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Sex Steroids 1
N/A
29
Medical
Professional
02/26/2010

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Term
Testosterone
Definition
Parenterally administered androgen

Highly bound to plasma proteins

Bioactivated to dihydrotestosterone by 5a-reductase
Term
Oxandrolone
Definition
Promotes weight gain following extensive sgx, chronic infxn, trauma

Approved for alcoholic hepatitis, Turner's, and HIV weight loss

Not readily aromatized to estrogen
Term
Danazol
Definition
Term
Flutamide
Definition
Non-steroidal anti-androgen

Used in rx of prostatic cancer
Term
Bicalutamide
Definition
Non-steroidal anti-androgen

Now replacing flutamide due to less hepatotoxic effects and once a day dosing
Term
Finasteride
Definition
Inhibitor of 5a-reductase

Used to rx BPH and male pattern baldness

*Reduces incidence of prostate cancer, but cases more severe
Term
Cyproterone
Definition
Steroidal anti-andronergic

Weak partial agonist for androgen rec
Term
GnRH
Definition
released from the hypothalamus in a pulsatile fashion

acts on ant pituitary to stimulate FSH and LH release
Term
Clomiphene
Definition
Anti-estrogen

Fertility rx used to rx ovarian failure

Blocks estrogen-mediate inh of FSH/LH release

Can work too well! Many babies!
Term
Urofollitropin
Definition
Purified FSH recovered from urine of menopausal women

Produces follicular stimulation
Term
Follitropin
Definition
Recombinant FSH collected from urine of menopausal women

Produces follicular stimulation
Term
Menotropins (2)
Definition
Urofollitropin
Follitropin
Term
Human chorionic gonadotropin
Definition
Collected from urine of pregnant women

Action similar to LH (induces ovulation)
Mimics LH surge following use of menotropin
Term
Danazol
Definition
Synthetic androgen used to inh FSH/LH in endometriosis in females

Atrophies ectopic endometrial tissue
Term
Leuprolide
Definition
GnRH analog

Rx of infertility due to hypothalamic amenorrhea

INTERMITTANT administration results in sustained FSH/LH release and OVULATION

FREQUENT administration desensitizes GnRH receptors and suppresses FSH/LH, cxing infertility

Used in PROSTATE CA to supress FSH/LH release
Term
Goserelin
Definition
GnRH analog

Rx of infertility due to hypothalamic amenorrhea

INTERMITTANT administration results in sustained FSH/LH release and OVULATION

FREQUENT administration desensitizes GnRH receptors and suppresses FSH/LH, cxing infertility
Term
Nafarelin
Definition
GnRH analog

Rx of infertility due to hypothalamic amenorrhea

INTERMITTANT administration results an sustained FSH/LH release and OVULATION

FREQUENT administration desensitizes GnRH receptors and suppresses FSH/LH, cxing infertility
Term
Ganirelix
Definition
Pure GnRH Antagonist

Inh FSH/LH release w/o initial increase

Used in management of infertility to prevent premature LH surge
Term
Abarelix
Definition
Pure GnRH Antagonist

Inh FSH/LH release w/o initial increase

Used in management of infertility to prevent premature LH surge
Term
Estradiol
Definition
The major endogenous estrogen in humans

Weak oral potency
Term
Pharmacokinetics of Steroidal Estrogens
Definition
Highly lipophilic, so well absorbed in GI

Extensively bound to plasma proteins

Hepatic metabolism
Term
Uses of Estrogens
Definition
Premenopausal hypogonadism
Hormone replacement therapy
Rx breast, prostatic, and ENDOMETRIAL cancers
Oral contraceptives
Term
Ethinyl estradiol
Definition
steroidal estrogen

orally effective
Term
Mestranol
Definition
steroidal estrogen

orally effective pro-drug, quickly demethylated to ethinyl estradiol
Term
Mechanism of estrogens
Definition
Estradiol enters liver and binds to ER which dimerizes and binds to Estrogen Response Elements in promoter region of estrogen-activated genes
Term
Metabolic effects of estrogens (7)
Definition
Inc bone density
inc HDL, dec LDL
vasodilation
fluid retention
inc chol secretion, dec bile secretion in GB
facilitates clot formation
Inc plasma hormone binding proteins
Term
Adverse responses to estrogens (7)
Definition
1. Inc endometiral cancer w estrogen alone
2. Inc risk of clear-cell vaginal and cervical adenoCA after exposure in utero
3. Thromboemblic
4. Fetal abnormalities (NEVER GIVE IN PREGNANCY)
5. Inc GB dz
6. Migraines
7. N/V
Term
Hormone replacement therapy effects (3)
Definition
Prevent osteoporosis
Rx vasomotor disturbances
Rx vaginal/vulvular atrophy
Term
Conjugated estrogens
Definition
Slow release oral estrogens
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