Cytotoxic Agents Flashcards
name alkylating agents
- cyclophosphamide
what is the mechanism of action of cyclophosphamide?
- alkylating agent
- causes cross-linking in DNA
what are the adverse effects of cyclophosphamide?
- haemorrhagic cystitis
- myelosuppression
- transitional cell carcinoma
name cytotoxic antibiotics
- bleomycin
- anthracyclines (e.g. doxorubicin)
what is the mechanism of action of bleomycin?
degrades preformed DNA
what is the adverse effect of bleomycin?
- lung fibrosis
what is the mechanism of action of anthracyclines?
e.g. doxorubicin
stabilises DNA-topoisomerase II complex inhibits DNA and RNA synthesis
what is the adverse effect of anthracyclines?
e.g. doxorubicin
cardiomyopathy
name antimetabolites
- methotrexate
- fluorouracil (5-FU)
- 6-mercaptopurine
- cytarabine
what is the mechanism of action of methotrexate?
inhibits dihydrofolate reductase and thymidylate synthesis
what are the adverse effects of methotrexate?
- myelosuppression
- mucositis
- liver fibrosis
- lung fibrosis
what is the mechanism of action of fluorouracil?
pyrimidine analogue inducing cell cycle arrest and apoptosis by blocking thymidylate synthase
what are the adverse effects of fluorouracil?
- myelosuppresion
- mucositis
- dermatitis
what is the mechanism of action of 6-mercaptopurine?
purine analogue that is activated by HGPRTase, decreasing purine synthesis
what is the adverse effect of 6-mercaptopurine?
myelosuppression
what is the mechanism of action of cytarabine?
- pyrimidine antagonist
- interferes with DNA synthesis and inhibits DNA polymerase
what are the adverse effects of cytarabine?
- myelosuppression
- ataxia
name drugs which act on microtubules
- vincristine, vinblastine
- docetaxel
what is the mechanism of action of vincristine and vinbalstine?
inhibits formation of microtubules
what are the adverse effects of vincristine?
- peripheral neuropathy (reversible)
- paralytic ileus
what is the adverse effect of vinblastine?
myelosuppression
what is the mechanism of action of docetaxel?
prevents microtubule depolymerisation and disassembly, decreasing free tubulin
what is the adverse effect of docetaxel?
neutropenia
name topoisomerase inhibitors
- irinotecan
what is the mechanism of action of irinotecan?
inhibtis topoisomerase I which prevents relaxation of supercoiled DNA
what is the adverse effect of irinotecan?
myelosuppression
what is the mechanism of action of cisplatin?
causes cross-linking in DNA
what are the adverse effects of cisplatin?
- ototoxicity
- peripheral neuropathy
- hypomagnesaemia
what is the mechanism of action of hydroxyurea (hydroxycarbamide)?
inhibits ribonucleotide reductase, decreasing DNA synthesis
what is the adverse effect of hydroxyurea (hydroxycarbamide)?
myelosuppression
what is the adverse effect of hydroxyurea (hydroxycarbamide)?
myelosuppression
