Traykor

General characteristics. Structure:

Active agent:

Fenofibrat (micronized) 145,0 mg

Excipients:

Sucrose of 145,0 mg

Sodium lauryl sulfate of 10,2 mg

Lactoses monohydrate of 132,0 mg

Krospovidon of 75,5 mg

Cellulose of microcrystallic 84,28 mg

Silicon dioxide of colloid 1,72 mg

Gipromelloza of 29,0 mg

Docusate of sodium of 2,9 mg

Magnesium stearate of 0,9 mg

Cover (Opadri® of OY-B-28920): 25,1 mg

Polyvinyl alcohol of 11,43 mg

Titanium dioxide of 8,03 mg

Talc of 5,02 mg

Lecithin of soy 0,50 mg

Gum of xanthane 0,12 mg

Description

Oblong tablets film coated white color, with a text "145" on one party, and a logo on other party of a tablet.

Pharmacological properties:

Pharmacodynamics. Activating the RAPP-alpha (the alpha receptors activated by a proliferator of peroxisomas), фенофибрат strengthens a lipolysis and removal from plasma of atherogenous lipoproteids with the high content of triglycerides by activation of lipoproteinlipase and reduction of synthesis of SSh apoprotein. Activation the RAPP-alpha also leads to strengthening of synthesis of AI and AII apoproteins.

Fenofibrat is derivative fibroyevy acid which ability to change the maintenance of lipids in a human body, is mediated by activation the RAPP-alpha.

The effects of a fenofibrat described above on lipoproteids lead to reduction of maintenance of fraction of lipoproteids of low (LPNP) and very low density (LPONP) to which number apoprotein B, and to increase in maintenance of fraction of lipoproteids of the high density (LPVP) to which number AI and AII apoproteins belong belongs.

Besides, due to correction of disturbances of synthesis and a catabolism of LPONP, фенофибрат increases clearance of LPNP and reduces contents dense and the small particle size LPNP which increase is observed at patients with an atherogenous phenotype of lipids, frequent disturbance at patients with risk of coronary heart disease.

During clinical trials it was noted that use of a fenofibrat reduces the level of the general cholesterol by 20 — 25% and triglycerides for 40 — 55% at increase in level of LPVP-cholesterol for 10 — 30%. At patients with a hypercholesterolemia, at whom the level of LPNP-cholesterol decreases by 20 — 35%, use of a fenofibrat led to decrease in ratios: "the general cholesterol / ЛПВП-холестерин", "LPNP-holesterin/LPVP-holesterin" and "Apo In / Apo of AI", being markers of atherogenous risk.

Considering influence of a fenofibrat on the level of LPNP-cholesterol and triglycerides, use of drug is effective at patients with the hypercholesterolemia which both is followed, and which is not followed by a gipertriglitseridemiya including a secondary giperlipoproteinemiya, for example at a diabetes mellitus of the 2nd type.

During treatment fenofibraty can decrease considerably and even completely to disappear extravasated deposits of cholesterol (tendinous and tuberous xanthomas).

At the patients with the increased level of fibrinogen who received treatment fenofibraty considerable decrease in this indicator as well as at patients with the increased level of lipoproteids is noted. Other markers of an inflammation, such as S-reactive protein, also decrease at treatment fenofibraty.

For patients with a dislipidemiya and a hyperuricemia the additional benefit consists in the uricosuric effect of a fenofibrat leading to decrease in concentration of uric acid approximately by 25%.

During clinical trial and in experiments on animals it was shown what фенофибрат reduces the aggregation of thrombocytes caused by adenosinediphosphate, arachidonic acid and Epinephrinum.

Pharmacokinetics. Traykor 145 mg of a tablet film coated contain 145 mg of the micronized fenofibrat in the form of nanoparticles.

Initial фенофибрат in plasma it is not found. The main plasma metabolite is fenofibroyevy acid.

Absorption: the maximum concentration in a blood plasma (Cmax) is reached in 2-4 hours after intake. At prolonged use concentration of drug in plasma remains stable, irrespective of specific features of the patient.

Unlike the previous dosage forms of a fenofibrat, the maximum concentration in a blood plasma and the systemic effect of a fenofibrat in the form of nanoparticles does not depend on meal. Therefore Traykor 145 mg can be accepted irrespective of meal at any time.

Distribution: fenofibroyevy acid strongly contacts plasma albumine (more than 99%).

Elimination half-life: an elimination half-life of fenofibroyevy acid (T½) - about 20 hours.

Metabolism and removal: after use inside фенофибрат it is quickly hydrolyzed by esterases. In plasma only the main active metabolite of a fenofibrat — fenofibroyevy acid is found. Fenofibrat is not substrate for CYP 3A4. Does not take part in microsomal metabolism.

It is removed, mainly, with urine in the form of fenofibroyevy acid and a conjugate of a glucuronide. Within 6 days фенофибрат it is removed almost completely. The general clearance of fenofibroyevy acid defined at elderly patients does not change.

Drug does not kumulirutsya after a single dose and at prolonged use.

At a hemodialysis it is not removed.

Indications to use:

The hypercholesterolemia and gipertriglitseridemiya isolated or mixed (a dislipidemiya the type IIa, IIb, III, IV, V) at patients for whom the diet or other non-drug medical actions (for example, decrease in body weight or increase in physical activity) were inefficient, especially with the risk factors connected with a dislipidemiya, such as an arterial hypertension and smoking.

For treatment of a secondary giperlipoproteinemiya drug is used when the giperlipoproteinemiya remains, despite effective treatment of a basic disease (for example, a dislipidemiya at a diabetes mellitus).

Route of administration and doses:

Traykor's tablets of 145 mg should be swallowed entirely, without chewing, washing down with water.

Traykor 145 mg can be accepted at any time, irrespective of meal.

Adults. On one tablet of Traykor of 145 mg once a day.

The patients accepting on one capsule of a fenofibrat 200 mg or on one tablet of a fenofibrat of 160 mg a day can pass to reception of 1 tablet of Traykor 145 mg without additional correction of a dose.

Elderly patients. It is recommended to accept a standard dose for adults (on one tablet of Traykor of 145 mg once a day).

Patients with a liver failure.

Use of drug for patients with a liver failure is not studied.

Drug it is necessary to accept a long time, at the same time continuing to keep to a diet to which the patient adhered prior to treatment of Traykory 145 mg.

Features of use:

Before starting treatment of Traykory 145 mg, it is necessary to carry out the corresponding treatment for elimination of the reason of a secondary hypercholesterolemia, for example, at such diseases as an uncontrollable diabetes mellitus 2 types, a hypothyroidism, a nephrotic syndrome, a disproteinemia, obstructive diseases of a liver, an effect of medicamentous therapy, alcoholism.

Efficiency of therapy should be estimated on the maintenance of lipids (the general cholesterol, LPNP, triglycerides) in blood serum. In the absence of therapeutic effect after several months of therapy (as a rule, after 3 months) it is necessary to consider expediency of purpose of the accompanying or alternative therapy.

It is necessary to find out from the patients with a lipidemia accepting the estrogen or hormonal contraceptives containing estrogen whether the lipidemia has primary or secondary nature. In such cases increase in level of lipids can be caused by reception of estrogen.

Function of a liver: At Traykor's reception 145 mg and other drugs reducing concentration of lipids at some patients increase in level of "hepatic" transaminases is described. In most cases such increase was temporary, insignificant and asymptomatic. Within the first 12 months of treatment it is recommended to control the level of transaminases (ALT, nuclear heating plant) every 3 month. Patients at whom against the background of treatment concentration of transaminases increased require attention, and in case of increase in concentration of ALT and nuclear heating plant more than by 3 times in comparison with the upper bound of norm stop administration of drug.

Pancreatitis: Cases of development of pancreatitis during treatment of Traykory 145 mg were described. The possible reasons of pancreatitis in these cases were: insufficient efficiency of drug at patients with a heavy gipertriglitseridemiya, direct influence of drug, and also the secondary phenomena connected with existence of the stones or formation of a deposit in a gall bladder which are followed by impassability of the general bilious channel.

Muscles: At Traykor's reception 145 mg and other medicines reducing concentration of lipids are described cases of toxic influence on muscular tissue, including very exceptional cases of a rabdomioliz. Frequency of such disturbance increases in case of a hypoalbuminemia and a renal failure in the anamnesis.

Toxic influence on muscular tissue can be suspected on the basis of complaints of the patient to weakness, a diffusion mialgiya, a miositis, muscular spasms and spasms and/or the expressed increase in a kreatininfosfokinaza (KFK) (more than by 5 times in comparison with the upper bound of norm). In these cases treatment of Traykory 145 mg needs to be stopped.

The risk of development of a rabdomioliz can increase at patients with predisposition to a myopathy and/or a rabdomioliz, including age 70 years, the burdened anamnesis on hereditary muscular diseases, a renal failure, a hypothyroidism, an alcohol abuse are more senior. Such patients should appoint drug only if the expected advantage exceeds possible risk of development of a rabdomioliz.

At Traykor's reception 145 mg along with inhibitors of GMG-KOA-reduktazy or other fibrata the risk of serious toxic impact on muscle fibers, especially increases if the patient prior to treatment had a disease of muscles. In this regard, joint appointment of Traykor of 145 mg and statine is admissible only in the presence at the patient of the heavy mixed dislipidemiya and high cardiovascular risk, in the absence of a disease of muscles in the anamnesis and in the conditions of the fixed control directed to identification of signs of development of toxic influence on muscular tissue.

Renal function: In case of increase in concentration of creatinine treatment more than 50% higher than the upper bound of norm should be suspended. In the first three months of treatment it is recommended to define concentration of creatinine.

Influence on ability to driving and other mechanisms

At use of drug influence on ability to driving by the car and to control of mechanisms was not noted.

Side effects:

Undesirable effects are classified as follows: very often (≥1/10), it is frequent (≥1/100, <1/10), infrequently (≥1/1000, <1/100), is rare (≥1/10000, <1/1000) and is very rare (<1/10000), including single messages:

From digestive tract:

Often: moderate degree gastric and intestinal frustration (abdominal pain, nausea, vomiting, diarrhea, meteorism).

Not often: cases панкреатита*.

From a liver:

Often: moderate increase in concentration of serumal transaminases.

Not often: cholelithiasis.

Very seldom: hepatitis. At emergence of symptoms of hepatitis (jaundice, a skin itch) it is necessary to conduct laboratory researches and, in case of confirmation of hepatitis, to cancel фенофибрат. (See the section "Special Instructions").

From skeletal and muscular system and connecting fabric:

Seldom: diffusion mialgiya, miositis, spasm of muscles and weakness.

Very seldom: рабдомиолиз, increase in activity of a kreatinfosfokinaza (KFK).

Vascular disorders:

Not often: thromboembolism (thromboembolism of a pulmonary artery and deep vein thrombosis of the lower extremities).*

From circulatory and lymphatic system:

Seldom: decrease in hemoglobin and leukocytes.

From a nervous system:

Seldom: sexual dysfunction, headache.

From a respiratory organs:

Very seldom: intersticial pneumopathies.

From skin and a hypodermic fatty tissue:

Not often: rash, skin itch, small tortoiseshell or reactions of a photosensitivity.

Seldom: alopecia.

Very seldom: the photosensitization which is followed by an erythema, blistering or small knots on the sites of skin subjected to impact of a sunlight or artificial UF-lighting (for example, a quartz lamp) in some cases (even after months-long use without any complications).

Laboratory indicators:

Not often: increase in concentration of creatinine and an urea nitrogen in blood serum.

* In clinical trial at patients with a diabetes mellitus 2 types receiving фенофибрат were revealed statistically significant increase in cases of pancreatitis and increase in cases of a thromboembolism of a pulmonary artery. In the same research statistically insignificant increase in cases of a deep vein thrombosis was revealed.

Interaction with other medicines:

Peroral anticoagulants

Fenofibrat strengthens effect of peroral anticoagulants and can increase risk of bleedings that it is connected with replacement of anticoagulant from places of linkng with proteins of a blood plasma.

In an initiation of treatment fenofibraty it is recommended to lower a dose of anticoagulants approximately on a third with the subsequent gradual selection of a dose. Selection of a dose is recommended to be carried out under control of the INR (the international normalized relation) level.

Cyclosporine

Several hard cases of reversible decrease in renal function are described during simultaneous treatment fenofibraty and cyclosporine. Therefore it is necessary to control a condition of renal function at such patients and to cancel фенофибрат in case of serious change of laboratory parameters.

Inhibitors of GMG-KOA-reduktazy and other fibrata

At reception of a fenofibrat along with inhibitors of GMG-KOA-reduktazy or other fibrata the risk of serious toxic impact on muscle fibers increases (see the section "Special Instructions").

Derivatives of a tiazolidindion (glitazona)

At simultaneous use of a fenofibrat and glitazon it was reported about several cases of reversible paradoxical decrease in LPVP cholesterol. Therefore when performing simultaneous therapy control of concentration of LPVP cholesterol is recommended, and in case of detection of too low concentration of LPVP cholesterol to cancel drugs.

P450 cytochrome enzymes: researches of microsomes from a liver of the person of in vitro showed that фенофибрат and fenofibroyevy acid are not inhibitors of the following isoenzymes of P450 cytochrome (CYP3A4, CYP2D6. CYP2E1 or CYP1A2). In therapeutic concentration these connections are weak inhibitors of isoenzymes of CYP2C19 and CYP2A6 and weak or moderate CYP2C9 inhibitors.

Contraindications:

Drug is contraindicated in the following cases:

— hypersensitivity to a fenofibrat or other components of medicine,

— a liver failure (including cirrhosis),

— heavy renal failure (clearance of creatinine <30 ml/min.),

— age up to 18 years,

— existence in the anamnesis of a photosensitization or phototoxicity at treatment of a fibratama or ketoprofen,

— diseases of a gall bladder,

— pregnancy and period of a lactation,

— an inborn galactosemia, insufficiency of lactase, disturbance of absorption of glucose and a galactose (drug contains lactose),

— an inborn fruktozemiya, insufficiency of invertase-isomaltase (drug contains sucrose),

— allergic reaction to a peanut, peanut butter, soy lecithin or related products in the anamnesis (in connection with risk of development of hypersensitivity reaction),

— chronic or acute pancreatitis, except for cases of the acute pancreatitis caused by the expressed triglitseridemiya.

With care

at a liver and/or renal failure, a hypothyroidism; to the patients abusing alcohol, advanced age with the burdened anamnesis on hereditary muscular diseases; at a concomitant use of peroral anticoagulants, GMG-KOA-reduktazy inhibitors (see the section "Interaction with Other Medicines").

Pregnancy and period of a lactation

Pregnancy

Drug is contraindicated to use during pregnancy. There are not numerous data on use of a fenofibrat by pregnant women. In experiments on animals the teratogenic effect of a fenofibrat was not observed. Embriotoxity was noted at appointment during preclinical tests of doses, toxic for a maternal organism. The potential risk for the person is unknown.

Lactation period

Drug is contraindicated to use during breastfeeding (not enough data on use of drug during this period).

Overdose:

Cases of overdose are not described. The specific antidote is unknown. At suspicion it is necessary to appoint to overdose symptomatic and, if necessary, the supporting treatment.

The hemodialysis is inefficient.

Storage conditions:

List B. In the dry place at a temperature not above 25 °C in an original packing. To store in the place, unavailable to children! Period of validity 3 years. Not to apply after the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Tablets film coated 145 mg.

On 10 tablets in PVC/PE/PVDH / the blister Is scarlet. On 1, 2, 3, 5, 9, 10 blisters in a cardboard pack together with the application instruction.

On 14 tablets in PVC/PE/PVDH / the blister Is scarlet. On 2, 6, 7 blisters in a cardboard pack together with the application instruction.

On 10 tablets in PVC/PE/PVDH / the blister Is scarlet. On 28, 30 blisters in boxes cardboard (packaging for hospitals).