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22 Cards in this Set

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What 4 drugs are considered Antiandrogens?
-Finasteride
-Flutamide
-Ketoconazole
-Spironolactone
Finasteride:
-MOA?
-used for? (2)
A 5α-reductase inhibitor (↓ conversion of testosterone to dihydrotestosterone).

Useful in BPH. Also promotes hair growth––used to treat male-pattern baldness.
Flutamide:
-MOA?
-used for?
A nonsteroidal competitive inhibitor of androgens at the testosterone receptor.

Used in prostate carcinoma.
Ketoconazole and Spironolactone:
-MOA?
-used for?
Inhibit steroid synthesis

Used in the treatment of polycystic ovarian syndrome to prevent hirsutism
Sildenafil and Vardenafil:
-MOA?
Inhibit cGMP phosphodiesterase, causing ↑ cGMP, smooth muscle relaxation in the corpus cavernosum, ↑ blood flow, and penile erection.
Sildenafil and Vardenafil:
-clinical use?
Treatment of erectile dysfunction.
Sildenafil and Vardenafil:
-toxicity?
-C/I with what drugs?
Headache, flushing, dyspepsia, blue-green color vision.

Risk of life-threatening hypotension in patients taking nitrates.
Mnemonic for the MOA of Sildenafil and Vardenafil?
"SildenaFIL and VardenaFIL FILL the penis"
Leuprolide MOA?
GnRH analog with agonist properties when used in pulsatile fashion; antagonist properties when used in continuous fashion.
Clinical use of Leuprolide? (3)
-Infertility (pulsatile)
-Prostate cancer (continuous–– use with flutamide)
-Uterine fibroids.
Toxicity of Leuprolide? (3)
Antiandrogen, nausea, vomiting.
What happens when Leuprolide is used in a continuous fashion?
it causes transient initial burst of LH and FSH
MOA of Clomiphene?
A partial agonist at estrogen receptors in the pituitary gland.

Prevents normal feedback inhibition and ↑ release of LH and FSH from the pituitary, which stimulates ovulation.
Clinical use of Clomiphene?
Treatment of infertility.
Toxicity of Clomiphene? (4)
Hot flashes
Ovarian enlargement
Multiple simultaneous pregnancies
Visual disturbances.
MOA of Mifepristone (RU-486)?
Competitive inhibitor of progestins at progesterone receptors.
Clinical use of Mifepristone?
Abortifacient (prevents implantation).
Toxicity of Mifepristone? (3)
Heavy bleeding, GI effects (nausea, vomiting, anorexia), abdominal pain.
What are the advantages of oral contraception (synthetic progestins, estrogen)? (5)
Reliable (< 1% failure)
↓ risk of endometrial and ovarian CA
↓ incidence of ectopic pregnancy
↓ pelvic infections
Regulation of menses
What are the disadvantages of oral contraception (synthetic progestins, estrogen)? (5)
Taken daily
No protection against STDs
↑ triglycerides
Depression, weight gain, nausea, HTN
Hypercoagulable state
Use of Hormone Replacement Therapy (HRT)?
used for relief or prevention of menopausal symptoms (hot flashes, vaginal atrophy, etc.) and osteoporosis (due to diminished estrogen levels)
Risk of HRT? What can be used to decrease the risk?
unopposed estrogen replacement therapy (ERT) increases the risk of endometrial CA, so progesterone is added