Alkylating agents Flashcards
Name the 3 drugs in the nitrogen mustard class…
Mechlorethamine
Cyclophosphamide
Ifosfamide
Produce strong electrophiles through carbonic or ethyleneimonium ion intermediates–> covalently bond via alkylation of nucleophilic moieties in DNA
Alkylating agents
Name the alkylating agent that spontaneously converts to active metabolites in body fluids or enzymatically converts in the liver…
Mechlorethamine
Which 2 alkylating agent converts by hepatic cytochrome P450 to active metabolite phosphoramide mustard?
Cyclophosphamide and Ifosfamide
Name the 2 Nitrosoureas alkylating agents…
Carmustine
Lomustine
Alkylating agent used for the treatment of Hodgkin’s disease, T-cell lymphoma…
Mechlorethamine
What are the side effects of Mechlorethamine?
Severe N/V
Myelosuppression–leucopenia and thrombocytopenia
Which of the alkylating agents is the most widely used for ALL, CLL, non-hodgkins lymphoma, breast, lung and ovarian cancers?
Cyclophosphamide
Which alkylating agent is used for Sarcoma and testicular cancer and what class is this drug in?
Ifosfamide–nitrogen mustard
Name the side effects that can occur with the Nitrogen mustard alkylating agents Cyclophosphamide and Ifosfamide…
Hemorrhagic cystitis–treat with hydration and MESNA
N/V
Myelosuppression
What are the two alkylating agents used in the treatment of brain cancer and what class are these in?
Carmustine and Lomustine–Nitrosoureas
What are the side effect of the nitrosoureas alkylating agents Carmustine and Lomustine?
CNS toxicity
Profound myelosuppression
Severe N/V
Pulmonary fibrosis
What are the 3 triazene alkylating agents?
Dacrabazine
Procarbazine
Temozolomide
Which triazene alkylating agent produces free radicals?
Procarbazine
Which triazene alkylating agent is activated by liver cytochromes?
Dacarbazine