Lipantil® 200 M (Lipanthyl® 200 M)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceFenofibrateFenofibrate
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  • Lipantil® 200 M
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    Laboratories SA Fournier.     France
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    • Dosage form: & nbspcapsules
    Composition:

    1 capsule contains:

    Active substance:

    Fenofibrate (micronized) - 200 mg

    Excipients:

    Sodium lauryl sulfate 7 mg

    Lactose Monohydrate - 101 mg

    Pregelatinized starch - 30 mg

    Crospovidone 7 mg

    Magnesium stearate-5 mg

    Capsule shell:

    Titanium dioxide (E171) - 1 mg

    The iron oxide dye (E 172) - 0.83 mg

    Gelatine up to 75 mg
    Description:

    Hard gelatin capsules №1 of light brown color. The contents of capsules are white or almost white powder.

    Pharmacotherapeutic group:lipid-lowering agent - fibrate
    ATX: & nbsp

    C.10.A.B.05   Fenofibrate

    Pharmacodynamics:

    Fenofibrate - the active substance of the preparation, which is in the capsule, has a micronized form.

    Activating the receptors of PPAR-alpha (alpha receptors activated by the peroxisome proliferator), fenofibrate enhances lipolysis and removal from the blood plasma of atherogenic lipoproteins with a high concentration of triglycerides by activating lipoprotein lipase and reducing the synthesis of apoprotein 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 concentration of lipids in the human body, is mediated by the activation of PAPP-alpha. The effects of fenofibrate on lipoproteins described above lead to a decrease in the concentration of the fraction of low-density lipoproteins (LDL) and very low density (LLDPE), including apoprotein B and an increase in the concentration of high-density lipoprotein (HDL) fraction, which include apoproteins AI and AII.

    In addition, due to correction of violations of synthesis and catabolism of VLDLP fenofibrate increases the clearance of LDL and reduces the concentration of dense and small particle size LDL, an increase in 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% with an increase in the concentration of HDL-cholesterol by 10-30%. In patients with hypercholesterolemia,in which the concentration of LDL cholesterol is reduced by 20-35%, the use of fenofibrate led to a decrease in the ratio of "total cholesterol / HDL cholesterol", "LDL cholesterol / HDL cholesterol" and "Apo B / Apo AI", which are markers of atherogenic risk.

    Considering the influence of fenofibrate on the concentration of LMNP-cholesterol and triglycerides. the drug is effective in patients with hypercholesterolemia, either accompanied or not accompanied by hypertriglyceridemia, including secondary hyperlipoproteinemia, for example, in 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 concentrations treated with fenofibrate, there was a significant decrease in this index, as well as in patients with increased concentrations of lipoproteins. 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, leading to a decrease in the concentration of uric acid in the blood plasma 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:

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

    Suction: maximum concentration and blood plasma (CmOh) is achieved 4-5 hours after ingestion. With prolonged use, the concentration of the drug in the blood plasma remains stable regardless of the individual characteristics of the patient. Absorption of fenofibrate is enhanced by simultaneous admission with a beggar.

    Distribution: fenofibroevaya acid firmly binds to plasma albumin (more than 99%).

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

    Metabolism and excretion: after oral administration fenofibrate quickly hydrolyzed by esterases. In the blood plasma, only the main active metabolite of fenofibrate, fenofibroic acid, is found. Fenofibrate is not a substrate for isoenzyme CYP3A4 and does not participate in microsomal metabolism.

    It is excreted mainly 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 does not cumulate after a single dose and with prolonged use. When hemodialysis is not withdrawn.

    Indications:

    Hypercholesterolemia and hypertriglyceridemia isolated or mixed (dyslipidemia type IIa, IIb, III, Fredriksen IV) in patients for whom a diet or other non-medicamentous treatment measures (for example, weight loss or increased physical activity) have proved ineffective, especially in the presence of dyslipidemic-related risk factors such as hypertension and smoking.

    For the treatment of secondary hyperlipoprotemia, the drug is used in those cases, the boiler of hyperlipoproteinemia persists, despite the effective treatment of the underlying disease (eg, dyslipidemia in diabetes mellitus).

    Contraindications:

    - Hypersensitivity to fenofibrate or other components of the drug;

    - hepatic insufficiency (including biliary cirrhosis and non-rehearsing impairment of liver function of unclear etiology);

    - severe renal failure (creatinine clearance less than 30 ml / min);

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

    - the presence in the anamnesis of photosensitization or photo toxicity in the treatment of fibrates or ketoprofen;

    - history of gallbladder disease:

    - the period of breastfeeding;

    - lactose intolerance, lactase deficiency, impaired absorption of glucose and galactose (the preparation contains lactose);

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

    Patients with impaired renal function should be prescribed a lower dose of the drug. However, given the absence of fenofibrate in the Russian market at a lower dosage, the use of the drug Lipantil® 200 M is contraindicated in patients with impaired renal function of any severity.

    Carefully:

    In patients with factors predisposing to the development of myopathy and / or rhabdomyolysis, including elderly age (over 70 years), a history of hereditary muscle diseases, kidney failure, hypothyroidism and alcohol abuse (see below).section "Special instructions"); use during pregnancy; with the simultaneous administration of oral anticoagulants, inhibitors of HMG-CoA reductase (see section "Interaction with other drugs").

    Pregnancy and lactation:

    Pregnancy

    There is insufficient 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, use the drug Lipantil® 200 M during pregnancy can only be after a thorough assessment of the ratio of expected benefits to possible risks.

    Breastfeeding period

    There is insufficient information on the excretion of fenofibrate and / or its metabolites into breast milk. It is impossible to exclude the risk for infants. The drug is contraindicated for use during breastfeeding.

    Dosing and Administration:

    The drug should be taken, continuing to observe the hypocholesterolemic diet, which the patient adhered to before the treatment Lipantil® 200 M.

    Lipantil® capsules 200 M should be swallowed whole, with water.

    Adults. Lipantil® 200 M should be taken 1 capsule per day during the intake of food.

    Elderly patients without renal failure. It is recommended to take a standard dose for adults (1 capsule per day).

    The effectiveness of therapy should be assessed but the concentration of lipids (total cholesterol, LDL, triglycerides) in the serum. In the absence of therapeutic effect after several months of therapy (usually after 3 months), consideration should be given to the appropriateness of concomitant or alternative therapy.

    Side effects:

    During the placebo-controlled clinical trials, the following undesirable effects were observed, classified as follows: very often (≥1/10), often (≥1 / 100, <1/10) infrequently (≥1 / 1000, <1/100), rarely (≥1 / 10000, <1/1000) and very rarely (<1/10000), the frequency is not set:

    From the digestive system:

    Often: signs and symptoms of a disorder of the gastrointestinal tract (abdominal pain, nausea, vomiting, diarrhea, flatulence).

    Infrequently: pancreatitis. *

    From the liver and bile ducts:

    Often: increased activity of serum transaminases.

    Infrequently: cholelithiasis.

    Rarely: hepatitis.

    From the musculoskeletal system and connective tissue:

    Infrequent: muscle damage (eg, diffuse myalgia, myositis, muscle spasm and muscle weakness).

    Vascular disorders:

    Infrequent: thromboembolism (pulmonary embolism and deep vein thrombosis of lower extremities). *

    From the blood and lymphatic system:

    Rarely: a decrease in hemoglobin and leukocytes.

    From the nervous system:

    Infrequently: a headache.

    Rarely: increased fatigue, dizziness.

    On the part of the genitals:

    Infrequent: erectile dysfunction.

    From the skin and subcutaneous fat:

    Infrequent: skin reactions of hypersensitivity (for example, skin rash, dermal itching, urticaria).

    Rarely: alopecia, photosensitivity reactions.

    From the immune system:

    Rarely: hypersensitivity reactions.

    Laboratory indicators:

    Infrequent: increased serum creatinine concentration.

    Rarely: an increase in the concentration of urea nitrogen in the blood serum.

    * In a clinical study in patients with type 2 diabetes mellitus who received fenofibrate, a statistically significant increase in the incidence of pancreatitis and pulmonary embolism was observed compared with placebo.In the same study, a statistically unreliable increase in cases of deep vein thrombosis was revealed.

    In the period of post-marketing application there were spontaneous reports of a number of side effects. According to the available data, it is impossible to establish the exact frequency of these effects, therefore it is classified as "frequency not established".

    On the part of the respiratory system: interstitial lung disease.

    From the musculoskeletal system and connective tissue: rhabdomyolysis.

    From the liver and bile ducts: jaundice, complications of cholelithiasis (for example, cholecystitis, cholangitis, biliary colic).

    From the skin and subcutaneous fat: severe skin reactions (eg, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis).

    Overdose:

    There are only single reports of overdose. In most cases, no symptoms of overdose have been reported. The specific antidote is unknown. If you suspect an overdose, you should prescribe a symptomatic and, if necessary, supportive treatment. When hemodialysis is not withdrawn.

    Interaction:

    Oral anticoagulants

    Fenofibrate enhances the effect of oral anticoagulants and may increase the risk of bleeding, which is due to competition in binding 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 INR (the international normalized relationship).

    Cyclosporin

    Several severe cases of reversible renal function impairment during simultaneous treatment with fenofibrate and cyclosporine have been described. Therefore, careful monitoring of kidney function in these patients is necessary and, in the case of a serious change in laboratory parameters, the drug must be canceled.

    Inhibitors of GMC-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. Such combination therapy should be conducted with caution and carefully monitor the condition of patients for signs of toxic effects on muscle tissue (see section "Special instructions").

    The thiazolidinedione derivatives (glitazones)

    With the simultaneous use of fenofibrate and glitazones, several cases of reversible paradoxical decrease in the concentration of HDL cholesterol have been reported. Therefore, when combined therapy is recommended to control the concentration of HDL cholesterol, and if there is a significant decrease in the concentration of HDL cholesterol, drugs should be discarded.

    Isozymes of cytochrome P450

    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 isoenzyme inhibitors CYP2C9.

    Patients using fenofibrate together with drugs metabolized by isoenzymes CYP2C19, CYP2A6 and especially CYP2C9 with a narrow therapeutic index should be carefully monitored and, if necessary, it is recommended to adjust the doses of these drugs.

    Special instructions:

    Before starting treatment with the drug Lipantil® 200 M, appropriate treatment should be performed to eliminate the cause of secondary hypercholesterolemia,for example, with such diseases as uncontrolled diabetes mellitus 2 tina, hypothyroidism, nephrotic syndrome, dysproteinemia, obstructive liver disease, the consequences of drug therapy, alcoholism.

    Increase in lipid concentration can be caused by taking estrogens. 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.

    Function liver: When taking the drug Lipantil® 200 M 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. It is recommended to monitor the activity of transaminases (alanine aminotransferase (ALT), aspartate aminotransferase (ACT)) every 3 months for the first 12 months and periodically during further treatment.

    Patients who have increased transaminase activity against the background of treatment require attention and, in the case of increased ALT activity and ACT more than 3 times compared with the upper limit of the norm, the drug is stopped.When symptoms of hepatitis (jaundice, pruritus) appear, laboratory tests should be performed and, if confirmed with a diagnosis of hepatitis, cancel fenofibrate.

    Pancreatitis: Cases of pancreatitis during the treatment with Lipantil® 200M were described. Possible causes of pancreatitis in these cases were: insufficient efficacy of the drug in patients with severe hypertriglyceridemia, direct exposure to the drug, and secondary phenomena associated with the presence of stones or the formation of sediment in the bile ducts , accompanied by obstruction of the common bile duct.

    Muscles: When taking Lipantil® 200 M and other lipid lowering drugs, cases of toxic effects on muscle tissue with or without renal failure are described, 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.

    The toxic effect on muscle tissue can be suspected on the basis of the patient's complaints of weakness, diffuse myalgia, myositis,muscle cramps and convulsions and / or a marked increase in creatinine phosphokinase (CK) activity (more than 5 times the upper limit of the norm) In these cases, treatment with Lipantyl® 200 M 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, kidney failure, hypothyroidism, and alcohol abuse. Such patients should be prescribed a drug only if the expected benefit exceeds the possible risk of rhabdomyolysis.

    If you take Lipantyl® 200 M together with HMG-CoA reductase inhibitors or other fibrates, the risk of serious toxic effects on muscle fibers increases, especially if the patient had muscle diseases before starting treatment. In this regard, the joint administration of the drug Lipantil® 200 M and statins is permissible only if the patient has severe mixed dyslipidemia and high cardiovascular risk, in the absence of a history of muscle disease and under the conditions of regular monitoring aimed at revealing signs of the development of toxic effects on muscle the cloth.

    Renal function: In case of increasing the concentration of creatinine in the blood plasma by more than 50% above the upper limit of the norm, treatment should be stopped. It is recommended to determine the concentration of creatinine in the first 3 months and periodically during further treatment.

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

    Lipantil® 200 M does not influence or affects to a minimum the ability to drive a vehicle or operate machinery, so care must be taken (risk of developing dizziness).

    Form release / dosage:Capsules, 200 mg.
    Packaging:

    10 capsules in PVC / Al blister. For 3 blisters in a cardboard pack together with instructions for use.

    For 15 capsules in PVC / Al blister. For 2 blisters in a cardboard bundle, together with instructions for use.

    Storage conditions:

    In a dry place at a temperature of 15 ° C to 25 ° C.

    Keep out of the reach of children.
    Shelf life:

    3 years.

    Do not use after the expiry date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:П N013707 / 01
    Date of registration:05.05.2008
    The owner of the registration certificate:Laboratories SA Fournier.Laboratories SA Fournier. France
    Manufacturer: & nbsp
    Representation: & nbspABBOTT LABORATORIES LLC ABBOTT LABORATORIES LLC Russia
    Information update date: & nbsp20.09.2015
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