Atorvastatin-Teva, pills 40mg 30pcs

Composition

1 tablet contains:

Active ingredient:

atorvastatin calcium trihydrate 40 mg;

Auxiliary substances:

calcium carbonate;

MCC;

StarCap 1500 (corn starch and pre-gelatinized starch);

colloidal silicon dioxide (aerosil);

talc;

magnesium stearate;

Opadry II (series 85) (polyvinyl alcohol, macrogol, talc, titanium dioxide, iron oxide yellow dye, iron oxide red dye).

Pharmacological action

Pharmacodynamics

Atorvastatin is a hypolipidemic agent from the statin group. Selective competitive inhibitor of HMG-CoA reductase, an enzyme that converts 3-hydroxy-3-methylglutaryl coenzyme A to mevalonic acid, a precursor of sterols, including cholesterol. Triglycerides (TG) and cholesterol in the liver are incorporated into very low-density lipoproteins (VLDL), enter the blood plasma and are transported to peripheral tissues. Low-density lipoproteins (LDL) are formed from VLDL during interaction with LDL receptors. Atorvastatin reduces plasma cholesterol and lipoprotein levels by inhibiting 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 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 treatment with lipid-lowering agents. 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 lipoproteins) and apolipoprotein A. Dose-dependent reduces the level of LDL in patients with homozygous hereditary hypercholesterolemia, resistant to therapy with other lipid-lowering agents.

Pharmacokinetics

Absorption is high. The maximum concentration (Cmax) in blood plasma is reached in 1-2 hours, Cmax in women is 20% higher, the area under the curve/concentration, time (AUC) is 10% lower; Cmax in patients with alcoholic cirrhosis of the liver is 16 times higher, AUC is 11 times higher than normal.

Food slightly reduces the rate and duration of drug absorption (by 25% and 9%, respectively), but the reduction in LDL cholesterol is similar to that when using Atorvastatin without food. The concentration of Atorvastatin when used in the evening is lower than in the morning (by approximately 30%). A linear relationship was found between the degree of absorption and the dose of the drug.

Bioavailability – 12%, systemic bioavailability of inhibitory activity against HMG-CoA reductase-30%. Low systemic bioavailability is due to presystemic metabolism in the gastrointestinal mucosa and during the” first pass ” through the liver.

The average volume of distribution is 381 liters, and the binding to plasma proteins is 98%. It is mainly metabolized in the liver under the action of cytochrome CYP3A4, CYP3A5 and CYP3A7 with the formation of pharmacologically active metabolites (ortho – and parahydroxylated derivatives, beta-oxidation products). In vitro, ortho-and parahydroxylated metabolites have an inhibitory effect on HMG-CoA reductase comparable to that of Atorvastatin. The inhibitory effect of the drug on HMG-CoA reductase is approximately 70% determined by the activity of circulating metabolites.

It is excreted in bile after hepatic and / or extrahepatic metabolism (does not undergo pronounced enterohepatic recirculation).

The elimination half-life is 14 hours. Inhibitory activity against HMG-CoA reductase persists for about 20-30 hours due to the presence of active metabolites. Less than 2% of the oral dose of the drug is detected in the urine. It is not excreted during hemodialysis.

Indications

• in conjunction with diet to reduce elevated levels of total Cholesterol, Cholesterol-LDL, and apolipoprotein b and triglycerides and improve HDL-C 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 elevated serum TG levels (type IV according to Fredrickson) and patients with dysbetalipoproteinemia (type III Fredrickson), whose diet does not provide an adequate effect;
• to reduce the levels 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 of treatment for the fetus.

Contraindications

• active liver diseases;
• increased activity of liver enzymes of unknown origin (more than 3 times compared to ULN);
• liver failure (Child-Pugh class A and B);
• pregnancy;
• lactation;
• age up to 18 years (efficacy and safety have not been established);
• hypersensitivity to the components of the drug.

The drug should be used with caution in patients with chronic alcoholism, a history of liver diseases, severe electrolyte disturbances, endocrine and metabolic disorders, arterial hypotension, severe acute infections (sepsis), uncontrolled epilepsy, extensive surgical interventions, injuries, and skeletal muscle diseases.

Side effects

Nervous system disorders:  insomnia, dizziness; 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:  amblyopia, tinnitus, dry conjunctiva, accommodation disorders, retinal hemorrhage, deafness, glaucoma, parosmia, loss of taste sensations, taste distortion.

From the cardiovascular system:  chest pain; palpitations, symptoms of vasodilation, orthostatic hypotension, increased blood pressure, phlebitis, arrhythmia, angina pectoris.

From the hematopoietic system:  anemia, lymphadenopathy, and thrombocytopenia.

Respiratory system disorders:  bronchitis, rhinitis; pneumonia, dyspnoea, exacerbation of bronchial asthma, nosebleeds.

From the digestive system:  nausea; 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, impaired liver function, rectal bleeding, melena, bleeding gums, tenesmus.

Musculoskeletal disorders:  arthritis; leg muscle cramps, bursitis, tendosynovitis, myositis, myopathy, arthralgia, myalgia, rhabdomyolysis, torticollis, muscle hypertonus, joint contractures, joint swelling, tendopathy (in some cases with tendon rupture).

From the genitourinary system:  urogenital infections, peripheral edema;

Dermatological reactions:  alopecia, xeroderma, photosensitivity, increased sweating, eczema, seborrhea, ecchymosis, petechiae.

From the endocrine system:  gynecomastia, mastodynia.

From the side of metabolism:  weight gain, exacerbation of gout.

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

Laboratory parameters:  hyperglycemia, hypoglycemia, increased serum creatinine clearance, albuminuria.

Interaction

The risk of myopathy during treatment with other drugs derived from statins increases with the simultaneous use of cyclosporine, fibrates, erythromycin, antifungal agents related to azoles, and nicotinic acid.

With simultaneous ingestion Atorvastatin and a suspension containing magnesium hydroxide and aluminum hydroxide, the concentration of atorvastatin in blood plasma decreased by about 35%, but the degree of reduction in LDL-C levels did not change.

When used simultaneously Atorvastatin does not affect the pharmacokinetics of antipyrine (phenazone), so interaction with other drugs metabolized by the same cytochrome P450 isoenzymes is not expected.

How to take it, course of administration and dosage

Inside.

Usually, the initial dose is 10 mg once a day. The dose varies from 10 to 80 mg / day.The drug can be taken at any time of the day once a day, regardless of food intake. Doses should be selected individually, taking into account the initial LDL cholesterol level, the purpose of therapy, and the patient’s response to treatment. At the beginning and/or during an increase in the dose of Atorvastatin-Teva, it is necessary to monitor the level of lipids in blood plasma every 2-4 weeks and adjust the dose accordingly.

Dose adjustments should be made at intervals of at least 4 weeks. The maximum daily dose is 80 mg.

For patients with established CHD and other patients at high risk of cardiovascular events, the following lipid correction targets are recommended: LDL cholesterol of less than 3 mmol/L (or less than 115 mg/dl) and total cholesterol of less than 5 mmol/L (or less than 190 mg/dl).

Primary hypercholesterolemia and combined (mixed) hyperlipidemia

In most patients, the necessary control of lipid levels is provided by taking 10 mg of Atorvastatin-Teva 1 time a day. A significant therapeutic effect is usually observed after 4 weeks. With long-term treatment, this effect persists.

Heterozygous familial hypercholesterolemia

Treatment of patients should begin with the appointment of 10 mg of Atorvastatin-Teva per day. Individual dose adjustments should be made every 4 weeks to 40 mg / day. After that, you can increase the dose to a maximum level of 80 mg / day, or use a combined appointment of 40 mg of Atorvastatin-Teva and bile acid sequestrant.

Homozygous familial hypercholesterolemia

The drug is prescribed at a dose of 80 mg once a day.

In patients with renal insufficiency

, renal diseases do not affect the concentration of atorvastatin in blood plasma or the degree of lipid reduction when it is used; therefore, no dose adjustment is required in patients with kidney disease.

In patients with hepatic insufficiency

In case of hepatic insufficiency, it may be necessary to reduce the dose or cancel the drug.

Overdose

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

Special instructions

Before and during treatment with Atorvastatin, especially if symptoms of liver damage appear, it is necessary to monitor liver function indicators.

If the level of transaminases increases, their activity should be monitored until normalization. If the activity of AST or ALT, more than 3 times higher than normal, persists, it is recommended to reduce the dose or cancel Atorvastatin.

Form of production

Tablets

Storage conditions

At a temperature not exceeding 30 °C

Shelf life

2 years

Active ingredient

Atorvastatin

Conditions of release from pharmacies

By prescription

Dosage form

Tablets