akn
Musclechemistry Member
Androgenic 100
Anabolic 100
Chemical Names 4-androsten-3-one-17beta-ol
17beta-hydroxy-a ndrost-4-en-3-one
Estrogenic Activity moderate
Progestational Activity low
Description:
AndroGel® is a transdermal hydroalcoholic testosterone
gel that contains a 1% concentration of testosterone by
weight. It was originally released in 2.5 gram and 5-gram
sachets, equating to a total per-application testosterone
dose of 25 mg and 50 mg respectively. The AndroGel®
prescribing information states that the product has a
transdermal bioavailability of approximately 10% • This
means that each 2.5 or 5 gram dose will deliver
approximately 2.5 mg or 5 mg of hormone systemically.
With this mode of administration, testosterone levels begin
to elevate approximately 30 minutes after the gel is
applied to the body, and substantial elevations in serum
androgen levels are achieved within 4 hours. Testosterone
levels will remain elevated for approximately 24 hours after
administration, so that that the drug is applied once per
day. Regular dosing will provide a steady hormone balance
over each 24-hour period.
History:
AndroGel® was developed in the United States by Unimed
Pharmaceuticals, a division of Solvay. It was approved by
the FDA for sale as a prescription drug in February of 2000.
It is indicated for use in adult males with conditions
associated with a deficiency or absence of endogenous
testosterone. This includes cases of primary
hypogonadism, which may be caused by cryptorchidism,
bilateral torsion, orchitis, vanishing testis syndrome,
orchiectomy, Klinefelter's syndrome, chemotherapy, or
alcohol/heavy metal toxicity. It is also prescribed to treat
hypogonadotrophic hypogonadism, including patients
with luteinizing hormone or luteinizing hormone-releasing
hormone (LHRH) deficiency caused by tumors, injury, or
radiation. Primary hypogonadism is usually characterized
by low testosterone and high gonadotropin (LH/FSH)
levels, while hypogonadotrophic hypogonadism is usually
associated with low testosterone and low to normal
gonadotropin levels. AndroGel® is said to have a clinical
success rate of 870/0, perhaps owing to the greater patient
comfort and compliance this form of testosterone offers in
comparison with hormone injections.
Other transdermal testosterone hydroalcoholic gels have
been released in the U.S. and abroad since the introduction
of AndroGel®. Testim® by Auxilium Pharmaceuticals is
perhaps the most well-known competing brand, sold
widely in the U.S. and Europe. This product also comes in
the form of a 1% testosterone gel claiming a 10% level of
bioavailability. Studies have demonstrated that Testim®
delivers as much as 380/0 more free testosterone for a given
dose compared to AndroGel®, however.419 Testim® is
noted to use a thicker and stickier gel compared to
AndroGel®, which may explain the greater transfer of
hormone. In January 2006, the FDA approved the first
generic testosterone gel in the U.S., made by Watson
Pharmaceuticals. Testosterone gels are one of the most
popular methods of testosterone delivery in clinical
medicine at the present time, and are likely to be soon
found in every market globally that supports an active
hormone replacement therapy industry.
How Supplied:
Hydroalcoholic transdermal testosterone gels are available
in many human drug markets. Composition and dosage
may vary by country and manufacturer, but usually contain
1% testosterone by weight; packaged in volume tubes or
single-dose packets containing 2.5 grams or 5 grams of gel.
AndroGel® (U.S.) is also produced in a pump dispenser
containing 75 grams of gel, which delivers 60 metered
applications of 1.25 grams each.
Structural Characteristics:
AndroGel® is a hydroalcoholic gel containing 1% of
testosterone (free) by weight. It is designed to provide a
continuous transdermal delivery of testosterone for 24
hours following application to the skin. Approximately 100/0
of the applied dose is absorbed across the skin during each
24-hour period.
Side Effects (Estrogenic):
Testosterone is readily aromatized in the body to estradiol
(estrogen). The aromatase (estrogen synthetase) enzyme
is responsible for this metabolism of testosterone.
Elevated estrogen levels ca n ca use side effects such as
increased water retention, body fat gain, and
gynecomastia. Testosterone is considered a moderately
estrogenic steroid. Exceeding therapeutic doses will
increase the likelihood of estrogenic side effects. In such
cases, an anti-estrogen such as clomiphene citrate or
tamoxifen citrate is commonly applied to prevent
estrogenic side effects. One may alternately use an
aromatase inhibitor like Arimidex® (anastrozole), which
more efficiently controls estrogen by preventing its
synthesis. Aromatase inhibitors can be quite expensive in
comparison to anti-estrogens, however, and may also
have negative effects on blood lipids.
Side Effects (Androgenic):
Testosterone is the primary male androgen, responsible
for maintaining secondary male sexual characteristics.
Exceeding normal therapeutic doses is 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 testosterone. These may include
deepening of the voice, menstrual irregularities, changes
in skin texture, facial hair growth, and clitoral
enlargement.
In androgen-responsive target tissues such as the skin,
scalp, and prostate, the high relative androgenicity of
testosterone is dependant on its reduction to
dihydrotestosterone (DHT). The S-alpha reductase
enzyme is responsible for this metabolism of
testosterone. The concurrent use of a S-alpha reductase
inhibitor such as finasteride or dutasteride will interfere
with site-specific potentiation of testosterone action,
lowering the tendency of testosterone drugs to produce
androgenic side effects. It is important to remember that
anabolic and androgenic effects are both mediated via
the cytosolic androgen receptor. Complete separation of
testosterone's anabolic and androgenic properties is not
possible, even with totalS-alpha reductase inhibition.
Side Effects (Hepatotoxicity):
Testosterone does not have hepatotoxic effects; liver
toxicity is unlikely. One study examined the potential for
hepatotoxicity with high doses of testosterone by
administering 400 mg of the hormone per day (2,800 mg
per week) to a group of male subjects. The steroid was
taken orally so that higher peak concentrations would be
reached in hepatic tissues compared to intramuscular
injections. The hormone was given daily for 20 days, and
produced no significant changes in liver enzyme values
including serum albumin, bilirubin, alanine-aminotransferase,
and alkaline phosphatases.42o
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.
Anabolic/androgenic steroids may also adversely effect
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
testosterone used to correct insufficient androgen
production in otherwise healthy aging men are unlikely to
increase atherogenic risk, and may actually reduce the risk
of cardiovascular mortality.
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.
Testosterone is the primary male androgen, and offers
strong negative feedback on endogenous testosterone
production.Testosterone-based drugs will,likewise, have a
strong effect on the hypothalamic regulation of natural
steroid hormones. 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.
The above side effects are not inclusive. For more detailed
discussion ofpotential side effects, see the Steroid Side Effects
section of this book.
Administration (General):
Testosterone hydroalcoholic gel is applied daily
(preferably in the morning) to intact, clean, dry skin of the
shoulders, upper arms, and/or abdomen. Patients should
be careful about transferring testosterone to their female
partner(s). The prescribing information for AndroGel®
suggests that patients wash their hands immediately with
soap and water after application, and also recommends
covering the application site(s) with clothing after the gel
has dried. Studies with AndroGel® have demonstrated
that female partners of male patients noticed as much as
a doubling of serum testosterone levels following 15
minutes of rigorous skin-on-skin contact. This contact was
initiated between 2 and 12 hours after drug
administration. Testosterone transfer was completely
avoided when the male subjects wore a shirt.
Administration (Men):
To treat androgen insufficiency, the prescribing guidelines
for AndroGel® recommend initiating therapy with a 5g
daily dose (delivering 5 mg of testosterone systemically).
Serum testosterone levels are measured after 14 days, at
which point the physician may adjust upwards to 7.5g or
109 if necessary. For physique- or performanceenhancing
purposes, higher doses would be necessary to
achieve supraphysiological levels of testosterone. The
most common dose here is 20 grams per day, which
delivers approximately 20 mg of testosterone. This level is
sufficient for most users to notice significant gains in
muscle size and strength. Lower doses are also regularly
used by some athletes, but typically when accompanied
by other anabolic/androgenic steroids. Testosterone is
ultimately very versatile, and can be combined with many
other anabolic/androgenic steroids to tailor the desired
effect.
Administration (Women):
Hydroalcoholic transdermal testosterone gels are not FDA
approved for use in women. Testosterone is not
recommended for women for physique- or performanceenhancing
purposes due to its strong androgenic nature
and tendency to produce virilizing side effects.
Availability:
Given their high relative price and low delivery of
testosterone, hydroa Icoholic transdermaI testosterone
gels are not commonly traded on the black market.
Counterfeits have not yet been widely reported. The
various AndroGel® and Testim® preparations can
probably be considered real if located.
Author William Llewellyn's ANABBLleS, 9th ed.
Anabolic 100
Chemical Names 4-androsten-3-one-17beta-ol
17beta-hydroxy-a ndrost-4-en-3-one
Estrogenic Activity moderate
Progestational Activity low
Description:
AndroGel® is a transdermal hydroalcoholic testosterone
gel that contains a 1% concentration of testosterone by
weight. It was originally released in 2.5 gram and 5-gram
sachets, equating to a total per-application testosterone
dose of 25 mg and 50 mg respectively. The AndroGel®
prescribing information states that the product has a
transdermal bioavailability of approximately 10% • This
means that each 2.5 or 5 gram dose will deliver
approximately 2.5 mg or 5 mg of hormone systemically.
With this mode of administration, testosterone levels begin
to elevate approximately 30 minutes after the gel is
applied to the body, and substantial elevations in serum
androgen levels are achieved within 4 hours. Testosterone
levels will remain elevated for approximately 24 hours after
administration, so that that the drug is applied once per
day. Regular dosing will provide a steady hormone balance
over each 24-hour period.
History:
AndroGel® was developed in the United States by Unimed
Pharmaceuticals, a division of Solvay. It was approved by
the FDA for sale as a prescription drug in February of 2000.
It is indicated for use in adult males with conditions
associated with a deficiency or absence of endogenous
testosterone. This includes cases of primary
hypogonadism, which may be caused by cryptorchidism,
bilateral torsion, orchitis, vanishing testis syndrome,
orchiectomy, Klinefelter's syndrome, chemotherapy, or
alcohol/heavy metal toxicity. It is also prescribed to treat
hypogonadotrophic hypogonadism, including patients
with luteinizing hormone or luteinizing hormone-releasing
hormone (LHRH) deficiency caused by tumors, injury, or
radiation. Primary hypogonadism is usually characterized
by low testosterone and high gonadotropin (LH/FSH)
levels, while hypogonadotrophic hypogonadism is usually
associated with low testosterone and low to normal
gonadotropin levels. AndroGel® is said to have a clinical
success rate of 870/0, perhaps owing to the greater patient
comfort and compliance this form of testosterone offers in
comparison with hormone injections.
Other transdermal testosterone hydroalcoholic gels have
been released in the U.S. and abroad since the introduction
of AndroGel®. Testim® by Auxilium Pharmaceuticals is
perhaps the most well-known competing brand, sold
widely in the U.S. and Europe. This product also comes in
the form of a 1% testosterone gel claiming a 10% level of
bioavailability. Studies have demonstrated that Testim®
delivers as much as 380/0 more free testosterone for a given
dose compared to AndroGel®, however.419 Testim® is
noted to use a thicker and stickier gel compared to
AndroGel®, which may explain the greater transfer of
hormone. In January 2006, the FDA approved the first
generic testosterone gel in the U.S., made by Watson
Pharmaceuticals. Testosterone gels are one of the most
popular methods of testosterone delivery in clinical
medicine at the present time, and are likely to be soon
found in every market globally that supports an active
hormone replacement therapy industry.
How Supplied:
Hydroalcoholic transdermal testosterone gels are available
in many human drug markets. Composition and dosage
may vary by country and manufacturer, but usually contain
1% testosterone by weight; packaged in volume tubes or
single-dose packets containing 2.5 grams or 5 grams of gel.
AndroGel® (U.S.) is also produced in a pump dispenser
containing 75 grams of gel, which delivers 60 metered
applications of 1.25 grams each.
Structural Characteristics:
AndroGel® is a hydroalcoholic gel containing 1% of
testosterone (free) by weight. It is designed to provide a
continuous transdermal delivery of testosterone for 24
hours following application to the skin. Approximately 100/0
of the applied dose is absorbed across the skin during each
24-hour period.
Side Effects (Estrogenic):
Testosterone is readily aromatized in the body to estradiol
(estrogen). The aromatase (estrogen synthetase) enzyme
is responsible for this metabolism of testosterone.
Elevated estrogen levels ca n ca use side effects such as
increased water retention, body fat gain, and
gynecomastia. Testosterone is considered a moderately
estrogenic steroid. Exceeding therapeutic doses will
increase the likelihood of estrogenic side effects. In such
cases, an anti-estrogen such as clomiphene citrate or
tamoxifen citrate is commonly applied to prevent
estrogenic side effects. One may alternately use an
aromatase inhibitor like Arimidex® (anastrozole), which
more efficiently controls estrogen by preventing its
synthesis. Aromatase inhibitors can be quite expensive in
comparison to anti-estrogens, however, and may also
have negative effects on blood lipids.
Side Effects (Androgenic):
Testosterone is the primary male androgen, responsible
for maintaining secondary male sexual characteristics.
Exceeding normal therapeutic doses is 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 testosterone. These may include
deepening of the voice, menstrual irregularities, changes
in skin texture, facial hair growth, and clitoral
enlargement.
In androgen-responsive target tissues such as the skin,
scalp, and prostate, the high relative androgenicity of
testosterone is dependant on its reduction to
dihydrotestosterone (DHT). The S-alpha reductase
enzyme is responsible for this metabolism of
testosterone. The concurrent use of a S-alpha reductase
inhibitor such as finasteride or dutasteride will interfere
with site-specific potentiation of testosterone action,
lowering the tendency of testosterone drugs to produce
androgenic side effects. It is important to remember that
anabolic and androgenic effects are both mediated via
the cytosolic androgen receptor. Complete separation of
testosterone's anabolic and androgenic properties is not
possible, even with totalS-alpha reductase inhibition.
Side Effects (Hepatotoxicity):
Testosterone does not have hepatotoxic effects; liver
toxicity is unlikely. One study examined the potential for
hepatotoxicity with high doses of testosterone by
administering 400 mg of the hormone per day (2,800 mg
per week) to a group of male subjects. The steroid was
taken orally so that higher peak concentrations would be
reached in hepatic tissues compared to intramuscular
injections. The hormone was given daily for 20 days, and
produced no significant changes in liver enzyme values
including serum albumin, bilirubin, alanine-aminotransferase,
and alkaline phosphatases.42o
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.
Anabolic/androgenic steroids may also adversely effect
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
testosterone used to correct insufficient androgen
production in otherwise healthy aging men are unlikely to
increase atherogenic risk, and may actually reduce the risk
of cardiovascular mortality.
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.
Testosterone is the primary male androgen, and offers
strong negative feedback on endogenous testosterone
production.Testosterone-based drugs will,likewise, have a
strong effect on the hypothalamic regulation of natural
steroid hormones. 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.
The above side effects are not inclusive. For more detailed
discussion ofpotential side effects, see the Steroid Side Effects
section of this book.
Administration (General):
Testosterone hydroalcoholic gel is applied daily
(preferably in the morning) to intact, clean, dry skin of the
shoulders, upper arms, and/or abdomen. Patients should
be careful about transferring testosterone to their female
partner(s). The prescribing information for AndroGel®
suggests that patients wash their hands immediately with
soap and water after application, and also recommends
covering the application site(s) with clothing after the gel
has dried. Studies with AndroGel® have demonstrated
that female partners of male patients noticed as much as
a doubling of serum testosterone levels following 15
minutes of rigorous skin-on-skin contact. This contact was
initiated between 2 and 12 hours after drug
administration. Testosterone transfer was completely
avoided when the male subjects wore a shirt.
Administration (Men):
To treat androgen insufficiency, the prescribing guidelines
for AndroGel® recommend initiating therapy with a 5g
daily dose (delivering 5 mg of testosterone systemically).
Serum testosterone levels are measured after 14 days, at
which point the physician may adjust upwards to 7.5g or
109 if necessary. For physique- or performanceenhancing
purposes, higher doses would be necessary to
achieve supraphysiological levels of testosterone. The
most common dose here is 20 grams per day, which
delivers approximately 20 mg of testosterone. This level is
sufficient for most users to notice significant gains in
muscle size and strength. Lower doses are also regularly
used by some athletes, but typically when accompanied
by other anabolic/androgenic steroids. Testosterone is
ultimately very versatile, and can be combined with many
other anabolic/androgenic steroids to tailor the desired
effect.
Administration (Women):
Hydroalcoholic transdermal testosterone gels are not FDA
approved for use in women. Testosterone is not
recommended for women for physique- or performanceenhancing
purposes due to its strong androgenic nature
and tendency to produce virilizing side effects.
Availability:
Given their high relative price and low delivery of
testosterone, hydroa Icoholic transdermaI testosterone
gels are not commonly traded on the black market.
Counterfeits have not yet been widely reported. The
various AndroGel® and Testim® preparations can
probably be considered real if located.
Author William Llewellyn's ANABBLleS, 9th ed.
Last edited:
