These are substances which cause development of secondary sex characters in the castrated male. That testes are responsible for the male characters is known since prehistoric times. Its endocrine function was established by Berthold in 1849. Testosterone was isolated, its structure worked out and synthesized by the year 1935.
ANDROGENS
(Male Sex Hormones)
These are substances which cause development of secondary sex
characters in the castrated male. That testes are responsible for the male
characters is known since prehistoric times. Its endocrine function was
established by Berthold in 1849. Testosterone
was isolated, its structure worked out
and synthesized by the year 1935.
Testes of adult male
produce 5–12 mg of testosterone daily, a part of which is
converted in extraglandular tissues to the more active dihydrotestosterone; by the enzyme steroid 5 αreductase; cholesterol
is the starting material and the same pathway depicted in Fig. 20.1 is
utilized. Adrenal cortex produces small quantities of dehydroepiandrosterone and androstenedione
which are called ‘weak androgens’ (potency 1/20 to 1/30), but are infact
inactive as such and derive their weak activity from partial conversion to
testosterone by peripheral tissues. Adrenals themselves do not produce
significant quantity of testosterone. In women ovary produces small quantity of
testosterone; this together with that derived indirectly from adrenals amounts
to 0.25–0.5 mg/day.
Androsterone It is a metabolite of
testosterone which is excreted in
urine. It has 1/10 the activity of testosterone.
Methyltestosterone and fluoxymesterone
are 17alkyl substituted derivatives of testosterone which are
orally active because of resistance to first pass metabolism, but have
submaximal androgenic efficacy and potential to cause cholestatic jaundice.
Other orally active compounds are testosterone
undecanoate which administered as oily solution is absorbed through
lymphatics bypassing the liver, and mesterolone.
A number of lipidsoluble esters of testosterone
have been produced, suitable for injection in oily vehicle, from which they are
absorbed slowly and exert prolonged action after deesterification in the body.
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