Rosuvastatin
Rosuvastatin: 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. Drug interactions
- 14. Analogs
- 15. Terms and conditions of storage
- 16. Terms of dispensing from pharmacies
- 17. Reviews
- 18. Price in pharmacies
Latin name: Rosuvastatin
ATX code: C10AA07
Active ingredient: Rosuvastatin (Rosuvastatin)
Manufacturer: CANONPHARMA, Russia
Description and photo update: 19.10.2018
Prices in pharmacies: from 174 rubles.
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Rosuvastatin is a drug that improves the lipid profile in hypercholesterolemia.
Release form and composition
The dosage form of Rosuvastatin is film-coated tablets: pink, biconvex, the core in the cross section is white or almost white; 5 or 20 mg - round; 10 or 40 mg - oblong, on each side with a risk (in cans of 30 or 60 pcs., in a cardboard box 1 can; 5 mg - in blisters of 10, 14, 15 or 30 pcs., in a cardboard box a pack contains 1-4 or 6 packages; 10 or 20 mg - in blisters of 10, 14 or 15 pieces, 2-4 or 6 packages are placed in a cardboard box; 40 mg - in blisters of 6, 7, 10 or 15 pcs., 4–6 packages are placed in a cardboard box).
1 tablet contains:
- active substance: rosuvastatin - 5, 10, 20 or 40 mg (rosuvastatin calcium - 5.2 / 10.4 / 20.8 / 41.6;
- auxiliary components: magnesium stearate - 0.9 / 1.8 / 3.6 / 7.2 mg; lactose monohydrate - 54.9 / 109.8 / 219.6 / 439.2 mg; crospovidone - 4.5 / 9/18/36 mg; microcrystalline cellulose - 18/36/72/144 mg; calcium hydrogen phosphate dihydrate - 6.5 / 13/26/52 mg;
- shell: (titanium dioxide - 0.286 2 / 0.572 4 / 1.144 8 / 2.289 6 mg; hypromellose - 1.62 / 3.24 / 6.48 / 12.96 mg; macrogol 4000 - 0.243 / 0.486 / 0.972 / 1.944 mg; talc - 0.54 / 1.08 / 2.16 / 4.32 mg; red iron oxide - 0.010 8 / 0.021 6 / 0.043 2 / 0.086 4 mg) or (dry mixture for a film coating containing: talc - 20%; hypromellose - 60%; macrogol 4000 - 9%; titanium dioxide - 10.6%; red iron oxide - 0.4%) - 2.7 / 5.4 / 10.8 / 21.6 mg.
It is possible to vary the appearance of tablets, the composition of auxiliary components and packaging due to the presence of several official manufacturers of the drug.
Pharmacological properties
Pharmacodynamics
Rosuvastatin is one of the lipid-lowering drugs, selective competitive inhibitors of the enzyme hydroxymethylglutaryl coenzyme A (HMG-CoA) reductase, which converts HMG-CoA into mevalonate, a cholesterol precursor (CS).
The action of Rosuvastatin is directed to the liver, where the synthesis of Xc and catabolism of low density lipoproteins (LDL) occurs. As a result of the use of the drug on the surface of liver cells, the number of LDL receptors increases, the uptake and catabolism of LDL increases, which, in turn, leads to inhibition of the synthesis of very low density lipoproteins (VLDL) and a decrease in the total amount of LDL and VLDL.
Rosuvastatin lowers increased concentrations of LDL-cholesterol (LDL-C), triglycerides (TG), total cholesterol (TC), increases the concentration of high-density lipoprotein cholesterol (HDL-cholesterol), and also reduces the concentration of VLDL-C, apolipoprotein B (ApoB), TG-VLDL and increases the concentration of apolipoprotein A-I (ApoA-I).
The effect of Rosuvastatin is manifested in a decrease in the atherogenic coefficient, which in patients with hypercholesterolemia is characterized by an improvement in the lipid profile.
Atherogenic index = (OHs - Chs-HDL) / Chs-HDL.
The therapeutic effect develops within 7 days from the moment the drug was started. The maximum therapeutic effect is usually observed by the fourth week of therapy, and it persists with regular administration of the drug.
Rosuvastatin is effective in patients with hypercholesterolemia with / without hypertriglyceridemia, including patients with familial hypercholesterolemia and diabetes mellitus.
An additive effect is observed in combination with fenofibrate (in relation to the concentration of TG) and lipid-lowering doses of nicotinic acid (in relation to the concentration of HDL-C). The possibility of combination therapy is assessed by a physician.
Pharmacokinetics
- absorption and distribution: approximately 5 hours after oral administration, the maximum plasma concentration of rosuvastatin in the blood (Cmax) is reached. Absolute bioavailability is about 20%, the substance is metabolized mainly by the liver. Vd (volume of distribution) - about 134 liters. About 90% of the substance binds to blood plasma proteins, mainly albumin;
- metabolism: rosuvastatin is a non-core substrate for metabolism by isoenzymes of the cytochrome P450 system. The main isoenzyme involved in the metabolism of rosuvastatin is the CYP2C9 isoenzyme. The involvement of isoenzymes CYP2C19, CYP2D6 and CYP3A4 in metabolism occurs to a lesser extent. About 10% of the substance is metabolized;
- Excretion: approximately 90% of the dose of the drug is excreted unchanged through the intestines (including unabsorbed / absorbed substance). The remaining part is excreted by the kidneys. T 1/2 (plasma half-life) is approximately 19 hours, with an increase in the dose of the drug, T 1/2 does not change. The geometric mean plasma clearance is about 50 l / h.
The systemic exposure of rosuvastatin increases in proportion to the dose. With daily administration, no change in pharmacokinetic parameters occurs.
In patients of the Mongoloid race (Chinese, Japanese, Filipinos, Koreans and Vietnamese), there is an approximately twofold increase in the median AUC (area under the concentration-time curve) and Cmax of rosuvastatin in comparison with Caucasians; in Indian patients - 1.3 times. Among representatives of the Negroid race and Caucasians, the pharmacokinetic analysis of the drug did not reveal clinically significant differences in pharmacokinetics.
Indications for use
- primary hypercholesterolemia according to the Fredrickson classification (type IIa, including familial heterozygous hypercholesterolemia) or mixed hypercholesterolemia (type IIb) - as a supplement to diet in cases where compliance with it and the use of other non-drug therapeutic methods (for example, weight loss, exercise) are insufficient;
- familial homozygous hypercholesterolemia - as an addition to diet and other lipid-containing therapy, or in cases where such treatment is not effective enough;
- hypertriglyceridemia (type IV according to Fredrickson's classification) - as a supplement to the diet;
- main cardiovascular complications, including stroke, myocardial infarction, arterial revascularization - primary prevention in the absence of clinical signs of coronary artery disease (coronary heart disease), but with an increased risk of its occurrence (age over 50/60 years for men / women, increased concentration of C- reactive protein in the presence of at least 1 of the additional risk factors - arterial hypertension, low concentration of HDL cholesterol, smoking, a burdened history of early onset of coronary artery disease);
- atherosclerosis (as a means of slowing its progression) - in addition to the diet in patients who are shown measures to lower the concentration of total cholesterol and cholesterol-LDL.
Contraindications
Absolute:
- the presence of a predisposition to the occurrence of myotoxic complications;
- liver diseases occurring in the active phase, including a persistent increase in serum transaminase activity and any plasma increase in transaminase activity in the blood (exceeding the upper limit of the norm by more than 3 times);
- myopathy;
- glucose-galactose malabsorption, lactase deficiency or lactose intolerance;
- renal dysfunction: for a dose of 5, 10 or 20 mg per day - in severe course (with creatinine clearance less than 30 ml / min); for a dose of 40 mg per day - moderate severity (with creatinine clearance less than 60 ml / min);
- combined use with cyclosporine;
- lack of adequate contraceptive methods in women of reproductive age;
- pregnancy and lactation;
- age up to 18 years;
- individual intolerance to the components of the drug.
Additional absolute contraindications for the use of Rosuvastatin in a daily dose of 40 mg:
- the presence of a risk of myopathy / rhabdomyolysis: renal failure, hypothyroidism, a history of myotoxicity associated with the use of other HMG-CoA reductase inhibitors or fibrates, a family / personal history of muscle diseases;
- conditions in which the plasma concentration of rosuvastatin may increase;
- alcohol abuse;
- belonging to the Mongoloid race;
- combination therapy with fibrates.
Relative (diseases / conditions in the presence of which the appointment of Rosuvastatin requires caution):
- carrying out extensive surgical interventions;
- burdened history of liver disease;
- trauma;
- arterial hypotension;
- sepsis;
- uncontrolled seizures or severe metabolic, electrolyte, or endocrine disorders;
- age from 65 years.
Additional relative contraindications for the use of Rosuvastatin in a daily dose of 5, 10 or 20 mg:
- the presence of a risk of myopathy / rhabdomyolysis: renal failure, hypothyroidism, a history of myotoxicity associated with the use of other inhibitors of HMG-CoA reductase or fibrates, a personal or family history of muscle diseases;
- conditions in which the plasma concentration of rosuvastatin may increase;
- alcohol abuse;
- belonging to the Mongoloid race;
- combined use with fibrates.
An additional relative contraindication for the use of Rosuvastatin in a daily dose of 40 mg is renal failure of mild severity (with creatinine clearance of more than 60 ml / min).
Instructions for the use of Rosuvastatin: method and dosage
Rosuvastatin should be taken orally whole, without crushing or chewing, with water. Food intake does not affect the effectiveness of the drug.
The daily dose is taken at a time.
Before starting the treatment course, it is necessary to adhere to the standard hypocholesterolemic diet (it is required to follow it throughout the therapy).
The doctor selects the dose of Rosuvastatin individually, depending on the goals and the received therapeutic response to treatment, taking into account the current recommendations for the target lipid concentration.
At the beginning of the course or after transferring from other HMG-CoA reductase inhibitors, it is recommended to prescribe 5 or 10 ml of Rosuvastatin per day. When choosing a dose, it is necessary to take into account the existing likelihood of developing cardiovascular complications, and an assessment of the likelihood of adverse reactions is also required. After 4 weeks, if necessary, the doctor may increase the dose.
When taking the drug in a daily dose of 40 mg, the likelihood of side effects significantly increases, therefore, such a dose can be prescribed only in the following cases: severe hypercholesterolemia and a high risk of cardiovascular complications (especially with familial hypercholesterolemia) if the desired result was not achieved from taking Rosuvastatin at a dose of 20 mg. Treatment should only be carried out under the supervision of a specialist.
Patients who have not previously sought medical help should not be prescribed the drug in a dose of 40 mg. After 2–4 weeks from the start of taking or increasing the dose of Rosuvastatin, it is necessary to monitor lipid metabolism. Based on its results, the dose can be adjusted.
With creatinine clearance of 30-60 ml / min, Rosuvastatin is prescribed at an initial dose of 5 mg. The use of the drug in a daily dose of 40 mg is contraindicated. Patients with creatinine clearance less than 30 ml / min, as well as in cases of liver disease in the active phase, the drug is not prescribed.
The recommended starting dose for patients of the Mongoloid race is 5 mg. At a dose of 40 mg, the drug is not prescribed to this group of patients.
For patients with c.521CC or c.421AA genotypes, the recommended maximum daily dose of Rosuvastatin is 20 mg.
In cases of predisposition to the development of myopathy, the recommended initial dose is 5 mg, the maximum dose is 20 mg.
When prescribing combination therapy, it is necessary to assess the likelihood of developing myopathy.
Side effects
Disorders observed during therapy are usually dose-dependent and unexpressed and go away on their own.
Possible side reactions (> 10% - very often;> 1% and 0.1% and 0.01% and <0.1% - rarely; <0.01% - very rarely; if it is impossible to assess the frequency of occurrence of violations - with unspecified frequency):
- endocrine system: often - type 2 diabetes mellitus;
- immune system: rarely - angioedema and other hypersensitivity reactions;
- central nervous system: often - dizziness, headache;
- musculoskeletal system: often - myalgia; rarely - rhabdomyolysis, myopathy, including myositis (with an increase in creatine phosphokinase activity more than 5 times, the use of Rosuvastatin is suspended);
- digestive system: often - nausea, constipation, pain in the abdomen; rarely - pancreatitis;
- urinary system: proteinuria (usually decreases / disappears during treatment and is not a sign of acute or progression of existing kidney disease);
- laboratory parameters: increased concentration of bilirubin, glucose, activity of gamma-glutamyl transpeptidase, alkaline phosphatase, functional disorders of the thyroid gland;
- skin: infrequently - rash, pruritus, urticaria;
- liver: increased activity of hepatic transaminases (usually dose-dependent, insignificant, asymptomatic and temporary);
- other reactions: often - asthenic syndrome.
Violations identified during post-registration studies:
- digestive system: very rarely - hepatitis, jaundice; rarely - increased activity of hepatic transaminases; with an unknown frequency - diarrhea;
- musculoskeletal system: very rarely - arthralgia; with an unknown frequency - immune-mediated necrotizing myopathy;
- urinary system: very rarely - hematuria;
- reproductive system and mammary gland: with an unknown frequency - gynecomastia;
- respiratory system: with an unknown frequency - shortness of breath, cough;
- hematopoietic system: with an unknown frequency - thrombocytopenia;
- central nervous system: very rarely - decrease / loss of memory; with an unspecified frequency - peripheral neuropathy;
- skin and subcutaneous fat: with an unknown frequency - Stevens-Johnson syndrome;
- others: with an unknown frequency - peripheral edema.
During therapy with some statins, the following adverse reactions have been reported: sexual dysfunction, depression, hyperglycemia, sleep disturbances, including nightmares and insomnia, an increase in the concentration of glycosylated hemoglobin. There are isolated reports of the development of interstitial lung disease, especially during long-term treatment.
Overdose
In cases of simultaneous administration of several daily doses, no change in the pharmacokinetic parameters of Rosuvastatin is observed.
Possible symptoms: increased side reactions.
Therapy: hemodialysis is ineffective; there is no specific antidote; it is recommended to flush the stomach in a timely manner and carry out symptomatic treatment; shows control of hepatic function and creatine phosphokinase activity, as well as activities that are aimed at maintaining the functions of vital systems and organs.
special instructions
When using high doses of Rosuvastatin (usually 40 mg), tubular proteinuria may occur, which is usually transient. This violation does not indicate an exacerbation / progression of kidney disease. Patients taking the maximum dose of the drug are recommended to monitor the indicators of renal function.
To avoid distorting the results, it is not recommended to determine the activity of creatine phosphokinase after increased physical exertion or in the presence of other possible reasons for an increase in its activity. If at the beginning of therapy the initial activity of creatine phosphokinase is significantly exceeded (more than 5 times), a second measurement must be performed after 5-7 days. When the indicators are confirmed, treatment is not started.
The sudden onset of muscle pain / weakness or cramps, especially when combined with fever and malaise, requires medical attention. In such cases, it is necessary to determine the activity of creatine phosphokinase. If the symptoms disappear and the indicators return to normal, it is possible to consider re-prescribing rosuvastatin in lower doses under close monitoring of the patient's condition. In the absence of symptoms, routine monitoring of creatine phosphokinase activity is impractical.
There is information about very rare cases of immune-mediated necrotizing myopathy, proceeding with clinical manifestations (persistent weakness of the proximal muscles and increased serum creatine phosphokinase activity) during therapy or upon discontinuation of Rosuvastatin. Additionally, serological studies, examination of the nervous and muscular systems, and the use of immunosuppressive drugs may be required.
When taking Rosuvastatin and concomitant therapy, there are no signs of an increase in the effect on skeletal muscles. However, there are reports of an increase in the number of cases of myopathy and myositis in patients taking other inhibitors of HMG-CoA reductase in combination with fibric acid derivatives, including with gemfibrozil, cyclosporin, nicotinic acid in lipid-lowering doses (more than 1000 mg per day), azole antifungal agents, HIV protease inhibitors and macrolide antibiotics. Gemfibrozil increases the risk of myopathy when used together with some HMG-CoA reductase inhibitors (the combination is not recommended).
When used together with fibrates or lipid-lowering doses of nicotinic acid, the benefits must be carefully balanced against the risk. Rosuvastatin at a dose of 40 mg is contraindicated in combination with fibrates.
If patients have a glucose concentration of 5.6–6.9 mmol / L, the likelihood of type 2 diabetes mellitus increases.
Dose reduction / withdrawal of therapy is indicated in cases where the activity of hepatic transaminases in the blood serum exceeds the upper limit of the norm by 3 times or higher.
If there is a suspicion of the development of interstitial lung disease (manifested as shortness of breath, unproductive cough, weakness, weight loss, fever and deterioration in general well-being), Rosuvastatin is canceled.
Influence on the ability to drive vehicles and complex mechanisms
Due to the likelihood of developing weakness and dizziness, patients should be careful while driving vehicles during the period of therapy.
Application during pregnancy and lactation
The period of pregnancy and lactation is a contraindication to the use of the drug.
Women of reproductive age are shown to use adequate methods of contraception.
Pediatric use
According to the instructions, Rosuvastatin is not prescribed for children under 18 years of age.
With impaired renal function
- daily dose of 5, 10 or 20 mg: severe impairment of renal function (with creatinine clearance less than 30 ml / min) - therapy is contraindicated; renal failure - use requires caution;
- daily dose of 40 mg: renal failure of moderate severity (with creatinine clearance less than 60 ml / min) - therapy is contraindicated; renal failure - use requires caution.
The recommended dose at the beginning of therapy for patients with moderate impairment of renal function is 5 mg.
For violations of liver function
- active phase of liver diseases, including a persistent increase in serum transaminase activity and any increase in serum transaminase activity in the blood - therapy is contraindicated;
- burdened history of liver disease - use requires caution.
There is no experience of using Rosuvastatin for severe liver functional disorders (more than 9 points on the Child-Pugh scale).
Drug interactions
- cyclosporine: significant increase in exposure to rosuvastatin (the combination is contraindicated);
- inhibitors of transport proteins OATP1B1 and BCRP: an increase in the plasma concentration of rosuvastatin and the likelihood of myopathy;
- human immunodeficiency virus (HIV) protease inhibitors: significant increase in exposure to rosuvastatin (combination not recommended);
- gemfibrozil, fenofibrate, other fibrates and lipid-lowering doses of nicotinic acid (more than 1000 mg per day): an increase in the likelihood of developing myopathy (the recommended dose of Rosuvastatin at the beginning of the course is 5 mg, taking 40 mg per day is contraindicated for combined use);
- gemfibrozil and other drugs with hypolipidemic action: a significant increase in exposure to rosuvastatin and its maximum plasma concentration, pharmacodynamic interaction may be observed;
- antacids: a significant decrease in the plasma concentration of rosuvastatin (this effect is reduced in cases where the interval between taking drugs is at least 2 hours);
- ezetimibe: significant increase in exposure to rosuvastatin in patients with hypercholesterolemia; the likelihood of adverse reactions may increase;
- fusidic acid: the likelihood of developing rhabdomyolysis (if necessary, combined use may require temporary withdrawal of rosuvastatin);
- erythromycin: a significant decrease in exposure to rosuvastatin and a decrease in its maximum plasma concentration;
- vitamin K antagonists: at the beginning of therapy / with an increase in the dose of rosuvastatin - an increase in INR (International Normalized Ratio); when the drug is canceled / its dose is reduced, the INR is reduced, which requires monitoring of this indicator;
- oral contraceptives / hormone replacement therapy: significant increase in exposure to ethinylestradiol and norgestrel (these data should be taken into account when choosing the dose of drugs; therapy is generally well tolerated by patients).
In cases where combined use with drugs that increase the exposure to rosuvastatin is necessary, its dose should be adjusted.
Analogs
Rosuvastatin analogues are: Suvardio, Mertenil, Rosulip, Reddistatin, Acorta, Ro-statin, Crestor, Lipoprime, Rosistark, Roxera, Rosart, Tevastor, Rustor, Rosucard, Rosufast.
Terms and conditions of storage
Store in a dark place at temperatures up to 25 ° C. Keep out of the reach of children.
Shelf life is 2 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Rosuvastatin
According to reviews, Rosuvastatin is not very affordable (in comparison with other drugs from this group), but an effective drug. However, many patients report the development of various negative side effects, including muscle pain, dizziness, and increased blood pressure.
The price of Rosuvastatin in pharmacies
Approximate price for Rosuvastatin:
- 10 mg (30 pcs in a package) - 560–575 rubles;
- 20 mg (28 or 30 in a package) - 680 or 765-800 rubles;
- 40 mg (30 pcs in the package) - 1650 rubles.
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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!
