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Cam's Cards > Pharmacology of Androgens > Flashcards

Pharmacology of Androgens Flashcards

1
Q

GnRH is released by the ______, which stimulates release of _____ and _____ from the ant. pituitary.

A

Hypothalamus

LH and FSH

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2
Q

LH stimulates ____ cells to produce testosterone.

A

Leydig cells

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3
Q

Testosterone promotes production of _____ by sertolli cells.

A

Sperm

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4
Q

Testosterone is converted to DHT by?

A

5 alpha reductase

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5
Q

Testosterone is converted to estradiol by?

A

aromatase

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6
Q

Testosterone and DHT work on what receptors?

A

Androgen receptors

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7
Q

Estradiol works on what receptors?

A

Estrogen receptors

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8
Q

Testosterone is the most important androgen in _____ and _____.

A

Muscle and liver

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9
Q

Testosterone levels peak at what time?

A

8-10 am

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10
Q

Normal testosterone levels are between ____ and ____ at their peak.

A

500-700 ng/dl

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11
Q

Hypogonadism is marked by testosterone levels of _____.

A

<200ng/dl

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12
Q

DHT is the predominant androgen in ____ and _____.

A

Prostate and reproductive tissue.

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13
Q

T/F? DHT can be converted to estradiol by aromatase.

A

False - only testosterone is the only substrate for aromatase.

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14
Q

The most significant action mediated by estrogen receptors occurs in ______.

A

Bone

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15
Q

What are the clinical uses for androgens?

A

Hypogonadal men/boys
Osteoporosis
Muscle wasting in AIDS pts
Hormone replacement therapy in aging men

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16
Q

What are symptoms of androgen deficiency?

A

Low libido
Low bone mineral density
Gynecomastia

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17
Q

T/F? Testosterone can help treat impaired spermatogenesis.

A

False - Testosterone suppression of gonadotropin secretion would further impair spermatogenesis

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18
Q

What should be recommended to patients with low normal T levels?

A

Diet, lifestyle changes, and weight loss

19
Q

IM dosing of testosterone provides what benefits?

Drawbacks?

A

Less frequent injections but higher fluctuation in T levels.

20
Q

Oral testosterone is hardly ever used do to what side effects?

A

Hepatic side effects

21
Q

What adverse effect of a testosterone patch requires discontinuance in up to 1/3 of patients trying the patch?

A

Severe skin rash

22
Q

List the adverse effects of testosterone.

A

Decreased HDL and increased LDL
Hypomania (roid rage)
Cardiovascular risks

23
Q

T/F? All anabolic hormones also have androgenic side effects.

A

True

24
Q

Pulsatile administration of GnRH ______ (increases/decreases) LH and FSH release.
Continuous administration of GnRH _______ LH and FSH release.

A

Increases

Blocks

25
Q

Targets for Anti-Androgen drug action include?

A

GnRH receptors
CYP17 (testosterone synthesis)
5 alpha reductase
Androgen receptors

26
Q

Give an example of a CYP17 inhibitor.

A

Ketoconazole

27
Q

Give an example of a 5 alpha reductase inhibitor.

A

Finasteride

28
Q

Give an example of an androgen receptor inhibitor.

A

Flutamide

Spironolactone

29
Q

List the clinical uses of anti-androgens.

A

BPH
Androgenic alopecia
Prostate cancer
Hirsutism of polycystic ovarian syndrome

30
Q

List 3 alpha blockers for BPH treatment.

A

Tamsulosin (flomax) - uroselective
Silodosin (rapaflo) - uroselective
Doxazosin - non selective.

31
Q

Common side effect of alpha blockers?

A

Orthostatic hypotension

32
Q

For BPH patients who cannot tolerate alpha blockers, what medications would you recommend?

A

5 alpha reductase inhibitors
FInasteride
Dutasteride

33
Q

Adverse effects of 5 alpha reductase inhibitors?

A

decreased libido
ejaculatory or erectile dysfunction
weakness

34
Q

What oral medication is available for treatment for androgenic alopecia?

A

Finasteride

35
Q

Is there a difference in dose of finasteride for treatment of BPH vs androgenic alopecia?

A

Yes
BPH - 1mg
Androgenic alopecia - 5mg

36
Q

What topical medication is available for androgenic alopecia?

A

Minoxidil (Rogaine)

37
Q

What class of medications used to treat prostate cancer is associated with an initial flare of bone pain and urinary tract symptoms?

A

GnRH agonists

38
Q

What medications are examples of GnRH agonists used to treat prostate cancer?

A

Leuprolide (Lupron)

Histrelin (Supprelin)

39
Q

What is the preferred androgen receptor blocker used for prostate cancer?

A

Bicalutamide

40
Q

Role of bicalutamide in prostate cancer?

A

Reduces flare symptoms

41
Q

When are GnRH antagonists indicated for prostate cancer?

A

Advanced prostate cancer

42
Q

T/F? GnRH antagonists are associated with flare symptoms.

A

False

43
Q

First line treatment for hirsutism of PCOS?

A

Combined oral contraceptive.

44
Q

Your patient you are treating for hirsutism of PCOS has had a suboptimal response to a COC. What medication would you consider adding?

A

Spironolactone

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