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17 Cards in this Set
- Front
- Back
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What are:
Anastrozole Exemestane |
aromatase inhibitors used in postmenopasual women with breast cancer.
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Mifepristone?
- aka? - mech? - uses? coadmined with what? - tox? |
RU-486
- competitive inhibitor of progestins at progesterone receptors. - termination of pregnancy, admined with misoprostol (PGE1) - heavy bleeding, GI effects, abdominal pain |
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Which of the SERM's works on bone too?
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Raloxifene, it's an agonist on bone, reduces resorption of bone, used to tx osteoporosis.
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Clomiphene?
- uses? (2) - weird potential toxicitiy? |
partial agonist at E receptors in hypothalamus... prevents normal feedback inhibition -> ^^FSH/LH pituitary release --> stim ovulation.
- tx infertility and PCOS. - may cause mult simulatneous pregnancies, visual disturbances, hot flashes, and ovarian enlargement. |
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Contraindications to Estrogen (Ethinyl estradiol, DES, mestranol) use?
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ER (+) breast cancer, history of DVT.
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Finasteride mech?
- uses |
inhib 5-a-reductase
- BPH, male pattern baldness. |
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Flutamide mech?
- uses? |
nonsteroidal competitive inhibitor fo androgens at the testosterone receptor.
- prostate carcinoma |
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What two drugs are used in the tx of PCOS to prevent hirsuitism?
- common side effects? - mech? |
Ketoconazole and Spironolactone
- gynecomastia, amenorrhea. - Ketoconazole inhibits P450 which is necessary for Testosterone production (M and F). |
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Why can Ketoconazole be used to inhibit Testosterone?
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it inhibits P450 system enzyme desmolase.
.... which is needed for the FIRST step in steroid synthesis, a cleavage of cholesterol side-chains. |
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How does spironolactone exert antiandrogen action?
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inhibits binding, and also has a small effect on synthesis.
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Exogenous Testosterone toxicity in males?
- lipid effects? |
Reduces intratesticular T by inhibiting LH release... --> gonadal atrophy. also premature closure of epiphyseal plates.
- ^^LDL, \\HDL (opposite of estrogen) |
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Leuprolide does what?
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GnRH analog with agoinst propertes when used in pulsatile fashion, agonist properties when used continuously.
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advantages of OCP?
Disadvantages? |
\\endometrial cancer, \\ovarian cancer... \\ectopic preg... \\pelvic infections.
^^TG, depression, WG, nausea, HTN; hypercoagulable state. |
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Dinoprostone
- mech? |
PGE2 analog causing cervical dilation and uterine contraction --> inducing labor
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Ritodrine
Terbutaline |
B2 agonists that relax the uterus, reduce premature uterine contractions ("return to dreams" = ritodrine)
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Tamsulosin
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a1-antagonist used to tx BPH by inhibiting smooth muscle contraction. Selective for a-1a,d receptors (on prostate) vs vascular a-1b receptors.
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Sildenafil
vardenafil mech? - tox? |
inhibit cGMP phosphodiesterase, causing ^^ cGMP --> smooth muscle relaxtion.
- HA, flushing, dyspepsia, impaired blue-green color viz, risk of life-threatening hypotension in pts taking nitrates. |
