Reproductive Pharmacology 2 Flashcards
anti-progestin - example
*mifepristone
mifepristone - MOA
*anti-progestin
*MOA: competitively binds to the progesterone receptor, blocking the effects of progesterone:
1. breakdown of endometrium
2. embryo detachment
3. contraction-inducting activity in myometrium
4. cervical dilation & expulsion of embryo
mifepristone (anti-progestin) - ADEs
*vaginal bleeding
*cramping
*N/V/D
*chills
*headache
*dizziness
mifepristone (anti-progestin) - place in therapy
*used in termination of intrauterine pregnancy (first trimester)
*labor induction
*hyperglycemia in pts with Cushing syndrome
termination of pregnancy - overview
*mifepristone → 24-48 hours → misoprostol
*misoprostol (e.g. Cytotec; prostaglandin analogue) causes cervix to soften/dilate → expulsion
*very high efficacy early on in pregnancy
*buccal misoprostol > vaginal
*no evidence to suggest adverse outcomes with subsequent pregnancies
misoprostol - overview
*aka Cytotec
*a prostaglandin E1 analog
*effects: softens / dilates (ripens) the cervix to allow for easier expulsion
*place in therapy:
-following mifepristone during medical abortion
-component of labor induction to soften cervix
roles of endogenous testosterone
*anabolic effects (muscle mass/strength)
*maturation of sex organs and development of secondary sex characteristics
*recall: testosterone is converted to estradiol via aromatase enzyme
synthetic androgen - example
*danazol
danazol - MOA
*synthetic androgen
*MOA: suppresses FSH and LH at the pituitary → atrophy of endometrial tissue (antiestrogen)
*also inhibits gonadal synthesis of hormones
danazol (synthetic androgen) - ADEs
*voice deepening
*hirsutism
*weight gain
*acne
*hot flashes
*decreased breast size
*hepatic dysfunction and dyslipidemia
*anovulation
*amenorrhea
*teratogenic
danazol (synthetic androgen) - place in therapy
*endometriosis (last line)
*fibrocystic breast disease
exogenous androgens: testosterone & methyltestosterone - MOA
*stimulates androgen receptors in organs and tissues to promote growth and development of male sex organs and maintains secondary sex characteristics in androgen-deficient males
androgens: testosterone & methyltestosterone - ADEs
*sodium retention (HTN/HF)
*acne
*facial hair growth
*deepened voice
*increased muscle development
*decreased spermatogenesis
*gynecomastia
*liver abnormalities
*aggressive behavior
*BPH
*erythrocytosis
androgens: testosterone & methyltestosterone - place in therapy
*delayed puberty (males)
*hypogonadism
*hormone therapy in transgender males (female to male)
considerations for male hypogonadism treatment
*exogenous androgen is NOT recommended for men with NORMAL testosterone levels (goal to achieve normal levels)
*benefits of exogenous androgen: development of secondary sex characteristics and increase libido, muscle strength, bone density, and mood (3-24 months)
*PO testosterone products has rapid hepatic clearance, so alternative routes are typically preferred (topical gels)
*monitoring: screen for prostate cancer, monitor hematocrit, and consider CV risk factors
anti-androgens (androgen antagonists) - examples
*flutamide
*bicalutamide
*nilutamide
*enzalutamide
anti-androgens (androgen antagonists) - MOA
*inhibits androgen uptake and/or inhibits binding of androgen in target tissues → blocking bindings of dihydrotestosterone
examples: flutamide, bicalutamide, nilutamide, enzalutamide
anti-androgens (androgen antagonists) - ADEs
*gynecomastia
*hot flashes
*GI disturbances
*elevated LFTs
*breast tenderness
*sexual dysfunction
examples: flutamide, bicalutamide, nilutamide, enzalutamide