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Pharma 2:) > Estrogens & Androgens > Flashcards

Estrogens & Androgens Flashcards

1
Q

All gonadal hormones are synthesized from_________

A

cholesterol

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2
Q

Natural estrogens include:

A

– 17β-estradiol
– Estrone
– Estriol

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3
Q

The most potent natural estrogen is_________

A

17β-estradiol.

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4
Q

__________is the immediate precursor of estradiol

A

Testosterone

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5
Q

Synthetic estrogens include:Steroidal agents

A

– Ethinylestradiol

– Mestranol

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6
Q

Nonsteroidal compounds:

A

– Diethylstilbestrol (DES)

– Dienestrol

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7
Q

Therapeutic uses of Estrogens alone and in combination with progesterone

A 
alone  
Treatment of menopausal symptoms
Contraception
in combinations 
• Primary hypogonadism
• Premature menopause or premature ovarian failure
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8
Q

menopausal symptoms:

A

-vasomotor instability (“hot flashes”
or “hot flushes”) and vaginal atrophy.
-Loss of libido, depression.

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9
Q

High con of estrogen compared to progesterone, this hormonal imbalance can cause the uterus to become ______ which results in__________

A

thicker, endometrial carcinoma

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10
Q

a__________ is always included
with the estrogen therapy, because the combination reduces the risk of
endometrial carcinoma associated with unopposed estrogen.

A

progestogen

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11
Q

progesterone have an _____ estrogenic effect

A

anti

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12
Q

The amount of estrogen used in replacement therapy is________ than the
doses used in oral contraception. Thus, the adverse effects are usually less
pronounced

A

less

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13
Q

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.

A

lowest ,shortest

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14
Q

The combination of an estrogen and progestogen provides effective
contraception via the ________________ route

A

oral, transdermal, or vaginal route

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15
Q

Synthetic estrogen analogs have a _________ action and a_______potency
compared to those of natural estrogens.

A

prolonged, higher

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16
Q

__________ have a prolonged action and a higher potency

compared to those of_______________.

A

Synthetic estrogen analogs, natural estrogens

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17
Q

they are stored in adipose tissue, from which they are________

A

slowly released

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17
Q

Estrogens are stored in adipose tissue, from which they are________

A

slowly released

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18
Q

Adverse effects of Estrogens

A

Breast tenderness (common)
Increased the risk of thromboembolic events and MI
Peripheral edema and hypertension
Increased the risk of breast and endometrial cancer

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19
Q

Increased the risk of breast and endometrial cancer is adverse effect of ________

A

estrogen alone

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20
Q

Agonist in some tissues and antagonist in others is ________

A

SERM

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21
Q

SERM includes

A

Tamoxifen, Raloxifene and Clomiphene

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22
Q

Tamoxifen and Raloxifene have __________ effect in breast

A

Antagonist effect

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23
Q

Tamoxifen and Raloxifene compete ______________in breast tissue

A

estrogen

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24
Q

__________compete with estrogen for binding to the

estrogen receptor in breast tissue

A

Tamoxifen and Raloxifene

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25
Q

_________ also acts as an estrogen agonist in bone

A

Raloxifene

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26
Q

leading to decreased
bone resorption, increased bone density, and decreased vertebral
fractures in __________ drug

A

Raloxifene

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27
Q

__________Does Not Have estrogen
receptor agonist activity in the endometrium; does not predispose to
endometrial cancer.

A

Raloxifene

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28
Q

_______ and ________ have agonist activity in uterus,

therefor they are predisposing to endometrial carcinoma

A

tamoxifen,Estrogen

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29
Q

____________acts as a partial estrogen agonist and interferes with the
negative feedback of estrogens on the hypothalamus.

A

Clomiphene

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30
Q

leading to stimulation of ovulation in which SERM drug

A

clomiphene

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31
Q

______________used in the treatment of metastatic breast cancer, or as
adjuvant therapy following mastectomy or radiation for breast cancer.

A

Tamoxifen

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32
Q

Tamoxifen is used in the treatment of___________or as

adjuvant therapy following _________,or_________

A

metastatic breast cancer,
mastectomy
radiation for breast cancer.

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33
Q

__________&__________can be used as prophylactic therapy to

reduce the risk of breast cancer in high-risk patients.

A

tamoxifen and raloxifene

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34
Q

___________is also approved for the prevention and treatment of
osteoporosis in postmenopausal women.

A

Raloxifene

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35
Q

___________is useful for the treatment of infertility associated with
anovulatory cycles.

A

Clomiphene

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36
Q

Adverse effect of Tamoxifen:

A

Hot flashes and nausea.
Endometrial hyperplasia and malignancies due to its estrogenic activity
in the endometrium.

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37
Q

Adverse effect of Raloxifene

A

Hot flashes and leg cramps.
Increased risk of deep vein thrombosis, pulmonary embolism, and
retinal vein thrombosis

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38
Q

Adverse effect of Clomiphene

A

Vasomotor flushes, visual disturbances, and ovarian enlargement.
Increased the risk of multiple births (twins or triplets)

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39
Q

Block the receptor and make conformational change ___________ drugs

A

Danazol , fluvestrant (anti- estrogens)

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40
Q

Fulvestrant is used to treat women with progressive breast cancer after
__________

A

tamoxifen

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41
Q

___________is used to treat women with progressive breast cancer after Tamoxifen

A

fluvestrant

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42
Q

A testosterone derivative with antiandrogen and antiestrogenic activities is ________ drug

A

Danazol

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43
Q

what Danazol can do:

A

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.

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44
Q

Antiestrogens (Danazol)

• Clinical use:

A

⮚ Inhibition of ovarian function,
⮚ Treatment of endometriosis
⮚ Treatment of fibrocystic disease of the breast.

45
Q

Antiestrogens (Danazol) side effect

A 
⮚ Edema
⮚ masculinization (deepening of the voice and decreased breast size) in
some women,
⮚ headache,
⮚ hepatocellular disease.
46
Q

⮚ pregnant women
⮚ patients with hepatic disease.
they contraindication for which drug __________

A

Danazol

47
Q

Contraindication of Danazol

A

⮚ pregnant women

⮚ patients with hepatic disease.

48
Q

masculinization (deepening of the voice and decreased breast size) in
some women is an adverse effect of __________

A

Danazol

49
Q

Progestogens in female is secreted from ___________

A

corpus luteum, primarily during the second

half of the menstrual cycle, and by the placenta.

50
Q

In males progestogens secreted _____________

A

by the testes (anti-estrogenic effects)

51
Q

in both sex progestogens is secreted from __________

A

adrenal cortex

52
Q

Therapeutic uses of progestogens

A 
Contraception (+/- estrogen)
Treatment of hormone deficiency
Control of dysfunctional uterine bleeding
Treatment of dysmenorrhea
Management of endometriosis
Management of some types of infertility
53
Q

________are mainly used, more stable to first-

pass metabolism

A

Synthetic progestogens (Progestins)

54
Q

Adverse effects Progestogens

A
  • Headache
  • Depression
  • Weight gain
  • Changes in libido
55
Q

________ may raise serum potassium due to antimineralocorticoid
effects

A

Drospirenone

56
Q

Some have prominent androgenic activity and can cause acne and hirsutism in which drugs____________&_________&__________&_______________

A

(Norethindrone, Norethindrone acetate, Norgestrel, Levonorgestrel)

57
Q

Less androgenic progestins

A

(Norgestimate and drospirenone)

58
Q

_____________is a progesterone antagonist with partial agonist
activity

A

Mifepristone (RU-486)

59
Q

Mifepristone (RU-486) uses

A

administered in early pregnancy to induce abortion

60
Q

Misoprostol __________

A

induce

uterine contractions

61
Q

Mifepristone (RU-486) combined with the _____________to induce
uterine contractions

A

Misoprostol

62
Q

major adverse effects of Mifepristone

A

Significant uterine bleeding

Possibility of an incomplete abortion

63
Q

The most common estrogen in the combination pills is ______

A

ethinyl estradiol.

64
Q

The most common progestins in the combination pills are

A

norethindrone, norethindrone acetate,

levonorgestrel, desogestrel, norgestimate, and drospirenone.

65
Q

Most common type of oral contraceptives contain a constant dose of estrogen and
progestin given over 21 to 24 days

A

Monophasic combination pills

66
Q

deliver the same amount of estrogen each day,

but the level of progestin is increased about halfway through the cycle

A

Biphasic combination pills

67
Q

The amount of estrogen may change as well as the amount of progestin in ___________

A

Triphasic combination pills

68
Q 
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
A

ethinyl estradiol & levonorgestrel

69
Q

______contains the same hormones taken continuously for 365 days to
suppress menstruation completely

A

lybrel

70
Q

lybrel how prevent conception

A

thickening cervical mucus
speeding ovum transport through the fallopian tubes
making the endometrium less favorable for implantation

71
Q

Transdermal patch containing ________ and the ____________.

A

ethinyl estradiol &progestin norelgestromin

72
Q

Progestin-only pills (mini-pill) usually

A

norethindrone

73
Q

May produce irregular menstrual cycles (Breakthrough bleeding is as high as
25%)

A

Progestin-only pills (mini-pill)

74
Q

mechanism of progestin-only pills in contraception

A 
atrophic endometrium (which impairs
implantation) and viscous cervical mucus
75
Q

Progestin-only pills (mini-pill)

Used for:

A

Breast-feeding women (unlike estrogen, progestins do not affect milk
production)
Women intolerant to estrogen
Smokers
When estrogen- containing products are contraindications

76
Q

Injectable progestin every 3 months

A

Medroxyprogesterone acetate is administered IM or SC

77
Q

Injectable progestin side effect

A

― 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)

78
Q

Progestin implants Effective for approximately 3 years Contain

A

Etonogestrel

79
Q

Progestin implants side effect

A

are irregular menstrual bleeding and headaches

80
Q

Progestin intrauterine device highly effective method of contraception for 3 to 5 years
depending on the system.

A

Levonorgestrel-releasing intrauterine system

81
Q

Progestin intrauterine device suitable for

A

― Women who desire long-term contraception

― Those who have contraindications to estrogen therapy

82
Q

IUD is contraindicated in

A

patients with pelvic inflammatory disease or a

history of ectopic pregnancy.

83
Q

Postcoital (emergency) contraception

A

Uses high doses of levonorgestrel (preferred) or high doses of ethinyl
estradiol plus levonorgestrel.

84
Q

For maximum effectiveness, it should be taken as soon as possible after
unprotected intercourse and preferably within 72 hours.

A

Postcoital (emergency) contraception

85
Q

ulipristal is an agonist and antagonist how ?

A

It depends on the level of progesterone
If progesterone levels is high , work as antagonist
If progesterone levels is low, work as agonist

86
Q

Rare side effects (most common among women over age 35 and smokes): in oral contraceptives

A

― Thromboembolism
― thrombophlebitis
― Myocardial infarction
― Stroke

87
Q

Oral contraceptives are associated with a decreased risk of ___________&_________

A

cervical and

ovarian cancer

88
Q

Contraindication of oral contraceptives

A

• 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!

89
Q

Testosterone is synthesized by:

A
  • Leydig cells in the testes
  • Thecal cells in the ovaries (smaller amounts)
  • Adrenal gland in both sexes
90
Q

Physiological functions of Androgens

A

1) Normal maturation in the male
2) Sperm production
3) Increase synthesis of muscle proteins and hemoglobin
4) Decrease bone resorption

91
Q

Therapeutic uses of Androgens

A

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

92
Q

contraindication in using androgens in females

A

Should not be used by pregnant women because of possible

developmental effects of the female fetus

93
Q

Excess androgens can cause:in males

A
  • Impotence
  • Decreased spermatogenesis
  • Gynecomastia
  • Stimulate growth of the prostate
  • Baldness
94
Q

Adverse effects of Androgens in children

A

• Androgens can cause abnormal sexual maturation
• Growth disturbances resulting from premature closing of the epiphyseal
plates, which stunts growth and interrupts development

95
Q

Adverse effects of Androgens in Athletes

A

Premature closing of the epiphysis of the long bones.

  • Reduction of testicular size
  • Hepatic abnormalities
  • Increased aggression
  • Major mood disorders.
96
Q

General Adverse effects of Androgens

A
  • Can increase serum LDL and lower serum HDL.

* Fluid retention leading to edema

97
Q

Anti-androgens

A

Finasteride and Dutasteride &Flutamide

98
Q

Finasteride and Dutasteride

A

inhibit 5α-reductase resulting in decreased
formation of dihydrotestosterone.
These agents are used for the treatment of benign prostatic hyperplasia.

99
Q

These agents are used for the treatment of benign prostatic hyperplasia.

A

Finasteride and Dutasteride

100
Q

is competitive inhibitors of androgens at the target cell. It is
used for the treatment of prostate cancer.

A

Flutamide

101
Q
  1. Which is NOT a sex steroid hormone?
    a. Estradiol.
    b. Progesterone.
    c. Testosterone.
    d. Cortisol.
A

Cortisol.

102
Q

The effects of estrogen on which organ increase the risk of thromboembolism?

a. Liver.
b. Ovary.
c. Uterus.
d. Kidney.

A

liver

103
Q

. Estrogen therapy reduces the occurrence of which condition?

a. Acne.
b. Osteoporosis.
c. Hypertension.
d. Endometrial cancer.

A

osteoporosis

104
Q

Which drug is a pure estrogen receptor antagonist?

a. Raloxifene.
b. Tamoxifen.
c. Fulvestrant.
d. Clomiphene.

A

fluvestrant

105
Q

the drug used for the treatment of estrogen‐dependent breast cancer
is : a) Tamoxifen d) Mifepristone
b) Raloxifene e) Ergometrine
c) Clomiphene

A

a)tamoxifen

106
Q

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)

A

d) The “triphasic pill” contains estrogen, progestin, and luteinizing hormine (LH)

107
Q

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

A

d) All of the above

108
Q

Mifepristone (RU‐486) is used as a contraceptive and abortifacient. This
consideration is:
a) True
b) False

A

a)true

109
Q 
The postcoital contraceptive is :
a‐  tamoxifen 
b‐  ulipristal
c‐ Mifepristone 
d‐ anastrozole 
e‐  Raloxifen
A

B

110
Q 
The best drug for postmenopausal osteoporosis is :
a‐ Cholecalciferol 
b‐  Octreotide 
c‐ Raloxifene 
d‐ Alendronate 
e‐ Calcitonin
A

c‐ Raloxifene

Pharma 2:) (3 decks)

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