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Propecia started out as an observation made by a scientist/doctor called Pindaros Roy Vagelos. Pindaros, while working as the research chief for the pharmaceutical giant Merck in 1975, came across a presentation about a group of children in the Caribbean. The presentation related a rare genetic mutation in the enzyme 5a- reductase (5aR), which is responsible for converting testosterone to dihydrotestosterone (DHT), and many other hormonal actions.  The children were subject to medical attention throughout their development, and observed to have smaller prostates and full heads of hair!

Thus the reduction/inactivation in the 5aR enzyme due to genetic mutation had been observed to cause reduced prostate size and reduce male pattern baldness.

Dr Pindaros was excited to see this correlation, and he began working on a drug that could be used in older men for exactly that purpose, reducing prostate size. This drug, called finasteride would be approved in 1992 by the US FDA (17 years later!), and marketed as Proscar (5mg), for the treatment of benign prostatic hyperplasia.

In 1997, the FDA approved the use of Finasteride for male pattern baldness as well, this time as a 1 mg tablet under the brand name Propecia. (Same drug, different dose, application, and name)

The drug Propecia (as well as the generic Finasteride and brand Proscar) should not be used by women or children, as it will cause the adverse development of the developing foetus or child.   This is true in humans as well as female rats, in which low doses of the drug have produced serious complications in the sexual development of male rats.

 

 

Comparisons of the normal male hairy scalp, with that of balding men, revealed that the balding scalp contained increased amounts of DHT, and smaller hair follicles, so called miniaturised follicles.
The drug works by inhibiting the enzyme 5a-reductase (5aR), which converts testosterone to DHT. It specifically targets the 5aR isoenzyme 2 (variation of the enzyme), but there are three 5aR (actually 5 if GPSN2 and GPSN2L proteins are included) isoenzymes, type1, 2 and 3 all of which the drug targets to varying degree. This decreases DHT levels throughout the body, but in particular in those tissues where 5aR is more concentrated, such as the prostate, hair follicles, adrenal glands, and testes. Type 2 is predominant in hair follicles, seminal vesicles, epididymides, prostate and liver, while type 1 is found primarily in sebaceous glands of the skin including liver and scalp.

According to Merck, Propecia has 100 times more affinity for type 2-5aR over type 1- 5aR in native tissue of the male scalp and prostate. Other studies demonstrate preference to type 3 isoenzyme as well, but these were conducted on human embryonic kidney cells genetically engineered to express the 5aR enzymes, and not native tissue.
The truth is that the isoenzymes of 5aR have been found in most tissues of the human body, where they obviously play a critical role in regulating the hormonal balance in these tissues.

Also known is that 5aR will bind many other hormones, not just testosterone. For example, it will also bind, progesterone, androstenedione, epi-Testosterone, cortisol, aldosterone, and deoxycorticosterone. It is also largely true that the physiologic role of these other 5aR metabolised hormones remains to be clarified.

Vague assumptions about their role in the human body can be drawn from the prevalence of these hormonal metabolites in different tissue.

For example the aqueous humor (watery part between cornea and lens) of the eye contains dihydrocortisol, which is synthesised in the lens, thus it may play a role in production of aqueous humor and lens function.

Similarly the kidney will increase synthesis of dihydroaldosterone when sodium intake is restricted, suggesting it plays a role in sodium conservation.

5α-dihydroprogesterone (5α-DHP) is a major hormone in the circulation of both normal cycling and pregnant women, so it obviously has a purpose, yet another reason women should not take Propecia!

For both men and women, it may have the effect of producing feelings and emotions related to “social isolation” (see side effects section). 5α-dihydroprogesterone is also a negative allosteric modulator (reduces effect) of GABAa-rho receptor. This receptor is found in very high concentration in the retina of the eye (the light sensitive layer in the back of the eye)- (see side effects section)

Propecia Effectiveness Declines After 2 Years!

Propecia was originally evaluated in 3 studies involving 1879 men (88% Caucasian) aged 18 – 41 with mild to moderate male pattern baldness. This involved what is known as double blind (neither the patients nor doctors know who is getting what), randomized, placebo (some do not get the testing drug) controlled studies. The study lasted for about 5 years, in which various groups were given 12 months of placebo followed by Propecia for 12 months and vice versa including other combinations. The results indicated that hair count was higher in the groups that were given Propecia compared to placebo.

The maximum improvement occurred over the first 2 years, after which improvement declined, and men started to lose hair. They still had more hair than the placebo group, but the fact is, Propecia could not stop the hair number reducing with years to come.

An interesting observation of the above mentioned studies was the hair number comparison of men started on Propecia initially compared to those started on placebo initially and then given Propecia in the 12 months after the first year on placebo.

The men receiving Propecia from the beginning had 91 hairs above baseline at the end of the 12 month drug treatment, compared to 56 hairs above baseline at the end of 12 months for placebo (in an area equal to a circle with diameter one inch on balding scalp = 0.78 inch squared = 5.03 cm squared). This advantage for men initially started on the drug as opposed to placebo lasted for the duration of the trial.

It would appear that the stress of losing hair while believing one is receiving cutting edge scientific hair loss drugs, had its toll on the men receiving the placebo during the first 12 months. The stress of seeing hair fall out, even after the “last hope” of saving what was left had obviously impacted this placebo group in a negative psychological way.

If anything, what this proves is that stress will indeed make hair fall out. Another observation is that the initially “stressed” placebo group did not recover in subsequent years, their absolute hair count per area remained below that of the group that received the proper treatment from the beginning and thus saw “stress free” improvement and gained confidence in saving their hair from the beginning.

Not surprisingly, the men who were receiving the placebo for the full five years were less in number at the end of the trial, than those that continued on the Propecia throughout the 5 years. This is not to say that all the men that started on Propecia stayed for the duration of the 5 years. Indeed 50.58 % (about half) had remained after 5 years on the drug, compared to only 31.91% (less than one third) on placebo after 5 years.
Thus it is noted that approximately half the Propecia treated men from the beginning had dropped out by the 5th year. Could it be due to the fact that, as stated, after the initial 2 years there is a decline in the ability of the drug (efficacy) to prevent hair loss?
Indeed that is true. But that is not the only reason why many men would drop out of such a clinical trial. The other major reasons people drop out of these trials (more often than not dangerous), apart from failure to see desired results, are the intolerable “side effects”, and less often personal issues such as moving to a new country, or state, or not having any confidence in the people administering the treatments.

Contrary to what Merck says, these side effects could last a lifetime, and some might even kill you!
As outlined above, the 5a-Reductase enzymes that this drug targets are found in tissues all over the human body. One might conclude that there would be some serious side effects from such a drug tinkering with the hormonal signals in so many tissues. The answer is of course there are serious side effects.
Here is a list of symptoms determined while testing the drug (In clinical trials over a few years)
Propecia 1mg tablet % side effects after 1st year:

• Impotence 1.3%
• Decreased libido 1.8%
• Decreased volume of ejaculate + ejaculation disorder: 2%
• Other issues related to adverse sexual experiences: 1.2%

Eye and vision problems, this is not reported by Merck, but complaints are abundant! (Remember that hormone found in the eye? Dihydrocortisol)
Breast (chest) cancer, breast enlargement and tenderness: not reported as a percentage for Propecia but in one study, 4 males on Proscar (same drug higher dose) developed breast cancer as opposed to none in the placebo group.

Below is the same drug (brand name Proscar). The only difference is the dose, and is directed to males with prostate enlargement, as opposed to Propecia which is lower dose directed to males with hair loss issues only.
Clearly we can see a rise in adverse symptoms as concentration rises.

Proscar (same drug 5mg tablet) % after 1st year

• Impotence 8.1%
• Decreased libido 6.4%
• Decreased volume of ejaculate + ejaculation disorder 4.5%
• Antisocial or non-interest in other people
• Eye and vision problems:

Eye  problems are not reported by Merck, but complaints are abundant! (Remember that hormone found in the eye? Dihydrocortisol)

Breast (chest) cancer, breast enlargement and tenderness 0.9% (We will examine how this might be possible). In years 2, 3 and 4 this raises from 0.9% to 2.5%.

Prostate cancer: This was conducted with healthy men (no prostate problems) over 55 years of age. At the end of 7 years 4 men on Proscar had developed prostate cancer as opposed to zero in the placebo group! Another 5a reductase inhibitor, Dutasteride, gave similar results, with double the amount of prostate cancer in the drug group compared to the placebo.

These results signify the importance of 5a-reductase in preventing prostate cancer, and its inhibition only promotes prostate cancer in vulnerable or susceptible populations.

Merck markets these drugs as preventing benign prostatic hyperplasia, and states they are not meant to prevent prostate cancer.
Merck also states that, quote: “The clinical significance of these findings with respect to use of PROPECIA by men is unknown”.
In other words, in high doses it can cause prostate cancer, but in lower doses they don’t know. (interesting, dont you think?)

 

 

These are real world symptoms reported by the real world population after the drug is approved for sale by the US FDA, and subsequently marketed to doctors who then prescribe it to the every day Joe.
These reactions are reported voluntarily by men to their doctors, who then report back to the pharma industry.
In addition to all the above mentioned side effects that were known from the clinical trials, the following were also reported by real men.
Hypersensitivity reactions:
Rash
Pruritus (Itch sensation – often associated with systemic conditions)
Urticarial (Hives, or pale red raised itchy bumps)
Angioedema (swelling of internal organs)
Swelling of lips, throat, tongue, and face.

Reproductive symptoms:

• Male infertility
• Poor semen quality
• Testicular pain

 

Nervous system / psychiatric;

Remember those GABAa receptors in the brain? Well 5α-dihydroprogesterone, one of the metabolites of the enzyme 5a reductase that Propecia inhibits, is its positive allosteric modulator. This means that it prevents neurons from “firing” more effectively, and creates a sense of “relaxation”. Without this the opposite would occur, one would be more susceptible than usual to stress and irritation.

Depressed patients, like socially isolated mice, show resistance to GABA anxiolytic and sedative inducing drugs. In other words, the reduction of these “relaxing hormones” in the brain would cause a certain down regulation of the receptors and possibly some resistance to relaxation and good feelings.

Depression (associated with anxiety and dysphoria in humans)
Anxiety, worry, inability to relax
Inability to relate or feel emotions to loved ones
Dysphoria (un-satisfaction with life)

Neoplasms: These are directly related to lower DHT.
Male breast cancer (Merck did “not know” the significance of its findings with Proscar for men taking Propecia. It seems the real men know. )
Breast disorders: Lower DHT.
Breast enlargement and tenderness.

Eye problems:
Inability to focus, as in when reading close to face
Bad night vision (remember the receptor in the retina?)
Kidney problems:
Many research articles have documented low androgens with increased kidney damage. Propecia is essentially lowering a potent androgen DHT.
Men report problems and pain in their kidneys, and certain studies have raised this point.

Androgen Deprivation Therapy (ADT) and Risk of Acute Kidney Injury in Patients With Prostate Cancer (JAMA. 2013; 310(3):289-296)

Conclusions and Relevance: “In a cohort of patients with newly diagnosed non-metastatic prostate cancer, the use of ADT was significantly associated with an increased risk of Acute Kidney Injury. These findings require replication in other well-designed studies as well as further investigation of their clinical importance”.

 

Take the poll, but…

 

This Drug Was Originally Aimed At Men with Benign Hypertrophic Prostate, or Benign Prostatic Hyperplasia (Non-Cancerous Enlargement of Prostate)

It was by accident that its effect on hair loss was observed.

What If I Told You: DHT Is Not The Cause of Prostate Enlargement?

You’re probably thinking you don’t care about prostate enlargement (yet), or cancer, right?

You only care about “male pattern baldness”
This information will surprise you!

 

 

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