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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?

A

Hirsutism

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
Q

What is the clinical indication for the androgen receptor antagonists?

A

Prostate cancer

26
Q

What toxicities are associated with the androgen receptor antagonists?

A
  • Gynecomastia

- Mild liver toxicity

27
Q

What drugs are commonly added to Flutamide and Biclatumide therapy? Why?

A

Androgen receptor blockade increases LH secretion from the pituitary gland; thus, increase Testosterone

Given with a GnRH analog

28
Q

What is the MOA of Enzalutamide?

A

Competitive androgen receptor antagonist that ALSO:

1) Inhibits nuclear translocation of the androgen receptor
2) Blocks DNA binding
3) Blocks transcriptional coactivator recruitment

29
Q

List the GnRH agonists.

A

Leuprolide

Goserelin

30
Q

What are the clinical indications for GnRH agonists?

A

Prostate cancer

31
Q

What is the MOA of the GnRH agonists?

A

Constantly elevated GnRH:

1) Desesitizes receptors on pituitary gonadotrophs
2) Decreases LH production and secretion
3) Decreases Testosterone

32
Q

What is the major adverse effect of GnRH agonists in the treatment of prostate cancer?

A

Testosterone surge that can cause growth of the cancer

33
Q

How is the Testosterone surge with GnRH agonists prevented in the treatment of prostate cancer?

A

AR receptor antagonist coadministration (Flutamide or Bicalutamide)

34
Q

What is the hallmark GnRH antagonist?

A

Degarelix

35
Q

What are the advantages of Degarelix in the treatment of prostate cancer?

A

1) Faster onset

2) No LH/ Testosterone surge

36
Q

What class of drug is Abiraterone?

A

Androgen biosynthetic inhibitor

37
Q

What is the clinical indication for Abiraterone?

A

Metastatic prostate cancer

38
Q

What is the MOA of Abiraterone?

A

Inhibits 17a-hydroxylase

39
Q

List the 5a-reductase inhibitors.

A

Finasteride

Dutasteride

40
Q

What are the clinical indications for 5a-reductase inhibitors?

A

BPH

Alopecia

41
Q

How do 5a-reductase inhibitors treat alopecia?

A
  • High DHT is thought to cause alopecia by inducing apoptosis of dermal papilla
  • 5a-reductase inhibitors prevent formation of DHT from Testosterone
42
Q

What are the adverse effects associated with the 5a-reductase inhibitors?

A

1) Impotence
2) Gynecomastia
3) LOWER PSA levels leading to FALSE NEGATIVE testing

43
Q

What is the function of PDE-5 in the penile erection?

A

Converts cGMP to 5’GMP

cGMP is needed for smooth muscle relaxation and erection

44
Q

List the PDE-5 inhibitors. What are these drugs clinically indicated for?

A

Sildenafil
Vardenafil
Tadalafil

1) ED
2) Pulmonary arterial HTN

45
Q

How does Tadalafil differ from SIldenafil and Vardenafil?

A
  • Double the time to peak concentration

- Half-life of 18 hours

46
Q

What is a contraindication of PDE-5 inhibitors?

A

HIV protease inhibitors and Nitrates (can lead to hypotension)

*CYP 3A4 effects INCREASE efficacy of PDE-5

47
Q

What adverse effects are associated with PDE-5 inhibitors?

A

1) Cardiac events
2) Priapism
3) Sudden vision loss (blood flow to optic nerve blocked)

Pharmacology (64 decks)

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