Cytotoxic drugs Flashcards
Cyclophosphamide MOA
alkylating agent - causes cross-linking in DNA
Cyclophosphamide adverse effects
haemorrhagic cystitis
myelosuppression
transitional cell carcinoma
Bleomycin MOA
degrades preformed DNA
Bleomycin adverse effects
lung fibrosis
Anthracyclines (eg. doxorubicin) MOA
stabilises DNA topoisomerase 2 complex
inhibits DNA and RNA synthesis
Anthracyclines (eg. doxorubicin) adverse effects
cardiomyopathy
Methotrexate MOA
inhibits dihydrofolate reductase and thymidylate synthesis
Methotrexate adverse effects
myelosuppression
mucositis
liver fibrosis
lung fibrosis
Fluorouracil MOA
pyrimidine analogue inducing cell cycle arrest and apoptosis by blocking thymidylate synthase (works during S phase)
Fluorouracil adverse effects
myelosuppression
mucositis
dermatitis
6-mercaptopurine MOA
purine analogue that is activated by HGPRTase, decreasing purine synthesis
6-mercaptopurine adverse effects
myelosuppression
Cytarabine MOA
pyrimidine antagonist
interferes with DNA synthesis specifically at S phase of cell cycle and inhibits DNA polymerase
Cytarabine adverse effects
myelosuppression
ataxia
Which cytotoxic drug is an alkylating agent?
cyclophosphamide
Which cytotoxic drugs are cytotoxic antibiotics?
bleomycin
anthracyclines (eg. doxorubicin)
Which cytotoxic drugs are antimetabolites?
methotrexate
fluorouracil
6-mercaptopurine
cytarabine
Which cytotoxic drugs act on microtubules?
vincristine/vinblastine
docetaxel
Which cytotoxic drugs are topoisomerase inhibitors?
irinotecan
Vincristine/vinblastine MOA
inhibits formation of microtubules
Vincristine/vinblastine adverse effects
vincristine = peripheral neuropathy (reversible), paralytic ileus
vinblastine = myelosuppression
Docetaxel MOA
prevents microtubule depolymerisation and disassembly, decreasing free tubulin
Docetaxel adverse effects
neutropenia
Irinotecan MOA
inhibits topoisomerase I which prevents relaxation of supercoiled DNA
Irinotecan adverse effects
myelosuppression
Cisplatin MOA
causes cross-linking in DNA
Cisplatin adverse effects
ototoxicity
peripheral neuropathy
hypomagnesaemia
Hydroxyurea (hydroxycarbamide) MOA
inhibits ribonucleotide reductase, decreasing DNA synthesis
Hydroxyurea adverse effects
myelosuppression