Term
| What structural element of estrogens confers selectivity and HI affinity for estrogen R's? |
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Definition
| Phenolic A ring (C3 hydroxy) |
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Term
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Definition
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Term
| What is the principal source of estrogen in pre-menopausal women? (Post-menopausal women? Men?) |
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Definition
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Term
| Metabolic actions of estrogens |
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Definition
- salt & water retention --> edema, hypertension
- decr. LDL, incr. HDL (good)
- incr. coagulation factors (bad)
- overall incr. risk of cardiovascular disease!
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Term
| What is the current treatment of choice for dysmenorrhea (severe menstrual pain)? |
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Definition
- NSAID's
- block uterine production of prostaglandins
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Term
| Adverse effects of estrogen therapy |
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Definition
- cancers (e.g. endometrial, breast)
- co-administration of progesterone decr. endometrial but incr. breast cancer
- cardiovascular disease
- post-menopausal bleeding
- prevent w/ co-administration of progesterone
- nausea, breast tenderness, hyperpigmentation, migrane, cholestasis, hypertension
- use minimum effective dose to control
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Term
| What are the contraindications of estrogen therapy? |
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Definition
- pregnancy
- estrogen-dep neoplasms
- hx of thromboembolic disorder
- undiagnosed genital bleeding
- liver disease
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Term
| estrogen receptor competitive antagonists |
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Definition
- triarylethylene antiestrogens
- req activ'n by hydroxylation of A ring, C4
- trans config'n = estrogen R antagonists
- cis config'n = estrogen R agonists
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Term
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Definition
- block estrogen R's at hypothal & pituitary --> decr. neg feedback --> incr. GnRH --> incr. gametogenesis & steroidogenesis
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Term
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Definition
- anastrozole
- letrozole
- liarozole fumarate
" Ana Let Lia inhibit aromatase." |
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Term
| Indications for aromatase inhibitors |
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Definition
- post-menopausal women w/ breast cancer risk
- infertility in pre-menopausal women
- Letrozole: induces ovulation
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Term
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Definition
| ectopic growth of uterine tissue |
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Term
What are the treatments for endometriosis? (Hint: what is the goal of treatment?) |
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Definition
Goal: reduce estrogen levels Leuprolide (GnRH analog) Nafarelin (GnRH analog) oral progestins
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Term
| What are uterine fibroids and how are they treated? |
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Definition
Estrogen-sensitive benign tumors of the uterus. Tx w/ leuprolide & nafarelin (GnRH analogs) and Cetrorelix acetate (GnRH antagonist). |
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Term
| What structural feature of progestins confers selectivity and HI affinity for progesterone R's? |
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Definition
Ketone moeity @ C3 of the A Ring. |
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Term
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Definition
no androgenic activity medroxyprogesterone megestrol acetate
androgenic side effects norethindrone norgestrel ethynodiol
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Term
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Definition
comp. antagonist @ progesterone & glucocorticoid R's (anti-progestin act'y) abortifacient (comb. w/ prostaglandins) inhibits hypothalamic feedback of adrenocortical axis --> incr. CRF, ACTH --> incr. adrenal steroidogenesis
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Term
| What are the adverse reactions of oral contraceptives? |
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Definition
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Term
What accounts for the difference in hematocrit b/w men and women? |
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Definition
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Term
| What are the adverse effects of testosterone therapy? |
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Definition
masculinization of women feminization of men (due to aromatase act'y) skel. abnormalities in children edema (Na+ retention) jaundice (cholestatic hepatitis) hepatic adenocarcinoma (long term tx risk)
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Term
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Definition
testosterone testosterone salts oxymetholone oxandrolone methyltestosterone fluoxymesterone danazol
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Term
| Anti-androgens (hint: 2 types) |
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Definition
Comp. antagonists Synth. inhibitors
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