Description
Release form dry-open srdlfrd pdf47 colors, round, biconvex in cross section, the core of the tablet is white or almost white.
Indications
– in combination with a diet to reduce elevated levels of total Chs, Chs-LDL, apolipoprotein B and TG and increase the levels of Chs-HDL in patients with primary hypercholesterolemia, heterozygous familial and non-familial hypercholesterolemia (combined type II) and IIb according to Fredrickson)
– in combination with a diet for the treatment of patients with elevated serum TG levels (type IV according to Fredrickson) and patients with dysbetalipoproteinemia (type III according to Fredrickson), in which diet therapy does not give an adequate effect of
– to reduce the levels of total Chs and Chs-LDL in patients with homozygous familial hypercholesterolemia, when diet therapy and other non-pharmacological methods of treatment are not effective enough.
Contraindications
– active liver disease
– increased activity of liver enzymes of unclear origin (more than 3 times compared with HBV)
– liver failure (classes A and B on the Child-Pugh scale)
– pregnancy lactation srdlpk – age under 18 years (effectiveness and safety have not been established)
– hypersensitivity to the components of the drug.
Caution should be used in patients with chronic alcoholism, with a history of liver disease, severe electrolyte imbalance, endocrine and metabolic disorders, arterial hypotension, severe acute infections (sepsis), uncontrolled epilepsy, extensive surgery, injuries, skeletal muscle diseases .
Use during pregnancy and lactation
Atorvastatin is contraindicated in pregnancy and lactation (breastfeeding).
It is not known whether atorvastatin is excreted in breast milk. Given the possibility of adverse events in infants, if necessary, use of the drug during lactation should decide on the termination of breastfeeding.
Women of reproductive age should use adequate contraceptive methods during treatment. Atorvastatin can be prescribed to women of reproductive age only if their probability of pregnancy is very low, and the patient is informed about the possible risk of treatment for the fetus.
Special instructions
Before starting atorvastatin therapy, it is necessary to try to achieve control of hypercholesterolemia by adequate diet therapy, increased physical activity, weight loss in patients with obesity and treatment of other conditions. Patients must observe a hypocholesterol diet during the entire treatment period.
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, 6 weeks, 12 weeks after starting atorvastatin and after each dose increase, and periodically, for example, every 6 months. An increase in the activity of hepatic enzymes in the blood serum can be observed during therapy with atorvastatin. In such cases, the condition of patients should be monitored until the activity of liver enzymes is normalized. If the ALT or ACT values are more than 3 times higher than VGN, it is recommended to reduce the dose of Atorvastatin or stop treatment. 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. Patients with common myalgia, muscle soreness or weakness, and / or a marked increase in CPK activity have a chance of developing myopathy (muscle pain and weakness in combination with an increase in CPK activity by more than 10 times compared with VGN). 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 azole antifungal agents. Many of these drugs inhibit CYP3A4 isoenzyme metabolism and / or drug transport. Atorvastatin is biotransformed by CYP3A4. When prescribing atorvastatin in combination with fibrates, erythromycin, immunosuppressants, azole antifungal agents or nicotinic acid in hypolipidemic doses, the expected benefit and risk of treatment should be carefully weighed and patients should be monitored regularly to detect muscle pain or weakness, especially during the first months of 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).
Patients should be warned that they should immediately consult a doctor if unexplained pain or muscle weakness occurs, especially if you feel unwell or have a fever.
Influence on the ability to drive vehicles and operate machinery
Patients should be careful when driving or operating machinery. when using Atorvastatin, there is a risk of dizziness.
In case of impaired renal function
In patients with renal failure and kidney disease, the concentration of atorvastatin in the blood plasma does not change, the degree of decrease in LDL cholesterol remains, therefore, changing the dose of the drug is not required.
In case of impaired liver function
The drug is contraindicated in active liver diseases, increased activity of liver enzymes of unknown origin (more than 3 times compared with VGN) with liver failure (Child-Pugh classes A and B).
In case of liver failure, the dose should be reduced.
Use in childhood
Contraindicated in children under 18 years of age (efficacy and safety not established).
Composition of
active substance: atorvastatin calcium in terms of atorvastatin – 20 mg
excipients (core): lactose monohydrate (milk sugar) – 124.0 mg calcium carbonate – 66.0 mg povidone K 30 (polyvinylpyrrolidone – average molecular weight) , 0 mg croscarmellose sodium (primellose) – 13.5 mg sodium stearyl fumarate – 3, 0 mg silicon colloidal dioxide (Aerosil) – 1.5 mg microcrystalline cellulose – 60.0 mg
excipients (shell): Opadry II (polyvinyl alcohol, partially hydrolyzed – 3.96 mg macrogol (polyethylene glycol) 3350 – 1.1115 mg talc – 1.8 mg of titanium dioxide E 171 – 1.7253 mg soy lecithin E 322 – 0.315 mg dye-based aluminum varnish indigo carmine – 0.0054 mg dye-based aluminum varnish – azorubine – 0.0459 mg dye-based aluminum varnish [Ponceau 4R] – 0.0369 mg).
Dosage and administration of
Before prescribing atorvastatin, the patient should be advised of a standard lipid-lowering diet, which he must follow throughout the treatment period.
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 LDL-C, the purpose of therapy and the 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.
The initial dose is on average 10 mg 1 time / day and subsequently varies from 10 mg to 80 mg 1 time / day.
With simultaneous use with cyclosporine, the daily dose of atorvastatin should not exceed 10 mg.
With primary hypercholesterolemia and mixed hyperlipidemia with an increase in serum TG (Fredrickson type IV), as well as with dysbetalipoproteinemia (Fredrickson type III), in most cases, a dose of 10 mg 1 time / day is sufficient. A significant therapeutic effect is usually observed after 2 weeks, the maximum therapeutic effect is usually observed after 4 weeks. With prolonged treatment, this effect persists.
With homozygous familial hypercholesterolemia, the drug is prescribed in a dose of 80 mg (4 tablets of 20 mg) 1 time / day.
In patients with renal failure and kidney disease, the concentration of atorvastatin in the blood plasma does not change, the degree of decrease in the content of LDL-C is maintained, therefore, a dose change is not required.
In case of liver failure, the dose should be reduced.
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.
Side effects of the
From the nervous system:> 1% – insomnia, dizziness <1% - headache, asthenia, malaise, drowsiness, nightmares, paresthesia, peripheral neuropathy, amnesia, emotional lability, ataxia, paralysis of the face , migraine, depression, hypesthesia, loss of consciousness. On the part of the sensory organs: <1% - amblyopia, tinnitus, dry conjunctiva, disturbed accommodation, hemorrhage in the retina, deafness, glaucoma, parosmia, loss of taste, perversion of taste. From the cardiovascular system:> 1% – chest pain <1% - heartbeat, symptoms of vasodilation, orthostatic hypotension, increased blood pressure, phlebitis, arrhythmia, angina pectoris. From the hemopoietic system: <1% - anemia, lymphadenopathy, thrombocytopenia. From the respiratory system:> 1% – bronchitis, rhinitis <1% - pneumonia, dyspnea, exacerbation of bronchial asthma, nosebleeds. From the digestive system:> 1% – nausea <1% - heartburn, constipation or diarrhea, flatulence, gastralgia, abdominal pain, decreased or increased appetite, dry mouth, 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 musculoskeletal system:> 1% – arthritis <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:> 1% – urogenital infections, peripheral edema <1% - dysuria (including pollakiuria, nocturia, urinary incontinence or urinary retention, mandatory urination), leukocyturia, nephritis, hematuria, vaginal bleeding , nephrourolithiasis, metrorrhagia, epididymitis, decreased libido, impotence, impaired ejaculation. Dermatological reactions:> 1% – alopecia, xeroderma, photosensitivity, increased sweating, eczema, seborrhea, ecchymosis, petechiae.
From the endocrine system: <1% - gynecomastia, mastodynia. From the side of metabolism: <1% - increase in body weight, exacerbation of gout. Allergic reactions: <1% - itchy skin, rash, contact dermatitis, rarely - urticaria, angioedema, facial edema, anaphylaxis, erythema multiforme exudative (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell syndrome ) Laboratory indicators: <1% - hyperglycemia, hypoglycemia, increased serum CPK, albuminuria. Drug interaction With the simultaneous use of atorvastatin with cyclosporine, HIV protease inhibitors (indinavir, ritonavir), antibiotics (erythromycin, clarithromycin, quinupristine / dalphopristine), antifungal drugs from itazonazole, nefazazole azole, acid, nicotinic acid or diltiazem, the concentration of atorvastatin in plasma increases, which increases the risk of developing myopathy with rhabdomyolysis and acute renal failure. With the simultaneous administration of Atorvastatin and a suspension containing magnesium hydroxide and aluminum hydroxide, the concentration of atorvastatin in the blood plasma decreased by about 35%, but the degree of decrease in LDL-C did not change. With the simultaneous use of atorvastatin does not affect the pharmacokinetics of antipyrine (phenazone), therefore, interaction with other drugs metabolized by the same isoenzymes of the cytochrome P450 system is not expected. With the simultaneous use of colestipol, the concentration of atorvastatin in blood plasma decreases by about 25%. However, the lipid-lowering effect of the combination of atorvastatin and colestipol exceeded that of each drug individually. With repeated use of digoxin and atorvastatin at a dose of 10 mg Css digoxin in plasma did not change. However, when digoxin was used in combination with Atorvastatin at a dose of 80 mg / day, the concentration of digoxin increased by about 20%. When using this combination, the condition of the patients should be monitored. With the simultaneous use of atorvastatin and erythromycin (500 mg 4 times / day) or clarithromycin (500 mg 2 times / day), which inhibit the CYP3A4 isoenzyme, an increase in plasma concentration of atorvastatin was observed. With the simultaneous use of atorvastatin (10 mg 1 time / day) and azithromycin (500 mg 1 time / day), the concentration of atorvastatin in the blood plasma did not change. Atorvastatin did not have a clinically significant effect on the concentration of terfenadine in the blood plasma, which is metabolized mainly with the participation of CYP3A4, therefore it seems unlikely that atorvastatin is able to significantly affect the pharmacokinetic parameters of other substrates of the CYP3A4 isoenzyme. With the simultaneous use of atorvastatin and an oral contraceptive containing norethindrone and ethinyl estradiol, a significant increase in the AUC of norethindrone and ethinyl estradiol was observed by about 30% and 20%, respectively. This effect should be considered when choosing an oral contraceptive for a woman receiving atorvastatin. Concomitant use with drugs that reduce the concentration of endogenous steroid hormones (including with cimetidine, ketoconazole, spironolactone) increases the risk of lowering endogenous steroid hormones (caution is required with these combinations). When studying the interaction of Atorvastatin with warfarin and cimetidine, no clinically significant interaction was detected. With the simultaneous use of atorvastatin at a dose of 80 mg and amlodipine at a dose of 10 mg, the pharmacokinetics of atorvastatin did not change in equilibrium. No clinically significant adverse effects of atorvastatin and antihypertensive agents have been observed. The concomitant use of atorvastatin with protease inhibitors known as CYP3A4 inhibitors (grapefruit juice) was accompanied by an increase in the concentration of atorvastatin in blood plasma, and therefore the use of this juice should be avoided. The simultaneous use of atorvastatin with inducers of the isoenzyme CYP3A4 (efavirenz, rifampicin) leads to a decrease in the concentration of atorvastatin with blood plasma. Pharmaceutical incompatibility not known. Overdose Treatment: there is no specific antidote, symptomatic therapy is carried out. Hemodialysis is ineffective. Storage conditions The product should be stored out of reach of children, in a dry, dark place at a temperature not exceeding 25 ° C. Expiration 3 years. active substance Atorvastatin Terms leave through pharmacies In retseptu lekarstvennaja form tablet Prescribing For adults as prescribed by the doctor Indications Indications Atherosclerosis, Prevention of heart attacks and strokes North Star, Russia
