Sex steroids Flashcards
Estradiol has which pharmacokinetic properties
orally ineffective, slow release depot esters of estradiol
comes in topical preps
Therapeutic uses of Estradiol
used in HRT and hypogonadism
Conjugated estrogens, phamacokinetics
metabolized estrogen, can be given orally, IV, IM, vaginal
Therapeutic use of conjugated estrogens
HRT
What is the prototype synthetic estradiol analog
ethinyl estradiol
Pharmacokinetics of ethinyl estradiol
ethinyl group slows metabolism, increases potency and oral effectiveness
Side effects of estrogens
nausea, edema, breast tenderness, hyperpigmentation, migrane, cholestasis, insulin resistance, liver and gaul bladder disease. Thrombophlebitis, endrometrial cancer (reduced by progestin combos), feminization in men
Therapeutic uses of estrogens
oral contraceptives and HRT
Pharmacokinetics of progesterone
IM, creams, suppositories, IUD
Prototype of synthetic progesterones
medroxyprogesterone acetate
Use for progesterones
HRT, IM birth control
What are the synthetic progestin structurally related to testosterone
Norethindrone, and norgestimate (less androgen effects)
Therapeutic uses of progestins
alone or with estrogens as contraception or HRT
decrease endometrium proliferation
endometiral and breast cancer
Progestin related side effects
menstraul changes, nausea, bloating, breast tenderness, teratogenesis possibility
Androgen mediated side effects
acne, weight gain, masculinization, altered libido, decreased HDL increased LDL
What are the effect of long-term hormone replacement
bone health increase, but cardiovascular health decrease, increased endometrial cancer w/ estrogen alone, some improvement w/ both. E and P both increase breast cancer risk.
HRT regimens
Oral conjugated estrogens and medroxyprogesterone is most common
cyclic estrogen plus progestin
continuous estrogen plus cyclic progestin
continuous estrogen and progestin
estrogen alone only if hysterectomy
Agonist effect at estrogen receptors used for osteoperosis
Raloxifene
Antagonist effect in breast cancer
Tamoxifen
Tamoxifen agonist/antagonist actions on different tissues
antagonist- prevents breast cancer, menopausal side effects
agonist- increase uterine cancer risk, reduce osteoperosis, improve heart health
Raloxifene agonist/antagonist actions on different tissues
antagonist- prevents breast and uterine cancer, causes menopausal side effects
agonist- decrease osteoperosis, increase thrombosis
Most common ingredients of oral contraceptives
ethinyl estradiol and norethindrone or norgestimate
Which progesterones have androgenic properties
norethindrone, levonorgestrel
which progesterones have neither androgenic nor estrogenic properties
norgestimate
Which progesterone has anti-androgenic effects
drospirenone
which drugs are in the 3-week vaginal ring
etonogestrel and ethinyl estradiol
Adverse effects of oral contraceptives due to estrogen component
nausea, irritability, headache, fluid retention, cyclic weight gain, breast enlargement and tenderness, menstrual changes, altered libido
Adverse effects of oral contraceptives due to progestin
nausea, bloating, menstrual changes, depression, fatigue. Androgen properties can cause acne, hirsutism, increased libido, weight gain.
Progestin used for IM contraception
Medroxyprogesterone
Progestin used in “emergency” contraceptives
levonorgestrel
Pharmacokinetics of testosterone
ineffective orally, limited parenteral effectiveness, rapidly metabolized. Topical preps becoming important for low T
Testosterone ester pharmacokinetics
IM injection 2-3 times per week, some longer preps
Adverse effects of testosterone
masculinization, feminization, testicular atrophy, prostatic enlargement, acne, hypertension, salt and water retention, liver disease, psychosis
