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PMCOL 343 > Androgens and Antiandrogens > Flashcards

Androgens and Antiandrogens Flashcards

1
Q

Describe the events that occur in the HPG axis to regulate gametogenesis.

A
  1. hypothalamus –> GnRH (pulsatile)
  2. GnRH (+) ant pit –> LH and FSH
  3. LH (+) Leydig cells –> testosterone
  4. FSH (+) Sertoli cells –> steroid hormone-binding protein and inhibin
  5. testosterone, FSH, androgen-binding protein (+) spermatogenesis

negative feedback:
6. inhibin (-) pituitary –> FSH
7. testosterone (-) hypothalamus –> GnRH

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2
Q

Which cells synthesize testosterone? What is the precursor of testosterone?

A

leydig cells; cholesterol

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3
Q

Via which pathways can testosterone act? (consider enzymes and different hormones, and where it acts)

A
  • amplification path: 5-alpha-reductase converts T to DHT; gonads, prostate, skin, hair
  • direct path: T acts on liver, muscle, adipose tissue
  • diversification path: aromatase converts T to E2; brain and bone
  • inactivation path: deactivate T; hepatic oxidation and conjugation –> renal excretion
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4
Q

What are the mechanisms of action of androgen?

A
  • androgen-dependent pathway (slow classic genomic mechanism)
  • androgen-independent pathway (slow classic genomic mechanism)
  • rapid non-genomic mechanisms
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5
Q

When is the androgen-dependent mechanism of action activated?

A

when androgen levels are high

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6
Q

When is the androgen-independent mechanism of action activated?

A

activation of Arby phosphorylation mediated by receptors downstream growth factor receptors

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7
Q

When are the rapid non-genomic mechanisms of action activated?

A

when androgen levels are low

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8
Q

Before puberty, does an increase of androgens prevent or stimulate reaching full height?

A

prevent

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9
Q

metabolic effects of androgens?

A
  • increase protein synthesis
  • decrease protein breakdown
  • decrease HDL levels
  • stimulate erythrocyte production
  • more prone to acne
  • salt and water retention

(i.e. anabolic and block catabolism)

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10
Q

Rank the following characteristics of T and DHT:
- affinity for androgen receptor
- dissociation rate

A
  • affinity for androgen receptor: T < DHT (twofold)
  • dissociation rate: T > DHT (fivefold)
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11
Q

pharmacological uses of androgens?

A
  • androgen replacement therapy: hypogonadism, pituitary deficiency, aging
  • anabolic agents
  • osteoporosis
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12
Q

pharmacological uses of antiandrogens?

A
  • benign prostatic hyperplasia (BHP)
  • prostate cancer
  • precocious puberty
  • hair loss
  • hirsutism
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13
Q

pharmacological uses of selective androgen receptor modulators (SARMs)?

A

no FDA-approved indications; promise for safe use in treatment of prostate cancer, male hormonal contraception, breast cancer, etc.

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14
Q

primary vs secondary hypogonadism? what can be used to treat hypogonadism?

A
  • primary = defect of testes
  • secondary = defect of HPG axis
  • treatment: androgen replacement therapy
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15
Q

Which hormone does androgen replacement therapy use?

A

only testosterone

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16
Q

Besides hypogonadism, what can androgen replacement therapy be used to treat?

A

andropause (decrease in T levels in aging males)

17
Q

What are therapeutic uses of androgens (besides andropause and hypogonadism)?

A
  • anemia (erythrocyte production)
  • osteoporosis
  • protein anabolic agents –> increase muscle mass
  • male contraceptive –> inhibit GnRH via negative feedcback
18
Q

adverse effects of androgen therapy?

A
  • serious adverse effects are rare
19
Q

What are the different types/MOA of antiandrogens?

A
  • testosterone synthesis inhibitors
  • 5-alpha-reductase inhibitors
  • AR blockers
20
Q

list the following for ketoconazole:
- class of drug
- MOA

A
  • class: antiandrogen; T synthesis inhibitor
  • MOA: inhibit 17-alpha-hydroxylase
21
Q

list the following for abiraterone acetate:
- class of drug
- MOA
- uses

A
  • antiandrogen; T synthesis inhibitor
  • MOA: inhibit 17-alpha-hydroxylase and 17, 20 lyase
  • uses: androgen dependent PC
22
Q

list the following for finasteride:
- class of drug
- MOA
- uses

A
  • class: antiandrogen; 5-alpha-reductase inhibitor
  • MOA: inhibit conversion of T to DHT
  • uses: BPH
23
Q

list the following for flutamide:
- class of drug
- MOA
- uses

A
  • class: antiestrogen; AR blocker
  • MOA: nonsteroidal competitive antagonists of AR
  • uses: prostate cancer
24
Q

list the following for darolutamide:
- class of drug
- MOA

A
  • class: antiandrogen; AR blocker
  • MOA: second generation blocker; inhibit AR nuclear translocation
25
Q

list the following for SARMs:
- MOA
- uses

A
  • MOA: bind AR and display tissue selective activation of androgenic signaling
  • uses: muscle wasting, osteoporosis, breast cancer, prostate cancer
26
Q

Which drug is highly attractive for doping in sports and illegal bodybuilding use? why?

A

SARMs; anabolic effects

PMCOL 343 (27 decks)

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