Onc Pharm Flashcards
Cisplatin
Alkylating Agent (all stages) - cross links DNA
Acute: Nausea, Nephrotoxicity, Ototoxicity, EMETOGENIC
Delayed: IRREVERSIBLE NEUROTOXICITY
Carboplatin
Alkylating Agent (all stages) - cross links DNA
Acute: Nausea, Vomiting, Ototoxicity, Nephrotoxicity
Delayed: Myelosuppression
Oxaliplatin
Alkylating Agent (all stages)
Acute: Family, Toxicities
Delayed: Reversible Neurotoxicity
Busulfan
Alkylating Agent (all stages)
Acute: Nausea, Vomiting
Delayed: Pulmonary Fibrosis*, Myelosuppression
Cyclophosphamide
Alkylating Agent (all stages)
Acute: Nausea, Vomiting
Delayed: Hemorrhagic Cystitis*, Myelosuppression
Carmustine
Alkylating Agent (all stages) (can cross BBB)
Acute: Nausea, Vomiting
Delayed: Myelosuppression, CNS Toxicity
Procarbazine
Alkylating Agent (all stages)
Acute: Nausea, Vomiting
Delayed: Myelosuppression,
RISK OF SECONDARY MALIGNANCY
Adverse drug interactions with anti-depressants (b/c metabolites act as MAOinhibitors)
Antimetabolites
Cell Cycle Specificity
Mechanism
S-Phase Specific
Interferes with DNA synthesis
6-Mercaptopurine
Anti-Metabolite (S-Phase)
Purine Analog, Inhibits enzymes of purine synthesis
Myelosuppression*. Diarrhea
Thiopurine Methyl Transferase (TPMT) deficiency can result in severe toxicities
Cladribine
Anti-Metabolite (S-Phase)
Purine Analog, Inhibits enzymes of purine synthesis
Myelosuppression, Immunosuppression (CD4, CD8)
Cytarabine (Ara-C)
Anti-Metabolite (S-Phase)
Pyrimidine Analog (Hematologic Malignancies Only) Inhibits DNA Polymerase*
Acute: GI
Chronic: Myelosuppression (panCYtopenia)
NOTE: Ara-CTP is a major cytotoxic metabolite
5-Fluorouracil (5-FU)
Anti-Metabolite (S-Phase)
Pyrimidine Analog
FdUMP inhibits TS
FdUTP inhibits DNA synthesis
FUTP inhibits RNA processing
Catabolized by Dihydropyridine Dehydrogenase (DPD)
If DPD low in liver, TOXICITY is LIFE THREATENING
Myelosuppression, Neutotoxicity
Derm -> Hand-Foot Syndrome w/ continuous infusion
Capecitabine
Anti-Metabolite (S-Phase)
Pro/Pro Drug
Metabolites converted to 5-FU in liver
Consider DPD levels
Myelosuppression, Neutotoxicity
Derm -> Hand-Foot Syndrome w/ continuous infusion
Methotrexate
Anti-Metabolite (S-Phase)
Folic Acid Analog, Competitively inhibits DHFR and TS
Myelosuppression*
rescued by Leucovorin*
Pemetrexid
Anti-Metabolite (S-Phase)
Folic Acid Analog, Inhibits TS
Myelosuppression, Skin Rashes, Mucositis, Diarrhea, Fatigue
Gemcitabine
Anti-Metabolite (S-Phase)
Pyrimidine Analog
Inhibits DNA Poly, Blocks DNA/RNA repair, Chain Termination
Neutropenia, Hemolytic Uremic Syndrome (HUS)*
Vinca Alkaloids
Mechanism, Phase
Inhibits microtubule polymerization by binding to beta-tubulin (preventing spindle formation)
Mitotic Phase Arrest (M Phase)
Vinblastine
Vinca Alkaloid (M-Phase)
Inhibits microtubule polymerization by binding to beta-tubulin (preventing spindle formation)
Potent Vesicant (blistering agent)*
Alopecia
Myelosuppression, Nausea, Vomiting
Solid Tumors, Leukemias
Hodgkin Lymphoma
Vincristine
Vinca Alkaloid (M-Phase)
Inhibits microtubule polymerization by binding to beta-tubulin (preventing spindle formation)
Peripheral neuropathy*
Autonomic Defects* (ortho. hypotension, urinary retention)
SIADH*
Myelosuppresion
Solid Tumors, Leukemias
Non-Hodgkin Lymphoma
Taxanes
Mechanism, Phase
Enhances microtubule polymerization (cannot break down)
M Phase
Paclitaxel
Taxane (M-Phase)
Enhances microtubule polymerization (cannot break down)
Hypersensitivity* (prevented with meds that dilute drug)
Peripheral Sensory Neuropathy*
Nausea, Vomiting
Abraxane
Taxane (M-Phase)
Enhances microtubule polymerization (cannot break down)
Paclitaxel formulated with albumin carrier - decreases toxicity
NO HYPERSENSITIVITY*
Docetaxel
Taxane (M-Phase)
Enhances microtubule polymerization (cannot break down)
Hypersensitivity* (prevented with meds that dilute drug)
Peripheral Sensory Neuropathy*
Nausea, Vomiting
Ixebepilone
Epothilone B Agent (M-Phase)
Binds tubulin and stabilizes microtubules
Myelosuppresion, Hypersensitivity, Neurotoxicity
Approved for Breast Cancer
Etoposide
Epipodophylotoxin
Topoisomerase II Inhibitor (S-Phase)
Alopecia, Myelosuppresion, GI
Topotecan
Camptothecan
Topoisomerase I Inhibitor (S-Phase)
APPROVED FOR SCLC*
Alopecia, Myelosuppresion, GI
Irinotecan
Camptothecan
Topoisomerase I Inhibitor (S-Phase)
Pro-drug converted in the liver
DIARRHEA (late can be severe)
Anthracycline
(Anti-Tumor Antibiotic)
Mechanism, Toxicity
Inhibit Topoisomerase II DNA intercalation (blocks RNA and DNA) -> Breaks DNA Binds to Cell Membranes Generates Semi-Quinone Free Radicals** (CARDIOTOXICITY)
Doxorubicin
Adriomycin
Anthracycline
(Anti-Tumor Antibiotic)
Used in combination therapy (ABVD for HL)
IV Admin
CARDIOTOXICITY* (generates free radicals that intercalate with DNA, break DNA)
toxicity reduced with dexrazoxone (iron chelating)
Myelosuppression, GI
Daunorubicin
Anthracycline
Anti-Tumor Antibiotic
Idarubicin
Anthracycline
Anti-Tumor Antibiotic
Mitocantrone
Anthracycline
(Anti-Tumor Antibiotic)
BLUE SCLERA and FINGERNAILS**
Myelosuppression, GI, Alopecia
Mitomycin C
Antibiotic
Activated by reduction
All Phases
Acts on tumor cells in Hypoxic Environment*
Hemolytic Uremic Syndrome**
GI
Bleomycin
Antibiotic
Binds DNA - DS, SS Breaks
G2 Specific
Pulmonary Fibrosis
Retinoic Acid (ATRA)
Acute Promyelocytic Leukemia
t(15;17) PML-RARa
(AML, M3)
Treatment leads to cell differentiation and death
Leukocytosis
Capillary Leak Syndrome (pulm edema ,resp failure)
Renal Failure
Arsenic
Acute Promyelocytic Leukemia
t(15;17) PML-RARa
(AML, M3)
Imatinib
Tyrosine Kinase Inhibitor
“Gleevec”
BCR-ABL t(9;22) CML
Binds to catalytic cleft in ABL (tyrosine kinas)
Resistance from mutations that abrogate binding of drug
Dasatinib
Newer Tyrosine Kinase Inhibitor
Specifically to overcome imatinib resistance
Trastuzumab
“Herceptin”
HER2 (Human Epidermal Growth Factor Receptor 2)
Tras2zumab = Her2 HeartCeptin = cardiotoxicity
Trastuzumab DM1
Toxin-Conjugated Trastuzumab
Thrombocytopenia, Elevated Transaminases
Lapatinib
HER1, HER2 Competitive Inhibitor
Rash, Diarrhea