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26 Cards in this Set
- Front
- Back
Leuprolide
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MOA = GnRH analog
agonist when pulsatile fashion antagoinst properties when used in continuous fashion Use Pulsatile = infertility Continuous = prostate cancer w/ flutamide Uterine fibroids Toxicity = Antiandrogen, nausea, vomiting |
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Testosterone
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MOA = act at androgen receptors
USE = - hypogonadism - promote development of 2ndary sex characteristics - stimulate anabolism for recovery from burn or injury - treat ER-POSITIVE breast cancer (EXEMASTANE = aromatase inhibitor) |
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Testosterone toxicity
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- masculinization in females
- reduces intratesticular testosterone in males by inhibiting release of LH (via negative feedback) => GONADAL ATROPHY - premature closure of epiphyseal plates - Increase LDL and Decrease HDL |
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Finasteride (propecia)
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- 5 alpha-reductase inhibitor (dec converion of T to DHT)
- Used in BPH - Promotes hair growth = used to tx MALE-PATTERN BALDNESS |
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Flutamide
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- Nonsteroidal COMPETITIVE inhibitor of ANDROGRENS at testosterone receptor
- Used in PROSTATE CANCER |
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Ketoconazole and Spironolactone tx?
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Polycystic ovarian syndrome
- prevent HIRSUTISM - Side Fx = Gynecomastia and amenorrhea |
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Ketoconazole MOA
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- inhibits steroid synthesis (inhibits DESMOLASE)
- decrease androgen synthesis - side fx = gynecomastia and amenorrhea |
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Spironolactone MOA
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- Inhibits steroid binding to androgen receptor
- side fx = gynecomastia and amenorrhea |
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Estrogens
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- Ethinyl estradiol; DES; Mestranol
MOA = bind ESTROGEN receptors USE = - hypogonadism or ovarian failure - menstrual abnormalities - HRT in postmenopausal women - Men w/ androgen-dependent prostate cancer |
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Estrogen Toxicity
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- Increase risk of endometrial cancer
- bleeding in postmenopausal women - clear cell adenocarcinoma of vagina in females exposed to DES in utero - increasee risk of THROMBI |
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estrogen contraindications
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ER-positive breast cancer
history of DVTs |
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SERMs
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- Estrogen partial agonists
- Clomiphene - Tomoxifen - Raloxifene |
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Clomiphene
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SERM
- Partial agonist at Estrogen receptors in hypothalamus - Prevents normal feedback inhibition & inc release of LH and FSH from pituitary -> stimulates ovulation Use = - tx infertility and Polycystic ovarian Tox = - host flashes; ovarian enlargement; multiple simultaneous pregnancies; and visual disturbances |
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Tomoxifen
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SERM
- Antagonist on Breast Tissue - used to tx and prevent recurrence of ER-positive breast cancer |
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Raloxifene
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SERM
- AGONIST on BONE = reduces resorption of bone = used to tx osteoporosis - breast tissue antagonist actions therefore protection against Estrogen receptor |
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Hormone replacement therapy
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- relief or prevnetion of menopause symptoms (host flashes, vaginal atrophy)
- and osteoporosis (inc estrogen; dec osteoclast activity) - unopposed estrogen replacement therapy increase the risk of endometrial cancer, so progesterone is added - inc CV risk |
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Anastrozle
Exemestane |
- Aromatase inhibitors
used in postmenopausal women w/ breast cancer |
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Progestins
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MOA =
- Bind progesterone receptors - reduce growth and increase vascularization of endometrium Use = - oral contraceptives and in the tx of endometrial cancer and abnormal uterine bleeding |
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Mifepristone
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- RU-486
MOA = COMPETITIVE INHIBITORS of progestins at PROGESTERONE RECEPTORS Use = Termination of pregnancy - administered w/ MISOPROSTOL (PGE1) TOXICITY = - heavy bleeding - GI effects (nausea, vomiting, anorexia) - Abdominal pain |
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Oral contraceptives`
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- synthetic progestins and estrogen
- oral contraceptives prevent Estrogen surge - LH surge does not occur -> ovulation does not occur Decreases incidence of = - endometrial & ovarian cancer; incidence of ectopic pregnancy; and pelvic infxns Disadvantages = - inc TGs; Depression, weight gain, nausea, HTN; Hypercoagulable state |
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Contraindications of OCPs
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- smokers > 35 yrs (inc risk of CV events)
- Pts w/ hx of thromboembolism and - stroke or hx of estrogen-dependent tumor |
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Dinoprostone
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- PGE2 analog causing cervical dilation and uterine contraction
- induce labor |
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Ritodrine/
- terbutaline |
- Beta 2- agonists
- relax uterus - reduce premature uterine contractions Ritodrine allow the fetus to "Riturn to drines" |
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Tamsulosin
Prazosin, Terazosin, doxazosin |
- alpha 1-antagonists used to tx BPH by inhibiting smooth muscle contraction
Tamsulosin = selective for alpha-1A,D receptors (found on prostate) vs vascular alpha-1B receptors |
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Sildenafil
Vardenafil |
MOA = inhibit cGMP phosphodiesterase -> inc cGMP
- smooth muscle relaxation in the corpus cavernosum, inc blood flow, and penile erection Use = tx of erectile dysfxn |
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Sildenafil, vardenafil toxicity
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- headache, flushing, dyspepsia
- impaired blue-green color vision - risk of life-threatening HYPOTENSION in pts taking NITRATES - headache, heartburn, hypotension |