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Describe the use of GnRH analogs in both pulsatile and continuous dose continuous dose
- different actions if pulse or cont
- pulse= positive effect- give release of fsh lh
- continuous= negative effect-through downreg mech of receptors, no fsh lh release, can use this in Ca trmt. will get a tumor flare at first
- leuprolide
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Describe female hormones and how they are used
clinically g . List side effects of each female drug.
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Describe male hormones/drugs and how they are used clinically. List side effects of each male drug.
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Describe the use of adrenergic drugs in terms of uterinerelaxation and treatment of prostate hyperplasia.
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Gonadotropin releasing hormones 2 effects= leuprolide
gnrh analog- think back to phsyiology
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leuprolide, effect as contniuous?, pulsatile? clinical use
- gnrh analog-
- anatgonistic endometriosis, fibroids, prostate Ca, precocious puberty
- agonistic for infertility
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gnrh analog SE, contraindications?
- HA, nausea, flushing, light headedness
- continuous- menopause osteoporosis
- contra- breastfeeding and pregnancy
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estrogens- natural vs synthetic
- natural has major first pass effect- not absorbed well
- synthetic- increased oral effectiveness
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estrogen physiology
- regulate transcription
- stim development of organs ande secondary sex characteristics
- endometiral effects- continuous exposure leads to hyperplasia
- increase HDL, low LDL, increase TG H2O retention and water
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estrogen clinical uses (2)
- primary hypogonad- age 11-13
- postmenopausal hormone therapy- endometrial ca risk
- uterine biopsy if bleeding occurs, contra with estrogen tumors
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estrogen effects
- major cause of postmenopausal uterine bleeding
- nausea, breast tenderness, hyperpigmentation
- migraine ha, gallbladder, htn
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estrogen contraindications
- estrogen neoplasms
- heavy smokers increase risk over age 35
- genital bleeding
- use as short of time as possible
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progestins natural vs synthetic
synthetic absorb better
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3rd gen progestins and example
- - lower androgenic activity
- desogesterol
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progestins pharmacokinetics
- excreted in urine
- peanut allergy should be avoided- micronized
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progestin physiology
- decrease hdl, increase ldl, increase water and Na excretion
- opposite of estrogen
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progestins clinical use
- hormone replacement
- contraception
- used alone- prolonged anovulation and amenorrhea
- endometriosis
- bleeding disorders
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progestin contraindications
- increase bp
- ha, weight gain, depression, decrease libido
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hormonal contraception
- give progesterone and estrogen shuts off pit to stop lh fsh release- results in inhibition of ovulation
- will decrease breast milk production
- progestin alone- will not always inhibit ovulation
- cervical mucus thickening
- inhibits endometrial prolif
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OCP SE
- nv, failure to withdraw bleeding
- weigh gain, skin pigmentation, infections, hirsutism,
- thromboembolism, mi risk, stroke risk
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ocp contraindication
- rifampin
- epiphysial closure has not occurred
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depot provera and progestin implant note
longer these are insoma longer to reinstate ovulation
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estrogen receprots modulators partial ag and antagonists of estrodiol
partial agonist- tamoxifen- bind to estogen receptor will bind slightly but inhibits estrogen + breast ca
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raloxifene-
- prevention and treatment of osteoporosis after menopause
- decrease breast ca in post menpausal women
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clomiphene-use, se, trmt time risk
- ovulation disorders
- hot flashes, ha, constip, allergic skin rxn, hair loss
- over 1 year increase risk for ovarian ca
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mifepristone
- ru486 steroid inhibitors, used mostly for early preg termination
- proonged bleeding vomiting, diarrhea
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danazol
steroid inhibitors, suppress ovarian fn and get estrogen suprression through diff mech- get weight gain, acne, edema- testosterone like, used for endometriosis
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anastrozole
- aromatase inhibitors
- nonsteroidal
- good for tamoxifen resistance, or postmenopausal women with breast ca
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exemestane
- aromatase inhibitors
- steroid molecule, irreversable inhibitor of aromtase
- used for advance breast ca
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breast can treatment order
- tamoxifen
- anastrozole
- exemestane
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terbutaline
- beta 2 agonist- to relax uterus to decrease premature uterine contractions
- give time to give steroid to fetus for better survivability of lungs
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androgen and anabolic steroids
- oral testosterone associated with liver tumors
- stimulate growth in boys
- androgen prod decreases with age
- should not be used in infants
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male contraception
combo of testosterone and progestins to suppress sperm count
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se of androgen
- hisutism
- acne
- amennorrhea
- clitoral enlargemnt
- athlersclerosis- increase ldl, decrease dhl
- aggresion, psych
- reduce intratesticular testoserone by inhibiting lh release
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ketoconazole- steroid synthesis inhibitors antiandrogen- treatm,ent of PCOS increase estrogen:testosterone ratio
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finasteride-
- 5alpha reductase inhibitor
- reduce prostate size in bph, decrease dihydrotestoserone
- also male baldness
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flutamide
competitive inhibitor of test receptors- prostate ca
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spiranolactone
- inhibit dihydrotestosterone binding to androgen receptors
- hirusitm in women with pcos
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tamsulosin
sin alpha 1 blocker- prostate has particular alpha 1 receptors- greater potency in decreases prostate smooth muscle contraction good for bph
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sildenafil/ vardenafil
increase cGMP- cause relax of nonvascular smooth muscle and enhance erection
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alprostadil
- PGE1 analog
- used for failed viagra
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