Finasteride-OBL, pills 5 mg 30 pcs.

Composition

1 coated tablet contains:

Active ingredient:

finasteride 5 mg,

excipients:

lactose monohydrate,

calcium hydrophosphate dihydrate,

sodium croscarmellose,

sodium dodecyl sulfate,

microcrystalline cellulose,

hyprolose a (hydroxypropylcellulose),

magnesium stearate

Pharmacological action

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 isoenzyme 5α-reductase type 2, 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, but it does not affect the growth and morphology of the prostate. The drug does not have a pronounced affinity for androgen receptors. Finasteride significantly reduces plasma PSA levels by 41% – 71% in patients with BPH symptoms. However, the drug does not affect the ratio 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 caused by the drug were observed 6 months after the start of treatment. Glandular elements of prostate tissues 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 volume of absorption. The average bioavailability of finasteride is 63% (within 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 reached within 1-2 hours after administration. The drug accumulates in the body with repeated repeated injections. The establishment of an equilibrium concentration occurs after 17 days, the exact time is not known.

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

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

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 hepatic insufficiency have not been studied.

Indications

Treatment of benign prostatic hypertrophy.

Use during pregnancy and lactation

The drug Finasteride is not prescribed for women and children.

Contraindications

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

Side effects

the incidence of side effects is classified according to the recommendations of the world health organization: very often – at least 10%; often – not less than 1% but < 10%; infrequently – no more than 0.1% but < 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: rarely-drowsiness.

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

Allergic reactions: often – skin rash; rarely-pruritus, urticaria, angioedema of the lips and face.

From the side of laboratory parameters: rarely-a decrease in PSA concentration.

Interaction

There was no clinically significant interaction of finasteride with other drugs. When finasteride is used in combination with propranolol, digoxin, glibenclamide, warfarin, theophylline, angiotensin-converting enzyme inhibitors, paracetamol, acetylsalicylic acid, alpha-blockers, beta-blockers, calcium channel blockers, nitrates, diuretics, H2-histamine receptor blockers, HMG-CoA reductase inhibitors, nonsteroidal anti-inflammatory drugs, quinolones, and benzodiazepines did not show clinically significant drug interactions.

How to take, course of administration and dosage

Inside, wash it down with liquid and swallow the whole tablet (tablets can not be divided and crushed), regardless of food intake. The recommended dose is 5 mg (1 tablet) once a day.

The duration of treatment is up to 6 months, if necessary, treatment can be continued until a clinical effect is achieved. No dose adjustment is required in patients with hepatic insufficiency.

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

No dose adjustment is required in elderly patients.

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 adverse effects observed.

There are no recommendations for specific treatment of finasteride overdose.

Special instructions

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

Patients with large residual urine volumes and/or significantly reduced urine flow should be closely monitored for obstructive uropathy.

Patients taking 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, hypotension of the bladder, violation of its innervation and infectious prostatitis.

Since there is no experience in treating BPH with finasteride in patients with hepatic insufficiency, treatment of such patients should be carried out with caution, since an increase in the concentration of finasteride in blood plasma cannot be excluded.

Effects on PSA concentration and prostate cancer diagnosis Rectal examination and other methods of prostate cancer diagnosis should be performed before starting treatment with finasteride and periodically during treatment. Determination of serum PSA concentrations is also used to detect prostate cancer. A baseline PSA concentration above 10 ng / ml suggests a broader examination of the patient, including a prostate biopsy.

If 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 who do not have this disease may coincide to a large extent. Therefore, in men with BPH, a normal PSA concentration does not exclude prostate cancer regardless of finasteride treatment. The initial PSA concentration below 4 ng / ml also does not exclude prostate cancer.

Finasteride causes a decrease in serum PSA concentrations of 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 treated with finasteride does not exclude concomitant prostate cancer.

In patients receiving finasteride for 6 months or more, the PSA concentration index 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 ability to detect prostate cancer.

Any prolonged increase in PSA concentrations in patients receiving finasteride treatment requires a thorough investigation to determine the cause, including violation 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, correction of the values of this indicator is optional.

Impact on laboratory parameters

The concentration of PSA in the blood serum correlates with the patient’s age and prostate volume, and the prostate volume, in turn, depends on the patient’s age. When determining the PSA concentration, it should be taken into account 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 starting treatment.Therefore, in patients taking finasteride for 6 months or more, the PSA concentration should be doubled to compare with normal values in men who do not take finasteride.

Influence on the ability to drive vehicles and work with machinery

Care should be taken when driving vehicles and working with equipment due to the fact that when using the drug, an adverse reaction such as drowsiness may occur.

Form of production

Film-coated tablets

Storage conditions

Store in a dry place, protected from light, at a temperature not exceeding 25 °C

Shelf life

2 years

Active ingredient

Finasteride

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Prostatitis, Prostatic Hyperplasia

Weight

Weight: 16 gr.