Off-label uses
Finasteride is sometimes used in hormone replacement therapy for male-to-female transsexuals in combination with a form of estrogen due to its antiandrogen properties.[9][10] However, little clinical research of finasteride use for this purpose has been conducted and evidence of efficacy is limited. Indeed, finasteride is a substantially weaker antiandrogen in comparison to conventional antiandrogens like spironolactone and cyproterone acetate. Furthermore, it has been associated with inducing depression and anxiety at a high rate in both male and female patients,[11] symptoms that are very common in transsexuals, who are already at a high risk.[12] As a result, prescription of finasteride for this indication in male-to-female transsexuals may not be particularly useful, and could put them at risk for detrimental emotional side effects. Finasteride has also been found to mitigate the effects of withdrawal after chronic alcohol use.[13]
Sexual side effects
There are case reports of persistent diminished libido or erectile dysfunction, even after stopping the drug.[21] In December 2008, the Swedish Medical Products agency concluded a safety investigation of finasteride and advised that finasteride may cause irreversible sexual dysfunction. The Agency's updated safety information lists difficulty in obtaining an erection that persists indefinitely, even after the discontinuation of finasteride, as a possible side effect of the drug.[22] The UK's Medical and Healthcare Products Regulatory Agency (MHRA) cites reports of erectile dysfunction that persists once use of finasteride has stopped.[23] Similar labeling changes have been made by the Italian government. For a period of time there was a discrepancy between European and North American warning labels regarding the risks of developing persistent sexual side effects from taking Propecia but after two years in April 2011 Merck revised the United States' warning in consumer and medical leaflets to include erectile dysfunction that may persist after stopping finasteride.[24] In April 2012, the FDA chose to approve Merck's proposed labeling from 2011 only after the warning label was further strengthened to include reports of persistent libido disorders, ejaculation disorders, orgasm disorders, and decreased libido. [25][26][27]
Antiandrogens are classified as steroidal or nonsteroidal. Steroidal antiandrogens not only counter androgens, but also affect secondary sex characteristics. Steroidal antiandrogens directly affect gene expression due to their fat-soluble nature that allows them to diffuse through the plasma membrane’s phospholipid bilayer and prevent the binding of testosterone and dihydrotestosterone (DHT) to the androgen receptor.[7] Non-steroidal antiandrogens, or "pure" antiandrogens, such as nilutamide and flutamide, counter androgens and have no steroidal effects. Antiandrogens inhibit circulating androgens by blocking androgen receptors, suppressing androgen synthesis, or acting in both those ways.[8] The most common antiandrogens are androgen receptor (AR) antagonists which act on the target cell level and competitively bind to androgen receptors.[2]
Inhibition of androgen production occurs through a unique mechanism for each antiandrogen. For example, ketoconazole not only competes with androgens such as testosterone and DHT for androgen receptor binding, but also suppresses androgen synthesis by inhibiting cytochrome P450 and 17,20-lyase, which partake in synthesizing and degrading steroids, including the precursors of testosterone. The result is a decrease in the overall testosterone production of the adrenal cortex.[9] Gonadotrophins, pituitary hormones capable of altering androgen synthesis, are also affected by antiandrogens. Antiandrogens can have suppressive effects on gonadotropin secretion by down-regulating gonadotropin-releasing hormone receptors (GnRHR) in the pituitary gland. A decreased amount of GnRHRs results in gonadotropin-releasing hormone (GnRH) not being able to bind sufficiently. GnRH is responsible for the release of the gonadotropins luteinizing hormone (LH) and follicle-stimulating hormone (FSH). LH stimulates the Leydig cells of the testes and the theca cells of the ovaries to produce testosterone (and indirectly estradiol). Therefore, if GnRH cannot bind, testosterone synthesis is not induced in the testes or ovaries.[10]
Medical applications[edit]
Antiandrogenic pharmaceuticals are used to treat an array of medical conditions that are dependent on the androgen pathway. Antiandrogens are often prescribed for men with prostate cancer, benign prostatic hyperplasia, hypersexuality, male contraception, and for those that are undergoing gender reassignment
Pharmaceuticals for men[edit]
Antiandrogens in males can result in hyposexuality (diminished sexual desire or libido), reduced activity or function of the accessory male sex organs, and slowed or halted development or reversal of male secondary sex characteristics.[11]
Antiandrogenic drugs are often indicated to treat severe male sexual disorders, such as hypersexuality (excessive sexual desire) and sexual deviation such as paraphilia (a disorder involving intense recurrent sexual urges), since lowering male hormone levels decreases libido.[12] As a part of a program for registered sex offenders recently released from prisons, the offender is sometimes administered antiandrogen drugs to reduce the likelihood of repeat offenses by reducing sexual drive.[12] On occasion, antiandrogens are used as a male contraceptive agent.
Propecia Risks
Imagine a drug that shuts off androgen receptivity and production in the male body, literally castrating its users. Some might say this would be a perfect drug for repeat and violent sex offenders. However, someone got a better idea and decided to sell it to the general male public and all without mentioning any of the potential risks (Propecia in its hey day generated a little over $400 million per year in revenue.)
Yes, indeed, this castrating drug is called Propecia (generic name: finasteride) and you can buy it over the counter in countless stores for hair loss. As I cover in my link on Hair Loss, Propecia is rife with sexual side effects. Around one in ten men will experience significant erectile and sexual dysfunction after starting this nasty drug.
CAUTION: This drug is also sold under the trade name Proscar. Talk with your doctor before going off of any medication for prostate or other medical reasons.
Erectile dysfunction is just the beginning for many men. Around one in 50 will go on to experience severe androgen deficiency. There are many names for this, but Post Finasteride Syndrome has become quite common.
Do you know the foods and drinks that increase erection-boosting Nitric Oxide? Check out the Peak Erectile Strength Diet where I show you how to dramatically and naturally improve your erectile strength.
Regardless, what you call it, researchers do not really understand completely what is going on. Of course, Propecia is a strong anti-androgen that works by limiting 5 alpha reductase, the enzyme that converts testosterone to DHT. Propecia also binds to 5 alpha reductase and actually inserts itself into the same androgen locations. All of this results in some men in extreme and irreversible androgen insensitivity. Somehow permanent damage is done and, from what I have read, sometimes cannot be reversed with standard treatments given to steroid users who shut off their testosterone production.
The good news is that the industry is just now admitting the problem and a recent study in the Journal of Sexual Medicine admitted that permanent erectile damage did seem to be occurring with Propecia usage. [1] They even encouraged doctors to discuss these risks with their patients. Imagine that - discussing the potential risk of being chemically castrated before beginning a drug for prostate enlargement or hair lo
Adverse effects
Side effects of finasteride include impotence (1.1% to 18.5%), abnormal ejaculation (7.2%), decreased ejaculatory volume (0.9% to 2.8%), abnormal sexual function (2.5%), gynecomastia (2.2%), erectile dysfunction (1.3%), ejaculation disorder (1.2%) and testicular pain. According to the product package insert, resolution occurred in men who discontinued therapy with finasteride due to these side effects and in most men who continued therapy. The PPI also states that patients have reported persisting erectile dysfunction despite discontinuing the drug. In December 2010, Merck added depression as a side effect of finasteride.[14]
In November 1997, an FDA panel refused to recommend approval of the drug Propecia for male pattern baldness. Although it was not disputing its efficacy, the committee members expressed some concerns about the possibility of long-term side effects on sexual function and possibly even fertility, which arose because of some evidence of diminished ejaculate levels. [15]
