Andractim® (dihydrotestosterone) transdermal gel profile

akn · Jun 18, 2014

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Andractim is a prescription steroid preparation that contains
the potent androgenic steroid dihydrotestosterone. This
product comes in the form of a transdermal gel, typically
containing 2.5% dihydrotestosterone by weight in an 80gram
tube. As with Androgel, roughly 10% of the active steroid
will make it into circulation with each application.This
would equate to 80 doses of 25 mg, with each dose
delivering approximately 2.5 mg of steroid to the body.
Dihydrotestosterone itself is the most active androgen in the
human body, displaying an ability to bind and activate the
androgen receptor at least three or four times greater than that
of its parent steroid testosterone. This trait, however, is not
accompanied by equally powerful anabolic tendencies. In the
case of dihydrotestosterone, we have a steroid that is almost
purely androgenic, with only minimal muscle-building
(anabolic) action.
Dihydrotestosterone is a weak muscle builder because it is
extremely open to alteration by the 3-alpha-hydroxysteroiddehydrogenase
enzyme, responsible for breaking down
active steroids like DHT into their inactive metabolites. 3a-
HSD is present in high quantities in muscle tissue, running
interference between the outer cell membrane and the
androgen receptors that all steroid hormones are trying to
reach. In humans, little DHT ends up actually reaching this
receptor. Testosterone is very resistant to this enzyme,
however, which allows it to be a much more effective
muscle-building agent. 3a-HSD steroid deactivation in
muscle tissue causes the same problem with Proviron (1-
methyl-dihydrotestosterone). DHT and Proviron both have
very effective uses in areas such as fat loss, hardening,
increasing CNS activity, and pure strength gains, but they do
not perform well as anabolic agents.
History:
Dihydrotestosterone was first synthesized in 1935.412 This
strong androgen was put into consistent medical use during
the late 1950’s, after a series of experiments demonstrating
that it had measurable anabolic effects. Prior to this it was
largely believed that DHT was exclusively an androgenic
substance, and was of little value clinically.
Dihydrotestosterone gels were developed more recently, and
have been investigated for a number of medical purposes. At
present, these preparations are primarily indicated for the
treatment of androgen deficiency, gynecomastia, and
insufficient genital growth. Transdermal DHT has been
successful as an androgen replacement medication in older
men at risk for developing prostate hypertrophy largely
because of its non-aromatizable nature,413 414 as this disorder
is fueled partly by estrogens. The latter two indications are
considered local applications of the drug, and the DHT gel is
applied directly to the tissues requiring treatment.
The primary manufacturer of dihydrotestosterone gel globally
is Besins International, based in France. Besins produces the
drug under the Andractim name, selling it in France and
scarcely in other parts of Europe. Dihydrotestosterone gels
are found much less commonly outside of Europe, and
presently no such preparation is commercially available in
the United States. In 1995, U.S. manufacturer Unimed
Pharmaceuticals purchased the rights to Andractim from
Besins in the U.S., Mexico, and Canada. The firm announced
an interest in the drug for several uses, including androgen
replacement in men over age sixty, treating benign prostate
hypertrophy, and combating HIV- associated wasting. Its use
as an anabolic may be desirable with HIV because it had
been determined that many patients lack an ability to
properly convert testosterone to DHT, and therefore lack
sufficient levels of this important androgen. It appears that
Unimed has since sold its interests in the anabolic steroid
market, however, leaving the potential reemergence of
dihydrotestosterone in the U.S. in question.
How Supplied:
Hydroalcoholic transdermal dihydrotestosterone gels are
available in select human drug markets. Composition and
dosage may vary by country and manufacturer, but usually
contain 2.5% dihydrotestosterone by weight.
Structural Characteristics:
Andractim® is a hydroalcoholic gel containing 2.5% of
dihydrotestosterone (free) by weight. It is designed to
provide a continuous transdermal delivery of
dihydrotestosterone for 24 hours following application to the
skin. Approximately 10% of the applied dose is absorbed
across the skin during each 24-hour period.
Side Effects (Estrogenic):
Dihydrotestosterone is not aromatized by the body, and is not
measurably estrogenic. An anti-estrogen is not necessary
when using this steroid, as gynecomastia and water retention
should not be concerns even among sensitive individuals.
DHT also has inherent anti-estrogenic properties, competing
with other substrates for binding to the aromatase enzyme.
Percutaneous dihydrotestosterone may be an effective option
for the treatment of gynecomastia. Studies have reported a
good level of success when treating certain forms of this
disorder with Andractim, the drug affecting the ratio of
androgenic to estrogenic action in the breast area enough that
a notable regression of mammary tissue has been achieved in
many cases.415 416
Side Effects (Androgenic):
Dihydrotestosterone is the strongest natural male androgen.
Higher than normal therapeutic doses are likely to produce
androgenic side effects including oily skin, acne, and
body/facial hair growth. Men with a genetic predisposition
for hair loss (androgenetic alopecia) may notice accelerated
male pattern balding. Women are warned of the potential
virilizing effects of anabolic/androgenic steroids, especially
with a strong androgen such as dihydrotestosterone.These
may include deepening of the voice, menstrual irregularities,
changes in skin texture, facial hair growth, and clitoral
enlargement. Note that the 5-alpha reductase enzyme does not
metabolize dihydrotestosterone, so its relative androgenicity
is not affected by finasteride or dutasteride.
Side Effects (Hepatotoxicity):
Dihydrotestosterone does not have hepatotoxic effects; liver
toxicity is unlikely.
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.
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. Therapeutic doses of
dihydrotestosterone used to correct insufficient androgen
production in otherwise healthy aging men are unlikely to
increase atherogenic risk. Higher doses are likely to increase
atherogenic risk, but less dramatically than equivalent doses
of synthetic oral anabolic/androgenic steroids.
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 (Men):
To treat androgen insufficiency, hydroalcoholic transdermal
dihydrotestosterone gels have been used in doses ranging
from 16 to 64mg per day (1.6-6.4mg of hormone delivered).
For physique- or performance-enhancing purposes, higher
doses would be necessary to achieve strong
supraphysiological levels of dihydrotestosterone. Logical
effective doses begin in the range of 50-100 mg per day, or
5-10 mg of hormone delivered systemically.
Dihydrotestosterone is of little value for building muscle,
and is most commonly applied for cutting or pure-strengthpromoting
purposes.
Administration (Women):
Hydroalcoholic transdermal dihydrotestosterone gel is not
recommended for women for physique- or performanceenhancing
purposes due to its strong androgenic nature and
tendency to produce virilizing side effects.
Availability:
Pharmaceutical preparations containing transdermal
dihydrotestosterone gel remain scarce. The legitimate supply
seems to be scattered into isolated markets of Europe, Asia,
and South America. In reviewing some of the remaining
products and changes in the global pharmaceutical market,
we have made the following observations.
One of the most notable preparations is Andractim from
Besins-Iscovesco in France. It contains 25 mg/mL of
hormone in a 100 gram tube.
Andractim is produced in Belgium by Piette. It contains 25
mg/mL of hormone in an 80 gram tube.
Andractim is produced in India by Chemec. It contains 25
mg/mL of hormone in a 100 gram tube.

By WL

Andractim® (dihydrotestosterone) transdermal gel profile

akn

Musclechemistry Member

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