Wednesday, April 15, 2015

Dutasteride (Avodart) for blocking the conversion of the hormone Testosterone

Anabolic steroids are one type of performance-enhancing drug. They mimic testosterone in the body to enhance performance by making muscle cells larger and by allowing the body to recover more quickly from the stress of exercise.
Performance-enhancing drugs are no longer just for bodybuilders or pro athletes who are willing to try illegal and potentially dangerous means to improve their body's function. These drugs are being used every day by people of all ages, from middle-school, high-school and college students to older recreational athletes.
Dutasteride (Avodart) is a dual 5-a reductase inhibitor that inhibits conversion of testosterone to DHT. It was developed to treat benign prostatic hyperplasia (BPH), which is the enlargement of the prostate. Bodybuilders have used this compound to protect themselves from hair loss.

The difference between Dutasteride and Finasteride, is in the name. Dutasteride (dual-tasteride) works on both of the 5a-reductase enzymes, while Finasteride works on just one. Dutasteride has greater efficacy because of this, and it is more powerful at a lower dose. Treating symptoms of benign prostatic hyperplasia (BPH) or enlargement of the prostate gland. It also helps to reduce the risk of urinary blockage and the need for surgery to treat BPH. It may be used alone or along with another medicine (Tamsulosin).

Dutasteride works by blocking the conversion of the hormone testosterone to the more potent hormone dihydro testosterone. It does this by blocking an enzyme called 5-alpha reductase. Dihydrotestosterone is partly responsible for making the prostate enlarge. Therefore, a reduced amount of dihydro-testosterone in the prostate causes it to shrink. This helps you to pass urine more easily.

Sometimes, more than one type of medicine is needed to control the symptoms of prostate enlargement. Dutasteride is available in combination with another medicine for prostate enlargement, called Tamsulosin. The combination brand is called Combodart and it may give quicker and better relief of symptoms than either medicine alone.

To understand how Dutasteride works we must first learn about DHT. Dihydrotestosterone (DHT) is a sex steroid and androgen hormone. The enzyme 5a-reductase synthesizes DHT in the testes, hair follicles, adrenal glands, and prostate. Reductase inhibitors work by blocking the action of the enzymes that convert testosterone to DHT. This is why they work so well for protecting/re-growing head hair and helping with BPH. Dutasteride stacked with Finasteride can lower DHT in the body up to 95%.

When bodybuilders use anabolic-androgenic steroids, it can speed up head hair loss. This is due to increased testosterone hormones in the body. The more testosterone, the more conversion to DHT in the body. In addition, running DHT derivatives such as Masteron, Winstrol or Proviron will further increase DHT. To combat this, bodybuilders have experimented with 5a-reductase inhibitors, such as dutasteride, to protect their existing hair and even re-grow more. However, this can come at a price and a myriad of side effects.

Dutasteride has been used for acne control, as it will lower an overabundance of androgens in the body. Nonetheless, it’s not a very effective anti-acne drug, and its potential side effects aren’t worth the possible acne control.

Side Effects:

Preventing sex hormone DHT from being converted from testosterone might not be the best idea in the long term. If you care about your sex drive, Dutasteride might not be for you. The two main side effects from this drug are erectile dysfunction (ED) decreased sexual desire (libido). Additional side effects like gynecomastia can occur as well, due to severely low DHT levels. Even with short term use at low dosages, some users have reported serious problems problems with ED. Therefore, the user must be extremely careful when using duta, and use it only if absolutely necessary.

A dosage of 2.5 mgs per day is a popular starting point among bodybuilders. Most guys are splitting the dose into AM/PM, but that’s not necessary. The half-life of Dutasteride is very long – up to 5 weeks. So, you can dose it EOD (every other day) or longer if you wish.

Thursday, April 9, 2015

Synthetic cyclic heptapeptide Melanotan 2(MT2)

Melanotan 2(MT2) is a synthetic cyclic heptapeptide that is mainly used to increase tanning. It stimulates a natural increase in melanin production. Melanin is the main determinant of skin color in humans. Melanin is a brown pigment which causes skin to become darker in appearance when exposed to UV rays. According to scientific study that has been based on animal test subjects, the impetus of Melanotan 2’s overall functionality and mechanics can be tied to the pituitary gland. This pea-sized gland located at the bottom of the hypothalamus at the base of the brain essentially acts as the command center for the endocrine system, as it is chiefly charged with the regulation and control of several system-related functions including those related to growth, metabolism, thyroid gland function, and temperature regulation. Melanotan II’s relationship to the pituitary gland can be drilled down to a hormonal level; specifically, to hormones secreted by the pituitary gland known as melanocortins.

In essence, these particular hormones are responsible for the regulation and control of hair and skin pigmentation in an animal test subject. They achieve this measure of control by expressing melanin. The secretion of melanin is triggered by an animal test subject’s exposure to ultraviolet, or UV, rays. When the secretions are expressed, they are manifested upon the surface of the skin. This process in which this occurs is known as melanogenesis. The secretion acts as a natural means of protection against ultraviolet rays. This component, by extension, acts as a protective measure against a hot of various skin afflictions and ailments that result from prolonged exposure to ultraviolet rays. These rays include various forms of skin cancers. The primary issue with melanogenesis is the fact that the melanocortins that trigger this process has a rapid half-life that only lasts several minutes. Naturally, this means that the secretion’s overall effectiveness as a measure of protection against ultraviolet rays is very limited.

Melanotan II was first synthesized at the University of Arizona when looking at possible ways to treat skin cancer. They hypothesized that an effective way to reduce skin cancer rates in people would be to induce the body's natural pigmentary system to produce a protective tan prior to UV exposure.

Clinical trials have shown that Melanotan 2 safely promotes melanogenesis. This is a process were melanocytes produce melanin. Lighter-skinned people have low base levels of melanogenesis. Exposure to UV-B radiation causes an increased melanogenesis. The purpose of the melanogenesis is to protect the hypodermis, the layer under the skin, from the UV-B light that can damage it. It does this by absorbing all the UV-B light and blocking it from passing the skin layer.

MT2 has also been shown to have aphrodisiac effects. Giuliano F et al. showed MT2 exerting a dose-dependent effect on erections in anesthetized rats. They went on to show MT2 having inducer and facilitator activities on erection depending upon delivery route of the peptide. There are various studies showing similar results in both animals and humans. Wessells H et al. highlighted the positive effect MT2 has on sexual desire and erections in men suffering with erectile dysfunction and various organic risk factors.

Through clinical research it has been shown MT2 has excellent fat burning effects. It was previously thought that it assisted weight loss indirectly due to its appetite-reducing effect. However, it now appears that MT2 has direct fat burning effects. Strader AD et al. is a great example of the direct fat burning effect. They conducted a series of tests including one that shown MT2 treatment led to a general reduction in both visceral and subcutaneous fat tissue in high-fat-fed mice. Choi YH et al. also showed in addition to reducing food intake and inhibiting body weight gain, administration of MT2 reduces fat mass. They concluded this was most likely by accelerated lipid mobilization, but not by apoptosis (cell death).

A very interesting effect MT2 brings about is its ability to increase insulin sensitivity during researchers' trials. Heijboer AC et al studied the effects MT2 has on hepatic and whole-body insulin sensitivity. Results showed administration of MT2 increased insulin-mediated glucose disposal but did not affect the capacity of insulin to suppress EGP. MT2's acute effect on insulin sensitivity was further highlighted during studies done by the Nagoya University Graduate School of Medicine. Banno R et al.  examined the effects MT2 had on insulin sensitivity in diet-induced obese rats. The insulin tolerance test showed that insulin sensitivity was significantly improved in the MT2 group compared to the pair-fed group. Furthermore, MT2 treatment increased the number of small-sized adipocytes in epididymal white adipose tissues, suggesting that MT2 increased insulin sensitivity through action on the white adipose tissues.