Prostate

Question 1

Abiraterone

Answer 1

Prostate
Androgen Synthesis Enzyme Inhibitor
MOA
- Inhibit enzymes of androgen synthesis (in Testes or Prostate Cancer)

Question 2

Finasteride, Dutasteride

Answer 2

Prostate
5α-reductase inhibitors
MOA
- inhibits 5a-reductatse
- inhibits transformation of TEST-->DHT
A/Es
- reduced libido, 
- erectile dysfunction 
- Gynecomastia

Question 3

Prazosin, Terzosin, Doxazosin, Alfuzosin, Tamsulosin, Silodosin

Answer 3

Prostate
α1-blockers (Antagonists)
- “-osin”
- Fxn: Smooth Muscle Contraction inhibition (ie dilation)
*α1A
- Location: non-vascular smooth muscle (majority = Human Prostate)
- prostate (capsule and urethra), bladder base and neck.
- Fxn: regulates smooth muscle tone
- 70% of a1-adrenergic receptors in prostate are a1A subtype:
a) Postsynaptic blockade.
b) Fxn: prostatic urethral resistance
*α1B
- Location: vascular smooth muscle
- Fxn: Regulates blood pressure (Activation = Contraction)
A/Es
- tiredness, dizziness, postural hypotension, retrograde ejaculation and floppy iris syndrome
- *Intra Operative Floppy Iris Syndrome (IFIS) = Cataract Sx-related. Can lead to *Blindness.

Question 4

Histrelin, Leuprolide, Goserelin, Triptorelin, Nafarelin

Answer 4

Prostate
GnRH Receptor Agonists 
Indications
- Infertility
- Endometriosis
- Precocious Puberty
- Prostate Cancer
MOA
- initially causes a flare of LH and FSH
- then down regulates and desensitizes
ADE
- *flare considered adverse bc also causes TEST flare

Question 5

Ganirelix,Cetrorelix, Degarelix

Answer 5

Prostate
GnRH Receptor Antagonists (Blockers)
Indications
- Infertility
- Endometriosis
- Precocious Puberty
- Prostate Cancer
MOA
- blocks GnRH receptor
-NO LH and FSH

Question 6

Tadalafil (Cialis)

Answer 6

Prostate
PDE-5 inhibitor
Therapeutic
- ED & BPH

Question 7

Enzalutamide, Flutamide, Bicalutamide, Nilutamide

Answer 7

Prostate
Anti-androgens (block androgen receptors)
- “-lutamide”
Indication
- should precede or be co-administered with GnRH/LHRH-AGONIST due to **testosterone flare.
MOA (Enzalutamide)
- acts on different steps in the androgen receptor signaling pathway.
- Enzalutamide has been shown to competitively inhibit androgen binding to androgen receptors and inhibit androgen receptor nuclear translocation and interaction with DNA.
- Indication:
a) *Tx PT w/ metastatic castration-resistant prostate cancer (mCRPC) who have previously received Docetaxel (Chemo).