Finasteride

Package leaflet (information for patients)

Tradename
Finasteride

Dosage form
Tablets 5 mg.

Description
Round, flat, beveled to the edge white tablets with an imprint in the form of the brand name "V" on one side.

Structure
Active ingredient: Finasteride 5 mg.
Excipients: microcrystalline cellulose 102, calcium stearate, aerosil ® 200 (hydrophilic pyrogenic silicon dioxide).

Pharmacotherapeutic group
Antiestrogens

Pharmacological properties
Finasteride is a synthetic 4-azasteroid compound, a competitive and specific inhibitor of steroid 5-alpha reductase, an intracellular enzyme that converts testosterone into the active androgen 5-dihydrotestosterone. The growth of prostate tissue and the development of benign hyperplasia are due to the conversion of testosterone to dihydrotestosterone in the cells of the prostate gland. Under the influence of the drug, a significant decrease in the concentration of dihydrosterone occurs both in the blood plasma and in the gland tissue. Finastirid does not bind to androgen receptors. As a result of the use of the drug, the size of the prostate gland decreases, the severity of symptoms associated with prostatic hyperplasia decreases. The drug does not affect the concentration of plasma lipids, as well as the content of cortisol, estradiol, prolactin, thyroid-stimulating hormone, thyroxine in the blood plasma. Absorption and distribution: after taking the drug inside, finasteride is rapidly absorbed from the gastrointestinal tract. Bioavailability is about 80% and does not depend on food intake. The maximum plasma concentration is reached within 1-2 hours after ingestion. Plasma protein binding is about 90%. Metabolism and excretion: finasteride is metabolized by the liver and excreted as metabolites in the urine and feces. the half-life of the drug in patients over 60 years old is 6 hours, in patients over 70 years old it can be extended up to 8 hours.

Indications for use
Adjuvant therapy of early breast cancer with positive hormone receptors in postmenopausal women, including after adjuvant therapy with tamoxifen for 2-3 years. First line therapy for locally advanced or metastatic breast cancer, with positive or unknown hormone receptors in postmenopausal women. Second-line therapy for advanced breast cancer that progresses after tamoxifen treatment in postmenopausal women

Method of administration and dosage
It is indicated for benign prostatic hyperplasia (to reduce the size of the prostate gland, increase the maximum flow rate of urine and reduce symptoms associated with hyperplasia, reduce the risk of acute urinary retention and the associated likelihood of surgery.

Side effects
Allergic reactions, gynecomastia, breast tenderness, impotence, decreased libido and decreased ejaculate volume. The frequency of side effects does not exceed 3-4% and decreases during treatment. In some cases, there was an increase in the concentration of luteinizing and follicle-stimulating hormones and testosterone by approximately 10%, but these indicators remained within the normal range.

Contraindication
Hypersensitivity to finasteride and other components of the drug, prostate cancer, urinary tract obstruction, childhood. With caution - impaired liver function.

Overdose
Cases of simultaneous overdose of finasteride and tamsulosin have not been described. There are no clinical data on tamsulosin overdose. Theoretically, an acute overdose of tamsulosin can cause arterial hypotension, which can lead to cardiovascular disorders. To restore blood pressure and heart rate, the patient must be laid down; if necessary, plasma-substituting drugs and, depending on the patient's condition, vasopressor drugs should be used. It is recommended to monitor kidney function. Dialysis is not indicated due to the significant binding of tamsulosin to plasma proteins. To decrease absorption of the drug, it is advisable to induce vomiting. Gastric lavage after taking a large amount of the drug should be carried out together with the appointment of activated charcoal and an osmotic laxative (for example, sodium sulfate). Overdose of finasteride : the use of a single dose of finasteride 400 mg and repeated administration in a dose of up to 80 mg / day for 3 months did not reveal any adverse reactions. In case of an overdose, specific treatment is not required.

Precautions
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 seen by a urologist. Before treatment with finasteride, it is necessary to exclude diseases that stimulate the growth of the prostate gland and obstruction of the urethra - prostate cancer, urethral stricture, hypotension of the bladder, violation of its innervation and infectious prostatitis. Because of the lack of experience in treating BPH with finasteride in patients with hepatic impairment, these patients should be treated with caution. an increase in the concentration of finasteride in blood plasma cannot be ruled out. Influence on PSA concentration and diagnosis of prostate cancer Before starting treatment with finasteride and periodically during treatment, rectal examination and other methods of diagnosing prostate cancer should be performed. Determination of serum PSA concentration is also used to detect prostate cancer. A baseline PSA concentration above 10 ng / ml suggests a more extensive evaluation of the patient, including a prostate biopsy. When PSA concentration is in the range of 4-10 ng / ml, additional patient examination is recommended. PSA concentrations in prostate cancer patients and those without prostate cancer may be largely the same. 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 exclude prostate cancer. Finasteride causes a decrease in serum PSA concentration of about 50% in patients with BPH, even with 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. 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 ability to detect prostate cancer. Any prolonged increase in PSA concentration in patients receiving finasteride treatment requires careful examination to determine the cause, including a 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 not necessary. Impact on laboratory parameters Serum PSA concentration correlates with patient age and prostate volume, and prostate volume, in turn, depends on patient's age. When determining the PSA concentration, 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 starting treatment. In this regard, 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 and work with equipment Care should be taken when driving and working with equipment due to the fact that when using the drug, such an adverse reaction as drowsiness may occur

Interaction with other medicinal products
There was no clinically significant interaction of finasteride with other drugs. The combined use of finasteride with propranolol, digoxin, glibenclamide, warfarin, theophylline, angiotensin converting enzyme inhibitors, acetaminophen, acetylsalicylic acid, alpha- blockers, beta-blockers, calcium channel blockers, nitrates, diuretics, blockers of histamine H2-receptors GMG CoA - reductase inhibitors, non-steroidal anti-inflammatory drugs, quinolones and benzodiazepines, no clinically significant manifestations of drug interactions were found.

Special instructions
Before starting treatment, it is necessary to exclude diseases that can simulate benign prostatic hyperplasia, such as infectious prostatitis, prostate cancer, urethral stricture, hypotension of the bladder and a number of changes in the urinary system that occur in some diseases of the nervous system. Since when using finasteride, there is a decrease in prostate-specific antigen (by 41% and 48%, respectively, by 6 and 12 months from the start of therapy), periodically during the course of therapy it is necessary to examine patients to exclude prostate cancer from them. Women of childbearing age and pregnant women should avoid contact with crushed tablets of Finasteride, because the ability of the drug to suppress the conversion of testosterone to dihydrotestosterone can cause impaired development of the genital organs in the male fetus. Finasteride tablets are film-coated and during normal handling, if they are not ground into powder or their integrity is not broken, contact with the active substance is excluded.

Pregnancy and elbowing
Contraindicated in pregnancy. Breastfeeding should be discontinued during treatment

Influence on the ability to drive vehicles and work with mechanisms
Does not affect

Storage conditions
Store in a dry, dark place at a temperature not exceeding 25 ° C, out of the reach of children.

Shelf life
3 years. Do not use after the expiration date printed on the package.

Vacation conditions
On prescription.

Packaging
Finasteride 5 mg Tablets. There are 25 tablets in a blister. 4 blisters are packed in a cardboard box together with an enclosed leaflet.