Antimetabolites

Front 1

List of Antimetabolites

Back 1

ARA-A
ARA-C
5-FU
ThioGUANINE
Methotrexate
Tremethoprim
Pyremethamine
Azothioprine

Front 2

Methotrexate
MOA:
uses:
tox:
reverse

Back 2

MOA: S phase; folate analogue; blocks DHFReductase, thus DNA protein synth

uses: steroid resistant infxns, psoriasis, RA, leukemia, sarcoma, chorioCA, ectopic preg, molar preg, abortion

used to dx fragile x synd

tox: BM suppression, pulm fibrosis, liver failure, macrovesicular fatty liver, folate def, teratogenic, mucositis

BM suppression is reversible with leucovorin rescue (folinic acid)

Front 3

5FU
MOA:
uses:
tox
reverse tox

Back 3

MOA: S phase; pyrimidine analogue; inh thymidine synthase

uses: colon cancer, solid tumors, basal cell CA

tox: BM suppression, photosensitivity

reverse tox: thymidine

Front 4

6 mercaptapurine (6-MP)
MOA:
uses:
S/E:
CI:

Back 4

MOA: activated by HGPRTase; purine analogue; blocks de novo purine synthesis.

uses: leukemias, lymphomas (not CLL or Hodgkins- prednisone does these)

tox: BM, GI, liver; recognized by xanthine oxidase, promotes gout

CI: allopurinol

Front 5

6 thiaGUANINE
MOA:
uses:
S/E:

Back 5

MOA: activated by HGPRTase; guanine analogue; blocks de novo purine synthesis.

uses: ALL
S/E: does NOT cause gout (is not recognized by xanthine oxidase)

Front 6

Cytarabine:
MOA:
uses:
toxicity

Back 6

MOA: inh polymerase; pyrimadine analogue

uses: ALL, AML, Non-hodgkins

toxicity: low platelets, low WBC's megaloblastic anemia

Front 7

In general, antimetabolites are used to treat what type of cancers?

Back 7

fast growing

Front 8

clues for fast growing

Back 8

acute, anaplastic, undifferentiated, carcinoma, sarcoma

Front 9

Azothioprine:
MOA:
uses:
toxicity:

Back 9

MOA: converted to a purine analogue;
blocks DNA synthesis
uses: transplants, autoimmune dz's, RLDz, steroid resistant diseases
"STAR"
toxicity: gout, pancreatitis, liver tox, BM suppression

Front 10

which antimetabolites are used for steroid resistant infxns?
what NON-antimetaboite drug can be used for this too?

Back 10

antimetabolites
1st line: Methotrexate
2nd line: Azothiprine

NON-antimetabolite
3rd line- Cyclosporine

Front 11

Cyclosporine
(NOT an antimetabolite)
MOA:
uses:
tox:

Back 11

MOA: blocks calcineurin (which would dephosphorylate NFAT, which would bind to promoter for IL-2 formation)

uses: steroid resistant infections, Acute transplant rejections (where rejection that can occur up to 6 months post transplant)

tox: renal failure, gingival hyperplasia, hirsutism

Front 12

which antimetabolites cause gout?
which dont?

Back 12

cause gout: 6MP, Azothioprine,
dont: 6-thioGUANINE

Front 13

What drugs block calcineurin?

Back 13

Cyclosporin
Tacrolimus

Front 14

Which antimetabolites are deactivated by methylation in the liver?

Back 14

Azathioprine and 6MP