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71 Cards in this Set

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17-beta estradiol (E2) secreted from?
17-beta estradiol is secreted from the ovary
estrone (E1) is secreted from?
Estrone is secreted from the liver (formed from estradiol) and from peripheral tissues (formed from androstenedione)
estriol (E3) is secreted from?
Estriol is secreted from the placenta
What metabolizes estradiol, estrone, and estriol?
The liver metabolizes estradiol, estrone, and estriol
Ethinyl estradiol drug class?
Ethinyl estradiol is a synthetic steroidal estrogen
Diethylstilbestrol drug class?
Diethylstilbestrol is a nonsteroidal synthetic estrogen
Risk of diethylstilbestrol?
Risk of vaginal cancer in the offspring of mothers who took DES during pregnancy
Pharmacologic effects of estrogen?
Estrogen:
-female maturation
-hyperplasia of endometrium (increased risk of endometrial cancer)
-coagulability increased
-inhibit osteoclasts
-stimulate synthesis of transcortin, thyroxin binding protein, SHBG, rennin substrate, fibrinogen
-increase HDL, lower LDL, lower cholesterol, raise triglycerides
-increased risk of breast cancer
Tamoxifen drug class? ADRs? Benefit?
Tamoxifen is a SERM used to treat ER positive breast cancer
ADRs: increased risk of endometrial cancer, hot flashes, nausea, DVT, PE

Benefit: decreases bone resorption
Toremifene drug class?
Toremifene is a SERM to treat breast cancer
Raloxifene drug class? ADRs? Benefit over other drugs in its class?
Raloxifene is a SERM used to prevent osteoporosis and decrease risk fo invasive breast cancer

ADRs: PE, DVT

Doesn't cause proliferation of endometrial tissue
Clomiphene drug class?
Clomiphene- estrogen antagonist used to induce ovulation
Fluvestrant drug class?
Fluvestrant- estrogen antagonist used to treat breast cancer progressive after tamoxifen
Benefit of aromatase inhibitors over SERMS?
Aromatase inhibitors don't increase the risk of DVTs or PEs
Formestane drug class?
Formestane- steroidal suicide inhibitor of aromatase
Exemestane drug class?
Exemestane- steroidal suicide inhibitor of aromatase
Anastrozole drug class?
Anastrozole- nonsteroidal reversible inhibitor of aromatase
Letrozole drug class?
Letrozole- nonsteroidal reversible inhibitor of aromatase
Progesterone drug class? site of production? precursor for what compounds?
Progesterone- progestin synthesized in the ovary, testis, adrenal gland, placenta

Progesterone is a precursor for estrogen, androgens, and adrenocortical steroids
MOA of the side effects of synthetic progestins?
Synthetic progestins bind weakly to other steroid receptors including androgen, glucocorticoid, mineralocorticoid receptors
Medroxyprogesterone drug class?
Medroxyprogesterone- synthetic progestin
Desogestrel drug class?
Desogestrel- synthetic progestin
Drospirenone drug class?
Drospirenone- synthetic progestin
Norethindrone drug class?
Norethindrone- synthetic progestin
Norgestimate drug class?
Norgestimate- synthetic progestin
Ethynodiol drug class?
Ethynodiol- synthetic progestin
Norgestrel drug class?
Norgestrel- synthetic progestin
L-Norgestrel drug class?
L-Norgestrel- synthetic progestin
Pharmacologic effects of progestin?
Progestin:
-decreases GnRH pulses
-inhibits estrogen driven endometrial proliferation
-inhibits myometrial contraction
-produces thick secretions
-develop mammary glands
-increase sensitivity to pCO2 levels
-promote GABA receptors in brain
-increase basal levels of insulin
-stimulates lipoprotein lipase causing adipose deposition
Drugs administered 48 hours after Mifepristone?
Misoprostol (PGE1 analog) or Dinoprostol (PGE2 analog) administered after Mifepristone to induce uterine contraction to expel the detached conceptus
Mifepristone (RU-486) drug class?
Mifepristone- competitive antagonist of progesterone receptors, also inhibits corticosteroid and androgen receptors causing an increase in ACTH and increases in cortisol and androgen levels

Administered <49 days after start of last menstrual period
Ulipristal drug class?
Ulipristal- partial agonist at progesterone receptors, inhibits ovulation, emergency contraceptive if taken within 5 days
Primary agent of contraceptive effects in hormonal contraception?
Progestin primarily responsible for contraceptive effects (inhibit LH surge and increase secretions)
Effects of estrogen on gonadotropin? Clinical use?
Estrogen inhibits secretion of FSH, used to prevent break through bleeding
Severe ADRs of hormonal based contraception
Severe ADRs of hormonal contraception: DVT, PE, MI, cerebrovascular disease, cholestatic jaundice and increased gallstones (due to progestin preparations), increased risk of breast cancer
Sites of production of Dihydrotestosterone?
DHT is produced in PROSTATE, skin, seminal vesicles, epididymis
Steroid abused by athletes?
Methyltestosterone is abused by athletes
Clinical use of androgens?
Androgens used for:
-replacement therapy (if spermatogenesis not required)
-anabolic agent in AIDS wasting
-stimulate growth in delayed puberty (males)
ADRs of androgens?
ADRs of androgens:
-virilization of women
-hepatic dysfunction
-prostatic hyperplasia
-azoospermia
-hepatic adenomas and carcinomas
-addiction
Flutamide drug class? Clinical uses?
Flutamide- androgen receptor antagonist

Used in conjunction with GnRH for treatment of metastatic prostate cancer and treat female hirsutism
Finasteride drug class? Clinical uses?
Finasteride- 5-alpha reductase inhibitor used to treat BPH and male pattern baldness
Dutasteride drug class? Clincal use?
Dutasteride is a 5-alpha reductase inhibitor used to treat BPH
Gondaorelin drug class?
Gondaorelin- GnRH agonist
Goserelin drug class?
Goserelin- potent GnRH agonist
Histrelin drug class?
Histrelin- potent GnRH agonist
Leuprolide drug class?
Leuprolide- potent GnRH agonist
Naferelin drug class?
Naferelin- potent GnRH agonist
Pharmacodynamics of GnRH agonists?
GnRH agonists- first 7-10 days increase secretion of LH and FSH (flare) followed by a decrease in secretion of FSH, LH, and gonadal steroid hormones
Clinical uses of GnRH agonists?
GnRH agonist clinical uses:
-female infertility treatment
-male infertility treatment
-diagnose LH hyporesponsiveness (constitutional delay vs. hypogonadotropic hypogonadism)
-suppression of gonadotropic secretion during assisted reproduction techniques
-endometriosis treatment
-uterine leiomyomata treatment
-prostate cancer treatment (suppress flare with co-administration of androgen antagonist)
-inhibit precocious puberty
ADR of GnRH agonist?
GnRH agonist in women cause effects similar to menopause
Benefit of GnRH antagonist over GnRH agonist?
GnRH antagonist do not produce the flare of release
Ganirelix drug class? Clinical use?
Ganirelix- GnRH antagonist used for ovarian hyperstimulation procedures
Cetrorelix drug class? Clinical use?
Cetrorelix- GnRH antagonist used for ovarian hyperstimulation procedures
Degarelix drug class? Clinical use?
Degarelix- GnRH antagonist used to treat advanced prostate cancer
Menotropin (hMG) drug class? What does it contain?
Menotropin- human menopausal gonadotropin containing FSH and LH
Urofollitropin drug class?
Urofollitropin- FSH from urine of postmenopausal women
Follitropin (alpha and beta) drug class?
Follitropin- recombinant FSH
Lutropin alpha drug class?
Lutropin alpha- recombinant LH
Novarel drug class?
Novarel- urine derived hCG
Choriogonadotropin alpha drug class?
Choriogonadotropin alpha- recombinant hCG
Clincal uses of LH/hCG?
LH/hCG clinical uses:
-pregnancy testing
-diagnose endocrine disorder
-induce ovulation
-treat male infertility
ADRs of LH/hCG?
ADRs of LH/hCG:
-ovarian hyperstimulation and multiple pregnancies
Bromocriptine drug class?
Bromocriptine- D2 receptor agonist
Cabergoline drug class?
Cabergoline- D2 receptor agonist
Terazosin drug class? ADRs?
Terazosin- alpha1 receptor antagonist

ADRs: orthostatic hypotension, syncope, dizziness
Doxazosin drug class? ADRs?
Doxazosin- alpha1 receptor antagonist

ADRs: orthostatic hypotension, syncope, dizziness
Alfuzosin drug class? Benefits over other drugs in its class?
Alfuzosin- alpha1 receptor antagonist

Little cardiovascular effects at doses used to treat BPH
Tamsulosin drug class? Benefits over other drugs in its class? ADR?
Tamsulosin- alpha1 receptor antagonist

Little effects on peripheral vascular resistance and hypotension

ADR: ejaculatory dysfunction
Silodosin drug class? Benefits over other drugs in its class? ADR?
Silodosin- alpha1 receptor antagonist

Little effects on peripheral vascular resistance and hypotension

ADR: ejaculatory dysfunction
Finasteride drug class?
Finasteride- 5 alpha reductase inhibitor
Dutasteride drug class?
Dutasteride- 5 alpha reductase inhibitor