Atomax - instructions for use, reviews, analogs and formulations (10 mg and 20 mg tablets) medications to reduce elevated cholesterol and the treatment of hypercholesterolemia and hyperlipidemia in adults, children and pregnancy. Composition of statin

In this article, you can read the instructions for using the drug Atomax. Presented are reviews of visitors to the site - consumers of this medication, as well as opinions of doctors specialists on the use of Atomax in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of Atomax in the presence of existing structural analogs.Use for the treatment of hypercholesterolemia (high cholesterol in the blood) and hyperlipidemia in adults, children, as well as during pregnancy and lactation. Composition of the preparation.

Atomax - a hypolipidemic drug. Atorvastatin (active ingredient of the preparation Atomax) is a selective competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A-reductase (HMG-CoA reductase), a key enzyme that converts 3-hydroxy-3-methylglutarylcoenzyme A into mevalonic acid, the precursor of steroids, including cholesterol. In the liver, triglycerides (TG) and cholesterol (Xc) are included in the composition of very low density lipoproteins (VLDL), enter the blood plasma and transport to peripheral tissues. VLDLPs produce low-density lipoproteins (LDL), which are catabolized by interaction with high-affinity LDL receptors.

Atomax reduces cholesterol and lipoprotein levels in the blood plasma by inhibiting HMG-CoA reductase in the liver and increasing the number of LDL receptors on the surface of the liver cells, which leads to increased cholesterol uptake and catabolism in the form of low-density lipoproteins (Xc-LDL).

Atorvastatin reduces the production of LDL-C and the number of LDL particles. It causes a pronounced and persistent increase in the activity of LDL receptors, and also has a beneficial effect on the quality of circulating LDL. Atorvastatin effectively reduces the level of LDL-C in patients with homozygous hypercholesterolemia, which usually does not respond to therapy with other lipid-lowering drugs.

When studying the dose-dependence of the effect of atorvastatin, it was shown that the drug (in a dose of 10-80 mg) reduced the levels of total cholesterol (by 30-46%), Xc-LDL (by 41-61%), apolipoprotein B (by 34-50%) and triglycerides (by 14-33%). The results of treatment were similar in patients with heterozygous familial hypercholesterolemia, non-family forms of hypercholesterolemia and mixed hyperlipidemia, including in patients with non-insulin-dependent diabetes mellitus.

Atorvastatin reduces the levels of total cholesterol, LDL-C, cholesterol in the form of very low density lipoproteins (Xc-VLDL), apolipoprotein B, TG, and Xc, which is not part of high-density lipoprotein (HDL), and increases the level of cholesterol in the form of lipoproteins with high density (Xc-HDL) in patients with isolated hypertriglyceridemia.Atorvastatin reduces the level of cholesterol in the form of intermediate density lipoproteins (Xc-LLPP) in patients with disbetalipoproteinemia.

Like LDL, lipoproteins containing TG (including VLDL), intermediate-density lipoproteins (ALTs) and residues, also accelerate the development of atherosclerosis.

Elevated levels of TG in the blood plasma are often found in combination with a decrease in HDL-C level and the presence of small-size LDL particles, as well as in combination with non-lipid metabolic risk factors for ischemic heart disease (CHD). It has not yet been proven that an increase in the total level of TG in blood plasma is an independent risk factor for CHD. It has also not been shown that an increase in HDL-C level or a decrease in TG level in itself affects the risk of coronary and other cardiovascular complications and the mortality of patients.

The primary target organ of atorvastatin is the liver, where the synthesis of cholesterol and the clearance of LDL.

Dynamics of the level of LDL-C is better correlated with the dose of the drug than with its concentration in the blood plasma.

The dose of Atomax should be selected taking into account the therapeutic effect.

Composition

Atorvastatin + excipients.

Pharmacokinetics

Atorvastatin is rapidly absorbed after oral administration. The degree of absorption and concentration of atorvastatin in the blood plasma increases in proportion to the dose. The level of cholesterol / LDL reduction does not depend on the time of taking the drug during the day. Binding to plasma proteins - 98%. Atorvastatin is actively metabolized with the formation of ortho- and para-hydroxylated derivatives and various beta-oxidation products. Atorvastatin and its metabolites are excreted mainly with bile after hepatic and / or extrahepatic metabolism. After ingestion, less than 2% of the dose is detected in the urine.

Pharmacokinetics in special clinical cases

The concentration of atorvastatin in blood plasma in elderly people (aged more than 65 years) is higher than in adult patients of young age. However, there was no difference in safety, efficacy, or achievement of the goals of lipid-lowering therapy in the elderly in comparison with the general population.

Studies of the pharmacokinetics of the drug in children have not been conducted.

Concentrations of atorvastatin in blood plasma in women differ from those of men. However, there were no clinically significant differences in the effect of the drug on lipid metabolism in men and women.

Kidney disease does not affect the concentration of atorvastatin in the blood plasma or its effect on lipid metabolism. In this regard, a dose change in patients with impaired renal function is not required. Although studies have not been performed in patients with terminal stages of kidney disease, hemodialysis is unlikely to significantly increase the clearance of atorvastatin, as it actively binds to plasma proteins.

The concentrations of atorvastatin are significantly increased in patients with alcoholic cirrhosis of the liver.

Indications

• in combination with a diet to reduce elevated levels of total cholesterol, LDL-C, apolipoprotein B and TG, and an increase in HDL-C in patients with primary hypercholesterolemia, heterozygous familial and non-family hypercholesterolemia, and combined hyperlipidemia (types 2a and 2b according to Fredrickson) ;
• in combination with a diet for the treatment of patients with elevated serum TG (type 4 according to Fredrickson) and patients with dysetalopoproteinemia (type 3 according to Fredrickson), in which diet therapy does not provide an adequate effect;
• to reduce total cholesterol and LDL cholesterol in patients with homozygous familial hypercholesterolemia,when diet therapy and other non-pharmacological methods of treatment are not effective enough.

Forms of release

Tablets coated with a coating, 10 mg and 20 mg.

Instructions for use and dosing regimen

Before the appointment of Atomax, the patient should be recommended a standard lipid-lowering diet, which he must continue to observe throughout the period of therapy.

The initial dose is an average of 10 mg once a day. The dose varies from 10 to 80 mg once a day. The drug can be taken at any time of the day with food or whatever time it takes to eat. The dose is selected taking into account the baseline 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 Atomax, it is necessary to monitor the levels of lipids in the blood plasma every 2-4 weeks and adjust the dose accordingly.

With primary hypercholesterolemia and mixed hyperlipidemia, in most cases, Atomax is prescribed at a dose of 10 mg once a day. 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 insufficiency and kidney disease does not affect the level of atorvastatin in the blood plasma or the degree of decrease in the content of LDL-C during its application, therefore, a change in the dose of the drug is not required.

When using the drug in elderly patients, there were no differences in safety, effectiveness, or achievement of lipid-lowering therapy goals in comparison with the general population.

Side effect

• headache, dizziness;
• asthenic syndrome;
• insomnia or drowsiness;
• nightmarish dreams;
• amnesia (loss of memory);
• paresthesia (sensitivity disorders, characterized by sensations of numbness, tingling sensations, crawling crawling);
• peripheral neuropathy (peripheral nerve damage);
• emotional lability;
• ataxia (partial or complete loss of coordination of voluntary muscle movements);
• hyperkinetic (pathological sudden involuntary movements in one or a whole group of muscles);
• depression;
• hypoesthesia (weakening of sensitivity in certain parts of the body);
• amblyopia (functional, reversible vision reduction, in which one of the two eyes is almost or not involved in the visual process);
• tinnitus;
• dryness of the conjunctiva;
• violation of accommodation (adaptation of the organ of vision to changes in external conditions);
• hemorrhage in the eye;
• deafness;
• increased intraocular pressure;
• parosmia (impaired sense of smell);
• perversion of taste, loss of taste;
• chest pain;
• palpitation;
• vasodilation (vasodilation);
• Orthostatic hypotension (a violation of the ability of the body to maintain a normal level of blood pressure in the vertical position);
• phlebitis (inflammation of the walls of veins);
• arrhythmia;
• anemia, thrombocytopenia;
• lymphadenopathy (enlarged lymph nodes);
• bronchitis;
• rhinitis (runny nose);
• dyspnea (breathing disorder);
• bronchial asthma;
• nose bleed;
• nausea, heartburn;
• constipation or diarrhea;
• flatulence (bloating);
• gastralgia (pain in the stomach), abdominal pain;
• anorexia or increased appetite;
• dry mouth;
• eructation, dysphagia (difficulty swallowing);
• vomiting;
• stomatitis (inflammation of the oral mucosa);
• esophagitis (inflammation of the esophagus mucosa);
• glossitis (inflammation of the mucous membrane of the tongue);
• gastroenteritis;
• hepatitis, hepatic colic;
• cheilitis (inflammation of the red border, mucous membrane and skin of the lips);
• duodenal ulcer;
• pancreatitis;
• Cholestatic (due to difficulty of outflow of bile) jaundice;
• increased activity of hepatic transaminases;
• rectal (from the rectum) bleeding, melena (black semi-liquid stool);
• bleeding gums;
• tenesmus (painful and ineffectual urge to defecate or urinate);
• arthritis (inflammation of the joint);
• leg cramps;
• Bursitis (inflammation of the periarticular bag);
• myositis (inflammation of the muscle), myopathy (dystrophic lesion of muscle tissue);
• arthralgia, myalgia (pain in the joint, muscle);
• rhabdomyolysis (extreme degree of myopathy);
• contractures (limitation of passive movements) of joints;
• backache;
• increased serum creatine phosphokinase (CK);
• urogenital infections;
• peripheral edema;
• dysuria (disorders of urination);
• nephritis (inflammation of the kidneys);
• cystitis (inflammation of the bladder);
• hematuria (blood in the urine);
• urolithiasis disease;
• albuminuria (protein albumin in urine);
• vaginal bleeding, uterine bleeding;
• epididymitis (inflammation of the epididymis);
• decreased libido (sexual desire), impotence, ejaculation disorder;
• alopecia (baldness);
• sweating;
• eczema;
• seborrhea;
• ecchymosis (hemorrhages in the skin or mucous membrane, whose diameter usually exceeds 3 mm);
• hyperglycemia, hypoglycemia;
• increase in body weight;
• exacerbation of gout;
• increased body temperature;
• skin itching, skin rash;
• hives;
• multi-form exudative erythema, including Stevens-Johnson syndrome;
• toxic epidermal necrolysis (Lyell's syndrome).

Contraindications

• active liver disease or increased activity of serum transaminases (more than 3 times as compared with the upper limit of the norm) of an unknown genesis;
• pregnancy;
• lactation period;
• age under 18 years (effectiveness and safety not established);
• hypersensitivity to the components of the drug.

Use with caution in chronic alcoholism, with liver diseases in history, severe electrolyte imbalance, endocrine and metabolic disorders, arterial hypotension, severe acute infections (sepsis),uncontrolled epilepsy, extensive surgical interventions, injuries, skeletal muscle diseases.

Application in pregnancy and lactation

Atomax is contraindicated in pregnancy and lactation (breastfeeding).

It is not known whether atorvastatin is excreted in breast milk. Given the potential for adverse effects in infants, if necessary, use during lactation should decide the issue of termination of breastfeeding.

Women of reproductive age during treatment should use adequate methods of contraception. Atorvastatin can be administered to women of childbearing age only when the probability of pregnancy are very low and the patient informed of the potential risk of treatment to the fetus.

Use in children

Contraindicated for children and adolescents under 18 years of age (efficacy and safety not established).

Application in elderly patients

When using the drug in elderly patients, there were no differences in safety, effectiveness, or achievement of lipid-lowering therapy goals in comparison with the general population.

special instructions

Before starting therapy with Atomax, the patient should be given a standard hypocholesterol diet, which he must follow during the entire treatment period.

The use of HMG-CoA reductase inhibitors to reduce lipid levels in the blood can lead to a change in biochemical indicators that reflect liver function.

The function of the liver should be monitored before the start of therapy, 6 and 12 weeks after the start of taking Atomax and after each dose increase, and periodically, for example, every 6 months. An increase in the activity of hepatic enzymes in the serum can be observed during therapy with Atomax. Patients with an increased transaminase activity should be monitored until the enzyme level returns to normal. In that case, if the values ​​of alanine aminotransferase (ALT) or asparaginaminotrasferazy (AST) is more than 3 times the upper limit of normal (ULN), it is advisable to reduce the dose Atomaksa or discontinue treatment.

Atomax should be used with caution in patients who abuse alcohol and / or have liver disease. Active liver disease or persistent increase in transaminase activity of unknown originare contraindications to the appointment of the drug.

Treatment with atorvastatin can cause myopathy. The diagnosis of myopathy (pain and weakness in muscles combined with an increase in CKK activity by more than 10 times compared to IGN) should be borne in mind in patients with advanced myalgia, tenderness or weakness of the muscles and / or a marked increase in CKK activity. Patients should be warned that they should immediately inform the doctor of unexplained pain or weakness in the muscles if they are accompanied by a malaise or fever. Atomax therapy should be discontinued in the event of a marked increase in CK activity or in the presence of confirmed or suspected myopathy. The risk of myopathy in treatment with other drugs of this class was increased with the simultaneous use of cyclosporine, fibrates, erythromycin, niacin or azole antifungal agents. Many of these drugs inhibit metabolism mediated by the enzyme CYP3A4, and / or drug transport. Atorvastatin is biotransformed by the action of CYP3A4. Assigning atorvastatin in combination with fibrates, erythromycin, immunosuppressive agents,azole antifungal agents or niacin in hypolipidemic doses, the expected benefit and risk of treatment should be carefully weighed and patients monitored regularly to identify pain or weakness in the muscles, especially during the first months of treatment and during periods of increasing the dose of any drug. In such situations, it is possible to recommend a periodic determination of the activity of CKK, although such control does not prevent the development of severe myopathy.

When using atorvastatin, as well as other drugs in this class, cases of rhabdomyolysis with acute renal failure due to myoglobinuria are described. Atomax therapy should be temporarily discontinued or completely abolished if there is evidence of possible myopathy or the presence of a risk factor for developing renal failure against rhabdomyolysis (for example, severe acute infection, arterial hypotension, severe surgery, trauma, severe metabolic, endocrine and electrolyte disturbances and uncontrolled seizures).

Before starting therapy with Atomax, it is necessary to try to achieve control of hypercholesterolemia by adequate dietotherapy, increasing physical activity, reducing body weight in obese patients and treating other conditions.

Patients should be warned that they should immediately consult a doctor if unexplained pain or weakness in the muscles occurs, especially if they are accompanied by a malaise or fever.

Impact on the ability to drive vehicles and manage mechanisms

On the adverse impact of Atomax on the ability to drive vehicles and work with mechanisms were not reported.

Drug Interactions

The risk of myopathy during treatment with other drugs of this class is increased by the simultaneous use of cyclosporine, fibrates, erythromycin, antifungal drugs related to azoles, and niacin.

With simultaneous ingestion of atorvastatin and a suspension containing magnesium and aluminum hydroxides, the concentrations of atorvastatin in plasma decreased by approximately 35%, but the degree of decrease in the level of LDL-C was not changed.

With simultaneous use of Atomax does not affect the pharmacokinetics of antipyrin, therefore interaction with other drugs metabolized by the same isoenzymes of cytochrome is not expected.

With simultaneous application of colestipol, concentrations of atorvastatin in blood plasma decreased by approximately 25%.However, the hypolipidemic effect of the combination of atorvastatin and colestipol was superior to that of each drug individually.

With repeated administration of Digoxin and atorvastatin at a dose of 10 mg, the equilibrium concentrations of digoxin in the blood plasma did not change. However, when using digoxin in combination with atorvastatin at a dose of 80 mg per day, the digoxin concentration increased by about 20%. Patients receiving digoxin in combination with atorvastatin should be observed.

With the simultaneous use of atorvastatin and Erythromycin (500 mg 4 times daily) or Clarithromycin (500 mg twice daily), which inhibit the enzyme CYP3A4, an increase in the concentration of atorvastatin in blood plasma was observed.

With the simultaneous use of atorvastatin (10 mg once a day) and Azithromycin (500 mg once a day), the concentration of atorvastatin in the blood plasma did not change.

Atorvastatin had no clinically significant effect on the concentration of terfenadine in the blood plasma, which is metabolized mainly by CYP3A4; in this connection, it seems unlikely that atorvastatin can significantly affect the pharmacokinetic parameters of other CYP3A4 substrates.

With simultaneous use of Atomax and oral contraceptive containing norethindrone and ethinylestradiol, there was a significant increase in the area under the pharmacokinetic curve (AUC) of norethindrone and ethinylestradiol by approximately 30% and 20%, respectively. This effect should be considered when choosing an oral contraceptive for a woman receiving atorvastatin.

There was no clinically significant undesirable interaction of atorvastatin with estrogens.

When studying the interaction of atorvastatin with Warfarin and cimetidine, no signs of clinically significant interaction were found.

With simultaneous use of atorvastatin in a dose of 80 mg and Amlodipine at a dose of 10 mg, the pharmacokinetics of atorvastatin did not change in the equilibrium state.

Simultaneous use of atorvastatin with protease inhibitors, known as inhibitors of CYP3A4, was accompanied by an increase in the concentration of atorvastatin in blood plasma.

There was no clinically significant undesirable interaction of atorvastatin and antihypertensive agents.

Pharmaceutical incompatibility is not known.

Analogues of the drug Atomax

Structural analogs for the active substance:

• Anistat;
• Atokord;
• Ator;
• Atorvastatin;
• Atorvox;
• Atoris;
• The Vasator;
• Lipon;
• Lipofford;
• Liprimar;
• Novostat;
• TG-torus;
• Torvacard;
• Torvalip;
• Torvas;
• Tulip.

Analogues of the drug Atomax for the pharmacological group (statins):

• Akorta;
• Aktalipid;
• Anistat;
• Apexstatin;
• Atherostat;
• Atokord;
• Ator;
• Atorvastatin;
• Atorvox;
• Atoris;
• The Vasator;
• Vazilip;
• Vero-Simvastatin;
• Zocor;
• Zorstat;
• Cardiostatin;
• The Cross;
• Leskol;
• Lipobay;
• Lipon;
• Lipopraim;
• Lipostat;
• Lipofford;
• Liprimar;
• Lovacor;
• Lovastatin;
• Lovasterol;
• Mevakor;
• Medostatin;
• Mertenil;
• Novostat;
• Ovenkor;
• Pravastatin;
• Reddistatin;
• Ro-statin;
• Rovacor;
• Rosart;
• Rosystark;
• Rosuvastatin;
• Rosewood;
• Rosulip;
• Rozufast;
• Roxer;
• Rustor;
• Simva Hexal;
• Simvakol;
• Simvale;
• Simvastatin;
• Simvastol;
• Symvor;
• Simgal;
• Simlo;
• Sinquard;
• Suvardio;
• TG-torus;
• Tevastor;
• Torvacard;
• Torvalip;
• Torvas;
• Tulip;
• Holvasim;
• Holletar.

Response of a therapist

Widely used the drug Atomax in their practice about ten years ago. Now he practically ceased to enter the pharmacy network of our city, therefore I appoint more modern analogues from the group of statins.Assigned it to patients with high cholesterol and triglycerides in the blood, but on condition that they adhere to a diet with a reduced fat content. By the end of the first month of treatment, there was almost always a positive trend. But the side effects did not take long to wait. Complaints in patients were different (for headache, pain in muscles and joints, ringing in the ears, insomnia, etc.), but always have been.

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