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Active ingredients
Atorvastatin
Release form
Pills
Composition
Active ingredient: Atorvastatin (Atorvastatin) Concentration of the active substance (mg): 10
Pharmacological effect
Lipid-lowering agent from the group of statins. According to the principle of competitive antagonism, the statin molecule binds to the part of the coenzyme A receptor where HMG-CoA reductase is attached. Another part of the statin molecule inhibits the conversion of hydroxymethylglutarate to mevalonate, an intermediate product in the synthesis of the cholesterol molecule. Inhibition of HMG-CoA reductase activity leads to a series of consecutive reactions, which result in lowering the intracellular cholesterol content and a compensatory increase in the activity of LDL receptors and, accordingly, acceleration of cholesterol catabolism (Xc) of LDL. Hypolipidemic effect of statins is associated with a decrease in total Xc due to Xc -LPNP. A decrease in the level of LDL is dose-dependent and is not linear, but exponential. Atorvastatin's inhibitory effect on HMG-CoA reductase is approximately 70% determined by the activity of its circulating metabolites. 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 TG level is secondary and indirectly through their main effects on reducing the level of LDL-C. A moderate decrease in the level of TG in the treatment with statins seems to be associated with the expression of the remnant (apo E) receptors on the surface of hepatocytes involved in the catabolism of LPPP, which are approximately 30% TG. Compared with other statins (with the exception of rosuvastatin), atorvastatin causes a more pronounced decrease in TG level. In addition to the lipid-lowering action, statins have a positive effect on endothelial dysfunction (preclinical sign of early atherosclerosis), on the vascular wall, atheroma, improve the rheological properties of blood, have antioxidant , antiproliferative properties. Atorvastatin reduces cholesterol levels in patients with homozygous familial hypercholesterolemia, which usually does not respond I am treating hypolipidemic agents.
Pharmacokinetics
Atorvastatin is rapidly absorbed from the gastrointestinal tract.Absolute bioavailability is low - about 12%, due to presystemic clearance in the gastrointestinal mucosa and / or due to the first passage through the liver, mainly at the site of action. Atorvastatin is metabolized with the participation of the CYP3A4 isoenzyme to form a number of substances that are HMG-CoA reductase inhibitors. T1 / 2 from plasma is about 14 hours, although T1 / 2 inhibitor of HMG-CoA reductase activity is approximately 20-30 hours, due to the participation of active metabolites. Binding to plasma proteins is 98%. Atorvas Atin displayed advantageously in the form of metabolites in the bile.
Indications
Increased nervous irritability, insomnia, irritability.
Contraindications
Hypersensitivity to any of the components of the drug. Liver diseases in the active stage (including active chronic hepatitis, chronic alcoholic hepatitis). Hepatic insufficiency. Liver cirrhosis of any etiology. Increased activity of hepatic transaminases of unclear genesis more than 3 times compared to VGN.Skeletal muscle diseases. Lactase deficiency, lactose intolerance, glucose-galactose malabsorption syndrome. Pregnancy and breastfeeding period. Age up to 18 years (efficacy and safety applied I did not set) .With caution: alcoholism; liver disease in history.
Use during pregnancy and lactation
C caution should be used in patients who abuse alcohol; with indications of a history of liver disease. Before and during treatment with atorvastatin, especially when symptoms of liver damage appear, it is necessary to monitor indicators of liver function. With an increase in the level of transaminases, their activity should be monitored until normalization. If the activity of AST or ALT, more than 3 times higher than normal, remains, it is recommended to reduce the dose or cancel atorvastatin. When the symptoms of myopathy appear during the treatment, the activity of CPK should be determined. If a significant increase in the level of CPK is maintained, then it is recommended to reduce the dose or stop atorvastatin. The risk of myopathy during treatment with atorvastatin is increased while using cyclosporine, fibrates, erythromycin, antifungal drugs related to azoles,And niacin , impotence, hyperglycemia and hypoglycemia. In children, experience with atorvastatin at a dose of up to 80 mg / day is limited. Atorvastatin is used with caution in patients with chronic alcoholism.
Dosage and administration
Inside, regardless of food intake. Before the patient starts to use Atoris, the patient should be transferred to a diet that will reduce the concentration of lipids in the blood, which must be observed throughout the entire therapy with the drug. Before starting therapy, you should try to control hypercholesterolemia through exercise and weight loss in patients with obesity, as well as therapy of the underlying disease. Treatment begins with a recommended initial dose of 10 mg. The dose of the drug varies from 10 to 80 mg 1 time per day and is selected based on the initial concentration of LDL-C, the goal of therapy and individual therapeutic effect. The Atoris preparation can be taken once at any time of the day, but at the same time every day. The therapeutic effect is observed after 2 weeks of treatment, and the maximum effect develops after 4 weeks. Therefore, the dosage should not be changed earlier than 4 weeks after the start of the use of the drug in the previous dose. At the beginning of therapy and / or during the dose increase, plasma concentrations of lipids in the blood plasma should be monitored every 2-4 weeks and the dose should be adjusted accordingly. and polygenic) hypercholesterolemia (type IIa) and mixed hyperlipidemia (type IIb): treatment begins with the recommended initial dose, which is increased after 4 weeks, depending on the response of the patient. The maximum daily dose is 80 mg. Homozygous hereditary hypercholesterolemia: the dose range is the same as with other types of hyperlipidemia. The initial dose is selected individually, depending on the severity of the disease. In most patients with homozygous hereditary hypercholesterolemia, the optimal effect is observed when using the drug in a daily dose of 80 mg (once).The drug Atoris is used as an additional therapy to other methods of treatment (plasmapheresis) or as the main treatment if therapy with the help of other methods is not possible. Special groups of patients. Elderly patients. Elderly patients should not change the dose of Atoris. Renal dysfunction. Does not affect the concentration of atorvastatin in the blood plasma or the degree of decrease in the concentration of cholesterol-LDL when using atorvastatin, therefore, changing the dose of the drug is not required. Violation of the liver function. Patients with impaired liver function requires caution (due to the slowing down of the drug from the body). In such a situation, clinical and laboratory parameters should be closely monitored (regular monitoring of the activity of ACT and ALT). With a significant increase in hepatic transaminases, the dose of Atoris should be reduced or treatment should be discontinued. Use in combination with other HP. If necessary, the daily dose of Atoris should be used simultaneously with cyclosporine should not exceed 10 mg.
Side effects
When applied simultaneously with atorvastatin significantly increases the concentration of digoxin in krovi.Diltiazem plasma digoxin, verapamil, isradipine inhibit isozyme CYP3A4, which is involved in the metabolism of atorvastatin, therefore, while the application of these calcium channel blockers may increase the concentration of atorvastatin in the blood plasma and increased risk of myopathy .At the simultaneous use of itraconazole, the concentration of atorvastatin in the blood plasma significantly increases, apparently due to gibirovaniya itraconazole its metabolism in the liver, which occurs with the participation isozyme CYP3A4; increasing the risk of myopathy. With simultaneous use of colestipol, a decrease in plasma plasma levels of atorvastatin is possible, and the hypolipidemic effect increases. When used simultaneously, antacids containing magnesium hydroxide and aluminum hydroxide reduce the concentration of atorvastatin by about 35%. When using cyclosporine, fibrates simultaneously ( including gemfibrozil), antifungal preparations of azole derivatives,nicotinic acid increases the risk of myopathy. With simultaneous use of erythromycin, clarithromycin, atorvastatin concentration in plasma increases moderately, the risk of myopathy increases. Concurrent use of ethinyl estradiol, norethisterone (norethindrone) slightly increases the concentration of ethinyl estradiol, norethisterone and cefacinosteel, norethysterone and noretinstrona, norethysterone and norethinone, norethisterone, and ethynestradiol, norethisterone and ethylene estradiol, norethysterone and norethindrone slightly increase the concentration of ethinyl estradiol, norethisterone and norethisterone. the use of protease inhibitors increases the concentration of atorvastatin in the blood plasma, because protease inhibitors are inhibitors of the CYP3A4 isoenzyme.
Interaction with other drugs
Precautionary measures
special instructions
CNS and peripheral nervous system: headache, dizziness, asthenic syndrome, insomnia or drowsiness, nightmares, amnesia, paresthesias, peripheral neuropathy, emotional lability, ataxia, hyperkinesia, depression, hypesthesia, weakness, malaise. On the part of the senses: amblyopia, tinnitus, dry conjunctiva, accommodation disturbance, hemorrhage in the eyes, deafness, glaucoma, parosmia, loss of taste sensations. For CVS: palpitations, vasodilation, migraine, postural hypotension, increased blood pressure, phlebitis, arrhythmia, chest pain, vasculitis. From the hematopoietic system: anemia, lymphadenopathy, thrombocytopenia. From the respiratory system: bronchitis, rhinitis, dyspnea, bronchial asthma, nasal bleeding. From the digestive system: nausea, heartburn, constipation or diarrhea, flatulence, gastralgia, abdominal pain, anorexia or increased appetite, dry mouth, belching, dysphagia, vomiting, stomatitis, esophagitis, glossitis, gastroenteritis, hepatitis, hepatic colic, cheilitis, duodenal ulcer, gastroenteritis, hepatitis, hepatic, hepatic, hepatic, hepatitis, duodenal ulcer jaundice, increased activity of liver enzymes, rectal bleeding, melena, bleeding gums, tenesmus. On the part of the musculoskeletal system: myalgia, arthralgia, back pain, joint swelling, myopathy, muscle cramps, myositis, rhabdomyolysis, tendopathy (in some cases with tendon rupture). From the genitourinary system: urogenital infections, dysuria (including pollakiuria, nocturia, urinary incontinence or urinary retention, imperative urination to urinate), cystitis, hematuria,vaginal bleeding, uterine bleeding, urolithiasis, metrorrhagia, epididymitis, decreased libido, impotence, impaired ejaculation. On the skin: sweating, eczema, seborrhea, ecchymosis. edema, anaphylaxis, erythema multiforme exudative, Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome). Laboratory values: increased activity of serum CPK, increased activity LT, ACT, hyperglycemia, gipoglikemiya.Prochie: peripheral edema, weight gain, fatigue, fever.