Atoris, 30 pcs., 20 mg, film-coated tablets

Pharmacological properties of the drug Atoris

Lipid-lowering agent. The active ingredient of the drug - atorvastatin - reduces the level of TG, total cholesterol, LDL cholesterol and increases the level of HDL cholesterol in the blood. The mechanism of action of atorvastatin is due to inhibition of the activity of HMG-CoA reductase, an enzyme that catalyzes the conversion of HMG-CoA to mevalonic acid. This transformation is one of the initial stages of cholesterol synthesis in the body. Blockade of cholesterol synthesis by atorvastatin leads to an increase in the ability of receptors to bind LDL cholesterol in the liver and other organs. Atorvastatin reduces the formation of LDL, thereby reducing the level of cholesterol in the blood. Atorvastatin also slows down the secretion of VLDL cholesterol in the liver, which is the most likely mechanism for reducing TG levels in the blood, since the connection with apolipoprotein B is weakened and thereby their clearance increases. The mechanism of the effect of atorvastatin on increasing HDL cholesterol levels is not clear. In addition to the effect on plasma lipids, atorvastatin also has other effects that enhance its antiatherosclerotic effect. It inhibits the synthesis of isoprenoids - substances that cause proliferation of vascular smooth muscle cells. Reduces the viscosity of blood plasma and the activity of some coagulation and aggregation factors, thereby improving hemodynamics and promoting the balance of blood coagulation processes. In addition, HMG-CoA reductase inhibitors affect the metabolism of macrophages - inhibiting their activation, reducing the rupture of atherosclerotic plaques. Atorvastatin is rapidly absorbed from the gastrointestinal tract by approximately 80%. The maximum concentration in blood plasma is reached after 1–4 hours. Eating reduces the absorption of atorvastatin, but this does not affect its effectiveness. The bioavailability of atorvastatin is low - only 12%, which is due to the intensity of the first round of metabolism. More than 98% of atorvastatin is bound to plasma proteins. Does not penetrate the BBB. The half-life is on average 14 hours, and the half-life of inhibitory activity towards the target enzyme is 20-30 hours. Approximately 46% of atorvastatin is excreted in the feces and less than 2% in the urine.

Description of the dosage form

Tablets, 10 and 20 mg: round, slightly biconvex, white film-coated. Fracture appearance: white rough mass with a white or almost white film shell.

Tablets, 30 mg: round, slightly biconvex, film-coated, white or almost white, with a bevel.

Tablets, 60 mg: oval, biconvex, film-coated, white or almost white.

Tablets, 80 mg: capsule-shaped, biconvex, film-coated, white or almost white.

Tablets, 40 mg: round, slightly biconvex, white or almost white film-coated. Fracture appearance: white rough mass with a white or almost white film shell.

Use of the drug Atoris

Before prescribing Atoris, the patient should be placed on a low-lipid diet, which he must adhere to throughout the course of drug therapy. The recommended starting dose of Atoris is 1 tablet (10 mg) per day. If necessary, you can increase the daily dose of Atoris to 80 mg. The drug is taken once a day at the same time, before or after meals. The effect is observed after 2 weeks of treatment, the maximum - after 4 weeks. After 2–4 weeks from the start of treatment, it is necessary to take a lipid profile and adjust the dose based on its indicators. Primary (heterozygous familial or polygenic) hypercholesterolemia (type IIa) and mixed hyperlipidemia (type IIb) Treatment begins with the recommended initial dose (10 mg) per day, which is increased if necessary after 4 weeks (depending on the patient’s response). The maximum daily dose is 80 mg. Heterozygous familial hypercholesterolemia in children over 10 years of age It is recommended to prescribe an initial dose of 10 mg once daily. The maximum recommended dose is 20 mg once daily (doses greater than 20 mg have not been studied in patients in this age group). The dose is selected individually, dose adjustment can be carried out at intervals of 4 weeks or more. Homozygous familial hypercholesterolemia Adults: Dosage range is the same as for other forms of hyperlipidemia. The initial dose is adjusted depending on the condition of the disease. In most patients with homozygous familial hypercholesterolemia, the optimal effect is observed at a daily dose of 80 mg. Atoris is used as an adjuvant therapy with other treatments (plasmaphoresis) or as primary therapy if treatment with other methods is not possible. There is no need to reduce recommended doses in elderly patients and patients with impaired renal function. Patients with impaired liver function should use the drug with caution due to the slow elimination of atorvastatin from the body. Clinical and laboratory parameters should be constantly monitored; if pathological changes occur, the dose should be reduced or treatment should be stopped.

Nosological classification (ICD-10)

• E14 Diabetes mellitus, unspecified
• E78 Disorders of lipoprotein metabolism and other lipidemias
• E78.0 Pure hypercholesterolemia
• E78.1 Pure hyperglyceridemia
• E78.2 Mixed hyperlipidemia
• E78.5 Hyperlipidemia, unspecified
• E78.9 Disorders of lipoprotein metabolism, unspecified
• I10 Essential (primary) hypertension
• I15 Secondary hypertension
• I20.9 Angina pectoris, unspecified
• I21.9 Acute myocardial infarction, unspecified
• I25.9 Chronic ischemic heart disease, unspecified
• I64 Stroke not specified as hemorrhage or infarction
• Z72.0 Tobacco use
• Z82.4 Family history of coronary heart disease and other diseases of the cardiovascular system

Side effects of the drug Atoris

Side effects are minor and temporary in most patients. From the immune system: very rarely - allergic reactions. Metabolic and nutritional disorders: very rarely - anorexia. From the reproductive system: very rarely - impotence. From the central nervous system: insomnia, headache; very rarely - paresthesia, peripheral neuropathy, dizziness. From the respiratory system, chest and mediastinum: very rarely - chest pain. From the gastrointestinal tract: constipation, flatulence, dyspepsia, nausea, diarrhea, abdominal pain; very rarely - vomiting, pancreatitis. From the hepatobiliary system: very rarely - hepatitis, cholestasis. From the skin and subcutaneous tissues: very rarely - angioedema, rash, pruritis, alopecia. From the musculoskeletal system and connective tissue: myalgia, muscle weakness; very rarely - myopathy, muscle cramps, myositis. General disorders: asthenia. Violation of laboratory parameters: increased level of creatine kinase (CPK) in the blood; rarely - increased levels of liver transaminases (ALAT, AST), increased or decreased blood glucose levels. The increase in transaminase levels in blood plasma is dose-dependent. An increase in creatine kinase levels greater than 10 times the normal value was observed in 0.4% of patients. 0.1% of these patients experienced muscle pain, tenderness, or muscle weakness. If severe side effects are observed, treatment with the drug should be stopped.

Release form

Film-coated tablets, 10 mg and 20 mg. 10 pcs. in a blister made of a combined material polyamide/aluminum foil/PVC-aluminum foil. 1, 3, 6 or 9 bl. in a cardboard box.

When packaging at the Russian enterprise KRKA-RUS LLC and Vector-Medica CJSC: 1, 3, 6 or 9 bl. in a cardboard pack.

Film-coated tablets, 30 mg, 60 mg and 80 mg. 10 pcs. in a blister made of a combined material of oriented polyamide/aluminum/PVC-aluminum foil. 3, 6 or 9 bl. in a cardboard pack.

Film-coated tablets, 40 mg. 10 pcs. in a blister (blister pack) made of a combined material polyamide/aluminum foil/PVC-aluminum foil. 1, 3, 6 or 9 bl. in a cardboard pack.

When packaging at the Russian enterprise KRKA-RUS LLC: 1, 3, 6 or 9 bl. in a cardboard pack.

In production at KRKA-RUS LLC, Russia: 10 tablets each. in a blister pack (blister) made of a combined material polyamide/aluminum foil/PVC in accordance with GOST 52145-2003 and aluminum foil in accordance with GOST 745-2003, or TU 48-21-270-94, or according to the specifications of JSC KRKA, d.d. , Novo Mesto”, Slovenia (Coldforming OPA/Al/PVC-Al).

1, 3, 6 or 9 blister packs (blisters) are placed in a cardboard pack in accordance with GOST 7933-89.

Special instructions for the use of the drug Atoris

Prescribe with caution to patients who abuse alcohol or have a history of liver disease. During treatment with Atoris, an increase in the activity of liver enzymes may be observed. Such an increase is in most cases insignificant and has no clinical significance; however, it is recommended to monitor the activity of liver enzymes before starting treatment and regularly during treatment. If ALT and/or AST levels exceed normal levels by more than 3 times, treatment with atorvastatin should be discontinued. Atorvastatin is not recommended for use in women of reproductive age who do not use reliable methods of contraception. If during treatment with Atoris the patient decides to become pregnant, she must stop taking the drug no later than a month before the planned pregnancy. Treatment with atorvastatin may be associated with a risk of myopathy, rhabdomyolysis and renal dysfunction. The risk of such a complication increases when taking one or a combination of several drugs in parallel: fibric acid derivatives, niacin, cyclosporine, nefazodone, some antibiotics, azole antifungals and HIV protease inhibitors. If there are symptoms of myopathy, it is recommended to determine the activity of CPK in the blood serum. If it increases significantly, treatment should be stopped. The possibility of increased CPK activity in the blood serum during treatment with Atoris should also be paid attention to in the differential diagnosis of chest pain. If myopathy develops, followed by rhabdomyolysis and acute renal failure (a rare but extremely undesirable side effect), the drug is immediately discontinued and diuretics and sodium bicarbonate are prescribed. If necessary, hemodialysis is started. Rhabdomyolysis can lead to hyperkalemia, which is corrected by intravenous infusion of calcium chloride or calcium gluconate, glucose with insulin, and the use of ion exchange resins. Since atorvastatin is mainly bound to plasma proteins, hemodialysis is ineffective.

Contraindications

hypersensitivity to any of the components of the drug;

liver diseases in the active stage (including active chronic hepatitis, chronic alcoholic hepatitis);

liver failure;

liver cirrhosis of any etiology;

increased activity of liver transaminases of unknown origin by more than 3 times compared to ULN;

skeletal muscle diseases;

lactase deficiency, lactose intolerance, glucose-galactose malabsorption syndrome;

pregnancy and breastfeeding;

age under 18 years (efficacy and safety of use have not been established).

With caution: alcoholism; history of liver disease.

Drug interactions Atoris

When taking Atoris simultaneously with cyclosporine, antibiotics (erythromycin, clarithromycin, quinupristin/dalfopristin), protease inhibitors (amprenavir, indinavir, ritonavir), antifungals (fluconazole, ketoconazole, itraconazole) or nefazodone, an increase in Atoris serum levels may occur, which may cause myopathy with rhabdomyolysis and renal dysfunction. All of these drugs inhibit the P450 (CYP) 3A4 enzyme, which is involved in the metabolism of Atoris. Concomitant use of Atoris with fibric acid derivatives or niacin may increase Atoris serum levels. Phenytoin is a P450 (CYP) 3A4 inducer, so its simultaneous use with Atoris may reduce the effectiveness of the latter. Parallel use of atorvastatin and antacids (suspension of magnesium and aluminum hydroxide) reduces the level of atorvastatin in the blood plasma by 35%, but this does not significantly affect its effectiveness. When atorvastatin and colestipol are taken simultaneously, the plasma level of atorvastatin is reduced by 25%, but the therapeutic effect of this combination exceeds that of atorvastatin alone. In patients taking 80 mg of atorvastatin and digoxin simultaneously, plasma digoxin levels increase by approximately 20%. Parallel use of Atoris and oral contraceptives (norethindrone, ethinyl estradiol) can enhance the absorption of the latter and increase their level in the blood plasma. Concomitant use of atorvastatin and warfarin may enhance the effect of the latter on blood coagulation parameters. In a clinical study, concurrent use of these drugs led to a temporary decrease in prothrombin time in the first days of treatment. After 15 days of therapy, the prothrombin time value returned to the level determined before the start of parallel treatment. Drinking grapefruit juice during treatment with Atoris may increase the level of the latter in the blood plasma.

Compound

Manufacturer

1. JSC "KRKA, d.d., Novo Mesto". Šmarješka cesta 6, 8501 Novo Mesto, Slovenia.

When packaging and/or packaging at a Russian enterprise, the following is indicated: KRKA-RUS LLC. 143500, Russia, Moscow region, Istra, st. Moskovskaya, 50.

Tel.; Fax.

or

CJSC "Vector-Medica", 630559, Russia, Novosibirsk region, Novosibirsk district, settlement. Koltsovo, bldg. 13, bldg. 15.

Tel/fax

2. LLC "KRKA-RUS", 143500, Russia, Moscow region, Istra, st. Moskovskaya, 50; in cooperation with JSC "KRKA, d.d., Novo Mesto".

Tel.; Fax.

Representative office of JSC "KRKA, d.d., Novo Mesto" in the Russian Federation/organization receiving consumer complaints: 125212, Moscow, Golovinskoye Shosse, 5, bldg. 1, fl. 22.

Tel.; Fax.