Androgens and Antiandrogens Flashcards

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1
Q

What is hypogonadism

A

failure of testes to make testosterone

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2
Q

What are some health issues with hypogonadism

A
  • loss of energy
  • decreased libido
  • osteoporosis
  • loss of muscle mass
  • anemia
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3
Q

How is hypogonadism treated

A

give testosterone or testosterone esters

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4
Q

How is testosterone administered to a patient

A

IM or transdermal

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5
Q

How should you not administer testosterone to a patient?

A

oral

  • metabolized by small intestines
  • low bioavailability: extensive first pass effects
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6
Q

where are testosterone topical gels applied ? how do these topical gels work?

A

shoulders or upper arms

- 24 hour depot for slow release of hormone in blood

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7
Q

When are testosterone topical patches applied

A

applied daily

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8
Q

What is the trade name for testosterone topical patch

A

Androderm

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9
Q

where should androderm not be topically applied? why?

A

scrotum

- potential to absorb too much testosterone

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10
Q

When is the androgderm patch removed and why? side effects of left on?

A
  • MRI test
  • patch has aluminum
  • can cause burning
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11
Q

Why should female partners avoid touching the androderm patch

A

cause acne or abnormal hair growth

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12
Q

Where is the buccal testosterone given?

A
  • placed on gum

- forms gel

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13
Q

What is the FDA black box warning for all testosterone gels and topical solutions

A

virilization can occur in children exposed to topical testosterone
- children should not come in contact with product

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14
Q

Name 2 testosterone esters

A

testosterone cypionate and enanthate

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15
Q

How is testosterone ester administered

A

IM

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16
Q

What is an advantage of using testosterone ester over testosterone

A
  • testosterone esters have longer duration

- administered every 2 or 4 weeks

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17
Q

Testosterone is used to treat what

A
  1. hypogonadism

2. metastatic breast cancer in women

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18
Q

Name 2 17alpha-alkylated testosterone

A
  1. methyltestosterone

2. fluoxymesterone

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19
Q

what is the best route of aministration for methyltestosterone and fluoxymesterone

A

oral

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20
Q

What is 17alpha-alkylated testosterone used to treat

A
  1. hypogonadism

2. metastatic breast cancer in women

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21
Q

Methyltestosterone and fluoxymesterone has a high abuse potential for what

A

anabolic activity

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22
Q

17alpha-alkylated testosterone is contraindicated for who

A
  • male breast cancer
  • prostate cancer
  • pregnancy
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23
Q

low doses of methyltestosterone and fluoxymesterone have what adverse effects

A

cholestatic hepatitis

jaundice

24
Q

Testosterone analogues associated with methyltestosterone and fluoxymesterone have the greatest risk of what side effect

A

hepatotoxicity

25
Q

what are side effects of 17alpha-alkylated testosterone at normal doses

A
  • edema ( salt and water retention)
  • liver cancer
  • bleeding due to decline levels of clotting factors II, V, VII, and X
26
Q

what are contraindications for all testosterone analogs

A

prostate cancer
male breast cancer
pregnancy

27
Q

MOA for Danazol

A

depresses preovulatory surge in output of FSH and LH

  • reduction of ovarian estrogen and progesterone production
  • suppress midcycle surge of FSH and LH resulting in anovulation
28
Q

Why would women not want to take Danazol

A
  • weight gain
29
Q

What is Danazol used for

A
  • Endometriosis
  • hereditary angioedema
  • fibrocystic breast disease
30
Q

What are adverse effects of Danazol

A
  • weight gain
  • acne
  • thrombosis
  • mood swings
  • hepatic dysfunction
31
Q

what is Danazol contraindicated in

A

pregnancy

breast feeding

32
Q

MAO for Stanazolol

A

17-alpha-alkylated derivative of testosterone

- increases mRNA levels and protein levels of C1 INH and C4

33
Q

Who is Stanazolol contraindicated in

A
  1. pregnancy
  2. male breast or prostate cancer
  3. female breast cancer with hypercalcemia
34
Q

What is Stanazolol used for

A

Hereditary angioedema

35
Q

What are adverse effects of Stanazolol

A

HEPATIC TOXICITY
edema
acne
virilization in women , baldness

36
Q

MOA for Oxandrolone

A
  • synthetic testosterone derivative

- high anabolic to andgrogenic ratio

37
Q

What is Oxandrolone used for

A
  • weight gain patients who have undergone
    1. extensive surgery
    2. severe trauma
    3. long-term corticosteroid therapy
    and cannot gain weight
38
Q

side effects of Oxandrolone

A
  • edema
  • hypertension
  • irritability
39
Q

Oxandrolone is contraindicated in who

A
  • breast cancer
  • prostatic cancer
  • pregnancy
40
Q

Overall MOA for Finasteride and Dutasteride

A

reduce levels of dihydrotestosterone

41
Q

What enzyme converts testosterone to dihydrotestosterone

A

5alpha-reductase

42
Q

Specific MOA for Finasteride

A

-competitive inhibitor of type 2 form of 5alpha-reductase

43
Q

Specific MOA for Dutasteride

A
  • competitive inhibitor for Type 2 and 1 forms of 5alpha-reductase
44
Q

What are antiandrogens used for

A
  • benign prostatic hyperplasia

- may take 6 months to reduce size of prostate

45
Q

Finasteride can be used in combination with other drugs

A
  • Tamsulosin or Alfuzosin
46
Q

What is the MOA of Tamsulosin and Alfuzosin

A

alpha1-adrenergic receptor inhibitors

- decreases smooth muscle tone in prostate and bladder neck

47
Q

What is the specific MOA for Tamsulosin

A
  • inhibits smooth muscle contraction
  • decreases muscle tone in bladder neck and prostatic urethra, reduces urethral pressure and resistance which lessens bladder outlet obstruction
48
Q

What are adverse effects of Finasteride and Dutasteride

A
  • gynecomastia
  • decrease PSA values ( lower levels in males by 50%)
  • decrease dihydrotestosterone
  • elevated testosterone
49
Q

when should Fnasteride be used with caution

A

hepatic dysfunction

50
Q

Who is contraindicated for Finasteride and Dutasteride

A
  • women and children
  • pregnancy category X
  • pregnant women and breast feeding women should not handle tablets
51
Q

MOA for Leuprolide

A
  • GnRH agnoist
  • down regulation of LH and FSH
  • decrease levels of circulating testosterone in males
52
Q

what is Leuprolide used for

A

prostatic cancer

endometriosis

53
Q

Adverse effects of Leuprolide

A
  • hot flashes
  • edema
  • gynecomastia
54
Q

MOA for Fltuamide

A

intereferes with binding of testosterone and dihydrotestosterone

55
Q

what is Fltuamide used for? route of administration?

A
prostatic cancer ( oral )
acne ( topical)
56
Q

Side effect of Fltuamide

A
  • gynecomastia

- elevated liver function tests