Week 6 drugs

Question 1

Methotrexate

Answer 1

anti-neoplastic and anti-RA

blocks DHFR – inhibits folate metabolism

Question 2

Hydroxychloroquine

Answer 2

anti-RA

prevents acidification of macrophage cytosol; also blocks TLR-9 in DC which prevents IL and TNF release

Question 3

Leflunomide

Answer 3

anti-RA

inhibits pyrimidine synthesis by blocking the orotate pathway; affects DNA/RNA synthesis in T cells

Question 4

Sulfasalazine

Answer 4

anti-RA

alternative to Mtx; inhibits COX and scavenges free radicals

Question 5

Gold

Answer 5

anti-RA

reduces macrophage phagocytosis and affects APCs/T cells

Question 6

Cyclosporine

Answer 6

anti-RA

inhibits calcineurin, which inhibits T cells activation

Question 7

Etanercept and Inflixumab

Answer 7

anti-RA

block TNF action; Entanercept is a fake receptor coupled to TNF ab and Inflixumab is just a TNF ab

Question 8

Ankinra

Answer 8

anti-RA – not commonly used

IL-1 receptor antagonist

Question 9

Abatacept

Answer 9

anti-RA

binds CD80 on T cells to prevent APC activation of T cells

Question 10

Rituximab

Answer 10

anti-RA

binds CD20 which targets B cells for destruction, results in decreased Ab production

Question 11

ifosfamide

Answer 11

anti-neoplastic

alkylating agent that cross links DNA, converted to phosphoramide mustard in the liver; cell cycle non-specific

Question 12

etoposide

Answer 12

anti-neoplastic

blocks Topo II causing strand breaks; works in S and G2

Question 13

busulfan

Answer 13

anti-neoplastic

alkylating agent that cross links DNA, given prior to transplant; cell cycle non-specific

Question 14

fludarabine

Answer 14

anti-neoplastic

decreases DNA synthesis by interfering with dATP (purine blocker)

Question 15

Ara-C

Answer 15

anti-neoplastic

decreases DNA synthesis by interfering with dCTP (pyrimidine blocker)

Question 16

cisplatin

Answer 16

anti-neoplastic

alkylating agent that cross links DNA, contains platinum; cell cycle non-specific

Question 17

Mesna

Answer 17

given with cyclophosphamide and ifosfamide

binds acrolein, toxic product made when drug is converted to active form; used to prevent hemorrhagic cystitis

Question 18

Leucovorin

Answer 18

given as a rescue treatment for Mtx; admin. when folate levels drop too low – it replaces folate by allowing cells to bypass DHFR

Question 19

Delivered orally:

Answer 19

Cyclophosphamide/Ifosfamide are given orally because they need to be activated in the liver to form active drug

given with mesna

Question 20

Drugs that require kidney monitoring

Answer 20

Cyclophosphamide and Ifosfamide

Mtx and cisplatin

Question 21

Reason for Mtx monitoring

Answer 21

high plasma conc. are nephrotoxic and hepatotoxic; it is excreted renally

Question 22

Reason for Cyclophosphamide/Ifosfamide monitoring

Answer 22

acrolein bi-product is toxic; can lead to hemorrhagic cystitis

can also caused DNA translocation – AML

Question 23

Reason for cisplatin monitoring

Answer 23

most nephrotoxic anti-neoplastic drug known