Testosterone Undecanoate formulations, oral pills, and intravascular. Is this going to be an extra that safe, effective, and ethically used? And we’ll see why this ester of testosterone is not utilized extensively by bodybuilder’s powerlifters, strong men, and people looking to use other forms of testosterone esters for muscle building?
This is going to be focused on utilizing testosterone undecorated pills and intramuscular formulation for testosterone replacement for men that are hypogonadism, perhaps.
Testosterone Undecanoate History
- 1 Testosterone Undecanoate History
- 2 What is testosterone undecanoate used for?
- 3 Testosterone undecanoate Dosage and Half-life
- 4 Testosterone undecanoate Oral Safety?
- 5 Increase in DHT vs other esters
- 6 Is it worth taking testosterone undecanoate?
The history of Testosterone Undecanoate goes back to the 1970s, where it was introduced to the medical community in China, is it in a muscular formulation and then later in Europe as a pill oral formulation?
The greatest use, though, in the world that people are aware of is the utilization of this form and a brand name called Nebido intramuscular formulation in Europe and outside of America. It’s amazing that in America, the pharmaceutical companies tried to get a tag in this and try to get it passed through the FDA for many, many years and Aveed came into the market. Intramuscular testosterone underway in March of 2014 by Endo Pharmaceuticals. It was delayed for years and years as there was a safety issue, secondary to an anaphylactic reaction, secondary to pulmonary oil, micro embolisms. The FDA finally approved it after looking at the safety history at a smaller dose and a just less frequent dosing schedule, 750 milligrams intermittently injected every 10 weeks versus one gram, infamously injected every 10 to 14 weeks.
For Nebido outside America, the oral formulation of Testosterone Undecanoateis has been used for years as Andriol all in Europe. It was approved in America in March 2019 by the FDA as a brand name, JATENZO by Clarus Therapeutics. The pharmacology of testosterone undecanoate is in the oral formulation. It’s dissolved in oleic acid, castor oil, borage, seed oil, and peppermint oil. This makes for very fast absorption in the GI tract, and it bypasses the first-pass effect in the liver as it’s uptaking in the small bowel by the lymphatics.
What is testosterone undecanoate used for?
Aveed, Jatenzo, Nebido, and Andriol (testosterone undecanoate) medication is used by men who have low or no testosterone due to certain medical conditions (such as hypogonadism). Testosterone belongs to a class of drugs known as androgens. It helps the body to develop and maintain male sexual characteristics. Testosterone undecanoate is longer acting ester with a half-life of approximately thirty-four days.
Testosterone undecanoate Dosage and Half-life
Testosterone undecanoate dosed with food twice a day. The inner muscular formulation, which is so amazing that one aurally is super fast in her muscle formulation, is super long, the absolute longest ester in the world for testosterone. It’s slowly absorbed from the intramuscular injection in the glutes. Half-life is 34 days and it’s castor oil. This is amazing. That versus the other, more classic esters of testosterone, cypionate, and enanthate that are dissolved in cottonseed, linseed, and even grapeseed oils.
The approximate half-life of cypionate and enanthate is about seven days.
Testosterone undecanoate Oral Safety?
The safety issues are very interesting. The oral delivery mechanism of this medicine needs to be distinguished from oral anabolic androgenic steroids and that they never make it.
This medicine does not make it in the first pass effect into the liver because it’s up taken by the lymphatics out of the small bowel very quickly. So that does make it safe. And you would think doctors would think and people would think this is an oral anabolic steroid. It’s under that classification. So it’s going to be dangerous to the liver. It is not.
There are two studies that I’d like to use to point out. 2013 in the UK and in 2018 the United States, where an oral formulation of testosterone undecanoate was used for the treatment of non-alcoholic steatohepatitis, otherwise known as the initial stage of non-alcoholic fatty liver disease.
Now, this is where people have metabolic syndrome and they have liver disease, fat infiltration into their liver, secondary to being overweight. 30 million people in the United States as per the data based on the company that is doing this research. So isn’t it amazing that this drug and oral formulation of testosterone, not only are it orally safe and safe for the liver, it may be used one day to treat very common liver disease, non-alcoholic steatohepatitis?
We have to so focus on technology and you have to focus on aspects of clinical medicine here.
Side effects and safety continued for the oral formulation of this medicine as per the inbox warning for this formulation of oral testosterone. Hypertension is a black box warning.
In addition to other side effects that we would see with any formulation testosterone:
- Increase in CBC
- Androgen-induced polycythemia
- Sleep apnea
- Cardiac effects
- Increasing LDL
- Lowering HDL
Now, my feeling is that apart from hypertension, I think this utilization in this type of testosterone, Ester probably is going to be the same as far as safety with any other formulations taking testosterone injections, cypionate and enanthate you definitely can get hypertension. So I think the studies they presented to the Fed in America showed hypertension and the other studies that were also done so long ago for cypionate and enanthate, the Fed just didn’t see or notice or were aware of hypertension. But if they did it today, you’d see hypertension along with all the other aspects. So so far, oral formulation, I think, is safe so far.
Increase in DHT vs other esters
One amazing piece that they come up with is that the increase DHT levels that are derived secondary to the oral formulation are higher and they don’t compare to cypionate and enanthate. But they mention in the literature that I read carefully that they’re higher now.
Could that end up being better for Mood and libido?
It could be. That’s DHT is certainly one of them. And target antigens that stimulate the central nervous system, not to mention the muscles and why men feel good. This is why it’s used. Now, it’s not going to be good for hair. Absolutely. Maybe not even good for acne, because acne is going to be the interplay of stimulating the situation to produce acne. Voulgaris It’s not just estrogen guys. It’s going to be an interplay of androgens, testosterone in the end, and DHT, no question.
And there’s so much genetics involved in this. But one of the interesting safety concerns I would think is an expert in testosterone replacement for men is that increases DHT level systemically. Is it going to affect the prostate BPH and also worsening prostate cancer?
If a man has a malignancy when he starts testosterone, this is what we know today. But the literature says that the DHT that’s derived systemically from this or formulation does not increase DHT in the prostate.
Now, I want to get more discussion on this. I want a Ph.D. in pharmacology and other experts in the world to explain this more to me and you and to all of us. Is this going to be a concern in the future?
Can the brain feel better because DHT levels are up?
We know that’s potential and also potentially some mood problems from too much DHT. This is going to be the man for man, but will it worsen BPH enlargening a prostate or causing worsening prostate cancer if a man has it?
We have to think about this. Safety concerns for the intermuscular formulation right up front is going to be pulmonary micro oil embolism and anaphylactic reaction. This is why the FDA in America held up the approval for so long.
Now, when you look at other anabolic steroids, let’s think about Tren. But even with small injections of testosterone men have this coughing pulmonary response.
Is it from benzyl alcohol?
Because I’m assuming there’s a lot of benzyl alcohol that’s in this intramuscular formulation. So we don’t know and if you look at what happened in the studies, the attention to detail of exactly where and how this delivered in an intramuscular is so important, it has to be in the glue. It’s 750 milligrams to America and gram in Europe. You can’t put that much. I believe it’s three mills, you can’t put that much in your deltoid or the vast laterals, it has to go into the glue.
So think about it. How can you make sure you’re aspirating first with that type of intramuscular administration and the safety of that and the technical ability of the person giving it?
This is why it’s stated that it has to be done in a doctor’s office. You have to be observed after every injection for the side effects. Amazing. So this is again in the future. Why four guys that want to do it at home and do it more regularly.
It’s safe with small intermediating esters versus this, which cannot be given by a man himself, although I’m sure men will do it, but needs to be the limitation is in a doctor’s office and observe the side effects.
Now, the key to the safety of intramuscular with all the other aspects from hair loss, mood changes, CBC issues, polycythemia, coronary artery disease, sleep apnea, prostate, in my opinion, it’s going to be the same.
I think what’s missing here is that looking at formulations of shorter-acting esters, cypionate, and enanthate, versus this very long-acting tester, is the free testosterone. When they presented their data for Effectivity, they showed it on a scale of total testosterone, not free. We know that one of the reasons why men feel so much better on small doses, micro-dosing, if you will, of testosterone esters, cypionate, and enanthate is because the free portion goes just up higher, just slightly elevated compared to the total.
That’s it. We don’t see the data is not talked about. No, doctors are talking about that. That’s going to be the difference you’re going to see across the board for the free beyond this potential anaphylactic delivery. And affectivity let’s go into that right off the bat. You’re going to see that.
Is it worth taking testosterone undecanoate?
Is it effective to the man mind taking injections himself for men that don’t want that, this is going to be a great alternative to them having it done every ten weeks in America and Europe, every 12 weeks, for example, there is a slight difference. They call it seasonal in Europe.
The difference will be, in my opinion, that because we don’t know this in America, because it’s so new and people haven’t been using it, I think that will change that. The free testosterone with this long-acting, Esther, is not going to go up because of the castor oil, because of the pharmacodynamics it’s not going to liberate as it does quickly and launch off regularly as we do with the other esters and with those small esters. That’s why men feel great. So that’s the difference. Is free testosterone. No question. I look at labs. I’ve been doing it for years, always seeing a disparity between the total in the free, of course, the sex when buying and is involved here.
So it’s going to be interesting. Does this long, Esther, push down Sex Hormone Binding Globulin (SHBG) as it does?
We see with a shorter-acting ester that’s to be seen and discussed.
The effectiveness of the oral formulation is too new for us to discuss. But I think apart from the dosing schedule, that you have to take this twice a day with fatty foods and the cost. A lot of people can’t take medicine once a day. They forget.
Now, you imagine you have to take medicine twice a day that’s going to affect this medicine and the future use. And of course, until it’s generic, there’s going to be some cost. But for some men, this definitely will be a great alternative.
It’s another great tool in our bag for offering men testosterone and again, free testosterone levels. We just don’t have any data on that, on the oral formulation verses we know that intermediate contracting esters are higher. And, in my opinion, women feel better and you can control it.
Now, those DHT levels with your formulation, could this be a game-changer for men that feel better with just higher DHT levels, apart from worsening hair, acne, and the prostate? We just don’t know. The last piece is there is an ethical consideration. If you look at the inbox warning, it says contraindicated for women, children, and adolescents. There is evolving literature and a consensus in America and I’m sure abroad that testosterone esters and this is going to be a big one for this, for transgender women to men are going to be used.
So we don’t know. And I’m presenting this just simply presenting this as ethical considerations. We don’t have any long-term outcome data on giving women long-term androgens, we have to be very careful with this, I think because we don’t have data and this is going to happen in the future. So we’re going to see what’s going to happen to these people using esters of both enanthate and cypionate and this long-term type ester on someone’s health over decades.
So thank you so much. I hope this article helps men in the world that are interested in seeing another alternative form of testosterone delivery.