Male Sex Hormones Flashcards

1
Q

What is the most potent androgen?

A

5alpha-DHT

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2
Q

How potent is testosterone?

A

Moderately

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3
Q

What is the least potent androgen?

A

DHEA

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4
Q

At what age does plasma testosterone start to decline?

A

50

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5
Q

What enzyme converts testosterone to DHT?

A

5alpha-reductase

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6
Q

What % testosterone is unbound?

A

2%

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7
Q

What % testosterone is bound to SHBG?

A

65%

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8
Q

What % testosterone bound to albumin

A

33%

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9
Q

Where is testosterone converted to DHT?

A

Target tissues, not the blood since most is bound

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10
Q

Where is testosterone converted to estrodiol?

A

Adipose and liver

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11
Q

What enzyme converts testosterone to estrodiol?

A

Aromatase

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12
Q

What hormones bind to androgen receptor?

A

Testosterone and DHT

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13
Q

What is the co-activator of androgen receptor?

A

ARA70, must bind to receptor complex for androgen receptor to function

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14
Q

What are the physiological effects of testosterone?

A
  • Male sex drive and performance
  • Muscle mass inc
  • Penile and scrotal growth
  • Vocal cord thickening
  • Spermatogenesis
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15
Q

What are the physiological effects of DHT?

A
  • Inc facial and body hair
  • Acne
  • Scalp hair recession
  • Prostate enlargement
  • Skeletal growth and epiphyseal closure
  • Stimulate lean body mass
  • Stimulate erythropoietin and clotting factor production
  • Dec HDL
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16
Q

Are the effects of testosterone and DHT general or tissue specific?

A

Tissue specific

17
Q

What are some therapeutic uses of synthetic androgens?

A
  • Androgen replacement therapy for hypogonadism or aging males
  • Protein anabolic effects for catabolic disorders
  • Anemia via EPO
  • Anabolic steroids in athletes
18
Q

What are synthetic androgens?

A

Full androgen agonists can be esterified or alkylated

19
Q

Potency of esterified synthetic androgens?

A

Similar to testosterone

20
Q

Potency of alkylated synthetic androgens?

A

more pronounced anabolic properties so they are more specific for things like catabolic disorders

21
Q

What are the risks in male athletes associated with anabolic steroids?

A
  • Inhibit LH/FSH
  • Withdrawal=infertility (azoospermia)
  • Loss of libido/impotence
  • Feminization (T–>E)
  • Liver toxicity
  • CV toxicity
22
Q

What are the benefits in male and female athletes associated with anabolic steroids?

A

-Anabolic and EPO effects

23
Q

What are the risks in female athletes associated with anabolic steroids?

A
  • Inhibit LH/FSH
  • Menstruation effects
  • Anovular cycles/infertility
  • Loss of libido
  • Virilization
  • Liver tox
  • CV tox
24
Q

What is a drug used for synthesis inhibition/anti-androgen therapy?

A

Finasteride

25
Q

What is the MOA of Finesteride?

A

Competitive inhibition of 5alpha-reductase type II–>blocks DHT formation in prostate gland, reducing serum DHT levels by 70%

26
Q

What are the two 5alpha-reductase isoforms and where are they located?

A

Type I
-low expression in prostate, hair follicles. High in sebaceous glands (acne) and is only weakly inhibited by finasteride

Type II
-High expression in prostate, hair follicles, low in sebaceous glands, potently inhibited by finasteride

27
Q

What is finasteride approved for?

A
  • Benign prostatic hyperplasia (BPH)–>dec prostate volume because prostate enlargement is dependent on DHT formation via type II
  • Male pattern baldness: bald men have more DHT in hair follicles.
28
Q

What is an example of an androgen receptor antagonist?

A

Flutamide

29
Q

What is the MOA of flutamide?

A

Pure androgen receptor antagonist (prevents ARA70 binding?)

30
Q

What are the therapeutic uses of flutamide?

A
  • Hormone sensitive prostate cancer. Block DHT binding, reduce gene transcription and androgen effects on tumor growth
  • Precocious puberty
  • Female virilization (dev of male characteristics)