Fenofibrate tabs 145mg #30

Instruction for Fenofibrate

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Fenofibrate is a lipid-lowering agent.

Release form and composition

The drug is produced in the form of film-coated tablets, oval, biconvex, almost white or white (in a blister strip 7, 10, 14 or 15 pcs., In a cardboard box, instructions for the use of Fenofibrate and 4, 12, 14 packs of 7 tablets, or 1,2, 3, 5, 6, 9, 10 packs of 10 tablets, or 2, 6, 7 packs of 14 tablets, or 2, 4, 6 packs of 15 tablets).
Composition of 1 tablet:
    active substance: fenofibrate - 145 mg;
    auxiliary components: magnesium stearate, microcrystalline cellulose, colloidal silicon dioxide, mannitol, croscarmellose sodium, povidone K-30, corn starch;
    film casing: Opadray II [talc, polyvinyl alcohol, titanium dioxide, macrogol (polyethylene glycol 4000)].

Pharmacodynamics

By its structure, fenofibrate is a derivative of fibric acid. Its ability to reduce lipids in the body is mediated by the activation of PPAR-alpha (alpha receptors).
Under the action of the drug, RAPP-alpha is activated. As a result, the activity of lipoprotein lipase increases and the synthesis of apoproteins C-III (ApoC-III) decreases, thereby increasing lipolysis, increasing the excretion of atherogenic lipoproteins with a high content of triglycerides (TG) from the plasma. In addition, the activation of PPAR-alpha stimulates the synthesis of apoproteins A-I (ApoA-I) and A-II (ApoA-II).
When taking Fenofibrate decreases the content of low density lipoproteins (LDL) and very low density lipoproteins (VLDL), including apoprotein B (ApoB). Also, under the influence of the drug, the content of high density lipoproteins (HDL), including ApoA-I and ApoA-II, increases.
Given the ability of the active substance to disrupt the synthesis and catabolism of VLDL, Fenofibrate also increases the clearance of LDL. It reduces the content of small dense LDL particles in patients with atherogenic lipid phenotype and in patients at risk of coronary heart disease with impaired content. In clinical studies, it was found that fenofibrate reduces the concentration of total cholesterol (TC) by 20-25% and the level of TG by 40-55% in the case of an increase in HDL by no more than 30%. In patients with hypercholesterolemia, accompanied by a decrease in LDL by 20–35%, fenofibrate is able to reduce the TOC / HDL, LDL / HDL and ApoB / ApoA-I ratios, which are markers of a high atherogenic coefficient.
Due to the significant effect of the drug on the concentration of LDL and TG, Fenofibrate is effective for hypercholesterolemia, including accompanied by hypertriglyceridemia, including secondary hyperlipoproteinemia, for example, concomitant type 2 diabetes mellitus. Fenofibrate can significantly reduce and even completely eliminate tuberous and tendon xanthomas (extravascular cholesterol deposits). With an increased level of fibrinogen, Fenofibrate significantly reduces this indicator, similar to the action in patients with increased levels of lipoproteins. Other markers of inflammation, such as C-reactive protein, are also reduced in people taking the drug.
With hyperuricemia and dyslipidemia, the drug has another positive effect - the uricosuric effect, which causes a decrease in the concentration of uric acid by about 25%.
In experimental animal studies and clinical studies, it was found that Fenofibrate also attenuates platelet aggregation caused by drugs such as epinephrine, adenosine diphosphate and arachidonic acid.

Pharmacokinetics

The drug Fenofibrate contains a micronized active substance with a higher bioavailability. In its original form, the active ingredient is not found in blood plasma. The main plasma metabolite, fenofibric acid, is revealed.
The main pharmacokinetic parameters of fenofibrate:
    absorption: fenofibrate is rapidly absorbed into the bloodstream after oral administration, the maximum plasma concentration reaches within 4–5 hours. With long-term treatment, the plasma concentration remains stable. In the case of taking the drug simultaneously with food, the absorption of the substance is enhanced;
    distribution: the main plasma metabolite in a high degree (not less than 99%) binds to blood plasma albumin;
    metabolism: only fenofibric acid is found in pure form in plasma. It does not participate in microsomal metabolism, it is not a substrate for the CYP3A4 isoenzyme. The half-life of fenofibric acid is approximately 20 hours;
    excretion: fenofibrate is excreted from the body by the kidneys mainly in the form of the main plasma metabolite and in the form of a glucuronide conjugate. Within 6 days after administration, the drug is excreted almost completely. In the elderly, the total detectable clearance of fenofibric acid does not change.
With prolonged use, Fenofibrate does not accumulate in the body. It is not excreted during hemodialysis.

Indications for use

Fenofibrate  is prescribed in combination with diet therapy in the following cases:
    severe hyperglyceridemia (dyslipidemia IV and V type according to Fredrickson) - to reduce the concentration of triglycerides;
    primary hyperlipidemia and mixed dyslipidemia (type IIa, IIb, III, IV according to Fredrickson) - to reduce total cholesterol, increased concentrations of LDL, TG and Apo-B, as well as to increase the level of HDL;
    mixed dyslipidemia (type IIa, IIb according to Fredrickson) in patients with coronary heart disease or a high risk of its development (diabetes mellitus, abdominal aortic aneurysm, peripheral arterial atherosclerosis, symptomatic carotid atherosclerosis, or the presence of multiple risk factors corresponding to a 10-year risk of coronary complications more than 20%) - to reduce TG and increase HDL. In this case, Fenofibrate  is prescribed in combination with statins - inhibitors of HMG-CoA (3-hydroxy-3-methylglutaryl-coenzyme A) reductase.

Contraindications

Absolute:
    history of gallbladder disease;
    severe renal failure [creatinine clearance (CC) <20 ml / min];
    liver failure, including persistent liver dysfunction of unknown etiology and biliary cirrhosis;
    the development of photosensitization or phototoxicity with previous treatment with ketoprofen or fibrates;
    acute or chronic pancreatitis, with the exception of an acute condition caused by severe hypertriglyceridemia;
    age under 18;
    lactation period;
    hypersensitivity to any component of the drug.
Relative (Fenofibrate  tablets should be taken with extreme caution, after a careful assessment of the balance of benefits and risks):
    hypothyroidism;
    renal dysfunction with CC> 20 ml / min;
    alcohol abuse;
    advanced age of patients with a burdened history of hereditary muscle diseases;
    concomitant use of HMG-CoA reductase inhibitors or oral anticoagulants;
    period of pregnancy.

Instructions for use: method and dosage

Fenofibrate  film-coated tablets should be taken orally, swallowed whole with food.
Adult patients are prescribed 1 tablet 1 time per day. Patients receiving fenofibrate 200 mg capsules can be switched to Fenofibrate  145 mg tablets without dose adjustment.
It is prohibited to exceed the dose. Elderly patients do not change the dosage regimen.
Treatment with the drug is long-term and should be carried out against the background of standard diet therapy, which was prescribed by the doctor before the appointment of  Fenofibrate.

Side effects

During the use of fenofibrate, the following side effects were reported (in frequency they are classified as follows: very often -> 10% of cases, often - from> 1% to <10%, infrequently - from> 0.1% to <1%, rarely - from> 0.01% to <0.1%, very rarely - <0.01%):
    from the digestive tract: often - moderate severity of flatulence and diarrhea, nausea, vomiting, abdominal pain; infrequently - pancreatitis;
    on the part of the hepatobiliary system: often - an increase in the concentration of serum transaminases of a moderate degree; infrequently - the formation of gallstones; very rarely - hepatitis (the first symptoms are itching, jaundice);
    from the respiratory system: very rarely - interstitial pneumopathies;
    from the musculoskeletal system: rarely - muscle weakness, muscle spasm, myositis, diffuse myalgia; very rarely - increased activity of creatine phosphokinase, rhabdomyolysis;
    from the central and peripheral nervous system: rarely - headache, sexual dysfunction;
    on the part of the circulatory and lymphatic systems: rarely - an increase in the level of hemoglobin and leukocytes;
    vascular disorders: infrequently - venous thromboembolism (deep vein thrombosis, pulmonary embolism);
    on the part of the skin and subcutaneous fat: infrequently - itching, urticaria, rash, photosensitivity reactions; rarely - alopecia; very rarely - photosensitivity accompanied by erythema, the formation of nodules / blisters on areas of the skin exposed to sunlight or UV light;
    laboratory data: infrequently - an increase in the concentration of urea and creatinine in the blood serum.

Overdose

To date, no cases of fenofibrate overdose have been reported. The specific antidote to the substance has not been established.
In case of suspicion of intoxication, symptomatic and supportive therapy is indicated. Hemodialysis is ineffective.

Special instructions

Fenofibrate should be prescribed after appropriate treatment aimed at eliminating the cause of the development of secondary hypercholesterolemia, for example, hypothyroidism, uncontrolled type 2 diabetes mellitus, dysproteinemia, nephrotic syndrome, obstructive liver disease, alcoholism, complications of drug therapy.
The effectiveness of the treatment is assessed by the content of TC, TG, LDL in the blood serum. If there is no improvement after several months (usually three) after starting the drug, the doctor considers the appropriateness of prescribing alternative or concomitant therapy.
In patients with hyperlipidemia who are taking hormonal contraceptives or estrogen preparations, before prescribing Fenofibrate, it is necessary to find out the nature of the development of hyperlipidemia (primary or secondary), since estrogens can cause an increase in lipid concentration.

Pancreatitis

There are rare cases of pancreatitis during treatment with fenofibrate. The alleged causes of this complication:
    direct exposure to fenofibrate;
    insufficient efficacy of  Fenofibrate in patients with severe hypertriglyceridemia;
    secondary phenomena due to the formation of sediment or the presence of stones in the gallbladder, which is accompanied by obstruction of the common bile duct.

Musculoskeletal system

Lipid-lowering drugs can be toxic to muscle tissue. Rare cases of the development of such a serious complication as rhabdomyolysis are described. The risk of its occurrence increases in patients with hypoalbuminemia and renal failure, including a history.
It is necessary to suspect a toxic effect on muscle tissue when the patient develops the following disorders: myositis, muscle weakness, diffuse myalgia, muscle spasms, convulsions, a pronounced increase in creatine phosphokinase activity ≥ 5 times compared to the upper limit of the norm. Fenofibrate  in this case is canceled.
The risk of rhabdomyolysis may also be increased in patients predisposed to myopathy and / or rhabdomyolysis. This group includes persons over 70 years of age, patients with hypothyroidism, renal dysfunction, a history of hereditary muscle diseases, and alcohol abuse. Fenofibrate  is prescribed for at-risk patients only if the expected benefit from therapy significantly outweighs the potential risk of developing rhabdomyolysis.
With the joint administration of HMG-CoA reductase inhibitors or other fibrates, the threat of dangerous toxic effects on muscle fibers increases, especially with concomitant muscle diseases. For this reason, Fenofibrate together with these drugs is prescribed only to patients with severe mixed dyslipidemia and high cardiovascular risk, provided that there is no history of muscle diseases. In this case, treatment is carried out under especially close medical supervision in relation to the timely detection of signs of the toxic effect of the drug on muscle tissue.

Liver function

Lipid-lowering drugs can increase the activity of hepatic transaminases. As a rule, this violation is temporary, mild and asymptomatic. However, during the first 12 months of taking  Fenofibrate, it is recommended that transaminase activity be checked every 3 months. In case of an increase in their concentration, careful medical supervision is required. If the indicators of alanine aminotransferase and aspartate aminotransferase have increased ≥ 3 times compared with the upper limit of normal, it is necessary to cancel this lipid-lowering agent.

Renal function

Fenofibrate, used both in combination with statins and as a monotherapy, can reversibly increase serum creatinine concentration. However, this disorder is stable during the entire treatment period. With long-term therapy, a further increase in the indicator was not observed. After discontinuation of the drug, the concentration returned to the initial values. The clinical significance of such changes has not been established.
When treating patients with renal insufficiency with Fenofibrate , it is recommended to monitor renal function. Special supervision is required for persons at risk of developing renal failure: the elderly and patients with diabetes mellitus. If, while taking the drug, the concentration of creatinine increases 2 times or more from the upper limit of the norm, the therapy is stopped. It is recommended to determine the concentration of creatinine within the first three months after the start of taking the drug, as well as periodically after its cancellation.

Influence on the ability to drive vehicles and complex mechanisms

No negative influence of Fenofibrate  on visual acuity, reaction speed and ability to concentrate was noted.

Application during pregnancy and lactation

In experimental studies conducted on animals, fenofibrate was not teratogenic. Embryotoxicity has been noted in preclinical trials of doses that are toxic to the mother. In this regard, the exact risk to humans has not been established, therefore, Fenofibrate  is prescribed to pregnant women if the expected benefits of treatment are higher than the potential risks.
During lactation, a lipid-lowering agent is contraindicated due to insufficient data on its safety for the child if the mother takes fenofibrate during this period.

Childhood use

Fenofibrate 145 mg tablets are not prescribed for patients under 18 years of age, since studies on its safety and efficacy have not been conducted in this category of patients.

With impaired renal function

    contraindicated: severe renal failure (CC <20 ml / min);
    with caution: renal dysfunction (CC> 20 ml / min).

For violations of liver function

Fenofibrate  is contraindicated in patients with hepatic insufficiency, including patients with liver dysfunction of unknown etiology and with biliary cirrhosis.

Use in the elderly

In elderly patients, Fenofibrate  is used with caution, especially in the case of a burdened history of hereditary muscle diseases.

Drug interactions

    oral anticoagulants: their effect is enhanced, the risk of bleeding increases (since fenofibrate displaces the anticoagulant from the sites of binding to plasma proteins). Patients who received anticoagulants should reduce their dose by about ⅓ part at the beginning of the use of Fenofibrate , in the future the dose is gradually adjusted under the control of the level of the International Normalized Ratio (INR);
    statins and other fibrates: the risk of dangerous toxic effects on muscle fibers increases;
    isozymes of the cytochrome P450 system: in vitro studies on human liver microsomes have shown that fenofibrate and fenofibric acid are not inhibitors of cytochrome P450 isoenzymes (CYP1A2, CYP2E1, CYP2D6, CYP3A4). At therapeutic concentrations, these compounds weakly inhibit the isoenzymes CYP2A6 and CYP2C19, weakly or moderately inhibit CYP2C9;
    cyclosporine: There are several severe cases of reversible decline in renal function with the combination of fenofibrate and cyclosporine, therefore treatment should be carried out under strict control of renal function. In case of serious changes in laboratory parameters, Fenofibrate  must be canceled.

Terms and conditions of storage

Store in a dry, dark place, out of the reach of children, at a temperature not exceeding 25 ° C.
Shelf life is 2 years.

Reviews of Fenofibrate

There are no reviews of Fenofibrate from patients on specialized sites and forums.
Various foreign studies have found that fenofibrate, by reducing total cholesterol, is able to reduce the risks of cardiovascular diseases, stroke and heart attack. In addition, factors such as endothelial dysfunction, inflammation, and vascular remodeling make an important contribution to the development of atherosclerosis (which is a common cause of stroke and heart attack). Fenofibrate activates PPAR-alpha receptors, thereby exerting anti-inflammatory effects by reducing inflammatory markers such as C-reactive protein and interleukin-6. However, it has not yet been established whether the drug can reduce mortality in the described group of patients.
In 2012, scientists at the University of Colorado (USA) in a small clinical study proved that fenofibrate can rejuvenate human blood vessels in just 7 days. By activating PPAR-alpha, the main metabolite (fenofibric acid) enhances the breakdown of fats and increases the elimination of triglycerides and LDL ("bad" cholesterol) from the blood. In addition, fenofibric acid reduces the synthesis of ApoC-III, which is also important for blood vessels. Thus, short-term use of fenofibrate in healthy people of different ages improves vascular endothelial function by reducing oxidative stress, as well as increasing endothelial nitric oxide synthase, an important component involved in the expansion of blood vessels while lowering high blood pressure.

Terms of sell

You don't need a prescription from a doctor to buy Fenofibrate.