Liprimar pills 20mg №100

Dosage form

Coated tablets

Composition

In 1 tablet, film coated, contains:

- Active substances
- Atorvastatin (in the form of Calcium salt) 20 mg.

- Calcium carbonate excipients, microcrystalline cellulose, lactose monohydrate, croscarmellose sodium, polysorbate-80, hyprolosis, Magnesium stearate.

- Composition of the shell Opadray white YS-1-7040 (contains hypromellose, polyethylene glycol, titanium dioxide, talc), simethicone emulsion (contains simethicone, stearic emulsifier, sorbic acid, water), candelica wax.

Packing

In the blister of 10 tablets. In the package 10 blisters.

Mechanism of action

Liprimar-atorvastatin is a selective competitive inhibitor of HMG-CoA reductase, a key enzyme that converts 3-hydroxy-3-methylglutaryl-CoA into mevalonate, the precursor of steroids, including cholesterol; synthetic lipid-lowering agent.

In patients with homozygous and heterozygous familial hypercholesterolemia, non-familial forms of hypercholesterolemia and mixed dyslipidemia.very low density lipoproteins (Xc-VLDL) and triglycerides (TG), causes an unstable increase in high-density lipoprotein cholesterol (Xc-HDL).

Reduces the concentration of cholesterol and lipoproteins in the blood plasma, inhibiting HMG-CoA reductase and cholesterol synthesis in the liver and increasing the number of hepatic LDL receptors on the cell surface, which leads to increased uptake and catabolism of Xc-LDL.

Reduces the formation of Xc-LDL and the number of LDL particles. Causes a pronounced and persistent increase in the activity of LDL receptors, in combination with favorable qualitative changes in LDL particles. Reduces the level of cholesterol-LDL in patients with homozygous hereditary hypercholesterolemia, resistant to treatment with other lipid-lowering drugs.

Liprimar at a dose of 10-80 mg reduces the level of total cholesterol by 30-46%, Xc-LDL by 41-61%, apolipoprotein B by 34-50% and triglyceride by 14-33%. The results of treatment are similar in patients with heterozygous familial hypercholesterolemia, non-familial forms of hypercholesterolemia and mixed hyperlipidemia, including in patients with non-insulin dependent diabetes mellitus.

In patients with isolated hypertriglyceridemia, Liprimar lowers total cholesterol, Xc-LDL, Xc-VLDL, apo-B, and TG and increases the level of Xc-HDL. In patients with dysbetalipoproteinemia, lowers lipoprotein cholesterol intermediate density.

In patients with type IIa and IIb hyperlipoproteinemia according to Fredrickson's classification, the mean value of increased HD-C HDL-C levels during treatment with Liprimar (10-80 mg), compared with baseline, is 5.1-8.7% and is not dose dependent.There is a significant dose-dependent decrease in the ratio: total cholesterol / Xc-HDL and Xc-LDL / Xc-HDL by 29-44% and 37-55%, respectively.

Liprimar at a dose of 80 mg reliably reduces the risk of ischemic complications and death by 16% after a 16-week course, and the risk of re-hospitalization for angina, accompanied by signs of myocardial ischemia, by 26%. In patients with different baseline levels of Xc-LDL, Liprimar causes a reduction in the risk of ischemic complications and death (in patients with myocardial infarction without Q wave and unstable angina, men and women, patients younger than 65 years of age).

The decrease in plasma Hc-LDL correlates better with the dose of the drug than with its concentration in the blood plasma.

- Prevention of cardiovascular diseases In an Anglo-Scandinavian study of cardiac outcomes, a lipid-lowering branch (ASCOT-LLA), the effect of atorvastatin on fatal and non-lethal outcomes of coronary heart disease (cardiovascular mortality, hospitalization for unstable angina) was evaluated in patients with cardiovascular mortality, hospitalization for unstable angina, was evaluated in patients with cardiovascular mortality, hospitalization for unstable angina) was evaluated in patients with cardiovascular mortality, hospitalization for unstable angina) was assessed in patients with cardiovascular mortality, hospitalization for unstable angina) was assessed in patients with cardiovascular mortality, hospitalization for unstable angina) was evaluated in patients with cardiovascular mortality, hospitalization for unstable angina) was assessed in patients with cardiovascular mortality, hospitalization for unstable angina) was evaluated in patients with cardiovascular mortality, hospitalization for unstable angina) was evaluated in patients with heart failure, cardiovascular mortality, hospitalization for unstable angina) were evaluated in patients with cardiovascular mortality, hospitalization for unstable angina). 80 years (63 on average) without a myocardial infarction (MI) in the anamnesis and with an initial level of total cholesterol of more than 6.5 mmol / l (251 mg / dl). All patients also had at least 3 cardiovascular risk factors: male gender, age over 55 years old, smoking, diabetes mellitus, ischemic heart disease in a first-degree relative, the ratio of total cholesterol to HD-C HDL levels of more than 6, peripheral disease vessels, left ventricular hypertrophy, history of cerebral circulation, specific ECG changes, proteinuria and albuminuria.In the study, patients with arterial hypertension simultaneously with prescribed antihypertensive therapy (target BP less than 140/90 mmHg for all patients and less than 130/80 for patients with diabetes mellitus) were administered atorvastatin in a dose of 10 mg / day or placebo. Due to the fact that according to the interim analysis, the effect of the drug therapy significantly exceeded the effect of using placebo, it was decided to terminate the study early after 3.3 years instead of the expected 5 years. Atorvastin significantly reduced the risk of the following complications: Complications Reduced risk Coronary complications (coronary artery disease and fatal MI) 36% General cardiovascular complications and revascularization procedures 20% General coronary complications 29% Stroke (fatal and non-fatal) 26% Significant reduction in indicators there was no overall mortality and mortality from cardiovascular causes, although positive trends were observed.

- Diabetes mellitus In a joint study of the effect of atorvastatin on fatal and non-fatal outcomes of cardiovascular diseases in type 2 diabetes mellitus (CARDS), it was shown that atorvastatin therapy reduced the risk of developing the following cardiovascular complications regardless of gender, age of the patient or baseline Xc- LDL: Complications Reducing the risk of Major cardiovascular complications (fatal and nonfatal acute myocardial infarction (MI), hidden MI, death due to exacerbation of coronary artery disease, unstable angina,coronary artery bypass, subcutaneous transluminal coronary angioplasty, revascularization, stroke) 37% Myocardial infarction (fatal and non-fatal acute MI, hidden MI) 42% Stroke (fatal and non-fatal) 48%

- Atherosclerosis In the study of the reverse development of coronary atherosclerosis with intensive lipid-lowering therapy (REVERSAL) with atorvastatin 80 mg in patients with coronary artery disease, it was found that the average decrease in the total volume of atheroma (primary efficacy criterion) since the beginning of the study was 0.4%.

- Recurrent stroke. In an intensive cholesterol-lowering program (SPARCL), it was found that atorvastatin at a dose of 80 mg per day reduced the risk of recurring fatal or non-fatal stroke in patients who had a stroke or transient ischemic attack (TIA) without a history of CHD 15% compared to placebo. At the same time, the risk of major cardiovascular complications and revascularization procedures was significantly reduced. A reduction in the risk of cardiovascular disorders in therapy with atorvastatin was noted in all groups except for the one that included patients with primary or recurrent hemorrhagic stroke (7 in the atorvastatin group versus 2 in the placebo group).

- Hemorrhagic stroke In patients who received atorvastatin therapy at a dose of 80 mg, the incidence of hemorrhagic or ischemic stroke (265 vs. 311) or IHD (123 vs. 204) was less than in the control group.

- Secondary prevention of cardiovascular complications Btreatment of the New Purpose Study (TNT) compared the effect of atorvastatin at doses of 80 mg / day and 10 mg / day on the risk of developing cardiovascular complications in patients with clinically confirmed coronary artery disease. Atorvastatin at a dose of 80 mg significantly reduced the development of the following complications: Complications Atorvastatin 80 mg Primary endpoint The first important cardiovascular complication (coronary heart disease and fatal myocardial infarction) 8.7% nonfatal IM, non-related 4.9% Stroke ( fatal and nonfatal) 2.3% Secondary end point First hospitalization for congestive heart failure 2.4% First coronary artery bypass or other revascularization procedures 13.4% First documented angina pectoris 10.3%

- Primary hypercholesterolemia (heterozygous familial and non-familial hypercholesterolemia (Frederickson type IIa).
- Combined (mixed) hyperlipidemia (Frederickson type IIa and IIb types).
- Dysbetalipoproteinemia (type III according to Frederickson) (as a supplement to the diet).
- Familial endogenous hypertriglyceridemia (type IV according to Frederickson), resistant to diet.
ELIBRARY.RU. Homozygous familial hypercholesterolemia with insufficient effectiveness of diet therapy and other non-pharmacological treatment methods.
- Primary prevention of cardiovascular complications in patients without clinical signs of coronary artery disease, but having several risk factors for its development:
- Age over 55 years.
- Nicotine addiction.
- Arterial hypertension .
- Diabetes.
- Low concentrations of Xc-HDL in plasma.
- Genetic predisposition, incl. against dyslipidemia.

- In patients with coronary artery disease with the aim of reducing the total mortality rate.
- Myocardial infarction.
- Stroke.
- Re-hospitalization for angina and the need for revascularization.

- Hypersensitivity to any of the components of the drug.
- Active liver disease or increased serum transaminase activity (AST, ALT) (more than 3 times compared with the upper limit of normal) of unclear genesis.
- Women of reproductive age who do not use adequate methods of contraception.
- Pregnancy.
- Lactation (breastfeeding).
- Age up to 18 years (not enough clinical data on the efficacy and safety of the drug in this age group).

Carefully:

- Alcohol abuse.
- Liver disease (in history).

Liprimar is contraindicated in pregnancy.

Women of reproductive age during treatment should use adequate methods of contraception. Liprimar can be prescribed to women of reproductive age only if the probability of pregnancy is very low and the patient is informed of the possible risk to the fetus during treatment.

Liprimar is contraindicated during lactation.

It is not known whether atorvastatin is excreted in breast milk.If necessary, the appointment of the drug during lactation, breastfeeding should be stopped to avoid the risk of adverse events in infants.

Inside Take at any time of the day, regardless of the meal.

Before starting treatment with Liprimar, you should try to control hypercholesterolemia with diet, exercise and weight loss in obese patients, as well as treatment of the underlying disease.

When prescribing the drug, the patient should be advised to recommend a standard cholesterol-lowering diet, which he must follow during treatment.

The dose of the drug varies from 10 to 80 mg 1 time per day and is titrated based on the initial content of Xc-LDL, the goal of therapy and the individual effect.

The maximum daily dose for a single dose is 80 mg.

At the beginning of treatment and / or during a dose increase of Liprimar, it is necessary to monitor plasma lipid levels every 2-4 weeks and adjust the dose accordingly.

- With primary hypercholesterolemia and combined (mixed) hyperlipidemia. For most patients - 10 mg 1 time / day. The therapeutic effect occurs within 2 weeks and usually reaches a maximum within 4 weeks. With long-term treatment, the effect is preserved.

- When homozygous familial hypercholesterolemia. The drug is prescribed at a dose of 80 mg 1 time / day (in most cases, therapy led to a decrease in the level of Xc-LDL by 18-45%).

- In case of insufficient liver function, the Liprimar dose should be reduced, with constant monitoring of the activity of “liver” transaminases: aspartate aminotransferase (ACT) and alanine aminotransferase (ALT).

- In case of insufficiency of the kidney function Impaired renal function does not affect the plasma atorvastatin level or the degree of decrease in the LDL-C content when using Liprimar, therefore, changing the dose of the drug is not required.

- In elderly patients There were no differences in safety, efficacy, or achievement of lipid-lowering therapy goals in comparison with the general population.

- Use in combination with other drugs. If necessary, the joint use with cyclosporine dose of the drug should not exceed 10 mg.

In determining the goal of treatment, you can use the following recommendations:

- A. Recommendations of the National Cholesterol Education Program NCEP, USA. Category of risk Target content of Hc-LDL (mg / dl) Content of Hc-LDL, which recommends a change in lifestyle (mg / dl) Content of Hc-LDL, at which pharmacotherapy is recommended (mg / dl) IHD or the risk of developing IHD (10- summer risk> 20%)