Repro Pharm Flashcards
MOA of leuprolide?
GnRH analog with agonist (pulsatile) and antagonist (continuous) properties
How does leuprolide work continuously?
Downregulates GnRH receptors in pituitary decreasing FSH/LH
Uses of leuprolide?
1) Pulsatile = infertility
2) Continuous = prostate cancer (with flutamide), uterine fibroids, precocious puberty
AEs of leuprolide?
Antiandrogen, N/V, hot flashes, mood lability, vaginal dryness (dyspareunia)
MOA of testosterone, methyltestosterone?
Agonist at androgen receptors
Uses of testosterone?
1) Hypogonadism
2) Promotes secondary sex characteristics
3) Stimulates anabolism for burns or injuries
AEs of testosterone?
Masculinization in females, reduces intratesticular testosterone in males causing gonadal atrophy and azoospermia, premature closure of epiphyseal plates
What does testosterone do to lipids?
Increases LDL, decreases HDL
What are the antiandrogens?
1) Finasteride
2) Flutamide
3) Ketoconazole
4) Spironolactone
MOA of finasteride?
5a-reductase inhibitor
MOA of flutamide?
Nonsteroidal competitive inhibitor of androgens at testosterone receptors
MOA of ketoconazole?
Inhibits steroid synthesis (inhibits 17,20-desmolase)
MOA of spironolactone?
Inhibits steroid binding
Uses for finasteride?
BPH, male pattern baldness
Uses for flutamide?
Prostate cancer
Uses for ketoconazole and spironolactone?
Prevent hirsutism in PCOS
AEs of antiandrogens?
Gynecomastia galactorrhea, sexual dysfunction
Uses for ethinyl estradiol, DES, mestranol?
1) Hypogonadism or ovarian failure
2) Menstrual irregularities
3) HRT in postmenopausal women
4) Androgen-dependent prostate cancer
AEs of estrogens?
Endometrial cancer, postmenopausal bleeding, clear cell adeno with DES, thrombosis
What are the contraindications of estrogens?
ER+ breast cancer, hx of DVTs
MOA of clomiphene?
Partial agonist at ERs in hypothalamus, prevents normal feedback inhibition and increases release of LH/FSH which stimulates ovulation
Uses of clomiphene?
Infertility in PCOS
AEs of clomiphene?
Hot flashes, ovarian enlargement, multiple simultaneous pregnancies, visual disturbance
MOA of tamoxifen?
Antagonist in breast, agonist in endometrium
Uses of tamoxifen?
Tx and prevent recurrence of ER+ breast cancer
MOA of raloxifene?
Agonist in bone reducing bone resorption–used in osteoporosis
Uses for HRT?
1) Relief or prevention of menopausal sxs
2) Osteoporosis
AEs of HRT?
Increased risk of endometrial cancer (gotta add progesterone if they have a uterus), possible CV risk
Aromatase inhibitors?
Anastrozole, exemstane
Uses for aromatase inhibitors?
Postmenopausal women with breast cancer (adjuvant therapy, 2nd line)
MOA of progestins?
Reduces growth and increase vascularization of endometrium
Uses of progestins?
1) OCPs
2) Endometrial cancer
3) Abnormal uterine bleeding
MOA of mifepristone (RU-486)?
Competitive inhibitor of progestins at progesterone receptors
Uses of mifepristone?
Termination of pregnancy (with misoprostol)
AEs of mifepristone?
Heavy bleeding, GI, abdominal pain
MOA of OCPs?
1) Combo inhibits LH/FSH and thus prevents estrogen surge inhibiting ovulation
2) Progestins cause cervical mucus thickening and inhibits endometrial proliferation
Contraindications of OCPs?
Smokers >35, hx of TE and stroke, hx of estrogen-dependent tumor, hypertriglyceridiemia, liver dz
What do OCPs decrease the risk of?
1) Ovarian tumors
2) Endometrial tumors
Terbutaline?
B2-agonist that relaxes uterus to tx premature contractions
MOA of tamsuloson?
Alpha-1 blocker to tx BPH and HTN
Dinoprostone?
PGE2 agonist that causes cervical softening, dilation, stimulates contractions
Misoprostol?
PGE1 agonist that causes cervical softening, stimulates contractions, tx for postpartum hemorrhage or induced abortion
MOA of sildenafil and vardenafil?
Inhibits PDE5 causing increase in cGMP, SM relaxation in corpus cavernosum, increasing blood flow
AEs of PDE5 inhibitors?
HA, flushing, dyspepsia, impaired blue green vision, risk of life-threatening hypotension with nitrates
MOA of danazol?
Synthetic androgen that acts as a partial agonist at androgen receptors, suppresses LF/FSH and ovarian estrogen release (brings about a state of medical menopause)
Uses for danazol?
1) Endometriosis
2) Hereditary angioedema
AEs of danazol?
Weight gain, edema, acne, hirsutism, masculinization, decreased HDL, hepatotoxicity