Fenofibrate. 100 mg. 50 capsules
Fenofibrate. 100 mg. 50 capsules
QUALITATIVE AND QUANTITATIVE COMPOSITION
Each capsule contains the drug substance in an amount of fenofibrate and 100 mg.
3 . PHARMACEUTICAL FORM
4 . CLINICAL DATA
Treatment of hypercholesterolemia (type la ) and endogenous hypertriglyceridemia isolated (type IV) or combined (type IIb and III), when regular good diet has proved insufficient , especially if your cholesterol level remains high following a diet and / or there are risks factors.
4.2 . Dosage and method of administration
Administered orally 3 times daily 100 mg with meals . After achieving a therapeutic effect by a maintenance dose of 200 mg daily . The course of treatment is 3-6 months.
Patients with renal impairment :
In patients with mild to moderate renal insufficiency fenofibrate should be given in reduced doses: recommended dose clearance 60 to 20 ml / min , respectively, from 200 to 100 mg daily.
Has not been proven harmful in the long-term treatment of children with dyslipidemias and unknown effects on the growing organism , and therefore use of fenofibrate in children is not recommended
4.3 . Contraindications
Known hypersensitivity to the active substance or any component of the product; phototoxic / photoallergic reactions during treatment with fenofibrate or substances with similar structures , especially ketoprofen ; severe functional impairment of the kidneys; severe hepatic impairment , biliary stone disease, pregnancy and lactation .
4.4 . Special warnings and precautions for use
In the absence of a satisfactory therapeutic effect in the treatment with the drug for 3 to 6 months may need a change in treatment.
During treatment with fenofibrate is necessary to perform a systematic control of transaminases. If the values of ALAT and ASAT exceed three times the upper limit of the reference values , treatment with fenofibrate is terminated.
It is necessary to periodically monitor blood counts during the first months of treatment.
Suspicion of cholelithiasis need an ultrasound of the gallbladder. In establishing gallstones treatment with fenofibrate should be discontinued .
When treating with a group of fibrates may in rare cases to rhabdomyolysis . The risk is greater in patients with impaired renal function. Attention should be paid to patients with symptoms such as unexplained muscle pain, izstrapvane , weakness, particularly if accompanied by fever . If these symptoms it is necessary to trace levels of creatine phosphokinase and aspartate . With increasing plasma levels and presence of symptoms described treatment with fenofibrate is terminated. In hypothyroidism the risk of rhabdomyolysis have been reported with a group of fibrates has increased , so in patients with a history of such violations should be monitored
thyroid function before beginning the treatment with fenofibrate .
This product contains a colorant (E 110) - azootsvetyavasht agent that may cause allergic-type reactions including asthma. The risk of allergy is greater in patients allergic to aspirin .
4.5 . Medicinal and other vazimodeystviya
• Fenofibrate potentiate the action of oral anticoagulants and increases the risk of bleeding due to interaction at the level of plasma proteins. It is necessary to regularly monitor the prothrombin time and, if necessary to reduce the dose of anticoagulant (about one third ) .
• Concomitant use with other products in the fibrates or statins leads to increased risk of adverse drug reactions.
• Concurrent use with uricosuric products are recommended to reduce their dose as fenofibrate lowers elevated levels of uric acid.
4.6 . Use in pregnancy and lactation
Fenofibrate has embryotoxicity and teratogenicity in studies in rats and rabbits. Although no controlled clinical trials in this regard , drug use during pregnancy is contraindicated.
Although no information on the passage of fenofibrate in human milk is not recommended for use during breastfeeding .
4.7 . Effects on ability to drive and use machines
No effect on alertness and reactions , so that no data limits its use while driving or operating machinery .
4.8 . Undesirable effects
Fenofibrate is a product which is well tolerated by patients. Known adverse effects are:
- Of the digestive tract - nausea, belching , flatulence , abdominal pain, diarrhea ;
- By the skin and appendages - erythema , urticaria , increased
sweating , hair loss - by the Musculoskeletal
- Diffuse myalgia, tenderness , muscle weakness, blood levels of creatine phosphokinase and aspartate ;
- By the hepato-biliary system - elevations of serum transaminases , hepatitis, cholelithiasis ;
- CNS - dizziness , weakness , headache, insomnia ;
- Hematology - leukopenia ;
- Allergies - photosensitivity reactions .
4.9 . overdose
In clinical practice are not registered overdose. Possible symptoms are: nausea, vomiting , abdominal pain , headache, weakness. In case of overdose, the first measures are focused on the rapid elimination of unabsorbed drug from the body by inducing vomiting , stomach lavage. Treatment is symptomatic , as no specific antidote .
5 . Pharmacological
5.1. Pharmacodynamic properties
Fenofibrate has expressed antilipemic action , which is achieved by interference of the various enzymes responsible for the synthesis of cholesterol and triglycerides . Inhibition of cholesterol synthesis is effected by moderate blocking the enzyme hydroxymethylglutaryl CoA reductase . This leads to an increase in the number of receptors for low density lipoproteins , which bind and excrete bile with a greater amount of cholesterol. An advantage of this product is that it does not produce a compensatory increase in the enzyme that , as observed with other lipid-lowering agents . Fenofibrate reduces the concentration of the SBS apoprotein mainly CIII , which assists the activation of lipoprotein lipase , which causes the lowering of triglycerides. Increases clearance of VLDL and chylomicrons from the plasma. Fenofibrate results in increases in the content of Xc and reduce HDL clearance from plasma
Fenofibrate reduces emission of homocysteine by the kidneys, resulting in the increase of serum level of about 40 %.
Fenofibrate reduces the level of uric acid and fibrinogen and decreasing blood viscosity . Can act as antivitamin K.
5.2 . pharmacokinetics
Pharmacokinetic studies of Fenofibrate show that it is rapidly and almost completely from the gastrointestinal tract after oral administration with meals . Oral absorption is significantly reduced when taken on an empty stomach . Maximum plasma concentrations are reached 5 hours after administration, plasma half-life is about 20 hours. Fenofibrate is bound to plasma proteins to a high degree . It is metabolized rapidly and completely in the liver to form fenofibratova acid . The product is mainly excreted in the urine.
5.3 . Preclinical safety data
The survey results of the acute toxicity of the product after a single oral administration to mice and rats have shown that:
- LD5o rat ( p.o. ) was> 2000 mg / kg
- LD50 in rats ( p.o. ) was> 2000 mg / kg
According to the classification of Hodge and Sterner, oral rat Fenofibrate belongs to less toxic substances. After a month of treatment of rats at doses of 100 and 200 mg / kg body weight , and after 90 days of treatment at doses of 50 and 100 mg / kg body weight , no abnormalities were observed in hematology and biochemical parameters , is not mortality observed in test animals .
In a study of chronic (180 day ) toxicity in rats ( in a dose of 50 and 100 mg / kg) and dogs ( at a dose of 50 mg / kg), no statistically significant changes in the observed hematological and biochemical parameters . In studies in pregnant rats and rabbits found that fenofibrate has teratogenic effects.
6 . PHARMACEUTICAL PARTICULARS
6.1. List of ingredients and their quantities per capsule in mg:
Mannitol 54.5 mg
Lactose monohydrate 90.0 mg
Magnesium stearate 2.5 mg
Silica colloidal anhydrous 3.0 mg
Titanium dioxide ( E171 ) Sunset yellow (E 110 ) Gelatine
6.2 . Incompatibilities
6.3. Expiration date
6.4 . Special precautions for storage
At temperatures below 30 ° C.
6.5. Packaging Data
10 capsules in blister pack of solid , transparent PVC and aluminum foil.
5 blister with leaflet placed in a folding carton.
6.6. Recommendations for use
Do not apply after the expiry date stated on the packaging !
Keep out of reach of children!