Sex hormones Flashcards
17 beta estradiol
Most important physiological estrogen
Pharm: eliminated by liver, poor oral availability, transdermal patches to avoid hepatic first pass
Uses: post-menopausal therapy
estrone sulfate, equiline sulfate
conjugated estrogens
Pharm: PO, absorbed lower GI tract
Uses: oral hormone replacement therapy in post menopausal women
estradiol valerate, estradiol cypionate
Esterified estrogens
Pharm: parenteral injections in oil, slower
Uses: prolonged systemic delivery of 17 beta estradiol to circulation 2-4 weeks that reduces hepatic effects of estrogens
ethinyl estradiol, mestranol
Synthetic steroidal estrogens
Pharm: PO, decreases hepatic first pass metabolism, long half life
Uses: combo with oral contraceptives
DES
Synthetic non-steroidal estrogen
Pharm: PO potent estrogen with prolonged effects
Uses: paliative treatment of metastatic prostate or breast cancer, relieves bone pain and improves quality of life
Side effect: CV toxicity due to high doses
medroxyprogesterone acetate
Progestin: support pregnancy in experimental animals, anti aldosterone effects, inhibit LH and FSH release
Pharm: DepoProvera given PO
Uses: hormone replacement regimens for post menopausal women
megestrol acetate
Progestin: support pregnancy in experimental animals, anti aldosterone effects, inhibit LH and FSH release
Uses: stimulate appetite and weight gain in patients with AIDS
norethindrone, levonorgestrel
Pharm: good PO availability, produce decidual change in endometrium, stronger inhibitors of LH and FSH
- weak androgen and antiestrogen effects
Uses: combo oral contraceptives, progestin alone, patches, emergency
Norethynodrel
Pharm: good PO availability, produce decidual change in endometrium, stronger inhibitors of LH and FSH
- estrogenic effects
Uses: combo oral contraceptives, progestin alone, patches, emergency
desogestrel, norgestimate
Pharm: good PO availability, produce decidual change in endometrium, stronger inhibitors of LH and FSH
- minimal androgenic or estrogenic effects
Uses: combo oral contraceptives, progestin alone, patches, emergency
dienogest
Pharm: good PO availability, produce decidual change in endometrium, stronger inhibitors of LH and FSH
- antiandrogenic
Uses: combo oral contraceptives, progestin alone, patches, emergency
drospirenone
spironolactone related progestin
Pharm: anti-mineralocorticoid similar to progesterone, no androgenic activity
Side effects: less water retention and breast tenderness
ulipristal acetate
Selective progesterone receptor modulator with agonist and antagonist effects
- used for emergency contraception
Testosterone (T)
Pharm: poor systemic bioavailability after oral dosing or subq or IM
Side effects: induce pubertal changes, no hepatotoxicity
testosterone ethanate, testosterone cypionate
Pharm: IM
Uses: induce pubertal changes in hypogonadal boys
Side effects: no hepatotoxicity
methyl testosterone, fluoxymesterone, oxandrolone
anabolic steroids - dose related hepatotoxicity
danazol
Pharm: synthetic steroid derivative PO use
- mix of weak androgen, antiestrogen, progestin, glucocorticoid activity
Side effects: acne, cholestatic jaundice, liver tox, benign hepatic tumors, increased aggression
Uses: endometriosis, prevent hereditary angioneurotic edema in patients with complement C1 inhibitor deficiency
Progestin only contraceptives
Used when estrogen is contraindicated
Side effects: weight gain, abnormal bleeding, delayed onset fertility, increases risk of osteoporosis
Uses: birth control, dysmenorrhea, endometriosis
Combo: dysmenorrhea, acne, hirsutism
Levonorgestrel
Plan B
- used when begun within 72 hour of intercourse
Pharm: large doses of estrogen, estrogen and progestin
Side effects: nausea
ella - ulpristal acetate
Selective progesterone receptor modulator
Uses: prevents ovulation and impairs implantation
- started within 120 hours of intercourse
Side effects: headache, nausea, dysmenorrhea
medroxyprogesterone acetate with estrogen replacement therapy
Avoid risk of uterine cancer due to exposure to estrogen alone
Uses: menopause sx, decrease risk of osteoporosis
- no change in atherosclerosis, colon cancer, alzheimer’s disease
Side effects: increase risk of breast CA
Estrogen premenopausal adverse effects
Side effects: nausea, breast tenderness, headache, altered skin pigmentation, increased risk of gall bladder disease, increased DVT, increased MI and stroke
Estrogen postmenopausal adverse effects
VTE, DVT, uterine cancer unless progestin used as well
flutamide, bicalutamide
Non steroidal antagonist of androgen receptor
Uses: prostate cancer therapy in combo with GnRH, prevents tumor flare due to rise in testosterone
Bicalutamide - potent, longer acting less hepatotoxicity
spironolactone
weak androgen receptor antagonist
- reduces testis levels of steroid 17 alpha hydroxylase
Uses: hirsutism
ketoconazole
Antifungal that can inhibit multiple steroidigenic enzymes to decrease androgen as well as corticosteroid synthesis
finasteride
5 alpha reductase inhibitor
Uses: treatment of benign prostatic hypertrophy or male pattern baldness
abiraterone
17 alpha hydroxylase that blocks androgen synthesis
Pharm: orally with glucocorticoid replacement
Uses: treatment of prostate CA after castration and doxetaxel therapy
tamoxifen
selective estrogen receptor modulators
Uses: breast CA treatment and prevention, osteoporosis, infertility
- ER positive breast CA, prevention of breast CA in high risk patients
Side effects: estrogen effects to increase risk of venous thromboembolism, chronic use increases uterine cancer risk
raloxifen
selective estrogen receptor modulators
Uses: osteoporosis,
Side effects: minimal estrogen agonist effects on uterus, less risk of uterine cancer with chronic use
clomiphene
Selective estrogen receptor modulators
Uses: treatment of infertility
anastrozole, letrozole, exemestane
Aromatase inhibitors
Pharm: inhibit CYP19, androgens to estrogens
Uses: breast cancer resistant to tamoxifen or aromatase inhibitors
Side effects: osteoporosis
fluvestrant
pure estrogen receptor antagonist
uses: advanced breast cancer resistant to other therapies
side effects: increased risk of osteoporosis
mifepristone
Progesterone receptor antagonist - used to induce first trimester abortions
- first 7 weeks of conception
Uses: stimulates uterine contractions to abort fetus
Side effects: nausea, vomiting, diarrhea, vaginal bleeding
