Updated: 2/12/2018

Antiandrogens

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Topic
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Questions
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Evidence
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Finasteride
  • Mechanism
    • 5α-reductase inhibitor
      • ↓ conversion of testosterone to dihydrotestosterone
  • Indications
    • BPH
    • male-pattern baldness
      • both hairloss and prostate hyperplasia are DHT driven processes
Flutamide
  • Mechanism
    • testosterone receptor blocker
  • Indications
    • prostate carcinoma
Ketoconazole
  • Mechanism
    • steroid synthesis inhibitor
      • inhibits desmolase 
    • used at higher doses than as an anti-fungal
  • Indications
    • PCOS
      • specifically the symptoms of hirsutism
    • androgen receptor-positive prostate cancer
  • Toxicity
    • gynecomastia, amenorrhea
Spironolactone
  • Mechanism
    • inhibits steroid binding
  • Indications
    • PCOS
      • specifically the symptoms of hirsutism
    • K-sparing diuretic
  • Toxicity
    • gynecomastia, amenorrhea
 

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Questions (4)
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(M1.RP.15.75) A 19-year-old South Asian male presents to the family physician concerned that he is beginning to go bald. He is especially troubled because his father and grandfather "went completely bald by the age of 25," and he is willing to try anything to prevent his hair loss. The family physician prescribes a medication that prevents the conversion of testosterone to dihydrotestosterone. Which of the following enzymes is inhibited by this medication? Tested Concept

QID: 106838
1

Desmolase

2%

(1/55)

2

Aromatase

9%

(5/55)

3

5-alpha-reductase

87%

(48/55)

4

cGMP phosophodiesterase

0%

(0/55)

5

Cyclooxygenase 2

2%

(1/55)

M 1 D

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(M1.RP.13.14) A 75-year-old male is diagnosed with advanced metastatic prostate cancer. After further evaluation and staging, the patient is started on flutamide therapy. Addition of which of the following medications to this patient’s medication regimen would be of greatest benefit in the treatment of this patient’s condition? Tested Concept

QID: 100315
1

Leuprolide

70%

(107/152)

2

Anastrozole

11%

(17/152)

3

Clomiphene

4%

(6/152)

4

Tamoxifen

7%

(10/152)

5

Cyproterone

5%

(8/152)

M 3 E

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(M1.RP.13.60) A 57-year-old presents to your clinic complaining of baldness. He is overweight, has been diagnosed with BPH, and is currently taking atorvastatin for hyperlipidemia. The patient has tried several over-the-counter products for hair-loss; however, none have been effective. After discussing several options, the patient is prescribed a medication to treat his baldness that has the additional benefit of treating symptoms of BPH as well. Synthesis of which of the following compounds would be expected to decrease in response to this therapy? Tested Concept

QID: 100361
1

GnRH

6%

(7/113)

2

DHT

69%

(78/113)

3

LH

1%

(1/113)

4

Testosterone

17%

(19/113)

5

FSH

3%

(3/113)

M 3 E

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Evidence (5)
Topic COMMENTS (10)
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