Atorvastatin pills 20mg, 90pcs

Composition

1 tab. – atorvastatin (in the form of atorvastatin calcium trihydrate) 20 mg. Auxiliary substances: 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.

Composition of the film shell:

hypromellose-4.5 mg,

talc-1.764 mg,

giprolose-1.746 mg,

titanium dioxide-0.99 mg

Pharmacological action

Hypolipidemic drug from the statin group. Selective competitive inhibitor of HMG-CoA reductase, an enzyme that converts 3-hydroxy-3-methylglutarylcoenzyme A to mevalonic acid, a precursor of sterols, including cholesterol. Triglycerides and cholesterol in the liver are incorporated into VLDL, enter the blood plasma and are transported to peripheral tissues. LDL is formed from VLDL during interaction with LDL receptors. Atorvastatin reduces plasma cholesterol and lipoprotein concentrations by inhibiting HMG-CoA reductase, cholesterol synthesis in the liver, and increasing the number of LDL receptors in the liver on the cell surface, which leads to increased LDL uptake and catabolism. Reduces the formation of LDL, causes a pronounced and persistent increase in the activity of LDL receptors. Reduces LDL levels in patients with homozygous familial hypercholesterolemia, which usually does not respond to lipid-lowering therapy. Reduces 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-dependent reduces the LDL content in patients with homozygous hereditary hypercholesterolemia, resistant to therapy with other lipid-lowering agents.

Indications

Atorvastatin is used:

— in combination with diet to reduce elevated total cholesterol, cholesterol/LDL, and apolipoprotein b and triglycerides and increase HDL cholesterol concentrations 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 a high content of triglycerides in the blood serum (type IV according to Fredrickson) and patients with dysbetalipoproteinemia (type III Fredrickson), whose diet does not provide an adequate effect;

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

Use during pregnancy and lactation

Atorvastatin is contraindicated for use during pregnancy and lactation (breastfeeding). It is not known whether atorvastatin is excreted in breast milk. Taking into account the possibility of adverse events in infants, if it is necessary to use the drug during lactation, the question of stopping breastfeeding should be decided. Women of reproductive age should use adequate methods of contraception 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.

Side effects

Nervous system disorders:  more often 2% – insomnia, dizziness; less often 2% – headache, asthenia, malaise, drowsiness, nightmares, paresthesia, peripheral neuropathy, amnesia, emotional lability, ataxia, facial nerve paralysis, hyperkinesis, migraine, depression, hypesthesia, loss of consciousness.

From the side of the senses:  less than 2% – amblyopia, tinnitus, conjunctival dryness, accommodation disorders, retinal hemorrhage, deafness, glaucoma, parosmia, loss of taste sensations, taste distortion.

From the cardiovascular system:  more often 2% – chest pain; less often 2% – palpitation, symptoms of vasodilation, orthostatic hypotension, increased blood pressure, phlebitis, arrhythmia, angina pectoris.

From the hematopoietic system:  less than 2% – anemia, lymphadenopathy, thrombocytopenia.

Respiratory system disorders:  more often 2% – bronchitis, rhinitis; less often 2% – pneumonia, dyspnoea, exacerbation of bronchial asthma, nosebleeds.

From the digestive system:  more often 2% – nausea; less often 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, liver dysfunction, rectal bleeding, melena, bleeding gums, tenesmus.

Musculoskeletal disorders:  more often 2% – arthritis; less often 2% – leg muscle cramps, bursitis, tendosynovitis, myositis, myopathy, arthralgia, myalgia, rhabdomyolysis, torticollis, muscle hypertonus, joint contractures.

From the urinary system:  more often 2% – peripheral edema; less often 2% – dysuria (including pollakiuria, nocturia, urinary incontinence or urinary retention, imperative urge to urinate, nephritis, hematuria, nephrourolithiasis.

From the genitals and breast:  more often 2% – urogenital infections; less often 2% – vaginal bleeding, metrorrhagia, epididymitis, decreased libido, impotence, ejaculation disorders, gynecomastia, mastodynia.

Skin and subcutaneous tissue disorders:  more often than 2% – alopecia, xeroderma, increased sweating, eczema, seborrhea, ecchymosis, petechiae.

Allergic reactions:  less than 2% – pruritus, skin rash, contact dermatitis ” rarely-urticaria, angioedema, facial edema, photosensitization, anaphylaxis, erythema multiforme (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell’s syndrome).

From the side of laboratory parameters:  less than 2% – hyperglycemia, hypoglycemia, increased serum creatinine clearance, albuminuria.

Other services:  less often 2% – weight gain, exacerbation of gout.

Interaction

The risk of myopathy during treatment with other drugs of this class increases with the simultaneous use of cyclosporine, fibrates, erythromycin, antifungal agents related to azoles, and nicotinic acid. 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 cholesterol/LDL concentrations did not change. Concomitant use of atorvastatin does not affect the pharmacokinetics of antipyrine (phenazone), so interaction with other agents metabolized by the same cytochrome isoenzymes is not expected. With simultaneous use of colestipol, the concentration of atorvastatin in blood plasma decreased by about 25%. However, the lipid-lowering effect of the combination of atorvastatin and colestipol exceeded that of each drug separately. With repeated use of digoxin and atorvastatin at a dose of 10 mg, the Css of digoxin in blood plasma did not change. However, when digoxin was used in combination with atorvastatin at a dose of 80 mg/day, the digoxin concentration increased by about 20%. Patients receiving digoxin in combination with Atorvastatin should be monitored. Concomitant use of atorvastatin and erythromycin (500 mg 4 times / day) or clarithromycin (500 mg 2 times / day), which inhibit cytochrome CYP3A4, an increase in the concentration of atorvastatin in blood plasma was observed. Concomitant use of atorvastatin (10 mg 1 time/day) and azithromycin (500 mg 1 time/day) did not change the concentration of atorvastatin in blood plasma. Atorvastatin did not have a clinically significant effect on the plasma concentration of terfenadine, which is mainly metabolized by the cytochrome CYP3A4; therefore, it seems unlikely that Atorvastatin can significantly affect the pharmacokinetic parameters of other CYP3A4 substrates. When atorvastatin was co-administered with an oral contraceptive containing norethindrone and ethinylestradiol, there was a significant increase in the 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. Concomitant use with drugs that reduce the concentration of endogenous steroid hormones (including cimetidine, ketoconazole, spironolactone) increases the risk of reducing endogenous steroid hormones (caution should be exercised). When studying the interaction of atorvastatin with warfarin and cimetidine, no signs of clinically significant interaction were found. Concomitant use of atorvastatin 80 mg and amlodipine 10 mg did not alter the pharmacokinetics of atorvastatin at steady state. There was no clinically significant adverse interaction between atorvastatin and antihypertensive agents. Concomitant use of atorvastatin with protease inhibitors, known as CYP3A4 inhibitors, was accompanied by an increase in the concentration of atorvastatin in blood plasma. Pharmaceutical incompatibility is unknown.

How to take it, course of use and dosage

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 drug is taken orally, 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.The initial dose is on average 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 Atorvastatin, it is necessary to monitor the content of lipids in blood plasma every 2-4 weeks and adjust the dose accordingly.

In primary hypercholesterolemia and mixed hyperlipidemia, as well as hyperlipidemia of type III and IV according to Fredrickson, in most cases, it is sufficient to prescribe the drug at a dose of 10 mg 1 time/day. A significant therapeutic effect is usually observed after 2 weeks; the maximum therapeutic effect is usually observed after 4 weeks. With long-term treatment, this effect persists.

In homozygous familial hypercholesterolemia, the drug is prescribed at a dose of 80 mg (4 tablets of 20 mg) 1 time/day.

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.

In case of hepatic insufficiency, the dose should be reduced.

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 indicated. Hemodialysis is ineffective.

Special instructions

Before starting therapy with Atorvastatin, the patient should be prescribed a standard hypocholesterolemic diet, which he should follow during the entire treatment period. The use of HMG-CoA reductase inhibitors to reduce the concentration of lipids in the blood can 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 who show an increase in enzyme activity should be monitored until the indicators return to normal values. If the ALT or ACT values are more than 3 times higher than the ULN, 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 CPK activity by more than 10 times compared to ULN) 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 during treatment with 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 by 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 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 risk factors for developing renal failure associated with 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.

Influence on the ability to drive motor vehicles and manage mechanisms

No adverse effects of Atorvastatin on the ability to drive a car or work with mechanisms have been reported.

Form of production

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

Storage conditions

The drug should be stored out of the reach of children, dry, protected from light at a temperature not exceeding 25°C.

Shelf

life is 2 years.

Active ingredient

Atorvastatin

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Atherosclerosis, Prevention of heart attacks and strokes