Repro drugs Flashcards
Leuprolide MOA
GnRH analog
Pulsatile = agonist action
Continuous = antagonist action
Pulsatile leuprolide for:
infertility
continuous leuprolide for:
prostate cancer, fibroids, precocious puberty
Leuprolide AE
Anti-androgens (if continuous), N/V
Synthetic estrogens:
ethinyl estradiol, DES, mestranol
estrogen use in men:
androgen-sensitive prostate cancer
estrogen toxicity:
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
Clomipine MOA
SERM; hypothalamic estrogen receptor antagonist; so prevents feedback inhibition, so increases LH and FSH
Clomiphene use
induce ovulation (via LH and FSH surge) in anovulatory states (i.e PCOS)
Clomiphene AE
VISUAL DISTURBANCES, hot flashes, ovarian enlargement, multiple simultaneous pregnancies
Tamoxifen use/MOA
agonist: uterus and bone
antagonist: breast
use: ER+ treat and prevent recurrence of ER+ /PR+ great cancer
Tamoxifen AE
endometrial cancer and thromboembolisms
Raloxifen use/MOA
agonist: bone
antagonist: breast and uterus
use: osteoporosis (ER+ prevention)
Raloxifen AE
thromboembolisms
HRT use
relief of menopausal symptoms (hot flashes, vaginal atrophy), osteoporosis
HRT AE
endometrial cancer (add progesterone to decrease risk). Maybe increase CV risk
Anastrazole/exemestane MOA/use
aromatase inhibitor (decrease E). Used in post-menopausal ER+ breast CA
Progestins MOA and use
MOA = decrease growth and vascularization of endometrium. Use = OCP, rx of endometrial CA, rx of abnormal uterine bleeding
Mifepristone (RU-486) MOA
COMPETITIVE progestin-R inhibitor
Mifepristone (RU-486) use
abortions (progesterone keeps pregnancy going, so now you are blocking progesterones receptor)
Mifepristone (RU-486) co-drug
misoprostol (PGE1) - PG sensitize endometrium to the drug
Mifepristone (RU-486) AE
heavy bleeding, N/V/anorexia, abdominal pain
Combined OCPs: components
estrogen + progestins
Combined OCPs MOA
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
Combined OCPs contraindications
SMOKERS >35, TE/stroke Hx, ER+ tumour hx
Terbutaline
b2 agonist to relax uterus; used to stop contractions frequency in labour
Ritodrine
b2 agonist to relax uterus; used to stop contractions frequency in labour
Danazol MOA
partial agonist at androgen-Rs (synthetic androgen)
Danazol use
endometriosis, HEREDITARY ANGIOEDEMA
Danazol toxicity
weight gain, edema, hirsutism, masculinization, acne, lowers HCL, hepatotoxicity
Testosterone/methyltestosterone use
hypogonadism, promotes 2’ sex characteristiics, ANABOLISM post-burn or injury
Testosterone/methyltestosterone toxicity
masculinize females. testicular atrophy. premature EPIPHYSEAL PLATE CLOSURE. increase LDLs and decrease HDLs
Finasteride MOA
5a-reductase inhibitor
Finasteride use
male-pattern baldness and BPH (can actually decrease side of prostate)
Flutamide MOA
NON-steroidal competitive inhibitor @ androgen-Rs
Flutamide use
prostate CA
Ketoconazole MOA
inhibits 17,20-desmolase; stops steroid synthesis
Spironolactone MOA
inhibits 17,20-desmolase and 17-a-hydroxylase; stops steroid synthesis
Ketoconazole use
PCOS to reduce androgenic symptoms
Ketoconazole AE
Gynecomastia and amenorrhea
Spironolactone use
PCOS to reduce androgenic symptoms
Spironolactone AE
Gynecomastia and amenorrhea
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)
PDE-5 inhibitors:
sildenafil, vardenafil, tadalafil
sildenafil, vardenafil, tadalafil MOA
PDE-5 inhibitors = increased cGMP = VD corpus cavernosum = bonerrrr
sildenafil, vardenafil, tadalafil AE
headache, flushing, DYSPEPSIA, CYANOPSIA (see blue tint). Absolute contraindication with nitrates!!
Minoxidil
Direct arteriolar VD
Minoxidil use
androgneic alopecia, severe refractory HTN
