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1
Q

Leuprolide

  • MOA
  • Use
  • Toxicity
A 
MOA: GnRH analog
- pulsatile = agonist
- continuous = antagonist -- downregulate GnRH receptor in pituitary 
  --> continuous: initial increase in T + DHT + estrogen followed by decrease, "start up flare" 
Use:
- infertility (pulsatile)
- Endometriosis 
- prostate cancer w/ flutamide (continuous) 
- uterine fibroids (continuous)
- precocious puberty (continuous)
Toxicity
- antiandrogen
- nausea
- vomiting
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2
Q

Testosterone

  • MOA
  • Use
  • Toxicity
A

MOA: agonist at androgen receptors
Use:
- hypogonadism
- promote secondary sex characteristic development
- stimulate anabolism for recovery in burn or injury
Toxicity:
- masculinization in females
- reduces intratesticular testosterone in males causing gonad atrophy (inhibits release of LH via negative feedback)
- Premature closure of epiphyseal plates
- increase LDH, decrease HDL

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3
Q

Methyltestosterone

  • MOA
  • Use
  • Toxicity
A

MOA: agonist at androgen receptors
Use:
- hypogonadism
- promote secondary sex characteristic development
- stimulate anabolism for recovery in burn or injury
Toxicity:
- masculinization in females
- reduces intratesticular testosterone in males causing gonad atrophy (inhibits release of LH via negative feedback)
- Premature closure of epiphyseal plates
- increase LDH, decrease HDL

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4
Q

Finesteride

  • MOA
  • Use
  • Toxicity
A 
Antiandrogen
MOA: 
- 5-alpha reductase inhibitor
- no conversion of T --> DHT
Use:
- BPH (takes months for gland to decrease in size and symptoms to improve)
- male pattern baldness 
Toxicity
- gynecomastia
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5
Q

Flutamide

  • MOA
  • Use
A 
Antiandrogen
MOA: 
- nonsteroidal competitive inhibitor of androgens at the testosterone receptor 
Use:
- prostate cancer
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6
Q

Ketaconazole

  • MOA
  • Use
  • Toxicity
A 
Antiandrogen
MOA: 
- inhibits steroid synthesis (inhibits 17,20 desmolase)
Use:
- PCOS - prevent hirsutism
Toxicity
- gynecomastia 
- amenorrhea
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7
Q

Spironolactone

  • MOA
  • Use
  • Toxicity
A 
Antiandrogen / K+ sparing diuretic 
MOA:
- inhibits steroid binding to androgen receptor 
Use:
- PCOS - prevent hirsutism
Toxicity
- gynecomastia
- amenorrhea
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8
Q

Ethinyl estradiol

  • MOA
  • Use
  • Toxicity
A 
Estrogen
MOA: bind estrogen receptor
Use:
- hypogonadism
- ovarian failure
- menstrual abnormalities
- HRT postmenopause 
- PCOS - decrease LH levels 
- Men = androgen dependent prostate cancer 
Toxicity:
- risk of endometrial cancer
- bleeding in postmenopausal women
- thrombi
Contraindications
- estrogen positive breast cancer
- DVT history
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9
Q

Magnesium Sulfate

  • MOA
  • Use
  • Toxicity
A

MOA: block membrane + intracellular calcium channel
Use:
- preeclampsia
- decreases risk of cerebral palsy in infant

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10
Q

DES

  • MOA
  • Use
  • Toxicity
A 
Estrogen
MOA: bind estrogen receptor
Use:
- hypogonadism
- ovarian failure
- menstrual abnormalities
- HRT postmenopause 
- PCOS - decrease LH levels 
- Men = androgen dependent prostate cancer 
Toxicity:
- risk of endometrial cancer
- bleeding in postmenopausal women
- Exposed in utero: clear cell adenocarcinoma of the vagina 
- thrombi
Contraindications
- estrogen positive breast cancer
- DVT history
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11
Q

Mestranol

  • MOA
  • Use
  • Toxicity
A 
Estrogen
MOA: bind estrogen receptor
Use:
- hypogonadism
- ovarian failure
- menstrual abnormalities
- HRT postmenopause 
- PCOS - decrease LH level 
- Men = androgen dependent prostate cancer 
Toxicity:
- risk of endometrial cancer
- bleeding in postmenopausal women
- thrombi
Contraindications
- estrogen positive breast cancer
- DVT history
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12
Q

Clomiphene

  • MOA
  • Use
  • Toxicity
A 
SERM
MOA: partial agonist at estrogen receptors in hypothalamus*
- prevents normal feedback inhibition 
- increases release of LH + FSH
- stimulates ovulation 
Use:
- infertility 
- PCOS - lets you get pregnant 
Toxicity:
- hot flashes
- ovarian enlargement
- multiple simultaneous pregnancies
- visual problems
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13
Q

Tamoxifen

  • MOA
  • Use
  • Toxicity
A 
SERM
MOA:
- antagonist on breast tissue 
- agonist in bone
- agonist in endometrium
Use:
- treat + prevent recurrence of ER(+) breast cancer
Toxicity
- endometrial cancer risk
- hot flashes
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14
Q

Raloxifene

  • MOA
  • Use
  • Toxicity
A 
SERM
MOA:
- agonist on bone
- endometrial + breast antagonist
Use
- osteoporosis
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15
Q

Hormone replacement therapy

A

Use
- menopausal symptoms (hot flashes, vag atrophy)
- osteoporosis (increased estrogen, decreased osteoclast activity)
Toxicity
- unopposed = increased risk of endometrial cancer
—-> add progesterone
- CV risk

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16
Q

Anastrozole

  • MOA
  • Use
  • Toxicity
A

MOA: aromatase inhibitors
- no estrogen synthesis from androgenic substrate
Use:
- postmenopausal women with breast cancer

17
Q

Exemestane

  • MOA
  • Use
  • Toxicity
A

MOA: aromatase inhibitors
- no estrogen synthesis from androgenic substrate
Use:
- postmenopausal women with breast cancer

18
Q

Progestins

  • MOA
  • Use
A 
MOA: bind progesterone receptors
- reduce growth of endometrium
- increase vascularization of endometrium
Use: 
- oral contraceptives
- treat endometrial cancer
- abnormal uterine bleeding
19
Q

Mifepristone (RU-486)

  • MOA
  • Use
  • Toxicity
A 
MOA: competitive inhibitor of progestins at progesterone receptor
Use:
- terminate pregnancy
- give with misoprostol* (PGE1)
Toxicity
- heavy bleed
- GI (n,v,anorexia)
- abdominal pain
20
Q

Oral Contraceptives

  • componentes
  • MOA
  • Contraindications
A
  • Synthetic progestins + estrogen
    MOA:
  • both: inhibit LH/ FSH –> no estrogen surge –> no LH surge (low gonadotropins) –> no ovulation
  • Progestin: thickening of cervical mucus (limiting access of sperm to uterus), inhibit endometrial proliferation (less suitable for implantation)
  • may prevent ovarian and endometrial cancer
    Contraindications
  • smokers > 35 yoa
  • hx of thromoembolism and stroke
  • hx of estrogen dependent tumors
21
Q

Terbutaline

  • MOA
  • Use
A

MOA: B2 agonist that relaxes uterus
Use:
- reduce premature uterine contractions

22
Q

Tamsulosin

  • MOA
  • Use
  • Toxicity
A

MOA: a1 antagonist
Use:
- BPH symptom relief
– relax smooth muscle in bladder neck, prostate capsule, prostate urethra
– selective for alpha1A,D receptor on prostate
Toxicity
- Orthostatic hypotension

23
Q

Sildenafil

  • MOA
  • Use
  • Toxicity
A 
MOA: inhibit phosphodiesterase 5
-  increase cGMP (inhibit phosphodiesterase- no cGMP breakdown) = decrease intracellular Ca+ = myosin dephosphorylation 
- smooth muscle relaxation in corpus cavernosum*
- increase blood flow
- erection
Use: erectile dysfunction
Toxicity
- headache
- flushing
- dyspepsia
- impaired blue green color vision
- life threatening hypotension if taking nitrates
24
Q

Vardenafil

  • MOA
  • Use
  • Toxicity
A 
MOA: inhibit phosphodiesterase 5
-  increase cGMP (inhibit phosphodiesterase- no cGMP breakdown) = decrease intracellular Ca+ = myosin dephosphorylation 
- smooth muscle relaxation in corpus cavernosum
- increase blood flow
- erection
Use: erectile dysfunction
Toxicity
- headache
- flushing
- dyspepsia
- impaired blue green color vision
- life threatening hypotension if taking nitrates
25
Q

Danazol

  • MOA
  • Use
  • Toxicity
A 
MOA: synthetic androgen 
- partial agonist at androgen receptors
Use: 
- endometriosis
- hereditary angioedema
Toxicity
- weight gain
- edema
- acne
- hirsutism
- masculinization
- decreased HDL 
- hepatotoxicity

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