Reproductive Flashcards
Leuprolide
MOA: GnRH analog with agonist properties when used in pulsatile fashion
Antagonistic when continuous (downregulates GnRH receptor)
Clinical: Infertililty (pulsatile)
Continuous: Prostate cancer (with flutamide), uterin fibroids, precroscious puberty
Toxicity: antiandrogen, nausea, vomiting
Tamoxifen
Selective estrogen receptor modulator
MOA: antagonist on breast tissue, agonist at uterus and bone (Increases bone mineral density), decreases LDL
Clinical: treat and prevent recurrence of estrogen responding breast cancer
Toxicity: endometrial cancer (endometrial polyps, hyperplasia)
Tamsulosin and terazosin
MOA: a1 antagonist
Clinical: prevents smooth muscle contraction in BPH, treats symptoms
SE: orthastatic hypotension, dizziness
Hormone replacement therapy
Used for relief or prevention of meonopausal symptoms (hot flashes, vaginal atrophy) and osteoporosis (increased estrogen, decreased osteoclast activity)
Toxicity: unopposed estrogen replacement therapy increases the risk of endometrial cancer so progesterone is added
Possible increased cardiovascular risk
Anastrozole/exemestane, letrozole
MOA: aromatase inhibitors
Clinical: breast cancer in postmenopausal women
Progestins
MOA: bind progestereon receptors, decreasing growth and increases vascularization of endometrium
Clinical: oral contraceptives and treatment of endometrial cancer and abnormal uterine bleeding
Menotropin
Acts like FSH leading to formation of dominant follicle
Raloxifene
Selective estrogen receptor modulator
MOA: agonist on bone, antagonist at uterus
Clinical: osteoporosis (decreases resorption of bone)
Toxicity: increase risk of thormoembolic events
Mifepristone (RU-486)
MOA: competitive inhibitor of progestins at progesterone receptors
Clinical: termination of pregnancy. Admistered with misoprostol
Toxicity: heavy bleeding, GI effects (nausea, vomiting, anorexia), abdominal pain
Synthetic progestins, estrogen
Oral contraception
Estrogen and progestins inhibit LH/FSH preventing estrogen surge (no ovulation)
Progestins: thickening of cervical mucus limiting access of sperm to uterus
Inhibit endometrial proliferation making endometrium less suitable for implantation
CI: smokers>35 y.o. (increased risk of CV events-DVT, pulmonary embolism, ischemic stroke), patients with thromobemolism and stoke, estrogen dependent tumor, hypertryglyceridemia, decompensated or active liver disease, pregnancy
SE: breakthrough menstrual bleeding, breast tenderness, weight gain
Estrogens
Ethinyl estradiol, DES, mestranol
MOA: bind estrogen receptors
Clinical: Hypogonadism or ovarian failure, menstrual abnormalities, HRT in postmenopausal women, men with androgen dependent prostate cancer
Toxicity: increase risk of endometrial cancer, bleeding in postmenopausal women, clear cell adenocarcinoma of vagina in females exposed to DES in utero, increased risk of thrombi
CI: Estrogen respoding breast cancer, history of DVTs
Terbutaline
B2 agonist that relaxes the uterus
Decreases contraction frequency in labor
Danazol
MOA: synthetic androgen that acts as partial agonist at androgen receptors
Clinical: endometriosis and hereditary angioedema
Toxicity: weight gain, edema, acne, hirsutism, masculization, decresaed HDL levels, hepatoxicity
Testosterone/methyltestosterone
MOA: agonist at androgen receptors
Clinical: treats hypogonadism and promotes development of secondary sex characteristics, stimulation of anabolism to promote recovery from burn or injury
Toxicity: masculinization in females, decreased intratesticular testosterone inhibiting release of LH leading to gonadal atrophy
Premature closure of epiphyseal plates
increase LDL, decrease HDL
Finasteride, dutasteride
MOA: 5a reductase inhibitor (decrease conversion of testosterone to DHT)
Clinical: BPH, hair growth
SE: decrease libido, erectile dysfunction, takes 6-12 months
Spironolactone
MOA: inhibits steroid binding (17a hydroxylase and 17, 20 desmolase)
Clinical: used with ketoconazole to prevent hirstuism in PCOD
SE: gynecomastia and amenorrhea
Clomiphene
Selective estrogen receptor modulator
Antagonist at hypothalamus receptors
Prevents normal feedback inhibition and increase release of LH and FSH from pituitary stimulating ovulation
Clinical: infertility due anovulation (PCOS)
Toxicity: hot flashes, ovarian enlargement, multiple simultaneous pregnancies, and visual disturbances
Ketoconazole
MOA: inhibits steroid synthesis (17, 20 desmolase)
Clinical: used with spironolactone to prevent hirstuism in PCOD
SE: gynecomastia and amenorrhea
Sildenafil, vardenafil
MOA: phosphodiesterase inhibitor leading to incresae cGMP
Smooth muscle relaxation in corpus cavernousm increasing blood flow and penile erection
Clinical: treatment of ED
Toxicity: headache, flushing, dyspepsia, impaired blue-green color vision
Life threating hypotension in patients taking nitrates
Flutamide
MOA: nonsteroidal competitive inhibitor of androgens at the testosterone receptor
Decreasing stimulatory effect of androgens on primary tumor or mestatases leading to decreased size
Clinical: prostate carcinoma
Use with leuprolide to decrease rise in testosterone
SE: hot flashes, gynecomastia, and impotence
Magnesium Sulfate
IV used for eclampsia
