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STEP 1 > Repro Drugs > Flashcards

Repro Drugs Flashcards

(53 cards)

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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

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A

unopposed estrogen replacement therapy –> increased risk of:

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

Mechanism and use of anastrozole/exemestane

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A

aromatase inhibitors used in postmenopausal women with ER+ breast cancer

24
Q

Mechanism of progestins

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A

bind progesterone receptors and decrease growth and vascularization of the endometrium

25
Use of progestins
oral contraceptives treatment of endometrial cancer abnormal uterine bleeding
26
Mechanism of mifepristone
competitive inhibitor of progestins at progesterone receptors
27
Use of mifepristone
termination of pregnancy (administered with misopristol (PGE1)
28
Toxicity of mifepristone
``` heavy bleeding GI effects (nausea, vomiting, anorexia) abdominal pain ```
29
Mechanism of oral contraception (progestins and estrogen)
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
Mechanism of progestins in OCP
thicken cervical mucus | inhibit endometrial proliferation (less suitable for implantation)
31
Contraindications for OCP use
smokers >35 years old (increase CVD risk) patients with history of thromboembolism and stroke history of estrogen-dependent tumor
32
Mechanism and use of terbutaline and ritodrine
beta2-agonist that relax uterus | used to decrease contraction frequency in women during labor (prolong labor)
33
Mechanism of danazol
synthetic androgen that acts as partial agonist at androgen receptors
34
Use of danazol
endometriosis | hereditary angioedema
35
Toxicity of danazol
``` weight gain edema acne hirsutism masculinization decrease HDL levels hepatotoxicity ```
36
Mechanism of testosterone, methyltestosterone
agonists at androgen receptors
37
Use of testosterones
treat hypogonadism promote development of secondary sex characteristics stimulate anabolism to recovery after burn or injury
38
Toxicity of testosterones
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
Antiandrogens
finasteride, flutamide, ketoconazole, sprionolactone testosterone --> DHT via 5-alpha reductase
40
Mechanism of finasteride
5alpha-reductase inhibitor (decreases conversion of testosterone to DHT)
41
Use of finasteride
BPH to decrease size and male pattern baldness
42
Mechanism of flutamide
nonsteroidal competitive inhibitor at androgen receptors
43
Use of flutamide
prostate carcinoma
44
Mechanism of ketoconazole
inhibits steroid synthesis (inhibits 17,20 desmolase)
45
Mechanims of spironolactone
inhibits steroid binding, 17alpha-hydroxylase, and 17,20 desmolase
46
Use of ketoconazole and spironolactone
to treat PCOS to reduce androgenic symptoms
47
Side effects of ketoconazole and sprinonolactone
gynecomastia and amenorrhea
48
Mechanism and use of tamulosin
alpha1-antagonist used to treat BPH by inhibiting smooth muscle contraction selective for alpha1A,D receptors (found on prostate) vs. vascular alpha1B receptors
49
Mechanism of sildenafil, vardenafil, tadalafil
inhibit PDE5 --> increased cGMP and smooth muscle relaxation in corpus cavernosum --> increased blood flow and penile erection
50
Use of sildenafil, vardenafil, tadalafil
erectile dysfunction
51
Toxicity of sildenafil, vardenafil, tadalafil
headache, flushing, dyspepsia, cyanopsia (blue-tinted vision) risk of life-treatening hypotension in patients taking nitrates
52
Mechanism of minoxidil
direct arteriolar vasodilator
53
Use of minoxidil
androgenetic alopecia | severe refractory hypertension

STEP 1 (26 decks)

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