Chemo Drugs Flashcards
Agents Directly Modifying DNA Structure
Anthracycline Antibiotics
Bleomycin
Cisplatin/Cyclophospamide
Antimetabolites
5-FU
Methotrexate
– interfere with precursors to purine and pyrimidine synthesis
Microtubule Inhibitors
Vinca alkaloids and Taxanes
Doxorubicin and Daunorubicin
Anthracycline Antibiotic
The molecule first intercaltes in DNA, stopping transcription and replication.
The intercalated antibiotic molecule physically interferes with
Topoisomerase II activity which normally repairs DNA
Generate free radicals by binding to Fe2+ that lead to apoptosis after DNA damage.
Bleomycin
Glycopeptide antibiotic
Produces free radicals with Fe2+
Attack phosphodiester bonds in the DNA
strand resulting in a cutting or scission of DNA strands.
Most effective during G2
Pulmonary
toxicity
Cytotoxic alkylating agents
Covalently Bind to DNA cross linking it
The maximal effect of alkylating agents is during ‘S’ phase.
Methotrexate
Methotrexate acts by inhibiting DHFR to interfere with folate metabolism
Folates are vital for production of purine nucleotides and thymidilate
Stopping DNA and RNA synthesis
Antimetabolites are cell cycle specific in their action – ‘S’ phase
5 fluro uracil
5-FU is an analogue of the pyrimidine base uracil. This inhibits Thymidilate synthesis
Thymidine-less cell death
Antimetabolites are cell cycle specific in their action – ‘S’ phase
Vinca alkaloids
Vincristine
and vinblastine
Specifically binding with the B-tubulin subunit that then
prevents formation of the microfilaments that make up the microtubule. This means the
mitotic spindle does not form and the cell cycle is arrested in mitotic metaphase.
Taxanes
Paclitaxel
Binding stabilises
the microtubules and inhibits their disassembly. These microtubules are rendered nonfunctional
and they cannot disassemble to pull the chromosome apart
