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26 Cards in this Set

  • Front
  • Back
Leuprolide
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
Testosterone
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)
Testosterone toxicity
- 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
Finasteride (propecia)
- 5 alpha-reductase inhibitor (dec converion of T to DHT)

- Used in BPH

- Promotes hair growth = used to tx MALE-PATTERN BALDNESS
Flutamide
- Nonsteroidal COMPETITIVE inhibitor of ANDROGRENS at testosterone receptor

- Used in PROSTATE CANCER
Ketoconazole and Spironolactone tx?
Polycystic ovarian syndrome

- prevent HIRSUTISM

- Side Fx = Gynecomastia and amenorrhea
Ketoconazole MOA
- inhibits steroid synthesis (inhibits DESMOLASE)
- decrease androgen synthesis

- side fx = gynecomastia and amenorrhea
Spironolactone MOA
- Inhibits steroid binding to androgen receptor

- side fx = gynecomastia and amenorrhea
Estrogens
- 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
Estrogen Toxicity
- 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
estrogen contraindications
ER-positive breast cancer

history of DVTs
SERMs
- Estrogen partial agonists

- Clomiphene
- Tomoxifen
- Raloxifene
Clomiphene
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
Tomoxifen
SERM
- Antagonist on Breast Tissue

- used to tx and prevent recurrence of ER-positive breast cancer
Raloxifene
SERM
- AGONIST on BONE = reduces resorption of bone = used to tx osteoporosis

- breast tissue antagonist actions therefore protection against Estrogen receptor
Hormone replacement therapy
- 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
Anastrozle

Exemestane
- Aromatase inhibitors

used in postmenopausal women w/ breast cancer
Progestins
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
Mifepristone
- 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
Oral contraceptives`
- 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
Contraindications of OCPs
- smokers > 35 yrs (inc risk of CV events)

- Pts w/ hx of thromboembolism and
- stroke or hx of estrogen-dependent tumor
Dinoprostone
- PGE2 analog causing cervical dilation and uterine contraction

- induce labor
Ritodrine/

- terbutaline
- Beta 2- agonists

- relax uterus

- reduce premature uterine contractions

Ritodrine allow the fetus to "Riturn to drines"
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
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
Sildenafil, vardenafil toxicity
- headache, flushing, dyspepsia

- impaired blue-green color vision

- risk of life-threatening HYPOTENSION in pts taking NITRATES

- headache, heartburn, hypotension