Primobolan® (methenolone acetate) ANABOLIC ANDROGENIC STEROID PROFILE

akn · Jun 16, 2014

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Primobolan® is a brand name for the anabolic steroid
methenolone acetate. This agent is very similar in action to
Primobolan® Depot (methenolone enanthate), except here the
drug is designed for oral administration instead of injection.
Methenolone acetate is a non-c17-alpha-alkylated oral
steroid, one of only a few commercially available oral
agents that presents limited liver toxicity to the user. It is also
highly favored for its properties as a moderately effective
anabolic with low androgenic and no estrogenic properties.
It is, likewise, commonly used during cutting phases of
training, when lean tissue growth and solid muscularity, not
raw bulk, are the key objectives.
History:
Methenolone was first described in 1960.577 Squibb would
introduce the drug (as methenolone acetate) to the United
States in 1962.578 This agent was sold for a very short time
as a 20 mg tablet, under the brand name of Nibal®. Schering
in West Germany (now Bayer) would be granted rights to the
drug that same year, and would sell it under the Primobolan®
name. Nibal® was soon removed from the U.S. market,
never to return as a commercial product. Schering now had
exclusive patent rights to produce methenolone acetate, and
would continue to sell the drug uninterrupted since 1962, and
consumers had naturally come to identify methenolone
acetate as a product of Schering.
Primobolan® has always been identified as a European
steroid, and during the 1960’s and ’70’s was being offered
for sale in such countries as Germany, Austria, Belgium,
France, the Netherlands, and Finland. At one time Schering
also manufactured a 20 mg/ml oil-based injectable of
methenolone acetate in limited markets (called Primobolan®
Acetate), but it has been out of manufacture since 1993.
Injectable methenolone acetate proved to be very popular for
pre-contest cutting use, and was gravely missed among
European competitors when discontinued. Although we still
have the acetate in oral form, it is a close, but not equal,
substitute (injection is a much more efficient form of delivery
for this steroid).
Primobolan® is prescribed as a lean tissue building anabolic
agent, often used in cases where body wasting has occurred
secondary to major surgery, infection, wasting disease,
aggressive corticosteroid administration, or malnutrition.
(Some clinicians also prescribe this agent for treating
osteoporosis and sarcopenia, or the natural loss of muscle
mass with aging). This steroid has also been used to promote
weight gain in underweight premature infants and children in
clinical studies, and was able to do so effectively and
without signs of toxicity or undesirable effects.579 Athletes
have long favored the combined strong anabolic, weak
androgenic, and non-estrogenic nature of this drug, which
makes it very desirable for building lean muscularity without
side effects.
Although Primobolan® demonstrated a good record of
clinical safety, Schering had withdrawn this drug from most
markets by the early 2000s. No 50 mg versions are still in
manufacture, and at most a select couple of products
containing 5 mg or 25 mg may still be in circulation. The
only confirmed sources for oral brand name Primobolan in
recent years were in Japan and South Africa, and these were
sold under the Schering name. It is unknown if any such
products have been brought over to the new Bayer label.
Aside from this, a very small number of pharmaceutical
preparations containing methenolone acetate may still be in
production.
How Supplied:
All forms of Schering Primobolan® contain 5 mg, 25 mg, or
50 mg (no longer available) of methenolone acetate per
tablet. Composition and dosage of other brands may vary by
country and manufacturer.
Structural Characteristics:
Methenolone is a derivative of dihydrotestosterone. It
contains one additional double bond between carbons 1 and
2, which helps to stabilize the 3-keto group and increase the
steroid’s anabolic properties, and an additional 1-methyl
group, which protects the steroid against hepatic metabolism.
Primobolan makes use of methenolone with a carboxylic acid
ester (acetic acid) attached to the 17-beta hydroxyl group to
further help protect it from oxidation during oral
administration. Studies have demonstrated the methenolone is
an effective oral anabolic agent in both the acetate and
unesterified forms.580 581
Side Effects (Estrogenic): Methenolone is not aromatized by the body,582 and is not
measurably estrogenic. Estrogen-linked side effects should
not be seen when administering this steroid. Sensitive
individuals need not worry about developing gynecomastia,
nor should they be noticing any appreciable water retention
with this drug. The increase seen with methenolone should be
quality muscle mass, not the smooth bulk that often
accompanies steroids open to aromatization. During a cycle,
the user should additionally not notice strong elevations in
blood pressure, as this effect is also related (generally) to
estrogen and water retention. Methenolone is a steroid most
favored during cutting phases of training, when water and fat
retention are major concerns, and sheer mass not the central
objective.
Side Effects (Androgenic):
Although classified as an anabolic steroid, androgenic side
effects are still possible 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. Women are 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. Methenolone is still a very mild steroid
however, and strong androgenic side effects are typically
related to higher doses. Women often find this preparation an
acceptable choice, observing it to be a very comfortable and
effective anabolic.
Side Effects (Hepatotoxicity):
Methenolone is not considered a hepatotoxic steroid; liver
toxicity is unlikely. Studies have failed to produce
appreciable changes in markers of hepatic stress when the
drug was given in therapeutic levels.583 This steroid does
have some resistance to hepatic breakdown, however, and
liver toxicity, failure, and death was reported in one elderly
patient receiving oral methenolone acetate.584 Although
unlikely, hepatotoxicity cannot be completely excluded,
especially with very high oral doses.
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 non
aromatizable), and level of resistance to hepatic metabolism.
Methenolone should have a stronger negative effect on the
hepatic management of cholesterol than testosterone or
nandrolone due to its non-aromatizable nature, but a much
weaker impact than c-17 alpha alkylated steroids. Due to the
route of delivery, oral methenolone will have a slightly
stronger negative effect on lipids compared to methenolone
enanthate injections. 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. Primobolan® is generally described as having a
low impact on endogenous testosterone production. While
this may be true in small clinical doses (20-25 mg daily), this
may not be a major distinction when used for physique- or
performance-enhancing purposes. In one study, more than
half of the patients receiving only 30-45 mg per day noticed a
15-65% suppression of gonadotropin levels.585 While this is
far from having no hormonal impact, the suppression caused
by methenolone acetate may still be less pronounced than
with many other agents. If Primobolan® is used at moderate
doses for less than 8 weeks, hormonal recovery should not
be a protracted experience.
Administration (General):
Studies have shown that taking an oral anabolic steroid with
food may decrease its bioavailability.586 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 prescribing guidelines for Primobolan® recommend a
maximum daily dosage of 100-150 mg per day. The usual
administration protocols for physique- or performanceenhancing
purposes call for 75-150 mg daily, which is taken
for 6 to 8 weeks. This level is sufficient to impart a
measurable anabolic effect, although one usually doesn’t
expect to achieve great gains in muscle mass with this drug.
Instead, Primobolan® is utilized when the athlete has a
specific need for a mild anabolic agent, most notably in
cutting phases of training.
Due to its mild nature, Primobolan® is often used in
conjunction with other steroids for a stronger effect. In such
cases, a slightly lower dose is often used (50-100 mg per
day). During a dieting or cutting phase, thought to be its
primary application, a non-aromatizing androgen like
Halotestin® or trenbolone is often added. Such combinations
would enhance the physique without water retention, and
help bring out a harder and more defined look of muscularity.
Non-aromatizing androgen/anabolic stacks like this are very
popular among competing bodybuilders, and prove quite
reliable for rapidly improving the contest form. This
compound is also occasionally used with more potent
androgens during bulking phases of training. The addition of
testosterone, Dianabol or Anadrol 50® is common, although
the gains are often accompanied by some level of smoothness
due to the added estrogenic component, as well as
hepatotoxicity in the case of the latter two agents.
Administration (Women):
The prescribing guidelines for Primobolan® do not offer
separate dosing recommendations for women, although it is
indicated that women who are pregnant, or may become
pregnant, should not use the drug. Female athletes generally
respond well to 50-75 mg daily, with no signs of virilization
symptoms. One would not expect a tremendous amount of
muscle mass with this drug, and instead find a slow and
steady (quality) increase. Some women choose to further
add-in other anabolics such as Winstrol® or oxandrolone, in
an effort to increase the muscle-building effectiveness of a
cycle. While both of these compounds are quite tolerable,
one must be sure not to use too high an accumulated dosage.
Taken at too high a dosage, these weak anabolics can quickly
cause masculinizing side effects.
Availability:
Pharmaceutical preparations containing methenolone acetate
remain scarce. The drug has been unavailable in western
nations for many years now, and the bulk of the supply
presently comes from underground steroid manufacturers. In
reviewing some of the remaining products and changes in the
global pharmaceutical market, we have made the following
observations.
Balkan Pharmaceuticals produces Primobol in Moldova. It
comes in 50 mg tablets, with 20 sealed in each foil and
plastic strip.

By WL

Primobolan® (methenolone acetate) ANABOLIC ANDROGENIC STEROID PROFILE

akn

Musclechemistry Member

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