Chemotherapy Flashcards
Major categories/ mechanisms of chemotherapy agents? (4)
DNA-damaging agents
- Coss-linking
- Free radical creators
DNA repair inhibitors
- anthracyclines
- topoisomerase inhibitors
Anti-metabolites
- pyramidine, purine antagonists
- anti folates
Anti-tubulin agents
- tubilin binding
- taxanes
Other
- bleomycin, mitomycin
Main types of DNA damaging chemotherapy drugs
Alkylating agents
Platinum compounds
Free radicals
Main types of Anti-tubulin chemotherapy agents?
Tubulin binding/ Vinka alkaloids (cincristine, vinorelbine)
Taxanes: paclitaxel, docetaxel
Main types of anti-metabolite chemotherapy drugs
Pyramidine antagonists
- 5-FU,
- capecitabine,
- cytarabine
Purine Antagonists
- mercaptopurine
- tioguanine
Folic acid antagonists
- methotrexate
- pemetrexed
How do alkylating agents work (in chemotherapy)
covalently bind alkyl groups,
major effect is to cross-link DNA
Example(s) of alkylating agents?
bendamustine
cyclophosphamide
How do platinum compund agents work (in chemotherapy)
cause interstand cross-links of DNA
Example(s) of platinum compound agent in chemotherapy?
cisplatin, carboplatin, oxaliplatin
How do antimetabolites work (in chemotherapy)?
usually structural analogues of naturally occurring metabolites that interfere with normal synthesis of nucleic acids by falsely substituting purines and pyrimidines in metabolic pathways.
Example(s) of Folic Acid antagonists (in chemotherapy)?
methotrexate
pametrexate
What is normally given with Folic Acid antagonists?
Folinic Acid.
To rescue normal tissue from the effect of high dose methotrexate.
Example(s) of Pyrimidine antagonists (in chemotherapy)?
5-Fluorouracil (5-FU)
Oral capecitabine is metabolized to 5-FU, as is tegafur with uracil.
Example(s) of Purine antagonists (in chemotherapy)?
6-mercaptopurine
6-tioguanine
Example(s) of Arabinosides (in chemotherapy)?
Cytarabine (used almost exclusively in the treatment of acute myeloid leukaemia)
What type of agents are anthracyclines?
Cytotoxic antibodies, (DNA repair inhibitors)
act by intercalating adjoining nucleotide pairs on the same strand of DNA and by inhibiting topoisomerase-II DNA repair
What type of agents are vincristine, vinblastine and vinorelbine?
Vinca Alkaloids (Anti-tubulin agents)
How do Vinca Alkaloids work (in chemotherapy)
binding to tubulin and inhibiting microtubule formation during mitosis
What type of chemotherapy agent is bendamustine and cyclophosphamide?
alkylating agents
What type of chemotherapy agent is cisplatin?
platinum compound
What type of chemotherapy agent is methetrexane a pametrexate?
Folic Acid antagonists
What type of chemotherapy agent is 5-Fluorouracil (5-FU)?
Pyrimidine antagonists
What type of chemotherapy agent is 6-mercaptopurine,
6-tioguanine?
Purine antagonists
How do arabinosides work (in chemotherapy)? E.g cytarabine
inhibit DNA synthesis by inhibiting DNA polymerase
What are the 5 most common chemotherapy side effects?
- CTZ targeted (chemoreceptor trigger zone) -> nausea
- Hair targeted (alopecia)
- Endothelial cells targeted (mucosal lining)
- Myelosuppression
- Ovaries/ gonads targeted
Also fatigue/ chemo brain
Folfox combination?
Oxaliplatin, 5-fluorouracil, folinic acid
Chemo particularly associated with cardiotoxicity?
anthracyclines (e.g. daunorubicin, doxorubicin, epirubicin)
This is a rare side-effect of chemotherapy and is usually associated with anthracyclines such as doxorubicin;
effects can present as an acute arrhythmia during administration or cardiac failure due to cardiomyopathy after chronic exposure. This effect is dose-related and can largely be prevented by restricting the cumulative total dose of anthracyclines within the safe range
5 FU and its prodrug, capecitabine, can cause cardiac ischaemia.
How do taxanes work? (In Chemo)
bind to tubulin dimers and prevent their assembly into microtubules.
(e.g. paclitaxel and docetaxel)
Which chemo agents are particularly associated with nausea?
platinum agents
Chemo agents particularly associated with skin toxicity?
5-FU, capecitabine and docetaxel
Agent to ameliorate severe chemotherapy- and radiotherapy-induced mucositis.
Palifermin (Kepivance), a recombinant keratinocytederived growth factor
Particular anti-emetic used in chemotherapy?
Aprepitant, a neurokinin receptor antagonist, is helpful in preventing acute and delayed nausea and vomiting.
used with dexamethasone and a 5-HT 3 antagonist.
Drugs such as cyclizine, olanzapine and levomepromazine, and benzodiazepines, can be used to control persistent nausea.
Chemo agents associated with neurotoxicity?
Vinca alkaloids, taxanes and platinum analogues (but not carboplatin).
It is dose-related and cumulative.
Vinca alkaloids, such as vincristine, must never be given intrathecally, as the neurological damage is progressive and fatal.
Chemo agents associated with nephrotoxicity?
Cisplatin (but not oxaliplatin or carboplatin), methotrexate and ifosfamide can potentially cause renal damage.
Avoid with hydration
Chemo agents associated with sterility?
- alkylating agents
- anthracyclines
- docetaxel
Chemo agents particularly associated with secondary malignancies?
The alkylating agents, anthracyclines and epipodophyllotoxins are particularly implicated.
