Archive for June 2015

Letrozole-femara

Letrozole~femara

Letrozole (Femara) is the chemical name of Novartis´ selective third generation Aromatase Inhibitor (AI). This drug was developed to fight breast cancer by inhibiting the aromatization. It is usually used as a part of an aggressive treatment in post-menopausal women, to fight and reverse the spread of breast cancer after other treatments (such as Tamoxifen therapy) has failed. It´s probably the most efficient product on the market for this purpose currently  It is very similar in structure and action to it´s predecessor Arimidex.

Letrozole (Femara) also does quite a few things which would be of interest to both bodybuilders and athletes.

Firstly, it has been shown to reduce estrogen levels by 98% or greater . In at least one documented incidence, Letrozole (Femara) reduced estrogen in the test subject to undetectable levels, and increased LH, FSH and SHBG. Clearly this is all of interest to bodybuilders, as less estrogen in the body means less chance of certain side effects such as water-retention, Gynocomastia, and acne.

This makes Letrozole (Femara) an appropriate choice for even the heaviest bulking or cutting cycles including harsh androgens. Also, if you are a competitive bodybuilder, Letrozole (Femara) is a must have product for contest prep; no other Ancillary compound will produce a dry and tight look like Letro will.

 

An effective dose of Letrozole (Femara)

is .25-.5mg/day (I use .25mgs/day), but be forewarned, if you go over that amount, it can kill your sex drive. Also worth noting is that there´s a rebound effect on your estrogen when you come off Letrozol. Maximum inhibition of the aromatase enzyme has been found to happen at doses as low as 100mcg!

Letrozole (Femara)´s effects on serum lipids (cholesterol, both HDL and LDL) are, in the words of one researcher: “inconsistent. ” Clearly, however, you´ll eventually suffer an impaired lipid profile and immune system if you keep your estrogen levels too low for too long. Your sex drive will also probably suffer from extraordinarily low levels of estrogen present.

As previously mentioned, Letrozole (Femara) can be used to raise LH and FSH (which are hormones which signal your testes to produce more testosterone). It also, of course, will raise your testosterone levels (6) via this mechanism. Again, this is of interest to athletes and bodybuilders for obvious reasons. Letrozole (Femara), of course, can be used for post-cycle-therapy (PCT) to raise test levels, but for various reasons, Tamoxifen may be a better choice. Still, I have successfully used Letrozole (Femara) for this purpose.

How good is this compared with Aromasin and Arimidex, it´s too other main rivals? Well, In non-cellular systems, Letrozole (Femara) is 2-5 times more potent than anastrozole and exemestane in its inhibition of the aromatase enzyme and activity, and in cellular systems it is 10-20x more potent! It also lasts quite a long time in your body,but takes awhile to get going& Letrozole (Femara) has a whopping 2-4 day (!) ½ life, and you need to take Letrozole (Femara) for 60 days to get a steady blood plasma level.

Those are impressive numbers, but here´s one of the most interesting things about Letrozole (Femara):

It may reduce/eliminate/reverse existing gynocomastia!

In a study conducted on mice (*no, I know it´s not perfect), gyno-like-changes in the mammary gland were totally destroyed! Here´s a direct quote from that study:
“Our results also indicate aromatase overexpression-induced changes in mammary glands can be abrogated [destroyed] with very low concentrations of the aromatase inhibitor, Letrozole (Femara).”
In addition, I´ve used Letro to get rid of my own gyno, as has a friend of mine, and we both used it at a dose of 2.5mgs/day, tapering down to .25mgs/day, and then finally off..the gyno never returned in both our cases.

I´d say that this stuff is pretty great, considering its availability and cost (when you consider the fact that .25mgs/day is more than enough protection from estrogen-related sides on most cycles), not to mention it´s overall utility for a variety of functions (destroying gyno, preventing estrogenic sides, and for PCT).

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Melanotan II the breakdown

Melanotan II the breakdown

Melanotan is a peptide that is produced in the body as a way of making an animal’s skin tan. This is used as a response to exposure to UV rays to protect the animal’s body against skin cancer and other damage. This chemical has been synthesized as Melanotan 2, which was developed by researchers at the University of Arizona. This synthetic analog mimics the behaviors of the melanocortin peptide hormone alpha-melaocyte stimulating hormone.

The synthetic version of this peptide has been found to produce similar melanogenesis effects and aphrodisiac effects in animal test subjects, in the initial clinical trials that have been performed. To date, no compounds that contain melanotan 2 peptides have been approved for human use as clinical trials are still ongoing. However, initial research indicates that this peptide may be very useful in preventing a variety of cancers and other diseases if the effects of it can be regulated to minimize side effects.

This has increased the desire for bulk purchases of this peptide. There are a variety of ways to secure melanotan 2 for research purposes, but a great deal of care will need to be given in order to ensure that the product you purchase is the proper quality for this purpose.

Warnings for Melanotan Shoppers

 

Because products containing melanotan have not been approved for the public market, the variety of products that claim to contain these ingredients actually don’t.

Products that contain any form of melanotan 2 are not allowed to be sold for human use; there are a variety of items online that claim to contain this ingredient because they have been manufactured in markets that do not have a ban on melanotan.
In many cases these products contain fraudulent ingredients that are designed to mimic the effects of melanotan 2 to take advantage of less than credible customers. There are a variety of regulatory bodies that are currently attempting to catalogue these products and issue a warning to those that might attempt to purchase them due to the severe risk of interacting with these unknown chemical mixes.
Those that are investing in melanotan as part of a research study can save a great deal of money and time by purchasing stores of melanotan from internet retailers, but the same risks that are posed to customers attempting to bend the rules may apply to these research facilities as well. If a product claims to contain melanotan 2, but is actually a counterfeit product, it could throw off research results. This could also pose a danger for animal test subjects which could experience unpredictable side effects that could be life threatening.
In order to eliminate the risk of working with counterfeit products during research, scientists should only purchase melanotan 2 from companies that are certified to sell research quality peptides.

These products will be sterilized and contain a specific list of the methods used to create the peptide so that researchers can ensure that they can predict how these chemicals will behave in chemical trials when they are applied to animal test subjects. This will also ensure that any bulk purchases are consistent to avoid any potential for an alteration of reactions during clinical trials that cannot be accounted for.

Evolution of Melanotan Development

Pilot studies using cylic heptapeptide analogs of aMSH and melanotan 2 have found to have super potent melanotropic activities in vitro.

Aingle blind studies utilizing alternating day trials with placebo controlled trials were conducted on male animal test subjects with initial applications of .01mg/kg of melanotan 2. Subcutaneous injections of saline or melantotan 2 were applied daily during weekdays for two weeks.
Two of the test subjects saw an increase in the increments of melanotan applications with .0005, .03 and .025mg/kg applications given throughout the length of the study. In these two subjects, .03mg/kg applications and higher were found to cause fatigue and somnolence.
Test subjects given applications of melanotan also showed signs of mild nausea at most dosing levels. Stretching and yawning complex appeared to correlate with applications around 1-5 hours after the chemical was applied. However, the length of time between these reactions appeared to correlate with the size of the application of melanotan 2 that was provided.
Of the three test subjects that were used in this study, two saw increased pigmentation around the face and upper body which was determined by comparing pictures of the test subjects against visual perception a week into the study. This was also compared a week after applications of melanotan 2 had ceased. These results help to demonstrate the tanning ability of melanotan 2 at 5 low applications up to 5 days of subcutaneous injections can provide.

It is currently recommended for future animal research that applications begin at single applications of .025mg/kg a day in animal test subjects, though this can be increased– based on the animal’s reaction to the chemical and the size of the test subject.

Additional Considerations for Melanotan Research

Much of the research surrounding melanotan focuses on mimicking the peptides that are naturally found in animal skin, but there are some uses for this product that could pose for additional promise for the future use of melanotan 2 products.

Melanotan was initially designed to mimic the chemicals in an animal’s body that are used to darken the skin tone as a protective barrier against UV rays from the sun. This pigment can also be released after the skin is damaged, which can lead to the pigmentation which is shown in an area that has been scarred, though this is an effect that need not be replicated in a pharmaceutical setting.
If this reaction can be mimicked with an artificial version of melanotan 2 it could be used as a means of tanning the skin to prevent damage, including skin cancer, which is caused by overexposure to the sun. Some would also like to use melanotan 2 for cosmetic reasons, causing the skin to take on an attractive tan color without the unnecessary risks that are associated with staying out in the sun or using tanning beds.
At this time melanotan has not been developed to the point where it can create a controlled reaction by an animal’s body, which is restricting researcher’s ability to release products containing this peptide to the public.
Because melanocortin naturally has a very short half-life, the peptide has been altered to create melanotan 2. This altered chemical composition has been found to be helpful in creating a peptide that has a longer shelf life and effectiveness when exposed to the bloodstream. These altered chemical bonds within the peptide have been found to have alternative effects, when exposed to animal tissues. This altered reaction may be helpful in allowing this peptide to be used for previously unpredicted chemical reactions.

Melanotan has been found to cause a variety of side effects in test subjects during clinical trials. Even low applications in animals could cause nausea, stretching and yawning. Male animals have also been found to experience spontaneous penile erections when they are exposed to melanotan 2 applications.

These side effects on their own are not typically considered to be dangerous for test subjects involved in this research, but it is believed that larger applications could impact the severity of these side effects, which should be accounted for when working with a variety of animals during study.

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