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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
- gastroesophageal reflux disease (GERD), incl. Erosive and ulcerative reflux esophagitis and symptoms associated with GERD (heartburn, acid regurgitation, pain when swallowing); - erosive and ulcerative lesions of the stomach and duodenum associated with NSAIDs; stomach ulcer and duodenal ulcer, treatment and prevention. eradication of Helicobacter pylori in combination with two antibiotics - Zollinger-Ellison syndrome and other pathological conditions associated with increased gastric secretion.
Contraindications
Hypersensitivity to any of the components of the drug, liver disease in the active stage (including active chronic hepatitis, chronic alcoholic hepatitis), liver failure, liver cirrhosis of any etiology, increased activity of “liver” transaminases of obscure genesis, skeletal muscle disease, pregnancy and lactation period; age up to 18 years (efficacy and safety of use has not been established)
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 CPK levels is maintained, 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. in all cases, a clear connection was established with atorvastatin administration: muscle cramps, myositis, myopathy, paresthesia, peripheral neuropathy, pancreatitis, hepatitis, cholestatic jaundice, anorexia, vomiting, alopecia, pruritus, rash, impotence, hyperglycemia, and hypoglycemia. Children experience atorvastatin up to 80 mg / day is limited. Atorvastatin is used with caution in patients with chronic alcoholism.
Dosage and administration
Before starting treatment with Atoris, the patient should be transferred to a diet ensuring a reduction in the lipid content in the blood, which must be observed during drug therapy. The drug is taken orally, on an empty stomach or after a meal. The recommended starting dose is 10 mg daily. Depending on the desired effect, the daily dose may be increased to 80 mg. Atoris can be taken once at any time of the day, but at the same time every day. A significant therapeutic effect is observed after two weeks of treatment, and the maximum effect develops after four weeks. Therefore, the dosage should not be changed earlier than four weeks after starting the drug in the previous dose. Primary (heterozygous hereditary and polygenic) hypercholesterolemia (type IIa) and mixed hyperlipidemia (type IIb) Treatment begins with the recommended initial dose, which is increased after four weeks depending on the response of the patient. The maximum daily dose is 80 mg. Homozygous hereditary hypercholesterolemia The range of doses 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 was observed when using the drug in a daily dose of 80 mg (once). 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 impossible. In elderly people and patients with kidney diseases, the dose of Atoris should not be changed. Patients with impaired liver function must be cautious in connection with slowing the elimination of the drug from the body. In such a situation, clinical and laboratory findings should be carefully monitored, and if significant pathological changes are detected, the dose should be reduced or treatment should be discontinued.
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 drugs derived azole, nicotinic acid increases the risk of myopathy. With the simultaneous use of Eritra Omycin, clarithromycin moderately increases plasma concentration of atorvastatin, increases the risk of myopathy. With simultaneous use of ethinyl estradiol, norethisterone (norethindrone), the concentration of ethinyl estradiol, norethisterone and (norethindrone) in the blood plasma slightly increases. because protease inhibitors are inhibitors of the CYP3A4 isoenzyme.
Interaction with other drugs
Precautionary measures
special instructions
Nervous system disorders: headache, dizziness, asthenic syndrome, insomnia or drowsiness, nightmares, amnesia, paresthesias, peripheral neuropathy, emotional lability, ataxia, hyperkinesis, depression, hyperesthesia. From the senses: amblyopia, tinnitus, dry conjunctiva, disturbed accommodation, bleeding in the eyes, deafness, glaucoma, parosmia, loss of taste. Since the cardiovascular system: palpitations, vasodilation, migraine, postural hypotension, increased blood pressure, phlebitis, arrhythmia; From the hemopoietic system: anemia, lymphadenopathy, thrombocytopenia. On the part of the respiratory system: bronchitis, rhinitis, dyspnea, bronchial asthma, nosebleeds. On the part of 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, chyne duodenal ulcer, pancreatitis, cholestatic jaundice, increased activity of liver enzymes, rectal bleeding, melena, gingival bleeding, tenesmus. On the part of the musculoskeletal system: arthritis, leg muscle cramps, bursitis, myositis, myopathy, arthralgia, myalgia, rhabdomyolysis, joint contractures. On the part of the genitourinary system: urogenital infections, dysuria (including pollakiuria, nocturia, urinary incontinence or urinary retention, urgency to urinate), cystitis, hematuria, vaginal bleeding, uterine bleeding, urolithiasis, metrorrhagia, epididymide. , impotence, impaired ejaculation. On the part of the skin: alopecia, sweating, eczema, seborrhea, ecchimatosis. Allergic reactions: pruritus, skin rash, contact dermatitis, rarely urticaria, angioedema, facial edema, photosensitization, anaphylaxis, erythema multiforme exudative, Stephen-Johnson syndrome, toxic epidermal necrolysis (Layel syndrome). Laboratory indicators: hyperglycemia, hypoglycemia, increased serum CPK, albuminuria, increased activity of ALT, ACT Others: peripheral edema, weight gain, gynecomastia, exacerbation of gout.