Chemotherapeutics Flashcards
What happens in the M stage of the cell cycle
mitosis
What happens in the G0 stage of the cell cycle
resting
What happens in the S stage of the cell cycle
synthesis - doubling of cell’s DNA
list the 6 major categories of anticancer drugs
alkylating agents
antimetabolites
antitumor antibiotics
topoisomerase inhibitors
tubulin binding drugs
signal transduction modifiers
How does intermittent chemotherapy work?
allow for breaks from chemo for highly proliferative cells to regrow
**malignant cells must grow slower than normal cells for this to be effective
How do phase specific chemotherapeutic agents work?
they only work during a specific phase of the cell cycle
How do phase non-specific agents work?
work during several phases of the cell cycle
List the tissues that are highly damaged from chemotherapeutics
rapidly proliferating cell types
- bone marrow
- GI tract
- hair
- reproduction
List some symptoms of extravasation of chemotherapeutics
pain
burning
swelling
redness
lack of blood return
List some alkylating agents
nitrogen mustards (Cyclophosphamide)
nitrosureas (Carmustine)
platinum compounds (Cisplatin, Carboplatin)
How do alkylating agents work?
reactive alkyl groups form covalent bonds with nucleotide bases in RN/DNA –> DNA cannot uncoil to replicate
Major AE of alkylating agents
bone marrow suppression
Unique serious AE of carmustine
pulmonary toxicity
List some platinum compounds
Cisplatin
Carboplatin
Oxaliplatin
Mechanism of action of platinum compounds
similar to alkylating agents (often classified with them)
cross links DNA –> cannot uncoil –> cannot replicate
Major toxicities for platinum compounds
nephrotoxicity
peripheral neuropathy
severe N/V
bone marrow suppression
otoxocity
List some antimetabolites
folate analogues (methotrexate)
pyrimidine analogues (fluorouracil)
purine analogues (mercaptopurine)
mechanism of action of antimetabolites
structural analogues of endogenous metabolites. Inhibit DNA via one of:
- direct enzyme inhibition
- incorporation directly into DNA
What phase of the cell cycle do antimetabolites target
S
mechanism of action of methotrexate
binds dihydrofolate reductase w/ higher affinity than folate. Thus prevents formation of FH4 which is required for nucleoside synthesis
(results in decreased DNA/RNA/protein synthesis)
Toxicities that are SPECIFIC to methotrexate
pulmonary fibrosis/edema
renal toxicity
hepatic toxicity
Toxicities that are SPECIFIC to fluorouracil
increased risk of MI x1 week post-admin
neurologic defects
hand & foot syndrome
Mechanism of action of topoisomerase inhibitors
inhibit topoisomerase, thus DNA cannot uncoil –> replication cannot occur
List some topoisomerase inhibitors
topotcan
irinatecan
etoposide
teniposide
anthracycline (doxorubicin, danorubicin)
non-anthracyclines (bleomycin)
