Steroid Agents

Question 1

testosterone

Answer 1

Androgen
Transdermal or topical agent (low bioavailability)
MOA: bind nuclear hormone receptor–> translocate into nucleus–>activate or inhibit transcription
Use: stimulate sexual development, hypogonadism, sexual dysfunction, osteoporosis, endometriosis, anabolic effects
Adverse effects: increased muscle and tendon injury, decrease HDL, increase LDL, edema, polycythemia, mood swings
Decrease spermatogenesis and hypogonadism (decrease in GnRH)

Question 2

methyltestosterone

Answer 2

17-alkylated Androgen
Oral admin, slow release into blood stream
Enhanced anabolic effects and decreased androgenic effects
MOA: bind nuclear hormone receptor–> translocate into nucleus–>activate or inhibit transcription
Use: stimulate sexual development, hypogonadism, sexual dysfunction, osteoporosis, endometriosis, anabolic effects
Adverse effects: increased muscle and tendon injury, decrease HDL, increase LDL, edema, polycythemia, mood swings
Decrease spermatogenesis and hypogonadism (decrease in GnRH)

Question 3

testosterone enanthate

Answer 3

Androgen
Intramuscular admin
MOA: bind nuclear hormone receptor–> translocate into nucleus–>activate or inhibit transcription
Use: stimulate sexual development, hypogonadism, sexual dysfunction, osteoporosis, endometriosis, anabolic effects
Adverse effects: increased muscle and tendon injury, decrease HDL, increase LDL, edema, polycythemia, mood swings, liver toxicity
Decrease spermatogenesis and hypogonadism (decrease in GnRH)

Question 4

flutamide

bicalutamide

Answer 4

Antiandrogen therapy
Nonsteroidal androgen receptor antagonists
MOA: competitive antagonist of androgen receptors
Use: prostate cancer
Adverse effects: gynecomastia, reversible liver toxicity
In combo b/c increased LH secretion stimulates higher testosterone levels
Administered prior o GnRH analog tx to prevent testosterone surge

Question 5

ezalutamide

Answer 5

Antiandrogen
Nonsteroidal androgen receptor antagonist
MOA: competitive antagonist of androgen receptor; inhibit nuclear translocation of AR, block DNA binding, block transcriptional coactivator recruitment
Use: prostate cancer

Question 6

leuprolide

goserelin

Answer 6

GnRH receptor agonists
MOA: desensitize receptors of pituitary–>decrease LH production–>decrease testosterone secretion
Use: prostate cancer
In combo with androgen receptor antagonists to reduce initial testosterone surge
Adverse effects: sexual dysfunction, bone mineral density loss, anemia, fatigue, initial surge in testosterone levels–> growth of prostate

Question 7

degarelix

Answer 7

GnRH receptor antagonists
MOA: antagonist of GnRH receptor
Use: prostate cancer
Quickly reduces testosterone 
NO LH/testosterone surge

Question 8

abiraterone

Answer 8

Inhibitor of testosterone synthesis
MOA: inhibit 17 alpha-hydroxylase activity
Use: metastatic prostate cancer
Adverse effects: hepatic toxicity, decrease in cortisol, increase in aldosterone–>hypertension, hypokalemia, fluid retention
In combo with prednisone

Question 9

finasteride

dutasteride

Answer 9

5 alpha-reductase inhibitor
MOA: inhibit 5 alpha-reductase–> decrease DHT
Use: benign prostatic hypertrophy, male pattern baldness
Adverse effects: impotence, gynecomastia, reduced spermatogenesis, false negatives in PSA cancer screen

Question 10

sildenafil (Viagra)
vardenafil (Levitra)
tadalafil (Cialis)

Answer 10

Phosphodiesterase type 5 inhibitors
MOA: prevent decrease in cGMP levels–>inhibit constriction of smooth muscle
Use: erectile dysfunction and pulmonary arterial hypertension
Adverse effects: cardiac events, priapism (erection lasting longer than 4-6 hrs), sudden vision loss
Drug interactions: nitrites or nitrates–>hypotension; protease inhibitors for HIV

Question 11

diethylstilbesrol
estradiol
ethinyl estradiol
mestranol

Answer 11

estrogens

Question 12

medroxyprogesterone acetate (MPA)
19-nortestoserone 
norelgestromin
norethindrone
norgestimate
norgestrel

Answer 12

progesterones

Question 13

clomiphene

Answer 13

Estrogen receptor partial agonist
MOA: blocks/reduces negatie feedback regulation of estrogen–> increase LH and FSH surge
Use: fertility drug
Adverse effects: multiple births, hot flashes, ovary enlargement, blurred vision
Dose during follicular phase

Question 14

tamoxifen

Answer 14

Selective estrogen receptor modulators (SERMs)
MOA: agonist in bone, partial agonist in endometrium (proliferation), antagonist in breast and HPG axis
Use: ER and breast cancer
Adverse effects: hot flashes, endometrial cancer, nasuea, vomiting

Question 15

raloxifene

Answer 15

Selective estrogen receptor modulators (SERMs)
MOA: agonist in bone, antagonist in breast/uterus/HPG axis
Use: cancer, postmenopausal bone loss
Adverse effects: hot flashes, nausea, vomiting

Question 16

danazole

Answer 16

Inhibition of estrogen
MOA: displace estrogen from binding to serum proteins–> clear estrogen from body rapidly; decrease release of LH and FSH–>decrease estrogen synthesis
Use: endometriosis, breast fibrocystic disease
Adverse effects: weight gain, edema, oily skin, acne, hirsutism, hot flashes
Metabolite ethisterone has androgenic effect

Question 17

anastrozole

letrozole

Answer 17

Inhibition of estrogen
MOA: inhibit enzyme aromatase–> block synthesis of estrogens from androgens
Use: breast cancer
Adverse effects: arthralgias, GI disturbances, hot flashes, fatigue

Question 18

mifepristone

Answer 18

Manipulate progestin action–abortifacient
MOA: antiprogestin binds progesterone receptor–> reduce progesterone receptor activation–> contraction of uterus and endometrial lining breakdown
Use: terminate pregnancies in 1st trimester
Adverse effects: bleeding, pelvic pain, vomiting, diarrhea

Question 19

ulipristal

Answer 19

Manipulate progestin activity
MOA: partial agonist
Use: emergency contraceptive that can be used up to 5 days after intercourse