Zetor 20mg 30 tablets

Zetori (Rosuvastatin) Composition Each Zetori film-coated tablet contains 10 mg, 20 mg, or 40 mg of the active substance rosuvastatin (as calcium salt). Excipients: microcrystalline cellulose, lactose, calcium hydrogen phosphate, sodium starch glycolate, crospovidone type A, magnesium stearate, coating powder. Mechanism of Action Hypolipidemic drug. It is a selective, competitive inhibitor of the enzyme 3-hydroxy-3-methylglutaryl-coenzyme A reductase (HMG-CoA reductase), which converts 3-hydroxy-3-methylglutaryl-coenzyme A to mevalonate, a precursor of cholesterol (CH). Rosuvastatin's action is mainly manifested in the liver, where cholesterol synthesis and low-density lipoprotein (LDL) catabolism occur. Rosuvastatin increases the number of hepatic LDL receptors on the cell surface, enhances LDL binding and catabolism, which in turn inhibits the synthesis of very low-density lipoproteins (VLDL) and consequently reduces the total amount of LDL and VLDL. Zetori reduces elevated LDL-CH, total cholesterol, and triglyceride (TG) levels, increases HDL-CH (high-density lipoprotein) content, and also reduces apolipoprotein B (ApoB), non-HDL-CH, VLDL-CH, TG-VLDL, and increases apolipoprotein A-1 (ApoA-1) levels. It reduces the ratio of LDL-CH / HDL-CH, total cholesterol / HDL-CH, and non-HDL-CH / HDL-CH, as well as ApoB / ApoA-1. Zetori is effective in adult patients with hypercholesterolemia with or without hypertriglyceridemia, regardless of race, sex, and age (including patients with diabetes mellitus and familial hypercholesterolemia). An additive effect is observed with the combination of Zetori (rosuvastatin) and fenofibrate regarding triglycerides, and with nicotinic acid regarding HDL-CH. Studies on the effect of rosuvastatin on reducing complications caused by lipid metabolism disorders (such as ischemic heart disease) are not yet completed. Zetori 40 mg is indicated for patients with severe hypercholesterolemia and a high risk of cardiovascular disease. See blog: Zetori - A drug for regulating high cholesterol. Pharmacokinetics Cmax is reached in approximately 5 hours. Bioavailability is approximately 20%. It is approximately 90% bound to plasma proteins. Rosuvastatin is partially metabolized (10%) in the liver. The main isoenzyme involved in its metabolism is CYP2C9. 90% of the drug's pharmacological activity is associated with rosuvastatin, and the remainder with its metabolites. The main part of rosuvastatin (90%) is excreted unchanged in feces, and the rest in urine. The half-life (T1/2) is approximately 19 hours. Also, see: Rosulip - Rosulip 20 mg 28 tablets. Indications - Primary hypercholesterolemia according to Fredrickson's classification (type IIa, including heterozygous familial hypercholesterolemia) or mixed hypercholesterolemia (type IIb). Indicated as an adjunct to diet when diet and other non-drug treatment methods (physical exercise, weight correction) are insufficient; - Familial homozygous hypercholesterolemia, as an adjunct to diet or other lipid-lowering therapy (e.g., LDL apheresis), or when such treatment is ineffective; - Hypertriglyceridemia (type IV according to Fredrickson's classification), as an adjunct to diet; - To slow the progression of atherosclerosis, as an adjunct to diet in patients for whom reduction of total cholesterol and LDL-CH levels is indicated. Contraindications For 10 mg and 20 mg tablets: - Hypersensitivity to rosuvastatin or any component of the drug; - Liver diseases in the active phase, including persistent increase in serum activity of transaminases and any activity of serum transaminases (3-fold or more compared to the upper limit of normal); - Severe renal impairment (creatinine clearance less than 30 ml/min); - Myopathy; - Concomitant use of cyclosporine; - Pregnancy and lactation, absence of adequate contraception methods; - Predisposition to myotoxic complications; - Lactose intolerance, lactase deficiency, or glucose-galactose malabsorption (the drug contains lactose). For 40 mg tablets: In addition to the above contraindications: - Presence of risk factors for the development of myopathy/rhabdomyolysis: moderate renal insufficiency (CrCl less than 60 ml/min); hypothyroidism; personal or family history of muscle disease; history of myotoxicity with HMG-CoA reductase inhibitors or fibrates; excessive alcohol consumption; conditions that may lead to increased plasma concentration of rosuvastatin; concomitant use of fibrates; patients of Asian race. Use with caution For 10 mg and 20 mg tablets: In the presence of risk factors for the development of myopathy/rhabdomyolysis - renal insufficiency, hypothyroidism, personal or family history of muscle disease, and a history of muscle toxicity with other HMG-CoA reductase inhibitors or fibrates; excessive alcohol consumption; age over 65 years; conditions that lead to increased plasma concentration of rosuvastatin; racial origin (Asian race); concomitant administration with fibrates; history of liver disease; sepsis; arterial hypotension; major surgery, trauma, severe metabolic, endocrine, and electrolyte disorders, or uncontrolled epileptic seizures. Use with caution For 40 mg tablets: Mild to moderate renal insufficiency (CrCl greater than 60 ml/min); age over 65 years; history of liver disease; sepsis; arterial hypotension; major surgery, trauma, severe metabolic, endocrine, and electrolyte disorders, or uncontrolled epileptic seizures. Precautions When taking Zetori 40 mg, monitoring of kidney function parameters is recommended. Cases of myalgia, myopathy, and rarely rhabdomyolysis have been reported with any dose of rosuvastatin, especially above 20 mg. Creatine phosphokinase (CPK) should not be measured after intense physical exertion or if there are other possible causes of increased creatine phosphokinase levels, as this may lead to misinterpretation of results. If the baseline CPK level is significantly elevated (more than 5 times the upper limit of normal), a repeat analysis should be performed after 5-7 days. If the repeat test confirms the elevated level (more than 5 times the upper limit of normal), therapy should not be initiated. In patients with risk factors for rhabdomyolysis, when prescribing Zetori (or other HMG-CoA reductase inhibitors), the ratio of expected benefit to potential risks should be assessed, and appropriate clinical observation should be carried out. Patients should be informed to immediately report muscle pain, muscle weakness, or cramps to their doctor, especially if they occur with fever and malaise. In such cases, CPK level determination is necessary. If the CPK level is significantly elevated (more than 5 times the upper limit of normal) or if muscle symptoms are severe and cause daily discomfort (even if the CPK level is less than 5 times the upper limit of normal), therapy should be discontinued. After the disappearance of symptoms and normalization of CPK levels, re-initiation of Zetori or other HMG-CoA reductase inhibitors may be considered, but at lower doses and with constant monitoring of the patient's condition. Routine CPK monitoring is not recommended in the absence of symptoms. No skeletal muscle toxicity has been observed with rosuvastatin in combination therapy. However, since cases of myositis and myopathy have been reported with other HMG-CoA reductase inhibitors in combination with fibrates, cyclosporine, nicotinic acid, azole antifungals, protease inhibitors, and macrolide antibiotics, concomitant use of Zetori with these agents is not recommended, especially with gemfibrozil, fibrates, and niacin. Lipid metabolism should be monitored 2-4 weeks after starting Zetori treatment or after dose increase, and the dose should be adjusted if necessary. Liver function parameters should be determined before starting Zetori treatment and 3 months after initiation. If the serum transaminase activity level exceeds 3 times the upper limit of normal, Zetori should be discontinued or the dose reduced. Before starting treatment with Zetori for hypocholesterolemia caused by hypothyroidism or nephrotic syndrome, patients should be treated for the underlying disease. The efficacy and safety of rosuvastatin in children under 18 years of age have not been established, therefore, Zetori is not recommended for patients in this age group. Effect on driving and operating machinery The effect of rosuvastatin on the ability to drive and operate machinery has not been studied, but considering its pharmacodynamic properties, it should not have an effect. The possibility of dizziness during therapy should be considered. Pregnancy and lactation Use of Zetori during pregnancy and lactation is contraindicated. Women of reproductive age should use adequate contraception methods. If pregnancy occurs during therapy, the drug should be discontinued immediately. There is no data on the excretion of rosuvastatin in breast milk. Therefore, breastfeeding should be discontinued immediately if the drug is taken. Overdose Simultaneous intake of several daily doses does not change the pharmacokinetic parameters of rosuvastatin. Treatment: There is no specific antidote. Symptomatic treatment and maintenance of vital organ and system functions are recommended. Liver function and creatine phosphokinase levels should be monitored. Hemodialysis is not effective. Drug Interactions Concomitant administration of rosuvastatin and cyclosporine increases rosuvastatin concentration in plasma. Rosuvastatin in combination with vitamin K antagonists (e.g., warfarin) may increase prothrombin time. Combined use of rosuvastatin and gemfibrozil leads to a twofold increase in the maximum concentration and AUC of rosuvastatin in blood plasma. No clinically significant pharmacokinetic interactions are expected with fenofibrates, although pharmacodynamic interactions are possible. Gemfibrozil, other fibrates, and lipid-lowering doses of nicotinic acid, when used concomitantly with HMG-CoA reductase inhibitors, increase the risk of myopathy, which is also observed with monotherapy. Therefore, in combination with these drugs (at doses of 1 g/day or more), Zetori should be initiated at a dose of 5 mg. No change in pharmacokinetic parameters of either drug was observed during concomitant administration of rosuvastatin and ezetimibe. Although the exact mechanism of interaction is unknown, concomitant administration of protease inhibitors may lead to a significant increase in rosuvastatin exposure. Therefore, their concomitant use in patients with HIV infection is not recommended. Concomitant use of rosuvastatin and antacids containing aluminum and magnesium hydroxide suspension reduces plasma rosuvastatin content by approximately 50%. This effect is less pronounced if antacids are taken 2 hours after rosuvastatin. The clinical significance of such an interaction has not been studied. Erythromycin reduces plasma concentrations of rosuvastatin. This interaction may be due to erythromycin's enhancement of intestinal motility. Rosuvastatin increases plasma concentrations of oral contraceptives - ethinylestradiol and norgestrel. This should be considered when selecting the dose of oral contraceptives. This effect should also be considered during hormone replacement therapy. Clinically, no significant interaction between rosuvastatin and digoxin is expected. No clinically significant interactions between rosuvastatin and fluconazole and ketoconazole have been reported. Combined use of rosuvastatin and itraconazole increases rosuvastatin pharmacokinetics (clinically insignificant). Thus, interactions related to cytochrome P450 metabolism are not expected. Dosage and Administration The drug is administered orally at any time of the day, regardless of food intake. Tablets should be swallowed whole with water, not chewed or crushed. If a 5 mg dose is required, a 10 mg tablet should be divided in half. Before starting Zetori treatment, the patient should follow a standard hypolipidemic diet and continue to follow the diet during treatment. The dose of the drug should be selected individually, based on indications and response to treatment, as well as lipid levels recommendations. The recommended starting dose of Zetori for patients initiating treatment or switching from other HMG-CoA reductase inhibitors is 5-10 mg once daily. When selecting the starting dose, the cholesterol content and the possible risk of cardiovascular complications, as well as the risk of side effects, should be considered. If necessary, the dose can be increased after 4 weeks. Dose increases up to 40 mg should only be made in patients with severe hypercholesterolemia and a high risk of cardiovascular complications (especially in patients with familial hypercholesterolemia) who have not achieved the desired result with a 20 mg dose and who should be under specialist supervision. Patients receiving a 40 mg dose require constant monitoring, as side effects are expected. The 40 mg dose is not recommended for patients who have not previously consulted a specialist. Lipid metabolism parameters should be monitored 2-4 weeks after initiation and/or dose increase of Zetori, and the dose should be adjusted if necessary. Elderly patients do not require dose adjustment. Patients with mild to moderate renal insufficiency do not require dose adjustment. Rosuvastatin is contraindicated in patients with severe renal insufficiency (CrCl less than 30 ml/min). The drug is contraindicated at a dose of 40 mg in patients with moderate renal impairment (CrCl less than 60 ml/min). For patients with moderate renal impairment, a starting dose of Zetori 5 mg is recommended. In patients predisposed to myopathy, a dose of 40 mg is contraindicated. The recommended starting dose for patients in this group is 5 mg. Side Effects Side effects during Zetori administration are usually mild and resolve spontaneously. As with other HMG-CoA reductase inhibitors, the frequency of side effects is mainly dose-dependent. Allergic reactions: rarely - hypersensitivity reactions, urticaria; rarely - angioneurotic edema. Central nervous system: often - headache, dizziness; very rarely - polyneuropathy. Gastrointestinal tract: often - constipation, nausea, abdominal pain; sometimes - mild, asymptomatic dose-dependent increase in liver transaminase activity; rarely - pancreatitis; very rarely - jaundice, hepatitis, diarrhea. Dermatological reactions: sometimes - itching, rash. Musculoskeletal system: often - myalgia; rarely - myopathy (including myositis), rhabdomyolysis with or without acute renal failure. A dose-dependent increase in creatine phosphokinase levels is observed in a small number of patients taking rosuvastatin. The increase is usually mild, asymptomatic, and transient. If creatine phosphokinase levels increase (more than 5 times the upper limit of normal), therapy should be discontinued. Also - arthralgia. Urinary system: proteinuria; from minimal (trace) to "++" or more (<1% of patients taking 10-20 mg and about 3% of patients taking 40 mg). In most cases, proteinuria decreases or disappears completely during therapy and does not indicate the presence of acute or progressive kidney disease. Laboratory data: increased glucose and bilirubin concentrations, increased GGT and alkaline phosphatase activity. Miscellaneous: often - asthenic syndrome; possible thyroid dysfunction. Shelf life and storage conditions Shelf life - 3 years. Store at a temperature not exceeding 25°C. Keep out of reach of children! Dosage form Film-coated tablet 10 mg, 20 mg, or 40 mg; 30 tablets in blisters, secondary packaging - cardboard box. Dispensing category: Pharmaceutical product group II, dispensed by prescription #3.