Antineoplasics Flashcards
cyclophophamide
bischloroethylamines (nitrogen mustards); alkylating agent
PO
activated in liver and tumors (tumor selective)
Mechlorethamine
bischloroethylamines (nitrogen mustards); alkylating agent
IV
Short Half life
Most toxic
nitrosoureas
alkylating agents, similar action to bischloroethylamines
cross BBB->brain tumor tx
Procarbazine
alkylating agent Multiple cytotoxic intermediates (alkylating and free radicals) little cross resistance leukemogenic 10-15% used in MOPP for Hodgkin's lymphoma
MOPP
Mechlorethamine, (oncovin) vincristine, procarbazine, prednisone
tx Hodgkin’s lymphoma
Methotrexate
anti-metabolite
folic acid analog
DHFR inhibitor: blocks synthesis, of DNA, RNA, proteins
accumulates polyglutamates-> increased localization/toxicity
S phase specific
resistance: amplification of DHFR, DHFR mutation escape, decrease uptake, increased efflux (MRP 2/4)
Leucovorin used for “rescue”
6-mercaptopurine
anti metabolite purine antagonist fraudulent incorporation s phase specific activated by hypoxanthine guanine phosphoribosyl transferase (HGPRT) inactivated by xanthine oxidase
6-thioguanine
anti metabolite purine antagonist fraudulent incorporation s phase specific activated by hypoxanthine guanine phosphoribosyl transferase (HGPRT)
Fluorouracil (5-FU)
Anti metabolite Pyrimidine antagonist metabolized to FdUMP inhibits thymidylate synthetase (->thymineless death) also fraudulent incorperation s phase specific IV usually Synergistic effect with leucovorin
Capecitabine
anti metabolite pyrimidine antagonist PO activated selective in tumors coln and refractory breast ca
cytarabine (araC)
anti metabolite
pyrimidine analog
converted to araCTP
fraudulent incorporation halts polymeration
resistance from mutational loss of deoxycytine kinase
anthracyclines (daunorubicin, doxorubicin)
antibiotic broad spectrum intercalating agent topoisomerase II inhibitor cardiac tocixity
bleomycin
antibiotic DNA strand scission broad spectrum no myelosuppresion pulmonary toxicity anaphylactic potential in ABVD for Hodgkin's lymphoma
ABVD
Doxorubricin- anthracycline antibiotic
Bleomycin- antibiotic
vinblastine- mitotic spindle poison
dacarbazine- alkylating agent
Vinblastine
Vinca alkyloid M phase specific AE N/V, bone marrow depression (does limiting) resistance via tubulin gene mutation in ABVD for Hodgkin's lymphoma