Orabolin® (ethylestrenol) oral anabolic steroid profile and administraition

akn · Jun 2, 2014

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Ethylestrenol is an oral anabolic steroid derived from
nandrolone. As is typical for many 19-nor steroids, this agent
exhibits far greater anabolic properties than androgenic, is
only weakly estrogenic, and is strongly progestational.
Structurally, ethylestrenol most closely resembles Nilevar
(norethandrolone). The two differ only by the absence of an
oxygen atom at the c3 position of ethylestrenol, and in the
body ethylestrenol actually has a notable affinity to convert
to norethandrolone.560 This path of metabolism is
responsible for much of the anabolic, androgenic, and
estrogenic activity we see with this compound, and in most
regards ethylestrenol can be viewed as a pro-drug to
norethandrolone. Although ethylestrenol is strongly anabolic
relative to its androgenicity, athletes generally find this
steroid to be extremely weak. The level of muscle growth
obtained with this steroid is generally much less noticeable
than that expected with either Nilevar or Deca-Durabolin®,
and it is considerably less effective than both stanozolol and
oxandrolone on a milligram for milligram basis.
History:
Ethylestrenol was first described in 1959.561 It was
developed into an oral medicine by Organon (now
Merck/MSD), appearing in most markets between 1961 and
1964. Organon sold the tablets under the trade name
Maxibolin in the U.S., and as Orabolin, Orgabolin, and
Durabolin-O in other markets. The latter name is a
compressed form of “Durabolin-Oral,” noting that the drug is
an oral cousin to Durabolin (nandrolone phenylpropionate).
Organon also produced oral ethylestrenol solutions, such as
Maxibolin Elixir (U.S.) and Fertabolin (India, Philippines).
Ethylestrenol was initially indicated for several uses, mainly
focused on preserving lean mass. Early U.S. product
literature states,“… along with a good dietary regimen,
Maxibolin promotes tissue-building and weight gain,
stimulation of appetite and sense of wellbeing, renewal of
vigor, is an aid in bone matrix reconstruction and in
combating the depression and weakness of chronic illness or
prolonged convalescence. It can also prevent or reverse
certain catabolic effects associated with corticosteroid
therapy.”
Ethylesterenol became a steroid of great controversy during
the early 1980’s, when Western media attention was given to
the marketing of the drug to malnourished children in Third-
World markets such as India, Bangladesh, and the
Philippines. Advertising on Fertabolin in India claimed the
drug would “help children gain full weight and height,”
“simulates physiological appetite,” and “ensures optimal
assimilation of food.” It also described a “delicious
[raspberry] syrup flavor children love.” The main point of
contention was the promotion of an anabolic steroid to treat
the lack of adequate food supply, the real issue at hand. Many
viewed Organon’s actions as potentially dangerous and
highly unethical, and the company soon discontinued
Fertabolin and related marketing practices. Maxibolin and
Maxibolin Elixir were voluntarily withdrawn from the U.S.
market during the late 1980’s as well, and most Western
ethylestrenol products from Organon soon followed. Today,
Merck/MSD retains only a limited interest in the drug.
Ethylestrenol is currently a rare find, as it is only
manufactured (as a generic drug or under other brand names)
is a select few countries.
How Supplied:
Ethylestrenol is available in select human and veterinary
drug markets. Composition and dosage may vary by country
and manufacturer, but typically contains 2mg of steroid per
tablet. Oral solutions have also been produced in the past,
such as Maxibolin Elixir, which contained 2mg/5 mL in a 4
ounce bottle. Fertabolin for children contained .2mg/2 mL of
solution.
Structural Characteristics:
Ethylestrenol is a modified form of nandrolone. It differs by:
1) the addition of an ethyl group at carbon 17-alpha to
protect the hormone during oral administration and 2) the
removal of the 3-oxygen.
Side Effects (Estrogenic):
Ethylestrenol is aromatized by the body, and converts to a
synthetic estrogen with a high level of biological activity
(17alpha-ethyl-estradiol). Rate of aromatization is so low,
however, that it remains classified as a weakly estrogenic
steroid. Gynecomastia is possible during treatment, but
generally only when higher doses are used. Water and fat
retention can also become issues, again depending on dose.
Sensitive individuals may need to addition an anti-estrogen
such as Nolvadex®. One may alternately use an aromatase
inhibitor like Arimidex® (anastrozole), which is a more
effective remedy for estrogen control. Aromatase inhibitors,
however, can be quite expensive in comparison to standard
estrogen maintenance therapies, and may also have negative
effects on blood lipids.
It is of note that ethylestrenol has strong activity as a
progestin in the body.562 The side effects associated with
progesterone are similar to those of estrogen, including
negative feedback inhibition of testosterone production and
enhanced rate of fat storage. Progestins also augment the
stimulatory effect of estrogens on mammary tissue growth.
There appears to be a strong synergy between these two
hormones here, such that gynecomastia might even occur with
the help of progestins without excessive estrogen levels
being present. The use of an anti-estrogen, which inhibits the
estrogenic component of this disorder, is often sufficient to
mitigate gynecomastia caused by this steroid.
Side Effects (Androgenic):
Although classified as an anabolic steroid, androgenic side
effects are still common with this substance. This may
include bouts of oily skin, acne, and body/facial hair growth.
Anabolic/androgenic steroids may also aggravate male
pattern hair loss. Individuals sensitive to the androgenic
effects of this steroid may find a milder anabolic such as
Deca-Durabolin® to be more comfortable. Women are
additionally warned of the potential virilizing effects of
anabolic/androgenic steroids. These may include a
deepening of the voice, menstrual irregularities, changes in
skin texture, facial hair growth, and clitoral enlargement.
Note that in androgen-responsive target tissues such as the
skin, scalp, and prostate, the relative androgenicity of
ethylestrenol is reduced by its reduction to weaker “dihidyo”
metabolites. The 5-alpha reductase enzyme is responsible for
this metabolism. The concurrent use of a 5-alpha reductase
inhibitor such as finasteride or dutasteride will interfere with
site-specific reduction of ethylestrenol action, increasing the
tendency of the drug to produce androgenic side effects.
Reductase inhibitors should be avoided with this steroid if
maintaining low relative androgenicity is desired.
Side Effects (Hepatotoxicity):
Ethylestrenol is a c17-alpha alkylated compound. This
alteration protects the drug from deactivation by the liver,
allowing a very high percentage of the drug entry into the
bloodstream following oral administration. C17-alpha
alkylated anabolic/androgenic steroids can be hepatotoxic.
Prolonged or high exposure may result in liver damage. In
rare instances life-threatening dysfunction may develop. It is
advisable to visit a physician periodically during each cycle
to monitor liver function and overall health. Intake of c17-
alpha alkylated steroids is commonly limited to 6-8 weeks,
in an effort to avoid escalating liver strain. Severe liver
complications are rare given the periodic nature in which
most people use oral anabolic/androgenic steroids, although
cannot be excluded with this steroid, especially with high
doses and/or prolonged administration periods.
The use of a liver detoxification supplement such as Liver
Stabil, Liv-52, or Essentiale Forte is advised while taking
any hepatotoxic anabolic/androgenic steroids.
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.
Ethylestrenol has a strong effect on the hepatic management
of cholesterol due to its structural resistance to liver
breakdown and route of administration. Anabolic/androgenic
triglycerides, reduce endothelial relaxation, and support left
ventricular hypertrophy, all potentially increasing the risk of
cardiovascular disease and myocardial infarction.
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. Without the intervention
of testosterone-stimulating substances, testosterone levels
should return to normal within 1-4 months of drug secession.
Note that prolonged hypogonadotrophic hypogonadism can
develop secondary to steroid abuse, necessitating medical
intervention.
Administration (General):
Studies have shown that taking an oral anabolic steroid with
food may decrease its bioavailability.563 This is caused by
the fat-soluble nature of steroid hormones, which can allow
some of the drug to dissolve with undigested dietary fat,
reducing its absorption from the gastrointestinal tract. For
maximum utilization, this steroid should be taken on an empty
stomach.
Administration (Men):
Original prescribing guidelines recommend a dosage of 4 mg
to 8 mg per day, taken for no more than 6 consecutive weeks.
After a break for 4 weeks, the drug is resumed for an
additional 6 weeks if indicated. When used for physique- or
performance-enhancing purposes, a daily dosage of 20 mg to
40 mg is most common, which equates to ten to twenty 2mg
tablets.The drug is typically used in cycles lasting no longer
than 6-8 weeks, in an effort to minimize hepatic strain. This
level is sufficient for some measurable gains in muscle size
and strength, although experienced steroid users are likely to
still be disappointed with the results. Instead of increasing
the dosage, most opt to add a second steroid to the cycle,
usually an injectable such as testosterone cypionate or
enanthate, boldenone undecylenate, or methenolone enanthate
(usually at a dose of 200-400 mg per week), which do not
provide additional liver toxicity.
Administration (Women):
Original prescribing guidelines recommend a dosage of 4 mg
to 8mg per day, taken for no more than 6 consecutive weeks.
After a break for 4 weeks, the drug is resumed for an
additional 6 weeks if indicated. When used for physique- or
performance-enhancing purposes, a daily dosage of 10 mg to
16 mg is most common, taken for no longer than 4
weeks.This level seems to be fairly effective for promoting
new muscle growth. Higher doses are likely to produce
virilizing side effects, and are not recommended. Note that
virilizing side effects are still sometimes noticed at lower
doses.
Availability:
Pharmaceutical preparations containing ethylestrenol remain
scarce. In reviewing some of the remaining products and
changes in the global pharmaceutical market, we have made
the following observations.
At the present time, the legitimate supply of ethylestrenol
appears to be isolated to Australia, where it is found in a
small number of veterinary compounds including Nandora
tablets and Nitrotain paste.

By William lewellyn

Orabolin® (ethylestrenol) oral anabolic steroid profile and administraition

akn

Musclechemistry Member

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