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Sex hormones
Dr. Chavan P.R.
Classification of hormones
Hormones
o Body's chemical messengers.
o Travel in your bloodstream to tissues or organs.
o Work slowly, over time, and affect many different
processes, including
 Growth and development
 Metabolism - how your body gets energy from the
foods you eat
 Sexual function
 Reproduction
 Mood
Sex hormones
 Testosterone
 Estrogen
 Progesterone
 Inhibin
 Relaxin
Testosterone
 Male sex hormone
 Develop secondary sex
characters in the
castrated male.
 Its endocrine function
was established by
Berthold in 1849.
 It was synthetically
prepared by the year
1935.
Actions
1. Sex organs and secondary sex characters (Androgenic)
-Testosterone is responsible for all the changes that occur
in a boy at puberty
2. Testes
- spermatogenesis and maturation of spermatozoa
3. Skeleton and skeletal muscles (Anabolic)
- There is rapid bone growth, both in thickness as well as in
length
4. Erythropoiesis
Side effects
1. Virilization
2. Acne
3. painful erections
4. Oligozoospermia
5. Precocious puberty, premature sexual behaviour,
and stunting of stature due to early closure of
epiphysis
6. Salt retention and edema
7. Cholestatic jaundice
8. Hepatic carcinoma
9. Gynaecomastia
10. Lowering of HDL and rise in LDL levels
Contraindications
 Carcinoma of prostate and male breast
 Liver and kidney disease
 During pregnancy (masculinization of female foetus)
 Age >65 years, and those with coronary artery
disease or CHF
 Androgen therapy can worsen sleep apnoea,
migraine and epilepsy.
Uses
1. Testicular failure
2. Hypopituitarism
3. AIDS related muscle wasting
4. Hereditary angioneurotic edema
5. Ageing
6. Idiopathic male infertility
Synthesis of Estrogen & Progesterone
Mechanism of action of estrogen
Actions
1. Regulation of sex organ functions, pubertal growth
and development
2. Development of secondary sex characters
3. Metabolic effects
Pharmacokinetics
 Absorption oral and transdermal but natural
estrogens are inactive by the oral route due to
rapid metabolism in liver.
 Large plasma protein binding— to shbg as well
as to albumin.
 Estradiol -- estrone --estriol
 Glucuronic acid and sulfate conjugation
 Excretion -urine and bile
 T½ 12–24 hours
Adverse Effects
1. Suppression of libido, gynaecomastia and
feminization in males.
2. Fusion of epiphyses and reduction of adult stature in
children.
3. Increase the risk of irregular bleeding and
endometrial carcinoma in postmenopausal women
4. Acceleration of growth of existing breast cancer
5. Gallstones, benign hepatomas
6. Migraine, epilepsy and endometriosis
7. Increased incidence of vaginal and cervical
carcinoma, genital abnormalities
Estrogens are contraindicated during pregnancy.
Uses
 Hormone replacement therapy (HRT)
 Menopausal symptoms and atrophic changes
 Osteoporosis and fracture
 Cardiovascular events
 Cognitive function and dementia
 Cancer
 Gallstone, migraine
 Senile vaginitis
 Delayed puberty in girls
 Dysmenorrhoea
 Acne
 Dysfunctional uterine bleeding
 Carcinoma prostate
Progesterone mechanism of action
Actions
1. Uterus - secretory changes in the estrogen primed
endometrium: hyperemia, tortuocity of glands and
increased secretion occurs while epithelial proliferation
is halted
2. Cervix - converts the watery cervical secretion induced
by estrogens to viscid, scanty and cellular secretion
which is hostile to sperm penetration.
3. Vagina - induces pregnancy like changes in the vaginal
mucosa: leukocyte infiltration of cornified epithelium
occurs.
4. Breast - causes proliferation of acini in the mammary
5. CNS - High circulating concentration of progesterone
(during pregnancy) appears to have a sedative effect.
It can also affect mood.
6. Body temperature - A slight (0.5oc) rise in body
temperature by resetting the hypothalamic thermostat
and increasing heat production is induced
7. Respiratory – Stimulation of respiration
8. Metabolism
9. Pituitary - Weak inhibitor of Gn secretion from pituitary.
Pharmacokinetics
 Inactive orally
 Mostly injected i.M. In oily solution
 Excreted in urine
 Metabolism - glucuronide and sulfate conjugates
 Absorption occurs through lymphatic's bypassing
liver
 Though bioavailability is low, effective
concentrations are attained in the body
 T½ 8–24 hours.
Adverse effects
 Breast engorgement, headache, rise in body
temperature, edema, esophageal reflux, acne and
mood swings may occur with higher doses
 Irregular bleeding or amenorrhea
 Long-term use of progestin in HRT may increase the
risk of breast cancer
 Blood sugar may rise and diabetes may be
precipitated
 Masculinization of female foetus and other
congenital abnormalities.
Uses
1. As contraceptive
2. Hormone replacement therapy (HRT)
3. Dysfunctional uterine bleeding
4. Endometriosis
5. Premenstrual syndrome/tension
6. Threatened/habitual abortion
7. Endometrial carcinoma
Inhibin Synthesis
Mechanism
Actions
 Inhibin designated inhibin-A and Inhibin-B.
 It secreted by the gonads by Sertoli cells in the male
and the granulosa cells in the female.
 It inhibit the production of follicle-stimulating
hormone (FSH) by the pituitary gland .
 The inhibins are also involved in the control of the
production of gametes and embryonic and fetal
development .
Side Effects
 Down syndrome
 Inhibin-A is included in the maternal serum screening
tests for Down syndrome in the second trimester of
pregnancy .
Relaxin
 In women, relaxin is secreted into the circulation by
the corpus luteum in the ovary and during pregnancy
it released from the placenta.
 In men, relaxin is secreted from the prostate gland
and can be detected in the semen, but is not
generally found in the blood circulation.
 The role of relaxin in men is less clear. However,
there is evidence that it may increase the movement
of sperm cells in the semen.
Mechanism & Synthesis
Actions
 Relaxin levels in the circulation rise after ovulation and
relax the wall of the uterus by inhibiting contractions, and
it also prepares the lining of the uterus for pregnancy.
 In early pregnancy relaxin inhibits contractions in the wall
of the uterus, to prevent premature childbirth.
 In first trimester of pregnancy relaxin promote
implantation of the developing fetus into the wall of the
uterus and the growth of the placenta.
 Relaxin decreases tissue fibrosis in the kidney, heart,
lungs and liver, and promotes wound healing.
Thank you

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sex hormones pharmacology

  • 3. Hormones o Body's chemical messengers. o Travel in your bloodstream to tissues or organs. o Work slowly, over time, and affect many different processes, including  Growth and development  Metabolism - how your body gets energy from the foods you eat  Sexual function  Reproduction  Mood
  • 4. Sex hormones  Testosterone  Estrogen  Progesterone  Inhibin  Relaxin
  • 5. Testosterone  Male sex hormone  Develop secondary sex characters in the castrated male.  Its endocrine function was established by Berthold in 1849.  It was synthetically prepared by the year 1935.
  • 6.
  • 7. Actions 1. Sex organs and secondary sex characters (Androgenic) -Testosterone is responsible for all the changes that occur in a boy at puberty 2. Testes - spermatogenesis and maturation of spermatozoa 3. Skeleton and skeletal muscles (Anabolic) - There is rapid bone growth, both in thickness as well as in length 4. Erythropoiesis
  • 8. Side effects 1. Virilization 2. Acne 3. painful erections 4. Oligozoospermia 5. Precocious puberty, premature sexual behaviour, and stunting of stature due to early closure of epiphysis 6. Salt retention and edema 7. Cholestatic jaundice 8. Hepatic carcinoma 9. Gynaecomastia 10. Lowering of HDL and rise in LDL levels
  • 9. Contraindications  Carcinoma of prostate and male breast  Liver and kidney disease  During pregnancy (masculinization of female foetus)  Age >65 years, and those with coronary artery disease or CHF  Androgen therapy can worsen sleep apnoea, migraine and epilepsy.
  • 10. Uses 1. Testicular failure 2. Hypopituitarism 3. AIDS related muscle wasting 4. Hereditary angioneurotic edema 5. Ageing 6. Idiopathic male infertility
  • 11. Synthesis of Estrogen & Progesterone
  • 12. Mechanism of action of estrogen
  • 13. Actions 1. Regulation of sex organ functions, pubertal growth and development 2. Development of secondary sex characters 3. Metabolic effects
  • 14. Pharmacokinetics  Absorption oral and transdermal but natural estrogens are inactive by the oral route due to rapid metabolism in liver.  Large plasma protein binding— to shbg as well as to albumin.  Estradiol -- estrone --estriol  Glucuronic acid and sulfate conjugation  Excretion -urine and bile  T½ 12–24 hours
  • 15. Adverse Effects 1. Suppression of libido, gynaecomastia and feminization in males. 2. Fusion of epiphyses and reduction of adult stature in children. 3. Increase the risk of irregular bleeding and endometrial carcinoma in postmenopausal women 4. Acceleration of growth of existing breast cancer 5. Gallstones, benign hepatomas 6. Migraine, epilepsy and endometriosis 7. Increased incidence of vaginal and cervical carcinoma, genital abnormalities Estrogens are contraindicated during pregnancy.
  • 16. Uses  Hormone replacement therapy (HRT)  Menopausal symptoms and atrophic changes  Osteoporosis and fracture  Cardiovascular events  Cognitive function and dementia  Cancer  Gallstone, migraine  Senile vaginitis  Delayed puberty in girls  Dysmenorrhoea  Acne  Dysfunctional uterine bleeding  Carcinoma prostate
  • 18. Actions 1. Uterus - secretory changes in the estrogen primed endometrium: hyperemia, tortuocity of glands and increased secretion occurs while epithelial proliferation is halted 2. Cervix - converts the watery cervical secretion induced by estrogens to viscid, scanty and cellular secretion which is hostile to sperm penetration. 3. Vagina - induces pregnancy like changes in the vaginal mucosa: leukocyte infiltration of cornified epithelium occurs. 4. Breast - causes proliferation of acini in the mammary
  • 19. 5. CNS - High circulating concentration of progesterone (during pregnancy) appears to have a sedative effect. It can also affect mood. 6. Body temperature - A slight (0.5oc) rise in body temperature by resetting the hypothalamic thermostat and increasing heat production is induced 7. Respiratory – Stimulation of respiration 8. Metabolism 9. Pituitary - Weak inhibitor of Gn secretion from pituitary.
  • 20. Pharmacokinetics  Inactive orally  Mostly injected i.M. In oily solution  Excreted in urine  Metabolism - glucuronide and sulfate conjugates  Absorption occurs through lymphatic's bypassing liver  Though bioavailability is low, effective concentrations are attained in the body  T½ 8–24 hours.
  • 21. Adverse effects  Breast engorgement, headache, rise in body temperature, edema, esophageal reflux, acne and mood swings may occur with higher doses  Irregular bleeding or amenorrhea  Long-term use of progestin in HRT may increase the risk of breast cancer  Blood sugar may rise and diabetes may be precipitated  Masculinization of female foetus and other congenital abnormalities.
  • 22. Uses 1. As contraceptive 2. Hormone replacement therapy (HRT) 3. Dysfunctional uterine bleeding 4. Endometriosis 5. Premenstrual syndrome/tension 6. Threatened/habitual abortion 7. Endometrial carcinoma
  • 25. Actions  Inhibin designated inhibin-A and Inhibin-B.  It secreted by the gonads by Sertoli cells in the male and the granulosa cells in the female.  It inhibit the production of follicle-stimulating hormone (FSH) by the pituitary gland .  The inhibins are also involved in the control of the production of gametes and embryonic and fetal development .
  • 26. Side Effects  Down syndrome  Inhibin-A is included in the maternal serum screening tests for Down syndrome in the second trimester of pregnancy .
  • 27. Relaxin  In women, relaxin is secreted into the circulation by the corpus luteum in the ovary and during pregnancy it released from the placenta.  In men, relaxin is secreted from the prostate gland and can be detected in the semen, but is not generally found in the blood circulation.  The role of relaxin in men is less clear. However, there is evidence that it may increase the movement of sperm cells in the semen.
  • 29. Actions  Relaxin levels in the circulation rise after ovulation and relax the wall of the uterus by inhibiting contractions, and it also prepares the lining of the uterus for pregnancy.  In early pregnancy relaxin inhibits contractions in the wall of the uterus, to prevent premature childbirth.  In first trimester of pregnancy relaxin promote implantation of the developing fetus into the wall of the uterus and the growth of the placenta.  Relaxin decreases tissue fibrosis in the kidney, heart, lungs and liver, and promotes wound healing.