Estrogens and Androgens Flashcards
Estrogens MOA and side effects
MOA: Binds intracellularly and regulates gene transcription.
Side effects: Endometrial cancer risk, uterine bleeding, Thrombus, HA, MI, peripheral edema, HTN, nausea.
GnRH analogs. Pulse doses do what?
Chronic doses do what?
Pulse doses:
Spermatogenesis and induce ovulation
Continuous:
Tx prostate cancer and endometriosis
SERMs MOA and side effects
Non steroid compounds that bind to estrogen receptors. Can be agonist or antag.
Causes hot flashes, nausea, drug drug interactions.
MOA for raloxifene and tamoxifen
and clomiphene
raloxifene and tamoxifen - compete with estrogen for binding in breast tissue. Causes regression of some breast tumors.
Tamoxifen may increase changes of uterine cancer.
Raloxifine decreases bone resorption.
clomiphene- antagonist. Blocks neg feedback loop. More LH and FSH released. Helps with infertility.
Tamoxifen side effects
Crystalline ret Macular edema Corneal opacities Cataract ON
Progestogens MOA and side effects
MOA: Tx hormonal deficiency, contraception.
Side effects: HA depression weight gain
Synthetic progestogens that are more stable to first pass metabolism
Medroxyprogesterone.
Megostrol
Norethindrone
Mifepristone
Progesterone antagonist. Admin causes abortion
MOA of androgens
Anabolic agent. Promotes bone growth, development of genitals and increases muscle mass.
Testosterone binds specific nuclear receptor and regulates gene expression.
Therapeutic use of androgens
Males with low testosterone secretion. Hypogonadism. Osteoporosis or chronic wasting.
MOA of anti androgens
Biclutamide and Nilutamide prevent the production of GnRH to decrease testosterone production. Tx BPH and prostate cancer.
Flutamide- blocks action of testosterone in target organs. Tx prostate cancer.
Contraceptive side effects
Usually due to estrogen component. Fluid retention, HA, nausea, vomiting.
Increase risk of cervical cancer.
Weight gain
Increase HDL and decrease LDL
LH controls the production of what two hormones
Estrogen and testosterone. These will act as negative feedback on the hypothalamus and stop release of GnRH.
Progestogen is produced in response to
LH in both males and females. Promotes development of endometrium in women.
Admin of testosterone
Ineffective orally due to first pass