alkylating agents Flashcards
(18 cards)
generally what is the mechanism of alkylating agents ?
they add an alkyl group to nucleotide bases they all cross link DNA
inhibit DNA replication and cause DNA damage
what is the association of alkylating agents with the cell cycle ?
all of them are cell cycle non specific
what are the alkylating agents ?
busulfan
nitrosoureas
nitrogen mustards
procarbazine
what are examples of nitrogen mustards ?
cyclophosphamides
what is the specific function of cyclophosphamide ?
guanin N7 alkylating agents
what is the specific side effect associated with cyclophosphamide ?
hemorrhagic cystitis
SIADH - associated with hyponatremia and seizures
which metabolite of cyclophosphamide is toxic to the bladder ?
acrolein
what are the uses of cyclophophamide ?
solid tumors , leukemia , lymohoma
how is cyclophophamide activated ?
by the liver through the p450 enzymes
how can we lower the levels of acrolein in association with cyclophophamide ?
proper hydration and the use of mesna
what are the side effects associated with ifosfamide ?
nephrotoxicity - may cause fanconi syndrome
encephalopathy
what are the nitrosureas and where are they activated ?
ay 7aga with must in the middle , activated in the liver
what are the main uses for nitrosoureas ?
mainly used for brain tumors
specifically glioblastoma multiforme
what are the side effects associated with nitrosoureas ?
encephalopathy and seizures
pulmonary fibrosis
myelosuppression
what is busulfan used for ?
used to ablate the patients BM before transplantation - myeloablation
what are the toxicities associated with busulfan ?
myelosuppression
skin hyperpigmentation
seizures
pulmonary toxicity
what is dacarbazine used for ?
part of the ABVD protocol for hodgkin lymphoma
what is procarbazine used for and what is the MOA ?
it is a weak MAO inhibitor that is used as part of the MOPP protocol for Hodgkin lymphoma