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STEP 1 > Repro Drugs > Flashcards

Repro Drugs Flashcards

1
Q

Mechanism of leuprolide

A

GnRH analog with agonist properties when used in pulsatile fashion

antagonist when used in continuous fashion (downregulates GnRH receptor in pituitary –> decreased FSH/LH)

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2
Q

Pulsatile use of leuprolide

A

infertility

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3
Q

Continuous use of leuprolide

A

prostate cancer (following androgen receptor blockade with flutamide)
uterine fibroids
precocious puberty

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4
Q

Toxicity of leuprolide

A

antiandrogen, nausea, vomiting

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5
Q

Name the estrogens

A

ethinyl estradiol, DES, mestranol

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6
Q

Mechanism of estrogens

A

bind estrogen receptors

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7
Q

Use of estrogens in females

A

hypogonadism or ovarian failure, menstrual abnormalities, hormone replacement therapy in postmenopausal women

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8
Q

Use of estrogens in males

A

androgen-dependent prostate cancer

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9
Q

Toxicity of estrogens

A

increase risk of endometrial cancer
bleeding in postmenopausal women
clear cell adenomcarcinoma of the vagina (in women exposed to DES in utero)
increased risk of thrombi

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10
Q

Contraindications to estrogen use

A

ER+ breast cancer

history of DVTs

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11
Q

Name the selective estrogen receptor modulators

A

clomiphene, tamoxifen, raloxifene

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12
Q

Mechanism of clomiphene

A

antagonist at estrogen receptors in the hypothalamus

prevents normal feedback inhibition and increases release of LH and FSH from pituitary to stimulate ovulation

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13
Q

Use of clomiphene

A

infertility due to anovulation (PCOS)

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14
Q

Toxicity of clomiphene

A

hot flashes
ovarian enlargement
multiple simultaneous pregnancies
visual disturbances

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15
Q

Mechanism of tamoxifen

A

antagonist at breast

agonist at bone, uterus

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16
Q

Use of tamoxifen

A

to treat and prevent recurrence of ER/PR+ breast cancers

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17
Q

Toxicity of tamoxifen

A

increased risk of thromboembolic events

increased risk of endometrial cancer

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18
Q

Mechanism of raloxifene

A

antagonist at breast, uterus

agonist at bone

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19
Q

Use of raloxifene

A

to treat osteoporosis

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20
Q

Toxicity of raloxifene

A

increased risk of thromboembolic events only

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21
Q

Use of hormone replacement therapy

A

to relieve or prevent menopause symptoms (hot flashes, vaginal atrophy)
to treat osteoporosis (increase estrogen, decrease osteoclast activity)

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22
Q

Toxicity of hormone replacement therapy

A

unopposed estrogen replacement therapy –> increased risk of:

  • endometrial cancer (so add progesterone)
  • cardiovascular risk (possibly)
23
Q

Mechanism and use of anastrozole/exemestane

A

aromatase inhibitors used in postmenopausal women with ER+ breast cancer

24
Q

Mechanism of progestins

A

bind progesterone receptors and decrease growth and vascularization of the endometrium

25
Q

Use of progestins

A

oral contraceptives
treatment of endometrial cancer
abnormal uterine bleeding

26
Q

Mechanism of mifepristone

A

competitive inhibitor of progestins at progesterone receptors

27
Q

Use of mifepristone

A

termination of pregnancy (administered with misopristol (PGE1)

28
Q

Toxicity of mifepristone

A 
heavy bleeding
GI effects (nausea, vomiting, anorexia)
abdominal pain
29
Q

Mechanism of oral contraception (progestins and estrogen)

A

estrogen and progestins inhibit LH/FSH and thus prevent the estrogen surge
no estrogen surge prevents an LH surge and thus no ovulation occurs

30
Q

Mechanism of progestins in OCP

A

thicken cervical mucus

inhibit endometrial proliferation (less suitable for implantation)

31
Q

Contraindications for OCP use

A

smokers >35 years old (increase CVD risk)
patients with history of thromboembolism and stroke
history of estrogen-dependent tumor

32
Q

Mechanism and use of terbutaline and ritodrine

A

beta2-agonist that relax uterus

used to decrease contraction frequency in women during labor (prolong labor)

33
Q

Mechanism of danazol

A

synthetic androgen that acts as partial agonist at androgen receptors

34
Q

Use of danazol

A

endometriosis

hereditary angioedema

35
Q

Toxicity of danazol

A 
weight gain
edema
acne
hirsutism
masculinization
decrease HDL levels
hepatotoxicity
36
Q

Mechanism of testosterone, methyltestosterone

A

agonists at androgen receptors

37
Q

Use of testosterones

A

treat hypogonadism
promote development of secondary sex characteristics
stimulate anabolism to recovery after burn or injury

38
Q

Toxicity of testosterones

A

masculinization in females
decreased intratesticular testosterone in males by inhibiting release of LH (via negative feedback) –> gonadal atrophy
premature closure of epiphyseal plates
increased LDL and decreased HDL

39
Q

Antiandrogens

A

finasteride, flutamide, ketoconazole, sprionolactone

testosterone –> DHT via 5-alpha reductase

40
Q

Mechanism of finasteride

A

5alpha-reductase inhibitor (decreases conversion of testosterone to DHT)

41
Q

Use of finasteride

A

BPH to decrease size and male pattern baldness

42
Q

Mechanism of flutamide

A

nonsteroidal competitive inhibitor at androgen receptors

43
Q

Use of flutamide

A

prostate carcinoma

44
Q

Mechanism of ketoconazole

A

inhibits steroid synthesis (inhibits 17,20 desmolase)

45
Q

Mechanims of spironolactone

A

inhibits steroid binding, 17alpha-hydroxylase, and 17,20 desmolase

46
Q

Use of ketoconazole and spironolactone

A

to treat PCOS to reduce androgenic symptoms

47
Q

Side effects of ketoconazole and sprinonolactone

A

gynecomastia and amenorrhea

48
Q

Mechanism and use of tamulosin

A

alpha1-antagonist used to treat BPH by inhibiting smooth muscle contraction
selective for alpha1A,D receptors (found on prostate) vs. vascular alpha1B receptors

49
Q

Mechanism of sildenafil, vardenafil, tadalafil

A

inhibit PDE5 –> increased cGMP and smooth muscle relaxation in corpus cavernosum –> increased blood flow and penile erection

50
Q

Use of sildenafil, vardenafil, tadalafil

A

erectile dysfunction

51
Q

Toxicity of sildenafil, vardenafil, tadalafil

A

headache, flushing, dyspepsia, cyanopsia (blue-tinted vision)

risk of life-treatening hypotension in patients taking nitrates

52
Q

Mechanism of minoxidil

A

direct arteriolar vasodilator

53
Q

Use of minoxidil

A

androgenetic alopecia

severe refractory hypertension

STEP 1 (26 decks)

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