Liprimar is a selective competitive inhibitor of HMG-CoA reductase; synthetic lipid-lowering drug.
Release form and composition
Liprimara dosage form - tablets: elliptical, film-coated white; on the break - white core:
- With “10” engraving on one side and PD “155” - on the other (10 pieces in blisters, in a cardboard box of 3 or 10 blisters);
- With “20” engraving on one side and PD “156” - on the other (10 pieces in blisters, in a cardboard box 3 or 10 blisters);
- With “40” engraving on one side and PD “157” - on the other (10 pieces in blisters, in a cardboard box 3 blisters);
- With “80” engraving on one side and PD “158” - on the other (10 pieces in blisters, in a cardboard box 3 blisters).
Each tablet contains:
- Active ingredient: atorvastatin (in the form of a calcium salt) - 10, 20, 40 or 80 mg;
- Auxiliary components: croscarmellose sodium, magnesium stearate, lactose monohydrate, microcrystalline cellulose, calcium carbonate, hyprolose, polysorbate;
- The composition of the film shell: opadry white YS-1-7040 (candelamine wax, titanium dioxide, polyethylene glycol, talc, hypromellose, simethicone emulsion (emulsifier stearic, sorbic acid, simethicone, water)).
Indications for use
Treatment of the following diseases:
- Primary hypercholesterolemia (heterozygous familial and non-familial hypercholesterolemia (type IIa according to Fredrickson's classification);
- Familial endogenous hypertriglyceridemia (type IV according to the Fredrickson classification), resistant to diet;
- Disbetalipoproteinemia (type III according to Fredrickson's classification) (in addition to the diet);
- Combined hyperlipidemia (IIa and IIb types according to the Fredrickson classification);
- Homozygous familial hypercholesterolemia (the drug is used in case of insufficient effectiveness of non-pharmacological treatment methods, including diet therapy).
Liprimar is also prescribed for preventive purposes:
- Primary prevention of cardiovascular complications in patients without clinical signs of coronary heart disease, but with several risk factors contributing to its development: age over 55 years old, smoking, diabetes mellitus, hypertension, genetic predisposition, low concentration of high-density lipoprotein cholesterol (Xc-HDL) in plasma;
- Secondary prevention of cardiovascular complications in patients with coronary heart disease in order to reduce the risk of angina pectoris, stroke, myocardial infarction, death, and the need for revascularization.
- Active liver disease or increased activity of hepatic transaminases of unclear genesis (more than 3 times as compared with that in congenital adrenal hyperplasia);
- Age up to 18 years;
- Lactation (or feeding should be stopped);
- Hypersensitivity to the drug.
Relative (special caution required):
- A history of liver disease;
- Alcohol abuse.
Dosing and Administration
Before starting Liprimar, it is necessary to control hypercholesterolemia with the help of diet therapy, exercise and weight loss in patients with obesity, as well as through the treatment of the underlying disease.
The drug should be taken orally once a day at any time of the day, regardless of the meal.
The daily dose can vary from 10 to 80 mg. The doctor selects the dose, taking into account the indications, the initial cholesterol content of low-density lipoprotein (Xc-LDL) and the therapeutic efficacy of Liprimar.
With primary hypercholesterolemia and combined hyperlipidemia, a daily dose of 10 mg is sufficient for most patients. The therapeutic effect is manifested within 2 weeks, reaching a maximum after about 4 weeks.
With homozygous familial hypercholesterolemia, the drug is usually prescribed in a daily dose of 80 mg.
Patients with hepatic insufficiency should lower the dose of Liprimar under the constant control of the activity of alanine aminate transferase (ALT) and aspartate aminotransferase (AST).
The entire period of treatment, the patient must adhere to the doctor recommended standard cholesterol-lowering diet.
Every 2-4 weeks at the beginning of treatment and at each dose increase it is necessary to control the content of lipids in the blood and, if necessary, adjust the dose.
If necessary, combined treatment with the use of cyclosporine dose Liprimar should not exceed 10 mg.
Basically, the drug is well tolerated. Side effects, if they occur, usually have a slight severity and transient nature.
Possible adverse reactions:
- Central nervous system: often (≥1%) - headache, insomnia, asthenic syndrome; rarely (≤1%) - dizziness, hypesthesia, paresthesia, malaise, peripheral neuropathy, amnesia;
- The digestive system: often - abdominal pain, flatulence, dyspepsia, nausea, diarrhea, constipation; rarely - vomiting, cholestatic jaundice, pancreatitis, hepatitis, anorexia;
- Musculoskeletal system: often - myalgia; rarely - myositis, muscle cramps, myopathy, rhabdomyolysis, back pain, arthralgia;
- Hematopoietic system: rarely - thrombocytopenia;
- Metabolism: rarely - hyperglycemia, hypoglycemia, increased serum creatine phosphokinase levels;
- Allergic reactions: rarely - itching, skin rash, urticaria, bullous rash, toxic epidermal necrolysis, erythema multiforme exudative, anaphylactic reactions;
- Other: rarely - chest pain, impotence, fatigue, weight gain, tinnitus, alopecia, secondary renal failure, peripheral edema.
Like other lipid-lowering drugs of the same class, Liprimar may affect the activity of liver enzymes. For this reason, before his appointment, after 6 and 12 weeks after the start of use, with each increase in dose, as well as periodically throughout the course of treatment, it is necessary to monitor the functional indicators of the liver. The study of liver function is necessary in the case of clinical signs of its defeat. If the increase in ALT or AST activity is more than 3 times compared with the same indicator in case of congenital adrenal hyperplasia, the dose should be reduced or the drug withdrawn.
There are reports of rare cases of rhabdomyolysis, accompanied by acute renal failure due to myoglobinuria, in patients taking Liprimar. For this reason, if there is a risk factor for renal failure due to rhabdomyolysis (such as severe acute infection, trauma, extensive surgical intervention, arterial hypotension, endocrine, electrolyte and metabolic disorders, uncontrolled seizures) or when symptoms appear that can be suspected myopathy, Liprimar should be temporarily or completely canceled.
All patients must be warned that they should immediately see a doctor if they develop weakness or unexplained muscle pain, especially if they are accompanied by fever and / or malaise.
Women of reproductive age Liprimar can be prescribed only if the probability of pregnancy in them is minimized, and the patients themselves are informed of the possible risks. The entire period of treatment should use reliable methods of contraception.
Information about the effect of atorvastatin on the reaction rate and concentration of attention is missing.
With the simultaneous use of fibrates, cyclosporins, nicotinic acid in lipid-lowering doses, clarithromycin, erythromycin and antifungal agents derived from azole, the risk of myopathy increases.
Atorvastatin is metabolized by a CYP3A4 isoenzyme, therefore inhibitors of this isoenzyme (including clarithromycin, itraconazole and erythromycin, diltiazem) can significantly increase the plasma concentration of atorvastatin.
It should be borne in mind that grapefruit juice contains at least one component that inhibits the CYP3A4 isoenzyme, so its excessive consumption (more than 1.2 liters per day) can lead to an increase in atorvastatin concentration in the blood.
Inductors of cytochrome CYP3A4 isoenzyme (for example, efavirenz and rifampicin) can reduce the concentration of atorvastatin in the blood plasma. If necessary, the simultaneous use of rifampicin, both drugs are recommended to take at the same time, because The delayed use of Liprimar after rifampicin leads to a significant decrease in the level of atorvastatin in the blood.
OATP1B1 inhibitors (for example, cyclosporin) can increase the bioavailability of atorvastatin.
At the same time taking antacids containing aluminum or magnesium hydroxide, the concentration of atorvastatin is reduced by about 35%, however, this does not affect the degree of decrease in the level of Xc-LDL.
Colestipol reduces plasma atorvastatin concentrations by about 25%, however, the lipid-lowering effect of this combination surpasses the effects of taking each drug separately.
If necessary, the appointment of Liprimar simultaneously with digoxin requires clinical monitoring.
When choosing an oral contraceptive for a woman undergoing Liprimar treatment, it should be borne in mind that atorvastatin significantly increases the concentration of ethinyl estradiol and norethisterone (approximately 20% and 30%, respectively).
Terms and conditions of storage
Keep out of the reach of children at a temperature not exceeding 25 ° C.
Shelf life - 3 years.