Flutafarm

General characteristics. Structure:

Active ingredient: флутамид;

1 tablet contains a flutamid in terms of 100% substance – 250 mg (0,25 g);

excipients: potato starch, lactoses monohydrate, silicon dioxide colloid anhydrous, calcium stearate.

Pharmacological properties:

Pharmacodynamics. The Flutafarm is nonsteroid drug with anti-androgenic action. It is capable to block cellular receptors of androgens, imitating effect of an orkhiektomiya and interfering with testicular and adrenal androgens to stimulate growth of malignant tumors (adenocarcinoma) of a prostate in fabrics, sensitive to androgens. It leads to braking of proliferation of epithelial tumor cells and promotes reduction of the sizes and density of the prostate and metastasises in fabrics at patients with cancer of a prostate.

At women with the hyper androgenic states which are followed by infertility and disturbances of an ovarian and menstrual cycle (for example, a syndrome of scleropolycystic ovaries), the Flutafarm blocks pathogenic influence of endogenous androgens on ovaries and other reproductive organs, and also on gipotalamo-pituitary system. Thanks to it at patients symptoms of a giperandrogeniya (hirsutism) are weakened, periods renew, the folliculogenesis and a menstrual cycle improves that probably leads to recovery of fertile potential at a part of patients.

Pharmacokinetics. Flutamid is well soaked up from a digestive tract. The maximum concentration in blood is observed in 2 hours after oral administration. It is quickly metabolized with formation of an active metabolite – a 2-gidroksiflutamid and other substances. The elimination half-life of an active metabolite makes 5 – 6 hours. It Eliminirutsya generally with urine. In 2 days 91%, in 3 days – 98% of the entered dose are brought out of an organism.

Pharmaceutical characteristics

Main physical and chemical properties: tablets of light yellow color, with a flat surface, risky and a facet.

Indications to use:

Treatment of the locally-spread or metastasizing prostate cancer as means of monotherapy (with or without orkhiektomiya) or in a combination with agonists of the luteinizing hormone of rileasing-hormone (LHRH) at patients to whom did not appoint in general any  treatment earlier, or treatment of patients who do not react or at whom resistance to hormonal therapy developed.

As a part of complex therapy of locally limited prostate cancer of a stage of B2-C2 (T2b-T4) for reduction of volume of a tumor, strengthening of control over a tumor and increase in the period between exacerbations of a disease.

Treatment of women with a functional giperandrogeniya which is followed by disturbances of an ovarian and menstrual cycle, a hirsutism, a syndrome of scleropolycystic ovaries and infertility.

Route of administration and doses:

To appoint Flutafarm the patient with cancer of a prostate as monotherapy (after or without orkhiektomiya), or in a combination with LGRG agonists on 1 tablet (250 mg) 3 times a day each 8 hours. In case of a combination therapy with LGRG agonists it is possible to appoint both drugs at the same time or reception of Flutafarm is begun in 24 hours prior to the first reception of an agonist of LGRG.

In case of use of radiation therapy to appoint Flutafarm in 8 weeks prior to its beginning and to continue administration of drug throughout all course of radiation therapy.

To women with hyper androgenic states to appoint Flutafarm inside on 1/2 tablets (125 mg) 3 times a day within 3 – 6 months. To accept in time or after food. Use of non-hormonal contraceptives, in particular, barrier is obligatory.

Features of use:

Patients have to be under constant observation of the doctor. Special attention should be paid to effect of drug on function of a liver and a spermatogenesis at patients to whom the orchidectomy was not carried out (surgical or medicamentous).

Treatment by drug should not be begun if levels of hepatic transaminases in blood serum by 2-3 times exceed the upper bound of norm. Control of function of a liver should be exercised during the entire period of treatment by drug. Levels of transaminases in blood serum need to be determined prior to therapy flutamidy, monthly within the first 4 months of administration of drug, periodically further and at the first symptoms of dysfunction of a liver (for example, an itch, urine darkening, nausea, vomiting, increased fatigue, anorexia, jaundice, pains in right hypochondrium or unclear grippopodobny symptoms). At emergence of jaundice or increase in activity of hepatic transaminases 2-3 times higher norms (in the absence of the metastasises in a liver confirmed with a biopsy) reception of a flutamid should be stopped immediately and to carefully control function of a liver before clarification of a situation.

Patients should see immediately a doctor at emergence of the first symptoms of an abnormal liver function, such as skin itch, urine darkening, nausea, vomiting, steady anorexia, yellowing of scleras and skin, morbidity in right hypochondrium and grippopodobny symptoms.

Damages of a liver are usually reversible after the therapy termination, and at some patients − even after a dose decline.

Flutamid is brought generally by kidneys therefore the dosage of drug can demand correction from patients with a renal failure.

As at treatment flutamidy levels of testosterone and oestradiol in a blood plasma increase, the liquid delay in body tissues is possible. Therefore флутамид patients should appoint with care with heart diseases. Besides, growth of level of oestradiol can increase risk of development of a thromboembolism.

At patients without orchidectomy who a long time are treated flutamidy it is necessary to define quantity of spermatozoa periodically.

At patients with latent or actual deficit of glyukozo-6-phosphate the methemoglobinemia can develop. In case of cyanosis, a methemoglobinemia it is necessary to consider a possible factor of exceeding of a dosage.

Flutamid contains lactose therefore patients with rare hereditary forms of intolerance of a galactose, insufficiency of lactase or a syndrome glyukozo- galaktozny       malabsorption should not use drug.

At a combination therapy Flutafarm and the LGRG-agonist possible side effects of each of drugs have to be taken into account.

Patients should be informed on what флутамид and the medicines intended for medical castration needs to be applied in a combination and it is impossible to stop their reception or to change doses without preliminary consultation with the doctor.

Before Flutafarm use women need to exclude a giperandrogeniya of an organic origin (a tumor of ovaries and bark of adrenal glands).

During treatment it is not necessary to take alcohol.

Ability to influence speed of response at control of motor transport or work with other mechanisms

 

Individual reaction of the patient to drug will not be found out yet, it is necessary to abstain from control of motor transport or other mechanisms, considering that during treatment flutamidy were observed the increased fatigue, sometimes dizziness, drowsiness and visual disturbances.

Side effects:

At monotherapy.

Reproductive system: the gynecomastia and/or pain in the field of chest glands which sometimes is followed by a galactorrhoea. The specified reactions disappear after the termination of treatment or reduction of a dose of drug. Frequency of cases of a gynecomastia considerably decreases at simultaneous use of agonists of LGRG. Decrease in a libido, decrease in quantity of spermatozoa.

Infections and invasions: the surrounding herpes.

Blood and lymphatic system: hypostases, ecchymomas, lymphostasis.

Immune system: volchanochnopodobny syndrome.

Mental disturbances: depression, concern, agitation, alarm.

Nervous system: sleeplessness, headache, dizziness.

Organs of sight: sight illegibility.

Respiratory system: диспноэ, cough.

Digestive tract: diarrhea, nausea, vomiting, increase in appetite, dysfunction of digestive tract, pain in a stomach, yazvennopodobny pain, heartburn, a lock, anorexia, thirst.

Gepatobiliarny system: increase in activity of liver enzymes, tranzitorny disorders of function of a liver, jaundice, hepatitis.

Skin and hypodermic cellulose: itch, rash.

General disturbances: increased fatigue, indisposition, weakness, fever, thorax pain.

Disturbances from cardiovascular system arise much less often in comparison with diethylstulbestrole use.

At a combination therapy.

Reproductive system: decrease in a libido, impotence, inflows, gynecomastia.

Benign and malignant tumors: new growths in chest glands at men.

Alimentary system: diarrhea, nausea, vomiting, nonspecific gastrointestinal frustration, pains in a stomach.

Blood and lymphatic system: anemia, leukopenia, thrombocytopenia, hypostases, hemolitic anemia, macrocytic anemia, methemoglobinemia, sulfhemoglobinemia. The thromboembolism is possible.

Metabolic frustration, disturbances of a trophicity: anorexia, hyperglycemia, diabetes mellitus aggravation.

Mental disturbances: depression, alarm, concern, neurosis.

Nervous system: drowsiness, confusion of consciousness, irritability.

Cardiovascular system: arterial hypertension. Separate cases of thrombophlebitis, pulmonary embolism and myocardial infarction were noted.

Respiratory system: asthma, intersticial damages of lungs.

Gepatobiliarny system: jaundice, hepatitis, cholestatic jaundice, a gepatoentsefalopatiya, гепатонекроз, abnormal liver functions, usually reversible after the end of therapy; it was reported about separate lethal cases owing to severe damage of a liver.

Skin and hypodermic cellulose: rashes, reactions of a photosensitization, including an erythema, formation of ulcers, violent rashes, an epidermal necrolysis.

Musculoskeletal system and connecting fabric: arthralgias, mialgiya, neuromuscular symptoms (including muscular weakness, paresthesias, spasms).

Urinary system: a dysuria, change of frequency of an urination, urine discoloration to amber and flavovirent that can be connected with flutamidy and/or its metabolites.

General disturbances: feeling of heat.

Laboratory indicators: increase in levels of liver enzymes, bilirubin, residual nitrogen of urea in blood serum, increase in level of creatinine in blood serum.

Besides, such by-effects were observed during drug use: hemolitic anemia, macrocytic anemia, a methemoglobinemia, a sulfhemoglobinemia, photosensitivity reactions (including an erythema, ulceration, violent rashes and an epidermal necrolysis) and urine discolorations to amber and flavovirent that can be connected with flutamidy and/or its metabolites. Also cholestatic jaundice, hepatic encephalopathy, a liver necrosis can be observed. Abnormal liver functions, usually reversible, after the therapy termination; nevertheless, there are messages on a lethal case owing to the severe damage of a liver connected using a flutamid.

It was reported about extremely isolated cases of development of a hyperglycemia and deterioration in a current of a diabetes mellitus.

Changes of results of laboratory analyses which included an abnormal liver function, increase in level of an urea nitrogen of blood and isolated cases of increase in level of creatinine in blood serum were noted.

Interaction with other medicines:

At patients, it is long receiving warfarin, after the beginning of monotherapy flutamidy increase in a prothrombin time is observed. Therefore at combined use of Flutafarm and warfarin careful control of a prothrombin time and, perhaps, correction of doses of anticoagulant is necessary.

Flutamid can slow down metabolism of corticosteroids.

It is necessary to avoid the accompanying use of a flutamid with potentially hepatotoxic drugs.

At use of a flutamid along with theophylline increase in concentration of theophylline in a blood plasma is possible.

It is necessary to avoid excessive alcohol intake during treatment flutamidy.

Contraindications:

Hypersensitivity to a flutamid or to other components of drug. For women additional contraindications for reception of Flutafarm are the giperandrogeniya of an organic origin (a tumor of ovaries and bark of adrenal glands), the Heavy liver failure (the basic level of liver enzymes should be estimated prior to treatment).

Overdose:

The single dose of a flutamid which would cause symptoms of overdose or posed a threat for life, is not established.

At overdose dialysis is inefficient, considering high extent of linkng of a flutamid with proteins of a blood plasma.

As well as at treatment of overdose of any medicine, it is necessary to consider a possibility of a concomitant use of several drugs. In case of overdose if there is no spontaneous vomiting, it is necessary to cause vomiting. The gastric lavage can be required.

The standard supporting actions at constant surveillance over the patient and over the vital functions are shown.

Use during pregnancy or feeding by a breast

At drug use women should pay special attention to prevention of pregnancy by means of non-hormonal, in particular, barrier contraceptives. In case of a positive take of the test for pregnancy administration of drug needs to be stopped immediately. The sexual relations with the purpose of approach of desired pregnancy can be renewed not earlier than in 48 hours after the last reception of Flutafarm.

Children

Not to use drug for treatment of children.

Storage conditions:

Period of validity 3 years. Not to use drug after the termination of the period of validity specified on packaging. In the place protected from light at a temperature not above 25 °C. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

On 10 tablets in the blister, on 5 blisters in a pack.