, weight loss) are insufficient.

– Familial homozygous hypercholesterolemia as an adjunct to diet and other lipid-lowering therapy (for example, LDL apheresis), or in cases where such therapy is not effective enough.

– Hypertriglyceridemia (Fredrickson type IV) as a dietary supplement.

– Primary dysbetalipoproteinemia (Frederickson type III) as a dietary supplement.

– To slow the progression of atherosclerosis as an adjunct to diet in patients who are indicated for therapy to reduce the concentration of total cholesterol and LDL-C.

– Primary prevention of major cardiovascular complications (stroke, heart attack, arterial revascularization) in adult patients without clinical signs of coronary heart disease, but with an increased risk of its development (the age of 50 years for men and over 60 years for women, the increased concentration of C-reactive protein (≥ 2 mg/l) in the presence of at least one additional risk factors such as arterial hypertension, a low concentration of HDL-C, Smoking, family history of early CHD).

Contraindications

For the drug Rosuvastatin-SZ in a daily dose of 5 mg,10 mg and 20 mg:  

– hypersensitivity to rosuvastatin or any of the components of the drug

– lactose intolerance, lactase deficiency or glucose-galactose malabsorption (the drug contains lactose) 

– children under 18 years

of age – 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 the upper limit of normal) 

– severe renal insufficiency (creatinine clearance less than 30 ml / min) 

– myopathy

– concomitant use of cyclosporine

– in women: pregnancy; breast-feeding, lack of adequate methods of contraception

-increased creatine phosphokinase (CPK) concentration in the blood by more than 5 times compared to the upper limit of normal

– combined use with HIV protease inhibitors

-in patients predisposed to the development of myotoxic complications

For the drug Rosuvastatin-SZ in a daily dose of 40 mg:  

– hypersensitivity to rosuvastatin or any of the components of the drug

– lactose intolerance, lactase deficiency or glucose-galactose malabsorption (the drug contains lactose) 

– children up to age 18 years

– concomitant use of cyclosporine

in women: pregnancy, breastfeeding, lack of adequate methods of contraception

– increasing the concentration of creatine phosphokinase (CPK) in the blood more than 5 times compared with the upper limit of normal

joint use of inhibitors of HIV protease

– renal failure of moderate and severe (CC less than 60 ml/min) 

– liver disease in the active phase, including a persistent increase in serum transaminases and any increase of transaminases in blood serum (more than 3 times compared with the upper limit of normal) in patients with risk factors for myopathy/rhabdomyolysis, namely:

– hypothyroidism

– myotoxicity in patients receiving other inhibitors of HMG-COA reductase inhibitors or fibrates in history

– excessive alcohol consumption

– States, which may lead to increased plasma concentrations of rosuvastatin

– concurrent use of fibrates 

– myopathy

-personal or family history of muscle diseases

– for patients of the Mongolian race

With caution

For the drug Rosuvastatin-SZ in a daily dose of 5 mg,10 mg and 20 mg: There is a risk of developing myopathy/rhabdomyolysis – renal insufficiency, hypothyroidism, personal or family history of hereditary muscle diseases and a previous history of muscle toxicity with the use of other HMG-CoA reductase inhibitors or fibrates; excessive alcohol consumption; age over 65 years; conditions in which an increase in the plasma concentration of rosuvastatin is noted * race (Mongoloid race); concomitant use with fibrates (see section “Pharmacokinetics”); a history of liver disease; sepsis; hypotension; extensive surgery, trauma, severe metabolic, endocrine or electrolyte disorders, or uncontrolled seizures. Concomitant use with colchicine and ezetimibe (see section “Interactions with other medicinal products”). For the drug Rosuvastatin-SZ in a daily dose of 40 mg: Mild renal failure (creatinine clearance more than 60 ml / min); age over 65 years; a history of liver disease; sepsis; hypotension; extensive surgical interventions, injuries, severe metabolic, endocrine or electrolyte disorders or uncontrolled convulsive seizures. Concomitant use with colchicine and ezetimibe (see section “Interactions with other medicinal products”). Patients with hepatic insufficiency There are no data or experience of using the drug in patients with more than 9 points on the Child-Pugh scale (seesections “Pharmacodynamics” and “Special instructions”).

Side effects

Side effects observed when taking the drug Rosuvastatin, usually expressed slightly and go away on their own. As with other HMG-CoA reductase inhibitors, the frequency of side effects is mainly dose-dependent. The frequency of undesirable effects is presented as follows: often (> 1/100, ><1/10); infrequently (> 1/1000, <1/10); infrequently (><1/100); rarely (> 1/10000, <1/100); rarely (>< 1/1000); very rarely ( 

The immune system

Rarely: hypersensitivity reactions, including angioedema.

Endocrine System

Common: Type 2 diabetes mellitus

From the central nervous system

Often: headache, dizziness

From the digestive tract

Often: constipation, nausea, abdominal pain Rarely: pancreatitis

From the side of the skin

Infrequently: pruritus, rash, urticaria

Musculoskeletal disorders

Common: myalgia Rare: myopathy (including myositis), rhabdomyolysis

Other

Common: asthenic syndrome

From the urinary system

Patients treated with Rosuvastatin may develop proteinuria. Changes in the amount of protein in the urine (from no or trace amounts to ++ or more) are observed in less than 1% of patients receiving 10-20 mg of the drug, and in approximately 3% of patients receiving 40 mg of the drug. A slight change in the amount of protein in the urine was observed when taking a dose of 20 mg. In most cases, proteinuria decreases or disappears during therapy and does not indicate the occurrence of acute or progressive existing kidney disease.

From the musculoskeletal system

The following effects on the musculoskeletal system have been reported when Rosuvastatin is used at all doses and, in particular, when taking doses of the drug exceeding 20 mg: myalgia, myopathy (including myositis), in rare cases – rhabdomyolysis with or without acute renal failure. A dose-dependent increase in creatine phosphokinase (CPK) activity is observed in a small number of patients taking rosuvastatin. In most cases, it was minor, asymptomatic, and temporary. In case of an increase in CPK activity (more than 5 times compared to the upper limit of normal), therapy should be suspended.

From the liver

When using rosuvastatin, a dose-dependent increase in the activity of “hepatic” transaminases is observed in a small number of patients. In most cases, it is minor, asymptomatic, and temporary.

Laboratory parameters

When using the drug Rosuvastatin, the following changes in laboratory parameters were also observed: increased glucose concentration, bilirubin, gamma-glutamyltranspeptidase activity, alkaline phosphatase, and thyroid function disorders.

Post-marketing application

The following side effects have been reported in post-marketing use of Rosuvastatin:: 

From the digestive tract

Very rare: jaundice, hepatitis Rare: increased activity of “hepatic” transaminases. Frequency unknown: diarrhea, fatal and non-fatal liver failure

From the musculoskeletal system

Very rare: arthralgia. Frequency unknown: immune-mediated necrotizing myopathy

From the central nervous system

Very rare: polyneuropathy, forgetfulness, amnesia, memory loss, respiratory confusion Frequency unknown: cough, shortness of breath

From the urinary system

Very rare: hematuria, microhematuria

From the skin and subcutaneous fat

Frequency unknown: Stevens-Johnson syndrome From the reproductive system and breast Frequency unknown: gynecomastia 

Other

Frequency unknown: peripheral edema; thrombocytopenia; interstitial lung disease. The following side effects have been reported with some statins: depression, sleep disorders including insomnia and nightmares, and sexual dysfunction.

Interaction

of Cyclosporine and gemfibrozil enhances the effects of rosuvastatin. Antacids that contain magnesium or aluminum reduce the plasma concentration of rosuvastatin by about 50% (they should be taken 2 hours after taking rosuvastatin). Erythromycin increases gastrointestinal motility and reduces the effects of rosuvastatin. Rosuvastatin enhances the effects of oral contraceptives. Gemfibrozil, other fibrates, and nicotinic acid in lipid-lowering doses (approximately 1 g/day) increase the possibility of myopathy when combined with rosuvastatin. When rosuvastatin is co-administered with itraconazole, the AUC of rosuvastatin increases by 28% (which is clinically insignificant). When rosuvastatin is co-administered with drugs that reduce the content of endogenous steroid hormones (including cimetidine, ketoconazole, spironolactone), a more pronounced decrease in endogenous steroid hormones is possible.

How to take, course of use and dosage

Inside, do not chew or crush the tablet, swallow whole, with water. The drug can be prescribed at any time of the day, regardless of food intake. Before starting therapy with Rosuvastatin, the patient should begin to follow a standard hypocholesterolemic diet and continue to follow it during treatment.

The dose of the drug should be selected individually, depending on the goals of therapy and the therapeutic response to treatment, taking into account current recommendations for target lipid concentrations. The recommended starting dose for patients starting to take the drug, or for patients transferred from taking other HMG-CoA reductase inhibitors, should be 5 mg or 10 mg of Rosuvastatin 1 time per day.

When choosing the initial dose, you should be guided by the individual cholesterol content and take into account the possible risk of cardiovascular complications, as well as the potential risk of side effects. If necessary, the dose can be increased to a larger one after 4 weeks.

Due to the possible development of side effects when taking a dose of 40 mg, compared with lower doses of the drug, an increase in the dose to 40 mg, after an additional dose above the recommended initial dose for 4 weeks of therapy, can only be carried out in patients with severe hypercholesterolemia and at high risk of cardiovascular complications (especially in patients with familial hypercholesterolemia),

Especially careful monitoring of patients receiving the drug at a dose of 40 mg is recommended. It is not recommended to prescribe a dose of 40 mg to patients who have not previously consulted a doctor. After 2-4 weeks of therapy and/or with an increase in the dose of Rosuvastatin, monitoring of lipid metabolism parameters is necessary (if necessary, dose adjustment is required).

Homozygous hereditary hypercholesterolemia

The recommended starting dose is 20 mg once daily.

Elderly patients

Patients over the age of 65 years are recommended to start using the drug with a dose of 5 mg once a day.

Patients with renal insufficiency

No dose adjustment is required in patients with mild or moderate renal insufficiency.

In patients with severe renal insufficiency (creatinine clearance less than 30 ml/min), the use of Rosuvastatin is contraindicated. It is contraindicated to use the drug at a dose of 40 mg in patients with moderate renal impairment (creatinine clearance 30-60 ml / min). In patients with moderate renal impairment, an initial dose of 5 mg is recommended.

Patients with hepatic insufficiency

Rosuvastatin is contraindicated in patients with active liver disease (see section “Contraindications”).

Special populations.

Ethnic groups When studying the pharmacokinetic parameters of rosuvastatin in patients belonging to different ethnic groups, an increase in the systemic concentration of rosuvastatin among Japanese and Chinese was noted. This fact should be taken into account when prescribing Rosuvastatin to these groups of patients. When prescribing doses of 10 mg and 20 mg, the recommended starting dose for patients of the Mongolian race is 5 mg. It is contraindicated to prescribe the drug at a dose of 40 mg to patients of the Mongolian race.

Patients predisposed to myopathy

It is contraindicated to prescribe the drug at a dose of 40 mg to patients with factors that may indicate a predisposition to the development of myopathy. When prescribing doses of 10 mg and 20 mg, the recommended initial dose for this group of patients is 5 mg.

Use in concomitant therapy

When the drug is used concomitantly with gemfibrozil, fibrates, nicotinic acid in a dose of more than 1 g / day, an initial dose of 5 mg is recommended for patients. The dose of Rosuvastatin should not exceed 10 mg once a day.

Overdose

With simultaneous use of several daily doses, the pharmacokinetic parameters of rosuvastatin do not change. There is no specific treatment for rosuvastatin overdose.In case of overdose, it is recommended to carry out symptomatic treatment and measures aimed at maintaining the functions of vital organs and systems. Monitoring of liver function and CKD levels is necessary. It is unlikely that hemodialysis will be effective.

Special instructions

Use with caution in the presence of risk factors for rhabdomyolysis (including renal failure, hypothyroidism, a personal or family history of hereditary muscle diseases and a previous history of muscle toxicity when using other HMG-CoA reductase inhibitors or fibrates), in chronic alcoholism, in patients over the age of 65, with a history of liver disease, sepsis, arterial hypotension, during extensive surgical interventions, injuries, severe metabolic disorders. endocrine or electrolyte disorders, uncontrolled epilepsy, in people of Asian descent (Chinese, Japanese).

Therapy should be discontinued if the CK level is significantly increased (more than 5 times higher than ULN) or if muscle symptoms are severe and cause daily discomfort (even if the CK level is 5 times lower than ULN).

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

In most cases, proteinuria decreases or disappears during therapy and does not indicate the occurrence of acute or progressive existing kidney disease.

An increased incidence of myositis and myopathy has been reported in patients treated with other HMG-CoA reductase inhibitors in combination with fibrinic acid derivatives (including gemfibrozil), cyclosporine, nicotinic acid, azole antifungal drugs, protease inhibitors, and macrolide antibiotics. Gemfibrozil increases the risk of myopathy when co-administered with certain HMG-CoA reductase inhibitors. Therefore, concomitant use of rosuvastatin and gemfibrozil is not recommended. The risk-benefit ratio of rosuvastatin and fibrates or niacin should be carefully weighed.

It is recommended to determine liver function indicators before the start of therapy and 3 months after the start of therapy. The use of rosuvastatin should be discontinued or the dose should be reduced if the level of 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 the underlying diseases should be carried out before starting treatment with rosuvastatin.

Influence on the ability to drive motor vehicles and manage mechanisms

When engaging in potentially dangerous activities, patients should be aware that dizziness may occur during therapy.

Storage conditions

Store in a dry place protected from light at a temperature not exceeding 30°C.

Active ingredient

Rosuvastatin

Conditions of release from pharmacies

By prescription

Dosage form

Tablets