- AR antagonist - treats PCOS by targeting AR - blocks masculinizing effects of testosterone like excessive androgen stim of hair follicles (hirsutism)

- Treats PCOS by targeting associated pathways - anti-diabetic drug that decreases hepatic gluconeogenesis leading to decreases in insulin - increases fertility w/in weeks, masculinizing symptoms take longer to resolve

- dopamine AGONIST - used to treat hyperprolactinemia (inhibitory effect) - suppresses prolactin secretion and tumor size

- ER ANTAGONIST - treatment of breast cancers expressing ERs

- GnRH AGONIST - same as goserelin and nafarelin - causes receptor desensitization in pituitary; but initial spike before suppression - treats prostate cancer, some BCs, uterine fibroids, endometriosis, premature puberty - prevents premature ovulation (IVF) and can delay puberty for transgender children

- GnRH AGONIST - same as leuprolide and nafarelin (below) - causes receptor desensitization in pituitary; but initial spike before suppression - treats prostate cancer, some BCs, uterine fibroids, endometriosis, premature puberty - prevents premature ovulation (IVF) and can delay puberty for transgender children

- GnRH AGONIST - same as leuprolide and Goserelin - causes receptor desensitization in pituitary; but initial spike before suppression - treats prostate cancer, some BCs, uterine fibroids, endometriosis, premature puberty - prevents premature ovulation (IVF) and can delay puberty for transgender children

- GnRH ANTAGONIST - blocks release of LH and FSH; no initial stim - delays ovulation for IVF (controlled stim)

- GnRH ANTAGONIST - blocks release of LH and FSH; no initial stim - controlled ovarian hyperstim for IVF

- type II 5alpha-reductase inhibitor - slows growth of prostate tissue and promotes apoptosis - treats BPH and prostate cancer - 1 year treatment can reduce prostate size by 25% - prostate cancer treatment most effective in those with larger prostates - BPH: improve symptoms of decreased urine flow (prevents progression) - adverse: decreased libido, ED

- type I and II 5alpha-reductase inhibitor - slows growth of prostate tissue and promotes apoptosis - treats BPH and prostate cancer - prostate cancer treatment most effective in those with large prostates - BPH: improve symptoms of decreased urine flow (prevents progression) - adverse: decreased libido, ED

- competitive aromatase inhibitor - compete for binding w/ androgenic precursors to aromatase - treatment of postmenopausal (ONLY!) metastatic BC; also prophylactic recurrences of cancers treated with surgery and radiation - if cancer not estrogen sensitive, will not work - completely ablates estrogen production - adverse: fewer serious side effects than SERMs, increased risk of osteoporotic fractures, heart problems

- competitive aromatase inhibitor - compete for binding with androgenic precursors to aromatase - treatment of postmenopausal (ONLY!) metastatic BC; also prophylactic recurrences of cancers treated with surgery and radiation - if cancer not estrogen sensitive, will not work - completely ablates estrogen production - adverse: fewer serious side effects than SERMs, increased risk of osteoporotic fractures, heart problems

- covalently-bound aromatase inhibitor - treatment of postmenopausal (ONLY!) metastatic BC; also prophylactic recurrences of cancers treated with surgery and radiation - if cancer not estrogen sensitive, will not work - completely ablates estrogen production - adverse: fewer serious side effects than SERMs, increased risk of osteoporotic fractures, heart problems

- covalently-bound aromatase inhibitor - treatment of post-menopausal (ONLY!) metastatic BC; also prophylactic recurrences of cancers treated with surgery and radiation - if cancer not estrogen sensitive, will not work - completely ablates estrogen production - adverse: fewer serious side effects than SERMs, increased risk osteoporotic fractures, heart problems

- SERM - only SERM approved in treatment AND prevention of BC - selectivity: ER ANTAGONIST in breast tissue, ER partial agonist in endometrium, ER partial agonist in bone - used in palliative treatment of metastatic BC; used as adjuvant therapy after lumpectomy - inhibits estrogen-dependent growth of BC - stims endo growth - associated with 4-6 fold increase in endometrial cancer --> administered no more than 5 years before switched to aromatase inhibitor - more deep vein thrombosis and cataracts (in addition to endo-related) than Raloxifene, but prevented more cases of non-invasive BC - 50% reduction in devel of invasive BC in high risk women (STAR Trial)

- SERM - selectivity: ER ANTAGONIST in breast tissue, ER agonist in bone, ER ANTAGONIST in endo - does NOT increase endometrial cancer risk - decreases bone resorption (beneficial in slowing osteoporosis) - in STAR trial compared to Tamoxifen, both agents 50% reduction in devel of invasive BC in high-risk women - less endo-related side effects, less deep vein thrombosis, less cataract devel than Tamoxifen - prevented LESS cases of invasive BC than Tamoxifen

- SERM - selectivity: ER ANTAGONIST in hypo and anterior pituitary which inhibits neg feedback by E2, increases GnRH; ER partial agonist in ovaries - used to induce ovulation: increases release of GnRH and gonadotropins, increased levels of FSH stims follicle growth, follicle give estrogen trigger signal, LH surge and ovulation happen - adverse: can cause multiple follicles to grow which can result in increased ovarian size - use is seldom associated with ovarian hyperstim syndrome

- competitive AR ANTAGONIST - blocks action of T and DHT - used to treat prostate cancer

- competitive AR ANTAGONIST - also progestational effects - used as progestin in some combination contraceptives

Exam 2 Drugs: Repro (50) Flashcards by Lauren Stippich

Spironolactone

AR antagonist
treats PCOS by targeting AR
blocks masculinizing effects of testosterone like excessive androgen stim of hair follicles (hirsutism)

How well did you know this?

Not at all

Perfectly

Metformin

Treats PCOS by targeting associated pathways
anti-diabetic drug that decreases hepatic gluconeogenesis leading to decreases in insulin
increases fertility w/in weeks, masculinizing symptoms take longer to resolve

How well did you know this?

Not at all

Perfectly

Cabergoline

dopamine AGONIST
used to treat hyperprolactinemia (inhibitory effect)
suppresses prolactin secretion and tumor size

How well did you know this?

Not at all

Perfectly

Bromocriptin

dopamine AGONIST
used to treat hyperprolactinemia (inhibitory effect)
suppresses prolactin secretion and tumor size

How well did you know this?

Not at all

Perfectly

Fulvesterant

ER ANTAGONIST

- treatment of breast cancers expressing ERs

How well did you know this?

Not at all

Perfectly

Leuprolide

GnRH AGONIST
same as goserelin and nafarelin
causes receptor desensitization in pituitary; but initial spike before suppression
treats prostate cancer, some BCs, uterine fibroids, endometriosis, premature puberty
prevents premature ovulation (IVF) and can delay puberty for transgender children

How well did you know this?

Not at all

Perfectly

Goserelin

GnRH AGONIST
same as leuprolide and nafarelin (below)
causes receptor desensitization in pituitary; but initial spike before suppression
treats prostate cancer, some BCs, uterine fibroids, endometriosis, premature puberty
prevents premature ovulation (IVF) and can delay puberty for transgender children

How well did you know this?

Not at all

Perfectly

Nafarelin

GnRH AGONIST
same as leuprolide and Goserelin
causes receptor desensitization in pituitary; but initial spike before suppression
treats prostate cancer, some BCs, uterine fibroids, endometriosis, premature puberty
prevents premature ovulation (IVF) and can delay puberty for transgender children

How well did you know this?

Not at all

Perfectly

Cetrorelix

GnRH ANTAGONIST
blocks release of LH and FSH; no initial stim
delays ovulation for IVF (controlled stim)

How well did you know this?

Not at all

Perfectly

Ganirelix

GnRH ANTAGONIST
blocks release of LH and FSH; no initial stim
controlled ovarian hyperstim for IVF

How well did you know this?

Not at all

Perfectly

Finasteride

type II 5alpha-reductase inhibitor
slows growth of prostate tissue and promotes apoptosis
treats BPH and prostate cancer
1 year treatment can reduce prostate size by 25%
prostate cancer treatment most effective in those with larger prostates
BPH: improve symptoms of decreased urine flow (prevents progression)
adverse: decreased libido, ED

How well did you know this?

Not at all

Perfectly

Dutasteride

type I and II 5alpha-reductase inhibitor
slows growth of prostate tissue and promotes apoptosis
treats BPH and prostate cancer
prostate cancer treatment most effective in those with large prostates
BPH: improve symptoms of decreased urine flow (prevents progression)
adverse: decreased libido, ED

How well did you know this?

Not at all

Perfectly

Anastrozole

competitive aromatase inhibitor
compete for binding w/ androgenic precursors to aromatase
treatment of postmenopausal (ONLY!) metastatic BC; also prophylactic recurrences of cancers treated with surgery and radiation
if cancer not estrogen sensitive, will not work
completely ablates estrogen production
adverse: fewer serious side effects than SERMs, increased risk of osteoporotic fractures, heart problems

How well did you know this?

Not at all

Perfectly

Letrozole

competitive aromatase inhibitor
compete for binding with androgenic precursors to aromatase
treatment of postmenopausal (ONLY!) metastatic BC; also prophylactic recurrences of cancers treated with surgery and radiation
if cancer not estrogen sensitive, will not work
completely ablates estrogen production
adverse: fewer serious side effects than SERMs, increased risk of osteoporotic fractures, heart problems

How well did you know this?

Not at all

Perfectly

Exemestane

covalently-bound aromatase inhibitor
treatment of postmenopausal (ONLY!) metastatic BC; also prophylactic recurrences of cancers treated with surgery and radiation
if cancer not estrogen sensitive, will not work
completely ablates estrogen production
adverse: fewer serious side effects than SERMs, increased risk of osteoporotic fractures, heart problems

How well did you know this?

Not at all

Perfectly

Formestane

covalently-bound aromatase inhibitor
treatment of post-menopausal (ONLY!) metastatic BC; also prophylactic recurrences of cancers treated with surgery and radiation
if cancer not estrogen sensitive, will not work
completely ablates estrogen production
adverse: fewer serious side effects than SERMs, increased risk osteoporotic fractures, heart problems

How well did you know this?

Not at all

Perfectly

Tamoxifen

SERM
only SERM approved in treatment AND prevention of BC
selectivity: ER ANTAGONIST in breast tissue, ER partial agonist in endometrium, ER partial agonist in bone
used in palliative treatment of metastatic BC; used as adjuvant therapy after lumpectomy
inhibits estrogen-dependent growth of BC
stims endo growth
associated with 4-6 fold increase in endometrial cancer –> administered no more than 5 years before switched to aromatase inhibitor
more deep vein thrombosis and cataracts (in addition to endo-related) than Raloxifene, but prevented more cases of non-invasive BC
50% reduction in devel of invasive BC in high risk women (STAR Trial)

How well did you know this?

Not at all

Perfectly

Raloxifene

SERM
selectivity: ER ANTAGONIST in breast tissue, ER agonist in bone, ER ANTAGONIST in endo
does NOT increase endometrial cancer risk
decreases bone resorption (beneficial in slowing osteoporosis)
in STAR trial compared to Tamoxifen, both agents 50% reduction in devel of invasive BC in high-risk women
less endo-related side effects, less deep vein thrombosis, less cataract devel than Tamoxifen
prevented LESS cases of invasive BC than Tamoxifen

How well did you know this?

Not at all

Perfectly

Clomiphene

SERM
selectivity: ER ANTAGONIST in hypo and anterior pituitary which inhibits neg feedback by E2, increases GnRH; ER partial agonist in ovaries
used to induce ovulation: increases release of GnRH and gonadotropins, increased levels of FSH stims follicle growth, follicle give estrogen trigger signal, LH surge and ovulation happen
adverse: can cause multiple follicles to grow which can result in increased ovarian size
use is seldom associated with ovarian hyperstim syndrome

How well did you know this?

Not at all

Perfectly

Flutamide

competitive AR ANTAGONIST
blocks action of T and DHT
used to treat prostate cancer

How well did you know this?

Not at all

Perfectly

Enzalutamide

competitive AR ANTAGONIST
blocks action of T and DHT
used to treat prostate cancer

How well did you know this?

Not at all

Perfectly

Bicalutamide

competitive AR ANTAGONIST
blocks action of T and DHT
used to treat prostate cancer

How well did you know this?

Not at all

Perfectly

Drospirenone

competitive AR ANTAGONIST
also progestational effects
used as progestin in some combination contraceptives

Mifepristone

competitive progest receptor antagonist
used to induce 1st trimester abortions
95% effective
results in decay and death of the decidua
lack of nourishment causes blastocyst to die and detach from uterus –> stops secretion of hCG so corpus luteum involutes
decreases progesterone synth and secretion
commonly given with misoprostol
given as single dose so adverse is rare
main complication is excessive bleeding

Misoprostol

- synthetic prostaglandin E1 analogue - stims uterine contractions - given with mifepristone to induce abortion (1st T) - adverse: nausea and vomiting

Ethinyl Estradiol

- used as estrogen in combo BC

Mestranol

- used as estrogen in combo BC

Norgestrel

- progestin in combo BC | - highest androgenic activity (1 of 2)

Levonorgestrel

- progestin in combo BC | - highest androgenic activity (1 of 2)

Norethidrone

- progestin in combo BC | - lower androgenic activity (1 of 2)

Norethidrone acetate

- progestin in combo BC | - lower androgenic activity (1 of 2)

Etonogestrel

- progestin in combo BC - 3rd gen - even lower AR cross-reactivity (1 of 5)

Ethynodiol

- progestin in combo BC - 3rd gen - even lower AR cross-reactivity

Norgestimate

- progestin in combo BC - 3rd gen - even lower AR cross-reactivity

Gestodene

- progestin in combo BC - 3rd gen - even lower AR cross-reactivity

Desogestrel

- progestin in combo BC - 3rd gen - even lower AR cross-reactivity

Vaginal Ring

- Ethinyl Estradiol and etonogestrel (3rd gen progestin)

Transdermal Patches

- Ethinyl Estradiol and norelgestromin

Oral Tablets 84 days on, 7 days off

- Ethinyl Estradiol and levonorgestrel (high androgenic activity)

Quadphasic Formulations

- Dinogest/Estradiol

Mini-Pill

- Norgestrel (high AR cross reactivity), Norethindrone (lower androgenic activity)

Injectable- Progestin only

- Medroxyprogesterone Acetate

Implant - Progestin only

- Etonogestrel (3rd gen progestin)

IUD

- levonogestrel (high androgenic cross-reactivity, but low amts gets into circulation)

Emergency Contraceptive

- Oral Levonogestrel (high cross reactivity)

Male Contraceptives (from trials)

- Testosterone enanthate - Testosterone enanthate + oral levonorgestrel (high AR cross reactivity) - Testosterone undecanoate + medroxyprogesterone acetate - combinations more effective and more reversible

Hormone replacement Men: IM

- testosterone enanthate | - testosterone cyprionate

Sildenafil

- PDE5 inhibitor - first effective oral agent for ED - effect observed 30-60 mins - metabolized after 8 hours - nitrates should not be taken for 24 hours after use - affects clearance of coumadin and tolbutamide - clearance is affected by cimetidine and erythromycin - more drug drug interactions than other PDE5 inhibitors - adverse: headache, flushing, resp tract disorders

Vardenafil

- PDE5 inhibitor - similar rates of uptake and metabolism to sildenafil (30-60 min; 8 hrs) - nitrates should not be taken for 24 hours after use - clearance affected by erythromycin - adverse: headache, flushing, resp tract disorders

Tadalafil

- PDE5 inhibitor - uptake 60 mins - 36 hr duration - should not take nitrates for >36 hours - clearance affected by erythromycin - adverse: headache, flushing, resp tract disorders

Premarin

- vaginal estrogen cream (1 of 3) | - used to treat female sexual dysfunction

Estrace

- vaginal estrogen cream (1 of 3) | - used to treat female sexual dysfunction

Ogen

- vaginal estrogen cream (1 of 3) | - used to treat female sexual dysfunction

Estring

- Vaginal estrogen ring | - used to treat female sexual dysfunction

Flibanserin

- "female viagra" - used to treat female sexual dysfunction - risk of serious hypo and syncope especially in patients with hepatic dysfunction or taking meds that inhibit CYP3A4 - originally developed as an anti-depressant

Androstenedione

- adrenal androgen precursor abused in steroid use

Dehydroepiandrosterone

- DHEA | - abused in steroid use