Assignment: Sex Hormones ( Hormonal Contraceptive, Anti-
estrogen, anti-progesterone, Androgens, and Anti-Androgens).
Name : Hadeel Anwar Izedeen
ID : 202311956
Outlines :
Physiology of the female menstrual cycle
Estrogen & progesterone ( Effects, uses and side effects)
Hormonal Contraceptive
Anti-estrogen and Anti- progesterone
Androgens and Anti- Androgens
Estrogen Effects:
1. Development of primary sex hormones e.g.: External genitalia,
uterus, ovaries, Fallopian tube, and menstrual cycle regulation.
2. Development of secondary sex characteristics e.g.: Fat
distribution, breasts, and pubic hair.
3. Increase coagulation factor
4. Decrease bone reabsorption
5. CNS: libido and moods
`
Uses :
Hormone Replacement Therapy (HRT ) in PMS
Hormonal contraception
Dysfunctional uterine bleeding
Hormonal Replacement Therapy:
Postmenopausal syndrome: loss of ovarian hormones can result in
postmenopausal syndrome in 50% of women.
Symptoms: Vasomotor symptoms ( Hot flushes or flashes ), sleep
disturbance, CVS problems, vaginal dryness, osteoporosis, and
depression. HRT can significantly improve these symptoms.
Women with removed uterus take E2 alone.
Women with intact uterus require E2 combined with Pg to
decrease the risk of endometrial hyperplasia and cancer.
Postmenopausal HRT should not be used to treat osteoporosis.
Progesterone: Half-life 5 minutes,
synthetic form: progestin and progestogens.
Effects :
To maintain the thickened uterine lining during the luteal phase to
prepare it for implantation.
Uses :
1- Combined with estrogen for hormonal contraception,
postmenopausal HRT, and treatment of endometriosis.
2- Alone to delay menstruation for medical purposes.
Adverse effects :
Androgenic effects e.g: acne, hirsutism, and increased skin
pigmentation, especially in dark-skinned women .
Hormonal Contraception
According to the Mechanism of Action
1-Negative feedback inhibition of pituitary
gonadotropins when Estrogen is high.
2- Estrogen and progesterone produce endometrial
changes and interfere with the coordination of the
cervix, uterus, and fallopian tubes.
3-Increased viscosity of cervical mucus impedes
sperm penetration.
Hormonal Contraceptive Types
1-Combined Pills: contain both estrogen and
progesterone. One tablet is taken every day for 21
days followed by a 7-day break to induce withdrawal
bleeding.
Monophasic pills: The pills contain constant
doses of both estrogen and progesterone.
Multiphasic: The pills contain a constant dose of
estrogen with increasing doses of progesterone
to mimic the natural female cycle.
2-Transdermal Patches: Contain estrogen and
progesterone . During the 28-day cycle, one patch is
applied each week for 3 weeks to the abdomen. No
patch is worn during the fourth week, and
withdrawal bleeding occurs.
3-Progestin- Only pills
Progestin-only pills: contain progestin alone and
given once daily for 21 days. They are less
effective than combined pills.
Long-acting injectable progestin: contains
medroxyprogesterone acetate to be injected IM
or SC every 3 months.
Progestin implants: offer contraception for 3
years.
Emergency pills ( postcoital, morning- after ):
one tablet contains 1.5 levonorgestrel and is
administered within 72 hours after unprotected
intercourse.
Adverse Effect :
1. CVS effects :
Hypertension and fluid retention. Because contraceptives
are steroidal. Steroids can make salt and fluid retention.
Thrombotic complications: Estrogen production
Increase formation of clotting factors.
Endothelial cell proliferation, Damage.
Chronic venous stasis, Estrogen slows circulation.
2. CNS effects :
Migraine headache: The hormonal fluctuations caused by
contraceptive pills can dysregulate the blood flow to the brain
causing headaches.
Mood changes and mental depression.
3. GTI effects :
Nausea, vomiting and breast tenderness
Cholestatic jaundice and gallstones. Because estrogen increases
the biliary concentrations of cholesterol, resulting in decreased
cholesterol solubility and stone formation.
4. Endocrinal effects :
Impaired glucose tolerance
Weight gain and edema due to fluid retention.
Menstrual irregularities, e.g.: breakthrough bleeding and
prolonged amenorrhea.
Progesterone induces androgenic effects, e.g.: acne, hirsutism,
and increased skin pigmentation, especially in dark-skinned
women.
5. Cancer:
Estrogen increases the risk of endometrial and breast cancers,
especially in women who have a family history of the disease.
Warning: Estrogen can cause endometrium and breast cancer.
Pharmacology of Anti-Estrogens and Anti- Progesterone
Anti- Estrogen Drugs :
1-Selective Estrogen Receptor Modulators ( SERMs):
Tamoxifen , Raloxifene & Bazedoxifene (agonist and antagonist )
Tamoxifen Raloxifene
Mechanism Works on uterus and bones Work just on
the bone
Uses Adjustive treatment of ER+ Same
breast cancer ( for < 5 y) Postnuptial
following surgical removal of Osteoporosis
cancer
Adverse Hot flushes Hot
Effects VTE flashes
Increase risk of VTE
endometrial cancer
Hot flashes because SERMS works anti-agonist on the
hypothalamus.
VTE because it works as an agonist on the blood
agents .Estrogen
2 types of breast cancer ER+ Surgery , Chemotherapy
and Hormonal treatment .
ER- Surgery and Chemotherapy .
2- Estrogen Receptor Blockers: Pure Blockers
Clomiphene and fulvestrant
Clomiphene Fulvestrant
(Clomate)
Mechanis Works antagonist on the Works on
hypothalamus and hypothalamus,
m
pituitary gland breasts, uterus,
and bones.
Uses To stimulate ovulation Used in ER+ breast
use for female infertility cancer patients
and normal ovary who are resistant
to tamoxifen and
aromatase
inhibitors
Adverse 1-Increased ovarian
effect size, polycystic
ovary.
2-Hot flushes
Anti- Estrogen Drugs
3- Aromatase Inhibitors :
Anastrozole & Letrozole ) Femara)
Used as adjustive treatment of postmenopausal women
with ER+ breast cancer .
Study Showes that it is most effective treatment.
Anti- Progesterone
Mifepristone: It is used for the termination of pregnancy
in the first trimester.
Misoprostol: is given 48 hours after Mifepristone to
further increase myometrial contractions.
Mifepristone damages of endometrium to prevent
pregnancy.
Misoprostol: To induce medical abortions. Just in the
first trimester.
Pharmacology of Androgens & Anti-Androgens
A. Testosterone is the natural form.
B. Synthetic Androgens
1- Methyltestosterone
2- Anabolic Steroids, e.g. : nandrolone
Is testosterone derivative with a higher, anabolic to
androgenic ratio than testosterone.
Make anabolic effects to build body muscles more than
androgenic effects.
Drug Abuse: Athletes use it in a wide range to build body.
Testosterone is the natural androgen. It is synthesized in
the interstitial cells of the tests ( Leydig cells ) under the
influence of LH. It is steroids.
Sources of Testosterone :
1- Testis (95%)
2- Adrenal gland
3- Adipose tissue
Pharmacological effects:
1- Androgenic Actions, e.g.: development of primary
&secondary sex characteristics.
2- Anabolic Actions, e.g. growth of bone and soft tissue
3- Behavioral effects, e.g. aggressiveness and increased
libido.
Therapeutic uses:
1- Replacement therapy in male hypogonadism.
2- Anabolic Steroids are used by IM injection.
Abuse for athletes worldwide as body-building
injections.
Chronic debilitating diseases e.g. AIDS
Chronic refractory anemia (Erythropoietin is now
used instead).
Adverse effects:
1- Suppression of testicular function and sperm production.
2- Methyltestosterone is hepatotoxic.
3- Virilizing effects in women.
Anti-Androgens
1- 5a- Reductase Inhibitors :
Finasteride & Dutasteride
Testosterone 5a- reductase DHT :
Androgenic alopecia 1 mg in a day for 3-4 months
BPH 5 mg in a day for 6 months
Uses of this family reduced BPH. And treat of
Androgenic alopecia for men.
2-Androgen Receptor Blockers :
Flutamide is a potent AR blocker used for the
treatment of prostatic cancer. For several years after
surgery to prevent metastasis.
Cyproterone acetate is a competitive AR blocker and
used for treatment of hirsutism and ovarian cysts in
women and male hypersexuality.
