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Pharm Exam 5 > Androgens > Flashcards

Androgens Flashcards

1
Q

-Where is testosterone mainly synthesized? What cells?

A

-In testes and ovaries – Leydig cells

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2
Q

Hypothalamic-Pituitary-Gonadal axis

-Describe this sucker

A

1) gonadotropin-releasing hormone (GnRH) synthesized and released by hypothalamus
- pulsatile release
2) GnRH binds to gonadotropes=release of lutinizing hormone (LH) + follicle stimulating hormone
3) LH bind leydig cells–> testosterone production + secretin
- testosterone diffuses to sertoli cells=spermatogenesis
- acts on other cells via blood
4) FSH stimulates sertoli cells to produce ABP-androgen binding protein–>concentrates testosterone at the site of spermatogenesis
5) FSH stim sertoli cells to produce inhibin–>inh FSH production @ ant pit

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3
Q

Negative feedback pathways of the Hypothalamic-pit-gonadal axis:

A

1) Testosterone –> inh ant pituitary release of LH + inh GnRH release by hypothala
2) testosterone and its products converted into 5alhpa-dihydrotestosterone and estradiol –> inh ant pit release of LH
3) FSH stim sertoli cells to produce inhibin–>inh FSH production @ ant pit

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4
Q

What enzyme do LEydig cells have that is different from the adrenal cortex? What does it convert?

A
  • 17beta-hydroxysteroid dehydrogenase (17beta-HSD)

- converts androstenedione to testosterone

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5
Q

Testosterone in the blood…

A

bound to albumin (weak binding - considered bioavailable) or bound to sex hormone-binding globulin (SHBG-strong binding=not bioavailable)

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6
Q

Testosterone MOA & conversion products:

A
  • binds to intracellular androgen receptor (AR) –> inc or dec gene transcription
  • converted to 5alpa-dihydrotestosterone in prostate(DHT)= way hgiher biological activity when bound to AR then - longer t.5
  • converted to estradiol by CYP19 (aromatase-in many tissues)
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7
Q

5alpha-Dihydrotestosterone role in male vs testosterone role:

A
  • 5alpha role=dev of penis, scrotum, urethra, prostate, sebum, beard, sperm production,
  • testosterone role = epidydimis, vas deferens,
  • both do: seminal vesicles, sperm production, penis size
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8
Q

Anabolic effects of androgens:

A
  • stimulates resting metabolic rate

- inh lipid accumulation in adipocytes, stimulates lipolysis, inh differentiation of adipocyte precursors

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9
Q

Androgen effects on skeleton:

A
  • reduces bone reabsorption and enhances bone formation

- testosterone converted to estradiol = estrdiol closes epiphyseal plate (stops bone growth)

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10
Q

Androgen effects on RBC:

A

-inc erythropoietin production

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11
Q

Androgen effect on muscle:

A

inc protein synthesis and inh protein breakdown

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12
Q

Primary hypogonadism:

  • what happens?
  • causes?
A

1) problem is testicular dysf=dec in testosterone production
- loss of neg feedback=inc in circulating gonadotrophins (hypergonadotropic hypognadsm)
2) Causes: cryptorchidism(undescended testes); kleinfelters; medication (chemo)

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13
Q

Secondary hypogonadism

-what happens?

A

-problem is w/ hypothalapituitary or morbid obesity
dec is circulating gonadotrophins (hypogonadotropic hypognadsm)
-low testosterone with low LH and FSH

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14
Q

Which hypogonadism has low and which has high levels of circulating gonadotropins?

A

primary has HYPERGONADOTROPIC hypogonadism bc loss of neg feedback (testicular dysfunction)

secondary has HYPOGONADOTROPIC hypogonadism (hypothala/pit are broken)

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15
Q

relationship bw metabolic syndrome and hypogonadism:

A
  • go hand in hand (obesity+insulin resistance+ hypogonadism)

- testosterone converted to estradiol by adipose

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16
Q
  • What does adipose tissue do to testosterone?

- What effect does this have?

A
  • testosterone converted to estradiol by adipose
  • estradiol effects–> inh LH release from pit ==> reduced testosterone levels ==> less Testosterone means more adipose and its a viscious cycle
17
Q

Hypogonadism - what dec leydig cells production of testosterone?

A

insulin resistance due to adipose tissue

18
Q

Hypogonadism - what dec hypothala/pit producion of LH (and less LH = dec stimulation of leydig cells to produce testosterone)?

A

leptin, adipokines, and estradiol from adipose tissue

19
Q

As we age what happens to free testosterone?

A 
decreases and associated wtih a much of conditionss
-prostate cancer
-libido
-cognition
muscle stretngth
-mood
...etc
20
Q

androgen therapeutic uses:

A
  • stimulate sexual dev + inc in height in teens
  • repleacement therapy in hypogonadal men
  • aging-maintain vitality/vigor, reduce bone loss, sexual dysf
  • osteoporosis
  • gynecological disorders
  • anabolic effects a) debilitated states-AIDS,prolonged immobilization b) athletics
21
Q

17alpha-alkylated androgen drugs? route of administration?

A
  • methyltestosterone (oral + sublingual)
  • fluoxymesterone (oral)
  • danzaol (oral)
22
Q

testosterone ester androgen drugs? route of administration?

A

(fatty acids added to testosterone)

  • testosterone enanthate (IM)
  • testosterone cypionate (IM)

-slower metabolism and longer duration

23
Q

Which androgen drug is administrated as a transdermal/topical gel?

A

testosterone itself bro

24
Q

testosterone ester androgen drugs- benefit to use?

A
  • slower metabolism and longer duration

- fatty acid attached = fat soluble = given intramuscular

25
Q

17 alkylated androgen drugs - benefit to use?

A
  • more anabolic effects and less androgenic effects (dont want these effects)
  • oral
26
Q

Androgen therapy (abuse) - AEs (DOSE DEPENDENT):

A

1) musculoskeletal
- premature epiphyseal closure
- inc muscle and tendon injuries (cant handle inc muscle mass)
2) hepatic dysf (with 17-alkyated)
- cholestatic jaundice
- peliosis
- carcinoma
3) lipid metabolism
- dec HDL
- inc LDL
- inc risk for atherosclerosis and MI
4) edema- fluid retention (HTN)- Renal dysf
5) mental disturb
- mood swing, aggression, depression, pschosis

27
Q

antiandrogen- uses?

A

-female=hirsutism
-male=
precocious puberty
prostatis hyperplasia/cancer
alopecia
contraceptive
-psychosocial deviance (chemical castration)

28
Q

GnRH analogs

  • the drugs?
  • use to treat?
A
  • Leuprolide
  • Goserelin

-prostate cancer

29
Q

GnRH analogs:

  • compared to actual GnRH hormone?
  • effects?
  • problems?
A

1) inc receptor binding affinity and dec proteolysis vs regular GnRH
2) inc LH and testosterone production
3) over time get de-sensitization and down reg of GnRH receptors on pituitary
- need AR receptor antagonist bc initial testosterone surge can inc (prostate)cancer growth

30
Q

GnRH antagonist

  • name the drugs?
  • benefits to use/effects?
A
  • Degarelix
  • faster onset that GnRH agonsits
  • no LH (testosterone) surge
  • reduce LH/FSH production and release
  • dec testosterone production –> more effective testosterone suppression
31
Q

Degarelix is what kind of drug?

what does it do?

A

GnRH antagonist

  • faster onset that GnRH agonsits
  • no LH (testosterone) surge
  • reduce LH/FSH production and release
  • dec testosterone production –> more effective testosterone suppression
32
Q

Testosterone synthesis inh drugs??

A
  • spironolactone

- ketoconazole

33
Q

Spironolactone

  • type?
  • used for?
  • MOA?
A
  • testosterone synth inh
  • used to treat hirsutism
  • lowers androgen synth by reducing 17alpha-hydroxylase activity
  • competitive inh of androgen receptor (MOSTLY THIS
34
Q

Ketoconazole

  • tpe?
  • use for?
  • MOA?
A
  • anti-fungal but also testosterone synth inh
  • inh 17alpha-hydroxylase acitivty
  • not generally used to inh androgen synth bc it also inh cortisol synthesis
35
Q

5alpha-reductase inh drugs:

  • name these guys
  • used for?
  • side effects?
A
  • Finasteride
  • Dutasteride
  • reduce prostate growth in BPH
  • reduce baldness but at high levels reduces hair growth

-impotence and gynecomastia are infrequent

36
Q

Androgen receptor antagonists

-name the drugs

A
  • flutamide
  • nilutamide
  • bicalutamide
37
Q

Flutamide

  • type?
  • MOA?
  • TX?
  • AE?
  • use?
A
  • androgen receptor antagonist
  • competitive antagonisms at androgen receptor
  • treats prostate cancer; prevents testosterone sruge if given prior to GnRH administration
  • mild gynecomastia
  • reversible liver tox

Pharm Exam 5 (10 decks)

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