Atorvastatin - instructions for use, dose, side effects, contraindications

Competitively inhibits HMG-CoA reductase, an enzyme that converts 3-hydroxy-3-methylglutaryl coenzyme A into mevalonic acid, a precursor of styrenes, including cholesterol.

It inhibits the synthesis of cholesterol in hepatocytes,which leads to an increase in the synthesis and subsequent increase in the density of low-density lipoprotein receptors on the surface of these cells. As a result, the capture of low density lipoproteins from the blood plasma increases, which leads to a decrease in the cholesterol content.

In a dose of 40 mg lowers the concentration in the plasma: cholesterol by 30-46%, low density lipoprotein - by 40-60%, triglycerides - by 14-33%, apolipoproteins B100 - by 35-50%; increases the concentration of high-density lipoproteins and apoliproteins A.

Has a positive effect on the intima of the vessels in the preclinical phase of the development of atherosclerosis due to antiproliferative and antioxidant effects, improves the rheological properties of the blood. Minimizes the risk of vascular complications of coronary heart disease, reduces the risk of repeated myocardial infarction.

Pharmacokinetics:

Absorbed in the gastrointestinal tract. Communication with plasma proteins is 98%.

Half-Elimination (half-life) of the drug is 13 hours, active metabolites - up to 24-30 hours.

Metabolism in the liver with the participation of enzymes: 3A4 and CYP3A3. Elimination with feces, about 2% - by the kidneys.

Indications:

It is used to treat hypercholesterolemia, when the methods of diet therapy are not enough.

ICD-10

IV.E70-E90.E78.1 Pure hyperglyceridemia

IV.E70-E90.E78.0 Pure hypercholesterolemia

IV.E70-E90.E78.2 Mixed hyperlipidemia

Contraindications:

Hepatitis in the active phase.

Individual intolerance.

Carefully:

In chronic inflammatory processes in the liver. With an increase in activity alanine aminotransferase and aspartate aminotransferase > three times the elimination of the drug.

Pregnancy and lactation:

Pregnancy and lactation: recommendations for Food and Drug Administration (US Food and Drug Administration) - category X. Possible violation of fetal embryonic development due to inhibition of the synthesis of mevalonic acid involved in replication deoxyribonucleic acid. There is no evidence of ingestion into breast milk. Atorvastatin is contraindicated in pregnancy and lactation.

Dosing and Administration:

It is taken orally, once a day. The initial dose is 10 mg per day. The effect is detected two weeks after the start of treatment. The dose is adjusted depending on the effectiveness of therapy.

The highest daily dose: 80 mg.

The highest single dose: 80 mg.

Use in children

It is used from the age of 10 years with family forms of hyperlipidemia. From 10 to 17 years, 10 mg per day. Increase in the dose gradually - after two weeks of admission. The maximum dose: 80 mg per day.

Side effects:

Central and peripheral nervous system: headache, dizziness, unpleasant dreams, peripheral neuropathy, migraine.

Cardiovascular system: palpitation, orthostatic hypotension, arrhythmia.

The system of hematopoiesis: anemia, thrombocytopenia.

Respiratory system: exacerbation of bronchial asthma.

Muscular system: myopathy, myositis, rhabdomyolysis (rarely).

Digestive system: nausea, dysphagia, stomatitis, hepatitis, rectal bleeding (melena), tenesmus.

Analyzers: noises in the ears, amblyopia, loss of taste sensations.

Genitourinary system: dysuric disorders, impotence.

Allergic reactions.

Overdose:

Cases of overdose are not described.

Treatment is symptomatic, hemodialysis is ineffective.

Interaction:

Grapefruit juice increases the concentration of atorvastatin - an increase in side effects (myopathy).

At reception of alcohol during treatment by a preparation activity of transaminases raises.

Antifungal agents, erythromycin, ciclosporin - increase the concentration of atorvastatin by 40%. Digoxin - by 20%. With simultaneous use, a dose adjustment is required.

Special instructions:

The drug is not compatible with alcohol - people with chronic alcoholism, atorvastatin not assigned.

In the treatment of atorvastatin in patients with chronic renal failure, the progression of the disease slows down, or proteinuria decreases or ceases.

Instructions

Atorvastatin (Atorvastatinum)