Finasteride sold under the brand names Proscar and Propecia among others,prevents the conversion of testosterone to dihydrotestosterone (DHT) in the body. DHT is involved in the development of benign prostatic hyperplasia (BPH).
Finasteride is 4-azaandrost-1-ene-17-carboxamide, N-(1,1-dimethylethyl)-3-oxo-,(5α,17ß)-. The empirical formula of finasteride is C23H36N2O2 and its molecular weight is 372.55. Finasteride is a white crystalline powder with a melting point near 250°C. It is freely soluble in chloroform and in lower alcohol solvents, but is practically insoluble in water.
Finasteride (Propecia) is used for the treatment of male pattern hair loss. Finasteride (Proscar) is used to treat symptoms of benign prostatic hyperplasia (BPH) in men with an enlarged prostate.This medicine is for use in men only.
Male pattern hair loss happens because hair follicles are susceptible to a process called androgenic miniaturization. Hair follicles shrink and eventually stop producing hair due to the conversion from ordinary testosterone to a form of testosterone called DHT. Some men’s scalp hair follicles respond to increasing levels of DHT by shrinking and producing thinner hair, until sometimes stopping hair production altogether. It affects up to 70% of men over their lifetimes.
Finasteride is a 5α-reductase inhibitor, specifically the type II and III isoenzymes.By inhibiting 5α-reductase, finasteride prevents conversion of testosterone to dihydrotestosterone (DHT) by the type II and III isoenzymes, resulting in a decrease in serum DHT levels by about 65–70% and in prostate DHT levels by up to 85–90%,where expression of the type II isoenzyme predominates.
Unlike triple inhibitors of all three isoenzymes of 5α-reductase like dutasteride which can reduce DHT levels in the entire body by more than 99%, finasteride does not completely suppress DHT production because it lacks significant inhibitory effects on the 5α-reductase type I isoenzyme, with 100-fold less affinity for I as compared to II.
By blocking DHT production, finasteride reduces androgen activity in the scalp. In the prostate, inhibition of 5α-reductase reduces prostate volume, which improves BPH and reduces risk of prostate cancer. Inhibition of 5α-reductase also reduces epididymal weight, and decreases motility and normal morphology of spermatozoa in the epididymis.
Neurosteroids like 3α-androstanediol and allopregnanolone activate the GABAA receptor; because finasteride prevents the formation of neurosteroids, it may contribute to a reduction of GABAA activity (see also neurosteroidogenesis inhibitor).
Reduction of GABAA receptor activation by these neurosteroids has been implicated in depression, anxiety, and sexual dysfunction.
In addition to inhibiting 5α-reductase, finasteride has also been found to competitively inhibit 5β-reductase (AKR1D1), although its affinity for the enzyme is substantially less than for 5α-reductase (an order of magnitude less than 5α-reductase type I) and hence is unlikely to be of clinical significance.
Finasteride reduces prostate volume by 20 to 30% in men with benign prostatic hyperplasia.
Physicians sometimes use finasteride for the treatment of BPH, informally known as an enlarged prostate. Finasteride may improve the symptoms associated with BPH such as difficulty urinating, getting up during the night to urinate, hesitation at the start of urination, and decreased urinary flow. It provides less symptomatic relief than alpha-1 blockers such as tamsulosin and symptomatic relief is slower in onset (six months or more of treatment with finasteride may be required to determine the therapeutic results of treatment). Symptomatic benefits are mainly seen in those with prostate volume > 40 cm3. In long-term studies finasteride but not alpha-1 inhibitors reduce the risk of acute urinary retention (−57% at 4 years) and the need for surgery (−54% at 4 years). If the drug is discontinued, any therapeutic benefits reverse within about 6–8 months.
Finasteride is sometimes used to treat pattern hair loss (androgenetic alopecia) in men only. Treatment slows further hair loss and provides about 30% improvement in hair loss after six months of treatment, with effectiveness usually only persisting as long as the drug is taken, although on occasion hair loss is slowed indefinitely following withdrawal. Finasteride has also been tested for pattern hair loss in women; the results were no better than placebo.
Finasteride has been found to be effective in the treatment of hirsutism (excessive facial and/or body hair growth) in women. In a study of 89 women with hyperandrogenism due to persistent adrenarche syndrome, finasteride produced a 93% reduction in facial hirsutism and a 73% reduction bodily hirsutism after 2 years of treatment.Other studies using finasteride for hirsutism have also found it to be clearly effective.
Finasteride is sometimes used in hormone replacement therapy for transgender women due to its antiandrogen properties, in combination with a form of estrogen . However, little clinical research of finasteride use for this purpose has been conducted and evidence of efficacy is limited.Moreover, caution has been recommended when prescribing finasteride to transgender women, as finasteride may be associated with side effects such as depression, anxiety, and suicidal ideation, symptoms that are particularly prevalent in the transgender population and in others at high risk already.
Read the Patient Information Leaflet provided by your pharmacist before you start taking finasteride and each time you get a refill. If you have any questions regarding the information, consult your doctor or pharmacist.
Take this medication by mouth, with or without food, usually once a day, or as directed by your doctor.
If the tablet is crushed or broken, it should not be handled by a woman who is pregnant or by a woman who may become pregnant (see also Precautions section).
Use this medication regularly in order to get the most benefit from it. Remember to use it at the same time each day. Do not stop taking this medication without consulting your doctor.
It may take 6-12 months to notice a benefit.
Inform your doctor if your condition persists or worsens.
Usual Adult Dose for Benign Prostatic Hyperplasia:
5 mg orally once a day
-Dosing is the same both in monotherapy and in combination therapy.
Usual Adult Dose for Androgenetic Alopecia:
For the treatment of male pattern hair loss (androgenetic alopecia) in men only. (Safety and efficacy have been demonstrated in men between 18 to 41 years of age with mild to moderate hair loss of the vertex and anterior mid scalp area):
-Daily use for 3 months or more is necessary before benefit is observed. Continued use is recommended to sustain benefit.
-Withdrawal of treatment leads to reversal of effect within 12 months.
Use: For the treatment of male pattern hair loss (androgenetic alopecia) in men only. (Safety and efficacy have been demonstrated in men between 18 to 41 years of age with mild to moderate hair loss of the vertex and anterior mid scalp area).
Other drugs may interact with finasteride, including prescription and over-the-counter medicines, vitamins, and herbal products. Tell each of your health care providers about all medicines you use now and any medicine you start or stop using.
Finasteride tablets USP are contraindicated in the following:
• Hypersensitivity to any component of this medication.
• Pregnancy. Finasteride use is contraindicated in women when they are or may potentially be pregnant. Because of the ability of Type II 5α-reductase inhibitors to inhibit the conversion of testosterone to 5α-dihydrotestosterone (DHT), Finasteride may cause abnormalities of the external genitalia of a male fetus of a pregnant woman who receives Finasteride. If this drug is used during pregnancy, or if pregnancy occurs while taking this drug, the pregnant woman should be apprised of the potential hazard to the male fetus.
[See also Warnings and Precautions , Use in Specific Populations, How Supplied/Storage and Handling and Patient Counseling Information In female rats, low doses of Finasteride administered during pregnancy have produced abnormalities of the external genitalia in male offspring.
Women should not handle crushed or broken Finasteride tablets USP when they are pregnant or may potentially be pregnant because of the possibility of absorption of Finasteride and the subsequent potential risk to a male fetus. Finasteride tablets USP are coated and will prevent contact with the active ingredient during normal handling, provided that the tablets have not been broken or crushed
Prior to initiating treatment with Finasteride tablets USP, consideration should be given to other urological conditions that may cause similar symptoms. In addition, prostate cancer and BPH may coexist.
Patients with large residual urinary volume and/or severely diminished urinary flow should be carefully monitored for obstructive uropathy. These patients may not be candidates for Finasteride therapy.
Treatment with Finasteride tablets USP for 24 weeks to evaluate semen parameters in healthy male volunteers revealed no clinically meaningful effects on sperm concentration, mobility, morphology, or pH. A 0.6 mL (22.1%) median decrease in ejaculate volume with a concomitant reduction in total sperm per ejaculate was observed.
These parameters remained within the normal range and were reversible upon discontinuation of therapy with an average time to return to baseline of 84 weeks.
A 2010 Cochrane review concluded that side effects from finasteride are rare when used for BPH. Compared with placebo, men taking finasteride are, however, at increased risk for impotence, erectile dysfunction, decreased libido, and ejaculation disorder for the first year of treatment.In this review the rates of these effects became indistinguishable from placebo after 2–4 years and these side effects usually got better over time.Another 2010 review found that when used for hair loss finasteride increased rates of sexual problems.A 2016 review of 5α-reductase inhibitors for prostatic hyperplasia found that sexual dysfunction was 2.5 times more likely in those who used them.
In men with prostatic hyperplasia the use of both a 5α-reductase inhibitor and a α1-adrenergic receptor blocker resulted in a greater risk of erectile dysfunction compared to either agent alone.
Finasteride (Propecia) has been approved for men with pattern baldness since 1998 with a relatively low side effect profile.1 Potential side effects include decreased libido and disturbed sexual function, but the majority of research shows that these sexual side effects are reversed when the drug is withdrawn.
A number of new reports that are based on patient questionnaires suggest that the sexual side effects of finasteride may actually be permanent, and that the drug may also cause depressive symptoms and suicidal thoughts in patients who suffer from persistent sexual side effects.The studies have become a hot topic among dermatologists and other healthcare professionals who treat patients with hair loss, and it appears to be unclear, just yet, how widespread the issue of long-term sexual side effects is.
Finasteride is an inhibitor of steroid Type II 5a-reductase, that works by decreasing the amount of a natural body hormone dihydrotestosterone (DHT) that causes growth of the prostate, and is used to treat symptoms of benign prostatic hyperplasia (BPH) in men with an enlarged prostate. Proscar is available in generic form. Common side effects of Proscar include.
loss of interest in sex,
trouble having an orgasm,
swelling in your hands or feet,
swelling or tenderness in your breasts,
runny nose, or
In some men, Proscar can decrease the amount of semen released during sex. This is harmless. Proscar may also increase hair growth. The sexual side effects of Proscar may continue after you stop taking it. Talk to your doctor if you have concerns about these side effects.
The recommended dose of Proscar is one tablet (5 mg) taken once a day. Other drugs may interact with Proscar. Tell your doctor all prescription and over-the-counter medications and supplements you use. Proscar is not recommended for use in women and must not be used during pregnancy. This medication is not usually used in women. Therefore, it is unlikely to be used during pregnancy or breast-feeding.
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