Beruflich Dokumente
Kultur Dokumente
(1-2-13)
You are responsible for the mechanisms and side effects of single drugs. The bolded ones are the most important exemplars of each class.
Brand name
Toxicities / Special considerations Common alkylator; causes intra-strand and interstrand cross-links between DNA bases. Common alkylator :myelosuppression including thrombocytopenia, anemia, granulocytopenia, alopecia, gonadal dysfunction, mucositis (= irritation of gut lining), second neoplasms, and pulmonary fibrosis. Toxicity:heme>>>>renal/neuro ; dose by AUC Common alkylator; cross blood brain barrier Common alkylator; oral bioavailability Toxicity:renal>neuro / oto>heme Attenuate renal toxicity by hydration Common alkylator; Prodrug: active alkylator produced as a result of hepatic metabolism; metabolites bladder toxic therefore high doses use MESNA for bladder protection; High doses: cardiac toxicity Used in curative regimens for non-Hodgkins lymphoma CHOP: Cyclophosphamide + doxorubicin + vincristine + prednisone CVP: Cyclophosphamide + vincristine + prednisone Common alkylator; very emetogenic Similar to cyclophosphamide in mechanism but more favorable activity in certain disease types e.g. sarcoma. REQUIRE bladder protection with MESNA at all doses. Encephalopathic especially with renal compromise. Fanconi syndrome, azotemia also common Common alkylator; oral bioavailable; cross blood brain barrier
RIBOMUSTIN; TREANDA
Busulfan
BUSULFEX, MYLERAN
Carboplatin
Carmustine Chlorambucil
Cisplatin
Cyclophosphamide
CYTOXAN
Dacarbazine
DTIC
Ifosfamide
IFEX, MITOXANA
Lomustine (CCNU)
1
The particular brand name does not suggest or recommend use of any drug; it is only provided to give an appreciation of common brand names Common alkylator toxicities: myelosuppression including thrombocytopenia, anemia, granulocytopenia, alopecia, gonadal dysfunction, mucositis (= irritation of gut lining), second neoplasms, and pulmonary fibrosis.
Common alkylator; oral bioavailable Parent drug of the class; common alkylator toxicity; vesicant; emetogenic Toxicity: neuro>>heme>>>>>renal Common alkylator; neurotoxic with altered mood, somnolence Common alkylator; oral bioavailability; cross blood brain barrier
Antibiotics
Bleomycin
BLEOCIN, BLENOXANE
Dactinomycin
COSMEGEN
Renal clearance therefore reduce dose in renal compromise; dose related pulmonary toxicity; late recall on exposure to high PO2 or with radiation; Raynauds hypersensitivity therefore precede with test dose Curative regimens ABVD (Adriamycin + bleomycin + vinblastine + dacarbazine) for Hodgkins and PEB (Cisplatin + etoposide + bleomycin) for germ cell neoplasms Myelosuppression; Nausea / vomiting; Mucositis; Diarrhea; Vesicant-avoid extravasation; Radiation recall Curative pediatric neoplasm regimens
Topo II Inhibitors
Daunorubucin Doxorubicin or
hydroxy-daunorubicin Epirubicin Etoposide Mitoxantrone Idarubicin
Common anthracycline toxicities: myelosuppression; vesicant; mucositis; gastrointestinal (nausea; diarrhea) dose related cardiac toxicity; interaction with radiation therapy Common anthracycline but more mucositis on a dose per dose basis than dauno Common anthracyclinetoxicities Myelosuppression, alopecia Related to anthracyclines but somewhat less cardiotoxic; also myelosuppression, mucositis, gastrointestinal Common anthracycline but less cardiotoxic on a weight basis
Antibodies (mAbs)
Alemtuzumab
CAMPATH
Ipilimumab
YERVOY
Anti CD52; use in CLL, T cell leukemias; infusion reaction (chills, fever, shortness of breath +/hypotension) tumor lysis syndrome Anti Vascular Endothelial Growth Factor; bleeding, clotting, hypertension, proteinuria, seizures / altered mental status, perforated viscus Anti EGF receptor; diarrhea, rash Anti CD20; use in B cell lymphomas; Infusion reaction (chills fever, shortness of breath +/- hypotension) Anti-erbB2; Infusion reaction (chills, fever, shortness of breath +/- hypotension); cardiac toxicity Anti-CTLA4; stimulate immunity; infusion reactions (chills, fever, shortness of breath +/- hypotension); exaggerated autoimmunity esp hepatic and gut dysfunction
Antimetabolites
Decitabine, Azacitidine
Cytarabine(cytosine
arabinoside) Fludarabine
Fluorouracil Gemcitabine
Mercaptopurine
Methotrexate
TREXALL
Pentostatin
NIPENT
Nucleosides: Myelosuppression and hypomethylate DNA at low doses Nucleoside: Myelosuppression, nausea, rash, mucositis, ocular irritation and cerebellar toxicity other CNS at high doses Nucleoside: Myelosuppression, CNS and neuro; immunosuppression and rare hemolytic anemia Pyrimidine analog: Myelosuppression, mucositis, CNS at high doses Nucleoside: Myelosuppression; hand-foot syndrome Purine analog: Myelosuppression, nausea, uncommon hepatic Antifolate: Mucositis, myelosuppression; renal clearance therefore enhanced toxicity at increased Cr; renotoxic by direct effect on tubules and by precipitation at high doses; inhibit dihydrofolate reductase therefore rescue with reduced folates especially leucovorin Adenosine deaminase inhibitor therefore increase dATP pools and inhibit production of other dNTPs and
Pemetrexed
ALIMTA
induce apoptosis in T lymphocyte lineage; renal, CNS toxicity Antifolate but also target additional enzymes of purine and pyrimidine synthesis; give with low doses of B12 and folate
Anti-microtubular
Docetaxel Ixabepilone
Myelosuppression; neuropathy; vascularleak syndrome = fluidretention Myelosuppression, neuropathy Myelosuppression, neuropathy; vascularleak syndrome = fluidretention Myelosuppression, neuropathy Neuropathy>myelotoxicity Myelosuppression; neuropathy
Growth/CS factors
Erythropoietin (epoetin)
Filgrastim (r-metHuG-CSF) G-CSF or GM-CSF Sargramostim (rHuGMCSF)
Clotting if to Hgb> 10 ?promote tumor growth Fever, chills, bone pain ; exacerbation of inflammatory states Somewhat higher incidence of fever
HDAC Inhibitor
Romidepsin
Vorinostat
ISTODAX ZOLINZA
Hormonal oncologics
Anastrazole
Bicalutamide Diethylstilbestrol (DES) Exemestane Flutamide Fulvestrant
ARIMIDEX CASODEX
Aromatase inhibitor: Bone loss; fatigue Androgen receptor antagonist; Bone loss Estrogen receptor antagonist: Bone loss; thromboses Aromatase inhibitor: Bone loss; fatigue Androgen receptor antagonist: nausea Indirect estrogen receptor antagonist; Bone loss Hypothalamic stimulator of continuous LH release therefore lose normal pulsatile release and effectively decrease net LH release Aromatase antagonist: bone loss, musculoskeletal fatigue LikeGoserelin Progesterone-related side effects : fluid retention, constipation
AROMASIN EULEXIN FASLODEX ZOLADEX (LHRH analog) FEMARA (LHRH analog) LUPRON MEGACE ANDROID NILANDRON (in CHOP and CVP)
Goserelin Letrozole
Leuprolide Megestrol Methyltestosterone Nilutamide
Prednisone Tamoxifen
NOLVADEX
Glucocorticoid excess: hyperglycemia, fluid retention gastric irritation Cushings syndrome, increased opportunistic infections; myopathy; CNS changes Bone loss, thrombogenic with deep venous and large organ thromboses; uterine neoplasms as partial agonist in uterus
Topoisomerase-I inhibitors
Irinotecan
Topotecan
CAMPTOSAR HYCAMTIN
Myelosuppression, nausea, diarrhea (acute diarrhea treat with anti-cholinergic; late diarrhea with loperamide); Dose according to UGT allele status Myelosuppression, nausea
Crizotinib Dasatinib
Erlotinib
Gefitinib
Imatinib
Anti-ALK (anaplastic lymphoma kinase)/c-MET/HGFR; nausea, vomiting, or diarrhea Targets include BCR/ABL, Srd, c-Kit, ephrin receptors, other TKs, but not EGFR or Her2 Anti EGF-R ; diarrhea, rash Anti EGF-R : diarrhea, rash Anti bcr-abl: fluid retention, hepatic,
Nilotinib
TASIGNA NEXAVAR
Sorafenib Sunitinib
Boustinib Ponatinib Vemurafenib Other oncologics Bortezomib
myelosuppression; rare cardiac Inhibits the kinases (BCR-ABL, KIT, LCK, EPHA3, EPHA8, DDR1, DDR2, PDGFRB, MAPK11 and ZAK Multi-target with prominent Anti raf, VEGF-R: rash, diarrhea, hypertension, rare hepatic; clotting / bleeding proteinuria ALSO: hand-foot syndrome Multi-target with prominent Anti VEGF-R: rash, diarrhea, hypertension, rare hepatic; clotting / bleeding proteinuria Recurrent CML CML with T315I mutation B-RAF mutated melanoma Thrombocytopenia, neuropathy Myelosuppression, mucositis Immune modulator for myeloma, myelodysplasia Cytopenias, thrombosis, edema Immune modulator for myeloma, Cytopenias, thrombosis, edema
Hydroxyurea
Lenalidomide Thalidomide
Leucovorin
Aprepitant Dexamethasone(steroid) Dolasetron Granisetron Ondansetron Palonosetron (LA)
ISOVORIN ; SODIOFOLIN
EMEND DECADRON ANZEMET KYTRIL ZOFRAN ALOXI Cushings syndrome; can also be used as an oncologic therapeutic
Additional hematologic
Unique use in acute promyelocytic leukemia: Prolonged QT syndrome, hepatic, renal Fever, infusion reactions with hypotension and vascular leak syndrome Fever Unique use in acute promyelocytic leukemia;
You are responsible for the mechanisms and side effects of single drugs. The bolded ones in the second list are the most important exemplars of each class.
ALPHABETICAL LIST
INTRON-A CAMPATH AGRYLIN ARIMIDEX EMEND (see Cytarabine) VIDAZA RIBOMUSTIN; TREANDA AVASTATIN, AVASTIN (see carmustine) CASODEX BLEOCIN; BLENOXANE VELCADE MYLERAN PARAPLATIN BCNU ERBITUX LEUKERAN Cyclophosphamide, hydroxy(doxo)rubicin, ONCOVIN (vincristine), prednisone PLATINOL ACCUTANE XALKORI Cyclophosphamide, vincristine, prednisone CYTOXAN ARABINOSIDE C, ARA-C DTIC
Additional hematologic Antibiotics Additional hematologic Hormonal Oncologics Anti-emetic therapy Antimetabolites Alkylating agents Antibodies (mAbs) (VEGF) Hormonal Oncologics Antibiotics-oncologics Proteasome inhibitor Alkylating agents Alkylating agents Alkylating agents Antibodies (mAbs) Alkylating agents
Anastrazole
Aprepitant ARA-C Azacitidine Bendamustine
Bevacuzimab
BCNU Bicalutamide
Carboplatin
Carmustine
Cetuximab
Chlorambucil CHOP
Alkylating agents Additional hematologic Anti-ALK (anaplastic lymphoma kinase Alkylating agents Antimetabolites Alkylating agents
Dactinomycin Dasatinib
COSMEGEN SPRYCEL CERUBIDINE; DAUNOMYCIN; RUBIDOMYCIN DACOGEN DECADRON TAXOTERE ANZEMET ADRIAMYCIN; DOXIL ELLENCE TARCEVA EPOGEN; PROCRIT EMCYT AROMASIN NEUPOGEN FLUDARA ADRUCIL EULEXIN FASLODEX LEUKINE (see Sargramostim) IRESSA GEMZAR ZOLADEX KYTRIL HYDREA IFEX; MITOXANA
Daunorubucin
Decitabine Dexamethasone (steroid) Diethylstilbestrol (DES) Docetaxel Dolasetron
Antibiotics-oncologics Tyrosine kinase inhibitor, but NOT EGFR or Her2 Antibiotics-oncologics, Topo II Inhibitors Antimetabolites Anti-emetic therapy Hormonal Antitubulin Anti-emetic therapy Antibiotics-oncologics, Topo II Inhibitors Antibiotics-oncologics Tyrosine kinase inhibitors(EGFR) Growth factors Hormonal Oncologics Hormonal Oncologics Growth factor Antimetabolites Antimetabolites Hormonal Oncologics Hormonal Oncologics Growth factors Tyrosine kinase inhibitors(EGFR) Antimetabolites Hormonal Oncologics (LHRH analog) Anti-emetic therapy Other oncologics Alkylating agents
Doxorubicin (hydroxydaunorubicin)
Epirubicin
Fluorouracil
Flutamide Folinic acid (see leucovorin) Fulvestrant
GCSF
Gefitinib
Gemcitabine Goserelin
Granisetron
Hydroxyurea
Ifosfamide
IL-2
Imatinib
Ixabepilone
Additional hematologic Tyrosine kinase inhibitors, BCRABLhematologic Antimicrotubular Topoisomerase I inhibitors Hormonal Oncologics Antidote to folic acid antagonists;
Mechlorethamine
Megestrol
MUSTARGEN MEGACE ALKERAN PURINETHOL TREXALL; RHEUMATREX ANDROID NOVANTRONE TASIGNA NILANDRON ZOFRAN ELOXITIN TAXOL; ONXEL (ABRAXANE ) ALOXI NIPENT (in CHOP or CVP) MUTALANE
3
Alkylating agents Hormonal Oncologics Alkylating agents Antimetabolites Antimetabolites Hormonal Oncologics Antibiotics-oncologics Tyrosine kinase inhibitors Hormonal Oncologics Anti-emetic therapy Alkylating agents Antitubulin Anti-emetic therapy Antimetabolites Adjunctive medication Alkylating agents
Melphalan
Mercaptopurine
Methotrexate
Methyltestosterone Mitoxantrone Nilotinib Nilutamide
Prednisone Procarbazine
RITUXAN ISODAX LEUKINE NEXAVAR SUTENT NOLVADEX HYCAMTIN FARESTON TEMODAR HERCEPTIN RETIN-A; VESANOID
Antibodies (mAbs)(CD20) HDAC Inhibitor Growth factor Tyrosine kinase inhibitors (VEGF) Tyrosine kinase inhibitors (VEGF) Hormonal Oncologics Topoisomerase I inhibitors Hormonal Oncologics Alkylating agents Antibodies (mAbs) (HER -2neu) Additional hematologic
Vinblastine Vincristine
Vinorelbine