Cheque Drops® (mibolerone) ORAL ANABOLIC STEROID DESCRIPTION

akn

Musclechemistry Member
<!--[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:
Mibolerone is an oral anabolic steroid, structurally derived
dimethylated nandrolone. This agent is specifically 7,17-
dimethylated nandrolone, significantly more potent as an
anabolic and androgenic agent than its non-methylated parent.
Over the years, mibolerone has earned a reputation among
bodybuilders as being one of the strongest steroids ever
made. This is correct in a technical sense, as it is one of only
a select few commercial steroid products effective in
microgram, not milligram, amounts. During standard animal
assays, mibolerone was determined to have 41 times the
anabolic activity of methyltestosterone when given orally. In
contrast, it had only 18 times the androgenic activity.
Although both properties are strongly pronounced with this
agent, it retains a primarily anabolic character (in a relative
sense). Estrogenic and progestational properties are also
very pronounced with this drug, however. Among athletes it
is most commonly applied during bulking phases of training,
or to stimulate aggression before a workout or competition.
History:
Mibolerone was first described in 1963.430 It was developed
into a veterinary medicine during the 1960’s by Upjohn,
which sold the drug under the brand name Cheque Drops.
The preparation contained 100 mcg/ml of steroid in a 55 mL
bottle, for a total steroid content of 5.5 milligrams
(illustrating the high relative potency of mibolerone).
Pharmacia & Upjohn later also sold a preparation called
Cheque Medicated Dog Food, of obvious composition. The
drug was administered orally, and had been used to interrupt
the estrous cycle of female dogs, preventing them from going
into heat. It is approved for use in an animal for no longer
than 24 months. Use of the drug is considered carefully by
most veterinarians, mainly because longer-term
administration can produce side effects such as clitoral
enlargement, aggression, urinary difficulties, and liver
damage.
Among athletes, mibolerone has always been seen with a
high level of mystique, perhaps partly due to its limited
availability. Those actually familiar with the Upjohn (then
Pharmacia & Upjohn) product were likely disappointed
during the early 2000’s, when the Cheque products were
officially discontinued by the manufacturer. The company,
now Pfizer Animal Health, presently lists no miboleronecontaining
products on its inventory, despite retaining the
rights to market the drug. Mibolerone is still available in the
U.S., but only in generic form from a private compounding
pharmacy, obtained under special order by a licensed
veterinarian. The removal of the Pharmacia & Upjohn
products from the U.S. market marked the commercial end of
mibolerone. No prescription preparation, human or
veterinary, is currently known to contain mibolerone
worldwide.
How Supplied:
Mibolerone is no longer available as a prescription drug
product. When produced it most commonly came in the form
of an oral solution based in propylene glycol, carrying
100mcg of steroid per milliliter in a 55 mL bottle.
Structural Characteristics:
Mibolerone is a modified form of nandrolone. It differs by 1)
the addition of a methyl group at carbon 17-alpha to protect
the hormone during oral administration and 2) the
introduction of a methyl group at carbon 7 (alpha), which
inhibits 5-alpha reduction and increases relative
androgenicity. 7,17-dimethylated steroids also tend to be
very resistant to metabolism and serum-binding proteins,
greatly enhancing their relative biological activity.
Side Effects (Estrogenic):

Mibolerone is aromatized by the body, and is considered a
highly estrogenic steroid due to its conversion to 7,17-
dimethylestradiol (an estrogen with high biological activity).
Gynecomastia may be a concern during treatment, especially
when higher than normal therapeutic 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. To avoid strong estrogenic
side effects, it may be necessary to use 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 mibolerone also displays strong activity as a
progestin in the body. 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 mibolerone.
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 7-methylation inhibits steroid 5-alpha reduction.431
The relative androgenicity of mibolerone is not affected by
the concurrent use of finasteride or dutasteride.
Side Effects (Hepatotoxicity):
Mibolerone 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. Note that
U.S. prescribing information for Cheque Drops mentions
only one human study being conducted on mibolerone, and
that the study was terminated early due to high hepatotoxicity.
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.
Mibolerone 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.432 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):
Mibolerone was never approved for use in humans.
Prescribing guidelines are unavailable. In the athletic arena,
the drug is used intermittently due to its high level of
hepatotoxicity, with cycles usually lasting no more than 6
weeks followed by 6-8 weeks off. A daily dosage of 200 to
500mcg is most common for bodybuilding purposes. This
level is typically sufficient for gains in strength and muscle
mass (bulk). The high progestational and estrogenic activity
of mibolerone makes it of little value in speed and endurance
sports, causing an unwanted retention of water weight.
Administration (Women):
Mibolerone was never approved for use in humans.
Prescribing guidelines are unavailable. Mibolerone is
generally not recommended for women for physique- or
performance-enhancing purposes due to its very strong nature
and tendency to produce virilizing side effects.
Availability:
Mibolerone is sold in the U.S. as a compounded veterinary
medicine only. No commercial preparations containing this
drug are known to exist worldwide. Mibolerone remains
available on the black market in underground preparations
only.

BY WL
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