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Undeleted > Pharmacology Gonadal Steroids/Reproductive Hormones > Flashcards

Pharmacology Gonadal Steroids/Reproductive Hormones Flashcards

1
Q

Progesterone A is mostly a transcripitional (activator/repressor)

A

activator

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2
Q

Progesterone B is mostly a transcripitional (activator/repressor)

A

repressor

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3
Q

Cross reacts with other steroid receptors more than natural progesterone

A

Norethindrone

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4
Q

Used in combination type contraceptives

A 
Norethindorne 
Ethinyl estrodiol (most common)
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5
Q

_____: progestin with enhanced activity as minoeralocorticoid (agonist/antagonist) and androgen (agonist/antagonist)

A

Drospirenone (oral)
Antagonist
Antagonist

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6
Q

____: selective progesterone receptor modulator (PRM)

Used for: ___

A

Ulipristal (oral)
Can be agonist or antagonist, depending on tissue
Post sex contraceptive

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7
Q

____: Progesterone antagonist

Used for abortions

A

Minfepristone (oral)

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8
Q

Estrone sulfate (oral) used in ___

A

hormone replacement therapy

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9
Q

1st non-steroidal estrogens
No longer in use
Bad side effects of offspring and mothers

A

Diethylstilbestrol (DES)

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10
Q

Environmental contaminant with estrogen-like effects

A

Bisphenol A (BPA)

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11
Q

Tamoxifen (oral)

A

Selective estrogen receptor modulator (SERM)

Agonist or antagonist depending on tissue

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12
Q

Contraception

A

Progestins
Estrogens
Progesterone receptor modulator (PRM)

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13
Q

Suppression of hypothalamic-pituitary-gonadal axis

A

Progestins

Estrogens

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14
Q

Replacement therapy

A

Progestins
Estrogens
Selective estrogen receptor modulator (SERM)

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15
Q

Ovulation inductions

A

Estrogen antagonists

Aromatase inhibitors

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16
Q

Breast cancer therapy

A

Selective estrogen receptor modulator (SERM)

Aromatase inhibitors

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17
Q

Abortion

A

Progesterone antagonists

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18
Q

Continuous administration of progestin as contraceptive agents
Oral (daily) (2)

A

Norethindrone

Norgestrel

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19
Q

IM injections (every 3 months) of progestins as contraceptive agents

A

Medroxyprogesterone acetate

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20
Q

Subcutaneous implants (every 3 years) of progestins as contraceptive agents

A

Etongestrel

Most effective

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21
Q

IUDs (every 1-5 years) of progestins as contraceptive agents

A

Norethidrone
Norgestrel

Most effective

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22
Q

Mechanisms of action of progestins (2)

A
  1. Decrease amount and increase viscosity of cervical mucus –> Prevent fertilization b/c sperm can’t reach egg
  2. Inhibit gonadotropin secretion –> Prevent ovulation
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23
Q

Oral preparation of progestins + estrogens as contraceptive agents contain:

A 
Norethidrone or drospirenone (progestin)
Ethinyl estradiol (estrogen)
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24
Q

Mechanisms of action of progestins + estrogens (2)

A
  1. Inhibit hypothalamus and pituitary –> prevent ovulation
  2. Progestins: Decrease amount and increase viscosity of cervical mucus –> Prevent fertilization b/c sperm can’t reach egg
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25
Q

Efficacy of combination-type contraceptives is reduced by: (2)

A
  1. Rifampin family of antibiotics

2. Anticonvulsants

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26
Q

Postcoital contraceptives contain:

A

2-4x the amount of progestins

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27
Q

Mechanism of action of postcoital contraceptives (non prescription)

A

Inhibitory effect of progesterone on gonadotropin secretion but using high doses
Only if ovulation has not occurred prior to unprotected intercourse, must be taken before LH surge

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28
Q

Postcoital contraceptive more effective than norgestrel and maintains efficacy for longer times, 5 days after unprotected intercourse

A

ELLA: selective progesterone receptor modulator, PRM (ulipristal)

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29
Q

Mechanism of action of postcoital contraceptive (prescription)

A
  1. Antagonist of progesterone receptor in granulosa cells: progesterone action on granulosa cell progesterone receptor is essential for follicular rupture (ovulation)
  2. Agonist of progesterone receptor in hypothalamus and pituitary –> delays LH surge by mimicking inhibitory actions of progesterone on gonadotropin secretion
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30
Q

____ used to suppress hypothalamic-pituitary-ovarian axis in treatment of dysmenorrhea and endometriosis

A

Progestins

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31
Q

____ used as replacement therapy in ovarian dysfunction

A

Progestin/estrogen combinations

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32
Q

____ used as replacement therapy for treatment of postmenopausal symptoms and postmenopausal osteoporosis

A

Progestin/estrogen combinations

Lowest effective dose and shortest duration possible

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33
Q

Agonist or antagonist in bone?

Estradiol

A

Agonist

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34
Q

Agonist or antagonist in breast?

Estradiol

A

Agonist

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35
Q

Agonist or antagonist in CV system?

Estradiol

A

Agonist

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36
Q

Agonist or antagonist in endometrium?

Estradiol

A

Agonist

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37
Q

Agonist or antagonist in vaginal epithelium?

Estradiol

A

Agonist

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38
Q

Agonist or antagonist in bone?

Clomiphene/Fulvestrant

A

Antagonist

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39
Q

Agonist or antagonist in breast?

Clomiphene/Fulvestrant

A

Antagonist

40
Q

Agonist or antagonist in CV system?

Clomiphene/Fulvestrant

A

Antagonist

41
Q

Agonist or antagonist in endometrium?

Clomiphene/Fulvestrant

A

Antagonist

42
Q

Agonist or antagonist in vaginal epithelium?

Clomiphene/Fulvestrant

A

Antagonist

43
Q

Agonist or antagonist in bone?

Tamoxifen

44
Q

Agonist or antagonist in breast?

Tamoxifen

A

Antagonist

45
Q

Agonist or antagonist in CV system?

Tamoxifen

46
Q

Agonist or antagonist in endometrium?

Tamoxifen

47
Q

Agonist or antagonist in vaginal epithelium?

Tamoxifen

48
Q

Agonist or antagonist in bone?

Raloxifene

49
Q

Agonist or antagonist in breast?

Raloxifene

A

Antagonist

50
Q

Agonist or antagonist in CV system?

Raloxifene

51
Q

Agonist or antagonist in endometrium?

Raloxifene

52
Q

Agonist or antagonist in vaginal epithelium?

Raloxifene

53
Q

Agonist or antagonist in bone?

Ospemifene

54
Q

Agonist or antagonist in breast?

Ospemifene

A

Antagonist

55
Q

Agonist or antagonist in CV system?

Ospemifene

56
Q

Agonist or antagonist in endometrium?

Ospemifene

57
Q

Agonist or antagonist in vaginal epithelium?

Ospemifene

58
Q

Agonist or antagonist in bone?

Bazedoxifene

59
Q

Agonist or antagonist in breast?

Bazedoxifene

A

Antagonist

60
Q

Agonist or antagonist in endometrium?

Bazedoxifene

A

Antagonist

61
Q

Agonist or antagonist in vaginal epithelium?

Bazedoxifene

62
Q

Clomiphene is used to ____.

It is a ____.

A

Induced ovulation

Estrogen receptor antagonist

63
Q

When clomiphene is given in early stages of follicular phase of menstrual cycle, _____

A

prevent the early inhibitory effects of estrogen on gonadotropin secretion –> enhance stimulatory effect of endogenous estrogens on gonadotropin secretion during periovulatory period

64
Q

Raloxifene is a ____.
Used as estrogen agonist in ____
Antagonist in ____

A

SERM
Bone: postmenopausal symptoms, osteoporosis
Breast: estrogen dependent breast cancer

65
Q

____ has the advantage as a SERM by not being an agonist in endometrium. Does not stimulate endometrial proliferation.

A

Raloxifene

66
Q

____: Approved for treatment of vaginal atrophy in postmenopausal women.
Agonistic effects on vaginal epithelium.

A

Ospemifene

67
Q

____: Approved for treatment of postmonopausal symptoms

(Agonistic/antagonistic) effects on bone and (agonistic/antagonistic) effect on breast and endometrium

A

Bazedoxifene
Agonistic
Antagonistic

68
Q

____: inhibit conversion of androgens to estrogens.

Used for: (2)

A

Aromatase inhibitors

  1. Treatment of breast cancer in postmenopausal women
  2. Induce ovulation
69
Q

Steroidal aromatase inhibitor

A

Exemestane

70
Q

Non-steroidal aromatase inhibitor

A

Anastrozole

71
Q

____: progesterone receptor antagonist

Used for: (3)

A

RU486, mifepristone

  1. Abortions (followed by oral prostaglandin agonist to induce uterine contractions)
  2. Postcoital contraception: antagonizes progesterone actions everywhere, including endometrium
  3. Glucocorticoid antagonist: treatment of Cushing’s and type 2 diabetes
72
Q

Testosterone is metabolize to ____ by ____

A

Dihydrotestosterone

5-alpha-reductase

73
Q

Testosterone analogs (2) that are modified at C17. Can be taken orally.

A
  1. methyltestosterone (-OH)

2. danazole (C triple bond)

74
Q

Testosterone esters administered ____

A

intramuscularly

75
Q

Testosterone administered ____ (2)

A
  1. transdermally

2. buccal tablets

76
Q

____ effective when given orally but have more side effects, especially hepatic toxicity.

A

17 alpha-alkylated androgens (Danazol)

77
Q

Used to treat syndromes of androgen excess or androgen-dependent disorders

A

Antiandrogens

78
Q

5-alpha-reductase inhibitors (2)

A

Antiandrogens:
Finasteride
Dutasteride

79
Q

Androgen receptor antagonists (3)

A

Antiandrogens:
Flutamide
Bicalutamide
Nilutamide

80
Q

Inhibitors of steroid synthesis (2)

A

Antiandrogens:
Ketoconazole
Spironolactone

81
Q

____ used to treat male-pattern baldness

A

Finasteride

82
Q

____ inhibits testicular, adrenal and ovarian steroidogenesis

A

Ketoconazole

83
Q

____ inhibits 17-alpha hydroxylase, androgen receptor, mineralocorticoid receptor antagonist

A

Spironolactone

84
Q

Side effect of antiandrogens

A

Gynecomastia

85
Q

Side effect of 5-alpha reductase inhibitors

A

Persistent sexual dysfunction

86
Q

Male contraceptive made of:

A

Testosterone and nestorone (progestin) transdermally

87
Q

Pulsatile GNRH (increases/decreases) _____ secretion from _____.

A

Increases
Gonadotropin
Pituitary

88
Q

____: stimulate gonadotropin secretion
Used to treat:
Administered in ____fashion

A

Synthetic GnRH: gonadorelin
Treats: delayed puberty in boys and girls, anovulatory disorders in women
Pulsatile

89
Q

Suppression of gonadotropin secretion used for: (4)

A
  1. treatment of endometriosis and dysmenorrhea
  2. ovulation induction
  3. Precocious puberty
  4. Androgen excess in males
90
Q

Long-acting synthetic GnRH agonist

A

Luprolide - injectable

Act like suppression of gonadotropin secretion due to desensitization

91
Q

GnRH antagonist

A

cetrorelix - injectable

92
Q

____ IM injection induce follicular growth

A

FSH (GONAL-F)

93
Q

____ IM injection induce ovulation

A

CG (PREGNYL) - longer half life

LH (LUVERIS)

94
Q

1st drug used to treat female infertility

A

Long acting GnRH agonist or GnRH antagonist to prevent endogenous gonadotropin secretion

95
Q

2nd drug used to treat female infertility

A

FSH to induce follicular growth

96
Q

3rd drug used to treat female infertility

A

LH or hCG to induce ovulation when follicular growth is deemed appropriate

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