Chemotherapy drugs Flashcards
What are the 6 classes of cytotoxic drugs?
- Alkylating drugs
- Platinating drugs
- Anti-metabolites
- Cytotoxic antibodies
- Mitotic inhibitors
- Topoisomerase inhibitors
What is the mechanism of action of alkylating agents?
The reactive alkyl group forms covalent bonds with DNA, crosslinking DNA & disrupting its replication & transcription
What are the 2 alkylating drugs?
Cyclophosphamide, chlorambucil
What are the 3 methods of resistance to alkylating agents?
- Decreased entry into or increased exit of agent from cell
- Inactivation of agent in cell
- Enhanced repair of DNA lesions produced by alkylation - upregulation of DNA repair genes
What are the 4 general side effects of chemotherapy?
- Myelosuppression
- Nausea, vomiting, GI effects
- Mucous membrane ulceration
- Alopecia
What is the mechanism of action of platinum-based chemotherapy drugs?
Platinum-based drugs act as alkylating agents, causing intra-strand crosslinks hence disrupting DNA replication & transcription
What are the 3 platinum-based chemotherapy drugs?
cisplatin, carboplatin, oxaliplatin
What are the adverse effects of platinum-based chemotherapy drugs?
Nephrotoxicity as excreted renally; contraindicated in patients with renal dysfunction
Cisplatin & oxaliplatin may cause peripheral sensory neuropathy
What is the mechanism of action of anti-metabolites?
Anti-metabolites interfere with the synthesis of nucleotides purine & pyramidine, inhibiting DNA replication
What are the 2 cell-cycle specific chemotherapy drugs?
Anti-metabolies & mitotic inhibitors
What are the 4 cell-cycle non-specific chemo drugs?
Alkylating, platinum-based, cytotoxic antibiotics & topoisomerase inhibitors
What are the 2 anti-metabolites?
Methotrexate & 5-fluorouracil
What is the mechanism of action of methotrexate?
Methotrexate is an anti-metabolite that inhibits dihydrofolate reductase, preventing thymidine monophosphate synthesis
What is the mechanism of action of 5-fluorouracil?
5-fluorouracil is an anti-metabolite which inhibits thymidylate synthase (TS) and is used in place of uracil, hence causing DNA damage
What are the clinical indications for methotrexate?
Lymphoma & breast cancer