Anti cancer drugs 2
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- when do these drugs work best?
- In G1 and S phase but CAN work outside of that.
- Mechanism of action of alkylating agents?
- drugs are electrophilic and they attack the N7 position on guanine resulting in DNA damage by inter/intra strand cross linking, abnormal base pairing, DNA strand breakage
- Resistance to alkylating agents?
- increased repari, decreased permeability to drug and increased production of thiol trapping agents
- Prototype of alkylating agents?
- cyclophosphamide
- toxicity of cyclophosphamide?
- GI, myelosuppression, alopecia, HEMORRHAGIC CYSTITIS from acrolein (helped with mesna). cardiac dysfunction and pulmonary toxicity, inappropriate ADH secretion
- What type of drug is mechorethane?
- DNA alkylating agents
- Toxicity of mechlorethane/
- same and secondary cancer due o to induction of mutations in healthy tissues
- what is special about nitrosoureas?
-
very greasy can cross BBB and are used for brain tumors
they have high CNS toxicity - What is the toxicity of platinum agent cisplatinum?
- cisplatinum has little bone marrow effect. GI distress, mild hematotoxicity, neurotoxicity, NEPHROTOXICITY - which can be reduced with forced hydration.
- toxicity of carboplatin?
- Less nephrotoxic than cis but cause myelosuppression and hearing loss