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MOHD3 Exam 1 > 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)AntagonistAntagonist

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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 antagonistUsed 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 useBad 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

ProgestinsEstrogensProgesterone receptor modulator (PRM)

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13
Q

Suppression of hypothalamic-pituitary-gonadal axis

A

ProgestinsEstrogens

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14
Q

Replacement therapy

A

ProgestinsEstrogensSelective estrogen receptor modulator (SERM)

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15
Q

Ovulation inductions

A

Estrogen antagonistsAromatase 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

NorethindroneNorgestrel

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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

NorethidroneNorgestrel 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 egg2. 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 ovulation2. 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 dosesOnly 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

A

Agonist

44
Q

Agonist or antagonist in breast?Tamoxifen

A

Antagonist

45
Q

Agonist or antagonist in CV system?Tamoxifen

A

Agonist

46
Q

Agonist or antagonist in endometrium?Tamoxifen

A

Agonist

47
Q

Agonist or antagonist in vaginal epithelium?Tamoxifen

A

Agonist

48
Q

Agonist or antagonist in bone?Raloxifene

A

Agonist

49
Q

Agonist or antagonist in breast?Raloxifene

A

Antagonist

50
Q

Agonist or antagonist in CV system?Raloxifene

A

Agonist

51
Q

Agonist or antagonist in endometrium?Raloxifene

A

Neutral

52
Q

Agonist or antagonist in vaginal epithelium?Raloxifene

A

Neutral

53
Q

Agonist or antagonist in bone?Ospemifene

A

Agonist

54
Q

Agonist or antagonist in breast?Ospemifene

A

Antagonist

55
Q

Agonist or antagonist in CV system?Ospemifene

A

Agonist

56
Q

Agonist or antagonist in endometrium?Ospemifene

A

Neutral

57
Q

Agonist or antagonist in vaginal epithelium?Ospemifene

A

Agonist

58
Q

Agonist or antagonist in bone?Bazedoxifene

A

Agonist

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

A

Agonist

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, osteoporosisBreast: 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

BazedoxifeneAgonisticAntagonistic

68
Q

____: inhibit conversion of androgens to estrogens.Used for: (2)

A

Aromatase inhibitors1. Treatment of breast cancer in postmenopausal women2. Induce ovulation

69
Q

Steroidal aromatase inhibitor

A

Exemestane

70
Q

Non-steroidal aromatase inhibitor

A

Anastrozole

71
Q

____: progesterone receptor antagonistUsed 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

Dihydrotestosterone5-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. transdermally2. 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:FinasterideDutasteride

79
Q

Androgen receptor antagonists (3)

A

Antiandrogens:FlutamideBicalutamideNilutamide

80
Q

Inhibitors of steroid synthesis (2)

A

Antiandrogens:KetoconazoleSpironolactone

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

IncreasesGonadotropinPituitary

88
Q

____: stimulate gonadotropin secretionUsed to treat:Administered in ____fashion

A

Synthetic GnRH: gonadorelinTreats: delayed puberty in boys and girls, anovulatory disorders in womenPulsatile

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 - injectableAct 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 lifeLH (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

MOHD3 Exam 1 (2 decks)

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