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Pharmacology > EXAM #5: ANDROGENS, ANTIANDROGENS, ED > Flashcards

EXAM #5: ANDROGENS, ANTIANDROGENS, ED Flashcards

1
Q

Where is Testosterone synthesized?

A

1) Leydig cells of the Testes (de novo)

2) Adrenal cortex (low potency androgens that get converted)

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2
Q

What does the hypothalamus produce in the synthetic pathway of the androgens?

A

GnRH

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3
Q

What does they pituitary produce in the synthetic pathway of the androgens?

A

LH and FSH

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4
Q

What is the function of LH?

A

1) LH binds Leydig cells in testes
2) Induces the production and secretion of testosterone
3) Testosterone diffuses into the Sertoli cells

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5
Q

What is the function of Testosterone in the Sertoli cells?

A

Stimulation of spermatogenesis

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6
Q

What is the function of FSH?

A
  • Induces the synthesis of Androgen Binding Protein (ABP) by Sertoli cells
  • ABP concentrates Testosterone at the site of spermatogenesis in the Sertoli cells
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7
Q

Describe Testosterone’s feedback in the HPA axis.

A

Testosterone directly inhibits:

1) LSH and FSH from pituitary
2) GnRH from hypothalamus

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8
Q

What is the function of 17a-hydroxylase in the synthesis of the androgens?

A

Converts androstenedione to testosterone

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9
Q

What is the function of 5a-reductase in the synthesis of androgens?

A

Converts testosterone to DHT

*Note that DHT will inhibit the secretion of GnRH and LH

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10
Q

What are the two general effects of the androgens?

A

1) Androgenic

2) Metabolic effects

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11
Q

What are the “androgenic” effects of the androgens?

A
  • Growth/ development of male reproductive tract

- Male secondary sex characteristics

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12
Q

What are the metabolic effects of the androgens?

A

Actions on non-reproductive tissue e.g.

  • Muscle growth
  • Liver production of serum proteins
  • Kidney, stimulates EPO
  • Bone growth
  • Bone marrow stem cell production
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13
Q

What are the three therapeutic androgen preparations?

A

Methyltestosterone
Testosterone enanthate
Testosterone

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14
Q

What is the problem with oral Testosterone? How is this combated?

A

Low bioavailability b/c it undergoes extensive first pass metabolism

Administered topically in a gel or transdermal patch

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15
Q

Structurally, how does Testosterone Enanthate differ from Testosterone?

A

Fatty acid conjugated to Testosterone via an ESTER bond

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16
Q

How is Testosterone Enanthate administered?

A

Dissolved in oil and administered IM

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17
Q

What is the colloquial name for 17-alkylated derivatives of Testosterone?

A

Anabolic steroids

This was an attempt to make a drug with METABOLIC effects and without androgenic effects

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18
Q

What is the hallmark 17-alkyated testosterone derivative?

A

Methyltestosterone

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19
Q

How is Methyltestosterone administered?

A

Orally, undergoes less first pass metabolism than Testosterone

20
Q

What adverse effects are associated with androgen therapy?

A
  • Reduction in spermatogenesis and testis size
  • Acne
  • Polycythemia
  • Prostatic enlargement
  • Na+/ H20 retention–> HTN
  • Increased LDL and decrease HDL–>atherosclerosis
  • Mood swings, depression, aggression
21
Q

What is the theraputic use of antiandrogens in females?

22
Q

What are the therapeutic uses for antiandrogens in males?

A

1) Percocious puberty
2) BPH
3) Prostate cancer
4) Alopecia

23
Q

What are the androgen receptors antagonists?

A

Flutamide and Biclatumide

24
Q

What is the MOA of the androgen receptor antagonists?

A

Competitive antagonists of the androgen receptor

25
What is the clinical indication for the androgen receptor antagonists?
Prostate cancer
26
What toxicities are associated with the androgen receptor antagonists?
- Gynecomastia | - Mild liver toxicity
27
What drugs are commonly added to Flutamide and Biclatumide therapy? Why?
Androgen receptor blockade increases LH secretion from the pituitary gland; thus, increase Testosterone *Given with a GnRH analog*
28
What is the MOA of Enzalutamide?
Competitive androgen receptor antagonist that ALSO: 1) Inhibits nuclear translocation of the androgen receptor 2) Blocks DNA binding 3) Blocks transcriptional coactivator recruitment
29
List the GnRH agonists.
Leuprolide | Goserelin
30
What are the clinical indications for GnRH agonists?
Prostate cancer
31
What is the MOA of the GnRH agonists?
Constantly elevated GnRH: 1) Desesitizes receptors on pituitary gonadotrophs 2) Decreases LH production and secretion 3) Decreases Testosterone
32
What is the major adverse effect of GnRH agonists in the treatment of prostate cancer?
Testosterone surge that can cause growth of the cancer
33
How is the Testosterone surge with GnRH agonists prevented in the treatment of prostate cancer?
AR receptor antagonist coadministration (Flutamide or Bicalutamide)
34
What is the hallmark GnRH antagonist?
Degarelix
35
What are the advantages of Degarelix in the treatment of prostate cancer?
1) Faster onset | 2) No LH/ Testosterone surge
36
What class of drug is Abiraterone?
Androgen biosynthetic inhibitor
37
What is the clinical indication for Abiraterone?
Metastatic prostate cancer
38
What is the MOA of Abiraterone?
Inhibits 17a-hydroxylase
39
List the 5a-reductase inhibitors.
Finasteride | Dutasteride
40
What are the clinical indications for 5a-reductase inhibitors?
BPH | Alopecia
41
How do 5a-reductase inhibitors treat alopecia?
- High DHT is thought to cause alopecia by inducing apoptosis of dermal papilla - 5a-reductase inhibitors prevent formation of DHT from Testosterone
42
What are the adverse effects associated with the 5a-reductase inhibitors?
1) Impotence 2) Gynecomastia 3) LOWER PSA levels leading to FALSE NEGATIVE testing
43
What is the function of PDE-5 in the penile erection?
Converts cGMP to 5'GMP *cGMP is needed for smooth muscle relaxation and erection*
44
List the PDE-5 inhibitors. What are these drugs clinically indicated for?
Sildenafil Vardenafil Tadalafil 1) ED 2) Pulmonary arterial HTN
45
How does Tadalafil differ from SIldenafil and Vardenafil?
- Double the time to peak concentration | - Half-life of 18 hours
46
What is a contraindication of PDE-5 inhibitors?
HIV protease inhibitors and Nitrates (can lead to hypotension) *CYP 3A4 effects INCREASE efficacy of PDE-5
47
What adverse effects are associated with PDE-5 inhibitors?
1) Cardiac events 2) Priapism 3) Sudden vision loss (blood flow to optic nerve blocked)

Pharmacology (64 decks)

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