Description
Description
Round biconvex tablets, film-coated, light yellow in color with a brownish tint. On the cross section is the inner layer of a white or cream-white color.
Pharmacological action
Hypolipidemic agent from the group of statins. Selective competitive inhibitor of HMG-CoA reductase, an enzyme that converts 3-hydroxy-3-methylglutaryl coenzyme A to mevalonic acid, a precursor of sterols, including cholesterol. Triglycerides (TG) and cholesterol in the liver are included in the composition of very low density lipoproteins (VLDL), enter the blood plasma and are transported to peripheral tissues. Low density lipoproteins (LDL) are formed from VLDL during interaction with LDL receptors. Atorvastatin reduces plasma cholesterol and lipoprotein levels by inhibiting HMG-CoA reductase, the synthesis of cholesterol in the liver and an increase in the number of hepatic LDL receptors on the cell surface, leading to increased uptake and catabolism of LDL. Reduces the formation of LDL, causes a pronounced and persistent increase in the activity of LDL receptors. Decreases LDL levels in patients with homozygous familial hypercholesterolemia, which usually does not respond to therapy with lipid-lowering drugs. It reduces the level of total cholesterol by 30-46%, LDL – by 41-61%, apolipoprotein B – by 34-50% and TG – by 14-33% causes an increase in the level of HDL cholesterol (high density lipoproteins) and apolipoprotein A. Dose-dependent lowers LDL levels in patients with homozygous hereditary hypercholesterolemia, resistant to therapy with other lipid-lowering drugs.
Indications
Atorvastatin is used:
in combination with a diet to reduce elevated levels of total cholesterol, cholesterol / LDL, apolipoprotein B and triglycerides and increase HDL cholesterol in patients with primary hypercholesterolemia, heteroimenosis and heteroimenosis mixed heteroimenosis types IIa and IIb according to Fredrickson)
in combination with a diet for the treatment of patients with elevated serum levels of triglycerides (type IV Fredrickson) and patients with diabetes lipoproteinemia (Fredrickson type III), in which diet therapy does not provide an adequate
effect to lower total cholesterol and cholesterol / LDL levels in patients with homozygous familial hypercholesterolemia, when diet therapy and other non-pharmacological treatments are not effective
Recommendations for use of
Before prescribing Atorvastatin, the patient should be advised of a standard lipid-lowering diet, which he must continue to follow throughout the duration of therapy.
The initial dose is an average of 10 mg 1 time / day. The dose varies from 10 to 80 mg 1 time / day. The maximum daily dose of the drug is 80 mg.
The drug can be taken at any time of the day with food or regardless of the meal time. The dose is selected taking into account the initial levels of cholesterol / LDL, the purpose of therapy and individual effect. At the beginning of treatment and / or during an increase in the dose of Atorvastatin, it is necessary to monitor plasma lipid levels every 2-4 weeks and adjust the dose accordingly. To ensure the dosage regimen for the drug given below, it is possible to use the drug Atorvastatin in another dosage form: film-coated tablets of 10 and 20 mg.
With simultaneous use with cyclosporine, the daily dose of atorvastatin should not exceed 10 mg.
Primary hypercholesterolemia and mixed hyperlipidemia
In most cases, a dose of 10 mg of Atorvastatin once daily is sufficient. A significant therapeutic effect is observed after 2 weeks, as a rule, and the maximum therapeutic effect is usually observed after 4 weeks. With prolonged treatment, this effect persists.
The use of the drug in patients with renal failure and kidney disease does not affect the level of atorvastatin in the blood plasma or the degree of decrease in cholesterol / LDL when it is used, therefore, changing the dose of the drug is not required.
In case of hepatic insufficiency, the dose should be reduced (see section “With caution” and “Special instructions”).
When using the drug in elderly patients, there were no differences in safety, effectiveness or achievement of the goals of lipid-lowering therapy in comparison with the general population.
Special instructions
Before starting therapy with Atorvastatin, the patient must be prescribed a standard hypocholesterol diet, which he must follow during the entire period of treatment.
The use of HMG-CoA reductase inhibitors to lower blood lipids can lead to a change in biochemical parameters that reflect liver function. Liver function should be monitored before starting therapy, after 6 weeks, 12 weeks after starting atorvastatin and after each dose increase, as well as periodically, for example, every 6 months. An increase in the activity of liver enzymes in the blood serum can be observed during therapy with Atorvastatin. Patients with an increase in enzyme activity should be monitored until the enzyme levels return to normal. In the event that the values of alanine aminotransferase (ALT) or aspartic aminotransferase (AST) are more than 3 times the level of the upper acceptable limit, it is recommended to reduce the dose of Atorvastatin or stop treatment.
Atorvastatin should be used with caution in patients who abuse alcohol and / or have liver disease. Active liver disease or a persistent increase in the activity of aminotransferases of unknown origin serve as contraindications to the appointment of Atorvastatin.
Treatment with atorvastatin may cause myopathy. The diagnosis of myopathy (muscle pain and weakness in combination with an increase in the activity of creatine phosphokinase (CPK) by more than 10 times compared with the upper limit of the norm) should be discussed in patients with common myalgia, pain or muscle weakness and / or a marked increase in CPK activity. Patients should be warned that they should immediately inform the doctor about the appearance of unexplained pain or weakness in the muscles if they are accompanied by malaise or fever. Atorvastatin therapy should be discontinued if there is a marked increase in CPK activity or in the presence of confirmed or suspected myopathy. The risk of myopathy in the treatment of other drugs of this class increased with the simultaneous use of cyclosporine, fibrates, erythromycin, nicotinic acid or antifungal agents derived from azole. Many of these drugs inhibit the metabolism mediated by cytochrome P450 3A4 and / or drug transport. Atorvastatin is biotransformed under the influence of CYP 3A4. When prescribing atorvastatin in combination with fibrates, erythromycin, immunosuppressive agents, antifungal agents, azole derivatives or nicotinic acid in hypolipidemic doses, the expected benefit and risk of treatment should be carefully weighed and patients should be regularly observed to detect muscle pain or weakness, especially during the first months treatment and during periods of increasing doses of any drug. In such situations, periodic determination of CPK activity can be recommended, although such control does not prevent the development of severe myopathy.
When using Atorvastatin, as well as other drugs of this class, cases of rhabdomyolysis with acute renal failure due to myoglobinuria are described. Atorvastatin therapy should be temporarily discontinued or completely discontinued if there are signs of a possible myopathy or a risk factor for the development of renal failure due to rhabdomyolysis (for example, severe acute infection, arterial hypotension, serious surgery, trauma, severe metabolic, endocrine and electrolyte disturbances and uncontrolled seizures).
Before starting atorvastatin therapy, it is necessary to try to achieve control of hypercholesterolemia by adequate diet therapy, increase physical activity, weight loss in patients with obesity and treatment of other conditions.
Patients should be warned that they should immediately consult a doctor if unexplained muscle pain or weakness occurs, especially if they are accompanied by malaise or fever.
Influence on the ability to drive and operate machinery
Care must be taken when driving and operating machinery, as there is a risk of dizziness.
Composition
1 film-coated tablet contains:
active substance: atorvastatin calcium trihydrate – 43.4 mg, which corresponds to 40 mg of atorvastatin
excipients: calcium carbonate 35.4 mg, microcrystalline cellulose 24.0 mg, StarKap1500 [corn starch and pregelatinized starch] 53.6 mg, colloidal silicon dioxide (aerosil) 400 Ñg, talc 1.6 mg, magnesium stearate 1.6 mg, opadry II (85 series) (polyvinyl alcohol 2.56 mg, macrogol 1.29 mg, talc 0.94 mg, titanium dioxide 1.56 mg, dye iron oxide yellow 0.032 / mg, dye iron oxide red 0.00128 mg) 6.4 mg.
Side effects
From the nervous system – more often 1% – insomnia, dizziness less than 1% – headache, asthenia, malaise, drowsiness, nightmares, paresthesia, peripheral neuropathy, amnesia, emotional lability, ataxia, paralysis , depression, hyperesthesia, loss of consciousness.
On the part of the sensory organs: less than 1% – amblyopia, tinnitus, dryness of the conjunctiva, disturbance of accommodation, hemorrhage in the eyes, deafness, glaucoma, parosmia, loss of taste, perversion of taste.
From the cardiovascular system: more often 1% – chest pain less than 1% – palpitations, vasodilation, migraine, orthostatic hypotension, increased blood pressure, phlebitis, arrhythmia, angina pectoris.
From the hemopoietic system: less than 1% – anemia, lymphadenopathy, thrombocytopenia, leukocyturia.
From the respiratory system: more often 1% – bronchitis, rhinitis less often 1% – pneumonia, dyspnea, bronchial asthma, nosebleeds.
From the digestive system: more often 1% – nausea less than 1% – heartburn, constipation or diarrhea, flatulence, gastralgia, abdominal pain, anorexia, decreased or increased appetite, dry oral mucosa, belching, dysphagia, vomiting, stomatitis, esophagitis, glossitis, erosive and ulcerative lesions of the oral mucosa, gastroenteritis, hepatitis, biliary colic, cheilitis, duodenal ulcer, pancreatitis, cholestatic jaundice, impaired liver function, rectal bleeding, melena, bleeding gums, tenesmus.
From the side of the musculoskeletal system: more often 1% – arthritis less than 1% – leg muscle cramps, bursitis, tendosynovitis, myositis, myopathy, arthralgia, myalgia, rhabdomyolysis, torticollis, muscle hypertonicity, joint contracture, joint swelling, tendonopathy (in some cases with tendon rupture).
From the genitourinary system: more often 1% – urogenital infections, peripheral edema less than 1% – dysuria (including pollakiuria, nocturia, urinary incontinence or urinary retention, imperative urination), nephritis, hematuria, vaginal bleeding, nephrosis , metrorrhagia, epididymitis, decreased libido, impotence, impaired ejaculation.
From the skin: more often 1% – alopecia, xeroderma, increased sweating, eczema, seborrhea, ecchymosis, petechiae.
Allergic reactions: less than 1% – itching, skin rash, contact dermatitis, rarely – urticaria, angioedema, localized edema, photosensitivity, anaphylaxis, erythema multiforme exudative (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell’s syndrome).
Laboratory indicators: less than 1% – hyperglycemia, hypoglycemia, increased serum CPK, albuminuria.
Other: less than 1% – weight gain, gynecomastia, mastodynia, exacerbation of gout.
Overdose
Treatment: there is no specific antidote, symptomatic therapy is carried out.
Hemodialysis is ineffective.
Storage conditions
In a dry, dark place at a temperature of no higher than 25 ° C.
Keep out of the reach of children.
The Expiration of
is 3 years. Do not use after the expiry date stated on the packaging.
Deystvuyuschee substances
Atorvastatin
Form of Treatment
tablets
