Binfin tablets 5 mg No. 30

Instructions for use Binfin tablets 5 mg No. 30

Composition

active ingredient: finasteride;

1 tablet contains finasteride 5 mg;

excipients: lactose monohydrate; pregelatinized starch; microcrystalline cellulose; sodium starch glycolate; docusate sodium; magnesium stearate; Opadry Blue 03A80928 (hypromellose, titanium dioxide (E 171), talc, indigo carmine aluminum lake (E 132), iron oxide yellow (E 172)).

Dosage form

Film-coated tablets.

Main physicochemical properties: round, blue, film-coated tablets, with the inscription "H" on one side and "37" on the other side.

Pharmacotherapeutic group

Drugs used for benign prostatic hypertrophy. ATC code G04C B01.

Pharmacological properties

Pharmacodynamics.

Finasteride is a specific inhibitor of 5-alpha-reductase type II, an intracellular enzyme that converts testosterone to the more active androgen dihydrotestosterone (DHT). In benign prostatic hyperplasia (BPH), its enlargement depends on the conversion of testosterone to DHT in prostate tissue. Finasteride is highly effective in reducing both circulating and intraprostatic DHT. Finasteride has no affinity for androgen receptors.

In clinical trials in patients with moderate to severe BPH, an enlarged prostate on digital rectal examination, and low residual urine volume, Binfin reduced the incidence of acute urinary retention from 7/100 to 3/100 over 4 years and the need for surgery (transurethral resection of the prostate and prostatectomy) from 10/100 to 5/100. This reduction was accompanied by a 2-point improvement in the QUASI-AUA symptom score (range 0-34), a significant regression of prostate volume by approximately 20%, and a significant increase in urine flow rate.

The MTOPS (Medical Treatment of Prostatic Symptoms) study was a 4- to 6-year study of 3047 men with symptomatic BPH who were randomized to receive finasteride (5 mg/day), doxazosin (4 mg/day or 8 mg/day), a combination of finasteride (5 mg/day) and doxazosin (4 mg/day or 8 mg/day), or placebo. The primary endpoint was time to clinical progression of BPH (defined as an increase from baseline of 4 or more points on the symptom rating scale, an episode of acute urinary retention, BPH-related renal failure, recurrent urinary tract infection or urosepsis or urinary incontinence). Compared with placebo, treatment with finasteride, doxazosin, or the combination resulted in a significant reduction in the risk of clinical progression of BPH by 34% (p = 0.002), 39% (p < 0.001), and 67% (p < 0.001), respectively. The majority of cases (274 of 351) that constituted BPH progression were confirmed by an increase of ≥ 4 points on the symptom rating scale; with treatment, the risk of symptom progression was reduced by 30% (95% confidence interval 6-48%), 46% (95% confidence interval 25-60%), and 64% (95% confidence interval 48-75%) in the finasteride, doxazosin, and combination groups, respectively, compared with placebo. Acute urinary retention was observed in 41 of 351 cases of BPH progression; Under treatment, the risk of acute urinary retention was reduced by 67% (p = 0.011), 31% (p = 0.296), and 79% (p = 0.001) in the finasteride, doxazosin, and combination groups, respectively, compared with placebo. Only the finasteride and combination groups were significantly different from the placebo group.

Pharmacokinetics.

In men, after a single oral dose of 14C-labeled finasteride, 39% of the dose was excreted in the urine as metabolites (presumably a small amount of unchanged finasteride was also excreted in the urine). 57% of the dose was excreted in the feces. Studies have also shown that two metabolites of finasteride have a less pronounced inhibitory effect on 5-alpha-reductase. The bioavailability of finasteride when taken orally is approximately 80%. Food intake does not affect the bioavailability of the drug. The maximum concentration of finasteride in the blood plasma is achieved approximately 2 hours after oral administration. Absorption of the drug from the gastrointestinal tract is completed 6-8 hours after its intake. The half-life of finasteride in the blood plasma is on average 6 hours. Binding to plasma proteins is 93%. Systemic clearance is approximately 165 ml/min, volume of distribution is 76.1 liters.

In patients with chronic renal failure (creatinine clearance from 9 to 55 ml/min), no difference in the rate of elimination of a single dose of finasteride labeled with carbon isotopes 14C was found compared with healthy volunteers. Binding to plasma proteins in these groups of patients was also not different. This is explained by the fact that in patients with renal failure, the proportion of finasteride metabolites that are normally excreted in the urine is excreted in the feces. This is confirmed by an increase in the number of finasteride metabolites in the feces in these patients with a simultaneous decrease in their concentration in the urine. Therefore, for patients with renal failure for whom hemodialysis is not indicated, dose adjustment of the drug is not required.

There are no data on the pharmacokinetics of the drug in patients with hepatic insufficiency.

Finasteride crosses the blood-brain barrier. Small amounts of finasteride have been detected in seminal fluid.

Indication

Treatment and control of benign prostatic hyperplasia (BPH) in patients with an enlarged prostate gland to:

reduction in size (regression) of the enlarged gland, improvement in urine flow, and reduction of symptoms associated with BPH;

reducing the risk of acute urinary retention and the need for surgical intervention, including transurethral resection of the prostate and prostatectomy.

Contraindication

Hypersensitivity to finasteride or to any component of this drug.

The drug Binfin is not indicated for use in women and children.

Pregnancy or if the patient may potentially be pregnant (see section "Use during pregnancy or breastfeeding").

Interaction with other medicinal products and other types of interactions

No clinically significant interactions with other drugs have been identified. The drug Binfin does not have a significant effect on the enzyme system that metabolizes drugs associated with cytochrome P 450. Although the risk of finasteride affecting the pharmacokinetics of other drugs is assessed as small, there is a possibility that inhibitors and inducers of cytochrome P 450 3A4 will affect the concentration of finasteride in the blood plasma. However, given the established safety profile, any increase in finasteride concentration due to the simultaneous use of cytochrome P450 3A4 inhibitors is unlikely to be of clinical significance. Compounds tested in humans include propranolol, digoxin, glyburide, warfarin, theophylline and antipyrine; no clinically significant interactions were found.

Application features

General measures

Patients with high residual urine volume and/or severely reduced urine flow should be monitored closely for the possible development of obstructive uropathy.

Impact on prostate-specific antigen (PSA) and prostate cancer diagnosis

To date, no beneficial clinical effect of treatment with Binfin has been shown in patients with prostate cancer. Patients with prostate adenoma and elevated PSA levels have been observed in controlled clinical trials with multiple PSA determinations and prostate biopsy. In these studies, the use of Binfin did not affect the incidence of prostate cancer. The overall incidence of prostate cancer was not significantly different in the groups of patients receiving Binfin or placebo.

It is recommended that patients be screened for prostate cancer by digital rectal examination and other methods before and during treatment with Binfin. Serum PSA is also used to detect prostate cancer. In general, a baseline PSA level of more than 10 ng/mL (Hybritech) should prompt a thorough evaluation, including biopsy if necessary. Further evaluation is recommended for PSA levels between 4 and 10 ng/mL. There is considerable overlap in PSA levels between men with and without prostate cancer. Therefore, in men with benign prostatic hyperplasia, normal PSA values do not rule out prostate cancer, regardless of Binfin treatment. A baseline PSA level of less than 4 ng/mL does not rule out prostate cancer.

Any prolonged increase in PSA levels in a patient receiving finasteride 5 mg treatment requires a thorough examination to determine the causes, including non-compliance with the Binfin medication regimen.

Effect of the drug on laboratory data

Impact on PSA levels

Serum PSA levels correlate with patient age and prostate volume, with prostate volume correlating with patient age. When evaluating laboratory PSA values, it is important to consider the fact that PSA levels decrease during treatment with Binfin. Most patients experience a rapid decline in PSA during the first few months of treatment, after which PSA levels stabilize at a new level that is approximately half of baseline. From this review, typical patients receiving Binfin for 6 months or more should have PSA values that are twice as high as those in untreated individuals.

The drug Binfin does not significantly reduce the percentage of free PSA (the ratio of free PSA to total). The ratio of free to total PSA remains constant even under the influence of the drug Binfin. When determining the percentage of free PSA, which is used to diagnose prostate cancer, correction of its values is not required.

Breast cancer in men

During clinical trials and in the post-marketing period, breast cancer has been reported in men taking finasteride 5 mg. Physicians should instruct their patients to report immediately any changes in breast tissue, such as swelling, pain, gynecomastia, or nipple discharge.

Mood swings and depression

Mood changes, including depressed mood, depression and, less commonly, suicidal ideation, have been reported in patients treated with finasteride 5 mg. Patients should be monitored for psychiatric symptoms and advised to seek medical attention if they occur.

Lactose

The drug contains lactose, therefore patients with rare hereditary forms of galactose intolerance, lactase deficiency or glucose-galactose malabsorption syndrome should not use Binfin.

Liver failure

The effect of hepatic insufficiency on the pharmacokinetics of finasteride has not been studied.

Use during pregnancy or breastfeeding

Use during pregnancy

The drug Binfin is contraindicated in pregnant women.

The effect of finasteride is a risk to the male fetus.

Women of childbearing potential and pregnant women should avoid contact with crushed or broken Binfin tablets due to the possibility of finasteride entering the body and the subsequent potential risk to a male fetus. Binfin tablets are coated and this prevents contact with the active ingredient provided that the tablets are not crushed or broken.

There is evidence of small amounts of finasteride being excreted in the semen of a patient taking finasteride at a dose of 5 mg/day. It is not known whether a male fetus may be adversely affected if its mother has been exposed to the semen of a patient treated with finasteride. If the patient's sexual partner is or may potentially be pregnant, the patient should be advised to prevent exposure of the female partner to the semen.

Due to the ability of 5-alpha-reductase type II inhibitors to inhibit the conversion of testosterone to dihydrotestosterone, these drugs, including finasteride, may cause abnormalities in the development of the external genitalia in a male fetus.

Use during breastfeeding

The drug Binfin is not indicated for women. It is not known whether finasteride passes into breast milk.

Ability to influence reaction speed when driving vehicles or other mechanisms

Does not affect the ability to drive a car or operate machinery.

Method of administration and doses

The recommended dose is 1 tablet of 5 mg once a day, regardless of food intake.

The drug Binfin can be used as monotherapy in combination with the alpha-blocker doxazosin (see section "Pharmacological properties").

The duration of treatment is determined by the doctor individually. Although improvement of symptoms may be observed earlier, at least six months of taking the drug are necessary to assess the effectiveness of the action, after which treatment should be continued.

For elderly patients and patients with varying degrees of renal insufficiency (decreased creatinine clearance to 9 ml/min), dose adjustment is not required.

There are no data on the use of the drug in patients with impaired liver function.

Do not use on children.

Children.

The drug Binfin is contraindicated in children.

Safety and effectiveness for use in children have not been established.

Overdose

In patients who received the drug Binfin at a dose of up to 400 mg once and the drug Binfin at a dose of up to 80 mg per day for 3 months, there were no undesirable effects.

There are no specific recommendations for the treatment of overdose with this medicine.

Side effects

The most common adverse reactions are impotence and decreased libido. These adverse reactions occur early in the course of therapy and resolve with continued treatment in most patients.

Adverse reactions reported during clinical trials and/or during post-marketing use are listed in the table below.

The frequency of adverse reactions is defined as: very common (≥1/10), common (≥1/100 - <1/10), uncommon (≥1/1000 - <1/100), rare (≥1/10000 - <1/1000), very rare (<1/10000), frequency unknown (cannot be estimated from the available data).

Additionally, breast cancer has been reported in men taking finasteride in clinical trials and during post-marketing use. Any changes in breast tissue, such as swelling, pain, gynecomastia, or nipple discharge, should be reported to your doctor immediately.

When comparing the safety profiles of finasteride (5 mg/day) and doxazosin (4 or 8 mg/day) monotherapy with the combination therapy of finasteride (5 mg/day) and doxazosin (4 or 8 mg/day) and placebo, the safety and tolerability profile of the combination therapy was consistent with the safety profile of the individual components. The incidence of ejaculation disorders in patients receiving combination therapy was comparable to the sum of the adverse reactions of the two monotherapies.

There is no information on the association between long-term use of finasteride and tumors with Gleason scores of 7-10.

Laboratory test data

When evaluating prostate-specific antigen (PSA) laboratory data, it should be noted that PSA levels decrease in patients taking Binfin. In most patients, a rapid decrease in PSA is observed during the first months of therapy, after which the PSA level stabilizes to a new baseline level. The baseline level after treatment is approximately half the pre-treatment value. Therefore, in most patients taking Binfin for 6 months or more, PSA values should be doubled to compare with normal ranges in untreated men.

When conducting standard laboratory tests, there were no other differences between patients receiving the drug Binfin and patients receiving placebo.

Reporting of suspected adverse reactions

Reporting adverse reactions after the registration of a medicinal product is important. This allows monitoring of the benefit/risk ratio when using this medicinal product. Medical and pharmaceutical professionals, as well as patients or their legal representatives, should report all cases of suspected adverse reactions and lack of efficacy of the medicinal product via the Automated Information System for Pharmacovigilance at the link: https://aisf.dec.gov.ua.

Expiration date

3 years.

Storage conditions

Store at a temperature not exceeding 25 °C out of the reach of children.

Packaging

15 film-coated tablets in a blister.

2 blisters in a cardboard box.

Vacation category

According to the recipe.

Producer

Hetero Labs Limited.

Location of the manufacturer and address of its place of business.

Unit III, Formulation Plot No. 22 - 110 IDA, Jeedimetla, Hyderabad, 500 055 Telangana, India.