Index of drugs

The drug is indicated for use as an additive to the diet and other non-pharmacological treatments (eg physical exercise, weight loss) in the following cases: treatment of severe hypertriglyceridemia with low HDL cholesterol or without; mixed hyperlipidemia, if the use of statins is contraindicated or they are not tolerated; mixed hyperlipidemia in patients at high risk of cardiovascular disease as an adjunct to statin therapy, if triglycerides and HDL cholesterol levels are not adequately controlled.

One capsule contains 100 mg of fenofibrate. One capsule contains 200 mg of micronized fenofibrate. The preparation contains lactose.

A lipid-lowering drug, a fibrin derivative. Lipid-modifying activity takes place through the activation of alpha-type nuclear receptors (PPARα). By activating PPARα, fenofibrate increases lipolysis and plasma elimination of aterogenic triglyceride-rich particles by activating lipoprotein lipase and reducing the production of apolipoprotein CIII. PPARα activation also increases the synthesis of apolipoprotein AI and AII. The above action of fenofibrate on lipoproteins leads to the reduction of low and very low density cholesterol (VLDL and LDL) fractions containing apolipoprotein B as well as to the increase of high density lipoprotein (HDL) containing apolipoproteins AI and AII. In addition, by modifying the synthesis and catabolism of the VLDL fraction, fenofibrate enhances the removal of the LDL fraction and reduces the concentration of small, dense LDL particles, which is increased in atherogenic dyslipidemia and is a risk factor for ischemic heart disease. After oral administration of C_max in plasma is achieved after 4-5 h. Plasma concentration is constant during its long-term intake. Fenofibric acid binds strongly to plasma albumin (over 99%). After oral ingestion, fenofibrate is quickly hydrolysed by esterase to the active metabolite, fenofibrin acid. There is no unchanged fenofibrate in plasma. Fenofibrate is not a substrate for CYP3A4. There is no hepatic microsomal metabolism. The drug is excreted mainly in the urine, primarily in the form of fenofibric acid and its glucuronide derivatives. Kinetic studies showed no accumulation of the drug both after a single administration and after long-term treatment. Hemodialysis does not remove fenofibric acid from the body. T_0,5 fenofibric acid in the plasma is about 20 h.

Hypersensitivity to the active substance or to any of the excipients. Hepatic insufficiency (including biliary cirrhosis and unexplained prolonged hepatic dysfunction, eg prolonged elevations of serum transaminases). Renal failure (creatinine clearance <20 ml / min). Gallbladder disease. Sensitization to light or phototoxic reactions when using fibrates or ketoprofen. Chronic or acute pancreatitis with the exception of acute pancreatitis caused by severe hypertriglyceridemia. Children (under 18 years).

Secondary causes of hypercholesterolemia, such as: uncontrolled type 2 diabetes, hypothyroidism, nephrotic syndrome, dysproteinemia, cholestasis, alcoholism, should be adequately treated before starting fenofibrate therapy. Adequate treatment should also be implemented if the causes of hypercholesterolemia include prior pharmacological treatment. In patients with hyperlipidemia taking oestrogens or estrogen-containing contraceptives, it is important to check whether hyperlipidaemia is primary or secondary (possible increase in lipid levels caused by estrogens administered orally). For the first 12 months of administration, monitoring of aminotransferase levels is recommended every 3 months, then periodically. Attention should be paid to patients who have increased transaminase levels and discontinued treatment, if AST and ALT increase above 3 times the upper limit of values ​​considered normal. If signs suggestive of hepatitis (eg jaundice or pruritus) appear and are confirmed by laboratory tests, treatment with fenofibrate should be discontinued.Cases of pancreatitis have been reported in patients taking fenofibrate - it may be the result of a lack of effective treatment in patients with severe hypertriglyceridemia, direct drug effects, or it may be caused secondary by the formation of gallstones or deposits obstructing the common bile duct. After administration of fibrates, there is a risk of muscle toxicity, including rare cases of rhabdomyolysis with or without kidney damage, especially in patients with hypoalbuminemia and concomitant renal insufficiency. Toxic effects on muscles should be suspected in patients suffering from disseminated muscular pains in whom there is inflammation, cramps, muscle weakness and / or a significant increase in creatine kinase activity (CK activity 5 times above normal) - in this case treatment with fenofibrate should be discontinued. In patients with predisposing factors for myopathy and / or decay of striated muscles, including: age over 70 years, individual or familial tendency to muscle diseases, renal dysfunction, hypothyroidism and alcoholism, the risk and risk ratio should be carefully evaluated. benefits before starting treatment. The risk of muscle toxicity may increase if the medicine is used with another fibrate or HMG-CoA reductase inhibitor, especially if muscle disorders have occurred previously - combination therapy with fenofibrate and statin or with another fibrate should only be used in patients with severe, mixed dyslipidemia and large the risk of cardiovascular disease in which no muscle disease has previously occurred. Combination therapy should be used with extreme caution and patients should be monitored for muscle toxicity. Treatment should be discontinued if the creatinine level is increased above 50% GGN. It is recommended to measure creatinine during the first 3 months after starting treatment and then periodically during treatment. The preparation contains lactose - should not be used in patients with rare hereditary galactose intolerance, lactase deficiency (Lapp type) or malabsorption of glucose-galactose.

Due to the lack of sufficient data during pregnancy, the preparation should only be used after a thorough benefit and risk assessment. There are no data on the penetration of fenofibrate and its metabolites in breast milk - the preparation should not be used during breastfeeding.

Common: signs and symptoms from the stomach and intestines (abdominal pain, nausea, vomiting, diarrhea and bloating with the passing of winds), increase in transaminases. Uncommon: headache, thromboembolism (pulmonary embolism, deep vein thrombosis), pancreatitis, cholelithiasis, hypersensitivity of the skin (eg rash, pruritus, urticaria), muscle disorders (eg mialgia, myositis, cramps and weakness muscles), potency disorders, increased blood creatinine. Rare: reduced hemoglobin, decreased white blood cell count, hypersensitivity, hepatitis, alopecia, hypersensitivity to light, increased blood urea. Not known: interstitial lung disease, jaundice, cholelithiasis complications (eg cholecystitis, cholangitis, biliary colic, etc.), rhabdomyolysis, severe skin reactions (eg erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis ).

Orally. Patients should use the appropriate diet and other recommended non-pharmacological treatments for hyperlipidemia.Kaps. 100 mg. Adults: the recommended dose is 3 capsules per day during the main meal in one or several divided doses; if the cholesterol level remains above 4 g / l despite the diet, the initial dose may be 4 capsules per day. The initial dose should be administered until normalization of serum cholesterol. When the concentration is constant, a dose of 2 capsules per day may be recommended and the cholesterol concentration should be checked every 3 months. If the lipid concentration increases again, the dose should be returned to 3 capsules a day.Capsules 200 mg. AdultsThe recommended dose is 1 capsule once a day with meals. If necessary, the dose can be increased to 1 capsules of 267 mg once a day or 4 capsules of 100 mg once a day. Serum lipids should be monitored to check the effectiveness of treatment.If the expected result is not achieved after a few (eg three) months of treatment, additional or different treatment should be used. The drug to take during the meal, because the absorption of the drug on an empty stomach is weaker. Swallow the capsules whole and drink with water.Special groups of patients. In elderly patients with no concomitant renal insufficiency a dose is recommended as in adults. In patients with renal impairment (creatinine clearance 20-60 ml / min), 1 capsule 100 mg daily should be used; do not use fenofibrate in patients with creatinine clearance below 20 ml / min. In patients with hepatic impairment, the preparation is not recommended due to the lack of clinical data for this group. Fenofibrate is not recommended for patients under 18 years of age.