Atorvastatin | Atoris tablets 10 mg, 30 pcs.

film release s rdlkp Film-coated tablets

Packing

30 pcs

Pharmacological action

Atorvastatin is a lipid-lowering drug from the group of statins. The main mechanism of action of atorvastatin is the inhibition of the activity of HMG-CoA reductase, an enzyme that catalyzes the conversion of HMG-CoA to mevalonic acid. This transformation is one of the earliest steps in the cholesterol (cholesterol) synthesis chain in the body. Atorvastatin suppression of cholesterol synthesis leads to increased reactivity of LDL receptors in the liver, as well as in extrahepatic tissues. These receptors bind LDL particles and remove them from the blood plasma, which leads to a decrease in the concentration of LDL-C in the blood.

The antiatherosclerotic effect of atorvastatin is a consequence of its effect on the walls of blood vessels and blood components. Atorvastatin inhibits the synthesis of isoprenoids, which are growth factors for cells of the inner lining of blood vessels. Under the influence of atorvastatin, endothelium-dependent expansion of blood vessels improves, the concentration of LDL cholesterol, apolipoprotein B, triglycerides (TG) decreases, the concentration of HDL cholesterol and apolipoprotein A.

increases. Atorvastatin reduces blood plasma viscosity and blood clotting activity. Due to this, it improves hemodynamics and normalizes the state of the coagulation system. HMG-CoA reductase inhibitors also affect the metabolism of macrophages, block their activation and prevent rupture of atherosclerotic plaques.

Generally the therapeutic effect of atorvastatin develops after 2 weeks of using Atoris®, and the maximum effect is achieved after 4 weeks.

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

Indications

Hyperlipidemia: Decreased concentrations of total cholesterol, cholesterol-LDL, apolipoprotein B and triglycerides in the blood serum of patients with primary hyperlipidemia (Fredrickson types IIa and IIb), including polygenic hypercholesterolemia, familial heterozygous hypercholesterolemia and mixed hyperlipidemia.

Decreased elevated concentrations of total cholesterol, cholesterol-LDL and apolipoprotein B in patients with homozygous familial hypercholesterolemia.

The drug AtorisВ® increases the concentration of HDL-C in the blood serum and reduces the ratio of LDL-C / HDL-C.

Used in case of insufficient effectiveness of diets familial heterozygous hypercholesterolemia and mixed hyperlipidemia.

Decreased elevated concentrations of total cholesterol, cholesterol-LDL and apolipoprotein B in patients with homozygous familial hypercholesterolemia.

The drug AtorisВ® increases the concentration of HDL-C in the blood serum and reduces the ratio of LDL-C / HDL-C.

Used in case of insufficient effectiveness of diets familial heterozygous hypercholesterolemia and mixed hyperlipidemia.

Decreased elevated concentrations of total cholesterol, cholesterol-LDL and apolipoprotein B in patients with homozygous familial hypercholesterolemia.

The drug AtorisВ® increases the concentration of HDL-C in the blood serum and reduces the ratio of LDL-C / HDL-C.

Used in case of insufficient effectiveness of dietsTherapy and other non-pharmacological treatments.

Prevention of cardiovascular diseases: Primary prevention of cardiovascular complications in patients without clinical signs of coronary heart disease, but with several risk factors for its development: age older than 55 years, nicotine addiction, arterial hypertension, diabetes mellitus, low levels of HDL-C blood plasma, genetic predisposition, incl. against the background of dyslipidemia.

Secondary prevention of cardiovascular complications in patients with coronary heart disease in order to reduce the total mortality rate, myocardial infarction, stroke, re-hospitalization for angina pectoris and the need for revascularization.

Use during pregnancy and lactation

The drug AtorisВ® is contraindicated during pregnancy and during breastfeeding. Animal studies indicate that the risk to the fetus may exceed any possible benefit to the mother.

In women of reproductive age who do not use reliable methods of contraception, the use of AtorisВ® is not recommended. When planning a pregnancy, you must stop using AtorisВ® at least 1 month before your planned pregnancy.

There is no evidence of the release of atorvastatin with breast milk. However, in some animal species, the concentration of atorvastatin in blood and breast milk is similar. If necessary, use the drug AtorisВ® during lactation, in order to avoid the risk of adverse events in infants, breastfeeding should be discontinued.

Composition

1 tablet contains:

Active ingredient: atorvastatin calcium 10.36 mg, (equivalent to 10 mg atorvastatin, respectively).

Excipients: povidone - 5.8 mg sodium lauryl sulfate - 2.9 mg calcium carbonate - 31.84 mg MCC - 29 mg lactose monohydrate - 57, 125 mg croscarmellose sodium - 7.25 mg magnesium stearate - 0.725 mg.

Film sheath: Opadry II HP 85F28751 white (polyvinyl alcohol, titanium dioxide (E171),macrogol 3000, talc) - 4.35 mg.

Dosage and administration of

Ketilept is taken orally, regardless of food intake, 2 times a day.

Adults. The total daily dose in the first 4 days of therapy is 50 mg (in the 1st In such a situation, clinical and laboratory parameters should be carefully monitored (regular monitoring of ACT and ALT activity). With a significant increase in hepatic transaminases, the dose of Atoris® should be reduced or treatment should be discontinued.

Use in combination with other drugs.

If it is necessary to use simultaneously with cyclosporine, the daily dose of Atoris® should not exceed 10 mg.

Side effects of

From the side of the central nervous system and peripheral nervous system: headache, dizziness, asthenic syndrome, insomnia or drowsiness, nightmares, amnesia, paresthesia, peripheral neuropathy, emotional lability, ataxia, hyperkinesia, depression, depression.

On the part of the sensory organs: amblyopia, tinnitus, dry conjunctiva, disturbance of accommodation, eye hemorrhage, deafness, glaucoma, parosmia, loss of taste sensations.

From the CCC side: palpitations, vasodilation, migraine, postural hypotension, increased blood pressure, phlebitis, arrhythmia, chest pain, vasculitis.

From the hematopoietic system: anemia, lymphadenopathy, thrombocytopenia.

From the respiratory system: bronchitis, rhinitis, dyspnea, bronchial asthma, nosebleeds.

From the digestive system: nausea, heartburn, constipation or diarrhea, flatulence, gastralgia, abdominal pain, anorexia or increased appetite, dry mouth, belching, dysphagia, vomiting, stomatitis, esophagitis, glossitis, gastroenteritis, hepatitis, hepatitis, liver , duodenal ulcer, pancreatitis, cholestatic jaundice, increased activity of liver enzymes, rectal bleeding, melena, bleeding gums, tenesmus.

From the musculoskeletal system: myalgia, arthralgia, back pain, swelling of the joints, myopathy, muscle cramps, myositis, rhabdomyolysis, tendopathy (in some cases, with tendon rupture).

From the genitourinary system: urogenital infections, dysuria (i.e. including pollakiuria, nocturia, urinary incontinence or urinary retention, imperative urination), cystitis, hematuria, vaginal bleeding, uterine bleeding, urolithiasis, metrorrhagia, epididymitis, decreased libido, impotence, impaired ejaculation.

From the skin: sweating, eczema, seborrhea, ecchymosis.

Allergic reactions: itching, skin rash, contact dermatitis, rarely urticaria, angioedema, anaphylaxis, exudative erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome).

Laboratory indicators: increased serum CPK activity, increased ALT activity, ACT, hyperglycemia, hypoglycemia.

Other: peripheral edema, weight gain, fatigue, fever.

Drug Interaction

Concurrent use of atorvastatin with cyclosporin, antibiotics (erythromycin, clarithromycin, quinupristine / dalfopristin), HIV protease inhibitors (indinavir, ritonavir), antifibulol, antifungal ketoconazole) or with nefazodone can lead to an increase in the concentration of atorvastatin in the serum, which increases the risk of myopathy with rhabdomyolysis and renal failure. Thus, with concomitant use with erythromycin Tmax, atorvastatin increases by 40%. All of these drugs inhibit the CYP3A4 isoenzyme, which is involved in the metabolism of atorvastatin in the liver.

A similar interaction is possible when atorvastatin is co-administered with fibrates and nicotinic acid in lipid-lowering doses (greater than 1 g / day).

Co-administration of atorvastatin at 40 mg with diltiazem at 240 mg leads to an increase in the concentration of atorvastatin in the blood plasma. Co-administration of atorvastatin with phenytoin and rifampicin, which are inducers of the CYP3A4 isoenzyme, may reduce the effectiveness of atorvastatin. Because atorvastatin is metabolized by the CYP3A4 isoenzyme, concomitant use of atorvastatin with CYP3A4 isoenzyme inhibitors may lead to an increase in the concentration of atorvastatin in the blood plasma.

OATP1B1 transport protein inhibitors (eg cyclosporine) may increase atorvastatin bioavailability. When used with antacids (suspension of magnesium hydroxides and aluminum), the concentration of atorvastatin in the blood plasma is reduced.

Atorvastatin concomitantly with colestipol, plasma concentrations of atorvastatin are reduced by 25%, but the therapeutic effect of the combination is higher than that of one atorvastatin.

Concurrent 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).

In patients receiving 80 mg atorvastatin and digoxin concurrently, the plasma digoxin content is increased by approximately 20%, so such patients should be monitored.

Co-administration of atorvastatin with oral contraceptives (norethindrone and ethinylestradiol) may increase the absorption of contraceptives and increase their concentration in blood plasma. The choice of contraceptives in women receiving atorvastatin should be monitored.

Concurrent administration of atorvastatin with warfarin may increase the effect of warfarin on blood coagulation rates (decrease in PV) in the first days. This effect disappears after 15 days of co-administration of these drugs.

No concurrent changes in the pharmacokinetics of terfenadine were observed with atorvastatin and terfenadine.

Atorvastatin does not affect the pharmacokinetics of phenazone.

Co-administration with protease inhibitors leads to an increase in the concentration of atorvastatin in blood plasma.

Atorvastatin 80 mg and 10 mg amlodipine did not change the atorvastatin pharmacokinetics at steady state.

Cases of rhabdomyolysis have been reported in patients using atorvastatin and fusidic acid.

Concomitant therapy.

When using atorvastatin with antihypertensive agents and estrogens, no evidence of clinically significant undesirable interaction was observed within the replacement therapy.

The use of grapefruit juice during the use of Atoris® can lead to increased plasma concentrations of the drug. In this regard, patients taking Atoris® should avoid using grapefruit juice of more than 1.2 liters per day.

overdose

Symptoms: in the development of myopathy followed by rhabdomyolysis and acute renal failure (a rare but severe side effect), the drug should be discontinued immediately.

Treatment: the patient needs to enter a diuretic and sodium bicarbonate solution. Hemodialysis should be performed if necessary. Rhabdomyolysis can lead to hyperkalemia, which requires the administration of calcium chloride or gluconate calcium, the infusion of 5% dextrose (glucose) solution with insulin, and the use of potassium exchange resins. Because atorvastatin is highly bound to plasma proteins, hemodialysis is ineffective.

General activities: monitoring and maintenance of vital functions of the body and prevention of further absorption of the drug (gastric lavage, administration of activated charcoal or laxatives).

Storage conditions

At a temperature not exceeding 25 РC, in the original packaging.

Keep out of the reach of children.

Active ingredient

Atorvastatin

dosage form

tablets

Prescription

Prescription of

For adults appointment doctor

KRKA d.d. Novo mesto AO, Slovenia