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39 Cards in this Set

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