Active substanceFenofibrateFenofibrate
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  • Dosage form: & nbspfilm-coated tablets
    Composition:

    1 tablet, film-coated, contains:

    active substance: fenofibrate 145 mg;

    Excipients: corn starch 137 mg, silicon dioxide colloid 10 mg, croscarmellose sodium 33 mg, mannitol 170 mg, magnesium stearate 6 mg, povidone K-30 44 mg, cellulose microcrystalline 105 mg;

    film sheath: Opadrai II white 20 mg, including: polyvinyl alcohol 9.38 mg, macrogol (polyethylene glycol 4000) 4.72 mg, talc 3.48 mg, titanium dioxide 2.42 mg.

    Description:Oval, biconvex tablets covered with a film coating of white or almost white color. On the cross-section - almost white.
    Pharmacotherapeutic group:lipid-lowering agent - fibrate
    ATX: & nbsp

    C.10.A.B.05   Fenofibrate

    Pharmacodynamics:

    Activating RAPP-alpha (alpha receptors activated by the peroxisome proliferator), fenofibrate enhances lipolysis and removal from the blood plasma of atherogenic lipoproteins with a high triglyceride content by activating the lipoprotein lipase and reducing the synthesis of apoproteins CIII. Activation of PPA-alpha also results in increased synthesis of apoproteins AI and AII.

    Fenofibrate is a derivative of fibroic acid, whose ability to change the lipid content in the human body, is mediated by the activation of RAPP-alpha. The effects of fenofibrate on lipoproteins described above lead to a reduction in the low-density and very low-density lipoprotein (LLDPE) fraction, including apoprotein B, and an increase in the high-density lipoprotein (HDL) fraction, including apoproteins AI and AII.

    In addition, due to correction of the synthesis and catabolism of VLDLP, fenofibrate increases the clearance of LDL and reduces the content of dense and small particle size of LDL, the increase of which is observed in patients with atherogenic lipid phenotype, a frequent violation in patients with risk of coronary heart disease. In clinical trials, it was noted that the use of fenofibrate reduces the concentration of total cholesterol by 20-25% and triglycerides by 40-55% when the concentration of HDL-cholesterol is increased by 10-30%. In patients with hypercholesterolemia,in which the LDL cholesterol concentration is reduced by 20-35%, the use of fenofibrate led to a decrease in the ratios "total cholesterol / HDL cholesterol", "LDL cholesterol / HDL cholesterol" and "A to B /A to AI", which are markers of atherogenic risk.

    Given the significant effect on the concentration of LDL cholesterol and triglycerides, the use of fenofibrate is effective in patients with hypercholesterolemia, either accompanied or not accompanied by hypertriglyceridemia, including secondary hyperlipoproteinemia, for example, type 2 diabetes mellitus. During treatment with fenofibrate, extravascular deposits of cholesterol (tendon and tuberous xanthomas) can be significantly reduced and even completely lost. In patients with elevated fibrinogen levels who received fenofibrate treatment, there was a significant decrease in this index, as well as in patients with elevated lipoprotein levels. Other markers of inflammation, such as C-reactive protein, also decrease with fenofibrate treatment.

    For patients with dyslipidemia and hyperuricemia, an additional advantage is the uricosuric effect of fenofibrate, which leads to a decrease in the uric acid concentration by approximately 25%.

    In a clinical trial and in animal experiments, it was shown that fenofibrate reduces aggregation of platelets caused by adenosine diphosphate, arachidonic acid and epinephrine.

    Pharmacokinetics:

    Fenofibrate Canon 145 mg, film-coated tablets, contain 145 mg of micronized fenofibrate.

    The preparation Fenofibrate Canon in the form of micronized fenofibrate has a higher bioavailability.

    Initial fenofibrate in the blood plasma is not detected. The main plasma metabolite is fenofibroic acid.

    Suction: the maximum concentration in the blood plasma (CmOh) is achieved 4-5 hours after ingestion. With prolonged use, the concentration of the drug in the blood plasma remains stable. Absorption of fenofibrate is enhanced by simultaneous intake with food.

    Distribution: fenofibroevaya acid strongly binds to albumin of blood plasma (more than 99%).

    Half-life: half-life of fenofibroic acid (T1/2 ) - about 20 hours.

    Metabolism and excretion: in the blood plasma only the main metabolite of fenofibrate is found - fenofibroic acid. Fenofibrate is not a substrate for isoenzyme CYP3A4. Does not participate in microsomal metabolism.

    It is mainly excreted by the kidneys in the form of fenofibric acid and glucuronide conjugate. Within 6 days fenofibrate is output almost completely. The total clearance of fenofibric acid, determined in elderly patients does not change.

    The drug is not cumulated after a single dose and with prolonged use. When hemodialysis is not withdrawn.

    Indications:

    The drug Fenofibrate Canon is indicated in combination with a diet:

    - combined therapy with HMG-CoA reductase inhibitors (statins) of mixed dyslipidemia (type IIa, IIb according to Fredrickson), in order to reduce triglycerides (TG) and increase the concentration of HDL in patients with IHD or at a high risk of developing coronary heart disease (other clinical forms of atherosclerotic disease: peripheral arterial atherosclerosis, abdominal aortic aneurysm and symptomatic carotid artery atherosclerosis, diabetes mellitus, multiple factors risk, which corresponds to a 10-year risk of developing coronary events> 20%);

    - to reduce the concentration of TG in patients with severe hyperglyceridemia (dyslipidemia IV, V type by Fredrickson);

    - with the aim of reducing the elevated concentrations of LDL, total cholesterol, triglycerides and ApoB (apolipoprotein B) and increasing HDL-C levels in patients with primary hyperlipidemia or mixed dyslipidemia (type IIa, IIb, III, IV by Fredrickson).

    Contraindications:

    The drug is strictly contraindicated in the following cases:

    - increased sensitivity to fenofibrate or other components of the drug,

    - hepatic insufficiency (including biliary cirrhosis and persistent liver dysfunction of unclear etiology),

    - severe renal failure (creatinine clearance <20 mL / min),

    - age under 18 years (effectiveness and safety not established),

    - the presence in the anamnesis of photosensitization or phototoxicity in the treatment of fibrates or ketoprofen,

    - a history of a gallbladder,

    - the period of breastfeeding,

    - chronic or acute pancreatitis, except for cases of acute pancreatitis due to severe hypertriglyceridemia.

    Carefully:

    - With hypothyroidism;

    - patients who abuse alcohol;

    - Patients with impaired renal function (QC more than 20 ml / min);

    - the elderly, with a history of hereditary muscle diseases;

    - with the simultaneous administration of oral anticoagulants, inhibitors of HMG-CoA reductase (see section "Interaction with other drugs").

    Pregnancy and lactation:

    Pregnancy

    There are few data on the use of fenofibrate in pregnant women. In animal experiments, the teratogenic effect of fenofibrate was not observed. Embryotoxicity was noted when prescribing doses toxic to the mother's organism during preclinical trials. The potential risk to humans is unknown. Therefore, during pregnancy, the preparation of Fenofibrate Canon can be used only after a thorough assessment of the relationship between risk and benefit.

    Breastfeeding period

    The drug Fenofibrate Canon is contraindicated for use during breastfeeding (not enough data on the use of the drug in this period).

    Dosing and Administration:

    Tablets should be swallowed whole, without chewing, while taking piniand.

    Adults. One tablet once a day. Patients taking one capsule of fenofibrate 200 mg,can switch to taking one tablet of the drug Fenofibrate Canon 145 mg without additional dose adjustment. The maximum daily dose of 145 mg.

    Elderly patients. It is recommended to take 1 tablet of 145 mg for adults (one tablet once a day).

    Patients with liver disease. The use of the drug in patients with liver disease has not been studied.

    The drug should be taken for a long time, while continuing to follow the diet, which the patient adhered to before the treatment with the drug Fenofibrate Canon.

    Side effects:

    Side effects for therapeutic doses are given with frequency distribution and system-organ classes according to WHO classification:

    Often

    > 1/10 appointments (> 10%)

    often

    from> 1/100 to <1/10 of appointments (> 1% and <10%)

    infrequently

    from> 1/1000 to <1/100 of prescriptions (> 0,1% and <1%)

    rarely

    from> 1/10000 to <1/1000 appointments (> 0,01% and <0,1%)

    rarely

    <1/10000 assignments (<0,01%)

    From the digestive system:

    often - pain in the abdomen, nausea, vomiting, diarrhea and flatulence of moderate severity;

    infrequently - cases of pancreatitis.

    From the side of the liver:

    often - moderate increase in the concentration of serum transaminases; infrequently - formation of gallstones;

    rarely - Hepatitis.When there are symptoms of hepatitis (jaundice, pruritus), you should conduct laboratory tests and, in case of confirmation of hepatitis, cancel fenofibrate. (see section "Special instructions").

    From the musculoskeletal system and connective tissue:

    rarely - diffuse myalgia, myositis, muscle spasm and weakness;

    rarely - rhabdomyolysis, increased activity of creatine phosphokinase (CKF).

    Vascular disorders:

    infrequently - venous thromboembolism (pulmonary embolism, deep vein thrombosis).

    From the side of the blood and lymphatic system:

    rarely - increased hemoglobin and leukocytes.

    From the nervous system:

    rarely - Sexual dysfunction, headache.

    On the part of the respiratory system:

    rarely - interstitial pneumopathy.

    From the rut and subcutaneous fat:

    infrequently - a rash, itchy skin, hives, or photosensitivity reactions;

    rarely - alopecia;

    rarely - photosensitization, accompanied by erythema, the formation of blisters or nodules in areas of skin exposed to sunlight or artificial UV lighting (for example, a quartz lamp) in individual cases (even after months of use without any complications).

    Laboratory research:

    infrequently - increasing the concentration of creatinine and urea in the blood serum.

    Overdose:

    Cases of overdose are not described. Specific antidote is unknown. If you suspect an overdose, you should prescribe a symptomatic and, if necessary, supportive treatment. Hemodialysis is ineffective.

    Interaction:

    Oral anticoagulants

    Fenofibrate enhances the effect of oral anticoagulants and may increase the risk of bleeding, which is due to the displacement of the anticoagulant from the binding sites to plasma proteins.

    At the beginning of treatment with fenofibrate, it is recommended that the dose of anticoagulants be reduced by about a third, followed by a gradual selection of a dose. The choice of a dose is recommended to be carried out under the control of the INR level (the international normalized relationship).

    Cyclosporin

    Several severe cases of reversible reduction of renal function during simultaneous treatment with fenofibrate and cyclosporine have been described. Therefore, it is necessary to monitor the state of renal function in such patients and to cancel fenofibrate in the case of a serious change in laboratory indicators.

    Inhibitors of HMG-CoA reductase (statins) and other fibrates

    When taking fenofibrate concomitantly with HMG-CoA reductase inhibitors or other fibrates, the risk of serious toxic effects on muscle fibers increases (see section "Special instructions").

    Isozymes of the cytochrome P450 system

    Studies of microsomes from human liver in vitro showed that fenofibrate and fenofibroic acid are not inhibitors of the following cytochrome P450 isoenzymes (CYP3A4, CYP2D6, CYP2E1 or CYP1A2). In therapeutic concentrations, these compounds are weak inhibitors of isoenzymes CYP2C19 and CYP2A6 and mild or moderate inhibitors CYP2C9.

    Special instructions:

    Before treatment drug fenofibrate Canon should conduct an appropriate treatment to eliminate the cause of secondary hypercholesterolaemia, e.g., in diseases such as uncontrolled type 2 diabetes mellitus, hypothyroidism, nephrotic syndrome, Dysproteinemia, obstructive liver disease, the effects of drug therapy, alcoholism.

    The effectiveness of therapy should be assessed by the content of lipids (total cholesterol, LDL, triglycerides) in serum. In the absence of a therapeutic effect after several months of therapy (as a rule,after 3 months) should consider the feasibility of concomitant or alternative therapy.

    In patients with hyperlipidemia, taking estrogens or hormonal contraceptives containing estrogens, it is necessary to find out whether hyperlipidemia has a primary or secondary nature. In such cases, the increase in lipid levels can be caused by the use of estrogens.

    Liver function: when taking fenofibrate and other drugs that reduce lipid concentrations, some patients described an increase in the activity of "liver" transaminases. In most cases, this increase was temporary, minor and asymptomatic. During the first 12 months of treatment, it is recommended to monitor the activity of transaminases (alanine aminotransferase (ALT), aspartate aminotransferase (ACT)) every 3 months. Patients who have increased concentrations of transaminases against the background of treatment, require attention, and in the case of increased concentrations of ALT and ACT more than 3 times compared with the upper limit of normal reception of the drug is stopped.

    Pancreatitis: cases of development of pancreatitis during the treatment with fenofibrate have been described.Possible causes of pancreatitis in these cases were: insufficient effectiveness of the drug in patients with severe hypertriglyceridemia, direct exposure to the drug, as well as secondary phenomena associated with the presence of stones or the formation of sediment in the gallbladder, accompanied by obstruction of the common bile duct.

    Muscles: when taking fenofibrate and other drugs that reduce lipid concentrations, there are cases of toxic effects on muscle tissue, including very rare cases of rhabdomyolysis. The frequency of such a disorder is increased in the case of hypoalbuminemia and renal insufficiency in the anamnesis. The possibility of this complication increases in cases of hypoalbuminemia and renal failure.

    Toxic effects on muscle tissue can be suspected on the basis of patient complaints of weakness, diffuse myalgia, myositis, muscle spasms and convulsions and / or a pronounced increase in creatinine phosphokinase (CK) activity (more than 5 times the upper limit of normal). In these cases, treatment with fenofibrate should be discontinued.

    The risk of rhabdomyolysis may increase in patients with a predisposition to myopathy and / or rhabdomyolysis, including age over 70 years, a history of hereditary muscle diseases, renal dysfunction, hypothyroidism, alcohol abuse. Such patients should be prescribed a drug only if the expected benefit exceeds the possible risk of rhabdomyolysis. When taking Fenofibrate Canon simultaneously with inhibitors of HMG-CoA reductase or other fibrates, the risk of serious toxic effects on muscle fibers increases, especially if the patient suffered from muscle disease before starting treatment. In this regard, the joint administration of the drug Fenofibrate Canon and statin is allowed only if the patient has severe mixed dyslipidemia and high cardiovascular risk, in the absence of a history of muscle disease and under close monitoring aimed at revealing signs of the development of toxic effects on muscle tissue.

    Renal function: When using Fenofibrate Canon as a monotherapy or in combination with statins, a reversible increase in serum creatinine concentration was noted in patients.The increase in creatinine concentration was generally stable for a time without signs of a further increase in serum creatinine concentration with prolonged therapy, with a tendency to return to baseline values ​​after treatment withdrawal. The clinical significance of these observations is not established. In patients with renal insufficiency, it is recommended that kidney function be monitored when taking Fenofibrate Canon. Control of renal function should be performed in patients at risk of developing renal failure, namely, elderly patients and patients with diabetes mellitus. Treatment should be reversed if the concentration of creatinine> 50% of the upper limit of the norm is increased. It is recommended to determine the concentration of creatinine during the first 3 months after the start of treatment, and also periodically after its termination.

    Effect on the ability to drive transp. cf. and fur:

    When applying the drug, there was no effect on the ability to drive and other mechanisms.

    Form release / dosage:

    Tablets, film-coated, 145 mg.

    Packaging:

    By 7, 10, 14 or 15 tablets in a contour cell pack of film polyvinyl chloride or PVC / PVDC film or PVC / PVTFE film and aluminum printed lacquer foil.

    By 4, 12, 14 contour cell packs of 7 tablets or by 1,2, 3, 5, 6, 9, 10 contour cell packs of 10 tablets or 2, 6, 7 contour packs of 14 tablets or 2, 4, 6 contour cell packs of 15 tablets together with instructions for use are placed in a pack of cardboard.

    Storage conditions:

    In a dry, protected from light place at a temperature of no higher than 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    2 years.

    Do not use after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:LP-002740
    Date of registration:02.12.2014
    The owner of the registration certificate:CANONFARMA PRODUCTION, CJSC CANONFARMA PRODUCTION, CJSC Russia
    Manufacturer: & nbsp
    Representation: & nbspCANONFARMA PRODUCTION CJSC CANONFARMA PRODUCTION CJSC Russia
    Information update date: & nbsp20.09.2015
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