Finasterid - Teva

General characteristics. Structure:

Active ingredient финастерид 5,0 mg;
excipients: lactoses monohydrate (200 meshes) of 108,0 mg, starch of prezhelatinizirovanny 5,0 mg, sodium lauryl sulfate of 0,5 mg, sodium carboxymethylstarch (type A) of 10,0 mg, povidon-KZO 2,0 mg, cellulose of microcrystallic 18,5 mg, magnesium stearate of 1,0 mg, film cover of Opadray blue 03G20795 (gipromelloza-bsr (E464) of 2,50 mg, titanium dioxide (E171) of 0,7944 mg, macrogoal-6000 of 0,40 mg, macrogoal-400 of 0,25 mg, indigo carmine varnish aluminum (E132) of 0,0556 mg).

Description
Tablets of a kapsulovidny form, film coated blue color, on one party with an engraving of "FNT 5" and smooth with another. On cross section the kernel of a tablet of white or almost white color is visible.

Pharmacological properties:

Pharmacodynamics. Finasterid - a synthetic 4 azosteroid, a specific competitive inhibitor 5 - type alpha reductases II - a desmoenzyme which turns testosterone into more active androgen - dihydrotestosterone (DGT). Effectively reduces concentration of DGT both in blood serum, and in prostate gland tissue. Suppression of formation of DGT is followed by reduction of volume of a prostate, increase in the maximum speed of current of urine and decrease in expressiveness of the symptoms connected with the benign hyperplasia of a prostate (BHP).
Finasterid has no affinity to receptors of androgens, does not exert impact on a lipidic profile, and also on contents in a blood plasma of cortisol, oestradiol, prolactin, thyritropic hormone and thyroxine.
At patients with DGPZh which accepted финастерид in a dose 5 mg/days within 3 years decrease in concentration of DGT in blood serum approximately for 70% and reduction of volume of a prostate approximately for 27% in comparison with reference values was observed. Concentration of the prostates specific antigens (PSA) decreased approximately by 50% in comparison with reference values that assumes reduction of growth of epithelial cells of a prostate. Concentration of testosterone in blood serum increased approximately by 10-20%.
It is established that long (more than 4 years) use of a finasterid for patients with DGPZh (at moderately or much the expressed disease symptoms) reduced risk of development of urological complications and surgical interventions (a transurethral resection of a prostate or a prostatectomy; the acute ischuria demanding catheterization) for 51% was also followed by the expressed and permanent reduction of volume of a prostate, and also permanent increase in the maximum speed of current of urine and improvement of symptomatology (Research PLESS).

Pharmacokinetics. Absorption
Absorption of a finasterid from digestive tract comes to an end in 6-8 h after intake. At intake bioavailability makes about 80%. Meal does not reduce bioavailability of a finasterid. The maximum concentration (Cmax) in a blood plasma is reached approximately in 2 h after intake.
Distribution
Linkng with proteins of plasma makes 93%. Clearance from plasma of 165 ml/min. The seeming volume of distribution makes 76 l. At repeated use of a finasterid in therapeutic doses accumulation of a finasterid in an organism in small quantities is possible for a long time. At daily intake of a finasterid in a dose of 5 mg/days its concentration in a blood plasma reaches 8-10 ng/ml and remains for a long time. Finasterid gets through a blood-brain barrier, in 7-10 days it is found in cerebrospinal fluid, however does not reach significant concentration.
At reception of a finasterid in a dose of 5 mg/days its penetration into semen was also noted. At the same time concentration of a finasterid in semen of adult men was 50-100 times lower than its concentration in a blood plasma.
Metabolism and removal
Finasterid is metabolized in a liver. Has no noticeable effect on activity of isoenzymes of system of P450 cytochrome. It is established that two metabolites of a finasterid possess less expressed inhibiting effect on 5 - alpha reductase, than финастерид. The elimination half-life (T1/2) of a finasterid averages 6 h. It is removed in the form of metabolites with urine (39%) and with a stake (57%).
Pharmacokinetics in special clinical cases
At patients of advanced age the clearance of a finasterid decreases a little. At men 70 years of T1/2 of a finasterid are more senior makes about 8 h. However it is not the basis for reduction of a dose of a finasterid at patients of advanced age.
At patients with a renal failure of varying severity (the clearance of creatinine (CC) from 9 to 55 ml/min.) distinctions in the speed of removal of a single dose of a finasterid in comparison with healthy volunteers are not revealed. Linkng with proteins of plasma at patients of these groups also did not differ. This results from the fact that patients with a renal failure have a share of metabolites of a finasterid in normal conditions excreted with urine is removed with a stake. It is confirmed by increase at these patients of quantity of metabolites of a finasterid in Calais at simultaneous decrease in their concentration in urine. Due to stated, with a renal failure to whom the hemodialysis is not shown dose adjustment of a finasterid is not required from patients.

Indications to use:

Treatment of a benign hyperplasia of a prostate on purpose:
- reduction of the sizes of the increased prostate, improvement of current of urine and reduction of expressiveness of the symptoms connected with a benign hyperplasia of a prostate;
- preventions of urological complications (decrease in risk of an acute ischuria) and decrease in need of carrying out surgeries (including transurethral prostatectomy and prostatectomy).

Route of administration and doses:

Inside, washing down with liquid and swallowing a tablet entirely (tablets cannot be divided and made small), irrespective of meal.
The recommended dose makes 5 mg (1 tablet) once a day.
Treatment duration up to 6 months, if necessary treatment can be continued before achievement of clinical effect.
With a liver failure dose adjustment is not required from patients.
With a renal failure of varying severity (at decrease in KK to 9 ml/min.) dose adjustment is not required from patients.
Dose adjustment is not required from patients of advanced age.

Features of use:

Finasterid is applied at patients with the increased prostate which volume more than 40 cm3.
Patients with the large volume of a residual urine and/or essential reduced current of urine need careful observation regarding an obstructive uropathy.
Patients who accept финастерид have to be observed at the urologist.
Before treatment finasteridy it is necessary to exclude the diseases stimulating growth of a prostate and obstruction of an urethra - a prostate cancer, an urethra stricture, bladder hypotonia, disturbance of its innervation and infectious prostatitis.
As there is no experience of treatment of DGPZh finasteridy at patients with a liver failure, treatment of such patients has to be carried out with care since it is impossible to exclude increases in concentration of a finasterid in a blood plasma.
Influence on concentration of the DOG and diagnosis of a prostate cancer Before an initiation of treatment finasteridy and periodically in the course of treatment it is necessary to conduct a rectal research and other diagnostic methods of a prostate cancer. Definition of serumal concentration of the DOG is also used for detection of a prostate cancer. Initial concentration of the DOG higher than 10 ng/ml assumes carrying out broader inspection of the patient, including a prostate biopsy. At concentration of the DOG within 4-10 ng/ml additional inspection of the patient is recommended. Concentration of the DOG at patients a prostate cancer and the patients who do not have this disease can match substantially. Therefore, at men with DGPZh normal value of concentration of the DOG does not allow to exclude a prostate cancer irrespective of treatment finasteridy. Initial concentration of the DOG lower than 4 ng/ml also does not allow to exclude a prostate cancer.
Finasterid causes reduction of serumal concentration of the DOG approximately for 50% in patients with DGPZh even in the presence of a prostate cancer. In this regard it must be kept in mind that decrease in concentration of the DOG at patients from DGPZh receiving treatment finasteridy does not exclude the accompanying prostate cancer. At the patients receiving финастерид within 6 months and more the indicator of concentration of the DOG has to be doubled for comparison with normal values of this indicator at the patients who are not receiving treatment. This correction keeps sensitivity and specificity of the analysis of an indicator of the DOG and a possibility of detection of a prostate cancer.
Any long increase in concentration of the DOG demands careful inspection for clarification of the reason from the patients receiving treatment finasteridy, including disturbance of the mode of use of a finasterid.
Finasterid significantly does not reduce percent of the DOG free fraction (a ratio free the DOG / the general of the DOG). This indicator remains to constants even under the influence of a finasterid. If for diagnosis of a prostate cancer the percent of a free DOG is used, correction of values of this indicator is optional.
Influence on laboratory indicators
Concentration of the DOG in blood serum correlates the patient and prostate volume with age, and prostate volume, in turn, depends on age of the patient. When determining concentration of the DOG it is necessary to consider that this indicator decreases at the patients accepting финастерид. At most of patients bystry decrease in concentration of the DOG is observed within the first months of therapy then there is a stabilization of this indicator on new value which usually makes a half from the value received prior to treatment. In this regard at the patients accepting финастерид within 6 and more months it is necessary to double concentration of the DOG for comparison with normal values at the men who are not accepting финастерид.

Influence on ability to management of transport and work with the equipment
It is necessary to be careful at management of transport and work with the equipment because at use of drug emergence of such side reaction as drowsiness is possible.

Side effects:

Frequency of development of side effects is classified according to recommendations of World Health Organization: very often - not less than 10%; often - not less than 1%, but less than 10%; infrequently - not less than 0,1%, but less than 1%; seldom - not less than 0,01%, but less than 0,1%; very seldom (including isolated cases) - less than 0,01%.
From a nervous system: infrequently - drowsiness.
From generative organs and a mammary gland: very often - impotence, it is frequent - decrease in a libido, disturbance of an ejaculation, reduction of volume of an ejaculate, increase and morbidity of chest glands; infrequently - pain in testicles; very seldom - allocation of a secret from mammary glands, nodulation in mammary glands. At most of patients these phenomena had tranzitorny character.
Allergic reactions: often - skin rash; seldom - a skin itch, a small tortoiseshell, a Quincke's disease of lips and the person.
From laboratory indicators: seldom - decrease in concentration of the DOG.

Interaction with other medicines:

Clinically significant interaction of a finasterid with other drugs is not revealed.
At the combined use of a finasterid with propranolol, digoxin, glibenclamide, warfarin, theophylline, an angiotensin-converting enzyme inhibitors, paracetamol, acetylsalicylic acid, alpha adrenoblockers, beta adrenoblockers, blockers of calcium channels, nitrates, diuretics, blockers of H2-histamine receptors, GMG-KOA-reduktazy inhibitors, non-steroidal anti-inflammatory drugs, hinolona and benzodiazepines are not revealed clinically significant manifestations of medicinal interaction.

Contraindications:

Hypersensitivity to a finasterid and other components of drug; obstructive uropathy; lactose intolerance; insufficiency of lactase; syndrome of glyukozo-galaktozny malabsorption; for use for women; age up to 18 years.

With care
Patients with the large volume of a residual urine and/or essential reduced current of urine; liver failure.

Use during pregnancy and during breastfeeding
Women of reproductive age and pregnant women have to avoid contact with the tablets of a finasterid crushed or lost integrity because of a possibility of its penetration into an organism and the subsequent risk for male fetation.
In connection with ability of inhibitors 5 - alpha reductases like II to suppress transformation of testosterone into dihydrotestosterone these drugs, including финастерид, can cause pathology of pre-natal formation of external genitals in a male fruit.
There are no data on allocation of a finasterid with breast milk. Drug Finasterid - Teva is contraindicated for use during breastfeeding.

Overdose:

Patients received финастерид in a single dose up to 400 mg and in repeated doses to 80 mg/days within 3 months, at the same time any undesirable effects were not observed.
Recommendations about specific treatment of overdose finasteridy are absent.

Storage conditions:

At a temperature not above 30 °C. To store in the place, unavailable to children. Period of validity 2 years. Not to use after the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Tablets, film coated, 5 mg.
On 7 tablets in the blister from a film of PVH/PVDH and aluminum foil.
4 blisters together with the application instruction in a cardboard pack.
Or on 10 tablets in the blister from a film of PVH/PVDH and aluminum foil.
2, 3, 6 or 10 blisters together with the application instruction in a cardboard pack.