Flutamid Pliva

General characteristics. Structure:

Active agent: 250 mg of a flutamid.

Excipients: lactose, sodium lauryl sulfate, microcrystallic cellulose, kukuzuzny starch, silicon dioxide anhydrous, magnesium stearate.

Description

Tablets of light yellow color, round form, with a diameter of 13 mm.

Pharmacological properties:

Flutamid is the nonsteroid drug possessing anti-androgenic action. The mechanism of action includes inhibition of capture of an androgen and/or inhibition of binding of an androgen in kernels of cells of target tissues. Its ability to interfere with effect of testosterone at the cellular level serves as addition to the medicinal "castration" caused by agonists of the luteinizing hormone-a hormone rileasing (LHHR). Target organs of pharmacological action of a flutamid are the prostate and seed bubbles. Flyutamid has no oestrogenic, anti-oestrogenic progestagenny and antigestagenny activity.

Pharmacokinetics. The analysis of plasma, urine and a calla at healthy volunteers after reception of a single dose of a flutamid (200 mg), marked radioactive hyzone, showed that drug is completely and quickly soaked up, being exposed to biotransformation in a liver. The main metabolite found in a blood plasma which maximum concentration is reached in 2 hours is to biologically active α-hydroxylated derivatives (2-oksiflutamid). 94-96% of a α-hydroxylated metabolite contact proteins. From an organism drug is emitted preferential with urine. About 4,2% are allocated with a stake within 72 hours. The elimination half-life of an active metabolite makes about 6 hours of plasma (patients of advanced age have 8 hours after a single dose and 9,6 hours at stable concentration). After multiple dose in a flutamid on 250 mg 3 times a day the stable level of concentration of drug and its active metabolite in plasma was reached after the fourth dose of a flutamid.

Indications to use:

Treatment of the metastasizing prostate cancer when suppression of effect of testosterone is shown:
• in an initiation of treatment in a combination with LGRG agonists;
• as additional treatment of the patients who are already receiving therapy by LGRG agonists;
• at patients with surgical castration;
• treatment of patients who had inefficient other types of hormonal therapy or not transferring similar treatment.

Route of administration and doses:

Flutamid appoint on 1 tablet 3 times a day each 8 hours. In case of achievement of positive effect drug is used before emergence of signs of progressing of a tumoral disease.

In case of the combined therapy with LGRG agonists, both drugs can be appointed at the same time or begin reception of a flutamid three days before the first reception of an agonist of LGRG.

Features of use:

Treatment flutamidy should be carried out under control of level of liver enzymes to blood (the corresponding laboratory analyses should be carried out within the first 4 months once a month and further it is regular).

In case of increase in level of liver enzymes by 2-3 times in comparison with an upper limit of normal values and/or emergence of jaundice in lack of metastasises in a liver use of a flyutamid should be stopped.

Patients have to see immediately a doctor at emergence of the first symptoms of an abnormal liver function, such as skin itch, urine darkening, nausea, vomiting, permanent loss of appetite, yellowing of integuments or whites of the eyes, painful feelings in right hypochondrium or grippodobny symptoms.

Side effects:

at motor-therapy

Most often встечающиеся by-effects - the gynecomastia and/or pains in the field of chest glands sometimes accompanied with a galactorrhoea. These phenomena disappear at the termination of reception or after a dose decline. Disturbances from cardiovascular system arise seldom. Diarrhea, nausea, vomiting, increase in appetite, sleeplessness, fatigue, a tranzitorny abnormal liver function, hepatitis are possible.

The following side effects are in rare instances also noted: decrease in a libido, disturbance from digestive tract, lack of appetite, heartburn, a lock, the pains similar to pains at stomach ulcer, hypostases, hypodermic hemorrhages, shingles, an itch, a lupoid and similar syndrome, a headache, dizziness, weakness, the obscured sight, thirst, thorax pain, concern, a depression. At prolonged treatment suppression of a spermatogenesis is noted.

at treatment in a combination with LGRG agonists

Inflows, decrease a libido, impotence, diarrhea, nausea, vomiting, a gynecomastia are most often possible. Frequency of emergence of these by-effects, except for diarrhea, same, as at motor-therapy by LGRG agonists.

The following side effects can seldom be observed: anemia, a leukopenia, thrombocytopenia, gastrointestinal frustration of not clear etiology, lack of appetite, irritation in the place of an injection and rash, hypostases, symptoms of neuromuscular frustration, jaundice, symptoms of disturbances of urinogenital system, arterial hypertension and by-effects from the central nervous system (drowsiness, a depression, confusion of consciousness, concern, neurosis). Very seldom there are a breath disturbance, hepatitis, the raised photosensitivity.

The following spontaneous side effects of a flutamid are also noted: hemolitic anemia, macrocytic anemia, a methemoglobinemia, reactions of a photosensitivity (including an erythema, an ultseration, bubbles, an epidermal necrolysis), obturatsionny jaundice, hepatic encephalopathy, a liver necrosis. These side effects are usually reversible after the therapy termination.

In rare instances at patients change of coloring of urine from amber to flavovirent is observed.

Interaction with other medicines:

In view of possible strengthening of anticoagulative action at simultaneous use of warfarin and a flutamid, the dose of anticoagulant should be selected under control of a prothrombin time.

Contraindications:

Flutamid is contraindicated to patients with hypersensitivity to a flutamid or to other components of drug.

Flyutamid it is necessary to apply with care at patients with reduced function of a liver, at patients with tendency to fibrinferments and at cardiovascular diseases.

Overdose:

At overdose if the patient in consciousness and without spontaneous vomiting, it is necessary to cause vomiting. It is necessary to apply symptomatic therapy at constant observation of the patient and zhiznennovazhny functions.

Storage conditions:

Store at a temperature below 25 °C, in the place protected from light. To STORE IN the PLACE, UNAVAILABLE TO CHILDREN! Period of validity 3 years. Drug cannot be used after the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Tablets on 250 mg. On 100 tablets in packaging.