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TESTOSTERONE
GEL
Testosterone
Transdermal gel: In transdermal testosterone, the
hormone is released slowly through the skin to deliver a constant
level in the blood, again not a routine pattern, but convenient.
Compounding
pharmacists can offer many options to provide for different
blood level profiles and convenience of administration. Topical
testosterone can be applied using different vehicles to more
closely mimic the normal adult physiological pattern, i.e.,
apply early in the morning where it should be absorbed over
a period of a few hours.
Testosterone,
the most common agent used in male hormone replacement therapy,
occurs as white or slightly creamy white crystals or crystalline
powder that is odorless and stable in air. It is practically
insoluble in water, soluble 1 g in 5 mL of ethanol, 2 mL of
chloroform and 100 mL of ether and is soluble in vegetable
oils, melts between 153 and 157ºC., and is subject to photodegradation
in the presence of light. Testosterone is not very bioavailable
when given as an oral-swallow preparation, but is absorbed
when administered bucally and sublingually. The different
esters of testosterone are hydrolyzed to free testosterone
and, subsequently, are metabolized in the same way as testosterone
itself .
Treatment
The therapeutic goal is enable the adult man to maintain or
improve strength to function better and more consistently.
Many physicians hesitate to use testosterone supplementation
as it is new, they have heard stories (sometimes related to
synthetic androgen supplementation), and they are unsure of
the results as it takes quite some time for them to become
evident. There is no evidence that exogenous testosterone
stimulates the development of prostate carcinoma; there has
been no relationship established between endogenous testosterone
and BPH. However, a contraindication to androgen replacement
therapy is the presence of prostate cancer.
Who
qualifies for testosterone therapy programs.
The decision to use HRT is an individual one, based on the
individual's particular risks. The goals of natural HRT are
to:
-
Alleviate the symptoms caused by the natural decrease in
production
of hormones by the body.
-
Replace
the hormones to the extent to provide positive benefits.
-
Bring
the body back to normal hormonal balance.
-
Imitate
the body's natural processes as much as possible.
Natural
testosterone replacement is central to the treatment of all
aspects of "male menopause". Testosterone
supplementation has resulted in decreasing body fat mass from
6.4% to 1.4% and increases in lean mass from 3.2% to 5%.
Increases in strength (grip strength) also are reported.
Total
cholesterol and low density lipoproteins tend to significantly
decrease with testosterone administration. Three steroids
of importance in the male reproductive function are testosterone,
dihydrotestosterone and estradiol. By far the greatest
percentage of testosterone (over 95%) is secreted by the testicular
Leydig cells. The dihydrotestosterone and estradiol
are derived from both the direct secretion from the testes
(20%) and also from conversion in peripheral tissues on androgen
and estrogen precursors secreted by both the testes and adrenal
glands (80%).
Hormone
preparations that have been used include testosterone, testosterone
propionate, testosterone enanthate, testosterone cypionate,
fluoxymestrone, methyltestosterone (methyltestosterone is
toxic to the liver and heart and may have clouded the benefits
of testosterone replacement therapy), oxandrolone, progesterone,
and estradiol. Commercial testosterone products have
been administered either by injection, implants/pellets, orally
or as transdermal patches.
Possible
side effects
The goal of testosterone replacement therapy is to achieve
normal to optimal levels of testosterone. For most patients,
testosterone replacement therapy is safe. Possible side effects,
however, include water retention, male pattern baldness, gynecomastia
(enlarged breasts). The oral forms are also associated with
liver problems. The use of large doses of testosterone (in
bodybuilding, for example) increases the risks of side effects.
Decreased normal testosterone production, prolonged or excessive
testosterone therapy prompts the pituitary gland to stop producing
the hormone gonadotropin. This in turn, surpresses normal
testosterone and sperm production, accompanied by shrinkage
of the testicles and frequent or continuing (and sometimes
painful) erections. Because of this, testosterone replacement
therapy is usually prescribed in cycles. After a 2- or 3-month
period, the patient takes a different drug (such as HCG) that
stimulates the testicles to begin production of natural testosterone
again.
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