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Pharmacology > Antiandrogens & Androgen Inhibitors > Flashcards

Antiandrogens & Androgen Inhibitors Flashcards

1
Q

T/F
Free testosterone and dihydrotestosterone (DHT) are biologically active androgens that affect various target tissues such as the pilosebaceous unit

A

True

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2
Q

What is anti androgen ?

A

Agents that block the androgen receptor (AR)

Eg. Spironolactone
Flutamide
Cyproterone acetate

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3
Q

What is an androgen inhibitor ?

A

Agents that block androgen synthesis

Eg
Finasteride
Dutasteride
- both 5a reductase inhibitors
Leuprolide (GnRH agonist)
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4
Q

T/F

Sex hormones affect T-helper 1 (Th1)/Th2 cell balance

A

T

We now know that androgens affect this balance

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5
Q

Androgen and oestrogen receptors are present on most immune competent cells

A

T

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6
Q

List dermatologic androgen excess disorders

A

Acne vulgaris
Androgenetic alopecia
Hirsutism
HS

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7
Q

T/F

5-a reductase type I isoenzyme is found predominantly on genital skin and sebaceous gland ducts

A

F
This is in non genital skin : sebaceous gland lobules , liver , kidney , spleen

Type 2 is found in hair follicles and sebaceous gland ducts , genital skin of men and women , urogenital tract of men

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8
Q

T/F

Canrenone is the active metabolite of spironolactone

A

T

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9
Q

T/F

Protein binding of spironolactone is 13-25%

A

False
13-25% protein binding for cimetidine
Spironolactone is 98% protein bound

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10
Q

T/F

All antiandrogens are renally excreted

A

False

Spironolactone predominantly hepatobiliary route

Medroxyprogesterone acetate especially renal and also hepatobiliary

Cimetidine predominantly renal

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11
Q

T/F

Spironolactone does not inhibit 5-a reductase

A

T

Aldosterone antagonist and a relatively weak antiandrogen that blocks the AR and inhibits androgen biosynthesis

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12
Q

T/F

Food increases absorption of spironolactone

A

T

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13
Q

T/F

Finasteride is extensively metabolized in the liver to inactive metabolites

A

True

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14
Q

T/F

Of the antiandrogens and androgen inhibitors , Spironolactone has the greatest bioavailability

A

True >90%
Others ~60-69%

Or variable (medroxyprogesterone acetate)
Or unknown (ketoconazole)
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15
Q

T/F

Drosperinone has antiandrogenic activity but no androgenic, estrogenic or glucocorticoid activity

A

True

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16
Q

What is the role of type 2 5a reductase ?

A

Catalyses conversion of testosterone to DHT

17
Q

T/F

Finasteride binds to the androgen receptor

A

F

Not anti androgen

18
Q

MoA of finasteride

A

Type 2 5-a reductase inhibitor

May inhibit local level of DHT in hair follicle

May have secondary effects on AR by suppressing DHT and via feedback mechanisms that affect AR levels

19
Q

Spironolactone had half life of 2h

A

F

10-35h

20
Q

Finasteride inhibits both type 1 and 2 5a reductase

A

F
Type 2 only
Distasteride inhibits both

21
Q

Finasteride is metabolized by Cyp3A4

A

Yes

22
Q

Ketoconazole has secondary pharm effect of inhibiting cyp3a4 enzymes involved in steroid hormone biosynthesis
– reduced production of both GC and androgenic steroids

A

T

23
Q

Spironolactone increases LH

A

F

Decreased response of LH to GnRH leading to lower LH:FSH ratio

24
Q

Spironolactone is more effective at reducing hirsutism than finasteride

A

T

25
Q

Strongest CI for Spironolactone is agents that increased risk of hyperK+
Eg ACE inhibitors , ARBS, other aldosterone antagonists

A

T

26
Q 
Half lives
Spironolactone 
Medroxyprogesterone acetate
Cimetidine 
Finasteride 
Dutasteride
Ketoconazole
A 
Spironolactone 10-35h
Medroxyprogesterone acetate 8-9h
Cimetidine 2h
Finasteride 4-8h
Dutasteride4-8h
Ketoconazole  8h
27
Q 
Protein binding of 
Spironolactone 
Medroxyprogesterone acetate
Cimetidine 
Finasteride 
Dutasteride
Ketoconazole
A 
Spironolactone  98%
Medroxyprogesterone acetate varies
Cimetidine 13-25%
Finasteride 90%
Dutasteride 90%
Ketoconazole 95-99%
28
Q 
Excretion
Spironolactone 
Medroxyprogesterone acetate
Cimetidine 
Finasteride 
Dutasteride
Ketoconazole
A

All predominantly faecal except cimetidine and medroxy is predom renal

Pharmacology (63 decks)

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