10-Gonadal Hormones

Gonadal hormones
dr. RUSUL ALI

FEB 2024
Background
Gonadal hormones that produced by the gonads and are
synthesized from the precursor, cholesterol, in a series of
steps, the importance of Sex hormones are:
‫تَصْميم‬
• conception ovulation ‫زيادة االستروجني تسوي‬
• embryonic maturation,
• development of primary and secondary sexual
characteristics at puberty.
• Replacement therapy
ِ‫مَنْع الحَمْل‬
menopause ‫يعوضون النقص مثال في حاله‬
• Contraception. ‫وحده او كومبنشن‬
• Management of menopausal symptoms

• Antagonists are effective in cancer chemotherapy.
Cancer depends on Estrogen
Estrogen( Estradiol)(17β-estradiol)
 Estradiol secreted by the ovary.
menopause ‫هو االستروجني لكن في حالة‬
 Estrone : primary circulating estrogen after menopause,

estrogen ‫يعني‬
has one-third the estrogenic potency of estradiol.

in potency ‫ وكذالك اقل من االستروجني‬pregnancy ‫نلكاه بال‬
 Estriol: is another metabolite of estradiol, less potent

than is estradiol, during pregnancy, because it is the
principal estrogen produced by the placenta.
‫مومهم الرسم‬
Mechanism of action
dimerization
ً‫مهم جدا‬
Therapeutic uses
1. Postmenopausal hormonal threapy:
a. women is menopausal symptoms, such as vasomotor instability ( eg.
hot flashes )and vaginal atrophy.
‫في حالة الرحم موجود‬
b. women who have an intact uterus, give (combination estrogen

endometrial carcinoma ‫وحده بهالحاله نزيد مخاطر‬estrogen ‫إذا انطيناه‬
and progesterone ) reduce risk of endometrial carcinoma associated
with unopposed estrogen. ‫ مالته‬lipid ‫ماستفادينه من‬ ‫االهم مانسوي كانسر حتلو‬
‫ الن اساساً الرحم مشيول فعادي ننطي إستروجني وحده‬carcinoma ‫ماعدها مخاطر حصول هالحاله‬
‫الرحم شايلينه‬
c. Women with hysterectomy: unopposed estrogen therapy is
recommended because progestins may unfavorably alter the
beneficial effects of estrogen on lipid parameters(inc.HDL,dec.LDL)
2. Osteoporosis :Estrogen decreases the resorption of bone, decreases
the frequency of hip fracture in menopausal women
3. Contraception combination or mono therapy‫ك‬
4. Others: stimulate development of secondary sex characteristics in
young women with primary hypogonadism, premature ovarian failure.
Pharmacokinetics
Naturally occurring estrogens:
 absorbed through the gastrointestinal tract, skin, and mucous
membranes.
 Taken orally, estradiol is rapidly metabolized (and partially
inactivated) by the microsomal enzymes of the liver
Synthetic estrogen analogs
 such as :Ethinyl estradiol, Mestranol, Estradiol valerate,
 are well absorbed after oral administration then meta. to fat
soluble compounds
 stored in adipose tissue, from which they are slowly released
 have a prolonged action and a higher potency compared to
those of natural estrogens
Side effects ‫السبب مطلوب‬
Increase breast tissue

Irritating to gastric mucosa vasoconstriction ‫بسبب‬
Fluid retention RAAS ‫بسبب تنشيط‬
‫فيسوي زيادة بال‬
aldosterone
Increase
Hypertension because
coagulation Fluid retention vasoconstriction
factor
Selective estrogen receptor
agonists or antagonists ‫ممكن تشتغل‬ ‫ الي ديشتغل عليه او املستقبالت املوجوده بي‬type of tissue ‫اعتمادا ع‬
modulators
 these are include:
EStrogen analogue ‫كلهن‬
 Tamoxifen, Toremifene, Raloxifene, Clomiphene, and

Ospemifene.
a class of estrogen-related compounds that display selective
agonist or antagonism for estrogen receptors depending on the
tissue type.(endometrium breast ,ovary, bones)
‫جداً جدا مهم اجه العام‬

Clomiphene
interferes with the
negative feedback
Partial
agonist SERM
of estrogens on the
hypothalamus.
‫يبقى األستروجني عالي‬
Stimulation antagonist
ovulation Agonist
agonists ‫يشتغل ع مستقبالت االستروجني الي ببطانة الرحم فيكون ك‬

‫ يعني يزيد االستروجني‬risk of carcinoma ‫فيكون‬
breast as antagonists‫بال‬
tamoxifen, agonist in endometrium estrogen
receptors , predispose to endometrial cancer, Tamoxifen, toremifene,reloxifene
Raloxifene agonsit on bone , decreased bone are compete with estrogen for
resorption, increased bone density, and binding to the estrogen receptor in
intact uterus ‫مايفيد ننطي لل‬
decreased vertebral fractures ,no estrogen breast tissue( effective in breast
receptor agonist activity on endometrium , does cancer especially estrogen
not predispose to endometrial cancer dependent breast cancer
lipid ‫فائدة ع مستوى‬ Breast cancer du to Estrogen
lowers S.cholesterol and LDL ‫فيفيدنه هالعالج يقلل تقدم الكانسو‬
‫يشتغل على مستوى العضم فيقلل مخاطر الكسر فيفيدنه بالنساء الكبار بالعمر‬
receptor ‫ألن حيكعد مكانه ويسد ال‬
:Uses Of selective Estrogen receptors
‫مساعد‬
 metastatic breast cancer, or as adjuvant therapy following
breast ‫شايلني‬
mastectomy or radiation for breast cancer(Tamoxifen)
 prophylactic therapy to reduce the risk of breast cancer in ‫كوقاية‬
high-risk patient(Both tamoxifen and raloxifene)

 prevention and treatment of osteoporosis in postmenopausal
women(Raloxifene)
 treatment of infertility associated with an ovulatory
cycles(Clomiphene) Induction of ovulation
 treatment of dyspareunia related to menopause.

( Ospemifene)
: Side effects Of selective Estrogen receptors

 Hot flashes and nausea
 Endometrial hyperplasia and malignancies have been reported
with Tamoxifen
 Tamoxifen is subject to many drug interactions.
 Deep vein thrombosis, pulmonary embolism, and retinal vein
thrombosis
 Clomiphene increases the risk of multiple births (twins or
triplets).
progestogen
• Progesterone, the natural progestogen, , is produced by both

females and males in response to luteinizing hormone (LH).
Area of secretions of progestogen
• in female from corpus luteum(2nd half of cycle ) and by the

placenta.
• In males (secreted by the testes)
• adrenal cortex in both sexes
Action ‫فقط‬
Mechanisms ‫هي نفسها‬
Mechanism of action: ‫الي باملخطط الفوك‬
‫وضيفه يهيء بيئه جيده لغرس الجنني واذا‬
In females, progesterone ‫فشلت فيقل الدنى مستوى‬
 promotes the development of a secretory endometrium that

can accommodate implantation of a newly forming embryo.
GnRH
 inhibit the production of gonadotropin and, so that it
prevent further ovulation.(this is due to high level of
progesterone in 2nd half of the cycle).
 maintaining the endometrium in a favorable state for the
continuation of the pregnancy and reducing uterine
contractions.(when pregnancy occur)
 When pregnancy does not occur, progesterone from the
corpus luteum stops abruptly lead to menstruation
Therapeutic uses of progestogens
 Hormone deficiency.
 Contraception, in combination with estrogens
Idiopathic bleeding
 Control of dysfunctional uterine bleeding
 Dysmenorrhea.
 Management of endometriosis.
 Infertility
Side effects:
 headache, depression, weight gain, and changes in libido.
 Progestins that are derived from 19-nortestosterone (norethindrone,

Androgen like effects
norethindrone acetate, norgestrel, levonorgestrel) can cause acne and
hirsutism because of their structural similarity to testosterone .
norgestimate and drospirenone, have less androgen effect,
Acne & hirsutism ‫اقل‬
 Hyperkalemia espicially Drospirenone due to anti mineralocorticoid

effects
Antiprogestin
Mifepristone
 progesterone antagonist activity
 When given in early pregnancy it causes abortion due to
interference with the progesterone needed to maintain pregnancy
Abortion ‫هم يسوي‬
 often combined with the prostaglandin analog misoprostol (orally or
intravaginally) lead to uterine contractions
Side effect:
 uterine bleeding.
 abortion.

10-Gonadal Hormones

Uploaded by

Copyright:

Available Formats

10-Gonadal Hormones

Uploaded by

Document Information

Original Title

Copyright

Available Formats

Share this document

Share or Embed Document

Sharing Options

Did you find this document useful?

Is this content inappropriate?

Copyright:

Available Formats

10-Gonadal Hormones

Uploaded by

Copyright:

Available Formats

Gonadal hormones

dr. RUSUL ALI

• Contraception. ‫وحده او كومبنشن‬

• Management of menopausal symptoms

 Estradiol secreted by the ovary.

menopause ‫هو االستروجني لكن في حالة‬

 Estrone : primary circulating estrogen after menopause,

has one-third the estrogenic potency of estradiol.

 Estriol: is another metabolite of estradiol, less potent

b. women who have an intact uterus, give (combination estrogen

Side effects ‫السبب مطلوب‬

Increase breast tissue

 Tamoxifen, Toremifene, Raloxifene, Clomiphene, and

‫جداً جدا مهم اجه العام‬

agonists ‫يشتغل ع مستقبالت االستروجني الي ببطانة الرحم فيكون ك‬

high-risk patient(Both tamoxifen and raloxifene)

 treatment of dyspareunia related to menopause.

: Side effects Of selective Estrogen receptors

• Progesterone, the natural progestogen, , is produced by both

• in female from corpus luteum(2nd half of cycle ) and by the

• In males (secreted by the testes)

• adrenal cortex in both sexes

‫وضيفه يهيء بيئه جيده لغرس الجنني واذا‬

In females, progesterone ‫فشلت فيقل الدنى مستوى‬

 promotes the development of a secretory endometrium that

 Progestins that are derived from 19-nortestosterone (norethindrone,

 Hyperkalemia espicially Drospirenone due to anti mineralocorticoid

You might also like