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Flashcards in deck_3556451 Deck (96):
1

Progesterone A is mostly a transcripitional (activator/repressor)

activator

2

Progesterone B is mostly a transcripitional (activator/repressor)

repressor

3

Cross reacts with other steroid receptors more than natural progesterone

Norethindrone

4

Used in combination type contraceptives

Norethindorne Ethinyl estrodiol (most common)

5

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

Drospirenone (oral)AntagonistAntagonist

6

____: selective progesterone receptor modulator (PRM) Used for: ___

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

7

____: Progesterone antagonistUsed for abortions

Minfepristone (oral)

8

Estrone sulfate (oral) used in ___

hormone replacement therapy

9

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

Diethylstilbestrol (DES)

10

Environmental contaminant with estrogen-like effects

Bisphenol A (BPA)

11

Tamoxifen (oral)

Selective estrogen receptor modulator (SERM)Agonist or antagonist depending on tissue

12

Contraception

ProgestinsEstrogensProgesterone receptor modulator (PRM)

13

Suppression of hypothalamic-pituitary-gonadal axis

ProgestinsEstrogens

14

Replacement therapy

ProgestinsEstrogensSelective estrogen receptor modulator (SERM)

15

Ovulation inductions

Estrogen antagonistsAromatase inhibitors

16

Breast cancer therapy

Selective estrogen receptor modulator (SERM)Aromatase inhibitors

17

Abortion

Progesterone antagonists

18

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

NorethindroneNorgestrel

19

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

Medroxyprogesterone acetate

20

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

Etongestrel Most effective

21

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

NorethidroneNorgestrel Most effective

22

Mechanisms of action of progestins (2)

1. Decrease amount and increase viscosity of cervical mucus --> Prevent fertilization b/c sperm can't reach egg2. Inhibit gonadotropin secretion --> Prevent ovulation

23

Oral preparation of progestins + estrogens as contraceptive agents contain:

Norethidrone or drospirenone (progestin)Ethinyl estradiol (estrogen)

24

Mechanisms of action of progestins + estrogens (2)

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

25

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

1. Rifampin family of antibiotics 2. Anticonvulsants

26

Postcoital contraceptives contain:

2-4x the amount of progestins

27

Mechanism of action of postcoital contraceptives (non prescription)

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

28

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

ELLA: selective progesterone receptor modulator, PRM (ulipristal)

29

Mechanism of action of postcoital contraceptive (prescription)

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

30

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

Progestins

31

____ used as replacement therapy in ovarian dysfunction

Progestin/estrogen combinations

32

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

Progestin/estrogen combinations Lowest effective dose and shortest duration possible

33

Agonist or antagonist in bone?Estradiol

Agonist

34

Agonist or antagonist in breast?Estradiol

Agonist

35

Agonist or antagonist in CV system?Estradiol

Agonist

36

Agonist or antagonist in endometrium?Estradiol

Agonist

37

Agonist or antagonist in vaginal epithelium?Estradiol

Agonist

38

Agonist or antagonist in bone?Clomiphene/Fulvestrant

Antagonist

39

Agonist or antagonist in breast?Clomiphene/Fulvestrant

Antagonist

40

Agonist or antagonist in CV system?Clomiphene/Fulvestrant

Antagonist

41

Agonist or antagonist in endometrium?Clomiphene/Fulvestrant

Antagonist

42

Agonist or antagonist in vaginal epithelium?Clomiphene/Fulvestrant

Antagonist

43

Agonist or antagonist in bone?Tamoxifen

Agonist

44

Agonist or antagonist in breast?Tamoxifen

Antagonist

45

Agonist or antagonist in CV system?Tamoxifen

Agonist

46

Agonist or antagonist in endometrium?Tamoxifen

Agonist

47

Agonist or antagonist in vaginal epithelium?Tamoxifen

Agonist

48

Agonist or antagonist in bone?Raloxifene

Agonist

49

Agonist or antagonist in breast?Raloxifene

Antagonist

50

Agonist or antagonist in CV system?Raloxifene

Agonist

51

Agonist or antagonist in endometrium?Raloxifene

Neutral

52

Agonist or antagonist in vaginal epithelium?Raloxifene

Neutral

53

Agonist or antagonist in bone?Ospemifene

Agonist

54

Agonist or antagonist in breast?Ospemifene

Antagonist

55

Agonist or antagonist in CV system?Ospemifene

Agonist

56

Agonist or antagonist in endometrium?Ospemifene

Neutral

57

Agonist or antagonist in vaginal epithelium?Ospemifene

Agonist

58

Agonist or antagonist in bone?Bazedoxifene

Agonist

59

Agonist or antagonist in breast?Bazedoxifene

Antagonist

60

Agonist or antagonist in endometrium?Bazedoxifene

Antagonist

61

Agonist or antagonist in vaginal epithelium?Bazedoxifene

Agonist

62

Clomiphene is used to ____. It is a ____.

Induced ovulation Estrogen receptor antagonist

63

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

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

64

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

SERM Bone: postmenopausal symptoms, osteoporosisBreast: estrogen dependent breast cancer

65

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

Raloxifene

66

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

Ospemifene

67

____: Approved for treatment of postmonopausal symptoms (Agonistic/antagonistic) effects on bone and (agonistic/antagonistic) effect on breast and endometrium

BazedoxifeneAgonisticAntagonistic

68

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

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

69

Steroidal aromatase inhibitor

Exemestane

70

Non-steroidal aromatase inhibitor

Anastrozole

71

____: progesterone receptor antagonistUsed for: (3)

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

Testosterone is metabolize to ____ by ____

Dihydrotestosterone5-alpha-reductase

73

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

1. methyltestosterone (-OH)2. danazole (C triple bond)

74

Testosterone esters administered ____

intramuscularly

75

Testosterone administered ____ (2)

1. transdermally2. buccal tablets

76

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

17 alpha-alkylated androgens (Danazol)

77

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

Antiandrogens

78

5-alpha-reductase inhibitors (2)

Antiandrogens:FinasterideDutasteride

79

Androgen receptor antagonists (3)

Antiandrogens:FlutamideBicalutamideNilutamide

80

Inhibitors of steroid synthesis (2)

Antiandrogens:KetoconazoleSpironolactone

81

____ used to treat male-pattern baldness

Finasteride

82

____ inhibits testicular, adrenal and ovarian steroidogenesis

Ketoconazole

83

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

Spironolactone

84

Side effect of antiandrogens

Gynecomastia

85

Side effect of 5-alpha reductase inhibitors

Persistent sexual dysfunction

86

Male contraceptive made of:

Testosterone and nestorone (progestin) transdermally

87

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

IncreasesGonadotropinPituitary

88

____: stimulate gonadotropin secretionUsed to treat:Administered in ____fashion

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

89

Suppression of gonadotropin secretion used for: (4)

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

90

Long-acting synthetic GnRH agonist

Luprolide - injectableAct like suppression of gonadotropin secretion due to desensitization

91

GnRH antagonist

cetrorelix - injectable

92

____ IM injection induce follicular growth

FSH (GONAL-F)

93

____ IM injection induce ovulation

CG (PREGNYL) - longer half lifeLH (LUVERIS)

94

1st drug used to treat female infertility

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

95

2nd drug used to treat female infertility

FSH to induce follicular growth

96

3rd drug used to treat female infertility

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