deck_3556451 Flashcards
Progesterone A is mostly a transcripitional (activator/repressor)
activator
Progesterone B is mostly a transcripitional (activator/repressor)
repressor
Cross reacts with other steroid receptors more than natural progesterone
Norethindrone
Used in combination type contraceptives
Norethindorne Ethinyl estrodiol (most common)
_____: progestin with enhanced activity as minoeralocorticoid (agonist/antagonist) and androgen (agonist/antagonist)
Drospirenone (oral)AntagonistAntagonist
____: selective progesterone receptor modulator (PRM) Used for: ___
Ulipristal (oral)Can be agonist or antagonist, depending on tissue Post sex contraceptive
____: Progesterone antagonistUsed for abortions
Minfepristone (oral)
Estrone sulfate (oral) used in ___
hormone replacement therapy
1st non-steroidal estrogens No longer in useBad side effects of offspring and mothers
Diethylstilbestrol (DES)
Environmental contaminant with estrogen-like effects
Bisphenol A (BPA)
Tamoxifen (oral)
Selective estrogen receptor modulator (SERM)Agonist or antagonist depending on tissue
Contraception
ProgestinsEstrogensProgesterone receptor modulator (PRM)
Suppression of hypothalamic-pituitary-gonadal axis
ProgestinsEstrogens
Replacement therapy
ProgestinsEstrogensSelective estrogen receptor modulator (SERM)
Ovulation inductions
Estrogen antagonistsAromatase inhibitors
Breast cancer therapy
Selective estrogen receptor modulator (SERM)Aromatase inhibitors
Abortion
Progesterone antagonists
Continuous administration of progestin as contraceptive agents Oral (daily) (2)
NorethindroneNorgestrel
IM injections (every 3 months) of progestins as contraceptive agents
Medroxyprogesterone acetate
Subcutaneous implants (every 3 years) of progestins as contraceptive agents
Etongestrel Most effective
IUDs (every 1-5 years) of progestins as contraceptive agents
NorethidroneNorgestrel Most effective
Mechanisms of action of progestins (2)
- Decrease amount and increase viscosity of cervical mucus –> Prevent fertilization b/c sperm can’t reach egg2. Inhibit gonadotropin secretion –> Prevent ovulation
Oral preparation of progestins + estrogens as contraceptive agents contain:
Norethidrone or drospirenone (progestin)Ethinyl estradiol (estrogen)
Mechanisms of action of progestins + estrogens (2)
- Inhibit hypothalamus and pituitary –> prevent ovulation2. Progestins: Decrease amount and increase viscosity of cervical mucus –> Prevent fertilization b/c sperm can’t reach egg
Efficacy of combination-type contraceptives is reduced by: (2)
- Rifampin family of antibiotics 2. Anticonvulsants
Postcoital contraceptives contain:
2-4x the amount of progestins
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
Postcoital contraceptive more effective than norgestrel and maintains efficacy for longer times, 5 days after unprotected intercourse
ELLA: selective progesterone receptor modulator, PRM (ulipristal)
Mechanism of action of postcoital contraceptive (prescription)
- 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
____ used to suppress hypothalamic-pituitary-ovarian axis in treatment of dysmenorrhea and endometriosis
Progestins
____ used as replacement therapy in ovarian dysfunction
Progestin/estrogen combinations
____ used as replacement therapy for treatment of postmenopausal symptoms and postmenopausal osteoporosis
Progestin/estrogen combinations Lowest effective dose and shortest duration possible
Agonist or antagonist in bone?Estradiol
Agonist
Agonist or antagonist in breast?Estradiol
Agonist
Agonist or antagonist in CV system?Estradiol
Agonist
Agonist or antagonist in endometrium?Estradiol
Agonist
Agonist or antagonist in vaginal epithelium?Estradiol
Agonist
Agonist or antagonist in bone?Clomiphene/Fulvestrant
Antagonist
Agonist or antagonist in breast?Clomiphene/Fulvestrant
Antagonist
Agonist or antagonist in CV system?Clomiphene/Fulvestrant
Antagonist
Agonist or antagonist in endometrium?Clomiphene/Fulvestrant
Antagonist
Agonist or antagonist in vaginal epithelium?Clomiphene/Fulvestrant
Antagonist
Agonist or antagonist in bone?Tamoxifen
Agonist
Agonist or antagonist in breast?Tamoxifen
Antagonist
Agonist or antagonist in CV system?Tamoxifen
Agonist
Agonist or antagonist in endometrium?Tamoxifen
Agonist
Agonist or antagonist in vaginal epithelium?Tamoxifen
Agonist
Agonist or antagonist in bone?Raloxifene
Agonist
Agonist or antagonist in breast?Raloxifene
Antagonist
Agonist or antagonist in CV system?Raloxifene
Agonist
Agonist or antagonist in endometrium?Raloxifene
Neutral
Agonist or antagonist in vaginal epithelium?Raloxifene
Neutral
Agonist or antagonist in bone?Ospemifene
Agonist
Agonist or antagonist in breast?Ospemifene
Antagonist
Agonist or antagonist in CV system?Ospemifene
Agonist
Agonist or antagonist in endometrium?Ospemifene
Neutral
Agonist or antagonist in vaginal epithelium?Ospemifene
Agonist
Agonist or antagonist in bone?Bazedoxifene
Agonist
Agonist or antagonist in breast?Bazedoxifene
Antagonist
Agonist or antagonist in endometrium?Bazedoxifene
Antagonist
Agonist or antagonist in vaginal epithelium?Bazedoxifene
Agonist
Clomiphene is used to ____. It is a ____.
Induced ovulation Estrogen receptor antagonist
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
Raloxifene is a ____.Used as estrogen agonist in ____Antagonist in ____
SERM Bone: postmenopausal symptoms, osteoporosisBreast: estrogen dependent breast cancer
____ has the advantage as a SERM by not being an agonist in endometrium. Does not stimulate endometrial proliferation.
Raloxifene
____: Approved for treatment of vaginal atrophy in postmenopausal women.Agonistic effects on vaginal epithelium.
Ospemifene
____: Approved for treatment of postmonopausal symptoms (Agonistic/antagonistic) effects on bone and (agonistic/antagonistic) effect on breast and endometrium
BazedoxifeneAgonisticAntagonistic
____: inhibit conversion of androgens to estrogens.Used for: (2)
Aromatase inhibitors1. Treatment of breast cancer in postmenopausal women2. Induce ovulation
Steroidal aromatase inhibitor
Exemestane
Non-steroidal aromatase inhibitor
Anastrozole
____: 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
Testosterone is metabolize to ____ by ____
Dihydrotestosterone5-alpha-reductase
Testosterone analogs (2) that are modified at C17. Can be taken orally.
- methyltestosterone (-OH)2. danazole (C triple bond)
Testosterone esters administered ____
intramuscularly
Testosterone administered ____ (2)
- transdermally2. buccal tablets
____ effective when given orally but have more side effects, especially hepatic toxicity.
17 alpha-alkylated androgens (Danazol)
Used to treat syndromes of androgen excess or androgen-dependent disorders
Antiandrogens
5-alpha-reductase inhibitors (2)
Antiandrogens:FinasterideDutasteride
Androgen receptor antagonists (3)
Antiandrogens:FlutamideBicalutamideNilutamide
Inhibitors of steroid synthesis (2)
Antiandrogens:KetoconazoleSpironolactone
____ used to treat male-pattern baldness
Finasteride
____ inhibits testicular, adrenal and ovarian steroidogenesis
Ketoconazole
____ inhibits 17-alpha hydroxylase, androgen receptor, mineralocorticoid receptor antagonist
Spironolactone
Side effect of antiandrogens
Gynecomastia
Side effect of 5-alpha reductase inhibitors
Persistent sexual dysfunction
Male contraceptive made of:
Testosterone and nestorone (progestin) transdermally
Pulsatile GNRH (increases/decreases) _____ secretion from _____.
IncreasesGonadotropinPituitary
____: stimulate gonadotropin secretionUsed to treat:Administered in ____fashion
Synthetic GnRH: gonadorelinTreats: delayed puberty in boys and girls, anovulatory disorders in womenPulsatile
Suppression of gonadotropin secretion used for: (4)
- treatment of endometriosis and dysmenorrhea 2. ovulation induction 3. Precocious puberty 4. Androgen excess in males
Long-acting synthetic GnRH agonist
Luprolide - injectableAct like suppression of gonadotropin secretion due to desensitization
GnRH antagonist
cetrorelix - injectable
____ IM injection induce follicular growth
FSH (GONAL-F)
____ IM injection induce ovulation
CG (PREGNYL) - longer half lifeLH (LUVERIS)
1st drug used to treat female infertility
Long acting GnRH agonist or GnRH antagonist to prevent endogenous gonadotropin secretion
2nd drug used to treat female infertility
FSH to induce follicular growth
3rd drug used to treat female infertility
LH or hCG to induce ovulation when follicular growth is deemed appropriate