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What activate estrogen receptors on bone and vascular tissue while antagonizing estrogen receptors on uterine and breast tissue?
- SERMs (Selective Estrogen Receptor Modulators)
- Tamoxifen (Nolvadex)
- Rolaxafene (Evista)
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What is the primary risk factor from estrogen and progesterone?
CVD
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What was the 1st SERM that doesn't completely block estrogen receptors on uterine tissue and may stimulate endometrial proliferation (increases uterine cancers)?
Tamoxifen (Nolvadex)
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What does Raloxafene (Evista) do?
- SERM
- Blocks estrogen receptors on breast and uterine tissues
- Treating osteoporosis
- Side effects: hot flashes depression, insomnia, GI disturbances, joint muscle pain
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What do antiestrogens do?
- Antagonize all estrogen receptors
- High levels of estrogen inhibit FSH and LH
- Treat infertility
- Clomiphene (Clomid, Serophene)
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What do antiprogestins do?
- Antagonist to progesterone receptors in uterus
- Causes detachment of placenta
- Used to terminate pregnancy/ abort
- Mifepristone (Mifeprex): morning after pill (RU486)- w/in 1st 7 wks of pregnancy
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How do contraceptives work?
- Inhibit ovulation and impair development of endometrium
- High levels of est/progest limit release of FSH and LH (limiting LH prevents ovulation)
- Birth control pill typically has fixed amount of est/progest
- Progesterone only: Norplant and Depo Provera
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What are rehab considerations of taking hormones?
- Monitor BP
- Education about androgen abuse
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What are male and female sex hormones and where are they made?
- Androgens: testes
- Estrogens and progestins: ovaries
- (Made in gonads)
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Where is testosterone made? How is it regulated?
- LEYDIG CELLS located in interstitial space betw seminiferous tubules where spermatogenesis occurs
- Regulated by gonadotropins LH and FSH from anterior pituitary
- GH, prolactin, and other homrones also have influence
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What does LH do in men?
- Both LH and FSH control spermatogenesis
- Primary hormone that stimulates testosterone production
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What does FSH do in men?
- Controls spermatogenesis along with LH
- Stimulates growth and function of Sertoli cells
- Responsible for development and maturation of normal sperm
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What are clinical uses of Androgens?
- Replacement therapy
- Catabolic states
- Delayed puberty
- Breast cancer
- Anemia
- Hereditary angioedema
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What is used to inhibit the synthesis of effects of endogenous androgen production? (and in prostate cancer or BPH)
Antiandrogens
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What helps treat hirsutism in women or treat prostate cancer?
- Flutamide (Eulexin)
- Antagonist of cellular androgen receptor
- Antiandrogen
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What is Buserelin?
- (Suprefact)
- Antiandrogen
- GnRH analog: desensitizes GnRH receptors to decrease LH and testosterone production
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What inhibits conversion of testosterone to dihydrotestosterone?
- Finasteride (Proscar)
- Dutasteride (Avodart)
- Antiandrogen
- Accelerates growth of prostate gland
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What is Abarelix?
- (Plenaxis)
- Directly blocks GnRH receptor on pituitary (decreases LH production)
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How are androgens abused?
- Anabolic steroids taken to enhance athletic performance
- 7-14 wk cycles with increase in dosage
- Promote skeletal muscle growth and increase lean body mass
- increased aggressiveness
- Many side effects, even fatal
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What do estrogen and progesterone do?
- Promote sexual differentiation and maturation
- Estrogen (Estradiol): initiates growth and development of female reproductive system
- Progesterone: facilitates and maintains pregnancy
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What is the menstrual cycle?
- 28 days
- Stimulates ovaries to produce an ovum available for fertilization
- Prepares endometrium for implantation of ovum
- Follicular (Proliferative), Ovulation, and Luteal (Secretory) Phases
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What is the Follicular phase?
- Proliferative phase
- 1st half
- Ant pituitary releases FSH which stimulates maturation of several follicles in the ovary (one follicle fully matures and yields ovum)
- Developing follicle secretes estrogen (causes endometrial growth)
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What occurs during Ovulation?
- LH release causes ovum release
- Mature follicle ruptures releasing ovum from the ovary
- Travels down fallopian tubes to uterus
- Follicle is corpus luteum after release of ovum
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What occurs during the Luteal phase?
- Secretory phase
- 2nd half of cycle
- Corpus luteum grows and develops for 1 week after ovulation and secretes est/progest (this thickens uterine lining)
- Uterus gets ready for implantation
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What happens if egg in not fertilized/implantation doesn't occur?
endometrium sloughs off creating menstrual bleeding
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What are conditions treated with Estrogen and Progesterone?
- Replacement Therapy
- Hypogonadism
- Failure of ovarian development
- Menstrual irregularities
- Endometriosis
- Carcinoma
- Conjugated estrogens (Premarin): oral, transdermal
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What happens if fertilization occurs?
- Corpus luteum continues to produce progesterone
- Human chorionic gonadotropin (HCG) is released fron the fertilized ovum and takes over role of LH and rescues corpus luteum from destruction
- Corpus luteum degenerates betw weeks 9 and 14 of gestation
- Placenta produces estrogen and progesterone
- Progest. increases growth of mammary glands
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