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141 Cards in this Set
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Antimetabolites most effective Phase |
S phase |
|
Antimetabolites subclasses |
Fluorinated pyrimidines cytidine analogs purines antifolates |
|
Antmetabolites major tox |
bone marrow suppression GI: stomatitis, n/v |
|
Antimetabolites MOA |
Inhibits replication by falsely incorporating into DNA, causes death |
|
Fluorinated Pyrimidines Drugs |
5-Fu Capecitabine Floxuridine |
|
5-FU MOA |
Prevents synthesis of thymidine needed for DNA synth, Acts as a "false" base |
|
5-FU drug interactions |
It is a strong CYP2C9 inhibitor, increases concentration of warfarin |
|
5-FU Continuous infusion AE |
hand-foot syndrome diarrhea |
|
5-FU bolus AE |
neutropenia thrombocytopenia anemia |
|
Capecitabine Route |
Oral Prodrug of 5-FU |
|
Fluorinated Pyrimidines Tox |
Diarrhea Hand-Foot syndrome n/v mucositis Photosensitivity, Ocular tox |
|
Cytidine analogs drugs |
cytarabine gemcitabine azacitidine decitabine |
|
Cytarabine Route |
intrathecal, injection, liposomal |
|
cytidine analogs hypomethylating agents |
azacitidine decitabine |
|
Cytarabine MOA |
ara-CTP competitively inhibits DNA polyermerase which decreases DNA synth and repair Also inhibits replication |
|
Cytarabine liposomal formulation |
only for intrathecal administration |
|
cytarabine resistances |
decreased membrane transport decreased formation of phosphorylated derivatives increased breakdown of drug |
|
cytarabine tox |
dose dependent: n/v cerebellar tox, conjunctivitis, ataxia, seizure risk over 50yo and renal/hepatic dysfunction |
|
cytarabine intrathecal tox |
n/v arachnoiditis, dizzy, HA, dehydration Tumor Lysis syndrome |
|
gemcitabine MOA |
incorporated into DNA, inhibits DNA polymerase also inhibits ribonucleotide reductase |
|
gemcitibine intracellular concentrations |
20x higher than cytarabine |
|
gemcitibine tox |
myelosuppression: thrombocytopenia flu-like rash elevation of liver enz SEVERE: respiratory distress, pulmonary edema, hemolytic uremic syndrome |
|
Antifolates drugs |
methotrexate pemetrexed pralatrexate |
|
methotrexate routes |
oral, injection, INTREATHECAL |
|
methotrexate MOA |
binds reversibly to dihydrofolate reductase, inhibiting cell's ability to activate folate impairs cells ability to synth DNA Looks just like folic acid and leucovorin |
|
Doses of MTX when leucovorin rescue required |
over 500-1000mg/m2 |
|
MTX clearance |
depends on renal fx avoid cocominant NSAID, penicillins, PPIs, bactrim |
|
MTX tox |
HYDRATION IS CRUCIAL tox mitigated by lecovorin bone marrow supp, cucositis, n/v, CNS TOX renal/hep tox, tumor lysis syndrome, oppo infect |
|
pemetrexed MOA |
multi-targeted that inhibits ihymidine and purine synth |
|
pemetrexed supplements |
REQUIRES FOLIC ACID AND VB12 lower risk of tox and mortality |
|
pemetrexed pre-medication |
dexamethasone prevent rash |
|
pemetrexed CrCl required |
at least 45mL/min |
|
pemetrexed tox |
fatigue, myelosupp, stomatitis, pharyngitis, rash |
|
pemetrexed avoid concomitant |
NSAIDS 2-5 days prior to pemetrexed and 2 days following |
|
purine and purine analogs drugs |
6-mercaptopurine fludarabine cladribine clofarabine nelarabine pentostatin |
|
6-mercaptopurine MOA |
rabid metab to ribonucleotides that inhibit purine synth |
|
6-mercaptopurine tox |
myelosupp, dry skin, photosensitivity, hep tox, n/v |
|
6-mercaptopurine DDI |
allopurinol, AZA, febuxostat |
|
fludarabine MOA |
interferes with DNA polymerase causing chain termination, also inhibits transcription |
|
fludarabine tox |
myelosuppression, pulm tox, tumor lysis syndrome immunosuppression neurotox with high doses |
|
microtubule targeting agents classes |
vinca alkaloids taxanes epothilones halichondrins |
|
Vinca alkaloids drugs |
vincristine vinblastine vinorelbine |
|
vincristing routes |
injection, liposomal |
|
vinca alkaloids only route |
ONLY IV, FATAL IF GIVEN BY OTHER ROUTES Vesicants |
|
Vinca alkaloids MOA |
inhibits mitosis binds to tubulin and inhibits assembly of microtubules cells undergo apoptosis |
|
vinca alkaloids metab |
liver monitor LFTs |
|
vincristine tox |
neuropathy: can be irreversible LOW RISK MYELOSUPP constipation |
|
vincristine DDI |
major 3a4 substrate, p-gp |
|
Taxanes drugs |
paclitaxel docetaxel cabazitaxel |
|
taxanes MOA |
promote microtubule assembly, interfere with disassembly makes nonfx microtubules inhibit angiogenesis |
|
taxanes resistances |
alterations in tubulin or tubulin binding sites p-gp multidrug resistance |
|
paclitaxel tox |
myelosupp, infection, hypersensitivity rxn, periph neuropathy, myalgias, TOTAL BODY HAIR LOSS |
|
paclitaxel pre-medication |
dexamethasone, benydryl, h2 antag prevents hypersensitivity |
|
paclitaxel CI |
treatment of solid tumors in pT with neutrophil lower than 1500 |
|
docetaxel pre-medication |
dexamethasone |
|
docetaxel CI |
neutrophil count less than 1500 |
|
docetaxel tox |
myelosuppression, fluid retention, hypersensitivity, n/v/d, rash stomatitis, caution with hepatic impairment |
|
topoisomerase inhibitors classes |
anthrancene derivatives camptothecins semisynthetic podophyllotoxin derivatives |
|
anthracene derivatives drugs |
DOXORUBICIN idarubicin daunorubicin epirubicin mitoxantrone valrubicin |
|
all IV anthracene derivatives are... |
VESICANTS |
|
doxorubicin CI |
recent MI, severe arrhythmia, severe myelosupp, severe myocardial insuff |
|
doxorubicin tox |
myelosupp cardiotox 2ndary malignancy n/v, alopecia, mucositis, arrhythmias |
|
doxorubicin DDI |
major substrate of CYP2D6, 3A4 |
|
doxorubicin resistance |
P-gp altered topoisomerase 2 activity |
|
doxorubicin clinical pearls |
prior to initiation, must determine baseline heart fx with either: MUGA (multigated acquistion) ECHO (echocardiogram) LVEF more than 50 percent |
|
dexrazoxane clinical pearl |
chemoprotectant that reduces cardiotox and treats anthracycline extravasation |
|
campothecins |
ininotecan topotecan |
|
irinotecan tox |
myelosupp diarrhea n/v, alopecia, mucositis, weakness |
|
irinotecan DDI |
substrate of BCRP, 3A4, PGP, UGT1A1 |
|
irinotecan caution |
PT HOMOZYGOUS FOR UGT1A1*28 hepatic impairment |
|
semisynthetic podophyllotoxin derivatives drugs |
etoposide teniposide |
|
etoposide tox |
myelosupp, n/v, alopecia, hypotension, hypersensitivity to polysorbate 80 |
|
etoposide caution in |
renal impair: dose adj CrCl50 |
|
etoposide DDI |
substrate of pgp, 3a4, INHIBITS 2C9 |
|
etoposide capsules counseling |
must keep capsules refrigerated |
|
Alkylating agents classes |
Nitrogen mustards nitronoureas platnims triazenes "other" |
|
alkylating agents class effects |
cytotoxic mutagenic teratogenic carcinogenic myelosuppressive |
|
alkylating agents resistance |
increased activation inside cells DNA repair up decreased entry into cells lack of cell death after DNA damage |
|
nitrogen mustards drugs |
cyclophosphamide chlorambucil mechlorethamine melphalan ifosfamide dendamustine |
|
cyclophosphamide CI |
urinary outflow obstruction |
|
cyclophosphamide tox |
hemorrhagic cystitis (active metab) n/v, SIADH, alopecia cardiotox |
|
cyclophosphamide DDI |
2c9 inducer 2b6 substrate |
|
cyclophosphamide caution in |
hepatic impairment |
|
cyclophosphamide prevention of hemorrhagic cystitis |
2L of oral or IV fluid/day and/or mesna. |
|
ifosfamide CI |
urinary outflow obstruction |
|
ifosfamide tox |
HEMORRHAGIC CYSTIS CNS TOX NEPHROTOX n/v, SIADH, infertility, sterility, alopecia |
|
ifosfamide DDI |
2c9 inducer 2b6 substrate |
|
ifosfamide caution in |
renal impairment consider aurinalysis to assess for hematuria |
|
Nitrosoureas drugs |
carmustine lomustine streptozocin |
|
carmustine (BCNU) tox |
n/v, TOTAL BODY HAIR LOSS, MYELOSUPP PULM TOX |
|
platinums drugs |
cisplatin carboplatin oxaliplatin |
|
cisplatin tox |
NEPHROTOX OTOTOX HYPERSENSITIVITY n/v, k/mg waste, less myelosupp |
|
cisplatin prevent tox |
HYDRATION, aggressive antiemetics |
|
carboplatin total dose(mg) equation |
target area under the curve (AUC) x (GFR+25) |
|
carboplatin tox |
MYELOSUPP N/V HYPERSENSITIVITY |
|
triazenes drugs |
dacarbazine temozolomide |
|
temozolomide CI |
hypersensitivity to dacarbazine |
|
temozolomide tox |
myelosupp, n/v, fatigue, constipation |
|
temozolomide DDI |
VPA |
|
temozolomide clinical pearl |
readily crosses BBB |
|
temozolomide phrophylaxis |
must admin PCP prophy in pT on temozolomide and radiation |
|
Misc agents drugs |
arsenic trioxide ASPARAGINASE bexarotene BLEOMYCIN dactinomycin HYDROXYUREA |
|
asparaginase MOA |
hydrolyzes L0asparagine to ammonia inhibits protien synth apoptosis |
|
asparaginase CI |
pancreatitis, thrombosis, other hemorrhagic event with prior asparaginase tx |
|
asparaginase tox |
pancreastitis thrombosis and bleed hyperammonemia hypertriglyceridemia |
|
bleomycin MOA |
inhibits synth of DNA, binds DNA, breaks strands inhibits RNA and protien synth |
|
bleomycin tox |
PULMONARY FIBROSIS flu sx, hepatotox |
|
bleomycin clinical pearls |
obtain PFTs before use and if signs develop during tx |
|
hydroxyurea MOA |
potents inhibitor of ribonucleotide reductase halts cell cycle at G1/S phase rapid decrease WBC in acute leukemia |
|
hydroxyurea tox |
skin/nail pigmentation tumor lysis sundrome |
|
hydroxyurea caution in |
renal dysfx |
|
-tu- meaning |
tumor |
|
-ci- meaning |
cardiovascular |
|
-li- meaning |
inflammation |
|
monoclonal Abx classes |
target cell surface glycoprotiens target growth factor recpt and ligands target VEGF signal pathways immunotx |
|
Agents that target cell surface glycoprotiens |
rituximab brentuximab |
|
rituximab MOA |
targets CD20 on b-lymph mediats cell lysis |
|
rituximab tox |
HEP B reactivate PML infusion rxn |
|
rituximab pT should avoid |
live vax |
|
brentuximab vedotin MOA |
targets CD30, is internalized, releases MMAE messes with microtubules causes apoptosis |
|
brentuximab vedotin tox |
n/v/d, neuropathy, rash, infustion rxn, neutropenia |
|
Agents that target VGEF pathways |
Bevacizumab |
|
bevacizumab tox |
GI PERFORATION HEMMORRHAGE IMPAIRED WOUND HEALING HTN, proteinuria, thrombolic events |
|
bevacizumab monitoring peram |
BP with tx, proteinuria |
|
Agents that target growth factor receptors and ligands |
cetuximab (EGFR1/HER1) trastuzumab (EGFR2/HER2) |
|
cetuximab tox |
INFUSION RXN CARDIOPULMONARY ARREST hypoMg, weakness, fatigue |
|
trastuzumab tox |
CARDIOMYOPATHY INFUSION RXN, PULM TOX PREGNANCY pain, HA, nausea, cough |
|
trastuzumab verify what before tx |
HER2 status, ejection fraction |
|
Immunotherapy agents |
ipilimumab nivolumab |
|
ipilumumab tox |
fatigue, immune-mediated tox, HA, nausea |
|
immune related tox |
pneumonitis, hep, pancreatitis, arthritis, dermatitis, thyroiditis |
|
nivolumab MOA |
prevents programmed cell death by binding PD1 receptor |
|
nivolumab tox |
rash, pruritus, fatigue, n/d, immune mediated SE |
|
biologic cytokines |
interferon alfa interleukin |
|
interleukin 2 tox |
CNS CAPILLARY LEAK SYNDROME INFECTIONS |
|
BCR-ABL MOA |
halts proliferation via BCR-ABL causes apoptosis |
|
sunitinib clinical pearl |
causes hepatotox |
|
nilotinib clinical pearl |
causes QTc prolongation |
|
lapatinib clinical pearl |
causes hepatotoxicity |
|
cabozantinib clinical pearls |
GI perforation hemorrhage |
|
b b |
b |