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71 Cards in this Set
- Front
- Back
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17-beta estradiol (E2) secreted from?
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17-beta estradiol is secreted from the ovary
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estrone (E1) is secreted from?
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Estrone is secreted from the liver (formed from estradiol) and from peripheral tissues (formed from androstenedione)
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estriol (E3) is secreted from?
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Estriol is secreted from the placenta
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What metabolizes estradiol, estrone, and estriol?
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The liver metabolizes estradiol, estrone, and estriol
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Ethinyl estradiol drug class?
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Ethinyl estradiol is a synthetic steroidal estrogen
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Diethylstilbestrol drug class?
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Diethylstilbestrol is a nonsteroidal synthetic estrogen
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Risk of diethylstilbestrol?
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Risk of vaginal cancer in the offspring of mothers who took DES during pregnancy
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Pharmacologic effects of estrogen?
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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 |
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Tamoxifen drug class? ADRs? Benefit?
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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 |
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Toremifene drug class?
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Toremifene is a SERM to treat breast cancer
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Raloxifene drug class? ADRs? Benefit over other drugs in its class?
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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 |
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Clomiphene drug class?
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Clomiphene- estrogen antagonist used to induce ovulation
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Fluvestrant drug class?
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Fluvestrant- estrogen antagonist used to treat breast cancer progressive after tamoxifen
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Benefit of aromatase inhibitors over SERMS?
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Aromatase inhibitors don't increase the risk of DVTs or PEs
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Formestane drug class?
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Formestane- steroidal suicide inhibitor of aromatase
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Exemestane drug class?
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Exemestane- steroidal suicide inhibitor of aromatase
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Anastrozole drug class?
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Anastrozole- nonsteroidal reversible inhibitor of aromatase
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Letrozole drug class?
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Letrozole- nonsteroidal reversible inhibitor of aromatase
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Progesterone drug class? site of production? precursor for what compounds?
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Progesterone- progestin synthesized in the ovary, testis, adrenal gland, placenta
Progesterone is a precursor for estrogen, androgens, and adrenocortical steroids |
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MOA of the side effects of synthetic progestins?
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Synthetic progestins bind weakly to other steroid receptors including androgen, glucocorticoid, mineralocorticoid receptors
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Medroxyprogesterone drug class?
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Medroxyprogesterone- synthetic progestin
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Desogestrel drug class?
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Desogestrel- synthetic progestin
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Drospirenone drug class?
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Drospirenone- synthetic progestin
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Norethindrone drug class?
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Norethindrone- synthetic progestin
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Norgestimate drug class?
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Norgestimate- synthetic progestin
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Ethynodiol drug class?
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Ethynodiol- synthetic progestin
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Norgestrel drug class?
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Norgestrel- synthetic progestin
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L-Norgestrel drug class?
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L-Norgestrel- synthetic progestin
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Pharmacologic effects of progestin?
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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 |
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Drugs administered 48 hours after Mifepristone?
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Misoprostol (PGE1 analog) or Dinoprostol (PGE2 analog) administered after Mifepristone to induce uterine contraction to expel the detached conceptus
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Mifepristone (RU-486) drug class?
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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 |
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Ulipristal drug class?
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Ulipristal- partial agonist at progesterone receptors, inhibits ovulation, emergency contraceptive if taken within 5 days
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Primary agent of contraceptive effects in hormonal contraception?
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Progestin primarily responsible for contraceptive effects (inhibit LH surge and increase secretions)
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Effects of estrogen on gonadotropin? Clinical use?
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Estrogen inhibits secretion of FSH, used to prevent break through bleeding
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Severe ADRs of hormonal based contraception
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Severe ADRs of hormonal contraception: DVT, PE, MI, cerebrovascular disease, cholestatic jaundice and increased gallstones (due to progestin preparations), increased risk of breast cancer
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Sites of production of Dihydrotestosterone?
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DHT is produced in PROSTATE, skin, seminal vesicles, epididymis
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Steroid abused by athletes?
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Methyltestosterone is abused by athletes
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Clinical use of androgens?
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Androgens used for:
-replacement therapy (if spermatogenesis not required) -anabolic agent in AIDS wasting -stimulate growth in delayed puberty (males) |
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ADRs of androgens?
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ADRs of androgens:
-virilization of women -hepatic dysfunction -prostatic hyperplasia -azoospermia -hepatic adenomas and carcinomas -addiction |
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Flutamide drug class? Clinical uses?
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Flutamide- androgen receptor antagonist
Used in conjunction with GnRH for treatment of metastatic prostate cancer and treat female hirsutism |
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Finasteride drug class? Clinical uses?
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Finasteride- 5-alpha reductase inhibitor used to treat BPH and male pattern baldness
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Dutasteride drug class? Clincal use?
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Dutasteride is a 5-alpha reductase inhibitor used to treat BPH
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Gondaorelin drug class?
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Gondaorelin- GnRH agonist
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Goserelin drug class?
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Goserelin- potent GnRH agonist
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Histrelin drug class?
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Histrelin- potent GnRH agonist
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Leuprolide drug class?
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Leuprolide- potent GnRH agonist
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Naferelin drug class?
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Naferelin- potent GnRH agonist
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Pharmacodynamics of GnRH agonists?
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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
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Clinical uses of GnRH agonists?
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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 |
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ADR of GnRH agonist?
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GnRH agonist in women cause effects similar to menopause
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Benefit of GnRH antagonist over GnRH agonist?
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GnRH antagonist do not produce the flare of release
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Ganirelix drug class? Clinical use?
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Ganirelix- GnRH antagonist used for ovarian hyperstimulation procedures
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Cetrorelix drug class? Clinical use?
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Cetrorelix- GnRH antagonist used for ovarian hyperstimulation procedures
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Degarelix drug class? Clinical use?
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Degarelix- GnRH antagonist used to treat advanced prostate cancer
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Menotropin (hMG) drug class? What does it contain?
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Menotropin- human menopausal gonadotropin containing FSH and LH
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Urofollitropin drug class?
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Urofollitropin- FSH from urine of postmenopausal women
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Follitropin (alpha and beta) drug class?
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Follitropin- recombinant FSH
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Lutropin alpha drug class?
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Lutropin alpha- recombinant LH
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Novarel drug class?
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Novarel- urine derived hCG
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Choriogonadotropin alpha drug class?
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Choriogonadotropin alpha- recombinant hCG
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Clincal uses of LH/hCG?
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LH/hCG clinical uses:
-pregnancy testing -diagnose endocrine disorder -induce ovulation -treat male infertility |
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ADRs of LH/hCG?
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ADRs of LH/hCG:
-ovarian hyperstimulation and multiple pregnancies |
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Bromocriptine drug class?
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Bromocriptine- D2 receptor agonist
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Cabergoline drug class?
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Cabergoline- D2 receptor agonist
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Terazosin drug class? ADRs?
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Terazosin- alpha1 receptor antagonist
ADRs: orthostatic hypotension, syncope, dizziness |
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Doxazosin drug class? ADRs?
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Doxazosin- alpha1 receptor antagonist
ADRs: orthostatic hypotension, syncope, dizziness |
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Alfuzosin drug class? Benefits over other drugs in its class?
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Alfuzosin- alpha1 receptor antagonist
Little cardiovascular effects at doses used to treat BPH |
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Tamsulosin drug class? Benefits over other drugs in its class? ADR?
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Tamsulosin- alpha1 receptor antagonist
Little effects on peripheral vascular resistance and hypotension ADR: ejaculatory dysfunction |
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Silodosin drug class? Benefits over other drugs in its class? ADR?
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Silodosin- alpha1 receptor antagonist
Little effects on peripheral vascular resistance and hypotension ADR: ejaculatory dysfunction |
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Finasteride drug class?
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Finasteride- 5 alpha reductase inhibitor
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Dutasteride drug class?
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Dutasteride- 5 alpha reductase inhibitor
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