Primobolan Acetate is a naturally occurring hormonal analog that is
orally bioavailable and active in it’s original form. This new class of
hormone analog does not require conversion into another form of synthetic
testosterone like most pro-hormones. Primobolan Acetate orals stimulate the
natural production of total and active testosterone. It does this by
regulating estrogen biosynthesis which produces a signal in the body to
promote luteinizing hormone (LH) and decrease (SHBG) in order to increase
natural production of testosterone while simultaneously stimulating free or
active testosterone.
Highlights:
Inhibits estrogen formation.
Orally active in its original form, No conversion necessary
Stimulates natural production of total and free testosterone
Long term use recommended - Does not need to be cycled
Does not breakdown into banned substances or metabolites
Promotes fat free mass, strength and endurance
Can be taken alone or may be stacked with other steroids & pro-steroids
The chemical term 4-Androstenoldione Acetate refers to the isomer:
4-Androsten-4-ol-3beta,17beta-dione Acetate. 4-Androstenoldione Acetate is
the acetate ester derivative of 4-Hydroxy-4-Androstenedione, which is an
analog or derivative of the naturally occurring precursor hormone
4-Androstenedione. This compound concerns the isomer form of
4Androsten-4-ol-3beta,17beta-dione Acetate.
4-Androstenoldione Acetate is a steroidal aromatase inhibitor that inhibits
estrogen biosynthesis, increases natural production of total and free
testosterone, and may inhibit DHT formation. It does this by inhibiting the
Cytochrone P-450 enzyme, which converts testosterone to estrogen. Once
estrogen levels fall a signal is sent to the hypothalamic pituitary axis to
produce (LH) luteinizing hormone and decrease (SHBG) steroid hormone binding
globulin. LH then stimulates the testes to increase total testosterone
production, in which a large portion is free or active testosterone due to
the decrease in SHBG. This increased amount of testosterone is then
metabolized with less estrogen and DHT conversion.
The compound is mainly eliminated by metabolism, renal excretion of
metabolites accounting for 95% of dose. The excretory balance of
14C-compounds in urine and feces totals up to 98.9+/-0.8% of the i.v. dose
after 168 h. The 14C-compounds in plasma and urine were separated by HPLC,
and three major metabolites were submitted to structural analysis by MS, NMR
and UV spectroscopy. One of the metabolites is the direct 4-O-glucuronide of
formestane. The other two represent 3-O-sulfates of the exocons
3beta,4beta-dihydroxy-5alpha-androstane-17-one and
3alpha,4beta-dihydroxy-5alpha-androstane-17-one, their ratio being 7:3.
These exocons are formed by stereoselective 3-keto reduction, accompanied by
reduction of the 4,5-enol function. The exocons do not inhibit human
placental aromatase activity in vitro.
The half-life orally was approximately 3 h, whereas the apparent half-life
of injected drug was between 5 and 10 days after a more rapid clearance
during the first 4 days after injection. The formulated material achieved a
significantly higher mean peak concentration (88% greater than that obtained
using the unformulated powder) and a higher mean AUC (not significant). The
median time to peak was 1.5 h for both preparations and the elimination rate
constants were similar (0.31 for micronized 4-OHA and 0.36 h-1 for
formulated 4-OHA). Significant biological activity was demonstrated with the
formulated material in its suppression of plasma oestradiol levels.
Another interesting note is the ability of 4-Androsten-4-ol-3, 17-dione
acetate to directly stimulate testosterone whether in the presence of LH or
not. Researchers examined the effects of placebo, luteinizing hormone (LH),
4-acetoxy-4-androstenedione, and luteinizing hormone (LH) plus
4-acetoxy-4-androstenedione on rat follicles in vitro. In regards to
testosterone they found that within the first 8 hours
4-acetoxy-4-androstenedione had the ability to directly stimulate
testosterone alone and greatly stimulate testosterone in combination with
luteinizing hormone (LH). Interestingly enough within the next 16 hours they
discovered 4-acetoxy-4-androstenedione alone was stimulating testosterone 3
times as much as luteinizing hormone (LH) while the combination also
continued to stimulate testosterone.
Estrogen inhibition was significant with 4-Androsten-4-ol-3, 17-dione
acetate alone producing the greatest inhibition at both 8 and 24 hour
intervals.
Primobolan Acetate [4-Androsten-4-ol-3beta,17beta-dione Acetate for oral
ingestion] is indicated for the long-term promotion of testosterone and
regulation of estrogen in humans.
As a dietary supplement, take 1 to 2 tablets 3 times daily. Do not exceed
recommended dose. The recommended daily dose in adults is 1-5 mg/kg body
weight per day. The usual effective dose is 1-2 mg/kg/day but higher doses
may be required, and the dose should be individualized. Response is not
often immediate, and a minimum trial of three to six months should be given.
Not to be used with any other medications especially oral hypoglycemic
agents ie. Glyburide. Not for use by individuals under the age of 18. Do not
use if you are pregnant, contemplating pregnancy or lactating. Consult a
physician prior to use if you have any medical condition.
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