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Heme/Onc Exam 1 Drugs
Drugs and Treatments for Heme/Onc Exam 1
75
Medical
Professional
08/27/2011

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Term
Lytic IL-2 Fc
Definition
treatment for RCC, induces cell death, requires ICU admission due to 103F fever/HTN/causes immunocompromise
Term
sunitinib
Definition
tyrosine kinase inhibitor against VEGFR-1&2&3/PDGFR/cKit/Flt-3
Term
sorafinib
Definition
tyrosine kinase inhibitor against VEGFR2&3/PDGFR-B/FLT3/Raf-1
Term
sirolimus
Definition
inhibits mTOR
Term
vandetanib
Definition
tyrosine kinase inhibitor against VEGFR2, EGFR, and RET
Term
axitinib
Definition
tyrosine kinase inhibitor against VEGR-1&2&3/PDGFR/cKit
Term
pegaptanib
Definition
VEGF aptamer, for wet AMD
Term
ranibizumab
Definition
Fab from humanized VEGF mAb, for wet AMD
Term
bevacizumab
Definition
VEGF-A blocking antibody, for colorectal cancer/NSCLC/glioblastoma multiforme
Term
VEGF trap
Definition
IgG1 Fc with VEGFR1 subunit 2 and VEGFR2 subunit 3
Term
cetuximab
Definition
EGFR antibody
Term
Tamoxifen
Definition
estrogen receptor antagonist, converted to endoxifen by CYP2D6
Term
Trastuzumab
Definition
antibody against HER2, complement-mediated toxicity, blockade of signal transduction, cardiotoxicity
Term
imatinib mesylate (gleevac)
Definition
tyrosine kinase inhibitor for BCR-abl/c-kit/PDGFR, T315I mutation causes resistance, neutorpenia/thrombocytopenia, hepatic/renal toxicity, not during pregnancy
Term
mepolizumab
Definition
antibody against IL-5, treats hypereosinophilic syndrome
Term
Eltrombopag
Definition
oral TPO-R agonist
Term
methylene blue
Definition
reduces Fe3+ to Fe2+, treatment for methemoglobinemia
Term
O2-affinity lowering
Definition
CADET- CO2/Acid/DPG/Exercise/Temperature
Term
Anthracycline, vincas, taxanes, epidophyllotxins
Definition
drugs susceptible to increased efflux
Term
Gardasil
Definition
vaccine against HPV 6,11,16,18
Term
Sipuleucel-T
Definition
APCs taken from patient are treated with prostate-cancer associated antigen (PAP), matured with GM-CSF, returned to patient to activate Tcells, for HRPC
Term
Mechloremethane (Nitrogen Mustard)
Definition
bifunction alkylating agent, 1st antineoplastic drug, risk of extravasation injuries
Term
Cyclophosphamide (nitrogen mustard)
Definition
alkylating agent, bioactivated by liver p450 to 4-OH-cyclophosphamide, acrolein metabolite causes renal/bladder toxicity, interacts with P450 drugs
Term
Alkylating agents
Definition
covalent binding to DNA/RNA/proteins, cell-cycle nonspecific, dose-limiting based on bone marrow suppression, mutagenic/carcinogenic, resistance via DNA repair/detoxification/apoptosis
Term
acrolein
Definition
cyclphosphamide metabolite, responsible for bladder/renal toxicity
Term
mesna
Definition
neutralizes acrolein, prophylactic with cyclophosphamide
Term
Nitrosourea
Definition
alkylating agent, spontaneous activity, lipid soluble, crosses BBB
Term
Carmustine (BCNU)
Definition
difunctional alkylating agent, oral absorption and rapid degradation, cumulative myelosuppression, for brain tumors
Term
Streptozocin
Definition
monofunctional alkylating agent, uptaken by GLUT2, accumulates in liver/kidneys/pancreas, diabetogenic (destruction of B-cells), renal/liver toxicity, for pancreatic cancers
Term
cisplatin
Definition
cross-links DNA, resistance via detox/DNA repair/uptake/efflux/apoptosis, pronounced hypersensitivity/vomting, dose-limiting renal toxicity, peripheral and central neurotoxicity, hearing loss from acoustic nerve damage
Term
Antibiotics
Definition
DNA intercalation/ssDNA breaks/topoisomerase II inhibition, cell cycle non-specific, resistance via efflux/Topoisomerase II affinity and expression/DNA repair/GST detox
Term
Actinomycin D
Definition
intercalates DNA/inhibits topoisomerase II, dose-limiting myelosuppression, risk of extravasation injury, increased sensitivity to UV radiation
Term
Mitomycin
Definition
IV, bioactivated in liver, cross-links DNA/generates ROS for DNA damage, cumulative myelosuppression, kidney damage & lung fibrosis
Term
Bleomycin
Definition
intercalates DNA/forms ROS for DNA damage, metabolized by bleomycin hydrolase, dose-limiting pulmonary fibrosis, hypersensitivity/skin hyperpigmentation/lung toxicity
Term
Anthracyclines
Definition
topoisomerase II/helicase inhibitors, DNA intercalation, ROS formation
Term
Doxorubicin/daunorubicin
Definition
anthracyclines, dose-limiting myelosuppression, cardiac toxicity/EKG changes, <400mg/m2 cumulative lifetime dose, RECORD ALL DOSING, risk of extravasation injury
Term
Antimetabolites
Definition
interfere with DNA/RNA synthesis and protein synthesis, S-phase selective, actively transported into cells
Term
Methotrexate (MTX)
Definition
inhibits dihydrofolate reductase, prevents tetrahydrofolate formation, dose-limiting myelosuppression, renal toxicity at high doses, liver toxicity at chronic use, rescued with folinic acid
Term
5-fluoruracil (5FU)
Definition
false nucleotides (5-UTP) incorporated into DNA/RNA pyrimidines, inhibits thymidylate synthase, enhanced by folinic acid, fatal reaction with dihydropyrimidine dehydrogenase deficiency
Term
capecitabine
Definition
oral 5-FU prodrug
Term
folinic acid
Definition
circumvents folic acid pathway, rescues normal cells after methotrexate, enhances 5-FU activity
Term
6-mercaptopurine
Definition
purine analogue converted by HGPRTase, triphosphate form incorporated into DNA for damage, monophosphate form inhibits purine synthesis, TPMT catalyzes 5-methylation (deficiency causes adverse effects), reduced clearance with allopurinol
Term
allopurinol
Definition
inhibits xanthine oxidase, reduces 6-mercaptopurine clearance
Term
plant alkaloids
Definition
resistance via efflux/protein mutation
Term
Vinca alkaloids
Definition
depolymerization of microtubules, block cells in G2/M phases, resistance via tubulin synthesis/efflux, fatal if given intrathecal, risk of extravasation injury
Term
vincristine
Definition
increased neurotoxicity, decreased myelosupression, neurotoxicity-limiting
Term
vinblastine
Definition
increased myelosuppression, decreased neurotoxicity, myelosuppression-limiting
Term
Paclitaxel & docetaxel
Definition
stabilize microtubules, block G2-M transition, peripheral neuropathy
Term
dexamethason, prednisone, prednisolone (gluocorticoids)
Definition
induce apoptosis in lymphocytes, anti-inflammatory to prevent immune cell proliferation, orally available, supportive during during chemo to protect against anthracycline cardiac toxicity, adrenal atrophy, impaired wound healing, systemic infections, HTN/fluid & Na+ retention/edema/CHF, don't use in Cushing's Syndrome/CHF/HTN/diabetes/osteoporosis
Term
irinotecan
Definition
activated in liver to SN-38, inhibits topoisomerase I/ssDNA unwinding/DNA breaks, inactivated by glucuronide, decreased metabolism in Glibert's Disease
Term
etoposide, teniposide (epipodophyllotoxins)
Definition
inhibit topoisomerase II, S/G2 phase specific, resistance via efflux, myelosuppression
Term
cetuximab, panitumumab
Definition
EGFR antibodies, IgG1 humanized (cetuximab), IgG2 fully human (panitumumab), binds HER1, for patients with non-mutated Kras, interstitial lung disease, skin rash worsened by sun exposure, avoid use in pregnancy
Term
retuximab
Definition
binds CD20 on Bcells, complement-mediated toxicity, moderate allergic reactions, rare cases of fatal reactions
Term
Ibritumumoab tiuxetan
Definition
binds CD20 on Bcells, IgG1 with radioisotope, first dose has indium-111 for imaging, second dose has yttrium-90 for B-radiation
Term
erlotinib, gefitinib
Definition
tyrosine kinase inhibitor of EGFR, weakness and risk of fatal bleeding
Term
Bortezomib
Definition
inhibits 26S proteasome, decreases protein degradation, disruption of cell signaling/cell cycle arrest/ apoptosis/decreased angiogenesis, decreased tumor growth/increased cytotoxic effects of radiation
Term
thalidomide, lenalidomide
Definition
direct anti-tumor activity, inhibits TNFa/IFN/IL, inhibition of VEGF/bFGF, black box warning for blood clotting, birth defects due to loss of immature blood vessels during development
Term
methotrexate, hydroxyurea, AZT, phenytoin
Definition
affect DNA sequence and cause megaloblastic anemia
Term
Hydroxyurea
Definition
increases HbF
Term
Folic acid, tansfusions, hydroxyurea, BMT
Definition
treatment for sickle cell disease
Term
Antimalarials, sulfonamides, nitrofurantoin, phenaceptin, aspirin, vitamin K
Definition
drugs that generate ROS, exacerbate G6PD
Term
rHuEPO
Definition
binds BFU-E/CFU-E to simulate maturation, for chronic renal failure/anemia of aids/surgery/autologous donation, reduces need for transfusions, limited value to 1-2 units, IV/SC, target Hct 33-36%, resistance due to inflammation or nutrient deficiency, causes HTN in renal failure (reversible with anti-HTN and decreased drug)
Term
Darbopoietin
Definition
2 more carbohydrate chains than rHuEPO, increased half-life
Term
Filgastrim
Definition
G-CSF, increases neutrophils, for autologous BMT/congenital neutropenia, mild-moderate bone pain, granulocytosis, mild-moderate splenomegaly
Term
Pegfilgastrim
Definition
G-CSF, pegylated form of filgastrim, longer half-life
Term
Sargromastim
Definition
GM-CSF, for autologous BMT/neutropenia of AIDS or chemo/stimulating myelopoiesis, more severe side-effects than G-CSF (generally not used)
Term
Oprelvekin
Definition
rhIL-11, stimulates megakaryocytopoiesis, for high-dose cancer patients
Term
Romiplostim
Definition
stimulates thrombopoietin receptor Mpl, coupled to 2 Fc fragments, increased half life, for idiopathic thrombocytopenia purpura
Term
Oral iron (iron sulfate)
Definition
Fe2+ absorbed more readily, absorbed in upper small intestine, take before meals, antacids reduce bioavailability, spread doses throughout day to not interrupt RBC production, absorption is non-linear, 200mg/day adults, 120mgx4/day deficients, increased 15-30mg/day in prevention therapy
Term
Parenteral iron (sodium ferric gluconate, iron sorbitol, iron sucrose)
Definition
anaphylactic reaction to iron dextran, for oral iron intolerance/malabsorption/supplemented TPN/conjoined EPO therapy
Term
Vitamin B12 (cyanocobalamin, hydroxocobalamin)
Definition
converts N5-methyltetrahydrofolate to tetrahydrofolate, deficiency depletes folate pools, neurological sequelae, due to insufficient digestive enzymes/insufficient IF/deficiency of transcobalamin II, IM or deep SC, oral if not deficits in absorption
Term
folic acid
Definition
RDV non-pregnant people is 400ug, >600ug/day if pregnant or bleeding, prevents neural tube defects, destoryed by cooking, hepatic modification and recirculation into gut, oral or parenteral if absorption is defective, relives megaloblastic anemia, does not relive mental deficits due to B12 deficiency
Term
folinic acid
Definition
5-formyl modification, circumvents DHFR, for congenital DHFR deficiency
Term
ondansetron & granisetron
Definition
serotonin receptor agonists, for nausea/vomiting
Term
metoclopramide
Definition
DA receptor agonist, for nausea/vomiting
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