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Pharmacology II > Pituitary and Gonadal Hormones III > Flashcards

Pituitary and Gonadal Hormones III Flashcards

1
Q

Two cells located in the testis?

A

Sertoli

Leydig

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2
Q

Hypothalamic-Pituitary-testes axis :
LH produces what and in which cells?
FSH produces what and in which cells?

A

LH : Testosterone in Leydig cells
FSH : components needed for spermatogenesis (hormone binding protein/globulin or androgen binding protein) in Sertoli cells

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3
Q

Hypothalamic-Pituitary-testes axis :

Testosterone inhibits the release of what? (2)

A

GnRH

Gonadotropins

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4
Q

Sertoli cells produce what? (2) roles?

A

Inhibin : inhibits FSH release

Activin : stimulates FSH release

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5
Q

Testosterone is synthesized from which hormones? In which cells is it produced?

A

Free cholesterol
Pregnenolone
Leydig cells

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6
Q

What happens to testosterone adipose, liver and hypothalamus?

A

Converted to estradiol by aromatase

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7
Q

Where is testosterone degraded? Where is it secreted?

A

Liver

Urine

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8
Q

Testosterone is bound to what in circulation?

When it enters the cell, it is converted to what and with which enzyme?

A

Bound to SHBG
Converted into dihydrotestosterone
5a-reductase

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9
Q

Is dihydrotestosterone (DHT) and more potent or less potent agonist of the androgen receptor?

A

More potent

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10
Q

After testo. is converted to DHT and binds to receptor, what happens and where does it do?

A

Ligand-receptor dimerizes and translocates to nucleus to initiate transcription

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11
Q

What is the final action of testosterone (DHT) once it initiates transcription?

A

Induces metabolic changes:

  • Increase lean body mass
  • Increase liver synthesis of clotting factors
  • Decrease HDL and hormone binding protein
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12
Q

3 clinical uses of androgens?

A 
Male hypogonadism (low testosterone)
Osteoporosis
Postpartum reduction of breast, endometriosis and postmenopausal hormone replacement in women
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13
Q

Two types of male hypogonadism?

What are the symptoms? (4)

A
  1. Congenital
  2. Acquired
    Delayed sexual development, low sex drive, erectile dysfunction, mood disturbances
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14
Q

Do androgens have low or high bioavailability?

A

Low

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15
Q

3 examples of drugs involved in androgen replacement therapy? How are they administered?

A

Testosterone enanthate : IM injectable
Androderm : Transdermal patch
Striant : Buccal system

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16
Q

2 types of anabolic steroids?

A

Testosterone

Oxymetholone

17
Q

Androgen Suppression Therapy are effective in which cases? (6)

A 
Precocious puberty
Male pattern baldness
Hypersexuality
Transgender hormone therapy
Benign Prostate Hyperplasia
Prostate Cancer
18
Q

2 GnRH analogs?

What is the MOA (initially (1) and more long-term (3) )

A 
Nafarelin
Leuprolide
-Initially gonadotropin release is increased
-Receptors are desensitized
-Gonadrotropin release is decreased
-Release of testosterone is decreased
19
Q

How is leuprolide administered?

What is an undesirable effect and how is this treated?

A

As subcutaneous pellets
Undesirable initial flare (increase in testosterone)
AR antagonists are given until testosterone decreases

20
Q

Example of GnRH antagonist? Where does it act?

A

Degarelix

Blocks GnRH receptors

21
Q

What are the effects of Degarelix (GnRH antagonist)?

What disease does it treat?

A

Decreases gonadotropin release (decrease in testosterone levels)
-Advanced prostate cancer

22
Q

Does Degarelix cause an initial flare and increase in testosterone like GnRH agonists?

A

No

23
Q

2 Testosterone Synthesis suppressors?

A

Ketoconazole

Spironolactone

24
Q

High doses of Ketoconazole inhibit _____ and _____ hormone synthesis

A

Adrenal

Gonadal

25
Q

What is the MOA of ketoconazole?

A

Displaces DHT and estrogen from SHBP in plasma

26
Q

What is the MOA of spironolactone?

A

Inhibits testosterone synthesis by reducing 17a-hydroxylase activity
(Competes with DHT for AR binding)

27
Q

2 5a-reductase inhibitors?

A

5a-reductase

Finasteride

28
Q

MOA of 5a-reductase?

A

Converts testosterone to more potent DHT

29
Q

MOA of finasteride?

A

competes with testosterone for binding with 5a-reductase

30
Q

food-derived substances that could inhibit 5a-reductase?

A

Saw Palmetto berries

31
Q

2 androgen receptor antagonists?

A

Flutamide

Spironolactone

32
Q

MOA of flutamide?

Used in combination with ________ in prostate cancer?

A

AR blocker

GnRH analogs

Pharmacology II (21 decks)

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