Steroids Flashcards
Oral Contraceptives AA
ramping, bleeding, headache, decreased libido, no menses, weight gain, skin issues, acne, vaginal infections, thromboembolism, MI, hypertension, cerebrovascular disease, Gi issues, depression, cervical cancer, hypertension, diabetics, smokers, VTE, ischemic heart disease, cancer
Estrogens and Progesterones INTERACTIONS:
warfarin(increased with OCs), abx(decreases efficacy via cycling), rifampin(liver metabolism increase), phenytoin(increased catabolism), cimetidine(decreased catabolism)
Estrogens and Progesterones
LAB DRUG INTERACTIONS
AST and ALT levels, alter lipid panels, prothrombin time, and T4 bc of thyroid binding globulin.
Ethinyl estradiol:
oral and more resistant to metabolism. Can also be transdermal patch
conjugated equine estrogens (CEE)
for post menopausal women
Estrogens:
stradiol binds to sex hormone bidning globulin strongly, less to albumin.
Oral estrogens undergo enterohepatic recirculation. Excreted via kidneys.Good for contraception, post menopausal women, priary hypogonadism.
Progesterones Gestrel/gest:
precursor to estrogens, androgens, adrenocortical steroids. Thickens cervical mucus, maintains pregnancy, increases metabolism, decreases thyroid binding globulin and increases thyroid hormone activity. Loves albumin and transcortin. Enterohepatic recirculation. Excreted via kidneys
Medroxyprogesterone acetate (MPA)
long acting depo shot, irregular bleeding
Levonorgestrel (LNG):
IUDs, also a progesterone receptor modulator
Ulipristal :
progesterone receptor modulator
Anti estrogens:
Binds to ERa and ERB as competitive antagonists, for infertility and tamoxifen resistant BC.
Clomifene:
long HL(5-7 days) bc of enterohepatic recirc and accumulation in fatty tissues
Fluvestrant:
IM, anti estrogen. concentrations reached after 7 days, 13.5-18.5 h half life
Anti progesterone:
blocks uterine progesterone receptors, ensures expulsion of blastocyst
Anti progesterone drugs
Mifepristone, glucocorticoid antagonist
SERMs Ifen.Ifenes:
to compete with 17β-estradiol (E2) at the receptor site and to block the promotional role of E2 in breast cancer
Tamoxifen
agonist and antagonist effects, nonsteroidal, oral. CYP2D6
Raloxifene:
post menopausal osteoporosis, prophylatically for Bc with high risk fctors
Aromatase Inhibitors
blocks conversion of testosterone to estradiol(E2) and androstenedione to estrone(E1). Good for early and late stage ER+ BC and adjunct to GnRH agonists to treat premature follicular maturation, ovarian suppression. AA: loss of BMD, arthralgias, vaginal dryness, sexual dysfunction, normal ovarian function.
Exemestane:
type I, steroid, aromatase inhibitors
Anastrozole
type II, non steroidal, aromatase inhibitors
Testosterones
major degradation in liver, 65% bound to sex hormoen binding globulin,2% free for nculear receptors. Converted to DHT for cellular effects.
Testosterone Indications:
hypogonadism, chemo, endometriosis, cancer cachexia, anemia, osteoporosis, delayed puberty, slowing aging, androgen abuse in sports.
Testosterone Contraindications:
pregnant women, breast or prostate cancer, developing juveniles, renal or cardiac disease, HCC.
Higher androgenic to anabolic
effects is favorable for androgen replacement tx
Higher anabolic to androgenic
effects is favorable for anemia, osteoporosis, and protein loss.
Olones/zolol
anemia, testosterone
Androgen receptor antagonists
Flutamide: competitive androgen receptor antagonist, tx of prostate cancer and for women with androgen excess.
androgen synthesis inhibitors
Finasteride: 5a reductase inhibitor, treats prostatic hyperplasia and prevent male pattern baldness
