Alkylating Agents Flashcards
What cancer drug prevents DNA synthesis by blocking DHFR?
Is it cell cycle specific or nonspecific?
Methotrexate
CCS to S-phase
What cancer drug inhibits DNA synthesis by blocking thymidylate synthase? Does this affect pyrimidines or purines? Is it cell cycle specific or nonspecific?
5-fluorouracil
pyrimidines
S-phase
What cancer drug prevents DNA synthesis by blocking DNA polymerase? Is it cell cycle specific or nonspecific?
Fludarabine
CCS for S-phase
What are the 3 alkylating agents we learned?
cyclophosphamide
ifosfamide
bulsulfan
What do the alkylating agents do? Are they cell cycle specific or nonspecific?
They damage DNA by forming cross links in the DNA
THey’re cell cycle nonspecific
What is the drug that contains platinum and causes DNA damage by cross-linking DNA?
cisplatin
How does Doxorubicin damage DNA? Cell cycle specific or nonspecific?
It intercalates the DNA
Cell cycle nonspecific
What drug causes DNA damage by blocking the action of topoisomerase 2? Is it cell cycle specific or nonspecific?
Etoposide
It’s CCS to s-phase through to G2
How does Paclitaxel work? Is it cell cycle specific or nonspecific?
It is antimitotic that stabilizes the microtubules so they can’t divide during M phase.
What will all cycotoxic drugs cause as side effects?
They will damage rapidly dividing cells, so…
bone marrow suppression
GI tract - nausea, vomiting, diarrhea
Alopecia
What is the very seriously side effect that can arise from any cancer drug that causes DNA damage as it’s main mode of action (so cyclophosphamide, ifosfamide, bulsulfan, and cisplatin)?
they can be carcinogenic, mutagenic, and teratogenic
in particular, they can cause secondary AML
Which 4 drugs have negative side effects on the renal system (or bladder in one instance)?
Methotrexate
cisplating
cyclophosphamide, ifosfamide
Why is cisplatin bad for the renal system?
It’s a heavy medal which can clog the renal tubules and limit the GFR
How do cyclophosphamide and ifosfamide damage the bladder? What is the side effect this can cause? What drug is given to counteract this?
Once it reaches the tumor, it is metabolized into two things;
- phosphoramide mustard, which is the active agent
- acrolein, which is urotoxic and causes bladder damage
you can get hemorrhagic cystitis
treat with mesna, which will inactivate the acrolein
Why does renal function need to be monitored when giving methotrexate?
It is excreted in the urine and if it doesn’t, you’ll get severe myelosuppression
the primary issue is that it’s a weak acid, so it may not be excreted quite as well
