Atorvastatin pills 40mg, 30pcs

Composition

Active ingredient:

atorvastatin calcium trihydrate;

Auxiliary substances:

calcium carbonate;

MCC;

StarCap 1500 (corn starch and pre-gelatinized starch);

colloidal silicon dioxide (aerosil);

talc; magnesium stearate;

Opadry II (series 85) (polyvinyl alcohol, macrogol, talc, titanium dioxide, iron oxide yellow dye, iron oxide red dye).

Pharmacological action

Atorvastatin is a hypolipidemic drug of the third generation from the statin group.

Indications

— combined with diet to reduce elevated levels of total Cholesterol, Cholesterol-LDL, and apolipoprotein b and triglycerides and improve HDL-C in patients with primary hypercholesterolemia, heterozygous familial and non-family hypercholesterolemia and combined (mixed) hyperlipidemia (types IIa and IIb according to Fredrickson);

— in combination with diet for the treatment of patients with elevated serum TG levels (type IV according to Fredrickson) and patients with dysbetalipoproteinemia (type III Fredrickson), whose diet does not provide an adequate effect;

— to reduce the levels of total Cholesterol and Cholesterol-LDL in patients with homozygous familial hypercholesterolemia when diet and other non-pharmacological therapies are not sufficiently effective.

Contraindications

active liver disease;

— increased activity of liver enzymes of unknown origin (more than 3 times compared to the ULN);

— liver failure (classes A and b according to child-Pugh);

— pregnancy;

— lactation period;

— age under 18 years (effectiveness and safety not established);

— hypersensitivity to the components of the drug.

The drug should be used with caution in patients with chronic alcoholism, a history of liver diseases, severe electrolyte disturbances, endocrine and metabolic disorders, arterial hypotension, severe acute infections (sepsis), uncontrolled epilepsy, extensive surgical interventions, injuries, and skeletal muscle diseases.

Side effects

In controlled clinical trials (n=2502), less than 2% of patients discontinued treatment due to atorvastatin-related side effects. The most common adverse effects associated with atorvastatin were constipation, flatulence, dyspepsia, and abdominal pain.

From the nervous system and sensory organs: ≥2% – headache, asthenic syndrome, insomnia, dizziness;

From the cardiovascular system: ≥2% – chest pain; blood pressure, phlebitis, arrhythmia, angina pectoris, anemia, lymphadenopathy, thrombocytopenia.

Respiratory system disorders: ≥2% – sinusitis, pharyngitis, bronchitis, rhinitis;

From the digestive tract: ≥2% — abdominal pain, constipation or diarrhea, dyspepsia, flatulence, nausea;

Musculoskeletal disorders: ≥2% – arthralgia, myalgia, arthritis;

From the genitourinary system: ≥2% – urogenital infections, peripheral edema;

From the skin: Allergic reactions: ≥2% – skin rash;

Other: ≥2% – infections, accidental injury, flu-like syndrome, back pain; ALP, increased ALT or AST, exacerbation of gout.

Side effects reported in post-marketing studies with atorvastatin therapy: anaphylaxis, angioedema, bullous rash (including erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis), rhabdomyolysis, tendon rupture.

Interaction

The risk of developing myopathy during statin treatment increases when they are used in combination with cyclosporine, fibrates, erythromycin, nicotinic acid in lipid-lowering doses, strong CYP3A4 inhibitors (including clarithromycin, HIV protease inhibitors, itraconazole).

When using atorvastatin in combination with inhibitors of the CYP3A4 isoenzyme (for example, cyclosporine, macrolide antibiotics — erythromycin and clarithromycin; itraconazole, HIV protease inhibitors), plasma concentrations of atorvastatin may increase (atorvastatin is metabolized with the participation of CYP3A4); special caution should be exercised when using atorvastatin in combination with the above-mentioned agents (see “Special Instructions”).

Combined use of atorvastatin 40 mg and itraconazole 200 mg once daily resulted in a 3-fold increase in the AUC of atorvastatin compared to that of monotherapy. Concomitant use of atorvastatin with protease inhibitors (lopinavir/ritonavir, ritonavir/saquinavir) was accompanied by an increase in the concentration of atorvastatin in blood plasma.

Concomitant use of atorvastatin 40 mg and a combination of lopinavir+ritonavir (400/100 mg twice daily) resulted in a 5.9-fold increase in the AUC of atorvastatin compared to that of monotherapy. When using atorvastatin at a dose of 40 mg with a combination of ritonavir+saquinavir (at a dose of 400/400 mg 2 times a day), its AUC increased 3.9 times.

Antacids reduce the concentration of atorvastatin by 35% (the effect on LDL cholesterol does not change). With repeated use of digoxin and atorvastatin, the Css of digoxin increases by about 20% (patients should be monitored).

When atorvastatin is co-administered with oral contraceptives, the AUC of norethindrone and ethinyl estradiol increases by approximately 30 and 20% (this effect should be taken into account when choosing an oral contraceptive for a woman receiving atorvastatin).

When co-administered with erythromycin (a CYP3A4 inhibitor), the plasma concentration of atorvastatin increases by approximately 40%.

The hypolipidemic effect of the combination of atorvastatin with colestipol is superior to that of each drug separately.

Concomitant use with drugs that reduce the concentration or activity of endogenous steroid hormones (including ketoconazole, spironolactone, cimetidine) increases the risk of reducing the production of endogenous steroid hormones (caution should be exercised).

Concomitant oral use of atorvastatin and a suspension containing magnesium and aluminum hydroxide reduced plasma concentrations of atorvastatin by approximately 35%, but the degree of reduction in LDL/cholesterol levels did not change.

How to take, course of use and dosage

Inside. Before prescribing Atorvastatin, the patient should be recommended a standard lipid-lowering diet, which he should continue to follow throughout the entire period of therapy.

The initial dose is on average 10 mg / day. The dose varies from 10 to 80 mg / day.

The drug can be taken at any time of the day with food or regardless of the time of meal. The dose is selected taking into account the initial cholesterol/LDL levels, 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 blood lipid levels every 2-4 weeks and adjust the dose accordingly.

To ensure the following dosage regimen of the drug, it is possible to use Atorvastatin in a different dosage form: film-coated tablets,10 mg and 20 mg.

The maximum daily dose of the drug is 80 mg. When used concomitantly with cyclosporine, the daily dose of Atorvastatin should not exceed 10 mg.

Primary hypercholesterolemia and mixed hyperlipidemia. In most cases, it is sufficient to prescribe a dose of 10 mg of Atorvastatin once a day.

A significant therapeutic effect is observed after 2 weeks, and the maximum therapeutic effect is usually observed after 4 weeks. With long-term treatment, this effect persists.

Special groups of patients with impaired renal function.

The use of the drug in patients with renal insufficiency and kidney diseases does not affect the level of Atorvastatin in blood plasma or the degree of reduction in cholesterol/LDL when it is used, so a change in the dose of the drug is not required. Liver function disorders.

In case of hepatic insufficiency, the dose should be reduced. Elderly patients. When using the drug in elderly patients, there were no differences in the safety, effectiveness or achievement of the goals of lipid-lowering therapy in comparison with the general population.

Overdose

Treatment: there is no specific antidote, symptomatic therapy is performed.

Hemodialysis is ineffective.

Special instructions

Before starting therapy with Atorvastatin, the patient should be prescribed a standard hypocholesterolemic diet, which he must follow during the entire treatment period.

The use of HMG-CoA reductase inhibitors to reduce blood lipids may lead to changes 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, 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 elevated enzyme levels should be monitored until their enzyme levels return to normal. If the values of alanine aminotransferase (ALT) or asparagine aminotransferase (AST) are more than 3 times higher than the upper permissible limit, it is recommended to reduce the dose of Atorvastatin or discontinue 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 combined with an increase in creatine phosphokinase (CPK) activity more than 10 times higher than the upper limit of normal) should be discussed in patients with advanced 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 CKD activity or if there is a confirmed or suspected myopathy.

The risk of myopathy associated with other drugs in this class was increased with concomitant use of cyclosporine, fibrates, erythromycin, nicotinic acid, or azole antifungal agents. Many of these drugs inhibit cytochrome P450-3A4-mediated metabolism and / or drug transport.

Atorvastatin is biotransformed by CYP 3A4. 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 monitored for muscle pain or weakness, especially during the first months of treatment and during periods of increasing the dose of any drug.

In such situations, periodic monitoring of CPK activity can be recommended, although such monitoring 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 have been described. Atorvastatin therapy should be temporarily discontinued or completely discontinued if there are signs of possible myopathy or a risk factor for developing renal failure due to rhabdomyolysis (for example, severe acute infection, hypotension, serious surgery, trauma, severe metabolic, endocrine and electrolyte disorders, and uncontrolled seizures).

Before starting therapy with Atorvastatin, it is necessary to try to achieve control of hypercholesterolemia by adequate diet therapy, increased physical activity, weight loss in obese patients, and treatment of other conditions. Patients should be warned to seek immediate medical attention if they experience unexplained muscle pain or weakness, especially if they are accompanied by malaise or fever.

Form of production

Round biconvex tablets, film-coated in white or almost white color.

On a cross-section, the core is white or almost white in color.

Storage conditions

Store in a dry place protected from light, out of reach of children, at a temperature of 15 C to 30 C.

Shelf

life is 2 years.

Active ingredient

Atorvastatin

Conditions of release from pharmacies

By prescription

Dosage form

Tablets