Finasteride-Teva - instructions for use, dose, side effects, contraindications

Excipientslactose monohydrate (200 mesh) 108.0 mg, pregelatinized starch 5.0 mg, sodium lauryl sulfate 0.5 mg, sodium carboxymethyl starch (type A) 10.0 mg, povidone-K30 2.0 mg, microcrystalline cellulose 18.5 mg, magnesium stearate 1.0 mg, film coat Opadrai blue 03G20795 (hypromellose-6sP (E464) 2.50 mg, titanium dioxide (E171) 0.7944 mg, macrogol-6000 0.40 mg, macrogol-400 0.25 mg, indigocarmine lacquer aluminum (E132) 0.0556 mg) .

Description:

Tablets of capsular form, covered with a film coating of blue color, on one side with engraving "FNT 5 "and smooth on the other.The cross-section shows the core of the tablet is white or almost white.

Pharmacotherapeutic group:5-alpha reductase inhibitor

ATX: & nbsp

G.04.C.B.01 Finasteride

Pharmacodynamics:

Finasteride is a synthetic 4-azosteroid, a specific competitive inhibitor of type-5 alpha-reductase, an intracellular enzyme that converts testosterone in a more active androgen - dihydrotestosterone (DHT). Effectively reduces the concentration of DHT in both serum and prostate tissue. Suppression of DHT formation is accompanied by a decrease in the volume of the prostate gland, an increase in the maximum rate of urine flow and a decrease in the severity of symptoms associated with benign prostatic hyperplasia (BPH).

Finasteride does not have an affinity for androgen receptors, it has no effect on the lipid profile, and also on the blood plasma levels of cortisol, estradiol, prolactin, thyroid-stimulating hormone and thyroxine.

In patients with BPH, who took finasteride at a dose of 5 mg / day for 3 years, there was a decrease in serum DHT by approximately 70% and a decrease in prostate volume by approximately 27% compared to baseline values. The concentration of prostate-specific antigen (PSA) decreased by approximately 50% compared with baseline values, suggesting a decrease in the growth of prostatic epithelial cells. The concentration of testosterone in the blood serum increased by about 10-20%.

It has been established that the long-term (more than 4 years) application of finasteride in patients with BPH (with moderate or significant symptoms) reduced the risk of urological complications and surgical interventions (transurethral resection of the prostate or prostatectomy, acute urinary retention requiring catheterization) by 51% and accompanied by a pronounced and persistent decrease in the volume of the prostate gland, as well as a steady increase in the maximum rate of urine flow and improvement in symptoms (Study PLESS).

Pharmacokinetics:

Suction

Absorption of finasteride from the gastrointestinal tract ends 6-8 hours after ingestion.When administered, the bioavailability is about 80%. Eating does not reduce the bioavailability of finasteride. The maximum concentration (C_mOh) in the blood plasma is achieved approximately 2 hours after ingestion.

Distribution

Binding to plasma proteins is 93%. The clearance from plasma is 165 ml / min. The apparent volume of distribution is 76 liters. With the repeated use of finasteride in therapeutic doses for a long time, it is possible to accumulate finasteride in the body in small amounts. With daily intake of finasteride at a dose of 5 mg / day, its concentration in the blood plasma reaches 8-10 ng / ml and persists for a long time. Finasteride penetrates the blood-brain barrier, after 7-10 days it is found in the cerebrospinal fluid, but does not reach significant concentrations.

When taking finasteride at a dose of 5 mg / day, it was also noted that it penetrated the seminal fluid. The concentration of finasteride in the seminal fluid of adult men was 50-100 times lower than its concentration in blood plasma.

Metabolism and excretion

Finasteride is metabolized in the liver.Has no significant effect on the activity of cytochrome P system isoenzymes450. It has been established that two metabolites of finasteride have a less pronounced inhibitory effect on 5-alpha-reductase than finasteride. The half-life (T₁_/₂) finasteride averages 6 hours. It is excreted in the form of metabolites with urine (39%) and with feces (57%).

Pharmacokinetics in special clinical cases

In elderly patients The clearance of finasteride is somewhat reduced. In men older than 70 years, T₁_/₂ finasteride is about 8 hours. However, this is not a reason to reduce the dose of finasteride in elderly patients.

In patients with renal insufficiency varying severity (creatinine clearance (CC) from 9 to 55 ml / min) revealed no differences in the clearance rate of a single dose of finasteride compared with healthy volunteers. The binding to plasma proteins in patients of these groups also did not differ. This is explained by the fact that in patients with renal insufficiency the share of finasteride metabolites, excreted in the urine in normal conditions, is excreted with feces. This is confirmed by an increase in these patients the amount of finasteride metabolites in the feces while reducing their concentration in the urine.In connection with the above, in patients with renal insufficiency, which does not show hemodialysis, correction of the dose of finasteride is not required.

Indications:

Treatment of benign prostatic hyperplasia in order to:

- reducing the size of the enlarged prostate gland, improving the urine flow and reducing the severity of symptoms associated with benign prostatic hyperplasia;

- preventing urological complications (reducing the risk of acute urinary retention) and reducing the need for surgical operations (including transurethral resection of the prostate and prostatectomy).

Contraindications:

Hypersensitivity to finasteride and other components of the drug; obstructive uropathy; lactose intolerance; Lactase deficiency; syndrome of glucose-galactose malabsorption; for use in women; age to 18 years.

Carefully:

Patients with a large volume of residual urine and / or significantly reduced urine flow; liver failure.

Pregnancy and lactation:

Women of reproductive age and pregnant women should avoid contact with crushed or lost integrity tablets of finasteridebecause of the possibility of its penetration into the body and the subsequent risk for the development of the male fetus.

In connection with the ability of inhibitors of 5-alpha-reductase type II inhibit the conversion of testosterone to dihydrotestosterone, these drugs, including finasteride, can cause a pathology of intrauterine formation of the external genital organs in a male fetus.

There is no data on the isolation of finasteride with breast milk. The drug Finasteride-Teva is contraindicated for use during breastfeeding.

Dosing and Administration:

Inside, squeezed liquid and swallowing the tablet whole (tablets can not be divided and crushed), regardless of food intake.

The recommended dose is 5 mg (1 tablet) 1 time per day.

Duration of treatment up to 6 months, if necessary treatment can be continued until the clinical effect is achieved.

In patients with hepatic insufficiency correction of the dose is not required.

In patients with renal insufficiency varying degrees of severity (with a decrease in QC to 9 ml / min), dose adjustment is not required.

In elderly patients correction of the dose is not required.

Side effects:

The incidence of side effects is classified according to the recommendations of the 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%; rarely - not less than 0.01%, but less than 0.1%; very rarely (including isolated cases) - less than 0.01%.

From the nervous system: infrequently - drowsiness.

From the genitals and the breast: very often - impotence, often - decreased-libido, ejaculatory disorders, decreased ejaculate volume, increased and soreness of the mammary glands; infrequently - pain in the testicles; very rarely - the secretion of secretions from the mammary glands, the formation of nodules in the mammary glands. In most patients, these phenomena were transient.

Allergic reactions: often - skin rash; rarely - skin itching, hives, angioedema, edema of the lips and face.

From the laboratory indicators: rarely - decrease in PSA concentration.

Overdose:

Patients received finasteride in a single dose up to 400 mg and in multiple doses up to 80 mg / day for 3 months, with no undesirable effects observed.

There are no recommendations for specific treatment of overdose with finasteride.

Interaction:

There was no clinically significant interaction of finasteride with other drugs.

When combined with finasteride propranolol, digoxin, glibenclamide, warfarin, theophylline, angiotensin-converting enzyme inhibitors, paracetamol; acetylsalicylic acid, alpha-adrenoblockers, beta-blockers, calcium channel blockers, nitrates, diuretics, H blockers₂-gistaminovyh receptors, HMG-CoA-reductase inhibitors, non-steroidal anti-inflammatory drugs, quinolones and benzodiazepines, there were no clinically significant manifestations of drug interaction.

Special instructions:

Finasteride is used in patients with an enlarged prostate gland whose volume is more than 40 cm³.

Patients with a large volume of residual urine and / or significantly reduced urine flow need careful monitoring for obstructive uropathy.

Patients who take finasteride, should be observed in the urologist. Before treatment with finasteride, it is necessary to exclude diseases that stimulate the growth of the prostate and obstruction of the urethra - prostate cancer, urethral stricture, bladder hypotension, violation of its innervation and infectious prostatitis.

Since there is no experience of treating BPH with finasteride in patients with hepatic insufficiency, treatment of such patients should be done with caution, since it is impossible to exclude an increase in the concentration of finasteride in blood plasma.

Effect on the concentration of PSA and diagnosis of prostate cancer

Before the start of treatment with finasteride and periodically during the treatment should be carried out rectal examination and other methods of diagnosis of prostate cancer. The determination of serum PSA concentration is also used to detect prostate cancer. The initial concentration of PSA above 10 ng / ml involves a broader examination of the patient, including prostate biopsy. At a concentration of PSA within 4-10 ng / ml, an additional examination of the patient is recommended. The concentration of PSA in patients with prostate cancer and patients who do not have this disease can coincide to a large extent. Therefore, in men with BPH normal value - the concentration of PSA does not allow to exclude prostate cancer regardless of the treatment with finasteride.The initial concentration of PSA below 4 ng / ml also does not allow to exclude prostate cancer.

Finasteride causes a decrease in serum PSA concentration by approximately 50% in patients with BPH even in the presence of prostate cancer. In this regard, it should be borne in mind that a decrease in the concentration of PSA in patients with BPH receiving treatment with finasteride does not exclude concomitant prostate cancer.

In patients receiving finasteride for 6 months or more, the PSA concentration should be doubled in order to compare with the normal values of this parameter in patients not receiving treatment. This correction preserves the sensitivity and specificity of the PSA analysis and the possibility of detecting prostate cancer.

Any prolonged increase in the concentration of PSA in patients receiving finasteride treatment, requires a thorough examination to determine the cause, including a violation of the mode of application finasteride.

Finasteride does not significantly reduce the percentage of free PSA fractions (free PSA / total PSA ratio). This indicator remains constant even: under the influence of finasteride.If the percentage of free PSA is used to diagnose prostate cancer, correction of the values of this indicator is not necessary.

Impact on laboratory performance

The concentration of PSA in the serum correlates with the age of the patient and the volume of the prostate gland, and the volume of the prostate, in turn, depends on the age of the patient. When determining the concentration of PSA, it should be taken into account that this indicator decreases in patients taking finasteride. In most patients, a rapid decrease in PSA is observed during the first months of therapy, after which the stabilization of this index occurs at a new value, which is usually half of the value obtained before the start of treatment. In this regard, patients receiving finasteride for 6 months or more; It should be doubled the concentration of PSA for comparison with normal values in men who do not take finasteride.

Effect on the ability to drive transp. cf. and fur:

Care should be taken when managing transportation and working with machinery, because the appearance of such an adverse reaction as drowsiness is possible with the use of the drug.

Form release / dosage:

Tablets, film-coated, 5 mg.

Packaging:

For 7 tablets in a blister of PVC / PVDC film and aluminum foil.

4 blisters together with instructions for use in a cardboard box.

Or 10 tablets per blister of PVC / PVDC film and aluminum foil.

2, 3, 6 or 10 blisters together with instructions for use in a cardboard box.

Storage conditions:

At a temperature of no higher than 30 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-001187

Date of registration:11.11.2011

Date of cancellation:2016-11-11

The owner of the registration certificate:Teva Pharmaceutical Enterprises Co., Ltd.Teva Pharmaceutical Enterprises Co., Ltd. Israel

Manufacturer: & nbsp

TEVA Pharmaceutical Works Private, Ltd. Co. Hungary

Representation: & nbspTeva Teva Israel

Information update date: & nbsp24.09.2015

Illustrated instructions

Instructions

Finasteride-Teva (Finasteride-Teva)