Pharm 5 Androgens

Question 1

Primary stimulator of testosterone synthesis and androgen-binding globulin

Answer 1

LH - testosterone (leydig cells)

FSH - ABG

Question 2

LH, FSH stimulated by

Answer 2

GnRH (pulsatile)

Question 3

LH, FSH inhibitors (male)

Answer 3

Testosterone, Estradiol

Question 4

Site of female androgen synthesis

Answer 4

Corpus luteum

Question 5

Testosterone metabolism

Answer 5

5a-reductase -> dihydrotestosterone
P450 aromatase (CYP19) -> estradiol

Question 6

5a reductase & CYP19 locations

Answer 6

5a reductase - Skin, bone, liver, genitals

CYP19 aromatase - Fat, liver, bone

Question 7

Testosterone action

Answer 7

A-R ->

• Internal genitalia (Wolffian development)
• Skeletal muscle (puberty)
• Erythropoiesis

Question 8

Dihydrotestosterone action

Answer 8

A-R ->

• Eternal genitalia (differentiation and maturation)
• Hair follicles (puberty)

Question 9

Estradiol action

Answer 9

E-R ->

• Bone density and epiphyses closure
• Regulation of male reproductive tract fluid

Question 10

Transdermal androgen Tx

Answer 10

Testosterone

Question 11

IM deposit androgen Tx

Answer 11

Testosterone cypionate

Question 12

Oral androgen Tx

Answer 12

• Methyltestosterone
• Oxandrolone
• Danazol

Question 13

Endometriosis androgen Tx

Answer 13

Danazol

Question 14

Unusual clinical uses for androgens

Answer 14

Hereditary angioedema

• AIDS muscle wasting
• Severe anemia (stimulate erythropoiesis)

Question 15

Androgen Tx tumor risk

Answer 15

Liver tumors

Question 16

Androgen Tx contraindications (3)

Answer 16

Pregnancy
Prostate/Breast cancer
Infants/Young children

Question 17

-Danazol-
MOA
indications

Answer 17

Weak androgen, progestin, glucocorticoid

• INHIBITS gonadal steroidogenesis
• Endometriosis, Fibrocystic breast disease

Question 18

-Ketoconazole-

indication

Answer 18

Inhibits P450 required for steroid synthesis

-Prostate cancer

Question 19

-Finasteride-
MOA
indication

Answer 19

5a-reductase inhibitor

• Blocks dihydrotestosterone production
• Benign prostatic hyperplasia

Question 20

-Flutamide-

indication

Answer 20

Nonsteroidal competitive A-R antagonist

-Prostate cancer

Question 21

-Spironolactone-
MOA
indication

Answer 21

Blocks Aldosterone-R and Androgen-R

• Inhibits 17a-hydroxylase
• Hirsutism

Question 22

-Tetrahydrogestrinone-

indication

Answer 22

The “clear” - THG

-Designer steroid to avoid drug test detection

Question 23

Steroid abuse AE

Answer 23

• Retention of sodium and water
• CAD risk (+LDL, -HDL)
• Severe acne
• Hyperinsulinemia, altered glucose tolerance
• Liver toxicity
• Premature bone fusion
• Testicular atrophy and gynecomastia