Sex Steroids and HRT Flashcards
All sex hormones share similar structures to ____
Adrenal steroids
Main role of progestins
Promote gestation
Sex steroids act on which receptors?
Nuclear transcription factor receptors (effects protein synthesis)
Which sex steroids have active metabolites that are used as drugs?
Estrogen
Testosterone
Estrogens stimulate growth of ____
Endometrium
Estrogen provides feedback inhibition on anterior pituitary to suppress ___ release
FSH
Progestins inhibit ___ growth
Endometrial
Functions of progestin
Inhibit endometrial growth
Maintain vascular supply and secretory capacity
Progestin feedback inhibition on anterior pituitary suppresses ___ release
LH
Withdrawal of ____ leads to menstruation/abortion
Progestins
Physiologic effects of estrogen
Sexual maturation
Stimulation.of long bone growth
Decreases bone resorption
Improve lipid profiles/decrease CV risk
Increases risk of clotting
Clinical uses of estrogen
Hypogonadism/hypopituitarism
Postmenopausal
Birth control
Menstruql disorders
Estrogen drug used mainly for HRT and hypogonadism
Estradiol
Routes of administration for estradiol
Oral
Slow release IM injections (Depo)
Topical (vaginal creams or transdermal patches)
Main use of conjugated estrogens
HRT
Conjugated estrogens contain which active metabolites of estrogen?
Estrone and estriol
Ethinyl estradiol main use
Synthetic estrogen used in almost all contraceptives
Also HRT
Estrogen side effects
Nausea
Edema
Breast tenderness
Migraines
Liver disease
Increased risk of clotting
Gynecomastia and feminization in males
Estrogens increase risk of which cancers?
Endometrial and breast
Why should estrogens not be prescribed alone?
Need to be prescribed with progestins to reduce risk of cancer from estrogen
Clinical uses of progestins
Replacement therapy with estrogens
Birth control (alone or with estrogen)
Abnormal Uterine bleeding
Endometriosis
Dysmenorrhea
Type of progestin in IUDs
Progesterone
Benefit of medroxyprogesterone acetate
Mainly progesterone-like effects with little/no androgen or estrogen activity
Synthetic progestin that is structurally related to testosterone
Norethindrone
Adverse effects of all progestins
Menstrual changes
Nausea
Bloating
Potential teratogen
Adverse effects of nor-progestins
Androgenic effects
Acne
Weight gain
Masculinization
Worsened lipid profile
Postmenopausal HRT uses
Alleviate symptoms of menopause
Prevent/treat osteoporosis
When can estrogen be used alone without progesterone
Pre-puberty for enhancing bone growth
If uterus has been removed
Side effects of HRT
Return of menstrual bleeding
Increased risk of cancer and CV risk (mitigated by local administration)
Current recommendation on when to use HRT for Postmenopausal women
Short-term use (<5 yrs) of E+P for menopause onset symptoms
Not recommended for long term health maintenance
Selective estrogen response modifiers (SERMs) are non-steroidal analogs with ____ properties on estrogen receptors
Mixed agonist-antagonist
SERM drugs
Raloxifene
Tamoxifen
Difference between raloxifene and tamoxifen
Raloxifene decreases risk of uterine cancer
Tamoxifen increases risk of uterine cancer
Similarities between Raloxifene and tamoxifen
Decrease osteoporosis
Improve lipids
Decrease breast cancer
Increase risk of clotting
Increase hot flashes