Atorvastatin tab p / 10 mg of the film 30 pcs Izvarino Pharma

Description

Composition
Active substance:
1 tablet contains: atorvastatin 10 mg or 20 mg.
Excipients:
Microcrystalline Cellulose – 52.52 mg pregelatinized corn starch – 52.51 mg Colloidal silicon dioxide – 0.38 mg Magnesium carbonate – 33 mg magnesium stearate – 0.75 mg. shell composition Tablets: Opadry II white (85F18422) – 4.5 mg (polyvinyl alcohol – 40% titanium dioxide – 25%, macrogol-3350 – 20.2% talc – 14.8%).
Description:
Tablets, film-coated white or almost white, round, biconvex; in cross-section – the core of a white or nearly white.
Product form:
Tablets, film-coated 10 mg or 20 mg. 10 pieces. – packings Valium planimetric (2) – packs cardboard. 10 pieces. – packings Valium planimetric (3) – packs cardboard.
Contraindications
Liver disease in the active stage, elevated serum transaminase more than 3 times of unclear origin, pregnancy, lactation (breast-feeding), women of childbearing age not applying a reliable means of contraception; Hypersensitivity to atorvastatin. liver disease in the active stage.
With careful use of atorvastatin in patients with chronic alcoholism.
Dosage
10 mg
Indications
Primary hypercholesterolemia with poor diet, combined hypercholesterolemia and hypertriglyceridemia, heterozygous and homozygous familial hypercholesterolemia when poor diet.
Interaction with other drugs
When applied simultaneously with digoxin atorvastatin significantly increases the concentration of digoxin in plasma.
Diltiazem, verapamil, isradipine inhibit isoenzyme of CYP3A4, which is involved in the metabolism of atorvastatin, therefore, while the application of these calcium channel blockers may increase the concentration of atorvastatin in plasma and increased risk of myopathy.
With simultaneous application of itraconazole dramatically increased atorvastatin plasma concentration, apparently due to inhibition of itraconazole its metabolism in the liver, which occurs with the participation isozyme CYP3A4; increased risk of myopathy.
With simultaneous application of colestipol may decrease atorvastatin plasma concentration, wherein the hypolipidemic effect is enhanced.
With simultaneous use of antacids containing magnesium hydroxide and aluminum hydroxide, the concentration of atorvastatin reduced by approximately 35%.
With simultaneous application of cyclosporine, fibrates (including gemfibrozil), antifungal azole derivatives, nicotinic acid increases the risk of myopathy.
With simultaneous use of erythromycin, clarithromycin moderately increases the concentration of atorvastatin in plasma, increases the risk of myopathy.
With simultaneous use of ethinyl estradiol, norethisterone (norethindrone) significantly increases the concentration of ethinyl estradiol and norethisterone (norethindrone) in the blood plasma.
With simultaneous use of protease inhibitors increased the concentration of atorvastatin in plasma, because protease inhibitors are inhibitors of CYP3A4 isoenzyme.
pharmachologic effect
Pharmacological group:
Lipid-lowering drugs – HMG-CoA reductase inhibitor.
Pharmacodynamics:
Hypolipidemic agent from the group of statins. According to the principle of competitive antagonism statin molecule binds to a receptor that part of coenzyme A, which is attached HMG-CoA reductase. Another part of the statin molecule inhibits the conversion process gidroksimetilglutarata to mevalonate, an intermediate product in the synthesis of cholesterol molecules. Inhibition of HMG-CoA reductase leads to a series of successive reactions, resulting in reduced intracellular cholesterol and occurs compensatory increase in the activity of LDL receptors and consequently accelerate the catabolism of cholesterol (Xc) LDL.
Lipid-lowering effect of statins is associated with a reduction in total cholesterol at the expense of LDL-C. Reducing LDL is dose-dependent and is not linear, but exponential. The inhibitory effect of atorvastatin in relation to the HMG-CoA reductase inhibitor of approximately 70% is determined by its activity of circulating metabolites.
Statins not affect the activity of hepatic lipase and lipoprotein do not significantly affect the synthesis and catabolism of free fatty acids, so their effects on triglyceride levels and secondarily mediated through their major effects on the reduction of LDL-C levels. Moderate lowering TG in the treatment of statins, apparently associated with the expression remnantnyh (apo E) receptor on the surface of hepatocytes involved in the catabolism LPPP, in which the composition of about 30% TG. Compared with other statins (except rosuvastatin), atorvastatin causes a more marked reduction in triglycerides.
Besides hypolipidemic action, statins have positive effects at the endothelium dysfunction (preclinical signs of early atherosclerosis), on the vascular wall, the state of atheroma, improve blood rheology, and possess antioxidant, antiproliferative properties.
Atorvastatin lowers cholesterol in patients with homozygous familial hypercholesterolemia, which usually can not be lipid-lowering therapy means.
Pharmacokinetics:
Atorvastatin is rapidly absorbed from the gastrointestinal tract. Absolute bioavailability is low – about 12% due to presystemic clearance in gastrointestinal mucosa and / or as a result of “first pass” through the liver, predominantly in the site of action.
Atorvastatin is metabolized by the CYP3A4 isoenzyme to form a number of substances that are inhibitors of HMG-CoA reductase.
T1 / 2 of the plasma is about 14 hours, although the T1 / 2 inhibitor of HMG-CoA reductase is about 20-30 hours, due to the participation of active metabolites.
Plasma protein binding is 98%.
Atorvastatin is output in the form of metabolites predominantly in the bile.
Pregnancy and breast-feeding
Atorvastatin is contraindicated during pregnancy and lactation (breastfeeding).
It is not known whether atorvastatin is excreted in breast milk. Given the potential for adverse effects in infants, if necessary, use during lactation should decide the issue of termination of breastfeeding.
Women of reproductive age during treatment should use adequate contraception methods. Atorvastatin can be used in women of childbearing age only when the probability of pregnancy is very low, and the patient informed of the potential risk of treatment to the fetus.
Conditions of supply of pharmacies
Prescription.
side effects
From the nervous system:> 1% – insomnia, dizziness;
From the senses:
Cardio-vascular system:> 1% – pain in the chest;
From hemopoiesis system:
The respiratory system:> 1% – bronchitis, rhinitis;
From the digestive system:> 1% – nausea;
From the musculoskeletal system:> 1% – arthritis;
With the genitourinary system:> 1% – urogenital infections, peripheral edema;
Dermatologic reactions:> 1% – alopecia, dermatoxerasia, photosensitivity, sweating, eczema, seborrhea, ecchymosis, petechiae.
From endocrine system:
From a metabolism:
Allergic reactions:
Laboratory findings:
special instructions
Before and during treatment with atorvastatin, especially with the appearance of symptoms of liver disease, it is necessary to monitor liver function. At higher levels of transaminase activity should be monitored until the normalization. If the activity of AST or ALT, more than 3 times the norm persists recommended dose reduction or elimination of atorvastatin.
At occurrence of myopathy during treatment with symptoms should determine the activity of CK. If a significant increase in CPK persists, it is recommended to reduce the dose or stop atorvastatin.
The risk of myopathy during treatment with atorvastatin increases with simultaneous application of cyclosporine, fibrates, erythromycin, antifungal agents belonging to the azole and niacin.
There is the likelihood of developing these side effects, but not in all cases, a clear link with atorvastatin: muscle cramps, myositis, myopathy, paresthesia, peripheral neuropathy, pancreatitis, hepatitis, cholestatic jaundice, anorexia, vomiting, alopecia, pruritus, rash, impotence, hyperglycemia and hypoglycemia.
Children experience with atorvastatin at a dose of 80 mg / day is limited.
Storage conditions
In the dark place at a temperature not higher than 25 C.
Dosing and Administration
Treatment is carried out against the background of the standard diet for patients with hypercholesterolemia. Dose set individually depending on the starting cholesterol. Taken orally. The initial dose is typically 10 mg of 1 time / day. The effect is evident within 2 weeks, and the maximum effect – during 4 weeks. If necessary, the dose can be gradually increased at intervals of 4 weeks or more. The maximum daily dose – 80 mg.
Information
Appearance may differ from that depicted in the picture. There are contraindications. You need to read the manual or consult with a specialist