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Flashcards in Male Urogenital Pharm - Fitz Deck (14)
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Describe hormones in the H-P-Testes axis and what they do (GnRH, FSH, LH, T, E, DHT)

- GnRH --> FSH and LH (pulsatile)
- LH --> Leydig cells --> testosterone production (pulsatile)
- FSH + Testosterone --> Sertoli cells --> Sperm
- Aromatase (sertoli cells) converts some testosterone to estradiol
- 5-alpha reductase (leydig cells) convert some testosterone to DHT


What enzyme is required to turn Androstenedione into Testosterone OR Estradiol?

17-beta hydroxylase


Feedback inhibition of H-P-T axis

Testosterone (androgens) AND Estradiol both cause inhibition at hypothalamus and pituitary


Molecular indicator of potential prostate cancer

Prostate cancer grading system

PSA level

Gleason Scale (1-10)


First line therapy for slowing/stopping the growth of prostate cancer

Androgen deprivation


3 GnRH-related drugs used for fertility issues /prostate cancer

Gonadorelin (natural GnRH)
Leuprolide (agonist)
Degarelix (antagonist)


After administering Leuprolide, what will you see?

Why does this happen?

Initial surge of FSH, LH, and testosterone, followed eventually by down-regulation of the GnRH receptor and decreased hormone levels

Not PULSATILE like it normally is


What are other potential issues w/ Leuprolide/testosterone that must also be managed?

Adrenals OR tumor cells may make their own testosterone, thus not allowing for sufficient androgen deprivation


How are the Leuprolide testosterone surge and other testosterone productions managed?


Molecular result?

Androgen receptor antagonists


No dimerization, transport, or transcription by androgen receptor


Abiraterone - MoA

Used for what?

What else is important? Why?

Inhibits 17-alpha hydroxylase AND 17, 20-lyase (CYP17), thus preventing testosterone production

Androgen deprivation in prostate tumor cells

Must be given w/ PREDNISONE or other corticoids -- CORTISOL production is also inhibited and ALDOSTERONE accumulates


How is Ketoconazole different than Abiraterone?

Difference in findings/side effects?

Ketoconazole -- also blocks pregnenolone production from cholesterol

NO aldosterone accumulation


When is Ketoconazole used?

With what else?

Side effect?

Men with advanced prostate cancer that need prompt drops in testosterone levels

Corticosteroid (cortisol replacement)



What is Finasteride? What is it used for? Can it be used for prostate cancer?

- 5-alpha reductase inhibitor
- NO -- may increase growth of the cancer (according to studies)


A male patient has a low sperm count, and LH/FSH levels are low. Cause?

Want to stimulate spermatogenesis in the short term. Tx?

Issue with this?

Better way to Tx?

2º hypogonadism -- Exogenous steroids not taken in pulsatile way

Beta-hCG = acts like LH but w/ longer 1/2 life

Testosterone will still cause negative feedback on the system

Clomiphene (ER antagonist) or Anastrozole (aromatase inhibitor) --> cause loss of negative feedback by estradiol --> causing increased GnRH