Nebido (testosterone undecanoate) profile , dosage , history and administration

akn · Jun 11, 2014

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Nebido® is an injectable steroid that contains testosterone
undecanoate, a very slow-acting ester of testosterone. This is
the active drug that is used in Andriol, but in that case it is
part of an oral medication, not an injectable. Nebido is being
marketed as a replacement for established injectable
testosterone products like Delatestryl®, Depo-
Testosterone®, and Sustanon®, which are actually much
faster acting in comparison. It is designed to offer a much
less frequent injection schedule, and, therefore, much greater
comfort for the patient. Nebido is a drug developed under a
similar focus as testosterone buciclate, which is another very
slow-acting injectable ester of testosterone.
History:
Nebido® was developed by international giant Schering AG,
Germany (now Bayer). It first surfaced as a prescription drug
in Finland and Germany in October and November of 2004,
respectively. Within a year it had been approved for sale
throughout Europe. Schering/Bayer has since also brought
this product to Mexico, Brazil, Argentina, South Africa,
Colombia, Korea, Venezuela, and various countries in
Eastern Europe (86 countries in total). In July 2005, the U.S.
pharmaceuticals firm Indevus purchased the rights to market
Nebido under the Aveed trade name. The FDA has since held
up U.S. approval of the drug, however, focusing on a small
number of adverse reports in Germany. These specifically
involve post-injection anaphylactic reactions and pulmonary
oil microembolism. Most of these reactions are likely not
due to a problem with the drug itself, but incorrect
administration of the high-volume injection. Future approval
in the U.S. is expected, but unclear.
Nebido® was described by Schering as being the, “first
long-acting injection for the treatment of male
hypogonadism.” This may be a matter of perspective, as
other slow-acting esters do exist. Schering, however, is
taking the lead to market in most regions. The applications
for Nebido® are extremely narrow, being approved for use
in men as a long-term treatment option for low androgen
levels only. It is not labeled for use in women, or in males
for other uses. Given the growing acceptance of androgen
replacement therapy, and the comfort advantage that
Nebido® seems to offer male hormone replacement therapy
patients (esters like enanthate and cypionate generally
require between 13 and 26 injections per year), it may very
well become a dominant testosterone product in the years to
come, especially with the marketing support of a
pharmaceutical giant like Bayer.
How Supplied:
Testosterone undecanoate (injection) is available in various
human drug markets. All products (Nebido®) contain 250
mg/ml of steroid dissolved in oil; packaged in 4ml ampules
containing 1,000 mg of steroid in total.
Structural Characteristics:
Testosterone undecanoate is a modified form of testosterone,
where a carboxylic acid ester (undecanoic acid) has been
attached to the 17-beta hydroxyl group. Esterified forms of
testosterone are less polar than free testosterone, and are
absorbed more slowly from the area of injection. Once in the
bloodstream, the ester is removed to yield free (active
testosterone. Esterified forms of testosterone are designed to
prolong the window of therapeutic effect following
administration, allowing for a less frequent injection
schedule compared to injections of free (unesterified)
steroid. Nebido® is designed to maintain physiological
levels of testosterone for up to 14 weeks after injection.548
Side Effects (Estrogenic):
Testosterone is readily aromatized in the body to estradiol
(estrogen). The aromatase (estrogen synthetase) enzyme is
responsible for this metabolism of testosterone. Elevated
estrogen levels can cause side effects such as increased
water retention, body fat gain, and gynecomastia.
Testosterone is considered a moderately estrogenic steroid.
An anti-estrogen such as clomiphene citrate or tamoxifen
citrate may be necessary to prevent estrogenic side effects.
One may alternately use an aromatase inhibitor like
Arimidex® (anastrozole), which more efficiently controls
estrogen by preventing its synthesis. Aromatase inhibitors
can be quite expensive in comparison to anti-estrogens,
however, and may also have negative effects on blood lipids.
Estrogenic side effects will occur in a dose-dependant
manner, with higher doses (above normal therapeutic levels)
of testosterone more likely to require the concurrent use of an
anti-estrogen or aromatase inhibitor. Since water retention
and loss of muscle definition are common with higher doses
of testosterone, this drug is usually considered a poor choice
for dieting or cutting phases of training. Its moderate
estrogenicity makes it more ideal for bulking phases, where
the added water retention will support raw strength and
muscle size, and help foster a stronger anabolic environment.
Side Effects (Androgenic):
Testosterone is the primary male androgen, responsible for
maintaining secondary male sexual characteristics. Elevated
levels of testosterone are likely to produce androgenic side
effects including oily skin, acne, and body/facial hair growth.
Men with a genetic predisposition for hair loss (androgenetic
alopecia) may notice accelerated male pattern balding.
Those concerned about hair loss may find a more
comfortable option in nandrolone decanoate, which is a
comparably less androgenic steroid. Women are warned of
the potential virilizing effects of anabolic/androgenic
steroids, especially with a strong androgen such as
testosterone. These may include deepening of the voice,
menstrual irregularities, changes in skin texture, facial hair
growth, and clitoral enlargement.
In androgen-responsive target tissues such as the skin, scalp,
and prostate, the high relative androgenicity of testosterone is
dependant on its reduction to dihydrotestosterone (DHT).
The 5-alpha reductase enzyme is responsible for this
metabolism of testosterone. The concurrent use of a 5-alpha
reductase inhibitor such as finasteride or dutasteride will
interfere with site-specific potentiation of testosterone
action, lowering the tendency of testosterone drugs to
produce androgenic side effects. It is important to remember
that anabolic and androgenic effects are both mediated via
the cytosolic androgen receptor. Complete separation of
testosterone’s anabolic and androgenic properties is not
possible, even with total 5-alpha reductase inhibition.
Side Effects (Hepatotoxicity):
Testosterone does not have hepatotoxic effects; liver toxicity
is unlikely. One study examined the potential for
hepatotoxicity with high doses of testosterone by
administering 400 mg of the hormone per day (2,800 mg per
week) to a group of male subjects. The steroid was taken
orally so that higher peak concentrations would be reached in
hepatic tissues compared to intramuscular injections. The
hormone was given daily for 20 days, and produced no
significant changes in liver enzyme values including serum
albumin, bilirubin, alanine-amino-transferase, and alkaline
phosphatases.549
Side Effects (Cardiovascular):
Anabolic/androgenic steroids can have deleterious effects on
serum cholesterol. This includes a tendency to reduce HDL
(good) cholesterol values and increase LDL (bad)
cholesterol values, which may shift the HDL to LDL balance
in a direction that favors greater risk of arteriosclerosis. The
relative impact of an anabolic/androgenic steroid on serum
lipids is dependant on the dose, route of administration (oral
vs. injectable), type of steroid (aromatizable or nonaromatizable),
and level of resistance to hepatic metabolism.
Anabolic/androgenic steroids may also adversely affect
blood pressure and triglycerides, reduce endothelial
relaxation, and support left ventricular hypertrophy, all
potentially increasing the risk of cardiovascular disease and
myocardial infarction.
Testosterone tends to have a much less dramatic impact on
cardiovascular risk factors than synthetic steroids. This is
due in part to its openness to metabolism by the liver, which
allows it to have less effect on the hepatic management of
cholesterol. The aromatization of testosterone to estradiol
also helps to mitigate the negative effects of androgens on
serum lipids. In one study, 280 mg per week of testosterone
ester (enanthate) had a slight but not statistically significant
effect on HDL cholesterol after 12 weeks, but when taken
with an aromatase inhibitor a strong (25%) decrease was
seen.550 Studies using 300 mg of testosterone ester
(enanthate) per week for twenty weeks without an aromatase
inhibitor demonstrated only a 13% decrease in HDL
cholesterol, while at 600 mg the reduction reached 21%.551
The negative impact of aromatase inhibition should be taken
into consideration before such drug is added to testosterone
therapy.
Due to the positive influence of estrogen on serum lipids,
tamoxifen citrate or clomiphene citrate are preferred to
aromatase inhibitors for those concerned with cardiovascular
health, as they offer a partial estrogenic effect in the liver.
This allows them to potentially improve lipid profiles and
offset some of the negative effects of androgens. With doses
of 600 mg or less per week, the impact on lipid profile tends
to be noticeable but not dramatic, making an anti-estrogen
(for cardioprotective purposes) perhaps unnecessary. Doses
of 600 mg or less per week have also failed to produce
statistically significant changes in LDL/VLDL cholesterol,
triglycerides, apolipoprotein B/C-III, C-reactive protein, and
insulin sensitivity, all indicating a relatively weak impact on
cardiovascular risk factors.552 When used in moderate doses,
injectable testosterone esters are usually considered to be the
safest of all anabolic/androgenic steroids.
To help reduce cardiovascular strain it is advised to
maintain an active cardiovascular exercise program and
minimize the intake of saturated fats, cholesterol, and simple
carbohydrates at all times during active AAS administration.
Supplementing with fish oils (4 grams per day) and a natural
cholesterol/antioxidant formula such as Lipid Stabil or a
product with comparable ingredients is also recommended.
Side Effects (Testosterone Suppression):
All anabolic/androgenic steroids when taken in doses
sufficient to promote muscle gain are expected to suppress
endogenous testosterone production. Testosterone is the
primary male androgen, and offers strong negative feedback
on endogenous testosterone production. Testosterone-based
drugs will, likewise, have a strong effect on the hypothalamic
regulation of natural steroid hormones. Without the
intervention of testosterone stimulating substances,
testosterone levels should return to normal within 1-4 months
after the drug has fully cleared the body. Note that prolonged
hypogonadotrophic hypogonadism can develop secondary to
steroid abuse, necessitating medical intervention.
Administration (General):
Due to the large injection volume, prescribing guidelines
recommend that each injection be given slowly, taking
approximately 60 seconds to administer the full 4ml dose.
Nebido® should always be injected deep in the gluteal
muscle.
Administration (Men):
To treat androgen insufficiency, the prescribing guidelines
for testosterone undecanoate (Nebido®) call for a dosage of
1,000 mg (4ml) every twelve weeks. Therapy is usually
initiated with a loading phase, which requires that the second
injection of 1,000 mg be given at approximately the six-week
mark. For bodybuilding purposes, supraphysiological (rather
than physiological) hormone levels would require injecting
the drug on a more regular basis. The most logical protocol
would be to administer a 4ml injection of Nebido every 2-4
weeks, for an approximate average weekly dosage of 250-
500 mg of testosterone ester. At this level one could expect
results very much in line with other testosterone esters, albeit
with a less frequent injection schedule. The onset of action
may, however, be much slower with Nebido. Some may opt
to begin their cycle with a faster acting ester, such as
enanthate or cypionate, which would allow testosterone
levels to reach into supraphysiological ranges sooner.
Testosterone is ultimately very versatile, and can be
combined with many other anabolic/androgenic steroids
depending on the desired effect.
Administration (Women):
Testosterone undecanoate is not approved for use with
women in clinical medicine. This drug is not recommended
for women for physique- or performance-enhancing purposes
due to its strong androgenic nature, tendency to produce
virilizing side effects, and very slow acting characteristics
(making blood levels difficult to control).
Availability:
Testosterone undecanoate injection continues to increase in
prominence as a pharmaceutical product. It is presently
approved for sale in 86 countries worldwide. In reviewing
some of the more popular products and changes on the global
pharmaceutical market, we have made the following
observations.
Nebido gained approval for Europe-wide sales in 2005. The
product is has since distributed throughout Europe, and is
widely available in this region.
Indevus, a subsidiary of Endo Pharmaceuticals, has
continued to push for FDA approval of Aveed in the United
States, but such approval has not yet been granted

guardianactual · Jun 25, 2014

***Nebido, test undecanoate (TU) been around since 96, been a couple of long term studies done, IE 5-8 years for HRT, clinical trials seem very promising from what iv'e read so far.A loading dose of 1g then another at 6-8wks then injections every 12-14wks.*** Testosterone Undecanoate)
</br>
</br> Testosterone + Undecanoate ester Formula: C19 H28 O2 Molecular Weight (base): 288.429 Molecular Weight (ester): 186.2936 Manufacturer: Schering AG Effective Dose (Men): 1,000mg every 4wks Effective Dose (Women): Not recommended Half-Life: Approx. 3 months Detection Time: Approx. 6 months Anabolic/Androgenic Ratio: 100:100
</br>
</br> 1000mg every 6 weeks? "For the purpose of treating low testosterone, the primary purpose of use, standard Nebido doses will normally be 1,000mg every 12 weeks. Most plans will call for a second 1,000mg dose to be applied 6 weeks after the first injection, and from there the standard 12 week protocol will follow. That’s it, that’s all there is too it. Because it is such a slow and long lasting testosterone, you could actually get by and get by well with only a handful of injections per year and see your low testosterone condition vanish. In a performance setting, most will need approximately 1,000mg every 2-4 weeks to see desired results. However, Nebido truly isn’t a compound well-suited for most performance plans and there are better options available" thought that was unique.

- - - Updated - - -

***Nebido, test undecanoate (TU) been around since 96, been a couple of long term studies done, IE 5-8 years for HRT, clinical trials seem very promising from what iv'e read so far.A loading dose of 1g then another at 6-8wks then injections every 12-14wks.*** Testosterone Undecanoate)
</br>
</br> Testosterone + Undecanoate ester Formula: C19 H28 O2 Molecular Weight (base): 288.429 Molecular Weight (ester): 186.2936 Manufacturer: Schering AG Effective Dose (Men): 1,000mg every 4wks Effective Dose (Women): Not recommended Half-Life: Approx. 3 months Detection Time: Approx. 6 months Anabolic/Androgenic Ratio: 100:100
</br>
</br> 1000mg every 6 weeks? "For the purpose of treating low testosterone, the primary purpose of use, standard Nebido doses will normally be 1,000mg every 12 weeks. Most plans will call for a second 1,000mg dose to be applied 6 weeks after the first injection, and from there the standard 12 week protocol will follow. That’s it, that’s all there is too it. Because it is such a slow and long lasting testosterone, you could actually get by and get by well with only a handful of injections per year and see your low testosterone condition vanish. In a performance setting, most will need approximately 1,000mg every 2-4 weeks to see desired results. However, Nebido truly isn’t a compound well-suited for most performance plans and there are better options available" thought that was unique.

Nebido (testosterone undecanoate) profile , dosage , history and administration

akn

Musclechemistry Member

guardianactual

MuscleChemistry Registered Member

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