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15 Cards in this Set

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For what and how is Leuprolide used?

What are its SEx?
Leuprolides is a GnRH analog.

Use pulsatile for infertility (mimetic)

Use continuous for prostate cancer (add flutamide)
SEx of leuprolide include antiandrogen symptoms, nausea and vomiting.
How does tstosterone affect the testicles? Bones?

How does testosterone affect lipids?
Testosterone will down regulate LH to cause gonadal atrophy.

Testosterone leads to premature closure of epiphyseal plates.
Testosterone --> increase LDL and decreased HDL.
What are the antiandrogens?
Finasteride (propecia) - 5-a-reductase inh

Flutamide - nonsteroidal cometitive inh of androgens at testosterone receptor

Ketoconazole - inh steroid syn (inh desmolase)

Spironolactone - inh steroid binding
What anti-androgens are used in Tx of PCOS?
PCOS Tx: spironolactone and ketoconazole as they have SEx of amenorrhea and gynecomastia.
For what conditions are the following drugs used?
- Finasteride
- Flutamide
Finasteride - BPH, male-pattern baldness (prevents test--> DHT)

Flutamide - used in prostate carcinoma (inh androgens at test receptor)
DES exposure
DES exposure --> clear cell cancer of vagina
What are the SERMS?

How are they different?
SERMS - clomiphene, tamoxifen, raloxifne
Clomiphene - partial agonist of estrogen receptors at hypothalamus (decreased LH and FSH release)

Tamoxifen - antagonist on breast tissue (for ER-positive breast cancer)

Raloxifene (like tamoxifen but with more bone effects, anti-osteoporotic)
Why is anastrozole or exemestane useful for Tx of breast cancer?
Anastrazole and exemestane are aromatose inhibitors. They inhibit the conversion of androstenedione to estrogen at the granulosa cell. Thus, they are beneficial in Tx of estrogen dependent breast cancer (older women).
Mifepristone
Mifepristone = RU 486
- Competitive inh of progestins that is used for termination of pregnancy (along with misoprostol, a PGE1)
How do oral contraceptives affect lipids?
OCP's --> increased triglyceride
Dinoprostone
PGE2 analog used to dilate cervix and cause uterine contraction, for inducing labor.
Ritodrine and terbutaline
B2 agonists that relax the uterus, they reduce uterine contractions
Ritodrine allows the fetus to "return to dreams" by preventing early delivery.
A patient is having premature contractions that you want to delay. Should you reach for dinoprostone or ritodrine?

What other drug works?
Ritodrine and terbutaline are B2 agonists that reduce premature contractions.

Dinoprostone is a PGE2 analog that will induce labor.
Tamsulosin
Tamsulosin is an a1-agonist used to treat BPH by inhibiting SMC. It is selective for a1A,D receptor in prostate as opposed to a1B vascular receptors.
How are sildenafil and vardenafil used?

What is their mechanism?

What are their SEx?
Sildenafil and vardenafil inh cGMP phosphodiesterase, causing increased cGMP which relaxes SMC in corpus cavernosum.
Sildenafil and vardenafil fill penis.

SEx of sildenafil, vardenafil;
Hot and sweaty, but then headache, heartburn and hypotension (w/ nitrates)

Also, blue-green vision impairment.