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Undeleted > Pharmacology Gonadal Steroids/Reproductive Hormones > Flashcards

Pharmacology Gonadal Steroids/Reproductive Hormones Flashcards

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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
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 doses Only 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, osteoporosis Breast: 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
Bazedoxifene Agonistic Antagonistic
68
____: inhibit conversion of androgens to estrogens. | Used for: (2)
Aromatase inhibitors 1. Treatment of breast cancer in postmenopausal women 2. Induce ovulation
69
Steroidal aromatase inhibitor
Exemestane
70
Non-steroidal aromatase inhibitor
Anastrozole
71
____: progesterone receptor antagonist | Used 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 ____
Dihydrotestosterone | 5-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. transdermally | 2. 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: Finasteride Dutasteride
79
Androgen receptor antagonists (3)
Antiandrogens: Flutamide Bicalutamide Nilutamide
80
Inhibitors of steroid synthesis (2)
Antiandrogens: Ketoconazole Spironolactone
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 _____.
Increases Gonadotropin Pituitary
88
____: stimulate gonadotropin secretion Used to treat: Administered in ____fashion
Synthetic GnRH: gonadorelin Treats: delayed puberty in boys and girls, anovulatory disorders in women Pulsatile
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 - injectable | Act 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 life | LH (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

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