Circulatory Shock, types and stages, compensatory mechanisms
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Pharmacology of sex hormons
1. Slide ( 1 / 48 )
Dalia K. Zaafar
Lecturer of Pharmacology
2. Slide ( 2 / 48 )
Female sex hormones
⢠In females, the ovaries and adrenal glands are
the main producers of sex hormones.
⢠Female sex hormones include estrogen,
progesterone, and small quantities of
testosterone.
Sex hormones
3. Slide ( 3 / 48 )
Regulation of menstrual cycle
Sex hormones
4. Slide ( 4 / 48 )
Pharmacological action of Estrogens
⢠Required for normal sexual
maturation & growth of female
⢠Stimulate development of vagina,
uterus & uterine tubes as well as
secondary sex characteristics
⢠Stimulate stromal development &
ductal growth in breast
⢠Responsible for accelerated growth
phase
Estrogens
5. Slide ( 5 / 48 )
Pharmacological action of Estrogens
⢠Epiphysial closure of long bones at
puberty
⢠Distribution of body fat alteration to
produce typical female body shape
⢠â rate of resorption of bone by
antagonizing effects of parathyroid
hormone
⢠stimulate adipose tissue production
Estrogens
6. Slide ( 6 / 48 )
Pharmacological action of Estrogens
⢠â in high density lipoproteins (HDL)
â in low-density lipoproteins (LDL)
⢠â in total plasma cholesterol levels
⢠Plasma triglyceride levels are â
⢠â Platelet adhesiveness
Estrogens
8. Slide ( 8 / 48 )
Estrogen Receptors
⢠There are two types of Estrogen
receptors which are tissue specific
ERι and ERβ
⢠ERι is found endometrium, breast,
hypothalamus and blood vessels
⢠ERβ is found in prostate gland in,
ovaries, brain and heart cells
Estrogens
9. Slide ( 9 / 48 )
I-Selective Estrogen Receptor Modulators
(SERMs)
⢠They are drugs with tissue selective
actions
⢠Estrogenic action in some tissue and
non estrogenic action in some other
tissue
⢠mixed agonists/antagonists
⢠Examples: Clomiphene, Tamoxifen
and Raloxifene
Anti-estrogens
11. Slide ( 11 / 48 )
Clomiphene
⢠Binds to both ERι & ERà & acts as a
pure estrogen antagonist in all
human tissues
⢠Induces Gn secretion in women by
blocking estrogenic feedback
inhibition of pituitary gland
⢠Consequently, ovaries enlarge &
ovulation occurs
⢠Used in ttt of infertility due to
ovulation failure
Anti-estrogens
12. Slide ( 12 / 48 )
Tamoxifen
⢠Binds to both ERι & ERβ
⢠acts as an estrogen agonist on bone
and lipid metabolism
⢠Act as a partial agonist on
endometrium
⢠Act as an antagonist on breast cells
and so can be used in treatment of
advanced breast cancer in
postmenopausal patients
Anti-estrogens
14. Slide ( 14 / 48 )
Raloxifene
⢠Binds to both ERι & ERβ
⢠acts as a estrogen agonist in bone
and lipid metabolism
⢠Antagonist on endometrium and
breast
⢠Used in post menopausal
osteoporosis
Anti-estrogens
15. Slide ( 15 / 48 )
II- Aromatase Inhibitors
⢠Anastrozole
⢠Selective inhibitor of aromatase
enzyme
⢠Decrease estrogen synthesis
⢠Used in treatment of breast cancer
in post menopausal patients
resistant to tamoxifen
Anti-estrogens
16. Slide ( 16 / 48 )
Progesterone
⢠A natural steroidal hormone
⢠Precursor to estrogens, androgens &
adrenocortical steroids
⢠Secreted by the corpus luteum and
the placenta
Progesterone
17. Slide ( 17 / 48 )
Progesterone
⢠Rapidly absorbed following
administration by any route
⢠Half-life in plasma 5 minutes
⢠Completely metabolized by liver
ineffective when administered orally
⢠High-dose oral micronized
progesterone preparations have
been developed that provide
adequate effect
Progesterone
18. Slide ( 18 / 48 )
Synthetic progestin
⢠A number of synthetic progestin
with high oral activity has been
produced.
norethisterone, levonorgestrel,
norgestrel, desogestrel
Progesterone
20. Slide ( 20 / 48 )
Anti-progestin (Mifepristone)
⢠binds strongly to progesterone
receptor & inhibits activity of
progesterone
⢠Major use terminate early
pregnancies
⢠used in treatment of endometriosis,
breast cancer & other neoplasms
that contain glucocorticoid or
progesterone receptors
Progesterone
21. Slide ( 21 / 48 )
Hormonal Contraceptives
⢠Hormonal preparations used for
reversible suppression of fertility
receptor & inhibits activity of
estrogen and progesterone
⢠They can be used in improvement of
menstrual cycle regularity, decrease
risk of endometriosis and
management of perimenopause
Contraceptives
22. Slide ( 22 / 48 )
Oral contraceptive pills (Combined pills)
⢠Monophasic pills
Each tablet contain a fixed
concentration of both estrogen and
progestin
⢠Biphasic pills
Each tablet contain a fixed amount of
estrogen and but the amount of
progestin increases in the second half
of the cycle
Contraceptives
23. Slide ( 23 / 48 )
Oral contraceptive pills (Combined pills)
⢠Triphasic pills
Introduced to permit reduction in
total steroid dose without
compromising efficacy
⢠mimic normal hormonal pattern in a
menstrual cycle
⢠Estrogen dose is constant (or varied
slightly) while amount of progestin
is low in first phase & is
progressively higher in second &
third phases
Contraceptives
24. Slide ( 24 / 48 )
Oral contraceptive pills (Combined pills)
⢠Combined pills are taken for 21
consecutive days followed by 7 pill
free days causing a withdrawal
bleed
Contraceptives
25. Slide ( 25 / 48 )
Oral contraceptive pills (Combined pills)
⢠MOA: Estrogen inhibits secretion of
FSH by -ve feedbackâŚâŚ. Suppress
the development of ovarian follicle
⢠Progestin inhibits secretion of LHâŚâŚ
Prevent ovulation
⢠Both estrogen and progestin alter
the endometrium in a way to
discourage implantation
Contraceptives
26. Slide ( 26 / 48 )
Oral contraceptive pills (Combined pills)
⢠Common adverse effects
⢠Weight gain (due to fluid retention
or anabolic effect)
⢠Nausea, depression, dizziness and
irritability
⢠Acne or increased pigmentation
⢠Thromboembolism and
hypertension
Contraceptives
27. Slide ( 27 / 48 )
Oral contraceptive pills (Combined pills)
⢠Contraindications
⢠Thromboembolic& cerebrovascular
disease
⢠Moderate-to-severe hypertension
and hyperlipidemia
⢠Active liver disease
⢠Suspected malignancy of genitals/
breast
⢠Impending major surgeryâto avoid
excess risk of postoperative
thromboembolism
Contraceptives
28. Slide ( 28 / 48 )
Oral contraceptive pills (progestin only
pills)
⢠Progestins used: levonorgestrel,
norethisterone.
⢠Taken daily without interruption
⢠Less reliable than combined pills
⢠Used when estrogen is
contraindicated
Contraceptives
29. Slide ( 29 / 48 )
Pharmacokinetics
⢠Ora contraceptives are metabolized
by hepatic cytochrome p450 system
⢠So any concomitant use of enzyme
inducers may lead to contraceptive
failure
⢠Examples of these drugs:
Carbamazepine, phenytoin,
Griseofulvin and rifampicin
Contraceptives
30. Slide ( 30 / 48 )
Injectable contraceptives
⢠Depot medroxyprogesterone
acetate (DMPA) 150 mg at 3-month
intervals
⢠Norethindrone (Norethisterone)
enanthate (NEE) 200 mg at 2-month
intervals
⢠Highly effective
⢠Given i.m as oily solution
Contraceptives
31. Slide ( 31 / 48 )
Injectable contraceptives
⢠Major limitations
⢠Menstrual irregularities, excessive
bleeding or amenorrhea are very
common
⢠Return of fertility may take 6â30
months after discontinuation
⢠May cause permanent sterility
Contraceptives
32. Slide ( 32 / 48 )
Testosterone
⢠It is the male sex hormone which is
responsible of the normal
development in males at puberty
and to maintain fertility and libido
⢠Produced by testes, adrenal gland
and ovary
Androgens
33. Slide ( 33 / 48 )
Testosterone
⢠Pharmacological action
⢠Skeletal muscle growth stimulation
⢠Acceleration of bone epiphysis
closure
⢠Stimulation of renal erythropoietin
Androgens
35. Slide ( 35 / 48 )
Testosterone
⢠Pharmacokinetics
⢠Due to extensive hepatic
metabolism it is taken transdermally
or i.m.
⢠Methyltestosterone is resistant to
hepatic metabolism so can be taken
orally
Androgens
36. Slide ( 36 / 48 )
Danazol
⢠A synthetic steroid with
antigonadotrophic and anti-
estrogenic activities and some
androgenic properties
⢠used in the treatment of
endometriosis and some benign
breast disorders
⢠Voice changes, hirsutism and acne
are the main side effects
Androgens
37. Slide ( 37 / 48 )
Types of anti-androgens
⢠1- Androgen receptor antagonist
⢠Cyproterone acetate: active orally,
with increased risk of liver toxicity
and thromboembolic disease
Anti-androgens
38. Slide ( 38 / 48 )
Types of anti-androgens
⢠2- GnRH agonist
⢠GnRH agonists initially increase FSh
and LH secretion âFlare effectâ.
After 2 weeks of administration a
profound hypogonadal effect is
achieved through receptor down
regulation
Anti-androgens
39. Slide ( 39 / 48 )
Types of anti-androgens
⢠2- GnRH agonist
A- Goserelin: used for breast cancer
B- Leuprolide: used for breast and
prostate cancer
C- Buserelin: used for prostate cancer
and male baldness
Anti-androgens
40. Slide ( 40 / 48 )
Types of anti-androgens
⢠3- Androgen synthesis inhibitor
A- Finasteride
⢠Used for hirsutism, male pattern
baldness and benign prostatic
hyperplasia
⢠Taken orally
⢠Inhibit the 5-ι reductase II enzyme
So inhibit the conversion of
testosterone into DHT
Anti-androgens
41. Slide ( 41 / 48 )
Types of anti-androgens
⢠3- Androgen synthesis inhibitor
B- Ketoconazole
⢠At high dosages it inhibits the
conversion of cholesterol to
testosterone and glucocorticoids
⢠it can be used as a second-line
treatment for advanced prostate
cancer and in the treatment of
Cushingâs syndrome
Anti-androgens