The effect of finasteride on the female body. Finasteride: instructions for use. Finasteride in bodybuilding

Finasteride is a medicine for stopping hair loss in men and treating prostate adenoma. Slows down the conversion of testosterone to dihydrotestosterone by binding to the second type of 5-alpha reductase enzyme. It affects the root cause of baldness, but does not stimulate new hair growth, therefore it is used in conjunction with minoxidil. Retains existing hair and slows down further balding. The drug is available in pill form and is taken orally every day.

Questions and answers about finasteride:

If you intend to take finasteride-based drugs for the treatment of baldness, then first you should definitely consult your therapist and trichologist. Finasteride should not be taken by women and children.

What are the names of finasteride-based drugs?

Propecia or Propecia- a drug based on finasteride to stop baldness. In this preparation, there is 1 mg of finasteride for each tablet. For treatment, one tablet is taken per day.

Finpecia- Indian analogue of Propecia, which is produced by CIPLA. Does not differ from Propecia in composition or dosage. Each tablet contains 1 mg of finasteride. The price is significantly lower than the original.

There are drugs in which the active ingredient is finasteride, but with which prostate adenoma is treated. They do not differ in composition, but differ in dosage. 5 mg instead of 1 mg in Propecia and Finpecia. List of drugs:

• Penester
• Proscar
• Finast
• Finasteride
• Alfinal
• Vero-finasteride
• Proteride

What is the difference between 1 mg and 5 mg drugs other than dosage?

No. The drugs for the treatment of prostate adenoma contain only one active substance - finasteride. There are no other active substances.

How does finasteride work?

Once in the bloodstream, it binds with type 2 5-alpha reductase instead of testosterone, which leads to a decrease in dihydrotestosterone levels.

What is type 2 5-alpha reductase?

5-alpha reductase- a human enzyme that converts the male sex hormone testosterone into the more potent androgen dihydrotestosterone, and also participates in the formation of the neurosteroids allopregnanolone and THDOC. Thus, by reducing the amount of 5-alpha reductase (through its binding to finasteride), the total amount of dihydrotestosterone decreases. It is for this that finasteride is used - to reduce the concentration of dihydrotestosterone in the body.

What is DHT?

Dihydrotestosterone- a biologically active form of testosterone, formed from it in the cells of target organs under the influence of the enzyme 5-alpha reductase. Dihydrotestosterone binds much more strongly to tissue androgen receptors than the parent compound (testosterone). Increased formation of dihydrotestosterone in hair follicles is associated with excessive body hair growth and / or "male" type of hair loss on the head in both sexes. Dihydrotestosterone performs the following functions:

• Stimulates sebum secretion of the sebaceous glands;
• Stimulates the division of prostate cells;
• Stimulates or inhibits the growth of hair on certain parts of the body;
• Stimulates the growth of the genitals in men during puberty;
• Has an effect on erectile function in men (desire, while testosterone is responsible for erection);
• Presumably influences recovery from heavy physical exertion.

Will a decrease in DHT levels affect the body?

Once you start taking finasteride, your DHT levels will begin to decrease, and will remain at such a low level until you stop taking the drug. The testosterone level in this case is increased (by a maximum of 10%) to compensate for the decrease in dihydrotestosterone. Gradually, the concentration of dihydrotestosterone in the hair follicles will decrease, which is required for treatment.

How long should I take finasteride?

As long as you are taking finasteride, it works. If you stop taking it, the effect stops. Finasteride should be taken while your hair is dear, that is, all your life. Or until a new, more effective remedy is invented.

When will the first results appear?

The first results can be seen in 6-12 months. In extremely rare cases, improvements may appear within three months.

Can Finasteride Grow New Hair?

The drug affects the root cause and stops baldness. In some cases, the use of finasteride alone may be accompanied by the growth of new hair. Rarely is it possible to restore most of the lost hair, as in this case. The man took 1 mg of finasteride every day for three years and had good results. Usually, you can only achieve a suspension of prolapse; to stimulate growth, you need to use minoxidil.

Why doesn't finasteride always stop baldness?

Type 2 5-alpha reductase is inhibited, which accounts for approximately 70% of the total amount of 5-alpha reductase in the body. But there is also 5-alpha-reductase of the first type, on which finasteride has no effect. Therefore, this enzyme continues to exist in the hair follicles. In addition, if the follicles are hypersensitive to DHT, then even a small amount will be sufficient to continue shedding.

A situation is possible when the 5-alpha-reductase of the first type is significantly more active than the 5-alpha-reductase of the second in a particular individual. In such a case, dutasteride can help, which binds to both types.

Is it possible to cure alopecia areata or universal alopecia?

No. Finasteride is used only for androgenetic alopecia, that is, with male pattern baldness.

If you have any additional questions or comments, please leave a comment. This article was helped by gudkov from the volosy.com forum.

Pharmacological group: Drugs for the treatment of benign prostatic hyperplasia
Pharmacological action: A drug for the treatment of benign prostatic hyperplasia (BPH). A competitive and specific inhibitor of type II 5-alpha reductase - an intracellular enzyme that converts testosterone into a more active androgen - dihydrotestosterone (DHT). It is a synthetic 4-azasteroid compound. Effectively reduces the level of DHT both in the blood and in the tissue of the gland.
Systematic (IUPAC) name: N- (1,1-dimethylethyl) -3-oxo (5alpha, 17beta) -4-aza-androst-1-ene-17-carboxylic acid
Legal status: available by prescription only (UK, US)
Application: oral
Bioavailability: 63%
Metabolism: liver
Half-life: Elderly 8 hours; Adults 6 hours
Excretion: fecal (57%), in urine (39%) as metabolites
Formula: C 23 H 36 N 2 O 2
Like. mass: 372.549 g / mol

Finasteride (trademarks Proscar and Propecia from Merck, among other generic names) is a synthetic drug for the treatment of benign prostatic hyperplasia (BPH) and male pattern baldness. The drug is a type II 5-alpha reductase inhibitor. 5alpha-reductase is an enzyme that is responsible for converting testosterone to dihydrotestosterone (DHT).

Finasteride: application

Benign prostatic hyperplasia

In medical practice, Finasteride is used to treat benign prostatic hyperplasia (BPH), popularly known as "enlarged prostate". The FDA approved dose is 5 mg once a day. To achieve therapeutic results, it may take six or more months of treatment with Finasteride. When you stop taking the drug, the disease may start to develop again within about 6 to 8 months. Finasteride reduces the manifestation of symptoms associated with prostate adenoma, such as difficulty urinating, night trips to the toilet, retention at the onset of urination, and decreased urine flow.

Action

Synthetic 4-azasteroid compound, competitive inhibitor of type II steroid 5-alpha reductase. This intracellular enzyme converts testosterone into the active 5-alpha-dihydrotestosterone (DHT). Inhibition of DHT production leads to a decrease in the size of the prostate gland. Finasteride does not have an affinity for the androgen receptor, so that during its use, testosterone-dependent symptoms such as weight gain and hirsutism do not appear. As a result of the use of finasteride, the concentration of DHT in serum, urine and DHT present in the prostate decreases, which reduces the size of the prostate, increases the maximum volumetric flow rate of urine, reduces the risk of acute urinary retention and the risk of requiring surgery. A decrease in the concentration of DHT in the scalp prevents the miniaturization of hair follicles, halting the balding process. After oral administration, bioavailability is about 80%, food intake does not affect absorption. Finasteride binds approximately 93% to plasma proteins, crosses the blood-brain barrier. Metabolism occurs in the liver under the influence of the isoenzyme CYP3A4 of cytochrome P-450. About 60% of the drug is excreted in the feces, about 40% in the urine. t1 / 2 is 5-6 hours, in patients over the age of 70 - 8 hours. The effect of the action, which consists in reducing the concentration of DHT, is retained for 24 hours.

Finasteride: indications for use

It is used exclusively in men to control the course and treatment of benign prostatic hyperplasia in order to reduce the size of an enlarged prostate gland, increase the maximum urine flow rate and reduce symptoms associated with hyperplasia, reduce the risk of acute urinary retention and the associated likelihood of surgery (including transurethral resection of the prostate and prostatectomy). Treatment of male pattern baldness (only in men).

Finasteride: contraindications

Hypersensitivity to any component of the drug. Do not use in women and children (due to the ability to inhibit the conversion of testosterone into dihydrotestosterone, this drug, when taken by women during pregnancy, can cause anomalies in the development of the external genital organs of male fetuses). The condition of patients with a large residual urine volume should be carefully monitored for the development of uropathy caused by urinary tract obstruction.

Drug interactions

There were no clinically significant interactions with other drugs.

Pregnancy and lactation

Method of administration and dosage

Benign prostatic hyperplasia: 5 mg once a day, regardless of food intake. In order to evaluate the effect of treatment, finasteride must be taken for at least 6 months. A decrease in the risk of acute urinary retention occurs within 4 months of treatment. There is no need to change the dose in renal failure or in elderly patients. Male pattern baldness: 1 mg once a day; the duration of treatment should be at least 3 months.

Finasteride for baldness

In a 5-year study of men with mild to moderate hair loss, hair counts found that two out of three men who took 1 mg of Finasteride daily regained hair growth. In contrast, all men in the study who did not take Finasteride experienced hair loss. In the same study, based on photographs reviewed by an independent group of dermatologists, it was determined that 48% of patients taking Finasteride experienced visible hair regrowth, and another 42% experienced no further hair loss. The average hair count in the treatment group remained above baseline, and the difference in hair count between participants in the Finasteride and placebo groups increased steadily over the five years of the study. Finasteride is only effective while it is being used. Hair that has grown during treatment falls out within 6-12 months after stopping therapy. In clinical studies, it has been shown that Finasteride and Minoxidil affect both the parietal region and the hairline, but it is more effective on the parietal region. A recent 10-year study of 118 men with androgenic alopecia (alopecia) who took Finasteride 1 mg / day showed that 86% of men who continued treatment for all 10 years experienced an increase or maintenance of their hair growth rate, and only 14% of patients reported further hair loss. It was found that patients who showed the most hair growth during the first year of treatment had more pronounced hair growth after 5 years of treatment, with almost 69% of these patients continuing to grow hair, but many patients who did not experience growth during the first year of treatment experienced further improvement. It has also been found that in patients over 30 years of age, hair growth tends to increase in the long term, presumably due to the fact that such patients experience more hair loss during their lifetime compared to other age groups in the population. Side effects were observed in only 5.9% of patients, and none of them reported symptoms such as depression or gynecomastia. The authors concluded that the effectiveness of Finasteride in the treatment of androgenetic alopecia does not decrease over time, even in elderly patients (including patients over 40 years of age), and that the drug is generally well tolerated. The study separately considered patients who continued to use the drug. A recent case-control study of male pattern baldness who experienced psychiatric complications after discontinuation of Finasteride reported the presence of depressive symptoms and suicidal thoughts in patients who also experienced sexual side effects when using the drug. Some users, in an attempt to save money, instead of Propecia buy Proscar (Finasteride 5 mg), and divide the Proscar tablet into several parts, thus bringing the dosage closer to the dosage of Propecia. To prevent contact with the active ingredient during use, the tablets are coated with a special layer. Dust or crumbs from broken Proscar tablets should be kept away from pregnant women or women who may become pregnant.

Improper use

Because of its antiandrogenic properties, Finasteride is sometimes used in hormone replacement therapy in transgender men in combination with a form of estrogen. However, there are too few data from clinical studies of the use of Finasteride for this purpose and the evidence for its effectiveness in this area is very limited. Indeed, Finasteride is significantly weaker than conventional antiandrogens such as spironolactone and cyproterone acetate. In addition, its use is associated with a high risk of depression and anxiety in both men and women; transsexuals are at a particularly high risk as such symptoms are very common among this group of patients. Therefore, it is not recommended to prescribe Finasteride as an antiandrogen for transgender men, as the drug increases the risks of harmful emotional side effects. Finasteride has also been found to help mitigate the effects of withdrawal after chronic alcohol use.

Finasteride side effects

Finasteride side effects include impotence (1.1 - 18.5%), excessive ejaculation (7.2%), decreased ejaculate volume (0.9 - 2.8%), sexual dysfunction (2.5%), gynecomastia (2.2%), erectile dysfunction (1.3%), impaired ejaculation (1.2%) and testicular pain. According to the information included in the packaging of the product, recovery was observed both in men who discontinued treatment with Finasteride due to these side effects, and in most men who continued therapy. The manufacturer also speaks of patient reports of persistent erectile dysfunction despite discontinuation of the drug. In December 2010, Merck added depression to the list of Finasteride side effects. In November 1997, the FDA refused to recommend approval of Propecia for the treatment of male pattern baldness. Although not challenging its effectiveness, Committee members expressed some concerns about the potential for long-term adverse effects on sexual function and perhaps even on reproductive capacity due to the evidence of decreased ejaculate levels.

Prostate cancer

The FDA has added a warning to Finasteride's packaging that the drug may increase the risk of high-grade prostate cancer. Although the effect of Finasteride on the risk of prostate cancer has not been established, evidence suggests that the drug can temporarily reduce the growth and prevalence of benign prostate tumors, but may also mask the early signs of prostate cancer. The main problem is presented by patients in whom prostate cancer, when taking Finasteride, develops to benign prostatic hyperplasia, which, in turn, can lead to a delay in the diagnosis and early treatment of prostate cancer, thereby potentially increasing the risk of developing full-fledged prostate cancer in these patients. The 2005 Prostate Cancer Prevention Trial showed that at a dose of 5 mg per day, usually prescribed for BPH (benign prostatic hyperplasia), participants taking Finasteride were 25% less likely to develop prostate cancer at the end of the study compared with placebo. ... One might mistakenly think that Finasteride increases the specificity and selectivity of detecting prostate cancer, thereby creating a visible increase in the risk of developing tumors with high Gleason scores. An update to this 2008 study found that finasteride reduced the risk of prostate cancer by 30%. In the original study, Finasteride-induced contraction of the prostate gland aided in the identification of bundles of cancer and aggressive cells. Most of the men in the study, with low and high rates of prostate cancer, chose to undergo treatment, and many of them had surgery to remove their prostate. The pathologist then carefully analyzed each of the 500 prostates and compared the cancers found during surgery with those originally diagnosed on biopsy. This study showed that finasteride did not increase the risk of developing high-grade prostate cancer.

Sexual side effects

There have been reports of cases of sustained decrease in libido or erectile dysfunction, even after discontinuation of the drug. In December 2008, the Swedish Agency for Medical Products conducted a safety study for Finasteride and concluded that taking Finasteride could lead to the development of irreversible sexual dysfunction. In the safety update, the Agency identified the occurrence of erection difficulties that persist indefinitely as a possible side effect of the drug, even after discontinuation of Finasteride. The UK Healthcare Products Regulatory Agency (MHRA) reports data on erectile dysfunction that persisted after Finasteride was discontinued. Similar changes have been made to the labeling by the Italian government. For some time, there was a discrepancy between European and North American warnings about the dangers of developing persistent sexual side effects when taking Propecia. However, two years later, in April 2011, Merck revised the US warning for consumer and medical leaflets to include erectile dysfunction that persisted after Finasteride was discontinued. In April 2012, the FDA decided to endorse Merck's proposed labeling since 2011, after including reports of persistent libido disorders, ejaculation disorders, orgasm disorders, and decreased libido on the warning label.

Anxiety and depression

Finasteride has been found to induce depressive and anxious behavior in animals. Accordingly, its clinical use has been associated with depression and anxiety in both men and women, as demonstrated by several reports from the medical literature. In one study, Finasteride 1 mg daily caused moderate to severe depression in 19 of 23 (83%) participants, including all patients. In addition, in some cases, marked anxiety has accompanied the development of depressive symptoms. Another study with a large sample of 128 men (no women) taking Finasteride 1 mg per day found that Finasteride increased both the Beck Scale and the Hospital Depression Scale for depression. The authors concluded that Finasteride should be used with caution in patients at high risk of depression. In late 2010, Merck revised the Propecia label information in the United States and Canada, adding depression to the list of possible side effects of the drug. In August 2012, a study of 61 former Finasteride users with persistent sexual side effects found that 75% of them experienced a significant increase in depressive symptoms compared to a control group. Among men taking the drug, 36% experienced severe symptoms, 28% moderate, and 11% mild. In addition, 44% of men had suicidal thoughts. In a control group of 29 men, 10% showed depressive symptoms, all of which were mild, and 3% reported suicidal thoughts. It was concluded that Finasteride can cause symptoms of depression and suicidal thoughts in some individuals, which persist even after stopping treatment.

Breast cancer in men

In December 2009, the UK Medicines and Medical Devices Regulatory Agency announced an update to the safety guidelines for Finasteride and the potential risk of breast cancer in men. The agency concluded that although there was no significant increase in the overall incidence of breast cancer in men in clinical trials with Finasteride 5 mg, an increased risk of breast cancer in men cannot be ruled out with Finasteride. A warning of such risk will be included in the product information. Merck has revised the warning on consumer and health leaflets in the United States to include the risk of breast cancer in men.

Finasteride for women

The FDA has classified Finasteride as a Category X drug for pregnancy. This means that the drug can cause birth defects in the fetus. Pregnant women or women who may become pregnant should avoid any interaction with crushed or broken Finasteride tablets, as the drug may seep through the skin. Finasteride is known to cause birth defects in developing male children. Exposure to whole tablets should be avoided whenever possible, although exposure is not harmful as long as the tablet is not swallowed. It is not known whether finasteride passes into breast milk, so women should avoid using the drug. Finasteride can penetrate the semen of men, but Merck points out that contact of a pregnant woman with the semen of a man taking Finasteride is not dangerous. Finasteride affects donated blood and potential donors are generally restricted from donating for at least a month after the last Finasteride dose.

Finasteride in bodybuilding

Many sports organizations have banned Finasteride because the drug can be used to disguise the use of steroids. Since 2005, Finasteride has been included in the list of substances prohibited by the World Anti-Doping Agency. However, in 2009 the drug was removed from this list. A number of famous athletes who have used Finasteride as a hair loss remedy and have been excluded from international competitions are led by skeleton athlete Zach Lund, bobsledder Sebastian Gattuso, footballer Romario and ice hockey goalkeeper Jose Theodore.

Mechanism of action

Testosterone in men is produced primarily in the testes and also in the adrenal glands. Most of the testosterone in the body is bound to sex hormone binding globulin (SHBG), a protein produced in the liver that transports testosterone through the bloodstream, prevents its metabolism, and prolongs its half-life. When released from its bond with SHBG, free testosterone can enter cells throughout the body. In some tissues, in particular in the tissues of the scalp, skin and prostate gland, testosterone, under the action of the enzyme 5alpha-reductase, is converted into 5alpha-dihydrotestosterone (DHT). DHT is a more potent androgen than testosterone (approximately 3-10 times more active against the androgen receptor, the site of action of androgen hormones), so 5alpha reductase can be considered to enhance the androgenic effect of testosterone in the tissues where it is located. Finasteride, a 4-azasteroid and testosterone analogue, acts as a potent and specific, competitive inhibitor of one of two subtypes of 5alpha reductase, specifically the type II isoenzyme. In other words, it binds by an enzyme and prevents the metabolism of endogenous substrates such as testosterone. 5alpha-reductase types I and II account for approximately one-third and two-thirds of systemic DHT production, respectively. Other substrates of 5a-reductase include progesterone, androstenedione, epi-testosterone, cortisol, aldosterone, and deoxycorticosterone. The full physiological effect of their recovery is unknown, but it is probably related to their release or is physiological in itself. Besides the fact that the drug acts as a catalyst in limiting the rate of testosterone reduction reaction, isoforms I and II of the enzyme 5alpha-reductase reduce progesterone to dihydroprogesterone (DHP) and deoxycorticosterone to dihydrodeoxycorticostenor (DHDOC). In vitro and animal models show that subsequent 3alpha reduction of DHT, DHP and DHDOC leads to the creation of steroid metabolites that affect brain function by increasing β-acid inhibition. These neuroactive steroid derivatives increase levels at GABA (A) receptors and have anticonvulsant, antidepressant and anxiolytic effects, as well as sex and alcohol-related behavior. 5alpha-dihydrocortisol from the intraocular fluid is synthesized in the lenses, and itself can participate in the production of intraocular fluid. Allopregnanolone and DHDOC are neurosteroids, and the latter can affect the susceptibility of animals to epilepsy. 5alpha-dihydroaldosterone is a potent antidiuretic, although different from aldosterone. Its formation in the kidneys is enhanced by restricting dietary salt, which suggests that sodium can be stored as follows:

Substrate + NADPH + H + → 5alpha-substrate + NADP +

5alpha-BPH is one of the main hormones in the bloodstream in women with normal cycles and in pregnant women. When 5-alpha reductase is inhibited, Finasteride prevents the formation of testosterone in DHT by the type II isoenzyme, which leads to a decrease in serum DHT levels by about 65-70%, and an increase in DHT levels in the prostate to 85-90%, where it is dominated expression of type II isoenzyme. Unlike dual inhibitors of both 5alpha-reductase isoenzymes, which can reduce DHT levels throughout the body by more than 99%, Finasteride is not able to completely suppress DHT production, since it cannot significantly inhibit the type I isoenzyme 5alpha-reductase due to its 100 times lower affinity for I in comparison with II. In addition to blocking the type II isoenzyme, Finasteride competitively inhibits the type II isoenzyme 5beta-reductase, but this is not believed to affect androgen metabolism. By blocking the production of DHT, Finasteride reduces the activity of androgens in the scalp. In the prostate gland, inhibition of 5alpha-reductase reduces the volume of the prostate gland, reducing the development of benign prostatic hyperplasia (BPH) and the risk of prostate cancer. Inhibition of 5alpha-reductase also reduces epididymal weight, reduces motility, and alters the normal placement of sperm in the epididymis. Cause of mood-related and sexual side effects DHT and neuroactive steroids (NAS) such as allopregnanolone (ALLO) and tetrahydrodeoxyorticosterone (THDOC) are powerful positive allosteric modulators of the GABA receptor (acting on the same sites as euphoric substances and anxiolytic drugs such as benzodiazepines and alcohol), and are important endogenous neuroregulators with potent antidepressant and anxiolytic effects, and also play a positive role in sexual functioning. Their biosynthesis depends on both isoforms of 5alpha-reductase. Finasteride reduces their formation in the body. This effect of Finasteride is the likely cause of the emotional and sexual side effects associated with the drug. In addition, since it involves not only DHT but also NAS, it could potentially also explain the fact that the effects associated with mood and anxiety are observed not only in men, but also in women.

Forms of issue

Trade names include Propecia and Proscar, which are used first to treat male pattern baldness and secondly to treat benign prostatic hyperplasia (BPH), both of which are Merck & Co. products. Propecia contains 1 mg Finasteride and Proscar 5 mg. Merck's patent for Finasteride for BPH expired on June 19, 2006. Merck has received a separate patent for the use of Finasteride for the treatment of male pattern baldness. This patent expires in November 2013. Studies have shown that the dose of Finasteride required to treat male pattern baldness is less than 1 mg. Petitions have been filed with the FDA to revise the approved dosages in light of the statistics and possible long-term risks. However, the FDA said that there are results from a study where, at a dose of 1 mg versus 0.2 mg, an increase in the effect was shown without additional risks. The same study also concluded that doses of 0.01 mg per day were ineffective in treating hair loss. Finasteride is a lipophilic substance. Recently, the development of the topical Finasteride liposomal system has begun. Topical formulas may have some effect on reversing androgenic effects on hair follicles as well as hirsutism. More recent studies have looked at topical microemulsions and liquid crystal nanoparticles of Finasteride. In the latter case, the addition of glycerin, propylene glycol and polyethylene glycol 400 increased the penetration of Finasteride, while the addition of oleic acid reduced this penetration. Topical finasteride in combination with minoxidil is more effective than minoxidil alone. In small studies, topical finasteride in combination with other drugs has also been found to be effective. Surfactants can promote local penetration of the drug. Finasteride in the form of a gel for topical application has also shown its effectiveness.

History

In 1974, Julianne Imperato-McGinley of Cornell Medical College in New York attended a conference on birth defects. She reported a group of children, boys and girls in the Caribbean, with undetermined gender at birth, and originally raised as girls. However, with age, these girls developed external male reproductive organs and after the onset of puberty, other characteristic male characteristics appeared. The research team found that these children shared a common genetic mutation, resulting in a deficiency of the enzyme 5-alpha reductase and the male hormone (DHT), which was found to be etiologically responsible for abnormalities in the development of male genital organs. After maturation, these people showed a smaller prostate size, an underdeveloped prostate, and no male pattern baldness. In 1975, copies of the Imperato-McGinley presentation were spotted by P. Roy Vagelos, who was in charge of basic research at Merck at the time. The scientist was interested in the fact that a decrease in DHT levels leads to a shrinkage of the prostate. Dr. Vagelos set about creating a drug that could mimic the condition seen in these children to treat older men suffering from benign prostatic hyperplasia. In 1992, Finasteride (5 mg) was approved by the US FDA for the treatment of benign prostatic hyperplasia (BPH), and is marketed by Merck under the brand name Proscar. In 1997, Merck was able to obtain FDA approval for a second indication for Finasteride (1 mg) for the treatment of male pattern baldness, marketed under the brand name Propecia.

Availability:

Finasteride is a drug used to treat benign prostatic hyperplasia (BPH). A competitive and specific inhibitor of type II 5-alpha reductase - an intracellular enzyme that converts testosterone into a more active androgen - dihydrotestosterone (DHT). It is a synthetic 4-azasteroid compound. Effectively reduces the level of DHT both in the blood and in the tissue of the gland. Dispensed from pharmacies with a doctor's prescription.

Notes (edit)

So far, no positive clinical effect of treatment with finasteride in patients diagnosed with prostate cancer has been shown. Before starting the drug and during treatment, it is recommended to conduct research in order to exclude prostate cancer. This is due to the fact that finasteride causes a decrease in the concentration of prostate specific antigen (PSA) in the serum of patients by about 50% and can mask the actual increased concentration of this antigen. The drug has no significant effect on the ratio of free PSA to total PSA. In patients taking finasteride for 6 months or more, PSA values ​​should be doubled compared to normal values ​​in untreated individuals.

Men, according to medical statistics, are more susceptible to the development of baldness than women. The main reason for the loss of hair is the improper production of male hormones. The main hormone from the androgen group is testosterone.

Male hormones help to stimulate the growth of bones and muscles, facial hair, trunk and scalp. But there are times when they have a detrimental effect on the growth of hair. In the dermal cells of the frontal region, and even the crown, testosterone is exposed to the action of an enzyme that converts it into another hormone-like substance. It is it that provokes inhibition of hair growth, as well as the development of baldness.

In the fight against male pattern baldness, a variety of drugs and formulations are used today. However, Finasteride for hair is considered one of the most effective remedies in the fight against hair loss.

Therapy for thinning hair should be timely and appropriate. This is the only way to get rid of the aesthetic problem, as well as the complexes associated with it. However, in order for the treatment to be effective, and the drug used to bring maximum benefit, before starting its use, you should consult a specialist.

How does the remedy work

The medicine helps to block the newly formed hormone, as well as to lower its content by 70%. It should be understood that Finasteride for hair is not able to eliminate the root cause of the pathology, however, it helps in blocking the harmful effects of the hormone. It is for this reason that after stopping the use of the product, the hair can thin again within a year.

Therefore, in order to preserve hair, it is necessary to use the composition constantly. The tool helps to block the effects of the hormone immediately after application. However, it takes time for new vegetation to appear. Healthy new hair grows back about one centimeter in 30 days. A visible result can be achieved after six months.

It happens that the hair grows back in a few months. But this is all individual and depends on the characteristics of the organism. If after prolonged use of Finasteride for hair - for a year or more, the effect is not visible, you need to stop using it, and then use a different composition. However, most often the drug helps men fight baldness. According to the studies, more than 80% of the stronger sex have achieved a positive result. The hair began to grow more actively, in particular in the region of the crown.

There are several analogues of Finasteride. These are drugs with a similar principle of action and a similar composition. The use of Propecia, Minoxidil and Finpecia is often prescribed.

Finasteride is a 5-alpha reductase inhibitor. The active ingredient of the drug is finasteride. In addition to it, the composition is endowed with magnesium stearate, crospovidone, lactose, povidone.

Duration of admission

The drug does not completely cure the disease. It only helps to protect hair follicles from the effects of dihydrotestosterone.

In order to slow down the pathological process, the medicine should be taken constantly.

The medicine is not recommended for women. You can't give it to children. The intake of the composition is contraindicated for people with individual intolerance, as well as those suffering from obstruction of the urinary tract, prostate cancer, and also malfunctions in the functioning of the liver.

In addition, it is forbidden to contact the medicine, even to touch it to women during the period of gestation and breastfeeding. This can adversely affect the development of the fetus.

Side effects

Side effects, as well as drug overdose, are rare. If you take the composition according to the annotation, do not abuse it, it will bring exceptional benefits to the body. However, the appearance of side effects is not excluded. This may be due to both the susceptibility of the organism or individual characteristics, as well as the inappropriate use of the composition. Side effects, according to patient reviews, are mild and pass quickly.

Taking Finasteride for hair may be accompanied by:

• hypersensitivity reactions: swelling of the lips, the appearance of loose elements;
• decreased sex drive;
• deterioration in potency;
• difficulty with erection.

Finasteride: when you can feel the result, price and analogues, why is the product contraindicated for women

The first results after using the medicine, namely the signs that the hair is recovering, can be felt two to three months after the start of taking Finasteride.

Typically, the hairs will be discolored and fine at first. Only over time will they darken and also become thicker. The final result can be felt after a year of continuous use of tablets with the active ingredient finasteride. The maximum results can be achieved by taking the composition for two years.

According to the results of numerous studies, Finasteride is a safe and effective remedy to help fight baldness. In addition, the drug contributes to both the cessation of thinning of the hair, and the improvement of its condition.

How much does the medicine cost

You can buy the composition both in a pharmacy and in an online store. Everyone can afford to buy a medicine. Its average cost is 900 rubles. You just have to be as careful and careful as possible when buying funds via the Internet, as there is a risk of acquiring a fake. In order not to fall for the tricks of unscrupulous sellers, it is preferable to order the composition from a well-established seller.

Analogs

There are many similar remedies. These are either drugs with a similar effect, or formulations based on finasteride. Drug release form - tablets.

The reception of such Finasteride analogs is often prescribed:

• Finasta, costs 800 rubles;
• Alfinal - 770 rubles;
• Proterida - 650 rubles;
• Penestara - 850 RUB

How to take the medicine

The composition is used regardless of the meal. The recommended dosage is 5 mg per day. The tablet does not need to be chewed or bitten, it is swallowed whole with water.

The composition is accepted on an ongoing basis, every day. If you skip taking a pill, you should not drink a double dosage. This will not bring a positive effect, but can only harm. Continue treatment as usual.

Why the drug is contraindicated for women

The product is not recommended for use in women with hair loss. This is due to the increased risk of side effects. Moreover, Finasteride is contraindicated in women of childbearing age. Taking medication during pregnancy is fraught with critical consequences, in particular, causing enormous harm to the fetus, as well as the birth of a baby with a large number of deviations.

Is it possible to drink the drug for a man who plans to conceive a child

The tool has a negative effect exclusively on the body of a pregnant woman and the fetus. Therefore, it is contraindicated for girls, as well as women of childbearing age.

As for men, the use of the medicine does not in any way affect the ability to conceive a healthy child. There should be no reason to worry about this. The medicine penetrates into the seminal fluid in a small dose, which does not harm the unborn baby at all.

The effectiveness of Finasteride

The drug has proven to be effective. This is confirmed by patient reviews and research results. The use of the composition contributes to: the cessation of the progression of pathology, the restoration of vegetation, an increase in the volume of hair, its improvement.

The remedy is effective, but in order not to face the problem again, you need to drink pills constantly. This is the only way to preserve the result and prevent further progression of androgenic and other forms of alopecia.

One of the existing forms of male pattern baldness is androgenic, or androgenetic. This is the most common, which is difficult to treat and causes a psychological disorder in the patient, subsequently contributing to a deterioration in his quality of life.

To combat androgenic alopecia, the drug “Finasteride” was developed and introduced - an effective and safe remedy intended for long-term use.

A little about androgenic alopecia

It develops due to impaired regulation of the function of the hair follicle by certain hormones.

It is known that the main hormone belonging to the group of androgens is testosterone, the action of which is aimed at the formation of such characteristics of the male body as:

• maintaining muscle and bone growth;
• stimulating hair growth on the head, body and face.

However, in most men, androgens have the opposite effect on the hair of the frontal and parietal parts of the head. When exposed to the action of type 2 5α-reductase, testosterone is converted into dihydrotestosterone, a stronger hormone, which inhibits the work of hair follicles, contributing to their death and further baldness. That is why this type of baldness is usually called androgenic, which occurs in most males.

What is Finasteride?

Finasteride ”is the only drug for internal use and has been approved by the US regulatory agency FDA as a treatment and control of androgenic alopecia in men. At the very beginning, this drug was produced under the name "Proscar", was developed and intended to combat diseases that are directly related to the prostate gland.

However, those patients who suffered from androgenic alopecia in parallel, while using Proscar, began to notice a unique “side effect” - the hair stopped falling out, and after a certain time, new growth was observed.

This fact served as an impetus for the company's specialists to conduct complex clinical trials. Based on the research results, it was decided to process the drug, which has a new name, which included the active ingredient finasteride (dosage - 1 mg). Already since 1997 "Finasteride" (which has another name - "Propecia") has been produced for the treatment of androgenic alopecia.

The principle of the drug

The area of ​​application of the drug are: the crown, the middle region of the head, the front hairline, the areas of the scalp most susceptible to androgenic alopecia. It was noted that the first results were observed already 4 months after regular use of the drug.

The action of "Finasteride" is due to the maximum effect of the active component on the hair follicles, due to blocking the work of type 2 5α-reductase.

At the very beginning of treatment, newly growing hair is thin, colorless and lifeless. In the future, they thicken, gradually acquiring a healthy appearance. After two years of regular use, the maximum effect can be observed.

It is believed that the patient can continue treatment with Finasteride if the effect of the application is observed. If, after a year after intensive use, the effect is not observed, then the drug is not subject to further use.

Since the drug acts only on the activity of 5α-reductase, after the termination of treatment with "Finasteride", the loss of grown hair is possible, followed by the progression of the baldness process. Therefore, "Finasteride" is indicated for constant use by those patients who do not have any contraindications and sensitivity to the active ingredient.

Instructions for use

If the patient is dealing with tablets, then the recommended dose should be 1 tablet per day. In the case of lotion, the product is applied twice a day (morning and evening), applied directly to the scalp.

Are there any contraindications for use?

Finasteride has a number of contraindications that should be taken into account. One of the main limitations is due to the presence of an allergic reaction in the patient to the active ingredient of the drug. With the use of the drug, there is a decrease in the concentration of the PSA chemical, which reflects the work of the prostate gland. If a doctor prescribes a PSA test, you should inform him about taking the drug.

In addition, the active substance can adversely affect the development and normal formation of the fetus, therefore, the patient is not recommended to become a blood donor in order to avoid a possible blood transfusion to a pregnant woman. If the patient plans to conceive a child, he should stop taking the drug three months before conception.

Side effects from use

With regular use of "Finasteride", some side effects are possible, characterized by:

• decreased libido (sex drive);
• difficulty in ejaculation;
• erectile dysfunction;
• decreased sperm count;
• pain in the testicles.

These effects were observed only in 2% of patients. In many patients, these effects disappeared even after continued use of the drug.

Similar effects can be observed with local use of "Finasteride". The reason is the partial ingress of the drug into the general bloodstream. If non-patient-specific effects occur, it is recommended to stop using the drug or consult a specialist.

What should you know about the drug?

The maximum effect of the use of the drug should be expected at an early stage of development of androgenic alopecia. In more advanced cases, the expected result is reduced.

Finasteride is intended for men only and is not recommended for women.

Pregnant women are strictly prohibited from "Finasteride", they should avoid direct contact with the drug in order to avoid the development of congenital defects in the embryo.

One coated tablet of Finasteride contains 5 mg of the active substance of the same name.

Auxiliary components: corn starch, lauryl macrogolglycerides, magnesium stearate, lactose, sodium starch, microcrystalline cellulose, Opadry blue shell.

Release form

Blue round biconvex tablets with "F5" engraving on one side.

• 10 such tablets in a contour package; one, two, three or four packages in a cardboard box.
• 14 such tablets in a contour package; one, two, three or four packages in a cardboard box.
• 7 such tablets in a contour package; one, two, three or four packages in a cardboard box.

pharmachologic effect

It has antiandrogenic action.

Pharmacodynamics and pharmacokinetics

Pharmacodynamics

Finasteride is a hormonal drug, a synthetic selective blocker 5α-reductase the second type.

5α-reductase the second type is an intracellular enzyme that transforms into a more active androgen dihydrotestosterone ... At prostate adenoma its increase directly depends on the transformation of testosterone into dihydrotestosterone in the tissues of the gland.

Finasteride effectively reduces both free and tissue dihydrotestosterone ... Does not show tropism for androgen receptors, does not have other hormonal effects.

Pharmacokinetics

It is quickly and completely absorbed from the intestines. Absorption ends approximately 7 hours after. Bioavailability averages 80%. The maximum concentration in the circulating blood is recorded after 1-2 hours.

93% of molecules react with plasma proteins. The remedy goes through blood-brain barrier when taken within 7-10 days. It is metabolized in the liver to form five metabolites, two of which are active.

The half-life is about six hours. Approximately 39% of the ingested dose is excreted in the form of derivatives in the urine, the remainder is excreted in the faeces.

Indications for use

• (to reduce its size);
• the need to improve the flow of urine and reduce the symptoms of hyperplasia;
• the need to reduce the likelihood of development, which requires catheterization or surgery.

Contraindications

• sensitization to finasteride;
• prostate cancer ;
• obstructive uropathy;
• not used in women and children.

Side effects

• External reactions immune systems: hypersensitivity reactions.
• Mental reactions: weakened libido .
• External reactions circulatory system: palpitation.
• External reactions digestive system: activation of liver enzymes.
• External reactions skin: , .
• External reactions mammary glands and reproductive system: , violation ejaculation, gynecomastia, testicular pain, decreased volume ejaculate.

Instructions for use (Method and dosage)

For patients with various forms of dose selection is not required, since pharmacokinetic studies have not revealed changes in Finasteride in this situation.

For older people, there is no need for dose selection, although pharmacokinetic studies indicate that the excretion of the drug in people over 70 years of age is slightly reduced.

Overdose

Patients received a single dose of the drug up to 400 mg and regular doses up to 80 mg per day for three months without the occurrence of undesirable effects.

Interaction

When used together with ACE inhibitors, nitrates, beta-blockers, alpha-blockers, calcium channel blockers, NSAIDs, H2-receptor blockers, diuretics, HMG-CoA reductase blockers, benzodiazepines and quinolones no significant interaction was found.