Chemo Drugs 4: Antimetabolites

Question 1

Methotrexate (antifolate)
YELLOW drug

class/MoA
CCS
admin
Rescue
Use

Answer 1

class: antimetabolite
MoA: inh DIHYDROFOLATE REDUCTASE
CCS: S ph
INTRATHECAL admin = meningitis
POLYGLUTAMATED = stays in CA cells and inh purine and thymidylate synth.
high dose w/ LEUCOVORIN (tetrahydrofolate rescue of BM and epi cells)
Use: first cure of choriocarcinoma

Question 2

5 qualities of Methotrexate

table things

Answer 2

1. highly protein bound: interacts w/ penicillin, sulfonamides
2. distributes: total body water = ascites and pleural effusions
3. solubility inc alkaline pH
4. probenecid dec renal exretion via inc H+, inc toxicity
5. dose red: renal insufficiency

Question 3

Cytarabine
(CYTOSINE arabinoside)

class/MoA
Sch X X
BioA
admin/use

Answer 3

class: antimetabolite - pyrimidine antag
MoA: inh DNA polymerase, incoporates, inh chain elongation
sch dep CYTOTOXICITY
CCCS: S-ph
Bio: phosphorylation
INTRATHECAL admin = meningitis
use: ALL 3+7 REGIMEN red doxorubicin & continuous IV cytarabine

Question 4

5-Fluorouracil (5-FU)

class/MoA
CCS
Inc Toxicity
AE
Use

Answer 4

class: antimetabolite
MoA: inc into RNA and DNA. Phosphorylated to 5-DUMP, binds thymidylate syntehetase = THYMINELESS DEATH of cells
CCS: S-ph
Inc Toxicity: LEUCOVORIN coadmin (and cytotoxicity), DIHYDROPYRIMIDINE deficiency
AE: hyperpig, inc sens. sun, cerebellar ataxia, lacrimation, HFoot syn
Use: radiation sensitizer

Question 5

6-mercaptoPURINE

class/MoA
CCS
Met
Drug interaction
Use

Answer 5

class: antimetabolite - purine antag
MoA: inh denovo PURINE SYNTH enzymes, inc DNA
CCS: S-ph
Met: XANTHINE OXIDASE
DI: REDUCE 6MP by 50-75% if given to pt on allopurinol
Use: Kid Acute lymphoblastic leukemia (ALL)

Question 6

Name all of the bis(chloroethyl)amine Alkylating Agents “mide”(3)

Answer 6

Cyclophosphamide
Ifosfamide
Temozolomide

Question 7

Name all of the platinum coordination compound Alkylating Agents “platin”(3)

Answer 7

Cisplatin (aka Cis-DDP aka Cis-diaminedichloroplatinum II)
Carboplatin
Oxaliplatin

Question 8

Name all of the Plant Alkaloids (4)

Answer 8

Vincristine
Vinblastine
Taxol (aka Paclitaxel)
Etoposide

Question 9

Name all of the ABX antitumor agents (3)

DIB

Answer 9

Doxorubicin
Irinotecan
Bleomycin

Question 10

Name all of the Hormonal Agents (6)

Answer 10

Prednisone
Dexamethasone
Tamoxifen
Anastrozole
Flutamide
Leuprolide acetate

Question 11

Name all of the Antimetabolites (4)

56 Meth “Cytes”

Answer 11

Methotrexate (antifolate)
Cytarabine
5-Fluorouracil (5-FU)
6-Mercaptopurine

Question 12

Name the Miscellaneous Agents (4)

HAAA

Answer 12

Asparaginase
Hydroxyurea
All trans retinoic acid (tretinoin)
Arsenic trioxide

Question 13

Name the Small molecule Inh “nib” (4)

VICE

Answer 13

Vemurafenib
Imatinib
Crizotinib
Erlotinib

Question 14

Name all the Monoclonal Antibodies “mab” (3)

Answer 14

Cetuximab
Trastuzumab
Bevacizumab