Male Pharmacology Flashcards

1
Q

Testosterone –> Dihydrotestosterone

A

5a reductase

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2
Q

Testosterone –> Estradiol

A

Aromatase

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3
Q

External genitalia
Hair follicles (balding)
Prostate hyperplasia

A

Dihydrotestosterone – Androgen receptor

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4
Q

Internal genitalia
Skeletal muscle
Erythropoiesis

A

Testosterone – Androgen receptor

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5
Q

Epiphyses
Bone density
Libido

A

Estradiol – Estrogen receptor

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6
Q

Testosterone Preparations

A

Transdermal - Testosterone
IM injection - Cypionate (Testosterone Esters)
Oral - Stanozolol (17-alkylated compounds)

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7
Q

Longest 1/2 life of testosterone preparations

A

Esters - Cypionate (IM) –> Days
Patch –> Hours
Gel –> 1 Day

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8
Q

Therapeutic uses of androgens

A
Male hypogonadism (testosterone deficiency) 
Goal is to mimic normal serum testosterone concentrations
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9
Q

SE of testosterone

A

Acne
Gynecomastia
Aggressive sexual behavior
**Must assess height and growth status of the patient

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10
Q

Other uses of androgens

A
  1. Male senescence
  2. Women with low testosterone
  3. Muscle wasting – associated with AIDS
  4. Blood dycrasias – (Danazol) for hemolytic anemia and idiopathic TTP
  5. Angioedema – 17-alkylated androgens (Stanozolol) stimulate hepatic synthesis of the esterase inhibitor
  6. Danazol is used for treatment of endometriosis and fibrocystic breast disease
  7. Improve athletic performance
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11
Q

What is one concern surrounding the use of testosterone in older men with pre-existing heart disease?

A

Two-fold increase in the relative risk of MI

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12
Q

Androstenedione and DHEA

A

Weak androgens

Increases popularity as a mean stop increase testosterone because they are treated as nutritional supplements

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13
Q

Adverse effects of androgen abuse

A
  1. Decreased endogenous testosterone and sperm production resulting in diminished fertility
  2. Decreased testicular size (after many years)
  3. High doses cause erythrocytosis
  4. Gynecomastia (testosterone converted to estrogen)
  5. 17-alkylated androgens cause hepatotoxicity – also more likely to increase LDL and decrease HDL
  6. In women and children virilization can occur
  7. Boys experience phallic enlargement, and women experience clitoral enlargement
  8. Stunting of linear growth (children)
  9. Psychological disorders and sudden death d/t cardiac disease
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14
Q

GnRH analog

Inhibits testosterone secretion by inhibiting LH secretion

A

Leuprolide

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15
Q

Therapeutic uses of Leuprolide

A

Treatment of advanced prostate cancer
Endometriosis
Central precocious puberty

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16
Q

SE of Leuprolide

A

Hot flashes
Decreased bone density
Vaginal dryness/atrophy in women
Erectile dysfunction in men

17
Q

Nonsteroidal, competitive inhibitor of the androgen receptor
Increase LH secretion, used in conjunction with a GnRH analog

A

Flutamide

18
Q

Therapeutic use of Flutamide

A

Metastatic prostate cancer

Hirsutism in women (off label)

19
Q

SE of Flutamide

A
Galactorrhea 
Breast tenderness
Gynecomastia
Hot flashes
Impotence
Decreased libido 
Tumor flare 
Black box - hepatic failure
20
Q

5-a reductase inhibitor (esp type II)

Blocks conversion of testosterone to dihydrotestosterone

A

Finasteride

21
Q

Therapeutic use of 5a-reductase inhibitors (Finasteride)

A

Benign prostate hyperplasia

Male pattern baldness

22
Q

SE of Finasteride

A

Impotence

Decreased libido

23
Q

PGE1

Given as intracavernous injection or urethral suppository for erectile dysfunction

A

Alprostadil

24
Q

SE of Alprostadil

A

Penile pain and urethral burning

25
Q

PDE5 inhibitors

inhibits breakdown of cGMP –> penile engorgement

A

Sildenafil
Tadalafil
Vardenafil

26
Q

Duration of action of PDE5 inhibitors

A

Sildenafil - up to 5 hours
Tadalafil - up to 36 hours
Vardenafil - up to 5 hours

27
Q

SE of PDE5 inhibitors

A

H/A, flushing, visual disturbances (d/t PDE6 interaction)

28
Q

What group of patients are PDE5 inhibitors CI in?

A

Patients taking nitrates –> combo could lead to extreme hypotension