Repro drugs Flashcards

1
Q

Leuprolide MOA

A

GnRH analog
Pulsatile = agonist action
Continuous = antagonist action

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2
Q

Pulsatile leuprolide for:

A

infertility

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3
Q

continuous leuprolide for:

A

prostate cancer, fibroids, precocious puberty

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4
Q

Leuprolide AE

A

Anti-androgens (if continuous), N/V

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5
Q

Synthetic estrogens:

A

ethinyl estradiol, DES, mestranol

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6
Q

estrogen use in men:

A

androgen-sensitive prostate cancer

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7
Q

estrogen toxicity:

A

Endometrial cancer, post-meno bleeding, thrombi, clear cells adenocarcinoma in vagina of kids whose moms took DES. Contraindicated in ER+ breast cancer, or DVT Hx

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8
Q

Clomipine MOA

A

SERM; hypothalamic estrogen receptor antagonist; so prevents feedback inhibition, so increases LH and FSH

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9
Q

Clomiphene use

A

induce ovulation (via LH and FSH surge) in anovulatory states (i.e PCOS)

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10
Q

Clomiphene AE

A

VISUAL DISTURBANCES, hot flashes, ovarian enlargement, multiple simultaneous pregnancies

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11
Q

Tamoxifen use/MOA

A

agonist: uterus and bone
antagonist: breast
use: ER+ treat and prevent recurrence of ER+ /PR+ great cancer

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12
Q

Tamoxifen AE

A

endometrial cancer and thromboembolisms

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13
Q

Raloxifen use/MOA

A

agonist: bone
antagonist: breast and uterus
use: osteoporosis (ER+ prevention)

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14
Q

Raloxifen AE

A

thromboembolisms

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15
Q

HRT use

A

relief of menopausal symptoms (hot flashes, vaginal atrophy), osteoporosis

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16
Q

HRT AE

A

endometrial cancer (add progesterone to decrease risk). Maybe increase CV risk

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17
Q

Anastrazole/exemestane MOA/use

A

aromatase inhibitor (decrease E). Used in post-menopausal ER+ breast CA

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18
Q

Progestins MOA and use

A
MOA = decrease growth and vascularization of endometrium.
Use = OCP, rx of endometrial CA, rx of abnormal uterine bleeding
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19
Q

Mifepristone (RU-486) MOA

A

COMPETITIVE progestin-R inhibitor

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20
Q

Mifepristone (RU-486) use

A

abortions (progesterone keeps pregnancy going, so now you are blocking progesterones receptor)

21
Q

Mifepristone (RU-486) co-drug

A

misoprostol (PGE1) - PG sensitize endometrium to the drug

22
Q

Mifepristone (RU-486) AE

A

heavy bleeding, N/V/anorexia, abdominal pain

23
Q

Combined OCPs: components

A

estrogen + progestins

24
Q

Combined OCPs MOA

A

E and P in pill feedback to inhibit LH and FSH. no LH/FSH = no E surge = no LH surge = no ovulation.

Progestins also thicken cervical mucus and inhibit endometrial proliferation

25
Combined OCPs contraindications
SMOKERS >35, TE/stroke Hx, ER+ tumour hx
26
Terbutaline
b2 agonist to relax uterus; used to stop contractions frequency in labour
27
Ritodrine
b2 agonist to relax uterus; used to stop contractions frequency in labour
28
Danazol MOA
partial agonist at androgen-Rs (synthetic androgen)
29
Danazol use
endometriosis, HEREDITARY ANGIOEDEMA
30
Danazol toxicity
weight gain, edema, hirsutism, masculinization, acne, lowers HCL, hepatotoxicity
31
Testosterone/methyltestosterone use
hypogonadism, promotes 2' sex characteristiics, ANABOLISM post-burn or injury
32
Testosterone/methyltestosterone toxicity
masculinize females. testicular atrophy. premature EPIPHYSEAL PLATE CLOSURE. increase LDLs and decrease HDLs
33
Finasteride MOA
5a-reductase inhibitor
34
Finasteride use
male-pattern baldness and BPH (can actually decrease side of prostate)
35
Flutamide MOA
NON-steroidal competitive inhibitor @ androgen-Rs
36
Flutamide use
prostate CA
37
Ketoconazole MOA
inhibits 17,20-desmolase; stops steroid synthesis
38
Spironolactone MOA
inhibits 17,20-desmolase and 17-a-hydroxylase; stops steroid synthesis
39
Ketoconazole use
PCOS to reduce androgenic symptoms
40
Ketoconazole AE
Gynecomastia and amenorrhea
41
Spironolactone use
PCOS to reduce androgenic symptoms
42
Spironolactone AE
Gynecomastia and amenorrhea
43
Tamsulosin MOA and use
a1-A and a1-D selective a1-antagonists, found specifically on the prostate. inhibit smooth muscle contraction to relieve PBH symptoms (does NOT decrease prostate size like finasteride)
44
PDE-5 inhibitors:
sildenafil, vardenafil, tadalafil
45
sildenafil, vardenafil, tadalafil MOA
PDE-5 inhibitors = increased cGMP = VD corpus cavernosum = bonerrrr
46
sildenafil, vardenafil, tadalafil AE
headache, flushing, DYSPEPSIA, CYANOPSIA (see blue tint). Absolute contraindication with nitrates!!
47
Minoxidil
Direct arteriolar VD
48
Minoxidil use
androgneic alopecia, severe refractory HTN