Sex hormones

HORMONES

1. ADITYA INSTITUTE OF PHARMACY DEPARTMENT OF PHARMACOLOGY ADVANCED PHARMACOLOGY II PRESENTATION ON “ SEX HORMONES” SUBMITTED TO: DR.N VENKATESAN PREPARED BY: RAJESH YADAV

2. INTRODUCTION Sex Hormones or Sex Steroids are group of steroids biosynthesized in testes, ovaries, adrenals and placenta during pregnancy. It is controlled by anterior lobe of pituitary gland.

3. TYPES The two main classes of sex steroids are androgens and estrogens, of which the most important human derivatives are  testosterone  and  estradiol . Other contexts will include  progestogens  as a third class of sex steroids, distinct from androgens and estrogens.   Progesterone  is the most important and only naturally occurring human progestogen . In general, androgens are considered "male sex hormones", since they have masculinizing effects. While estrogens and progestogens are considered "female sex hormone” Although all types are present in each sex, albeit at different levels.

4. 1. Androgens – Male sex hormone Testes produce mainly one androgen namely testosterone. It is produced more in males; however, females produce this hormone in lower amount. It promotes male sex characteristics-androgenic activity. It promotes muscle building activity- anabolic activity.

5. ANDROSTERONE DEHYDRO EPIANDROSTERONE TESTOSTERONE

6. Testosterone is the main natural androgen. It is synthesised mainly by the interstitial cells of the testes and in smaller amounts by the ovaries and adrenal cortex. In adult males, its secretion iscontrolled by hormonal signals from hypothalamus, by the way of pituitary gland secretion of FSH and LH.

7. 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

8. Natural Androgens: From Testes: Testosterone (5-12 mg daily) Dihydrotestosterone (more active) by 5 α- reductase From Adrenal cortex: (weak androgens) Dehydroepiandrosterone Androstenedione Androsterone – metabolite of testosterone Synthetic Androgens: Methyltestosterone , Fluoxymesterone Propionate Mesterolone

9. BIOLOGICAL EFFECT OF TESTOSTERONE 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

10. TESTOSTERONE – ANABOLIC EFEECTS 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

11. PHARMACOKINETICS 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 Testosterone is ineffective orally (inactivated by liver), and is usually given as i.m . injections of testosterone esters

12. THERAPEUTIC USE OF ANDROGEN 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 If untreated, does not shorten life expectancy, but is associated with significant morbidity 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

13. 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 impotence ͞

14. ADVERSE EFFECT 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

15. ANABOLIC STEROIDS 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

16. ANTIANDROGENS Danazol Cyproterone acetate Flutamide Finasteride attenuat

17. 2. ESTROGEN – female sex hormone It can induce estrous cycle in spayed animals. It is primary female sex hormone. It is maily synthesised by the ovary and placenta and in small amount in testes and adrenal cortex. 3 main endogeneous estrogens in humans are estradiol , estrone and estriol . Estradiol is the main estrogen secreted by ovary.

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