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View Full Version : Nilevar® (norethandrolone) anabolic steroid profile , history and administration



akn
06-04-2014, 09:39 PM
<!--[if gte mso 9]><xml> <w:WordDocument> <w:View>Normal</w:View> <w:Zoom>0</w:Zoom> <w:TrackMoves/> <w:TrackFormatting/> <w:PunctuationKerning/> <w:ValidateAgainstSchemas/> <w:SaveIfXMLInvalid>false</w:SaveIfXMLInvalid> <w:IgnoreMixedContent>false</w:IgnoreMixedContent> <w:AlwaysShowPlaceholderText>false</w:AlwaysShowPlaceholderText> <w:DoNotPromoteQF/> <w:LidThemeOther>EN-US</w:LidThemeOther> <w:LidThemeAsian>X-NONE</w:LidThemeAsian> <w:LidThemeComplexScript>X-NONE</w:LidThemeComplexScript> <w:Compatibility> <w:BreakWrappedTables/> <w:SnapToGridInCell/> <w:WrapTextWithPunct/> <w:UseAsianBreakRules/> <w:DontGrowAutofit/> <w:SplitPgBreakAndParaMark/> <w:DontVertAlignCellWithSp/> <w:DontBreakConstrainedForcedTables/> <w:DontVertAlignInTxbx/> <w:Word11KerningPairs/> <w:CachedColBalance/> <w:UseFELayout/> </w:Compatibility> <w:DoNotOptimizeForBrowser/> <m:mathPr> <m:mathFont m:val="Cambria Math"/> <m:brkBin m:val="before"/> <m:brkBinSub m:val="--"/> <m:smallFrac m:val="off"/> <m:dispDef/> <m:lMargin m:val="0"/> <m:rMargin m:val="0"/> <m:defJc m:val="centerGroup"/> <m:wrapIndent m:val="1440"/> <m:intLim m:val="subSup"/> <m:naryLim m:val="undOvr"/> </m:mathPr></w:WordDocument> </xml><![endif]--> Description:
Norethandrolone is an anabolic steroid closely related to
nortestosterone (nandrolone) in structure. The activity of this
steroid is that of a mild to moderate oral anabolic steroid,
which is accompanied by distinguishable androgenic and
estrogenic components. Although this steroid is essentially
nandrolone modified (alkylated) to make oral dosing viable,
it cannot be looked at simply as an oral alternative to Deca-
Durabolin®. Most notably, the greatly increased
estrogenicity caused by 17-alkylation makes norethandrolone
much more problematic when trying to build quality (lean
muscle mass. In administering an effective amount of steroid
in terms of muscle growth, the user has to deal with much
more in terms of estrogenic side effects. The muscle
accumulation with norethandrolone is also going to be
accompanied by a high level of water and (likely) fat
retention, not the quality muscularity normally associated
with nandrolone decanoate.
History:
Norethandrolone was first described in 1954.553 It was
developed into a medicine by Searle, which introduced it
into the U.S. prescription drug market under the Nilevar
brand name during the late 1950’s. The drug was originally
sold as an oral tablet, an oral solution (with dropper bottle),
and an injectable solution (in 25 mg ampules). The latter
form of norethandrolone has been out of commerce for so
long that few remember it was once also given by injection.
Nilevar was prescribed for a variety of illnesses that were
benefited by a protein sparing anabolic agent, Listed
indications included preparation for and recovery from
surgery, severe or prolonged illness, anorexia nervosa,
severe burns and trauma, decubitus ulcers, osteoporosis,
bone fracture healing, gastrointestinal disease, prolonged
corticosteroid administration, and various forms of
malnourishment in adults and children.
Norethandrolone ultimately saw only limited success as a
prescription anabolic agent. It did make its way to Europe
and certain other markets, but not widely. The drug was an
early functional anabolic, displaying more tissue-building
properties than androgenic effects. But it also remained an
agent with a troubling estrogenic side. This eventually led to
norethandrolone being passed over clinically for more
refined compounds as they became available. Searle decided
to discontinue the sale of Nilevar in the U.S. during the
1960’s, and instead began focusing energies on its newer,
more strongly anabolic, and non-estrogenic steroid
oxandrolone (sold as Anavar). Most other markets carrying
norethandrolone, either by Searle or other companies, soon
began losing this compound as well. Today, this drug is
available on a limited basis, most notably in Australia where
it remains viable on the veterinary drug market.
How Supplied:
Norethandrolone is available in select veterinary drug
markets. Composition and dosage may vary by country and
manufacturer, but typically contain 5 or 10 mg of steroid per
tablet.
Structural Characteristics:
Norethandrolone is a modified form of nandrolone. It differs
by the addition of an ethyl group at carbon 17-alpha to
protect the hormone during oral administration.
Side Effects (Estrogenic):
Norethandrolone is aromatized by the body, and converts to a
synthetic estrogen with a high level of biological activity
(17alpha-ethyl-estradiol). As a result, it is a highly
estrogenic steroid. Gynecomastia is often a concern during
treatment, and may present itself quite early into a cycle
(particularly when higher doses are used). At the same time
water retention can become a problem, causing a notable
loss of muscle definition as both subcutaneous water
retention and fat levels build. Sensitive individuals may want
to keep the estrogen under control with the addition of 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 norethandrolone has some additional activity
as a progestin in the body.554 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 norethandrolone.
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
norethandrolone is reduced by its reduction to
dihydronorethandrolone. 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 norethandrolone
action, considerably 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):
Norethandrolone 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.
Norethandrolone has a strong effect on the hepatic
management of cholesterol due to its structural resistance to
liver breakdown and route of administration.
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.
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.555 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):
The original prescribing guidelines for Nilevar called for a
daily dosage of 20 to 30 mg. This was to be administered on
an intermittent basis, with the drug taken for no more than 12
consecutive weeks. Thereafter, a break of at least 1 month
was advised before therapy was resumed. When used for
physique- or performance-enhancing purposes, the drug is
also used intermittently, with cycles usually lasting between
6 and 8 weeks in length followed by 6-8 weeks off. A daily
dosage of 20 to 40 mg is most common for such applications.
This level is typically sufficient for rapid gains in strength
and muscle mass (bulk). The high estrogenicity makes
norethandrolone of little value in speed and endurance
sports, causing an unwanted retention of water weight. When
given by injection, the same milligram dosage is
recommended as when the drug is given orally.
Administration (Women):
The original prescribing guidelines for Nilevar made no
special dosing recommendations for women, although it did
warn that androgenicity is likely on a high dosage. When
used by women for physique- or performance-enhancing
purposes, a daily dosage of 5-10 mg is most common, taken
for no longer than 4 weeks. This level is quite effective for
promoting new muscle growth. Note that virilizing side
effects are still sometimes noticed at lower doses,and need
to be carefully examined for.
Availability:
Pharmaceutical preparations containing norethandrolone
remain scarce, and are rarely diverted for black market sale.
The only region of note where this compound is still made is
Australia.
By William Llewellyn
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