Chemo Drugs I

Question 1

Cyclophospamide

• type
• mechanism
• tox (3)

Answer 1

Nitrogen Mustard=Alkylating Agent

Forms DNA cross links resulting in inhibition of DNA syn and fxn

Acute-N/V
Delayed-decease of peripheral BC
Excessive-Severe bone marrow depression and hemorrhagic cystitis

Question 2

Carmustine

• aka
• type
• mechanism
• Tox (3)
• delivery

Answer 2

Nitrosurea

Alkylating agent-DNA cross link of n7 and O6 of guanine and GC cross links

Acute-N/V
Delayed-Myelosuppresion
Rare-Gives interstitial lung disease or nephritis

Highly lipid soluble-can enter CNS, given orally

Question 3

Procarbazine

• type
• mechanism
• Tox (5)

Answer 3

Non-classic alkylating agent

inhibits DNA, RNA, and protein synthesis

1. Acute-NV
2. Delayed-myelosupression
   - high risk secondary malignancy
3. Adverse drug reaction due to MAOI metabolite activity
4. Adverse interaction with ETOH, CNS dep, antihistamines, anti-dep

Question 4

Cisplatin

• type
• mechanism
• part of CC when fxn best
• Tox (2)
• special

Answer 4

Pt based alkylating agent

sticks to DNA strands, cyto/nuc proteins

Cytotoxic at all stages of cell cycle

Acute-highly emeticgenic
Delayed-nepho/oto tox, and irreversible nerve dysfxn

synergy well with other chemo agents

Question 5

Methotrexate

• type
• mechanism
• part of CC when fxn best
• Tox (4)
• special (2)

Answer 5

Folic acid analog-binds and inhibits Dihydrofolate reductase and thymidylate synthase (cant make thymine)

S

Mucositis, diarrhea, neutropenia, and thombocytopenia (myelosup)

Leucovorin reverses effects
Resistance occurs

Question 6

Leucovorin (2)

Answer 6

Reduced folate

Treats methotrexate poisoning

Question 7

5-FU

• aka
• type
• mechanism
• part of CC when fxn best
• Tox (4)
• special

Answer 7

Fluorouracil

Antimetabolite-purine analog

Orally inactive
Inhibits TS while metabolites inhibit DNA and RNA fxn (DNAi/RNAi)

S

Myelosup
NVD/mucositis
neurotox
Hand-Foot blistering syndrome at continuous infusion

Severe tox in decreased/absent DPD

Question 8

DPD-AKA and mech

Answer 8

dihydropyramidine dehydrogenase

DPD in saliva catalyzes 85% of dose of 5-FU

Question 9

Capecitabine

• type
• mechanism
• part of CC when fxn best
• Tox (2)

Answer 9

Antimetabolic-purine analog

Orally active
Pro-pro drug of 5FU-active metabolites are generated in liver and then converted to 5FU in tumor (inhibit TS and D/RNAi stuff)

S

Continuous infusion-Hand-Foot and D
Alopecia

Question 10

Cladribine

• type
• mechanism (2)
• Tox (3)

Answer 10

Purine analog

Inhibit ribonucleotide reductase-inhibits DNA syn/repair
Incorporated into DNA to induce apop

Myelosup
Immunosup (CD4 and CD8 T cells)
N/V

Question 11

6-Meracaptopurine

• type
• mechanism (2)
• Tox (2)
• Special (2)

Answer 11

Purine antagonist

Inhibits enzymes of purine syn
Incorporated into both RNA and DNA

Myelosup
diarrhea

Severe tox at TPMT def or Allopurinol (degraded by xanthine oxidase)

Question 12

TPMT-aka and special

Answer 12

Thiopurine methyltrasferase

@deficiency gives severe myelosup and diarrhea when given with 6-Mercaptopurine

Question 13

Allopurinol-mech and special

Answer 13

Xanthine oxidase inhibitor

XO inhibits 6-Meracaptopurine so results in toxicity when given together

Question 14

Vincristine

• type
• mech
• part of CC when fxn best
• Tox (4)

Answer 14

Natural product-Vinca alkaloid

Binds to beta tubulin and inhibits assembly=arrest in M phase

M

Neurotox+peripheral neuropathy
ANS dysfxn (ortho htn, uriinary retention)
SIADH
Myelosupression

Question 15

Paclitaxel

• type
• mech
• part of CC when fxn best
• Tox (2)
• Special (2)

Answer 15

Taxane

Enhance microtubule polymerization

M

Acute NV and hypotension
Delayed-Neurotix, peripheral sensory neuropathy, and myelosuppresion

• Acute-Hypersensitivity (prevent with dexamenthasome or diphenyldramine
• p53 metabolism-adjust dose @liver dysfxn

Question 16

Abraxane

• type (2)
• mech
• part of CC when fxn best
• Tox

Answer 16

Taxane
Paclitaxel bound to protein or albumin-avoids hypersensitivity

Enhance microtubule polymerization

M

Decreased tox when compared to Paclitaxel

Question 17

Irinotecan

• Type
• Mech
• part of CC when fxn best
• Tox (2.5)

Answer 17

Natural Product-Campthecin

Topisomerase I inhbiitor-DNA damage and S phase arrest

S

Serious diarrhea
-early is cholinergic
-late (2-10 days) is severe
Bone marrow sup

Question 18

Doxorubicin

• Type
• mech (2)
• part of CC when fxn best
• Tox (3)
• Special

Answer 18

Antibiotic-Anthracycline

Inhibits Topisomerase II
-high affinity for DNA intercalation (blocks DNA and RNA syn
Generates quinine free radicals-binds to cell membranes and alters fluidity/transport

G1-G2

Cardiotox (via semi-quinone free radicals
-acute (2-3d) arrhythmias
-Chronic-dose dependent dilated cardiomyopathy
Myelosuppresion with neutropenia

Trx with Dexrazoxane-Can reduce cardiotox events in high risk pts

Question 19

Dexrazoxane (mech and special)

Answer 19

Fe chelator

Reduce cardiotox events in Doxorubicin pts

Question 20

Bleomycin

• type
• mech
• part of CC when fxn best
• Tox

Answer 20

Antibiotic

Binds DNA-causes breaks and inhibits DNA synthesis-G2 arrest

G2-M

Pulmonary fibrosis

Question 21

Mitomycin C

• type
• mech
• part of CC when fxn best
• tox (2)
• special

Answer 21

Antibiotic

Potent cross linker via alkylation

Acts during all phases

NV and HUS

Needs to be reduced (tumors make hypoxic environment which favors reduction)

Question 22

DO CHEMO MAN

Answer 22

DO CHEMO MAN