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Phar 441 > Sex Steroids > Flashcards

Sex Steroids Flashcards

1
Q

Which enzyme converts testosterone to dihydrotestosterone?

A

5-alpha-reductase

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2
Q

What is the function of Aromatase?

A

Convert testosterone to estradiol

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3
Q

Which tissues are dihydrotestosterone active in?

A

Hair follicles
Prostate
Skin

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4
Q

In which tissues are testosterone converted to estradiol?

A

Bone - termination of bone growth; maintenance of bone density
Gonads - gonadotropin regulation

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5
Q

What is the action of androgen in bone?

A

Increases linear bone growth; also role in termination of bone growth and maintaining bone density

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6
Q

What is the function of androgen in kidney?

A

Stimulates erythropoietin production - men have higher hematocrit than women

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7
Q

Testosterone is converted to DHT before or after entering the cell?

A

After entering the cell

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8
Q

After testosterone binds to androgen receptors in the cytoplasm, what happens next?

A
  • Dissociation of corepressor
  • Dimerization
  • Translocation into nucleus
  • Binding to androgen response element
  • Interaction with coactivators
  • Altered regulation of target genes
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9
Q

What is late-onset hypogonadism (LOH)?

A

Characterized by symptoms and a deficiency in serum testosterone (Both required for diagnosis)

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10
Q

What are some uses of androgen in therapy?

A
  • Androgen Replacement Therapy
  • Delayed growth and puberty in males due to true hypogonadism or constitutional delay
  • Catabolic or muscle wasting conditions - AIDS patients (must be male)
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11
Q

How is testosterone ester administered?

A

It is a depot preparation administered IM every 2-4 weeks

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12
Q

How does testosterone undecanoate bypass first pass metabolism?

A

It is absorbed into lymphatic system and not through the blood

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13
Q

Explain structure of Methyltestosterone. How is it different from other androgens?

A

17-alpha-alkylated androgen

It is resistant to hepatic breakdown however it can cause hepatotoxicity and therefore not recommended.

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14
Q

Why are anabolic steroids dangerous to use?

A

Most are 17-alpha-alkylated androgens so there’s a risk of hepatotoxicity.

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15
Q

Name 2 androgen preparations that have higher anabolic activity.

A

Oxymetholone, Nandrolone decanoate

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16
Q

What are the adverse effects of androgens?

A

Suppression of spermatogenesis; testicular atrophy; Decreased HDL, increased LDL; Gynecomastia; Increased aggression

17
Q

What is the mechanism of non-steroidal anti-androgens?

A

Competitive antagonists - prevents binding of androgen to its receptor. Blocks androgen actions in target tissues.

18
Q

Why does non-steroidal anti-androgens cause increase in testosterone production?

A

No negative feed back because androgens are not binding to receptors

19
Q

Name 3 non-steroidal anti-androgens.

A

Flutamide, bicalutamide, nilutamide

20
Q

Which class does cyproterone acetate belong to?

A

Steroidal anti-androgen

Androgen receptor antagonist

21
Q

How does cyproterone work? And what is it’s main use?

A

Competitive antagonist at androgen receptors but also progesterone activity. It blocks gonadotropin secretion. Uses include treatment of severe cystic acne.

22
Q

Name some 5-alpha-reductase inhibitors.

A

Finasteride, Dutasteride

23
Q

Which 5-alpha reductase inhibitor inhibit both Type 1 and Type 2 aromatase?

A

Dutasteride

24
Q

Which type of aromatase inhibitor is most concentrated in the prostate and genitals?

A

Type 2

25
Q

5AR inhibitors are used in BPH and often in conjunction with what other agent?

A

Alpha-blockers; faster onset but don’t decrease risk of complications

26
Q

5AR inhibitors treat BPH by:

A

Decreasing size of prostate and improving urinary flow and symptoms
Decreasing risk of long term complications by 50% (i.e. urinary retention and surgery)

27
Q

Which 5AR inhibitor is approved for use in androgenic alopecia?

A

Finasteride

28
Q

What is the effect of 5AR inhibitor on prostate cancer?

A

-Both drugs shown to reduce risk of prostate cancer but increase risk of serious prostate cancer

Phar 441 (5 decks)

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