Repro_Pharm Flashcards

1
Q

Leuprolide- MOA?

A

GnRH analog w/ agonist properties when used in pulsatile fashion
- antagonist properties when used in continuous fashion (downregulates GnRH receptor in pituitary –> dec’d FSH/LH)

“LEUprolide can be used in LIEU of GnRH”

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2
Q

Leuprolide- Clinical uses?

A
  • Infertility (pulsatile)
  • Prostate cancer (continuous w/ Flutamide)
  • Uterine fibroids (continuous)
  • Precocious puberty (continuous)
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3
Q

Leuprolide- Toxicity?

A
  • Anti-androgen
  • Nausea
  • Vomiting
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4
Q

Testosterone- MOA?

A

Agonist @ androgen receptors

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5
Q

Testosterone- Clinical uses?

A
  • Treats hypogonadism & promotes development of secondary sex characteristics
  • Stimulation of anabolism to promote recovery after burn or injury
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6
Q

Testosterone- Toxicity?

A
  • Causes masculinization in females
  • Reduces intratesticular testosterone in males by inhibiting release of LH (via negative feedback), leading to gonadal atrophy
  • Premature closure of epiphyseal plates
  • Inc’d LDL, dec’d HDL
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7
Q

Methyltestosterone- MOA?

A

Agonist @ androgen receptors

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8
Q

Methyltestosterone- Clinical uses?

A
  • Treats hypogonadism & promotes development of secondary sex characteristics
  • Stimulation of anabolism to promote recovery after burn or injury
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9
Q

Methyltestosterone- Toxicity?

A
  • Causes masculinization in females
  • Reduces intratesticular testosterone in males by inhibiting release of LH (via negative feedback), leading to gonadal atrophy
  • Premature closure of epiphyseal plates
  • Inc’d LDL, dec’d HDL
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10
Q

5-alpha-reductase: function?

A

Converts Testosterone –> DHT (more potent)

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11
Q

Finasteride- MOA?

A

5-alpha-reductase inhibitor (dec’d conversion of Testosterone to DHT)

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12
Q

Finasteride- Clinical uses?

A
  • BPH
  • Promotes hair growth – used to treat male-pattern baldness

(to prevent male-pattern baldness, give a drug that will encourage female breast growth)

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13
Q

Flutamide- MOA?

A

A non-steroidal competitive inhibitor of androgens @ the Testosterone receptor

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14
Q

Flutamide- Clinical uses?

A

Prostate Carcinoma

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15
Q

Ketoconazole- MOA?

A

Inhibits steroid synthesis (inhibitrs 17,20-desmolase)

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16
Q

Ketoconazole- Clinical uses?

A

Polycystic Ovarian Syndrome (to prevent hirsutism)

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17
Q

Ketoconazole- Side effects?

A

Gynecomastia & amenorrhea

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18
Q

Spironolactone- MOA?

A

Inhibits steroid binding

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19
Q

Spironolactone- Clinical uses?

A

Polycystic Ovarian Syndrome (to prevent hirsutism)

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20
Q

Spironolactone- Side effects?

A

Gynecomastia & amenorrhea

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21
Q

Ethinyl Estradiol- MOA?

A

(Estrogen)

Binds estrogen receptors

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22
Q

Ethinyl Estradiol- Clinical uses?

A

Women:

  • Hypogonadism or ovarian failure
  • Menstrual abnormalities
  • HRT in postmenopausal women

Men:
- Androgen-dependent prostate cancer

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23
Q

Ethinyl Estradiol- Toxicity?

A
  • Inc’d risk of endometrial cancer
  • Bleeding in postmenopausal women
  • Inc’d risk of thrombi
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24
Q

Ethinyl Estradiol- Contraindications?

A
  • ER-positive breast cancer

- History of DVTs

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25
Q

DES- MOA?

A

(Estrogen)

Binds estrogen receptors

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26
Q

DES- Clinical uses?

A

Women:

  • Hypogonadism or ovarian failure
  • Menstrual abnormalities
  • HRT in postmenopausal women

Men:
- Androgen-dependent prostate cancer

27
Q

DES- Toxicity?

A
  • Inc’d risk of endometrial cancer
  • Bleeding in postmenopausal women
  • Clear cell adenocarcinoma of vagina if exposed in-utero
  • Inc’d risk of thrombi
28
Q

DES- Contraindications?

A
  • ER-positive breast cancer

- History of DVTs

29
Q

Mestranol- MOA?

A

(Estrogen)

Binds estrogen receptors

30
Q

Mestranol- Clinical uses?

A

Women:

  • Hypogonadism or ovarian failure
  • Menstrual abnormalities
  • HRT in postmenopausal women

Men:
- Androgen-dependent prostate cancer

31
Q

Mestranol- Toxicity?

A
  • Inc’d risk of endometrial cancer
  • Bleeding in postmenopausal women
  • Inc’d risk of thrombi
32
Q

Mestranol- Contraindications?

A
  • ER-positive breast cancer

- History of DVTs

33
Q

Clomiphene- MOA?

A

Selective Estrogen Receptor Modulator (SERM)

  • Partial agonist @ estrogen receptors in hypothalamus
  • Prevents normal feedback inhibition & increases release of LH & FSH from pituitary, which stimulates ovulation
34
Q

Clomiphene- Clinical uses?

A
  • Infertility

- Polycystic Ovarian Syndrome

35
Q

Clomiphene- Adverse effects?

A
  • Hot flashes
  • Ovarian enlargement
  • Multiple, simultaneous pregnancies
  • Visual disturbances
36
Q

Tamoxifen- MOA?

A

Selective Estrogen Receptor Modulator (SERM)

  • Antagonist on breast tissue
37
Q

Tamoxifen- Clinical uses?

A

Used to treat & prevent recurrence of ER-positive breast cancer

38
Q

Raloxifene- MOA?

A

Selective Estrogen Receptor Modulator (SERM)

  • Agonist on bone, CV system, & blood lipoproteins (reduces resorption of bone)
  • Antagonist in breast & uterus
39
Q

Raloxifene- Clinical uses?

A

Used to treat Osteoporosis

also decreases risk of both breast & uterine cancer

40
Q

Hormone Replacement Therapy –

a) What is it used for?
b) What are its components?
c) Potential AEs?

A

a) Used for relief or prevention of menopausal symptoms (e.g. hot flashes, vaginal atrophy) & osteoporosis ( ↑estrogen, ↓osteoclast activity)
b) Unopposed estrogen replacement therapy (ERT) ↑the risk of endometrial cancer, so progesterone is added
c) Possible ↑CV risk

41
Q

Anastrozole - MOA?

A

Aromatase inhibitor

42
Q

Anastrozole - Clinical uses?

A

Used in postmenopausal women w/ breast cancer

43
Q

Exemestane - MOA?

A

Aromatase inhibitor

44
Q

Exemestane - Clinical uses?

A

Used in postmenopausal women w/ breast cancer

45
Q

Progestins - MOA?

A

Bind progesterone receptors, reduce growth & ↑ vascularization of endometrium

46
Q

Progestins - Clinical uses?

A
  • Oral contraceptives

- Tx of endometrial cancer & abnormal uterine bleeding

47
Q

Mifepristone (RU-486) - MOA?

A

Competitive inhibitor of progestins @ progesterone receptor

48
Q

Mifepristone - Clinical uses?

A

Termination of pregnancy

– Administered w/ Misoprostol (PGE1)

49
Q

Mifepristone - Toxicity?

A
  • Heavy bleeding
  • GI effects (nausea, vomiting, anorexia)
  • Abdominal pain
50
Q

Terbutaline - MOA?

A

B2-agonist that relaxes the uterus

51
Q

Terbutaline - Clinical uses?

A

Reduces premature uterine contractions

52
Q

Tamsulosin - MOA?

A

α-1 antagonist

- selective for α-1A,D receptors (found on prostate) & vascular α-1B receptors

53
Q

Tamsulosin- Clinical uses?

A

Used to treat BPH by inhibiting smooth muscle contraction

54
Q

Sildenafil - MOA?

A

Inhibits phosphodiesterase 5, causing ↑cGMP, smooth muscle relaxation in the corpus cavernous, ↑blood flow, & penile erection

55
Q

Sildenafil - Clinical uses?

A

Treatment of erectile dysfunction

56
Q

Vardenafil - MOA?

A

Inhibits phosphodiesterase 5, causing ↑cGMP, smooth muscle relaxation in the corpus cavernous, ↑blood flow, & penile erection

57
Q

Vardenafil - Clinical uses?

A

Treatment of erectile dysfunction

58
Q

Sildenafil - Toxicity?

A
  • Headache
  • Flushing
  • Dyspepsia
  • Impaired blue-green color vision
  • Risk of life-threatening hypotension in patients taking nitrates

” Hot & Sweaty,” but then Headache, Heartburn, & Hypotension

59
Q

Vardenafil - Toxicity?

A
  • Headache
  • Flushing
  • Dyspepsia
  • Impaired blue-green color vision
  • Risk of life-threatening hypotension in patients taking nitrates

” Hot & Sweaty,” but then Headache, Heartburn, & Hypotension

60
Q

Danazol - MOA?

A

Synthetic androgen that acts as a partial agonist @ androgen receptors

61
Q

Danazol - Clinical uses?

A

Endometriosis & hereditary angioedema

62
Q

Danazol - Toxicity?

A
  • Weight gain
  • Edema
  • Acne
  • Hirsutism
  • Masculinization
  • ↓HDL levels
  • Hepatotoxicity
63
Q

Medroxyprogesterone - Clinical uses?

A
  • Reduces the incidence of endometrial hyperplasia & the risk of endometrial carcinoma in postmenopausal women on estrogen replacement therapy
  • Also used parentally as long-acting contraceptive
64
Q

Medroxyprogesterone - AEs of prolonged use?

A

Decreased bone mineral density in women of all ages