Vasator pills 10mg, 30pcs

Composition

1 tablet contains: Active ingredients:  atorvastatin calcium is 10.34 mg, which corresponds to the content of atorvastatin 10 mg. Excipients: microcrystalline cellulose-54.4 mg, lactose monohydrate-54.95 mg, calcium carbonate-5 mg, povidone-5 mg, colloidal silicon dioxide-5 mg, croscarmellose sodium-7 mg, magnesium stearate-3 mg.

Composition of the film shell:  Hypromellose-4.1 mg, macrogol 6000-1.2 mg, titanium dioxide-0.6 mg, talc-1.2 mg, iron oxide red dye-0.07 mg

Pharmacological action Pharmacotherapy group: Hypolipidemic agent-HMG-CoA reductase inhibitorpharmacological action

Hypolipidemic agent from the statin group. Selective competitive inhibitor of HMG-CoA reductase, an enzyme that converts Z-hydroxy-Z-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 the concentration of cholesterol and lipoproteins in blood plasma 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 uptake and catabolism of LDL. Reduces the formation of LDL, causes a pronounced and persistent increase in the activity of LDL receptors. Reduces LDL concentrations in patients with homozygous familial hypercholesterolemia, which usually does not respond to lipid-lowering therapy. Reduces the concentration of total cholesterol by 30-46%, LDL-by 41-61%, apolinoprotein B-by 34-50% and TG-by 14-33%; causes an increase in the concentration of HDL cholesterol (high-density linoprotins) 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. C_max in blood plasma is reached in 1-2 hours, C_max in women is 20% higher, the area under the concentration-time curve (AUC) is 10% lower; C_max in patients with alcoholic cirrhosis of the liver is 16 times higher, AUC is 11 times higher than normal.

Food intake 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.

V_d– 381 l, binding to plasma proteins-98%. It is mainly metabolized in the liver under the action of isoenzymes 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 through the intestine with bile after hepatic and / or extrahepatic metabolism (does not undergo pronounced enterohepatic recirculation). T_1/2 – 14 h. 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 increasing HDL cholesterol 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 triglyceride levels (type IV according to Fredrickson) and patients with dysbetalipoproteinemia (type III Fredrickson), whose diet does not provide an adequate effect;
• to reduce 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

Vasizer 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 with Vasator.

Vazor can only be prescribed to women of reproductive age if the probability of pregnancy is very low, and the patient is informed about the possible risk of treatment for the fetus.

Contraindications

• hypersensitivity to the components of the drug;
• active liver disease or increased activity of “liver” enzymes of unknown origin (more than 3 times compared with the upper limit of normal); hepatic failure (severity classes A and b according to the classification of child-Pugh);
• pregnancy;
• lactation;
• lactase deficiency, lactose intolerance, glucose-galactose malabsorption;
• the age of 18 years (effectiveness and safety not established).

With caution:  alcohol abuse, a history of liver disease, severe water-electrolyte balance disorders, endocrine and metabolic disorders, hypotension, severe acute infections (sepsis), uncontrolled epilepsy, extensive surgical interventions, injuries, skeletal muscle diseases.

Side effects

From the central nervous system:  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.

From the respiratory system: 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, liver dysfunction, rectal bleeding, melena, bleeding gums, tenesmus.

From the musculoskeletal system:  arthritis; leg muscle cramps, bursitis, tendosynovitis, myositis, myopathy, arthralgia, myalgia, rhabdomyolysis, torticollis, muscle hypertonus, joint contractures.

From the genitourinary system:  urogenital infections, peripheral edema; dysuria (including pollakiuria, nocturia, urinary incontinence or urinary retention, imperative urination), nephritis, hematuria, vaginal bleeding, nephrourolithiasis, metrorrhagia, epididymitis, decreased libido, impotence, ejaculation disorders.

From the side of the skin:  alopecia, xeroderma, increased sweating, eczema, seborrhea, ecchymosis, petechiae.

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

Laboratory parameters:  hyperglycemia, hypoglycemia, increased serum creatine phosphokinase (CPK), albuminuria.

Other services:  weight gain, gynecomastia, mastodynia, gout exacerbation.

Interaction

The risk of myopathy during treatment with other drugs of this class increases with the simultaneous use of cyclosporine, fibrates, erythromycin, antifungal agents related to azoles, and nicotinic acid. Concomitant oral administration of atorvastatin and a suspension containing magnesium and aluminum hydroxide reduced plasma concentrations of atorvastatin by approximately 35%, but the degree of reduction in LDL/cholesterol levels did not change. Concomitant use of atorvastatin does not affect the pharmacokinetics of antipyrine (phenazone), so interaction with other agents metabolized by the same cytochrome isoenzymes is not expected.

When colestipol was co-administered, plasma concentrations of atorvastatin decreased by approximately 25%. However, the lipid-lowering effect of the combination of atorvastatin and colestipol exceeded that of each drug separately. Steady-state plasma concentrations of digoxin and atorvastatin did not change with repeated use of digoxin and atorvastatin at a dose of 10 mg. However, when using digoxin in combination with atorvastatin at a dose of 80 mg/day, the concentration of digoxin increased by about 20%. Patients receiving digoxin in combination with atorvastatin should be monitored. Concomitant use of atorvastatin and erythromycin (500 mg 4 times / day) or clarithromycin (500 mg 2 times / day), which inhibit the SURZA 4 isoenzyme, an increase in the concentration of atorvastatin in blood plasma was observed. Concomitant use of atorvastatin (10 mg 1 time/day) and azithromycin (500 mg 1 time/day) did not change the concentration of atorvastatin in blood plasma.

Atorvastatin did not have a clinically significant effect on the plasma concentration of terfenadine, which is mainly metabolized by SURZA 4; therefore, it seems unlikely that atorvastatin can significantly affect the pharmacokinetic parameters of other substrates of the SURZA 4 isoenzyme.

When atorvastatin was co-administered with an oral contraceptive containing norethisterone and ethinylestradiol, a significant increase in the AUC of norethindrone and ethinylestradiol by approximately 30% and 20%, respectively, was observed. This effect should be considered when choosing an oral contraceptive for a woman receiving atorvastatin.

Concomitant use with drugs that reduce the concentration of endogenous steroid hormones (including cimetidine, ketoconazole, spironolactone) increases the risk of reducing endogenous steroid hormones (caution should be exercised).

When studying the interaction of atorvastatin with warfarin and cimetidine, no clinically significant interaction was found.

Concomitant use of atorvastatin 80 mg and amlodipine 10 mg did not alter the pharmacokinetics of atorvastatin at steady state.

There was no clinically significant adverse interaction between atorvastatin and antihypertensive agents.

Concomitant use of atorvastatin with protease inhibitors, known as SURZA 4 inhibitors, was accompanied by an increase in the concentration of atorvastatin in blood plasma. Pharmaceutical incompatibilities are not known.

How to take, course of use and dosage

Before prescribing Vazor, the patient should be recommended a standard lipid-lowering diet, which he should continue to follow throughout the entire period of therapy.

The initial dose is on average 10 mg 1 time/day. The dose varies from 10 to 80 mg 1 time/day.

The drug can be taken at any time of the day with food or regardless of the time of meal. The dose is selected taking into account the initial cholesterol/LDL levels, the purpose of therapy and the individual effect. At the beginning of treatment and/or during an increase in the dose of atorvastatin, it is necessary to monitor the concentration of lipids in blood plasma every 2-4 weeks and adjust the dose accordingly.

Primary hypercholesterolemia and mixed hyperlipidemia. as well as type III and IV according to Fredrickson: in most cases, it is sufficient to prescribe a dose of 10 mg of Vasizer 1 time/day. A significant therapeutic effect is observed after 2 weeks, as a rule, and the maximum therapeutic effect is usually observed after 4 weeks. With long-term treatment, this effect persists.

Homozygous familial hypercholesterolemia: the drug is used in a dose of 80 mg (4 tablets of 20 mg) 1 time/day. Do not use more than 4 tablets of 10 mg dosage per day-do not replace the 20 mg dosage with a 10 mg dosage with a daily dose of 80 mg

The use of the drug in patients with renal insufficiency and kidney diseases does not affect the level of atorvastatin in blood plasma or the degree of reduction in cholesterol/LDL when it is used, so a change in the dose of the drug is not required.

In case of hepatic insufficiency, the dose should be reduced (see sections “With caution” and “Special instructions”).

When using the drug in elderly patients, there were no differences in the safety, effectiveness or achievement of the goals of lipid-lowering therapy in comparison with the general population.

Overdose

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

Special instructions

Before starting therapy with Vasator, the patient should be prescribed a standard hypocholesterolemic diet, which he must follow during the entire treatment period.

The use of HMG-CoA reductase inhibitors to reduce the concentration of lipids in the blood can lead to changes in biochemical parameters that reflect liver function. Liver function should be monitored before starting therapy,6 weeks,12 weeks after starting Vasizer and after each dose increase, as well as periodically, for example, every 6 months. An increase in the activity of “liver” enzymes in the blood serum can be observed during Vasator therapy. Patients who show an increase in enzyme activity should be monitored until the enzyme activity returns to normal. In the event that the ALT or ACT values are more than 3 times higher than the upper permissible limit, it is recommended to reduce the dose of Vasator or stop treatment.

Vasizer should be used with caution in patients who abuse alcohol and / or have liver disease. Active liver disease or a persistent increase in the activity of” liver ” transferases of unknown origin serve as contraindications to the appointment of a Vasizer.

Vasodilator treatment can cause myopathy. The diagnosis of myopathy (muscle pain and weakness combined with an increase in CK activity of more than 10 times the upper limit of normal) should be discussed in patients with advanced myalgia, muscle soreness or weakness, and/or a pronounced increase in CK activity. Patients should be warned that they should immediately inform the doctor about the appearance of unexplained pain or weakness in the muscles, if they are accompanied by malaise or fever. Vasator therapy should be discontinued if there is a marked increase in CKD activity or if there is a confirmed or suspected myopathy. The risk of myopathy during treatment with other drugs of this class increased with the simultaneous use of cyclosporine, fibrates, erythromycin, nicotinic acid in lipid-lowering doses or azole antifungal agents. Many of these drugs inhibit SURZA 4-mediated metabolism and / or drug transport.

Atorvastatin is biotransformed under the action of the SURZA 4 isoenzyme. When prescribing a Vasizer in combination with fibrates, erythromycin, immunosuppressive agents, azole antifungal agents or nicotinic acid in lipid-lowering doses, the expected benefit and risk of treatment should be carefully weighed and patients should be regularly monitored for muscle pain or weakness, especially during the first months of treatment and during the period of increasing the dose of any drug. In such situations, periodic monitoring of CPK activity can be recommended, although such monitoring does not prevent the development of severe myopathy.

Cases of rhabdomyolysis with acute renal failure due to myoglobinuria have been reported with the use of the Vasator, as well as other agents of this class. Vasator therapy should be temporarily discontinued or completely discontinued if there are signs of possible myopathy or a risk factor for developing renal failure due to rhabdomyolysis (for example, severe acute infection, hypotension, extensive surgery, trauma, severe metabolic, endocrine and electrolyte disorders, and uncontrolled seizures).

Before starting therapy with Vasator, it is necessary to try to achieve control of hypercholesterolemia through adequate diet therapy, increased physical activity, weight loss in obese patients, and treatment of other conditions. Patients should be warned to seek immediate medical attention if they experience unexplained muscle pain or weakness, especially if they are accompanied by malaise or fever.

Influence on the ability to drive vehicles and mechanisms

In some patients, the drug may cause dizziness and other side effects that may affect the ability to drive vehicles and work with mechanisms. In this regard, when using the Vaz, care should be taken when driving vehicles and other complex mechanisms that require increased attention.

Storage conditions

Keep out of reach of children, dry and protected from light at a temperature not exceeding 25 °C.

Shelf

life is 2 years.

Active ingredient

Atorvastatin

Conditions of release from pharmacies

By prescription

Dosage form

Tablets