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39 Cards in this Set
- Front
- Back
When is magnesium sulfate contraindicated for use as a tocolytic?
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Being phased out, but absolute contraindication in myasthenia gravis and renal impairment.
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What is the use of 17-OH Progesterone in preventing preterm labor?
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Prevention only. Progesterone receptor modulator decreases estrogen-mediated enhancement of oxytocin-induced contractions. Prophylaxis in women with history of PTL. Intramuscular / vaginal delivery.
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To avoid 1st pass effect in hormone replacement therapy, other admin options include:
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transdermal patch (less gallstones/VTE), creams (local only), rings (systemic)
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Types of progesterone used in HRT:
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MPA (medroxyprogesterone acetate), drospirenone (aldosterone antagonist), micro-ionized progesterone
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Types of progestin used in HRT:
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Androgenic progesterone: norethindrone, levonorgestrel
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Common side effects of progesterone HRT
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Hirsutism, "spotting", abnormal bleeding, weight gain, HTN
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Treatment for irregular menses and anovulation due to obesity.
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Oral contraceptives (likely has PCOS); no DepoProvera due to hirsutism (probably already bad)
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Treatment for 40 y/o w/ irregular menses, DM, HTN, normal TSH/FSH/pap/us/endometrial biopsy.
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Loevonorgestrel (not estrogen, may have vascular disease and endothelial damage- Virchow's Triad)
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1st line SERM for ER+ breast cancer
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Tamoxifen
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MOA for Tamoxifen
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Metabolized by cyp2D6 to more bioactive metabolite with high affinity for ERα & Erβ receptors. Binds co-repressor in breast/hypothalamus and co-activator in blood/uterus.
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Agonist/Antagonist effects of Tamoxifen
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Antagonist at breast / hypothalamus (hot flashes). Agonist at blood (VTE, clot) / uterus (endometrial hyperplasia). Partial agonist in bone (blocks resorption).
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Use for Toremifene
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Acts like Tamoxifen (ER receptor agonist/antagonist) more active than its metabolites (does not need cyp activation.) - Used in Tamoxifen resistant cancer.
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Raloxifene Use
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Breast cancer prevention (primary or reoccurence) (1st line in osteoporosis for agonist action in bone)
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Raloxifene vs. Tamoxifen
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Raloxifene is antagonist in uterus- no endometrial hyperplasia (no longterm risk of endometrial cancer) and more potent bone agonist (increases bone mass)
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Action of Aromatase Inhibitors
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Block action of aromatase enzyme in converting androstenedione to estrogen.
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Aromatase Inhibitors indicated in what type of patient
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Postmenopausal women (1st line for Stage III)
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MOA for Anastrazole
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Reversible Aromatase Inhibitor
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MOA for Exemestane
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Irreversible Aromatase Inhibitor
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Major side effects of Exemestane
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Androgenic effects: build-up of substrate (androstenedione) unable to out-compete drug due to "suicide" mechanism
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MOA for Fulvestrant
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Competitive antagonist @ ER receptors
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Indication for Fulvestrant Use
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Alternative for postmenopausal women if SERM or aromatase inhibitors fail.
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Progestins in order of most to least androgenic
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Levonorgestrel > Norgestrel > Etonogestrel > Norethindrone > Desogestrel > Norgestimate/Norelgestromin > Drospirenone
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Least androgenic progestin
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Dropsirenone (Yasmin) (Spironolactone derivative)
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Tx for menorrhagia if estrogen contraindicated
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Oral MPA (medroxyprogesterone acetate), Norethindrone minipill, Levonorgestrel IUS
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Fertility Tx for male hypothalamic hypogonadism
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Clomiphene citrate, hCG injections, IVF
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MOA for infertility drugs: Clomiphene citrate, Anastrozole/Letrozole
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Estrogen receptor antagonist, aromtase inhibitor. Block estrogen action on hypothalamus, increasing FSH production in HPO axis.
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MOA for infertility drugs: Gonadotropins
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FSH/LH increases, skipping HPO axis, leads to multiple gestations
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MOA for infertility drugs: hCG
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Triggers ovulation
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Prostate therapies
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GnRH antagonist (degarelix), GnRH agonist (leuprolide), androgen synthesis inhibitors (aminoglutethimide, ketoconazole), aromatase inhibitor, 5-alpha reductase inhibitor (finasteride), androgen receptor antagonist (flutamide)
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Doxazosin MOA (Terazosin, alfuzosin)
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α1-adrenergic receptor antagonist, relax prostate smooth muscle (symptomatic relief)
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Tamsulosin MOA
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Selective alpha-1A antagonist, less hypotension, nasal congestion
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Finasteride MOA
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5alpha-reductase inhibitor (Finasteride- selective, Dutasteride- nonselective); decrease serum PSA, impotence/libido, rare inc. of male breast cancer
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AE of Aminoglutethimide
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Hypothyroidism, hyperlipidemia
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Flutamide MOA
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DHT receptor antagonist in prostate; gynecomastia, libido drop, hepatix dysfunction
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Degarelix MOA
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GnRH antagonist, shuts down LH/FSH w/o testosterone spike (better for adv. Stage)
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Nitric oxide MOA
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Goes into smooth muscle cells of penis and stimulates production of cGMP: erection
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PDE5 MOA
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causes breakdown of cGMP leading to contraction of smooth muscle: decreased blood flow in / increased blood flow out.
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Viagra MOA
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PDE5 inhibitor; inc. cGMP levels, delays tumesences (Cialis, Levitra)
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Direct vasodilators MOA
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PGE1 (Caverject, Edex) or Papavarine, direct injectables into penis
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