chemotherapy Flashcards
what are the 4 main therapeutic agents used in chemotherapy?
alkylating agents
antimetabolites
cytotoxic antibodies
plant derivatives
what do alkylating agents do to cause conformational changes in DNA?
they form covalent bonds with nucleophilic substances in the cell and cross link DNA which prevents DNA polymerase accessing to replicate the DNA
how exactly is the DNA changed by alkylating agents?
modifies guanine so it mispairs with Thymine which causes the cell to undergo apoptosis
what type of alkylating agent is cyclophosphamide?
a nitrogen mustard
what enzyme in the liver activates cyclophosphamide?
p450 enzymes
what is the cytotoxic product of nitrogen mustards?
phosphor amide mustartd
what is the toxic by-product of the activation of nitrogen mustards which is counteracted by mesna?
acrolein
which alkylating agent is used in chronic granulocyte leukaemia to prevent formation of granulocytes and platelets in low dosage and RBCs in high dosage?
Busulphan (an alkylsulphonate)
which type of alkylating agent is used to treat brain tumours because of its lipid soluble properties which allow it to cross the blood-brain barrier?
nitrosoureas (eg lomustine and carmustine)
what class of alkylating agent is a water soluble complex?
platinum based compounds (e.g. cisplatin)
what are the three classes of antimetabolite chemotherapy drugs?
antifolates
antipyrimidines
antipurines
what is an example of the drug which is a competitive inhibitor of the folate pathway and is giving orally usually?
methotrexate
what are two examples of antipyrimides which mimic the structure of pyrimidines and inhibit DNA polymerase?
Fluorouracil (5-FU) gemcitabine (and its analogue cytarabine)
what are some examples of antipurines which act as fraudulent nucleotides and inhibit DNA polymerase?
mercaptopurine, thioguanin, fludarabine
what are the four different cytotoxic antibiotic classes?
anthracyclines
dactinomycin
bleomycin
mitomycin