Agovirin Depot (testosterone isobutyrate) injectable anabolic androgenic steroid

akn · Jun 20, 2014

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Testosterone isobutyrate is an injectable steroid preparation
that contains the isobutyrate ester of testosterone in a water
base. Among bodybuilders, testosterone isobutyrate is often
considered analogous to testosterone suspension (no ester).
Although both are usually found as water-based suspensions,
the pharmacokinetics of the two products are admittedly very
different. While testosterone (free) suspension is very fastacting,
requiring injections to be given every few days,
testosterone isobutyrate is much slower to release, and is
usually administered once every two weeks in a clinical
setting. As an injectable testosterone, testosterone isobutyrate
is favored for its ability to promote rapid gains in muscle
mass and strength.
History:
Injectable testosterone isobutyrate microcrystal suspension
was first described in 1952.379 This agent was developed in
an effort to create an injectable (depot) form of testosterone
that would be slower acting that regular (free) testosterone
suspension or testosterone propionate, the most widely
prescribed forms of testosterone at the time. This is
accomplished by providing a microcrystalline depot with
very low water solubility, delaying the release of free
steroid into the bloodstream. Although effective for this
purpose, testosterone isobutyrate was developed at a time
when many new esters of testosterone were being introduced
to the market. By the mid-1950’s, testosterone enanthate
would emerge as the dominant slow-acting injectable
testosterone, and the isobutyrate ester would ultimately see
little commercial success.
The only modern steroid product to use testosterone
isobutyrate is Agovirin Depot, developed by Biotika in
Czechoslovakia. It is primarily prescribed to treat males
with insufficient androgen levels and adolescents with
delayed puberty, although it is indicated for a variety of other
purposes including the treatment of Klinefelter syndrome (a
disease where an extra chromosome results in an imbalance
of androgenicity and estrogenicity), aplastic anemia,
Cushing’s syndrome (as an anabolic agent to preserve lean
tissue), postmenopausal osteoporosis, advanced breast
cancer, mastodynia (breast pain), and cachexia (wasting of
the body due to severe illness). Agovirin Depot is still
produced by Biotika (currently in the Slovak Republic), and
remains a popular export to European black markets.

Structural Characteristics:
Testosterone isobutyrate is a modified form of testosterone,
where a carboxylic acid ester (2-methyl propionic acid) has
been attached to the 17-beta hydroxyl group. Esterified forms
of testosterone are less polar than free testosterone, and are
absorbed more slowly from the area of injection. Once in the
bloodstream, the ester is removed to yield free (active)
testosterone. Esterified forms of testosterone are designed to
prolong the window of therapeutic effect following
administration, allowing for a less frequent injection
schedule compared to injections of free (unesterified)
steroid. Testosterone isobutyrate microcrystalline suspension
is designed to provide physiological androgen concentrations
for approximately 2 weeks following injection.
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 can cause side effects such as increased
water retention, body fat gain, and gynecomastia.
Testosterone is considered a moderately estrogenic steroid.
An anti-estrogen such as clomiphene citrate or tamoxifen
citrate may be necessary 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.
Estrogenic side effects will occur in a dose-dependant
manner, with higher doses (above normal therapeutic levels)
of testosterone more likely to require the concurrent use of an
anti-estrogen or aromatase inhibitor. Since water retention
and loss of muscle definition are common with higher doses
of testosterone, this drug is usually considered a poor choice
for dieting or cutting phases of training. Its moderate
estrogenicity makes it more ideal for bulking phases, where
the added water retention will support raw strength and
muscle size, and help foster a stronger anabolic environment.
Side Effects (Androgenic):
Testosterone is the primary male androgen, responsible for
maintaining secondary male sexual characteristics. Elevated
levels of testosterone 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.
Those concerned about hair loss may find a more
comfortable option in nandrolone decanoate, which is a
comparably less androgenic steroid. 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 5-alpha reductase enzyme is responsible for this
metabolism of testosterone. The concurrent use of a 5-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 total 5-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-amino-transferase, and alkaline
phosphatases. 380
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 effect
blood pressure and triglycerides, reduce endothelial
relaxation, and support left ventricular hypertrophy, all
potentially increasing the risk of cardiovascular disease and
myocardial infarction.
Testosterone tends to have a much less dramatic impact on
cardiovascular risk factors than synthetic steroids. This is
due in part to its openness to metabolism by the liver, which
allows it to have less effect on the hepatic management of
cholesterol. The aromatization of testosterone to estradiol
also helps to mitigate the negative effects of androgens on
serum lipids. In one study, 280 mg per week of testosterone
ester (enanthate) had a slight but not statistically significant
effect on HDL cholesterol after 12 weeks, but when taken
with an aromatase inhibitor a strong (25%) decrease was
seen.381 Studies using 300 mg of testosterone ester
(enanthate) per week for 20 weeks without an aromatase
inhibitor demonstrated only a 13% decrease in HDL
cholesterol, while at 600 mg the reduction reached 21%.382
The negative impact of aromatase inhibition should be taken
into consideration before such drug is added to testosterone
therapy.
Due to the positive influence of estrogen on serum lipids,
tamoxifen citrate or clomiphene citrate are preferred to
aromatase inhibitors for those concerned with cardiovascular
health, as they offer a partial estrogenic effect in the liver.
This allows them to potentially improve lipid profiles and
offset some of the negative effects of androgens. With doses
of 600 mg or less of testosterone per week, the impact on
lipid profile tends to be noticeable but not dramatic, making
an anti-estrogen (for cardioprotective purposes) perhaps
unnecessary. Doses of 600 mg or less per week have also
failed to produce statistically significant changes in
LDL/VLDL cholesterol, triglycerides, apolipoprotein B/CIII,
C-reactive protein, and insulin sensitivity, all indicating a
relatively weak impact on cardiovascular risk factors.383
When used in moderate doses, injectable testosterone esters
are usually considered to be the safest of all
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. 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.
Administration (General):
The design of testosterone isobutyrate (as Agovirin Depot) is
slightly different than that of most testosterone esters, which
are usually made as oily solutions. Agovirin Depot instead
contains a microcrystalline aqueous suspension.The crystals
form a repository in the muscle following injection, where
they slowly dissolve over time. Injections of testosterone
isobutyrate may require a large needle (21 gauge), and may
result in local irritation, pain, and redness.
Administration (Men):
To treat androgen insufficiency, testosterone isobutyrate
suspension is usually administered in a dose of 50-100 mg
every 14 days. When used for muscle-building purposes,
testosterone isobutyrate suspension is often administered at a
dose of 200-400 mg (4-8ml) per week. Although active for
longer periods of time, weekly injections would be preferred
due to the low dosage and tendency for pain at the site of
injection (large injection volumes would not be advised). To
reduce injection volume, the weekly dosage may be further
subdivided into smaller injections, which are taken every
2nd or 3rd day. Cycles are generally between 6 and 12
weeks in length. This level is sufficient to provide noticeable
gains in muscle size and strength. Testosterone drugs are
ultimately very versatile, and can be combined with many
other anabolic/androgenic steroids depending on the desired
effect.

Availability:
Pharmaceutical preparations containing testosterone
isobutyrate are rare. The only known product at this time is
Agovirin Depot, produced in the Slovak Republic by
Biotika. It contains 50 mg per 2 mL ampule; 5 packaged per
box.

By WL

Agovirin Depot (testosterone isobutyrate) injectable anabolic androgenic steroid

akn

Musclechemistry Member

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