Prototype Nutrition Ketoforce

Aug

29

Some information on methods of administering TRT (as asked to me by Dr. Pete)

By Patrick Arnold

Dr. Pete asked “Patrick, I’m assuming it’s not feasible to inject testosterone without some ester side chain, such as cypionate, else people would be doing it.

Do we know what happens to all of that cleaved off cypionate over time?
Any reason to prefer pellets or pure T cream over injection, given the need for an ester? “
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Free Testosterone has a solubility in oil that i believe is no more than 20mg per cc.   Also, having poor lipophilicity it is released quickly from the depot site and would require daily injections
Cyclopropionate (cypionate) is a safe fatty acid, albeit synthetic, When attached to testosterone via an ester bond the lipid solubility is increased  at least ten fold.   Heptanoate (enanthate) increases solubility even more so, and heptanoate (C7) is an endogenous and healthy fatty acid.    However, I don’t think with either of these esters the concentration should exceed 200mg per mL.  Greater concentrations may lead to to injection site inflammtion and in some cases even sterile abcesses.   Undecanoate esters may be an exception.
When you inject an anabolic steroid ester (in this case testosterone ester) dissolved in a vegetable oil or similar vehicle it forms a depot  that is dispersed in muscle tissue.    This oil depot generally stays put until esterases slowly release the free testosteone – and at that time the hormone enters the circuation.   This is what provides the prolonged release effect and alllows for less frequent IM dosing.   It should be noted that some ester itself may release “as is” and then hydrolyze rapidly in the blood, howerver this is more likely to happen with less lipophilic shorter chain esters.
Still, the pharmacokinetics of most test esters (propionate being the worst and undecanoate being the best currently on the market) all have an initial burst release of hormone over 24 to 72 hours followed by a more or less logarithmic decline.  This results in a a patient feeling great effects for five days or so, and then by the 2nd week they are hypogonadal again and feeling not so great
  Pellets are designed to release a testosterone that is pressed in a manner (layers of concentration) such that after admistration into the muscle (or subQ)  a more steady state level can be acheived for a longer period of time.   The pharmacokinetics are better than esters in oils and the frequency of adminstration is months instead of weekly or biweekly.  Unfortunately they are adminstered using a large trocar which some people may find scary, and I am assuming there is considerable irritation for a period after the pellets are inserted as well
Creams / transdermals are the superior choice for pharmacokinetics and patient comfort.   They are applied once a day and after a few days a steady state of testosterone will be acheived in serum.   This is due to the fact that it takes time for the hormone to penetrate the stratum corneum and reach the dermis and epidermis where blood vessels are plentiful. Hence,  the skin itself provides a depot effect with reliably consistent release.   These formulation do have downsides too as you probably guessed.   About 90% of the testosterone never makes it to bloodstream and a considerable amount remains on surface of skin.      From an economic perspective however that lost 90% of hormone – USP testosterone is cheap (well  it should be) – I believe is irrelevant.   What is highly relevant as most people know is any in advertant transfer of  testosterone sitting on the skin to other individuals who should not be exposed to any considerable amount of the hormone.   At the top of the list of course are infants.   Pregnant women may or may not be a problem.  Pregnant women actually have elevated testosterone compared to normal women, and normal women shouldn’t be at much risk, unless the contact is in the genitalia area. The clitoris is highly sensitive and direct exposure to androgens may cause clitoralmegaly (growth of the clitoris)

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