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Pharmacology III > Exam 2 Drugs: Repro (50) > Flashcards

Exam 2 Drugs: Repro (50) Flashcards

1
Q

Spironolactone

A
  • AR antagonist
  • treats PCOS by targeting AR
  • blocks masculinizing effects of testosterone like excessive androgen stim of hair follicles (hirsutism)
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2
Q

Metformin

A
  • 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
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3
Q

Cabergoline

A
  • dopamine AGONIST
  • used to treat hyperprolactinemia (inhibitory effect)
  • suppresses prolactin secretion and tumor size
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4
Q

Bromocriptin

A
  • dopamine AGONIST
  • used to treat hyperprolactinemia (inhibitory effect)
  • suppresses prolactin secretion and tumor size
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5
Q

Fulvesterant

A
  • ER ANTAGONIST

- treatment of breast cancers expressing ERs

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6
Q

Leuprolide

A
  • 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
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7
Q

Goserelin

A
  • 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
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8
Q

Nafarelin

A
  • 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
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9
Q

Cetrorelix

A
  • GnRH ANTAGONIST
  • blocks release of LH and FSH; no initial stim
  • delays ovulation for IVF (controlled stim)
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10
Q

Ganirelix

A
  • GnRH ANTAGONIST
  • blocks release of LH and FSH; no initial stim
  • controlled ovarian hyperstim for IVF
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11
Q

Finasteride

A
  • 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
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12
Q

Dutasteride

A
  • 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
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13
Q

Anastrozole

A
  • 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
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14
Q

Letrozole

A
  • 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
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15
Q

Exemestane

A
  • 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
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16
Q

Formestane

A
  • 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
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17
Q

Tamoxifen

A
  • 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)
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18
Q

Raloxifene

A
  • 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
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19
Q

Clomiphene

A
  • 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
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20
Q

Flutamide

A
  • competitive AR ANTAGONIST
  • blocks action of T and DHT
  • used to treat prostate cancer
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21
Q

Enzalutamide

A
  • competitive AR ANTAGONIST
  • blocks action of T and DHT
  • used to treat prostate cancer
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22
Q

Bicalutamide

A
  • competitive AR ANTAGONIST
  • blocks action of T and DHT
  • used to treat prostate cancer
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23
Q

Drospirenone

A
  • competitive AR ANTAGONIST
  • also progestational effects
  • used as progestin in some combination contraceptives
24
Q

Mifepristone

A
  • 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
25
Q

Misoprostol

A
  • synthetic prostaglandin E1 analogue
  • stims uterine contractions
  • given with mifepristone to induce abortion (1st T)
  • adverse: nausea and vomiting
26
Q

Ethinyl Estradiol

A
  • used as estrogen in combo BC
27
Q

Mestranol

A
  • used as estrogen in combo BC
28
Q

Norgestrel

A
  • progestin in combo BC

- highest androgenic activity (1 of 2)

29
Q

Levonorgestrel

A
  • progestin in combo BC

- highest androgenic activity (1 of 2)

30
Q

Norethidrone

A
  • progestin in combo BC

- lower androgenic activity (1 of 2)

31
Q

Norethidrone acetate

A
  • progestin in combo BC

- lower androgenic activity (1 of 2)

32
Q

Etonogestrel

A
  • progestin in combo BC
  • 3rd gen
  • even lower AR cross-reactivity (1 of 5)
33
Q

Ethynodiol

A
  • progestin in combo BC
  • 3rd gen
  • even lower AR cross-reactivity
34
Q

Norgestimate

A
  • progestin in combo BC
  • 3rd gen
  • even lower AR cross-reactivity
35
Q

Gestodene

A
  • progestin in combo BC
  • 3rd gen
  • even lower AR cross-reactivity
36
Q

Desogestrel

A
  • progestin in combo BC
  • 3rd gen
  • even lower AR cross-reactivity
37
Q

Vaginal Ring

A
  • Ethinyl Estradiol and etonogestrel (3rd gen progestin)
38
Q

Transdermal Patches

A
  • Ethinyl Estradiol and norelgestromin
39
Q

Oral Tablets 84 days on, 7 days off

A
  • Ethinyl Estradiol and levonorgestrel (high androgenic activity)
40
Q

Quadphasic Formulations

A
  • Dinogest/Estradiol
41
Q

Mini-Pill

A
  • Norgestrel (high AR cross reactivity), Norethindrone (lower androgenic activity)
42
Q

Injectable- Progestin only

A
  • Medroxyprogesterone Acetate
43
Q

Implant - Progestin only

A
  • Etonogestrel (3rd gen progestin)
44
Q

IUD

A
  • levonogestrel (high androgenic cross-reactivity, but low amts gets into circulation)
45
Q

Emergency Contraceptive

A
  • Oral Levonogestrel (high cross reactivity)
46
Q

Male Contraceptives (from trials)

A
  • Testosterone enanthate
  • Testosterone enanthate + oral levonorgestrel (high AR cross reactivity)
  • Testosterone undecanoate + medroxyprogesterone acetate
  • combinations more effective and more reversible
47
Q

Hormone replacement Men: IM

A
  • testosterone enanthate

- testosterone cyprionate

48
Q

Sildenafil

A
  • 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
49
Q

Vardenafil

A
  • 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
50
Q

Tadalafil

A
  • 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
51
Q

Premarin

A
  • vaginal estrogen cream (1 of 3)

- used to treat female sexual dysfunction

52
Q

Estrace

A
  • vaginal estrogen cream (1 of 3)

- used to treat female sexual dysfunction

53
Q

Ogen

A
  • vaginal estrogen cream (1 of 3)

- used to treat female sexual dysfunction

54
Q

Estring

A
  • Vaginal estrogen ring

- used to treat female sexual dysfunction

55
Q

Flibanserin

A
  • “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
56
Q

Androstenedione

A
  • adrenal androgen precursor abused in steroid use
57
Q

Dehydroepiandrosterone

A
  • DHEA

- abused in steroid use

Pharmacology III (18 decks)

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