Anticancer Flashcards
What are the classes of chemotherapy drugs?
antimetabolites alkylating agents plants alkaloids antibiotics hormones immunotherapy miscellaneous
Antimetabolites
target S phase of the cell cycle by interfering with replication
SE: bone marrow suppression
What are the types of antimetabolites?
folate antagonists
pyrimidine analogs
purine analogs
Methotrexate
pemetrexed
pralatrexate
inhibit DHF reductase
decrease T, A, G
What are the side effects of antifolate dx?
BMS, diarrhea, N+V
pneumonitis , hepatic fibrosis
puritic rash
NSAID, penicillin toxicity
What treats antifolate toxicity?
leucovorin
What are the pyramid analogs
5 flurouracil
capecitabine
cytarabine
gemcitabine
5 fluoruacil & capecitabine
inhibit thymidylate synthase
What are the side effects of 5 fluoruacil & capecitabine
BMS, N+V. diarrhea
hand foot syndrome
neurotoxicity
Cytarabine (ARa-C)
inhibit DNA polymerase after phosphorylation and incorporation in DNA
What are the side effects of Cytarabine (ARa-C)
BMS, N+V, diarrhea
neurotoxicity
heaptotoxicity
Gemcitabine
inhibit DNA polymerase
inhibit ribonucleotide reductase
What are the side effects of Gemcitabine
BMS , N+V, diarrhea, mucosistis
interstitial pneumonitis
progressive HUS
Pruine analogs
mecaptopurine
6- thiofuanine
mecaptopurine
6- thiofuanine
activated by HGPRTase to monphosphate
inhibit PRPP amidotransferase
What are the side effects of mecaptopurine
6- thiofuanine
BMS, N+V, mucositis , diarrhoea
hyperpigmentation of skin
immunosuppression
Alkylating agents types
non cell cycle specific nitrogen mustards platinum analog methylhydrazine nitrosoureas
What are the nitrogen mustards?
cyclophosphamide
ifosfamide
Mechlorethamine
cyclophosphamide
ifosfamide side effects
BMS< N+V
hemorrhagic cystitis d/t acrolein
MENSA is protective
Mechlorethamine side effects?
severe N+V
BMS
What are the platinum analogs
Cisplatin
carboplatin
oxaliplatin
Cisplatin
carboplatin
oxaliplatin side effects
nephrotoxicity - tx amifostine severe N+V -tx ondansetron otoxicity peripheral neuropathies BMS hypersensitivity to platinum carboplatin less toxic oxaliplatin less nephrology/ototoxic
Methylhydrazine
procarbazine
procarbazine side effets
BMS
disulfram life reaction
metabolite of MAO inhibitor
Nitrosurea
carmustine
lomustine -crosses BBB
carmustine
lomustine side effects
BMS, N+V
interstitial nephritis
Vunblastine
vincristine
vinorelbine
vinca alkaloids
M phase specific - inhibit microtubules polymerization
arrest in metaphase
Side effects of Vunblastine
vincristine
vinorelbine
BMS,peripheral neuropathies
constipation, SIADH
Paclitacel
docetaxel
cabazitaxel
taxanes
m phase specific- inhibit microtubule depolymerization
arrest in prophase
What are the side effects of Paclitacel
docetaxel
cabazitaxel ?
hypersensitivity
BMS , N+V , diarrhea
peripheral neuropathies
irinotecan
toptecan
camptothecin analogs
S phase specific
inhibition of topoisomerase I
What are the side effects of irinotecan
toptecan ?
BMS, N+V
astenia
etoposide
teniposide
s phase specific
inhibition of topoisomerase II
What are the side effects of etoposide
teniposide ?
BMS, N+V
hypersensitivity
hypotension
Antinomycin D
antibiotics used in cancer
inhibit RNA polymerase - between G-C base pairs
What are the side effect of antinomycin D?
BMS. N+V, diarrhea
hyperpigmentaiton
hepatotoxic
Daunorubicin
doxorubicin
epirubicin
idarubicin
intercalate in DNA
free radical formation
block topoisomerase II
What are the side effects of Daunorubicin
doxorubicin
epirubicin
idarubicin ?
BMS, N+V\red orange urine
dose dependent cardio toxicity
cardiomyopathy
Tx: Dexrazoxane
Bleomycin
G2 phase specific
antibiotic used in cancer
binds to iron , forms free radicals –> strand scission
What are the side effects of bleomycin?
pulmonary fibrosis
skin reaction
hypersensitivity
Tamoxifen
toremifene
competitive inhibitor of estradiol binding to ER in breast tissue
What are the side effects of Tamoxifen
toremifene
hot flashes vaginal mucosal atrophy vaginal bleeding endometrial hyperplasia slow development of osteoporosis lowers total cholesterol , LDL
fulvestrant
SERDs
pure ER antagonist
prevent dimerization
enhances degradation of receptor
What are the side effects of fulvestrant?
nausea, headache
hot flashes
Anastrozole
letrozole
exemestane
aromatase inhibitors
bind to heme of CYP19 aromatase
competitive & irreversible inhibition
What are the side effects of Anastrozole
letrozole
exemestane ?
hot flashes
hypercholesterolemia
osteoporosis
joint muscle pain
Leuprolide
goserelin
triptorelin
GnRH analogs
initial surge in LH, FSH
increase testosterone
degarelix
GnRH antagonist
no surge in Lh, FSH
Flutamide
nilutamide
bicalutamide
enzalutamide
competitive androgen receptor antagonist
What are the side effects to anti androgen therapy ?
hot flashes decreased libido erectile dysfunction gynecomastia osteoperosis
Rituximab
MOA: CD20 , sensitizes B cell to chemotherapy
used: NHL. CLL , weaner granulomatosis, microscopic polyangitis
Alemtuzumab
MOA: CD52, PMNs & lymphocyte
SE: meylo /immuno suppression
used :CLL
Trastuzumab
MOA: Erb2 / Her 2/neu , elf receptor
used :metastatic erb2 breast cancer, erb2 gastric or gastroesophageal adenocarcinoma
Cetuximab
MOA: erb1/ Her1/neu , elf receptor
USED: EGFR metatstatic colorectal cancer
Bevacizumab
MOA: VEGF
SE: hypertensioin , proteinuria,
GI perforation and hemorrhage
USED: metastatic colorectal cacer, non small cell lung cancer, erb2 - breast cancer
metastatic renal cell carcinoma
glioblastoma
Imatinib
TKIs
target: bar-abl, c-kit, PDGFR
used: CML, gastrointestinal stroma tuner, hypereosinophillc syndrome
Getinib
Erlotinib
TKIs
target: erbB1
used : non small cell lung cancer , pancreatic cancer
sorafenib
TKIs
target: multiple tyrosine kinases
used: RCC, HCC, thyroid cancer
Sunitibib
TKIs
target: multiple TK receptors
used: metastatic RCC, GISTs, pancreatic neuroendocrine tumors
Rapamycin
mTOR inhibitor
decreases cell growth, proliferation and motility
used in transplant rejection
L-Asparaginase
hydrolysis to aspartate and ammonia decrease asparagine for tumor survival
What is the side effect of L-asparginase
decreased protein synthesis , hyperglycaemia, pancreatitis , hemorrhagic events
ATRA
all trans retinoid acid
cause differentiation of promyelocytes
Retinoid acid syndrome
fever, dyspnea, weight gain
pulmonary , pleural, pericarditis
mental confusion , death
Inflicimab
inhibit tumor necrosis factor-alpha
Rituximab
inhibit CD20 - b cell lymphomas
Cyclosporine
decrease T lymphocytes
SE: nephrotoxicity
neuropathy
gingival hyperplasia
