$26.00
Manufacturer: Poland
Atorvasterol (atorvastatin) is used for the prevention of cardiovascular disease, as well as an adjunct to diet to reduce elevated levels of cholesterol.
Description
Ingredients
active substance: atorvastatin;
1 film-coated tablet contains 10.36 mg of atorvastatin calcium, which corresponds to 10 mg of atorvastatin, respectively;
excipients : mannitol (E 421), microcrystalline cellulose, calcium carbonate, povidone, croscarmellose sodium, sodium lauryl sulfate, colloidal anhydrous silicon dioxide, magnesium stearate, hypromellose, titanium dioxide (E 171), macrogol 6000, talc.
Medicinal form
Film-coated tablets.
Main physicochemical properties:
10 mg: white, round, biconvex, film-coated tablets, 7 mm in size.
Pharmacotherapeutic group
Drugs that reduce the level of cholesterol and triglycerides in blood serum. HMG-CoA reductase inhibitors. ATX code C10A A05.
Pharmacodynamics
Atorvastatin is a synthetic hypolipidemic drug. Atorvastatin is an inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase. This enzyme catalyzes the conversion of HMG-CoA into mevalonate, an early step in cholesterol biosynthesis that limits the rate of its formation.
Atorvastatin is a selective competitive inhibitor of HMG-CoA reductase, an enzyme that determines the rate of conversion of 3-hydroxy-3-methylglutaryl coenzyme A into mevalonate, a precursor of sterols, including cholesterol. Cholesterol and triglycerides circulate in the bloodstream in a complex with lipoproteins. These complexes are separated by ultracentrifugation into HDL (high-density lipoprotein), LDL (intermediate-density lipoprotein), LDL (low-density lipoprotein) and VLDL (very low-density lipoprotein) fractions. Triglycerides (TG) and cholesterol in the liver are incorporated into LDL and released into the blood plasma for transport to peripheral tissues. LDL is formed from LDL and is catabolized by interaction with high-affinity LDL receptors. Clinical and pathological studies show that
Elevated levels of total cholesterol, LDL cholesterol and apo B (membrane complex for LDL cholesterol) provoke the development of atherosclerosis. Similarly, reduced levels of HDL cholesterol (and its transport complex – apo B) are associated with the development of atherosclerosis.
Epidemiological studies have found that cardiovascular morbidity and mortality vary directly with total and LDL cholesterol levels and inversely with HDL cholesterol levels.
Atorvastatin lowers total cholesterol, LDL cholesterol, and apo B in patients with homozygous and heterozygous familial hypercholesterolemia, nonfamilial hypercholesterolemia, and mixed dyslipidemia. Atorvastatin also lowers HDL-cholesterol and TG, as well as causing persistent increases in HDL-cholesterol and apolipoprotein A-1. Atorvastatin lowers total cholesterol, LDL-cholesterol, LDL-cholesterol, apo B, triglycerides, and non-HDL-cholesterol and increases HDL-cholesterol in patients with isolated hypertriglyceridemia. Atorvastatin reduces LDL-C in patients with dysbetalipoproteinemia.
Like LDL, cholesterol- and triglyceride-enriched lipoproteins, including LDL, LDL, and remnants, may also contribute to atherosclerosis. Elevated plasma triglyceride levels are often found in the triad of low HDL-C and small LDL particles, as well as in association with nonlipid metabolic risk factors for coronary heart disease. It has not been consistently proven that the total level of plasma triglycerides as such is an independent risk factor for the development of coronary heart disease. In addition, there was no independent effect of increased HDL or decreased triglycerides on the risk of coronary and cardiovascular morbidity and mortality.
Atorvastatin, as well as some of its metabolites, are pharmacologically active in humans. The main site of action of atorvastatin is the liver, which plays a major role in cholesterol synthesis and LDL clearance. The dose of the drug, in contrast to the systemic concentration of the drug, correlates better with a decrease in LDL cholesterol. Individual selection of the dose of the drug should be carried out depending on the therapeutic response.
Indications
Prevention of cardiovascular disease in adults
For adult patients without clinically evident coronary heart disease but with several risk factors for coronary heart disease, such as age, smoking, hypertension, low HDL levels, or a family history of early coronary heart disease, Atorvasterol is indicated for:
- reducing the risk of myocardial infarction;
- reducing the risk of stroke;
- reducing the risk of revascularization procedures and angina pectoris.
For adult patients with type II diabetes and without clinically evident coronary heart disease, but with several risk factors for the development of coronary heart disease, such as retinopathy, albuminuria, tobacco smoking or arterial hypertension, the drug Atorvasterol (atorvastatin) is indicated for:
- reducing the risk of myocardial infarction;
- reducing the risk of stroke.
For adult patients with clinically pronounced coronary heart disease, Atorvasterol (atorvastatin) is indicated for:
- reducing the risk of non-fatal myocardial infarction;
- reducing the risk of fatal and non-fatal stroke;
- reducing the risk of revascularization procedures;
- reducing the risk of hospitalization due to congestive heart failure;
- reducing the risk of angina pectoris.
Hyperlipidemia
in adult patients
- As an adjunct to diet to reduce elevated levels of total cholesterol, LDL cholesterol, apolipoprotein B and triglycerides, and to raise HDL cholesterol in patients with primary hypercholesterolaemia (heterozygous familial and non-familial) and mixed dyslipidaemia (Fredrickson types IIa and IIb) .
- As an adjunct to diet for the treatment of patients with elevated serum triglyceride levels (Fredrickson type IV).
- For the treatment of patients with primary dysbetalipoproteinemia (type III according to the Fredrickson classification) in cases where adherence to a diet is insufficiently effective.
- To reduce total cholesterol and LDL cholesterol in patients with homozygous familial hypercholesterolemia as an adjunct to other lipid-lowering treatments (eg, LDL apheresis) or when such treatments are not available.
In children
- As an adjunct to the diet to reduce the levels of total cholesterol, LDL cholesterol and apolipoprotein B in children aged 10 to 17 years with heterozygous familial hypercholesterolemia, if after appropriate dietary therapy the test results are as follows:
a) LDL cholesterol remains ≥ 190 mg/dl (4.91 mmol/l) or
b) LDL cholesterol ≥ 160 mg/dl (4.14 mmol/l) and:
- in the family history there are early cardiovascular diseases or
- two or more other risk factors for the development of cardiovascular diseases are present in a pediatric patient.
Contraindications
- Active liver disease, which may include a persistent increase in liver transaminase levels of unknown etiology.
- Hypersensitivity to any of the components of this medicinal product.
- Pregnancy.
- Breast-feeding.
Method of application and dosage
Hyperlipidemia (heterozygous familial and non-familial) and mixed dyslipidemia (type IIa and IIb according to the Fredrickson classification)
The recommended starting dose of atorvastatin is 10 or 20 mg once a day. For patients requiring a significant reduction in LDL cholesterol (greater than 45%), therapy can be initiated at doses of 40 mg once daily. The dosage range of the drug is from 10 to 80 mg once a day. Atorvasterol (atorvastatin)can be taken in a single dose at any time, regardless of meals. Initial and maintenance doses of the drug should be selected individually depending on the treatment goal and response. After initiation of treatment and titration of the atorvastatin dose, lipid levels should be analyzed for a period of 2 to 4 weeks and the dose adjusted accordingly.
Heterozygous familial hypercholesterolemia in pediatric patients (10-17 years old)
The recommended initial dose of the drug is 10 mg/day; the maximum recommended dose is 20 mg/day (doses of the drug exceeding 20 mg have not been studied in this group of patients). Doses of the drug should be selected individually in accordance with the recommended goal of treatment. Dose adjustments should be made at intervals of 4 weeks or more.
Homozygous familial hypercholesterolemia
The dose of Atorvasterol (atorvastatin) for patients with homozygous familial hypercholesterolemia ranges from 10 to 80 mg per day. Atorvastatin should be used as an adjunct to other lipid-lowering treatments (eg, LDL apheresis) or as primary therapy if lipid-lowering treatments are not available.
Simultaneous hypolipidemic therapy
Atorvasterol (atorvastatin) can be used with bile acid sequestrants. The combination of HMG-CoA reductase inhibitors (statins) and fibrates should generally be used with caution.
Dosage for patients with impaired renal function
Renal disease does not affect either plasma concentrations or LDL-cholesterol reduction with atorvastatin; therefore, adjustment of the dose of the drug for patients with impaired renal function is not required.
Dosage for patients taking cyclosporine, clarithromycin, itraconazole, letermovir, or certain protease inhibitors
Treatment with Atorvasterol (atorvastatin) should be avoided in patients taking cyclosporine, HIV protease inhibitors (tipranavir + ritonavir), or hepatitis C virus protease inhibitor (telaprevir). Atorvastatin should be used with caution in HIV patients receiving lopinavir + ritonavir and at the lowest dose necessary. For patients taking clarithromycin, itraconazole, and for HIV patients taking the combination of saquinavir + ritonavir, darunavir + ritonavir, fosamprenavir or fosamprenavir + ritonavir, the therapeutic dose of Atorvasterol (atorvastatin) should be limited to a dose of 20 mg, and appropriate clinical examinations are recommended for determination of the minimum necessary dose of atorvastatin. For patients taking the HIV protease inhibitor nelfinavir or the hepatitis C virus protease inhibitor boceprevir,
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