Estrogens & Androgens Flashcards
All gonadal hormones are synthesized from_________
cholesterol
Natural estrogens include:
– 17β-estradiol
– Estrone
– Estriol
The most potent natural estrogen is_________
17β-estradiol.
__________is the immediate precursor of estradiol
Testosterone
Synthetic estrogens include:Steroidal agents
– Ethinylestradiol
– Mestranol
Nonsteroidal compounds:
– Diethylstilbestrol (DES)
– Dienestrol
Therapeutic uses of Estrogens alone and in combination with progesterone
alone Treatment of menopausal symptoms Contraception in combinations • Primary hypogonadism • Premature menopause or premature ovarian failure
menopausal symptoms:
-vasomotor instability (“hot flashes”
or “hot flushes”) and vaginal atrophy.
-Loss of libido, depression.
High con of estrogen compared to progesterone, this hormonal imbalance can cause the uterus to become ______ which results in__________
thicker, endometrial carcinoma
a__________ is always included
with the estrogen therapy, because the combination reduces the risk of
endometrial carcinoma associated with unopposed estrogen.
progestogen
progesterone have an _____ estrogenic effect
anti
The amount of estrogen used in replacement therapy is________ than the
doses used in oral contraception. Thus, the adverse effects are usually less
pronounced
less
HT (in postmenopausal) should be prescribed at the ______effective dose for the _______
possible time to relieve menopausal symptoms to reduce the risk of
cardiovascular events.
lowest ,shortest
The combination of an estrogen and progestogen provides effective
contraception via the ________________ route
oral, transdermal, or vaginal route
Synthetic estrogen analogs have a _________ action and a_______potency
compared to those of natural estrogens.
prolonged, higher
__________ have a prolonged action and a higher potency
compared to those of_______________.
Synthetic estrogen analogs, natural estrogens
they are stored in adipose tissue, from which they are________
slowly released
Estrogens are stored in adipose tissue, from which they are________
slowly released
Adverse effects of Estrogens
Breast tenderness (common)
Increased the risk of thromboembolic events and MI
Peripheral edema and hypertension
Increased the risk of breast and endometrial cancer
Increased the risk of breast and endometrial cancer is adverse effect of ________
estrogen alone
Agonist in some tissues and antagonist in others is ________
SERM
SERM includes
Tamoxifen, Raloxifene and Clomiphene
Tamoxifen and Raloxifene have __________ effect in breast
Antagonist effect
Tamoxifen and Raloxifene compete ______________in breast tissue
estrogen
__________compete with estrogen for binding to the
estrogen receptor in breast tissue
Tamoxifen and Raloxifene
_________ also acts as an estrogen agonist in bone
Raloxifene
leading to decreased
bone resorption, increased bone density, and decreased vertebral
fractures in __________ drug
Raloxifene
__________Does Not Have estrogen
receptor agonist activity in the endometrium; does not predispose to
endometrial cancer.
Raloxifene
_______ and ________ have agonist activity in uterus,
therefor they are predisposing to endometrial carcinoma
tamoxifen,Estrogen
____________acts as a partial estrogen agonist and interferes with the
negative feedback of estrogens on the hypothalamus.
Clomiphene
leading to stimulation of ovulation in which SERM drug
clomiphene
______________used in the treatment of metastatic breast cancer, or as
adjuvant therapy following mastectomy or radiation for breast cancer.
Tamoxifen
Tamoxifen is used in the treatment of___________or as
adjuvant therapy following _________,or_________
metastatic breast cancer,
mastectomy
radiation for breast cancer.
__________&__________can be used as prophylactic therapy to
reduce the risk of breast cancer in high-risk patients.
tamoxifen and raloxifene
___________is also approved for the prevention and treatment of
osteoporosis in postmenopausal women.
Raloxifene
___________is useful for the treatment of infertility associated with
anovulatory cycles.
Clomiphene
Adverse effect of Tamoxifen:
Hot flashes and nausea.
Endometrial hyperplasia and malignancies due to its estrogenic activity
in the endometrium.
Adverse effect of Raloxifene
Hot flashes and leg cramps.
Increased risk of deep vein thrombosis, pulmonary embolism, and
retinal vein thrombosis
Adverse effect of Clomiphene
Vasomotor flushes, visual disturbances, and ovarian enlargement.
Increased the risk of multiple births (twins or triplets)
Block the receptor and make conformational change ___________ drugs
Danazol , fluvestrant (anti- estrogens)
Fulvestrant is used to treat women with progressive breast cancer after
__________
tamoxifen
___________is used to treat women with progressive breast cancer after Tamoxifen
fluvestrant
A testosterone derivative with antiandrogen and antiestrogenic activities is ________ drug
Danazol
what Danazol can do:
Inhibits several enzymes involved in steroidogenesis, but does not inhibit
aromatase
May bind to estrogen and androgen receptors
It inhibits gonadotropin release in both men and women.
Antiestrogens (Danazol)
• Clinical use:
⮚ Inhibition of ovarian function,
⮚ Treatment of endometriosis
⮚ Treatment of fibrocystic disease of the breast.
Antiestrogens (Danazol) side effect
⮚ Edema ⮚ masculinization (deepening of the voice and decreased breast size) in some women, ⮚ headache, ⮚ hepatocellular disease.
⮚ pregnant women
⮚ patients with hepatic disease.
they contraindication for which drug __________
Danazol
Contraindication of Danazol
⮚ pregnant women
⮚ patients with hepatic disease.
masculinization (deepening of the voice and decreased breast size) in
some women is an adverse effect of __________
Danazol
Progestogens in female is secreted from ___________
corpus luteum, primarily during the second
half of the menstrual cycle, and by the placenta.
In males progestogens secreted _____________
by the testes (anti-estrogenic effects)
in both sex progestogens is secreted from __________
adrenal cortex
Therapeutic uses of progestogens
Contraception (+/- estrogen) Treatment of hormone deficiency Control of dysfunctional uterine bleeding Treatment of dysmenorrhea Management of endometriosis Management of some types of infertility
________are mainly used, more stable to first-
pass metabolism
Synthetic progestogens (Progestins)
Adverse effects Progestogens
- Headache
- Depression
- Weight gain
- Changes in libido
________ may raise serum potassium due to antimineralocorticoid
effects
Drospirenone
Some have prominent androgenic activity and can cause acne and hirsutism in which drugs____________&_________&__________&_______________
(Norethindrone, Norethindrone acetate, Norgestrel, Levonorgestrel)
Less androgenic progestins
(Norgestimate and drospirenone)
_____________is a progesterone antagonist with partial agonist
activity
Mifepristone (RU-486)
Mifepristone (RU-486) uses
administered in early pregnancy to induce abortion
Misoprostol __________
induce
uterine contractions
Mifepristone (RU-486) combined with the _____________to induce
uterine contractions
Misoprostol
major adverse effects of Mifepristone
Significant uterine bleeding
Possibility of an incomplete abortion
The most common estrogen in the combination pills is ______
ethinyl estradiol.
The most common progestins in the combination pills are
norethindrone, norethindrone acetate,
levonorgestrel, desogestrel, norgestimate, and drospirenone.
Most common type of oral contraceptives contain a constant dose of estrogen and
progestin given over 21 to 24 days
Monophasic combination pills
deliver the same amount of estrogen each day,
but the level of progestin is increased about halfway through the cycle
Biphasic combination pills
The amount of estrogen may change as well as the amount of progestin in ___________
Triphasic combination pills
Contain \_\_\_\_\_\_\_\_\_ and\_\_\_\_\_\_\_\_\_\_and are taken every day for 84 days followed by 7 days of inert tablets (Seasonale) or 7 days of low-dose ethinyl estradiol (Seasonique) &Produce four menstrual periods per year
ethinyl estradiol & levonorgestrel
______contains the same hormones taken continuously for 365 days to
suppress menstruation completely
lybrel
lybrel how prevent conception
thickening cervical mucus
speeding ovum transport through the fallopian tubes
making the endometrium less favorable for implantation
Transdermal patch containing ________ and the ____________.
ethinyl estradiol &progestin norelgestromin
Progestin-only pills (mini-pill) usually
norethindrone
May produce irregular menstrual cycles (Breakthrough bleeding is as high as
25%)
Progestin-only pills (mini-pill)
mechanism of progestin-only pills in contraception
atrophic endometrium (which impairs implantation) and viscous cervical mucus
Progestin-only pills (mini-pill)
Used for:
Breast-feeding women (unlike estrogen, progestins do not affect milk
production)
Women intolerant to estrogen
Smokers
When estrogen- containing products are contraindications
Injectable progestin every 3 months
Medroxyprogesterone acetate is administered IM or SC
Injectable progestin side effect
― Weight gain (common)
― Amenorrhea (due to high sustained levels of progestin
― Return to fertility may be delayed for several months after
discontinuation
― Increase risk of osteoporosis and fractures (Not recommended for
more than 2 years)
Progestin implants Effective for approximately 3 years Contain
Etonogestrel
Progestin implants side effect
are irregular menstrual bleeding and headaches
Progestin intrauterine device highly effective method of contraception for 3 to 5 years
depending on the system.
Levonorgestrel-releasing intrauterine system
Progestin intrauterine device suitable for
― Women who desire long-term contraception
― Those who have contraindications to estrogen therapy
IUD is contraindicated in
patients with pelvic inflammatory disease or a
history of ectopic pregnancy.
Postcoital (emergency) contraception
Uses high doses of levonorgestrel (preferred) or high doses of ethinyl
estradiol plus levonorgestrel.
For maximum effectiveness, it should be taken as soon as possible after
unprotected intercourse and preferably within 72 hours.
Postcoital (emergency) contraception
ulipristal is an agonist and antagonist how ?
It depends on the level of progesterone
If progesterone levels is high , work as antagonist
If progesterone levels is low, work as agonist
Rare side effects (most common among women over age 35 and smokes): in oral contraceptives
― Thromboembolism
― thrombophlebitis
― Myocardial infarction
― Stroke
Oral contraceptives are associated with a decreased risk of ___________&_________
cervical and
ovarian cancer
Contraindication of oral contraceptives
• The presence of cerebrovascular and thromboembolic disease
• Estrogen-dependent neoplasms
• Liver disease: associated with cholestasis and development of hepatic
adenoma
• Pregnancy.
• Combination oral contraceptives should not be used in patients over the
age of 35 who are heavy smokers
• Liver enzyme inducer drugs and those affecting enterohepatic recycling
(e.g. Antibiotics) can reduce the effectiveness of contraception!
Testosterone is synthesized by:
- Leydig cells in the testes
- Thecal cells in the ovaries (smaller amounts)
- Adrenal gland in both sexes
Physiological functions of Androgens
1) Normal maturation in the male
2) Sperm production
3) Increase synthesis of muscle proteins and hemoglobin
4) Decrease bone resorption
Therapeutic uses of Androgens
Males with primary hypogonadism
Secondary hypogonadism
treat chronic wasting associated with
human immunodeficiency virus (HIV) or cancer
to increase lean body mass, muscle
strength, and endurance in athletes and body builders
contraindication in using androgens in females
Should not be used by pregnant women because of possible
developmental effects of the female fetus
Excess androgens can cause:in males
- Impotence
- Decreased spermatogenesis
- Gynecomastia
- Stimulate growth of the prostate
- Baldness
Adverse effects of Androgens in children
• Androgens can cause abnormal sexual maturation
• Growth disturbances resulting from premature closing of the epiphyseal
plates, which stunts growth and interrupts development
Adverse effects of Androgens in Athletes
Premature closing of the epiphysis of the long bones.
- Reduction of testicular size
- Hepatic abnormalities
- Increased aggression
- Major mood disorders.
General Adverse effects of Androgens
- Can increase serum LDL and lower serum HDL.
* Fluid retention leading to edema
Anti-androgens
Finasteride and Dutasteride &Flutamide
Finasteride and Dutasteride
inhibit 5α-reductase resulting in decreased
formation of dihydrotestosterone.
These agents are used for the treatment of benign prostatic hyperplasia.
These agents are used for the treatment of benign prostatic hyperplasia.
Finasteride and Dutasteride
is competitive inhibitors of androgens at the target cell. It is
used for the treatment of prostate cancer.
Flutamide
- Which is NOT a sex steroid hormone?
a. Estradiol.
b. Progesterone.
c. Testosterone.
d. Cortisol.
Cortisol.
The effects of estrogen on which organ increase the risk of thromboembolism?
a. Liver.
b. Ovary.
c. Uterus.
d. Kidney.
liver
. Estrogen therapy reduces the occurrence of which condition?
a. Acne.
b. Osteoporosis.
c. Hypertension.
d. Endometrial cancer.
osteoporosis
Which drug is a pure estrogen receptor antagonist?
a. Raloxifene.
b. Tamoxifen.
c. Fulvestrant.
d. Clomiphene.
fluvestrant
the drug used for the treatment of estrogen‐dependent breast cancer
is : a) Tamoxifen d) Mifepristone
b) Raloxifene e) Ergometrine
c) Clomiphene
a)tamoxifen
All of the following statements about oral contraceptives are true, EXCEPT:
a) The “combination pill” contains both estrogen and progestin
b) Ethinyl estradiol and mestranol are commonly used in oral
contraceptives
c) The “minipill” contains progestin alone
d) The “triphasic pill” contains estrogen, progestin, and luteinizing hormine
(LH)
d) The “triphasic pill” contains estrogen, progestin, and luteinizing hormine (LH)
Actions of mifepristone (RU‐486) include:
a) Inhibition of ovulation during the follicular phase by blocking
hypothalamic‐pituitary progesterone receptors, which
suppresses midcycle gonadotropin release
b) During the luteal phase, inhibition of progesterone action on the uterus,
which induces prostaglandin release from the
endometrium
c) Termination of pregnancy by facilitating luteolysis, menstruation,
uterine motility, softening of the cervix, and
detachment of the embryo.
d) All of the above
d) All of the above
Mifepristone (RU‐486) is used as a contraceptive and abortifacient. This
consideration is:
a) True
b) False
a)true
The postcoital contraceptive is : a‐ tamoxifen b‐ ulipristal c‐ Mifepristone d‐ anastrozole e‐ Raloxifen
B
The best drug for postmenopausal osteoporosis is : a‐ Cholecalciferol b‐ Octreotide c‐ Raloxifene d‐ Alendronate e‐ Calcitonin
c‐ Raloxifene
