Term
| Cyclophosphamide (Cytoxan) |
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Definition
Alkylating agent - nitrogen mustard;
Prodrug, converted into active Aldophosphamide;
Also, for immunosuppression;
SE - renal failure, urotoxicity (hemorrhagic cystitis) |
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Term
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Definition
Alkylating agent - nitrogen mustard;
SE - renal failure, urotoxicity (tx: MESNA), CNS TOXICITY |
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Term
| Mechlorethamine (Mustargen) |
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Definition
| Alkylating agent - nitrogen mustard |
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Term
|
Definition
Alkylating agent;
Oral or IV, hepatic metabolism;
SE - Addison-like, hepatic toxicity (veno-occlusive liver dz) |
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Term
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Definition
Alkylating agent - Nitrosoureas (brain tumors);
1. Alkylates O6-guanine, DNA breakage;
2. Isocyanate protein metabolite, inh DNA repair;
SE - injection site rxn, pulm fibrosis, CNS tox, hepatic tox (tx: Defibrotide) |
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Term
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Definition
| Alkylating agent - Nitrosoureas (brain tumors); |
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Term
|
Definition
Alkylating agent - aziridine;
Rapidly met to TEPA, will form interstrand DNA cross-links;
SE - neurotoxic, injection site rxn, bladder tox (if IVe) |
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Term
|
Definition
Alkylating agent - antibiotic;
Metabolically activated;
Gen free radicals;
SE - myelosuppression, injection site rxn, hemolytic anemia |
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Term
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Definition
Alkylating agent;
Intrastrand DNA links, primarily at N7-guanine;
IV only;
SE - ototoxic, nephrotoxic, N/V, progressive neuropathy,
secondary malignancy (AML) |
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Term
|
Definition
Alkylating agent;
Intrastrand DNA links, primarily at N7-guanine;
IV only;
SE - ototoxic, nephrotoxic, N/V, progressive neuropathy,
secondary malignancy (AML), myelosuppression is limiting |
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Term
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Definition
Methylating agent;
At O6-guanine, w/out Cl-;
Metabolically activated;
IV only; |
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Term
|
Definition
Methylating agent;
At O6-guanine;
Prodrug, activated in liver;
SE - weak MAO inhibitor, disulfriam-like rxns (+alcohol = malaise) |
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Term
| Methotrexate (Trexall, Rheumatrex) |
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Definition
Antimetabolite agent - DMARD;
Inhibits DHFR, thymidylate synthase;
Polyglutamaded form is active but can't leave cell;
SE - BM hemorrhage, renal tox, pneumonitis;
(Rescue w/ Leucovorin) |
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Term
|
Definition
Antimetabolite agent;
Strongly inh GART;
Tx mesothelioma |
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Term
| Fluorouracil, 5-FU (Adrucil) |
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Definition
Antimetabolite agent - pyrimidine analog;
Inh thymidylate synthase - req "triple complex," enhanced by Leucovorin;
SE - angina, myelosuppression, Hand-Foot syndrome |
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Term
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Definition
Antimetabolite agent - pyrimidine analog;
Blocks base stacking, chain elongation;
Prodrug, conv to ARA-CTP;
S phase specific;
SE - POTENT myelosuppression |
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Term
|
Definition
Antimetabolite agent - pyrimidine analog;
Locks cell division (not S phase specific);
SE - myelosuppression, FLU-LIKE syndrome, inc liver transaminases, interstitial pneumonitis |
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Term
|
Definition
Antimetabolite agent - pyrimidine analog;
Oral precursor of 5-FU;
SE - Hand-Foot syndrome is more common than with 5-FU |
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Term
| Mercaptopurine, 6-MP (Purinethol) |
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Definition
Antimetabolite agent - purine analog;
Unknown mech;
Oral;
Resistance @ HGPRT, alkaline phosphatase;
SE - myelo, inc hepatic enzymes;
Look at TPMT;
Interact w/ Allopurinol |
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Term
|
Definition
Antimetabolite agent - purine analog;
Inh adenosine deaminase;
Parenteral;
SE - myelo is dose-limiting |
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Term
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Definition
Antimetabolite agent - purine analog;
Oral prodrug met by deoxycytidine kinase to active triphosphate;
SE - myelo, lingering immunosupp |
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Term
|
Definition
Antimetabolite agent - purine analog;
Oral prodrug met by deoxycytidine kinase to active triphosphate;
SE - myelo, lingering immunosupp |
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Term
| Thioguanine, 6-TG (Tabloid) |
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Definition
Antimetabolite agent - purine analog;
Similar to 6-MP;
No allopurinol conflict |
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Term
|
Definition
"Natural product" - Vinca alkaloid;
Bind beta-tubulin, preventing polymerization, metaphase arrest;
Resistance - P-gp or binding site;
SE - neurotox, alopecia, local cellulitis |
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Term
|
Definition
"Natural product" - vinca alkaloids;
Bind beta-tubulin, preventing polymerization, metaphase arrest;
NO LEUKOPENIA;
SE - alopecia, local cellulitis, NUMBNESS AND TINGLING, LOSS OF DTR & MOTOR FUNCTION |
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Term
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Definition
"Natural product" - vinca alkaloids;
Bind beta-tubulin, preventing polymerization, metaphase arrest;
SE - leukopenia, alopecia, local cellulitis |
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Term
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Definition
"Natural product" - camptothecin analog;
Inh Topo-1, break strands;
Resistance - change in Topo-1or2;
SE - neutropenia, diarrhea, N/V, inc hepatic enzymes;
CI - Gilbert Syndrome |
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Term
|
Definition
"Natural product" - camptothecin analog;
Inh Topo-1, break strands;
Resistance - change in Topo-1or2;
SE - neutropenia, diarrhea, N/V, inc hepatic enzymes, ACH-ase INHIBITION;
CI - Gilbert Syndrome |
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Term
| Etoposide, VP-16 (Toposar) |
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Definition
"Natural product" - podophyllotoxin;
Inh Topo-II, prevents resealing of DNA breaks;
Oral;
SE - myelo, N/V |
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Term
|
Definition
"Natural product" - podophyllotoxin;
Inh Topo-II, prevents resealing of DNA breaks;
IV;
SE - myelo, N/V |
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Term
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Definition
"Natural product" - Taxanes;
Bind beta-tubulin, preventing de-polymerization, mitotic arrest;
Needs surfactant for solubility;
SE - +Cremaphor=HYPERSENSITIVITY, mylo, STOCKING GLOVE SENSORY NEUROPATHY |
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Term
|
Definition
"Natural product" - taxane;
More potent, fewer surfactant problems;
SE - neutropenia, fluid retention (tx: dexamethasone) |
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Term
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Definition
"Natural product" - anthracycline;
Inh Topo-II;
Makes free radicals, apoptosis;
SE - myelo, alopecia, extravasational necrosis, cardiotox, red urine |
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Term
| Daunorubicin (Cerubidine) |
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Definition
"Natural product" - anthracycline;
Inh Topo-II;
Makes free radicals, apoptosis;
SE - myelo, alopecia, extravasational necrosis, cardiotox, red urine |
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Term
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Definition
"Natural product" - anthracycline;
Inh Topo-II;
Makes free radicals, apoptosis;
SE - myelo, alopecia, extravasational necrosis, cardiotox (less than others), red urine |
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Term
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Definition
"Natural product" - anthracycline;
Inh Topo-II;
Makes free radicals, apoptosis;
SE - myelo, alopecia, extravasational necrosis, red urine |
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Term
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Definition
"Natural product" - anthracycline;
Inh Topo-II;
Makes free radicals, apoptosis;
SE - myelo, alopecia, extravasational necrosis, cardiotox, red urine |
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Term
| Mitoxantrone (Novantrone) |
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Definition
"Natural product" - anthracycline;
Inh Topo-II, bind cytoskeleton/
IV dosing, hepatic elim;
SE - cardiotox, blue urine |
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Term
|
Definition
"Natural product";
Complex w/ Fe, oxidative damage to deoxyribose, DNA breaks (sim result as Topo block);
SE - pulm fibrosis, dry cough, cutaneous tox (hyperpig, hyperkeratosis) |
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Term
Dactinomycin, Actinomycin-D
(Cosmegen) |
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Definition
"Natural product";
Intercalates DNA, breaks ssDNA via topo-II action;
IV;
SE - pancytopenia, anorexia, N/V, diarrhea, alopecia, extravasational necrosis, derm manifestations |
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Term
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Definition
"Natural product";
Dec protein synth;
Immunosupp;
Dec insulin, hypergly;
SE - PANCREATITIS, hypersensitivity rxn |
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Term
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Definition
Interferes with conversion of ribonucleotides by scavenging the free radical cofactor of ribonucleotide reductase;
Oral admin;
Resisted by inc reductase;
SE - desquamative interstitial pneumonitis, hematopoietic depression, GI, myelo (prophylaxis against myeloprolif dz) |
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Term
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Definition
Inc NK cells;
Inh anti-apoptosis;
Dec angiogenesis;
Prevents tumor cell adhesion;
SE - sedation, constipation, peripheral sensory neuropathy, teratogen |
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Term
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Definition
Promotes diff (maturation of WBCs) and disrupts repressive fusion gene being overexpressed in APL;
Tx - APL (a type of AML);
SE - retinoic acid syndrome, teratogen, inc liver enzymes, cheilitis, dry skin, hyperlipid |
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Term
| Glucocorticoids (dexamethasone or predinosone) |
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Definition
Anti-inflamm + immunosup;
Used in chemo;
SE - cushingoid syndrome |
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Term
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Definition
Blocks VEGF - anti-angiogenesis;
Limits growth of tumor;
SE - HTN!, CHF< pulm hemorrhage, GI perforation |
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Term
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Definition
Binds EGFR-2, HER-2/NEU;
Tx breast cancer;
SE - cardiomyopathy |
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Term
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Definition
Binds EGFR-1, HER-1;
Tx colorectal cancer |
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Term
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Definition
Binds EGFR-1, HER-1;
Tx colorectal cancer |
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Term
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Definition
Binds CD-20 - B-cell depletion;
Binds and dimerizes w/ cell surface receptors (apop);
Provides target for complement (C1q);
Provides target for macrophages);
Chemo and RA uses;
SE - lymphopenia, infusion rxn |
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Term
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Definition
Binds CD-20 - B-cell depletion;
Stable binding, effective against low lvls of CD-20 expression;
SE - neutropenia, progressive multifocal neutropenia |
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Term
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Definition
Binds CD-52 - T-cell depletion;
SE - pancytopenia |
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Term
| Ibritumomab Tiuxetan (Zevalin) |
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Definition
| Binds CD-20 - B-cell depletion; |
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Term
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Definition
Binds CD-20 - B-cell depletion;
SE - bone marrow suppression, hypothyroid |
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Term
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Definition
TK inhibitor;
Prevents EGFR-TK from phosphorylating, blocks signal transduction;
Rapid resistance via expansion of clones w/ mutated target;
SE - fatigue, rash, N/V/D, anorexia |
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Term
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Definition
TK inhibitor;
Prevents EGFR-TK from phosphorylating, blocks signal transduction;
Rapid resistance via expansion of clones w/ mutated target;
SE - fatigue, rash, N/V/D, anorexia |
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Term
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Definition
TK inhibitor;
Targets EGFR (HER-1,2);
SE - hepatotox, cardiotox |
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Term
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Definition
TK inhibitor;
Targets BCR-ABL;
Oral admin;
High lvls of resistance;
SE - cytopenia, N/V/D, edema, muscle cramps, fatigue, rash |
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Term
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Definition
TK inhibitor;
Targets BCR-ABL;
Oral admin;
SE - cytopenia, N/V/D, edema, muscle cramps, fatigue, rash |
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Term
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Definition
TK inhibitor;
Targets BCR-ABL;
Inc potency;
SE - pancytopenia, QT elong, inc serum lipase, N/V/D, edema, rash, abdominal pain |
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Term
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Definition
TK inhibitor;
Multi-inhibitor incl VEGFR, PDGFR, KIT, FLT;
SE - cardiotox, inc hepatic enzymes, lymphopenia, thrombocytopenia, graying of hair, skin discolor |
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Term
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Definition
TK inhibitor;
Multi-inhibitor incl VEGFR, PDGFR, KIT, FLT;
SE - hand-foot syn, cytopenia, diarrhea |
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Term
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Definition
TK inhibitor;
Multi-inhibitor incl VEGFR, PDGFR, KIT, FLT;
SE - inc hepatic enzymes, HTN, elong QT, hypothyroid |
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Term
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Definition
Proteosome inhibitor;
Inh UQ-proteosome path;
Prevents degradation of IkBa, activates caspases, inh binding of myeloma cell to stroma, dec angiogenesis, inh cytokine interactions;
SE - thrombocytopenia, peripheral neuropathy |
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Term
| Interferon Alfa-2a (Roferon) |
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Definition
Mimics endogenous INF - anti-viral, anti-neoplastic;
Cell cycle arrest in Go, apoptosis, inc immunologic response;
SE - neuropsychiatric, flu-like symptoms, CYP450 inhibition |
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Term
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Definition
mTOR inhibitor;
Dec synthesis of proteins needed for nutrient uptake, angiogenesis, ribosome biogenesis, cell growth and prolif; |
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Term
|
Definition
mTOR inhibitor;
Dec synthesis of proteins needed for nutrient uptake, angiogenesis, ribosome biogenesis, cell growth and prolif; |
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Term
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Definition
mTOR inhibitor;
Dec synthesis of proteins needed for nutrient uptake, angiogenesis, ribosome biogenesis, cell growth and prolif; |
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Term
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Definition
Hormone-ish;
GnRH agonist, hyperstimulation leads to desenitization and "castration";
Avoid initial flare w/ AR blocker;
SC or IM admin;
SE - sweat, dec libido, hot flashes, nausea, dec bone and muscle; |
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Term
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Definition
Hormone-ish;
GnRH agonist, hyperstimulation leads to desenitization and "castration";
Avoid initial flare w/ AR blocker;
SC or IM admin;
SE - sweat, dec libido, hot flashes, nausea, dec bone and muscle; |
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Term
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Definition
Hormone-ish - AR blocker;
Inh androgen binding, reflex inc levels of testosterone and andro's;
Oral admin;
SE - gynecomastia, vasomotor flushing, mastodynia, dec libido |
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Term
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Definition
Hormone-ish - AR blocker;
Inh androgen binding, reflex inc levels of testosterone and andro's;
Oral admin;
SE - gynecomastia, vasomotor flushing, mastodynia, dec libido |
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Term
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Definition
SERD - hormone-ish;
Completely suppresses estrogen receptor expression;
IM admin;
Resistance - inc growth factor signals;
SE - nausea, asthenia, vasodilation |
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Term
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Definition
SERM - hormone-ish;
Estrogen agonist at bone (inc density);
Estrogen antagonist at mammary's;
Dec cholesterol;
Oral admin;
SE - endometrial hypertrophy (cancer risk), thromboembolism, retinal degen |
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Term
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Definition
SERM - hormone-ish;
Estrogen agonist at bone (inc density);
Estrogen antagonist at mammary's;
Dec cholesterol;
Oral admin;
SE - endometrial hypertrophy (cancer risk), thromboembolism, retinal degen |
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Term
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Definition
AI - aromatase is inv in hormone conversion to estrone & estrodiol in periphery;
Non-steroidal - competitive inhibition;
Oral admin;
SE - arthralgia, diarrhea, nausea, hot flash |
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Term
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Definition
AI - aromatase is inv in hormone conversion to estrone & estrodiol in periphery;
Non-steroidal - competitive inhibition;
Oral admin;
SE - arthralgia, diarrhea, nausea, hot flash |
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Term
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Definition
AI - aromatase is inv in hormone conversion to estrone & estrodiol in periphery;
Steroidal - irreversible inhibition;
Oral admin;
SE - arthralgia, diarrhea, nausea, hot flash |
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Term
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Definition
Hormone-ish;
Alkylating agent that targets cells w/ estrogen receptors;
Binds microtubules - disassembly;
DNA breakage, apoptosis;
SE - N/V/D, gynecomastia, mastalgia |
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Term
|
Definition
Blocks XO;
Protective of kidney |
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Term
|
Definition
| Inc Urate Oxidase - conv of uric acid to soluble allatoin for excretion |
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Term
2-Mercaptoethanesulfonate, Mesna
(Mesnex) |
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Definition
Chemoprotectant against hemorrhagic cystitis;
Administer prior to chemo!;
Problem drugs - cyclophosphamide, ifosfamide |
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Term
|
Definition
| Tx nephrotoxic effect of cisplatin, carboplatin |
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Term
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Definition
Rescue for methotrexate;
Enhancement of 5-FU function |
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Term
|
Definition
| Dec cardiotox of Anthracyclines ("-rubicin") |
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Term
|
Definition
| Tumors - head, neck, BREAST |
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Term
|
Definition
| Tumors - BREAST, lung, pancreas, colon, esophagus, endometrium, cervix |
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