Pharmacology-Reproductive Flashcards

1
Q

Leuprolide: mechanism and action when pulsatile

A

GnRH analog, agonist when pulsatile

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2
Q

Leuprolide: mechanism and action when continuous

A

GnRH analog, antagonist when continuous (downregulates GnRH receptor in pituitary leading to decreased FSH and LH)

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3
Q

Leuprolide: use (pulsatile)

A

infirtility

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4
Q

Leuprolide: use (continuous)

A

uterine fibroids, precocious puberty, prostate cancer

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5
Q

what must be given with Leuprolide for the treatment of prostate cancer?

A

flutamide

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6
Q

Leuprolide: toxicity

A

Antiandrogen, nausea, vomiting

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7
Q

Testosterone, methyltestosterone: mechanism

A

agonist at androgen receptors

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8
Q

Testosterone, methyltestosterone: use

A
  • treat hypogonadism and promotes secondary sex characteristics
  • (+) anabolism to promote recovery after burn or injury!
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9
Q

Testosterone, methyltestosterone: toxicity

A
  • masculinization in females
  • reduces intratesticular testosterone in males by (-) Lh release
  • gonadal atrophy
  • premature closure of epiphyseal plates
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10
Q

Testosterone, methyltestosterone: effect on LDL, HDL

A
  • increased LDL and decreased HDL
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11
Q

Antiandrogens: names

A

finasteride, flutamide, ketoconazol, spironolactone

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12
Q

What enzyme converts testosterone to DHT

A

5alpha-reductase

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13
Q

Finasteride: mechanism

A

5alpha reductase inhibitor

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14
Q

Finasteride: use

A
  • BPH
  • promotes hair growth (male pattern baldness)
  • (can encourage female breast growth)
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15
Q

Flutamide: mechanism

A

non-steroidal competitive inhibitor of androgens at Test. receptor

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16
Q

Flutamide: use

A

prostate carcinoma

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17
Q

Ketoconazole: mechanism

A

inhibit steroid synthesis

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18
Q

Ketoconazol: what specific enzyme does it inhibit

A

17-20 desmolase

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19
Q

Spironolactone: mechanism

A

inhibits steroid binding

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20
Q

Ketoconazol and Spironolactone: use

A

treatment of polycystic ovarian syndrome to prevent hirsutism

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21
Q

Ketoconazol and spironolactone: side effects

A

gynecomastia, amenorrhea

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22
Q

Estrogens: names

A

ethinyl estradoil, DES, mestranol

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23
Q

Estrogens: mechanism

A

bind to estrogen receptors

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24
Q

Estrogens: use

A

hypogonadism or ovarian failure
menstrual abnormalities
HRT in postmenopausal women

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25
Q

Estrogen use in men with what?

A

androgen-dependent prostate cancer

26
Q

Estrogen: toxicity

A
  • bleeding in post-menopausal women

- increased risk of thrombi

27
Q

Estrogen: increased risk of what cancers

A
  • endometrial cancer

- clear cell adenoma of vagina in females exposed to DES in utero

28
Q

Estrogen: contraindications

A
  • ER(+) breast cancer

- history of deep vein thrombosis

29
Q

Selective estrogen receptor modulators (SERMS) names:

A

Clomiphene, Tamoxifen, Raloxifen

30
Q

Clomiphene: mechanism + use

A
  • partial agonist at estrogen receptors in hypothal

- prevents normal feedback inhibition, increases release of LH and FSH (+) ovulation

31
Q

Clomiphene: uses

A

infertility and polycystic ovarian syndrome

32
Q

Clomiphene: side effects

A

hot flashes, ovarian enlargement, multiple pregnancies, visual disturbances

33
Q

Tamoxifen: mechanism

A

estrogen receptor antagonist on breast tissue

34
Q

Tamoxifen: use

A

treat and prevent recurrence of ER(+)breast cancer

35
Q

Raloxifene: mechanism

A

esterogen receptor agonist on bone

36
Q

Raloxifene: use

A

reduce resorption of bone so treat osteoporosis

37
Q

HRT: use

A
  • relief or prevention of menopausal symptoms + osteoporosis
38
Q

Why must add progesterone to HRT?

A

unopposed ERT increases risk of endometrial cancer, so use progesterone too but will increase risk of CV accident

39
Q

Anastrozole/exemestane: mechanism

A

aromatase inhibitor

40
Q

Anastrozole/exemestane: use

A

postmenopausal women with breast cancer

41
Q

Progestins: mechanism

A

bind progesterone receptors, reduce growth and increase vascularization of endometrium

42
Q

Progestins: use

A
  • oral contraceptives
  • endometrial cancer
  • abnormal uterine bleeding
43
Q

Mifepristone: what is code?

A

RU-486

44
Q

Mifepristone: mechanism

A

competitive inhibitor of progestins @ progesterone receptors

45
Q

Mifepristone: use

A
  • termination of pregnancy
46
Q

What do you admin w/ Mifepristone?

A

Misoprostol (PGE1)

47
Q

Mifepristone: toxicity

A

Heavy bleeding, GI effects (nausea, vomiting, anorexia), abdominal pain

48
Q

Oral Contraception (synth progestins + estrogens): mechanism

A
  • (-) LH/FSH surge -> (-) estrogen surge -> no LH surge -> no ovulation
49
Q

Action of Progestins:

A

thicken cervical mucus, inhibit endometrial prolif

50
Q

Oral Contraception: contraindications:

A

Smokers over 35 (increased risk of cardiovasc events)

Patients w/ history of thrombi, stroke, or estrogen-dependent tumor

51
Q

Terbutaline: mechanism

A

B2 agonist that relaxes uterus

52
Q

Terbutaline: use

A

reduces premature uterine contractions

53
Q

Tamsulosin: mechanism

A

a1 antagonist (a1A,D selective), inhibiting smooth muscle contraction

54
Q

Tamsulosin: use

A

treat BPH

55
Q

Sildenafil, vardenafil: mechanism/use

A

(-) phosphodiesterase 5, causing increased in cGMP, smooth muscle relaxation in corpus cavernosum, increasing blood flow, leading to penile erection

56
Q

Sildenafil, vardenafil: toxicity

A

headache, flushing, dyspepsia, impaired blue-green coloured vision

57
Q

Sildenafil, vardenafil: what occurs in patients on nitrates?

A

life-threatening hypotension

58
Q

Danazol: mechanism

A

synthetic androgens, act as partial agonist at androgen receptors

59
Q

Danazol: use

A

endometriosis

hereditary angioedema

60
Q

Danazol: toxicity

A

weight gain, edema, acne, hirsutism, masculinization, hepatotoxicity

61
Q

Danazol: what effects on HDL?

A

decrease