Antineoplastic Drugs Flashcards
Methotrexate MOA
-inhibition of DHF reductase
(“meat sticks chef trying to replace the folate leafs”)
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Methotroxate is useful in treating ...
-cancers
(“Cracked crab”)
-MTX with misoprostol used as abortifacient and ectopic pregnancy
(“Empty uterus backpack”)
(“baby keychain on the side”)
-invasive molar pregnancy, trophoblastic tumors and choriocarcinoma
(“Mole keychain”)
-Methotrexate treats psoriasis
(“Silver knee/elbow pads”)
-Methotrexate is first line treatment for rheumatoid arthritis or DMARD
(“Joint lantern with flame”)
-used for immunosuppressive therapy such as IBD, SLE, vasculitis, dematomyositis
(“Torn antibody latern”)
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Methotrexate Side Effects
-folate deficiency
(“Foliage falling”)
-megaloblastic anemia
(“Blasting firework lantern”)
-pancytopenia, myelosuppression
(“Falling pan of sushi:”)
-immunosuppressed have increased risk for infection
(“Cane”)
-lung fibrosis (restrictive lung dz)
(“Fibrotic lung bonsai”)
-
hepatotoxicity, monitor LFTs
(“Liver spot on apron”)
-causes baldness
(“Bald guy”)
-
mucositis
(“Guy eating hot meat stick”)
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what is the antidote for Methotroxate toxcity ?
folinic acid
(“Lucky feline”)
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5’-Fluorouracil MOA
inhibits thymidylate synthase to block thymidine production
- increase dUMP via inhibition of thymidylate synthase
(“Buildup of dumpling plates”)
(“Full guy”)
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5’-Fluorouracil Side Effects
-diarrhea
(“Stained pants”)
-photosensitivity and rash
(“Sensitive photos”)
-increases myelosuppression and infection
(“Falling pan of sushi”)
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5 -Fluorouracil Antidote
NO ANTIDOTE! MUAHAHAHAHA!!!!!!!
(“Knocked over cat”)
Hydroxyurea MOA
(“Hydro rock area”)
ribonucleotide reductase inhibitor, blocks thymidine synthesis
- ribonucleotide reductase converts UDP to deoxy-UDP
(“Crossed out OXY”) - UDP (uridine diphosphate) is precursor to pyrimidine nucleosides
(“UDP sign”)
(“inhibited wait list waitress”)
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Hydroxyurea can treat …
sickle cell anemia
-
increase HbF, protection against HbS
(“Raised baby with Hb coin”)
(“Zen sickle”)
Hydroxyurea Side Effect
myelosuppression and increased infection side effect
(“Falling pan of sushi”)
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6 Mercaptopurine MOA
(“CAPTured gypsy”)
Azathioprine is prodrug
(“AZmeralda”)
——————————————————————————–
-cytotoxic purine analog
- need HGPRT (enzyme) to activate 6-MP
(“HiGh Priest”)
-block synthesis of IMP
(“captive toppling imp”)
-inhibits DNA synthesis, blocks S phase
(“broken stair way”)
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6-Mercaptopurine can treat …
hematogenous malignancies
- ALL
(“stained glass window with crabs, antibody archers and T knights”)
-used for immunosuppressive therapies
- SLE
- grafts
- inflammations
(“torn lanterns with antibodies and bone”)
-rheumatoid arthritis, DMARD
(“bone lantern”)
-Inflammatory Bowel Disease
(“inflamed colonic lanterns”)
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6-Mercaptopurine Side Effects
-bone marrow suppression
(“nun with bone tray feeding bird”)
-immunosuppression and increased risk for infection monitor pt with CBCs
(“statue with cane”)
-pancreatitis
(“pancreas sponge”)
-hepatotoxicity or hepatitis
(“liver stain on apron”)
-allopurinol inhibits breakdown of 6 mercaptopurine and azathioprine increasing risk of toxicity
- may cause a mild rash
(“purine bead necklace”)
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Mycophenolate Mofetil MOA
(“quasimoto”)
-IMP dehydrogenase inhibitor
- decrease GMP synthesis, decreased lymphocyte production
(“knocking over GruMPy statue”)
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Mycophenolate Mofetil is used to treat …
(“Quasimoto”)
-for immunosuppressive therapy
- grafts
- SLE
- MG
- rheumatoid arthritis (DMARD)
(“swinging on lanterns”)
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Mycophenolate Mofetil Side Effects
(“Quasimoto”)
-GI effects
(“nauseated quasi-mofetil”)
-immunosuppressive side effects
(“nuns”)
-increased infection in immunosuppressed
(“cane”)
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Cladribine, Cytarabine, Gemcitabine MOA
-inhibit DNA polymerase → inhibit the S phase of the cell cycle
(“Cracked replication fork”)
(“Stone Phase”)
- cytarabine and gemcitabine are pyrimidine analogs
(“Pyrimidine shapes”) - cladribine is a purine analog
(“Purine shaped hammer”)
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Cladribine can treat …
hairy cell leukemia
(“Hairy caveman”)
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Cytarabine can treat …
only active against hematologic malignancies
(“Scratched out antibody archers and T-cell swordsman”)
- AML
- non-Hodgkin lymphoma
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Gemcitabine can treat…
(“gems inside geode”)
- active against both hematologic malignancies and
- *solid** tumors
(“Cracked crab fossil on solid rocks”)
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Cladribine, Cytarabine, Gemcitabine Side Effects
-can cause immunosuppression and increased risk of infection
(“Immunosuppressed cane”)
-can cause myelosuppression
(“Broken marrow”)
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Name the Alkylating agents
Cyclophosphamide
(“Cyclops Polyphemus”)
Busulfan
(“Beautiful sirens”)
Nitrosureas
(“Mustang”)
- Carmustine
- Lomustine
Ifosfamide
Cyclophosphamide
Busulfan
Nitroureas
MOA
alkylating agents donate an alkyl group → DNA cross-links
- cell cycle NON-specific
**Cyclophosphamide is activated by CYP450**
Cyclophosphamide can be used to treat …
treats many hematologic and solid malignancies
- leukemias and lymphomas,
- breast cancer,
- ovarian cancer
(“Torn cancer crab”)
potent immunosuppressive therapy
treatment of
- nephrotic syndrome,
- nephritic syndrome,
- vasculitis,
- autoimmune hemolytic anemia
(“Torn antibody”)
Cyclophosphamide Side Effects
can cause myelosuppression
(“Broken marrow”)
-can cause hemorrhagic cystitis
(“Red urine kid fountain”)
- co-administration of 2-mercaptoethanesulfonate (MESNA) prevents hemorrhagic cystitis
(“Protective maze surrounding red urine fountain”)
-increases risk of bladder cancer
(“Cancer crab belt buckle”)
- high grade transitional cell carcinoma
can cause hyponatremia due to SIADH
(“Inappropriately wet head”)
-cause infertility and premature menopause
(“Dried up fruit tree”)
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Busulfan can be used to treat …
(“beautiful sirens”)
useful as a conditioning agent prior to bone marrow transplantation
(“Severely depleted marrow”)
Nitrosoureas
Carmustine
Lomustine
(“Mustang Centaurs”)
Streptozotocin
(“Striped zebra centaur”)
are used to treat …
highly lipophilic →cross BBB → treat brain tumors
- glioblastoma multiform
(“Brain tree”)
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Nitrosoureas
Carmustine
Lomustine
(“Mustang Centaurs”)
Streptozotocin
(“Striped zebra centaur”)
Side Effects
can cause neurotoxicity
(“Dizzy centaur”)
- convulsions
- dizziness
- ataxia
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Busulfan Side Effects
(“Beautiful Sirens”)
-can cause lung toxicity
- acute lung injury
- interstitial fibrosis
- alveolar hemorrhage
-can cause a hyperpigmentation reaction
(“Beautiful TAN sirens”)
Name Cytotoxic Platinum analogs
- *Cis**platin
- *Carbo**platin
- *Oxali**platin
Cisplatin
Carboplatin
Oxaliplatin
MOA
bind DNA and form intrastrand and interstrand cross-links
(“Cross-linked helix necklace”)
Cisplatin
Carboplatin
Oxaliplatin
can treat …
treat various solid malignancies
- non-small cell lung cancer,
- small cell lung cancer,
- testicular cancer,
- ovarian cancer, bladder cancer
(“Crumpled crab”)
Cisplatin
Carboplatin
Oxaliplatin
Side Effects
can cause ototoxicity → especially cisplatin
- sensorineural hearing loss, tinnitus
(“Ototoxic earrings”)
can cause neurotoxicity→especially cisplatin
- peripheral neuropathy
(“Neuropathic gloves”)
can cause nephrotoxicity → especially cisplatin
- acute kidney injury
(“Nephrotoxic purse”) - amifostine (an organic thiophosphate) can prevent cisplatin-induced nephrotoxicity (“Amethyst”) → scavenges free radicals produced by cisplatin in the kidney (“Free, rare”)
-
IV saline diuresis prevents cisplatin-induced nephrotoxicity
(“saline fluids”)
-can cause acute tubular necrosis
- muddy brown casts
(“Muddy drain tube”)
-can cause immunosuppression and increased risk of
infection→especially carboplatin
(“Immunosuppresed cane”)
-can cause myelosuppression→especially carboplatin (“Depleted bone jewelry box”)
Name the Kinase Inhibitors
(“Broken nib”)
Imatinib
(“Imitating”)
Erlotinib
(“Earl Geoffrey”)
Sunitinib
(“Rising sun”)
Sorafenib
(“Soaring eagle”)
Vemurafenib
(“Venom”)
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Imatinib
(“Imitating”)
MOA
tyrosine kinase inhibitor
(“Inhibited tire swing”)
- imatinib blocks the tyrosine kinase domain of the BCR/ABL fusion protein →in CML
(“BREAKABLE”) - imatinib blocks the c-kit tyrosine kinase →in GIST (“Congress kit”)
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Imatinib can be used to treat
-treat a variety of hematologic and solid malignancies
-
chronic myeloid leukemia -CML (increased levels of mature granulocytes – eosinophils, neutrophils, basophils [[BCR/ABL]]
(“Copious pink, white, and blue granules”) - gastrointestinal stromal tumors (GIST) [[c-kit]]
(“Crab buttons on belly”)
(“Cracked crab”)
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Imatinib Side Effects
can cause fluid retention→ ankle and periorbital edema
(“Baggy pantaloons”)
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Erlotinib MOA
(“British Earl”)
Blocks the epidermal growth factor receptor (EGFR) tyrosine kinase
(“Earl Geoffrey”)
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Erlotinib
(“British Earl”)
treats solid tumors with EGFR overexpression
- e.g. non-small cell lung cancer – NSCLC
(“Big lapel with crab badge”)
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Erlotinib Side Effects
can cause a papulopustular acneiform rash
(“Spotty rash”)
can cause diarrhea
(“Muddy pantaloons”)
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Sunitinib/Sorafenib
MOA
(“Rising sun”)
(“Soaring eagle”)
inhibits the vascular endothelial growth factor receptor →VEGFR tyrosine kinase
(“Inhibiting vegetables”)
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Sunitinib and Sorafenib can treat…
cancer with VEGFR overexpression
- e.g. renal cell carcinoma
(“Flank crab buckles”)
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sunitinib and sorafenib
Side effects
can cause hyperkeratosis and skin rashes
VEGF-targeted therapies are associated with an increased risk of hemorrhage
(“Bleeding wound”)
(“Callused and sunburned”)
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Vemurafenib MOA
(“Venom”)
-blocks B-Raf kinase
(“B. Fra”)
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Vemurafenib can treat…
vemurafenib treats V600E BRAF positive malignant melanoma
(“Disseminated ink”)
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Name the Monoclonal Antibodies used in treatment of Cancer
Rituximab
(“coronation ritual”)
Cetuximab
(“tusks”)
Bevacizumab
(“Beverage lady”)
Alemtuzumab
(“Alms”)
Trastuzumab
(“Tapestry weaver”)
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Rituximab MOA
Rituximab and Cetuximab are chimeric monoclonal antibodies
(“Chimera sigil”)
binds CD20 on B-cells
(“Grabbing “XX” straps”)
rituximab depletes B cells (binds CD20)
(“Pulling down antibody archer”)
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Rituximab can be used to treat …
treats chronic lymphocytic leukemia (CLL)
(“Chronic tapestry with antibody archers and T knights”)
- rituximab treats rheumatoid arthritis
- disease modifying anti-rheumatic drug – DMARD
(“Rheumatic lantern”)
-is useful for immunosuppressive therapy
(e.g. microscopic polyangiitis, Wegener’s granulomatosis)
(“Torn antibody”)
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Rituximab Side Effects
can cause immunosuppression and increased risk of infection
(“Immunosuppressed cane”)
-may be associated with a higher risk of progressive multifocal leukoencephalopathy (PML)
(“White laurel leaves”)
-can cause an infusion reaction (e.g. headache, fever, skin rash, pruritus, dyspnea, hypotension)
(“Swollen cherub with ivy”)
-chimeric antibodies (e.g. rituximab, rarely cetuximab) can cause serum sickness e.g. fever, rash, arthralgia within 7-10 days
(“Delayed onset poisoning”)
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Cetuximab MOA
(“Tusks”)
binds the epidermal growth factor receptor (EGFR)
- EGFR is a receptor tyrosine kinase
(“Tire swing”)
(“Giraffe”)
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Cetuximab can treat …
treats solid tumors
- e.g. colorectal cancer, squamous cell carcinoma
(“Cracked crab”)
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Cetuximab Side Effects
can cause a papulopustular acneiform rash
(“Red spots”)
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Bevacizumab MOA
(“Beverage Lady”)
binds VEGF
- inhibits growth of blood vessels in tumors binds VEGF
(“Chopping vessels”)
(“Chopped vegetables”)
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Bevacizumab can treat …
treats metastatic tumors
- e.g. colorectal cancer, squamous cell carcinoma
(“Cracked crab”)
-treats wet macular degeneration
(“Wet center of retina pillow”)
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Bevacizumab Side Effects
-can cause bleeding
(“Blood spatter”)
-increases the risk for thrombotic events
(“Ice clots”)
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Alemtuzumab MOA
(“Alms”)
-binds CD52 on B and Tcells
depletes B and T cells (binds CD52)
(“Pulling down antibody archer and T knight”)
(“52 pattern”)
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Alemtuzumab can treat…
treats chronic lymphocytic leukemia (CLL)
(“Chronic tapestry with antibody archers and T knights”)
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Trastuzumab MOA
(“Tapestry weaver”)
binds epidermal growth factor receptor 2
- HER2, c-erbB2
- HER2 is a receptor tyrosine kinase
(“Tire swing”)
(“Her 2 babies”)
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Trastuzumab can treat …
treats HER2 positive breast cancer
(“Crab bra”)
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Trastuzumab can cause …
trastuzumab can cause cardiotoxicity
- e.g. decreased LVEF, heart failure
(“Unraveling heart”)
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