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36 Cards in this Set
- Front
- Back
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Estrogen receptor agonists
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Estradiol, esters, estrone, conjugated estrogens. Synthetic-diethylstilbestrol (lipophilic and teratogen)
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Semi-synthetic estrogen agonists
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17-ethinylestradiol and mestranol.
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Estrogen agonists/antagonists
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xenoestrogens, pytoestrogens, environmental estrogens
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Estrogen receptor antagonist
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Clomiphene0useful for anovulatory infertility treatment. Tamoxifen-useful for estrogen dependent cancer
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Aromatase Inhibitors
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anastrozole, exemestane, and letrozole
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Raloxifene
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selective estrogen receptor modulator. Selective affinity for sublasses of estrogen receptors. Raloxifene is useful for maintaining bone mass post-menopausally without extreme stimulation of breast tissue
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Progesterone receptor agonists
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Natural-progesterone
Semi-syn- Medrosyprogesterone and derivatives Syn-19-nortestosterones |
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In terms of efficacy and everything else, describe the evolution of progestin drugs through the generations
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increasing potency and decreasing androgenic effect
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Progesterone Receptor Antagonist
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Mifepristone (RU486). Inhibits uterine quieting effect. Use in cushing's, glaucoma, OB/Gyn.
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Danazol
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Antigonadotropin derived from androgens and exerts negative feedback on the pituitary. Impeded androgen modification. Side note. Old women are a good source of gonadotropins.
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GnRH analons.
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Gonadorelin, leuprolide, nafarelin, goserelin
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How do you give GnRH analogs specifically.
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Pulsatile. Pump every 90minutes to mimic and continuously to block. Mimic is helpful to kickstart puberty and continuous is useful for prostatic cancer, endometriosis, and precocious puberty.
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The inhibition of ovulation and the cardiovascular side effects are both attributed to what component of oral contraceptives.
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The estrogenic one.
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What are bi and triphasics OC's
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They are meant to more closely mimic the normal cycle.
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Mirena
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soft, flexible IUD that releases small amounts of hormone. It give you birth control you can count for 5 years.
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ParaGard (copper)
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Approved for 10 years. IUD that actually can remain active for 12 years.
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What are the pharmokinetics and ADME of OC's.
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Rapid, complete GI absorption. Minor first pass metabolism. Extensively protein bound.
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What are important drug interactions of OC's?
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Increase clotting factors by messing with anticoagulants. Lipid alterations by microsomal enzyme inducers. Increased TBG and total T4 by messing with broad spectrum antibiotics (messes with intrahepatic cycle???).
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Common side effects.
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Excess estrogen gives you Na and H20 retention. BIG ONES. Excess progestin think androgenic effects of 10-nortestosterones. Think of virilization.
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Serious side effects of OCs.
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Actually get reduced incidences in a lot of things but you also never give OC's in history of thromboembolism, hepatic dysfunction, estrogen dependet neoplasm., pregnancy, smoking. Relative contraindication is migraine, HTN, DM, epilepsy.
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What can bromocryptine do in OBGYN
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It can decrease the hyperprolactinemia and make pregnancy more common.
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In polycystic ovaries what would we give to promote pregnancy.
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Cycline OCs, clomiphene
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Topical estrogen is used in what condition that is restricting pregnancy.
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Unfavorable cervical mucus.
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With endometriosis what can we do to promote pregnancy?
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GnRH analogs.
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Clomiphene
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Used to treat feedback anomaly. It stimulates hypothalamus to produce GnRH. This is in anovulatory therapy.
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Oxytocics
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Stimulates uterine contraction. (Estrogens, PGs, oxytocin)
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Tocolytics
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Relax the uterus. (progesterone, B-agonists.
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Oxytocin
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Oxytocic drug. Milk EJECTION. In labor it facilitates contraction only when receptor density increases during pregnancy. Similar function to ADH and can have problems in severe cases. From paraventricular nucleus. Short plasma half life.
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Prostaglandins for pregnancy.
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Oxytocic agent. Steeper dose-response mechanism than oxytocin. Much earlier response during pregnancy than oxytocin. E2 is used for cervical softening. Misoprostol stimulates contractions.
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Ergot alkaloids (Ergonovine and methylergonovine
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Derived from fungus. Useful for headaches. Mainly used for post-partum bleeding control. Don't give in large doses b/c can cause too much constriction or for labor.
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Reasons to induce labor.
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Diabetes, prolonged pregnancy, htn, bleeding, preeclampsia.
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Reasons to not induce labor.
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Fetopelvic disproportion. Unfavorable presentation. Invasive cervical CA.
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MGSO4 use in pregnancy.
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Used for preeclampsia. relex uterus. Calcium gluconate reverses problems. with too much.
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B2 agonists in pregnancy.
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Ritodrine, terbutaline. Used for premature labor.
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Indomethacin, nifedifpine.
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Also used for premature labor.
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