Atorvastatin tab p / 10 mg of quinacrine 30 pc

Description

Composition
Active substance:
Atorvastatin calcium salt 10.84 / 21.68 mg, in an amount equivalent to 10/20 mg atorvastatin ;.
Excipients:
Calcium carbonate, 20/40 mg, 43/86 mg microcrystalline cellulose, lactose 17.5 / 35.0 mg Tween 80 0.5 / 1.0 mg hydroxypropylcellulose 1.0 / 2.0 mg croscarmellose 5.66 / 11.32 mg magnesium stearate 0.75 / 1.5 mg; sheath: hydroxypropyl methylcellulose (hypromellose) 1.5 / 3.0 mg titanium dioxide 0.35 / 0.7 mg, 0.15 polyethylene glycol / 0.3 mg.
Description:
White round tablets, biconvex, film-coated. At the turn of the tablets are white or almost white.
White round tablets, biconvex, film-coated. At the turn of the tablets are white or almost white.
Product form:
Coated tablets with 10 mg and 20 mg.
At 7, 10 or 14 tablets in blister Al / PVC.
1, 2, 3, 4, 9 in the blister cardboard pack together with instructions for use.
Contraindications
Hypersensitivity to any component of the drug, liver disease in active phase (including chronic active hepatitis, chronic alcoholic hepatitis), increased activity of “liver” transaminases (more than 3 times compared with the upper limit of normal) of unclear origin, hepatic failure (classes A and B according to the classification Child-Pugh) liver cirrhosis of any cause, pregnancy, lactation, infancy to 18 years (efficacy and safety have not been established), lactose intolerance, lactase deficiency s, glyukozogalaktoznaya malabsorption, use in women planning pregnancy and not using reliable methods of contraception.
Dosage
10 mg
Indications
Primary hypercholesterolemia, mixed hyperlipidemia, heterozygous and homozygous familial hypercholesterolemia (as a supplement to the diet).
Interaction with other drugs
When concomitant administration of cyclosporine, fibrates, erythromycin, clarithromycin, immunosuppressive, antifungal agents (belonging to azoles) and nicotinamide concentration of atorvastatin in plasma (and the risk of myopathy) increases.
Antacids reduce the concentration to 35% (effect on LDL cholesterol is not changed).
Simultaneous use of atorvastatin with inhibitors of proteases known as inhibitors of the cytochrome P450 CYP3A4, accompanied by an increase in plasma concentrations of atorvastatin.
In the application of digoxin in combination with atorvastatin 80 mg / day digoxin concentration increases by about 20%.
Increases concentration of 20% (the designation with atorvastatin 80 mg / day) oral contraceptives containing norethindrone and ethinyl estradiol.
The hypolipidemic effect of the combination with colestipol than that for either agent alone.
When concomitantly with warfarin in the first days decreased prothrombin time, but after 15 days the figure is normalized. Therefore, patients taking atorvastatin with warfarin should be more often than usual to monitor the prothrombin time.
The use of grapefruit juice during treatment with atorvastatin can lead to increased plasma concentrations of drug. Therefore, patients taking the drug should avoid drinking this juice.
Overdose
Treatment. Cpetsificheskogo no antidote. Symptomatic therapy. Take measures to maintain the vital functions of the body and measures to prevent further absorption of the drug: gastric lavage, activated charcoal. Hemodialysis is not effective.
If signs and the presence of risk factors for acute liver failure with rhabdomyolysis (a rare but serious side effect), the drug should be immediately repealed.
Since atorvastatin is largely bound to plasma proteins, hemodialysis is an inefficient way of removing the substance from the body.
pharmachologic effect
Pharmacological group:
Lipid-lowering drugs – HMG-CoA reductase.
Pharmacodynamics:
Hypolipidemic agent from the group of statins. The main mechanism of action is inhibition of atorvastatin 3-hydroxy-3-metilglutarilkoenzim A (HMG-CoA) reductase, the enzyme that catalyzes the conversion of HMG-CoA to mevalonic acid. This transformation is one of the earliest stages in the chain of cholesterol synthesis in the body. Inhibition of cholesterol synthesis atorvastatin LDL receptor leads to enhanced reactivity (low density lipoproteins) in the liver, as well as in extrahepatic tissues. These receptors bind LDL particles and remove them from the plasma, resulting in a reduction of LDL cholesterol in the blood. Anti-sclerotic effect atorvastatin is a consequence of effects of the drug on the vessel walls and blood components. The drug inhibits the synthesis of isoprenoids, non-vascular growth factors inner sheath cells. Under the effect of atorvastatin is improved endothelium-dependent vasodilation. Atorvastatin reduces cholesterol, low density lipoproteins, apolipoprotein B, triglycerides. Causes an increase in HDL cholesterol (HDL) and apolipoprotein A. The action of the drug, usually develops after 2 weeks of treatment, and the maximum effect is achieved after four weeks.
Pharmacokinetics:
Absorption – high. Time to maximum concentration – 2.1 h, the maximum concentration in women above 20%, AUC (area under curve) – below 10%, the maximum concentration in patients with alcoholic liver cirrhosis 16 times, AUC – 11 times higher than normal. Food somewhat reduces the rate and duration of absorption of the drug (25% and 9% respectively) but LDL cholesterol reduction similar to that in the application of atorvastatin without food. The concentration of atorvastatin in the application in the evening lower than in the morning (approximately 30%). A linear relationship between the degree of absorption and the dose of the drug.
Bioavailability – 14% systemic bioavailability of inhibitory activity against HMG-CoA reductase – 30%. The low systemic bioavailability due to first-pass metabolism in the mucosa of the gastrointestinal tract, and the “first pass” through the liver.
The average distribution volume – 381 liters, the connection with plasma proteins – 98%.
Metabolized mainly in the liver by the action of cytochrome P450 CYP3A4, CYP3A5 and CYP3A7 to produce pharmacologically active metabolites (ortho and paragidroksilirovannyh derivatives, beta-oxidation products). The inhibitory effect of the drug against HMG-CoA reductase inhibitor of approximately 70% determined by the activity of circulating metabolites.
Excreted in the bile after hepatic and / or extrahepatic metabolism (not subjected to severe enterohepatic recirculation).
The half-life time -. 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 dose of an oral preparation is defined in the urine.
Not output during hemodialysis.
Pregnancy and breast-feeding
The drug Atorvastatin is contraindicated in pregnancy.
Women of reproductive age during treatment should use adequate contraception methods. Atorvastatin drug can be administered to women of childbearing age only when the probability of pregnancy are very low and the patient informed of the potential risk to the fetus during treatment.
Controlled clinical trials of atorvastatin in pregnant women was conducted. rare reports have been received of congenital abnormalities of fetal development after exposure to inhibitors of HMG-CoA reductase. Studies in animals have shown the presence of the toxic effects of atorvastatin on the reproductive function. Treatment mothers drug Atorvastatin can reduce the formation of mevalonate in fetal liver cells, which is a precursor of cholesterol. Atherosclerosis is a chronic process and the discontinuation of lipid-lowering usually drugs during pregnancy should have little impact on the long-term risk associated with primary hypercholesterolemia. For these reasons, Atorvastatin drug should not be used for women who are planning a pregnancy and who did not rule out pregnancy. Treatment with atorvastatin should be suspended during pregnancy or until such time as it is determined that the woman is not pregnant.
The drug Atorvastatin is contraindicated during breast-feeding.
It is not known whether atorvastatin is excreted in breast milk. If necessary, the appointment during lactation, breast-feeding should be discontinued in order to avoid the risk of adverse events in infants.
Conditions of supply of pharmacies
On prescription.
side effects
Classification of the incidence of side effects of the World Health Organization (WHO): very common (> 1/10), common (> 1/100 to
special instructions
Carefully
A history of liver disease, severe disorders of electrolyte balance, endocrine and metabolic disorders, alcoholism, hypotension, severe acute infection (sepsis), uncontrolled seizures, extensive surgery, trauma.
Abnormal liver function
Use of inhibitors of HMG-CoA reductase to reduce the level of lipids in the blood can lead to changes in biochemical parameters that reflect liver function.
liver function should be monitored before treatment and after 6 weeks, 12 weeks after the start of atorvastatin and improve after each dose, and periodically, e.g., every 6 months. Changes in the activity of liver enzymes is usually observed during the first three months after the start of atorvastatin. Patients in whom there is an increase in transaminase levels should be controlled to the level of enzymes return to normal. In that case, if the values ​​of alanine aminotransferase (ALT) or asparaginaminotransferazy (AST) is more than 3 times higher than the level of the upper allowable limit, it is advisable to reduce the dose of atorvastatin or discontinue treatment.
skeletal muscles
Patients with diffuse myalgia, muscle weakness or flaccidity and / or a significant increase in CPK are a risk group for the development of myopathy (defined as pain in the muscle with a concomitant increase in CPK levels more than 10 times compared with the upper limit of normal).
When assigning the combined therapy of atorvastatin with cyclosporin derivatives of fibric acid, erythromycin, clarithromycin, immunosuppressive and antifungal agents azole structure and also causing reduction of lipid doses of niacin is necessary to compare the potential benefit and risk assessment for a given treatment and to monitor patients in where there are signs or symptoms of muscle pain, weakness, or weakness, particularly during the first months of treatment and at higher doses of any and of drugs.
Atorvastatin should be suspended or terminated at the serious condition of the development that is likely to be a consequence of myopathy, as well as the presence of risk factors for the development of acute renal failure due to rhabdomyolysis (eg, acute severe infection, hypotension, major surgery, trauma, severe metabolic and endocrine disorders, as well as electrolyte balance disorders).
In women of reproductive age who are not using reliable contraception, the use of atorvastatin is not recommended. If the patient is planning to become pregnant, she should stop taking atorvastatin for at least one month before the planned pregnancy.
The patient should seek medical advice immediately if the appearance of unexplained pain or weakness in muscles, especially if accompanied by malaise and fever.
Effects on ability to drive and operate machinery
On the adverse effects of atorvastatin on the ability to drive and operate machinery that require increased attention, it has been reported.
Storage conditions
In a dry, dark place at a temperature below 25 ° C.
Keep out of the reach of children.
Dosing and Administration
Prior to initiating treatment with atorvastatin patient should be transferred to a diet providing a reduction in lipid content in the blood, which must be observed during drug treatment.
Inside, take at any time of the day (but at the same time), regardless of the meal.
The recommended starting dose – 10 mg 1 time per day. Further dose picked individually depending on the content of cholesterol – LDL. Change the dose should be separated by at least 4 weeks. The maximum daily dose – 80 mg per 1 reception.
Primary (heterozygous and polygenic hereditary) hypercholesterolemia (type IIa) and mixed hyperlipidaemia (type IIb).
Treatment started with a recommended starting dose, which is increased after 4 weeks of treatment depending on the patient response. The maximum daily dose is 80 mg.
Homozygous Familial Hypercholesterolemia.
The dose range is the same as for other types of hyperlipidemia. The initial dose is selected individually depending on the disease severity. The majority of patients with homozygous familial hypercholesterolemia an optimal effect is observed when using the drug in a daily dose of 80 mg (once).
In patients with renal insufficiency and in elderly patients, dose adjustment of atorvastatin is required.
In patients with impaired hepatic function should be cautious due to the slowing of excretion of the drug. Clinical and laboratory values ​​should be carefully monitored and the detection of significant pathological changes the dose should be reduced or the treatment should be discontinued.
Information
Appearance may differ from that depicted in the picture. There are contraindications. You need to read the manual or consult with a specialist