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Year 2 Pharmacology > Androgen agents > Flashcards

Androgen agents Flashcards

1
Q

where is testosterone synthesized? from what molecule?

A

leydig cells

cholesterol

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2
Q

what enzymes is responsible for converting androsteonedione to testosterone?

A

17B-hydroxysteroid dehydrogenase (17B-HSD)

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3
Q

17B-hydroxysteroid dehydrogenase (17B-HSD) is responsible for what conversion?

A

androsteonedione to testosterone

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4
Q

is albumin bound testosterone considered bioavailable or not bioavailable?

A

bioavailable

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5
Q

primary hypogonadism is due to what cause? what is the result? what are the testosterone, GnRH / LH / FSH levels?

A

testicular dysfunction leading to decrease in testosterone production

loss of negative feedback - decrease in testosterone does not inhibit GnRH, LH, FSH

testosterone - low
GnRH / LH / FSH - high

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6
Q

secondary hypogonadism is due to what cause? what is the result? what are the testosterone and LH / FSH levels?

A

hypothalamus / pituitary - decrease in circulating gonadotropins

decrease in circulating gonadotropins

testosterone - low
LH / FSH - low

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7
Q

what is the route for methyltestosterone? what type of testosterone derivative is it?

A

oral, sublingual

17 alkylated

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8
Q

what is the route for testosterone enanthate? what type of testosterone derivative is it?

A

IM

testosterone ester

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9
Q

what is the route for testosterone?

A

transdermal or topical

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10
Q

how are the pharmacokinetics of testosterone esters different from testosterone?

A

increased lipophilicity
IM
slow release, slower metabolism
longer duration

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11
Q

how are the pharmacokinetics of 17-alkylated derivatives different from testosterone?

A

slower catabolism
oral route
liver toxicity and hepatic cancer

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12
Q

what are the antiandrogen classes?

A

androgen receptor antagonists
GnRH agonists
GnRH antagonists
steroid synthesis inhibitors

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13
Q

flutamide and bicalutamide are what class of drug? what is their MOA?

A

non steroidal anti-androgens

competitive inhibitor of androgen binding to AR

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14
Q

flutamide and bicalutamide are used for what condition/

A

prostate cancer

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15
Q

what class of drug is enzalutamide? what is the MOA?

A

androgen receptor antagonists

competitive inhibitor of androgen binding to AR

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16
Q

what are the additional effects of enzalutamide?

A

inhibits nuclear translocation of AR
blocks DNA binding
blocks coactivator recruitment

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17
Q

what class of drug are leuprolide and goserelin? what are they used for?

A

GnRH agonists

prostate cancer

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18
Q

what is the result of leuprolide and goserelin administration?

A

initially increases LH and testosterone production

over time, leads to desensitization and downregulation of GnRH receptors on pituitary gonadotropes (pulsatile vs continuous) - DECREASE IN TESTOSTERONE LEVELS

19
Q

what are the adverse effects of GnRH agonists?

A 
sexual dysfunction 
bone mineral density loss 
anemia 
fatigue 
initial surge in testosterone levels that can cause growth of prostate cancer
20
Q

what must be used to prevent the initial testosterone surge prior to leuprolide / goserelin treatment that can increase cancer growth? what is the rationale for this?

A

an AR receptor antagonist (flutamide)

preventing the EFFECT of the testosterone surge (but not the surge itself)

21
Q

what class of drug is degarelix?

A

GnRH receptor antagonist

22
Q

what makes degarelix different from GnRH agonists?

A

faster onset
no LH (testosterone) surge
reduce LH / FSH production and release
decrease testosterone production - more effective

23
Q

what class of drug is abiraterone? what is it used for? which drug is it combined with?

A

androgen biosynthesic inhibitor

metastatic prostate cancer

prednisone

24
Q

how can abiraterone cause HTN, hypokalemia, and fluid retention?

A

intermediates from 17a-HSD inhibition are shunted into aldosterone pathway - increased mineralcorticoids (aldosterone)

25
Q

what class of drug are finasteride and dutasteride? what are they used for?

A

5a-reductase inhibitors

BPH

26
Q

what is thought to be the causative agent of androgenic alopecia?

A

DHT (increased levels)

27
Q

what is used to treat male pattern baldness?

A

finasteride (Propecia)

28
Q

what are the adverse effects of 5a-reductase inhibitors?

A

lower PSA levels (false negatives for prostate cancer)

impotence, gynecomastia

29
Q

ED drugs inhibit what enzyme? what is the result?

A

PDE-5

increase cGMP in smooth muscle - continued relaxation

30
Q

what are the PDE5 inhibitors?

A

sildenafil (Viagra)
vardenafil (Levitra)
tadalafil (Cialis)

31
Q

how are PDE5 inhibitors metabolized?

A

metabolized primarily by cyp450 enzymes

32
Q

what are the adverse effects of the PDE5 inhibitors?

A

dangerously low BP in patients taking nitrates / nitrites
priapism
sudden vision loss

33
Q

what are the androgenic functions of androgens in the male?

A

maturation and continued function of male reproductive tract and production of secondary male sexual characteristics

34
Q

androgens have metabolic functions in which areas of the male body?

A

muscle, bone, bone marrow, liver

35
Q

which molecule stimulates the production of testosterone by Leydig cells?

A

LH

36
Q

what is the function of 5a reductase?

A

converts testosterone to DHT

37
Q

which is more potent - DHT or testosterone?

A

DHT

38
Q

what is a significant adverse effect of the 17-alkylated testosterone derivatives?

A

carcinoma

39
Q

what is the general MOA of the GnRH agonists and GnRH antagonists?

A

reduce secretion of LH (thus reducing testosterone)

40
Q

what drugs are given before administration of GnRH analog treatment? why?

A

flutamide and bicalutamide

prevent effects of initial testosterone surge via LH

41
Q

what is the MOA of abiraterone?

A

blocks 17a-hydroxylase

42
Q

what is a side effect of inhibiting 17a-hydroxylase?

A

adrenal insufficiency (loss of glucocorticoid production)

43
Q

which compounds cause an initial surge in testosterone production? which drugs need to be included to prevent this?

A

GnRH agonists

AR antagonists

Year 2 Pharmacology (70 decks)

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