Androgens and Antiandrogens Flashcards
What is hypogonadism
failure of testes to make testosterone
What are some health issues with hypogonadism
- loss of energy
- decreased libido
- osteoporosis
- loss of muscle mass
- anemia
How is hypogonadism treated
give testosterone or testosterone esters
How is testosterone administered to a patient
IM or transdermal
How should you not administer testosterone to a patient?
oral
- metabolized by small intestines
- low bioavailability: extensive first pass effects
where are testosterone topical gels applied ? how do these topical gels work?
shoulders or upper arms
- 24 hour depot for slow release of hormone in blood
When are testosterone topical patches applied
applied daily
What is the trade name for testosterone topical patch
Androderm
where should androderm not be topically applied? why?
scrotum
- potential to absorb too much testosterone
When is the androgderm patch removed and why? side effects of left on?
- MRI test
- patch has aluminum
- can cause burning
Why should female partners avoid touching the androderm patch
cause acne or abnormal hair growth
Where is the buccal testosterone given?
- placed on gum
- forms gel
What is the FDA black box warning for all testosterone gels and topical solutions
virilization can occur in children exposed to topical testosterone
- children should not come in contact with product
Name 2 testosterone esters
testosterone cypionate and enanthate
How is testosterone ester administered
IM
What is an advantage of using testosterone ester over testosterone
- testosterone esters have longer duration
- administered every 2 or 4 weeks
Testosterone is used to treat what
- hypogonadism
2. metastatic breast cancer in women
Name 2 17alpha-alkylated testosterone
- methyltestosterone
2. fluoxymesterone
what is the best route of aministration for methyltestosterone and fluoxymesterone
oral
What is 17alpha-alkylated testosterone used to treat
- hypogonadism
2. metastatic breast cancer in women
Methyltestosterone and fluoxymesterone has a high abuse potential for what
anabolic activity
17alpha-alkylated testosterone is contraindicated for who
- male breast cancer
- prostate cancer
- pregnancy
low doses of methyltestosterone and fluoxymesterone have what adverse effects
cholestatic hepatitis
jaundice
Testosterone analogues associated with methyltestosterone and fluoxymesterone have the greatest risk of what side effect
hepatotoxicity
what are side effects of 17alpha-alkylated testosterone at normal doses
- edema ( salt and water retention)
- liver cancer
- bleeding due to decline levels of clotting factors II, V, VII, and X
what are contraindications for all testosterone analogs
prostate cancer
male breast cancer
pregnancy
MOA for Danazol
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
Why would women not want to take Danazol
- weight gain
What is Danazol used for
- Endometriosis
- hereditary angioedema
- fibrocystic breast disease
What are adverse effects of Danazol
- weight gain
- acne
- thrombosis
- mood swings
- hepatic dysfunction
what is Danazol contraindicated in
pregnancy
breast feeding
MAO for Stanazolol
17-alpha-alkylated derivative of testosterone
- increases mRNA levels and protein levels of C1 INH and C4
Who is Stanazolol contraindicated in
- pregnancy
- male breast or prostate cancer
- female breast cancer with hypercalcemia
What is Stanazolol used for
Hereditary angioedema
What are adverse effects of Stanazolol
HEPATIC TOXICITY
edema
acne
virilization in women , baldness
MOA for Oxandrolone
- synthetic testosterone derivative
- high anabolic to andgrogenic ratio
What is Oxandrolone used for
- weight gain patients who have undergone
1. extensive surgery
2. severe trauma
3. long-term corticosteroid therapy
and cannot gain weight
side effects of Oxandrolone
- edema
- hypertension
- irritability
Oxandrolone is contraindicated in who
- breast cancer
- prostatic cancer
- pregnancy
Overall MOA for Finasteride and Dutasteride
reduce levels of dihydrotestosterone
What enzyme converts testosterone to dihydrotestosterone
5alpha-reductase
Specific MOA for Finasteride
-competitive inhibitor of type 2 form of 5alpha-reductase
Specific MOA for Dutasteride
- competitive inhibitor for Type 2 and 1 forms of 5alpha-reductase
What are antiandrogens used for
- benign prostatic hyperplasia
- may take 6 months to reduce size of prostate
Finasteride can be used in combination with other drugs
- Tamsulosin or Alfuzosin
What is the MOA of Tamsulosin and Alfuzosin
alpha1-adrenergic receptor inhibitors
- decreases smooth muscle tone in prostate and bladder neck
What is the specific MOA for Tamsulosin
- inhibits smooth muscle contraction
- decreases muscle tone in bladder neck and prostatic urethra, reduces urethral pressure and resistance which lessens bladder outlet obstruction
What are adverse effects of Finasteride and Dutasteride
- gynecomastia
- decrease PSA values ( lower levels in males by 50%)
- decrease dihydrotestosterone
- elevated testosterone
when should Fnasteride be used with caution
hepatic dysfunction
Who is contraindicated for Finasteride and Dutasteride
- women and children
- pregnancy category X
- pregnant women and breast feeding women should not handle tablets
MOA for Leuprolide
- GnRH agnoist
- down regulation of LH and FSH
- decrease levels of circulating testosterone in males
what is Leuprolide used for
prostatic cancer
endometriosis
Adverse effects of Leuprolide
- hot flashes
- edema
- gynecomastia
MOA for Fltuamide
intereferes with binding of testosterone and dihydrotestosterone
what is Fltuamide used for? route of administration?
prostatic cancer ( oral ) acne ( topical)
Side effect of Fltuamide
- gynecomastia
- elevated liver function tests
