Finasteride 5mg

1 coated tablet contains:

active substance:

finasteride 

Excipients:

lactose monohydrate,

calcium hydrogen phosphate dihydrate,

croscarmellose sodium,

sodium dodecyl sulfate,

microcrystalline cellulose,

hyprolose (hydroxypropyl cellulose),

magnesium stearate

Pharmacodynamics

Finasteride is a 4-azasteroid compound that selectively and competitively inhibits 5α-reductase. This nicotinamide adenine dinucleotide phosphate (NADP) -dependent enzyme converts testosterone to dihydrotestosterone.

The drug specifically inhibits type 2 5α-reductase isoenzyme, which leads to a significant decrease in the level of dihydrotestosterone in the prostate gland (> 90%) and in the circulatory system (from 60% to 80%).

Finasteride increases the level of prostate testosterone (approximately 85%) in patients with BPH, this does not affect the growth and morphology of the prostate gland. The drug does not have a pronounced affinity for androgen receptors. Finasteride significantly reduces plasma PSA by 41% - 71% in patients with symptoms of BPH. Nevertheless, the drug does not affect the ratio of the values ​​of unbound and total PSA levels.

The size of the prostate gland decreases under the influence of finasteride due to atrophy and apoptosis. Histological changes due to the action of the drug were observed 6 months after the start of treatment. The glandular elements of prostate tissue are most sensitive to finasteride. The drug reduces detrusor tone in patients with urinary retention caused by BPH.

Pharmacokinetics

Finasteride is well absorbed in the gastrointestinal tract, food slows down the rate of absorption, but does not affect the amount of absorption. The average bioavailability of finasteride is 63% (range 34–71%), based on the ratio of the area under the curve to the intravenous control dose. The maximum concentration of finasteride in plasma is 37 ng / ml (27 - 49%) and is achieved within 1 - 2 hours after administration. The drug accumulates in the body with repeated repeated injections. The establishment of equilibrium concentration occurs after 17 days, the exact time is not known.

About 90% of finasteride circulates in a state bound to plasma proteins. The distribution volume of finasteride is high (76 l in stable condition); the drug crosses the blood-brain barrier and a small amount is found in semen. The drug can be absorbed through the skin in contact with crushed tablets.

Finasteride is metabolized primarily by the liver to form inactive metabolites. The plasma clearance of finasteride is 165 ml / min (70 -279 ml / min) and a half-life of 6 hours. About 39% (32 - 46%) of the dose taken is excreted in the urine as metabolites and 57 (51 - 64%) through the intestines.

The pharmacokinetics of the drug as a whole does not change with an increase in the duration of renal failure. The pharmacokinetics of the drug in conditions of insufficiency of liver function has not been studied.

Treatment of benign prostatic hypertrophy.

The drug Finasteride is not prescribed for women and children.

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

The incidence of side effects is classified according to the recommendations of the World Health Organization: very often - at least 10%; often - at least 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.

On the part of the genitals and mammary gland: very often - impotence, often a decrease in libido, ejaculation disorders, a decrease in ejaculate volume, an increase and tenderness of the mammary glands; infrequently - pain in the testicles; very rarely - secretion from the mammary glands, the formation of nodules in the mammary glands. In most patients, these phenomena were transient in nature.

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

On the part of laboratory indicators: rarely - a decrease in the concentration of PSA.

No clinically significant interaction of finasteride with other drugs was found.
With the combined use of finasteride with propranolol, digoxin, glibenclamide, warfarin, theophylline, angiotensin-converting enzyme inhibitors, paracetamol, acetylsalicylic acid, alpha-adrenergic blockers, beta-adrenergic blocking agents, calcium channel blockers, G-blockers, nitrates, nitrates reductase inhibitors, non-steroidal anti-inflammatory drugs, quinolones and benzodiazepines were not found clinically significant manifestations of drug interactions.

Inside, washed down with liquid and swallowing the whole tablet (tablets cannot be divided and crushed), regardless of the meal.
The recommended dose is 5 mg (1 tablet) 1 time per day.

The duration of treatment is up to 6 months, if necessary, treatment can be continued until a clinical effect is achieved.
In patients with liver failure, dose adjustment is not required.

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

In elderly patients, dose adjustment is not required.

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

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

Finasteride is used in patients with an enlarged prostate gland, the volume of which is more than 40 cm3.

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

Patients who take finasteride should be monitored by a urologist.

Before treatment with finasteride, it is necessary to exclude diseases that stimulate prostate growth and urethral obstruction - prostate cancer, urethral stricture, bladder hypotension, impaired innervation and infectious prostatitis.

Since there is no experience in the treatment of BPH with finasteride in patients with liver failure, treatment of such patients should be carried out with caution, because an increase in plasma concentration of finasteride cannot be ruled out.

Effect on PSA concentration and diagnosis of prostate cancer Before starting treatment with finasteride and periodically during the treatment process, a rectal examination and other methods for diagnosing prostate cancer should be performed. Determination of serum PSA concentration is also used to detect prostate cancer. An initial PSA concentration above 10 ng / ml suggests a wider examination of the patient, including prostate biopsy.

When the PSA concentration is in the range of 4-10 ng / ml, an additional examination of the patient is recommended. The concentration of PSA in patients with prostate cancer and patients without this disease can coincide to a large extent. Therefore, in men with BPH, a normal PSA concentration does not exclude prostate cancer, regardless of treatment with finasteride. An initial PSA concentration below 4 ng / ml also does not preclude 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 PSA concentration in patients with BPH receiving treatment with finasteride does not exclude concomitant prostate cancer.

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

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

Finasteride does not significantly reduce the percentage of free PSA fraction (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, the correction of this indicator is optional.

Influence on laboratory indicators

The serum PSA concentration correlates with the patient’s age and prostate volume, and the prostate volume, in turn, depends on the patient’s age. When determining the concentration of PSA, it should be borne in mind that this indicator decreases in patients taking finasteride.

In most patients, a rapid decrease in PSA concentration is observed during the first months of therapy, after which this indicator stabilizes at a new value, which is usually half of the value obtained before treatment. In this regard, in patients taking finasteride for 6 months or more, the concentration of PSA should be doubled for comparison with normal values ​​in men not taking finasteride.

Influence on the ability to drive vehicles and work with equipment

Caution should be exercised when driving vehicles and working with equipment due to the fact that the use of the drug may cause such an adverse reaction as drowsiness.

Coated tablets