Aromatase Inhibitors and Hormonal Therapy for Prostate Cancer

Question 1

Aromatase

Answer 1

Catalyzes the conversion of testosterone to estradiol and androstenedione to estrone

Question 2

In post-menopausal women, aromase

Answer 2

is responsible for the majority of circulating estrogen

Question 3

3rd Generation Aromatase Inhibitors

Answer 3

 3rd generation is most specific for aromatase and not just all steroids
 No skin rash, no adrenal inhibition, very potent/specific for aromatase

Question 4

Non-Steroidal Aromatase Inhibitors

Answer 4

Letrozole (femara)

Anastrazole (arimidex)

Question 5

Steroidal Aromatase Inhibitors

Answer 5

Exemestane

Question 6

Anastrazole (arimidex) Use

Answer 6

Prevention of breast cancer

Question 7

Aromatase Inhibitors SE

Answer 7

 Asthenia, headache
 Hot flashes
 Bone and muscle pain

Question 8

Exemestane (aromasin) Use and MOA

Answer 8

o Use: advanced breast cancer in postmenopausal women

o MOA: irreversible inhibitor of aromatase

Question 9

Prostate + Hormones

Answer 9

Gland is dependent upon androgens

Growth is caused by DHT bind and making changes via conversion from testosterone through 5alpha reductase

Question 10

Where does testosterone come from?

Answer 10

 95% of testosterone is made in the testes

 5% is made in the adrenal gland

Question 11

LHRH Agonists Drugs

Answer 11

 Leuprolide (leupron)
 Goserelin (zoladex)
 Buserelin (suprefact)
 Nafarelin (synarel)

Question 12

LHRH Chronic Administration

Answer 12

Lead to internalization of the receptor (degradation)

Question 13

LHRH Agonists Use

Answer 13

Breast cancer and prostate cancer

Question 14

Leuprolide/Goserelin/Triptorelin SE

Answer 14

• Males: hot flashes, gynecomastia, decreased libido
• Females: hot flashes, decreased libido
• TUMOR FLARE

Question 15

Define Tumor Flare

Answer 15

Increase in size of the tumor initially due to increase in FSH initially

Question 16

Anti-Androgen Drugs

Answer 16

 Flutamide (eulexin)
 Bicalutamide (casodex)
 Nilutamide (milandron)
 Enzalutamide (Xtandi)

Question 17

Anti-Androgrens MOA

Answer 17

block the binding of androgens to androgen receptors → no prostate proliferation

Question 18

Flutamide and Bicalutamide SE and drug interaction

Answer 18

 SE: Gynecomastia. Hot flashes. Decreased libido

 Drug Interaction: May increase effect of warfarin

Question 19

Nilutamide SE and drug interactions

Answer 19

 SE: Gynecomastia. Hot flashes. Decreased libido

 Drug Interaction: disulfiram-like reaction with alcohol

Question 20

Corticosteroid Drugs

Answer 20

 Prednisone (deltasone)
 Methylprednisolone (solu-medrol)
 Dexamathasone (decadron)

Question 21

Corticosteroid Use

Answer 21

leukemias, lymphomas, myelomas

Question 22

Corticosteroid MOA

Answer 22

 When cortisol comes into the cell, it binds to the receptor and is dissociated from HSP to be translocated to the nucleus
 It then binds the response elements gene leading to transcriptions that cause tumor cell death (BAX genes)

Question 23

Corticosteroid SE

Answer 23

 Cushing syndrome (weigh gain, abdominal fat and fat deposition on the neck and around the face, loss of fat from limbic regions)
 Insomnia/restlessness
 Hirsutism (hair growth)
 Hyperglycemia