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ANDROGENS MALE SEX
HORMONES
Mohamed khalid Ali Newera
• Pharmacological
actions
• Pharmacokinetics
• Therapeutic uses
• Adverse effects
• Anti-androgens
• Androgens are the substances which
cause development of secondary sex
characters in castrated male
• Testes are responsible for male
characters
• Testes Functions:
1. Spermatogenesis occurring within the
seminiferous tubules
2. Production of Androgenic hormones
Natural Androgens:
From Testes:
Testosterone (5-12 mg daily)
Dihydrotestosterone (more active) by 5 α-
reductase
From Adrenal cortex: (weak androgens)
Dehydroepiandrosterone
Androstenedione
{Females testosterone: 0.25 – 0.5 mg/day
(ovary + adrenals)}
Androsterone – metabolite of testosterone
Synthetic androgens:
Methyltestosterone, Fluoxymesterone
Propionate and enanthate
Testosterone undecanoate and
Mesterolone
Testes:
•Promotion of spermatogenesis and maturation of sperm
•Moderately high dose causes testicular atrophy by inhibiting Gn
secretion
Androgenic Effects:
In the foetus, testosterone promotes development of male
reproductive tract – internal genitalia, vas deferens, epididymis
and external genitalia (sex differentiation)
During puberty, testosterone promotes development of :
primary sexual characteristics (e.g. enlargement of penis, scrotum
and testes)
secondary sexual characteristics (e.g. male body shape,
axillary/pubic hair, deeper pitch of voice, thickeing of skin –
greasy, loss of subcuaneous fat) - Adulthood: Baldness, BHP,
Prostatic cancer
Pubertal spurt of growth at
puberty – both boy and girl
Bone growth – thickness and
length
Estrogen from testosterone – fuse
of bones and mineralization
Muscle building – if aided by
exercise
Positive nitrogen, minerals and
water balance – increase in weight
Increase in appetite
Acceleration of erythropoiesis
Absorption: undergoes high first pass
metabolism. Therefore IM injections or
synthetic preparations are used
Transport: highly protein bound
Metabolism:
by liver enzymes : androsterone &
etiocholanolone
excretion by urine after conjugation
small quantity of oestrogen also produced
from testosterone
N.B. Testosterone is ineffective orally (inactivated
by liver), and is usually given as i.m. injections of
testosterone esters
Androgen replacement therapy (ART)
ART uses derivatives of testosterone, rather than
synthetic Androgens, because they are safe, effective
and easy to monitor
1.Androgen deficiency: clinical diagnosis confirmed by
hormone assays
is usually caused by
underlying testicular disorders (high LH, but
low testosterone levels)
hypothalamic-pituitary disorders (low LH and
low testosterone levels)
Goal: Mimic the normal testosterone concentration as
closely as possible (serum concentration monitoring)
If untreated, does not shorten life expectancy, but is
associated with significant morbidity (ambiguous
genitalia, delayed puberty & infertility)
Treated by androgen replacement therapy (ART),
usually for the remainder of life. The aim is to restore
tissue androgen exposure by using the natural
androgen testosterone
2. Hypopituitarism
Monitoring at anticipated time of puberty
3. AIDS related muscle wasting
4. Hereditary angioneurotic edema
(methyltestosterone)
5. Ageing
Misuse: involves prescription with no
acceptable medical indication
Examples of misuse include:
male infertility
male sexual dysfunction or impotence
ale e opause (andropause)
no convincing evidence that androgen therapy
is either effective treatment or safe for older
men unless there is frank androgen deficiency
Virilization:
may occur in women receiving relatively
high doses for prolonged periods, such
as for estrogen-dependent mammary
carcinoma
Cholestatic Jaundice
may be produced by steroids possessing
a 17-alkyl substituted group
Priapism (sustained erection)
Oligospermia
Oedema--via promotion of salt and water
retention
Precocious puberty and short stature
Acne
Hepatic carcinoma`````
Gynaecomastia
Synthetic androgens – higher anabolic
but lower androgenic activity
Uses:
1. Catabolic states: Acute illness, severe
trauma, major surgery
2. Renal insufficiency
3. Osteoporosis
4. Suboptimal growth in boys
5. Anaemia
6. Perfomance enhancement
• Danazol
• Cyproterone acetate
• Flutamide
• Finasteride attenuat
Danazol
• Uses:
– Endometriosis
– Menorrhagia
– Fibrocystic breast disease
– Hereditary angioneurotic edema
– Gynecomastia
– Infertility
Flutamide
Uses:
• Cancer of prostate along with GnRH
agonist
• Female hirusitism
Finasteride
Uses:
1. Benign prostatic hypertrophy
2. decrease in prostate volume
3. improved urinary flow
4. reversion of disease progression
5. Male pattern baldness

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Androgens male sex hormones

  • 2. • Pharmacological actions • Pharmacokinetics • Therapeutic uses • Adverse effects • Anti-androgens
  • 3. • Androgens are the substances which cause development of secondary sex characters in castrated male • Testes are responsible for male characters • Testes Functions: 1. Spermatogenesis occurring within the seminiferous tubules 2. Production of Androgenic hormones
  • 4. Natural Androgens: From Testes: Testosterone (5-12 mg daily) Dihydrotestosterone (more active) by 5 α- reductase From Adrenal cortex: (weak androgens) Dehydroepiandrosterone Androstenedione {Females testosterone: 0.25 – 0.5 mg/day (ovary + adrenals)} Androsterone – metabolite of testosterone Synthetic androgens: Methyltestosterone, Fluoxymesterone Propionate and enanthate Testosterone undecanoate and Mesterolone
  • 5. Testes: •Promotion of spermatogenesis and maturation of sperm •Moderately high dose causes testicular atrophy by inhibiting Gn secretion Androgenic Effects: In the foetus, testosterone promotes development of male reproductive tract – internal genitalia, vas deferens, epididymis and external genitalia (sex differentiation) During puberty, testosterone promotes development of : primary sexual characteristics (e.g. enlargement of penis, scrotum and testes) secondary sexual characteristics (e.g. male body shape, axillary/pubic hair, deeper pitch of voice, thickeing of skin – greasy, loss of subcuaneous fat) - Adulthood: Baldness, BHP, Prostatic cancer
  • 6. Pubertal spurt of growth at puberty – both boy and girl Bone growth – thickness and length Estrogen from testosterone – fuse of bones and mineralization Muscle building – if aided by exercise Positive nitrogen, minerals and water balance – increase in weight Increase in appetite Acceleration of erythropoiesis
  • 7. Absorption: undergoes high first pass metabolism. Therefore IM injections or synthetic preparations are used Transport: highly protein bound Metabolism: by liver enzymes : androsterone & etiocholanolone excretion by urine after conjugation small quantity of oestrogen also produced from testosterone N.B. Testosterone is ineffective orally (inactivated by liver), and is usually given as i.m. injections of testosterone esters
  • 8. Androgen replacement therapy (ART) ART uses derivatives of testosterone, rather than synthetic Androgens, because they are safe, effective and easy to monitor 1.Androgen deficiency: clinical diagnosis confirmed by hormone assays is usually caused by underlying testicular disorders (high LH, but low testosterone levels) hypothalamic-pituitary disorders (low LH and low testosterone levels) Goal: Mimic the normal testosterone concentration as closely as possible (serum concentration monitoring) If untreated, does not shorten life expectancy, but is associated with significant morbidity (ambiguous genitalia, delayed puberty & infertility) Treated by androgen replacement therapy (ART), usually for the remainder of life. The aim is to restore tissue androgen exposure by using the natural androgen testosterone
  • 9. 2. Hypopituitarism Monitoring at anticipated time of puberty 3. AIDS related muscle wasting 4. Hereditary angioneurotic edema (methyltestosterone) 5. Ageing Misuse: involves prescription with no acceptable medical indication Examples of misuse include: male infertility male sexual dysfunction or impotence ale e opause (andropause) no convincing evidence that androgen therapy is either effective treatment or safe for older men unless there is frank androgen deficiency
  • 10. Virilization: may occur in women receiving relatively high doses for prolonged periods, such as for estrogen-dependent mammary carcinoma Cholestatic Jaundice may be produced by steroids possessing a 17-alkyl substituted group Priapism (sustained erection) Oligospermia Oedema--via promotion of salt and water retention Precocious puberty and short stature Acne Hepatic carcinoma````` Gynaecomastia
  • 11. Synthetic androgens – higher anabolic but lower androgenic activity Uses: 1. Catabolic states: Acute illness, severe trauma, major surgery 2. Renal insufficiency 3. Osteoporosis 4. Suboptimal growth in boys 5. Anaemia 6. Perfomance enhancement
  • 12. • Danazol • Cyproterone acetate • Flutamide • Finasteride attenuat
  • 13. Danazol • Uses: – Endometriosis – Menorrhagia – Fibrocystic breast disease – Hereditary angioneurotic edema – Gynecomastia – Infertility
  • 14. Flutamide Uses: • Cancer of prostate along with GnRH agonist • Female hirusitism
  • 15. Finasteride Uses: 1. Benign prostatic hypertrophy 2. decrease in prostate volume 3. improved urinary flow 4. reversion of disease progression 5. Male pattern baldness