Atorvastatin | atorvastatin tablets coated.ob. 20 mg 90 pcs.

Latin name

ATORVASTATIN

Release form

Film-coated tablets of white or almost white color, round, biconvex in cross section, the core is white or almost white.

Pharmacological action

Hypolipidemic drug from the group of statins. Selective competitive inhibitor of HMG-CoA reductase - an enzyme, converting 3-hydroxy-3-methylglutaryl coenzyme A to mevalonic acid, a precursor of sterols, including cholesterol.

Triglycerides and cholesterol in the liver are included in VLDL, enter the blood plasma and are transported to peripheral tissues. LDL is formed from VLDL during interaction with LDL receptors.

Atorvastatin lowers plasma cholesterol and lipoprotein concentrations by inhibiting HMG-CoA reductase, synthesizing cholesterol in the liver and increasing the number of LDL receptors in the liver on the cell surface, which leads to increased uptake and catabolism of LDL.

Reduces the formation of LDL, causes a pronounced and persistent increase in the activity of LDL receptors. Reduces LDL in patients with homozygous familial hypercholesterolemia, which usually does not respond to therapy with lipid-lowering drugs.

Decreases the concentration of total cholesterol by 30-46%, LDL - by 41-61%, apolipoprotein B - by 34-50% and triglycerides - by 14-33% causes an increase in the concentration of HDL cholesterol and apolipoprotein A.

Dose-dependently lowers LDL in patients with homozygous hereditary hypercholesterolemia, resistant to therapy with other hypolipidemic agents.

Indications

Atorvastatin is used:

- in combination with a diet to reduce high cholesterol, cholesterol / LDL, apolipoprotein B and triglycerides and increasing HDL cholesterol concentration in patients with primary hypercholesterolemia, heterozygous familial and non-familial hypercholesterolemia and combined (mixed) hyperlipidemia (types IIa and IIb according to Fredrickson)

- in combination with high blood serum for diet (type IV according to Fredrickson) and patients with dysbetalipoproteinemia (type III according to Fredrickson) in whom diet therapy does not give an adequate effect of

- to reduce the concentration of total cholester ina and cholesterol / LDL in patients with homozygous familial hypercholesterolemia, when diet therapy and other non-pharmacological treatments are not effective enough.

Contraindications

- active liver disease or increased activity of liver enzymes of unclear origin (more than 3 times compared with VGN)

- liver failure (severity according to Child Pugh classification A and B)

- pregnancy

- lactation period srd - age under 18 years (effectiveness and safety have not been established)

- hypersensitivity to the components of the drug.

With caution, the drug should be prescribed for alcohol abuse, a history of liver disease, severe electrolyte imbalance, endocrine and metabolic disorders, arterial hypotension, severe acute infections (sepsis), uncontrolled epilepsy, extensive surgical interventions, injuries, and 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.

Considering 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 the probability of pregnancy is very low, and the patient is informed about the possible risk to the fetus during therapy.

Special instructions

Before starting therapy with the drug Atorvastatin, the patient must be prescribed a standard hypocholesterol diet, which he must follow during the entire treatment period. The use of inhibitors of HMG-CoA reductase to reduce the concentration of lipids in the blood 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 the start of the use of 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. Patients who have an increase in enzyme activity should be monitored until the indicators return to normal values. In the event that 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.

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 CPK activity by more than 10 times compared with VGN) should be discussed in patients with common myalgia, muscle soreness or 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 if there is a 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 from the azole group.

Many of these drugs inhibit CYP3A4-mediated metabolism and / or drug transport. Atorvastatin is biotransformed under the action of CYP3A4. When prescribing atorvastatin in combination with fibrates, erythromycin, immunosuppressive agents, azole antifungal agents, 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 possible myopathy or there are risk factors 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 treatment with Atorvastatin, 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 should be warned that 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 vehicles and control mechanisms

The adverse effects of the drug Atorvastatin on the ability to drive a car and work with mechanisms were not reported.

Composition

1 tablet atorvastatin (in the form of atorvastatin calcium trihydrate) 20 mg.

Excipients:

microcrystalline cellulose - 99.36 mg,

lactose monohydrate - 80 mg,

calcium carbonate - 66 mg,

crospovidone - 15 mg,

sodium carboxymethyl starch - 9 mg,

hyprolose - 6 mg,

magnesium stearate - 3 mg.

Film composition:

hypromellose - 4.5 mg,

talc - 1.764 mg,

hyprolysis - 1.746 mg,

titanium dioxide - 0.99 mg.

Dosage and administration 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 drug is taken orally, at any time of the day with food or regardless of meal times.

Dose is adjusted based on baseline cholesterol / LDL levels, treatment goals, and individual effects. The initial dose is an average of 10 mg 1 time / day. The dose varies from 10 to 80 mg 1 time / day.

At the beginning of treatment and / or during an increase in the dose of the drug Atorvastatin, it is necessary to monitor the plasma lipid content every 2-4 weeks and adjust the dose accordingly.

With primary hypercholesterolemia and mixed hyperlipidemia, as well as type III and IV hyperlipidemia according to Fredrickson, in most cases it is sufficient to prescribe a drug at a dose of 10 mg 1 time / day. A significant therapeutic effect is observed, usually 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.

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 liver failure, the dose must 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: more than 2% - insomnia, dizziness less than 2% - headache, asthenia, malaise, drowsiness, nightmares, paresthesia, peripheral neuropathy, amnesia, emotional lability, ataxia, paralysis hyperkinesis, migraine, depression, hypesthesia, loss of consciousness.

On the part of the sensory organs: less than 2% - amblyopia, ringing in the ears, dryness of the conjunctiva, disturbed accommodation, hemorrhage in the retina, deafness, glaucoma, parosmia, loss of taste, perversion of taste.

From the cardiovascular system: more often 2% - chest pain less than 2% - palpitations, vasodilation symptoms, orthostatic hypotension, increased blood pressure, phlebitis, arrhythmia, angina pectoris.

From the hemopoietic system: less than 2% - anemia, lymphadenopathy, thrombocytopenia.

From the respiratory system: more than 2% - bronchitis, rhinitis less often 2% - pneumonia, dyspnea, exacerbation of bronchial asthma, nosebleeds.

From the digestive system: more often 2% - nausea less than 2% - 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: more often 2% - arthritis less often 2% - leg muscle cramps, bursitis, tendosynovitis, myositis, myopathy, arthralgia, myalgia, rhabdomyolysis, torticollis, muscle hypertonicity, joint contractures.

From the urinary system: more often 2% - peripheral edema less than 2% - dysuria (including pollakiuria, nocturia, urinary incontinence or urinary retention, imperative urination, nephritis, hematuria, nephrourolithiasis.

From the genitals and mammary gland: more often 2% - urogenital infections less than 2% - vaginal bleeding, metrorrhagia, epididymitis, decreased libido, impotence, impaired ejaculation, gynecomastia, mastodynia.

From the skin and subcutaneous tissues: more than 2% - alopecia, xeroderma, increased sweating, eczema, seborrhea, ecchymosis, petechiae.

Allergic reactions: less than 2% - itchy skin, rash, contact dermatitis rarely - urticaria, angioedema, facial edema, photosensitivity, anaphylaxis, erythema multiforme exudative (including Stevens-Johnson syndrome), toxic epidermal necrolysis Lyella).

On the part of laboratory parameters: less than 2% - hyperglycemia, hypoglycemia, increased serum CPK, albuminuria.

Other: less than 2% - weight gain, exacerbation of gout.

Overdose

Treatment: No specific antidote has been shown for symptomatic therapy. 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 РC.

Shelf life

2 years.

Deystvuyushtee substance

Atorvastatin

dosage form

tablets

Appointment

Appointment

For adults appointment doctor