the goal is use as an advance in develop drugs that selectively target specific cancer cells.
name all the anticancer drugs
alkylating agents
antimetabolites
natural products
antitumor antibiotics
miscellaneous
hormonal
drugs under this alkylating agent _
cyclophosphamide
cisplatin
antimetabolites drugs under these are:
5-FU or fluorouracil
methotrexate
gemcitabine
6-mercaptopurine
what are the drugs under these natural products
etoposide
paclitaxel
vincristine
antitumor antibiotics drugs _
bleomycin
doxorubicin
mitomycin
miscellaneous drugs _?
imatinib
cetuximab
what are the hormonal drugs_
prednisone
tamoxifen
MOA of resistance to anticancer drugs
increased DNA repair
formation of trapping agents
changes in target enzymes
decreased activation of prodrugs
inactivation of anticancer drugs
decreased drug accumulation
exert their actions selectively on cycling cells _
cell cycle-specific drugs
cell cycle-nonspecific (CCNS) drugs
it kills tumor cells in both cycling and resting phases of the cell cycle (although cycling cells are more sensitive)
log-kill hypothesis
proposes that the magnitude of tumor cell kill by anticancer drugs is a logarithmic function
cancer treatment modalities
primary induction chemotherapy
neoadjuvant chemotherapy
adjuvant chemotherapy
it is a form of tetrahydrofolate that is accumulated more readily by normal than by neoplastic cells, bypasses the dihydrofolate reductase step in folic acid synthesis, administered for the toxicity with high doses of methotrexate.
leucovorin
it traps acrolein released from cyclophosphamide, reduces the incidence of hemorrhagic cystitis.
mercaptoethanesulfonate (mesna)
it inhibits free radical formation, affords protection against the cardiac toxicity of anthracyclines.
dexrazoxane
what drugs are under alkylating agents
nitrogen mustards
nitrosoureas
alkyl sulfonates
give examples of nitrogen mustards drugs
chlorambucil
cyclophosphamide
mechlorethamine
give examples of nitrosoureas
carmustine
lomustine
give example of alkyl sulfonates drug
busulfan
other drugs under alkylating agents are_
cisplatin
dacarbaine
procarbazine
form reactive molecular species that alkylate nucleophilic groups on DNA bases, particularly the N-7 position of guanine, leading to crosslinking of bases, abnormal base-pairing, and DNA strand breakage.
alkylating agents
what does the tumor cell resistance do to alkylating agents
increased DNA repair
decreased drug permeability
production of trapping agents (thiols)
suppress the immune system. to treat cancer of the ovaries, breast, blood and lymph system and nerves (mainly in children)
cyclophosphamide
one of the breakdown products_
acrolein
uses of cyclophosphamide
leukemia
non-Hodgkin's lymphoma
breast and ovarian cancers
neuroblastoma
give adverse effects of cyclophosphamide:
gastrointestinal distress
myelosuppression
alopecia
hemorrhagic cystitis
cardiac dysfunction
pulmonary toxicity
SIADH
this is spontaneously converts in the body to a reactive cytotoxic product
mechlorethamine
give some uses of mechlorethamine
Hodgkin's
give toxicity of mechlorethamine
gastrointestinal disease
mild hematotoxicity
neurotoxic
nephrotoxity
it less nephrotoxic than cisplatin, less likely to cause tinnitus and hearing loss, has greater myelosuppressant actions.
carboplatin
what drug is less nephrotoxic than cisplatin?
carboplatin
dose-limiting neurotoxicity
oxaliplatin
forms hydrogen peroxide, generates free radicals that cause DNA strand scission, orally active, penetrates into most tissues including the cerebrospinal fluid, hepatic elimination.
procarbazine
give one use of procarbazine
non-Hodgkin's lymphoma
toxicity of procarbazine
gastrointestinal distress
myelosuppression
alopecia
sterility
toxicity of BCNU (carmustine) and CCNU(lomustine)
myelosuppressant
gastrointestinal irritation
CNS dysfunction
vesicant
peripheral neuropathy
it is used in chronic myelogenous leukemia, causes adrenal insufficiency, pulmonary fibrosis, skin pigmentation
bulsulfan
it is the adjuncts in the management of brain tumors