Pharmacological properties of the drug Lipitor

Lipitor is used in conjunction with a specific diet to lower cholesterol and fat (triglycerides) levels in the blood. This remedy is usually used in cases where cholesterol-lowering medications (eg, dietary changes, weight loss, if overweight) have not been successful enough. Lowering your cholesterol levels can help prevent a heart attack. Lipitor is used in adults and children (10 years and older). Young girls must have had their first menstrual period before starting this drug. This medication belongs to an enzyme blocker, also known as "statin".

Lipid-lowering agent from the statin group. Selective competitive inhibitor of HMG-CoA reductase, an enzyme that converts 3-hydroxy-3-methylglutaryl coenzyme A into mevalonic acid, which is a precursor of sterols, including cholesterol.

TG and cholesterol in the liver are included in VLDL, enter the plasma and are transported to peripheral tissues. LDL is formed from VLDL in the course of interaction with LDL receptors.

Taking the drug reduces plasma cholesterol and lipoprotein levels by inhibiting HMG-CoA reductase, 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 LDL.

Reduces the formation of LDL, causes a pronounced and persistent increase in the activity of LDL receptors. Reduces the level of LDL in patients with homozygous familial hypercholesterolemia, which usually does not respond to lipid-lowering drugs.

Reduces the level of total cholesterol by 30-46%, LDL - by 41-61%, apolipoprotein B - by 34-50% and TG - by 14-33%; causes an increase in the level of HDL cholesterol (high density lipoprotein) and apolipoprotein A.

Taking the drug Lipitor dose-dependently reduces the level of LDL in patients with homozygous hereditary hypercholesterolemia resistant to therapy with other

lipid-lowering drugs.

Treatment with Lipitor significantly reduces the risk of ischemic complications (including the development of death from myocardial infarction) by 16%, the risk of re-hospitalization for angina pectoris, accompanied by signs of myocardial ischemia, by 26%.

Atorvastatin has no carcinogenic or mutagenic effects.

Mechanism of action

Lipitor reduces the levels of cholesterol and lipoproteins in the blood plasma while suppressing the activity of HMG-CoA reductase, cholesterol synthesis in the liver and an increase in the number of hepatic LDL receptors on the cell surface, which leads to increased uptake and catabolism of LDL.

The drug leads to a reduced formation of LDL, to a pronounced and persistent increase in the activity of LDL receptors. Reduces the level of LDL in patients with homozygous familial hypercholesterolemia, resistant to treatment with other lipid-lowering drugs.

Efficacy

According to the results of clinical studies, Lipitor significantly reduces the risk of ischemic complications (including death from myocardial infarction), the risk of re-hospitalization due to angina pectoris, accompanied by signs of myocardial ischemia.

Indications for use the drug Lipitor

• heterozygous familial and nonfamilial (primary) hypercholesterolemia, according to Frederickson's type IIa), combined hyperlipidemia (according to Frederickson's types IIb and III), dysbetalipoproteinemia (according to Frederickson's type III) (in addition to diet), familial endogenous hypertriodenitis ), which cannot be corrected by diet.

• homozygous hereditary hypercholesterolemia (in addition to hypolipidemic therapy, including autohemotransfusion of blood purified from LDL).

• cardiovascular diseases against the background of dyslipidemia,

• secondary prevention to reduce the overall risk of death, myocardial infarction and re-hospitalization due to angina pectoris.

Method of administration of the drug Lipitor

The dose is set individually, depending on the initial cholesterol level.

The drug is taken orally, regardless of food intake. The initial dose of Lipitor is 10 mg once a day. The maximum daily dose is 80 mg once a day.

The effect appears within 2 weeks, and the maximum effect within 4 weeks.

Application during pregnancy and lactation

The drug is contraindicated during pregnancy and lactation.

Interaction with other drugs

With the simultaneous administration of cyclosporine, fibrates, erythromycin, clarithromycin, immunosuppressive, antifungal drugs (related to azoles) and nicotinamide with atorvastatin, the concentration of atorvastatin in plasma (and the risk of myopathy) increases.

Antacids reduce the concentration by 35% (the effect on LDL cholesterol does not change).

The simultaneous use of atorvastatin with protease inhibitors, known as inhibitors of cytochrome CYP3A4, is accompanied by an increase in the concentration of the drug in plasma.

When using digoxin in combination with atorvastatin at a dose of 80 mg / day, the concentration of digoxin increases by about 20%.

Increases the concentration by 20% (when administered with the drug at a dose of 80 mg / day) of oral contraceptives containing norethindrone and ethinyl estradiol.

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

Overdose

Treatment of overdose: there is no specific antidote, symptomatic therapy is performed. Hemodialysis is ineffective.

Contraindications

• high sensitivity to the drug;

• liver disease with severe dysfunction;

• pregnancy, lactation.

Side effect

From the nervous system: more often 2% - insomnia, dizziness; less often 2% - headache, asthenia, malaise, drowsiness, unusual dreams, amnesia, paresthesia, peripheral neuropathy, amnesia, emotional lability, ataxia, paralysis of the facial nerve, hyperkinesis, depression, hyperesthesia, loss of consciousness.

From the senses: less often 2% - amblyopia, ringing in the ears, dryness of the conjunctiva, impaired accommodation, bleeding in the eyes, deafness, glaucoma, parosmia, loss of taste, taste perversion.

From the digestive system: more often 2% - nausea; less often 2% - heartburn, constipation or diarrhea, flatulence, gastralgia, abdominal pain, anorexia, 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.

From the respiratory system: more often 2% - bronchitis, rhinitis; less often 2% - pneumonia, dyspnea, bronchial asthma, nosebleeds.

From the CCC: more often 2% - chest pain; less often 2% - palpitations, vasodilation, migraine, postural hypotension, increased blood pressure, phlebitis, arrhythmia, angina pectoris.

From the hematopoietic system: less often 2% - anemia, lymphadenopathy, thrombocytopenia.

From the side of the musculoskeletal system: more often 2% - arthritis; less often 2% - leg muscle cramps, bursitis, tendosynovitis, myositis, myopathy, arthralgia, myalgia, rhabdomyolysis, torticollis, muscle hypertonia, joint contractures.

From the genitourinary system: more often 2% - urogenital infections, peripheral edema; less often 2% - dysuria (including

pollakiuria, nocturia, urinary incontinence or urinary retention, urgency to urinate), nephritis, hematuria, vaginal bleeding, nephrourolithiasis, metrorrhagia, epididymitis, decreased libido, impotence, impaired ejaculation.

On the part of the skin: more often 2% - alopecia, xeroderma, increased sweating, eczema, seborrhea, ecchymosis, petechiae.

Allergic reactions to the components of the drug: less often 2% - itching, skin rash, contact dermatitis, rarely - urticaria, angioedema, facial edema, photosensitivity, anaphylaxis, exudative erythema multiforme (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome).

Laboratory indicators: less often 2% - hyperglycemia, hypoglycemia, increased serum CPK, albuminuria.

Others: less often 2% - increase in body weight, gynecomastia, mastodynia, exacerbation of gout.

Seek immediate medical attention if you develop these muscle problems (especially fever or unusual tiredness). If you experience such unusual but serious side effects of Lipitor as stomach heaviness / abdominal pain, nausea, yellowing of the eyes and skin, dark urine, severe fatigue, changes in the amount of urine, then inform your doctor right away.

Seek medical attention if you experience a severe allergic reaction. Symptoms of serious allergic reactions are: severe dizziness, hives, itching, swelling, and breathing problems.