Chemo Rx Flashcards
CYTOTOXIC Chemotherapeutic agents can be divided into two groups based on their effects at different stages of the cell cycle and have effects on different types of cancer:
- Cell-cycle specific (CCS): hematologic malignancies, solid tumors high growth fraction
- Cell-cycle non-specific (CCNS): solid tumors with low or high growth fraction
What are the 3 bone-marrow sparing chemotherapy agents?
- bleomycin
- cisplatin
- vincristine
Alkylating agents are mutagenic and can lead to _____. Which is the most likely to cause this?
- leukemia
- Procarbazine
List the 4 alkylating agents (chemo rx)
- Cyclophosphamide
- Procarbazine
- Cisplatin
- Carboplatin
Which 2 alkylating agents are platinum analogs?
- cisplatin
- carboplatin
(-“platin” rx = platinum)
The log kill hypothesis says that chemotherapy drugs are ______ kinetics
first order
(3 log kill = 109 -10 6 cancer cells)
_______ (3 chemotherapeutic agents) cause pulmonary side effects .
- Bleomycin
- Busulfan
- Procarbazine
(“Bleomycin & Busulfan Block your Breath”)
________( 2 chemotherapeutic agents) cause cardiotoxicity.
- Mitoxantrone (least cardiotoxic)
- Dexrazoxane (delayed CHF)
Which chemo rx cause nephrotoxicity?
- Cisplatin
- Methotrexate (Pemetrexed)
______ treats nephrotoxicity caused by Cisplatin
Amifostine
Side effect shared by vinka alkaloids, -“taxanes” and Procarbazine
neurotoxicity
_____ is the chemo rx least likely to cause neurotoxicity
Vinblastine
(does BLAST the Bone marrow though)
Hemorrhagic cystitis is an adverse reaction to ________ (chemo rx).
Cyclophosphamide
______ is a second generation platinum analog (alkylating agent) and therefore, has less toxicity.
(myelosuppression is the main dose-limiting toxicity)
carboplatin
(second gen. to cisplatin)
Neurotoxicity and ototoxicity are the side effects of _______.
cisplatin
(platinum analog - alkylating agent)
The MOA for the alkylating agents is the alkyl group forms a _______ leading to DNA strand breakage.
cross-link
(cell-cycle checkpoints will recognize → apoptosis)
Hepatic VOD is an adverse effect of the ______ class of chemo rx.
alkylating agents
5 Mechanisms of resistance against alkylating agents
- increase glutathione
- increase DNA repair
- decrease permeability to agent
- degrade rx
- impair apoptotic pathways
Cyclophosphamide is converted into _______ which alkylates DNA → cytotoxicity.
phosphoramide mustard & acrolein
Which alkylating agent treats NHL, breast, ovarian, neuroblastoma and leukemia?
cyclophosphamide
______ (alkylating agent) makes free radicals and converts CYP into methylating species.
Procarbazine
(inhibits DNA & RNA synthesis)
Procarbazine is also a ______ inhibitor.
MAO
(caution w/patients on SSRI/SNRI)
______ (alkylating agent) treats Hodgkin and brain tumors
Procarbazine
BM suppression, pulmonary toxicity, neurotoxicity are _____ (alkylating agent) side effects
Procarbazine side effects
Platinum analogs form intra- and inter-strand cross-links causing cytotoxicity used to treat ________ (5) cancers.
solid tumor: breast, lung, bladder, testicular, ovarian
Antimetabolite chemo rx are considered ____(CCS/CCNS)
CCS
Antimetabolic chemo rx inhibit DNA and RNA synthesis by interfering with ________.
purine or pyrimidine nucleotide precursors
________ MOA: inhibits dihydrofolate reductase → decreased thymidylate, purine nucleotides and amino acids.
methotrexate & pemetrexed
Decreased rx transport into cell, increased dihydrofolate reductase & decreased sensitivity to rx are the mechanisms of resistance to _______ (antimetabolite chemo rx)
methotrexate & pemetrexed
Which 2 antimetabolite chemo rx treat leukemia, lymphoma & breast cancer?
- methotrexate & pemetrexed
- mercaptopurine & thioguanine
(5-fluorouracil also treats breast cancer)
Which antimetabolite chemo rx are pyrimidine antagonists*** and which are pyrimidine ***analogs?
- antagonists: cytarabine, capecitabine
- analog: fluorouracil
(not to be confused w/the purine antagonist: Fludarabine)
_______ (antimetabolite chemo rx) is a DNA polymerase inhibitor → terminates chain elongation.
Cytarabine
(tx for AML)
Cytarabine is the only antimetabolite chemo rx that treats _____.
AML
Fluorouracil has no antineoplastic activity, but is converted to _____→ inhibits DNA synthesis by inhibiting _____. How does it inhibit RNA synthesis?
- 5-FdUMP
- thymidylate synthase
- conversion to 5-FdUTP
Fluorouracil treats solid tumors, such as : (3)
- breast
- colon
- gastric
(can cause life-threatening diarrhea)
2 Resistance mechanisms of 5-FU
- increase thymidylate synthase levels
- increase DPD (dihydropyrimidine) → catabolize 5-FU
(pts w/decreased DPD → toxicity)
Caution in combo therapy: cisplatin & ______ have a drug interaction
methotrexate
Capecitabine is a prodrug that is converted into ______.
5-FU
(same MOA & target cancers)
______ is a unique side-effect of Capecitabine (antimetabolite chemo rx).
Hand-foot syndrome
(erythema of hands and feet)
______ inhibits ribonucleotide reductase → decreasing the pool of nucleotides for DNA synthesis
Gemcitabine (antimetabolite chemo rx)
(must be phosphorylated first)
Which antimetabolite chemo rx treats pancreatic, non-small cell lung and bladder cancer?
Gemcitabine
Which antimetabolite chemo rx treats low-grade NHL & CLL?
Fludarabine
________ (2) are converted to TIMP by HGPRT → blocks purine synthesis
- Mercaptopurine (6MP)
- Thioguanine (6TG)
(antimetabolite chemo rx)
Doses of 6MP must be reduced in patients taking ______.
allopurinol
Skin pigmentation, adrenal insufficiency, and pulmonary fibrosis are side effects of ______.
Busulfan