Reproductive Flashcards
Leuprolide
GnRH analog
Agonist properties when used in pulsatile fashion
Antagonist properties when used in continuous fashion (downregulates GnRH receptor in pituitary to decrease FSH/LH)
“Leuprolide can be used in lieu of GnRH”
Leuprolide uses
GnRH analog Infertility = pulsatile Prostate cancer = continuous, used with flutamide Uterine fibroids = continuous Precocious puberty = continuous
Leuprolide toxicity
Antiandrogen
Nausea
Vomiting
Estrogens
Ethinyl estradiol
DES (Diethylstilbestrol)
Mestranol
Bind estrogen receptors
Estrogens
Toxicity?
Contraindications?
Increased risk of endometrial cancer
Bleeding in postmenopausal women
Clear cell adenocarcinoma of vagina in females exposed to DES in utero
Increased risk of thrombi
Contraindications = ER + breast cancer, history of DVTs
Selective estrogen receptor modulators = SERMs
Clomiphene
Tamoxifen
Raloxifene
Clomiphene
Uses?
Side effects?
SERM
Antagonist at estrogen receptors in hypothalamus
Prevents normal feedback inhibition and increases release of LH and FSH from pituitary = stimulates ovulation
Use = tx of infertility due to anovulation (PCOS)
SE = hot flashes, ovarian enlargement, multiple simultaneous pregnancies, visual disturbances
Tamoxifen
SERM
Antagonist on breast tissue
Agonist at uterus (risk cancer) and bone
Associated with endometrial cancer and thromboembolic events
Use = treat/prevent recurrence of ER + breast cancer
Raloxifene
SERM Agonist on bone Antagonist at uterus Increased risk of thromboembolic events Decreased resorption of bone = used to treat OSTEOPOROSIS
Hormone replacement therapy
Used for relief or prevention of menopausal symptoms (hot flashes, vaginal atrophy) and osteoporosis (increase estrogen, decrease osteoclast activity)
What is the risk with unopposed estrogen replacement therapy?
Increased risk of endometrial cancer
As a result, progesterone is added
Possible increased cardiovascular risk as well
Anastrozole and Exemestane
Aromatase inhibitors
Used in postmenopausal women with breast cancer
Progestins
Bind progesterone receptors = decrease growth and increase vascularization of endometrium
Uses = oral contraceptives; tx of endometrial cancer and abnormal uterine bleeding
Mifepristone (RU-486)
Use?
Toxicity?
Competitive inhibitor of progestins at progesterone receptors
Use = termination of pregnancy; administered with misoprostol (PGE1)
Toxicity = heavy bleeding, GI effects (n/v, anorexia), abdominal pain
Oral contraception (synthetic progestins, estrogen)
Estrogen and progestins inhibit LH/FSH and thus prevent estrogen surge
No estrogen surge = no LH surge = no ovulation
Effects of progestins in contraception
Thickening of cervical mucus = limiting access of sperm to uterus
Inhibition of endometrial proliferation = less suitable for implantation of embryo
Oral contraception contraindications
Smokers > 35 years old (increased risk of CV events)
Patients with history of thromboembolism and stroke or history of estrogen-dependent tumor
Terbutaline
B2-agonist that relaxes uterus
Used to decrease contraction frequency in women during labor
When might terbutaline be used?
To prevent premature labor
Danazole
Uses?
Synthetic androgen that acts as partial agonist at androgen receptors
Uses = endometriosis and hereditary angioedema
Danazole toxicity
Synthetic androgen that acts as partial agonist at androgen receptors Weight gain Edema Acne Hirsuitism Masculinization Decreased HDL levels Hepatotoxicity
Testosterone and Methyltestosterone
Toxicity?
Agonist at androgen receptors
Causes masculinization in females
Decreases intratesticular testosterone in males by inhibiting release of LH (via neg feedback) = gonadal atrophy
Premature closure of epiphyseal plates
Increased LDL and decreased HDL
Antiandrogens
Finasteride
Flutamide
Ketoconazole
Spironolactone
Finasteride
5a-reductase inhibitor = decreases conversion of testosterone to DHT
Uses = BPH and male-pattern baldness (promotes hair growth)
Flutamide
Nonsteroidal competitive inhibitor of androgens at the testosterone receptor
Uses = prostate carcinoma
Ketoconazole
Inhibits steroid synthesis (inhibits 17,20-desmolase)
Use = tx PCOS to prevent hirsutism
SE = gynecomastia and amenorrhea
Spironolactone
Inhibits steroid binding, 17a-hydroxylase, and 17,20-desmolase
Use = tx PCOS to prevent hirsutism
SE = gynecomastia and amenorrhea
Which drugs can cause gynecomastia?
"Some Dope Drugs Easily Create Awkward Hairy DD Knockers" Spironolactone Dope/marijuana Digitalis/digoxin Estrogen Cimetidine Alcohol Heroin Dopamine D2 antagonists Ketoconazole
Shortened = “Some Drugs Cause Awesome Knockers”
Tamsulosin (FloMax)
a1-antagonist used to treat BPH by inhibiting smooth muscle contraction
Selective for a1A,D receptors (found on prostate) vs. vascular a1B receptors
Sildenafil
Vardenafil
Tadalafil
Sildenafil = Viagra
Vardenafil = Levitra
Tadalafil = Cialis
“-fil” the penis
Inhibit phosphodiesterase 5 = increased cGMP, smooth muscle relaxation in corpus cavernosum, increased blood flow, and PENILE ERECTION
PDE5 inhibitor toxicity
Headache
Flushing
Dyspepsia
Impaired blue-green color vision
Risk life-threatening hypotension in patients taking nitrates
“Hot and sweaty” but then Headache, Heartburn, Hypotension”
What should you never give to a patient who is taking a PDE5 inhibitor?
NITRATES
Risk life-threatening hypotension
