Androgens -12 Flashcards

1
Q

Testosterone

  • testosterone is secreted by the ___
  • in men, there is a constant ___ of testosterone produced daily (95% ___ cells, 5% by adrenal glands)
  • testosterone plasma levels: men - ___ mcg/dL after puberty. women - ___ mcg/dL
  • circulating testoserone is bound to ___ (65%), ___ (33%), ___ (2%)
A
  • testis
  • 8 mg, Leydig
  • 0.6 mcg/dL, 0.3 mcg/dL
  • sex-hormone binding globulin (SHBG)
  • albumin
  • free
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2
Q

Regulation of testosterone synthesis

  1. the hypothalamus releases ___
  2. anterior pituitary releases ___ and ___
  3. LH triggers ___ cells in the testis to produce ___. FSH triggers ___ cells to produce ___.
  4. Testosterone is responsible for the development of sex organs and also inhibits the ___ and ___ through negative feed back.
A
  • GnRH (Gonadotropin-releasing hormone)
  • LH (luteinizing hormone) and FSH (follicle stimulating hormone), sperm
  • hypothalamus and anterior pituitary
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3
Q

Testosterone metabolism

  • in target tissues, testosterone is broken down into ___ by 5α-reductase
  • testosterone can also be broken down into ___ by aromatase
A
  • 5α-Dihydrotestosterone
  • 17β-Estradiol
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4
Q

T or F: 5α-Dihydrotestosterone is a more potent major active androgen

A

True

better binding/more activity than testosterone

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5
Q

Testosterone excretion

  • occurs in the ___
  • inactivated to ___ and ___
  • then conjugated and excreted to the ___
A
  • liver
  • androsterone and etiocholanolone
  • urine
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6
Q

Adrenal androgens

3 intermediates of testosterone
* ___, ___, and ___
* have ___ androgen effects
* large amounts produced in the ___

A
  • androstenedione, dihydroepiandrosterone (DHEA), dihydroepiandrosterone sulfate (DHEAS)
  • weak
  • adrenal glands
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7
Q

Physiologic effects

  • penile and scrotal growth
  • ___ and ___ skin
  • pubic, axillary, and beard hair
  • deepening of voice
  • skeletal growth followed by ___ closure
  • increase in lean body mass → positive ___ balance
  • stimulation and maintenance of sexual function
  • stimulation of ___ production
  • decrease in ___ levels
A
  • oily and thick
  • epiphyseal
  • nitrogen
  • erythrocyte
  • HDL
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8
Q

clinical uses

Androgen replacement therapy in men
* Male ____ (testosterone deficiency)
* Hypopituitarism - promote production of ___ to produce sperm

A
  • hypogonadism
  • FSH
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9
Q

clinical use

Gynecologic disorders
* endometriosis (___)
* replacement therapy for ___ women (in combo with estrogens) (controversial)
* eliminates ___ bleeding
* enhances ___

A
  • danazol
  • postmenopausal
  • endometrial
  • libido

must be used with great caution due to adverse effects

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10
Q

clinical use

Protein anabolic agents
* reverse ___ loss after trauma/surgery/prolonged immobilization. Promotes ___ growth.

  • can also be used for ___pause
A
  • protein
  • andropause
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11
Q

Synthetic androgens

  • when administered ___, testosterone is readily absorbed but largely ___.
  • ___ forms are more active orally. Example: ___
  • ___ forms have prolonged absorption time and greater activity for intramuscular administration. Examples: ___, ___, and ___
A
  • orally, inactivated
  • 17-alkyl, methyltestosterone
  • ester, propionate, enanthate, cypionate
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12
Q

Anabolic steroids in sports

  • doses ___ times larger than the daily normal production
  • harmful changes in ___ levels
  • acne
  • high ___
  • hepatic dysfunction in case of ___ steroids
  • large doses of anabolic steroids suppress the secretion of ___ → testicular ___
A
  • 10-200
  • cholesterol
  • high blood pressure
  • 17-alkyl
  • gonadotropins, atrophy
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13
Q

Adverse effects in women

A
  • hirsutism
  • acne
  • amenorrhea
  • clitoral enlargement
  • deepening of voice
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14
Q

Adverse effects in men

A
  • acne
  • sleep apnea
  • gynecomastia
  • azoospermia and testicular atrophy
  • increased aggresiveness adn psychotic symptoms
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15
Q

Antiandrogens

___ inhibitors
* block the conversion from testosterone to 5α-dihydrotestosterone.

A

5α-reductase

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16
Q

Antiandrogens

Androgen receptor inhibitors
* block the binding of ___ androgens or inhibit the activation of the ____
* steroidal and non-steroidal inhibitors

A
  • endogenous
  • receptors
17
Q

5α-reductase inhibitors

Finasteride
* Proscar: used to treat ___
* Propecia: used to treat ___
* for women: ___

A
  • benign prostatic hyperplasia
  • male pattern baldness
  • hirsutism
18
Q

5α-reductase inhibitors

Dutasteride
* used for ___ and ___

A

BPH and male pattern baldness

19
Q

Steroidal androgen receptor inhibitors

Cyproterone and cyproterone ester
* for women: ___
* for men: ___

A
  • hirsutism
  • excessive sexual drive
20
Q

Steroidal androgen receptor inhibitors

Spironolactone
* for women: ___
* ___ (in pup this was not an FDA approved use)

A
  • hirsutism
  • acne
21
Q

Non-steroidal androgen receptor inhibitors

Flutamide
* ___ anti-androgen used for ___

A

non-steroidal, prostate cancer

22
Q

Non-steroidal androgen receptor inhibitors

Enzalutamide
* ___anti-androgen used for ___

A

non-steroidal, Metastatic castration-resistant prostate cancer

23
Q

What is this?

A

5a-dihydrotestosterone

24
Q

What is this?

A

17B-Estradiol

25
Q

What is this?

A

Androstenedione

26
Q

What is this?

A

Androsterone

27
Q

What is this?

A

Cyproterone

28
Q

What is this?

A

Dihydroepiandrosterone (DHEA)

29
Q

What is this?

A

Dihydroepiandrosterone Sulfate (DHEAS)

30
Q

What is this?

A

Dutasteride

31
Q

What is this?

A

Enzalutamide

32
Q

What is this?

A

Finasteride

33
Q

What is this?

A

Flutamide

34
Q

What is this?

A

Methyltestosterone

35
Q

What is this?

A

Spironolactone

36
Q

What is this?

A

Testosterone

37
Q

What is this?

A

Testosterone cypionate

38
Q

What is this?

A

Testosterone enanthate