NEBIDO in Bodybuilding

Something odd happened with Nibido. Bodybuilders always closely monitored scientific development on steroids. These researches are meant to treat diseases or meant to develop a male anti-conception compound. Especially means against male hypogonadism had our warm interest. Bodybuilders in the past always experimented with testosterone, methyl-testosteron, dianabol etc. The pharmaceutical companies worked hard on means that required less labor (read injections) from doctors or nurses. Compounds like cypionate and enanthate where frequently used, but their kinetics where undesirable because of the quick peaks and downs, it caused an emotional rollercoaster with moodswings, and libido that was extremely high followed be a sexual disinterest. Organon developed Sustanon a compound containing four different testosterone esters that in theory caused a more stable testosterone level.

Sustanon actually had the monopoly as treatment for male hypogonadism. Then in 2003 Nibido hit the market. Because Organon had given many countries a license to produce Sustanon under different names in many countries it doesn’t bring much profit for the “Big Pharma’s. ” .

Sustanon was and still is used by many bodybuilders, life-extensionists and anti-aging guys. All these people want an increase in their testosterone level, but a desirable stable increase. Because a stable level also goes along with improved estrogen and other side-effects. I’ll go into that later.

We heard very little about Nibido as a compound to be used to increase musclemass in Bodybuilders. One reason could be Nibido was not approved for the USA and Canada and that is because Bayer from Germany has the rights on this compound. But the miracle just happened. In March 2014 the news came out that Aveed (called Nebido outside the Us) has finally been approved by the FDA. Another reason is the fact that it is a 4 ml amp that should be used at once (as a treat against hypogonadism) and Bayer warns that if you split the doses Nibido’s special advantages will disappear.

Aveed contains testosterone undecanoate, which Endo licensed through its subsidiary Endo Pharmaceuticals Solutions Inc. from Bayer Pharma AG. Outside the U.S., Bayer Pharma AG and its subsidiaries have been marketing testosterone undecanoate injections since 2003.

The US Food and Drug Administration (FDA) has approved testosterone undecanoate injectable (Aveed, Endo Pharmaceuticals), for the treatment of men with hypogonadism, but with a boxed warning and very strong prescribing restrictions. The FDA is requiring that Aveed's label contain a boxed warning regarding the risks of serious pulmonary-oil micro embolism (POME) and anaphylaxis and is making the product available only through a restricted distribution scheme known as a risk evaluation and mitigation strategy (REMS) to ensure that it is used only in men for whom the benefits outweigh the risks.

Aveed is a long-acting depot formulation of testosterone in castor oil and benzyl benzoate. It offers a novel dosing schedule, with a single 3-mL (750 mg) intramuscular injection given once at initiation of therapy, at 4 weeks, and then every 10 weeks thereafter.

Nibido is heavily hyped. And I can kinda understand it. Injections every 8-12 weeks is pretty nice - if it works that is.

Test is Test

Is this a new compound with magical properties? Nope!! Like I explained in “Common sense cycling” //juicedmuscle.com/jmblog/content/common-sense-cycling

Many things are known for years and part of normal (pharmaco)kinetics. Most bodybuilders are also aware of these facts. If you use longer slower esters the clearance and half-life rates are delayed. If you use carrier oils with a higher viscosity, inject more frequent or use higher doses. The kinetics change.

Depending on the compound manufacturing the half-life of testosterone enanthate is 10.5 days, from testosterone cypionate is 12 days, from testosterone Decanoate is 15 days. Then there's undecanoate which has a half-life reported of up to 16.5 days Pharmaceutical companies are completely aware of how the enanthate and cypionate ester is resulting in fluctuating mood, sexual performance, and energy levels, and they are looking at undecanoate as a solution.

The longer the ester, the more gradual the release of testosterone. Which of course means stability of serum levels. Once you are able to keep the blood-serum testosterone level completely stable, then everything else (estrogen, DHT, aggression, fluid retention, gynecomastia, etc). becomes easier to manage.

Study 1999 DESIGN: 8 injects van 125 mg/ml

In study I, 1000 mg TU in tea seed oil (125 mg/ml) were injected in equal parts into the gluteal muscles of seven hypogonadal men. In study II, 1000 mg TU in castor oil (250 mg/ml) were injected into one gluteal muscle of 14 patients.

RESULTS:

In comparison with published data on testosterone enanthate, most widely used for i.m. injections, the kinetic profiles of both TU preparations showed extended half-lives and serum levels not exceeding the upper limit of normal. The castor oil preparation had a longer half-life than TU in tea seed oil (34 vs 21 days).

CONCLUSION:

The longer half-life and the smaller injection volume make TU in castor oil a strong candidate for further applications in substitution therapy and in trials for male contraception.

The interesting thing is, that it seems that nobody ever tried to inject Nebido in multiple shots. I think it is just an esterified testosterone compound just like the enathate, cypionate or decanoate , but the manufacturer is building a myth around Nebido that it has some special properties when the 4 ml are injected at once.

Bodybuilders avoid AAS lows by injecting more frequently, maintaining an anabolic concentration. During an AAS-only cycle, bodybuilders endure two or more intramuscular injections weekly, depending upon the dosing schedule and number of AAS stacked. Competitive and more hard-core bodybuilders may compound this number with orals and/or injections of insulin, growth hormone, inflammatory agents, prostaglandins, etc.

I remember a cycle Brock Strasser posted about in his column “Strasseroids”. He called it Test Stand Alone. It was a very simple cycle. On the first week you injected 3 gram (3000 mg) of Sustanon and then the next 10-12 weeks you injected 1000 mg. We mostly used NILE Sustanon since it was very cheap at the time. Some tapered down with 100 to 500 to 250 mg. Others just let the long ester (decanoate) decrease and then started PCT. Others injected HCG at 500 iu E3D from week 2 until the end and then followed PCT. Reading the kinetics of Nibido, I thought that this compound would be better suited for such a cycle, creating such stable plasma levels.

And how about stacking Nibido with other compounds and orals?

There was a study made in China by Zang et al 1998 , where the hypogonadal men received 500mg instead of 1000 , but there was also a control group , receiving 1000 mg.

Quote: Pharmacokinetic analysis showed a terminal elimination half-life of 18.3+/-2.3 and 23.7+/-2.7 days and showed a mean residence time of 21.7+/-1.1 and 23.0+/-0.8 days for the lower and higher doses, respectively. The area under the serum T concentration-time curve and the T-distribution value related to serum T concentration were significantly higher following the 1,000-mg dose than following the 500-mg dose.

The 500-mg dose, when given as the second injection, yielded optimal pharmacokinetics (defined as mean peak T values not exceeding the normal range and persistence of normal levels for at least 7 weeks), suggesting that repeated injections of 500 mg at 6-8-week intervals may provide optimal T replacement.

This shows me that the half-life is getting a little shorter, probably because of the smaller surface, but anyways, it is working in smaller doses too. This leads me to my conclusion that there has to be a way to inject every 8 days approximately.

Let me quote an another interesting text, it is from Nebido’s own website:

Question: “What happens if only 1-2 ml of Nebido® (250-500mg testosterone undecanoate) are injected?”

Answer: “No clinical studies have been performed applying such regimens. It would lead to insufficient testosterone substitution requiring a shorter interval until the next injections and therefore losing one of the products main features, the long intervals of about 3 months between administration.”

Well, Now we have seen what the results are from the Chinese study with administration of 500 mg, followed by a 1000 mg injection and visa versa. We know what Bayer said about it AND in the USA the 250 mg/ml is available, just as UG Testosterone Enanthate. So what is stopping bodybuilders from experimenting with this compound?

Probably the price. It is very expensive. A typical fill can cost $882 or more for 1 vial (3ml) of Aveed 750mg/3ml. Nibido (1000 mg) in Europe costs around 200 euro. BUT… we can buy underground made compounds made by reliable manufacturers for only a fraction of the price, official manufacturers would charge you.

And that’s exactly why the FDA hunts down UGLabs.

Nebido testosterone preparation restores fat man’s health ..a case study

Overweight can be deadly, but the remedy – eating less and moving more – is more than some fat people can deal with. According to Russian endocrinologists working at the Research Center for Endocrinology, Moscow, injections of a slow-working testosterone ester can be a great help to people trying to lose weight, at least for overweight men. They published a case study in Arquivos Brasileiros de Endocrinologia e Metabologia.

The subject of the researchers’ case study was a 42-year-old man who weighed over 150 kg. He’s in the photo left[A]. The guy was not only overweight, but also ill. His blood contained more fat and cholesterol than doctors consider healthy; he had high blood pressure, was depressed and tired, had a reduced libido and impotence to boot. He was aware that he needed to lose weight, and had made unsuccessful attempts in the past, but by the time he became the subject of the study he had given up even trying to get more exercise or change his diet.

This may have been because he was suffering from depression, the researchers suspected. And that may have been caused by a low testosterone level – which is not unusual in obese men. This may have made him unable to make lifestyle changes, and why he continued to overeat. A vicious circle. But the Russians wondered whether it would be possible to break this with synthetic testosterone. They decided to give it a try.

They treated the man for sixteen months with Bayer’s long-lasting testosterone preparation Nebido. The active ingredient in Nebido is testosterone undecanoate. The doctors gave the man a 1000 mg injection in weeks 0, 6 and 12. Thereafter he was given a 1000 mg injection once every twelve weeks.

The researchers measured the man’s PSA level every three months. The more of this protein there is in your blood, the greater your chance of developing prostate cancer.

The man started to feel better immediately. He took up swimming twice a week and walking on the other days. He also started eating more healthily. The photo on the right [B] shows how the man looked after 16 months.

He became healthier, which is hardly surprising if you shed 50 kg surplus weight. Before the 16 months began he was suffering from metabolic syndrome, a complex of disturbances in the body caused by being overweight. At the end of the 16 months, the disorders had disappeared.

"The dramatic weight loss and recovery of the metabolic syndrome was unexpectedly quick and successful", the Russians write. "A case report does not allow to make far reaching conclusions as to the mechanism but it could be that, in addition to breaking the self-sustaining vicious circle of metabolic syndrome-obesity hypogonadal testosterone levels, the mood-elevating effects of normalizing testosterone may have played a role."

Source: Arq Bras Endocrinol Metabol. 2009 Nov; 53(8): 1047-51.