Rosuvastatin - instructions for use, reviews, analogs and formulations (5 mg, 10 mg, 20 mg and 40 mg tablets) of a statin drug for the treatment of hypercholesterolemia and lowering cholesterol levels in adults, children and pregnancy. Composition

In this article, you can read the instructions for the use of a statin drug Rosuvastatin. Comments from visitors to the site - consumers of this medication, as well as opinions of doctors specialists on the use of Rosuvastatin in their practice are presented. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Rosuvastatin analogues in the presence of existing structural analogues.Use to treat hypercholesterolemia and lower blood cholesterol levels in adults, children, as well as in pregnancy and lactation. Composition of the preparation.

Rosuvastatin - a hypolipidemic agent from the group of statins, an inhibitor of HMG-CoA reductase. According to the principle of competitive antagonism, the statin molecule binds to that part of the coenzyme A receptor where this enzyme is attached. Another part of the statin molecule inhibits the conversion of hydroxymethylglutarate to mevalonate, an intermediate in the synthesis of the cholesterol molecule. Inhibition of the activity of HMG-CoA reductase results in a series of consecutive reactions that result in a decrease in intracellular cholesterol and a compensatory increase in LDL receptor activity and, accordingly, acceleration of LDL cholesterol catabolism (Xc).

The hypolipidemic effect of statins is associated with a decrease in the level of total cholesterol due to Xc-LDL. The decrease in LDL is dose-dependent and has a non-linear, but an exponential nature.

Statins do not affect the activity of lipoprotein and hepatic lipases, do not have a significant effect on the synthesis and catabolism of free fatty acids,therefore their effect on the level of TG is secondary and mediated through their main effects on the decrease in the level of LDL-C. The moderate decrease in TG levels in statin therapy appears to be due to the expression of the receptor (apo E) receptors on the surface of hepatocytes participating in the catabolism of the disease, which includes approximately 30% TG.

In addition to lipid-lowering effects, statins have a positive effect on endothelial dysfunction (preclinical signs of early atherosclerosis), on the vascular wall, atheroma state, improve the rheological properties of blood, and possess antioxidant, antiproliferative properties.

The therapeutic effect is manifested within 1 week after the start of therapy and after 2 weeks of treatment it is 90% of the maximum possible effect, which is usually achieved by 4 weeks and after that remains constant.

Composition

Calcium rosuvastatin + excipients.

Pharmacokinetics

After oral administration of Cmax, rosuvastatin in blood plasma is reached after approximately 5 hours. Bioavailability is approximately 20%. Rosuvastatin accumulates in the liver. Binding to plasma proteins (predominantly with albumin) is approximately 90%.Biotransformed to a small extent (about 10%), being a non-core substrate for cytochrome P450 isoenzymes. The main isoenzyme involved in the metabolism of rosuvastatin is CYP2C9. Isozymes CYP2C19, CYP3A4 and CYP2D6 are less involved in metabolism. The main revealed metabolites of rosuvastatin are N-dysmethyl and lactone metabolites. N-dimethyl is about 50% less active than rosuvastatin, lactone metabolites are not pharmacologically active. About 90% of the dose of rosuvastatin is excreted unchanged with feces. The remainder is excreted in the urine.

Indications

• Primary hypercholesterolemia according to Fredrickson classification (type 2a, including familial heterozygous hypercholesterolemia) or mixed hypercholesterolemia (type 2b) as a supplement to the diet, when diet and other non-medicamentous therapies (for example, physical exercises, weight loss) are insufficient;
• familial homozygous hypercholesterolemia as a supplement to diet and other lipid-lowering therapy (eg, LDL-apheresis) or in cases where such therapy is not effective enough;
• hypertriglyceridemia (type 4 according to Fredrickson's classification) as a supplement to the diet;
• slowing the progression of atherosclerosis as a supplement to the diet in patients who are shown 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 (age over 50 for men and over 60 for women, increased concentration of C-reactive protein (more than 2 mg / l) in the presence of at least one of additional risk factors, such as hypertension, low concentration of HDL-C, smoking, family history of early onset of coronary heart disease).

Forms of release

Tablets coated with 5 mg, 10 mg, 20 mg and 40 mg.

Instructions for use and dosing regimen

Take in, without chewing and grinding, swallowing whole, washing down with water. The drug can be administered at any time of the day, regardless of food intake.

Before starting therapy with Rosuvastatin, the patient should begin to follow the standard hypocholesterolemic diet and continue to observe it during treatment.The dose of the drug should be selected individually, depending on the purpose of therapy and the therapeutic response to treatment, taking into account current recommendations for target lipid concentrations.

The recommended initial dose is 10 mg once a day. If necessary, the dose can be increased to 20 mg after 4 weeks. A dose increase of up to 40 mg is possible only in patients with severe hypercholesterolemia and a high risk of cardiovascular complications (especially in patients with familial hypercholesterolemia) with insufficient efficacy at a dose of 20 mg and under the condition of a doctor's control.

Do not administer 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 the drug Rosuvastatin, it is necessary to monitor the lipid metabolism (if necessary, dose adjustment is required).

Side effect

• headache;
• dizziness;
• asthenic syndrome;
• anxiety;
• depression;
• insomnia;
• neuralgia;
• paresthesia;
• constipation;
• nausea;
• abdominal pain;
• reversible transient dose-dependent increase in hepatic transaminase activity;
• dyspepsia (including diarrhea, flatulence, vomiting);
• gastritis;
• gastroenteritis;
• pharyngitis;
• rhinitis;
• sinusitis;
• bronchial asthma;
• bronchitis;
• cough;
• dyspnea;
• pneumonia;
• angina pectoris;
• increased blood pressure;
• palpitation;
• vasodilation;
• myalgia;
• arthralgia;
• arthritis;
• muscular hypertonia;
• backache;
• myopathy;
• rhabdomyolysis (simultaneously with impaired renal function, against the background of taking the drug at a dose of 40 mg);
• tubular proteinuria (in less than 1% of cases - for doses of 10 and 20 mg, 3% for doses of 40 mg);
• peripheral edema (arms, legs, ankles, lower legs);
• lower abdominal pain;
• urinary tract infection;
• skin rash;
• itching;
• angioedema;
• transient dose-dependent increase in the activity of CKK (if the activity of CK is increased by more than 5 times compared with VGN therapy should be temporarily suspended);
• asthenic syndrome;
• anemia;
• pain in the chest;
• diabetes;
• ecchymosis;
• influenza-like syndrome;
• periodontal abscess.

Contraindications

For all daily doses:

• increased sensitivity to rosuvastatin or any of the components of the drug;
• lactose intolerance, lactase deficiency or glucose-galactose malabsorption (the preparation contains lactose);
• simultaneous administration of cyclosporine;
• increase in the concentration of CK in the blood more than 5 times compared with VGN;
• joint application with HIV protease inhibitors;
• myopathy;
• lack of adequate methods of contraception;
• pregnancy;
• the period of breastfeeding;
• children's age till 18 years.

In addition to the drug Rosuvastatin in a daily dose of 5, 10, 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-fold compared with IGN);
• severe renal failure (creatinine clearance less than 30 ml / min);
• patients who are predisposed to the development of myotoxic complications.

In addition to the drug Rosuvastatin in a daily dose of 40 mg:

• renal insufficiency of moderate and severe degree (creatinine clearance less than 60 ml / min);
• liver diseases in the active phase, including persistent increase in serum activity of transaminases and any increase in serum transaminase activity (more than 3 times as compared with IGN) in patients with risk factors for myopathy / rhabdomyolysis;
• personal or family anamnesis of muscular diseases;
• patients of the Mongoloid race.

Application in pregnancy and lactation

Rosuvastatin is contraindicated in pregnancy and during breastfeeding.

Women of reproductive age should apply adequate methods of contraception.

Because cholesterol and its biosynthetic products are important for fetal development, the potential risk of inhibiting HMG-CoA reductase exceeds the benefit of using the drug in pregnant women.

In case of pregnancy in the process of therapy, taking the drug should be stopped immediately.

Data on the allocation of rosuvastatin to breast milk are not available, so during breastfeeding, the drug should be discontinued.

Use in children

Contraindicated in children and adolescents under the age of 18 years (efficacy and safety not established).

special instructions

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

Therapy should be discontinued if the level of CK is significantly increased (more than 5 times compared with IGN) or if the muscle symptoms are pronounced and cause daily discomfort (even if the level of CK is 5 times less than that of VGN).

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

In most cases, proteinuria decreases or disappears during therapy and does not indicate the onset or progression of an existing kidney disease.

An increase in the incidence of myositis and myopathy in patients taking other HMG-CoA reductase inhibitors in combination with fibrin acid derivatives (including gemfibrozil), cyclosporine, nicotinic acid, azole antifungal agents, protease inhibitors and macrolide antibiotics has been reported. Gemfibrozil increases the risk of myopathy when combined with certain HMG-CoA reductase inhibitors.Thus, the simultaneous administration of rosuvastatin and gemfibrozil is not recommended. The risk-to-benefit ratio should be carefully weighed against the combined use of rosuvastatin and fibrates or niacin.

It is recommended to carry out the determination of liver function indices before the start of therapy and 3 months after the start of therapy. The use of rosuvastatin should stop or reduce the dose, if the level of activity of transaminases in the serum is 3 times higher than VGN.

In patients with hypercholesterolemia due to hypothyroidism or nephrotic syndrome, the treatment of underlying diseases should be performed prior to the initiation of treatment with rosuvastatin.

Impact on the ability to drive vehicles and manage mechanisms

When dealing with potentially hazardous activities, patients should be aware that dizziness may occur during therapy.

Drug Interactions

With simultaneous application of rosuvastatin and cyclosporin AUC, rosuvastatin was on average 7 times higher than the value observed in healthy volunteers, the plasma concentration of cyclosporine did not change.

The initiation of rosuvastatin therapy or an increase in the dose of the drug in patients receiving both vitamin K antagonists (eg, warfarin) may lead to an increase in prothrombin time and INR, and cancellation of rosuvastatin or a decrease in dose may result in a decrease in INR (in such cases, INR monitoring is recommended).

The combined use of rosuvastatin and gemfibrozil leads to a 2-fold increase in Cmax in the blood plasma and AUC of rosuvastatin.

The simultaneous use of rosuvastatin and antacids containing aluminum and magnesium hydroxide leads to a decrease in the plasma concentration of rosuvastatin by approximately 50%. This effect is less pronounced if antacids are administered 2 hours after rosuvastatin administration (clinical significance is unknown).

The simultaneous use of rosuvastatin and Erythromycin leads to a 20% decrease in AUC of rosuvastatin and 20% in rosuvastatin Cmax, and probably by a 30% increase in motility of the intestine caused by erythromycin.

The simultaneous use of rosuvastatin and oral contraceptives increases the AUC of ethinylestradiol and AUC norgestrel by 26% and 34%, respectively. It is impossible to exclude such interaction with simultaneous application of rosuvastatin and hormone replacement therapy.

Gemfibrozil, other fibrates and hypolipidemic doses of nicotinic acid (more than 1 g per day) increased the risk of myopathy with other HMG-CoA reductase inhibitors, possibly due to the fact that they can cause myopathy and when used as monotherapy.

The combined use of rosuvastatin and Itraconazole (CYP3A4 inhibitor) increases rosuvastatin AUC by 28% (clinically insignificant).

Analogues of the drug Rosuvastatin

Structural analogs for the active substance:

• Akorta;
• The Cross;
• Mertenil;
• Rosart;
• Rosystark;
• Calcium rosuvastatin;
• Rosuvastatin canon;
• Rosuvastatin C3;
• Rosewood;
• Rosulip;
• Roxer;
• Rustor;
• Suvardio;
• Tevastor.

Analogues for the pharmacological group (statins):

• Akorta;
• Aktalipid;
• Anistat;
• Apexstatin;
• Atherostat;
• Atokord;
• Atomax;
• Ator;
• Atorvastatin;
• Atorvox;
• Atoris;
• The Vasator;
• Vazilip;
• Zocor;
• Zokor forte;
• Zorstat;
• Cardiostatin;
• The Cross;
• Leskol;
• Leskol Fort;
• Lipobay;
• Lipon;
• Lipostat;
• Liprimar;
• Liptonorm;
• Lovacor;
• Lovastatin;
• Lovasterol;
• Mevakor;
• Mertenil;
• Novostat;
• Ovenkor;
• Pravastatin;
• Rovacor;
• Rosart;
• Rosewood;
• Rosulip;
• Roxer;
• Rustor;
• Simvakol;
• Simvale;
• Simvastatin;
• Simvastol;
• Symvor;
• Simgal;
• Simlo;
• Sinquard;
• Tevastor;
• Torvazine;
• Torvacard;
• Torvalip;
• Torvas;
• Tulip;
• Holletar.

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