Cancer Pharmacology - Antimetabolites

Question 1

Are Antimetabolites cell cycle specific?

Answer 1

YES

Question 2

Antimetabolites are cell cycle specific. Which phase do they work in?

Answer 2

S phase

Question 3

Antimetabolites are cell cycle specific. Which phase do they work in?

Answer 3

S phase

Question 4

What are Antimetabolites?

Answer 4

Structural analogs to compounds necessary for cell proliferation
– Block or subvert cell replication

Question 5

What is a Folic Acid Analog?

Answer 5

Methotrexate

Question 6

What is a Folic Acid Analog?

Answer 6

Methotrexate

Question 7

MOA for Methotrexate?

Answer 7

(-) dihydrofolate reductase

= folic acid will not be converted to tetrahydrofolic acid

Question 8

At low doses, what can Methotrexate treat?

Answer 8

RA and Psoriasis

Question 9

At higher doses, what does Methotrexate do?

Answer 9

Causes injury to healthy tissues

Question 10

At higher doses, Methotrexate causes injury to healthy tissues. What can prevent this?

Answer 10

Leucovorin

Question 11

At higher doses, Methotrexate causes injury to healthy tissues. What can prevent this?

Answer 11

Leucovorin

Question 12

What does Leucovorin do?

Answer 12

Allows thymidine synthesis to proceed

Question 13

Leucovorin spares the patient what symptoms?

Answer 13

GI and bone marrow toxicity

Question 14

What is a Pyrimidine Analog?

Answer 14

Fluorouracil

Question 15

What is Pyrimidine Analog?

Answer 15

Fluorouracil

Question 16

MOA for Fluorouracil?

Answer 16

Binds and (-) thymidylate synthetase 
= No DNA synthesis

Question 17

Fluorouracil is pro-drug. What does it converted to?

Answer 17

5-FU –> FdUMP

Question 18

Adverse effects of Fluorouracil?

Answer 18

Anorexia, nausea, diarrhea, stomatitis

Question 19

Adverse effects of Fluorouracil?

Answer 19

Anorexia, nausea, diarrhea, stomatitis

Question 20

What is a Purine Analog?

Answer 20

Mercaptopurine (6-MP)

Question 21

What is a Purine Analog?

Answer 21

Mercaptopurine (6-MP)

Question 22

MOA for Mercaptopurine?

Answer 22

(-) purine nucleotide synthesis by incorporating triphosphate

Question 23

During Mercaptopurine’s biotransformation, it gets inactivated by?

Answer 23

Xanthine oxidase

Question 24

Mercaptopurine’s effects can be diminished by xanthine oxidase. What can be added to therapy to prevent this?

Answer 24

A Xanthine oxidase inhibitor = Allopurinol!

Question 25

Mercaptopurine's effects can be diminished by xanthine oxidase. What can be added to therapy to prevent this?

Answer 25

A Xanthine oxidase inhibitor = Allopurinol!